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US 2021/0230156 A1Published application
NOVEL HUMAN DIHYDROOROTATE DEHYDROGENASE (hDHODH) INHIBITORS AND THEIR USE IN TARGETING ONCOLOGICAL DISEASES SENSITIVE TO PYRIMIDINE STARVATION
AssigneeDrug Discovery and Clinic S.R.L.
InventorsDonatella BOSCHI, Marta GIORGIS, Marco Lucio LOLLI, Giovanni MARTINELLI, Giuseppe SAGLIO
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Abstract
Compounds of formulae (I) and (II) which are novel inhibitors of human dihydroorotate dehydrogenase (hDHODH) and pharmaceutical compositions containing the compounds of formulae (I) and (II) are provided. A method for treating tumor diseases, including acute myelogenous leukemia (AML), triple-negative breast cancer, PTEN-mutant tumors, and KRAS-driven tumors by administering pharmaceutical compositions containing the compounds of formulae (I) and (II) is also provided.
Claims18
A compound having formula (I)
- wherein:
- R1, R2, R4 and R5 are independently selected from the group consisting of a hydrogen atom, a halogen atom, a C1-C4 alkyl group, an alkyloxy group, an alkylthio group and a halo C1-C4 alkyl group;
- R3 is selected from the group consisting of phenyl, pyridil, pyridinil, phenoxy, pyridiloxy, pyridinoxy, thiophenoxy, thiophenyl, phenylthio, phenylcarboxamido, and a phenylaminocarbonyl group;
- R7, R8 and R9 are independently selected from a hydrogen atom, a halo C1-C4 alkyl group, a thio C1-C4 alkyl group, an amino C1-C4 alkyl group, a C1-C4 alkyl group and a hydroxy C1-C4 alkyl group;
- R6 is selected from a C1-C4 alkyloxy group, an aciloxy group, a hydroxyl group, a thiol group and a salt thereof;
- and
- X, Y and Z are independently selected from a carbon atom and a nitrogen atom, wherein if X or Y or Z is nitrogen, the other two are carbon atoms.
4 more elements
A compound having formula (II)
- wherein:
- R1, R2, R4 and R5 are independently selected from the group consisting of a hydrogen atom, a halogen atom, a C1-C4 alkyl group, an alkyloxy group, an alkylthio group and a halo C1-C4 alkyl group;
- R3 is selected from the group consisting of phenyl, pyridil, pyridinil, phenoxy, pyridiloxy, pyridinoxy, thiophenoxy, thiophenyl, phenylthio, phenylcarboxamido, and a phenylaminocarbonyl group, wherein if R3 is an aromatic group, a substituent independently selected from a halogen atom, an alkyl group, a trifluoromethyl group, and a trifluoromethoxy group can be present on the ring, and wherein if R3 is an aliphatic group, a substituent independently selected from an alkyl group, a trifluoromethyl group, and a trifluoromethoxy group can be present on the ring;
- R7, R8 and R9 are independently selected from a halo C1-C4 alkyl group, a thio C1-C4 alkyl group, an amino C1-C4 alkyl group, a C1-C4 alkyl group and a hydroxy C1-C4 alkyl group;
- R6 is selected from a C1-C4 alkyloxy group, an aciloxy group, a hydroxyl group, a thiol group and a salt thereof;
- and
- X, Y and Z are independently selected from a carbon atom and a nitrogen atom, wherein if X or Y or Z is nitrogen, the other two are carbon atoms.
4 more elements
Dependencies are inferred from the claim text.