RU2009124589A - SUBSTITUTED ESTRATRIENE DERIVATIVES AS 17BETA HSD INHIBITORS - Google Patents

Abstract

 1. The compound of General formula I! ! where -X-A-Y- collectively represents a group selected from! (a) -CO-NR4-,! (b) -CO-O-,! (c) -CO-,! (d) -CO-NH-NR4-,! (e) -NR3-CO-NR4-,! (f) -NR3-CO-O-,! (g) -NR3-CO-,! (h) -NR3-CO-NH-SO2-,! (i) -NR3-SO2-NR4-,! (j) -NR3-SO2-O-,! (k) -NR3-SO2-! (l) -O-CO-NR4-,! (m) -O-CO-,! (n) -O-CO-NH-SO2-NR4-,! (o) -O-,! (p) groups! or ; ! where R3 is —H or - (C1-C4) alkyl; ! R1 is selected from the group consisting of! (a) -B (OR9) (OR10),! (b) -CO-OR6,! (c) -CO-NR7R8,! (d) -NR7R8,! (e) -NR5-CO-R6,! (f) -NR5-SO2-R6,! where R5 is —H or - (C1-C4) alkyl; ! R6, R7, R8, R9 and R10 are independently selected from the group consisting of! (a) -H,! (b) optionally substituted - (C1-C14) alkyl,! (c) optionally substituted aryl or aryl- (C1-C14) alkyl,! (e) optionally substituted heteroaryl or heteroaryl- (C1-C14) alkyl,! (d) optionally substituted cycloheteroalkyl or cycloheteroalkyl- (C1-C14) alkyl, or! R7 and R8, together with the nitrogen atom to which they are attached, form a heterocyclic 4-, 5-, 6-, 7- or 8-membered ring, which is optionally saturated, partially unsaturated or aromatic and which optionally contains 1, 2 or 3 additional heteroatoms selected from the group consisting of N, O and S, wherein the number of additional N atoms is 0, 1, 2 or 3, and the number of O and S atoms for each is 0, 1 or 2; and which optionally may be part of a complex condensed ring system, where the rings or ring system are optionally substituted; ! in case R1 represents an —NR5-CO-R6 group, R5 and R6 together with the nitrogen atom to which R5 is attached and the carbonyl group to which R6 is attached can form 4-, 5-, 6-, 7- or an 8-membered lactam ring,! if R1 is -NR5-SO2-R6, then R5 and R6 are

Claims (54)

1. The compound of General formula I

, where -X-A-Y- collectively represents a group selected from (a) -CO-NR ⁴ -, (b) -CO-O-, (c) -CO-, (d) -CO-NH-NR ⁴ -, (e) -NR ³ -CO-NR ⁴ -, (f) -NR ³ -CO-O-, (g) -NR ³ -CO-, (h) -NR ³ -CO-NH-SO ₂ -, (i) -NR ³ -SO ₂ -NR ⁴ -, (j) -NR ³ -SO ₂ -O-, (k) -NR ³ -SO ₂ - (l) -O-CO-NR ⁴ -, (m) -O-CO-, (n) -O-CO-NH-SO ₂ -NR ⁴ -, (o) -O-, (p) groups

or

; where R ³ represents -H or - (C ₁ -C ₄ ) alkyl; R ¹ selected from the group consisting of (a) -B (OR ⁹ ) (OR ¹⁰ ), (b) -CO-OR ⁶ , (c) -CO-NR ⁷ R ⁸ , (d) -NR ⁷ R ⁸ , (e) -NR ⁵ -CO-R ⁶ , (f) —NR ⁵ —SO ₂ —R ⁶ , where R ⁵ represents -H or - (C ₁ -C ₄ ) alkyl; R ⁶ , R ⁷ , R ⁸ , R ⁹ and R ^{10 are} independently selected from the group consisting of (a) -H, (b) optionally substituted - (C ₁ -C ₁₄ ) alkyl, (c) optionally substituted aryl or aryl- (C ₁ -C ₁₄ ) alkyl, (e) optionally substituted heteroaryl or heteroaryl- (C ₁ -C ₁₄ ) alkyl, (d) optionally substituted cycloheteroalkyl or cycloheteroalkyl- (C ₁ -C ₁₄ ) alkyl, or R ⁷ and R ^8, together with the nitrogen atom to which they are attached, form a heterocyclic 4-, 5-, 6-, 7- or 8-membered ring, which is optionally saturated, partially unsaturated or aromatic and which optionally contains 1, 2 or 3 additional heteroatoms selected from the group consisting of N, O and S, wherein the number of additional N atoms is 0, 1, 2 or 3, and the number of O and S atoms for each is 0, 1 or 2; and which optionally may be part of a complex condensed ring system, where the rings or ring system are optionally substituted; in case R ¹ represents an —NR ⁵ —CO — R ⁶ group, R ⁵ and R ⁶ together with the nitrogen atom to which R ⁵ is attached and the carbonyl group to which R ⁶ is attached can form 4-, 5 -, 6-, 7- or 8-membered lactam ring, in case R ¹ represents —NR ⁵ —SO ₂ —R ⁶ , then R ⁵ and R ⁶ together with the nitrogen atom to which R ⁵ is attached and the sulfoxide group to which R ⁶ is attached can form 4-, A 5-, 6-, 7- or 8-membered sultamic ring, or R ⁹ and R ^10, together with the boronic acid group to which they are attached, form a 5- or 6-membered ring, which is optionally substituted with 1, 2, 3 or 4 - (C ₁ -C ₄ ) alkyl groups; n represents 1, 2, 3, 4, 5 or 6, or, if -XAY- represents -CO-NR ⁴ -, -CO-O-, -CO- or -CO-NH-NR ⁴ - groups, then n may also be 0; R ¹¹ represents H, - (C ₁ -C ₁₄ ) alkyl, (C ₁ -C ₁₄ ) alkoxy or (C ₁ -C ₁₄ ) alkoxy- (C ₁ -C ₁₄ ) alkyl; R ¹² and R ¹³ together represent = O, or R ¹² and R ¹³ each individually represent F; R ² and R ^{4 are} independently selected from (a) -H, (b) optionally substituted - (C ₁ -C ₁₄ ) alkyl, (c) optionally substituted acyl, provided that -XAY- collectively is -CO-NH-NR ⁴ or groups

