首页> 外国专利> Compound, pharmaceutical composition, use of a compound, and, method for treating a condition associated with reduced nicotine transmission, for treatment or prophylaxis of psychotic disorders or disorders of intellectual impairment and for treatment or prophylaxis of human diseases or conditions

Compound, pharmaceutical composition, use of a compound, and, method for treating a condition associated with reduced nicotine transmission, for treatment or prophylaxis of psychotic disorders or disorders of intellectual impairment and for treatment or prophylaxis of human diseases or conditions

机译：化合物，药物组合物，化合物的用途以及用于治疗与尼古丁传播减少有关的疾病的方法，用于治疗或预防精神病或智力障碍的疾病以及用于治疗或预防人类疾病或病况的方法

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摘要

"COMPOUND, PHARMACEUTICAL COMPOSITION, USE OF A COMPOUND, AND, METHODS FOR TREATMENT OF A CONDITION ASSOCIATED WITH REDUCED TRANSMISSION OF NICOTINE, FOR TREATMENT OR PROPHYLAXIS OF PSYCHOTIC DISTURBANCES OR DISTURBANCES OF DETERIORATION OF EARTH DETECTION. A compound of Formula (I), wherein R ^ 1 ^ represents hydrogen or C ~ 1 ~ -C ~ 4 ~ alkyl, C ~ 2 ~ -C ~ 4 ~ alkenyl, C ~ 2 ~ -C ~ 4 ~ alkynyl or (CH ~ 2 ~) nAr; W represents C (O), C (O) O, C (O) NR ^ 6 ^ or a bond; R ^ 2 ^ represents hydrogen, Ar, or (CH ~ 2 ~) ~ p ~ CH [(CH ~ 2 ~) ~ q ~ R ^ 7 ^] (CH ~ 2 ~) ~ t ~ R ^ 8 ^; or together R ^ 2 ^ and R ^ 6 ^ represent (CH ~ 2 ~) ~ j ~ Y (CH ~ 2 ~) ~ k ~; R ^ 3 ^ and R ^ 5 ^ independently represent hydrogen, halogen or C ~ 1 ~ -C ~ 4 ~ alkyl; X represents oxygen, or NH; R ^ 4 ^ represents hydrogen, C ~ 1 ~ -C ~ 4 ~ alkyl (CH ~ 2 ~) ~ u ~ Ar, R ^ 9 ^ CO, or R ^ 9 ^ SO ~ 2 ~; R ^ 6 ^ represents hydrogen, C ~ 1 ~ -C ~ 4 ~ alkyl, aryl or heteroaryl, or together R ^ 2 ^ and R ^ 6 ^ represent (CH ~ 2 ~) ~ j ~ Y (CH ~ 2 ~) ~ k ~; R ^ 7 ^ and R ^ 8 ^ independently represent hydrogen or halogen, CN, -C 154 CH, N ~ 3 ~, CF ~ 3 ~, NO ~ 2 ~, AR, OR ^ 10 ^, NR ^ 10 ^ R ^ 11 ^, C (O) OR ^ 10 ^, OC (O) R ^ 10 ^, C (O) NR ^ 10 ^ R ^ 11 ^, NR ^ 10 ^ C (O) R ^ 11 ^ , SO ~ 2 ~ NR ^ 10 ^ R ^ 11 ^, or NR ^ 10 ^ SO ~ 2 ~ R ^ 11 ^; R 9 represents C ~ 1 ~ -C ~ 4 ~ alkyl, or Ar; Ar represents phenyl, naphthyl or a 5- or 6-membered heterocyclic ring, containing 0-3 nitrogens, 0-1 sulfur and 0-1 oxygen; Air is optionally substituted by one or more substituents independently selected from: hydrogen, halogen, C ~ 1 ~ -C ~ 4 ~ alkyl, C ~ 2 ~ -C ~ 4 ~ alkenyl, C ~ 2 ~ -C ~ 4 ~ alkynyl, (CH ~ 2 ~) ~ n ~ aryl, CN, NO ~ 2 ~, CF ~ 3 ~, OR ^ 12 ^, NR ^ 12 ^ R ^ 13 ^ and COOR ^ 12 ^, R ^ 10 ^, R ^ 11 ^, R ^ 12 ^ and R ^ 13 ^ independently represent hydrogen, C ~ 1 ~ -C ~ 4 ~ alkyl, aryl or heteroaryl; or together R ^ 10 ^ and R ^ 11 ^ and / or R ^ 12 ^ and R ^ 13 ^ independently represent (CH ~ 2 ~) ~ j ~ Y (CH ~ 2 ~) ~ k ~; Y represents oxygen, sulfur, NR ^ 14 ^ or a bond; j is 2-4; k, m, n, p, q, t and u are independently 0-2; R ^ 14 ^ ^ represents hydrogen, C ~ 1 ~ C ~ 4 ~ alkyl, aryl or heteroaryl; or an enanciomer, and its pharmaceutically acceptable salts, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, especially for treating conditions associated with reductions in nicotinic transmission. The compounds of the invention increase the effectiveness of agonists at nicotinic receptors.

