首页> 外国专利> Derivatives of quinolinamida positive allosteric modulators of Muscarinic M1 Receptors, Pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease, Schizophrenia and other disorders of the central nervous system.

Derivatives of quinolinamida positive allosteric modulators of Muscarinic M1 Receptors, Pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease, Schizophrenia and other disorders of the central nervous system.

机译：毒蕈碱M1受体的喹啉酰胺正变构调节剂的衍生物，含有它们的药物组合物及其在治疗阿尔茨海默氏病，精神分裂症和中枢神经系统其他疾病中的用途。

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Claim 1: a formula compound (1), wherein X1 is selected from the group consisting of (1) n, and (2) n; x2-x3 is selected from the group consisting of (1) - ch2-ch2 -.That's it, that's it.(3) -CH2-O-,That's it, that's it.each of X4, X5, X6 and X7 is selected from the group consisting of (1) N, (2) N «O, (3) CH, (4) O, provided that one of X4, X5, X6 and X7 it may be absent, thereby forming a five-member ring; R1 selects from the group consisting of (1) hydrogen, (2) halogen, (3) -C1-6 alkyl, (4) -C2-6 alkynyl, (4) phenyl, (5) = O, (6) = CH2, (7) hydroxyl, wherein the alkyl, alkynyl or phenyl group R1 is optionally substituted with one or more (a) hydroxyl, or (b) halogen; R2A and R2B, independently-select from the group consisting of (1) hydrogen, (2) hydroxyl, and (3) halogen, or R2A and R2B together form = O;R3 is optional, exists in one or more cyclic carbon atoms, and is independently selected from a group consisting of (1) halogen, (2) - or - tar C1-6, (3) - s-tar C1-6, or (4) a heteromorphic group, which is a cyclic aromatic group with 5 to 12 atoms in the ring; this is a cyclic atom. Select from C, O, N, n 'or s, at least one of which is O, n' or s, where C1-6 tar can be selected to replace the heteromorphism; R4 may exist in one or more ring atoms and be selected from the group consisting of (1) hydroxy, (2) halogenated (3) - C1-6 tar, (4) - or C1-6 tar.(5) - C1-6 (6) - cyclo-c3-8 (7) - arilo C6-10 (8) - CN (9) is a heteromorphic group, which is a cyclic aromatic group, with 5 to 12 atoms in the ring; these cyclic atoms are selected from C, O, n 'or s, at least one of which is o, n' or s, (10) - o-isopropene (11) - nrab, Where R and Rb are selected from (a) hydrogen, or (b) C1-6 tar, or RA and Rb groups, and form 4-6 carbon rings together with the attached nitrogen, wherein one or two carbon atoms of the ring can be optionally replaced by a nitro, oxygen or sulfur,and the ring is optionally substituted with one or more (a) halogen, (b) hydroxyl, (c) C1-6 alkyl, (d) -O-C1-6 alkyl, (e) -C (= O) - ( O) n-C1-6 alkyl; where n is 0-1; and the alkyl, cycloalkyl, aryl or heteroaryl group R 4 is optionally substituted with one or more (a) halogen, (b) hydroxy, (c) -O-C 1-6 alkyl, (d) -C 1-6 alkyl, (e ) -S-C 1-6 alkyl, or (f) a heteroaryl group, which is an aromatic cyclic group, having between five and twelve ring atoms; said ring atoms are selected from C, O, N, N 'O or S, at least one of which is O, N, N' O or S, where the alkyl, aryl or heteroaryl moiety is optionally substituted with one or more (i) halogen,(II) hydroxy, (III) - or - C1-6 tar, or (IV) C1-6 tar; or two R4 groups are combined to form a compound cyclic heteromorphic group consisting of three or four atoms selected from C, or n 'or s, at least one of which is O, n' or s, or a salt acceptable for a drug.

机译：2.根据权利要求1所述的式化合物（1），其中X 1选自（1）n和（2）n; x2-x3是从（1）-ch2-ch2-组成的组中选择的。就是这样，就是这样。（3）-CH2-O-，就是这样，每个X4，X5，X6和X7是选自（1）N，（2）N«O，（3）CH，（4）O，条件是X4，X5，X6和X7之一可能不存在，从而形成五元环; R1选自由以下组成的组：（1）氢，（2）卤素，（3）-C1-6烷基，（4）-C2-6炔基，（4）苯基，（5）= O，（6）= CH2，（7）羟基，其中烷基，炔基或苯基R1任选地被一个或多个（a）羟基或（b）卤素取代; R2A和R2B独立地选自（1）氢，（2）羟基和（3）卤素，或R2A和R2B一起形成= O; R3是可选的，存在于一个或多个环状碳原子中，且独立地选自由以下组成的组：（1）卤素，（2）-或-焦油C1-6，（3）-s-焦油C1-6或（4）为环芳基的杂晶基团环中有5至12个原子;这是一个环状原子。从C，O，N，n'或s中选择，其中至少一个是O，n'或s，其中可以选择C1-6焦油来代替异质性; R 4可以存在于一个或多个环原子中，并且选自（1）羟基，（2）卤化（3）-C1-6焦油，（4）-或C1-6焦油。（5）-C1 -6（6）-环-c3-8（7）-芳基C6-10（8）-CN（9）是杂环基，是环状的芳香族基团，在环中具有5至12个原子;这些环原子选自C，O，n'或s，其中至少一个为o，n'或s，（10）-邻异丙烯（11）-阿拉伯，其中R和Rb选自（a ）氢，或（b）C1-6焦油，或RA和Rb基团，与连接的氮一起形成4-6个碳环，其中环的一个或两个碳原子可被硝基，氧或硫，并且该环任选地被一个或多个（a）卤素，（b）羟基，（c）C1-6烷基，（d）-O-C1-6烷基，（e）-C（= O）取代-（O）正C 1-6烷基;其中n是0-1;并且烷基，环烷基，芳基或杂芳基基团R 4任选地被一个或多个（a）卤素，（b）羟基，（c）-OC 1-6烷基，（d）-C 1-6烷基，（ e）-SC 1-6烷基，或（f）杂芳基，其为具有五个至十二个环原子的芳族环状基团;所述环原子选自C，O，N，N'O或S，其中至少一个是O，N，N'O或S，其中烷基，芳基或杂芳基部分可选地被一个或多个取代（ i）卤素，（II）羟基，（III）-或-C1-6焦油或（IV）C1-6焦油;或两个R 4基团结合形成由三个或四个选自C或n'或s的原子组成的化合物环状杂晶基团，其中至少一个是O，n'或s，或药物可接受的盐。

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公开/公告号AR079510A1

专利类型
公开/公告日2012-02-01

原文格式PDF
申请/专利权人 MERCK SHARP & DOHME CORP.;
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申请/专利号AR2010P104723
发明设计人
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申请日2010-12-17
分类号C07D215/48;C07D401/06;C07D401/14;C07D403/06;C07D405/14;C07D405/12;C07D413/14;C07D417/14;A61K31/47;A61K31/4709;A61P25/28;A61P25/18;A61P25/04;
国家 AR
入库时间 2022-08-21 17:25:35

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