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38 条记录 (耗时 0.024 秒)

    N-[substituted alkylidene]fused-bicycloalkylidene quinolinamines useful for enhancing the cholinergic function in a mammal
    23.
    发明授权
    N-[substituted alkylidene]fused-bicycloalkylidene quinolinamines useful for enhancing the cholinergic function in a mammal 失效
    用于增强哺乳动物胆碱能功能的N- [取代亚烷基]稠合双亚烷基喹啉胺

    公开(公告)号：US5037833A

    公开(公告)日：1991-08-06

    申请号：US480388

    申请日：1990-02-15

    申请人： Gregory M. Shutske ,  Kevin J. Kapples

    发明人： Gregory M. Shutske ,  Kevin J. Kapples

    IPC分类号： C07D221/22 ,  C07D495/04

    CPC分类号： C07D495/04 ,  C07D221/22

    摘要： There are disclosed novel compounds having the formula, ##STR1## wherein, m is an integer of 0-3;n is an integer of 1-4;R.sub.1 is hydrogen, alkyl, cycloalkyl, arylloweralkyl, aryl, naphthyl, furyl, thienyl, pyridinyl or pyrrolyl; each R.sub.2 and R.sub.3 are independently hydrogen, loweralkyl or arylloweralkyl, or alternatively R.sub.2 and R.sub.3 taken together form a methylene or ethylene bridge;X is hydrogen, loweralkyl, cycloalkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, formyl, loweralkoxycarbonyl, arylcarbonyl, --SH, loweralkylthio, --NHCOR.sub.4 or --NR.sub.5 R.sub.6, R.sub.4 being hydrogen or loweralkyl, and R.sub.5 and R.sub.6 being independently hydrogen, loweralkyl or cycloalkyl;Y is CH.sub.2, CH.dbd.CH, O, S or NR.sub.7, R.sub.7 being hydrogen, loweralkyl or arylloweralkyl; with the proviso that the number of said methylene or ethylene bridge shall not exceed 1 and that when Y is CH.sub.2, one and only one combination of R.sub.2 and R.sub.3 must constitute a methylene or ethylene bridge;stereo, optical and geometrical isomers thereof, and pharmaceutically acceptable acid addition salts thereof, which are useful for enhancing memory.

    摘要翻译： 公开了具有下式的新化合物，其中m是0-3的整数; n为1-4的整数; R 1是氢，烷基，环烷基，芳基低级烷基，芳基，萘基，呋喃基，噻吩基，吡啶基或吡咯基。 每个R2和R3独立地是氢，低级烷基或芳基低级烷基，或者R2和R3一起形成亚甲基或乙烯桥; X是氢，低级烷基，环烷基，低级烷氧基，卤素，羟基，硝基，三氟甲基，甲酰基，低级烷氧基羰基，芳基羰基，-SH，低级烷硫基，-NHCOR4或-NR5R6，R4是氢或低级烷基，R5和R6独立地是氢， 或环烷基; Y是CH 2，CH = CH，O，S或NR 7，R 7是氢，低级烷基或芳基低级烷基; 条件是所述亚甲基或乙烯桥的数目不得超过1，而当Y为CH2时，R2和R3之间的一个组合只能构成亚甲基或乙烯桥; 立体，光学和几何异构体及其药学上可接受的酸加成盐，其可用于增强记忆。

    9-amino-1,4ethano-1,2,3,4-tetrahydroacridine and related compounds
    25.
    发明授权
    9-amino-1,4ethano-1,2,3,4-tetrahydroacridine and related compounds 失效
    9-氨基-1,4-乙烷-1,2,3,4-四氢吖啶及相关化合物

