Immunosuppressive agents

FIELD: chemistry.

SUBSTANCE: present invention refers to compounds of Formula II and to methods of immune response suppression, e.g. by inhibition of indirect MHC type II of T-cells activation. Compounds under invention can be applied to treatment or prevention of derangements, such as rheumatoid arthritis and/or multiple sclerosis.

EFFECT: production of compounds which can be used for immune response suppression.

25 cl, 19 dwg, 4 tbl, 22 ex

 

The text descriptions are given in facsimile form.

1. The compound of formula II

where, if permitted by the valency and stability

But no;

In is a sequence of 2-6 amino acid residues or amino acid residue analogues,

where the first residue is selected from the Disc, Tic, azaTic, Thiq,

the second residue selected from G, Met, Met(O), Nle, Ile, Odapdc,

the third residue is a βPhPro or missing,

the fourth residue represents [Sψ(oxas)L] or missing,

W denotes a OR7or NR8R9;

V represents C=O,

X is absent;

R is independently in each case represents H or (C1-C6)alkyl group;

R1means (C1-C6)alkyl group;

R2means (C1-C6TSE is realtyline group, containing as the heteroatom atom S, (C3-C8)cycloalkyl(C1-C6)alkyl group, aracelio group;

i denotes an integer from 0 to 1;

j denotes an integer from 1 to 2;

k represents from 1 to 3;

R6no;

R7, R8and R9independently represent substituents selected from H and (C1-C6)alkyl, possibly substituted-HE-group or group-och2CH2HE, aralkyl, heterocyclic group, represents a 5-7 membered cycle, which includes from one to 4 heteroatoms selected from O, N or S.

2. The compound according to claim 1, characterized in that at least one of R1, R7, R8and R9denotes a hydrophobic residue.

3. The compound according to claim 1, characterized In that means 2-4 amino acid residues or residues of amino acid analogs.

