Cycloalkylidene compounds, pharmaceutical compositions based on them, their use and method of selective bonding er α - and er β -estrogen receptors

FIELD: chemistry.

SUBSTANCE: present invention pertains to new cycloalkylidene compounds with formula (I), to their pharmaceutical salts, esters and amide, capable of selective bonding ERα- and ERβ-estrogen receptors, as well as to pharmaceutical compositions based on them, their use in making medicinal preparations and the method of selective bonding ERα- and ERβ-estrogen receptors. . Denotations of R1-R7, X, p, q, as well as specific representatives of new cycloalkylidene compounds are given in the formula of invention.

EFFECT: obtaining new cylcoalkylidene compounds.

31 cl, 6 dwg, 108 ex

 

The text descriptions are given in facsimile form.

1. The compound of formula (I)

including its pharmaceutically acceptable salts, esters and amides,

where R1represents IT;

each of R2and R4independently selected from HE, C1-12the alkyl or halogen;

each of p and q is independently selected from 0,1 or 2;

R3represents a -(Y)z-R8;

z is 0 or 1;

Y represents-C≡or CRe=CRf-;

X represents -(CH2)n-, where n means the AET 0, 1, 2, or 3, -C(Rg)2-, -O - or-S-;

each R5represents N; or together both R5form a bridge alkylenes chain -(CH2)m-where m is 2, 3 or 4, when each R6and each R7represents H, and X represents -(CH2)m-2-;

each of R6and R7selected from N or C1-12of alkyl;

when z is 0, R8represents a C1-12alkyl, cyano, -O(Rh)tCN, -CO2N -(Rh)tCO2H, -O(Rh)tCO2H -(Rh)tOH, O(Rh)tOH, -O(Rh)tO(Rh)tOH, -CONRaRb, -SO2Rd, -NRaSO2Rd, -CORc, -NRaCORc; 5 - or 6-membered heteroaryl containing one or two heteroatoms, selected from nitrogen and oxygen, possibly substituted C1-12the alkyl, C1-12alkoxy, -CO2N, -CONRaRb, -(Rh)tHe, HE, cyano, halogen, -SO2Rd, -CH=SSOON; phenyl, possibly substituted C1-12the alkyl, C1-12alkoxy, -CO2N, -CONRaRb, -(Rh)tOH, HE, cyano, halogen, -NRaSO2Rd, -NRaCORc, -SO2Rd, -CH=CHCOOH, 5 - or 6-membered heterocyclyl containing nitrogen and oxygen as heteroatoms;

when z is 1, R8predstavljaet a-CO 2N -(Rh)tCO2H -(Rh)tOH, -CONRaRbor RHO3NRa; or

when z is 1, and Y represents-C≡ -, R8may also represent H;

t denotes a number from 1 to 8;

Rarepresents H, C1-12alkyl, possibly substituted-CO2N, or C3-10cycloalkyl;

Rbrepresents H, C1-12alkyl, possibly substituted-CO2N, or C3-10cycloalkyl;

Rcrepresents a C1-12alkyl, C3-10cycloalkyl or phenyl;

Rdrepresents a C1-12alkyl, C3-10cycloalkyl or phenyl; or

Raand Rbcan be combined with the atoms to which they are linked, with the formation of 5 - or 6-membered heterocyclyl ring, possibly substituted-CO2N; and

each of Reand Rfindependently selected from H and C1-12of alkyl;

Rgrepresents a C1-12alkyl;

each Rhindependently represents-CRjRk-, where each Rjand Rkindependently selected from H and C1-12the alkyl.

2. The compound according to claim 1, where the specified alkyl represents a C1-8the alkyl and the alkoxy is a1-8alkoxy.

3. The compound according to claim 1, where each of p and q is 0.

4. With the Association according to claim 1, where z is 1, Y is-CRe=CRf-, and R8represents-CO2N.

5. The compound according to claim 4, where Reand Rfrepresent N or C1-8alkyl.

6. The compound according to claim 1, where z is 1, Y is-CRe=CRf-, and R8represents-C(O)NRaRb.

7. The connection according to claim 6, where each of Raand Rbrepresents N.

8. The compound according to claim 1, where z is 1, Y is- ≡C-, and R8represents-CO2N -(Rh)tCO2H or -(CH2)tOH.

9. The compound according to claim 1, where each of R6and R7represents N or C1-8alkyl.

10. The compound according to claim 1, in which X represents -(CH2)n-.

11. The connection of claim 10, where n means 1.

12. Connection to item 11, where R6and R7represent1-12alkyl.

13. The connection of claim 10, where n represents 2 or 3.

14. The connection indicated in paragraph 13, where R6and R7represent hydrogen.

15. The compound according to claim 1, where X represents-O-.

16. The connection indicated in paragraph 15, where R6and R7represent1-12alkyl.

17. The compound according to claim 1, where z is 0, and R8represents-CO2H, -NRaSO2Rd, phenyl or 5 - or 6-membered heteroaryl containing one or two heteroatoms selected from nitrogen the oxygen.

