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85 条记录 (耗时 0.03 秒)

    3-(1H-indazol-3-yl)-4-pyridinamines
    4.
    发明授权
    3-(1H-indazol-3-yl)-4-pyridinamines 失效
    3-（1H-吲唑-3-基）-4-吡啶胺

    公开(公告)号：US5166163A

    公开(公告)日：1992-11-24

    申请号：US694973

    申请日：1991-05-06

    申请人： Richard C. Effland ,  Joseph T. Klein

    发明人： Richard C. Effland ,  Joseph T. Klein

    IPC分类号： C07D213/73 ,  C07D213/75 ,  C07D401/04

    CPC分类号： C07D213/73 ,  C07D213/75 ,  C07D401/04

    摘要： This invention relates to 3-(1H-indazol-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; R.sub.3 is hydrogen, loweralkyl or aryl and 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 and as topical antiinflammatory agents for the treatment of various dermatoses.

    摘要翻译： 本发明涉及式（Ia）的3-（1H-吲唑-3-基）-4-吡啶胺，其中R 1是氢，低级烷基，芳烷基或酰基; R2是氢，低级烷基或芳基烷基; R 3是氢，低级烷基或芳基，X是氢，卤素，硝基或氨基或其药学上可接受的加成盐，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。 本发明的化合物可用作止痛剂和用作治疗各种皮肤病的局部抗炎剂。

    1-(substituted pyridinylamino)-1H-indol-5-yl substituted carbamates
    5.
    发明授权
    1-(substituted pyridinylamino)-1H-indol-5-yl substituted carbamates 失效
    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。

    Medical compositions of 1-aryloxy-2,3,4,5-tetrahydro-3-benzazepines and use thereof
    8.
    发明授权
    Medical compositions of 1-aryloxy-2,3,4,5-tetrahydro-3-benzazepines and use thereof 失效
    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。

    N-heteroaryl-4-quinolinamines
    9.
    发明授权
    N-heteroaryl-4-quinolinamines 失效
    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.

    Pyrazol and indazolpyridinamines
    10.
    发明授权
    Pyrazol and indazolpyridinamines 失效
    吡唑和吲唑吡啶胺

    公开(公告)号：US4806554A

    公开(公告)日：1989-02-21

    申请号：US141852

    申请日：1988-01-11

    申请人： Richard C. Effland ,  Joseph T. Klein

    发明人： Richard C. Effland ,  Joseph T. Klein

    IPC分类号： C07D401/12 ,  A61K31/44 ,  A61K31/4427 ,  A61P25/04 ,  A61P25/24 ,  A61P25/26 ,  C07D401/04 ,  C07D521/00 ,  A61K31/415

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/04

    摘要： There are described compounds of the formula ##STR1## where n is 0 or 1; R.sub.1 is independently hydrogen, loweralkyl, loweralkenyl, loweralkynyl, loweralkoxycarbonylloweralkyl, loweralkylaminocarbonylloweralkyl, aminocarbonylloweralkyl, arylloweralkyl, phenyl, nitrophenyl, cyanophenyl, trifluoromethylphenyl, aminophenyl, loweralkanoylaminophenyl, loweralkoxycarbonyl, arylloweralkoxycarbonyl, aryloxycarbonyl, loweralkylaminocarbonyl, arylloweralkylaminocarbonyl, arylaminocarbonyl, alkanoyl, arylloweralkanoyl, aroyl, alkenoyl, alkynoyl or --R.sub.5 --NR'R" where R.sub.5 is loweralkylene, loweralkenylene or loweralkynylene and R' and R" are each independently loweralkyl or alternatively the group --NR'R" as a whole is 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 4-loweralkyl-1-piperazinyl or 4-aryl-1-piperazinyl;R.sub.2 is hydrogen or loweralkyl;R.sub.3 and R.sub.4 are each independently hydrogen or loweralkyl, or alternatively R.sub.3 and R.sub.4 taken together form --CH.dbd.CH--CH.dbd.CH-- so that the moiety ##STR2## becomes an indazole ring; and X is hydrogen, nitro, amino, halogen, loweralkanoylamino, arylloweralkanoylamino, aroylamino, alkylamino, arylloweralkylamino, loweralkyl, and cyano; which compounds are useful as analgesic and antidepressant agents.