4. The compound according to claim 1, characterized in that it has an immunosuppressive activity.

5. The compound according to claim 1, characterized in that it inhibits MHC-mediated activation of T cells.

6. The compound according to claim 1, characterized in that the amino acid residues are alpha-amino acid residues.

7. The compound according to claim 1, wherein R1XV together represent an acyl group.

8. The connection according to claim 7, distinguishing the I, what acyl group is alkylcarboxylic group.

9. The connection according to claim 7, characterized in that the acyl group represents a (C1-C6)alkanoyloxy group.

10. The connection according to claim 7, wherein the acyl group is an acetyl group.

11. The compound according to claim 1, selected from

Ac-Cha-Gpg-Disc-Met-βPhPro-[S(oxaz)L]-NMe2

Ac-Cha-Gpg-Disc-Met-βPhPro-[S(oxaz)L)-NMe2

Ac-Cha-Gpg-Disc-Met-βPhPro-OH

Ac-Cha-Gpg-Disc-Met-βPhPro-OH

Ac-Cha-Gpg-Tic-Met(O)-βPhPro-[S(oxaz)L]-NMe2

Ac-Phe-Gpg-Tic-Met(O)-βPhPro-[S(oxaz)L]-NMe2

Ac-Cha-Gpg-Tic-Nle-βPhPro-[S(oxaz)L]-NMe2

Ac-Cha-Gpg-Tic-Nle-βPhPro-N(Me)CH2CH2OH

Ac-Phe-Gpg-Tic-Nle-βPhPro-[S(oxaz)L]-NMe2

Ac-Phe-Gpg-Tic-Nle-βPhPro-N(Me)CH2CH2OH

Ac-Hfe-Gpg-Tic-Nle-βPhPro-[S(oxaz)L]-NMe2

Ac-Thi-Gpg-Tic-Nle-βPhPro-[S(oxaz)L]-NMe2

Ac-Cha-Gpg-Tic-IIe-βPhPro-[S(oxaz)L]-NMe2

Ac-Cha-Gpg-Tic-Met-βPhPro-[S(oxaz)L]-NMe2

Ac-Cha-Gpg-Disc-Nle-βPhPro-[S(oxaz)L]-NMe2

Ac-Cha-Gpg-Disc-Nle-βPhPro-[S(oxaz)L]-NMe2

Ac-Phe-Gpg-Disc-Met-βPhPro-[S(oxaz)L]-NMe2

Ac-Phe-Gpg-Disc-Met-βPhPro-[S(oxaz)L]-NMe2

Ac-Thi-Gpg-Disc-Met-βPhPro-[S(oxaz)L]-NMe2

Ac-Thi-Gpg-Disc-Met-βPhPro-[S(oxaz)L]-NMe2

Ac-Cha-Gpg-Disc-Met(O)-βPhPro-[S(oxaz)L]-NMe2

Ac-Thi-Gpg-Disc-Met(O)-βPhPro-[S(oxaz)L]-NMe2

Ac-Cha-Gpg-Disc-Met-NH2

Ac-Cha-Gpg-Disc-Met-NH2

Ac-Cha-Gpg-Tic-Met-NH2

Ac-Cha-Gpg-Tic-Nle-N(H)Bn

Ac-Cha-Gpg-Tic-Nle-N(H)CH2CH2Ph

Ac-Cha-Gpg-Tic-Nle-N(H)CH2CH2OCH2CH2OH

Ac-Cha-Gpg-Tic-Nle-N(Me)Bn

Ac-ha-Gpg-Disc-Nle-N(Me)Bn

Ac-Cha-Gpg-Disc-Nle-N(Me)Bn

Ac-Cha-Gpg-Tic-Nle-tetrahydroisoquinoline

Ac-Cha-Gpg-Tic-Nle-N(Bn)CH2CH2OH

Ac-Cha-Gpg-Tic-Met-βPhProNH2

Ac-Cha-Gpg-Tic-Nle-N(Bn)CH2CH2OCH2CH2OH

Ac-Cha-Gpe-Tic-Met-N(Bn)CH2CH2OCH2CH2OH

or constructed from the following subunits

td align="left"> lle
AUChaGpgAlaMetAlaSerLeu-NH2
4-aminobutyrylNbaC(Acm)Nleβ-PhProtLeu
3-aminopropyl4-MeChaC(Prm)ChgN(H)CH(CH2OH)2
SOAMePhgHaicN(CH3)CH2CH2OH
HfeC(Ac)OdapdcN(H)CH2CH2OH
PheNvaMet(O)[S-ψ(oxaz)L]-N(CH3)2
Tic[S-ψ(imid)-L]-N(CH3)2
DiscN(H)CH2tBu
ThiqD-Leu-ol
aza TicD-Pro-ol
N(H)Bn
N(CH3)Bn
N(H)CH2CH2Ph
N(CH3)CH2CH2Ph
N(CH3)CH2CH2OH
N(Bn)CH2CH2OH
Ȁ N(CH2CH2Ph)CH2CH2OH
N(H)CH2CH2OCH2CH2OH
N(Bn)CH2CH2OCH2CH2OH
N(CH2CH2Ph)CH2CH2OCH2CH2OH
tetrahydroisoquinoline
isoindoline
AUChaGpgAlaMetN(H)Bn

12. The compound according to claim 1, characterized in that it is chosen from Ac-Cha-Gpg-Tic-Met-βPhPro-[Sψ(oxaz)L]NMe2Ac-Cha-Gpg-Tic-Nle-βPhPro-[Sψ(oxaz)L]NMe2Ac-Cha-Gpg-Tic-Met(O)-βPhPro-[Sψ(oxaz)L]NMe2Ac-Cha-Gpg-Disc-Met-βPhPro-Sψ(oxaz)L]NMe2Ac-Cha-Gpg-Tic-Nle-NHCH2CH2Ph, Ac-Cha-Gpg-Disc-Met-NH2Ac-Cha-Gpg-Disc-Nle-N(Me)Bn, Ac-Cha-Gpg-Tic-Met-NH2Ac-Cha-Gpg-Tic-Nle-N(Me)Bn, Ac-Cha-Gpg-Tic-Met-βPhPro-NH2Ac-Cha-Gpg-Tic-Nle-N(Bn)CH2CH2OCH2CH OH and Ac-Cha-Gpg-Tic-Met-N(Bn)CH2CH2OCH2CH2OH.

