Alpha-ketoamide derivatives

A compound of the general formula I

• wherein
• R1 represents lower alkyl, halo-lower alkyl, cyano-lower alkyl, lower alkylthio-lower alkyl, aryl-lower alkylthio-lower alkyl, aryl-lower alkyl, heteroaryl-lower alkyl, lower alkenyl, or lower alkynyl;
• R2 represents lower alkyl, hydroxy-lower alkyl, carboxy-lower alkyl, aryl-lower alkyl, aminocarbonyl-lower alkyl, lower cycloalkyl-lower alkyl, aryl-lower alkoxy-aryl-lower alkyl, heteroaryl-lower alkyl, or dihalo aryl lower alkoxy aryl-lower alkyl;
• R3 represents hydrogen or lower alkyl;
• or
• R2 and R3 together form a cyclic bridge selected from the group consisting of —CH2—CH2—, —CH2—CH2—CH2—, —CHOH—CH2—, —CH2—CHOH—, —CH2—CH2—CHOH—, —CH2—CHOH—CH2—, and —CHOH—CH2—CH2—;
• R4 represents lower alkyl, hydroxy-lower alkyl, lower cycloalkyl-lower alkyl, carboxy-lower alkyl, aryl-lower alkyl, aryl-lower alkoxy-aryl-lower alkyl, aryl-lower alkoxy-lower alkyl, aryl-lower alkoxycarbonyl-lower alkyl, lower alkylthio-lower alkyl, cyano-lower alkylthio-lower alkyl, aryl-lower alkylthio-lower alkyl, lower alkenyl, aryl, heteroaryl-lower alkyl, arylsulphonyl-guanidino-lower alkyl, acetamidothio-lower alkyl, lower alkylcarbonylamino-lower alkyl, formamido-lower alkyl, or lower cycloalkyl;
• R5 represents lower alkyl, hydroxy-lower alkyl, lower alkylthio-lower alkyl, aryl-lower alkyl, aryl-lower alkylthio-lower alkyl, cyano-lower alkylthio-lower alkyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl-lower alkoxycarbonyl-lower alkyl, aryl-lower alkoxy-aryl-lower alkyl, aryl, arylsulphonyl-guanidino-lower alkyl, aryl-lower alkoxy-lower alkyl, heteroaryl-lower alkyl, or formamido-lower alkyl;
• R6 represents hydrogen or lower alkyl;
• R7 represents hydrogen, lower alkyl, carboxy-lower alkyl, hydroxy-lower alkyl, aryl-lower alkyl, lower cycloalkyl-lower alkyl, lower cycloalkyl, aryl, heteroaryl-lower alkyl, nitroguanidino-lower alkyl, aryl-lower alkoxy-lower alkyl, aryl-lower alkylthio-lower alkyl, aryl-lower alkoxycarbonyl-lower alkyl, arylsulphonylguanidino-lower alkyl, acetamidothio-lower alkyl, lower alkylsulphonyl-lower alkyl, heteroaryl-lower alkyl, aryl-lower alkoxy-aryl-lower alkyl, aryl-lower alkoxy-heteroaryl-lower alkyl, lower alkylcarbonyloxy-lower alkyl, lower alkylcarbonylamino-lower alkyl, aryl-lower alkyl-heteroaryl-lower alkyl, lower alkenyloxycarbonyl-lower alkyl, lower alkylthio-lower alkyl, formamido-lower alkyl, or nitro substituted aryl-lower alkyl;
• R8 represents lower alkyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, carboxy-lower alkyl, hydroxy-lower alkyl, hydroxy substituted aryl-lower alkyl, aryl-lower alkyl, mercapto-lower alkyl, lower alkylsulphonyl-lower alkyl, aryl-lower alkoxy-lower alkyl, aryl-heteroaryl-lower alkyl, aryl-lower alkoxy-aryl-lower alkyl, nitroguanidino-lower alkyl, aryl, acetamidothio-lower alkyl, aryl-sulphonylguanidino-lower alkyl, aminocarbonyl-lower alkyl, aryl-lower alkoxy-lower alkyl-heteroaryl-lower alkyl, lower alkylsulphinyl-lower alkyl, lower alkylamino-carbonyl-lower alkyl, heteroaryl-lower alkyl, lower alkylthio-lower alkyl or formamido-lower alkyl;
• and
• R9 represents hydrogen or lower alkyl;
• or
• R8 and R9 together form a cyclic bridge selected from the group consisting of —CH2—CH2—CH2—, —CH2—S—CH2—, —CH2—CH2—S—, and —S—CH2—CH2—;
• R10 represents lower alkylcarbonyl, carboxy-lower alkylcarbonyl, arylcarbonyl, lower alkoxycarbonyl, aryl-lower alkoxycarbonyl, aryl-lower alkylcarbonyl, heteroaryl-lower alkylcarbonyl, arylamino-carbonyl-lower alkylcarbonyl, heteroarylthio-lower alkylcarbonyl, heteroarylcarbonyl, hydroxyfluorenylcarbonyl, heteroarylcarbonyl-lower alkylcarbonyl, lower alkoxy-lower alkylcarbonyl, aryl-carbonyl-lower alkylcarbonyl, lower alkoxy-lower alkoxy-lower-alkoxy-lower alkylcarbonyl, aryl-carbonyl-amino-lower alkylcarbonyl, heterocyclylcarbonyl, lower alkyl-carbonyloxy-lower alkylcarbonyl, aryloxy-lower alkylcarbonyl, lower alkynylcarbonyl, lower cyclo alkylcarbonyl, di(lower alkyl)amino-lower alkylcarbonyl, aryl-lower alkoxycarbonylamino-lower alkylcarbonyl, lower alkoxy-lower alkylcarbonyl, lower alkylcarbonylamino-lower alkenylcarbonyl, heterocyclyl-lower alkylcarbonyl, lower alkylthio-lower alkylcarbonyl, lower alkoxycarbonyl-lower alkylcarbonyl, aryl-lower alkenylcarbonyl, lower cycloalkenylcarbonyl, di(lower alkyl)aminocarbonyl-lower alkylcarbonyl, halo-lower alkylcarbonyl, lower alkenylcarbonyl, lower alkylcarbonylamino-lower alkylcarbonyl, lower cycloalkyl-lower alkylcarbonyl, lower alkylsulphonyl, arylsulphonyl arylaminocarbonyloxy-lower alkylcarbonyl, lower alkylsulphonyl-lower alkylcarbonyl, lower alkylcarbonyl-lower alkylcarbonyl, hydroxy-halo-lower alkylcarbonyl, di(lower alkoxy)phosphinyl-lower alkylcarbonyl, mono or di (lower alkylamino) lower alkyl carbonyl, mono or di (lower alkyl) amino substituted arylcarbonyl, lower alkoxy lower cycloalkylcarbonyl, lower alkyl substituted arylcarbonyl lower alkylcarbonyl, cyclo lower alkylcarbonyl, aryl substituted cyclo lower alkyl carbonyl, or nitro substituted aryl-lower alkylcarbonyl;
• and
• R11 and R12 each individually represent hydrogen, lower alkyl, aryl, heteroaryl, aryl-lower alkyl, diaryl-lower alkyl, lower cycloalkyl-lower alkyl, lower alkylaminocarbonyl-lower alkyl, lower alkylthio-lower alkyl, lower alkoxy, hydroxy, lower alkoxy substituted aryl lower alkyl, nitro substituted aryl lower alkyl, hydroxy substituted aryl lower alkyl or hydroxylower alkyl substituted aryl lower alkyl or heteroaryl-lower alkyl;
• and salts thereof.