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1. 发明专利

JP2011225580A 3,4-substituted piperidine derivative as renin inhibitor 有权
标题翻译： 3,4-取代的哌啶衍生物作为RININ抑制剂
公开(公告)号：JP2011225580A
公开(公告)日：2011-11-10
申请号：JP2011123057
申请日：2011-06-01
申请人： Merck Frosst Canada Ltd , Merck Sharp & Dohme Ltd , メルクシャープエンドドームリミテッド , メルクフロストカナダリミテツド
发明人： CHEN AUSTIN CHIH-YU , DUBE DANIEL , FOURNIER PIERRE-ANDRE , GRIMM ERICH L , LACOMBE PATRICK , LALIBERTE SEBASTIEN , MACDONALD DWIGHT , MACKAY D BRUCE , MCKAY DANIEL JAMES , WU TOM YAO-HSIANG , CAMPEAU LOUIS-CHARLES , SCOTT JEREMY PETER , BREMEYER NADINE
IPC分类号： A61K31/4545 , A61P3/10 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/00 , A61P13/12 , A61P15/08 , A61P15/10 , A61P25/22 , A61P25/28 , A61P27/02 , A61P27/06 , A61P43/00 , C07D401/04
CPC分类号： C07D401/14 , C07D401/04 , C07D417/14
摘要： PROBLEM TO BE SOLVED: To provide orally active renin inhibitors which are of long duration of action and active in indications beyond blood pressure regulation, which are of a non-peptidic nature and activates the tissular renin-chymase system leading to pathophysiologically altered local functions such as renal, cardiac, and vascular remodeling, atherosclerosis, and possibly restenosis.SOLUTION: A 3,4-substituted piperidinyl-based renin inhibitor compounds of the following formula bear oxopyridine at 4-position.
摘要翻译：要解决的问题：提供口服活性肾素抑制剂，其具有长期作用并且在血压调节之外具有非肽性质的活性，并且激活导致病理生理学改变的组织肾素 - 胃促胰酶系统局部功能如肾，心脏和血管重塑，动脉粥样硬化和可能的再狭窄。解决方案：下述式的3,4-取代哌啶基肾素抑制剂化合物在4-位含有氧代吡啶。版权所有（C）2012，JPO＆INPIT

2. 发明专利

JP2011225579A 3,4-substituted piperidine derivative as renin inhibitor 有权
标题翻译： 3,4-取代的哌啶衍生物作为RININ抑制剂
公开(公告)号：JP2011225579A
公开(公告)日：2011-11-10
申请号：JP2011123054
申请日：2011-06-01
申请人： Merck Frosst Canada Ltd , Merck Sharp & Dohme Ltd , メルクシャープエンドドームリミテッド , メルクフロストカナダリミテツド
发明人： CHEN AUSTIN CHIH-YU , DUBE DANIEL , FOURNIER PIERRE-ANDRE , GRIMM ERICH L , LACOMBE PATRICK , LALIBERTE SEBASTIEN , MACDONALD DWIGHT , MACKAY D BRUCE , MCKAY DANIEL JAMES , WU TOM YAO-HSIANG , CAMPEAU LOUIS-CHARLES , SCOTT JEREMY PETER , BREMEYER NADINE
IPC分类号： C07D401/04 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/506 , A61K31/5377 , A61P3/10 , A61P5/42 , A61P9/04 , A61P9/10 , A61P9/12 , A61P13/12 , A61P15/10 , A61P17/00 , A61P25/22 , A61P25/28 , A61P27/02 , A61P27/06 , A61P37/02 , A61P43/00 , C07D401/14
CPC分类号： C07D401/14 , C07D401/04 , C07D417/14
摘要： PROBLEM TO BE SOLVED: To provide new renin inhibitor compounds.SOLUTION: There are provided 3,4-substituted piperidinyl-based renin inhibitor compounds bearing at 4-position oxopyridine, having formula (I), and having the specific crystalline form. In addition, a process for preparing the compounds by the specific coupling and a pharmaceutical composition containing the compounds are provided. The compounds can be used in treating disease of cardiovascular events and renal insufficiency as renin inhibitors.
摘要翻译：要解决的问题：提供新的肾素抑制剂化合物。提供了具有式（I）的4-位氧代吡啶的3,4-取代的哌啶基肾素抑制剂化合物，并具有特定的结晶形式。此外，提供了通过特异性偶联制备化合物的方法和含有这些化合物的药物组合物。该化合物可用于治疗心血管事件和肾功能不全的疾病，作为肾素抑制剂。版权所有（C）2012，JPO＆INPIT

