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1. 发明申请

WO2007067615A3 THIADIAZOLE DERIVATIVES AS ANTIDIABETIC AGENTS 审中-公开
公开(公告)号：WO2007067615A3
公开(公告)日：2007-06-14
申请号：PCT/US2006/046545
申请日：2006-12-06
申请人： NOVARTIS AG , NOVARTIS PHARMA GmbH , BARNES, David , BEBERNITZ, Gregory Raymond , COPPOLA, Gary Mark , NAKAJIMA, Katsumasa , STAMS, Travis , TOPIOL, Sidney Wolf , VEDANANDA, Thalaththani Ralalage , WAREING, James Richard
发明人： BARNES, David , BEBERNITZ, Gregory Raymond , COPPOLA, Gary Mark , NAKAJIMA, Katsumasa , STAMS, Travis , TOPIOL, Sidney Wolf , VEDANANDA, Thalaththani Ralalage , WAREING, James Richard
IPC分类号： C07D285/10 , C07D417/04 , C07D417/10 , A61K31/433 , A61P3/10
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 (such as prostate or breast cancer), osteoporosis, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.

2. 发明申请

WO2007115058A3 THIADIAZOLIDINONE INHIBITORS OF PTPASE 审中-公开
公开(公告)号：WO2007115058A3
公开(公告)日：2007-10-11
申请号：PCT/US2007/065421
申请日：2007-03-29
申请人： NOVARTIS AG , NOVARTIS PHARMA GmbH , NEUBERT, Alan , BARNES, David , KWAK, Young-shin , NAKAJIMA, Katsumasa , BEBERNITZ, Gregory Raymond , COPPOLA, Gary Mark , KIRMAN, Louise , SERRANO-WU, Michael H. , STAMS, Travis , TOPIOL, Sidney Wolf , VEDANANDA, Thalaththani Ralalage , WAREING, James Richard
发明人： NEUBERT, Alan , BARNES, David , KWAK, Young-shin , NAKAJIMA, Katsumasa , BEBERNITZ, Gregory Raymond , COPPOLA, Gary Mark , KIRMAN, Louise , SERRANO-WU, Michael H. , STAMS, Travis , TOPIOL, Sidney Wolf , VEDANANDA, Thalaththani Ralalage , WAREING, James Richard
IPC分类号： C07D285/10 , C07D417/10 , A61P3/10 , A61K31/433
摘要： Compounds of the formula (I) 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.

3. 发明申请

WO2007067612A1 1-ORTHOFLUOROPHENYL SUBSTITUTED 1, 2 , 5-THIAZOLIDINEDIONE DERIVATIVES AS PTP-AS INHIBITORS 审中-公开
标题翻译：作为PTP-AS抑制剂取代1,2-5-羟基苯并噻唑衍生物
公开(公告)号：WO2007067612A1
公开(公告)日：2007-06-14
申请号：PCT/US2006/046542
申请日：2006-12-06
申请人： NOVARTIS AG , NOVARTIS PHARMA GmbH , BARNES, David , COPPOLA, Gary Mark , STAMS, Travis , TOPIOL, Sidney Wolf
发明人： BARNES, David , COPPOLA, Gary Mark , STAMS, Travis , TOPIOL, Sidney Wolf
IPC分类号： C07D285/10 , C07D417/10 , A61K31/433 , A61P3/10
CPC分类号： C07D417/10 , C07D285/10
摘要： Compounds of the formula (I) 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（I）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。

4. 发明申请

WO2007067614A1 l , l , 3-TRI0X0-l , 2 , 5-THIADIAZ0LIDINES AND THEIR USE AS PTP-ASES INHIBITORS 审中-公开
标题翻译： 1,3-TRI0X0-1,2,5-THIADIAZ0LININES及其作为PTP-ASES抑制剂的用途
公开(公告)号：WO2007067614A1
公开(公告)日：2007-06-14
申请号：PCT/US2006/046544
申请日：2006-12-06
申请人： NOVARTIS AG , NOVARTIS PHARMA GmbH , BARNES, David , COPPOLA, Gary Mark , DAMON, Robert Edson , NAKAJIMA, Katsumasa , RAUDENBUSH, Brian Christopher , STAMS, Travis , TOPIOL, Sidney Wolf , VEDANANDA, Thalaththani Ralalage
发明人： BARNES, David , COPPOLA, Gary Mark , DAMON, Robert Edson , NAKAJIMA, Katsumasa , RAUDENBUSH, Brian Christopher , STAMS, Travis , TOPIOL, Sidney Wolf , VEDANANDA, Thalaththani Ralalage
IPC分类号： C07D285/10 , C07D417/10 , A61K31/433 , A61K31/4439 , 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, 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

