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1. 发明授权

US5424322A A personality disorder treatment method and composition 失效
标题翻译：人格障碍治疗方法及组成
公开(公告)号：US5424322A
公开(公告)日：1995-06-13
申请号：US38427
申请日：1993-03-25
申请人： Richard C. Effland , Joseph T. Klein , Lawrence L. Martin
发明人： Richard C. Effland , Joseph T. Klein , Lawrence L. Martin
IPC分类号： C07D401/12 , C07D409/12 , C07D417/12 , A61K31/44
CPC分类号： C07D401/12 , C07D409/12 , C07D417/12
摘要： This invention relates to compositions of substituted pyridinylamino-1H-indoles of the formula ##STR1## wherein Q is N or NR.sub.2 ;Y is CHR.sub.1 is hydrogen, loweralkyl, loweralkynyl, loweralkenyl, arylloweralkyl, loweralkoxycarbonylaminoloweralkylcarbonyl, arylloweralkoxycarbonylaminoloweralkylcarbonyl, aminoloweralkylcarbonyl, loweralkoxycarbonyl or acyl;R.sub.2 is hydrogen or loweralkyl;R.sub.3 is hydrogen or loweralkyl;X is hydrogen, loweralkyl, halogen; andn is 0 or 1 with utility in the treatment of personality disorders as obsessive compulsive disorders.
摘要翻译：本发明涉及式（I）的取代吡啶基氨基-1H-吲哚的组合物，其中Q是N或NR2; Y是CHR 1是氢，低级烷基，低级炔基，低级烯基，芳基低级烷基，低级烷氧基羰基氨基低级烷基羰基，芳基低级烷基羰基，低级烷氧基羰基或酰基。 R2是氢或低级烷基; R3是氢或低级烷基; X是氢，低级烷基，卤素; n为0或1，可用于治疗人格障碍作为强迫症。

2. 发明授权

US5229401A Substituted pyridinylamino benzo[b]thiophene compounds 失效
标题翻译：取代的吡啶基氨基苯并[b]噻吩化合物
公开(公告)号：US5229401A
公开(公告)日：1993-07-20
申请号：US925842
申请日：1992-08-07
申请人： Richard C. Effland , Joseph T. Klein , Lawrence L. Martin
发明人： Richard C. Effland , Joseph T. Klein , Lawrence L. Martin
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： This invention relates to substituted pyridinylamino-1H-indoles, 1H-indazoles, 2H-indazoles, benzo[b]thiophenes and 1,2-benzisothiazoles of the formula ##STR1## wherein Q is S, N or NR.sub.2 ;Y is CH, N or NR.sub.2 ;R.sub.1 is hydrogen, loweralkyl, loweralkynyl, loweralkenyl, arylloweralkyl, loweralkoxycarbonylaminoloweralkylcarbonyl, arylloweralkoxycarbonylaminoloweralkylcarbonyl, aminoloweralkylcarbonyl, loweralkoxycarbonyl or acyl;R.sub.2 is hydrogen or loweralkyl;R.sub.3 is hydrogen or loweralkyl;X is hydrogen, loweralkyl, halogen; andn is 0 or 1; or a pharmaceutically acceptable acid addition salt thereof.The compounds of this invention are useful in the treatment of memory dysfunctions characterized by a cholinergic deficit such as the type associated with Alzhemier's disease and other memory disorders.Compounds of this invention also have utility as modulators of neurotransmitter function such as noradrenergic and serotonergic and as such are useful for treatment of depression and personality disorders such as obsessive compulsive disorders.Additionally, compounds of this invention are useful as topical antiinflammatory agents for the treatment of various dermatoses.
摘要翻译：本发明涉及式（I）的取代吡啶基氨基-1H-吲哚，1H-吲唑，2H-吲唑，苯并[b]噻吩和1,2-苯并异噻唑，其中Q是S，N或NR2; Y是CH，N或NR2; R 1是氢，低级烷基，低级炔基，低级烯基，芳基低级烷基，低级烷氧基羰基氨基低级烷基羰基，芳基低级烷基羰基，低级烷氧基羰基或酰基。 R2是氢或低级烷基; R3是氢或低级烷基; X是氢，低级烷基，卤素; 并且n为0或1; 或其药学上可接受的酸加成盐。本发明的化合物可用于治疗以胆碱能缺乏为特征的记忆功能障碍，例如与Alzhemier氏病和其他记忆障碍相关的类型。本发明的化合物还可用作神经递质功能的调节剂，例如去甲肾上腺素能和5-羟色胺能，因此可用于治疗抑郁症和人格障碍，例如强迫症。此外，本发明的化合物可用作治疗各种皮肤病的局部抗炎剂。

