Original document(35 pages)  中文版
    The present invention relates to compounds of formula (I), R-Q-X, wherein R = cyclo (Arg-Gly-Asp-Z), whereby Z is bonded in a side chain to Q or to X if Q is lacking, Q is lacking and represents -CO-R1-NH-m, -NH-R1-CO-m, -CO-R1-CO-, -(CO-CH2-O-CH2CH2-O-CH2CH2-NH-)n, -(NH-CH2-O-CH2CH2-O-CH2CH2-CO-)n, -(NH-CH2CH2-O-CH2CH2-O-CH2-CO-)n or -(CO-CH2-O-CH2CH2-O-CH2-CH2-NH-)n-CO-R1-NH-m, X = -CO-CH=CH2, -CO-C(CH3) = CH2, -NH-CH = CH2, -NH-C(CH3)=CH2 or -NH-(CH2)p-SH, Z means, independently from each other, an amino acid radical or a dipeptide or tripeptide radical, whereby the amino acids, independently from each other, are selected from a group consisting of Ala, Asn, Asp, Arg, Cys, Gln, Glu, Gly, His, Ile, Leu, Lys, Met, Phe, Pro, Ser, Thr, Trp, Tyr, Val or M, whereby the above-mentioned amino acids can also be derivatized, and the amino acid radicals are linked to each other like peptides by the alpha amino and alpha carboxy groups, and whereby M is always contained, M = NH(R8)-CH(R3)-COOH, and R1, R3, R8, m, n and p have the meanings cited in claim 1, in addition to the salts thereof, whereby said substances can be used as integrin inhibitors, especially in the treatment of implant-induced diseases, defects, inflammations and osteolytic diseases (such as osteoporosis), thrombosis, cardiac infarction, and arteriosclerosis, in addition to accelerating and amplifying the integration process of an implant or biocompatible surface in tissues.
Application Number
98812195 Application Date
Title 名称 Cyclopeptide derivatives with integrin inhibitor properties
Publication Number
1282337 Publication Date
Approval Pub. Date Granted Pub. Date
International Classification 分类号 A61K38/04;C07K7/64
Applicant(s) Name
Merck Patent GmbH
Address 地址
Inventor(s) Name 发明人 J. Meyer;B. Nies;D. Finsinger
Attorney & Agent 代理人 guo jianxin

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