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1. 发明授权

US07368471B2 Substituted indole acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1) 失效
标题翻译：取代的吲哚酸衍生物作为纤溶酶原激活物抑制剂-1（PAI-1）的抑制剂
公开(公告)号：US07368471B2
公开(公告)日：2008-05-06
申请号：US11391893
申请日：2006-03-29
申请人： Hassan Mahmound Elokdah , Geraldine Ruth McFarlane , David Zenan Li , Lee Dalton Jennings , David LeRoy Crandall
发明人： Hassan Mahmound Elokdah , Geraldine Ruth McFarlane , David Zenan Li , Lee Dalton Jennings , David LeRoy Crandall
IPC分类号： A61K31/404 , C07D209/42
CPC分类号： C07D209/12
摘要： This invention provides compounds of the formula: wherein: X is a chemical bond, —CH2— or —C(O)—; R1 is alkyl, cycloalkyl, —CH2-cycloalkyl, pyridinyl, —CH2-pyridinyl, phenyl or benzyl; R2 is H, alkyl, cycloalkyl, —CH2-cycloalkyl, or perfluoroalkyl; R3 is H, halo, alkyl, perfluoroalkyl, alkoxy, cycloalkyl, —CH2-cycloalkyl, —NH2, or —NO2; R4 is optionally substituted phenyl, benzyl, benzyloxy, pyridinyl, or —CH2-pyridinyl, or the salt or ester forms thereof, as well as methods for using the compounds as inhibitors of plasminogen activator inhibitor-1 (PAI-1) and as therapeutic compositions for treating conditions resulting from fibrinolytic disorders such as deep vein thrombosis and coronary heart disease, and pulmonary fibrosis.
摘要翻译：本发明提供下式的化合物：其中：X为化学键，-CH 2 - 或-C（O） - ; R 1是烷基，环烷基，-CH 2 - 环烷基，吡啶基，-CH 2 - 吡啶基，苯基或苄基; R 2是H，烷基，环烷基，-CH 2 - 环烷基或全氟烷基; R 3是H，卤素，烷基，全氟烷基，烷氧基，环烷基，-CH 2 2-环烷基，-NH 2或-NO 3， SUB> 2 R 4是任选取代的苯基，苄基，苄氧基，吡啶基或-CH 2 - 吡啶基，或其盐或酯形式，以及使用该化合物的方法作为纤维蛋白溶酶原激活物抑制剂-1（PAI-1）的抑制剂以及用于治疗由纤维蛋白溶解性疾病如深静脉血栓形成和冠心病引起的病症和肺纤维化的治疗组合物。

2. 发明申请

US20080214647A1 SUBSTITUTED INDOLE ACID DERIVATIVES AS INHIBITORS OF PLASMINOGEN ACTIVATOR INHIBITOR-1 (PAI-1) 审中-公开
标题翻译：作为PLASMINOGEN ACTIVATOR INHIBITOR-1（PAI-1）的抑制剂的取代的吲哚酸衍生物
公开(公告)号：US20080214647A1
公开(公告)日：2008-09-04
申请号：US12098916
申请日：2008-04-07
申请人： Hassan Mahmoud Elokdah , Geraldine Ruth McFarlane , David Zenan Li , Lee D. Jennings , David LeRoy Crandall
发明人： Hassan Mahmoud Elokdah , Geraldine Ruth McFarlane , David Zenan Li , Lee D. Jennings , David LeRoy Crandall
IPC分类号： A61K31/403 , A61P7/04
CPC分类号： C07D209/12
摘要： This invention provides compounds of the formula: wherein: X is a chemical bond, —CH2— or —C(O)—; R1 is alkyl, cycloalkyl, —CH2— cycloalkyl, pyridinyl, —CH2-pyridinyl, phenyl or benzyl; R2 is H, alkyl, cycloalkyl, —CH2-cycloalkyl, or perfluoroalkyl; R3 is H, halo, alkyl, perfluoroalkyl, alkoxy, cycloalkyl, —CH2-cycloalkyl, —NH2, or —NO2; R4 is optionally substituted phenyl, benzyl, benzyloxy, pyridinyl, or —CH2-pyridinyl, or the salt or ester forms thereof, as well as methods for using the compounds as inhibitors of plasminogen activator inhibitor-1 (PAI-1) and as therapeutic compositions for treating conditions resulting from fibrinolytic disorders such as deep vein thrombosis and coronary heart disease, and pulmonary fibrosis.
摘要翻译：本发明提供下式的化合物：其中：X为化学键，-CH 2 - 或-C（O） - ; R 1是烷基，环烷基，-CH 2 - 环烷基，吡啶基，-CH 2 - 吡啶基，苯基或苄基; R 2是H，烷基，环烷基，-CH 2 - 环烷基或全氟烷基; R 3是H，卤素，烷基，全氟烷基，烷氧基，环烷基，-CH 2 2-环烷基，-NH 2或-NO 3， SUB> 2 R 4是任选取代的苯基，苄基，苄氧基，吡啶基或-CH 2 - 吡啶基，或其盐或酯形式，以及使用该化合物的方法作为纤维蛋白溶酶原激活物抑制剂-1（PAI-1）的抑制剂以及用于治疗由纤维蛋白溶解性疾病如深静脉血栓形成和冠心病引起的病症和肺纤维化的治疗组合物。

