58336-71-3

Upstream product

• 600-00-0 ethyl 2-bromoisobutyrate 
• 18672-06-5 ethyl 2-methyl-2-(4-methylphenoxy)propanoate 
• 639784-43-3 ethyl 2-[4-(hydroxymethyl)phenoxy]-2-methylpropanoate 

Downstream Products

• 639784-56-8 2-methyl-2-(4-methylaminomethyl-phenoxy)-propionic acid ethyl ester 
• 85938-28-9 1-benzoyl-3-[4-(1-ethoxycarbonyl-1-methylethoxy)benzyl]imidazolium bromide 
• 1347432-77-2 Example 50 
• 1347901-08-9 Example 35 
• 1348663-05-7 Example 49 
• 1347730-66-8 Example 39 
• 1347719-01-0 24 
• 1027251-82-6 2-methyl-2-[4-{[(4-methyl-2-[4-trifluoromethylphenyl]-thiazol-5-ylmethyl)-N-methyl-amino]methyl}phenoxy]propionic acid 
• 639783-80-5 Example 56 
• 1207603-95-9 ethyl 2-methyl-2-(4-((4-methyl-2-propyl-1H-benzo[d]imidazol-1-yl)methyl)phenoxy)propanoate 
• 872990-46-0 2-{4-[2-(3-bromo-2,6-dimethoxy-phenyl)-2-(tert-butyl-dimethyl-silanyloxy)-2-cyano-ethyl]-phenoxy}-2-methyl-propionic acid ethyl ester 
• 58336-70-2 ethyl 2-[4-(pyridin-2-ylaminomethyl)phenoxy]-2-methyl-propionate 

Relevant academic research and scientific papers

Design, Synthesis, and Biological Evaluation of Triazolone Derivatives as Potent PPARα/δDual Agonists for the Treatment of Nonalcoholic Steatohepatitis

Peroxisome proliferator-activator receptors α/δ(PPARα/δ) are regarded as potential therapeutic targets for nonalcoholic steatohepatitis (NASH). However, PPARα/δdual agonist GFT-505 exhibited poor anti-NASH effects in a phase III clinical trial, probably due to its weak PPARα/δagonistic activity and poor metabolic stability. Other reported PPARα/δdual agonists either exhibited limited potency or had unbalanced PPARα/δagonistic activity. Herein, we report a series of novel triazolone derivatives as PPARα/δdual agonists. Among them, compound H11 exhibited potent and well-balanced PPARα/δagonistic activity (PPARα EC50 = 7.0 nM; PPARδEC50 = 8.4 nM) and a high selectivity over PPARγ(PPARγEC50 = 1316.1 nM) in PPAR transactivation assays. The crystal structure of PPARδin complex with H11 revealed a unique PPARδ-agonist interaction. H11, which had excellent PK properties and a good safety profile, showed potent in vivo anti-NASH effects in preclinical models. Together, H11 holds a great promise for treating NASH or other inflammatory and fibrotic diseases.

Design, synthesis, and docking studies of novel benzimidazoles for the treatment of metabolic syndrome

In addition to lowering blood pressure, telmisartan, an angiotensin (AT1) receptor blocker, has recently been shown to exert pleiotropic effects as a partial agonist of nuclear peroxisome proliferator-activated receptor γ (PPARγ). On the basis of these findings and docking pose similarity between telmisartan and rosiglitazone in PPARγ active site, two classes of benzimidazole derivatives were designed and synthesized as dual PPARγ agonist/angiotensin II antagonists for the possible treatment of metabolic syndrome. Compound 4, a bisbenzimidazole derivative showed the best affinity for the AT1 receptor with a Ki=13.4 nM, but it was devoid of PPARγ activity. On the other hand 9, a monobenzimidazole derivative, showed the highest activity in PPARγ transactivation assay (69% activation) with no affinity for the AT1 receptor. Docking studies lead to the designing of a molecule with dual activity, 10, with moderate PPARγ activity (29%) and affinity for the AT1 receptor (Ki=2.5 μM).

1,2-BIS-(SUBSTITUTED-PHENYL)-2-PROPEN-1-ONES AND PHARMACEUTICAL COMPOSITIONS THEREOF

The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula (I), or its pharmaceutically acceptable salt or ester, wherein the substituents are defined in the application.

TRIAZOLE, OXADIAZOLE AND THIADIAZOLE DERIVATIVE AS PPAR MODULATORS FOR THE TREATMENT OF DIABETES

The present invention is directed to compounds represented by the following structural formula, Formula (I): wherein: (a) X is selected from the group consisting of a single bond, O, S, S(O)2 and N; (b) U is an aliphatic linker; (c) Y is selected from the group consisting of O, C, S, NH and a single bond; (d) W is N, O or S; (e) E is C(R3)(R4)A or A and wherein; (f) A is selected from the group consisting of carboxyl, tetrazole, C1-C6 alkylnitrile, carboxamide, sulfonamide and acylsufonamide. The other substituents are defined in the claims; the compounds are modulators of peroxisome proleferator activated receptors (PPARs) and are useful for the treatment of diabetes and other metabolic disorders.

CHEMICAL COMPOUNDS

A compound of formula (I) or a pharmaceutically acceptable salt, solvate, or hydrolysable ester thereof, wherein: (...).

Substituted-phenyl substituted-alkyl ethers and the preparation thereof

The present invention relates to new substituted-phenyl substituted-alkyl ethers and pharmaceutically acceptable salts thereof, which have hypolipidemic activity, and to processes for the preparation thereof, the compound having the following formula STR1