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公开(公告)号：US06933303B2
公开(公告)日：2005-08-23
申请号：US10274546
申请日：2002-10-18
IPC分类号： A61K31/437 , A61K31/573 , A61K31/64 , A61K38/28 , A61K45/00 , A61P3/00 , A61P3/04 , A61P3/08 , A61P3/10 , A61P5/10 , A61P17/06 , A61P25/28 , A61P29/00 , A61P31/00 , A61P31/04 , A61P31/18 , A61P35/00 , A61P37/04 , A61P37/06 , A61P37/08 , A61P43/00 , C07D471/04
CPC分类号： C07D471/04
摘要： This invention provides compounds which are useful as inhibitors of protein tyrosine phosphatases (PTPases). As inhibitors of PTPases, the compounds of the invention are useful for the management, treatment, control and adjunct treatment of diseases mediated by PTPase activity. Such diseases include type I diabetes, type II diabetes, immune dysfunction, AIDS, autoimmunity, glucose intolerance, obesity, cancer, psoriasis, allergic diseases, infectious diseases, inflammatory diseases, diseases involving the modulated synthesis of growth hormone or the modulated synthesis of growth factors or cytokines which affect the production of growth hormone, or Alzheimer's disease.
摘要翻译： 本发明提供可用作蛋白酪氨酸磷酸酶（PTPases）抑制剂的化合物。 作为PTPase的抑制剂，本发明的化合物可用于由PTPase活性介导的疾病的治疗，治疗，控制和辅助治疗。 这些疾病包括I型糖尿病，II型糖尿病，免疫功能障碍，AIDS，自身免疫，葡萄糖不耐受，肥胖症，癌症，牛皮癣，过敏性疾病，感染性疾病，炎症性疾病，涉及调节生长激素合成的疾病或生长调节合成 影响生长激素或阿尔茨海默病生产的因子或细胞因子。
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公开(公告)号：US20110077399A1
公开(公告)日：2011-03-31
申请号：US12958237
申请日：2010-12-01
申请人： Adnan M. M. Mjalli , Robert C. Andrews , Ravindra R. Yarragunta , Rongyuan Xie , Govindan Subramanian , James C. Quada, JR. , Murty N. Arimilli , Dharma R. Polisetti
发明人： Adnan M. M. Mjalli , Robert C. Andrews , Ravindra R. Yarragunta , Rongyuan Xie , Govindan Subramanian , James C. Quada, JR. , Murty N. Arimilli , Dharma R. Polisetti
IPC分类号： C07D413/04 , C07D233/64 , C07D405/10 , C07D401/04
CPC分类号： C07D417/12 , C07D233/54 , C07D263/32 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/10 , C07D403/12 , C07D405/10 , C07D405/12 , C07D413/04
摘要： This invention provides azoles which may be useful as inhibitors of protein tyrosine phosphatases (PTPases). The present invention provides compounds of Formula (I), methods of their preparation, pharmaceutical compositions comprising the compounds and their use in treating human or animal disorders. The compounds of the invention may be useful as inhibitors of protein tyrosine phosphatases and thus can be useful for the management, treatment, control and adjunct treatment of diseases mediated by PTPase activity. Such diseases include Type I diabetes, Type II diabetes.
