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Heteroaryl-keto-fused azadecalin glucocorticoid receptor modulators

A phenyl and ketone technology, applied in four R2 fields, can solve the problems of no positioning and GR-β inequality

Active Publication Date: 2018-10-02
CORCEPT THERAPEUTICS INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since these include a ligand-binding domain, GR-β cannot bind ligand, is constantly localized in the nucleus, and has no transcriptional activity

Method used

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  • Heteroaryl-keto-fused azadecalin glucocorticoid receptor modulators
  • Heteroaryl-keto-fused azadecalin glucocorticoid receptor modulators
  • Heteroaryl-keto-fused azadecalin glucocorticoid receptor modulators

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0080] Example 1. (R)-(1-(4-fluorophenyl)-6-((4-(trifluoromethyl)phenyl)sulfonyl)-4,4a,5,6,7,8- Hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(pyridin-2-yl)methanone,

Embodiment 1A

[0081] Example 1A. (R)-(1-(4-fluorophenyl)-6-((4-(trifluoromethyl)phenyl)sulfonyl)-4,4a,5,6,7,8- Hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(1-methyl-1H-imidazol-2-yl)methanone,

Embodiment 1B

[0082] Example 1B. (R)-(1-(4-fluorophenyl)-6-((4-(trifluoromethyl)phenyl)sulfonyl)-4,4a,5,6,7,8- Hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(pyridin-3-yl)methanone,

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Abstract

The present invention provides heteroaryl ketone-fused azadecalin compounds and methods of using the compounds as modulators of the glucocorticoid receptor. In some embodiments, the present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of formula I. In some embodiments, the present invention provides a method of modulating glucocorticoid receptors, the method comprising contacting glucocorticoid receptors with a compound of formula I, thereby modulating the glucocorticoid receptors, and a method of modulating A method of treating a disease with glucocorticoids, the method comprising administering a therapeutically effective amount of a compound of formula (I) to a subject in need of such treatment, thereby treating the disease.

Description

[0001] Cross References to Related Applications [0002] This application claims U.S. Provisional Application No. 61 / 781,269, filed March 14, 2013, U.S. Provisional Application No. 61 / 759,520, filed February 1, 2013, U.S. Provisional Application No. 61 / 715,907, filed October 19, 2012 , U.S. Provisional Application No. 61 / 691,083, filed August 20, 2012, and U.S. Provisional Application No. 61 / 651,669, filed May 25, 2012, which are hereby incorporated by reference in their entirety for all purposes. Background technique [0003] In most species, including humans, the physiological glucocorticoid is Cortisol (hydrocortisone). Glucocorticoids are secreted in response to ACTH (adrenocorticotropic hormone), which exhibits changes in circadian rhythm and rises in response to stress and food. Cortisol levels respond within minutes to many physical and physiological stressors, including trauma, surgery, exercise, anxiety and depression. Cortisol is a steroid and acts by binding to th...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D471/02C07D471/04C07D519/00A61K31/5377
CPCC07D471/04A61P25/22A61P25/24A61P29/00A61P3/04A61P43/00A61P5/46A61P9/12A61K31/5377C07D471/02A61K31/4725A61K31/497A61K31/506A61K31/5383C07D498/04
Inventor H·亨特T·约翰逊N·雷I·沃尔特斯
Owner CORCEPT THERAPEUTICS INC