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Last Updated: March 28, 2024

Claims for Patent: 7,576,221


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Summary for Patent: 7,576,221
Title:Substituted imidazole derivatives
Abstract: The present invention relates to new substituted imidazole compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds. The compounds of the invention have the following general formula: ##STR00001##
Inventor(s): Wang; Weibo (Moraga, CA), Barsanti; Paul A. (Pleasant Hill, CA), Xia; Yia (Palo Alto, CA), Boyce; Rustum (Singapore, SG), Pecchi; Sabina (Oakland, CA), Brammeier; Nathan (Walnut Creek, CA), Phillips; Megan C. (Walnut Creek, CA), Mendenhall; Kris (Concord, CA), Wayman; Kelly (San Rafael, CA), Lagniton; Liana Marie (Berkeley, CA), Constantine; Ryan (Salt Lake City, UT), Yang; Hong (Pleasant Hill, CA), Mieuli; Elizabeth (Oakland, CA), Ramurthy; Savithri (Walnut Creek, CA), Jazan; Elisa (Richmond, CA), Sharma; Anu (El Cerrito, CA), Jain; Rama (Fremont, CA), Subramanian; Sharadha (San Ramon, CA), Renhowe; Paul A. (Danville, CA), Bair; Kenneth W. (Oakland, CA), Duhl; David (Oakland, CA), Walter; Annette (Mill Valley, CA), Abrams; Tinya (Richmond, CA), Huh; Kay (San Mateo, CA), Martin; Eric (El Cerrito, CA), Knapp; Mark (Oakland, CA), Le; Vincent P. (San Francisco, CA)
Assignee: Novartis Vaccines and Diagnostics, Inc. (Emeryville, CA)
Application Number:11/158,574
Patent Claims:1. A compound represented by the formula: ##STR00546## wherein: X.sup.1 is --C(O)--; A.sup.2 is selected from the group consisting of aryl, heteroaryl, heterocyclic, and cycloalkyl, all of which may be optionally substituted with 1 to 4 substituents selected from the group consisting of alkyl, substituted alkyl, alkoxy, substituted alkoxy, amino, halo, hydroxy, and nitro; A is selected from the group consisting of hydrogen, optionally substituted alkyl, optionally substituted alkoxy, optionally substituted aryl, carboxyl, carboxyl ester, aminoacyl, optionally substituted heteroaryl, optionally substituted heterocyclic, and optionally substituted cycloalkyl, wherein the optionally substituted groups are substituted with 1 to 4 substituents selected from the group consisting of alkyl, substituted alkyl, alkoxy, substituted alkoxy, amino, substituted amino, aryloxy, substituted aryloxy, cyano, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocyclic, substituted heterocyclic, heterocyclyloxy, substituted heterocyclyloxy, acyl, carboxyl, carboxyl ester, oxo (except when A is optionally substituted aryl or optionally substituted heteroaryl), halo, hydroxy, --S(O).sub.2--R.sup.9 where R.sup.9 is alkyl, substituted alkyl, aryl, substituted aryl, heteroaryl or substituted heteroaryl, and nitro; R.sup.8 is selected from the group consisting of alkyl, alkenyl, alkynyl, --CF.sub.3, alkoxy, cyano, halo, and hydroxy; R.sup.4 is -[alkylene].sub.p-NR.sup.10R.sup.11 wherein p is an integer from 0 to 1, alkylene is a straight chained alkylene optionally mono- or disubstituted with one of the foregoing substituents selected from the group consisting of amino, substituted amino, hydroxy, alkyl, substituted alkyl, carboxyl, carboxyl ester, oxo, spirocycloalkyl, and halo; R.sup.10 and R.sup.11 are independently selected from the group consisting of hydrogen, alkyl, substituted alkyl, --S(O)-alkyl, --S(O)-substituted alkyl, --S(O).sub.2-alkyl, --S(O).sub.2-substituted alkyl, heterocyclic, substituted heterocyclic, acyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, and substituted cycloalkyl or when R.sup.10 is hydrogen, R.sup.11 is hydroxy, alkoxy or substituted alkoxy; R.sup.15 is selected from the group consisting of ethyl, isopropyl, t-butyl, or phenyl; R.sup.16 is hydrogen or methyl; R.sup.17 is hydrogen or methyl; m.sup.1 is an integer equal to 0,1 or 2; or pharmaceutically acceptable salts, esters or prodrugs thereof.

2. The compound of claim 1, wherein R.sup.15 is t-butyl.

3. The compound of claim 1, wherein R.sup.17 is hydrogen.

4. The compound of claim 1, wherein A is unsubstituted and selected from the group consisting of 1,3-benzothiadiazol-4-yl, t-butoxy, butoxy, n-butoxy, carboxyl, cyclohexyl, 2,2-dimethylpropoxy, ethoxy, furan-3-yl, hydrogen, isoxazol-3-yl, methoxy, methyl, 2-methylpropoxy, phenyl, piperidin-3-yl, piperidin-4-yl, n-propoxy, pyridin-2-yl, pyrazin-2-yl, tetrahydrofuran-2-yl, tetrahydrofuran-3-yl, tetrahydro-2H-pyran-4-yl, 1H-tetrazol-1-yl, 2H-tetrazol-2-yl, thiazol-4-yl, 1,3,4-thiadiazol-2-yl, 1,3-benzothiadiazol-6-yl, 3,3-dihydrobenzo[1,2,3]thiadiazol-4-yl, benzimidazol-2-yl, benzimidazol-6-yl, benzo[1,2,5]thiadiazole, benzoxadiazol-4-yl, cyclopentyl, imidazol-4-yl, indazol-6-yl, isooxazol-5-yl, morpholin-2-yl morpholino, oxazol-4-yl, piperidin-N-yl, pyrazol-3-yl, pyrrolidin-2-yl'pyrrolidin-3-yl, pyrrolidin-N-yl, tetrazol-5-yl, and thiadiazol-4-yl.

5. The compound of claim 1, wherein A is a substituted aryl or heteroaryl group selected from the group consisting of 5-methyl-2H-imidazol-4yl, 2-aminothiazol-4-yl, 4-t-butylphenyl, 2-chlorophenyl, 2-chloro-6-methylpyrid-4-yl, 3-chlorophenyl, 4-chlorophenyl, 6-chloropyridin-3-yl, 3,4-dichlorophenyl, 2,4-difluorophenyl, 1,5-dimethyl-1H-pyrazol-3-yl, 2,4-dimethylthiazol-5-yl, 1-ethyl-3-methyl-1H-pyrazol-5-yl, 2-methoxyphenyl, 4-methoxyphenyl, 4-methylisoxazol-3-yl, 5-methylisoxazol-4-yl, 4-methylphenyl, 1-methyl-3-trifluoromethyl-1H-pyrazol-4-yl, 1-methyl-5-chloro-1H-pyrazol-4-yl, 5-methyl-1H-pyrazol-3-yl, 6-methylpyridin-3-yl, 2-pyrrolidin-3-ylphenyl, 4-(trifluoromethyl)phenyl, 6-(trifluoromethyl)pyridin-3-yl, 2,5-dimethyloxazol-4-yl, 2-aminothiazol-4-yl, 4-methylpyrazol-5-yl, 3-trifluoromethylpyrazol-4-yl, 2-methyl-3-trifluoromethylpyrazol-5-yl, 4-chloro-1,3-dimethylpyrazolo [3,4]pyridine, and 1-methylbenzimidazol-2-yl.

6. The compound of claim 1, wherein A is a substituted heterocyclic or cycloalkyl selected from the group consisting of 3-[(aminoacetyl)amino]cyclohexyl, 3-(2-aminoethylsulfonylamino)cyclohexyl, 1-methylpiperazin-4-yl, 1-methylcarbonylpiperidin-4-yl, 1-methoxycarbonylpiperidin-4-yl, quinuclidin-3-yl, 2-oxopyrrolidin-5-yl, 2-oxopyrrolidin-4-yl, 2-oxo-dihydrofuran-5-yl, 2-oxothiazolidin-4-yl, and 3-hydroxypyrrolidin-5-yl.

