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121 条记录 (耗时 0.046 秒)

    4- and 6-carbamates related to physostigmine and intermediates for the preparation thereof
    94.
    发明授权
    4- and 6-carbamates related to physostigmine and intermediates for the preparation thereof 失效
    与毒扁豆碱相关的4-和6-氨基甲酸酯及其制备的中间体

    公开(公告)号：US5726323A

    公开(公告)日：1998-03-10

    申请号：US708590

    申请日：1996-09-05

    申请人： Edward J. Glamkowski ,  Barbara E. Kurys

    发明人： Edward J. Glamkowski ,  Barbara E. Kurys

    IPC分类号： C07D209/34 ,  C07D487/04

    CPC分类号： C07D487/04 ,  C07D209/34

    摘要： This invention relates to 4- and 6-carbamates related to physostigmine of the formula ##STR1## where R.sub.1 is alkyl, cycloalkyl, bicycloalkyl, aryl or arylloweralkyl; R.sub.2 is hydrogen or alkyl or the group --NR.sub.1 R.sub.2 taken together forms a monocyclic or bicyclic ring of 5 to 12 carbons; m is 0, 1, or 2; each X is independently hydrogen, halogen, loweralkyl, nitro or amino; and the pharmaceutically acceptable acid addition salts thereof, and where applicable, the geometric and optical isomers and racemic mixtures thereof. This invention also relates to novel intermediates useful in the preparation of the 4- and 6-carbamates. The compounds of this invention display utility for alleviating various memory dysfunctions characterized by a decreased cholinergic function, such as Alzheimer's disease.

    摘要翻译： 本发明涉及与式（I）的毒扁豆碱相关的4-和6-氨基甲酸酯，其中R1是烷基，环烷基，双环烷基，芳基或芳基低级烷基; R 2是氢或烷基，或者-NR 1 R 2一起形成5至12个碳的单环或双环; m为0,1或2; 每个X独立地是氢，卤素，低级烷基，硝基或氨基; 及其药学上可接受的酸加成盐，以及适用的几何和光学异构体及其外消旋混合物。 本发明还涉及可用于制备4-和6-氨基甲酸酯的新型中间体。 本发明的化合物显示用于减轻由胆碱能功能降低（诸如阿尔茨海默病）所特征的各种记忆功能障碍的效用。

    Memory enhancing and analgesic 1,2,3,3a,8,8a-Hexahydro-3a,8(and 1,3a,8)-Di (and Tri)methylpyrrolo(2,3-b) indoles
    95.
    发明授权
    Memory enhancing and analgesic 1,2,3,3a,8,8a-Hexahydro-3a,8(and 1,3a,8)-Di (and Tri)methylpyrrolo(2,3-b) indoles 失效
    记忆增强和止痛1,2,3,3a，8,8a-六氢-3a，8（和1,3a，8）-Di（和三）甲基吡咯并（2,3-b）吲哚

    公开(公告)号：US5663190A

    公开(公告)日：1997-09-02

    申请号：US962080

    申请日：1992-10-16

    申请人： Richard L. Hamer ,  Grover C. Helsley ,  Edward J. Glamkowski ,  Yulin Chiang

    发明人： Richard L. Hamer ,  Grover C. Helsley ,  Edward J. Glamkowski ,  Yulin Chiang

    IPC分类号： A61K31/40 ,  A61K31/44 ,  A61K31/495 ,  A61K31/535 ,  A61P25/04 ,  A61P25/28 ,  C07D487/04 ,  A61K31/405 ,  C07D487/12

    CPC分类号： C07D487/04

    摘要： There are described compounds of the formula ##STR1## where (a) X is O or S;(b) R is H, loweralkyl, ##STR2## where Y is O or S; R.sub.2 is alkyl, cycloalkyl, bicycloalkyl, cycloalkenyl, aryl, arylloweralkyl, heteroaryl or heteroarylloweralkyl, R.sub.3 is H or alkyl, or the group --NR.sub.2 R.sub.3 taken as a whole is 1-pyrrolidinyl, 1-piperldinyl, 4-morpholinyl, 4-thiomorpholinyl, 1-piperazinyl, 4-methyl-1-piperazinyl or 2-(2,6-dichlorophenylimino)-1-imidazolidinyl) and R.sub.4 is hydrogen, loweralkyl, arylloweralkyl, diarylloweralkyl, aryl or heteroaryl,(c) m is 1 or 2;(d) each Z is independently H, loweralkyl, halogen, nitro, --NH.sub.2, loweralkylcarbonylamino, arylcarbonylamino, loweralkoxycarbonylamino or loweralkylamino, and(e) R.sub.1 is H, loweralkyl, arylloweralkyl, heteroarylloweralkyl, cycloalkylmethyl or loweralkenylmethyl,with the proviso that when X is O, m is 1, Z is H and R.sub.1 is methyl, R is not --CONHCH.sub.3, --CONHC.sub.6 H.sub.5, hydrogen, methyl or ethyl and that when X is O, m is 1 and Z and R.sub.1 are both hydrogen, R is not hydrogen or methyl, and pharmaceutically acceptable acid addition salts thereof which are useful as memory-enhancing and analgesic agents.