18. The connection 17, where R8represents phenyl, possibly substituted by one or more of cyano, halogen, 5 - or 6-membered heterocyclyl containing nitrogen and oxygen as heteroatoms, -CO2H -(Rh)tOH, -SO2Rd, -C(O)NRaRb, -NRaCORc, -NRaSO2Rdand-CH=CH-CO2N.

19. Connection p, where Rarepresents H, Rbrepresents H, Rcrepresents a C1-12alkyl, and Rdrepresents a C1-12alkyl.

20. The connection 17, where R8represents-CO2N.

21. The connection 17, where R8represents-NRaSO2Rd, Rarepresents N, and Rdrepresents a C1-12alkyl or phenyl.

22. The connection 17, where R8represents isoxazolyl, oxazolyl, pyrimidyl, pyridyl or furyl.

23. The compound according to claim 1, where R8is a-CONRaRband Raand Rbtogether with the formation of 5 - or 6-membered heterocyclyl ring, possibly substituted-CO2N.

24. The compound according to claim 1, chosen from:

(2E)-3-{4-[cyclopentolate(4-hydroxyphenyl)methyl]phenyl}-2-propanolol acids;

(2E)-3-{4-[cyclohexylidene(4-hydroxyphenyl)methyl]phenyl}-2-propanolol acids;

(2E)-3-{4-[cycle is reptilian(4-hydroxyphenyl)methyl]phenyl}-2-propanolol acid;

(2E)-3-{4-[cyclohexylidene(4-hydroxyphenyl)methyl]phenyl}-2-propenamide;

(2E)-3-{4-[cycloheptylamine(4-hydroxyphenyl)methyl]phenyl}-2-propenamide;

(2E)-3-{4-[(4-hydroxyphenyl)(3,3,5,5-tetramethylcyclopentadiene)methyl]phenyl}-2-propanolol acids;

(2E)-3-{4-[(4-hydroxyphenyl)(3,3,5,5-tetramethylcyclopentadiene)-methyl]phenyl} -2-propenamide;

4-[[4-(1H-pyrrol-2-yl)phenyl](3,3,5,5-tetramethylcyclopentadiene)-methyl]phenol;

(2E)-3-{4-[(4,4-dimethylcyclohexyl)(4-hydroxyphenyl)methyl]phenyl}-2-propanolol acids;

4-[(4-hydroxyphenyl)(3,3,5,5-tetramethylcyclopentadiene)-methyl]benzoic acid;

(2E)-3-{4-[cyclohexylidene(4-hydroxy-2-were)methyl]phenyl}-2-propanolol acids;

(2E)-3-{4-[cyclohexylidene(4-hydroxy-3-were)methyl]phenyl}-2-propanolol acids;

(2E)-3-{4-[(4-hydroxyphenyl)(tetrahydro-4H-thiopyran-4-ilidene)methyl]phenyl}-2-propanolol acids;

1-((2E)-3-{4-[cycloheptylamine(4-hydroxyphenyl)methyl]phenyl}-2-propenyl)-3-piperidinecarboxylic acids;

1-((2E)-3-{4-[cycloheptylamine(4-hydroxyphenyl)methyl]phenyl}-2-propenyl)-4-piperidinecarbonitrile acids;

1-((2E)-3-{4-[cycloheptylamine(4-hydroxyphenyl)methyl]phenyl}-2-propanol)Proline;

(2E)-3-{4-[bicyclo[3.3.1]non-9-ilidene(4-hydroxyphenyl)methyl]phenyl)-2-propanolol acids;

(2E)-3-{4-[(4-hydroxyphenyl)(tetrahydro-4H-Piran-4-Liden)methyl]-phenyl}prop-2-ene acid;

(2E)-3-{4-[cyclooctylamine(4-hydroxyphenyl)methyl]phenyl}prop-2-ene acid;

(2E)-3-{4-[(4-hydroxyphenyl)(2,2,6,6-tetramethylethylene-4H-Piran-4-ilidene)methyl]phenyl}prop-2-ene acid;

