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38 条记录 (耗时 0.027 秒)

    Hexahydro-1H-quino[4,3,2-ef][1,4]benzoxazepines and related compounds
    35.
    发明授权
    Hexahydro-1H-quino[4,3,2-ef][1,4]benzoxazepines and related compounds 失效
    六氢-1H-喹啉[4,3,2-ef] [1,4]苯并氧氮杂及相关化合物

    公开(公告)号：US5112829A

    公开(公告)日：1992-05-12

    申请号：US563141

    申请日：1990-08-06

    申请人： Gregory M. Shutske ,  Kevin J. Kapples ,  John D. Tomer, IV

    发明人： Gregory M. Shutske ,  Kevin J. Kapples ,  John D. Tomer, IV

    IPC分类号： C07D219/10 ,  C07D498/06 ,  C07D513/06

    CPC分类号： C07D513/06 ,  C07D219/10

    摘要： Novel 9-amino-1,2,3,4-tetrahydroacridines and related compounds of the formula ##STR1## wherein R.sup.1 is H, loweralkyl, or benzyl; R.sup.3 is H, loweralkyl, a group of the formula CH.sub.2 CHR.sup.2 Hal wherein R.sup.2 is hydrogen, loweralkyl, or phenyl and Hal is chloro, bromo, or iodo, or a group of the formula CHR.sup.2 CO.sub.2 R.sup.5 wherein R.sup.2 is as above and R.sup.5 is H or loweralkyl; Z is O or S; X is H, halogen, loweralkoxy, loweralkyl, or trifluoromethyl; n is 1, 2, or 3; the group ZR.sup.3 is bound to either the A- or B-position of the heteroaromatic nucleus; the pharmaceutically acceptable salts thereof; and the optical isomers thereof, useful as intermediates for the preparation of memory dysfunction relieving hexahydro-1H-quino[4,3,2-ef][1,4]benzoxazepines are related compounds and for relieving memory dysfunction are disclosed.

    摘要翻译： 新型9-氨基-1,2,3,4-四氢rid啶及其相关化合物，其中R 1为H，低级烷基或苄基; R3是H，低级烷基，式CH2CHR2Hal的基团，其中R2是氢，低级烷基或苯基，Hal是氯，溴或碘，或式CHR2CO2R5的基团，其中R2如上，R5是H或低级烷基; Z是O或S; X是H，卤素，低级烷氧基，低级烷基或三氟甲基; n为1,2或3; ZR3基团与杂芳族核的A-位或B-位结合; 其药学上可接受的盐; 及其旋光异构体，可用作缓冲六氢-1H-喹啉[4,3,2-ef] [1,4]苯并氧氮杂记忆功能障碍的中间体是相关化合物，并且用于缓解记忆功能障碍。

    Fused heterocyclic derivatives of 1,2,3,4-tetrahydroacridine
    36.
    发明授权
    Fused heterocyclic derivatives of 1,2,3,4-tetrahydroacridine 失效
    1,2,3,4-四氢吖啶的稠合杂环衍生物

    公开(公告)号：US4927820A

    公开(公告)日：1990-05-22

    申请号：US276259

    申请日：1988-11-25

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

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

    IPC分类号： A61K31/47 ,  A61K31/535 ,  A61P25/28 ,  C07D471/06 ,  C07D498/06

    CPC分类号： C07D471/06

    摘要： There are disclosed compounds having the formula ##STR1## where R.sub.1 is hydrogen, loweralkyl or arylloweralkyl;Z is hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, nitro or trifluoromethyl;Y is O or NR.sub.2, R.sub.2 being hydrogen, loweralkyl or arylloweralkyl; andX is CR.sub.3, CHR.sub.3, C.dbd.O, C.dbd.S or CHN(CH.sub.3).sub.2, R.sub.3 being hydrogen, loweralkyl or aryl;stereo isomers thereof and pharmaceutically acceptable acid addition salts thereof, which are useful for the treatment of various memory dysfunctions characterized by decreased cholinergic function, such as Alzheimer's disease.

