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US 7,745,451 B2Granted
Tetrahydronaphthyridine and tetrahydropyrido[4,3-d]pyrimidine compounds and compositions thereof useful in the treatment of conditions associated with neurological and inflammatory disorders and dysfunctions
AssigneeRenovis, Inc.
InventorsMichael G. Kelly, John Kincaid, Carl J. Kaub
Life of this patent
Estimating the term…
Abstract
Fused heterocyclic compounds are disclosed that have formula 1: where A, B, L, N, R1, R3, R4′, Y and Z are as defined herein. The compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, cognitive disorders, anxiety, depression, and others.
Claims31
A compound having a formula 1:
- wherein
- A and B are independently CR2′R2′, CO, or CS;
- Y is CR2′R2′;
- W is N;
- Z is O or NR2;
- L is substituted or unsubstituted C1-C9 alkylene or substituted or unsubstituted C1-C9 heteroalkylene;
- R1 is a substituted or unsubstituted carbocyclic group or a substituted or unsubstituted heterocyclic group;
- R2 is hydrogen, C1-C6 alkyl, or C3-C8 cycloalkyl;
- each R2′ is independently hydrogen, C1-C6 alkyl, C3-C8 cycloalkyl, aryl, or aralkyl;
- R3 is substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl;
- and
- R4′ is R4 or —Z-L′-R4, wherein Z′ is a single bond, NR2′, O, S, SO, SO2, COO, or CONR2′, and L′ is (C1-C6)alkylene;
- and wherein R4 is selected from the group consisting of H, alkyl, —C(O)R20, —NR21C(O)R22, alkylamino, alkylthio, alkoxy, alkoxycarbonyl, alkylarylamino, arylalkyloxy, amino, aryl, arylalkyl, —SO2R23, substituted sulfanyl, aminosulfonyl, arylsulfonyl, dihydroxyphosphoryl, azido, carbamoyl, carboxyl, cyano, cycloalkyl, cycloheteroalkyl, dialkylamino, halo, heteroaryloxy, heteroaryl, heteroalkyl, hydroxy, nitro, and —SH;
- wherein
- R20 is hydrogen, alkyl, cycloalkyl, cycloheteroalkyl, aryl, arylalkyl, heteroalkyl, heteroaryl, or heteroarylalkyl;
- R21 is hydrogen, alkyl, cycloalkyl, cycloheteroalkyl, aryl, arylalkyl, heteroalkyl, heteroaryl, or heteroarylalkyl;
- R22 is alkyl, alkoxy, cycloalkyl, cycloheteroalkyl, aryl, arylalkyl, heteroalkyl, heteroaryl, or heteroarylalkyl;
- and
- R23 is alkyl, aryl, or heteroaryl;
- or a pharmaceutically acceptable salt, a stereoisomer, a tautomer or an isotopic variant thereof.
17 more elements
A compound having a formula 1:
- wherein
- A and B are independently CR2′R2′, CO, or CS;
- Y is CR2′R2′;
- W is N;
- Z is O or NR2;
- L is a single bond;
- R1 is a substituted or unsubstituted carbocyclic group or a substituted or unsubstituted heterocyclic group;
- R2 is hydrogen, C1-C6 alkyl, or C3-C8 cycloalkyl;
- each R2 is independently hydrogen, C1-C6 alkyl, C3-C8 cycloalkyl, aryl, or aralkyl;
- R3 is a carbocyclic group or a heterocyclic group;
- and
- R4′ is R4 or —Z′-L′-R4, wherein Z′ is a single bond, NR2′, O, S, SO, SO2, COO, or CONR2′, and L′ is (C1-C6)alkylene;
- and wherein R4 is selected from the group consisting of H, alkyl, —C(O)R20, —NR21C(O)R22, alkylamino, alkylthio, alkoxy, alkoxycarbonyl, alkylarylamino, arylalkyloxy, amino, aryl, arylalkyl, —SO2R23, substituted sulfanyl, aminosulfonyl, arylsulfonyl, dihydroxyphosphoryl, azido, carbamoyl, carboxyl, cyano, cycloalkyl, cycloheteroalkyl, dialkylamino, halo, heteroaryloxy, heteroaryl, heteroalkyl, hydroxy, nitro, and —SH;
- wherein
- R20 is hydrogen, alkyl, cycloalkyl, cycloheteroalkyl, aryl, arylalkyl, heteroalkyl, heteroaryl, or heteroarylalkyl;
- R21 is hydrogen, alkyl, cycloalkyl, cycloheteroalkyl, aryl, arylalkyl, heteroalkyl, heteroaryl, or heteroarylalkyl;
- R22 is alkyl, alkoxy, cycloalkyl, cycloheteroalkyl, aryl, arylalkyl, heteroalkyl, heteroaryl, or heteroarylalkyl;
- and
- R23 is alkyl, aryl, or heteroaryl;
- or a pharmaceutically acceptable salt, a stereoisomer, a tautomer or an isotopic variant thereof.
17 more elements
Dependencies are inferred from the claim text.