13. The compound according to claim 1, characterized in that it binds with protein MHC class II.

14. The connection 13, characterized in that the protein MHC class II is a DR molecule.

15. The connection 13, characterized in that the protein MHC class II choose from 0401, 0101 and 0404.

16. The connection 13, characterized in that it binds with protein MHC II with the value of the IC50less than 4 μm, 2 μm, 1 μm, 500 nm or 200 nm.

17. The compound according to claim 1, which represents the Ac-Cha-Gpg-Tic-Nle-NHCH2CH2Ph.

18. The compound according to claim 1, which represents the Ac-Cha-Gpg-Tic-Nle-βPhPro-[Sψ(oxas)L]-NMe2.

19. Pharmaceutical composition having antidepressive activity containing a compound according to claim 1 and pharmaceutically acceptable excipient.

20. The use of compounds according to claim 1 for the preparation of pharmaceutical compositions for the treatment or prevention of a condition characterized by mediated MHC class II activation of T cells or protein expression of MHC class II at the site of inflammation in the pathology.

21. The application of claim 20, wherein the condition is selected from rheumatoid arthritis, juvenile arthritis, multiple sclerosis, graves ' disease, insulin-dependent diabetes, narcolepsy, psoriasis, systemic lupus erythematosus, ankylosing spondylitis, allograft rejection, rejection is transplantat, homologous illness, disease, Hashimoto's disease, myasthenia gravis, vulgar pemphigidae (vulgar bladderworts), thyroiditis, glomerulonephritis, pancreatitis, primary biliary cirrhosis, Sjogren syndrome, scleroderma, polymyositis, dermatomyositis, medical pemphigoid syndrome?, autoimmune hemolytic anemia, pernicious anemia, idiopathic thrombocytopenic purpura, insulite, irritable bowel syndrome and Addison disease.

22. The application of claim 20, wherein the condition is selected from rheumatoid arthritis and multiple sclerosis.

23. The method of suppressing the immune response, which consists in the introduction to the animal an effective amount of a compound according to claim 1.

24. The compound of the formula I

where, if permitted by the valency and stability

But no;

In is a sequence of 2-6 amino acid residues or amino acid residue analogues,

where the first residue is selected from the Disc, Tic, azaTic, Thiq,

the second residue selected from G, Met, Met(O), Nle, Ile, Odapdc,

the third residue is a βPhPro or missing,

the fourth residue represents [Sψ(oxas)L] or missing,

W denotes a OR7or NR8R9;

V represents C=O,

X is absent;

R is independently in each case represents H or (C1-C6)alkyl group;

R1means (C1-C6)alkyl group;

R2means (C1-C6)heteroalkyl group containing as the heteroatom atom S, (C3-C8)cycloalkyl(C1-C6)alkyl group, aracelio group,

R3denotes Arg or Gpg,

R7, R8and R9independently represent substituents selected from H and (C1-C6)alkyl, possibly substituted-HE-group or group-och2CH2HE, aralkyl, heterocyclic group, represents a 5-7 membered cycle, which includes from one to 4 heteroatoms selected from O, N or S,

where W includes at least 6 non-hydrogen atoms.

25. The connection point 24, characterized in that at least one of R8and R9selected from benzyl, Venetia, 2-hydroxyethyl and CH2CH2OCH2CH2OH.



 

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