New derivatives of aminocyclohexane

 

The invention relates to organic chemistry, in particular to new compounds of the formula (I)

in which U represents O or a lone pair of electrons; V represents O, S, - CH2-, - CH=CH - or - C-; W represents CO, COO, CONR1CSO , CSNR1, SO2or SO2NR1; m and n independently of one another each represents a number from 0 to 7, and the sum of m+n is from 0 to 7, provided that m represents 0, if V denotes O or S; And1represents H, lower alkyl, hydroxy(ness.)alkyl or (ness.)alkenyl; And2means (ness.)alkyl, cycloalkyl, cycloalkyl(lower)alkyl or (ness.)alkenyl, optionally substituted by a group R2;3and4each denotes a hydrogen atom or (ness.)alkyl; And5denotes H, (ness.)alkyl, (ness.)alkenyl or aryl(ness.)alkyl; And6means (ness.)alkyl, cycloalkyl, aryl, aryl(lower)alkyl, heteroaryl, heteroaryl(ness.)alkyl, (ness.)alkoxycarbonyl(ness.)alkyl; R2denotes hydroxy, hydroxy(ness.)alkyl, (ness.)alkoxy, (ness.)alkoxycarbonyl, N(R4,R5) or thio(ness.)alkoxy; R1, R3, R4and R5each independently from each other, oboznachaet is false esters. These compounds can be used in the treatment and/or prophylaxis of diseases which are associated with a 2.3-Occidentale-linearality, such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, fungal infections and parasitic infections. 4 C. and 31 C.p. f-crystals, 1 table.

Description text in facsimile form (see graphic part)

Claims

1. The compounds of formula (I)

in which U represents O or a lone pair of electrons;

V represents O, S, - CH2-, - CH=CH - or - C-;

W represents CO, COO, CONR1CSO , CSNR1, SO2or SO2NR1;

m and n independently of one another each represents a number from 0 to 7, and the sum of m+n is from 0 to 7, provided that m represents 0, if V denotes O or S;

And1represents H, lower alkyl, hydroxy(ness.)alkyl or (ness.)alkenyl;

And2means (ness.)alkyl, cycloalkyl, cycloalkyl(lower)alkyl or (ness.)alkenyl, optionally substituted by a group R2;

And3and4each denotes a hydrogen atom or (ness.)alkyl or

And1and2or And1and3associated m is)alkylene or (ness.)albaniles, optionally substituted by a group R2where one group - CH2- combinations-And1-And2- or - A1-And3may be optionally substituted by a group NR, S or O, or

And3and4linked to form a ring together with the carbon atom to which they are attached, and the mix - And3-And4- represents the group - (CH2)2-5- which may be optionally mono - or polyamidine (ness.)by alkyl;

And5denotes H, (ness.)alkyl, (ness.)alkenyl or aryl(ness.)alkyl;

And6means (ness.)alkyl, cycloalkyl, aryl, aryl(lower)alkyl, heteroaryl, heteroaryl(ness.)alkyl, (ness.)alkoxycarbonyl(ness.)alkyl;

R2denotes hydroxy, hydroxy(ness.)alkyl, (ness.)alkoxy, (ness.)alkoxycarbonyl, N(R4,R5) or thio(ness.)alkoxy;

R1, R3, R4and R5each independently of one another denotes a hydrogen atom or (ness.)alkyl,

and their pharmaceutically acceptable salts and/or pharmaceutically acceptable esters.

2. Connection on p. 1, in which And3and4are not interconnected to form a ring together with the carbon atom to which they relate.

3. Connection And2And3And4And5and6have the values listed in any of the p. 1 or 2.

4. Compounds according to any one of paragraphs.1-3, in which U denotes a lone pair of electrons.

5. Compounds according to any one of paragraphs.1-4, in which V denotes O.

6. Compounds according to any one of paragraphs.1-4, in which V denotes-CH2-.

7. Compounds according to any one of paragraphs.1-4, in which V denotes-C=C-.

8. Compounds according to any one of paragraphs.1-4, in which V denotes-C=C.

9. Compounds according to any one of paragraphs.1-8, in which W represents CO, COO, CONR1, CSNR1, SO2; or SO2NR1, a R denotes a hydrogen atom.

10. Compounds according to any one of paragraphs.1-9, in which W represents COO or SO2.

11. Compounds according to any one of paragraphs.1-10, in which n denotes 0.

12. Compounds according to any one of paragraphs.1-10, in which n denotes 1.

13. Compounds according to any one of paragraphs.1-12, in which m denotes a number from 1 to 6.

14. Compounds according to any one of paragraphs.1-12, in which m denotes 0, and V denotes-C=C-or-C=C.

15. Compounds according to any one of paragraphs.1-14, in which And1denotes H, methyl, ethyl, isopropyl, 2-hydroxyethyl or 2-propenyl.