7. The compound of claim 1, wherein A is a substituted alkyl selected from the group consisting of 3-amino-2-oxo-1(2H)-pyridinylmethyl, cyanomethyl, (N,N-dimethylamino)methyl, ethoxymethyl, p-fluorophenoxymethyl, hydroxymethyl, 1H-imidazol-1-ylmethyl, methoxymethyl, (N-methylamino)methyl, methylsulfonylmethyl, (5-methyl-1H-tetrazol-1-yl)methyl, (5-methyl-2H-tetrazol-2-yl)methyl, morpholin-4-ylmethyl, 1H-pyrazol-1-ylmethyl, 1H-1,2,3-triazol-1-ylmethyl, 2H-1,2,3-triazol-2-ylmethyl, 1H-1,2,4-triazol-1-ylmethyl, 2H-1,2,4-triazol-2-ylmethyl, 4H-1,2,4-triazol-4-ylmethyl, 1H-tetrazol-1-ylmethyl, 1H-tetrazol-5-ylmethyl, 2H-tetrazol-2-ylmethyl, imidazol-4-ylmethyl, 1-methylpyrazol-3-ylmethyl, piperidin-4-ylmethyl, trifluoromethyl, dimethylaminoethyl, and 2-oxo-3-aminopyrrolidin-1-ylmethyl.

8. The compound of claim 1, wherein A is N-methylaminocarbonyl.

9. The compound of claim 1, wherein R.sup.4 is selected from the group consisting of: --(CH.sub.2).sub.2-NH.sub.2, --CH.sub.2CH(NH.sub.2)CH.sub.2OH, --(CH.sub.2).sub.3--NH.sub.2, --(CH.sub.2).sub.3--NHCH.sub.3, --(CH.sub.2).sub.3--N(CH.sub.3).sub.2, --(CH.sub.2).sub.3--NHOCH.sub.3, --(CH.sub.2).sub.3--NHSO.sub.2CH.sub.3, --(CH.sub.2).sub.3NH-(5-cyanopyridin-2-yl), --(CH.sub.2).sub.3NH-cyclopropyl, --(CH.sub.2).sub.3NH-cyclobutyl, --(CH.sub.2).sub.3NH(2-hydroxymethylphenyl), --(CH.sub.2).sub.3NH-(5-trifluoromethylpyridin-2-yl), --(CH.sub.2).sub.3NHCH.sub.2-cyclopropyl, --(CH.sub.2).sub.3NHCH.sub.2-{5-(pyridin-3-yloxy)-1H-indazol-3-yl}, --(CH.sub.2).sub.3NHCH.sub.2-(5-methoxy-1-H-indazol-3-yl), --(CH.sub.2).sub.3NHCH.sub.2-(6-fluoro-1H-indazol-3-yl), --CH.sub.2CHOHCH.sub.2NH.sub.2, --CH.sub.2CH(CH.sub.2OH)CH.sub.2NH.sub.2, --CH.sub.2C(CH.sub.3).sub.2CH.sub.2--N(CH.sub.3).sub.2, --(CH.sub.2).sub.2CH(NH.sub.2)C(O)NH.sub.2, --(CH.sub.2).sub.2CH(NH.sub.2)C(O)OH, --(CH.sub.2).sub.2CH(NH.sub.2)CH.sub.2C(O)NH.sub.2, --(CH.sub.2).sub.2CH(NH.sub.2)CH.sub.2OH, --(CH.sub.2).sub.2CH(NH.sub.2)CH.sub.3, --(CH.sub.2).sub.3NHC(O)CH.sub.2NH.sub.2, --(CH.sub.2).sub.3NHC(O)CH(NH.sub.2)CH(CH.sub.3).sub.2, --CH.sub.2CHFCH.sub.2NH.sub.2, --(CH.sub.2).sub.2NHC(O)CH.sub.2NH.sub.2, --(CH.sub.2).sub.3--NHCH.sub.2CH.sub.2OH, --(CH.sub.2).sub.3-NHCH.sub.2CO.sub.2H, --(CH.sub.2).sub.3--NHCH.sub.2CO.sub.2CH.sub.2CH.sub.3, --(CH.sub.2).sub.3--N(CH.sub.2CH.sub.2OH).sub.2, --(CH.sub.2).sub.3-NHCH(CH.sub.2OH).sub.2, --(CH.sub.2).sub.2CH(NH.sub.2)CH.sub.2OH, --(CH.sub.2).sub.2C(CH.sub.3).sub.2NH.sub.2, --(CH.sub.2).sub.2CH(NH.sub.2)CH.sub.2OCH.sub.3, --(CH.sub.2).sub.2CH(NH.sub.2)CH.sub.2F, --CH.sub.2CHFCH(NH.sub.2)CH.sub.2OH, and (CH2)2spirocyclopropyl-NH2.

10. The compound of claim 1, wherein A.sup.2 is selected from the group consisting of phenyl, 6-aminopyridin-2-yl, 3-chlorophenyl, 3-cyanophenyl, 2,4-difluorophenyl, 2,5-difluorophenyl, 3,5-difluorophenyl, 2-fluorophenyl, 3-fluorophenyl, 4-fluorophenyl, 3-hydroxyphenyl, 3-methoxyphenyl, 1-(5-methyl)-isoxazol-3-yl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, tetrahydropyran-4-yl, thiazol-4-yl, and 5-trifluoromethylfuran-2-yl.

11. The compound of claim 1, wherein R.sup.16 is hydrogen.

12. The compound of claim 1, wherein ##STR00547## is selected from the group consisting of phenyl, 3-bromophenyl, 3-chlorophenyl, 4-cyanophenyl, 2,5-difluorophenyl, 3-fluorophenyl, 2-methoxyphenyl, 3-methoxyphenyl, 4-methoxyphenyl, 4-methylphenyl, 2-trifluoromethylphenyl, and 3-trifluoromethylphenyl.

