Heterocycles as inhibitors of leukocyte adhesion and vla - 4 antagonists

 

The invention relates to means for inhibiting the adhesion or migration of cells, or inhibition of VLA-4 receptor, representing the heterocycles of General formula (I), where W means R1-A-C (R13), Y represents carbonyl, Z denotes N(R0), And means a divalent residue of phenylene, divalent (C1-C6)-alkalinity balance, means the divalent (C1-C6)-alkalinity residue which may be substituted (C1-C8)-alkyl, D is C(R2) (R3), E mean R10CO., R and R0independently of one another denote hydrogen, if necessary substituted (C6-C14)-aryl, if necessary substituted heteroaryl, if necessary substituted in the aryl residue (C6-C14)-aryl-(C1-C6)-alkyl or, if necessary, substituted in the heteroaryl residue heteroaryl-(C1-C6)-alkyl, R1means hydrogen, Gets the remainder R28N (R21)-C(O)-, R2means hydrogen, R3means CONHR4, R11NH, R4means (C1-C28)-alkyl, which optionally may be single - or multi-substituted by identical or different residues selected from tifa substituted (C6-C14)-aryl, R10means hydroxyl or (C1-C6)-alkoxy, R11means R12CO., R12means R15-O-, R13means (C1-C6)-alkyl, R15means R16-(C1-C6)-alkyl, R16means 7-12-membered bicyclic or tricyclic residue, a saturated or partially unsaturated and which may be substituted by one or more identical or different (C1-C4)-alkyl residues, R21means hydrogen, R28means R21, Het denotes a mono - or polycyclic, 4-14-membered, aromatic or non-aromatic cycle, which may contain 1, 2, 3 or 4 nitrogen atom, b, C, d and f independently of one another denote 0 or 1, but at the same time may not mean zero, e, g and h independently of one another denote 0, 1, 2, 3, 4, 5 or 6, in all their stereoisomeric forms and mixtures thereof in any ratio, and their physiologically acceptable salts. Also described pharmaceutical preparations containing the compounds according to the invention. 7 C. and 30 C. p. F.-ly, 1 PL.

Description text in facsimile form (see graphic material)

Forms is Ceptor, representing the heterocycles of General formula (I)

where W stands for R1-A-C(R13);

Y represents a carbonyl;

Z means N(R0);

A represents the bivalent residue of phenylene, divalent (C1-C6)-alkalinity balances;

In the mean bivalent (C1-C6)-alkalinity residue which may be substituted (C1-C8)-alkyl;

D means C(R2)(R3);

E. means R10CO;

R and R0, independently of one another, mean hydrogen, if necessary substituted (C6-C14)-aryl, if necessary substituted heteroaryl, if necessary substituted in the aryl residue (C6-C14)-aryl-(C1-C6)-alkyl or, if necessary, substituted in the heteroaryl residue heteroaryl-(C1-C6)-alkyl;

R1means hydrogen, Gets the remainder R28N(R21)-C(O)-;

R2means hydrogen;

R3means CONHR4, R11NH;

R4means (C1-C28)-alkyl, which optionally may be single - or multi-substituted by identical or different residues selected from the range of hydroxycarbonyl, (C1-C6-alcox is sup>10means hydroxyl or (C1-C6)-alkoxy;

R11means R12CO;

R12means R15-O-;

R13means (C1-C6)-alkyl;

R15means R26-(C1-C6)-alkyl;

R16means 7-12-membered bicyclic or tricyclic residue, a saturated or partially unsaturated and which may be substituted by one or more identical or different (C1-C4)-alkyl residues;

R21means hydrogen;

R28means R21;

Het denotes a mono - or polycyclic, 4-14-membered, aromatic or non-aromatic cycle, which may contain 1, 2, 3 or 4 nitrogen atom;

b, C, d and f, independently of one another, denote 0 or 1, but cannot mean zero;

e, g and h, independently of one another, mean 0, 1, 2, 3, 4, 5 or 6, in all their stereoisomeric forms and mixtures thereof in any ratio,

and their physiologically acceptable salts.

2. Means under item 1, wherein in the formula (I) W implies R1-A-C(R13), Y represents carbonyl, Z denotes N(R0), And means a divalent residue of a number consisting of methylene, ethylene, trimethylene, tetramethylene, pentamethylene, substituted methylene or ethylene, of phenylene, E mean R10CO., R means hydrogen or benzyl, R0means, if necessary, substituted (C6-C14)-aryl, if necessary substituted in the aryl residue (C6-C14)-aryl-(C1-C6)-alkyl, R1means the residue R28N (R21) -C(O)-, R3means CONHR4, R11NH, e, g and h, independently of one another, denote 0, 1, 2 or 3, in all their stereoisomeric forms and mixtures thereof in any ratio, and their physiologically acceptable salts.

