Substituted peptidylamine calcium channel blockers
AssigneeWarner-Lambert Company
InventorsLain-Yen Hu, Thomas Charles Malone, Laszlo Nadasdi, Michael Francis Rafferty, Todd Robert Ryder, Diego F. Silva, Yuntao Song, Balazs G. Szoke, Laszlo Urge
Life of this patent
Estimating the term…
Abstract
The present invention provides compounds that block calcium channels having the Formula I shown below. ##STR1## The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, or epilepsy and to pharmaceutical compositions that contain the compounds of Formula I.
Claims29
A compound having Formula I ##STR37## wherein:
- * is a first chiral center;
- @ is a second chiral center;
- R.sup.1 and R.sup.2 independently are:
- (a) C.sub.1 -C.sub.8 alkyl, unsubstituted or substituted with one or two of halo, hydroxy, amino, alkylamino or dialkylamino;
- (b) C.sub.2 -C.sub.8 alkenyl, unsubstituted or substituted with one or two of halo, hydroxy, amino, C.sub.1 -C.sub.4 -alkylamino or di(C1-C4)-alkylamino;
- (c) (CH.sub.2).sub.n --C.sub.3 -C.sub.7 cycloalkenyl, unsubstituted or substituted by one or two of halo, hydroxy, C.sub.1 -C.sub.4 alkyl, amino, C.sub.1 -C.sub.4 -alkylamino or di(C.sub.1 -C.sub.4)-alkylamino;
- (d) (CH.sub.2).sub.n --C.sub.3 -C.sub.7 cycloalkyl, unsubstituted or substituted with one or two of halo hydroxy, C.sub.1 -C.sub.4 alkyl, amino, C.sub.1 -C.sub.4 -alkylamino or di(C.sub.1 -C.sub.4)-alkylamino;
- (e) (CH.sub.2).sub.n phenyl, unsubstituted or substituted with one or two of C.sub.1 -C.sub.4 alkyl, benzyloxy, amino, C.sub.1 -C.sub.4 alkylamino, di(C.sub.1 -C.sub.4)-alkylamino, halo, C.sub.1 -C.sub.4 alkoxy;
- (f) (CH.sub.2).sub.n -pyridyl ##STR38## R.sup.3, R.sup.5 and R.sup.6 independently are hydrogen or C.sub.1 -C.sub.8 alkyl;
- R.sup.4 is:
- (a) C.sub.1 -C.sub.8 alkyl;
- (b) (CH.sub.2).sub.n --C.sub.3 -C.sub.7 cycloalkyl, unsubstituted or substituted with one or two of halo, hydroxy, C.sub.1 -C.sub.4 alkyl, amino, C.sub.1 -C.sub.4 alkylamino or di-C.sub.1 -C.sub.4 alkylamino;
- or
- (c) (CH.sub.2).sub.n phenyl;
- X is:
- (a) --NHR.sup.3 ;
- (b) --NR.sup.3 R.sup.5 ;
- (c) --NH(CH.sub.2).sub.n NR.sup.3 R.sup.5 ;
- (d) --NH(CH.sub.2).sub.n NH(CH.sub.2).sub.n phenyl;
- (e) --NH (CH.sub.2).sub.n NH(CH.sub.2).sub.n --OH;
- ##STR39## n is 0 to 5;
- and the pharmaceutically acceptable salts thereof.
A compound selected from:
- 2-Dimethylamino-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-Dimethylamino-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(piperidine-1-carbonyl)-ethyl]-amide;
- 2-Dimethylamino-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(2-piperidin-1-yl-ethylcarbamoyl)-ethyl]-amide;
- 2-Dimethylamino-4-methyl-pentanoic acid [1-(4-benzyloxy-benzyl)-2-(4-benzyl-piperazin-1-yl)-2-oxo-ethyl]-amide;
- 2-Dimethylamino-4-methyl-pentanoic acid [2-(4-benzyloxy-benzyl)-1-(1-benzyl-piperidin-4-yl-carbamoyl)-ethyl]-amide
- 2-Dimethylamino-4-methyl-pentanoic acid [1-(4-benzyloxy-benzyl)-2-(4-methyl-piperazin-1-yl)-2-oxo-ethyl]-amide;
- 4-Methyl-2-[methyl-(3-methyl-butyl)-amino]-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 4-Methyl-2-[methyl-(3-methyl-butyl)-amino]-pentanoic acid [1-(4-benzyloxy-benzyl)-2-oxo-2-piperidin-1-yl-ethyl]-amide;
- 4-Methyl-2-[methyl-(3-methyl-butyl)-amino]-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(2-piperidin-1-yl-ethylcarbamoyl)-ethyl]-amide;
- 4-Methyl-2-[methyl-(3-methyl-butyl)-amino]-pentanoic acid [1-(4-benzyloxy-benzyl)-2-(4-benzyl-piperazin-1-yl)-2-oxo-ethyl]-amide;
- 4-Methyl-2-[methyl-(3-methyl-butyl)-amino]-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(1-benzyl-piperidin-4-ylcarbamoyl)-ethyl]-amide;
- 4-Methyl-2-[methyl-(3-methyl-butyl)-amino]-pentanoic acid [1-(4-benzyloxy-benzyl)-2-(4-methyl-piperazin- 1-yl)-2-oxo-ethyl]-amide;
- 2-[(4-tert-Butyl-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-[(4-tert-Butyl-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(piperidine-1-carbonyl)-ethyl]-amide;
- 2-[(4-tert-Butyl-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(2-piperidin-1-yl-ethylcarbamoyl)-ethyl]-amide;
- 2-[(4-tert-Butyl-benzyl)-methyl-amino]-4-methyl-pentanoic acid [1-(4-benzyloxy-benzyl)-2-(4-benzyl-piperazin-1-yl)-2-oxo-ethyl]-amide;
