Imidazole derivatives

 

Describes the imidazole derivatives of General formula I, II or III, representingwhere m = 0; n = 1; r, s and t = 0 or 1; p is 0, 1 or 2; V represents hydrogen; W and X are independently hydrogen or oxygen; Y is chr9or; Z represents chr9, CO, CO2, SO2, SO3, CONR12CN(CN), CN(CN)NR13or Z may be absent; R4represents H; R5represents H, halo, nitro, cyano or U-R23where U is an NR24, SO2, CO2, NR26NR27, NHSO2, CONH or NHCO, or U may be absent; R1, R2, R3independently represent hydrogen, lower alkyl, optionally substituted by hydroxy, phenyl, naphthyl or imidazole; C3-C6cycloalkyl; alkoxy; phenoxy; pyridyl; phenyl; naphthyl; imidazole; or any R1, R2and R3can be connected with the formation of cycloalkyl group; R6, R7, R8, R9, R12, R13, R26and R27independently represent hydrogen, optionally substituted lower alkyl, where specified by the Deputy is amino or phenyl group; or CN; R23is abouy halogen, amino or dimethylaminoethyl, pyridyl, tetrahydropyranyl, pyrimidinyl, thiophenyl or furanyl, R24represents hydrogen, R, S and T is selected from the group consisting of CH2, CO and CH(CH2)pQ, where Q represents NR36R37, OR38or CN, a R36, R37and R38independently represent hydrogen or lower alkyl; and a represents a nitrogen or carbon, and b, C and D represent carbon, provided that 1) W and X together can be oxygen only if Z is absent or represents chr9; 2) R23may be hydrogen except when U is a SO2; 3) R8may be hydrogen except when Z is a SO2or CO2;where X, V, W, R1, R2, R4, R5and R6represent hydrogen; a is a sulfur; b and C are CH; m, r, s, and t = 0; n = 1; Y represents CH2; Z represents SO2and R3represents a C1-4alkyl; R7represents a C1-4alkyl; R8represents phenyl, substituted with halogen;where a, b, C and D represent carbon; p>4and R5independently represent hydrogen, lower alkyl, halo or phenyl; R8represents naphthyl, cycloalkyl or alkyl substituted amino or dialkylamino; Z represents CO or CH2; R1and R2independently represent hydrogen or alkyl, substituted phenyl or alkylthio; their enantiomers, diastereoisomers and pharmaceutically acceptable salts, prodrugs and a solvate, which inhibit farnesyltransferase, which is the enzyme involved in the expression of the oncogene ras. 4 C.p. f-crystals.

Description text in facsimile form (see graphic part)/

Claims

1. Imidazole derivatives of General formula I, II or III, representing

where m is 0;

n means 1;

r, s and t denote 0 or 1;

p is 0, 1 or 2;

V represents hydrogen;

W and X are independently hydrogen or oxygen;

Y represents chr9or;

Z represents chr9, CO, CO2, SO2, SO3, CONR12CN(CN), CN(CN)NR13or Z may be absent;

R4represents N;

R5represents H, halo, nitro, tianli NHCO or U may be missing;

R1, R2, R3independently represent hydrogen, lower alkyl, optionally substituted by hydroxy, phenyl, naphthyl or imidazole; C3-C6cycloalkyl; alkoxy; phenoxy; pyridyl; phenyl; naphthyl; imidazole; or any R1, R2and R3can be connected with the formation of cycloalkyl groups;

R6, R7, R8, R9, R12, R13, R26and R27independently represent hydrogen, optionally substituted lower alkyl, where specified by the Deputy is amino or phenyl group; or CN;

R23represents hydrogen, lower alkyl, optionally substituted by hydroxy or phenoxy group, phenyl, optionally substituted with halogen, amino or dimethylaminoethyl, pyridyl, tetrahydropyranyl, pyrimidinyl, thiophenyl or furanyl radical;

R24represents hydrogen;

R, S and T is selected from the group consisting of CH2, CO and CH(CH2)pQ, where Q represents NR36R37, OR38or CN, a R36, R37and R38independently represent hydrogen or lower alkyl;

A represents a nitrogen or carbon;

B, C and D represent carbon, provided that

1. W and X together mogut> may be hydrogen except when U is a SO2;

3. R8may be hydrogen except when Z is a SO2or CO2;

where X, V, W, R1, R2, R4, R5and R6represent hydrogen;

And represents sulfur;

B and C are CH;

m, r, s and t denote 0;

n means 1;

Y represents CH2Z represents SO2and R3represents a C1-4alkyl;

R7represents a C1-4alkyl;

R8represents phenyl, substituted with halogen;

where a, b, C and D represent carbon;

Y represents CH2;

X, V, W, R3, R6and R7represent hydrogen;

r, s, t and m denote 0;

n means 1;

R4and R5independently represent hydrogen, lower alkyl, halo, or phenyl;

R8represents naphthyl, cycloalkyl or alkyl substituted amino or dialkylamino;

Z represents CO or CH2;

R1and R2independently represent hydrogen or alkyl, substituted phenyl or alkylthio;

their enantio raintrousers, which is the enzyme involved in the expression of oncogene rs.

2. Connection on p. 1, in which the compound is selected from the group consisting of

or

3. Connection on p. 2, in which a represents carbon.

4. Connection on p. 1, in which the compound is a compound of the formula

where a represents carbon.

5. Connection on p. 1, selected from the group consisting of the following compounds:

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine, hydrochloride;

8-Chloro-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine, hydrochloride;

1,2,3,4-Tetrahydro-4-[(3H-imidazol-4-yl)methyl]-1-(naphthalene-1-ylcarbonyl)cinoxacin, dihydrochloride;

2,3,4,5-Tetrahydro-4-(1H-imidazol-4-ylmethyl)-1-(1-1-naphthaleneboronic)-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-2-methyl-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine, hydrochloride;

2,3,4,5-Tetrahydro-4-(1-naphthalenesulfonyl)-1-[[1-(phenylmethyl)-1H-imidazol-5-yl]methyl]-1H-1,4-benzodiazepine, hydrochloride;

2,3,4,5-Tetrahydro-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine, ghidrah is in, hydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-N-methyl-N-phenyl-4H-1,4-benzodiazepine-4-carboxamide, hydrochloride;

2-[2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-1H-1,4-benzodiazepine-4-yl]sulfonyl]benzoic acid, methyl ester, hydrochloride;

7-Bromo-2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine, hydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-7-phenyl-1H-1,4-benzodiazepine, hydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-2-ylmethyl)-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-Tetrahydro-1-[3-(1H-imidazol-2-yl)propyl]-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine, dihydrochloride;

1-[3-Amino-3-(1H-imidazol-2-yl)propyl]-2,3,4,5-tetrahydro-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine, trihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-methyl-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine, hydrochloride;

(S)-2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-[2-(methylthio)ethyl]-4-(1-naphthaleneacetic)-1H-1,4-benzodiazepine, hydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-9-methyl-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-Tetrahydro-4-(1H-imidazol-4-ylmethyl)-9-methyl-1-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine, di the pin, trihydrochloride;

1-[[2-Aminomethyl)-1H-imidazol-4-yl]methyl]-2,3,4,5-tetrahydro-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine, trihydrochloride;

N-[2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine-8-yl]ndimethylacetamide, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-1H-pyrido[2,3-e]-1,4-diazepin, trihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-1H-oil[2,3-e]-1,4-diazepin, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-8-nitro-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-8-amino-1H-1,4-benzodiazepine, dihydrochloride;

N-[2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine-8-yl]benzamide, dihydrochloride;

N-[2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine-8-yl]cyclohexanone, dihydrochloride;

2,3,4,5-Tetrahydro-1-[2-(1H-imidazol-4-yl)ethyl]-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-Tetrahydro-1-[2-(1H-imidazol-4-yl)ethyl]-4-(1-naphthalenesulfonyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

7-Bromo-2,3,4,5-tetrahydro-1-[2-(1H-imidazol-4-yl)ethyl]-4-(1-naftalina vinylcarbenes)-7-phenyl-1H-1,4-benzodiazepine, trihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine-4-carboxylic acid, fenilmetilovy ether;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-4-[2-(triptoreline)benzoyl]-1H-1,4-benzodiazepine;

1,2,3,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-N-methyl-N,7-diphenyl-4H-1,4-benzodiazepine-4-carboxamide, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-7-(1-piperidinylcarbonyl)-1H-1,4-benzodiazepine, monohydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-7-pyridin-2-yl-1H-1,4-benzodiazepine, trihydrochloride;

7-(2-Furanyl)-2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-7-(2-thienyl)-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-7-(4-pyridinyl)-1H-1,4-benzodiazepine, trihydrochloride;

2,3,4,5-Tetrahydro-1-[3-(1H-imidazol-2-yl)propyl)-4-(1-naphthalenesulfonyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

7-Bromo-2,3,4,5-tetrahydro-4-(1H-imidazol-4-ylmethyl)-1-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine, dihydrochloride;

8-Chloro-2,3,4,5-tetrahydro-4-(1H-imidazol-4-ylmethyl)-1-(1-naphthalene who yl)-7-phenyl-1H-1,4-benzodiazepine, hydrochloride;

