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Triazole derivative, preparation method and uses thereof

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

Active Publication Date: 2019-04-23
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, preparation method and uses thereof
  • Triazole derivative, preparation method and uses thereof
  • Triazole derivative, preparation method and uses thereof

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Embodiment Construction

[0080] Definitions and Common Terms

[0081] Unless stated to the contrary, the following terms used in the specification and claims have the following meanings.

[0082] 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 .

[0083] "Alkyl" means a saturated aliphatic hydrocarbon group, including straight and branched chain groups. C 1 -C 6 Al...

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Abstract

The present invention relates to a PDE inhibitor, particularly to a PDE[delta] inhibitor, specifically to a triazole derivative represented by a general formula (I), a preparation method and uses thereof. According to the present invention, a series of the compounds have good PDE[delta] inhibitory activities, can be used for preparing drugs for treating or preventing KRas-PDE[delta]-mediated diseases, and are particularly suitable for the preparation of KRas-PDE[delta]-mediated antitumor drugs, wherein each substituent in the general formula (I) is the same as the definition of the specification. The formula I is defined in the specification.

Description

technical field [0001] The present invention relates to PDE inhibitors, in particular to triazole derivatives and their preparation methods and applications. Background technique [0002] 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 latest cancer report data, the number of cancer cases in China in 2015 was 4.292 million, accounting for about one-fifth of the global incidence; the number of cancer deaths was 2.814 million, accounting for about one-quarter of the global cancer deaths th...

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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