- 2-[(4-tert-Butyl-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(1-benzyl-piperidin-4-yl-carbamoyl)-ethyl]-amide ;
- 2-[(4-tert-Butyl-benzyl)-methyl-amino]-4-methyl-pentanoic acid [1-(4-benzyloxy-benzyl)-2-(4-methyl-piperazin-1-yl)-2-oxo-ethyl]-amide;
- 2-(Cyclohexyl-methyl-amino)-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-(Cyclohexyl-methyl-amino)-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(piperidine-1-carbonyl)-ethyl]-amide;
- 2-(Cyclohexyl-methyl-amino)-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(2-piperidin-1-yl-ethylcarbamoyl)-ethyl]-amide;
- 2-(Cyclohexyl-methyl-amino)-4-methyl-pentanoic acid [1-(4-benzyloxy-benzyl)-2-(4-benzyl-piperazin-1-yl)-2-oxo-ethyl]-amide;
- 2-(Cyclohexyl-methyl-amino)-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(1-benzyl-piperidin-4-ylcarbamoyl)-ethyl]-amide;
- 2-(Cyclohexyl-methyl-amino)-4-methyl-pentanoic acid [1-(4-benzyloxy-benzyl)-2-(4-methyl-piperazin-1-yl)-2-oxo-ethyl]-amide;
- 2-(Cyclohexylmethyl-methyl-amino)-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-(Cyclohexylmethyl-methyl-amino)-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(piperidine-1-carbonyl)-ethyl]-amide;
- 2-(Cyclohexylmethyl-methyl-amino)-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(2-piperidin-1-yl-ethylcarbamoyl)-ethyl]-amide;
- 2-(Cyclohexylmethyl-methyl-amino)-4-methyl-pentanoic acid [1-(4-benzyloxy-benzyl)-2-(4-benzyl-piperazin-1-yl)-2-oxo-ethyl]-amide;
- 2-(Cyclohexylmethyl-methyl-amino)-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(1-benzyl-piperidin-4-ylcarbamoyl)-ethyl]-amide;
- 2-(Cyclohexylmethyl-methyl-amino)-4-methyl-pentanoic acid [1-(4-benzyloxy-benzyl)-2-(4-methyl-piperazin-1-yl)-2-oxo-ethyl]-amide;
- 3-(4-Benzyloxy-phenyl)-2-[4-methyl-2-(3-methyl-but-2-enylamino)-pentanoylam ino]-propionic acid tert-butyl ester;
- 3-(4-Benzyloxy-phenyl)-2-[2-(4-tert-butyl-benzylamino)-4-methyl-pentanoylam ino]-propionic acid tert-butyl ester;
- 2-(2-Benzylamino-4-methyl-pentanoylamino)-3-(4-benzyloxy-phenyl)-propionic acid tert-butyl ester;
- 4-Methyl-2-[methyl-(3-methyl-butyl)-amino]-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 4-Methyl-2-methylamino-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-[(3,3-Dimethyl-butyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-Diethylamino-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl-]-amide;
- 2-[(4-tert-Butyl-cyclohexyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 4-Methyl-2-[methyl-(4-methyl-cyclohexyl)-amino]-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-[(4-Dimethylamino-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbarnoyl-ethyl]-amide;
- 2-(Butyl-methyl-amino)-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-(Isobutyl-methyl-amino)-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 4-Methyl-2-methylamino-pentanoic acid [1-(4-benzyloxy-benzyl)-2-(4-benzyl-piperazin-1-yl)-2-oxo-ethyl]-amide;
- 3-Methyl-2-[methyl-(3-methyl-butyl)-amino]-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 4-Methyl-2-[ethyl-(3-methyl-butyl)-amino]-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 4-Methyl-2-[methyl-(3-methyl-butyl)-amino]-butyric acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-(Cyclohex-2-enyl-methyl-amino)-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-[(4-tert-Butyl-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-(Cyclohex-2-enylamino)-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-(4-tert-Butyl-benzylamino)-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 4-Methyl-2-[methyl-(3-methyl-but-2-enyl)-amino]-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-(4-tert-Butyl-benzylamino)-4-methyl-pentanoic acid [1-(4-benzyloxy-benzyl)-2-(4-benzyl-piperazin-1-yl)-2-oxo-ethyl]-amide;
- 4-Methyl-2-(3-methyl-but-2-enylamino)-pentanoic acid [1-(4-benzyloxy-benzyl)-2-(4-benzyl-piperazin-1-yl)-2-oxo-ethyl]-amide;
- 2-(Benzyl-methyl-amino)-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-[(4-tert-Butyl-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzylamino-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- and
- 2-(Cyclohexyl-methyl-amino)-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide.