13. A compound of claim 1 selected from the group consisting of: N-(3-aminopropyl)-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2-methyl- propyl]-4-methylbenzamide; N-(3-aminopropyl)-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2-methyl- propyl]benzamide; N-(3-aminopropyl)-N-[(R)-(1-benzyl-4-phenyl-1H-imidazol-2-yl)(phenyl)meth- yl]-4-methylbenzamide; N-(3-aminopropyl)-N-[(R)-(1-benzyl-4-phenyl-1H-imidazol-2-yl)(phenyl)meth- yl]benzamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-bromophenyl)-1H-imidazol-2-yl]- -2-methylpropyl}benzamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-bromophenyl)-1H-imidazol-2-yl]- -2-methylpropyl}-4-methylbenzamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-bromophenyl)-1H-imidazol-2-yl]- -2-methylpropyl}-4-(trifluoromethyl)benzamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-bromophenyl)-1H-imidazol-2-yl]- -2-methylpropyl}-2,4-difluorobenzamide; N-(3-aminopropyl)-4-methyl-N-{2-methyl-1-[1-(3-methylbenzyl)-4-phenyl-1H-- imidazol-2-yl]propyl}benzamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-methoxyphenyl)-1H-imidazol-2-y- l]-2-methylpropyl}benzamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-methoxyphenyl)-1H-imidazol-2-y- l]-2-methylpropyl}-4-methylbenzamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-methoxyphenyl)-1H-imidazol-2-y- l]-2-methylpropyl}-4-(trifluoromethyl)benzamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-methoxyphenyl)-1H-imidazol-2-y- l]-2-methylpropyl}-2,4-difluorobenzamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}benzamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}-4-methylbenzamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}-4-(trifluoromethyl)benzamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}-2,4-difluorobenzamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(4-methylphenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}benzamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(4-methylphenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}-4-methylbenzamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(4-methylphenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}-4-(trifluoromethyl)benzamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(4-methylphenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}-2,4-difluorobenzamide; N-(3-aminopropyl)-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-dime- thylpropyl]-4-methylbenzamide; N-(3-aminopropyl)-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-dime- thylpropyl]benzamide; N-(3-aminopropyl)-N-{(1R)-1-[1-(3,5-difluorobenzyl)-4-phenyl-1H-imidazol-- 2-yl]-2-methylpropyl}-4-methylbenzamide; N-(3-aminopropyl)-N-{(1R)-1-[1-(3,5-difluorobenzyl)-4-phenyl-1H-imidazol-- 2-yl]-2-methylpropyl}benzamide; N-{(1R)-1-[1-benzyl-4-(3-bromophenyl)-1H-imidazol-2-yl]-2-methylpropyl}-4- -methyl-N-{3-[(methylsulfonyl)amino]propyl}benzamide; N-(3-aminopropyl)-4-methyl-N-{(1R)-2-methyl-1-[1-(4-methylbenzyl)-4-pheny- l-1H-imidazol-2-yl]propyl}benzamide; N-(3-aminopropyl)-N-{(1R)-2-methyl-1-[1-(4-methylbenzyl)-4-phenyl-1H-imid- azol-2-yl]propyl}benzamide; N-(3-aminopropyl)-4-methyl-N-{(1R)-2-methyl-1-[1-(2-methylbenzyl)-4-pheny- l-1H-imidazol-2-yl]propyl}benzamide; N-(3-aminopropyl)-N-{(1R)-2-methyl-1-[1-(2-methylbenzyl)-4-phenyl-1H-imid- azol-2-yl]propyl}benzamide; N-(3-aminopropyl)-N-((1R)-1-{1-benzyl-4-[2-(trifluoromethyl)phenyl]-1H-im- idazol-2-yl}-2-methylpropyl)benzamide; N-(3-aminopropyl)-N-((1R)-1-{1-benzyl-4-[2-(trifluoromethyl)phenyl]-1H-im- idazol-2-yl}-2-methylpropyl)-4-methylbenzamide; N-(3-aminopropyl)-N-((1R)-1-{1-benzyl-4-[2-(trifluoromethyl)phenyl]-1H-im- idazol-2-yl}-2-methylpropyl)-2,4-difluorobenzamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}-4-methoxybenzamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}-3-chlorobenzamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}-4-chlorobenzamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}-4-tert-butylbenzamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}-3,4-dichlorobenzamide; N-{(1R)-1-[1-benzyl-4-(3-bromophenyl)-1H-imidazol-2-yl]-2-methylpropyl}-N- -{3-[(5-cyanopyridin-2-yl)amino]propyl}benzamide; N-{(1R)-1-[1-benzyl-4-(3-bromophenyl)-1H-imidazol-2-yl]-2-methylpropyl}-N- -(3-{[5-(trifluoromethyl)pyridin-2-yl]amino}propyl)benzamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}cyclohexanecarboxamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}-6-chloronicotinamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2,2-dimethylpropyl}benzamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2,2-dimethylpropyl}-4-methylbenzamide; N-(3-aminopropyl)-N-{(1R)-1-[4-(3-chlorophenyl)-1-(2,4-difluorobenzyl)-1H- -imidazol-2-yl]-2,2-dimethylpropyl}benzamide; N-(3-aminopropyl)-N-{(1R)-1-[4-(3-chlorophenyl)-1-(2,4-difluorobenzyl)-1H- -imidazol-2-yl]-2,2-dimethylpropyl}-4-methylbenzamide; N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2-methylpropyl]-N-[3-(dime- thylamino)-2,2-dimethylpropyl]benzamide; N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2-methylpropyl]-N-[3-(dime- thylamino)-2,2-dimethylpropyl]-4-methylbenzamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2,2-dimethylpropyl}-6-chloronicotinamide; N-(3-aminopropyl)-6-chloro-N-{(1R)-1-[4-(3-chlorophenyl)-1-(3,5-difluorob- enzyl)-1H-imidazol-2-yl]-2,2-dimethylpropyl}nicotinamide; N-(3-aminopropyl)-N-[(1R)-1-(1-benzyl-5-methyl-4-phenyl-1H-imidazol-2-yl)- -2-methylpropyl]benzamide; N-(3-aminopropyl)-N-[(1R)-1-(1-benzyl-5-methyl-4-phenyl-1H-imidazol-2-yl)- -2-methylpropyl]-4-methylbenzamide; N-(3-aminopropyl)-N-[(1R)-1-(1-benzyl-5-methyl-4-phenyl-1H-imidazol-2-yl)- -2-methylpropyl]-2,4-difluorobenzamide; N-(3-aminopropyl)-N-[(1R)-1-(1-benzyl-5-methyl-4-phenyl-1H-imidazol-2-yl)- -2-methylpropyl]-6-chloronicotinamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}-2-chlorobenzamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}-2-chloro-6-methylisonicotinamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}-3-furamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}-5-methyl-2H-imidazole-4-carboxamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}-2-methoxybenzamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}pyridine-2-carboxamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}-1,5-dimethyl-1H-pyrazole-3-carboxamide; N-(3-aminopropyl)-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-1,2-dime- thylpropyl]benzamide; N-(3-aminopropyl)-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-1,2-dime- thylpropyl]-4-methylbenzamide; N-(2-aminoethyl)-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2-methylp- ropyl]-4-methylbenzamide; N-(2-aminoethyl)-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2-methylp- ropyl]benzamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}-1,3-thiazole-4-carboxamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}-4-methylisoxazole-3-carboxamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}isoxazole-3-carboxamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}-5-methyl-1H-pyrazole-3-carboxamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}-2,4-dimethyl-1,3-thiazole-5-carboxamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}tetrahydrofuran-3-carboxamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}piperidine-4-carboxamide; 2-amino-N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imida- zol-2-yl]-2-methylpropyl}-1,3-thiazole-4-carboxamide; N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-dimethylpropyl]-N-[3-(- cyclobutylamino)propyl]benzamide; N-(3-aminopropyl)-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-dime- thylpropyl]-6-methylnicotinamide; N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-dimethylpropyl]-N-{3-[- (cyclopropylmethyl)amino]propyl}benzamide; N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-dimethylpropyl]-N-(3-{- [(6-fluoro-1H-indazol-3-yl)methyl]amino}propyl)benzamide; N-(3-aminopropyl)-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-dime- thylpropyl]-1,5-dimethyl-1H-pyrazole-3-carboxamide; N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-dimethylpropyl]-N-[(3R- )-3,5-diamino-5-oxopentyl]benzamide; N-{3-[(aminoacetyl)amino]propyl}-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol- -2-yl)-2,2-dimethylpropyl]benzamide; N-{2-[(aminoacetyl)amino]ethyl}-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-- 2-yl)-2,2-dimethylpropyl]benzamide; (2R)-N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol- -2-yl]-2-methylpropyl}tetrahydrofuran-2-carboxamide; (2S)-N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol- -2-yl]-2-methylpropyl}tetrahydrofuran-2-carboxamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}pyrazine-2-carboxamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}-1-methyl-3-(trifluoromethyl)-1H-pyrazole-4-carboxamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}-5-chloro-1-methyl-1H-pyrazole-4-carboxamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}-2-(dimethylamino)acetamide; N-(3-aminopropyl)-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2-methyl- propyl]-1,5-dimethyl-1H-pyrazole-3-carboxamide; N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-dimethylpropyl]-N-{3-[- (2-hydroxyethyl)amino]propyl}benzamide; N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-dimethylpropyl]-N-[3-(- cyclopropylamino)propyl]benzamide; N-(3-aminopropyl)-N-{(1R)-2-methyl-1-[4-phenyl-1-(1,3-thiazol-4-ylmethyl)- -1H-imidazol-2-yl]propyl}benzamide; N-(3-aminopropyl)-4-methyl-N-{(1R)-2-methyl-1-[4-phenyl-1-(1,3-thiazol-4-- ylmethyl)-1H-imidazol-2-yl]propyl}benzamide; N-(3-aminopropyl)-2,4-difluoro-N-{(1R)-2-methyl-1-[4-phenyl-1-(1,3-thiazo- l-4-ylmethyl)-1H-imidazol-2-yl]propyl}benzamide; N-(3-aminopropyl)-6-chloro-N-{(1R)-2-methyl-1-[4-phenyl-1-(1,3-thiazol-4-- ylmethyl)-1H-imidazol-2-yl]propyl}nicotinamide; N-(3-aminopropyl)-N-[(1R)-1-(1-benzyl-4-pyridin-2-yl-1H-imidazol-2-yl)-2,- 2-dimethylpropyl]-6-chloronicotinamide; N-(2-amino-3-hydroxypropyl)-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl- )-2-methylpropyl]benzamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}-5-methylisoxazole-4-carboxamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}acetamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}-2-(4-fluorophenoxy)acetamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}-2-(1H-imidazol-1-yl)acetamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}-2-morpholin-4-ylacetamide; [(3-{benzoyl[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-dimethylprop- yl]amino}propyl)amino]acetic acid; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}-2-hydroxyacetamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}-2-methoxyacetamide; N-(3-aminopropyl)-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-dime- thylpropyl]-2-hydroxyacetamide; N-(3-aminopropyl)-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-dime- thylpropyl]-2-methoxyacetamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}-1-ethyl-3-methyl-1H-pyrazole-5-carboxamide; ethyl[(3-{benzoyl[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-dimethy- lpropyl]amino}propyl)amino]acetate; N-{3-[(2-amino-3-methylbutanoyl)amino]propyl}-N-[(1R)-1-(1-benzyl-4-pheny- l-1H-imidazol-2-yl)-2,2-dimethylpropyl]benzamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}tetrahydro-2H-pyran-4-carboxamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}-2-(methylamino)acetamide; N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-dimethylpropyl]-N-{3-[- bis(2-hydroxyethyl)amino]propyl}benzamide; N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-dimethylpropyl]-N-(3-{- [2-hydroxy-1-(hydroxymethyl)ethyl]amino}propyl)benzamide; N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-dimethylpropyl]-N-(3-{- [2-(hydroxymethyl)phenyl]amino}propyl)benzamide; N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl]-2-methylpropyl}-- N-piperidin-4-ylbenzamide; N-[(2R)-3-amino-2-fluoropropyl]-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-- 2-yl)-2,2-dimethylpropyl]benzamide; (3R)-N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol- -2-yl]-2-methylpropyl}piperidine-3-carboxamide; (3S)-N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol- -2-yl]-2-methylpropyl}piperidine-3-carboxamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}-2-(1H-1,2,4-triazol-1-yl)acetamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-chlorophenyl)-1H-imidazol-2-yl- ]-2-methylpropyl}-2,1,3-benzothiadiazole-4-carboxamide; N-[(2S)-3-amino-2-hydroxypropyl]-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol- -2-yl)-2,2-dimethylpropyl]benzamide; N-[(2S)-3-amino-2-fluoropropyl]-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-- 2-yl)-2,2-dimethylpropyl]-1,5-dimethyl-1H-pyrazole-3-carboxamide; N-[(2S)-3-amino-2-hydroxypropyl]-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol- -2-yl)-2,2-dimethylpropyl]-1,5-dimethyl-1H-pyrazole-3-carboxamide; N-[(2S)-3-amino-2-hydroxypropyl]-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol- -2-yl)-2,2-dimethylpropyl]-2-methoxyacetamide; N-[(2R)-3-amino-2-fluoropropyl]-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-- 2-yl)-2,2-dimethylpropyl]-1,5-dimethyl-1H-pyrazole-3-carboxamide; methyl

