发明名称 QUINOLINE DERIVATIVE AS TACHYKININ NK3 RECEPTOR ANTAGONIST
摘要 PROBLEM TO BE SOLVED: To obtain the subject new nonpeptidic compound stable from a metabolic standpoint and capable of manifesting latent therapeutic effectiveness in treatment of pneumonopathies, dermatopathies and prurigos, nervous inflammations and diseases in the central nervous system(CNS). SOLUTION: This compound is represented by formula I (Ar is phenyl, naphthyl, a 5-7C cycloalkadienyl or the like; R is a 1-8C alkyl or the like; R1 and R2 are each H, a 1-6C alkyl or the like; R3 and R4 are each H, a 1-6C alkyl or the like; R5 is a 1-6C alkyl, a 3-7C cycloalkyl or the like; X is O, S or N-C≡N) or its solvent hydrate or a salt thereof, e.g. (R,S)-N-(α- methylbenzyl)-2-phenylquinoline-4-carboxyamide. The compound represented by formula I is obtained by reacting a compound represented by formula II (R', R'1, R'2 and Ar' are each same as R, R1, R2, Ar or the like) with a compound represented by formula III (R'3, R'4, R'5 and X' are each same as R3, R4, R5, X or the like) or its active derivative, providing a compound represented by formula IV and then converting the resultant compound represented by formula IV into a desired compound.
申请公布号 JP2000026314(A) 申请公布日期 2000.01.25
申请号 JP19990172597 申请日期 1999.06.18
申请人 SMITHKLINE BEECHAM FARMACEUT SPA 发明人 FARINA CARLO;GIARDINA GIUSEPPE ARNALDO MARIA;GRUGNI MARIO;RAVEGLIA LUCA FRANCESCO
分类号 A61K31/00;A61K31/47;A61K31/4709;A61K31/473;A61K45/00;A61P1/00;A61P1/14;A61P1/16;A61P3/00;A61P3/04;A61P11/00;A61P11/02;A61P11/06;A61P13/00;A61P13/02;A61P13/12;A61P17/00;A61P17/06;A61P25/00;A61P25/04;A61P25/08;A61P25/14;A61P25/16;A61P25/18;A61P25/20;A61P25/22;A61P25/24;A61P25/28;A61P27/00;A61P27/02;A61P27/16;A61P29/00;A61P37/08;A61P43/00;C07D215/52;C07D221/18;C07D401/04;C07D401/12;C07D405/04;C07D405/12;C07D409/04;C07D409/12;C07D417/04;(IPC1-7):A61K45/00 主分类号 A61K31/00
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