Claims
- 1. A compound of the formula: ##STR52## wherein R.sub.1 is H, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.12 acyl, --CH.sub.2 A-- or --C(O)--A; ##STR53## where L and M are independently H, F, Cl, Br, NO.sub.2, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, CF.sub.3, OCF.sub.3, CN, phenyl or COOR', where R' is H, CH.sub.3 or C.sub.2 H.sub.5 ;
- R.sub.2 and R.sub.3 are independently CF.sub.3, CF.sub.2 Cl or CF.sub.2 H;
- R.sub.4 is NR.sub.6 R.sub.7, O--R.sub.5, S--R.sub.5 or Cl;
- R.sub.5 is H, C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.10 alkenyl, A or --R.sub.8 --A;
- R.sub.6 and R.sub.7 are independently H, C.sub.1 -C.sub.6 alkyl, A or --R.sub.8 --A;
- R.sub.8 is C.sub.1 -C.sub.6 alkyl;
- Y and Z are independently H, NO.sub.2, C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.3 alkylthio, Cl, Br, F, C.sub.1 -C.sub.4 alkyl, NH.sub.2 or N(CH.sub.3).sub.2 ;
- X is ##STR54## n is 1, 2 or 3; provided that:
- (a) when Y and Z are H, then X is other than ##STR55## (b) when Y is other than OCH.sub.3, then R.sub.6 and R.sub.7 are CH.sub.3 ; and
- (c) when Y and Z are H and X is ##STR56## then R.sub.4 is other than NR.sub.6 R.sub.7.
- 2. A compound of according to claim 1, having the formula ##STR57##
- 3. A compound of claim 2 wherein n is 1.
- 4. A compound of claim 2 where R.sub.1 is H.
- 5. A compound of claim 2 where Y is OCH.sub.3 or OC.sub.2 H.sub.5.
- 6. A compound of claim 2 where Z is H.
- 7. A compound of claim 2 where X is --CH.sub.2 CH.sub.2 --.
- 8. A compound of claim 2 where R.sub.4 =OR.sub.5 or Cl.
- 9. A compound of claim 8 where R.sub.5 is H, CH.sub.3 or C.sub.2 H.sub.5.
- 10. A compound of claim 2 where R.sub.4 =N(CH.sub.3).sub.2.
- 11. A compound of claim 2 where R.sub.2 and R.sub.3 are both CF.sub.3.
- 12. A compound of claim 2 where
- R.sub.1 is H;
- Y is OCH.sub.3 or OC.sub.2 H.sub.5 ;
- Z is H;
- X is --CH.sub.2 CH.sub.2 --;
- R.sub.4 is OH, OCH.sub.3, OC.sub.2 H.sub.5, or N(CH.sub.3).sub.2 ; and
- R.sub.2 and R.sub.3 are both CF.sub.3.
- 13. The compound of claim 2 which is 3-{2-methoxy-4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl}propanoic acid.
- 14. The compound of claim 2 which is methyl 2-methoxy-4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]benzenepropanoate.
- 15. The compound of claim 2 which is ethyl 2-methoxy-4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]benzenepropanoate.
- 16. A compound according to claim 1, having the formula ##STR58##
- 17. A pharmaceutical composition consisting essentially of a suitable pharmaceutical carrier and an effective antihypertensive amount of a compound of claim 2 where R.sub.4 is other than Cl.
- 18. A pharmaceutical composition consisting essentially of a suitable pharmaceutical carrier and an effective antihypertensive amount of a compound of claim 12 where R.sub.4 is other than Cl.
- 19. A pharmaceutical composition consisting essentially of a suitable pharmaceutical carrier and an effective antihypertensive amount of a compound of claim 12 where R.sub.4 is other than Cl.
- 20. A pharmaceutical composition consisting essentially of a suitable pharmaceutical carrier and an effective antihypertensive amount of a compound of claim 14 where R.sub.4 is other than Cl.
- 21. A pharmaceutical composition consisting essentially of a suitable pharmaceutical carrier and an effective antihypertensive amount of a compound of claim 15 where R.sub.4 is other than Cl.
- 22. A method of treating hypertension in mammals which comprises administering to the mammal an effective hypertensive amount of a compound of claim 2 where R.sub.4 is other than Cl.
- 23. A method of treating hypertension in mammals which comprises administering to the mammal an effective hypertensive amount of a compound of claim 12 where R.sub.4 is other than Cl.
- 24. A method of treating hypertension in mammals which comprises administering to the mammal an effective hypertensive amount of a compound of claim 13 where R.sub.4 is other than Cl.
- 25. A method of treating hypertension in mammals which comprises administering to the mammal an effective hypertensive amount of a compound of claim 14 where R.sub.4 is other than Cl.
- 26. A method of treating hypertension in mammals which comprises administering to the mammal an effective hypertensive amount of a compound of claim 15 where R.sub.4 is other than Cl.
RELATED APPLICATIONS
This application is a continuation of application Ser. No. 306,411, filed Sept. 28, 1981, which is a continuation-in-part of application Ser. No. 061,045, filed on July 26, 1979, now abandoned.
US Referenced Citations (1)
Number |
Name |
Date |
Kind |
4450172 |
Yoa |
May 1981 |
|
Continuations (1)
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Number |
Date |
Country |
Parent |
306411 |
Sep 1981 |
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Continuation in Parts (1)
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Number |
Date |
Country |
Parent |
61045 |
Jul 1979 |
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