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1. 发明授权

EP0748800B1 Pyrimidinedione, pyrimidinetrione, triazinedione derivatives as alpha-1-adrenergic receptor antagonists 失效
标题翻译： Pyrimidindion-，Pyrimidintrion-，Triazindion-Derivate als alpha-1-adrenergische Rezeptorantagonisten
公开(公告)号：EP0748800B1
公开(公告)日：2001-05-09
申请号：EP96108493.6
申请日：1996-05-28
申请人： F. HOFFMANN-LA ROCHE AG
发明人： Bantle, Gary W. , Elworthy, Todd R. , Guzman, Angel , Jaime-Figueroa, Saul , Lopez-Tapia, Francisco J. , Morgans, David J., Jr. , Perez-Medrano, Arturo , Pfister, Jürg R. , Sjogren, Eric B. , Talamas, Francisco X.
IPC分类号： C07D239/54 , C07D239/60 , C07D253/06 , C07D403/06 , A61K31/505 , A61K31/53
CPC分类号： C07D239/54 , C07D239/545 , C07D239/553 , C07D239/557 , C07D239/60 , C07D239/96 , C07D253/075 , C07D401/06 , C07D403/06 , C07D405/06 , C07D413/12

2. 发明公开

EP0748800A3 Pyrimidinedione, pyrimidinetrione, triazinedione, tetrahydroquinazolinedione derivatives as alpha-1-adrenergic receptor antagonists 失效
标题翻译：作为α-1-肾上腺素能受体拮抗剂的嘧啶二酮，嘧啶三酮，三嗪二酮，四氢喹唑啉二酮衍生物
公开(公告)号：EP0748800A3
公开(公告)日：1996-12-27
申请号：EP96108493.6
申请日：1996-05-28
申请人： F. HOFFMANN-LA ROCHE AG
发明人： Bantle, Gary W. , Elworthy, Todd R. , Guzman, Angel , Jaime-Figueroa, Saul , Lopez-Tapia, Francisco J. , Morgans, David J., Jr. , Perez-Medrano, Arturo , Pfister, Jürg R. , Sjogren, Eric B. , Talamas, Francisco X.
IPC分类号： C07D239/54 , C07D239/60 , C07D253/06 , C07D239/96 , C07D407/12 , C07D407/04 , C07D403/06 , C07D409/04 , C07D407/06 , C07D401/06 , C07D413/12 , C07D403/12 , A61K31/505 , A61K31/53
CPC分类号： C07D239/54 , C07D239/545 , C07D239/553 , C07D239/557 , C07D239/60 , C07D239/96 , C07D253/075 , C07D401/06 , C07D403/06 , C07D405/06 , C07D413/12
摘要： The present invention relates to novel α 1 -adrenoceptor antagonists of the formula I
in which:
R 1 is acetylamino, amino, cyano, trifluoroacetylamino, halo, hydro, hydroxy, nitro, methylsulfonylamino, 2-propynyloxy, a group selected from (C 1-6 )alkyl, (C 3-6 )cycloalkyl, (C 3-6 )cycloalkyl(C 1-4 )alkyl, (C 1-6 )alkyloxy, (C 3-6 )cycloalkyloxy, (C 3-6 )cycloalkyl(C 1-4 )alkyloxy and (C 1-4 )alkylthio (which group is optionally further substituted with one to three halo atoms) or a group selected from aryl, aryl(C 1-4 )alkyl, heteroaryl, heteroaryl(C 1-4 )alkyl, aryloxy, aryl(C 1-4 )alkyloxy, heteroaryloxy and heteroaryl(C 1-4 )alkyloxy (which aryl and heteroaryl are optionally further substituted with one to two radicals independently selected from halo and cyano); R 2 is cyano, halo, hydro, hydroxy or a group selected from (C 1-6 )alkyl and (C 1-6 )alkyloxy (which group is optionally further substituted with one to three halogen atoms); R 3 and R 4 are both hydro or methyl or together are ethylene; and R 5 is a group selected from Formulae (a), (b), (c) and (d):
