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1. 发明公开

EP0790248A1 3-Aza-piperidone- (tetrahydropyrimidin-2-one) and 3-oxa-piperidone (1,3 oxazin-2-one) derivatives, their preparation and their use as tachykinin/neurokinin antagonists 失效
标题翻译： 3-氮杂 - 哌啶酮（四氢嘧啶-2-酮）和3-氧化 - 哌啶酮（1,3-恶嗪-2-酮）衍生物，德国Herstellung und deren Verwendung als速激肽/神经激肽拮抗剂
公开(公告)号：EP0790248A1
公开(公告)日：1997-08-20
申请号：EP97200156.4
申请日：1997-01-20
申请人： Pfizer Limited , Pfizer Research and Development Company, N.V./S.A.
发明人： Mackenzie, Alexander Roderick , Marchington, Allan Patrick , Meadows, Sandra Dora , Middleton, Donald Stuart
IPC分类号： C07D413/06 , C07D403/06 , C07D403/14 , A61K31/535 , A61K31/495
CPC分类号： C07D403/06 , C07D413/06
摘要： Compounds of the formula:
wherein:
X is O, NH or NR 1 ; R 1 is C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl, C 3 -C 7 cycloalkyl(C 1 -C 4 )alkyl, aryl or aryl (C 1 -C 4 )alkyl; wherein the C 1 -C 6 alkyl group is optionally substituted by fluorine and the C 3 -C 7 cycloalkyl or C 3 -C 7 cycloalkyl(C 1 -C 4 )alkyl group is optionally substituted in the cycloalkyl ring by up to two substituents each independently selected from halo, C 1 -C 4 alkoxy or halo(C 1 -C 4 )alkoxy; R 2 is phenyl optionally substituted with one or two halo substituents, indolyl or thienyl; R 3 is NH 2 , -NR 4 SO 2 (C 1 -C 6 alkyl), -NR 4 SO 2 aryl, -NR 4 CO(C 1 -C 6 alkyl), -NR 4 CO aryl or a 5 to 7-membered N-linked cyclic group incorporating W in the ring wherein W is O, NR 5 , CH(OH), CHCO 2 H, CHN(R 4 ) 2 , CHF, CF 2 , C = O or CH 2 ; R 4 is H or C 1 -C 6 alkyl; R 5 is H, C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl, C 3 -C 7 cycloalkyl(C 1 -C 6 )alkyl, C 2 -C 6 alkanoyl, C 4 -C 8 cycloalkanoyl, C 3 -C 7 cycloalkyl(C 2 -C 6 )alkanoyl, aryl CO-, C 1 -C 6 alkyl SO 2 -, C 3 -C 7 cycloalkyl SO 2 -, C 3 -C 7 cycloalkyl(C 1 -C 6 )alkyl SO 2 -, aryl-SO 2 - or (R 6 ) 2 NSO 2 -, wherein each R 6 is independently H or C 1 -C 4 alkyl or the two groups may be joined to form with the nitrogen atom to which they are attached, a pyrrolidinyl, piperidino, morphlino or piperazinyl group; m is O, 1 or 2 with the proviso that m is not O when W is NR 5 , C=O, or O; and n is an integer of from 1 to 4; are neurokinin receptor antagonists of utility in the treatment of a variety of medical conditions including urinary incontinence, asthma and related conditions.
摘要翻译：下式化合物：其中：X为O，NH或NR 1; R 1是C 1 -C 6烷基，C 3 -C 7环烷基，C 3 -C 7环烷基（C 1 -C 4）烷基，芳基或芳基（C 1 -C 4）烷基; 其中C 1 -C 6烷基任选被氟取代，并且C 3 -C 7环烷基或C 3 -C 7环烷基（C 1 -C 4）烷基任选在环烷基环中被至多两个各自独立地选自卤素， C4烷氧基或卤代（C1-C4）烷氧基; R 2是任选被一个或两个卤素取代基取代的苯基，吲哚基或噻吩基; R 3是NH 2，-NR 4 SO 2（C 1 -C 6烷基），-NR 4 SO 2芳基，-NR 4 CO（C 1 -C 6烷基），-NR 4 CO芳基或在其中W为O，NR 5，CH（OH），CHCO 2 H，CHN（R 4）2，CHF，CF 2，C = O或CH 2的环中结合W的5至7元N-连接的环状基团 ; R 4是H或C 1 -C 6烷基; R 5是H，C 1 -C 6烷基，C 3 -C 7环烷基，C 3 -C 7环烷基（C 1 -C 6）烷基，C 2 -C 6烷酰基，C 4 -C 8环烷酰基，C 3 -C 7环烷基（C 2 -C 6）烷酰基，芳基 CO-，SO 2 - ，C 3 -C 7环烷基SO 2 - ，C 3 -C 7环烷基（C 1 -C 6）烷基SO 2 - ，芳基-SO 2 - 或（R 6）2NSO 2 - ，其中每个R 6，独立地是H或C 1 -C 4烷基或两个基团可以与它们所连接的氮原子一起形成，吡咯烷基，哌啶子基，吗啉基或哌嗪基; m为O，1或2，条件是当W为NR 5，C = O或O时m不为O; n为1〜4的整数，是用于治疗各种医学状况（包括尿失禁，哮喘和相关病症）的神经激肽受体拮抗剂。

