Quinoline derivatives as p13 kinase inhibitors
AssigneeSmithKline Beecham Corporation
InventorsNicholas D. Adams, Amita M. Chaudhari
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Abstract
Invented is a method of inhibiting the activity/function of PI3 kinases using quinoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoline derivatives.
Claims25
A compound of Formula (I):
- in which
- R2 is an optionally substituted ring system selected from a group consisting of:
- formula (II), (III), (IV), (V), (VI), (VII), (VIII), (IX), and (X):
- R1 is selected from a group consisting of:
- heterocycloalkyl, substituted heterocycloalkyl, aryl, substituted aryl, heteroaryl and substituted heteroaryl;
- each R3 and R4 is independently selected from:
- hydrogen, halogen, acyl, amino, substituted amino, C1-6alkyl, substituted C1-6alkyl, C3-7cycloalkyl, substituted C3-7cycloalkyl, C3-7heterocycloalkyl, substituted C3-7heterocycloalkyl, alkylcarboxy, aminoalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, arylalkyl, substituted arylalkyl, arylcycloalkyl, substituted arylcycloalkyl, heteroarylalkyl, substituted heteroarylalkyl, cyano, hydroxyl, alkoxy, nitro, acyloxy, and aryloxy;
- n is 1-2;
- X is C or N;
- Y is C, O, N, or S;
- or a pharmaceutically acceptable salt thereof;
- provided that in each of formula (V) to (X) at least one X or Y is not carbon, and that R2 is not a pyridinyl or substituted pyridinyl group;
- further provided that R2 is not quinoline or substituted quinoline.
A method of inhibiting one or more phosphatoinositides 3-kinases (PI3Ks) in a human;
- comprising administering to the human a therapeutically effective amount of a compound of Formula (I)
- or a pharmaceutically acceptable salt thereof;
- in which
- R2 is an optionally substituted ring system selected from a group consisting of:
- formula (II), (III), (IV), (V), (VI), (VII), (VIII), (IX), and (X):
- R1 is selected from a group consisting of:
- heterocycloalkyl, substituted heterocycloalkyl, aryl, substituted aryl, heteroaryl and substituted heteroaryl;
- each R3 and R4 is independently selected from:
- hydrogen, halogen, acyl, amino, substituted amino, C1-6alkyl, substituted C1-6alkyl, C3-7cycloalkyl, substituted C3-7cycloalkyl, C3-7heterocycloalkyl, substituted C3-7heterocycloalkyl, alkylcarboxy, aminoalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, arylalkyl, substituted arylalkyl, arylcycloalkyl, substituted arylcycloalkyl, heteroarylalkyl, substituted heteroarylalkyl, cyano, hydroxyl, alkoxy, nitro, acyloxy, and aryloxy;
- n is 1-2;
- X is C or N;
- Y is C, O, N, or S;
- or a pharmaceutically acceptable salt thereof;
- provided that in each of formula (V) to (X) at least one X or Y is not carbon and that R2 is not a pyridinyl or substituted pyridinyl group.
Dependencies are inferred from the claim text.