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Peptide derivatives
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A technology for peptide derivatives and compounds, applied in the field of new peptide derivatives, can solve problems such as toxicity
Inactive Publication Date: 2003-12-10
ZENECA LTD
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Often these drugs are generally cytotoxic compounds that have limited potency and can cause serious toxicity problems
Method used
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Embodiment 3
[0074] Example 3 (SEQ ID NO: 6)
Embodiment 6
[0076] Another aspect of the invention includes protected (for example with Fmoc) or unprotected amino acids of formula II, wherein n, X, R 1 and R 2 Any useful group having the above definition, including specific and preferred useful groups.
[0077] For peptide derivatives with sufficient basicity, e.g., with free amino groups, pharmaceutically acceptable salts thereof include, for example, salts with acids that form physiologically acceptable anions, such as salts with inorganic acids, The inorganic acids are, for example, hydrogen halides such as hydrogenchloride and hydrogenbromide, sulfonic acids, and phosphonic acids; and salts with organic acids such as acetic acid, oxalic acid, tartaric acid, mandelic acid, p-toluenesulfonic acid, Methanesulfonic acid, trifluoroacetic acid, etc., and for sufficiently acidic peptide derivatives, such as peptide derivatives with free carboxylic acid groups, their pharmaceutically acceptable salts include, for example, the formation ...
Embodiment 2
[0146] Fmoc-Pip-OH: NMR (DMSO-d 6 )1.3(m, 2H), 1.7(m, 2H), 2.5(m, 2H), 2.9(t, 2H), 3.7(m, 1H), 4.2(t, 1H), 4.4(d, 2H), 7.4 (m, 4H), 7.7 (d, 2H), 7.9 (d, 2H); mass spectrum m / e (ES + )352.2 (MH + ) Example 2 Preparation of Phv-II-Ala-Ala-Lys-Val-Ala-Ala-Ala-Pip-NH 2 (SEQ ID NO: 2) (Formula II: n=1; X=carbonyl; R 1 = R 2 =-CH 2 CH 2 OCH 2 CH 2 OCH 2 CH 2 OCH 3 )
[0147] Using a method similar to that described in Example 1.2, by adding Fmoc-Lys(Boc)-OH (468mg, 1mmole), Fmoc-Ala-OH (311mg, 1mmole), Fmoc-Ala-OH (311mg, 1mmole), Fmoc -Asp(PE)-OH (323 mg, 0.5 mmole) and 5-phenylpentanoic acid (178 mg, 1 mmole) were coupled sequentially (manually) to Fmoc-Val-Ala-Ala-Ala-Pip-NH-resin (manually The synthesis was carried out on ) obtained by coupling. Using conditions similar to those described in Example 1, the peptide was cleaved from the resin and the crude product was purified. The product was identified by HPLC, mass spectrometry and amino acid analysis as follow...
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Abstract
Novel peptide derivatives, pharmaceutically acceptable salts thereof and pharmaceutical compositions containing then are useful in treating MHC class II dependent T-cell method autoimmune or inflammatory diseases, such as rheumatoid arthritis.
Description
Technical field: [0001] The present invention relates to certain novel peptide derivatives having pharmacologically useful properties useful in the treatment of autoimmune diseases or medical disorders such as rheumatoid arthritis and other MHC class II dependent T cell mediated diseases. The present invention also includes pharmaceutical compositions of said novel peptide derivatives, processes for their production and their use in the treatment of one or more of the aforementioned diseases or medical disorders and in the production of novel medicaments for such medical treatment. Background technique [0002] Stimulation of the human immune response depends on the recognition of protein antigens by T cells. However, T cells cannot respond to antigen alone, only when the antigen is complexed with major histocompatibility complex (MHC) molecules on the surface of antigen-presenting cells such as B cells, macrophages or dendritic cells, to trigger T cells. [0003] MHC clas...
Claims
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Application Information
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