Title:
CLASS- AND ISOFORM-SPECIFIC HDAC INHIBITORS AND USES THEREOF
Document Type and Number:
WIPO Patent Application WO/2011/019393
Kind Code:
A3
Abstract:
HDAC inhibitors of the general formula (I) and (II) and pharmaceutically acceptable salts thereof, as described herein, are useful as inhibitors of histone deacetylases or other deacetylases, and thus are useful for the treatment of various diseases and disorders associated with acetylase/deacetylase activity as described herein (e.g., cancer). In certain embodiments, the compounds of the invention selectively target either a class or isoform of the HDAC family. Another aspect of the invention provides an assay for determining the inhibitory effect of a test compound on an HDAC protein comprising: incubating the HDAC protein with a substrate of general formula (IIIc) in the presence of a test compound; and determining the activity of the HDAC protein.
Inventors:
MAZITSCHEK RALPH (US)
BRADNER JAMES ELLIOT (US)
BRADNER JAMES ELLIOT (US)
Application Number:
PCT/US2010/002220
Publication Date:
June 16, 2011
Filing Date:
August 11, 2010
Export Citation:
Assignee:
HARVARD COLLEGE (US)
DANA FARBER CANCER INST INC (US)
MAZITSCHEK RALPH (US)
BRADNER JAMES ELLIOT (US)
DANA FARBER CANCER INST INC (US)
MAZITSCHEK RALPH (US)
BRADNER JAMES ELLIOT (US)
International Classes:
C07C243/38; A61K31/175; A61P35/00; C07C237/04; C07C241/04
Domestic Patent References:
| WO1991000257A1 | 1991-01-10 | |||
| WO2009063054A1 | 2009-05-22 | |||
| WO2008040934A1 | 2008-04-10 |
Other References:
BRADNER, J. E. ET AL.: "Chemical phylogenetics of histone deacetylases", NATURE CHEMICAL BIOLOGY, SUPPLEMENTARY INFORMATION, vol. 6, no. 3, 7 February 2010 (2010-02-07), pages 238 - 243, XP055198519, DOI: doi:10.1038/nchembio.313
MAHBOOBI, S. ET AL.: "Design of Chimeric Histone Deacetylase- and Tyrosine Kinase-Inhibitors: A Series of Imatinib Hybrides as Potent Inhibitors of Wild-Type and Mutant BCR-ABL, PDGF-R.beta., and Histone Deacetylases", JOURNAL OF MEDICINAL CHEMISTRY, vol. 52, no. 8, 30 March 2009 (2009-03-30), pages 2265 - 2279, XP055117467, DOI: doi:10.1021/jm800988r
MAHBOOBI, S. ET AL.: "Design of Chimeric Histone Deacetylase- and Tyrosine Kinase-Inhibitors: A Series of Imatinib Hybrides as Potent Inhibitors of Wild-Type and Mutant BCR-ABL, PDGF-R.beta., and Histone Deacetylases", JOURNAL OF MEDICINAL CHEMISTRY, vol. 52, no. 8, 30 March 2009 (2009-03-30), pages 2265 - 2279, XP055117467, DOI: doi:10.1021/jm800988r
Attorney, Agent or Firm:
BAKER, C., Hunter (Greenfield & Sacks P.C.,600 Atlantic Avenu, Boston MA, US)
Download PDF:
Previous Patent: INTERACTIVE SPORTS-THEMED GAME
Next Patent: MULTIPLE LAYER SUBSTRATE SUPPORT AND EXHAUST GAS TREATMENT DEVICE
Next Patent: MULTIPLE LAYER SUBSTRATE SUPPORT AND EXHAUST GAS TREATMENT DEVICE