Chiral cis-imidazolines

IPC classes for russian patent Chiral cis-imidazolines (RU 2487127):

C07D417/14 - containing three or more hetero rings

C07D409/14 - containing three or more hetero rings

C07D405/14 - containing three or more hetero rings

C07D403/14 - containing three or more hetero rings

C07D403/04 - directly linked by a ring-member-to-ring- member bond

C07D401/14 - containing three or more hetero rings

C07D401/04 - directly linked by a ring-member-to-ring- member bond

A61P35 - Antineoplastic agents

A61K31/454 -

Another patents in same IPC classes:

Novel amide derivative and use thereof as medicinal agent / 2487124

Invention relates to an amide derivative of formula (I), where A is benzene or pyridine, where the benzene or pyridine optionally contain 1 or 2 or 3 identical or different substitutes selected from an alkyl containing 1-6 carbon atoms, a cycloalkyl containing 3-6 carbon atoms, an alkoxy containing 1-6 carbon atoms, a halogen atom, nitro, cyano, alkylsulphonyl containing1-6 carbon atoms, amino, cyclic amine selected from 1,1-di-oxoisothiazolidinyl, 2-oxooxazolidinyl, oxopyrrolidinyl, 1,1-dioxothiazinyl and 2-oxoimidazolidinyl optionally having a substitute selected from an alkyl containing 1-6 carbon atoms and an alkylcarbonyl containing a total of 2-7 carbon atoms, acylamino containing a total of 2-7 carbon atoms, and an alkylsulphonyl amino containing 1-6 carbon atoms, wherein the right-side bond is linked to the carbonyl and the left-side bond is linked to the nitrogen atom, R¹ and R² are identical or different and each is a hydrogen, an alkyl containing 1-6 carbon atoms and optionally containing 3 halogen atoms as substitutes, a cycloalkyl containing 3-6 carbon atoms, a phenyl, a halogen atom or a cyano group and R¹ and R² are not a hydrogen atom at the same time, R³ is a hydrogen atom, an alkyl containing 1-6 carbon atoms, an alkenyl containing 2-6 carbon atoms, a cycloalkyl containing 3-6 carbon atoms, or a halogen, R^4a, R^4b and R^4c are each independently a hydrogen atom, an alkyl containing 1-6 carbon atoms, or an oxo, R^5a, R^5b and R^5c are identical or different and each is a hydrogen atom, an alkyl containing 1-6 carbon atoms and optionally containing substitute(s) selected from phenyl, an alkoxy group containing 1-6 carbon atoms, optionally substituted with an alkoxy group containing 1-6 carbon atoms, a phyenylcarbonyloxy group and a hydroxy group, or a phenyl, X is a carbon atom (any of R^4a, R^4b and R^4c can be bonded to a carbon atom, but the carbon atom is not substituted with oxo) or a nitrogen atom (if Y is a single bond, the nitrogen atom can be oxidised to form an N oxide), Y is a single bond, a carbonyl or an oxygen atom, Z¹ and Z² are each independently a carbon atom (substitute R³ is optionally bonded to a carbon atom) or a nitrogen atom, and m equals 1 or 2, a pharmacologically acceptable salt thereof. The amide derivative is used as a preventive/therapeutic drug for treating autoimmune diseases, inflammatory bowel diseases or osteoarthritis.

Dipeptide prodrugs and use thereof / 2486183

Application describes prodrugs being 2-amino-6-({[2-(4-chlorophenyl)-1,3-thiazol-4-yl]methyl}thio)-4-[4-(2-hydroxyethoxy)-phenyl]pyridine-3,5-dicarbonitryl derivatives, and a method for preparing them.

Method of producing substituted pyrimidin-5-yl carboxylic acids / 2485083

Invention relates to a method of producing substituted pyrimidin-5-yl carboxylic acids of formula I and can be used in organic chemistry. The method is realised by reacting N-substituted guanidines and hetarylamidines with ethoxymethylene derivatives of 1,3-ketoesters according to a scheme given below (where the substitutes are as defined in the claim).

Isoxazolo-pyridine derivatives / 2484091

Invention relates to isoxazole-pyridine derivatives of formula , where X; R¹; R², R³, R⁴, R⁵ and R⁶ are as described in claim 1 of the invention and a pharmaceutically acceptable salt thereof. The invention also relates to a medicinal agent for treating diseases associated with the binding site of the GABA A α5 receptor based on compounds of formula I and use of said compounds in preparing a medicinal agent.

Phosphatidylinositol-3-kinase inhibitors / 2481346

Invention refers to compounds of formula I , wherein R² means methyl, Y means carbon or nitrogen, and R¹, R³ and R⁴ have the value specified in the patent claim. Also, the invention refers to a pharmaceutical composition for the use as a pharmaceutical drug having activity of a phosphatidylinositol-3-kinase inhibitor, to the use of the compounds of formula I for preparing the pharmaceutical drug for treating a disease mediated by phosphatidylinositol 3-kinase and to a method for preparing the compounds of formula I .

Nitrogen-containing aromatic heterocyclic compound / 2481330

Invention refers to compounds of general formula (I), wherein A represents a pyrrole group or a pyrazole group, and X represents a carbon atom or a nitrogen atom; R¹ represents a carboxy group; R² independently represents a group specified in a substitute group α; R³ independently represents phenyl(C₁-C₆alkyl)group substituted by, phenyl(C₁-C₆alkyl)group (wherein the substitute(s) represents (represent) 1-4 groups independently specified in the substitute group α); m is equal to 0, 1, 2 or 3, n is equal to 0 or 1; each of R⁴, R⁵, R⁶ and R⁷ independently represents a hydrogen atom, C₁-C₆alkyl group or a halogen atom; B represents a substituted naphthyl group (wherein the substitute(s) represents (represent) 1-4 groups independently specified in the substitute group α), or the group represented by formula (II), wherein B¹, B² and α are those as specified in the patent claim. Also, the invention refers to a pharmaceutical composition possessing lipolysis inhibiting activity, to the use of the compounds of formula (I) in preparing a drug preparation for treating hyperlipidemia, dislipidemia, abnormal lipid metabolism, arteriosclerosis or type II diabetes mellitus and to a method of treating or preventing the mentioned diseases.

