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US 2025/0074880 A1Published application
Novel quinoline derivatives and uses thereof
OwnerSaverio MINUCCI, Peter Arthur Irene DE WULF +6inventors
InventorsSaverio MINUCCI, Peter Arthur Irene DE WULF, Mauro ROMANENGHI, Riccardo CAZZOLI, Michela DAMIZIA, Romano SILVESTRI, Giuseppe LA REGINA, Antonio COLUCCIA
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Abstract
The invention refers to new quinoline-4-carboxamide derivatives, pharmaceutical compositions containing thereof and the use of the same as inhibitors of Ndc80 kinetochore subcomplex-MIT binding and of kinetochore-MIT binding, more preferably for use in the treatment of cell proliferative disorders including cancers and drug-resistant cancer.
Claims17
A compound having the following formula (I):
- wherein
- R1 is selected among phenyl, heterocycle, benzofused heterocycle, hydrogen optionally substituted at one or more position(s) with following same or different groups:
- alkyl, alkyl substituted at one or more position(s) with halogen(s), C3-C10 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 alkoxy, C2-C6 alkoxycarbonyl, 3-10 membered heterocycloalkyl, halogen, —CN, Nth, OH, NO2, NHR1′ NR1′R1 OR1′ where R1′, R1″ is alkyl, C3-C10 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 alkoxy, C2-C6 alkoxycarbonyl, 3-10 membered heterocycloalkyl or aromatic ring selected from phenyl, phenoxy, benzyl, benzyloxy, naphthyl, naphthyloxy, biphenyl or heterocycle, said aromatic ring optionally substituted at one or more position(s) with following same or different groups:
- alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 alkoxy, C2-C6 alkoxycarbonyl, 3-10 membered heterocycloalkyl, halogen, —CN, —NH2, —OH, —NO2;
- R2 is selected among hydrogen, phenyl, heterocycle, benzofused heterocycle, optionally substituted at one or more position(s) with following same or different groups:
- alkyl, C3-C10 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 alkoxy, C2-C6 alkoxycarbonyl, 3-10 membered heterocycloalkyl, halogen, —CN, NH2, OH, NO2, NHR1′ NR1′Rf OR1′ where R1′, R1″ is alkyl, C3-C10 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 alkoxy, C2-C6 alkoxycarbonyl 3-10 membered heterocycloalkyl or aromatic ring selected from phenyl, phenoxy, benzyl, benzyloxy, naphthyl, naphthyloxy, biphenyl or heterocycle, said aromatic ring optionally substituted at one or more position(s) with following same or different groups:
- alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 alkoxy, C2-C6 alkoxycarbonyl, 3-10 membered heterocycloalkyl, halogen, —CN, —NH2, —OH, —NO2;
- R3 is selected among hydrogen, alkyl, C3-C10 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 alkoxy, C2-C6 alkoxycarbonyl, 3-10 membered heterocycloalkyl, halogen, —CN, Nth, OH, NO2;
- R4 is selected among hydrogen, alkyl, C3-C10 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 alkoxy, C2-C6 alkoxycarbonyl, 3-10 membered heterocycloalkyl, halogen, —CN, NH2, OH, NO2;
- R5 is selected among hydrogen, alkyl, C3-C10 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 alkoxy, C2-C6 alkoxycarbonyl, 3-10 membered heterocycloalkyl, halogen, —CN, NH2, OH, NO2.
7 more elements
Dependencies are inferred from the claim text.