发明名称 Peptide vectors
摘要 Disclosed is a protein-camptothecin conjugate according to the formula X-B1-B2-B3-B4-Z wherein: X is selected from camptothecin or a camptothecin derivative; Each of B1, B2, B3 and B4 is independently for each occurrence (Doc)m, (Aepa)n, -(C(O)-A1-A2-A3-A4-A5-C(O))s- or (amino acid)p; wherein the amino acid is selected from the group consisting of Gly, Val, Abu, Gaba, Doc, and Sar; each of A1 and A5 is, for each occurrence, CH2; each of A2, A3, and A4 is, independently for each occurrence, CH2 or (CH2)t or absent; integers m, n, p, s and t are as described in the specification; and Z is a peptide selected from the list of -Lys-DTyr-DTyr-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH2 ; -DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH2 ; -DPhe-cyclo(Cys-3ITyr-DTrp-Lys-Val-Cys)-Thr-NH2; -Gln-Trp-Ala-Val-betaAla-His-Leu-Leu-NH2 ; -DPhe-Gln-Trp-Ala-Val-betaAla-His-Leu-Leu-NH2 ; -Gln-Trp-Ala-Val-betaAla-His-Leu-Nle-NH2 ; -DCys-3Pal-DTrp-Lys-DCys-Thr-Tyr-NH2; and -pGlu-His-Trp-Ser-Tyr-DLys[Nepsilon~]-Leu-Arg-Pro-Gly-NH2; or a pharmaceutically acceptable salt thereof. In particular the conjugated protein may be a somatostatin, LHRH or bombesin analogue. The compounds disclosed are useful as targeted cytotoxic agents. Also disclosed herein are intermediates for the production of compounds of formula (I).
申请公布号 NZ564694(A) 申请公布日期 2009.11.27
申请号 NZ20040564694 申请日期 2004.04.21
申请人 SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES S.A.S. 发明人 DONG, ZHENG XIN;SHEN, YEELANA;COMSTOCK, JEANNE MARY;KIM, SUN H
分类号 A61K38/04;A61K;A61K38/01;A61K38/02;A61K38/03;A61K38/05;A61K38/06;A61K38/07;A61K38/08;A61K38/09;A61K38/10;A61K38/12;A61K38/16;A61K38/22;A61K38/24;A61K38/31;A61K47/48;C07K2/00;C07K7/00;C07K7/08;C07K7/23;C07K7/50;C07K7/64;C07K14/00;C07K14/655;C07K14/665;C07K19/00 主分类号 A61K38/04
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