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US 4,727,180 AGranted
Antihypertensive polyhalohydroxylisopropyl phenylalkanoic and phenylalkenoic acids, amides and esters and intermediates thereto
AssigneeE. I. Du Pont de Nemours and Company
InventorsPaul E. Aldrich, Gilbert H. Berezin
Life of this patent
Estimating the term…
Abstract
Polyhalohydroxyisopropyl phenylalkanoic and phenylalkenoic acids, amides, and esters, such as methyl 2-methoxy-4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]benzenepro panoate, are useful as antihypertensive agents.
Claims26
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.
10 more elements
Dependencies are inferred from the claim text.