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A formamide-based and indazole-based technology, applied in the field of amido-substituted indazole and benzotriazole compounds, can solve the problem of weak inhibitory activity
Inactive Publication Date: 2016-03-23
BETTA PHARM CO LTD
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However, these molecules are weakly inhibitory and have other effects unrelated to PARP inhibitory activity
Method used
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Embodiment 1
[0221] Synthesis of 3-methyl-2(piperidin-4-yl)-7-carboxamido-2H-indazole:
[0224] A mixture of methyl 3-formyl-2-nitrobenzoate 1 (1.0eq) and tert-butyl 4-amino-piperidine-1-carboxylate 2 (1.05eq) was dissolved in ethanol (0.2M) under nitrogen Stir under reflux for 2 hours, until TLC showed that the reaction was complete (hexane / EtOAc=75:25). The solvent was removed by evaporation to give compound 3 as a white solid which was used in the next step without further purification. 1 HNMR (400MHz, CDCl 3 , 300K): δ8.51 (1H, d, J = 7.3Hz), 8.41 (1H, s), 8.11 (1H, d, J = 7.8Hz), 7.67 (1H, t, J = 7.8Hz), 7.43 (2H, t, J = 7.8Hz), 7.31 (1H, t, J = 7.3Hz), 7.16 (2H, d, J = 7.8Hz), 3.94 (3H, s).
[0234] Synthesis of 3-methyl-2-(piperidin-3-yl)-7-carboxamido-2H-indazole:
[0235]
[0236] The target title compound was synthesized according to the same steps and conditions described in Example 1, and 4-amino-piperidine-1-carboxylic acid tert-butyl was replaced with 3-amino-piperidine-1-carboxylic acid tert-butyl ester, and C 14 h 18 N 4 The theoretical value of O is 258, and the measured value is 259 (M+H) + .
Embodiment 3
[0238] Synthesis of 3-methyl-2-(piperidin-2-yl)-7-carboxamido-2H-indazole:
[0239]
[0240] Synthesize the target title compound according to the same steps and conditions described in Example 1, and replace 4-amino-piperidine-1-carboxylic acid tert-butyl with 2-amino-piperidine-1-carboxylic acid tert-butyl ester, calculate C 14 h 18 N 4 The theoretical value of O is 258, and the measured value is 259 (M+H) + .
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Abstract
Amide substituted indazoles and benzotriazoles as inhibitors of the enzyme poly(ADP-ribose)polymerase(PARP). The compounds of the present invention are useful as mono-therapies in tumors with specific defects in DNA-repair pathways, as enhancers of certain DNA-damaging agents such as anticancer agents and radiotherapy, for reducing cellnecrosis (in stroke and myocardial infarction), regulating inflammation and tissue injury, treating retroviral infections, and protecting against the toxicity of chemotherapy.
Description
technical field [0001] The invention relates to an amido-substituted indazole and benzotriazole compound which can be used as a poly(ADP-ribose) polymerase (Poly(ADP-ribose) polymerase, PARP) inhibitor. PARP was previously also known as poly(ADP-ribose) synthase and poly(ADP-ribose) synthase (poly(ADP-ribosyl) synthase). polymerase). Compounds of the present invention can be used as monotherapy for tumors associated with specific defects in DNA repair pathways, as well as enhancers of specific DNA damage drugs (such as anticancer drugs) and radiotherapy. Further, the present invention The compounds described are also useful for reducing cellular necrosis (in stroke and myocardial infarction), downregulating inflammation and tissue damage, treating retroviral infections, and preventing chemotherapytoxicity. Background technique [0002] Poly (ADP-ribose) polymerase (Poly (ADP-ribose) polymerase, PARP) constitutes a superfamily including 18 proteins, all of which contain PAR...
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