The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Jun. 22, 2010
Filed:
Mar. 01, 2005
Philip Wilson Howard, St Albans, GB;
Stephen John Gregson, London, GB;
Philip Wilson Howard, St Albans, GB;
Stephen John Gregson, London, GB;
Spirogen Limited, Ryde, Isle of Wight, GB;
Abstract
The present inventors have developed a key intermediate for the production of C2 substituted PBDs, which has a leaving group at the C2 position, a carbamate protecting group at the N10 position and a protected hydroxy group at the C11 position. In a first aspect, the present invention comprises a compound with a the formula (I), wherein: Ris a carbamate-based nitrogen protecting group; Ris an oxygen protecting group; and Ris a labile leaving group. In a further aspect, the present invention comprises a method of synthesising a compound of formula (III), or a solvate thereof, from a compound of formula (I) as defined in the first aspect, Ris either O—R11, wherein Ris as defined in the first aspect, or OH, or Rand Rtogether form a double bond between N10 and C11; and Ris R. The other substituents are defined in the claims. Further aspects of the present invention relate to compounds of formula (III) (including solvates thereof when Rand Rform a double bond between N10 and C11, and pharmaceutical salts thereof), pharmaceutical compositions comprising these, and their use in the manufacture of a medicament for the treatment of a proliferative disease.