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13 条记录 (耗时 0.015 秒)

    Medicaments
    1.
    发明授权
    Medicaments 失效
    药剂

    公开(公告)号：US5637611A

    公开(公告)日：1997-06-10

    申请号：US442719

    申请日：1995-05-15

    申请人： Francis D. King ,  Laramie M. Gaster ,  Alberto J. Kaumann ,  Rodney C. Young

    发明人： Francis D. King ,  Laramie M. Gaster ,  Alberto J. Kaumann ,  Rodney C. Young

    IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K31/4427 ,  A61K31/445 ,  A61K31/454 ,  A61P25/04 ,  A61P25/06 ,  A61P43/00 ,  C07D20060101 ,  C07D209/88 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D209/82

    CPC分类号： C07D209/88

    摘要： Use of a compound of general formula (I): ##STR1## wherein: R.sup.1 represents hydrogen, halogen, trifluoromethyl, nitro, hydroxy, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, arylC.sub.1-6 alkoxy, --CO.sub.2 R.sup.4, --(CH.sub.2).sub.n CN, --(CH.sub.2).sub.n CONR.sup.5 R.sup.6, --(CH.sub.2).sub.n SO.sub.2 NR.sup.5 R.sup.6, C.sub.1-6 alkanoylamino (CH.sub.2).sub.n, or C.sub.1-6 alkylsulphonylamino (CH.sub.2).sub.n ;R.sup.4 represents hydrogen, C.sub.1-6 alkyl or arylC.sub.1-6 alkyl;R.sup.5 and R.sup.6 each independently represent hydrogen or C.sub.1-6 alkyl, or R.sup.5 and R.sup.6 together with the nitrogen atom to which they are attached form a ring;n represents 0, 1 or 2; andR.sup.2 and R.sup.3 each independently represent hydrogen, C.sub.1-6 alkyl or benzyl or together with the nitrogen atom to which they are attached form a pyrrolidino, piperidino or hexahydroazepino ring;or a physiologically acceptable salt thereof, in the manufacture of a medicament for the treatment of a condition where a 5-HT.sub.1 -like agonist is indicated, for example migraine. Novel compounds of formula (I), processes for preparing them and pharmaceutical compositions containing them are also described.

    摘要翻译： 通式（I）的化合物：其中：R 1表示氢，卤素，三氟甲基，硝基，羟基，C 1-6烷基，C 1-6烷氧基，芳基C 1-6烷氧基，-CO 2 R 4， - （CH 2 ）nCN， - （CH 2）nCONR 5 R 6， - （CH 2）n SO 2 NR 5 R 6，C 1-6烷酰基氨基（CH 2）n或C 1-6烷基磺酰基氨基（CH 2）n; R 4表示氢，C 1-6烷基或芳基C 1-6烷基; R 5和R 6各自独立地表示氢或C 1-6烷基，或者R 5和R 6与它们所连接的氮原子一起形成环; n表示0,1或2; 并且R 2和R 3各自独立地表示氢，C 1-6烷基或苄基，或与它们所连接的氮原子一起形成吡咯烷子基，哌啶子基或六氢氮杂环; 或其生理上可接受的盐在制备用于治疗其中指示5-HT1样激动剂的病症的药物中，例如偏头痛。 还描述了新的式（I）化合物，其制备方法和含有它们的药物组合物。

    Azabicyclic compounds as 5-HT4 receptor antagonists
    4.
    发明授权
    Azabicyclic compounds as 5-HT4 receptor antagonists 失效
    氮杂环化合物作为5-HT 4受体拮抗剂

    公开(公告)号：US5552398A

    公开(公告)日：1996-09-03

    申请号：US204428

    申请日：1994-11-14

    申请人： Francis D. King ,  Laramie M. Gaster ,  Paul A. Wyman

    发明人： Francis D. King ,  Laramie M. Gaster ,  Paul A. Wyman

    IPC分类号： A61K31/40 ,  A61K31/435 ,  A61K31/55 ,  A61P9/06 ,  A61P43/00 ,  C07D405/12 ,  C07D413/04 ,  C07D413/12 ,  C07D455/02 ,  C07D471/04 ,  C07D487/04 ,  C07D453/02 ,  C07D401/12 ,  A16K31/55

