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US 9,006,238 B2Granted
Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
AssigneeGenkyotex SA
InventorsPatrick Page, Mike Orchard, Benoit Laleu, Francesca Gaggini
Life of this patent
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Abstract
The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).
Claims23
A method for the inhibiting, arresting the development of, relieving the symptoms of and/or causing regression of the symptoms of a patient suffering from cardiovascular disorders, respiratory disorders, metabolism disorders, skin disorders, bone disorders, neuroinflammatory and/or neurodegenerative disorders, kidney diseases, reproduction disorders, diseases affecting the eye and/or the lens and/or conditions affecting the inner ear, inflammatory disorders, liver diseases, pain, cancers, allergic disorders, traumatisms, septic, hemorrhagic and anaphylactic shock, disorders of the gastrointestinal system, angiogenesis and angiogenesis-dependent conditions, the method comprising administering a pyrazolo pyridine derivative according to Formula (I):
- wherein G1 is selected from H;
- optionally substituted acyl;
- optionally substituted acyl C1-C6 alkyl;
- optionally substituted alkyl C3-C8-cycloalkyl alkyl;
- optionally substituted heterocycloalkyl alkyl;
- optionally substituted aryl alkyl;
- and optionally substituted heteroaryl alkyl;
- G2 is selected from —CHR1R2 and a saturated ring system selected from optionally substituted C3-C8-cycloalkyl and optionally substituted heterocycloalkyl;
- R1 and R2 are independently selected from H;
- optionally substituted alkoxy;
- optionally substituted alkoxy C1-C6 alkyl;
- optionally substituted amino;
- optionally substituted aminoalkyl;
- optionally substituted acyl;
- C1-C6 alkyl;
- optionally substituted C2-C6 alkenyl;
- optionally substituted C2-C6 alkynyl;
- optionally substituted aryl;
- optionally substituted C1-C6 alkyl aryl;
- optionally substituted aryl C1-C6 alkyl;
- optionally substituted heteroaryl;
- optionally substituted C1-C6 alkyl heteroaryl;
- optionally substituted heteroaryl C1-C6 alkyl;
- optionally substituted C2-C6 alkenyl aryl;
- optionally substituted aryl C2-C6 alkenyl;
- optionally substituted C2-C6 alkenyl heteroaryl;
- optionally substituted heteroaryl C2-C6 alkenyl;
- optionally substituted C3-C8-cycloalkyl;
- optionally substituted heterocycloalkyl;
- optionally substituted C1-C6 alkyl C3-C8-cycloalkyl;
- optionally substituted C3-C8-cycloalkyl C1-C6 alkyl;
- optionally substituted C1-C6 alkyl heterocycloalkyl and optionally substituted heterocycloalkyl C1-C6 alkyl;
- or —CHR1R2 form together a ring selected from optionally substituted C3-C8-cycloalkyl and optionally substituted heterocycloalkyl;
- G3 is selected from H;
- optionally substituted amino;
- optionally substituted aminoalkyl;
- optionally substituted aminocarbonyl;
- optionally substituted alkoxy;
- optionally substituted alkoxy C1-C6 alkyl;
- optionally substituted carbonyl;
- optionally substituted C1-C6 alkyl;
- optionally substituted C2-C6 alkenyl;
- optionally substituted C2-C6 alkynyl;
- optionally substituted aryl;
- optionally substituted aryl C1-C6 alkyl;
- optionally substituted heteroaryl;
- optionally substituted C1-C6 alkyl heteroaryl;
- optionally substituted heteroaryl C1-C6 alkyl;
- optionally substituted C2-C6 alkenyl aryl;
