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1. 发明申请

WO2007021711A3 SUBSTITUTED-3-SULFONYLINDAZOLE DERIVATIVES AS 5-HYDROXYTRYPTAMINE-6 LIGANDS 审中-公开
公开(公告)号：WO2007021711A3
公开(公告)日：2007-02-22
申请号：PCT/US2006/030965
申请日：2006-08-08
申请人： WYETH , ELOKDAH, Hassan, Mahmoud , GREENFIELD, Alexander, Alexei , LIU, Kevin , MCDEVITT, Robert, Emmett , MCFARLANE, Geraldine, Ruth , GROSANU, Cristina , LO, Jennifer, Rebecca , LI, Yanfang , ROBICHAUD, Albert, Jean , BERNOTAS, Ronald, Charles
发明人： ELOKDAH, Hassan, Mahmoud , GREENFIELD, Alexander, Alexei , LIU, Kevin , MCDEVITT, Robert, Emmett , MCFARLANE, Geraldine, Ruth , GROSANU, Cristina , LO, Jennifer, Rebecca , LI, Yanfang , ROBICHAUD, Albert, Jean , BERNOTAS, Ronald, Charles
IPC分类号： C07D231/56 , C07D401/12 , C07D403/12 , C07D413/12 , C07D403/06 , A61K31/40 , A61P25/00
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.

2. 发明申请

WO2007032833A1 AZINYL-3-SULFONYLINDAZOLE DERIVATIVES AS 5-HYDROXYTRYPTAMINE-6 LIGANDS 审中-公开
标题翻译：作为5-羟基木聚糖-6配位体的亚氨基-3-磺酰基吖啶衍生物
公开(公告)号：WO2007032833A1
公开(公告)日：2007-03-22
申请号：PCT/US2006/030837
申请日：2006-08-08
申请人： WYETH , GROSANU, Cristina , ELOKDAH, Hassan, Mahmoud , GREENFIELD, Alexander, Alexei , LIU, Kevin , MCFARLANE, Geraldine, Ruth , LO, Jennifer, Rebecca , ROBICHAUD, Albert, Jean
发明人： GROSANU, Cristina , ELOKDAH, Hassan, Mahmoud , GREENFIELD, Alexander, Alexei , LIU, Kevin , MCFARLANE, Geraldine, Ruth , LO, Jennifer, Rebecca , ROBICHAUD, Albert, Jean
IPC分类号： C07D231/56 , C07D401/12 , C07D403/12 , A61P25/00
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病症的用途。

3. 发明申请

WO2004052854A2 ARYL, ARYLOXY, AND ALKYLOXY SUBSTITUTED 1H-INDOL-3-YL GLYOXYLIC ACID DERIVATIVES AS INHIBITORS OF PLASMINOGEN ACTIVATOR INHIBITOR-1 (PAI-1) 审中-公开
标题翻译： ARYL，ARYLOXY和ALKYLOXY取代的1-Indol-3-YL GLYOXYLIC酸衍生物作为PLASMINOGEN ACTIVATOR INHIBITOR-1（PAI-1）的抑制剂，
公开(公告)号：WO2004052854A2
公开(公告)日：2004-06-24
申请号：PCT/US2003/038934
申请日：2003-12-09
申请人： WYETH , JENNINGS, Lee, Dalton , ELOKDAH, Hassan, Mahmoud , MCFARLANE, Geraldine, Ruth
发明人： JENNINGS, Lee, Dalton , ELOKDAH, Hassan, Mahmoud , MCFARLANE, Geraldine, Ruth
IPC分类号： C07D209/00
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 R 1 , R 2 and R 3 , are as defined herein, as well ad 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R 1，R 2和R 3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用于治疗所产生的病症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。