3-aminopropyl[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-dimethylpro- pyl]carbamate; N-(3-aminopropyl)-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-dime- thylpropyl]-2-(1H-tetrazol-1-yl)acetamide; N-(3-aminopropyl)-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-dime- thylpropyl]-2-(2H-tetrazol-2-yl)acetamide; N-(3-aminopropyl)-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-dime- thylpropyl]-2-(1H-1,2,4-triazol-1-yl)acetamide; N-(3-aminopropyl)-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-dime- thylpropyl]-2-(4H-1,2,4-triazol-4-yl)acetamide; N-(3-aminopropyl)-N-[(1S)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2-hydrox- y-2-methylpropyl]benzamide; (2S)-N-(3-aminopropyl)-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2- -dimethylpropyl]tetrahydrofuran-2-carboxamide; N-(3-aminopropyl)-N-{(1R)-1-[4-(3-chlorophenyl)-1-(3-cyanobenzyl)-1H-imid- azol-2-yl]-2-methylpropyl}benzamide; N-(3-aminopropyl)-N-{(1R)-1-[4-(3-chlorophenyl)-1-(3-cyanobenzyl)-1H-imid- azol-2-yl]-2-methylpropyl}-4-methylbenzamide; N-(3-aminopropyl)-N-{(1R)-1-[4-(3-chlorophenyl)-1-(3-methylbenzyl)-1H-imi- dazol-2-yl]-2-methylpropyl}-4-methylbenzamide; N-(3-aminopropyl)-N-{(1R)-1-[4-(3-chlorophenyl)-1-(3-methylbenzyl)-1H-imi- dazol-2-yl]-2-methylpropyl}benzamide; ethyl 3-aminopropyl[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-dimethylpro- pyl]carbamate; neopentyl 3-aminopropyl[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-dimethylpro- pyl]carbamate; isobutyl 3-aminopropyl[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-dimethylpro- pyl]carbamate; propyl 3-aminopropyl[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-dimethylpro- pyl]carbamate; N-(3-aminopropyl)-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-dime- thylpropyl]-2-cyanoacetamide; butyl 3-aminopropyl[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-dimethylpro- pyl]carbamate; N-[(2R)-3-amino-2-fluoropropyl]-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-- 2-yl)-2,2-dimethylpropyl]-2-(2H-tetrazol-2-yl)acetamide; N-[(2R)-3-amino-2-fluoropropyl]-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-- 2-yl)-2,2-dimethylpropyl]-2-(1H-tetrazol-1-yl)acetamide; N-[(2R)-3-amino-2-fluoropropyl]-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-- 2-yl)-2,2-dimethylpropyl]-2-methoxyacetamide; N-[(2S)-3-amino-2-fluoropropyl]-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-- 2-yl)-2,2-dimethylpropyl]-2-methoxyacetamide; N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-dimethylpropyl]-N-[(3S- )-3,4-diamino-4-oxobutyl]benzamide; N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-dimethylpropyl]-N-[(3R- )-3,4-diamino-4-oxobutyl]benzamide; N-[(3S)-3-amino-4-hydroxybutyl]-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-- 2-yl)-2,2-dimethylpropyl]benzamide; (2S)-2-amino-4-{benzoyl[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-d- imethylpropyl]amino}butanoic acid; N-[(2R)-3-amino-2-fluoropropyl]-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-- 2-yl)-2,2-dimethylpropyl]-2-hydroxyacetamide; N-(3-aminopropyl)-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-dime- thylpropyl]-2-(1H-tetrazol-5-yl)acetamide; N-[(2S)-3-amino-2-hydroxypropyl]-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol- -2-yl)-2,2-dimethylpropyl]-2-hydroxyacetamide; N-[(2S)-3-amino-2-fluoropropyl]-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-- 2-yl)-2,2-dimethylpropyl]-2-(1H-tetrazol-1-yl)acetamide; N-[(2S)-3-amino-2-fluoropropyl]-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-- 2-yl)-2,2-dimethylpropyl]-2-(2H-tetrazol-2-yl)acetamide; N-(3-aminopropyl)-N-{(1R)-1-[1-(3-cyanobenzyl)-4-phenyl-1H-imidazol-2-yl]- -2,2-dimethylpropyl}benzamide; N-(3-aminopropyl)-N-{(1R)-1-[1-(3-cyanobenzyl)-4-phenyl-1H-imidazol-2-yl]- -2,2-dimethylpropyl}-2-methoxyacetamide; N-(3-aminopropyl)-N-{(1R)-2,2-dimethyl-1-[1-(3-methylbenzyl)-4-phenyl-1H-- imidazol-2-yl]propyl}-2-methoxyacetamide; N-[(3S)-3-amino-4-hydroxybutyl]-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-- 2-yl)-2,2-dimethylpropyl]-1,5-dimethyl-1H-pyrazole-3-carboxamide; N-(3-amino-2-hydroxypropyl)-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl- )-2,2-dimethylpropyl]-2-(1H-tetrazol-1-yl)acetamide; N-(3-amino-2-hydroxypropyl)-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl- )-2,2-dimethylpropyl]-2-(2H-tetrazol-2-yl)acetamide; N-(3-aminopropyl)-N-{(1R)-2,2-dimethyl-1-[1-(3-methylbenzyl)-4-phenyl-1H-- imidazol-2-yl]propyl}benzamide; N-[(3S)-3-amino-4-hydroxybutyl]-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-- 2-yl)-2,2-dimethylpropyl]-2-methoxyacetamide; N-[(2S)-3-amino-2-fluoropropyl]-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-- 2-yl)-2,2-dimethylpropyl]-2-(1H-1,2,3-triazol-1-yl)acetamide; N-[(2S)-3-amino-2-fluoropropyl]-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-- 2-yl)-2,2-dimethylpropyl]-2-(2H-1,2,3-triazol-2-yl)acetamide; N-[(3S)-3-amino-4-hydroxybutyl]-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-- 2-yl)-2,2-dimethylpropyl]-2-(1H-tetrazol-1-yl)acetamide; N-[(3S)-3-amino-4-hydroxybutyl]-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-- 2-yl)-2,2-dimethylpropyl]-2-(2H-tetrazol-2-yl)acetamide; N-[(3S)-3-amino-4-hydroxybutyl]-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-- 