Patent ID: 6440968
Filing Date: 2002-08-27
Classification: A61K,A61P,C07D

Abstract:
Compounds and salts of Formula 4whereinR1 is hydrogen, or branched-chain, or straight-chain C1-12alkyl residue optionally substituted one or more times by â€”OH, â€”SH, â€”NH2, â€”NHC1-6alkyl, â€”N(C1-6alkyl)2, â€”NHC6 -14aryl, â€”N(C6-14aryl)2, â€”N(C1-6alkyl)(C6-14aryl), â€”NHCOR7, â€”NO2, â€”CN, â€”F, â€”Cl, â€”Br, â€”I, â€”Oâ€”C1-6alkyl, â€”Oâ€”C6-14aryl, â€”O(CO)R7, â€”Sâ€”C1-6-alkyl, â€”Sâ€”C6-14aryl, â€”SOR8, â€”SO2R8, â€”OSO2C1-6alkyl, â€”OSO2C6-14aryl, â€”(CS)R7, â€”O(CO)R7, â€”(CO)R9, a mono-, bi- or tricyclic saturated or mono- or polyunsaturated carbocycle with 3-14 ring members, mono-, bi- or tricyclic saturated or mono- or polyunsaturated heterocycle with 5-15 ring members and 1-6 heteroatoms, wherein the C6-14 aryl groups and the included carbocylic and heterocyclic substituents can be optionally substituted one or more times by R10, a mono- or polyunsaturated, straight-chain or branched-chain C2-12alkenyl residue optionally substituted one or more times by â€”OH, â€”SH, â€”NH2, â€”NHC1-6alkyl, â€”N(CH1-6 alkyl)2, â€”NHC6-14aryl, â€”N(C6-14aryl)2, â€”N(C1-6alkyl)(C6-14aryl), â€”NHCOR7, â€”NO2, â€”CN, â€”F, â€”Cl, â€”Br, â€”I, â€”Oâ€”C1-6alkyl, â€”Oâ€”C6-14-aryl, â€”O(CO)R7, â€”Sâ€”C1-6alkyl, â€”Sâ€”C6-14aryl, â€”SOR8, â€”SO2R8, â€”OSO2C1-6alkyl, â€”OSO2C6-14aryl, â€”(CS)R7, â€”O(CO)R7, â€”(CO)R9, mono-, bi- or tricyclic saturated or mono- or polyunsaturated carbocycle with 3-14 ring members, a mono-, bi- or tricyclic saturated or mono- or polyunsaturated heterocycle with 5-15 ring members and 1-6 heteroatoms, the C6-14 aryl groups and the included carbocyclic and heterocyclic substituents can be optionally substituted one or more times by R10, mono-, bi- or tricyclic saturated or mono- or polyunsaturated carbocycle with 3-14 ring members, optionally substituted one or more times by â€”OH, â€”SH, â€”NH2, â€”NH C1-6alkyl, â€”N(C1-6alkyl)2, â€”NHC6-14aryl, â€”N(C6-14aryl)2, â€”N(C1-6alkyl)(C6-14aryl), â€”NHCOR7, â€”NO2, â€”CN, â€”F, â€”Cl, â€”Br, â€”I, â€”Oâ€”C1-6-alkyl, â€”Oâ€”C6-14aryl, â€”O(CO)R7, â€”Sâ€”C1-6 alcyl, â€”Sâ€”C6-14aryl, â€”SOR8, â€”SO2R8, â€”OSO2C1-6alkyl, â€”OSO2C6-14aryl, â€”(CS)R7, â€”O(CO)R7, â€”(CO)R9, the C6-14 aryl groups can be optionally substituted one or more times by R10, a mono-, bi- or tricyclic saturated or mono- or polyunsaturated heterocycle with 5-15 ring members and 1-6 heteroatoms, optionally substituted one or more times by â€”OH, â€”SH, â€”NH2, â€”NHC1-6alkyl, â€”N(C1-6alkyl)2, â€”NHC6-14aryl, â€”N(C6-14aryl)2, â€”N(C1-6alkyl)(C6-14aryl), â€”NHCOR7, â€”NO2, â€”CN, â€”F, â€”Cl, â€”Br, â€”I, â€”Oâ€”C1-6alkyl, â€”Oâ€”C6-14aryl. â€”O(CO)R7, â€”Sâ€”C1-6alkyl, â€”Sâ€”C6-14aryl, â€”SOR8, â€”SO2R8, â€”OSO2C1-6alkyl, â€”OSOC2C6-14aryl, â€”(CS)R7, â€”O(CO)R7â€”(CO)R8, the C6-14aryl groups can be optionally substituted one or more times by R10, carbo- or a heterocyclic saturated or mono- or polyunsaturated spirocycles with 3-10 ring members, where heterocyclic systems contain 1-6 heteroatoms optionally substituted one or more times by