TW201300378A - 用於治療、控制、減輕或改善發炎性疼痛的組合物和方法 - Google Patents
用於治療、控制、減輕或改善發炎性疼痛的組合物和方法 Download PDFInfo
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- TW201300378A TW201300378A TW101119019A TW101119019A TW201300378A TW 201300378 A TW201300378 A TW 201300378A TW 101119019 A TW101119019 A TW 101119019A TW 101119019 A TW101119019 A TW 101119019A TW 201300378 A TW201300378 A TW 201300378A
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Abstract
本發明係關於一種用於治療、控制、減輕或改善發炎性疼痛之組合物，其包含解離糖皮質激素受體促效劑(「DIGRA」)、其前藥、其醫藥可接受鹽或其醫藥可接受酯。該組合物可包含額外消炎藥，且可經調配用於局部施用、注射或植入。其可在處理手術後眼睛疼痛之方法中使用，因此降低由其他治療劑所導致不良副作用的風險。
Description
本發明係關於用於治療、控制、減輕或改善發炎性疼痛之組合物及方法。特定言之，本發明係關於包含解離糖皮質激素受體促效劑(「DIGRA」)之組合物，及用於治療、減輕或改善發炎性疼痛之方法。更特定言之，本發明係關於包含解離糖皮質激素促效劑(「DIGRA」)之組合物及用於治療、減輕或改善手術後疼痛之方法。
發炎係組織對刺激、損傷或感染之反應。發炎之症狀包括疼痛、腫脹、表面變紅，及有時候會喪失行動或功能。已熟知引起關節炎(一種慢性發炎病症)之疼痛成分。導致急性發炎之暫時性組織損傷或創傷(如，由手術過程引起)亦會產生疼痛。
由慢性或急性發炎導致之組織傷害會使內源性介體釋放至傷害感受器周圍之細胞外空間中。發炎性介體緩激肽、血清素及前列腺素E2(「PGE2」)相互作用，而激發及敏化傷害感受器神經產生疼痛感受。O.Lindhart等人，Neuroscience,Vol.118,69(2003)。
由來自受損細胞膜之二醯基甘油或磷脂之磷脂酶A2(「PLA2」)釋放花生四烯酸後，其即藉由組成性表現之環氧合酶-1(「COX-1」)或可誘導之環氧合酶-2(「COX-2」)及過氧化物酶轉化為前列腺素H2(「PGH2」)。PGH2隨後藉由PGE合成酶(「PGES」)轉化為PGE2。S.Kunori等人，Glia,
Vol.59,208(2011)。
非類固醇消炎藥(「NSAID」)係控制開刀後(或手術後)疼痛之有效止痛劑。其作用機轉包括同時抑制COX-1及COX-2同功酶。據信將COX-2之抑制作用轉換成其治療作用(即，退熱、止痛及消炎作用)，同時COX-1之抑制作用會導致胃腸不良事件、腎功能受損及一些罕見充血性心臟衰竭事件。已發展出選擇性COX-2抑制劑(coxibs)來減少非選擇性NSAID之不良副作用。已發現選擇性COX-2抑制劑係有效之止痛劑，且其中有數種可以幫助緩解關節炎病患之慢性疼痛。然而，使用某些選擇性COX-2抑制劑時仍觀察到心血管不良事件。M.G.Sciulli等人，Pharmacological Reports,Vol.57，Suppl.,66(2005)。
糖皮質激素(亦稱為「皮質類固醇」或「類固醇」)代表一定範圍之發炎性病症(包括急性發炎)之最有效臨床治療中之一者。糖皮質激素尤其抑制PLA2之表現，導致前列腺素(包括PGE2)及白三烯素下降。此外，糖皮質激素抑制COX同功酶之合成，進而抑制PGE2。如上述文獻。然而，類固醇藥物可具有威脅病患整體健康之副作用。
已知特定糖皮質激素提高眼內壓(IOP)之潛力高於其他相同類別之化合物及其他消炎藥。例如，已知潑尼松龍(prednisolone)(極強力眼部消炎藥)提高IOP之趨勢高於氟米龍(fluorometholone)(其具有中等眼部消炎活性)。亦已知與眼睛局部使用糖皮質激素相關之IOP升高的風險會隨時間提高。換言之，長期使用此等藥劑來治療或控制持久性
眼部病症會提高顯著升高IOP之風險。此外，亦已知使用皮質類固醇會隨劑量-及持續時間變化之方式提高白內障形成之風險。一旦發展為白內障，即使已終止皮質類固醇治療，仍會持續惡化。因此，不建議在眼睛中長期使用糖皮質激素。
糖皮質激素之長期投與亦會因抑制腸部吸收鈣及抑制骨骼形成而導致藥物誘導骨質疏鬆症。長期投與糖皮質激素之其他不良副作用包括由於此等藥物對身體代謝過程之作用而導致之高血壓、高血糖、高血脂(甘油三酸酯濃度提高)及高膽固醇血症(膽固醇濃度提高)。
因此，用於適度控制至長期控制或改善發炎性疼痛之現有治療選項仍有待改良。因此，仍需提供一種用於控制、減輕或改善發炎性疼痛之化合物、組合物及方法。此外，亦極需提供至少具有少數或僅低度副作用之此等化合物、組合物及方法。
一般而言，本發明提供用於控制、減輕或改善發炎性疼痛之化合物、組合物及方法。
於一態樣中，本發明之化合物及組合物使至少一種不良副作用程度低於至少包含用於治療或控制相同疾病、病況或病症之先前技藝糖皮質激素之組合物。
於另一態樣中，本發明提供用於控制、減輕或改善手術後發炎性疼痛之化合物、組合物及方法。
於另一態樣中，此等手術後發炎性疼痛係於眼部手術過
程後發生。
於另一態樣中，該手術過程係選自由屈光角膜切開術、白內障移除手術、人工晶狀體(「IOL」)植入、角膜雷射矯視手術(「LASIK」)、傳導性角膜成形術、放射狀角膜切開術，及其等組合組成之群。
於另一態樣中，該至少一種不良副作用包括或係由IOP升高或其另一不良副作用組成。
於另一態樣中，該等化合物或組合物至少包含用於控制、減輕或改善發炎性疼痛之糖皮質激素模擬劑。
於另一態樣中，用於控制、減輕或改善發炎性疼痛之化合物或組合物至少包含解離糖皮質激素受體促效劑(「DIGRA」)、其前藥、醫藥可接受鹽或其醫藥可接受酯。
於另一態樣中，本發明之組合物進一步包含另一消炎藥，其選自由非類固醇消炎藥(「NSAID」)、過氧化物酶體增殖劑活化受體(「PPAR」)配位體、抗組織胺藥、促炎細胞素之拮抗劑或抑制劑(如抗-TNF、抗介白素、抗-NF-B)、氧化氮合成酶抑制劑、過氧化物酶抑制劑、其組合及其混合物組成之群。
於另一態樣中，本發明之組合物包含局部調配物；可注射調配物或可植入調配物、系統或裝置。
於另一態樣中，本發明提供一種治療、控制、減輕或改善發炎性疼痛之方法。該方法包括將至少包含DIGRA、其前藥、其醫藥可接受鹽或其醫藥可接受酯之組合物投與需要此等治療、控制、減輕或改善之個體。於一實施例中，
該發炎性疼痛包括或由手術後疼痛組成。於另一實施例中，該發炎性疼痛包括或由眼部手術後疼痛組成。於另一實施例中，該發炎性疼痛係由眼部手術過程引起。
本發明之其他特徵及優點將藉由以下詳細論述及申請專利範圍闡明。
如本文中所使用，解離糖皮質激素受體促效劑(「DIGRA」)係可結合至糖皮質激素受體(其係多肽)且在結合時可對基因表現產生不同程度之轉抑制及轉活化之化合物。會結合多肽之化合物在本文中有時稱為配位體。
如本文中所使用，術語「前藥」意指該化合物係經過修飾之治療劑或化合物，且在標的位置會轉化(例如，經由酶觸轉化)為該治療劑或化合物。將前藥投與病患可以例如加強治療劑或化合物本身之生物利用率或降低其毒性。
如本文中所使用，術語「烷基」意指可未取代或經取代之直線型或分支鏈型飽和脂族烴單價基團。該基團可經鹵原子(F、Cl、Br或I)部分或完全取代。烷基之非限制性實例包括甲基、乙基、正丙基、1-甲基乙基(異丙基)、正丁基、正戊基、1,1-二甲基乙基(第三丁基)及類似者。其可縮寫為「Alk」。「低碳數烷基」具有1至5個碳原子。
如本文中所使用術語「烯基」意指含有至少一個碳-碳雙鍵之直線型或分支鏈型脂族烴單價基團。此術語之示例性基團為乙烯基、丙烯基、正丁烯基、異丁烯基、3-甲基丁-2-烯基、正戊烯基、庚烯基、辛烯基、癸烯基及類似者。「低
碳數烯基」具有2至5個碳原子。
如本文中所使用，術語「炔基」意指具有至少一個碳-碳參鍵之直線型或分支鏈型脂族烴單價基團。此術語之示例性基團為乙炔基、丙炔基、正丁炔基、2-丁炔基、3-甲基丁炔基、正戊炔基、庚炔基、辛炔基、癸炔基及類似者。「低碳數炔基」具有2至5個碳原子。
如本文中所使用，術語「伸烷基」意指具有指定數量碳原子之直線型或分支鏈型飽和脂族烴二價基團。此術語之示例性基團為亞甲基、伸乙基、伸丙基、伸正丁基及類似者，且在本文中之替代及同等表示法為「-(烷基)-」。「低碳數伸烷基」具有1至5個碳原子。
術語「伸烯基」意指具有指定數量之碳原子及至少一個碳-碳雙鍵之直線型或分支鏈型脂族烴二價基團。此術語之示例性基團為伸乙烯基、伸丙烯基、伸正丁烯基及類似者，且在本文中之替代及同等表示法為「-(烯基)-」。「低碳數伸烯基」具有2至5個碳原子。
術語「伸炔基」意指含有至少一個碳-碳參鍵之直線型或分支鏈型脂族烴二價基團。此術語之示例性基團為伸乙炔基、伸丙炔基、伸正丁炔基、2-伸丁炔基、3-甲基伸丁炔基、伸正戊炔基、伸庚炔基、伸辛炔基、伸癸炔基及類似者，且其替代及同等表示法為「-(炔基)-」。「低碳數伸炔基」具有2至5個碳原子。
如本文中所使用，術語「芳基」意指以5至14個碳原子組成單環(例如，苯基或伸苯基)、多重稠合環(例如，萘基或
蒽基)或多個橋聯環(例如，聯苯基)之芳族碳環單價或二價基團。除非另外說明，否則芳基環可附接在任何適宜碳原子上，以獲得穩定結構，及若經取代，則可在任何適宜碳原子上取代，以獲得穩定結構。芳基之非限制性實例包括苯基、萘基、蒽基、菲基、茚滿基、茚基、聯苯基及類似者。其可縮寫為「Ar」。
術語「雜芳基」意指穩定芳族5-至14-員單環或多環單價或二價基團，其可包含一或多個稠合或橋聯環，較佳係在環中具有獨立地選自氮、氧及硫之一至四個雜原子之5-至7-員單環或7-至10-員雙環基團，其中任何硫雜原子可視需要經氧化，及任何氮雜原子可視需要經氧化或四級化。除非另外說明，否則該雜芳環可附接在任何適宜雜原子或碳原子上，以獲得穩定結構，及若經取代，則可在任何適宜雜原子或碳源上取代，以獲得穩定結構。雜芳基之非限制性實例包括呋喃基、噻吩基、吡咯基、噁唑基、噻唑基、咪唑基、吡唑基、異噁唑基、異噻唑基、噁二唑基、三唑基、四唑基、噻二唑基、吡啶基、噠嗪基、嘧啶基、吡嗪基、三嗪基、吲哚嗪基、氮雜吲哚嗪基、吲哚基、氮雜吲哚基、二氮雜吲哚基、二氫吲哚基、二氫氮雜吲哚基、異吲哚基、氮雜異吲哚基、苯并呋喃基、呋喃并吡啶基、呋喃并嘧啶基、呋喃并吡嗪基、呋喃并噠嗪基、二氫苯并呋喃基、二氫呋喃并吡啶基、二氫呋喃并嘧啶基、苯并噻吩基、噻吩并吡啶基、噻吩并嘧啶基、噻吩并吡嗪基、噻吩并噠嗪基、二氫苯并噻吩基、二氫噻吩并吡啶基、二氫噻
吩并嘧啶基、吲唑基、氮雜吲唑基、二氮雜吲唑基、苯并咪唑基、咪唑并吡啶基、苯并噻唑基、噻唑并吡啶基、噻唑并嘧啶基、苯并噁唑基、苯并噁嗪基、苯并噁嗪酮基、噁唑并吡啶基、噁唑并嘧啶基、苯并異噁唑基、嘌呤基、色滿基、氮雜色滿基、喹嗪基、喹啉基、二氫喹啉基、四氫喹啉基、異喹啉基、二氫異喹啉基、四氫異喹啉基、噌啉基、氮雜噌啉基、酞嗪基、氮雜酞嗪基、喹唑啉基、氮雜喹唑啉基、喹喔啉基、氮雜喹喔啉基、萘啶基、二氫萘啶基、四氫萘啶基、蝶啶基、咔唑基、吖啶基、吩嗪基、吩噻嗪基及吩噁嗪基，及類似者。
術語「雜環」、「雜環基團」、「雜環基」、「雜環型」或「雜環型基團」意指穩定非芳族5-至14-員單環或多環單價或二價環，其可包含一或多個稠合或橋聯環，較佳係在至少一個環中具有分別獨立選自氮、氧及硫之一至三個雜原子之5-至7-員單環或7-至10-員雙環，其中任何硫雜原子可視需要經氧化，及任何氮雜原子可視需要經氧化或四級化。如本文中所使用，雜環基不包括雜環烷基、雜環烯基及雜環炔基。除非另外說明，否則雜環基環可附接在任何適宜雜原子或碳原子上，以獲得穩定結構，及若經取代，則可在任何適宜雜原子或雜原子上取代，以獲得穩定結構。雜環之非限制性實例包括吡咯啉基、吡咯啶基、吡唑啉基、吡唑啶基、哌啶基、嗎啉基、硫代嗎啉基、哌嗪基、四氫哌喃基、四氫硫代哌喃基、四氫呋喃基、六氫嘧啶基、六氫噠嗪基及類似者。
術語「環烷基」意指僅由碳及氫原子組成之穩定脂族飽和3-至15-員單環或多環單價基團，其可包含一或多個稠合或橋聯環，較佳係5-至7-員單環或7-至10-員雙環。除非另外說明，否則環烷基環可附接任何碳原子，以獲得穩定結構，及若經取代，則可在任何適宜碳原子上取代，以獲得穩定結構。示例性環烷基包括環丙基、環丁基、環戊基、環己基、環庚基、環辛基、環壬基、環癸基、降莰烷基、金剛烷基、四氫萘基(萘滿基)、1-十氫萘基、雙環[2.2.2]辛基、1-甲基環丙基、2-甲基環戊基、2-甲基環辛基及類似者。「低碳數環烷基」具有1至5個碳原子。
術語「環烯基」意指具有至少一個碳-碳雙鍵且僅由碳及氫原子組成之穩定脂族5-至15-員單環或多環單價基團，其可包含一或多個稠合或橋聯環，較佳係5-至7-員單環或7-至10-員雙環。除非另外說明，否則環烯基環可附接任何碳原子，以獲得穩定結構，及若經取代，則可在任何適宜碳原子上取代，以獲得穩定結構。示例性環烯基包括環戊烯基、環己烯基、環庚烯基、環辛烯基、環壬烯基、環癸烯基、降烯基、2-甲基環戊烯基、2-甲基環辛烯基及類似者。「低碳數環烯基」具有2至5個碳原子。
術語「環炔基」意指具有至少一個碳-碳參鍵且僅由碳及氫原子組成之穩定脂族8-至15-員單環或多環單價基團，其可包含一或多個稠合或橋聯環，較佳係8-至10-員單環或12-至15-員雙環。除非另外說明，否則環炔基環可附接任何碳原子，以形成穩定結構，及若經取代，則可在任何適宜碳
原子上取代，以獲得穩定結構。示例性環炔基包括環辛炔基、環壬炔基、環癸炔基、2-甲基環辛炔基及類似者。「低碳數環炔基」具有2至5個碳原子。
術語「碳環」或「碳環基」意指僅由碳及氫原子組成之穩定脂族3-至15-員單環或多環單價或二價基團，其可包含一或多個稠合或橋聯環，較佳係5-至7-員單環或7-至10-員雙環。除非另外說明，否則碳環可附接任何碳原子，以獲得穩定結構，及若經取代，則可在任何適宜碳原子上取代，以獲得穩定結構。該術語包括環烷基(包括螺環烷基)、伸環烷基、環烯基、伸環烯基、環炔基及伸環炔基及類似者。
術語「雜環烷基」、「雜環烯基」及「雜環炔基」分別意指分別在至少一個環中具有至少一個雜原子之環烷基、環烯基及環炔基。
糖皮質激素(GC)係用於治療過敏性及慢性發炎性疾病或由感染引起之發炎之最有力藥物。然而，如上所述，長期以GC治療常導致許多不良副作用，如IOP升高、糖尿病、骨質疏鬆症、高血壓、青光眼或白內障。此等副作用(如同其他生理表現)係由負責此等疾病之基因之異常表現引起。近十年來的研究已對GC所介導GC-反應性基因之表現的分子基礎進行重要探討。GC藉由結合至細胞質GC受體(GR)而產生其中大部分基因組作用。GC對GR之結合誘導GC-GR複合物轉移至細胞核，並在此處藉由正(轉活化)或負(轉抑制)調節模式調控基因轉錄。越來越多證據證明GC治療之有利及不利作用係由此兩機轉之無差異之表現程度引
起；換言之，其等在相似的有效程度下運作。雖然仍無法確定GC在慢性發炎性疾病中之最關鍵作用，但已證明GC對細胞素合成之抑制作用可能特別重要。GC透過轉抑制機轉來抑制與發炎性疾病相關之數種細胞素(包括IL-1β(介白素-1β)、IL-2、IL-3、IL-6、IL-11、TNF-α(腫瘤壞死因子-α)、GM-CSF(顆粒球巨噬細胞群落刺激因子))及將發炎性細胞吸引至發炎位置之趨化細胞素(包括IL-8、RANTES、MCP-1(單核細胞趨化蛋白-1)、MCP-3、MCP-4、MIP-1α(巨噬細胞-發炎性蛋白-1α)及嗜酸性粒細胞趨化因子(eotaxin))之轉錄作用。P.J.Barnes,Clin.Sci.,Vol.94,557-572(1998)。另一方面，有說服性證據證明GC會增強合成IBα(其係對NF-B促炎轉錄因子具有抑制作用之蛋白質)。此等促炎轉錄因子調節編碼許多發炎性蛋白質(如細胞素、發炎酶、黏著分子及發炎受體)之基因之表現。S.Wissink等人，Mol.Endocrinol,Vol.12,No.3，354-363(1998)；P.J.Barnes及M.Karin,New Engl.J.Med.,Vol.336,1066-1077(1997)。因此，GC對不同基因之轉抑制及轉活化兩種功能可對發炎抑制產生有利作用。另一方面，類固醇所誘導糖尿病及青光眼似乎係由GC對負責此等疾病之基因之轉活化作用產生。H.Schäcke等人，Pharmacol.Ther.,Vol.96,23-43(2002)。因此，雖然GC對特定基因之轉活化可產生有利作用，但相同GC對其他基因之轉活化可能產生不利副作用，如IOP升高或青光眼。因此，GC不適宜或不建議用於治療、控制、減輕或改善眼部發炎性疼痛，包括手術後眼部疼痛。
因此，極需提供對GC-反應性基因產生不同轉活化及轉抑制活性之醫藥化合物及組合物，以治療、控制、減輕或改善眼部發炎性疼痛，包括手術後眼部疼痛。
一般而言，本發明提供用於控制、減輕或改善發炎性疼痛之化合物、組合物及方法。
於一態樣中，本發明之化合物及組合物使至少一種不良副作用之程度低於至少包含用於治療或控制相同疾病、病況或病症之先前技藝糖皮質激素之組合物。
於另一態樣中，本發明提供用於控制、減輕或改善手術後發炎性疼痛之化合物、組合物及方法。
於另一態樣中，此等手術後發炎性疼痛係於眼部手術過程後發生。
於另一態樣中，該手術過程係選自由屈光角膜切開術、白內障移除手術、人工晶狀體(「IOL」)植入、角膜雷射矯視手術(「LASIK」)、傳導性角膜成形術、放射狀角膜切開術，及其等組合組成之群。
於另一態樣中，該至少一種不良副作用包括或係由IOP升高或其另一種不良副作用組成。
於另一態樣中，該等化合物或組合物至少包含用於控制、減輕或改善發炎性疼痛之糖皮質激素模擬劑。
於另一態樣中，用於控制、減輕或改善發炎性疼痛之化合物或組合物至少包含解離糖皮質激素受體促效劑(「DIGRA」)、其前藥、醫藥可接受鹽或其醫藥可接受酯。
於另一態樣中，本發明之組合物進一步包含另一種消炎
藥，其選自下列各物所組成群中：非類固醇消炎藥(「NSAID」)、過氧化物酶體增殖劑活化受體(「PPAR」)配位體、抗組織胺藥、促炎細胞素之拮抗劑或抑制劑(如抗-TNF、抗介白素、抗-NF-B)、氧化氮合成酶抑制劑、過氧化物酶抑制劑、其組合及其混合物。
於另一態樣中，本發明之組合物包含局部調配物；可注射調配物或可植入調配物、系統或裝置。
於另一態樣中，本發明提供一種治療、控制、減輕或改善發炎性疼痛之方法。該方法包括將至少包含DIGRA、其前藥、其醫藥可接受鹽或其醫藥可接受酯之組合物投與需要此等治療、控制、減輕或改善之個體。於一實施例中，該發炎性疼痛包括或由手術後疼痛組成。於另一實施例中，該發炎性疼痛包括或由眼部手術後疼痛組成。於另一實施例中，該發炎性疼痛係由眼部手術過程引起。
於另一態樣中，該等化合物或組合物至少包含糖皮質激素之模擬劑。如本文中所使用，糖皮質激素模擬劑係或包括展現或產生類似糖皮質激素之有利生理作用但結構上並非類固醇之化合物。
於另一態樣中，該等化合物或組合物至少包含解離糖皮質激素受體促效劑(「DIGRA」)。如本文中所使用，DIGRA可包含該分子之任何對映異構體或該等對映異構體之消旋混合物。
於另一態樣中，該等化合物或組合物包含至少DIGRA之前藥、醫藥可接受鹽、醫藥可接受酯。
於另一態樣中，該等化合物或組合物包含：(a)DIGRA、其前藥、其醫藥可接受鹽或其醫藥可接受酯；及(b)與該DIGRA、其前藥、其醫藥可接受鹽及其醫藥可接受酯不同之消炎藥。此等消炎藥之非限制性實例揭示於下文中。
於另一態樣中，該至少DIGRA具有式I。
於一實施例中，B可包含一或多個不飽和碳-碳鍵。
於另一實施例中，B可包括伸烷羰基、伸烷氧羰基、伸烷羰氧基、伸烷氧羰基胺基、伸烷胺基、伸烯基羰基、伸烯氧基羰基、伸烯基羰氧基、伸烯氧基羰基胺基、伸烯基胺基、伸炔基羰基、伸炔氧基羰基、伸炔基羰氧基、伸炔氧基羰基胺基、伸炔基胺基、芳基羰氧基、芳氧基羰基或脲基。
於另一實施例中，A及Q獨立地選自由經至少C1至C10烷基(或者，C1至C5烷基，或C1至C3烷基)、鹵原子、氰基、羥基或C1至C10烷氧基(或者，C1至C5烷氧基，或C1至C3烷氧基)取代之芳基及雜芳基組成之群；R1、R2及R3獨立地選自由未取代及經取代C1至C5烷基(較佳，C1至C3烷基)組成之群；B係C1至C5伸烷基(或者，C1至C3伸烷基)；D係-NH-或-NR'-基團，其中R'係C1至C5烷基(較佳，C1至C3烷基)；及E係羥基。
於另一實施例中，A包括經鹵素取代之二氫苯并呋喃基；
Q包括經C1至C10烷基取代之喹啉基或異喹啉基；R1及R2獨立地選自由未取代及經取代C1至C5烷基(較佳，C1至C3烷基)組成之群；B係C1至C3伸烷基；D係-NH-基團；E係羥基；及R3包括完全鹵化之C1至C10烷基(較佳，完全鹵化之C1至C5烷基；更佳，完全鹵化之C1至C3烷基)。
於另一實施例中，A包括經氟原子取代之二氫苯并呋喃基；Q包括經甲基取代之喹啉基或異喹啉基；R1及R2獨立地選自由未取代及經取代C1至C5烷基組成之群；B係C1至C3伸烷基；D係-NH-基團；E係羥基；及R3包括三氟甲基。
於另一實施例中，該至少DIGRA具有式II或III。
於另一實施例中，該至少DIGRA具有式IV。
用於製備如式I、II、III或IV之方法揭示於例如美國專利案6,897,224；6,903,215；6,960,581中，該等案係以引用其等全文之方式併入本文。用於製備此等化合物之其他方法亦可參見美國專利申請公告案2006/0116396，該案之內容係以引用之方式併入本文，或PCT專利申請案WO 2006/050998 A1。
如式I之化合物之非限制性實例包括5-[4-(5-氟-2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基-戊胺基]-2-甲基喹啉、5-[4-(5-氟-2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基-戊胺基]-1-甲基異喹啉、5-[4-(5-氟-2,3-二氫苯
并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基-戊胺基]異喹啉-1(2H)-酮、5-[4-(5-氟-2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基-戊胺基]-2,6-二甲基喹啉、5-[4-(5-氟-2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基-戊胺基]-6-氯-2-甲基喹啉、5-[4-(5-氟-2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基-戊胺基]異喹啉、5-[4-(5-氟-2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基-戊胺基]喹啉、5-[4-(2,3-二氫-5-氟-7-苯并呋喃基)-2-羥基-4-甲基-2-三氟甲基-戊胺基]喹啉-2[1H]-酮、6-氟-5-[4-(5-氟-2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基-戊胺基]-2-甲基喹啉、8-氟-5-[4-(5-氟-2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基-戊胺基]-2-甲基喹啉、5-[4-(5-氟-2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基-戊胺基]-2-甲基異喹啉-1-[2h]-酮、及其對映異構體。
於另一實施例中，該至少DIGRA具有式I，其中a)A係視需要獨立地經一至三個取代基取代之芳基，該等取代基獨立地選自由C1至C5烷基、C2至C5烯基、C2至C5炔基、C1至C3烷醯基、C3至C8環烷基、雜環基、芳基、雜芳基、C1至C5烷氧基、C2至C5烯氧基、C2至C5炔氧基、芳氧基、醯基、C1至C5烷氧羰基、芳醯基、胺基羰基、烷胺基羰基、二烷胺基羰基、胺基羰氧基、C1至C5烷胺基羰氧基、C1至C5二烷胺基羰氧基、C1至C5烷醯基胺基、C1至C5烷氧羰基胺基、C1至C5烷基磺醯胺基、胺基磺醯基、C1至C5烷胺基磺醯基、C1至C5二烷胺基磺醯基、鹵素、羥基、
羧基、氰基、三氟甲基、三氟甲氧基、硝基、胺基(其中氮原子視需要獨立地經C1至C5烷基或芳基單或二取代)、脲基(其中任一氮原子視需要獨立地經C1至C5烷基取代)、C1至C5烷硫基(其中硫原子視需要氧化形成亞碸或碸)組成之群；b)R1及R2各自獨立地係氫或C1至C5烷基；c)R3係三氟甲基；d)B係C1至C5烷基、C2至C5烯基或C2至C5炔基，各者視需要獨立地經一至三個取代基取代，其中B之各取代基獨立地係C1至C3烷基、羥基、鹵素、胺基或側氧基；e)D不存在；f)E係羥基；及g)Q係視需要獨立地經一至三個取代基取代之氮雜吲哚基，其中Q之各取代基獨立地係C1至C5烷基、C2至C5烯基、C2至C5炔基、C3至C8環烷基、雜環基、芳基、雜芳基、C1至C5烷氧基、C2至C5烯氧基、C2至C5炔氧基、芳氧基、醯基、C1至C5烷氧羰基、C1至C5烷醯氧基、胺基羰基、烷胺基羰基、二烷胺基羰基、胺基羰氧基、C1至C5烷胺基羰氧基、C1至C5二烷胺基羰氧基、C1至C5烷醯基胺基、C1至C5烷氧羰基胺基、C1至C5烷基磺醯胺基、胺基磺醯基、C1至C5烷胺基磺醯基、C1至C5二烷胺基磺醯基、鹵素、羥基、羧基、氰基、三氟甲基、三氟甲氧基、三氟甲硫基、硝基或胺基(其中氮原子視需要獨立地經C1至C5烷基單或二取代)、脲基(其中任一氮原子視需要獨立地經C1至C5烷基取代)、C1至C5烷硫基(其中硫原子視需要氧化以形成亞碸或
碸)，其中Q之各取代基視需要獨立地經一或三個取代基取代，該等取代基選自由C1至C3烷基、C1至C3烷氧基、鹵素、羥基、側氧基、氰基、胺基及三氟甲基組成之群。
此等化合物之非限制性實例包括1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基-2-(1H-吡咯并[2,3-c]吡啶-2-基甲基)戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基-2-(1H-吡咯并[3,2-c]吡啶-2-基甲基)戊-2-醇、1,1,1-三氟-4-甲基-4-苯基-2-(1H-吡咯并[2,3-c]吡啶-2-基甲基)戊-2-醇、1,1,1-三氟-4-(4-氟-2-甲氧基苯基)-4-甲基-2-(1H-吡咯并[2,3-c]吡啶-2-基甲基)戊-2-醇、1,1,1-三氟-4-甲基-4-苯基-2-(1H-吡咯并[3,2-c]吡啶-2-基甲基)戊-2-醇、1,1,1-三氟-4-(4-氟-2-甲氧基苯基)-4-甲基-2-(1H-吡咯并[3,2-c]吡啶-2-基甲基)戊-2-醇、5-氟-2-[4,4,4-三氟-3-羥基-1,1-二甲基-3-(1H-吡咯并[2,3-c]吡啶-2-基甲基)丁基]酚、4-氟-2-[4,4,4-三氟-3-羥基-1,1-二甲基-3-(1H-吡咯并[2,3-c]吡啶-2-基甲基)丁基]酚、1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基-2-(1H-吡咯并[3,2-c]吡啶-2-基甲基)戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基-2-(3-甲基-1H-吡咯并[2,3-c]吡啶-2-基甲基)戊-2-醇及4-氟-2-[4,4,4-三氟-3-羥基-1,1-二甲基-3-(1H-吡咯并[2,3-c]吡啶-2-基甲基)丁基]酚。
於另一實施例中，該至少DIGRA具有式I，其中a)A係各自視需要獨立地經一至三個取代基取代之芳基或雜芳基，該等取代基獨立地選自由C1至C5烷基、C2至C5烯基、C2至C5炔基、C1至C3烷醯基、C3至C8環烷基、雜環
基、芳基、雜芳基、C1至C5烷氧基、C2至C5烯氧基、C2至C5炔氧基、芳氧基、醯基、C1至C5烷氧羰基、芳醯基、胺基羰基、烷胺基羰基、二烷胺基羰基、胺基羰氧基、C1至C5烷胺基羰氧基、C1至C5二烷胺基羰氧基、C1至C5烷醯基胺基、C1至C5烷氧羰基胺基、C1至C5烷基磺醯胺基、胺基磺醯基、C1至C5烷胺基磺醯基、C1至C5二烷胺基磺醯基、鹵素、羥基、羧基、氰基、三氟甲基、三氟甲氧基、硝基、胺基(其中氮原子視需要獨立地經C1至C5烷基或芳基單或二取代)、脲基(其中任一氮原子視需要獨立地經C1至C5烷基取代)、C1至C5烷硫基(其中硫原子視需要氧化以形成亞碸或碸)組成之群；b)R1及R2各自獨立地係氫或C1至C5烷基，或R1及R2藉由其等共同連接之碳原子一起形成C3至C8螺環烷基環；c)B係亞甲基或羰基；d)R3係碳環、雜環基、芳基、雜芳基、碳環-C1至C8烷基、芳基-C1至C8烷基、芳基-C1至C8鹵烷基、雜環基-C1至C8烷基、雜芳基-C1至C8烷基、碳環-C2至C8烯基、芳基-C2至C8烯基、雜環基-C2至C8烯基或雜芳基-C2至C8烯基，各者視需要獨立地經一至三個取代基取代；e)D係-NH-基團；f)E係羥基；及g)Q包括甲基化苯并噁嗪酮。
此等化合物之非限制性實例包括2-苄基-4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基戊酸(4-甲基-1-側氧基-1H-苯并
[d][1,2]噁嗪-6-基)醯胺、2-苄基-4-(5-氟-2-羥基苯基)-2-羥基-4-甲基戊酸(4-甲基-1-側氧基-1H-苯并[d][1,2]噁嗪-6-基)醯胺、2-環己基甲基-4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基戊酸(4-甲基-1-側氧基-1H-苯并[d][1,2]噁嗪-6-基)醯胺、2-環己基甲基-4-(5-氟-2-羥基苯基)-2-羥基-4-甲基戊酸(4-甲基-1-側氧基-1H-苯并[d][1,2]噁嗪-6-基)醯胺、2-苄基-2-羥基-4-甲基-4-甲基戊酸(4-甲基-1-側氧基-1H-苯并[d][1,2]噁嗪-6-基)醯胺及2-環己基甲基-2-羥基-4-甲基戊酸(4-甲基-1-側氧基-1H-苯并[d][1,2]噁嗪-6-基)醯胺。
於另一實施例中，該至少DIGRA具有式I，其中a)A係各自視需要獨立地經一至三個取代基取代之芳基或雜芳基，該等取代基獨立地選自由C1至C5烷基、C2至C5烯基、C2至C5炔基、C1至C3烷醯基、C3至C8環烷基、雜環基、芳基、雜芳基、C1至C5烷氧基、C2至C5烯氧基、C2至C5炔氧基、芳氧基、醯基、C1至C5烷氧羰基、芳醯基、胺基羰基、烷胺基羰基、二烷胺基羰基、胺基羰氧基、C1至C5烷胺基羰氧基、C1至C5二烷胺基羰氧基、C1至C5烷醯基胺基、C1至C5烷氧羰基胺基、C1至C5烷基磺醯胺基、胺基磺醯基、C1至C5烷胺基磺醯基、C1至C5二烷胺基磺醯基、鹵素、羥基、羧基、氰基、三氟甲基、三氟甲氧基、硝基、胺基(其中氮原子視需要獨立地經C1至C5烷基或芳基單或二取代)、脲基(其中任一氮原子視需要獨立地經C1至C5烷基取代)、C1至C5烷硫基(其中硫原子視需要氧化以形成亞碸或碸)組成之群；
b)R1及R2各自獨立地係氫或C1至C5烷基，或R1及R2藉由其等共同連接之碳原子一起形成C3至C8螺環烷基環；c)R3係三氟甲基；d)B係C1至C5烷基、C2至C5烯基或C2至C5炔基，各者視需要獨立地經一至三個取代基取代，其中B之各取代基獨立地係C1至C3烷基、羥基、鹵素、胺基或側氧基；e)D不存在；f)E係羥基；及g)Q係視需要獨立地經一至三個取代基取代之芳基或雜芳基，該等取代基獨立地係選自由C1至C5烷基、C2至C5烯基、C2至C5炔基、C1至C3烷醯基、C3至C8環烷基、雜環基、芳基、雜芳基、C1至C5烷氧基、C2至C5烯氧基、C2至C5炔氧基、芳氧基、醯基、C1至C5烷氧羰基、芳醯基、胺基羰基、烷胺基羰基、二烷胺基羰基、胺基羰氧基、C1至C5烷胺基羰氧基、C1至C5二烷胺基羰氧基、C1至C5烷醯基胺基、C1至C5烷氧羰基胺基、C1至C5烷基磺醯胺基、胺基磺醯基、C1至C5烷胺基磺醯基、C1至C5二烷胺基磺醯基、鹵素、羥基、羧基、氰基、三氟甲基、三氟甲氧基、硝基、胺基(其中氮原子視需要獨立地經C1至C5烷基單或二取代)、脲基(其中任一氮原子視需要獨立地經C1至C5烷基取代)、C1至C5烷硫基(其中硫原子視需要氧化以形成亞碸或碸)組成之群，其中Q之各取代基係視需要經一至三個取代基取代，該等取代基選自由C1至C3烷基、C1至C3烷氧基、醯基、C1至C3矽烷氧基、C1至C5烷氧羰基、羧基、鹵素、羥基、側氧基、氰
基、雜芳基、雜環基、胺基(其中氮原子視需要獨立地經C1至C5烷基或芳基單或二取代)、脲基(其中任一氮原子視需要獨立地經C1至C5烷基取代)及三氟甲基組成之群。
此等化合物之非限制性實例包括2-(3,5-二氟苄基)-1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基戊-2-醇、2-聯苯-4-基甲基-1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基戊-2-醇、2-(3,5-二甲基苄基)-1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基戊-2-醇、2-(3-溴苄基)-1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基戊-2-醇、2-(3,5-二氯苄基)-1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基戊-2-醇、2-(3,5-雙-三氟甲基苄基)-1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-2-(3-氟-5-三氟甲基苄基)-4-甲基戊-2-醇、2-(3-氯-2-氟-5-三氟甲基苄基-)-1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基戊-2-醇、4-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]苯甲腈、2-(3,5-二溴苄基)-1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-2-(2-氟-3-三氟甲基苄基)-4-甲基戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-2-(2-氟-5-三氟甲基苄基)-4-甲基戊-2-醇。
於另一實施例中，該至少DIGRA具有式I，其中a)A係各自視需要獨立地經一至三個取代基取代之芳基、雜芳基或C5至C15環烷基，該等取代基獨立地選自由C1至C5烷基、C2至C5烯基、C2至C5炔基、C1至C3烷醯基、C3至C8環烷基、雜環基、芳基、雜芳基、C1至C5烷氧基、C2
至C5烯氧基、C2至C5炔氧基、芳氧基、醯基、C1至C5烷氧羰基、芳醯基、胺基羰基、烷胺基羰基、二烷胺基羰基、胺基羰氧基、C1至C5烷胺基羰氧基、C1至C5二烷胺基羰氧基、C1至C5烷醯基胺基、C1至C5烷氧羰基胺基、C1至C5烷基磺醯胺基、胺基磺醯基、C1至C5烷胺基磺醯基、C1至C5二烷胺基磺醯基、鹵素、羥基、羧基、氰基、三氟甲基、三氟甲氧基、硝基、胺基(其中氮原子視需要獨立地經C1至C5烷基或芳基單或二取代)、脲基(其中任一氮原子視需要獨立地經C1至C5烷基取代)、C1至C5烷硫基(其中硫原子視需要氧化以形成亞碸或碸)組成之群；b)R1及R2各自獨立地係氫、C1至C5烷基、C5至C15芳基烷基，或R1及R2藉由其等共同連接之碳原子一起形成C3至C8螺環烷基環；c)R3係三氟甲基；d)B係羰基或亞甲基，其視需要獨立地經一或兩個選自C1至C5烷基、羥基及鹵素之取代基取代；e)D不存在；f)E係羥基或胺基，其中氮原子視需要獨立地經C1至C5烷基單或二取代；及g)Q包括吡咯啶、嗎啉、硫代嗎啉、哌嗪、哌啶、1H-吡啶-4-酮、1H-吡啶-2-酮、1H-亞吡啶-4-基胺、1H-亞喹啉-4-基胺、哌喃、四氫哌喃、1,4-二氮雜環庚烷、2,5-二氮雜雙環[2.2.1]庚烷、2,3,4,5-四氫苯并[b][1,4]二氮呯、二氫喹啉、四氫喹啉、5,6,7,8-四氫-1H-喹啉-4-酮、四氫異喹啉、
十氫異喹啉、2,3-二氫-1H-異吲哚、2,3-二氫-1H-吲哚、色滿、1,2,3,4-四氫喹喔啉、1,2-二氫吲唑-3-酮、3,4-二氫-2H-苯并[1,4]噁嗪、4H-苯并[1,4]噻嗪、3,4-二氫-2H-苯并[1,4]噻嗪、1,2-二氫苯并[d][1,3]噁嗪-4-酮、3,4-二氫苯并[1,4]噁嗪-4-酮、3H-喹唑啉-4-酮、3,4-二氫-1H-喹喔啉-2-酮、1H-喹啉-4-酮、1H-喹唑啉-4-酮、1H-[1,5]萘啶-4-酮、5,6,7,8-四氫-1H-[1,5]萘啶-4-酮、2,3-二氫-1H-[1,5]萘啶-4-酮、1,2-二氫吡啶并[3,2-d][1,3]噁嗪-4-酮、吡咯并[3,4-c]吡啶-1,3-二酮、1,2-二氫吡咯并[3,4-c]吡啶-3-酮或四氫[b][1,4]二氮呯酮基團，各者視需要獨立地經一至三個取代基取代，其中Q之各取代基獨立地係C1至C5烷基、C2至C5烯基、C2至C5炔基、C3至C8環烷基、雜環基、芳基、雜芳基、C1至C5烷氧基、C2至C5烯氧基、C2至C5炔氧基、芳氧基、醯基、C1至C5烷氧羰基、C1至C5烷醯氧基、胺基羰基、烷胺基羰基、二烷胺基羰基、胺基羰氧基、C1至C5烷胺基羰氧基、C1至C5二烷胺基羰氧基、C1至C5烷醯基胺基、C1至C5烷氧羰基胺基、C1至C5烷基磺醯胺基、C1至C5烷胺基磺醯基、C1至C5二烷胺基磺醯基、鹵素、羥基、羧基、側氧基、氰基、三氟甲基、三氟甲氧基、三氟甲硫基、硝基、胺基(其中氮原子視需要獨立地經C1至C5烷基單或二取代)、脲基(其中任一氮原子視需要獨立地經C1至C5烷基取代)、或C1至C5烷硫基(其中硫原子視需要氧化以形成亞碸或碸)，其中Q之各取代基視需要獨立地經一至三個取代基取代，該等取代基選自C1至C3烷基、C1至C3烷氧基、C1至C3烷氧羰基、醯
基、芳基、苄基、雜芳基、雜環基、鹵素、羥基、側氧基、氰基、胺基(其中氮原子視需要獨立地經C1至C5烷基單或二取代)或脲基(其中任一氮原子視需要獨立地經C1至C5烷基取代)。
