公开(公告)号：US07183304B2

公开(公告)日：2007-02-27

申请号：US10495992

申请日：2002-11-20

申请人： Andrew Thomas Bach ,  Prasad Koteswara Kapa ,  George Tien-San Lee ,  Eric M. Loesser ,  Michael Lloyd Sabio ,  James Lawrence Stanton ,  Thalaththani Ralalage Vedananda

发明人： Andrew Thomas Bach ,  Prasad Koteswara Kapa ,  George Tien-San Lee ,  Eric M. Loesser ,  Michael Lloyd Sabio ,  James Lawrence Stanton ,  Thalaththani Ralalage Vedananda

IPC分类号： A61K31/422 ,  A61K31/405 ,  C07D263/32 ,  C07D209/30

CPC分类号： C07D205/04 ,  C07D207/16 ,  C07D209/42 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

摘要： Compounds of the formula provide pharmacological agents which are potent agonists of Peroxisome Proliferator-Activated Receptors (PPARs). Accordingly, the compounds of the instant invention are useful for the treatment of conditions mediated by the PPAR receptor activity in mammals. Such conditions include dyslipidemia, hyperlipidemia, hypercholesteremia, atherosclerosis, hypertriglyceridemia, heart failure, myocardial infarction, vascular diseases, cardiovascular diseases, hypertension, obesity, inflammation, arthritis, cancer, Alzheimer's disease, skin disorders, respiratory diseases, ophthalmic disorders, inflammatory bowel diseases, ulcerative colitis and Crohn's disease. The compounds of the present invention are particularly useful in mammals as hypoglycemic agents for the treatment and prevention of conditions in which impaired glucose tolerance, hyperglycemia and insulin resistance are implicated, such as type-1 and type-2 diabetes, and Syndrome X. Preferred are the compounds of the invention which are dual agonists of PPARα and PPARγ receptors.

摘要翻译： 配方的化合物提供作为过氧化物酶体增殖物激活受体（PPARs）的有效激动剂的药理学试剂。 因此，本发明的化合物可用于治疗由哺乳动物中的PPAR受体活性介导的病症。 这些病症包括血脂异常，高脂血症，高胆固醇血症，动脉粥样硬化，高甘油三酯血症，心力衰竭，心肌梗塞，血管疾病，心血管疾病，高血压，肥胖症，炎症，关节炎，癌症，阿尔茨海默病，皮肤病，呼吸系统疾病，眼科疾病，炎症性肠病 ，溃疡性结肠炎和克罗恩病。 本发明的化合物在哺乳动物中特别可用作降血糖药，用于治疗和预防葡萄糖耐量降低，高血糖症和胰岛素抵抗等疾病，如1型和2型糖尿病，以及X综合征。 是本发明的化合物，它们是PPARα和PPARγ受体的双重激动剂。

公开(公告)号：US20110251171A1

公开(公告)日：2011-10-13

申请号：US13166663

申请日：2011-06-22

申请人： Andrew Thomas Bach ,  Prasad Koteswara Kapa ,  George Tien-San Lee ,  Eric M. Loeser ,  Michael Lloyd Sabio ,  James Lawrence Stanton ,  Thalaththani Ralalage Vedananda

发明人： Andrew Thomas Bach ,  Prasad Koteswara Kapa ,  George Tien-San Lee ,  Eric M. Loeser ,  Michael Lloyd Sabio ,  James Lawrence Stanton ,  Thalaththani Ralalage Vedananda

IPC分类号： A61K31/397 ,  A61K31/5415 ,  A61K31/4725 ,  C07D417/12 ,  A61K31/422 ,  A61K31/404 ,  A61K31/427 ,  A61K31/40 ,  A61P3/10 ,  A61K31/538 ,  C07D401/12 ,  C07D411/12 ,  C07D413/12 ,  C07D209/30 ,  C07D207/48 ,  C07D205/04 ,  A61P9/12 ,  A61P9/00 ,  A61P11/00 ,  A61P27/02 ,  A61P25/28 ,  A61P1/00 ,  A61P17/00 ,  A61P3/06

CPC分类号： C07D205/04 ,  C07D207/16 ,  C07D209/42 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

摘要： Compounds of the formula provide pharmacological agents which are potent agonists of Peroxisome Proliferator-Activated Receptors (PPARs). Accordingly, the compounds of the instant invention are useful for the treatment of conditions mediated by the PPAR receptor activity in mammals. Such conditions include dyslipidemia, hyperlipidemia, hypercholesteremia, atherosclerosis, hypertriglyceridemia, heart failure, myocardial infarction, vascular diseases, cardiovascular diseases, hypertension, obesity, inflammation, arthritis, cancer, Alzheimer's disease, skin disorders, respiratory diseases, ophthalmic disorders, inflammatory bowel diseases, ulcerative colitis and Crohn's disease. The compounds of the present invention are particularly useful in mammals as hypoglycemic agents for the treatment and prevention of conditions in which impaired glucose tolerance, hyperglycemia and insulin resistance are implicated, such as type-1 and type-2 diabetes, and Syndrome X. Preferred are the compounds of the invention which are dual agonists of PPARα and PPARγ receptors.