    CPC分类号： C07D405/12 ,  C07D413/04 ,  C07D413/10 ,  C07D455/02 ,  C07D471/04

    摘要： Compounds of formula (I), ##STR1## wherein L is N or CR.sub.c, wherein R.sub.c is hydrogen, alkoxy, halo, alkyl or cyano; Q is NR.sub.1, CH.sub.2, O, or S; R.sub.a is hydrogen, halo, alkyl, amino, nitro or alkoxy; R.sub.b is hydrogen, halo, alkyl or alkoxy; R.sub.1 is hydrogen, alkyl, alkenyl, aralkyl, alkanoyl, or alkanoylalkyl; R.sub.2 is alkoxy; R.sub.3 is hydrogen, chloro or fluoro; R.sub.4 is hydrogen, alkyl, amino optionally substituted by alkyl, halo, hydroxy or alkoxy; R.sub.5 is hydrogen, halo, alkyl, alkoxy, nitro, amino or alkylthio; R.sub.6 is hydrogen, halo, alkyl, alkoxy or amino; n is 0, 1, 2, 3, or 4; p and m are independently 0, 1 or 2; and R.sub.q is hydrogen or C.sub.1-6 are 5-HT.sub.4 receptor antagonists.

    摘要翻译： PCT No.PCT / GB92 / 01612 Sec。 371日期：1994年11月14日 102（e）日期1994年11月14日PCT提交1992年9月3日PCT公布。 出版物WO93 / 05040 日本1993年3月18日化学式（I），其中R为N或CRc，其中R c为氢，烷氧基，卤素，烷基或氰基;（a） Q是NR1，CH2，O或S; R a是氢，卤素，烷基，氨基，硝基或烷氧基; Rb是氢，卤素，烷基或烷氧基; R1是氢，烷基，烯基，芳烷基，烷酰基或烷酰基烷基; R2是烷氧基; R3是氢，氯或氟; R4是氢，烷基，任选被烷基，卤素，羟基或烷氧基取代的氨基; R5是氢，卤素，烷基，烷氧基，硝基，氨基或烷硫基; R6是氢，卤素，烷基，烷氧基或氨基; n为0,1,2,3或4; p和m独立地为0,1或2; Rq为氢或C1-6为5-HT4受体拮抗剂。

    Pentacyclic compounds
    6.
    发明授权
    Pentacyclic compounds 失效
    五环化合物

    公开(公告)号：US4504480A

    公开(公告)日：1985-03-12

    申请号：US472218

    申请日：1983-03-04

    申请人： Laramie M. Gaster ,  Barry S. Orlek

    发明人： Laramie M. Gaster ,  Barry S. Orlek

    IPC分类号： A61K31/55 ,  A61P25/24 ,  A61P25/26 ,  C07C67/00 ,  C07C227/00 ,  C07C229/56 ,  C07D223/14 ,  C07D223/32 ,  C07D241/38 ,  C07D487/06 ,  A61K31/495

    CPC分类号： C07D241/38 ,  C07D223/14 ,  C07D223/32 ,  C07D487/06

    摘要： Compounds of formula (I), ##STR1## or an N-oxide or pharmaceutically acceptable salt thereof, wherein R.sub.1 is hydrogen, C.sub.1-7 alkyl, C.sub.3-7 cycloalkyl, C.sub.4-7 cycloalkenyl or C.sub.1-4 alkyl substituted by C.sub.2-7 alkenyl, C.sub.2-7 alkynyl, C.sub.3-7 cycloalkyl, hydroxy, thiol, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, carboxy, C.sub.1-4 alkoxycarbonyl, C.sub.1-4 alkanoyl, amino optionally substituted by one or two C.sub.1-4 alkyl or by C.sub.4-6 polymethylene optionally containing an oxygen or nitrogen atom, aminocarbonyl optionally N-substituted by one or two C.sub.1-4 alkyl, or benzoyl or phenyl either being optionally ring-substituted by C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or trifluoromethyl, R.sub.2 and R.sub.3 are the same or different and are hydrogen, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alklthio, halogen or trifluoromethyl, m is 1 to 3 and n is 1 or 2, the hydrogen atom bonded to the C.sub.a carbon atom being trans to the hydrogen atom bonded to the C.sub.b carbon atom, having mood-modifying activity such as anti-depressant activity.

