71229-85-1Relevant academic research and scientific papers
Pyrazole N-alkylation method
-
Paragraph 0021; 0022; 0030-0032, (2018/12/14)
The invention provides a pyrazole N-alkylation method. Pyrazole or pyrazole derivatives and alkyl halogenated hydrocarbons react in a solvent under the existence of quaternary ammonium salt catalysts;N-alkyl substituted pyrazole is obtained. The method provided by the invention has the advantages that the operation is simple; the cost is low; the anhydrous oxygen-free environment is not needed; heating is not needed; the yield is high; the amplified industrialized production can be easily realized.
AUTOTAXIN INHIBITORS AND USES THEREOF
-
Paragraph 00324; 00327, (2016/12/22)
Described herein are methods and compositions for the treatment of conditions, diseases, or disorders associated with autotaxin activity. The methods and compositions disclosed herein include the use of at least one autotaxin inhibitor compound.
PROTEIN KINASE INHIBITORS
-
Paragraph 0150, (2015/02/18)
A compound of formula (I), wherein R3, R4, G, B, M, and Z are as defined in the claims, and pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (I) possess utility as FGFR inhibitors and are useful in the treatment of a condition, where FGFR kinase inhibition is desired, such as cancer.
NRF2 REGULATORS
-
Page/Page column 403, (2015/07/07)
The present invention relates to bis aryl analogs, pharmaceutical compositions containing them and their use as Nrf2 regulators.
AUTOTAXIN INHIBITOR COMPOUNDS
-
Paragraph 00341, (2015/06/08)
Described herein are compounds that are autotaxin inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorde
Methods for the treatment of metabolic disorders by a selective small molecule autotaxin inhibitor
-
Paragraph 0258, (2015/06/16)
Described herein are methods and compositions for treatment or prevention of metabolic disorder(s) in an individual. The methods and compositions disclosed herein include the use of at least one autotaxin inhibitor compound.
Fragment-based identification of amides derived from trans-2-(pyridin-3-yl) cyclopropanecarboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT)
Giannetti, Anthony M.,Zheng, Xiaozhang,Skelton, Nicholas J.,Wang, Weiru,Bravo, Brandon J.,Bair, Kenneth W.,Baumeister, Timm,Cheng, Eric,Crocker, Lisa,Feng, Yezhen,Gunzner-Toste, Janet,Ho, Yen-Ching,Hua, Rongbao,Liederer, Bianca M.,Liu, Yongbo,Ma, Xiaolei,O'Brien, Thomas,Oeh, Jason,Sampath, Deepak,Shen, Youming,Wang, Chengcheng,Wang, Leslie,Wu, Hongxing,Xiao, Yang,Yuen, Po-Wai,Zak, Mark,Zhao, Guiling,Zhao, Qiang,Dragovich, Peter S.
, p. 770 - 792 (2014/03/21)
Potent, trans-2-(pyridin-3-yl)cyclopropanecarboxamide-containing inhibitors of the human nicotinamide phosphoribosyltransferase (NAMPT) enzyme were identified using fragment-based screening and structure-based design techniques. Multiple crystal structures were obtained of initial fragment leads, and this structural information was utilized to improve the biochemical and cell-based potency of the associated molecules. Many of the optimized compounds exhibited nanomolar antiproliferative activities against human tumor lines in in vitro cell culture experiments. In a key example, a fragment lead (13, KD = 51 μM) was elaborated into a potent NAMPT inhibitor (39, NAMPT IC 50 = 0.0051 μM, A2780 cell culture IC50 = 0.000 49 μM) which demonstrated encouraging in vivo efficacy in an HT-1080 mouse xenograft tumor model.
PROTEIN KINASE INHIBITORS
-
Page/Page column 36, (2013/04/25)
A compound of formula (I), wherein R3, R4, G, B, M, and Z are as defined in the claims, and pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (I) possess utility as FGFR inhibitors and are useful in the treatment of a condition, where FGFR kinase inhibition is desired, such as cancer.
Crucial role of paramagnetic ligands for magnetostructural anomalies in "breathing crystals"
Tretyakov, Evgeny V.,Tolstikov, Svyatoslav E.,Suvorova, Anastasiya O.,Polushkin, Aleksey V.,Romanenko, Galina V.,Bogomyakov, Artem S.,Veber, Sergey L.,Fedin, Matvey V.,Stass, Dmitry V.,Reijerse, Edward,Lubitz, Wolfgang,Zueva, Ekaterina M.,Ovcharenko, Victor I.
, p. 9385 - 9394 (2012/11/13)
Breathing crystals based on polymer-chain complexes of Cu(hfac)2 with nitroxides exhibit thermally and light-induced magnetostructural anomalies in many aspects similar to a spin crossover. In the present work, we report the synthesis and investigation of a new family of Cu(hfac)2 complexes with tert-butylpyrazolylnitroxides and their nonradical structural analogues. The complexes with paramagnetic ligands clearly exhibit structural rearrangements in the copper(II) coordination units and accompanying magnetic phenomena characteristic for breathing crystals. Contrary to that, their structural analogues with diamagnetic ligands do not undergo rearrangements in the copper(II) coordination environments. This confirms experimentally the crucial role of paramagnetic ligands and exchange interactions between them and copper(II) ions for the origin of magnetostructural anomalies in this family of molecular magnets.
Synthesis of pinacol esters of 1-alkyl-1H-pyrazol-5-yl- and 1-alkyl-1H-pyrazol-4-ylboronic acids
Ivachtchenko, Alexandre V.,Kravchenko, Dmitry V.,Zheludeva, Valentina I.,Pershin, Dmitry G.
, p. 931 - 939 (2007/10/03)
Starting from 1H-pyrazol, a wide number of 1-alkyl-1H-pyrazol-4-yl and 1-alkyl-1H-pyrazol-5-ylboronic acids and their pinacol esters were synthesized and characterized. The key step in the described methodology is the regioselective lithiation of the pyrazole ring. The synthesized pinacolates are stable under prolonged storage and can be used as convenient reagents in organic synthesis.
