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82. 发明专利

BRPI0811842A2 未知
公开(公告)号：BRPI0811842A2
公开(公告)日：2014-11-18
申请号：BRPI0811842
申请日：2008-05-22
申请人： MERCK & CO INC
发明人： BRESLIN MICHAEL J , COLEMAN PAUL J , COX CHRISTOPHER D , SCHREIER JOHN D
IPC分类号： C07D401/12 , A61K31/4525 , A61K31/4535 , A61K31/454 , A61K31/506 , A61P25/00 , C07D401/14 , C07D413/14 , C07D417/14
摘要： The present invention is directed to pyridyl piperidine compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

83. 发明专利

BRPI0719361A2 未知
公开(公告)号：BRPI0719361A2
公开(公告)日：2014-02-04
申请号：BRPI0719361
申请日：2007-11-30
申请人： MERCK & CO INC
发明人： BERGMAN JEFFREY M , BRESLIN MICHAEL J , COLEMAN PAUL J , COX CHRISTOPHER D , MERCER SWATI P , ROECKER ANTHONY J
IPC分类号： C07D401/14 , A61K31/551 , A61P3/04 , A61P25/20 , C07D403/14 , C07D413/14 , C07D471/04 , C07D487/04 , C07D491/048 , C07D491/052 , C07D495/04
摘要： The present invention is directed to substituted diazepan compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

84. 发明专利

CA2670892C SUBSTITUTED DIAZEPAN COMPOUNDS AS OREXIN RECEPTOR ANTAGONISTS 未知
公开(公告)号：CA2670892C
公开(公告)日：2013-08-13
申请号：CA2670892
申请日：2007-11-30
申请人： MERCK & CO INC
发明人： BERGMAN JEFFREY M , BRESLIN MICHAEL J , COLEMAN PAUL J , COX CHRISTOPHER D , MERCER SWATI P , ROECKER ANTHONY J
IPC分类号： C07D403/14 , A61K31/551 , A61P3/04 , A61P25/20 , C07D401/14 , C07D413/14 , C07D471/04 , C07D487/04 , C07D491/048 , C07D495/04
摘要： The present invention is directed to substituted diazepan compounds which are antagonists of orexin receptors, and which may be used in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds. These compositions may be used in the prevention or treatment of such diseases in which orexin receptors are involved.

85. 发明专利

CY1107746T1 ΑΝΤΑΓΩΝΙΣΤΕΣ ΤΟΥ ΑΛΦΑ V ΙΝΤΕΓΚΡΙΝΙΚΟΥ ΥΠΟΔΟΧΕΑ 未知
公开(公告)号：CY1107746T1
公开(公告)日：2013-04-18
申请号：CY071101242
申请日：2007-09-27
申请人： MERCK & CO INC
发明人： COLEMAN PAUL J , DUGGAN MARK E , HALCZENKO WASYL , HARTMAN GEORGE D , HUTCHINSON JOHN H , MEISSNER ROBERTS , PATANE MICHAEL A , PERKINS JAMES J , WANG JIABING , BRESLIN MICHAEL J
IPC分类号： A61K31/506 , A61K31/437 , A61K31/4375 , A61K31/4709 , A61K31/498 , A61K31/501 , A61K31/505 , A61K31/536 , A61K31/55 , A61P9/00 , A61P9/08 , A61P9/10 , A61P17/00 , A61P19/08 , A61P19/10 , A61P27/02 , A61P29/00 , A61P31/12 , A61P35/00 , A61P35/04 , A61P43/00 , C07D213/02 , C07D221/00 , C07D223/14 , C07D239/24 , C07D239/48 , C07D241/36 , C07D265/28 , C07D401/06 , C07D471/02 , C07D471/04 , C07D519/00
摘要： Ηπαρούσαεφεύρεσηαναφέρεταισενέαπαράγωγατουεννεανοϊκούοξέος, τηνσύνθεσηαυτώνκαιτηνχρήσηαυτώνσανανταγωνιστέςτουαλφα V ιντεγκρινικούυποδοχέα. Ειδικότερα, οιενώσειςτηςπαρούσαςεφεύρεσηςείναιανταγωνιστέςτωνυποδοχέωντωνιντεγκρινώναλφα V βητα3 καιαλφα V βητα5 καιείναιχρήσιμεςγιατηναναστολήτηςοστικήςεπαναρρόφησης, τηνθεραπείακαιτηνπρόληψητηςοστεοπόρωσης, καιαναστολήτηςαγγειακήςεπαναστένωσης, διαβητικήςνεφροπάθειας, κηλιδώδουςεκφυλισμού, αγγειογένεσης, αρτηριοσκλήρυνσης, φλεγμονής, φλεγμονώδουςαρθρίτιδας, ιικήςασθένειας, καρκίνου, καιμεταστατικήςαύξησηςόγκου.

