PE20180552A1 - Nuevos compuestos biciclicos como inhibidores duales de atx/ca - Google Patents
Nuevos compuestos biciclicos como inhibidores duales de atx/caInfo
- Publication number
- PE20180552A1 PE20180552A1 PE2018000079A PE2018000079A PE20180552A1 PE 20180552 A1 PE20180552 A1 PE 20180552A1 PE 2018000079 A PE2018000079 A PE 2018000079A PE 2018000079 A PE2018000079 A PE 2018000079A PE 20180552 A1 PE20180552 A1 PE 20180552A1
- Authority
- PE
- Peru
- Prior art keywords
- inhibitors
- compounds
- substituted phenyl
- substituted
- atx
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 230000009977 dual effect Effects 0.000 title 1
- WRGQSWVCFNIUNZ-GDCKJWNLSA-N 1-oleoyl-sn-glycerol 3-phosphate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OC[C@@H](O)COP(O)(O)=O WRGQSWVCFNIUNZ-GDCKJWNLSA-N 0.000 abstract 3
- AWUCVROLDVIAJX-UHFFFAOYSA-N alpha-glycerophosphate Natural products OCC(O)COP(O)(O)=O AWUCVROLDVIAJX-UHFFFAOYSA-N 0.000 abstract 3
- 102100021977 Ectonucleotide pyrophosphatase/phosphodiesterase family member 2 Human genes 0.000 abstract 2
- 108050004000 Ectonucleotide pyrophosphatase/phosphodiesterase family member 2 Proteins 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 102000003846 Carbonic anhydrases Human genes 0.000 abstract 1
- 108090000209 Carbonic anhydrases Proteins 0.000 abstract 1
- 230000002757 inflammatory effect Effects 0.000 abstract 1
- 210000000653 nervous system Anatomy 0.000 abstract 1
- 150000002894 organic compounds Chemical class 0.000 abstract 1
- 230000001575 pathological effect Effects 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 230000011664 signaling Effects 0.000 abstract 1
- 125000001544 thienyl group Chemical group 0.000 abstract 1
- 230000002792 vascular Effects 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
- A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
- A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Ophthalmology & Optometry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Referido a compuestos de la formula (I), en donde R1 fenilo sustituido, fenil-alquilo C1-6 sustituido, entre otros; R2 es fenilo sustituido, piridinilo sustituido o tiofenilo sustituido, entre otros; Y es un -OC(O)- o -C(O)-; W es -C(O)-, -S(O)2- o -CR6R7-; m, n, p y q se eligen con independencia entre 1 y 2. Estos son compuestos organicos inhibidores daules de la autotaxina (ATX)/ la anhidrasa carbonica, que son inhibidores de la produccion de acido lisofosfatidico (LPA), por ello moduladores de los niveles de LPA y de la senalizacion asociada. Siendo util en el tratamiento de estados patologicos inflamatorios, del sistema nervioso, vasculares entre otros.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP15186633 | 2015-09-24 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20180552A1 true PE20180552A1 (es) | 2018-04-02 |
Family
ID=54199035
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2018000079A PE20180552A1 (es) | 2015-09-24 | 2016-09-21 | Nuevos compuestos biciclicos como inhibidores duales de atx/ca |
Country Status (20)
| Country | Link |
|---|---|
| US (2) | US10647719B2 (es) |
| EP (1) | EP3353178B1 (es) |
| JP (1) | JP6877413B2 (es) |
| KR (1) | KR20180054634A (es) |
| CN (1) | CN107922415B (es) |
| AR (1) | AR106099A1 (es) |
| AU (1) | AU2016328436B2 (es) |
| BR (1) | BR112018006080A2 (es) |
| CA (1) | CA2991612A1 (es) |
| CL (1) | CL2018000685A1 (es) |
| CO (1) | CO2018000668A2 (es) |
| CR (1) | CR20180057A (es) |
| IL (1) | IL256724A (es) |
| MA (1) | MA42923A (es) |
| MX (1) | MX372962B (es) |
| PE (1) | PE20180552A1 (es) |
