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 (cg-RX-API-DMAC10.html) | 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 (cg-RX-API-DMAC10.html) |
| EP (1) | EP2709609B1 (cg-RX-API-DMAC10.html) |
| JP (1) | JP6130827B2 (cg-RX-API-DMAC10.html) |
| WO (1) | WO2012158844A1 (cg-RX-API-DMAC10.html) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5951625B2 (ja) | 2010-11-24 | 2016-07-13 | ザ・トラスティーズ・オブ・コランビア・ユニバーシティー・イン・ザ・シティー・オブ・ニューヨークＴｈｅ Ｔｒｕｓｔｅｅｓ Ｏｆ Ｃｏｌｕｍｂｉａ Ｕｎｉｖｅｒｓｉｔｙ Ｉｎ Ｔｈｅ Ｃｉｔｙ Ｏｆ Ｎｅｗ Ｙｏｒｋ | 加齢性黄斑変性症およびシュタルガルト病の処置のための非レチノイドｒｂｐ４アンタゴニスト |
| KR101589837B1 (ko) | 2011-06-22 | 2016-01-29 | 퍼듀 퍼머 엘피 | 디히드록시 치환기를 포함하는 trpv1 길항제 및 그의 용도 |
| US9394293B2 (en) | 2011-08-10 | 2016-07-19 | Purdue Pharma L.P. | TRPV1 antagonists including dihydroxy substituent and uses thereof |
| US9333202B2 (en) | 2012-05-01 | 2016-05-10 | The Trustees Of Columbia University In The City Of New York | Non-retinoid antagonists for treatment of age-related macular degeneration and stargardt disease |
| US20150376198A1 (en) * | 2013-02-18 | 2015-12-31 | The Scripps Research Institute | Modulators of vasopressin receptors with therapeutic potential |
| EP2968303B1 (en) | 2013-03-14 | 2018-07-04 | The Trustees of Columbia University in the City of New York | Octahydrocyclopentapyrroles, their preparation and use |
| WO2014151936A1 (en) | 2013-03-14 | 2014-09-25 | The Trustees Of Columbia University In The City Of New York | Octahydropyrrolopyrroles, their preparation and use |
| ES2705247T3 (es) | 2013-03-14 | 2019-03-22 | Univ Columbia | 4-fenilpiperidinas, su preparación y uso |
| 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 |
| AU2015253232B2 (en) | 2014-04-30 | 2020-10-01 | The Trustees Of Columbia University In The City Of New York | Substituted 4-phenylpiperidines, their preparation and use |
| CN113121450A (zh) | 2014-08-29 | 2021-07-16 | Tes制药有限责任公司 | α-氨基-β-羧基粘康酸半醛脱羧酶抑制剂 |
| WO2016168535A1 (en) * | 2015-04-15 | 2016-10-20 | Valent Biosciences Corporation | (s)-2'-vinyl-abscisic acid derivatives |
| MX378998B (es) | 2015-06-03 | 2025-03-11 | Bristol Myers Squibb Co | Agonistas de receptor de apelina (apj) de 4-hidroxi-3-(heteroaril) piridin-2-ona como para uso en el tratamiento de trastornos cardiovasculares. |
| 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 |
| CA3091142C (en) | 2018-02-26 | 2023-04-11 | Gilead Sciences, Inc. | Substituted pyrrolizine compounds and uses thereof |
| JPWO2024095962A1 (cg-RX-API-DMAC10.html) | 2022-10-31 | 2024-05-10 |
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 |
| DE69529172T2 (de) | 1994-10-07 | 2003-04-17 | Fujisawa Pharmaceutical Co., Ltd. | Zyklische hexapeptide mit antibiotischer aktivität |
| CZ285870B6 (cs) | 1995-06-21 | 1999-11-17 | Shionogi & Co., Ltd. | Bicyklické aminoderiváty a antagonist PGD2, který je obsahuje |
| JPH11139969A (ja) * | 1997-08-07 | 1999-05-25 | Tanabe Seiyaku Co Ltd | 医薬組成物 |
