Claims
- 1. A compound of the formula ##STR54## wherein X is ##STR55## m is zero or 1; n is zero, 1 or 2;
- p is zero or 1 to 6 provided that m and p are not both zero;
- R.sub.1 is hydrogen, lower alkyl, halo substituted lower alkyl, ##STR56## --(CH.sub.2).sub.r --COR.sub.9, --(CH.sub.2).sub.r --cycloalkyl, --(CH.sub.2).sub.r --(.alpha.-naphthyl), --(CH.sub.2).sub.r --(.beta.-naphthyl), ##STR57## --(CH.sub.2).sub.r --NH.sub.2, --(CH.sub.2).sub.r --SH, --(CH.sub.2).sub.r --S-lower alkyl, --(CH.sub.2).sub.r --OH, ##STR58## --(CH.sub.2).sub.r --O-lower alkyl, ##STR59## R.sub.2 and R.sub.9 are independently hydroxy, lower alkoxy, (phenyl) lower alkoxy, ##STR60## --O.sup.- M.sup.+ where M.sup.+ is a salt forming metal ion, ##STR61## or --NRR'; R and R' are independently hydrogen, alkyl or ##STR62## R.sub.3 is hydrogen or ##STR63## R.sub.4 is hydrogen, lower alkyl of 1 to 4 carbons, lower alkoxy of 1 to 4 carbons, lower alkylthio of 1 to 4 carbons, halo, hydroxy, CF.sub.3, phenyl, ##STR64## R.sub.5 is lower alkyl, ##STR65## --(CH.sub.2).sub.q --(.alpha.-naphthyl), --(CH.sub.2).sub.q --(.beta.-naphthyl), or --(CH.sub.2).sub.q -cycloalkyl;
- R.sub.6 is hydrogen, lower alkyl, cycloalkyl or phenyl;
- R.sub.7 is hydrogen, lower alkyl, lower alkoxy or phenyl;
- r is an integer from 1 to 4; and
- q is zero or an integer from 1 to 7.
- 2. A compound of claim 1 wherein:
- R.sub.3 is hydrogen, ##STR66## and X is ##STR67## --(CH.sub.2).sub.2 --COOH, ##STR68##
- 3. The compound of claim 1 wherein
- n is zero;
- X is ##STR69## and R.sub.3 is hydrogen or ##STR70##
- 4. The compound of claim 3, N-[3,3,3-trifluoro -2-(mercaptomethyl)-1-oxopropyl]-L-leucine, isomer A or N-[3,3,3-trifluoro-2-(mercaptomethyl)-1-oxopropyl]-L-leucine, isomer B.
- 5. A compound of claim 1 wherein
- R.sub.3 is hydrogen or ##STR71## n is zero; X is ##STR72##
- 6. A compound of claim 2 wherein
- R.sub.3 is hydrogen;
- n is one; and
- X is ##STR73##
- 7. A pharmaceutical composition useful for reducing blood pressure and producing diuresis and natriuresis as well as treating congestive heart failure, renal failure, or hepatic cirrhosis comprising a pharmaceutically acceptable carrier and an effective amount of an endopeptidase inhibiting compound of the formula ##STR74## wherein X, n and R.sub.3 are as defined in claim 1.
RELATED APPLICATION
This application is a division of Ser. No. 690,436 filed Apr. 24, 1991, now U.S. Pat. No. 5,223,516, which is a continuation-in-part of Ser. No. 497,386 filed Mar. 22, 1990, now abandoned.
US Referenced Citations (14)
Foreign Referenced Citations (7)
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Country |
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Oct 1981 |
BEX |
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Jan 1984 |
EPX |
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Non-Patent Literature Citations (1)
Entry |
Wilkerson, "Antihypertensive Thioester Compounds", 2244 Research Disclosure (1986) Jun., No. 266. |
Divisions (1)
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Number |
Date |
Country |
Parent |
690436 |
Apr 1991 |
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Continuation in Parts (1)
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Number |
Date |
Country |
Parent |
497386 |
Mar 1990 |
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