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1. 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。

2. 发明授权

US5032599A N-(pyrrol-l-yl)pyridinamines 失效
标题翻译： N-（吡咯-1-基）吡啶胺
公开(公告)号：US5032599A
公开(公告)日：1991-07-16
申请号：US245252
申请日：1988-09-16
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 n is 0 or 1; R is hydrogen or loweralkyl; R.sub.1 is hydrogen, loweralkyl, halogen, cyano, loweralkanoyl, arylloweralkanoyl, aroyl, --CH(OH)R.sub.4, --C(OH)R.sub.4 R.sub.5 or --CH.sub.2 OR.sub.5, --CH.dbd.CR.sub.6 R.sub.7, --CH.dbd.CHCN, --CH.dbd.CHOCH.sub.3, --CH.dbd.CHCO.sub.2 C.sub.2 H.sub.5, ##STR2## R.sub.4 being hydrogen, loweralkyl, arylloweralkyl or aryl, R.sub.5 being loweralkyl, aryl or arylloweralkyl, R.sub.6 being hydrogen or loweralkyl and R.sub.7 being hydrogen, loweralkyl or aryl; R.sub.2 is hydrogen, loweralkyl, loweralkenyl, loweralkynyl, --CH.sub.2 CO.sub.2 C.sub.2 H.sub.5, arylloweralkyl, phenyl, nitrophenyl, cyanophenyl, trifluoromethylphenyl, aminophenyl, loweralkanoylaminophenyl, loweralkoxycarbonyl, arylloweralkoxycarbonyl, aryloxycarbonyl, loweralkylaminocarbonyl, arylloweralkylaminocarbonyl, arylaminocarbonyl, alkanoyl, arylloweralkanoyl, aroyl, alkenoyl, alkynoyl, --CH.sub.2 C.tbd.CCH.sub.2 --NR'R", --CH.sub.2 CH.dbd.CHCH.sub.2 --NR'R" or --CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 --NR'R", R' and R" being independently loweralkyl or --NR'R" taken as a whole being ##STR3## and R.sub.3 is hydrogen, NO.sub.2, NH.sub.2, halogen, loweralkanoylamino, arylloweralkanoylamino, aroylamino or loweralkyl; with the proviso that when n is 0, R.sub.2 is phenyl, R.sub.3 is hydrogen and the pyridine moiety is 2-pyridinyl, R and R.sub.1 may not be 2-methyl and 5-methyl; 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 a method of treating a patient in need of memory enhancement which comprises administering such a compound to the patient.
摘要翻译：公开了新颖的化合物，其中n为0或1; R是氢或低级烷基; R 1是氢，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）R 4，-C（OH）R 4 R 5或-CH 2 OR 5，-CH = CR 6 R 7，-CH = CHCN，-CH = CHOCH 3，-CH R 2是氢，低级烷基，芳基低级烷基或芳基，R 5是低级烷基，芳基或芳基低级烷基，R 6是氢或低级烷基，R 7是氢或低级烷基，R 7是氢，是氢，低级烷基或芳基; R2是氢，低级烷基，低级烯基，低级炔基，-CH2CO2C2H5，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， CH2C 3BOND CCH2-NR'R“，-CH2CH = CHCH2-NR'R”或-CH2CH2CH2CH2-NR'R“，R'和R”独立地为低级烷基或-NR'R“ 并且R 3是氢，NO 2，NH 2，卤素，低级烷酰基氨基，芳基低级烷酰基氨基，芳酰基氨基或低级烷基; 条件是当n是0时，R2是苯基，R3是氢，吡啶部分是2-吡啶基，R和R1可以不是2-甲基和5-甲基; 其可用于增强记忆，其合成方法，包含有效记忆增加量的这种化合物的药物组合物和治疗需要记忆增强的患者的方法，其包括给予这种化合物给病人