2,3,4,5-Tetrahydro-1,4-bis(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthaleneacetic)-7-phenyl-1H-1,4-benzodiazepine, triptorelin;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-methoxy-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine-7-carboxylic acid, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-5-ylmethyl)-4-(1-naphthalenesulfonyl)-7-cyclohexyl-1H-1,4-benzodiazepine, hydrochloride 2.5;

7-Butyl-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine, dihydrochloride;

1-[[2-(2-amino-ethyl)-1H-imidazol-4-yl]methyl]-2,3,4,5-tetrahydro-4-(1-naphthalenesulfonyl)-7-phenyl-1H-1,4-benzodiazepine, trihydrochloride;

1-[[2-(Aminomethyl)-1H-imidazol-4-yl]methyl]-2,3,4,5-tetrahydro-4-(1-naphthalenesulfonyl)-7-phenyl-1H-1,4-benzodiazepine, trihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-8-[N,N-bis-(phenylmethyl)amino]-1H-1,4-benzodiazepine, trihydrochloride;

N-[2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine-8-yl]phenylsulfonyl, dihydrochloride;

N-Phenyl-2,3,4,5-tetrahydro-1-(1H-IMO-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine-8-yl]-3-methylbenzamide, the dihydrochloride;

N-[2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine-8-yl]-4-methylbenzamide, dihydrochloride;

3-Chloro-N-[2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine-8-yl]benzamide, dihydrochloride;

7-Bromo-2,3,4,5-tetrahydro-1-[[2-[(dimethylamino)-methyl]-1H-imidazol-4-yl]methyl]-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine, dihydrochloride;

7-(4-Chlorophenyl)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine, dihydrochloride;

7-(3-AMINOPHENYL)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine, trihydrochloride;

1-Methyl-N-[2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine-8-yl]-1H-pyrrol-2-carboxamid, trihydrochloride;

N-[2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine-8-yl]-3-furancarboxylic, dihydrochloride;

7-(3-Chlorophenyl)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine, dihydrochloride;

2-Methyl-N-[2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine-8-yl]-benzamide, dihydrochloride;

N-Phenyl-N’-[2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthaleneboronic)-7-(3-pyridinyl)-1H-1,4-benzodiazepine, trihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-9-methoxy-4-(1-naphthalenesulfonyl)-1H-1,4-diazepin, dihydrochloride;

2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-7-phenyl-1H-pyrido[2,3-e]-1,4-diazepin, trihydrochloride;

(R)-2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-[2-(methylthio)ethyl]-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine, hydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, hydrochloride;

2,3,4,5-Tetrahydro-3-(2-hydroxyethyl)-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine, triptorelin;

2,3,4,5-Tetrahydro-4-(1H-imidazol-4-ylmethyl)-3-[2-(methylthio)ethyl]-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine, triptorelin;

(S)-2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, triptorelin;

4-Acetyl-7-bromo-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, hydrochloride;

2,3,4,5-Tetrahydro-4-(1H-imidazol-4-ylmethyl)-1-(1-naphthalenesulfonyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, hydrochloride 1.5;

7-Bromo-1,2,3,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4H-1,4-benzodiazepine-4-carboxamid, triptorelin;

7-Bromo-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ilma is-ylmethyl)-7-phenyl-3-(phenylmethyl)-1H-1,4-benzodiazepine, triptorelin;

4-Acetyl-7-bromo-3-[(4-chlorophenyl)methyl]-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-1H-1,4-benzodiazepine, dihydrochloride;

4-Acetyl-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-1H-oil[2,3-e]-1,4-diazepin, monohydrochloride;

N-Cyclohexyl-N’-[2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl) -4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine-8-yl]urea, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(methylsulphonyl)-3-(phenylmethyl)-1H-oil[2,3-e]-1,4-diazepin, monohydrochloride;

2,2-Dimethyl-N-[2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine-8-yl]-propanamide, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-7-phenyl-1H-1,4-benzodiazepine, monohydrochloride;

4-Acetyl-7-bromo-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(2-naphthaleneacetic)-1H-1,4-benzodiazepine, dihydrochloride;

4-Acetyl-7-bromo-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(1-naphthaleneacetic)-1H-1,4-benzodiazepine, dihydrochloride;

7-(2-Chlorophenyl)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, monohydrochloride;

1-Methyl-N-[2,3,4,5-tetrahydro-1-(1H-imidazol-4-elmet the ro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine-8-yl]-4-morpholinylcarbonyl, the dihydrochloride;

N-[2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine-8-yl]-3-methylbutanoic, dihydrochloride;

1,2,3,4-Tetrahydro-4-[(1H-imidazol-4-yl)methyl]-1-(naphthalene-1-ylsulphonyl)cinoxacin, dihydrochloride;

1,2,3,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-N,N,7-triphenyl-4H-1,4-benzodiazepine-4-carboxamide, dihydrochloride;

1,2,3,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4H-oil[2,3-e]-1,4-diazepin-4-carboxylic acid, methyl ester, monohydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-4-[(4-phenyl-1,2,3-thiadiazole-5-yl)carbonyl]-1H-1,4-benzodiazepine, triptorelin;

8-[[(Cyclohexylamino)carbonyl]amino]-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-1H-1,4-benzodi-azepine-4-carboxylic acid, 1,1-dimethylethylene ether;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-8-[[(4-were)sulfonyl]amino]-3-(phenylmethyl)-1H-1,4-benzodi-azepine-4-carboxylic acid, 1,1-dimethylethylene ether;

7-Bromo-1,2,3,4-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-5H-1,4-benzodiazepine-5-he, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-[1-oxo-3-(1-piperidinyl)propyl]-7-phenyl-1H-1,4-benzodiazepine, trihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-4-(4-chinainternational)-7-phenyl-1H-1,4-benzodiazepine, trihydrochloride;

(S)-4-[2-(Dimethylamino)-1-oxo-3-phenylpropyl]-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, trihydrochloride;

2,3,4,5-Tetrahydro-4-[4-hydroxy-3-(4-morpholinylmethyl)benzoyl]-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, trihydrochloride;

(S)-2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-[(1-methyl-2-pyrrolidinyl)carbonyl]-7-phenyl-1H-1,4-benzodiazepine, trihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-4-[[2-(propylthio)-3-pyridinyl]carbonyl]-1H-1,4-benzodiazepine, trihydrochloride;

4-((2-Chloro-6-methyl-4-pyridinyl)-carbonyl]-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, trihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-4-[[2-(phenylthio)-3-pyridinyl]carbonyl]-1H-1,4-benzodiazepine, trihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-[[2-(4-methylphenoxy)-3-pyridinyl]carbonyl]-7-phenyl-1H-1,4-benzodiazepine, trihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-[(2-methoxy-3-pyridinyl]carbonyl]-7-phenyl-1H-1,4-benzodiazepine, trihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-4-[(5-phenyl-4-oxazolyl) carbonyl]-1H-1,4-benzodiazepine, dihydrochloride;

4-Acetyl-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, Disain, the dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-[(2-methoxyethoxy)acetyl]-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-[4-(4-morpholinylmethyl)benzoyl]-7-phenyl-1H-1,4-benzodiazepine, trihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-[4-(methylsulphonyl)benzoyl]-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-[1-oxo-3-(phenylsulfonyl)propyl]-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-4-(3-pyridinylmethyl)-1H-1,4-benzodiazepine, trihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-4-(2-hinoklidilkarbinola)-1H-1,4-benzodiazepine, tetrahydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(4-izohinolinove)-7-phenyl-1H-1,4-benzodiazepine, trihydrochloride;

4-[(2-Chloro-3-pyridinyl)carbonyl]-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, trihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-4-(3-pyridylcarbonyl)-1H-1,4-benzodiazepine, trihydrochloride;

4-[(2,6-Dimethoxy-3-pyridinyl)carbonyl]-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, trihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-penisol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, the dihydrochloride;

4-[3-(Dimethylamino)benzoyl]-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, trihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-4-[(1-vinylcyclopropyl)carbonyl]-1H-1,4-benzodiazepine, dihydrochloride;

4-[(Bicyclo[4,2,0]OCTA-1,3,5-trien-7-yl)carbonyl]-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

4-Benzoyl-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

4-(2-Chlorobenzoyl)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

4-(2,3-Dichlorobenzoyl)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

N-[2-[[2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine-4-yl]carbonyl]phenyl]ndimethylacetamide, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(2-phenoxybenzoyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(2-methoxybenzoyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

4-(2,3-Dimethoxybenzoyl)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

4-(2,4-Dimethoxybenzoyl)-2,3,4,5-tetrahydro-1(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, digidroid;

4-(2,6-Dimethoxybenzoyl)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

4-(2,3-Dihydroxybenzyl)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

4-([1,1’-Biphenyl]-2-ylcarbonyl)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(2-methylbenzoyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

4-(2,3-Dimethylbenzoyl)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

4-(3-Cyanobenzoyl)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

4-(3-Chlorobenzoyl)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(3-phenoxybenzoyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(3-methoxybenzoyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

4-(3,4-Dimethoxybenzoyl)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

4-(3,5-Dimethoxybenzoyl)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-illiminator-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, the dihydrochloride;

4-[(2-Ethoxy-1-naphthalenyl)carbonyl]-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(2-naphthalenesulfonyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

4-(Pertenecer)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

4-(Diphenylacetyl)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-Tetrahydro-4-(2-hydroxy-1-oxo-2-phenylpropyl)-1H-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1H-indol-2-ylcarbonyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1H-indol-3-ylcarbonyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1H-indol-5-ylcarbonyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-[(1-methyl-1H-indol-2-yl)carbonyl]-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

