Table 4.
Filed patents for CPU inhibitors with their corresponding lead compounds and highest development status reported.
| Company | Patents | Chemical Structure | Lead Compound | Highest Development Status Reported | Reference |
|---|---|---|---|---|---|
| AstraZeneca | WO/2000/66550 WO/2000/066557 WO/2000/066152 WO/2003/106420 WO/2003/027128 |
Phosphor and/or thiol-containing compounds | AZD9684 | Phase II completed; development halted |
[36,147,148] |
| WO/2005/039617 | Cyclic anabaenopeptin-type peptides | Unknown | Discovery | ||
| Unknown | Conformationally restricted imidazole derivatives | Compounds 7 and 12 | Preclinical | [149] | |
| Meiji Seika Kaisha/ MediciNova * | WO/2001/19836 | Phosphonic and phosphinic acid derivatives | EF6265/MN-462 * | Preclinical | [150,151] |
| Pfizer | WO/2002/14285 WO/2003/061652 WO/2003/061653 |
Imidazole propanoic acid derivatives | UK-396082 | Phase I completed, development halted |
[152,153] |
| Merck | WO/2003/013526 | Imidazole acetic acid derivatives | Compound 10j/ Compound (-)-8 |
Preclinical | [154,155] |
| Berlex Biosciences (Bayer) | WO/2003/080631 WO/2006/041808 |
Aryl guanidinic and mercaptopropionic acid derivatives | BX 528 | Preclinical | [156,157,158] |
| Sanofi | WO/2005/105781 WO/2007/045339 WO/2010/130718 WO/2013/076178 WO/2013/076179 WO/2008/067909 |
Imidazole, urea & sulfamide containing compounds | SAR104772 SAR126119 |
Phase I completed Phase II initiated in 2013 |
[159] |
| Sanofi | WO/2009/146802 WO/2014/198620 |
Macrocyclic urea derivatives | Unknown | Preclinical | [160,161,162] |
| Unknown | FFC.HTZ4.059 | Preclinical | [163] | ||
| Servier | WO/2010/149888 | 2-mercapto-cyclopentane carboxylic acid compounds |
Unknown | Discovery | |
| WO/2017/121969 | Phosphinane & azaphosphinane derivatives |
S62798 | Phase I completed | [95,164] | |
| Taisho Pharmaceutical | WO/2011/034215 | Dihydroimidazo-quinoline compounds | Unknown | Discovery | |
| Daiichi Sankyo | WO/2011/115064 WO/2011/115065 WO/2013/039202 |
Cycloalkyl-substituted imidazole, cyclopropanecarboxylic acid, and acrylic acid derivatives |
DS-1040 | Phase Ib/II completed; development halted | [52,53,165,166] |
| WO/2016/204239 WO/2016/104678 |
Combinations of a CPU inhibitor with other compounds | DS-1040 + rtPA DS-1040 + Edoxaban |
|||
| WO/2017/170460 | CPU inhibitor application in inflammatory bowel disease |
* EF6265 was obtained by MediciNova from MSK in 2006 and renamed MN-462.