Patent ID: 6825208
Filing Date: 2004-11-30
Classification: A61P,C07D

Abstract:
A compound of Formula (I): or a stereoisomer or pharmaceutically acceptable salt form thereof, wherein;X is â€”NHâ€”; ring A, including the two atoms of Ring B to which it is attached, is a phenyl ring; wherein, in addition to RA, ring A is substituted with 0-3 RAA; RA is selected from: F, Cl, Br, OH, OCH3, OCH2CH3, OCH(CH3)2, â€”OCH2CH2CH3, â€”OCF3, â€”CN, â€”NH2, â€”NH2NH3, C(&boxH;NR1)NR2R3, â€”NHC(&boxH;NR1)NR2R3, â€”NR2CH(&boxH;NR1), â€”C(O)NR2R3, â€”S(O)2NR2aR3, â€”NR2R3, â€”CH2NR2R3, â€”CH2CH2NR2R3, â€”CH(CH3)NR2R3, â€”CH2CH2CH2NR2R3, â€”CH2CH(CH3)NR2R3, â€”CH(CH2CH3)NR2R3, â€”CH(CH3)CH2NR2R3, â€”C(CH3)2NR2R3, â€”(C1-3 alkyl)CO2H, â€”Oâ€”(C1-3 alkyl)CO2H, â€”Sâ€”(C1-3 alkyl)CO2H, â€”(C1-3 alkyl)CH(NH2)CO2H, â€”C(O)NHCH2CH2NH(C1-3 alkyl), â€”C(O)NHCH2CH2N(C1-3 alkyl)2, â€”CH2NCOO(C1-4 alkyl), R1 is selected from: H, OH, â€”NH2, C1-6 alkyl, C1-6 alkoxy, phenylCH2â€”, and phenylCH2CH2â€”; R1a, at each occurrence, is selected from: H and C1-4 alkyl; R1b is selected from: H, Cl, C1-4 alkyl, NH2, and NHNH2; R1c is selected from: H and C1-4 alkyl; R2, at each occurrence, is selected from: H, OH, C1-6 alkyl, C1-6 alkylcarbonyl, C1-4 alkoxycarbonyl, phenyl, phenyl(C1-3 alkyl)â€”, C6-10 aryloxy, C6-10 aryloxycarbonyl, C6-10 arylmethylcarbonyl, (C1-4 alkylcarbonyloxy)C1-4 alkoxycarbonyl, (C6-10 arylcarbonyloxy)C1-4 alkoxycarbonyl, C1-6 alkylaminocarbonyl, phenylaminocarbonyl, and (phenyl)C1-4 alkoxycarbonyl; R2a, at each occurrence, is selected from: H, C1-6 alkyl, â€”C(&boxH;NH)NH2, pyridinyl, pyrimidinyl, (CH3O)pyrimidinyl, (CH3O)2pyrimidinyl, oxazolyl, (CH3)oxazolyl, and (CH3)2oxazolyl; R3, at each occurrence, is selected from: H, C1-6 alkyl, phenylCH2â€”, and phenylCH2CH2â€”; RAA is, at each occurrence, selected from: H, halo, C1-4 alkyl, C3-6 cycloalkylâ€”, â€”OH, C1-4 alkoxy, (C1-4 alkyl)Sâ€”, (C1-4 alkyl)S(O)â€”, (C1-4 alkyl)SO2â€”, â€”NH2, (C1-4 alkyl)2Nâ€”, (C1-4 alkyl)NHâ€”, â€”CN, â€”NO2, (C1-4 alkyl)C(&boxH;O)â€”, HO2Câ€”, (C1-4 alkyl)OC(&boxH;O)â€”, H2NC(&boxH;O)â€”, (C1-4 alkyl)NHC(&boxH;O)â€”, (C1-4 alkyl)C(&boxH;O)NHâ€”, C1-4 haloalkyl, and C1-4 haloalkyloxy; RB is a 5-10 membered ring system consisting of carbon atoms and 0, 1 or 2 heteroatoms selected from the group consisting of N, O, and S; wherein said ring system may be unsaturated, partially unsaturated or saturated; and RB is substituted with 0, 1, 2, 3, 4, or 5 substituents selected from Rb1, Rb2, Rb3, Rb4, and Rb5; alternatively RB is C1-4 alkyl substituted with 5-10 membered ring system consisting of carbon atoms and 0, 1 or 2 heteroatoms selected from the group consisting of N, O, and S; wherein said ring system may be unsaturated, partially unsaturated or saturated; and RB is substituted with 0, 1, 2, 3, 4, or 5 substituents selected from Rb1, Rb2, Rb3, Rb4, and Rb5; Rb1, Rb2, Rb3, Rb4, and Rb5, at each occurrence, are independently selected from: