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Heteroryl-isozolidines, their method of manufacture, use in the manufacture of medicinal products and medicinal products containing these compounds.

机译:杂异-异唑烷类及其制造方法,用于制造医药产品和含有这些化合物的医药产品。

摘要

Heteroaryl-oxazolidinone compounds of formula (I), and their stereoisomers, stereoisomer mixtures and salts are new. R1 = CO2R2, SO2R2, CO-R3 or CO-NR4R5; R2 = phenyl or 1-7C alkyl; R3 = CF3 or 1-6C alkyl (optionally substituted by halo or CF3); R4, R5 = H, phenyl or 1-5C alkyl; A = beta -carbolin-3-yl, indolizinyl linked via the 6-membered ring, C-linked mono-, bi- or tri- cyclic aromatic heterocycle with 6-membered rings, at least one of which contains nitrogen, or a C-linked 5-membered aromatic heterocycle containing up to 3 heteroatoms (optionally benzo- or naphtho-fused) (all optionally ring-substituted by NR6R7, Q, a group of formula (a) and/or 1-3 Q'); Q' = COOH, halo, CN, mercapto, CHO, CF3, NO2, alkoxy, alkoxycarbonyl, alkylthio, acyl or alkyl (optionally substituted by OH, 1-5C alkoxy, 1-5C acyl or NR61R71); Q = 2-8C alkylphenyl, phenyl or Het (all optionally substituted by one of CONR8R9, NR10R11, NR12SO2R13, SO2NR14R15 or S(O)aR16, and/or 1-2 Q'); R6, R7, R61, R71, R10, R11 = H, 3-6C cycloalkyl, 1-5C alkyl, or phenyl; or NR6R7, NR61R71, NR10R11 = 5-6 membered, saturated heterocycle, optionally containing a second heteroatom and which may be substituted (on C or on a second N atom) by 1-3C alkyl or 1-3C acyl; R8, R9, R12, R14, R15 = H, alkyl or phenyl; R13, R16 = 1-4C alkyl, or phenyl (optionally substituted by 1-4C alkyl); a, n = 0-2; heteroatom = N, O or S; alkyl, alkoxy have 1-6C unless specified otherwise.
机译:式(I)的杂芳基-恶唑烷酮化合物及其立体异构体,立体异构体混合物和盐是新的。 R1 = CO2R2,SO2R2,CO-R3或CO-NR4R5; R2 =苯基或1-7C烷基; R3 = CF3或1-6C烷基(任选被卤素或CF3取代); R4,R5 = H,苯基或1-5C烷基; A =通过6-元环连接的β-咔啉-3-基,吲哚啉基,具有6-元环的C联单环,双环或三环芳族杂环,其中至少一个含氮或C -连接的5元芳族杂环,其含有至多3个杂原子(任选地为苯并或萘稠合的)(全部任选地被NR 6 R 7,Q,式(a)和/或1-3 Q'的基团环取代); Q′= COOH,卤素,CN,巯基,CHO,CF 3,NO 2,烷氧基,烷氧羰基,烷硫基,酰基或烷基(任选被OH,1-5C烷氧基,1-5C酰基或NR61R71取代); Q = 2-8C烷基苯基,苯基或Het(全部可选地被CONR8R9,NR10R11,NR12SO2R13,SO2NR14R15或S(O)aR16和/或1-2 Q'之一取代); R6,R7,R61,R71,R10,R11 = H,3-6C环烷基,1-5C烷基或苯基;或NR 6 R 7,NR 61 R 71,NR 10 R 11 = 5-6元的饱和杂环,任选地包含第二个杂原子,并且可以被1-3C烷基或1-3C酰基取代(在C上或在第二N原子上); R8,R9,R12,R14,R15 = H,烷基或苯基; R13,R16 = 1-4C烷基或苯基(任选地被1-4C烷基取代); a,n = 0-2;杂原子= N,O或S;除非另有说明,否则烷基,烷氧基具有1-6C。

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