    公开(公告)号：US5401749A

    公开(公告)日：1995-03-28

    申请号：US218755

    申请日：1988-07-08

    申请人： Gregory M. Shutske ,  Kevin J. Kapples

    发明人： Gregory M. Shutske ,  Kevin J. Kapples

    IPC分类号： A61K31/47 ,  A61P25/02 ,  A61P25/28 ,  C07C251/24 ,  C07D219/10 ,  C07D221/22 ,  C07D221/18 ,  A61K31/435

    CPC分类号： C07D219/10 ,  C07C251/24 ,  C07D221/22 ,  C07C2102/18

    摘要： There are disclosed compounds having the formula ##STR1## wherein R is hydrogen, loweralkyl or loweralkylcarbonyl; R.sub.1 is hydrogen, loweralkyl, loweralkylcarbonyl, aryl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, oxygen-bridged arylloweralkyl or oxygen-bridged diarylloweralkyl; R.sub.2 and R.sub.3 are independently H or CH.sub.3 ; X is hydrogen, loweralkyl, cycloalkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, formyl, loweralkylcarbonyl, arylcarbonyl, --SH, loweralkylthio, --NHCOR.sub.4 or --NR.sub.5 R.sub.6 where R.sub.4 is hydrogen or loweralkyl, and R.sub.5 and R.sub.6 are independently hydrogen, loweralkyl or cycloalkyl; Y and Z are independently a direct bond, CR.sub.7 R.sub.8 or CR.sub.7 R.sub.8 --CR.sub.9 R.sub.10 ; and L and Q are independently CR'.sub.7 R'.sub.8, CR'.sub.7 R'.sub.8 --CR'.sub.9 R'.sub.10, CR'.sub.7 .dbd.CR'.sub.9 or CR'.sub.7 R'.sub.8 --CR'.sub.9 R'.sub.10 --CR.sub.11 R.sub.12, where each of R.sub.7 through R.sub.12 and R'.sub.7 through R'.sub.10 is independently H or CH.sub.3 ; a stereo, optical and geometrical isomers thereof, and pharmaceutically acceptable acid addition salts thereof, which are useful for enhancing memory.

    摘要翻译： 公开了具有式“IMAGE”的化合物，其中R是氢，低级烷基或低级烷基羰基; R 1是氢，低级烷基，低级烷基羰基，芳基，二低级烷基氨基低级烷基，芳基低级烷基，二芳基低级烷基，氧桥连的芳基低级烷基或氧桥连的二芳基低级烷基。 R2和R3独立地是H或CH3; X是氢，低级烷基，环烷基，低级烷氧基，卤素，羟基，硝基，三氟甲基，甲酰基，低级烷基羰基，芳基羰基，-SH，低级烷硫基，-NHCOR4或-NR5R6，其中R4是氢或低级烷基，R5和R6独立地是氢， 或环烷基; Y和Z独立地是直接键，CR7R8或CR7R8-CR9R10; L和Q独立地为CR'7R'8，CR'7R'8-CR'9R'10，CR'7 = CR'9或CR'7R'8-CR'9R'10-CR11R12，其中R7 通过R12和R'7至R'10独立地是H或CH3; 其立体，光学和几何异构体及其药学上可接受的酸加成盐，其可用于增强记忆。

    Isoxazolobenzoxazepines
    28.
    发明授权
    Isoxazolobenzoxazepines 失效
    异氮杂苯并氧氮杂