3. 发明申请

US20060167059A1 Substituted indole acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1) 失效
标题翻译：取代的吲哚酸衍生物作为纤溶酶原激活物抑制剂-1（PAI-1）的抑制剂
公开(公告)号：US20060167059A1
公开(公告)日：2006-07-27
申请号：US11391893
申请日：2006-03-29
申请人： Hassan Mahmoud Elokdah , Geraldine Ruth McFarlane , David Zenan Li , Lee Jennings , David LeRoy Crandall
发明人： Hassan Mahmoud Elokdah , Geraldine Ruth McFarlane , David Zenan Li , Lee Jennings , David LeRoy Crandall
IPC分类号： A61K31/4439 , A61K31/405 , C07D403/02 , C07D209/18
CPC分类号： C07D209/12
摘要： This invention provides compounds of the formula: wherein: X is a chemical bond, —CH2— or —C(O)—; R1 is alkyl, cycloalkyl, —CH2-cycloalkyl, pyridinyl, —CH2-pyridinyl, phenyl or benzyl; R2 is H, alkyl, cycloalkyl, —CH2-cycloalkyl, or perfluoroalkyl; R3 is H, halo, alkyl, perfluoroalkyl, alkoxy, cycloalkyl, —CH2-cycloalkyl, —NH2, or —NO2; R4 is optionally substituted phenyl, benzyl, benzyloxy, pyridinyl, or —CH2-pyridinyl, or the salt or ester forms thereof, as well as methods for using the compounds as inhibitors of plasminogen activator inhibitor-1 (PAI-1) and as therapeutic compositions for treating conditions resulting from fibrinolytic disorders such as deep vein thrombosis and coronary heart disease, and pulmonary fibrosis.
摘要翻译：本发明提供下式的化合物：其中：X为化学键，-CH 2 - 或-C（O） - ; R 1是烷基，环烷基，-CH 2 - 环烷基，吡啶基，-CH 2 - 吡啶基，苯基或苄基; R 2是H，烷基，环烷基，-CH 2 - 环烷基或全氟烷基; R 3是H，卤素，烷基，全氟烷基，烷氧基，环烷基，-CH 2 2-环烷基，-NH 2或-NO 3， SUB> 2 R 4是任选取代的苯基，苄基，苄氧基，吡啶基或-CH 2 - 吡啶基，或其盐或酯形式，以及使用该化合物的方法作为纤维蛋白溶酶原激活物抑制剂-1（PAI-1）的抑制剂以及用于治疗由纤维蛋白溶解性疾病如深静脉血栓形成和冠心病引起的病症和肺纤维化的治疗组合物。