3. Means under item 1 or 2, characterized in that in formula (I) W implies R1-A-C(R13), Y represents carbonyl, Z denotes N(R0), And means ethylene, trimethylene, tetramethylene, pentamethylene, phenylene, means unsubstituted or substituted methylene residue, D is C(R2) (R3), E mean R10CO., R is hydrogen, R0means, if necessary, substituted (C6-C14)-aryl, if necessary substituted in the aryl residue (C6-C14)-aryl-(C1-C6)-alkyl, R1means the residue R28N(R21)-C(O)-, R2means hydrogen, R3means CONHR4, R4means methyl, which is substituted by hydroxycarbonyl or(C110means hydroxyl or (C1-C6)-alkoxy, preferably (C1-C4)-alkoxy, R13means (C1-C6)-alkyl, in particular methyl, b, C and d mean 1, e, f and g denote 0, h is 1 or 2, preferably 1, in all their stereoisomeric forms and mixtures thereof in any ratio, and their physiologically acceptable salts.

4. Means under item 1 or 2, characterized in that in formula (I) W implies R1-A-C (R13), Y represents carbonyl, Z denotes N(R0), And means ethylene, trimethylene, tetramethylene, pentamethylene, phenylene, means unsubstituted or substituted methylene residue, D is C(R2) (R3), E mean R10CO., R is hydrogen, R0means, if necessary, substituted (C6-C14)-aryl, if necessary substituted in the aryl residue (C6-C14)-aryl-(C1-C6)-alkyl, R1means the residue R28N (R21)-C(O)-, R2means hydrogen, R3means R11NH, R10means hydroxyl or (C1-C6)-alkoxy, preferably (C1-C4)-alkoxy, R13means (C1-C6)-alkyl, in particular methyl, b, C, d and e mean 1, f and g denote 0, h 0 means, at all.

5. Tool according to one or more paragraphs.1-4, characterized in that suitable for the production of pharmaceuticals for inhibition of inflammation.

6. Tool according to one or more paragraphs.1-4, characterized in that suitable for the production of pharmaceuticals for the treatment and prevention of rheumatoid arthritis, inflammatory diseases of the digestive tract, systemic lupus erythematosus or inflammatory diseases of the Central nervous system.

7. Tool according to one or more paragraphs.1-4, characterized in that suitable for the production of pharmaceuticals for the treatment and prevention of asthma and allergies.

8. Tool according to one or more paragraphs.1-4, characterized in that suitable for the production of pharmaceuticals for the treatment and prevention of cardiovascular diseases, arteriosclerosis, restenosis or diabetes, to prevent damage to transplants of organs, to suppress tumor growth or metastasis of tumors or to treat malaria.

9. Tool according to one or more paragraphs.1-4, characterized in that suitable for the treatment and prevention of diseases in which the adhesion and/or migration of leukocytes in undesirable scale, or diseases, when Kotelnich diseases of the digestive tract, systemic lupus erythematosus, inflammatory diseases of the Central nervous system, asthma, allergies, cardiovascular diseases, arteriosclerosis, restenosis, diabetes, to prevent damage to transplants of organs, to inhibit the growth or metastasis of tumors, to treat malaria or as inhibiting inflammation funds.

10. The heterocycles of the formula (Ib)

where W stands for R1-A-C(R13);

Y represents a carbonyl;

A represents phenylene;

In means (C1-C6-alkylen;

D means C(R2)(R3);

E mean R10CO;

R and R0, independently of one another, mean hydrogen, if necessary substituted (C6-C14)-aryl, if necessary substituted heteroaryl, if necessary substituted in the aryl residue (C6-C14)-aryl-(C1-C6)-alkyl or, if necessary, substituted in the heteroaryl residue heteroaryl-(C1-C6)-alkyl;

R1means the residue R28N(R21)-C(O)-;

R2means hydrogen;

R3means CONHR4;

R4means (C1-C28)-alkyl, which may optionally be one or many of the ub>)-alkoxycarbonyl and R5;

R5means, if necessary, substituted (C6-C14)-aryl;

R10means hydroxyl and (C1-C6)-alkoxy;

R13means (C1-C6)-alkyl;

R21means hydrogen;

R28means R21;

b, C, d and f, independently of one another, denote 0 or 1, but cannot mean zero;

e, g and h, independently of one another, mean 0, 1, 2, 3, 4, 5 or 6, in all their stereoisomeric forms and mixtures thereof in any ratio,

and their physiologically acceptable salts.

11. The heterocycles of the formula (Ib) under item 10 and/or their physiologically acceptable salts are used as medicines.