4-(2-Benzofurazanyl)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-4-(3-pyridylcarbonyl)-1H-1,4-growing presence who zodiazepine, trihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-4-(2-chinainternational)-1H-1,4-benzodiazepine, trihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-4-(1-izohinolinove)-1H-1,4-benzodiazepine, trihydrochloride;

4-(3-Chloro-2-nitrobenzoyl)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(2-nitrobenzoyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(3-methoxy-2-nitrobenzoyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1H-indol-4-ylcarbonyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

4-[(2,6-Dihydroxy-3-naphthalenyl)carbonyl]-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

4-(1H-Benzimidazole-5-ylcarbonyl)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, trihydrochloride;

4-(1H-Benzotriazol-5-ylcarbonyl)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-[(4-methoxy-2-chinoline)carbonyl]-7-phenyl-1H-1,4-benzodiazepine, trihydrochloride;

N-[3-[[2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-Ben the CSR-2-fenoprofen)-7-phenyl-1H-1,4-benzodiazepine, the dihydrochloride;

4-[2-(Dimethylamino)benzoyl]-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, trihydrochloride;

4-(3-Ethoxybenzoyl)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-Tetrahydro-4-(2-hydroxy[1,1’-biphenyl]-3-ylcarbonyl)-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-Tetrahydro-4-[2-[(2-hydroxyethyl)thio]benzoyl]-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-[(2-methoxy-1-naphthalenyl)carbonyl]-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-Tetrahydro-4-[(2-hydroxy-4-chinoline)carbonyl]-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

2-[[2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine-4-yl]carbonyl]benzamide, dihydrochloride;

N-(1,1-Dimethylethyl)-2-[[2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine-4-yl]carbonyl]benzamide, dihydrochloride;

N-(4-Forfinal)-N’-[3-[[2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine-4-yl]carbonyl]phenyl]urea, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-[(3-methyl-4-oxo-2-phenyl-4H-benzopyran-8-yl)carbonyl]-7-phenyl-1H-1,4-benzodiazepine, digital chlorid;

4-(2-Cyanobenzoyl)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-[2-[[(4-were)sulfonyl]amino]benzoyl]-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-4-(6-chinainternational)-1H-1,4-benzodiazepine, trihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-4-(8-chinainternational)-1H-1,4-benzodiazepine, trihydrochloride;

4-(Benzo[b]thiophene-2-ylcarbonyl)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

4-[[4-(Dimethylamino)-1-naphthalenyl]carbonyl]-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, trihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-4-(1H-purine-6-ylcarbonyl)-1H-1,4-benzodiazepine, trihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(methoxyphenylacetyl)-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-[(5-methyl-1-phenyl-1H-pyrazole-4-ylcarbonyl]-7-phenyl-1H-1,4-benzodiazepine, trihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-[2-(2-were)-1-oxopropyl]-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-4-[(then it is carbonated who)-4-[2-(methylpentylamino)benzoyl]-7-phenyl-1H-1,4-benzodiazepine, trihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-4-(4-chinainternational)-1H-1,4-benzodiazepine, N-oxide, dihydrochloride;

N-Methyl-N-(2-pyridinylmethyl)-2-[[2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine-4-yl]carbonyl]benzamide, trihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(3-izohinolinove)-7-phenyl-1H-1,4-benzodiazepine, trihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-[(2-naphthalenethiol)acetyl]-1H-1,4-benzodiazepine, triptorelin (1:2);

4-[3-(3,4-Acid)-1-oxopropyl]-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-1H-1,4-benzodiazepine, triptorelin (1:2);

4-([1,1’-Biphenyl]-4-ylacetic)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-1H-1,4-benzodiazepine, triptorelin (1:2);

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(2-naphthaleneacetic)-1H-1,4-benzodiazepine, triptorelin (1:2);

4-([1,1’-Biphenyl]-2-ylcarbonyl)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-1H-1,4-benzodiazepine, triptorelin (1:2);

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-[(2-phenyl-4-chinoline)carbonyl]-1H-1,4-benzodiazepine, triptorelin (1:3);

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(3-pyridinylmethyl)-1H-1,4-benzodiazepine, triptorelin (1:3);

4-(N-Fluoren-9-ylacetic)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl) is l-4-ylmethyl)-1H-1,4-benzodiazepine, triptorelin (1:3);

(S)-2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-[(2-oxo-4-phenyl-3-oxazolidinyl)acetyl]-1H-1,4-benzodiazepine, triptorelin (1:2);

4-(9-Akademikerne)-2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-1H-1,4-benzodiazepine, triptorelin (1:3);

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(3-phenoxybenzoyl)-1H-1,4-benzodiazepine, triptorelin (1:2);

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-[[4’-(trifluoromethyl)[1,1’-biphenyl]-2-yl]carbonyl]-1H-1,4-benzodiazepine, triptorelin (1:2);

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(4-phenoxybenzoyl)-1H-1,4-benzodiazepine, triptorelin (1:2);

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(2-naphthalenesulfonyl)-1H-1,4-benzodiazepine, triptorelin (1:2);

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-oxo-4-phenylbutyl)-1H-1,4-benzodiazepine, triptorelin (1:2);

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-[(2-phenoxyphenyl)acetyl]-1H-1,4-benzodiazepine, triptorelin (1:2);

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-[2-[(4-were)sulfinil]benzoyl]-1H-1,4-benzodiazepine, triptorelin (1:2);

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-[2-[(phenylmethyl) amino]benzoyl]-1H-1,4-benzodiazepine, triptorelin (1:3);

1,2,3,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-N,N-diphenyl-4H-1,4-benzodiazepine-4-carboxamid, Lowy ether, hydrochloride;

4-Acetyl-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, hydrochloride;

(R)-7-Bromo-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(methylsulphonyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, hydrochloride;

(R)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(methylsulphonyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine-7-carbonitrile, monohydrochloride,

(R)-4-Acetyl-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-3-(phenylmethyl)-1H-1,4-benzodiazepine, monohydrochloride;

7-Bromo-4-[[2-(dimethylamino)ethyl]sulfonyl]-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4H-1,4-benzodiazepine, triptorelin (1:2);

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-4-[(1,2,3,4-tetrahydro-1-chinoline)carbonyl]-1H-1,4-benzodiazepine, monohydrochloride;

N-Ethyl-1,2,3,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-N,7-diphenyl-4H-1,4-benzodiazepine-4-carboxamid, monohydrochloride;

4-[(2,3-Dihydro-1H-indol-1-yl)carbonyl]-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, monohydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(methylsulphonyl)-3-(phenylmethyl)-7-(4-pyridinyl)-1H-1,4-benzodiazepine, trihydrochloride;

(R)-4-[[2-(Dimethylamino)ethyl]sulfonyl]-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-3-(phenylmethyl)-1H-1,4-benzodiazepine]karamanova acid, cyclohexyloxy ester, dihydrochloride;

(R)-7-Bromo-2,3,4,5-tetrahydro-1-(1-methyl-1H-imidazol-5-ylmethyl)-4-(methylsulphonyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, hydrochloride;

(R)-7-Cyano-2,3,4,5-Tetrahydro-1-[(1-methyl-1H-imidazol-5-yl)methyl]-4-(methylsulphonyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, monohydrochloride;

(R)-2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(methylsulphonyl)-7-phenyl-3-(phenylmethyl)-1H-pyrido[3,2-e]-1,4-diazepin, monohydrochloride;

4-[2-(4-Chlorophenyl)-1,2-dioxaoctyl]-2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, hydrochloride;

4-(1,2-Disopropyl)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, hydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-[2-(4-nitrophenyl)-1,2-dioxaoctyl]-7-phenyl-1H-1,4-benzodiazepine, hydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-[2-(4-methoxyphenyl)-1,2-dioxaoctyl]-7-phenyl-1H-1,4-benzodiazepine, hydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-4-(3,3,3-Cryptor-1,2-disopropyl)-1H-1,4-benzodiazepine, triptorelin (1:2);

(R)-7-Chloro-2,3,4,5-tetrahydro-1-[(1H-imidazol-4-yl)methyl]-4-(methylsulphonyl)-3-(phenylmethyl)-1H-pyrido[3,2-e]-1,4-diazepin, hydrochloride;

6,7,8,9-Tetrahydro-5-(1H-imidazol-4-ylmethyl)-8-(1-naphthalenesulfonyl)-2-phenyl-5H-pyrimido-[5,4-e][1,4]diazepin, zodiazepine, monohydrochloride;

(R)-7-Bromo-2,3,4,5-tetrahydro-1-(2-1H-imidazol-4-retil)-4(methylsulphonyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, monohydrochloride;

8-[(Cyclohexylcarbonyl)amino]-1,2,3,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4H-1,4-benzodiazepine-4-carboxylic acid, methyl ester, dihydrochloride;

N-[2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine-8-yl]-1-piperazinecarboxamide, dihydrochloride;

(R)-7-Cyano-1,2,3,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4H-1,4-benzodiazepine-4-carboxylic acid, ethyl ester, hydrochloride;

N-[2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(methylsulphonyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine-8-yl]cyclohexanecarboxylic, dihydrochloride;

