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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

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。

4. 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。

5. 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。

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

US20100197744A1 Organic Compounds 审中-公开
标题翻译：有机化合物
公开(公告)号：US20100197744A1
公开(公告)日：2010-08-05
申请号：US12602709
申请日：2008-06-03
申请人： David Barnes , Gary Mark Coppola , Travis Stams , Sidney Wolf Topiol , James Richard Wareing
发明人： David Barnes , Gary Mark Coppola , Travis Stams , Sidney Wolf Topiol , James Richard Wareing
IPC分类号： A61K31/433 , C07D285/08 , A61P3/10 , A61P13/12 , A61P9/06 , A61P9/12 , A61P9/10 , A61P3/06 , A61P35/00 , A61P19/10 , A61P25/16 , A61P25/28
CPC分类号： C07D285/10
摘要： Novel compounds that 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 the present invention 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：作为蛋白酪氨酸磷酸酶抑制剂（PTPases）的新型化合物，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，本发明的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。

9. 发明申请

US20100035942A1 1-orthofluorophenyl substituted 1,2,5-thiazolidinedione derivatives as ptp-as inhibitors 失效
标题翻译： 1-正氟苯基取代的1,2,5-噻唑烷二酮衍生物作为抑制剂
公开(公告)号：US20100035942A1
公开(公告)日：2010-02-11
申请号：US12096432
申请日：2006-12-06
申请人： David Barnes , Gary Mark Coppola , Travis Stams , Sidney Wolf Topiol
发明人： David Barnes , Gary Mark Coppola , Travis Stams , Sidney Wolf Topiol
IPC分类号： A61K31/433 , C07D285/10
CPC分类号： C07D417/10 , C07D285/10
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。

10. 发明授权

US08252820B2 1-orthofluorophenyl substituted 1,2,5-thiazolidinedione derivatives as PTP-as inhibitors 失效
标题翻译： 1-正氟苯基取代的1,2,5-噻唑烷二酮衍生物作为PTP-抑制剂
公开(公告)号：US08252820B2
公开(公告)日：2012-08-28
申请号：US12096432
申请日：2006-12-06
申请人： David Barnes , Gary Mark Coppola , Travis Stams , Sidney Wolf Topiol
发明人： David Barnes , Gary Mark Coppola , Travis Stams , Sidney Wolf Topiol
IPC分类号： A61K31/433 , C07D285/10
CPC分类号： C07D417/10 , C07D285/10
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。

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