摘要翻译： 配方的化合物提供作为过氧化物酶体增殖物激活受体（PPARs）的有效激动剂的药理学试剂。 因此，本发明的化合物可用于治疗由哺乳动物中的PPAR受体活性介导的病症。 这些病症包括血脂异常，高脂血症，高胆固醇血症，动脉粥样硬化，高甘油三酯血症，心力衰竭，心肌梗死，血管疾病，心血管疾病，高血压，肥胖症，炎症，关节炎，癌症，阿尔茨海默病，皮肤病，呼吸系统疾病，眼科疾病，炎症性肠病 ，溃疡性结肠炎和克罗恩病。 本发明的化合物在哺乳动物中特别可用作降血糖药，用于治疗和预防葡萄糖耐量降低，高血糖症和胰岛素抵抗等疾病，如1型和2型糖尿病，以及X综合征。 是PPARα和PPARγ受体的双重激动剂的本发明化合物。

公开(公告)号：US20090118160A1

公开(公告)日：2009-05-07

申请号：US12349239

申请日：2009-01-06

申请人： Andrew Thomas Bach ,  Prasad Koteswara Kapa ,  George Tien-San Lee ,  Eric M. Loeser ,  Michael Lloyd Sabio ,  James Lawrence Stanton ,  Thalaththani Ralalage Vedananda

发明人： Andrew Thomas Bach ,  Prasad Koteswara Kapa ,  George Tien-San Lee ,  Eric M. Loeser ,  Michael Lloyd Sabio ,  James Lawrence Stanton ,  Thalaththani Ralalage Vedananda

IPC分类号： A61K38/28 ,  C07D209/04 ,  A61K31/404 ,  C07D413/02 ,  A61K31/422 ,  C07D205/04 ,  A61K31/397 ,  A61P9/04 ,  C07D403/02 ,  A61P9/00 ,  C07D401/02 ,  A61K31/4709 ,  A61P9/12 ,  A61K31/423 ,  A61P19/02 ,  A61K31/538 ,  C07D417/02 ,  A61K31/427 ,  C07D263/30 ,  A61P3/04 ,  A61P35/00 ,  A61P25/28 ,  A61P1/00 ,  A61P3/10 ,  A61P17/00 ,  A61P11/00 ,  A61P27/02

CPC分类号： C07D205/04 ,  C07D207/16 ,  C07D209/42 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

摘要： Compounds of the formula provide pharmacological agents which are potent agonists of Peroxisome Proliferator-Activated Receptors (PPARs). Accordingly, the compounds of the instant invention are useful for the treatment of conditions mediated by the PPAR receptor activity in mammals. Such conditions include dyslipidemia, hyperlipidemia, hypercholesteremia, atherosclerosis, hypertriglyceridemia, heart failure, myocardial infarction, vascular diseases, cardiovascular diseases, hypertension, obesity, inflammation, arthritis, cancer, Alzheimer's disease, skin disorders, respiratory diseases, ophthalmic disorders, inflammatory bowel diseases, ulcerative colitis and Crohn's disease. The compounds of the present invention are particularly useful in mammals as hypoglycemic agents for the treatment and prevention of conditions in which impaired glucose tolerance, hyperglycemia and insulin resistance are implicated, such as type-1 and type-2 diabetes, and Syndrome X. Preferred are the compounds of the invention which are dual agonists of PPARα and PPARγ receptors.

摘要翻译： 配方的化合物提供作为过氧化物酶体增殖物激活受体（PPARs）的有效激动剂的药理学试剂。 因此，本发明的化合物可用于治疗由哺乳动物中的PPAR受体活性介导的病症。 这些病症包括血脂异常，高脂血症，高胆固醇血症，动脉粥样硬化，高甘油三酯血症，心力衰竭，心肌梗死，血管疾病，心血管疾病，高血压，肥胖症，炎症，关节炎，癌症，阿尔茨海默病，皮肤病，呼吸系统疾病，眼科疾病，炎症性肠病 ，溃疡性结肠炎和克罗恩病。 本发明的化合物在哺乳动物中特别可用作降血糖药，用于治疗和预防葡萄糖耐量降低，高血糖症和胰岛素抵抗等疾病，如1型和2型糖尿病，以及X综合征。 是本发明的化合物，它们是PPARα和PPARγ受体的双重激动剂。