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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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62.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：US07901688B2
公开(公告)日：2011-03-08
申请号：US11197038
申请日：2005-08-03
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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64.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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65.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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公开(公告)号：US07022730B2
公开(公告)日：2006-04-04
申请号：US10273795
申请日：2002-10-18
IPC分类号： A61K31/404 , C07D403/14 , C07D405/14
CPC分类号： C07D405/14 , C07D209/08 , C07D209/10
摘要： This invention provides compounds which are useful as inhibitors of protein tyrosine phosphatases (PTPases). As inhibitors of PTPases the compounds of the invention are useful for the management, treatment, control and adjunct treatment of diseases in mammals mediated by PTPase activity. Such diseases include type I diabetes, type II diabetes, immune dysfunction, AIDS, autoimmunity, glucose intolerance, obesity, cancer, psoriasis, allergic diseases, infectious diseases, inflammatory diseases, diseases involving the modulated synthesis of growth hormone or the modulated synthesis of growth factors or cytokines which affect the production of growth hormone, or Alzheimer's disease.
摘要翻译： 本发明提供可用作蛋白酪氨酸磷酸酶（PTPases）抑制剂的化合物。 作为PTPase的抑制剂，本发明的化合物可用于由PTPase活性介导的哺乳动物疾病的管理，治疗，控制和辅助治疗。 这些疾病包括I型糖尿病，II型糖尿病，免疫功能障碍，AIDS，自身免疫，葡萄糖不耐受，肥胖症，癌症，牛皮癣，过敏性疾病，感染性疾病，炎症性疾病，涉及调节生长激素合成的疾病或生长调节合成 影响生长激素或阿尔茨海默病生产的因子或细胞因子。
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67.发明授权Method for synthesis of &agr;-sulfonamido amide, carboxylic acid and hydroxamic acid derivatives 失效α-亚磺酰氨基酰胺，羧酸和异羟肟酸衍生物的合成方法公开(公告)号：US06583318B2
公开(公告)日：2003-06-24
申请号：US10146713
申请日：2002-05-15
申请人： Eugene Campian , Boliang Lou , Adnan M. M. Mjalli
发明人： Eugene Campian , Boliang Lou , Adnan M. M. Mjalli
IPC分类号： C07C30300
CPC分类号： C07C303/40 , C07C311/19 , C07C311/29
摘要： A method of synthesizing &agr;-sulfonamido amide, carboxylic acid or hydroxamic acid derivatives comprising providing a set of polymer-bound reactant(s) (sulfonamide, aldehyde or ketone, isocyanide or acid) to react with three sets of the other three reactants to form an array of polymer-bound &agr;-sulfonamido amide-type intermediates and use of such intermediates for the preparation of combinatorial libraries.
摘要翻译： 一种合成α-亚磺酰氨基酰胺，羧酸或异羟肟酸衍生物的方法，包括提供一组聚合物结合的反应物（磺酰胺，醛或酮，异氰化物或酸）与三组其他三种反应物反应形成 聚合物结合的α-亚磺酰氨基酰胺型中间体阵列以及这种中间体用于制备组合文库的用途。
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公开(公告)号：US06117940A
公开(公告)日：2000-09-12
申请号：US174521
申请日：1998-10-16
申请人： Adnan M. M. Mjalli
发明人： Adnan M. M. Mjalli
IPC分类号： C07D233/54 , C07D241/18 , C07D243/14 , C07D403/04 , C07D405/04 , C07D471/04 , C07D487/04 , C07D487/14 , C08F8/30 , C08F283/00 , C08F290/06 , C08G65/333 , C08G63/48 , C08K5/07 , G01N33/00
CPC分类号： C07D233/64 , C07D241/18 , C07D243/14 , C07D403/04 , C07D405/04 , C07D471/04 , C07D487/04 , C07D487/14 , C08F283/00 , C08F290/06 , C08F290/065 , C08G65/33317 , Y10T436/173845 , Y10T436/200833
摘要： A solid support template for solid phase synthesis of amino group containing compounds is provided that comprises amino-ketone core compounds of the general formula:A-L-NH(CR.sub.1 R.sub.2).sub.n COR.sub.3linked to appropriate insoluble substrates to create solid support templates having the general formula:Polymer-X-L-NH(CR.sub.1 R.sub.2).sub.n COR.sub.3where L is a multifunctional monomer carrying a first functional group that forms a covalent bond with X and a second functional group comprising an amine and L, R.sub.1, R.sub.2 and R.sub.3 are selected from the group consisting of alkyl, alkyl-aryl, alkenyl, alkenyl-aryl groups having up to 6 carbon atoms and substituted forms thereof. The amino-ketone templates are useful for the solid phase synthesis of compounds such as the imidazoles, benzodiazepines, pyrazines, and steroid mimics.
