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公开(公告)号：US08431575B2
公开(公告)日：2013-04-30
申请号：US13028036
申请日：2011-02-15
申请人： Devi R Gohimukkula , David Robert Jones , Ghassan Qabaja , Jeff J Zhu , Jeremy T Cooper , William K Banner , Kurt Sundermann , Muralidhar Bondlela , Mohan Rao , Pingzhen Wang , Suparna Gupta , Anitha Hari , Raju B Gowda , Robert C Andrews
发明人： Devi R Gohimukkula , David Robert Jones , Ghassan Qabaja , Jeff J Zhu , Jeremy T Cooper , William K Banner , Kurt Sundermann , Muralidhar Bondlela , Mohan Rao , Pingzhen Wang , Suparna Gupta , Anitha Hari , Raju B Gowda , Robert C Andrews
IPC分类号： A01N43/58 , A01N43/60 , A61K31/50 , A61K31/495
CPC分类号： C07D401/12 , A61K31/497 , C07D237/14 , C07D237/24 , C07D401/14 , C07D403/12 , C07D405/14 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/14 , C07D451/06 , C07D453/02 , C07D471/04
摘要： The present invention provides phenyl-heteroaryl derivatives of Formula (I) and pharmaceutically acceptable salts thereof These compounds are useful in the treatment of RAGE-mediated diseases such as Alzheimer's Disease. The present invention further relates to methods for the preparation of compounds of Formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising such compounds, and the use of such compounds and/or pharmaceutical compositions in treating RAGE-mediated diseases.
摘要翻译： 本发明提供式（I）的苯基 - 杂芳基衍生物及其药学上可接受的盐。这些化合物可用于治疗RAGE介导的疾病如阿尔茨海默氏病。 本发明还涉及制备式（I）的化合物及其药学上可接受的盐，包含这些化合物的药物组合物的方法，以及这些化合物和/或药物组合物在治疗RAGE介导的疾病中的用途。
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12.发明申请Substituted Azoanthracene Derivatives, Pharmaceutical Compositions, and Methods of Use Thereof 有权取代的偶氮蒽衍生物，药物组合物及其使用方法公开(公告)号：US20130096150A1
公开(公告)日：2013-04-18
申请号：US13707265
申请日：2012-12-06
发明人： Adnan M.M. Mjalli , Christopher Behme , Daniel P. Christen , Devi Reddy Gohimukkula , Dharma Rao Polisetti , James C. Quada, JR. , Jennifer L.R. Freeman , Kalpathy Santhosh , Muralidhar Bondlela , Mustafa Guzel , Ravindra Reddy Yarragunta , Robert Carl Andrews , Stephen Thomas Davis , Thomas Scott Yokum
IPC分类号： C07D491/056
CPC分类号： C07D491/056 , C07D319/20 , C07D491/06
摘要： The present invention is directed to substituted azoanthracene derivatives or pharmaceutically acceptable salts thereof that modulate the human GLP-1 receptor and that may be useful in the treatment of diseases, disorders, or conditions in which modulation of the human GLP-1 receptor is beneficial, such as diabetes mellitus type 2. The invention is also directed to pharmaceutical compositions comprising these compounds and to the use of these compounds and compositions in the treatment of such diseases, disorders, or conditions in which modulation of the human GLP-1 receptor is beneficial.
摘要翻译： 本发明涉及调节人GLP-1受体并且可用于治疗人GLP-1受体调节有益的疾病，病症或病症的取代的偶氮蒽衍生物或其药学上可接受的盐， 例如2型糖尿病。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人GLP-1受体调节有益的疾病，病症或病症中的用途 。
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13.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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14.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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15.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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公开(公告)号：US20110230529A1
公开(公告)日：2011-09-22
申请号：US12961454
申请日：2010-12-06
申请人： Anthony Murray , Jesper Lau , Lone Jeppesen , Per Vedso
发明人： Anthony Murray , Jesper Lau , Lone Jeppesen , Per Vedso
IPC分类号： A61K31/427 , A61K31/426 , A61P3/10
CPC分类号： C07D277/54 , C07D277/46 , C07D417/12 , Y02P20/582
摘要： The present invention relates to N-heteroaryl-benzamides of the formula (I), pharmaceutical compositions comprising the same, and methods of using the same. The N-heteroaryl-benzamides are useful as glucokinase activators.
