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    Lincosamide derivatives and antimicrobial agents comprising the same as active ingredient
    1.
    发明授权
    Lincosamide derivatives and antimicrobial agents comprising the same as active ingredient 失效
    林可酰胺衍生物和包含与活性成分相同的抗微生物剂

    公开(公告)号：US07867980B2

    公开(公告)日：2011-01-11

    申请号：US12451752

    申请日：2008-05-30

    申请人： Eijirou Umemura ,  Kou Kumura ,  Satomi Masaki ,  Kazutaka Ueda ,  Yoshinari Wakiyama ,  Yasuo Sato ,  Mikio Yamamoto ,  Keiichi Ajito ,  Takashi Watanabe ,  Chizuko Kaji

    发明人： Eijirou Umemura ,  Kou Kumura ,  Satomi Masaki ,  Kazutaka Ueda ,  Yoshinari Wakiyama ,  Yasuo Sato ,  Mikio Yamamoto ,  Keiichi Ajito ,  Takashi Watanabe ,  Chizuko Kaji

    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 (I) or their pharmacologically acceptable salts or solvates wherein A represents aryl while R1 represents a five- or six-membered monocyclic heterocyclic group, or A represents a four- to six-membered monocyclic heterocyclic group while R1 represents aryl or a five- or six-membered monocyclic heterocyclic group; R2 represents a hydrogen atom or C1-6 alkyl; R3 represents C1-6 alkyl or C3-6 cycloalkyl-C1-4 alkyl; R4, R5, and R6 represent a hydrogen atom; R7 represents C1-6 alkyl; and m is 1 to 3. The compounds are novel lincosamide derivatives that have a potent activity against resistant Streptococcus pneumoniae. 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（I）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，而R1表示五元或六元单环杂环基，或A表示四至六元 单环杂环基，而R1代表芳基或五元或六元单环杂环基; R2表示氢原子或C1-6烷基; R 3表示C 1-6烷基或C 3-6环烷基-C 1-4烷基; R4，R5和R6表示氢原子; R 7表示C 1-6烷基; 并且m为1至3.该化合物是对耐药性肺炎链球菌具有有效活性的新型长春花胺衍生物。 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
    2.
    发明申请
    Lincomycin Derivatives and Antimicrobial Agents Comprising the Same as Active Ingredient 失效
    含有与活性成分相同的林可霉素衍生物和抗微生物剂

    公开(公告)号：US20090156512A1

    公开(公告)日：2009-06-18

    申请号：US12086279

    申请日：2006-12-11

    申请人： Eijirou Umemura ,  Yoshinari Wakiyama ,  Kazutaka Ueda ,  Kou Kumura ,  Satomi Masaki ,  Takashi Watanabe ,  Mikio Yamamoto ,  Chizuko Kaji ,  Keiichi Ajito

    发明人： Eijirou Umemura ,  Yoshinari Wakiyama ,  Kazutaka Ueda ,  Kou Kumura ,  Satomi Masaki ,  Takashi Watanabe ,  Mikio Yamamoto ,  Chizuko Kaji ,  Keiichi Ajito

    IPC分类号： A61K31/7004 ,  C07H15/16 ,  A61P31/04

    CPC分类号： C07H15/16

    摘要： This invention provides compounds of formula (I) or its pharmacologically acceptable salt or solvate, wherein A represents aryl or a monocyclic or bicyclic heterocyclic group, R1 represents a halide, nitro, substituted C1-6 alkyl, optionally substituted amino, C1-6 alkyloxycarbonyl, optionally substituted aryl, a heterocyclic group, or heterocyclic carbonyl, R2 represents a hydrogen atom or C1-6 alkyl, R3 represents C1-6 alkyl, all of R4, R5, and R6 represent a hydrogen atom, R7 represents C1-6 alkyl, m is 1 or 2, and n is 1. The compounds are novel lincomycin derivatives having a potent activity against resistant pneumococci. The compounds can be used as an antimicrobial agent and are useful for preventing or treating bacterial infectious diseases.

    摘要翻译： 本发明提供式（I）化合物或其药理学上可接受的盐或溶剂合物，其中A表示芳基或单环或双环杂环基，R 1表示卤素，硝基，取代的C 1-6烷基，任选取代的氨基，C 1-6烷氧基羰基 ，任选取代的芳基，杂环基或杂环羰基，R 2表示氢原子或C 1-6烷基，R 3表示C 1-6烷基，所有R 4，R 5和R 6表示氢原子，R 7表示C 1-6烷基 ，m为1或2，n为1.该化合物是对耐药性肺炎球菌有强力活性的新型林可霉素衍生物。 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
    3.
    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

    申请人： Yoshinari Wakiyama ,  Kou Kumura ,  Satomi Masaki ,  Kazutaka Ueda ,  Yasuo Sato ,  Chika Kikuchi ,  Eijirou Umemura ,  Yoko Hirai ,  Hiroshi Kondo

    发明人： Yoshinari Wakiyama ,  Kou Kumura ,  Satomi Masaki ,  Kazutaka Ueda ,  Yasuo Sato ,  Chika Kikuchi ,  Eijirou Umemura ,  Yoko Hirai ,  Hiroshi Kondo

    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
    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：US07871982B2

