70080-54-5Relevant articles and documents
Aryl ketone amide compound, preparation method and application thereof
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Paragraph 0132-0134, (2020/11/09)
The invention discloses an aryl ketoamide compound or a pharmaceutically acceptable salt thereof, a preparation method and application thereof, wherein the compound has a structure represented by a general formula I, and in the formula, substituent groups are defined in the specification and claims. According to the invention, the compound provided by the invention can simultaneously inhibit the activity of various kinases, especially KDR, and further cell level detection results find that the compound has a remarkable inhibition effect on VEGF-induced human umbilical vein endothelial cell HUVEC proliferation, and is a small-molecular VEGFR-2 inhibitor with good activity at the enzyme level and the cell level, so that the compound provided by the invention can be developed into a medicinefor preventing and/or treating tumors or cancers.
NOVEL INHIBITORS
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Page/Page column 99, (2011/05/03)
The invention relates to novel pyrrolidine derivatives of formula (I): wherein R1, R2 and R3 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.
Inhibitors of lipoprotein(a) assembly
Sexton, Karen E.,Lee, Helen T.,Massa, Mark,Padia, Janak,Patt, William C.,Liao, Peggy,Pontrello, Jason K.,Roth, Bruce D.,Spahr, Mark A.,Ramharack, Randy
, p. 4827 - 4845 (2007/10/03)
Compounds of the general structure A and B were investigated for their activity as lipoprotein(a), [Lp(a)], assembly (coupling) inhibitors. SAR around the amino acid derivatives (structure A) gave compound 14-6 as a potent coupling inhibitor. Oral dosing