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31. 发明授权

US5268468A N-nitrosophenoxybenzenepropanamine and N-1-chloroethyl carbamate intermediates 失效
标题翻译： N-亚硝基苯氧基苯丙胺和N-1-氯乙基氨基甲酸酯中间体
公开(公告)号：US5268468A
公开(公告)日：1993-12-07
申请号：US65298
申请日：1993-05-24
申请人： Richard C. Effland , Joseph T. Klein
发明人： Richard C. Effland , Joseph T. Klein
IPC分类号： C07C243/06 , C07C243/18 , C07C243/28 , C07C243/32 , C07C281/02 , C07C207/04 , C07C271/16
CPC分类号： C07C281/02 , C07C243/06 , C07C243/18 , C07C243/28 , C07C243/32
摘要： Novel 2-(3-phenylpropyl)hydrazines, intermediates in and processes for the preparation thereof, and a method of treating personality disorders utilizing compounds or compositions thereof are disclosed.
摘要翻译：公开了新的2-（3-苯基丙基）肼，其中间体及其制备方法，以及使用化合物或其组合物治疗人格障碍的方法。

32. 发明授权

US5055476A 3-(1,2-benzisoxazol-3-yl)-4-pyridinamines and derivatives 失效
标题翻译： 3-（1,2-苯并异恶唑-3-基）-4-吡啶胺及其衍生物
公开(公告)号：US5055476A
公开(公告)日：1991-10-08
申请号：US566932
申请日：1990-08-13
申请人： Richard C. Effland , Joseph T. Klein
发明人： Richard C. Effland , Joseph T. Klein
IPC分类号： A61K31/44 , A61K31/423 , A61K31/4427 , A61K31/4439 , A61P17/00 , A61P25/04 , A61P25/28 , A61P29/00 , C07D213/75 , C07D261/20 , C07D413/04
CPC分类号： C07D413/04
摘要： This invention relates to 3-(1,2-benzisoxazol-3-yl)-4-pyridinamines of the formula ##STR1## where R.sub.1 is hydrogen, loweralkyl, arylalkyl or acyl; R.sub.2 is hydrogen, loweralkyl or arylalkyl, X is hydrogen, halogen, nitro or amino; or the pharmaceutically acceptable addition salts thereof, and where applicable, the geometric and optical isomers and racemic mixtures thereof. The compounds of this invention are useful as analgesics, for alleviating various memory dysfunctions characterized by a decreased cholinergic function, as cognition enhancers in the treatment of senile dementia such as Alzheimer's disease and as topical antiinflammatory agents for the treatment of various dermatoses.

33. 发明授权

US5039687A N-(pyrrol-1-yl)pyridinamine compounds having enhancing activity 失效
标题翻译：具有增强活性的N-（吡咯-1-基）吡啶胺化合物
公开(公告)号：US5039687A
公开(公告)日：1991-08-13
申请号：US478182
申请日：1990-02-09
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： C07D401/12
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 H, loweralkyl, arylloweralkyl, phenyl, nitrophenyl, cyanophenyl, trifluoromethylphenyl, aminophenyl, loweralkanoylaminophenyl, loweralkoxycarbonyl, arylloweralkylkoxycarbonyl, 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; 芳基低级烷基氨基苯基，低级烷氧基羰基，芳基低级烷基烷氧基羰基，芳氧基羰基， 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。

34. 发明授权

US4900742A N-(pyrrol-1-yl)pyridinamine compounds having memory enhancing properties 失效
标题翻译：具有记忆增强特性的N-（吡咯-1-基）吡啶胺化合物
公开(公告)号：US4900742A
公开(公告)日：1990-02-13
申请号：US200983
申请日：1988-06-01
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： C07D401/12
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。

35. 发明授权

US4880822A 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：US4880822A
公开(公告)日：1989-11-14
申请号：US171102
申请日：1988-04-04
申请人： Richard C. Effland , Joseph T. Klein
发明人： Richard C. Effland , Joseph T. Klein
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如本说明书中所定义，该化合物可用于增强记忆力，也可用作镇痛药和抗抑郁药。