此等化合物之非限制性實例包括2-(2,6-二甲基嗎啉-4-基甲基)-1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基戊-2-醇、1-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-3,5-二甲基哌啶-4-酮、1-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-3-甲基-1H-喹啉-4-酮、1-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-2,3-二氫-1H-喹啉-4-酮、1-[4-(4-氟苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-[4-(3-氟苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-[4-(4-氟-2-羥基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-[4-苯基-2-羥基-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-[4-(5-氟-2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-[4-(5-溴-2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-[4-(5-甲基-2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-[4-(5-氯-2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-[4-(2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-[4-(5-氟-2-羥基苯
基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-[1,5]萘啶-4-酮、1-[4-(5-氟-2-甲氧基苯基)-2-羥基-2,4-二甲基戊基]-3,5-二甲基-1H-吡啶-4-酮、1-[2-羥基-4-(2-甲氧基-5-噻吩-2-基苯基)-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-[4-(6-溴苯并[1,3]二氧雜環戊烯-4-基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-[4-(5-氟-2-羥基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-3-甲基-1H-喹啉-4-酮、1-[2-羥基-4-(4-羥基聯苯-3-基)-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-{4-[5-(3,5-二甲基異噁唑-4-基)-2-羥基苯基]-2-羥基-4-甲基-2-三氟甲基戊基}-1H-喹啉-4-酮、1-[2-羥基-4-(2-羥基-5-噻吩-3-基苯基)-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-{4-[5-(3,5-二甲基異噁唑-4-基)-2-甲氧基苯基]-2-羥基-4-甲基-2-三氟甲基戊基}-1H-喹啉-4-酮、1-[2-羥基-4-甲基-4-(3-吡啶-3-基苯基)-2-三氟甲基戊基]-1H-喹啉-4-酮、4-甲氧基-3-[4,4,4-三氟-3-羥基-1,1-二甲基-3-(4-側氧基-4H-喹啉-1-基甲基)丁基]苯甲醛、1-[2-羥基-4-(2-甲氧基-5-噻吩-3-基苯基)-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-[4-(5-呋喃-3-基-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-[2-羥基-4-(4-甲氧基聯苯-3-基)-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-[4-(5-乙醯基-2-羥基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-[3,3,3-三氟-2-(6-氟-4-甲基色滿-4-基甲基)-2-羥基丙基]-1H-喹啉-4-酮、1-(4-{3-[1-(芐氧基亞胺基)乙基]苯基}-2-羥基-4-甲基-2-三氟甲基戊基)-1H-喹啉-4-酮、
1-[4-(5-乙醯基-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-(2-羥基-4-{3-[1-(甲氧基亞胺基)乙基]苯基}-4-甲基-2-三氟甲基戊基)-1H-喹啉-4-酮、1-[4-(5-溴-2-羥基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-(2-羥基-4-{3-[1-(羥基亞胺基)乙基]苯基}-4-甲基-2-三氟甲基戊基)-1H-喹啉-4-酮、1-[4-(5-溴-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-[4-(3,5-二氟苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-[4-(3,5-二甲基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-{2-羥基-4-甲基-4-[3-(2-甲基-[1,3]二氧雜環戊-2-基)苯基]-2-三氟甲基戊基}-1H-喹啉-4-酮、1-[4-(2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-[1,5]萘啶-4-酮、1-[4-(3-[1,3]二氧雜環己-2-基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-{4-[3-(3,5-二甲基異噁唑-4-基)苯基]-2-羥基-4-甲基-2-三氟甲基戊基}-1H-喹啉-4-酮、1-[4-(2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-3,5-二甲基-1H-吡啶-4-酮、1-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-2-羥基甲基-3,5-二甲基-1H-吡啶-4-酮、1-[4-(5-氟-2-羥基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-3-羥基甲基-1H-喹啉-4-酮、1-[4-(3-溴苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-6-甲基-1H-喹啉-4-酮、6-氟-1-[4-(5-氟-2-羥基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-喹啉
-4-酮、1-[-4-(2-二氟甲氧基-5-氟苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-(4-聯苯-3-基-2-羥基-4-甲基-2-三氟甲基戊基)-1H-喹啉-4-酮、1-[2-羥基-4-(2-羥基-5-甲基苯基)-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-[2-羥基-4-(3-異丙氧基苯基)-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-[4-(3-乙氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-[2-羥基-4-(2-甲氧基-5-甲基苯基)-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-[4-(2,5-二甲基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-[2-羥基-4-(3-甲氧基苯基)-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-[4-(5-氟-2-羥基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1,2-二氫吲唑-3-酮、7-氟-1-[4-(5-氟-2-羥基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-[4-(5-氟-2-羥基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-3,5-二甲基-1H-吡啶-4-酮、7-氟-1-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-(2-羥基-4-甲基-4-苯基-2-三氟甲基己基)-1H-喹啉-4-酮、1-[4-(4-氟-2-甲基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-H-喹啉-4-酮、1-[4-(3,4-二甲基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、8-氟-1-[4-(5-氟-2-羥基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、6-氟-1-[4-(5-氟-2-羥基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、7-氯-1-[4-(5-氟-2-羥基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-[4-(5-氟-2-異丙氧基苯基)-2-羥基-4-
甲基-2-三氟甲基戊基]-H-喹啉-4-酮、1-[4-(2-乙氧基-5-氟苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、8-氟-1-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、6-氟-1-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-[2-羥基-4-(5-甲烷磺醯基-2,3-二氫苯并呋喃-7-基)-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-[2-羥基-4-甲基-4-(5-甲基硫基-2,3-二氫苯并呋喃-7-基)-2-三氟甲基戊基]-1H-喹啉-4-酮、7-氯-1-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、3-氯-1-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-5-三氟甲基-1H-吡啶-2-酮、1-[2-羥基-4-(5-甲烷磺醯基-2,3-二氫苯并呋喃-7-基)-4-甲基-2-三氟甲基戊基]-3-甲基-1H-喹啉-4-酮、1-[2-羥基-4-(2-甲氧基-5-吡啶-3-基苯基)-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-[2-羥基-4-(2-羥基-3,5-二甲基苯基)-4-甲基-2-三氟甲基戊基]-H-喹啉-4-酮、1-[4-(3-[1,3]二氧雜環己-2-基-4-氟苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、2-(1,1-二側氧基-2,3-二氫-1H-1λ6-苯并[1,4]噻嗪-4-基甲基)-1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基戊-2-醇、2-(2,3-二氫苯并[1,4]噁嗪-4-基甲基)-1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基戊-2-醇、1-[4-(5-氟-2-羥基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-H-喹啉-4-酮、1-[4-(5-氟-2-羥基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-H-[1,5]萘啶-4-酮、1-[4-(5-氟-2-甲基苯基)-2-羥基-4-甲基-2-三氟甲基戊
基]-H-喹啉-4-酮、1-[4-(2,4-二甲基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-[4-(4-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-H-喹啉-4-酮、1-[4-(3-氟-4-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-(4-苯并[1,3]二氧雜環戊烯-4-基-2-羥基-4-甲基-2-三氟甲基戊基)-1H-喹啉-4-酮、1-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1,2-二氫吲唑-3-酮、1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基-2-(1-側氧基-2,3-二氫-1H-1λ4-苯并[1,4]噻嗪-4-基甲基)戊-2-醇、1-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-2-羥基甲基-3,5-二甲基-1H-吡啶-4-酮、1-[4-(2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-3-甲基-1H-喹啉-4-酮、1-[2-羥基-4-(2-甲氧基-3,5-二甲基苯基)-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮、1-[2-羥基-4-(2-羥基-5-吡啶-3-基苯基)-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮及1-[2-羥基-4-(2-羥基-5-吡啶-5-基苯基)-4-甲基-2-三氟甲基戊基]-1H-喹啉-4-酮。
於另一實施例中，該至少DIGRA具有式I，其中A、R1、R2、B、D、E及Q具有以上所揭示之含義，及R3係氫、C1至C8烷基、C2至C8烯基、C2至C8炔基、碳環、雜環基、芳基、雜芳基、碳環-C1至C8烷基、羧基、烷氧羰基、芳基-C1至C8烷基、芳基-C1至C8鹵烷基、雜環基-C1至C8烷基、雜芳基-C1至C8烷基、碳環-C2至C8烯基、芳基-C2至C8烯基、雜環基-C2至C8烯基或雜芳基-C2至C8烯基，各者視需要獨立地
經一至三個取代基取代，其中R3之各取代基獨立地係C1至C5烷基、C2至C5烯基、C2至C5炔基、C3至C8環烷基、苯基、C1至C5烷氧基、苯氧基、C1至C5烷醯基、芳醯基、C1至C5烷氧羰基、C1至C5烷醯氧基、胺基羰氧基、C1至C5烷胺基羰氧基、C1至C5二烷胺基羰氧基、胺基羰基、C1至C5烷胺基羰基、C1至C5二烷胺基羰基、C1至C5烷醯基胺基、C1至C5烷氧羰基胺基、C1至C5烷基磺醯胺基、C1至C5烷胺基磺醯基、C1至C5二烷胺基磺醯基、鹵素、羥基、羧基、氰基、側氧基、三氟甲基、硝基、胺基(其中氮原子視需要獨立地經C1至C5烷基單或二取代)、脲基(其中任一氮原子視需要獨立地經C1至C5烷基取代)、C1至C5烷硫基(其中硫原子視需要氧化以形成亞碸或碸)，其中R3不可為三氟甲基。
於另一實施例中，該至少DIGRA具有式I，其中a)A係各自視需要獨立地經一至三個取代基取代之芳基、雜芳基或C5至C15環烷基，該等取代基獨立地選自由C1至C5烷基、C2至C5烯基、C2至C5炔基、C1至C3烷醯基、C3至C8環烷基、雜環基、芳基、雜芳基、C1至C5烷氧基、C2至C5烯氧基、C2至C5炔氧基、芳氧基、醯基、C1至C5烷氧羰基、芳醯基、胺基羰基、烷胺基羰基、二烷胺基羰基、胺基羰氧基、C1至C5烷胺基羰氧基、C1至C5二烷胺基羰氧基、C1至C5烷醯基胺基、C1至C5烷氧羰基胺基、C1至C5烷基磺醯胺基、胺基磺醯基、C1至C5烷胺基磺醯基、C1至C5二烷胺基磺醯基、鹵素、羥基、羧基、氰基、三氟甲基、三氟甲氧基、硝基、胺基(其中氮原子視需要獨立地經C1至
C5烷基或芳基單或二取代)、脲基(其中任一氮原子視需要獨立地經C1至C5烷基取代)、C1至C5烷硫基(其中硫原子視需要氧化以形成亞碸或碸)組成之群；b)R1及R2各自獨立地係氫或C1至C5烷基，或R1及R2藉由其等共同連接之碳原子一起形成C3至C8螺環烷基環；c)R3係三氟甲基；d)B係羰基；e)D係-NH-基團；f)E係羥基；及g)Q包括呈下式之視需要經取代苯基
其中X1、X2、X3及X4各自獨立地選自由氫、鹵素、羥基、三氟甲基、三氟甲氧基、C1至C5烷基、C2至C5烯基、C2至C5炔基、C1至C5烷氧基、C1至C5烷硫基(其中硫原子係視需要經氧化以形成亞碸或碸)、C1至C5烷醯基、C1至C5烷氧羰基、C1至C5醯氧基、C1至C5烷醯胺基、C1至C5胺基甲醯基氧基、脲基、芳基及胺基組成之群(其中氮原子可獨立地經C1至C5烷基單或二取代)及其中該芳基視需要經一或多個羥基或C1至C5烷氧基取代，及其中脲基中之任一氮原子可獨立地經C1至C5烷基取代；或Q係在環中具有選自氮、氧及
硫之一至四個雜原子且視需要獨立地經一至三個取代基取代之芳族5-至7-員單環，其中該等取代基選自由氫、鹵素、羥基、三氟甲基、三氟甲氧基、C1至C5烷基、C2至C5烯基、C2至C5炔基、C1至C5烷氧基、C1至C5烷硫基(其中硫原子視需要經氧化以形成亞碸或碸)、C1至C5烷醯基、C1至C5烷氧羰基、C1至C5醯氧基、C1至C5烷醯胺基、C1至C5胺基甲醯基氧基、脲基、視需要經一或多個羥基或C1至C5烷氧基取代之芳基及胺基(其中氮原子可獨立地經C1至C5烷基單-或二取代)組成之群，且其中脲基中之任一氮原子可獨立地經C1至C5烷基取代。
此等化合物之非限制性實例包括4-(5-氟-2-羥基-苯基)-2-羥基-4-甲基-2-三氟甲基-戊酸(3,5-二氯-苯基)-醯胺、4-(5-氟-2-羥基-苯基)-2-羥基-4-甲基-2-三氟甲基-戊酸(3-氯-苯基)-醯胺、4-(5-氟-2-羥基-苯基)-2-羥基-4-甲基-2-三氟甲基-戊酸(2-氯-苯基)-醯胺、4-(5-氟-2-羥基-苯基)-2-羥基-4-甲基-2-三氟甲基-戊酸(2,6-二氯-嘧啶-4-基)-醯胺、4-(5-氟-2-羥基-苯基)-2-羥基-4-甲基-2-三氟甲基-戊酸(2,6-二氯-吡啶-4-基)-醯胺、4-(5-氟-2-羥基-苯基)-2-羥基-4-甲基-2-三氟甲基-戊酸(2,3-二氯-苯基)-醯胺、4-(5-氟-2-羥基-苯基)-2-羥基-4-甲基-2-三氟甲基-戊酸(3,5-二甲基-苯基)-醯胺、4-(5-氟-2-羥基-苯基)-2-羥基-4-甲基-2-三氟甲基-戊酸(3,5-雙-三氟甲基-苯基)-醯胺、4-(5-氟-2-羥基-苯基)-2-羥基-4-甲基-2-三氟甲基-戊酸(2,5-二氯-苯基)-醯胺、4-(5-氟-2-羥基-苯基)-2-羥基-4-甲基-2-三氟甲基-戊酸(3-溴-苯
基)-醯胺、4-(5-氟-2-羥基-苯基)-2-羥基-4-甲基-2-三氟甲基-戊酸(3,5-二氟-苯基)-醯胺、4-(5-氟-2-羥基-苯基)-2-羥基-4-甲基-2-三氟甲基-戊酸(3,5-二溴-苯基)-醯胺。
於另一實施例中，該至少DIGRA具有式I，其中a)A係各自視需要獨立地經一至三個取代基取代之芳基或雜芳基，該等取代基獨立地係選自由C1至C5烷基、C2至C5烯基、C2至C5炔基、C1至C3烷醯基、C3至C8環烷基、雜環基、芳基、雜芳基、C1至C5烷氧基、C2至C5烯氧基、C2至C5炔氧基、芳氧基、醯基、C1至C5烷氧羰基、芳醯基、胺基羰基、烷胺基羰基、二烷胺基羰基、胺基羰氧基、C1至C5烷胺基羰氧基、C1至C5二烷胺基羰氧基、C1至C5烷醯基胺基、C1至C5烷氧羰基胺基、C1至C5烷基磺醯胺基、胺基磺醯基、C1至C5烷胺基磺醯基、C1至C5二烷胺基磺醯基、鹵素、羥基、羧基、氰基、三氟甲基、三氟甲氧基、硝基、胺基(其中氮原子視需要獨立地經C1至C5烷基或芳基單或二取代)、脲基(其中任一氮原子視需要獨立地經C1至C5烷基取代)、C1至C5烷硫基(其中硫原子視需要氧化以形成亞碸或碸)組成之群；b)R1及R2各自獨立地係氫或C1至C5烷基；c)R3係C1至C8烷基、C2至C8烯基、C2至C8炔基、碳環、雜環基、芳基、雜芳基、碳環-C1至C8烷基、芳基-C1至C8烷基、芳基-C1至C8鹵烷基、雜環基-C1至C8烷基、雜芳基-C1至C8烷基、碳環-C2至C8烯基、芳基-C2至C8烯基、雜環基-C2至C8烯基或雜芳基-C2至C8烯基，各者視需要獨立地經一至
三個取代基取代，其中R3之各取代基獨立地係C1至C5烷基、C2至C5烯基、C2至C5炔基、C3至C8環烷基、苯基、C1至C5烷氧基、苯氧基、C1至C5烷醯基、芳醯基、C1至C5烷氧羰基、C1至C5烷醯氧基、胺基羰氧基、C1至C5烷胺基羰氧基、C1至C5二烷胺基羰氧基、胺基羰基、C1至C5烷胺基羰基、C1至C5二烷胺基羰基、C1至C5烷醯基胺基、C1至C5烷氧羰基胺基、C1至C5烷基磺醯胺基、C1至C5烷胺基磺醯基、C1至C5二烷胺基磺醯基、鹵素、羥基、羧基、氰基、側氧基、三氟甲基、硝基、胺基(其中氮原子視需要獨立地經C1至C5烷基單或二取代)、脲基(其中任一氮原子視需要獨立地經C1至C5烷基取代)、C1至C5烷硫基(其中硫原子視需要氧化以形成亞碸或碸)，其中R3不可為三氟甲基；d)B係C1至C5伸烷基、C2至C5-伸烯基或C2至C5伸炔基，各者視需要獨立地經一至三個取代基取代，其中B之各取代基獨立地係C1至C3烷基、烷氧基、鹵素、胺基或側氧基；e)D不存在；f)E係羥基；及g)Q包括視需要獨立地經一至三個取代基取代之氮雜吲哚基，其中Q之各取代基獨立地係C1至C5烷基、C2至C5烯基、C2至C5炔基、C3至C8環烷基、雜環基、芳基、雜芳基、C1至C5烷氧基、C2至C5烯氧基、C2至C5炔氧基、芳氧基、醯基、C1至C5烷氧羰基、C1至C5烷醯氧基、胺基羰基、烷胺基羰基、二烷胺基羰基、胺基羰氧基、C1至C5烷胺基羰氧基、C1至C5二烷胺基羰氧基、C1至C5烷醯基胺基、C1至
C5烷氧羰基胺基、C1至C5烷基磺醯胺基、胺基磺醯基、C1至C5烷胺基磺醯基、C1至C5二烷胺基磺醯基、鹵素、羥基、羧基、氰基、三氟甲基、三氟甲氧基、三氟甲硫基、硝基、胺基(其中氮原子視需要獨立地經C1至C5烷基單或二取代)、脲基(其中任一氮原子視需要獨立地經C1至C5烷基取代)、C1至C5烷硫基(其中硫原子視需要氧化以形成亞碸或碸)，其中Q之各取代基視需要獨立地經一或三個取代基取代，該等取代基選自由C1至C3烷基、C1至C3烷氧基、鹵素、羥基、側氧基、氰基、胺基及三氟甲基組成之群。
此等化合物之非限制性實例包括1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基-2-(1H-吡咯并[2,3-c]吡啶-2-基甲基)戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基-2-(1H-吡咯并[2,3-b]吡啶-2-基甲基)戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基-2-(1H-吡咯并[3,2-c]吡啶-2-基甲基)戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基-2-(1H-吡咯并[3,2-b]吡啶-2-基甲基)戊-2-醇、4-氟-2-[4,4,4-三氟-3-羥基-1,1-二甲基-3-(1H-吡咯并[2,3-c]吡啶-2-基甲基)丁基]酚、4-氟-2-[4,4,4-三氟-3-羥基-1,1-二甲基-3-(1H-吡咯并[2,3-b]吡啶-2-基甲基)丁基]酚、4-氟-2-[4,4,4-三氟-3-羥基-1,1-二甲基-3-(1H-吡咯并[3,2-c]吡啶-2-基甲基)丁基]酚、4-氟-2-[4,4,4-三氟-3-羥基-1,1-二甲基-3-(1H-吡咯并[3,2-b]吡啶-2-基甲基)丁基]酚、1,1,1-三氟-4-(3-氟苯基)-4-甲基-2-(1H-吡咯并[2,3-c]吡啶-2-基甲基)戊-2-醇、1,1,1-三氟-4-(4-氟苯基)-4-甲基-2-(1H-吡咯并[2,3-c]吡啶-2-基甲基)
戊-2-醇、4-(2,3-二氫苯并呋喃-7-基)-1,1,1-三氟-4-甲基-2-(1H-吡咯并[2,3-c]吡啶-2-基甲基)戊-2-醇、4-(2,3-二氫苯并呋喃-7-基)-1,1,1-三氟-4-甲基-2-(1H-吡咯并[3,2-c]吡啶-2-基甲基)戊-2-醇、1,1,1-三氟-4-甲基-4-苯基-2-(1H-吡咯并[2,3-c]吡啶-2-基甲基)戊-2-醇、1,1,1-三氟-4-(4-氟-2-甲氧基苯基)-4-甲基-2-(1H-吡咯并[2,3-c]吡啶-2-基甲基)戊-2-醇、1,1,1-三氟-4-(4-氟-2-甲氧基苯基)-4-甲基-2-(1H-吡咯并[3,2-c]吡啶-2-基甲基)戊-2-醇、1,1,1-三氟-4-甲基-4-苯基-2-(1H-吡咯并[3,2-c]吡啶-2-基甲基)戊-2-醇、1,1,1-三氟-4-(4-氟苯基)-4-甲基-2-(1H-吡咯并[3,2-c]吡啶-2-基甲基)戊-2-醇、5-氟-2-[4,4,4-三氟-3-羥基-1,1-二甲基-3-(1H-吡咯并[2,3-c]吡啶-2-基甲基)丁基]酚、1,1,1-三氟-4-(5-氟-2-甲基苯基)-4-甲基-2-(1H-吡咯并[2,3-c]吡啶-2-基甲基)戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基-2-(3-甲基-1H-吡咯并[2,3-c]吡啶-2-基甲基)戊-2-醇、4-氟-2-[4,4,4-三氟-3-羥基-1,1-二甲基-3-(3-甲基-1H-吡咯并[2,3-c]吡啶-2-基甲基)丁基]酚、5-氟-2-[4,4,4-三氟-3-羥基-1,1-二甲基-3-(1H-吡咯并[3,2-c]吡啶-2-基甲基)丁基]戊-2-醇、1,1,1-三氟-4-(5-氟-2,3-二氫苯并呋喃-7-基)-4-甲基-2-(1H-吡咯并[2,3-c]吡啶-2-基甲基)戊-2-醇、4-氟-2-[4,4,4-三氟-3-羥基-1,1-二甲基-3-(1H-吡咯并[2,3-c]-[3-甲基吡啶]-2-基甲基)丁基]酚、4-氟-2-[4,4,4-三氟-3-羥基-1,1-二甲基-3-(1H-吡咯并[2,3-c]-[2-氟吡啶]-2-基甲基)丁基]酚及4-氟-2-[4,4,4-三氟-3-羥基-1,1-二甲基-3-(1H-吡咯并
[2,3-c]-[2-三氟甲基吡啶]-2-基甲基)丁基]酚。
於另一實施例中，該至少DIGRA具有式I，其中a)A係各自視需要獨立地經一至三個取代基取代之芳基或雜芳基，該等取代基獨立地係選自由C1至C5烷基、C2至C5烯基、C2至C5炔基、C1至C3烷醯基、C3至C8環烷基、雜環基、芳基、雜芳基、C1至C5烷氧基、C2至C5烯氧基、C2至C5炔氧基、芳氧基、醯基、C1至C5烷氧羰基、芳醯基、胺基羰基、烷胺基羰基、二烷胺基羰基、胺基羰氧基、C1至C5烷胺基羰氧基、C1至C5二烷胺基羰氧基、C1至C5烷醯基胺基、C1至C5烷氧羰基胺基、C1至C5烷基磺醯胺基、胺基磺醯基、C1至C5烷胺基磺醯基、C1至C5二烷胺基磺醯基、鹵素、羥基、羧基、氰基、三氟甲基、三氟甲氧基、硝基、胺基(其中氮原子視需要獨立地經C1至C5烷基或芳基單或二取代)、脲基(其中任一氮原子視需要獨立地經C1至C5烷基取代)、C1至C5烷硫基(其中硫原子視需要氧化以形成亞碸或碸)組成之群；b)R1及R2各自獨立地係氫或C1至C5烷基，或R1及R2藉由其等共同連接之碳原子一起形成C3至C8螺環烷基環；c)R3係三氟甲基；d)B係C1至C5伸烷基、C2至C5伸烯基或C2至C5伸炔基，各者視需要獨立地經一至三個取代基取代，其中B之各取代基獨立地係C1至C3烷基、羥基、鹵素、胺基或側氧基；e)D不存在；f)E係羥基；及
g)Q包括視需要獨立地經一至三個取代基取代之雜芳基，該等取代基獨立地係選自由C1至C5烷基、C2至C5烯基、C2至C5炔基、C1至C3烷醯基、C3至C8環烷基、雜環基、芳基、雜芳基、C1至C5烷氧基、C2至C5烯氧基、C2至C5炔氧基、芳氧基、醯基、C1至C5烷氧羰基、芳醯基、胺基羰基、烷胺基羰基、二烷胺基羰基、胺基羰氧基、C1至C5烷胺基羰氧基、C1至C5二烷胺基羰氧基、C1至C5烷醯基胺基、C1至C5烷氧羰基胺基、C1至C5烷基磺醯胺基、胺基磺醯基、C1至C5烷胺基磺醯基、C1至C5二烷胺基磺醯基、鹵素、羥基、羧基、氰基、三氟甲基、三氟甲氧基、硝基、胺基(其中氮原子視需要獨立地經C1至C5烷基或芳基單或二取代)、脲基(其中任一氮原子視需要獨立地經C1至C5烷基取代)、C1至C5烷硫基(其中硫原子視需要氧化以形成亞碸或碸)組成之群，其中Q之各取代基係視需要經一至三個取代基取代，該等取代基選自由C1至C3烷基、C1至C3烷氧基、醯基、C1至C3矽烷氧基、C1至C5烷氧羰基、羧基、鹵素、羥基、側氧基、氰基、雜芳基、雜環基、胺基(其中氮原子視需要獨立地經C1至C5烷基或芳基單或二取代)、脲基(其中任一氮原子視需要獨立地經C1至C5烷基取代)或三氟甲基組成之群。
此等化合物之非限制性實例包括4-環己基-1,1,1-三氟-4-甲基-2-喹啉-4-基甲基戊-2-醇、4-嘧啶-5-基-2-[4,4,4-三氟-3-羥基-1,1-二甲基-3-(1H-吡咯并[2,3-c]吡啶-2-基甲基)丁基]酚、4-嘧啶-5-基-2-[4,4,4-三氟-3-羥基-1,1-二甲基
-3-(1H-吡咯并[3,2-c]吡啶-2-基甲基)丁基]酚、1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基-2-(3-甲基-1H-吡咯并[3,2-c]吡啶-2-基甲基)戊-2-醇、1,1,1-三氟-4-(5-氟-2,3-二氫苯并呋喃-7-基)-4-甲基-2-(1H-吡咯并[3,2-c]吡啶-2-基甲基)戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲基苯基)-4-甲基-2-(3-甲基-1H-吡咯并[2,3-c]吡啶-2-基甲基)戊-2-醇、2-(4,6-二甲基-1H-吡咯并[3,2-c]吡啶-2-基甲基)-1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基戊-2-醇、2-(5,7-二甲基-1H-吡咯并[2,3-c]吡啶-2-基甲基)-1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基戊-2-醇、2-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吡咯并[3,2-b]吡啶-5-甲腈、1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基-2-(6-甲基-1H-吡咯并[3,2-c]吡啶-2-基甲基)戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基-2-(4-甲基-1H-吡咯并[3,2-c]吡啶-2-基甲基)戊-2-醇、2-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-4-甲基-1H-吡咯并[3,2-c]吡啶-6-甲腈、2-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吡咯并[2,3-c]吡啶-5-甲腈、2-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吡咯并[3,2-c]吡啶-4-甲腈、1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基-2-(5H-吡咯并[3,2-d]嘧啶-6-基甲基)戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基-2-噻吩并[2,3-d]噠嗪-2-基甲基戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基-2-(5H-吡咯并[2,3-d]噠嗪-6-基甲基)戊-2-醇、1,1,1-三氟-4-(5-氟-2-
甲氧基苯基)-4-甲基-2-(2-甲基-5H-吡咯并[3,2-d]嘧啶-6-基甲基)戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲基苯基)-4-甲基-2-(1H-吡咯并[2,3-d]噠嗪-2-基甲基)戊-2-醇、2-(4,6-二甲基-H-吡咯并[3,2-c]吡啶-2-基甲基)-1,1,1-三氟-4-(5-氟-2-甲基苯基)-4-甲基戊-2-醇、4-(5-氯-2,3-二氫苯并呋喃-7-基)-2-(4,6-二甲基-1H-吡咯并[3,2-c]吡啶-2-基甲基)-1,1,1-三氟-4-甲基戊-2-醇、2-[4-(5-氟-2-甲基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吡咯并[3,2-b]吡啶-5-甲腈、4-(5-氯-2,3-二氫苯并呋喃-7-基)-1,1,1-三氟-4-甲基-2-(3-甲基-1H-吡咯并[2,3-c]吡啶-2-基甲基)戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲基苯基)-4-甲基-2-(5H-吡咯并[3,2-c]-噠嗪-6-基甲基)戊-2-醇、4-(5-氯-2,3-二氫苯并呋喃-7-基)-1,1,1-三氟-4-甲基-2-(5H-吡咯并[3,2-c]噠嗪-6-基甲基)戊-2-醇、4-(5-氯-2,3-二氫苯并呋喃-7-基)-1,1,1-三氟-4-甲基-2-(1-H-吡咯并[2,3-d]噠嗪-2-基甲基)戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-2-(7-氟-1H-吡咯并[2,3-c]吡啶-2-基甲基)-4-甲基戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基-2-(4-甲基-1H-吡咯并[2,3-c]吡啶-2-基甲基)戊-2-醇、2-(5,7-二氯-1H-吡咯并[2,3-c]吡啶-2-基甲基)-1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基-2-(5-三氟甲基-1H-吡咯并[2,3-c]吡啶-2-基甲基)戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-2-(5-甲氧基-1H-吡咯并[2,3-c]吡啶-2-基甲基)-4-甲基戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲基苯基)-4-甲基-2-(4-甲基-1H-吡咯并
[2,3-c]吡啶-2-基甲基)戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲基苯基)-2-(5-異丙氧基-1H-吡咯并[2,3-c]吡啶-2-基甲基)-4-甲基戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲基苯基)-2-(5-甲氧基-1H-吡咯并[2,3-c]吡啶-2-基甲基)-4-甲基戊-2-醇、4-(5-氯-2,3-二氫苯并呋喃-7-基)-1,1,1-三氟-2-(5-甲氧基-1H-吡咯并[2,3-c]吡啶-2-基甲基)-4-甲基戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲基苯基)-2-(7-氟-1H-吡咯并[2,3-c]吡啶-2-基甲基)-4-甲基戊-2-醇、4-(5-氯-2,3-二氫苯并呋喃-7-基)-1-三氟-4-甲基-2-(5-三氟甲基-1H-吡咯并[2,3-c]吡啶-2-基甲基)戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲基苯基)-4-甲基-2-(5-三氟甲基-1H-吡咯并[2,3-c]吡啶-2-基甲基)戊-2-醇、4-(5-氯-2,3-二氫苯并呋喃-7-基)-1,1,1-三氟-2-(5-異丙氧基-1H-吡咯并[2,3-c]吡啶-2-基甲基)-4-甲基戊-2-醇、4-(5-氯-2,3-二氫苯并呋喃-7-基)-1,1,1-三氟-2-(7-氟-1H-吡咯并[2,3-c]吡啶-2-基甲基)-4-甲基戊-2-醇、4-(5-氯-2,3-二氫苯并呋喃-7-基)-2-(5-二甲基胺基-1H-吡咯并[2,3-c]吡啶-2-基甲基)-1,1,1-三氟-4-甲基戊-2-醇、4-(5-氯-2,3-二氫苯并呋喃-7-基)-1,1,1-三氟-4-甲基-2-(5-哌啶-1-基-1H-吡咯并[2,3-c]吡啶-2-基甲基)戊-2-醇、4-(5-氯-2,3-二氫苯并呋喃-7-基)-1,1,1-三氟-4-甲基-2-(5-嗎啉-4-基-1H-吡咯并[2,3-c]吡啶-2-基甲基)戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲基苯基)-4-甲基-2-(5-哌啶-1-基-1H-吡咯并[2,3-c]吡啶-2-基甲基)戊-2-醇、4-(5-氯-2,3-二氫苯并呋喃-7-基)-2-(5-乙氧基-1H-吡咯并[2,3-c]吡啶-2-基甲基)-1,1,1-三氟-4-甲基戊-2-醇、
