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公开(公告)号：US20120190721A1
公开(公告)日：2012-07-26
申请号：US13440284
申请日：2012-04-05
IPC分类号： A61K31/403 , A61P9/00 , A61P25/00
CPC分类号： A61K31/403
摘要： The present invention is directed to racemic 1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane, (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane, racemic 1-(4-methylphenyl)-3-azabicyclo[3.1.0]hexane, and (+)-1-(4-methylphenyl)-3-azabicyclo[3.1.0]hexane, and methods of their use for treating certain nervous system disorders and conditions, including, inter alia, vasomotor symptoms (VMS) and chronic pain.
摘要翻译： 本发明涉及外消旋的1-（3,4-二氯苯基）-3-氮杂双环[3.1.0]己烷，（+） - 1-（3,4-二氯苯基）-3-氮杂双环[3.1.0]己烷 ，外消旋的1-（4-甲基苯基）-3-氮杂双环[3.1.0]己烷和（+） - 1-（4-甲基苯基）-3-氮杂双环[3.1.0]己烷及其用于治疗 某些神经系统疾病和病症，尤其包括血管舒缩症状（VMS）和慢性疼痛。
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公开(公告)号：US5559120A
公开(公告)日：1996-09-24
申请号：US402571
申请日：1995-03-13
IPC分类号： A61K31/395 , A61K31/44 , A61K31/675 , C07D491/06 , C07D498/04 , C07D498/16
CPC分类号： A61K31/70
摘要： A compound of the structure ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10, A, B and Ar are all defined in the body of the specification or a pharmaceutically acceptable salt thereof which is useful as an immuno-suppressive, antiinflammatory, antifungal, antiprliferative and antitumor agent.
摘要翻译： 结构
的化合物，其中R1，R2，R3，R4，R5，R6，R7，R8，R9，R10，A，B和Ar均在本说明书的主体或其药学上可接受的盐中定义， 可用作免疫抑制，抗炎，抗真菌，抗增殖和抗肿瘤剂。 -
公开(公告)号：US5559119A
公开(公告)日：1996-09-24
申请号：US391399
申请日：1995-02-27
IPC分类号： A61K31/395 , A61K31/44 , A61K31/675 , C07D491/06 , C07D498/04 , C07D498/16
CPC分类号： A61K31/70
摘要： A compound of the structure ##STR1## wherein R and R.sup.1 are each, independently, hydrogen, ##STR2## R.sup.2 and R.sup.3 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, --CO.sub.2 R.sup.5, --COR.sup.5, --CN, --NO.sub.2, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --OR.sup.5, --SR.sup.5, or Ar;R.sup.4 is hydrogen, alkyl, alkenyl, alkynyl, --CF.sub.3, --NR.sup.5 R.sup.6, --CO.sub.2 R.sup.5, --COR.sup.5, CONR.sup.5 R.sup.6, --NO.sub.2, halogen, --OR.sup.5, --SR.sup.5, --CN, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --SO.sub.2 NR.sup.5 R.sup.6, or Ar;R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, or Ar; ##STR3## are each, independently, a 5-7 membered saturated, unsaturated, or partially unsaturated heterocyclic radical, that is optionally fused to a phenyl ring or a cycloalkane or cycloalkene ring, wherein the heterocyclic ring may optionally contain O, S, or NR.sup.8 in the heterocyclic ring, and may be optionally substituted by R.sup.7 ;R.sup.7 is alkyl of 1-6 carbon atoms, alkenyl, alkynyl, --CF.sub.3, --NR.sup.5 R.sup.6, --CO.sub.2 R.sup.5, --COR.sup.5, CONR.sup.5 R.sup.6, --NO.sub.2, halogen, --OR.sup.5, --SR.sup.5, --CN, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --SO.sub.2 NR.sup.5 R.sup.6, or Ar;R.sup.8 is