Oxazolones as potent inhibitors of 11β-hydroxysteroid dehydrogenase type 1
摘要:
2,5,5-Trisubstituted oxazolones were identified as potent inhibitors of 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1). The synthesis, structure-activity relationship and metabolic stability of these compounds are presented. (c) 2007 Elsevier Ltd. All rights reserved.
[EN] COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF INTERLEUKIN-1 RECEPTOR-ASSOCIATED KINASE 1 PROTEINS<br/>[FR] COMPOSÉS ET PROCÉDÉS POUR LA DÉGRADATION CIBLÉE DE PROTÉINES DE KINASE 1 ASSOCIÉS AU RÉCEPTEUR DE L'INTERLEUKINE 1
申请人:JANSSEN PHARMACEUTICA NV
公开号:WO2021018118A1
公开(公告)日:2021-02-04
The present invention relates to compounds comprising an interleukin-1 receptor-associated kinase 1 (IRAK1) protein binding moiety and a Von Hippel-Lindau (VHL) E3 ubiquitin ligase binding moiety, and associated methods of use. The compounds are useful as modulators of targeted ubiquitination, especially with respect to IRAK1, which is degraded by the compounds according to the invention.
[EN] SYNTHESIS OF GLYCOLS VIA TRANSFER HYDROGENATION OF ALPHA-FUNCTIONAL ESTERS WITH ALCOHOLS<br/>[FR] SYNTHÈSE DE GLYCOLS AU MOYEN D'UNE HYDROGÉNATION PAR TRANSFERT D'ESTERS ALPHA-FONCTIONNELS AVEC DES ALCOOLS
申请人:EASTMAN CHEM CO
公开号:WO2019027948A1
公开(公告)日:2019-02-07
A transfer hydrogenation process for forming vicinal diols by hydrogenating 1,2-dioxygenated organic compounds using alcohols as the reducing agent instead of the traditional H2 gas. The transfer hydrogenation is carried out under milder conditions of temperature and pressure than is typical for ester hydrogenation with H2. The milder conditions of operation provide benefits, such as lower operating and capital costs for industrial scale production as well as savings in product purification due to the avoidance of by-products from exposure of reaction mixtures and products to high temperatures.
[EN] INDAZOLE AND BENZOISOXAZOLE DIHYDROOROTATE DEHYDROGENASE INHIBITORS<br/>[FR] INHIBITEURS DE LA DIHYDROOROTATE DÉSHYDROGÉNASE DE TYPE INDAZOLE ET BENZOISOXAZOLE
申请人:JANSSEN BIOTECH INC
公开号:WO2021240424A1
公开(公告)日:2021-12-02
Disclosed are compounds, compositions and methods for treating diseases, disorders, or medical conditions that are affected by the modulation of DHODH. Such compounds are represented by Formula (I) as follows, wherein R1, R2, R3 and R5 are defined herein.