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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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公开(公告)号：US20110230458A1
公开(公告)日：2011-09-22
申请号：US13028036
申请日：2011-02-15
申请人： Devi R. Gohimukkula , David Jones , Ghassan Qabaja , Jeff J. Zhu , Jeremy T. Cooper , William K. Banner , Kurt Sundermann , Muralidhar Bondlela , Mohan Rao , Pingzhen Wang , Raju B. Gowda , Robert C. Andrews , Suparna Gupta , Anitha Hari
发明人： Devi R. Gohimukkula , David Jones , Ghassan Qabaja , Jeff J. Zhu , Jeremy T. Cooper , William K. Banner , Kurt Sundermann , Muralidhar Bondlela , Mohan Rao , Pingzhen Wang , Raju B. Gowda , Robert C. Andrews , Suparna Gupta , Anitha Hari
IPC分类号： A61K31/397 , C07D401/12 , A61K31/501 , C07D413/12 , A61K31/5377 , C07D401/14 , C07D413/14 , A61P29/00 , A61P17/00 , A61P11/00 , A61P3/10 , A61P13/12 , A61P9/00 , A61P25/00 , A61P15/10 , A61P19/10 , A61P35/04
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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3.发明申请Azole derivatives and fused bicyclic azole derivatives as therapeutic agents 审中-公开唑衍生物和稠合双环唑衍生物作为治疗剂公开(公告)号：US20100256119A1
公开(公告)日：2010-10-07
申请号：US12799971
申请日：2010-05-05
申请人： Adnan M.M. Mjalli , Robert C. Andrews , Ramesh Gopalaswamy , Anitha Hari , Kwasi S. 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 S. Avor , Ghassan Qabaja , Xiao-Chuan Guo , Suparna Gupta , David R. Jones , Xin Chen
IPC分类号： A61K31/55 , A61K31/496 , A61K31/4184 , A61K31/454 , A61K31/439 , A61K31/5377 , A61K31/4545 , A61K31/4439 , A61K31/4164 , A61K31/422 , A61K31/4178 , A61K31/4709 , A61P11/00 , A61P11/06 , A61P27/02 , A61P9/10 , A61P29/00 , A61P17/00
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, nephrdpathy, 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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4.发明申请AZOLE DERIVATIVES AND FUSED BICYCLIC AZOLE DERIVATIVES AS THERAPEUTIC AGENTS 审中-公开作为治疗剂的偶氮衍生物和融合的双相氨基衍生物公开(公告)号：US20120088778A1
公开(公告)日：2012-04-12
申请号：US13270208
申请日：2011-10-10
申请人： Adnan M.M. Mjalli , Robert C. Andrews , Ramesh Gopalaswamy , Anitha Hari , Kwasi S. 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 S. Avor , Ghassan Qabaja , Xiao-Chuan Guo , Suparna Gupta , David R. Jones , Xin Chen
IPC分类号： A61K31/496 , A61K31/4725 , A61P27/02 , A61P9/10 , A61K31/4178 , A61K31/422 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4164
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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5.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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7.发明授权公开(公告)号：US07361678B2
公开(公告)日：2008-04-22
申请号：US10382203
申请日：2003-03-05
申请人： Adnan M. M. Mjalli , Robert C. Andrews , Ramesh Gopalaswamy , Anitha Hari , Kwasi S. 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 S. 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.
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，β-淀粉样蛋白和两性蛋白之间相互作用的调节剂 ，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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8.发明申请公开(公告)号：US20070021386A1
公开(公告)日：2007-01-25
申请号：US11511163
申请日：2006-08-28
申请人： Adnan Mjalli , Robert Andrews , Ramesh Gopalaswamy , Anitha Hari , Kwasi Avor , Ghassan Qabaja , Xiao-Chuan Guo , Suparna Gupta , David Jones , Xin Chen
发明人： Adnan Mjalli , Robert Andrews , Ramesh Gopalaswamy , Anitha Hari , Kwasi Avor , Ghassan Qabaja , Xiao-Chuan Guo , Suparna Gupta , David Jones , Xin Chen
IPC分类号： A61K31/695 , A61K31/4172
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，β-淀粉样蛋白和两性蛋白之间相互作用的调节剂 ，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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9.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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10.发明申请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：US20100056587A1
公开(公告)日：2010-03-04
申请号：US12547018
申请日：2009-08-25
IPC分类号： A61K31/427 , C07D409/12 , C07D409/14
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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