2-(5-芐氧基-1H-吡咯并[2,3-c]吡啶-2-基甲基)-1,1,1-三氟-4-(5-氟-2-甲基苯基)-4-甲基戊-2-醇、2-(5-芐氧基-1H-吡咯并[2,3-c]吡啶-2-基甲基)-4-(5-氯-2,3-二氫苯并呋喃-7-基)-1,1,1-三氟-4-甲基戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-2-(5-氯-1H-吡咯并[2,3-c]吡啶-2-基甲基)-4-甲基戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基-2-[5-(甲基胺基)-1H-吡咯并[2,3-c]吡啶-2-基甲基]戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基-2-(5-胺基-1H-吡咯并[2,3-c]吡啶-2-基甲基)戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲基苯基)-4-甲基-2-(6-胺基-1H-吡咯并[2,3-c]吡啶-2-基甲基)戊-2-醇、4-(5-氯-2,3-二氫苯并呋喃-7-基)-1,1,1-三氟-2-(5-胺基-1H-吡咯并[2,3-c]吡啶-2-基甲基)-4-甲基戊-2-醇、4-(5-氯-2,3-二氫苯并呋喃-7-基)-1,1,1-三氟-4-甲基-2-(5-甲基胺基-1H-吡咯并[2,3-c]吡啶-2-基甲基)戊-2-醇、7-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吡咯并[2,3-b]吡啶-7-鎓氯化物、6-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-2-甲基-1H-吡咯并[2,3-c]吡啶-6-鎓氯化物、4-(5-溴-2,3-二氫苯并呋喃-7-基)-1,1,1-三氟-4-甲基-2-(1H-吡咯并[2,3-c]吡啶-2-基甲基)戊-2-醇、1,1,1-三氟-4-甲基-4-(5-甲基-2,3-二氫苯并呋喃-7-基)-2-(1H-吡咯并[2,3-c]吡啶-2-基甲基)戊-2-醇、4-(5-氯-2,3-二氫苯并呋喃-7-基)-1,1,1-三氟-4-甲基-2-(1H-吡咯并[2,3-c]吡啶-2-基甲基)戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基-2-吡咯并[2,3-b]吡啶-1-基甲基戊-2-醇、
1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基-2-(6-氧基-1H-吡咯并[2,3,c]吡啶-2-基甲基)戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基-2-吡咯并[2,3-c]吡啶-1-基甲基戊-2-醇、2-苯并[b]噻吩-2-基甲基-1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基-2-噻吩并[2,3-c]吡啶-2-基甲基戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-2-吲唑-1-基甲基-4-甲基戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基-2-吡唑并[1,5-a]吡啶-2-基甲基戊-2-醇、4-(5-氯-2,3-二氫苯并呋喃-7-基)-2,4-二甲基-1-噻吩并[2,3-c]吡啶-2-基戊-2-醇、4-(5-氟-2-甲基苯基)-2,4-二甲基-1-噻吩并[2,3-c]吡啶-2-基戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-2-呋喃并[2,3-c]吡啶-2-基甲基-4-甲基戊-2-醇、4-(5-氯-2,3-二氫苯并呋喃-7-基)-1-呋喃并[2,3-c]吡啶-2-基-2,4-二甲基戊-2-醇、4-(5-氟-2-甲基苯基)-1-呋喃并-[2,3-c]吡啶-2-基-2,4-二甲基戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲基苯基)-4-甲基-2-(1H-吡咯并[3,2-c]吡啶-2-基甲基)戊-2-醇、1,1,1-三氟-4-甲基-4-(5-甲基-2,3-二氫苯并呋喃-7-基)-2-(1H-吡咯并[3,2-c]吡啶-2-基甲基)戊-2-醇、4-(5-氯-2,3-二氫苯并呋喃-7-基)-1,1,1-三氟-4-甲基-2-(1H-吡咯并[3,2-c]吡啶-2-基甲基)戊-2-醇、4-(5-溴-2,3-二氫苯并呋喃-7-基)-1,1,1-三氟-4-甲基-2-(1H-吡咯并[3,2-c]吡啶-2-基甲基)戊-2-醇、2-(3-二甲基胺基甲基-1H-吡咯并[3,2-c]吡啶-2-基甲基)-1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-
甲基-2-吡咯并[3,2-c]吡啶-1-基甲基戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基-2-吡咯并[3,2-b]吡啶-1-基甲基戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-2-呋喃并[3,2-c]吡啶-2-基甲基-4-甲基戊-2-醇、4-(5-氯-2,3-二氫苯并呋喃-7-基)-1,1,1-三氟-4-甲基-2-吡咯并[3,2-b]吡啶-1-基甲基戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基-2-噻吩并[3,2-c]吡啶-2-基甲基戊-2-醇、4-(5-氯-2,3-二氫苯并呋喃-7-基)-1,1,1-三氟-4-甲基-2-噻吩并[3,2-c]吡啶-2-基甲基戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲基苯基)-4-甲基-2-吡咯并[3,2-b]吡啶-1-基甲基戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲基苯基)-4-甲基-2-噻吩并[3,2-c]吡啶-2-基甲基戊-2-醇、4-氟-2-(4,4,4-三氟-3-羥基-1,1-二甲基-3-噻吩并[3,2-c]吡啶-2-基甲基丁基)酚、4-氟-2-(4,4,4-三氟-3-呋喃并[3,2-c]吡啶-2-基甲基-3-羥基-1,1-二甲基丁基)酚、4-氟-2-(4,4,4-三氟-3-羥基-1,1-二甲基-3-吡咯并[3,2-b]吡啶-1-基甲基丁基)酚、2-[4-(5-氟-2-羥基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚-6-甲酸、2-[4-(5-氟-2-羥基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚-6-甲酸二甲醯胺、{2-[4-(5-氟-2-羥基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚-6-基}嗎啉-4-基甲酮、2-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚-6-甲酸二甲醯胺、{2-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚-6-基}嗎啉-4-基甲酮、2-[4-(5-氟-2-羥基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚-6-甲酸醯胺、2-[4-(5-氟-2-
甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚-6-甲酸醯胺、4-氟-2-[4,4,4-三氟-3-羥基-1,1-二甲基-3-(5-硝基-1H-吲哚-2-基甲基)丁基]酚、2-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚-6-甲腈、2-[4-(5-氟-2-羥基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚-6-甲腈、N-{2-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚5-基}乙醯胺、1,1,1-三氟-4-(4-氟-2-甲氧基苯基)-2-(7-氟-4-甲基-1H-吲哚-2-基甲基)-4-甲基戊-2-醇、5-氟-2-[4,4,4-三氟-3-(7-氟-4-甲基-1H-吲哚-2-基甲基)-3-羥基-1,1-二甲基丁基]酚、2-[4-(3-[1,3]二氧雜環戊-2-基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚-5-甲腈、2-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚-5-甲酸-2-三甲基矽烷基乙基酯、2-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚-5-甲酸、2-[4-(4-氟-2-羥基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-4-甲基-1H-吲哚-6-甲腈、{2-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚5-基}哌啶-1-基甲酮、2-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚-5-甲酸甲醯胺、{2-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚5-基}吡咯啶-1-基甲酮、1-{2-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]1H-吲哚-5-羰基}哌啶-4-酮、2-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚-5-甲酸(2-羥基乙基)醯胺、{2-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-
甲基-2-三氟甲基戊基]-1H-吲哚5-基}(4-羥基哌啶-1-基)甲酮、{2-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚5-基}(3-羥基吡咯啶-1-基)甲酮、2-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚-5-甲酸氰基甲醯胺、2-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚-5-甲酸(2-二甲基胺基乙基)醯胺、{2-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚5-基}(4-甲基哌嗪-1-基)甲酮、({2-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚-5-羰基}胺基)乙酸甲基酯、2-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚-5-甲酸胺基甲醯基甲醯胺、4-({2-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚-5-羰基}胺基)丁酸甲基酯、({2-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚-5-羰基}胺基)乙酸、4-({2-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚-5-羰基}胺基)丁酸、2-[4-(3-二甲基胺基甲基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚-5-甲腈、4-氟-2-[4,4,4-三氟-3-羥基-1,1-二甲基-3-(5-三氟甲基-1H-吲哚-2-基甲基)丁基]酚、2-[4-(5-溴-2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-4-甲基-1H-吲哚-6-甲腈、2-[2-羥基-4-(5-甲烷磺醯基-2,3-二氫苯并呋喃-7-基)-4-甲基-2-三氟甲基戊基]-4-甲基-1H-吲哚-6-甲腈、2-[4-(5-溴-2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚-5-甲酸、2-[4-(5-溴
-2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚-5-甲酸醯胺、2-[4-(5-溴-2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚-5-甲酸二甲醯胺、2-[4-(5-溴-2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚-5-甲酸氰基甲醯胺、{2-[4-(5-溴-2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚5-基}吡咯啶-1-基甲酮、{2-[4-(5-溴-2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟-甲基戊基]-1H-吲哚-5-基}嗎啉-4-基甲酮、2-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚-5-甲酸醯胺、{2-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚5-基}嗎啉-4-基甲酮、2-(4-苯并[1,3]二氧雜環戊烯-4-基-2-羥基-4-甲基-2-三氟甲基戊基)-4-甲基-1H-吲哚-6-甲腈、1,1,1-三氟-4-甲基-4-苯基-2-喹啉-4-基甲基己-2-醇、2-[2-羥基-4-甲基-4-(5-甲基硫基-2,3-二氫苯并呋喃-7-基)-2-三氟甲基戊基]-1H-吲哚-3-甲腈、7-(4,4,4-三氟-3-羥基-1,1-二甲基-3-喹啉-4-基甲基丁基)-2,3-二氫苯并呋喃-5-甲腈、2-[2-羥基-4-(5-甲烷磺醯基-2,3-二氫苯并呋喃-7-基)-4-甲基-2-三氟甲基戊基]-1H-吲哚-3-甲腈、2-[2-羥基-4-(2-羥基-5-甲基苯基)-4-甲基-2-三氟-甲基戊基]-4-甲基-1H-吲哚-6-甲腈、1,1,1-三氟-4-(5-氟-2,3-二氫苯并呋喃-7-基)-4-甲基-2-(5-甲基硫基-1H-吲哚-2-基甲基)戊-2-醇、2-[2-羥基-4-(2-甲氧基-5-甲基硫基苯基)-4-甲基-2-三氟甲基戊基]-1H-吲哚-3-甲腈、2-[2-羥基-4-(5-甲烷磺醯基-2-甲氧基苯基)-4-甲基-2-
三氟甲基戊基]-1H-吲哚-3-甲腈、2-[4-(5-氟-2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚-5-磺酸二甲醯胺、1,1,1-三氟-4-(5-氟-2,3-二氫苯并呋喃-7-基)-4-甲基-2-(5-苯基-1H-吲哚-2-基甲基)戊-2-醇、2-[4-(5-第三丁基-2-羥基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚-3-甲腈、2-[2-羥基-4-(2-羥基-5-異丙基苯基)-4-甲基-2-三氟甲基戊基]-1H-吲哚-3-甲腈、2-[2-羥基-4-(2-羥基-3,5-二甲基苯基)-4-甲基-2-三氟甲基戊基]-1H-吲哚-3-甲腈、2-[2-羥基-4-(5-羥基-2,4-二甲基苯基)-4-甲基-2-三氟甲基戊基]-1H-吲哚-3-甲腈、2-[4-(5-第三丁基-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚-3-甲腈、2-[4-(5-第三丁基-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1-甲基-1H-吲哚-3-甲腈、2-[2-羥基-4-(5-異丙基-2-甲氧基苯基)-4-甲基-2-三氟甲基戊基]-1H-吲哚-3-甲腈、2-[2-羥基-4-(5-異丙基-2-甲氧基苯基)-4-甲基-2-三氟甲基戊基]-1-甲基-1H-吲哚-3-甲腈、2-[2-羥基-4-(2-羥基-5-甲烷磺醯基苯基)-4-甲基-2-三氟甲基戊基]-1H-吲哚-3-甲腈、2-[2-羥基-4-(2-甲氧基-5-甲基苯基)-4-甲基-2-三氟甲基戊基]-4-甲基-1H-吲哚-6-甲腈、1,1,1-三氟-4-甲基-2-喹啉-4-基甲基-4-鄰甲苯基戊-2-醇、1,1,1-三氟-4-甲基-2-喹啉-4-基甲基-4-間甲苯基戊-2-醇、1,1,1-三氟-4-(2-氟苯基)-2-(1H-吲哚-2-基甲基)-4-甲基戊-2-醇、1,1,1-三氟-4-(2-氟苯基)-4-甲基-2-喹啉-4-基甲基戊-2-醇、1,1,1-三氟-4-(3-氟苯基)-2-(1H-吲哚-2-基甲基)-4-甲基戊-2-醇、1,1,1-三氟
-4-(3-氟苯基)-4-甲基-2-喹啉-4-基甲基戊-2-醇、1,1,1-三氟-4-(4-氟苯基)-2-(1H-吲哚-2-基甲基)-4-甲基戊-2-醇、1,1,1-三氟-4-(4-氟苯基)-4-甲基-2-喹啉-4-基甲基戊-2-醇、3-(4,4,4-三氟-3-羥基-1,1-二甲基-3-喹啉-4-基甲基丁基)酚、1,1,1-三氟-4-甲基-2-喹啉-4-基甲基-4-(2-三氟甲基苯基)戊-2-醇、1,1,1-三氟-2-(1H-吲哚-2-基甲基)-4-甲基-4-(4-三氟甲基苯基)戊-2-醇、1,1,1-三氟-4-甲基-2-喹啉-4-基甲基-4-(4-三氟甲基苯基)戊-2-醇、4-(3-氯苯基)-1,1,1-三氟-2-(1H-吲哚-2-基甲基)-4-甲基戊-2-醇、4-(3-氯苯基)-1,1,1-三氟-4-甲基-2-喹啉-4-基甲基戊-2-醇、4-(4-二甲基胺基苯基)-1,1,1-三氟-2-(1H-吲哚-2-基甲基)-4-甲基戊-2-醇、4-聯苯-3-基-1,1,1-三氟-4-甲基-2-喹啉-4-基甲基戊-2-醇、4-(3-溴苯基)-1,1,1-三氟-2-(1H-吲哚-2-基甲基)-4-甲基戊-2-醇、4-(2-二氟甲氧基-5-氟苯基)-1,1,1-三氟-2-(1H-吲哚-2-基甲基)-4-甲基戊-2-醇、4-聯苯-3-基-1,1,1-三氟-2-(1H-吲哚-2-基甲基)-4-甲基戊-2-醇、4-(4-二甲基胺基苯基)-1,1,1-三氟-4-甲基-2-喹啉-4-基甲基戊-2-醇、2-[4-(5-氟-2-甲基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1,6-二氫吡咯并[2,3-c]吡啶-5-酮、2-[4-(5-氟-2-甲基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-6-甲基-1,6-二氫吡咯并[2,3-c]吡啶-5-酮、2-[4-(5-氟-2-甲基-苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-4-甲基-1,4-二氫吡咯并[3,2-b]吡啶-5-酮、1,1,1-三氟-4-(5-氟-2-甲基苯基)-2-(6-甲氧基-1H-吡咯并[3,2-c]吡啶-2-基甲基)-4-甲基戊-2-醇、2-[4-(5-氟-2-甲基苯基)-2-羥基
-4-甲基-2-三氟甲基戊基]-5-甲基-1,5-二氫吡咯并[3,2-c]吡啶-6-酮、2-[4-(5-氟-2-甲基-苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1,3a-二氫吡咯并[3,2-c]吡啶-6-酮、2-[4-(5-氟-2-甲基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1,7-二氫吡咯并[3,2-c]吡啶-4,6-二酮、6-[4-(5-氟-2-甲基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-3-甲基-1,7-二氫吡咯并[2,3-d]嘧啶-2,4-二酮、2-[4-(5-氯-2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟-甲基戊基]-1,6-二氫吡咯并[2,3-c]吡啶-5-酮、2-[4-(5-氯-2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-6-甲基-1,6-二氫吡咯并[2,3-c]吡啶-5-酮、2-[4-(5-氯-2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-1,4-二氫吡咯并[3,2-b]吡啶-5-酮、2-[4-(5-氯-2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-4-甲基-1,4-二氫吡咯并[3,2-b]吡啶-5-酮、2-[4-(5-氯-2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟-甲基戊基]-1,5-二氫吡咯并[3,2-c]吡啶-6-酮、2-[4-(5-氯-2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-5-甲基-1,5-二氫吡咯并[3,2-c]吡啶-6-酮、4-(5-氯-2,3-二氫苯并呋喃-7-基)-1,1,1-三氟-2-(6-甲氧基-5,6-二氫-1H-吡咯并[3,2-c]吡啶-2-基甲基)-4-甲基戊-2-醇、2-[4-(5-氯-2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-1,7-二氫吡咯并[3,2-c]吡啶-4,6-二酮、6-[4-(5-氯-2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-3-甲基-1,7-二氫吡咯并[2,3-d]嘧啶-2,4-二酮、2-[4-(3-二甲基胺基甲基苯
基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚-5-甲腈、1,1,1-三氟-2-(1H-吲哚-2-基甲基)-4-甲基-4-(3-嗎啉-4-基甲基苯基)戊-2-醇、1,1,1-三氟-4-甲基-4-(3-嗎啉-4-基甲基苯基)-2-(1H-吡咯并[2-,3-d]噠嗪-2-基甲基)戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲基苯基)-4-甲基-2-(5-嗎啉-4-基甲基-1H-吲哚-2-基甲基)戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲基苯基)-4-甲基-2-(5-嗎啉-4-基甲基-1H-吡咯并[2,3-c]吡啶-2-基甲基)戊-2-醇、{2-[4-(5-氟-2-甲基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚5-基}苯基甲酮、{2-[4-(5-氟-2-甲基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吡咯并[2,3-c]吡啶-5-基}苯基甲酮、{2-[4-(5-氟-2-甲基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚5-基}呋喃-2-基甲酮、{2-[4-(5-氟-2-甲基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吡咯并[2,3-c]吡啶-5-基}呋喃-2-基甲酮、1,1,1-三氟-2-(1H-吲哚-2-基甲基)-4-甲基-4-吡啶-2-基戊-2-醇、1,1,1-三氟-4-甲基-4-吡啶-4-基-2-喹啉-4-基甲基戊-2-醇、2-(2,6-二甲基吡啶-4-基甲基)-1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基戊-2-醇、2-[3-(2,6-二甲基吡啶-4-基甲基)-4,4,4-三氟-3-羥基-1,1-二甲基丁基]-4-氟酚、1,1,1-三氟-4,4-二甲基-5-苯基-2-喹啉-4-基甲基戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基-2-吡啶-4-基甲基戊-2-醇、4-氟-2-[4,4,4-三氟-3-(2-氟吡啶-4-基甲基)-3-羥基-1,1-二甲基丁基]酚、2-[3-(2-溴吡啶-4-基甲基)-4,4,4-三氟-3-羥基-1,1-二甲基丁基]-4-氟酚、2-(6,8-二甲基喹啉-4-基甲基)-1,1,1-三氟-4-(5-
氟-2-甲氧基-苯基)-4-甲基戊-2-醇、4-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]吡啶-2-甲腈、2,6-二氯-4-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]菸鹼腈、4-[4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]喹啉-2-醇、2,6-二氯-4-[4-(5-氟-2-羥基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]菸鹼腈、2-(2-氯-8-甲基喹啉-4-基甲基)-1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基戊-2-醇、2-(2,6-二氯喹啉-4-基甲基)-1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基戊-2-醇、2-[3-(2-氯-8-甲基喹啉-4-基甲基)-4,4,4-三氟-3-羥基-1,1-二甲基丁基]-4-氟酚、2-[3-(2,6-二氯喹啉-4-基甲基)-4,4,4-三氟-3-羥基-1,1-二甲基丁基]-4-氟酚、4-(2,3-二氫苯并呋喃-7-基)-2-(2,6-二甲基吡啶-4-基甲基)-1,1,1-三氟-4-甲基戊-2-醇、2-(2,6-二甲基吡啶-4-基甲基)-1,1,1-三氟-4-(3-氟苯基)-4-甲基戊-2-醇、2-(2,6-二甲基吡啶-4-基甲基)-1,1,1-三氟-4-(4-氟苯基)-4-甲基戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲基苯基)-4-甲基-2-喹啉-4-基甲基戊-2-醇、2-(2,6-二甲基吡啶-4-基甲基)-1,1,1-三氟-4-(5-氟-2-甲基苯基)-4-甲基戊-2-醇、2-(2,6-二甲基吡啶-4-基甲基)-1,1,1-三氟-4-甲基-4-間甲苯基戊-2-醇、1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基-2-(2-甲基喹啉-4-基甲基)戊-2-醇、4-氟-2-(4,4,4-三氟-3-羥基-1,1,1-二甲基-3-喹啉-4-基甲基丁基)酚、4-氟-2-[4,4,4-三氟-3-羥基-1,1-二甲基-3-(2-甲基喹啉-4-基甲基)丁基]酚、2-(2,6-二甲基吡啶-4-基甲基)-1,1,1-三氟-4-(4-氟-2-甲氧基苯基)-4-甲基戊-2-醇、
1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基-2-(7-甲基喹啉-4-基甲基)戊-2-醇、2-[3-(2,6-二甲基吡啶-4-基甲基)-4,4,4-三氟-3-羥基-1,1-二甲基丁基]-5-氟酚及2-(5,7-二甲基喹啉-4-基甲基)-1,1,1-三氟-4-(5-氟-2-甲氧基苯基)-4-甲基戊-2-醇。
於另一實施例中，該至少DIGRA具有式I，其中a)A係各自視需要獨立地經一至三個取代基取代之芳基或雜芳基，該等取代基獨立地係選自由C1至C5烷基、C2至C5烯基、C2至C5炔基、C1至C3烷醯基、C3至C8環烷基、雜環基、芳基、雜芳基、C1至C5烷氧基、C2至C5烯氧基、C2至C5炔氧基、芳氧基、醯基、C1至C5烷氧羰基、芳醯基、胺基羰基、烷胺基羰基、二烷胺基羰基、胺基羰氧基、C1至C5烷胺基羰氧基、C1至C5二烷胺基羰氧基、C1至C5烷醯基胺基、C1至C5烷氧羰基胺基、C1至C5烷基磺醯胺基、胺基磺醯基、C1至C5烷胺基磺醯基、C1至C5二烷胺基磺醯基、鹵素、羥基、羧基、氰基、三氟甲基、三氟甲氧基、硝基、胺基(其中氮原子視需要獨立地經C1至C5烷基或芳基單或二取代)、脲基(其中任一氮原子視需要獨立地經C1至C5烷基取代)、C1至C5烷硫基(其中硫原子視需要氧化以形成亞碸或碸)組成之群；b)R1及R2各自獨立地係氫或C1至C5烷基；c)R3係氫、C1至C8烷基、C2至C8烯基、C2至C8炔基、碳環、雜環基、芳基、雜芳基、碳環-C1至C8烷基、羧基、烷氧羰基、芳基-C1至C8烷基、芳基-C1至C8鹵烷基、雜環基-C1
至C8烷基、雜芳基-C1至C8烷基、碳環-C2至C8烯基、芳基-C2至C8烯基、雜環基-C2至C8烯基或雜芳基-C2至C8烯基，各者視需要獨立地經一至三個取代基取代，其中R3之各取代基獨立地係C1至C5烷基、C2至C5烯基、C2至C5炔基、C3至C8環烷基、苯基、C1至C5烷氧基、苯氧基、C1至C5烷醯基、芳醯基、C1至C5烷氧羰基、C1至C5烷醯氧基、胺基羰氧基、C1至C5烷胺基羰氧基、C1至C5二烷胺基羰氧基、胺基羰基、C1至C5烷胺基羰基、C1至C5二烷胺基羰基、C1至C5烷醯基胺基、C1至C5烷氧羰基胺基、C1至C5烷底磺醯胺基、C1至C5烷胺基磺醯基、C1至C5二烷胺基磺醯基、鹵素、羥基、羧基、氰基、側氧基、三氟甲基、硝基、胺基(其中氮原子視需要獨立地經C1至C5烷基單或二取代)、脲基(其中任一氮原子視需要獨立地經C1至C5烷基取代)、C1至C5烷硫基(其中硫原子視需要氧化以形成亞碸或碸)，其中R3不可為三氟甲基；d)B係C1至C5伸烷基、C2至C5伸烯基或C2至C5伸炔基，各者視需要獨立地經一至三個取代基取代，其中B之各取代基獨立地係C1至C3烷基、羥基、鹵素、胺基或側氧基；e)D不存在；f)E係羥基；及g)Q包括視需要獨立地經一至三個取代基取代之雜芳基，該等取代基獨立地係選自由C1至C5烷基、C2至C5烯基、C2至C5炔基、C1至C3烷醯基、C3至C8環烷基、雜環基、芳基、雜芳基、C1至C5烷氧基、C2至C5烯氧基、C2至C5炔氧
基、芳氧基、醯基、C1至C5烷氧羰基、芳醯基、胺基羰基、烷胺基羰基、二烷胺基羰基、胺基羰氧基、C1至C5烷胺基羰氧基、C1至C5二烷胺基羰氧基、C1至C5烷醯基胺基、C1至C5烷氧羰基胺基、C1至C5烷基磺醯胺基、胺基磺醯基、C1至C5烷胺基磺醯基、C1至C5二烷胺基磺醯基、鹵素、羥基、羧基、氰基、三氟甲基、三氟甲氧基、硝基、胺基(其中氮原子視需要獨立地經C1至C5烷基或芳基單或二取代)、脲基(其中任一氮原子視需要獨立地經C1至C5烷基取代)、C1至C5烷硫基(其中硫原子視需要氧化以形成亞碸或碸)組成之群，其中Q之各取代基係視需要經一至三個取代基取代，該等取代基選自由C1至C3烷基、C1至C3烷氧基、醯基、C1至C3矽烷氧基、C1至C5烷氧羰基、羧基、鹵素、羥基、側氧基、氰基、雜芳基、雜環基、胺基(其中氮原子視需要獨立地經C1至C5烷基或芳基單或二取代)、脲基(其中任一氮原子視需要獨立地經C1至C5烷基取代)或三氟甲基組成之群。
此等化合物之非限制性實例包括2-環丙基-4-(5-氟-2-甲氧基苯基)-4-甲基-1-(1H-吡咯并[3,2-c]吡啶-2-基)戊-2-醇、4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-(1H-吡咯并[2,3-c]吡啶-2-基甲基)戊酸、4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-(1H-吡咯并[2,3-c]吡啶-2-基甲基)戊酸甲基酯、2-環丙基-4-(5-氟-2-甲基苯基)-4-甲基-1-(1H-吡咯并[2,3-c]吡啶-2-基)戊-2-醇、4-(5-氯-2,3-二氫苯并呋喃-7-基)-2-環丙基-4-甲基-1-(1H-吡咯并[2,3-c]吡啶-2-基)戊-2-醇、2-環丙基
-4-(5-氟-2-甲基苯基)-4-甲基-1-(1H-吡咯并[3,2-c]吡啶-2-基)戊-2-醇、4-(5-氯-2,3-二氫苯并呋喃-7-基)-2-環丙基-4-甲基-1-(1H-吡咯并[3,2-c]吡啶-2-基)戊-2-醇、4-(5-氟-2-甲氧基苯基)-2,4-二甲基-1-(1H-吡咯并[2,3-c]吡啶-2-基)戊-2-醇、5-(5-氟-2-甲氧基苯基)-2,5-二甲基-3-(1H-吡咯并[2,3-c]吡啶-2-基甲基)己-3-醇、5-(5-氟-2-甲氧基苯基)-2,2,5-三甲基-3-(1H-吡咯并[2,3-c]吡啶-2-基甲基)己-3-醇、2-環己基-4-(5-氟-2-甲氯基苯基)-4-甲基-1-(1H-吡咯并[2,3-c]吡啶-2-基)戊-2-醇、2-環戊基-4-(5-氟-2-甲氧基苯基)-4-甲基-1-(1H-吡咯并[2,3-c]吡啶-2-基)戊-2-醇、5-(5-氟-2-甲氧基苯基)-5-甲基-3-(1H-吡咯并[2,3-c]吡啶-2-基甲基)己-3-醇、2-(5-氟-2-甲氧基苯基)-2,6-二甲基-4-(1H-吡咯并[2,3-c]吡啶-2-基甲基)庚-4-醇、2-(5-氟-2-甲氧基苯基)-2,5,5-三甲基-4-(1H-吡咯并[2,3-c]吡啶-2-基甲基)庚-4-醇、1,1-二氟-4-(5-氟-2-甲氧基苯基)-4-甲基-2-(1H-吡咯并[2,3-c]吡啶-2-基甲基)戊-2-醇、1-環己基-4-(5-氟-2-甲氧基苯基)-4-甲基-2-(1H-吡咯并[2,3-c]吡啶-2-基甲基)戊-2-醇、5-(5-氟-2-甲基苯基)-2,5-二甲基-3-(1H-吡咯并[2,3-c]吡啶-2-基甲基)己-3-醇、5-(5-氟-2-甲基苯基)-2,2,5-三甲基-3-(1H-吡咯并[2,3-c]吡啶-2-基甲基)己-3-醇、5-(5-氯-2,3-二氫苯并呋喃-7-基)-2,5-二甲基-3-(1H-吡咯并[2,3-c]吡啶-2-基甲基)己-3-醇、2-環丁基-4-(5-氟-2-甲氧基苯基)-4-甲基-1-(1H-吡咯并[2,3-c]吡啶-2-基)戊-2-醇、2-(5-氟-2-甲氧基苯基)-2,6,6-三甲基-4-(1H-吡咯并[2,3-c]吡啶-2-基甲基)庚-4-醇、5-(5-
氟-2-甲氧基苯基)-5-甲基-3-(1H-吡咯并[2,3-c]吡啶-2-基甲基)己-1-烯-3-醇、5-(5-氟-2-甲氧基苯基)-5-甲基-3-(1H-吡咯并[2,3-c]吡啶-2-基甲基)己-1-炔-3-醇、1-氟-4-(5-氟-2-甲氧基苯基)-4-甲基-2-(1H-吡咯并[2,3-c]吡啶-2-基甲基)戊-2-醇、2,2-二氟-5-(5-氟-2-甲氧基苯基)-5-甲基-3-(1H-吡咯并[2,3-c]吡啶-2-基甲基)己-3-醇、2-氟-5-(5-氟-2-甲氧基苯基)-2,5-二甲基-3-(1H-吡咯并[2,3-c]吡啶-2-基甲基)己-3-醇、2-氟-5-(5-氟-2-甲氧基苯基)-5-甲基-3-(1H-吡咯并[2,3-c]吡啶-2-基甲基)己-3-醇、5-(5-氟-2-甲氧基苯基)-2,5-二甲基-3-(1H-吡咯并[2,3-c]吡啶-2-基甲基)己-1-烯-3-醇、1,1,1-三氟-5-(5-氟-2-甲氧基苯基)-5-甲基-3-(1H-吡咯并[2,3-c]吡啶-2-基甲基)己-3-醇、4-(5-氟-2-甲氧基苯基)-4-甲基-2-苯基-1-(1H-吡咯并[2,3-c]吡啶-2-基)戊-2-醇、5-(5-氯-2,3-二氫苯并呋喃-7-基)-2,2,5-三甲基-3-(1H-吡咯并[2,3-c]吡啶-2-基甲基)己-3-醇、5-(5-氟-2-甲基苯基)-2,2,5-三甲基-3-噻吩并[2,3-c]吡啶-2-基甲基己-3-醇、1,1-二氟-4-(5-氟-2-甲氧基苯基)-4-甲基-2-(1H-吡咯并[3,2-c]吡啶-2-基甲基)戊-2-醇、5-(5-氟-2-甲氧基苯基)-2,5-二甲基-3-(1H-吡咯并[3,2-c]吡啶-2-基甲基)己-3-醇、5-(5-氟-2-甲氧基苯基)-2,2,5-三甲基-3-(1H-吡咯并[3,2-c]吡啶-2-基甲基)己-3-醇、2-(1-氟環丙基)-4-(5-氟-2-甲氧基苯基)-4-甲基-1-(1H-吡咯并[2,3-c]吡啶-2-基)戊-2-醇、2-(1-氟環丙基)-4-(4-氟苯基)-4-甲基-1-喹啉-4-基戊-2-醇、2-[4,4-二氟-3-羥基-1,1-二甲基-3-(1H-吡咯并[3,2-c]吡啶-2-基甲基)丁
基]-4-氟酚、5-(5-氯-2,3-二氫苯并呋喃-7-基)-2,5-二甲基-3-(1H-吡咯并[3,2-c]吡啶-2-基甲基)己-3-醇、5-(5-氟-2-甲基苯基)-2,5-二甲基-3-(1H-吡咯并[3,2-c]吡啶-2-基甲基)己-3-醇、5-(5-氟-2-甲基苯基)-2,2,5-三甲基-3-(1H-吡咯并[3,2-c]吡啶-2-基甲基)己-3-醇、4-(5-氯-2,3-二氫苯并呋喃-7-基)-1,1-二氟-4-甲基-2-(1H-吡咯并[3,2-c]吡啶-2-基甲基)戊-2-醇、4-(5-氯-2,3-二氫苯并呋喃-7-基)-1,1-二氟-4-甲基-2-吡咯并[3,2-b]吡啶-1-基甲基戊-2-醇、5-(5-氯-2,3-二氫苯并呋喃-7-基)-2,2,5-三甲基-3-(1H-吡咯并[3,2-c]吡啶-2-基甲基)己-3-醇、5-(5-氟-2-甲基苯基)-2,2,5-三甲基-3-(3-甲基-1H-吡咯并[2,3-c]吡啶-2-基甲基)己-3-醇、5-(5-氯-2,3-二氫苯并呋喃-7-基)-2,5-二甲基-3-(3-甲基-1H-吡咯并[2,3-c]吡啶-2-基甲基)己-3-醇、5-(5-氯-2,3-二氫苯并呋喃-7-基)-2,5-二甲基-3-(5-苯基-1H-吡咯并[2,3-c]吡啶-2-基甲基)己-3-醇、5-(5-氟-2-甲基苯基)-2,2,5-三甲基-3-(5-苯基-1H-吡咯并[2,3-c]吡啶-2-基甲基)己-3-醇、5-(5-氟-2-甲基苯基)-2,5-二甲基-3-(5-苯基-1H-吡咯并[2,3-c]吡啶-2-基甲基)己-3-醇、5-(5-氟-2-甲基苯基)-5-甲基-3-(5-苯基-1H-吡咯并[2,3-c]吡啶-2-基甲基)己-3-醇、4-(5-氟-2-甲基苯基)-2,4-二甲基-1-(5-苯基-1H-吡咯并[2,3-c]吡啶-2-基)戊-2-醇、4-(5-氯-2,3-二氫苯并呋喃-7-基)-1,1-二氟-4-甲基-2-(6-甲基-1H-吡咯并[3,2-c]吡啶-2-基甲基)戊-2-醇、5-(5-氟-2-甲基苯基)-2,5-二甲基-3-(5-吡啶-3-基-1H-吡咯并[2,3-c]吡啶-2-基甲基)己-3-醇、5-(5-氯-2,3-二氫苯并呋喃
-7-基)5-甲基-3-(5-苯基-1H-吡咯并[2,3-c]吡啶-2-基甲基)己-3-醇、4-(5-氯-2,3-二氫苯并呋喃-7-基)-2,4-二甲基-1-(5-苯基-1H-吡咯并[2,3-c]吡啶-2-基)戊-2-醇、1,1-二氟-4-(5-甲烷磺醯基-2,3-二氫苯并呋喃-7-基)-4-甲基-2-(1H-吡咯并[2,3-c]吡啶-2-基甲基)戊-2-醇、5-(5-氯-2,3-二氫苯并呋喃-7-基)-2,5-二甲基-3-(5-吡啶-3-基-1H-吡咯并[2,3-c]吡啶-2-基甲基)己-3-醇、2-(5-溴-1H-吲哚-2-基甲基)-1,1-二氟-4-(5-甲烷磺醯基-2,3-二氫苯并呋喃-7-基)-4-甲基戊-2-醇、及2-[2-二氟甲基-2-羥基-4-(5-甲烷磺醯基-233-二氫苯并呋喃-7-基)-4-甲基戊基]-4-甲基-1H-吲哚-6-甲腈。
