- Kras-G12C inhibitor heterocyclic compounds
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The invention relates to Kras-G12C inhibitor heterocyclic compounds represented by formula I, a preparation method thereof, and application of the Kras-G12C inhibitor heterocyclic compounds in prevention and treatment of tumor diseases such as lung cancer, colorectal cancer and pancreatic cancer. In the preparation process, the compounds of the general formula I are obtained through a series of reactions such as SN2 reaction, protection, coupling reaction, deprotection, condensation reaction and the like.
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Paragraph 0228; 0231-0234
(2021/06/23)
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- Structure-activity relationships of trans-substituted-propenoic acid derivatives on the nicotinic acid receptor HCA2 (GPR109A)
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Nicotinic acid (niacin) has been used for decades as an antidyslipidemic drug in man. Its main target is the hydroxy-carboxylic acid receptor HCA2 (GPR109A), a G protein-coupled receptor. Other acids and esters such as methyl fumarate also interact with the receptor, which constituted the basis for the current study. We synthesized a novel series of substituted propenoic acids, such as fumaric acid esters, fumaric acid amides and cinnamic acid derivatives, and determined their affinities for the HCA2 receptor. We observed a rather restricted binding pocket on the receptor with trans-cinnamic acid being the largest planar ligand in our series with appreciable affinity for the receptor. Molecular modeling and analysis of the structure-activity relationships in the series suggest a planar trans-propenoic acid pharmacophore with a maximum length of 8 ? and out-of-plane orientation of the larger substituents.
- Van Veldhoven,Blad,Artsen,Klopman,Wolfram,Abdelkadir,Lane,Brussee,Ijzerman
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supporting information; experimental part
p. 2736 - 2739
(2011/06/20)
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- Selective monoesterification of dicarboxylic acids catalysed by ion-exchange resins
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Symmetrical dicarboxylic acids with 4-14 carbon atoms gave selectively the corresponding monoesters in high yields in the transesterification catalysed by strongly acidic ion-exchange resins in ester-hydrocarbon mixtures. It was found that the rate of the esterification of the dicarboxylic acids is much higher than that of the monocarboxylic acids formed. This result can explain the high selectivity for the monoester formation and can also be explained by the existence of an aqueous layer on the surface of the resins. This method of selective esterification is quite simple and practical. The Royal Society of Chemistry 1999.
- Nishiguchi, Takeshi,Ishii, Yasuhiro,Fujisaki, Shizuo
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p. 3023 - 3027
(2007/10/03)
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- Hair spray resin composition
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What is provided herein is an improved hair spray resin composition including a terpolymer consisting essentially of a vinyl ester, preferably vinyl acetate, a water-insoluble or water-miscible alkyl maleate half-ester, preferably mono-N-butyl maleate and an N-substituted acrylamide, preferably N-t-butyl acrylamide, N-t-octyl acrylamide or N-[1-(2-pyrrolidonyl)ethyl]acrylamide, in the molar ratio of 1:0.6-0.8:0.08-0.12, respectively, and having a relative viscosity of about 1.2-2.0.
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