Phenylacetic acid compounds in treating abnormal platelet aggregation
AssigneeMerck & Co., Inc.
InventorsTsung-Ying Shen, Jorge P. Li, Conrad P. Dorn, Jr.
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Abstract
Pharmaceutical Compositions based on 4-(Benzoxazol-2-yl)phenylacetic acids, alcohols, esters, amides and their non-toxic pharmaceutically acceptable salts and method of treating abnormal platelet aggregation.
Claims24
A method for treating a condition exhibiting abnormal platelet aggregation which comprises the administration to humans and animals of a therapeutically effective amount of a compound having the formula:
- ##SPC7##
- or a pharmaceutically acceptable salt thereof, wherein
- R.sub..alpha. is hydrogen or methyl;
- R'.sub..alpha. is hydrogen, or R.sub..alpha. and R'.sub..alpha. taken together can be methylene:
- of R'.sub..alpha. can be a methylene linkage attached to the unsubstituted ortho position of the benzenoid ring;
- X, y, r.sub.2 and R.sub.3 are the same or different and each is hydrogen, C.sub.1-5 alkyl, chloro, bromo, fluoro;
- and
- R.sub.4 is COOH;
- COOR, wherein R may be C.sub.1-5 alkyl, CONH.sub.2, ##EQU2## where Y may be C.sub.1-3 alkyl.
A method of treating a condition exhibiting abnormal platelet aggregation which comprises the administration to humans and animals of a therapeutically effective amount of a compound having the formula:
- ##SPC9##
- or a pharmaceutically acceptable salt thereof, wherein
- R.sub..alpha. is hydrogen or methyl;
- R.sub.2, r.sub.3, x and Y are each hydrogen, chloro, bromo, or fluoro;
- and
- R.sub.4 is COOH;
- Coor, where R may be C.sub.1-5 alkyl, CONH.sub.2 ;
- or ##EQU3## where Y may be C.sub.1-3 alkyl.
A pharmaceutical composition comprising a pharmaceutical carrier and an effective non-toxic amount of 0.1 to 50 mg per kilogram of body weight of a compound of the formula:
- ##SPC13##
- or pharmaceutically acceptable salt thereof, wherein
- R.sub..alpha. is hydrogen or methyl:
- R'.sub..alpha. is hydrogen, or R.sub..alpha. and R'.sub..alpha. taken together can be methylene;
- or R'.sub..alpha. can be a methylene linkage attached to the unsubstituted ortho position of the benzenoid ring;
- X, y, r.sub.2 and R.sub.3 are the same or different and each is hydrogen, C.sub.1-5 alkyl, chloro, bromo, fluoro, and
- R.sub.4 is COOH, COOR, where R may be C.sub.1-5 alkyl, CONH.sub.2, ##EQU4## where Y may be C.sub.1-3 alkyl.
A pharmaceutical composition comprising a pharmaceutical carrier and an effective non-toxic amount of a compound of the formula:
- ##SPC15##
- or pharmaceutically acceptable salt thereof, wherein
- R.sub..alpha. is hydrogen or methyl;
- R.sub.2, r.sub.3, x and Y are each hydrogen, chloro, bromo, or fluoro;
- and
- R.sub.4 is COOH;
- COOR, where R may be C.sub.1-5 alkyl, CONH.sub.2 ;
- or ##EQU5## where Y may be C.sub.1-3 alkyl.
Dependencies are inferred from the claim text.