Thiosulfonate compound as an inhibitor of matrix metalloprotease and methods of treatment

 

The invention relates to thiosulfonate compounds of General formula Ia, which can be used as inhibitors of the matrix metalloprotease-13 (MMP-13). In the formula Ia, R1is a substituted phenyl, R2and R3represent a radical selected from the group consisting of a hydrogen atom, a C1-C6of alkyl, aralkyl with one ring having 1-3 carbon atoms in the alkyl chain, or R2and R6together with the carbon atoms to which they are linked, form a 5 - or 6-membered ring; R6represents a radical selected from the group consisting of C1-C6of alkyl, carboxyl, C1-C6alkoxycarbonyl. The invention also relates to methods for treating pathological conditions associated with abnormal activity of the matrix metalloprotease related to MMP-13. 5 C. and 15 C.p. f-crystals, 51 PL.

Description text in facsimile form (see graphic part)

Claims

1. Thiosulfonate compounds of General formula (Ia)

where R1represents phenyl, substituted R11, R11the a-position C1-C4alkoxy;

R2and R3are radicals independently selected from the group consisting of hydrogen, C1-C6of alkyl, aralkyl with one ring having 1-3 carbon atoms in the alkyl chain, or

R2and R6together with the carbon atoms to which they are linked, form a 5 - or 6-membered ring;

R6represents a radical selected from the group consisting of C1-C6of alkyl, carboxyl, C1-C6alkoxycarbonyl,

as an inhibitor of matrix metalloprotease.

2. Connection on p. 1, where R1represents phenyl, substituted C1-C6alkoxy, phenoxy or thiophenoxy.

3. Connection on p. 1, where R1represents phenyl substituted in position 4 C1-C6alkoxy, phenoxy or thiophenoxy.

4. Connection on p. 1, where R1represents phenyl, substituted R11in position 4, a R11is phenoxy, which itself is substituted in the meta - or para-positions of the C1-C4alkoxy.

5. Thiosulfonate compounds of General formula (Ib):

where PhR11represents phenyl, substituted R11in position 4;

R11is C1-C6al alkoxygroup;

R2represents a radical selected from the group consisting of a hydrogen atom, a C1-C6of alkyl, aralkyl with one ring having 1-3 carbon atoms in the alkyl chain, or

R2and R6together with the carbon atoms to which they are linked, form a 5 - or 6-membered ring;

R6represents a radical selected from the group consisting of C1-C6alkoxycarbonyl;

R2and R6are hydrogen atoms, if R2and R6together with the carbon atoms to which they are linked, form a 5 - or 6-membered ring, as an inhibitor of matrix metalloprotease type MMP-13.

6. Connection on p. 5, in which R11selected from the group consisting of phenoxy, thiophenoxy, where phenoxy, thiophenoxy substituted in the meta - or para-positions of the C1-C4alkoxy.

7. Connection on p. 6, in which R11represents phenoxy, substituted in the para-position of the C1-C7alkoxy.

8. Thiosulfonate compounds of General formula (IVa) or (Va):

where R1represents phenyl, substituted R11, R11is C1-C6alkoxy, phenoxy or thiophenoxy, Cora matrix metalloprotease type MMP-13.

9. Connection on p. 8, in which R1represents phenyl, substituted R11in position 4, and where R11selected from the group consisting of C1-C6alkoxy, phenoxy, thiophenoxy.

10. Connection on p. 8, in which R1represents phenyl, substituted R11in position 4, and R11selected from the group consisting of C1-C6alkoxy, phenoxy, thiophenoxy, where phenoxy or thiophenoxy substituted in meta or paraprotex C1-C4alkoxy.

11. A method of treating a mammal having a condition associated with pathological activity of the matrix of metalloprotease type MMP-13 by introducing to a mammal the compound or its pharmaceutically acceptable salt in an effective amount and a specified compound corresponds to the formula

where R1represents phenyl, substituted R11,

R11is C1-C6alkoxy, phenoxy or thiophenoxy, which can be substituted in the meta - or para-position C1-C4alkoxy;

R2and R3are radicals independently selected from the group consisting of hydrogen, C1-C6of alkyl, aralkyl with one ring having 1-3 asresult 5 - or 6-membered ring;

R6represents a radical selected from the group consisting of C1-C6of alkyl, carboxyl, C1-C6alkoxycarbonyl.

12. The method according to p. 11, where the condition associated with pathological activity of the matrix of metalloprotease type MMP-13, selected from the group consisting of osteoarthritis and angiogenesis.

13. The method according to p. 11, where R1is phenyl, substituted in position 4 by a Deputy selected from the group consisting of C1-C6alkoxy, phenoxy, thiophenoxy.

14. The method according to p. 11, where R1represents phenyl, substituted R11in position 4, and R11represents phenoxy substituted in the meta - or para-positions of the C1-C6alkoxy.

15. A method of treating a mammal having a condition associated with pathological activity of the matrix of metalloprotease type MMP-13, by introducing to a mammal the compound or its pharmaceutically acceptable salt in an effective amount and a specified compound corresponds to the formula

where PhR11represents phenyl, substituted R11in position 4;

R11is C1-C6alkoxy, phenoxy or thiophenoxy, which may be samewe is isimo selected from the group consisting of a hydrogen atom, a C1-C6of alkyl, aralkyl with one ring having 1-3 carbon atoms in the alkyl chain, or

R2and R6together with the carbon atoms to which they are linked, form a 5 - or 6-membered ring;

R6represents a radical selected from the group consisting of C1-C6alkoxycarbonyl;

R2and R6are hydrogen atoms, if R2and R6together with the carbon atoms to which they are linked, form a 5 - or 6-membered ring.

16. The method according to p. 15, where the condition associated with pathological activity of the matrix of metalloprotease type MMP-13, selected from the group consisting of osteoarthritis and angiogenesis.

17. The method according to p. 16, where R11is C1-C6alkoxy, phenoxy or thiophenoxy substituted in the meta - or para-position C1-C4alkoxygroup.

18. The method according to p. 16, where R11represents phenoxy and substituted in the para-position of the C1-C4alkoxy.

19. The method according to p. 11, where the condition associated with pathological activity of the matrix of metalloprotease is angiogenesis.

20. The method according to p. 15, where the condition associated with pathological activity of the matrix of metalloprotease is angiogen

 

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