Polymorphs of suberoylanilide hydroxamic acid

作者: Thomas A Miller , Victoria M Richon , Judy H Chiao

DOI:

关键词:

摘要: The present invention provides methods of selectively inducing terminal differentiation, cell growth arrest and/or apoptosis neoplastic cells, inhibiting histone deacetylase (HDAC) by administration pharmaceutical compositions comprising potent HDAC inhibitors. oral bioavailability the active compounds in is surprisingly high. Moreover, unexpectedly give rise to high, therapeutically effective blood levels over an extended period time. further a safe, daily dosing regimen these compositions, which easy follow, and results amount inhibitors vivo. also novel Form I polymorph SAHA, characterized unique X-ray diffraction pattern Differential Scanning Calorimetry profile, as well crystalline structure.

参考文章(86)
Miguel A Rubio, Cristina Lopez-Rodriguez, Arsenio Nueda, Patricio Aller, Angel L Armesilla, Miguel A Vega, Angel L Corbí, Granulocyte-macrophage colony-stimulating factor, phorbol ester, and sodium butyrate induce the CD11c integrin gene promoter activity during myeloid cell differentiation Blood. ,vol. 86, pp. 3715- 3724 ,(1995) , 10.1182/BLOOD.V86.10.3715.BLOODJOURNAL86103715
Lawrence Blas Perez, Sushil Kumar Sharma, Michael A. Green, Stacy William Remiszewski, Richard William Versace, Lidia Sambucetti, Kenneth Walter Bair, Hydroxamate derivatives useful as deacetylase inhibitors ,(2001)
Ada Rephaeli, Abraham Nudelman, Oxyalkylene phosphate compounds and uses thereof ,(1998)
John C. Byrd, Charlotte Shinn, Rajani Ravi, Carl R. Willis, Jamie K. Waselenko, Ian W. Flinn, Nancy A. Dawson, Michael R. Grever, Depsipeptide (FR901228): A novel therapeutic agent with selective, in vitro activity against human B-cell chronic lymphocytic leukemia cells Blood. ,vol. 94, pp. 1401- 1408 ,(1999) , 10.1182/BLOOD.V94.4.1401
Anna Rubartelli, Roberto Sitia, Neris Bonifaci, High Rates of Thioredoxin Secretion Correlate with Growth Arrest in Hepatoma Cells Cancer Research. ,vol. 55, pp. 675- 680 ,(1995)
Martin J. Edelman, Kenneth Bauer, Shyam Khanwani, Nancy Tait, Jane Trepel, Judith Karp, Noble Nemieboka, Eun-Joo Chung, David Van Echo, Clinical and pharmacologic study of tributyrin: an oral butyrate prodrug. Cancer Chemotherapy and Pharmacology. ,vol. 51, pp. 439- 444 ,(2003) , 10.1007/S00280-003-0580-5
Benjamin Pomerantz, Giulia Porro, Leonid Reznikov, Flavio Leoni, Paolo Pagani, Soo-Hyun Kim, Pietro Pozzi, Paolo Mascagni, Britta Siegmund, Charles Dinarello, Giancarlo Dona, Philip Bufler, Giamila Fantuzzi, Histone deacetylase enzyme-inhibiting derivatives of hydroxamic acid as new cytokine synthesis-inhibiting anti-inflammatory drugs ,(2002)