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21. 发明专利

GEP20053626B Substituted 8-Arylquinoline Phosphodiesterase-4 Inhibitors, Pharmaceutical Composition Containing Them and Use Thereof 未知
公开(公告)号：GEP20053626B
公开(公告)日：2005-10-10
申请号：GEAP2000004903
申请日：2000-12-20
申请人： MERCK FROSST CANADA LTD
发明人： DESCHENES DENIS , DUBE DANIEL , GALLANT MICHEL , GIRARD YVES , LACOMBE PATRICK , MACDONALD DWIGHT , MASTRACCHIO ANTHONY , PERRIER HELENE
IPC分类号： A61K31/47 , A61K31/4709 , A61K45/00 , A61P1/04 , A61P7/12 , A61P9/00 , A61P11/00 , A61P11/06 , A61P11/16 , A61P13/12 , A61P17/00 , A61P17/04 , A61P17/06 , A61P19/02 , A61P19/10 , A61P37/08 , C07D215/12 , C07D215/14 , C07D401/10 , C07D401/14 , C07D405/12 , C07D409/10 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/12 , C07D417/14
摘要： 1. Technical Result Strengthening chemical properties with minimal side-effects. 2. Essence A compound of formula I (R1, R2, R3, S1, S2, S3 and A are provided in the description), pharmaceutically acceptable salt thereof, pharmaceutical composition containing them and use thereof as phosphodiesterase inhibitor. 3. Field of Application Medicine.

23. 发明专利

MX2010012067A DERIVADOS DE 3,4-PIPERIDINA SUSTITUIDA COMO INHIBIDORES DE LA RENINA. 未知
公开(公告)号：MX2010012067A
公开(公告)日：2010-12-06
申请号：MX2010012067
申请日：2009-05-04
申请人： MERCK FROSST CANADA LTD
发明人： DUBE DANIEL , LACOMBE PATRICK , MACDONALD DWIGHT , GRIMM ERICH L , LALIBERTE SEBASTIEN , CHEN AUSTIN CHIH-YU , FOURNIER PIERRE-ANDRE , 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 3,4-piperidinilo sustituido que portan en la posición 4 oxopiridina y que tienen la fórmula (I); (ver fórmulas (I)) la invención se refiere adicionalmente a composiciones farmacéuticas que contienen dichos compuestos, así como su uso en el tratamiento de acontecimientos cardiovasculares e insuficiencia renal.

24. 发明专利

MY138681A 4-OXO-1-(3-SUBSTITUTED PHENYL-1,4-DIHYDRO-1,8-NAPHTHYRIDINE-3-CARBOXAMIDE PHOSPHODIESTERASE-4 INHIBITORS 未知
公开(公告)号：MY138681A
公开(公告)日：2009-07-31
申请号：MYPI20041394
申请日：2004-04-15
申请人： MERCK FROSST CANADA LTD
发明人： DUBE DANIEL , GALLANT MICHEL , LACOMBE PATRICK , ASPIOTIS RENEE , DUBE LAURENCE , MACDONALD DWIGHT
摘要： COMPOUNDS REPRESENTED BY FORMULA (I): OR A PHARMACEUTICAL ACCEPTABLE SALT THEREOF, ARE PHOSPHODIESTERRASE 4 INHIBITORS USEFUL IN THE TREATMENT OF ASTHMA AND INFLAMMATION AND USEFUL FOR THE ENCHANCEMENT OF COGNITION.

25. 发明专利

UA82208C2 未知
公开(公告)号：UA82208C2
公开(公告)日：2008-03-25
申请号：UA2005006089
申请日：2003-11-19
申请人： MERCK FROSST CANADA LTD
发明人： DUBE DANIEL , GALLANT MICHEL , LACOMBE PATRICK , ASPIOTIS RENEE , DUBE LAURENCE , GIRARD YVES , MACDONALD DWIGHT
IPC分类号： A61P25/00 , A61K31/4375 , A61K31/4745 , A61K31/506 , C07D221/00 , C07D471/02 , C07D471/04
摘要： Соединения, представленныеформулой (І), илиихфармацевтическиприемлемыесоли, которыеявляютсяингибиторамифосфодиэстеразы-4, пригоднымидлялеченияастмыи воспаления, атакжедляулучшенияпознавательнойспособности.

26. 发明专利

DE60312520T2 未知
公开(公告)号：DE60312520T2
公开(公告)日：2007-11-22
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.