16. Compounds according to any one of paragraphs.1-15, in which And1means (ness.)alkyl, cycloalkyl(ness.)alkyl or (ness.)alkenyl, neobezatelna according to any one of paragraphs.1-16, in which a denotes a methyl, ethyl, 2-hydroxyethyl, 2-propenyl, propyl or isopropyl.

18. Compounds according to any one of paragraphs.1-14, in which And1and2linked with the formation of rings, and the mix-And1-And2- means (ness.)alkylene or (ness.)albaniles, optionally substituted by a group R2where one group-CH2- combinations-And1-And2- may be optionally replaced by a group NR3, S or O, where R2and R3have the values listed in paragraph 1.

19. Connection on p. 18, which1and2linked with the formation of rings, and the mix-And1-And2- means (ness.)alkylene or (ness.)albaniles, optionally substituted by a group R, where one group-CH2- combinations-And1-And2- may be optionally replaced by an atom Oh, where R2denotes hydroxy or 2-hydroxyethyl.

20. Connection on p. 19, in which And1and2linked with the formation of rings, and the mix-And1-And2- represents -(CH2)5-.

21. Compounds according to any one of paragraphs.1-20, in which And3denotes a hydrogen atom.

22. Compounds according to any one of paragraphs.1-21, in which And4denotes a hydrogen atom.

23. Soy is ring together with the carbon atom, with which they are associated, and the mix-And3-And4- represents -(CH2)2-.

24. Compounds according to any one of paragraphs.1-23, have And5denotes H, (ness.)alkyl, (ness.)alkenyl or benzyl, optionally substituted by a halogen atom.

25. Compounds according to any one of paragraphs.1-24, And have5denotes methyl or ethyl.

26. Compounds according to any one of paragraphs.1-25, And have6means (ness.)alkyl, cycloalkyl, phenyl, naphthyl, phenyl(ness.)alkyl, pyridyl, indolyl, indolinyl, thienyl, thienylmethyl, furylmethyl, benzodioxol, hinely, isoxazolyl or imidazolyl, optionally substituted by one or more substituents selected from the group comprising (ness.)alkyl, (ness.)alkoxy, (ness.)alkylsulphonyl, (ness.)alkoxycarbonyl, fluorine atoms, chlorine, bromine, CN, CF3, NO2and N(R6,R7), where each of R6and R7independently from each other represent a hydrogen atom or (ness.)alkyl.

27. Compounds according to any one of paragraphs.1-26, And have6denotes phenyl, optionally substituted by one or more substituents selected from the group comprising fluorine atoms, chlorine, bromine and CF3.

28. Compounds according to any one of paragraphs.1-27, have And6represents 4-chlorophenyl, 4-bromophenyl ifir TRANS-{4-[6-(allylmethylamine)-hexyloxy]cyclohexyl}methylcarbamate acid,

4-cryptomaterial ether of TRANS-{4-[4-(allylmethylamine)butoxy]cyclohexyl}methylcarbamate acid,

TRANS-N-[4-(6-diethylaminoethoxy)cyclohexyl]-N-methyl-4-triftoratsetilatsetonom,

4-hlorfenilovy ether of TRANS-{4-[4-(allylmethylamine)butoxy]cyclohexyl}methylcarbamate acid,

4-hlorfenilovy ether of TRANS-{4-[2-(allylmethylamine)ethylsulfanyl]cyclohexyl}methylcarbamate acid,

4-hlorfenilovy ether of TRANS-{4-[5-(allylmethylamine)pentyl]cyclohexyl}methylcarbamate acid,

4-cryptomaterial ester, TRANS-(4-{4-[ethyl(2-hydroxyethyl)amino]butoxy}cyclohexyl)methylcarbamate acid,

TRANS-N-[4-(3-allylamines)cyclohexyl]-N-methyl-4-triftoratsetilatsetonom,

4-cryptomaterial ether of TRANS-{4-[5-(allylmethylamine)pentyl]cyclohexyl}methylcarbamate acid,

4-cryptomaterial ester, TRANS-(4-{5-[ethyl(2-hydroxyethyl)amino]pentyl}cyclohexyl)methylcarbamate acid,

4-brompheniramine ester, TRANS-(4-{5-[ethyl(2-hydroxyethyl)amino]pentyl} cyclohexyl)methylcarbamate acid,

