DK2344492T3 - Pyrazolopyridinderivater som NADPH-oxidaseinhibitorer - Google Patents

Pyrazolopyridinderivater som NADPH-oxidaseinhibitorer Download PDF

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DK2344492T3
DK2344492T3 DK09787271.7T DK09787271T DK2344492T3 DK 2344492 T3 DK2344492 T3 DK 2344492T3 DK 09787271 T DK09787271 T DK 09787271T DK 2344492 T3 DK2344492 T3 DK 2344492T3
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optionally substituted
pyrazolo
methyl
pyridine
dione
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Patrick Page
Mike Orchard
Benoît Laleu
Francesca Gaggini
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Genkyotex Sa
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Claims (16)

1. Pyrazolopyridinderivat med fnrmlfin l:
(i) hvori Gi er valgt blandt H; eventuelt substitueret acyl; eventuelt substitueret acyl-Cr C6-alkyl; eventuelt substitueret alkyl-C3-C8-cycloalkylalkyl; eventuelt substitueret heterocycloalkylalkyl; eventuelt substitueret arylalkyl; og eventuelt substitueret heteroarylalkyl; G2 er valgt blandt H; eventuelt substitueret C-|-C6-alkyl; eventuelt substitueret C2-C6-alkenyl; eventuelt substitueret C2-C6-alkynyl; eventuelt substitueret aryl; eventuelt substitueret CrC6-alkylaryl; eventuelt substitueret aryl-CrC6-alkyl; eventuelt substitueret heteroaryl; eventuelt substitueret alkylheteroaryl; eventuelt substitueret heteroaryl-CrC6-alkyl; eventuelt substitueret C2-C6-alkenylaryl; eventuelt substitueret aryl-C2-C6-alkenyl; eventuelt substitueret C2-C6-alkenylheteroaryl; eventuelt substitueret heteroaryl-C2-C6-alkenyl; eventuelt substitueret C3-C8-cycloalkyl; eventuelt substitueret heterocycloalkyl; eventuelt substitueret alkyl-C3-C8-cycloalkyl; eventuelt substitueret C3-C8-cycloalkyl-CrC6-alkyl; eventuelt substitueret CrC6- alkylheterocycloalkyl og eventuelt substitueret heterocycloalkyl-C-i-C6-alkyl; G3 er valgt blandt H; eventuelt substitueret amino; eventuelt substitueret aminoalkyl; eventuelt substitueret aminocarbonyl; eventuelt substitueret alkoxy; eventuelt substitueret alkoxy-CrC6-alkyl; eventuelt substitueret carbonyl; eventuelt substitueret Ci-C6-alkyl; eventuelt substitueret C2-C6-alkenyl; eventuelt substitueret C2-C6-alkynyl; eventuelt substitueret aryl; eventuelt substitueret aryl-CrC6-alkyl; eventuelt substitueret heteroaryl; eventuelt substitueret C-i-C6-alkylheteroaryl; eventuelt substitueret heteroaryl-C-i-C6-alkyl; eventuelt substitueret C2-C6-alkenylaryl; eventuelt substitueret aryl-C2-C6-alkenyl; eventuelt substitueret C2-C6-alkenylheteroaryl; eventuelt substitueret heteroaryl-C2-C6-alkenyl; eventuelt substitueret C3-C8-cycloalkyl; eventuelt substitueret heterocycloalkyl; eventuelt substitueret CrCe-alkyl-Cs-Cs-cycloalkyl; eventuelt substitueret C3-C8-cycloalkyl-CrC6-alkyl; eventuelt substitueret CrC6- alkylheterocycloalkyl og eventuelt substitueret heterocycloalkyl-C-i-C6-alkyl; G4 er valgt blandt -NR2-C(0)-R1 og -(CHR3)m-(CH2)n-R4, hvori R1 er valgt blandt H; amino; -NR5R6; 62 eventuelt substitueret alkoxy; eventuelt substitueret alkoxy-C-i-C6-alkyl; eventuelt substitueret aryl; eventuelt substitueret C-i-C6-alkylaryl; eventuelt substitueret aryl-C-i-C6-alkyl; heteroaryl; eventuelt substitueret C-i-C6-alkylheteroaryl; eventuelt substitueret heteroaryl-CrC6-alkyl; eventuelt substitueret C3-C8-cycloalkyl; eventuelt substitueret Ci-C6-alkyl-C3-C8-cycloalkyl; eventuelt substitueret C3-C8-cycloalkyl-Ci-C6-alkyl; eventuelt substitueret heterocycloalkyl; eventuelt substitueret Ci-C6-alkylhetero-cycloalkyl; og eventuelt substitueret heterocycloalkyl-Ci-C6-alkyl; R2 er valgt blandt H; eventuelt substitueret alkoxy-C-i-C6-alkyl; eventuelt substitueret aryl; eventuelt substitueret C-|-C6-alkylaryl; eventuelt substitueret aryl-C-|-C6-alkyl; eventuelt substitueret heteroaryl; eventuelt substitueret C-i-C6-alkylheteroaryl; eventuelt substitueret heteroaryl-C-i-C6-alkyl; eventuelt substitueret C3-C8-cycloalkyl; eventuelt substitueret CrCe-alkyl-Cs-Cs-cycloalkyl; eventuelt substitueret Cs-Cs-cycloalkyl-CrCe-alkyl; eventuelt substitueret heterocycloalkyl; eventuelt substitueret CrC6-alkylheterocycloalkyl; eventuelt substitueret heterocycloalkyl-Ci-C6-alkyl; R3 er valgt blandt H; halogen; eventuelt substitueret alkoxy; eventuelt substitueret alkoxy-CrC6-alkylaryl; eventuelt substitueret CrC6-alkylaryl; eventuelt substitueret aryl-Ci-C6-alkyl; eventuelt substitueret heteroaryl; eventuelt substitueret Ci-C6-alkylheteroaryl; eventuelt substitueret heteroaryl-CrC6-alkyl; eventuelt substitueret C3-C8-cycloalkyl; eventuelt substitueret Ci-C6-alkyl-C3-C8-cycloalkyl; eventuelt substitueret C3-C8-cycloalkyl-Ci-C6-alkyl; heterocycloalkyl; eventuelt substitueret CrC6-alkylhetero-cycloalkyl; og eventuelt substitueret heterocycloalkyl-C-|-C6-alkyl; R4 er valgt blandt H; -C(0)R7; -A-B; -CHR8R9 og -(CH2)q-E; R5 og R6 indbyrdes uafhængigt er valgt blandt H; eventuelt substitueret alkoxy-Ci-C6-alkyl; eventuelt substitueret aryl; eventuelt substitueret CrC6-alkylaryl; eventuelt substitueret aryl-CrC6-alkyl; eventuelt substitueret heteroaryl; eventuelt substitueret Ci-C6-alkylheteroaryl; eventuelt substitueret heteroaryl-CrC6-alkyl; eventuelt substitueret