(R)-7-Cyano-4-[[2-(dimethylamino)ethyl]sulfonyl]-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4H-1,4-benzodiazepine, dihydrochloride;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-[[2-(4-morpholinyl)ethyl]sulfonyl]-3-(phenylmethyl)-4H-1,4-benzodiazepine, dihydrochloride;

N-[2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(2-methoxy-3-methylbenzoyl)-1H-1,4-benzodiazepine-8-yl]cyclohexanecarboxylic, dihydrochloride;

8-[(Cyclohexylcarbonyl)amino]-2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-N-phenyl-1H-1,4-benzodiazepine-is diazepin-8-yl]cyclohexanone, the dihydrochloride;

N-[2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-[(2-methoxyphenyl)carbonyl]-1H-1,4-benzodiazepine-8-yl]cyclohexanone, dihydrochloride;

(R)-7-Cyano-1,2,3,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-phenylmethyl)-4H-1,4-benzodiazepine-4-sulfonic acid, ethyl ester, hydrochloride;

(3R)-7-Bromo-1-[cyano(1H-imidazol-4-yl)methyl]-2,3,4,5-tetrahydro-4-(methylsulphonyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, monohydrochloride;

3R-1-[2-Amino-1-(1H-imidazol-4-yl)ethyl]-2,3,4,5-tetrahydro-4-(methylsulphonyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, dihydrochloride;

(3R)-1-[2-(Dimethylamino)-1-(1H-imidazol-4-yl)ethyl]-2,3,4,5-tetrahydro-4-(methylsulphonyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, dihydrochloride;

(3R)-1-[2-Amino-1-(1H-imidazol-4-yl)ethyl]-7-bromo-2,3,4,5-tetrahydro-4-(methylsulphonyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, dihydrochloride;

(3R)-1-[2-(Dimethylamino)-1-(1H-imidazol-4-yl)ethyl]-7-bromo-2,3,4,5-tetrahydro-4-(methylsulphonyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, dihydrochloride;

7-Cyano-1,3,4,5-tetrahydro-1-(1-methyl-1H-imidazol-5-ylmethyl)-3-(phenylmethyl)-4-(phenylsulfonyl)-2H-1,4-benzodiazepine-2-it, monohydrochloride;

7-Cyano-1,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-(phenylsulfonyl)-2H-1,4-benzodiazepine-2-it, monohydrochloride;

7-Bromo-2,3,4,5-tetrahydro-1-(1H-them is Il]-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(methylsulphonyl)-1H-1,4-benzodiazepine, the dihydrochloride;

(R)-7-Bromo-3-(cyclohexylmethyl)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(methylsulphonyl)-1H-1,4-benzodiazepine, dihydrochloride;

7-Bromo-3-[(2-chlorophenyl)methyl]-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(methylsulphonyl)-1H-1,4-benzodiazepine, dihydrochloride;

(S)-7-Bromo-3-(cyclohexylmethyl)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(methylsulphonyl)-1H-1,4-benzodiazepine, dihydrochloride;

7-Bromo-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-[(4-methoxyphenyl)methyl]-4-(methylsulphonyl)-1H-1,4-benzodiazepine, dihydrochloride;

4-Acetyl-7-bromo-3-[(2-chlorophenyl)methyl]-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-1H-1,4-benzodiazepine, dihydrochloride;

4-Acetyl-7-bromo-3-[(3-chlorophenyl)methyl]-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-1H-1,4-benzodiazepine, dihydrochloride;

7-Bromo-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-[(4-hydroxyphenyl)methyl]-4-(methylsulphonyl)-1H-1,4-benzodiazepine, dihydrochloride;

(R)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(methylsulphonyl)-7-phenyl-3-(3-pyridinylmethyl)-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-Tetrahydro-8-(hydroxymethyl)-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-8-(phenoxymethyl)-1H-1,4-benzodi enzodiazepin-8-carboxamide, the dihydrochloride;

N-(Cyclohexylmethyl)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-1H-1,4-benzodiazepine-8-carboxamide, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-naphthalenesulfonyl)-N-(phenylmethyl)-1H-1,4-benzodiazepine-8-carboxamide, dihydrochloride;

(R)-4-Acetyl-7-[2-[(dimethylamino)methyl]phenyl]-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, dihydrochloride;

(R)-4-Acetyl-7-cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, monohydrochloride;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(1-oxobutyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, monohydrochloride;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(2-methyl-1-oxopropyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, monohydrochloride;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-(2-pyridinylmethyl)-1H-1,4-benzodiazepine, dihydrochloride;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-(2-thienylmethyl)-1H-1,4-benzodiazepine, monohydrochloride;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-[(1-methylethyl)sulfonyl]-3-(phenylmethyl)-1H-1,4-benzodiazepine, monohydrochloride;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl is methyl)-3-(phenylmethyl)-4-(propylsulfonyl)-1H-1,4-benzodiazepine, monohydrochloride;

(R)-7-Bromo-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-(phenylsulfonyl)-1H-1,4-benzodiazepine, monohydrochloride;

(R)-2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-3-(phenylmethyl)-4-(phenylsulfonyl)-1H-1,4-benzodiazepine, monohydrochloride;

(R)-2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-3-(phenylmethyl)-4-(propylsulfonyl)-1H-1,4-benzodiazepine, monohydrochloride;

(R)-7-Cyano-4-[(4-forfinal)sulfonyl]-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, monohydrochloride;

(R)-7-Cyano-4-[(3-cyanophenyl)sulfonyl]-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, monohydrochloride;

(R)-7-Cyano-2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-[(1-methyl-1H-imidazol-2-yl)sulfonyl]-3-(phenylmethyl)-1H-1,4-benzodiazepine, dihydrochloride;

(R)-4-[(3-Bromophenyl)sulfonyl]-7-cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, monohydrochloride;

(R)-N-[5-[[7-cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine-4-yl]sulfonyl]-4-methyl-2-thiazolyl]ndimethylacetamide, dihydrochloride;

4-Acetyl-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-7-(4-pyridinyl)-1H-1,4-benzodiazepine, trihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-or the l-4-ylmethyl)-7-(4-pyridinyl)-4-[2-(triptoreline)benzoyl]-1H-1,4-benzodiazepine, trihydrochloride;

(R)-2,3,4,5-Tetrahydro-1-[(1-methyl-1H-imidazol-5-yl)methyl]-4-(methylsulphonyl)-7-phenyl-3-(phenylmethyl)-1H-1,4-benzodiazepine;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4(phenylacetyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, monohydrochloride;

4-(2-Benzothiazolyl)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-1H-1,4-benzodiazepine, trihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-7-(3-pyridinyl)-4-(TRIFLUOROACETYL)-1H-1,4-benzodiazepine, trihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(methylsulphonyl)-3-(phenylmethyl)-7-(3-pyridinyl)-1H-1,4-benzodiazepine, trihydrochloride;

7-Bromo-3-[(1,1-dimethylmethoxy)methyl]-1,2,3,4-tetrahydro-1-(1H-imidazol-4-ylmethyl)-5H-1,4-benzodiazepine-5-he;

7-Bromo-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(methylsulphonyl)-3-(phenoxymethyl)-1H-1,4-benzodiazepine, dihydrochloride;

7-Bromo-2,3,4,5-tetrahydro-3-(hydroxymethyl)-1-(1H-imidazol-4-ylmethyl)-4-(methylsulphonyl)-1H-1,4-benzodiazepine, monohydrochloride;

7-Bromo-3-[(1,1-dimethylmethoxy)methyl]-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(methylsulphonyl)-1H-1,4-benzodiazepine

7-Bromo-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine-8-yl]karamanova acid, 2-methylpropyloxy ether, trihydrochloride;

[4-AC-methylpropyloxy ether;

N-[4-Acetyl-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine-8-yl]cyclohexanecarboxylic, dihydrochloride;

7-Bromo-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(methylsulphonyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine-8-yl]karamanova acid, 2-methylpropyloxy ether;

(R)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(phenylsulfonyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine-7-carbonitrile, monohydrochloride;

7-Bromo-1,2,3,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4H-1,4-benzodiazepine-4-ndimethylacetamide;

7-Bromo-4-[(dimethylamino)acetyl]-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine;

(R)-7-Bromo-4-(1,2-disopropyl)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, triptorelin;

(R)-7-Bromo-4-(cyclopropanecarbonyl)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, triptorelin;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-(propylsulfonyl)-1H-1,4-benzodiazepine, monohydrochloride;

7-Bromo-2,3,4,5-tetrahydro-1,4-bis(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, dihydrochloride;

7-Bromo-1,2,3,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-N,N-dimethyl-3-(phenylmethyl)-4H-1,4-benzodiazepine-4-sulfonamide, monohydrochloride;

2,3,4,5-chloride;

(R)-7-Cyano-1,2,3,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-N,N-dimethyl-3-(phenylmethyl)-4H-1,4-benzodiazepine-4-carboxamid, monohydrochloride;

N,N-Diethyl-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(methylsulphonyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine-7-carboxamide, monohydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-4-(1-phenyl-1H-tetrazol-5-yl)-1H-1,4-benzodiazepine, monohydrochloride;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-(2-pyrazinecarboxamide)-4H-1,4-benzodiazepine, monohydrochloride;

(R)-4-[7-Bromo-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4H-1,4-benzodiazepine-4-yl]-4-oxobutanoic acid, methyl ester, monohydrochloride;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(4-morpholinylcarbonyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, monohydrochloride;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-[[2-(1-pyrrolidinyl)ethyl]sulfonyl]-1H-1,4-benzodiazepine, dihydrochloride;

