66737-88-0Relevant academic research and scientific papers
Novel benzofuran derivative as well as preparation method and application thereof
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Paragraph 0083; 0084, (2017/05/03)
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
Nano- and microcrystals of a Mn-based metal-oligomer framework showing size-dependent magnetic resonance behaviors
Yuan, Guozan,Zhu, Chengfeng,Liu, Yan,Cui, Yong
, p. 3180 - 3182 (2011/05/07)
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-
Isoreticular chiral metal-organic frameworks for asymmetric alkene epoxidation: Tuning catalytic activity by controlling framework catenation and varying open channel sizes
Song, Feijie,Wang, Cheng,Falkowski, Joseph M.,Ma, Liqing,Lin, Wenbin
supporting information; experimental part, p. 15390 - 15398 (2011/01/10)
A family of isoreticular chiral metal-organic frameworks (CMOFs) of the primitive cubic network topology was constructed from [Zn4(μ 4-O)(O2CR)6] secondary building units and systematically elongated dicarboxyla
BICYCLIC COMPOUNDS USEFUL AS CATHEPSIN S INBHIBITORS
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Page/Page column 38, (2010/11/29)
Compounds of formula (I), wherein R1, R2, R3, Ra and E are are defined within, and pharmaceutically acceptable salts, solvates, hydrates and N-oxides thereof having utility in the treatment of disorders mediated by cathepsin S.
Discovery, structure - Activity relationship, and pharmacological evaluation of (5-substituted-pyrrolidinyl-2-carbonyl)-2-cyanopyrrolidines as potent dipeptidyl peptidase IV inhibitors
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.
, p. 3520 - 3535 (2007/10/03)
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.
CATHEPSIN S INHIBITORS
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Page/Page column 92-93, (2010/11/08)
Compounds of the formula (I) where R1 is C1-C4 straight or branched alkyl, optionally substituted with up to three substituents selected from halo and hydroxy; R2 is halo, hydroxy, methyloxy, or C1-C2 alkyl, which alkyl is optionally substituted with up to three halogens or an hydroxy or a methyloxy; D is - C3-C7 alkylene-, thereby defining a cycloalkyl ring; E is -C(=O)-, -S(=O)m-, -NRdS(=O)m-, -NRaC(=O)-, -OC(=O)-, R3 is an optionally substituted carbocyclic or heterocyclic ring R10 is H, ORc, SRc or together with the gem H is =O or (ORc)2; Ra is independently selected from H, C1-C4 alkyl; have utility in the inhibition of cathepsin S and are thus useful pharmaceuticals against disorders such as autoimmune disorders and chronic pain.