    公开(公告)日：2011-01-18

    申请号：US12086279

    申请日：2006-12-11

    申请人： Eijirou Umemura ,  Yoshinari Wakiyama ,  Kazutaka Ueda ,  Kou Kumura ,  Satomi Masaki ,  Takashi Watanabe ,  Mikio Yamamoto ,  Chizuko Kaji ,  Keiichi Ajito

    发明人： Eijirou Umemura ,  Yoshinari Wakiyama ,  Kazutaka Ueda ,  Kou Kumura ,  Satomi Masaki ,  Takashi Watanabe ,  Mikio Yamamoto ,  Chizuko Kaji ,  Keiichi Ajito

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

    CPC分类号： C07H15/16

    摘要： This invention provides compounds of formula (I) or its pharmacologically acceptable salt or solvate, wherein A represents aryl or a monocyclic or bicyclic heterocyclic group, R1 represents a halide, nitro, substituted C1-6 alkyl, optionally substituted amino, C1-6 alkyloxycarbonyl, optionally substituted aryl, a heterocyclic group, or heterocyclic carbonyl, R2 represents a hydrogen atom or C1-6 alkyl, R3 represents C1-6 alkyl, all of R4, R5, and R6 represent a hydrogen atom, R7 represents C1-6 alkyl, m is 1 or 2, and n is 1. The compounds are novel lincomycin derivatives having a potent activity against resistant pneumococci. The compounds can be used as an antimicrobial agent and are useful for preventing or treating bacterial infectious diseases.

    摘要翻译： 本发明提供式（I）化合物或其药理学上可接受的盐或溶剂合物，其中A表示芳基或单环或双环杂环基，R 1表示卤素，硝基，取代的C 1-6烷基，任选取代的氨基，C 1-6烷氧基羰基 ，任选取代的芳基，杂环基或杂环羰基，R 2表示氢原子或C 1-6烷基，R 3表示C 1-6烷基，所有R 4，R 5和R 6表示氢原子，R 7表示C 1-6烷基 ，m为1或2，n为1.该化合物是对耐药性肺炎球菌有强力活性的新型林可霉素衍生物。 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。

    Cephem derivatives
    5.
    发明授权
    Cephem derivatives 失效
    Cephem衍生物

    公开(公告)号：US06242437B1

    公开(公告)日：2001-06-05

    申请号：US09319437

    申请日：1999-06-07

    申请人： Kazuko Kobayashi ,  Eijirou Umemura ,  Kunio Atsumi ,  Takashi Ida

    发明人： Kazuko Kobayashi ,  Eijirou Umemura ,  Kunio Atsumi ,  Takashi Ida

    IPC分类号： A61K31546

    CPC分类号： C07D519/00

    摘要： A compound represented by the following formula (I) is disclosed. This compound has potent antimicrobial activity against a wide spectrum of bacteria from Gram-positive bacteria to Grame-negative bacteria including &bgr;-lactamase producing bacteria. In particular, it has higher antimicrobial activity against methicilline-resistant Staphylococcus aureus (MRSA), penicillin-resistant Streptococcus pneumoniae (PRSP), and imipenem-resistant Pseudomonas aeruginosa than the existing onium salt type cephem derivatives and hence is very useful as a therapeutic agent for infectious diseases derived from various pathogenic bacteria. wherein X represents CH or N, R1 represents a hydrogen atom, substituted or unsubstituted C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, or cycloalkyl; any one of R2, R3, R4, and R5 represents R6R7NSO2NH—C1-6 alkyl where R6 and R7, which may be the same or different, represent a hydrogen atom or C1-6 alkyl; and n is 0 or 1.

    摘要翻译： 公开了由下式（I）表示的化合物。 该化合物对革兰氏阳性菌对包括β-内酰胺酶生产细菌在内的Grame-negative细菌的广谱细菌具有有效的抗菌活性。 具体而言，与现有的鎓盐型头孢烯衍生物相比，耐甲氧西林金黄色葡萄球菌（MRSA），青霉素耐药性肺炎链球菌（PRSP）和亚胺培南耐药铜绿假单胞菌具有较高的抗菌活性，因此作为治疗剂非常有用 用于衍生自各种病原菌的感染性疾病，其中X表示CH或N，R 1表示氢原子，取代或未取代的C 1-6烷基，C 2-6烯基，C 2-6炔基或环烷基; R2，R3，R4和R5中的任一个表示R6R7NSO2NH-C1-6烷基，其中R6和R7可以相同或不同，表示氢原子或C1-6烷基; n为0或1。

    LINCOMYCIN DERIVATIVES AND ANTIMICROBIAL AGENTS COMPRISING THE SAME AS ACTIVE INGREDIENT
    6.
    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

    申请人： Yoshinari Wakiyama ,  Kou Kumura ,  Satomi Masaki ,  Kazutaka Ueda ,  Yasuo Sato ,  Chika Kikuchi ,  Eijirou Umemura ,  Yoko Hirai ,  Hiroshi Kondo

    发明人： Yoshinari Wakiyama ,  Kou Kumura ,  Satomi Masaki ,  Kazutaka Ueda ,  Yasuo Sato ,  Chika Kikuchi ,  Eijirou Umemura ,  Yoko Hirai ,  Hiroshi Kondo

    IPC分类号： A61K31/7056 ,  C07H15/16 ,  A61P31/04 ,  A61P11/00

    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。