於另一實施例中，該至少DIGRA具有式I，其中a)A係各自視需要獨立地經一至三個取代基取代之芳基或雜芳基，該等取代基獨立地係選自由C1至C5烷基、C2至C5烯基、C2至C5炔基、C1至C3烷醯基、C3至C8環烷基、雜環基、芳基、雜芳基、C1至C5烷氧基、C2至C5烯氧基、C2至C5炔氧基、芳氧基、醯基、C1至C5烷氧羰基、芳醯基、胺基羰基、烷胺基羰基、二烷胺基羰基、胺基羰氧基、C1至C5烷胺基羰氧基、C1至C5二烷胺基羰氧基、C1至C5烷醯基胺基、C1至C5烷氧羰基胺基、C1至C5烷基磺醯胺基、胺基磺醯基、C1至C5烷胺基磺醯基、C1至C5二烷胺基磺醯基、鹵素、羥基、羧基、氰基、三氟甲基、三氟甲氧基、硝基、胺基(其中氮原子視需要獨立地經C1至C5烷基或芳基單或二取代)、脲基(其中任一氮原子視需要獨立地經C1至C5烷基取代)、C1至C5烷硫基(其中硫原子視需要氧化以形成亞碸或
碸)組成之群；b)R1及R2各自獨立地係C1至C5烷基，其中一或兩者獨立地經羥基、C1至C5烷氧基、C1至C5烷硫基(其中硫原子視需要氧化以形成亞碸或碸)、胺基(其中氮原子視需要獨立地經C1至C5烷基或芳基單-或二取代)取代；c)R3係氫、C1至C8烷基、C2至C8烯基、C2至C8炔基、碳環、雜環基、芳基、雜芳基、碳環-C1至C8烷基、羧基、烷氧羰基、芳基-C1至C8烷基、芳基-C1至C8鹵烷基、雜環基-C1至C8烷基、雜芳基-C1至C8烷基、碳環-C2至C8烯基、芳基-C2至C8烯基、雜環基-C2至C8烯基或雜芳基-C2至C8烯基，各者視需要獨立地經一至三個取代基取代，其中R3之各取代基獨立地係C1至C5烷基、C2至C5烯基、C2至C5炔基、C3至C8環烷基、苯基、C1至C5烷氧基、苯氧基、C1至C5烷醯基、芳醯基、C1至C5烷氧羰基、C1至C5烷醯氧基、胺基羰氧基、C1至C5烷胺基羰氧基、C1至C5二烷胺基羰氧基、胺基羰基、C1至C5烷胺基羰基、C1至C5二烷胺基羰基、C1至C5烷醯基胺基、C1至C5烷氧羰基胺基、C1至C5烷基磺醯胺基、C1至C5烷胺基磺醯基、C1至C5二烷胺基磺醯基、鹵素、羥基、羧基、氰基、側氧基、三氟甲基、硝基、胺基(其中氮原子視需要獨立地經C1至C5烷基單或二取代)、脲基(其中任一氮原子視需要獨立地經C1至C5烷基取代)、C1至C5烷硫基(其中硫原子視需要氧化以形成亞碸或碸)；d)B係C1至C5伸烷基、C2至C5伸烯基或C2至C5伸炔基，各者視需要獨立地經一至三個取代基取代，其中B之各取代
基獨立地係C1至C3烷基、羥基、鹵素、胺基或側氧基；e)D不存在；f)E係羥基；及g)Q包括視需要獨立地經一至三個取代基取代之雜芳基，該等取代基獨立地係選自由C1至C5烷基、C2至C5烯基、C2至C5炔基、C1至C3烷醯基、C3至C8環烷基、雜環基、芳基、雜芳基、C1至C5烷氧基、C2至C5烯氧基、C2至C5炔氧基、芳氧基、醯基、C1至C5烷氧羰基、芳醯基、胺基羰基、烷胺基羰基、二烷胺基羰基、胺基羰氧基、C1至C5烷胺基羰氧基、C1至C5二烷胺基羰氧基、C1至C5烷醯基胺基、C1至C5烷氧羰基胺基、C1至C5烷基磺醯胺基、胺基磺醯基、C1至C5烷胺基磺醯基、C1至C5二烷胺基磺醯基、鹵素、羥基、羧基、氰基、三氟甲基、三氟甲氧基、硝基、胺基(其中氮原子視需要獨立地經C1至C5烷基或芳基單或二取代)、脲基(其中任一氮原子視需要獨立地經C1至C5烷基取代)、C1至C5烷硫基(其中硫原子視需要氧化以形成亞碸或碸)組成之群，其中Q之各取代基係視需要經一至三個取代基取代，該等取代基選自由C1至C3烷基、C1至C3烷氧基、醯基、C1至C3矽烷氧基、C1至C5烷氧羰基、羧基、鹵素、羥基、側氧基、氰基、雜芳基、雜環基、胺基(其中氮原子視需要獨立地經C1至C5烷基或芳基單或二取代)、脲基(其中任一氮原子視需要獨立地經C1至C5烷基取代)或三氟甲基組成之群。
於另一實施例中，該至少DIGRA具有式I，其中
a)A係芳基、雜芳基、雜環基或C3至C8環烷基，各者視需要獨立地經一至三個取代基取代，該等取代基獨立地選自由C1至C5烷基、C2至C5烯基、C2至C5炔基、C1至C3烷醯基、C3至C8環烷基、雜環基、芳基、雜芳基、C1至C5烷氧基、C2至C5烯氧基、C2至C5炔氧基、芳氧基、醯基、C1至C5烷氧羰基、芳醯基、胺基羰基、烷胺基羰基、二烷胺基羰基、胺基羰氧基、C1至C5烷胺基羰氧基、C1至C5二烷胺基羰氧基、C1至C5烷醯基胺基、C1至C5烷氧羰基胺基、C1至C5烷基磺醯胺基、胺基磺醯基、C1至C5烷胺基磺醯基、C1至C5二烷胺基磺醯基、鹵素、羥基、羧基、氰基、三氟甲基、三氟甲氧基、硝基、胺基(其中氮原子視需要獨立地經C1至C5烷基或芳基單或二取代)、脲基(其中任一氫原子視需要獨立地經C1至C5烷基取代)、C1至C5烷硫基(其中硫原子視需要氧化以形成亞碸或碸)組成之群；b)R1及R2各自獨立地係氫、C1至C5烷基、C5至C15芳烷基，或R1及R2藉由其等共同連接之碳原子一起形成C3至C8螺環烷基環；c)B係羰基或亞甲基，其視需要獨立地經一或兩個取代基取代，該等取代基選自由C1至C3烷基、羥基及鹵素組成之群；d)R3係三氟甲基；e)D不存在；f)E係羥基或胺基，其中氮原子視需要獨立經C1至C5烷基單-或二-取代；及
g)Q包括5-至7-員雜環基與5-至7-員雜芳基或雜環基環之稠合環，各者視需要獨立地經一至三個取代基取代，其中Q之各取代基獨立地係C1至C5烷基、C2至C5烯基、C2至C5炔基、C3至C8環烷基、雜環基、芳基、雜芳基、C1至C5烷氧基、C2至C5烯氧基、C2至C5炔氧基、芳氧基、醯基、C1至C5烷氧羰基、C1至C5烷醯氧基、胺基羰基、烷胺基羰基、二烷胺基羰基、胺基羰氧基、C1至C5烷胺基羰氧基、C1至C5二烷胺基羰氧基、C1至C5烷醯基胺基、C1至C5烷氧羰基胺基、C1至C5烷基磺醯胺基、C1至C5烷胺基磺醯基、C1至C5二烷胺基磺醯基、鹵素、羥基、羧基、側氧基、氰基、三氟甲基、三氟甲氧基、三氟甲硫基、硝基、胺基(其中氮原子視需要獨立地經C1至C5烷基單或二取代)、脲基(其中任一氮原子視需要獨立地經C1至C5烷基取代)、C1至C5烷硫基(其中硫原子視需要氧化以形成亞碸或碸)，其中Q之各取代基視需要獨立地經一或三個取代基取代，該等取代基選自由C1至C3烷基、C1至C3烷氧基、C1至C3烷氧羰基、醯基、芳基、苄基、雜芳基、雜環基、鹵素、羥基、側氧基、氰基、胺基(其中氮原子視需要獨立地經C1至C5烷基單-或二-取代)及脲基(其中任一氮原子視需要獨立地經C1至C5烷基取代)或三氟甲基組成之群，其中Q不可為1H-[1,5]萘啶-4-酮。
此等化合物之非限制性實例包括4-[4-(5-氟-2-甲氧苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-4H-噻吩并[3,2-b]吡啶-7-酮、4-[4-(5-氟-2-羥基苯基)-2-羥基-4-甲基-2-三氟甲基
戊基]-4H-噻吩并[3,2-b]吡啶-7-酮、4-[4-(2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-4H-噻吩并[3,2-b]吡啶-7-酮、1-[4-(5-氟-2-甲氧苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-[1,6]萘啶-4-酮、1-[4-(5-氟-2-羥基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-[1,6]萘啶-4-酮、4-[4-(5-氟-2-甲基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-4H-噻吩并[3,2-b]吡啶-7-酮、4-[2-羥基-4-(5-甲磺醯基-2,3-二氫苯并呋喃-7-基)-4-甲基-2-三氟甲基戊基]-4H-噻吩并[3,2-b]吡啶-7-酮、1-[2-羥基-4-(5-甲磺醯基-2,3-二氫苯并呋喃-7-基)-4-甲基-2-三氟甲基戊基]-1H-[1,6]萘啶-4-酮、1-[4-(5-氟-2-甲基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-[1,6]萘啶-4-酮、4-[2-羥基-4-(2-甲氧基-3-甲基苯基)-4-甲基-2-三氟甲基戊基]-4H-噻吩并[3,2-b]吡啶-7-酮、4-[2-羥基-4-(2-甲氧苯基)-4-甲基-2-三氟甲基戊基]-4H-噻吩并[3,2-b]吡啶-7-酮、4-[4-(3-溴-2-甲氧苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-4H-噻吩并[3,2-b]吡啶-7-酮、4-[2-羥基-4-(2-羥基-3-甲基苯基)-4-甲基-2-三氟甲基戊基]-4H-噻吩并[3,2-b]吡啶-7-酮、4-[4-(3-溴-2-羥基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-4H-噻吩并[3,2-b]吡啶-7-酮、3-溴-1-[4-(5-氯-2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-[1,6]萘啶-4-酮、6-氯-4-[4-(2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-4H-噻吩并[3,2-b]吡啶-7-酮、6-溴-4-[4-(2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-4H-噻吩并[3,2-b]吡啶-7-酮、3-氯-1-[4-(5-氟-2-羥基
苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-[1,6]萘啶-4-酮、1-[4-(5-氯-2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-3-甲基-1H-[1,6]萘啶-4-酮、1-[4-(5-氯-2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-3-甲基-1H-[1,7]萘啶-4-酮、1-[2-羥基-4-(2-甲氧基-3,5-二甲基苯基)-4-甲基-2-三氟甲基戊基]-3-甲基-1H-[1,6]萘啶-4-酮、1-[2-羥基-4-(2-甲氧基-3,5-二甲基苯基)-4-甲基-2-三氟甲基戊基]-3-甲基-1H-[1,7]萘啶-4-酮、1-[2-羥基-4-(2-羥基-3,5-二甲基苯基)-4-甲基-2-三氟甲基戊基]-3-甲基-1H-[1,6]萘啶-4-酮、1-[4-(5-氟-2-甲基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-[1,8]萘啶-4-酮、1-[4-(5-氟-2-甲基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-[1,7]萘啶-4-酮、4-[4-(5-氟-2-羥基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-4H-噻唑并[4,5-b]吡啶-7-酮、4-[4-(5-氟-2-羥基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-4H-噁唑并[4,5-b]吡啶-7-酮、4-[4-(5-氟-2-甲基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-4H-呋喃并[3,2-b]吡啶-7-酮、7-[4-(5-氟-2-甲基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-7H-噻吩并[2,3-b]吡啶-4-酮、4-[4-(5-氟-2-羥基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-4H-噁唑并[5,4-b]吡啶-7-酮、4-[4-(5-氟-2-羥基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-4H-噻唑并[5,4-b]吡啶-7-酮、7-[4-(5-氟-2-甲基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-7H-呋喃并[2,3-b]吡啶-4-酮、4-[4-(5-氟-2-甲基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1,4-二氫吡咯并[3,2-b]吡啶
-7-酮、1-[4-(5-氟-2-羥基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-5,6,7,8-四氫-1H-[1,6]萘啶-4-酮、1-[4-(5-氟-2-甲基苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-6-甲基-5,6,7,8-四氫-1H-[1,6]萘啶-4-酮、1-[4-(2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-[1,8]萘啶-4-酮、1-[2-羥基-4-(5-甲磺醯基-2,3-二氫苯并呋喃-7-基)-4-甲基-2-三氟甲基戊基]-1H-[1,7]萘啶-4-酮、4-[2-羥基-4-(5-甲磺醯基-2,3-二氫苯并呋喃-7-基)-4-甲基-2-三氟甲基戊基]-4-H-噻唑并[4,5-b]吡啶-7-酮、4-[4-(2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-4H-噁唑并[4,5-b]吡啶-7-酮、4-[2-羥基-4-(5-甲磺醯基-2,3-二氫苯并呋喃-7-基)-4-甲基-2-三氟甲基戊基]-4H-呋喃并[3,2-b]吡啶-7-酮、7-[4-(2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-7H-噻吩并[2,3-b]吡啶-4-酮、4-[2-羥基-4-(5-甲磺醯基-2,3-二氫苯并呋喃-7-基)-4-甲基-2-三氟甲基戊基]-4H-噁唑并[5,4-b]吡啶-7-酮、4-[2-羥基-4-(5-甲磺醯基-2,3-二氫苯并呋喃-7-基)-4-甲基-2-三氟甲基戊基]-4H-噻唑并[5,4-b]吡啶-7-酮、7-[4-(2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-7H-呋喃并[2,3-b]吡啶-4-酮、4-[4-(2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-1,4-二氫吡咯并[3,2-b]吡啶-7-酮、1-[2-羥基-4-(5-甲磺醯基-2,3-二氫苯并呋喃-7-基)-4-甲基-2-三氟甲基戊基]-5,6,7,8-四氫-1H-[1,6]萘啶-4-酮、1-[4-(2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-6-甲基-5,6,7,8-四氫-1H-[1,6]萘啶-4-酮、
1-[4-(2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-5-甲基-5,6,7,8-四氫-1H-[1,5]萘啶-4-酮、1-[4-(2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-5-甲基-5,6,7,8-四氫-1H-[1,5]萘啶-4-酮、4-[2-羥基-4-(4-甲氧基聯苯-3-基)-4-甲基-2-三氟甲基戊基]-4H-噻吩并[3,2-b]吡啶-7-酮、4-[2-羥基-4-(2-甲氧基-5-吡啶-3-基苯基)-4-甲基-2-三氟甲基戊基]-4H-噻吩并[3,2-b]吡啶-7-酮、4-[2-羥基-4-(2-甲氧基-5-嘧啶-5-基苯基)-4-甲基-2-三氟甲基戊基]-4H-噻吩并[3,2-b]吡啶-7-酮、4-[2-羥基-4-(2-甲氧基-5-噻吩-3-基苯基)-4-甲基-2-三氟甲基戊基]-4H-噻吩并[3,2-b]吡啶-7-酮、4-[2-羥基-4-(4-羥基聯苯-3-基)-4-甲基-2-三氟甲基戊基]-4H-噻吩并[3,2-b]吡啶-7-酮、4-[2-羥基-4-(2-羥基-5-吡啶-3-基苯基)-4-甲基-2-三氟甲基戊基]-4H-噻吩并[3,2-b]吡啶-7-酮、4-[2-羥基-4-(2-羥基-5-嘧啶-5-基苯基)-4-甲基-2-三氟甲基戊基]-4H-噻吩并[3,2-b]吡啶-7-酮、4-[2-羥基-4-(2-羥基-5-噻吩-3-基苯基)-4-甲基-2-三氟甲基戊基]-4H-噻吩并[3,2-b]吡啶-7-酮、1-[2-羥基-4-(4-甲氧基聯苯-3-基)-4-甲基-2-三氟甲基戊基]-1H-[1,6]萘啶-4-酮、1-[2-羥基-4-(2-甲氧基-5-吡啶-3-基苯基)-4-甲基-2-三氟甲基戊基]-1H-[1,5]萘啶-4-酮、1-[2-羥基-4-(2-甲氧基-5-嘧啶-5-基苯基)-4-甲基-2-三氟甲基戊基]-1H-[1,6]萘啶-4-酮、1-[2-羥基-4-(2-甲氧基-5-噻吩-3-基苯基)-4-甲基-2-三氟甲基戊基]-1H-[1,6]萘啶-4-酮、1-[2-羥基-4-(2-甲氧基-5-噻吩-3-基苯基)-4-甲基-2-三氟甲基戊基]-1H-[1,6]萘啶-4-酮、1-[2-
羥基-4-(2-羥基-5-吡啶-3-基苯基)-4-甲基-2-三氟甲基戊基]-1H-[1,6]萘啶-4-酮、1-[2-羥基-4-(2-羥基-5-嘧啶-5-基苯基)-4-甲基-2-三氟甲基戊基]-1H-[1,6]萘啶-4-酮、1-[2-羥基-4-(2-羥基-5-噻吩-3-基苯基)-4-甲基-2-三氟甲基戊基]-1H-[1,6]萘啶-4-酮、5-[4-(5-氟-2-甲氧苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-5H-吡啶并[3,2-d]嘧啶-8-酮、1-[4-(5-氟-2-甲氧苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吡啶并[2,3-d]噠嗪-4-酮、5-[4-(5-氟-2-甲氧苯基)-2-羥基-4-甲基-2-三氟甲基戊基]-5H-吡啶并[3,2-c]噠嗪-8-酮、4-[4-(2-二氟甲氧基-3-甲基苯基-)-2-羥基-4-甲基-2-三氟甲基戊基]-4H-噻吩并[3,2-b]吡啶-7-酮、3-氯-1-[4-(2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-[1,6]萘啶-4-酮、4-(4-苯并[1,3]二氧雜環戊烯-4-基-2-羥基-4-甲基-2-三氟甲基戊基)-6-溴-4H-噻吩并[3,2-b]吡啶-7-酮、4-(4-苯并[1,3]二氧雜環戊烯-4-基-2-羥基-4-甲基-2-三氟甲基戊基)-6-氯-4H-噻吩并[3,2-b]吡啶-7-酮、6-氯-4-[2-羥基-4-甲基-4-(5-吡啶-3-基-2,3-二氫苯并呋喃-7-基)-2-三氟甲基戊基]-4H-噻吩并[3,2-b]吡啶-7-酮、1-(4-苯并[1,3]二氧雜環戊烯-4-基-2-羥基-4-甲基-2-三氟甲基戊基)-3-氯-1H-[1,6]萘啶-4-酮、6-氯-4-[2-羥基-4-甲基-4-(5-嘧啶-5-基-2,3-二氫苯并呋喃-7-基)-2-三氟甲基戊基]-4H-噻吩并[3,2-b]吡啶-7-酮、3-氯-1-[2-羥基-4-甲基-4-(5-嘧啶-5-基-2,3-二氫苯并呋喃-7-基)-2-三氟甲基戊基]-1H-[1,6]萘啶-4-酮、3-氯-1-[2-羥基-4-甲基-4-(5-吡啶-3-基-2,3-二氫
苯并呋喃-7-基)-2-三氟甲基戊基]-1H-[1,6]萘啶-4-酮、4-[2-羥基-4-甲基-4-(5-嘧啶-5-基-2,3-二氫苯并呋喃-7-基)-2-三氟甲基戊基]-4H-噻吩并[3,2-b]吡啶-7-酮、1-[2-羥基-4-甲基-4-(5-嘧啶-5-基-2,3-二氫苯并呋喃-7-基)-2-三氟甲基戊基]-1H-[1,6]萘啶-4-酮、6-氯-4-[2-羥基-4-(2-甲氧基-5-吡啶-3-基苯基)-4-甲基-2-三氟甲基戊基]-4H-噻吩并[3,2-b]吡啶-7-酮、6-氯-4-[2-羥基-4-(2-甲氧基-5-嘧啶-5-基苯基)-4-甲基-2-三氟甲基戊基]-4H-噻吩并[3,2-b]吡啶-7-酮、6-氯-4-[2-羥基-4-(2-羥基-5-吡啶-3-基苯基)-4-甲基-2-三氟甲基戊基]-4H-噻吩并[3,2-b]吡啶-7-酮、6-氯-4-[2-羥基-4-(-2-羥基-5-嘧啶-5-基苯基)-4-甲基-2-三氟甲基戊基]-4H-噻吩并[3,2-b]吡啶-7-酮、4-(4-聯苯-3-基-2-羥基-4-甲基-2-三氟-甲基戊基)-6-氯-4H-噻吩并[3,2-b]吡啶-7-酮、4-(4-聯苯-3-基-2-羥基-4-甲基-2-三氟甲基戊基)-4H-噻吩并[3,2-b]吡啶-7-酮、3-氯-1-{4-[5-(5-氯吡啶-3-基)-2,3-二氫苯并呋喃-7-基]-2-羥基-4-甲基-2-三氟甲基戊基}-1H-[1,6]萘啶-4-酮、6-氯-4-{4-[5-(2,6-二甲基吡啶-4-基)-2-甲氧苯基]-2-羥基-4-甲基-2-三氟甲基戊基}-4H-噻吩并[3,2-b]吡啶-7-酮、4-[2-羥基-4-(2-羥基-5-吡啶-2-基苯基)-4-甲基-2-三氟甲基戊基]-4H-噻吩并[3,2-b]吡啶-7-酮、6-氯-4-[2-羥基-4-甲基-4-(5-吡嗪-2-基-2,3-二氫苯并呋喃-7-基)-2-三氟甲基戊基]-4H-噻吩并[3,2-b]吡啶-7-酮、3-氯-1-[2-羥基-4-甲基-4-(5-嘧啶-2-基-2,3-二氫苯并呋喃-7-基)-2-三氟甲基戊基]-1H-[1,6]萘啶-4-酮、5-{7-[3-(6-氯-7-側氧基-7H-噻吩并
[3,2-b]吡啶-4-基甲基)-4,4,4-三氟-3-羥基-1,1-二甲基丁基]-2,3-二氫苯并呋喃-5-基}菸鹼腈、4-{4-甲氧基-3-[4,4,4-三氟-3-羥基-1,1-二甲基-3-(7-側氧基-7H-噻吩并[3,2-b]吡啶-4-基甲基)丁基]苯基}吡啶-2-甲腈、6-氯-4-{4-[5-(2-氟-6-甲基吡啶-4-基)-2-甲氧苯基]-2-羥基-4-甲基-2-三氟甲基戊基}-4H-噻吩并[3,2-b]吡啶-7-酮、3-氯-1-{2-羥基-4-[5-(1H-哚唑-4-基)-2,3-二氫苯并呋喃-7-基]-4-甲基-2-三氟甲基戊基}-1H-[1,6]萘啶-4-酮、6-氯-4-[2-羥基-4-甲基-4-(5-嗎啉-4-基-2,3-二氫苯并呋喃-7-基)-2-三氟甲基戊基]-4H-噻吩并[3,2-b]吡啶-7-酮、及1-[2-羥基-4-甲基-4-(5-哌啶-1-基-2,3-二氫苯并呋喃-7-基)-2-三氟甲基戊基]-1H-[1,6]萘啶-4-酮。
於另一實施例中，該至少DIGRA具有式I，其中A、B、D、E、R1及R2具有以上揭示之含義，及R3係氫、C1至C8烷基、C2至C8烯基、C2至C8炔基、碳環、雜環基、芳基、雜芳基、碳環-C1至C8烷基、羧基、烷氧羰基、芳基-C1至C8烷基、芳基-C1至C8鹵烷基、雜環基-C1至C8烷基、雜芳基-C1至C8烷基、碳環-C2至C8烯基、芳基-C2至C8烯基、雜環基-C2至C8烯基或雜芳基-C2至C8烯基，各者視需要獨立地經一至三個取代基取代，其中R3之各取代基獨立地係C1至C5烷基、C2至C5烯基、C2至C5炔基、C3至C8環烷基、苯基、C1至C5烷氧基、苯氧基、C1至C5烷醯基、芳醯基、C1至C5烷氧羰基、C1至C5烷醯氧基、胺基羰氧基、C1至C5烷胺基羰氧基、C1至C5二烷胺基羰氧基、胺基羰基、C1至C5烷胺基羰基、C1
至C5二烷胺基羰基、C1至C5烷醯基胺基、C1至C5烷氧羰基胺基、C1至C5烷基磺醯胺基、C1至C5烷胺基磺醯基、C1至C5二烷胺基磺醯基、鹵素、羥基、羧基、氰基、側氧基、三氟甲基、硝基、胺基(其中氮原子視需要獨立地經C1至C5烷基單或二取代)、脲基(其中任一氮原子視需要獨立地經C1至C5烷基取代)、C1至C5烷硫基(其中硫原子視需要氧化以形成亞碸或碸)，其中R3不可係三氟甲基。
於另一實施例中，該至少DIGRA具有式I，其中a)A係芳基、雜芳基、雜環基或C3至C8環烷基，各者視需要獨立地經一至三個取代基取代，該等取代基獨立地選自由C1至C5烷基、C2至C5烯基、C2至C5炔基、C1至C3烷醯基、C3至C8環烷基、雜環基、芳基、雜芳基、C1至C5烷氧基、C2至C5烯氧基、C2至C5炔氧基、芳氧基、醯基、C1至C5烷氧羰基、芳醯基、胺基羰基、烷胺基羰基、二烷胺基羰基、胺基羰氧基、C1至C5烷胺基羰氧基、C1至C5二烷胺基羰氧基、C1至C5烷醯基胺基、C1至C5烷氧羰基胺基、C1至C5烷基磺醯胺基、胺基磺醯基、C1至C5烷胺基磺醯基、C1至C5二烷胺基磺醯基、鹵素、羥基、羧基、氰基、三氟甲基、三氟甲氧基、硝基、胺基(其中氮原子視需要獨立地經C1至C5烷基或芳基單或二取代)、脲基(其中任一氮原子視需要獨立地經C1至C5烷基取代)、C1至C5烷硫基(其中硫原子視需要氧化以形成亞碸或碸)組成之群；b)R1及R2各自獨立地係氫或C1至C5烷基；c)R3係三氟甲基；
d)B係C1至C5伸烷基、C2至C5伸烯基或C2至C5伸炔基，各者視需要獨立地經一至三個取代基取代，其中B之各取代基獨立地係C1至C3烷基、羥基、鹵素、胺基或側氧基；e)D不存在；f)E係羥基；及g)Q包括視需要獨立地經一至三個取代基取代之吲哚基，該等取代基獨立地係選自由C1至C5烷基、C2至C5烯基、C2至C5炔基、C3至C8環烷基、雜環基、芳基、雜芳基、C1至C5烷氧基、C2至C5烯氧基、C2至C5炔氧基、芳氧基、醯基、C1至C5烷氧羰基、C1至C5烷醯氧基、胺基羰基、烷胺基羰基、二烷胺基羰基、胺基羰氧基、C1至C5烷胺基羰氧基、C1至C5二烷胺基羰氧基、C1至C5烷醯基胺基、C1至C5烷氧羰基胺基、C1至C5烷基磺醯胺基、胺基磺醯基、C1至C5烷胺基磺醯基、C1至C5二烷胺基磺醯基、鹵素、羥基、羧基、氰基、三氟甲基、三氟甲氧基、三氟甲硫基、硝基、胺基(其中氮原子視需要獨立地經C1至C5烷基單或二取代)、脲基(其中任一氮原子視需要獨立地經C1至C5烷基取代)、或C1至C5烷硫基(其中硫原子視需要氧化以形成亞碸或碸)組成之群，其中Q之各取代基係視需要經一至三個取代基取代，該等取代基選自由C1至C3烷基、C1至C3烷氧基、鹵素、羥基、側氧基、氰基、胺基及三氟甲基組成之群。
此等化合物之非限制性實例包括4-(5-溴-2,3-二氫苯并呋喃-7-基)-1,1,1-三氟-2-(1H-吲哚-2-基甲基)-4-甲基戊-2-醇、1,1,1-三氟-2-(1H-吲哚-2-基甲基)-4-甲基-4-吡啶-2-基戊-2-
醇、4-(2,3-二氫-5-氰基苯并呋喃-7-基)-1,1,1-三氟-2-(1H-吲哚-2-基-甲基)-4-甲基戊-2-醇、4-(2,3-二氫苯并呋喃-7-基)-1,1,1-三氟-2-(1H-吲哚-2-基甲基)-4-甲基戊-2-醇、1,1,1-三氟-4-(5-氟-2,3-二氫苯并呋喃-7-基)-2-(1H-吲哚-2-基甲基)-4-甲基戊-2-醇、1,1,1-三氟-2-(1H-吲哚-2-基甲基)-4-甲基-4-(5-甲基-2,3-二氫苯并呋喃-7-基)戊-2-醇、4-(2,3-二氫苯并呋喃-5-基)-1,1,1-三氟-2-(1H-吲哚-2-基甲基)-4-甲基戊-2-醇、2-[4-(2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚-3-甲腈、2-[4-(5-氟-2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚-3-甲腈、2-[4-(5-溴-2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚-3-甲腈、2-[4-(2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-4-甲基-1H-吲哚-6-甲腈、2-[4-(2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚-5-甲腈、4-(2,3-二氫苯并呋喃-7-基)-1,1,1-三氟-2-(7-氟-1H-吲哚-2-基甲基)4-甲基戊-2-醇、1-[4-(2,3-二氫苯并呋喃-7-基)-2-羥基-4-甲基-2-三氟甲基戊基]-1H-吲哚-3-甲腈、4-(2,3-二氫苯并呋喃-7-基)-1,1,1-三氟-4-甲基-2-(5-三氟甲基-1H-吲哚-2-基甲基)戊-2-醇、及1,1,1-三氟-2-(1H-吲哚-2-基甲基)-4-甲基-4-噻吩-3-基戊-2-醇。
於另一實施例中，該至少DIGRA具有式I，其中a)A係芳基或雜芳基，各者視需要獨立地經一至三個取代基取代，該等取代基獨立地選自由C1至C5烷基、C2至C5
烯基、C2至C5炔基、C1至C3烷醯基、C3至C8環烷基、雜環基、芳基、雜芳基、C1至C5烷氧基、C2至C5烯氧基、C2至C5炔氧基、芳氧基、醯基、C1至C5烷氧羰基、芳醯基、胺基羰基、烷胺基羰基、二烷胺基羰基、胺基羰氧基、C1至C5烷胺基羰氧基、C1至C5二烷胺基羰氧基、C1至C5烷醯基胺基、C1至C5烷氧羰基胺基、C1至C5烷基磺醯胺基、胺基磺醯基、C1至C5烷胺基磺醯基、C1至C5二烷胺基磺醯基、鹵素、羥基、羧基、氰基、三氟甲基、三氟甲氧基、硝基、胺基(其中氮原子視需要獨立地經C1至C5烷基或芳基單或二取代)、脲基(其中任一氮原子視需要獨立地經C1至C5烷基取代)、C1至C5烷硫基(其中硫原子視需要氧化以形成亞碸或碸)組成之群；b)R1及R2各自獨立地係氫或C1至C5烷基，或R1及R2藉由其等共同連接之碳原子一起形成C3至C8螺環烷基環；c)R3係碳環、雜環基、芳基、雜芳基、碳環-C1至C8烷基、羧基、烷氧羰基、芳基-C1至C8烷基、芳基-C1至C8鹵烷基、雜環基-C1至C8烷基、雜芳基-C1至C8烷基、碳環-C2至C8烯基、芳基-C2至C8烯基、雜環基-C2至C8烯基或雜芳基-C2至C8烯基，各者視需要獨立地經一至三個取代基取代，其中R3之各取代基獨立地係C1至C5烷基、C2至C5烯基、C2至C5炔基、C3至C8環烷基、苯基、C1至C5烷氧基、苯氧基、C1至C5烷醯基、芳醯基、C1至C5烷氧羰基、C1至C5烷醯氧基、胺基羰氧基、C1至C5烷胺基羰氧基、C1至C5二烷胺基羰氧基、胺基羰基、C1至C5烷胺基羰基、C1至C5二烷胺基羰基、
C1至C5烷醯基胺基、C1至C5烷氧羰基胺基、C1至C5烷基磺醯胺基、C1至C5烷胺基磺醯基、C1至C5二烷胺基磺醯基、鹵素、羥基、羧基、氰基、側氧基、三氟甲基、硝基、胺基(其中氮原子視需要獨立地經C1至C5烷基單或二取代)、脲基(其中任一氮原子視需要獨立地經C1至C5烷基取代)、C1至C5烷硫基(其中硫原子視需要氧化以形成亞碸或碸)；d)B係亞甲基或羰基；e)E係-NH-基團；f)E係羥基；及g)Q包括基團
此等化合物之非限制性實例包括2-苄基-2-羥基-4-甲基-4-苯基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-羥基-4-甲基-2,4-二苯基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-羥基-4-甲基-2-苯乙基-4-苯基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-羥基-2-(3-甲氧基苄基)4-甲基-4-苯基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-羥基-2-(4-甲氧基苄基)-4-甲基-4-苯基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-羥基-2-[2-(4-甲氧基苯基)乙基]4-甲基-4-苯基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-環己基甲基-2-羥基-4-甲基-4-苯基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-(4-第三丁基苄
基)-2-羥基-4-甲基-4-苯基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-聯苯-4-基甲基-2-羥基-4-甲基-4-苯基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-羥基-4-甲基-2-萘-2-基甲基-4-苯基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-羥基-2-(3-羥基苄基)-4-甲基-4-苯基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-羥基-4-甲基-2-(2-甲基-2-苯基丙基)-4-苯基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-苄基-4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-環己基甲基-4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-苄基-4-(5-氟-2-羥基苯基)-2-羥基-4-甲基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-環己基甲基-4-(5-氟-2-羥基苯基)-2-羥基-4-甲基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、4-(5-氟-2-羥基苯基)-2-羥基-4-甲基-2-(2-甲基-2-苯基丙基)戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-(2-氯-6-氟苄基)-4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-(3-氟苄基)-4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-(2-氟苄基)-4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-(3,4-二氟苄基)-4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-(2-氯-6-氟苄基)-4-(5-氟-2-羥基苯基)-2-羥基-4-
甲基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-(3-氟苄基)-4-(5-氟-2-羥基苯基)-2-羥基-4-甲基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-(2-氟苄基)-4-(5-氟-2-羥基苯基)-2-羥基-4-甲基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-(3,4-二氟苄基)-4-(5-氟-2-羥基苯基)-2-羥基-4-甲基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-(4-氟苄基)-4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-(3-甲基苄基)戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-(4-氟苄基)-4-(5-氟-2-羥基苯基)-2-羥基-4-甲基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、4-(5-氟-2-羥基苯基)-2-羥基-4-甲基-2-(3-甲基苄基)戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-(3,5-二氟苯基)-4-(5-氟-2-羥基苯基)-2-羥基-4-甲基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-(2-甲基苄基)戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-(3,5-二甲基苄基)-4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-(2,5-二氟苄基)-4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-(2,5-二氟苄基)-4-(5-氟-2-羥基苯基)-2-羥基-4-甲基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、4-(5-氟-2-羥基苯基)-2-羥基-4-甲基-2-(2-甲基苄基)戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-(3,5-二甲基苄基)-4-(5-氟-2-
