8-AZABICYCLO[3,2,1]OCTAN-8-CARBOXAMIDE DERIVATIVE Russian patent published in 2016 - IPC C07D451/02 C07D451/04 C07D451/06 A61K31/497 A61K31/501 A61K31/506 A61K31/5377 A61P1/00 A61P3/00 A61P5/14 A61P7/04 A61P25/00 A61P9/00 

Abstract RU 2574597 C2

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds of formula

and their pharmaceutically acceptable salts having the property of 11β dehydrogenase hydroxysteroid type 1 (11βHSD1) inhibitor, based medicinal and therapeutic agents, a method for prevention or treatment with using them, and using them for treating 11βHSD1-mediated diseases, such as type 2 diabetes mellitus, impaired glucose tolerance, hyperglycemia, insulin resistance, lipid dismetabolism, hypertension, arterial sclerosis, angiosclerosis, etc. In formula (1) A represents a group, which is presented by formula ; R1a and R1b are identical or different, and each independently represents C1-6 alkyl, which can be optionally substituted by 1-3 halogen atoms; each of m and n independently represents an integer from 0 to 5; X1 represents hydroxyl or aminocarbonyl; Z1 represents a single bond, oxygen atom, sulphur atom, -SO-, -SO2- or -N(R3)-; R2 represents optionally substituted C1-6 alkyl, optionally substituted C3-7 cycloalkyl, optionally substituted C6-10 aryl, optionally substituted C7-16 aralkyl, optionally substituted 3-7-merous heterocycle, optionally substituted 3-7-merous heterocyclic C1-6 alkyl, optionally substituted 5-12-merous mono- or polycyclic heteroaryl, optionally substituted 5-12-merous mono- or polycyclic heteroaryl-C1-6 alkyl, or optionally substituted 5-7-merous cyclic amino group; R3 represents C1-6 alkyl, C3-7 cycloalkyl, C6-10 aryl, or C7-16 aralkyl; or its pharmaceutically acceptable saly.

EFFECT: producing the pharmacologically acceptable salts possessing the property of 11β hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor.

42 cl, 47 tbl, 438 ex

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RU 2 574 597 C2

Authors

Khoriuti Esikhiro

Savamura Kieto

Fudzivara Khiroaki

Dates

2016-02-10Published

2010-11-11Filed