Substituted dipeptides as inhibitors of enkephalinases

Claim 2

A compound having structural formula I R.sub.1 C*H(COR.sub.2)--NH--C*HR.sub.3 --CONH(CH.sub.2).sub.p --C*(R.sub.4 R.sub.5)--COR.sub.6 and the racemates, enantiomers and diastereoisomers thereof and the pharmaceutically acceptable salts thereof, wherein: R 1 is alkyl having from 1 to 6 carbon atoms, adamantylmethyl, cycloalkylmethyl having from 4 to 8 carbon atoms or A--X m --C n H 2n -- {wherein X is oxygen or sulfur; A is phenyl which may be substituted with the group Y (wherein Y is halogen, hydroxy, trifluoromethyl, alkoxy having from 1 to 6 carbon atoms, alkyl having from 1 to 6 carbon atoms, 2- or 3-furanyl, 2- or 3- thienyl, or phenyl (which may be substituted with halogen, hydroxy, trifluoromethyl, alkoxy having from 1 to 6 carbon atoms or alkyl having from 1 to 6 carbon atoms)), benzyl (the phenyl ring of which may be substituted with the group Y as defined herein), 1- or 2-naphthyl, 2- or 3-furanyl or 2- or 3-thienyl; m is 0 or 1; and n is 0, 1, 2, 3, or 4}; R 2 and R 6 may be the same or different and each is independently selected from hydroxy, alkoxy having from 1 to 8 carbon atoms, B--X m --C n H 2n --O-- {wherein B is phenyl (which may be substituted with the group Y as defined herein) or 1- and 2- naphthyl; and X, m, and n are as defined herein provided that, when n=0, m is zero}, --OCH 2 OCO-alkyl having from 3 to 8 carbon atoms, --OCH 2 CO--phenyl {the phenyl ring of which may be substituted with the group Y as defined herein}, 1-glyceryl, ##STR8## {wherein R 7 is hydrogen, alkyl having from 1 to 6 carbon atoms, or phenyl which may be substituted with the group Y as defined herein, and R 8 is hydrogen or alkyl having from 1 to 6 carbon atoms}; R 2 may also be --NR 7 R 8 wherein R 7 and R 8 are as defined herein; R 3 is alkyl having from 1 to 6 carbon atoms, cycloalkylmethyl having from 4 to 8 carbon atoms, 2- or 3-thienylmethyl, 2- or 3-furanylmethyl, 1- or 2-naphthylmethyl, or benzyl the phenyl ring of which may be substituted with the group Y as defined herein; R 4 is D--C n H 2n --O m -- wherein D is selected from hydrogen, alkyl having from 1 to 4 carbon atoms or phenyl which may be substituted with the group Z; {wherein Z is halogen, hydroxy, trifluoromethyl, alkoxy having from 1 to 6 carbon atoms, or alkyl having from 1 to 6 carbon atoms}; and m and n are as defined herein; R 4 may also be --NR 5 COR 7 {wherein R 5 and R 7 are as defined herein}, or --NR 5 CO 2 R 9 {wherein R 5 is defined herein and R 9 is alkyl having from 1 to 6 carbon atoms or phenyl which may be substituted with the group Y as defined herein}; R 5 is hydrogen or alkyl having from 1 to 6 carbon atoms; and p is 1 or 2.

Claim 3

A compound according to claim 1 wherein: R 1 is selected from benzyl, p-chlorobenzyl, p-methoxybenzyl, p-methylbenzyl, p-phenylbenzyl, 2-phenylethyl, 1-naphthylmethyl or 2-naphthymethyl; R 2 and R 6 may be the same or different and each is independently selected from hydroxy, methoxy, ethoxy, benzyloxy, 2-phenoxyethoxy, 1-glyceryl, ##STR9## or pivaloyloxymethoxy; R 3 is benzyl, p-methylbenzyl, p-phenylbenzyl, 1-naphthylmethyl or 3-thienylmethyl; R 4 is hydrogen, methyl or benzyl; R 5 is hydrogen; and p is 1 or 2.

Claim 4

A compound according to claim 1 wherein: R 1 is benzyl or p-phenylbenzyl; R 2 is hydroxy, 2-phenoxyethoxy, 1-glyceryl, ##STR10## pivaloyloxymethoxy or benzyloxy; R 3 is benzyl or p-phenylbenzyl; R 4 is hydrogen, methyl or benzyl; R 5 is hydrogen; R 6 is hydroxy; and p is 1.

