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    • 42. 发明授权
    • Oxime derivatives of fenamates as inhibitors of prostaglandin
biosynthesis
    • 芥酸肟衍生物作为前列腺素生物合成的抑制剂
    • US5840758A
    • 1998-11-24
    • US659474
    • 1996-06-06
    • Clint D. W. BrooksTeodozyj KolasaWendy LeeAndrew O. Stewart
    • Clint D. W. BrooksTeodozyj KolasaWendy LeeAndrew O. Stewart
    • C07C251/16C07C251/60C07C259/06C07D257/04A61K31/41A61K31/165A61K31/19A61K31/275
    • C07D257/04C07C251/16C07C251/60C07C259/06Y10S514/824Y10S514/825Y10S514/863Y10S514/886Y10S514/887Y10S514/916
    • Compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein Y is selected from halogen, alkyl, and haloalkyl; n is 0, 1, 2, or 3; A is selected from (a) optionally substituted alkylene, (b) optionally substituted cycloalkylene, (c) optionally substituted cycloalkylene wherein one or two of the carbon atoms is replaced with one or two heteroatoms independently selected from O, S, and N, (d) optionally substituted alkenylene and (e) ##STR2## X is absent or is alkylene; Z is selected from (a) hydrogen, (b) COM wherein M is selected from --OR.sup.4, --NR.sup.6 R.sup.7, and a pharmaceutically acceptable metabolically cleavable group, (c) --OR.sup.2, (d) tetrazolyl, (e) --CH(OR.sup.2)--CH.sub.2 OR.sup.8, (f) --CH(OR.sup.2)--CH.sub.2 --CH.sub.2 OR.sup.8, (g) --CH(OR.sup.2)--CH(OR.sup.8)--CH.sub.2 OR.sup.9, and (h).dbd.N--OR.sup.2 ; and R.sup.1 is selected from hydrogen, alkyl, and optionally substituted phenyl, are prostaglandin biosynthesis inhibitors and are useful in the treatment of inflammatory disease states. Also disclosed are prostaglandin inhibiting compositions, a method of inhibiting prostaglandin biosynthesis in a mammal.
    • 具有式“IMAGE”的化合物或其药学上可接受的盐,其中Y选自卤素,烷基和卤代烷基; n为0,1,2或3; A选自(a)任选取代的亚烷基,(b)任选取代的亚环烷基,(c)任选取代的亚环烷基,其中一个或两个碳原子被一个或两个独立地选自O,S和N的杂原子置换,( d)任选取代的亚烯基和(e)X不存在或是亚烷基; Z选自(a)氢,(b)COM,其中M选自-OR4,-NR6R7和药学上可接受的代谢可裂解基团,(c)-OR2,(d)四唑基,(e)-CH(OR2) )-CH 2 OR 8,(f)-CH(OR 2)-CH 2 -CH 2 OR 8,(g)-CH(OR 2)-CH(OR 8)-CH 2 OR 9和(h)= N-OR 2; 并且R 1选自氢,烷基和任选取代的苯基,是前列腺素生物合成抑制剂,并且可用于治疗炎性疾病状态。 还公开了前列腺素抑制组合物,在哺乳动物中抑制前列腺素生物合成的方法。