CN103619817A - 新颖的二环含氮杂芳基tgr5受体调节剂 - Google Patents
新颖的二环含氮杂芳基tgr5受体调节剂 Download PDFInfo
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- CN103619817A CN103619817A CN201280031836.7A CN201280031836A CN103619817A CN 103619817 A CN103619817 A CN 103619817A CN 201280031836 A CN201280031836 A CN 201280031836A CN 103619817 A CN103619817 A CN 103619817A
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- alkyl
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- 0 Cc(c(*)c1C2=C(C)CC(**)CCC2)c(*)c2c1SCCN2C(C**[U]c1c(*)c(*)c(*)*(*)c1*)=O Chemical compound Cc(c(*)c1C2=C(C)CC(**)CCC2)c(*)c2c1SCCN2C(C**[U]c1c(*)c(*)c(*)*(*)c1*)=O 0.000 description 4
- NUVCHIRBNLDKJQ-UHFFFAOYSA-N Brc1c2OCCNc2ccc1 Chemical compound Brc1c2OCCNc2ccc1 NUVCHIRBNLDKJQ-UHFFFAOYSA-N 0.000 description 1
- HRCMXYXVAWHBTH-UHFFFAOYSA-N C1Oc(cccc2)c2N1 Chemical compound C1Oc(cccc2)c2N1 HRCMXYXVAWHBTH-UHFFFAOYSA-N 0.000 description 1
- VHEPADRAYRQXLU-UHFFFAOYSA-N CC(C(Nc1ccc2)=O)Oc1c2Br Chemical compound CC(C(Nc1ccc2)=O)Oc1c2Br VHEPADRAYRQXLU-UHFFFAOYSA-N 0.000 description 1
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- WGGASHRVZWVPDZ-UHFFFAOYSA-N CC(CN(C(C1C(COc2cccc(C)c2C)C1)=O)c1ccc2)=Cc1c2Br Chemical compound CC(CN(C(C1C(COc2cccc(C)c2C)C1)=O)c1ccc2)=Cc1c2Br WGGASHRVZWVPDZ-UHFFFAOYSA-N 0.000 description 1
- SZEYQYWRMAIUMK-UHFFFAOYSA-N CCC[n]1ncc(-c2c(CCCN3C(CCCO)=O)c3ccc2)c1 Chemical compound CCC[n]1ncc(-c2c(CCCN3C(CCCO)=O)c3ccc2)c1 SZEYQYWRMAIUMK-UHFFFAOYSA-N 0.000 description 1
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- CGSHHIFVWDGTQL-UHFFFAOYSA-N CCOC(CCCOc1cccc(C)c1C)=O Chemical compound CCOC(CCCOc1cccc(C)c1C)=O CGSHHIFVWDGTQL-UHFFFAOYSA-N 0.000 description 1
- HMCAYFBGOBOVHC-UHFFFAOYSA-N Cc(c(Cl)ccc1)c1OCC1(CC1)C(N1c2cccc(Br)c2CCC1)=O Chemical compound Cc(c(Cl)ccc1)c1OCC1(CC1)C(N1c2cccc(Br)c2CCC1)=O HMCAYFBGOBOVHC-UHFFFAOYSA-N 0.000 description 1
- XPSLIIOIORMHLA-UHFFFAOYSA-N Cc(c(OCCOC(N(C1)c2cccc(-c3c[n](Cc(c(F)cc(C(O)=O)c4)c4Cl)nc3)c2OCC1F)=O)ccc1)c1Cl Chemical compound Cc(c(OCCOC(N(C1)c2cccc(-c3c[n](Cc(c(F)cc(C(O)=O)c4)c4Cl)nc3)c2OCC1F)=O)ccc1)c1Cl XPSLIIOIORMHLA-UHFFFAOYSA-N 0.000 description 1
- NXYTXHSGGMNOBV-UHFFFAOYSA-N Cc1c(C)c(NC(CCC(OC)=O)=O)ccc1 Chemical compound Cc1c(C)c(NC(CCC(OC)=O)=O)ccc1 NXYTXHSGGMNOBV-UHFFFAOYSA-N 0.000 description 1
