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31. 发明专利

DE60312520D1 未知
公开(公告)号：DE60312520D1
公开(公告)日：2007-04-26
申请号：DE60312520
申请日：2003-06-23
申请人： MERCK FROSST CANADA LTD
发明人： DESCHENES DENIS , DUBE DANIEL , DUBE LAURENCE , GALLANT MICHEL , GIRARD YVES , LACOMBE PATRICK , MACDONALD DWIGHT
IPC分类号： C07D215/04 , A61K31/4709 , A61P29/00 , C07D215/12 , C07D401/04 , C07D401/10 , C07D403/10 , C07D407/10 , C07D409/10 , C07D413/10 , C07D413/14 , C07D417/10 , C07D471/02 , C07D471/04 , C07F7/08 , C07F9/60
摘要： 8-(biaryl) quinolines wherein the bi-aryl group at the 8-position is in a meta relationship to the quinoline group, are PDE4 inhibitors useful in the treatment of asthma, chronic bronchitis, chronic obstructive pulmonary disease, eosinophilic granuloma, psoriasis and other benign or malignant proliferative skin diseases, endotoxic shock, laminitis in horses, colic in horses, septic shock, ulcerative colitis, Crohn's disease, reperfusion injury of the myocardium and brain, inflammatory arthritis, chronic glomerulonephritis, atopic dermatitis, urticaria, adult respiratory distress syndrome, chronic obstructive pulmonary disease in animals, diabetes insipidus, allergic rhinitis, allergic conjunctivitis, vernal conjunctivitis, arterial restenosis, ortherosclerosis, atherosclerosis, neurogenic inflammation, pain, cough, rheumatoid arthritis, ankylosing spondylitis, transplant rejection, graft versus host disease, hypersecretion of gastric acid, bacterial, fungal induced sepsis, viral induced sepsis, fungal induced septic shock, viral induced septic shock, inflammation-mediated chronic tissue degeneration, cytokine-mediated chronic tissue degeneration, osteoarthritis, cancer, cachexia, muscle wasting, depression, memory impairment, tumour growth, or cancerous invasion of normal tissues. In another aspect, the present invention is directed to a method of enhancing cognition in a healthy subject comprising administering a safe cognition enhancing amount of phosphodiesterase-4 inhibitor. In particular, this invention is directed to a method of enhancing memory, learning, retention, recall, awareness and judgement in health subjects comprising administering a safe and cognition enhancing amount of a phosphodiesterase-4 inhibitor.

33. 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

34. 发明专利

AU2006272348B2 Renin inhibitors 未知
公开(公告)号：AU2006272348B2
公开(公告)日：2011-06-16
申请号：AU2006272348
申请日：2006-07-20
申请人： MERCK FROSST CANADA LTD
发明人： CHEN AUSTIN C , POWELL DAVID A , DUBE DANIEL , MACDONALD DWIGHT , LACOMBE PATRICK , GRIMM ERICH L , MCKAY DANIEL , DUBE LAURENCE , BAYLY CHRISTOPHER I , GALLANT MICHEL
IPC分类号： C07C237/20 , C07C317/10 , C07D211/40 , C07D215/12 , C07D215/14 , C07D401/06 , C07D413/12

35. 发明专利

SV2010003723A DERIVADOS DE PIPERIDINA 3,4-SUSTITUIDA COMO INHIBIDORES DE RENINA 未知
公开(公告)号：SV2010003723A
公开(公告)日：2011-01-24
申请号：SV2010003723
申请日：2010-11-04
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 , LACOMBRE PATRICK , LALIBERTE SEBASTIEN , MACDONALD DWIGHT , MACKAY D BRUCE , MCKY DANIEL JAMES , WU TOM YAO-HSIANG , CAMPEUA LOUIS-CHARLES , SCOTT JEREMY PETER , BREMEYER NADINE
IPC分类号： A61K31/4545 , A61P9/00 , C07D401/04 , C07D401/14 , C07D413/14 , C07D417/14
摘要： COMPUESTOS INHIBIDORES DE RENINA BASADAS EN PIPERIDINILO 3,4-SUSTITUIDO QUE TIENEN OXOPIRIDINA EN LA POSICIÓN 4 Y PRESENTAN LA FORMULA (I). LA INVENCIÓN, ASIMISMO, SE REFIERE A COMPOSICIONES FARMACÉUTICAS QUE CONTIENEN DICHOS COMPUESTOS, ASÍ COMO A SU USO EN EL TRATAMIENTO DE EPISODIOS CARDIOVASCULARES E INSUFICIENCIA RENAL

36. 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.

