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51.发明授权Aryl acrylic acid derivatives useful as protein tyrosine phosphatase inhibitors 失效用作蛋白酪氨酸磷酸酶抑制剂的芳基丙烯酸衍生物
公开(公告)号：US5770620A
公开(公告)日：1998-06-23
申请号：US543630
申请日：1995-10-16
IPC分类号： A61K38/00 , C07C59/52 , C07C59/84 , C07C59/88 , C07C69/732 , C07C69/738 , C07C69/92 , C07C235/12 , C07C235/34 , C07C235/78 , C07C235/80 , C07C237/22 , C07C323/60 , C07D209/26 , C07D233/54 , C07D233/90 , C07D241/42 , C07D263/34 , C07D277/30 , C07D307/54 , C07D307/71 , C07D317/60 , C07D401/04 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07K5/06 , C07K5/062 , C07K5/065 , C07K5/083 , A61K31/405 , C07D209/18
CPC分类号： C07D233/64 , C07C235/12 , C07C235/34 , C07C235/78 , C07C235/80 , C07C237/22 , C07C323/60 , C07C59/52 , C07C59/84 , C07C59/88 , C07C69/732 , C07C69/738 , C07C69/92 , C07D209/26 , C07D233/90 , C07D241/42 , C07D263/34 , C07D277/30 , C07D307/54 , C07D307/71 , C07D317/60 , C07D401/04 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07K5/06017 , C07K5/06034 , C07K5/06078 , C07K5/06191 , C07K5/0806 , A61K38/00 , C07C2101/14
摘要： The present invention provides novel protein tyrosine phosphatase modulating compounds having an aryl acrylic acid structure, compositions comprising the compounds, and methods of making and using the same.
摘要翻译： 本发明提供具有芳基丙烯酸结构的新型蛋白质酪氨酸磷酸酶调节化合物，包含该化合物的组合物及其制备和使用方法。
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公开(公告)号：US08877192B2
公开(公告)日：2014-11-04
申请号：US12983604
申请日：2011-01-03
IPC分类号： A61K38/00 , C07K14/705
CPC分类号： C07K14/705 , A61K38/00
摘要： Disclosed are RAGE fusion proteins comprising RAGE polypeptide sequences linked to a second, non-RAGE polypeptide. The RAGE fusion protein may utilize a RAGE polypeptide domain comprising a RAGE ligand binding site and an interdomain linker directly linked to an immunoglobulin CH2 domain. Such fusion proteins may provide specific, high affinity binding to RAGE ligands. Also disclosed is the use of the RAGE fusion proteins as therapeutics for RAGE-mediated pathologies.
摘要翻译： 公开了包含与第二非RAGE多肽连接的RAGE多肽序列的RAGE融合蛋白。 RAGE融合蛋白可以利用包含RAGE配体结合位点和直接连接到免疫球蛋白CH2结构域的域间连接体的RAGE多肽结构域。 这样的融合蛋白可以提供与RAGE配体的特异的高亲和力结合。 还公开了RAGE融合蛋白作为RAGE介导的病理学的治疗剂的用途。
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53.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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公开(公告)号：US08524708B2
公开(公告)日：2013-09-03
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： 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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55.发明授权公开(公告)号：US08383644B2
公开(公告)日：2013-02-26
申请号：US12825631
申请日：2010-06-29
申请人： Adnan M. M. Mjalli , Christopher Behme , Daniel P. Christen , Devi Reddy Gohimukkula , Dharma Rao Polisetti , James Quada , Jennifer L. R. Freeman , Kalpathy Santhosh , Muralidhar Bondlela , Mustafa Guzel , Ravindra Reddy Yarragunta , Robert Carl Andrews , Stephen Thomas Davis , Thomas Scott Yokum
发明人： Adnan M. M. Mjalli , Christopher Behme , Daniel P. Christen , Devi Reddy Gohimukkula , Dharma Rao Polisetti , James Quada , 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 , A61K31/436
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.
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56.发明授权Substituted isoquinoline derivatives, pharmaceutical compositions, and methods of use as beta-secretase inhibitors 失效取代的异喹啉衍生物，药物组合物和用作β-分泌酶抑制剂的方法公开(公告)号：US08350039B2
公开(公告)日：2013-01-08
申请号：US13214434
申请日：2011-08-22
申请人： Adnan M. M. Mjalli , Bapu Gaddam , Devi Reddy Gohimukkula , Dharma Rao Polisetti , Hassan El Abdellaoui , Mohan Rao , Pingzhen Wang , Robert Carl Andrews , Rongyuan Xie , Tan Ren
发明人： Adnan M. M. Mjalli , Bapu Gaddam , Devi Reddy Gohimukkula , Dharma Rao Polisetti , Hassan El Abdellaoui , Mohan Rao , Pingzhen Wang , Robert Carl Andrews , Rongyuan Xie , Tan Ren
IPC分类号： C07D217/26 , A61K31/472 , A61K31/4725 , A61P25/28
CPC分类号： C07D401/12 , C07D401/14
摘要： The present invention is directed to substituted isoquinoline derivatives, pharmaceutically acceptable salts thereof, and tautomers of such compounds or salts, that inhibit β-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment 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 treatment of such diseases in which BACE is involved.
