Patent ID: 6399606
Filing Date: 2002-06-04
Classification: A61P,C07D

Abstract:
A compound having the structure: or a stereoisomer or pharmaceutically acceptable salt thereof,wherein:R1 is pyridyl; R2 is â€”NR2bR2c; R3 is hydrogen, keto, â€”C(&boxH;O)OR3aor â€”C(&boxH;O)NR3bR3c; R4 is hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, â€”C(&boxH;O)R4a, â€”C(&boxH;O)OR4b, â€”C(&boxH;O)NR4cR4d, â€”OC(&boxH;O)NR4cR4d or â€”SO2R4e, or wherein R3 and R4 taken together form a heterocyclic ring or substituted heterocyclic ring; and R5 is hydrogen, alkyl or cycloalkyl; provided that at least one of R3 and R5 is hydrogen; and wherein:R2b and R2c taken together with the nitrogen atom to which they are attached from a heterocyclic ring; R3a, R3b and R3c, are the same or different and independently hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substitued arylalkyl, heterocycle, substituted heterocyle, heterocyclealkyl, substituted heterocyclealkyl, or a radical of the formula â€”Y3â€”Z3â€”R3d, where Y3 is alkanediyl, substitute alkanediyl or a direct bond, Z3 is â€”Oâ€”, â€”Sâ€”, â€”SO2â€”, â€”N(R3e)â€”, â€”C(&boxH;O)â€”, â€”C(&boxH;O)Oâ€”, â€”OC(&boxH;O)â€”, â€”NHC(&boxH;O)â€”, â€”C(&boxH;O)N(R3e)â€” or a direct bond, and R3d and R3e are the same or different and independently hydrogen, amino, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, heterocycle, substituted heterocycle, heterocylealkyl or substituted heterocyclealkyl, or R3d and R3e taken together with the nitrogen atom to which they are attached form a heterocycle or substituted heterocycle; or R3b and R3c taken together with the nitrogen atom to which they are attached from a heterocyclic ring or substituted heterocyclic ring; R4a, R4b, R4c, R4d and R4e are the same or different and independently hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, or a radical of the formula â€”Y4â€”Z4â€”R4f, where Y4 is alkanediyl, substituted alkanediyl or a direct bond, Z4 is â€”Oâ€”, â€”Sâ€”, â€”SO2â€”, â€”N(R4g)â€”, â€”C(&boxH;O)â€”, â€”C(&boxH;O)Oâ€”, â€”OC(&boxH;O)â€”, â€”NHC(&boxH;O)â€”, â€”C(&boxH;O)N(R4g)â€” or a direct bond, and R4f and R4g are the same or different and independently hydrogen, amino, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, heterocycle, substituted heterocycle, heterocylealkyl or substituted heterocyclealkyl, or R4f and R4g taken together with the nitrogen atom to which they are attached form a heterocycle or substituted heterocycle; or R and R4d taken together with the nitrogen atom to which they are attached from a heterocyclic ring or substituted heterocyclic ring; and each of said substituted moieties being substituted with at least one alkyl, alkanediyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclic or heterocyclealkyl.