发明名称 ISOQUINOLINONE DERIVATIVES AS NK3 ANTAGONISTS
摘要 The invention relates to compounds of formula [I], wherein A represents CH; each Rrepresents hydrogen, C-alkyl, X represents hydrogen, C-alkyl, optionally substituted with halogen or -CRR-X', wherein X' represents a monocyclic saturated moiety having 5-6 ring atoms one of which is N and wherein one additional ring atom may be a hetero atom selected from N, which monocyclic ring may be substituted with one or more substituents W, wherein W is selected from C-alkyl or (=O); Rand Reach represents hydrogen; Q represents a bond, -CH-, -NH-, or -O-; Y represents C-alkyl, C-alkenyl or C-alkynyl, wherein said alkyl, alkenyl or alkynyl may be substituted with one or more substituents P, wherein P is selected from halogen, hydroxy group, C-alkoxy group, cyano group, -S-C-alkyl, and a monocyclic saturated moiety having 5-6 ring atoms, one ring atom of which may be N and the rest are C; or Y may represent a monocyclic saturated moiety having 4-6 ring atoms, wherein one of said ring atoms may be selected from N and O, the rest being C, and which monocyclic saturated moiety may be substituted with one or more substituents Z, wherein Z is selected from C-alkyl, (=O), -C(O)-C-alkyl; each of R-Rand R-Rindependently represents hydrogen, halogen, hydroxy group; provided that said compound is different from 2-methyl-1-oxo-1,2-dihydroisoquinoline-4-carboxylic acid (1-phenylethyl)amide; and pharmaceutically acceptable salts thereof. The invention also relates to pharmaceutical compositions having antagonistic activity to NK3 receptors, comprising said compounds and to the use of said compounds in the manufacture of a medicament for the treatment of a psychosis disease.
申请公布号 EA021581(B1) 申请公布日期 2015.07.30
申请号 EA20110070447 申请日期 2009.09.11
申请人 H. LUNDBECK A/S 发明人 KHANZHIN NIKOLAY;JUHL KARSTEN;NIELSEN SOEREN, MOELLER;SIMONSEN KLAUS, BAEK
分类号 C07D217/26;A61K31/472;A61P25/18;C07D401/06;C07D403/06;C07D407/04 主分类号 C07D217/26
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