3. 发明专利

DOP2010000329A INHIBIDORES DE LA RENINA 未知
公开(公告)号：DOP2010000329A
公开(公告)日：2011-01-15
申请号：DO2010000329
申请日：2010-11-03
申请人： MERCK FROSST CANADA LTD , MERCK SHARP & DOHME
发明人： LACOMBE PATRICK , MACDONALD DWIGHT , CHEN AUSTIN CHIH-YU , FORUNIER PIERRE-ANDRE , DUBE DANIEL , GRIMM ERICH L , LALIBERTE SEBASTIEN , MACKAY D BRUCE , MCKAY DANIEL JAMES , WU TOM YAO-HSIANG , CAMPEAU LOUIS-CHARLES , SCOTT JEREMY PETER , BREMEYER NADINE
IPC分类号： C07D401/04 , C07D401/14 , C07D413/14 , C07D417/14
摘要： LA PRESENTE INVENCIÓN SE REFIERE A COMPUESTOS INHIBIDORES DE RENINA BASADOS EN PERIDINILO 3,4-SUBSTITUIDOS TENIENDO EN 4-POSICIONES OXOPIRIDINA Y CON LA FÓRMULA (L). LA INVENCIÓN SE REFIERE ADEMÁS A COMPOSICIONES FARMACÉUTICAS CONTENTIVAS DE DICHOS COMPUESTOS, ASÍ COMO A SU USO EN EL TRATAMIENTO DE ACONTECIMIENTOS CARDIOVASCULARES E INSUFICIENCIA RENAL.

4. 发明专利

PE03322011A1 COMPUESTOS DERIVADOS DE 4-(OXOPIRDIN-4-IL)-3-PIPERIDINCARBOXILAMINA COMO INHIBIDORES DE RENINA 未知
公开(公告)号：PE03322011A1
公开(公告)日：2011-06-22
申请号：PE0011692009
申请日：2009-10-05
申请人： MERCK FROSST CANADA LTD , MERCK SHARP & DOHME
发明人： CHEN AUSTIN CHIH-YU , DUBE DANIEL , FOURNIER PIERRE-ANDRE , GRIMM ERICH L , LACOMBE PATRICK , LALIBERTE SEBASTIEN , MACDONALD DWIGHT , MACKAY D BRUCE , MCKAY DANIEL JAMES , WU TOM YAO-HSIANG , CAMPEAU LOUIS-CHARLES , SCOTT JEREMY PETER , BREMEYER NADINE
IPC分类号： C07D401/04 , A61K31/4545 , A61P9/00 , C07D401/14 , C07D413/14 , C07D417/14
摘要： SE REFIERE A UN COMPUESTO DE FORMULA I DONDE R1 ES ALQUILO C1-C6, CICLOALQUILO C3-C6, ALQUENILO C2-C6, ENTRE OTROS; R2 Y R3 SON INDEPENDIENTEMENTE H, ALQUILO C1-C5, CICLOALQUILO C3-C8, ENTRE OTROS; W ES CICLOPROPILO OPCIONALMENTE SUSTITUIDO POR 1-5 ATOMOS DE FLUOR; X ES H, OH, -(ALQUILENO C1-C5)-, ENTRE OTROS; Z ES ALQUILENO C1-C2 OPCIONALMENTE SUSTITUIDO POR HALOGENO, ALQUILO C1-C3, CICLOALQUILO C3; Y ES CARBOCICLICO O HETEROCICLICO AMBOS 5-6 MIEMBROS DONDE EL HETEROCICLICO POSEE DE 1-3 HETEROATOMOS SELECCIONADOS ENTE N, O Y S; n1 ES 0-1. SON COMPUESTOS PREFERIDOS: trans-N-CICLOPROPIL-N-[(2,3-DICLOROFENIL)METIL]-4-(1-METIL-2-OXO-1,2-DIHIDRO-4-PIRIDINIL)-3-PIPERIDINACARBOXAMIDA; trans-N-[{5-CLORO-2-[3-(METILOXI)PROPIL]-4-PIRIDINIL}METIL]-N-CICLOPROPIL-4-(1-METIL-2-OXO-1,2-DIHIDRO-4-PIRIDINIL)-3-PIPERIDINACARBOXAMIDA; trans-N-({2-CLORO-5-[3-(METILOXI)PROPIL]FENIL}METIL)-N-CICLOPROPIL-4-(1-METIL-2-OXO-1,2-DIHIDRO-4-PIRIDINIL)-3-PIPERIDINACARBOXAMIDA; ENTRE OTROS. SE REFIERE TAMBIEN A UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHO COMPUESTO ES UN INHIBIDOR DE RENINA UTIL EN EL TRATAMIENTO DE LA HIPERTENSION, INSUFICIENCIA CARDIACA CONGESTIVA, HIPERTENSION PULMONAR, ENTRE OTRAS

