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    • 13. 发明专利
    • New dihydropyrimidine derivatives and their corresponding mesomers useful as antiviral agents
    • DE19817264A1
    • 1999-10-21
    • DE19817264
    • 1998-04-18
    • BAYER AG
    • STOLTEFUS JUERGENGOLDMANN SIEGFRIEDPAESSENS ARNOLDGRAEF ERWINLOTTMANN STEFAN
    • C07D213/78A61K31/506A61P1/16A61P31/12C07D213/00C07D213/84C07D215/00C07D239/00C07D239/22C07D277/62C07D401/04C07D401/14C07D417/14C07D403/04C07D405/04C07D409/04C07D417/04C07D491/048A61K31/505
    • Dihydropyrimidine derivatives (I) and their mesomers (I') are new. Dihydropyrimidine derivatives of formula (I) and their mesomers of formula (I') are new. R = phenyl, furyl, thienyl, triazolyl, pyridyl, 3-6C cycloalkyl, 4-isoquinolinyl, 3-phenylquinolin-5-yl or 2-phenylbenzothiazol-4-yl (the ring systems are (a) optionally substituted by one or more halo, CF3, NO2, CN, OCF3, COOH, OH, 1-6C alkoxy, (1-6C alkoxy)carbonyl or 1-6C alkyl groups, where the latter may itself be substituted by 6-10C aryl or halo, and/or (b) may contain one or more hetero groups selected from S-R , NR R , CONR R , SO2-CF3 and A-CH2-R ); R = phenyl optionally substituted by halo; R -R = independently H, phenyl, hydroxyphenyl, OH, 1-6C acyl or 1-6C alkyl, which itself may be substituted by OH, (1-6C alkoxy)carbonyl, phenyl or hydroxyphenyl; A = O, S, SO or SO2; R = phenyl (optionally substituted by one or more halo, NO2, CF3, 1-6C alkyl or 1-6C alkoxy groups); R = XR or NR R ; X = O or a bond; R = H, (1-6C alkoxy)carbonyl or a 1-8C hydrocarbon (which may be cyclic and/or be interrupted by one or two O, CO, NH, NH(1-4C alkyl), N(1-4C alkyl)2, S or SO2 groups and which is optionally substituted by halo, NO2, CN, OH, 6-10C aryl or aralkyl, heteroaryl or NR R ; R , R = H, benzyl or 1-6C alkyl; R , R = H, 1-6C alkyl or 3-6C cycloalkyl; R = H, NH2 or CH(OCH3)2, or CHO, CN, CF3 or pyridyl, or a 1-8C hydrocarbon group which is optionally substituted by 6-10C aryloxy, N3, CN, OH, COOH, (1-6C alkoxy)carbonyl, a 5-7 membered heterocycle, 1-6C alkylthio or 1-6C alkoxy (which itself may be substituted by N3 or NH2) and/or by triazolyl (which may itself be substituted by 1-3 (1-6C alkoxy)carbonyl groups), and/or by OSO2-CH3 or (CO)a-NR R ; a = 0 or 1; R , R = independently H or 6-10C aryl or aralkyl, or 1-6C alkyl (optionally substituted by (1-6C alkoxy)carbonyl, OH, phenyl or benzyl (where the phenyl or benzyl groups are themselves optionally substituted by OH, COOH, 1-6C alkyl or 1-6C alkoxy), or by NH-CO-CH3 or NH-CO-CF3); or NR R = morpholine, piperidine or pyrrolidine; R = may also be phenyl or methoxyphenyl; or R +R = O-CH2; R = H, 1-4C alkyl, 2-4C alkenyl, benzoyl or 2-6C acyl; R = pyridyl (optionally substituted by 1-3 halo, OH, CN, CF3, 1-6C alkoxy, 1-6C alkyl, 1-6C alkylthio, carbalkoxy (sic), 1-6C acyloxy, NH2, NO2, or mono- or di-(1-6C alkylamino). An Independent claim is also included for preparation of (I).
    • 14. 发明专利
    • New dihydropyrimidine derivatives and their corresponding mesomers useful in treatment of hepatitis
    • DE19817262A1
    • 1999-10-21
    • DE19817262
    • 1998-04-18
    • BAYER AG
    • GOLDMANN SIEGFRIEDSTOLTEFUS JUERGENPAESSENS ARNOLDGRAEF ERWINLOTTMANN STEFAN
    • C07D417/04A61K20060101A61K31/425A61K31/505A61K31/506A61P1/16C07D20060101C07D413/04C07D417/14
    • Dihydropyrimidine derivatives (I) and their mesomers (I') are new. Dihydropyrimidine derivatives of formula (I) and their mesomers of formula (I') are new. R = phenyl, furyl, thienyl, pyridyl, 3-6C cycloalkyl, 4-isoquinolinyl, 3-phenylquinolin-5-yl or 2-phenylbenzothiazol-4-yl (the ring systems are (a) optionally substituted by one or more halo, CF3, NO2, CN, OCF3, COOH, OH, 1-6C alkoxy, (1-6C alkoxy)carbonyl or 1-6C alkyl groups, where the latter may itself be substituted by 6-10C aryl or halo, and/or (b) may contain one or more hetero groups selected from S-R , NR R , CONR R , SO2-CF3 and A-CH2-R ); R = phenyl optionally substituted by halo; R -R = independently H, phenyl, hydroxyphenyl, OH, 1-6C acyl or 1-6C alkyl, which itself may be substituted by OH, (1-6C alkoxy)carbonyl, phenyl or hydroxyphenyl; A = O, S, SO or SO2; R = phenyl (optionally substituted by one or more halo, NO2, CF3, 1-6C alkyl or 1-6C alkoxy groups); R = OR or NR R ; R = H, (1-6C alkoxy)carbonyl or a 1-8C hydrocarbon (which may be cyclic and/or be interrupted by one or two O, CO, NH, NH(1-4C alkyl), N(1-4C alkyl)2, S or SO2 groups and which is optionally substituted by halo, NO2, CN, OH, 6-10C aryl or aralkyl, heteroaryl or NR R ; R , R = H, benzyl or 1-6C alkyl; R , R = H, 1-6C alkyl or 3-6C cycloalkyl; R = H, NH2 or CH(OCH3)2, or CHO, CN or CF3, or a 1-8C hydrocarbon group which is optionally substituted by 6-10C aryloxy, N3, CN, OH, COOH, (1-6C alkoxy)carbonyl, a 5-7 membered heterocycle, 1-6C alkylthio or 1-6C alkoxy (which itself may be substituted by N3 or NH2) and/or by triazolyl (which may itself be substituted by 1-3 (1-6C alkoxy)carbonyl groups), and/or by OSO2-CH3 or (CO)a-NR R ; a = 0 or 1; R , R = independently H or 6-10C aryl or aralkyl, or 1-6C alkyl (optionally substituted by (1-6C alkoxy)carbonyl, OH, phenyl or benzyl (where the phenyl or benzyl groups are themselves optionally substituted by OH, COOH, 1-6C alkyl or 1-6C alkoxy), or by NH-CO-CH3 or NH-CO-CF3); R = H, 1-4C alkyl, acetyl or benzoyl; D = O or S; R = H, halo or 1-6C alkyl. An Independent claim is also included for preparation of (I).