摘要翻译： 本发明提供可用作蛋白酪氨酸磷酸酶（PTPases）的抑制剂的唑类。 本发明提供式（I）化合物，其制备方法，包含该化合物的药物组合物及其在治疗人或动物疾病中的用途。 本发明的化合物可用作蛋白酪氨酸磷酸酶的抑制剂，因此可用于由PTPase活性介导的疾病的管理，治疗，控制和辅助治疗。 这些疾病包括I型糖尿病，II型糖尿病。
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3.发明授权Substituted imidazole derivatives, compositions, and methods of use as PTPase inhibitors 有权取代的咪唑衍生物，组合物和作为PTPase抑制剂的方法公开(公告)号：US07723369B2
公开(公告)日：2010-05-25
申请号：US11699780
申请日：2007-01-30
申请人： Adnan M. M. Mjalli , Dharma R. Polisetti , Govindan Subramanian , James C. Quada , Ravindra R. Yarragunta , Robert C. Andrews , Rongyuan Xie
发明人： Adnan M. M. Mjalli , Dharma R. Polisetti , Govindan Subramanian , James C. Quada , Ravindra R. Yarragunta , Robert C. Andrews , Rongyuan Xie
IPC分类号： A61K31/4178 , C07D233/64
CPC分类号： C07D417/14 , C07D417/10
摘要： The present invention provides imidazole derivatives of Formula (I-IV), methods of their preparation, pharmaceutical compositions comprising the compounds of Formula (I-IV), and their use in treating human or animal disorders. The compounds of the invention inhibit protein tyrosine phosphatase 1B and thus can be useful for the management, treatment, control, or the adjunct treatment of diseases mediated by PTPase activity. Such diseases include Type I diabetes and Type II diabetes.
摘要翻译： 本发明提供式（I-IV）的咪唑衍生物，其制备方法，包含式（I-IV）化合物的药物组合物及其在治疗人或动物疾病中的用途。 本发明的化合物抑制蛋白酪氨酸磷酸酶1B，因此可用于对由PTPase活性介导的疾病的治疗，治疗，控制或辅助治疗。 这些疾病包括I型糖尿病和II型糖尿病。
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4.发明授权Substituted imidazole derivatives, compositions, and methods of use as PTPase inhibitors 有权取代的咪唑衍生物，组合物和作为PTPase抑制剂的方法公开(公告)号：US08404731B2
公开(公告)日：2013-03-26
申请号：US12685178
申请日：2010-01-11
申请人： Adnan M. M. Mjalli , Dharma R. Polisetti , Govindan Subramanian , James C. Quada , Ravindra R. Yarragunta , Robert C. Andrews , Rongyuan Xie
发明人： Adnan M. M. Mjalli , Dharma R. Polisetti , Govindan Subramanian , James C. Quada , Ravindra R. Yarragunta , Robert C. Andrews , Rongyuan Xie
IPC分类号： A61K31/4178 , C07D233/64
CPC分类号： C07D417/14 , C07D417/10
摘要： The present invention provides imidazole derivatives of Formula (I-IV), methods of their preparation, pharmaceutical compositions comprising the compounds of Formula (I-IV), and their use in treating human or animal disorders. The compounds of the invention inhibit protein tyrosine phosphatase 1B and thus can be useful for the management, treatment, control, or the adjunct treatment of diseases mediated by PTPase activity. Such diseases include Type I diabetes and Type II diabetes.
摘要翻译： 本发明提供式（I-IV）的咪唑衍生物，其制备方法，包含式（I-IV）化合物的药物组合物及其在治疗人或动物疾病中的用途。 本发明的化合物抑制蛋白酪氨酸磷酸酶1B，因此可用于对由PTPase活性介导的疾病的治疗，治疗，控制或辅助治疗。 这些疾病包括I型糖尿病和II型糖尿病。
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公开(公告)号：US20110092553A1
公开(公告)日：2011-04-21
申请号：US12950967
申请日：2010-11-19
申请人： Adnan M.M. Mjalli , Dharma R. Polisetti , Govindan Subramanian , James C. Quada, JR. , Murty N. Arimilli , Ravindra R. Yarragunta , Robert C. Andrews , Rongyuan Xie
发明人： Adnan M.M. Mjalli , Dharma R. Polisetti , Govindan Subramanian , James C. Quada, JR. , Murty N. Arimilli , Ravindra R. Yarragunta , Robert C. Andrews , Rongyuan Xie
IPC分类号： A61K31/433 , C07D233/64 , C07D403/10 , C07D285/06 , A61K31/4164 , A61K31/4178 , A61K31/417 , A61P3/10 , A61P35/00 , A61P3/04 , A61P37/00
CPC分类号： C07D233/64 , C07D401/12 , C07D403/10 , C07D409/10 , C07D413/10 , C07D417/10 , C07D417/14
摘要： The present invention provides azole derivatives of Formula (I), methods of their preparation, pharmaceutical compositions comprising the compounds of Formula (I), and their use in treating human or animal disorders. The compounds of the invention can be useful as inhibitors of protein tyrosine phosphatases and thus can be useful for the management, treatment, control, or the adjunct treatment of diseases mediated by PTPase activity. Such diseases include Type I diabetes and Type II diabetes.
