IL40711A

IL40711A - 2,4-diamino-5-(3-alkoxy-4,5-methylenedioxybenzyl)pyrimidines,their manufacture and pharmaceutical compositions containing them

Info

Publication number: IL40711A
Application number: IL40711A
Authority: IL
Original assignee: Sparamedica Ag
Priority date: 1971-12-01
Filing date: 1972-10-31
Publication date: 1976-04-30
Also published as: FI55654C; HU164442B; IE37224L; ES409124A1; IL40711A0; AR199887A1; DK131150C; ZA727692B; PH10165A; DK131150B; IE37224B1; PH11029A; FI55654B

Claims

Having now particularly described and ascertained the nature of our said invention and in what manner the same is to be performed, we declare that what we claim is:

1. A process for the manufacture of compounds of the general formula wherein R is lower alkoxy, and addition salts thereof with pharmaceutically acceptable acids, comprising reacting a compound of the general formula wherein R is as above and is C-^-C^-alkyl, with guanidine, and if desired, converting the basic reaction product into an acid addition salt with a pharmaceutically acceptable acid.

2. A process according to Claim 1, wherein R is methoxy.

3. A process according to Claim 1, wherein R is ethoxy. 40711/2

4. Process according to claim 1 for the preparation of "benzylpyrimidines as hereinbefore particularly described, especially with reference to the foregoing Examples.

5. Process for the manufacture of preparations having antibacterial properties, characterized in that one part of a compound of the general formula • wherein R is lower alkoxy, or an acid addition salt thereof with a pharmaceutically acceptible acid^is mixed, as active substance, with about 1 > about 50 parts of a sulfonamide or a salt thereof with a pharmaceutically acceptible base, or of a penicillin or oxytetracycline, and with non-toxic, inert, therapeutically compatible solid or liquid carriers, commonly used in such preparations, and/or excipients.

6. A therapeutic antibacterial composition comprising from about 1 to about 50 parts of a sulfonamide or salts thereof with pharmaceutically acceptable bases and one part of a pyrimidine of the formula 40711/2 . r R wherein R is lower alkoxy, or acid addition salts thereof with pharmaceutically acceptable acids, and a carrier.

7. A composition according to claim 6, wherein the sulfonamide is N1-(3*4-dimethyl-5-isoxazolyl) sulfonamide.

8. A therapeutic antibacterial composition comprising from about 1 to about 50 parts of a penicillin or oxytetracycline and one part of a pyrimidine of the formula wherein R is lower alkoxy, or acid addition salts thereof with pharmaceutically acceptable acids, and a carrier.

9. A composition in accordance with claim 8, wherein the antibiotic is oxytetracycline.

10. A compound of the formula wherein R is lower alkoxy, or addition salts thereof with pahrmaceutically acceptable acids, whenever prepared according to the process of claim 1 or by an obvious chemical equivalent thereof.

11. 2, -Diamino-5- (3-methoxy- , 5-methylenedioxybenzyl ) pyrimidine, whenever prepared according to the process of claim 1 or 2 or by an obvious chemical equivalent thereof.

12. 2> -Diamino-5-(3-ethoxy- ,5-methylenedioxybenzyl) pyrimidine, whenever prepared according to the process of claim 1 or or by an obvious chemical equivalent thereof. 40711/2 A

13. A compound of the formula wherein R is lower alkoxy, or addition salts thereof with pharmaceutically acceptable acids.

14. 2,4-Diamino-5-(3-methoxy-4,5-methylenedioxybenzyl) pyrimidine.

15. 2,4-Diamino-5- (5-ethoxy-4, 5-methylenedioxybenzyl) pyrimidine.