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
Title | Year | Author | Number |
---|---|---|---|
AZADECALINS CONDENSED WITH HETEROARYLKETONES - GLUCOCORTICOID RECEPTOR MODULATORS | 2013 |
|
RU2639867C2 |
OXAZINMONOACYLGLYCERIN LIPASE (MAGL) INHIBITORS | 2019 |
|
RU2794334C2 |
TRICYCLIC TRIAZOLIC COMPOUNDS | 2014 |
|
RU2666728C2 |
HUMAN IMMUNODEFICIENCY VIRUS REPLICATION INHIBITORS | 2019 |
|
RU2812128C2 |
SUBSTITUTED [1,2,4]TRIAZOLO[1,5-A]PYRIMIDINE-7-YL COMPOUNDS AS THE INHIBITORS OF PDE2 | 2015 |
|
RU2659070C9 |
METHOD FOR PRODUCING PHARMACEUTICAUY ACCEPTABLE SALTS OF TRANS-4AR-6H-PROPYL-4,4A,5,6,7,8,8A,9-OCTAHYDRO-1H (AND 2H)PYRAZOLO(3,4-D)QUINONE | 0 |
|
SU1299506A3 |
NOVEL HETEROCYCLIC COMPOUNDS AS MONOACYLGLYCEROL LIPASE INHIBITORS | 2019 |
|
RU2769507C1 |
NOVEL COMPOUNDS | 2015 |
|
RU2691389C2 |
SUBSTITUTED HETEROCYCLIC FUSED CYCLIC COMPOUND, METHOD FOR PRODUCTION THEREOF AND PHARMACEUTICAL USE THEREOF | 2020 |
|
RU2815814C1 |
PYRAZINE COMPOUNDS AND THEIR USE | 2019 |
|
RU2809631C2 |
Authors
Dates
2018-12-14—Published
2014-11-21—Filed