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    • 29. 发明专利
    • New 1-heterocyclyl-5-carbonylaminomethyl-isoxazoline and 1-heterocyclyl-5-thionocarbonylaminomethyl-isoxazoline derivatives useful as antibacterial agents in human and veterinary medicine
    • DE19909785A1
    • 2000-09-07
    • DE19909785
    • 1999-03-05
    • BAYER AG
    • WILD HANNORADDATZ SIEGFRIEDHAERTER MICHAELROSENTRETER ULRICHBARTLE STEPHANENDERMANN RAINERKROLL HEIN-PETER
    • C07D413/04C07D498/04A61K31/42C07D413/14C07D417/04C07D471/04C07D487/04C07D513/04
    • 1-Heterocyclyl-5-(thiono)carbonylaminomethyl-isoxazoline derivatives (I) are new. 1-Heterocyclyl-5-(thiono)carbonylaminomethyl-isoxazoline derivatives of formula (I) and their tautomers and salts are new. Z' = O or S; R = H, alkoxy, benzyloxy, CF3, cycloalkyl (optionally substituted by halo or aryl), aryl or saturated or aromatic heterocyclyl (each optionally mono- or disubstituted by halo, CN, NO2, OH or phenyl), alkyl (optionally substituted by phenoxy, benzyloxy, COOH, halo, alkoxycarbonyl, acyl or heterocyclyl), or optionally mono- or disubstituted amino; A = group of formula (a) - (h); G , L , M = H, COOH, halo, CN, CHO, CF3, NO2, alkyl, or optionally mono- or disubstituted aminocarbonyl; R = H, cycloalkylcarbonyl, cycloalkyl, alkoxycarbonyl, alkyl or alkenyl optionally substituted by one of 15 groups selected from pyrrolidin-3-yl, 5-nitro-pyrid-2-yl, pyrid-2-yl, pyrid-4-yl, piperidin-4-yl, 1-benzyl-piperidin-4-yl, 1-benzyl-pyrrolidin-3-yl, COCl3 (sic), acyl optionally substituted with 4 groups, optionally mono- or disubstituted amino or aminocarbonyl, optionally substituted sulfonylamino or aminosulfonyl, or (alkyl, benzyl, phenyl or tolyl)-S(O)f; f = 0-2; D , E = O or S; or E = substituted imino when R is not H; R , R 1', R 1'' = H or halo; D , D2', D2'' = N, or C optionally substituted by groups; E , E2' and E2'' = N or C optionally substituted by 11 groups; L , L2' and L2'' = N or C optionally substituted by 8 groups; Q = O, S, SO2, SO, CO, or C optionally mono- or disubstituted by halo; T = C optionally mono- or disubstituted by 5 groups, CO, CS or optionally substituted methylidene or imino; V = O, S, SO, or SO2; W = O, S, CO, CS, SO, SO2, optionally substituted amino, or C optionally mono- or disubstituted by halo, alkyl or benzyl or monosubstituted with alkoxy, acyloxy or benzyloxy; Y = CO or C optionally mono- or disubstituted by halo, alkyl or benzyl or monosubstituted with alkoxy, acyloxy or benzyloxy; or W + Y = -CH=CH-; R = H, halo, or alkyl; E = H or halo; A + D = C(R )(R )L C(R )(R ) or C(R )(R )L3'C(R )(R )C(R )(R ); L , L3' = O, NH, or N substituted by COOH, cycloalkyl, alkoxycarbonyl or optionally substituted acyl; D , D4' and D4'' = H, COOH, halo, CN, CHO, CF3, NO2, or alkoxy, alkoxycarbonyl, alkylthio, acyl or alkyl; E , E4' = CH2, O, S, SO, or SO2; L = O, S, or optionally substituted imino; R - R , R - R = H, or alkyl or alkenyl each optionally substituted by aryl or heteroaryl; or R + R , R + R , R + R , R + R = =O, =CH2 or aryl-substituted or heteroaryl-substituted methylidene; R , R , R = H, alkyl, alkoxycarbonyl, or arylcarbonyl, heteroarylcarbonyl or alkylcarbonyl (each optionally substituted). The full definitions are given in the DEFINITIONS (Full Definitions) Field.