&bgr;-phenylalanine derivatives as integrin antagonists

US6589972B2 · kind B2 · utility

Assignee

• BAYER HEALTHCARE LLC · DE

Inventors

• Andreas Schoop · Overath, DE
• Gerhard Mueller · Leverkusen, DE
• Ulf Brueggemeier · Madison, US
• Delf Schmidt · Wuppertal, DE
• Beatrix Stelte-Ludwig · Wülfrath, DE
• Joerg Keldenich · Wuppertal, DE

Key dates

• Filing date: May 30, 2001
• Grant date: Jul 8, 2003
• Expiry date: May 30, 2021

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C311/47
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention relates to compounds of the general formula (1) wherein R4 is —SO2R4′, —COOR4″, —COR4′, —CONR4′2 or —CSNR4′2; R4′ is hydrogen, a substituted or unsubstituted alkyl or cycloalkyl residue, a substituted or unsubstituted aryl residue or a saturated or unsaturated, optionally substituted heterocyclic residue; R4″ is a substituted or unsubstituted alkyl or cycloalkyl residue, a substituted or unsubstituted aryl residue or a saturated or unsaturated, optionally substituted heterocyclic residue; L is a sulphonamide, amide, ether, ester, keto, urea, thioether, sulphoxide or sulphone unit optionally extended by one or two methylene groups; and X is N, O or S; and their physiologically acceptable salts and stereoisomers. The present invention furthermore relates to a process for the preparation of the compounds of the formula (1), a pharmaceutical composition containing at least one of these compounds, and the use of compounds of the formula (1) for the production of a pharmaceutical composition having integrin-antagonistic action and in particular for the therapy and prophylaxis of cancer, osteolyt…