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    1-N-[(S)-.alpha.-hydroxy-.omega.-aminoacyl] derivatives of 3',4'-dideoxykanamycin B and 3'-deoxykanamycin B antibiotics
    1.
    发明授权
    1-N-[(S)-.alpha.-hydroxy-.omega.-aminoacyl] derivatives of 3',4'-dideoxykanamycin B and 3'-deoxykanamycin B antibiotics 失效
    1-N- {8（S） - {6-羟基 - {107-氨基酰基{9 {3的衍生物{40,4 {40-脱氧卡那霉素B和3 {40-脱氧卡那霉素B抗生素

    公开(公告)号：US4107424A

    公开(公告)日：1978-08-15

    申请号：US708076

    申请日：1976-07-23

    申请人： Hamao Umezawa ,  Sumio Umezawa ,  Kenji Maeda ,  Osamu Tsuchiya ,  Shinichi Kondo ,  Shunzo Fukatsu

    发明人： Hamao Umezawa ,  Sumio Umezawa ,  Kenji Maeda ,  Osamu Tsuchiya ,  Shinichi Kondo ,  Shunzo Fukatsu

    IPC分类号： C07H15/224 ,  C07H15/23 ,  C07H15/236 ,  C07H15/22 ,  A61K31/70

    CPC分类号： C07H15/224 ,  C07H15/23 ,  C07H15/234 ,  Y02P20/55

    摘要： A new and useful 1-N-[(S)-.alpha.-hydroxy-.omega.-aminoacyl] derivative of an aminoglycosidic antibiotic, including its deoxy derivative, such as kanamycin B, 3'-deoxyneamine, 3',4'-dideoxyneamine, 3',4'-dideoxyribostamycin or 3',4'-dideoxykanamycin B is now synthetized from the parent substance, aminoglycosidic antiobiotic. The new 1-N-[(S)-.alpha.-hydroxy-.omega.-aminoacyl] derivative shows a wider and/or higher antibacterial activity than the parent substance and is useful in the treatment of infections by gram-negative and gram-positive bacteria, including drug-resistant strains thereof. The preparation of this new derivative may be made by 1-N-acylating the parent aminoglycosidic antibiotic with (S)-.alpha.-hydroxy-.omega.-aminocarboxylic acid with the amino group being protected, and chromatographically separating the acylated products to isolate the desired 1-N-acyl derivative, followed by the removal of the amino-protecting group.

    摘要翻译： 一种新的有用的氨基糖苷类抗生素的1-N - [（S）-α-羟基-ω-氨基酰基]衍生物，包括其脱氧衍生物，如卡那霉素B，3'-脱氧烯胺，3'，4'-二脱氧苯胺， 3'，4'-双脱氧核糖霉素或3'，4'-双脱氧卡那霉素B现在由母体物质氨基糖苷类抗生素合成。 新的1-N - [（S）-α-羟基 - ω-氨基酰基]衍生物显示比母体更广泛和/或更高的抗菌活性，并且可用于治疗革兰氏阴性和革兰氏阳性细菌感染 ，包括其耐药菌株。 这种新衍生物的制备可以通过用（S）-α-羟基 - ω-氨基羧酸与被保护的氨基进行1-N-酰化母体氨基糖苷类抗生素，并将酰化产物色谱分离以分离所需的1 -N-酰基衍生物，然后除去氨基保护基。

    1-N-[(S)-.alpha.-hydroxy-.omega.-aminoacyl]
    2.
    发明授权
    1-N-[(S)-.alpha.-hydroxy-.omega.-aminoacyl] 失效
    1-N - （（S） - ' - 羟基-γ-氨基乙酰胺）UMEZAWA; 哈马

    公开(公告)号：US4001208A

    公开(公告)日：1977-01-04

    申请号：US402085

    申请日：1973-10-01

    申请人： Hamao Umezawa ,  Sumio Umezawa ,  Kenji Maeda ,  Osamu Tsuchiya ,  Shinichi Kondo ,  Shunzo Fukatsu

    发明人： Hamao Umezawa ,  Sumio Umezawa ,  Kenji Maeda ,  Osamu Tsuchiya ,  Shinichi Kondo ,  Shunzo Fukatsu

