Lincomycin derivatives and antimicrobial agents comprising the same as active ingredient
    4.
    发明授权
    Lincomycin derivatives and antimicrobial agents comprising the same as active ingredient 失效
    林可霉素衍生物和包含与活性成分相同的抗微生物剂

    公开(公告)号:US07879808B2

    公开(公告)日:2011-02-01

    申请号:US12451744

    申请日:2008-05-30

    IPC分类号: A01N43/04 A61K31/70 C07H15/16

    CPC分类号: C07H15/16

    摘要: An objective of the present invention is to provide compounds of formula (1) or their pharmacologically acceptable salts or solvates wherein A represents aryl; R1 represents N-optionally substituted C1-6 alkyl-N-optionally substituted C1-6 alkylamino-C1-6 alkyl; R2 represents a hydrogen atom or optionally substituted C1-6 alkyl; R3 represents optionally substituted C1-6 alkyl or C3-6 cycloalkyl-C1-4 alkyl; m is 1 to 3; n is 0; and p is 0 to 2. The compounds are novel lincomycin derivatives that have a potent activity against resistant Streptococcus pneumoniae, which have recently posed problems, in the treatment of infectious diseases. Further, the compounds are usable as antimicrobial agents and are useful for preventing or treating bacterial infectious diseases.

    摘要翻译: 本发明的目的是提供式(1)化合物或其药理学上可接受的盐或溶剂化物,其中A表示芳基; R1表示N-任选取代的C 1-6烷基-N-任选取代的C 1-6烷基氨基-C 1-6烷基; R2表示氢原子或任选取代的C 1-6烷基; R3表示任选取代的C 1-6烷基或C 3-6环烷基-C 1-4烷基; m为1〜3; n为0; 并且p为0至2.该化合物是对感染性疾病的治疗中最近引起问题的抗性肺炎链球菌具有有效活性的新型林可霉素衍生物。 此外,该化合物可用作抗微生物剂,并且可用于预防或治疗细菌感染性疾病。

    LINCOMYCIN DERIVATIVES AND ANTIMICROBIAL AGENTS COMPRISING THE SAME AS ACTIVE INGREDIENT
    5.
    发明申请
    LINCOMYCIN DERIVATIVES AND ANTIMICROBIAL AGENTS COMPRISING THE SAME AS ACTIVE INGREDIENT 失效
    LINCOMYCIN衍生物和包含它们作为活性成分的抗微生物剂

    公开(公告)号:US20100210570A1

    公开(公告)日:2010-08-19

    申请号:US12451744

    申请日:2008-05-30

    CPC分类号: C07H15/16

    摘要: An objective of the present invention is to provide compounds of formula (1) or their pharmacologically acceptable salts or solvates wherein A represents aryl; R1 representsN-optionally substituted C1-6 alkyl-N-optionally substituted C1-6 alkylamino-C1-6 alkyl; R2 represents a hydrogen atom or optionally substituted C1-6 alkyl; R3 represents optionally substituted C1-6 alkyl or C3-6 cycloalkyl-C1-4 alkyl; m is 1 to 3; n is 0; and p is 0 to 2. The compounds are novel lincomycin derivatives that have a potent activity against resistant Streptococcus pneumoniae, which have recently posed problems, in the treatment of infectious diseases. Further, the compounds are usable as antimicrobial agents and are useful for preventing or treating bacterial infectious diseases.

    摘要翻译: 本发明的目的是提供式(1)化合物或其药理学上可接受的盐或溶剂化物,其中A表示芳基; R1表示N-任选取代的C 1-6烷基-N-任选取代的C 1-6烷基氨基-C 1-6烷基; R2表示氢原子或任选取代的C 1-6烷基; R3表示任选取代的C 1-6烷基或C 3-6环烷基-C 1-4烷基; m为1〜3; n为0; 并且p为0至2.该化合物是对感染性疾病的治疗中最近引起问题的抗性肺炎链球菌具有有效活性的新型林可霉素衍生物。 此外,该化合物可用作抗微生物剂,并且可用于预防或治疗细菌感染性疾病。

    Phosphonic acid derivatives having carboxypeptidase b inhibitory activity
    6.
    发明授权
    Phosphonic acid derivatives having carboxypeptidase b inhibitory activity 失效
    具有羧肽酶b抑制活性的膦酸衍生物

    公开(公告)号:US06576627B1

    公开(公告)日:2003-06-10

    申请号:US09926125

    申请日:2001-11-13

    IPC分类号: A61K31662

    摘要: A compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof: wherein R1 represents hydrogen atom, an alkyl group, a substituted alkyl group and the like; R2 and R3 represent hydrogen atom, an alkyl group, a substituted alkyl group, an alkoxyl group and the like; X represents —CH2—, —O—, or —NH—; A represents the following group (II): [in which R7 and R8 represent hydrogen atom, an alkyl group, an acyl group, an alkoxycarbonyl group and the like; R9 and R10 represents hydrogen atom, a halogen atom, hydroxyl group, phenyl group, an alkyl group and the like] and the like; and E represents hydrogen atom and the like, which has inhibitory activity against carboxypeptidase B and is useful for therapeutic and/or preventive treatment of a thrombotic disease.

    摘要翻译: 由以下通式(I)表示的化合物及其药理学上可接受的盐:其中R1表示氢原子,烷基,取代的烷基等; R2和R3表示氢原子,烷基,取代的烷基,烷氧基等; X表示-CH 2 - , - O-或-NH-; A表示以下的基团(II):[其中R7和R8表示氢原子,烷基,酰基,烷氧基羰基等; R9和R10表示氢原子,卤原子,羟基,苯基,烷基等〕等; E表示氢原子等,其对羧肽酶B具有抑制活性,可用于治疗和/或预防性治疗血栓性疾病。

    Phosphonic acid derivative having inhibitory activity against carboxypeptidase B
    7.
    发明授权
    Phosphonic acid derivative having inhibitory activity against carboxypeptidase B 失效
    对羧肽酶B具有抑制活性的膦酸衍生物

    公开(公告)号:US06737416B2

    公开(公告)日:2004-05-18

    申请号:US10265400

    申请日:2002-10-07

    IPC分类号: A61K3144

    摘要: A compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof: wherein R1 represents hydrogen atom, an alkyl group, a substituted alkyl group and the like; R2 and R3 represent hydrogen atom, an alkyl group, a substituted alkyl group, an alkoxyl group and the like; X represents —CH2—, —O—, or —NH—; A represents the following group (II): [in which R7 and R8 represent hydrogen atom, an alkyl group, an acyl group, an alkoxycarbonyl group and the like; R9 and R10 represents hydrogen atom, a halogen atom, hydroxyl group, phenyl group, an alkyl group and the like] and the like; and E represents hydrogen atom and the like, which has inhibitory activity against carboxypeptidase B and is useful for therapeutic and/or preventive treatment of a thrombotic disease.

    摘要翻译: 由以下通式(I)表示的化合物及其药理学上可接受的盐:其中R 1表示氢原子,烷基,取代的烷基等; R 2和R 3代表氢原子,烷基,取代的烷基,烷氧基等; X表示-CH 2 - , - O-或-NH-; A表示以下的基团(II):[其中R 7和R 8表示氢原子,烷基,酰基,烷氧基羰基等; R 9和R 10代表氢原子,卤原子,羟基,苯基,烷基等〕等; E表示氢原子等,其对羧肽酶B具有抑制活性,可用于治疗和/或预防性治疗血栓性疾病。