5. 发明专利

PE20110332A1 COMPUESTOS DERIVADOS DE 4-(OXOPIRDIN-4-IL)-3-PIPERIDINCARBOXILAMINA COMO INHIBIDORES DE RENINA 未知
公开(公告)号：PE20110332A1
公开(公告)日：2011-06-22
申请号：PE2009001169
申请日：2009-10-05
申请人： MERCK FROSST CANADA LTD , MERCK SHARP & DOHME
发明人： CHEN AUSTIN CHIH-YU , DUBE DANIEL , FOURNIER PIERRE-ANDRE , GRIMM ERICH L , LACOMBE PATRICK , LALIBERTE SEBASTIEN , MACDONALD DWIGHT , MACKAY D BRUCE , MCKAY DANIEL JAMES , WU TOM YAO-HSIANG , CAMPEAU LOUIS-CHARLES , SCOTT JEREMY PETER , BREMEYER NADINE
IPC分类号： C07D401/04 , A61K31/4545 , A61P9/00 , C07D401/14 , C07D413/14 , C07D417/14
摘要： SE REFIERE A UN COMPUESTO DE FORMULA I DONDE R1 ES ALQUILO C1-C6, CICLOALQUILO C3-C6, ALQUENILO C2-C6, ENTRE OTROS; R2 Y R3 SON INDEPENDIENTEMENTE H, ALQUILO C1-C5, CICLOALQUILO C3-C8, ENTRE OTROS; W ES CICLOPROPILO OPCIONALMENTE SUSTITUIDO POR 1-5 ATOMOS DE FLUOR; X ES H, OH, -(ALQUILENO C1-C5)-, ENTRE OTROS; Z ES ALQUILENO C1-C2 OPCIONALMENTE SUSTITUIDO POR HALOGENO, ALQUILO C1-C3, CICLOALQUILO C3; Y ES CARBOCICLICO O HETEROCICLICO AMBOS 5-6 MIEMBROS DONDE EL HETEROCICLICO POSEE DE 1-3 HETEROATOMOS SELECCIONADOS ENTE N, O Y S; n1 ES 0-1. SON COMPUESTOS PREFERIDOS: trans-N-CICLOPROPIL-N-[(2,3-DICLOROFENIL)METIL]-4-(1-METIL-2-OXO-1,2-DIHIDRO-4-PIRIDINIL)-3-PIPERIDINACARBOXAMIDA; trans-N-[{5-CLORO-2-[3-(METILOXI)PROPIL]-4-PIRIDINIL}METIL]-N-CICLOPROPIL-4-(1-METIL-2-OXO-1,2-DIHIDRO-4-PIRIDINIL)-3-PIPERIDINACARBOXAMIDA; trans-N-({2-CLORO-5-[3-(METILOXI)PROPIL]FENIL}METIL)-N-CICLOPROPIL-4-(1-METIL-2-OXO-1,2-DIHIDRO-4-PIRIDINIL)-3-PIPERIDINACARBOXAMIDA; ENTRE OTROS. SE REFIERE TAMBIEN A UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHO COMPUESTO ES UN INHIBIDOR DE RENINA UTIL EN EL TRATAMIENTO DE LA HIPERTENSION, INSUFICIENCIA CARDIACA CONGESTIVA, HIPERTENSION PULMONAR, ENTRE OTRAS