or

, (d) optionally substituted aryl or aryl- (C ₁ -C ₁₄ ) alkyl, (e) optionally substituted heteroaryl or heteroaryl- (C ₁ -C ₁₄ ) alkyl, (f) optionally substituted cycloheteroalkyl or cycloheteroalkyl- (C ₁ -C ₁₄ ) alkyl; or R ² and R ⁴ together with the nitrogen atom to which R ² and R ^{4 are} attached form a heterocyclic 4-, 5-, 6-, 7- or 8-membered ring, which is optionally saturated, partially unsaturated or aromatic and which optionally contains 1, 2 or 3 additional heteroatoms selected from the group consisting of N, O and S, wherein the number of additional N atoms is 0, 1, 2 or 3, and the number of O and S atoms for each is 0, 1 or 2 ; and which optionally may be part of a complex condensed ring system, where the rings or ring system are optionally substituted; and all its stereoisomers, pharmaceutically acceptable salts, metabolites, solvates and prodrugs. 2. The compound of General formula I according to claim 1, which is an optically pure enantiomer of the formula (II)

or a pharmaceutically acceptable salt thereof. 3. The compound of General formula I according to claim 1, which is an optically pure enantiomer of formula (III)

or a pharmaceutically acceptable salt thereof. 4. The compound according to claim 1, where -X-A-Y- collectively represents a group selected from (a) -CO-NR ⁴ -, (b) -CO-O-, (c) -CO-, (d) -CO-NH-NR ⁴ -, (e) -NH-CO-NH-, (f) -NH-CO-O-, (g) -NH-CO-, (h) -NH-CO-NH-SO ₂ -, (i) -NH-SO ₂ -NH-, (j) -NH-SO ₂ -O-, (k) -NH-SO ₂ - (l) -O-CO-NH-, (m) -O-CO-, (n) -O-CO-NH-SO ₂ -NR ⁴ -, (o) -O-, (p) groups

or

. 5. The compound according to claim 4, in which -X-A-Y- collectively represents a group selected from (a) -CO-NR ⁴ - and (b) groups

