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- Nachgewiesen in: USPTO Patent Applications
- Sprachen: English
- Document Number: 20110195933
- Publication Date: August 11, 2011
- Appl. No: 13/057510
- Application Filed: July 27, 2009
- Claim: 1. A compound of formula I: [chemical expression included] or a pharmaceutically acceptable salt or hydrate thereof; wherein: Z is —-N(R1)— or —O—; X1 is selected from the group consisting of: H, halogen, C1-6alkyl, C2-6alkenyl, C3-6cycloalkyl, CF3, methoxy, CN, CON(R3)2, (trimethylsilyl)ethynyl, phenyl and a monocyclic or bicyclic ring system comprising up to 10 ring atoms, of which 1-3 are selected from N, O and S and the remainder are C, said phenyl and ring system bearing 0-3 substituents independently selected from halogen and C1-4alkyl, optionally substituted with up to 3 halogen atoms; X2 is selected from the group consisting of: H, halogen, C1-6alkyl, C2-6alkenyl, C3-6cycloalkyl, CF3, methoxy, CN, CON(R3)2, (trimethylsilyl)ethynyl, and phenyl bearing 0 to 5 halogen substituents; X3 is selected from the group consisting of: H, OR3, N(R3)2, C1-6alkyl, C2-6alkenyl, C3-6cycloalkyl, CF3, methoxy, CN, CON(R3)2, (trimethylsilyl)ethynyl, and halogen; X4 is selected from the group consisting of: H, halogen, C3-6cycloalkyl, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-6cycloalkenyl, —CN, nitro and N(R3)2; said C1-6alkyl optionally substituted with up to 3 halogen atoms and said C2-6alkenyl and C2-6alkynyl optionally substituted with up to 3 R5 groups Y is selected from the group consisting of: N and CH; R1 represents H or C1-4alkyl which is optionally substituted with OH, CN, CF3, C1-4alkoxy, amino, C1-4alkylamino or di(C1-4alkyl)amino; R2 is selected from: (i) H; (ii) C1-8alkyl or C2-8alkenyl, either of which optionally bears up to 3 substituents independently selected from halogen, OH, CN, CF3, OR3, SR4, SO2R4, SO2N(R3)2, COR3, CO2R3, CON(R3)2, N(R3)2, NR3COR4, NR3SO2R4 and phenyl, said phenyl bearing 0 to 5 halogen substituents; and (iii) C3-10cycloalkyl, C3-10cycloalkylC1-4alkyl, Het, HetC1-4alkyl, aryl or arylC1-4alkyl, any of which optionally bears up to 4 substituents independently selected from halogen, OH, oxo, CN, CF3, R4, OR3, SR4, SO2R4, SO2N(R3)2, COR3, CO2R3, CON(R3)2, N(R3)2, NR3COR4, NR3SO2R4 and —P(O)—(OR3)2; where “aryl” refers to phenyl or 5- or 6-membered heteroaryl, either of which phenyl or heteroaryl is optionally fused to a 5- or 6-membered carbocycle or heterocycle, “Het” refers to a nonaromatic or partially aromatic mono- or bicyclic heterocyclic system of up to 10 ring atoms and C3-10cycloalkyl and the cyclic portion of C3-10cycloalkylC1-4alkyl may be fused with phenyl or a 5- or 6-membered heteroaryl; or R1 and R2 together may complete a mono- or bicyclic heterocyclic system of up to 10 ring atoms which optionally bears up to 3 substituents independently selected from halogen, OH, oxo, CN, CF3, R4, OR3, SR4, SO2R4, SO2N(R3)2, COR3, CO2R3, CON(R3)2, N(R3)2, NR3COR4 and NR3SO2R4; each R3 independently represents H or C1-6alkyl which is optionally substituted with up to 3 halogen atoms or with OH, CN, CF3, C1-4alkoxy, amino, C1-4alkylamino or di(C1-4alkyl)amino, or R3 represents phenyl, benzyl or 5- or 6-membered heteroaryl, any of which optionally bears up to 3 substituents independently selected from halogen, OH, CN, CF3, C1-4alkyl, C1-4alkoxy, amino, C1-4alkylamino and di(C1-4alkyl)amino; or two R3 groups attached to the same atom may complete a heterocycle of up to 6 ring atoms which optionally bears up to 3 substituents independently selected from halogen, OH, oxo, CN, CF3, C1-4alkoxy, amino, C1-4alkylamino and di(C1-4alkyl)amino; R4 has the same definition as R3 except that R4 is not H; and R5 is selected from the group consisting of: phenyl, hydroxy, C3-6cycloalkyl, and methoxy.