A compound selected from:
- 2-[(4-Chloro-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-[(2-Chloro-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-[(3-Chloro-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-[(4-Methoxybenzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-[(4-Ethoxybenzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-[(3-Methoxybenzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-[(2-Methoxybenzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-[(4-Pyridyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-(2-Hydroxycyclohexyl-methyl-amino)-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 4-Methyl-2-[methyl-(N,N-dimethyl-3-amino-propyl)-amino]-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-(Cyclohexyl-amino)-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-[(Isoprop-2-yl)-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-[(Isoprop-2-yl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-[(N-methyl-piperidin-4-yl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-[(N-methyl-piperidin-4-yl)-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-[(Pyran-4-yl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-[(Pyran-4-yl)-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-Pyrrolidine-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-Piperidine-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-Hexamethyleneimine-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-[(4-Fluoro-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(piperidine-1-carbamoyl-ethyl]-amide;
- 2-[(4-Chloro-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(piperidine-1-carbamoyl-ethyl]-amide;
- 2-[(4-Bromo-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(piperidine-1-carbamoyl-ethyl]-amide;
- 2-[(2-Chloro-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(piperidine-1-carbamoyl-ethyl]-amide;
- 2-[(3-Chloro-benzyl)-methyl-amino-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(piperidine-1-carbamoyl-ethyl]-amide;
- 2-[(4-Hydroxybenzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(piperidine-1-carbamoyl-ethyl]-amide;
- 2-[(4-Methoxybenzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(piperidine-1-carbamoyl-ethyl]-amide;
- 2-[(4-Ethoxybenzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-(piperidine-1-carbamoyl-ethyl]-amide;
- 2-[(3-Methoxybenzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(piperidine-1-carbamoyl-ethyl]-amide;
- 2-[(2-Methoxybenzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(piperidine-1-carbamoyl-ethyl]-amide;
- 2-[(4-Pyridyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(piperidine-1-carbamoyl-ethyl]-amide;
- 2-[(2-Hydroxycyclohexyl-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(piperidine-1-carbamoyl-ethyl]-amide;
- 4-Methyl-2-[methyl-(N,N-dimethyl-3-amino-propyl)-amino]-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(piperidine-1-carbamoyl-ethyl]-amide;
- 2-(Cyclohexyl-amino)-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(piperidine-1-carbamoyl-ethyl]-amide;
- 2-(Isoprop-2-yl)-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(piperidine-1-carbamoyl-ethyl]-amide;
- 2-(Isoprop-2-yl)-methyl-amino)-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(piperidine-1-carbamoyl-ethyl]-amide;
- 2-[N-methyl-piperidin-4-yl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(piperidine-1-carbamoyl-ethyl]-amide;
- 2-[(N-methyl-piperidin-4-yl)-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(piperidine-1-carbamoyl-ethyl]-amide;
- 2-[(Pyran-4-yl)-methyl-amino]4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(piperidine-1-carbamoyl-ethyl]-amide;
- 2-[(Pyran-4-yl)-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(piperidine-1-carbamoyl-ethyl]-amide;
- 2-Pyrrolidine-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(piperidine-1-carbamoyl-ethyl]-amide;
- 2-Piperidine-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl-1-(piperidine-1-carbamoyl-ethyl]-amide;
- 2-Hexamethyleneimine-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(piperidine-1-carbamoyl-ethyl]-amide;
- 2-[(4-Fluoro-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-[(4-Chloro-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-[(4-Bromo-benzyl)-methyl-amino]4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-[(2-Chloro-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-[(3-Chloro-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-[(4-Hydroxybenzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-[(4-Methoxybenzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-[(4-Ethoxybenzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-[(3-Methoxybenzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-[(2-Methoxybenzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-[(4-Pyridyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-(2-Hydroxycyclohexyl-methyl-amino)-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 4-Methyl-2-[methyl-(N,N-dimethyl-3-amino-propyl)-amino]-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- 2-(Cyclohexyl-amino)-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-2-(4-methyl-piperazin-1-yl]-2-oxo-ethyl]-amide;
- 2-[(Isoprop-2-yl)-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-2-(4-methyl-piperazin-1-yl)-2-oxo-ethyl]-amide;
- 2-[(Isoprop-2-yl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-2-(4-methyl-piperazin-1-yl)-2-oxo-ethyl]-amide;
- 2-Pyrrolidine-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-2-(4-methyl-piperazin-1-yl)-2-oxo-ethyl]-amide;
- 2-Piperidine-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-2-(4-methyl-piperazin-1-yl)-2-oxo-ethyl]-amide;
- and
- 2-Hexamethyleneimine-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-2-(4-methyl-piperazin-1-yl)-2-oxo-ethyl]-amide.
