31924-81-9Relevant articles and documents
COMPOSITIONS AND METHODS FOR SUBSTITUTED 7-(PIPERAZIN-1-YL)PYRAZOLO[1,5-A]PYRIMIDINE ANALOGS AS INHIBITORS OF KRAS
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, (2021/06/22)
In one aspect, the disclosure relates to compounds useful as inhibitors of mutant KRAS proteins, methods of making the same, pharmaceutical compositions comprising the same, and methods of treating cancers associated with mutated forms of KRAS using the same. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.
APELIN RECEPTOR AGONISTS AND METHODS OF USE THEREOF
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, (2019/02/25)
Provided herein are agonists of the apelin receptor for the treatment of disease. The compounds disclosed herein are useful for the treatment of a range of cardiovascular, renal and metabolic conditions.
N -Acetyl-3-aminopyrazoles block the non-canonical NF-kB cascade by selectively inhibiting NIK
Pippione, Agnese C.,Sainas, Stefano,Federico, Antonella,Lupino, Elisa,Piccinini, Marco,Kubbutat, Michael,Contreras, Jean-Marie,Morice, Christophe,Barge, Alessandro,Ducime, Alex,Boschi, Donatella,Al-Karadaghi, Salam,Lolli, Marco L.
, p. 963 - 968 (2018/06/27)
NF-κB-inducing kinase (NIK), an oncogenic drug target that is associated with various cancers, is a central signalling component of the non-canonical pathway. A blind screening process, which established that amino pyrazole related scaffolds have an effect on IKKbeta, led to a hit-to-lead optimization process that identified the aminopyrazole 3a as a low μM selective NIK inhibitor. Compound 3a effectively inhibited the NIK-dependent activation of the NF-κB pathway in tumour cells, confirming its selective inhibitory profile.
Structure and tautomerism of 4-substituted 3(5)-aminopyrazoles in solution and in the solid state: NMR study and Ab initio calculations
Emelina,Petrov,Filyukov
, p. 412 - 421 (2014/06/09)
Annular tautomerism of 3(5)-aminopyrazoles containing a cyano, thiocyanato, or aryl substituent in the 4-position has been studied by 1H and 13C NMR in solution, cross-polarization and magic-angle spinning 13C NMR in the s
Synthesis and biological evaluation of 7-trifluoromethylpyrazolo[1,5-a]pyrimidines as anti-inflammatory and antimicrobial agents
Aggarwal, Ranjana,Masan, Eakta,Kaushik, Pawan,Kaushik, Dhirender,Sharma, Chetan,Aneja
, p. 16 - 24 (2015/03/05)
A series of 2-H/methyl-3-phenyl-5-alkyl/aryl/heteroaryl-7-trifluoromethylpyrazolo[1,5-a]pyrimidines (4a-l) were synthesized by refluxing 3(5)-amino-4-phenyl-5(3)-H/methyl-1H-pyrazoles (1-2) with trifluoromethyl-?2-diketones (3a-f) in ethanol for 6 h. The
Study of regioselectivity of reactions between 3(5)-aminopyrazoles and 2-acetylcycloalkanones
Petrov,Kasatochkin,Emelina
, p. 1111 - 1120 (2013/01/15)
Regioselectivity was examined of reactions between nine 3(5)-aminopyrazoles and 2-acetylcyclopentanone and 2-acetylcyclohexanone under various conditions. A series of cyclopenta[e]pyrazolo-[1,5-a]pyrimidines was obtained. The highest regioselectivity of the reaction was observed in alcohol at 20°C in the presence of a catalytic quantity of trifl uoroacetic acid. The regiostructure of compounds was established by 1H and 13C NMR spectroscopy. Pleiades Publishing, Ltd., 2012.
Reactions with Diazoazoles, VIII. - Syntheses of Azolo-1,2,3,5-tetrazin-4(3H)-ones
Ege, Guenter,Gilbert, Karlheinz,Maurer, Kurt
, p. 1375 - 1396 (2007/10/02)
Azolo-1,2,3,5-tetrazin-4(3H)-ones 4 and 5 are formed by cycloaddition reactions of α-diazoazoles 2 with aryl or alkyl isocyanates 3a-p, respectively, as well as with diisocyanates 3q,r (Method A).Alternative syntheses for 4 are presented by diazoti