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Azaspiro n,m-alkanes and diazaspiro n,m-alkanes

机译:Azaspiro n,间烷烃和diazaspiro n,间烷烃

摘要

A compound of formula I, having antibacterial activity and a pharmaceutical composition containing the compound of formula I: CHEM wherein a represents an integer equal to 0 or 1; b represents an integer equal to 2 through 5, inclusive; c represents an integer equal to 0 or 1; and d represents an integer equal to 0 through 2, inclusive; Z represents @CHR1, @NR2, @C=NOR3, an oxygen atom or a sulfur atom, wherein R1 represents a hydrogen atom, an amino group, a monoalkylamino group of 1 to 6 carbon atoms, a dialkylamino group containing 1 to 6 carbon atoms per alkyl, a hydroxyl group, an alkoxy group of 1 to 6 carbon atoms or a hydroxyalkyl group of 1 to 6 carbon atoms; R2 represents a hydrogen atom, an alkyl group of 1 to 6 carbon atoms, a hydroxyalkyl group of 1 to 6 carbon atoms, a haloalkyl group of 1 to 6 carbon atoms, a formyl group or an alkylcarbonyl group of 2 to 7 carbon atoms; and R3 represents a hydrogen atom or an alkyl group of 1 to 6 carbon atoms; Q represents a partial structure of formula II: CHEM wherein R4 represents an alkyl group of 1 to 6 carbon atoms, an alkenyl group of 2 to 6 carbon atoms, a haloalkyl group of 1 to 6 carbon atoms, a substituted or unsubstituted cycloalkyl group of 3 to 6 carbon atoms, a substituted or unsubstituted aryl group, a substituted or unsubstituted heteroaryl group, an alkoxy group of 1 to 6 carbon atoms or an alkylamino group of 1 to 6 carbon atoms; R5 represents a hydrogen atom or an alkyl group of 1 to 6 carbon atoms; R6 represents a hydrogen atom, a substituted or unsubstituted amino group, a hydroxyl group, an alkoxy group of 1 to 6 carbon atoms or a halogen atom; A represents a nitrogen atom or @C-R7, wherein R7 represents a hydrogen atom, an alkyl group of 1 to 6 carbon atoms, a halogen atom, an alkoxy group of 1 to 6 carbon atoms, a haloalkyl group of 1 to 6 carbon atoms or a cyano group; R4 may, taken together with R5 and/or R7, form a substituted or unsubstituted ring which can include an oxygen, nitrogen or sulfur atom, wherein the substituent is an alkyl group of 1 to 6 carbon atoms or a haloalkyl group of 1 to 6 carbon atoms; X represents a halogen atom; Y represents a hydrogen atom, an alkyl group of 1 to 6 carbon atoms, an alkoxyalkyl group of 1 to 6 carbon atoms, a phenylalkyl group containing 1 to 6 carbon atoms in its alkyl moiety, a dihaloboron group, a phenyl group, an acetoxymethyl group, a pivaloyloxymethyl group, an ethoxycarbonyloxy group, a choline group, a dimethylaminoethyl group, a 5-indanyl group, a phthalidinyl group, a 5-substituted-2-oxo-1,3-dioxazol-4-ylmethyl group or a 3-acetoxy-2-oxobutyl group, or a salt thereof.
机译:具有抗菌活性的式I化合物和包含式I化合物的药物组合物:[化学式]其中a表示等于0或1的整数; b表示等于2到5的整数(含2和5); c表示等于0或1的整数; d表示0至2的整数,包括0和2。 Z代表@CHR 1,@ NR 2,@ C = NOR 3,氧原子或硫原子,其中R 1代表氢原子,氨基,1至1的单烷基氨基。 6个碳原子,每个烷基含1至6个碳原子的二烷基氨基,羟基,1至6个碳原子的烷氧基或1至6个碳原子的羟烷基; R 2代表氢原子,1至6个碳原子的烷基,1至6个碳原子的羟烷基,1至6个碳原子的卤代烷基,甲酰基或2至7个烷基羰基碳原子R 3表示氢原子或碳原子数1〜6的烷基。 Q代表式II的部分结构:<化学式>其中R 4代表碳数为1至6的烷基,碳数为2至6的烯基,碳数为1至6的卤代烷基,或3至6个碳原子的未取代的环烷基,取代或未取代的芳基,取代或未取代的杂芳基,1至6个碳原子的烷氧基或1至6个碳原子的烷基氨基;或R 5表示氢原子或碳原子数1〜6的烷基。 R 6表示氢原子,取代或未取代的氨基,羟基,1〜6个碳原子的烷氧基或卤素原子。 A代表氮原子或@CR 7,其中R 7代表氢原子,1-6个碳原子的烷基,卤原子,1-6个碳原子的烷氧基,卤代烷基。 1-6个碳原子或氰基; R 4可以与R 5和/或R 7一起形成取代或未取代的环,其可以包括氧,氮或硫原子,其中取代基是1-6个碳的烷基原子或1-6个碳原子的卤代烷基; X代表卤原子; Y代表氢原子,1至6个碳原子的烷基,1至6个碳原子的烷氧基烷基,在其烷基部分含有1至6个碳原子的苯烷基,二卤代硼烷基,苯基,乙酰氧基甲基基团,新戊酰氧基甲基基团,乙氧基羰基氧基基团,胆碱基团,二甲基氨基乙基基团,5-茚满基基团,邻苯二甲酰基,5-取代的-2-氧代-1,3-二恶唑-4-基甲基或3 -乙酰氧基-2-氧丁基或其盐。

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