- LJOCFCHDBVNYMP-ABPREGFTSA-N Cc1c(C)c(OCC(C2)C2C(N(C2)c3cccc(-c4c[n](Cc5cccc(C(O)=O)c5)nc4)c3[C@@H]3C2=C3)=O)ccc1 Chemical compound Cc1c(C)c(OCC(C2)C2C(N(C2)c3cccc(-c4c[n](Cc5cccc(C(O)=O)c5)nc4)c3[C@@H]3C2=C3)=O)ccc1 LJOCFCHDBVNYMP-ABPREGFTSA-N 0.000 description 1
- UPLFNAKFLORCKE-UHFFFAOYSA-N Cc1c(C)c(OCCCC(N(CCCC2)c3c2c(-c2c[n](Cc4cccc(C5OC5O)c4)nc2)ccc3)=O)ccc1 Chemical compound Cc1c(C)c(OCCCC(N(CCCC2)c3c2c(-c2c[n](Cc4cccc(C5OC5O)c4)nc2)ccc3)=O)ccc1 UPLFNAKFLORCKE-UHFFFAOYSA-N 0.000 description 1
- FUDOJUCDHNSNCS-UHFFFAOYSA-N Cc1cccc(OCCCC(N2c3cccc(-c4c[nH]nc4)c3CCC2)=O)c1C Chemical compound Cc1cccc(OCCCC(N2c3cccc(-c4c[nH]nc4)c3CCC2)=O)c1C FUDOJUCDHNSNCS-UHFFFAOYSA-N 0.000 description 1
- FVWULJONKSJYKT-UHFFFAOYSA-N Cc1cccc(OCCCC(N2c3cccc(-c4c[n](Cc5cccc(C(NCCN)=O)c5)nc4)c3CCC2)=O)c1C Chemical compound Cc1cccc(OCCCC(N2c3cccc(-c4c[n](Cc5cccc(C(NCCN)=O)c5)nc4)c3CCC2)=O)c1C FVWULJONKSJYKT-UHFFFAOYSA-N 0.000 description 1
- PPUGYSZZQBXXSM-UHFFFAOYSA-N Cc1cccc(OCCCC(N2c3cccc(-c4c[n](Cc5cccc(CN)c5)nc4)c3CCC2)=O)c1C Chemical compound Cc1cccc(OCCCC(N2c3cccc(-c4c[n](Cc5cccc(CN)c5)nc4)c3CCC2)=O)c1C PPUGYSZZQBXXSM-UHFFFAOYSA-N 0.000 description 1
- YHKILGTWNKSEPN-UHFFFAOYSA-N Cc1cccc(OCCCC(N2c3cccc(-c4c[n](Cc5cccc(N/C(/N)=N/C#N)c5)nc4)c3CCC2)=O)c1C Chemical compound Cc1cccc(OCCCC(N2c3cccc(-c4c[n](Cc5cccc(N/C(/N)=N/C#N)c5)nc4)c3CCC2)=O)c1C YHKILGTWNKSEPN-UHFFFAOYSA-N 0.000 description 1
- YBHAWCDJUSXCGP-UHFFFAOYSA-N Cc1cccc(OCCCC(N2c3cccc(-c4c[n](Cc5ccnc(S(C)(=O)=O)n5)nc4)c3CCC2)=O)c1C Chemical compound Cc1cccc(OCCCC(N2c3cccc(-c4c[n](Cc5ccnc(S(C)(=O)=O)n5)nc4)c3CCC2)=O)c1C YBHAWCDJUSXCGP-UHFFFAOYSA-N 0.000 description 1
- CWFGRCUGCOLZAI-UHFFFAOYSA-N Cc1cccc(OCCCC(N2c3cccc(-c4cccc(CNC(CC(O)=O)=O)c4)c3CCC2)=O)c1C Chemical compound Cc1cccc(OCCCC(N2c3cccc(-c4cccc(CNC(CC(O)=O)=O)c4)c3CCC2)=O)c1C CWFGRCUGCOLZAI-UHFFFAOYSA-N 0.000 description 1
- YYNHKHQKBGOVCZ-UHFFFAOYSA-N Cc1cccc(OCCCC(N2c3cccc(-c4n[n](Cc5cccc(N)c5)nn4)c3CCC2)=O)c1C Chemical compound Cc1cccc(OCCCC(N2c3cccc(-c4n[n](Cc5cccc(N)c5)nn4)c3CCC2)=O)c1C YYNHKHQKBGOVCZ-UHFFFAOYSA-N 0.000 description 1
- MNBRZADWFFCCFK-UHFFFAOYSA-N Cc1cccc2c1OCNC2 Chemical compound Cc1cccc2c1OCNC2 MNBRZADWFFCCFK-UHFFFAOYSA-N 0.000 description 1
- BDIWDYRZYUJQSL-UHFFFAOYSA-N Cc1ccccc1OCCCC(N1c2cccc(-c3cccc(COC(NCCC(O)=O)=O)c3)c2CCC1)=O Chemical compound Cc1ccccc1OCCCC(N1c2cccc(-c3cccc(COC(NCCC(O)=O)=O)c3)c2CCC1)=O BDIWDYRZYUJQSL-UHFFFAOYSA-N 0.000 description 1
- HJXULOGMYXVHMM-UHFFFAOYSA-N O=C(C1)OC2=C1C=CCC2 Chemical compound O=C(C1)OC2=C1C=CCC2 HJXULOGMYXVHMM-UHFFFAOYSA-N 0.000 description 1
