Miles Stuart Congreve,Lynsey Helen Fazal,Martyn Frederickson,Christopher William Murray,Michael Alistair OBrien,Andrew James Woodhead,John Francis Lyons,Neil Thomas Thompson
申请号：
US12445154
公开号：
US08779132B2
申请日:
2007.10.12
申请国别(地区):
US
年份:
2014
代理人:
摘要：
The invention provides a compound for use in medicine, the compound being a compound of the formula (VI0) or a salt, solvate, tautomer or N-oxide thereof:wherein the bicyclic group:is selected from the structures C1, C5 and C6:wherein n is 0, 1, 2 or 3 R1 is hydrogen, hydroxy, or O—Rz R2a is hydroxy, methoxy or O—Rz provided that at least one of R1 and R2a is O—Rz Rz is Lp-Rp1 SO3H a glucuronide residue a mono-, di- or tripeptide residue orLp is a bond, C═O, (C═O)O, (C═O)NRp1 or S(O)xNRp1 x is 1 or 2 Rp1 is hydrogen or a an optionally substituted C1-25 hydrocarbyl group containing 0, 1 or 2 carbocyclic rings and 0, 1, 2, 3, 4, 5 or 6 carbon-carbon multiple bonds, provided that Rp1 is not hydrogen when Lp is a bond, C═O or (C═O)O and provided also that O—Rz does not contain an O—O moiety and excluding compounds wherein R1 is hydroxy and R2a is methoxy Rp2 and Rp3 are the same or different and each is a group Rp1 and R3, R4a, R8 and R10 are defined in the claims.The compounds of formula (VI0) are pro-drugs of parent compounds wherein R1 and/or R2a are hydroxy, wherein the parent compounds have Hsp90 inhibiting activity.