The compounds:
- [S-(R*,R*)]-4-Methyl-2-[methyl-(3-methyl-butyl)-amino]-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(2-morpholin-4-yl-ethylcarbamoyl)-ethyl]-amide;
- [S-(R*,R* )]-4-Methyl-2-[methyl-(3-methyl-butyl)-amino]-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(2-pyridin-2-yl-ethylcarbamoyl)-ethyl]-amide;
- [S-(R*,R*)]-4-Methyl-2-[methyl-(3-methyl-butyl)-amino]-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(3-imidazol-1-yl-propylcarbamoyl)-ethyl]-amide;
- [S-(R*,R*)]-4-Methyl-2-[methyl-(3-methyl-butyl)-amino]-pentanoic acid [1-(2-benzylamino-ethylcarbamoyl)-2-(4-benzyloxy-phenyl)-ethyl]-amide;
- [S-(R*,R*)]-4-Methyl-2-[methyl-(3-methyl-butyl)-amino]-pentanoic acid [1-(4-benzyloxy-benzyl)-2-oxo-2-thiomorpholin-4-yl-ethyl]-amide;
- [S-(R* ,R*)]-4-Methyl-2-[methyl-(3-methyl-butyl)-amino]-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(2-hydroxy-1-hydroxymethyl-1-methyl-ethylcarbamo yl)-ethyl]-amide;
- [S-(R*,R*)]-4-Methyl-2-[methyl-(3-methyl-butyl)-amino]-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(1-methoxymethyl-propylcarbamoyl)-ethyl]-amide;
- [S-(R*,R*)]-4-Methyl-2-[methyl-(3-methyl-butyl)-amino]-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(2-pyrrolidin-1-yl-ethylcarbamoyl)-ethyl]-amide;
- [S-(R*,R*)]-4-Methyl-2-[methyl-(3-methyl-butyl)-amino]-pentanoic acid [1-(4-benzyloxy-benzyl)-2-(4-hydroxy-piperidin-1-yl)-2-oxo-ethyl]-amide;
- and
- [S-(R*,R*)]-4-Methyl-2-[methyl-(3-methyl-butyl)-amino]-pentanoic acid {2-(4-benzyloxy-phenyl)-1-[2-(2-hydroxy-ethylamino)-ethylcarbamoyl]-ethyl} -amide.
The compounds:
- [S-(R*,R*)]-4-Methyl-2-[methyl-(3-methyl-butyl)-amino]-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(1-benzyl-pyrrolidin-3-ylcarbamoyl)-ethyl]-amide ;
- [S-(R*,R*)]-4-Methyl-2-morpholin-4-yl-pentanoic acid [1-(2-benzylamino-ethylcarbamoyl)-2-(4-benzyloxy-phenyl)-ethyl]-amide;
- [S-(R*,R*)]-4-Methyl-2-morpholin-4-yl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(1-benzyl-pyrrolidin-3-ylcarbamoyl)-ethyl]-amide ;
- [S-(R*,R*)]-4-Methyl-2-morpholin-4-yl-pentanoic acid [1-(4-benzyloxy-benzyl)-2-oxo-2-piperidin-1-yl-ethyl]-amide;
- [S-(R*,R*)]-4-Methyl-2-(tetahydro-pyran-4-ylamino)-pentanoic acid [1-(2-benzylamino-ethylcarbamoyl)-2-(4-benzyloxy-phenyl)-ethyl]-amide;
- [S-(R*,R*)]-4-Methyl-2-(tetrahydro-pyran-4-ylamino)-pentanoic acid [1-(4-benzyloxy-benzyl)-2-oxo-2-thiomorpholin-4-yl-ethyl]-amide;
- [S-(R*,R*)]-4-Methyl-2-(tetrahydro-pyran-4-ylamino)-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(2-hydroxy-1,1-dimethyl-ethylcarbamoyl)-ethyl]-a mide;
- [S-(R*,R*)]-4-Methyl-2-(tetrahydro-pyran-4-ylamino)-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(1,1-bis-hydroxymethyl-propylcarbamoyl)-ethyl]-a mide;
- [S-(R*,R*)]-4-Methyl-2-(tetrahydro-pyran-4-ylamino)-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(1-methoxymethyl-propylcarbamoyl)-ethyl]-amide;
- and
- [S-(R*,R*)]-4-Methyl-2-(tetrahydro-pyran-4-ylamino)-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(1-benzyl-pyrrolidin-3-ylcarbamoyl)-ethyl]-amide .
The compounds:
- [S-(R*,R*)]-4-Methyl-2-(tetrahydro-pyran-4-ylamino)-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(2-piperidin-1-yl-ethylcarbamoyl)-ethyl]-amide;
- [S-(R*,R*)]-4-Methyl-2-(tetrahydro-pyran-4-ylamino)-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- [S-(R*,R*)]-4-Methyl-2-(tetrahydro-pyran-4-ylamino)-pentanoic acid [1-(4-benzyloxy-benzyl)-2-oxo-2-piperidin-1-yl-ethyl]-amide;
- [S-(R*,R*)]-2-[(4-Fluoro-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- [S-(R*,R*)]-2-[(4-Bromo-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- [S-(R*,R*)]-2-[(4-Hydroxy-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- [S-(R*,R*)]-4-Methyl-2-(methyl-pyridin-4-ylmethyl-amino)-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- [S-(R*,S*)]-4-Methyl-2-[methyl-(3-methyl-butyl)-amino]-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- [S-(R*,R*)]-3-(4-Benzyloxy-phenyl)-2-[4-methyl-2-(tetrahydro-pyran-4-ylamin o)-pentanoylamino]-propionic acid tert-butyl ester;
- and
- [S-(R*,R*)]-2-(Isopropyl-methyl-amino)-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide.