摘要翻译： 本发明涉及取代的异喹啉衍生物，其药学上可接受的盐，以及此类化合物或盐的互变异构体，其可抑制β-淀粉样蛋白前体蛋白切割酶（BACE），并可用于治疗疾病，其中 BACE参与，如阿尔茨海默病。 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涉及BACE的疾病中的用途。
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57.发明申请SUBSTITUTED ISOQUINOLINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE AS BETA-SECRETASE INHIBITORS 失效取代的异喹啉衍生物，药物组合物和使用作为β-分泌酶抑制剂的方法公开(公告)号：US20120101125A1
公开(公告)日：2012-04-26
申请号：US13214434
申请日：2011-08-22
申请人： Adnan M. M. Mjalli , Bapu Gaddam , Devi Reddy Gohimukkula , Dharma Rao Polisetti , Hassan El Abdellaoui , Mohan Rao , Pingzhen Wang , Robert Carl Andrews , Rongyuan Xie , Tan Ren
发明人： Adnan M. M. Mjalli , Bapu Gaddam , Devi Reddy Gohimukkula , Dharma Rao Polisetti , Hassan El Abdellaoui , Mohan Rao , Pingzhen Wang , Robert Carl Andrews , Rongyuan Xie , Tan Ren
IPC分类号： A61K31/472 , A61K31/4725 , A61P25/28 , C07D217/26
CPC分类号： C07D401/12 , C07D401/14
摘要： The present invention is directed to substituted isoquinoline derivatives, pharmaceutically acceptable salts thereof, and tautomers of such compounds or salts, that inhibit β-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment 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 treatment of such diseases in which BACE is involved.
摘要翻译： 本发明涉及取代的异喹啉衍生物，其药学上可接受的盐，以及这些化合物或盐的互变异构体，其可抑制β-淀粉样蛋白前体蛋白切割酶（BACE），并可用于治疗疾病，其中 BACE参与，如阿尔茨海默病。 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涉及BACE的疾病中的用途。
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58.发明授权N-heteroaryl indole carboxamides and analogues thereof, for use as glucokinase activators in the treatment of diabetes 有权N-杂芳基吲哚羧酰胺及其类似物，用作糖尿病治疗中的葡糖激酶活化剂公开(公告)号：US08148413B2
公开(公告)日：2012-04-03
申请号：US12895761
申请日：2010-09-30
申请人： Jesper Lau , Per Vedsø , János Tibor Kodra , Anthony Murray , Lone Jeppesen , Michael Ankersen , Govindan Subramanian , Adnan M. M. Mjalli , Robert Carl Andrews , Dharma Rao Polisetti , Daniel Peter Christen
发明人： Jesper Lau , Per Vedsø , János Tibor Kodra , Anthony Murray , Lone Jeppesen , Michael Ankersen , Govindan Subramanian , Adnan M. M. Mjalli , Robert Carl Andrews , Dharma Rao Polisetti , Daniel Peter Christen
IPC分类号： A61K31/427 , C07D417/12
CPC分类号： C07D401/12 , C07D403/12 , C07D417/12 , C07D491/04
摘要： This invention relates to compounds that are activators of glucokinase and thus may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial. The compounds are of the general formula (I) wherein A and B are further defined in the application.
摘要翻译： 本发明涉及作为葡萄糖激酶活化剂的化合物，因此可用于治疗，治疗，控制或辅助治疗疾病，其中增加葡糖激酶活性是有益的。 所述化合物具有通式（I），其中A和B在本申请中进一步定义。
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公开(公告)号：US07964608B2
公开(公告)日：2011-06-21
申请号：US12532861
申请日：2009-01-23
IPC分类号： A01N43/54 , A61K31/505 , C07D239/70 , C07D471/00
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-alpha 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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60.发明申请N-HETEROARYL INDOLE CARBOXAMIDES AND ANALOGUES THEREOF, FOR USE AS GLUCOKINASE ACTIVATORS IN THE TREATMENT OF DIABETES 有权N-羟基吲哚类化合物及其类似物，用作治疗糖尿病的糖尿病激活剂公开(公告)号：US20110082144A1
公开(公告)日：2011-04-07
申请号：US12895761
申请日：2010-09-30
申请人： Jesper F. Lau , Per Vedsø , János Tibor Kodra , Anthony Murray , Lone Jeppesen , Michael Ankersen , Govindan Subramanian , Adnan M. M. Mjalli , Robert Carl Andrews , Dharma Rao Polisetti , Daniel Peter Christen
发明人： Jesper F. Lau , Per Vedsø , János Tibor Kodra , Anthony Murray , Lone Jeppesen , Michael Ankersen , Govindan Subramanian , Adnan M. M. Mjalli , Robert Carl Andrews , Dharma Rao Polisetti , Daniel Peter Christen
IPC分类号： A61K31/5377 , C07D403/12 , A61K31/427 , C07D471/04 , A61K31/437 , C07D403/14 , A61K31/506 , C07D401/14 , A61K31/4439 , C07D413/14 , A61P3/10
CPC分类号： C07D401/12 , C07D403/12 , C07D417/12 , C07D491/04
摘要： This invention relates to compounds that are activators of glucokinase and thus may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial. The compounds are of the general formula (I) wherein A and B are further defined in the application.
摘要翻译： 本发明涉及作为葡萄糖激酶活化剂的化合物，因此可用于治疗，治疗，控制或辅助治疗疾病，其中增加葡糖激酶活性是有益的。 所述化合物具有通式（I），其中A和B在本申请中进一步定义。
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