摘要翻译： 提供了用于固相合成含氨基化合物的固体支持模板，其包含通式AL-NH（CR1R2）nCOR3的氨基酮核心化合物，其连接到合适的不溶性底物以产生具有以下通式的固体支持模板：聚合物 - XL-NH（CR1R2）nCOR3其中L是携带与X形成共价键的第一官能团的多官能单体和包含胺的第二官能团，L，R 1，R 2和R 3选自烷基，烷基 具有至多6个碳原子的芳基，烯基，链烯基 - 芳基及其取代形式。 氨基酮模板可用于化合物如咪唑，苯并二氮杂，吡嗪和类固醇模拟物的固相合成。
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69.发明授权
公开(公告)号：US6107274A
公开(公告)日：2000-08-22
申请号：US270121
申请日：1999-03-15
申请人： Adnan M. M. Mjalli , James Christopher Mason , Kristen Lee Arienti , Kevin Michael Short , Rachel Denise Anne Kimmich , Todd Kevin Jones
发明人： Adnan M. M. Mjalli , James Christopher Mason , Kristen Lee Arienti , Kevin Michael Short , Rachel Denise Anne Kimmich , Todd Kevin Jones
IPC分类号： C07D241/08 , A61K31/495 , A61K31/4985 , A61K38/00 , A61K38/12 , A61P3/10 , A61P43/00 , C07D471/04 , C07K5/078 , C07K5/12
CPC分类号： C07D241/08 , C07D471/04 , C07K5/06139 , A61K38/00
摘要： Compounds of formula A are disclosed: ##STR1## wherein R.sup.1 is aralkyl or cycloalkyl; R.sup.2 is cycloalkylmethyl, alkyl, or aralkyl;R.sup.3 is hydrogen, alkyl, substituted phenyl (including p-phenoxy-phenyl), or fluorene;R.sup.4 is hydrogen, alkyl, substituted phenyls (including 1-alkyl-4-carboxy-substituted phenyls), alkyl carboxylic acids;R.sup.5 is hydrogen or R.sup.1 and R.sup.5 taken together forming a tetrahydroisoquinoline ring or a piperidine ring.These compounds exhibit inhibitory action against fructose-1,6-bisphosphatase (FBPase) and are indicated in the treatment or management of Type II diabetes.
摘要翻译： 公开了式A的化合物：其中R 1是芳烷基或环烷基; R2是环烷基甲基，烷基或芳烷基; R3是氢，烷基，取代的苯基（包括对苯氧基 - 苯基）或芴; R4是氢，烷基，取代的苯基（包括1-烷基-4-羧基取代的苯基），烷基羧酸; R5是氢或R1和R5一起形成四氢异喹啉环或哌啶环。 这些化合物对果糖-1,6-二磷酸酶（FBPase）表现出抑制作用，并在II型糖尿病的治疗或治疗中表现出。
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公开(公告)号：US5723451A
公开(公告)日：1998-03-03
申请号：US694998
申请日：1996-08-09
IPC分类号： A61K31/495 , A61K31/496
CPC分类号： A61K31/495 , A61K31/496
摘要： There are disclosed methods useful for the inhibition of inducible nitric oxide synthase by the adminstration of a compound of the Formula I: ##STR1## to a patient in need of such inhibition such as hypotension, inflammation, autoimmune diseases and septic shock and the like.
摘要翻译： 公开了通过给予需要这种抑制的患者例如低血压，炎症，自身免疫性疾病和败血性休克等的式I化合物：IMA图像抑制诱导型一氧化氮合酶的方法。
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