Pharmaceutical compounds

US8383619B2 · kind B2 · utility

Assignee

• ASTEX THERAPEUTICS LIMITED · GB

Inventors

• Brian John Williams · Clitheroe, GB
• Martyn Frederickson · Cambridge, GB

Key dates

• Filing date: Oct 12, 2010
• Grant date: Feb 26, 2013
• Expiry date: Oct 12, 2030

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D209/44
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The invention provides a compound of the formula (1):or a salt, solvate, N-oxide or tautomer thereof;wherein either R1 is R1a and R2 is R2a; or R1 is R1b and R2 is R2b; provided that in each case at least one of R1 and R2 is other than hydrogen;R1a and R2a are the same or different and each is selected from hydrogen, C1-4 alkyl, C2-4 alkenyl and C2-4 alkynyl wherein the C1-4 alkyl is optionally substituted by C1-2 alkoxy;R1b and R2b are the same or different and are selected from hydrogen, C(O)NR4R5, C(O)R6 and C(O)OR6 where R6 is C1-4 alkyl, R4 and R5 are both C1-4 alkyl, or NR4R5 forms a 4 to 7 membered saturated heterocyclic ring optionally containing a second heteroatom ring member selected from O, N or S and oxidized forms of N and S, the heterocyclic ring being optionally substituted by one or two C1-4 alkyl groups and/or one or two oxo groups; andR3 is a group D:wherein the asterisk denotes the point of attachment to the isoindoline ring;but excluding acetic acid 5-acetoxy-4-isopropyl-2-[5-(4-methyl-piperazin-1-ylmethyl)-1,3-dihydro-isoindole-2-carbonyl]-phenyl ester.