- Claim: 2. A compound according to claim 1, wherein: Z is —N(R1)—; X1 is selected from the group consisting of: H, halogen, phenyl, and a monocyclic or bicyclic ring system comprising up to 10 ring atoms, of which 1-3 are selected from N, O and S and the remainder are C, said phenyl and ring system bearing 0-3 substituents independently selected from halogen and C1-4alkyl, optionally substituted with up to 3 halogen atoms; X2 is selected from the group consisting of: H, halogen and phenyl bearing 0 to 5 halogen substituents; X3 is selected from the group consisting of: H, OR3, N(R3)2, C1-6alkyl and halogen; X4 is selected from the group consisting of: H, halogen, C3-6cycloalkyl and C1-6alkyl, optionally substituted with up to 3 halogen atoms; R2 is selected from: (i) H; (ii) C1-8alkyl or C2-8alkenyl, either of which optionally bears up to 3 substituents independently selected from halogen, OH, CN, CF3, OR3, SR4, SO2R4, SO2N(R3)2, COR3, CO2R3, CON(R3)2, N(R3)2, NR3COR4, NR3SO2R4 and phenyl, said phenyl bearing 0 to 5 halogen substituents; and (iii) C3-10cycloalkyl, C3-10cycloalkylC1-4alkyl, Het, HetC1-4alkyl, aryl or arylC1-4alkyl, any of which optionally bears up to 3 substituents independently selected from halogen, OH, oxo, CN, CF3, R4, OR3, SR4, SO2R4, SO2N(R3)2, COR3, CO2R3, CON(R3)2, N(R3)2, NR3COR4 and NR3SO2R4; where “aryl” refers to phenyl or 5- or 6-membered heteroaryl, either of which phenyl or heteroaryl is optionally fused to a 5- or 6-membered carbocycle or heterocycle, and “Het” refers to a nonaromatic mono- or bicyclic heterocyclic system of up to 10 ring atoms; or R1 and R2 together may complete a mono- or bicyclic heterocyclic system of up to 10 ring atoms which optionally bears up to 3 substituents independently selected from halogen, OH, oxo, CN, CF3, R4, OR3, SR4, SO2R4, SO2N(R3)2, COR3, CO2R3, CON(R3)2, N(R3)2, NR3COR4 and NR3SO2R4; each R3 independently represents H or C1-6alkyl which is optionally substituted with up to 3 halogen atoms or with OH, CN, CF3, C1-4alkoxy, amino, C1-4alkylamino or di(C1-4-alkyl)amino, or R3 represents phenyl, benzyl or 5- or 6-membered heteroaryl, any of which optionally bears up to 3 substituents independently selected from halogen, OH, CN, CF3, C1-4alkyl, C1-4alkoxy, amino, C1-4alkylamino and di(C1-4alkyl)amino; or two R3 groups attached to the same nitrogen atom may complete a heterocycle of up to 6 ring atoms which optionally bears up to 3 substituents independently selected from halogen, OH, oxo, CN, CF3, C1-4alkyl, C1-4alkoxy, amino, C1-4alkylamino and di(C1-4alkyl)amino; and R4 has the same definition as R3 except that R4 is not H.
- Claim: 3. A compound according to claim 2 wherein Y is CH.
- Claim: 4. A compound according to claim 2 wherein Y is N.
- Claim: 5. A compound according to claim 2 wherein X1 is phenyl bearing 0 to 3 halogen substituents.
- Claim: 6. A compound according to claim 2 wherein X1 is H.
- Claim: 7. A compound according to claim 2 wherein X1 is halogen.
- Claim: 8. A compound according to claim 2 wherein X1 is 1-methyl-1H-pyrazol-4-yl.
- Claim: 9. A compound according to claim 2 wherein X3 is H or methoxy.
- Claim: 10. A compound according to claim 2 wherein X4 is H, halogen or methyl.
- Claim: 11. A compound according to claim 2 wherein R1 is H.
- Claim: 12. A compound according to claim 2 wherein R2 is C3-10cycloalkyl bearing up to 3 substituents independently selected from halogen, OH, oxo, CN, CF3, R4, OR3, SR4, SO2R4, SO2N(R3)2, COR3, CO2R3, CON(R3)2, N(R3)2, NR3COR4 and NR3SO2R4.
- Claim: 13. A compound according to claim 2 wherein R2 is cyclohexyl bearing up to 3 substituents independently selected from halogen, OH, oxo, CN, CF3, R4, OR3, SR4, SO2R4, SO2N(R3)2, COR3, CO2R3, CON(R3)2, N(R3)2, NR3COR4 and NR3SO2R4.
- Claim: 14. A compound according to claim 2 wherein R2 is C1-8alkyl, which optionally bears up to 3 substituents independently selected from halogen, OH, CN, CF3, OR3, SR4, SO2R4, SO2N(R3)2, COR3, CO2R3, CON(R3)2, N(R3)2, NR3COR4, NR3SO2R4 and phenyl, said phenyl bearing 0 to 5 halogen substituents.
