Novel aminobenzoephenones

A compound of the general formula I

• 151
• wherein
• X represents oxygen, sulphur or N—ORC;
• R1 represents a substituent selected from the group consisting of halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, —CONH2, phenyl and nitro;
• R2 represents one or more, same or different substituents selected from the group consisting of hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, —CONH2, phenyl and nitro;
• R3 represents one or more, same or different substituents selected from the group consisting of hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, cyano, carboxy, carbamoyl, nitro, (C1-C10)alkyl, (C2-C10)olefinic group, (C3-C12) cyclic hydrocarbon group, (C1-C10)alkoxy, (C1-C10)alkylthio, (C1-C10)alkoxycarbonyl and phenyl;
• R4 represents hydrogen, (C1-C6)alkyl, (C2-C6)olefinic group, (C3-C6) cyclic hydrocarbon group or —C(O)O—C(Rd)(Re)(—O—C(O)—R14);
• wherein the R14 group are optionally substituted by one or more, same or different substituents represented by R8;
• R5 represents one or more, same or different substituents selected from the group consisting of hydrogen and R1;
• R6 represents (C1-C10)alkyl-heterocyclyl, (C1-C10)alkyl-(C3-C12)cyclic hydrocarbon group, (C1-C10)alkyl, (C2-C10)olefinic group, (C3-C12)cyclic hydrocarbon group, heterocyclyl, (C2-C10)alkynyl, Y1R21, Y2R22 or Y4R24;
• wherein the (C1-C10)alkyl, (C2-C10)olefinic group and (C3-C12)cyclic hydrocarbon group are substituted by one or more, same or different substituents represented by R7, and wherein the (C1-C10)alkyl-heterocyclyl, (C1-C10)alkyl-(C3-C12)cyclic hydrocarbon group, heterocyclyl and (C2-C10)alkynyl, are optionally substituted by one or more, same or different substituents represented by R7;
• R7 represents R12 Y—H or Y—R14;
• wherein the R12 and Y—R14 group are optionally substituted by one or more, same or different substituents represented by R8;
• R8 represents R12, Y—H, Y—R14 or R14;
• wherein the R12, Y—R14 and R14 group are optionally substituted by one or more, same or different substituents represented by R9;
• R9 represents R12, Y—H, Y—R14 or R14;
• wherein the R12, Y—R14 and R14 group are optionally substituted by one or more, same or different substituents represented by R10;
• R10 represents R12, Y—H, Y—R14 or R14;
• wherein the R12, Y—R14 and R14 group are optionally substituted by one or more, same or different substituents represented by R11;
• R11 represents R12 or R14;
• wherein the R12 and R14 group are optionally substituted by one or more, same or different substituents represented by R12;
• R12 represents halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, (C1-C9)trialkylammonium in association with an anion, (C2-C10)dialkylphosphinoyl, (C1-C5)alkyl(hydroxy)phosphinoyl, (C2-C10)dialkylphosphinoyloxy, (C1-C5)alkyl(hydroxy)phosphinoyloxy, dihydroxyphosphinoyl, dihydroxyphosphinoyloxy, cyano, azido, nitro, —CHO, —COOH, —CONH2, —CONHR′ or —CONRR′, wherein R and R′ represent (C1-C3)alkyl;
• Y represents —O—, —S—, —S(O)—, —S(O)2—, —NRa—, —NRaC(Z)—, —NRaC(Z)NRb—, —NRaC(Z)—, —C(Z)NRa—, —C(O)—, —C(S)—, —C(Z)O—, —C(O)Z—, —C(S)S— —OC(Z)—, —NRaC(Z)O—, —OC(Z)NRa—, —S(O)2O—, —OS(O)2—, —S(O)2NRa—, —NRaS(O)2—, —OC(Z)O—, —OC(Z)Z—, —OP(O)(ORa)O—, —P(O)(ORa)O—, —C(NRa)—, —C(NORa)—, —N═C(Ra)—, —N═C(ORa)—, —N(ORa)—, —ON(Ra)—, —N(Ra)O—, —N(Ra)C(═NRb)NRC—, —C(═NRa)NRb— or —N(Ra)C(═NRb)—;
• Z represents oxygen or sulphur;
• R14 represents (C1-C6)alkyl, (C2-C6)olefinic group, (C3-C12)cyclic hydrocarbon group, heterocyclyl or (C2-C6)alkynyl;
• Y1 represents —NRaC(S)NRb—, —C(O)—, —C(S)—, —C(S)O—, —C(O)S—, —C(S)S—, —OC(S)—, —OC(O)—, —NRaC(S)O—, —OC(Z)NRa—, —S(O)2O—, —OS(O)2—, —S(O)2NRa—, —NRaS(O)2—, —OC(Z)O—, —OC(Z)Z—, —OP(O)(ORa)O—, —P(O)(ORa)O—, —C(NRa)—, —C(NORa)—, —N═C(Ra)—, —N═C(ORa)—, —N(ORa)—, —ON(Ra)—, —N(Ra)O—, N(Ra)C(═NRb)NRC—, —C(═NRa)NRb— or —N(Ra)C(═NRb)—;
• R21 represents (C1-C10)alkyl-heterocyclyl, (C1-C10)alkyl-(C3-C12)cyclic hydrocarbon group, (C1-C10)alkyl, (C2-C10)olefinic group, (C3-C12)cyclic hydrocarbon group, heterocyclyl or (C2-C10)alkynyl;
