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    BICYCLE THIOPHENES AND THIAZOLES
    95.
    发明申请
    BICYCLE THIOPHENES AND THIAZOLES 审中-公开
    BICYCLE THIOPHENES和THIAZOLES

    公开(公告)号：US20020025974A1

    公开(公告)日：2002-02-28

    申请号：US09442175

    申请日：1999-11-16

    发明人： ELLEN W. BAXTER ,  ROBERT E. BOYD ,  JOHN R. CARSON ,  MICHELLE C. JETTER ,  ALLEN B. REITZ

    IPC分类号： A61K031/4178 ,  A61K031/427 ,  C07D277/02 ,  C07D233/00

    CPC分类号： C07D409/12 ,  C07D417/06

    摘要： Certain imidazo benzthiophenes/thiazoles of the formula: 1 where Z is N or C-Y (Y is absent where the imidazole containing substituent is attached at the 3-position); n is 0 or 1; Y is independently selected from the group consisting of hydrogen, C1-4alkyl, bromine, chlorine, iodide, trifluoromethyl, C1-4alkoxy, nullSO2NH2 and nitro; X is independently selected from the group consisting of hydrogen, hydroxy, C1-4 alkyl, C1-4 alkoxy, trifluoromethyl and phenyl; and A is independently selected from the group consisting of hydrogen, C1-4alkyl, chlorine, trifluoromethyl, C1-4alkoxy and nitro, or is absent where the imidazole containing substituent is attached at the 2-position; are null2-adrenoceptor modulators which are useful in the treatment of hypertension, glaucoma, sexual dysfunction, depression, attention deficit hyperactivity disorder, the need for anesthesia, cardiac arrythmia or the need for analgesia.

    摘要翻译： 某些下式的咪唑并苯并噻吩/噻唑：其中Z为N或C-Y（Y为不含咪唑的取代基在3-位）; n为0或1; Y独立地选自氢，C 1-4烷基，溴，氯，碘，三氟甲基，C 1-4烷氧基，-SO 2 NH 2和硝基; X独立地选自氢，羟基，C 1-4烷基，C 1-4烷氧基，三氟甲基和苯基; 并且A独立地选自氢，C 1-4烷基，氯，三氟甲基，C 1-4烷氧基和硝基，或者如果含有咪唑的取代基在2-位连接，则不存在; 是治疗高血压，青光眼，性功能障碍，抑郁症，注意力缺陷多动障碍，麻醉需要，心脏心律失常或需要镇痛的α2-肾上腺素能受体调节剂。

    Use of N-(4-aryl-thiazol-2-yl)-sulfonamides
    97.
    发明授权
    Use of N-(4-aryl-thiazol-2-yl)-sulfonamides 失效
    使用N-（4-芳基 - 噻唑-2-基） - 磺酰胺

    公开(公告)号：US5958910A

    公开(公告)日：1999-09-28

    申请号：US197070

    申请日：1998-11-20

    申请人： Andrea Cesura ,  Stephan Rover

    发明人： Andrea Cesura ,  Stephan Rover

    IPC分类号： C07D277/20 ,  A61K31/00 ,  A61K31/425 ,  A61K31/426 ,  A61K31/427 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/4439 ,  A61P9/00 ,  A61P25/00 ,  A61P25/08 ,  A61P25/18 ,  A61P25/20 ,  A61P25/28 ,  A61P31/00 ,  A61P37/00 ,  A61P37/02 ,  A61P43/00 ,  C07D277/00 ,  C07D277/02 ,  C07D277/22 ,  C07D277/50 ,  C07D277/52 ,  C07D417/12

    CPC分类号： A61K31/427 ,  A61K31/426

    摘要： The invention is concerned with the use of sulfonamide derivatives of the general formula ##STR1## wherein R Signifies lower-alkyl, phenyl, benzyl, naphthyl, pyridyl or thienyl, optionally substituted by one or more lower-alkyl, lower-alkoxy, lower-alkyl carbonyl-amino, halogen, cycloalkyl, nitro, amino, methylenedioxy, phenoxy or benzyloxy substituents, and the aromatic rings, can, in turn, be substituted by nitro, halogen or amino,R.sup.1 -R.sup.4 signify hydrogen, halogen, hydroxy, lower-alkyl, nitro, cyano, amino, lower-alkoxy, benzyloxy, trifluoromethyl or phenyl, optionally substituted by one or more lower-alkyl, trifluoromethyl, nitro, amino or hydroxy substituents, and wherein R.sup.1 and R.sup.2 or R.sup.2 and R.sup.3 together can form a benzene ring which optionally can be substituted by halogen, trifluoromethyl, nitro, lower-alkyl or lower alkoxy,and of their pharmaceutically acceptable salts as kynurenin-3-hydroxylase inhibitors in the control or prevention of neuro-degenerative disorders, neurological disorders resulting from an activation of the immune system, or psychiatric illnesses and, respectively, for the production of corresponding medicaments.

    摘要翻译： 本发明涉及使用以下通式的磺酰胺衍生物，其中R表示低级烷基，苯基，苄基，萘基，吡啶基或噻吩基，任选地被一个或多个低级烷基，低级烷氧基，低级烷基羰基 - 氨基，卤素，环烷基，硝基，氨基，亚甲二氧基，苯氧基或苄氧基取代基，芳环可以被硝基，卤素或氨基取代，R 1 -R 4表示氢，卤素，羟基，低级烷基， 硝基，氰基，氨基，低级烷氧基，苄氧基，三氟甲基或苯基，任选地被一个或多个低级烷基，三氟甲基，硝基，氨基或羟基取代基取代，并且其中R 1和R 2或R 2和R 3一起可以形成苯环 其任选地可以被卤素，三氟甲基，硝基，低级烷基或低级烷氧基取代，以及它们的药学上可接受的盐作为犬尿胆素-3-羟化酶抑制剂在控制或预防神经退行性疾病，神经障碍 是由于免疫系统的激活或精神疾病，以及分别用于生产相应的药物而产生的。