hydrogen, alkyl, alkenyl, alkynyl, --CF.sub.3, --NR.sup.5 R.sup.6, --CO.sub.2 R.sup.5, --COR.sup.5, CONR.sup.5 R.sup.6, --OR.sup.5, --SR.sup.5, --CN, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --SO.sub.2 NR.sup.5 R.sup.6, or Ar;Ar is phenyl, naphthyl, or hetaryl, wherein the foregoing may be optionally substituted; with the proviso that R and R.sup.1 are both not hydrogen, or a pharmaceutically acceptable salt thereof, which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
摘要翻译： 结构式II的化合物，其中R和R 1各自独立地为氢，R 2和R 3各自独立地为氢，烷基，烯基，炔基，-CO 2 R 5，-COR 5，-CN ，-NO 2，-SO 2 R 5，-SO 3 R 5，-OR 5，-SR 5或Ar; R4是氢，烷基，烯基，炔基，-CF3，-NR5R6，-CO2R5，-COR5，CONR5R6，-NO2，卤素，-OR5，-SR5，-CN，-SO2R5，-SO3R5，-SO2NR5R6或Ar; R 5和R 6各自独立地为氢，烷基，烯基，炔基或Ar; 每个独立地是5-7元饱和的，不饱和的或部分不饱和的杂环基团，其任选地与苯环或环烷烃或环烯烃稠合，其中杂环可以任选地含有O， S或NR8，并且可以任选被R 7取代; R7是1-6个碳原子的烷基，烯基，炔基，-CF3，-NR5R6，-CO2R5，-COR5，CONR5R6，-NO2，卤素，-OR5，-SR5，-CN，-SO2R5，-SO3R5，-SO2NR5R6 ，或Ar; R 8是氢，烷基，烯基，炔基，-CF 3，-NR 5 R 6，-CO 2 R 5，-COR 5，CONR 5 R 6，-OR 5，-SR 5，-CN，-SO 2 R 5，-SO 3 R 5，-SO 2 NR 5 R 6或Ar; Ar是苯基，萘基或杂芳基，其中前述可以任选被取代; 条件是R和R 1都不是氢，或其药学上可接受的盐，其可用作免疫抑制，抗炎，抗真菌，抗增殖和抗肿瘤剂。
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公开(公告)号：US5532355A
公开(公告)日：1996-07-02
申请号：US395012
申请日：1995-02-27
IPC分类号： A61K31/395 , A61K31/44 , A61K31/675 , C07D491/06 , C07D498/04 , C07D498/16
CPC分类号： A61K31/70
摘要： A compound of the structure ##STR1## wherein R and R.sup.1 are each, independently, hydrogen, ##STR2## R.sup.2 and R.sup.3 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, --CO.sub.2 R.sup.5, --COR.sup.5, --CN, --NO.sub.2, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --OR.sup.5, --SR.sup.5, or Ar;R.sup.4 is hydrogen, alkyl, alkenyl, alkynyl, --CF.sub.3, --NR.sup.5 R.sup.6, --CO.sub.2 R.sup.5, --COR.sup.5, CONR.sup.5 R.sup.6, --NO.sub.2, halogen, --OR.sup.5, --SR.sup.5, --CN, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --SO.sub.2 NR.sup.5 R.sup.6 or Ar;R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, or Ar; ##STR3## are each, independently, a 5-7 membered saturated, unsaturated, or partially unsaturated heterocyclic radical, that is optionally fused to a phenyl ring or a cycloalkane or cycloalkene ring, wherein the heterocyclic ring may optionally contain O, S, or NR.sup.8 in the heterocyclic ring, and may be optionally substituted by R.sup.7 ;R.sup.7 is alkyl of 1-6 carbon atoms, alkenyl, alkynyl, --CF.sub.3, --NR.sup.5 R.sup.6, --CO.sub.2 R.sup.5, --COR.sup.5, CONR.sup.5 R.sup.6, --NO.sub.2, halogen, --OR.sup.5, --SR.sup.5, --CN, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --SO.sub.2 NR.sup.5 R.sup.6, or Ar;R.sup.8 is hydrogen, alkyl, alkenyl, alkynyl, --CF.sub.3, --NR.sup.5 R.sup.6, --CO.sub.2 R.sup.5, --COR.sup.5, CONR.sup.5 R.sup.6, --OR.sup.5, --SR.sup.5, --CN, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --SO.sub.2 NR.sup.5 R.sup.6, or Ar;Ar is phenyl, naphthyl, or hetaryl, wherein the foregoing may be optionally substituted; with the proviso that R and R.sup.1 are both not hydrogen, or a pharmaceutically acceptable salt thereof, which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
