摘要:
The invention relates to compounds of formula (I) B-Q-X1, wherein B is a bioactive, cell adhesive mediating molecule, selected from the group (i) and Thr-Trp-Tyr-Lys-Ile-Ala-Phe-Gln-Arg-Asn-Arg-Lys (SEQ ID NO: 1) (ii), Trp-Tyr-Lys-Ile-Ala-Phe-Gln-Arg-Asn-Arg-Lys (SEQ ID NO: 2) (iii), Tyr-Lys-Ile-Ala-Phe-Gln-Arg-Asn-Arg-Lys (SEQ ID NO: 3) (iv), Thr-Trp-Tyr-Lys-Ile-Ala-Phe-Gln-Arg-Asn-Arg (SEQ ID NO: 4) (v), Thr-Trp-Tyr-Lys-Ile-Ala-Phe-Gln-Arg-Asn (SEQ ID NO: 5) (vi), Thr-Trp-Tyr-Lys-Ile-Ala-Phe-Gln-Arg (SEQ ID NO: 6) (vii), wherein (i) X, Y, Z, R2, R3, R4, A, Ar, Hal, Het, Het1, n, m, o, p, q, s, t have the meanings cited in claim 1, Q is absent or is an organic spacer molecule, X1 is an anchor molecule selected from the group cited in claim 1, and the salts thereof, which can be used as integrin inhibitors particularly for treatment of illness, deficiencies and inflammations caused by implants and osteolytic illnesses such as osteoporosis, thrombosis, cardiac infarction and arteriosclerosis, in addition to the acceleration and strengthening of the integration process of implants or the biocompatible surface in tissue.
摘要翻译:本发明涉及式(I)BQX 1的化合物,其中B是选自(i)和Thr-Trp-Tyr-Lys-Ile-Ala的生物活性的细胞粘附介导分子 -Ph-Gln-Arg-Asn-Arg-Lys(SEQ ID NO:1)(ii),Trp-Tyr-Lys-Ile-Ala-Phe-Gln-Arg-Asn-Arg-Lys(SEQ ID NO: )(iii),Tyr-Lys-Ile-Ala-Phe-Gln-Arg-Asn-Arg-Lys(SEQ ID NO:3)(iv),Thr-Trp-Tyr-Lys-Ile-Ala-Phe-Gln -Arg-Asn-Arg(SEQ ID NO:4)(v),Thr-Trp-Tyr-Lys-Ile-Ala-Phe-Gln-Arg-Asn(SEQ ID NO:5)(vi) -Tyr-Lys-Ile-Ala-Phe-Gln-Arg(SEQ ID NO:6)(vii),其中(i)X,Y,Z,R 2,R 3 A,Ar,Hal,Het,Het 1,n,m,o,p,q,s,t具有引用的含义 在权利要求1中,Q不存在或是有机间隔分子,X 1是选自权利要求1所述的基团的锚定分子及其盐,其可以用作整联蛋白抑制剂,特别是用于 治疗由植入物和溶骨性疾病引起的疾病,缺陷和炎症 例如骨质疏松症,血栓形成,心肌梗死和动脉硬化,以及植入物或组织中生物相容性表面的整合过程的加速和加强。
摘要:
The invention relates to compounds of formula (1) B-Q-X1, wherein B is bioactive cell adhesive mediating molecule. Q is absent or is an inorganic spacer molecule and X1 is an anchor molecule, selected from the group Lys-(CO—CH2—(CH2)n—PO3H2)2(I), -Lys-[-Lys-(CO—CH2—(CH2)a—PO3H2)2]2(ii) or -Lys-(Lys[-Lys-(CO—CH2—(CH2)n—PO3H2]2 (iii), and n independently represents 0, 1, 2 or 3, wherein a free amino group of group B is linked in peptide form to a free carboxyl group of the spacer molecule Q or of the anchor molecule X1, or a free amino group of the radical Q is linked in peptide form to a free carboxyl group of the radical X1. The invention also relates to the salts thereof. The inventive compounds can be used as integrin inhibitors for the treatment of illnesses, deficiencies, inflammations caused by implants and osteolytic illnesses such as osteoporosis, thrombosis, cardiac infarction and arteriosclerosis, in addition to the acceleration and strengthening of the integration process of implants or the biocompatible surface in tissue.