88563-83-1Relevant academic research and scientific papers
Pyrrolopyrazole derivative, preparation method and medical application thereof
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Paragraph 0111; 0113, (2021/02/24)
The invention relates to pyrrolopyrazole derivative, a preparation method and application thereof in medicines. Specifically, the invention relates to a new pyrrolopyrazole derivative as shown in a general formula (I), a preparation method and application of the pyrrolopyrazole derivative or a pharmaceutical composition containing the pyrrolopyrazole derivative as a therapeutic agent, particularlyas a gastric acid secretion inhibitor and potassium-competitive acid blockers (P-CABs) in biological medicines. Specifically, the substituents (R1, R2, R3 and R4) in the general formula (I) are the same as the definitions in the specification.
Development of 2,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one inhibitors of aldehyde dehydrogenase 1A (ALDH1A) as potential adjuncts to ovarian cancer chemotherapy
Buchman, Cameron D.,Buckanovich, Ronald J.,Chtcherbinine, Mikhail,Debnath, Bikash,Felton, Jeremy,Grimley, Edward,Huddle, Brandt C.,Hurley, Thomas D.,Larsen, Scott D.,Li, Siwei,Mao, Shuai,McGonigal, Stacy C.,Neamati, Nouri,Pan, Shu,Sun, Duxin,Takahashi, Cyrus,Wen, Bo
, (2020/12/21)
There is strong evidence that inhibition of one or more Aldehyde Dehydrogenase 1A (ALDH1A) isoforms may be beneficial in chemotherapy-resistant ovarian cancer and other tumor types. While many previous efforts have focused on development of ALDH1A1 select
PYRIDINONE DICARBOXAMIDE FOR USE AS BROMODOMAIN INHIBITORS
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Page/Page column 141, (2017/03/21)
The present invention relates to compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and to their use in therapy.
MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
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Paragraph 00330; 00331, (2013/08/28)
Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
Catalytic enantioselective cross-couplings of secondary alkyl electrophiles with secondary alkylmetal nucleophiles: Negishi reactions of racemic benzylic bromides with achiral alkylzinc reagents
Binder, Joerg T.,Cordier, Christopher J.,Fu, Gregory C.
supporting information, p. 17003 - 17006,4 (2012/12/11)
We have developed a nickel-catalyzed method for the asymmetric cross-coupling of secondary electrophiles with secondary nucleophiles, specifically, stereoconvergent Negishi reactions of racemic benzylic bromides with achiral cycloalkylzinc reagents. In contrast to most previous studies of enantioselective Negishi cross-couplings, tridentate pybox ligands are ineffective in this process; however, a new, readily available bidentate isoquinoline-oxazoline ligand furnishes excellent ee's and good yields. The use of acyclic alkylzinc reagents as coupling partners led to the discovery of a highly unusual isomerization that generates a significant quantity of a branched cross-coupling product from an unbranched nucleophile.
Catalytic enantioselective cross-couplings of secondary alkyl electrophiles with secondary alkylmetal nucleophiles: Negishi reactions of racemic benzylic bromides with achiral alkylzinc reagents
Binder, Joerg T.,Cordier, Christopher J.,Fu, Gregory C.
supporting information, p. 17003 - 17006 (2013/01/15)
We have developed a nickel-catalyzed method for the asymmetric cross-coupling of secondary electrophiles with secondary nucleophiles, specifically, stereoconvergent Negishi reactions of racemic benzylic bromides with achiral cycloalkylzinc reagents. In contrast to most previous studies of enantioselective Negishi cross-couplings, tridentate pybox ligands are ineffective in this process; however, a new, readily available bidentate isoquinoline-oxazoline ligand furnishes excellent ee's and good yields. The use of acyclic alkylzinc reagents as coupling partners led to the discovery of a highly unusual isomerization that generates a significant quantity of a branched cross-coupling product from an unbranched nucleophile.
Synthetic studies on morphine-based analgesics. Intramolecular Diels-Alder approach to a 4a-aryldecahydroisoquinolines
Handa, Sheetal,Jones, keith,Newton, Christopher G.
, p. 1623 - 1634 (2007/10/02)
An efficient, stereospecific synthesis of the trans-4a-aryldecahydroisoquinoline skeleton, a substructure of morphine known to possess analgesic activity, is described.