| JP2004501867A (ja) | 2000-03-07 | 2004-01-22 | ランバクシー ラボラトリーズ リミテッド | 真菌感染症に対する治療薬としてのアゾール化合物 |
| JP2004525071A (ja) | 2000-07-20 | 2004-08-19 | ニューロジェン コーポレイション | カプサイシン受容体リガンド |
| PE20021081A1 (es) | 2001-04-12 | 2002-12-18 | Pharmacopeia Drug Discovery | Aril y biaril piperidinas con actividad moduladora mch |
| US7084156B2 (en) | 2001-11-27 | 2006-08-01 | Merck & Co., Inc. | 2-Aminoquinoline compounds |
| AU2003212882A1 (en) | 2002-02-01 | 2003-09-02 | Euro-Celtique S.A. | 2 - piperazine - pyridines useful for treating pain |
| 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 |
| PT1556354E (pt) | 2002-06-28 | 2008-04-17 | Euro Celtique Sa | Derivados de piperazina úteis como agentes terapêuticos para o tratamento da dor |
| 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 |
| MXPA05003948A (es) | 2002-10-17 | 2005-06-17 | Amgen Inc | Derivados de bencimidazol y su uso como ligandos de receptor vaniloide. |
| US7582635B2 (en) | 2002-12-24 | 2009-09-01 | Purdue Pharma, L.P. | Therapeutic agents useful for treating pain |
| AR044688A1 (es) | 2003-06-12 | 2005-09-21 | Euro Celtique Sa | Agentes terapeuticos utiles para el tratamiento del dolor |
| SI1867644T1 (sl) | 2003-07-24 | 2009-10-31 | Euro Celtique Sa | Heteroaril-tetrahidropiperidilne spojine, koristne za zdravljenje ali preprečevanje bolečine |
| ATE430741T1 (de) * | 2003-07-24 | 2009-05-15 | Euro Celtique Sa | Piperidinverbindungen und pharmazeutische zusammensetzungen, die diese enthalten |
| SI1648880T1 (sl) | 2003-08-01 | 2010-05-31 | Euro Celtique Sa | Terapevtska sredstva uporabna za zdravljenje bolečine |
| HRP20080492T3 (hr) | 2003-09-22 | 2008-11-30 | Euro-Celtique S.A. | Fenil-karboksamidni spojevi korisni za liječenje boli |
| JP4630871B2 (ja) | 2003-09-22 | 2011-02-09 | ユーロ−セルティーク エス．エイ． | 疼痛を治療するのに有用な治療薬 |
| 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 |
| MY149038A (en) | 2004-05-26 | 2013-07-15 | Eisai R&D Man Co Ltd | Cinnamide compound |
| 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 |
| TWI362930B (en) | 2007-04-27 | 2012-05-01 | Purdue Pharma Lp | Trpv1 antagonists and uses thereof |
| CA2719789A1 (en) | 2008-04-17 | 2009-10-22 | Pfizer Inc. | 4-benzylidene-3-methylpiperidine aryl carboxamide compounds useful as faah inhibitors |
| JP5579170B2 (ja) | 2008-06-05 | 2014-08-27 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | Ｄｇａｔ阻害剤とｐｐａｒ作動薬を含有する薬剤組み合わせ物 |
| US8546388B2 (en) | 2008-10-24 | 2013-10-01 | Purdue Pharma L.P. | Heterocyclic TRPV1 receptor ligands |
| 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 |
| 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 |
-
2012
- 2012-05-16 EP EP12785516.1A patent/EP2709609B1/en active Active
- 2012-05-16 JP JP2014511504A patent/JP6130827B2/ja active Active
- 2012-05-16 WO PCT/US2012/038215 patent/WO2012158844A1/en not_active Ceased
- 2012-05-16 US US14/118,113 patent/US9156830B2/en not_active Expired - Fee Related