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    11-substituted 5H,11H-pyrrolo(2,1-C) (1,4)benzoxazepines as antipsychotic and analgesic agents
    6.
    发明授权
    11-substituted 5H,11H-pyrrolo(2,1-C) (1,4)benzoxazepines as antipsychotic and analgesic agents 失效
    11-取代的5H，11H-吡咯并（2,1-C）（1,4）苯并氧杂吖庚因作为抗精神病药和镇痛药

    公开(公告)号：US4667039A

    公开(公告)日：1987-05-19

    申请号：US811135

    申请日：1985-12-19

    申请人： Richard C. Effland ,  Larry Davis ,  Kevin J. Kapples

    发明人： Richard C. Effland ,  Larry Davis ,  Kevin J. Kapples

    IPC分类号： C07D401/06 ,  C07D498/04

    CPC分类号： C07D401/06

    摘要： There are described to novel 11-substituted 5H,11H-pyrrolo[2,1-c][1,4]benzoxazepines of the general formula ##STR1## where m and n are each independently 0, 1 or 2 and m+n is 1 or 2, X and Y are each independently hydrogen, loweralkyl or halogen, and R is hydrogen, cyano, --C(NH.sub.2)NOH, ##STR2## unsubstituted loweralkyl, or substituted loweralkyl having one to three substituents each of which being independently cyano, hydroxy, cyclohexyl, furyl, thienyl, ##STR3## k being 1, 2 or 3, W being each independently hydrogen, halogen, hydroxy, loweralkyl, trifluoromethyl, loweralkoxy, nitro, amino, diloweralkylamino, phenoxy, or benzyloxy, and Z being hydrogen, loweralkyl or halogen, which are useful as antipsychotic and analgesic agents; novel intermediate compounds therefor; and methods of synthesizing the foregoing compounds.

    摘要翻译： 描述了通式为其中m和n各自独立地为0,1或2的新的11-取代的5H，11H-吡咯并[2,1-c] [1,4]苯并氧氮杂，m和n各自独立地为0,1或2，m + n为1或2，X和Y各自独立地为氢，低级烷基或卤素，R为氢，氰基，-C（NH 2）NOH，未取代的低级烷基或具有一至三个取代基的取代的低级烷基， 独立地是氰基，羟基，环己基，呋喃基，噻吩基，是1,2或3，W各自独立地为氢，卤素，羟基，低级烷基，三氟甲基，低级烷氧基，硝基，氨基 ，二卤烷基氨基，苯氧基或苄氧基，Z为氢，低级烷基或卤素，其可用作抗精神病药和止痛剂; 新型中间体化合物; 和上述化合物的合成方法。

    Spiro[(piperidine- pyrrolidine- or hexahydroazepinyl substituted) pyrrolo[2,][1,4]benzoxazepines]
    7.
    发明授权
    Spiro[(piperidine- pyrrolidine- or hexahydroazepinyl substituted) pyrrolo[2,][1,4]benzoxazepines] 失效
    螺[（哌啶 - 吡咯烷 - 或六氢氮杂吖啶基）吡咯并[2,1-c] [1,4]苯并氧氮杂]

    公开(公告)号：US4918069A

    公开(公告)日：1990-04-17

    申请号：US290343

    申请日：1988-12-29

    申请人： Richard C. Effland ,  Larry Davis ,  Kevin J. Kapples

    发明人： Richard C. Effland ,  Larry Davis ,  Kevin J. Kapples

    IPC分类号： C07D401/04 ,  C07D401/14 ,  C07D498/20

    CPC分类号： C07D401/04 ,  C07D401/14

    摘要： This invention relates to spiro-[(piperidine-, pyrrolidine-, or -hexahydroazepinyl substituted) pyrrolo[2,1-c][1,4]-benzoxazepines] having the following formula ##STR1## wherein R is hydrogen, lower alkyl, arylloweralkyl, acyl, lower alkenyl, lower alkynyl, and loweralkylbenzisoxazole; X is hydrogen, halogen, loweralkoxy, and trifluoromethyl; Y is hydrogen; 2' or 3' acyl, formyl, carbinol of the formula ##STR2## where R.sub.1 and R.sub.2 are the same or different and are independently hydrogen, loweralkyl, arylloweralkyl, aryl, loweralkenyl, lower alkynyl and lower alkylbenzisoxazole; loweralkyl, loweralkenyl and halogen; and n is an integer of 1 to 3. The compounds of this invention display utility as analgesic and antihypertensive agents.

    摘要翻译： 本发明涉及具有下列结构式的螺[ - （哌啶 - ，吡咯烷 - 或六氢氮杂环己烷基取代的）吡咯并[2,1-c] [1,4] - 苯并恶唑]，其中R是氢，低级烷基， 芳基低级烷基，酰基，低级烯基，低级炔基和低级烷基苯并异恶唑; X是氢，卤素，低级烷氧基和三氟甲基; Y是氢; 其中R 1和R 2相同或不同并且独立地是氢，低级烷基，芳基低级烷基，芳基，低级烯基，低级炔基和低级烷基苯并异恶唑;式2'或3'酰基，甲酰基甲醇， 低级烷基，低级烯基和卤素; 并且n为1至3的整数。本发明化合物显示出作为镇痛和抗高血压药物的用途。

