发明名称 Fused imidazole derivatives for improving oral bioavailability of pharmaceuticalagents
摘要 This invention concerns the use of compounds of formulathe N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein the dotted line is an optional bond; n is 1 or 2; R1 is hydrogen; halo; formyl; C1-4alkyl optionally substituted with hydroxy, C1-4alkyloxy, C1-4alkylcarbonyloxy, imidazolyl, thiazolyl or oxazolyl; or a radical of formula -X-COOR5, -X-CONR6R7 or -X-COR10 wherein -X-is a direct bond, C1-4alkanediyl or C2-6alkenediyl; R5 is hydrogen, C1-12alkyl, Ar, Het, C1-6alkyl substituted with C1-4alkyloxy, aryl or heteroaryl; R6 and R7 each independently are hydrogen or C1-4alkyl; R2 is hydrogen, halo, C1-4alkyl, hydroxyC1-4alkyl, C1-4alkyloxycarbonyl, carboxyl, formyl or phenyl; R3 is hydrogen, C1-4alkyl or C1-4alkyloxy; R4 is hydrogen, halo, C1-4alkyl, C1-4alkyloxy or haloC1-4alkyl; Z is -CH2-, -CH2-CH2-, -CH=CH-, -CHOH-CH2-, -O-CH2-, 13 C(=O)-CH2-or -C(=NOH)-CH2-; -A-B-is a bivalent radical; A1 is a direct bond, optionally substituted C1-6alkanediyl, C1-6alkanediyl-oxy-C1-6alkanediyl, carbonyl, C1-6alkanediylcarbonyl, optionally substituted C1-6alkanediyloxy; A2 is a direct bond or C1-6alkanediyl; and Q is aryl; for the manufacture of a medicine for improving the bioavailability of a second pharmaceutical agent which is co-administered orally to a warm-blooded animal.
申请公布号 AU1146099(A) 申请公布日期 1999.04.05
申请号 AU19990011460 申请日期 1998.09.10
申请人 JANSSEN PHARMACEUTICA N.V. 发明人 HENRICUS JOHANNES MATHEUS SNOECK
分类号 C07D487/04;A61K31/337;A61K31/439;A61K31/4738;A61K31/513;A61K31/55;A61K31/553;A61K31/675;A61K31/704;A61K31/7048;A61K33/24;A61K45/06;A61P35/00;A61P43/00;C07D487/14;C07D495/14;C07D498/04 主分类号 C07D487/04
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