The compounds:
- [S-(R*,R*)]-4-Methyl-2-[methyl-(tetrahydro-pyran-4-yl)-amino]-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- [S-[R*,R*,(RS)]]-2-[(2-Hydroxy-1-methyl-ethyl)-methyl-amino]-4-methyl-penta noic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- [S-(R*,R*)]-4-Methyl-2-[methyl-(1H-pyrrol-2-ylmethyl)-amino]-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- [S-(R*,R*)]-2-(Furan-2-ylmethyl-methyl-amino)-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- [S-(R*,R*)]-3-(4-Benzyloxy-phenyl)-2-[2-(cyclohexylmethyl-amino)-4-methyl-p entanoylamino]-propionic acid tert-butyl ester;
- [S-(R*,R*)]-3-(4-Benzyloxy-phenyl)-2-(2-isopropylamino-4-methyl-pentanoylam ino)-propionic acid tert-butyl ester;
- [S-(R*,R*)]-3-3-(4-Benzyloxy-phenyl)-2-(2-cyclohexylamino-4-methyl-pentanoy lamino)-propionic acid tert-butyl ester;
- [S-(R*,R*)]-4-Methyl-2-morpholin-4-yl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- [S-(R*,R*)]-3-(4-Benzyloxy-phenyl)-2-[4-methyl-2-(3-methyl-butylamino)-pent anoylamino]-propionic acid tert-butyl ester;
- and
- [S-(R*,R*)]-({1-[2-(4-Benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethylcarbamoy l]-3-methyl-butyl}-methyl-amino)-acetic acid ethyl ester.
The compounds:
- [S-(R*,R*)]-2-[(3-Hydroxy-butyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- [S-(R*,R*)]-2-[(4-Methoxy-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- [S-(R*,R*)]-4-Methyl-2-piperidin-1-yl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- [S-(R*,R*)]-2-Ethylamino-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- [S-(R*,R*)]-4-Methyl-2-(methyl-pyridin-3-ylmethyl-amino)-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- [S-(R*,R*)]-3-(4-Benzyloxy-phenyl)-N-tert-butyl-2-{2-[methyl-(3-methyl-buty l)-amino]-acetylamino}-propionamide;
- [S-[R*,R*,(RS)]]-2-(sec-Butyl-methyl-amino)-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- (S)-N-[2-(4-Benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-2-(3-methyl-buty lamino)-isobutyramide;
- [S-(R*,R*)]-4-Methyl-2-(3-methyl-butylamino)-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- and
- 4-Methyl-2-[methyl-(tetrahydro-pyran-4-yl)-amino]-pentanoic acid [2-(4-benzyloxyphenyl)-1-(1-methoxymethyl-propylcarbamoyl)-ethyl]-amide.
The compounds:
- 4-Methyl-2-[methyl-(3-methylbutyl)-amino]3-pentanoic acid [2-(4-benzyloxyphenyl)-1-(1-methoxymethyl-propylcarbamoyl)-ethyl]-amide;
- 2-(Isopropyl-methyl-amino)-4-methyl-pentanioc acid [2-(4-benzyloxyphenyl)-1-(1-methoxymethyl-propylcarbamoyl)-ethyl]-amide;
- -2-[(4-tert-butyl-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxyphenyl)-1-(1-methoxymethyl-propylcarbamoyl)-ethyl]-amide;
- 2-[(4-Dimethylamino-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxyphenyl)-1-(1-methoxymethyl-propylcarbamoyl)-ethyl]-amide;
- 4-Methyl-2-[methyl-tetrahydropyran-4-yl)-amino]-pentanoic acid [2-(4-benzyloxyphenyl)-1-(1-propyl-piperidin-3-ylcarbamoyl)-ethyl]-amide;
- 4-Methyl-2-[methyl-(3-methyl-butyl-amino]-pentanoic acid [2-(4-benzyloxyphenyl)-1-(1-propyl-piperidin-3-ylcarbamoyl)-ethyl]-amide;
- 2-(Isopropyl-methyl-amino)-methyl-pentanoic acid [2-(4-benzyloxyphenyl)-1-(1-propyl-piperidin-3-ylcarbamoyl)-ethyl]-amide;
- 2-[(4-tertButyl-benzyl-)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxyphenyl)-1-(1-propyl-piperidin-3-ylcarbamoyl)-ethyl]-amide;
- 2-[(4-Dimethylamino-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy phenyl)-1-(1-propyl-piperidin-3-ylcarbamoyl)-ethyl]-amide;
- [S,(R*,R*)]-4-Methyl-2-piperidin-1-yl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- and
- [S,(R*,R*)]-4-Methyl-2-morpholin-4-yl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide monohydrochloride.