36. 发明授权

US4800203A Pyrrolo(1,2-b)cinnolines 失效
标题翻译：吡咯（1,2-b）噌啉
公开(公告)号：US4800203A
公开(公告)日：1989-01-24
申请号：US100700
申请日：1987-09-24
申请人： R. Russell Hamer , Richard C. Effland , Joseph T. Klein
发明人： R. Russell Hamer , Richard C. Effland , Joseph T. Klein
IPC分类号： A61K31/50 , A61P25/02 , A61P25/04 , A61P25/28 , C07D487/04
CPC分类号： C07D487/04
摘要： There are described pyrrolo[1,2-b]cinnolines having the formula ##STR1## where R.sub.1 when present is hydrogen, loweralkyl, arylloweralkyl or --CH.sub.2 CO.sub.2 C.sub.2 H.sub.5 ; R.sub.2 is hydrogen, loweralkyl, arylloweralkyl, chlorine, bromine, iodine, formyl, nitro, --Ch.dbd.CR.sub.3 R.sub.4 or --CH.sub.2 CHR.sub.3 R.sub.4, R.sub.3 and R.sub.4 being independently hydrogen, loweralkyl, aryl or arylloweralkyl; X is oxygen, amino, loweralkylamino, arylloweralkylamino or methoxy; and Y is hydrogen, fluorine, chlorine, bromine, iodine, trifluoromethyl or nitro, and pharmaceutically acceptable acid addition salts thereof which are useful as analgesic agents and as enhancers of cholinergic function and hence for the treatment of memory dysfunctions and senile dementia's such as Alzheimer's disease characterized by diminished cholinergic function.

37. 发明授权

US4789678A Memory enhancing .alpha.-alkyl-4-amino-3-quinolinemethanols and 1-(4-aralkylamino-3-quinolinyl)alkanones and related compounds 失效
标题翻译：记忆增强α-烷基-4-氨基-3-喹啉甲醇和1-（4-芳烷基氨基-3-喹啉基）烷酮及相关化合物
公开(公告)号：US4789678A
公开(公告)日：1988-12-06
申请号：US899584
申请日：1986-08-25
申请人： Richard C. Effland , Joseph T. Klein
发明人： Richard C. Effland , Joseph T. Klein
IPC分类号： A61K31/47 , A61P25/28 , A61P43/00 , C07D215/42 , C07D215/44 , C07D215/14
CPC分类号： C07D215/42
摘要： There are described compounds of the formula ##STR1## where X is hydrogen, halogen, loweralkyl, loweralkoxy or trifluoromethyl; R is ##STR2## R.sub.4 being loweralkyl; R.sub.1 is hydrogen, loweralkyl or arylloweralkyl; R.sub.2 is hydrogen, loweralkyl or arylloweralkyl; and R.sub.3 is loweralkyl, with the proviso that when R is acetyl, R.sub.3 is methyl and X is hydrogen, R.sub.1 and R.sub.2 are not both hydrogen, or pharmaceutically acceptable acid addition salts thereof, which are useful in the treatment of various memory dysfunctions characterized by decreased cholinergic function.

38. 发明授权

US4588727A Intermediates for pyrrolo[1,2-b][1,2,5]triazepines 失效
标题翻译：吡咯并[1,2-b] [1,2,5]三氮杂的中间体
公开(公告)号：US4588727A
公开(公告)日：1986-05-13
申请号：US698196
申请日：1985-02-04
申请人： Richard C. Effland , Joseph T. Klein , R. Richard L. Hamer
发明人： Richard C. Effland , Joseph T. Klein , R. Richard L. Hamer
IPC分类号： C07D207/50 , C07D487/04 , A61K31/40
CPC分类号： C07D487/04 , C07D207/50
摘要： There are described novel pyrrolo[1,2-b][1,2,5]triazepines of the general formula ##STR1## where R is hydrogen, loweralkyl, loweralkylaminoloweralkyl or diloweralkylaminoloweralkyl; X is hydrogen, halogen (fluorine, chlorine, bromine or iodine), trifluoromethyl or nitro; and Y is hydrogen, halogen or loweralkyl. Also described are derivatives of 1-amino-2-benzoylpyrrole having the general formula ##STR2## where R, X and Y are as defined above, and R.sub.1 is hydrogen, ##STR3##Compounds I and II are useful as analgesic, anxiolytic and/or anticonvulsant agents, and many of Compounds II are useful as intermediates for synthesizing Compounds I.
摘要翻译：描述了通式“IMAGE”的新型吡咯并[1,2-b] [1,2,5]三氮，其中R是氢，低级烷基，低级烷基氨基低级烷基或二低烷基氨基低级烷基; X是氢，卤素（氟，氯，溴或碘），三氟甲基或硝基; Y是氢，卤素或低级烷基。还描述了具有通式为：其中R，X和Y如上所定义，并且R 1是氢的具有通式“（II）”的1-氨基-2-苯甲酰基吡咯的衍生物，其中R 1是氢，化合物I和II可用作止痛剂，抗焦虑剂和/或抗惊厥剂，许多化合物II可用作合成化合物I的中间体。

