US 5,703,099 A · Phenoxyacetic acid derivatives

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, arteriosclerosis, ischemic heart diseases, gastric ulcer and hypertension.

Claims7

Dependent claims

A phenoxyacetic acid compound of the formula (I):

##STR153## wherein A is ##STR154## T is i) single bond,
ii) C1-6 alkylene,
iii) C2-6 alkenylene or
iv) --O--(CH.sub.2).sub.s --;
D is
i) --CO.sub.2 R.sup.10 or
ii) --CONR.sup.11 R.sup.12 ;
R.sup.9 is
i) hydrogen,
ii) phenyl,
iii) C1-4 alkyl or
iv) C1-4 alkyl substituted by one or two of phenyl or 4-7 membered monocyclic hetero ring containing one nitrogen;
R.sup.10 is hydrogen or C1-12 alkyl;
R.sup.11 and R.sup.12 each, independently, is hydrogen or C1-4 alkyl or
R.sup.11 and R.sup.12, taken together with nitrogen bond to R.sup.11 and R.sup.12 is the residue of an amino acid;
R.sup.13 is hydrogen, C1-4 alkyl, C1-4 alkoxy or nitro;
n is 1-2,
s is 2-4;
and the rings of the phenyl or the hetero ring of R.sup.9 may also be substituted by one to three of C1-C4 alkyl, C1-C4 alkoxy, halogen, nitro or trihalomethyl;
or a non-toxic salt thereof or a non-toxic acid addition salt thereof.

17 more elements

Dependencies are inferred from the claim text.

Phenoxyacetic acid derivatives

Life of this patent

Phenoxyacetic acid derivatives

Life of this patent

Abstract

Claims7