8-AZABICYCLO[3,2,1]OCTANE COMPOUNDS AND THEIR APPLICATION AS MU-OPIOID RECEPTOR ANTAGONISTS Russian patent published in 2011 - IPC C07D451/02 A61K31/46 A61P1/10 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new compounds of formula (I): , where: R¹ is selected from -OR^a, -C(O)NR^aR^b, -NHS(O)₂R^c, -C(O)OR^a; A means C_1-4alkylenyl; R² means C_3-12cycloalkyl or C_6-10aryl which is optionally substituted by one -OR^a, one or two halogen atoms, one or two C_1-3alkyls substituted by two or three halogen atoms; or one, two, three or four C_1-3alkyls; G means C_1-4alkylenyl; R³ is selected from hydrogen, -C(O)R⁴, -C(O)NHR⁵, -S(O)₂R^c and -S(O)₂NR^aR^b; R⁴ means C_3-6cycloalkyl or C_1-6alkyl, C_3-6cycloalkyl is optionally substituted by one -OR^a, and C_1-6alkyl is optionally substituted by one or two substitutes selected from -OR^a, -C(O)OR^a, -S(O)₂R⁶, -C(O)NR^aR^b, -NR^aR^b, -CN, C_3-6cycloalkyl and phenyl; or by one -D-(CH₂)_j-R⁷ where D means , j is equal to 1, n is equal to 1 or 2; R⁶ means C_1-3alkyl optionally substituted by R⁷; R⁷ means -C(O)OR^a; R⁵ means C_1-6alkyl, benzo[1.3]dioxole or -(CH₂)_q-phenyl; where phenyl is optionally substituted by one or two substitutes selected from halogen, -OR^a, C_1-3alkiyl and C_1-3alkoxy where C_1-3alkyl and C_1-3alkoxy optionally substituted by 2 or 3 halogen atoms, and q is equal to 0, 1; R^a and R^b independently mean hydrogen or C_1-4alkyl; and R^c means C_1-3alkyl; provided when R² means phenyl substituted in position 4, R³ is not -C(O)R⁴ where R⁴ means C_1-4alkyl substituted by C(O)OR^a; to their pharmaceutically acceptable salts. Also, the invention refers to a pharmaceutical composition, to a method of preparing the compound of formula (I), to compounds of formula (II), (III), to application of the compounds on any claim 1-14, to a method of analysing a biological system or a sample containing a mu-opioid receptor, and also to a method of treating a mammal suffering a disease caused by mu-opioid receptor activity.

EFFECT: production of the new biologically active compounds exhibiting mu-opioid receptor antagonist activity.

26 cl, 204 ex