A class of substituted azetidine, pyrrolidine and piperidine derivatives are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.
NOVEL COMPOUNDS HAVING ESTROGEN RECEPTOR ALPHA DEGRADATION ACTIVITY AND USES THEREOF
申请人:ACCUTAR BIOTECHNOLOGY INC.
公开号:US20200157078A1
公开(公告)日:2020-05-21
The present disclosure relates to novel compounds having estrogen receptor alpha degradation activity, pharmaceutical compositions containing such compounds, and their use in prevention and treatment of cancer and related diseases and conditions.
Reaction of alkoxyhydroperoxides with metal salts alkyl halide preparation
作者:G. Cardinale、J.C. Grimmelikhuysen、J.A.M. Laan、F.P. van Lier、D. van der Steen、J.P. Ward
DOI:10.1016/s0040-4020(01)89123-7
日期:1989.1
A synthesis is described of alkyl chlorides by reaction of methoxy hydroperoxides, prepared from 1-alkenes by ozonisation in methanol, with ferric chloride: RCHCH2→RCH(OOH)OCH3→R·→RC1. Yields of 1-chlorotetradecane were about 60%; those of other halides from 38 to 57%.
[EN] AZETIDINE, PYRROLIDINE AND PIPERIDINE DERIVATIVES<br/>[FR] DERIVES DE L'AZETIDINE, DE LA PYRROLIDINE ET DE LA PIPERIDINE
申请人:MERCK SHARP & DOHME LIMITED
公开号:WO1996004274A1
公开(公告)日:1996-02-15
(EN) A class of substituted azetidine, pyrrolidine and piperidine derivatives are selective agonists of 5-HT1-like receptors, being potent agonists of the human 5-HT1D$g(a) receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT1D$g(a) receptor subtype relative to the 5-HT1D$g(b) subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT1D receptor agonists.(FR) Classe de dérivés substitués de l'azétidine, de la pyrrolidine et de la pipéridine constituant des agonistes sélectifs des récepteurs du genre 5-HT1 qui sont puissants agonistes du sous-type de récepteur humain 5-HT1D$g(a) tout en possédant une affinité sélective au moins 10 fois plus forte pour le sous-type 5-HT1D$g(a) que le sous-type 5-HT1D$g(b). Ils s'avèrent de ce fait utiles dans le traitement et/ou la prévention d'états cliniques tels que la migraine ou des troubles associés pour lesquels un sous-type sélectif d'agoniste des récepteurs du 5-HT1D est indiqué, tout en provoquant moins d'effets secondaires, tels que certains phénomènes cardio-vasculaires adverses, que ceux qui sont associés à des agonistes non sélectifs du sous-type du récepteur du 5-HT1D.
Compounds having estrogen receptor alpha degradation activity and uses thereof
申请人:ACCUTAR BIOTECHNOLOGY INC.
公开号:US10696659B2
公开(公告)日:2020-06-30
The present disclosure relates to novel compounds having estrogen receptor alpha degradation activity, pharmaceutical compositions containing such compounds, and their use in prevention and treatment of cancer and related diseases and conditions.