3. 发明授权

US5519032A Substituted aminothienopyridines, pharmaceutical composition and use 失效
公开(公告)号：US5519032A
公开(公告)日：1996-05-21
申请号：US132731
申请日：1993-10-06
申请人： Richard C. Effland , Joseph T. Klein , Lawrence L. Martin
发明人： Richard C. Effland , Joseph T. Klein , Lawrence L. Martin
IPC分类号： A61K31/40 , A61K31/435 , A61P1/08 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P43/00 , C07D495/04 , A61K31/44
CPC分类号： C07D495/04
摘要： This application relates to compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, m and n are as defined in the specification which are useful as modulators of neurotransmitter function such as serotonergic and adrenergic, and as such are useful as antidepressants, anxiolytics, atypical antipsychotics, antiemetics, and for the treatment of personality disorders such as obsessive compulsive disorders. Certain of the compounds are also useful as glycine partial agonists.

4. 发明授权

US5328920A Substituted (pyridinylamino)-indoles 失效
标题翻译：取代（吡啶基氨基） - 吲哚
公开(公告)号：US5328920A
公开(公告)日：1994-07-12
申请号：US964546
申请日：1992-10-21
申请人： Richard C. Effland , Joseph T. Klein , Lawrence L. Martin , Gregory M. Shutske , Kevin J. Kapples , John D. Tomer, IV
发明人： Richard C. Effland , Joseph T. Klein , Lawrence L. Martin , Gregory M. Shutske , Kevin J. Kapples , John D. Tomer, IV
IPC分类号： A61K31/44 , A61K31/423 , A61K31/428 , A61K31/4427 , A61K31/4433 , A61K31/47 , A61P1/08 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , C07D401/12 , C07D401/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12
CPC分类号： C07D413/12 , C07D401/12 , C07D409/12 , C07D413/10 , C07D417/12
摘要： There are disclosed various compounds of the formula below, ##STR1## where R, R.sub.1, W, X, Y and Z are as defined in the specification; which are useful for alleviating various memory dysfunctions such as Alzheimer's disease, as modulators of neurotransmitter functions such as serotonergic and adrenergic, and as such are useful as antidepressants, anxiolytics, atypical antipsychotics, antiemetics, and for the treatment of personality disorders such as obsessive compulsive disorder.
摘要翻译：公开了下式的各种化合物，其中R，R 1，W，X，Y和Z如说明书中所定义; 其可用于缓解诸如阿尔茨海默病的各种记忆功能障碍，作为神经递质功能如5-羟色胺能和肾上腺素能的调节剂，并且因此可用作抗抑郁药，抗焦虑药，非典型抗精神病药，止吐药和用于治疗人格障碍如强迫症紊乱。

5. 发明授权

US5252581A Substituted aminothienopyridines, pharmaceutical composition and use 失效
标题翻译：取代氨基噻吩并吡啶类，药物组成及用途
公开(公告)号：US5252581A
公开(公告)日：1993-10-12
申请号：US917247
申请日：1992-07-20
申请人： Richard C. Effland , Joseph T. Klein , Lawrence L. Martin
发明人： Richard C. Effland , Joseph T. Klein , Lawrence L. Martin
IPC分类号： A61K31/40 , A61K31/435 , A61P1/08 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P43/00 , C07D495/04 , A61K31/44 , C07D213/28
CPC分类号： C07D495/04
摘要： This application relates to compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, m and n are as defined in the specification which are useful as modulators of neurotransmitter function such as serotonergic and adrenergic, and as such are useful as antidepressants, anxiolytics, atypical antipsychotics, antiemetics, and for the treatment of personality disorders such as obsessive compulsive disorders. Certain of the compounds are also useful as glycine partial agonists.

