Pyrazol-1-yl phenoxyacetic acid compounds which have useful phar

Details Pyrazol-1-yl phenoxyacetic acid compounds which have useful phar Pyrazol-1-yl phenoxyacetic acid compounds which have useful phar

1993-03-01

1995-01-03

Ivy, C. Warren

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514341, 514406, 546256, 546279, 5483751, 5483761, C07D23112, A61K 31415

Patent

active

053787161

ABSTRACT:
We proposed a novel compound having an activity of PGI.sub.2 receptor agonist.
A phenoxyacetic acid derivative of the formula ##STR1## A is --C(R.sup.1).dbd.N.about.OR.sup.2, --CH(R)NH--OR.sup.2, --COE, --SO.sub.2 E, --CH.sub.2 --NR.sup.3 --Y, --Z -- NR.sup.3 --CONR.sup.4 R.sup.5, --CH.sub.2 --OR.sup.6, --CO.sub.2 R.sup.6, --CH.sub.2 --O.about.N.dbd.CR.sup.7 R.sup.8, --CH.sub.2 --O--NHCHR.sup.7 R.sup.8, substituted by imidazolyl(methyl), pyrazolylmethyl, oxazolyl(methyl), thioxazolyl, isoxazolyl, isothiazolyl, oxadiazolyl, triazolylmethyl;
T is alkylene, alkenylene, etc.;
D is --CO.sub.2 R.sup.10, --CONR.sup.11 R.sup.12 ;
E is (substitution) amino, hydradino;
Y is substituted (thio) carbonyl, substituted sulfonyl;
Z is --CH.dbd.N--, --CH.sub.2 NR.sup.3 --;
R.sup.1, R.sup.3, R.sup.10 -R.sup.13 is each H or alkyl, etc.;
R.sup.2, R.sup.4 -R.sup.9 is each H, alkyl or alkyl substituted by phenyl or hetero ring, etc. and non-toxic salts thereof, non-toxic acid addition salts thereof, possess an agonistic on PGI.sub.2 receptor, so it is useful for prevention and/or treatment of thrombosis, arteriosclosis, ischemic heart diseases, gastric ulcer and hypertention.

REFERENCES:
patent: 3585199 (1971-06-01), Cragoe et al.
patent: 4278678 (1981-07-01), Hamazaki et al.
patent: 4632934 (1986-12-01), Iizuka
patent: 4911863 (1990-03-01), Sage et al.
patent: 4956379 (1990-09-01), Meanwell
patent: 5011851 (1991-04-01), Meanwell
patent: 5021415 (1991-06-01), Meanwell
Nature, vol. 263, Oct. 21, 1976, pp. 663-665, "An enzyme isolated from Arteries transforms prostaglandin endoperoxides to an unstable substance that inhibits platelet aggregation", S. Moncado et al.
Prostaglandins, vol. 12, No. 5, Nov. 1976, pp. 685-713, "Arterial Walls Are Protected Against Deposition of Platelet Thrombi by a Substance (Prostaglandin X) Which They Make . . . Endoperoxides".
Prostaglandins, vol. 12, No. 6, Dec. 1976, pp. 915-929, "The Chemical Structure of Prostaglandin X (Prostacyclin)", Roy A. Johnson et al.
Prostaglandins, vol. 12, No. 13, Mar. 1977, pp. 375-389, "Modulation of Human Platelet Adenylate Cyclase by Prostacyclin (PGX)", R. R. Gorman et al.
Chemical & Engineering News, Dec. 20, 1976, pp. 17-19, Science, "New compound shakes up Prostaglandin ideas".
Br. J. Pharmac., vol. 76, 1982, pp. 423-438, "Antagonism of the Thromboxane-Sensitive Contractile Systems of the Rabbit Aorta, Dog Saphenous Vein and Guinea-Pig Trachea", R. L. Jones et al.
Br. J. Pharmac., vol. 84, 1985, pp. 595-607, "Competitive Antagonism at Thromboxane Receptors in Human Platelets", Roma A. Armstrond et al.
Br. J. Pharac., vol. 102, 1991, pp. 251-259, "Octimibate, A Potent Non-Prostanoid Inhibitor of Platelet Aggregation, Acts Via the Prostacyclin Receptor", Janet E. Merritt et al.

Affiliated with

Also associated with

Rating

Pyrazol-1-yl phenoxyacetic acid compounds which have useful phar does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Pyrazol-1-yl phenoxyacetic acid compounds which have useful phar, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Pyrazol-1-yl phenoxyacetic acid compounds which have useful phar will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-2211724