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71. 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.

72. 发明授权

US5179204A N-substituted-4-pyrimidinamines and pyrimidinediamines 失效
标题翻译： N-取代-4-嘧啶胺和嘧啶二胺
公开(公告)号：US5179204A
公开(公告)日：1993-01-12
申请号：US584554
申请日：1990-09-18
申请人： Richard C. Effland , Joseph T. Klein , Larry Davis , Gordon E. Olsen
发明人： Richard C. Effland , Joseph T. Klein , Larry Davis , Gordon E. Olsen
IPC分类号： C07D403/12 , C07D403/14
CPC分类号： C07D403/12 , C07D403/14
摘要： This invention relates to N-heteroaryl-4-pyrimidinamines of the formula ##STR1## where R.sub.1 is hydrogen, loweralkyl, aryl, or arylloweralkyl; R.sub.2 and R.sub.3 are independently hydrogen or loweralkyl, or R.sub.2 and R.sub.3 taken together are aryl; R.sub.4 and R.sub.5 are independently hydrogen or loweralkyl, or R.sub.4 and R.sub.5 taken together are aryl; X is hydrogen, halogen, cyano, nitro, amino, loweralkyl, loweralkoxy, trifluoromethyl or ##STR2## where Y is hydrogen, halogen or loweralkyl; m is an integer of 1 to 3; and the pharmaceutically acceptable acid addition salts thereof and where applicable the geometrical and optical isomers and racemic mixtures thereof. The compounds of this invention display utility as memory enhancing agents and as analgesic agents.
摘要翻译：本发明涉及式（I）的N-杂芳基-4-嘧啶胺，其中R 1是氢，低级烷基，芳基或芳基低级烷基; R2和R3独立地是氢或低级烷基，或R2和R3一起是芳基; R4和R5独立地是氢或低级烷基，或R4和R5一起是芳基; X是氢，卤素，氰基，硝基，氨基，低级烷基，低级烷氧基，三氟甲基或者其中Y是氢，卤素或低级烷基; m为1〜3的整数。和其药学上可接受的酸加成盐，并且在适用的情况下，其几何和旋光异构体及其外消旋混合物。本发明的化合物显示效用作为记忆增强剂和止痛剂。

73. 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.

74. 发明授权

US5095019A 4-substituted dihydropyrido(4,3-D)pyrimidines as analgesics and topical antiinflammatory agents for the treatment of skin disorders 失效
标题翻译： 4-取代二氢吡啶（4,3-D）嘧啶作止痛剂和用于治疗皮肤病症的局部抗炎剂
公开(公告)号：US5095019A
公开(公告)日：1992-03-10
申请号：US740171
申请日：1991-08-05
申请人： Richard C. Effland , Joseph T. Klein
发明人： Richard C. Effland , Joseph T. Klein
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： There are described compounds of the formula ##STR1## where R.sub.1 is hydrogen, loweralkyl, arylloweralkyl or aryl;R.sub.2 when present is hydrogen, loweralkyl, arylloweralkyl; andR.sub.3 is hydrogen, loweralkyl, cycloalkyl or aryl;which compounds are useful as analgesics and topical antiinflammatory agents for the treatment of skin disorders.
摘要翻译：描述了式“IMAGE”的化合物，其中R 1是氢，低级烷基，芳基低级烷基或芳基; 当存在时，R 2为氢，低级烷基，芳基低级烷基; 并且R 3是氢，低级烷基，环烷基或芳基; 哪些化合物可用作止痛剂和用于治疗皮肤病症的局部抗炎剂。

75. 发明授权

US5059688A 1-aryloxy-2,3,4,5-tetrahydro-3-benzazepine preparation 失效
标题翻译： 1-芳氧基-2,3,4,5-四氢-3-苯并氮杂制剂
公开(公告)号：US5059688A
公开(公告)日：1991-10-22
申请号：US513400
申请日：1990-04-23
申请人： Richard C. Effland , Joseph T. Klein , Larry Davis
发明人： Richard C. Effland , Joseph T. Klein , Larry Davis
IPC分类号： C07D223/16
CPC分类号： C07D223/16
摘要： The invention relates to 1-aryloxy-2,3,4,5-tetrahydro-3-benzazepines of the formula ##STR1## wherein Y is the same or different and is hydrogen and lower alkoxy; X is hydrogen, halogen, lower alkyl, lower alkoxy, CF.sub.3, No.sub.2, CN and NH.sub.2 ; R is hydrogen, lower alkyl, cycloalkyllower alkyl, ##STR2## Ar lower alkyl of the formula ##STR3## where Z is hydrogen, lower alkyl, lower alkoxy, halogen CF.sub.3, NO.sub.2 and NH.sub.2 ; Aryloxy lower alkyl of the formula ##STR4## where Z is as previously defined; and an alkylene amine of the formula ##STR5## where R.sub.1 and R.sub.2 are the same or different and are hydrogen and lower alkyl, n is an integer of 1 or 2; and the pharmaceutically acceptable acid addition salts thereof.
摘要翻译：本发明涉及式（I）的1-芳氧基-2,3,4,5-四氢-3-苯并吖庚因，其中Y相同或不同，为氢和低级烷氧基; X是氢，卤素，低级烷基，低级烷氧基，CF 3，NO 2，CN和NH 2; R是氢，低级烷基，环烷基低级烷基，其中Z是氢，低级烷基，低级烷氧基，卤素，CF 3，NO 2和NH 2; 其中Z如前所定义的式“IMAGE”的芳氧基低级烷基; 和式“IMAGE”的亚烷基胺，其中R 1和R 2相同或不同，为氢和低级烷基，n为1或2的整数; 及其药学上可接受的酸加成盐。

