454464-38-1

Upstream product

• 873-75-6 4-bromobenzenemethanol 
• 1122-91-4 4-bromo-benzaldehyde 
• 128796-39-4 4-trifluoromethylphenylboronic acid 
• 5798-75-4 Ethyl 4-bromobenzoate 
• 589-17-3 p-bromobenzyl chloride 
• 457889-46-2 (4′-(trifluoromethyl)-[1,1′-biphenyl]-4-yl)methanol 
• 647842-34-0 ethyl 4'-(trifluoromethyl)-[1,1'-biphenyl]-4-carboxylate 

Downstream Products

• 613239-54-6 [2-Methyl-4-(4'-trifluoromethyl-biphenyl-4-ylmethylsulfanyl)-phenoxy]-acetic Acid Methyl Ester 
• 613239-80-8 [5-Chloro-2-methyl-4-(4'-trifluoromethyl-biphenyl-4-ylmethylsulfanyl)-phenoxy]-acetic Acid Methyl Ester 
• 934737-89-0 [2-(4'-Trifluoromethylbiphenyl-4-yl-methoxy)phenyl]methanol 
• 934818-60-7 [5-Fluoro-2-(4'-trifluoromethylbiphenyl-4-ylmethoxy)phenyl]methanol 
• 1030367-79-3 2-methyl-4-(((4′-(trifluoromethyl)-[1,1′-biphenyl]-4-yl)methyl)thio)phenol 
• 935253-61-5 4-[(4E)-3-[4-(1H-Tetrazol-5-yl)benzyl]-5-(2-{[4'-(trifluoromethyl)biphenyl-4-yl]-methoxy}phenyl)pent-4-en-1-yl}benzoic acid 
• 935253-34-2 Methyl 4-[(4E)-3-[4-(1H-tetrazol-5-yl)benzyl]-5-(2-{[4'-(trifluoromethyl)biphenyl-4-yl]methoxy}-phenyl)pent-4-en-1-yl]benzoate 
• 1030368-00-3 C₃₀H₂₄F₃O₃S^(1-)*K⁽¹⁺⁾ 
• 1030367-98-6 C₃₃H₂₉F₃O₃S 
• 1030367-96-4 2-(2-methyl-4-((2-phenyl-1-(4′-(trifluoromethyl)-[1,1′-biphenyl]-4-yl)ethyl)thio)phenoxy)acetic acid 
• 1030367-94-2 C₃₅H₃₅F₃O₃S 

Relevant academic research and scientific papers

RADIOLABELED DARAPLADIB AND ANALOGS THEREOF AND THEIR USE AS IMAGING COMPOUNDS

The present inventors have developed new radiolabeled Darapladib and analogs thereof which can be used for the specific detection of vulnerable atherosclerotic plaques by targeting lipoprotein-associated phospholipase A2 (Lp-PLA2) which is a biomarker of

Pd-catalyzed, highly selective C(sp2)-Br bond coupling reactions of o-(or m-, or p-) chloromethyl bromobenzene with arylboronic acids

Highly selective C(sp2)–C(sp2) cross-coupling of dihalogenated hydrocarbons comprising C(sp2)–Br and C(sp3)–Cl bonds with arylboronic acids is reported. This highly selective coupling reaction of the C(sp2)–Br bond is successfully achieved using Pd(OAc)2 and PCy3·HBF4 as the palladium source and ligand, respectively. A series of chloromethyl-1,1′-biphenyl compounds are obtained in moderate-to-excellent yields. Moreover, this protocol can be extended to the one-pot dual arylation of 1-bromo-4-(chloromethyl)benzene with two arylboronic acids, leading to diverse unsymmetrical 4-benzyl-1,1′-biphenyl derivatives.

Synthesis and evaluation of an orally available “Y”-shaped biaryl peroxisome proliferator-activated receptor δ agonist

In this study, we designed and synthesized several novel “Y”-shaped biaryl PPARδ agonists. Structure-activity relationship (SAR) studies demonstrated that compound 3a was the most active agonist with an EC50 of 2.6 nM. We also synthesized and evaluated enantiospecific R and S isomers of compound 3a to confirm that R isomer (EC50 = 0.7 nM) shows much more potent activity than S isomer (EC50 = 6.1 nM). Molecular docking studies between the PPAR ligand binding domain and enantiospecific R and S isomers of compound 3a were performed. In vitro absorption, distribution, metabolism, excretion, and toxicity (ADMET) and in vivo PK profiles show that compound 3a possesses superior drug-like properties including good bioavailability. Our overall results clearly demonstrate that this orally administrable PPARδ agonist 3a is a viable drug candidate for the treatment of various PPARδ-related disorders.

Dicarboxylic Acid Derivatives and their Use

The present application relates to novel dicarboxylic acid derivatives, process for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, es

Tetrazole Derivatives and Their Use for the Treatment of Cardiovascular Diseases

The present application relates to novel tetrazole derivatives, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especial

Heterocyclic compounds with carboxyl isostere groups and their use for the treatment of cardiovascular diseases

The present application relates to novel heterocyclic compounds, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especia

Difluorophenol Derivatives and Their Use

The present application relates to novel difluorophenol derivatives, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.

NOVEL DERIVATIVES OF DICARBOXYLIC ACID HAVING PHARMACEUTICAL PROPERTIES

The invention relates to compounds of formulae (II), (IV), and (VI) as shown below, wherein the several variable groups are as defined in the specification and claims. Processes for making these materials, and methods for using them in the synthesis of compounds for treatment of cardiovascular disorders and fibrotic disorders are also disclosed.

Compounds that modulate PPAR activity and methods of preparation

This invention relates to compounds that alter PPAR activity. The invention also relates to pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable compositions comprising the compounds or their salts, and methods of using them as therapeutic agents for treating or preventing dyslipidemia, hypercholesterolemia, obesity, hyperglycemia, atherosclerosis, hypertriglyceridemia and hyperinsulinemia in a mammal. The present invention also relates to methods for making the disclosed compounds.

Compounds that modulate PPAR activity and methods for their preparation

This invention discloses compounds that alter PPAR activity. The invention also discloses pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable compositions comprising the compounds or their salts, and methods of using them as therapeutic agents for treating or preventing disipidemia, hypercholesteremia, obesity, eating disorders, hyperglycemia, atherosclerosis, hypertriglyceridemia, hyperinsulinemia and diabetes in a mammal as well as methods of supressing appetite and modulating leptin levels in a mammal. The present invention also discloses methods for making the disclosed compounds.