Pyrimidine compounds as antagonists of SRS-A
OwnerKiyoshi Murase, Toshiyasu Mase +2inventors
InventorsKiyoshi Murase, Toshiyasu Mase, Hiromu Hara, Kenichi Tomioka
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Abstract
Novel heterocyclic compounds shown by the general formula ##STR1## or the pharmaceutically acceptable salts thereof useful as medicament in particular as antagonist of slow reacting substance of anaphylaxis(SRS-A).
Claims11
A heterocyclic compound represented by the following formula (I) ##STR114## or a salt thereof;
- wherein R.sup.1 represents a lower alkanoyl group;
- R.sup.2 represents a lower alkyl group;
- A represents a lower alkylene group which may be substituted by a hydroxy group;
- Y represents an oxygen atom, a sulfur atom, a carbonylimino group, or an iminocarbonyl group;
- represents a pyrimidine ring;
- R.sup.3, R.sup.4 and R.sup.5, which may be the same or different, each represents a hydrogen atom, a lower alkyl group, a group shown by the formula --A.sup.1 --R.sup.6 (wherein A.sup.1 represents a lower alkylene group and R.sup.6 represents a hydroxy group, a mercapto group, a carboxy group or a lower alkoxycarbonyl group), a hydroxy group, a mercapto group, a lower alkoxy group, a lower alkylthio group, a group shown by the formula --Y.sup.1 --A.sup.2 --R.sup.7 (wherein Y.sup.1 represents an oxygen atom or a sulfur atom;
- A.sup.2 represents a lower alkylene group, and R.sup.7 represents a carboxy group, a lower alkoxycarbonyl group, a hydroxyaminocarbonyl group, a mono- or di-lower alkylaminocarbonyl group or an N-lower alkyl-hydroxyaminocarbonyl group), an oxo group, a thioxo group, an amino group, a group shown by the formula --NH--R.sup.8 (wherein R.sup.8 represents a carboxy lower alkyl group or a lower alkoxycarbonyl lower alkyl group), a group shown by the formula --NH--CO--R.sup.9 (wherein R.sup.9 represents a carboxy-lower alkyl group, a lower alkoxycarbonyl lower alkyl group, a carboxy group or a lower alkoxycarbonyl group), a carboxy group or a group shown by the formula --CO--R.sup.10 (wherein R.sup.10 represents a lower alkoxy group).
A pharmaceutical composition useful as an antagonist of slow reacting substance of anaphylaxis (SRS-A) and containing as an individual adult dose amount, from 0.1 to 500 mg. of a heterocyclic ring compound represented by the formula (I) ##STR115## or a pharmaceutically acceptable salt thereof wherein R.sup.1 represents a lower alkanoyl group;
- R.sup.2 represents a lower alkyl group;
- A represents a lower alkylene group which may be substituted by a hydroxyl group;
- Y represents oxygen, sulfur, a carbonylimino group (--CONH--), or an iminocarbonyl group (--NHCO--);
- represents a pyrimidine ring;
- R.sup.3, R.sup.4 and R.sup.5, which may be the same or different, each represents a hydrogen atom, a lower alkyl group, a group shown by the formula --A.sup.1 --R.sup.6 (wherein A.sup.1 represents a lower alkylene group, R.sup.6 represents a hydroxyl group, a mercapto group, a carboxy group or a lower alkoxycarbonyl group), a hydroxyl group, a mercapto group, a lower alkoxy group, a lower alkylthio group, a group shown by the formula --Y.sup.1 --A.sup.2 --R.sup.7 (wherein Y.sup.1 represents oxygen or sulfur, A.sup.2 represents a lower alkylene group, R.sup.7 represents a carboxy group, a lower alkoxycarbonyl group, a hydroxyaminocarbonyl group, a mono- or di-lower alkylaminocarbonyl group or an N-lower alkyl-hydroxyaminocarbonyl group), an oxo group (.dbd.O), a thioxo group (.dbd.S), an amino group, a group shown by the formula --NH--R.sup.8 wherein R.sup.8 represents a carboxy lower alkyl group or a lower alkoxycarbonyl lower alkyl group), a group shown by the formula --NH--CO--R.sup.9 (wherein R.sup.9 represents a carboxy-lower alkyl group, a lower alkoxycarbonyl lower alkyl group, a lower alkoxypheny lower alkoxycarbonyl lower alkyl group, a carboxy group or a lower alkoxycarbonyl group), a carboxy group or a group shown by the formula --CO--R.sup.10 (wherein R.sup.10 represents a lower alkoxy group).
A pharmaceutical composition containing a heterocyclic ring compound represented by the general formula (I) ##STR116## or a pharmaceutically acceptable salt thereof wherein R.sup.1 represents an acyl group;
- R.sup.2 represents a lower alkyl group;
- A represents a lower alkylene group which may be substituted by hydroxyl group;
- Y represents an oxygen atom, a sulfur atom, a carbonylimino group (--CONH--), or an iminocarbonyl group (--NHCO--);
- represents a pyrimidine ring R.sup.3, R.sup.4 and R.sup.5, which may be the same or different, each represents a hydrogen atom, a lower alkyl group, a group shown by the formula --A.sup.1 --R.sup.6 (wherein A.sup.1 represents a lower alkylene group, R.sup.6 represents a hydroxyl group, a mercapto group, a carboxy group or a lower alkoxycarbonyl group), a hydroxyl group, a mercapto group, a lower alkoxy group, a lower alkylthio group, a group shown by the formula --Y.sup.1 --A.sup.2 --R.sup.7 (wherein Y.sup.1 represents an oxygen atom or a sulfur atom, A.sup.2 represents a lower alkylene group, R.sup.7 represents a carboxy group, a lower alkoxycarbonyl group, a hydroxyaminocarbonyl group, mono- or di-lower alkylaminocarbonyl group or N-lower alkyl-hydroxyaminocarbonyl group), an oxo group (.dbd.O), a thioxo group (.dbd.S), an amino group, a group shown by the formula --NH--R.sup.8 (wherein R.sup.8 represents a carboxy lower alkyl group or a lower alkoxycarbonyl lower alkyl group), a group shown by the formula --NH--CO--R.sup.9 (wherein R.sup.9 represents a carboxy-lower alkyl group, a lower alkoxycarbonyl lower alkyl group, a lower alkoxyphenyl lower alkoxycarbonyl lower alkyl group, a carboxy group or a lower alkoxycarbonyl group), a carboxy group or a group shown by the formula --CO--R.sup.10 (wherein R.sup.10 represents a lower alkoxy group).
Dependencies are inferred from the claim text.