Phenylpropionic acid derivative and use thereof / 2479579

Invention relates to novel compounds of general formula (1) and pharmaceutically acceptable salts thereof, which exhibit inhibitory activity on phospholipase A₂ enzyme and therefore have prostaglandin and/or leucotriene production suppressing action. In formula X is a halogen atom, cyano group, C₁-C₃ alkyl group, which can be substituted with halogen atoms, C₁-C₃ alkoxy group or hydroxy group, C₂-C₄ alkenyl group, C₁-C₃ alkoxy group or hydroxy group; Y is a hydrogen atom or C₁-C₃ alkyl group; Z is C₁-C₃ alkyl group; G is selected from formulae and , where in formulae (G²) and (G⁵) R⁴ is a hydrogen atom or C₁-C₆ alkyl group which can be substituted with halogen atoms; D is -NR¹⁰C(O)-, -C(O)NR¹⁰-, -S(O)₂NR¹⁰- or -N(R¹¹)-; R¹⁰ is a hydrogen atom; R¹¹ is a hydrogen atom or C₁-C₃ alkyl group; A is a single bond, C₁-C₆ alkylene, which can be substituted with a phenyl group, or C₂-C₄ alkenylene; Q is a phenyl group or a 5-6-member aromatic heterocyclic group containing 1-3 heteroatoms selected from N, O, S, optionally substituted with a benzene ring; R⁵, R⁶ and R⁷ all or independently denote a hydrogen atom, a halogen atom, C₁-C₆ alkyl group which can be substituted with halogen atoms, C₁-C₆ alkoxy group which can be substituted with halogen atoms, phenyloxy group, phenyl group or a 5-6-member aromatic heterocyclic group containing 1-3 heteroatoms selected from N, O, where said phenyl group and 5-6-member aromatic heterocyclic group can be substituted with a C₁-C₃ alkyl group which can be substituted with halogen atoms or a C₁-C₃ alkoxy group. The invention also relates to specific compounds, a medicinal agent, a pharmaceutical composition, a phospholipase A₂ enzyme activity inhibitor and a treatment method.

Heteroaryl pyrrolidinyl and piperidinyl ketone derivatives / 2479575

Invention relates to a compound of formula I or use thereof to prepare a medicine for treating depression, anxiety or both: or pharmaceutically acceptable salts thereof, where m is 0-3; n is 0-2; Ar is: optionally substituted indolyl; optionally substituted indazolyl; azaindolyl; 2,3-dihydro-indolyl; 1,3-dihydro-indol-2-one-yl; optionally substituted benzothiophenyl; benzothiazolyl; benzisothiazolyl; optionally substituted quinolinyl; 1,2,3,4-tetrahydroquinolinyl; quinolin-2-one-yl; optionally substituted naphthalenyl; optionally substituted pyridinyl; optionally substituted thiophenyl or optionally substituted phenyl; R¹ is: C_1-6alkyl; hetero-C_1-6alkyl; halo-C_1-6alkyl; halo-C_2-6alkenyl; C_3-7cycloalkyl; C_3-7cycloalkyl-C_1-6alkyl; C_1-6alkyl-C_3-6cycloalkyl-C_1-6alkyl; C_1-6alkoxy; C_1-6alkylsulphonyl; phenyl; tetrahydropyranyl-C_1-6alkyl; phenyl-C_1-3alkyl, where the phenyl part is optionally substituted; heteroaryl-C_1-3alkyl; R² is: hydrogen or C_1-6alkyl; and each R^a and R^b is independently: hydrogen; C_1-6alkyl; C_1-6alkoxy; halo; hydroxy or oxo; or R^a and R^b together form C_1-2alkylene; under the condition that, when m is 1, n is 2, and Ar is an optionally substituted phenyl, then R¹ is not methyl or ethyl, and where optionally substituted denotes 1-3 substitutes selected from alkyl, cycloalkyl, alkoxy, halo, haloalkyl, haloalkoxy, cyano, amino, acylamino, monoalkylamino, dialkylamino, hydroxyalkyl, alkoxyalkyl, pyrazolyl, -(CH₂)_q-S(O)_rR^f; -(CH₂)_q-C(=O)-NR^gR^h; -(CH₂)_q-N(R^f)-C(=O)-Rⁱ or -(CH₂)_q-C(=O)-Rⁱ; where q is 0, r is 0 or 2, each R^f, R^g and R^h is independently hydrogen or alkyl, and each Rⁱ is independently alkyl, and where "heteroaryl" denotes a monocyclic radical having 5-6 ring atoms, including 1-2 ring heteroatoms selected from N or S, wherein the rest of the ring atoms are C atoms, "heteroalkyl" denotes an alkyl radical, including a branched C₄-C₇-alkyl, where one hydrogen atom is substituted by substitutes selected from a group consisting of -OR^a, -NR^bH, based on the assumption that the bonding of heteroalkyl radical occurs through a carbon atom, where R^a is hydrogen or C_1-6alkyl, R^b is C_1-6alkyl. Pharmaceutical compositions based on said compound are also disclosed.

