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Last Updated: July 14, 2020

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Claims for Patent: 8,318,791

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Summary for Patent: 8,318,791
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:12/455,798
Patent Claims:1. A method of treating a colon cancer in a mammalian patient comprising administering to a mammalian patient in need of such treatment a therapeutically effective amount of 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 a pharmaceutically acceptable salts thereof.

2. The method of claim 1, further comprising administering to the mammalian patient one additional agent for the treatment of cancer.

3. The method of claim 2, wherein the additional agent for the treatment of cancer is selected from the group consisting of irinotecan, topotecan, gemcitabine, imatinib, 5-fluorouracil, leucovorin, carboplatin, cisplatin, docetaxel, paclitaxel, tezacitabine, cyclophosphamide, vinca alkaloids, anthracyclines, rituximab, and trastuzumab.

4. The method of claim 1, wherein R.sup.15 is t-butyl.

5. The method of claim 1, wherein R.sup.17 is hydrogen.

6. The method 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, 2,2dimethylpropoxy, ethoxy, furan-3-yl, hydrogen, isoxazol-3-yl, methoxy, methyl, 2methylpropoxy, 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.

7. The method of claim 1, wherein A is a substituted aryl or heteroaryl group selected from the group consisting of 5-methyl-2H-imidazol-4-yl, 2-aminothiazol-4-yl, 4-t-butylphenyl, 2-chlorophenyl, 2-chloro-6-methylpyrid-4-yl, 3-chlorophenyl, 4-chlorophenyl, 6chloropyridin-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-3yl, 2-pyrrolidin-3-ylphenyl, 4-(trifluoromethyl)phenyl, 6-(trifluoromethyl)pyridin-3-yl, 2,5dimethyloxazol-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.

8. The method 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.

9. The method 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-1yl)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-1,2,4triazol-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.

10. The method of claim 1, wherein A is N-methylaminocarbonyl.

11. The method 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-1H-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.2NHC(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--NHCH2CO.sub.2CH.sub.2CH.sub.3, --(CH.sub.2).sub.3--N(CH.sub.2CH.sub.2OH).sub.2, --(CH2).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.2OCH3, --(CH.sub.2).sub.2CH(NH.sub.2)CH.sub.2F, CH.sub.2CHFCH(NH.sub.2)CH.sub.2OH, and --(CH.sub.2).sub.2spirocyclopropyl-NH.sub.2.

12. The method of claim 1, wherein A.sup.2 is selected from the group consisting of phenyl, 6-aminopyridin-2-yl, 3-chlorophenyl, 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.

13. The method of claim 1, wherein R.sup.16 is hydrogen.

14. The method of claim 1, wherein A.sup.2 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, 4methylphenyl, 2-trifluoromethylphenyl, and 3-trifluoromethylphenyl.

15. The method 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.

16. The method of claim 15 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 --(CH.sub.2).sub.2spirocyclopropyl-NH.sub.2.

17. The method of claims 1 wherein the compound is 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-(I-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-2y1- ]-2-methylpropyl}benzamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-methoxyphenyl)-1H-imidazol-2yl- ]-2-methylpropyl}-4-methylbenzamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-methoxyphenyl)-1H-imidazol-2yl- ]-2-methylpropyl}-4-(trifluoromethyl)benzamide; N-(3-aminopropyl)-N-{(1R)-1-[1-benzyl-4-(3-methoxyphenyl)-1H-imidazol-2yl- ]-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)-2,2dimet- hylpropyl]-4-methylbenzamide; N-(3-aminopropyl)-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2dimet- hylpropyl]benzamide; N-(3-aminopropyl)-N-{(1R)-1-[1-(3,5-difluorobenzyl)-4-phenyl-1H-imidazol-- 2yl]-2-methylpropyl}-4-methylbenzamide; N-(3-aminopropyl)-N-{(1R)-1-[1-(3,5-difluorobenzyl)-4-phenyl-1H-imidazol-- 2yl]-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(dimet- hylamino)-2,2-dimethylpropyl]benzamide; N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2-methylpropyl]-N-[3(dimet- hylamino)-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-(3,5difluorobe- nzyl)-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-1,2dimeth- ylpropyl]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(c- yclobutylamino)propyl]benzamide; N-(3-aminopropyl)-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2dimet- hylpropyl]-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-- 2yl)-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- -2yl]-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)-2methylp- ropyl]-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(c- yclopropylamino)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-4y- lmethyl)-1H-imidazol-2-yl]propyl}benzamide; N-(3-aminopropyl)-2,4-difluoro-N-{(1R)-2-methyl-1-[4-phenyl-1-(1,3-thiazo- l-4ylmethyl) -1H-imidazol-2-yl]propyl}benzamide; N-(3-aminopropyl)-6-chloro-N-{(1R)-2-methyl-1-[4-phenyl-1-(1,3-thiazol-4y- lmethyl)-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-{(or)-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-{- [2hydroxy-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-- 2yl)-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--

