JP2014515349A5 - - Google Patents
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- Publication number
- JP2014515349A5 JP2014515349A5 JP2014511504A JP2014511504A JP2014515349A5 JP 2014515349 A5 JP2014515349 A5 JP 2014515349A5 JP 2014511504 A JP2014511504 A JP 2014511504A JP 2014511504 A JP2014511504 A JP 2014511504A JP 2014515349 A5 JP2014515349 A5 JP 2014515349A5
- Authority
- JP
- Japan
- Prior art keywords
- halo
- alkyl
- pharmaceutically acceptable
- independently
- solvate
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 125000001475 halogen functional group Chemical group 0.000 claims description 70
- 150000001875 compounds Chemical class 0.000 claims description 65
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 54
- 150000003839 salts Chemical class 0.000 claims description 31
- 125000000623 heterocyclic group Chemical group 0.000 claims description 16
- 125000006370 trihalo methyl group Chemical group 0.000 claims description 16
- 229910052799 carbon Inorganic materials 0.000 claims description 12
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 7
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 6
- 239000003937 drug carrier Substances 0.000 claims description 6
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 6
- 102000003566 TRPV1 Human genes 0.000 claims description 5
- 101150016206 Trpv1 gene Proteins 0.000 claims description 5
- 125000000217 alkyl group Chemical group 0.000 claims description 5
- 125000001072 heteroaryl group Chemical group 0.000 claims description 5
- 239000000203 mixture Substances 0.000 claims description 5
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 4
- -1 -OR 7 Chemical group 0.000 claims description 4
- YLQBMQCUIZJEEH-UHFFFAOYSA-N Furan Chemical compound C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims description 4
- 208000025865 Ulcer Diseases 0.000 claims description 4
- 231100000397 ulcer Toxicity 0.000 claims description 4
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 3
- 125000004432 carbon atom Chemical group C* 0.000 claims description 3
- 125000005016 hydroxyalkynyl group Chemical group 0.000 claims description 3
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims description 2
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims description 2
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical compound C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 claims description 2
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims description 2
- CTAPFRYPJLPFDF-UHFFFAOYSA-N isoxazole Chemical compound C=1C=NOC=1 CTAPFRYPJLPFDF-UHFFFAOYSA-N 0.000 claims description 2
- WCPAKWJPBJAGKN-UHFFFAOYSA-N oxadiazole Chemical compound C1=CON=N1 WCPAKWJPBJAGKN-UHFFFAOYSA-N 0.000 claims description 2
- 229910052760 oxygen Inorganic materials 0.000 claims description 2
- 229910052717 sulfur Inorganic materials 0.000 claims description 2
- 239000012453 solvate Substances 0.000 claims 29
- 125000006375 C2-C10 alkynyl group Chemical group 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 description 4
- 125000006590 (C2-C6) alkenylene group Chemical group 0.000 description 4
- 125000006591 (C2-C6) alkynylene group Chemical group 0.000 description 4
- 230000002401 inhibitory effect Effects 0.000 description 3
- 125000000392 cycloalkenyl group Chemical group 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 230000002265 prevention Effects 0.000 description 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 description 1
- 125000000304 alkynyl group Chemical group 0.000 description 1
- 238000004132 cross linking Methods 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161487224P | 2011-05-17 | 2011-05-17 | |
| US61/487,224 | 2011-05-17 | ||
| PCT/US2012/038215 WO2012158844A1 (en) | 2011-05-17 | 2012-05-16 | Heterocyclic compounds |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014515349A JP2014515349A (ja) | 2014-06-30 |
| JP2014515349A5 true JP2014515349A5 (enExample) | 2016-10-27 |
