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    • 5. 发明申请
    • ANTIBACTERIAL AGENTS
    • 抗菌剂
    • WO1998025932A1
    • 1998-06-18
    • PCT/US1997022356
    • 1997-12-05
    • WARNER-LAMBERT COMPANYDOMAGALA, John, MichaelELLSWORTH, Edmund, LeeSTIER, Michael, AndrewHUANG, LirenMICETICH, Ronald, GeorgeSINGH, RajeshwarWRIGLEY, Stephen, KeithWANG, ShoumingROE, MichaelTHORNTON, David, Michael
    • WARNER-LAMBERT COMPANY
    • C07D498/04
    • C07D487/04C07D513/04
    • Described are antibacterial agents of formula (I): X is O, S or N-R8; R1, R2, R3 and R8 are independently H, straight or branched alkyl of 1-6 carbons, cycloalkyl of 3-6 carbons, alkenyl or alkynyl of from 2 to 6 atoms, heterocyclic ring of from 5-8 atoms with 1-3 heteroatoms as nitrogen, oxygen or sulfur, or phenyl, all of which rings may be optionally substituted up to 3 times by halogen, OR, NR2, NR'COR', CN, CO2R' or CONR2', halogen, CN, CO2R, COR, CON(R)2, CON(R")2, SR, SON, SCO2R or SCON(R)2; R4 is H, straight or branched alkyl of from 1-6 carbon atoms, alkenyl or alkynyl of from 2 to 6 atoms, heterocyclic ring of from 5-8 atoms with 1-3 heteroatoms as nitrogen, oxygen or sulfur or phenyl, all of which rings may be optionally substituted up to 3 times by halogen, OR, NR2, NR'COR', CN, CO2R' or CONR2', halogen, CN, NO2, N(R)2, NRCOR, NRCOR", COR, CO2R, CON(R)2, CON(R")2, NRCON(R)2, NRCO2R; R5 is 1-6 straight or branched alkyl, a cycloalkyl of 3-6 carbons, alkenyl or alkynyl of from 2 to 6 atoms, heterocyclic ring of from 5-8 atoms with 1-3 heteroatoms as nitrogen, oxygen or sulfur or phenyl, all of which rings may be optionally substituted up to 3 times by halogen, OR, NR2, NR'COR', CN, CO2R' or CONR2', halogen, OR, N(R)2, NRCOR, NRCOR", COR, CON(R)2, CON(R")2, SR or SO2R; R6, R7 are independently H, straight or branched alkyl of 1-6 carbons, cycloalkyl of 3-6 carbons, COR, COR", SO2NR2, CONR2 and these may be optionally substituted by any of the groups listed for R5; R is H, straight or branched alkyl of 1-6 carbon atoms, cycloalkyl of from 3-6 carbon atoms, heterocyclic ring of from 5-8 atoms with 1-3 heteroatoms as nitrogen, oxygen or sulfur, or pheny, all of which may be optionally substituted by halogen, OR', NR'2, NR'COR', CN, CO2R', CONR'2; R' is H, alkyl of from 1-3 carbon atoms or Ph; R" is part of a naturally occurring amino acid connected via an amide or acyl bond as determined by the formula; halogen is any one of fluoro, chloro, bromo or iodo; or a pharmaceutically acceptable salt.
    • 描述了式(I)的抗菌剂:X是O,S或N-R8; R1,R2,R3和R8独立地为H,1-6个碳的直链或支链烷基,3-6个碳原子的环烷基,2-6个碳原子的烯基或炔基,5-8个原子的杂环,1-3个 杂原子作为氮,氧或硫或苯基,所有这些环可以任选被卤素,OR,NR 2,NR'COR',CN,CO 2 R'或CONR 2',卤素,CN,CO 2 R,COR ,CON(R)2,CON(R“)2,SR,SON,SCO 2 R或SCON R 2; R 4是H,1-6个碳原子的直链或支链烷基,2至6的烯基或炔基 原子,5-8个原子与1-3个杂原子作为氮原子的杂环,氧或硫或苯基,所有这些环可以任选地被卤素OR,NR 2,NR'COR',CN, CO 2 R,CONR 2,CON(R“)2,NRCON(R)2,NRCO 2 R; R 5是 1-6个直链或支链烷基,3-6个碳原子的环烷基,2-6个碳原子的烯基或炔基,5-8个原子的杂环和1-3个杂原子 作为氮,氧或硫或苯基,所有这些环可以任选被卤素,OR,NR 2,NR'COR',CN,CO 2 R'或CONR 2',卤素,OR,N(R) 2,NRCOR,NRCOR“,COR,CON(R)2,CON(R”)2,SR或SO2R; R 6,R 7独立地是H,1-6个碳的直链或支链烷基,3-6个碳的环烷基,COR,COR“,SO2NR2,CONR2,并且它们可以任选被R5所列的任何基团取代; R是H ,1-6个碳原子的直链或支链烷基,3-6个碳原子的环烷基,5-8个原子的杂环,1-3个杂原子作为氮,氧或硫或苯基,所有这些可以是任选的 被卤素取代,OR',NR'2,NR'COR',CN,CO2R',CONR'2; R'是H,1-3个碳原子的烷基或Ph; R“是天然存在的氨基 通过由式决定的酰胺或酰基键连接酸; 卤素是氟,氯,溴或碘中的任何一种; 或药学上可接受的盐。