3-substituted isoquinolin-1-yl derivatives

US6469025B1 · kind B1 · utility

Assignee

• Celltech R&D Limited · GB

Inventors

• John Clifford Head · Maidenhead, GB
• Catherine McKay · Nashua, US
• John Robert Porter · Chinnor, GB

Key dates

• Filing date: Aug 1, 2001
• Grant date: Oct 22, 2002
• Expiry date: Aug 1, 2021

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D413/12
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Squaric acid derivatives of formula (1) are described: whereinR1 is a hydrogen atom or a C1-6alkyl group;L1 is a covalent bond or a linker atom or group;Alk1 is an optionally substituted aliphatic chain;n is zero or the integer 1;R2 is a hydrogen atom or an optionally substitued heteroaliphatic, cycloaliphatic, heterocycloaliphatic, polycycloaliphatic, heteropolycycloaliphatic, aromatic or heteroaromatic group;Alk is a chain—CH2CH(R)—, —CH═C(R)—, in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof;Ar2 is an optionally substituted aromatic or heteroaromatic linking group;L2 is a covalent bond or a linker atom or group;R16 is the group —L3(Alk2)tL4R20 in which L3 and L4 which may be the same or different is each a covalent bond or a linker atom or group, t is zero or the integer 1, Alk2 is an optionally substituted aliphatic or heteroaliphatic chain and R20 is an optionally substituted aromatic or heteroaromatic group;The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders, or disorders including the inappropria…