羥基苯基)-2-羥基-4-甲基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-(3-氯苄基)-4-(5-氟-2-羥基苯基)-2-羥基-4-甲基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、4-(5-氟-2-甲氧基苯基)-2-羥基-2-[2-(4-甲氧基苯基)乙基]-4-甲基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、4-(5-氟-2-甲氧基苯基)-2-羥基-2-(2-甲氧基苄基)4-甲基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-苯乙基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-(2-氯苄基)-4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、4-(5-氟-2-羥基苯基)-2-羥基-4-甲基-2-苯乙基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、4-(5-氟-2-羥基苯基)-2-羥基-2-[2-(4-羥基苯基)乙基]-4-甲基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-(2-氯苄基)-4-(5-氟-2-羥基苯基)-2-羥基-4-甲基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、4-(5-氟-2-羥基苯基)-2-羥基-2-(2-羥基苄基)-4-甲基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-(2-溴苄基)-4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-(2-溴苄基)-4-(5-氟-2-羥基苯基)-2-羥基-4-甲基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-(5-氟-2-甲氧基芐基)-2-羥基-4-甲基-4-苯基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-(5-氟-2-羥基苄基)-2-羥基-4-甲基-4-苯基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-(5-氟-2-甲氧基
苄基)-4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-(5-氟-2-羥基苄基)-4-(5-氟-2-羥基苯基)-2-羥基-4-甲基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-(3,5-二甲氧基苄基)-2-羥基-4-甲基-4-苯基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-(3,5-二羥基苄基)-2-羥基-4-甲基-4-苯基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)-醯胺、2-羥基-2-(2-甲氧基苄基)4-甲基-4-苯基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、12-羥基-2-(2-羥基苄基)-4-甲基-4-苯基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-羥基-2-[2-(4-羥基苯基)乙基]-4-甲基-4-苯基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、15-[2-苄基-4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基戊基胺基]-3H-異苯并呋喃-1-酮、4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-(1-苯基乙烯基)戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-羥基-4-甲基-4-苯基-2-吡啶-2-基甲基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基-2-(1-苯基乙基)戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、4-(5-氟-2-羥基苯基)-2-羥基-4-甲基-2-(1-苯基乙基)戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-環戊基-4-(5-氟-2-甲氧基苯基)-2-羥基-4-甲基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-環戊基-4-(5-氟-2-羥基苯基)-2-羥基-4-甲基戊酸(1-側氧基-1,3-二氫異苯并呋喃-5-基)醯胺、2-環戊基甲基-4-(5-氟-2-羥基苯基)-2-羥基-4-甲基戊酸(1-側氧基-1,3-
二氫異苯并呋喃-5-基)醯胺、及2-苄基-2-羥基-N-(1-側氧基-1,3-二氫異苯并呋喃-5-基)4-苯基-丁醯胺。
於另一實施例中，該至少DIGRA具有式I，其中a)A係芳基或雜芳基，各者視需要獨立地經一至三個取代基取代，該等取代基獨立地選自由C1至C5烷基、C2至C5烯基、C2至C5炔基、C1至C3烷醯基、C3至C8環烷基、雜環基、芳基、雜芳基、C1至C5烷氧基、C2至C5烯氧基、C2至C5炔氧基、芳氧基、醯基、C1至C5烷氧羰基、芳醯基、胺基羰基、烷胺基羰基、二烷胺基羰基、胺基羰氧基、C1至C5烷胺基羰氧基、C1至C5二烷胺基羰氧基、C1至C5烷醯基胺基、C1至C5烷氧羰基胺基、C1至C5烷基磺醯胺基、胺基磺醯基、C1至C5烷胺基磺醯基、C1至C5二烷胺基磺醯基、鹵素、羥基、羧基、氰基、三氟甲基、三氟甲氧基、硝基、胺基(其中氮原子視需要獨立地經C1至C5烷基或芳基單或二取代)、脲基(其中任一氮原子視需要獨立地經C1至C5烷基取代)、C1至C5烷硫基(其中硫原子視需要氧化以形成亞碸或碸)組成之群；b)R1及R2各自獨立地係氫或C1至C5烷基，或R1及R2藉由其等共同連接之碳原子一起形成C3至C8螺環烷基環；c)R3係三氟甲基；d)B係C1至C5伸烷基、C2至C5伸烯基或C2至C5伸炔基，各者視需要獨立地經一至三個取代基取代，其中B之各取代基獨立地係C1至C3烷基、羥基、鹵素、胺基或側氧基；e)D不存在；
f)E係-NR6R7，其中R6及R7各自獨立地係氫、C1至C8烷基、C2至C8烯基、C2至C8炔基、C1至C8烷氧基、C2至C8烯氧基、C2至C8炔氧基、羥基、碳環基、雜環基、芳基、芳氧基、醯基、雜芳基、碳環-C1至C8烷基、芳基-C1至C8烷基、芳基-C1至C8鹵烷基、雜環基-C1至C8烷基、雜芳基-C1至C8烷基、碳環-C2至C8烯基、芳基-C2至C8烯基、雜環基-C2至C8烯基、雜芳基-C2至C8烯基或C1至C5烷硫基(其中硫原子經氧化以形成亞碸或碸)，各者視需要獨立地經一至三個取代基取代，其中R6及R7之各取代基獨立地係C1至C5烷基、C2至C5烯基、C2至C5炔基、C3至C8環烷基、苯基、C1至C5烷氧基、苯氧基、C1至C5烷醯基、芳醯基、C1至C5烷氧羰基、C1至C5烷醯氧基、胺基羰基、C1至C5烷胺基羰基、C1至C5二烷胺基羰基、胺基羰氧基、C1至C5烷胺基羰氧基、C1至C5二烷胺基羰氧基、C1至C5烷醯基胺基、C1至C5烷氧羰基胺基、C1至C5烷基磺醯胺基、胺基磺醯基、C1至C5烷胺基磺醯基、C1至C5二烷胺基磺醯基、鹵素、羥基、羧基、氰基、側氧基、三氟甲基、三氟甲氧基、硝基、胺基(其中氮原子視需要獨立地經C1至C5烷基單或二取代)、脲基(其中任一氮原子視需要獨立地經C1至C5烷基取代)、或C1至C5烷硫基(其中硫原子視需要氧化以形成亞碸或碸)；及g)Q包括視需要經一至三個取代基取代之雜芳基，其中Q之各取代基獨立地係C1至C5烷基、C2至C5烯基、C2至C5炔基、C3至C8環烷基、雜環基、芳基、雜芳基、C1至C5烷氧基、C2至C5烯氧基、C2至C5炔氧基、芳氧基、醯基、C1至
C5烷氧羰基、C1至C5烷醯氧基、胺基羰基、C1至C5烷胺基羰基、C1至C5二烷胺基羰基、胺基羰氧基、C1至C5烷胺基羰氧基、C1至C5二烷胺基羰氧基、C1至C5烷醯基胺基、C1至C5烷氧羰基胺基、C1至C5烷基磺醯胺基、胺基磺醯基、C1至C5烷胺基磺醯基、C1至C5二烷胺基磺醯基、鹵素、羥基、羧基、氰基、三氟甲基、三氟甲氧基、三氟甲硫基、硝基或胺基(其中氮原子視需要獨立地經C1至C5烷基單或二取代)、或脲基(其中任一氮原子視需要獨立地經C1至C5烷基取代)、或C1至C5烷硫基(其中硫原子視需要氧化以形成亞碸或碸)，其中Q之各取代基係視需要經一至三個取代基取代，該等取代基選自由C1至C3烷基、C1至C3烷氧基、鹵素、羥基、側氧基、氰基、胺基或三氟甲基組成之群。
此等化合物之非限制性實例包括3-(5-氟-2-甲氧基-苯基)-3-甲基-1-(吡啶-2-基甲基)-1-三氟甲基-丁基胺、3-(5-氟-2-甲氧基-苯基)-1-(1H-吲哚-2-基甲基)-3-甲基-1-三氟甲基-丁基胺、1-(2,6-二氯-吡啶-4-基甲基)-3-(5-氟-2-甲氧基-苯基)-3-甲基-1-三氟甲基-丁基胺、1-(4,6-二甲基-吡啶-2-基甲基)-3-(5-氟-2-甲氧基-苯基)-3-甲基-1-三氟甲基-丁基胺、1-(2-氯-吡啶-4-基甲基)-3-(5-氟-2-甲氧基-苯基)-3-甲基-1-三氟甲基-丁基胺、3-(5-氟-2-甲基-苯基)-3-甲基-1-(3-甲基-1H-吲哚-2-基甲基)-1-三氟甲基-丁基胺、3-(5-氟-2-甲氧基-苯基)-3-甲基-1-(3-甲基-1H-吲哚-2-基甲基)-1-三氟甲基-丁基胺、1-(6-氟-1H-吲哚-2-基甲基)-3-(5-氟-2-甲氧基-苯基)-3-甲基-1-三氟甲基-丁基胺、3-(4-氟-苯基)-3-甲基-1-(3-
甲基-1H-吲哚-2-基甲基)-1-三氟-甲基-丁基胺、3-苯并呋喃-7-基-1-(2,6-二氯-吡啶-4-基甲基)-3-甲基-1-三氟甲基-丁基胺、3-(2,3-二氫-苯并呋喃-7-基)-1-(6-氟-1H-吲哚-2-基甲基)-3-甲基-1-三氟甲基-丁基胺、3-(5-氟-2-甲氧基-苯基)-3-甲基-1-喹啉-4-基甲基-1-三氟甲基-丁基胺、1-(2-氯-喹啉-4-基甲基)-3-(5-氟-2-甲基-苯基)-3-甲基-1-三氟甲基-丁基胺、3-(4-氟-苯基)-3-甲基-1-喹啉-4-基甲基-1-三氟甲基-丁基胺、7-[3-胺基-3-(1H-苯并咪唑-2-基甲基)-4,4,4-三氟-1,1-二甲基-丁基]-2,3-二氫苯并呋喃-5-甲腈、1-(6-氟-1H-苯并咪唑-2-基甲基)-3-(5-氟-2-甲基-苯基)-3-甲基-1-三氟甲基-丁基胺、2-[3-胺基-3-(1H-苯并咪唑-2-基甲基)-4,4,4-三氟-1,1-二甲基-丁基]4-氟-酚、1-(1H-苯并咪唑-2-基甲基)-3-(4-氟-苯基)-3-甲基-1-三氟甲基-丁基胺、1-(1H-吲哚-2-基甲基)-3-甲基-3-吡啶-3-基-1-三氟甲基-丁基胺、1-(1H-苯并咪唑-2-基甲基)-3-甲基-3-吡啶-4-基-1-三氟甲基-丁基胺、3-甲基-1-(3-甲基-1H-吲哚-2-基甲基)-3-吡啶-3-基-1-三氟甲基-丁基胺、1-(6-氟-1H-吲哚-2-基甲基)-3-甲基-3-吡啶-3-基-1-三氟甲基-丁基胺、3-(2,3-二氫-苯并呋喃-7-基)-1-(1H-吲哚-2-基甲基)-3-甲基-1-三氟甲基-丁基胺、[3-(5-氟-2-甲氧基-苯基)-3-甲基-1-喹啉-4-基甲基-1-三氟甲基-丁基]-甲基-胺、乙基-[3-(5-氟-2-甲氧基-苯基)-3-甲基-1-喹啉-4-基甲基-1-三氟甲基-丁基]-胺、[3-(5-氟-2-甲氧基-苯基)-3-甲基-1-喹啉-4-基甲基-1-三氟甲基-丁基]-丙基胺、[3-(5-氟-2-甲氧基-苯基)-3-甲基-1-喹啉-4-基甲基-1-三
氟甲基-丁基]-異丁基胺、丁基-[3-(5-氟-2-甲氧基-苯基)-3-甲基-1-喹啉-4-基甲基-1-三氟甲基-丁基]-胺、[3-(5-氟-2-甲氧基-苯基)-3-甲基-1-喹啉-4-基甲基-1-三氟-甲基-丁基]-二甲基胺、N-[3-(5-氟-2-甲氧基-苯基)-3-甲基-1-喹啉-4-基甲基-1-三氟甲基-丁基]-乙醯胺、N-[3-(5-氟-2-甲氧基-苯基)-3-甲基-1-喹啉-4-基甲基-1-三氟甲基-丁基]-甲醯胺、N-[3-(5-氟-2-甲氧基-苯基)-3-甲基-1-喹啉-4-基甲基-1-三氟甲基-丁基]-甲磺醯胺、1-(2,6-二甲基-吡啶-4-基甲基)-3-(5-氟-2-甲氧基-苯基)-3-甲基-1-三氟甲基-丁基胺、3-(5-氟-2-甲氧基-苯基)-3-甲基-1-(1H-吡咯并[2,3-c]吡啶-2-基甲基)-1-三氟甲基-丁基胺、2-[2-胺基-4-(5-氟-2-甲氧基-苯基)-4-甲基-2-三氟甲基-戊基]-4-甲基-1H-吲哚-6-甲腈、N-[3-(5-氟-2-甲氧基-苯基)-3-甲基-1-喹啉-4-基甲基-1-三氟甲基-丁基]-羥基胺、及2-(3-胺基-4,4,4-三氟-1,1-二甲基-3-喹啉-4-基甲基-丁基)-4-氟-酚。
於另一實施例中，該至少DIGRA具有式I，其中A、B、D、E、R1、R2、R6及R7具有以上揭示之含義，及R3係C1至C8烷基、C2至C8烯基、C2至C8炔基、碳環、雜環基、芳基、雜芳基、碳環-C1至C8烷基、羧基、烷氧羰基、芳基-C1至C8烷基、芳基-C1至C8鹵烷基、雜環基-C1至C8烷基、雜芳基-C1至C8烷基、碳環-C2至C8烯基、芳基-C2至C8烯基、雜環基-C2至C8烯基或雜芳基-C2至C8烯基，各者視需要獨立地經一至三個取代基取代，其中R3之各取代基獨立地係C1至C5烷基、C2至C5烯基、C2至C5炔基、C3至C8環烷基、苯基、C1
至C5烷氧基、苯氧基、C1至C5烷醯基、芳醯基、C1至C5烷氧羰基、C1至C5烷醯氧基、胺基羰氧基、C1至C5烷胺基羰氧基、C1至C5二烷胺基羰氧基、胺基羰基、C1至C5烷胺基羰基、C1至C5二烷胺基羰基、C1至C5烷醯基胺基、C1至C5烷氧羰基胺基、C1至C5烷基磺醯胺基、C1至C5烷胺基磺醯基、C1至C5二烷胺基磺醯基、鹵素、羥基、羧基、氰基、側氧基、三氟甲基、硝基、胺基(其中氮原子視需要獨立地經C1至C5烷基單或二取代)、脲基(其中任一氮原子視需要獨立地經C1至C5烷基取代)、C1至C5烷硫基(其中硫原子視需要氧化以形成亞碸或碸)，其中R3不可係三氟甲基。
此等化合物之非限制性實例包括1-(2,6-二氯-吡啶-4-基甲基)-3-(5-氟-2-甲氧基-苯基)-1,3-二甲基-丁基胺、1-乙基-3-(5-氟-2-甲氧基-苯基)-3-甲基-1-喹啉-4-基甲基-丁基胺、1-環己基甲基-3-(5-氟-2-甲氧基-苯基)-1-(1H-吲哚-2-基甲基)-3-甲基-丁基胺、1-(2-氯-喹啉-4-基甲基)-1-環戊基-3-(5-氟-2-甲氧基-苯基)-3-甲基-丁基胺、1-(2-氯-吡啶-4-基甲基)-1-環戊基甲基-3-(5-氟-2-甲氧基-苯基)-3-甲基-丁基胺、3-(5-氟-2-甲氧基-苯基)-1,3-二甲基-1-喹啉-4-基甲基-丁基胺、1-環丙基-3-(5-氟-2-甲氧基-苯基)-3-甲基-1-喹啉-4-基甲基-丁基胺、3-(5-氟-2-甲氧基-苯基)-1,3-二甲基-1-(1H-吡咯并[2,3-c]吡啶-2-基甲基)-丁基胺、1-環丙基-3-(5-氟-2-甲氧基-苯基)-3-甲基-1-(1H-吡咯并[2,3-c]-吡啶-2-基甲基)-丁基胺、2-[3-胺基-1,1,3-三甲基-4-(1H-吡咯并[2,3-c]吡啶-2-基)-丁基]-4-氟-酚、2-[2-胺基-4-(5-氟-2-甲氧基-苯
基)-2,4-二甲基-戊基]-4-甲基-1H-吲哚-6-甲腈。
於另一實施例中，DIGRA具有如美國專利申請公告案US 2009/0326009A1所揭示之式V，該案之內容已以引用之方式併入本文，
環Xa表示苯環或吡啶環；Ra 1表示鹵原子、具有至少一個取代基之C1至C10(或C1至C5或C1至C3)烷基、羥基、具有至少一個取代基之C1至C10(或C1至C5或C1至C3)烷氧基、具有至少一個取代基之C2至C10(或C2至C5或C2至C3)烯氧基、C1至C10(或C1至C5或C1至C3)烷羰基、胺基、硝基或氰基；p表示0至5之整數；於各情況中，當p為2至5時，各Ra 1可相同或不同；Ra 2表示鹵原子、可具有至少一個取代基之C1至C10(或C1至C5或C1至C3)烷基、羥基、羥基酯或可具有至少一個取代基之C1至C10(或C1至C5或C1至C3)烷氧基；q表示0至2之整數；於各情況中，當q係2時，Ra 2各可相同或不同；Ra 3表示氫原子、可具有至少一個取代基之C1至C10(或C1
至C5或C1至C3)烷基、可具有至少一個取代基之C2至C10(或C2至C5或C2至C3)烯基、可具有至少一個取代基之C2至C10(或C2至C5或C2至C3)炔基、可具有至少一個取代基之C5至C14(或，C5至C10)芳基、可具有至少一個取代基之C1至C10(或C1至C5或C1至C3)烷羰基、可具有至少一個取代基之C2至C10(或C2至C5或C2至C3)烯基羰基、可具有至少一個取代基之C2至C10(或C2至C5或C2至C3)炔基羰基或可具有至少一個取代基之C5至C14(或，C5至C10)芳基羰基；Ra 4及Ra 5可相同或不同及表示氫原子或C1至C10(或C1至C5或C1至C3)烷基；Ra 4及Ra 5可組合一起形成3-至8-員環烷基環；Ra 6表示氫原子或C1至C10(或C1至C5或C1至C3)烷基；A表示C1至C10(或C1至C5或C1至C3)伸烷基或羰基；Ra 7表示ORa 8、NRa 8Ra 9、SRa 8、S(O)Ra 8或S(O)2Ra 8；Ra 8表示可具有至少一個取代基之C1至C10(或C1至C5或C1至C3)烷基、具有至少一個取代基之C2至C10(或C2至C5或C2至C3)烯基、可具有至少一個取代基之C2至C10(或C2至C5或C2至C3)炔基、可具有至少一個取代基之C3至C10(或C3至C5)環烷基、可具有至少一個取代基之芳基、可具有至少一個取代基之雜環基、甲醯基、可具有至少一個取代基之C1至C10(或C1至C5或C1至C3)烷羰基、可具有至少一個取代基之C2至C10(或C2至C5或C2至C3)烯基羰基、可具有至少一個取代基之C2至C10(或C2至C5或C2至C3)炔基羰基、可具有至少一個取代基之C3至C10(或C3至C5)環烷羰基、可具有至少一
個取代基之C5至C14(或，C5至C10)芳羰基、可具有至少一個取代基之雜環羰基、羧基、可具有至少一個取代基之C1至C10(或C1至C5或C1至C3)烷氧羰基、可具有至少一個取代基之C2至C10(或C2至C5或C2至C3)烯氧羰基、可具有至少一個取代基之C2至C10(或C2至C5或C2至C3)炔氧羰基、可具有至少一個取代基之C3至C10(或C3至C5)環烷氧羰基、可具有至少一個取代基之C5至C14(或，C5至C10)芳氧羰基、可具有至少一個取代基之雜環氧羰基、可具有至少一個取代基之低碳數烷磺醯基、可具有至少一個取代基之C2至C10(或C2至C5或C2至C3)烯基磺醯基、可具有至少一個取代基之C2至C10(或C2至C5或C2至C3)炔基磺醯基、可具有至少一個取代基之C3至C10(或C3至C5)環烷磺醯基、可具有至少一個取代基之C5至C14(或，C5至C10)芳基磺醯基、可具有至少一個取代基之雜環磺醯基、胺基羰基、可具有至少一個取代基之C1至C10(或，C1至C5或C1至C3)烷胺基羰基、可具有至少一個取代基之C2至C10(或，C2至C5或C2至C3)烯基胺基羰基、可具有至少一個取代基之C2至C10(或，C2至C5或C2至C3)炔基胺基羰基、可具有至少一個取代基之C3至C10(或，C3至C5)環烷胺基羰基、可具有至少一個取代基之C5至C14(或，C5至C10)芳胺基羰基或可具有至少一個取代基之雜環胺基羰基；Ra 9表示氫原子、可具有至少一個取代基之C1至C10(或C1至C5或C1至C3)烷基、可具有至少一個取代基之C2至C10(或C2至C5或C2至C3)烯基、可具有至少一個取代基之C2至
C10(或C2至C5或C2至C3)炔基、可具有至少一個取代基之C3至C10(或，C3至C5)環烷基、可具有至少一個取代基之C5至C14(或，C5至C10)芳基、可具有至少一個取代基之雜環基、甲醯基、可具有至少一個取代基之C1至C10(或C1至C5或C1至C3)烷羰基、可具有至少一個取代基之C2至C10(或C2至C5或C2至C3)烯基羰基、可具有至少一個取代基之C2至C10(或C2至C5或C2至C3)炔基羰基、可具有至少一個取代基之C3至C10(或，C3至C5)環烷羰基、可具有至少一個取代基之C5至C14(或，C5至C10)芳羰基、可具有至少一個取代基之雜環羰基、羧基、可具有至少一個取代基之C1至C10(或C1至C5或C1至C3)烷氟羰基、可具有至少一個取代基之C2至C10(或C2至C5或C2至C3)烯氧羰基、可具有至少一個取代基之C2至C10(或C2至C5或C2至C3)炔氧羰基、可具有至少一個取代基之C3至C10(或，C3至C5)環烷氧羰基、可具有至少一個取代基之C5至C14(或，C5至C10)芳氧羰基、可具有至少一個取代基之雜環氟羰基、可具有至少一個取代基之C1至C10(或，C1至C5或C1至C3)烷磺醯基、可具有至少一個取代基之C2至C10(或，C2至C5或C2至C3)烯基磺醯基、可具有至少一個取代基之C2至C10(或，C2至C5或C2至C3)炔基磺醯基、可具有至少一個取代基之C3至C10(或，C3至C5)環烷磺醯基、可具有至少一個取代基之C5至C14(或，C5至C10)芳基磺醯基、可具有至少一個取代基之雜環磺醯基、胺基羰基、可具有至少一個取代基之C1至C10(或，C1至C5或C1至C3)烷胺基羰基、可具有至少一個取代基之C2至C10(或，C2至C5或C2至
C3)烯基胺基羰基、可具有至少一個取代基之C2至C10(或，C2至C5或C2至C3)炔基胺基羰基、可具有至少一個取代基之C3至C10(或，C3至C5)環烷胺基羰基、可具有至少一個取代基之C5至C14(或，C5至C10)芳胺基羰基或可具有至少一個取代基之雜環胺基羰基；且，在Ra 7係NRa 8Ra 9的情況中，Ra 8及Ra 9可組合一起形成可具有取代基之3-至8-員含氮雜環。以上基團中任一者的取代基可包含或由C1至C15(或，C1至C10或C1至C5或C1至C3)直線或分支鏈型烷基、羥基、胺基、鹵素、氰基、C1至C15(或，C1至C10或C1至C5或C1至C3)烷氧基、羧基、C5至C14芳基或具有選自N、O或S之1至3個雜原子之5至14員雜芳基組成。
此等化合物之非限制性實例包括：5-乙醯氧基甲基-6-(2-甲氧基苯基)-2,2,4-三甲基-1,2-二氫喹啉、5-苯甲醯氧基甲基-6-(2-甲氧基苯基)-2,2,4-三甲基-1,2-二氫喹啉、6-(2-甲氧基苯基)-5-[(噻吩-2-基)羰氧基甲基]-2,2,4-三甲基-1,2-二氫喹啉、5-(4-第三丁基苯甲醯氧基甲基)-6-(2-甲氧基苯基)-2,2,4-三甲基-1,2-二氫喹啉、5-苯甲醯氧基甲基-6-(4-氟-2-甲氧基苯基)-2,2,4-三甲基-1,2-二氫喹啉、6-(4-氟-2-甲氧基苯基)-5-(3-甲氧基苯甲醯氧基甲基)-2,2,4-三甲基-1,2-二氫喹啉、6-(4-氟-2-甲氧基苯基)-5-(2-甲氧基苯甲醯氧基甲基)-2,2,4-三甲基-1,2-二氫喹啉、6-(4-氟-2-甲氧基苯基)-5-(4-甲氧基苯甲醯氧基甲基)-2,2,4-三甲基-1,2-二氫喹啉、6-(4-氟-2-甲氧基苯基)-5-[(噻吩-2-基)羰氧基甲基]-2,2,4-三甲基-1,2-二氫喹啉、6-(4-氟-2-甲氧基苯
基)-5-(4-甲基苯甲醯氧基甲基)-2,2,4-三甲基-1,2-二氫喹啉、6-(4-氟-2-甲氧基苯基)-5-(3-甲基苯甲醯氧基甲基)-2,2,4-三甲基-1,2-二氫喹啉、6-(4-氟-2-甲氧基苯基)-5-(2-甲基苯甲醯氧基甲基)-2,2,4-三甲基-1,2-二氫喹啉、6-(4-氟-2-甲氧基苯基)-5-苯氧基甲基-2,2,4-三甲基-1,2-二氫喹啉、6-(4-氟-2-甲氧基苯基)-5-(4-甲氧基苯氧基甲基)-2,2,4-三甲基-1,2-二氫喹啉、6-(4-氟-2-甲氧基苯基)-5-(4-氟苯氧基甲基-2,2,4-三甲基-1,2-二氫喹啉、6-(4-氟-2-甲氧基苯基)-5-(4-氟苯氧基甲基-2,2,4-三甲基-1,2-二氫喹啉、6-(4-氟-2-甲氧基苯基)-5-(4-氟苯氧基甲基-2,2,4-三甲基-1,2-二氫喹啉、6-(4-氟-2-甲氧基苯基)-5-(3-甲氧基苯氧基甲基)-2,2,4-三甲基-1,2-二氫喹啉、6-(4-氟-2-甲氧基苯基)-5-(2-甲氧基苯氧基甲基)-2,2,4-三甲基-1,2-二氫喹啉、6-(4,5-二氟-2-甲氧基苯基)-5-(3-氟苯氧基甲基)-2,2,4-三甲基-1,2-二氫喹啉、6-(4-氟-2-甲氧基苯基)-5-(4-甲基苯氧基甲基-2,2,4-三甲基-1,2-二氫喹啉、6-(4-氟-2-甲氧基苯基)-5-(3-甲基苯氧基甲基-2,2,4-三甲基-1,2-二氫喹啉、6-(4-氟-2-甲氧基苯基)-5-(2-甲基苯氧基甲基-2,2,4-三甲基-1,2-二氫喹啉、6-(4-氟-2-甲氧基苯基)-5-(2-羥基甲基苯氧基甲基)-2,2,4-三甲基-1,2-二氫喹啉、6-(4-氟-2-甲氧基苯基)-5-(5-氟-2-甲基苯氧基甲基)-2,2,4-三甲基-1,2-二氫喹啉、6-(4-氟-2-甲氧基苯基)-5-(5-氯-2-甲基苯氧基甲基)-2,2,4-三甲基-1,2-二氫喹啉、6-(4,5-二氟-2-甲氧基苯基)-5-(5-氟-2-甲基苯氧基甲基)-2,2,4-三甲基-1,2-二氫喹
啉、6-(4-氟-2-甲氧基苯基)-5-(2-甲氧基-5-硝基苯氧基甲基)-2,2,4-三甲基-1,2-二氫喹啉、6-(4-氟-2-甲氧基苯基)-5-[2-(2-羥基乙基)苯氧基甲基]-2,2,4-三甲基-1,2-二氫喹啉、6-(4-氟-2-甲氧基苯基)-5-(2-甲基-5-硝基苯氧基甲基)-2,2,4-三甲基-1,2-二氫喹啉、6-(4-氟-2-甲氧基苯基)-5-(2-烯丙基苯氧基甲基)-2,2,4-三甲基-1,2-二氫喹啉、6-(5-氯-2-甲氧基苯基)-5-[2-(2-羥基乙基)苯氧基甲基]-2,2,4-三甲基-1,2-二氫喹啉、5-(5-氟-2-甲基苯氧基甲基)-6-(4-羥基-2-甲氧基苯基)-2,2,4-三甲基-1,2-二氫喹啉、5-(5-氟-2-甲基苯氧基甲基)-6-(5-羥基-2-甲氧基苯基)-2,2,4-三甲基-1,2-二氫喹啉、6-(4-羥基-2-甲氧基苯基)-5-(4-甲基苯甲醯氧基甲基)-2,2,4-三甲基-1,2-二氫喹啉、6-(2-甲氧基苯基)-5-苯基胺基甲基-2,2,4-三甲基-1,2-二氫喹啉、6-(4-氟-2-甲氧基苯基)-5-苯基胺基甲基-2,2,4-三甲基-1,2-二氫喹啉、6-(4-氟-2-甲氧基苯基)-5-(4-甲氧基苯基胺基甲基)-2,2,4-三甲基-1,2-二氫喹啉、6-(4-氟-2-甲氧基苯基)-5-(4-氟苯基胺基甲基)-2,2,4-三甲基-1,2-二氫喹啉、6-(4-氟-2-甲氧基苯基)-5-(3-氟苯基胺基甲基)-2,2,4-三甲基-1,2-二氫喹啉、6-(4-氟-2-甲氧基苯基)-5-(2-氟苯基胺基甲基)-2,2,4-三甲基-1,2-二氫喹啉、6-(4-氟-2-甲氧基苯基)-5-(3-甲氧基苯基胺基甲基)-2,2,4-三甲基-1,2-二氫喹啉、6-(5-胺基-2-甲氧基苯基)-5-(5-氟-2-甲基苯氧基甲基)-2,2,4-三甲基-1,2-二氫喹啉、5-(2-氟苯甲醯氧基甲基)-6-(4-氟-2-甲氧基苯基)-2,2,4-三甲基-1,2-二氫喹啉、
5-(3-氟苯甲醯氧基甲基)-6-(4-氟-2-甲氧基苯基)-2,2,4-三甲基-1,2-二氫喹啉、5-(4-氟苯甲醯氧基甲基)-6-(4-氟-2-甲氧基苯基)-2,2,4-三甲基-1,2-二氫喹啉、6-(4-氟-2-甲氧基苯基)-5-(4-甲基苯基胺基甲基)-2,2,4-三甲基-1,2-二氫喹啉、6-(4-氟-2-甲氧基苯基)-5-(3-甲基苯基胺基甲基)-2,2,4-三甲基-1,2-二氫喹啉、6-(4-氟-2-甲氧基苯基)-5-(2-甲基苯基胺基甲基)-2,2,4-三甲基-1,2-二氫喹啉、及6-(4-氟-2-甲氧基苯基)-5-(2-甲基苯基硫代甲基)-2,2,4-三甲基-1,2-二氫喹啉。
於另一實施例中，DIGRA具有如美國專利申請公告案US 2010/0137307A1中所揭示式VI，該案之內容係以引用的方式併入本文，
Rb 1表示可具有取代基之低碳數烷基、可具有取代基之低碳數環烷基、可具有取代基之C5至C14(或，C5至C10)芳基、可具有取代基之雜環基或可具有取代基之C5至C14(或，C5至C10)芳烷基；Rb 2表示氫原子或可具有取代基之低碳數烷基；
Rb 3表示氫原子或可具有取代基之低碳數烷基；Rb 4及Rb 5可相同或不同及表示氫原子或可具有取代基之低碳數烷基；Rb 6表示氫原子或可具有取代基之低碳數烷基；Rb 7表示表示氫原子、可具有取代基之低碳數烷基、可具有取代基之低碳數烯基、可具有取代基之低碳數炔基、可具有取代基之低碳數環烷基、可具有取代基之芳基或可具有取代基之雜環基；Wb表示氧原子、硫原子或NRb 8；Rb 8表示氫原子或可具有取代基之低碳數烷基；Xb表示氧原子或硫原子；Yb表示可具有取代基之低碳數伸烷基；Zb表示氧原子、硫原子、NRb 9、OCO或OSO2；Rb 9表示氫原子或可具有取代基之低碳數烷基。
以上基團中任一者的取代基可包含或由C1至C15(或，C1至C10，或C1至C5或C1至C3)直線或分支鏈型烷基、羥基、胺基、鹵素、氰基、C1至C15(或，C1至C10，或C1至C5或C1至C3)烷氧基、羧基、C5至C14芳基或具有選自N、O或S之1至3個雜原子之5至14員雜芳基組成。
此等化合物之非限制性實例包括：8-(5-氟-2-甲基苯氧基甲基)-7-(2-甲氧基-4-甲基磺醯氧基苯基)-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、8-(5-氟-2-甲基苯氧基甲基)-7-(2-甲氧基-4-苯基磺醯氧基苯基)-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、8-(5-氟-2-甲基苯氧基甲基)-7-(2-甲
氧基-4-三氟甲基磺醯氧基苯基)-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、8-(5-氟-2-甲基苯氧基甲基)-7-(2-甲氧基-4-丙基磺醯氧基苯基)-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、8-(5-氟-2-甲基苯氧基甲基)-7-[2-甲氧基-4-(呋喃-2-基磺醯氧基)苯基]-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、7-(2-甲氧基-4-甲基磺醯氧基苯基)-8-(5-甲基噻吩-2-基羰氧基甲基)-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、7-[4-(2-氯苯基磺醯氧基)-2-甲氧基苯基]-8-(5-氟-2-甲基苯氧基甲基)-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、7-(4-苄基磺醯氧基-2-甲氧基苯基)-8-(5-氟-2-甲基苯氧基甲基)-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、8-(5-氟-2-甲基苯氧基甲基)-7-[2-甲氧基-4-(2-甲氧基羰基乙基磺醯氧基)苯基]-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、7-(4-丁基磺醯氧基-2-甲氧基苯基)-8-(5-氟-2-甲基苯氧基甲基)-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、7-(4-乙基磺醯氧基-2-甲氧基苯基)-8-(5-氟-2-甲基苯氧基甲基)-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、8-(5-氟-2-甲基苯氧基甲基)-7-(4-異丙基磺醯氧基-2-甲氧基苯基)-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、8-(5-氟-2-甲基苯氧基甲基)-7-[2-甲氧基-4-(4-甲基苄基磺醯氧基)苯基]-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、7-[4-(4-氯苄基磺醯氧基)-2-甲氧基苯基]-8-(5-氟-2-甲基苯氧基甲基)-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、8-(5-氟-2-甲基苯氧基甲基)-7-(4-異丁基磺醯氧基-2-甲氧基苯基)-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、8-(5-
氟-2-甲基苯氧基甲基)-7-[2-甲氧基-4-(3,3,3-三氟丙基磺醯氧基)苯基]-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、7-(4-環丙基磺醯氧基-2-甲氧基苯基)-8-(5-氟-2-甲基苯氧基甲基)-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、8-(5-氟-2-甲基苯氧基甲基)-7-(2-甲氧基-4-甲基磺醯胺基苯基)-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、7-[4-(2-氯苄基磺醯氧基)-2-甲氧基苯基]-8-(5-氟-2-甲基苯氧基甲基)-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、8-(5-氟-2-甲基苯氧基甲基)-7-[2-甲氧基-4-(2-甲基芐基磺醯氧基)苯基]-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、7-(4-環戊基磺醯氧基-2-甲氧基苯基)-8-(5-氟-2-甲基苯氧基甲基)-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、7-(4-環己基磺醯氧基-2-甲氧基苯基)-8-(5-氟-2-甲基苯氧基甲基)-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、8-(5-氟-2-甲基苯氧基甲基)-7-[2-甲氧基-4-(3-甲基苄基磺醯氧基)苯基]-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、7-(4-環丙基磺醯氧基-2-甲氧基苯基)-8-(5-甲基噻吩-2-基羰氧基甲基)-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、7-[2-甲氧基-4-(3,3,3-三氟丙基磺醯氧基)苯基]-8-(5-甲基噻吩-2-基羰氧基甲基)-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、7-(4-異丁基磺醯氧基-2-甲氧基苯基)-8-(5-甲基噻吩-2-基羰氧基甲基)-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、7-(2-甲氧基-4-丙基磺醯氧基苯基)-8-(5-甲基噻吩-2-基羰氧基甲基)-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、7-(4-異丙基磺醯氧基-2-甲氧基苯
基)-8-(5-甲基噻吩-2-基羰氧基甲基)-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、7-(4-環戊基磺醯氧基-2-甲氧基苯基)-8-(5-甲基噻吩-2-基羰氧基甲基)-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、7-(2-甲氧基-4-甲基磺醯氧基苯基)-8-(2-甲氧基苯基胺基甲基)-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、7-(4-環丙基磺醯氧基-2-甲氧基苯基)-8-(2-甲氧基苯基胺基甲基)-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、7-(2-甲氧基-4-甲基磺醯氧基苯基)-8-(2-甲氧基-5-硝基苯氧基-甲基)-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、8-(2-甲氧基-5-硝基苯氧基甲基)-7-[2-甲氧基-4-(3,3,3-三氟丙基磺醯氧基)苯基]-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、7-(4-異丙基磺醯氧基-2-甲氧基苯基)-8-(2-甲氧基-5-硝基苯氧基甲基)-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、7-(4-環丙基磺醯氧基-2-甲氧基苯基)-8-(2-甲氧基-5-硝基苯氧基甲基)-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、7-(4-環丙基磺醯氧基-2-甲氧基苯基)-8-(2-甲基-5-硝基苯氧基甲基)-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、7-[2-甲氧基-4-(3,3,3-三氟丙基磺醯氧基)苯基]-8-(2-甲基-5-硝基苯氧基甲基)-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、7-(2-甲氧基-4-甲基磺醯氧基苯基)-8-(2-甲基-5-硝基苯氧基甲基)-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、7-(2-甲氧基-4-丙基磺醯氧基苯基)-8-(4-甲基苯甲醯氧基甲基)-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、8-(2-甲氧基苯基胺基甲基)-7-[2-甲氧基-4-(3,3,3-三氟丙基磺醯氧基)苯基]-1,3,3-