C3-C8-cycloalkyl; eventuelt substitueret CrC6-alkyl-C3-C8-cycloalkyl; eventuelt substitueret C3-C8-cycloalkyl-CrC6-alkyl; eventuelt substitueret heterocycloalkyl; eventuelt substitueret CrC6-alkylhetero-cycloalkyl; og eventuelt substitueret heterocycloalkyl-Ci-C6-alkyl, eller -NR5R6 tilsammen danner en ring valgt blandt eventuelt substitueret heteroaryl og eventuelt substitueret heterocycloalkyl; R7 er valgt blandt eventuelt substitueret amino; eventuelt substitueret alkoxy; eventuelt substitueret aminoalkyl; eventuelt substitueret alkoxy-C-i-C6-alkyl; eventuelt substitueret CrC6-alkyl; eventuelt substitueret C2-C6-alkenyl; eventuelt substitueret C2-C6-alkynyl; -NR5R6; eventuelt substitueret aryl; eventuelt substitueret CrC6-alkylaryl; eventuelt substitueret aryl-CrC6-alkyl; eventuelt substitueret heteroaryl; eventuelt substitueret CrC6-alkylheteroaryl; eventuelt substitueret heteroaryl-CrCe-alkyl; eventuelt substitueret C3-C8-cycloalkyl; eventuelt substitueret CrCe-alkyl-Cs-Ce-cycloalkyl; eventuelt substitueret C3-C8-cycloalkyl-CrC6-alkyl; eventuelt substitueret heterocycloalkyl; eventuelt substitueret CrC6-alkylheterocycloalkyl; og eventuelt substitueret heterocycloalkyl-Ci-C6-alkyl; R8 og R9 indbyrdes uafhængigt er valgt blandt eventuelt substitueret aryl; eventuelt substitueret heteroaryl; eventuelt substitueret C3-C8-cycloalkyl og eventuelt substitueret heterocycloalkyl; R10 er valgt blandt eventuelt substitueret aryl; og eventuelt substitueret heteroaryl; R11 og R12 indbyrdes uafhængigt er valgt blandt H; eventuelt substitueret acyl; eventuelt substitueret Ci-C6-alkyl; eventuelt substitueret C2-C6-alkenyl; eventuelt substitueret C2-C6-alkynyl; eventuelt substitueret aryl; eventuelt substitueret CrCe-alkylaryl; eventuelt substitueret aryl-Ci-Ce-alkyl; eventuelt substitueret heteroaryl; eventuelt substitueret CVCe-alkylheteroaryl; eventuelt substitueret heteroaryl-CrC6-alkyl; eventuelt substitueret C3-C8-cycloalkyl; eventuelt substitueret CrC6-alkyl-C3-C8-cycloalkyl; eventuelt substitueret C3-C8-cycloalkyl-Ci-C6-alkyl; eventuelt substitueret heterocycloalkyl; eventuelt substitueret CrC8-alkylhetero-cycloalkyl; og eventuelt substitueret heterocycloalkyl-CrC6-alkyl, eller -NR11R12 tilsammen danner en ring valgt blandt eventuelt substitueret heteroaryl og eventuelt substitueret heterocycloalkyl; R13 er valgt blandt eventuelt substitueret aryl; eventuelt substitueret heteroaryl; eventuelt substitueret C3-C8-cycloalkyl og eventuelt substitueret heterocycloalkyl; R14, R15 og R16 indbyrdes uafhængigt er valgt blandt H og eventuelt substitueret Ci-C6-alkyl; R17 er valgt blandt eventuelt substitueret C-|-C6-alkyl; eventuelt substitueret C2-C6-alkenyl; eventuelt substitueret C2-C6-alkynyl; aryl; eventuelt substitueret CrC6-alkylaryl; eventuelt substitueret aryl-CrC6-alkyl; eventuelt substitueret heteroaryl; eventuelt substitueret CrC6-alkylheteroaryl; eventuelt substitueret heteroaryl-CrC6-alkyl; eventuelt substitueret C3-C8-cycloalkyl; eventuelt substitueret CrC6-alkyl-C3-C8-cycloalkyl; eventuelt substitueret C3-C8-cycloalkyl-CrC6-alkyl; eventuelt substitueret heterocycloalkyl; eventuelt substitueret CrC6-alkylheterocycloalkyl; og eventuelt substitueret heterocycloalkyl-CrC6-alkyl; A er valgt blandt eventuelt substitueret aryl, og eventuelt substitueret heteroaryl; B er valgt blandt -OR10, -NR11R12 og -(CH2)P-R13; E er valgt blandt eventuelt substitueret C3-C8-cycloalkyl; eventuelt substitueret C2-C6-alkynyl; -NR14R15; -(CH2)r-OR15 og NR16C(0)-R17; m, n, p og q er hele tal valgt blandt 0 til 5; r er et helt tal valgt blandt 3 til 5; G5 er valgt blandt H; eventuelt substitueret CrC6-alkyl; eventuelt substitueret C2-C6-alkenyl; eventuelt substitueret C2-C6-alkynyl; eventuelt substitueret aryl; eventuelt substitueret Ci-C6-alkylaryl; eventuelt substitueret aryl-CrC6-alkyl; eventuelt substitueret heteroaryl; eventuelt substitueret CrC6-alkylheteroaryl; eventuelt substitueret heteroaryl-CrC6-alkyl; eventuelt substitueret C2-C6-alkenylaryl; eventuelt substitueret aryl-C2-C6-alkenyl; eventuelt substitueret C2-C6-alkenylheteroaryl; eventuelt substitueret heteroaryl-C2-C6-alkenyl; eventuelt substitueret C3-C8-cycloalkyl; eventuelt substitueret heterocycloallcyl; eventuelt substitueret Ci-C6-alkyl-C3-C8-cycloalkyl; eventuelt substitueret C3-C8-cycloalkyl-CrC6-alkyl; eventuelt substitueret CrC6-alkylheterocycloalkyl og eventuelt substitueret heterocycloalkyl-CrC6-alkyl; samt farmaceutisk acceptable salte deraf.
2. Derivat ifølge krav 1, hvori Gi er H.
3. Derivat ifølge krav 1 eller 2, hvori G3 er CrC6-alkyl.
4. Derivat ifølge krav 1 eller 2, hvori G3 er amino.
5. Derivat ifølge et hvilket som helst af de foregående krav, hvori G4 er -NR2-C(0)-R1; R1 og R2 er som defineret i et hvilket som helst af de foregående krav.
6. Derivat ifølge et hvilket som helst af kravene 1 til 4, hvori G4 er -(CHR3)m-(CH2)n-R4; R3, R4, m og n er som defineret i et hvilket som helst af de foregående krav.
7. Derivat ifølge krav 1 eller 6, hvori R4 er -C(0)R7; R7 er som defineret i et hvilket som helst af de foregående krav.
8. Derivat ifølge krav 1 eller 6, hvori R4 er -A-B; A og B er som defineret i et hvilket som helst af de foregående krav.