TRANS-N-(4-{5-[ethyl(2-hydroxyethyl)amino]pentyl}cyclohexyl)-N-methyl-4-triftoratsetilatsetonom,

4-cryptomaterial ether of TRANS-N-[4-(4-di is about)pentyl]cyclohexyl}methylcarbamate acid,

4-hlorfenilovy ether of TRANS-{4-[3-(allylmethylamine)prop-1-inyl]cyclohexyl}methylcarbamate acid,

TRANS-N-{4-[5-(allylmethylamine)pentyl]cyclohexyl}-N-methyl-4-triftoratsetilatsetonom,

4-hlorfenilovy ester, TRANS-(4-{3-[ethyl(2-hydroxyethyl)amino]propyl}cyclohexyl)methylcarbamate acid,

4-hlorfenilovy ether of TRANS-{4-[4-(allylmethylamine)butyl]cyclohexyl}methylcarbamate acids and their pharmaceutically acceptable salts.

30. The compound according to any one of paragraphs.1-29 selected from the group including

TRANS-N-[4-dimethylamino-1-inyl)cyclohexyl]-N-methyl-4-triftoratsetilatsetonom,

4-hlorfenilovy ester, TRANS-methyl[4-(5-piperidine-1-alpental)cyclohexyl]carbamino acid,

4-cryptomaterial ester, TRANS-methyl[4-(5-methylaminomethyl)cyclohexyl]carbamino acid,

4-hlorfenilovy ester, TRANS-(4-{5-[ethyl(2-hydroxyethyl)amino]Penta-1-inyl}cyclohexyl)methylcarbamate acid,

TRANS-N-ethyl-N-(4-{4-[(2-hydroxyethyl)methylamino]butoxy}cyclohexyl)-triftoratsetilatsetonom,

TRANS-(1E)-N-(4-{3-[ethyl(2-hydroxyethyl)amino]propenyl}cyclohexyl)-N-methyl-4-triftoratsetilatsetonom,

TRANS-4-bromo-N-[4-(2-diisopropylaminoethyl)cyclohexyl]-N - methylbenzenesulfonamide,

4-b is piperidine-1-libutil)cyclohexyl]-4-triftoratsetilatsetonom,

TRANS-N-(4-{4-[bis(2-hydroxyethyl)amino]butoxy}cyclohexyl)-N-ethyl-4-triftoratsetilatsetonom,

TRANS-4-bromo-N-methyl-N-[4-(2-piperidine-1-ylethoxy)cyclohexyl]benzosulfimide,

TRANS-N-[4-(4-dimethylaminoethoxy)cyclohexyl]-N-ethyl-4-triftoratsetilatsetonom,

4-hlorfenilovy ester, TRANS-methyl - {4-[3-(methylpropylamine)prop-1-inyl]cyclohexyl}carbamino acid,

TRANS-(1E)-N-methyl-N-{4-[3-(methylpropylamine)propenyl]cyclohexyl}-4-triftoratsetilatsetonom,

TRANS-N-(4-{4-[ethyl(2-hydroxyethyl)amino]but-l-inyl}cyclohexyl)-N-methyl-4-triftoratsetilatsetonom,

TRANS-N-methyl-N-{4-[4-(methylpropylamine)buta-1-inyl]cyclohexyl}-4-triftoratsetilatsetonom,

TRANS-N-(4-[2-(l-dimethylaminoisopropyl)ethoxy]cyclohexyl}-N-methyl-4-triftoratsetilatsetonom and their pharmaceutically acceptable salts.

31. Method of preparing compounds according to any one of paragraphs.1-30, which includes the interaction of the compounds of formula (II)

in which And5matter specified in paragraph 1,

Z represents the group (A1And2)N-C (3,A4)-(CH2)m-V-(CH2)nor BUT-(CH2)nthat And1And2And3And4, V, m and n have C1SO2NR1-A6where And6matter specified in paragraph 1.

32. Compounds according to any one of paragraphs.1-30, obtained according to the method according to p. 31.

33. Pharmaceutical composition having the property of inhibiting 2,3-Occidentale-lanostanolides (oscs), comprising the compound according to any one of paragraphs.1-30, and a pharmaceutically acceptable carrier and/or adjuvant.

34. Compounds according to any one of paragraphs.1-30 for use as therapeutically active substances.

35. The method of treatment and/or prevention of diseases that are associated with a 2.3-Occidentale-linearality (oscs), such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, fungal infections and parasitic infections, which includes the introduction of the human or animal a compound according to any one of paragraphs.1-30.

 

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< / BR>
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