Non-steroidal male hormone receptor regulating agent and medical uses thereof

An androgen receptor, non-steroidal technology, applied in the field of a class of non-steroidal androgen receptor modulators and their medical applications, can solve the problems such as the use has not been described

Inactive Publication Date: 2008-10-15
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although it is disclosed in the use that this type of compound has the effect of androgen receptor modulator, it only discloses the use of the compound as an androgen receptor antagonist, and does not make any reference to its use as an androgen receptor agonist. explain

Method used

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  • Non-steroidal male hormone receptor regulating agent and medical uses thereof
  • Non-steroidal male hormone receptor regulating agent and medical uses thereof
  • Non-steroidal male hormone receptor regulating agent and medical uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] Synthesis of 3-phenyl-3-(4-nitroanilino)-1-(4-chlorophenyl)-1-propanone (MWW6003)

[0062]

[0063] Add 10.60 grams (0.1mol) of benzaldehyde, 13.81 grams (0.1mol) of 4-nitroaniline, and 150ml of absolute ethanol into the reaction flask, stir at room temperature for 10 minutes, then add 15.46 grams (0.1mol) of 4-chloroacetophenone And catalytic amount of concentrated hydrochloric acid, then stirred at room temperature for 20 hours. After the reaction, the reaction solution was cooled overnight, and the precipitated solid was filtered with suction and washed with absolute ethanol. The resulting solid was suspended in 150ml of 95% ethanol, stirred at room temperature for 2 hours, washed with saturated NaHCO 3 Neutralize the solution to alkaline, continue to stir for 1 hour, filter with suction, wash the filter cake with a small amount of absolute ethanol, and recrystallize the crude product from a mixed solvent of ethanol / water (1:1) to obtain 29.09 g of needle crystal...

Embodiment 2

[0066] Synthesis of 3-phenyl-3-(4-nitroanilino)-1-(4-bromophenyl)-1-propanone (MWW6015)

[0067]

[0068] Add 10.60 grams (0.1mol) of benzaldehyde, 13.81 grams (0.1mol) of 4-nitroaniline, and 150ml of absolute ethanol into the reaction flask, stir at room temperature for 10 minutes, then add 19.91 grams (0.1mol) of 4-bromoacetophenone And catalytic amount of concentrated hydrochloric acid, then stirred at room temperature for 20 hours. After the reaction, the reaction solution was cooled overnight, and the precipitated solid was filtered with suction and washed with absolute ethanol. The resulting solid was suspended in 150ml of 95% ethanol, stirred at room temperature for 2 hours, washed with saturated NaHCO 3 Neutralize the solution to alkaline, continue to stir for 1 hour, filter with suction, wash the filter cake with a small amount of absolute ethanol, and recrystallize the crude product from a mixed solvent of ethanol / water (1:1) to obtain 30.66 g of needle crystals,...

Embodiment 3

[0071] Biological activity test

[0072] 1. Material equipment

[0073] 1.1 Plasmids and cell lines: androgen receptor expression plasmids and luciferase reporter gene plasmids were constructed by the National Center for Drug Screening; human cervical cancer epithelial cell line HeLa, human breast cancer cell line MDA-MB-453 and human prostate cancer cell line LNCaP were purchased from ATCC, USA.

[0074] 1.2 Reagents: fetal bovine serum (Fetal bovine serum, FBS, GIBCO / BRL, USA); activated carbon and dextran treated fetal bovine serum (CD-FBS, Hyclone, USA); DMEM and RPMI1640 medium (GIBCO / BRL, USA ); IMEM medium (Bioresource, USA), luciferase detection kit (Promega Corporation, USA); Fugene 6 (Roche Ltd., USA); [ 3 H] Dihydrotestosterone (Dehydrotestosterone, DHT, Amersham, UK); scintillation fluid (SuperMixTM, PerkinElmer, USA); androgen receptor protein is the expression product of the receptor gene in insect cells.

[0075] 1.3 Instruments: Envision 2101 Multilabel Read...

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PUM

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Abstract

The invention relates to a non-steroidal male sex hormone receptor modulator or the receivable slat thereof in pharmacy, in particular to a compound for preparing non-steroidal drugs used for preventing and/or curing the partial androgen deficiency in aging males, osteoporosis, myophagism, female sexual insufficiency, anorexia, female polytrichia, severe androgen-dependent type alopecia, acne, cachexia, benign prostatic hyperplasia, prostatic cancer, breast cancer, alzheimer disease, parkinsonism syndrome, etc. The invention also relates to a drug combination containing a general formula I compound or an acceptable salt thereof in pharmacy, and the use of the drug combination containing the general formula I compound or the acceptable salt in pharmacy for preparing drugs to cure the above symptoms or diseases.

Description

technical field [0001] The present invention relates to the use of a class of non-steroidal androgen receptor modulators and pharmaceutical compositions thereof in the prevention and / or treatment of symptoms or diseases caused by androgen and androgen receptor dysfunction, including but not limited to middle-aged and elderly people Androgen partial deficiency syndrome, osteoporosis, sarcopenia, female sexual insufficiency, anorexia, female hirsutism, severe androgen-dependent alopecia, acne, cachexia, benign prostatic hyperplasia, prostate cancer, Breast cancer, Alzheimer's disease (Alzheimer's disease, AD) and Parkinson's disease (Parkinson's disease, PD), etc. Background technique [0002] Androgen is an important class of steroidal sex hormones in the human body. It promotes cell differentiation and tissue growth by combining with Androgen Receptor (AR), and participates in many key physiological functions such as male fetal reproductive organs (such as prostate , semina...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C225/22A61K31/136A61P5/26
CPCC07C225/16A61P5/26A61P13/08A61P17/10A61P17/14A61P25/28A61P35/00A61P43/00
Inventor 王明伟武国海周彩红李群益
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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