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    • 8. 发明申请
    • NEW ENZYME INHIBITOR COMPOUNDS
    • 新型酶抑制剂化合物
    • WO2013037411A1
    • 2013-03-21
    • PCT/EP2011/065967
    • 2011-09-14
    • PROXIMAGEN LIMITEDEVANS, DavidCARLEY, AllisonSTEWART, AlisonHIGGINBOTTOM, MichaelSAVORY, EdwardSIMPSON, IainNILSSON, MarianneHARALDSSON, MartinNORDLING, ErikKOOLMEISTER, Tobias
    • EVANS, DavidCARLEY, AllisonSTEWART, AlisonHIGGINBOTTOM, MichaelSAVORY, EdwardSIMPSON, IainNILSSON, MarianneHARALDSSON, MartinNORDLING, ErikKOOLMEISTER, Tobias
    • C07D471/04A61K31/437
    • C07D471/04
    • 2-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}ethan-1-amine; 3- aminopropyl 4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidine-1-carboxylate; 1-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}-4- (dimethylamino)butan-1-one; 5-amino-1-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3- yl]piperidin-1-yl}pentan-1-one; N-(2-aminoethyl)-4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3- c]pyridin-3-yl]piperidine-1-carboxamide; N-(3-aminopropyl)-4-[1-(4-chlorophenyl)-1H- pyrrolo[2,3-c]pyridin-3-yl]piperidine-1-carboxamide; 4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3- c]pyridin-3-yl]-N-[3-(dimethylamino)propyl]piperidine-1-carboxamide; 1-({4-[1-(4- chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)piperazine; 4-({4-[1-(4- chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)morpholine; 1-({4-[1-(4- chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)-1,4-diazepane; ethyl 1- [1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxylate; ethyl 1-[1-(4- methylphenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxylate; 1-[1-(4- chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxylic acid; N-(2- aminoethyl)-1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxamide; 4-({1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-4 yl}carbonyl)morpholine; 1-({1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin- 4-yl}carbonyl)piperazine; {4-[1-(4-methylphenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin- 3-yl}methanol; {4-[1-(4-methylphenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-2-yl}methanol; [(3R)-4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-3- yl]methanol; methyl 4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholine-3- carboxylate; N-(2-aminoethyl)-4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3- yl]morpholine-3-carboxamide; 2-{4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3- yl]morpholin-3-yl}ethan-1-ol; methyl 1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3- yl]piperidine-2-carboxylate; N-(2-aminoethyl)-1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4- c]pyridin-3-yl]piperidine-2-carboxamide; 1-({1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4- c]pyridin-3-yl]piperidin-2-yl}carbonyl)piperazine; 4-[1-(4-methylphenyl)-1H-pyrrolo[2,3- c]pyridin-3-yl]morpholine; 1-(4-chlorophenyl)-3-(piperidin-4-yl)-1H-pyrrolo[2,3-c]pyridin-4- ol; N-butyl-1-(4-chlorophenyl)-N-methyl-1H-pyrazolo[3,4-c]pyridin-3-amine; 1-[4- (fluoromethyl)phenyl]-3-(oxan-4-yl)-1H-pyrazolo[3,4-c]pyridine; and 3-({4-[1-(4- chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-1-yl}methyl)pyridine are useful for the inhibition of SSAO activity.
    • 2- {4- [1-(4-氯苯基)-1H-吡咯并[2,3-c]吡啶-3-基]哌啶-1-基}乙-1-胺; 4- [1-(4-氯苯基)-1H-吡咯并[2,3-c]吡啶-3-基]哌啶-1-甲酸3-氨基丙酯; 1- {4- [1-(4-氯苯基)-1H-吡咯并[2,3-c]吡啶-3-基]哌啶-1-基} -4-(二甲基氨基)丁-1-酮; 5-氨基-1- {4- [1-(4-氯苯基)-1H-吡咯并[2,3-c]吡啶-3-基]哌啶-1-基}戊-1-酮; N-(2-氨基乙基)-4- [1-(4-氯苯基)-1H-吡咯并[2,3-c]吡啶-3-基]哌啶-1-甲酰胺; N-(3-氨基丙基)-4- [1-(4-氯苯基)-1H-吡咯并[2,3-c]吡啶-3-基]哌啶-1-甲酰胺; 4- [1-(4-氯苯基)-1H-吡咯并[2,3-c]吡啶-3-基] -N- [3-(二甲基氨基)丙基]哌啶-1-甲酰胺; 1 - ({4- [1-(4-氯苯基)-1H-吡咯并[2,3-c]吡啶-3-基]哌啶-1-基}羰基)哌嗪; 4 - ({4- [1-(4-氯苯基)-1H-吡咯并[2,3-c]吡啶-3-基]哌啶-1-基}羰基)吗啉; 1 - ({4- [1-(4-氯苯基)-1H-吡咯并[2,3-c]吡啶-3-基]哌啶-1-基}羰基)-1,4-二氮杂环庚烷; 1- [1-(4-氯苯基)-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-4-甲酸乙酯; 1- [1-(4-甲基苯基)-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-4-甲酸乙酯; 1- [1-(4-氯苯基)-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-4-甲酸; N-(2-氨基乙基)-1- [1-(4-氯苯基)-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-4-甲酰胺; 4 - ({1- [1-(4-氯苯基)-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-4-基}羰基)吗啉; 1 - ({1- [1-(4-氯苯基)-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-4-基}羰基)哌嗪; {4- [1-(4-甲基苯基)-1H-吡唑并[3,4-c]吡啶-3-基]吗啉-3-基}甲醇; {4- [1-(4-甲基苯基)-1H-吡唑并[3,4-c]吡啶-3-基]吗啉-2-基}甲醇; [(3R)-4- [1-(4-氯苯基)-1H-吡唑并[3,4-c]吡啶-3-基]吗啉-3-基]甲醇; 4- [1-(4-氯苯基)-1H-吡唑并[3,4-c]吡啶-3-基]吗啉-3-羧酸甲酯; N-(2-氨基乙基)-4- [1-(4-氯苯基)-1H-吡唑并[3,4-c]吡啶-3-基]吗啉-3-甲酰胺; 2- {4- [1-(4-氯苯基)-1H-吡唑并[3,4-c]吡啶-3-基]吗啉-3-基}乙-1-醇; 1- [1-(4-氯苯基)-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-2-甲酸甲酯; N-(2-氨基乙基)-1- [1-(4-氯苯基)-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-2-甲酰胺; 1 - ({1- [1-(4-氯苯基)-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-2-基}羰基)哌嗪; 4- [1-(4-甲基苯基)-1H-吡咯并[2,3-c]吡啶-3-基]吗啉; 1-(4-氯苯基)-3-(哌啶-4-基)-1H-吡咯并[2,3-c]吡啶-4-醇; N-丁基-1-(4-氯苯基)-N-甲基-1H-吡唑并[3,4-c]吡啶-3-胺; 1- [4-(氟甲基)苯基] -3-(氧代-4-基)-1H-吡唑并[3,4-c]吡啶; 和3 - ({4- [1-(4-氯苯基)-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-1-基}甲基)吡啶可用于抑制SSAO活性。