or

. 6. The compound according to claim 1, where R ² and R ^{4 are} independently selected from (a) —H, where if —XAY— collectively is —CO — O— or —CO—, then R ^{2 is} not —H, (b) - (C ₁ -C ₁₂ ) alkyl, which is optionally substituted with one or more substituents independently selected from the group consisting of halogen, —CN, —OR ¹⁴ , —SR ¹⁴ , —NR ¹⁵ R ¹⁶ , —CONR ¹⁵ R ¹⁶ , —SO ₂ NR ¹⁵ R ¹⁶ , —CO — R ¹⁷ , —COOR ¹⁴ , —NH — CO — R ^17, and —O — SO ₂ —R ¹⁸ ; the number of these substituents is 1, 2, 3, 4 or 5 for halogens and 1 or 2 for any combination of substituents, (c) acyl - (C = O) -Z, where Z is hydrogen, (C ₁ -C ₄ ) alkyl, aryl, aryl- (C ₁ -C ₄ ) alkyl or heteroaryl- (C ₁ -C ₄ ) alkyl; where each aryl or aryl- (C ₁ -C ₄ ) alkyl is optionally substituted at the aryl moiety with 1, 2 or 3 substituents independently selected from the group consisting of a hydroxy group, halogen, —O- (C ₁ -C ₄ ) alkyl, - (C ₁ -C ₄ ) alkyl or halogenated - (C ₁ -C ₄ ) alkyl; (d) aryl and aryl- (C ₁ -C ₁₂ ) alkyl, in which the aryl moiety is optionally substituted with one or more substituents independently selected from the group consisting of halogen, -OR ¹⁴ , - (C ₁ -C ₆ ) alkyl, halogenated - (C ₁ -C ₆ ) alkyl, -COOR ¹⁴ , - (C ₁ -C ₆ ) alkyl-COOR ¹⁴ , -CONR ¹⁵ R ¹⁶ , -CN, -CO-R ¹⁷ , -SR ¹⁴ , -SO ₂ -R ¹⁸ , -SO ₂ NR ¹⁵ R ¹⁶ , -NO ₂ , -NR ¹⁵ R ¹⁶ , -NH-CO-R ¹⁷ and heteroaryl; the number of these substituents is 1, 2, 3, 4 or 5 for halogens and 1, 2 or 3 for any combination of these substituents, and where each heteroaryl is optionally substituted with 1 or 2 substituents independently selected from oxo group, halogen, - (C ₁ -C ₄ ) alkyl and halogenated - (C ₁ -C ₄ ) alkyl, or in which the aryl moiety is optionally substituted with two groups that are attached to adjacent carbon atoms and combined into one saturated or partially unsaturated cyclic 5-, 6-, 7- or an 8 membered ring system, optionally containing 1, 2 or 3 heteroatoms selected from the group consisting of N, O and S, the number of N atoms is 0, 1, 2 or 3, and the number of O and S atoms for each is 0, 1 or 2; and in which (C ₁ -C ₁₂ ) the alkyl part is optionally substituted with 1, 2 or 3 halogens or 1 or 2 hydroxyl groups; (e) heteroaryl and heteroaryl- (C ₁ -C ₁₂ ) alkyl, in which the heteroaryl part is optionally substituted with one or more substituents independently selected from the group consisting of halogen, —OR ¹⁴ , - (C ₁ -C ₆ ) alkyl, halogenated - (C ₁ -C ₆ ) alkyl, - (C ₁ -C ₆ ) acyl-COCR ¹⁴ , -COOR ¹⁴ , -CONR ¹⁵ R ¹⁶ , -CN, -CO-R ¹⁷ , -SR ¹⁴ , -SO ₂ -R ¹⁸ , -SO ₂ NR ¹⁵ R ¹⁶ , -NR ¹⁵ R ¹⁶ , -NH-CO-R ¹⁷ , aryl- (C ₁ -C ₄ ) -alkyl and aryl, the number of these substituents is 1, 2, 3 4 or 5 for halogens and 1, 2 or 3 for any combination of these substituents, and where each aryl is optionally substituted with 1, 2 or 3 substituents, n independently selected from the group consisting of hydroxyl, halogen, - (C ₁ -C ₆ ) alkoxy, - (C ₁ -C ₆ ) alkyl, halogenated - (C ₁ -C ₆ ) alkyl and halogenated - (C ₁ -C ₆ ) alkoxy groups; and where (C ₁ -C ₁₂ ) the alkyl part is substituted with 1, 2 or 3 halogens; (f) cycloheteroalkyl and cycloheteroalkyl- (C ₁ -C ₁₂ ) alkyl, wherein the cycloheteroalkyl moiety is optionally substituted with one or more substituents independently selected from the group consisting of oxo, - (C ₁ -C ₆ ) -alkyl, aryl, aryl - (C ₁ -C ₄ ) -alkyl, -OR ¹⁴ , -COOR ¹⁴ , - (C ₁ -C ₆ ) alkyl-COOR ¹⁴ , -SR ¹⁴ , -CN, -SO ₂ NR ¹⁵ R ¹⁶ , -NR ¹⁵ R ¹⁶ , -CONR ¹⁵ R ¹⁶ , -CO-R ¹⁷ and -NH-CO-R ¹⁷ groups, the number of these substituents is 1, 2, 3, 4 or 5 for halogens and 1, 2 or 3 for any combination of these substituents , and where each aryl group is optionally substituted with 1, 2 or 3 substituents, not pendently selected from the group consisting of hydroxyl, halogen, - (C ₁ -C ₆₎ alkoxy, - (C ₁ -C ₆₎ alkyl, halogenated - (C ₁ -C ₆₎ alkyl and halogenated - (C ₁ -C ₆ ) alkoxy groups; or R ² and R ⁴ together with the nitrogen atom to which R ² and R ^{4 are} attached form a heterocyclic 4-, 5-, 6-, 7- or 8-membered ring, which is optionally saturated, partially unsaturated or aromatic, which optionally contains 1, 2 or 3 additional heteroatoms selected from the group consisting of N, O and S, the number of additional N atoms is 0, 1, 2 or 3, and the number of O and S atoms for each is 0, 1 or 2; and where the ring is optionally part of a multiple condensed ring system, where the ring and ring system are optionally substituted with 1, 2 or 3 substituents independently selected from the group consisting of oxo group, - (C ₁ -C ₆ ) alkyl, halogen, -OR ¹⁴ , -COOR ¹⁴ , - (C ₁ -C ₆ ) alkyl-COOR ¹⁴ , -SR ¹⁴ , -CN, -NR ¹⁵ R ¹⁶ , -CONR ¹⁵ R ¹⁶ , -SO ₂ NR ¹⁵ R ¹⁶ , aryl, aryl- (C ₁ -C ₄ ) -alkyl, heteroaryl and cycloheteroalkyl groups, where each (C ₁ -C ₆ ) alkyl group is optionally substituted with 1, 2 or 3 substituents independently selected from hydroxyl, halogen, - (C ₁ -C ₄ ) alkox or halogenated - (C ₁ -C ₄₎ alkoxy groups, wherein each aryl or heteroaryl moiety is optionally substituted with 1, 2 or 3 substituents independently selected from the group consisting of hydroxyl, halogen, - (C ₁ -C ₆₎ alkyl, - (C ₁ -C ₆ ) alkoxy, halogenated - (C ₁ -C ₆ ) alkyl, halogenated - (C ₁ -C ₆ ) alkoxy, - (C ₁ -C ₆ ) alkyl-COOR ¹⁴ and —COOR ¹⁴ groups, or where each aryl part is optionally substituted by two groups that are attached to adjacent carbon atoms and form a saturated or partially unsaturated cyclic 5-, 6- or 7-membered ring a system, optionally containing 1 or 2 heteroatoms selected from N, O and S, wherein the number of N atoms is 0, 1 or 2, and the number of O and S atoms for each is 0, 1 or 2, and where each cycloheteroalkyl is optionally substituted with 1, 2 or 3 substituents independently selected from the group consisting of oxo group, - (C ₁ -C ₆ ) alkyl, aryl, aryl (C ₁ -C ₄ ) alkyl, hydroxyl, - (C ₁ -C ₆ ) alkoxy, - (C ₁ -C ₆ ) alkyl-COOR ¹⁴ and COOR ¹⁴ groups; or the ring is optionally substituted by two groups that are attached to one carbon atom and form a saturated or partially unsaturated cyclic 4-, 5-, 6-, 7- or 8-membered ring system, optionally containing 1, 2 or 3 heteroatoms selected from N , O and S, wherein the number of N atoms is 0, 1, 2 or 3, and the number of O and S atoms for each is 0, 1 or 2, and