6. 发明专利

CR11809A DERIVADOS DE PIPERIDINA 3,4-SUSTITUIDA COMO INHIBIDORES DE RENINA 未知
公开(公告)号：CR11809A
公开(公告)日：2011-01-10
申请号：CR11809
申请日：2010-11-24
申请人： MERCK FROSST CANADA LTD , MERCK SHARP & DOHME , PFIZER LTD
发明人： CHEN AUSTIN CHIH-YU , DUBE DANIEL , FOURNIER PIERRE-ANDRE , GRIMM ERICH L , LACOMBE PATRICK , LALIBERTE SEBASTIEN , MACDONALD DWIGHT , MACKAY D BRUCE , MCKAY DANIEL JAMES , WU TOM YAO-HSIANG , CAMPEAU LOUIS-CHARLES , SCOTT JEREMY PETER , BREMEYER NADINE
IPC分类号： C07D401/04 , A61K31/4545 , A61P9/00 , C07D401/14 , C07D413/14 , C07D417/14
摘要： La presente invención se refiere a compuestos inhibidores de la renina basados en amino amida que soporta piridina, y a su uso en el tratamiento de acontecimientos cardiovasculares e insuficiencia renal.

7. 发明专利

CA2722734A1 3, 4 - SUBSTITUTED PIPERIDINE DERIVATIVES AS RENIN INHIBITORS 未知
公开(公告)号：CA2722734A1
公开(公告)日：2009-11-12
申请号：CA2722734
申请日：2009-05-04
申请人： MERCK FROSST CANADA LTD , MERCK SHARP & DOHME
发明人： SCOTT JEREMY PETER , BREMEYER NADINE , CHEN AUSTIN CHIH-YU , DUBE DANIEL , FOURNIER PIERRE-ANDRE , GRIMM ERICH L , LACOMBE PATRICK , LALIBERTE SEBASTIEN , MACDONALD DWIGHT , MACKAY D BRUCE , MCKAY DANIEL JAMES , WU TOM YAO-HSIANG , CAMPEAU LOUIS-CHARLES
IPC分类号： C07D401/04 , A61K31/4545 , A61P9/00 , C07D401/14 , C07D413/14 , C07D417/14
摘要： The present invention relates to 3,4-substituted piperidinyl-based renin inhibitor compounds bearing at 4-position oxopyridine and having the formula (I). The invention further relates to pharmaceutical compositions containing said compounds, as well as their use in treating cardiovascular events and renal insufficiency.

8. 发明专利

CA2722734C 3,4-SUBSTITUTED PIPERIDINE DERIVATIVES AS RENIN INHIBITORS 未知
公开(公告)号：CA2722734C
公开(公告)日：2013-11-05
申请号：CA2722734
申请日：2009-05-04
申请人： MERCK FROSST CANADA LTD , MERCK SHARP & DOHME
发明人： SCOTT JEREMY PETER , BREMEYER NADINE , CHEN AUSTIN CHIH-YU , DUBE DANIEL , FOURNIER PIERRE-ANDRE , GRIMM ERICH L , LACOMBE PATRICK , LALIBERTE SEBASTIEN , MACDONALD DWIGHT , MACKAY D BRUCE , MCKAY DANIEL JAMES , WU TOM YAO-HSIANG , CAMPEAU LOUIS-CHARLES
IPC分类号： C07D401/04 , A61K31/4545 , A61P9/00 , C07D401/14 , C07D413/14 , C07D417/14
摘要： The present invention relates to 3,4-substituted piperidinyl-based renin inhibitor compounds bearing at 4-position oxopyridine and having the formula (I). The invention further relates to pharmaceutical compositions containing said compounds, as well as their use in treating cardiovascular events and renal insufficiency.

