Claims
- 1. A 1,2-dithiole of the formula: ##STR11## wherein Het represents pyrimidin-2-yl, pyrimidin-4-yl, or pyrimidin-5-yl, or a said pyrimidin-2-yl, pyrimidin-4-yl or pyrimidin-5-yl substituted by halogen, alkyl of 1 through 4 carbon atoms, alkoxy of 1 through 4 carbon atoms, mercapto, alkylthio of 1 through 4 carbon atoms, or dialkylamino having 1 through 4 carbon atoms in each alkyl, and R represents halogen, alkyl of 1 through 4 carbon atoms, alkyl of 1 through 4 carbon atoms substituted by alkoxycarbonyl having 1 through 4 carbon atoms in the alkoxy, carboxy, alkoxycarbonyl having 1 through 4 carbon atoms in the alkoxy, carbamoyl, N-alkylcarbamoyl having 1 through 4 carbon atoms in the alkyl, or R.sub.1 --CH(OH)-- in which R.sub.1 represents hydrogen or alkyl of 1 through 3 carbon atoms.
- 2. A dithiole according to claim 1 wherein Het represents pyrimidin-2-yl, pyrimidin-4-yl, or pyrimidin-5-yl, or pyrimidin-2-yl, pyrimidin-4-yl, or pyrimidin-5-yl substituted by halogen, alkyl of 1 through 4 carbon atoms, alkoxy of 1 through 4 carbon atoms, alkylthio of 1 through 4 carbon atoms, or dialkylamino having 1 through 4 carbon atoms in each alkyl, and R represents alkyl of 1 through 4 carbon atoms, carboxy, alkoxycarbonyl having 1 through 4 carbon atoms in the alkoxy, carbamoyl, or N-alkylcarbamoyl having 1 through 4 carbon atoms in the alkyl.
- 3. A dithiole derivative according to claim 1 wherein Het represents pyrimidin-2-yl, pyrimidin-4-yl, or pyrimidin-5-yl, or pyrimidin-2-yl, pyrimidin-4-yl or pyrimidin-5-yl substituted by halogen, alkyl of 1 through 4 carbon atoms, alkylthio of 1 through 4 carbon atoms, or dialkylamino having 1 through 4 carbon atoms in each alkyl, and R represents alkyl of 1 through 4 carbon atoms, alkoxycarbonyl having 1 through 4 carbon atoms in the alkoxy, or R.sub.1 --CH(OH)-- in which R.sub.1 represents hydrogen or alkyl of 1 through 3 carbon atoms.
- 4. A 1,2-dithiole according to claim 1 which is 4-ethyl-5-(pyrimidin-5-yl)-1,2-dithiole-3-thione.
- 5. A 1,2-dithiole according to claim 1 which is 4-methyl-5-(5-methylthiopyrimidin-4-yl)-1,2-dithiole-3-thione.
- 6. A 1,2-dithiole according to claim 1 which is 5-(5-chloropyrimidin-4-yl)-4-methyl-1,2-dithiole-3-thione.
- 7. A pharmaceutical anti-bilharzia composition which consists essentially of an effective amount of a 1,2-dithiole as claimed in claim 1 in association with one or more compatible and pharmaceutically acceptable diluents or adjuvants.
Priority Claims (2)
Number |
Date |
Country |
Kind |
76 03604 |
Feb 1976 |
FRX |
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76 38901 |
Dec 1976 |
FRX |
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Parent Case Info
This is a division of application Ser. No. 766,966 filed Feb. 9, 1977, now U.S. Pat. No. 4,110,450.
US Referenced Citations (1)
Number |
Name |
Date |
Kind |
3979388 |
Krenzer |
Sep 1976 |
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Foreign Referenced Citations (1)
Number |
Date |
Country |
1526768 |
Nov 1963 |
FRX |
Non-Patent Literature Citations (3)
Entry |
"The Chemistry of Heterocyclic Compounds", vol. 21, First Part, pp. 382-384 (1966). |
Bottcher et al., Chem. Ber. 84, pp. 458-463 (1951). |
Legrand et al., Bull. Soc. Chim, France, pp. 79-83 (1955). |
Divisions (1)
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Number |
Date |
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Parent |
766966 |
Feb 1977 |
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