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1.发明申请Rage Antagonists As Agents To Reverse Amyloidosis And Diseases Associated Therewith 审中-公开愤怒的拮抗剂作为反应与之相关的淀粉样变性和疾病的药物公开(公告)号：US20090035302A1
公开(公告)日：2009-02-05
申请号：US12238087
申请日：2008-09-25
IPC分类号： A61K39/395 , A61K31/4164 , A61K31/4184 , A61K31/16 , A61K38/00
CPC分类号： A61K31/4164 , A61K31/4184 , A61K31/425
摘要： Disclosed are RAGE antagonist compounds that have the ability to reverse pre-existing amyloidosis. Treatment with the RAGE antagonist compounds described herein may be used to reduce plaque size and improve cognition for subjects in the later stages of Alzheimer's disease. Additionally, the RAGE antagonists described herein may be used to reduce the onset of plaque formation and thereby prevent loss of cognition and other symptoms associated with Alzheimer's Disease and other diseases of amyloid deposition.
摘要翻译： 公开了具有逆转预先存在的淀粉样变性的能力的RAGE拮抗剂化合物。 本文所述的RAGE拮抗剂化合物的治疗可用于减少斑块大小并改善阿尔茨海默病后期受试者的认知。 此外，本文所述的RAGE拮抗剂可用于减少斑块形成的发作，从而防止与阿尔茨海默病和其他淀粉样蛋白沉积疾病相关的认知和其它症状的丧失。
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公开(公告)号：US07122580B2
公开(公告)日：2006-10-17
申请号：US10637900
申请日：2003-08-08
申请人： Adnan M. M. Mjalli , Robert C. Andrews , Xiao-Chuan Guo , Daniel Peter Christen , Devi Reddy Gohimmukkula , Guoxiang Huang , Robert Rothlein , Sameer Tyagi , Tripura Yaramasu , Christopher Behme
发明人： Adnan M. M. Mjalli , Robert C. Andrews , Xiao-Chuan Guo , Daniel Peter Christen , Devi Reddy Gohimmukkula , Guoxiang Huang , Robert Rothlein , Sameer Tyagi , Tripura Yaramasu , Christopher Behme
IPC分类号： A61K31/245 , C07C233/87
CPC分类号： C07D207/267 , C07C233/29 , C07C233/87 , C07C235/42 , C07C235/52 , C07C235/60 , C07C235/66 , C07C237/36 , C07C237/42 , C07C237/44 , C07C255/60 , C07C257/18 , C07C271/20 , C07C271/44 , C07C311/18 , C07C311/19 , C07C311/44 , C07C317/14 , C07C317/28 , C07C317/36 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2603/74 , C07D207/09 , C07D211/26 , C07D213/30 , C07D213/70 , C07D213/71 , C07D213/74 , C07D213/81 , C07D217/02 , C07D217/16 , C07D217/22 , C07D231/12 , C07D231/14 , C07D231/18 , C07D233/84 , C07D239/94 , C07D249/08 , C07D261/10 , C07D263/32 , C07D271/10 , C07D277/46 , C07D285/08 , C07D295/088 , C07D295/155 , C07D307/66 , C07D307/79 , C07D307/85 , C07D317/60 , C07D333/24 , C07D333/38 , C07D333/70 , C07D401/04 , C07D409/04 , C07D409/06 , C07D413/04
摘要： This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as antagonists, or more preferably, partial antagonist of factor IX and thus, may be used to inhibit the intrinsic pathway of blood coagulation. The compounds are useful in a variety of applications including the management, treatment and/or control of diseases caused in part by the intrinsic clotting pathway utilizing factor IX. Such diseases or disease states include stroke, myocardial infarction, aneurysm surgery, and deep vein thrombosis associated with surgical procedures, long periods of confinement, and acquired or inherited pro-coagulant states.
摘要翻译： 本发明提供某些化合物，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拮抗剂，或更优选为因子IX的部分拮抗剂，因此可用于抑制血液凝固的内在途径。 该化合物可用于各种应用，包括通过利用因子IX的内在凝血途径部分引起的疾病的管理，治疗和/或控制。 这些疾病或疾病状态包括中风，心肌梗死，动脉瘤手术以及与外科手术相关的深部静脉血栓形成，长时间的约束，以及获得性或遗传的促凝血状态。
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公开(公告)号：US07544699B2
公开(公告)日：2009-06-09
申请号：US10913168
申请日：2004-08-06
申请人： Adnan M. M. Mjalli , Robert C. Andrews , Xiao-Chuan Guo , Daniel Peter Christen , Devi Reddy Gohimmukkula , Guoxiang Huang , Robert Rothlein , Sameer Tyagi , Tripura Yaramasu , Christopher Behme
发明人： Adnan M. M. Mjalli , Robert C. Andrews , Xiao-Chuan Guo , Daniel Peter Christen , Devi Reddy Gohimmukkula , Guoxiang Huang , Robert Rothlein , Sameer Tyagi , Tripura Yaramasu , Christopher Behme
IPC分类号： C07D217/00 , A61K31/47
CPC分类号： C07D295/155 , C07C233/87 , C07C235/42 , C07C235/52 , C07C235/60 , C07C235/66 , C07C237/36 , C07C237/42 , C07C271/20 , C07C311/08 , C07C311/09 , C07C311/21 , C07C311/44 , C07C317/32 , C07C323/36 , C07C2601/08
摘要： This invention provides aryl and heteroaryl compounds, 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 antagonists, or partial antagonist of factor IX and/or factor XI and thus, may be useful for inhibiting the intrinsic pathway of blood coagulation. The compounds may be useful in a variety of applications including the management, treatment and/or control of diseases caused in part by the intrinsic clotting pathway.
摘要翻译： 本发明提供芳基和杂芳基化合物，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病症中的用途。 本发明的化合物可以是拮抗剂或因子IX和/或因子XI的部分拮抗剂，因此可用于抑制凝血的内在途径。 所述化合物可用于各种应用，包括部分由内在凝血途径引起的疾病的管理，治疗和/或控制。
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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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6.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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7.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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8.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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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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