86. 发明专利

MX2009012579A ANTAGONISTAS PIRIDIL PIPERIDINA DEL RECEPTOR DE OREXINA. 未知
公开(公告)号：MX2009012579A
公开(公告)日：2009-12-08
申请号：MX2009012579
申请日：2008-05-22
申请人： MERCK & CO INC
发明人： BRESLIN MICHAEL J , COLEMAN PAUL J , COX CHRISTOPHER D , SCHREIER JOHN D
IPC分类号： C07D401/12 , A61K31/4525 , A61K31/4535 , A61K31/454 , A61K31/506 , A61P25/00 , C07D401/14 , C07D413/14 , C07D417/14
摘要： La presente invención se refiere a compuestos de piridil piperidina que son antagonistas de los receptores de orexina y que son útiles en el tratamiento o prevención de trastornos y enfermedades neurológicas y psiquiátricas en las que están implicados los receptores de orexina. La invención también se refiere a composiciones farmacéuticas que comprenden estos compuestos y al uso de estos compuestos y composiciones en la prevención o tratamiento de dichas enfermedades en las que están implicados los receptores de orexina.

87. 发明专利

ES2288861T3 ANTAGONISTAS DE LOS RECEPTORES DE LAS INTEGRINAS ALFA V. 未知
公开(公告)号：ES2288861T3
公开(公告)日：2008-02-01
申请号：ES00942652
申请日：2000-05-30
申请人： MERCK & CO INC
发明人： COLEMAN PAUL J , DUGGAN MARK E , HALCZENKO WASYL , HARTMAN GEORGE D , HUTCHINSON JOHN H , MEISSNER ROBERT S
IPC分类号： A61K31/506 , A61K31/437 , A61K31/4375 , A61K31/4709 , A61K31/498 , A61K31/501 , A61K31/505 , A61K31/536 , A61K31/55 , A61P9/00 , A61P9/08 , A61P9/10 , A61P17/00 , A61P19/08 , A61P19/10 , A61P27/02 , A61P29/00 , A61P31/12 , A61P35/00 , A61P35/04 , A61P43/00 , C07D213/02 , C07D221/00 , C07D223/14 , C07D239/24 , C07D239/48 , C07D241/36 , C07D265/28 , C07D401/06 , C07D471/02 , C07D471/04 , C07D519/00
摘要： Un compuesto que tiene la fórmula (IV): o una sal farmacéuticamente aceptable del mismo, en la que X es R2 se selecciona del grupo constituido por halógeno, alquilo C1-8, cicloalquilo C3-8, cicloheteroalquilo C3-8, (cicloalquil C3-8)alquilo C1-6, (cicloheteroalquil C3-8)-alquilo C1-6, arilo, arilalquilo C1-6, amino, aminoalquilo C1-6, acilamino C1-3, (acilamino C1-3)alquilo C1-6, (alquil C1-6)1-2 amino, (cicloalquil C3-6)amino C0-2, (alquil C1-6)1-2 aminoalquilo C1-6, alcoxi C1-6, (alcoxi C1-4)alquilo C1-6, hidroxicarbonilo, hidoxicarbonilalquilo C1-6, (alcoxi C1-3)carbonilo, (alcoxi C1-3)carbonilalquilo C1-6, hidroxi, hidroxialquilo C1-6, nitro, ciano, trifluorometilo, trifluorometoxi, trifluoroetoxi, (alquil C1-8)-S(O)0-2, (alquil C1-8)0-2 aminocarbonilo, {0>C1-8 alquiloxycarbonilamino, (C1-8 alquilh-2 aminocarboniloxy, (aril C1-3 alquil)1-2 amino, (arilh-2 amino, (alquiloxi C1-8)carbonilamino, (alquil C1-8)1-2aminocarboniloxi, (arilalquil C1-3)1-2 amino, (aril)1-2amino, aril(alquilC1-3)sulfonilamino y (alquil C1-8)sulfonilamino; R7 es arilo, en el que el grupo arilo se selecciona del grupo constituido por (1) fenilo, (2) naftilo, (3) piridilo, (4) furilo, (5) tienilo, (6) pirrolilo, (7) oxazolilo, (8) tiazolilo, (9) imidazolilo, (10) pirazolilo, (11) isoxazolilo, (12) isotiazolilo, (13) pirimidinilo, (14) pirazinilo, (15) piridazinilo, (16) tetrazolilo, (17) quinolilo, (18) isoquinolilo, (19) bencimidazolilo, (20) benzofurilo, (21) benzotienilo, (22) indolilo, (23) benzotiazolilo, (24) benzoxazolilo, (25) dihidrobenzofurilo, (26) benzo(1, 3)dioxolanilo, (27) benzo(1, 4)dioxanilo, (28) quinazolilo, (29) quinoxalilo, y (30) 3, 4-dihidro-2H-1, 4-dioxa-5-aza-naftalenilo: en el que el grupo arilo tal como se define anteriormente en los puntos (1) a (30) no está sustituido o está sustituido con de uno a tres sustituyentes que se seleccionan independientemente a partir del grupo constituido por hidroxi, hidroxialquilo C1-6, halógeno, alquilo C1-8, cicloalquilo C3-8, arilo,arilalquilo C1-3, amino, aminoalquilo C1-6, acilamino C1-3, (acilamino C1-3)-alquilo C1-6, (alquil C1-6)amino, di(alquil C1-6)amino, (alquil C1-6)aminoalquilo C1-6, di(alquil C1-6)aminoalquilo C1-6, alcoxi C1-4, (alquil C1-4)tio, (alquil C1-4)sulfinilo, (alquil C1-4)sulfonilo, (alcoxi C1-4)alquilo C1-6, hidroxicarbonilo, hidroxicarbonilalquilo C1-6, (alcoxi C1-5)carbonilo, (alcoxi C1-3)carbonilalquilo C1-6, (alquil C1-5)carboniloxi, ciano, trifluorometilo, 1, 1, 1-trifluoroetilo, trifluorometoxi, trifluoroetoxi, y nitro; o dos sustituyentes adyacentes junto con los átomos de carbono a los que están enlazados para formar un anillo saturado o insaturado de cinco o seis miembros que contiene 1 ó 2 heteroátomos que se seleccionan del grupo constituido por N, O, y S, cuyos átomos de carbono del anillo pueden estar sustituidos con oxo o alquilo C1-3; y R8 es hidrógeno o alquilo C1-3.

