An efficient synthesis of highly functionalized chiral lactams
摘要:
A new method was developed to synthesize highly functionalized lactams via a one pot reductive amination/lactam formation reaction. This methodology is amenable for parallel synthesis and was used to prepare a large number of lactam analogs in a library format with good ee (de) retention. (C) 2011 Elsevier Ltd. All rights reserved.
The invention is concerned with novel imidazopyrimidine derivatives of formula (I)
wherein R
1
, R
2
and R
8
are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as pharmaceuticals.
[EN] N-(IMIDAZOPYRIMIDIN-7-YL)-HETEROARYLAMIDE DERIVATIVES AND THEIR USE AS PDE10A INHIBITORS<br/>[FR] DÉRIVÉS DE N-(IMIDAZOPYRIMIDIN-7-YL)-HÉTÉROARYLAMIDE ET LEUR UTILISATION COMME INHIBITEURS DE PDE10A
申请人:HOFFMANN LA ROCHE
公开号:WO2011117264A1
公开(公告)日:2011-09-29
The invention is concerned with novel imidazopyrimidine derivatives of formula (I) wherein R1, R2 and R8 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDEIOA and used as medicaments.
The present invention relates to azole compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
TETRAZOLE-SUBSTITUTED ARYLAMIDES AS P2X3 AND P2X2/3 ANTAGONISTS
申请人:Dillon Michael Patrick
公开号:US20150191487A1
公开(公告)日:2015-07-09
Compounds of the formula I:
or a pharmaceutically acceptable salt thereof, wherein, R
1
is optionally substituted tetrazolyl, R
2
is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R
3
, R
4
, R
5
and R
6
are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X
3
and/or a P2X
2/3
receptor antagonist and methods of making the compounds.
[EN] NOVEL PYRROLIDINE DERIVED BETA 3 ADRENERGIC RECEPTOR AGONISTS<br/>[FR] NOUVEAUX AGONISTES DE RÉCEPTEURS ADRÉNERGIQUES BÊTA 3 DÉRIVÉS DE PYRROLIDINE
申请人:MERCK SHARP & DOHME
公开号:WO2011025690A1
公开(公告)日:2011-03-03
The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of β3-adrenoceptor.