(S)-2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(methylsulphonyl)-7-phenyl-3-(3-pyridinylmethyl)-1H-1,4-benzodiazepine, dihydrochloride;

(R)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-3-(3-pyridinylmethyl)-4-(2-thienylmethyl)-1H-1,4-benzodiazepine, dihydrochloride;

(R)-2,3,4,5-Tetrahydro-1-(1H-imidazol-4-Almeida-1-(1H-imidazol-4-ylmethyl)-4-(methylsulphonyl)-3-(2-pyridinylmethyl)-1H-1,4-benzodiazepine, monohydrochloride;

2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(methylsulphonyl)-3-(phenylmethyl)-7-(2-pyrimidinyl)-1H-1,4-benzodiazepine, dihydrochloride;

(R)-7-Bromo-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-[(trifluoromethyl)sulfonyl]-1H-1,4-benzodiazepine, monohydrochloride;

(R)-2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-3-(phenylmethyl)-4-(TRIFLUOROACETYL)-1H-1,4-benzodiazepine, monohydrochloride;

(R)-2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-methylsulphonyl)-3-(phenylmethyl)-7-(4-pyridinyl)-1H-1,4-benzodiazepine, dihydrochloride;

(R)-2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-7-(4-pyridinyl)-4-(2-thienylmethyl)-1H-1,4-benzodiazepine, dihydrochloride;

(R)-2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-(phenylsulfonyl)-7-(4-pyridinyl)-1H-1,4-benzodiazepine, dihydrochloride;

(R)-2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-(propylsulfonyl)-7-(4-pyridinyl)-1H-1,4-benzodiazepine, dihydrochloride;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-[(3,5-dimethylisoxazol-4-yl)sulfonyl]-1H-1,4-benzodiazepine, dihydrochloride;

(R)-7-Cyano-4-[(4-cyanophenyl)sulfonyl)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, dihydrochloride;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidoyl)sulfonyl]-7-cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, the dihydrochloride;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-[(4-methoxyphenyl)sulfonyl]-3-(phenylmethyl)-1H-1,4-benzodiazepine, dihydrochloride;

N-[[7-Bromo-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(methylsulphonyl)-1H-1,4-benzodiazepine-3-yl]methyl]benzamide, dihydrochloride;

(R)-7-Cyano-1,2,3,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-N,N-dimethyl-3-(phenylmethyl)-4H-1,4-benzodiazepine-4-sulfonamide, hydrochloride;

(R)-7-Cyano-1,2,3,5-tetrahydro-N,N-dimethyl-1-[(1-methyl-1H-imidazol-5-yl)methyl]-3-(phenylmethyl)-4H-1,4-benzodiazepine-4-sulfonamide, hydrochloride;

(R)-7-Chloro-2,3,4,5-tetrahydro-1-[(1-methyl-1H-imidazol-5-yl)methyl]-4-(methylsulphonyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, monohydrochloride;

(R)-7-Chloro-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(methylsulphonyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, monohydrochloride;

(R)-7-Chloro-2,3,4,5-tetrahydro-1-[(1-methyl-1H-imidazol-5-yl)methyl]-4-(phenylsulfonyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, monohydrochloride;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(pyridine-3-ylmethyl)-4-(methylsulphonyl)-1H-1,4-benzodiazepine, tetrahydrochloride;

(R)-7-Bromo-2,3,4,5-tetrahydro-1-(1H-imidazol-2-ylmethyl)-4-(methylsulphonyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, dihydrochloride;

(R)-7-Bromo-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-[(1-methyl-1H-imidazol-5-ylmethyl)-4-[(2-morpholine-4-retil)sulfonyl]-3-(phenylmethyl)-1H-1,4-benzodiazepine, the dihydrochloride;

(R)-7-Chloro-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-[(2-morpholine-4-retil)sulfonyl]-3-(phenylmethyl)-1H-1,4-benzodiazepine, dihydrochloride;

(R)-7-Chloro-4-[(dimethylamino)sulfonyl]-1-[(1-methyl-1H-imidazol-5-yl)methyl]-3-(phenylmethyl)-1H-1,4-benzodiazepine, monohydrochloride;

(R)-7-Chloro-2,3,4,5-tetrahydro-1-(1-Mei-5-yl-methyl)-4-[(4-methylpiperidin-4-yl-ethyl)sulfonyl]-3-(phenylmethyl)-1H-1,4-benzodiazepine, dihydrochloride;

(R)-7-Bromo-2,3,4,5-tetrahydro-1-(1-Mei-5-ylmethyl)-4-[(4-methylpiperidin-4-retil)sulfonyl]-3-(phenylmethyl)-1H-1,4-benzodiazepine, dihydrochloride;

(R)-7-Cyano-1,2,3,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4H-1,4-benzodiazepine-4-carboxylic acid, isopropyl ester, hydrochloride;

(R)-7-Bromo-2,3,4,5-tetrahydro-4-[[2-(1H-imidazol-1-yl)ethyl]sulfonyl]-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, dihydrochloride;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(propylsulfonyl)-3-(3-pyridinylmethyl)-1H-1,4-benzodiazepine, hydrochloride;

7-Bromo-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine-5-he hydrochloride;

(R)-7-Bromo-2,3,4,5-tetrahydro-1-(1H-imidazol-1-ylacetic)-4-(methylsulphonyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, triptorelin;

1,2,4,5-Tetrahydro-1-(1H-imidazo is 2-(2-phenylethyl)-1H-1,4-benzodiazepine, monohydrochloride;

(R)-2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(methylsulphonyl)-7-phenyl-3-(4-pyridinylmethyl)-1H-1,4-benzodiazepine, dihydrochloride;

(R)-2,3,4,5-Tetrahydro-1-(1H-imidazol-2-ylmethyl)-4-(phenylsulfonyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine-7-carbonitrile, hydrochloride;

(R)-7-Cyano-1,2,3,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-N,N-dimethyl-3-(3-pyridinylmethyl)-4H-1,4-benzodiazepine-4-carboxamide, dihydrochloride;

(R)-7-Cyano-1,2,3,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-N,N-dimethyl-3-(3-pyridinylmethyl)-4H-1,4-benzodiazepine-4-sulfonamide, dihydrochloride;

4-[(4-Forfinal)sulfonyl]-2,3,4,5-tetrahydro-1-[(1-methyl-1H-imidazol-5-yl)-3-(phenylmethyl)-1H-thieno[2,3-e]-1,4-diazepin, monohydrochloride;

(R)-2,3,4,5-Tetrahydro-1-(1-(4-cyanovinylene)imidazol-5-ylmethyl)-4-(methylsulphonyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine-7-carbonitrile, hydrochloride;

(R)-2,3,4,5-Tetrahydro-1-(1-(4-cyanovinylene)imidazole-4-ylmethyl)-4-(methylsulphonyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine-7-carbonitrile, hydrochloride;

(R)-4-Benzoyl-7-cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, monohydrochloride;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-[(1-methyl-1H-imidazol-5-yl)methyl]-3-(pyridine-3-ylmethyl)-4-(methylsulphonyl)-1H-1,4-benzodiazepine, dihydrochloride;

(R)-7-Cyano-2,3,4,5-tetrad;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-[(1H-imidazol-4-yl)methyl]-3-(pyridine-3-ylmethyl)-4-(phenylsulfonyl)-1H-1,4-benzodiazepine, dihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(methylsulphonyl)-7-phenyl-3-(phenylmethyl)-1H-1,4-benzodiazepine;

1,2,3,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-N-(1-naphthalenyl)-7-phenyl-4H-1,4-benzodiazepine-4-carboxamid, monohydrochloride;

(S)-7-Bromo-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(methylsulphonyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, hydrochloride;

N-[2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(2,3-dimethylbenzoyl)-1H-1,4-benzodiazepine-8-yl]cyclohexanecarboxylic, dihydrochloride;

(R)-7-Cyano-N-[2-(dimethylamino)ethyl]-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-N-methyl-3-(phenylmethyl)-1H-1,4-benzodiazepine-4-carboxamid, triptorelin (1:2);

7-Bromo-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(methylsulphonyl)-2-oxo-3-(phenylmethyl)-1H-1,4-benzodiazepine, triptorelin;

(R)-7-Cyano-4-(2-fornicator)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, triptorelin (1:1);

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-[(4-nitrophenyl)sulfonyl]-3-(phenylmethyl)-1H-1,4-benzodiazepine, triptorelin;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-[[4-(4-methyl-1-piperazinil)phenyl]sulfonyl]-3 is ylamino)phenyl]sulfonyl]-3-(phenylmethyl)-1H-1,4-benzodiazepine, triptorelin;

(R)-7-Bromo-4-[[2-(dimethylamino)ethyl]sulfonyl]-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4H-1,4-benzodiazepine, dihydrochloride;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-(3-pyridylsulfonyl)-1H-1,4-benzodiazepine, trihydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(methylsulphonyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, dihydrochloride;

(R)-7-Bromo-2,3,4,5-tetrahydro-1-[(1-methyl-1H-imidazol-4-ylmethyl]-4-(methylsulphonyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, dihydrochloride;

(R)-4-[[3-(Dimethylamino)propyl]sulfonyl]-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-3-(phenylmethyl)-1H-1,4-benzodiazepine, dihydrochloride;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, trihydrochloride;

4-Butyl-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, trihydrochloride;

