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91 条记录 (耗时 0.059 秒)

    Indole derivatives
    45.
    发明授权
    Indole derivatives 失效

    公开(公告)号：US5559129A

    公开(公告)日：1996-09-24

    申请号：US466645

    申请日：1995-06-06

    申请人： John E. Macor ,  Martin J. Wythes

    发明人： John E. Macor ,  Martin J. Wythes

    IPC分类号： A61K31/40 ,  C07D401/06 ,  C07D403/06 ,  A61K37/40

    CPC分类号： A61K31/40 ,  C07D401/06 ,  C07D403/06

    摘要： Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, X and n are as defined in the claims and the pharmaceutically acceptable salts thereof are new. These compounds are useful psychotherapeutics and are potent serotonin (5-HT.sub.1) agonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain, chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting hypertensives and vasodilators. A process for forming indoles by transition metal catalyzed cyclization of dihalogenated intermediate is also disclosed.

    Acylaminoindole derivatives as 5-ht1 agonists
    46.
    发明授权
    Acylaminoindole derivatives as 5-ht1 agonists 失效
    酰基氨基吲哚衍生物作为5-ht1激动剂

    公开(公告)号：US5498626A

    公开(公告)日：1996-03-12

    申请号：US295792

    申请日：1994-09-14

    申请人： John E. Macor

    发明人： John E. Macor

    IPC分类号： A61K31/40 ,  A61K31/395 ,  A61K31/404 ,  A61K31/4427 ,  A61K31/445 ,  A61P3/04 ,  A61P9/12 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  C07D401/06 ,  C07D403/06 ,  C07D403/14

    CPC分类号： C07D403/06 ,  C07D403/14

    摘要： ##STR1## Compounds of formula (I) where n is 0, 1, or 2; m is 0 or 1; Y and W are each an amino acid residue; R
    1 is hydrogen, C
    1 -C
    6 alkyl, C
    3 -C
    6 alkenyl, C
    3 -C
    6 alkynyl, aryl, C
    1 -C
    3 alkylaryl, or C
    1 -C
    3 alkylheteroaryl, and --(CH
    2 )
    p R
    3 ; R
    2 is CF
    3 , C
    1 -C
    6 alkyl, aryl, C
    1 -C
    3 alkylaryl, and --OR
    5 ; R
    3 is cyano, trifluoromethyl, or --OR
    4 ; R
    4 is hydrogen, C
    1 -C
    6 alkyl, C
    1 -C
    3 alkylaryl, or aryl; R
    5 is C
    1 -C
    6 alkyl, C
    1 -C
    3 alkylaryl, or aryl; R
    6 is hydrogen, --OR
    7 , or --NHCOR
    7 ; R
    7 is hydrogen, C
    1 to C
    6 alkyl, aryl or C
    1 to C
    3 alkyl-aryl; p is 1, 2, or 3; and the above aryl groups and the aryl moieties of the above alkyl-aryl groups are independently selected from phenyl and substituted phenyl, wherein said substituted phenyl may be substituted with one to three groups selected from C
    1 to C
    4 alkyl, halogen, hydroxy, cyano, carboxamide, nitro, and C
    1 to C
    4 alkoxy and the pharmaceutically acceptable salts thereof. These compounds are useful in treating migraine and other disorders. These compound are useful psychotherapeutics and are potent serotonin (5-HT
    1 ) agonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain, and chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting antihypertensives and vasodilators.

    摘要翻译： PCT No.PCT / US93 / 01807 Sec。 371日期：1994年9月14日 102（e）1994年9月14日PCT 1993年3月4日PCT公布。 出版物WO93 / 21180 PCT （I）其中n为0,1或2的式（I）化合物; m为0或1; Y和W各自为氨基酸残基; R 1是氢，C 1 -C 6烷基，C 3 -C 6烯基，C 3 -C 6炔基，芳基，C 1 -C 3烷基芳基或C 1 -C 3烷基杂芳基，和 - （CH 2）p R 3; R2是CF3，C1-C6烷基，芳基，C1-C3烷基芳基和-OR5; R3是氰基，三氟甲基或-OR4; R4是氢，C1-C6烷基，C1-C3烷基芳基或芳基; R5是C1-C6烷基，C1-C3烷基芳基或芳基; R6是氢，-OR7或-NHCOR7; R 7为氢，C 1至C 6烷基，芳基或C 1至C 3烷基 - 芳基; p为1,2或3; 并且上述芳基和上述烷基 - 芳基的芳基部分独立地选自苯基和取代的苯基，其中所述取代的苯基可以被一至三个选自C 1 -C 4烷基，卤素，羟基，氰基， 甲酰胺，硝基和C1至C4烷氧基及其药学上可接受的盐。 这些化合物可用于治疗偏头痛和其他疾病。 这些化合物是有用的精神治疗药物，是有效的5-羟色胺（5-HT1）激动剂，可用于治疗抑郁症，焦虑症，进食障碍，肥胖症，药物滥用，丛集性头痛，偏头痛，疼痛和慢性阵发性血尿素和头痛相关 血管疾病和由血清素能神经传递缺陷引起的其他疾病。 该化合物也可用作中枢作用的抗高血压药和血管扩张剂。