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1.发明申请Substituted Fused Imidazole Derivatives, Pharmaceutical Compositions, and Methods of Use Thereof 有权取代的熔融咪唑衍生物，药物组合物及其使用方法公开(公告)号：US20110201604A1
公开(公告)日：2011-08-18
申请号：US13028406
申请日：2011-02-16
申请人： Adnan M. M. Mjalli , Dharma Rao Polisetti , Jareer Nabeel Kassis , Matthew J. Kostura , Mustafa Guzel , Otis Clinton Attucks , Robert Carl Andrews , Samuel Victory , Suparna Gupta
发明人： Adnan M. M. Mjalli , Dharma Rao Polisetti , Jareer Nabeel Kassis , Matthew J. Kostura , Mustafa Guzel , Otis Clinton Attucks , Robert Carl Andrews , Samuel Victory , Suparna Gupta
IPC分类号： A61K31/428 , C07D417/12 , C07D417/14 , A61K31/5377 , C07D471/04 , A61K31/437 , A61K31/454 , A61K31/496 , A61K31/541 , A61K31/506 , A61P11/00 , A61P1/16 , A61P31/12 , A61P17/06 , A61P17/00 , A61P25/28 , A61P25/16 , A61P9/12 , A61P9/00 , A61P7/02 , A61P29/00 , A61P11/06 , A61P13/12 , A61P27/02 , A61P3/10 , A61P3/04 , A61P35/00
CPC分类号： C07D417/12 , A61K31/4168 , A61K31/4188 , A61K31/428 , A61K31/437 , C07D235/30 , C07D417/14 , C07D471/04 , C07D513/04
摘要： Substituted fused imidazole derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted fused imidazole derivative, and methods of use in treating inflammation are provided. The substituted fused imidazole derivatives may control the activity or the amount or both the activity and the amount of heme-oxygenase.
摘要翻译： 提供取代的稠合咪唑衍生物，其制备方法，包含取代的稠合咪唑衍生物的药物组合物和用于治疗炎症的方法。 取代的稠合咪唑衍生物可以控制血红素氧合酶的活性或活性和量的量。
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2.发明授权Substituted fused imidazole derivatives, pharmaceutical compositions, and methods of use thereof 有权取代的稠合咪唑衍生物，药物组合物及其使用方法公开(公告)号：US08759535B2
公开(公告)日：2014-06-24
申请号：US13028406
申请日：2011-02-16
申请人： Adnan M. M. Mjalli , Dharma Rao Polisetti , Jareer Nabeel Kassis , Matthew J. Kostura , Mustafa Guzel , Otis Clinton Attucks , Robert Carl Andrews , Samuel Victory , Suparna Gupta
发明人： Adnan M. M. Mjalli , Dharma Rao Polisetti , Jareer Nabeel Kassis , Matthew J. Kostura , Mustafa Guzel , Otis Clinton Attucks , Robert Carl Andrews , Samuel Victory , Suparna Gupta
IPC分类号： C07D417/12 , C07D235/30 , C07D513/04 , A61K31/437 , A61K31/428 , A61K31/4188 , A61K31/4168
CPC分类号： C07D417/12 , A61K31/4168 , A61K31/4188 , A61K31/428 , A61K31/437 , C07D235/30 , C07D417/14 , C07D471/04 , C07D513/04
摘要： Substituted fused imidazole derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted fused imidazole derivative, and methods of use in treating inflammation are provided. The substituted fused imidazole derivatives may control the activity or the amount or both the activity and the amount of heme-oxygenase.
摘要翻译： 提供取代的稠合咪唑衍生物，其制备方法，包含取代的稠合咪唑衍生物的药物组合物和用于治疗炎症的方法。 取代的稠合咪唑衍生物可以控制血红素氧合酶的活性或活性和量的量。
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3.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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4.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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5.发明申请SUBSTITUTED THIAZOL-2-YLAMINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE AS 11-BETA HSD1 MODULATORS 失效取代的噻唑-2-基胺衍生物，药物组合物和使用11-BETA HSD1调节剂的方法公开(公告)号：US20120029029A1
公开(公告)日：2012-02-02
申请号：US13189640
申请日：2011-07-25
IPC分类号： A61K31/4439 , C07D417/12 , C07D277/56 , A61P27/02 , A61K31/427 , A61P3/00 , A61P3/10 , A61P3/06 , A61P3/04 , A61P9/12 , A61P9/00 , A61P9/10 , A61P19/10 , A61P21/00 , A61P25/28 , A61P25/18 , A61K31/426
CPC分类号： C07D277/56 , C07D417/12
摘要： The present invention is directed to substituted thiazol-2-ylamine derivatives and pharmaceutically acceptable salts thereof that inhibit 11βHSD1 and that may be useful in the treatment of diseases in which modulation or inhibition of 11βHSD1 is beneficial or where a reduction in intracellular glucorticoid levels is desirable. 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, disorders, or conditions in which modulation or inhibition of 11βHSD1 is beneficial or where a reduction in intracellular glucorticoid levels is desirable.