| JP6130827B2 JP6130827B2 (ja) | 2017-05-17 |
Family
ID=47177330
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014511504A Active JP6130827B2 (ja) | 2011-05-17 | 2012-05-16 | ヘテロ環化合物 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US9156830B2 (enExample) |
| EP (1) | EP2709609B1 (enExample) |
| JP (1) | JP6130827B2 (enExample) |
| WO (1) | WO2012158844A1 (enExample) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2642998B1 (en) | 2010-11-24 | 2020-09-16 | The Trustees of Columbia University in the City of New York | A non-retinoid rbp4 antagonist for treatment of age-related macular degeneration and stargardt disease |
| US9273043B2 (en) | 2011-06-22 | 2016-03-01 | Purdue Pharma L.P. | TRPV1 antagonists including dihydroxy substituent and uses thereof |
| AU2012293417A1 (en) | 2011-08-10 | 2013-05-02 | Purdue Pharma L.P. | TRPV1 antagonists including dihydroxy substituent and uses thereof |
| WO2013166037A1 (en) | 2012-05-01 | 2013-11-07 | The Trustees Of Columbia University In The City Of New York | Non-retinoid antagonists for treatment of eye disorders |
| EP2956441A4 (en) * | 2013-02-18 | 2016-11-02 | Scripps Research Inst | MODULATORS OF VASOPRESSIN RECEPTORS WITH THERAPEUTIC POTENTIAL |
| WO2014151936A1 (en) | 2013-03-14 | 2014-09-25 | The Trustees Of Columbia University In The City Of New York | Octahydropyrrolopyrroles, their preparation and use |
| US9938291B2 (en) | 2013-03-14 | 2018-04-10 | The Trustess Of Columbia University In The City Of New York | N-alkyl-2-phenoxyethanamines, their preparation and use |
| ES2700541T3 (es) | 2013-03-14 | 2019-02-18 | Univ Columbia | Octahidrociclopentapirroles, su preparación y uso |
| WO2014152013A1 (en) | 2013-03-14 | 2014-09-25 | The Trustees Of Columbia University In The City Of New York | 4-phenylpiperidines, their preparation and use |
| DK4036094T3 (da) | 2014-04-30 | 2026-03-23 | Univ Columbia | Erstattede 4-fenylpiperidiner, deres fremstilling og anvendelse |
| EP3186242B1 (en) | 2014-08-29 | 2021-10-06 | Tes Pharma S.r.l. | Inhibitors of alpha-amino-beta-carboxymuconic acid semialdehyde decarboxylase |
| AU2016250265A1 (en) * | 2015-04-15 | 2017-10-12 | Valent Biosciences Llc | (S)-2'-vinyl-abscisic acid derivatives |
| CA2988147C (en) | 2015-06-03 | 2023-06-13 | Bristol-Myers Squibb Company | 4-hydroxy-3-(heteroaryl)pyridine-2-one apj agonists for use in the treatment of cardiovascular disorders |
| JOP20190024A1 (ar) | 2016-08-26 | 2019-02-19 | Gilead Sciences Inc | مركبات بيروليزين بها استبدال واستخداماتها |
| CN108218848B (zh) * | 2018-01-22 | 2020-12-18 | 贵州大学 | 一种三氟甲基吡啶联噁二唑（醚）类衍生物及其应用 |
| KR102526964B1 (ko) | 2018-02-26 | 2023-04-28 | 길리애드 사이언시즈, 인코포레이티드 | Hbv 복제 억제제로서의 치환된 피롤리진 화합물 |
| CN120513091A (zh) | 2022-10-31 | 2025-08-19 | 盐野义制药株式会社 | 作为trpv1拮抗剂的吡啶衍生物的用途 |
| TW202604903A (zh) * | 2024-06-11 | 2026-02-01 | 大陸商上海濟煜醫藥科技有限公司 | 作為kras抑制劑的稠合吡啶酮類化合物的製備方法、中間體及其製備方法 |
Family Cites Families (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA1261835A (en) | 1984-08-20 | 1989-09-26 | Masaaki Toda | (fused) benz(thio)amides |
| US5639754A (en) | 1994-07-12 | 1997-06-17 | Janssen Pharmaceutica N.V. | Urea and thiourea derivatives of azolones |
| JP2897427B2 (ja) | 1994-10-07 | 1999-05-31 | 藤沢薬品工業株式会社 | 抗微生物活性を有する環状ヘキサペプチド化合物 |
| ATE337294T1 (de) | 1995-06-21 | 2006-09-15 | Shionogi & Co | Bizyklische aminoderivate und enthaltende pgd2- antagonisten |
| JPH11139969A (ja) * | 1997-08-07 | 1999-05-25 | Tanabe Seiyaku Co Ltd | 医薬組成物 |
| EP1278755A2 (en) | 2000-03-07 | 2003-01-29 | Ranbaxy Laboratories, Limited | Azole compounds as therapeutic agents for fungal infections |
| WO2002008221A2 (en) * | 2000-07-20 | 2002-01-31 | Neurogen Corporation | Capsaicin receptor ligands |
| ATE460163T1 (de) | 2001-04-12 | 2010-03-15 | Pharmacopeia Llc | Arly und diaryl piperidinderivate verwendbar als mch-hemmer |
| CA2468015A1 (en) | 2001-11-27 | 2003-06-05 | Merck & Co., Inc. | 2-aminoquinoline compounds |
