Pyridine Derivatives, a Medicine, a Pharmaceutical composition, a Kinase Inhibitor betaikappab, an anti-inflammatory Drug, an immunosuppressant medicine for ischemia, an anti-tumor Medicine and the use of these derivatives for the preparation of a medicament

摘要

Pyridine Derivatives, comprising a Derivative of formula (1), in which R1 represents a rest of formula (2), (3) or (4), in which R11 is Hydrogen, halogen, alkyl of C1 - 6, - 12 Hydroxy, alkoxy C1 alkyl, Nitro, amino, C1 sulfonylamino - 6, 6 - alkoxy alkyl carbonyl C1, C1 - 6 - amino alkyl di (C1 - 6 Amino) - 6 - amino alcanoil C1, C1, fenilalquil phenylsulfonylamino - 6 - amino - or, or - (CH2) n - R111,In which n is an integer between 0 and 6 selected, and alquenilo R111 is C2 Benzoyl, 6, difenilmetilo di (alkyl, amino, C1 - 6) alcanoilo C1 - 6alcoxi C1 - 6carbonilo, or a saturated or unsaturated Ring 3 - 10 members of 0 - 3 presents hetero Atoms selected from the Group constituted by S or n heteroatoms and as and is optionally substituted by alkyl or dihalogeno C1 - 6, Monkey,Alkyl substituted C1 - 6 with Halogen, Nitro, cyano, C1 - 6 - alkoxy carbonyl phenyl alkyl, Hydroxy, amino, C1 6 - amino -, di (alquilc1 6 - amino) - 6 - amino alcanoil C1, C1 -, alkoxy or carbamoilo 6; R2 represents Hydrogen or Halogen; R3 represents Hydrogen or cr31r32r33 3,6-tetrahydropyridine 1,2,3,4 -, in which r 31 is Hydrogen or alkyl of C1 - 6, R32 is Hydrogen, Alpha aminobencilo,C1 - 6 alkyl optionally substituted by one or two substituents selected from the group consisting of Hydroxy, amino, amino substituted phenyl, phenyl, phenyl and phenyl substituted Halogen substituted with alkoxy C1 - 6, or a saturated Ring 5 - 8 members of 0 - 3 heteroatoms s presents Selected from the group consisting of S,O and n as hetero Atoms and optionally substituted by alkyl C1 - 6 and R33 is Hydrogen, amino alkoxy carbonylamino alquenil C1 - C2 - 6, 6 - oxicarbonilamino, piperidinalquil C1 - 6 - carbonylamino piperidinialquil C1 -, 6 - or carbonylamino R32, R33, and can form,Along with the carbon Atom adjacent to a saturated Ring 5 - 8 members present 0-3 hetero Atoms selected from the group consisting of N, o and s as heteroatoms, whose ring is optionally substituted with fenilalquilo C1 - 6 - 6, fenilalquilo C1 C1 substituted with alkoxy alkyl - 6 C1 - 6, cyano, amino, Hydroxy, carboxy, carbamoilo, - 6 - amino alkyl C1, C1 - 6 - alkoxy carbonylDi (alkyl C1 - 6) Benzylamino amino alkyl sulfonyl C1 -, 6 -, piperidinalquil C1 - 6 - carbonyl or optionally FUSED benzene; or - nr34r35, in which R34 is Hydrogen or alkyl of C1 - 6 and R35 is saturated with Hydrogen, a Ring Member presents 5 - 8 0 3 heteroatoms selected Group Co Nstituido by N, o, and s as heteroatoms.O - (CH2) - nr351r352 m (m is any integer from 1 to 6), in which r351representa Hydrogen or alkyl of C1 - 6 and r352 represents Hydrogen, alkyl alcanoilo C1 C1 - 6, 6 -, phenyl alkyl substituted benzoyl alcanoilo C1, C1 - 6 - 6, fenilaminocarbonilo, fenilsulfonilo R34 or R35 and Can fo