9. Derivat ifølge krav 1 eller 6, hvori R4 er -CHR8R9; R8 og R9 er som defineret i et hvilket som helst af de foregående krav.
10. Derivat ifølge krav 1 eller 6, hvori R4 er -(CH2)q-E; E og q er som defineret i et hvilket som helst af de foregående krav.
11. Derivat ifølge et hvilket som helst af de foregående krav, hvori G5 er H.
12. Derivat ifølge et hvilket som helst af kravene 1 til 11 valgt blandt følgende gruppe: 2-(2-chlorphenyl)-4-methyl-5-(2-morpholin-4-ylbenzyl)-1H-pyrazolo[4,3-c]pyridin- 3,6(2H,5H)-dion; 2-(2-chlorphenyl)-4-methyl-5-{4-[(4-methylpiperazin-1-yl)methyl]benzyl}-1H-pyrazolo- [4,3-c]pyridin-3,6(2H,5H)-dion; 2-(2-chlorphenyl)-4-methyl-5-(2-morpholin-4-yl-2-phenylethyl)-1H-pyrazolo[4,3-c]- pyridin-3,6(2H,5H)-dion; 2-(2-chlorphenyl)-5-[2-(4-hydroxyphenyl)ethyl]-4-methyl-1H-pyrazolo[4,3-c]pyridin- 3,6(2H,5H)-dion; 5-(3-ethoxypropyl)-4-methyl-2-(4-phenyl-1,3-thiazol-2-yl)-1H-pyrazolo[4,3-c]pyridin- 3,6(2H,5H)-dion; 2-(2-chlorphenyl)-4,5-dimethyl-1H-pyrazolo[4,3-c]pyridin-3,6(2H,5H)-dion; 2-(2-fluorphenyl)-4,5-dimethyl-1H-pyrazolo[4,3-c]pyridin-3,6(2H,5H)-dion; 4- methyl-5-(3-phenoxybenzyl)-2-(4-phenyl-1,3-thiazol-2-yl)-1H-pyrazolo[4,3-c]pyridin-3,6(2H,5H)-dion; 4,5-dimethyl-2-(4-phenyl-1,3-thiazol-2-yl)-1H-pyrazolo[4,3-c]pyridin-3,6(2H,5H)-dion; 2-(3-chlorphenyl)-4,5-dimethyl-1H-pyrazolo[4,3-c]pyridin-3,6(2H,5H)-dion; N-[2-(2-chlorphenyl)-4-methyl-3,6-dioxo-1,2,3,6-tetrahydro5H-pyrazolo[4,3-c]pyridin- 5- yl]-2-(4-fluorphenoxy)acetamid; 2-(2-chlorphenyl)-4-methyl-5-(3-phenoxybenzyl)-1H-pyrazolo[4,3-c]pyridin-3,6(2H,5H)- dion; 5-(3-ethoxypropyl)-2-(2-fluorphenyl)-4-methyl-1H-pyrazolo[4,3-c]pyridin-3,6(2H,5H)- dion; 2-(3-chlorphenyl)-5-(3-ethoxypropyl)-4-methyl-1H-pyrazolo[4,3-c]pyridin-3,6(2H,5H)- dion; 2-(3-chlorphenyl)-4-methyl-5-[2-(morpholin-4-ylmethyl)benzyl]-1H-pyrazolo[4,3-c]- pyridin-3,6(2H,5H)-dion; 2-(2-fluorphenyl)-4-methyl-5-[2-(morpholin-4-ylmethyl)benzyl]-1H-pyrazolo[4,3-c]- pyridin-3,6(2H,5H)-dion; 2-(2-fluorphenyl)-4-methyl-5-[(6-morpholin-4-ylpyridin-2-yl)methyl]-1H-pyrazolo[4,3-c]- pyridin-3!6(2H,5H)-dion; 2-(2-fluorphenyl)-4-methyl-5-[4-(morpholin-4-ylmethyl)benzyl]-1H-pyrazolo[4,3-c]- pyridin-3,6(2H,5H)-dion; 2- (3-chlorphenyl)-4-methyl-5-[(6-morpholin-4-ylpyridin-2-yl)methyl]-1H-pyrazolo[4,3-3]pyridin-3,6(2H,5H)-dion; 3- (4,5-dimethyl-3,6-dioxo-1,3,5,6-tetrahydro-2H-pyrazolo[4,3-c]pyridin-2-yl)benzonitril; 2-(2-fluorphenyl)-4-methyl-5-(3-phenoxybenzyl)-1H-pyrazolo[4,3-c]pyridin-3,6(2H,5H)- dion; 2-(3-chlorphenyl)-4-methyl-5-(3-phenoxybenzyl)-1H-pyrazolo[4,3-c]pyridin-3,6(2H,5H)- dion; 2-(2-chlorphenyl)-5-(3-ethoxypropyl)-4-methyl-1H-pyrazolo[4,3-c]pyridin-3,6(2H,5H)- dion; 2-(2-chlorphenyl)-4-methyl-5-[(6-morpholin-4-ylpyridin-2-yl)methyl]-1H-pyrazolo[4,3- c]pyridin-3,6(2H,5H)-dion; 2-(3-chlorphenyl)-4-methyl-5-[4-(4-methylpiperazin-1-yl)-4-oxobutyl]-1H-pyrazolo[4,3- c]pyridin-3,6(2H,5H)-dion; 2-(3-chlorphenyl)-4-methyl-5-[4-(morpholin-4-ylmethyl)benzyl]-1H-pyrazolo[4,3-c]- pyridin-3,6(2H,5H)-dion; 2-[2-(2-fluorphenyl)-4-methyl-3,6-dioxo-1,2,3,6-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5- yl]-N-(pyridin-2-ylmethyl)acetamid; 2-(2-chlorphenyl)-4-methyl-5-[4-(morpholin-4-ylmethyl)benzyl]-1H-pyrazolo[4,3-c]- pyridin-3,6(2H,5H)-dion; 2- (2-chlorphenyl)-4-methyl-5-[2-(morpholin-4-ylmethyl)benzyl]-1H-pyrazolo[4,3-c]-pyridin-3,6(2H,5H)-dion; 4- methyl-5-(3-phenoxybenzyl)-2-[1,2,4]triazolo[4,3-b]pyridazin-6-yl-1H-pyrazolo[4,3-c]-pyridin-3,6(2H,5H)-dion; 3- [5-(3-ethoxypropyl)-4-methyl-3,6-dioxo-1,3,5,6-tetrahydro-2H-pyrazolo[4,3-c]pyridin-2-yl]benzonitril; 2-[4-(benzyloxy)phenyl]-4,5-dimethyl-1H-pyrazolo[4,3-c]pyridin-3,6(2H,5H)-dion; 