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1.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：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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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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5.发明授权Benzazole derivatives, compositions, and methods of use as aurora kinase inhibitors 失效苯并唑衍生物，组合物和用作极光激酶抑制剂的方法公开(公告)号：US08377983B2
公开(公告)日：2013-02-19
申请号：US12703604
申请日：2010-02-10
申请人： Adnan M. M. Mjalli , Brian S. Grella , Govindan Subramanian , Murty N. Arimilli , Ramesh Gopalaswamy , Robert C. Andrews , Stephen Davis , Xiaochuan Guo , Jeff Zhu
发明人： Adnan M. M. Mjalli , Brian S. Grella , Govindan Subramanian , Murty N. Arimilli , Ramesh Gopalaswamy , Robert C. Andrews , Stephen Davis , Xiaochuan Guo , Jeff Zhu
IPC分类号： A01N43/38 , A01N43/52 , A61K31/405 , A61K31/497 , A61K31/535 , A61K31/415 , C07D403/00 , C07D405/00 , C07D409/00 , C07D411/00
CPC分类号： C07D417/14 , C07D401/14 , C07D403/12 , C07D403/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D487/04
摘要： The present invention relates to compounds and methods from the treatment of cancer. The invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising compounds that inhibit Aurora kinase, and methods for the treatment of cancer using the compounds of the presentation invention or pharmaceutical compositions comprising compounds of the present invention.
摘要翻译： 本发明涉及治疗癌症的化合物和方法。 本发明提供抑制极光激酶的化合物，包含抑制极光激酶的化合物的药物组合物，以及使用本发明化合物或包含本发明化合物的药物组合物治疗癌症的方法。
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6.发明授权Benzazole derivatives, compositions, and methods of use as aurora kinase inhibitors 有权苯并唑衍生物，组合物和用作极光激酶抑制剂的方法公开(公告)号：US07820821B2
公开(公告)日：2010-10-26
申请号：US11704431
申请日：2007-02-09
申请人： Adnan M. M. Mjalli , Brian S. Grella , Govindan Subramanian , Murty N. Arimilli , Ramesh Gopalaswamy , Robert C. Andrews , Stephen Davis , Xiaochuan Guo , Jeff Zhu
发明人： Adnan M. M. Mjalli , Brian S. Grella , Govindan Subramanian , Murty N. Arimilli , Ramesh Gopalaswamy , Robert C. Andrews , Stephen Davis , Xiaochuan Guo , Jeff Zhu
IPC分类号： A61K31/496 , C07D401/14 , C07D403/14
CPC分类号： C07D417/14 , C07D401/14 , C07D403/12 , C07D403/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D487/04
摘要： The present invention relates to compounds and methods from the treatment of cancer. The invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising compounds that inhibit Aurora kinase, and methods for the treatment of cancer using the compounds of the presentation invention or pharmaceutical compositions comprising compounds of the present invention.
摘要翻译： 本发明涉及治疗癌症的化合物和方法。 本发明提供抑制极光激酶的化合物，包含抑制极光激酶的化合物的药物组合物，以及使用本发明化合物或包含本发明化合物的药物组合物治疗癌症的方法。
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公开(公告)号：US07820704B2
公开(公告)日：2010-10-26
申请号：US11110499
申请日：2005-04-20
申请人： Adnan M. M. Mjalli , Bapu R. Gaddam , Ghassan Qabaja , Govindan Subramanian , Jeff Zhu , John Dankwardt , Murty N. Arimilli , Robert C. Andrews , Samuel Victory , Ye E. Tian
发明人： Adnan M. M. Mjalli , Bapu R. Gaddam , Ghassan Qabaja , Govindan Subramanian , Jeff Zhu , John Dankwardt , Murty N. Arimilli , Robert C. Andrews , Samuel Victory , Ye E. Tian
IPC分类号： A61K31/427 , A61K31/381 , C07D277/38 , C07D409/12
CPC分类号： C07D277/52 , C07D239/42 , C07D277/26 , C07D277/42 , C07D277/50 , C07D277/56 , C07D277/82 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/04 , C07D417/12 , C07D417/14
摘要： The present invention provides substituted heteroaryl derivatives of Formula (I), methods of their preparation, pharmaceutical compositions comprising the compounds of Formula (I), and methods of use in treating human or animal disorders. The compounds of the invention can be useful as inhibitors of action of AgRP on a melanocortin receptor and thus can 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： 本发明提供式（I）的取代杂芳基衍生物，其制备方法，包含式（I）化合物的药物组合物，以及用于治疗人或动物病症的方法。 本发明的化合物可用作AgRP对黑皮质素受体的作用抑制剂，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的调节（包括肥胖症 - 相关疾病。
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公开(公告)号：US07763726B2
公开(公告)日：2010-07-27
申请号：US11704431
申请日：2007-02-09
申请人： Adnan M. M. Mjalli , Brian S. Grella , Govindan Subramanian , Murty N. Arimilli , Ramesh Gopalaswamy , Robert C. Andrews , Stephen Davis , Xiaochuan Guo , Jeff Zhu
发明人： Adnan M. M. Mjalli , Brian S. Grella , Govindan Subramanian , Murty N. Arimilli , Ramesh Gopalaswamy , Robert C. Andrews , Stephen Davis , Xiaochuan Guo , Jeff Zhu
IPC分类号： A61K31/496 , C07D401/14 , C07D403/14
摘要： The present invention relates to compounds and methods from the treatment of cancer. The invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising compounds that inhibit Aurora kinase, and methods for the treatment of cancer using the compounds of the presentation invention or pharmaceutical compositions comprising compounds of the present invention.