2. 发明公开

EP0791592A3 Azetidines 失效
标题翻译：氮杂环丁烷
公开(公告)号：EP0791592A3
公开(公告)日：2000-05-17
申请号：EP97200200.0
申请日：1997-01-24
申请人： Pfizer Limited , Pfizer Research and Development Company, N.V./S.A.
发明人： Mackenzie, Alexander Roderick , Marchington, Allan Patrick , Meadows, Sandra Dora , Middleton, Donald Stuart
IPC分类号： C07D401/06 , C07D401/12 , A61K31/44 , C07D211/88
CPC分类号： C07D401/06 , C07D211/88
摘要： The present invention provides compounds of the formula (I):- and the pharmaceutically acceptable salts thereof, wherein R is C 3 -C 7 cycloalkyl, aryl or C 1 -C 6 alkyl, said C 1 -C 6 alkyl being optionally substituted by fluoro, -COOH, -COO(C 1 -C 4 ) alkyl, C 3 -C 7 cycloalkyl, adamantyl, aryl or het 1 , and said C 3 -C 7 cycloalkyl being optionally substituted by 1 or 2 substituents each independently selected from C 1 -C 4 alkyl, C 3 -C 7 cycloalkyl, C 1 -C 4 alkoxy, hydroxy, fluoro, fluoro(C 1 -C 4 ) alkyl and fluoro(C 1 -C 4 )alkoxy; R1 is phenyl, benzyl, naphthyl, thienyl, benzothienyl or indolyl, each optionally substituted by 1 or 2 substituents each independently selected from C1-C4 alkyl, C1-C4 alkoxy, halo and trifluoromethyl; R2 represents various groups; X is C1-C4 alkylene; and X1 is a direct link or C1-C6 alkylene. Such compounds and salts are useful as tachykinin antagonists.

