2-oxo-1,2-dihydropyridine-3-carboxamide compounds and their use as dual inhibitors of pdk1/aura
AssigneeInternational Society for Drug Development S.R.L.
InventorsSimona SESTITO, Simona DANIELE, Claudia MARTINI, Simona RAPPOSELLI, Guido PURICELLI
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Abstract
The present invention concern a 2-oxo-1,2-dihydropyridine-3-carboxamide compound of Formula (I) in the treatment of pathologies which require a dual inhibitor of PDK1/AurA enzymes such as for instance tumours, particularly glioblastoma.
Claims26
A method for treating pathologies requiring the use of a dual inhibitor of PDK1/AurA enzymes, said method comprising administering a 2-oxo-1,2-dihydropyridine-3-carboxamide compound of Formula (I)
- or a pharmaceutical salt thereof
- wherein
- B is CH-D, where D is imidazolyl;
- and
- A is selected from the group consisting of (—NH—CO—CH2—), (—NH—CO—CH2—CH2), (—NH—CO—CH(Ph)-) and (—NH—CO—CH2—CH2—CH2)
- R1 is H or CH3, R2 is H or Br or R1 and R2 taken together form the group —(N═CH—CH═CH)—
- with the proviso that
- when A is selected from (—NH—CO—CH2—CH2) and (—NH—CO—CH2—CH2—CH2), then R1 and R2 are H.
A 2-oxo-1,2-dihydropyridine-3-carboxamide compound of Formula (I)
- or a pharmaceutical salt thereof
- wherein
- B is CH-D, where D is imidazolyl;
- and
- A is selected from the group consisting of (—NH—CO—CH2—), (—NH—CO—CH(Ph)-) and (—NH—CO—CH2—CH2—CH2)
- R1 is H or CH3, R2 is H or Br or R1 and R2 together represent the group —(N═CH—CH═C)—
- with the proviso that
- when A is (—NH—CO—CH2—CH2—CH2) then R1 and R2 are H and
- when A is (—NH—CO—CH2—) or (—NH—CO—CH(Ph)-), then R1 and R2 are not simultaneously H.
(canceled)
A pharmaceutical combination comprising at least one PDK1 inhibitor and at least one AurA inhibitor.
Dependencies are inferred from the claim text.