2-yl)-2,2-dimethylpropyl]-2-(1H-1,2,3-triazol-1-yl)acetamide; N-(3-aminopropyl)-2-hydroxy-N-{(1R)-1-[-(3-hydroxybenzyl)-4-phenyl-1H-imi- dazol-2-yl]-2,2-dimethylpropyl}acetamide; N-(3-aminopropyl)-N-{(1R)-2,2-dimethyl-1-[1-(3-methylbenzyl)-4-phenyl-1H-- imidazol-2-yl]propyl}-1,5-dimethyl-1H-pyrazole-3-carboxamide; N-(3-aminopropyl)-N-{(1R)-1-[1-(3-hydroxybenzyl)-4-phenyl-1H-imidazol-2-y- l]-2,2-dimethylpropyl}benzamide; N-(3-aminopropyl)-N-{(1R)-1-[1-(3-methoxybenzyl)-4-phenyl-1H-imidazol-2-y- l]-2,2-dimethylpropyl}benzamide; N-(3-aminopropyl)-2-methoxy-N-{(1R)-1-[1-(3-methoxybenzyl)-4-phenyl-1H-im- idazol-2-yl]-2,2-dimethylpropyl}acetamide; N-(3-aminopropyl)-N-{(1R)-1-[1-(3-cyanobenzyl)-4-phenyl-1H-imidazol-2-yl]- -2,2-dimethylpropyl}-2-hydroxyacetamide; N-(3-aminopropyl)-N-{(1R)-1-[1-(3-methoxybenzyl)-4-phenyl-1H-imidazol-2-y- l]-2,2-dimethylpropyl}-1,5-dimethyl-1H-pyrazole-3-carboxamide; N-[(3S)-3-amino-4-methoxybutyl]-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-- 2-yl)-2,2-dimethylpropyl]benzamide; N-(3-aminopropyl)-N-{(1R)-1-[1-(3-cyanobenzyl)-4-phenyl-1H-imidazol-2-yl]- -2,2-dimethylpropyl}-1,5-dimethyl-1H-pyrazole-3-carboxamide; N-[(2R)-3-amino-2-fluoropropyl]-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-- 2-yl)-2,2-dimethylpropyl]-2-(1H-1,2,3-triazol-1-yl)acetamide; N-[(2R)-3-amino-2-fluoropropyl]-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-- 2-yl)-2,2-dimethylpropyl]-2-(2H-1,2,3-triazol-2-yl)acetamide; N-(3-aminopropyl)-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-dime- thylpropyl]-2-ethoxyacetamide; N-[(2S)-3-amino-2-fluoropropyl]-N-[(1S)-1-(1-benzyl-4-phenyl-1H-imidazol-- 2-yl)-2-hydroxy-2-methylpropyl]-2-(1H-tetrazol-1-yl)acetamide; N-[(2S)-3-amino-2-fluoropropyl]-N-[(1S)-1-(1-benzyl-4-phenyl-1H-imidazol-- 2-yl)-2-hydroxy-2-methylpropyl]-2-(2H-tetrazol-2-yl)acetamide; N-[(2S)-3-amino-2-fluoropropyl]-N-{(1R)-1-[1-benzyl-4-(3-fluorophenyl)-1H- -imidazol-2-yl]-2,2-dimethylpropyl}-2-(1H-tetrazol-1-yl)acetamide; N-[(2S)-3-amino-2-fluoropropyl]-N-{(1R)-1-[1-benzyl-4-(3-fluorophenyl)-1H- -imidazol-2-yl]-2,2-dimethylpropyl}-2-(2H-tetrazol-2-yl)acetamide; N-[(2S)-3-amino-2-(hydroxymethyl)propyl]-N-[(1R)-1-(1-benzyl-4-phenyl-1H-- imidazol-2-yl)-2,2-dimethylpropyl]-N'-methylethanediamide; N-[(2R)-3-amino-2-(hydroxymethyl)propyl]-N-[(1R)-1-(1-benzyl-4-phenyl-1H-- imidazol-2-yl)-2,2-dimethylpropyl]-N'-methylethanediamide; N-[(3R)-3-amino-4-hydroxybutyl]-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-- 2-yl)-2,2-dimethylpropyl]-2-methoxyacetamide; N-[(3R)-3-amino-4-hydroxybutyl]-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-- 2-yl)-2,2-dimethylpropyl]-2-(1H-tetrazol-1-yl)acetamide; N-[(3R)-3-amino-4-hydroxybutyl]-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-- 2-yl)-2,2-dimethylpropyl]-2-(2H-tetrazol-2-yl)acetamide; N-[(3S)-3-amino-4-hydroxybutyl]-N-{(1R)-1-[1-benzyl-4-(3-fluorophenyl)-1H- -imidazol-2-yl]-2,2-dimethylpropyl}-2-(1H-tetrazol-1-yl)acetamide; N-[(3S)-3-amino-4-hydroxybutyl]-N-{(1R)-1-[1-benzyl-4-(3-fluorophenyl)-1H- -imidazol-2-yl]-2,2-dimethylpropyl}-2-(2H-tetrazol-2-yl)acetamide; N-[(3S)-3-amino-4-methoxybutyl]-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-- 2-yl)-2,2-dimethylpropyl]-2-methoxyacetamide; N-[(3S)-3-amino-4-hydroxybutyl]-N-{(1R)-1-[1-benzyl-4-(3-fluorophenyl)-1H- -imidazol-2-yl]-2,2-dimethylpropyl}-2-methoxyacetamide; N-[(2R)-3-amino-2-fluoropropyl]-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-- 2-yl)-2,2-dimethylpropyl]-2-(5-methyl-2H-tetrazol-2-yl)acetamide; N-[(2R)-3-amino-2-fluoropropyl]-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-- 2-yl)-2,2-dimethylpropyl]-2-(5-methyl-1H-tetrazol-1-yl)acetamide; N-[(2S,3R)-3-amino-2-fluoro-4-hydroxybutyl]-N-[(1R)-1-(1-benzyl-4-phenyl-- 1H-imidazol-2-yl)-2,2-dimethylpropyl]-2-methoxyacetamide; N-[(3S)-3-amino-4-fluorobutyl]-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2- -yl)-2,2-dimethylpropyl]-2-methoxyacetamide; N-[(3R)-3-amino-4-fluorobutyl]-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2- -yl)-2,2-dimethylpropyl]-2-methoxyacetamide; N-((R)-3-Amino-2-fluoro-propyl)-N-{(R)-1-[1-benzyl-4-(3-methoxy-phenyl)-1- H-imidazol-2-yl]-2,2-dimethyl-propyl}-2-ethoxy-acetamide; N-((R)-3-Amino-2-fluoro-propyl)-N-{(R)-1-[1-benzyl-4-(3-methoxy-phenyl)-1- H-imidazol-2-yl]-2,2-dimethyl-propyl}-2-methoxy-acetamide; N-((R)-3-Amino-2-fluoro-propyl)-N-[(R)-1-(1-benzyl-4-phenyl-1H-imidazol-2- -yl)-2,2-dimethyl-propyl]-2-ethoxy-acetamide; (S)-Tetrahydro-furan-2-carboxylic acid ((R)-3-amino-2-fluoro-propyl)-[(R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)- -2,2-dimethyl-propyl]-amide; N-((S)-3-Amino-4-fluoro-butyl)-N-[(R)-2,2-dimethyl-1-(4-phenyl-1-pyridin-- 3-ylmethyl-1H-imidazol-2-yl)-propyl]-2-methoxy-acetamide; N-((R)-3-Amino-4-fluoro-butyl)-N-[(R)-2,2-dimethyl-1-(4-phenyl-1-pyridin-- 3-ylmethyl-1H-imidazol-2-yl)-propyl]-2-methoxy-acetamide; N-((S)-3-Amino-4-methoxy-butyl)-N-{(R)-1-[1-benzyl-4-(3-fluoro-phenyl)-1H- -imidazol-2-yl]-2,2-dimethyl-propyl}-2-methoxy-acetamide; N-((R)-3-Amino-2-fluoro-propyl)-N-{(R)-1-[1-benzyl-4-(4-cyano-phenyl)-1H-- imidazol-2-yl]-2,2-dimethyl-propyl}-2-methoxy-acetamide; N-((R)-3-Amino-2-fluoro-propyl)-N-{(R)-1-[1-benzyl-4-(4-methoxy-phenyl)-1- H-imidazol-2-yl]-2,2-dimethyl-propyl}-2-methoxy-acetamide; N-((R)-3-Amino-2-fluoro-propyl)-N-{(R)-1-[1-(2-fluoro-benzyl)-4-phenyl-1H- -imidazol-2-yl]-2,2-dimethyl-propyl}-2-methoxy-acetamide; N-((R)-3-Amino-2-fluoro-propyl)-N-{(R)-1-[1-(3-fluoro-benzyl)-4-phenyl-1H- -imidazol-2-yl]-2,2-dimethyl-propyl}-2-methoxy-acetamide; N-((R)-3-Amino-2-fluoro-propyl)-N-{(R)-1-[1-(3-chloro-benzyl)-4-phenyl-1H- -imidazol-2-yl]-2,2-dimethyl-propyl}-2-methoxy-acetamide; N-((R)-3-Amino-2-fluoro-propyl)-N-{(R)-1-[1-(3-cyano-benzyl)-4-phenyl-1H-- imidazol-2-yl]-2,2-dimethyl-propyl}-2-methoxy-acetamide; N-((R)-3-Amino-2-fluoro-propyl)-N-{(R)-2,2-dimethyl-1-[4-phenyl-1-(tetrah- ydro-pyran-4-ylmethyl)-1H-imidazol-2-yl]-propyl}-2-methoxy-acetamide; (S)-Tetrahydro-furan-2-carboxylic