Shire Orphan Therapies Gmbh

Grit Zahn

Ulrich Reineke

Frank Osterkamp

Gerd Hummel

Gunther Zischinsky

Roland Stragies

Dirk Scharn

Holger Kalkhof

Doerte Vossmeyer

Claudia Christner-Albrecht

Sascha Birkner

Jochen Knolle

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

This invention is directed to compounds of structure (I). Particularly this invention is directed to compounds of structure (VIII) wherein the variables are defined as in the description. These compounds are integrin inhibitors and are useful in the treatment of diseases in which an inhibition of angiogenesis is desired. 

Compounds for the inhibition of angiogenesis 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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Berlin, Germany

Grit Zahn