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1. 发明授权

US08084448B2 Organic compounds 有权
标题翻译：有机化合物
公开(公告)号：US08084448B2
公开(公告)日：2011-12-27
申请号：US12295545
申请日：2007-03-29
申请人： Alan Neubert , David Barnes , Young-Shin Kwak , Katsumasa Nakajima , Gregory Raymond Bebernitz , Gary Mark Coppola , Louise Kirman , Michael H. Serrano-Wu , Travis Stams , Sidney Wolf Topiol , Thalaththani Ralalage Vedananda , James Richard Wareing
发明人： Alan Neubert , David Barnes , Young-Shin Kwak , Katsumasa Nakajima , Gregory Raymond Bebernitz , Gary Mark Coppola , Louise Kirman , Michael H. Serrano-Wu , Travis Stams , Sidney Wolf Topiol , Thalaththani Ralalage Vedananda , James Richard Wareing
IPC分类号： A61K31/55 , A61K31/445 , A61K31/41 , C07D487/00 , C07D401/00 , C07D285/10
CPC分类号： C07D285/10 , C07D417/10
摘要： Compounds of the formula are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated. In addition, the compounds of the present invention may be employed to treat and/or prevent cancer, osteoporosis, musculoskeletal, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.
摘要翻译：式的化合物是蛋白酪氨酸磷酸酶（PTPases）的抑制剂，因此可用于治疗由PTPase活性介导的病症。本发明的化合物也可以用作以磷酸酪氨酸结合区如SH2结构域为特征的其它酶的抑制剂。因此，式（I）化合物可用于预防和/或治疗与大，小血管的肥胖，葡萄糖不耐受，糖尿病，高血压和缺血性疾病相关的胰岛素抵抗，伴随2型糖尿病的病症，包括高脂血症，高甘油三酯血症，动脉粥样硬化，血管再狭窄，肠易激综合征，胰腺炎，脂肪细胞肿瘤，以及诸如脂肪肉瘤，血脂异常和其它指示胰岛素抵抗的疾病。此外，本发明的化合物可用于治疗和/或预防癌症，骨质疏松症，肌肉骨骼，神经变性和感染性疾病以及涉及炎症和免疫系统的疾病。

2. 发明授权

US07700633B2 Organic compounds 失效
标题翻译：有机化合物
公开(公告)号：US07700633B2
公开(公告)日：2010-04-20
申请号：US12096439
申请日：2006-12-06
申请人： David Barnes , Gregory Raymond Bebernitz , Gary Mark Coppola , Travis Stams , Sidney Wolf Topiol , Thalaththani Ralalage Vedananda , James Richard Wareing , Katsumasa Nakajima
发明人： David Barnes , Gregory Raymond Bebernitz , Gary Mark Coppola , Travis Stams , Sidney Wolf Topiol , Thalaththani Ralalage Vedananda , James Richard Wareing , Katsumasa Nakajima
IPC分类号： A61K31/433 , C07D285/10
CPC分类号： C07D285/10 , C07D417/04 , C07D417/10
摘要： Compounds of the formula are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. The compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated. In addition, the compounds of the present invention may be employed to treat and/or prevent cancer, osteoporosis, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.
摘要翻译：式的化合物是蛋白酪氨酸磷酸酶（PTPases）的抑制剂，因此可用于治疗由PTPase活性介导的病症。本发明的化合物也可以用作以磷酸酪氨酸结合区如SH2结构域为特征的其它酶的抑制剂。式（I）化合物可用于预防和/或治疗与大，小血管的肥胖，葡萄糖不耐受，糖尿病，高血压和缺血性疾病相关的胰岛素抵抗，伴随2型糖尿病的病症，包括高脂血症，高甘油三酯血症，动脉粥样硬化，血管再狭窄，肠易激综合征，胰腺炎，脂肪细胞肿瘤和诸如脂肪肉瘤，血脂异常和其它指示胰岛素抵抗的疾病。此外，本发明的化合物可用于治疗和/或预防癌症，骨质疏松症，神经变性和感染性疾病以及涉及炎症和免疫系统的疾病。

