3,7-dithiaprostanoic acid derivative
AssigneeOno Pharmaceutical Co., Ltd.
InventorsToru Maruyama, Shuichi Ohuchida
Life of this patent
Estimating the term…
Abstract
A 3,7-dithiaprostanoic acid derivative of the formula (I) ##STR1## (wherein R.sup.1 is OH, C1-4 alkoxy, NR.sup.6 R.sup.7 (wherein R.sup.6, R.sup.7 are H, C1-4);R.sup.2 is H, OH; R.sup.3 is (i)alkyl, alkenyl, alkynyl (ii) phenyl, cycloalkyl (iii) alkyl, alkenyl, alkynyl substituted by phenyl, cycloalkyl (when R.sup.2 is H, alkyl, alkenyl, alkynyl in (i) or (iii) may be substituted by OH) possesses a binding activity for PGE.sub.2 receptor (especially for EP4). Therefore they are useful for the treatment and/or prevention of immunologic diseases (autoimmune diseases, immunological deficiency diseases, organ transplantation etc.), asthma, abnormal bone formation, neuronal cell death, liver damage, nephritis, hypertension, myocardiac ischemia etc.
Claims12
A 3,7-dithiaprostanoic acid derivative of the formula (I):
- ##STR302## (wherein R.sup.1 is hydroxy, C1-4 alkoxy or a group of the formula:
- --NR.sup.6 R.sup.7
- wherein R.sup.6 and R.sup.7, independently, are hydrogen atom or C1-4 alkyl,
- R.sup.2 is hydrogen atom or hydroxy,
- R.sup.3 is
- (i) C1-8 alkyl, C2-8 alkenyl or C2-8 alkynyl,
- (ii) phenyl or C3-7 cycloalkyl,
- (iii) C1-8 alkyl, C2-8 alkenyl or C2-8 alkynyl substituted by phenyl or C3-7 cycloalkyl,
- with the proviso that, alkyl, alkenyl, alkynyl in (i) or (iii) may be substituted by one hydroxy group, when R.sup.2 is hydrogen atom;
- the symbol -- is a double or single bond;
- the formula including 8-epi equilibrium compound thereof);
- a non-toxic salt thereof or a cyclodextrin clathrate thereof.
An intermediate of the formula (II):
- ##STR303## (wherein R.sup.2a is hydrogen atom or hydroxy protected by a protecting group which is eliminated under an acidic condition, R.sup.20 is a protecting group which is eliminated under an acidic condition, R.sup.3a is (I) C1-8 alkyl, C2-8 alkenyl or C2-8 alkynyl, (ii) phenyl or C3-7 cycloalkyl, (iii) C1-8 alkyl, C2-8 alkenyl or C2-8 alkynyl which are substituted by phenyl or C3-7 cycloalkyl (with the proviso that when R.sup.2a is hydrogen, alkyl, alkenyl and alkynyl groups in (I) or (iii) may be substituted by one hydroxy protected by a protecting group which is eliminated under an acidic condition);
- the symbol:
- ##STR304## is a double or single bond).
Dependencies are inferred from the claim text.