The compounds:
- [S-(R*,R*)]-2-Dimethylamino-4-methyl-pentanoic acid {1-tert-butylcarbamoyl-2-[4-(pyridin-3-ylmethoxy)-phenyl]-ethyl}-amide;
- [S-(R*,R*)]-2-(Cyclohexyl-methyl-amino)-4-methyl-pentanoic acid {1-tert-butylcarbamoyl-2-[4-(pyridin-3-ylmethoxy)-phenyl]-ethyl}-amide;
- [S-(R*,R*)]-4-Methyl-2-[methyl-(3-methyl-butyl)-amino]-pentanoic acid {1-tert-butylcarbamoyl-2-[4-(pyridin-3-ylmethoxy)-phenyl]-ethyl}-amide;
- [S-(R*,R*)]-2-[(4-tert-Butyl-benzyl)-methyl-amino]-4-methyl-pentanoic acid {1-tert-butylcarbamoyl-2-[4-(pyridin-3-ylmethoxy)-phenyl]-ethyl}-amide;
- [S-(R*,R*)]-2-[(3-Methoxy-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- [S-(R*,R*)]-2-[(2-Methoxy-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- [S-(R*,R*)]-2-[(4-Chloro-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- [S-(R*,R*)]-2-[(3-Chloro-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbarnoyl-ethyl]-amide;
- [S-(R*,R*)]-2-[(2-Chloro-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide;
- and
- [S-(R*,R*)]-4-Methyl-2-[methyl-(4-methylsulfanyl-benzyl)-amino]-pentanoic acid [2-(4-benzyloxy-phenyl)-1-tert-butylcarbamoyl-ethyl]-amide.
The compounds:
- [S-(R*,R*)]-4-Methyl-2-[methyl-(tetrahydro-pyran-4-yl)-amino]-pentanoic acid {2-(4-benzyloxy-phenyl)-1-[3-(2-oxo-pyrrolidin-1-yl)-propylcarbamoyl] -ethyl}-amide;
- [S-(R*,R*)]-4-Methyl-2-[methyl-(3-methyl-butyl)-amino]-pentanoic acid {2-(4-benzyloxy-phenyl)-1-[3-(2-oxo-pyrrolidin-1-yl)-propylcarbamoyl]-ethy l }-amide;
- [S-(R*,R*)]-2-(Isopropyl-methyl-amino)-4-methyl-pentanoic acid {2-(4-benzyloxy-phenyl)-1-[3-(2-oxo-pyrrolidin-1-yl)-propylcarbamoyl]-ethy l}-amide;
- [S-(R*,R*)]-2-[(3-Hydroxy-butyl)-methyl-amino]-4-methyl-pentanoic acid {2-(4-benzyloxy-phenyl)-1-[3-(2-oxo-pyrrolidin-1-yl)-propylcarbamoyl]-ethy l}-amide;
- [S-(R*,R*)]-2-[(4-tert-Butyl-benzyl)-methyl-amino]-4-methyl-pentanoic acid {2-(4-benzyloxy-phenyl)-1-[3-(2-oxo-pyrrolidin-1-yl)-propylcarbamoyl]-ethy l }-amide;
- [S-(R*,R*)]-2-[(4-Dimethylamino-benzyl)-methyl-amino]-4-methyl-pentanoic acid {2-(4-benzyloxy-phenyl)-1-[3-(2-oxo-pyrrolidin-1-yl)-propylcarbamoyl]-ethy l}-amide;
- [S-(R*,R*)]-2-(Isopropyl-methyl-amino)-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(2-piperidin-1-yl-ethylcarbamoyl)-ethyl]-amide;
- [S-(R*,R*)]-2-[(3-Hydroxy-butyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(2-piperidin-1-yl-ethylcarbamoyl)-ethyl]-amide;
- [S-(R*,R*)]-2-[(4-tert-Butyl-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(2-piperidin-1-yl-ethylcarbamoyl)-ethyl]-amide;
- and
- [S-(R*,R*)]-2-[(4-Dimethylamino-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(2-piperidin-1-yl-ethylcarbamoyl)-ethyl]-amide.
The compounds:
- [S-(R*,R*)]-4-Methyl-2-[methyl-(tetrahydro-pyran-4-yl)-amino]-pentanoic acid [1-(4-benzyloxy-benzyl)-2-[1,4']bipiperidinyl-1'-yl-2-oxo-ethyl]-amid e;
- [S-(R*,R*)]-4-Methyl-2-[methyl-(3-methyl-butyl)-amino]-pentanoic acid [1-(4-benzyloxy-benzyl)-2-[1,4']bipiperidinyl-1'-yl-2-oxo-ethyl]-amide;
- [S-(R*,R*)]-2-(Isopropyl-methyl-amino)-4-methyl-pentanoic acid [1-(4-benzyloxy-benzyl)-2-[1,4']bipiperidinyl-1'-yl-2-oxo-ethyl]-amide;
- 2-[(3-Hydroxy-butyl)-methyl-amino]-4-methyl-pentanoic acid [1-(4-benzyloxy-benzyl)-2-[1,4']bipiperidinyl-1'-yl-2-oxo-ethyl]-amide;
- [S-(R*,R*)]-2-[(4-tert-Butyl-benzyl)-methyl-amino]-4-methyl-pentanoic acid [1-(4-benzyloxy-benzyl)-2-[1,4']bipiperidinyl-1'-yl-2-oxo-ethyl]-amide;
- [S-(R*,R*)]-2-[(4-Dimethylamino-benzyl)-methyl-amino]-4-methyl-pentanoic acid [1-(4-benzyloxy-benzyl)-2-[1,4']bipiperidinyl-1'-yl-2-oxo-ethyl]-amide;
- [S-(R*,R*)]-2-[(4-tert-Butyl-benzyl)-methyl-amino]-4-methyl-pentanoic acid [1-(2-benzylamino-ethylcarbamoyl)-2-(4-benzyloxy-phenyl)-ethyl]-amide;
- and
- [S-(R*,R*)]-2-[(4-Dimethylamino-benzyl)-methyl-amino]-4-methyl-pentanoic acid [1-(2-benzylamino-ethylcarbamoyl)-2-(4-benzyloxy-phenyl)-ethyl]-amide.