4. 发明申请

WO2003000671A1 NAPHTHYL BENZOFURAN 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）的抑制剂的萘磺隆衍生物
公开(公告)号：WO2003000671A1
公开(公告)日：2003-01-03
申请号：PCT/US2002/019231
申请日：2002-06-18
申请人： WYETH
发明人： ELOKDAH, Hassan, Mahmoud , MCFARLANE, Geraldine, Ruth , MAYER, Scott, Christian , CRANDALL, David, LeRoy
IPC分类号： C07D307/79
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 (1), wherein: R, R 1 , R 2 , and R 3 are H, alkyl, cycloalkyl, -CH 2 -(cycloalkyl), alkanoyl, halo, hydroxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, perfluoroalkyl, alkoxy, amino, -NH(alkyl), -N(alkyl) 2 , or perfluoroalkoxy; R 4 is H, alkyl, perflouroalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, alkenyl, alkenyl-aryl, aryl, -CH 2 R 5 , -CH(OH)R 5 , -C(O)R 5 , -CH(SH)R 5 , or -G(S)R 5 ; R 5 is H, alkyl, perflouroalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, alkenyl, alkenyl-aryl; R 6 is H, alkyl, cycloalkyl, -CH 2 -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, and processes for the preparation of such compounds.
摘要翻译：本发明提供了作为式（1）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 1，R 2，R 3是H，烷基，环烷基，-CH 2， - （环烷基），烷酰基，卤素，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）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，链烯基 - 芳基，芳基，-CH 2， C（O）R 5，-CH（SH）R 5或-G（S）R 5。芳基，取代的芳基，杂芳基，取代的杂芳基，烯基，链烯基 - 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和肺纤维化的药物组合物和方法，以及制备这些化合物的方法化合物。

5. 发明申请

WO2003000253A1 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：WO2003000253A1
公开(公告)日：2003-01-03
申请号：PCT/US2002/019344
申请日：2002-06-18
申请人： WYETH
发明人： ELOKDAH, Hassan, Mahmoud , MCFARLANE, Geraldine, Ruth , LI, David, Zenan , JENNINGS, Lee, Dalton , CRANDALL, David, Leroy
IPC分类号： A61K31/405
CPC分类号： C07D209/12
摘要： This invention provides compounds of the formula : (I) wherein: X is a chemical bond, -CH 2 - or -C(O)-; R 1 is alkyl, cycloalkyl, -CH 2 -cycloalkyl, pyridinyl, -CH 2 -pyridinyl, phenyl or benzyl; R 2 is H, alkyl, cycloalkyl, -CH 2 -cycloalkyl, or perfluoroalkyl; R3 is H, halo, alkyl, perfluoroalkyl, alkoxy, cycloalkyl, -CH 2 -cycloalkyl, -NH 2 , or -NO 2 ; R 4 is optionally substituted phenyl, benzyl, benzyloxy, pyridinyl, or -CH 2 -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, and processes for their preparation.
摘要翻译：本发明提供下式的化合物：（I）其中：X是化学键，-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; R2是H，烷基，环烷基，-CH2-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 - 环烷基，-NH 2或-NO 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，以及使用该化合物作为纤溶酶原激活物抑制剂-1（PAI-1）抑制剂和作为治疗剂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的组合物和肺纤维化，及其制备方法。

6. 发明授权

EP1397130B1 SUBSTITUTED INDOLE ACID DERIVATIVES AS INHIBITORS OF PLASMINOGEN ACTIVATOR INHIBITOR-1 (PAI-1) 有权
标题翻译：取代INDOLSÄUREDERIVATE纤溶酶原激活物抑制剂-1的抑制剂（PAI-1）
公开(公告)号：EP1397130B1
公开(公告)日：2007-07-25
申请号：EP02744425.6
申请日：2002-06-18
申请人： Wyeth
发明人： ELOKDAH, Hassan, Mahmoud , MCFARLANE, Geraldine, Ruth , LI, David, Zenan , JENNINGS, Lee, Dalton , CRANDALL, David, Leroy
IPC分类号： A61K31/405 , C07D209/12
CPC分类号： C07D209/12
摘要： This invention provides compounds of the formula : (I) 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, and processes for their preparation.