4. 发明授权

US07074817B2 Substituted indole acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1) 失效
公开(公告)号：US07074817B2
公开(公告)日：2006-07-11
申请号：US10174159
申请日：2002-06-18
申请人： Hassan Mahmoud Elokdah , Geraldine Ruth McFarlane , David Zenan Li , Lee D. Jennings , David LeRoy Crandall
发明人： Hassan Mahmoud Elokdah , Geraldine Ruth McFarlane , David Zenan Li , Lee D. Jennings , David LeRoy Crandall
IPC分类号： A61K31/404 , C07D209/42
CPC分类号： C07D209/12
摘要： This invention provides compounds of the formula: wherein: X is a chemical bond, —CH2— or —C(O)—; R1 is alkyl, cycloalkyl, —CH2-cycloalkyl, pyridinyl, —CH2-pyridinyl, phenyl or benzyl; R2 is H, alkyl, cycloalkyl, —CH2-cycloalkyl, or perfluoroalkyl; R3 is H, halo, alkyl, perfluoroalkyl, alkoxy, cycloalkyl, —CH2-cycloalkyl, —NH2, or —NO2; R4 is optionally substituted phenyl, benzyl, benzyloxy, pyridinyl, or —CH2-pyridinyl, or the salt or ester forms thereof, as well as methods for using the compounds as inhibitors of plasminogen activator inhibitor-1 (PAI-1) and as therapeutic compositions for treating conditions resulting from fibrinolytic disorders such as deep vein thrombosis and coronary heart disease, and pulmonary fibrosis.

5. 发明授权

US06599925B2 Substituted naphthyl benzofuran derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1) 失效
标题翻译：取代的萘基苯并呋喃衍生物作为纤溶酶原激活物抑制剂-1（PAI-1）的抑制剂
公开(公告)号：US06599925B2
公开(公告)日：2003-07-29
申请号：US10174166
申请日：2002-06-18
申请人： Hassan Mahmoud Elokdah , Geraldine Ruth McFarlane , Scott Christian Mayer , David LeRoy Crandall
发明人： Hassan Mahmoud Elokdah , Geraldine Ruth McFarlane , Scott Christian Mayer , David LeRoy Crandall
IPC分类号： A61K3142
CPC分类号： C07D405/12 , C07D307/80
摘要： This invention provides compounds which act as inhibitors of plasminogen activator inhibitor-1 (PAI-1) of the formula: wherein: R, R1, R2, and R3 are H, alkyl, cycloalkyl, —CH2-(cycloalkyl), alkanoyl, halo, hydroxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, perfluoroalkyl, alkoxy, amino, —NH(alkyl), —N(alkyl)2, or perfluoroalkoxy; R4 is H, alkyl, perflouroalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, alkenyl, alkenyl-aryl, aryl, —CH2R5, —CH(OH)R5, —C(O)R5, —CH(SH)R5, or —C(S)R5; R5 is H, alkyl, perflouroalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, alkenyl, alkenyl-aryl; R6 is H, alkyl, cycloalkyl, —CH2-cycloalkyl, alkylaryl, aryl, substituted aryl, heteroaryl, or substituted heteroaryl; n is an integer of 0-6; A is COOH, or an acid mimic; or a pharmaceutically acceptable salt or ester form thereof, as well as pharmaceutical compositions and methods using these compounds to treat or prevent conditions resulting from fibrinolytic disorders such as deep vein thrombosis and coronary heart disease, and pulmonary fibrosis.
摘要翻译：本发明提供了作为下式的纤溶酶原激活物抑制剂-1（PAI-1）的抑制剂的化合物：其中：R，R 1，R 2和R 3是H，烷基，环烷基，-CH 2 - （环烷基），烷酰基，，羟基，芳基，取代的芳基，杂芳基，取代的杂芳基，全氟烷基，烷氧基，氨基，-NH（烷基），-N（烷基）2或全氟烷氧基; R 4是H，烷基，全芳基烷基，芳基，取代的芳基，杂芳基，取代的杂芳基，烯基，烯基 - 芳基，芳基，-CH 2 R 5，-CH（OH）R 5，-C（O）或-C（S）R 5; R5是H，烷基，全芳基烷基，芳基，取代的芳基，杂芳基，取代的杂芳基，烯基，烯基 - 芳基; R 6是H，烷基，环烷基，-CH 2 - 环烷基，烷基芳基，芳基，取代的芳基，杂芳基或取代的杂芳基; n是0-6的整数; A是COOH或酸模拟物; 或其药学上可接受的盐或酯形式，以及使用这些化合物治疗或预防由纤维蛋白溶解性疾病如深静脉血栓形成和冠心病引起的病症以及肺纤维化的药物组合物和方法。