the cyclic ring system is optionally substituted with 1 or 2 substituents independently selected from the group consisting of from an oxo group, (C ₁ -C ₆ ) alkyl, aryl and aryl- (C ₁ -C ₄ ) -alkyl groups; where R ¹⁴ , R ¹⁵ , R ¹⁶ , R ¹⁷ and R ^{18 are} independently selected from the group consisting of -H, - (C ₁ -C ₄ ) alkyl, halogenated - (C ₁ -C ₄ ) alkyl, aryl and aryl- (C ₁ -C ₄ ) alkyl, or R ¹⁵ and R ¹⁶ together with the nitrogen atom to which they are attached form a heterocyclic 5-, 6- or 7-membered ring, optionally containing 1 or 2 additional heteroatoms selected from N , O and S, wherein the number of N atoms is 0, 1 or 2, and the number of O and S atoms for each is 0 or 1, and where n represents (a) 1, 2, 3, 4, 5, or 6, if -XAY- collectively is -NH-CO-NR ⁴ -, -NH-CO-O-, -NH-CO-, -NH-CO -NH-SO ₂ -, -NH-SO ₂ -NR ⁴ -, -NH-SO ₂ -O-, -SO ₂ -NH-, -O-CO-NR ⁴ -, -O-CO-, -O —CO — NH — SO ₂ —NR ⁴ - or —O—, or (b) 0, 1, 2, 3, 4, or 5 if —XAY— collectively is —CO — NR ⁴ -, —CO — O—, —CO—, or —CO-NH-NR ⁴ -. 7. The compound according to claim 1, where R ⁶ , R ⁷ , R ⁸ , R ⁹ and R ^{10 are} independently selected from the group consisting of (a) -H, (b) - (C ₁ -C ₁₂ ) alkyl, which is optionally substituted with halogen, —CN, —OR ¹⁴ , —SR ¹⁴ , —NR ¹⁵ R ¹⁶ , —CONR ¹⁵ R ¹⁶ , —SO ₂ NR ¹⁵ R ¹⁶ , - CO — R ¹⁷ , —COOR ¹⁴ , —NH — CO — R ^17, or —O — SO ₂ —R ¹⁸ groups; the number of these substituents is up to 5 for halogens and 1 or 2 for any combination of substituents, (c) aryl and aryl- (C ₁ -C ₁₂ ) alkyl a, in which the aryl part in the aryl or aryl (C ₁ -C ₁₂ ) alkyl groups is optionally substituted with one or more substituents independently selected from the group consisting of halogen , -OR ¹⁹ , - (C ₁ -C ₆ ) alkyl, halogenated - (C ₁ -C ₆ ) alkyl, -COOR ¹⁹ , - (C ₁ -C ₆ ) alkyl-COOR ¹⁹ , -CONR ²⁰ R ²¹ , - CN, —CO — R ²² , —SR ¹⁹ , —SO ₂ —R ²³ , —SO ₂ NR ²⁰ R ²¹ , —NO ₂ , —NR ²⁰ R ²¹ , —NH — CO — R ²² and heteroaryl; the number of said substituents is 1, 2, 3, 4 or 5 for halogens and 1, 2 or 3 for any combination of these substituents, and where each heteroaryl is optionally substituted with 1 or 2 substituents independently selected from an oxo group, halogen, - (C ₁ -C ₄ ) alkyl and halogenated - (C ₁ -C ₄ ) alkyl groups; or where the aryl moiety in the aryl or aryl (C ₁ -C ₁₂ ) alkyl groups is optionally substituted with two groups that are attached to adjacent carbon atoms and form one saturated or partially unsaturated cyclic 5-, 6-, 7- or 8-membered system rings optionally containing 1, 2 or 3 heteroatoms selected from the group consisting of N, O and S, the number of N atoms being 0, 1, 2 or 3, and the number of O and S atoms for each being 0, 1 or 2 wherein the ring system is optionally substituted with 1 or 2 oxo groups; and where (C ₁ -C ₁₂ ) the alkyl part is optionally substituted with 1, 2 or 3 halogens or 1 or 2 hydroxyl groups; (d) heteroaryl and heteroaryl- (C ₁ -C ₁₂ ) alkyl, in which the heteroaryl moiety is optionally substituted with one or more substituents independently selected from the group consisting of halogen, oxo, -OR ¹⁹ , - (C ₁ -C ₆ ) alkyl, halogenated - (C ₁ -C ₆ ) alkyl, -COOR ¹⁹ , - (C ₁ -C ₆ ) alkyl-COOR ¹⁹ , -CONR ²⁰ R ²¹ , -CN, -CO-R ²² , -SR ¹⁹ , - SO ₂ -R ²³ , -SO ₂ NR ²⁰ R ²¹ , -NR ²⁰ R ²¹ , -NH-CO-R ²² , aryl- (C, -C ₄ ) -alkyl and aryl, and the number of these substituents is 1, 2 , 3, 4 or 5 for halogens and 1, 2 or 3 for any combination of these substituents, and where each aryl is optionally substituted with 1, 2 or 3 batch Ithel independently selected from the group consisting of hydroxyl, halogen, - (C ₁ -C ₆₎ -alkoxy, - (C ₁ -C ₆₎ alkyl, halogenated - (C ₁ -C ₆₎ alkyl and halogenated - (C ₁ -C ₆ ) alkoxy groups; and where (C ₁ -C ₁₂ ) the alkyl part is optionally substituted with 1, 2 or 3 halogens; (e) cycloheteroalkyl and cycloheteroalkyl- (C ₁ -C ₁₂ ) alkyl, in which the cycloheteroalkyl moiety is optionally substituted with one or more substituents independently selected from the group consisting of oxo, - (C ₁ -C ₆ ) -alkyl, aryl, aryl- (C ₁ -C ₄ ) -alkyl, -OR ¹⁹ , -COOR ¹⁹ , - (C ₁ -C ₆ ) alkyl-COOR ¹⁹ , -SR ¹⁹ , -CN, -SO ₂ NR ²⁰ R ²¹ , -NR ²⁰ R ²¹ , -CONR ²⁰ R ²¹ , -CO-R ²² and -NH-CO-R ²² groups, the number of the indicated substituents being 1, 2, 3, 4 or 5 for halogens and 1, 2 or 3 for any combination these substituents, and where each aryl group is optionally substituted with 1, 2 or 3 amestitelyami independently selected from the group consisting of hydroxyl, halogen, (C ₁ -C ₆₎ alkoxy, - (C ₁ -C ₆₎ alkyl, halogenated - (C ₁ -C ₆₎ alkyl and halogenated - (C ₁ -C ₆ ) alkoxy groups; or R ⁷ and R ⁸ together with the nitrogen atom to which they are attached form a heterocyclic 4-, 5-, 6-, 7- or 8-membered ring, which is optionally saturated, partially unsaturated or aromatic, which optionally contains 1, 2 or 3 additional heteroatoms selected from the group consisting of N, O and S, the number of additional N atoms is 0, 1, 2 or 3, the number of O and S atoms for each is 0, 1 or 2; and where the ring is not necessarily part of a system of several condensed rings, and where the ring or ring system is optionally substituted with 1, 2 or 3 substituents independently selected from the group consisting of oxo group, - (C ₁ -C ₆ ) alkyl, halogen, -OR ¹⁹ , -COOR ¹⁹ , - (C ₁ - C ₆ ) alkyl-COOR ¹⁹ , -SR ¹⁹ , -CN, -NR ²⁰ R ²¹ , -CONR ²⁰ R ²¹ , -SO ₂ NR ²⁰ R ²¹ , aryl, aryl (C ₁ -C ₄ ) -alkyl groups, where each (C ₁ -C ₆ ) alkyl group is optionally substituted with 1, 2 or 3 substituents independently selected from hydroxyl, halogen, - (C ₁ -C ₄ ) alkoxy or halogenated - (C ₁ -C ₄ ) alkoxy groups, wherein each aryl moiety is optionally substituted with 1, 2 or 3 substituents independently selected from the group consisting of hydroxyl, halogen, - (C ₁ -C ₆ ) alkyl, - (C ₁ -C ₆ ) alkoxy, halogenated - (C ₁ - C ₆ ) alkyl, halogenated - (C ₁ -C ₆ ) alkoxy, - (C ₁ -C ₆ ) alkyl-COOR ¹⁹ and -COOR ¹⁹ groups, or where R ¹⁹ , R ²⁰ , R ²¹ , R ²² and R ^{23 are} independently selected from the group consisting of -H, - (C ₁ -C ₄ ) alkyl, halogenated - (C ₁ -C ₄ ) alkyl, aryl and aryl- (C ₁ -C ₄ ) alkyl, or R ²⁰ and R ²¹ together with the nitrogen atom to which they are attached form a heterocyclic 5-, 6- or 7-membered ring, optionally containing 1 or 2 additional heteroatoms selected from N , O and S, wherein the number of N atoms is 0, 1 or 2, and the number of O and S atoms for each is 0 or 1, if R ¹ is —NR ⁵ —CO — R ⁶ , then R ⁵ and R ⁶ may form together with the nitrogen atom to which R ⁵ is attached and the carbonyl group to which R ⁶ , 4-, 5-, 6 are attached -, 7- or 8-membered lactam ring, if, R ¹ is —NR ⁵ —SO ₂ —R ⁶ , then R ⁵ and R ⁶ can form together with the nitrogen atom to which R ⁵ is attached and a sulfoxide group to which R ⁶ , 4-, 5- is attached A 6-, 7-, or 8-membered sultamic ring, or R ⁹ and R ¹⁰ together with the boron atom to which they are attached form a 5- or 6-membered ring, which is optionally substituted with 1, 2, 3 or 4 - (C ₁ -C ₄ ) alkyl groups. 