- Novel benzofuran derivative as well as preparation method and application thereof
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The invention belongs to the field of medicines, and in particular relates to a novel benzofuran derivative or a pharmaceutical salt thereof, a preparation method of the derivative, a medicinal composition containing the derivative, and application of the
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Paragraph 0085; 0086
(2017/05/03)
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- PHENOXYMETHYL DERIVATIVES
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The invention provides novel compounds having the general formula (I), wherein RA, RB, RC, RC1 and W are as defined herein, compositions including the compounds and methods of using the compounds.
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Page/Page column 147
(2017/03/21)
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- NOVEL PHENOL DERIVATIVE
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Disclosed are a novel compound and a pharmaceutical product, each having a remarkable uricosuric effect. Specifically disclosed are: a novel phenol derivative represented by general formula (1) that is shown in FIG. 1; a pharmaceutically acceptable salt t
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Page/Page column 13
(2012/07/28)
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- Nano- and microcrystals of a Mn-based metal-oligomer framework showing size-dependent magnetic resonance behaviors
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A robust 3D Mn-based metal-organic framework containing metallosalen hexamers is synthesized and its nano- and microcrystals are fabricated by using surfactant-mediated hydrothermal and solvent precipitation methods; the particles exhibit an inverse size-
- Yuan, Guozan,Zhu, Chengfeng,Liu, Yan,Cui, Yong
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scheme or table
p. 3180 - 3182
(2011/05/07)
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- 2-ARYLTHIAZOLE DERIVATIVES AS CXCR3 RECEPTOR MODULATORS
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The invention encompasses compounds of Formula I or pharmaceutically acceptable salts thereof, which are modulators of the CXCR3 chemokine receptor function useful for the treatment or prevention of pathogenic inflammatory processes, autoimmune diseases or graft rejection processes. Methods of use and pharmaceutical compositions are also encompassed.
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Page/Page column 58
(2010/11/28)
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- Discovery, structure - Activity relationship, and pharmacological evaluation of (5-substituted-pyrrolidinyl-2-carbonyl)-2-cyanopyrrolidines as potent dipeptidyl peptidase IV inhibitors
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A series of (5-substituted pyrrolidinyl-2-carbonyl)-2-cyanopyrrolidine (C5-Pro-Pro) analogues was discovered as dipeptidyl peptidase IV (DPPIV) inhibitors as a potential treatment of diabetes and obesity. X-ray crystallography data show that these inhibitors bind to the catalytic site of DPPIV with the cyano group forming a covalent bond with the serine residue of DPPIV. The C5-substituents make various interactions with the enzyme and affect potency, chemical stability, selectivity, and PK properties of the inhibitors. Optimized analogues are extremely potent with subnanomolar Ki's, are chemically stable, show very little potency decrease in the presence of plasma, and exhibit more than 1,000-fold selectivity against related peptidases. The best compounds also possess good PK and are efficacious in lowering blood glucose in an oral glucose tolerance test in ZDF rats.
- Pei, Zhonghua,Li, Xiaofeng,Longenecker, Kenton,Von Geldern, Thomas W.,Wiedeman, Paul E.,Lubben, Thomas H.,Zinker, Bradley A.,Stewart, Kent,Ballaron, Stephen J.,Stashko, Michael A.,Mika, Amanda K.,Beno, David W. A.,Long, Michelle,Wells, Heidi,Kempf-Grote, Anita J.,Madar, David J.,McDermott, Todd S.,Bhagavatula, Lakshmi,Fickes, Michael G.,Pireh, Daisy,Solomon, Larry R.,Lake, Marc R.,Edalji, Rohinton,Fry, Elizabeth H.,Sham, Hing L.,Trevillyan, James M.
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p. 3520 - 3535
(2007/10/03)
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- New enzymes and prodrugs for ADEPT
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The present invention relates to nucleic acid molecules encoding mutant human carboxypeptidase A enzymes, and encoding conjugates of targeting molecules and mutant human carboxypeptidase A enzymes. The invention further relates to vectors and cell lines containing such nucleic acid molecules.
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