- Claim: 15. A compound according to claim 2 wherein: X1 is selected from the group consisting of H, halogen, phenyl bearing 0 to 3 halogen substituents and 1-methyl-1H-pyrazol-4-yl; X3 is H or methoxy; X4 is H, halogen or methyl; R1 is H; and R2 is selected from the group consisting of: (i) C1-8alkyl, which optionally bears up to 3 substituents independently selected from halogen, OH, CN, CF3, OR3, SR4, SO2R4, SO2N(R3)2, COR3, CO2R3, CON(R3)2, N(R3)2, NR3COR4, NR3SO2R4 and phenyl, said phenyl bearing 0 to 5 halogen substituents; and (ii) cyclohexyl bearing up to 3 substituents independently selected from halogen, OH, oxo, CN, CF3, R4, OR3, SR4, SO2R4, SO2N(R3)2, COR3, CO2R3, CON(R3)2, N(R3)2, NR3COR4 and NR3SO2R4.
- Claim: 16. A compound selected from the group consisting of: N-[(1R,6R)-6-amino-2,2-difluorocyclohexyl]-5-chloro-4-[6-fluorophenyl)pyrazolo[1,5-a]pyridin-3-yl]-1,3-thiazole-2-carboxamide; N-[(1R,6R)-6-amino-2,2-difluorocyclohexyl]-5-chloro-pyrazolo{1,5-a]pyridine-3-yl-1,3-thiazole-2-carboxamide; N-(2-amino-3,3,3-trifluoro-1-phenylpropyl)-5-chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-[(1R,2R)-2-amino-1,2-diphenylethyl)-5-chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-N-(2,2,2-trifluoroethyl)-1,3-thiazole-2-carboxamide; N-[2-amino-1-phenylethyl)-5-chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-amino-2,2-difluorocyclohexyl]-5-chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-[(1R,6R)-6-amino-2,2-difluorocyclohexyl]-5-bromo-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-[(1R,6R)-6-amino-2,2-difluorocyclohexyl]-5-chloro-4-fluoropyrazolo{1,5-a]pyridine-3-yl-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-amino-2,2-difluorocyclohexyl]-5-chloro-4-fluoropyrazolo{1,5-a]pyridine-3-yl-1,3-thiazole-2-carboxamide; N-[(1R,6R)-6-amino-2,2-difluorocyclohexyl]-5-methyl-pyrazolo{1,5-a]pyridine-3-yl-1,3-thiazole-2-carboxamide; N-[(1R,6R)-6-amino-2,2-difluorocyclohexyl]-4-(4-fluoropyrazolo[1,5-a]pyridin-3-yl)-5-methyl-1,3-thiazole-2-carboxamide; N-[(1R,6R)-6-amino-2,2-difluorocyclohexyl]-4-(6-chloropyrazolo[1,5-a]pyridin-3-yl)-5-methyl-1,3-thiazole-2-carboxamide; N-[(1R,6R)-6-amino-2,2-difluorocyclohexyl]-4-(6-bromopyrazolo[1,5-a]pyridin-3-yl)-5-methyl-1,3-thiazole-2-carboxamide; N-[(1R,2R)-2-amino-1,2-diphenylethyl]-5-methyl-4-pyrazolo[1,5-a]pyridin-3-yl]-1,3-thiazole-2-carboxamide; N-[(cis)-2-aminocyclohexyl]-5-methyl-4-pyrazolo[1,5-a]pyridin-3-yl]-1,3-thiazole-2-carboxamide; N-[(cis)-2-aminocyclohexyl]-5-methyl-4-[6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyridin-3-yl]-1,3-thiazole-2-carboxamide; N-(2-amino-1-phenylethyl)-5-methyl-4-[6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyridin-3-yl]-1,3-thiazole-2-carboxamide; N-[(1S,2S)-2-amino-1,2-diphenyl]-5-methyl-4-[6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyridin-3-yl]-1,3-thiazole-2-carboxamide; N-[(1R,6R)-6-amino-2,2-difluorocyclohexyl]-5-methyl-4-[6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyridin-3-yl]-1,3-thiazole-2-carboxamide; N-[(1S)-2-hydroxy-1-phenylethyl]-5-methyl-4-[6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyridin-3-yl]-1,3-thiazole-2-carboxamide; N-[(1S)-1-(2-chlorophenyl)-2-hydroxyethyl]-5-methyl-4-[6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyridin-3-yl]-1,3-thiazole-2-carboxamide; N-[(1S)-1-(3-chlorophenyl)-2-hydroxyethyl]-5-methyl-4-[6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyridin-3-yl]-1,3-thiazole-2-carboxamide; N-[(1S)-1-(3-chloro-5-fluorophenyl)-2-hydroxyethyl]-5-methyl-4-[6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyridin-3-yl]-1,3-thiazole-2-carboxamide; N-[(1S)-1-(4-chlorophenyl)-2-hydroxyethyl]-5-methyl-4-[6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyridin-3-yl]-1,3-thiazole-2-carboxamide; N-[(1S)-1-(3-fluorophenyl)-2-hydroxyethyl]-5-methyl-4-[6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyridin-3-yl]-1,3-thiazole-2-carboxamide; N-[(1S)-1-(4-chlorophenyl)-2-hydroxyethyl]-5-methyl-4-[6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyridin-3-yl]-1,3-thiazole-2-carboxamide; N-[(cis)-2-aminocyclohexyl]-4-(4-methoxy-6-[phenylpyrazolo{1,5-a]pyridine-3-yl)-2-thiophenecarboxamide; N-[(1R,6R)-6-amino-2,2-difluorocyclohexyl]-4-methoxy-6-phenylpyrazolo[1,5-a]pyridin-3-yl]-2-thiophenecarboxamide; 