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38 条记录 (耗时 0.02 秒)

    N-[substituted alkylidene]fused-bicycloalkylidene quinolinamines useful for enhancing the cholinergic function in a mammal
    4.
    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。

    N-(pyrrol-l-yl)pyridinamines
    5.
    发明授权
    N-(pyrrol-l-yl)pyridinamines 失效
    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

    9-amino-1,4ethano-1,2,3,4-tetrahydroacridine and related compounds
    8.
    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。