6. 发明授权

US07629377B2 Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1) 失效
标题翻译：取代的萘基吲哚衍生物作为纤溶酶原激活物抑制剂1型（PAI-1）的抑制剂
公开(公告)号：US07629377B2
公开(公告)日：2009-12-08
申请号：US12026272
申请日：2008-02-05
申请人： David LeRoy Crandall , Scott Christian Mayer , Eric Gould Gundersen , Hassan Mahmoud Elokdah
发明人： David LeRoy Crandall , Scott Christian Mayer , Eric Gould Gundersen , Hassan Mahmoud Elokdah
IPC分类号： A61K31/404 , C07D209/04
CPC分类号： C07D403/12 , C07D209/12
摘要： This invention provides PAI-1 inhibiting compounds of Formula I: wherein: R1, R2, R3, and R4 are each H, alkyl, alkanoyl, halo, OH, aryl optionally substituted with R8, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; R5 is H, alkyl, perfluoroalkyl, aryl optionally substituted with R5, alkanoyl, aroyl optionally substituted with R8; R6 is H, alkyl, alkylaryl, benzyl optionally substituted with R8, alkanoyl, aroyl optionally substituted with R8; R7 is H, alkyl, alkylaryl, aryl optionally substituted with R8; n is 0-6; A is COOH, or an acid mimic such as tetraazole, SO3H, PO3H2, tetronic acid, etc.; R8 is H, alkyl, cycloalkyl, alkanoyl, halo, OH, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; or a pharmaceutically acceptable salt thereof; as well as pharmaceutical compositions and methods of treatment using these compounds.
摘要翻译：本发明提供了PAI-1抑制式I化合物：其中：R1，R2，R3和R4分别为H，烷基，烷酰基，卤素，OH，任选被R8，全氟烷基，烷氧基，氨基，烷基氨基，二烷基氨基，全氟烷氧基 R5是H，烷基，全氟烷基，任选被R 5取代的芳基，烷酰基，任选被R 8取代的芳酰基; R6是H，烷基，烷芳基，任选被R8，烷酰基取代的苄基，任选被R8取代的芳酰基; R7是H，烷基，烷芳基，任选被R8取代的芳基; n为0-6; A是COOH，或酸性模拟物如四唑，SO 3 H，PO 3 H 2，四氢萘等; R8是H，烷基，环烷基，烷酰基，卤素，OH，全氟烷基，烷氧基，氨基，烷基氨基，二烷基氨基，全氟烷氧基; 或其药学上可接受的盐; 以及使用这些化合物的药物组合物和治疗方法。

7. 发明授权

US07534894B2 Biphenyloxy-acids 失效
标题翻译：联苯氧基酸
公开(公告)号：US07534894B2
公开(公告)日：2009-05-19
申请号：US10947710
申请日：2004-09-23
申请人： Thomas Joseph Commons , Susan Christman Croce , Eugene John Trybulski , Hassan Mahmoud Elokdah , David LeRoy Crandall
发明人： Thomas Joseph Commons , Susan Christman Croce , Eugene John Trybulski , Hassan Mahmoud Elokdah , David LeRoy Crandall
IPC分类号： C07D257/06 , C07D333/02 , C07D333/50 , C07D307/02 , C07D307/77
CPC分类号： C07D405/12 , C07C233/60 , C07C233/75 , C07C235/56 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2603/18 , C07D209/30 , C07D209/42 , C07D231/14 , C07D307/68 , C07D307/84 , C07D333/38 , C07D333/68 , C07D403/12
摘要： The present invention relates generally to substituted biphenyloxy acids (such as 4′-aryl-amido-biphenyl-4(3)-yloxy-acids and 4′-aryl-amidomethyl-biphenyl-4(3)-yloxy-acids) and methods of using them, for example, as PAI-1 inhibitors.
摘要翻译：本发明一般涉及取代的联苯氧基酸（例如4'-芳基 - 酰氨基 - 联苯-4（3） - 氧基酸和4'-芳基 - 酰氨基甲基 - 联苯-4（3） - 氧基酸）和方法使用它们，例如，作为PAI-1抑制剂。