机译：“化合物，药物成分，化合物的使用，以及与烟碱减少的传播有关的疾病的治疗方法，用于精神紊乱的治疗或预防，或对地球变态的破坏的干扰，其中，（式）化合物： R ^ 1 ^代表氢或C〜1〜-C〜4〜烷基，C〜2〜-C〜4〜烯基，C〜2〜-C〜4〜炔基或（CH〜2〜）nAr; W代表C（O），C（O）O，C（O）NR ^ 6 ^或键; R ^ 2 ^表示氢，Ar或（CH〜2〜）〜p〜CH [（CH〜2〜）〜q〜R ^ 7 ^]（CH〜2〜）〜t〜R ^ 8 ^;或R ^ 2 ^和R ^ 6 ^一起表示（CH〜2〜）〜j〜Y（CH〜2〜）〜k〜; R ^ 3 ^和R ^ 5 ^独立代表氢，卤素或C〜1〜-C〜4〜烷基; X代表氧或NH; R ^ 4 ^代表氢，C〜1〜-C 〜4〜烷基（CH〜2〜）〜u〜Ar，R ^ 9 ^ CO或R ^ 9 ^ SO〜2〜; R ^ 6 ^代表氢，C〜1〜-C〜4〜烷基，芳基或杂芳基，或R ^ 2 ^和R ^ 6 ^共同表示（ CH〜2〜）〜j〜Y（CH〜2〜）〜k〜; R ^ 7 ^和R ^ 8 ^独立代表氢或卤素，CN，-C <154> CH，N〜3〜，CF〜3〜，NO〜2〜，AR，OR ^ 10 ^，NR ^ 10 ^ R ^ 11 ^，C（O）OR ^ 10 ^，OC（O）R ^ 10 ^，C（O）NR ^ 10 ^ R ^ 11 ^，NR ^ 10 ^ C（O）R ^ 11 ^，SO 〜2〜NR ^ 10 ^ R ^ 11 ^，或NR ^ 10 ^ SO〜2〜R ^ 11 ^; R 9表示C〜1〜-C〜4〜烷基或Ar; Ar表示苯基，萘基或5-或6-元杂环，含有0-3个氮，0-1个硫和0-1个氧;空气任选地被一个或多个独立地选自以下的取代基取代：氢，卤素，C〜1〜-C〜4〜烷基，C〜2〜-C〜4〜烯基，C〜2〜-C〜4〜炔基，（CH〜2〜）〜n〜芳基，CN，NO〜2〜，CF〜3〜，OR ^ 12 ^，NR ^ 12 ^ R ^ 13 ^和COOR ^ 12 ^，R ^ 10 ^，R ^ 11 ^，R ^ 12 ^和R ^ 13 ^独立地表示氢，C〜1〜-C〜4〜烷基，芳基或杂芳基;或R ^ 10 ^和R ^ 11 ^和/或R ^ 12 ^和R ^ 13 ^一起独立地表示（CH〜2〜）〜j〜Y（CH〜2〜）〜k〜; Y代表氧，硫，NR ^ 14 ^或键; j是2-4; k，m，n，p，q，t和u独立为0-2; R ^ 14 ^^代表氢，C〜1〜C〜4〜烷基，芳基或杂芳基;对映异构体或对映异构体及其药学上可接受的盐，其制备方法，含有它们的药物组合物及其在治疗中的用途，特别是在治疗与烟碱传递降低有关的疾病中。本发明的化合物增加了对烟碱受体的激动剂的有效性。

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公开/公告号BR0015193A

专利类型
公开/公告日2002-06-18

原文格式PDF
申请/专利权人 ASTRAZENECA AB;
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申请/专利号BR20000015193
发明设计人 DAVID GURLEY;JAMES ROSAMOND;
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申请日2000-11-01
分类号C07D209/42;A61K31/404;A61K31/405;A61P25/00;
国家 BR
入库时间 2022-08-22 00:46:10

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