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Triazole derivative as well as preparation method and application thereof

A technology for triazole derivatives, applied in the field of triazole derivatives and their preparation, can solve the problems of poor cell activity, poor druggability, single molecular skeleton, etc.

Inactive Publication Date: 2020-11-03
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

The molecular activity of these three types of inhibitors is very good, but the cell activity is relatively poor, and the molecular skeleton is single, and the druggability is not good

Method used

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  • Triazole derivative as well as preparation method and application thereof
  • Triazole derivative as well as preparation method and application thereof
  • Triazole derivative as well as preparation method and application thereof

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Embodiment Construction

[0079] Definitions and Common Terms

[0080] Unless stated to the contrary, the following terms used in the specification and claims have the following meanings.

[0081] The term "optionally substituted with one or more substituents" in the present invention means substituted with one or more substituents, or unsubstituted. Specifically, "optional" or "optionally" means that the subsequently described event or circumstance may but need not occur, and that the description includes instances where the event or circumstance occurs or does not occur. For example, a "heterocyclic group optionally substituted with an alkyl group" means that an alkyl group may but need not be present, and the description includes cases where the heterocycle group is substituted with an alkyl group and cases where the heterocycle group is not substituted with an alkyl group .

[0082] "Alkyl" means a saturated aliphatic hydrocarbon group, including straight and branched chain groups. C 1 -C 6 Al...

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Abstract

The invention relates to a PDE inhibitor, in particular to a PDEdelta inhibitor. Specifically, the invention relates to a triazole derivative as shown in a general formula (I) and a preparation methodand application thereof. The series of compounds have good PDEdelta inhibition activity, are suitable for preparing medicines for treating or preventing KRas-PDEdelta mediated diseases, and are especially suitable for preparing KRas-PDEdelta-mediated antitumor medicines, wherein, the definition of each substituent group in the general formula (I) is the same as the definition in the specification.

Description

[0001] This application is a divisional application of a patent application with the application date of October 17, 2017, the title of the invention is "triazole derivatives and its preparation method and use", and the application number is 2017109648846. technical field [0002] The present invention relates to PDE inhibitors, in particular to triazole derivatives and their preparation methods and uses. Background technique [0003] Malignant tumors seriously threaten human health and life, and are the main cause of global morbidity and death. According to the data released by the World Health Organization, there were about 14 million new cancer cases and 8.2 million cancer deaths in the world in 2012. In the next 20 years, it is estimated that the annual number of new cancer cases will rise from 14 million in 2012 to 24 million. The incidence of cancer in my country is close to the world level, but the mortality rate is higher than the world level. According to the lates...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12C07D249/08C07D249/12C07D403/12A61K31/4439A61K31/4196A61K31/422A61K31/4709A61K31/5377A61K31/496A61P35/00
CPCA61P35/00C07D249/08C07D249/12C07D401/12C07D403/12
Inventor 沈竞康熊兵陈丹琦王昕张乃霞黄敏
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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