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1. 发明授权

US5405856A Certain nitro-3-pyrinamines and 3-oxy-analogues 失效
标题翻译：某些硝基-3-吡啶胺和3-氧基 - 类似物
公开(公告)号：US5405856A
公开(公告)日：1995-04-11
申请号：US42502
申请日：1993-04-02
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 , A61K31/44 , C07D213/61 , C07D213/72 , C07D213/75
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, loweralkyl 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;eachR.sub.4 is independently hydrogen or loweralkyl; andY 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; 并且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。

2. 发明授权

US5102891A 1-(substituted pyridinylamino)-1H-indol-5-yl substituted carbamates 失效
标题翻译： 1-（取代的吡啶基氨基）-1H-吲哚-5-基取代的氨基甲酸酯
公开(公告)号：US5102891A
公开(公告)日：1992-04-07
申请号：US555890
申请日：1990-07-23
申请人： Richard C. Effland , Larry Davis , Gordon E. Olsen , Joseph T. Klein , David G. Wettlaufer , Peter A. Nemoto
发明人： Richard C. Effland , Larry Davis , Gordon E. Olsen , Joseph T. Klein , David G. Wettlaufer , Peter A. Nemoto
IPC分类号： A61K31/44 , A61K31/4427 , A61K31/535 , A61K31/55 , A61P25/28 , A61P43/00 , C07D401/12 , C07D401/14 , C07D413/14 , C12N9/99
CPC分类号： C07D401/12 , C07D401/14
摘要： There are disclosed various compounds of the formula below, ##STR1## where n is 0 or 1;X is hydrogen, halogen, nitro, amino, trifluoromethyl, loweralkyl, or loweralkoxy;Y is hydrogen, halogen, nitro, amino, trifluoromethyl, loweralkyl, or loweralkoxy;R.sub.1 is hydrogen, loweralkyl, arylloweralkyl, loweralkenyl, loweralkynyl, loweralkanoyl, arylloweralkanoyl, heteroarylloweralkyl or heteroarylloweralkanoyl;R.sub.2 is hydrogen, loweralkyl, formyl or cyano;R.sub.3 is hydrogen or loweralkyl;R.sub.4 is loweralkyl, arylloweralkyl, cycloalkyl, aryl or heteroaryl; or alternatively, --NR.sub.3 R.sub.4 taken together constitutes ##STR2## R.sub.5 being hydrogen, loweralkyl, aryl, arylloweralkyl, heteroaryl or heteroarylloweralkyl,which compounds are useful for the treatment of various memory dysfunctions characterized by a cholinergic deficit such as Alzheimer's disease.
摘要翻译：公开了下式的各种化合物，其中n为0或1; X是氢，卤素，硝基，氨基，三氟甲基，低级烷基或低级烷氧基; Y是氢，卤素，硝基，氨基，三氟甲基，低级烷基或低级烷氧基; R 1是氢，低级烷基，芳基低级烷基，低级烯基，低级炔基，低级烷酰基，芳基低级烷酰基，杂芳基低级烷基或杂芳基低级烷酰基。 R2是氢，低级烷基，甲酰基或氰基; R3是氢或低级烷基; R4是低级烷基，芳基低级烷基，环烷基，芳基或杂芳基; 或者可选地，-NR 3 R 4一起构成R 5为氢，低级烷基，芳基，芳基低级烷基，杂芳基或杂芳基低级烷基，该化合物可用于治疗以胆碱能缺乏为特征的各种记忆功能障碍如阿尔茨海默氏病。

3. 发明授权

US4970218A N-(pyridinyl)-1H-indol-1-amines 失效
标题翻译： N-（吡啶基）-1H-吲哚-1-胺
公开(公告)号：US4970218A
公开(公告)日：1990-11-13
申请号：US405156
申请日：1989-09-11
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## where 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。

4. 发明授权

US4935418A Medical compositions of 1-aryloxy-2,3,4,5-tetrahydro-3-benzazepines and use thereof 失效
标题翻译： 1-芳氧基-2,3,4,5-四氢-3-苯并氮杂的医药组合物及其用途
公开(公告)号：US4935418A
公开(公告)日：1990-06-19
申请号：US236104
申请日：1988-08-23
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。

5. 发明授权

US4916135A N-heteroaryl-4-quinolinamines 失效
标题翻译： N-杂芳基-4-喹啉胺
公开(公告)号：US4916135A
公开(公告)日：1990-04-10
申请号：US348937
申请日：1989-05-08
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： A61K31/47 , A61P25/04 , A61P25/28 , C07D401/12
CPC分类号： C07D401/12
摘要： There are described compounds of the formula ##STR1## where --R is ##STR2## --R.sub.3 and R.sub.3 being independently --H, loweralkyl, --CHO, --CH.dbd.CH.sub.2, --CH.dbd.CH--loweralkyl, --CH.dbd.CHCO.sub.2 C.sub.2 H.sub.5, --CH.sub.2 N(C.sub.2 H.sub.5).sub.2 or ##STR3## --R.sub.1 when existent is --H, loweralkyl, --CH.sub.2 C.tbd.CH, ##STR4## R.sub.5 being methyl or phenyl optionally mono-substituted with loweralkyl or loweralkoxy;--R.sub.2 when existent is loweralkyl or --CH.sub.2 C.tbd.CH;--X is --H, loweralkyl, loweralkoxy, halogen or trifluoromethyl; and the two --Y groups when existent are both --H, or combine to constitute --(CH.sub.2).sub.4 --;which compounds are useful as analgesic agents, and for treating various memory dysfunctions characterized by decreased cholinergic function such as Alzheimer's disease.

