PE20080348A1 - Moduladores tiazolopirimidina de trpv1 - Google Patents
Moduladores tiazolopirimidina de trpv1Info
- Publication number
- PE20080348A1 PE20080348A1 PE2007000838A PE2007000838A PE20080348A1 PE 20080348 A1 PE20080348 A1 PE 20080348A1 PE 2007000838 A PE2007000838 A PE 2007000838A PE 2007000838 A PE2007000838 A PE 2007000838A PE 20080348 A1 PE20080348 A1 PE 20080348A1
- Authority
- PE
- Peru
- Prior art keywords
- phenyl
- alkyl
- pyrimidin
- diamine
- trifluoromethyl
- Prior art date
Links
- 102000003566 TRPV1 Human genes 0.000 title abstract 2
- 101150016206 Trpv1 gene Proteins 0.000 title abstract 2
- 150000008634 thiazolopyrimidines Chemical class 0.000 title 1
- -1 THIAZOLOPYRIMIDINE COMPOUND Chemical class 0.000 abstract 4
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical class [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- SLRMQYXOBQWXCR-UHFFFAOYSA-N 2154-56-5 Chemical class [CH2]C1=CC=CC=C1 SLRMQYXOBQWXCR-UHFFFAOYSA-N 0.000 abstract 1
- 208000002193 Pain Diseases 0.000 abstract 1
- 208000003251 Pruritus Diseases 0.000 abstract 1
- 230000002757 inflammatory effect Effects 0.000 abstract 1
- 230000007803 itching Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 210000000929 nociceptor Anatomy 0.000 abstract 1
- 108091008700 nociceptors Proteins 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/04—Antipruritics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pain & Pain Management (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Biomedical Technology (AREA)
- Dermatology (AREA)
- Urology & Nephrology (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
SE REFIERE A UN COMPUESTO DE TIAZOLOPIRIMIDINA DE FORMULA I DONDE R1 ES H, ALQUILO C1-C6, O-(ALQUILO C1-C6), S-(ALQUILO C1-C6), ENTRE OTROS; R2 ES H, ALQUILO C1-C6; R3 ES CICLOALQUILO MONOCICLICO, FENILO, BENCILO, INDANILO, ENTRE OTROS; R4 ES H, ALQUILO C1-C6; R5 ES FENILO, HETEROARILO MONOCICLICO DE 5 MIEMBROS O HETEROARILO MONOCICLICO DE 6 MIEMBROS SUSTITUIDO O NO. SON COMPUESTOS PREFERIDOS: N2-(2,6-DICLORO-FENIL)-N7-(4-TRIFLUOROMETIL-FENIL)-TIAZOLO[5,4-d]PIRIMIDIN-2,7-DIAMINA; N2-o-TOLIL-N7-(4-TRIFLUOROMETIL-FENIL)-TIAZOLO[5,4-d]PIRIMIDIN-2,7-DIAMINA; 5-METIL-N2-(5-METIL-3-FENIL-ISOXAZOL-4-IL)-N7-(6-TRIFLUOROMETIL-PIRIDIN-3-IL)-TIAZOLO[5,4-d]PIRIMIDIN-2,7-DIAMINA; ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO DE PREPARACION Y UNA COMPOSICION FARMACEUTICA. DICHO COMPUESTO ES UN MODULADOR DE TRPV1 LIGADA A NOCICEPTORES Y ES UTIL EN EL TRATAMIENTO DEL DOLOR, PRURITO, TOS Y OTROS ESTADOS INFLAMATORIOS
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US81815306P | 2006-06-30 | 2006-06-30 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20080348A1 true PE20080348A1 (es) | 2008-04-25 |
Family
ID=38740251
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2007000838A PE20080348A1 (es) | 2006-06-30 | 2007-07-02 | Moduladores tiazolopirimidina de trpv1 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US20080004253A1 (es) |