2-aza-bicyclo[3,3,0]octane derivatives / 2478099

Invention relates to a 2-aza-bicyclo[3.3.0]octane derivative of formula , with stereogenic centres in a (1S,3S,5S)-configuration, where A is a thiazolyl which is unsubstituted or monosubstituted, where the substitute is independently selected from a group comprising C_1-4alkyl, C_3-6cycloalkyl and NH₂; B is phenyl which is unsubstituted or mono- or disubstituted, where the substitutes are independently selected from a group comprising C_1-4alkyl, trifluoromethyl, NHC(O)CH₃ and halogen; and R¹ is an imidazo[2,1·b]thiazolyl or benzoisoxazolyl group, where said groups are independently unsubstituted or monosubstituted, where the substitutes are independently selected from a group comprising C_1-4alkyl; or R¹ is a 2,3-dihydrobenzofuranyl group; or a pharmaceutically acceptable salt. The 2-aza-bicyclo[3.3.0]octane derivative of formula (I) is as a medicinal agent having the activity of orexin receptor antagonists.

Substituted n-phenylbipyrrolidine carboxamides and therapeutic use thereof / 2477719

Invention relates to substituted N-phenylbipyrrolidine carboxamides of formula , where values of R, R₁, R₂, R₃ and R₄ are given in claim 1.

Drug preparation possessing antiaggrregant activity / 2486182

Invention refers to a biologically active substance possessing the antiaggregant properties. The technical effect: what is produced is a drug preparation of a new compound of (2E)-3-[1-(2-hydroxy-3-piperidin-1-ylpropyl)-1 H-indol-3-yl]-1-(2-thienyl)prop-2-en-1-one hydrochloride of formula I possessing antiaggregant action:

Pyrimidyl cyclopentanes as akt/protein kinase inhibitors / 2486181

Invention refers to new compounds of formula I, enantiomers and pharmaceutically acceptable salts thereof having the properties of AKT/protein kinase inhibitors. In formula 1 G represents phenyl, naphthalene, 5-member heteroaryl with 1 sulphur atom in a ring or 9-member bicyclic heteroaryl specified in indolyl wherein phenyl, naphthalene, 5-member heteroaryl is optionally substituted by one of three R^a groups; R¹ and R^1a are independently specified in H, Me, Et, -CH₂OH, CF₃, CHF₂ or CH₂F; R² represents H, -OH, -OMe or F; R^2a representsH, Me or F; R³ represents H, Me, Et; R⁴ represents H, 6-member heterocyclyl containing an oxygen atom as a heteroatom, cyclopropyl methyl or C₁-C₄ alkyl is optionally substituted F,-OH or -O(C₁-C₃ alkyl); R⁵ and R^5a are independently specified in H and C₁-C₄ alkyl, or R⁵ and R^5a together with an atom whereto attached form a carbonyl group or 5-6-member cycloalkyl; each R^a independently represents halogen, C₁-C₆-alkyl, C₃-C₆-cycloalkyl,-O-(C₁-C₆-alkyl), CF₃, CN, phenyl, pyrazole, CH₂F, CHF₂, -OCH₂F, -OCHF₂, -OH, -SO₂(C₁-C₆-alkyl), C(O)NH₂; and j represents 1 or 2; and provided j represents 2, j-ring carbon atom, opposite NR⁴, may be substituted by heteroatom O.

Pyrimidyl cyclopentanes as akt-protein kinase inhibitors / 2486178

Present invention refers to new compounds of formula I, enantiomers and pharmaceutically acceptable salts thereof which have selective inhibitory action on AKT protein kinase, in particular protein kinase B. In formula I: A represents R¹ and R^1a are independently specified in H, Me, Et. vinyl, CF₃, CHF₂ or CH₂F:R₂ represents H, OH, OMe or F; R^2a represents H, Me or F; R³ represents H. Me. Et or CF₃; G represents phenyl optionally substituted by one to four groups R^c, or 5-6-member heteroaryl containing one heteroatom specified in sulphur optionally substituted by halogen; R⁵ and R⁶ independently represent H, OCH₃, C₃-C₆-cycloalkyl independently substituted by F, OH, C₁-C₃alkyl or O(C₁-C₃alkyl), 4-6-member heterocyclyl containing one heteroatom specified in nitrogen optionally substituted by F, OH, C₁-C₃alkyl, cyclopropylmethyl or -C(=O)(C₁-C₃alkyl), or C₁-C₆-alkyl optionally substituted by one or more groups independently specified in OH, oxo O(C₁-C₆-alkyl), CN, F, NH₂. NH(C₁-C₆-alkyl), O(C₁-C₆-alkyl)₂. cyclopropyl. phenyl, imidazolyl, piperidinyl, pyrrolidinyl, morpholinyl, tetrahydrofuranyl, oxetanil or tetrahydropyranyl. The other radical values are specified in the patent claim.

