Labeled analogues of glutamine and lysine

 

The invention relates to compounds of the formula Y-(CR2)n-X-NHJ, where X represents C=O or CR2; n is an integer having a value of from 1 to 6; Y is an L(A)mor R1R2CR-, where L - metallocomplexes agent, And represents-CR2-, -NRCO-, -CONR - or polyalkyleneglycol; m is an integer having a value of from 0 to 10, where one of R1and R2is-NH(B)pZ1and the other is-CO(B)qZ2where p and q are integers having a value of from 0 to 20, and each independently selected from Q or amino acid residue, where Q is a cyclic peptide; Z1and Z2- protective groups which are biocompatible group which inhibits or suppresses the metabolism of the peptide in vivo; J and each R group is independently selected from H, C1-4the alkyl or C1-4alkoxyalkyl; provided that (i) the total number of amino acid residues in R1and R2the group does not exceed 20; (ii) if X is CR2then Y is-CRR1R2and Z2is metallocomplexes agent; (ii) if Y is-CRR1R2then at least one of R1and R2carries at least one detective obtaining compounds, slightly affected by metabolism in vivo. The compounds are useful for the diagnosis of thrombosis, embolism, atherosclerosis, infections or cancer. Also described metal complex comprising compounds according to the invention, the set of its receipt, preparation for the introduction of a man and a peptide fragment including metallocomplexes agent. 5 C. and 13 C.p. f-crystals, 6 tab., 2 Il.

Description text in facsimile form (see graphic part). TC

Claims

1. The compound of the formula Y-(CR2)n-X-NHJ, where X represents C= O or CR2; n is an integer having a value of from 1 to 6; Y is an L(A)mor R1R2CR-, where L - metallocomplexes agent, And represents-CR2-, -NRCO-, -CONR - or polyalkyleneglycol, m is an integer having a value of from 0 to 10, one of R1and R2is-NH(B)pZ1and the other is-CO(B)qZ2where p and q are integers having a value of from 0 to 20, each independently selected from Q or amino acid residue, where Q is a cyclic peptide, Z1and Z2- protective groups which are biocompatible groups, kotelkina, With1-4alkoxyalkyl; provided that (i) the total number of amino acid residues in R1and R2the group is not more than 20, (ii) if X is CR2then Y is-CRR1R2and Z2is metallocomplexes agent, (iii) if Y is-CRR1R2then, at least one of R1and R2carries at least one detektiruya particle.

2. Connection on p. 1, where R1or R2include one or more peptide fragments2-antiplasmin, fibronectin,-casein, tetanus protein, amyloid, trappin and residues polyglutamine, and these peptide fragments contain at least three amino acid residue.

3. Connection on p. 2, where the peptide fragment is a fragment2-antiplasmin.

4. Connection on p. 3, where the amino acid in position 2 of the N-Terminus of the peptide is glutamine.

5. Connection PP. 1-4, where J is N.

6. Connection under item 5 of the formula Y-(CR2)x-(CH2)2CONH2or Y-(CR2)y-(CH2)4NH2where x is an integer having a value of from 0 to 4, y is an integer having a value of 0 is, the de at least one of the Z1and Z2is metallocomplexes agent.

9. Connection on p. 8, where Z1is metallocomplexes agent, and Z2is not metallocomplexes agent.

10. The compound according to any one of paragraphs. 1-9 for use in the diagnosis of places thrombosis or embolism.

11. Metal complex compounds on p. 8 or 9.

12. The metal complex according to p. 11, where the metal is a radioactive metal.

13. Radiotelescopes under item 12, where the radioactive metal is99mTS.

14. The metal complex according to any one of paragraphs. 11-13 for use in the diagnosis of places thrombosis or embolism.

15. Preparation for the introduction of man and acting as a substrate for the enzyme factor XIIIa containing compound according to any one of paragraphs. 1-9 or metal complex on PP. 11-13.

16. The set containing the compound according to any one of paragraphs. 1-9, useful to obtain a metal complex according to any one of paragraphs. 11-13.

17. Peptide fragment2-antiplasmin, fibronectin,-casein, tetanus protein, amyloid, trappin and polyglutamine, and the specified peptide fragment contains at least 3-20 amino acid residue and transfers plexopathy agent is located at the C-end.

 

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