| EP (1) | EP2044086A2 (es) |
| AR (1) | AR061761A1 (es) |
| CL (1) | CL2007001921A1 (es) |
| PE (1) | PE20080348A1 (es) |
| TW (1) | TW200821320A (es) |
| UY (1) | UY30454A1 (es) |
| WO (1) | WO2008005303A2 (es) |
Families Citing this family (47)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009073153A2 (en) * | 2007-11-28 | 2009-06-11 | Dana Farber Cancer Institute | Small molecule myristate inhibitors of bcr-abl and methods of use |
| CL2008003749A1 (es) | 2007-12-17 | 2010-01-15 | Janssen Pharmaceutica Nv | Compuestos derivados de imidazol, oxazol, y tiazol pirimidina, moduladores de trpv1, proceso de preparacion, composicion farmaceutica y su uso en el tratamiento de enfermedades, trastornos o condicion de dolor, prurito, artritis, tos, asma, trastorno del oido interno y enfermedad inflamatoria intestinal, entre otras. |
| US20090156598A1 (en) * | 2007-12-17 | 2009-06-18 | Lebsack Alec D | Imidazolopyrimidine modulators of TRPV1 |
| RU2522430C2 (ru) * | 2008-01-22 | 2014-07-10 | ДАУ АГРОСАЙЕНСИЗ ЭлЭлСи | 5-фторпиримидиновые производные в качестве фунгицидов |
| WO2010093704A1 (en) * | 2009-02-10 | 2010-08-19 | Abbott Laboratories | Agonists and antagonists of the s1p5 receptor, and methods of uses thereof |
| JP5647998B2 (ja) * | 2009-03-13 | 2015-01-07 | カトリーケ ユニバーシテイト ルーヴェン、ケー.ユー. ルーヴェン アール アンド ディー | 免疫抑制剤としてのチアゾロピリミジン調節因子 |
| CN104945420A (zh) | 2009-06-29 | 2015-09-30 | 因塞特公司 | 作为pi3k抑制剂的嘧啶酮类 |
| UA112284C2 (uk) * | 2009-08-07 | 2016-08-25 | ДАУ АГРОСАЙЄНСІЗ ЕлЕлСі | Похідні 5-фторпіримідинону |
| UA107671C2 (en) | 2009-08-07 | 2015-02-10 | Dow Agrosciences Llc | N1-substityted-5-fluoro-2-oxopyrimidinone-1(2h)-carboxamide derivatives |
| PE20120691A1 (es) * | 2009-08-07 | 2012-06-08 | Dow Agrosciences Llc | Derivados de n1-sulfonil-5-fluoropirimidinona |
| UA106889C2 (uk) * | 2009-08-07 | 2014-10-27 | ДАУ АГРОСАЙЄНСІЗ ЕлЕлСі | Похідні n1-ацил-5-фторпіримідинону |
| US8759359B2 (en) | 2009-12-18 | 2014-06-24 | Incyte Corporation | Substituted heteroaryl fused derivatives as PI3K inhibitors |
| KR101814835B1 (ko) | 2010-01-07 | 2018-01-04 | 다우 아그로사이언시즈 엘엘씨 | 티아졸로[5,4-d]피리미딘 및 그의 농약으로서의 용도 |
| WO2011130342A1 (en) | 2010-04-14 | 2011-10-20 | Incyte Corporation | FUSED DERIVATIVES AS ΡI3Κδ INHIBITORS |
| GB201012889D0 (en) | 2010-08-02 | 2010-09-15 | Univ Leuven Kath | Antiviral activity of novel bicyclic heterocycles |
| US9062055B2 (en) | 2010-06-21 | 2015-06-23 | Incyte Corporation | Fused pyrrole derivatives as PI3K inhibitors |
| GB201015411D0 (en) | 2010-09-15 | 2010-10-27 | Univ Leuven Kath | Anti-cancer activity of novel bicyclic heterocycles |
| CA2822070C (en) | 2010-12-20 | 2019-09-17 | Incyte Corporation | N-(1-(substituted-phenyl)ethyl)-9h-purin-6-amines as pi3k inhibitors |
