694-68-8Relevant academic research and scientific papers
DUAL-INHIBITORS OF CELLULAR NECROPTOSIS AND FERROPTOSIS FOR USE IN THE TREATMENT OF ORGAN TRANSPLANT PATIENTS
-
Paragraph 0170, (2021/09/09)
The invention relates to chemical compounds for use as a medicament in the prevention of organ transplant rejection and/or transplant organ damage. In embodiments of the invention, the compound inhibits and/or reduces ferroptosis and necroptosis of cells of the transplanted organ. In further embodiments, the patient is at risk of transplant rejection and/or is at risk of or shows signs of ischemia-reperfusion injury and/or necroinflammation.
USE OF HETEROCYCLIC DERIVATIVES WITH CARDIOMYOCYTE PROLIFERATION ACTIVITY FOR TREATMENT OF HEART DISEASES
-
Page/Page column 17, (2021/06/22)
Provided herein is the use of heterocyclic derivatives with cardiomyocyte proliferation activity for treatment of heart diseases. Specifically, disclosed is the use of compounds of formula (I) or a pharmaceutically acceptable salt, a solvate, a stereoisomer or a prodrug thereof; and application thereof. Definition of each group in the formula can be found in the specification for details.
NOVEL HETEROCYCLIC DERIVATIVES WITH CARDIOMYOCYTE PROLIFERATION ACTIVITY FOR TREATMENT OF HEART DISEASES
-
Page/Page column 20; 22; 23, (2021/06/22)
Provided are novel heterocyclic derivatives with cardiomyocyte proliferation activity for treatment of heart diseases. Specifically, provided are the compounds of formula (I) or pharmaceutically acceptable salts, stereoisomers, solvates or prodrugs, prepa
N-ACYL AMINO ACID COMPOUNDS AND METHODS OF USE
-
Paragraph 0511, (2018/03/28)
The invention relates to compounds of formula (I), or a salt thereof wherein R1, A, L, and R2 and n are as described herein. Compounds of formula (I) and pharmaceutical compositions thereof are ανβ1 integrin inhibitors that are useful for treating tissue specific fibrosis.
Inhibition of Cancer-Associated Mutant Isocitrate Dehydrogenases by 2-Thiohydantoin Compounds
Wu, Fangrui,Jiang, Hong,Zheng, Baisong,Kogiso, Mari,Yao, Yuan,Zhou, Chao,Li, Xiao-Nan,Song, Yongcheng
supporting information, p. 6899 - 6908 (2015/09/22)
Somatic mutations of isocitrate dehydrogenase 1 (IDH1) at R132 are frequently found in certain cancers such as glioma. With losing the activity of wild-type IDH1, the R132H and R132C mutant proteins can reduce α-ketoglutaric acid (α-KG) to d-2-hydroxyglutaric acid (D2HG). The resulting high concentration of D2HG inhibits many α-KG-dependent dioxygenases, including histone demethylases, to cause broad histone hypermethylation. These aberrant epigenetic changes are responsible for the initiation of these cancers. We report the synthesis, structure-activity relationships, enzyme kinetics, and binding thermodynamics of a novel series of 2-thiohydantoin and related compounds, among which several compounds are potent inhibitors of mutant IDH1 with Ki as low as 420 nM. X-ray crystal structures of IDH1(R132H) in complex with two inhibitors are reported, showing their inhibitor-protein interactions. These compounds can decrease the cellular concentration of D2HG, reduce the levels of histone methylation, and suppress the proliferation of stem-like cancer cells in BT142 glioma with IDH1 R132H mutation.
Synthesis of N,N′-bis(5-arylidene-4-oxo-3,5-dihydro-4H-imidazol-2-yl) diamines bearing various linkers and biological evaluation as potential inhibitors of kinases
Coulibaly, Wacothon Karime,Paquin, Ludovic,Bénie, Anoubilé,Bekro, Yves-Alain,Durieu, Emilie,Meijer, Laurent,Bazureau, Jean Pierre
, p. 581 - 590 (2013/02/23)
The synthesis in 4 steps of new N,N′-bis(5-arylidene-4-oxo-3,5- dihydro-4H-imidazol-2-yl)diamines issued from various symmetric primary diamines as linkers was reported. The key step of our strategy has been the sulphur/nitrogen displacement of (5Z)-5-arylidene-2-ethylsulfanyl-3,5-dihydro- 4H-imidazol-4-ones 6 with respectively ethylenediamine 7a, piperazine 7b and N,N′-bis(3-aminopropyl)piperazine 7c using solvent-free reaction conditions under microwave irradiation with retention of configuration. These compounds were tested for their kinase inhibitory potencies toward four kinases (GSK-3α/β, DYRK1A, CLK1 and CLK3).
Facile synthesis of hydantoins and thiohydantoins in aqueous solution
Baccolini, Graziano,Boga, Carla,Delpivo, Camilla,Micheletti, Gabriele
experimental part, p. 1713 - 1717 (2011/05/05)
A series of hydantoins and thiohydantoins have been synthesized in water at room temperature from urea (or N-methylurea, or thiourea) and simple aldehydes (as glyoxal, and its simple derivatives) in the presence of phosphoric anhydride. The reaction time is 10 min using an equimolar amount of P 4O10 with respect to the other reagents, but the reaction occurs also, even if with longer reaction times, with very small amounts of P4O10. In addition, this method provides a clean and 'green' approach to hydantoins, compounds of great interest in biological and pharmacological fields.
IMIDAZAOLONE DERIVATIVES,PREPARATION THEREOF AND BIOLOGICAL USE OF SAME
-
Page/Page column 8, (2010/09/05)
Imidazolone derivatives, as medicaments, of formula wherein: R1═H, C1 to C5 alkyl, aryl or a 5- or 6-membered heterocyclic group;Ar1=optionally substituted aryl or an aromatic heterocycle;R═R2—S—, Rs
5-(Pyridylmethylidene)-substituted 2-thiohydantoins and their complexes with CuII, NiII, and CoII: Synthesis, electrochemical study, and adsorption on the cystamine-modified gold surface
Beloglazkina,Majouga,Yudin,Frolova,Zyk,Dolzhikova,Moiseeva,Rakhimov,Butin
, p. 1015 - 1027 (2008/02/01)
A series of CuII, NiII, and CoII complexes with 5-(pyridylmethylidene)-substituted 2-thiohydantoins (L) were synthesized by the reactions of the corresponding organic ligands with MCl 2?nH2O. The resu
Microwave-mediated solventless synthesis of new derivatives of marine alkaloid Leucettamine B
Chérouvrier, Jean-René,Carreaux, Fran?ois,Bazureau, Jean Pierre
, p. 3581 - 3584 (2007/10/03)
New access to N-alkyl derivatives of the marine alkaloid Leucettamine B are described using two three-step convergent routes. For the formation of the 2-amino imidazolone ring, the key steps involve solvent-free condensations under microwaves and guanylation reactions with non-sterically hindered primary amines.
