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Condensed ring pyridazinone compound with bridge ring structure as well as preparation method and application thereof

A bridged ring structure and compound technology, applied in medical preparations containing active ingredients, organic chemistry, drug combinations, etc., can solve problems such as difficult research and development, unstable metabolism, and low bioavailability

Inactive Publication Date: 2014-02-12
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] 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
There are many reasons for these disadvantages, and the cyclic tertiary amine in the molecular structure is one of the main causes of metabolic instability

Method used

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  • Condensed ring pyridazinone compound with bridge ring structure as well as preparation method and application thereof
  • Condensed ring pyridazinone compound with bridge ring structure as well as preparation method and application thereof
  • Condensed ring pyridazinone compound with bridge ring structure as well as preparation method and application thereof

Examples

Experimental program
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Embodiment Construction

[0091] 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.

[0092] One, preparation embodiment

[0093] 1 H-NMR was measured with a Varian Mercury AMX300 instrument; MS was measured with a VG ZAB-HS or VG-7070 instrument, and all were EI sources (70ev) unless otherwise noted; all solvents were re-distilled before use, and no 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...

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Abstract

The invention relates to a condensed ring pyridazinone compound with a bridge ring structure, which is as shown in a general formula I in the specification, isomers or pharmaceutically acceptable salts, esters, prodrugs or hydrates thereof, as well as a preparation method of the compound, a pharmaceutical composition containing the compound, and an application of the compound serving as a ribose poly ADP (adenosine diphosphate)-ribose polymerase inhibitor in the prevention and / treatment of diseases related to ribose poly ADP-ribose polymerase.

Description

technical field [0001] The present invention relates to the field of pharmacy, and specifically relates to a class of fused-ring pyridazinone compounds with bridged ring structures or their isomers or pharmaceutically acceptable salts, esters, prodrugs or hydrates thereof, and their pharmaceutical compositions, Its preparation method and its use in preventing and / or treating diseases related to ribose poly ADP-ribose polymerase (PARP). Background technique [0002] 1. Structural subtypes and biological activities of PARP [0003] PARP includes numerous family members. Among them, PARP-1 is the earliest discovered nuclear enzyme with the function of catalyzing polyadenosine diphosphate ribosyl, and later isolated PARP-2, PARP-3, PARP-4 (VPARP), PARP-5a (tankyrase1), Subtypes such as PARP-5b (tankyrase2), PARP-7 (TiPARP) and sPARP-1. At present, according to the structure of the catalytic domain of PARP-1, 18 structural subtypes with potential PARP activity have been confir...

Claims

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Application Information

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IPC IPC(8): C07D487/08C07D471/08A61K31/502A61P9/10A61P25/16A61P25/28A61P21/00A61P35/00
CPCC07D471/08C07D487/08
Inventor 张翱缪泽鸿叶娜宦霞娟宋子兰陈川惠子陈奕丁健
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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