三甲基-3,4-二氫-1H-喹噁啉-2-酮、7-(4-異丁基磺醯氧基-2-甲氧基苯基)-8-(2-甲氧基苯基胺基甲基)-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、7-(4-環丙基磺醯氧基-2-甲氧基苯基)-8-(5-氟-2-甲基苯基胺基甲基)-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、8-(5-氟-2-甲基苯基胺基甲基)-7-(2-甲氧基-4-丙基磺醯氧基苯基)-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、7-(4-苄基胺基丙基磺醯氧基-2-甲氧基苯基)-8-(5-氟-2-甲基苯氧基甲基)-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、8-(5-氟-2-甲基苯氧基甲基)-7-[2-甲氧基-4-(3-丙基胺基丙基磺醯氧基)苯基]-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、8-(5-氟-2-甲基苯氧基甲基)-7-[2-甲氧基-4-(嗎啉-4-基)丙基磺醯氧基苯基]-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、8-(5-氟-2-甲基苯氧基甲基)-7-[2-甲氧基-4-(哌啶基)氯丙基磺醯氧基苯基]-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、8-(5-氟-2-甲基苯氧基甲基)-7-[2-甲氧基-4-(N-二甲基胺基乙基-N-甲基)胺基丙基磺醯氧基苯基]-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮、及8-(5-氟-2-甲基苯氧基甲基)-7-[2-甲氧基-4-(N-甲基-N-甲基胺基乙基)胺基丙基磺醯氧基苯基]-1,3,3-三甲基-3,4-二氫-1H-喹噁啉-2-酮。
可用作DIGRA之其他化合物及其等製造方法揭示於例如美國專利申請公告案2004/0029932、2004/0162321、2004/0224992、2005/0059714、2005/0176706、2005/0203128、2005/0234091、2005/0282881、2006/0014787、2006/0030561及2006/0116396中，該等案之
內容係以引用其等全文之方式併入本文。
於另一態樣中，本發明提供一種治療或預防青光眼或其惡化之眼用醫藥組合物。該眼用醫藥組合物包含(a)至少DIGRA、其前藥、其醫藥可接受鹽或其醫藥可接受酯；及(b)與該DIGRA、其前藥、其醫藥可接受鹽、及其醫藥可接受酯不同之消炎藥。於一態樣中，該醫藥組合物進一步包含醫藥可接受載劑。於另一態樣中，該載劑係眼用可接受載劑。
於此眼用組合物中之DIGRA、其前藥、其醫藥可接受鹽或其醫藥可接受酯之濃度係介於約0.0001至約1000 mg/ml之間(或，約0.001至約500 mg/ml，或約0.001至約300 mg/ml，或約0.001至約250 mg/ml，或約0.001至約100 mg/ml，或約0.001至約50 mg/ml，或約0.01至約300 mg/ml，或約0.01至約250 mg/ml，或約0.01至約100 mg/ml，或約0.1至約100 mg/ml，或約0.1至約50 mg/ml)。
於一實施例中，本發明之組合物係呈懸浮液或分散液形式。於另一實施例中，該懸浮液或分散液係基於水性溶液。例如，本發明之組合物可包含無菌鹽水溶液。於另一實施例中，該DIGRA、或其前藥、其醫藥可接受鹽、或其醫藥可接受酯及消炎藥的微米-或奈米級-顆粒可藉由生理可接受表面活性劑(其非限制性實例揭示於下文)塗覆，隨後將經塗覆顆粒分散於液體介質中。塗層可維持顆粒懸浮。此液體介質可經選擇以產生緩釋懸浮液。例如，該液體介質可係難溶解於接受投與該懸浮液的眼部環境中之介質。於另
一實施例中，將活性成分懸浮或分散於疏水介質(如，油)中。
DIGRA及與該DIGRA、其前藥、其醫藥可接受鹽及其醫藥可接受酯不同的消炎藥係以有效治療、控制、減輕、改善、緩解或預防病況的量存在。於一實施例中，此消炎藥係選自由以下藥品組成之群：非類固醇消炎藥(NSAID)；過氧化物酶體增殖物活化受體(PPAR)配位體(如PPARα、PPARδ或PPARγ配位體)；抗組織胺藥；促炎細胞素拮抗劑或抑制劑(如抗-TNF、抗介白素、抗-NF-B)；氧化氮合成酶抑制劑；其組合；及其混合物。抗組織胺藥之非限制性實例包括Patanol®(奧洛他定(olopatadine))、Emadine®(依美斯汀(emedastine))及Livostin®(左卡巴斯汀(levocabastine))。抗-TNF藥之非限制性實例包括Remicade®(英利昔單抗(infliximab))、Enbrel®(依那西普(etanercept))及Humira®(阿達木單抗(adalimumab))。抗介白素藥之非限制性實例包括Kineret(阿那白滯素(anakinra))、Zenapax(達克力莫(daclizumab))、Simulect(巴利昔單抗(basixilimab))、環孢靈素(cyclosporine)及他克莫司(tacrolimus)。
NSAID之非限制性實例係：胺基芳基羧酸衍生物(例如，苯乙胺茴酸(enfenamic acid)、依託芬那酯(etofenamate)、氟滅酸(flufenamic acid)、異尼克辛(isonixin)、甲氯滅酸(meclofenamic acid)、甲滅酸(mefenamic acid)、尼氟滅酸(niflumic acid)、他尼氟酯(talniflumate)、特羅胺酯(terofenamate)、托芬那酸(tolfenamic acid)、丙烯乙酸衍生
物(例如，乙醯氯芬酸(aceclofenac)、阿西美辛(acemetacin)、阿氯芬酸(alclofenac)、胺芬酸(amfenac)、呱胺托美丁(amtolmetin guacil)、溴芬酸(bromfenac)、丁苯羥酸(bufexamac)、桂美辛(cinmetacin)、氯吡酸(clopirac)、雙氯芬酸鈉(diclofenac sodium)、依託度酸(etodolac)、聯苯乙酸(felbinac)、芬克洛酸(fenclozic acid)、芬替酸(fentiazac)、葡美辛(glucametacin)、異丁芬酸(ibufenac)、茚甲新(indomethacin)、三苯唑酸(isofezolac)、伊索克酸(isoxepac)、氯那唑酸(lonazolac)、甲吩噻嗪乙酸(metiazinic acid)、莫苯唑酸(mofezolac)、奧沙美辛(oxametacine)、氯苯基氟苯基吡唑乙酸(pirazolac)、丙榖美辛(proglumetacin)、舒林酸(sulindac)、噻拉米特(tiaramide)、托麥汀(tolmetin)、吲哚美辛托品(tropesin)、氯苯醯二甲基吡咯乙酸(zomepirac))、芳基丁酸衍生物(例如，布馬地宗(bumadizon)、異丁苯丁酸(butibufen)、芬布芬(fenbufen)、聯苯丁酸(xenbucin))、芳基羧酸(例如，環氯茚酸(clidanac)、克多炎(ketorolac)、替諾立定(tinoridine))、芳基丙酸衍生物(例如，阿明洛芬(alminoprofen)、苯惡洛芬(benoxaprofen)、柏莫洛芬(bermoprofen)、布氯酸(bucloxic acid)、卡洛芬(carprofen)、非諾洛芬(fenoprofen)、氟諾洛芬(flunoxaprofen)、氟比洛芬(flurbiprofen)、布洛芬(ibuprofen)、異丁普生(ibuproxam)、吲哚洛芬(indoprofen)、酮基布洛芬(ketoprofen)、環氧洛芬(loxoprofen)、萘普生(naproxen)、惡丙嗪(oxaprozin)、吡酮洛芬(piketoprolen)、
吡咯洛(pirprofen)、普拉洛芬(pranoprofen)、丙替嗪酸(protizinic acid)、蘇普芬酸(suprofen)、噻洛芬酸(tiaprofenic acid)、肟環苯丙酸(ximoprofen)、扎托洛芬(zaltoprofen))、吡唑類(例如，雙苯咪唑(difenamizole)、依匹唑(epirizole))、吡唑啉酮類(例如，阿扎丙宗(apazone)、芐哌立隆(benzpiperylon)、非潑拉酮(feprazone)、莫非保松(mofebutazone)、馬拉宗(morazone)、羥基保泰松(oxyphenbutazone)、保泰松(phenylbutazone)、哌保松(pipebuzone)、異丙胺替比林(propyphenazone)、雷米那酮(ramifenazone)、琥保松(suxibuzone)、噻唑丁炎酮(thiazolinobutazone))，水楊酸衍生物(例如，醋胺沙羅(acetaminosalol)、阿斯匹靈(aspirin)、撲炎痛(benorylate)、溴水楊醇(bromosaligenin)、乙醯水楊酸鈣(calcium acetylsalicylate)、雙氟尼酸(diflunisal)、依特柳酯(etersalate)、芬多沙(fendosal)、龍膽酸(gentisic acid)、水楊酸乙二醇酯(glycol salicylate)、水楊酸咪唑酯(imidazole salicylate)、乙醯水楊酸賴胺酸酯(lysine acetylsalicylate)、美沙拉嗪(mesalamine)、水楊酸嗎啉酯(morpholine salicylate)、水楊酸1-萘酯(1-naphthyl salicylate)、奧沙拉嗪(olsalazine)、帕沙米特(parsalmide)、乙醯水楊酸苯酯(phenyl acetylsalicylate)、水楊酸苯酯(phenyl salicylate)、醋水楊胺(salacetamide)、水楊醯胺鄰乙酸(salicylamide o-acetic acid)、水楊基硫酸(salicylsulfuric acid)、雙水楊酯(salsalate)、柳氮磺胺吡啶(sulfasalazine))、噻嗪甲醯胺類
(thiazinecarboxamides)(例如，安吡昔康(ampiroxicam)、哚昔康(droxicam)、異惡噻醯胺(isoxicam)、芬諾昔康(lornoxicam)、吡羅昔康(piroxicam)、替諾昔康(tenoxicam))，ε-乙醚胺基己酸(ε-acetamidocaproic acid)、S-(5'-腺苷)-L-甲硫胺酸(S-(5'-adenosyl)-L-methionine)、3-胺基-4-羥基丁酸(3-amino-4-hydroxybutyric acid)、阿米曲林(amixetrine)、芐達酸(bendazac)、消炎靈(benzydamine)、α-沒藥醇(α-bisabolol)、布克隆(bucolome)、吡啶基聯苯基乙醯胺(difenpiramide)、地他唑(ditazol)、依莫法宗(emorfazone)、非普地醇(fepradinol)、癒創薁(guaiazulene)、萘普酮(nabumetone)、尼美舒利(nimesulide)、奧沙西羅(oxaceprol)、瑞尼托林(paranyline)、苯基異噁唑基六氫吡啶乙醇(perisoxal)、普羅喹宗(proquazone)、超氧化歧化酶(superoxide dismutase)、替尼達普(tenidap)、棄白通(zileuton)，其生理可接受鹽、其組合及其混合物。
於本發明之另一態樣中，消炎藥係PPAR結合分子。於一實施例中，此PPAR結合分子係PPARα-、PPARδ-或PPARγ-結合分子。於另一實施例中，此PPAR結合分子係PPARα、PPARδ或PPARγ促效劑。此PPAR配位體結合並活化PPAR，以調控在其啟動子區域中含有適當過氧化物酶體增殖劑反應性元素之基因的表現。
PPARγ促效劑可抑制人類巨噬細胞(C-Y.Jiang等人，Nature,Vol.391,82-86(1998))及T淋巴細胞(A.E.Giorgini等人，Horm.Metab.Res.Vol.31,1-4(1999))產生TNF-α及
其他炎症細胞素。最近，已發現天然PPARγ促效劑15-脫氧-△-12,14-前列腺素J2(或「15-脫氧-△-12,14-PG J2」)抑制大鼠角膜中之新血管形成及血管新生(X.Xin等人，J.Biol.Chem.Vol.274：9116-9121(1999))。Spiegelman等人在美國專利案6,242,196中揭示藉由使用PPARγ促效劑抑制PPARγ-反應性過度增生細胞的增殖之方法；Spiegelman等人揭示許多合成性PPARγ促效劑，及診斷PPARγ-反應性過度增生細胞之方法。本文中所引述所有文獻之內容係以引用之方式併入本文。PPAR在疾病與正常細胞中之表現方式不同。PPARγ在各種眼部組織，如某些視網膜及角膜層、脈絡膜毛細血管層、葡萄膜、結膜上皮及眼內肌肉中依不同程度表現(參見例如美國專利案6,316,465)。
於一態樣中，用於本發明組合物或方法中之PPARγ促效劑係噻唑烷二酮、其衍生物或其類似物。噻唑烷二酮型PPARγ促效劑之非限制性實例包括吡格列酮(pioglitazone)、曲格列酮(troglitazone)、環格列酮(ciglitazone)、恩格列酮(englitazone)、羅格列酮(rosiglitazone)及其化學衍生物。其他PPARγ促效劑包括降固醇酸酯(Clofibrate)(2-(4-氯苯氧基)-2-甲基丙酸乙酯)、降固醇酸(clofibric acid)(2-(4-氯苯氧基)-2-甲基丙酸)、GW 1929(N-(2-苯甲醯苯基)-O-{2-(甲基-2-吡啶基胺基)乙基}-L-酪胺酸)、GW 7647(2-{{4-{2-{{(環己基胺基)羰基}(4-環己基丁基)胺基}乙基}苯基}硫代}-2-甲基丙酸)及WY 14643({{4-氯-6-{(2,3-二甲基苯基)胺基}-2-嘧啶基}硫
代}乙酸)。GW 1929、GW 7647及WY 14643可自例如Koma Biotechnology,Inc.(韓國首爾)購置。於一實施例中，PPARγ促效劑係15-脫氧-△-12,14-PG J2。
PPAR-α促效劑之非限制性實例包括纖維酸酯類(fibrates)，如非諾貝特(Fenofibrate)及二甲苯氧庚酸(gemfibrozil)。PPAR-δ促效劑之非限制性實例係GW501516(購自Axxora LLC,San Diego,California或EMD Biosciences,Inc.,San Diego,California)。
於另一態樣中，本發明之組合物進一步包含抗感染藥(如抗細菌藥、抗病毒藥、抗原蟲藥或抗真菌藥，或其組合)。
於此眼部組合物中之NSAID、PPAR-結合分子、抗組織胺藥、促炎細胞素之拮抗劑或抑制劑、氧化氮合成酶抑制劑或抗感染藥之濃度可介於約0.0001至約1000 mg/ml(或者，約0.001至約500 mg/ml，或約0.001至約300 mg/ml，或約0.001至約250 mg/ml，或約0.001至約100 mg/ml，或約0.001至約50 mg/ml，或約0.01至約300 mg/ml，或約0.01至約250 mg/ml，或約0.01至約100 mg/ml，或約0.1至約100 mg/ml，或約0.1至約50 mg/ml)之範圍內。
生物衍生性抗菌藥之非限制性實例包括胺基糖苷類(aminoglycosides)(例如，丁胺卡那黴素(amikacin)、阿泊拉黴素(apramycin)、阿貝卡星(arbekacin)、班貝黴素(bambermycins)、丁胺菌素(butirosin)、地貝卡星(dibekacin)、二氫鏈霉素(dihydrostreptomycin)、福提黴素(fortimicin)、慶大黴素(gentamicin)、異帕米星
(isepamicin)、康黴素(kanamycin)、小奴黴素(micronomicin)、新黴素(neomycin)、十一烯酸新黴素(neomycin undecylenate)、奈替米星(netilmicin)、巴龍黴素(paromomycin)、核糖黴素(ribostamycin)、西索黴素(sisomicin)、壯觀黴素(spectinomycin)、鏈黴素(streptomycin)、妥布黴素(tobramycin)、丙大觀黴素(trospectomycin))、醯胺醇類(例如，疊氮氯黴素(azidamfenicol)、氯黴素(chloramphenicol)、氟甲磺氯黴素(florfenicol)、甲磺氯黴素(thiamphenicol))、袢黴素類(ansamycins)(例如，利福醯胺(rifamide)、利福平(rifampin)、利福黴素(rifamycin sv)、利福噴丁(rifapentine)、利福昔明(rifaximin))、β-內醯胺類(β-lactams)(例如，碳頭孢烯(carbacephems)(例如，氯拉卡比(loracarbef))、碳青黴烯類(carbapenems)(例如，比阿培南(biapenem)、亞胺培南(imipenem)、倍能(meropenem)、帕尼培南(panipenem))、頭孢菌素(cephalosporins)(例如，氯頭孢黴素(cefaclor)、頭孢羥胺芐(cefadroxil)、頭孢孟多(cefamandole)、羥胺唑頭孢黴素(cefatrizine)、頭孢西酮(cefazedone)、唑啉頭孢黴素(cefazolin)、頭孢卡品匹伏酯(cefcapene pivoxil)、頭孢立定(cefclidin)、頭孢地尼(cefdinir)、頭孢托侖(cefditoren)、頭孢吡肟(cefepime)、頭孢他美(cefetamet)、頭孢克肟(cefixime)、頭孢甲肟(cefinenoxime)、頭孢地嗪(cefodizime)、頭孢尼西(cefonicid)、頭孢哌酮(cefoperazone)、頭孢雷特
(ceforanide)、頭孢噻肟(cefotaxime)、頭孢替安(cefotiam)、頭孢唑蘭(cefozopran)、頭孢咪唑(cefpimizole)、頭孢匹胺(cefpiramide)、頭孢匹羅(cefpirome)、頭孢泊肟(cefpodoxime proxetil)、頭孢羅齊(cefprozil)、頭孢沙定(cefroxadine)、頭孢磺啶(cefsulodin)、頭孢他啶(ceftazidime)、頭孢特侖(cefteram)、頭孢替唑(ceftezole)、頭孢布坦(ceftibuten)、頭孢唑肟(ceftizoxime)、頭孢三嗪(ceftriaxone)、頭孢呋辛(cefuroxime)、頭孢唑喃(cefuzonam)、頭孢鈉乙腈(cephacetrile sodium)、頭孢氨苄(cephalexin)、胺基苯乙烯頭孢黴素(cephaloglycin)、先鋒黴素(cephaloridine)、先鋒黴素(cephalosporin)、先鋒黴素(cephalothin)、頭孢匹林鈉(cephapirin sodium)、塞發來定(cephradine)、特頭孢氨芐(pivcefalexin))、頭黴素類(cephamycins)(例如，頭孢布宗(cefbuperazone)、頭孢美唑(cefinetazole)、頭孢米諾(cefininox)、頭孢替坦(cefotetan)、頭孢西丁(cefoxitin))、單菌黴素類(monobactams)(例如，噻肟單醯胺菌素(aztreonam)、卡魯莫南(carumonam)、替吉莫南(tigemonam))、氧頭孢烯類(oxacephems)、頭孢佛英(flomoxef)、拉氧頭孢(moxalactam))、青黴素類(penicillins)(例如，阿姆迪諾西林(amdinocillin)、阿姆迪諾西林雙酯(amdinocillin pivoxil)、阿莫西林(amoxicillin)、胺比西林(ampicillin)、阿帕西林(apalcillin)、阿撲西林(aspoxicillin)、疊氮西林(azidocillin)、阿洛西林(azlocillin)、巴卡西林(bacampicillin)、苄基青霉酸
(benzylpenicillinic acid)、苄基青黴素鈉(benzylpenicillin sodium)、羧芐青黴素(carbenicillin)、卡茚西林(carindacillin)、氯甲西林(clometocillin)、氯灑西林(cloxacillin)、環青黴素(cyclacillin)、雙氯青黴素(dicloxacillin)、依匹西林(epicillin)、芬貝西林(fenbenicillin)、氟氯青黴素(floxacillin)、海他西林(hetacillin)、利南西林(lenampicillin)、美坦西林(metampicillin)、甲氧苯青黴素鈉(methicillin sodium)、美洛西林(mezlocillin)、乙氧萘青黴素鈉(nafcillin sodium)、惡灑西林(oxacillin)、醋甲西林(penamecillin)、氫碘酸噴沙西林(penethamate hydriodide)、芐乙胺青黴素G(penicillin G benethamine)、芐星青黴素G(penicillin G benzathine)、二苯甲胺青黴素G(penicillin G benzhydrylamine)、鈣青黴素G(penicillin G calcium)、哈胺青黴素G(penicillin G hydrabamine)、鉀青黴素G(penicillin G potassium)、普魯卡因青黴素G(penicillin G procaine)、青黴素N(penicillin N)、青黴素O(penicillin O)、青黴素V(penicillin V)、芐星青黴素V(penicillin V benzathine)、哈胺青黴素V(penicillin V hydrabamine)、青黴素V鉀哌四環素(penimepicycline)、苯氧乙基青黴素鉀(phenethicillin potassium)、氧哌嗪青黴素(piperacillin)、氨芐西林(pivampicillin)、苯丙西林(propicillin)、喹那西林(quinacillin)、磺芐青黴素(sulbenicillin)、舒他西林(sultamicillin)、酞氨芐青黴素(talampicillin)、替莫西林(temocillin)、替卡西林
(ticarcillin))、利替培南(ritipenem)、林可醯胺類(lincosamides)(例如，氯林可黴素(clindamycin)、林肯黴素(lincomycin))、大環內酯類(macrolides)(例如，阿奇黴素(azithromycin)、碳黴素(carbomycin)、克拉黴素(clarithromycin)、地紅黴素(dirithromycin)、紅黴素(erythromycin)、醋硬脂紅黴素(erythromycin acistrate)、無味紅黴素(erythromycin estolate)、紅黴素葡庚糖酸鹽(erythromycin glucoheptonate)、乳糖酸紅黴素(erythromycin lactobionate)、丙酸紅黴素(erythromycin propionate)、硬脂酸紅黴素(erythromycin stearate)、交沙黴素(josamycin)、白黴素(leucomycins)、麥迪黴素(midecamycins)、米奧卡黴素(miokamycin)、竹桃黴素(oleandomycin)、伯黴素(primycin)、羅他黴素(rokitamycin)、薔薇黴素(rosaramicin)、羅紅黴素(roxithromycin)、螺旋黴素(spiramycin)、醋竹桃黴素(troleandomycin))、多肽類(polypeptides)(例如，雙黴素(amphomycin)、桿菌肽素(bacitracin)、卷曲黴素(capreomycin)、黏菌素(colistin)、持久殺菌素(enduracidin)、結核放線菌素(enviomycin)、鐮孢真菌素(fusafungine)、短桿菌肽S(gramicidin s)、短桿菌肽(gramicidin(s))、蜜柑黴素(mikamycin)、多黏菌素(polymyxin)、原始黴素(pristinamycin)、瑞斯西丁素(ristocetin)、替考拉寧(teicoplanin)、硫鏈絲菌肽(thiostrepton)、結核放線菌素(tuberactinomycin)、短桿菌酪肽(tyrocidine)、短桿菌素(tyrothricin)、萬古黴素
(vancomycin)、紫黴素(viomycin)、維及黴素(virginiamycin)、桿菌肽鋅(zinc bacitracin))、四環素類(tetracyclines)(例如，阿哌環素(apicycline)、氯四環素(chlortetracycline)、羥甲金黴素(clomocycline)、地美環素(demeclocycline)、強力黴素(doxycycline)、胍甲環素(guamecycline)、賴甲四環素(lymecycline)、甲氯環素(meclocycline)、甲烯土黴素(methacycline)、二甲胺四環素(minocycline)、氧四環素(oxytetracycline)、青哌環素(penimepicycline)、匹哌環素(pipacycline)、羅利環素(rolitetracycline)、生環素(sancycline)、四環素(tetracycline))、環絲胺酸(cycloserine)、膜匹羅星(mupirocin)、及馬鈴薯球蛋白(tuberin)。
合成性抗菌藥之非限制性實例包括2,4-二胺基嘧啶類(例如，溴莫普林(brodimoprim)、四氧普林(tetroxoprim)、甲氧芐胺基嘧啶(trimethoprim))、硝基呋喃類(nitrofurans)(例如，呋喃他酮(furaltadone)、呋唑氯銨(furazolium chloride)、硝呋拉定(nifuradene)、硝呋拉太(nifuratel)、硝呋福林(nifurfoline)、硝呋吡醇(nifurpirinol)、硝呋拉嗪(nifurprazine)、硝呋妥因醇(nifurtoinol)、硝呋妥因(nitrofuirantoin))、喹諾酮類(quinolones)及類似物(例如，西諾沙星(cinoxacin)、環丙沙星(ciprofloxacin)、克林沙星(clinafloxacin)、二氟沙星(difloxacin)、依諾沙星(enoxacin)、氟羅沙星(fleroxacin)、氟甲喹(flumequine)、加替沙星(gatifloxacin)、格雷沙星(grepafloxacin)、左氧氟
沙星(levofloxacin)、洛美沙星(lomefloxacin)、米羅沙星(miloxacin)、莫西沙星(moxifloxacin)、那氟沙星(nadifloxacin)、萘啶酸(nalidixic acid)、諾氟沙星(norfloxacin)、氧氟沙星(ofloxacin)、奧索利酸(oxolinic acid)、帕珠沙星(pazufloxacin)、培氟沙星(pefloxacin)、吡哌酸(pipemidic acid)、吡咯嘧啶酸(piromidic acid)、羅索沙星(rosoxacin)、蘆氟沙星(rufloxacin)、施帕沙星(sparfloxacin)、替馬氟沙星(temafloxacin)、三氟沙星(tosufloxacin)、曲伐沙星(trovafloxacin)或具有以下化學名之氟喹諾酮(fluoroquinolone)：7-[(3R)-3-胺基六氫-1H-氮呯-1-基]-8-氯-1-環丙基-6-氟-1,4-二氫-4-側氧基-3-喹啉甲酸單鹽酸鹽))、磺醯胺類(sulfonamides)(例如，乙醯磺胺甲氧吡嗪(acetyl sulfamethoxypyrazine)、芐磺胺(benzylsulfamide)、氯胺B(chloramines B)、氯胺T(chloramines T)、二氯胺T(dichloramine T)、n2-甲醯磺胺異二甲嘧啶(n2-formylsulfisomidine)、n4-β-D-葡糖基苯磺醯胺(n4-β-D-glucosylsulfanilamide)、磺胺米隆(mafenide)、4'-(甲基胺磺醯基)磺胺苯胺(4'-(methylsulfamoyl)sulfanilanilide)、諾丙磺醯胺(noprylsulfamide)、鄰苯二甲醯磺胺乙醯胺(phthalylsulfacetamide)、鄰苯二甲醯磺胺噻唑(phthalylsulfathiazole)、水楊基偶氮磺胺二甲嘧啶(salazosulfadimidine)、琥珀醯基磺胺噻唑(succinylsulfathiazole)、磺胺苯沙明(sulfabenzamide)、磺胺乙醯胺(sulfacetamide)、磺胺氯達嗪(sulfachlorpyridazine)、
磺胺柯衣酸(sulfachrysoidine)、磺胺乙胞嘧啶(sulfacytine)、磺胺嘧啶(sulfadiazine)、磺胺戊烯(sulfadicramide)、磺胺二甲氧噠嗪(sulfadimethoxine)、磺胺多辛(sulfadoxine)、磺胺乙二唑(sulfaethidole)、磺胺胍(sulfaguanidine)、磺胺胍諾(sulfaguanol)、磺胺林(sulfalene)、磺胺洛西酸(sulfaloxic acid)、磺胺甲基嘧啶(sulfamerazine)、磺胺對甲氧嘧啶(sulfameter)、磺胺二甲基嘧啶(sulfamethazine)、磺胺甲噻二唑(sulfamethizole)、磺胺甲氧甲嘧啶(sulfamethomidine)、磺胺甲噁唑(sulfamethoxazole)、磺胺甲氧噠嗪(sulfamethoxypyridazine)、磺胺曲羅(sulfametrole)、磺胺柯衣定(sulfamidochrysoidine)、磺胺噁唑(sulfamoxole)、磺胺(sulfanilamide)、4-磺胺基水楊酸(4-sulfanilamidosalicylic acid)、n4-雙磺胺(n4-sulfanilylsulfanilamide)、磺胺醯脲(sulfanilylurea)、N-磺胺-3,4-醯基醯胺(N-sulfanilyl-3,4-xylamide)、磺胺硝苯(sulfanitran)、磺胺培林(sulfaperine)、磺胺苯吡唑(sulfaphenazole)、磺胺丙氧苯醯(sulfaproxyline)、磺胺吡嗪(sulfapyrazine)、磺胺吡啶(sulfapyridine)、磺胺咪唑(sulfasomizole)、磺胺均三嗪(sulfasymazine)、磺胺噻唑(sulfathiazole)、磺胺硫脲(sulfathiourea)、硫胺托拉米(sulfatolamide)、磺胺索嘧啶(sulfisomidine)、磺胺異噁唑(sulfisoxazole))、碸類(sulfones)(例如，醋胺苯碸(acedapsone)、醋地碸(acediasulfone)、磺胺苯碸鈉(acetosulfone sodium)、胺苯碸(dapsone)、地百里碸(diathymosulfone)、葡糖碸鈉
(glucosulfone sodium)、苯丙碸(solasulfone)、琥珀胺苯碸(succisulfone)、磺胺酸(sulfanilic acid)、對磺胺醯基芐胺(p-sulfanilylbenzylamine)、阿地碸鈉(sulfoxone sodium)、噻唑碸(thiazolsulfone))、氯福克酚(clofoctol)、海克西定(hexedine)、烏洛托品(methenamine)、脫水亞甲枸櫞烏洛托品(methenamine anhydromethylene citrate)、馬尿酸烏洛托品(methenamine hippurate)、杏仁酸烏洛托品(methenamine mandelate)、磺基水楊酸烏洛托品(methenamine sulfosalicylate)、硝羥喹啉(nitroxoline)、甲雙二嗪(taurolidine)及希波酚(xibomol)。於一實施例中，本發明之組合物包含選自由以下物質組成之群之抗感染藥：西諾沙星(cinoxacin)、環丙沙星(ciprofloxacin)、克林沙星(clinafloxacin)、二氟沙星(difloxacin)、依諾沙星(enoxacin)、氟羅沙星(fleroxacin)、氟甲喹(flumequine)、加替沙星(gatifloxacin)、格雷沙星(grepafloxacin)、左氧氟沙星(levofloxacin)、洛美沙星(lomefloxacin)、米羅沙星(miloxacin)、莫西沙星(moxifloxacin)、那氟沙星(nadifloxacin)、萘啶酸(nalidixic acid)、諾氟沙星(norfloxacin)、氧氟沙星(ofloxacin)、奧索利酸(oxolinic acid)、帕珠沙星(pazufloxacin)、培氟沙星(pefloxacin)、吡哌酸(pipemidic acid)、吡咯嘧啶酸(piromidic acid)、羅索沙星(rosoxacin)、蘆氟沙星(rufloxacin)、施帕沙星(sparfloxacin)、替馬氟沙星(temafloxacin)、三氟沙星(tosufloxacin)、曲伐沙星(trovafloxacin)、及具有化學名7-[(3R)-3-胺基六氫-1H-氮呯
-1-基]-8-氯-1-環丙基-6-氟-1,4-二氫-4-側氧基-3-喹啉甲酸單鹽酸鹽之氟喹諾酮(fluoroduinolone)。
抗病毒藥之非限制性實例包括利福平(Rifampin)、病毒唑(Ribavirin)、普來可那立(Pleconaryl)、西多福韋(Cidofovir)、阿昔洛韋(Acyclovir)、噴昔洛韋(Pencyclovir)、更昔洛韋(Gancyclovir)、伐昔洛韋(Valacyclovir)、泛昔洛韋(Famciclovir)、膦甲酸(Foscarnet)、阿糖腺苷(Vidarabine)、金剛胺(Amantadine)、扎那米韋(Zanamivir)、奧塞米韋(Oseltamivir)、瑞喹莫德(Resquimod)、抗蛋白酶(antiproteases)、聚乙二醇化干擾素(PegasysTM)、抗HIV蛋白酶(例如，洛匹那韋(lopinivir))、沙奎那韋(saquinivir)、安普那韋(amprenavir)、HIV融合抑制劑、核苷酸HIV RT抑制劑(例如，AZT、拉米夫定(Lamivudine)、阿巴卡韋(Abacavir))、非核苷酸HIV RT抑制劑、多康唑(Doconosol)、干擾素、丁基化羥基甲苯("BHT")、及金絲桃蒽酮(Hypericin)。
生物衍生性抗真菌劑之非限制性實例包括多烯烴類(例如，兩性黴素B(amphotericin B)、殺念珠黴素(candicidin)、制皮菌素(dermostatin)、菲律賓菌素(filipin)、制黴色基素(fungichromin)、曲古黴素(hachimycin)、哈黴素(hamycin)、光明黴素(lucensomycin)、美帕曲星(mepartricin)、游黴素(natamycin)、制黴菌素(nystatin)、培西洛星(pecilocin)、表黴素(perimycin))、氮絲胺酸(azaserine)、灰黃黴素(griseofulvin)、寡黴素(oligomycins)、十一烯酸新黴素
(neomycin undecylenate)、硝吡咯黴素(pyrrolnitrin)、癬可寧(siccanin)-7-去氮腺苷(tubercidin)、及綠膠黴素(viridin)。
合成性抗真菌藥之非限制性實例包括烯丙胺類(例如，布替萘芬(butenafine)、萘替芬(naftifine)、特比萘芬(terbinafine))、咪唑類(imidazoles)(例如，聯苯芐唑(bifonazole)、布康唑(butoconazole)、氯登妥因(chlordantoiin)、氯米達唑(chlormidazole)、氯康唑(cloconazole)、克黴唑(clotrimazole)、益康唑(econazole)、恩康唑(enilconazole)、芬替康唑(fenticonazole)、氟三唑(flutrimazole)、異康唑(isoconazole)、甲酮康唑(ketoconazole)、拉諾康唑(lanoconazole)、黴康唑(miconazole)、雙醚康唑(omoconazole)、硝酸奧昔康唑(oxiconazole nitrate)、絲他康唑(sertaconazole)、硫康唑(sulconazole)、噻康唑(tioconazole))、硫代胺基甲酸酯類(例如，托西拉酯(tolciclate)、托林達酯(tolindate)、托萘酯(tolnaftate))、三唑類(例如，氟康唑(fluconazole)、伊曲康唑(itraconazole)、沙泊那唑(saperconazole)、特康唑(terconazole))、吖啶瑣辛(acrisorcin)、阿莫羅芬(amorolfine)、苯柳胺酯(biphenamine)、溴柳氯苯胺(bromosalicylchloranilide)、丁氯柳胺(buclosamide)、丙酸鈣(calcium propionate)、氯酚甘油醚(chlorphenesin)、環匹羅司(ciclopirox)、氯羥喹(cloxyquin)、埃索帕爾(coparaffinate)、地馬唑二鹽酸鹽(diamthazole dihydrochloride)、依沙醯胺(exalamide)、氟胞嘧啶(flucytosine)、哈利他唑(halethazole)、
海克替啶(hexetidine)、氯氟卡班(loflucarban)、硝呋拉太(nifuratel)、碘化鉀(potassium iodide)、丙酸(propionic acid)、羥基吡啶硫酮(pyrithione)、水楊醯苯胺(salicylanilide)、丙酸鈉(sodium propionate)、舒苯汀(sulbentine)、替諾尼唑(tenonitrozole)、三醋精(triacetin)、芐硫噻二嗪乙酸(ujothion)、十一碳烯酸(undecylenic acid)及丙酸鋅(zinc propionate)。
抗原蟲藥之非限制性實例包括硫酸多鏈絲黴素B(polymycin B sulfate)、桿菌肽鋅(bacitracin zinc)、硫酸新黴素(neomycine sulfate)(例如，新孢黴素(Neosporin))、咪唑類(例如克黴唑(clotrimazole)、黴康唑(miconazole)、甲酮康唑(ketoconazole))、芳族二脒類(例如，羥乙磺酸普羅帕脒(propamidine isethionate)、羥乙磺酸雙溴丙脒(Brolene))、聚六亞甲基雙胍(polyhexamethylene biguanide)("PHMB"))、洗必太(chlorhexidine)、乙嘧啶(pyrimethamine(Daraprim®))、磺胺嘧啶(sulfadiazine)、亞葉酸(folinic acid(leucovorin))、克林達黴素(clindamycin)及甲氧芐胺嘧啶-磺胺甲基異噁唑(trimethoprim-sulfamethoxazole)。
