OCTAHYDRO FUSED AZADECALIN GLUCOCORTICOID RECEPTOR MODULATORS Russian patent published in 2018 - IPC C07D471/04 C07D498/04 A61K31/4745 A61K31/5383 A61P1/04 A61P3/04 A61P3/10 A61P9/10 A61P11/06 A61P19/02 A61P25/14 A61P25/16 A61P25/28 A61P25/32 A61P29/00 A61P31/18 A61P35/00 A61P37/00 

Abstract RU 2674983 C1

FIELD: chemistry.

SUBSTANCE: present invention provides octahydro fused azadecalin compounds of general formula (I) or stereoisomers thereof and pharmaceutically acceptable salts thereof. In formula (I) R1 is a heteroaryl ring selected from pyridine and thiazole, optionally substituted with 1–4 groups, each of which is independently selected from R1a; each R1a is independently selected from a group consisting of hydrogen, C1-6 alkyl, C1-6 haloalkyl; ring J is selected from the group consisting of phenyl, pyridine, pyrazole, and triazole; each of R2 independently selected from the group consisting of hydrogen, C1-6 alkyl, halogen, C1-6 haloalkyl and -CN; or alternatively two R2 groups on adjacent atoms of the ring are combined to form a morpholino ring, each R3a independently represents halogen; the subscript n is an integer from 1 to 3. Said compounds have a glucocorticoid receptor binding affinity and modulatory activity suitable for pharmaceutical use. Also provided is a pharmaceutical composition comprising an effective amount of a compound of formula (I), and the use of said compounds in methods of treating glucocorticoid receptor mediated disorders in a subject.

.

EFFECT: octahydro fused azadecalin glucocorticoid receptor modulators are disclosed.

16 cl, 4 dwg, 1 tbl, 3 ex

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RU 2 674 983 C1

Authors

Khant Khejzel

Uolters Ian

Gurdet Benua

Dates

2018-12-14Published

2014-11-21Filed