摘要翻译： 本发明提供式（I）的唑衍生物，其制备方法，包含式（I）化合物的药物组合物及其在治疗人或动物疾病中的用途。 本发明的化合物可用作蛋白酪氨酸磷酸酶的抑制剂，因此可用于由PTPase活性介导的疾病的治疗，治疗，控制或辅助治疗。 这些疾病包括I型糖尿病和II型糖尿病。
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6.发明申请Substituted Imidazole Derivatives, Compositions, and Methods of Use as PTPase Inhibitors 审中-公开替代咪唑衍生物，组合物和作为PTPase抑制剂的方法公开(公告)号：US20120196906A1
公开(公告)日：2012-08-02
申请号：US13412747
申请日：2012-03-06
申请人： Adnan M.M. Mjalli , Dharma R. Polisetti , Govindan Subramanian , James C. Quada , Ravindra R. Yarragunta , Robert C. Andrews , Rongyuan Xie
发明人： Adnan M.M. Mjalli , Dharma R. Polisetti , Govindan Subramanian , James C. Quada , Ravindra R. Yarragunta , Robert C. Andrews , Rongyuan Xie
IPC分类号： A61K31/433 , A61P3/10 , A61P31/18 , A61P37/08 , A61P25/28 , A61P17/06 , A61P31/00 , A61P3/04 , A61P35/00 , C07D417/10 , A61P29/00
CPC分类号： C07D417/14 , C07D417/10
摘要： The present invention provides imidazole derivatives of Formula (I-IV), methods of their preparation, pharmaceutical compositions comprising the compounds of Formula (I-IV), and their use in treating human or animal disorders. The compounds of the invention inhibit protein tyrosine phosphatase 1B and thus can be useful for the management, treatment, control, or the adjunct treatment of diseases mediated by PTPase activity. Such diseases include Type I diabetes and Type II diabetes.
摘要翻译： 本发明提供式（I-IV）的咪唑衍生物，其制备方法，包含式（I-IV）化合物的药物组合物及其在治疗人或动物疾病中的用途。 本发明的化合物抑制蛋白酪氨酸磷酸酶1B，因此可用于对由PTPase活性介导的疾病的治疗，治疗，控制或辅助治疗。 这些疾病包括I型糖尿病和II型糖尿病。
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7.发明授权Benzazole derivatives, compositions, and methods of use as β-secretase inhibitors 有权苯并唑衍生物，组合物和作为分泌酶抑制剂的方法公开(公告)号：US07893267B2
公开(公告)日：2011-02-22
申请号：US11885096
申请日：2006-03-14
申请人： Adnan M. M. Mjalli , David Jones , Devi Reddy Gohimmukkula , Guoxiang Huang , Jeff Zhu , Mohan Rao , Robert C. Andrews , Tan Ren
发明人： Adnan M. M. Mjalli , David Jones , Devi Reddy Gohimmukkula , Guoxiang Huang , Jeff Zhu , Mohan Rao , Robert C. Andrews , Tan Ren
IPC分类号： C07D217/12 , A61K31/47
CPC分类号： C07D401/14 , A61K31/4725 , C07D235/30 , C07D401/04 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/14 , C07D407/14 , C07D409/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D473/00 , C07D491/04 , C07D495/04 , C07D513/04
摘要： The present invention is directed to benzazole compounds that inhibit β-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment or prevention of diseases in which BACE is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which BACE is involved.