acid ((R)-3-amino-2-fluoro-propyl)-{(R)-1-[1-benzyl-4-(3-fluoro-phenyl)-1H-imi- dazol-2-yl]-2,2-dimethyl-propyl}-amide; (S)-Tetrahydro-furan-2-carboxylic acid ((R)-3-amino-2-fluoro-propyl)-{(R)-1-[1-benzyl-4-(2-methoxy-phenyl)-- 1H-imidazol-2-yl]-2,2-dimethyl-propyl}-amide; (S)-Tetrahydro-furan-2-carboxylic acid ((R)-3-amino-2-fluoro-propyl)-{(R)-1-[1-benzyl-4-(3-trifluoromethyl-pheny- l)-1H-imidazol-2-yl]-2,2-dimethyl-propyl}-amide; (S)-Tetrahydro-furan-2-carboxylic acid ((R)-3-amino-2-fluoro-propyl)-{(R)-1-[1-benzyl-4-(3-bromo-phenyl)-1H-imid- azol-2-yl]-2,2-dimethyl-propyl}-amide; N-((R)-3-Amino-2-fluoro-propyl)-N-{(R)-1-[1-benzyl-4-(3-fluoro-phenyl)-1H- -imidazol-2-yl]-2,2-dimethyl-propyl}-2-methoxy-acetamide; N-((R)-3-Amino-2-fluoro-propyl)-N-{(R)-1-[1-benzyl-4-(2-methoxy-phenyl)-1- H-imidazol-2-yl]-2,2-dimethyl-propyl}-2-methoxy-acetamide; N-((R)-3-Amino-2-fluoro-propyl)-N-{(R)-1-[1-benzyl-4-(3-trifluoromethyl-p- henyl)-1H-imidazol-2-yl]-2,2-dimethyl-propyl}-2-methoxy-acetamide; N-((R)-3-Amino-2-fluoro-propyl)-N-{(R)-1-[1-benzyl-4-(3-bromo-phenyl)-1H-- imidazol-2-yl]-2,2-dimethyl-propyl}-2-methoxy-acetamide; N-((R)-3-Amino-2-fluoro-propyl)-N-[(R)-1-(1-benzyl-4-p-tolyl-1H-imidazol-- 2-yl)-2,2-dimethyl-propyl]-2-methoxy-acetamide; N-((S)-3-Amino-4-fluoro-butyl)-N-[(R)-2,2-dimethyl-1-(4-phenyl-1-pyridin-- 4-ylmethyl-1H-imidazol-2-yl)-propyl]-2-methoxy-acetamide; N-((R)-3-Amino-4-fluoro-butyl)-N-[(R)-2,2-dimethyl-1-(4-phenyl-1-pyridin-- 4-ylmethyl-1H-imidazol-2-yl)-propyl]-2-methoxy-acetamide; N-((S)-3-Amino-4-fluoro-butyl)-N-{(R)-2,2-dimethyl-1-[1-(5-methyl-isoxazo- l-3-ylmethyl)-4-phenyl-1H-imidazol-2-yl]-propyl}-2-methoxy-acetamide; N-((R)-3-Amino-4-fluoro-butyl)-N-{(R)-2,2-dimethyl-1-[1-(5-methyl-isoxazo- l-3-ylmethyl)-4-phenyl-1H-imidazol-2-yl]-propyl}-2-methoxy-acetamide; N-((S)-3-Amino-4-fluoro-butyl)-N-[(R)-2,2-dimethyl-1-(4-phenyl-1-pyridin-- 2-ylmethyl-1H-imidazol-2-yl)-propyl]-2-methoxy-acetamide; N-((R)-3-Amino-4-fluoro-butyl)-N-[(R)-2,2-dimethyl-1-(4-phenyl-1-pyridin-- 2-ylmethyl-1H-imidazol-2-yl)-propyl]-2-methoxy-acetamide; N-((S)-3-Amino-4-fluoro-butyl)-N-{(R)-1-[1-benzyl-4-(3-fluoro-phenyl)-1H-- imidazol-2-yl]-2,2-dimethyl-propyl}-2-methoxy-acetamide; N-((R)-3-Amino-4-fluoro-butyl)-N-{(R)-1-[1-benzyl-4-(3-fluoro-phenyl)-1H-- imidazol-2-yl]-2,2-dimethyl-propyl}-2-methoxy-acetamide; N-(3-Amino-3-methyl-butyl)-N-[(R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-- 2,2-dimethyl-propyl]-2-methoxy-acetamide; N-((S)-3-Amino-2-fluoro-propyl)-N-{(R)-2,2-dimethyl-1-[4-phenyl-1-(5-trif- luoromethyl-furan-2-ylmethyl)-1H-imidazol-2-yl]-propyl}-2-methoxy-acetamid- e; N-((S)-3-Amino-2-fluoro-propyl)-N-{(R)-2,2-dimethyl-1-[1-(5-methyl-isox- azol-3-ylmethyl)-4-phenyl-1H-imidazol-2-yl]-propyl}-2-methoxy-acetamide; (S)-Tetrahydro-furan-2-carboxylic acid ((S)-3-amino-2-fluoro-propyl)-{(R)-2,2-dimethyl-1-[1-(5-methyl-isoxazol-3- -ylmethyl)-4-phenyl-1H-imidazol-2-yl]-propyl}-amide; (S)-Tetrahydro-furan-2-carboxylic acid ((S)-3-amino-2-fluoro-propyl)-{(R)-2,2-dimethyl-1-[4-phenyl-1-(5-trifluor- omethyl-furan-2-ylmethyl)-1H-imidazol-2-yl]-propyl}-amide; N-((S)-3-Amino-4-methoxy-butyl)-N-{(R)-1-[1-(3-fluoro-benzyl)-4-(3-fluoro- -phenyl)-1H-imidazol-2-yl]-2,2-dimethyl-propyl}-2-methoxy-acetamide; N-((S)-3-Amino-4-hydroxy-butyl)-N-{(R)-1-[1-(3-fluoro-benzyl)-4-(3-fluoro- -phenyl)-1H-imidazol-2-yl]-2,2-dimethyl-propyl}-2-methoxy-acetamide; N-((S)-3-Amino-4-fluoro-butyl)-N-{(R)-1-[1-(2,5-difluoro-benzyl)-4-phenyl- -1H-imidazol-2-yl]-2,2-dimethyl-propyl}-2-methoxy-acetamide; N-((R)-3-Amino-4-fluoro-butyl)-N-{(R)-1-[1-(2,5-difluoro-benzyl)-4-phenyl- -1H-imidazol-2-yl]-2,2-dimethyl-propyl}-2-methoxy-acetamide; N-((R)-3-Amino-2-fluoro-propyl)-N-{(R)-1-[1-(4-fluoro-benzyl)-4-phenyl-1H- -imidazol-2-yl]-2,2-dimethyl-propyl}-2-methoxy-acetamide; N-((R)-3-Amino-2-fluoro-propyl)-2-methoxy-N-{(R)-1-[1-(3-methoxy-benzyl)-- 4-phenyl-1H-imidazol-2-yl]-2,2-dimethyl-propyl}-acetamide; N-((R)-3-Amino-2-fluoro-propyl)-N-{(R)-2,2-dimethyl-1-[1-(2-methyl-benzyl- )-4-phenyl-1H-imidazol-2-yl]-propyl}-2-methoxy-acetamide; N-((R)-3-Amino-2-fluoro-propyl)-N-{(R)-2,2-dimethyl-1-[1-(3-methyl-benzyl- )-4-phenyl-1H-imidazol-2-yl]-propyl}-2-methoxy-acetamide; N-((S)-3-Amino-2-fluoro-propyl)-N-{(R)-2,2-dimethyl-1-[1-(3-methyl-benzyl- )-4-phenyl-1H-imidazol-2-yl]-propyl}-2-methoxy-acetamide; N-(3-Amino-propyl)-N-[(R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-dime- thyl-propyl]-acetamide; N-((S)-3-Amino-2-fluoro-propyl)-N-[(R)-1-(1-benzyl-1H-imidazol-2-yl)-2,2-- dimethyl-propyl]-2-methoxy-acetamide; (S)-Tetrahydro-furan-2-carboxylic acid ((S)-3-amino-2-fluoro-propyl)-[(R)-1-(1-benzyl-1H-imidazol-2-yl)-2,2- -dimethyl-propyl]-amide; N-((S)-3-Amino-4-fluoro-butyl)-N-{(R)-1-[1-(3-fluoro-benzyl)-4-(3-fluoro-- phenyl)-1H-imidazol-2-yl]-2,2-dimethyl-propyl}-2-methoxy-acetamide; N-((R)-3-Amino-4-fluoro-butyl)-N-{(R)-1-[1-(3-fluoro-benzyl)-4-(3-fluoro--