3. 发明申请

US20090181928A1 ORGANIC COMPOUNDS 有权
标题翻译：有机化合物
公开(公告)号：US20090181928A1
公开(公告)日：2009-07-16
申请号：US12295545
申请日：2007-03-29
申请人： Alan Neubert , David Barnes , Young-Shin Kwak , Katsumasa Nakajima , Gregory Raymond Bebernitz , Gary Mark Coppola , Louise Kirman , Michael H. Serrano-Wu , Travis Stams , Sidney Wolf Topiol , Thalaththani Ralalage Vedananda , James Richard Wareing
发明人： Alan Neubert , David Barnes , Young-Shin Kwak , Katsumasa Nakajima , Gregory Raymond Bebernitz , Gary Mark Coppola , Louise Kirman , Michael H. Serrano-Wu , Travis Stams , Sidney Wolf Topiol , Thalaththani Ralalage Vedananda , James Richard Wareing
IPC分类号： A61K31/695 , C07D285/10 , A61K31/433 , A61K31/454 , C07D417/10 , C07D417/12 , A61K31/55 , C07F7/10 , A61P3/10
CPC分类号： C07D285/10 , C07D417/10
摘要： Compounds of the formula are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated. In addition, the compounds of the present invention may be employed to treat and/or prevent cancer, osteoporosis, musculoskeletal, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.
摘要翻译：式的化合物是蛋白酪氨酸磷酸酶（PTPases）的抑制剂，因此可用于治疗由PTPase活性介导的病症。本发明的化合物也可以用作以磷酸酪氨酸结合区如SH2结构域为特征的其它酶的抑制剂。因此，式（I）化合物可用于预防和/或治疗与大，小血管的肥胖，葡萄糖不耐受，糖尿病，高血压和缺血性疾病相关的胰岛素抵抗，伴随2型糖尿病的病症，包括高脂血症，高甘油三酯血症，动脉粥样硬化，血管再狭窄，肠易激综合征，胰腺炎，脂肪细胞肿瘤，以及诸如脂肪肉瘤，血脂异常和其它指示胰岛素抵抗的疾病。此外，本发明的化合物可用于治疗和/或预防癌症，骨质疏松症，肌肉骨骼，神经变性和感染性疾病以及涉及炎症和免疫系统的疾病。

4. 发明申请

US20080262050A1 Organic Compounds 失效
标题翻译：有机化合物
公开(公告)号：US20080262050A1
公开(公告)日：2008-10-23
申请号：US12096439
申请日：2006-12-06
申请人： David Barnes , Gregory Raymond Bebernitz , Gary Mark Coppola , Katsumasa Nakajima , Travis Stams , Sidney Wolf Topiol , Thalaththani Ralalage Vedananda , James Richard Wareing
发明人： David Barnes , Gregory Raymond Bebernitz , Gary Mark Coppola , Katsumasa Nakajima , Travis Stams , Sidney Wolf Topiol , Thalaththani Ralalage Vedananda , James Richard Wareing
IPC分类号： A61K31/433 , C07D285/10 , A61P3/00 , A61P25/00 , A61P9/00 , C07D417/02
CPC分类号： C07D285/10 , C07D417/04 , C07D417/10
摘要： Compounds of the formula are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. The compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated. In addition, the compounds of the present invention may be employed to treat and/or prevent cancer, osteoporosis, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.
摘要翻译：式的化合物是蛋白酪氨酸磷酸酶（PTPases）的抑制剂，因此可用于治疗由PTPase活性介导的病症。本发明的化合物也可以用作以磷酸酪氨酸结合区如SH2结构域为特征的其它酶的抑制剂。式（I）化合物可用于预防和/或治疗与大，小血管的肥胖，葡萄糖不耐受，糖尿病，高血压和缺血性疾病相关的胰岛素抵抗，伴随2型糖尿病的病症，包括高脂血症，高甘油三酯血症，动脉粥样硬化，血管再狭窄，肠易激综合征，胰腺炎，脂肪细胞肿瘤和诸如脂肪肉瘤，血脂异常和其它指示胰岛素抵抗的疾病。此外，本发明的化合物可用于治疗和/或预防癌症，骨质疏松症，神经变性和感染性疾病以及涉及炎症和免疫系统的疾病。

