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2. 发明授权

US06211209B1 Method of inhibiting connective tissue degradation 失效
标题翻译：抑制结缔组织降解的方法
公开(公告)号：US06211209B1
公开(公告)日：2001-04-03
申请号：US09130215
申请日：1998-08-06
申请人： Vijaykumar Baragi , Diane Harris Boschelli , David Thomas Connor , Richard Raymond Renkiewicz , Howard Glenn Welgus
发明人： Vijaykumar Baragi , Diane Harris Boschelli , David Thomas Connor , Richard Raymond Renkiewicz , Howard Glenn Welgus
IPC分类号： A61K3141
CPC分类号： A61K31/433 , A61K31/341 , A61K31/4196 , A61K31/4245 , A61K31/426
摘要： The present invention provides a method of inhibiting connective tissue degradation that comprises administering to a patient having a condition in which connective tissue is degraded a therapeutically effective amount of a compound having the formula where R1, R2, R3, and R4 are independently hydrogen, hydroxy, halo, amino, nitro, C1-C6 alkyl, C3-C6 cycloalkyl, C1-C6 alkoxy, CF3, CN, S(O)n—, R6 and R7 are independently hydrogen, C1-C6 alkyl, or acyl; n is 0 to 2; R8 is hydrogen or C1-C6 alkyl; W is S or O; Z is C1-C6 alkyl, C1-C6 alkoxy, or NR9R10; R9 and R10 are independently hydrogen or C1-C6 alkyl; and R5 is where Y is hydroxy, thiol, amino, or NHCN; X is sulfur or oxygen; and Q is sulfur, oxygen, NH, or NCN, and the pharmaceutically acceptable salts and prodrugs thereof. Also provided is a method of inhibiting the production of matrix metalloproteinases comprising administering to a patient having a condition associated with matrix metalloproteinase-mediated tissue degradation a therapeutically effective amount of a compound having the formula where R1, R2, R3, and R4 are independently hydrogen, hydroxy, halo, amino, nitro, C1-C6 alkyl, C3-C6 cycloalkyl, C1-C6 alkoxy, CF3, CN, S(O)n—, R6 and R7 are independently hydrogen, C1-C6 alkyl or acyl; n is 0 to 2; R8 is hydrogen or C1-C6 alkyl; W is S or O; Z is C1-C6 alkyl, C1-C6 alkoxy, or NR9R10; R9 and R10 are independently hydrogen or C1-C6 alkyl; and R5 is where Y is hydroxy, thiol, amino, or NHCN; X is sulfur or oxygen; and Q is sulfur, oxygen, NH, or NCN, and the pharmaceutically acceptable salts and prodrugs thereof.
摘要翻译：本发明提供了一种抑制结缔组织降解的方法，其包括对患有结缔组织降解的病症的患者施用治疗有效量的具有下式的化合物：R 1，R 2，R 3和R 4独立地为氢，羟基，卤素，氨基，硝基，C 1 -C 6烷基，C 3 -C 6环烷基，C 1 -C 6烷氧基，CF 3，CN，S（O）n - ，R 6和R 7独立地是氢，C 1 -C 6烷基或酰基; n是0 R 2是氢或C 1 -C 6烷基; W是S或O; Z是C 1 -C 6烷基，C 1 -C 6烷氧基或NR 9 R 10; R 9和R 10独立地是氢或C 1 -C 6烷基; 和R 5是其中Y是羟基，硫醇，氨基或NHCN; X是硫或氧; 和Q是硫，氧，NH或NCN，及其药学上可接受的盐和前药。还提供了抑制基质金属蛋白酶产生的方法，包括对具有与基质金属蛋白酶介导的组织降解有关的病症的患者施用治疗有效量的具有下式的化合物：R1，R2，R3和R4独立地是氢，羟基，卤素，氨基，硝基，C1-C6烷基，C3-C6环烷基，C1-C6烷氧基，CF3，CN，S（O）n，R6和R7独立地是氢，C1-C6烷基或酰基; n是 0至2; R 8是氢或C 1 -C 6烷基; W是S或O; Z是C 1 -C 6烷基，C 1 -C 6烷氧基或NR 9 R 10; R 9和R 10独立地是氢或C 1 -C 6烷基; 和R 5是其中Y是羟基，硫醇，氨基或NHCN; X是硫或氧; 和Q是硫，氧，NH或NCN，及其药学上可接受的盐和前药。

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