- REUYOGFVIXVCRX-UHFFFAOYSA-N OS(CCNC(c1cc(C[n]2ncc(-c3c(CCCN4C(CCCC(c(cc5)ccc5Cl)(F)F)=O)c4ccc3)c2)ccc1)=O)(=O)=O Chemical compound OS(CCNC(c1cc(C[n]2ncc(-c3c(CCCN4C(CCCC(c(cc5)ccc5Cl)(F)F)=O)c4ccc3)c2)ccc1)=O)(=O)=O REUYOGFVIXVCRX-UHFFFAOYSA-N 0.000 description 1
- JYGRLCRHEGTISO-UHFFFAOYSA-N OS(CNC(c1cc(C[n]2ncc(-c3c(CCCN4C(CCCC(c(cc5)ccc5Cl)(F)F)=O)c4ccc3)c2)ccc1)=O)(=O)=O Chemical compound OS(CNC(c1cc(C[n]2ncc(-c3c(CCCN4C(CCCC(c(cc5)ccc5Cl)(F)F)=O)c4ccc3)c2)ccc1)=O)(=O)=O JYGRLCRHEGTISO-UHFFFAOYSA-N 0.000 description 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/04—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms
- C07D215/08—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms with acylated ring nitrogen atom
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- C07D215/12—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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- C07D215/12—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D215/14—Radicals substituted by oxygen atoms
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- C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
- C07D221/04—Ortho- or peri-condensed ring systems
- C07D221/06—Ring systems of three rings
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- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
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- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
- C07F9/576—Six-membered rings
- C07F9/60—Quinoline or hydrogenated quinoline ring systems
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| US61/479,917 | 2011-04-28 | ||
| PCT/US2012/035327 WO2012149236A1 (en) | 2011-04-28 | 2012-04-27 | Novel bicyclic nitrogen containing heteroaryl tgr5 receptor modulators |
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| CN103619817A true CN103619817A (zh) | 2014-03-05 |
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| JP (1) | JP2014518853A (https=) |
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| TW (1) | TW201247627A (https=) |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110536886A (zh) * | 2017-03-22 | 2019-12-03 | 先正达参股股份有限公司 | 杀有害生物活性环丙基甲基酰胺衍生物 |
| CN114199812A (zh) * | 2021-12-28 | 2022-03-18 | 南通联亚药业有限公司 | 一种盐酸美金刚缓释制剂中盐酸美金刚的检测方法 |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103665043B (zh) | 2012-08-30 | 2017-11-10 | 江苏豪森药业集团有限公司 | 一种替诺福韦前药及其在医药上的应用 |