4-(4-methoxy-6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyridin-3-yl]-2-thiophenecarboxamide; N-[(1S)-2-hydroxy-1-phenylethyl]-4-methoxy-6-phenylpyrazolo[1,5-a]pyridin-3-yl]-2-thiophenecarboxamide; N-[(1S)-2-hydroxy-1-phenylethyl]-4-methoxy-6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyridin-3-yl]-2-thiophenecarboxamide; N-[(1R,6R)-6-amino-2,2-difluorocyclohexyl]-4-[6-fluorophenyl)pyrazolo[1,5-a]pyridin-3-yl]-5-methyl-2-thiophenecarboxamide; N-(3-amino-4,4,4-trifluorobutyl)-4-(4-methoxy-6-phenylpyrazolo[1,5-a]pyridin-3-yl]-2-thiophenecarboxamide; N-[(cis)-2-aminocyclohexyl]-4-pyrazolo[1,5-a]pyridin-3-yl]-2-thiophenecarboxamide; and N-[(1R,6R)-6-amino-2,2-difluorocyclohexyl]-5-chloro-4-pyrazolo[1,5-a]pyridin-3-yl-2-thiophenecarboxamide; or a pharmaceutically acceptable salt of any of the foregoing compounds.
- Claim: 17. A compound selected from the group consisting of: {4-[(5-Chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazol-2-yl)carbonyl]piperazin-2-yl}methanol; 3-(5-Chloro-2-{[2-(difluoromethyl)piperazin-1-yl]carbonyl}-1,3-thiazol-4-yl)pyrazolo[1,5-a]pyridine; {4-[(5-Chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazol-2-yl)carbonyl]morpholin-3-yl}methanol; 5-Chloro-N-(4-hydroxy-1,1-dioxidotetrahydro-3-thienyl)-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 3-(5-Chloro-2-{[2-(trifluoromethyl)piperazin-1-yl]carbonyl}-1,3-thiazol-4-yl)pyrazolo[1,5-a]pyridine; (3R,4R)-1-[(5-Chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazol-2-yl)carbonyl]-3-fluoropiperidin-4-amine; (3S,4R)-1-[(5-Chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazol-2-yl)carbonyl]-3-fluoropiperidin-4-amine; N-[(3R,4R)-4-amino-1-benzylpyrrolidin-3-yl]-5-chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 2-[(5-Chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazol-2-yl)carbonyl]-2,3-dihydro-1H-spiro[isoquinoline-4,4′-piperidine]; 5-Chloro-N-[(4-phenylpiperidin-4-yl)methyl]-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-Chloro-N-(2,3-dihydrospiro[indene-1,4′-piperidin]-3-yl)-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-Chloro-N-[(3S)-1-methylpyrrolidin-3-yl]-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-Chloro-4-pyrazolo[1,5-a]pyridin-3-yl-N-(1,2,3,4-tetrahydroisoquinolin-1-ylmethyl)-1,3-thiazole-2-carboxamide; {3-Amino-1-[(5-chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazol-2-yl)carbonyl]pyrrolidin-3-yl}methanol; 5-Chloro-N-piperidin-3-yl-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 1-[(5-Chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazol-2-yl)carbonyl]pyrrolidin-3-amine; 3-[5-Chloro-2-(piperazin-1-ylcarbonyl)-1,3-thiazol-4-yl]pyrazolo[1,5-a]pyridine; N-(2-Aminoethyl)-5-chloro-N-methyl-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-(2-Aminoethyl)-5-chloro-N-ethyl-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 1-[(5-Chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazol-2-yl)carbonyl]-N-methylpyrrolidin-3-amine; 3-{5-Chloro-2-[(2-methylpiperazin-1-yl)carbonyl]-1,3-thiazol-4-yl}pyrazolo[1,5-a]pyridine; N-[(1-Aminocyclopentyl)methyl]-5-chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-[(1-Aminocyclohexyl)methyl]-5-chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 1-[(5-Chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazol-2-yl)carbonyl]-1,2,3,4-tetrahydroquinolin-3-amine; N-(2-Amino-2-phenylethyl)-5-chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-(2-Aminoethyl)-5-chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-Chloro-4-pyrazolo[1,5-a]pyridin-3-yl-N-pyrrolidin-3-yl-1,3-thiazole-2-carboxamide; 3-{5-Chloro-2-[(3-methylpiperazin-1-yl)carbonyl]-1,3-thiazol-4-yl}pyrazolo[1,5-a]pyridine; N-(3-Aminocyclohexyl)-5-chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 3-{5-Chloro-2-[(3-methylpiperazin-1-yl)carbonyl]-1,3-thiazol-4-yl}pyrazolo[1,5-a]pyridine; N-(3-Aminocyclohexyl)-5-chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 