| RU (1) | RU2724899C2 (es) |
| TW (1) | TW201720823A (es) |
| WO (1) | WO2017050791A1 (es) |
| ZA (1) | ZA201800480B (es) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2618703T3 (es) | 2012-06-13 | 2017-06-22 | F. Hoffmann-La Roche Ag | Nuevos compuestos diazaspirocicloalcano y azaspirocicloalcano |
| CN104684915B (zh) | 2012-09-25 | 2017-10-31 | 霍夫曼-拉罗奇有限公司 | 新型双环衍生物 |
| AR095079A1 (es) | 2013-03-12 | 2015-09-16 | Hoffmann La Roche | Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo |
| KR20160087900A (ko) | 2013-11-26 | 2016-07-22 | 에프. 호프만-라 로슈 아게 | 신규한 옥타하이드로-사이클로부타[1,2-c;3,4-c'']다이피롤-2-일 |
| AU2015238537B2 (en) | 2014-03-26 | 2019-08-01 | F. Hoffmann-La Roche Ag | Bicyclic compounds as autotaxin (ATX) and lysophosphatidic acid (LPA) production inhibitors |
| CN106029667B (zh) | 2014-03-26 | 2019-08-23 | 豪夫迈·罗氏有限公司 | 作为自分泌运动因子(atx)和溶血磷脂酸(lpa)生产抑制剂的稠合[1,4]二氮杂*化合物 |
| MA41898A (fr) | 2015-04-10 | 2018-02-13 | Hoffmann La Roche | Dérivés de quinazolinone bicyclique |
| EP3344619B1 (en) | 2015-09-04 | 2020-10-28 | H. Hoffnabb-La Roche Ag | Phenoxymethyl derivatives |
| CN115124538A (zh) | 2015-09-24 | 2022-09-30 | 豪夫迈·罗氏有限公司 | 作为atx抑制剂的二环化合物 |
| KR20180054635A (ko) * | 2015-09-24 | 2018-05-24 | 에프. 호프만-라 로슈 아게 | 오토탁신(atx) 억제제로서 이환형 화합물 |
| RU2725138C2 (ru) | 2015-09-24 | 2020-06-30 | Ф. Хоффманн-Ля Рош Аг | Новые бициклические соединения в качестве двойных ингибиторов аутотаксина (atx)/карбоангидразы (ca) |
| KR20180054634A (ko) | 2015-09-24 | 2018-05-24 | 에프. 호프만-라 로슈 아게 | 이중 오토탁신(atx)/탄산 무수화효소(ca) 억제제로서 신규한 이환형 화합물 |
| JP7090099B2 (ja) * | 2017-03-16 | 2022-06-23 | エフ.ホフマン-ラ ロシュ アーゲー | Atxインヒビターとしての新規二環式化合物 |
| JP7157755B2 (ja) | 2017-03-16 | 2022-10-20 | エフ.ホフマン-ラ ロシュ アーゲー | 二重atx/ca阻害剤として有用な複素環式化合物 |
| AR111295A1 (es) | 2017-03-20 | 2019-06-26 | Forma Therapeutics Inc | Composiciones de pirrolopirrol como activadores de piruvato quinasa (pkr) |
| US20200129485A1 (en) | 2018-09-19 | 2020-04-30 | Forma Therapeutics, Inc. | Treating sickle cell disease with a pyruvate kinase r activating compound |
| WO2020061255A1 (en) * | 2018-09-19 | 2020-03-26 | Forma Therapeutics, Inc. | Activating pyruvate kinase r |
| EP3852792A4 (en) * | 2018-09-19 | 2022-07-06 | Forma Therapeutics, Inc. | INHIBITION OF UBIQUITIN-SPECIFIC PEPTIDASE 9X |
| CA3113423A1 (en) * | 2018-09-19 | 2020-03-26 | Forma Therapeutics, Inc. | Inhibiting ubiquitin specific peptidase 9x |
| WO2020191022A1 (en) * | 2019-03-18 | 2020-09-24 | Forma Therapeutics, Inc. | Inhibiting ubiquitin specific peptidase 9x |
| RS67259B1 (sr) | 2019-09-19 | 2025-10-31 | Novo Nordisk Healthcare Ag | Kompozicije koje aktiviraju piruvat kinazu r (pkr) |
| CN116806150A (zh) | 2021-01-05 | 2023-09-26 | 载度思生命科学有限公司 | 新的自分泌运动因子抑制剂 |
| US12128035B2 (en) | 2021-03-19 | 2024-10-29 | Novo Nordisk Health Care Ag | Activating pyruvate kinase R |
| CN120225503A (zh) | 2022-11-21 | 2025-06-27 | 诺和诺德医疗保健公司 | 吡咯并[3,4-c]吡咯的合成 |
Family Cites Families (131)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE1252898B (de) | 1965-06-12 | 1967-10-26 | Bayer Ag | Verfahren zur Herstellung von Copolymerisaten des Trioxans |
| US5240928A (en) | 1989-07-03 | 1993-08-31 | Merck & Co., Inc. | Substituted quinazolinones as angiotensin II antagonists |
| DE3930262A1 (de) | 1989-09-11 | 1991-03-21 | Thomae Gmbh Dr K | Kondensierte diazepinone, verfahren zu ihrer herstellung und diese verbindungen enthaltende arzneimittel |
| KR910009330B1 (ko) * | 1989-10-23 | 1991-11-11 | 재단법인 한국화학연구소 | 항균작용을 갖는 퀴놀린계 화합물과 그의 제조방법 |
