利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

222 条记录 (耗时 0.022 秒)

    Medical use for tachykinin antagonists
    3.
    发明授权
    Medical use for tachykinin antagonists 失效
    速激肽拮抗剂的医疗用途

    公开(公告)号：US07214692B2

    公开(公告)日：2007-05-08

    申请号：US09985679

    申请日：2001-11-05

    申请人： Russell Michael Hagan ,  Keith Thomas Bunce

    发明人： Russell Michael Hagan ,  Keith Thomas Bunce

    IPC分类号： A61K31/445 ,  A61K31/165

    CPC分类号： C07D487/08 ,  A61K31/44 ,  A61K31/445 ,  A61K31/57 ,  A61K45/06 ,  Y10S514/872 ,  A61K31/435 ,  A61K31/415 ,  A61K31/165 ,  A61K2300/00

    摘要： The present invention relates to the use of tachykinin antagonists, including substance P antagonists and other neurokinin antagonists, in the treatment of emesis. Also described are novel tachykinin antagonists of formula (I), processes for their preparation, pharmaceutical compositions containing them and their medical use. wherein R represents the ring A or 2-pyridinyl or 2-pyridinyl-N-oxide; R1 is selected from halogen atoms and C1-4alkyl, C1-4alkoxy, trifluoromethyl, and S(O)nC1-4alkyl groups; R2 and R3, which may be the same or different, each independently are selected from hydrogen and halogen atoms and C1-4alkyl, C1-4alkoxy, trifluoromethyl and cyano groups; n represents zero, 1 or 2; and pharmaceutically acceptable salts and solvates thereof.

    摘要翻译： 本发明涉及速激肽拮抗剂（包括P物质拮抗剂和其他神经激肽拮抗剂）在治疗呕吐中的用途。 还描述了式（I）的新型速激肽拮抗剂，其制备方法，含有它们的药物组合物及其医疗用途。 其中R表示环A或2-吡啶基或2-吡啶基-N-氧化物; R 1选自卤素原子和C 1-4烷基，C 1-4烷氧基，三氟甲基和S（O） C 1-4烷基; R 2和R 3可以相同或不同，各自独立地选自氢和卤素原子和C 1-4烷基 C 1-4烷氧基，三氟甲基和氰基; n表示0，1或2; 及其药学上可接受的盐和溶剂化物。

    Novel medical use for tachykinin antagonists
    6.
    发明申请
    Novel medical use for tachykinin antagonists 失效
    速激肽拮抗剂的新型医疗用途

    公开(公告)号：US20020052351A1

    公开(公告)日：2002-05-02

    申请号：US09985679

    申请日：2001-11-05

    申请人： Glaxo Group Limited

    发明人： Russell Michael Hagan ,  Keith Thomas Bunce

    IPC分类号： A61K038/16 ,  A61K031/704 ,  A61K031/7048 ,  A61K031/7068 ,  A61K031/4375 ,  A61K031/573 ,  A61K033/24

    CPC分类号： C07D487/08 ,  A61K31/44 ,  A61K31/445 ,  A61K31/57 ,  A61K45/06 ,  Y10S514/872 ,  A61K31/435 ,  A61K31/415 ,  A61K31/165 ,  A61K2300/00

    摘要： The present invention relates to the use of tachykinin antagonists, including substance P antagonists and other neurokinin antagonists, in the treatment of emesis. Also described are novel tachykinin antagonists of formula (I), processes for their preparation, pharmaceutical compositions containing them and their medical use. 1 wherein R represents the ring A 2 or 2-pyridinyl or 2-pyridinyl-N-oxide; R1 is selected from halogen atoms and C1-4alkyl, C1-4alkoxy, trifluoromethyl, and S(O)nC1-4alkyl groups; R2 and R3, which may be the same or different, each independently are selected from hydrogen and halogen atoms and C1-4alkyl, C1-4alkoxy, trifluoromethyl and cyano groups; n represents zero, 1 or 2; and pharmaceutically acceptable salts and solvates thereof.

