Biomet Deutschland Gmbh

Merck Patent Gmbh

Merck Patent Gesellschaft MIT

Christoph Gibson

Horst Kessler

Guenter Hoelzemann

Berthold Nies

Simon Lawrence Goodman

Martin Kantlehner

Joerg Meyer

G&uuml;nter H&ouml;lzemann

Michel Dard

Gabor Sulyok

Ulrich Hersel

J&ouml;rg Simon Schmitt

Gab&oacute;r Sulyok

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

Diacylhydrazine derivatives

Diacylhydrazine derivatives as integrin inhibitors

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Ihringen, Germany

Christoph Gibson