WO2007067613A1 1,2,5-THIAZOLIDINE DERIVATIVES USEFUL FOR TREATING CONDITIONS MEDIATED BY PROTEIN TYROSINE PHOSPHATASES (PTPASE) 审中-公开
标题翻译：用于处理由蛋白酪氨酸磷酸酶（PTPASE）介导的条件的1,2,5-噻唑烷衍生物
公开(公告)号：WO2007067613A1
公开(公告)日：2007-06-14
申请号：PCT/US2006/046543
申请日：2006-12-06
申请人： NOVARTIS AG , NOVARTIS PHARMA GmbH , BARNES, David , BEBERNITZ, Gregory Raymond , COPPOLA, Gary Mark , STAMS, Travis , TOPIOL, Sidney Wolf , VEDANANDA, Thalaththani Ralalage , WAREING, James Richard
发明人： BARNES, David , BEBERNITZ, Gregory Raymond , COPPOLA, Gary Mark , STAMS, Travis , TOPIOL, Sidney Wolf , VEDANANDA, Thalaththani Ralalage , WAREING, James Richard
IPC分类号： C07D285/16 , A61K31/433 , A61P3/10
CPC分类号： C07D285/16
摘要： Compounds of the formula (I) 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（I）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. 发明公开

EP1963293A1 1-ORTHOFLUOROPHENYL SUBSTITUTED 1, 2 , 5-THIAZOLIDINEDIONE DERIVATIVES AS PTP-AS INHIBITORS 审中-公开
标题翻译： 1-ORTHOFLENCHENYLSUBSTITUIERTE 1,2,5-三唑烷二异氰酸酯PTP-AS抑制剂
公开(公告)号：EP1963293A1
公开(公告)日：2008-09-03
申请号：EP06844889.3
申请日：2006-12-06
申请人： Novartis AG , Novartis Pharma GmbH
发明人： BARNES, David , COPPOLA, Gary Mark , STAMS, Travis , TOPIOL, Sidney Wolf
IPC分类号： C07D285/10 , C07D417/10 , A61K31/433 , A61P3/10
CPC分类号： C07D417/10 , C07D285/10
摘要： Compounds of the formula (I) 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.

7. 发明授权

EP1963294B1 1,2,5-THIAZOLIDINE DERIVATIVES USEFUL FOR TREATING CONDITIONS MEDIATED BY PROTEIN TYROSINE PHOSPHATASES (PTPASE) 有权
标题翻译： FOR PROTEIN BY-酪氨酸磷酸酶的治疗1,2,5-噻唑烷衍生物（PTP酶）引起的疾病
公开(公告)号：EP1963294B1
公开(公告)日：2012-10-10
申请号：EP06839092.1
申请日：2006-12-06
申请人： Novartis AG , Novartis Pharma GmbH
发明人： BARNES, David , BEBERNITZ, Gregory Raymond , COPPOLA, Gary Mark , STAMS, Travis , TOPIOL, Sidney Wolf , VEDANANDA, Thalaththani Ralalage , WAREING, James Richard
IPC分类号： C07D285/16 , A61K31/433 , A61P3/10
CPC分类号： C07D285/16

