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    Organic compounds
    2.
    发明授权
    Organic compounds 失效
    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。

    1,2,5-Thiazolidine Derivatives Useful for Treating Conditions Mediated by Protein Tyrosine Phosphatases (Ptpase)
    3.
    发明申请
    1,2,5-Thiazolidine Derivatives Useful for Treating Conditions Mediated by Protein Tyrosine Phosphatases (Ptpase) 有权
    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。

    1,2,5-thiazolidine derivatives useful for treating conditions mediated by protein tyrosine phosphatases (PTPase)
    4.
    发明授权
    1,2,5-thiazolidine derivatives useful for treating conditions mediated by protein tyrosine phosphatases (PTPase) 有权
    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。

    Organic Compounds
    6.
    发明申请
    Organic Compounds 失效
    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。

    Organic Compounds
    7.
    发明申请
    Organic Compounds 审中-公开
    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。

    5-substituted 1,1-dioxo-1,2,5,-thiadiazolidin-3-one derivatives
    8.
    发明授权
    5-substituted 1,1-dioxo-1,2,5,-thiadiazolidin-3-one derivatives 有权
    5-取代的1,1-二氧代-1,2,5-噻二唑烷-3-酮衍生物

    公开(公告)号：US07291635B2

    公开(公告)日：2007-11-06

    申请号：US10510026

    申请日：2003-04-02

    申请人： Gary Mark Coppola ,  John William Davies ,  Charles Francis Jewell, Jr. ,  Yu-Chin Li ,  James Richard Wareing ,  Donald Mark Sperbeck ,  Travis Mathew Stams ,  Sidney Wolf Topiol ,  Isidoros Vlattas

    发明人： Gary Mark Coppola ,  John William Davies ,  Charles Francis Jewell, Jr. ,  Yu-Chin Li ,  James Richard Wareing ,  Donald Mark Sperbeck ,  Travis Mathew Stams ,  Sidney Wolf Topiol ,  Isidoros Vlattas

    IPC分类号： A61K31/433 ,  C07D285/10

    CPC分类号： C07D285/10 ,  C07D417/06 ,  C07D417/10 ,  C07K5/06078

    摘要： Compounds of the formula provide pharmacological agents which are inhibitors of PTPases, in particular, the compounds of formula I inhibit PTP-1B and TC PTP, and thus may be employed for the treatment of conditions associated with PTPase activity. The compounds of the present invention may also be employed for inhibition of other enzymes with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula I may be employed for prevention or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels. The compounds of the present invention may also be employed in the treatment, prevention or control of a number of 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 or prevent cancer, osteoporosis, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.

    摘要翻译： 式的化合物提供作为PTPase抑制剂的药理学试剂，特别是式I化合物抑制PTP-1B和TC PTP，因此可用于治疗与PTPase活性相关的病症。 本发明的化合物也可用于抑制具有磷酸酪氨酸结合区的其它酶，例如SH2结构域。 因此，式I化合物可用于预防或治疗与肥胖，葡萄糖不耐受，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。 本发明的化合物还可用于治疗，预防或控制伴随2型糖尿病的多种病症，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，脂肪细胞瘤和癌。 作为脂肪肉瘤，血脂异常和其他指示胰岛素抵抗的疾病。 此外，本发明的化合物可用于治疗或预防癌症，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-Substituted 1,1-Dioxo- 1,2,5- Thiadiazolidin-3-One Derivatives
    9.
    发明申请
    5-Substituted 1,1-Dioxo- 1,2,5- Thiadiazolidin-3-One Derivatives 审中-公开
    5-取代的1,1-二氧-1,2,5-噻二唑烷-3-酮衍生物

    公开(公告)号：US20080139576A1

    公开(公告)日：2008-06-12

    申请号：US11860034

    申请日：2007-09-24

    申请人： Gary Mark Coppola ,  John William Davies ,  Charles Francis Jewell ,  Yu-Chin Li ,  James Richard Wareing ,  Donald Mark Sperbeck ,  Travis Matthew Stams ,  Sidney Wolf Topiol ,  Isidoros Vlattas

    发明人： Gary Mark Coppola ,  John William Davies ,  Charles Francis Jewell ,  Yu-Chin Li ,  James Richard Wareing ,  Donald Mark Sperbeck ,  Travis Matthew Stams ,  Sidney Wolf Topiol ,  Isidoros Vlattas

    IPC分类号： A61K31/497 ,  C07D285/10 ,  C07D403/02 ,  A61K31/47 ,  A61P3/00 ,  C07D215/00 ,  A61K31/41

    CPC分类号： C07D285/10 ,  C07D417/06 ,  C07D417/10 ,  C07K5/06078

    摘要： Compounds of the formula provide pharmacological agents which are inhibitors of PTPases, in particular, the compounds of formula I inhibit PTP-1B and TC PTP, and thus may be employed for the treatment of conditions associated with PTPase activity. The compounds of the present invention may also be employed for inhibition of other enzymes with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula I may be employed for prevention or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels. The compounds of the present invention may also be employed in the treatment, prevention or control of a number of 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 or prevent cancer, osteoporosis, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.

    摘要翻译： 式的化合物提供作为PTPase抑制剂的药理学试剂，特别是式I化合物抑制PTP-1B和TC PTP，因此可用于治疗与PTPase活性相关的病症。 本发明的化合物也可用于抑制具有磷酸酪氨酸结合区的其它酶，例如SH2结构域。 因此，式I化合物可用于预防或治疗与肥胖，葡萄糖不耐受，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。 本发明的化合物还可用于治疗，预防或控制伴随2型糖尿病的多种病症，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，脂肪细胞瘤和癌。 作为脂肪肉瘤，血脂异常和其他指示胰岛素抵抗的疾病。 此外，本发明的化合物可用于治疗或预防癌症，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。