7. 发明公开

EP1569901A2 ARYL, ARYLOXY, AND ALKYLOXY SUBSTITUTED i 1H /i -INDOL-3-YL GLYOXYLIC ACID DERIVATIVES AS INHIBITORS OF PLASMINOGEN ACTIVATOR INHIBITOR-1 (PAI-1) 有权
标题翻译： ARYL-，ARYLOXY-ALKYLOXYSUBSTITUIERTE 1H-INDOL-3-YL-GLYOXYLSAUREDERIVATEALS INHIBITOREN DES PLASMINOGENAKTIVATORINHIBITORS-1（PAI-1）
公开(公告)号：EP1569901A2
公开(公告)日：2005-09-07
申请号：EP03812847.6
申请日：2003-12-09
申请人： Wyeth
发明人： JENNINGS, Lee, Dalton , ELOKDAH, Hassan, Mahmoud , MCFARLANE, Geraldine, Ruth
IPC分类号： C07D209/12
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 ad 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.

8. 发明公开

EP1915348A1 AZINYL-3-SULFONYLINDAZOLE DERIVATIVES AS 5-HYDROXYTRYPTAMINE-6 LIGANDS 审中-公开
标题翻译：吖嗪基-3- SULFONYLINDAZOL衍生物作为5-HYDROXYTRYTAMIN-6配体
公开(公告)号：EP1915348A1
公开(公告)日：2008-04-30
申请号：EP06800937.2
申请日：2006-08-08
申请人： Wyeth
发明人： ELOKDAH, Hassan, Mahmoud , GREENFIELD, Alexander, Alexei , LIU, Kevin , MCFARLANE, Geraldine, Ruth , LO, Jennifer, Rebecca , ROBICHAUD, Albert, Jean , GROSANU, Cristina
IPC分类号： C07D231/56 , C07D401/12 , C07D403/12 , A61P25/00
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.

9. 发明公开

EP1397130A1 SUBSTITUTED INDOLE ACID DERIVATIVES AS INHIBITORS OF PLASMINOGEN ACTIVATOR INHIBITOR-1 (PAI-1) 有权
标题翻译：取代INDOLSÄUREDERIVATE纤溶酶原激活物抑制剂-1的抑制剂（PAI-1）
公开(公告)号：EP1397130A1
公开(公告)日：2004-03-17
申请号：EP02744425.6
申请日：2002-06-18
申请人： Wyeth
发明人： ELOKDAH, Hassan, Mahmoud , MCFARLANE, Geraldine, Ruth , LI, David, Zenan , JENNINGS, Lee, Dalton , CRANDALL, David, Leroy
IPC分类号： A61K31/405 , C07D209/12
CPC分类号： C07D209/12
摘要： This invention provides compounds of the formula : (I) 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, and processes for their preparation.

10. 发明授权

EP1569901B1 ARYL, ARYLOXY, AND ALKYLOXY SUBSTITUTED i 1H /i -INDOL-3-YL GLYOXYLIC ACID DERIVATIVES AS INHIBITORS OF PLASMINOGEN ACTIVATOR INHIBITOR-1 (PAI-1) 有权
标题翻译：芳基，芳氧基和ALKYLOXYSUBSTITUIERTE -1H-吲哚-3-基 - GLYOXYLSÄUREDERIVATEALS纤溶酶原激活物抑制剂-1的抑制剂（PAI-1）
公开(公告)号：EP1569901B1
公开(公告)日：2008-10-15
申请号：EP03812847.6
申请日：2003-12-09
申请人： Wyeth
发明人： JENNINGS, Lee, Dalton , ELOKDAH, Hassan, Mahmoud , MCFARLANE, Geraldine, Ruth
IPC分类号： C07D209/12
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 ad 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.

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