5. 发明申请

US20080293776A1 1,2,5-Thiazolidine Derivatives Useful for Treating Conditions Mediated by Protein Tyrosine Phosphatases (Ptpase) 有权
标题翻译：用于治疗由蛋白酪氨酸磷酸酶（Ptpase）介导的病症的1,2,5-噻唑烷衍生物
公开(公告)号：US20080293776A1
公开(公告)日：2008-11-27
申请号：US12096393
申请日：2006-12-06
申请人： David Barnes , Gregory Raymond Bebernitz , Gary Mark Coppola , Travis Stams , Sidney Wolf Topiol , Thalaththani Ralalage Vedananda , James Richard Wareing
发明人： David Barnes , Gregory Raymond Bebernitz , Gary Mark Coppola , Travis Stams , Sidney Wolf Topiol , Thalaththani Ralalage Vedananda , James Richard Wareing
IPC分类号： A61K31/4439 , C07D285/10 , A61K31/433 , A61P3/00 , C07D417/10
CPC分类号： C07D285/16
摘要： Compounds of the formula are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated. In addition, the compounds of the present invention may be employed to treat and/or prevent cancer, osteoporosis, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.
摘要翻译：式的化合物是蛋白酪氨酸磷酸酶（PTPases）的抑制剂，因此可用于治疗由PTPase活性介导的病症。本发明的化合物也可以用作以磷酸酪氨酸结合区如SH2结构域为特征的其它酶的抑制剂。因此，式（I）化合物可用于预防和/或治疗与大，小血管的肥胖，葡萄糖不耐受，糖尿病，高血压和缺血性疾病相关的胰岛素抵抗，伴随2型糖尿病的病症，包括高脂血症，高甘油三酯血症，动脉粥样硬化，血管再狭窄，肠易激综合征，胰腺炎，脂肪细胞肿瘤，以及诸如脂肪肉瘤，血脂异常和其它指示胰岛素抵抗的疾病。此外，本发明的化合物可用于治疗和/或预防癌症，骨质疏松症，神经变性和感染性疾病以及涉及炎症和免疫系统的疾病。

6. 发明授权

US08119666B2 1,2,5-thiazolidine derivatives useful for treating conditions mediated by protein tyrosine phosphatases (PTPase) 有权
标题翻译：可用于治疗由蛋白酪氨酸磷酸酶（PTPase）介导的病症的1,2,5-噻唑烷衍生物
公开(公告)号：US08119666B2
公开(公告)日：2012-02-21
申请号：US12096393
申请日：2006-12-06
申请人： David Barnes , Gregory Raymond Bebernitz , Gary Mark Coppola , Travis Stams , Sidney Wolf Topiol , Thalaththani Ralalage Vedananda , James Richard Wareing
发明人： David Barnes , Gregory Raymond Bebernitz , Gary Mark Coppola , Travis Stams , Sidney Wolf Topiol , Thalaththani Ralalage Vedananda , James Richard Wareing
IPC分类号： A61K31/4436 , A61K31/433 , C07D417/10 , C07D285/10
CPC分类号： C07D285/16
摘要： Compounds of the formula are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated. In addition, the compounds of the present invention may be employed to treat and/or prevent cancer, osteoporosis, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.
摘要翻译：式的化合物是蛋白酪氨酸磷酸酶（PTPases）的抑制剂，因此可用于治疗由PTPase活性介导的病症。本发明的化合物也可以用作以磷酸酪氨酸结合区如SH2结构域为特征的其它酶的抑制剂。因此，式（I）化合物可用于预防和/或治疗与大，小血管的肥胖，葡萄糖不耐受，糖尿病，高血压和缺血性疾病相关的胰岛素抵抗，伴随2型糖尿病的病症，包括高脂血症，高甘油三酯血症，动脉粥样硬化，血管再狭窄，肠易激综合征，胰腺炎，脂肪细胞肿瘤，以及诸如脂肪肉瘤，血脂异常和其它指示胰岛素抵抗的疾病。此外，本发明的化合物可用于治疗和/或预防癌症，骨质疏松症，神经变性和感染性疾病以及涉及炎症和免疫系统的疾病。