| CA2037630C (en) | 1990-03-07 | 2001-07-03 | Akira Morimoto | Nitrogen-containing heterocylic compounds, their production and use |
| US5470975A (en) | 1990-10-16 | 1995-11-28 | E.R. Squibb & Sons, Inc. | Dihydropyrimidine derivatives |
| US5290780A (en) | 1991-01-30 | 1994-03-01 | American Cyanamid Co. | Angiotensin II receptor blocking 2,3,6 substituted quinazolinones |
| US5238942A (en) | 1991-05-10 | 1993-08-24 | Merck & Co., Inc. | Substituted quinazolinones bearing acidic functional groups as angiotensin ii antagonists |
| DE4121214A1 (de) * | 1991-06-27 | 1993-01-14 | Bayer Ag | 7-azaisoindolinyl-chinolon- und -naphthyridoncarbonsaeure-derivate |
| US5202322A (en) | 1991-09-25 | 1993-04-13 | Merck & Co., Inc. | Quinazolinone and pyridopyrimidine a-II antagonists |
| US5532243A (en) | 1992-02-14 | 1996-07-02 | The Dupont Merck Pharmaceutical Company | Antipsychotic nitrogen-containing bicyclic compounds |
| US5358951A (en) | 1993-04-23 | 1994-10-25 | American Cyanamid Company | Angiotensin II receptor blocking 2, 3, 6 substituted quinazolinones |
| DE4407047A1 (de) | 1994-03-03 | 1995-09-07 | Merck Patent Gmbh | Acetamide |
| US20010016657A1 (en) | 1997-03-18 | 2001-08-23 | Smithkline Beecham P.L.C. | Substituted isoquinoline derivatives and their use as anticonvulsants |
| WO1999040070A1 (en) | 1998-02-04 | 1999-08-12 | Banyu Pharmaceutical Co., Ltd. | N-acyl cyclic amine derivatives |
| JP2001039950A (ja) | 1999-07-30 | 2001-02-13 | Banyu Pharmaceut Co Ltd | N−アシル環状アミン誘導体 |
| JP2003514777A (ja) | 1999-10-27 | 2003-04-22 | シーオーアール セラピューティクス インコーポレイテッド | フィブリノゲン依存性血小板凝集の阻害剤としてのピリジル含有スピロ環化合物 |
| MXPA03008109A (es) | 2001-03-07 | 2003-12-12 | Pfizer Prod Inc | Moduladores de la actividad de receptores de quimiocinas. |
| JP4459629B2 (ja) | 2002-04-12 | 2010-04-28 | メルク エンド カムパニー インコーポレーテッド | 二環式アミド |
| GB0303852D0 (en) | 2003-02-19 | 2003-03-26 | Pfizer Ltd | Triazole compounds useful in therapy |
| WO2005023762A1 (en) | 2003-09-04 | 2005-03-17 | Abbott Laboratories | Pyrrolidine-2-carbonitrile derivatives and their use as inhibitors of dipeptidyl peptidase-iv (dpp-iv) |
| SE0302811D0 (sv) | 2003-10-23 | 2003-10-23 | Astrazeneca Ab | Novel compounds |
| GB0324790D0 (en) | 2003-10-24 | 2003-11-26 | Astrazeneca Ab | Amide derivatives |
| US7226951B2 (en) | 2003-12-17 | 2007-06-05 | Allergan, Inc. | Compounds having selective cytochrome P450RAI-1 or selective cytochrome P450RAI-2 inhibitory activity and methods of obtaining the same |
| EP1720545B1 (en) | 2004-03-03 | 2014-10-29 | ChemoCentryx, Inc. | Bicyclic and bridged nitrogen heterocycles |
| PL1761542T3 (pl) | 2004-06-09 | 2008-06-30 | Hoffmann La Roche | Pochodne oktahydropirolo[3,4-c]pirolu i ich zastosowanie jako środków przeciwwirusowych |
| AU2005271161B2 (en) | 2004-08-10 | 2011-05-12 | Janssen Pharmaceutica N.V. | HIV inhibiting 1,2,4-triazin-6-one derivatives |
| US7410949B2 (en) | 2005-01-18 | 2008-08-12 | Hoffmann-La Roche Inc. | Neuropeptide-2 receptor (Y-2R) agonists and uses thereof |
| BRPI0610433A2 (pt) | 2005-04-28 | 2010-11-23 | Wyeth Corp | forma polimórfica ii de tanaproget, processos para preparar a mesma, e para preparar forma micronizada de um composto, composição farmacêutica, método de preparação de uma composição farmacêutica, e, uso da forma polimórfica ii de tanaproget ou da forma micronizada |
| US7737279B2 (en) | 2005-05-10 | 2010-06-15 | Bristol-Myers Squibb Company | 1,6-dihydro-1,3,5,6-tetraaza-as-indacene based tricyclic compounds and pharmaceutical compositions comprising same |
| TW200800999A (en) | 2005-09-06 | 2008-01-01 | Astrazeneca Ab | Novel compounds |