於一態樣中，抗感染藥係選自由以下物質組成之群：桿菌肽鋅(bacitracin zinc)、氯黴素(chloramphenicol)、鹽酸環丙沙星(ciprofloxacin hydrochloride)、紅黴素(erythromycin)、加替沙星(gatifloxacin)、硫酸慶大黴素(gentamycin sulfate)、左氧氟沙星(levofloxacin)、莫西沙星(moxifloxacin)、氧氟沙星(ofloxacin)、乙醯磺胺鈉(sulfacetamide sodium)、多黏
菌素B(polymyxin B)、硫酸妥布黴素(tobramycin sulfate)、三氟尿苷(trifluridine)、阿糖腺苷(vidarabine)、阿昔洛韋(acyclovir)、伐昔洛韋(valacyclovir)、泛昔洛韋(famcyclovir)、膦甲酸(foscarnet)、更昔洛韋(ganciclovir)、福米韋生(formivirsen)、西多福韋(cidofovir)、兩性黴素B(amphotericin B)、游黴素(natamycin)、氟康唑(fluconazole)、伊曲康唑(itraconazole)、甲酮康唑(ketoconazole)、黴康唑(miconazole)、硫酸多黏菌素B(polymyxin B sulfate)、硫酸新黴素(neomycin sulfate)、克黴唑(clotrimazole)、羥乙磺酸普羅帕脒(propamidine isethionate)、聚六亞甲基雙胍(polyhexamethylene biguanide)、洗必太(chlorhexidine)、乙嘧啶(pyrimethamine)、磺胺嘧啶(sulfadiazine)、亞葉酸(folinic acid(leucovorin))、克林達霉素(clindamycin)、甲氧芐胺嘧啶-磺胺甲基異噁唑(trimethoprim-sulfamethoxazole)及其等組合。
於另一態樣中，本發明之組合物可進一步包含非離子性表面活性劑，如聚山梨醇酯(如聚山梨醇酯80(聚環氧乙烷山梨糖醇單油酸酯)、聚山梨醇酯60(聚環氧乙烷山梨糖醇單硬脂酸酯)、聚山梨醇酯20(聚環氧乙烷山梨糖醇單月桂酸酯)，其等商標名常稱為Tween® 80，Tween® 60、Tween® 20)、泊洛沙姆(poloxamers)(環氧乙烷與環氧丙烷之合成嵌段聚合物，如商標名常稱為Pluronic®之彼等聚合物，例如，Pluronic® F127或Pluronic® F108))，或泊洛沙明(poloxamines)(附接至乙二胺之環氧乙烷與環氧丙烷之合
成嵌段聚合物，如商標名常稱為Tetronic®之彼等聚合物，例如，Tetronic® 1508或Tetronic® 908等，其他非離子性表面活性劑，如Brij®、Myrj®及碳鏈具有約12或更多個碳原子(例如，如：約12至約24個碳原子)之長鏈脂肪醇(即，油醇、硬脂醇、十四烷醯基醇、二十二烷六烯醇等)。此等化合物出示於Martindale之第34版，pp.1411-1416(Martindale,「The Complete Drug Reference」,S.C.Sweetman(Ed.),Pharmaceutical Press,London,2005)及Remington之「The Science and Practice of Pharmacy」，第21版，p.291及第22章之內容，Lippincott Williams & Wilkins,New York,2006)；此等章節之內容係以引用之方式併入本文。當本發明組合物中包含非離子性表面活性劑時，其濃度可介於約0.001至約5重量百分比(或，約0.01至約4，或約0.01至約2，或約0.01至約1，或約0.01至約0.5重量百分比)之範圍內。
此外，本發明之組合物可包括添加劑，如緩衝劑、稀釋劑、載劑、佐劑或其他賦形劑。可使用適宜施用至眼睛之任何藥理學可接受緩衝劑。可針對各種不同目的將其他製劑用於組合物中。例如，可採用緩衝劑、防腐劑、共溶劑、油、保濕劑、潤膚劑、穩定劑或抗氧化劑。可採用之水可溶防腐劑包括亞硫酸氫鈉、硫酸氫鈉、硫代硫酸鈉、氯化苄二甲烴銨、氯丁醇、硫柳汞、乙醇、對羥基苯甲酸甲酯、聚乙烯醇、芐醇及苯乙醇。此等製劑之個別含量可為約0.001至約5重量%(較佳，約0.01%至約2重量%)。可使用之適宜水可溶性緩衝劑係碳酸鈉、硼酸鈉、磷酸鈉、乙酸鈉、
碳酸氫鈉等，如United States Food and Drug Administration(US FDA)針對所需投藥途徑所提出。此等製劑之含量應足以維持系統pH在約2與約11之間。因此，緩衝劑可至佔總組合物重量之約5重量%。調配物中亦可包含諸如但不限制於氯化鈉及氯化鉀之電解質。
於一態樣中，組合物之pH係於約4至約11之範圍內。或者，組合物之pH係於約5至約9，約6至約9，或約6.5至約8之範圍內。於另一態樣中，組合物包含pH在其中一種pH範圍內之緩衝劑。
於另一態樣中，組合物之pH約7。或者，組合物之pH在約7至約7.5範圍內。
於另一態樣中，組合物之pH約7.4。
於另一態樣中，組合物亦可包含黏性改質化合物，該等化合物經設計以促進組合物投與個體或增進個體之生物利用率。於另一態樣中，黏性改質化合物可經選擇，以使組合物在投與玻璃體後不會輕易分散。此等化合物可增強組合物之黏度，且包括但不限制於：單體多元醇，如甘油、丙二醇、乙二醇；聚合多元醇，如聚乙二醇；纖維素家族之各種不同聚合物，如羥丙基甲基纖維素(HPMC)、羧甲基纖維素(CMC)鈉、羥丙基纖維素(HPC)；多醣，如玻尿酸及其鹽、硫酸軟骨素及其鹽、葡聚糖，如葡聚糖70；水可溶蛋白質，如明膠；乙烯聚合物，如，聚乙烯醇、聚乙烯吡咯酮、聚維酮；卡波姆(carbomer)，如卡波姆934P、卡波姆941、卡波姆940或卡波姆974P；及丙烯酸聚合物。一般而
言，如，藉由Brookfield Engineering製造之具有CP-40或CP-52軸之黏度計模型DV-III Ultra或LV-III Ultra，在0.5 ml樣品容量，10至15/秒剪切速率，25℃下測量時，所需黏度可介於約1至約400厘泊(cps)之範圍內。
於另一態樣中，製備本發明組合物之方法包括組合：(i)至少DIGRA、其前藥、其醫藥可接受鹽或其醫藥可接受酯；及(ii)醫藥可接受載劑；其中該至少DIGRA係本文中所揭示之DIGRA化合物中之任一者。
於另一態樣中，製備本發明組合物之方法包括組合：(i)至少DIGRA、其前藥、其醫藥可接受鹽或其醫藥可接受酯；及(ii)與該DIGRA、該其前藥，及該其醫藥可接受鹽不同之消炎藥；及(iii)醫藥可接受載劑；其中該至少DIGRA係本文中所揭示之DIGRA化合物中之任一者。於一實施例中，此載劑可係無菌生理食鹽水溶液或生理可接受緩衝液。於另一實施例中，此載劑包含疏水性介質，如醫藥可接受油。於另一實施例中，此載劑包含疏水材料之與水之乳液。
生理可接受緩衝液包括(但不限制於)磷酸鹽緩衝液或Tris-HCl緩衝液(包含參(羥甲基)胺基甲烷及HCl)。例如，pH為7.4之Tris-HCl包含3 g/l參(羥甲基)胺基甲烷及0.76 g/l HCl。於另一態樣中，緩衝液係10×磷酸鹽緩衝液生理食鹽水(PBS)或5×PBS溶液。
在某些環境中，亦可適宜或需要其他緩衝液，如：基於以下物質之緩衝液：HEPES(N-{2-羥乙基}哌嗪-N'-{2-乙磺酸})，在25℃下之pKa為7.5且pH範圍在約6.8至8.2之範圍
內；BES(N,N-雙{2-羥乙基}2-胺基乙磺酸)，在25℃下之pKa為7.1且pH在約6.4至7.8之範圍內；MOPS(3-{N-嗎啉基}丙磺酸)，在25℃下之pKa為7.2且pH在約6.5至7.9之範圍內；TES(N-參{羥甲基}-甲基-2-胺基乙磺酸)，在25℃下之pKa為7.4且pH在約6.8至8.2之範圍內；MOBS(4-{N-嗎啉基}丁磺酸)，在25℃下之pKa為7.6且pH在6.9至8.3之範圍內；DIPSO(3-(N,N-雙{2-羥乙基}胺基)-2-羥基丙烷)，在25℃下之pKa為7.52且pH在約7至8.2之範圍內；TAPSO(2-羥基-3-{參(羥甲基)甲基胺基}-1-丙磺酸)，在25℃下之pKa為7.61且pH在約7至8.2之範圍內；TAPS({(2-羥基-1,1-雙(羥甲基)乙基)胺基}-1-丙磺酸)，在25℃下之pKa為8.4且pH在約7.7至9.1之範圍內；TABS(N-參(羥甲基)甲基-4-胺基丁磺酸)，在25℃下之pKa為8.9且pH在約8.2至9.6之範圍內；AMPSO(N-(1,1-二甲基-2-羥乙基)-3-胺基-2-羥基丙磺酸)，在25℃下之pKa為9.0且pH在約8.3至9.7之範圍內；CHES(2-(環己基胺基)乙磺酸)，在25℃下之pKa為9.5且pH在約8.6至10.0之範圍內；CAPSO(3-(環己基胺基)-2-羥基-1-丙磺酸)，在25℃下之pKa為9.6且pH在約8.9至10.3之範圍內；或CAPS(3-(環己基胺基)-1-丙烷磺酸)，在25℃下之pKa為10.4且pH在約9.7至11.1之範圍內。
於特定實施例中，本發明之組合物係在具有酸性pH(如：約4至約6.8，或約5至約6.8)之緩衝液中調配。於此等實施例中，組合物之緩衝能力需讓組合物在投與病患之後快速到達生理pH。
應理解，以下實例中之各組分或混合物之比例可針對適當情況進行修改。
分別藉由混合表1中所出示之成分製造兩種混合物I及II。將五份(重量比)混合物I與一份(重量比)混合物II混合15分鐘或更長時間。利用1 N NaOH將組合混合物之pH調整至6.2至6.4，以獲得本發明之組合物。
或者，可改用諸如魚肝油、花生油、芝麻油、椰子油、向日葵油、玉米油或橄欖油之油替代純水，以產生包含式IV化合物之油基調配物。
分別藉由混合表2中所出示之成分製造兩種混合物I及II。將五份(重量比)混合物I與兩份(重量比)混合物II混合15分鐘或更長時間。利用1 N NaOH將組合混合物之pH調整至6.2至6.4以獲得本發明之組合物。
或者，可改用諸如魚肝油、花生油、芝麻油、椰子油、向日葵油、玉米油或橄欖油之油替代純水，以產生包含式IV化合物之油基調配物。
分別藉由混合表3中所出示之成分製造兩種混合物I及II。將五份(重量比)混合物I與兩份(重量比)混合物II混合15分鐘或更長時間。利用1 N NaOH將組合混合物之pH調整至6.2至6.4以獲得本發明之組合物。
分別藉由混合物表4中所出示之成分製造兩種混合物I及II。將五份(重量比)混合物I與一份(重量比)混合物II混合15分鐘或更長時間。利用1 N NaOH將組合混合物之pH調整至6.2至6.4以獲得本發明之組合物。
將表5中所出示之成分一起混合至少15分鐘。利用1 N NaOH將混合物之pH調整至6.2至6.4以獲得本發明之組合物。
將表6中所出示之成分一起混合至少15分鐘。利用1 N NaOH將混合物之pH調整至6.2至6.4以獲得本發明之組合物。
將表7中所出示之成分一起混合至少15分鐘。利用1 N
NaOH將混合物之pH調整至6.2至6.4以獲得本發明之組合物。
將表8中所出示之成分一起混合至少15分鐘。利用1 N NaOH將混合物之pH調整至6.2至6.4以獲得本發明之組合物。
將表9中所出示之成分一起混合至少15分鐘。利用1 N NaOH將混合物之pH調整至6.2至6.4以獲得本發明之組合物。
將表10中所出示之成分一起混合至少15分鐘。利用1 N NaOH將混合物之pH調整至6.2至6.4以獲得本發明之組合物。
分別藉由混合表11中所出示之成分製造混合物I及II。將五份(重量比)混合物I與一份(重量比)混合物II混合15分鐘或更長時間。利用1 N NaOH將組合混合物之pH調整至6.2至6.4以獲得本發明之組合物。
分別藉由混合表12中所出示之成分製造混合物。將一份(重量比)此混合物添加至200 g純水，及劇烈混合15分鐘或更長時間。利用1 N NaOH將組合混合物之pH調整至6.4至7.0以獲得本發明之組合物。
分別藉由混合表13中所出示之成分製造混合物。將一份
(重量比)此混合物添加至200 g純水，及劇烈混合15分鐘或更長時間。利用1 N NaOH將組合混合物之pH調整至6.4至7.0以獲得本發明之組合物。
分別藉由混合表14中所出示之成分製造混合物。將一份(重量比)此混合物添加至200 g純水，及劇烈混合15分鐘或更長時間。利用1 N NaOH將組合混合物之pH調整至6.4至7.0以獲得本發明之組合物。
於另一態樣中，將DIGRA、其前藥、其醫藥可接受鹽或其醫藥可接受酯及消炎藥合併成用於局部投與、系統投與、眼周注射或玻璃體內注射之調配物。可注射玻璃體內調配物適宜包含載劑，該載劑提供活性成分緩釋，如持續超過約1週(或超過約1、2、3、4、5或6個月)之時間內。於
特定實施例中，該緩釋調配物宜包含不溶或僅難溶於玻璃體中之載劑。此載劑可係油性液體、乳液、凝膠或半固體。油性液體之非限制性實例包括蓖麻油、花生油(peanut oil)、橄欖油、椰子油、芝麻油、棉籽油、玉米油、向日葵油、魚油、花生油(arachis oil)及液體蠟。
於一實施例中，本發明之化合物或組合物可利用細針頭(如25至30號)注射至眼部組織中。一般而言，將約25 μl至約100 μl量之包含DIGRA、其前藥、其醫藥可接受鹽或其醫藥可接受酯之組合物投與病患。此DIGRA、其前藥或其醫藥可接受酯之濃度係在上述範圍內選擇。
於另一態樣中，將DIGRA、其前藥、其醫藥可接受鹽或其醫藥可接受酯合併至眼科裝置或系統中，該裝置或系統包含生物可降解材料，及該裝置可注射或植入個體以長期(例如，超過約1週，或超過約1、2、3、4、5或6個月)治療或預防眼部發炎性疼痛。此裝置系統可藉由熟悉此相關技術之醫師注射或植入個體眼部或眼周組織。
於另一態樣中，治療、控制、減輕或改善發炎性疼痛之方法包括：(a)提供包含DIGRA、其前藥、其醫藥可接受鹽或其醫藥可接受酯之組合物；及(b)將有效量之該組合物以足夠高的頻率投與個體(如個體之眼睛)，以治療、控制、減輕或改善發炎性疼痛。
於另一態樣中，治療、控制、減輕或改善手術後發炎性疼痛之方法包括：(a)提供包含DIGRA、其前藥、其醫藥可接受鹽或其醫藥可接受酯之組合物；及(b)將有效量之該組
合物以足夠高的頻率投與個體(例如，受影響之組織)，以治療、控制、減輕或改善手術後發炎性疼痛。
於另一態樣中，治療、控制、減輕或改善手術後眼部疼痛之方法包括：(a)提供包含DIGRA、其前藥、其醫藥可接受鹽或其醫藥可接受酯之組合物；及(b)將有效量之該組合物以足夠高的頻率投與個體之受影響眼睛，以治療、控制、減輕或改善手術後眼部疼痛；其中該DIGRA係本文中所揭示之DIGRA化合物中之任一者。
於另一態樣中，治療、控制、減輕或改善手術後眼部疼痛之方法包括將有效量之包含DIGRA、其前藥、其醫藥可接受鹽或其醫藥可接受酯之組合物以足夠高的頻率投與個體之受影響眼睛，以治療、控制、減輕或改善手術後眼部疼痛，其中該方法使個體中IOP之升高程度低於使用糖皮質激素時之方法，及其中該DIGRA係本文中所揭示之DIGRA化合物中之任一者。
於另一態樣中，治療、控制、減輕或改善手術後眼部疼痛之方法包括將有效量之包含DIGRA、其前藥、其醫藥可接受鹽或其醫藥可接受酯之本發明組合物以足夠高的頻率投與個體之受影響眼睛，以治療、控制、減輕或改善手術後眼部疼痛；其中該方法使個體中IOP之升高程度低於使用地塞米松(dexamethasone)或潑尼松龍(prednisolone)時之方法，及其中該DIGRA係本文中所揭示之DIGRA化合物中之任一者。
於另一態樣中，治療、控制、減輕或改善手術後眼部疼
痛之方法包括將有效量之包含DIGRA、其前藥、其醫藥可接受鹽或其醫藥可接受酯之組合物以足夠高的頻率投與個體之受影響眼睛，以治療、控制、減輕或改善手術後眼部疼痛；其中糖皮質激素不適合或不建議用於該個體；及其中該DIGRA係本文中所揭示之DIGRA化合物中之任一者。
於另一態樣中，治療、控制、減輕或改善手術後眼部疼痛之方法包括：(a)提供包含DIGRA、其前藥、其醫藥可接受鹽或其醫藥可接受酯之組合物，及(b)將有效量之該組合物以足夠高的頻率投與個體之受影響眼睛，以治療、控制、減輕或改善發炎性疼痛；其中糖皮質激素不適合或不建議用於該個體，因為無法接受IOP升高之風險。
於一實施例中，該DIGRA係選自以上揭示之彼等化合物。
於另一實施例中，此疼痛之根本原因係發炎。於另一實施例中，此發炎係持續一或多週(例如，1、2、3、4、5、6或更多週)之發炎。
於另一實施例中，本發明提供一種治療、控制、改善、緩解或預防由眼部創傷或損傷(如眼部手術)所導致之眼部疼痛之方法。治療、控制、減輕、改善、緩解或預防由眼部創傷或損傷導致之眼部疼痛(手術後眼部疼痛)之方法包括：(a)提供包含DIGRA、其前藥、其醫藥可接受鹽或其醫藥可接受酯之組合物，及(b)將有效量之該組合物以足夠高的頻率投與個體之受影響眼睛，以治療、控制、減輕、改善、緩解或預防手術後眼部疼痛；其中糖皮質激素不適合或不建議用於該個體，因為無法接受IOP升高之風險；及其
中該DIGRA係本文中所揭示之DIGRA化合物中之任一者。
於另一實施例中，用於以上方法之任一者中之組合物進一步包含與DIGRA、其前藥、其醫藥可接受鹽及其醫藥可接受酯不同之消炎藥。此消炎藥係選自上文所揭示之彼等物質。DIGRA、其前藥、其醫藥可接受鹽、其醫藥可接受酯及消炎藥之濃度係在以上揭示之範圍內選擇。
於另一實施例中，用於以上方法之任一者中之組合物進一步包含NSAID(如溴芬酸(bromfenac)、奈帕芬胺(nepafenac)、酮咯酸(ketorolac)或茚甲新(indomethacin))。
於另一態樣中，本發明之組合物係經玻璃體內或眼周投與。於另一態樣中，本發明之組合物係合併至眼部植入系統或裝置中，及該植入系統或裝置係以手術方式植入玻璃體腔中或病患眼睛之後方，用於持續或長期釋放活性成分。適宜用於本發明方法中之常見植入系統或裝置包含生物可降解基質及浸漬或分散於其中之活性成分。用於持續釋放活性成分之眼部植入系統或裝置之非限制性實例揭示於美國專利案5,378,475、5,773,019、5,902,598、6,001,386、6,051,576及6,726,918中，該等案之內容係以引用之方式併入本文。
於另一態樣中，本發明之組合物每天投與一次，每天數次(例如，兩次、三次、四次或更多次)、每週一次、每週兩次、每週三次、每週四次或以經過確定適合病況的適宜頻率投與，歷時一或多週，或直至疼痛實質上已消失。
本發明之方法可與常用於控制、減輕、治療或預防發炎性疼痛(如手術後疼痛或手術後眼部疼痛)之其他治療性及輔助或預防藥物一起使用，藉此增強總體治療或增強用於治療及處理此類發炎性疼痛之其他治療性藥物、預防性藥物及輔助性藥物之作用。用於控制、減輕、治療或預防發炎性疼痛之治療性藥物包括止痛劑或NSAID，其等直接投與至受影響之組織或經口投與。
某些目前使用的治療性藥劑可能需要高劑量達到目標反應程度，但通常可能導致較高頻率之劑量相關不良作用。因此，本發明化合物或組合物與常用於控制、減輕、治療或預防發炎性疼痛之藥物的組合使用容許使用相對低劑量之此等其他藥物，進而使與長期投與此等治療劑相關的不良副作用之頻率下降。因此，本發明之化合物或組合物之另一適應症係減少用於控制、減輕、治療或預防發炎性疼痛之先前技藝藥物的不良副作用，如全身性不良副作用之惡化(例如，胃腸道不良事件、腎功能受損、充血性心臟衰竭事件、IOP升高或糖尿病)。
糖皮質激素及DIGRA之副作用可在其等用於治療示例性發炎時進行對比。
於一態樣中，在體內或體外確定至少一種不良副作用程度。例如，該至少一種不良副作用程度係在體外進行細胞培養，及確定與該副作用相關的生物標記之濃度來測定。此等生物標記可包括參與或作為導致該不良副作用之生物
化學級聯的產物之蛋白質(例如，酶)、脂質、糖及其衍生物。代表性之體外測試方法進一步揭示於下文。
於另一實施例中，該至少一種不良副作用程度係在體內，於該糖皮質激素或DIGRA(或其前藥、其醫藥可接受鹽或其醫藥可接受酯)首次投與且存在於該個體後約一天時測定。於另一實施例中，該至少一種不良副作用程度係在該組合物首次投且及存在於該個體後約14天時測定。於另一實施例中，該至少一不良副作用程度係在該組合物首次投與且存在於該個體中後約30天時測定。或者，該至少一種不良副作用程度係在該等化合物或組合物首次投與且存在於該個體中後約2、3、4、5或6個月時確定。
於另一態樣中，用於治療該示例性炎症之該糖皮質激素係以足夠高的劑量及頻率投與該個體，以在歷經相同時間後，對該炎症產生等效於本發明化合物或組合物的有益作用。
糖皮質激素療法(如消炎療法)之最常見之非所需作用之一係類固醇糖尿病。此非所需病症之原因係使蛋白質降解所生成之游離胺基酸進行糖生成及代謝(糖皮質激素異化代謝作用)之肝臟酶被誘導轉錄，刺激肝內之糖生成作用。在肝內之異化代謝作用之關鍵酶係酪胺酸胺基轉移酶(TAT)。此酶之活性可藉由光度測定經處理大鼠肝細胞之細胞培養物之方式測定。因此，可藉由測量此酶之活性，比較由糖皮質激素導致之糖生成作用與由DIGRA導致之糖生成作用。例如，於一方案中，以測試物質(DIGRA或糖皮質
激素)處理細胞達24小時，及隨後測量TAT活性。然後比較所選擇之DIGRA與糖皮質激素之TAT活性。可使用其他肝臟酶替代TAT，如磷酸烯醇丙酮酸羧激酶、葡萄糖-6-磷酸酶或果糖-2,6-雙磷酸酶。或者，可直接測量動物模型之血糖濃度並比較接受糖皮質激素治療所選擇病況及藉由DIGRA治療相同病況之個體。
糖皮質激素療法之另一非所需結果係GC誘導白內障。化合物或組合物之白內障形成能力可藉由定量該化合物或組合物在體外對鉀離子通過水晶體細胞(如哺乳動物水晶體上皮細胞)膜之流量之作用來測定。此離子流量可藉由例如電生理學技術或離子流量成像技術(如藉由使用螢光染料)測定。用於測定化合物或組合物之白內障形成能力之示例性體外方法揭示於美國專利申請公告案2004/0219512中，該案之內容係以引用之方式併入本文。
糖皮質激素療法之另一非所需結果係高血壓。可直接測量藉由糖皮質激素及DIGRA治療發炎性病況之類似匹配個體之血壓並比較。
糖皮質激素療法之另一非所需結果係IOP升高。可直接測量接受糖皮質激素及DIGRA治療發炎性病況之類似匹配個體之IOP並比較。
用於對比性測試(例如，以上方案)中之糖皮質激素可選自由以下物質組成之群：21-乙酸基孕烯醇酮(21-acetoxypregnenolone)、阿氯米松(alclometasone)、阿爾孕酮(algestone)、安西縮松(amcinonide)、倍氯米松
(beclomethasone)、倍他米松(betamethasone)、布地索松(budesonide)、氯潑尼松(chloroprednisone)、氯倍他索(clobetasol)、氯倍他松(clobetasone)、氯可托龍(clocortolone)、氯潑尼醇(cloprednol)、腎上腺酮(corticosterone)、可的松(cortisone)、可的伐唑(cortivazol)、地夫可特(deflazacort)、羥潑尼縮松(desonide)、去羥米松(desoximetasone)、地塞米松(dexamethasone)、雙氟拉松(diflorasone)、雙氟米松(diflucortolone)、二氟潑尼松龍酯(difluprednate)、甘草次酸(enoxolone)、氟扎可送(fluazacort)、氟氯奈德(flucloronide)、氟米松(flumethasone)、氟尼索松(flunisolide)、氟輕鬆(fluocinolone acetonide)、氟欣諾能(fluocinonide)、氟可汀丁酯(fluocortin butyl)、氟可龍(fluocortolone)、氟米龍(fluorometholone)、醋酸氟培龍(fluperolone acetate)、醋酸氟潑尼定(fluprednidene acetate)、氟潑尼龍(fluprednisolone)、氟氫縮松(flurandrenolide)、丙酸氟替卡松(fluticasone propionate)、醛基縮松(formocortal)、哈西縮松(halcinonide)、丙酸鹵倍他索(halobetasol propionate)、鹵美他松(halometasone)、醋酸鹵潑尼松(halopredone acetate)、氫可松胺酯(hydrocortarnate)、氫化可的松(hydrocortisone)、氯替潑諾碳酸乙酯(loteprednol etabonate)、馬潑尼酮(mazipredone)、甲羥松(medrysone)、甲潑尼松(meprednisone)、甲強龍(methylprednisolone)、糠酸莫米他松(mometasone furoate)、帕拉米松(paramethasone)、潑
尼卡酯(prednicarbate)、潑尼松龍(prednisolone)、25-二乙基胺基乙酸潑尼松龍(prednisolone 25-diethylamino-acetate)、磷酸潑尼松龍鈉(prednisolone sodium phosphate)、強的松(prednisone)、潑尼松龍戊酸酯(prednival)、潑尼立定(prednylidene)、雙甲丙醯龍(rimexolone)、氫可的松(tixocortol)、去炎松(triamcinolone)、丙炎松(triamcinolone acetonide)、苯曲安奈德(triamcinolone benetonide)、己曲安奈德(triamcinolone hexacetonide)、其生理可接受鹽、其組合及其混合物。於一實施例中，該糖皮質激素係選自由以下物質組成之群：地塞米松(dexamethasone)、強的松(prednisone)、潑尼松龍(prednisolone)、甲強龍(methylprednisolone)、甲羥松(medrysone)、去炎松(triamcinolone)、氯替潑諾碳酸乙酯(loteprednol etabonate)、其生理可接受鹽、其組合及其混合物。於另一實施例中，該糖皮質激素可接受用於眼部。於另一實施例中，該糖皮質激素係潑尼松龍、地塞米松或去炎松。
發炎過程之起源為多方向性，且其特徵在於涉及許多均無法證實之組分之複雜之細胞及分子事件。前列腺素屬於此等介體，且在特定之眼部炎症形式中具有重要作用。兔眼睛前房穿刺因擾亂血-房水障壁(BAB)而誘發發炎性反應，此至少部份地由前列腺素E2介導[以下參考文獻1至3]。
在眼內或局部投與PGE2會擾亂BAB。[以下參考文獻4]。在此研究中所採用之治療計劃係類似在病患進行白內障手術前由外科醫生所使用臨床NSAID(歐克芬(Ocufen))治療計劃。吾人在兔穿刺模型上研究不同劑量下之解離糖皮質激素受體促效劑(BOL-303242-X，具有上式IV之化合物)，評估房水生物標記濃度，及虹膜睫狀體MPO活性，並與媒劑、地塞米松(dexamethasone)、氯替潑諾(loteprednol)及氟比洛芬(flurbiprofen)對比。
BOL-303242-X(0.1%、0.5%及1%局部調配物)，批號2676-MLC-107，美國Rochester之Bausch & Lomb Incorporated(B&L)。
媒劑(10% PEG 3350；1% Tween 80；磷酸鹽緩衝液pH 7.00)，批號2676-MLC-107，美國B&L Rochester。
Visumetazone®(0.1%地塞米松(dexamethasone)局部調配物)，批號T253，義大利羅馬之Visufarma。
Lotemax®(0.5%氯替潑諾(Loteprednol)局部調配物)，批號078061，義大利Macherio之B&L IOM。
Ocufen®(0.03%氟比洛芬(flurbiprofen)局部調配物)，批號E45324，愛爾蘭Westport之Allergan。
物種：兔
品種：紐西蘭
來源：Morini(Reggio Emila，義大利)
性別：雄性
實驗開始時之年齡：10週
實驗開始時之體重範圍：2.0至2.4 kg
動物總數量：28
識別：以文數編碼標記耳朵(即，A1意指測試物A及動物1)。
評斷性：兔係用於藥物動力學研究中之標準非齧齒物種。用於此研究中之動物之數量係(由相關研究者判斷)合理實施此類研究所需之最小數量，且遵守世界管制指導原則。
適應/檢疫：到達後，由獸醫評估動物之基本健康。在動物接收至實驗開始經歷7天，以使動物適應實驗室環境，並觀察其等感染疾病之進展。
動物飼養：將所有動物飼養在清潔且已消毒之室內，恒定溫度(22±1℃)，濕度(相對濕度30%)，及在恒定光照-黑暗循環下(光照時間為8：00至20：00)。可自由攝取來自市售商品之飼料及自來水。在實驗前測量其等體重(表T-1)。所有動物均具有位於體重分佈曲線之中央部分(10%)內之體重。以來自同一供應商之類似年齡及體重的動物替換四隻兔子，係因其中三隻出現眼部炎症跡象及一隻在到達時死亡。
動物福利提供：所有實驗係依照ARVO(視覺及眼科研究協會(Association for Research in Vision and Ophthalmology))對研究中之動物使用之指導原則進行。沒有已充分驗證以
容許替代活的動物在此研究中的用途之備選測試系統。已竭盡所能獲得盡可能最大量資訊，同時儘量減少此研究所需的動物數量。就吾人所知，此研究並非不必要或重複。研究準則係交由卡塔尼亞大學(University of Catania)之機構動物照顧及使用委員會(Institutional Animal Care and Use Committee)(IACUC)審核，且遵從動物福利照料的可接受標準。
將28隻兔隨機編排成如下表所顯示之7組(4隻動物/組)。
將字母A至G隨機分配與各測試物
A=媒劑(10% PEG3350/1% Tween 80/PB pH 7.00)
B=歐克芬(Ocufen)(氟比洛芬(flurbiprofen)，0.03%)
C=Visumetazone(地塞米松(dexamethasone)0.1%)
D=Lotemax(氯替潑諾碳酸乙酯(loteprednol etabonate)0.5%)
E=BOL-303242-X 0.1%(1 mg/g)
F=BOL-303242-X 0.5%(5 mg/g)
G=BOL-303242-X 1%(10 mg/g)
將3.9 g NaH2PO4 2H2O溶於容量瓶中，以水補足至500 ml。藉由3 N NaOH將pH調整至pH=6。
將0.5 g十六烷基-三甲基溴化銨溶於100 ml磷酸鹽緩衝液中。
新鮮製備該溶液。加水稀釋10微升H2O2(30重量%)至1 ml(溶液A)。將7.5 mg鄰聯茴香胺2HCl溶於45 ml磷酸鹽緩衝液中，及添加75 μl溶液A。
將每隻兔放置在約束裝置中，及以文數編碼標記。在首次穿刺前之180、120、90及30分鐘時，及隨後在首次穿刺後之15、30、90分鐘時，將調配物滴注(50 μl)至兩眼之結膜囊中。為了實施首次穿刺，藉由靜脈內注射5 mg/kg Zoletil®(Virbac；2.5 mg/kg噻環乙胺(tiletamine)HCl及2.5
mg/kg唑氟氮草(zolazepam)HCl)麻醉動物，及將一滴局部麻醉劑(Novesina®，Novartis)投與眼睛。藉由連接至結核菌素注射器之26 G針頭實施前房穿刺；將針頭經角膜插入前房，小心地進行以免破壞組織。在首次穿刺2小時後，以0.4 ml Tanax®(Intervet International B.V.)殺死動物，及進行二次穿刺。在二次穿刺時取出約100 μl眼房液。將眼房液立即分為四份樣液，及保存在-80℃下直至分析。隨後摘除兩眼球，及小心切除虹膜睫狀體，置於聚丙烯試管中，並保存在-80℃下直至分析。
藉由Castroviejo測徑規測量首次穿刺前180分鐘及5分鐘時及二次穿刺前5分鐘時之兩眼之瞳孔直徑。
藉由裂隙燈(4179-T；Sbisà，義大利)在首次穿刺前之180分鐘及5分鐘時及二次穿刺前之5分鐘時實施兩眼睛之臨床評估。依照以下計劃給予臨床得分：
0=正常
1=虹膜及結膜血管離散擴張
2=虹膜及結膜血管中等擴張
3=嚴重虹膜充血及前房閃輝
4=嚴重虹膜充血及前房閃輝且存在纖維狀滲出液。
吾人使用PGE2免疫檢測套組(R&D系統；目錄編號KGE004；批號240010)定量眼房液中之PGE2。藉由套組所
提供之校正稀釋劑溶液，將十一微升或16 μl眼房液稀釋至110 μl或160 μl。將一百微升樣品及標準品置於96-孔盤中，及以平板格式記錄。依照套組中所描述之檢測方案處理樣品。使用設定在450 nm(在540 nm下進行波長校正)之微量滴定盤讀數器(GDV，義大利；機型DV 990 B/V6)校正及分析樣品。
吾人使用蛋白質定量套組(Fluka；目錄編號77371；批號1303129)測定眼房液之蛋白質濃度。加水稀釋五微升眼房液至100 μl。將二十微升樣品及標準品置於96-孔盤中，以平板格式記錄。依照套組中所描述之檢測方案處理樣品。使用設定在670 nm之微量滴定盤讀數器(GDV，義大利；機型DV 990 B/V6)校正及分析樣品。
吾人使用血球計數器(Improved Neubauer Chamber；Bright-line，Hausser Scientific)及Polyvar 2顯微鏡(Reichert-Jung)測定白血球數量。
吾人使用LTB4免疫檢測套組(R&D系統；目錄編號KGE006；批號243623)定量眼房液之LTB4濃度。藉由套組所提供之校正稀釋劑溶液將11 μl眼房液稀釋至110 μl。將100 μl樣品及標準品置於96-孔盤中，及以平板格式記錄。依照套組中所描述之檢測方案處理樣品。使用設定在450 nm(在540 nm下進行波長校正)之微量滴定盤讀數器(GDV，
義大利；機型DV 990 B/V6)校正及分析樣品。
如上所述般由Williams等人[5]測量MPO活性。小心乾燥虹膜睫狀體，稱重及浸沒在1 ml十六烷基-三甲基-溴化銨溶液中。隨後，在冰上，藉由超音波均質器(HD 2070，Bandelin electronic)對樣品超音波處理10秒，凍熔三次，超音波處理10秒，及在14,000 g下離心10分鐘，以移除細胞碎片。使用鄰聯茴香胺2HCl/H2O2溶液稀釋上清液樣液(40至200 μl)至3 ml。藉由分光光度計(UV/Vis Spectrometer Lambda EZ 201；Perkin Elmer)在5分鐘內連續監視460 nm下之吸光度變化。確定各樣品之線性斜率(△/min)，及如下用於計算組織中之MPO單元數量：
其中ε=11.3 mM-1。
數值係以MPO單元/g組織表示。
瞳孔直徑、PGE2、蛋白質、PMN及MPO係以平均值±SEM表示。利用單向ANOVA，接著Newman-Keuls事後試驗法進行統計學分析。臨床得分係以眼睛%表示，且統計學分析係利用Kruskal-Wallis，接著Dunn事後試驗法進行。這兩種情況中，P<0.05視為具統計顯著性。將Prism 4軟體(GraphPad Software Inc.)用於分析及作圖。
原始數據顯示於表T-2及T-3中。CRT與所有處理之間未發現統計學顯著性。
原始數據顯示於表T-4及T-5中。僅有0.5% LE組相對於CTR出現顯著差異(p<0.05)。
原始數據顯示於表T-6及T-7中。0.03% F、0.5% LE、0.1% BOL及0.5% BOL之處理法均相對於CTR出現統計顯著性(p<0.05)。因此，在此測試中之0.5% BOL說明其可有效治療、控制或改善發炎性疼痛(如手術後發炎性疼痛或手術後眼部疼痛)。
原始數據顯示於表T-8及T-9中。已發現0.03% F及1% BOL處理相對於CTR出現統計學顯著性且p<0.01，及0.5% BOL處理法相對於CTR出現統計顯著性且p<0.05。
原始數據顯示於表T-10及T-11中。所有處理法均相對於CTR出現統計顯著性(p<0.001)。
所有樣品均在檢測之定量限值(約0.2 ng/ml)以下。
原始數據顯示於表T-12及T-13中。已發現所有處理法均相對於CTR出現統計顯著性，其中0.03% F為p<0.01，及對於0.1%
Dex、0.5% LE、0.1% BOL、0.5% BOL及1% BOL，p<0.001。
自所產生之數據獲得之初步結論係：
˙BOL-303242-X在此模型中呈活性。
˙BOL-303242-X與NSAID及類固醇正對照之間沒有巨大差異。
就BOL-303242-X而言，沒有出現顯著劑量反應，可能因為吾等已在此等劑量下獲得最大效能或最大藥物曝露量。然而，結果顯示，BOL-303242-X在作為消炎藥時之有效性類似於某些獲得廣泛接受之先前技藝類固醇或NSAID。某些其他最初步數據(未顯示)說明BOL-303242-X不具有腎上腺皮質類固醇之某些副作用。
1. Eakins KE (1977). Prostaglandin and non prostaglandin-mediated breakdown of the blood-aqueous barrier. Exp. Eye Res., Vol. 25, 483-498.
2. Neufeld AH, Sears ML (1973). The site of action of prostaglandin E2 on the disruption of the blood-aqueous barrier in the rabbit eye. Exp. Eye Res., Vol. 17, 445-448.
3. Unger WG, Cole DP, Hammond B (1975). Disruption of the blood-aqueous barrier following paracentesis in the rabbit. Exp. Eye Res., Vol. 20, 255-270.
4. Stjernschantz J (1984). Autacoids and Neuropeptides. In: Sears, ML (ed.) Pharmacology of the Eye.
Springer-Verlag, New York, pp. 311-365.
5. Williams RN, Paterson CA, Eakins KE, Bhattacherjee P (1983) Quantification of ocular inflammation: evaluation of polymorphonuclear leukocyte infiltration by measuring myeloperoxidase activity. Curr. Eye Res., Vol. 2, 465-469.