    Isoxazolobenzoxazepines
    37.
    发明授权
    Isoxazolobenzoxazepines 失效
    异氮杂苯并氧氮杂

    公开(公告)号：US4873234A

    公开(公告)日：1989-10-10

    申请号：US226930

    申请日：1988-08-01

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

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

    IPC分类号： 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, ##STR3## where R.sub.1 and R.sub.2 are independently (a) H, (b) lower alkyl, (c) arylloweralkyl, (d) lower alkylene ##STR4## where Z is H, halogen, loweralkyl, loweralkoxy, CF.sub.3, nitro or amino and n is a integer of 1 to 3; ##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 to 2; ##STR7## wherein R.sub.4 is H or loweralkyl and m' is an integer of 3 to 4; ##STR8## where Z and n are as previously defined; ##STR9## where m'" is an integer of 1,2 or 3 ##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 ##STR12## where R.sub.7 is loweralkyl, aryl, or arylloweralkyl; ##STR13## where R.sub.5 and R.sub.6 are as previously defined; and the pharmaceutically acceptable acid addition salts thereof and where applicable to the geometric, stereo and optical isomers thereof.

    摘要翻译： 本发明涉及具有下列通式的异恶唑基苯并氮杂吖庚因：其中X 1是H; X2是H或OH; 或者X 1和X 2一起是羰基氧，或者是（1）H，（2）低级烷基，（3）芳基低级烷基，（4）低级炔基，（5）低级链烯基，其中R 1和R 2独立地是 a）H，（b）低级烷基，（c）芳基低级烷基，（d）低级亚烷基，其中Z是H，卤素，低级烷基，低级烷氧基，CF 3，硝基或氨基，n是1至3的整数; 其中n“为1〜3的整数; 或（f）R 1和R 2与氮原子一起是取代或未取代的式为“IMAGE”的哌啶子基或吡咯烷子基，其中R 3为H，低级烷基或芳基，m为1至2的整数; （7）其中R4为H或低级烷基，m'为3〜4的整数; （8）其中Z和n如前所定义; （9）其中m“是1,2或3的整数（10）其中R 5和R 6是低级烷基，芳基低级烷基或独立地与N原子一起形成取代的 或未取代的式（I）的哌啶子基或吡咯烷子基，其中R 3和m如前所定义，其中R 7是低级烷基，芳基或芳基低级烷基; （12）其中R5和R6如前所定义; 和其药学上可接受的酸加成盐，并且适用于其几何，立体和旋光异构体。

    1,2,3,4-tetrahydro-1,9-acridinediamines, pharmaceutical compositions and use
    38.
    发明授权
    1,2,3,4-tetrahydro-1,9-acridinediamines, pharmaceutical compositions and use 失效
    1,2,3,4-四氢-1,9-吖啶亚胺，药物组合物和用途

    公开(公告)号：US4868177A

    公开(公告)日：1989-09-19

    申请号：US269038

    申请日：1988-11-29

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

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

    IPC分类号： A61K31/435 ,  A61P25/28 ,  C07D219/10 ,  C07D221/16 ,  C07D401/04

    CPC分类号： C07D401/04 ,  C07D219/10 ,  C07D221/16

    摘要： There are disclosed compounds having the formula ##STR1## where n is 1, 2 or 3;X is hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, nitro or trifluoromethylR.sub.1 and R.sub.2 are each independently hydrogen, lower alkyl or arylloweralkyl, but both may not be arylloweralkyl simultaneously;R.sub.3 and R.sub.4 are each independently hydrogen, lower alkyl, arylloweralkyl, formyl or lower alkylcarbonyl, or alternatively the group --NR.sub.3 R.sub.4 taken as a whole constitutes ##STR2## stereo isomers thereof and pharmaceutically acceptable acid addition salts thereof, which are useful for the treatment of various memory dysfunctions characterized by decreased cholinergic function, such as Alzheimer's disease.