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31.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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32.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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33.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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34.发明授权Tricyclic compounds as modulators of TNF-α synthesis and as PDE4 inhibitors 有权三环化合物作为TNF-α合成的调节剂和PDE4抑制剂公开(公告)号：US08853226B2
公开(公告)日：2014-10-07
申请号：US13040382
申请日：2011-03-04
IPC分类号： A61K31/519 , C07D471/04
CPC分类号： A61K31/519 , C07D471/04 , Y02A50/411
摘要： The present invention relates to chemical compounds of Formula (I) are as herein defined, pharmaceutical compositions, and methods of use in the treatment of conditions or disorders mediated by TNF-α or by PDE4, including but not limited to rheumatoid arthritis.
摘要翻译： 本发明涉及式（I）的化合物如本文所定义，药物组合物和用于治疗由TNF-α或PDE4介导的病症或病症的方法，包括但不限于类风湿性关节炎。
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35.发明申请Tricyclic Compounds as Modulators of TNF-alpha Synthesis and as PDE4 Inhibitors 有权三环化合物作为TNF-α合成的调节剂和PDE4抑制剂公开(公告)号：US20120172381A1
公开(公告)日：2012-07-05
申请号：US13410628
申请日：2012-03-02
IPC分类号： A61K31/519 , A61P11/06
CPC分类号： A61K31/519 , C07D471/04 , Y02A50/411
摘要： The present invention relates to chemical compounds of Formula (I) are as herein defined, pharmaceutical compositions, and methods of use in the treatment of conditions or disorders mediated by TNF-α or by PDE4, including but not limited to rheumatoid arthritis.
摘要翻译： 本发明涉及式（I）的化合物如本文所定义，药物组合物和用于治疗由TNF-α或PDE4介导的病症或病症的方法，包括但不限于类风湿性关节炎。
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公开(公告)号：US07906507B2
公开(公告)日：2011-03-15
申请号：US12849225
申请日：2010-08-03
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： C07D498/02 , A61K31/5365
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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公开(公告)号：US07067554B2
公开(公告)日：2006-06-27
申请号：US10611741
申请日：2003-07-01
申请人： Adnan M. M. Mjalli , Ramesh Gopalaswamy , Kwasi A. Avor , Christopher L. Wysong , Patron Andrew
发明人： Adnan M. M. Mjalli , Ramesh Gopalaswamy , Kwasi A. Avor , Christopher L. Wysong , Patron Andrew
IPC分类号： A61K31/21 , C07C233/00
CPC分类号： C07C311/19 , A61K31/16 , C07C237/20 , C07C237/22 , C07C271/22 , C07C275/24 , C07C279/14 , C07C311/06 , C07D307/42 , Y10S977/915
摘要： This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, 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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公开(公告)号：US06930200B2
公开(公告)日：2005-08-16
申请号：US10607234
申请日：2003-06-26
申请人： Adnan M. M. Mjalli
发明人： Adnan M. M. Mjalli
IPC分类号： C07B43/00 , C07B51/00 , C07B61/00 , C07C227/18 , C07C229/08 , C07C229/34 , C07C229/36 , C07C229/48 , C07C231/12 , C07C237/04 , C07C237/14 , C07C237/20 , C07C237/24 , C07C271/22 , C07D207/16 , C07D211/60 , C07D211/62 , C07D211/66 , C07D213/56 , C07D303/48 , C07D309/14 , C07D317/72 , C07D333/38 , C07D335/02 , C07F7/18 , C07C229/02 , C07D211/40 , C07D407/08 , C07D409/08
CPC分类号： C07D317/72 , C07C229/08 , C07C229/36 , C07C229/48 , C07C271/22 , C07C2601/08 , C07C2601/14 , C07C2603/18 , C07D207/16 , C07D211/60 , C07D211/66 , C07D213/56 , C07D309/14 , C07D333/38 , C07D335/02
摘要： Mono-substituted and di-substituted alpha-amino acids and derivatives thereof, substituted at the alpha positon with one (mono-) or two (di-) substituents (R2 and/or R3) as shown in Formula 1: N(R4R5)C(R2R3)CO(OR1).
摘要翻译： 在α位置上用一个（单）或两（二）取代基取代的单取代和二取代的α-氨基酸及其衍生物（R 2 O 2和/或R 2） 3）如式1所示：N（R 4，R 5）C（R 2 R 3） CO（OR 1））。
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公开(公告)号：US06294539B1
公开(公告)日：2001-09-25
申请号：US09487528
申请日：2000-01-19
申请人： Boliang Lou , Adnan M. M. Mjalli
发明人： Boliang Lou , Adnan M. M. Mjalli
IPC分类号： A61K31495
CPC分类号： C07D241/08 , C07D241/04
摘要： Novel compositions comprising heterocyclic hydroxamic acid derivatives of the general formula: These compounds are useful in the treatment of diseases and conditions in which matrix metalloproteinases are involved, such as cancer, arthritis, tumor metastasis and multiple sclerosis (MS).
摘要翻译： 包含以下通式的杂环异羟肟酸衍生物的新型组合物：这些化合物可用于治疗涉及基质金属蛋白酶的疾病和病症，例如癌症，关节炎，肿瘤转移和多发性硬化（MS）。
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40.发明授权Use of metformin in combination with a glucokinase activator and compositions comprising metformin and a glucokinase activator 有权二甲双胍与葡萄糖激酶活化剂和包含二甲双胍和葡糖激酶活化剂的组合物的组合使用公开(公告)号：US09359313B2
公开(公告)日：2016-06-07
申请号：US13114964
申请日：2011-05-24
IPC分类号： A61K31/425 , A61K31/155 , C07D277/54
CPC分类号： A61K31/426 , A61K31/155 , C07D277/54
摘要： The present invention provides uses of a glucokinase activator in combination with metformin. Uses include treating type 2 diabetes, lowering blood glucose, improving insulin sensitivity, enhancing phosphorylation of glucose, and improving the therapeutic effectiveness of metformin. The invention also provides pharmaceutical compositions that comprise a GK activator and metformin. The invention also provides a salt formed between metformin and a GK activator.
摘要翻译： 本发明提供葡糖激酶活化剂与二甲双胍组合的用途。 用途包括治疗2型糖尿病，降低血糖，改善胰岛素敏感性，增强葡萄糖磷酸化，提高二甲双胍的治疗效果。 本发明还提供包含GK活化剂和二甲双胍的药物组合物。 本发明还提供了在二甲双胍和GK活化剂之间形成的盐。
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