8. 发明申请

US20080182883A1 SUBSTITUTED NAPHTHYL INDOLE DERIVATIVES AS INHIBITORS OF PLASMINOGEN ACTIVATOR INHIBITOR TYPE-1 (PAI-1) 失效
标题翻译：作为PLASMINOGEN激活剂抑制剂类型1（PAI-1）的抑制剂的取代的萘基吲哚衍生物
公开(公告)号：US20080182883A1
公开(公告)日：2008-07-31
申请号：US12026272
申请日：2008-02-05
申请人： David LeRoy Crandall , Scott Christian Mayer , Eric Gould Gundersen , Hassan Mahmoud Elokdah
发明人： David LeRoy Crandall , Scott Christian Mayer , Eric Gould Gundersen , Hassan Mahmoud Elokdah
IPC分类号： A61K31/41 , C07D403/02 , A61P7/00 , A61P11/00 , A61P25/28 , A61P35/00
CPC分类号： C07D403/12 , C07D209/12
摘要： This invention provides PAI-1 inhibiting compounds of Formula I: wherein: R1, R2, R3, and R4 are each H, alkyl, , alkanoyl, halo, OH, aryl optionally substituted with R8, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, pertluoroalkoxy; R5 is H, alkyl, perfluoroalkyl, aryl optionally substituted with R5, alkanoyl, aroyl optionally substituted with R8; R6 is H, alkyl, alkylaryl, benzyl optionally substituted with R8, alkanoyl, aroyl optionally substituted with R8; R7 is H, alkyl, alkylaryl, aryl optionally substituted with R8; n is 0-6; A is COOH, or an acid mimic such as tetraazole, SO3H, PO3H2, tetronic acid, etc.; R8 is H, alkyl, cycloalkyl, alkanoyl, halo, OH, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; or a pharmaceutically acceptable salt thereof; as well as pharmaceutical compositions and methods of treatment using these compounds.
摘要翻译：本发明提供了PAI-1抑制式I化合物：其中：R 1，R 2，R 3和R 4 每个H，烷基，烷酰基，卤素，OH，任选被R 8 8，全氟烷基，烷氧基，氨基，烷基氨基，二烷基氨基，全氟烷氧基取代的芳基; R 5是H，烷基，全氟烷基，任选地被R 5， - 烷酰基，任选被R 8取代的芳酰基的芳基取代的芳基; R 6是H，烷基，烷基芳基，任选被R 8取代的苄基，烷酰基，任选被R 8取代的芳酰基; R 7是H，烷基，烷芳基，任选被R 8取代的芳基; n为0-6; A是COOH或酸模拟物，例如四唑，SO 3 H，PO 3 H 2 H 2，次ronic酸等; R 8是H，烷基，环烷基，烷酰基，卤素，OH，全氟烷基，烷氧基，氨基，烷基氨基，二烷基氨基，全氟烷氧基; 或其药学上可接受的盐; 以及使用这些化合物的药物组合物和治疗方法。

