NEW AMINO ACID DERIVATIVE

PROBLEM TO BE SOLVED: To obtain the subject new compound useful as a chemokine receptor antagonist capable of inhibiting diseases caused by the chemokine such as interleukin 8 or MIP-1 α. SOLUTION: This compound is represented by the formula; R -X -ph-X -A-Y- R [A is D or L-Arg, Lys or the like; X i...

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Hauptverfasser: YAMAZAKI TORU, SUZUKI SHIGERU, EDAMATSU TAKEO, YANAKA MIKIRO, DEWA TOSHIKAZU, TAKEMURA YOSHIYUKI, INOGUCHI EIJI, MARUOKA HIROSHI, HIROSE KUNITAKA, HAKOZAKI MITSUNORI
Format: Patent
Sprache:eng
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Zusammenfassung:PROBLEM TO BE SOLVED: To obtain the subject new compound useful as a chemokine receptor antagonist capable of inhibiting diseases caused by the chemokine such as interleukin 8 or MIP-1 α. SOLUTION: This compound is represented by the formula; R -X -ph-X -A-Y- R [A is D or L-Arg, Lys or the like; X is NH, O or the like; X is absent, SO2 or the like; Y is S, O or the like; R and R are each a 12-30C straight-chain alkyl, cholesteryl or the like], e.g. 2-(isopropylcarbamoyl)-benzoyl-L-arginine-n- hexadecylamide. The compound is obtained by condensing, e.g. an N-terminal protected amino acid with a compound represented by the formula; R -Y-H, then removing the N-terminal protecting group, condensing the resultant compound represented by the formula; A'-Y-R (A' is an amino acid having the protected side chain) with a compound represented by the formula; R X -ph-X -Z (Z is a halogen or hydroxyl group) and prepared by condensing a compound represented by the formula; R -X -Z with a compound represented by the formula; X -ph-X -OR (R is a protecting group) and subsequently deprotecting the obtained compound and further removing the side chain protecting group of the amino acid.