155826-26-9Relevant articles and documents
PYRAZOLO[1,5-A]PYRIMIDINE DERIVATIVES HAVING MULTIMODAL ACTIVITY AGAINST PAIN
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Page/Page column 213; 215-216, (2021/12/08)
The present invention relates to pyrazolopyrimidine derivatives having dual pharmacological activity towards both the α2δ subunit of the voltage-gated calcium channel and the sigma-1 (σ1) receptor, to processes of preparation of such compounds,
HETEROCYCLIC COMPOUND INTERMEDIATE, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
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Paragraph 0523; 0527-0528, (2021/10/07)
Disclosed by the invention is a heterocyclic compound, an intermediate, and a preparation method therefor and an application thereof. Provided by the invention are a heterocyclic compound as shown in formula I, and a stereoisomer, a geometric isomer, a tautomer, a nitrogen oxide, a hydrate, a solvate, a metabolite, an ester, a pharmaceutically acceptable salt or a prodrug thereof. The heterocyclic compound hasa high P2X3 antagonistic activity, and has good selectivity, low toxicity, good metabolic stability and little taste influence.
Reaction Mechanism in Ionic Liquids: Kinetics and Mechanism of the Aminolysis of 4-Nitrophenyl Acetate
Pavez, Paulina,Millán, Daniela,Rojas, Mabel,Morales, Javiera I.,Santos, José G.
, p. 337 - 343 (2016/05/02)
In this work, we report a kinetic study of the reactions of the title compound with secondary alicyclic amines at different temperatures in acetonitrile and several ionic liquids (ILs). From this study, we have described that the reactions in MeCN and in
Novel spiroketal pyrrolidine GSK2336805 potently inhibits key hepatitis C virus genotype 1b mutants: From lead to clinical compound
Kazmierski, Wieslaw M.,Maynard, Andrew,Duan, Maosheng,Baskaran, Sam,Botyanszki, Janos,Crosby, Renae,Dickerson, Scott,Tallant, Matthew,Grimes, Rick,Hamatake, Robert,Leivers, Martin,Roberts, Christopher D.,Walker, Jill
, p. 2058 - 2073 (2014/04/03)
Rapid clinical progress of hepatitis C virus (HCV) replication inhibitors, including these selecting for resistance in the NS5A region (NS5A inhibitors), promises to revolutionize HCV treatment. Herein, we describe our explorations of diverse spiropyrrolidine motifs in novel NS5A inhibitors and a proposed interaction model. We discovered that the 1,4-dioxa-7-azaspiro[4.4]nonane motif in inhibitor 41H (GSK2236805) supported high potency against genotypes 1a and 1b as well as in genotype 1b L31V and Y93H mutants. Consistent with this, 41H potently suppressed HCV RNA in the 20-day RNA reduction assay. Pharmacokinetic and safety data supported further progression of 41H to the clinic.