Biomet Deutschland Gmbh

Merck Patent Gesellschaft MIT Beschraenkter Haftung

Biomet Deutchland Gmbh

Merck Patent Department

Martin Kantlehner

Horst Kessler

Berthold Nies

Alfred Jonczyk

Dirk Finsinger

Guenter Hoelzemann

Christoph Gibson

Joerg Meyer

Michel Dard

Ulrich Hersel

Gabor Sulyok

Jörg Meyer

J&ouml;rg Meyer

The invention relates to compounds of formula (1) B-Q-X, wherein B is bioactive cell adhesive mediating molecule. Q is absent or is an inorganic spacer molecule and Xis an anchor molecule, selected from the group Lys-(CO&#x2014;CH&#x2014;(CH)&#x2014;POH)(I), -Lys-[-Lys-(CO&#x2014;CH&#x2014;(CH)&#x2014;POH)](ii) or -Lys-(Lys[-Lys-(CO&#x2014;CH&#x2014;(CH)&#x2014;POH](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 X, or a free amino group of the radical Q is linked in peptide form to a free carboxyl group of the radical X. 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.

Peptide and peptide mimetic conjugates with integrin-inhibitor properties

The invention relates to compounds of formula (I) B-Q-X, 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, R, R, R, A, Ar, Hal, Het, Het, n, m, o, p, q, s, t have the meanings cited in claim, Q is absent or is an organic spacer molecule, Xis an anchor molecule selected from the group cited in claim, 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.

Peptide and peptide mimetic derivatives with integrin-inhibitors properties II

Disclosed herein is a process for promoting the integration of a biocompatible device or implant into a tissue of a subject. The process comprises covalently bonding to the surface of the device or implant a compound of the formula IR-Q-X&#x2003;&#x2003;Iwherein R is cyclo-(Arg-Gly-Asp-Z), and wherein Q, X and Z are as defined herein.

Cyclopeptide derivatives

Cyclopeptide derivatives with integrin inhibitor properties

The invention describes the possibility of the biofunctionalization of biomaterials, in particular implants, by their made-to-measure coating with synthesized cell- or tissue-selective RGD peptides which in vitro stimulate the adhesion of mainly those cell species which in each case are intended to accomplish the tissue integration of the appropriate biomaterial.

Peptide-coated implants and methods for producing same

Growing community of inventors

Freising, Germany

Martin Kantlehner