Claims
- 1. A compound of formula (I) ##STR24## wherein R is
- (a) hydroxy;
- (b) a C.sub.1 -C.sub.6 alkoxy group unsubstituted or substituted by a ##STR25## group, wherein each of R.sub.4 and R.sub.5 independently is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group, or R.sub.4 and R.sub.5, taken together with the nitrogen atom to which they are linked, form an unsubstituted N-pyrrolidinyl or morpholino ring;
- R.sub.1 is a hydrogen atom or C.sub.1 -C.sub.6 alkyl;
- R.sub.2 is a hydrogen or a halogen atom or a C.sub.1 -C.sub.4 alkyl group;
- R.sub.3 is a 2-,3- or 4-pyridyl ring, each of which is unsubstituted or substituted by C.sub.1 -C.sub.6 alkyl; or R.sub.3 is a group of formula ##STR26## wherein each of R.sub.8, R.sub.9 and R.sub.10 independently represents hydrogen, halogen, trihalo-C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.4 -alkenyloxy, or a -(0).sub.p -R.sub.11 group, wherein p is zero or 1 and R.sub.11 represents a C.sub.1 -C.sub.6 alkyl group, and the pharmaceutically acceptable salts thereof.
- 2. A compound of formula (I), according to claim 1, wherein
- R is hydroxy, C.sub.1 -C.sub.4 alkoxy, di(C.sub.1 -C.sub.2 alkyl)amino-ethoxy;
- R.sub.1 is hydrogen;
- R.sub.2 is hydrogen, chlorine, bromine or C.sub.1 -C.sub.3 alkyl; and
- R.sub.3 is
- (a") a phenyl group unsubstituted or substituted by one or two substituents chosen from the group including fluorine, chlorine, C.sub.1 -C.sub.4 alkyl, and C.sub.1 -C.sub.4 alkoxy;
- (b") a 2-, 3- or 4-pyridyl group, each of which unsubstituted or substituted by a methyl group; and the pharmaceutically acceptable salts thereof.
- 3. A compound selected from the group consisting of:
- 6-chloro-7-trans-(2-phenyl-ethenyl)-5-oxo-5H-thiazolo[3,2-a]pyrimidine-2-carboxylic acid;
- 6-methyl-7-trans-[2-(2-methyl-phenyl)-ethenyl]-5-oxo-5H-thiazolo[3,2-a]pyrimidine-2-carboxylic acid;
- 6-methyl-7-trans-[2-(4-methyl-phenyl)-ethenyl]-5-oxo-5H-thiazolo[3,2-a]pyrimidine-2-carboxylic acid;
- 6-methyl-7-trans-[2-(3-pyridyl)-ethenyl]-5-oxo-5H-thiazolo[3,2-a]pyrimidine-2-carboxylic acid;
- 6-methyl-7-trans-[2-(3-methyl-phenyl)-ethenyl]-5-oxo-5H-thiazolo[3,2-a]pyrimidine-2-carboxylic acid;
- 6-methyl-7-trans-[2-(4-ethoxy-phenyl)-ethenyl]-5-oxo-5H-thiazolo[3,2-a]pyrimidine-2-carboxylic acid;
- 6-chloro-7-trans-[2-(3-methyl-phenyl)-ethenyl]-5-oxo-5H-thiazolo[3,2-a]pyrimidine-2-carboxylic acid;
- 6-chloro-7-trans-[2-(2-methyl-phenyl)-ethenyl]-5-oxo-5H-thiazolo[3,2-a]pyrimidine-2-carboxylic acid;
- 6-chloro-7-trans-[2-(2,4-dimethyl-phenyl)-ethenyl]-5-oxo-5H-thiazolo[3,2-a]pyrimidine-2-carboxylic acid;
- 6-chloro-3-phenyl-7-trans-(2-phenyl-ethenyl)-5-oxo-5H-thiazolo[3,2-a]pyrimidine-2-carboxylic acid;
- 6-chloro-3-methyl-7-trans-(2-phenyl-ethenyl)-5-oxo-5H-thiazolo[3,2-a]pyrimidine-2-carboxylic acid;
- 6-chloro-7-trans-[2-(4-methyl-phenyl)-ethenyl]-5-oxo-5H-thiazolo[3,2-a]pyrimidine-2-carboxylic acid;
- 6-chloro-7-trans-[2-(4-fluoro-phenyl)-ethenyl]-5-oxo-5H-thiazolo[3,2-a]pyrimidine-2-carboxylic acid;
- 6-bromo-7-trans-(2-phenyl-ethenyl)-5-oxo-5H-thiazolo[3,2-a]pyrimidine-2-carboxylic acid;
- 6-chloro-7-trans-[2-(2-methoxy-3-ethoxy-phenyl)-ethenyl]-5-oxo-5H-thiazolo[3,2-a]pyrimidine-2-carboxylic acid;
- 6-chloro-7-trans-[2-(2,5-dimethyl-phenyl)-ethenyl]-5-oxo-5H-thiazolo[3,2-a]pyrimidine-2-carboxylic acid;
- 6-chloro-7-trans-[2-(4-chloro-phenyl)-ethenyl]-5-oxo-5H-thiazolo[3,2-a]pyrimidine-2-carboxylic acid;
- 6-methyl-7-trans-[2-(2,4-dimethyl-phenyl)-ethenyl]-5-oxo-5H-thiazolo[3,2-a]pyrimidine-2-carboxylic acid;
- 6-methyl-7-trans-[2-(2-methoxy-3-ethoxy-phenyl)-ethenyl]-5-oxo-5H-thiazolo[3,2-a]pyrimidine-2-carboxylic acid;
- 6-methyl-7-trans-[2-(2,5-dimethyl-phenyl)-ethenyl]-5-oxo-5H-thiazolo[3,2-a]pyrimidine-2-carboxylic acid;
- 6-methyl-7-trans-[2-(2,6-dichloro-phenyl)-ethenyl]-5-oxo-5H-thiazolo[3,2-a]pyrimidine-2-carboxylic acid;
- 6-methyl-7-trans-[2-(4-chloro-phenyl)-ethenyl]-5-oxo-5H-thiazolo[3,2-a]pyrimidine-2-carboxylic acid;
- and the pharmaceutically acceptable salts thereof.
- 4. A pharmaceutical composition suitable for use as an anti-allergic agent, said composition comprising a therapeutically effective amount of a compound as claimed in claim 1, in association with a pharmaceutically acceptable carrier or diluent.
- 5. A pharmaceutical composition suitable for use as an anti-allergic agent, said composition comprising a therapeutically effective amount of a compound as claimed in claim 2, in association with a pharmaceutically acceptable carrier or diluent.
- 6. A pharmaceutical composition suitable for use as an anti-allergic agent, said composition comprising a therapeutically effective amount of a compound as claimed in claim 3, in association with a pharmaceutically acceptable carrier or diluent.
Priority Claims (1)
Number |
Date |
Country |
Kind |
8300728 |
Jan 1983 |
GBX |
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Parent Case Info
This is a divisional application of Ser. No. 569,693, filed Jan. 11, 1985, now U.S. Pat. No. 4,558,046.
US Referenced Citations (5)
Foreign Referenced Citations (1)
Number |
Date |
Country |
1334628 |
Oct 1973 |
GBX |
Divisions (1)
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Number |
Date |
Country |
Parent |
569693 |
Jan 1985 |
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