6. 发明授权

US5221682A 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：US5221682A
公开(公告)日：1993-06-22
申请号：US695156
申请日：1991-05-03
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, loweralkyl 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 dematoses.
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甲状腺炎的局部抗炎药。

7. 发明授权

US5037835A Benzocycloalkylaminopyridinamines and related compounds as topical antiinflammatory agents for the treatment of skin disorders 失效
标题翻译：苯并环烷基氨基吡啶胺和相关化合物作为治疗皮肤病症的局部抗炎药
公开(公告)号：US5037835A
公开(公告)日：1991-08-06
申请号：US588789
申请日：1990-09-27
申请人： Richard C. Effland , Joseph T. Klein , Gordon E. Olsen , Larry Davis
发明人： Richard C. Effland , Joseph T. Klein , Gordon E. Olsen , Larry Davis
IPC分类号： C07D401/04
CPC分类号： C07D401/04
摘要： There are described compounds of the formula, ##STR1## where R is hydrogen, loweralkyl, arylloweralkyl or loweralkylcarbonyl;k is 0 or 1;m is 1, 2 or 3;k+m is 2 or 3; andn is 0 or 1;which compounds are useful as topical antiinflammatory agents for the treatment of various dermatoses.
摘要翻译：描述了下式的化合物，其中R是氢，低级烷基，芳基低级烷基或低级烷基羰基; k为0或1; m为1,2或3; k + m为2或3; 并且n为0或1; 哪些化合物可用作治疗各种皮肤病的局部抗炎剂。

8. 发明授权

US5017578A N-heteroaryl-purin-6-amines useful as analgesic and anticonvulsant agents 失效
标题翻译： N-杂芳基 - 嘌呤-6-胺可用作止痛剂和抗惊厥剂
公开(公告)号：US5017578A
公开(公告)日：1991-05-21
申请号：US363837
申请日：1989-06-09
申请人： Richard C. Effland , Joseph T. Klein , Larry Davis , Gordon E. Olson
发明人： Richard C. Effland , Joseph T. Klein , Larry Davis , Gordon E. Olson
IPC分类号： A61K31/52 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7076 , A61P25/04 , C07D403/12 , C07D403/14 , C07D473/34 , C07H19/16 , C07H19/167
CPC分类号： C07H19/16 , C07D473/34
摘要： This invention relates to a N-heteroaryl-purin-6-amine of the formula ##STR1## where R.sub.1 is hydrogen, lower alkyl, and arylloweralkyl; R.sub.2 and R.sub.3 are independently hydrogen, lower alkyl or R.sub.2 and R.sub.3 taken together are aryl; R.sub.4 and R.sub.5 are independently hydrogen, lower alkyl, or R.sub.4 and R.sub.5 taken together are aryl; R.sub.6 is hydrogen, lower alkyl, aryl, arylloweralkyl, ##STR2## where R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as defined above, and the pharmaceutically acceptable acid addition salts thereof and where applicable the geometric and optical isomers and racemic mixtures thereof. The compounds of this invention display utility as analgesic and anticonvulsant agents.

9. 发明授权

US4992448A Benzocycloalkylaminopyridinamines and related compounds as topical antiinflammatory agents for the treatment of skin disorders 失效
标题翻译：苯并环烷基氨基吡啶胺和相关化合物作为治疗皮肤病症的局部抗炎药
公开(公告)号：US4992448A
公开(公告)日：1991-02-12
申请号：US425712
申请日：1989-10-24
申请人： Richard C. Effland , Joseph T. Klein , Gordon E. Olsen , Larry Davis
发明人： Richard C. Effland , Joseph T. Klein , Gordon E. Olsen , Larry Davis
IPC分类号： A61K31/44 , A61K31/4427 , A61K31/47 , A61P17/00 , A61P29/00 , C07D401/04
CPC分类号： C07D401/04
摘要： There are described compounds of the formula, ##STR1## where R is hydrogen, loweralkyl, arylloweralkyl or loweralkylcarbonyl;k is 0 or 1;m is 1,2 or 3;k+m is 2 or 3; andn is 0 or 1;which compounds are useful as topical antiinflammatory agents for the treatment of various dermatoses.

10. 发明授权

US4988690A 1-aryloxy-2,3,4,5-tetrahydro-3-benzazepines and anti-depressant use thereof 失效
标题翻译： 1-芳氧基-2,3,4,5-四氢-3-苯并氮杂及其抗抑郁剂
公开(公告)号：US4988690A
公开(公告)日：1991-01-29
申请号：US387916
申请日：1982-06-14
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： A61K31/55 , A61P9/12 , A61P25/04 , A61P25/24 , A61P25/26 , C07D223/16 , C07D233/16
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 -alkylene ##STR3## where Z is hydrogen, lower alkyl, lower alkoxy, halogen, CF.sub.3, NO.sub.2 and NH.sub.2 ; and an alkylene amine of the formula ##STR4## where R.sub.1 and R.sub.2 are the same of different and are hydrogen and lower alkyl, 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的式 - 亚烷基的低级烷基; 和其中R 1和R 2相同且为氢和低级烷基的式“IMAGE”的亚烷基胺及其药学上可接受的酸加成盐。

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