[EN] PYRROLOPYRIMIDINE DERIVATIVES AS MODULATORS OF MULTI-DRUG RESISTANCE (MDR) [FR] DERIVES PYRROLOPYRIMIDINIQUES CONVENANT COMME MODULATEURS DE LA MULTIRESISTANCE AUX MEDICAMENTS
본원에 개시된 것은 양전자 방출 단층 촬영을 이용하여 병원성 질환을 진단 및/또는 모니터링하기 위한 화합물, 조성물 및 방법이다. 또한 개시된 것은 B가 비타민 수용체 결합 리간드 (예컨대 폴레이트), PSMA 결합 리간드 또는 PSMA 억제제로부터 선택되는 표적화제의 라디칼이며; L이 아스파르트산, 라이신, 또는 아르기닌을 포함하는 2가 링커이고; P가 조영제 또는 방사선 요법제, 예컨대 방사성 핵종 또는 방사성 핵종 함유 기의 라디칼, 또는 방사성 핵종, 예컨대 금속 킬레이팅 기에 결합할 수 있는 화합물의 라디칼인 화학식 B-L-P의 콘쥬게이트이다.
[EN] ROR-GAMMA INHIBITORS<br/>[FR] INHIBITEURS DE ROR-GAMMA
申请人:GLAXOSMITHKLINE IP DEV LTD
公开号:WO2019063748A1
公开(公告)日:2019-04-04
The present invention relates to compounds of formula I and pharmaceutical compositions comprising compounds of formula I. Compounds of Formula I are useful in treatment of inflammatory, metabolic or autoimmune diseases which are mediated by RORy.
Isoquinoline-1,3-diones as Selective Inhibitors of Tyrosyl DNA Phosphodiesterase II (TDP2)
作者:Jayakanth Kankanala、Christophe Marchand、Monica Abdelmalak、Hideki Aihara、Yves Pommier、Zhengqiang Wang
DOI:10.1021/acs.jmedchem.5b01973
日期:2016.3.24
isoquinoline-1,3-dione as a viable chemotype for selectivelyinhibiting TDP2. The initial hit compound 43 was identified by screening our in-house collection of synthetic compounds. Further structure–activity relationship (SAR) studies identified numerous analogues inhibiting TDP2 in low micromolar range without appreciable inhibition against the homologous TDP1 at the highest testing concentration
[EN] CHROMAN - SPIROCYCLIC PIPERIDINE AMIDES AS MODULATORS OF ION CHANNELS<br/>[FR] AMIDES DE PIPÉRIDINE SPIROCYCLIQUE CHROMANIQUE EN TANT QUE MODULATEURS DES CANAUX IONIQUES
申请人:VERTEX PHARMA
公开号:WO2012112743A1
公开(公告)日:2012-08-23
The invention relates to chroman spirocyclic piperidine amide derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
Compounds of Formula I that inhibit the activity of the diacylglycerol acyltransferase 2 (DGAT2) and their uses in the treatment of diseases linked thereto in animals are described herein.