[EN] ETHYNE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF<br/>[FR] DÉRIVÉS D'ÉTHYNE, COMPOSITIONS PHARMACEUTIQUES ET LEURS UTILISATIONS
申请人:BOEHRINGER INGELHEIM INT
公开号:WO2012032014A1
公开(公告)日:2012-03-15
invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
Value of zeolites in asymmetric induction during photocyclization of pyridones, cyclohexadienones and naphthalenones
作者:Karthikeyan Sivasubramanian、Lakshmi S. Kaanumalle、Sundararajan Uppili、V. Ramamurthy
DOI:10.1039/b702572f
日期:——
approaches, have been examined within zeolites with the aim of achieving asymmetricinduction during the photocyclization of cyclohexadienone, naphthalenone and pyridone derivatives. Within zeolites, enantioselectivity as high as 55% and diastereoselectivity as high as 88% have been obtained. The observed stereoselectivities are significant given the fact that these reactions gave very little stereoselectivities
Addition of novel benzylmagnesium “ate” complexes of BnR2MgLi type to 2-(thio)pyridones and related compounds
作者:Jacek G. Sośnicki、Tomasz Idzik、Aleksandra Borzyszkowska、Emil Wróblewski、Gabriela Maciejewska、Łukasz Struk
DOI:10.1016/j.tet.2016.12.024
日期:2017.2
Novel benzylation reagents BnR2MgLi were obtained by mixing benzylmagnesium chloride (BnMgCl) and appropriate organolithiumcompounds (RLi). As BnR2MgLi complexes are more nucleophilic than the parent Grignardcompound they enabled regioselective C6-addition to electrophilic N-substituted 2-(thio)-pyridones and C4-addition to poorly reactive NH 2-(thio)pyridones in high and good yields, respectively
The invention provides novel compounds having the general formula (I)
wherein R
1
, R
2
and n are as described herein, compositions including the compounds and methods of using the compounds. The compounds are useful as inhibitors of hormone sensitive lipase (HSL) for the treatment of diabetes, metabolic syndrome and obesity.
[EN] NEW AZACYCLIC COMPOUNDS<br/>[FR] NOUVEAUX COMPOSÉS AZACYCLIQUES
申请人:HOFFMANN LA ROCHE
公开号:WO2012020035A1
公开(公告)日:2012-02-16
The invention provides novel compounds having the general formula (I) wherein R1, R2 and n are as described herein, compositions including the compounds and methods of using the compounds.