    IPC分类号： C07H15/224 ,  C07H15/23 ,  C07H15/236

    CPC分类号： C07H15/224 ,  C07H15/23 ,  C07H15/234 ,  Y02P20/55

    摘要： A new and useful 1-N-[(S)-.alpha.-hydroxy-.omega.-aminoacyl]derivative of an aminoglycosidic antiobiotic, including its deoxy derivative, such as kanamycin B, 3'-deoxyneamine, 3',4'-dideoxyneamine, 3',4'-dideoxyribostamycin or 3', 4'-dideoxykanamycin B is now synthetized from the parent substance, aminoglycosidic antibiotic. The new 1-N-[(S)-.alpha.-hydroxy-.omega.-aminoacyl] derivative shows a wider and/or higher antibacterial activity than the parent substance and is useful in the treatment of infections by gram-negative and gram-positive bacteria, including drug-resistant strains thereof. The preparation of this new derivative may be made by 1-N-acylating the parent aminoglycosidic antibiotic with (S)-.alpha.-hydroxy-.omega.-aminocarboxylic acid with the amino group being protected, and chromatographically separating the acylated products to isolate the desired 1-N-acyl derivative, followed by the removal of the amino-protecting group.

    Process for the synthetic production of 3-deoxy derivative of an aminoglycosidic antibiotic
    3.
    发明授权
    Process for the synthetic production of 3-deoxy derivative of an aminoglycosidic antibiotic 失效
    用于合成生产氨基糖苷类抗生素的3-脱氧衍生物的方法

    公开(公告)号：US4060682A

    公开(公告)日：1977-11-29

    申请号：US598379

    申请日：1975-07-23

    申请人： Hamao Umezawa ,  Sumio Umezawa ,  Osamu Tsuchiya ,  Eiichi Akita ,  Takeo Miyazawa ,  Yukio Horiuchi ,  Shunzo Fukatsu

    发明人： Hamao Umezawa ,  Sumio Umezawa ,  Osamu Tsuchiya ,  Eiichi Akita ,  Takeo Miyazawa ,  Yukio Horiuchi ,  Shunzo Fukatsu

    IPC分类号： C07H15/224 ,  B01J25/00 ,  C07B61/00 ,  C07H15/222 ,  C07H15/23 ,  C07H15/234 ,  C07H15/244 ,  A61K31/71 ,  C07H15/22

    CPC分类号： C07H15/222 ,  Y02P20/55

    摘要： 3'-Deoxy derivatives of neamine, 6'-N-alkylneamine, kanamycin B, 6'-N-alkylkanamycin B, ribostamycin, 6'-N-alkylribostamycin and paromamine may be produced by a new process comprising reducing the 3',4'-.alpha.-anhydro derivative (namely, the 3',4'-epoxide derivative) of the aminoglycosidic antibiotics with hydrogen in an alkaline lower alkanol medium containing an alkali metal hydroxide or alkoxide dissolved therein and in the presence of a reducing catalyst such as Raney nickel. The 3',4'-.alpha.-anhydro derivative may be prepared by treating the 3'-sulfonylated derivative of the amino-protected and hydroxyl-protected neamine, 6'-N-alkylneamine, kanamycin B, 6'-N-alkylkanamycin B, ribostamycin, 6'-N-alkylribostamycin or paromamine with an alkali metal hydroxide or alkoxide in a lower alkanol to effect epoxidation between the 4'-hydroxyl group and the carbon atom substituted by the 3'-sulfonic ester group.

    摘要翻译： 神经胺，6'-N-烷基胺，卡那霉素B，6'-N-烷基卡那霉素B，核糖霉素，6'-N-烷基三苯甲酰霉素和帕罗明胺的3'-脱氧衍生物可以通过新的方法制备，包括将3'，4'- 在含有碱金属氢氧化物或醇盐的碱性低级烷醇介质中，在氨基糖苷类抗生素的α-脱氢衍生物（即3'，4'-环氧化物衍生物） 阮内镍 3'，4'-α-脱水衍生物可以通过处理氨基保护的和羟基保护的神经胺，6'-N-烷基胺，卡那霉素B，6'-N-烷基卡那霉素B的3'-磺酰化衍生物 ，核糖霉素，6'-N-烷基三苯甲酰霉素或碱性金属氢氧化物或醇盐在低级链烷醇中进行环氧化，以实现4'-羟基和被3'-磺酸酯基取代的碳原子之间的环氧化。

