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    Anxiolytic aroyl piperidinyl and piperazinylacyl pyrroles
    2.
    发明授权
    Anxiolytic aroyl piperidinyl and piperazinylacyl pyrroles 失效
    溶血性芳酰基哌啶基和哌嗪基酰基吡咯

    公开(公告)号：US5565456A

    公开(公告)日：1996-10-15

    申请号：US403966

    申请日：1995-03-15

    申请人： Richard J. Carmosin ,  John R. Carson ,  Philip Pitis

    发明人： Richard J. Carmosin ,  John R. Carson ,  Philip Pitis

    IPC分类号： C07D207/32 ,  C07D207/335 ,  C07D401/06 ,  C07D403/12 ,  A61K31/445 ,  A61K31/505 ,  C07D401/14

    CPC分类号： C07D207/335 ,  C07D401/06 ,  C07D403/12

    摘要： Aroyl(piperidinyl and piperazinyl)acyl pyrroles of the following formula have anxiolytic activity: ##STR1## wherein, Y is selected from the group consisting of N, CH or COH;A.sup.1 is selected from the group consisting of ##STR2## n is an integer from 1 to 5; R1 is selected from the group consisting of H and C.sub.1-4 alkyl;R.sup.2 and R.sup.3 are selected from the group consisting of H and C.sub.1-4 alkyl;R.sup.4 is selected from the group consisting of halo, C.sub.1-4 alkyl, hydroxy, C.sub.1-4 alkoxy, nitro, amino, C.sub.1-4 acylamino, cyano, trihaloC.sub.1-4 alkyl, C.sub.1-4 alkylsulfonyl, C.sub.1-4 alkylsulfinyl and C.sub.1-4 acyl; andR.sup.5 is selected from the group consisting of halo, C.sub.1-4 alkyl, hydroxy, C.sub.1-4 alkoxy, nitro, amino, C.sub.1-4 acylamino, cyano, trihaloC.sub.1-4 alkyl, C.sub.1-4 alkylsulfonyl, C.sub.1-4 alkylsulfinyl and C.sub.1-4 acyl; and acid addition salts thereof.

    摘要翻译： 下式的芳酰基（哌啶基和哌嗪基）酰基吡咯具有抗焦虑活性：p由N，CH或COH组成; A1选自 + TR ，n是1至5的整数; R 1选自H和C 1-4烷基; R2和R3选自H和C1-4烷基; R 4选自卤素，C 1-4烷基，羟基，C 1-4烷氧基，硝基，氨基，C 1-4酰氨基，氰基，三卤代C 1-4烷基，C 1-4烷基磺酰基，C 1-4烷基亚磺酰基和C 1-4酰基; R 5选自卤素，C 1-4烷基，羟基，C 1-4烷氧基，硝基，氨基，C 1-4酰氨基，氰基，三卤代C 1-4烷基，C 1-4烷基磺酰基，C 1-4烷基亚磺酰基和C 1-4酰基; 及其酸加成盐。

    Hexahydropyrrolizine compounds useful as analgesics
    3.
    发明授权
    Hexahydropyrrolizine compounds useful as analgesics 失效
    六氢吡咯啉化合物可用作镇痛药

    公开(公告)号：US4800207A

    公开(公告)日：1989-01-24

    申请号：US115960

    申请日：1987-11-02

    申请人： Richard J. Carmosin ,  John R. Carson

    发明人： Richard J. Carmosin ,  John R. Carson

    IPC分类号： C07D487/04 ,  C07D487/02 ,  A61K31/40

    CPC分类号： C07D487/04

    摘要： Hexahydropyrrolizines of the formula (I): ##STR1## wherein A is a 3-7 carbon or hetero-containing ring,R.sup.1 is a substituent, andx is 0-3.Also, pharmaceutical compositions for treating pain and methods for synthesis and use as well as novel intermediates in the synthesis.