6. 发明授权

US5631270A Substituted pyridinylamino-1H-indoles, 1H-indazoles, 2H-indazoles, benzo [b ] 失效
标题翻译：取代的吡啶基氨基-1H-吲哚，1H-吲唑，2H-吲唑，苯并[b]噻吩和1,2-苯并异噻唑
公开(公告)号：US5631270A
公开(公告)日：1997-05-20
申请号：US464994
申请日：1995-06-05
申请人： Richard C. Effland , Joseph T. Klein , Lawrence L. Martin
发明人： Richard C. Effland , Joseph T. Klein , Lawrence L. Martin
IPC分类号： C07D401/12 , C07D409/12 , C07D417/12 , A61K31/44 , A61K31/38 , A61K31/405 , A61K31/415
CPC分类号： C07D401/12 , C07D409/12 , C07D417/12
摘要： This invention relates to substituted pyridinylamino-1H-indoles, 1H-indazoles, 2H-indazoles, benzo[b]thiophenes and 1,2-benzisothiazoles of the formula ##STR1## wherein Q is S, N or NR.sub.2 ;Y is CH, N or NR.sub.2 ;R.sub.1 is hydrogen, loweralkyl, loweralkynyl, loweralkenyl, arylloweralkyl, loweralkoxycarbonylaminoloweralkylcarbonyl, arylloweralkoxycarbonylaminoloweralkylcarbonyl, aminoloweralkylcarbonyl, loweralkoxycarbonyl or acyl;R.sub.2 is hydrogen or loweralkyl;R.sub.3 is hydrogen or loweralkyl;X is hydrogen, loweralkyl, halogen; andn is 0 or 1;or a pharmaceutically acceptable acid addition salt thereof that are useful in the treatment of memory dysfunctions.
摘要翻译：本发明涉及式（I）的取代吡啶基氨基-1H-吲哚，1H-吲唑，2H-吲唑，苯并[b]噻吩和1,2-苯并异噻唑，其中Q是S，N或NR2; Y是CH，N或NR2; R 1是氢，低级烷基，低级炔基，低级烯基，芳基低级烷基，低级烷氧基羰基氨基低级烷基羰基，芳基低级烷基羰基，低级烷氧基羰基或酰基。 R2是氢或低级烷基; R3是氢或低级烷基; X是氢，低级烷基，卤素; 并且n为0或1; 或其药学上可接受的酸加成盐，其可用于记忆功能障碍的治疗。