in which:
X is C(O), CH 2 or CH(OH); Y is CH 2 or CH(OH); Z is N or C(R 9 ), wherein R 9 is hydro, (C 1-6 )alkyl or hydroxy; R 6 is hydro, a group selected from (C 1-6 )alkyl, (C 3-6 )cycloalkyl, (C 3-6 )cycloalkyl(C 1-4 )alkyl (which group is optionally further substituted with one to three halo atoms) or a group selected from aryl, heteroaryl, aryl(C 1-4 )alkyl and heteroaryl(C 1-4 )alkyl (which aryl and heteroaryl are optionally further substituted with one to three radicals selected from halo, cyano, (C 1-6 )alkyloxy, (C 1-6 )alkyl and aryl); R 7 is (C 1-6 )alkanoyl, carbamoyl, cyano, di(C 1-6 )alkylamino, halo, hydro, hydroxy, hydroxyiminomethyl, (C 1-6 )alkylsulfonyl, (C 1-6 )alkylthio, a group selected from (C 1-6 )alkyl, (C 3-6 )cycloalkyl, (C 1-6 )alkyloxy and (C 1-6 )alkyloxy(C 1-4 )alkyl (which group is optionally further substituted with one to three radicals selected from halo, hydroxy or (C 1-6 )alkyloxy) or a group selected from aryl, heteroaryl, aryl(C 1-4 )alkyl and heteroaryl(C 1-4 )alkyl (which aryl and heteroaryl are optionally further substituted with one to three radicals selected from halo, cyano, (C 1-6 )alkyloxy, (C 1-6 )alkyl and aryl) or R 7 and R 9 together are tetramethylene; and each R 8 is independently hydro, hydroxy, methyl or ethyl; and the pharmaceutically acceptable salts and N -oxides thereof.
摘要翻译：本发明涉及式I的新型α1-肾上腺素受体拮抗剂，其中：R1是乙酰氨基，氨基，氰基，三氟乙酰氨基，卤素，羟基，硝基，甲基磺酰氨基，2-丙炔氧基，选自（C1-6）（C3-6）环烷基，（C3-6）环烷基（C1-4）烷基，（C1-6）烷氧基，（C3-6）环烷氧基，（C3-6）环烷基（C1-4）烷氧基和（C 1-4）烷硫基（该基团任选进一步被1-3个卤素原子取代）或选自芳基，芳基（C 1-4）烷基，杂芳基，杂芳基（C 1-4）烷基，芳氧基，芳基 4）烷氧基，杂芳氧基和杂芳基（C 1-4）烷氧基（其中芳基和杂芳基任选进一步被1-2个独立地选自卤素和氰基的基团取代）; R2是氰基，卤素，氢，羟基或选自（C1-6）烷基和（C1-6）烷氧基的基团（该基团任选进一步被1-3个卤素原子取代）。 R3和R4都是氢或甲基或一起是乙烯; R5是选自式（a），（b），（c）和（d）的基团：其中：X是C（O），CH2或CH（OH）。 Y是CH2或CH（OH）; Z是N或C（R9），其中R9是氢，（C1-6）烷基或羟基; R6是氢，选自（C1-6）烷基，（C3-6）环烷基，（C3-6）环烷基（C1-4）烷基（该基团任选进一步被1-3个卤素原子取代）或者芳基（C 1-4）烷基和杂芳基（C 1-4）烷基（其中芳基和杂芳基任选进一步被1-3个选自卤素，氰基，（C 1-6）烷氧基，（ C1-6）烷基和芳基）; （C1-6）烷酰基，氨基甲酰基，氰基，二（C1-6）烷氨基，卤素，羟基，羟基亚氨基甲基，（C1-6）烷基磺酰基，（C1-6）烷硫基，选自 6）烷基，（C3-6）环烷基，（C1-6）烷氧基和（C1-6）烷氧基（C1-4）烷基（该基团任选进一步被1-3个选自卤素，羟基或C1- -6）烷氧基）或选自芳基，杂芳基，芳基（C 1-4）烷基和杂芳基（C 1-4）烷基（其中芳基和杂芳基任选进一步被1-3个选自卤素，氰基，（ C1-6）烷氧基，（C1-6）烷基和芳基）或R7和R9一起为四亚甲基; 并且每个R 8独立地是氢，羟基，甲基或乙基; 及其药学上可接受的盐和N-氧化物。