2-[4-(benzyloxy)phenyl]-4-methyl-5-(3-phenoxybenzyl)-1H-pyrazolo[4,3-c]pyridin- 3,6(2H,5H)-dion; 2- [4-(benzyloxy)phenyl]-5-(3-ethoxypropyl)-4-methyl-1H-pyrazolo[4,3-c]pyridin-3,6(2H,5H)-dion; 3- {4-methyl-5-[4-(morpholin-4-ylmethyl)benzyl]-3,6-dioxo-1,3,5,6-tetrahydro-2H-pyrazolo[4,3-c]pyridin-2-yl}benzonitril; 2-(2-chlorphenyl)-5-(3-hydroxypropyl)-4-methyl-1H-pyrazolo[4,3-c]pyridin-3,6(2H,5H)- dion; 2-[2-(2-chlorphenyl)-4-methyl-3,6-dioxo-1,2,3,6-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5- yl]-N-(pyridin-2-ylmethyl)acetamid; 2-[2-(3-cyanophenyl)-4-methyl-3,6-dioxo-1,2,3,6-tetrahydro-5H-pyrazolo[4,3-c]pyridin- 5- yl]-N-(pyridin-2-ylmethyl)acetamid; 2-[2-(3-chlorphenyl)-4-methyl-3,6-dioxo-1,2,3,6-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-N-(pyridin-2-ylmethyl)acetamid; 2-(2-chlorphenyl)-5-(3-ethoxypropyl)-4-methyl-1-(pyridin-2-ylmethyl)-1 H-pyrazolo[4,3-c]pyridin-3,6(2H,5H)-dion; 2.4- dimethyl-5-(3-phenoxybenzyl)-1 H-pyrazolo[4,3-c]pyridin-3,6(2H,5H)-dion; 2-(2-chlorphenyl)-5-[3-(diethylamino)propyl]-4-methyl-1H-pyrazolo[4,3-c]pyridin-3,6(2H,5H)-dion; 2-(2-chlorphenyl)-5-(cyclohexylmethyl)-4-methyl-1H-pyrazolo[4,3-c]pyridin-3,6(2H,5H)- dion; 2-(3-chlorphenyl)-5-(3-hydroxypropyl)-4-methyl-1H-pyrazolo[4,3-c]pyridin-3,6(2H,5H)- dion; 2-(2-chlorphenyl)-4-methyl-5-[4-(4-methylpiperazin-1-yl)-4-oxobutyl]-1H-pyrazolo[4,3- c]pyridin-3,6(2H,5H)-dion; 2-(2-chlorphenyl)-5-(3-phenoxybenzyl)-1 H-pyrazolo[4,3-c]pyridin-3,6(2H,5H)-dion; 2-(3-chlorphenyl)-4-methyl-5-(3-morpholin-4-yl-3-phenylpropyl)-1H-pyrazolo[4,3-c]- pyridin-3,6(2H,5H)-dion; 2-(3-chlorphenyl)-4-methyl-5-(3-phenylprop-2-yn-1-yl)-1H-pyrazolo[4,3-c]pyridin- 3,6(2H,5H)-dion; 2-(2-chlor-4-fluorphenyl)-4-methyl-5-[2-(morpholin-4-ylmethyl)benzyl]-1 H-pyrazolo[4,3-c]pyridin-3,6(2H,5H)-dion; 4.5- dimethyl-2-{5-[(4-methylpiperazin-1-yl)sulfonyl]pyridin-2-yl}-1 H-pyrazolo[4,3-c]-pyridin-3,6(2H,5H)-dion; 2-(2-fluorphenyl)-4-methyl-5-(3-morpholin-4-yl-3-phenylpropyl)-1 H-pyrazolo[4,3-c]-pyridin-3,6(2H,5H)-dion; 2-(2,5-dichlorphenyl)-4-methyl-5-[2-(morpholin-4-ylmethyl)benzyl]-1H-pyrazolo[4,3-c]- pyridin-3,6(2H,5H)-dion; 2-[2-(benzyloxy)phenyl]-5-(3-ethoxypropyl)-4-methyl-1H-pyrazolo[4,3-c]pyridin- 3,6(2H,5H)-dion; 2-(2,5-dichlorphenyl)-4-methyl-5-(2-morpholin-4-yl-2-oxoethyl)-1H-pyrazolo[4,3-c]- pyridin-3,6(2H,5H)-dion; N-{2-[2-(2,5-dichlorphenyl)-4-methyl-3,6-dioxo-1,2,3,6-tetrahydro-5H-pyrazolo[4,3-c]- pyridin-5-yl]ethyl}acetamid; 2-(2-chlor-4-fluorphenyl)-4-(methoxymethyl)-5-[2-(morpholin-4-ylmethyl)benzyl]-1H- pyrazolo[4,3-c]pyridin-3,6(2H,5H)-dion; 2-(2-chlorphenyl)-5-[2-(dimethylamino)ethyl]-4-methyl-1 H-pyrazolo[4,3-c]pyridin-3,6(2H,5H)-dion; 2-[4-(benzyloxy)phenyl]-4-methyl-5-[2-(morpholin-4-ylmethyl)benzyl]-1H-pyrazolo[4,3- c]pyridin-3,6(2H,5H)-dion; 2-(3-chlorphenyl)-4-methyl-5-[2-(4-methylpiperazin-1-yl)benzyl]-1H-pyrazolo[4,3-c]- pyridin-3,6(2H,5H)-dion; 2-(3,4-dichlorphenyl)-4-methyl-5-[4-(4-methylpiperazin-1-yl)-4-oxobutyl]-1H-pyrazolo- [4,3-c]pyridin-3,6(2H,5H)-dion; 5-[2-(4-benzylpiperazin-1-yl)-2-oxoethyl]-2-(2,5-dichlorphenyl)-4-methyl-1H-pyrazolo- [4,3-c]pyridin-3,6(2H,5H)-dion; 2-(2-chlorphenyl)-4-methyl-5-(3-phenylprop-2-yn-1-yl)-1H-pyrazolo[4,3-c]pyridin- 3,6(2H,5H)-dion; N-{3-[5-(3-ethoxypropyl)-4-methyl-3,6-dioxo-1,3,5,6-tetrahydro-2H-pyrazolo[4,3-c]- pyridin-2-yl]phenyl}acetamid; 2-benzyl-4-methyl-5-[2-(morpholin-4-ylmethyl)benzyl]-1H-pyrazolo[4,3-c]pyridin- 3,6(2H,5H)-dion; 2-(3,4-dichlorphenyl)-4-methyl-5-[2-(morpholin-4-ylmethyl)benzyl]-1H-pyrazolo[4,3-c]- pyridin-3,6(2H,5H)-dion; 2-(2-chlor-4-fluorphenyl)-4,5-dimethyl-1H-pyrazolo[4,3-c]pyridin-3,6(2H,5H)-dion; 2-[4-(benzyloxy)phenyl]-4-methyl-5-(2-morpholin-4-yl-2-oxoethyl)-1H-pyrazolo[4,3-c]- pyridin-3,6(2H,5H)-dion; 