- optionally substituted aryl C2-C6 alkenyl;
- optionally substituted C2-C6 alkenyl heteroaryl;
- optionally substituted heteroaryl C2-C6 alkenyl;
- optionally substituted C3-C8-cycloalkyl;
- optionally substituted heterocycloalkyl;
- optionally substituted C1-C6 alkyl C3-C8-cycloalkyl;
- optionally substituted C3-C8-cycloalkyl C1-C6 alkyl;
- optionally substituted C1-C6 alkyl heterocycloalkyl and optionally substituted heterocycloalkyl C1-C6 alkyl;
- G4 is selected from H;
- optionally substituted acyl;
- optionally substituted acyl amino;
- optionally substituted acyl C1-C6 alkyl;
- optionally substituted C1-C6 alkyl;
- optionally substituted C2-C6 alkenyl;
- optionally substituted C2-C6 alkynyl;
- optionally substituted aryl;
- optionally substituted C1-C6 alkyl aryl;
- optionally substituted aryl C1-C6 alkyl;
- optionally substituted heteroaryl;
- optionally substituted C1-C6 alkyl heteroaryl;
- optionally substituted heteroaryl C1-C6 alkyl;
- optionally substituted C2-C6 alkenyl aryl;
- optionally substituted aryl C2-C6 alkenyl;
- optionally substituted C2-C6 alkenyl heteroaryl;
- optionally substituted heteroaryl C2-C6 alkenyl;
- optionally substituted C3-C8-cycloalkyl;
- optionally substituted heterocycloalkyl;
- optionally substituted C1-C6 alkyl C3-C8-cycloalkyl;
- optionally substituted C3-C8-cycloalkyl C1-C6 alkyl;
- optionally substituted C1-C6 alkyl heterocycloalkyl and optionally substituted heterocycloalkyl C1-C6 alkyl;
- G5 is selected from H;
- optionally substituted C1-C6 alkyl;
- optionally substituted C2-C6 alkenyl;
- optionally substituted C2-C6 alkynyl;
- optionally substituted aryl;
- optionally substituted C1-C6 alkyl aryl;
- optionally substituted aryl C1-C6 alkyl;
- optionally substituted heteroaryl;
- optionally substituted C1-C6 alkyl heteroaryl;
- optionally substituted heteroaryl C1-C6 alkyl;
- optionally substituted C2-C6 alkenyl aryl;
- optionally substituted aryl C2-C6 alkenyl;
- optionally substituted C2-C6 alkenyl heteroaryl;
- optionally substituted heteroaryl C2-C6 alkenyl;
- optionally substituted C3-C8-cycloalkyl;
- optionally substituted heterocycloalkyl;
- optionally substituted C1-C6 alkyl C3-C8-cycloalkyl;
- optionally substituted C3-C8-cycloalkyl C1-C6 alkyl;
- optionally substituted C1-C6 alkyl heterocycloalkyl and optionally substituted heterocycloalkyl C1-C6 alkyl;
- or a tautomer, geometrical isomer, optically active form as enantiomer, diastereomer and racemate forms or a pharmaceutically acceptable salt thereof, to a patient in need of treatment of said disease or condition.
96 more elements
A method for inhibiting angiogenesis in a patient suffering from angiogenesis or angiogenesis dependent disorder, wherein the method comprises administering an angiogenesis inhibitory dose of a compound of Formula (I)
- wherein G1 is selected from H;
- optionally substituted acyl;
- optionally substituted acyl C1-C6 alkyl;
- optionally substituted alkyl;
- optionally substituted C3-C8-cycloalkyl alkyl;
- optionally substituted heterocycloalkyl alkyl;
- optionally substituted aryl alkyl;
- and heteroaryl alkyl;
- G2 is selected from H;
- optionally substituted C1-C6 alkyl;
- optionally substituted C2-C6 alkenyl;
- optionally substituted C2-C6 alkynyl;
- optionally substituted aryl;
- optionally substituted C1-C6 alkyl aryl;
- optionally substituted aryl C1-C6 alkyl;
- optionally substituted heteroaryl;