| ES2427989T3 (es) | 2005-10-28 | 2013-11-05 | Ono Pharmaceutical Co., Ltd. | Compuesto que contiene un grupo básico y uso del mismo |
| ES2407115T3 (es) | 2005-11-18 | 2013-06-11 | Ono Pharmaceutical Co., Ltd. | Compuesto que contiene un grupo básico y uso del mismo |
| US20070208001A1 (en) | 2006-03-03 | 2007-09-06 | Jincong Zhuo | Modulators of 11- beta hydroxyl steroid dehydrogenase type 1, pharmaceutical compositions thereof, and methods of using the same |
| JP2008031064A (ja) | 2006-07-27 | 2008-02-14 | Astellas Pharma Inc | ジアシルピペラジン誘導体 |
| ATE523500T1 (de) | 2006-09-11 | 2011-09-15 | Organon Nv | Chinazolinon- und isochinolinon-acetamid-derivate |
| JP2010503675A (ja) | 2006-09-15 | 2010-02-04 | シェーリング コーポレイション | 疼痛、糖尿病および脂質代謝の障害の治療に有用なスピロ縮合アゼチジン誘導体 |
| US8735411B2 (en) | 2006-10-02 | 2014-05-27 | Abbvie Inc. | Macrocyclic benzofused pyrimidine derivatives |
| TWI454262B (zh) * | 2006-11-02 | 2014-10-01 | Targacept Inc | 菸鹼乙醯膽鹼受體亞型選擇性之二氮雜雙環烷類醯胺 |
| CA2669884A1 (en) | 2006-11-15 | 2008-05-22 | High Point Pharmaceuticals, Llc | Novel 2-(2-hydroxyphenyl)benzimidazoles useful for treating obesity and diabetes |
| TW200831085A (en) | 2006-12-13 | 2008-08-01 | Merck & Co Inc | Non-nucleoside reverse transcriptase inhibitors |
| EP1975165A1 (de) | 2007-03-27 | 2008-10-01 | Boehringer Ingelheim Pharma GmbH & Co. KG | Substituierte Pyrrolidinamide, deren Herstellung und deren Verwendung als Arzneimittel |
| JP2010522706A (ja) | 2007-03-29 | 2010-07-08 | エフ.ホフマン−ラ ロシュ アーゲー | 非ヌクレオシド逆転写酵素阻害剤 |
| CL2008001002A1 (es) | 2007-04-11 | 2008-10-17 | Actelion Pharmaceuticals Ltd | Compuestos derivados de oxazolidinona; composicion farmaceutica que comprende a dichos compuestos; y su uso para preparar un medicamento para tratar una infeccion bacteriana. |
| AU2008248996A1 (en) * | 2007-04-27 | 2008-11-13 | Sanofi-Aventis | 2 -heteroaryl- pyrrolo [3, 4-C] pyrrole derivatives and their use as SCD inhibitors |
| CN101687866B (zh) * | 2007-08-07 | 2014-06-04 | Abbvie德国有限责任两合公司 | 用于治疗响应于血色素5-ht6受体调节的疾病的喹啉化合物 |
| DE102007047737A1 (de) | 2007-10-05 | 2009-04-30 | Merck Patent Gmbh | Piperidin- und Piperazinderivate |
| US20090155176A1 (en) | 2007-10-19 | 2009-06-18 | Sarcode Corporation | Compositions and methods for treatment of diabetic retinopathy |
| US7935725B2 (en) | 2007-10-31 | 2011-05-03 | Janssen Pharmaceutica Nv | Aryl-substituted bridged or fused diamines as modulators of leukotriene A4 hydrolase |
| JP2009161449A (ja) | 2007-12-28 | 2009-07-23 | Lion Corp | Ppar活性促進剤並びに美容用飲食品、皮膚外用剤及び医薬 |
| CA2727914A1 (en) | 2008-06-19 | 2009-12-23 | Banyu Pharmaceutical Co., Ltd. | Spirodiamine-diaryl ketoxime derivative technical field |
| EP2328898B1 (de) * | 2008-09-09 | 2014-12-24 | Sanofi | 2-heteroaryl-pyrrolo[3,4-c]pyrrol- derivate und ihre verwendung als scd inhibitoren |
| TW201020247A (en) | 2008-11-06 | 2010-06-01 | Gruenenthal Gmbh | Substituierte disulfonamide |
| CA2739725A1 (en) | 2008-11-17 | 2010-05-20 | F. Hoffmann-La Roche Ag | Naphthylacetic acids used as crth2 antagonists or partial agonists |
| DE102008059578A1 (de) | 2008-11-28 | 2010-06-10 | Merck Patent Gmbh | Benzo-Naphtyridin Verbindungen |
| ES2407852T3 (es) | 2008-12-01 | 2013-06-14 | Merck Patent Gmbh | Pirido[4,3-d]pirimidinas 2,5-diamino sustituidas como inhibidores de autotaxina frente al cáncer |
| TW201035102A (en) | 2009-03-04 | 2010-10-01 | Gruenethal Gmbh | Sulfonylated tetrahydroazolopyrazines and their use as medicinal products |