H, F, Cl, Br, I, &boxH;O, â€”CN, â€”NO2, OR12, SR12, NR12R13, C(O)H, C(O)R12, C(O)OR12, C(O)NR12R13, OC(O)NR12R13, NR14C(O)R12, OC(O)R12, CH(&boxH;NR14)NR12R13, NHC(&boxH;NR14)NR12R13, S(O)R12, S(O)2R12, S(O)H, S(O)2H, S(O)NR12R13, S(O)2NR12R13, NR14S(O)R12, NR14S(O)2R12, NR12C(O)R15, NR12C(O)OR15, NR12S(O)2R15, NR12C(O)NHR15, (HO)2Bâ€”, C1-4 haloalkyl, C1-4 alkoxy, C2-4 alkenyloxy, C2-4 alkynyloxy, (C1-4 haloalkyl)oxy, C1-4 alkyl substituted with 0-3 R11, C2-4 alkenyl substituted with 0-3 R11, C2-4 alkynyl substituted with 0-3 R11, C1-4 alkoxy substituted with 0-3 R11, C3-10 carbocyclic residue substituted with 0-3 R31, aryl substituted with 0-5 R31, and 5-10 membered heterocyclic ring system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-3 R31; alternatively, Rb1 and Rb2, when substituents on adjacent carbons, or Rb2 and Rb3, when substituents on adjacent carbons, may be combined to form a methylenedioxy group; n is 1, 2, or 3; RC1, at each occurrence, is independently selected from: H, halo, â€”CN, â€”NO2, OR12, SR12, NR12R13, C(O)H, C(O)R12, C(O)NR12R13, OC(O)NR12R13, NR14C(O)R12, NR14C(S)R12, C(O)OR12, OC(O)R12, OC(O)OR12, CH(&boxH;NR14)NR12R13, NHC(&boxH;NR14)NR12R13, S(O)R12, S(O)2R12, S(O)NR12R13, S(O)2NR12R13, NR14S(O)R12, NR14S(O)2R12, NR12C(O)R15, NR12C(S)R15, NR12C(O)OR15, NR12S(O)2R15, NR12C(O)NHR15, C1-4 haloalkyl, (C1-4 haloalkyl)oxy, C1-10 alkyl substituted with 0-3 RCC, C2-10 alkenyl substituted with 0-3 RCC, C2-10 alkynyl substituted with 0-3 RCC, C1-10 alkoxy substituted with 0-3 RCC, C3-6 carbocyclic residue substituted with 0-3 RCC, aryl substituted with 0-5 RCC, and 5-6 membered heterocyclic ring system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-3 RCC; RC2 is selected from: H, C1-4 alkyl, OH, CN, and C1-4 alkoxy; RCC, at each occurrence, is independently selected from: H, halo, â€”CN, â€”NO2, OR12, SR12, NR12R13, C(O)H, C(O)R12, C(O)NR12R13, OC(O)NR12R13, NR14C(O)R12, NR14C(S)R12, C(S)NR12R13, C(O)OR12, OC(O)R12, OC(O)OR12, CH(&boxH;NR14)NR12R13, NHC(&boxH;NR14)NR12R13, S(O)R12, S(O)2R12, S(O)NR12R13, S(O)2NR12R13, NR14S(O)R12, NR14S(O)2R12, NR12C(O)R15, NR12C(S)R15, NR12C(O)OR15, NR12S(O)2R15, NR12C(O)NHR15, C1-4 haloalkyl, (C1-4 haloalkyl)oxy, C1-4 alkyl substituted with 0-3 R11, C2-4 alkenyl substituted with 0-3 R11, C2-4 alkynyl substituted with 0-3 R11, C1-4 alkoxy substituted with 0-3 R11, C3-6 carbocyclic residue substituted with 0-3 R31, aryl substituted with 0-5 R31, and 5-6 membered heterocyclic ring system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-3 R31; ring D, including the two atoms of Ring C to which it is attached, is a phenyl ring; and ring D is substituted with 0-4 RD; RD, at each occurrence, is independently selected from: H, halo, â€”CN, â€”NO2, OR16, SR16, NR16R16, C(O)H, C(O)R16, C(O)NR16R16, OC(O)NR16R16, NR14C(O)R16, C(O)OR16, OC(O)R16, OC(O)OR16, CH(&boxH;NR14)NR16R16, NHC(&boxH;NR14)NR16R16, S(O)R16, S(O)2R16, S(O)NR16R16, S(O)2NR16R16, NR14S(O)R16, NR14S(O)2R16, NR16C(O)R17, NR16C(O)OR17, NR16S(O)2R17, NR16C(O)NHR17, C1-4 