2yl)-2,2-dimethylpropyl]-1,5-dimethyl-1H-pyrazole-3-carboxamide; methyl3-aminopropyl[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-dimet- hylpropyl]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-imida- zol-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; ethyl3-aminopropyl[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-dimeth- ylpropyl]carbamate; neopentyl3-aminopropyl[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-di- methylpropyl]carbamate; isobutyl3-aminopropyl[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-dim- ethylpropyl]carbamate; propyl3-aminopropyl[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-dimet- hylpropyl]carbamate; N-(3-aminopropyl)-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-dime- thylpropyl]-2-cyanoacetamide; butyl3-aminopropyl[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2-dimeth- ylpropyl]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) -2,2dimethylpropyl]amino}butanoic acid; N-[(2R)-3-amino-2-fluoropropyl]-N-[(1R)-1-(1-benzyl-4-phenyl-1-H-imidazol- -2yl)-2,2-dimethylpropyl]-2-hydroxyacetamide; N-(3-aminopropyl)-N-[(1R)-1-(1-benzyl-4-phenyl-1H-imidazol-2-yl)-2,2dimet- hylpropyl]-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-[1-(3-hydroxybenzyl)-4-phenyl-1H-im- idazol-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-hydroxyacetarnide; 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-benzy1-4-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-pheny1-1H-imidazol-- 2-yl)-2,2-dimethylpropyl]-2-methoxyacetamide; N-[(3R)-3-amino-4-hydroxybutyl]-N-[(1R)-1-(1-benzyl-4-pheny1-1H-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-b enzyl-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-imidazo-2-yl]-2,2-dimethyl-ptopyl}-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-mino-2-fluoro-propyl)-N-{(R)-1-[1-benzyl-4-(2-methoxy-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-(3-trifluoromethylph- enyl)-1-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-luoro-propyl)-N-{(R)-2,2-dimethyl-1-[4-phenyl-1-(5-trifl- uoromethyl -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)-2,2dimethyl-1-[1-(5-methyl-isoxazo- l-3-ylmethyl)-4-phenyl-1H-imidazol-2-yl]-propyl}-amide; (S)-Tetrahydro-furan-2-carboxylic acid((S)-3-amino-2-fluoro-propyl)-{(R)-2,2dimethyl-1-[4-phenyl-1-(5-trifl- uoromethyl-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-fluorop- henyl)-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-d- imethyl -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-fluoroph- enyl)-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-fluoroph- enyl)-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-yl- )-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-pheny- l)-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-fluorob- enzyl)-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-i- midazol-2-yl]-2-methyl-propyl}-2-methoxy-aceamide; N-(S)-3-Amino-4-fluoro-butyl)-N-{(R)-1-[4-(3-chloro-phenyl)-1-(3-fluorobe- nzyl)-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-fluoroph- enyl)-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-fluoroph- enyl)-1H-imidazol-2-yl]-2,2-dimethyl-propyl}-acetamide; (S)-Tetrahydio-furan-2-carboxylic acid (S)-3-amino-2-fluoro-propyl)-{(R)-1-[1(-fluoro-benzyl)-4-(3-fluoro-phenyl- )-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-fluoroph- enyl)-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-fluoroph- enyl)-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)-1H- -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)-1H- -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-acetami- de; N-(R)-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-acet- amide; N-(S)-3-Amino-4-fluoro-butyl)-N-{(R)-1-[4-(3-fluoro-phenyl)-1-(3-hy- droxybenzyl)-1H-imidazol-2-yl]-2,2-dimethyl-propyl}-2-methoxy-acetamide; N-(R)-3-Amino-4-fluoro-butyl)-N-{(R)-1-[4-(3-fluoro-phenyl)-1-(3-hydroxyb- enzyl)-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-(2,5difluoro-phenyl)-1H-imidazol-2-yl- ]-2,2-dimethyl-propyl}-amide; 3-[{(R)-1-[1-(3-Fluoro-benzyl)-4-(3-fluoro-phenyl)-1H-imidazol-2-yl]-2,2d- imethyl-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.

