| 摘要 |
The compound is new. The compound of formula (I), their pharmaceutical useful derivatives, solvate, salts, tautomers and stereoisomers, are new. For formula (I), R 1> : Ar, benzo-2,1,3-thiadiazolyl or Het, where Ar is selected from phenyl, naphthyl or biphenyl, which are unsubstituted or once, twice or thrice substituted by hal, A, N(R 3>) 2, [C(R 3>) 2] nOR 3>, [C(R 3>) 2] nN(R 3>) 2, SR 3>, NO 2>, CN, COOR 3>, CON(R 3>) 2, NR 3>COA, NR 3>SO 2A, SO 2N(R 3>) 2, S(O) mA, CO-Het, Het, O[C(R 3>) 2] nN(R 3>) 2, O[C(R 3>) 2] nHet, NHCOOA, NHCON(R 3>) 2, NHCOO[C(R 3>) 2] nN(R 3>) 2, NHCOO[C(R 3>) 2] nHet, NHCONH[C(R 3>) 2] nN(R3)2, NHCONH[C(R 3>) 2] nHet, OCONH[C(R 3>) 2] nN(R3)2, OCONH[C(R 3>) 2] nHet, CONR 3>[C(R 3>) 2] nN(R 3>) 2, CONR 3>[C(R 3>) 2] nHet or COA, and Het is once, twice or thrice saturated or unsaturated or aromatic heterocycles with 1-4 N-, O- or S-atoms or piperidinyl, piperazinyl, pyrrolidinyl, morpholinyl, furyl, thienyl, pyrrolyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyridyl, pyrimidinyl, triazolyl, tetrazolyl, oxadiazolyl, thiadiazolyl, pyridazinyl, pyrazinyl, benzimidazolyl, benzotriazolyl, indolyl, benzo[1,3]dioxolyl, indazolyl, azabicyclo[3.2.1]octyl, azabicyclo[2.2.2]octyl, imidazolidinyl, azepanyl or benzo [2,1,3]thiadiazolyl, which are unsubstituted or once, twice or thrice substituted by halide, A, [C(R 3>) 2] nOR 3>, [C(R 3>) 2] nN(R 3>) 2, SR 3>, NO 2>, CN, COOR 3>, CON(R 3>) 2, NR 3>COA, NR 3>SO 2A, SO 2N(R 3>) 2, S(O) mA, CO-Het 1>, [C(R 3>) 2] nHet 1>, O[C(R 3>) 2] nN(R 3>) 2, O[C(R 3>) 2] nHet 1>, NHCOOA, NHCON(R 3>) 2, NHCOO[C(R 3>)2] nN(R 3>) 2, NHCOO[C(R 3>) 2] nHet 1>, NHCONH[C(R 3>) 2] nN(R 3>) 2, NHCONH[C(R 3>) 2] nHet 1>, OCONH[C(R 3>) 2] nN(R 3>) 2, OCONH[C(R 3>) 2] nHet 1>, [C(R 3>) 2] nOR 3>, [C(R 3>) 2] nNR 3>, CHO, COA, =S, =NH, =NA or =O (carboxylic oxygen) and where a nitrogen ring is oxidized, Het 1>is a saturated heterocycle with 1-2 N or O-atoms or pyrrolidinyl, piperidinyl, piperazinyl or morpholinyl, which are once or twice replaced by A, OA, OH, halide or =O (carboxylic oxygen), A is 3-7C-cycloalkyl or unbranched or branched 1-10C-alkyl, where 1-7H-atoms are replaced by F or Cl where one or two non-adjacent CH 2groups are replaced by O, NH, S, SO, SO 2or CH=CH-groups, halide is F, Cl, Br or I, m is 0-2, n is 0-4 and p is 1-4; R 2> : unsaturated, saturated or aromatic 6-membered heterocycle with 1-4 N, O or S atoms or pyrimidinyl, pyridazinyl, pyridinyl, [1,3]oxazinanyl, morpholinyl, piperidinyl or piperazinyl, which are unsubstituted or once, twice or trice substituted by halide, A, [C(R 3>) 2] nOR 3>, N=CR 3>N(R 3>) 2, SR 3>, NO 2, CN, COOR 3>, CON(R 3>) 2, NR 3>COA, NR 3>SO 2A, SO 2N(R 3>) 2, S(O) mA, [C(R 3>) 2] nN(R 3>) 2, [C(R 3>)2] nHet, O[C(R 3>) 2] pOR 3>, O[C(R 3>) 2] nN(R 3>) 2, O[C(R 3>) 2] nC=C[C(R 3>) 2] nN(R 3>) 2, O[C(R 3>) 2] nN +>O ->(R 3>) 2, O[C(R 3>) 2] nHet, S[C(R 3>) 2] nN(R 3>) 2, S[C (R 3>) 2] nHet, NR 3>[C(R 3>) 2] nN(R 3>) 2, NR 3>[C(R 3>) 2] nHet, NHCON(R 3>) 2, NHCONH[C(R 3>) 2] nN(R 3>) 2, NHCONH[C(R 3>) 2] nHet, [C(R 3>) 2] nNHCO[C(R 3>) 2] nN(R 3>) 2, [C(R 3>) 2] nNHCO[C(R 3>) 2] nHet, CON(R 3>) 2, CONR 3>[C(R 3>) 2] nN(R 3>) 2, CONR 3>[C(R 3>) 2] nNR 3>COOA, CONR 3>[C(R 3>) 2] nOR 3>, CONR 3>[C(R 3>) 2] nHet, COHet, COA, CH=CH-COOR 3>, CH=CH-N(R 3>) 2or =O (carboxylic oxygen), where halide is F, Cl, Br or I and A, Het, m, n and p are same as variables of A, Het, m, n and p of R 1>; R 3> : H, methyl, ethyl, propyl or A, where A is same as variables of A of R 1>; and R 4>,R 4> '> : H, halide, A, OR 3>, COOR 3>, CON(R 3>) 2, NR 3>COA, NR 3>SO 2A, SO 2N(R 3>) 2or S(O) mA, where halide is F, Cl, Br or I, and A and m are same as variables of A and m of R 1>. Independent claims are included for: (1) a method for producing the compound of formula (I), their pharmaceutical useful derivatives, solvate, salts, tautomers and stereoisomers; and (2) a kit, which has the compound of formula (I) or their pharmaceutically useful derivatives, solvate, salts, stereoisomers and their mixtures with a drug active ingredient. [Image] ACTIVITY : Cytostatic. MECHANISM OF ACTION : Kinase inhibitor; Kinase regulator; Kinase modulator; Tyrosine kinase inhibitor; Met kinase inhibitor. |