| US9108984B2 (en) | 2011-03-14 | 2015-08-18 | Incyte Corporation | Substituted diamino-pyrimidine and diamino-pyridine derivatives as PI3K inhibitors |
| US9126948B2 (en) | 2011-03-25 | 2015-09-08 | Incyte Holdings Corporation | Pyrimidine-4,6-diamine derivatives as PI3K inhibitors |
| CN103946226A (zh) | 2011-07-19 | 2014-07-23 | 无限药品股份有限公司 | 杂环化合物及其应用 |
| US8658660B2 (en) | 2011-08-17 | 2014-02-25 | Dow Agrosciences, Llc. | 5-fluoro-4-imino-3,4-dihydropyrimidin-2-(1H)-ones derivatives |
| AR087760A1 (es) | 2011-09-02 | 2014-04-16 | Incyte Corp | Heterociclilaminas como inhibidores de pi3k |
| AR090548A1 (es) | 2012-04-02 | 2014-11-19 | Incyte Corp | Azaheterociclobencilaminas biciclicas como inhibidores de pi3k |
| US8940742B2 (en) | 2012-04-10 | 2015-01-27 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| EP2938194B1 (en) | 2012-12-28 | 2019-11-27 | Adama Makhteshim Ltd. | N-(substituted)-5-fluoro-4-imino-3-methyl-2-oxo-3,4-dihydropyrimidine-1 (2h)-carboxylate derivatives |
| US9321734B2 (en) | 2012-12-28 | 2016-04-26 | Dow Agrosciences Llc | N-(substituted)-5-fluoro-4-imino-3-methyl-2-oxo-3,4-dihydropyrimidine-1(2H)-carboxamide derivatives |
| CN104994859B (zh) | 2012-12-28 | 2018-10-26 | 阿达玛马克西姆股份有限公司 | 1-(取代的苯甲酰基)-5-氟-4-亚氨基-3-甲基-3,4-二氢嘧啶-2(1h)-酮衍生物 |
| RU2644014C2 (ru) | 2012-12-31 | 2018-02-07 | Адама Мактешим Лтд. | Производные 3-алкил-5-фтор-4-замещенного-имино-3,4-дигидропиримидин-2(н)-она в качестве фунгицидов |
| RU2016110852A (ru) * | 2013-09-27 | 2017-10-30 | Нимбус Айрис, Инк. | Ингибиторы irak и их применения |
| WO2015051241A1 (en) | 2013-10-04 | 2015-04-09 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| HUE057734T2 (hu) | 2013-10-04 | 2022-06-28 | Infinity Pharmaceuticals Inc | Heterociklusos vegyületek és alkalmazásuk |
| CN103694243B (zh) * | 2013-12-20 | 2015-09-09 | 中国农业大学 | 2-取代吡啶基-1,2,4-三唑并[1,2-a]哒嗪化合物 |
| WO2015103261A1 (en) | 2013-12-31 | 2015-07-09 | Dow Agrosciences Llc | Synergistic fungicidal mixtures for fungal control in cereals |
| UA122200C2 (uk) | 2013-12-31 | 2020-10-12 | Адама Махтешім Лтд. | 5-фтор-4-іміно-3-(алкіл/заміщений алкіл)-1-(арилсульфоніл)-3,4-дигідропіримідин-2(1h)-он і способи його одержання |
| CN113616656B (zh) | 2014-03-19 | 2023-02-17 | 无限药品股份有限公司 | 用于治疗PI3K-γ介导的障碍的杂环化合物 |
| US10077277B2 (en) | 2014-06-11 | 2018-09-18 | Incyte Corporation | Bicyclic heteroarylaminoalkyl phenyl derivatives as PI3K inhibitors |
| WO2016054491A1 (en) | 2014-10-03 | 2016-04-07 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| PT3831833T (pt) | 2015-02-27 | 2023-02-06 | Incyte Corp | Processos para a preparação de um inibidor pi3k |
| WO2016183060A1 (en) | 2015-05-11 | 2016-11-17 | Incyte Corporation | Process for the synthesis of a phosphoinositide 3-kinase inhibitor |
| US9988401B2 (en) | 2015-05-11 | 2018-06-05 | Incyte Corporation | Crystalline forms of a PI3K inhibitor |