與免疫細胞締合之細胞素之濃度係此等細胞在發炎性病況中之活性之直接指標。此等細胞素之濃度下降說明測試化合物對炎症之正向治療作用。此研究經設計以確定BOL-303242-X對人類角膜上皮細胞(HCEC)中之IL-1β-誘導產生細胞素之作用。
使用30-細胞素Luminex套組確定BOL-303242-X對初代人類角膜上皮細胞中之IL-1β-刺激細胞素表現之作用。
將地塞米松(dexamethasone)用作對照。
將初代HCEC接種在24-孔盤中。24小時後，藉由溶於基本EpiLife培養基中之媒劑、IL-1β、IL-1β+地塞米松，或IL-1β+BOL-303242-X處理細胞18小時(表T-14)。各處理重複實施三次。收集培養基及利用30-細胞素Luminex套組用於確定細胞素含量。藉由alamarBlue檢測(LP06013)測定細胞存活率。
地塞米松(dexamethasone)：
批號：016K14521
母本MW：392.46
母本：總MW比=1.0
BOL-303242-X：
批號：6286
母本MW：46.48
母本：總MW比=1.0
基於Luminex所檢測之各細胞素標準曲線，將平均螢光強度(MFI)用於獲得各種細胞素之濃度(pg/ml)。採用各種細胞素之標準曲線之線性範圍來測定細胞素濃度。取各樣品兩重覆測定值之平均值。數據以平均值±SD表示。利用單向ANOVA-Dunnett試驗法進行統計學分析，及將P<0.05視為具統計顯著性。
在各處理中未觀察到對細胞代謝活性之統計顯著性作用(藉由alamarBlue檢測法測定)。
此研究中，在30種測試細胞素中偵測到16種顯著量之細胞素，且在14種細胞素中偵測到有13種係受到10 ng/ml IL-1β刺激所產生(表T-14)。將IL-1β自分析中剔除，因為其成為刺激物。剔除IL-1ra，因為MFI不在標準範圍內。
地塞米松(dexamethasone)及BOL-303242-X對6種細胞素(IL-6、IL-7、MCP-1、TGF-α、TNF-α及VEGF)以類似的效能顯著抑制IL-1β刺激產生細胞素，且在1 nM對IL-6及在10 nM對MCP-1、TGF-α及TNF-α的情況下，觀察到顯著抑制作用(表T-14及圖1A至1F)。已知IL-6、IL-8及TNF-α可誘導強烈痛覺過敏。IL-6亦可介導前列腺素合成。D.J.Tracey及J.S.Walker,Inflamm.Res.,Vol.44,407(1995)。BOL-303242-X抑制此等細胞素產生之能力進一步證實此化合物可治療、控制、減輕、改善或預防發炎性疼痛，尤其是手術後疼痛或手術後眼部疼痛之有用藥物。如本文中所揭示之測試所
證實，此藥物可提供使IOP升高之機率低於地塞米松(dexamethasone)之效益。
BOL-303242-X亦以高於地塞米松(dexamethasone)之效能顯著抑制IL-1β所刺激產生之G-CSF，及觀察到BOL-303242-X在10 μg/ml下具有顯著抑制作用，而地塞米松對此細胞素無顯著作用(圖2)。
BOL-303242-X亦以低於地塞米松(dexamethasone)之效能顯著抑制IL-1β所刺激產生之3種細胞素(GM-CSF、IL-8及RANTES)。於1 nM地塞米松(dexamethasone)及10 nM BOL-303242-X對GM-CSF產生顯著抑制作用。1 μM地塞米松對RANTES產生顯著抑制作用，而BOL-303242-X對此細胞素不產生顯著作用(圖3A至3C)。
就IL-6、IL-7、TGF-α、TNF-α、VGEF及MCP-1而言，BOL-303242及地塞米松對抑制HCEC中之IL-1β刺激產生細胞素具有類似效能。在抑制HCEC中之IL-1β刺激產生G-CSF之情況中，BOL-303242-X之效能高於地塞米松(dexamethasone)。在抑制HCEC中之IL-1β刺激產生GM-CSF、IL-8及RANTES之情況中，BOL-303242-X之效能稍低於地塞米松(dexamethasone)。
此研究之目的係評估當持續33天每日四次投與右眼時，局部BOL-303242-X對紐西蘭白兔之眼內壓(IOP)之作用。在31天後中斷投藥，因為存在高死亡率，且測試物供應有限。準則附加在附錄1。
三種測試物說明如下：
10 mg/g BOL-303242-X眼用懸浮液(批號2676-MLC-270)
5 mg/g BOL-303242-X眼用懸浮液(批號2676-MLC-270)
1 mg/g BOL-303242-X眼用懸浮液(批號2676-MLC-270)
亦提供負對照(平衡鹽溶液(BSS)，B.Braun Medical Inc.，批號J6N011，保存期限10/08)及正對照(0.1%地塞米松(dexamethasone)眼用懸浮液(Maxidex®,Alcon Laboratories,Inc.批號114619F，保存期限01/09))。調配物亦以現成形式提供，並保存在室溫下。在投藥前先振盪懸浮液，以使其等再懸浮。
自The Rabbit Source(Ramona,CA)獲得七十五隻雌性紐西蘭白兔。動物在IOP培養開始時為6至8週大，且體重隨機分佈在1.38至2.05 kg之間。準則指出動物體重應為至少1.5至2.5 kg；此偏差對研究結果不產生影響。動物係藉由耳朵標記及籠卡識別。
在運達後，檢查動物，以保證其等健康並檢疫10天，然後用於研究。在檢疫期結束時，再次檢查動物之基本健康參數及任何解剖學眼部異常。檢疫係依照國際操作方案進行。
將動物個別籠養在掛持式不鏽鋼籠中。籠養及清潔係依
照國際操作方案進行。
對動物餵與Teklad核准全球高纖維兔用膳食(Teklad Certified Global High Fiber Rabbit Diet)。膳食核准及分析係由獸醫Harlan Teklad提供。不實施製造商所提供以外的任何分析。動物可自由飲用充足自來水。水中不存在已知污染物且不實施本地水質規章所提供及國際操作方案所指出以外的額外分析。
依照國際操作方案監視環境參數。研究室溫為65至72℉，相對濕度58至77%。
在用於研究前，各動物接受處理前眼科檢查(裂隙燈及非直接檢眼鏡檢查)。依照McDonald Shadduck系統對觀察評分，及利用標準化數據收集表記錄。用於研究之接收標準如下：結膜充血及擴張得分1；所有其他觀察變量得分為0。
七十五隻兔子接受兩週IOP培養，以針對IOP測量進行調適。利用Medtronic Solan，機型30典型氣壓式眼壓計確定各隻動物兩眼之IOP。將丙美卡因(proparacaine)鹽酸鹽0.5%(1滴)滴入各眼睛，然後進行IOP測量。建立兩點式日曲線：在每週的週一、週三及週五，於8 a.m.及12 p.m.記錄IOP，此等時間各具有±1小時範圍。記錄測量時間。在兩週IOP調適期間，一隻兔死亡及兩隻兔因健康不良進行安樂死。
在兩週調適期結束時，基於各時間點之IOP測量之一致性
選擇50隻兔用於局部投藥。所選出之兔子繼續接受IOP測量達一週。
在投藥前，稱出50隻動物之重量及隨機分配至五個處理組中。處理組描述於表T3-1中。動物係依照修改之拉丁方格設計(Latin square)隨機分為處理組。
在第1至31天時，每日將適當測試物局部投與動物右眼。動物每日接受投與四次，每隔2小時投與一次劑量。利用經過校正之50-μL吸移管投藥。投藥後立即讓眼瞼閉合10秒。記錄各次劑量投與之時間。
準則指出動物每日接受投藥四次，持續33天。由試驗委託者及試驗主持人決定，在31天後停止投藥，因為存在高死亡率且測試物供應有限。此偏差不對研究結果產生負面作用。
每天兩次觀察動物之死亡率/致病率。藉由靜脈內注射市售安樂死藥物溶液對經確定致病之動物實施安樂死。
隨機稱出動物體重。
在第3、5、10、12、16、18、22、24、26、30及32天時確定動物兩眼之眼內壓(IOP)。藉由Medtronic Solan，機型30典型氣壓式眼壓計評估IOP。將丙美卡因(proparacaine)
鹽酸鹽0.5%(1滴)滴入各眼，然後進行IOP測量。在每週之週一、週三及週五測量IOP。建立兩點式日曲線：在第3天8 a.m.及12 p.m.及隨後幾天之8 a.m.及2 p.m.記錄IOP，此等時間各具有±1小時範圍。記錄測量之時間。
在第5、12、22、26及33天首次投藥之前實施眼科檢查(裂隙燈)。依照McDonald Shadduck系統對眼部現象評分及利用標準化數據收集表記錄。
在最後眼科觀察(第33天)完成之後，將餘下動物送回動物飼養所。
在各次測量間隔時製備各處理組IOP數據(分左及右眼)之描述性統計資料。統計資料包括觀察次數(N)、平均值、標準偏差(STD)及標準誤差(SEM)。利用統計學分析系統(SAS Institute,Inc.,Cary,NC,V8.0)對IOP結果進行統計學分析。利用變方差分析/GLM方案，接著Tukey標準化範圍測試(Tukey，1985)評估參數，以對組別平均值進行事後比較。對所有統計學方案之顯著水準設定p<0.05之機率。在各次間隔時，分別比較左及右眼之組IOP平均值。
將以下六類動物之IOP數據自組統計資料剔除：A組，編號3081、3037、3068及3011；C組，編號3034；及E組，編號3084。所剔除之A組動物對投與地塞米松(dexamethasone)沒有展現IOP反應，及所剔除之C組及E組
動物出現範圍外之IOP數據。
實施此研究以建立紐西蘭白兔之眼內壓之高血壓模型。曾探究實施此研究之替代方法；然而，為了合理建立該模型，需要全身測試系統。此研究遵循所有國際動物福利條例且由機構動物照顧及使用委員會(Institutional Animal Care and Use Committee)核准。
死亡率數據出示於表T3-2中。在第11天與第33天期間如下十隻動物死亡或接受安樂死：十隻接受投與地塞米松(dexamethasone)之兔中有六隻，十隻接受投與10 mg/g BOL-303242-X(0.5 mg/劑)之兔中有一隻，十隻接受投與5 mg/g BOL-303242-X(0.25 mg/劑)之兔中有兩隻，十隻接受投與1 mg/g BOL-303242-X(0.05 mg/劑)之兔中有一隻。發現七隻兔在死亡或安樂死前腹瀉，常描述為嚴重及出血。發現兩隻死亡之兔子並未觀察到健康不良跡象。觀察到之死亡率之進一步資訊顯示於下表中。
其餘兔子存活至研究完成(第33天)。有一隻接受10 mg/g BOL-303242-X(0.5 mg/劑)投藥之兔子於第18天出現腹瀉(B組，編號3048)。
裂隙燈眼科觀察結果出示於表T3-3中。對眼科觀察得分之解釋出示於表T3-4中。在大部分觀察中，眼睛表現正常。偶然發現輕微結膜充血(得分=1)，大部分在經處理之右眼中，測試或對照物無一致關聯性。僅有的其他現象係未處理左眼(A組，編號3086)中出現小面積角膜著色，在投與10 mg/g BOL-303242-X之右眼(B組，編號3083)中單點狀角膜瘢痕，及在投與1 mg/g BOL-303242-X之右眼(D組，編號3043)結膜下出血。所觀察到之角膜病灶可能與氣壓式眼壓計過程有關。
關於IOP之描述性統計資料出示於表T3-5(左眼，上午)、
表T3-6(右眼，下午)、表T3-7(左眼，下午)及表T3-8(右眼，下午)中。
在整個研究中，所有組之平均IOP不同；在各組內，左眼與右眼之偏差類似。就所有組而言(包括BSS投藥組)，在上午及下午讀取之左眼及右眼之平均IOP在第5至第10天之間達最大值。在研究期間，自上午至下午之IOP日變化不明顯，可能係因每日下午測量時先餵食兔後才進行。
就地塞米松(dexamethasone)組(A組)而言，左及右眼之平均IOP在開始處理之後急劇升高。在研究之任何點，BOL-303242-X組(B至D組)之平均IOP均未出現如此升高現象。在數天後，地塞米松(dexamethasone)組(A組)之單或雙眼平均IOP顯著高於(p<0.05)其他組中對應眼睛之平均IOP。此差異在上午時比在下午時更常見，且在未處理左眼中，其發生之時間點比經處理右眼多。在上午中，投與BSS之右眼(E組)之平均IOP基本上低於投與BOL-303242-X之右眼(B至D組)之平均IOP，但在下午時則不然。在BSS組與BOL-303242-X組之間平均IOP差異在統計上不顯著(p<0.05)。
此研究之目的係評估當每日四次投與右眼達33天時，局部BOL-303242-X對紐西蘭白兔之眼內壓(IOP)之作用。結論是，在兔眼中每日四次單側局部滴注BOL-303242-X懸浮液(0.05、0.25或0.5 mg/劑)、地塞米松(dexamethasone)懸浮液(0.05 mg/劑)或平衡鹽溶液達31天時，會導致偶發輕微結膜充血。投與地塞米松(dexamethasone)達31天(每10隻兔子有
6隻死亡)所導致死亡率高於投與BOL-303242-X達31天(在各投藥劑量下，每10隻兔子有1至2隻死亡)時。當與每日投與地塞米松(dexamethasone)比較時，每日投與BOL-303242-X懸浮液不會提高IOP。
表T3-4眼科觀察評分系統之解釋結膜充血1=主要局限在眼瞼結膜之滿布的微紅色，存在一些前虹膜充血，但主要局限於眼睛下及上部4：00至7：00及11：00至1：00位置。角膜1=損失一些透明度。僅涉及角膜基質之上皮及/或前半部。底層結構清晰可見但可輕易發現某些混濁。角膜患部表面1=1至25%之角膜基質面積混濁
此研究係雙盲、平行組、媒劑對照、分組序、劑量範圍研究，以確認BOL-303242-X眼用懸浮液對於治療白內障手術後之炎症及疼痛之最有效藥物濃度及投藥頻率。在此研究中存在8個處理組，由三種藥物劑量、媒劑及三種投藥頻率組成(亦參見表4-1)：
˙A組：1% BOL-303242-X眼用懸浮液，每日兩次(BID)
˙B組：2% BOL-303242-X眼用懸浮液，每日一次(QD)
˙C組：2% BOL-303242-X眼用懸浮液，BID
˙D組：2% BOL-303242-X眼用懸浮液，每日四次(QID)
˙E組：3% BOL-303242-X眼用懸浮液，QD
˙F組：3% BOL-303242-X眼用懸浮液，BID
˙G組：3% BOL-303242-X眼用懸浮液，QID
˙H組：BOL-303234-X之媒劑(平分為QID、BID及QD)
在就診3時(術後第1天，手術後之18至34小時)，將符合所有資格標準之個體隨機安排至處理組中之一者繼續接受研究，包括以1：1之比例安排至媒劑組。
個體自行投與研究藥物，將1至2滴研究藥物滴注至接受研究之眼睛中：以約4小時間隔QID，以約12小時間隔BID或早上一次QD，持續14天。首次投藥係在臨床就診3時進行及最後投藥係在就診6前一天(術後第15天±1天)。檢查個體及依照以下方案評估：就診1(篩選)，就診2(白內障手術)，就診3(術後第1天)，就診4(術後第3天±1天)，就診5(術後第8天±1天)，就診6(術後第15天±1天)，就診7(術後第18天±1天)。個體評估包括不良事件(AE)、合併用藥、眼部症狀、針孔斯耐倫(Snellen)
視敏度(VA)、眼內壓(IOP)、眼部症狀(活體組織檢視)、眼底鏡檢查及研究藥物液滴感受。此外，收集個體日誌及審查，以增強準確性及治療順服性。
在此研究之其他選納標準中，要求個體：˙在簽署知情同意表(ICF)當天年齡至少為18歲且具有自主同意之能力；˙接受研究之眼睛可接受例行無合併之白內障手術(藉由後房眼內水晶體(IOL)植入進行晶狀體乳化術，且不與任何其他手術組合)之候選者；˙在研究者選項中，接受研究之眼睛具有至少20/200之潛在術後針孔斯耐倫視敏度(VA)或0.1之針孔小數視敏度(Decimal VA)；˙接受研究之眼睛已接受例行無合併之白內障手術(藉由後房IOL植入進行晶狀體乳化術，不與任何其他手術組合)；及˙接受研究之眼睛具有等級2之前房(AC)細胞。
於此研究之其他選納標準中，要求個體：˙預期在整個研究期間需要藉由非類固醇消炎藥(NSAID)、肥大細胞穩定劑、抗組織胺藥或解充血劑進行同時眼部療法(任一眼睛)，或任一眼睛在手術前兩天內已使用以上藥物中之任一者；˙預期在整個研究期間需要藉由系統性NSAID進行治療，但排除81 mg/天之乙醯基水楊酸；˙預期在整個研究期間需要藉由免疫抑制劑(例如，麗眼
達(restasis))進行同時眼部療法或任一眼睛在手術前30天內已使用眼部免疫抑制劑；˙接受研究之眼睛在篩選就診前之3個月內或另一眼在2週內接受過眼部手術(包括雷射手術)；或˙具有升高之IOP(21 mm Hg)、未控制之青光眼，或在篩選時接受研究之眼睛正接受青光眼治療。
測試產品、劑量及投藥模式、批號：研究產品BOL-303242-X眼用懸浮液(1%、2%或3重量%)(批號：1%，C081102；2%，C090323；3%，C081104)係由德國柏林Bausch+Lomb GmbH，Brunsbuetteler Damm 165-173,13581 Berlin製造，且含有活性成分BOL-303242-X(1%，2%或3%重量/重量比)、防腐劑聚四級銨(Polyquaterium)-1及非活性物聚乙二醇、聚山梨醇酯80、硼酸、羥丙基甲基纖維素、甘油、二鹼價磷酸鈉、單鹼價磷酸鈉、EDTA、BHT、純水。個體自行投與研究藥物，依照以下隨機指派處理方法，將1至2滴研究藥物滴注至接受研究之眼睛：以約4小時間隔QID，以約12小時間隔BID或早上一次QD。
治療持續時間係14天。首次投藥係在臨床就診3(術後第1天)時進行，及最後投藥係在就診6(術後第15天±1天)前一天。
參考療法、劑量及投藥模式、批號：此研究中之比較物係BOL-303242-X之媒劑，由德國柏林
Bausch & Lomb GmbH，Brunsbuetteler Damm 165-173,13581 Berlin製造(批號C081101)。媒劑含有防腐劑聚四級銨-1及非活性物聚乙二醇、聚山梨醇酯80、硼酸、羥丙基甲基纖維素、甘油、二鹼價磷酸鈉、單鹼價磷酸鈉、EDTA、BHT、純水。
一級效能：此研究之一級效能終點係在就診5(術後第8天)時AC細胞完全消除之個體比例。AC細胞完全消除時定義為0級細胞。
二級效能：此研究之二級效能終點係在就診5(術後第8天)及在各次就診時具有0級疼痛、在各次就診時AC細胞完全消除、在各次就診時AC細胞及閃輝完全消除、在各次就診時AC閃輝完全消除、各次追蹤就診之組合及分開之AC細胞及AC閃輝離基線出現變化、具有眼部症狀之個體比例。
安全性：此研究之安全性終點為：AE發生、IOP變化、眼部跡象(活體組織檢視)、斯耐倫VA、眼底鏡檢查、研究藥物液滴感受評估。
對在就診5(術後第8天)時AC細胞完全消除之個體比例之一級效能終點分析證實，7隻研究藥物投與組中有6隻之AC細胞完全消除，此個體比例在統計學上顯著高於媒劑組：
˙對於超過效能邊界之所有三次投藥，2% QID(28.3%，p<0.001)、3% QD(25.4%，p=0.002)及3% QID(30.0%，p<0.001)組之AC細胞完全消除之個體比例在統計學上顯著高於媒劑組(5.0%)。3% QID組在就診5時，觀察到最大之AC細胞完全消除之個體比例。
對於不超過效能邊界之四次投藥，1% BID(21.7%，p=0.007)、2% QD(21.4%，p=0.018)及3% BID(25.0%，p=0.002)組之AC細胞完全消除之個體比例在統計學上顯著高於媒劑組。
˙利用完成計劃書療程(PP)人群進行之一級效能終點分析獲得類似結果。
對在就診5時0級疼痛之二級效能終點的分析證實，7隻研究藥物投與組中有4隻0級疼痛之個體比例在統計學上顯著高於媒劑組。觀察到以下投藥組0等疼痛之個體比例在統計學上顯著高於媒劑組：2% QID(78.3%，p=0.001)、3% QD(71.2%，p=0.018)、3% BID(75%，p=0.005)、3% QID(70.0%，p=0.025)。2% QID組在就診5時觀察到最大之0級疼痛之個體比例。
在就診5、6及7時，觀察到AC細胞完全消除之個體比例在統計學上顯著高於媒劑組：
˙就診5(術後第8天)：相較於媒劑組(5.0%)：2%
QID(28.3%，p<0.001)、3% QD(25.4%，p=0.002)、3% QID(30.0%，p<0.001)。對於以下不超過效能邊界之4個投藥組，其AC細胞完全消除之個體比例在統計學上顯著高於媒劑組：1% BID(21.7%，p=0.007)、2% QD(21.4%，p=0.018)及3% BID(25.0%，p=0.002)。
˙就診6(術後第15天)：2% QID(43.3%，p=0.003)、3% QD(47.5%，p<0.001)、3% BID(38.3%，p=0.015)、3% QID(38.3%，p=0.015)相對於媒劑組(18.3%)。
就診7(術後第18天)：1% BID(41.7%，p=0.010)、2% QID(53.3%，p<0.001)、3% QD(47.5%，p=0.002)、3% BID(43.3%，p=0.017)、3% QID(46.7%，p=0.002)相對於媒劑組(20.0%)。
在就診4、6及7時，觀察到0級疼痛之個體比例在統計學上顯著高於媒劑組：
˙就診4(術後第3天)：2% QID(73.3%，p=0.002)、3% QD(81.4%，p<o.001)、3% BID(70.0%，p=0.006)、3% QID(66.7%，p=0.017)相對於媒劑組(45.0%)。
˙就診6(術後第15天)：1% BID(61.7%,p<0.001)；2% QD(57.1%,p=0.023)；2% BID(57.1%,p=0.023)；2% QID(75.0%,p<0.001)；3% QD(71.2%,p<0.001)；3% BID(68.3%,p<0.001)；3% QID(70.0%,p<0.001)相對於媒劑組(31.7%)。
˙就診7(術後第18天)：1% BID(61.7%,p<0.001)；2% QD
(57.1%,p=0.023)；2% BID(53.6%,p=0.049)；2% QID(71.7%,p<0.001)；3% QD(66.1%,p<0.001)；3% BID(63.3%,p<0.001)；3% QID(58.3%,p<0.001)相對於媒劑組(31.7%)。
在就診4至7時觀察到AC閃輝完全消除之個體比例在統計學上顯著高於媒劑組：
˙就診4(術後第3天)：3% BID(38.3%,p=0.015)；3% QD(35.6%,p=0.034)相對於媒劑組(18.3%)。
˙就診5(術後第8天)：1% BID(41.7%,p=0.019)；2% QD(42.9%,p=0.040)；2% BID(50.0%,p=0.007)；2% QID(51.7%,p<0.001)；3% QD(55.9%,p<0.001)；3% BID(51.7%,p<0.001)；3% QID(55.0%,p<0.001)相對於媒劑組(21.7%)。
˙就診6(術後第15天)：1% BID(66.7%,p<0.001)；2% BID(60.7%,p=0.010)；2% QID(66.7%,p<0.001)；3% QD(66.1%,p<0.001)；3% BID(51.7%,p=0.026)；3% QID(61.7%,p<0.001)相對於媒劑組(31.7%)。
˙就診7(術後第18天)：1% BID(56.7%,p=0.003)；2% QID(66.7%,p<0.001)；3% QD(57.6%,p=0.002)；3% BID(56.7%,p=0.003)；3% QID(58.3%,p=0.002)相對於媒劑組(30.0%)。
在就診5、6及7時，觀察到AC細胞及閃輝之組合完全消
除之個體比例在統計學上顯著高於媒劑組：
˙就診5(術後第8天)：1% BID(20.0%,p=0.013)；2% QD(21.4%,p=0.018)；2% QID(26.7%,p=0.001)；3% QD(23.7%,p=0.004)；3% BID(23.3%,p=0.004)；3% QID(30.0%,p<0.001)相對於媒劑組(5.0%)。
就診6(術後第15天)：2% QD(35.7%,p=0.047)；2% QID(41.7%,p=0.003)；3% QD(47.5%,p<0.001)；3% BID(38.3%,p=0.008)；3% QID(36.7%,p=0.013)相對於媒劑組(16.7%)。
就診7(術後第18天)：1% BID(41.7%,p=0.010)；2% QID(53.3%,p<0.001)；3% QD(47.5%,p=0.002)；3% BID(43.3%,p=0.006)；3% QID(45.0%,p=0.003)相對於媒劑組(20.0%)。
相較於媒劑組，在以下術後就診時，觀察到數個投藥組之平均AC細胞從基線下降之平均值具有統計學上顯著性：
˙就診4：1% BID，2% QID，3% QD，3% QID。
˙就診5：1% BID，2% QD，2% QID，3% QD，3% BID，3% QID。
˙就診6：1% BID，2% BID，3% QD，3% BID，3% QID。
˙就診7：1% BID，2% QD，2% QID，3% QD，3% BID，3% QID。
在任何研究就診時，於任何投藥組與媒劑組之間，IOP自基線之變化平均值5 mmHg或10 mmHg之個體比例沒有統計學顯著差異。在就診4(術後第3天)至就診7(術後第18天)內，觀察到2% QID及3% QD組具有最低平均IOP值。
總體上，超過92%的個體之VA下降不超過兩條線或更少。
在任何術後就診時，在前玻璃體混濁、角膜水腫、角膜染色、眼瞼紅斑、眼前房出血及虹膜後黏連上均未觀察到任何投藥組之得分提高之個體比例存在統計學顯著差異。
在以下方面得分提高之個體比例在統計學上顯著較低：就診4(2% QD)及就診5(2% QID，3% QID)時之AC細胞；就診4(2% QID)及就診5(3% BID)時之AC閃輝；就診5(2% QID，3% BID，3% QID)時之球結膜充血；就診4(3% BID)時之球結膜水腫；就診4(2% QD)、就診5(1% BID，2% QID，3% BID，3% QID)及就診7(2% QID及3% QD)時之睫狀體部充血；就診5(1% BID，3% BID)時之眼瞼結膜充血。
結論是，此雙盲、平行組、媒劑對照、分組序、劑量範圍研究之結果證實，以下數種BOL-303242-X眼用懸浮液投藥劑量在就診5(術後第8天)時，對AC細胞及0級疼痛展現統計學上顯著之改善結果：2% QID、3% QD、3% BID及3% QID。QD投藥方案獲得最佳個體順服性且係未來研究之較佳方案。
將人類結膜纖維母細胞(HConF)接種在24孔盤之完全纖維母細胞培養基(FM)中，該培養基含有2%胎牛血清(FBS)及纖維母細胞生長補充物(FGS)。到達匯合(約95%)後，將細胞培養在已補充0.5%活性炭-葡聚糖處理之胎牛血清(CD-FBS)且不含纖維母細胞生長補充物(FGS)之基本FM中達24小時。藉由媒劑、IL-1β或IL-1β+6種劑量BOL-303242-X(3、10、30、100、300、1000 nM)處理細胞18小時。培養皿以一式三份進行。藉由ELISA評估培養基之PGE2釋放。結果顯示於圖6中。
藉由媒劑、馬拉克拉(mapracorat)或DEX預處理HConF達2小時，及隨後進一步藉由媒劑、IL-1β或IL-1β+馬拉克拉(mapracorat)或DEX-DMEM處理24小時。藉由冰冷PBS清洗細胞，並溶解在細胞溶解緩衝液(62.5 mM Tris-HCl，pH 6.8、2%十二烷基硫酸鈉(SDS)、10%甘油)中。以超音波處理細胞，及在12,000 rpm下離心及利用Micro BCA蛋白質檢測套組測定蛋白質濃度。藉由在10%凝膠上進行之SDS-聚丙烯醯胺電泳法分離細胞溶解樣液中之蛋白質(~20 μg蛋白質)並轉移至PVDF膜。藉由5% BSA封阻該等膜，及曝露於小鼠抗COX-2抗體(Caymen)。清洗點跡及曝露於辣根過氧化物酶-共軛抗小鼠二級抗體。清洗後，將點跡培養在ECL(增強化學發光)溶液，及利用FluorChem成像系統(AlphaInnotech,San Leandro,CA)檢視化學發光帶。隨後剝
離點跡，及再探測作為負載對照之甘油醛3-磷酸脫氫酶(GAPDH)(Zymed)抗體。重複該實驗3次。利用Alpha-Innotech Chemi-Imager軟體(Alpha Innotech；San Leandro,CA)分析擷取數位圖像中COX-2及GAPDH之西方點跡帶密度。將COX-2蛋白質濃度標準化為GAPDH。結果顯示在圖7中。
BOL-303242-X成功抑制IL-1β誘導HConF產生PGE2及COX-2，說明此化合物可減輕受影響患者之發炎性疼痛。
雖然本發明之具體實施例已描述於上文中，但熟習本項技術者將瞭解，可在不脫離附錄之專利申請範圍所界定之本發明精神及範圍下進行許多等效內容、修改、取代及變化。
圖1A至1F顯示BOL-303242-X及地塞米松(dexamethasone)對人類角膜上皮細胞(HCEC)中受IL-1β-刺激產生Il-6、IL-7、TGF-α、TNF-α、VGEF及MCP-1之影響，p<0.05。
圖2顯示BOL-303242-X及地塞米松對HCEC中受IL-1β-刺激產生G-CSF之影響，p<0.05。
圖3A至3C顯示BOL-303242-X及地塞米松對HCEC中受IL-1β-刺激產生GM至CSF、IL-8及RANTES之影響，p<0.05。
於上圖中，「＊」表示與對照組比較，及「＊＊」表示與IL-1β組比較。
圖4顯示在測試-4研究中得以解決疼痛之個體之百分比。
圖5顯示測試-4研究中之個體之平均IOP。
圖6顯示BOL-303242-X對人類結膜纖維母細胞(「HConF」)中IL-1β所誘導PGE2釋放之影響。＊P<0.05，相對於20 pg/ml IL-1β組。藉由雙向ANOVA-Tukey-Kramer試驗法分析數據，且以由泰勒(Taylor)級數展開式估算之幾何平均數±SE表示。
圖7顯示當藉由BOL-303242-X或地塞米松治療時對IL-β-所誘導HConF產生COX-2之抑制作用。
Claims (34)
- 一種組合物，其包含：(a)醫藥可接受載劑；及(b)有效量之治療、控制、減輕或改善個體發炎性疼痛之解離糖皮質激素受體促效劑(DIGRA)、其前藥、其醫藥可接受鹽或其醫藥可接受酯，其中該DIGRA包含具有式I之化合物
- 如請求項1之組合物，其中該組合物導致個體中之至少一 種不良副作用程度低於另一種包含至少糖皮質激素之組合物，其中該等組合物係用於治療、控制、減輕、改善或緩解相同病況。
- 如請求項2之組合物，其中該至少一種不良副作用之該程度係在體內測定。
- 如請求項2之組合物，其中該至少一糖皮質激素係選自由地塞米松(dexamethasone)、強的松(prednisone)、潑尼松龍(prednisolone)、甲強龍(methylprednisolone)、甲羥松(medrysone)、去炎松(triamcinolone)、去炎舒松(triamcinolone acetonide)、氟米龍(fluorometholone)、氯替潑諾碳酸乙酯(loteprednol etabonate)、其生理可接受鹽、其組合物及其混合物組成之群。
- 如請求項4之組合物，其中該至少一種不良副作用係選自由眼內壓升高、青光眼、白內障、高血壓、高血糖、高血脂及高膽固醇血症組成之群。
- 如請求項4之組合物，其中該至少一種不良副作用程度係在選自由該組合物首次投與且存在於個體後之約14天、約30天、約2個月、約3個月、約4個月、約5個月及約6個月組成之群之時間下確定。
- 如請求項5之組合物，其中該DIGRA具有式I
- 如請求項5之組合物，其中該DIGRA具有式I
- 如請求項2之組合物，其中該DIGRA具有式I
- 如請求項2之組合物，其中該DIGRA具有式II
- 如請求項2之組合物，其中該DIGRA具有式III
- 如請求項2之組合物，其中該DIGRA具有式IV
- 如請求項12之組合物，其進一步包含選自由非類固醇消炎藥(NSAID)、過氧化物酶體增殖劑活化受體(PPAR)配位體、抗組織胺藥、促炎細胞素拮抗劑、促炎細胞素抑制劑、氧化氮合成酶抑制劑、過氧化物酶抑制劑、其組合物及其混合物組成之群之額外治療劑。
- 如請求項12之組合物，其進一步包含NSAID。
- 如請求項12之組合物，其進一步包含氧化氮合成酶抑制劑。
- 如請求項12之組合物，其進一步包含過氧化物酶抑制劑。
- 一種組合物之用途，該組合物包含：(1)醫藥可接受載劑；及(2)DIGRA、其前藥、其醫藥可接受鹽或其醫藥可接受酯，其用於製造治療、控制、減輕或改善發炎性疼痛用之藥劑，其中該DIGRA具有式I
- 如請求項17之用途，其中該藥劑導致不良副作用程度低於針對相同病況使用糖皮質激素之方法。
- 如請求項17之用途，其中該藥劑導致IOP升高之程度低於使用糖皮質激素之方法。
- 如請求項18之用途，其中該藥劑進一步包含選自由非類固醇消炎藥(NSAID)、過氧化物酶體增殖劑活化受體(PPAR)配位體、抗組織胺藥、促炎細胞素拮抗劑、促炎細胞素抑制劑、氧化氮合成酶抑制劑、過氧化物酶抑制劑、其組合及其混合物組成之群之額外治療劑。
- 如請求項19之用途，其中該額外治療劑係選自由NSAID組成之群。
- 如請求項19之用途，其中該額外治療劑包含氧化氮合成 酶抑制劑。
- 如請求項19之用途，其中該額外治療劑包含過氧化物酶抑制劑。
- 如請求項18之用途，其中該DIGRA具有式II
- 如請求項18之用途，其中該DIGRA具有式III
- 如請求項18之用途，其中該DIGRA具有式IV
- 一種DIGRA、其前藥、其醫藥可接受鹽或其醫藥可接受酯之用途，其用於製造治療、控制、減輕或改善發炎性疼痛用之組合物；其中該DIGRA具有式I，
- 如請求項27之用途，其進一步包括與DIGRA、其前藥、其醫藥可接受鹽及其醫藥可接受酯不同之額外治療劑用於製造該組合物之用途。
- 一種製造治療、控制、減輕或改善發炎性疼痛用之組合物之方法，該方法包括：a)提供DIGRA、其前藥、其醫藥可接受鹽或其醫藥可接受酯；及b)將該DIGRA、其前藥、其醫藥可接受鹽或其醫藥可接受酯與醫藥可接受載劑組合，以製造該組合物；其中該DIGRA具有式I
- 如請求項29之方法，其中該DIGRA具有式I
- 如請求項29之方法，其中該DIGRA具有式I
- 如請求項29之方法，其中該DIGRA具有式II
- 如請求項29之方法，其中該DIGRA具有式III
- 如請求項29之方法，其中該DIGRA具有式IV
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| US201161494137P | 2011-06-07 | 2011-06-07 |
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| KR (1) | KR20140035481A (zh) |
| AR (1) | AR086686A1 (zh) |
| AU (1) | AU2012268692A1 (zh) |
| CA (1) | CA2838876A1 (zh) |
| MX (1) | MX2013014518A (zh) |
| TW (1) | TW201300378A (zh) |
| WO (1) | WO2012170175A1 (zh) |
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| GB201505527D0 (en) | 2015-03-31 | 2015-05-13 | Jmedtech Pte Ltd | Composition |
| JP2020536955A (ja) | 2017-10-06 | 2020-12-17 | ファウンドリー セラピューティクス， インコーポレイテッド | 治療剤の制御放出のための埋込み可能なデポー |
| US12364792B2 (en) | 2018-01-08 | 2025-07-22 | Foundry Therapeutics, Inc. | Devices, systems, and methods for treating intraluminal cancer via controlled delivery of therapeutic agents |
| US12458589B2 (en) | 2018-05-12 | 2025-11-04 | Foundry Therapeutics, Inc. | Implantable polymer depots for the controlled release of therapeutic agents |
| EP3843710A1 (en) | 2018-08-28 | 2021-07-07 | Foundry Therapeutics, Inc. | Polymer implants |
| KR20210119980A (ko) | 2019-01-22 | 2021-10-06 | 아크리베스 바이오메디컬 게엠베하 | 손상된 피부 상처를 치료하기 위한 선택적 글루코코르티코이드 수용체 개질제 |
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- 2012-05-17 MX MX2013014518A patent/MX2013014518A/es unknown
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- 2012-05-17 AU AU2012268692A patent/AU2012268692A1/en not_active Abandoned
- 2012-05-28 TW TW101119019A patent/TW201300378A/zh unknown
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| MX2013014518A (es) | 2014-01-31 |
| AR086686A1 (es) | 2014-01-15 |
| KR20140035481A (ko) | 2014-03-21 |
| AU2012268692A1 (en) | 2014-01-16 |
| WO2012170175A1 (en) | 2012-12-13 |
| CA2838876A1 (en) | 2012-12-13 |
| US20120316199A1 (en) | 2012-12-13 |
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