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US 2007/0167474 A1Published application
Use of opioid receptor antagonist compounds for the prevention and/or treatment of diseases associated with the target calcineurin
OwnerHelmut Schmidhammerinventor
Life of this patent
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Abstract
Morphinane derivatives of the formula (I) their pharmaceutically acceptable salts are provided for use as medicaments for the treatment and/or prevention of disorders associated with the target calcineurin.
Claims13
Use of a compound according to the formula (I)
- wherein
- R1 represents C1-C10 alkenyl;
- C4-C10 cycloalkylalkyl wherein the cycloalkyl is C3-C6 cycloalkyl and the alkyl is C1-C4 alkyl;
- C4-C10 cykloalkenylalkyl wherein the cycloalkenyl is C3-C6 cykloalkenyl and the alkyl is C1-C4 alkyl;
- C7-C16 arylalkyl wherein the aryl is C6-C10 aryl and the alkyl is C1-C6 alkyl;
- C8-C16 arylalkenyl wherein the aryl is C6-C10 aryl and the alkenyl is C2-C6 alkenyl;
- R2 represents hydrogen, hydroxy, C1-C6 alkoxy;
- C1-C6 alkenyloxy;
- C7-C16 arylalkyloxy wherein the aryl is C6-C10 aryl and the alkyloxy is C1-C6 alkyloxy;
- C7-C16 arylalkenyloxy wherein the aryl is C6-C10 aryl and the alkenyloxy is C1-C6 alkenyloxy;
- C1-C6 alkanoyloxy;
- C7-C16 arylalkanoyloxy wherein the aryl is C6-C10 aryl and the alkanoyloxy is C1-C6 alkanoyloxy;
- R3 represents hydrogen, C1-C6 alkyl;
- C1-C6 alkenyl;
- C7-C16 arylalkyl wherein the aryl is C6-C10 aryl and the alkyl is C1-C6 alkyl;
- C7-C16 arylalkenyl wherein the aryl is C6-C10 aryl and the alkenyl is C1-C6 alkenyl;
- hydroxy(C1-C6)alkyl;
- alkoxyalkyl wherein the alkoxy is C1-C6 alkoxy and the alkyl is C1-C6 alkyl;
- CO2H;
- CO2(C1-C6 alkyl);
- R4 is hydrogen, hydroxy;
- C1-C6 alkoxy;
- C7-C16 arylalkyloxy wherein the aryl is C6-C10 aryl and the alkyloxy is C1-C6 alkyloxy;
- C1-C6 alkenyloxy;
- C1-C6 alkanoyloxy;
- C7-C16 arylalkanoyloxy wherein the aryl is C6-C10 aryl and the alkanoyloxy is C1-C6 alkanoyloxy;
- C2-C10 alkyloxyalkoxy wherein alkyloxy is C1-C4 alkyloxy and alkoxy is C1-C6 alkoxy;
- R5 and R6 each independently represent hydrogen;
- OH;
- C1-C6 alkoxy;
- C1-C6 alkyl;
- hydroxyalkyl wherein the alkyl is C1-C6 alkyl;
- halo;
- nitro;
- cyano;
- thiocyanato;
- trifluoromethyl;
- CO2H;
- CO2(C1-C6 alkyl);
- CONH2;
- CONH(C1-C6 alkyl);
- CON(C1-C6 alkyl)2;
- amino;
- C1-C6 monoalkyl amino;
- C1-C6 dialkyl amino;
- C5-C6 cycloalkyl amino;
- SH;
- SO3H;
- SO3(C1-C6 alkyl);
- SO2(C1-C6 alkyl);
- SO2NH2;
- SO2NH(C1-C6alkyl);
- SO2NH(C7-C20 arylalkyl);
- SO(C1-C6 alkyl;
- or R5 and R6 together form a phenyl ring which may be unsubstituted or substituted by halo, nitro, cyano, thiocyanato;
- C1-C6 alkyl;
- trifluoromethyl;
- C1-C6 alkoxy, CO2H, CO(C1-C6 alkyl), amino, C1-C6 monoalkylamino, C1-C6 dialkylamino, SH;
- SO3H;
- H;
- SO3(C1-C6 alkyl), SO2(C1-C6 alkyl), SO(C1-C6 alkyl), and
- X represents oxygen;
- sulfur;
- CH═CH or NR9 wherein R9 is H, C1-C6 alkyl, C1-C6 alkenyl, C7-C16 arylalkyl
- wherein the aryl is C6-C10 aryl and the alkyl is C1-C6 alkyl, C7-C16 arylalkenyl wherein the aryl is C6-C10 aryl and the alkenyl is C1-C6 alkenyl;
- C1-C6 alkanoyl, and wherein aryl is unsubstituted or mono- or di- or trisubstituted independently with hydroxy, halo, nitro, cyano, thiocyanato, trifluoromethyl, C1-C3 alkyl, C1-C3 alkoxy, CO2H, CO2(C1-C3)alkyl, CONH2, CONH(C1-C3 alkyl), CON(C1-C3 alkyl), CO(C1-C3 alkyl), amino, (C1-C3 monoalkyl)amino, (C1-C3 dialkyl)amino, C5-C6 cycloalkylamino(C1-C3 alkanoyl)amino, SH, SO3H, SO3(C1-C3 alkyl), SO2(C1-C3 alkyl), SO(C1-C3 alkyl), C1-C3 alkylthio or C1-C3 alkanoylthio;
- and
- with the proviso that when R2 is hydroxy, R3 cannot be hydrogen, except when R4 is hydrogen, OCH2OCH3, OCH2OC2H5 or OC(Ph)3 and pharmacologically acceptable salts thereof, for the preparation of a medicament for the treatment and/or prevention of disorders susceptible to the inhibition of the target cacineurin.
65 more elements
Dependencies are inferred from the claim text.