9. 发明专利

NZ589019A 3, 4 - SUBSTITUTED PIPERIDINE DERIVATIVES AS RENIN INHIBITORS 未知
公开(公告)号：NZ589019A
公开(公告)日：2012-10-26
申请号：NZ58901909
申请日：2009-05-04
申请人： MERCK FROSST CANADA LTD , MERCK SHARP & DOHME
发明人： CHEN AUSTIN CHIH-YU , DUBE DANIEL , FOURNIER PIERRE-ANDRE , GRIMM ERICH L , LACOMBE PATRICK , LALIBERTE SEBASTIEN , MACDONALD DWIGHT , MACKAY D
IPC分类号： C07D401/04 , A61K31/4545 , A61P9/00 , C07D401/14 , C07D413/14 , C07D417/14
摘要： Disclosed are trans-4-(2-oxo-1,2-dihydro-pyridin-4-yl)-3-piperidinecarboxamide derivatives as represented by the general formula (I), wherein the substituents are as defined in the specification. Representative compounds include trans-N-[2-chloro-3,5-bis(3-methoxypropyl)benzyl]-N-cyclopropyl-4-(1-methyl-2-oxo-1,2-dihydro-pyridin-4-yl)-3-piperidinecarboxamide, trans-N-{ 3-bromo-5-[3-(difluoromethoxy)propyl]-4-methylbenzyl} -N-cyclopropyl-4-(1-methyl-2-oxo-1,2-dihydro-4-pyridinyl)-3-piperidinecarboxamide, trans-N-({ 3-bromo-4-methyl-5-[3-(methyloxy)propyl]phenyl} methyl)-N-cyclopropyl-4-(1-methyl-2-oxo-1,2-dihydro-4-pyridinyl)-3-piperidinecarboxamide, trans-N-Cyclopropyl-N-( { 2,3-dimethyl-5-[3-(methyloxy)propyl]phenyl} methyl)-4-(1-methyl-2-oxo-1,2-dihydro-4-pyridinyl)-3-piperidinecarboxamide, trans-N-Cyclopropyl-N-({ 4-fluoro-1-[(3-fluorophenyl)methyl]-1H-indol-3 -yl]methyl} -4-(1-methyl-2-oxo-1,2-dihydro-4-pyridinyl)-3-piperidinecarboxamide and trans-N-cyclopropyl-N-({ 2,3-dichloro-5-[3-(methyloxy)propyl] phenyl} methyl)-4-(1-methyl-2-oxo-1,2-dihydro-4-pyridinyl)-3-piperidinecarboxamide. Further disclosed is a pharmaceutical composition which comprises an effective amount of a compound as defined above, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, for the treatment or prophylaxis of diseases which are related to hypertension, congestive heart failure, pulmonary hypertension, renal insufficiency, renal ischemia, renal failure, renal fibrosis, cardiac insufficiency, cardiac hypertrophy, cardiac fibrosis, myocardial ischemia, cardiomyopathy, glomerulonephritis, renal colic, complications resulting from diabetes, glaucoma, elevated intra-ocular pressure, atherosclerosis, restenosis post angioplasty, complications following vascular or cardiac surgery, erectile dysfunction, hyperaldosteronism, lung fibrosis, scleroderma, anxiety, cognitive disorders, complications of treatments with immunosuppressive agents, and other diseases known to be related to the renin-angiotensin system.

10. 发明专利

TN2010000490A1 未知
公开(公告)号：TN2010000490A1
公开(公告)日：2012-05-24
申请号：TN2010000490
申请日：2010-10-21
申请人： MERCK FROSST CANADA LTD , MERCK SHARP & DOHME
发明人： CHEN AUSTIN CHIH-YU , DUBE DANIEL , FOURNIER PIERRE-ANDRE , GRIMM ERICH L , LACOMBE PATRICK , LALIBERTE SEBASTIEN , MACDONALD DWIGHT , MACKAY D BRUCE , MCKAY DANIEL JAMES , WU TOM YAO-HSIANG , CAMPEAU LOUIS-CHARLES , SCOTT JEREMY PETER , BREM
IPC分类号： A61K31/4545 , A61P9/00 , C07D401/04 , C07D401/14 , C07D413/14 , C07D417/14

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