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    N1-SUBSTITUTED BENZOPYRAZOLES AS INHIBITORS OF 5-HT2 RECEPTORS
    4.
    发明申请
    N1-SUBSTITUTED BENZOPYRAZOLES AS INHIBITORS OF 5-HT2 RECEPTORS 审中-公开
    作为5-HT2受体的抑制剂的N-取代的苯并噻唑

    公开(公告)号：WO0017170A3

    公开(公告)日：2000-08-03

    申请号：PCT/GB9903187

    申请日：1999-09-23

    Applicant: CEREBRUS PHARM LTD ,  ADAMS DAVID REGINALD ,  BENTLEY JONATHAN MARK ,  ROFFEY JONATHAN RICHARD ANTHON ,  DUNCTON MATTHEW ALEXANDER JAME

    Inventor： ADAMS DAVID REGINALD ,  BENTLEY JONATHAN MARK ,  ROFFEY JONATHAN RICHARD ANTHON ,  DUNCTON MATTHEW ALEXANDER JAME

    IPC: C07D231/56 ,  A61K31/415

    CPC classification number: C07D231/56

    Abstract: A chemical compound of formula (I): wherein R1 to R3 are independently selected from hydrogen and alkyl; R5 is selected from alkylthio, arylthio, alkylsulfoxyl, arylsulfoxyl, alkylsulfonyl and arylsulfonyl; R4, R6, and R7 are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, alkoxy, aryloxy, alkylthio, arylthio, arylsulfoxyl, alkylsulfoxyl, alkylsulfonyl, arylsulfonyl, amino, monoalkylamino, dialkylamino, nitro, cyano, carboxaldehyde, alkylcarbonyl, arylcarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkoxycarbonylamino, aminocarbonyloxy, monoalkylaminocarbonyloxy, dialkylaminocarbonyloxy, monoalkylaminocarbonylamino and dialkylaminocarbonylamino, and pharmaceutically acceptable salts and prodrugs thereof, and the use thereof in therapy, particularly for the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus; and sleep apnea, and particularly for the treatment of obesity.

    Abstract translation: 式（I）的化合物：其中R 1至R 3独立地选自氢和烷基; R5选自烷硫基，芳硫基，烷基亚磺酰基，芳基亚砜基，烷基磺酰基和芳基磺酰基; R4，R6和R7独立地选自氢，卤素，羟基，烷基，芳基，烷氧基，芳氧基，烷硫基，芳硫基，芳基亚砜基，烷基磺酰基，烷基磺酰基，芳基磺酰基，氨基，单烷基氨基，二烷基氨基，硝基，氰基， 芳基羰基，氨基羰基，单烷基氨基羰基，二烷基氨基羰基，烷氧基羰基氨基，氨基羰基氧基，单烷基氨基羰基氧基，二烷基氨基羰基氧基，单烷基氨基羰基氨基和二烷基氨基羰基氨基及其药学上可接受的盐和前药，以及其在治疗中的用途，特别是用于治疗中枢神经系统疾病。 损害中枢神经系统; 心血管疾病; 胃肠道疾病; 尿崩症 并且睡眠呼吸暂停，特别是用于治疗肥胖。

    INDAZOLE DERIVATIVES WITH 5-HT2 RECEPTOR ACTIVITY________________
    5.
    发明申请
    INDAZOLE DERIVATIVES WITH 5-HT2 RECEPTOR ACTIVITY________________ 审中-公开
    具有5-HT2受体活性的吲哚衍生物

    公开(公告)号：WO0012481A3

    公开(公告)日：2000-06-08

    申请号：PCT/GB9902875

    申请日：1999-09-01

    Applicant: CEREBRUS PHARM LTD ,  ADAMS DAVID REGINALD ,  BENTLEY JONATHAN MARK ,  ROFFEY JONATHAN RICHARD ANTHON ,  HAMLYN RICHARD JOHN ,  GEORGE ASHLEY ROGER

    Inventor： ADAMS DAVID REGINALD ,  BENTLEY JONATHAN MARK ,  ROFFEY JONATHAN RICHARD ANTHON ,  HAMLYN RICHARD JOHN ,  GEORGE ASHLEY ROGER

    IPC: A61K31/416 ,  A61P1/00 ,  A61P3/04 ,  A61P7/02 ,  A61P9/00 ,  A61P13/00 ,  A61P25/00 ,  A61P25/06 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/32 ,  A61P43/00 ,  C07D231/56

    CPC classification number: C07D231/56

    Abstract: A chemical compound of formula (I) wherein R1 to R3 are independently selected from hydrogen and alkyl; R4 to R7 are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, amino, monoalkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, arylthio, arylsulfoxyl, arylsulfonyl, alkylsulfoxyl, alkylsulfonyl, nitro, cyano, carboxaldehyde, alkylcarbonyl, arylcarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkoxycarbonylamino, aminocarbonyloxy, monoalkylaminocarbonyloxy, dialkylaminocarbonyloxy, monoalkylaminocarbonylamino and dialkylaminocarbonylamino; and R8 is selected from alkyl and alkoxy, and pharmaceutically acceptable salts and prodrugs thereof, and the use thereof in therapy, particularly for the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus, and sleep apnea, and particularly for the treatment of obesity.

    Abstract translation: 式（I）的化合物，其中R 1至R 3独立地选自氢和烷基; R4至R7独立地选自氢，卤素，羟基，烷基，芳基，氨基，单烷基氨基，二烷基氨基，烷氧基，芳氧基，烷硫基，芳硫基，芳基亚砜基，芳基磺酰基，烷基亚砜基，烷基磺酰基，硝基，氰基，甲醛，烷基羰基，芳基羰基，氨基羰基 单烷基氨基羰基，二烷基氨基羰基，烷氧基羰基氨基，氨基羰基氧基，单烷基氨基羰基氧基，二烷基氨基羰基氧基，单烷基氨基羰基氨基和二烷基氨基羰基氨基; 并且R 8选自烷基和烷氧基及其药学上可接受的盐和前药，及其在治疗中的用途，特别是用于治疗中枢神经系统疾病的用途; 损害中枢神经系统; 心血管疾病; 胃肠道疾病; 尿崩症和睡眠呼吸暂停，特别是用于治疗肥胖症。

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