Carboxamide compounds and use thereof as calpain inhibitors / 2485114

Present invention refers to new carboxamide compounds of formula I-A' or I-A" , as well as to tautomers thereof and pharmaceutically acceptable salts thereof, wherein R¹ means hydrogen, C₁-C₁₀-alkyl, C₃-C₇-cycloalkyl-C₁-C₄alkyl, aryl-C₁-C₆-alkyl or hetaryl-C₁-C₄-alkyl, wherein aryl and hetaryl in the two last mentioned radicals may be substituted or have 1 radical R^1c; wherein R^1a represents C₁-C₆-alkoxy, R^1c is independently specified in halogen, CN, CF₃, O-CF₃, O-CHF₂, C₁-C₆-alkyl, C₁-C₆-alkoxy, hetaryl, O-CH₂-aryl, - (CH₂)_p-NR^c6R^c7 with p = 0 or 1; wherein R^c6 represents C₁-C₆-alkyl or SO₂-C₁-C₆-alkyl, and R^c7 represents C₁-C₆-alkyl, or the two radicals R^c6 and R^c7 together with an N atom form 5- or 6-member, optionally substituted C₁-C₄-alkyl nitrogen-containing heterocyclyl which can optionally have 1 heteroatom from the group O and N as ring members, R² means C₁-C₁₀-alkyl, C₃-C₇-cycloalkyl, aryl, hetaryl, wherein aryl and hetaryl in the two last mentioned radicals may be unsubstituted or carry 1, 2 or 3 identical or different R^2c radicals; wherein R^2c have one of the values specified for R^1c; R^3a and R^3b together with a carbon atom whereto attached, are C=O; X means hydrogen or a radical of formulas C(=O)-O-R^x1 or C(=O)-NR^x2R^x3, wherein R^x1 means C₁-C₆-alkyl, R^x2 means H or C₁-C₆-alkyl, and R^x2 means H, one of the variables Y¹, Y², Y³ and Y⁴ forms a nitrogen atom, and the rest variables Y¹, Y², Y³ and Y⁴ mean CH, n is equal to 0 or 1, R^y is independently specified in halogen, CN, aryl, -NH-SO₂-R^y4, -(CH₂)_p-NR^y6R^y7 with p = 0; wherein R^y4 means C₁-C₆-alkyl, R^y6 has one of the values specified for R^c6, and R^y7 has one of the values specified for R^c7; m means 0 or 1 for formulas I-A', and R^w is specified in halogen, C₁-C₆-alkyl, C₁-C₆-alkoxy, wherein C₁-C₆-alkyl can have 1 substitute R^wa, aryl, -(CH₂)_p-NR^w6R^w7 with p = 0 or 1, R^wa has one of the values specified for R^1a, or represents NR^a2SO₂R^a4, R^a2 represents H, R^a4 represents C₁-C₆-alkyl, R^w6 has one of the values specified for R^c6, R^w7 has one of the values specified for R^c7, m is equal to 0, 1 or 2 for formula I-A", and R^w6* has one of the values specified for R^w, E has one of the values specified for: -CHR_E ²-CHR_E ³-, -CH₂-O-, -O-CH₂-, -S-CH₂-, -CH₂-S-, -CH₂-SO₂-, -SO₂-CH₂-, wherein R_e ², R_e ³ represent hydrogen; wherein aryls defined above, represent mono- or bicyclic aromatic hydrocarbon radicals such as phenyl or naphthyl, and hetaryls defined above, represent 5 - or 6-member aromatic heterocyclic radicals containing 1 or 2 heteroatoms specified in nitrogen, oxygen and sulphur and can additionally contain a condensed benzene ring. Also, the invention refers to specific compounds, pharmaceutical compositions containing them and use thereof.

3,8-diaminotetrahydroquinoline derivative / 2482117

Present invention refers to organic chemistry, namely new 3,8-diaminotetrahydroquinoline derivatives of formula (1a) or to their pharmaceutically acceptable salts wherein X represents CH₂, C=O or CH-OR; m is 1 or 2; Ar represents a phenyl group or a 5-merous or 6-merous aromatic heterocyclic group having one element specified in S and N, (wherein the phenyl group may be substituted by 1-2 halogen atoms); each R¹ and R² represents a hydrogen atom; R³ represents a C1-C6 alkyl group or indolyl-C_1-4 alkyl group (the indolyl group is optionally substituted by a C1-C6 alkyl group or a halogen atom), n is 0; R⁴ and R⁵ which may be identical or different, each represents a hydrogen atom or a C1-C6 linear or branched alkyl group; each R⁶ and R⁷ represents a hydrogen atom; and R represents a hydrogen atom. Also, the present invention refers to a drug preparation and a pharmaceutical composition of the basis of the compound of formula (1a), to the compound of formula (F1), to a method for preparing an intermediate compound (e).

Cyclopenta(d)pyrimidines as protein kinase akt inhibitors / 2481336

Invention refers to compounds of formula I , as well as to enantiomers and salts thereof, wherein R¹ and R^1a are independently specified in H, Me, Et, CH=CH₂, CH₂OH, CF₃, CHF₂ or CH₂F; R² and R^2a are independently specified in H or F; R⁵ represents H, Me, Et or CF₃; A is presented by formula: ; wherein G, R⁶, R⁷, R^a, R^b ,R^c, R^d, R⁸, m, n and p are presented in cl. 1 of the patent claim.

Hydroxylated and methoxylated cyclopenta[b]pyrimidines as protein kinase inhibitors / 2478632

Present invention refers to new compounds of general formula (I), (the radical values are presented in the patent claim) including their split enantiomers, split diastereomers, solvates and pharmaceutically acceptable salts. What is also described is a method for preparing new compounds, a pharmaceutical composition containing them.

Substituted n-phenylbipyrrolidine carboxamides and therapeutic use thereof / 2477719

Invention relates to substituted N-phenylbipyrrolidine carboxamides of formula , where values of R, R₁, R₂, R₃ and R₄ are given in claim 1.

Quinoxalinyl macrocyclic hepatitis c virus serine protease inhibitors / 2475494

Present invention relates to compounds of formula I

Polycyclic indazole-derivatives and their application as erk inhibitors for cancer treatment / 2475484

Invention relates to particular compounds, which demonstrate inhibiting activity with respect to ERK, whose structure formula is given in description, to their pharmaceutically acceptable salts, based on them pharmaceutical composition and their application for treatment of cancer, mediated by ERK activity.