2-(3,4-dichlorphenyl)-4-methyl-5-(2-morpholin-4-yl-2-oxoethyl)-1H-pyrazolo[4,3-c]- pyridin-3,6(2H,5H)-dion; methyl-[2-(2,5-dichlorphenyl)-4-methyl-3,6-dioxo-1,2,3,6-tetrahydro-5H-pyrazolo[4,3- c]pyridin-5-yl]acetat; N-{3-[2-(2,3-dichlorphenyl)-4-methyl-3,6-dioxo-1,2,3,6-tetrahydro-5H-pyrazolo[4,3-c]- pyridin-5-yl]phenyl}acetamid; 2-(2,3-dichlorphenyl)-4-methyl-5-[4-(4-methylpiperazin-1-yl)-4-oxobutyl]-1H-pyrazolo- [4,3-c]pyridin-3,6(2H,5H)-dion; N-{3-[2-(3-chlor-4-fluorphenyl)-4-methyl-3,6-dioxo-1,2,3,6-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]phenyl}acetamid; 5-[2-(4-benzylpiperazin-1-yl)-2-oxoethyl]-2-(3,4-dichlorphenyl)-4-methyl-1H-pyrazolo- [4,3-c]pyridin-3,6(2H,5H)-dion; 2.4- dimethyl-5-[2-(morpholin-4-ylmethyl)benzyl]-1H-pyrazolo[4,3-c]pyridin-3,6(2H,5H)-dion; 2.4- dimethyl-5-(3-morpholin-4-yl-3-phenylpropyl)-1H-pyrazolo[4,3-c]pyridin-3,6(2H,5H)-dion; N-{3-[2-(2-chlor-4-fluorphenyl)-4-methyl-3,6-dioxo-1,2,3,6-tetrahydro-5H-pyrazolo[4,3- c]pyridin-5-yl]phenyl}acetamid; 2-(3-chlorphenyl)-5-(3-ethoxypropyl)-4-(3-methoxybenzyl)-1H-pyrazolo[4,3-c]pyridin- 3,6(2H,5H)-dion; 2-(2,4-dimethyl-3,6-dioxo-1,2,3,6-tetrahydro5H-pyrazolo[4,3-c]pyridin-5-yl)-N-(pyridin- 2-ylmethyl)acetamid; 2-(3-chlor-4-fluorphenyl)-4-methyl-5-(2-morpholin-4-yl-2-oxoethyl)-1H-pyrazolo[4,3-c]- pyridin-3,6(2H,5H)-dion; 2-(3-chlor-4-fluorphenyl)-4-methyl-5-[4-(4-methylpiperazin-1-yl)-4-oxobutyl]-1 H-pyrazolo[4,3-c]pyridin-3,6(2H,5H)-dion; 2-(2-chlor-4-fluorphenyl)-4-methyl-5-(2-morpholin-4-yl-2-oxoethyl)-1H-pyrazolo[4,3-c]- pyridin-3,6(2H,5H)-dion; 5-[2-(4-benzylpiperazin-1-yl)-2-oxoethyl]-2-(2-chlor-4-fluorphenyl)-4-methyl-1H- pyrazolo[4,3-c]pyridin-3,6(2H,5H)-dion; 2-[4-(benzyloxy)phenyl]-4-methyl-5-[4-(4-methylpiperazin-1-yl)-4-oxobutyl]-1H- pyrazolo[4,3-c]pyridin-3,6(2H,5H)-dion; 2-(2,3-dichlorphenyl)-4-methyl-5-[2-(morpholin-4-ylmethyl)benzyl]-1H-pyrazolo[4,3-c]- pyridin-3,6(2H,5H)-dion; 2-(2-chlor-4-fluorphenyl)-4-methyl-5-[2-(4-methylpiperazin-1-yl)benzyl]-1H-pyrazolo- [4,3-c]pyridin-3,6(2H,5H)-dion; N-(3-{[2-(3-chlor-4-fluorphenyl)-4-methyl-3,6-dioxo-1,2,3,6-tetrahydro-5H-pyrazolo[4,3- c]pyridin-5-yl]methyl}phenyl)acetamid; 5-[2-(4-benzylpiperazin-1-yl)-2-oxoethyl]-2-(3-chlor-4-fluorphenyl)-4-methyl-1H- pyrazolo[4,3-c]pyridin-3,6(2H,5H)-dion; N-(3-{[2-(2-chlor-4-fluorphenyl)-4-methyl-3,6-dioxo-1,2,3,6-tetrahydro5H-pyrazolo[4,3- c]pyridin-5-yl]methyl}phenyl)acetamid; 2- (2-chlor-4-fluorphenyl)-4-methyl-5-[4-(4-methylpiperazin-1-yl)-4-oxobutyl]-1 H-pyrazolo[4,3-c]pyridin-3,6(2H,5H)-dion; 3- {4-methyl-5-[2-(morpholin-4-ylmethyl)benzyl]-3,6-dioxo-1,3,5,6-tetrahydro-2H- pyrazolo[4,3-c]pyridin-2-yl}benzonitril; N-{2-[2-(3-chlor-4-fluorphenyl)-4-methyl-3,6-dioxo-1,2,3,6-tetrahydro-5H-pyrazolo[4,3- c]pyridin-5-yl]ethyl}-4-fluorbenzamid; N-{2-[2-(2-chlor-4-fluorphenyl)-4-methyl-3,6-dioxo-1,2,3,6-tetrahydro-5H-pyrazolo[4,3- c]pyridin-5-yl]ethyl}-4-fluorbenzamid; 2-[2-(2-chlor-4-fluorphenyl)-4-methyl-3,6-dioxo-1,2,3,6-tetrahydro-5H-pyrazolo[4,3-c]- pyridin-5-yl]-N-(pyridin-2-ylmethyl)acetamid; N-(2-{2-[4-(benzyloxy)phenyl]-4-methyl-3,6-dioxo-1,2,3,6-tetrahydro-5H-pyrazolo[4,3- c]pyridin-5-yl}ethyl)-4-fluorbenzamid; 2-(3-chlor-4-fluorphenyl)-4-methyl-5-[2-(morpholin-4-ylmethyl)benzyl]-1H-pyrazolo[4,3- c]pyridin-3,6(2H,5H)-dion; N-(3-{4-methyl-5-[2-(morpholin-4-ylmethyl)benzyl]-3,6-dioxo-1,3,5,6-tetrahydro-2H- pyrazolo[4,3-c]pyridin-2-yl}phenyl)acetamid; 2-(4-chlorphenyl)-4-methyl-5-(3-phenoxybenzyl)-1H-pyrazolo[4,3-c]pyridin-3,6(2H,5H)- dion; 2-[2-(3-chlor-4-fluorphenyl)-4-methyl-3,6-dioxo-1,2,3,6-tetrahydro-5H-pyrazolo[4,3-c]- pyridin-5-yl]-N-(pyridin-2-ylmethyl)acetamid; 