摘要翻译： 结构式II的化合物，其中R和R 1各自独立地为氢，R 2和R 3各自独立地为氢，烷基，烯基，炔基，-CO 2 R 5，-COR 5，-CN ，-NO 2，-SO 2 R 5，-SO 3 R 5，-OR 5，-SR 5或Ar; R4是氢，烷基，烯基，炔基，-CF3，-NR5R6，-CO2R5，-COR5，CONR5R6，-NO2，卤素，-OR5，-SR5，-CN，-SO2R5，-SO3R5，-SO2NR5R6或Ar; R 5和R 6各自独立地为氢，烷基，烯基，炔基或Ar; 各自独立地是5-7元饱和的，不饱和的或部分不饱和的杂环基，其任选地与苯环或环烷烃或环烯烃稠合，其中杂环可以任选地含有O，S或 NR8在杂环中，并且可以任选地被R 7取代; R7是1-6个碳原子的烷基，烯基，炔基，-CF3，-NR5R6，-CO2R5，-COR5，CONR5R6，-NO2，卤素，-OR5，-SR5，-CN，-SO2R5，-SO3R5，-SO2NR5R6 ，或Ar; R 8是氢，烷基，烯基，炔基，-CF 3，-NR 5 R 6，-CO 2 R 5，-COR 5，CONR 5 R 6，-OR 5，-SR 5，-CN，-SO 2 R 5，-SO 3 R 5，-SO 2 NR 5 R 6或Ar; Ar是苯基，萘基或杂芳基，其中前述可以任选被取代; 条件是R和R 1都不是氢，或其药学上可接受的盐，其可用作免疫抑制，抗炎，抗真菌，抗增殖和抗肿瘤剂。
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公开(公告)号：US5302584A
公开(公告)日：1994-04-12
申请号：US54655
申请日：1993-04-23
IPC分类号： A61K31/435 , A61K31/395 , A61K31/436 , A61K31/44 , A61K31/675 , A61K31/70 , A61P9/00 , A61P29/00 , A61P37/06 , C07D20060101 , C07D221/00 , C07D273/00 , C07D311/00 , C07D487/18 , C07D491/06 , C07D498/18 , C07H19/01 , C07J1/00
CPC分类号： A61K31/70
摘要： A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, --CONH--[(CR.sup.3 R.sup.4).sub.m (--A--(CR.sup.5 R.sup.6).sub.n).sub.p ].sub.q --B; ##STR2## R.sup.3, R.sup.4, R.sup.5, R.sup.6, and B are each, independently, hydrogen, alkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, arylalkyl, cycloalkyl, --OR.sup.7, --SR.sup.7, halogen, --CN, --NO.sub.2, --CF.sub.3, --COR.sup.7, --CO.sub.2 R.sup.7, --CONHR.sup.7, --SO.sub.2 R.sup.7, --OSO.sub.3 R.sup.7, --NR.sup.7 R.sup.8, --NHCOR.sup.7, --NHSO.sub.2 R.sup.7, or Ar;R.sup.7 and R.sup.8 are each, independently, hydrogen, alkyl, arylalkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, cycloalkyl;R.sup.9 and R.sup.10 are each, independently, alkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, arylalkyl, --CF.sub.3, --COR.sup.7, --CO.sub.2 R.sup.7, --CONHR.sup.7, --SO.sub.2 R.sup.7, or Ar;A is --CH.sub.2 --, --NR.sup.7 --, --O--, --S--, --SO--, --SO.sub.2 --, --PR.sup.7 --, --CO--, --NHCO--, --NHSO--, or --P(O)(R.sup.7)--;Ar is phenyl, naphthyl, pyridyl, quinolyl, isoquinolyl, quinoxalyl, thienyl, thionaphthyl, furyl, benzofuryl, benzodioxyl, benzoxazolyl, benzoisoxazolyl, indolyl, thiazolyl, isoxazolyl, pyrimidinyl, pyrazinyl, imidazolyl, benzopyranyl, benz[b]thiophenolyl, benzimidazolyl, benzthiazolyl, benzodioxolyl, piperidinyl, morpholinyl, piperazinyl, tetrahydrofuranyl, or pyrrolidinyl; wherein the Ar group may be optionally mono-, di-, or tri- substituted; ##STR3## is a nitrogen containing heterocycle that may be saturated, unsaturated, or partially unsaturated, and may be optionally mono-, di-, or tri- substituted; with the proviso that R.sup.1 and R.sup.2 are not both hydrogen;m=0-6;n=0-6;p=0-1;q=0-1;or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
