Shire Orphan Therapies Gmbh

Holger Kalkhof

Ulrich Reineke

Frank Osterkamp

Gerd Hummel

Gunther Zischinsky

Dirk Scharn

Roland Stragies

Grit Zahn

Doerte Vossmeyer

Claudia Christner-Albrecht

The present invention is related to a compound of formula (I), wherein A is a nonaromatic heterocyclic ring, Ar is either absent or phenylene; &#x3a8; is a radical of formula (II), Ris a hydrophobic moiety; and G is a radical containing one or more moieties selected from the group consisting of NH, OH and a basic moiety. The compounds are inhibitors of integrins, especially antagonists of the fibronectin receptor alpha5beta1, useful as anti-angiogenic agents. 

Compounds for the inhibition of integrins and use thereof

The present invention relates to compounds of formula (I) wherein: A is a radical selected from the group comprising aromatic heterocyclic 5-membered ring systems; Ar is a radical selected from the group comprising optionally substituted 5- and 6-membered aromatic ring systems, whereby the ring system contains 0, 1, 2 or 3 heteroatoms selected from the group comprising N, O and S; Z is a linker and &#x3a8; is a radical of formula (II) and their use for the inhibition of integrin. 

Heterocyclic compounds for the inhibition of integrins and use thereof

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Holger Kalkhof