    摘要翻译： 描述了式（IMAGE）的化合物，其中（a）X是O或S; （b）R是H，低级烷基，其中Y是O或S; R2是烷基，环烷基，二环烷基，环烯基，芳基，芳基低级烷基，杂芳基或杂芳基低级烷基，R3是H或烷基，或者作为整体的基团-NR2R3是1-吡咯烷基，1-哌嗪基，4-吗啉基，4-硫代吗啉基， 1-哌嗪基，4-甲基-1-哌嗪基或2-（2,6-二氯苯基亚氨基）-1-咪唑烷基），R4是氢，低级烷基，芳基低级烷基，二芳基低级烷基，芳基或杂芳基，（c）m是1或2; （d）每个Z独立地是H，低级烷基，卤素，硝基，-NH 2，低级烷基羰基氨基，芳基羰基氨基，低级烷氧基羰基氨基或低级烷基氨基，和（e）R 1是H，低级烷基，芳基低级烷基，杂芳基低级烷基，环烷基甲基或低级链烯基甲基，条件是当X 是O，m是1，Z是H，R1是甲基，R不是-CONHCH3，-CONHC6H5，氢，甲基或乙基，当X是O时，m是1，Z和R1都是氢，R不是 氢或甲基及其药学上可接受的酸加成盐，其可用作记忆增强剂和止痛剂。

    Memory enhancing and analgesic 1,2,3,3a,8,8a,-hexahydro-3a,8(and 1,3a,8)-di(and tri)methylpyrrolo[2,3-b] indoles
    97.
    发明授权
    Memory enhancing and analgesic 1,2,3,3a,8,8a,-hexahydro-3a,8(and 1,3a,8)-di(and tri)methylpyrrolo[2,3-b] indoles 失效
    记忆增强和止痛1,2,3,3a，8,8a， - 六氢-3a，8（和1,3a，8） - 二（和三）甲基吡咯并[2,3-b]吲哚

    公开(公告)号：US5639892A

    公开(公告)日：1997-06-17

    申请号：US466013

    申请日：1995-06-06

    申请人： R. Richard L. Hamer ,  Grover C. Helsley ,  Edward J. Glamkowski ,  Yulin Chiang

    发明人： R. Richard L. Hamer ,  Grover C. Helsley ,  Edward J. Glamkowski ,  Yulin Chiang

    IPC分类号： A61K31/40 ,  A61K31/44 ,  A61K31/495 ,  A61K31/535 ,  A61P25/04 ,  A61P25/28 ,  C07D487/04

    CPC分类号： C07D487/04

    摘要： There are described compounds of the formula ##STR1## where X is O or S;(b) R is H, loweralkyl, ##STR2## where Y is O or S; R.sub.2 is alkyl, cycloalkyl, bicyclcalkyl, cycloalkenyl, aryl, arylloweralkyl, heteroaryl or heteroarylloweralkyl, R.sub.3 is H or alkyl, or the group --NR.sub.2.sub.R.sub.3 taken as a whole is 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 4-thiomorpholinyl, 1-piperazinyl, 4-methyl-1-piperazinyl or 2-(2,6-dichlorophenylimino)-1-imidazolidinyl) and R.sub.4 is hydrogen, loweralkyl, arylloweralkyl, diarylloweralkyl, aryl or heteroaryl,(c) m is 1 or 2;(d) each Z is independently H, loweralkyl, halogen, nitro, --NH.sub.2, loweralkylcarbonylamino, arylcarbonylamino, loweralkoxycarbonylamino or loweralkylamino, and(e) R.sub.1 is H, loweralkyl, arylloweralkyl, heheroarylloweralkyl, cycloalkylmethyl or loweralkenylmethyl, with the proviso that when X is O, m is l, Z is H and R.sub.1 is methyl, R is not --CONHCH.sub.3, --CONHC.sub.6 H.sub.5, hydrogen, methyl or ethyl, and that when X is O, m is l and Z and R.sub.1 are both hydrogen, R is not hydrogen or methyl, and, pharmaceutically acceptable acid addition salts thereof which are useful as memory-enhancing and analgesic agents.

    摘要翻译： 描述了式（I）的化合物，其中X是O或S; （b）R是H，低级烷基，其中Y是O或S; R2是烷基，环烷基，双环烷基，环烯基，芳基，芳基低级烷基，杂芳基或杂芳基低级烷基，R3是H或烷基，或作为整体的基团-NR2R3是1-吡咯烷基，1-哌啶基，4-吗啉基，4-硫代吗啉基， 1-哌嗪基，4-甲基-1-哌嗪基或2-（2,6-二氯苯基亚氨基）-1-咪唑烷基），R4是氢，低级烷基，芳基低级烷基，二芳基低级烷基，芳基或杂芳基，（c）m是1或2; （d）每个Z独立地是H，低级烷基，卤素，硝基，-NH 2，低级烷基羰基氨基，芳基羰基氨基，低级烷氧基羰基氨基或低级烷基氨基，和（e）R 1是H，低级烷基，芳基低级烷基，杂芳基芳基低级烷基，环烷基甲基或低级烯基甲基，条件是当X 是O，m是1，Z是H，R1是甲基，R不是-CONHCH3，-CONHC6H5，氢，甲基或乙基，当X是O时，m是1，Z和R1都是氢，R是 不是氢或甲基，和其药学上可接受的酸加成盐，其可用作记忆增强剂和止痛剂。