摘要翻译： 本发明涉及抑制β-淀粉样蛋白前体蛋白切割酶（BACE）的苯扎唑化合物，其可用于治疗或预防BACE所涉及的疾病如阿尔茨海默氏病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及BACE的疾病中的用途。
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8.发明授权Benzazole derivatives, compositions, and methods of use as β-secretase inhibitors 失效苯并唑衍生物，组合物和用作β-分泌酶抑制剂的方法公开(公告)号：US08598353B2
公开(公告)日：2013-12-03
申请号：US12950718
申请日：2010-11-19
申请人： Adnan M. M. Mjalli , David R. Jones , Devi Reddy Gohimukkula , Guoxiang Huang , Jeff J. Zhu , Mohan Rao , Robert C. Andrews , Tan Ren
发明人： Adnan M. M. Mjalli , David R. Jones , Devi Reddy Gohimukkula , Guoxiang Huang , Jeff J. Zhu , Mohan Rao , Robert C. Andrews , Tan Ren
IPC分类号： C07D401/12 , A61K31/4725
CPC分类号： C07D401/14 , A61K31/4725 , C07D235/30 , C07D401/04 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/14 , C07D407/14 , C07D409/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D473/00 , C07D491/04 , C07D495/04 , C07D513/04
摘要： The present invention is directed to benzazole compounds that inhibit β-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment or prevention of diseases in which BACE is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which BACE is involved.
摘要翻译： 本发明涉及抑制β-位淀粉样蛋白前体蛋白切割酶（BACE）的苯并唑化合物，其可用于治疗或预防BACE所涉及的疾病如阿尔茨海默氏病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及BACE的疾病中的用途。
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9.发明授权Bissulfonamide compounds as agonists of GalR1, compositions, and methods of use 失效作为GalR1的激动剂的双磺酰胺化合物，组合物和使用方法公开(公告)号：US07582673B2
公开(公告)日：2009-09-01
申请号：US11255000
申请日：2005-10-20
申请人： Adnan M. M. Mjalli , Bapu Gaddam , Mohan Rao , Muralidhar Bondlela , Ramesh Gopalaswamy , Robert C. Andrews , Stephen Davis , Suvi Simila , Tan Ren
发明人： Adnan M. M. Mjalli , Bapu Gaddam , Mohan Rao , Muralidhar Bondlela , Ramesh Gopalaswamy , Robert C. Andrews , Stephen Davis , Suvi Simila , Tan Ren
IPC分类号： A61K31/381 , A61K31/18 , C07D333/66 , C07C311/21
CPC分类号： C07D213/42 , C07C311/29 , C07D233/54 , C07D307/82 , C07D333/34 , C07D333/62 , C07D409/12 , C07D413/04 , C07D413/12 , C07D495/04
摘要： Embodiments of the present invention provide bissulfonamide compounds that are agonists of GalR1. The present invention further provides compositions comprising bissulfonamide compounds that are agonists of GalR1, and methods of use of such compounds and compositions.
摘要翻译： 本发明的实施方案提供作为GalR1的激动剂的双磺酰胺化合物。 本发明还提供了包含作为GalR1的激动剂的双磺酰胺化合物的组合物，以及这些化合物和组合物的使用方法。
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10.发明授权Substituted aminothiazole derivatives, pharmaceutical compositions, and methods of use 失效取代的氨基噻唑衍生物，药物组合物和使用方法公开(公告)号：US08563742B2
公开(公告)日：2013-10-22
申请号：US12547018
申请日：2009-08-25
IPC分类号： A61K31/427 , C07D417/12
CPC分类号： C07D417/14 , A61K31/425 , C07D417/12
摘要： Substituted aminothiazole derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted aminothiazole, and methods of use in treating human or animal disorders. The compounds may be useful as inhibitors of action of AgRP on a melanocortin receptor and thus may be useful for the management, treatment, control, or the adjunct treatment of diseases which may be responsive to the modulation of melanocortin receptors including obesity-related disorders.
摘要翻译： 取代的氨基噻唑衍生物，其制备方法，包含取代的氨基噻唑的药物组合物，以及用于治疗人或动物疾病的方法。 该化合物可用作AgRP对黑皮质素受体的作用的抑制剂，因此可用于治疗，治疗，控制或辅助治疗可能对黑皮质素受体（包括肥胖相关病症）的调节有反应的疾病。
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