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A class of piperidinylacetamide compounds capable of inhibiting epidermal growth factor receptors and applications thereof

A technology of epidermal growth factor and acetamide, which is applied in the field of medicine and can solve problems such as drug-resistant mutations of tumor cells

Inactive Publication Date: 2017-10-31
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In clinical practice, although the first-generation EGFR inhibitors have good therapeutic effects on tumors, tumor cells often develop drug-resistant mutations after a period of treatment, such as T790M mutations, etc.

Method used

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  • A class of piperidinylacetamide compounds capable of inhibiting epidermal growth factor receptors and applications thereof
  • A class of piperidinylacetamide compounds capable of inhibiting epidermal growth factor receptors and applications thereof
  • A class of piperidinylacetamide compounds capable of inhibiting epidermal growth factor receptors and applications thereof

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Embodiment 1

[0034] 1. Detection method

[0035] The homogeneous time-resolved fluorescence (HTRF) method is divided into two steps: one is the enzymatic reaction, that is, when the reaction is started after adding ATP, the kinase phosphorylates the substrate, and the phosphate is connected to the biotin-labeled substrate. The second is the termination and detection process, in which EDTA terminates the reaction, there is europium element labeled anti-phosphorylated tyrosine antibody close to the phosphate of the substrate, and the allophycocyanin labeled XL665 binds to the substrate On biotin labeling, two fluorescent groups undergo energy resonance transfer and generate fluorescence at 665nm when they are close to each other, and free TK antibody (labeled europium ion) generates fluorescence at 620nm, and this signal can be used as a background signal, while Free SA-XL665 only produces transient fluorescence, which can be ignored by delaying the detection time (detection 1 hour after add...

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PUM

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Abstract

The invention belongs to the technical field of medicines and discloses a piperidyl acetamide compound capable of inhibiting epidermal growth factor receptor (EGFR) and an application thereof. A structure of the piperidyl acetamide compound capable of inhibiting the EGFR is represented as the general formula (I), wherein R1 is a naphthenic group, an aromatic group or a substituted aromatic group being 4-7 in carbon number; and R2 is an alkyl group being 1-10 in carbon number, or a naphthenic group being 4-7 in carbon number, an aromatic group or a substituted aromatic group. The compound can be used for preparing an EGFR antagonist and provides more selections for preparation of targeted anti-tumor drugs.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a class of piperidinylacetamide compounds capable of inhibiting epidermal growth factor receptors and applications thereof. Background technique [0002] Epidermal growth factor receptor (EGFR) is a kind of cell membrane receptor of growth factor family, including 4 main members: EGFR (ErbB1), HER2 (ErbB2), HER3 (ErbB3) and HER4 (ErbB4). The EGFR family is a transmembrane receptor with tyrosine kinase activity, which can be divided into three parts: the extracellular region, the transmembrane region and the intracellular region. Ligands such as EGF bind to the extracellular region of EGFR family receptors, and the ligands themselves mediate EGFR dimerization to form homologous or heterologous dimers, and then phosphorylate the receptors to activate tyrosine kinases The receptor triggers the activation of a series of downstream signal transduction pathways, such as: Ras / Raf / MEK / ER...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D211/34A61P35/00
CPCC07D211/34
Inventor 林森森顾铭袁胜涛孙立严明张陆勇吴亮高鹏练进
Owner CHINA PHARM UNIV
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