(R)-7-Bromo-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-[[2-(4-morpholinyl)ethyl]sulfonyl]-3-(phenylmethyl)-1H-1,4-benzodiazepine, dihydrochloride;

(R)-7-Bromo-2,3,4,5-tetrahydro-1-[(1-methyl-1H-imidazol-5-yl)methyl]-4-[[2-(4-morpholinyl)ethyl]sulfonyl]-3-(phenylmethyl)-1H-1,4-benzodiazepine, dihydrochloride;

(R)-7-Cyano-1-(1H-imidazol-4-ylmethyl)-4-(4-morpholinylcarbonyl)-3-(phenylmethyl)-1H-1,4-b is ethyl)-1H-1,4-benzodiazepine, monohydrochloride;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-[(4-AMINOPHENYL)sulfonyl]-3-(phenylmethyl)-1H-1,4-benzodiazepine, hydrochloride;

2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-[(4-pyridylthio)acetyl]-7-phenyl-1H-1,4-benzodiazepine, dihydrochloride;

N-(4-Chlorophenyl)-N’-cyano-1,2,3,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-4H-1,4-benzodiazepine-4-imitated, monohydrochloride;

4-Acetyl-7-bromo-1,2,4,5,1’,3’-hexahydro-1-(1H-imidazol-4-ylmethyl)Spiro[3H-1,4-benzodiazepine-3,2’-[2H]inden], dihydrochloride;

7-Bromo-4-[3-(dimethylamino)-1-oxopropyl]-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, triptorelin (1:1);

(R)-2,3,4,5-Tetrahydro-1-(1-methyl-1H-imidazol-5-ylmethyl)-4-(phenylsulfonyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine-7-carbonitrile, monohydrochloride;

2,3,4,5-Tetrahydro-1-[(1-methyl-1H-imidazol-5-ylmethyl]-4(methylsulphonyl)-7-phenyl-3-(pyridine-3-ylmethyl)-1H-1,4-benzodiazepine, cleaners containing hydrochloride salt (1:1,5), trifurcata (1:0,75);

4-[4-(Forfinal)sulfonyl]-2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-2-(2-phenylethyl)-1H-1,4-benzodiazepine, monohydrochloride;

7-Bromo-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(methylsulphonyl)-2-(2-phenylethyl)-1H-1,4-benzodiazepine, monohydrochloride;

(R)-7-Cyano-2,3,4,5-Tetrahydro-1-(1-methyl-1H-imidazol-5-and is ahydro-1-(1H-imidazol-4-ylmethyl)-4-(methylsulphonyl)-3-(4-brompheniramine)-1H-1,4-benzodiazepine, hydrochloride;

(R)-7-Bromo-2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(methylsulphonyl)-3-(thiazol-4-ylmethyl)-1H-1,4-benzodiazepine, hydrochloride;

(R)-7-Bromo-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(propylsulfonyl)-3-(thiazol-4-ylmethyl)-1H-1,4-benzodiazepine, hydrochloride;

(R)-7-Bromo-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(propylsulfonyl)-3-(4-brompheniramine)-1H-1,4-benzodiazepine, hydrochloride;

(R)-7-Bromo-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(pyridine-3-ylmethyl)-4-(methylsulphonyl)-1H-1,4-benzodiazepine, trihydrochloride;

(R)-7-Bromo-2,3,4,5-tetrahydro-1-(1H-1-Mei-5-ylmethyl)-3-(pyridine-3-ylmethyl)-4-(methylsulphonyl)-1H-1,4-benzodiazepine, dihydrochloride;

1,2,3,4-Tetrahydro-7-bromo-4-[(1H-imidazol-4-ylmethyl]-2-phenylmethyl-1-(phenylmethylsulfonyl)cinoxacin, hydrochloride;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(phenylsulfonyl)-3-(4-cyanovinylene)-1H-1,4-benzodiazepine, hydrochloride;

(R)-7-Cyano-4-[(N-methyl-N-phenylmethyl)aminosulfonyl]-1-[(1H-imidazol-4-ylmethyl]-3-(phenylmethyl)-1H-1,4-benzodiazepine, monohydrochloride;

(R)-7-Cyano-4-[N-(tetrahydroisoquinolines)sulfonyl]-1-[(1H-imidazol-4-ylmethyl]-3-(phenylmethyl)-1H-1,4-benzodiazepine, monohydrochloride;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-4-(phenylsulfonyl)-3-(2-thienylmethyl)-1H-1,5-benzodiazepine-2-carboxylic acid, triptorelin (1:2);

(R)-7-Cyano-4-[(N-piperidinyl)sulfonyl]-1-[(1H-imidazol-4-ylmethyl]-3-(phenylmethyl)-1H-1,4-benzodiazepine, monohydrochloride;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-1-Mei-5-ylmethyl)-3-(phenylmethyl)-4-(2-thienylmethyl)-1H-1,4-benzodiazepine, hydrochloride;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(pyridine-3-ylmethyl)-4-[[2-(dimethylamino)ethyl]sulfonyl]-1H-1,4-benzodiazepine, trihydrochloride;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-1-Mei-5-ylmethyl)-3-(phenylmethyl)-4-(propylsulfonyl)-1H-1,4-benzodiazepine, hydrochloride;

N-(Cyano)-N’-methyl-1,2,3,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-7-phenyl-4H-1,4-benzodiazepine-4-imitated, hydrochloride;

(R)-7-Cyano-4-[(2-nitrophenyl)sulfonyl]-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, hydrochloride;

(R)-7-Cyano-4-[(4-methyl-phenyl)sulfonyl]-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, hydrochloride;

(R)-7-Cyano-4-(butylsulfonyl)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, hydrochloride;

(R)-7-Cyano-4-[(2-Cryptor-were)sulfonyl]-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, hydrochloride;

(R)-7-Cyano-4-[(2-trifloromethyl)sulfonyl]-2,3,4,5-tetrahydro-1-(1H-radioactive]-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, hydrochloride;

(R)-7-Cyano-4-[(2-methylsulfinylphenyl)sulfonyl]-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-1H-1,4-benzodiazepine, hydrochloride;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-(((4-methylsulphonyl)-phenyl)-sulfonyl)-1H-1,4-benzodiazepine;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-(((4-(trifluoromethyl)-phenyl)-sulfonyl)-1H-1,4-benzodiazepine;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-((3-methoxypropyl)-sulfonyl)-1H-1,4-benzodiazepine;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-((3,4-acid)-sulfonyl)-1H-1,4-benzodiazepine;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-((4-forfinal)methyl)-4-(phenylsulfonyl)-1H-1,4-benzodiazepine;

(R)-7-Cyano-4-[(N-cyclopropylmethyl-N-propyl)-aminosulfonyl]-1-[(1H-imidazol-4-yl)methyl]-3-(phenylmethyl)-1H-1,4-benzodiazepine;

(R)-7-Cyano-4-[(N,N-(dibutylamino))-sulfonyl]-1-[(1H-imidazol-4-yl)methyl]-3-(phenylmethyl)-1H-1,4-benzodiazepine;

(R)-7-Chloro-4-(methanesulfonyl)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-1H-pyrido[3,4-e]-1,4-diazepin;

1,2,3,4-Tetrahydro-7-bromo-4-[(1H-imidazol-4-yl)methyl]-2-phenylmethyl-1-(methylsulphonyl)cinoxacin;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ilmtal-4-ylmethyl)-3-((2-thienyl)methyl)-4-(propylsulfonyl)-1H-1,4-benzodiazepine;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-((2-thienyl)methyl)-4-((2-thienyl)-sulfonyl)-1H-1,4-benzodiazepine;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-((3-metaltipped)-sulfonyl)-1H-1,4-benzodiazepine;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-(((3-Metallica)-propyl)-sulfonyl)-1H-1,4-benzodiazepine;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-(((3-methylsulphonyl)-propyl)-sulfonyl)-1H-1,4-benzodiazepine;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-((2-methylpropyl)-sulfonyl)-1H-1,4-benzodiazepine;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-(cyclopentylmethyl)-1H-1,4-benzodiazepine;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-((4,4,4-trifloromethyl)-sulfonyl)-1H-1,4-benzodiazepine;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-((phenylmethyl)-sulfonyl)-1H-1,4-benzodiazepine;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-[[2-(5-(N-benzoyl)aminomethyl)thienyl]-sulfonyl]-1H-1,4-benzodiazepine;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-[[2-(1-(3-chloro-5-methyl-pyridine-2-yl))-pyrrolyl]-sulfonyl]-1H-1,4-benzodiazepine;

(R)-7-Cyano-IANA-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-[((3-methyl-1,2,4-oxadiazol-5-yl)-phenyl)-sulfonyl]-1H-1,4-benzodiazepine;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-((2,5-acid)-sulfonyl)-1H-1,4-benzodiazepine;

(R)-7-Cyano-4-[(N-tetrahydropyranyl)-sulfonyl]-1-[(1H-imidazol-4-yl)methyl]-3-(phenylmethyl)-1H-1,4-benzodiazepine;

(R)-7-Cyano-4-[(N,N-bis-[1-(2-methylpropyl)amino]-sulfonyl]-1-[(1H-imidazol-4-yl)methyl]-3-(phenylmethyl)-1H-1,4-benzodiazepine;