Claim 5

A compound according to claim 3 wherein R 2 is 2-phenoxyethoxy, 1-glyceryl, pivaloyloxymethoxy, ##STR11## and R 6 is hydroxy.

Claim 6

A compound according to claim 3 wherein R 2 is hydroxy and R 6 is 2-pheoxyethoxy, 1-glyceryl, pivaolyloxymethoxy, ##STR12##

Claim 7

A compound having the name N-[N-[(L-1-carboxy-2-phenyl)ethyl]-L-phenylalanyl]-β-alanine or a pharmaceutically accetable salt thereof.

Claim 8

A compound having the name N-[N-[(L-1-carboxy-2-phenyl)ethyl]-L-phenylalanyl]-β-alanine or a pharmaceutically accetable salt thereof.

Claim 9

A compound defined in claim 1 wherein p is 1.

Claim 10

A compound defined in claim 1 having the name: N-[N-[(L-1-carboxy-2-phenylethyl)]-L-phenylalanyl]-β-alanine; N-[N-[L-1-(2,2-dimethyl-1-oxopropoxy)-methoxy]-carbonyl]-2-phenylethyl]-L-phenylalanyl]-β-alanine, (2,12-dimethyl-1-oxopropoxy)methyl ester; N-[N-[L-1-[phenylmethoxy]carbonyl]-2-phenylethyl]-L-phenylalanyl]-β-alanine, (2,2-dimethyl-1-oxopropoxy)methylester; N-[N-[L-1-carboxy-2-(4-phenyl)phenylethyl]-L-phenylalanyl]-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1-oxopropoxy)-methoxy]carbonyl]-2-(4-phenyl)phenylethyl]-L-phenylalanyl]-β-alanine,(2,2-dimethyl-1-oxopropoxy)methyl ester; N-[N-[L-1-carboxy-2-phenylethyl]-L-(4-phenyl)phenylalanyl]-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1-oxopropoxy)-methoxy]carbonyl]-2-(4-phenyl)phenylethyl]-L-(4-phenyl)-phenylalanyl-βalanine, (2,2-dimethyl-1-oxopropoxy)methyl ester; N-[N-[L-[1-[(2,2-dimethyl-1-oxopropoxy)-methoxy]-carbonyl]-2-phenylethyl]-L-(4-phenyl)phenylalanyl]-β-alanine,(2,2-dimethyl-1-methyl ester;

