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1. 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。

2. 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.

3. 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。

4. 发明授权

US07056943B2 Substituted indole oxo-acetyl amino acetic acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1) 失效
公开(公告)号：US07056943B2
公开(公告)日：2006-06-06
申请号：US10731074
申请日：2003-12-09
申请人： Hassan Mahmoud Elokdah , Geraldine Ruth McFarlane , David Zenan Li
发明人： Hassan Mahmoud Elokdah , Geraldine Ruth McFarlane , David Zenan Li
IPC分类号： A61K43/38 , C07D209/90
CPC分类号： C07D403/06 , C07D209/22
摘要： This invention provides indole oxo-acetyl amino acetic acid derivatives which are useful as inhibitors of plasminogen activator inhibitor-1 (PAI-1) useful for treating fibrinolytic disorders, the compounds having the structure: wherein: R1 is alkyl or optionally substituted cycloalkyl, —CH2-cycloalkyl, pyridinyl, —CH2-pyridinyl, phenyl or benzyl; R2 is hydrogen, alkyl, cycloalkyl, —CH2-cycloalkyl, or perfluoroalkyl; R3 is hydrogen, halo, alkyl, perfluoroalkyl, alkoxy, cycloalkyl, —CH2-cycloalkyl, —NH2, or —NO2; R4 is optionally substituted phenyl, benzyl, benzyloxy, pyridinyl, or —CH2-pyridinyl; R8 is hydrogen, alkyl, cycloalkyl, —CH2-cycloalkyl, perfluoroalkyl, aryl, substituted aryl, alkyl-aryl, or substituted alkyl-aryl; R9 is hydrogen, alkyl, hydroxyalkyl, 4-hydroxybenzyl, 3-indolylymethylene, 4-imidazolylmethylene, HSCH2—, CH3SCH2CH2—, H2NC(═O)CH2—, H2NC(═O)CH2CH2—, HO2CCH2—, HO2CCH2CH2—, H2NCH2CH2CH2CH2—, H2NC(═NH)NHCH2CH2CH2—, or taken together with R8 as —CH2CH2CH2—; or a pharmaceutically acceptable salt or ester form thereof.

5. 发明授权

US07160918B2 Substituted indole oxo-acetyl amino acetic acid derivatives as inhibitors of plasminogen activator inhibitor (PAI-1) 失效
公开(公告)号：US07160918B2
公开(公告)日：2007-01-09
申请号：US11335233
申请日：2006-01-19
申请人： Hassan Mahmoud Elokdah , Geraldine Ruth McFarlane , David Zenan Li
发明人： Hassan Mahmoud Elokdah , Geraldine Ruth McFarlane , David Zenan Li
IPC分类号： A61K43/38 , C07D209/90
CPC分类号： C07D403/06 , C07D209/22
摘要： This invention provides indole oxo-acetyl amino acetic acid derivatives which are useful as inhibitors of plasminogen activator inhibitor-1 (PAI-1) useful for treating fibrinolytic disorders, the compounds having the structure: wherein: R1 is alkyl or optionally substituted cycloalkyl, —CH2-cycloalkyl, pyridinyl, —CH2-pyridinyl, phenyl or benzyl; R2 is hydrogen, alkyl, cycloalkyl, —CH2-cycloalkyl, or perfluoroalkyl; R3 is hydrogen, halo, alkyl, perfluoroalkyl, alkoxy, cycloalkyl, —CH2-cycloalkyl, —NH2, or —NO2; R4 is optionally substituted phenyl, benzyl, benzyloxy, pyridinyl, or —CH2-pyridinyl; R8 is hydrogen, alkyl, cycloalkyl, —CH2-cycloalkyl, perfluoroalkyl, aryl, substituted aryl, alkyl-aryl, or substituted alkyl-aryl; R9 is hydrogen, alkyl, hydroxyalkyl, 4-hydroxybenzyl, 3-indolylymethylene, 4-imidazolylmethylene, HSCH2—, CH3SCH2CH2—, H2NC(═O)CH2—, H2NC(═O)CH2CH2—, HO2CCH2—, HO2CCH2CH2—, H2NCH2CH2CH2CH2—, H2NC(═NH)NHCH2CH2CH2—, or taken together with R8 as —CH2CH2CH2—; or a pharmaceutically acceptable salt or ester form thereof.