27. 发明专利

ES2282667T3 INHIBIDORES DE PDE4 8-(BIARIL)QUINOLINAS. 未知
公开(公告)号：ES2282667T3
公开(公告)日：2007-10-16
申请号：ES03760540
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
IPC分类号： C07D215/04 , A61K31/47 , A61K31/4709 , A61K31/497 , 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： Un compuesto representado por la fórmula (I): o una sal farmacéuticamente aceptable del mismo, en el que A es C o N; X es fenilo, piridilo, pirazinilo, tiofenilo, quinolinilo, benzofuranilo, oxadiazolilo, diazolilpiridinilo, imidazolilpiridinilo, oxadiazolilfenilo, o benzodioxolilo; R1 es hidrógeno, halógeno; o un grupo -alquilo C1-6, -cicloalquilo C3-6, o alquenilo C1-6, en los que cualquiera de los grupos está sustituido opcionalmente con 1-6 sustituyentes; en los que cada sustituyente es de forma independiente halógeno, -OH, -CN, o -SO2-alquilo C1-6; R2, y R3 son cada uno de forma independiente hidrógeno, halógeno, hidroxilo, -CN, -NO2; o -alquilo C1-6, -alquenilo C2-6, -alquil C1-6(alquenilo C2-6)2, -alquil C0-4(cicloalquilo C3-6)2, -alquil C0-6-N(alquilo C0-6)2, -alquil C0-4-O-alquilo C1-6, -alquil C1-6-fenilo, -alquil C0-6-SO2-alquilo C1-6, -alquil C0-6-C(O)-alquilo C0-6, -alquil C0-6-C(O)-alquil C0-6-fenilo, -alquil C0-6-C(O)-alquil C0-4-O-alquilo C0-6, -alquil C0-6-C(O)-alquil C0-6-O-alquil C0-6-O-C0-6-C(O)-alquilo C0-6, alquenil C2-6-C(O)-alquil C0-4-O-alquilo C0-6, -alquil C0-4- cicloalquil C3-6-alquil C0-6-C(O)-alquilo C0-6, alquil C0-4-cicloalquil C3-6-alquil C0-6-C(O)-alquil C0-6-N(alquilo C0-6)2, -alquil C0-4-cicloalquil C3-6-alquil C0-6-C(O)-alquil C0-4-O-alquilo C0-6, - alquil C2-6-C(O)-alquil C0-4-N(alquil C0-6)-piridilo, -alquil C0-6- C (O)-alquil C0-4- N (alquilo C0-4)2, -alquil C0-6- C (O)-alquil C0-4- N (alquil C0-4)- cicloalquilo C3-6, alquenil C2-6- C(O)-alquil C0-4-N(alquil C0-4)- cicloalquilo C3-6, -SO2-alquil C0-6-fenilo, -SO2-alquil C0-6-(-alquil C0-6-fenil)(-alquil C0-6fenilo), -alquil C0-4- SO2-alquil C0-4- cicloalquil C3-6-alquil C0-4-C(O)-alquil C0-4-O-alquilo C0-4, -S(O)-alquilo C0-6, -P(O)(O-alquil C0-4)(O-alquil C0-4), alquenil C2-6-C(O)-alquil C0-4-N(alquil C0-4)-piridilo, -S-alquilo C1-6, -alquil C0-6-N(alquil C0-6)-C(O)-alquilo C0-6, -alquil C0-6-N(alquil C0-6)-C(O)-N(alquilo C0-6)2, -alquil C0-4-S-alquil C1-4-oxadiazolil(alquilo C0-4), -alquil C0-4-C(O)-alquil C0-4-fenilo, -alquil C0-4-O-alquil C0-4-fenilo, -alquil C0-4-cicloalquil C3-6-alquil C0-4-tetrazolilo, -SO2-N(alquilo C0-4)2, -alquil C0-4-S-alquil C0-4-tiadiazolil(alquilo C0-4), -alquil C0-4-S-alquil C0-4-diazolil(alquilo C0-4), -alquil C0-4-S-alquil C1-4-Si(alquilo C0-4)3, -alquil C0-4-S-alquil C0-4-fenil(alquilo C0-4), -alquil C0-4-S-alquil C0-4-C(O)-alquil C0-4-O-alquilo C0-4, o -alquil C0-4-S-alquil C0-4-cicloalquil C3-6-alquil C0-4-C(O)-alquil C0-4-O-alquilo C0-4, en los que cualquiera de los grupos alquilo, cicloalquilo, alquenilo, fenilo, o piridilo están cada uno opcionalmente sustituidos con 1-9 grupos que son de forma independiente halógeno, hidroxilo, -alquil C0-4-O-alquilo C1-6, o -alquil C0-4-S-alquilo C1-6; opcionalmente, R2 forma =O con un enlace adyacente; R4 es hidrógeno, o halógeno; y cualquier nitrógeno del anillo forma opcionalmente N-óxido o N-cloruro.

28. 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.

29. 发明专利

AU2003283167B2 4-oxo-1-(3-substituted phenyl-1,4-dihydro-1,8-naphthyridine-3-carboxamide phosphodiesterase-4 inhibitors 未知
公开(公告)号：AU2003283167B2
公开(公告)日：2009-01-08
申请号：AU2003283167
申请日：2003-11-19
申请人： MERCK FROSST CANADA LTD
发明人： DUBE DANIEL , LACOMBE PATRICK , DUBE LAURENCE , MACDONALD DWIGHT , GALLANT MICHEL , ASPIOTIS RENEE , GIRARD YVES
IPC分类号： C07D471/04 , A61K31/4375 , A61K31/4745 , A61K31/506 , A61P25/00 , C07D221/00 , C07D471/02
摘要： Compounds represented by Formula (I): or a pharmaceutically acceptable salt thereof, are phosphodiesterrase 4 inhibitors useful in the treatment of asthma and inflammation and useful for the enhancement of cognition.

30. 发明专利

AT402175T 未知
公开(公告)号：AT402175T
公开(公告)日：2008-08-15
申请号：AT03775029
申请日：2003-11-19
申请人： MERCK FROSST CANADA LTD
发明人： DUBE DANIEL , GALLANT MICHEL , LACOMBE PATRICK , ASPIOTIS RENEE , DUBE LAURENCE , GIRARD YVES , MACDONALD DWIGHT
IPC分类号： C07D471/04 , A61K31/4375 , A61K31/4745 , A61K31/506 , A61P25/00 , C07D221/00 , C07D471/02
摘要： Compounds represented by Formula (I): or a pharmaceutically acceptable salt thereof, are phosphodiesterrase 4 inhibitors useful in the treatment of asthma and inflammation and useful for the enhancement of cognition.

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