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    4-Aminoethoxy indolone derivatives
    1.
    发明授权
    4-Aminoethoxy indolone derivatives 失效
    4-氨基乙氧基吲哚酮衍生物

    公开(公告)号：US5760070A

    公开(公告)日：1998-06-02

    申请号：US909799

    申请日：1997-08-12

    申请人： Richard Eric Mewshaw ,  Michael Byron Webb

    发明人： Richard Eric Mewshaw ,  Michael Byron Webb

    IPC分类号： C07D409/12 ,  A61K31/40

    CPC分类号： C07D409/12

    摘要： A compound of the formula I: ##STR1## in which Y is hydrogen, halogen or alkoxy; R is hydrogen or alkylthio; R.sub.1 is hydrogen or alkyl; X is hydrogen, halogen, alkoxy, alkyl or phenyl; n is one of the integers 1, 2, 3 or 4; or a pharmaceutically acceptable salt thereof are inhibitors of dopamine synthesis and release, useful in the treatment of schizophrenia, Parkinson's Disease, Tourette's Syndrome, alcohol addiction, cocaine addiction, and addiction to analogous drugs.

    摘要翻译： 式I的化合物：其中Y是氢，卤素或烷氧基; R是氢或烷硫基; R1是氢或烷基; X是氢，卤素，烷氧基，烷基或苯基; n是整数1,2,3或4之一; 或其药学上可接受的盐是多巴胺合成和释放的抑制剂，可用于治疗精神分裂症，帕金森病，图雷特综合征，酒精成瘾，可卡因成瘾和类似药物的成瘾。

    4-aminoethoxy indoles
    2.
    发明授权
    4-aminoethoxy indoles 失效
    4-氨基乙氧基吲哚

    公开(公告)号：US5958965A

    公开(公告)日：1999-09-28

    申请号：US909803

    申请日：1997-08-12

    申请人： Richard Eric Mewshaw ,  Michael Byron Webb

    发明人： Richard Eric Mewshaw ,  Michael Byron Webb

    IPC分类号： C07D209/08 ,  C07D209/30 ,  A01N43/38 ,  C07D209/04

    CPC分类号： C07D209/30 ,  C07D209/08

    摘要： Compounds of the formula: ##STR1## in which R.sub.1 is hydrogen, alkyl, cycloalkylalkyl, arylalkyl, (haloaryl)alkyl, (alkoxyaryl)alkyl, thienylmethyl, furanylmethyl, pyridinylmethyl, alkylphenyl, 4-fluorobutyrophenone or 6-fluoro-1,2-benzisoxazol-yl-propyl; X is hydrogen, halogen, cyano, alkyl, acetyl, trifluoroacetyl, trifluoromethyl or formyl; Y is hydrogen, halogen, alkoxy or alkyl; or a pharmaceutically acceptable salt thereof are inhibitors of dopamine synthesis and release, useful in the treatment of schizophrenia, Parkinson's Disease, Tourette's Syndrome, alcohol addiction, cocaine addiction, and addiction to analagous drugs and they also have affinity for the 5-HT.sub.1A receptors which characterizes them as useful in the treatment of diseases attending disturbances in the serotinergic systems, such as anxiety, stress, depression, sexual dysfunctions and sleep disturbances.

    摘要翻译： 下式的化合物：其中R 1是氢，烷基，环烷基烷基，芳基烷基，（卤代芳基）烷基，（烷氧基芳基）烷基，噻吩基甲基，呋喃基甲基，吡啶基甲基，烷基苯基，4-氟苯丙酮或6-氟-1,2-苯并异恶唑 丙基; X是氢，卤素，氰基，烷基，乙酰基，三氟乙酰基，三氟甲基或甲酰基; Y是氢，卤素，烷氧基或烷基; 或其药学上可接受的盐是多巴胺合成和释放的抑制剂，其可用于治疗精神分裂症，帕金森氏病，图雷特综合征，酒精成瘾，可卡因成瘾和对肛门药物的成瘾，并且它们也对5-HT1A受体具有亲和力， 表征它们在治疗参与血清素能系统紊乱的疾病中有用，例如焦虑，压力，抑郁，性功能障碍和睡眠障碍。

    4-aminoethoxy indolone derivatives
    4.
    发明授权
    4-aminoethoxy indolone derivatives 失效
    4-氨基乙氧基吲哚酮衍生物

    公开(公告)号：US5817690A

    公开(公告)日：1998-10-06

    申请号：US909800

    申请日：1997-08-12

    申请人： Richard Eric Mewshaw

    发明人： Richard Eric Mewshaw

    IPC分类号： C07D209/34 ,  C07D401/12 ,  C07D403/12 ,  A61K31/40 ,  C07D209/12

    CPC分类号： C07D401/12 ,  C07D209/34 ,  C07D403/12

    摘要： A compound of the formula I: ##STR1## in which Y is hydrogen, halogen or lower alkoxy; R.sub.1 is hydrogen, lower alkyl or aryl(lower)alkyl; R.sub.2 is hydrogen, lower alkyl or --(CH.sub.2).sub.n X.sub.p Ar, where X is oxygen or carbonyl; Ar is cycloalkyl, aryl or arylaryl, oxindolyl, benzimidazolyl, indolyl, 2-oxobenzimidazolyl or 2-thioxobenzimidazolyl; or R.sub.1 and R.sub.2, taken together with the nitrogen atom to which they are attached, complete a 3,4-dihydro-1H-isoquinolinyl or 1,3-dihydro-isoindolyl; n is one of the integers 1,2,3,4,5 or 6; p is one of the integers 0 or 1; or a pharmaceutically acceptable salt thereof are inhibitors of dopamine synthesis and release, useful in the treatment of schizophrenia, Parkinson's Disease, Tourette's Syndrome, alcohol addiction, cocaine addiction, and addiction to analogous drugs.