3. 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。

4. 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。

5. 发明授权

US5194618A N-(pyrrol-1-yl)pyridinamines 失效
标题翻译： N-（吡咯-1-基）吡啶胺
公开(公告)号：US5194618A
公开(公告)日：1993-03-16
申请号：US748474
申请日：1991-05-23
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 compounds of the formula ##STR1## where n is 0 or 1; R is hydrogen or loweralkyl; R.sub.1 is hydrogen, loweralkyl, halogen, --CH(OH)R.sub.4, --C(OH)R.sub.4 R.sub.5 or --CH.sub.2 OR.sub.5, R.sub.4 being hydrogen, loweralkyl, arylloweralkyl or aryl, R.sub.5 being loweralkyl, aryl or arylloweralkyl, R.sub.6 being hydrogen or loweralkyl and R.sub.7 being hydrogen, loweralkyl or aryl; R.sub.2 is hydrogen, loweralkyl, loweralkenyl, loweralkynyl, --CH.sub.2 CO.sub.2 C.sub.2 H.sub.5, arylloweralkyl, phenyl, nitrophenyl, cyanophenyl, trifluoromethylphenyl, aminophenyl, loweralkanoylaminophenyl, loweralkoxycarbonyl, arylloweralkoxycarbonyl, aryloxycarbonyl, loweralkylaminocarbonyl, arylloweralkylaminocarbonyl, arylaminocarbonyl, alkanoyl, arylloweralkanoyl, aroyl, alkenoyl, alkynoyl, --CH.sub.2 C.tbd.CCH.sub.2 --NR'R", --CH.sub.2 CH=CHCH.sub.2 --NR'R" or --CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 --NR'R", R' and R" being independently loweralkyl or --NR'R" taken as a whole being ##STR2## and R.sub.3 is hydrogen, NO.sub.2, NH.sub.2, halogen, loweralkanoylamino, arylloweralkanoylamino, aroylamino or loweralkyl; with the proviso that when n is 0, R.sub.2 is phenyl, R.sub.3 is hydrogen and the pyridine moiety is 2-pyridinyl, R and R.sub.1 may not be 2 methyl and 5-methyl; or pharmaceutically acceptable acid addition salts thereof, which are useful for enhancing memory, methods for synthesizing them, pharmaceutical compositions comprising an effective memory enchancing amount of such a compound and a method of treating a patient in need of memory enhancement which comprises administering such a compound to the patient.
摘要翻译：公开了下式的化合物，其中n为0或1; R是氢或低级烷基; R1是氢，低级烷基，卤素，-CH（OH）R4，-C（OH）R4R5或-CH2OR5，R4是氢，低级烷基，芳基低级烷基或芳基，R5是低级烷基，芳基或芳基低级烷基，R6是氢或低级烷基，R7 是氢，低级烷基或芳基; R2是氢，低级烷基，低级烯基，低级炔基，-CH2CO2C2H5，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， CH2C 3BOND CCH2-NR'R“，-CH2CH = CHCH2-NR'R”或-CH2CH2CH2CH2-NR'R“，R'和R”独立地为低级烷基或-NR'R“ 并且R 3是氢，NO 2，NH 2，卤素，低级烷酰基氨基，芳基低级烷酰基氨基，芳酰基氨基或低级烷基; 条件是当n为0时，R 2为苯基，R 3为氢，吡啶部分为2-吡啶基，R和R 1可以不是2甲基和5-甲基; 其可用于增强记忆，其合成方法，包含有效的记忆增强量的这种化合物的药物组合物和治疗需要记忆增强的患者的方法，该方法包括给予这种化合物给病人