N-{4-[(4-hydroxyphenyl)(3,3,5,5-tetramethylcyclopentadiene)-methyl]phenyl}ndimethylacetamide;

(2E)-3-{4-[(4-hydroxyphenyl)(tetrahydro-4H-Piran-4-ilidene)methyl]phenyl}-2-methylprop-2-ene acid;

4-[[4-({2-[(2-hydroxyethyl)oxy]ethyl}oxy)phenyl](3,3,5,5-tetramethylcyclopentadiene)methyl]phenol;

ethyl-hydro-(E)-2-{4-[cycloheptylamine(4-hydroxyphenyl)methyl]-phenyl}aterfront;

(2E)-3-{4-[cyclohexylidene(4-hydroxyphenyl)methyl]-2-were}-2-propanolol acids;

(2E)-3-{3-chloro-4-[cyclohexylidene(4-hydroxyphenyl)methyl]phenyl}-2-propanolol acids;

(2E)-3-{4-[cyclohexylidene(4-hydroxyphenyl)methyl]-3-forfinal}-2-propanolol acids;

(2E)-3-{4-[cyclohexylidene(3-fluoro-4-hydroxyphenyl)methyl]phenyl}-2-propanolol acids;

(2E)-3-{4-[cyclohexylidene(4-hydroxyphenyl)methyl]-2-forfinal}-2-propanolol acids;

4-[[4-(methylsulphonyl)phenyl](3,3,5,5-tetramethylcyclopentadiene)-methyl]phenol;

4-[(4-hydroxyphenyl)(3,3,5,5-tetramethylcyclopentadiene)-methyl]benzamide;

4-[{4-[(2-hydroxyethyl)oxy]phenyl}(3,3,5,5-tetramethylcyclopentadiene)-methyl]phenol;

4'-[(4-hydroxyphenyl)(3,3,5,5-tetramethylcyclopentadienyl]-3-biphenylcarbonic acid;

4'-[(4-hydroxyphenyl)(3,3,5,5-tetramethylcyclopentadiene)methyl]-4-biphenylcarbonic acids;

(2E)-3-{4-[(3-chloro-4-hydroxyphenyl)(cyclohexylidene)methyl]phenyl}-2-propanolol acids;

(2E)-3-{4-[cyclohexylidene(2-fluoro-4-hydroxyphenyl)methyl]phenyl}-2-propanolol acids;

(2E)-3-{4-[cyclohexylidene(4-hydroxy-2,3-dimetilfenil)methyl]phenyl}-2-propanolol acids;

(2E)-3-{4-[cyclohexylidene(2,3-debtor-4-hydroxyphenyl)methyl]phenyl}-2-propanolol acids;

(2E)-3-{4-[(3-chloro-4-hydroxyphenyl)(cyclopeptide)methyl]phenyl}-2-propanolol acids;

(2E)-3-{4-[(3-chloro-4-hydroxyphenyl)(3,3,5,5-tetramethylcyclopentadiene)methyl]phenyl}-2-propanolol acids;

(2E)-3-{4-[(3-chloro-4-hydroxyphenyl)(2,2,6,6-tetramethylethylene-4H-Piran-4-ilidene)methyl]phenyl}-2-propanolol acids;

(2E)-3-{4-[(3-fluoro-4-hydroxyphenyl)(cyclopeptide)methyl]phenyl}-2-propanolol acids;

(2E)-3-{4-[(3-fluoro-4-hydroxyphenyl)(2,2,6,6-tetramethylethylene-4H-Piran-4-ilidene)methyl]phenyl}-2-propanolol acids;

(2E)-3-{4-[(3-fluoro-4-hydroxyphenyl)(3,3,5,5-tetramethylcyclopentadiene)methyl]phenyl}-2-propanolol acids;

4-[[4-(3-hydroxy-1-propyne-1-yl)phenyl](3,3,5,5-tetramethylcyclopentadiene)methyl]phenol;

4-[(4-ethynylphenyl)(3,3,5,5-tetramethylcyclopentadiene)methyl]phenol;

3-{4-[(4-hydroxyphenyl)(3,3,5,5-tetramethylcyclopentadiene)-methyl]phenyl}2-propanolol acid;

{4-[(4-hydroxyphenyl)(3,3,5,5-tetramethylcyclopentadiene)-methyl]phenyl}acetic acid;

4-[cycloheptylamine(4-hydroxyphenyl)methyl]benzoic acid;

4-[cyclohexylidene(4-hydroxyphenyl)methyl]benzoic acid;

