Estrogen receptor ligands. Part 8: Dihydrobenzoxathiin SERAMs with heteroatom-substituted side chains
摘要:
A series of benzoxathiin SERAMs with heteroatom-substituted amine side chains was prepared. Minor modifications in the side chain resulted in significant effects on biological activity, especially in uterine tissue. (C) 2004 Elsevier Ltd. All rights reserved.
INHIBITORS OF KEAP1-Nrf2 PROTEIN-PROTEIN INTERACTION
申请人:Janssen Pharmaceutica NV
公开号:US20200055874A1
公开(公告)日:2020-02-20
Sultam compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions associated with the KEAP1-Nrf2 interaction, such as inflammatory bowel disease, including Crohn's disease and ulcerative colitis.
A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease.
[EN] SMALL MOLECULES THAT TARGET THE RNA THAT CAUSES ALS<br/>[FR] PETITES MOLÉCULES CIBLANT L'ARN PROVOQUANT LA SLA
申请人:EXPANSION THERAPEUTICS INC
公开号:WO2022055922A1
公开(公告)日:2022-03-17
Disclosed herein are compounds that selectively bind an expanded transcribed repeat r(G4C2)exp, prevent sequestration of RNA-binding proteins, and inhibit translation of repeat associated non-ATG (RAN) translation responsible for generation of toxic dipeptide repeats underlying diseases such as amyotrophic lateral sclerosis (ALS) and frontotemporal dementia (FTD). The compounds and their pharmaceutical compositions are useful in treating a disease or condition characterized by an expanded G4C2 repeat RNA (r(G4C2)exp), such as ALS and FTD.
Optimisation of the synthesis of second generation 1,2,4,5 tetraoxane antimalarials
作者:Paul M. O' Neill、Sunil Sabbani、Gemma L. Nixon、Matthew Schnaderbeck、Natalie L. Roberts、Emma R. Shore、Christopher Riley、Ben Murphy、Paul McGillan、Stephen A. Ward、Jill Davies、Richard K. Amewu
DOI:10.1016/j.tet.2016.08.043
日期:2016.10
An efficient route to the synthesis of potent antimalarial aryloxy 1,2,4,5-tetraoxanes is described that permits parallel synthesis for Structure–Activity Relationship (SAR) investigations. Brief details of the in vitro and in vivo antimalarial evaluation are included which enables identification of antimalarial leads for further development. Also described is an improved approach to the synthesis of
[EN] NEW SPIROCYCLOHEXANE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND THEIR USES AS ANTI-APOPTOTIC INHIBITORS<br/>[FR] NOUVEAUX DÉRIVÉS DE SPIROCYCLOHEXANE, COMPOSITIONS PHARMACEUTIQUES LES CONTENANT ET LEURS UTILISATIONS COMME INHIBITEURS ANTI-APOPTOTIQUES
申请人:SERVIER LAB
公开号:WO2024008941A1
公开(公告)日:2024-01-11
Compounds of Formula (I): wherein R1, R2, R3, R4and are as defined in the description. Medicaments.