US 11,963,947 B2
Pharmaceutical combination, composition and compound preparation comprising glucokinase activator and DPP-IV inhibitor, and preparation method and use thereof
Li Chen, Shanghai (CN); Yongguo Li, Shanghai (CN); Gaosen Wang, Shanghai (CN); and Huisheng Gao, Shanghai (CN)
Assigned to HUA Medicine (Shanghai) Ltd., Shanghai (CN)
Appl. No. 17/058,903
Filed by HUA Medicine (Shanghai) Ltd., Shanghai (CN)
PCT Filed May 28, 2019, PCT No. PCT/CN2019/088864
§ 371(c)(1), (2) Date Nov. 25, 2020,
PCT Pub. No. WO2019/228365, PCT Pub. Date Dec. 5, 2019.
Claims priority of application No. 201810556685.6 (CN), filed on May 31, 2018.
Prior Publication US 2021/0196682 A1, Jul. 1, 2021
Int. Cl. A61K 31/4155 (2006.01); A61K 9/16 (2006.01); A61K 9/20 (2006.01); A61K 9/28 (2006.01); A61K 31/155 (2006.01); A61K 31/40 (2006.01); A61K 31/403 (2006.01); A61K 31/4035 (2006.01); A61K 31/4439 (2006.01); A61K 31/4985 (2006.01); A61K 31/522 (2006.01); A61K 31/7034 (2006.01); A61K 45/06 (2006.01); A61K 47/38 (2006.01); A61P 3/10 (2006.01); C07D 231/38 (2006.01); C07D 403/12 (2006.01)
CPC A61K 31/4155 (2013.01) [A61K 9/1611 (2013.01); A61K 9/1617 (2013.01); A61K 9/1635 (2013.01); A61K 9/1694 (2013.01); A61K 9/2009 (2013.01); A61K 9/2013 (2013.01); A61K 9/2027 (2013.01); A61K 9/2054 (2013.01); A61K 9/2086 (2013.01); A61K 9/2095 (2013.01); A61K 9/2813 (2013.01); A61K 9/284 (2013.01); A61K 9/2866 (2013.01); A61K 31/155 (2013.01); A61K 31/40 (2013.01); A61K 31/403 (2013.01); A61K 31/4035 (2013.01); A61K 31/4439 (2013.01); A61K 31/4985 (2013.01); A61K 31/522 (2013.01); A61K 31/7034 (2013.01); A61K 45/06 (2013.01); A61K 47/38 (2013.01); A61P 3/10 (2018.01); C07D 231/38 (2013.01); C07D 403/12 (2013.01)] 28 Claims
OG exemplary drawing
 
1. A fixed dose combination formulation, comprising:
(a) a glucokinase activator, which is a compound represented by the following formulae, or a pharmaceutically acceptable salt, an isotope labeled analogue, a crystalline form, a hydrate, a solvate, a diastereomeric or enantiomeric form thereof,
 
 

OG Complex Work Unit Chemistry
 
(b) a DPP-IV inhibitor, wherein the DDP-IV inhibitor is sitagliptin or sitagliptin phosphate monohydrate; and
(c) one or more excipients, wherein the weight ratio of the glucokinase activator to the DPP-IV inhibitor is about 4:1 to about 5:1.