6. 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。

7. 发明授权

US07790751B2 Azinyl-3-sulfonylindazole derivatives as 5-hydroxytryptamine-6 ligands 失效
标题翻译：氮茚基-3-磺基吲唑衍生物作为5-羟基色胺-6配体
公开(公告)号：US07790751B2
公开(公告)日：2010-09-07
申请号：US11504243
申请日：2006-08-14
申请人： Hassan Mahmoud Elokdah , Alexander Alexei Greenfield , Kevin Liu , Geraldine Ruth McFarlane , Cristina Grosanu , Jennifer Rebecca Lo , Albert Jean Robichaud
发明人： Hassan Mahmoud Elokdah , Alexander Alexei Greenfield , Kevin Liu , Geraldine Ruth McFarlane , Cristina Grosanu , Jennifer Rebecca Lo , Albert Jean Robichaud
IPC分类号： A61K31/454 , C07D403/02
CPC分类号： C07D231/56 , C07D401/12 , C07D403/12
摘要： The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.
摘要翻译：本发明提供式I化合物及其用于治疗与5-HT 6受体相关或受其影响的中枢神经系统疾病的用途。

8. 发明授权

US07674818B2 Aryl, aryloxy, alkyloxy substituted 1H-indol-3-yl glyoxylic acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1) 失效
标题翻译：芳基，芳氧基，烷氧基取代的1H-吲哚-3-基乙醛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：US07674818B2
公开(公告)日：2010-03-09
申请号：US11827579
申请日：2007-07-11
申请人： Lee Dalton Jennings , Hassan Mahmoud Elokdah , Geraldine Ruth McFarlane
发明人： Lee Dalton Jennings , Hassan Mahmoud Elokdah , Geraldine Ruth McFarlane
IPC分类号： A61K31/404 , C07D209/04
CPC分类号： C07D401/12 , C07D209/18 , C07D209/22 , C07D209/24 , C07D405/06 , C07D405/12 , C07D417/12
摘要： Compounds of formula I are provided: wherein: R1, R2, and R3, are as defined herein, as well as pharmaceutical composition and methods using the compounds as inhibitors of plasminogen activator inhibitor (PAI-1) and as therapeutic composition for treating conditions resulting from fibrinolytic disorders, such as deep vein thrombosis, coronary heart disease and pulmonary fibrosis.
摘要翻译：提供式I化合物：其中：R1，R2和R3如本文所定义，以及使用该化合物作为纤溶酶原激活物抑制剂（PAI-1）的抑制剂的药物组合物和方法，以及作为治疗条件的治疗组合物来自纤维蛋白溶解性疾病，如深静脉血栓形成，冠心病和肺纤维化。

9. 发明授权

US07163954B2 Substituted naphthyl benzothiophene acids 失效
标题翻译：取代的萘基苯并噻吩酸
公开(公告)号：US07163954B2
公开(公告)日：2007-01-16
申请号：US10947898
申请日：2004-09-23
申请人： Hassan Mahmoud Elokdah , Geraldine Ruth McFarlane
发明人： Hassan Mahmoud Elokdah , Geraldine Ruth McFarlane
IPC分类号： A61K31/41 , A61K31/38 , C07D257/04 , C07D333/56
CPC分类号： C07D409/12 , C07D333/56
摘要： The present invention relates generally to substituted naphthyl benzothiophene acids and methods of using them.
摘要翻译：本发明一般涉及取代的萘基苯并噻吩酸及其使用方法。

10. 发明授权

US07723329B2 Substituted-3-sulfonylindazole derivatives as 5-hydroxytryptamine-6 ligands 有权
标题翻译：取代的3-磺基吲唑衍生物作为5-羟色胺-6配体
公开(公告)号：US07723329B2
公开(公告)日：2010-05-25
申请号：US11504350
申请日：2006-08-14
申请人： Hassan Mahmoud Elokdah , Alexander Alexei Greenfield , Kevin Liu , Robert Emmett McDevitt , Geraldine Ruth McFarlane , Cristina Grosanu , Jennifer Rebecca Lo , Yanfang Li , Albert Jean Robichaud , Ronald Charles Bernotas
发明人： Hassan Mahmoud Elokdah , Alexander Alexei Greenfield , Kevin Liu , Robert Emmett McDevitt , Geraldine Ruth McFarlane , Cristina Grosanu , Jennifer Rebecca Lo , Yanfang Li , Albert Jean Robichaud , Ronald Charles Bernotas
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/416 , C07D413/02 , C07D231/56
CPC分类号： C07D231/56 , C07D401/12 , C07D403/06 , C07D403/12 , C07D413/12
摘要： The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.
摘要翻译：本发明提供式I化合物及其用于治疗与5-HT 6受体相关或受其影响的中枢神经系统疾病的用途。

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