发明名称 Prokinetic oxadiazoles
摘要 PCT No. PCT/EP96/00784 Sec. 371 Date Aug. 15, 1997 Sec. 102(e) Date Aug. 15, 1997 PCT Filed Feb. 21, 1996 PCT Pub. No. WO96/26937 PCT Pub. Date Sep. 6, 1996The present invention concerns novel oxadiazole derivatives of formula (I) <IMAGE> (I) the N-oxide forms, the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R1 is hydrogen or halo; R2 is C1-6alkyl, C2-6alkenyl or C2-6alkynyl; R3 is hydrogen; or R2 and R3 taken together may form a C2-3alkanediyl radical wherein one or two hydrogen atoms may be replaced by C1-4alkyl; R4 is hydrogen or C1-6alkyloxy; X is a bivalent radical of the formula <IMAGE> (a-1) <IMAGE> (a-2) L is a radical of formula -Alk-R5 or -Alk-O-R6, Alk is C1-12alkanediyl; R5 is hydrogen, cyano, C1-6alkylcarbonyl, C1-6alkylsulfinyl, C1-6alkylsulfonyl, aryl, arylcarbonyl, tetrahydrofuran, dioxolane, dioxolane substituted with C1-6 alkyl, dioxane, dioxane substituted with C1-6alkyl; R6 is hydrogen, aryl, C1-6alkyl, hydroxyC1-6alkyl, C1-6alkylcarbonyl; aryl is defined as phenyl or phenyl substituted with up to three substituents selected from halo, C1-6alkyl or C1-6alkyloxy. It further relates to pharmaceutical compositions comprising them, processes for preparing said compounds and compositions, and the use thereof as a medicine, in particular in the conditions involving a decreased motility of the colon.
申请公布号 AU4718896(A) 申请公布日期 1996.09.18
申请号 AU19960047188 申请日期 1996.02.21
申请人 JANSSEN PHARMACEUTICA N.V. 发明人 JEAN-PAUL RENE MARIE ANDRE BOSMANS
分类号 A61K31/445;A61P1/00;C07D413/04;C07D413/14 主分类号 A61K31/445
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