3. 发明公开

EP0791592A2 Azetidines 失效
标题翻译：氮杂环丁烷
公开(公告)号：EP0791592A2
公开(公告)日：1997-08-27
申请号：EP97200200.0
申请日：1997-01-24
申请人： Pfizer Limited , Pfizer Research and Development Company, N.V./S.A.
发明人： Mackenzie, Alexander Roderick , Marchington, Allan Patrick , Meadows, Sandra Dora , Middleton, Donald Stuart
IPC分类号： C07D401/06 , C07D401/12 , A61K31/44
CPC分类号： C07D401/06 , C07D211/88
摘要： The present invention provides compounds of the formula (I):-
and the pharmaceutically acceptable salts thereof, wherein
R is C 3 -C 7 cycloalkyl, aryl or C 1 -C 6 alkyl, said C 1 -C 6 alkyl being optionally substituted by fluoro, -COOH, -COO(C 1 -C 4 ) alkyl, C 3 -C 7 cycloalkyl, adamantyl, aryl or het 1 , and said C 3 -C 7 cycloalkyl being optionally substituted by 1 or 2 substituents each independently selected from C 1 -C 4 alkyl, C 3 -C 7 cycloalkyl, C 1 -C 4 alkoxy, hydroxy, fluoro, fluoro(C 1 -C 4 ) alkyl and fluoro(C 1 -C 4 )alkoxy;

R 1 is phenyl, benzyl, naphthyl, thienyl, benzothienyl or indolyl, each optionally substituted by 1 or 2 substituents each independently selected from C 1 -C 4 alkyl, C 1 -C 4 alkoxy, halo and trifluoromethyl;
R 2 represents various groups;
X is C 1 -C 4 alkylene; and
X 1 is a direct link or C 1 -C 6 alkylene.

Such compounds and salts are useful as tachykinin antagonists.
摘要翻译：本发明提供了式（I）化合物： - 及其药学上可接受的盐，其中R是C 3 -C 7环烷基，芳基或C 1 -C 6烷基，所述C 1 -C 6烷基任选被氟取代， COOH，-COO（C 1 -C 4）烷基，C 3 -C 7环烷基，金刚烷基，芳基或杂环，并且所述C 3 -C 7环烷基任选被1或2个独立地选自C 1 -C 4烷基， C7环烷基，C1-C4烷氧基，羟基，氟，氟（C1-C4）烷基和氟（C1-C4）烷氧基; R 1是苯基，苄基，萘基，噻吩基，苯并噻吩基或吲哚基，各自任选被1或2个独立地选自C 1 -C 4烷基，C 1 -C 4烷氧基，卤素和三氟甲基的取代基取代; R 2表示各种基团; X是C 1 -C 4亚烷基; 且X 1是直链或C 1 -C 6亚烷基。这些化合物和盐可用作速激肽拮抗剂。

4. 发明授权

EP0790248B1 3-Aza-piperidone- (tetrahydropyrimidin-2-one) and 3-oxa-piperidone (1,3 oxazin-2-one) derivatives, their preparation and their use as tachykinin/neurokinin antagonists 失效
标题翻译： 3-氮杂 - 哌啶酮（四氢嘧啶-2-酮）和3-氧杂哌啶酮（1,3-恶嗪-2-酮）衍生物，它们的制备和它们作为速激肽/神经激肽拮抗剂的用途
公开(公告)号：EP0790248B1
公开(公告)日：2003-05-28
申请号：EP97200156.4
申请日：1997-01-20
申请人： Pfizer Limited , Pfizer Research and Development Company, N.V./S.A.
发明人： Mackenzie, Alexander Roderick , Marchington, Allan Patrick , Meadows, Sandra Dora , Middleton, Donald Stuart
IPC分类号： C07D413/06 , C07D403/06 , C07D403/14 , A61K31/535 , A61K31/495
CPC分类号： C07D403/06 , C07D413/06

5. 发明授权

EP0791592B1 Azetidines 失效
标题翻译：氮杂环丁烷
公开(公告)号：EP0791592B1
公开(公告)日：2003-05-21
申请号：EP97200200.0
申请日：1997-01-24
申请人： Pfizer Limited , Pfizer Research and Development Company, N.V./S.A.
发明人： Mackenzie, Alexander Roderick , Marchington, Allan Patrick , Meadows, Sandra Dora , Middleton, Donald Stuart
IPC分类号： C07D401/06 , C07D401/12 , A61K31/44 , C07D211/88
CPC分类号： C07D401/06 , C07D211/88

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