- optionally substituted alkyl heteroaryl;
- optionally substituted heteroaryl C1-C6 alkyl;
- optionally substituted C2-C6 alkenyl aryl;
- optionally substituted aryl C2-C6 alkenyl;
- optionally substituted C2-C6 alkenyl heteroaryl;
- optionally substituted heteroaryl C2-C6 alkenyl;
- optionally substituted C3-C8-cycloalkyl;
- heterocycloalkyl;
- optionally substituted alkyl C3-C8-cycloalkyl;
- C3-C8-cycloalkyl C1-C6 alkyl;
- optionally substituted C1-C6 alkyl heterocycloalkyl and optionally substituted heterocycloalkyl C1-C6 alkyl;
- G3 is selected from —(CH2)n—R1 and —(CH2)p—R5;
- R1 is selected from —NR2R3;
- —OR4;
- optionally substituted heterocycloalkyl;
- optionally substituted heteroaryl;
- —CHR6R7;
- optionally substituted acyl and —C(O)NR2R3;
- R2 and R3 are independently selected from H;
- optionally substituted C1-C6 alkyl;
- optionally substituted C2-C6 alkenyl;
- optionally substituted C2-C6 alkynyl;
- optionally substituted aryl;
- optionally substituted C1-C6 alkyl aryl;
- optionally substituted aryl C1-C6 alkyl;
- optionally substituted heteroaryl;
- optionally substituted alkyl heteroaryl;
- optionally substituted heteroaryl C1-C6 alkyl;
- optionally substituted C2-C6 alkenyl aryl;
- optionally substituted aryl C2-C6 alkenyl;
- optionally substituted C2-C6 alkenyl heteroaryl;
- optionally substituted heteroaryl C2-C6 alkenyl;
- optionally substituted C3-C8-cycloalkyl;
- optionally substituted heterocycloalkyl;
- optionally substituted alkyl C3-C8-cycloalkyl;
- optionally substituted C3-C8-cycloalkyl C1-C6 alkyl;
- optionally substituted C1-C6 alkyl heterocycloalkyl and optionally substituted heterocycloalkyl C1-C6 alkyl or NR2R3 form a ring selected from optionally substituted heteroaryl and optionally substituted heterocycloalkyl;
- R4 is selected from H;
- optionally substituted alkoxy C1-C6 alkyl;
- optionally substituted C1-C6 alkyl;
- optionally substituted C2-C6 alkenyl;
- optionally substituted C2-C6 alkynyl;
- optionally substituted aryl;
- optionally substituted C1-C6 alkyl aryl;
- optionally substituted aryl C1-C6 alkyl;
- optionally substituted heteroaryl;
- optionally substituted alkyl heteroaryl;
- optionally substituted heteroaryl C1-C6 alkyl;
- optionally substituted C2-C6 alkenyl aryl;
- optionally substituted aryl C2-C6 alkenyl;
- optionally substituted C2-C6 alkenyl heteroaryl;
- optionally substituted heteroaryl C2-C6 alkenyl;
- optionally substituted C3-C8-cycloalkyl;
- optionally substituted heterocycloalkyl;
- optionally substituted alkyl C3-C8-cycloalkyl;
- optionally substituted C3-C8-cycloalkyl C1-C6 alkyl;
- optionally substituted C1-C6 alkyl heterocycloalkyl and optionally substituted heterocycloalkyl C1-C6 alkyl;
- R5 is selected from H;
- optionally substituted alkoxy;
- optionally substituted alkoxy C1-C6 alkyl;
- optionally substituted C1-C6 alkyl;
- optionally substituted C2-C6 alkenyl;
- optionally substituted C2-C6 alkynyl;
- optionally substituted aryl;
- optionally substituted C1-C6 alkyl aryl;
- optionally substituted aryl C1-C6 alkyl;
- optionally substituted heteroaryl;
- alkyl heteroaryl;
- optionally substituted heteroaryl C1-C6 alkyl;
- optionally substituted C2-C6 alkenyl aryl;
- aryl C2-C6 alkenyl;
- optionally substituted C2-C6 alkenyl heteroaryl;
- optionally substituted heteroaryl C2-C6 alkenyl;
- optionally substituted C3-C8-cycloalkyl;
- optionally substituted heterocycloalkyl;
