发明申请
- 专利标题: PHARMACEUTICAL COMPOUNDS
- 专利标题(中): 药物化合物
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申请号: US12445154申请日: 2007-10-12
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公开(公告)号: US20100152184A1公开(公告)日: 2010-06-17
- 发明人: Miles Stuart Congreve , Lynsey Helen Fazal , Martyn Frederickson , Christopher William Murray , Michael Alistair O'Brien , Andrew James Woodhead , John Francis Lyons , Neil Thomas Thompson
- 申请人: Miles Stuart Congreve , Lynsey Helen Fazal , Martyn Frederickson , Christopher William Murray , Michael Alistair O'Brien , Andrew James Woodhead , John Francis Lyons , Neil Thomas Thompson
- 申请人地址: GB Cambridge
- 专利权人: ASTEX THERAPEUTICS LIMITED
- 当前专利权人: ASTEX THERAPEUTICS LIMITED
- 当前专利权人地址: GB Cambridge
- 国际申请: PCT/GB2007/003860 WO 20071012
- 主分类号: A61K31/5377
- IPC分类号: A61K31/5377 ; C07D209/44 ; C07D215/14 ; C07D221/20 ; C07D471/04 ; C07D403/10 ; C07D413/12 ; A61K31/4035 ; A61K31/47 ; A61K31/438 ; A61K31/497 ; A61P35/00
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; or Lp 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.
公开/授权文献
- US08779132B2 Pharmaceutical compounds 公开/授权日:2014-07-15
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