| EP3350183B1 (en) | 2015-09-14 | 2025-04-02 | Twelve Therapeutics, Inc. | Solid forms of isoquinolinone derivatives, process of making, compositions comprising, and methods of using the same |
| WO2017161116A1 (en) | 2016-03-17 | 2017-09-21 | Infinity Pharmaceuticals, Inc. | Isotopologues of isoquinolinone and quinazolinone compounds and uses thereof as pi3k kinase inhibitors |
| WO2017214269A1 (en) | 2016-06-08 | 2017-12-14 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| EP3655396A1 (en) | 2017-07-17 | 2020-05-27 | Adama Makhteshim Ltd. | Polymorphs of 5-fluoro-4-imino-3-methyl-1-tosyl-3,4-dihydropyrimidin-2-one |
| KR102884803B1 (ko) | 2018-06-01 | 2025-11-12 | 인사이트 코포레이션 | Pi3k 관련 장애의 치료를 위한 투여 요법 |
| CN111187181B (zh) * | 2019-11-22 | 2023-05-05 | 吉林大学 | 一种2-(4-氨基苯基)-2-甲基丙腈化合物的制备方法 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6107300A (en) * | 1996-03-27 | 2000-08-22 | Dupont Pharmaceuticals | Arylamino fused pyrimidines |
| US6232320B1 (en) * | 1998-06-04 | 2001-05-15 | Abbott Laboratories | Cell adhesion-inhibiting antiinflammatory compounds |
| ATE419239T1 (de) * | 2000-10-20 | 2009-01-15 | Eisai R&D Man Co Ltd | Verfahren zur herstellung von 4-phenoxy chinolin derivaten |
| AU2004212490B2 (en) * | 2003-02-10 | 2008-05-15 | Amgen Inc. | Vanilloid receptor ligands and their use in treatments |
| KR20060118398A (ko) * | 2003-08-05 | 2006-11-23 | 버텍스 파마슈티칼스 인코포레이티드 | 전압 개폐 이온 채널 억제제로서의 축합 피라미딘 화합물 |
| EP1678173A2 (en) * | 2003-09-09 | 2006-07-12 | Neurogen Corporation | 4-heterobicyclylamino-substituted quinazolines and analogues thereof as capsaicin-antagonists |
| EP1670794A2 (en) * | 2003-09-30 | 2006-06-21 | Amgen Inc. | Vanilloid receptor ligands and their use in treatments |
| JP2007507494A (ja) * | 2003-10-07 | 2007-03-29 | アストラゼネカ・アクチエボラーグ | ケモカイン受容体アンタゴニストとりわけCX3CR1として有用な新規な2−置換4−アミノ−チアゾロ[4,5−d]ピリミジン |
| AU2006278627B2 (en) * | 2005-08-08 | 2011-08-18 | Janssen Pharmaceutica, N.V. | Thiazolopyrimidine kinase inhibitors |
-
2007
- 2007-06-28 WO PCT/US2007/015079 patent/WO2008005303A2/en not_active Ceased
- 2007-06-28 US US11/824,202 patent/US20080004253A1/en not_active Abandoned
- 2007-06-28 EP EP07810020A patent/EP2044086A2/en not_active Withdrawn
- 2007-06-29 TW TW096123615A patent/TW200821320A/zh unknown
- 2007-06-29 CL CL200701921A patent/CL2007001921A1/es unknown
- 2007-06-29 AR ARP070102936A patent/AR061761A1/es unknown
- 2007-07-02 UY UY30454A patent/UY30454A1/es unknown
- 2007-07-02 PE PE2007000838A patent/PE20080348A1/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| EP2044086A2 (en) | 2009-04-08 |
| AR061761A1 (es) | 2008-09-17 |
| US20080004253A1 (en) | 2008-01-03 |
| CL2007001921A1 (es) | 2008-03-14 |
| UY30454A1 (es) | 2008-01-31 |
| TW200821320A (en) | 2008-05-16 |
| WO2008005303A3 (en) | 2008-04-10 |
| WO2008005303A2 (en) | 2008-01-10 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FX | Voluntary withdrawal |