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US 10,851,082 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, Javier Izquierdo-Ferrer, Purav Vagadia, Matthew R. Clutter, Rama K. Mishra, Leonidas C. Platanias
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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.
Claims14
A compound having Formula:
- wherein:
- n is 0-6 and optionally (CH2)n is substituted with alkyl and forms a branched alkyl substituent;
- R1 is one 3-membered, one 4-membered ring, 5-membered ring, one 6-membered ring, or one 7-membered ring which ring is optionally saturated or unsaturated, or R1 is two fused rings which may be 5-membered rings or 6-membered rings which rings are optionally saturated or unsaturated, which one ring or rings are carbocycles or heterocycles including one or more heteroatoms, which one ring or rings optionally are substituted to include one or more non-hydrogen substituents, which non-hydrogen substituents optionally are selected from alkyl, halo, haloalkyl, hydroxyl, phenyl, amino, and carbonyl;
- R4 is hydrogen, alkyl, cycloalkyl;
- haloalkyl, halo, alkoxy, cyano, amino, hydroxyl, carboxyl, carboxy alkyl ester, phenyl optionally substituted with alkoxy, haloalkoxy, or benzamido;
- and
- R5 is hydrogen, alkyl, cycloalkyl, amino, carboxyl, carboxy alkyl ester, carboxy amido, carboxy alkyl amido, or N-benzimidazole.
4 more elements
A compound having Formula:
- wherein:
- n is 0-6 and optionally (CH2)n is substituted with alkyl and forms a branched alkyl substituent;
- R1 is one 3-membered, one 4-membered ring, 5-membered ring, one 6-membered ring, or one 7-membered ring which ring is optionally saturated or unsaturated, or R1 is two fused rings which may be 5-membered rings or 6-membered rings which rings are optionally saturated or unsaturated, which one ring or rings are carbocycles or heterocycles including one or more heteroatoms, which one ring or rings optionally are substituted to include one or more non-hydrogen substituents, which non-hydrogen substituents optionally are selected from alkyl, halo, haloalkyl, hydroxyl, phenyl, amino, and carbonyl;
- R3 has a structure
- R4 is hydrogen, alkyl, cycloalkyl;
- haloalkyl, halo, alkoxy, cyano, amino, hydroxyl, carboxyl, carboxy alkyl ester, phenyl optionally substituted with alkoxy, haloalkoxy, or benzamido;
- R5 is hydrogen, alkyl, cycloalkyl, amino, carboxyl, carboxy alkyl ester, carboxy amido, carboxy alkyl amido, or N-benzimidazole;
- and
- R9, R10, and R11 are the same or different and are selected from hydrogen, alkyl, alkoxy, halo, haloalkyl, nitro, carboxyalkyl, ester, and phenyl.
6 more elements
A compound selected from group consisting of:
Dependencies are inferred from the claim text.