76. 发明授权

US5039811A Preparation of N-(pyridinyl)-1H-indol-1-amines 失效
标题翻译： N-（吡啶基）-1H-吲哚-1-胺的制备
公开(公告)号：US5039811A
公开(公告)日：1991-08-13
申请号：US571473
申请日：1990-08-23
申请人： Richard C. Effland , Joseph T. Klein , Larry Davis , Gordon E. Olsen
发明人： Richard C. Effland , Joseph T. Klein , Larry Davis , Gordon E. Olsen
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： There are disclosed compounds of the formula, ##STR1## wherein m, n, p, R, R.sub.1, R.sub.2 and R.sub.3 are as defined in the specification; which compounds are useful for enhancing memory and also as analgesic and antidepressant agents.
摘要翻译：公开了下式的化合物，其中m，n，p，R，R 1，R 2和R 3如说明书中所定义; 哪些化合物可用于增强记忆力，也可用作镇痛药和抗抑郁药。

77. 发明授权

US5034403A Heteroarylamino-and heteroaryloxypyridinamines and related compounds 失效
标题翻译：杂芳基氨基和杂芳氧基吡啶胺及相关化合物
公开(公告)号：US5034403A
公开(公告)日：1991-07-23
申请号：US603086
申请日：1990-10-25
申请人： Richard C. Effland , Joseph T. Klein , Gordon E. Olsen , Larry Davis , Russell R. L. Hamer , Brian S. Freed
发明人： Richard C. Effland , Joseph T. Klein , Gordon E. Olsen , Larry Davis , Russell R. L. Hamer , Brian S. Freed
IPC分类号： C07D213/74 , C07D213/89 , C07D401/12 , C07D403/12
CPC分类号： C07D213/74 , C07D213/89 , C07D401/12 , C07D403/12
摘要： There are described compounds of the formula ##STR1## where n is 0 or 1;X is O or NR.sub.2, R.sub.2 being hydrogen, lowerallkyl or loweralkylcarbonyl;R is hydrogen, loweralkyl, arylloweralkyl or loweralkylcarbonyl; andR.sub.1 is ##STR2## wherein R.sub.3 is hydrogen, loweralkyl or loweralkylcarbonyl; m is 1 or 2; each R.sub.4 is independently hydrogen or loweralkyl; and Y is hydrogen, halogen, loweralkyl, loweralkoxy or trifluoromethyl; which compounds are useful as topical antiinflammatory agents for the treatment of various dermatoses.
摘要翻译：描述式为“IMAGE”的化合物，其中n为0或1; X是O或NR 2，R 2是氢，低级烷基或低级烷基羰基; R是氢，低级烷基，芳基低级烷基或低级烷基羰基; R1是其中R3是氢，低级烷基或低级烷基羰基; m为1或2; 每个R 4独立地是氢或低级烷基; Y为氢，卤素，低级烷基，低级烷氧基或三氟甲基; 哪些化合物可用作治疗各种皮肤病的局部抗炎剂。

78. 发明授权

US4959378A Aminopyridinylaminophenol compounds useful as topical antiinflammatory agents for the treatment of skin disorders 失效
标题翻译：氨基吡啶基氨基苯酚化合物可用作治疗皮肤病症的局部抗炎药
公开(公告)号：US4959378A
公开(公告)日：1990-09-25
申请号：US425713
申请日：1989-10-24
申请人： Richard C. Allen , Joseph T. Klein , Richard C. Effland
发明人： Richard C. Allen , Joseph T. Klein , Richard C. Effland
IPC分类号： C07D213/76 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61P17/00 , A61P37/08 , C07D213/74 , C07D213/75 , C07D213/89
CPC分类号： C07D213/74 , C07D213/75 , C07D213/89
摘要： There are described compounds of the formula ##STR1## where R is hydrogen, loweralkyl, arylloweralkyl or loweralkylcarbonyl;R.sub.1 is hydrogen, loweralkyl or loweralkylcarbonyl; andn is 0 or 1;which compounds are useful as topical antiinflammatory agents for the treatment of various dermatoses.