18. The method of claim 1, wherein X.sup.1 is--C(O)--; A.sup.2 is selected from the group consisting of phenyl, 6-aminopyridin-2-yl, 3-chlorophenyl, 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; A is 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, and 2H-tetrazol-2-ylmethyl; R.sup.8 is selected from the group consisting of alkyl, alkenyl, alkynyl, --CF.sub.3, alkoxy, halo, and hydroxyl; R.sup.4 is selected from the group consisting of hydrogen, --(CH.sub.2).sub.2--NH.sub.2--CH.sub.2-azetidin-3-yl, --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.3NHSO.sub.2CH.sub.3, --(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-1H-indazol-3-yl), --(CH.sub.2).sub.3NHCH2-(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.2C(O)NH.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.2(CO.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(CH3).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 --(CH.sub.2).sub.2spirocylcopropyl-NH.sub.2; 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 a pharmaceutically acceptable salt thereof.

19. The method of claim 18, wherein A.sup.2 is phenyl, 3-chlorophenyl, 2,4-difluorophenyl, 2,5-difluorophenyl, 3,5-difluorophenyl, 2-fluorophenyl, 3-fluorophenyl, 4-fluorophenyl, 3-hydroxyphenyl, 3-methoxyphenyl, 2-methylphenyl, 3-methylphenyl, or 4-methylphenyl; R.sup.8 is CF.sub.3 or halo; and m.sup.1 is 1 or 2.

20. The method of claim 19, wherein R.sup.16 and R.sup.17 are both H.

Details for Patent 8,318,791

Applicant Tradename Biologic Ingredient Dosage Form BLA Number Approval Date Patent No. Assignee Estimated Patent Expiration Status Orphan Source
Genentech RITUXAN rituximab SOLUTION;INTRAVENOUS 103705 001 1997-11-26   Start Trial Novartis Vaccines and Diagnostics, Inc. (Emeryville, CA) 2025-06-20 RX search
Genentech RITUXAN rituximab SOLUTION;INTRAVENOUS 103705 002 1997-11-26   Start Trial Novartis Vaccines and Diagnostics, Inc. (Emeryville, CA) 2025-06-20 RX search
Genentech HERCEPTIN trastuzumab VIAL; INTRAVENOUS 103792 001 1998-09-25   Start Trial Novartis Vaccines and Diagnostics, Inc. (Emeryville, CA) 2025-06-20 RX Orphan search
Genentech Inc RITUXAN HYCELA rituximab; hyaluronidase (human recombinant) SOLUTION;SUBCUTANEOUS 761064 001 2017-06-22   Start Trial Novartis Vaccines and Diagnostics, Inc. (Emeryville, CA) 2025-06-20 RX Orphan search
Genentech Inc RITUXAN HYCELA rituximab; hyaluronidase (human recombinant) SOLUTION;SUBCUTANEOUS 761064 002 2017-06-22   Start Trial Novartis Vaccines and Diagnostics, Inc. (Emeryville, CA) 2025-06-20 RX Orphan search
Genentech Inc HERCEPTIN HYLECTA trastuzumab; hyaluronidase-oysk INJECTABLE;SUBCUTANEOUS 761106 001 2019-02-28   Start Trial Novartis Vaccines and Diagnostics, Inc. (Emeryville, CA) 2025-06-20 RX search
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Number >Approval Date >Patent No. >Assignee >Estimated Patent Expiration >Status >Orphan >Source

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