- optionally substituted alkyl C3-C8-cycloalkyl;
- optionally substituted C3-C8-cycloalkyl C1-C6 alkyl;
- optionally substituted C1-C6 alkyl heterocycloalkyl and optionally substituted heterocycloalkyl C1-C6 alkyl;
- R6 and R7 are independently selected from optionally substituted C2-C6 alkenyl;
- optionally substituted C2-C6 alkynyl;
- optionally substituted aryl;
- optionally substituted C1-C6 alkyl aryl;
- optionally substituted aryl C1-C6 alkyl;
- optionally substituted heteroaryl;
- optionally substituted alkyl heteroaryl;
- optionally substituted heteroaryl C1-C6 alkyl;
- optionally substituted C2-C6 alkenyl aryl;
- optionally substituted aryl C2-C6 alkenyl;
- optionally substituted C2-C6 alkenyl heteroaryl;
- optionally substituted heteroaryl C2-C6 alkenyl;
- optionally substituted C3-C8-cycloalkyl;
- optionally substituted heterocycloalkyl;
- optionally substituted alkyl C3-C8-cycloalkyl;
- optionally substituted C3-C8-cycloalkyl C1-C6 alkyl;
- optionally substituted C1-C6 alkyl heterocycloalkyl and optionally substituted heterocycloalkyl C1-C6 alkyl or —CHR6R7 forms an optionally substituted ring selected from optionally substituted heteroaryl, optionally substituted cycloalkyl and optionally substituted heterocycloalkyl;
- n is an integer selected from 0 to 5;
- p is an integer selected from 3 to 5;
- G4 is selected from H;
- optionally substituted acyl;
- acyl amino;
- optionally substituted acyl C1-C6 alkyl;
- optionally substituted C1-C6 alkyl;
- optionally substituted C2-C6 alkenyl;
- optionally substituted C2-C6 alkynyl;
- optionally substituted aryl;
- optionally substituted C1-C6 alkyl aryl;
- optionally substituted aryl C1-C6 alkyl;
- heteroaryl;
- optionally substituted C1-C6 alkyl heteroaryl;
- optionally substituted heteroaryl C1-C6 alkyl;
- optionally substituted C2-C6 alkenyl aryl;
- optionally substituted aryl C2-C6 alkenyl;
- optionally substituted alkenyl heteroaryl;
- optionally substituted heteroaryl C2-C6 alkenyl;
- optionally substituted C3-C8-cycloalkyl;
- optionally substituted heterocycloalkyl;
- optionally substituted C1-C6 alkyl C3-C8-cycloalkyl;
- optionally substituted C3-C8-cycloalkyl C1-C6 alkyl;
- optionally substituted C1-C6 alkyl heterocycloalkyl and optionally substituted heterocycloalkyl C1-C6 alkyl;
- G5 is selected from H;
- optionally substituted C1-C6 alkyl;
- optionally substituted C2-C6 alkenyl;
- optionally substituted C2-C6 alkynyl;
- optionally substituted aryl;
- optionally substituted C1-C6 alkyl aryl;
- optionally substituted aryl C1-C6 alkyl;
- optionally substituted heteroaryl;
- optionally substituted C1-C6 alkyl heteroaryl;
- optionally substituted heteroaryl C1-C6 alkyl;
- optionally substituted C2-C6 alkenyl aryl;
- optionally substituted aryl C2-C6 alkenyl;
- optionally substituted C2-C6 alkenyl heteroaryl;
- optionally substituted heteroaryl C2-C6 alkenyl;
- optionally substituted C3-C8-cycloalkyl;
- optionally substituted heterocycloalkyl;
- optionally substituted C1-C6 alkyl C3-C8-cycloalkyl;
- optionally substituted C3-C8-cycloalkyl C1-C6 alkyl;
- optionally substituted C1-C6 alkyl heterocycloalkyl and optionally substituted heterocycloalkyl C1-C6 alkyl;
- or a tautomer, geometrical isomer, optically active form as enantiomer, diastereomer and racemate forms or a pharmaceutically acceptable salt thereof, in a patient in need thereof.
152 more elements
Dependencies are inferred from the claim text.