摘要翻译： 本发明涉及取代的噻唑-2-基胺衍生物及其药学上可接受的盐，其抑制11β和HSD1，并且其可用于治疗其中调节或抑制11β和HSD1有益的疾病或细胞内减少的疾病 糖皮质激素水平是理想的。 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其中调节或抑制11β和HSD1有益或其中细胞内糖皮质激素水平降低的疾病，病症或病症的用途 合意。
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公开(公告)号：US20110224244A1
公开(公告)日：2011-09-15
申请号：US13128045
申请日：2009-11-17
IPC分类号： A61K31/505 , C07D239/28 , A61K31/44 , C07D211/98 , C07D237/14 , A61K31/50 , C07D211/94 , C07D211/96 , A61P27/02 , A61P27/06
CPC分类号： A61K31/44 , C07D213/643 , C07D213/70 , C07D213/71 , C07D213/74 , C07D237/14 , C07D239/42
摘要： Embodiments of the present invention provide adamantyl benzamide derivtives and pharmaceutical compositions comprising adamantyl benzamide derivatives. Methods of use of such compounds and compositions to modulate the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) in a subject are also provided.
摘要翻译： 本发明的实施方案提供金刚烷基苯甲酰胺衍生物和包含金刚烷基苯甲酰胺衍生物的药物组合物。 还提供了使用这些化合物和组合物来调节受试者中11＆bgr-羟基类固醇脱氢酶1（11＆bgr; HSD1）的活性的方法。
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公开(公告)号：US08927549B2
公开(公告)日：2015-01-06
申请号：US13128045
申请日：2009-11-17
IPC分类号： C07D213/89 , A61K31/44 , C07D237/12 , A61K31/50 , C07D239/42 , A61K31/505 , A61P9/12 , A61P9/00 , A61P3/10 , A61P3/04
CPC分类号： A61K31/44 , C07D213/643 , C07D213/70 , C07D213/71 , C07D213/74 , C07D237/14 , C07D239/42
摘要： Embodiments of the present invention provide adamantyl benzamide derivatives and pharmaceutical compositions comprising adamantyl benzamide derivatives. Methods of use of such compounds and compositions to modulate the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) in a subject are also provided.
摘要翻译： 本发明的实施方案提供金刚烷基苯甲酰胺衍生物和包含金刚烷基苯甲酰胺衍生物的药物组合物。 还提供了使用这些化合物和组合物来调节受试者中11＆bgr-羟基类固醇脱氢酶1（11＆bgr; HSD1）的活性的方法。
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8.发明授权Substituted thiazol-2-ylamine derivatives, pharmaceutical compositions, and methods of use as 11-beta HSD1 modulators 失效取代的噻唑-2-基胺衍生物，药物组合物和用作11-βHSD1调节剂的方法公开(公告)号：US08513430B2
公开(公告)日：2013-08-20
申请号：US13189640
申请日：2011-07-25
IPC分类号： A61K31/426 , A61K31/427 , A61K31/4439 , C07D277/42 , C07D417/12
CPC分类号： C07D277/56 , C07D417/12
摘要： The present invention is directed to substituted thiazol-2-ylamine derivatives and pharmaceutically acceptable salts thereof that inhibit 11βHSD1 and that may be useful in the treatment of diseases in which modulation or inhibition of 11βHSD1 is beneficial or where a reduction in intracellular glucorticoid levels is desirable. 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, disorders, or conditions in which modulation or inhibition of 11βHSD1 is beneficial or where a reduction in intracellular glucorticoid levels is desirable.
摘要翻译： 本发明涉及抑制11betaHSD1的取代的噻唑-2-基胺衍生物及其药学上可接受的盐，其可用于治疗其中11betaHSD1的调节或抑制是有益的或者其中需要减少细胞内糖皮质激素水平的疾病 。 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其中调节或抑制11bβHSD1有益或其中期望细胞内糖皮质激素水平降低的疾病，病症或病症的用途。
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9.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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