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Morphinan derivatives containing a carboxamide group as opioid receptor ligands
专利权人:
Rensselaer Polytechnic Institute
发明人:
WENTLAND, Mark P.
申请号:
ES11715100
公开号:
ES2582306T3
申请日:
2011.03.22
申请国别(地区):
ES
年份:
2016
代理人:
摘要:
Compound of formula I: ** Formula ** where R1 is selected from -OH, -CN, -CHO, -COR10, -COOR10, -SO2R10, -CONH2, -CSNH2, - CONR10 ((C (R12) (R13) ) tCO-NR10R11, -CONR10 ((C (R12) (R13)) tCOOR11, -C (>; = S) R10 and -C (>; = NR10) R11; R2 is selected from hydrogen, halogen, -OH, -CN , -CHO, -OCH3, -OCH2CH3, -OCH (CH3) 2, - NO2, -COR10, -COOR10, -SO2R10, -CONR10R11, -CSNR10R11, -CONR10NR11R12, -CONR10OR11, -CONR10 ((C (R12) ( R13)) tCONR10R11, -CONR10 ((C (R12) (R13)) tCOOR11, -C (>; = S) R10, -C (>; = NOR11) R10, - C (>; = NR10) R11, -SO2NR10R11, heterocyclyl , optionally substituted (C1-C6) alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted aryl, halo (C1-C6) alkyl, halo (C1-C6) haloalkoxy, and (C1-C6) alkylthio; or, R1 and R2, together with the atoms to which they are attached and a fragment selected from -OCH2O-and -OCH2CH2O-, they form a ring; R3 is selected from hydrogen, hydrocarbon (C1-C8), heterocyclyl, aryl and hydroxyalkyl; R4 is selected from hydrogen , hydr oxyl, amino, (C1-C4) alkoxy, (C1-C20) alkyl and (C1-C20) alkyl substituted with hydroxyl or carbonyl; R5 is (C1-C6) alkyl; R6 is (C1-C6) alkyl; R7 is selected from hydrogen, NR10R11 and -OR10; or R4, R5, R6 and R7 together can form one, two, three or four rings, said rings having an optional additional substitution; R8 and R8a are both hydrogen, or R8 and R8a together are>; = O; R9 is selected from hydrogen and (C1-C6) alkyl; R10, R11, R12 and R13 are, independently in each case, hydrogen, optionally substituted (C1-C6) alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted aryl, hydroxy, -NR100R101 or optionally substituted (C1-C4) alkoxy , or R10 and R11, together with the nitrogen atom to which they are attached, form an optionally substituted fused heterocyclic or carbocyclic ring, of 5 to 7 ring members, of which up to 3 can be heteroatoms selected from N, O and S ; t is 0, 1, 2, 3, 4, 5 or 6;Compuesto de
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