    摘要翻译： 式（I）的六氢吡咯啉：其中A为3-7碳或含杂环，R1为取代基，x为0-3。 另外，用于治疗疼痛的药物组合物和合成和使用方法以及合成中的新型中间体。

    4-substituted octahydroquinolizine analgesic compounds and octahydroquinolizinium intermediates
    4.
    发明授权
    4-substituted octahydroquinolizine analgesic compounds and octahydroquinolizinium intermediates 失效
    4-取代八氢喹诺酮镇痛化合物和八氢喹啉鎓中间体

    公开(公告)号：US4716172A

    公开(公告)日：1987-12-29

    申请号：US850631

    申请日：1986-04-10

    申请人： Richard J. Carmosin ,  John R. Carson

    发明人： Richard J. Carmosin ,  John R. Carson

    IPC分类号： A61K31/435 ,  A61P25/04 ,  C07D455/02 ,  A61K31/345

    CPC分类号： C07D455/02

    摘要： Octahydroquinolizine and corresponding octahydroquinolizinium compounds of formulae (I) and (Va): ##STR1## where A is a 3 to 7 membered carbocyclic ring, R.sup.1 is a substituent, n is 0-2, x is 0-3, and Y is an anion. Also, pharmaceutical compositions for treating pain containing (I) and methods for synthesis and use as well as novel intermediates in the synthesis.

    摘要翻译： 八氢喹啉和相应的式（I）和（Va）的八氢喹啉鎓化合物：其中A为3至7元碳环，R1为取代基，n为0-2，x为0-3，Y为 阴离子 另外，用于治疗含有（I）的疼痛的药物组合物及其合成和使用方法以及合成中的新型中间体。

    4-arylcyclopenta[c]pyrrole analgesics
    9.
    发明授权
    4-arylcyclopenta[c]pyrrole analgesics 失效
    4-芳基环戊[c]吡咯镇痛药

    公开(公告)号：US5541217A

    公开(公告)日：1996-07-30

    申请号：US443142

    申请日：1995-05-17

    申请人： Richard J. Carmosin ,  John R. Carson ,  Philip M. Pitis

    发明人： Richard J. Carmosin ,  John R. Carson ,  Philip M. Pitis

    IPC分类号： C07D209/70 ,  A61K31/395 ,  C07D209/02

    CPC分类号： C07D209/70

    摘要： The 4-arylcyclopenta[c]pyrroles of the following formula are effective analgesics: ##STR1## including stereoisomers and pharmaceutically acceptable salts thereof, wherein ##STR2## with the proviso that the 3a and 6a hydrogens are cis and where there is a 4-position hydroxy then such is trans to the 3a and 6a hydrogens, andwith the proviso that R.sup.b is not hydrogen when the 4-position aryl is cis to the 3a and 6a hydrogens and there is no hydroxy at the 4-position.

    摘要翻译： 下式的4-芳基环戊基[c]吡咯是有效的镇痛药：其包括立体异构体及其药学上可接受的盐，其中，图3a和6a所示氢是顺式的， 然后4位羟基反应到3a和6a氢，条件是当4-位芳基与3a和6a氢是顺式的并且在4-位没有羟基时，Rb不是氢。

    5-substituted octahydroindolizine analgesics compounds and 7-keto intermediates
    10.
    发明授权
    5-substituted octahydroindolizine analgesics compounds and 7-keto intermediates 失效
    5-取代八氢吲哚啉镇痛药和7-酮中间体

    公开(公告)号：US4689329A

    公开(公告)日：1987-08-25

    申请号：US826167

    申请日：1986-02-04

    申请人： Richard J. Carmosin ,  John R. Carson

    发明人： Richard J. Carmosin ,  John R. Carson

    IPC分类号： A61K31/435 ,  A61P25/04 ,  C07D471/04 ,  A61K31/40

    CPC分类号： C07D471/04

    摘要： Octahydroindolizidines and corresponding ketones of the formulae (I) and (II): ##STR1## where A is a 3-7 carbon or hetero-containing ring, R.sup.1 is a substituent, n is 0-6 and x is 0-3. Also, pharmaceutical compositions for treating pain containing (I) or (II) and methods for synthesis and use as well as novel intermediates in the synthesis. A

    摘要翻译： （I）和（II）的八氢二吲嗪和相应的酮：其中A是3-7碳或含杂环，R1是取代基，n是0- 6，x为0-3。 另外，用于治疗含有（I）或（II）的疼痛的药物组合物及其合成和使用方法以及合成中的新型中间体。