12. The heterocycles of the formula (Ib) under item 10, suitable for inhibiting the adhesion or migration of cells or inhibition of VLA-4 receptor.

13. The heterocycles of the formula (Ib) under item 10, suitable for the production of pharmaceuticals for inhibition of inflammation.

14. The heterocycles of the formula (Ib) under item 10, suitable for medicinal products for treatment and prevention of rheumatoid arthritis, inflammatory diseases of the digestive tract, systemic lupus erythematosus or inflammatory diseases Centralia treatment and prevention of asthma and allergies.

16. The heterocycles of the formula (Ib) under item 10, suitable for the production of pharmaceuticals for the treatment and prevention of cardiovascular diseases, arteriosclerosis, restenosis or diabetes, to prevent damage to transplants of organs, to suppress tumor growth or metastasis of tumors or to treat malaria.

17. The heterocycles of the formula (Ib) under item 10, suitable for the treatment and prevention of diseases in which the adhesion and/or migration of leukocytes in undesirable scale, or diseases in which play the role of VLA-4-dependent adhesion processes for the treatment or prevention of rheumatoid arthritis, inflammatory diseases of the digestive tract, systemic lupus erythematosus, inflammatory diseases of the Central nervous system, asthma, allergies, cardiovascular diseases, arteriosclerosis, restenosis, diabetes, to prevent damage to transplants of organs, to inhibit the growth or metastasis of tumors, for the treatment of malaria or as inhibiting inflammation funds.

18. Pharmaceutical drug-based active agents and conventional additives, which are able to inhibit the adhesion and migration of leukocytes characterized Biologicheskie acceptable salt in an effective amount along with pharmaceutically acceptable carriers and/or additives.

19. The heterocycles of the formula (IC)

where W stands for R1-A-C(R13);

Y represents a carbonyl;

Z means N(R0);

A represents the bivalent (C1-C6)-alkalinity balances;

In means the divalent residue (C1-C6)-alkylene;

D means C(R2)(R3);

E. means R10CO;

R and R0, independently of one another, mean hydrogen, if necessary substituted (C6-C14)-aryl, if necessary substituted heteroaryl, if necessary substituted in the aryl residue (C6-C14)-aryl-(C1-C6)-alkyl or, if necessary, substituted in the heteroaryl residue heteroaryl-(C1-C6) -alkyl;

R1means hydrogen;

R2means hydrogen;

R3means CONHR4;

R4means (C1-C28)-alkyl, which optionally may be single - or multi-substituted by identical or different residues selected from the range of hydroxycarbonyl, (C1-C6)-alkoxycarbonyl and R5;

R5means, if necessary, substituted (C6-C14)-aryl;

R10means hydroxyl and (C1-C6)-1, however, at the same time may not mean zero;

e, g and h, independently of one another, mean 0, 1, 2, 3, 4, 5 or 6, in all their stereoisomeric forms and mixtures thereof in any ratio,

and their physiologically acceptable salts.

20. The heterocycles of the formula (IC) on p. 19 and/or their physiologically acceptable salts are used as medicines.

21. The heterocycles of the formula (IC) according to p. 19, suitable for inhibiting the adhesion or migration of cells or inhibition of VLA-4 receptor.

22. The heterocycles of the formula (IC) according to p. 19, suitable for the production of pharmaceuticals for inhibition of inflammation.

23. The heterocycles of the formula (IC) according to p. 19, suitable for medicinal products for treatment and prevention of rheumatoid arthritis, inflammatory diseases of the digestive tract, systemic lupus erythematosus or inflammatory diseases of the Central nervous system.

24. The heterocycles of the formula (IC) according to p. 19, suitable for medicinal products for treatment and prevention of asthma and allergies.

25. The heterocycles of the formula (IC) according to p. 19, suitable for medicinal products for treatment and prevention of cardiovascular diseases, arteriosclerosis, restenosis or diabetes who ia tumors or to treat malaria.

26. The heterocycles of the formula (IC) according to p. 19, suitable for the treatment and prevention of diseases in which the adhesion and/or migration of leukocytes in undesirable scale, or diseases in which play the role of VLA-4-dependent adhesion processes for the treatment or prevention of rheumatoid arthritis, inflammatory diseases of the digestive tract, systemic lupus erythematosus, inflammatory diseases of the Central nervous system, asthma, allergies, cardiovascular diseases, arteriosclerosis, restenosis, diabetes, to prevent damage to transplants of organs, to inhibit the growth or metastasis of tumors, for the treatment of malaria or as inhibiting inflammation funds.