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6.发明授权Use of aryl- and heteroaryl piperazinyl carboxamides in the treatment of various central nervous system disorders 失效芳基和杂芳基哌嗪基甲酰胺在治疗各种中枢神经系统疾病中的应用
公开(公告)号：US5278160A
公开(公告)日：1994-01-11
申请号：US848782
申请日：1992-03-10
IPC分类号： C07D209/42 , C07D239/42 , C07D295/13 , A61K31/50 , A61K31/495
CPC分类号： C07D239/42 , C07D209/42 , C07D295/13
摘要： There are disclosed the use of the compounds of the formula (I) ##STR1## wherein R.sup.1 is 1-adamantyl, 3-methyl-1-adamantyl, 3-noradamantyl, unsubstituted or substituted-2-indolyl, 3-indolyl, 2-benzofuranyl or 3-benzofuranyl wherein the substituents are selected from lower alkyl, lower alkoxy and halo; R.sup.2 is unsubstituted or substituted phenyl, benzyl, or pyrimidinyl wherein the substituents are selected from lower alkyl, lower alkoxy, trifluoromethyl and halo; R.sup.3 is H or lower alkyl of 1 to 3 carbon atoms; n is the integer 0 or 1; and m is the integer from 2 to 5 and the pharmaceutically acceptable salts thereof.
摘要翻译： 公开了式（I）化合物（I）的用途，其中R1是1-金刚烷基，3-甲基-1-金刚烷基，3-降金刚烷基，未取代的或取代的-2-吲哚基，3-吲哚基 2-苯并呋喃基或3-苯并呋喃基，其中取代基选自低级烷基，低级烷氧基和卤素; R2是未取代的或取代的苯基，苄基或嘧啶基，其中取代基选自低级烷基，低级烷氧基，三氟甲基和卤素; R3是H或1〜3个碳原子的低级烷基; n是整数0或1; 且m为2至5的整数及其药学上可接受的盐。
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7.发明授权Fused heterotricyclic imides with psychotropic activity and intermedrates thereof 失效融合的异三环酰亚胺具有精神活性及其中间体
公开(公告)号：US5053508A
公开(公告)日：1991-10-01
申请号：US491143
申请日：1990-03-09
IPC分类号： C07D307/93 , C07D495/04 , C07D498/08
CPC分类号： C07D495/04 , C07D307/93
摘要： There are disclosed compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 taken together represent ##STR2## R.sup.3 and R.sup.4 are hydrogen; R.sup.5 is 2-pyridinyl, 2-pyrazinyl, 2-pyrimidinyl, 3-pyridazinyl or any of the foregoing R.sup.5 moieties substituted by lower alkyl, lower alkoxy, halo lower alkyl, cyano, nitro or halo;X, Y and Z are, independently, N, S, O, NR.sup.6, SO, SO.sub.2, CR.sup.6 or CH.sub.2 ;A is lower alkylene, O or S;R.sup.6 is hydrogen, lower alkyl, aryl, aralkyl;m is 3-7;and the pharmaceutically acceptable salts thereof, and their use as antipsychotic/-anxiolytic agents having a low liability for extrapyramidal side effects.
摘要翻译： 公开了下式的化合物：其中R 1和R 2一起代表R 3和R 4是氢; R5是2-吡啶基，2-吡嗪基，2-嘧啶基，3-哒嗪基或由低级烷基，低级烷氧基，卤代低级烷基，氰基，硝基或卤素取代的前述R5部分中的任何一个; X，Y和Z独立地是N，S，O，NR6，SO，SO2，CR6或CH2; A是低级亚烷基，O或S; R6是氢，低级烷基，芳基，芳烷基; m为3-7; 及其药学上可接受的盐，以及它们作为对锥体束外副作用具有低负荷的抗精神病药/溶血性药物的用途。
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公开(公告)号：US4900835A
公开(公告)日：1990-02-13
申请号：US335076
申请日：1989-04-07
IPC分类号： C07D401/06 , C07D401/14
CPC分类号： C07D401/06 , C07D401/14
摘要： p is one of the integers 2, 3, 4 or 5;q is one of the integers 1, 2 or 3;and ##STR2## where R.sup.4 is hydrogen, alkyl, alkoxy or halo; or a pharmaceutically acceptable salt thereof are antipsychotic and anxiolytic agents.
