925154-93-4Relevant articles and documents
Design, synthesis and biological evaluation of spiropyrazolopyridone derivatives as potent dengue virus inhibitors
Chen, Haiying,Shi, Pei-Yong,Xie, Xuping,Xu, Jimin,Xue, Yu,Ye, Na,Zhou, Jia,Zou, Jing
, (2020/04/10)
The effective treatment for dengue virus infection continues to be a challenge. We herein reported our continued SAR exploration on the spiropyrazolopyridone scaffold. Introducing different substituents at the 3?- or 5?-site of the pyrazolopyridone core or moving the benzyl chain to the adjacent nitrogen led to a significant loss of potency on DENV-2. While a narrow range of substitutions were tolerated at the para-position of the phenyl ring, di-substitution on the phenyl ring is beneficial for DENV-2 potency and has variable influences on DENV-3 potency depending on the exact compound. Among these molecules, compounds 22 (JMX0376) with 4-chloro-3-fluorobenzyl and 24 (JMX0395) with 2,4-bis(trifluoromethyl)benzyl showed the most potent and broadest inhibitory activities against DENV-1 to ?3 with nanomolar to low micromolar EC50 values.
(PYRAZOL-3-YL)-1,3,4-THIADIAZOL-2-AMINE AND (PYRAZOL-3-YL)-1,3,4-THIAZOL-2-AMINE COMPOUNDS
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Page/Page column 26, (2012/04/23)
A compound of Formula (I) wherein: either X is N and Y is CR5 or X is C and Y is S; Z is selected from N and CH; R1 is selected from H and Me; R2 is selected from H, OH, OMe and Me; each R3 is independently selected from C1-3alkyl, F, Cl, Br, CF3 and NH2; R4 is selected from Me, CF3, NO2 and CHF2; R5 is selected from H, Me and CHF2; R6 is selected from H and Me; and p is 0-3, compositions containing them, their use in therapy, for example in the treatment of tuberculosis, and methods for the preparation of such compounds, are provided.
HETEROCYCLIC GAMMA SECRETASE MODULATORS
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Page/Page column 32, (2010/06/11)
The invention relates to methods for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome which comprise ad
Pyrazole glucokinase activators
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Page/Page column 37, (2008/06/13)
Disclosed herein are pyrazole glucokinase activators of the formula (I) useful for the treatment of metabolic diseases and disorders, preferably diabetes mellitus.