发明名称 1-TRIFLOUROMETHYL-4-HYDROXY-7-PIPERIDINYLAMINOMETHYLCHROMAN AS ANTAGONISTS OF SUBSTANCE P
摘要 1. A compound of the formula(I): and pharmaceutically acceptable salts thereof, wherein R<1> is C1-C6 alkyl; R<2> is hydrogen, C1-C6 alkyl, halo C1-C6 alkyl or phenyl; R<3> is hydrogen or halo; and R<4> and R<5> are independently hydrogen, C1-C6 alkyl or halo C1-C6 alkyl. 2. A compound according to claim 1, wherein R<1> is C1-C6 alkyl; R<2> is hydrogen, C1-C3 alkyl, halo C1-C3 alkyl or phenyl; R<3> is hydrogen or fluorine; and R<4> and R<5> are independently hydrogen, C1-C3 alkyl or haloC1-C3 alkyl. 3. A compound according to claim 2, wherein R<1> is methyl; R<2> is hydrogen, methyl, trifluoromethyl or phenyl; R<3> is hydrogen; and R<4> and R<5> are independently hydrogen. 4. A compound according to claim 1 which is (2S,3S)-3-(6-methoxy-4-hydroxy-1-methyl-1-trifluoromethylisochroman-7-yl) methylamino-2-phenylpiperidine or a pharmaceutically acceptable salt thereof. 5. A pharmaceutical composition for treating a disorder or condition, for which antagonist activity toward substance P is needed, in a mammal, which comprises an amount of the compound of claim 1, or a pharmaceutically acceptable salt thereof, that is effective in treating such disorder or condition, and a pharmaceutically acceptable carrier. 6. A method for treating a disorder or condition for which antagonist activity toward substance P is needed, in a mammal, which comprises an amount of the compound of claim 1, or a pharmaceutically acceptable salt thereof, that is effective in treating such disorder or condition, and a pharmaceutically acceptable carrier.
申请公布号 EA004233(B1) 申请公布日期 2004.02.26
申请号 EA20010001109 申请日期 2000.04.20
申请人 PFIZER PRODUCTS INC. 发明人 OBACH, RONALD, SCOTT;SCULLY, DOUGLAS, ALAN
分类号 A61K;A61K31/33;A61K31/435;A61K31/453;A61P;A61P1/00;A61P1/04;A61P1/08;A61P1/14;A61P1/16;A61P3/02;A61P9/10;A61P11/02;A61P11/06;A61P13/00;A61P13/02;A61P13/10;A61P15/08;A61P15/10;A61P17/06;A61P17/16;A61P19/02;A61P25/02;A61P25/04;A61P25/06;A61P25/14;A61P25/16;A61P25/18;A61P25/24;A61P25/28;A61P25/30;A61P27/02;A61P29/00;A61P31/04;A61P37/02;A61P37/08;A61P43/00;C07D;C07D211/00;C07D311/00;C07D405/12;(IPC1-7):C07D405/12 主分类号 A61K
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