Claim 11

N-[N-[L-1-carboxy-2-phenylethyl]-L-phenylalanyl]-L-(1-methyl)-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1-oxopropoxy)methoxy]-carbonyl]-2-phenylethyl]-L-phenylalanyl]-L-(1-methyl)-β-alanine,(2,2-dimethyl-1-oxopropoxy)methyl ester; N-[N-[(L-1-carboxy-2-phenylethyl)]-L-phenylalanyl]-β-alanine, 2-phenoxyethyl ester; N-[N-[(D-1-carboxy-2-phenylethyl)]-L-leucyl]-L-phenylalanine; N-[N-[(L-1-carboxy-2-phenylethyl)]-L-phenylalanyl]-L-phenylalanine; N-[N-[(L-1-carboxy-3-phenylpropyl)]-L-phenylalanyl]-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1-oxopropoxy)-methoxy]carbonyl]-2-phenylethyl]-L-phenylalanyl]-β-alanine; N-[N-[L-[1-[(2-phenoxy)ethoxy]carbonyl]-2-phenylethyl]-L-phenylalanyl]-.beta.-alanine; N-[N-[L-[1-[(1-oxo-3-isobenzofuranyloxy)]carbonyl]-2-phenylethyl]-L-phenylalanyl-β-alanine; N-[N-[L-[1-[(2,3-dihydroxy)-1-propoxy]carbonyl]-2-phenylethyl]-L-phenylalanyl]-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1,3-dioxolan-4-yl)methoxy]-carbonyl]-2-phenylethyl]-L-phenylananyl]-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1-oxypropoxy)methoxy]-carbonyl]-2-(4-phenyl)phenylethyl]-L-phenylalanyl]-β-alanine; N-[N-[L-[1-[(2-phenoxy)ethoxy]carbonyl]-2-(4- phenyl)-phenylethyl]-L-phenylalanyl]-β-alanine; N-[N-[L-[1-[(1-oxo-3-isobenzofuranyloxy)]-carbonyl]-2-(4-phenyl)phenylethyl]-L-phenylalanyl]-β-alanine; N-[N-[L-[1-[(2,3-dihydroxy)-1-propoxy]-carbonyl]-2-(4-phenyl)phenylethyl]-L-phenylalanyl]-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1,3-dioxolan-4-yl)methoxy]-carbonyl]-2-(4-phenyl)phenylethyl]-L-phenylalanyl]-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1-oxypropoxy)methoxy]-carbonyl]-2-phenylethyl]-L-(4-phenyl)phenylalanyl]-β-alanine; N-[N-[L-[1-[(2-phenoxy)ethoxy]carbonyl]-2-phenylethyl]-L-(4-phenyl)phenylalanyl]-β-alanine; N-[N-[L-[1-[(1-oxo-3-isobenzofuranyloxy)]-carbonyl]-2-phenylethyl]-L-(4-phenyl)phenylalanyl]-β-alanine; N-[N-[L-[1-[(2,3-dihydroxy)-1-propoxy]-carbonyl]-2-phenylethyl]-L-(4-phenyl)phenylalanyl]-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1,3-dioxolan-4-yl)methoxy]-carbonyl]-2-phenylethyl]-L-(4-phenyl)phenylalanyl]-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1-oxypropoxy)methoxy]-carbonyl]-2-(4-phenyl)phenylethyl]-L-(4-phenyl)phenylalanyl]-β-alanine; N-[N-[L-[1-[(2-phenoxy)ethoxy]carbonyl]-2-(4phenyl)phenylethyl]-L-(4-phenyl)phenylalanyl]-β-alanine; N-[N-[L-[1-[(1-oxo-3-isobenzofuranyloxy)]-carbonyl]-2-(4-phenyl)phenylethyl]-L-(4-phenyl)phenylalanyl]-β-alanine; N-[N-[L-[1-[2,3-dihydroxy)-1-propoxy]-carbonyl]-2-(4-phenyl)-phenylethyl]-L-(4-phenyl)-phenylalanyl]-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1,3-dioxolan-4-yl)methoxy]-carbonyl]-2-(4-phenyl)phenylethyl]-L-(4-phenyl)phenylalanyl]-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1-oxypropoxy)-methoxy]-carbonyl]-2-phenylethyl]-L-phenylalanyl]-D,L-α-methyl-β-alanine; N-[N-[L-[1-[(2-phenoxy)ethoxy]carbonyl]-2-phenylethyl]-L-phenylalanyl]-D,L-α-methyl-β-alanine; N-[N-[L-[1-[(1-oxo-3-isobenzofuranyloxy)]-carbonyl]-2-phenylethyl]-L-phenylalanyl]-D,L-α-methyl-β-alanine; N-[N-[L-[1-[(2,3-dihydroxy)-1-propoxy]-carbonyl]-2-phenylethyl]-L-phenylalanyl]-D,L-α-methyl-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1,3-dioxolan-4-yl)methoxy]-carbonyl]-2-phenylethyl]-L-phenylalanyl]-D,L-α-methylβ-alanine; N-[N-[L-[1-[(2,2-dimethyl-1-oxypropoxy)-methoxy]-carbonyl]-2-(4-phenyl)phenylethyl]-L-phenylalanyl]-D,L-α-methyl-β-alanine; N-[N-[L-[1-[(2-phenoxy)ethoxy]carbonyl]-2-(4- phenyl)-phenylethyl]-L-phenylalanyl]-D,L-α-methyl-β-alanine; N-[N-[L-[1-[(1-oxo-3-isobenzofuranyloxy)]carbonyl]-2-(4-phenyl)phenylethyl]-L-phenylalanyl]-D,L-α-methyl-β-alanine; N-[N-[L-[1-[(2,3-dihydroxy)-1-propoxy]carbonyl]-2-(4-phenyl)phenylethyl]-L-phenylalanyl]-D,L-α-methyl-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1,3-dioxolan-4-yl)methoxy]-carbonyl]-2-(4-phenyl)phenylethyl]-L-phenylalanyl]-D,L-α-methyl-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1-oxypropoxy)methoxy]-carbonyl]-2-phenylethyl]-L-(4-phenyl)phenylalanyl]-D,L-α-methyl-β-alanine; N-[N-[L-[1-[(2-phenoxy)ethoxy]carbonyl]-2phenylethyl]-L-(4-phenyl)phenylalanyl]-D,L-α-methyl-β-alanine; N-[N-[L-[1-[(1-oxo-3-isobenzofuranyloxy)]-carbonyl]-2-phenylethyl]-L-(4-phenyl)phenylalanyl]-D,L-α-methyl-β-alanine; N-[N-[L-[1-[(2,3-dihydroxy)-1-propoxy]-carbonyl]-2-phenylethyl]-L-(4-phenyl)phenylalanyl]-D,L-α-methyl-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1,3-dioxolan-4-yl)methoxy]-carbonyl]-2-phenylethyl]-L-(4-phenyl)phenylalanyl]-D,L-α-methyl-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1-oxypropoxy)methoxy]-carbonyl]-2-(4-phenyl)phenylethyl]-L-(4-phenyl)- phenylalanyl]-D,L-α-methyl-β-alanine; N-[N-[L-[1-[(2-phenoxy)ethoxy]carbonyl]-2-(4- phenyl)-phenylethyl]-L-(4-phenyl)phenylalanyl]-D,L-α-methyl-β-alanine; N-[N-[L-[1-[(1-oxo-3-isobenzofuranyloxy)]carbonyl]-2-(4-phenyl)phenylethyl]-L-(4-phenyl)phenylalanyl]-D,L-α-methyl-β-alanine; N-[N-[L-[1-[(2,3-dihydroxy)-1-propoxy]carbonyl]-2-(4-phenyl)phenylethyl]-L-(4-phenyl)-phenylalanyl]-D,L-α-methyl-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1,3-dioxolan-4-yl)methoxy]-carbonyl]-2-(4-phenyl)phenylethyl]-L-(4-phenyl)phenylalanyl]-D,L-α-methyl-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1-oxypropoxy)methoxy]-carbonyl]-2-phenylethyl]-L-2-thienylalanyl]-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1-oxypropoxy)-methoxy]carbonyl]-2-phenylethyl]-L-3-thienylalanyl]-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1-oxypropoxy)methoxy]carbonyl]-2-phenylethyl]-L-2-furoalanyl]-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1-oxypropoxy)methoxy]carbonyl]-2-phenylethyl]-L-phenylalanyl]-α-methylalanine; N-[N-[L-[1-[(2,2-dimethyl-1-oxypropoxy)methoxy]carbonyl]-2-phenylethyl]-L-phenylalanyl]-L-α-hydroxy-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1-oxypropoxy)methoxy]carbonyl]-2-phenylethyl]-L-phenylalanyl]-D-α-hydroxy-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1-oxypropoxy)methoxy]carbonyl]-2-phenylethyl]-L-phenylalanyl]-L-α-methoxy-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1-oxypropoxy)methoxy]carbonyl]-2-phenylethyl]-L-phenylalanyl]-D-α-methoxy-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1,3-dioxolan-4-yl)- hydroxy-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1,3-dioxolan-4-yl) methoxy]carbonyl]-2-phenylethyl]-(L)-phenylalanyl]-β-alanine, hemimaleate; N-[N-[(L)1-carboxy-2-phenylethyl)]-L-phenylalanyl]-S-2-[N-[(1,1-dimethylethoxy)carbonyl]amino-β-alanine; and the pharmaceutically acceptable salts thereof.