37. 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.

38. 发明专利

CA2696689A1 RENIN INHIBITORS 未知
公开(公告)号：CA2696689A1
公开(公告)日：2009-02-26
申请号：CA2696689
申请日：2008-08-18
申请人： MERCK FROSST CANADA LTD
发明人： JUTEAU HELENE , GALLANT MICHEL , DUBE DANIEL , ROY PATRICK , ASPIOTIS RENEE , FORTIN REJEAN , LACOMBE PATRICK , MCKAY DANIEL J , WU TOM YAO-HSIANG
IPC分类号： C07C217/54 , A61K31/137 , A61K31/16 , A61K31/21 , A61K31/277 , A61K31/44 , C07C233/00 , C07C237/00 , C07C255/00 , C07C271/00 , C07D213/04
摘要： The present invention relates to biphenyl compounds of formula (I). These compounds are renin inhibitors of a non- peptidic nature and of low molecular weight. The invention further relates to a pharmaceutical composition containing said compounds, as well as their use and method of treatment of cardiovascular events and renal insufficiency.

39. 发明专利

CA2688057A1 NOVEL CASE OF RENIN INHIBITORS 未知
公开(公告)号：CA2688057A1
公开(公告)日：2008-11-27
申请号：CA2688057
申请日：2008-05-23
申请人： MERCK FROSST CANADA LTD
发明人： LALIBERTE SEBASTIEN , ROY PATRICK , ASPIOTIS RENEE , GALLANT MICHEL , DUBE DANIEL , WU TOM YAO-HSIANG , CHEN AUSTIN , JUTEAU HELENE , GRIMM ERICH L
IPC分类号： C07D211/60 , A61K31/451 , A61K31/4523 , A61K31/5377 , A61P9/00 , A61P13/10 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to piperidine-based renin inhibitor compoun ds having carboxylate or carboxylic acid terminal groups. The disclosed low molecular weight, orally active renin inhibitors are of non-peptide nature a nd have long duration of action. The compounds can be used in the treatment of cardiovascular events and renal insufficiency.

40. 发明专利

AU2003243870B2 8-(biaryl) quinoline PDE4 inhibitors 未知
公开(公告)号：AU2003243870B2
公开(公告)日：2008-11-20
申请号：AU2003243870
申请日：2003-06-23
申请人： MERCK FROSST CANADA LTD
发明人： DESCHENES DENIS , LACOMBE PATRICK , DUBE LAURENCE , DUBE DANIEL , MACDONALD DWIGHT , GIRARD YVES , GALLANT MICHEL
IPC分类号： C07D215/04 , A61P29/00 , C07D215/12 , C07D401/04 , C07D401/10 , C07D403/10 , C07D407/10 , C07D409/10 , C07D413/10 , C07D413/14 , C07D417/10 , C07D471/02 , C07D471/04 , C07F7/08 , C07F9/60
摘要： 8-(biaryl) quinolines wherein the bi-aryl group at the 8-position is in a meta relationship to the quinoline group, are PDE4 inhibitors useful in the treatment of asthma, chronic bronchitis, chronic obstructive pulmonary disease, eosinophilic granuloma, psoriasis and other benign or malignant proliferative skin diseases, endotoxic shock, laminitis in horses, colic in horses, septic shock, ulcerative colitis, Crohn's disease, reperfusion injury of the myocardium and brain, inflammatory arthritis, chronic glomerulonephritis, atopic dermatitis, urticaria, adult respiratory distress syndrome, chronic obstructive pulmonary disease in animals, diabetes insipidus, allergic rhinitis, allergic conjunctivitis, vernal conjunctivitis, arterial restenosis, ortherosclerosis, atherosclerosis, neurogenic inflammation, pain, cough, rheumatoid arthritis, ankylosing spondylitis, transplant rejection, graft versus host disease, hypersecretion of gastric acid, bacterial, fungal induced sepsis, viral induced sepsis, fungal induced septic shock, viral induced septic shock, inflammation-mediated chronic tissue degeneration, cytokine-mediated chronic tissue degeneration, osteoarthritis, cancer, cachexia, muscle wasting, depression, memory impairment, tumour growth, or cancerous invasion of normal tissues. In another aspect, the present invention is directed to a method of enhancing cognition in a healthy subject comprising administering a safe cognition enhancing amount of phosphodiesterase-4 inhibitor. In particular, this invention is directed to a method of enhancing memory, learning, retention, recall, awareness and judgement in health subjects comprising administering a safe and cognition enhancing amount of a phosphodiesterase-4 inhibitor.

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