[EN] NOVEL TRICYCLIC COMPOUNDS AS INHIBITORS OF MUTANT IDH ENZYMES<br/>[FR] COMPOSÉS TRICYCLIQUES INNOVANTS SERVANT D'INHIBITEURS D'ENZYMES IDH MUTANTES
申请人:MERCK SHARP & DOHME
公开号:WO2016089797A1
公开(公告)日:2016-06-09
The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.
[EN] COMPOUNDS FOR THE TREATMENT OF ARENAVIRUS INFECTION<br/>[FR] COMPOSÉS POUR LE TRAITEMENT D'UNE INFECTION À ARÉNAVIRUS
申请人:ARISAN THERAPEUTICS INC
公开号:WO2016160677A1
公开(公告)日:2016-10-06
The present invention relates to the use of piperazinones for inhibiting arenavirus infection in humans, other mammals, or in cell culture, to methods of treating arenavirus infection such as Lassa, Bolivian, Argentine, Venezuelan, Brazilian, Chapare and Lujo hemorrhagic fevers, to methods of inhibiting the replication of arenaviruses, to methods of reducing the amount of arenaviruses, and to compositions that can be employed for such methods.
Provided herein are compounds and compositions useful in increasing PPARδ activity. The compounds and compositions provided herein are useful for the treatment of PPARδ related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).
Copper-Catalyzed Chan–Lam Cyclopropylation of Phenols and Azaheterocycles
作者:Joseph Derosa、Miriam L. O’Duill、Matthew Holcomb、Mark N. Boulous、Ryan L. Patman、Fen Wang、Michelle Tran-Dubé、Indrawan McAlpine、Keary M. Engle
DOI:10.1021/acs.joc.7b03100
日期:2018.4.6
Small molecules containing cyclopropane–heteroatom linkages are commonly needed in medicinal chemistry campaigns yet are problematic to prepare using existing methods. To address this issue, a scalable Chan–Lam cyclopropylation reaction using potassium cyclopropyl trifluoroborate has been developed. With phenol nucleophiles, the reaction effects O-cyclopropylation, whereas with 2-pyridones, 2-hydroxybenzimidazoles
The present invention relates to a class of tricyclic compounds and an application thereof as a sphingosine 1-phosphate type 1 (S1P1) receptor agonist. The invention specifically relates to a compound represented by formula (II), and a tautomer and pharmaceutically acceptable salt of same.