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Pirazolopirimidina derivatives

机译:Pirazolopirimidina衍生物

摘要

1. Requirement 1: a compound (1) with common formula characteristics,a. 0, 1, 2, 3, or 4; R from hydrogen, halogen, cyanogen, nitrogen-oh, c83321; bicycle, nh832222,-NH (C -alquilo)-N (C -alquilo)-S-C₁₋₄-alkyl, -S (O) -C₁₋₄-alkyl, -SO₂-C₁₋₄-alkyl, -S-C₁₋₄-halogenoalkyl, -S (O) -C₁₋₄-halogenoalkyl and -SO₂-C₁₋₄-halogenoalkyl having 1 to 5 halogen atoms; n is 0 or 1; X, Y are independently selected from the group consisting of CR⁵R⁶,O. S, and n-r8311;where at least one of X and Y is CR⁵R⁶;R¹ is selected from the group consisting of hydrogen, -CHO, -OH, C₁₋₄-alkyl, C₁₋₄-haloalkyl having 1 to 5 halogen atoms, C₁₋₄-alkoxy, C₁₋₄-haloalkoxy which it has between 1 and 5 halogen atoms, C₃₋₆-cycloalkyl, C₃₋₆-halogenocycloalkyl having between 1 and 5 halogen atoms, C₃₋₄-alkenyl, C₃₋₄-alkynyl, C₁₋₄-alkoxy-C₁₋ ₄-alkyl, C₃₋₆-cycloalkyl-C₁₋₃-alkyl, cyano-C₁₋₄-alkyl, amino-C₁₋₄-alkyl, C₁₋₄-alkylamino-C₁₋₄-alkyl, di- (C₁₋₄ -alkyl) amino-C₁₋₄-alkyl, C₁₋₄-alkylcarbonyl,C₁₋₄-halogenalkylcarbonyl having 1 to 5 halogen atoms, C₁₋₄-alkoxycarbonyl, benzyloxycarbonyl, C₁₋₄-alkoxy-C₁₋₄-alkylcarbonyl, -SO₂-C₁₋₄-alkyl, and -SO₂-C₁₋ ₄-halogenalkyl having 1 to 5 halogen atoms; R² is selected from the group consisting of hydrogen, halogen, cyano, -CHO, C₁₋₄-alkyl, C₂₋₄-alkenyl, C₂₋₄-alkynyl, C₃₋₆-cycloalkyl, C₁₋₄-halogenoalkyl having between 1 and 5 halogen atoms, C₁₋₄-alkoxy-C₁₋₄-alkyl, benzyl having between 1 and 5 halogen atoms, C₁₋₄-alkoxy, -NH₂,-NH (C -alquilo)-N (C -alquilo)-NH (C -cicloalquilo)-N (C₁₋₄-alkyl) (C₃₋₆-cycloalkyl),-NH (heterosexual of 4-7 members)-N (C₁₋₄ alkyl) (4-7 membered heterocycloalkyl),-NH (C -alcoxi)-N (C -alquil) (C -alcoxi)-NH-SO - (C -alquilo)-N (SO₂- [C₁₋₄-alkyl]) (C₁₋₄-alkyl),(C -alquil) -NH-C -alquilo-(C -alquil) -N-C -alquilo--S-C₁₋₄-alkyl, -S (O) -C₁₋₄-alkyl, -SO₂-C₁₋₄-alkyl, (C₁₋₄-alkoxyimino) -C₁₋₄-alkyl, and a monocyclic heterocycle selected from the 4- to 7-membered heterocycloalkyl group, the 5-membered heteroaryl having at least one nitrogen atom through which the heteroaryl ring connects to the rest of the molecule, and the 6-membered heteroaryl