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Imidazolyl progesterone antagonists

A technology of imidazolyl and alkyl, applied in the field of preparation of new compounds, can solve problems such as omission

Active Publication Date: 2016-04-27
EVESTRA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] In those patents, a variety of 11' substituents including different heterocycles have been described, but surprisingly, 11'N-imidazoles have not been reported, probably because the synthesis of these molecules requires special methods and omissions, but the general formula The structure has been claimed by Cook et al. in WO99 / 45022

Method used

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  • Imidazolyl progesterone antagonists
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Examples

Experimental program
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Effect test

Embodiment 1

[0219] Nuclear receptor analysis

[0220] Using GeneBLAzer TM Invitrogen’s β-lactamase reporter technology The Cell Based Nuclear Receptor Assay service performs the determination of the agonist / antagonist properties of test compounds. Essentially this assay uses a β-lactamase cDNA under the transcriptional control of an upstream activating sequence (UAS). UAS is activated by the GAL4 transcription factor DNA-binding domain (DBD), which is expressed as a fusion protein containing the ligand-binding domain (LBD) of the target receptor. Upon ligand binding, GAL4(DBD)-NR(LDB) binds to UAS, thereby controlling the transcription of β-lactamase. β-lactamases cleave specially engineered fluorogenic substrates, resulting in a change in the measured fluorescence wavelength.

[0221] The general protocol for progesterone antagonist screening initiated by the control agonist R5020 is as follows:

[0222] Progesterone receptor-LBD-UAS-blaHEK293T cells were thawed and prepared as d...

Embodiment 2

[0228] Pregnant guinea pig model as described by Walter Elger et al., J. Steroid Biochem, Vol. 25, No. 5B, pp. 835-845, 1986:

[0229] Adult female guinea pigs weighing approximately 500 g were housed and tested for cycle status by daily inspection of the vaginal opening.

[0230] In the second period, three females were co-housed with one male on day 15 following day 1 of testing the vaginal opening. Day 16 of the cycle was considered pregnancy day 1. Pregnant animals were randomized into different treatment groups and treated subcutaneously on days 43 and 44 of gestation with the test substances dissolved in 0,2 ml benzyl benzoate / castor oil. Animals were examined for vaginal bleeding and the number and timing of abortions. figure 1 shows a test result of 3mg / a / d, while figure 2 Test results for 10 mg / a / d are shown.

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Abstract

Described herein are imidazolyl compounds that exhibit progesterone antagonism without any sign of partial agonistic activity. Such compounds have application in fertility control and in the treatment of hormone dependent breast cancer. The present invention also relates to processes of preparation and the use in therapy of such novel compounds.

Description

technical field [0001] The present invention relates to novel compounds which exhibit progesterone antagonism without any signs of partial agonistic activity. These compounds have applications in birth control and the treatment of hormone-dependent breast cancer. The invention also relates to processes for the preparation and therapeutic use of these novel compounds. Background technique [0002] In the past, it has been hypothesized that progesterone antagonists may be beneficial in the treatment of a variety of diseases, including breast cancer and different forms of birth control. [0003] So far, only two compounds that fall into this category have been approved for clinical use. The prototype antagonist Mifepristone (Mifepristone) (see figure 1 ) is prescribed for the induction of abortion, and Ulipristal is approved for postcoital birth control. [0004] Both compounds were characterized as progesterone receptor modulators, suggesting that there may be a partial ag...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/58C07J43/00A61P35/00
CPCC07J21/006C07J71/001C07J43/003A61P15/00A61P15/04A61P35/00A61P43/00A61P5/36A61P15/08C07J21/00A61K31/58C07J21/003
Inventor K·尼克基希W·埃尔格B·桑塔哈马
Owner EVESTRA
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