(R)-7-Cyano-4-[(N-methyl-N-phenyl)aminosulfonyl]-1-[(1H-imidazol-4-yl)methyl]-3-(phenylmethyl)-1H-1,4-benzodiazepine;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(2-(2,6-dimetilfenil) ethyl)-4-(methylsulphonyl)-1H-1,4-benzodiazepine;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1-(N-phthalimidomethyl)-imidazole-5-ylmethyl)-3-(phenylmethyl)-4-(methylsulphonyl)-1H-1,4-benzodiazepine;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-[(2-(N,N-dimethylamino)-ethyl)-imidazol-5-ylmethyl]-3-(phenylmethyl)-4-(methylsulphonyl)-1H-1,4-benzodiazepine;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-[(2-amino-ethyl)-imidazol-5-ylmethyl]-3-(phenylmethyl)-4-(methylsulphonyl)-1H-1,4-benzodiazepine;

(R)-7-Bromo-4-(methanesulfonyl)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-1H-thieno[2,3-e]-1,4-diazepin;

(R)-7-Bromo-4-(methanesulfonyl)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-1H-thieno[3,2-e]-1,4-diazepin;

(R)-4-(methanesulfonyl)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(penile and)phenyl)methyl)-4-(phenylsulfonyl)-1H-1,4-benzodiazepine;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-((4-(2-dimethylamino)-ethoxy)-phenyl)methyl)-4-(phenylsulfonyl)-1H-1,4-benzodiazepine;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylsulphonyl)-3-(phenylmethyl)-4-(methylsulphonyl)-1H-1,4-benzodiazepine;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylsulphonyl)-3-(phenylmethyl)-4-(propylsulfonyl)-1H-1,4-benzodiazepine;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylsulphonyl)-3-(phenylmethyl)-4-(phenylsulfonyl)-1H-1,4-benzodiazepine;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylsulphonyl)-3-(phenylmethyl)-4-(2-thienylmethyl)-1H-1,4-benzodiazepine;

7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(R)-[(R)-1-phenylethyl]-4-(methylsulphonyl)-1H-1,4-benzodiazepine;

7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(R)-[(R)-1-phenylethyl]-4-(propylsulfonyl)-1H-1,4-benzodiazepine;

7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(R)-[(R)-1-phenylethyl]-4-(phenylsulfonyl)-1H-1,4-benzodiazepine;

7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(R)-[(R)-1-phenylethyl]-4-((2-thienyl)-sulfonyl)-1H-1,4-benzodiazepine;

7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(S)-[(R)-1-phenylethyl]-4-(methylsulphonyl)-1H-1,4-benzodiazepine;

7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(S)-[(R)-1-phenylethyl]-4-(propylsulfonyl)-1H-1,4-benzodiazepine;< 7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(S)-[(R)-1-phenylethyl]-4-((2-thienyl)-sulfonyl)-1H-1,4-benzodiazepine;

7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(R)-[(S)-1-phenylethyl]-4-(methylsulphonyl)-1H-1,4-benzodiazepine;

7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(R)-[(S)-1-phenylethyl]-4-(propylsulfonyl)-1H-1,4-benzodiazepine;

7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(R)-[(S)-1-phenylethyl]-4-(phenylsulfonyl)-1H-1,4-benzodiazepine;

7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(R)-[(S)-1-phenylethyl]-4-((2-thienyl)-sulfonyl)-1H-1,4-benzodiazepine;

7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(S)-[(S)-1-phenylethyl]-4-(methylsulphonyl)-1H-1,4-benzodiazepine;

7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(S)-[(S)-1-phenylethyl]-4-(propylsulfonyl)-1H-1,4-benzodiazepine;

7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(S)-[(S)-1-phenylethyl]-4-(phenylsulfonyl)-1H-1,4-benzodiazepine;

7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(S)-[(S)-1-phenylethyl]-4-((2-thienyl)-sulfonyl)-1H-1,4-benzodiazepine;

7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(R)-[(R)-vinylcyclopropyl]-4-(methylsulphonyl)-1H-1,4-benzodiazepine;

7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(R)-[(R)-vinylcyclopropyl]-4-(propylsulfonyl)-1H-1,4-benzodiazepine;

7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(R)-[(R)-vinylcyclopropyl]-4-(phenylsulfonyl)-1H-1,4-benzodiazepine;

7-t

7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(R)-[(S)-vinylcyclopropyl]-4-(methylsulphonyl)-1H-1,4-benzodiazepine;

7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(R)-[(S)-vinylcyclopropyl]-4-(propylsulfonyl)-1H-1,4-benzodiazepine;

7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(R)-[(S)-vinylcyclopropyl]-4-(phenylsulfonyl)-1H-1,4-benzodiazepine;

7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-

(R)-[(S)-vinylcyclopropyl]-4-((2-thienyl)-sulfonyl)-1H-1,4-benzodiazepine;

7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(S)-[(R)-vinylcyclopropyl]-4-(methylsulphonyl)-1H-1,4-benzodiazepine;

7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(S)-[(R)-vinylcyclopropyl]-4-(propylsulfonyl)-1H-1,4-benzodiazepine;

7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(S)-[(R)-vinylcyclopropyl]-4-(phenylsulfonyl)-1H-1,4-benzodiazepine;

7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(S)-[(R)-vinylcyclopropyl]-4-((2-thienyl)-sulfonyl)-1H-1,4-benzodiazepine;

7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(S)-[(S)-vinylcyclopropyl]-4-(methylsulphonyl)-1H-1,4-benzodiazepine;

7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(S)-[(S)-vinylcyclopropyl)-4-(propylsulfonyl)-1H-1,4-benzodiazepine;

7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(S)-[(S)-fenilcetonuria]-4-((2-thienyl)-sulfonyl)-1H-1,4-benzodiazepine;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-[(2-(5-(pyridine-2-yl)-thienyl)-sulfonyl])-1H-1,4-benzodiazepine;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-[(2-(5-(1,2-isoxazol-3-yl)-thienyl)-sulfonyl])-1H-1,4-benzodiazepine;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(3-(1H-imidazol-2-yl)-propyl)-3-(phenylmethyl)-4-(phenylsulfonyl)-1H-1,4-benzodiazepine;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(3-(1H-imidazol-2-yl)-propyl)-3-(phenylmethyl)-4-(methylsulphonyl)-1H-1,4-benzodiazepine;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(3-(1H-imidazol-2-yl)-propyl)-3-(phenylmethyl)-4-(propylsulfonyl)-1H-1,4-benzodiazepine;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(3-(1H-imidazol-2-yl)-propyl)-3-(phenylmethyl)-4-((2-thienyl)-sulfonyl)-1H-1,4-benzodiazepine;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(2-(1H-imidazol-2-yl)-ethylsulfanyl)-3-(phenylmethyl)-4-(phenylsulfonyl)-1H-1,4-benzodiazepine;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(2-(1H-imidazol-2-yl)-ethylsulfanyl)-3-(phenylmethyl)-4-(methylsulphonyl)-1H-1,4-benzodiazepine;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(2-(1H-imidazol-2-yl)-ethylsulfanyl)-3-(phenylmethyl)-4-(propylsulfonyl)-1H-1,4-benzodiazepin;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(2-(1H-imidazol-2-yl)ethylsulfonyl)-3-(phenylmethyl)-4-((2-thienyl)-sulfonyl)-1H-1,4-benzodiazepine;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-illiter)-4-(methanesulfonamido)-1H-1,4-benzodiazepine;

(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-(phenylcarbonylamino)-1H-1,4-benzodiazepine.

Priority points and attributes:

26.02.1996 - all signs on p. 1 except Z means CO2;

25.07.1996 - on the basis of Z means CO2.

 

Same patents:

The invention relates to novel condensed to thienopyrimidine formula I and their physiologically acceptable salts, having the effect of inhibitors of phosphodiesterase V(PDE V), and which can be used for the treatment of diseases of the cardiovascular system and for the treatment and/or therapy of disorders of potency

The invention relates to compounds of formula (1), where X and Y Is N or O; R1substituted alkyl, substituted arylalkyl or cycloalkyl; R2and R3Is h or alkyl; And a Is-C(O)-, -OC(O)-, -S(O)2-; R4- alkyl, cycloalkyl or (C5-C12)aryl; compounds of the formula (2), where X and Y are O, S or N; R1- alkyl, optionally substituted arylalkyl; R2and R3Is h or alkyl;- C(O)-; R6- Deputy, including the condensed heterocyclic rings; and compounds of the formula (3), where X and Y are O, S or N; R1- alkyl, alkylsilane, (C5-C12)arylalkyl, (C5-C12)aryl; R2and R3Is h or alkyl; R2' and R3' - N; R11, R12and E together form a mono - or bicyclic ring which may contain heteroatoms

The invention relates to new thienopyrimidine formula I, their pharmaceutically acceptable salts, having the effect of inhibitors of phosphodiesterase V, which can be used to combat diseases of the cardiovascular system and for the treatment and/or therapy of disorders, to pharmaceutical compositions in a form suitable for the treatment

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The invention relates to novel ortho-sulfonamidophenylhydrazine heteroaryl hydroxamic acids of the formula

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where W and X are both carbon, T is nitrogen, U represents CR1where R1represents hydrogen, or alkyl containing 1-8 carbon atoms, R represents-N(CH2R5)-SO2Z, Q represents -(C=O)-NHOH, with

