4,5-disubstituted-2-aminopyrimidines

US6600037B1 · kind B1 · utility

Assignee

• Celltech R&D Limited · GB

Inventors

• Jeremy Martin Davis · Slough, GB
• David Festus Charles Moffat · Woodstock, GB

Key dates

• Filing date: Oct 19, 2000
• Grant date: Jul 29, 2003
• Expiry date: Oct 19, 2020

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D403/12
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Pyrimidines of formla (1) are described: whereinR1 is a —XR6 group;R2 and R3 which may be the same or different is each a hydrogen or halogen atom or a group selected from an optionally substituted aliphatic, cycloaliphatic, heteroaliphatic, heterocycloaliphatic, —OH, —OR10 [where R10 is an optionally substituted aliphatic, cycloaliphatic, heteroaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group] —SH, —NO2, —CN, —SR10, —COR10, S(O)R10, —SO2R8, —SO2N(R8)(R9), —CO2R8, —CON(R8)(R9), —CSN(R8)(R9), —NH2 or substituted amino group;R4 is a X1R11 group where X1 is a covalent bond or a —C(R12)(R13)— [where each of R12 and R13 is a hydrogen or halogen atom or a hydroxyl, alkyl or haloalkyl group] or —C(O)— group and R11 is an optionally substituted phenyl, thienyl, thiazolyl or indolyl group;R5 is a halogen atom or an alkynyl group;and the salts, solvates, hydrates and N-oxides thereof.The compounds are selective KDR kinase and/or FGFr kinase inhibitors and are of use in the prophylaxis and treatment of disease states associated with angiogenesis.