144757-33-5

Upstream product

• 39815-78-6 methyl 3-oxoheptanoate 
• 124750-51-2 N-(triephenylmethyl)-5-<4'-(bromomethyl)-biphenyl-2-yl>tetrazole 

Downstream Products

• 148564-13-0 6-butyl-2-methyl-5-<<2'-<1-(triphenylmethyl)-1H-tetrazol-5-yl><1,1'-biphenyl>-4-yl>methyl>pyrimidin-4(1H)-one 
• 148564-34-5 methyl 2-<<4-butyl-2-methyl-6-oxo-5-<<2'-<1-(triphenylmethyl)-1H-tetrazol-5-yl><1,1'-biphenyl>-4-yl>methyl>-1(6H)-pyrimidinyl>methyl>-3-thiophenecarboxylate 
• 172292-49-8 3-{4-Butyl-2-methyl-6-oxo-5-[2'-(1-trityl-1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-6H-pyrimidin-1-ylmethyl}-thiophene-2-carboxylic acid methyl ester 
• 148564-35-6 2-{4-Butyl-2-methyl-6-oxo-5-[2'-(1-trityl-1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-6H-pyrimidin-1-ylmethyl}-furan-3-carboxylic acid methyl ester 
• 148597-80-2 methyl 2-<<4-butyl-2-methyl-6-oxo-5-<<2'-<1-(triphenylmethyl)-1H-tetrazol-5-yl><1,1'-biphenyl>-4-yl>methyl>-1(6H)-pyrimidinyl>methyl>benzoate 
• 172292-51-2 6-Butyl-2-methyl-3-thiophen-2-ylmethyl-5-[2'-(1-trityl-1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-3H-pyrimidin-4-one 
• 172292-50-1 3-Benzyl-6-butyl-2-methyl-5-[2'-(1-trityl-1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-3H-pyrimidin-4-one 
• 172292-58-9 methyl 2-<<4-butyl-2-methyl-6-oxo-5-<<2'-(1H-tetrazol-5-yl)<1,1'-biphenyl>-4-yl>methyl>-1(6H)-pyrimidinyl>methyl>-3-furancarboxylate 
• 148564-47-0 milfasartan 

Relevant academic research and scientific papers

N-3-Substituted Pyrimidones as Potent, Orally Active, AT1 Selective Angiotensin II Receptor Antagonists

A novel series of nonpeptide angiotensin II (A II) antagonists containing a pyrimidinone ring which carries a C-linked biphenyltetrazole moiety and a carboxyheteroaryl group on the 3-position have been prepared.Their affinity for the AT1 receptor was determined in a binding assay on rat adrenal cortical membranes.The in vivo antihypertensive properties were tested by evaluating the inhibition of the pressor response to A II followed by iv and id administration.Extensive molecular modeling studies, including comparison of molecular electrostatic potential distributions, conformational analysis, and overlays on a computational pharmacophore model of A II, were used to evaluate structural parameters of the new compounds, in comparison to other known A II antagonists (e.g., DUP-753 and SKandF 108566).According to the modeling studies, the introduction of a (carboxyheteroaryl)methyl moiety at the 3-position of the pyrimidinone ring led to derivatives with increased potency.Methyl 2-methyl>-1-(6H)-pyrimidinyl>methyl>-3-thiophenecarboxylate (3k, LR-B/081), one of the most potent compounds in the series (Ki = 1.4 nM), exhibited a marked antihypertensive activity on oral administration to conscious renal hypertensive rats, with long duration of action.It was selected for clinical evaluation in the treatment of hypertension in man.

PYRIMIDINONE DERIVATIVES FUSED TO NITROGEN HETEROCYCLES HAVING A II ANTAGONISTIC ACTIVITY

Derivatives of bicyclic heterocycles comprising a pyrimidone ring fused to another 5, 6, or 7 membered nitrogen heterocycle which is C-substituted, through a methylene bridge, by a biphenyl group.

4-pyrimidinone derivatives their preparation and their application in therapy

Compounds which can be expressed as tautomeric forms and having the formulas (I), (I') and (I") STR1 wherein R1 =a straight or branched (C1-7) alkyl group or a straight or branched (C3-9) alkenyl group or a cyclo(C3-7