613241-14-8

Upstream product

• 457889-46-2 (4′-(trifluoromethyl)-[1,1′-biphenyl]-4-yl)methanol 
• 97067-18-0 4'-methyl-4-trifluoromethyl-biphenyl 
• 128796-39-4 4-trifluoromethylphenylboronic acid 
• 1122-91-4 4-bromo-benzaldehyde 
• 90035-34-0 4-(4-trifluoromethylphenyl)benzaldehyde 

Downstream Products

• 613241-06-8 methyl 2-[2-butyl-4-({4-[4-(trifluoromethyl)phenyl]phenyl}methylthio)phenoxy]acetate 
• 1128268-09-6 Ethyl 5-(trifluoromethyl)-1-[6-(2-{[4'-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)pyridin-2-yl]-1H-pyrazole-4-carboxylate 
• 1417526-64-7 1-((4'-(trifluoromethyl)biphenyl-4-yl)methyl)-1H-benzo[d]imidazole 
• 1417531-67-9 methyl 3-((tert-butoxycarbonylamino)methyl)-4-((4'-(trifluoromethyl)biphenyl-4-yl)methyl)isoxazole-5-carboxylate 
• 1417531-64-6 methyl 3-((4-oxo-2-thioxo-2,3,4,5,6,7-hexahydro-1H-cyclopenta[d]pyrimidin-1-yl)methyl)-4-((4'-(trifluoromethyl)biphenyl-4-yl)methyl)isoxazole-5-carboxylate 
• 1417531-43-1 methyl 3-((2-(4-fluorobenzylthio)-4-oxo-4,5,6,7-tetrahydro-1H-cyclopenta[d]pyrimidin-1-yl)methyl)-4-((4'-(trifluoromethyl)biphenyl-4-yl)methyl)isoxazole-5-carboxylate 
• 1417531-44-2 2-(4-fluorobenzylthio)-1-((5-(hydroxymethyl)-4-((4'-(trifluoromethyl)biphenyl-4-yl)methyl)isoxazol-3-yl)methyl)-6,7-dihydro-1H-cyclopenta[d]pyrimidin-4(5H)-one 
• 1417531-45-3 1-((5-(chloromethyl)-4-((4'-(trifluoromethyl)biphenyl-4-yl)methyl)isoxazol-3-yl)methyl)-2-(4-fluorobenzylthio)-6,7-dihydro-1H-cyclopenta[d]pyrimidin-4(5H)-one 
• 1417531-46-4 1-((5-((diethylamino)methyl)-4-((4'-(trifluoromethyl)biphenyl-4-yl)methyl)isoxazol-3-yl)methyl)-2-(4-fluorobenzylthio)-6,7-dihydro-1H-cyclopenta[d]pyrimidin-4(5H)-one 
• 1417531-66-8 C₂₀H₁₇F₃N₂O₃ 

Relevant academic research and scientific papers

AZOLE HETEROCYCLIC COMPOUND, PREPARATION METHOD, PHARMACEUTICAL COMPOSITION AND USE

The present invention relates to the filed of pharmarcutical chemistry, and in particular, to a novel class of azole compounds represented by general formula (I), (II) or (III) amd a preparation method thereof, a pharmarcutical composition with the compounds as active components, and a use of the azole compounds and the pharmarcutical composition in the preparation of a medicament for treatment of diseases associated with Lp-PLA2 enzyme activities, wherein each substituent is as deinfed in the specifictaion.

AZOLE HETEROCYCLIC COMPOUND, PREPARATION METHOD, PHARMACEUTICAL COMPOSITION AND USE

The present invention relates to the field of pharmaceutical chemistry, and in particular, to a novel class of azole compounds represented by general formula (I), (II) or (III) and a preparation method thereof, a pharmaceutical composition with the compounds as active components, and a use of the azole compounds and the pharmaceutical composition in the preparation of a medicament for treatment of diseases associated with Lp-PLA2 enzyme activities, wherein each substituent is as defined in the specification.

PYRIMIDINE DERIVATIVES AS ACTIVATORS OF SOLUBLE GUANYLATE CYCLASE

Disclosed are compounds of formula (I) and or salts thereof which activate soluble guanylate cyclase (sGC), pharmaceutical compositions containing them, their use in the manufacture of a medicament for teating cardiovascular diseases, and processes for their preparation.

Fluorinated benzyloxyphenyl piperidine-4-carboxamides with dual function against thrombosis: Inhibitors of factor xa and platelet aggregation

A series of benzyloxy anilides of nipecotic (5, 6) and isonipecotic (7, 8) acids were synthesized and assayed in vitro as inhibitors of ADP-induced platelet aggregation and the blood coagulation enzymes factor Xa (FXa) and thrombin (Flla). An exploration of effects of the amidine group attached at the piperidine nitrogen, position and substitution (F, phenyl) of the benzyloxy group, and addition of fluorine/s on the second (distal) phenyl ring, led us to single out some promising isonipecotamide derivatives 7. Addition of meta-F and para-CF3 on the distal phenyl ring resulted in a 6-to-18-fold enhancement of the FXa potency and in 2-to- 4-fold increase of the antiplatelet potency, the last depending to a large extent upon lipophilicity. Two congeners of N-{[3-(1,1′-biphenyl-4-yl)methoxy]phenyljpiperidine-4-carboxamide (7m and 7p) proved to be potent FXa-selective inhibitors (Ki = 130 and 57 nM, respectively) and antiplatelet agents and were identified as leads for developing new dual function antithrombotic drugs.

2,6-DISUBSTITUTED PYRIDINES AS SOLUBLE GUANYLATE CYCLASE ACTIVATORS

Disclosed are compounds of formula (I) wherein R1 and R2 are independently selected from hydrogen, halo, CF3, C1-4alkyl and allyl; Y represents (II), (III), (IV) or (V) wherein R3 represents CF3 or C1-4alkyl; and R3a represents CF3 or C1-4alkyl.

GLUCAGON RECEPTOR ANTAGONISTS, PREPARATION AND THERAPEUTIC USES

The present invention discloses novel compounds of Formula (I), or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.

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.