    摘要翻译： 本发明涉及速激肽拮抗剂（包括P物质拮抗剂和其他神经激肽拮抗剂）在治疗呕吐中的用途。 还描述了式（I）的新型速激肽拮抗剂，其制备方法，含有它们的药物组合物及其医疗用途。 其中R表示环A或2-吡啶基或2-吡啶基-N-氧化物; R 1选自卤素原子和C 1-4烷基，C 1-4烷氧基，三氟甲基和S（O）n C 1-4烷基; R 2和R 3可以相同或不同，各自独立地选自氢和卤素原子和C 1-4烷基，C 1-4烷氧基，三氟甲基和氰基; n表示0，1或2; 及其药学上可接受的盐和溶剂化物。

    Methods for treating behavioral and other disorders using optically pure R(+) ondansetron
    7.
    发明授权
    Methods for treating behavioral and other disorders using optically pure R(+) ondansetron 失效
    使用光学纯的R（+）昂丹司琼治疗行为和其他障碍的方法

    公开(公告)号：US5962494A

    公开(公告)日：1999-10-05

    申请号：US12428

    申请日：1998-01-23

    申请人： James W. Young

    发明人： James W. Young

    IPC分类号： A61K9/08 ,  A61K9/48 ,  A61K31/415 ,  A61K31/4178

    CPC分类号： A61K31/4178 ,  A61K31/415 ,  Y10S514/872

    摘要： Methods and compositions are disclosed utilizing the optically pure R(+) isomer of ondansetron. This compound is a potent drug for the treatment of nausea and vomiting associated with chemotherapy and radiation therapy, while avoiding the concomitant liability of adverse effects associated with the racemic mixture of ondansetron. The R(+) isomer of ondansetron is also useful for the treatment of behavioral disorders such as mood anxiety and schizophrenia, and such other conditions as may be related to R(+) ondansetron's activity as a competitive antagonist of serotonin receptor subtype 5-HT.sub.3 such as disorders of gastrointestinal motility, depression, migraine, and as an aid for alcohol withdrawal, nicotine withdrawal, and drug (benzodiazepine et al.) withdrawal, without the concomitant liability of adverse effects associated with the racemic mixture of ondansetron. Furthermore, the R(+) isomer of ondansetron is also useful for the treatment of cognitive disorders such as dementia or age-associated memory impairment, while avoiding the concomitant liability of adverse effects associated with the racemic mixture of ondansetron.

    摘要翻译： 公开了使用昂丹司琼的光学纯的R（+）异构体的方法和组合物。 该化合物是用于治疗与化疗和放射治疗相关的恶心和呕吐的有效药物，同时避免与昂丹司琼外消旋混合物相关的副作用的伴随责任。 昂丹司琼的R（+）异构体也可用于治疗诸如情绪焦虑和精神分裂症等行为障碍，以及可能与R（+）昂丹司琼活性相关的其他条件，作为5-羟色胺受体亚型5-HT3的竞争性拮抗剂 例如消化道运动障碍，抑郁症，偏头痛，以及用于酒精戒断，尼古丁戒断和药物（苯并二氮杂类等）撤离的辅助，而不伴随昂丹司琼外消旋混合物的不良反应。 此外，昂丹司琼的R（+）异构体也可用于治疗诸如痴呆或年龄相关记忆障碍的认知障碍，同时避免与昂丹司琼的外消旋混合物相关的副作用的伴随责任。

    Compositions using optically pure R(+) ondansetron
    8.
    发明授权
    Compositions using optically pure R(+) ondansetron 失效
    使用光学纯的R（+）昂丹司琼的组合物

