Diphenyloxazolyl-oxazoles as platelet aggregation inhibitors
AssigneeBristol-Myers Squibb Company
InventorsJeffrey L. Romine, Nicholas A. Meanwell
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AssigneeBristol-Myers Squibb Company
InventorsJeffrey L. Romine, Nicholas A. Meanwell
Estimating the term…
A novel series of oxazole derivatives having enhanced water solubility bioavailability and metabolic stability is disclosed in the Formula I ##STR1## Y is CH.sub.3, Ph, or OH, provided that when Y is OH, the compound exists in the keto-enol tautaumerism form ##STR2## R.sup.1 is Ph or Th; R.sup.2 is H or CH.sub.2 R.sup.3 ; R.sup.3 is H, OCH.sub.3, C.sub.1 -C.sub.5 lower alkyl, or CO.sub.2 R.sup.4 ; R.sup.4 is H or C.sub.1 -C.sub.5 lower alkyl; R.sup.5 is H or CH.sub.3 ; R.sup.6 is OHCHN or H.sub.2 N; and R.sup.7 is H or OH; or pharmaceutically acceptable salt thereof. The compounds are useful as inhibitors of ADP-induced blood platelet aggregation in human platelet-rich plasma.
A compound of the formula ##STR51## Y is CH.sub.3, Ph, or OH, provided that when Y is OH, the compound exists in the keto-enol tautaumerism form ##STR52## R.sup.1 is Ph or Th;
The intermediate methyl 4,5-diphenyl-2-oxazole carboxylate.
The intermediate 2'-(4,5-diphenyl-2-oxazolyl)-[1,1'-biphenyl-3-ol].
The intermediate 3-[4-(4,5-diphenyl-2-oxazolyl)-[1-methylpyrazolyl]phenol.
The intermediate 1-[3-hydroxyphenyl]-2-[(dimethylamino)methylene]-2-(4,5-diphenyl-2-oxazoly l)ethanone.
The intermediate 1,1-dimethylethyl-[3-[3-[(dimethylamino)methylene]-2-(4,5-diphenyl-2-oxazo lyl)-1-oxo-2-propenyl]phenoxy]acetate.
The intermediate 2-[5-(3-methyoxyphenyl)-4-oxazolyl]-4,5-diphenyloxazole.
The intermediate 3-[4-(4,5-diphenyl-2-oxazolyl)-2-methyl-5-oxazolyl]phenol.
The intermediate 1,1-dimethylethyl-[3-[4-(4,5-diphenyl-2-oxazolyl)-5-pyrazolyl]phenoxy]acet ate.
Dependencies are inferred from the claim text.