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Carboxyalkyl dipeptides and anti-hypertensive use thereof
| Details |
Inventors: Gold, Elijah H.; Neustadt, Bernard R.; Smith, Elizabeth M.;
Assignee: Schering Corporation (Kenilworth, NJ)
Primary Examiner: Springer; David B.
Assistant Examiner:
Attorney, Agent or Firm: Magatti; Anita W., Nelson; James R., Miller; Stephen I.
The present invention relates to carboxyalkyl dipeptides which are inhibitors of angiotensin-converting enzyme and are useful as antihypertensive agents and in the treatment of congestive heart failure. The compounds of the present invention are compounds of the formulae ##STR1## and the pharmaceutically acceptable salts thereof, wherein R and R.sup.6 are the same or different and are hydroxy or lower alkoxy; R.sup.1 is benzyloxylower alkyl or benzylthiolower alkyl; R.sup.2 is benzylthiomethyl, 2-phenylethylthiomethyl, naphthylmethylthiomethyl, methylbenzylthiomethyl; 2-(carboxyphenyl)ethyl or 2-(alkoxycarbonylphenyl)ethyl; and R.sup.3 is hydrogen, lower alkyl or aminolower alkyl. |
|
DETAILED DESCRIPTION We claim: 1.
A compound represented by the formula ##STR12## and the pharmaceutically acceptable salts thereof, wherein R and R.
sup.
6 are the same or different and are hydroxy or lower alkoxy; R.
sup.
1 is benzyloxylower alkyl or benzylthiolower alkyl; and R.
sup.
3 is hydrogen, lower alkyl or aminolower alkyl.
2.
A compound of claim 1 wherein R is lower alkoxy.
3.
A compound of claim 1 wherein R is ethoxy.
4.
A compound of claim 1 wherein R.
sup.
6 is hydroxy.
5.
A compound of claim 1 wherein R.
sup.
3 is lower alkyl.
6.
A compound of claim 1 wherein R.
sup.
3 is methyl.
7.
A compound of claim 1 wherein R.
sup.
1 is benzyloxymethyl.
8.
A compound of claim 1 wherein R.
sup.
1 is benzylthiomethyl.
9.
A compound of claim 1 wherein R is lower alkoxy, R.
sup.
6 is hydroxy, R.
sup.
3 is lower alkyl, and R.
sup.
1 is benzyloxymethyl or benzylthiomethyl.
10.
A compound of claim 9 wherein R is ethoxy and R.
sup.
3 is methyl.
11.
A compound of claim 10 which is N-(1(R)-ethoxycarbonyl-2-benzylthioethyl)-(R,S)-alanyl-(S)-proline.
12.
A compound of claim 10 which is N-(1(S)-ethoxycarbonyl-2-benzyloxyethyl)-R,S)-alanyl-(S)-proline.
13.
An antihypertensive pharmaceutical composition comprising an antihypertensive effective amount of a compound of claim 1, together with a phartmaceutically acceptable carrier.
14.
A method for reducing blood pressure in a hypertensive mammal which comprises administering to such a mammal a composition of claim 13.
Description:
EXAMPLE 1 N-(1(R)-Ethoxycarbonyl-2-benzylthioethyl)-(R,S)-alanyl-(S)-proline hydrochloride Mix S-benzyl-L-cysteine ethyl ester hydrochloride (8.
28 g) with NaHCO.
sub.
3 solution until basic.
Extract with dichloromethane, dry with MgSO.
sub.
4, and concentrate to dryness at room temperature.
Dissolve the residue in tetrahydrofuran (80 ml) containing pyruvoyl-L-proline (2.
1 g) and 5 Angstrom molecular sieves (4 g).
Stir for 2 days and then add, dropwise over 4 hours, a solution of sodium cyanoborohydride in ethanol (20 ml).
Stir for 18 hours, filter, and concentrate the filtrate to dryness
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