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    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。

    Medicaments
    5.
    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。

    Use of tetrahydrocarbazone derivatives as 5HT.sub.1 receptor agonists
    6.
    发明授权
    Use of tetrahydrocarbazone derivatives as 5HT.sub.1 receptor agonists 失效
    四氢咔唑衍生物作为5HT1受体激动剂的用途

    公开(公告)号：US5464864A

    公开(公告)日：1995-11-07

    申请号：US167846

    申请日：1993-12-23

    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

    CPC分类号： C07D209/88

    摘要： ##STR1## Use of a compound of general formula (I), wherein R
    1 represents hydrogen, halogen, trifluoromethyl, nitro, hydroxy, C
    1-6 alkyl, C
    1-6 alkoxy, arylC
    1-6 alkoxy, --CO
    2 R
    4 , --(CH
    2 )
    n CN, --(CH
    2 )
    n CONR
    5 R
    6 , --(CH
    2 )
    n SO
    2 NR
    5 R
    6 , C
    1-6 alkanoylamino(CH
    2 )
    n , or C
    1-6 alkylsulphonylamino(CH
    2 )
    n ; R
    4 represents hydrogen, C
    1-6 alkyl or arylC
    1-6 alkyl; R
    5 and R
    6 each independently represent hydrogen or C
    1-6 alkyl, or R
    5 and R
    6 together with the nitrogen atom to which they are attached form a ring; n represents 0, 1 or 2; and R
    2 and R
    3 each independently represent hydrogen, C
    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
    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： PCT No.PCT / GB92 / 01082 Sec。 371日期：1993年12月23日 102（e）日期1993年12月23日PCT提交1992年6月17日PCT公布。 第WO93 / 00086号公报 （I）通式（I）的化合物的用途，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， （CH2）nCN， - （CH2）nCONR5R6， - （CH2）nSO2NR5R6，C1-6烷酰基氨基（CH2）n或C1-6烷基磺酰基氨基（CH2）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。

    Substituted indoles and their use as 5-HT.sub.3 receptor antagonists
    7.
    发明授权
    Substituted indoles and their use as 5-HT.sub.3 receptor antagonists 失效
    取代的吲哚及其用作5-HT 3受体拮抗剂

    公开(公告)号：US4920127A

    公开(公告)日：1990-04-24

    申请号：US155756

    申请日：1988-02-16

    申请人： Francis D. King ,  Karen A. Joiner

    发明人： Francis D. King ,  Karen A. Joiner

    IPC分类号： C07D451/04 ,  C07D453/02

    CPC分类号： C07D451/04 ,  C07D453/02

    摘要： Compounds of formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## wherein L is NH or O;R.sub.1 is hydrogen, fluoro or chloro;R.sub.2 and R.sub.5 are independently hydrogen or C.sub.1-6 alkyl or together are a bond; orR.sub.2 and R.sub.3 and/or R.sub.4 and R.sub.5, together are C.sub.2-7 polymethylene or --(CH.sub.2).sub.m --O--(CH.sub.2).sub.x -- where m and x. are 1 to 5 such that m+x is 2 to 6;R.sub.4 is C.sub.1-7 acyl, C.sub.1-6 alkoxycarbonyl, hydroxycarbonyl, aminocarbonyl optionally substituted by one or two C.sub.1-6 alkyl groups, CF.sub.3, C.sub.1-6 alkyl substituted by C.sub.1-6 alkoxy, C.sub.1-6 alkylthio or by C.sub.1-6 alkoxycarbonyl, or R.sub.4 is phenyl or phenyl-C.sub.1-4 alkyl optionally substituted in the phenyl ring by one or two of halogen, C.sub.1-6 alkyl or C.sub.1-6 alkoxy;Z is a group of formula (a), (b) or (c).

    Pharmaceutically useful esters and amides
    10.
    发明授权
    Pharmaceutically useful esters and amides 失效
    药用有用的酯和酰胺

    公开(公告)号：US4822795A

    公开(公告)日：1989-04-18

    申请号：US78105

    申请日：1987-07-27

    申请人： Francis D. King

    发明人： Francis D. King

    IPC分类号： C07D519/00 ,  A61K31/46 ,  C07D451/04

    CPC分类号： C07D519/00

    摘要： Compounds of formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## wherein L is NH or O;X is N or CR.sub.3 wherein R.sub.3 is hydrogen or C.sub.1-6 alkoxy;Y is N or CR.sub.4 wherein R.sub.4 is hydrogen, halogen, CF.sub.3, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkylsulphinyl, C.sub.1-7 acyl, cyano, C.sub.1-6 alkoxycarbonyl, C.sub.1-7 acylamino, hydroxy, nitro or amino, aminocarbonyl, or aminosulphonyl, optionally N-substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, and C.sub.3-8 cycloalkyl C.sub.1-4 alkyl or disubstituted by C.sub.4 or C.sub.5 polymethylene; phenyl or phenyl C.sub.1-4 alkyl group optionally substituted in the phenyl ring by one or two of halogen, C.sub.1-6 alkoxy or C.sub.1-6 alkyl groups;R.sub.1 and R.sub.2 are independently selected from hydrogen, or halogen;Z is a group of formula (a), (b) or (c): ##STR2## wherein n is 2 or 3; p is 1 or 2; q is 1 to 3; r is 1 to 3; andR.sub.5 or R.sub.6 is C.sub.1-4 alkyl; having 5-HT.sub.3 antagonist activity, a process for their preparation and their use as pharmaceuticals.

    摘要翻译： 式（I）化合物或其药学上可接受的盐：其中L是NH或O; X是N或CR 3，其中R 3是氢或C 1-6烷氧基; Y是N或CR 4，其中R4是氢，卤素，CF3，C1-6烷基，C1-6烷氧基，C1-6烷硫基，C1-6烷基磺酰基，C1-6烷基亚磺酰基，C1-7酰基，氰基，C1-6烷氧羰基 ，C 1-7酰基氨基，羟基，硝基或氨基，氨基羰基或氨基磺酰基，任选被选自C 1-6烷基，C 3-8环烷基和C 3-8环烷基C 1-4烷基中的一个或两个基团N-取代或被二取代的 C4或C5聚亚甲基; 苯基或苯基C 1-4烷基，任选在苯环中被一个或两个卤素，C 1-6烷氧基或C 1-6烷基取代; R 1和R 2独立地选自氢或卤素; Z是式（a），（b）或（c）的基团：其中n为2或3;（c）其中n为2或3; p为1或2; q为1〜3; r为1〜3; R5或R6是C1-4烷基; 具有5-HT 3拮抗剂活性，其制备方法及其作为药物的用途。