Pyrimidine derivatives as alk-5 inhibitors / 2485115

Invention relates to novel pyrimidine derivatives of formula (I) in free form or in form of a pharmaceutically acceptable salt or solvate, which are useful in treating inflammatory or obstructive airways, pulmonary hypertension, pulmonary fibrosis, liver fibrosis, muscle diseases and systemic skeletal disorders and other diseases which are mediated by activity of the ALK-5 receptor or ALK-4 receptor. The invention also relates to a method of producing compounds of formula (I) and pharmaceutical compositions. In formula , T is a pyridin-2-yl which is optionally substituted in one position with R¹; T¹ is a pyridinyl which is optionally substituted in one or two positions with R¹, R², R⁵, C₁-C₄-alkoxy group, C₁-C₄-alkoxycarbonyl or cyano group; and R^a and R^b are independently hydrogen; C₁-C₈-alkyl, optionally substituted in one, two or three positions with R⁴; C₃-C₁₀-cycloalkyl, which is optionally substituted in one or two positions with a hydroxy group, amino group, C₁-C₈-alkyl, C₁-C₈-alkoxy group, halogen, cyano group, oxo group, carboxy group or nitro group; or C₆-C₁₅-aryl, optionally substituted in one, two or three positions with a halogen, hydroxy group, amino group, cyano group, oxo group, carboxy group, nitro group or R⁵; R¹ is C₁-C₈-alkyl; R² is C₆-C₁₅-aryl, optionally substituted in one, two or three positions with a halogen, hydroxy group, R¹, R⁵, C₁-C₈-alkylthio group, amino group, C₁-C₈-alkylamino group, etc. The rest of the values of the radicals are given in the claim.

FIELD: chemistry.

SUBSTANCE: described are novel chiral cis-imidazolines selected from a group which includes 2-{4-[(4S,5R)-2-(2-tert-butyl-4-ethoxypyrimidin-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazin-1-yl}-acetamide, [(4S,5R)-2-(2-tert-butyl-4-ethoxypyrimidin-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazol-1-yl]-[4-(1,1-dioxohexahydrothiopyran-4-yl)-piperazin-1-yl]-methanone, [(4S,5R)-2-(2-tert-butyl-4-ethoxypyrimidin-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazol-1-yl]-[4-(3-methanesulphonylpropyl)-piperazin-1-yl]-methanone, 2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridin-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazin-1-yl}-N,N-bis-(2-methoxyethyl)-acetamide. 2-{1-[(48;5K)-2-(6-tert-butyl-4-ethoxypyridin-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperidin-4-yl}-acetamide and others described by the general structural formula (I), and pharmaceutical composition containing said compounds.

EFFECT: compounds can be used as anti-cancer agents, particularly as agents for treating solid tumours.

8 cl, 217 ex

The text descriptions are given in facsimile form.