8. The compound according to claim 1, where R ¹ selected from the group consisting of (a) -B (OH) ₂ , (b) —CO — OH, (c) -CO-NR ⁷ R ⁸ , (d) -NR ⁷ R ⁸ , (e) -NR ⁵ -CO-R ⁶ . 9. The compound of claim 8, wherein R ¹ is —CO — NR ⁷ R ⁸ , and R ⁷ and R ^{8 are} independently selected from the group consisting of —H and - (C ₁ –C ₆ ) alkyl. 10. The compound of claim 8, where R ¹ represents —NR ⁵ —CO — R ⁶ , R ⁵ and R ⁶ together with the nitrogen atom to which R ⁵ is attached and the carbonyl group to which R ⁶ is attached form a heterocyclic 5- or 6-membered lactam ring. 11. The compound of claim 8, where R ¹ is —NR ⁷ R ⁸ , and R ⁷ and R ^{8 are} independently selected from the group consisting of (a) -H, (b) - (C ₁ -C ₆ ) alkyl, (c) phenyl and phenyl- (C ₁ -C ₄ ) alkyl, in which the phenyl moiety is optionally substituted with 1 or 2 substituents independently selected from the group consisting of halogen, -OR ¹⁹ , - (C ₁ -C ₄ ) alkyl, halogenated - (C ₁ -C ₄ ) alkyl, —CN and —SO ₂ NR ²⁰ R ²¹ , or wherein the phenyl moiety is optionally substituted with two groups that are attached to adjacent carbon atoms and combined into one saturated or partially unsaturated cyclic 5- or 6-membered ring system, optionally containing 1 or 2 heteroatoms selected from the group consisting of O and S, and the quantities o the O and S atoms for each is 0, 1 or 2, and where the ring system is optionally substituted with 1 or 2 oxo groups; (d) heteroaryl and heteroaryl- (C ₁ -C ₄ ) alkyl wherein the heteroaryl moiety is optionally substituted with 1 or 2 oxo groups; (e) cycloheteroalkyl and cycloheteroalkyl- (C ₁ -C ₄ ) alkyl, in which the cycloheteroalkyl moiety is optionally substituted with an oxo group; or R ⁷ and R ^8, together with the nitrogen atom to which they are attached, form a heterocyclic 5-, 6- or 7-membered ring, which is optionally saturated, partially unsaturated or aromatic, which optionally contains 1 or 2 additional heteroatoms selected from a group consisting of N, O and S, wherein the number of additional N atoms is 0, 1 or 2, and the number of O and S atoms for each is 0 or 1, and where the ring is not necessarily part of a complex condensed ring system and where the ring and ring system are optionally substituted with 1 or 2 substituents independently selected from the group consisting of oxo group, - (C ₁ -C ₄ ) alkyl, -OR ¹⁹ , aryl and aryl (C ₁ -C ₂ ) -alkyl groups where each aryl part is optionally substituted with 1, 2 or 3 substituents independently selected from the group consisting of hydroxyl, halogen, - (C ₁ -C ₄ ) alkyl, - (C ₁ -C ₄ ) alkoxy, halogenated - (C ₁ - C ₄ ) alkyl and halogenated - (C ₁ -C ₄ ) alkoxy groups; where R ¹⁹ , R ²⁰ and R ^{21 are} independently selected from the group consisting of —H, - (C ₁ -C ₄ ) alkyl and halogenated - (C ₁ -C ₄ ) alkyl, or where R ²⁰ and R ²¹ together with an atom the nitrogen to which they are attached form a heterocyclic 5- or 6-membered ring, optionally containing 1 additional heteroatom selected from N, O and S. 12. The compound according to claim 1, where R ² and R ^{4 are} independently selected from (a) —H, where if —XAY— collectively is —CO — O— or —CO—, then R ^{2 is} not —H, (b) - (C ₁ -C ₆ ) alkyl and - (C ₁ -C ₆ ) cycloalkyl, which are optionally substituted with 1 or 2 substituents independently selected from the group consisting of halogen and -OR ¹⁴ , (c) phenyl and phenyl- (C ₁ -C ₄ ) alkyl, in which the phenyl part is optionally substituted with 1 or 2 substituents independently selected from the group consisting of halogen, —OR ¹⁴ , - (C ₁ -C ₆ ) alkyl, and halogenated - (C ₁ -C ₆ ) alkyl, or where the phenyl moiety is optionally substituted by two groups that are attached to adjacent carbon atoms and combined into one saturated or partially unsaturated cyclic 5- or 6-membered ring system, optionally containing 1 or 2 heteroatoms, independently selected from the group consisting of N, O atoms and S, wherein the number of N, O, and S atoms for each is 0, 1, or 2; (d) heteroaryl and heteroaryl- (C ₁ -C ₄ ) alkyl, in which the heteroaryl part is optionally substituted with 1 or 2 substituents independently selected from the group consisting of halogen, -OR ¹⁴ , - (C ₁ -C ₆ ) alkyl, and halogenated - (C ₁ -C ₆ ) alkyl; or R ² and R ⁴ together with the nitrogen atom to which R ² and R ^{4 are} attached form a heterocyclic 5-, 6- or 7-membered ring, which is optionally saturated or partially unsaturated, which optionally contains 1 or 2 additional heteroatoms, selected from N, O and S, wherein the number of additional N atoms is 0, 1 or 2, and the number of O and S atoms for each is 0 or 1, and where the ring is not necessarily part of a complex condensed ring system, wherein the ring and ring system are optionally substituted with 1 or 2 substituents independently selected from the group consisting of oxo group, - (C ₁ -C ₆ ) alkyl, halogen and —OR ¹⁴ groups, where R ¹⁴ selected from the group consisting of -H, - (C ₁ -C ₄ ) alkyl and halogenated - (C ₁ -C ₄ ) alkyl. 13. The compound according to claim 1, where R ¹¹ represents H, - (C ₁ -C ₄ ) alkyl, (C ₁ -C ₄ ) alkoxy, or (C ₁ -C ₄ ) alkoxy- (C ₁ -C ₄ ) alkyl. 14. The compound of claim 13, wherein R ¹¹ is H, ethyl, propyl, methoxyethyl, methoxy, ethoxy, or methoxyethoxy. 15. The compound of claim 14, wherein R ¹¹ is H. 16. The compound according to claim 1, where n represents 2, 3 or 4, preferably n represents 2 or 3. 17. The compound according to claim 1, where n is 2, the compound is an optically pure enantiomer of the formula (III-b)