2-[4-butyl-2-(3-chlor-4-fluorphenyl)-3,6-dioxo-1,2,3,6-tetrahydro-5H-pyrazolo[4,3-c]- pyridin-5-yl]-N-(pyridin-2-ylmethyl)acetamid; 2-[2-(2,3-dichlorphenyl)-4-methyl-3,6-dioxo-1,2,3,6-tetrahydro-5H-pyrazolo[4,3-c]- pyridin-5-yl]-N-(pyridin-2-ylmethyl)acetamid; 2-[2,4-bis-(3-chlorphenyl)-3,6-dioxo-1,2,3,6-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]- N-(pyridin-2-ylmethyl)acetamid; 4-(3-chlorphenyl)-5-(3-ethoxypropyl)-2-methyl-1H-pyrazolo[4,3-c]pyridin-3,6(2H,5H)- dion; 2-[4-(3-chlorphenyl)-2-methyl-3,6-dioxo-1,2,3,6-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5- yl]-N-(pyridin-2-ylmethyl)acetamid; N-(3-{[4-(3-chlorphenyl)-2-methyl-3,6-dioxo-1,2,3,6-tetrahydro-5H-pyrazolo[4,3-c]- pyridin-5-yl]methyl}phenyl)acetamid; 2,4-bis-(3-chlorphenyl)-5-(3-hydroxypropyl)-1H-pyrazolo[4,3-c]pyridin-3,6(2H,5H)-dion; 2-(2-chlorphenyl)-4-methyl-5-(2-morpholin-4-yl-2-oxoethyl)-1H-pyrazolo[4,3-c]pyridin- 3,6(2H,5H)-dion; 4-(3-chlorphenyl)-2-methyl-5-(2-morpholin-4-yl-2-oxoethyl)-1H-pyrazolo[4,3-c]pyridin- 3,6(2H,5H)-dion; 4-(4-chlorphenyl)-2-methyl-5-[4-(morpholin-4-ylmethyl)benzyl]-1H-pyrazolo[4,3-c]- pyridin-3,6(2H,5H)-dion; N-{3-[4-(3-chlorphenyl)-5-(3-hydroxypropyl)-3,6-dioxo-1,3,5,6-tetrahydro-2H- pyrazolo[4,3-c]pyridin-2-yl]phenyl}acetamid; 4-(3-chlorphenyl)-2-methyl-5-[3-(morpholin-4-ylmethyl)benzyl]-1H-pyrazolo[4,3-c]- pyridin-3,6(2H,5H)-dion; 2-[4-(4-chlorphenyl)-2-methyl-3,6-dioxo-1,2,3,6-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-N-(pyridin-2-ylmethyl)acetamid; 4-(3-chlorphenyl)-2-methyl-5-[2-(morpholin-4-ylmethyl)benzyl]-1H-pyrazolo[4,3-c]- pyridin-3,6(2H,5H)-dion; 4-(3-chlorphenyl)-2-methyl-5-[4-(morpholin-4-ylmethyl)benzyl]-1H-pyrazolo[4,3-c]- pyridin-3,6(2H,5H)-dion; 4-(3-chlorphenyl)-2-methyl-5-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]-1H-pyrazolo[4,3- c]pyridin-3,6(2H,5H)-dion; 2-(2-chlorphenyl)-4-methyl-5-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]-1H-pyrazolo[4,3- c]pyridin-3,6(2H,5H)-dion; 4-(4-chlorphenyl)-5-(3-ethoxypropyl)-2-methyl-1H-pyrazolo[4,3-c]pyridin-3,6(2H,5H)- dion; 4-(4-chlorphenyl)-2-methyl-5-[2-(morpholin-4-ylmethyl)benzyl]-1H-pyrazolo[4,3-c]- pyridin-3,6(2H,5H)-dion; N-(3-{[4-(4-chlorphenyl)-2-methyl-3,6-dioxo-1,2,3,6-tetrahydro-5H-pyrazolo[4,3-c]- pyridin-5-yl]methyl}phenyl)acetamid; 4-(4-chlorphenyl)-2-methyl-5-[3-(morpholin-4-ylmethyl)benzyl]-1H-pyrazolo[4,3-c]- pyridin-3,6(2H,5H)-dion; 4-(4-chlorphenyl)-2-methyl-5-[(6-morpholin-4-ylpyridin-2-yl)methyl]-1H-pyrazolo[4,3- c]pyridin-3,6(2H,5H)-dion; N-{2-[4-(4-chlorphenyl)-2-methyl-3,6-dioxo-1,2,3,6-tetrahydro-5H-pyrazolo[4,3-c]- pyridin-5-yl]ethyl}acetamid; 4-(4-chlorphenyl)-5-[3-(dimethylamino)benzyl]-2-methyl-1H-pyrazolo[4,3-c]pyridin- 3,6(2H,5H)-dion; 4-(4-chlorphenyl)-2-methyl-5-[(6-pyrrolidin-1-ylpyridin-2-yl)methyl]-1H-pyrazolo[4,3-c]- pyridin-3,6(2H,5H)-dion; 2-(2-chlorphenyl)-4-(4-chlorphenyl)-5-(3-ethoxypropyl)-1H-pyrazolo[4,3-c]pyridin- 3,6(2H,5H)-dion; 2-(2-chlorphenyl)-4-(4-chlorphenyl)-5-methyl-1H-pyrazolo[4,3-c]pyridin-3,6(2H,5H)- dion; 2-(2-chlorphenyl)-4-(2-fluorphenyl)-5-methyl-1H-pyrazolo[4,3-c]pyridin-3,6(2H,5H)- dion; 2-(2-chlorphenyl)-4-(4-chlorphenyl)-5-[3-(dimethylamino)propyl]-1 H-pyrazolo[4,3-c]-pyridin-3,6(2H,5H)-dion; 2-(2-chlorphenyl)-4-[3-(dimethylamino)phenyl]-5-methyl-1H-pyrazolo[4,3-c]pyridin- 3,6(2H,5H)-dion; 2-(2-chlorphenyl)-5-methyl-4-(3-morpholin-4-ylphenyl)-1H-pyrazolo[4,3-c]pyridin- 3,6(2H,5H)-dion; 2-(2-chlorphenyl)-4-[1-(3,4-difluorphenoxy)ethyl]-5-methyl-1H-pyrazolo[4,3-c]pyridin- 3,6(2H,5H)-dion; 4-[1-(benzyloxy)ethyl]-2-(2-chlorphenyl)-5-methyl-1H-pyrazolo[4,3-c]pyridin-3,6(2H,5H)-dion; og 4-[3-(dimethylamino)phenyl]-2-(2-methoxyphenyl)-5-methyl-1H-pyrazolo[4,3-c]pyridin- 3,6(2H,5H)-dion.