    公开(公告)号：US4960767A

    公开(公告)日：1990-10-02

    申请号：US302027

    申请日：1989-01-30

    申请人： Gregory M. Shutske ,  Kevin J. Kapples

    发明人： Gregory M. Shutske ,  Kevin J. Kapples

    IPC分类号： A61K31/55 ,  A61P25/04 ,  C07D498/06

    CPC分类号： C07D498/06

    摘要： This invention relates to isoxazolobenzoxazepines having the following formula ##STR1## wherein X.sub.1 is H; X.sub.2 is H or OH; or X.sub.1 and X.sub.2 taken together are carbonyl oxygen or ##STR2## R is (1) H, (2) loweralkyl, (3) arylloweralkyl, (4) loweralkynyl, (5) loweralkenyl, (6) ##STR3## where R.sub.1 and R.sub.2 are independently (a) H, (b) lower alkyl, (c) arylloweralkyl, (d) ##STR4## where Z is H, halogen, loweralkyl, loweralkoxy, CF.sub.3, nitro or amino and n' is an integer of 1 to 3; (e) ##STR5## where n" is an integer of 1 to 3; or (f) R.sub.1 and R.sub.2 taken together with the nitrogen atom are substituted or unsubstituted piperidino or pyrrolidino of the formula ##STR6## where R.sub.3 is H, loweralkyl or aryl, and m is an integer of 1 or 2; (7) ##STR7## where R.sub.4 is H or loweralkyl and m' is an integer of 3 or 4; (8) ##STR8## where Z and n' are as previously defined; (9) ##STR9## where m'" is an integer of 1, 2, or 3 (10) ##STR10## where R.sub.5 and R.sub.6 are lower alkyl, aryl lower alkyl or are independently taken together with the N atom to form a substituted or unsubstituted piperidino or pyrrolidino group of the formula ##STR11## where R.sub.3 and m are as previously defined (11) ##STR12## where R.sub.7 is loweralkyl, aryl, or arylloweralkyl; (12) ##STR13## where R.sub.5 and R.sub.6 are as previously defined; Y is H, halogen, loweralkyl, loweralkoxy, CF.sub.3, nitro or amino and n is an integer of 1 to 3, and the pharmaceutically acceptable acid addition salts thereof and where applicable to the geometric, stereo and optical isomers thereof.

    Substituted 9-amino-tetrahydroacridines and related compounds
    30.
    发明授权
    Substituted 9-amino-tetrahydroacridines and related compounds 失效
    取代的9-氨基 - 四氢rid啶及相关化合物

    公开(公告)号：US5391553A

    公开(公告)日：1995-02-21

    申请号：US244212

    申请日：1988-09-14

    申请人： Gregory M. Shutske ,  Grover C. Helsley ,  Kevin J. Kapples

    发明人： Gregory M. Shutske ,  Grover C. Helsley ,  Kevin J. Kapples

    IPC分类号： A61K31/47 ,  A61K31/473 ,  A61P25/02 ,  A61P25/28 ,  C07C67/00 ,  C07C241/00 ,  C07C251/18 ,  C07C251/20 ,  C07D219/04 ,  C07D219/06 ,  C07D219/10 ,  C07D221/16 ,  A61K31/435

    CPC分类号： C07D219/10 ,  C07D219/04 ,  C07D219/06

    摘要： There are disclosed compounds having the formula ##STR1## wherein n is 1-4; X is alkyl of 3-18 carbon atoms, cycloalkyl of 3-7 carbon atoms or cycloalkylloweralkyl; R is hydrogen, loweralkyl or loweralkylcarbonyl; R.sub.1 is hydrogen, loweralkyl, loweralkylcarbonyl, aryl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, oxygen-bridged arylloweralkyl or oxygen-bridged diarylloweralkyl; stereo isomers thereof and pharmaceutically acceptable acid addition salts thereof, which are useful for enhancing memory, methods for synthesizing them, and pharmaceutical compositions comprising an effective memory enhancing amount of such a compound.

    摘要翻译： 公开了具有式“IMAGE”的化合物，其中n为1-4; X是3-18个碳原子的烷基，3-7个碳原子的环烷基或环烷基低级烷基; R是氢，低级烷基或低级烷基羰基; R 1是氢，低级烷基，低级烷基羰基，芳基，二低级烷基氨基低级烷基，芳基低级烷基，二芳基低级烷基，氧桥连的芳基低级烷基或氧桥连的二芳基低级烷基。 其立体异构体和其药学上可接受的酸加成盐，其可用于增强记忆，合成它们的方法和包含有效记忆增加量的这种化合物的药物组合物。