9. 发明授权

US06939886B2 Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor Type-1 (PAI-1) 失效
标题翻译：取代的萘基吲哚衍生物作为纤溶酶原激活物抑制剂Type-1（PAI-1）的抑制剂
公开(公告)号：US06939886B2
公开(公告)日：2005-09-06
申请号：US10894618
申请日：2004-07-20
申请人： Scott Christian Mayer , Eric Gould Gundersen , Hassan Mahmoud Elokdah , David LeRoy Crandall
发明人： Scott Christian Mayer , Eric Gould Gundersen , Hassan Mahmoud Elokdah , David LeRoy Crandall
IPC分类号： A61K31/404 , A61K31/41 , A61P3/04 , A61P3/10 , A61P7/02 , A61P9/04 , A61P9/06 , A61P9/10 , A61P9/12 , A61P11/06 , A61P13/12 , A61P17/02 , A61P17/06 , A61P19/02 , A61P19/10 , A61P25/28 , A61P29/00 , A61P31/04 , A61P31/18 , A61P35/00 , A61P37/06 , A61P43/00 , C07D209/12 , C07D403/12 , C07D209/04 , C07D403/02
CPC分类号： C07D403/12 , C07D209/12
摘要： This invention provides PAI-1 inhibiting compounds of Formula I: wherein: R1, R2, R3, and R4 are each H, alkyl, alkanoyl, halo, OH, aryl optionally substituted with R8, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; R5 is H, alkyl, perfluoroalkyl, aryl optionally substituted with R8, alkanoyl, aroyl optionally substituted with R8; R6 is H, alkyl, alkylaryl, benzyl optionally substituted with R8, alkanoyl, aroyl optionally substituted with R8; R7 is H, alkyl, alkylaryl, aryl optionally substituted with R8; n is 0-6; A is COOH, or an acid mimic such as tetraazole, SO3H, PO3H2, tetronic acid, etc.; R8 is H, alkyl, cycloalkyl, alkanoyl, halo, OH, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; or a pharmaceutically acceptable salt thereof; as well as pharmaceutical compositions and methods of treatment using these compounds.
摘要翻译：本发明提供了PAI-1抑制式I化合物：其中：R 1，R 2，R 3和R 4 每个H，烷基，烷酰基，卤素，OH，任选被R 8 8，全氟烷基，烷氧基，氨基，烷基氨基，二烷基氨基，全氟烷氧基取代的芳基; R 5是H，烷基，全氟烷基，任选被R 8取代的芳基，烷酰基，任选被R 8取代的芳酰基; R 6是H，烷基，烷基芳基，任选被R 8取代的苄基，烷酰基，任选被R 8取代的芳酰基; R 7是H，烷基，烷芳基，任选被R 8取代的芳基; n为0-6; A是COOH或酸模拟物，例如四唑，SO 3 H，PO 3 H 2 H 2，次ronic酸等; R 8是H，烷基，环烷基，烷酰基，卤素，OH，全氟烷基，烷氧基，氨基，烷基氨基，二烷基氨基，全氟烷氧基; 或其药学上可接受的盐; 以及使用这些化合物的药物组合物和治疗方法。

10. 发明授权

US07351730B2 Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1) 失效
标题翻译：取代的萘基吲哚衍生物作为纤溶酶原激活物抑制剂1型（PAI-1）的抑制剂
公开(公告)号：US07351730B2
公开(公告)日：2008-04-01
申请号：US11158881
申请日：2005-06-22
申请人： Scott Christian Mayer , Eric Gould Gundersen , Hassan Mahmoud Elokdah , David LeRoy Crandall
发明人： Scott Christian Mayer , Eric Gould Gundersen , Hassan Mahmoud Elokdah , David LeRoy Crandall
IPC分类号： A61K31/404 , C07D209/04 , C07D403/02
CPC分类号： C07D403/12 , C07D209/12
摘要： This invention provides PAI-1 inhibiting compounds of Formula I: wherein: R1, R2, R3, and R4 are each H, alkyl, alkanoyl, halo, OH, aryl optionally substituted with R8, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; R5 is H, alkyl, perfluoroalkyl, aryl optionally substituted with R8, alkanoyl, aroyl optionally substituted with R8; R6 is H, alkyl, alkylaryl, benzyl optionally substituted with R8, alkanoyl, aroyl optionally substituted with R8; R7 is H, alkyl, alkylaryl, aryl optionally substituted with R8; n is 0-6; A is COOH, or an acid mimic such as tetraazole, SO3H, PO3H2, tetronic acid, etc.; R8 is H, alkyl, cycloalkyl, alkanoyl, halo, OH, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; or a pharmaceutically acceptable salt thereof; as well as pharmaceutical compositions and methods of treatment using these compounds.
摘要翻译：本发明提供了PAI-1抑制式I化合物：其中：R 1，R 2，R 3和R 4 每个H，烷基，烷酰基，卤素，OH，任选被R 8 8，全氟烷基，烷氧基，氨基，烷基氨基，二烷基氨基，全氟烷氧基取代的芳基; R 5是H，烷基，全氟烷基，任选被R 8取代的芳基，烷酰基，任选被R 8取代的芳酰基; R 6是H，烷基，烷基芳基，任选被R 8取代的苄基，烷酰基，任选被R 8取代的芳酰基; R 7是H，烷基，烷芳基，任选被R 8取代的芳基; n为0-6; A是COOH或酸模拟物，例如四唑，SO 3 H，PO 3 H 2 H 2，次ronic酸等; R 8是H，烷基，环烷基，烷酰基，卤素，OH，全氟烷基，烷氧基，氨基，烷基氨基，二烷基氨基，全氟烷氧基; 或其药学上可接受的盐; 以及使用这些化合物的药物组合物和治疗方法。

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