会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 10. 发明授权
    • Oxime derivatives of indole and indene compounds as inhibitors of
prostaglandin biosynthesis
    • 吲哚和茚化合物的肟衍生物作为前列腺素生物合成的抑制剂
    • US5750558A
    • 1998-05-12
    • US660048
    • 1996-06-06
    • Clint D. W. BrooksTeodozyj KolasaWendy LeeAndrew O. Stewart
    • Clint D. W. BrooksTeodozyj KolasaWendy LeeAndrew O. Stewart
    • C07C317/32C07D209/14C07D257/04C07D401/06C07D401/12C07D403/12C07D405/12C07D417/12C07D417/14A61K31/40
    • C07D257/04C07C317/32C07D209/14C07D401/06C07D401/12C07D403/12C07D405/12C07D417/12C07D417/14C07C2102/08
    • Described herein are compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein L is selected from the group consisting of ##STR2## R.sup.2 is selected from (a) ##STR3## R.sup.3 is selected from optionally substituted phenyl, and optionally substituted pyridyl; Y is selected from halogen, alkyl, haloalkyl, alkoxy, pyridylmethoxy, thiazolylmethoxy, benzothiazolylmethoxy, quinolylmethoxy, and optionally substituted quinolylmethoxy; W is selected from hydrogen, alkyl, hydroxyalkyl, and hydroxy; A is absent or is selected from optionally substituted alkylene optionally substituted cycloalkylene, 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, and ##STR4## and X is absent or is alkylene; Z is selected from (a) hydrogen, (b) COM wherein M is selected from (b-1) a pharmaceutically acceptable metabolically cleavable group, (b-2)--OR.sup.10,(b-3)--O(CH.sub.2).sub.w --CH(OR.sup.12)--CH.sub.2 OR.sup.13, and (b-4)--NR.sup.15 R.sup.16 (c)--OR.sup.17, (d) tetrazolyl, (e)--CH(OR.sup.17)--CH.sub.2 OR.sup.18,(f)--CH(OR.sup.17)--CH.sub.2 --CH.sub.2 OR.sup.18, (g)--CH(OR.sup.17)--CH(OR.sup.18)--CH.sub.2 OR.sup.19, and (h).dbd.N--OR.sup.17 ; and R.sup.1 and R.sup.4 selected from (a) hydrogen, (b) alkyl, and (c) optionally substituted phenyl, are prostaglandin biosynthesis inhibitors and are useful in the treatment of inflammatory disease states. Also disclosed are prostaglandin inhibiting compositions, and a method of inhibiting prostaglandin biosynthesis in a mammal.
    • 本文描述的是具有式“IMAGE”的化合物或其药学上可接受的盐,其中L选自由下列组成的组:R 2选自(a)图像(b)图像(c) (d)R 3选自任选取代的苯基和任选取代的吡啶基; Y选自卤素,烷基,卤代烷基,烷氧基,吡啶基甲氧基,噻唑基甲氧基,苯并噻唑基甲氧基,喹啉基甲氧基和任选取代的喹啉基甲氧基; W选自氢,烷基,羟基烷基和羟基; A不存在或选自任选取代的亚烷基任选取代的亚环烷基,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的杂原子替代,并且X不存在 或者是亚烷基; Z选自(a)氢,(b)COM,其中M选自(b-1)可药用代谢裂解基团,(b-2)-OR10,(b-3)-O(CH2)w- CH(OR 12)-CH 2 OR 13和(b-4)-NR 15 R 16(c)-OR 17,(d)四唑基,(e)-CH(OR 17)-CH 2 OR 18,(f)-CH(OR 17) (g)-CH(OR 17)-CH(OR 18)-CH 2 OR 19,和(h)= N-OR 17; 并且选自(a)氢,(b)烷基和(c)任选取代的苯基的R 1和R 4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和抑制哺乳动物中前列腺素生物合成的方法。