phenyl)-1H-imidazol-2-yl]-2,2-dimethyl-propyl}-2-methoxy-acetamide; N-[2-(1-Amino-cyclopropyl)-ethyl]-N-[(R)-1-(1-benzyl-4-phenyl-1H-imidazol- -2-yl)-2,2-dimethyl-propyl]-2-methoxy-acetamide; (S)-Tetrahydro-furan-2-carboxylic acid [2-(1-amino-cyclopropyl)-ethyl]-[(R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-y- l)-2,2-dimethyl-propyl]-amide; [2-(1-Amino-cyclopropyl)-ethyl]-[(R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-y- l)-2,2-dimethyl-propyl]-carbamic acid methyl ester; N-[2-(1-Amino-cyclopropyl)-ethyl]-N-{(R)-1-[1-benzyl-4-(3-fluoro-phenyl)-- 1H-imidazol-2-yl]-2,2-dimethyl-propyl}-2-methoxy-acetamide; (S)-Tetrahydro-furan-2-carboxylic acid [2-(1-amino-cyclopropyl)-ethyl]-{(R)-1-[1-benzyl-4-(3-fluoro-phenyl)-1H-i- midazol-2-yl]-2,2-dimethyl-propyl}-amide; N-(3-Amino-propyl)-N-{(R)-1-[1-benzyl-4-(2,5-difluoro-phenyl)-1H-imidazol- -2-yl]-2,2-dimethyl-propyl}-2-methoxy-acetamide; N-((S)-3-Amino-4-fluoro-butyl)-N-{(R)-1-[1-benzyl-4-(2,5-difluoro-phenyl)- -1H-imidazol-2-yl]-2,2-dimethyl-propyl}-2-methoxy-acetamide; N-((R)-3-Amino-4-fluoro-butyl)-N-{(R)-1-[1-benzyl-4-(2,5-difluoro-phenyl)- -1H-imidazol-2-yl]-2,2-dimethyl-propyl}-2-methoxy-acetamide; N-(3-Amino-propyl)-N-{1-[1-(3-fluoro-benzyl)-4-(3-fluoro-phenyl)-1H-imida- zol-2-yl]-1-methyl-ethyl}-2-methoxy-acetamide; N-(3-Amino-propyl)-N-{(R)-1-[1-(3-fluoro-benzyl)-4-(3-fluoro-phenyl)-1H-i- midazol-2-yl]-2,2-dimethyl-propyl}-2-methoxy-acetamide; (S)-Tetrahydro-furan-2-carboxylic acid ((S)-3-amino-4-fluoro-butyl)-{(R)-1-[1-(3-fluoro-benzyl)-4-(3-fluoro-phen- yl)-1H-imidazol-2-yl]-2,2-dimethyl-propyl}-amide; N-((S)-3-Amino-4-methoxy-butyl)-N-{(R)-1-[4-(3-chloro-phenyl)-1-(3-fluoro- -benzyl)-1H-imidazol-2-yl]-2-methyl-propyl}-2-methoxy-acetamide; N-((S)-3-Amino-4-fluoro-butyl)-N-{(R)-1-[1-benzyl-4-(3-chloro-phenyl)-1H-- imidazol-2-yl]-2-methyl-propyl}-2-methoxy-aceamide; N-((S)-3-Amino-4-fluoro-butyl)-N-{(R)-1-[4-(3-chloro-phenyl)-1-(3-fluoro-- benzyl)-1H-imidazol-2-yl]-2-methyl-propyl}-2-methoxy-acetamide; N-(3-Amino-4-fluoro-butyl)-N-{1-[1-(3-fluoro-benzyl)-4-(3-fluoro-phenyl)-- 1H-imidazol-2-yl]-1-methyl-ethyl}-2-methoxy-acetamide; N-((S)-3-Amino-4-fluoro-butyl)-N-{(R)-1-[1-(3-fluoro-benzyl)-4-(3-fluoro-- phenyl)-1H-imidazol-2-yl]-2,2-dimethyl-propyl}-acetamide; N-((R)-3-Amino-4-fluoro-butyl)-N-{(R)-1-[1-(3-fluoro-benzyl)-4-(3-fluoro-- phenyl)-1H-imidazol-2-yl]-2,2-dimethyl-propyl}-acetamide; (S)-Tetrahydro-furan-2-carboxylic acid ((S)-3-amino-2-fluoro-propyl)-{(R)-1-[1-(3-fluoro-benzyl)-4-(3-fluoro-phe- nyl)-1H-imidazol-2-yl]-2,2-dimethyl-propyl}-amide; (3-Amino-4-fluoro-butyl)-{(R)-1-[1-(3-fluoro-benzyl)-4-(3-fluoro-phenyl)-- 1H-imidazol-2-yl]-2,2-dimethyl-propyl}-carbamic acid methyl ester; N-((S)-3-Amino-4-fluoro-butyl)-N-{(R)-1-[1-(3-fluoro-benzyl)-4-(3-fluoro-- phenyl)-1H-imidazol-2-yl]-2,2-dimethyl-propyl}-formamide; N-((R)-3-Amino-4-fluoro-butyl)-N-{(R)-1-[1-(3-fluoro-benzyl)-4-(3-fluoro-- phenyl)-1H-imidazol-2-yl]-2,2-dimethyl-propyl}-formamide; N-(3-Dimethylamino-propyl)-N-{(R)-1-[1-(3-fluoro-benzyl)-4-(3-fluoro-phen- yl)-1H-imidazol-2-yl]-2,2-dimethyl-propyl}-2-methoxy-acetamide; N-((S)-3-Amino-butyl)-N-{(R)-1-[1-(3-fluoro-benzyl)-4-(3-fluoro-phenyl)-1- H-imidazol-2-yl]-2,2-dimethyl-propyl}-2-methoxy-acetamide; N-((R)-3-Amino-butyl)-N-{(R)-1-[1-(3-fluoro-benzyl)-4-(3-fluoro-phenyl)-1- H-imidazol-2-yl]-2,2-dimethyl-propyl}-2-methoxy-acetamide; N-((S)-3-Amino-4-fluoro-butyl)-N-{(R)-1-[1-(6-amino-pyridin-2-ylmethyl)-4- -(3-fluoro-phenyl)-1H-imidazol-2-yl]-2,2-dimethyl-propyl}-2-methoxy-acetam- ide; N-((R)-3-Amino-4-fluoro-butyl)-N-{(R)-1-[1-(6-amino-pyridin-2-ylmethy- l)-4-(3-fluoro-phenyl)-1H-imidazol-2-yl]-2,2-dimethyl-propyl}-2-methoxy-ac- etamide; N-((S)-3-Amino-4-fluoro-butyl)-N-{(R)-1-[4-(3-fluoro-phenyl)-1-(3- -hydroxy-benzyl)-1H-imidazol-2-yl]-2,2-dimethyl-propyl}-2-methoxy-acetamid- e; N-((R)-3-Amino-4-fluoro-butyl)-N-{(R)-1-[4-(3-fluoro-phenyl)-1-(3-hydro- xy-benzyl)-1H-imidazol-2-yl]-2,2-dimethyl-propyl}-2-methoxy-acetamide; N-{(R)-1-[1-(3-Fluoro-benzyl)-4-(3-fluoro-phenyl)-1H-imidazol-2-yl]-2,2-d- imethyl-propyl}-2-methoxy-N-(3-methylamino-propyl)-acetamide; N-(3-Amino-propyl)-N-{(R)-1-[1-benzyl-4-(2,5-difluoro-phenyl)-1H-imidazol- -2-yl]-2,2-dimethyl-propyl}-acetamide; (3-Amino-propyl)-{(R)-1-[1-benzyl-4-(2,5-difluoro-phenyl)-1H-imidazol-2-y- l]-2,2-dimethyl-propyl}-carbamic acid methyl ester; (S)-Tetrahydro-furan-2-carboxylic acid (3-amino-propyl)-{(R)-1-[1-benzyl-4-(2,5-difluoro-phenyl)-1H-imidazol-2-y- l]-2,2-dimethyl-propyl}-amide; 3-[{(R)-1-[1-(3-Fluoro-benzyl)-4-(3-fluoro-phenyl)-1H-imidazol-2-yl]-2,2-- dimethyl-propyl}-(2-methoxy-acetyl)-amino]-propionamide; N-(3-Amino-propyl)-N-{(R)-1-[1-benzyl-4-(2,5-difluoro-phenyl)-1H-imidazol- -2-yl]-2,2-dimethyl-propyl}-2-methanesulfonyl-acetamide; N-((S)-3-Amino-4-methoxy-butyl)-N-{(R)-1-[1-benzyl-4-(2,5-difluoro-phenyl- )-1H-imidazol-2-yl]-2,2-dimethyl-propyl}-2-methoxy-acetamide; (S)-Tetrahydro-furan-2-carboxylic acid ((S)-3-amino-4-fluoro-butyl)-{(R)-1-[1-benzyl-4-(2,5-difluoro-phenyl)-1H-- imidazol-2-yl]-2,2-dimethyl-propyl}-amide; (S)-Tetrahydro-furan-2-carboxylic acid ((S)-3-amino-4-methoxy-butyl)-{(R)-1-[1-benzyl-4-(2,5-difluoro-phenyl)-1H- -imidazol-2-yl]-2,2-dimethyl-propyl}-amide; N-((R)-3-Amino-butyl)-N-{(R)-1-[1-benzyl-4-(2,5-difluoro-phenyl)-1H-imida- zol-2-yl]-2,2-dimethyl-propyl}-2-methoxy-acetamide; N-((S)-3-Amino-butyl)-N-{(R)-1-[1-benzyl-4-(2,5-difluoro-phenyl)-1H-imida- zol-2-yl]-2,2-dimethyl-propyl}-2-methoxy-acetamide; N-((S)-3-Amino-4-fluoro-butyl)-N-{(R)-1-[1-benzyl-4-(2,5-difluoro-phenyl)- -1H-imidazol-2-yl]-2,2-dimethyl-propyl}-acetamide; and ((S)-3-Amino-4-fluoro-butyl)-{(R)-1-[1-benzyl-4-(2,5-difluoro-phenyl)-1H-- imidazol-2-yl]-2,2-dimethyl-propyl}-carbamic acid methyl ester; or a pharmaceutically acceptable salt thereof.