1-{1-[(5-Chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazol-2-yl)carbonyl]-4-phenylpiperidin-4-yl}methanamine; N-(4-Amino-1,1-dioxidotetrahydro-3-thienyl)-5-chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-(2-Amino-2-methylpropyl)-5-chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-Chloro-N-(2-oxopiperidin-3-yl)-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-[(1S,2R)-2-aminocyclopentyl]-5-chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-[(1-aminocycloheptyl)methyl]-5-chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-5-chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-Chloro-N-(1-methyl-2-oxopyrrolidin-3-yl)-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-Chloro-N-(3,3-difluorocyclopentyl)-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-(2-Azetidin-1-yl-3,3,3-trifluoropropyl)-5-chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 3-[5-Chloro-2-(morpholin-4-ylcarbonyl)-1,3-thiazol-4-yl]pyrazolo[1,5-a]pyridine; 3-{5-Chloro-2-[(2,6-dimethylmorpholin-4-yl)carbonyl]-1,3-thiazol-4-yl}pyrazolo[1,5-a]pyridine; 3-{5-Chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1,3-thiazol-4-yl}pyrazolo[1,5-a]pyridine; 5-Chloro-N-(2-morpholin-4-ylethyl)-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 1-[(5-Chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazol-2-yl)carbonyl]piperidin-4-ol; 1-[(5-Chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-yl)carbonyl]-N,N-dimethylpiperidin-4-amine; 5-Chloro-N-[1-(hydroxymethyl)-2-methylpropyl]-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; Diethyl {1-[(5-chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-yl)carbonyl]piperidin-4-yl}phosphonate; 5-Chloro-N-(2-hydroxycyclopentyl)-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-Chloro-N-(2,3-dihydroxypropyl)-N-methyl-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-Chloro-N-(2-hydroxy-2-methylpropyl)-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 1-[(5-Chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazol-2-yl)carbonyl]-N,N-dimethylpiperidin-3-amine; 5-Chloro-N-(2-oxopyrrolidin-3-yl)-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-Chloro-N-[(3R)-1-isopropylpyrrolidin-3-yl]-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-Chloro-N-[(3S)-1-isopropylpyrrolidin-3-yl]-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-Chloro-N-[2-(dimethylamino)-3,3,3-trifluoropropyl]-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-Chloro-4-pyrazolo[1,5-a]pyridin-3-yl-N-[3,3,3-trifluoro-2-(3-fluoroazetidin-1-yl)propyl]-1,3-thiazole-2-carboxamide; 5-Chloro-N-(4-hydroxy-1,1-dioxidotetrahydro-3-thienyl)-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; (2S)-2-Anilino-2-phenylethyl 5-chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxylate; (2S)-2-Anilinopropyl 5-chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxylate; 5-Chloro-N-[(1S)-2-hydroxy-1-methylethyl]-N-phenyl-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-Chloro-N-phenyl-4-pyrazolo[1,5-a]pyridin-3-yl-N-(2,2,2-trifluoroethyl)-1,3-thiazole-2-carboxamide; 5-Chloro-N-isopropyl-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-Chloro-N-ethyl-N-methyl-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-Chloro-N-(2-hydroxyethyl)-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-Chloro-N-ethyl-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-Chloro-N-(2-methoxyethyl)-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 3-[5-Chloro-2-(piperidin-1-ylcarbonyl)-1,3-thiazol-4-yl]pyrazolo[1,5-a]pyridine; 5-Chloro-4-pyrazolo[1,5-a]pyridin-3-yl-N-pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-Chloro-N-cyclohexyl-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-Benzyl-5-chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-Chloro-4-pyrazolo[1,5-a]pyridin-3-yl-N-(pyridin-3-ylmethyl)-1,3-thiazole-2-carboxamide; 5-Chloro-4-pyrazolo[1,5-a]pyridin-3-yl-N-(2-thienylmethyl)-1,3-thiazole-2-carboxamide; 5-Chloro-4-pyrazolo[1,5-a]pyridin-3-yl-N-(2-pyrrolidin-1-ylethyl)-1,3-thiazole-2-carboxamide; 5-Chloro-1-(2,6-dimethylphenyl)-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 3-{2-[(4-Acetylpiperazin-1-yl)carbonyl]-5-chloro-1,3-thiazol-4-yl}pyrazolo[1,5-a]pyridine; 5-Chloro-N-(3-phenylpropyl)-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-Chloro-N-(3-chlorobenzyl)-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-Chloro-4-pyrazolo[1,5-a]pyridin-3-yl-N-quinolin-7-yl-1,3-thiazole-2-carboxamide; 5-Chloro-4-pyrazolo[1,5-a]pyridin-3-yl-N-[4-(trifluoromethyl)benzyl]-1,3-thiazole-2-carboxamide; 3-{2-[(4-Benzylpiperidin-1-yl)carbonyl]-5-chloro-1,3-thiazol-4-yl}pyrazolo[1,5-a]pyridine; 3-(5-Chloro-2-{[4-(3-methoxyphenyl)piperazin-1-yl]carbonyl}-1,3-thiazol-4-yl)pyrazolo[1,5-a]pyridine; 