The compounds:
- [S-(R*,R*)]-4-Methyl-2-[methyl-(tetrahydro-pyran-4-yl)-amino]-pentanoic acid [1-(2-benzylamino-ethylcarbamoyl)-2-(4-benzyloxy-phenyl)-ethyl]-amide ;
- [S-(R*,R*)-4-Methyl-2-[methyl-(3-methyl-butyl)-amino]-pentanoic acid [1-(2-benzylamino-ethylcarbamoyl)-2-(4-benzyloxy-phenyl)-ethyl]-amide;
- [S-(R*,R*)]-2-[(3-Hydroxy-butyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(1-propyl-piperidin-3-ylcarbamoyl)-ethyl]-amide;
- and
- [S-(R*,R*)]-4-Methyl-2-methyl-(3-methyl-butyl)-amino]-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(1-propyl-piperidin-3-ylcarbamoyl)-ethyl]-amide.
The compounds:
- [S-(R*,R*)]-2-(Isopropyl-methyl-amino)-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(3-imidazol-1-yl-propylcarbamoyl)-ethyl]-amide;
- 2-[(3-Hydroxy-butyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(1,1-bis-hydroxymethyl-propylcarbamoyl)-ethyl]-a mide;
- [S-(R*,R*)]-2-[(4-tert-Butyl-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(1,1-bis-hydroxymethyl-propylcarbamoyl)-ethyl]-a mide;
- [S-(R*,R*)]-2-[(4-Dimethylamino-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(1,1-bis-hydroxymethyl-propylcarbamoyl)-ethyl]-a mide;
- [S-(R*,R*)]-2-[(4-tert-Butyl-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(3-imidazol-1-yl-propylcarbamoyl)-ethyl]-amide;
- [S-(R*,R*)]-2-[(4-Dimethylamino-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(3-imidazol-1-yl-propylcarbamoyl)-ethyl]-amide;
- [S-(R*,R*)]-2-(Isopropyl-methyl-amino)-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(3-imidazol-1-yl-propylcarbamoyl)-ethyl]-amide;
- and
- [S-(R*,R*)]-2-[(3-Hydroxy-butyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(3-imidazol-1-yl-propylcarbamoyl)-ethyl]-amide.
The compounds:
- [S-(R*,R*)]-2-(Isopropyl-methyl-amino)-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(2-hydroxy-1,1-dimethyl-ethylcarbamoyl)-ethyl]-a mide;
- 2-[(3 -Hydroxy-butyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(2-hydroxy-1,1-dimethyl-ethylcarbamoyl)-ethyl]-a mide;
- 2-[(4-tert-Butyl-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(2-hydroxy-1,1-dimethyl-ethylcarbamoyl)-ethyl]-a mide;
- 2-[(4-Dimethylamino-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(2-hydroxy-1,1-dimethyl-ethylcarbamoyl)-ethyl]-a mide;
- and
- 2-[(3-Hydroxy-butyl)-methyl-amino]4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(1-methoxymethyl-propylcarbamoyl)-ethyl]-amide.
The compounds:
- [S-(R*,R*)]-4-Methyl-2-[methyl-(3-methyl-butyl)-amino]-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(2-hydroxy-1,1-dimethyl-ethylcarbamoyl)-ethyl]-a mide;
- [S-(R*,R*)]-4-methyl-2-(3-methyl-butylamino)-pentanoic acid [2-(4-phenethyl-phenyl)-1-tert-butylcarbamoyl-ethyl] amide;
- [S-(R*,R*)]-4-methyl-2-(3-methyl-butylamino)-pentanoic acid [2-(4-(2-cyclohexyl-ethyl)-phenyl)-1-tert-butylcarbamoyl-ethyl] amide;
- [S-(R*,R*)]-4-methyl-2-(3-methyl-butylamino)-pentanoic acid [2-(4-(2-cyclopentyl-ethyl)-phenyl)-1-tert-butylcarbamoyl-ethyl] amide;
- and
- [S-(R*,R*)]-4-methyl-2-(3-methyl-butylamino)-pentanoic acid [2-(4-(2-cyclohexyl-ethyl)-phenyl)-1-(1,1-bis-hydroxymethyl-propylcarbamoy l)-ethyl] amide.