Claim 12

N-[N-[L-1-carboxy-2-phenylethyl]-L-phenylalanyl]-L-(1-methyl)-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1-oxopropoxy)methoxy]-carbonyl]-2-phenylethyl]-L-phenylalanyl]-L-(1-methyl)-β-alanine,(2,2-dimethyl-1-oxopropoxy)methyl ester; N-[N-[(L-1-carboxy-2-phenylethyl)]-L-phenylalanyl]-β-alanine, 2-phenoxyethyl ester; N-[N-[(D-1-carboxy-2-phenylethyl)]-L-leucyl]-L-phenylalanine; N-[N-[(L-1-carboxy-2-phenylethyl)]-L-phenylalanyl]-L-phenylalanine; N-[N-[(L-1-carboxy-3-phenylpropyl)]-L-phenylalanyl]-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1-oxopropoxy)-methoxy]carbonyl]-2-phenylethyl]-L-phenylalanyl]-β-alanine; N-[N-[L-[1-[(2-phenoxy)ethoxy]carbonyl]-2-phenylethyl]-L-phenylalanyl]-.beta.-alanine; N-[N-[L-[1-[(1-oxo-3-isobenzofuranyloxy)]carbonyl]-2-phenylethyl]-L-phenylalanyl-β-alanine; N-[N-[L-[1-[(2,3-dihydroxy)-1-propoxy]carbonyl]-2-phenylethyl]-L-phenylalanyl]-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1,3-dioxolan-4-yl)methoxy]-carbonyl]-2-phenylethyl]-L-phenylananyl]-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1-oxypropoxy)methoxy]-carbonyl]-2-(4-phenyl)phenylethyl]-L-phenylalanyl]-β-alanine; N-[N-[L-[1-[(2-phenoxy)ethoxy]carbonyl]-2-(4- phenyl)-phenylethyl]-L-phenylalanyl]-β-alanine; N-[N-[L-[1-[(1-oxo-3-isobenzofuranyloxy)]-carbonyl]-2-(4-phenyl)phenylethyl]-L-phenylalanyl]-β-alanine; N-[N-[L-[1-[(2,3-dihydroxy)-1-propoxy]-carbonyl]-2-(4-phenyl)phenylethyl]-L-phenylalanyl]-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1,3-dioxolan-4-yl)methoxy]-carbonyl]-2-(4-phenyl)phenylethyl]-L-phenylalanyl]-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1-oxypropoxy)methoxy]-carbonyl]-2-phenylethyl]-L-(4-phenyl)phenylalanyl]-β-alanine; N-[N-[L-[1-[(2-phenoxy)ethoxy]carbonyl]-2-phenylethyl]-L-(4-phenyl)phenylalanyl]-β-alanine; N-[N-[L-[1-[(1-oxo-3-isobenzofuranyloxy)]-carbonyl]-2-phenylethyl]-L-(4-phenyl)phenylalanyl]-β-alanine; N-[N-[L-[1-[(2,3-dihydroxy)-1-propoxy]-carbonyl]-2-phenylethyl]-L-(4-phenyl)phenylalanyl]-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1,3-dioxolan-4-yl)methoxy]-carbonyl]-2-phenylethyl]-L-(4-phenyl)phenylalanyl]-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1-oxypropoxy)methoxy]-carbonyl]-2-(4-phenyl)phenylethyl]-L-(4-phenyl)phenylalanyl]-β-alanine; N-[N-[L-[1-[(2-phenoxy)ethoxy]carbonyl]-2-(4phenyl)phenylethyl]-L-(4-phenyl)phenylalanyl]-β-alanine; N-[N-[L-[1-[(1-oxo-3-isobenzofuranyloxy)]-carbonyl]-2-(4-phenyl)phenylethyl]-L-(4-phenyl)phenylalanyl]-β-alanine; N-[N-[L-[1-[2,3-dihydroxy)-1-propoxy]-carbonyl]-2-(4-phenyl)-phenylethyl]-L-(4-phenyl)-phenylalanyl]-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1,3-dioxolan-4-yl)methoxy]-carbonyl]-2-(4-phenyl)phenylethyl]-L-(4-phenyl)phenylalanyl]-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1-oxypropoxy)-methoxy]-carbonyl]-2-phenylethyl]-L-phenylalanyl]-D,L-α-methyl-β-alanine; N-[N-[L-[1-[(2-phenoxy)ethoxy]carbonyl]-2-phenylethyl]-L-phenylalanyl]-D,L-α-methyl-β-alanine; N-[N-[L-[1-[(1-oxo-3-isobenzofuranyloxy)]-carbonyl]-2-phenylethyl]-L-phenylalanyl]-D,L-α-methyl-β-alanine; N-[N-[L-[1-[(2,3-dihydroxy)-1-propoxy]-carbonyl]-2-phenylethyl]-L-phenylalanyl]-D,L-α-methyl-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1,3-dioxolan-4-yl)methoxy]-carbonyl]-2-phenylethyl]-L-phenylalanyl]-D,L-α-methylβ-alanine; N-[N-[L-[1-[(2,2-dimethyl-1-oxypropoxy)-methoxy]-carbonyl]-2-(4-phenyl)phenylethyl]-L-phenylalanyl]-D,L-α-methyl-β-alanine; N-[N-[L-[1-[(2-phenoxy)ethoxy]carbonyl]-2-(4- phenyl)-phenylethyl]-L-phenylalanyl]-D,L-α-methyl-β-alanine; N-[N-[L-[1-[(1-oxo-3-isobenzofuranyloxy)]carbonyl]-2-(4-phenyl)phenylethyl]-L-phenylalanyl]-D,L-α-methyl-β-alanine; N-[N-[L-[1-[(2,3-dihydroxy)-1-propoxy]carbonyl]-2-(4-phenyl)phenylethyl]-L-phenylalanyl]-D,L-α-methyl-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1,3-dioxolan-4-yl)methoxy]-carbonyl]-2-(4-phenyl)phenylethyl]-L-phenylalanyl]-D,L-α-methyl-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1-oxypropoxy)methoxy]-carbonyl]-2-phenylethyl]-L-(4-phenyl)phenylalanyl]-D,L-α-methyl-β-alanine; N-[N-[L-[1-[(2-phenoxy)ethoxy]carbonyl]-2phenylethyl]-L-(4-phenyl)phenylalanyl]-D,L-α-methyl-β-alanine; N-[N-[L-[1-[(1-oxo-3-isobenzofuranyloxy)]-carbonyl]-2-phenylethyl]-L-(4-phenyl)phenylalanyl]-D,L-α-methyl-β-alanine; N-[N-[L-[1-[(2,3-dihydroxy)-1-propoxy]-carbonyl]-2-phenylethyl]-L-(4-phenyl)phenylalanyl]-D,L-α-methyl-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1,3-dioxolan-4-yl)methoxy]-carbonyl]-2-phenylethyl]-L-(4-phenyl)phenylalanyl]-D,L-α-methyl-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1-oxypropoxy)methoxy]-carbonyl]-2-(4-phenyl)phenylethyl]-L-(4-phenyl)- phenylalanyl]-D,L-α-methyl-β-alanine; N-[N-[L-[1-[(2-phenoxy)ethoxy]carbonyl]-2-(4- phenyl)-phenylethyl]-L-(4-phenyl)phenylalanyl]-D,L-α-methyl-β-alanine; N-[N-[L-[1-[(1-oxo-3-isobenzofuranyloxy)]carbonyl]-2-(4-phenyl)phenylethyl]-L-(4-phenyl)phenylalanyl]-D,L-α-methyl-β-alanine; N-[N-[L-[1-[(2,3-dihydroxy)-1-propoxy]carbonyl]-2-(4-phenyl)phenylethyl]-L-(4-phenyl)-phenylalanyl]-D,L-α-methyl-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1,3-dioxolan-4-yl)methoxy]-carbonyl]-2-(4-phenyl)phenylethyl]-L-(4-phenyl)phenylalanyl]-D,L-α-methyl-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1-oxypropoxy)methoxy]-carbonyl]-2-phenylethyl]-L-2-thienylalanyl]-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1-oxypropoxy)-methoxy]carbonyl]-2-phenylethyl]-L-3-thienylalanyl]-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1-oxypropoxy)methoxy]carbonyl]-2-phenylethyl]-L-2-furoalanyl]-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1-oxypropoxy)methoxy]carbonyl]-2-phenylethyl]-L-phenylalanyl]-α-methylalanine; N-[N-[L-[1-[(2,2-dimethyl-1-oxypropoxy)methoxy]carbonyl]-2-phenylethyl]-L-phenylalanyl]-L-α-hydroxy-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1-oxypropoxy)methoxy]carbonyl]-2-phenylethyl]-L-phenylalanyl]-D-α-hydroxy-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1-oxypropoxy)methoxy]carbonyl]-2-phenylethyl]-L-phenylalanyl]-L-α-methoxy-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1-oxypropoxy)methoxy]carbonyl]-2-phenylethyl]-L-phenylalanyl]-D-α-methoxy-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1,3-dioxolan-4-yl)- hydroxy-β-alanine; N-[N-[L-[1-[(2,2-dimethyl-1,3-dioxolan-4-yl) methoxy]carbonyl]-2-phenylethyl]-(L)-phenylalanyl]-β-alanine, hemimaleate; N-[N-[(L)1-carboxy-2-phenylethyl)]-L-phenylalanyl]-S-2-[N-[(1,1-dimethylethoxy)carbonyl]amino-β-alanine; and the pharmaceutically acceptable salts thereof.

Claim 13

The compound defined in claim 7 having the name N- N-[(L)-[1-[(2,2-dimethyl-1,3-dioxolan-4-yl)-methoxy]carbonyl]-2-phenylethyl]-L-phenylalanyl]-β-alanine; or a pharmaceutically acceptable salt thereof.

Claim 14

The compound defined in claim the form of a 1 to 1 salt with maleic acid.

Claim 15

A compound defined in claim 7 having the name N-[L-[1-(2,2-dimethyl-1,3-dioxolan-4-yl)-methoxy]carbonyl]-2-phenylethyl]-L-phenylalanyl]-R-α-hydroxy-β-alanine.