Patent ID: 6562811
Filing Date: 2003-05-13
Classification: A61P,C07D

Abstract:
A pyridine derivative of the formula (I) wherein â€”R1 represents in which R11 is hydrogen, C1-6 alkyl, halogen, hydroxy, C1-12 alkoxy, nitro, amino, C1-6 alkylsulfonylamino, C1-6 alkoxycarbonyl, C1-6 alkylamino, di(C1-6 alkyl)amino, C1-6 alkanoylamino, phenyl C1-6 alkylamino, phenylsulfonylamino, or â€”Oâ€”(CH2)nâ€”R111, wherein n represents an integer selected from 0 to 6, and R111 is C2-6 alkenyl, benzoyl, diphenylmethyl, di(C1-6 alkyl)amino, C1-6 alkanoyl, C1-6 alkoxycarbonyl, or a 3 to 10 membered saturated or unsaturated ring having 0 to 3 heteroatoms selected from the group consisting of S, O and N as heteroatoms and is optionally substituted by C1-6 alkyl, mono or di halogen, halogen substituted C1-6 alkyl, nitro, cyano, C1-6 alkoxycarbonyl, phenyl, hydroxy, amino, C1-6 alkylamino, di(C1-6 alkyl)amino, C1-6 alkanoylamino, C1-6 alkoxy, or carbamoyl; R2 represents hydrogen or halogen; R3 represents hydrogen or 1,2,3,6-Tetrahydro-pyridine, â€”CR31R32R33, â€ƒwherein R31 is hydrogen or C1-6 alkyl, R32 is hydrogen, &agr;-aminobenzyl, C1-6 alkyl optionally substituted by one or two substituents selected from the group consisting of hydroxy, amino, amino substituted phenyl, phenyl, halogen substituted phenyl, and C1-6 alkoxysubstituted phenyl, or a 5 to 8 membered saturated ring having 0 to 3 atoms selected from the group consisting of S, O and N as heteroatoms and optionally substituted by C1-6 alkyl, and R33 is hydrogen, amino, C1-6 alkoxycarbonylamino, C2-6 alkenyloxycarbonylamino, piperidino-C1-6 alkylcarbonylamino, piperidinyl-C1-6 alkylcarbonylamino, or R32 and R33 may form, together with the adjacent carbon atom, a 5 to 8 membered saturated ring having 0 to 3 heteroatoms selected from the group consisting of N, O and S as heteroatoms, which ring is optionally substituted by phenyl-C1-6 alkyl, C1-6 alkoxy substituted phenyl-C1-6 alkyl, C1-6 alkyl, amino, cyano, hydroxy, carbamoyl, carboxy, C1-6 alkylamino, C1-6 alkoxycarbonyl, di(C1-6 alkyl)amino, benzylamino, C1-6 alkylsulfonyl, piperidino C1-6 alkyl carbonyl, or optionally fused by benzene; or â€”NR34R35, â€ƒwherein R34 is hydrogen or C1-6 alkyl and R35 is hydrogen, a 5 to 8 membered saturated ring having 0 to 3 heteroatoms selected from the group consisting of N, O and S as heteroatoms, or â€”(CH2)mâ€”NR351R352 (m represents any of integers from 1 to 6) wherein R351 represents hydrogen, C1-6 alkyl, R352 represents hydrogen, C1-6 alkyl, C1-6 alkanoyl, C1-6 alkylsubstituted phenyl, benzoyl, C1-6 alkanoyl, phenylaminocarbonyl, phenylsulfonyl, or R34 and R35 may form, together with the adjacent N atom, a 5 to 8 membered saturated heterocyclic ring, and said ring may optionally contain NH, S or O atom other than the adjacent N atom and optionally substituted by carbamoyl, amino, or C1-6 alkyl; R4 and R5 form, â€”R40â€”COâ€”NHâ€”, â€”R40â€”SO2â€”NHâ€”, â€”R40â€”C(&boxH;S)â€”NHâ€”â€”R40â€”CH2â€”NHâ€”, â€ƒwherein said â€”R40â€” represents â€”CHR401â€”Oâ€”, â€”CH2â€”NR401â€”, â€”COâ€”NR401â€”, â€”CH2â€”CHR401â€”, â€”CH&boxH;CR401â€”, (in which R401 is C1-6 alkanoyl, C1-6 alkyl, phenyl, C1-6 alkylsulfonyl, C3-8 cycloalkylaminocarbonyl, hydrogen, halogen, nitro, amino, cyano, benzoylamino, phenylsulfonyl, carbamoyl, hydroxycarbonyl, C1-6 alkoxycarbonyl, C1-12 alkylaminocarbonyl, halogen substituted C1-6 alkylaminocarbonyl, C1-6 alkanoylamino, C1-6 alkylamino, di(C1-6 alkyl)aminocarbonyl, di(C1-6 alkyl)aminoC1-6 alkylaminocarbonyl, hydroindenylaminocarbonyl, diphenylmethylaminocarbonyl, pyrrolidinocarbonyl, C1-6 alkoxy C1-6 alkyl amino carbonyl, morpholinocarbonyl, piperazinocarbonyl, phenylC1-6alkylaminocarbonyl, hydroxycarbonylC1-6alkylaminocarbonyl, C3-8 cycloalkylaminocarbonyl, C3-8 cycloalkylC1-6alkylaminocarbonyl, hydroxyC1-6alkylaminocarbonyl, carboxyethylaminocarbonyl, C1-6alkylsulfonylaminocarbonyl) â€”CR41&boxH;Nâ€”NHâ€” (R41 is hydrogen, amino, or C1-6alkanoylamino), or â€”CR42&boxH;Nâ€”C&boxH;Nâ€” (R42 is hydrogen or amino); and salts thereof.