Claims
- 1. A pharmaceutical composition suitable for oral, parenteral or topical treatment of a susceptible fungal infection in man which comprises a pharmaceutical carrier and an antifungal amount of a compound of the formula ##STR27## where R is a phenyl group optionally substituted by 1 to 3 substituents each independently selected from halo, CF.sub.3, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 alkoxy;
- R.sup.1 is selected from (a) --SO.(C.sub.1 -C.sub.4 alkyl), (b) --SO.sub.2 (C.sub.1 -C.sub.4 alkyl), (c) --SO.sub.2 NR.sup.2 R.sup.3 where either R.sup.2 and R.sup.3 are both C.sub.1 -C.sub.4 alkyl, or R.sup.2 and R.sup.3 together with the N atom to which they are attached represent piperidino, (d) --NHSO.sub.2 (C.sub.1 -C.sub.4 alkyl) and (e) --CONR.sup.4 R.sup.5 where either R.sup.4 is H or C.sub.1 -C.sub.4 alkyl and R.sup.5 is C.sub.1 -C.sub.4 alkyl, or R.sup.4 and R.sup.5 together with the N atom to which they are attached represent piperidino; and
- n is 1 or 2; with the proviso that n is 2 when R.sup.1 is --NHSO.sub.2 (C.sub.1 -C.sub.4 alkyl);
- or a pharmaceutically acceptable or agriculturally acceptable acid addition salt thereof.
- 2. A composition according to claim 1, wherein R is phenyl substituted by 1 to 3 substituents which are each independently halo or CF.sub.3.
- 3. A composition according to claim 2, wherein R is phenyl substituted by 4-fluoro, 4-chloro, 4-bromo, 2,4-dichloro, 2,4-difluoro, 2,4,6-trifluoro or 4-bromo-2,5-difluoro.
- 4. A composition according to claim 3 wherein R is 2,4-dichloro.
- 5. A composition according to claim 4 wherein n is 1 and R.sup.1 is --SO(C.sub.1 -C.sub.4 alkyl), --SO.sub.2 --(C.sub.1 -C.sub.4 alkyl), or --SO.sub.2 NR.sup.4 R.sup.5.
- 6. The composition of claim 5 wherein R.sup.1 is --SOCH.sub.3.
- 7. The composition of claim 5 wherein R.sup.1 is --SO.sub.2 CH.sub.3.
- 8. The composition of claim 5 wherein R.sup.1 is ##STR28##
- 9. A composition according to claim 4 wherein n is 2 and R.sup.1 is --NHSO.sub.2 (C.sub.1 -C.sub.4 alkyl).
- 10. The composition of claim 9 wherein R.sup.1 is --NHSO.sub.2 CH.sub.3.
- 11. A composition according to claim 4 wherein n is 2 and R.sup.1 is --CONR.sup.4 R.sup.5.
- 12. The composition of claim 11 wherein R.sup.1 is --CON(CH.sub.3).sub.2.
- 13. The composition of claim 11 wherein R.sup.1 is --CONH(CH.sub.2).sub.3 CH.sub.3.
- 14. The composition of claim 11 wherein R.sup.1 is --CON(C.sub.2 H.sub.5).sub.2.
- 15. The composition of claim 11 wherein R.sup.1 is ##STR29##
- 16. A method of treating a susceptible fungal infection in man which comprises oral, parenteral or topical administration to said man of an antifungal amount of a composition of claim 1.
- 17. An agricultural composition suitable for eradicating or preventing a susceptible fungal infection in a plant or in plant seed which comprises an agriculturally acceptable carrier and an antifungal amount of a compound of the formula ##STR30## where R is a phenyl group optionally substituted by 1 to 3 substituents each independently selected from halo, CF.sub.3, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 alkoxy;
- R.sup.1 is selected from (a) --SO(C.sub.1 -C.sub.4 alkyl), (b) --SO.sub.2 (C.sub.1 -C.sub.4 alkyl), (c) --SO.sub.2 NR.sup.2 R.sup.3 where either R.sup.2 and R.sup.3 are both C.sub.1 -C.sub.4 alkyl, or R.sup.2 and R.sup.3 together with the N atom to which they are attached represent piperidino, (d) --NHSO.sub.2 (C.sub.1 -C.sub.4 alkyl) and (e) --CONHR.sup.4 R.sup.5 where either R.sup.4 is H or C.sub.1 -C.sub.4 alkyl and R.sup.5 is C.sub.1 -C.sub.4 alkyl, or R.sup.4 and R.sup.5 together with the N atom to which they are attached represent piperidino; and
- n is 1 or 2; with the proviso that n is 2 when R.sup.1 is --NHSO.sub.2 --(C.sub.1 -C.sub.4 alkyl);
- or an agriculturally acceptable acid addition salt thereof.
- 18. A composition according to claim 17, wherein R is phenyl substituted by 1 to 3 substituents which are each independently halo or CF.sub.3.
- 19. A composition according to claim 18, wherein R is phenyl substituted by 4-fluoro, 4-chloro, 4-bromo, 2,4-dichloro, 2,4-difluoro, 2,4,6-trifluoro or 4-bromo-2,5-difluoro.
- 20. A composition according to claim 19 wherein R is 2,4-dichloro.
- 21. A composition according to claim 20 wherein n is 1 and R.sup.1 is --SO--(C.sub.1 -C.sub.4 alkyl), --SO.sub.2 --(C.sub.1 -C.sub.4 alkyl), or --SO.sub.2 NR.sup.4 R.sup.5.
- 22. The composition of claim 21 wherein R.sup.1 is --SOCH.sub.3.
- 23. The composition of claim 21 wherein R.sup.1 is --SO.sub.2 CH.sub.3.
- 24. The composition of claim 21 wherein R.sup.1 is ##STR31##
- 25. A composition according to claim 20, wherein n is 2 and R.sup.1 is --NHSO.sub.2 (C.sub.1 -C.sub.4 alkyl).
- 26. The composition of claim 25 wherein R.sup.1 is --NHSO.sub.2 CH.sub.3.
- 27. A composition according to claim 20 wherein n is 2 and R.sup.1 is --CONR.sup.4 R.sup.5.
- 28. The composition of claim 27 wherein R.sup.1 is --CON(CH.sub.3).sub.2.
- 29. The composition of claim 27, wherein R.sup.1 is --CONH(CH.sub.2).sub.3 CH.sub.3.
- 30. The composition of claim 27 wherein R.sup.1 is --CON(C.sub.2 H.sub.5).sub.2.
- 31. The composition of claim 27 wherein R.sup.1 is ##STR32##
- 32. A method of eradicating or preventing a susceptible fungal infection in a plant or in plant seeds which comprises treating said plant or said seeds with an antifungal amount of a composition of claim 17.
Priority Claims (1)
Number |
Date |
Country |
Kind |
8221477 |
Jul 1982 |
GBX |
|
Parent Case Info
This is a division of application Ser. No. 499,709, filed on May 31, 1983, now U.S. Pat. No. 4,507,484.
Foreign Referenced Citations (1)
Number |
Date |
Country |
0061835 |
Oct 1982 |
EPX |
Divisions (1)
|
Number |
Date |
Country |
Parent |
499709 |
May 1983 |
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