Patent ID: 6340681
Filing Date: 2002-01-22
Classification: A61P,C07D

Abstract:
A compound of the following formula: or a salt thereof, whereinR1 and R2 are independently selected from hydrogen; halo; hydroxy; (C1-C4)alkyl; (C2-C4)alkenyl; (C2-C4)alkynyl; halo (C1-C4)alkyl; (C1-C4)alkoxy; (C1-C4)alkylsulfonyl; (C1-C4)alkyl-C(&boxH;O)â€”; carboxy; (C1-C4)alkyl-C(&boxH;O)Oâ€”; amino; NH2â€”C(&boxH;O)â€”; (C1-C4)alkyl-C(&boxH;O)â€”NHâ€”; (C1-C4)alkyl-SO2â€”NHâ€”; phenyl and naphthyl; R3 and R4 are independently selected from halo(C1-C10)alkyl; (C1-C6)alkyl substituted with one to two substituents independently selected from hydroxy, (C1-C4)alkoxy, (C1-C4)alkyl-Sâ€”, phenoxy, amino, oxo, mono[(C1-C4)alkyl]amino, di[(C1-C4)alkyl]amino, N-[(C7-C9)cycloalkyl-(C1-C4)alkyl]-N-(C1-C4)alkyl-amino, (C1-C4)alkoxy-C(&boxH;O)â€”, aryl selected from phenyl and naphthyl wherein the aryl is optionally substituted with one to three substituents independently selected from halo, hydroxy, (C1-C4)alkoxy, and trifluoro(C1-C4)alkoxy, and heterocyclyl selected from pyrrolidyl and piperidinyl wherein the heterocyclyl is optionally substituted with (C1-C4)alkyl; (C3-C8)cycloalkyl optionally substituted with (C1-C4)alkyl; (C3-C8)cycloalkenyl optionally substituted with (C1-C4)alkoxy-C(&boxH;O)â€”; 5- to 6-membered heterocyclyl, 5- to 6-membered heterocyclyl-(C&boxH;O)â€” and 5-to 6-membered heterocyclyl-(C1-C4)alkyl wherein each heterocyclyl contains in the ring one to three heteroatoms independently selected from oxygen, nitrogen and sulfur, is optionally fused to a phenyl ring, and is optionally substituted with one to two substituents independently selected from halo, (C1-C4)alkyl, benzyl and oxo; phenyl optionally substituted with one to three substituents independently selected from halo, (C1-C4)alkyl, halo(C1-C4)alkyl and (C1-C4)alkoxy; and 5- to 6-membered heteroaryl-(C1-C4)alkyl wherein said heteroaryl contains one to four ring atoms independently selected from oxygen, nitrogen and sulfur and is optionally fused to a phenyl ring; or R3 and R4, together with the nitrogen atom to which they are attached, form a fully saturated, partially saturated or fully unsaturated 5- to 8-membered nitrogen containing heterocyclic ring wherein said heterocyclic ring optionally contains in the ring one or two additional heteroatoms independently selected from nitrogen, oxygen and sulfur, optionally contains in the ring a group CR6R7 wherein R6 and R7 taken together form an oxo group or a cyclic acetal, and is optionally fused to a phenyl, naphthalene or (C5-C8)cycloalkyl ring, and optionally substituted with one to two substituents independently selected from halo; (C1-C4)alkyl; halo(C1-C4)alkyl; (C1-C4)alkoxy; hydroxy; carbonyl; benzhydryl; hydroxy-(C1-C4)alkyl; (C1-C4)alkoxy-(C1-C4)alkyl-; amino; amino-(C1-C4)alkyl-amino; mercapto; (C1-C4)alkoxy-C(&boxH;O)â€”; pyrrolidino-(C1-C4)alkyl, amino-C(&boxH;O)â€”; (C1-C4)alkyl-C(&boxH;O)â€”; (C1-C4)alkoxy-C(&boxH;O)â€”amino-; piperidinyl optionally substituted with one or two substituents independently selected from amino, mono[(C1-C4)alkyl]amino, di[(C1-C4)alkyl]amino-, benzylamino and di-(benzyl)amino; phenyl optionally substituted with one to three substituents selected from halo and (C1-C4)alkoxy; phenyl-(C1-C4)alkyl; phenyl-(C1-C4)alkenyl; phenyl-(C1-C4)alkoxy-C(&boxH;O)â€”; 1,3-benzodioxolyl-(C1-C4)alkyl-; trifluoromethyl; nitro; pyridyl optionally substituted with one to three substituents independently selected from halo and trifluoromethyl; quinolinyl optionally substituted with one to three substituents independently selected from halo and trifluoromethyl; pyrrolidinyl-(C1-C4)alkyl and pyrrolidinyl-(CH2)mâ€”CR8R9â€”(CH2)nâ€” wherein m and n are independently 1, 2, 3 or 4, and R8 and R9, taken together with the carbon atom to which they are attached, form (C3-C6)cycloalkyl; and R5 is phenyl or (C4-C11)cycloalkyl optionally substituted with one to three substituents independently selected from the group consisting of hydrogen, halo, hydroxy, (C1-C4)alkyl, halo (C1-C4)alkyl, (C1-C4)alkoxy, (C1-C4)alkylsulfonyl, (C1-C4)alkyl-C(&boxH;O)â€”, carboxy, (C1-C4)alkyl-C(&boxH;O)Oâ€”, amino, NH2-C(&boxH;O)â€”, (C1-C4)alkyl-C(&boxH;O)â€”NHâ€”, (C1-C4)alkyl-SO2â€”NHâ€”, phenyl and naphthyl.