发明名称 PYRROLIDINE DERIVATIVES AS NK-3 RECEPTOR ANTAGONISTS
摘要 FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to compounds of formulaand its pharmaceutically active salts; Rrepresents hydrogen, halogen; n represents 1 or 2, if n represents 2, then Rcan be different; Rrepresents C-alkyl or C-cycloalkyl; Rrepresents the groupwherein X represents CH; Rrepresents hydrogen, -C(O)-lower alkyl, -C(O)O-lower alkyl, S(O)-lower alkyl, -C(O)-CH-CN, or represents -C(O)-C-cycloalkyl, wherein the cycloalkyl groups can be optionally substituted by a lower alkyl, -CH-O-lower alkyl, lower alkoxy, CF, halogen or cyano, or represents -C(O)-(4-6-merous heterocycloalkyl containing 1 heteroatom specified in O, N), or represents -C(O)-(6-merous heteroaryl containing 1-2 heteroatoms N), or represents 6-merous heteroaryl containing 1-2 heteroatoms N, or represents -C(O)-phenyl, wherein heterocycloalkyl, heteroaryl or phenyl groups are optionally substituted by halogen, lower alkyl, =O, lower alkyl substituted by a halogen, lower alkyl substituted by hydroxy, -C(O)-CH-N(di-lower alkyl), C(O)NH, -O-C(O)-lower alkyl, C(O)-lower alkyl, S(O)-lower alkyl or cyano; Rrepresents phenyl substituted by a halogen. The invention also refers to the compound [(3S,4R)-4-(4-chloro-3-fluoro-phenyl)-1-(1-isopropyl-6-oxo-piperidin-3-carbonyl)-pyrrolidin-3-yl]-ethyl-carbamic acid 4-fluoro-phenyl ester; to a medicinal product possessing properties of an NK-3 receptor antagonist, containing one or more compounds of the inventions, and to the use of the compounds for preparing the medicinal product.EFFECT: there are prepared new compounds, which possess the properties of the NK-3 receptor antagonist.8 cl, 1 tbl, 126 ex
申请公布号 RU2561271(C2) 申请公布日期 2015.08.27
申请号 RU20120129361 申请日期 2010.12.14
申请人 F. KHOFFMANN-LJA ROSH AG 发明人 KNUST KHENNER;KOBLE ANDREAS;NETTEKOFEN MATTIAS;RATNI KHASAN;RIMER KLAUS;VIFIAN VAL'TER
分类号 C07D401/06;A61K31/44;A61P25/28;C07D401/14;C07D403/14;C07D405/14 主分类号 C07D401/06
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