7. 发明申请

US20080293782A1 1,1,3-Trioxo-1,2,5-Thiadiazolidines and Their Use as Ptp-Ases Inhibitors 审中-公开
标题翻译： 1,1,3-三氧杂-1,2,5-噻二唑烷及其作为Ptp-Ases抑制剂的用途
公开(公告)号：US20080293782A1
公开(公告)日：2008-11-27
申请号：US12096421
申请日：2006-12-06
申请人： David Barnes , Gary Mark Coppola , Robert Edson Damon , Katsumasa Nakajima , Brian Christopher Raudenbush , Travis Stams , Sidney Wolf Topiol , Thalaththani Ralalage Vedananda
发明人： David Barnes , Gary Mark Coppola , Robert Edson Damon , Katsumasa Nakajima , Brian Christopher Raudenbush , Travis Stams , Sidney Wolf Topiol , Thalaththani Ralalage Vedananda
IPC分类号： A61K31/433 , C07D285/10 , A61P3/10 , A61P3/04 , A61P9/10 , A61P25/28 , A61P35/00
CPC分类号： C07D285/10 , C07D417/10
摘要： Compounds of the formula are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated. In addition, the compounds of the present invention may be employed to treat and/or prevent cancer, osteoporosis, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.
摘要翻译：式的化合物是蛋白酪氨酸磷酸酶（PTPases）的抑制剂，因此可用于治疗由PTPase活性介导的病症。本发明的化合物也可以用作以磷酸酪氨酸结合区如SH2结构域为特征的其它酶的抑制剂。因此，式（I）化合物可用于预防和/或治疗与大，小血管的肥胖，葡萄糖不耐受，糖尿病，高血压和缺血性疾病相关的胰岛素抵抗，伴随2型糖尿病的病症，包括高脂血症，高甘油三酯血症，动脉粥样硬化，血管再狭窄，肠易激综合征，胰腺炎，脂肪细胞肿瘤，以及诸如脂肪肉瘤，血脂异常和其它指示胰岛素抵抗的疾病。此外，本发明的化合物可用于治疗和/或预防癌症，骨质疏松症，神经变性和感染性疾病以及涉及炎症和免疫系统的疾病。

8. 发明申请

US20110251171A1 HETEROCYCLIC COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译：杂环化合物和使用方法
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。

9. 发明授权

US07652061B2 N-acyl nitrogen heterocycles as ligands of peroxisome proliferator-activated receptors 失效
标题翻译： N-酰基氮杂环作为过氧化物酶体增殖物激活受体的配体
公开(公告)号：US07652061B2
公开(公告)日：2010-01-26
申请号：US10556988
申请日：2004-05-19
申请人： Gary Michael Ksander , Thalaththani Ralalage Vedananda
发明人： Gary Michael Ksander , Thalaththani Ralalage Vedananda
IPC分类号： A61K31/40 , C07D207/08
CPC分类号： C07D207/16 , C07D401/12 , C07D413/12 , C07D417/12
摘要： Compounds of the formula provide pharmacological agents which bind to 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, Crohn's disease, and conditions in which impaired glucose tolerance, hyperglycemia and insulin resistance are implicated, such as type-1 and type-2 diabetes, and Syndrome X.
摘要翻译：配方的化合物提供与过氧化物酶体增殖物激活受体（PPAR）结合的药理学试剂。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，克罗恩病，以及涉及葡萄糖耐量降低，高血糖症和胰岛素抵抗的病症，例如1型和2型糖尿病和X综合症。

10. 发明授权

US07538135B2 Benzenesulfonylamino compounds and pharmaceutical compositions containing these compounds 失效
标题翻译：苯磺酰氨基化合物和含有这些化合物的药物组合物
公开(公告)号：US07538135B2
公开(公告)日：2009-05-26
申请号：US10563708
申请日：2004-07-07
申请人： Thalaththani Ralalage Vedananda
发明人： Thalaththani Ralalage Vedananda
IPC分类号： A61K31/553 , A61K31/415 , A01N43/56
CPC分类号： C07D413/12
摘要： Compounds of the formula provide pharmacological agents which bind to 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 (IBDs), ulcerative colitis and Crohn's disease, and conditions in which impaired glucose tolerance, hyperglycemia and insulin resistance are implicated, such as type-1 and type-2 diabetes, and Syndrome X.
摘要翻译：配方的化合物提供与过氧化物酶体增殖物激活受体（PPAR）结合的药理学试剂。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（IBD），溃疡性结肠炎和克罗恩氏病，以及涉及葡萄糖耐量降低，高血糖症和胰岛素抵抗的病症，如1型和2型糖尿病，以及综合征X.

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