39. 发明授权

US4578394A Cholinergic function increasing 3-[N-(pyridyl) carbamoyl]-1,4-dihydropyridines 失效
标题翻译：胆碱功能增加3- [N-（吡啶基）氨基甲酰基] -1,4-二氢吡啶
公开(公告)号：US4578394A
公开(公告)日：1986-03-25
申请号：US680036
申请日：1984-12-10
申请人： Richard C. Allen , Richard C. Effland , Joseph T. Klein
发明人： Richard C. Allen , Richard C. Effland , Joseph T. Klein
IPC分类号： C07D213/82 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4425 , A61K31/4427 , A61K31/445 , A61P25/28 , C07D401/12 , A61K31/455
CPC分类号： C07D401/12
摘要： This invention relates to 1,4 dihydropyridines having the following formula ##STR1## wherein R is loweralkyl or Arloweralkyl; R.sub.1, R.sub.2 and R.sub.3 may be the same or different and are hydrogen, loweralkyl or halogen; X is hydrogen, NH.sub.2, ##STR2## and R.sub.4 is hydrogen or loweralkyl. The compounds of this invention display utility in the treatment of Alzheimer's disease and related cognitive disorders characterized by centrally deficient cholinergic function.
摘要翻译：本发明涉及具有下式的其中R为低级烷基或低级烷基的1,4-二氢吡啶; R 1，R 2和R 3可以相同或不同，为氢，低级烷基或卤素; X是氢，NH 2，R 3和R 4是氢或低级烷基。本发明的化合物可用于治疗阿尔茨海默病和以中枢缺乏胆碱能功能为特征的相关认知障碍。

40. 发明授权

US4551474A Methods of alleviating convulsions and pain employing 4-aryloxy-1,2,3,4 tetrahydroisoquinolines 失效
标题翻译：使用4-芳氧基-1,2,3,4四氢异喹啉减轻抽搐和疼痛的方法
公开(公告)号：US4551474A
公开(公告)日：1985-11-05
申请号：US639057
申请日：1984-08-09
申请人： Richard C. Effland , Larry Davis , Joseph T. Klein
发明人： Richard C. Effland , Larry Davis , Joseph T. Klein
IPC分类号： C07D217/24 , A61K31/47 , C07D401/06
CPC分类号： C07D217/24
摘要： This invention relates to 4-aryloxy-1,2,3,4-tetrahydroisoquinolines of the formula ##STR1## where Y is hydrogen and alkoxy; X is hydrogen, cyano, benzoyl, trifluoromethyl, phenyl, halogen, alkyl alkoxy and nitro; R is hydrogen and alkyl; R.sub.1 is hydrogen, alkyl, aralkyl, ##STR2## and CO.sub.2 R.sub.4 where R.sub.1 is aryl and alkyl; R.sub.2 and R.sub.3 are the same or differnt and are hydrogen and alkyl or R.sub.2 and R.sub.3 are fused together to form a pyrrolidino or a piperidino ring substituent; and m is an integer of 1 or 2; n is an integer of 2 or 3; and a pharmaceutically acceptable acid addition salt thereof.
摘要翻译：本发明涉及式为“IMAGE”的4-芳氧基-1,2,3,4-四氢异喹啉，其中Y为氢和烷氧基; X是氢，氰基，苯甲酰基，三氟甲基，苯基，卤素，烷基烷氧基和硝基; R是氢和烷基; R 1是氢，烷基，芳烷基，和CO 2 R 4，其中R 1是芳基和烷基; R2和R3相同或不同，为氢和烷基或R2和R3稠合在一起形成吡咯烷子基或哌啶子基环取代基; m为1或2的整数; n为2或3的整数; 及其药学上可接受的酸加成盐。

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