Composition for the treatment and prevention of glomerulopathy, new connections in her inbox, a pharmaceutical composition for the inhibition of matrix metalloproteinases and composition for inhibition of type iv collagenases

 

Describes a composition for the treatment and prevention of glomerulopathy, including in its composition a compound of the formula I, in which R1is hydrogen, (NISS. )alkyl, optionally substituted-CONHPh or (ness.)alkylthio, phenyl, optionally substituted by hydroxy, phenyl(ness.)alkyl or indol-3-yl(NISS. )alkyl, optionally substituted (NISS. )alkoxy; R2is hydrogen or (NISS. )alkyl; R3is 1,4-phenylene or 2,5-theoffender; R4- Deputy, presents structural fragments (a-l), where R5denotes hydrogen, hydroxy, (ness.)alkyloxy, optionally substituted, dialkylamino, (NISS. )allylthiourea, halogen, (NISS. )haloalkyl, amino group, optionally substituted (ness.)the alkyl, (ness.)alkyl, optionally substituted, azido or hydroxy, nitro, cyano, acyl, -CONH2, -NHCORDwhere RD- (ness.)alkyl, morpholino; R6- phenyl, (ness.)alkyl, optionally substituted hydroxy, (NISS. )alkyloxy, (NISS. )allylthiourea, amino group, optionally substituted (ness.)the alkyl, morpholino or 1-pyrrolidinyl, and Y IS NHOH or HE, its optically active isomer, pharmaceutically acceptable salt or hydrate. It also describes the new compounds of formulae XVII, XVIII, XIX, XX, XXII and XXIII, where R1has casenformacion.com composition for the inhibition of matrix metalloproteinases and composition for inhibition of type IV collagenases. 10 S. and 27 C.p. f-crystals, 13 tab., 5 Il.



Table T%


Claims

1. Composition for treatment or prevention of glomerulopathy, which includes a compound of formula (I)

in which R1is hydrogen, (ness.)alkyl, optionally substituted-CONHPh or (ness.)alkylthio, phenyl, optionally substituted by hydroxy, phenyl (NISS. )alkyl or indol-3-yl(ness.)alkyl, optionally substituted, (ness.)alkoxy
R2is hydrogen or (ness.)alkyl;
R3is 1,4-phenylene or 2,5-theoffender;
R4Deputy formula







where R5is hydrogen, hydroxy, (ness.)alkyloxy, optionally substituted, dialkylamino, (NISS. )allylthiourea, halogen, (ness.)haloalkyl, amino group, optionally substituted (ness.)the alkyl, (ness.)alkyl. optionally substituted, azido or hydroxy, nitro, cyano, acyl.-CONH2, -NHCORDwhere RD- (ness.)alkyl, morpholino;
R6- phenyl, (NISS. )alkyl, optionally substituted hydroxy, (NISS. )alkyloxy, (NISS. )allylthiourea, amino group, optionally substituted (ness.)the alkyl, morpholino or 1-pyrrolidinyl;
Y is NHOH or HE,
its optically active isomer, pharmaceutically acceptable salt or hydrate.

2. Composition under item 1, which comprises a compound of the formula (II)

in which R1, R2and R3have the values specified above;
R7Deputy formula




or

where R8denotes hydrogen, hydroxyl, (ness.)alkyloxy, (NISS. )allylthiourea, halogen, nitro, cyano, (ness.)haloalkyl, amino group, optionally substituted (ness.)the alkyl, (alseny hydroxy, or phenyl;
Y is NHOH or HE,
its optically active isomer, pharmaceutically acceptable salt or hydrate.

3. Composition under item 1, which comprises a compound of formula (I)

in which R1, R2and R3have the values specified above;
R4Deputy formula









or

where R10is hydrogen, (ness.)alkyloxy, optionally substituted, dialkylamino, (NISS. )allylthiourea, halogen, amino, optionally substituted (NISS. )alkyl, (NISS. )alkyl, optionally substituted, azido or hydroxy, morpholino, trifluoromethyl, cyano, acetyl, -CONH2, -NHCOMe, or a nitro-group;
R11- (ness.)alkyl, optionally substituted hydroxy, (ness.)alkyloxy, (ness.)allylthiourea, amino group, optionally substituted (ness.)the alkyl, phenyl, morpholino or 1-pyrrolidino;
Y is NHOH or HE,
its optically active isomer, the />
in which R1, R2and R3have the values specified above;
R7Deputy formula





where R12is hydrogen, halogen, the nitro-group, (ness.)alkyl, optionally substituted, azido or hydroxy, (NISS. )alkyloxy, (ness.)allylthiourea, trifluoromethyl, cyano, acetyl, -CONH2or-NHCOMe;
R13- (NISS. )alkyl, optionally substituted by hydroxy, phenyl, (NISS. )alkyloxy, (NISS. )allylthiourea, amino group, optionally substituted (ness.)the alkyl, morpholino or 1-pyrrolidino;
Y is NHOH or HE,
its optically active isomer, pharmaceutically acceptable salt or hydrate.

5. Composition under item 1, which comprises a compound of the formula (III):

in which R1, R10and Y have the meanings stated above;
R14is hydrogen or (ness.)alkyl,
its optically active isomer, pharmaceutically acceptable salt or hydrate.