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is a benzene ring, or is a heteroaryl ring of 5 to 6 atoms in the cycle, which may contain 0-2 heteroatoms selected from nitrogen, oxygen and sulfur, in addition to the heteroatom of nitrogen, denoted as W, where benzene or heteroaryl ring may optionally contain one or two substituent R1where permissible; Z is phenyl, which is optionally substituted by phenyl, alkyl with 1-8 carbon atoms, or a group OR2; R1represents halogen, alkyl with 1-8 carbon atoms, alkenyl with 2-6 carbon atoms, perfluoroalkyl from 1 to 4 carbon atoms, phenyl, optionally substituted by 1-2 groups OR2group-NO2group -(CH2)nZ, where Z is a phenyl which allows an alkyl with 1-8 carbon atoms, phenyl, optionally substituted with halogen, or heteroaryl radical containing 5 to 6 atoms in the cycle, including 1-2 heteroatoms selected from nitrogen, oxygen and sulfur; R5represents hydrogen, alkyl with 1-8 carbon atoms, phenyl, or heteroaryl containing 5 to 6 atoms in the cycle, including 1-2 heteroatoms selected from nitrogen, oxygen and sulfur; or their pharmaceutically acceptable salts

The invention relates to new thienopyrimidine General formula I or their physiologically acceptable salts, having the properties of an inhibitor of phosphodiesterase V, which can be used in the pharmaceutical industry for the treatment of diseases of the cardiovascular system, in particular heart failure, and for treatment of violations of a potentiality

The invention relates to sulfonamidnuyu to the compound of formula I, where R1- alkyl, alkenyl, quinil; a represents optionally substituted heterocyclic group, excluding benzimidazolyl, indolyl, 4,7-dehydrobenzperidol and 2,3-dihydrobenzofuranyl; X - alkylene, oxa, oxa(lower) alkylene; R2- optional substituted aryl, substituted biphenyl, its salts and pharmaceutical compositions comprising this compound

The invention relates to new thienopyrimidine, as well as their physiologically acceptable salts with inhibitory activity against phosphodiesterase V (PDE V), which can be used to combat diseases of the cardiovascular system and for the treatment and/or therapy of disorders of potency

The invention relates to thiophene derivative of the formula I, in which Ra and Rb may be the same or different and mean hydrogen, alkyl, acyl, alkenyl, phenyl, or Ra and Rb together may form a benzene ring or cyclohexanone ring, its pharmaceutically acceptable salts and hydrates

The invention relates to the class of heterocyclic metallocenes and containing catalytic systems, as well as the method of polymerization joining the polymerized monomers using a given catalytic system, and these heterocyclic metallocene correspond to the formula (I), YjRiZjjMeQkP1,

where Y represents a coordinating group containing the Central radical with six-electrons, directly coordinating IU, which condensed one or more rings containing at least one atom that is not carbon atom and is selected from S; R" represents a divalent bridging communication between the groups Y and Z; Z is a coordinating group having the same meaning as Y; Me represents a transition metal of group 3, 4, 5, 6; Q is halogen or linear or branched C1-C6-alkyl; R represents a counterion; i=0 or 1; j=1-3; jj=0-2; k=1-3 and 1= 0-2

The invention relates to new tricyclic pyrazole derivative or its pharmaceutically acceptable salt

The invention relates to new compounds of General formulas I, II, III

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or their pharmaceutically acceptable salts, in which the dotted lines indicate optional double bonds; A is-CR7or N; - - NR1R2, -CR1R2R11, -C(= CR2R12R1, -NHCHR1R2, -ОСHR1R2, -SCHR1R2, -CHR2OR12,

-CHR2SR12, -C(S)R2or-C(O)R2N-ethyl-2,2,2-triptorelin; G is oxygen, sulfur, NH, NH3hydrogen, methoxy, ethoxy, triptoreline, methyl, ethyl, dimethoxy, NH2, NHCH3N(CH3)2or trifluoromethyl; Y Is N; Z is NH, O, S, -N(C1-C2alkyl) or-C(R13R14), where R13and R14independently of one another represent hydrogen, trifluoromethyl or methyl, or one of the elements of R13and R14is cyano and the other is hydrogen or stands; R1- C1-C6alkyl which may be optionally substituted by one or two substituents R8independently from each other selected from the group comprising hydroxy, fluorine, chlorine, bromine, iodine, CF3C1-C4alkoxy, -O-CO-(C1-C4alkyl), where (C1-C2- C1-C12alkyl, aryl or -(C1-C4alkylene)aryl, where aryl is phenyl, naphthyl; R3is methyl, ethyl, fluorine, chlorine, bromine, iodine, cyano, methoxy, OCF3, methylthio, methylsulphonyl, CH2HE or CH2OCH3; R4is hydrogen, C1-C4alkyl, fluorine, chlorine, bromine, iodine, C1-C4alkoxy, triptoreline, -CH2OCH3, -CH2OCH2CH3, -CH2CH2OCH3, -CF3, amino, nitro, -NH(C1-C4alkyl), -N(CH3)2, -NHCOCH3, -NHCONHCH3, hydroxy, -CO(C1-C4alkyl), -Cho, COOH, cyano, or-COO(C1-C4alkyl), where C1-C4the alkyl may be substituted by one Deputy chosen from the group comprising hydroxy, amino, -NHCOCH3, -NH(C1-C2alkyl), -N(C1-C2alkyl)2, fluorine, chlorine, cyano, nitro; R5is phenyl, naphthyl, pyridyl, pyrimidyl, where each of the above groups R5substituted with one to three substituents that are independently from each other selected from fluorine, chlorine, C1-C6the alkyl or C1-C6alkoxyl, or one Deputy chosen from the group comprising hydroxy, iodine, bromine, formyl, cyano, nitro, trifluoromethyl, amino, -(C1-C6these groups of R5may be optionally substituted with one hydroxy-group; R6is hydrogen or C1-C6alkyl; R7is hydrogen, methyl; R11is hydrogen, hydroxy, fluorine or methoxy; R12is hydrogen or C1-C4alkyl, and R16and R17independently of one another represent hydrogen, hydroxy, methyl, ethyl, methoxy or ethoxy, except that both R16and R17cannot both be methoxy or ethoxy; or R16and R17together form oxo (=O) group; provided that if G is an atom of oxygen, sulfur, NH or NCH3he is joined by a double bond to a five-membered ring of the formula III, and further provided that R6is absent when the nitrogen atom to which it is linked, is attached by a double bond to an adjacent carbon atom in the ring

The invention relates to 4-hydroxy-3-chinainternational and hydrazides of General formula (I), where a represents a-CH2- or-NH-, a R1, R2, R3and R4such as defined in the claims

The invention relates to new derivatives pyrazolopyrimidinones General formula (1) or their pharmaceutically acceptable salts that may be used in the treatment of impotence, and method of production thereof

The invention relates to new derivatives of 1,5-dihydropyrazolo[3,4-d] pyrimidinone General formula (I) having the properties of an inhibitor of phosphodiesterase, which can be used, for example, high blood pressure, angina and heart disease

The invention relates to the field of organic chemistry, namely to new bicyclic derivative

The invention relates to new derivatives of benzothiadiazole, benzoxazoles and benzodiazines formula I in free base form or in the form of a pharmaceutically acceptable acid salt additive that can be used as an anxiolytic drug in the treatment of any condition, which is associated with increased endogenous levels of CRF or in which violated the regulation of the hPa system (hypothalamic - pituitary), or various diseases that are caused by CRF1or the manifestation of which contributes CRF1such as arthritis, asthma, allergies, anxiety, depression, etc

The invention relates to a new one with selective affinity to T6receptors, pyrazolo[1,5-a]pyrimidines and pyrazolo[1,5-a]triazines General formula I, where X denotes a =C(R4)- or =N-, R1denotes phenyl, optionally substituted by one or more radicals of lower alkyl, halogen, lower alkoxygroup, tolyl, pyridyl, naphthyl or thiophenyl, R2denotes hydrogen, (ness.)alkyl, (ness.)thioalkyl or hydroxy(ness.) alkoxygroup, R3denotes amino(ness.)alkylamino, di(ness.)alkylamino, piperazinil, optionally substituted by one or more radicals, lower alkyl, benzyl, phenyl or hydroxy(NISS

The invention relates to new derivatives of 1,3-diaryl-2-pyridin-2-yl-3-(pyridine-2-ylamino)propanol of the formula (I)

where Z denotes-NH-(C1-C16-alkyl)-(C=O)-; -(C=O)-(C1-C16-alkyl)-(C=O)-;

-(C=O)-phenyl-(C=O)-; AND1AND2AND3AND4denote independently of each amino-acid residue, E represents-SO2-R4and-CO-R4; R1- phenyl, thiazolyl, oxazolyl, thienyl, thiophenyl and others, R2- N., HE, CH2HE, OMe; R3Is h, F, methyl, OMe; R4denotes -(C5-C16-alkyl), -(C0-C16-alkylen)-R5, -(C=O)-(C0-C16-alkylen)-R5, -(C=O)-(C0-C16-alkylene)-NH-R5and others, R5denotes-COO-R6, -(C=O)-R6-(C1-C6-alkylen)-R7, phenyl, naphthyl and others, R6denotes H, -(C1-C6) alkyl; R7denotes H, -(C1-C7-cycloalkyl, phenyl, naphthyl and others, l, q, m, n, o, p denote 0 or 1, and l+q+m+n+o+p is greater than or equal to 1, and their pharmaceutically acceptable salts
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