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1. 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。

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

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

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

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。

7. 发明授权

US07057039B2 1-heterocyclylalkyl-3-sulfonylazaindole or -azaindazole derivatives as 5-hydroxytryptamine-6 ligands 失效
标题翻译： 1-杂环基烷基-3-磺酰基氮杂吲哚或吖草唑衍生物作为5-羟色胺-6配体
公开(公告)号：US07057039B2
公开(公告)日：2006-06-06
申请号：US10621432
申请日：2003-07-17
申请人： Ronald Charles Bernotas , Steven Edward Lenicek , Hassan Mahmoud Elokdah , David Zenan Li
发明人： Ronald Charles Bernotas , Steven Edward Lenicek , Hassan Mahmoud Elokdah , David Zenan Li
IPC分类号： C07D413/00 , A01N43/64 , A61K31/41
CPC分类号： C07D487/08 , A61K31/454 , A61K31/4745 , A61K31/498 , A61K31/503
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. 发明申请

US20080306106A1 1-HETEROCYCLYLALKYL-3-SULFONYLAZAINDOLE OR -AZAINDAZOLE DERIVATIVES AS 5-HYDROXYTRYPTAMINE-6 LIGANDS 审中-公开
标题翻译：作为5-羟基木聚糖-6配位体的1-环烷基亚甲基-3-磺酰基蓝或衍生物衍生物
公开(公告)号：US20080306106A1
公开(公告)日：2008-12-11
申请号：US12166761
申请日：2008-07-02
申请人： Ronald Charles Bernotas , Steven Edward Lenicek , Hassan Mahmoud Elokdah , David Zenan Li
发明人： Ronald Charles Bernotas , Steven Edward Lenicek , Hassan Mahmoud Elokdah , David Zenan Li
IPC分类号： C07D487/04 , A61K31/437 , A61P25/00 , A61P25/28 , A61P25/30
CPC分类号： C07D487/08 , A61K31/454 , A61K31/4745 , A61K31/498 , A61K31/503
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。

9. 发明授权

US07411064B2 1-Heterocyclylalkyl-3-sulfonylazaindole or -azaindazole derivatives as 5-hydroxytryptamine-6 ligands 失效
标题翻译： 1-杂环烷基-3-磺酰基氮杂吲哚或吖草唑衍生物作为5-羟色胺-6配体
公开(公告)号：US07411064B2
公开(公告)日：2008-08-12
申请号：US11354459
申请日：2006-02-15
申请人： Ronald Charles Bernotas , Steven Edward Lenicek , Hassan Mahmoud Elokdah , David Zenan Li
发明人： Ronald Charles Bernotas , Steven Edward Lenicek , Hassan Mahmoud Elokdah , David Zenan Li
IPC分类号： C07D413/00 , A01N43/64 , A61K31/41
CPC分类号： C07D487/08 , A61K31/454 , A61K31/4745 , A61K31/498 , A61K31/503
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

10. 发明授权

US07101903B2 Substituted dihydropyrano indole-3,4-dione derivatives as inhibitiors of plasminogen activator inhibitor-1 (PAI-1) 失效
标题翻译：取代的二氢吡喃并吲哚-3,4-二酮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：US07101903B2
公开(公告)日：2006-09-05
申请号：US10731290
申请日：2003-12-09
申请人： Hassan Mahmoud Elokdah , David Zenan Li
发明人： Hassan Mahmoud Elokdah , David Zenan Li
IPC分类号： A61K31/407 , C07D209/56
CPC分类号： C07D491/04 , C07D209/22
摘要： Compounds of formula (I) and II) are provided wherein: X is an alkali metal or a basic amine moiety; R1 is alkyl, cycloalkyl, —CH2-cycloalkyl, pyridinyl, —CH2-pyridinyl, phenyl or benzyl, the rings of these groups being optionally substituted; R2 is H, halogen, alkyl, perfluoroalkyl, alkoxy, cycloalkyl, —CH2-cycloalkyl, —NH2, or —NO2; R3 is phenyl, benzyl, benzyloxy, pyridinyl, or —CH2-pyridinyl, with the rings of these groups being optionally substituted; or a pharmaceutically acceptable salt or ester form thereof, as well as pharmaceutical compositions and methods using these 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：提供式（I）和II）的化合物，其中：X为碱金属或碱性胺部分; 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，这些环基团任选被取代; R 2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 2 - SUB> 2 R 3是苯基，苄基，苄氧基，吡啶基或-CH 2 - 吡啶基，这些基团的环任选被取代; 或其药学上可接受的盐或酯形式，以及使用这些化合物作为纤溶酶原激活物抑制剂-1（PAI-1）的抑制剂的药物组合物和方法，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和肺纤维化。

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