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Substitution five-heterocyclic alkyl aminoacyl compound and application thereof

A technology of compounds and hydrates, which is applied in the field of preparing compounds with anti-tumor activity, and can solve problems such as compound efficacy, stability or toxicity limitations, and no drugs on the market

Inactive Publication Date: 2010-12-29
INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although a series of IAPs inhibitors have been developed, there are no marketed drugs yet, and many compounds also involve limitations in potency, stability, or toxicity.

Method used

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  • Substitution five-heterocyclic alkyl aminoacyl compound and application thereof
  • Substitution five-heterocyclic alkyl aminoacyl compound and application thereof
  • Substitution five-heterocyclic alkyl aminoacyl compound and application thereof

Examples

Experimental program
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specific Embodiment approach

preparation example 1

preparation example 2

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PUM

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Abstract

The invention relates to a substitution five-heterocyclic alkyl aminoacyl compound and application thereof, in particular to a substitution five-heterocyclic alkyl aminoacyl derivative which has IAPs inhibition activity and is expressed by a general formula I and pharmaceutically-acceptable salt or hydrate thereof, wherein the definition of each substitution group in the general formula I is described in the specifications, and a preparation method of the compound expressed by the general formula I, a medicinal composition comprising the compound expressed by the general formula I or the pharmaceutically-acceptable salt or hydrate thereof, the application of the compound expressed by the general formula I or the pharmaceutically-acceptable salt or hydrate thereof to the production of medicaments and the application of the medicaments to the treatment or prevention of solid tumors and relevant rumor diseases derived from hematologic malignancies are all shown in the specifications.

Description

field of invention The present invention relates to substituted aminoacyl five-membered heterocycloalkane derivatives, their preparation method, pharmaceutical composition containing them and compounds with anti-tumor activity as IAPs (Inhibitor of Apoptosis Proteins) inhibitors the use of. Background technique Apoptosis, or programmed cell death, commonly occurs during the development and maintenance of healthy tissues in multicellular organisms. The apoptotic pathway is known to play an important role in embryonic development, viral pathogenesis, cancer, autoimmune and neurodegenerative diseases, among other events. Alterations in the apoptotic response have been found to be associated with the development of cancer, autoimmune diseases such as systemic lupus erythematosus and multiple sclerosis and with viral infections including those associated with herpesviruses, poxviruses and adenoviruses. IAPs (Inhibitor of Apoptosis Proteins) are endogenous inhibitors of caspase...

Claims

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Application Information

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IPC IPC(8): C07K5/062C07K5/083A61K38/05A61K38/06A61P35/00A61P35/02
CPCY02P20/55
Inventor 聂爱华顾为谭祖磊李斐汤立合陶林苏瑞斌李锦马小根
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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