NOVEL FORMS OF CDDO METHYL ESTER

Japanese Patent JP2018009001

A

PROBLEM TO BE SOLVED: To provide more effective triterpenoid analogs since the naturally occurring triterpenoids which are biosynthesized in plants by the cyclization of squalene display relatively weak biological activity, although they are candidates for medicinal use.SOLUTION: Provided is an anhydrous crystal of methyl 2-cyano-3,12-dioxoleana-1,9(11)-dien-28-oate (CDDO methyl ester) shown in FIG. 1, having an x-ray powder diffraction pattern with a certain peak based on the Cu Kα radiation data. The compound can be prepared, for example, from a saturated methanol solution, and has a non-crystalline glassy solid form and a non-hydrous crystalline form. The glassy form displays an enhanced bioavailability over the non-hydrous crystalline form, and a superior candidate for use for treating a variety of disease states, generally associated with inflammation. It is administered to a cancer patient in combination with other anticancer agents, or is used for treatment of diseases or disorders associated with inflammation characterized by overexpression of iNOS or COX2.SELECTED DRAWING: Figure 1

WALLING JOHN
PARENT STEPHAN D
JONAITIS DAVID T
KRAL ROBERT M

JP2017154939A

January 18, 2018

August 10, 2017

Click for automatic bibliography generation  

REATA PHARMACEUTICALS INC

C07J63/00; A61K31/56; A61P29/00; C07C15/04

JPH03275681A	1991-12-06
JPH01273020A	1989-10-31
JPH01163171A	1989-06-27
JP2004331657A	2004-11-25
JP2007509911A	2007-04-19

WO2006127926A2	2006-11-30
US20030119732A1	2003-06-26

J. MED. CHEM., vol. 43, no. 22, JPN6010041022, 2000, pages 4233 - 4246, ISSN: 0004033150
ACTA CRYSTALLOGRAPHICA, SECTION C, vol. 58, no. 3, JPN6010041023, 2002, pages 119 - 200, ISSN: 0004033151

Yusuke Hiraki
Satoshi Fujita
Eiichi Arai

Previous Patent: How to prepare a nucleoside prodrug

Next Patent: A between leaf stem cell and its directions