    摘要翻译： 式（I）化合物，其中R 1为氢，C 1-7烷基，C 3-7环烷基，C 4-7环烯基或C 1-4烷基取代的N-氧化物或其药学上可接受的盐 C2-7烯基，C2-7炔基，C3-7环烷基，羟基，硫醇，C1-4烷氧基，C1-4烷硫基，羧基，C1-4烷氧基羰基，C1-4烷酰基，任选被一个或两个C1- 4烷基或任选含有氧或氮原子的C4-6多亚甲基，任选被一个或两个C 1-4烷基取代的氨基羰基，或任选被C 1-4烷基，C 1-4烷氧基任意环取代的苯甲酰基或苯基 卤素或三氟甲基，R 2和R 3相同或不同，为氢，羟基，C 1-4烷基，C 1-4烷氧基，C 1-4烷硫基，卤素或三氟甲基，m为1至3，n为1或2， 与碳原子键合的氢原子反转到与Cb碳原子键合的氢原子，具有抑郁活性等情绪调节活性。

    Pentacyclic derivatives of piperazine
    7.
    发明授权
    Pentacyclic derivatives of piperazine 失效
    哌嗪的五环衍生物

    公开(公告)号：US4442098A

    公开(公告)日：1984-04-10

    申请号：US332347

    申请日：1981-12-18

    申请人： Derek V. Gardner ,  Laramie M. Gaster

    发明人： Derek V. Gardner ,  Laramie M. Gaster

    IPC分类号： A61K31/55 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  C07D223/20 ,  C07D267/20 ,  C07D471/16 ,  C07D487/04 ,  C07D498/04 ,  C07D498/16 ,  C07D513/04 ,  C07D513/16 ,  C07D471/06 ,  A61K31/495 ,  C07D498/06 ,  C07D513/06

    CPC分类号： C07D487/04 ,  C07D223/20 ,  C07D267/20

    摘要： Compounds of formula (I): ##STR1## wherein: X is CH.sub.2, O, S or NR wherein R is hydrogen or C.sub.1-4 alkyl;Y and Z are independently selected from hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or CF.sub.3 ;R.sub.1 is hydrogen, C.sub.1-6 alkyl, phenyl or phenyl-C.sub.1-4 alkyl any of which phenyl moieties may be substituted by one or more of C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or CF.sub.3 ;R.sub.2 is hydrogen, OH, C.sub.1-6 alkoxy, phenyl-C.sub.1-4 alkoxy, C.sub.1-7 acyloxy or NR.sub.4 R.sub.5 wherein R.sub.4 and R.sub.5 are independently selected from hydrogen or C.sub.1-6 alkyl; R.sub.4 is hydrogen and R.sub.5 is OH or C.sub.1-4 alkoxy; or R.sub.4 and R.sub.5 together form C.sub.3-6 polymethylene optionally interrupted by O or NR.sub.6 where R.sub.6 is hydrogen or C.sub.1-4 alkyl; or together with R.sub.1 forms an oxo group or .dbd.NOR.sub.7 wherein R.sub.7 is hydrogen or C.sub.1-6 alkyl; andR.sub.3 is hydrogen or C.sub.1-6 alkyl have useful pharmacological activity, processes for their preparation and their use.

    摘要翻译： 式（I）化合物：其中：X为CH 2，O，S或NR，其中R为氢或C 1-4烷基; Y和Z独立地选自氢，C 1-4烷基，C 1-4烷氧基，卤素或CF 3; R 1是氢，C 1-6烷基，苯基或苯基-C 1-4烷基，其中任一个苯基部分可以被一个或多个C 1-6烷基，C 1-6烷氧基，卤素或CF 3取代; R 2是氢，OH，C 1-6烷氧基，苯基-C 1-4烷氧基，C 1-7酰氧基或NR 4 R 5，其中R 4和R 5独立地选自氢或C 1-6烷基; R4是氢，R5是OH或C1-4烷氧基; 或R 4和R 5一起形成任选地被O或NR 6中断的C 3-6的多亚甲基，其中R 6是氢或C 1-4烷基; 或与R 1一起形成氧基或= NOR7，其中R 7为氢或C 1-6烷基; R3为氢或C1-6烷基具有有用的药理活性，其制备方法及其用途。

