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Title: Lactum drug compositions



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Claims: We claim:

1. A pharmaceutical composition having therapeutic properties as sedative and hypnotics comprising a compound of the general formula ##STR9## wherein R is a hydrogen atom or an alkyl radical with 1 to 3 carbon atoms and m is 2, 3 or 4, in a therapeutically effective amount to induce sedation, and a pharmaceutically acceptable carrier.

2. The composition of claim 1 wherein in the formula R is hydrogen.

3. The composition of claim 1 wherein in the formula m is 2.

4. The composition of claim 1 wherein in the formula m is 3.

5. The composition of claim 1 wherein in the formula m is 4.

6. The composition of claim 1 wherein in the formula R is alkyl of 1 to 3.

7. The composition of claim 6 wherein in the formula m is 3.

8. The composition of claim 1 wherein the compound is selected from the group consisting of 3-(o-sulfobenzoic acid imido)-pyrrolidone-2, 3-(o-sulfobenzoic acid imido)-piperidone-2, alpha-(o-sulfobenzoic acid imido)-caprolactam, 1-methyl-3-(o-sulfobenzoic acid imido)-piperidone-2, 1-ethyl-3-(o-sulfobenzoic acid imido)-piperidone-2, 1-n-propyl-3-(o-sulfobenzoic acid imido)-piperidone-2, 1-i-propyl-3-(o-sulfobenzoic acid imido)-piperidone-2, and 1-methyl-3-(o-sulfobenzoic acid imido)-pyrrolidone-2.

9. The pharmaceutical composition of claim 1 wherein the compound is present in a therapeutically effective amount of from about 1 to about 500 mg/kg body weight.

10. The pharmaceutical composition of claim 9 wherein the therapeutically effective amount is from about 50 to about 200 mg/kg body weight.

11. The pharmaceutical composition of claim 9 wherein the therapeutically effective amount for daily application is from about 1 to about 100 mg/kg body weight administered one to three times daily.

12. The pharmaceutical composition of claim 11 wherein the therapeutically effective amount is from about 20 to about 50 mg/kg body weight administered one to three times daily.

13. The pharmaceutical composition of claim 8 wherein the compound is 3-(o-sulfobenzoic acid imido)-piperidone-2.

14. The pharmaceutical composition of claim 13 wherein 3-(o-sulfobenzoic acid imido)-piperidone-2 is present in a therapeutically effective amount of from about 1 to about 500 mg/kg body weight.

15. The pharmaceutical composition of claim 1 in suitable form of oral administration.

16. The method of inducing sedation in warm-blooded animals which comprises administering to said warm-blooded animals a pharmaceutical composition comprising a compound of the general formula ##STR10## wherein R is a hydrogen atom or an alkyl radical with 1 to 3 carbon atoms and m is 2, 3 or 4 in a controlled dosage effective to induce sedation.

17. The method of claim 16 wherein R is hydrogen.

18. The method of claim 16 wherein m is 2 to 4.

19. The method of claim 16 wherein R is alkyl of 1 to 3.

20. The method of claim 19 wherein m is 3.

21. The method of claim 16 wherein the compound is selected from the group consisting of 3-(o-sulfobenzoic acid imido)-pyrrolidone-2, 3-(sulfobenzoic acid imido)-piperidone-2, alpha-(o-sulfobenzoic acid imido)-caprolactam, 1-methyl-3-(o-sulfobenzoic acid imido)-piperidone-2, 1-ethyl-3-(o-sulfobenzoic acid imido)-piperidone-2, 1-n-propyl-3-(o-sulfobenzoic acid imido)-piperidone-2, 1-i-propyl-3-(o-sulfobenzoic acid imido)-pyrrolidone-2 and 1-methyl-3-(o-sulfobenzoic acid imido)-pyrrolidone-2.

22. The method of claim 16 wherein the controlled dosage effective to induce sedation is from about 1 to 500 mg/kg body weight.

23. The method of claim 22 wherein the controlled dosage effective to induce sedation is from about 50 to 200 mg/kg body weight.

24. The method of claim 16 wherein the controlled dosage effective to induce sedation for daily application is from about 1 to 100 mg/kg body weight administered one to three times daily.

25. The method of claim 24 wherein the controlled dosage to induce sedation of daily application is from about 20 to 50 mg/kg body weight administered one to three times daily.

26. The method of claim 21 wherein the compound is 3- (o-sulfobenzoic acid imido)-piperidone-2.

27. The method of claim 26 wherein the controlled dosage effective to induce sedation is from about 1 to 500 mg/kg body weight.

28. The method of claim 16 in which the compound is administered orally.
Other info:


Inventors: Graudums, Ivars (Rhineland, DT)
Muckter, Heinrich (Aachen, DT)
Frankus, Ernst (Stolberg-Busbach, DT)

Application Number: 640288
Filing Date: 1975-12-12
Publication_date: 1978-01-10
Assignee: Chemie Grunenthal GmbH (Stolberg, DT)
Primary Class(es): 514/321 514/212.08, 514/373
Other Classes:
US Patent Ref:
3314960Apr, 1967Freed et al.260/281.

Other Refs:
Primary Examiner: Friedman, Stanley J.
Assistant Examiner:
Attorney: Weiser, Stapler & Spivak