Sign, together with the N atom of an adjacent saturated Heterocyclic Ring of 5 - 8 members,And the above-mentioned Ring can optionally contain Atoms of NH, S U o n different Atom adjacent carbamoilo and optionally substituted by alkyl, amino, or C1 - 6; R4 represents hidroxicarbonilo, alcanoilo C1 - 6, carbamoilo, cyano, Nitro, carbonyl, carbonyl - 6 - alkoxy alkyl C1, C1 Carba - 6 - Moilo, C1 - 6 - amino alkyl, heteroaryl (Hydroxy methyl) 5 - 10 members,Heteroarilalquilo C1 - 6 methyl 5 - 10 members or replaced by a saturated cyclic ring and Hydroxy 5 - 7 6 - member C1 alkyl, optionally replaced by a Substituent selected from the group consisting of Hydroxy, alkoxy alkyl - C1 - 6, 6 - sulfonylamino C1, C1 - 6 - carbonylamino alkyl, aryl C5 - 10, 10 - aryl - aryl sulfonyl C5, C5 - 10 - sulfanilo C5 aryl Oxy -, 10 -,Imidazolilo or pirrolidinoxi replaced with cyclohexanecarboxylic, - (CH2) pnhcor41, - (CH2) PNCH R41 (= S), where p is any integer from 1 to 6 and R41 represents C1 6 - alkoxy alkyl, amino, phenylamino C1, C1 - 6, 6 - amino alkyl -, di (alkyl C1 amino) - 6 - 10 - amino cicloalquil C3, R3 and R4 can be together; With the carbon Atoms in the Pyridine ring.Monocicloalquilo or bicicloalquilo 4 - 10 members optionally interrupted by NH and optionally substituted by benzyl, OR = OR = NH; R5 represents nr51r52, in which Hydrogen or alkyl R51 is C1 - 6; R52 is Hydrogen, alkyl, phenyl benzyl C1 - 6,Alcanoilo or nr51r52 can form a saturated Ring of 5-6 members containing hetero Atom or optionally NH or other than the adjacent or n Atom; R4 and R5 can form, - R40 - CO NH - R40 - SO2 -, - NH -, - R40 - C (= o) - NH -, - R40 - ch2-nh -, which represents the R40 - chr401 - or - CH2 -, - nr401, co nr401, ch2chr401, - ch = cr401 (in which r401 is alcanoilo C1 C1 - 6 - 6, alkyl, phenyl,Alkyl sulfonyl cicloalquil C1 - C3 - 6 -, 8 - aminocarbonilo, Hydrogen, halogen, Nitro, amino, cyano, benzoylamino, fenilsulfonilo, carbamoilo, hidroxicarbonilo C1 carbonyl alkoxy -, 6 -, 12 - aminicarbonilo C1 alkyl, alkyl C1 - 6 - aminocarbonilo replaced with Halogen, alcanoil C1 6 - amino -, di (alkyl C1 - 6) Minocarbonilo, di (alkyl aminoalquil C1 C1 - 6) - 6 - aminocarbonilo, hidroindenilaminocarbonilo,Difenilmetilaminocarbonilo, pirrolidincarbonilo, C1 - 6 - alkoxy alkyl C1 - 6 - aminocarbonilo, morfolincarbonilo, piperazinacarbonilo, fenilalquil C1 - 6 - aminocarbonilo, hidroxicarbonilalquil C1 - C3 - cicloalquil aminocarbonilo 6 -, 8 - aminocarbonilo, cicloalquil C1 - C3 alkyl - 8 - 6 - aminocarbonilo, hidroxialquil C1 - 6 - aminocarbonilo, carboxietilaminocarbonilo C1 alkyl -, 6 -, sulfonilaminocarbonilo)- cr41 = NH - N - (amino or alcanoil R41 is Hydrogen, C1 - 6 - amino) - cr42 = N - C = N - (R42 is Hydrogen or amino); or a Salt thereof; a Medicine, a Pharmaceutical composition, a Kinase Inhibitor betaikappab, an Antifungal Drug anti-inflammatory, immunosuppressive, a Medicine for R Squemia,Anti - tumor Medicine and the use of these derivatives for the preparation of a Medicament.