3,3-diphenyl prop-2-yl amino acid derivatives and their use as tachykinin antagonists
AssigneeMerck Sharp & Dohme Corp.
InventorsMartin R. Teall, Brian J. Williams
Life of this patent
Estimating the term…
Abstract
Compounds of formula (I), or a salt or prodrug thereof, wherein R.sup.1 represents H, C.sub.1-4 alkyl or CH.sub.2 COOH; R.sup.2 represents H or C.sub.1-4 alkyl, with the proviso that R.sup.1 and R.sup.2 are not both H; R.sup.3 and R.sup.4 each independently rely resent H, C.sub.1-, alkyl. C.sub.2-6 alkenyl C.sub.1-6 alkoxy, halo or trifluoromethyl; A.sup.1, A.sup.2, A.sup.3, and A.sup.4 each independently represent H, C.sub.1-6 alkyl, C.sub.1-6 alkenyl, C.sub.1-6 alkoxy, halo or trifluoromethyl; and A.sup.5 and A.sup.6 each independently represent H or C.sub.1-4 are tachykinin antagonists useful ##STR1##
Claims8
A compound of formula (I) as a pharmaceutically acceptable salt or prodrug thereof:
- ##STR10## wherein R.sup.1 represents H, C.sub.1-4 alkyl or CH.sub.2 COOH;
- R.sup.2 represents H or C.sub.1-4 alkyl, with the proviso that R.sup.1 and R.sup.2 are not both H;
- R.sup.3 and R.sup.4 each independently represent H, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.1-6 alkoxy, halo or trifluoromethyl;
- A.sup.1, A.sup.2 A.sup.3 and A.sup.4 each independently represent H, C.sub.1-6 alkyl, C.sub.1-6 alkenyl, C.sub.1-6 alkoxy, halo or trifluoromethyl;
- and A.sup.5 and A.sup.6 each independently represent H or C.sub.1-4 alkyl.
A compound of the formula (IA) or a pharmaceutically acceptable salt thereof:
- ##STR11## wherein R.sup.10 represents H, methyl or CH.sub.2 COOH;
- R.sup.11 represents H, methyl or ethyl, with the proviso that when R.sup.10 is H, R.sup.11 is not H;
- and
- R.sup.12 and R.sup.13 each independently represent C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.1-6 alkoxy, halo, or trifluoromethyl.
A compound selected from:
- (S)-N-(1-((3,5-bis(trifluoromethyl)phenyl)methyloxy)-3,3-diphenylprop-2-yl) -N-methylglycine;
- (S)-N-(1-(((3-t-butyl-5-chloro)phenyl)methyloxy)-3,3-diphenylprop-2-yl)-N-m ethylglycine;
- (S)-N-(1-((3,5-dimethyl)phenyl)methyloxy)-3,3-diphenylprop-2-yl)-N-methylgl ycine;
- (S)-N-(1-(((3-chloro-5-methyl)phenyl)methyloxy)-3,3-diphenylprop-2-yl)-N-me thylglycine;
- (S)-N-(1-(((3-bromo-5-methyl)phenyl)methyloxy)-3,3-diphenylprop-2-yl)-N-met hylglycine;
- (S)-N-(1-(((3,5-dichlorophenyl)methyloxy)-3,3-diphenylprop-2-yl)-N-methylgl ycine;
- (S)-N-(1-(((3-methyl-5-vinyl)phenyl)methyloxy)-3,3-diphenylprop-2-yl)-N-met hylglycine;
- (S)-N-(1-(((3-ethyl-5-methyl)phenyl)methyloxy)-3,3-diphenylprop-2-yl)-N-met hylglycine;
- (S)-N-(1-((3,5-bis(trifluoromethyl)phenyl)methyloxy)-3,3-diphenylprop-2-yl) alanine;
- (S)-2-(N,N-bis(carboxymethyl)amino)-1-((3,5-bis (trifluoromethyl)phenyl)methyloxy)-3,3diphenylpropane;
- (S)-N-(1-(((3-methoxy-5-methyl)phenyl)methyloxy)-3,3-diphenylprop-2-yl)-N-m ethylglycine;
- (S)-N-(1-((3,5-bis(trifluoromethyl)phenyl)methyloxy)-3,3-diphenylprop-2-yl) -N-ethylglycine;
- and pharmaceutically acceptable salts thereof.
A pharmaceutical compositions comprising one or more compounds of formula (I), or salts or prodrugs thereof, in association with a pharmaceutically acceptable carrier.
Dependencies are inferred from the claim text.