• any of which are optionally substituted by one or more, same or different substituents represented by R7;
• Y2 represents —O—, —S—, —C(O)O— or —C(O)NRa)—;
• R22 represents (C1-C10)alkyl-heterocyclyl, (C1-C10)alkyl-(C3-C12)cyclic hydrocarbon group, heterocyclyl, (C2-C10)alkynyl, (C1-C10)alkyl, (C2-C10)olefinic group or (C3-C8)monocyclic hydrocarbon group;
• wherein the (C1-C10)alkyl is substituted by one or more, same or different substituents represented by R7 and wherein the (C1-C10)alkyl-heterocyclyl, (C1-C10)alkyl-(C3-C12)cyclic hydrocarbon group, heterocyclyl, (C2-C10)alkynyl, (C2-C10)olefinic group and (C3-C12)monocyclic hydrocarbon group are optionally substituted by one or more, same or different substituents represented by R7;
• Y4 represents —NRaC(O)NRbCH(Rc)—, —NRaC(O)NRbS(O)2—, —NRa—, —NRaC(Z)—, —NRaC(O)OCH(Rc)—, —NRaC(O)NRbC(Rd)(Re)—OC(O)— or —NRaC(O)OC(Rd)(Re)—OC(O)—;
• R24 represents (C1-C10)alkyl-heterocyclyl, (C1-C10)alkyl-(C3-C12)cyclic hydrocarbon group, heterocyclyl, (C2-C10)alkynyl, (C1-C10)alkyl, (C2-C10)olefinic group or (C3-C12)cyclic hydrocarbon group;
• wherein the (C1-C10)alkyl, (C2-C10)olefinic group and (C3-C12)cyclic hydrocarbon group are substituted by one or more, same or different substituents represented by R15, and wherein the (C1-C10)alkyl, (C2-C10)olefinic group, (C3-C12)cyclic hydrocarbon group, (C1-C10)alkyl-heterocyclyl, (C1-C0)alkyl-(C3-C12)cyclic hydrocarbon group, heterocyclyl and (C2-C10)alkynyl are optionally substituted by one or more, same or different substituents represented by R7;
• R15 represents R12a, R12b or R12c;
• wherein R12a, R12b and R12c are optionally substituted by one or more, same or different substituents represented by R7;
• R12a represents (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, —CONHR′ or —CONRR′ wherein R and R′ represent (C1-C3)alkyl;
• any of which are substituted by one or more, same or different substituents represented by R42;
• with the proviso that when R12a or R15, including further substitution by R42, represent groups of the formulas —(Q—O)n—Q or —CH2(Q—O)n—Q, wherein Q is a (C1-C3)alkyl and n is an integer larger than 1, then said groups comprise a continuous linear sequence of atoms with at least 16 atoms;
• R12b represents (C4-C10)alkoxy, (C4-C10)alkylthio, (C7-C12)alkylamino, (C4-C10)alkoxycarbonyl, —CONHR′ or —CONRR′ wherein R and R′ represent (C4-C10)alkyl;
• any of which are optionally substituted by one or more, same or different substituents represented by R7;
• R12c represents —Y5(C1-C10)alkyl, —Y-aryl, —Y-heterocyclyl, —Y—(C3-C12)cyclic hydrocarbon group and —Y—(C2-C10)olefinic group;
• any of which are optionally substituted by one or more, same or different substituents represented by R7;
• Y5 represents —S(O)—, —S(O)2—, —NRaC(Z)—, —NRaC(Z)NRb—, —C(S)NRa—, —C(O)—, —C(S)—, —C(S)O—, —C(O)S—, —C(S)S— —OC(Z)—, —NRaC(Z)O—, —OC(Z)NRa—, —S(O)2O—, —OS(O)2—, —S(O)2NRa—, —NRaS(O)2—, —OC(Z)O—, —OC(Z)Z—, —OP(O)(ORa)O—, P(O)(ORa)O—, C(NRa)—, —C(NORa)—, —N═C(Ra)—, —N═C(ORa)—, —N(ORa)—, —ON(Ra)—, N(Ra)O—, N(Ra)C(═NRb)NRC—, —C(═NRa)NRb— or —N(Ra)C(═NRb)—;
• R42 represents —Y—H, Y—R14, R52, halogen, trifluoromethyl, cyano, azido or nitro;
• wherein, R52 and —Y—R14 are optionally substituted by one or more, same or different substituents represented by R7;
• R52 represents (C6-C10)alkyl, (C2-C6)olefinic group, (C3-C12)cyclic hydrocarbon group, heterocyclyl, (C2-C6)alkynyl or heteroaryl;
• Ra, Rb, and Rc represent independently hydrogen, (C1-C6)alkyl, (C2-C6)olefinic group, (C3-C12)cyclic hydrocarbon group, aryl, heterocyclyl or (C2-C6)alkynyl;
• any of which are optionally substituted by one or more, same or different substituents represented by R12;
• Rd and Re independently represent hydrogen, (C1-C6)alkyl, (C2-C6)olefinic group or (C3-C12)cyclic hydrocarbon group;
• any of which are optionally substituted by one or more, same or different substituents represented by R12;
• and pharmaceutically acceptable salt, solvates and hydrates thereof.