| RU2480463C1 (ru) | 2009-03-05 | 2013-04-27 | Дайити Санкио Компани, Лимитед | Пиридилокси производные, полезные в качестве активатора/модулятора гамма-рецептора, активируемого пролифератором пероксисом (ppar) гамма |
| WO2010108268A1 (en) * | 2009-03-23 | 2010-09-30 | Merck Frosst Canada Ltd. | Heterocyclic compounds as inhibitors of stearoyl-coenzyme a delta-9 desaturase |
| TW201038572A (en) | 2009-03-25 | 2010-11-01 | Gruenenthal Gmbh | Substituted spiro-amide compounds |
| DE102009014737A1 (de) | 2009-03-25 | 2010-10-07 | Mars, Incorporated | Verfahren und Vorichtung zum Frittieren von Nahrungsmitteln |
| BRPI1012679A2 (pt) | 2009-04-02 | 2016-04-05 | Merck Patent Gmbh | derivados de piperidina e piperazina como inibidores de autotaxina |
| AU2010230646B2 (en) | 2009-04-02 | 2015-11-26 | Merck Patent Gmbh | Heterocyclic compounds as autotaxin inhibitors |
| AU2010230585B2 (en) | 2009-04-02 | 2016-03-24 | Merck Patent Gmbh | Autotaxin inhibitors |
| FR2945534B1 (fr) | 2009-05-12 | 2012-11-16 | Sanofi Aventis | DERIVES DE CYCLOPENTAL[c]PYRROLE-2-CARBOXYLATES, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE |
| US8648066B2 (en) | 2009-05-22 | 2014-02-11 | Exelixis, Inc. | Benzoxazepines as inhibitors of PI3K/mTOR and methods of their use and manufacture |
| WO2010141817A1 (en) | 2009-06-05 | 2010-12-09 | Janssen Pharmaceutica Nv | Heteroaryl-substituted spirocyclic diamine urea modulators of fatty acid amide hydrolase |
| DE102009033392A1 (de) | 2009-07-16 | 2011-01-20 | Merck Patent Gmbh | Heterocyclische Verbindungen als Autotaxin-Inhibitoren II |
| WO2011017350A2 (en) | 2009-08-04 | 2011-02-10 | Amira Pharmaceuticals, Inc. | Compounds as lysophosphatidic acid receptor antagonists |
| UA107360C2 (en) | 2009-08-05 | 2014-12-25 | Biogen Idec Inc | Bicyclic aryl sphingosine 1-phosphate analogs |
| AR079022A1 (es) | 2009-11-02 | 2011-12-21 | Sanofi Aventis | Derivados de acido carboxilico ciclico sustituidos con acilamino, su uso como productos farmaceuticos, composicion farmaceutica y metodo de preparacion |
| KR20120112755A (ko) | 2010-01-07 | 2012-10-11 | 이 아이 듀폰 디 네모아 앤드 캄파니 | 살진균제 복소환 화합물 |
| US8815869B2 (en) | 2010-03-18 | 2014-08-26 | Abbvie Inc. | Lactam acetamides as calcium channel blockers |
| CA2792234C (en) | 2010-03-19 | 2014-05-27 | Pfizer Inc. | 2,3 dihydro-1h-inden-1-yl-2,7-diazaspiro [3.5] nonane derivatives and their use as antagonists or inverse agonists of the ghrelin receptor |
| AU2011232058B2 (en) | 2010-03-26 | 2016-09-08 | Merck Patent Gmbh | Benzonaphthyridinamines as autotaxin inhibitors |
| GB201008005D0 (en) | 2010-05-13 | 2010-06-30 | Sentinel Oncology Ltd | Pharmaceutical compounds |
| EP2575794A2 (en) | 2010-06-04 | 2013-04-10 | B.S.R.C. "Alexander Fleming" | Autotaxin pathway modulation and uses thereof |
| AR082590A1 (es) | 2010-08-12 | 2012-12-19 | Hoffmann La Roche | Inhibidores de la tirosina-quinasa de bruton |
| US9000025B2 (en) | 2010-08-20 | 2015-04-07 | Amira Pharmaceuticals, Inc. | Autotaxin inhibitors and uses thereof |
| AU2011297961B2 (en) | 2010-09-02 | 2015-07-02 | Merck Patent Gmbh | Pyrazolopyridinone derivatives as LPA receptor antagonists |
| WO2012071684A1 (en) * | 2010-12-02 | 2012-06-07 | Shanghai De Novo Pharmatech Co Ltd. | Heterocyclic derivates,preparation processes and medical uses thereof |
| DK2835131T3 (en) | 2010-12-14 | 2017-12-04 | Electrophoretics Ltd | Casein kinase 1 delta inhibitors (CK1 delta) |
| EP2714680B1 (en) | 2011-05-27 | 2015-11-25 | Amira Pharmaceuticals, Inc. | Heterocyclic autotaxin inhibitors and uses thereof |
| US8664213B2 (en) | 2011-08-29 | 2014-03-04 | Bristol-Myers Squibb Company | Spiro bicyclic diamine derivatives as HIV attachment inhibitors |