1. A compound selected from the group including
2-{4-[(4S,5R)-2-(2-tert-butyl-4-ethoxypyridine-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-acetamide", she
[(4S,5R)-2-(2-tert-butyl-4-ethoxypyridine-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihyd imidazol-1-yl]-[4-(1,1-dioxotetrahydrofuran-4-yl)-piperazine-1-yl]-methanon,
[(4S,5R)-2-(2-tert-butyl-4-ethoxypyridine-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-(3-methanesulfonyl)-piperazine-1-yl]-methanon,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-(3-methanesulfonyl)-piperazine-1-yl]-methanon,
rat-[(4S*,5R*)-2-(6-tert-butyl-2-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-(3-methanesulfonyl)-piperazine-1-yl]-methanon,
rat-[(4S*,5R*)-4,5-bis-(4-chlorophenyl)-2-(2,4-dimethoxypyrimidine-5-yl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-(3-methanesulfonyl)-piperazine-1-yl]-methanon,
rat-[(4S*,5R*)-4,5-bis-(4-chlorophenyl)-2-(2-dimethylamino-4-ethoxypyridine-5-yl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-(3-methanesulfonyl)-piperazine-1-yl]-methanon,
rat-[(4S*,5R*)-4,5-bis-(4-chlorophenyl)-2-(4-ethoxy-2-pyridine-3-Yeremey-5-yl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-(3-methanesulfonyl)-piperazine-1-yl]-methanon,
rat-[(4S*,5R*)-4,5-bis-(4-chlorophenyl)-2-(2,6-dimethoxypyridine-3-yl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-(3-methanesulfonyl)-piperazine-1-yl]-methanon,
4-[(4S,5R)-2-(2-tert-butyl-4-ethoxypyridine-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-2-it,
rat-[(4S*,5R*)-2-(2-tert-butyl-4-ethoxypyridine-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-(2-hydroxyethyl)-piperazine-1-yl]-methanon,
2-(2-tert-butyl-4-ecoxib rimidine-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-piperazine-1-ylmethanone,
[2-(2-tert-butyl-4-ethoxypyridine-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-((R)-3,4-dihydroxybutyl)-piperazine-1-yl]-methanon,
dimethylamide 4-[2-(2-tert-butyl-4-ethoxypyridine-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-carboxylic acid,
N-(2-{4-[2-(2-tert-butyl-4-ethoxypyridine-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-ethyl)-acetamide", she
1-{4-[2-(2-tert-butyl-4-ethoxypyridine-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-Etalon,
[(4S,5R)-2-(2-tert-butyl-4-ethoxypyridine-5-yl)-4,5-bis-(4-chlorophenyl)-
4,5-dimethyl-4,5-dihydroimidazole-1-yl]-{4-[2-(2-hydroxyethoxy)-ethyl]-piperazine-1-yl}-methanon,
[2-(2-tert-butyl-4-ethoxypyridine-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-(3-hydroxypropyl)-piperazine-1-yl]-methanon,
2-{4-[2-(2-tert-butyl-4-ethoxypyridine-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-N,N-dimethylacetamide,
[1,4']-bipiperidine-1'-yl-[2-(2-tert-butyl-4-ethoxypyridine-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-methanon,
[2-(2-tert-butyl-4-ethoxypyridine-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-(4-hydroxy-[1,4']-bipiperidine-1'-yl)-methanon,
[2-(2-tert-butyl-4-ethoxypyridine-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-(3-Ki-the Roxy-[1,4']-bipiperidine-1'-yl)-methanon,
[2-(2-tert-butyl-4-ethoxypyridine-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-(3-hydroxymethyl-[1,4']-bipiperidine-1'-yl)-methanon,
[2-(2-tert-butyl-4-ethoxypyridine-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-(4-pyrrolidin-1-reparacin-1-yl)-methanon,
[2-(2-tert-butyl-4-ethoxypyridine-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-(3-hydroxypiperidine-1-yl)-methanon,
[2-(2-tert-butyl-4-ethoxypyridine-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-(3-hydroxyethylpiperazine-1-yl)-methanon,
1-{1-[2-(2-tert-butyl-4-ethoxypyridine-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperidine-4-yl}-[1,4]diazepan-5-he,
[2-(2-tert-butyl-4-ethoxypyridine-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-(4-hydroxypiperidine-1-yl)-methanon,
amide 1-[2-(2-tert-butyl-4-ethoxypyridine-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperidine-4-carboxylic acid,
amide 1-[2-(2-tert-butyl-4-ethoxypyridine-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperidine-3-carboxylic acid,
[(4S,5R)-2-(2-tert-butyl-4-ethoxypyridine-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-((S)-2,3-dihydroxypropyl)-piperazine-1-yl]-methanon,
rat-[(4S*,5R*)-2-(2-tert-butyl-4-ethoxypyridine-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-(2-methane is sulfonylated)-piperazine-1-yl]-methanon,
rat-[(4S*,5R*)-2-(2-tert-butyl-4-ethoxypyridine-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-(2-methoxyethyl)-piperazine-1-yl]-methanon,
rat-N-tert-butyl-2-{4-[(4S*,5R*)-2-(2-tert-butyl-4-ethoxypyridine-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-acetamide", she
rat-2-{4-[(4S*,5R*)-2-(2-tert-butyl-4-ethoxypyridine-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-1-morpholine-4-ylatason,
rat-4-{4-[(4S*,5R*)-2-(2-tert-butyl-4-ethoxypyridine-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-butyronitrile,
rat-[(4S*,5R*)-4,5-bis-(4-chlorophenyl)-2-(4-ethoxy-2-methylsulfonylamino-5-yl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-(3-methanesulfonyl)-piperazine-1-yl]-methanon,
rat-4-[(4S*,5R*)-4,5-bis-(4-chlorophenyl)-2-(4-ethoxy-2-methylsulfonylamino-5-yl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-2-it,
rat-4-[(4S*,5R*)-4,5-bis-(4-chlorophenyl)-2-(4-ethoxy-2-morpholine-4-Yeremey-5-yl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-2-it,
rat-[(4S*,5R*)-4,5-bis-(4-chlorophenyl)-2-(2,4-detoxification-5-yl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-(3-methanesulfonyl)-piperazine-1-yl]-methanon,
rat-[(4S*,5R*)-4,5-bis-(4-chlorophenyl)-2-(4-methoxy-2-methylsulfonylamino-5-yl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-(3-methanesulfonyl)-piperazine-1-yl]-methanon,
2-{4-[(4S,5R)-2-(6-tert-butyl-4-etox is pyridin-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-acetamide", she
rat-[(4S*,5R*)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-((S)-2,3-dihydroxypropyl)-piperazine-1-yl]-methanon,
1-[(4S,5R)-2-(2-tert-butyl-4-ethoxypyridine-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-[1,4]diazepan-5-he,
1-{1-[(4S,5R)-2-(2-tert-butyl-4-ethoxypyridine-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperidine-4-yl}-[1,4]diazepan-5-he,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-(4-methanesulfonylaminoethyl-1-yl)-methanon,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-(2-methanesulfonyl)-piperidine-1-yl]-methanon,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-(1,1-dioxohexane-1λ⁶-thiopyran-4-yl)-piperazine-1-yl]-methanon,
amide 3-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-propane-1-sulfonic acid,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-(2-methanesulfonyl)-piperazine-1-yl]-methanon,
4-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-butyronitrile,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-the l)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-(3,3,3-cryptochromes)-piperazine-1-yl]-methanon,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-(3-acanaloniidae)-piperazine-1-yl]-methanon,
N-(2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-ethyl)-acetamide", she
1-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-2-(thiazol-2-ylamino)-Etalon,
1-{4-[(4S, 5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-2-methylpropan-1-he,
1-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-2,2-DIMETHYLPROPANE-1-he,
2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-N-(2-methoxyethyl)-ndimethylacetamide,
2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-N-cyclopropylacetic,
dimethylamide (4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carboxylic acid,
1-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-2-tetrazol-1-ylatason,
3-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dim the Teal-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-propionamide,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-(1-methyl-1H-pyrrole-2-carbonyl)-piperazine-1-yl]-methanon,
2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-N-cyclopropylamine,
