Vinblastine 20″ amides: synthetic analogs that maintain or improve potency and simultaneously overcome Pgp-derived efflux and resistance
申请人:The Scripps Research Institute
公开号:US10689381B2
公开(公告)日:2020-06-23
A vinca alkaloid compound substituted at the 20′-position with a carboxamido group is disclosed. The carbonyl of the carboxamido group is bonded to a 20′-amino group and to a ring system that contains up to three 5-, 6- or 7-membered rings that are fused or otherwise bonded together. Each ring can be carbocyclic or heterocyclic, with a heterocyclic ring containing up to three hetero ring atoms that are the same or different and are selected from nitrogen, oxygen and sulfur. The ring system can include up to four substituent groups other than hydrogen that are discussed within. Methods of preparing the compounds are disclosed as are compositions for their use and methods of treatment using d compound. A particularly preferred compound has an activity in specified cancer cell growth inhibition assays that is the same or better than its parental, unsubstituted vinca compound and is not subject to Pgp-mediated efflux.
VINBLASTINE 20' AMIDES: SYNTHETIC ANALOGS THAT MAINTAIN OR IMPROVE POTENCY AND SIMULTANEOUSLY OVERCOME Pgp-DERIVED EFFLUX AND RESISTANCE
申请人:The Scripps Research Institute
公开号:US20190119277A1
公开(公告)日:2019-04-25
A vinca alkaloid compound substituted at the 20′-position with a carboxamido group is disclosed. The carbonyl of the carboxamido group is bonded to a 20′-amino group and to a ring system that contains up to three 5-, 6- or 7-membered rings that are fused or otherwise bonded together. Each ring can be carbocyclic or heterocyclic, with a heterocyclic ring containing up to three hetero ring atoms that are the same or different and are selected from nitrogen, oxygen and sulfur. The ring system can include up to four substituent groups other than hydrogen that are discussed within. Methods of preparing the compounds are disclosed as are compositions for their use and methods of treatment using d compound. A particularly preferred compound has an activity in specified cancer cell growth inhibition assays that is the same or better than its parental, unsubstituted vinca compound and is not subject to Pgp-mediated efflux.
[EN] 1,2-NAPHTHOQUINONE DERIVATIVE AND METHOD FOR PREPARING SAME<br/>[FR] DÉRIVÉ DE 1,2-NAPHTHOQUINONE ET SON PROCÉDÉ DE PRÉPARATION<br/>[KO] 1,2 나프토퀴논 유도체 및 이의 제조방법
申请人:KT&G LIFE SCIENCES CORP
公开号:WO2016159576A2
公开(公告)日:2016-10-06
본 발명은 제1항에 정의된 화학식 (1)로 표시되는 화합물, 그것의 약제학적으로 허용되는 염, 수화물, 용매화물, 프로드럭, 토토머(tautomer), 거울상 이성질체 또는 약학적으로 허용 가능한 부분입체 이성질체를 제공한다.
Regioselectivity in the Friedel-Crafts tert-Butylation of 1-Naphthol