4-[cyclooctylamine(4-hydroxyphenyl)methyl]benzoic acid;

4-[[4-(1,3-oxazol-2-yl)phenyl](3,3,5,5-tetramethylcyclopentadiene)-methyl]phenol;

4'-[(4-hydroxyphenyl)(3,3,5,5-tetramethylcyclopentadiene)methyl]-3-biphenylcarboxylic;

4-[[4-(5-pyrimidinyl)phenyl](3,3,5,5-tetramethylcyclopentadiene)-methyl]phenol;

4-[[4'-(methylsulphonyl)-4-biphenylyl](3,3,5,5-tetramethylcyclopentadiene)methyl]phenol;

(2E)-3-{4'-[(4-hydroxyphenyl)(3,3,5,5-tetramethylcyclopentadiene)methyl]-3-biphenylyl}-2-propanolol acids;

trifenatate 4-[[4-(3-pyridinyl)phenyl](3,3,5,5-tetramethylcyclopentadiene)methyl]phenol;

3-{4-[(4-hydroxyphenyl)(3,3,5,5-tetramethylcyclopentadiene)methyl]phenyl}propionic acid;

4-[(4,4-dimethylcyclohexyl)-(4-hydroxyphenyl)-methyl]-benzoic acid;

4-[cyclopeptide-(3-fluoro-4-hydroxyphenyl)-methyl]-benzoic acid;

3-{4-[cyclopeptide-(4-hydroxyphenyl)-methyl]-3-forfinal}-acrylic acid;

N-{4-[(4-hydroxyphenyl)-(3,3,5,5-tetramethylcyclopentadiene)-methyl]-phenyl}-methanesulfonamide;

N-{4-[(4-hydroxyphenyl)-(3,3,5,5-t is trimethylcyclohexylidene)-methyl]-phenyl}-benzosulfimide;

(2E)-3-{4-[cycloheptylamine(4-hydroxyphenyl)methyl]-2-forfinal}-2-propanolol acids;

({4-[cycloheptylamine(4-hydroxyphenyl)methyl]phenyl}oxy)acetic acid;

4-{cyclopeptide[4-(3-furanyl)phenyl]methyl}phenol;

4-{cyclopeptide[4-(2-furanyl)phenyl]methyl}phenol;

4-{cyclooctadiene[4-(2-furanyl)phenyl]methyl}phenol;

4-{cyclooctadiene[4-(3-furanyl)phenyl]methyl}phenol;

4-{cyclooctadiene[4-(3,5-dimethyl-4-isoxazolyl)phenyl]methyl}phenol;

4-{cyclopeptide[4-(3,5-dimethyl-4-isoxazolyl)phenyl]methyl}phenol;

4-[cycloheptylamine(4-hydroxyphenyl)methyl]benzonitrile;

4-[(4-hydroxyphenyl)(3,3,5,5-tetramethylcyclopentadiene)methyl]benzonitrile;

(2E)-3-{4-[(4-hydroxyphenyl)(2,2,6,6-tetramethylethylene-4H-Piran-4-ilidene)methyl]phenyl}-2-methyl-2-propanolol acids;

(2E)-3-{4-[cyclooctylamine(4-hydroxyphenyl)methyl]phenyl}-2-methyl-2-propanolol acids;

({4-[cycloheptylamine(4-hydroxyphenyl)methyl]phenyl}oxy)acetonitrile;

4-({4-[cycloheptylamine(4-hydroxyphenyl)methyl]phenyl}oxy)butyric acid;

({4-[(4-hydroxyphenyl)(3,3,5,5-tetramethylcyclopentadiene)-methyl]phenyl}oxy)acetic acid;

4-({4-[(4-hydroxyphenyl)(3,3,5,5-tetramethylcyclopentadiene)-methyl]phenyl}oxy)butyric acid;

4-(cyclopeptide{4-[(2-hydroxyethyl)oxy]phenyl}is ethyl)phenol;

2-({4-[cycloheptylamine(4-hydroxyphenyl)methyl]phenyl}oxy)-2-methylpropionic acids;

2-({4-[(4-hydroxyphenyl)(3,3,5,5-tetramethylcyclopentadiene)-methyl]phenyl}oxy)-2-methylpropionic acids;

((4-[(4-hydroxyphenyl)(3,3,5,5-tetramethylcyclopentadiene)-methyl]phenyl}oxy)acetonitrile;

4-(cyclopeptide{4-[(2-hydroxy-1,1-dimethylethyl)oxy]phenyl}methyl)phenol;