2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-N-(tetrahydrofuran-2-ylmethyl)-ndimethylacetamide,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-(3-methanesulfonyl)-piperidine-1-yl]-methanon,
1-{4-[(4S,5R)-2-(b-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-2-(4-methylthiazole-2-yl)-Etalon,
tert-butyl ester 9-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-3,9-diazaspiro[5.5]undecane-3-carboxylic acid,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-(3,9-diazaspiro[5.5]undec-3-yl)-methanon,
2-{9-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-3,9-diazaspiro[5.5]undec-3-yl}-acetamide", she
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-(1,1-dioxotetrahydrofuran-1λ⁶-thiophene-3-yl)-PI is erasin-1-yl]-methanon,
amide 3-{4-[(4S,5R)-2-(2-tert-butyl-4-ethoxypyridine-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-propane-1-sulfonic acid,
rat-[(4S*,5R*)-2-(2-tert-butyl-4-ethoxypyridine-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-piperidine-1-ylmethanone,
2-{1-[(4S,5R)-2-(2-tert-butyl-4-ethoxypyridine-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperidine-4-yl}-acetamide", she
[(4S,5R)-2-(2-tert-butyl-4-ethoxypyridine-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-(2-methanesulfonyl)-piperidine-1-yl]-methanon,
rat-[(4S*,5R*)-2-(2-tert-butyl-4-ethoxypyridine-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-(1,2-dihydroxyethyl)-piperidine-1-yl]-methanon,
[(4S,5R)-2-(2-tert-butyl-4-ethoxypyridine-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-(4-methanesulfonylaminoethyl-1-yl)-methanon,
[(4S,5R)-2-(2-tert-butyl-4-ethoxypyridine-5-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-(3-methanesulfonyl)-piperidine-1-yl]-methanon,
rat-[(4S*,5R*)-4,5-bis-(4-chlorophenyl)-2-(3,6-dimethoxypyridine-4-yl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-(3-methanesulfonyl)-piperazine-1-yl]-methanon,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-(4-acanaloniidae-1-yl)-methanon,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-CHL is henyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-(2-hydroxyethyl)-piperidine-1-yl]-methanon,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-(2-methoxyethyl)-piperazine-1-yl]-methanon,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-(4-pyrrolidin-1-reparacin-1-yl)-methanon,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-(4-isopropylpiperazine-1-yl)-methanon,
[1,4']-bipiperidine-1'-yl-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-methanon,
1-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-Etalon,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-(4-dimethylaminopyridine-1-yl)-methanon,
hydrochloride {4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-acetic acid,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-(tetrahydrofuran-2-carbonyl)-piperazine-1-yl]-methanon,
dimethylamide 4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-carboxylic acid,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-is]-[4-(3-methoxypropyl)-piperazine-1-yl]-methanon,
2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-1-(1,1-dioxo-λ⁶-thiomorpholine-4-yl)-Etalon,
4-(2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-acetyl)-piperazine-2-it,
1-(2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-acetyl)-[1,4]diazepan-5-he,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-(4-hydroxypiperidine-1-yl)-methanon,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-(3-hydroxypiperidine-1-yl)-methanon,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-(4-hydroxyethylpiperazine-1-yl)-methanon,
2-{4-[(4S,5R-)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-1-pyrrolidin-1-ylatason,
1-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-[1,4]diazepan-5-he,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-((R)-3-methylpiperazin-1-yl)-methanon,
2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazo the ol-1-carbonyl]-piperazine-1-yl}-N-(2,3-dihydroxypropyl)-ndimethylacetamide,
2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-N-isopropyl-N-methylacetamide,
N-tert-butyl-2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-acetamide", she
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-(4-methanesulfonylaminoethyl-1-yl)-methanon,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-{4-[2-(2-hydroxyethoxy)-ethyl]-piperazine-1-yl}-methanon,
2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-1-(4-methylpiperazin-1-yl)-Etalon,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-(4-cyclopropanecarbonyl-1-yl)-methanon,
4-[4-(2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-acetyl)-piperazine-1-yl]-benzonitrile,
2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-N-(2-hydroxy-1,1-dimethylethyl)-ndimethylacetamide,
2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-N-(2-hydroxy-1-hydroxymethyl-1-m is teletel)-ndimethylacetamide,
4-{1-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperidine-4-yl}-piperazine-2-it,
4-{1-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperidine-4-yl}-1-methylpiperazin-2-it,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-(3,4-dihydroxybutyl)-piperazine-1-yl]-methanon,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-(1,1-dioxo-1-thiomorpholine-4-yl)-methanon,
2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-1-piperidine-1-ylatason,
2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-N-(2-hydroxyethyl)-acetamide", she
2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-N-[1,4]dioxane-2-ylmethylene,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-(3-hydroxypyrrolidine-1-yl)-methanon,
tert-butyl ester {(S)-1-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-pyrrolidin-3-yl}-carbamino acid,
2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-N-thiazol-5-ylacetamide,
2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-N-pyridin-3-ylacetamide,
2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-N-phenylacetamide,
2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-N-pyridin-4-ylacetamide,
(3-aminopyrrolidine-1-yl)-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-methanon,
N-{1-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-pyrrolidin-3-yl}-oxalate,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-(2,3,4,5-tetrahydrobenzo[b][1,4]diazepin-1-yl)-methanon,
2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-1-(3-hydroxyazetidine-1-yl)-Etalon,
2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-N-(tetrahydropyran-4-yl)-acetamide", she
ethyl ester of (1S,5R)-3-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-3-azabicyclo[3.1.0]hexane-6-carboxylic acid,
2-{4-[(4S,5R)-2-(6-tert-butyl-4-ataxie the one-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-N,N-bis-(2-methoxyethyl)-ndimethylacetamide,
1 azetidin-1-yl-2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-Etalon,
2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-N,N-bis-(2-hydroxyethyl)-acetamide", she
2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-N-[2-(4-methoxyphenyl)-ethyl]-acetamide", she
2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-N-[2-(2-methoxyphenyl)-ethyl]-acetamide", she
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-(7,8-dimethoxy-1,2,3,5-tetrahydrobenzo[e][1,4]diazepin-4-yl)-methanon,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-(7,8-dimethoxy-2,3,4,5-tetrahydrobenzo[e][1,4]diazepin-1-yl)-methanon,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[(1S,5R)-6-(3-hydroxyazetidine-1-carbonyl)-3-azabicyclo[3.1.0]Gex-3-yl]-methanon,
(2-hydroxyethyl)-amide and (1S,5R)-3-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-3-azabicyclo[3.1.0] hexane-6-carboxylic acid,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-d is hydromedusa-1-yl]-[(1S,5R)-6-(3-hydroxypyrrolidine-1-carbonyl)-3-azabicyclo[3.1.0]Gex-3-yl]-methanon,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-(4-methyl-[1,4]diazepan-1-yl)-methanon,
2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]diazepan-1-yl}-acetamide", she