having at least one atom of nitrogen, each of which in R² is optionally substituted with 1, 2 or 3 substituents independently selected from the group consisting of hydrogen, halogen, cyano, nitro, -OH, oxo, thiono, C₁₋₄-alkyl,c. C8321c83318324 - halogen-1 to 5 halogen atoms, c8321;-NH (C -alquilo)-N (C -alquilo)-SC -alquilo -S (O) -C -alquilo -SO -C -alquilo -SC -hal genoalquilo -S (O) -C -hal genoalquilo y -SC -hal genoalquilo que tiene entre 1 y 5 tomos de hal geno -NH (C -alquilo)-N (C -alquilo)ciano carboxi carbamoilo alcoxicarbonilo -C (O) -NH (C -alquilo)-C (O) -N (C₁₋₄-alkyl) ₂,-C (O) -NH (C -cicloalquilo)C₁₋₄-alkoxy, -S-C₁₋₄-alkyl, -S (O) -C₁₋₄-alkyl, -SO₂-C₁₋₄-alkyl, or optionally substituted with a monocyclic heterocycle selected from the group of heterocycloalkyl of 4-7 membered or 5-membered heteroaryl having at least one nitrogen atom through which the heteroaryl ring connects to C₁₋₄-alkyl or C₃₋₆-cycloalkyl, each of which is optionally substituted by 1 , 2 or 3 substituents independently selected from the group consisting of hydrogen, halogen, cyano, nitro, -OH, oxo, thiono, C₁₋₄-alkyl, C₁₋₄-halogenalkyl having 1 to 5 halogen atoms ,c. C83321c833317a-8324a-alcoxi, c83321a-838331a-8324-halogenoalcoxic, including 1 to 5 halogen atoms, c833238331a-c833226c-cyclo-nhl-83222;-NH (C -alquilo)-N (C -alquilo)-S-C₁₋₄-alkyl, -S (O) -C₁₋₄alkyl, -SO₂-C₁₋₄-alkyl, -S-C₁₋₄-halogenalkyl, -S (O) -C₁₋₄-halogenalkyl and - SO₂-C₁₋₄-halogenalkyl having 1 to 5 halogen atoms; R³ is selected from the group consisting of hydrogen, halogen, C₁₋₄-alkyl, C₁₋₄-haloalkyl having 1 to 5 halogen atoms, and C₃₋₆-cycloalkyl; R⁴ is selected from the group consisting of hydrogen, halogen, C₁₋₄-alkyl, C₁₋₄-halogenalkyl having 1 to 5 halogen atoms, C₃₋₆-cycloalkyl, -S-C₁₋₄-alkyl, - S (O) -C₁₋₄-alkyl, and -SO₂-C₁₋₄-alkyl;R⁵ is selected from the group consisting of hydrogen, fluorine, and C₁₋₄-alkyl; R⁶ is selected from the group consisting of hydrogen, fluorine, and C₁₋₄-alkyl; R⁷ is selected from the group consisting of hydrogen and C₁₋₄-alkyl; Q is selected from the group consisting of 6 or 10-membered aryl and 5 to 10-membered heteroaryl, each of which may be optionally substituted with 1, 2, 3, 4 or 5 substituents; or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, or a mixture thereof.