摘要翻译：
其中虚线表示可选的不饱和度; p是整数2,3,4或5之一; q是整数1,2或3之一; 和其中R 4是氢，烷基，烷氧基或卤素的 或其药学上可接受的盐是抗精神病药和抗焦虑剂。 -
公开(公告)号：US4892943A
公开(公告)日：1990-01-09
申请号：US237106
申请日：1988-08-26
IPC分类号： C07D401/12 , C07D403/12
CPC分类号： C07D401/12 , C07D403/12
摘要： There are disclosed compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 represent the structure ##STR2## R.sup.3 and R.sup.4 are hydrogen, or R.sup.3 and R.sup.4 taken together form a 3-5 membered saturated carbocyclic ring;R.sup.5 and R.sup.6 are hydrogen, or R.sup.5 and R.sup.6 taken together form a 3-6 membered carbocyclic ring or a cyclobutenyl ring; with the proviso that when R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are hydrogen, n is other than zero;m is 2-4;n is 0-4;X is lower alkylene, vinylene or O;R.sup.7 is unsubstituted or substituted phenyl, 2-pyridinyl, 2-pyrimidinyl, 2-pyrazinyl or 3-pyridazinyl; where the substituents are selected from the group lower alkyl, lower alkoxy, halo, cyano, nitro and trifluoromethyl;and the pharmaceutically acceptable salts thereof and their use as antipsychotic/anxiolytic agents having a low liability for extrapyramidal side effects.
摘要翻译： 公开了下式的化合物：其中R 1和R 2表示结构，R 3和R 4是氢，或者R 3和R 4一起形成3-5元饱和碳环; R5和R6是氢，或R5和R6一起形成3-6元碳环或环丁烯基环; 条件是当R3，R4，R5和R6是氢时，n不为0; m为2-4; n为0-4; X是低级亚烷基，亚乙烯基或O; R7是未取代或取代的苯基，2-吡啶基，2-嘧啶基，2-吡嗪基或3-哒嗪基; 其中取代基选自低级烷基，低级烷氧基，卤素，氰基，硝基和三氟甲基; 及其药学上可接受的盐及其作为锥体束外副作用负担低的抗精神病药/抗焦虑剂的用途。
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公开(公告)号：US4882432A
公开(公告)日：1989-11-21
申请号：US294853
申请日：1989-01-09
IPC分类号： C07D239/42 , C07D295/13
CPC分类号： C07D239/42 , C07D295/13
摘要： The compounds of the formula: ##STR1## wherein Ad is 1-adamantyl, 2-adamantyl or 3-noradamantyl; X is --O-- or ##STR2## n is 1,2,3 or 4; R.sup.1 and R.sup.2 are, independently, hydrogen, alkyl, phenyl, benzyl, or substituted phenyl or benzyl in which the substituent is alkyl, alkoxy, halo, cyano, nitro or trifluoromethyl; and R.sup.3 is phenyl, benzyl or substituted phenyl or benzyl in which the substituent is alkyl, alkoxy, halo, nitro, cyano or perhalomethyl, 2-, 3-, or 4-pyridinyl, 2-, 4-or 5-pyrimidiny; or 2- or 3-pyrazinyl; R.sup.4 and R.sup.5 are independently, hydrogen, methyl, phenyl or benzyl; or a pharmaceutically acceptable salt thereof, are useful anxiolytic/antidepressant agents, with elements of antipsychotic activity.
摘要翻译： 下式的化合物：其中Ad是1-金刚烷基，2-金刚烷基或3-降金刚烷基; X为-O-或
n为1,2,3或4; R 1和R 2独立地是氢，烷基，苯基，苄基或取代的苯基或苄基，其中取代基是烷基，烷氧基，卤素，氰基，硝基或三氟甲基; R 3是苯基，苄基或取代的苯基或苄基，其中取代基是烷基，烷氧基，卤素，硝基，氰基或全卤代甲基，2-，3-或4-吡啶基，2-，4-或5-嘧啶基; 或2-或3-吡嗪基; R4和R5独立地是氢，甲基，苯基或苄基; 或其药学上可接受的盐是具有抗精神病活性成分的抗焦虑/抗抑郁药。
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