18. The compound according to claim 1, where b is 3, the compound is an optically pure enantiomer of the formula (II)

19. The compound according to claim 1, where -X-A-Y- collectively represents a group

or

20. The compound according to claim 1, where R ¹² and R ¹³ represent a group = O. 21. The compound according to claim 1, where R ¹² and R ¹³ each individually represents F. 22. The compound according to claim 1, where R ¹ represents —CO — OH or —CO — NR ⁷ R ⁸ , where R ⁷ and R ^{8 are} independently selected from —H and - (C ₁ -C ₄ ) alkyl; -XAY- collectively represents -CO-NR ⁴ -; R ¹¹ represents —H; R ¹² and R ¹³ represent a group = O, or R ¹² and R ¹³ each individually represents F; n represents 2 or 3. 23. The compound according to claim 1, where R ¹ represents —B (OH) ₂ , —XAY— collectively represents —CO — NR ⁴ -; R ¹¹ represents —H; R ¹² and R ¹³ represent a group = O, or R ¹² and R ¹³ each individually represents F; n represents 2 or 3. 24. The compound according to claim 1, where R ¹ represents NR ⁵ -CO-R ⁶ where R ⁵ and R ⁶ together with the nitrogen atom to which R ⁵ is attached and the carbonyl group to which R ⁶ is attached form a heterocyclic 5 membered lactam ring; -XAY- collectively represents -CO-NR ⁴ -; R ¹¹ represents —H; R ¹² and R ¹³ represent a group = O, or R ¹² and R ¹³ each individually represents F; n represents 2 or 3. 25. The compound according to claim 1, where R ¹ represents —NR ⁷ R ⁸ , —XAY— collectively represents —CO — NR ⁴ -; R ¹¹ represents —H; R ¹² and R ¹³ represent a group = O, or R ¹² and R ¹³ each individually represents F; n represents 2 or 3. 26. The compound of claim 25, wherein R ⁷ and R ^{8 are} independently selected from (a) -H, (b) - (C ₁ -C ₆ ) alkyl, (c) phenyl and phenyl- (C ₁ -C ₂ ) alkyl, in which the phenyl part is optionally substituted with 1 or 2 substituents independently selected from the group consisting of halogen, -OR ¹⁹ , - (C ₁ -C ₄ ) alkyl, halogenated - (C ₁ -C ₄ ) alkyl, —CN and —SO ₂ NR ²⁰ R ²¹ , or, where phenyl is optionally substituted with two groups that are attached to adjacent carbon atoms and combined into one saturated or partially unsaturated cyclic 5- or 6 a membered ring system, optionally containing 1 or 2 heteroatoms selected from the group consisting of O and S, wherein the number of O and S atoms for each is 0, 1 or 2 and wherein the ring system is optionally substituted by 1 or 2 oxo groups; (d) heteroaryl and heteroaryl- (C ₁ -C ₂ ) alkyl, in which the heteroaryl moiety is selected from the group consisting of indolyl, quinolinyl, benzothienyl and pyridinyl, in which the heteroaryl moiety is optionally substituted with 1 or 2 oxo groups; (e) cycloheteroalkyl and cycloheteroalkyl- (C ₁ -C ₄ ) alkyl, in which the cycloheteroalkyl moiety is selected from the group consisting of pyrrolidinyl and oxazolidinyl, in which the cycloheteroalkyl moiety is optionally substituted with an oxo group; or R ⁷ and R ⁸ together with the nitrogen atom to which they are attached form a heterocyclic 5- or 6-membered ring which is saturated or partially unsaturated, which optionally contains 1 additional heteroatom selected from the group consisting of N and O, and also where the ring is not necessarily an element of a complex condensed ring system, and where the ring and ring system are optionally substituted with residues selected from the group consisting of oxo group, phenyl and phenyl- (C ₁ -C ₂ -) -alkyl groups, where each phenyl moiety is optionally substituted with residues selected from the group consisting of halogen and - (C ₁ -C ₄ ) alkoxy; where R ¹⁹ , R ²⁰ and R ^{21 are} independently selected from the group consisting of —H, - (C ₁ -C ₄ ) alkyl and halogenated - (C ₁ -C ₄ ) alkyl groups, or where R ²⁰ and R ²¹ together with the nitrogen atom to which they are attached form a 6-membered heterocyclic ring, optionally containing 1 additional heteroatom selected from N and O. 27. The compound according to claim 1, where R ² and R ^{4 are} independently selected from (a) -H, (b) - (C ₁ -C ₄ ) alkyl, which is optionally substituted with —OR ¹⁴ , (c) - (C ₁ -C ₆ ) cycloalkyl, (d) phenyl and phenyl- (C ₁ -C ₂ ) alkyl, in which the phenyl moiety is optionally substituted with 1 or 2 substituents independently selected from the group consisting of halogen and —OR ¹⁴ , or where the phenyl moiety is optionally substituted by two groups that are attached to adjacent carbon atoms and combined into a saturated cyclic 5- or 6-membered ring system, optionally containing 1 or 2 heteroatoms, independently selected from the group consisting of N, O and S, and the amount the N, O, and S atoms for each is 0, 1, or 2; (e) heteroaryl and heteroaryl- (C ₁ -C ₂ ) alkyl, in which the heteroaryl part is selected from the group consisting of imidazolyl, pyridinyl, indolyl, thiazolyl, in which the heteroaryl part is optionally substituted with (C ₁ -C ₄ ) alkyl; or R ² and R ⁴ together with the nitrogen atom to which R ² and R ^{4 are} attached form a heterocyclic 5-, 6- or 7-membered saturated ring which optionally contains 1 additional heteroatom selected from N and O, where the ring is optional substituted by - (C ₁ -C ₄ ) alkyl; where R ¹⁴ selected from the group consisting of -H, - (C ₁ -C ₄ ) alkyl and halogenated - (C ₁ -C ₄ ) alkyl. 28. The compound according to claim 1, where R ¹ represents -B (OH) ₂ , -XAY- collectively represents a group