6. 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。

7. 发明授权

US4792562A N-(pyrrol-1-yl)pyridinamines having memory enhancing activity 失效
标题翻译：具有记忆增强活性的N-（吡咯-1-基）吡啶胺
公开(公告)号：US4792562A
公开(公告)日：1988-12-20
申请号：US926593
申请日：1986-11-12
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 , C07D401/02 , A61K31/44
CPC分类号： C07D401/12
摘要： There are disclosed novel compounds of the formula ##STR1## where n is 0 or 1; R is hydrogen or loweralkyl; R.sub.1 is hydrogen, loweralkyl, halogen, cyano, loweralkanoyl, arylloweralkanoyl, aroyl, --CH(OH)R.sub.4, --C(OH)R.sub.4 R.sub.5 or --CH.sub.2 OR.sub.5, --CH.dbd.CR.sub.6 R.sub.7, --CH.dbd.CHCN, --CH.dbd.CHOCH.sub.3, --CH.dbd.CHCO.sub.2 C.sub.2 H.sub.5, ##STR2## --CH.sub.2 CHR.sub.6 R.sub.7, --CH.sub.2 CH.sub.2 CN, --CH.sub.2 CH.sub.2 OCH.sub.3, --CH.sub.2 CH.sub.2 CO.sub.2 C.sub.2 H.sub.5, ##STR3## R.sub.4 being hydrogen, loweralkyl, arylloweralkyl or aryl, R.sub.5 being loweralkyl, aryl or arylloweralkyl, R.sub.6 being hydrogen or loweralkyl and R.sub.7 being hydrogen, loweralkyl or aryl; R.sub.2 is hydrogen, loweralkyl, loweralkenyl, loweralkynyl, --CH.sub.2 CO.sub.2 C.sub.2 H.sub.5, arylloweralkyl, phenyl, nitrophenyl, cyanophenyl, trifluoromethylphenyl, aminophenyl, loweralkanoylaminophenyl, loweralkoxycarbonyl, arylloweralkoxycarbonyl, aryloxycarbonyl, loweralkylaminocarbonyl, arylloweralkylaminocarbonyl, arylaminocarbonyl, alkanoyl, arylloweralkanoyl, aroyl, alkenoyl, alkynoyl, --CH.sub.2 C.tbd.CCH.sub.2 --NR'R", --CH.sub.2 CH.dbd.CHCH.sub.2 --NR'R" or --CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 --NR'R", R' and R" being independently loweralkyl or --NR'R" taken as a whole being ##STR4## and R.sub.3 is hydrogen, NO.sub.2, NH.sub.2, halogen, loweralkanoylamino, arylloweralkanoylamino, aroylamino or loweralkyl; with the proviso that when n is 0, R.sub.2 is phenyl, R.sub.3 is hydrogen and the pyridine moiety is 2-pyridinyl, R and R.sub.1 may not be 2-methyl and 5-methyl; 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 a method of treating a patient in need of memory enhancement which comprises administering such a compound to the patient.
摘要翻译：公开了新颖的化合物，其中n为0或1; R是氢或低级烷基; R 1是氢，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）R 4，-C（OH）R 4 R 5或-CH 2 OR 5，-CH = CR 6 R 7，-CH = CHCN，-CH = CHOCH 3，-CH = CHCO2C2H5， + TR -CH2CHR6R7，-CH2CH2CN，-CH2CH2OCH3，-CH2CH2CO2C2H5，R4是氢，低级烷基，芳基低级烷基或芳基，R5是低级烷基，芳基或芳基低级烷基，R6 是氢或低级烷基，R 7是氢，低级烷基或芳基; R2是氢，低级烷基，低级烯基，低级炔基，-CH2CO2C2H5，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， CH2C 3BOND CCH2-NR'R“，-CH2CH = CHCH2-NR'R”或-CH2CH2CH2CH2-NR'R“，R'和R”独立地为低级烷基或-NR'R“ 并且R 3是氢，NO 2，NH 2，卤素，低级烷酰基氨基，芳基低级烷酰基氨基，芳酰基氨基或低级烷基; 条件是当n是0时，R2是苯基，R3是氢，吡啶部分是2-吡啶基，R和R1可以不是2-甲基和5-甲基; 其可用于增强记忆，其合成方法，包含有效记忆增加量的这种化合物的药物组合物和治疗需要记忆增强的患者的方法，其包括给予这种化合物给病人

8. 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。

9. 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。

10. 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.

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