6. Composition under item 1, which comprises a compound of the formula (IV)

in which R1, R12

7. Composition under item 1, which comprises a compound of the formula (V)

in which R1, R10, R14and Y have the meanings mentioned above,
its optically active isomer, pharmaceutically acceptable salt or hydrate.

8. Composition under item 1, which comprises a compound of the formula (VI)

in which R1, R12, R14and Y have the meanings mentioned above,
its optically active isomer, pharmaceutically acceptable salt or hydrate.

9. Composition under item 1, which comprises a compound of the formula (VII)

in which R1, R10, R14and Y have the meanings mentioned above,
its optically active isomer, pharmaceutically acceptable salt or hydrate.

10. Composition under item 1, which comprises a compound of the formula (VIII):

in which R1, R12, R14and Y have the meanings mentioned above,
its optically active isomer, pharmaceutically acceptable salt or hydrate.

11. Composition under item 1, which comprises a compound of the formula (IX)

in which R1, R10, R14and Y have the meanings mentioned above,
his opet compound of formula (X)

in which R1, R12, R14and Y have the meanings mentioned above,
its optically active isomer, pharmaceutically acceptable salt or hydrate.

13. Composition under item 1, which comprises a compound of the formula (XI):

in which R1, R10, R14and Y have the meanings stated above, its optically active isomer, pharmaceutically acceptable salt or hydrate.

14. Composition under item 1, which comprises a compound of the formula (XII)

in which R1, R12, R14and Y have the meanings mentioned above,
its optically active isomer, pharmaceutically acceptable salt or hydrate.

15. Composition under item 1, which comprises a compound of the formula (XIII)

in which R1, R11, R14and Y have the meanings mentioned above,
its optically active isomer, pharmaceutically acceptable salt or hydrate.

16. Composition under item 1, which comprises a compound of the formula (XIV)

in which R1, R13, R14and Y have the meanings mentioned above,
its optically active isomer, pharmaceutically acceptable salt or gerarai R1, R11, R14and Y have the meanings mentioned above,
its optically active isomer, pharmaceutically acceptable salt or hydrate.

18. Composition under item 1, which comprises a compound of the formula (XVI)

in which R1, R13, R14and Y have the meanings mentioned above,
its optically active isomer, pharmaceutically acceptable salt or hydrate.

19. Composition according to any one of paragraphs.1-18, where R1is hydrogen, methyl, isopropyl, isobutyl, benzyl, indol-3-ylmethyl, optionally substituted (NISS. )alkyloxy, or phenylenecarbonyl.

20. Composition according to any one of paragraphs.1-18, where R1- isopropyl, benzyl or indole-3-ylmethyl.

21. Composition according to any one of paragraphs.1-20, where R2and R14- hydrogen atoms.

22. Composition according to any one of paragraphs.1-21, where Y IS HE.

23. Composition according to any one of paragraphs.1-22, where glomerulopathy is a glomerulonephritis.

24. Composition according to any one of paragraphs.1-22, where glomerulopathy is a diabetic nephropathy.

25. The compound of formula (XVII)

in which R1- (ness.)alkyl or phenyl(ness.)alkyl;
R10halogen or (ness.)alkyl;
R14is hydrogen;
Y is hydroxy,
egmd src="https://img.russianpatents.com/img_data/61/616011.gif">
in which R1- (ness.)alkyl;
R10- (ness.)alkyl;
R14is hydrogen;
Y is hydroxy,
its optically active isomer, pharmaceutically acceptable salt or hydrate.

27. The compound of formula (XIX)

in which R1- (ness.)alkyl;
R10is hydrogen;
R14is hydrogen;
Y is hydroxy,
its optically active isomer, pharmaceutically acceptable salt or hydrate.

28. The compound of formula (XX)

in which R1is hydrogen, (ness.)alkyl, phenyl(ness.)alkyl, indol-3-yl(ness.)alkyl;
R10is hydrogen, (ness.)alkyl, halogen (ness.)alkyl, (ness.)alkoxy, halogen, (ness.)allylthiourea or amino group, substituted (ness.)by alkyl;
R14is hydrogen;
Y is hydroxy,
its optically active isomer, pharmaceutically acceptable salt or hydrate.

29. The compound of formula (XXII)

in which R1- phenyl(ness.)alkyl;
R10- (ness.)alkyl;
R14is hydrogen;
Y is hydroxy,
its optically active isomer, pharmaceutically acceptable salt or hydrate.

30. The compound of formula (XXIII)

in which R1- (ness.)alkyl;
R10

31. Pharmaceutical composition for the inhibition of matrix metalloproteinases, including the compound according to any one of paragraphs.25-30.

32. Composition for the inhibition of type IV collagenases, including the compound according to any one of paragraphs.25-30.

33. Composition for treatment or prevention of glomerulopathy, which comprises a compound according to any one of paragraphs.25-30.

34. Composition under item 1, which comprises a compound of the formula (XXIV)

the combination of all of the substituents which are presented in table 1, its optically active isomer, pharmaceutically acceptable salt or hydrate: (see graphic part).

35. Composition under item 1, which comprises a compound of the formula (XXIV)

the combination of all of the substituents which are presented in table 2, its optically active isomer, pharmaceutically acceptable salt or hydrate: (see graphic part).

36. Composition according to any one of paragraphs.33-35, where glomerulopathy is a glomerulonephritis.

37. Composition according to any one of paragraphs.33-35, where glomerulopathy is a diabetic nephropathy.

 

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