Synthesis of 4-Substituted Chlorophthalazines, Dihydrobenzoazepinediones, 2-Pyrazolylbenzoic Acid, and 2-Pyrazolylbenzohydrazide via 3-Substituted 3-Hydroxyisoindolin-1-ones
作者:Hanh Nho Nguyen、Victor J. Cee、Holly L. Deak、Bingfan Du、Kathleen Panter Faber、Hakan Gunaydin、Brian L. Hodous、Steven L. Hollis、Paul H. Krolikowski、Philip R. Olivieri、Vinod F. Patel、Karina Romero、Laurie B. Schenkel、Stephanie D. Geuns-Meyer
DOI:10.1021/jo3000628
日期:2012.4.20
hydrazine, followed by chlorination with POCl3. We have also discovered twonovel transformations of 3-vinyl- and 3-alkynyl-3-hydroxyisoindolinones. Addition of vinyl organometallic reagents to N,N-dimethylaminophthalimide (8a) provided dihydrobenzoazepinediones 15a–15c via the proposed ringexpansion of 3-vinyl-3-hydroxyisoindolinone intermediates. 3-Alkynyl-3-hydroxyisoindolinones react with hydrazine and
[EN] LIVER X RECEPTOR (LXR) MODULATORS<br/>[FR] MODULATEURS DU RÉCEPTEUR X DU FOIE
申请人:ALEXAR THERAPEUTICS INC
公开号:WO2015035015A1
公开(公告)日:2015-03-12
Described herein are liver X receptor (LXR) modulators and methods of utilizing LXR modulators in the treatment of LXR-associated diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.
[EN] SUBSTITUTED 2-AZA-BICYCLO[2.2.1]HEPTANE-3-CARBOXYLIC ACID (BENZYL-CYANO-METHYL)-AMIDES INHIBITORS OF CATHEPSIN C<br/>[FR] (BENZYL-CYANO-MÉTHYL)-AMIDES SUBSTITUÉS DE L'ACIDE 2-AZA-BICYCLO[2.2.1]HEPTANE-3-CARBOXYLIQUE UTILISÉS COMME INHIBITEURS DE LA CATHÉPSINE C
申请人:BOEHRINGER INGELHEIM INT
公开号:WO2014140075A1
公开(公告)日:2014-09-18
This invention relates to 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)- amides of formula (1) and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
The present invention provides a compound which has the effect of PDE inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on.
A compound of formula (I
0
):
wherein
R
1
represents
a substituent,
R
2
represents
a hydrogen atom, or a substituent,
R
3
represents
a hydrogen atom, or a substituent,
Ring A represents
an aromatic ring which can be substituted, and
Ring B represents
a 5-membered heteroaromatic ring which can be substituted,
or a salt thereof.