13. Farmaceutisk sammensætning indeholdende mindst ét derivat ifølge et hvilket som helst af kravene 1 til 12 og et farmaceutisk acceptabelt bærestof, fortyndingsmiddel eller excipiens for dette.
14. Derivat ifølge et hvilket som helst af kravene 1 til 12 til anvendelse som medikament.
15. Pyrazolopyridinderivat ifølge et hvilket som helst af kravene 1 til 12 til behandling af en sygdom eller en lidelse valgt blandt hjertekarsygdomme, sygdomme i åndedrætsvejene, stofskifteforstyrrelser, hudlidelser, knoglelidelser, neuro-inflammatoriske og/eller neurodegenerative lidelser, nyresygdomme, forplantningssygdomme, sygdomme, der rammer øjet og/eller linsen, og/eller tilstande, der rammer det indre øre, inflammationssygdomme, leversygdomme, smerte, cancere, allergiske lidelser, traumatiseringer, septisk, hæmorrhagisk og anafylaktisk chok, sygdomme eller lidelser i mavetarmsystemet, angiogenese, angiogenese-afhængige tilstande og andre sygdomme og/eller lidelser, der står i forbindelse med nicotinamidadenin-dinukleotidphosphatoxidase (NADPH-oxidase).
16. Fremgangsmåde til fremstilling af en forbindelse med formlen I omfattende det trin at ringslutte en forbindelse med formlen VIII i nærvær af en base: ivm;
\*f hvori R18 er en CrC6-alkylgruppe, såsom methyl, ethyl, propyl, isopropyl eller butyl; Gi er H; G2, G3, G4 og G5 er som defineret i et hvilket som helst af de foregående krav.
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Families Citing this family (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2002835A1 (en) 2007-06-04 2008-12-17 GenKyo Tex Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
EP2000176A1 (en) * 2007-06-04 2008-12-10 GenKyo Tex Tetrahydroindole derivatives as NADPH Oxidase inhibitors
EP2166010A1 (en) * 2008-09-23 2010-03-24 Genkyo Tex Sa Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
EP2165707A1 (en) * 2008-09-23 2010-03-24 Genkyo Tex Sa Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
EP2166008A1 (en) * 2008-09-23 2010-03-24 Genkyo Tex Sa Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
EP2166009A1 (en) 2008-09-23 2010-03-24 Genkyo Tex Sa Pyrazolo pyridine derivatives as nadph oxidase inhibitors
EP2305679A1 (en) 2009-09-28 2011-04-06 GenKyoTex SA Pyrazoline dione derivatives as nadph oxidase inhibitors
EP2361911A1 (en) 2010-02-18 2011-08-31 GenKyoTex SA Pyrazolo piperidine derivatives as NADPH oxidase inhibitors
WO2012170752A1 (en) * 2011-06-10 2012-12-13 Glaxo Wellcome Manufacturing Pte Ltd Novel compounds
EP2591782A1 (en) * 2011-11-11 2013-05-15 Johann Wolfgang Goethe-Universität Nadph oxidase 4 inhibitors and use thereof
CN104918616A (zh) 2012-10-24 2015-09-16 格卢科克斯生物科技有限公司 用于治疗与烟酰胺腺嘌呤二核苷酸磷酸氧化酶相关的病况的三嗪衍生物
EP2857399A1 (en) 2013-10-03 2015-04-08 GenKyoTex SA Compounds useful for the treatment of PDE5 inhibitor-poorly responsive erectile dysfunction
JP2018505226A (ja) 2015-02-16 2018-02-22 グルコックス・バイオテック・アーベー Ｎ２−（３，４−ジメチルフェニル）−６−（（４−（ｐ−トリル）ピペラジン−１−イル）メチル）−１，３，５−トリアジン−２，４−ジアミン
US10251870B2 (en) * 2015-03-06 2019-04-09 Stc.Unm Method for treating obesity, diabetes, cardiovascular and kidney diseases by regulating GPR30/GPER activity
EP3098220A1 (en) 2015-05-28 2016-11-30 GenKyoTex SA Process for the preparation of a nadph oxidase inhibitor and its polymorphs and uses thereof
WO2017196982A1 (en) * 2016-05-10 2017-11-16 Georgia State University Research Foundation, Inc. Bicyclic fused pyrazole derivatives for the treatment of rsv
US10280164B2 (en) 2016-09-09 2019-05-07 Incyte Corporation Pyrazolopyridone compounds and uses thereof
CN115819417A (zh) 2016-09-09 2023-03-21 因赛特公司 作为hpk1调节剂的吡唑并吡啶衍生物及其用于治疗癌症的用途
WO2018049214A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyridine derivatives as hpk1 modulators and uses thereof for the treatment of cancer
US20180072741A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyrimidine compounds and uses thereof
WO2018152220A1 (en) 2017-02-15 2018-08-23 Incyte Corporation Pyrazolopyridine compounds and uses thereof
BR112019023109A2 (pt) 2017-05-04 2020-05-26 Glenmark Pharmaceuticals S.A. Composto, composição farmacêutica e método para tratar uma doença, distúrbio, síndrome ou afecção mediada por nadph oxidase em um indivíduo
WO2019028877A1 (zh) * 2017-08-11 2019-02-14 邦泰生物工程(深圳)有限公司 一种含有nadh和nadph的组合物及其应用
US10722495B2 (en) 2017-09-08 2020-07-28 Incyte Corporation Cyanoindazole compounds and uses thereof
EP3479843A1 (en) * 2017-11-01 2019-05-08 GenKyoTex Suisse SA Use of nox inhibitors for treatment of cancer
AU2018369912A1 (en) * 2017-11-15 2020-05-28 Vanderbilt University Methods and compositions for the improvement of lysosomal function and treatment of neurodegenerative disease
US10752635B2 (en) 2018-02-20 2020-08-25 Incyte Corporation Indazole compounds and uses thereof
US10745388B2 (en) 2018-02-20 2020-08-18 Incyte Corporation Indazole compounds and uses thereof
EP3755703B1 (en) 2018-02-20 2022-05-04 Incyte Corporation N-(phenyl)-2-(phenyl)pyrimidine-4-carboxamide derivatives and related compounds as hpk1 inhibitors for treating cancer
US11299473B2 (en) 2018-04-13 2022-04-12 Incyte Corporation Benzimidazole and indole compounds and uses thereof
US10899755B2 (en) 2018-08-08 2021-01-26 Incyte Corporation Benzothiazole compounds and uses thereof
WO2020068729A1 (en) 2018-09-25 2020-04-02 Incyte Corporation Pyrazolo[4,3-d]pyrimidine compounds as alk2 abd/or fgfr modulators
WO2020205937A1 (en) 2019-04-01 2020-10-08 Emory University Hyaluronic acid nanoparticles comprising nadph oxidases inhibitors and uses in treating cancer