| WO2013054185A1 (en) | 2011-10-13 | 2013-04-18 | Pfizer, Inc. | Pyrimidine and pyridine derivatives useful in therapy |
| WO2013065712A1 (ja) | 2011-10-31 | 2013-05-10 | 東レ株式会社 | ジアザスピロウレア誘導体及びその医薬用途 |
| US8809552B2 (en) | 2011-11-01 | 2014-08-19 | Hoffmann-La Roche Inc. | Azetidine compounds, compositions and methods of use |
| US9815851B2 (en) | 2011-12-02 | 2017-11-14 | Phenex Pharmaceuticals Ag | Pyrrolo carboxamides as modulators of orphan nuclear receptor RAR-related orphan receptor-gamma (RORγ, NR1F3) activity and for the treatment of chronic inflammatory and autoimmune diseases |
| TWI638802B (zh) | 2012-05-24 | 2018-10-21 | 芬蘭商奧利安公司 | 兒茶酚o-甲基轉移酶活性抑制化合物 |
| NZ702747A (en) | 2012-06-13 | 2017-03-31 | Incyte Holdings Corp | Substituted tricyclic compounds as fgfr inhibitors |
| ES2618703T3 (es) | 2012-06-13 | 2017-06-22 | F. Hoffmann-La Roche Ag | Nuevos compuestos diazaspirocicloalcano y azaspirocicloalcano |
| CN104684560B (zh) | 2012-07-27 | 2018-08-17 | 比奥根艾迪克Ma公司 | 作为s1p调节剂和/或atx调节剂的化合物 |
| WO2014018881A1 (en) | 2012-07-27 | 2014-01-30 | Biogen Idec Ma Inc. | Atx modulating agents |
| ES2687985T3 (es) | 2012-09-25 | 2018-10-30 | Bayer Pharma Aktiengesellschaft | Combinación de regorafenib y ácido acetilsalicílico para el tratamiento del cáncer colorrectal |
| CN104684915B (zh) | 2012-09-25 | 2017-10-31 | 霍夫曼-拉罗奇有限公司 | 新型双环衍生物 |
| AR092742A1 (es) | 2012-10-02 | 2015-04-29 | Intermune Inc | Piridinonas antifibroticas |
| LT3842420T (lt) | 2012-10-25 | 2023-02-27 | Tetra Discovery Partners Llc | Pde4 heteroarilo inhibitoriai |
| SG11201503670YA (en) * | 2012-12-31 | 2015-07-30 | Cadila Healthcare Ltd | Substituted phthalazin-1 (2h)-one derivatives as selective inhibitors of poly (adp-ribose) polymerase-1 |
| WO2014133112A1 (ja) | 2013-03-01 | 2014-09-04 | 国立大学法人東京大学 | オートタキシン阻害活性を有する8-置換イミダゾピリミジノン誘導体 |
| AR095079A1 (es) * | 2013-03-12 | 2015-09-16 | Hoffmann La Roche | Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo |
| TWI593692B (zh) | 2013-03-12 | 2017-08-01 | 美國禮來大藥廠 | 四氫吡咯并噻嗪化合物 |
| EP2970099A4 (en) | 2013-03-12 | 2016-12-21 | Acucela Inc | SUBSTITUTED 3-PHENYLPROPYLAMINE DERIVATIVES FOR THE TREATMENT OF EYE DISEASES AND DRESSES |
| AR095266A1 (es) | 2013-03-12 | 2015-09-30 | Abbvie Inc | Inhibidores de bromodominios tetraciclicos |
| US20160039825A1 (en) | 2013-03-15 | 2016-02-11 | Biogen Ma Inc. | S1p and/or atx modulating agents |
| SG11201600241RA (en) | 2013-07-18 | 2016-02-26 | Novartis Ag | Autotaxin inhibitors comprising a heteroaromatic ring-benzyl-amide-cycle core |
| PL3057959T3 (pl) | 2013-10-17 | 2018-08-31 | Vertex Pharmaceuticals Incorporated | Inhibitory DNA-PK |
| MX375706B (es) | 2013-11-22 | 2025-03-06 | Sabre Therapeutics Llc | Compuestos de inhibidor de autotaxina. |
| KR20160087900A (ko) | 2013-11-26 | 2016-07-22 | 에프. 호프만-라 로슈 아게 | 신규한 옥타하이드로-사이클로부타[1,2-c;3,4-c'']다이피롤-2-일 |
| AR098475A1 (es) | 2013-11-26 | 2016-06-01 | Bayer Cropscience Ag | Compuestos pesticidas y usos |
| CN106029667B (zh) | 2014-03-26 | 2019-08-23 | 豪夫迈·罗氏有限公司 | 作为自分泌运动因子(atx)和溶血磷脂酸(lpa)生产抑制剂的稠合[1,4]二氮杂*化合物 |
| AU2015238537B2 (en) | 2014-03-26 | 2019-08-01 | F. Hoffmann-La Roche Ag | Bicyclic compounds as autotaxin (ATX) and lysophosphatidic acid (LPA) production inhibitors |
| EP3122732B1 (en) | 2014-03-26 | 2018-02-28 | Basf Se | Substituted [1,2,4]triazole and imidazole compounds as fungicides |
| JO3512B1 (ar) | 2014-03-26 | 2020-07-05 | Astex Therapeutics Ltd | مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز |
