Patent ID: 6521614
Filing Date: 2003-02-18
Classification: A61P,C07D

Abstract:
A compound of formula I: or stereoisomer or pharmaceutically acceptable salt form thereof, wherein;one of D and Dâ€² is selected from CN, C(&boxH;NR11)NR12R13, NHC(&boxH;NR11)NR12R13, NR12CH(&boxH;NR11) C(O)NR12R13, and CH2NR12R13 and the other is H; R1 is selected from H, (CH2)rOR3, halo, C1-4 alkyl, (CH2)rNR4R4â€², (CH2)rCO2H, (CH2)rC(&boxH;O)R4, (CH2)rNR4C(&boxH;O)R4, (CH2)rSO2R5, and (CH2)rNR4SO2R5; R2 is selected from H, &boxH;O, C1-4 alkyl substituted with 0, 1, or 2 R7, C2-6 alkenyl substituted with 0, 1, or 2 R7, (CH2)rOR3, (CH2)rC(O)R4, (CH2)rOC(O)R4, (CH2)rNR3R3â€², (CH2)rNR3C(O)R4, (CH2)rSO2R5, (CH2)rNR3SO2R5, C3-10 carbocyclic residue substituted with 0-2 R6; and, 5-10 membered heterocyclic system containing from 1-3 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R6; R2a is absent; R3 and R3â€² are independently selected from H, C1-4 alkyl, benzyl and phenyl; R3 and R3â€² may be taken together to form a 5 or 6 membered ring substituted with 0-2 R6; R4 and R4â€² are independently selected from H, OR3, C1-4 alkyl, phenyl and NR3R3â€²; R5 is selected from C1-4 alkyl, phenyl and NR3R3â€²; Z is selected from a bond, C1-4 alkylene, (CH2)rO(CH2)r, (CH2)2NR3(CH2)r, (CH2)rC(O)(CH2)r, (CH2)rC(O)O(CH2)r, (CH2)2OC(O)(CH2)r, (CH2)rC(O)NR3(CH2)r, (CH2)2NR3C(O)(CH2)r, (CH2)2OC(O)O(CH2)r, (CH2)2OC(O)NR3(CH2)r, (CH2)2NR3C(O)O(CH2)r, (CH2)2NR3C(O)NR3(CH2)r, (CH2)rS(O)p(CH2)r, (CH2)rSO2NR3(CH2)r, (CH2)2NR3SO2(CH2)r, and (CH2)2NR3SO2NR3(CH2)r; A is selected from: C3-10 carbocyclic residue substituted with 0-2 R6, and 5-10 membered heterocyclic system containing from 1-3 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R6; B is selected from: Xâ€”Y, NR3R3â€², C(O)NR3R3â€², SO2NR3R3â€², benzyl substituted with 0-2 R6, C3-10 carbocyclic residue substituted with 0-2 R6, and 5-10 membered heterocyclic system containing from 1-3 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R6; X is selected from C1-4 alkylene, â€”C(O)â€”, â€”C(O)CR3R3â€²â€”, â€”CR3R3â€²C(O)â€”, â€”C(O)Oâ€”, â€”C(O)OCR3R3â€², â€”CR3R3â€²C(O)Oâ€”, â€”OC(O)â€”, â€”OC(O)CR3R3â€²â€”, â€”CR3R3â€²OC(O)â€”, â€”S(O)pâ€”, â€”S(O)pCR3R3â€²â€”, â€”CR3R3â€²S(O)pâ€”, â€”S(O)2NR3â€”, â€”NR3S(O)2â€”, â€”NR3S(O)2CR3R3â€²â€”, â€”CR3R3â€²S(O)2NR3â€”, â€”NR3S(O)2NR3â€”, â€”C(O)NR3â€”, â€”NR3C(O)â€”, â€”C(O)NR3CR3R3â€²â€”, â€”NR3C(O)CR3R3â€²â€”, â€”CR3R3â€²C(O)NR3â€”, â€”CR3R3â€²NR3C(O)â€”, â€”NR3C(O)Oâ€”, â€”OC(O)NR3â€”, â€”NR3C(O)NR3â€”, â€”NR3â€”, â€”NR3CR3R3â€²â€”, â€”CR3R3â€²NR3â€”, O, â€”CR3R3â€²Oâ€”, â€”OCR3R3â€”, S, â€”CR3R3â€²Sâ€”, and â€”SCR3R3â€”; Y is selected from: C1-4 alkyl substituted with 0-2 R6 C3-10 carbocyclic residue substituted with 0-2 R6, and 5-10 membered heterocyclic system containing from 1-3 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R6; R6 is selected from H, OH, CF3, (CH2)nOR3, halo, C1-4 alkyl, CN, NO2, (CH2)rNR3R3â€², (CH2)rC(O)R3, NR3C(O)R3â€², NR3C(O)NR3R3â€², SO2NR3R3â€², NR3SO2NR3R3â€², NR3SO2â€”C1-4 alkyl, SO2-phenyl, and NR3SO2R8; R7 is selected from: C3-10 carbocyclic residue substituted with 0-2 R6; and, 5-10 membered heterocyclic system containing from 1-3 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R6; R8 is selected from: C3-10 carbocyclic residue substituted with 0-2 R9; and, 5-10 membered heterocyclic system containing from 1-3 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R9; R9 is selected from H, OH, (CH2)nOR3, halo, C1-4 alkyl, CN, NO2, (CH2)rNR3R3â€², (CH2)rC(O)R3, NR3C(O)R3â€², NR3C(O)NR3R3â€², SO2NR3R3â€², NR3SO2NR3R3â€², and NR3SO2â€”C1-4 alkyl; R10 is selected from H, OR3, halo, C1-4 alkyl, CN, NO2, NR3R3â€², NR3C(O)R3â€², NR3C(O)OR3â€², NR3SO2-phenyl, and NR3SO2â€”C1-4 alkyl; R10a if a substituent on nitrogen is selected from H and C1-4 alkyl; R10a if a substituent on carbon is selected from H, C1-4 alkyl, NR3R3â€², NR3C(O)R3â€², NR3C(O)OR3â€², NR3SO2-phenyl, and NR3SO2â€”C1-4 alkyl; R11 is selected from H, OH, C1-6 alkyl, C1-6 alkylcarbonyl, C1-6 alkoxy, C1-4 alkoxycarbonyl, 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; R12 is selected from H, C1-6 alkyl and (CH2)n-phenyl; R13 is selected from H, C1-6 alkyl and (CH2)n-phenyl; n is 2; m is selected from 0 and 1; p is selected from 0, 1, and 2; q is selected from 1, 2, 3, 4, and 5; and, r is selected from 0, 1, and 2.