BR112021024310A2 (pt) 2019-06-05 2022-02-15 Univ Emory Peptidomiméticos para o tratamento de infecções por coronavírus e picornavírus
BR112022002059A2 (pt) 2019-08-06 2022-06-07 Incyte Corp Formas sólidas de um inibidor de hpk1
WO2022045836A1 (ko) * 2020-08-28 2022-03-03 (주)셀로스바이오텍 신규 티오히단토인 유도체 및 이의 용도
WO2023018560A1 (en) * 2021-08-13 2023-02-16 Georgia State University Research Foundation, Inc. Bicyclic fused pyrazole derivatives for the treatment of respiratory infections including rsv
US11896719B2 (en) 2022-01-24 2024-02-13 Calliditas Therapeutics Ab Pharmaceutical compositions
TW202413355A (zh) 2022-05-09 2024-04-01 瑞士商卡利迪塔斯療法瑞士股份有限公司 新醫藥用途

Family Cites Families (41)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3391407A (en) 1966-08-15 1968-07-09 William A. Waters Helmet
US3931407A (en) 1973-03-01 1976-01-06 American Hoechst Corporation Method of treatment with and compositions containing condensed pyrroles bearing an N-phenyl substituent
DE3728278A1 (de) 1986-12-17 1988-06-23 Bayer Ag Herbizide und fungizide mittel auf basis von substituierten pyrazolin-5-on derivaten
DE19518082A1 (de) 1995-05-17 1996-11-21 Merck Patent Gmbh 4(-Arylaminomethylen)-2,4-dihydropyrazol-3-one
US5763496A (en) 1995-11-27 1998-06-09 The Research Foundation Of State University Of New York Prevention of atherosclerosis using NADPH oxidase inhibitors
TW432073B (en) 1995-12-28 2001-05-01 Pfizer Pyrazolopyridine compounds
AU6320998A (en) 1997-02-21 1998-09-09 Bristol-Myers Squibb Company Benzoic acid derivatives and related compounds as antiarrhythmic agents
IL144468A0 (en) 2000-07-27 2002-05-23 Pfizer Prod Inc Use of growth hormone secretagogues for improvement of functional health status
US7902179B2 (en) 2001-04-26 2011-03-08 Ajinomoto Co., Inc. Heterocyclic compounds
EP1291017A3 (en) 2001-09-10 2003-07-02 Warner-Lambert Company Use of statins to inhibit formation of osteoclasts
US7662826B2 (en) * 2002-04-23 2010-02-16 Shionogi & Co., Ltd. Pyrazolo [1,5-a] pyrimidine derivative and nad (p) h oxidase inhibitor containing the same
WO2004005267A2 (en) 2002-07-03 2004-01-15 Janssen Pharmaceutica, N.V. Heteroaryl compounds useful in treating inflammatory disorders
AU2004216541A1 (en) 2003-02-28 2004-09-10 Howard Florey Institute Of Experimental Physiology And Medicine Therapeutic compositions
WO2004089412A1 (ja) 2003-04-08 2004-10-21 Mitsubishi Pharma Corporation 特異的ｎａｄ(ｐ)ｈオキシダーゼ抑制剤
TW200533356A (en) 2004-02-24 2005-10-16 Mitsubishi Pharma Corp Fused pyridazine derivatives
WO2007115306A2 (en) 2006-04-04 2007-10-11 Myriad Genetics, Inc. Compounds for diseases and disorders
AU2005294404A1 (en) 2004-10-04 2006-04-20 Myriad Genetics, Inc. Compounds for Alzheimer's disease
FR2882654B1 (fr) 2005-03-01 2007-04-27 Servier Lab Utilisation de derives de la diosmetine pour le traitement et la prevention des pathologies thrombotiques
US7759337B2 (en) 2005-03-03 2010-07-20 Amgen Inc. Phthalazine compounds and methods of use
US20070014739A1 (en) * 2005-07-14 2007-01-18 Eldridge Gary R Compositions and methods for controlling biofilms and bacterial infections
DE102005048897A1 (de) 2005-10-12 2007-04-19 Sanofi-Aventis Deutschland Gmbh Diacylindazol-derivate als Inhibitoren von Lipasen und Phospholipasen
WO2008030887A2 (en) * 2006-09-05 2008-03-13 Bipar Sciences, Inc. Methods for designing parp inhibitors and uses thereof
EP3597188A1 (en) * 2006-11-13 2020-01-22 PCB Associates, Inc. An isolated phycobilin for use in a method for prophylaxis or treatment of a medical condition
EP2002835A1 (en) 2007-06-04 2008-12-17 GenKyo Tex Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
EP2000176A1 (en) 2007-06-04 2008-12-10 GenKyo Tex Tetrahydroindole derivatives as NADPH Oxidase inhibitors
AR069526A1 (es) 2007-12-03 2010-01-27 Takeda Pharmaceutical Compuesto heterociclico que contiene nitrogeno y su uso
US20090163452A1 (en) 2007-12-20 2009-06-25 Schwartz Janice B Compositions and methods for lowering serum cholesterol
FR2929276B1 (fr) 2008-04-01 2010-04-23 Servier Lab Nouveaux derives de diosmetine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
EP2166010A1 (en) * 2008-09-23 2010-03-24 Genkyo Tex Sa Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
EP2166009A1 (en) 2008-09-23 2010-03-24 Genkyo Tex Sa Pyrazolo pyridine derivatives as nadph oxidase inhibitors
EP2165707A1 (en) 2008-09-23 2010-03-24 Genkyo Tex Sa Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
EP2166008A1 (en) 2008-09-23 2010-03-24 Genkyo Tex Sa Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
US8283002B2 (en) * 2008-11-18 2012-10-09 Plextronics, Inc. Aminobenzene compositions and related devices and methods
JP6046348B2 (ja) * 2008-11-18 2016-12-14 タケダ ヴァクシーンズ， インコーポレイテッド Ｒｓｖｆｖｌｐならびにその製造および使用の方法
JP5596047B2 (ja) * 2008-11-19 2014-09-24 バーテックス ファーマシューティカルズ インコーポレイテッド ｃ−Ｍｅｔタンパク質キナーゼのトリアゾロチアジアゾール阻害剤
EP2305679A1 (en) 2009-09-28 2011-04-06 GenKyoTex SA Pyrazoline dione derivatives as nadph oxidase inhibitors
CA2823974A1 (en) 2010-01-08 2011-07-14 Beth Israel Deaconess Medical Center Methods and compositions for the treatment of migraine headaches
EP2361911A1 (en) 2010-02-18 2011-08-31 GenKyoTex SA Pyrazolo piperidine derivatives as NADPH oxidase inhibitors
EP2361912A1 (en) 2010-02-18 2011-08-31 GenKyoTex SA Pyrazolo piperidine derivatives as NADPH oxidase inhibitors
CN102014373B (zh) 2010-11-22 2015-04-01 中兴通讯股份有限公司 一种激活配置的方法及装置
EP2591782A1 (en) 2011-11-11 2013-05-15 Johann Wolfgang Goethe-Universität Nadph oxidase 4 inhibitors and use thereof

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