8. 发明公开

EP2038267A2 THIADIAZOLIDINONE INHIBITORS OF PTPASE 审中-公开
标题翻译：硫代二唑啉酮PTPASE抑制剂
公开(公告)号：EP2038267A2
公开(公告)日：2009-03-25
申请号：EP07780835.0
申请日：2007-03-29
申请人： NOVARTIS AG , Novartis Pharma GmbH
发明人： NEUBERT, Alan , BARNES, David , KWAK, Young-shin , NAKAJIMA, Katsumasa , BEBERNITZ, Gregory Raymond , COPPOLA, Gary Mark , KIRMAN, Louise , SERRANO-WU, Michael H. , STAMS, Travis , TOPIOL, Sidney Wolf , VEDANANDA, Thalaththani Ralalage , WAREING, James Richard
IPC分类号： C07D285/10 , A61K31/433 , C07D417/10 , A61P3/10
CPC分类号： C07D285/10 , C07D417/10
摘要： Compounds of the formula (I) 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（I）化合物是蛋白酪氨酸磷酸酶（PTP酶）的抑制剂，因此可用于治疗由PTPase活性介导的病症。本发明的化合物还可以用作以磷酸酪氨酸结合区如SH2结构域为特征的其他酶的抑制剂。因此，式（I）化合物可用于预防和/或治疗与肥胖相关的胰岛素抵抗，葡萄糖耐受不良，糖尿病，高血压和大小血管缺血性疾病，伴有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，过敏性肠综合征，胰腺炎，脂肪细胞瘤和癌脂肪肉瘤，血脂异常和其他表示胰岛素抵抗的病症。此外，本发明化合物可用于治疗和/或预防癌症，骨质疏松症，肌肉骨骼，神经退行性疾病和感染性疾病，以及涉及炎症和免疫系统的疾病。

9. 发明公开

EP1963294A1 1,2,5-THIAZOLIDINE DERIVATIVES USEFUL FOR TREATING CONDITIONS MEDIATED BY PROTEIN TYROSINE PHOSPHATASES (PTPASE) 有权
标题翻译： FOR PROTEIN BY-酪氨酸磷酸酶的治疗1,2,5-噻唑烷衍生物（PTP酶）引起的疾病
公开(公告)号：EP1963294A1
公开(公告)日：2008-09-03
申请号：EP06839092.1
申请日：2006-12-06
申请人： Novartis AG , NOVARTIS-PHARMA GMBH
发明人： BARNES, David , BEBERNITZ, Gregory Raymond , COPPOLA, Gary Mark , STAMS, Travis , TOPIOL, Sidney Wolf , VEDANANDA, Thalaththani Ralalage , WAREING, James Richard
IPC分类号： C07D285/16 , A61K31/433 , A61P3/10
CPC分类号： C07D285/16
摘要： Compounds of the formula (I) 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.

10. 发明公开

EP1960377A1 l , l , 3-TRI0X0-l , 2 , 5-THIADIAZ0LIDINES AND THEIR USE AS PTP-ASES INHIBITORS 审中-公开
标题翻译： 1,1,1-1,3-TRIOXO-1,2,5-噻二唑鎓及其作为PTP-ASES抑制剂的用途
公开(公告)号：EP1960377A1
公开(公告)日：2008-08-27
申请号：EP06839093.9
申请日：2006-12-06
申请人： Novartis AG , Novartis Pharma GmbH
发明人： BARNES, David , COPPOLA, Gary Mark , DAMON, Robert Edson , NAKAJIMA, Katsumasa , RAUDENBUSH, Brian Christopher , STAMS, Travis , TOPIOL, Sidney Wolf , VEDANANDA, Thalaththani Ralalage
IPC分类号： C07D285/10 , C07D417/10 , A61K31/433 , A61K31/4439 , 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, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.
摘要翻译：下式化合物是蛋白酪氨酸磷酸酶（PTPases）的抑制剂，因此可以用于治疗由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域如SH2结构域为特征的其他酶的抑制剂。因此，式（I）化合物可用于预防和/或治疗与肥胖症，葡萄糖耐受不良，糖尿病，高血压和大血管和小血管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，脂肪细胞肿瘤和癌症如脂肪肉瘤，血脂异常和其它表现胰岛素抵抗的病症。另外，本发明的化合物可用于治疗和/或预防癌症，骨质疏松症，神经变性和传染病以及涉及炎症和免疫系统的疾病。

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