摘要翻译： 本发明涉及式（I）的N-杂芳基 - 苯甲酰胺，包含其的药物组合物及其使用方法。 N-杂芳基 - 苯甲酰胺可用作葡糖激酶活化剂。
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![Crystalline forms of [3-(4- {2-butyl- 1 -[4-(4-chloro-phenoxy)-phenyl]-1H-imidazol-4-yl}-phenoxy)-propyl]-diethyl-amine](/abs-image/US/2011/02/08/US07884219B2/abs.jpg.150x150.jpg)
17.发明授权Crystalline forms of [3-(4- {2-butyl- 1 -[4-(4-chloro-phenoxy)-phenyl]-1H-imidazol-4-yl}-phenoxy)-propyl]-diethyl-amine 有权[3-（4- {2-丁基-1- [4-（4-氯 - 苯氧基） - 苯基] -1H-咪唑-4-基} - 苯氧基） - 丙基] - 二乙基胺的结晶形式公开(公告)号：US07884219B2
公开(公告)日：2011-02-08
申请号：US12046872
申请日：2008-03-12
申请人： Anitha Hari
发明人： Anitha Hari
IPC分类号： C07D209/44
CPC分类号： C07D233/60
摘要： The present invention relates to crystalline forms of [3-(4-{2-butyl-1-[4-(4-chloro-phenoxy)-phenyl]-1H-imidazol-4-yl}-phenoxy)-propyl]-diethylamine (“COMPOUND I”) useful in the treatment of RAGE mediated diseases.
摘要翻译： 本发明涉及[3-（4- {2-丁基-1- [4-（4-氯 - 苯氧基） - 苯基] -1H-咪唑-4-基} - 苯氧基） - 丙基] - 可用于治疗RAGE介导的疾病的二乙胺（“化合物I”）。
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公开(公告)号：US20100324033A1
公开(公告)日：2010-12-23
申请号：US12872580
申请日：2010-08-31
申请人： Adnan M.M. Mjalli , Dharma Rao Polisetti , Thomas Scott Yokum , Kalpathy Santhosh , Mustafa Guzel , Christopher Behme , Stephen Thomas Davis
发明人： Adnan M.M. Mjalli , Dharma Rao Polisetti , Thomas Scott Yokum , Kalpathy Santhosh , Mustafa Guzel , Christopher Behme , Stephen Thomas Davis
IPC分类号： A61K31/5383 , A61P3/10 , A61P1/12 , A61P3/04
CPC分类号： C07D498/04 , C07D498/14
摘要： The present invention provides methods of use of oxadiazoanthracene derivatives of the formula (I) and pharmaceutically acceptable salts thereof, wherein A, B, C, R, R1, R2, R3, R4 and R5 are as herein described, and wherein said methods of use include uses for the treatment and/or prevention of disorders and diseases, such as diabetes.
摘要翻译： 本发明提供使用式（I）的恶二唑衍生物及其药学上可接受的盐的方法，其中A，B，C，R，R 1，R 2，R 3，R 4和R 5如本文所述，并且其中所述方法 包括用于治疗和/或预防疾病和疾病如糖尿病的用途。
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19.发明授权公开(公告)号：US07737285B2
公开(公告)日：2010-06-15
申请号：US11800085
申请日：2007-05-03
申请人： Adnan M. M. Mjalli , Robert C. Andrews , Ramesh Gopalaswamy , Anitha Hari , Kwasi A. Avor , Ghassan Qabaja , Xiao-Chuan Guo , Suparna Gupta , David R. Jones , Xin Chen
发明人： Adnan M. M. Mjalli , Robert C. Andrews , Ramesh Gopalaswamy , Anitha Hari , Kwasi A. Avor , Ghassan Qabaja , Xiao-Chuan Guo , Suparna Gupta , David R. Jones , Xin Chen
IPC分类号： C07D233/61 , A01N43/50
CPC分类号： C07D233/64 , C07D235/08 , C07D235/12 , C07D235/14 , C07D235/18 , C07D235/30 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/12 , C07D413/12 , C07D453/02
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 modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, β-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.
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晚期糖基化终产物（RAGE）的受体与其配体如晚期糖基化终产物（AGE），S100 /钙粒蛋白/ EN-RAGE，淀粉样蛋白和 两性霉素，以及由RAGE引起的人类疾病的管理，治疗，控制或辅助治疗。 这些疾病或疾病状态包括急性和慢性炎症，糖尿病晚期并发症的发展，例如血管通透性增加，肾病，动脉粥样硬化和视网膜病变，阿尔茨海默病的发展，勃起功能障碍和肿瘤侵袭和转移。
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公开(公告)号：US07714013B2
公开(公告)日：2010-05-11
申请号：US11511163
申请日：2006-08-28
申请人： Adnan M. M. Mjalli , Robert C. Andrews , Ramesh Gopalaswamy , Anitha Hari , Kwasi A. Avor , Ghassan Qabaja , Xiao-Chuan Guo , Suparna Gupta , David R. Jones , Xin Chen
发明人： Adnan M. M. Mjalli , Robert C. Andrews , Ramesh Gopalaswamy , Anitha Hari , Kwasi A. Avor , Ghassan Qabaja , Xiao-Chuan Guo , Suparna Gupta , David R. Jones , Xin Chen
IPC分类号： A61K31/4164 , A61K31/4178 , C07D233/64 , C07D403/02
CPC分类号： C07D233/64 , C07D235/08 , C07D235/12 , C07D235/14 , C07D235/18 , C07D235/30 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/12 , C07D413/12 , C07D453/02
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 modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, β-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.
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