haloalkyl, C1-4 alkoxy, (C1-4 haloalkyl)oxy, C1-4 alkyl substituted with 0-3 R31, C2-4 alkenyl substituted with 0-3 R31, and C2-4 alkynyl substituted with 0-3 R31; R11, at each occurrence, is independently selected from: H, halo, â€”CN, â€”NO2, OR12, SR12, NR12R13, C(O)H, C(O)R12, C(O)NR12R13, OC(O)NR12R13, NR14C(O)R12, C(O)OR12, OC(O)R12, OC(O)OR12, CH(&boxH;NR14)NR12R13, NHC(&boxH;NR14)NR12R13, S(O)R12, S(O)2R12, S(O)NR12R13, S(O)2NR12R13, NR14S(O)R12, NR14S(O)2R12, NR12C(O)R15, NR12C(O)OR15, NR12S(O)2R15, NR12C(O)NHR15, C1-4 haloalkyl, C1-4 alkoxy, C2-4 alkenyloxy, C2-4 alkynyloxy, (C1-4 haloalkyl)oxy, C1-4 alkyl substituted with 0-3 R12a, C2-4 alkenyl substituted with 0-3 R12a, C3-6 carbocyclic residue substituted with 0-3 R31, aryl substituted with 0-5 R31, and 5-6 membered heterocyclic ring system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-3 R31; R12, at each occurrence, is independently selected from: H, C1-4 alkyl substituted with 0-1 R12a, C2-4 alkenyl substituted with 0-1 R12a, C2-4 alkynyl substituted with 0-1 R12a, C3-6 cycloalkyl substituted with 0-3 R31, aryl substituted with 0-5 R31; C3-10 carbocyclic residue substituted with 0-3 R31, and 5-10 membered heterocyclic ring system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-3 R31; R12a, at each occurrence, is independently selected from: phenyl substituted with 0-5 R31, C3-6 carbocyclic residue substituted with 0-3 R31, and 5-6 membered heterocyclic ring system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-3 R31; R13, at each occurrence, is independently selected from: H, C1-4 alkyl, C2-4 alkenyl, and C2-4 alkynyl; alternatively, R12 and R13 may be combined, along with the nitrogen to which they are attached, to form a 5- or 6-membered ring optionally substituted with â€”Oâ€” or â€”N(R14)â€”; R14, at each occurrence, is independently selected from: H and C1-4 alkyl; R15, at each occurrence, is independently selected from: H, C1-4 alkyl, C2-4 alkenyl, and C2-4 alkynyl; R16, at each occurrence, is independently selected from: H, C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, and phenyl; R17, at each occurrence, is independently selected from: H, C1-4 alkyl, C2-4 alkenyl, and C2-4 alkynyl; R31, at each occurrence, is independently selected from: H, F, Cl, Br, I, &boxH;O, â€”CN, â€”NO2, OR32, SR32, NR32R33, C(O)H, C(O)R32, C(O)OH, C(O)OR32, C(O)NR32R33, OC(O)NR32R33, NR34C(O)R32, OC(O)R32, CH(&boxH;NR34)NR32R33, NHC(&boxH;NR34)NR32R33, S(O)R32, S(O)2R32, S(O)H, S(O)2H, S(O)3H, S(O)NR32R33, S(O)2NR32R33, NR34S(O)R32, NR34S(O)2R32, NR32C(O)R35, NR32C(O)OR35, NR32S(O)2R35, NR32C(O)NHR35, tetrazole, C1-4 haloalkyl, C1-4 alkoxy, C2-4 alkenyloxy, C2-4 alkynyloxy, (C1-4 haloalkyl)oxy, C1-4 alkyl, C2-4 alkenyl, and C2-4 alkynyl; and R32, R33, R34, R35, at each occurrence, are independently selected from: H, C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, and benzyl; provided RB is phenyl, or chloro-substituted phenyl, then RA is not chloro, bromo or methoxy.