发明名称 PHENYL HETEROCYCLES AS CYCLOOXYGENASE-2 INHIBITORS
摘要 Compounds useful in the treatment of cyclooxygenase-2- mediated diseases are provided of formula (I): <IMG> or a pharmaceutically acceptable salt thereof wherein: X-Y-Z- is selected from the group consisting of: (a) -CR5(R5')-O-C(O)- and (b) -C(O)-O-CR5'(R5')-' R1 is selected from the group consisting of (a) S(O)2CH3, (b) S(O)2NH2, (c) S(O)2NHC(O)CF3, (d) S(O)(NH)CH3, (e) S(O)(NH)NH2, (f) S(O)(NH)NHC(O)CF3, (g) P(O)(CH3)OH, and (h) P(O)(CH3)NH2, R2 is selected from the group consisting of (a) C1-6 alkyl, (b) C3, C4, C5, C6 and C7, cycloalkyl, (c) unsubstituted, mono-, di- or tri-substituted phenyl wherein the substituent is selected from the group consisting of (1) halo, (2) C1-6 alkoxy, (3) C1-6 alkylthio, (4) CN, (5) CF3, (6) C1-6 alkyl, (7) N3, (8) -CO2H, (9) -CO2C1-4 alkyl, (10) -C(R5)(R6)-OH, (11) -C(R5)(R6)-O-C1-4 alkyl, and (12) -C1-6 alkyl-CO2-R5; (d) unsubstituted, mono-, di- or tri-substituted heteroaryl wherein the heteroaryl is a mono-cyclic aromatic ring of 5 atoms, said ring having one hetero atom which is S, o or N, and optionally 1, 2 or 3 additionally N atoms; or the heteroaryl is a monocyclic ring of 6 atoms, said ring having one hetero atom which is N, and optionally 1,2 3 or 4 additional N atoms; and the substituents are selected from the group consisting of (1) halo, including fluoro, chloro, bromo and iodo, (2) C1-6 alkyl, (3) C1-6 alkoxy, (4) C1-6 alkylthio, (5) CN, (6) CF3, (7) N3, (8) -C (R5) (R6) -OH, and (9) -C (R5) (R6) -O-C1-4 alkyl; R5 and R6 are independently selected from: a) hydrogen, b) C1-6alkyl, or c) R5 and R6 together with the carbon to which they are attached form a monoclyclic ring of 3, 4, 5, 6 or 7 atoms; and each R5' is the same and is C1-6alkyl.
申请公布号 CA2176973(C) 申请公布日期 2000.08.22
申请号 CA19942176973 申请日期 1994.06.09
申请人 MERCK FROSST CANADA INC. 发明人 PRASIT, PETPIBOON;LEBLANC, YVES;WANG, ZHAOYIN;LEGER, SERGE;DUCHARME, YVES;GAUTHIER, JACQUES Y.;THERIEN, MICHEL
分类号 C07D333/06;A61K31/00;A61K31/10;A61K31/12;A61K31/122;A61K31/18;A61K31/19;A61K31/255;A61K31/34;A61K31/341;A61K31/35;A61K31/351;A61K31/365;A61K31/38;A61K31/381;A61K31/395;A61K31/40;A61K31/4015;A61K31/425;A61K31/426;A61K31/66;A61P1/00;A61P1/02;A61P1/04;A61P7/04;A61P11/06;A61P15/00;A61P17/02;A61P19/00;A61P19/02;A61P21/00;A61P25/28;A61P29/00;A61P31/12;A61P31/16;A61P35/00;A61P43/00;C07C;C07C13/08;C07C13/10;C07C305/18;C07C307/02;C07C311/15;C07C311/16;C07C311/29;C07C311/37;C07C311/46;C07C311/49;C07C311/51;C07C317/10;C07C317/24;C07C323/29;C07D207/26;C07D207/333;C07D207/38;C07D207/444;C07D207/448;C07D275/02;C07D277/02;C07D277/22;C07D277/24;C07D277/26;C07D307/33;C07D307/38;C07D307/58;C07D309/32;C07D333/04;C07D333/12;C07D333/16;C07D333/18;C07D333/24;C07D333/38;C07D333/40;C07D405/04;C07D407/04;C07D409/04;C07D413/04;C07D417/04;C07D503/04;C07F9/40;C07F9/547;C07F9/572;C07F9/6506;C07F9/653;C07F9/6539;C07F9/655;(IPC1-7):C07D307/58 主分类号 C07D333/06
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