7. 发明授权

US5328918A Substituted pyridinylamino 1H-indazoles 失效
标题翻译：取代的吡啶基氨基1H-吲唑
公开(公告)号：US5328918A
公开(公告)日：1994-07-12
申请号：US38317
申请日：1993-03-25
申请人： Richard C. Effland , Joseph T. Klein , Lawrence L. Martin
发明人： Richard C. Effland , Joseph T. Klein , Lawrence L. Martin
IPC分类号： A61K31/44 , A61K31/00 , A61K31/4427 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61P17/00 , A61P25/18 , A61P25/24 , A61P25/26 , A61P25/28 , A61P29/00 , C07D401/12 , C07D409/12 , C07D417/12
CPC分类号： C07D401/12
摘要： This invention relates to substituted pyridinylamino-1H-indoles, 1H-indazoles, 2H-indazoles, benzo[b]thiophenes and 1,2-benzisothiazoles of the formula ##STR1## wherein Q is S, N or NR.sub.2 ;Y is CH, N or NR.sub.2 ;R.sub.1 is hydrogen, loweralkyl, loweralkynyl, loweralkenyl, arylloweralkyl, loweralkoxycarbonylaminoloweralkylcarbonyl, arylloweralkoxycarbonylaminoloweralkylcarbonyl, aminoloweralkylcarbonyl, loweralkoxycarbonyl or acyl;R.sub.2 is hydrogen or loweralkyl;R.sub.3 is hydrogen or loweralkyl;X is hydrogen, loweralkyl, halogen; andn is 0 or 1; or a pharmaceutically acceptable acid addition salt thereof.The compounds of this invention are useful in the treatment of memory dysfunctions characterized by a cholinergic deficit such as the type associated with Alzheimer's disease and other memory disorders.Compounds of this invention also have utility as modulators of neurotransmitter function such as noradrenergic and serotonergic and as such are useful for treatment of depression and personality disorders such as obsessive compulsive disorders.Additionally, compounds of this invention are useful as topical antiinflammatory agents for the treatment of various dermatoses.
摘要翻译：本发明涉及式（I）的取代吡啶基氨基-1H-吲哚，1H-吲唑，2H-吲唑，苯并[b]噻吩和1,2-苯并异噻唑，其中Q是S，N或NR2; Y是CH，N或NR2; R 1是氢，低级烷基，低级炔基，低级烯基，芳基低级烷基，低级烷氧基羰基氨基低级烷基羰基，芳基低级烷基羰基，低级烷氧基羰基或酰基。 R2是氢或低级烷基; R3是氢或低级烷基; X是氢，低级烷基，卤素; 并且n为0或1; 或其药学上可接受的酸加成盐。本发明的化合物可用于治疗以胆碱能缺乏为特征的记忆功能障碍，例如与阿尔茨海默病和其他记忆障碍相关的类型。本发明的化合物还可用作神经递质功能的调节剂，例如去甲肾上腺素能和5-羟色胺能，因此可用于治疗抑郁症和人格障碍，例如强迫症。此外，本发明的化合物可用作治疗各种皮肤病的局部抗炎剂。

8. 发明授权

US5246947A Substituted pyridinylamino-1,2-benzisothiazoles and their use for treating depression 失效
标题翻译：取代的吡啶基氨基-1,2-苯并异噻唑及其用于治疗抑郁症的用途
公开(公告)号：US5246947A
公开(公告)日：1993-09-21
申请号：US925822
申请日：1992-08-07
申请人： Richard C. Effland , Joseph T. Klein , Lawrence L. Martin
发明人： Richard C. Effland , Joseph T. Klein , Lawrence L. Martin
IPC分类号： C07D401/12 , C07D409/12 , C07D417/12
CPC分类号： C07D401/12 , C07D409/12 , C07D417/12
摘要： This invention relates to substituted pyridinylamino-1H-indoles, 1H-indazoles, 2H-indazoles, benzo[b]thiophenes and 1,2-benzisothiazoles of the formula ##STR1## wherein Q is S, N or NR.sub.2 ;Y is CH, N or NR.sub.2 ;R.sub.1 is hydrogen, loweralkyl, loweralkynyl, loweralkenyl, arylloweralkyl, loweralkoxycarbonylaminoloweralkylcarbonyl, arylloweralkoxycarbonylaminoloweralkylcarbonyl, aminoloweralkylcarbonyl, loweralkoxycarbonyl or acyl;R.sub.2 is hydrogen or loweralkyl;R.sub.3 is hydrogen or loweralkyl;X is hydrogen, loweralkyl, halogen; andn is 0 or 1; or a pharmaceutically acceptable acid addition salt thereof.The compounds of this invention are useful in the treatment of memory dysfunctions characterized by a cholinergic deficit such as the type associated with Alzheimer's disease and other memory disorders.Compounds of this invention also have utility as modulators of neurotransmitter function such as noradrenergic and serotonergic and as such are useful for treatment of depression and personality disorders such as obsessive compulsive disorders.Additionally, compounds of this invention are useful as topical antiinflammatory agents for the treatment of various dermatoses.
摘要翻译：本发明涉及式（I）的取代吡啶基氨基-1H-吲哚，1H-吲唑，2H-吲唑，苯并[b]噻吩和1,2-苯并异噻唑，其中Q是S，N或NR2; Y是CH，N或NR2; R 1是氢，低级烷基，低级炔基，低级烯基，芳基低级烷基，低级烷氧基羰基氨基低级烷基羰基，芳基低级烷基羰基，低级烷氧基羰基或酰基。 R2是氢或低级烷基; R3是氢或低级烷基; X是氢，低级烷基，卤素; 并且n为0或1; 或其药学上可接受的酸加成盐。本发明的化合物可用于治疗以胆碱能缺乏为特征的记忆功能障碍，例如与阿尔茨海默病和其他记忆障碍相关的类型。本发明的化合物还可用作神经递质功能的调节剂，例如去甲肾上腺素能和5-羟色胺能，因此可用于治疗抑郁症和人格障碍，例如强迫症。此外，本发明的化合物可用作治疗各种皮肤病的局部抗炎剂。