| JP6553632B2 (ja) | 2013-11-18 | 2019-07-31 | フォーマ セラピューティクス,インコーポレイテッド | Betブロモドメイン阻害剤としてのテトラヒドロキノリン組成物 |
| CN106029076B (zh) | 2013-11-18 | 2019-06-07 | 福马疗法公司 | 作为bet溴域抑制剂的苯并哌嗪组合物 |
| WO2015089800A1 (en) * | 2013-12-19 | 2015-06-25 | Eli Lilly And Company | Fluorophenyl pyrazol compounds |
| WO2016036633A1 (en) * | 2014-09-05 | 2016-03-10 | Merck Sharp & Dohme Corp. | Tetrahydroisoquinoline derivatives useful as inhibitors of diacylglyceride o-acyltransferase 2 |
| WO2016036638A1 (en) * | 2014-09-05 | 2016-03-10 | Merck Sharp & Dohme Corp. | Isoquinoline derivatives useful as inhibitors of diacylglyceride o-acyltransferase 2 |
| US9877957B2 (en) | 2014-09-05 | 2018-01-30 | Merck Sharp & Dohme Corp. | Tetrahydroisoquinoline derivatives useful as inhibitors of diacylglyceride O-acyltransferase 2 |
| JP6592512B2 (ja) | 2014-10-24 | 2019-10-16 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | 三環式アトロプ異性体の化合物 |
| EA034931B1 (ru) | 2014-10-24 | 2020-04-08 | Бристол-Майерс Сквибб Компани | Индолкарбоксамидные соединения |
| US10654834B2 (en) * | 2016-07-01 | 2020-05-19 | Venenum Biodesign, LLC | Non-systemic TGR5 agonists |
| JP2022552655A (ja) | 2019-10-07 | 2022-12-19 | キャリーオペ,インク. | Gpr119アゴニスト |
| CA3166630A1 (en) | 2020-01-03 | 2021-07-08 | Berg Llc | Polycyclic amides as ube2k modulators for treating cancer |
| IL295825A (en) | 2020-02-28 | 2022-10-01 | Kallyope Inc | gpr40 agonists |
| WO2021236617A1 (en) | 2020-05-19 | 2021-11-25 | Kallyope, Inc. | Ampk activators |
| CA3183575A1 (en) | 2020-06-26 | 2021-12-30 | Iyassu Sebhat | Ampk activators |
| KR20240161147A (ko) | 2022-03-14 | 2024-11-12 | 슬랩 파마슈티컬스 엘엘씨 | 다중 사이클릭 화합물 |
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| CN1051038A (zh) * | 1989-10-20 | 1991-05-01 | 大塚制药株式会社 | 苯并杂环化合物 |
| CN1098406A (zh) * | 1993-04-13 | 1995-02-08 | 藤泽药品工业株式会社 | 新的苯甲酰胺衍生物及其制法和含有它们的药物组合物 |
| WO2010107768A1 (en) * | 2009-03-18 | 2010-09-23 | Schering Corporation | Bicyclic compounds as inhibitors of diacylglycerol acyltransferase |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| JP3362494B2 (ja) * | 1994-03-01 | 2003-01-07 | 三菱ウェルファーマ株式会社 | ベンゾオキサジン化合物 |
| JP2006063064A (ja) * | 2004-07-27 | 2006-03-09 | Takeda Chem Ind Ltd | 受容体作動剤 |
| US7989461B2 (en) * | 2005-12-23 | 2011-08-02 | Amgen Inc. | Substituted quinazolinamine compounds for the treatment of cancer |