27. Pharmaceutical drug-based active agents and conventional additives, which are able to inhibit the adhesion and migration of leukocytes, characterized in that the active substance it contains one or more compounds of formula (IC) on p. 19 and/or their physiologically acceptable salts in an effective amount along with pharmaceutically acceptable carriers and/or additives.

28. The heterocycles of the formula (Id)

where W stands for R1-A-C(R131
-C6)-alkalinity residue, which is substituted by (C1-C8)-alkyl;

D means C(R2)(R3);

E. means R10CO;

R means hydrogen;

R0means, if necessary, substituted (C6-C14)-aryl, if necessary substituted heteroaryl, if necessary substituted in the aryl residue (C6-C14)-aryl-(C1-C6)-alkyl or, if necessary, substituted in the heteroaryl residue heteroaryl-(C1-C6)-alkyl;

R1means hydrogen, the remainder Gets, R28N (R21)-C(O)-;

R2means hydrogen;

R3means CONHR4;

R4means (C1-C28)-alkyl, which optionally may be single - or multi-substituted by identical or different residues selected from the range of hydroxycarbonyl, (C1-C6)-alkoxycarbonyl and R5;

R5means, if necessary, substituted (C6-C14)-aryl;

R10means hydroxyl and (C1-C6)-alkoxy;

R13means (C1-C6)-alkyl;

R21means hydrogen;

R28means R21;

Het denotes a mono - or polycyclic, 4-14-membered, aromatizes the ha, mean 0 or 1, but cannot mean zero;

l, g and h, independently of one another, mean 0, 1, 2, 3, 4, 5 or 6, in all their stereoisomeric forms and mixtures thereof in any ratio,

and their physiologically acceptable salts.

29. The heterocycles of the formula (Id) on p. 28, where W means R1-A-C(R13);

Y represents a carbonyl;

Z means N(R0);

A represents the bivalent residue of the phenylene;

In the mean divalent methylene or ethylene residue, which is substituted by (C1-C8)-alkyl;

D means C(R2)(R3);

E. means R10CO;

R means hydrogen;

R0means, if necessary, substituted (C6-C14)-aryl, if necessary substituted heteroaryl, if necessary substituted in the aryl residue (C6-C14)-aryl-(C1-C6)-alkyl or, if necessary, substituted in the heteroaryl residue heteroaryl-(C1-C6)-alkyl;

R1means R28N(R21)-C(O)-;

R2means hydrogen;

R3means CONHR4;

R4means (C1-C10)-alkyl, which optionally may be single - or multi-substituted by identical or different OS's will appoints, if necessary, substituted (C6-C14)-aryl;

R10means hydroxyl and (C1-C6)-alkoxy;

R13means (C1-C4)-alkyl;

C, d mean 1;

f denotes 0;

e, h, independently of one another, denote 0 or 1;

g is 0, in all their stereoisomeric forms and mixtures thereof in any ratio,

and their physiologically acceptable salts.

30. The heterocycles of the formula (Id) on p. 28 or 29 and/or their physiologically acceptable salts are used as medicines.

31. The heterocycles of the formula (Id) on p. 28 or 29, suitable for inhibiting the adhesion or migration of cells or inhibition of VLA-4 receptor.

32. The heterocycles of the formula (Id) on p. 28 or 29, suitable for the production of pharmaceuticals for inhibition of inflammation.

33. The heterocycles of the formula (Id) on p. 28 or 29, suitable for medicinal products for treatment and prevention of rheumatoid arthritis, inflammatory diseases of the digestive tract, systemic lupus erythematosus or inflammatory diseases of the Central nervous system.

34. The heterocycles of the formula (Id) on p. 28 or 29, suitable for medicinal products for treatment and prevention of asthma and allergies.

35. The heterocycles of the formula (Id) on p. 28 Ivany, arteriosclerosis, restenosis or diabetes, to prevent damage to transplants of organs, to suppress tumor growth or metastasis of tumors or to treat malaria.

36. The heterocycles of the formula (Id) on p. 28 or 29, suitable for the treatment and prevention of diseases in which the adhesion and/or migration of leukocytes in undesirable scale, or diseases in which play the role of VLA-4-dependent adhesion processes for the treatment or prevention of rheumatoid arthritis, inflammatory diseases of the digestive tract, systemic lupus erythematosus, inflammatory diseases of the Central nervous system, asthma, allergies, cardiovascular diseases, arteriosclerosis, restenosis, diabetes, to prevent damage to transplants of organs, to inhibit the growth or metastasis of tumors, for the treatment of malaria or as inhibiting inflammation funds.

37. Pharmaceutical drug-based active agents and conventional additives, which are able to inhibit the adhesion and migration of leukocytes, characterized in that the active substance it contains one or more compounds of formula (Id) on p. 28 or 29 and/or their physiologically acceptable with the

 

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