    公开(公告)号：US5712302A

    公开(公告)日：1998-01-27

    申请号：US513368

    申请日：1995-08-10

    申请人： James W. Young

    发明人： James W. Young

    IPC分类号： A61K9/08 ,  A61K9/48 ,  A61K31/415 ,  A61K31/4178 ,  A61K31/45

    CPC分类号： A61K31/4178 ,  A61K31/415 ,  Y10S514/872

    摘要： Methods and compositions are disclosed utilizing the optically pure R(+) isomer of ondansetron. This compound is a potent drug for the treatment of nausea and vomiting associated with chemotherapy and radiation therapy, while avoiding the concomitant liability of adverse effects associated with the racemic mixture of ondansetron. The R(+) isomer of ondansetron is also useful for the treatment of behavioral disorders such as mood anxiety and schizophrenia, and such other conditions as may be related to R(+) ondansetron's activity as a competitive antagonist of serotonin receptor subtype 5-HT.sub.3 such as disorders of gastrointestinal motility, depression, migraine, and as an aid for alcohol withdrawal, nicotine withdrawal, and drug (benzodiazepine et al.) withdrawal, without the concomitant liability of adverse effects associated with the racemic mixture of ondansetron. Furthermore, the R(+) isomer of ondansetron is also useful for the treatment of cognitive disorders such as dementia or age-associated memory impairment, while avoiding the concomitant liability of adverse effects associated with the racemic mixture of ondansetron.

    摘要翻译： 公开了使用昂丹司琼的光学纯的R（+）异构体的方法和组合物。 该化合物是用于治疗与化疗和放射治疗相关的恶心和呕吐的有效药物，同时避免与昂丹司琼外消旋混合物相关的副作用的伴随责任。 昂丹司琼的R（+）异构体也可用于治疗诸如情绪焦虑和精神分裂症等行为障碍，以及可能与R（+）昂丹司琼活性相关的其他条件，作为5-羟色胺受体亚型5-HT3的竞争性拮抗剂 例如消化道运动障碍，抑郁症，偏头痛，以及用于酒精戒断，尼古丁戒断和药物（苯并二氮杂类等）撤离的辅助，而不伴随昂丹司琼外消旋混合物的不良反应。 此外，昂丹司琼的R（+）异构体也可用于治疗诸如痴呆或年龄相关记忆障碍的认知障碍，同时避免与昂丹司琼的外消旋混合物相关的副作用的伴随责任。

    Derivatives of substituted imidazo benzoxazin-1-one and process for their preparation
    9.
    发明授权
    Derivatives of substituted imidazo benzoxazin-1-one and process for their preparation 失效
    取代的咪唑并苯并恶嗪-1-酮的衍生物及其制备方法

    公开(公告)号：US5364854A

    公开(公告)日：1994-11-15

    申请号：US70860

    申请日：1993-06-03

    申请人： Mario Varasi ,  Franco Heidempergher ,  Claudio Arrigoni ,  Carla Caccia

    发明人： Mario Varasi ,  Franco Heidempergher ,  Claudio Arrigoni ,  Carla Caccia

    IPC分类号： A61K31/535 ,  A61P25/26 ,  C07D498/04 ,  C07D519/00 ,  C07D487/04 ,  A61K35/00

    CPC分类号： C07D519/00 ,  Y10S514/872

    摘要： Derivatives of 2,3,3a,4-tetrahydro-2-azabicyclo alkyl-1H-imidazo[5,1,-c][1,4]benzoxazin-1-one are provided of general formula (I) ##STR1## in which inter alia R.sub.3 represents ##STR2## wherein n is an integer of 1 or 2 and R.sub.8 is hydrogen, C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, formyl or C.sub.2 -C.sub.6 alkanoyl; and the pharmaceutically acceptable salts thereof, which are useful in the treatment of CNS disorders, gut motility disorders, emesis and migraine, as cognition activators, anti-drug addiction agents and analgesic.

    摘要翻译： 2,3,3a，4-四氢-2-氮杂双环烷基-1H-咪唑并[5,1，-c] [1,4]苯并恶嗪-1-酮的衍生物由通式（I）提供。 I），其中特别是R3表示其中n是1或2的整数，R8是氢，未被取代或被苯基，C 2 -C 4烯基，C 2 -C 4炔基，甲酰基或C 2 -C 6取代的C 1 -C 6烷基 烷酰基; 及其药学上可接受的盐，其可用于治疗CNS障碍，肠蠕动障碍，呕吐和偏头痛，作为认知激活剂，抗药成瘾剂和止痛剂。