5-Chloro-N-ethyl-N-phenyl-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-Chloro-N-isopropyl-N-phenyl-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-(2-Anilinocyclohexyl)-5-chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-Chloro-N-methyl-N-(3-methylphenyl)-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 3-(5-Chloro-2-{[3-(methylsulfonyl)pyrrolidin-1-yl]carbonyl}-1,3-thiazol-4-yl)pyrazolo[1,5-a]pyridine; N-[(1R)-1-(Aminomethyl)-2,2,2-trifluoroethyl]-5-chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-(2-Aminoethoxy)-5-chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-[(1S)-1-(Aminomethyl)-2,2,2-trifluoroethyl]-5-chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-Chloro-N-(2-hydroxyethoxy)-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-(2-Anilinocyclohexyl)-5-chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-Chloro-N-(2,4-difluorophenyl)-N-methyl-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-Chloro-N-(2,5-difluorophenyl)-N-methyl-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-Chloro-N-(2,3-difluorophenyl)-N-methyl-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-Chloro-N-(4-chlorophenyl)-N-methyl-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-(3-Aminophenyl)-5-chloro-N-methyl-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-Chloro-N-methyl-N-(4-methylphenyl)-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-Chloro-N-methyl-4-pyrazolo[1,5-a]pyridin-3-yl-N-pyridin-2-yl-1,3-thiazole-2-carboxamide; 5-Chloro-N-(2,6-difluorophenyl)-N-methyl-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-Chloro-N-methyl-N-(3-methylphenyl)-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-Chloro-4-pyrazolo[1,5-a]pyridin-3-yl-N-(2,2,2-trifluoroethyl)-1,3-thiazole-2-carboxamide; 5-Chloro-N-(3-hydroxyphenyl)-N-methyl-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-[(1R,6R)-2-Aminocyclohexyl]-5-chloro-4-[(6-trifluoromethyl)pyrazolo[1,5-a]pyridin-3-yl]-1,3-thiazole-2-carboxamide; 5-Chloro-N-(2-chlorophenyl)-N-methyl-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-Chloro-N-methyl-N-(2-methylphenyl)-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-Chloro-N-(4-fluorophenyl)-N-methyl-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-Chloro-N-(3-chlorophenyl)-N-methyl-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-Chloro-N-(3-fluorophenyl)-N-methyl-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-[(1S,6S)-2-Aminocyclohexyl]-5-chloro-4-[(6-trifluoromethyl)pyrazolo[1,5-a]pyridin-3-yl]-1,3-thiazole-2-carboxamide; 5-Chloro-N-(2-chlorophenyl)-N-methyl-4-pyrazolo pyridin-3-yl-1,3-thiazole-2-carboxamide; {4-[(5-Chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazol-2-yl)carbonyl]morpholin-2-yl}methanol; 1-[(5-Chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazol-2-yl)carbonyl]-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine; 5-Chloro-N-(3-fluorophenyl)-N-methyl-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-[1-(Aminomethyl)-6-fluoro-2,3-dihydro-1H-inden-1-yl]-5-chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-Chloro-N-methyl-N-phenyl-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-amino-2,2-difluorocyclohexyl]-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 3-[2-(Piperidin-1-ylcarbonyl)-1,3-thiazol-4-yl]pyrazolo[1,5-a]pyridine; N-[1-(Aminomethyl)-5-fluoro-2,3-dihydro-1H-inden-1-yl]-5-chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-[1-(Aminomethyl)-4-fluoro-2,3-dihydro-1H-inden-1-yl]-5-chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-[1-(Aminomethyl)-2,3-dihydro-1H-inden-1-yl]-5-chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-(2-Amino-3,3,3-trifluoro-1-phenylpropyl)-5-chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-(2-Amino-3,3,3-trifluoro-1-phenylpropyl)-5-chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-[(1S)-1-(Aminomethyl)-2,2,2-trifluoro-1-methylethyl]-5-chloro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 5-Chloro-N-(2-fluorophenyl)-N-methyl-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-[(1R,2S)-2-amino-6,6-difluoro-2-methylcyclohexyl]-5-chloro-4-(pyrazolo[1,5-a]pyridin-3-yl)-1,3-thiazole-2-carboxamide; 