Claims
- 1. A method for preventing gastro-intestinal ulcer in mammals undergoing anti-inflammatory treatment with a non-steroidal anti-inflammatory agent, which comprises orally administering a gastro-intestinal ulcer preventing effective amount of a quinazolinone of the formula, ##STR3## wherein R.sub.1 is C.sub.1-3 alkyl, cyclopropylmethyl or 2,2,2-trifluoroethyl, R.sub.2 is halogen, C.sub.1-3 alkyl or C.sub.1-3 alkoxy, and R.sub.3 is phenyl or thienyl, or a non-toxic pharmaceutically acceptable salt thereof, in combination with an anti-inflammatorily effective amount of the anti-inflammatory agent.
- 2. The method according to claim 1, wherein the quinazolinone is 1-cyclopropylmethyl-4-phenyl-6-chloro-2(1H)-quinazolinone.
- 3. The method according to claim 1, wherein the quinazolinone is 1-cyclopropylmethyl-4-phenyl-6-methoxy-2(1H)-quinazolinone.
- 4. The method according to claim 1, wherein the quinazolinone is 1-(2,2,2,-trifluoroethyl)-4-phenyl-6-chloro-2(1H)-quinazolinone.
- 5. The method according to claim 1, wherein the quinazolinone is 1-(2,2,2-trifluoroethyl)-4-phenyl-6-methoxy-2(1H)-quinazolinone.
- 6. The method according to claim 1, wherein the non-steroidal anti-inflammatory agent is a member selected from the group consisting of indolylacetic acid derivatives, anthranilic acid derivatives and pyrazole derivatives.
- 7. The method according to claim 6, wherein the indolylacetic acid derivative is a member selected from the group consisting of indomethacin, 1-cinnamoyl-5-methoxy-2-methyl-3-indolylacetic acid and 1-(3,4-methylenedioxybenzoyl)-5-methoxy-2-methyl-3-indolylacetic acid.
- 8. The method according to claim 6, wherein the anthranilic acid derivative is a member selected from the group consisting of mefenamic acid and flufenamic acid.
- 9. The method according to claim 6, wherein the pyrazole derivative is phenylbutazone.
- 10. A pharmaceutical composition for preventing gastro-intestinal ulcer caused by a non-steroidal anti-inflammatory agent when administered orally to mammals, comprising a pharmaceutically acceptable carrier or diluent and a gastro-intestinal ulcer preventing effective amount of a quinazolinone of the formula, ##STR4## wherein each of R.sub.1, R.sub.2 and R.sub.3 is as defined in claim 1 or a non-toxic pharmaceutically acceptable salt thereof and an anti-inflammatorily effective amount of the said anti-inflammatory agent.
- 11. The composition according to claim 10, wherein the quinazolinone is 1-cyclopropylmethyl-4-phenyl-6-chloro-2(1H)-quinazolinone.
- 12. The composition according to claim 10, wherein the quinazolinone is 1-cyclopropylmethyl-4-phenyl-6-methoxy-2(1H)-quinazolinone.
- 13. The composition according to claim 10, wherein the quinazolinone is 1-(2,2,2-trifluoroethyl)-4-phenyl-6-chloro-2(1H)-quinazolinone.
- 14. The composition according to claim 10, wherein the quinazolinone compound is 1-(2,2,2-trifluoroethyl)-4-phenyl-6-methoxy-2(1H)-quinazolinone.
- 15. The composition according to claim 10, wherein the non-steroidal anti-inflammatory agent is a member selected from the group consisting of indolylacetic acid derivatives, anthranilic acid derivatives and pyrazole derivatives.
- 16. The composition according to claim 15, wherein the indolylacetic acid derivative is a member selected from the group consisting of indomethacin, 1-cinnamoyl-5-methoxy-2-methyl-3-indolylacetic acid and 1-(3,4-methylenedioxybenzoyl)-5-methoxy-2-methyl-3-indolylacetic acid.
- 17. The composition according to claim 15, wherein the anthranilic acid derivative is a member selected from the group consisting of mefenamic acid and flufenamic acid.
- 18. The composition according to claim 15, wherein the pyrazole derivative is phenylbutazone.
- 19. The composition according to claim 10, wherein the weight ratio of the quinazolinone or its salt to the non-steroidal anti-inflammatory agent is within a range of from about 20:1 to about 1:5.
- 20. A method according to claim 1, wherein the quinazolinone is 1-methyl-4-phenyl-6-chloro-2(1H)-quinazolinone.
- 21. A method according to claim 1, wherein the quinazolinone is 1-ethyl-4-phenyl-6-chloro-2(1H)-quinazolinone.
- 22. The method according to claim 1, wherein the quinazolinone is 1-cyclopropylmethyl-4-phenyl-7-methyl-2(1H)-quinazolinone.
- 23. A method according to claim 1, wherein the quinazolinone is 1-cyclopropylmethyl-4-phenyl-7-methoxy-2(1H)-quinazolinone.
- 24. A method according to claim 1, wherein the quinazolinone is 1-cyclopropylmethyl-4-(2-thienyl)-6-methoxy-2(1H)-quinazolinone.
- 25. The composition according to claim 10, wherein the quinazolinone is 1-methyl-4-phenyl-6-chloro-2(1H)-quinazolinone.
- 26. The composition according to claim 10, wherein the quinazolinone is 1-ethyl-4-phenyl-6-chloro-2(1H)-quinazolinone.
- 27. The composition according to claim 10, wherein the quinazolinone is 1-cyclopropylmethyl-4-phenyl-7-methyl-2(1H)-quinazolinone.
- 28. The composition according to claim 10, wherein the quinazolinone is 1-cyclopropylmethyl-4-phenyl-7-methoxy-2(1H)-quinazolinone.
- 29. The composition according to claim 10, wherein the quinazolinone is 1- cyclopropylmethyl-4-(2-thienyl)-6-methoxy-2(1H)-quinazolinone.
Parent Case Info
This is a continuation of application Ser. No. 589,573 filed June 23, 1975, now abandoned.
US Referenced Citations (4)
Number |
Name |
Date |
Kind |
3712892 |
Inaba et al. |
Jan 1973 |
|
3812118 |
Yamamoto et al. |
May 1974 |
|
3859237 |
Inaba et al. |
Jan 1975 |
|
3937801 |
Lippmann |
Feb 1976 |
|
Non-Patent Literature Citations (1)
Entry |
Cutting-Handbook of Pharmacology, 4th Ed., pp. 618-625, (1969). |
Continuations (1)
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Number |
Date |
Country |
Parent |
589573 |
Jun 1975 |
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