| DK1472225T3 (da) | 2002-02-01 | 2010-08-09 | Euro Celtique Sa | 2-Piperazinpyridiner, som er anvendelige til behandling af smerte |
| US6974818B2 (en) | 2002-03-01 | 2005-12-13 | Euro-Celtique S.A. | 1,2,5-thiadiazol-3-YL-piperazine therapeutic agents useful for treating pain |
| ES2300613T3 (es) | 2002-06-28 | 2008-06-16 | Euro-Celtique S.A. | Derivados terapeuticos de piperacina utiles para tratar el dolor. |
| US7262194B2 (en) | 2002-07-26 | 2007-08-28 | Euro-Celtique S.A. | Therapeutic agents useful for treating pain |
| US7157462B2 (en) | 2002-09-24 | 2007-01-02 | Euro-Celtique S.A. | Therapeutic agents useful for treating pain |
| AU2003301436A1 (en) | 2002-10-17 | 2004-05-04 | Amgen Inc. | Benzimidazole derivatives and their use as vanilloid receptor ligands |
| US7582635B2 (en) | 2002-12-24 | 2009-09-01 | Purdue Pharma, L.P. | Therapeutic agents useful for treating pain |
| MY142655A (en) | 2003-06-12 | 2010-12-15 | Euro Celtique Sa | Therapeutic agents useful for treating pain |
| BRPI0412808A (pt) | 2003-07-24 | 2006-09-26 | Euro Celtique Sa | compostos de piperidina e composições farmacêuticas contendo os mesmos |
| EP2080757A1 (en) * | 2003-07-24 | 2009-07-22 | Euro-Celtique S.A. | Heteroaryl-tetrahydropiperidyl compounds useful for treating or preventing pain |
| SI1942106T1 (sl) | 2003-08-01 | 2012-01-31 | Euro Celtique Sa | Terapevtska sredstva, uporabna za zdravljenje bolečine |
| PT2017276E (pt) | 2003-09-22 | 2011-04-05 | Euro Celtique Sa | Compostos de fenilcarboxamida úteis para o tratamento da dor |
| DE602004017481D1 (de) | 2003-09-22 | 2008-12-11 | Euro Celtique Sa | Zur behandlung von schmerzen geeignete therapeutische mittel |
| US7592373B2 (en) | 2003-12-23 | 2009-09-22 | Boehringer Ingelheim International Gmbh | Amide compounds with MCH antagonistic activity and medicaments comprising these compounds |
| CN1902178A (zh) | 2003-12-30 | 2007-01-24 | 欧洲凯尔特公司 | 用于治疗疼痛的哌嗪 |
| US7605176B2 (en) | 2004-03-06 | 2009-10-20 | Boehringer Ingelheim International Gmbh | β-ketoamide compounds with MCH antagonistic activity |
| BRPI0511504A (pt) | 2004-05-26 | 2008-01-22 | Eisai R&D Man Co Ltd | composto ou um sal farmaceuticamente aceitável do mesmo, e, agente preventivo ou terapêutico para uma doença resultante de beta-amilóides |
| JP2009519208A (ja) | 2005-12-15 | 2009-05-14 | 塩野義製薬株式会社 | アミド誘導体を含有する医薬組成物 |
| DE102007018151A1 (de) * | 2007-04-16 | 2008-10-23 | Günenthal GmbH | Neue Vanilloid-Rezeptor Liganden und ihre Verwendung zur Herstellung von Arzneimitteln |
| EP2479173A1 (en) | 2007-04-27 | 2012-07-25 | Purdue Pharma LP | Therapeutic agents useful for treating pain |
| EP2604599A1 (en) | 2007-04-27 | 2013-06-19 | Purdue Pharma LP | TRPV1 antagonists and uses thereof |
| WO2009127946A1 (en) | 2008-04-17 | 2009-10-22 | Pfizer Inc. | 4-benzylidene-3-methylpiperidine aryl carboxamide compounds useful as faah inhibitors |
| PE20140572A1 (es) | 2008-06-05 | 2014-05-16 | Janssen Pharmaceutica Nv | Combinaciones de drogas que comprenden un inhibidor de dgat y un agonista de ppar |
| US8703962B2 (en) | 2008-10-24 | 2014-04-22 | Purdue Pharma L.P. | Monocyclic compounds and their use as TRPV1 ligands |
| US8759362B2 (en) | 2008-10-24 | 2014-06-24 | Purdue Pharma L.P. | Bicycloheteroaryl compounds and their use as TRPV1 ligands |
| US8546388B2 (en) | 2008-10-24 | 2013-10-01 | Purdue Pharma L.P. | Heterocyclic TRPV1 receptor ligands |
| WO2010064597A1 (ja) | 2008-12-01 | 2010-06-10 | 武田薬品工業株式会社 | ピペリジン誘導体 |
| GB0902173D0 (en) | 2009-02-10 | 2009-03-25 | Takeda Pharmaceutical | Compounds and their use |
| JP5876423B2 (ja) | 2010-06-22 | 2016-03-02 | 塩野義製薬株式会社 | Ｔｒｐｖ１阻害活性を有する化合物とその使用 |
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2012
- 2012-05-16 EP EP12785516.1A patent/EP2709609B1/en active Active
- 2012-05-16 US US14/118,113 patent/US9156830B2/en not_active Expired - Fee Related
- 2012-05-16 JP JP2014511504A patent/JP6130827B2/ja active Active
- 2012-05-16 WO PCT/US2012/038215 patent/WO2012158844A1/en not_active Ceased