Cu(I)-Catalyzed Diamination of Disubstituted Terminal Olefins: An Approach to Potent NK<sub>1</sub> Antagonist
作者:Yuehong Wen、Baoguo Zhao、Yian Shi
DOI:10.1021/ol900808z
日期:2009.6.4
This paper describes a diamination process using di-tert-butyldiaziridinone as nitrogen source and CuCl as catalyst. A wide variety of disubstituted terminalolefins can be efficiently diaminated in good yields under mild condition. This diamination process was used to synthesize potent NK1 antagonist Sch 425078.
本文描述了使用二叔丁基二氮杂环丙烷酮作为氮源和氯化铜作为催化剂的二胺化过程。多种二取代端烯烃可以在温和条件下以良好的产率有效地二胺化。这种二胺化过程用于合成有效的 NK 1拮抗剂Sch 425078。
12-EPI PLEUROMUTILINS
申请人:NABRIVA THERAPEUTICS AG
公开号:US20160332963A1
公开(公告)日:2016-11-17
A compound selected from 14-O-[((Alkyl-, cycloalkyl-, heterocycloalkyl-, heteoroaryl-, or aryl)-sulfanyl)-acetyl]-12-epi-mutilins, or 14-O-[((Alkyl-, cycloalkyl-, heterocycloalkyl-, heteoroaryl-, or aryl)-oxy)-acetyl]-12-epi-mutilins, wherein 12-epi-mutilin is characterized in that the mutilin ring at position 12 is substituted by two substituents, the first substituent at position 12 of the mutilin ring is a methyl group which methyl group has the inverse stereochemistry compared with the stereochemistry of the methyl group at position 12 of the naturally occurring pleuromutilin ring, the second substituent at position 12 of the mutilin ring is a hydrocarbon group comprising at least one nitrogen atom and all other substituents of the mutilin ring having the same stereochemistry compared with the stereochemistry of the substituents at the corresponding positions in the naturally occurring pleuromutilin ring; optionally in the form of a salt and/or solvate, wherein the naturally occurring pleuromutilin is of formula
processes for the preparation of such compounds and their use as pharmaceuticals.
NEW IMIDAZOLONE AND IMIDAZOLIDINONE DERIVATIVES AS 11B-HSD1 INHIBITORS
申请人:Ackermann Jean
公开号:US20080103183A1
公开(公告)日:2008-05-01
Compounds of formula
as well as pharmaceutically acceptable salts and esters thereof, wherein R
1
to R
6
have the significance given in claim
1
can be used in the form of pharmaceutical compositions.
[EN] BICYCLIC HETEROCYCLIC COMPOUNDS AS INHIBITORS OFBCDIN3D ACTIVITY<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES BICYCLIQUES EN TANT QU'INHIBITEURS DE L'ACTIVITÉ DE BCDIN3D
申请人:STORM THERAPEUTICS LTD
公开号:WO2020254831A1
公开(公告)日:2020-12-24
The present invention relates to compounds that function as inhibitors and/or degraders of BCDIN3D activity. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which BCDIN3D activity is implicated.
Regulation of enzymes which utilize tetrahydrobiopterin or
申请人:South Alabama Medical Science Foundation
公开号:US05401844A1
公开(公告)日:1995-03-28
6-[2'-Amino-2',2'-disubstituted-ethylamino]-pyrimidines of the structure: ##STR1## in which X=H, NH.sub.2 or NO.sub.2, which are novel intermediates in the synthesis of quinoid 6,6-disubstituted-dihydro- and 6,6-disubstituted-tetrahydro-pteridines, are claimed.