14. A pharmaceutical composition comprising a therapeutically effective amount of a compound of claim 1 and a pharmaceutically acceptable carrier.

15. The composition of claim 14 further comprising at least one additional agent for the treatment of cancer.

16. The composition of claim 15, wherein the additional agent for the treatment of cancer is selected from the group consisting of irinotecan, topotecan, gemcitabine, imatinib, trastuzumab, 5-fluorouracil, leucovorin, carboplatin, cisplatin, docetaxel, paclitaxel, tezacitabine, cyclophosphamide, vinca alkaloids, anthracyclines, rituximab, and trastuzumab.

17. The compound claim 1 wherein alkylene is a straight chained alkylene mono- or disubstituted with one of the foregoing substituents selected from the group consisting of amino, substituted amino, hydroxy, alkyl, substituted alkyl, carboxyl, carboxyl ester, oxo, spirocycloalkyl, and halo.

18. The compound of claim 17 wherein R.sup.4 is selected from the group consisting of --CH.sub.2CH(NH.sub.2)CH.sub.2OH, --CH.sub.2CHOHCH.sub.2NH.sub.2, --CH.sub.2CH(CH.sub.2OH)CH.sub.2NH.sub.2, --CH.sub.2C(CH.sub.3).sub.2CH.sub.2--N(CH.sub.3).sub.2, --(CH.sub.2).sub.2CH(NH.sub.2)C(O)OH, --(CH.sub.2).sub.2CH(NH.sub.2)CH.sub.2OH, --(CH.sub.2).sub.2CH(NH.sub.2)CH.sub.3, --CH.sub.2CHFCH.sub.2NH.sub.2, --(CH.sub.2).sub.2CH(NH.sub.2)CH.sub.2OH, --(CH.sub.2).sub.2C(CH.sub.3).sub.2NH.sub.2, --(CH.sub.2).sub.2CH(NH.sub.2)CH.sub.2F, --CH.sub.2CHFCH(NH.sub.2)CH.sub.2OH, and (CH2) 2spirocyclopropyl-NH2.

Details for Patent 7,576,221

Applicant Tradename Biologic Ingredient Dosage Form BLA Approval Date Patent No. Expiredate
Genentech, Inc. RITUXAN rituximab Injection 103705 11/26/1997 ⤷  Try a Trial 2024-06-18
Idec Pharmaceuticals Corp. RITUXAN rituximab Injection 103737 02/19/2002 ⤷  Try a Trial 2024-06-18
Genentech, Inc. HERCEPTIN trastuzumab For Injection 103792 09/25/1998 ⤷  Try a Trial 2024-06-18
Genentech, Inc. HERCEPTIN trastuzumab For Injection 103792 02/10/2017 ⤷  Try a Trial 2024-06-18
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