37088-07-6Relevant articles and documents
CHEMICAL COMPOUND OF ISOCITRATE DEHYDROGENASE INHIBITOR, AND APPLICATION THEREOF
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Paragraph 0110; 0111; 0112, (2019/06/07)
Provided are a chemical compound of an isocitrate dehydrogenase inhibitor, and an application thereof, belonging to the field of medicinal chemistry; specifically provided is the chemical compound represented by formula I, or its isomer, pharmaceutically acceptable salt, crystal, solvate, or prodrug, as well as their preparation methods and pharmaceutical compositions containing said chemical compound, and an application of said chemical compound or composition. The chemical compound has very good ability to inhibit mutant IDH2 enzyme activity and to inhibit mutant IDH2 neoplastic cells, and may be used for preventing and/or treating a tumor characterized by the presence of mutant IDH2.
Glycosynthase-Mediated Assembly of Xylanase Substrates and Inhibitors
Goddard-Borger, Ethan D.,Fiege, Brigitte,Kwan, Emily M.,Withers, Stephen G.
experimental part, p. 1703 - 1711 (2012/06/29)
An exo-β-xylosidase mutant with glycosynthase activity was created to aid in the synthesis of xylanase substrates and inhibitors. Simple monosaccharides were easily elaborated into di-, tri- and tetrasaccharides by using this enzyme. Some products proved
Amination of meso-bromophenyl(polyalkyl)porphyrins: Synthesis of porphyrins containing a hydroxypiperidine fragment
Artamkina,Sazonov,Shtern,Grishina,Veselov,Semeikin,Syrbu,Koifman,Beletskaya
, p. 421 - 431 (2008/12/22)
5,15-Bis(4-bromophenyl)-2,8,12,18-tetraethyl-3,7,13,17-tetramethylporphyrin and 5-(4-bromophenyl)-13,17-dibutyl-2,3,7,8,12,18-hexamethylporphyrin were synthesized, and their palladium-catalyzed amination with a number of cyclic secondary amines, including hydroxypiperidines, was studied [Pd(OAc) 2, ligand, THF or dioxane, t-BuONa, 80-100°C]. The reactions of the meso-bromophenylporphyrins with piperidine and morpholine gave the corresponding amination products in quantitative yield. The amination with hydroxypiperidines required excess amine (3 equiv per bromine atom) and excess base (6-8 equiv) and was accompanied by formation of hydrodebromination products; in the reactions with the bis(bromophenyl)derivative, mixed products resulting from amination at one phenyl group and reductive debromination at the other were also formed. The yields of the amination products varied from good {75-50percent in the reactions with 4-hydroxypiperidine and trans-3-hydroxy-4-[4-(2- fluorophenyl)piperazin-1-yl]piperidine} to moderate (20-50percent, 3-hydroxypiperidine) and poor [11-25percent, trans-3,4-dihydroxypiperidine and trans-3-hydroxy-4-(4-hydroxypiperidin-1-yl)piperidine].
2-Deoxyribose as a rich source of chiral 5-carbon building blocks
Wang, Dengjin,Nugent, William A.
, p. 7307 - 7312 (2008/02/11)
(Chemical Equation Presented) We have developed concise routes to a number of useful chiral 5-carbon synthetic building blocks using readily available O-1-methyl-2-deoxyribose as starting material. Novel transformations include the use of indium triflate
Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds
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Page/Page column 26, (2010/02/14)
The present invention relates to alkyne compounds of general formula I wherein the groups and radicals A, B, W, X, Y, Z, R1 and R2 have the meanings given in claim 1. Moreover the invention relates to pharmaceutical compositions containing at least one alkyne according to the invention. By virtue of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity and diabetes.
NOVEL ALKYNE COMPOUNDS WITH AN MCH-ANTAGONISTIC ACTION AND MEDICAMENTS CONTAINING SAID COMPOUNDS
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Page/Page column 69, (2010/02/14)
The invention relates to alkyne compounds of general formula (I), in which the groups and radicals A, B, W, X, Y, Z, R1 and R2 are defined as cited in claim 1. The invention also relates to medicaments containing at least one inventive alkyne. As a result of the antagonistic action against the MCH-receptor, the inventive medicaments are suitable for treating metabolic disorders and/or eating disorders, in particular adiposity and diabetes.
MODULATORS OF CELLULAR ADHESION
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Page/Page column 129-130, (2010/02/11)
The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof, wherein R1-R4, n, p, A, B, D, E, L and AR1 are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of disorders mediated by the CD11/CD18 family of cellular adhesion molecules (e.g., LFA-1).
Enantioselective Trans Dihydroxylation of Nonactivated C-C Double Bonds of Aliphatic Heterocycles with Sphingomonas sp. HXN-200
Chang, Dongliang,Heringa, Maarten F.,Witholt, Bernard,Li, Zhi
, p. 8599 - 8606 (2007/10/03)
The bacterial strain Sphingomonas sp. HXN-200 was used to catalyze the trans dihydroxylation of N-substituted 1,2,5,6-tetrahydropyridines 1 and 3-pyrrolines 4 giving the corresponding 3,4-dihydroxypiperidines 3 and 3,4-dihydroxypyrrolidines 6, respectivel
Iminosugars: Potential inhibitors of liver glycogen phosphorylase
Jakobsen, Palle,Lundbeck, Jane M,Kristiansen, Marit,Breinholt, Jens,Demuth, Helle,Pawlas, Jan,Torres Candela, Maria P,Andersen, Birgitte,Westergaard, Niels,Lundgren, Karsten,Asano, Naoki
, p. 733 - 744 (2007/10/03)
The first synthesis of the single isomers 3R, 4R, 5R); 3S,4S,5S); 3R,4R,5S) and 3S,4S, 5R) of 5-hydroxymethyl-piperidine-3,4-diol from Arecolin is reported, including the synthesis of a series of N-substituted derivatives of the 3R,4R,5R)-isomer Isofagomi