3. 发明公开

EP0748800A2 Pyrimidinedione, pyrimidinetrione, triazinedione, tetrahydroquinazolinedione derivatives as alpha-1-adrenergic receptor antagonists 失效
标题翻译：嘧啶二酮，嘧啶并 - 三氮茚，四氢化合物 - 衍生物α1-肾上腺素能激动剂
公开(公告)号：EP0748800A2
公开(公告)日：1996-12-18
申请号：EP96108493.6
申请日：1996-05-28
申请人： F. HOFFMANN-LA ROCHE AG
发明人： Bantle, Gary W. , Elworthy, Todd R. , Guzman, Angel , Jaime-Figueroa, Saul , Lopez-Tapia, Francisco J. , Morgans, David J., Jr. , Perez-Medrano, Arturo , Pfister, Jürg R. , Sjogren, Eric B. , Talamas, Francisco X.
IPC分类号： C07D239/54 , C07D239/60 , C07D253/06 , C07D239/96 , C07D407/12 , C07D407/04 , C07D403/06 , C07D409/04 , C07D407/06 , C07D401/06 , C07D413/12 , C07D403/12 , A61K31/505 , A61K31/53
CPC分类号： C07D239/54 , C07D239/545 , C07D239/553 , C07D239/557 , C07D239/60 , C07D239/96 , C07D253/075 , C07D401/06 , C07D403/06 , C07D405/06 , C07D413/12
摘要： The present invention relates to novel α 1 -adrenoceptor antagonists of the formula I
in which:

R 1 is acetylamino, amino, cyano, trifluoroacetylamino, halo, hydro, hydroxy, nitro, methylsulfonylamino, 2-propynyloxy, a group selected from (C 1-6 )alkyl, (C 3-6 )cycloalkyl, (C 3-6 )cycloalkyl(C 1-4 )alkyl, (C 1-6 )alkyloxy, (C 3-6 )cycloalkyloxy, (C 3-6 )cycloalkyl(C 1-4 )alkyloxy and (C 1-4 )alkylthio (which group is optionally further substituted with one to three halo atoms) or a group selected from aryl, aryl(C 1-4 )alkyl, heteroaryl, heteroaryl(C 1-4 )alkyl, aryloxy, aryl(C 1-4 )alkyloxy, heteroaryloxy and heteroaryl(C 1-4 )alkyloxy (which aryl and heteroaryl are optionally further substituted with one to two radicals independently selected from halo and cyano);
R 2 is cyano, halo, hydro, hydroxy or a group selected from (C 1-6 )alkyl and (C 1-6 )alkyloxy (which group is optionally further substituted with one to three halogen atoms);
R 3 and R 4 are both hydro or methyl or together are ethylene; and
R 5 is a group selected from Formulae (a), (b), (c) and (d):

in which:

X is C(O), CH 2 or CH(OH);
Y is CH 2 or CH(OH);
Z is N or C(R 9 ), wherein R 9 is hydro, (C 1-6 )alkyl or hydroxy;
R 6 is hydro, a group selected from (C 1-6 )alkyl, (C 3-6 )cycloalkyl, (C 3-6 )cycloalkyl(C 1-4 )alkyl (which group is optionally further substituted with one to three halo atoms) or a group selected from aryl, heteroaryl, aryl(C 1-4 )alkyl and heteroaryl(C 1-4 )alkyl (which aryl and heteroaryl are optionally further substituted with one to three radicals selected from halo, cyano, (C 1-6 )alkyloxy, (C 1-6 )alkyl and aryl);
R 7 is (C 1-6 )alkanoyl, carbamoyl, cyano, di(C 1-6 )alkylamino, halo, hydro, hydroxy, hydroxyiminomethyl, (C 1-6 )alkylsulfonyl, (C 1-6 )alkylthio, a group selected from (C 1-6 )alkyl, (C 3-6 )cycloalkyl, (C 1-6 )alkyloxy and (C 1-6 )alkyloxy(C 1-4 )alkyl (which group is optionally further substituted with one to three radicals selected from halo, hydroxy or (C 1-6 )alkyloxy) or a group selected from aryl, heteroaryl, aryl(C 1-4 )alkyl and heteroaryl(C 1-4 )alkyl (which aryl and heteroaryl are optionally further substituted with one to three radicals selected from halo, cyano, (C 1-6 )alkyloxy, (C 1-6 )alkyl and aryl) or R 7 and R 9 together are tetramethylene; and each R 8 is independently hydro, hydroxy, methyl or ethyl; and the pharmaceutically acceptable salts and N -oxides thereof.
摘要翻译：本发明涉及式I 的新型α1-肾上腺素受体拮抗剂，其中：R 1是乙酰氨基，氨基，氰基，三氟乙酰氨基，卤素，氢，羟基，硝基，甲基磺酰基氨基，2-丙炔氧基，选自（C 1-6）烷基，（C 3-6）环烷基，（C 3-6）环烷基（C 1-4）烷基，（C 1-6）烷氧基，（C 3-6）环烷氧基，（C 3-6） C 1-4）烷氧基和（C 1-4）烷硫基（该基团任选进一步被一至三个卤原子取代）或选自芳基，芳基（C 1-4）烷基，杂芳基，杂芳基（C 1-4）烷基，芳氧基，芳基（C 1-4）烷氧基，杂芳氧基和杂芳基（C 1-4）烷氧基（该芳基和杂芳基任选被一至两个独立地选自卤素和氰基的基团进一步取代）; R 2为氰基，卤素，氢，羟基或选自（C 1-6）烷基和（C 1-6）烷氧基（该基团任选进一步被一至三个卤素原子取代）的基团; R 3和R 4都是氢或甲基或一起是亚乙基; 并且R 5为选自式（a），（b），（c）和（d）的基团：其中：X为C（O），CH 2或CH（OH）; Y是CH 2或CH（OH）; Z是N或C（R 9），其中R 9是氢，（C 1-6）烷基或羟基; R 6是氢，选自（C 1-6）烷基，（C 3-6）环烷基，（C 3-6）环烷基（C 1-4）烷基（该基团任选进一步被一至三个卤素原子）或选自芳基，杂芳基，芳基（C 1-4）烷基和杂芳基（C 1-4）烷基的基团（该芳基和杂芳基任选进一步被一至三个选自卤素，氰基，（C 1-6）烷氧基，（C 1-6）烷基和芳基）; R 7是（C 1-6）烷酰基，氨基甲酰基，氰基，二（C 1-6）烷基氨基，卤素，氢，羟基，羟基亚氨基甲基，（C 1-6）烷基磺酰基，（C 1-6）烷硫基，（C 1-6）烷基，（C 3-6）环烷基，（C 1-6）烷氧基和（C 1-6）烷氧基（C 1-4）烷基（该基团任选进一步被一至三个选自卤素，羟基或（C 1-6）烷氧基）或选自芳基，杂芳基，芳基（C 1-4）烷基和杂芳基（C 1-4）烷基的基团（该芳基和杂芳基任选进一步被一至三个选自卤素，氰基，（C 1-6）烷氧基，（C 1-6）烷基和芳基）或R 7和R 9一起是四亚甲基; 并且每个R 8独立地是氢，羟基，甲基或乙基; 及其药学上可接受的盐和N-氧化物。

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