    Antihypertensive spiro(piperidine- pyrrolidine- or hexahydroazepinyl substituted) pyrrolo(2,1-c)(1,4)benzoxazepines)
    8.
    发明授权
    Antihypertensive spiro(piperidine- pyrrolidine- or hexahydroazepinyl substituted) pyrrolo(2,1-c)(1,4)benzoxazepines) 失效
    抗高血压螺（哌啶 - 吡咯烷或六氢氮杂环己基取代的）吡咯并（2,1-c）（1,4）苯并氧氮杂）

    公开(公告)号：US5215984A

    公开(公告)日：1993-06-01

    申请号：US440947

    申请日：1989-11-24

    申请人： Richard C. Effland ,  Larry Davis ,  Kevin J. Kapples

    发明人： Richard C. Effland ,  Larry Davis ,  Kevin J. Kapples

    IPC分类号： C07D401/04 ,  C07D401/14 ,  C07D498/20

    CPC分类号： C07D401/04 ,  C07D401/14

    摘要： This invention relates to spiro-](piperidine-, pyrrolidine-, or -hexahydroazepinyl substituted) pyrrolo[2,1-c][1,4]-benzoxazepines] having the following formula ##STR1## wherein R is hydrogen, lower alkyl, arylloweralkyl, acyl, lower alkenyl, lower alkynyl, and loweralkylbenzisoxazole; X is hydrogen, halogen, loweralkoxy, and trifluoromethyl; Y is hydrogen; 2' or 3' acyl, formyl, carbinol of the formula ##STR2## where R.sub.1 and R.sub.2 are the same or different and are independently hydrogen, loweralkyl, arylloweralkyl, aryl, loweralkenyl, lower alkynyl and lower alkylbenzisoxazole; loweralkyl, loweralkenyl and halogen; and n is an integer of 1 to 3. The compounds of this invention display utility as analgesic and antihypertensive agents.

    摘要翻译： 本发明涉及具有下列结构式的螺 - - （哌啶 - ，吡咯烷 - 或六氢氮杂环己烷基取代的）吡咯并[2,1-c] [1,4] - 苯并恶唑[其中R是氢，低级烷基， 芳基低级烷基，酰基，低级烯基，低级炔基和低级烷基苯并异恶唑; X是氢，卤素，低级烷氧基和三氟甲基; Y是氢; 其中R 1和R 2相同或不同并且独立地是氢，低级烷基，芳基低级烷基，芳基，低级烯基，低级炔基和低级烷基苯并异恶唑;式2'或3'酰基，甲酰基甲醇， 低级烷基，低级烯基和卤素; 并且n为1至3的整数。本发明化合物显示出作为镇痛和抗高血压药物的用途。

    11-substituted 5H,11H-pyrrolo[2,1-c][1,4]benzoxazepines as antipsychotic and analgesic agents
    9.
    发明授权
    11-substituted 5H,11H-pyrrolo[2,1-c][1,4]benzoxazepines as antipsychotic and analgesic agents 失效
    11-取代的5H，11H-吡咯并[2,1-c] [1,4]苯并氧杂吖庚因作为抗精神病药和镇痛药

    公开(公告)号：US4681879A

    公开(公告)日：1987-07-21

    申请号：US713938

    申请日：1985-03-20

    申请人： Richard C. Effland ,  Larry Davis ,  Kevin J. Kapples

    发明人： Richard C. Effland ,  Larry Davis ,  Kevin J. Kapples

    IPC分类号： C07D401/06 ,  C07D498/04 ,  C07D413/04 ,  A61K31/40 ,  A61K31/445

    CPC分类号： C07D401/06

    摘要： There are described novel 11-substituted 5H,11H-pyrrolo[2,1-c][1,4]benzoxazepines of the general formula ##STR1## where m and n are each independently 0, 1 or 2 and m+n is 1 or 2, X and Y are each independently hydrogen, loweralkyl or halogen, and R is hydrogen, cyano, --C(NH.sub.2)NOH, ##STR2## unsubstituted loweralkyl, or substituted loweralkyl having one to three substituents each of which being independently cyano, hydroxy, cycloalkyl of 3-6 carbon atoms, furyl, thienyl, ##STR3## k being 1, 2 or 3, W being each indepentently hydrogen, halogen, hydroxy, loweralkyl, trifluoromethyl, loweralkoxy, nitro, amino, diloweralkylamino, phenoxy, or benzyloxy, and Z being hydrogen, loweralkyl or halogen, which are useful as antipsychotic and analgesic agents; novel intermediate compounds therefor; and methods of synthesizing the foregoing compounds.

    摘要翻译： 描述了通式（IMA）（I）的新颖的11取代的5H，11H-吡咯并[2,1-c] [1,4]苯并氧杂吖庚因，其中m和n各自独立地为0,1或2，m + n为1或2，X和Y各自独立地为氢，低级烷基或卤素，R为氢，氰基，-C（NH 2）NOH，未取代的低级烷基或具有一至三个取代基的取代的低级烷基， 独立地是氰基，羟基，3-6个碳原子的环烷基，呋喃基，噻吩基，1,2或3个，各自独立地为氢，卤素，羟基，低级烷基，三氟甲基， 低级烷氧基，硝基，氨基，二低级烷基氨基，苯氧基或苄氧基，Z为氢，低级烷基或卤素，可用作抗精神病药和镇痛药; 新型中间体化合物; 和上述化合物的合成方法。

    N-(pyrrol-l-yl)pyridinamines
    10.
    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