Disclosed herein are substituted pyrimidine-based endothelin modulators of Formula I, processes of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
本文披露了一种Formula I的取代嘧啶基内皮素调节剂,其制备方法、药物组合物以及使用方法。
[EN] INDUSTRIAL PROCESS OF MONO-ALKYLATING A PIPERIDINE NITROGEN IN PIPERIDINE DERIVATIVES WITH DEUTERATED-ALKYL<br/>[FR] PROCÉDÉ INDUSTRIEL DE MONOALKYLATION D'UN AZOTE DE PIPÉRIDINE DANS DES DÉRIVÉS DE LA PIPÉRIDINE AVEC UN ALKYLE DEUTÉRÉ
申请人:OTSUKA PHARMA CO LTD
公开号:WO2019049918A1
公开(公告)日:2019-03-14
The present invention relates to a method of mono-alkylating a piperidine nitrogen in a piperidine derivative with a deuterated lower-alkyl, which comprises protecting the piperidine nitrogen with an aralkyl protective group, lower-alkylating the piperidine nitrogen with a deuterated-lower-alkylating agent under neutral or basic condition, and then deprotecting the aralkyl protective group.
Disclosed herein are substituted naphthalene-based melatonin (MT) receptor modulators and/or 5-HT receptor modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
METHOD FOR INTRODUCING DEUTERATED LOWER ALKYL INTO AMINE MOIETY OF COMPOUND CONTAINING SECONDARY AMINE
申请人:OTSUKA PHARMACEUTICAL CO., LTD.
公开号:US20220127206A1
公开(公告)日:2022-04-28
The present invention relates to a method of mono-deuterated-lower-alkylating the amine part in a compound having an amine protected with an aralkyl, which comprises introducing mono-deuterated lower-alkyl into the amine with a deuterated-lower-alkylating agent under neutral or basic condition, and then deprotecting the aralkyl group.
The present disclosure provides a compound represented by structural Formula (I): or a pharmaceutically acceptable salt thereof useful for treating a cancer.