| WO2008067222A1 (en) | 2006-11-28 | 2008-06-05 | Kalypsys, Inc. | Heterocyclic modulators of tgr5 |
| WO2008067219A2 (en) | 2006-11-29 | 2008-06-05 | Kalypsys, Inc. | Quinazolinone modulators of tgr5 |
| WO2008097976A1 (en) | 2007-02-09 | 2008-08-14 | Kalypsys, Inc. | Heterocyclic modulators of tgr5 for treatment of disease |
| US20090105124A1 (en) | 2007-08-23 | 2009-04-23 | Kalypsys, Inc. | Heterocyclic modulators of tgr5 |
| US20110136788A1 (en) * | 2008-08-07 | 2011-06-09 | Minoru Maruyama | Therapeutic agent for irritable bowel syndrome |
| WO2010016846A1 (en) | 2008-08-08 | 2010-02-11 | Kalypsys, Inc. | Heterocyclic modulators of tgr5 for treatment of disease |
| US8309734B2 (en) | 2008-10-29 | 2012-11-13 | Hoffmann-La Roche Inc. | Substituted pyridines as GPBAR1 agonists |
| ES2774368T3 (es) | 2008-11-19 | 2020-07-20 | Intercept Pharmaceuticals Inc | Moduladores de TGR5 y métodos de uso de los mismos |
| CN102395567A (zh) | 2009-02-12 | 2012-03-28 | 埃克塞利希斯股份有限公司 | 在治疗糖尿病和肥胖症中用作的tgr5激动剂的三唑和咪唑衍生物 |
| CN102781922A (zh) | 2009-12-11 | 2012-11-14 | 埃克塞利希斯股份有限公司 | Tgr5激动剂 |
-
2012
- 2012-04-27 WO PCT/US2012/035327 patent/WO2012149236A1/en not_active Ceased
- 2012-04-27 TW TW101115262A patent/TW201247627A/zh unknown
- 2012-04-27 CN CN201280031836.7A patent/CN103619817A/zh active Pending
- 2012-04-27 US US14/113,593 patent/US9062028B2/en active Active
- 2012-04-27 JP JP2014508573A patent/JP2014518853A/ja active Pending
- 2012-04-27 EP EP12723982.0A patent/EP2702042A1/en not_active Withdrawn
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN1051038A (zh) * | 1989-10-20 | 1991-05-01 | 大塚制药株式会社 | 苯并杂环化合物 |
| CN1098406A (zh) * | 1993-04-13 | 1995-02-08 | 藤泽药品工业株式会社 | 新的苯甲酰胺衍生物及其制法和含有它们的药物组合物 |
| WO2010107768A1 (en) * | 2009-03-18 | 2010-09-23 | Schering Corporation | Bicyclic compounds as inhibitors of diacylglycerol acyltransferase |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110536886A (zh) * | 2017-03-22 | 2019-12-03 | 先正达参股股份有限公司 | 杀有害生物活性环丙基甲基酰胺衍生物 |
| CN114199812A (zh) * | 2021-12-28 | 2022-03-18 | 南通联亚药业有限公司 | 一种盐酸美金刚缓释制剂中盐酸美金刚的检测方法 |
Also Published As
| Publication number | Publication date |
|---|---|
| US9062028B2 (en) | 2015-06-23 |
| WO2012149236A1 (en) | 2012-11-01 |
| US20140080788A1 (en) | 2014-03-20 |
| EP2702042A1 (en) | 2014-03-05 |
| TW201247627A (en) | 2012-12-01 |
| JP2014518853A (ja) | 2014-08-07 |
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