| WO2015154023A1 (en) | 2014-04-04 | 2015-10-08 | X-Rx Discovery, Inc. | Substituted spirocydic inhibitors of autotaxin |
| AU2015333610B2 (en) | 2014-10-14 | 2019-11-07 | Vitae Pharmaceuticals, Llc | Dihydropyrrolopyridine inhibitors of ROR-gamma |
| WO2016128529A1 (en) | 2015-02-15 | 2016-08-18 | F. Hoffmann-La Roche Ag | 1-(het)arylsulfonyl-(pyrrolidine or piperidine)-2-carboxamide derivatives and their use as trpa1 antagonists |
| MA41898A (fr) | 2015-04-10 | 2018-02-13 | Hoffmann La Roche | Dérivés de quinazolinone bicyclique |
| CN104927727B (zh) | 2015-07-06 | 2017-01-11 | 香山红叶建设有限公司 | 一种玻璃幕墙用结构密封胶及其制备方法 |
| PL415078A1 (pl) | 2015-09-04 | 2017-03-13 | Oncoarendi Therapeutics Spółka Z Ograniczoną Odpowiedzialnością | Podstawione aminotriazole przydatne jako inhibitory kwaśnej chitynazy ssaków |
| EP3344619B1 (en) | 2015-09-04 | 2020-10-28 | H. Hoffnabb-La Roche Ag | Phenoxymethyl derivatives |
| KR20180054635A (ko) | 2015-09-24 | 2018-05-24 | 에프. 호프만-라 로슈 아게 | 오토탁신(atx) 억제제로서 이환형 화합물 |
| CN115124538A (zh) | 2015-09-24 | 2022-09-30 | 豪夫迈·罗氏有限公司 | 作为atx抑制剂的二环化合物 |
| KR20180054634A (ko) | 2015-09-24 | 2018-05-24 | 에프. 호프만-라 로슈 아게 | 이중 오토탁신(atx)/탄산 무수화효소(ca) 억제제로서 신규한 이환형 화합물 |
| RU2725138C2 (ru) | 2015-09-24 | 2020-06-30 | Ф. Хоффманн-Ля Рош Аг | Новые бициклические соединения в качестве двойных ингибиторов аутотаксина (atx)/карбоангидразы (ca) |
| KR20180051626A (ko) | 2015-09-24 | 2018-05-16 | 아이오니스 파마수티컬즈, 인코포레이티드 | Kras 발현의 조절제 |
| MX2018006499A (es) | 2015-11-25 | 2018-08-01 | Dana Farber Cancer Inst Inc | Inhibidores de bromodominio bivalentes y usos de los mismos. |
| EP3385261A4 (en) | 2015-12-01 | 2019-04-24 | Nihon Nohyaku Co., Ltd. | 3H-PYRROLOPYRIDINE COMPOUND OR N-OXIDE OR SALT THEREOF, AGRICULTURAL AND HARDENING INSECTICIDE WITH THE CONNECTION AND USE THEREOF |
| WO2017139978A1 (zh) | 2016-02-19 | 2017-08-24 | 吴伟东 | 手机app更新方法及系统 |
| JP7157755B2 (ja) | 2017-03-16 | 2022-10-20 | エフ.ホフマン-ラ ロシュ アーゲー | 二重atx/ca阻害剤として有用な複素環式化合物 |
| JP7090099B2 (ja) | 2017-03-16 | 2022-06-23 | エフ.ホフマン-ラ ロシュ アーゲー | Atxインヒビターとしての新規二環式化合物 |
| AR111295A1 (es) * | 2017-03-20 | 2019-06-26 | Forma Therapeutics Inc | Composiciones de pirrolopirrol como activadores de piruvato quinasa (pkr) |
-
2016
- 2016-09-21 KR KR1020187008126A patent/KR20180054634A/ko not_active Withdrawn
- 2016-09-21 CA CA2991612A patent/CA2991612A1/en not_active Abandoned
- 2016-09-21 CR CR20180057A patent/CR20180057A/es unknown
- 2016-09-21 BR BR112018006080-1A patent/BR112018006080A2/pt not_active Application Discontinuation
- 2016-09-21 MA MA042923A patent/MA42923A/fr unknown
- 2016-09-21 JP JP2018514985A patent/JP6877413B2/ja active Active
- 2016-09-21 EP EP16770917.9A patent/EP3353178B1/en active Active
- 2016-09-21 WO PCT/EP2016/072347 patent/WO2017050791A1/en not_active Ceased
- 2016-09-21 PE PE2018000079A patent/PE20180552A1/es unknown
- 2016-09-21 CN CN201680049751.XA patent/CN107922415B/zh active Active
- 2016-09-21 MX MX2018001430A patent/MX372962B/es active IP Right Grant
- 2016-09-21 RU RU2018112237A patent/RU2724899C2/ru active
- 2016-09-21 AU AU2016328436A patent/AU2016328436B2/en not_active Ceased
- 2016-09-22 AR ARP160102879A patent/AR106099A1/es unknown
- 2016-09-23 TW TW105130875A patent/TW201720823A/zh unknown
-
2018
- 2018-01-03 IL IL256724A patent/IL256724A/en unknown
- 2018-01-23 ZA ZA2018/00480A patent/ZA201800480B/en unknown
- 2018-01-24 CO CONC2018/0000668A patent/CO2018000668A2/es unknown
- 2018-03-15 CL CL2018000685A patent/CL2018000685A1/es unknown
- 2018-03-23 US US15/933,701 patent/US10647719B2/en active Active
-
2020
