US 12,213,978 B2
Madrasin-derivative compounds, composition and uses thereof for treating cancer
Sébastien Apcher, Franconville (FR); Mouad Alami, Bussy Saint Georges (FR); Romain Darrigrand, Sauveterre de Béarn (FR); Samir Messaoudi, Ballainvilliers (FR); Valérie Salgues, Nogent sur Marne (FR); Zafiarisoa Dolor Renko, Les Ulis (FR); and Expedite Yen-Pon, Plaine des Palmistes (FR)
Assigned to INSERM (INSTITUT NATIONAL DE LA SANTÉ ET DE LA RECHERCHE MÉDICALE), Paris (FR); CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, Paris (FR); INSTITUT GUSTAVE ROUSSY, Villejuif (FR); and UNIVERSITE PARIS-SACLAY, Gif-sur-Yvette (FR)
Appl. No. 17/293,506
Filed by INSTITUT GUSTAVE ROUSSY, Villejuif (FR); INSERM (INSTITUT NATIONAL DE LA SANTÉ ET DE LA RECHERCHE MÉDICALE), Paris (FR); CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, Paris (FR); and UNIVERSITE PARIS-SACLAY, Gif-sur-Yvette (FR)
PCT Filed Nov. 15, 2019, PCT No. PCT/EP2019/081516
§ 371(c)(1), (2) Date May 13, 2021,
PCT Pub. No. WO2020/099650, PCT Pub. Date May 22, 2020.
Claims priority of application No. 18306499 (EP), filed on Nov. 15, 2018.
Prior Publication US 2022/0047597 A1, Feb. 17, 2022
Int. Cl. A61K 31/517 (2006.01); A61K 31/5377 (2006.01); A61K 31/661 (2006.01); A61K 31/7064 (2006.01); A61K 45/06 (2006.01); A61P 35/00 (2006.01)
CPC A61K 31/517 (2013.01) [A61K 31/5377 (2013.01); A61K 31/661 (2013.01); A61K 31/7064 (2013.01); A61K 45/06 (2013.01); A61P 35/00 (2018.01)] 15 Claims
 
1. A composition comprising a compound and a pharmaceutically acceptable carrier, optionally together with at least one anticancer agent, the compound being selected from the group consisting of:
5,6-Dimethyl-2-((4-methyl-7-(2-morpholinoethoxy)quinazolin-2-yl)amino)pyrimidin-4(3H)-one

OG Complex Work Unit Chemistry
Sodium 2-((4,5-dimethyl-6-oxo-1,6-dihydropyrimidin-2-yl)amino)-4-methylquinazolin-7-yl phosphate

OG Complex Work Unit Chemistry
and

OG Complex Work Unit Chemistry
wherein:
R1 and R2 are independently selected from H, CH3 (Methyl), Cl (Chlorine), and a thiosugar, and
R3 is

OG Complex Work Unit Chemistry
wherein:
R4 is absent, H, CH3 (Methyl), C2H5 (Ethyl) or n-Propyl,
Z is CH2 or C═O,
n is 1, 2 or 3, and
X is O, N or CH.