9. 发明授权

US5185350A Substituted pyridinylamino-1H-indoles,1H-indazoles,2H-indazoles, benzo (B)thiophenes and 1,2-benzisothiazoles 失效
标题翻译：取代的吡啶基氨基-1H-吲哚，1H-茚满，2H-茚满，苯并（B）噻吩和1,2-苄基双
公开(公告)号：US5185350A
公开(公告)日：1993-02-09
申请号：US764031
申请日：1991-09-23
申请人： Richard C. Effland , Joseph T. Klein , Lawrence L. Martin
发明人： Richard C. Effland , Joseph T. Klein , Lawrence L. Martin
IPC分类号： A61K31/44 , A61K31/00 , A61K31/4427 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61P17/00 , A61P25/18 , A61P25/24 , A61P25/26 , A61P25/28 , A61P29/00 , C07D401/12 , C07D409/12 , C07D417/12
CPC分类号： C07D401/12
摘要： This invention relates to substituted pyridinylamino-1H-indoles, 1H-indazoles, 2H-indazoles, benzo[b]thiophenes and 1,2-benzisothiazoles of the formula ##STR1## wherein Q is S, N or NR.sub.2 ;Y is CH, N or NR.sub.2 ;R.sub.1 is hydrogen, loweralkyl, loweralkynyl, loweralkenyl, arylloweralkyl, loweralkoxycarbonylaminoloweralkylcarbonyl, arylloweralkoxycarbonylaminoloweralkylcarbonyl, aminoloweralkylcarbonyl, loweralkoxycarbonyl or acyl;R.sub.2 is hydrogen or loweralkyl;R.sub.3 is hydrogen or loweralkyl;X is hydrogen, loweralkyl, halogen; andn is 0 or 1; or a pharmaceutically acceptable acid addition salt thereof.The compounds of this invention are useful in the treatment of memory dysfunctions characterized by a cholinergic deficit such as the type associated with Alzheimer's disease and other memory disorders.Compounds of this invention also have utility as modulators of neurotransmitter function such as noradrenergic and serotonergic and as such are useful for treatment of depression and personality disorders such as obsessive compulsive disorders.Additionally, compounds of this invention are useful as topical antiinflammatory agents for the treatment of various dermatoses.

10. 发明授权

US5177088A Substituted 3-(pyridinylamino)-indoles 失效
标题翻译：取代的3-（吡啶基氨基） - 吲哚
公开(公告)号：US5177088A
公开(公告)日：1993-01-05
申请号：US688964
申请日：1991-04-17
申请人： Richard C. Effland , Joseph T. Klein , Lawrence L. Martin
发明人： Richard C. Effland , Joseph T. Klein , Lawrence L. Martin
IPC分类号： A61K31/44 , A61K31/4427 , A61K31/4433 , A61K31/47 , A61P1/08 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , C07D401/12 , C07D401/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12
CPC分类号： C07D401/12 , C07D409/12 , C07D413/10 , C07D417/12
摘要： There are disclosed various compounds of the formula below, ##STR1## where R.sub.1, W, X, Y and Z are as defined in the specification; which are useful for alleviating various memory dysfunctions such as Alzheimer's disease, as modulators of neurotransmitter function such as serotonergic and adrenergic, and as such are useful as antidepressants, anxiolytics, atypical antipsychotics, antiemetics, and for the treatment of personality disorders such as obsessive compulsive disorders.

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