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Compound and composition as well as application thereof to drugs preparation

A technology of compounds and compositions, applied in the field of novel antagonist compounds, capable of solving problems such as insignificant ability of prostate cancer cells

Active Publication Date: 2018-12-11
CHANGSHA ZEDA MEDICAL TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the ability of the above-mentioned drugs to directly kill prostate cancer cells is not significant. In cell biology experiments, their IC50 is above 10uM

Method used

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  • Compound and composition as well as application thereof to drugs preparation
  • Compound and composition as well as application thereof to drugs preparation
  • Compound and composition as well as application thereof to drugs preparation

Examples

Experimental program
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Embodiment Construction

[0036] Compounds of the present invention have the structure of formula I:

[0037]

[0038] Wherein, R1 is selected from hydrogen, fluorine, chlorine; R2 and R3 are independently selected from hydrogen, alkyl, substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, aryl, R2 and R3 can be connected to form a ring which can be cycloalkyl, substituted cycloalkyl, aromatic heterocycle or non-aromatic heterocycle; R4 is selected from hydrogen, cyano, alkyl, substituted alkyl, alkenes Base or substituted alkenyl, alkynyl or substituted alkynyl, aryl; R5 is selected from hydrogen, halogen, haloalkyl.

[0039] The term "alkyl" as used herein denotes a branched or straight hydrocarbon chain, preferably having from about 1 to about 5 carbons, such as methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl , Isobutyl, tert-butyl, 2-methylpentyl, pentyl, etc. "Substituted alkyl" means that the aforementioned alkyl is replaced by one or more functional group...

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Abstract

The present invention relates to a compound having a structure of formula I or a pharmaceutically acceptable salt of the compound. Regarding the compound, R1 is selected from hydrogen, fluorine, and chlorine; R2 and R3 are independently selected from hydrogen, alkyl, substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, and aryl, wherein R2 and R3 can be bonded to forma ring, and the ring can be cycloalkyl, substituted cycloalkyl, an aromatic heterocyclic ring or a non-aromatic heterocyclic ring; R4 is selected from hydrogen, cyano, alkyl, substituted alkyl, alkene or substituted alkenyl, alkynyl or substituted alkynyl, and aryl; R5 is selected from hydrogen, halogen, and haloalkyl. The invention further relates to a pharmaceutical composition comprising the compound. The compound and composition provided by the invention shows significant activity in the treatment of prostate cancer. (The formulas are shown in the description.).

Description

technical field [0001] The present invention relates to novel antagonist compounds of the androgen receptor; to methods of using such compounds in the treatment of diseases associated with the androgen receptor, such as prostate cancer; and to pharmaceutical combinations comprising these compounds. Background technique [0002] Androgen receptor (AR) is a ligand-dependent transcriptional regulatory protein that belongs to the nuclear receptor superfamily. Binding of the androgen receptor and an androgen, such as testosterone or, more effectively, dihydrotestosterone (DTH), results in a conformational change leading to activation of the androgen receptor. The activated androgen receptor binds to a specific DNA sequence in the nucleus of the target cell in the form of a dimer - the Androgen Response Element (ARE), regulates the expression of the target gene, and produces corresponding biological effects on cell proliferation, survival and differentiation. The androgen recepto...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D235/02C07D233/86C07D401/04A61K31/4184A61K31/4166A61K31/4439A61P35/00
CPCA61P35/00C07D233/86C07D235/02C07D401/04A61K31/4166A61K31/4184
Inventor 陈永恒徐广宇周文强
Owner CHANGSHA ZEDA MEDICAL TECH CO LTD
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