88. 发明专利

DK1187592T3 未知
公开(公告)号：DK1187592T3
公开(公告)日：2007-11-05
申请号：DK00942652
申请日：2000-05-30
申请人： MERCK & CO INC
发明人： COLEMAN PAUL J , DUGGAN MARK E , HALCZENKO WASYL , HARTMAN GEORGE D , HUTCHINSON JOHN H , MEISSNER ROBERT S , PATANE MICHAEL A , PERKINS JAMES J , WANG JIABING , BRESLIN MICHAEL J
IPC分类号： A61K31/506 , A61K31/437 , A61K31/4375 , A61K31/4709 , A61K31/498 , A61K31/501 , A61K31/505 , A61K31/536 , A61K31/55 , A61P9/00 , A61P9/08 , A61P9/10 , A61P17/00 , A61P19/08 , A61P19/10 , A61P27/02 , A61P29/00 , A61P31/12 , A61P35/00 , A61P35/04 , A61P43/00 , C07D213/02 , C07D221/00 , C07D223/14 , C07D239/24 , C07D239/48 , C07D241/36 , C07D265/28 , C07D401/06 , C07D471/02 , C07D471/04 , C07D519/00
摘要： The present invention relates to novel nonanoic acid derivatives, their synthesis, and their use as alphav integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors alphavbeta3 and alphavbeta5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, inflammatory arthritis, viral disease, cancer, and metastatic tumor growth.

89. 发明专利

DE60222577D1 未知
公开(公告)号：DE60222577D1
公开(公告)日：2007-10-31
申请号：DE60222577
申请日：2002-10-15
申请人： MERCK & CO INC
发明人： COLEMAN PAUL J , NEILSON LOU ANNE
IPC分类号： C07D471/04 , C07D491/052 , A61K31/55 , A61K45/00 , A61P1/02 , A61P3/06 , A61P5/26 , A61P5/28 , A61P7/06 , A61P9/10 , A61P11/02 , A61P13/08 , A61P15/08 , A61P15/10 , A61P17/16 , A61P19/00 , A61P19/08 , A61P19/10 , A61P21/00 , A61P43/00 , C07D487/02 , C07D491/04 , C07D491/10 , C07D491/20

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