Title:
NON-STEROIDAL SELECTIVE GLUCOCORTICOID RECEPTOR AGONISTIC MODULATORS (SEGRAMs) AND USES THEREOF
Document Type and Number:
WIPO Patent Application WO/2019/081517
Kind Code:
A3
Abstract:
The present invention relates to the two enantiomers of a SElective Glucocorticoid Receptor Agonistic Modulator (SEGRAM) of Formula 1 or a derivative thereof; to a deuterated form of a SEGRAM of Formula 1 or a derivative thereof; and to the two deuterated enantiomers of a SEGRAM of (Formula 1) or a derivative thereof: or a pharmaceutically acceptable salt, solvate and/or prodrug thereof. The present invention also relates to a SEGRAM of Formula 1 or a derivative thereof, or a pharmaceutically acceptable enantiomer, deuterated form, salt, solvate and/or prodrug thereof, for use in the prevention or treatment of an inflammatory disorder in a subject in need thereof.
Inventors:
CHAMBON PIERRE (FR)
HUA GUOQIANG (FR)
HUA GUOQIANG (FR)
Application Number:
PCT/EP2018/079049
Publication Date:
June 20, 2019
Filing Date:
October 23, 2018
Export Citation:
Assignee:
ASSOCIATION POUR LA RECH A LIGBMC ARI (FR)
International Classes:
A61K31/137; A61K31/343; A61K31/381; A61P1/00; A61P11/06; A61P17/00; A61P17/06; A61P29/00; C07D201/00; C07D307/88
Foreign References:
| US6323199B1 | 2001-11-27 | |||
| US20060040933A1 | 2006-02-23 |
Other References:
GUOQIANG HUA ET AL: "Glucocorticoid-induced tethered transrepression requires SUMOylation of GR and formation of a SUMO-SMRT/NCoR1-HDAC3 repressing complex", PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, vol. 113, no. 5, 28 December 2015 (2015-12-28), pages E635 - E643, XP055517008, ISSN: 0027-8424, DOI: 10.1073/pnas.1522826113
MIKE BARKER ET AL: "Design and Synthesis of New Nonsteroidal Glucocorticoid Modulators through Application of an "Agreement Docking" Method", JOURNAL OF MEDICINAL CHEMISTRY, vol. 48, no. 14, 1 July 2005 (2005-07-01), pages 4507 - 4510, XP055517287, ISSN: 0022-2623, DOI: 10.1021/jm050345y
FOSTER A B: "Deuterium isotope effects in the metabolism of drugs and xenobiotics: implications for drug design", ADVANCES IN DRUG RESEA, ACADEMIC PRESS, LONDON, GB, vol. 14, 1 January 1985 (1985-01-01), pages 1 - 40, XP009086953, ISSN: 0065-2490
MIKE BARKER ET AL: "Design and Synthesis of New Nonsteroidal Glucocorticoid Modulators through Application of an "Agreement Docking" Method", JOURNAL OF MEDICINAL CHEMISTRY, vol. 48, no. 14, 1 July 2005 (2005-07-01), pages 4507 - 4510, XP055517287, ISSN: 0022-2623, DOI: 10.1021/jm050345y
FOSTER A B: "Deuterium isotope effects in the metabolism of drugs and xenobiotics: implications for drug design", ADVANCES IN DRUG RESEA, ACADEMIC PRESS, LONDON, GB, vol. 14, 1 January 1985 (1985-01-01), pages 1 - 40, XP009086953, ISSN: 0065-2490
Attorney, Agent or Firm:
ICOSA (FR)
Download PDF:
Previous Patent: METHOD FOR PRODUCING AN ELECTRICAL COIL AND WINDING DEVICE
Next Patent: AN INJECTION DEVICE WITH A VIBRATION GENERATOR
Next Patent: AN INJECTION DEVICE WITH A VIBRATION GENERATOR