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A class of nitrogen aryl benzothiazole PARP inhibitors and its preparation method and use

A benzothiazole and aryl technology, applied in the field of new PARP inhibitor compounds, can solve the problems of short action time and half-life, difficulty in research and development, and low bioavailability, and achieve long action time and half-life, and improved bioavailability , the effect of far-reaching social significance

Inactive Publication Date: 2019-05-17
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0011] However, compound AZD2281 has short action time and half-life in vivo (<1 hour), and low bioavailability (<15%), which brings difficulties to further research and development

Method used

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  • A class of nitrogen aryl benzothiazole PARP inhibitors and its preparation method and use
  • A class of nitrogen aryl benzothiazole PARP inhibitors and its preparation method and use
  • A class of nitrogen aryl benzothiazole PARP inhibitors and its preparation method and use

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Embodiment Construction

[0061] The present invention will be further described below in conjunction with specific examples, but these examples do not limit the scope of the present invention.

[0062] Preparation Example

[0063] In the following examples, 1 H-NMR is measured with a Varian Mercury AMX300 type instrument; MS is measured with a VG ZAB-HS or VG-7070 type instrument, and all are EI sources (70ev) unless otherwise noted; The water solvents were all obtained by drying according to standard methods; except for the instructions, all reactions were carried out under nitrogen protection and followed by TLC, and the post-treatment was washed with saturated sodium chloride aqueous solution and dried with anhydrous sodium sulfate; the purification of the product Unless otherwise specified, silica gel (200-300 mesh) column chromatography was used; among them, silica gel (200-300 mesh) was produced by Qingdao Ocean Chemical Factory, and GF254 thin-layer silica gel plate was produced by Yantai Jian...

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Abstract

The present invention discloses a class of novel PARP inhibitor compounds represented by the following general formula I and having a nitrogen aryl benzothiazole structure, stereoisomers, preparation methods and intermediates thereof, and applications of the novel PARP inhibitor compounds in preparation of drugs for prevention and treatment of PARP (poly ADP-ribose-ribose polymerase) related diseases. Compared to the similar drugs in the prior art, the compounds of the preset invention hava advantages of long in vivo action time, long half life, and significantly improved bioavailability. The general formula I is defined in the specification.

Description

technical field [0001] The present invention relates to a class of novel PARP inhibitor compounds with nitrogen aryl benzothiazole structures represented by the following general formula I, their stereoisomers, their preparation methods, intermediates and their use in the prevention and treatment of PARP ( Ribose poly(ADP-ribose polymerase) related diseases, said PARP related diseases include various ischemic diseases (brain, umbilical cord, heart, digestive tract, retina, etc.), neurodegenerative diseases (Parkinson's disease, Alzheimer's disease, muscular dystrophy, etc.) and cancers (breast cancer, ovarian cancer, liver cancer, melanoma, prostate cancer, colon cancer, gastric cancer and solid tumors, etc.). [0002] Background technique [0003] 1. PARP family and structural features [0004] PARP is a family of nuclear enzyme proteins that catalyze the synthesis of polyadenosine diphosphate-ribose. So far, 18 subtypes in the family have been isolated and identified,...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D277/82C07D417/12C07D487/04C07D487/08C07D487/10A61K31/428A61K31/5377A61K31/454A61K31/439A61K31/438A61K31/496A61K31/444A61K31/4725A61K31/4985A61P35/00A61P25/00A61P25/16A61P25/28A61P9/00A61P9/10A61P21/00
Inventor 张翱缪泽鸿王平原宦霞娟丁健
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI