Darbufelone Mesilate

Darbufelone mesilate is in phase III clinical trials by Pfizer and Zhuhai United Laboratories for the treatment of rheumatoid arthritis.

Index：

General Information

Update Date：2016-02-23

Drug Name：
Darbufelone Mesilate
Research Code：
CI-1004; PD-136095-0073
Trade Name：
MOA：
COX-2 inhibitor
Indication：
Rheumatoid arthritis (RA)
Status：
Phase III (Active)
Company：
Pfizer (Originator), 珠海联邦制药 (Originator)
Sales：
ATC Code：
Chemical Structure

Update Date：2015-12-01

Molecular Weight 428.57
Formula C18H24N2O2S • CH4O3S
CAS No. 139226-28-1 (Darbufelone);
139340-56-0 (Darbufelone mesylate);
Chemical Name 4(5H)-Thiazolone, 2-amino-5-[[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]methylene]-, (5Z)-, methanesulfonate (1:1)
Darbufelone （Free Acid/Base）Parameters：
MW HD HA FRB* PSA* cLogP*
332.46 3 4 4 101 4.846±0.373
*：Calculated by ACD/Labs software V11.02.
Synthesis & Impurities

Update Date：2016-03-03


1. J. Med. Chem. 1994, 37, 322-328.

2. Bioorg. Med. Chem. Lett. 1993, 3, 1729-1734.

3. US5143928.

4. Drugs Fut. 1999, 24, 853-857.

Impurity database is being updated！