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US 10,093,668 B2Granted
Substituted aromatic N-heterocyclic compounds as inhibitors of mitogen-activated protein kinase interacting kinase 1 (Mnk1) and 2 (Mnk2)
AssigneeNorthwestern University
InventorsGary E. Schiltz, Rama K. Mishra, Leonidas C. Platanias, Javier Izquierdo-Ferrer
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Abstract
Disclosed are substituted aromatic N-heterocyclic compounds. The disclosed compounds typically exhibit kinase inhibition activity, for example, and inhibit Mnk1 kinase and/or Mnk2 kinase. The disclosed compounds may be used in pharmaceutical compositions and methods for treating diseases or disorders associated with Mnk1 kinase activity and/or Mnk2 kinase activity, such as cancers, diabetes, autism, and fragile X syndrome.
Claims13
A compound having a formula selected from Formula II and III:
- wherein:
- Z is NH or O;
- n=0, 1, 2, or 3;
- R1 is hydrogen, alkyl, alkoxyl, hydroxyl, hydroxyalkyl, carboxyl, carboxyalkylester, cycloalkyl optionally substituted at one or more positions with hydroxyl or alkoxyl, amino optionally substituted with alkyl, amido optionally substituted with phenyl or substituted phenyl, thioamido, phenyl optionally substituted at one or more positions with halo or amido, pyridinyl, pyrrolidinyl, tetrahydropyranyl, tetrahydrofuranyl, oxetanyl, pyrrolidonyl, piperidinyl, piperazinyl optionally substituted with alkyl, morpholinyl, imidazolyl optionally substituted at one or more positions with alkyl, pyrazolyl, benzyamidyl, N-methylbenzamid-4-yl, benzoyl, benzoylpiperazine, N-phenylformamidyl, indolyl,
- or R1 has a structure selected from
- R4 is hydrogen, alkyl, haloalkyl, halo, alkoxyl, cyano, amino, hydroxyl, carboxyl, or carboxy alkyl ester;
- and
- R9, R10, and R11 are the same or different and are hydrogen, alkyl, or phenyl, wherein at least one of R9 and R10 is phenyl.
5 more elements
A compound having a formula:
- wherein:
- Z is NH or O;
- n=0, 1, 2, or 3;
- R1 is hydrogen, alkyl, alkoxyl, hydroxyl, hydroxyalkyl, carboxyl, carboxyalkylester, cycloalkyl optionally substituted at one or more positions with hydroxyl or alkoxyl, amino optionally substituted with alkyl, amido optionally substituted with phenyl or substituted phenyl, thioamido, phenyl optionally substituted at one or more positions with halo or amido, pyridinyl, pyrrolidinyl, tetrahydropyranyl, tetrahydrofuranyl, oxetanyl, pyrrolidonyl, piperidinyl, piperazinyl optionally substituted with alkyl, morpholinyl, imidazolyl optionally substituted at one or more positions with alkyl, pyrazolyl, benzyamidyl, N-methylbenzamid-4-yl, benzoyl, benzoylpiperazine, N-phenylformamidyl, indolyl, or R1 has a structure selected from
- and
- R4 is hydrogen, alkyl, haloalkyl, halo, alkoxyl, cyano, amino, hydroxyl, carboxyl, or carboxy alkyl ester.
3 more elements
A compound having a formula:
- wherein:
- n=0, 1, 2, or 3;
- R1 is hydrogen, alkyl, alkoxyl, hydroxyl, hydroxyalkyl, carboxyl, carboxyalkylester, cycloalkyl optionally substituted at one or more positions with hydroxyl or alkoxyl, amino optionally substituted with alkyl, amido optionally substituted with phenyl or substituted phenyl, thioamido, phenyl optionally substituted at one or more positions with halo or amido, pyridinyl, pyrrolidinyl, tetrahydropyranyl, tetrahydrofuranyl, oxetanyl, pyrrolidonyl, piperidinyl, piperazinyl optionally substituted with alkyl, morpholinyl, imidazolyl optionally substituted at one or more positions with alkyl, pyrazolyl, benzyamidyl, N-methylbenzamid-4-yl, benzoyl, benzoylpiperazine, N-phenylformamidyl, indolyl,
- or R1 has a structure selected from
- R4 is hydrogen, alkyl, haloalkyl, halo, alkoxyl, cyano, amino, hydroxyl, carboxyl, or carboxy alkyl ester.
2 more elements
Dependencies are inferred from the claim text.