4-(2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-[1,4]diazepan-1-yl}-acetyl)-piperazine-2-it,
2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-N-(6-methoxy-2-methylpyridin-3-yl)-acetamide", she
2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-N-(2-methylpyridin-3-yl)-acetamide", she
2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-N-(2-methoxypyridine-3-yl)-acetamide", she
2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-N-[-ethyl-N-pyridin-3-ylacetamide,
2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-N-(2,6-dimethylpyridin-3-yl)-acetamide", she
tert-butylamide (S)-4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-2-carboxylic acid,
[(4S,5R)-2-(tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-(4-methylpiperazin-1-yl)-piperidine-1-yl]-methanon,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-(4-(morpholine-4-reparacin-1-yl)-methanon,
N-{1-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperidine-4-yl}-acetamide", she
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-(4-methyl-[1,4']-bipiperidine-1'-yl)-methanon,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-(4-ethylpiperazin-1-yl)-piperidine-1-yl]-methanon,
N-{1-[(4S,5R)-2-(b-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperidine-4-yl}-N-methylmethanesulfonamide,
N-{1-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperidine-4-yl}-methanesulfonamide,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-(2-methanesulfonamido)-piperidine-1-yl]-methanon,
methyl ester {1-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperidine-4-yl}-acetic acid,
2-{1-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperidine-4-yl}-1-pyrrolidin-1-ylatason,
2-{1-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorphen is)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperidine-4-yl}-N,N-dimethylacetamide,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-(4-diethylaminophenyl-1-yl)-methanon,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-{4-[(2-methanesulfonyl)-methylamino]-piperidine-1-yl}-methanon,
2-{1-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperidine-4-yl}-N-(2-hydroxyethyl)-acetamide", she
1-{1-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperidine-4-yl}-3-metalmachine,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-(pyrrolidin-1-carbonyl)-piperidine-1-yl]-methanon,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-(piperazine-1-carbonyl)-piperidine-1-yl]-methanon,
1-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-3-methylsulfinylpropyl-1-he,
1-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-3-methanesulfonate-1-he,
(2-methanesulfonyl)-amide 1-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperidine-4-carboxylic acid,
(2-methanol phenylethyl)-methylamide 1-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperidine-4-carboxylic acid,
(2-hydroxyethyl)-amide 1-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperidine-4-carboxylic acid,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-(1,1-dioxo-1 X-thiomorpholine-4-carbonyl)-piperidine-1-yl]-methanon,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-(2-methansulfonate)-piperidine-1-yl]-methanon,
rat-4-[(4S*,5R*)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-2-it,
rat-[(4S*,5R*)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-[4-(morpholine-4-carbonyl)-piperazine-1-yl]-methanon,
4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-2-it,
2-{1-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperidine-4-yl}-acetamide", she
rat-1-{1-[(4S*,5R*)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-6HC-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperidine-4-yl}-[1,4]diazepan-5-he,
1-{1-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperidine-4-yl}-[1,4]diazepan-5-he,
2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-di is hydromedusa-1-carbonyl]-piperazine-1-yl}-N-pyridin-2-ylacetamide,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-piperazine-1-ylmethanone,
((S)-3,4-dihydroxybutyl)-amide of (4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carboxylic acid,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-(3,6-dihydro-2N-pyridine-1-yl)-methanon,
[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-(3,4-dihydroxypyridine-1-yl)-methanon,
methyl-((2S,3R,4R,5R)-2,3,4,5,6-pentahydroxy)-amide of (4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carboxylic acid,
2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-N-pyridin-2-ylmethylene,
2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-N-pyridin-3-ylmethylene,
2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-N-pyridin-4-ylmethylene,
2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-N-furan-2-ylmethylene,
{1-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl}-45-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperidine-4-yl}-acetic acid,
2-{1-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperidine-4-yl}-N-pyridin-2-ylmethylene,
2-{1-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperidine-4-yl}-N-pyridin-3-ylacetamide,
2-{1-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperidine-4-yl}-1-(4-methylpiperazin-1-yl)-Etalon,
2-{1-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperidine-4-yl}-N,N-bis-(2-methoxyethyl)-ndimethylacetamide,
dimethylamide 4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-sulfonic acid,
(2-hydroxyethyl)-amide of (4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carboxylic acid,
(2-hydroxyethyl)-methylamide (4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carboxylic acid,
bis-(2-methoxyethyl)-amide of (4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carboxylic acid,
tert-butyl ether ({1-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperidine-4-yl}-carbamino acid,
(4-aminopiperidin-1-the l)-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-yl]-methanon,
tert-butyl ether 4-{[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-amino}-piperidine-1-carboxylic acid,
(1-methanesulfonamido-4-yl)-amide (4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carboxylic acid,
ethylamide 4-{[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-amino}-piperidine-1-carboxylic acid,
(1-carbamoylmethyl-4-yl)-amide (4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carboxylic acid,
1-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperidine-4-one,
methyl ester 1-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperidine-4-carboxylic acid,
1-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperidine-4-carboxylic acid,
3-{1-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperidine-4-yloxy}-propionamide,
3-{1-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperidine-4-yloxy}-propionitrile,
1-{1-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine the-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperidine-4-yl}-3-isopropylamino,
1-{1-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperidine-4-yl}-3-pyridin-3-Ilocano and
2-{1-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperidine-4-ylamino}-ndimethylacetamide.

2. The Union, representing 2-{4-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperazine-1-yl}-N,N-bis-(2-methoxyethyl)-ndimethylacetamide.

3. The Union, representing 2-{1-[(4S,5R)-2-(6-tert-butyl-4-ethoxypyridine-3-yl)-4,5-bis-(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazole-1-carbonyl]-piperidine-4-yl}-ndimethylacetamide.

4. Pharmaceutical composition having anti-proliferative activity, comprising a compound according to any one of claims 1 to 3 together with a pharmaceutically acceptable inert filler.

5. The compound according to claims 1-3, intended for use as a medicine.

6. The compound according to claims 1-3, intended for use as a drug for cancer treatment.

7. The compound according to claims 1-3, intended for use as a drug for the treatment of solid tumors.

8. The compound according to claims 1-3, intended for use as a drug for the treatment of tumors of the breast, colon, lung and prostate is elez.