4-[[4-(3-hydroxypropyl)phenyl](3,3,5,5-tetramethylcyclopentadiene)-methyl]phenol;

N-{4'-[(4-hydroxyphenyl)-(3,3,5,5-tetramethylcyclopentadiene)-methyl]-biphenyl-4-yl}-ndimethylacetamide;

N-{4'-[(4-hydroxyphenyl)-(3,3,5,5-tetramethylcyclopentadiene)-methyl]-biphenyl-4-yl}-methanesulfonamide;

4-[[4-(3-furanyl)phenyl](3,3,5,5-tetramethylcyclopentadiene)-methyl]phenol;

4-[[4-(3,5-dimethyl-4-isoxazolyl)phenyl](3,3,5,5-tetramethylcyclopentadiene)methyl]phenol;

4-[[4'-(4-morpholinyl)-4-biphenylyl](3,3,5,5-tetramethylcyclopentadiene)-methyl]phenol;

3-fluoro-4'-[(4-hydroxyphenyl)(3,3,5,5-tetramethylcyclopentadiene)methyl]-4-biphenylcarboxylic;

4'-[(4-hydroxyphenyl)(3,3,5,5-tetramethylcyclopentadiene)methyl]-4-biphenylcarboxylic;

4'-[cyclooctylamine(4-hydroxyphenyl)methyl]-4-biphenylcarboxylic;

4-{cyclopeptide[4-(5-hydroxy-1-penten-1-yl)phenyl]methyl}phenol;

4-[[4-(3-hydroxy-3-methyl-1-butyn-1-yl)phenyl](3,3,5,5-tetramethylsilane siligen)methyl]phenol;

4-[[4-(4-hydroxy-1-buten-1-yl)phenyl](3,3,5,5-tetramethylcyclopentadiene)methyl]phenol;

5-{4-[(4-hydroxyphenyl)(3,3,5,5-tetramethylcyclopentadiene)-methyl]phenyl}-4-pentenovoi acids;

1-{4-[(4-hydroxyphenyl)(3,3,5,5-tetramethylcyclopentadiene)-methyl]phenyl}of ethanone;

4-[[4'-(hydroxymethyl)-4-biphenylyl](3,3,5,5-tetramethylcyclopentadiene)methyl]phenol;

4-[[3'-(hydroxymethyl)-4-biphenylyl](3,3,5,5-tetramethylcyclopentadiene)methyl]phenol;

4'-[(4-hydroxyphenyl)(3,3,5,5-tetramethylcyclopentadiene)methyl]-2-biphenylcarbonic acid; and

4-[[2'-(hydroxymethyl)-4-biphenylyl](3,3,5,5-tetramethylcyclopentadiene)methyl]phenol;

including their pharmaceutically acceptable salts, esters and amides.

25. Connection

including its pharmaceutically acceptable salts, esters and amides.

26. Pharmaceutical composition having the ability to selectively bind ERαand ERβ-estrogen receptors containing an effective amount of a compound according to any one of claims 1 to 25 and a pharmaceutically acceptable carrier.

27. The compound according to any one of claims 1 to 25, intended for the manufacture of drugs having the ability to selectively bind ERαand ERβ-estrogen receptors.

28. The use of compounds according to any one of claims 1 to 25 in about the svojstva medicines having the ability to selectively bind ERαand ERβ-estrogen receptors.

29. The use of compounds according to any one of claims 1 to 25 in the manufacture of medicaments for use in the treatment or prevention of osteoporosis, bone demineralization, reduced(CSOs) bone(CSOs) mass, density, or growth, osteoarthritis, obesity, cardiovascular disease or functional cardiac abnormalities, congestive heart failure, breast cancer, diabetes, depression, depressive symptoms, vaginal dryness, pruritus, dyspareunia, rheumatoid arthritis, menopausal or postmenopausal disorders, vasomotor symptoms, urogenital or vulvar vaginal atrophy, atrophic vaginitis, female sexual dysfunction, increase libido, for the treatment of hypoactive sexual disorder, sexual arousal disorder, for increasing the frequency and intensity of orgasms or endometriosis.

30. The use of compounds according to clause 29, where the condition or disorder is a menopausal or postmenopausal disorders, vasomotor symptoms, urogenital or vulvar vaginal atrophy, atrophic vaginitis, endometriosis, female sexual dysfunction, breast cancer, depressive symptoms, diabetes, demineralization KOs is her or osteoporosis.

31. Process for the selective binding of ERαand ERβ-estrogen receptors, which is administered an effective amount of a compound according to any one of claims 1 to 25.



 

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