    摘要翻译： 式I的化合物：其中Y是氢，卤素或低级烷氧基; R1是氢，低级烷基或芳基（低级）烷基; R2是氢，低级烷基或 - （CH2）nXpAr，其中X是氧或羰基; Ar是环烷基，芳基或芳基芳基，羟基吲哚基，苯并咪唑基，吲哚基，2-氧代苯并咪唑基或2-硫代苯并咪唑基; 或R 1和R 2与它们所连接的氮原子一起形成3,4-二氢-1H-异喹啉基或1,3-二氢 - 异吲哚基; n是整数1,2,3,4,5或6之一; p是整数0或1之一; 或其药学上可接受的盐是多巴胺合成和释放的抑制剂，可用于治疗精神分裂症，帕金森病，图雷特氏综合征，酒精成瘾，可卡因成瘾和类似药物的成瘾。

    4-aminoalkoxy-1,3-dihydro-benzoimidazol-2-thiones
    5.
    发明授权
    4-aminoalkoxy-1,3-dihydro-benzoimidazol-2-thiones 失效
    4-氨基烷氧基-1,3-二氢 - 苯并咪唑-2-硫酮

    公开(公告)号：US5972958A

    公开(公告)日：1999-10-26

    申请号：US25011

    申请日：1998-02-17

    申请人： James Albert Nelson ,  Richard Eric Mewshaw ,  Uresh Shantilal Shah

    发明人： James Albert Nelson ,  Richard Eric Mewshaw ,  Uresh Shantilal Shah

    IPC分类号： C07D235/28 ,  C07D401/12 ,  C07D409/12 ,  A61K31/415 ,  A61K31/47

    CPC分类号： C07D401/12 ,  C07D235/28 ,  C07D409/12

    摘要： This invention relates to a novel series of compounds having potency at the dopamine D.sub.2 receptor which are illustrated by the following Formula I: ##STR1## wherein: R.sup.1 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sup.2 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sup.3 is selected from hydrogen, straight-chain and branched alkyl group having up to 10 carbon atoms, cyclohexylmethyl or --CH.sub.2).sub.m Ar where Ar is phenyl, naphthyl, thienyl, furanyl or pyridinyl, each optionally substituted by one or two substituents selected independently from C.sub.1 -C.sub.6 alkyl, halogen, C.sub.1 -C.sub.6 alkoxide, trifluoromethyl, 4-fluorobutyrophenone;or NR.sup.2 R.sup.3 is 1, 2, 3, 4-tetrahydroquinolin-1-yl or 1, 2, 3, 4-tetrahydroisoquinolin-2-yl;m is 1-5;n is 1 or 2;Y is halogen, C.sub.1 -C.sub.6 alkyl, and C.sub.1 -C.sub.6 alkoxy; or a pharmaceutically acceptable salt thereof.

    摘要翻译： 本发明涉及一种在多巴胺D2受体上具有效力的新一系列化合物，其由下式I表示：其中：R1是氢或C1-C6烷基; R2是氢或C1-C6烷基; R 3选自具有至多10个碳原子的氢，直链和支链烷基，环己基甲基或-CH 2）mAr，其中Ar是苯基，萘基，噻吩基，呋喃基或吡啶基，各自任选被一个或两个独立地选自 C1-C6烷基，卤素，C1-C6醇盐，三氟甲基，4-氟代丁酰苯; 或NR 2 R 3是1,2,3,4-四氢喹啉-1-基或1,2,3,4,5-四氢异喹啉-2-基; m为1-5; n为1或2; Y是卤素，C 1 -C 6烷基和C 1 -C 6烷氧基; 或其药学上可接受的盐。

    4-aminoethoxyindazole derivatives
    6.
    发明授权
    4-aminoethoxyindazole derivatives 失效
    4-氨基乙氧基吲唑衍生物

    公开(公告)号：US5872144A

    公开(公告)日：1999-02-16

    申请号：US024600

    申请日：1998-02-17

    申请人： Richard Eric Mewshaw ,  Anthonie Johan Verwijs

    发明人： Richard Eric Mewshaw ,  Anthonie Johan Verwijs

    IPC分类号： C07D231/56 ,  C07D409/12 ,  A61K31/415

    CPC分类号： C07D231/56 ,  C07D409/12

    摘要： This invention relates to dopamine D.sub.2 agonists of the formula ##STR1## wherein: Y is hydrogen, halogen, or C.sub.1 -C.sub.6 alkoxy;R.sup.1 is hydrogen or C.sub.1 -C.sub.6 alkyl;X is methylene, oxygen or carbonyl;Ar is phenyl or thienyl, each optionally substituted with 1-2 groups independently selected from C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkyl, halogen, trifluoromethyl and phenyl;n=1-4,or pharmaceutically acceptable salts thereof. Dopamine D.sub.2 agonists are useful in the treatment of schizophrenia, Tourette's syndrome, drug and alcohol addiction, and also useful in the treatment of Parkinson's disease.

    摘要翻译： 本发明涉及下式的多巴胺D2激动剂：其中：Y是氢，卤素或C 1 -C 6烷氧基; R1是氢或C1-C6烷基; X是亚甲基，氧或羰基; Ar是苯基或噻吩基，各自任选被1-2个独立地选自C 1 -C 6烷氧基，C 1 -C 6烷基，卤素，三氟甲基和苯基的基团取代; n = 1-4，或其药学上可接受的盐。 多巴胺D2激动剂可用于治疗精神分裂症，Tourette综合征，药物和酒精成瘾，也可用于治疗帕金森病。