机译:1.要求1:具有共同分子式特征的化合物(1),a。 0、1、2、3或4; R来自氢,卤素,氰,氮-OH,c83321;自行车,nh832222,-NH(C -alquilo)-N(C -alquilo)-S-C₁₋₄-烷基,-S(O)-C₁₋₄-烷基,-SO 2-C₁₋₄-烷基,-S -C 1-卤代烷基,-S(O)-C 1-卤代烷基和-SO 2 -C 1-卤代烷基具有1-5个卤原子; n为0或1; X,Y独立地选自CR⁵R⁶,O。 S和n-r8311;其中X和Y中至少一个是CR 3 R 5; R 1选自氢,-CHO,-OH,C 1-烷基,具有1-5个卤素的C 1-卤代烷基原子,C 1-5卤原子的C 1-4烷氧基,C 1-4卤代烷氧基,1-5卤原子的C 1-4环烷基,C 1-4卤代环烷基,C 1-6烯基,C 1-6。 ₄-炔基,C 1-4-烷氧基-C 1-4烷基,C 1-4环烷基-C 1-4烷基,氰基-C 1-4烷基,氨基-C 1-4烷基,C 1-4烷基氨基- C 1-烷基,二-(C 1-烷基)氨基-C 1-烷基,C 1-烷基羰基,具有1-5个卤原子的C 1-卤代烷基羰基,C 1-烷氧基羰基,苄氧基羰基,C 4具有1至5个卤原子的C 1-烷氧基-C 1-烷基羰基,-SO 2 -C 4-烷基和-SO 2 -C 4 -C 1-卤代烷基; R 2选自氢,卤素,氰基,-CHO,C 1-烷基,C 2-8链烯基,C 2-8炔基,C 1-环烷基,C 1-8卤代烷基。 5个卤原子,C 1-烷氧基-C 1-烷基,具有1至5个卤原子的苄基,C 1-烷氧基,-NH 2,-NH(C-alquilo)-N(C-alquilo)-NH (C 1 -C 18环烷基)-N(C 1-4-烷基)(C 1-4-环烷基),-NH(4-7元的异性)-N(C 1-4烷基)(4-7元杂环烷基),-NH (C-醇氧基)-N(C-芳基)(C-醇氧基)-NH-SO-(C-醇基)-N(SO 2-[C 1-烷基])(C 1-烷基) -NH 2 -C 1-烷基,-SO 2 -C 1-烷基,-NH 2 -C 1-烷基,-SO 2 -C 4-烷基, (C 1-4烷氧基亚氨基)-C 1-6烷基,和选自4至7元杂环烷基的单环杂环,所述5元杂芳基具有至少一个氮原子,杂芳基环通过该氮原子与其余部分相连分子中的一个或多个具有至少一个氮原子的6-元杂芳基,R 2中的每个原子任选地是取代有1、2或3个独立地选自氢,卤素,氰基,硝基,-OH,氧代,硫代,C 1-8烷基的取代基的取代基。 C8321c83318324-1至5个卤素原子的卤素,c8321; -NH(C -alquilo)-N(C-alquilo)-SC -alquilo -S(O)-C -alquilo -SO -C -alquilo -SC -hal genoalquilo -S(O)-C -hal genalalquilo y -SC -hal genoalquilo que tiene entre 1 y 5 tomos de hal geno -NH(C -alquilo)-N(C -alquilo) NH(C-alquilo)-C(O)-N(C 1-4烷基)2,-C(O)-NH(C-cicloalquilo)C 1-4烷氧基,-S-C 4烷基,- S(O)-C 6-烷基,-SO 2 -C 6-烷基,或任选地被选自具有至少一个氮原子的4-7元或5元杂芳基的杂环烷基的单环杂环取代,并通过杂芳基环连接至C 1-烷基或C 1-环烷基的基团,它们各自任选地被1、2或3个独立地选自氢,卤素,氰基,硝基,-OH,氧代的取代基取代,硫代,具有1-5个卤原子的C 1-烷基,C 8-卤代烷基,c。 C83321c833317a-8324a-alcoxi,c83321a-838331a-8324-卤代含氧量,包括1-5个卤素原子,c833238331a-c833226c-cyclo-nhl-83222; -NH(C -alquilo)-N(C -alquilo)-S-C₁₋ ₄-烷基,-S(O)-C₁₋₄烷基,-SO 2-C₁₋₄-烷基,-S-C₁₋₄-卤代烷基,-S(O)-C₁₋₄-卤代烷基和-SO 2-C₁₋₄具有1-5个卤原子的-卤代烷基; R 3选自氢,卤素,C 1-4烷基,具有1-5个卤原子的C 1-4卤代烷基和C 1-4环烷基; R 5选自氢,卤素,C 1-8烷基,具有1-5个卤原子的C 1-8卤代烷基,C 1-6环烷基,-S-C 4烷基,-S(O) -C 1-烷基和-SO 2 -C 4-烷基; R 5选自氢,氟和C 1-烷基; R 5选自氢,氟和C 1-8烷基; R 5选自氢和C 1-8烷基; Q选自6或10元芳基和5至10元杂芳基,它们各自可以任选地被1、2、3、4或5个取代基取代;或其立体异构体,互变异构体,N-氧化物,水合物,溶剂化物或盐,或其混合物。

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