    Indeno pyrazine and benzoquinoxaline intermediates
    9.
    发明授权
    Indeno pyrazine and benzoquinoxaline intermediates 失效
    茚并吡嗪和苯醌喹喔啉中间体

    公开(公告)号：US4638066A

    公开(公告)日：1987-01-20

    申请号：US684080

    申请日：1984-12-20

    申请人： Laramie M. Gaster ,  Barry S. Orlek

    发明人： Laramie M. Gaster ,  Barry S. Orlek

    IPC分类号： A61K31/55 ,  A61P25/24 ,  A61P25/26 ,  C07C67/00 ,  C07C227/00 ,  C07C229/56 ,  C07D223/14 ,  C07D223/32 ,  C07D241/38 ,  C07D487/06 ,  C07D241/42 ,  C07D241/44 ,  C07D401/06

    CPC分类号： C07D241/38 ,  C07D223/14 ,  C07D223/32 ,  C07D487/06

    摘要： Compounds of formula (I), ##STR1## or an N-oxide or pharmaceutically acceptable salt thereof, wherein R.sub.1 is hydrogen, C.sub.1-7 alkyl, C.sub.3-7 cycloalkyl, C.sub.4-7 cycloalkenyl or C.sub.1-4 alkyl substituted by C.sub.2-7 alkenyl, C.sub.2-7 alkynyl, C.sub.3-7 cycloalkyl, hydroxy, thiol, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, carboxy, C.sub.1-4 alkoxycarbonyl, C.sub.1-4 alkanoyl, amino optionally substituted by one or two C.sub.1-4 alkyl or by C.sub.4-6 polymethylene optionally containing an oxygen or nitrogen atom, aminocarbonyl optionally N-substituted by one or two C.sub.1-4 alkyl, or benzoyl or phenyl either being optionally ring-substituted by C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or trifluoromethyl, R.sub.2 and R.sub.3 are the same or different and are hydrogen, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, halogen or trifluoromethyl, m is 1 to 3 and n is 1 or 2, the hydrogen atom bonded to the C.sub.a carbon atom being trans to the hydrogen atom bonded to the C.sub.b carbon atom, having mood-modifying activity such as anti-depressant activity.

    Pentacyclic compounds
    10.
    发明授权
    Pentacyclic compounds 失效
    五环化合物

    公开(公告)号：US4585588A

    公开(公告)日：1986-04-29

    申请号：US684038

    申请日：1984-12-20

    申请人： Laramie M. Gaster ,  Barry S. Orlek

    发明人： Laramie M. Gaster ,  Barry S. Orlek

    IPC分类号： A61K31/55 ,  A61P25/24 ,  A61P25/26 ,  C07C67/00 ,  C07C227/00 ,  C07C229/56 ,  C07D223/14 ,  C07D223/32 ,  C07D241/38 ,  C07D487/06 ,  A61K31/495

    CPC分类号： C07D241/38 ,  C07D223/14 ,  C07D223/32 ,  C07D487/06

    摘要： Compounds of formula (I), ##STR1## or an N-oxide or pharmaceutically acceptable salt thereof, wherein R.sub.1 is hydrogen, C.sub.1-7 alkyl, C.sub.3-7 cycloalkyl, C.sub.4-7 cycloalkenyl or C.sub.1-4 alkyl substituted by C.sub.2-7 alkenyl, C.sub.2-7 alkynyl, C.sub.3-7 cycloalkyl, hydroxy, thiol, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, carboxy, C.sub.1-4 alkoxycarbonyl, C.sub.1-4 alkanoyl, amino optionally substituted by one or two C.sub.1-4 alkyl or by C.sub.4-6 polymethylene optionally containing an oxygen or nitrogen atom, aminocarbonyl optionally N-substituted by one or two C.sub.1-4 alkyl, or benzoyl or phenyl either being optionally ring-substituted by C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or trifluoromethyl, R.sub.2 and R.sub.3 are the same or different and are hydrogen, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, halogen or trifluoromethyl, m is 1 to 3 and n is 1 or 2, the hydrogen atom bonded to the C.sub.a carbon atom being trans to the hydrogen atom bonded to the C.sub.b carbon atom, having mood-modifying activity such as anti-depressant activity.