or

; R ¹¹ represents H, ethyl, propyl, methoxyethyl, methoxy, ethoxy or methoxyethoxy, preferably H; R ¹² and R ¹³ represent a group = O, or R ¹² and R ¹³ each individually represents F; n represents 2 or 3. 29. The compound of claim 28, wherein R ^{2 is} selected from the group consisting of (a) - (C ₁ -C ₆ ) alkyl, (b) - (C ₁ -C ₆ ) cycloalkyl- (C ₁ -C ₄ ) alkyl; and (c) phenyl and phenyl- (C ₁ -C ₂ ) alkyl, in which the phenyl part is optionally substituted with 1 or 2 substituents independently selected from the group consisting of halogen, - (C ₁ -C ₄ ) alkyl, halogenated - (C ₁ -C ₄ ) alkyl, -OR ¹⁴ , and COOR ¹⁴ , where R ¹⁴ selected from the group consisting of -H, - (C ₁ -C ₄ ) alkyl and halogenated - (C ₁ -C ₄ ) alkyl. 30. The compound according to claim 1, selected from the group consisting of compounds according to the following examples: No. 3 15beta- (3 - [(5-methyl-1,3-thiazol-2-yl) amino] -3-oxopropyl) -17-oxoestra-1 (10), 2,4-triene-3-carboxamide, No. 8 17,17-difluoro-15beta- (3 - [(5-methyl-1,3-thiazol-2-yl) amino] -3-oxopropyl) estra-1 (10), 2,4-trien-3 carboxamide No. 11 [15alpha- (3 - [(5-methyl-1,3-thiazol-2-yl) amino] -3-oxopropyl) -17-oxoestra-1 (10), 2,4-trien-3-yl ] boronic acid, No. 12 [15alpha- (4 - [(3,4-dihydroxybenzyl) amino] -4-oxobutyl) -17-oxoestra-1 (10), 2,4-trien-3-yl] boronic acid, No. 13 [15alpha- [4- (1,3-benzodioxol-5-ylamino) -4-oxobutyl] -17-oxoestra-1 (10), 2,4-trien-3-yl] boronic acid, No. 16 [15alpha- (4 - [(5-methyl-1,3-thiazol-2-yl) amino] -4-oxobutyl) -17-oxoestra-1 (10), 2,4-trien-3-yl ] boronic acid, No. 19 [15alpha- (4 - [(1,3-benzodioxol-5-ylmethyl) amino] -4-oxobutyl) -17-oxoestra-1 (10), 2,4-trien-3-yl] boronic acid, No. 17 [15alpha- [4- (cyclohexylamino) -4-oxobutyl] -17-oxoestra-1 (10), 2,4-trien-3-yl] boronic acid, No. 20 [17-oxo-15alpha- (4-oxo-4-piperidin-1-ylbutyl) estra-1 (10), 2,4-trien-3-yl] boronic acid, No. 22 [15alpha- (4- [benzyl (methyl) amino] -4-oxobutyl) -17-oxoestra-1 (10), 2,4-trien-3-yl] boronic acid, No. 23 [15alpha- [4- (benzylamino) -4-oxobutyl] -17-oxoestra-1 (10), 2,4-trien-3-yl] boronic acid, No. 26 [15alpha- (4 - ([2- (3,4-dimethoxyphenyl) ethyl] (methyl) amino) -4-oxobutyl) -17-oxoestra-1 (10), 2,4-trien-3-yl ] boronic acid, No. 30 [(15beta- (3 - ([2- (7-methyl-1H-indol-3-yl) ethyl] amino) -3-oxopropyl) -17-oxoestra-1 (10), 2,4-triene -3-yl] boronic acid, No. 31 [(15beta- (3 - [(5-methyl-1,3-thiazol-2-yl) amino] -3-oxopropyl) -17-oxoestra-1 (10), 2,4-triene-3- sludge] boronic acid, No. 32 [(15 beta- [3- (cyclohexylamino) -3-oxopropyl] -17-oxoestra-1 (10), 2,4-trien-3-yl] boronic acid, No. 33 [(15beta- (3-morpholin-4-yl-3-oxopropyl) -17-oxoestra-1 (10), 2,4-trien-3-yl] boronic acid, No. 34 [(15beta- (3 - [(1,3-benzodioxol-5-ylmethyl) amino] -3-oxopropyl) -17-oxoestra-1 (10), 2,4-trien-3-yl] boronic acid , No. 35 [17-oxo-15beta- (3-oxo-3-piperidin-1-ylpropyl) estra-1 (10), 2,4-trien-3-yl] boronic acid, No. 37 [(15beta- (3- [benzyl (methyl) amino] -3-oxopropyl) -17-oxoestra-1 (10), 2,4-trien-3-yl] boronic acid, No. 39 [(15 beta- [3- (diethylamino) -3-oxopropyl] -17-oxoestra-1 (10), 2,4-trien-3-yl] boronic acid, No. 45 [(15 beta-[3- (1,3-benzodioxol-5-ylamino) -3-oxopropyl] -17-oxoestra-1 (10), 2,4-trien-3-yl] boronic acid, No. 48 [15alpha- [4- (cyclohexylamino) -4-oxobutyl] -17,17-difluoroestra-1 (10), 2,4-trien-3-yl] boronic acid, No. 49 [15alpha- [4- (diethylamino) -4-oxobutyl] -17,17-difluoroestra-1 (10), 2,4-trien-3-yl] boronic acid, No. 50 [15alpha- (4 - [(1,3-benzodioxol-5-ylmethyl) amino] -4-oxobutyl) -17,17-difluoroestra-1 (10), 2,4-trien-3-yl] boronic acids No. 51 [15alpha- (4 - ([2- (3,4-dimethoxyphenyl) ethyl] (methyl) amino) -4-oxobutyl) -17,17-difluoroestra-1 (10), 2,4-trien-3 -yl] boronic acid, No. 53 [17,17-difluoro-15alpha- (4-oxo-4 - [(pyridin-3-ylmethyl) amino]) estrabutyl-1 (10), 2,4-trien-3-yl] boronic acid, No. 54 [15alpha- [4- (benzylamino) -4-oxobutyl] -17,17-difluoroestra-1 (10), 2,4-trien-3-yl] boronic acid, No. 57 [17,17-difluoro-15alpha- (4-oxo-4-piperidin-1-ylbutyl) estra-1 (10), 2,4-trien-3-yl] boronic acid, No. 58 [(8x, 9x, 14x, 15b) -17,17-difluoro-15- (3 - [(5-methyl-1,3-t No. 53 [17,17-difluoro-15alfa- (4-oxo -4 - [(pyridin-3-ylmethyl) amino]) estrabutyl-1 (10), 2,4-trien-3-yl] boronic acid, No. 75 3 - ([3-methoxy-5- (trifluoromethyl) phenyl] amino) -15alpha- (4-morpholin-4-yl-4-oxobutyl) estra-1 (10) 2,4-trien-17one, No. 76 15 alpha- (4-morpholin-4-yl-4-oxobutyl) -3 - ([3- (morpholin-4-ylsulfonyl) phenyl] amino) estra-1 (10), 2,4-trien-17ona, No. 83 15alpha- (4-morpholin-4-yl-4-oxobutyl) -3- (quinolin-3-ylamino) estra-1 (10), 2,4-trien-17-one, No. 91 3 - [(1,1-dioxo-1-benzothien-6-yl) amino] -15alpha- (4-morpholin-4-yl-4-oxobutyl) estra-1 (10), 2,4-triene -17-she No. 98 3- (benzylamino) -15alpha- (4-morpholin-4-yl-4-oxobutyl) estra-1 (10), 2,4-trien-17-one and any pharmaceutically acceptable salts thereof. 31. The compound according to any one of claims 1 to 30 for use as a medicine. 32. A pharmaceutical composition comprising, as an active agent, a compound of formula (I) according to any one of claims 1-30, and at least one pharmaceutically acceptable carrier. 33. The use of an effective amount of a compound of formula (I) according to any one of claims 1-30 for the treatment or prevention of malignant estradiol-dependent diseases or disorders selected from the group consisting of breast cancer, ovarian cancer, uterine cancer, endometrial cancer and hyperplasia endometrium in humans or mammals. 34. The use of the compounds of formula (I) according to any one of claims 1-30 for the manufacture of medicines for the treatment and prevention of malignant estradiol-dependent diseases or disorders selected from the group consisting of breast cancer, ovarian cancer, uterine cancer, endometrial cancer and endometrial hyperplasia in humans or mammals. 35. The use of a compound of formula (I) according to claim 33, wherein the malignant disease or disorder is characterized by an detectable level of 17β-HSD1 in a tumor tissue sample. 36. The use of a compound of formula (I) according to claim 33, wherein the estradiol-dependent disease is breast cancer and the mammal is a woman after menopause. 37. The use of a compound of formula (I) according to claim 33, wherein the mammal is a pre- or perimenopausal woman. 