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NAFTIRIDONES AND QUINOLONAS 7-AMINO ALQUILIDENIL-HETEROCICLICAS.

机译:萘啶酮和喹诺酮7-氨基壬二烯-杂环。

摘要

A compound having a structure according to formula I ** (See formula) ** in which: n is an integer from 1 to 3; m is an integer from 1 to 3; z is an integer from 0 to 3; R is hydrogen, hydroxy or alkoxy; R 2 is hydrogen; R3 and R4 are independently hydrogen, halogen, amino, hydroxy, alkoxy, alkylthio, alkyl, alkenyl or alkynyl; R5 is hydrogen, hydroxyl, halogen, alkyl, aryl, alkoxy or alkylthio; and R6 is alkyl, hydroxy, alkoxy, alkylthio, alkenyl, alkynyl, aryl, alkoxyimino or halogen; or R5 and R6 join to form a 4- to 7-membered carbocyclic ring in which each carbon atom of the ring may be optionally substituted with R 12; R 12 is halogen, amino, hydroxy, alkoxy, alkylthio, alkyl, alkenyl, alkynyl, oxo, alkoxyimino or hydroxyimino; E is good: 1) ** (See formula) ** in which: q is an integer from 1 to 3; R7 and R8 are independently hydrogen or alkyl; or R7 and R8 join to form a 3 to 6 member carbocyclic ring; or any one between R7 or R8 can be independently linked with any one between R9 or R10 to form a heterocyclic ring containing the nitrogen atom to which R 9 or R 10 is attached; R9 and R10 are independently hydrogen, alkyl, acyl, alkoxycarbonyl or sulfonyl; or R9 and R10 join to form a heterocyclic ring containing the nitrogen atom to which they are attached; or 2) ** (See formula) ** in which: q is as defined above; R7 and R8 are independently hydrogen or alkyl; or R7 and R8 join to form a 3 to 6 member carbocyclic ring; R9 is hydrogen, alkyl, acyl, alkoxycarbonyl or sulfonyl; or 3) alkenyl; A is N or C (R11); R11 is hydrogen, alkyl, halogen, hydroxyl, alkoxy, alkylthio or cyano; X is C or N, such that if X is C, a is a double bond and b is a simple link, if X is N, a is a single link and b is a double bond; Y is N (R1) or C (R1), with the proviso that when Y is N (R1), X is C, and when Y is C (R1), X is N; and R1 is cycloalkyl (C3-C6), heterocycloalkyl (C4-C6), alkyl, alkene, a 6-membered aryl or a 6-membered heteroaryl, with the proviso that if A is C (R 11), X is C and Y is N (R 1), then R 11 and R 1 can be joined to form a 6-membered heterocyclic ring, if A is C (R 11), X is C and Y is N (R 1), then R 2 and R 1 can be joined to form a monocyclic or bicyclic heterocyclic ring, and if A is C (R11), X is C and Y is N (R1), then R2 and R can be joined to form a heterocyclic ring of 5 members; or an isomer, diastereomer or optical enantiomer thereof; a pharmaceutically acceptable salt or hydrate thereof.
机译:具有式I **(参见式)**的结构的化合物,其中:n为1至3的整数; m是1至3的整数; z是0至3的整数; R为氢,羟基或烷氧基; R 2为氢; R3和R4独立地是氢,卤素,氨基,羟基,烷氧基,烷硫基,烷基,烯基或炔基; R5是氢,羟基,卤素,烷基,芳基,烷氧基或烷硫基; R6为烷基,羟基,烷氧基,烷硫基,烯基,炔基,芳基,烷氧基亚氨基或卤素; R 5和R 6连接形成4至7元碳环,其中环的每个碳原子可任选地被R 12取代;或R 12为卤素,氨基,羟基,烷氧基,烷硫基,烷基,烯基,炔基,氧代,烷氧基亚氨基或羟基亚氨基; E好:1)**(请参见公式)**其中:q是1到3的整数; R7和R8独立地是氢或烷基; R7和R8连接形成3至6元碳环;或R 7或R 8之间的任一者可独立地与R 9或R 10之间的任一者连接而形成含有连接有R 9或R 10的氮原子的杂环。 R9和R10独立地是氢,烷基,酰基,烷氧羰基或磺酰基; R9和R10连接形成含有它们所连接的氮原子的杂环;或2)**(参见公式)**,其中:q如上定义; R7和R8独立地是氢或烷基; R7和R8连接形成3至6元碳环;或R9是氢,烷基,酰基,烷氧羰基或磺酰基;或3)烯基; A是N或C(R11); R11是氢,烷基,卤素,羟基,烷氧基,烷硫基或氰基; X为C或N,因此如果X为C,则a为双键,b为简单键;如果X为N,则a为单键,b为双键; Y为N(R1)或C(R1),条件是当Y为N(R1)时,X为C,当Y为C(R1)时,X为N;并且R1是环烷基(C3-C6),杂环烷基(C4-C6),烷基,烯烃,6元芳基或6元杂芳基,条件是如果A是C(R 11),则X是C并且Y为N(R 1),则R 11和R 1可以连接形成6元杂环,如果A为C(R 11),X为C并且Y为N(R 1),则R 2 R 1可以连接形成单环或双环杂环,如果A为C(R11),X为C和Y为N(R1),则R2和R可以连接形成5个成员的杂环;或其异构体,非对映异构体或旋光对映体;其药学上可接受的盐或水合物。

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