79. 发明授权

US4868190A N-pyridinyl-9H-carbazol-9-amines 失效
标题翻译： N-吡啶基-9H-咔唑-9-胺
公开(公告)号：US4868190A
公开(公告)日：1989-09-19
申请号：US289887
申请日：1988-12-27
申请人： Richard C. Effland , Joseph T. Klein , Larry Davis , Gordon E. Olsen
发明人： Richard C. Effland , Joseph T. Klein , Larry Davis , Gordon E. Olsen
IPC分类号： A61K31/00 , A61K31/44 , A61K31/4427 , A61P25/04 , A61P25/24 , A61P25/26 , A61P25/28 , C07D401/12 , C07D401/14
CPC分类号： C07D401/12 , C07D401/14
摘要： There are described compounds of the formula: ##STR1## where, X is hydrogen, loweralkyl, loweralkoxy or halogen;Y is hydrogen, loweralkyl or halogen;Z is hydrogen, loweralkyl or halogen;R is hydrogen, loweralkyl, loweralkenyl, loweralkylcarbonyl, dimethylaminoloweralkyl or ##STR2## m being an integer of 1 to 6, with the proviso that when R is loweralkenyl the double bond is not alpha to the nitrogen atom;which compounds are useful analgesic, anticonvulsant and antidepressant agents, and for treating various memory dysfunctions characterized by decreased cholinergic function such as Alzheimer's disease.
摘要翻译：描述下式的化合物：其中X是氢，低级烷基，低级烷氧基或卤素; Y是氢，低级烷基或卤素; Z是氢，低级烷基或卤素; R是氢，低级烷基，低级烯基，低级烷基羰基，二甲基氨基低级烷基或m为1至6的整数，条件是当R为低级链烯基时，双键不是氮原子的α; 哪些化合物是有用的止痛剂，抗惊厥药和抗抑郁药，以及用于治疗以胆碱能功能降低为特征的各种记忆功能障碍如阿尔茨海默病。

80. 发明授权

US4752610A N-(pyrrol-1-yl)pyridinamines having memory enhancing properties 失效
标题翻译：具有记忆增强特性的N-（吡咯-1-基）吡啶胺
公开(公告)号：US4752610A
公开(公告)日：1988-06-21
申请号：US804430
申请日：1985-12-04
申请人： Richard C. Effland , Joseph T. Klein , Kevin J. Kapples
发明人： Richard C. Effland , Joseph T. Klein , Kevin J. Kapples
IPC分类号： A61K31/44 , A61K31/4427 , A61P25/28 , C07D401/12 , C07D401/02
CPC分类号： C07D401/12
摘要： There are disclosed novel compounds of the formula ##STR1## where R is H, loweralkyl, halogen, cyano, loweralkanoyl, arylloweralkanoyl, aroyl, --CH(OH)r.sub.1, --C(OH)r.sub.1 r.sub.2 or --CH.sub.2 Or.sub.2, where r.sub.1 is H, loweralkyl, arylloweralkyl or aryl and r.sub.2 is loweralkyl; R.sub.1 is H, loweralkyl, arylloweralkyl, phenyl, nitrophenyl, cyanophenyl, trifluoromethylphenyl, aminophenyl, loweralkanoylaminophenyl, loweralkoxycarbonyl, arylloweralkoxycarbonyl, aryloxycarbonyl, loweralkylaminocarbonyl, arylloweralkylaminocarbonyl, arylaminocarbonyl, alkanoyl, arylloweralkanoyl, aroyl, alkenoyl or alkynoyl; and R.sub.2 is H, NO.sub.2, NH.sub.2, halogen, loweralkanoylamino, arylloweralkanoylamino, aroylamino or loweralkyl, or R.sub.2 as a whole is a combination of 2, 3 or 4 halogen atoms; or pharmaceutically acceptable acid addition salts thereof, which are useful for enhancing memory, methods for synthesizing them, pharmaceutical compositions comprising an effective memory enhancing amount of such a compound and methods of treating a patient in need of memory enhancement by administering such a compound to the patient.
摘要翻译：公开了下式的新化合物，其中R是H，低级烷基，卤素，氰基，低级烷酰基，芳基低级烷酰基，芳酰基，-CH（OH）r1，-C（OH）r1r2或-CH2Or2，其中r1是H，低级烷基，芳基低级烷基或芳基，R 2是低级烷基; R 1是H，低级烷基，芳基低级烷基，苯基，硝基苯基，氰基苯基，三氟甲基苯基，氨基苯基，低级烷酰基氨基苯基，低级烷氧基羰基，芳基低级烷氧基羰基，芳氧基羰基，低级烷基氨基羰基，芳基低级烷基氨基羰基，芳基氨基羰基，烷酰基，芳基低级烷酰基，芳酰基，烯酰基或炔酰基。 R2为H，NO2，NH2，卤素，低级烷酰基氨基，芳基低级烷酰基氨基，芳酰氨基或低级烷基，R2为整体，为2,3或4种卤素原子的组合; 可用于增强记忆力的药物组合物或其药学上可接受的酸加成盐，用于合成它们的方法，包含有效记忆增加量的这种化合物的药物组合物和通过将这种化合物给予治疗需要记忆增强的患者的方法患者。

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