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![SUBSTITUTED IMIDAZO[1,2-A]PYRIDINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE AS BETA-SECRETASE INHIBITORS](/abs-image/US/2012/04/26/US20120101093A1/abs.jpg.150x150.jpg)
9.发明申请SUBSTITUTED IMIDAZO[1,2-A]PYRIDINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE AS BETA-SECRETASE INHIBITORS 审中-公开取代的咪唑并[1,2-A]吡啶衍生物，药物组合物和使用作为β-分泌酶抑制剂的方法公开(公告)号：US20120101093A1
公开(公告)日：2012-04-26
申请号：US13214762
申请日：2011-08-22
申请人： Adnan M. M. Mjalli , Anitha Hari , Bapu Gaddam , Devi Reddy Gohimukkula , Dharma Rao Polisetti , Hassan El Abdellaoui , Mohan Rao , Robert Carl Andrews , Rongyuan Xie , Tan Ren
发明人： Adnan M. M. Mjalli , Anitha Hari , Bapu Gaddam , Devi Reddy Gohimukkula , Dharma Rao Polisetti , Hassan El Abdellaoui , Mohan Rao , Robert Carl Andrews , Rongyuan Xie , Tan Ren
IPC分类号： A61K31/437 , A61K31/496 , A61K31/444 , A61K31/506 , A61P25/28 , A61K31/4545 , C07D471/04 , A61K31/5377
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention is directed to substituted imidazo[1,2-a]pyridine derivatives, pharmaceutically acceptable salts thereof, and tautomers of such compounds or salts, that inhibit β-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment 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 treatment of such diseases in which BACE is involved.
摘要翻译： 本发明涉及取代的咪唑并[1,2-a]吡啶衍生物，其药学上可接受的盐，以及这些化合物或盐的互变异构体，其可抑制β-淀粉样蛋白前体蛋白切割酶（BACE），并且可以是 可用于治疗涉及BACE的疾病，例如阿尔茨海默病。 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治疗涉及BACE的疾病中的用途。
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![Substituted imidazo[1,2-b]pyridazine derivatives, pharmaceutical compositions, and methods of use as β-secretase inhibitors](/abs-image/US/2013/05/28/US08450354B2/abs.jpg.150x150.jpg)
10.发明授权Substituted imidazo[1,2-b]pyridazine derivatives, pharmaceutical compositions, and methods of use as β-secretase inhibitors 失效取代的咪唑并[1,2-b]哒嗪衍生物，药物组合物和用作β-分泌酶抑制剂的方法公开(公告)号：US08450354B2
公开(公告)日：2013-05-28
申请号：US13052544
申请日：2011-03-21
申请人： Adnan M. M. Mjalli , Anitha Hari , Bapu Gaddam , Devi Reddy Gohimukkula , Dharma Rao Polisetti , Mohan Rao , Raju Bore Gowda , Robert Carl Andrews , Rongyuan Xie , Soumya P. Sahoo , Tan Ren , William Kenneth Banner
发明人： Adnan M. M. Mjalli , Anitha Hari , Bapu Gaddam , Devi Reddy Gohimukkula , Dharma Rao Polisetti , Mohan Rao , Raju Bore Gowda , Robert Carl Andrews , Rongyuan Xie , Soumya P. Sahoo , Tan Ren , William Kenneth Banner
IPC分类号： A01N43/50 , A61K31/415 , C07D403/02
CPC分类号： C07D487/04 , C07D519/00
摘要： The present invention provides substituted imidazo[1,2-b]pyridazine derivatives, pharmaceutically acceptable salts thereof, and tautomers of any of the foregoing, where such compounds inhibit β-site amyloid precursor protein-cleaving enzyme (BACE), which may be useful in the treatment of diseases in which BACE is involved, such as Alzheimer's disease. The invention also provides pharmaceutical compositions comprising any of these compounds and the use of any of these compounds and compositions in the treatment of diseases, disorders, or conditions in which BACE is involved.
摘要翻译： 本发明提供了取代的咪唑并[1,2-b]哒嗪衍生物，其药学上可接受的盐和任何前述的互变异构体，其中这些化合物抑制β-位淀粉样蛋白前体蛋白切割酶（BACE），其可能是有用的 用于治疗BACE所涉及的疾病，如阿尔茨海默病。 本发明还提供包含任何这些化合物的药物组合物以及这些化合物和组合物中任何一种用于治疗BACE所涉及的疾病，病症或病症的用途。
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