发明名称 INDOLINE DERIVATIVES AS 5HT2C RECEPTOR ANTAGONISTS
摘要 A compound of formula (I) or a salt thereof, wherein: R<1> is hydrogen or C1-6alkyl; R<2>, R<3> and R<4> groups are independently hydrogen, halogen or C1-6alkyl optionally substituted by one or more fluorine atoms. R<5> and R<6> groups are independently hydrogen or C1-6alkyl; X and Y are independently CH or nitrogen, provided that X is nitrogen when Y is nitrogen and both R<5> and R<6> are hydrogen. The compounds exhibit enhanced 5HT2C receptor antagonist activity profile. 5HT2C receptor antagonists are believed to be of potential use in the treatment of CNS disorders such as anxiety, depression, epilepsy, obsessive compulsive disorders, migraine, Alzheimer's disease, sleep disorders, feeding disorders such as anorexia and bulimia, panic attacks, withdrawal from drug abuse such as cocaine, ethanol, nicotine and benzodiazepines, schizophrenia, and also disorders associated with spinal trauma and/or head injury such as hydrocephalus. Compounds of the invention are also expected to be of use in the treatment of glaucoma, certain GI (gastrointestinal) disorders such as IBS (Irritable Bowel Syndrome) as well as microvascular diseases such as macular oedema and retinopathy.
申请公布号 WO9852943(A1) 申请公布日期 1998.11.26
申请号 WO1998EP02992 申请日期 1998.05.13
申请人 SMITHKLINE BEECHAM PLC;BROMIDGE, STEVEN, MARK 发明人 BROMIDGE, STEVEN, MARK
分类号 C07D213/72;A61K31/4439;A61K31/497;A61P25/00;A61P25/06;A61P25/08;A61P25/18;A61P25/20;A61P25/22;A61P25/24;A61P25/28;A61P25/30;A61P27/02;A61P43/00;C07D401/12;C07D401/14;(IPC1-7):C07D401/12;A61K31/44 主分类号 C07D213/72
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