G protein coupled receptor agonist and application thereof in treatment of diabetes
The invention discloses a structure of a compound. The structural formula of the compound is shown in the description. Found by activity determination, the structure has the effect of a G protein coupled receptor 119 agonist; the G protein coupled receptor 119 agonist has the functions of not causing hypoglycemia of patients and promoting GLP-1 secretion. The compound disclosed by the invention can be further researched and developed as a diabetes-resisting drug. Besides, the invention further discloses a synthesis route and a synthesis method for the compound.
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Paragraph 0016
(2018/06/16)
Identification of a novel class of succinyl-nitrile-based Cathepsin S inhibitors
The synthesis and in vitro activities of a series of succinyl-nitrile-based inhibitors of Cathepsin S are described. Several members of this class show nanomolar inhibition of the target enzyme as well as cellular potency. The inhibitors displaying the greatest potency contain N-alkyl substituted piperidine and pyrrolidine rings spiro-fused to the α-carbon of the P1 residue.
Bekkali, Younes,Thomson, David S.,Betageri, Raj,Emmanuel, Michel J.,Hao, Ming-Hong,Hickey, Eugene,Liu, Weimin,Patel, Usha,Ward, Yancey D.,Young, Erick R.R.,Nelson, Richard,Kukulka, Alison,Brown, Maryanne L.,Crane, Kathy,White, Della,Freeman, Dorothy M.,Labadia, Mark E.,Wildeson, Jessi,Spero, Denice M.
p. 2465 - 2469
(2008/03/11)
A reversible cysteines protease aminonitrile effective as a new
Disclosed are novel nitrile compounds of formula (I) further defined herein, which compounds are useful as reversible inhibitors of cysteine proteases such as cathepsin K, S, F, L and B. These compounds are useful for treating diseases and pathological co
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Page/Page column 91-92
(2008/06/13)
Antiallergic cosmetic or pharmaceutical composition
The invention relates to the use of cucurbitine or extracts of Cucurbitaceae pips for the preparation of a cosmetic or pharmaceutical, in particular dermatological, composition having antiallergic activity, or for the preparation of cosmetic or pharmaceutical compositions having a reduced risk of being allergenic.
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(2008/06/13)
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