5-Chloro-N-[(1R,6S)-2,2-difluoro-6-hydroxycyclohexyl]-4-(pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-5-chloro-4-(6-iodopyrazolo[1,5-a]pyridin-3-yl)-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-4-(6-bromopyrazolo[1,5-a]pyridin-3-yl)-5-chloro-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-5-chloro-4-[5-(trifluoromethyl)pyrazolo[1,5-a]pyridin-3-yl]-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-5-chloro-4-[(6-trifluoromethyl)pyrazolo[1,5-a]pyridin-3-yl]-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-5-chloro-4-(6-methoxypyrazolo[1,5-a]pyridin-3-yl)-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-5-chloro-4-(6-ethylpyrazolo[1,5-a]pyridin-3-yl)-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-5-chloro-4-(5-cyanopyrazolo[1,5-a]pyridin-3-yl)-1,3-thiazole-2-carboxamide; 3-[2-({[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]amino}carbonyl)-5-chloro-1,3-thiazol-4-yl]pyrazolo[1,5-a]pyridine-5-carboxamide; N-[(1R,6S)-6-amino-2,2-difluorocyclohexyl]-5-chloro-4-(6-fluoropyrazolo[1,5-a]pyridin-3-yl)-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-amino-2,2-difluorocyclohexyl]-5-chloro-4-(5-chloropyrazolo[1,5-a]pyridin-3-yl)-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-5-chloro-4-(5-methylpyrazolo[1,5-a]pyridin-3-yl)-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-5-chloro-4-(5-chloro-6-fluoropyrazolo[1,5-a]pyridin-3-yl)-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-4-(6-ethylpyrazolo[1,5-a]pyridin-3-yl)-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-4-(5-chloro-6-fluoropyrazolo[1,5-a]pyridin-3-yl)-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-4-(6-methoxypyrazolo[1,5-a]pyridin-3-yl)-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-4-(5-cyanopyrazolo[1,5-a]pyridin-3-yl)-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-4-(6-iodopyrazolo[1,5-a]pyridin-3-yl)-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-4-(6-isopropenylpyrazolo[1,5-a]pyridin-3-yl)-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-4-(5-chloropyrazolo[1,5-a]pyridin-3-yl)-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-4-(6-cyanopyrazolo[1,5-a]pyridin-3-yl)-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-4-[6-methoxy-5-(trifluoromethyl)pyrazolo[1,5-a]pyridin-3-yl]-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-4-{6-[(trimethyl Silyl)ethynyl]pyrazolo[1,5-a]pyridin-3-yl}-1,3-thiazole-2-carboxamide; N-[(1R,6R)-6-Amino-2,2-difluorocyclohexyl]-5-chloro-4-(4,6-difluoropyrazolo[1,5-a]pyridin-3-yl)-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-4-(4-chloro-6-methoxypyrazolo[1,5-a]pyridin-3-yl)-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-4-(6-ethylpyrazolo[1,5-a]pyridin-3-yl)-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-4-(5-chloro-6-fluoropyrazolo[1,5-a]pyridin-3-yl)-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-4-(6-methoxypyrazolo[1,5-a]pyridin-3-yl)-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-5-chloro-4-(6-cyclopropylpyrazolo[1,5-a]pyridin-3-yl)-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-5-ethyl-4-(6-fluoropyrazolo[1,5-a]pyridin-3-yl)thiophene-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-5-isopropyl-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-[(1R,6R)-6-Amino-2,2-difluorocyclohexyl]-5-isopropyl-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-amino-2,2-difluorocyclohexyl]-5-ethyl-4-[6-(trifluoromethyl)pyrazolo[1,5-a]pyridin-3-yl]thiophene-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-5-ethyl-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-5-methyl-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-4-(6-fluoropyrazolo[1,5-a]pyridin-3-yl)-5-methyl-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-4-(4,6-difluoropyrazolo[1,5-a]pyridin-3-yl)-5-methylthiophene-2-carboxamide; N-[(trans)-4-Amino-1,1-dioxidotetrahydro-2H-thiopyran-3-yl]-5-methyl-4-(pyrazolo[1,5-a]pyridin-3-yl) thiophene-2-carboxamide; N-[(cis)-4-Amino-1,1-dioxidotetrahydro-2H-thiopyran-3-yl]-5-methyl-4-(pyrazolo[1,5-a]pyridin-3-yl) thiophene-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-5-ethyl-4-[6-(trifluoromethyl)pyrazolo[1,5-a]pyridin-3-yl]thiophene-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-5-ethyl-4-(6-fluoropyrazolo[1,5-a]pyridin-3-yl)thiophene-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-4-(4,6-difluoropyrazolo[1,5-a]pyridin-3-yl)-5-methylthiophene-2-carboxamide; N-[(trans)-4-amino-1,1-dioxidotetrahydro-2H-thiopyran-3-yl]-5-chloro-4-(pyrazolo[1,5-a]pyridin-3-yl) thiophene-2-carboxamide; N-[(cis)-4-amino-1,1-dioxidotetrahydro-2H-thiopyran-3-yl]-5-chloro-4-(pyrazolo[1,5-a]pyridin-3-yl) thiophene-2-carboxamide; N-[(trans)-3-amino-1,1-dioxidotetrahydro-2H-thiopyran-4-yl]-5-chloro-4-(pyrazolo[1,5-a]pyridin-3-yl) thiophene-2-carboxamide; N-[(cis)-3-amino-1,1-dioxidotetrahydro-2H-thiopyran-4-yl]-5-chloro-4-(pyrazolo[1,5-a]pyridin-3-yl) thiophene-2-carboxamide; N-[(1R,6R)-6-Amino-2,2-difluorocyclohexyl]-5-(phenylethynyl)-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-[(1R,6R)-6-Amino-2,2-difluorocyclohexyl]-5-(3-hydroxy-3-methylbut-1-yn-1-yl)-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-[(1R,6R)-6-Amino-2,2-difluorocyclohexyl]-5-ethynyl-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-[(1R,6R)-6-Amino-2,2-difluorocyclohexyl]-5-(cyclopropylethynyl)-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-[(1R,6R)-6-Amino-2,2-difluorocyclohexyl]-5-(3-methoxyprop-1-yn-1-yl)-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-[(1R,6R)-6-amino-2,2-difluorocyclohexyl]-5-cyclopent-1-en-1-yl-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-5-isopropenyl-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-5-isopropenyl-4-[6-(trifluoromethyl)pyrazolo[1,5-a]pyridin-3-yl]-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-4-pyrazolo[1,5-a]pyridin-3-yl-5-vinyl-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-4-(6-fluoropyrazolo[1,5-a]pyridin-3-yl)-5-isopropenyl-1,3-thiazole-2-carboxamide; N-[(1R,6R)-6-amino-2,2-difluorocyclohexyl]-5-[(1E)-but-1-en-1-yl]-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-[(1R,6R)-6-Amino-2,2-difluorocyclohexyl]-4-pyrazolo[1,5-a]pyridin-3-yl-5-vinyl-1,3-thiazole-2-carboxamide; N-[(1R,6R)-6-amino-2,2-difluorocyclohexyl]-5-(2-methylprop-1-en-1-yl)-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-[(1R,6R)-6-amino-2,2-difluorocyclohexyl]-5-[(E)-2-cyclohexylvinyl]-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-[(1R,6R)-6-amino-2,2-difluorocyclohexyl]-5-[(E)-2-cyclopropylvinyl]-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-amino-2,2-difluorocyclohexyl]-5-cyclopropyl-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-[(1R,6R)-6-amino-2,2-difluorocyclohexyl]-5-cyano-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-amino-2,2-difluorocyclohexyl]-5-(difluoromethyl)-4-pyrazolo[1,5-a]pyridin-3-ylthiophene-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-5-(difluoromethyl)-4-(6-fluoropyrazolo[1,5-a]pyridin-3-yl)-1,3-thiazole-2-carboxamide; N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-5-(difluoromethyl)-4-[6-(trifluoromethyl)pyrazolo[1,5-a]pyridin-3-yl]-1,3-thiazole-2-carboxamide; N-[(1R,6R)-6-Amino-2,2-difluorocyclohexyl]-5-nitro-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; 2-(Piperidin-1-ylcarbonyl)-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazol-5-amine; and N-[(1R,6S)-6-Amino-2,2-difluorocyclohexyl]-5-(dimethylamino)-4-pyrazolo[1,5-a]pyridin-3-yl-1,3-thiazole-2-carboxamide; or a pharmaceutically acceptable salt of any of the foregoing compounds.
- Claim: 18. A compound according to claim 1 according to Formula Ia [chemical expression included] or a pharmaceutically acceptable salt or hydrate thereof.
- Claim: 19. A pharmaceutical composition comprising a compound of formula I as defined in claim 1 or a pharmaceutically acceptable salt or hydrate thereof, and a pharmaceutically acceptable carrier.
- Claim: 20. A method for treating or preventing a neurodegenerative disease associated with hyperphosphorylation of tau in a human patient, said method comprising administering to said patient an effective amount of a compound of formula I as defined in claim 1 or a pharmaceutically acceptable salt or hydrate thereof.
- Claim: 21. The method according to claim 20 wherein the neurodegenerative disease is Alzheimer's disease.
- Claim: 22. A method for reducing the production of hyperphosphorylated tau in a human patient, said method comprising administering to said patient an effective amount of a compound of formula I as defined in claim 1 or a pharmaceutically acceptable salt or hydrate thereof.
- Current U.S. Class: 514/80
- Current International Class: 61; 07; 61; 61; 07; 61; 07; 61; 61; 07; 61; 61
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