The compounds:
- 4-Methyl-2-[methyl-(tetrahydro-pyran-4-yl)-amino]-pentanoic acid [2-(4-benzyloxyphenyl)-1-(1-methoxymethyl-propylcarbamoyl)-ethyl]-amide;
- 4-Methyl-2-[methyl-(3-methylbutyl)-amino]-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(1-methoxymethyl-propylcarbamoyl)-ethyl]-amide;
- 2-(Isopropyl-methyl-amino)-4-methyl-pentanioc acid [2-(4-benzyloxyphenyl)-1-(1-methoxymethyl-propylcarbamoyl)-ethyl]-amide;
- 2-[(4-tert-butyl-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxyphenyl)-1-(1-methoxymethyl-propylcarbamoyl)-ethyl]-amide;
- 2-[(4-Dimethylamino-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxyphenyl)-1-(1-methoxymethyl-propylcarbamoyl)-ethyl]-amide;
- 4-Methyl-2-[methyl-tetrahydropyran-4-yl)-amino]-pentanoic acid [2-(4-benzyloxyphenyl)-1-(1-propyl-piperidin-3-ylcarbamoyl)-ethyl]-amide;
- 4-Methyl-2-[methyl-(3-methyl-butyl-amino]-pentanoic acid [2-(4-benzyloxyphenyl)-1-(1-propyl-piperidin-3-ylcarbamoyl)-ethyl]-amide;
- 2-(Isopropyl-methyl-amino)-methyl-pentanoic acid [2-(4-benzyloxyphenyl)-1-(1-propyl-piperidin-3-ylcarbamoyl)-ethyl]-amide;
- 2-[(4-tertButyl-benzyl-)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxyphenyl)-1-(1-propyl-piperidin-3-ylcarbamoyl)-ethyl]-amide;
- and
- 2-[(4-Dimethylamino-benzyl)-methyl-amino]-4-methyl-pentanoic acid [2-(4-benzyloxyphenyl)-1-(1-propyl-piperidin-3-ylcarbamoyl)-ethyl]-amide.
The compounds:
- [S-(R*,R*)]-4-Methyl-2-morpholin-4-yl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(2-morpholin-4-yl-ethylcarbamoyl)-ethyl]-amide;
- [S-(R*,R*)]-4-Methyl-2-morpholin-4-yl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(2-pyridin-2-yl-ethylcarbamoyl)-ethyl]-amide;
- [S-(R*,R*)]-4-Methyl-2-morpholin-4-yl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(3-imidazol-1-yl-propylcarbamoyl)-ethyl]-amide;
- [S-(R*,R*)]-4-Methyl-2-morpholin-4-yl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(2-thiomorpholin-4-yl-ethylcarbamoyl)-ethyl]-ami de;
- [S-(R*,R*)]-4-Methyl-2-morpholin4-yl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(2-hydroxy-1,1-dimethyl-ethylcarbamoyl)-ethyl]-a mide;
- [S-(R*,R*)]-4-Methyl-2-morpholin-4-yl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(1,1-bis-hydroxymethyl-propyl-carbamoyl)-ethyl]- amide;
- [S-(R*,R*)]-4-Methyl-2-morpholin-4-yl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(2-pyrrolidin-1-yl-ethylcarbamoyl)-ethyl]-amide;
- [S-(R*,R*)]-4-Methyl-2-morpholin-4-yl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(4-hydroxypiperidinylcarbamoyl)-ethyl]-amide;
- [S-(R*,R*)]-4-Methyl-2-(tetrahydropyran-4-yl-amino)-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(2-morpholin-4-yl-ethylcarbamoyl)-ethyl]-amide;
- [S-(R*,R*)]-4-Methyl-2-(tetrahydropyran-4-yl-amino)-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(-(2-pyridin-2-yl-ethylcarbamoyl)-ethyl]-amide;
- [S-(R*,R*)]-4-Methyl-2-(tetrahydropyran-4-yl-amino)-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(3 -imidazol-1-yl-propylcarbamoyl)-ethyl]-amide;
- [S-(R*,R*)]-4-Methyl-2-(tetrahydropyran-4-yl-amino)-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(2-pyrrolidine-1-yl-ethylcarbamoyl]-amide;
- [S-(R*,R*)]-4-Methyl-2-(tetrahydropyran-4-yl-amino)-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(4-hydroxy-piperinylcarbamoyl]-amide;
- [S-(R*,R*)]-2-Dimethylamino-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(2-morpholin-4-yl-ethylcarbamoyl)-ethyl]-amide;
- [S-(R*,R*)]-2-Dimethylamino-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(2-(2-aminoethyl)pyridine carbamoyl)-ethyl]-amide;
- [S-(R*,R*)]-2-Dimethylamino-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(3-imidazol-1-yl-propylcarbamoyl)-ethyl]-amide;
- [S-(R*,R*)]-2-Dimethylamino-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(thiomorpholinecarbamol)-ethyl)-ethyl]-amide;
- [S-(R*,R*)]-2-Dimethylamino-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(2-aminopropan-1-ol carbamoyl)-ethyl]-amide;
- [S-(R*,R*)]-2-Dimethylamino-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(2 -hydroxymethylbutan-1-ol)-ethyl]-amide;
- [S-(R*,R*)]-2-Dimethylamino-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(1-methoxymethyl-propylcarbamoyl)-ethyl]-amide;
- [S-(R*,R*)]-2-Dimethylamino-4-methyl-pentanoic acid [2-(4-benzyloxy-phenyl)-1-(2-pyrrolidin-1-yl-ethylcarbamoyl)-ethyl]-amide;
- and
- [S-(R*,R*)]-2-Dimethylamino-4-methyl-pentanoic acid {2-(4-benzyloxy-phenyl)-1-[2-(2-hydroxy-ethylamino)-ethylcarbamoyl]-ethyl} -amide.
Dependencies are inferred from the claim text.