â€”OH, â€”SH, â€”NH2, â€”NHC1-6alkyl, â€”N(C1-6alkyl)2, â€”NHC6-14aryl, â€”N(C6-14aryl)2, â€”N(C1-6alkyl)(C6-14aryl), â€”NHCOR7, â€”NO2, â€”CN, â€”F, â€”Cl, â€”Br, â€”I, â€”Oâ€”C1-6 alkyl, â€”Oâ€”C6-14aryl, â€”O(CO)R7, â€”Sâ€”C1-6alkyl, â€”Sâ€”C6-14aryl, â€”SOR8, â€”SO2R8, â€”OSO2C1-6 alkyl, â€”OSO2C6-14 aryl, â€”(CS)R7, â€”O(CO)R7, â€”(CO)R8, the C6-4aryl groups can be optionally substituted one or more times by R10; R2, R3, R4, R5, R6 can be the same or different and are hydrogen, and a straight-chaim or branched-chain C1-6alkyl residue, optionally substituted one or more times by â€”OH, â€”SH, â€”NH2, â€”NHC1-6alkyl, â€”N(C1-6alkyl)2, â€”NHC6-14aryl, â€”N(C6-14aryl)2, â€”N(C1-6 alkyl)(C6-14aryl), â€”NHCOR7, â€”NO2, â€”CN, â€”(CO)R8, â€”(CS)R7, â€”F, â€”Cl, â€”Br, â€”I, â€”Oâ€”C1-6 akyl, â€”Oâ€”C6-14aryl, â€”O(CO)R7, â€”Sâ€”C1-6alkyl, â€”Sâ€”C6-14aryl, â€”SOR8, â€”SO2R8, COâ€”C1-6 alkyl, optionally substituted one or more times by â€”OH, â€”SH, â€”NH2, â€”NHC1-6alkyl, â€”N(C1-6 alkyl)2, â€”NHC6-14aryl, â€”N(C6-14aryl)2, â€”N(C1-6alkyl)(C6-14aryl), â€”NHCOR7, â€”NO2, â€”CN, â€”(CO)R8, â€”(CS)R7, â€”F, â€”Cl, â€”Br, â€”I, â€”Oâ€”C1-6alkyl, â€”Oâ€”C6-14aryl, â€”O(CO)R7, â€”Sâ€”C1-6 alkyl, â€”Sâ€”C6-14aryl, â€”SOR8, â€”SO2R8 COOâ€”C1-6alkyl residue, optionally substituted one or more times by â€”OH, â€”SH, â€”NH2, â€”NHC1-6alkyl, â€”N(C1-6alkyl)2, â€”NHC6-14aryl, â€”N(C6-14aryl)2, â€”N(C1-6alkyl)(C6-14aryl), â€”NHCOR7, â€”NO2, â€”CN, â€”(CO)R8, â€”(CS)R7, â€”F, â€”Cl, â€”Br, â€”I, â€”Oâ€”C1-6alkyl, â€”Oâ€”C6-14aryl, â€”O(CO)R7, â€”Sâ€”C1-6alkyl, â€”Sâ€”C6-14aryl, â€”SOR8, â€”SO2R8; R7 is a C1-6alkyl, â€”Oâ€”C1-6alkyl, â€”Oâ€”C6-14aryl, â€”NH2, â€”NHC1-6alkyl, â€”N(C1-6alkyl)2â€”NHC6-14aryl, â€”N(C6-14aryl)2, â€”N(C1-6alkyl)(C6-14aryl), â€”Sâ€”C1-6alkyl, residue, or a mono-, bi- or tricyclic saturated or mono- or polyunsaturated carbocycle with 3-14 ring members, or mono-, bi- or tricyclic saturated or mono- or polyunsaturated heterocycle with 5-15 ring members and 1-6 heteroatoms, R8 is â€”H, a â€”C1-6alkyl, â€”NH2, â€”NHC1-6alkyl, â€”N(C1-6alkyl)2, â€”NHC6-14aryl, â€”N(C6-14aryl)2, â€”N(C1-6alkyl)(C6-14aryl, â€”NHCOR7, â€”OH, â€”Oâ€”C1-6alkyl, â€”Oâ€”C6-14aryl), â€”Sâ€”C1-6alkyl, â€”Sâ€”C6-14aryl residue, or a mono-, bi- or tricyclic saturated or mono- or polyunsaturated carbocycle with 3-14 ring members, or mono-, bi- or tricyclic saturated or mono- or polyunsaturated heterocycle with 5-15 ring members and 1-6 hetero atoms; R9 is â€”H, a â€”C1-6alkyl residue, or mono-, bi- or tricyclic saturated or mono- or polyunsaturated carbocycle with 3-14 ring members, or a mono-, bi- or tricyclic saturated or mono- or polyunsaturated heterocycle with 5-15 ring members and 1-6 heteroatoms, R10 is â€”OH, a â€”SH, â€”NH2, â€”NHC1-6alkyl, â€”N(C1-6akyl)2, â€”NHC6-14aryl, â€”N(C6-14aryl)2, â€”N(C1-6alkyl)(C6-14aryl), â€”NHCOR7, â€”NO2, â€”CN, â€”(CO)R8, â€”(CS)R7, â€”F, â€”Cl, â€”Br, â€”I, â€”Oâ€”C1-6alkyl, â€”Oâ€”C6-14aryl, â€”O(CO)R7, â€”Sâ€”C1-6alkyl, â€”Sâ€”C6-14aryl, â€”SOR8, or an â€”SO2R8 residue, and A, B can be a â€”CH2â€”, â€”CH(OH) residue or A+B can be a â€”CH&boxH;CHâ€” residue, or with a pharmaceutically acceptable salt thereof, provided that R2 through R5 are not hydrogen when R6 is CH3.