- NOVEL ARYLOXYPIPERIDINE PYRAZOLE COMPOUNDS AS INDOLEAMINE 2,3-DIOXYGENASE INHIBITORS
-
Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
- -
-
Page/Page column 40; 41
(2020/03/15)
-
- NITROGEN HETEROCYCLE DERIVATIVES, PREPARATION THEREOF AND APPLICATION THEREOF IN HUMAN THERAPEUTICS
-
The present invention relates to compounds having general formula I characterised in that wherein in particular: R1 represents one or a plurality of groups such as: trifluoromethyl, halogen such as F, Cl, Br, methyl, nitro. R represents nitroge
- -
-
Paragraph 0214; 0215
(2013/03/26)
-
- DERIVATIVES OF 2H PYRIDAZIN- 3 -ONES, THEIR PREPARATION AND THEIR USE AS SCD-1 INHIBITORS
-
The present invention concerns compounds of general formula (I) characterized in that (formula 1) wherein, in particular: -R1 represents one or more groups such as: trif luoromethyl, halogen such as F, C1, -when n=m=1, W represents CH then Y represents oxygen, -U represents: ? either - (C=O) CH2NH- and is branched at position 4 of pyridazinone, then R2 represents H, ? or -(C=O)NH- and U is branched at positions (4), (5) or (6) of pyridazinone, then R2 represents H, - R3 represents a hydrogen or methyl and the addition salts with pharmaceutically acceptable bases and acids and the different isomers, and their mixtures in any proportion for use as SCD-1 enyzme inhibitors for the treatment of obesitz, tzpe-2 diabetes and lipid disorders.
- -
-
Page/Page column 31; 32
(2011/02/24)
-
- NOVEL PIPERAZINE DERIVATIVES AS INHIBITORS OF STEAROYL-CoA DESATURASE
-
The present invention relates to piperidine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.
- -
-
Page/Page column 23
(2009/10/01)
-
- Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors
-
A series of structurally novel stearoyl-CoA desaturase1 (SCD1) inhibitors has been identified via molecular scaffold manipulation. Preliminary structure-activity relationship (SAR) studies led to the discovery of potent, and orally bioavailable piperidine-aryl urea-based SCD1 inhibitors. 4-(2-Chlorophenoxy)-N-[3-(methyl carbamoyl)phenyl]piperidine-1-carboxamide 4c exhibited robust in vivo activity with dose-dependent desaturation index lowering effects.
- Xin, Zhili,Zhao, Hongyu,Serby, Michael D.,Liu, Bo,Liu, Mei,Szczepankiewicz, Bruce G.,Nelson, Lissa T.J.,Smith, Harriet T.,Suhar, Tom S.,Janis, Rich S.,Cao, Ning,Camp, Heidi S.,Collins, Christine A.,Sham, Hing L.,Surowy, Teresa K.,Liu, Gang
-
scheme or table
p. 4298 - 4302
(2009/04/06)
-
- Discovery of potent, selective, orally bioavailable stearoyl-CoA desaturase 1 inhibitors
-
Stearoyl-CoA desaturase 1 (SCD1) catalyzes the committed step in the biosynthesis of monounsaturated fatty acids from saturated, long-chain fatty acids. Studies with SCD1 knockout mice have established that these animals are lean and protected from leptin
- Liu, Gang,Lynch, John K.,Freeman, Jennifer,Liu, Bo,Xin, Zhili,Zhao, Hongyu,Serby, Michael D.,Kym, Philip R.,Suhar, Tom S.,Smith, Harriet T.,Cao, Ning,Yang, Ruojing,Janis, Rich S.,Krauser, Joel A.,Cepa, Steven P.,Beno, David W. A.,Sham, Hing L.,Collins, Christine A.,Surowy, Teresa K.,Camp, Heidi S.
-
p. 3086 - 3100
(2008/02/10)
-
- Substituted triazole derivatives as oxytocin antagonists
-
The present invention relates to substituted triazoles of formula (I), uses thereof, processes for the preparation thereof and compositions containing said compounds. These inhibitors have utility in a variety of therapeutic areas including sexual dysfunction.
- -
-
Page/Page column 30-31
(2008/06/13)
-