38. The use of an effective amount of a compound of formula (I) according to any one of claims 1-30 for the treatment or prevention of benign estradiol-dependent diseases or disorders selected from the group consisting of endometriosis, uterine fibrosis, uterine leiomyoma, adenomyosis, dysmenorrhea, menorrhagia, metrorrhagia and urinary dysfunction in humans or mammals. 39. The use of the compounds of formula (I) according to any one of claims 1-30 for the manufacture of medicines for the treatment and prevention of benign estradiol-dependent diseases or disorders selected from the group consisting of endometriosis, uterine fibrosis, uterine leiomyoma, adenomyosis, dysmenorrhea, menorrhagia, metrorrhagia and urinary dysfunction in humans or mammals. 40. The use of the compounds of formula (I) according to clause 37, where the mammal is a woman in pre- or perimenopause. 41. The use of an effective amount of a compound of formula (I) according to any one of claims 1-30 for the treatment or prevention of androgen-dependent diseases or disorders selected from the group consisting of prostate cancer, prostadinium, benign prostatic hyperplasia, urinary dysfunction, lower urinary syndrome pathways, prostatitis, acne, seborrhea, androgenetic alopecia, hirsutism, premature maturation, adrenal hyperplasia and polycystic ovarian syndrome in humans or mammals. 42. The use of the compounds of formula (I) according to any one of claims 1-30 for the manufacture of medicines for the treatment and prevention of androgen-dependent diseases or disorders selected from the group consisting of prostate cancer, prostadinium, benign prostatic hyperplasia, urinary dysfunction, syndrome lower urinary tract, prostatitis, acne, seborrhea, androgenetic alopecia, hirsutism, premature maturation, adrenal hyperplasia and polycystic ovarian syndrome in humans or mammals. 43. The use of an effective amount of a compound of formula (I) according to any one of claims 1-30 for the treatment or prevention of estrogen-dependent or androgen-dependent diseases or disorders requiring a decrease in the endogenous concentration of estrogens or androgens throughout the body or tissue-specific, and selected from the group consisting of squamous cell carcinoma, colon cancer, osteoporosis, rheumatoid arthritis, multiple sclerosis, myasthenia gravis, cognitive dysfunctions, senile dementia, Alzheimer's disease, thyroiditis, vasculitis, ulcerative colitis, Crohn’s disease, type I and type II diabetes, psoriasis, contact dermatitis, skin wrinkles, eczema, tissue injuries, systemic lupus erythematosus, graft versus host disease, organ failure after transplantation, cataracts and asthma in humans or mammals. 44. The use of a compound of formula (I) according to any one of claims 1-30 for the manufacture of medicines for the treatment and prevention of estrogen-dependent or androgen-dependent diseases or disorders requiring a decrease in the endogenous concentration of estrogens or androgens throughout the body or tissue-specific, and selected from the group consisting of squamous cell carcinoma, colon cancer, osteoporosis, rheumatoid arthritis, multiple sclerosis, myasthenia gravis, cognitive dysfunctions, senile dementia, Alzheimer's disease, thyroiditis, vask ulitis, ulcerative colitis, Crohn’s disease, type I and type II diabetes, psoriasis, contact dermatitis, skin wrinkles, eczema, tissue injuries, systemic lupus erythematosus, graft versus host disease, organ failure after transplantation, cataracts and asthma in humans or mammals . 45. The use of the compounds of formula (I) according to any one of claims 1-30 for the manufacture of a pharmaceutical composition for blocking spermatogenesis and / or for use as a contraceptive for men. 46. The compound of formula (I) according to any one of claims 1-30 for the treatment or prevention of malignant estradiol-dependent diseases or disorders selected from the group consisting of breast cancer, ovarian cancer, uterine cancer, endometrial cancer and endometrial hyperplasia in humans or mammals. 47. The compound of formula (I) according to item 46, where the malignant disease or disorder is characterized by a detectable level of 17β-HSD1 in a tumor tissue sample. 48. The compound of formula (I) according to item 46, where estradiol-dependent disease is breast cancer, and the mammal is a woman after menopause. 49. The compound of formula (I) according to item 46, where the mammal is a woman in pre- or perimenopause. 50. The compound of formula (I) according to any one of claims 1-30 for the treatment or prevention of benign estradiol-dependent diseases or disorders selected from the group consisting of endometriosis, uterine fibrosis, uterine leiomyoma, adenomyosis, dysmenorrhea, menorrhagia, metrorrhagia and urinary dysfunction in humans or mammals. 51. The compound of formula (I) according to claim 50, wherein the mammal is a pre- or perimenopausal woman. 52. The compound of formula (I) according to any one of claims 1-30 for the treatment or prevention of androgen-dependent diseases or disorders selected from the group consisting of prostate cancer, prostadinium, benign prostatic hyperplasia, urinary dysfunction, lower urinary tract syndrome, prostatitis , acne, seborrhea, androgenetic alopecia, hirsutism, premature ripening, adrenal hyperplasia and polycystic ovarian syndrome in humans or mammals. 53. The compound of formula (I) according to any one of claims 1 to 30 for the treatment or prevention of estrogen-dependent or androgen-dependent diseases or disorders requiring a decrease in the endogenous concentration of estrogens or androgens throughout the body or tissue-specific, and selected from the group consisting of squamous cell carcinoma, colon cancer, osteoporosis, rheumatoid arthritis, multiple sclerosis, myasthenia gravis, cognitive dysfunctions, senile dementia, Alzheimer's disease, thyroiditis, vasculitis, ulcerative colitis, Crohn’s disease, diabetes I and Type II, psoriasis, contact dermatitis, skin wrinkles, eczema, tissue injuries, systemic lupus erythematosus, graft versus host disease, organ failure after transplantation, cataracts and asthma in humans or mammals. 54. The compound of formula (I) according to any one of claims 1 to 30 for blocking spermatogenesis and / or for use as a contraceptive for men.