877681-12-4

Upstream product

• 658-89-9 4-(trifluoromethoxy)benzene-1,2-diamine 
• 57-13-6 urea 
• 2267-23-4 2-nitro-4-trifluoromethoxyaniline 
• 1737-06-0 N-(4-(trifluoromethoxy)phenyl)acetamide 
• 461-82-5 4-(trifluoromethoxy)aniline 
• 1351534-05-8 2-amino-4-trifluoromethoxy-N-acetylaniline 
• 787-57-5 2-nitro-4-trifluoromethoxy-N-acetylaniline 
• 530-62-1 1,1'-carbonyldiimidazole 

Downstream Products

• 886465-16-3 2-chloro-6-(trifluoromethoxy)-1H-benzo[d]imidazole 
• 1351534-24-1 (2R)-2-[2-chloro-5-[[3-(6-methoxybenzisoxazol-3-yl)-2-oxo-5-trifluoromethoxybenzimidazol-1-yl]methyl]phenoxy]propanoic acid 
• 1073558-81-2 3-phenyl-8-{5-[(trifluoromethyl)oxy]-1H-benzimidazol-2-yl}-1-oxa-3,8-diazaspiro-[4.5]decan-2-one hydrochloride 
• 1073559-38-2 3-phenyl-8-{5-[(trifluoromethyl)oxy]-1H-benzimidazol-2-yl}-1-oxa-3,8-diazaspiro-[4.5]decan-2-one 

Relevant academic research and scientific papers

CYANOPYRROLIDINE DERIVATIVES WITH ACTIVITY AS INHIBITORS OF USP30

The present invention relates to a class of substituted-cyanopyrrolidines of Formula (I) with activity as inhibitors of deubiquitilating enzymes, in particular, ubiquitin C-terminal hydrolase 30 or ubiquitin specific peptidase 30 (USP30), having utility i

Benzimidazolones: A new class of selective peroxisome proliferator- activated receptor γ (PPARγ) modulators

A series of benzimidazolone carboxylic acids and oxazolidinediones were designed and synthesized in search of selective PPARγ modulators (SPPARγMs) as potential therapeutic agents for the treatment of type II diabetes mellitus (T2DM) with improved safety profiles relative to rosiglitazone and pioglitazone, the currently marketed PPARγ full agonist drugs. Structure-activity relationships of these potent and highly selective SPPARγMs were studied with a focus on their unique profiles as partial agonists or modulators. A variety of methods, such as X-ray crystallographic analysis, PPARγ transactivation coactivator profiling, gene expression profiling, and mutagenesis studies, were employed to reveal the differential interactions of these new analogues with PPARγ receptor in comparison to full agonists. In rodent models of T2DM, benzimidazolone analogues such as (5R)-5-(3-{[3-(5-methoxybenzisoxazol-3-yl)benzimidazol-1-yl]methyl}phenyl) -5-methylox-azolidinedione (51) demonstrated efficacy equivalent to that of rosiglitazone. Side effects, such as fluid retention and heart weight gain associated with PPARγ full agonists, were diminished with 51 in comparison to rosiglitazone based on studies in two independent animal models. (Figure presented)

BENZIMIDAZOLES WITH A HETERO SPIRO-DECANE RESIDUE AS NPY-Y5 ANTAGONISTS

The present invention relates to compounds of formula (I), or a pharmaceutically acceptable salts, solvates, stereoisomers thereof, formula (I), R1 may be C1-C4 alkyl, aryl or heteroaryl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; R2 may be halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano, nitro; or aryl, heteroaryl or heterocycle, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; or R2 may correspond to -0-R3; R3 is a 6-membered aromatic carbocyclic ring which may contain 1 or 2 nitrogen X is carbon or oxygen; Z is carbon or nitrogen; G is a fused 6-membered aromatic carbocyclic ring which may contain 1 or 2 nitrogen; m may be 0 or an integer ranging from 1 to 4; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as NPY- Y5 receptor antagonists.