- 2020-03-27 US US16/832,553 patent/US20200223854A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| RU2724899C2 (ru) | 2020-06-26 |
| KR20180054634A (ko) | 2018-05-24 |
| RU2018112237A (ru) | 2019-10-29 |
| CN107922415B (zh) | 2022-04-15 |
| EP3353178B1 (en) | 2021-07-14 |
| US20180215765A1 (en) | 2018-08-02 |
| MA42923A (fr) | 2021-04-28 |
| MX2018001430A (es) | 2018-04-20 |
| AU2016328436B2 (en) | 2020-05-14 |
| AU2016328436A1 (en) | 2018-01-25 |
| WO2017050791A1 (en) | 2017-03-30 |
| WO2017050791A8 (en) | 2017-07-06 |
| MX372962B (es) | 2020-03-27 |
| BR112018006080A2 (pt) | 2018-10-09 |
| CN107922415A (zh) | 2018-04-17 |
| TW201720823A (zh) | 2017-06-16 |
| US10647719B2 (en) | 2020-05-12 |
| EP3353178A1 (en) | 2018-08-01 |
| US20200223854A1 (en) | 2020-07-16 |
| IL256724A (en) | 2018-03-29 |
| RU2018112237A3 (es) | 2020-01-17 |
| ZA201800480B (en) | 2018-11-28 |
| CL2018000685A1 (es) | 2018-08-10 |
| JP6877413B2 (ja) | 2021-05-26 |
| AR106099A1 (es) | 2017-12-13 |
| CO2018000668A2 (es) | 2018-05-10 |
| HK1252995A1 (zh) | 2019-06-06 |
| CA2991612A1 (en) | 2017-03-30 |
| CR20180057A (es) | 2018-04-02 |
| JP2018528227A (ja) | 2018-09-27 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| PE20180552A1 (es) | Nuevos compuestos biciclicos como inhibidores duales de atx/ca | |
| PE20180451A1 (es) | Nuevos compuestos biciclicos como inhibidores de atx | |
| PE20180233A1 (es) | Nuevos compuestos biciclicos como inhibidores duales de atx / ca | |
| PE20170206A1 (es) | Inhibidores espirociclicos sustituidos de la autotaxina | |
| JOP20200225A1 (ar) | مشتق كوينولين عالي النقاء وطريقة لإنتاجه | |
| ECSP17073191A (es) | Compuestos heterocíclicos como inhibidores de lsd1 | |
| PE20180461A1 (es) | Nuevos compuestos biciclicos como inhibidores de la atx | |
| PE20151162A1 (es) | Compuestos heterociclicos inhibidores del colesterol 24-hidroxilasa (ch24h) | |
| DOP2016000248A (es) | Inhibidores de diacilglicerol aciltransferasa 2 | |
| PE20160122A1 (es) | Compuestos nobles y composiciones para la inhibicion de fasn | |
| CO2017013229A2 (es) | Agonistas de receptor de apelina (apj) de 4-hidroxi-3-(heteroaril)piridin-2-ona como para uso en el tratamiento de trastornos cardiovasculares | |
| PE20200387A1 (es) | Proceso novedoso para la elaboracion de compuestos para su uso en el tratamiento del cancer | |
| EA201691625A1 (ru) | Ароматические гетероциклические соединения как противовоспалительные соединения | |
| PE20160845A1 (es) | Nuevo octahidro-ciclobuta[1,2-c;3,4-c']dipirrol-2-ilo | |
| ECSP11010830A (es) | Derivados de heteroarilo como inhibidores de dgat1 | |
| AR101816A1 (es) | Derivados de 3-[(pirazol-5-il)-heteroaril]-benzamidas como agentes pesticidas | |
| AR090086A1 (es) | COMPUESTO DE 1H-INDAZOL-3-CARBOXAMIDA COMO INHIBIDORES DE LA GLUCOGENO SINTASA CINASA 3 b | |
| CR20140494A (es) | Inhibidores de dgat1 de eter ciclico de cabeza de puente | |
| MA38645B1 (fr) | Nouveaux inhibiteurs de cyp17/antiandrogènes | |
| AR092555A1 (es) | 2-oxo-2,3-dihidro-indoles y su utilizacion para el tratamiento de trastornos del snc | |
| EA201690847A1 (ru) | Новые ингибиторы dgat2 | |
| AR107132A1 (es) | Cocristal, método de producción del mismo, y medicamento que contiene dicho cocristal | |
| PE20160203A1 (es) | Antagonistas de via para tratar trastornos del sueno por cambio de fase | |
| EA201890476A1 (ru) | ЗАМЕЩЕННЫЕ 1,2-ДИГИДРО-3H-ПИРРОЛО[1,2-c]ИМИДАЗОЛ-3-ОНЫ В КАЧЕСТВЕ АНТИБАКТЕРИАЛЬНЫХ СРЕДСТВ | |
| EA201790243A1 (ru) | 2-оксо-3,4-дигидрохинолин-6-ил-сульфонамиды и их применение в качестве регуляторов роста растений |