    Process for the production of 3'-deoxykanamycin A and intermediate product
    6.
    发明授权
    Process for the production of 3'-deoxykanamycin A and intermediate product 失效
    制备3'-脱氧卡那霉素A和中间产物的方法

    公开(公告)号：US4359572A

    公开(公告)日：1982-11-16

    申请号：US256131

    申请日：1981-04-21

    申请人： Hamao Umezawa ,  Sumio Umezawa ,  Shunzo Fukatsu ,  Toshio Yoneta

    发明人： Hamao Umezawa ,  Sumio Umezawa ,  Shunzo Fukatsu ,  Toshio Yoneta

    IPC分类号： C07H15/234 ,  C07H15/236 ,  A61K31/71 ,  C07H15/22

    CPC分类号： C07H15/234 ,  Y02P20/55

    摘要： 3'-Deoxykanamycin A useful as an antibacterial agent can be produced by a new process comprising reacting a 2',2"-di-O-acylated-3'-O-sulfonylated-tetra-N-protected derivative of kanamycin A with a base such as alkali metal alcoholate in a lower alkanol to effect 2',3'- and 3',4'-epoxidation and concurrently removal of the 2'- and 2"-acyl groups, reducing the resultant N-protected 2',3'-anhydro-3'-epi derivative and 3',4'-anhydro-3'-epi derivative of kanamycin A either with hydrogen in the presence of a known hydrogenation catalyst or with sodium borohydride to afford the corresponding N-protected 3'-deoxygenated derivative of kanamycin A and then removing the residual amino-protecting groups therefrom to give 3'-deoxykanamycin A.

    摘要翻译： 可用作抗菌剂的3'-脱氧卡那霉素A可以通过新的方法制备，包括使卡那霉素A的2'，2“ - 二-O-酰化-3'-O-磺酰化四-N-保护的衍生物与 碱如碱金属醇化物在低级链烷醇中进行2'，3'和3'，4'-环氧化并同时去除2'-和2“ - 酰基，将所得N-保护的2 '，3'-脱水-3'-外延衍生物和卡那霉素A的3'，4'-脱氢-3'-epi衍生物，与已知氢化催化剂或硼氢化钠存在下的氢气反应，得到相应的N- 保护的卡那霉素A的3'-脱氧衍生物，然后从其中除去残留的氨基保护基，得到3'-脱氧卡那霉素A.

    3',4'-Episulfido kanamycin B compounds
    7.
    发明授权
    3',4'-Episulfido kanamycin B compounds 失效
    3'，4'-二硫代卡那霉素B化合物

    公开(公告)号：US4195170A

    公开(公告)日：1980-03-25

    申请号：US880401

    申请日：1978-02-23

    申请人： Hamao Umezawa ,  Sumio Umezawa ,  Shigeo Seki ,  Shunzo Fukatsu ,  Shuntaro Yasuda

    发明人： Hamao Umezawa ,  Sumio Umezawa ,  Shigeo Seki ,  Shunzo Fukatsu ,  Shuntaro Yasuda

    IPC分类号： C07H15/236 ,  C07H15/22

    CPC分类号： C07H15/234 ,  Y02P20/55

    摘要： New routes are provided for the synthesis of 3',4'-dideoxykanamycin B which is effective in inhibiting kanamycin-resistant organisms from kanamycin B through new intermediate, of which a fundamental process comprises a new reaction of a 3',4'-epoxy derivative of amino- and hydroxyl-protected kanamycin B with a xanthate to form a corresponding 3',4'-dideoxy-3'-eno derivative followed by removal of the amino- and hydroxyl-protecting groups thereof and by hydrogenation of the resulting 3',4'-dideoxy-3'-eno-kanamycin B. A 3',4'-episulfide derivative corresponding to the 3',4'-epoxy derivative which is formed as second product in the reaction of 3',4'-epoxy derivative with xanthate is also used as intermediate for the preparation of 3',4'-dideoxykanamycin B.

    摘要翻译： 提供了用于合成3'，4'-双脱氧卡那霉素B的新途径，其通过新的中间体有效抑制卡那霉素B的卡那霉素抗性生物，其中基本方法包括3'，4'-环氧基 氨基和羟基保护的卡那霉素B与黄原酸酯的衍生物形成相应的3'，4'-二脱氧-3'-烯衍生物，然后除去其氨基和羟基保护基团，并通过氢化得到的3 '，4'-二脱氧-3'-烯 - 卡那霉素B.对应于3'，4'-环氧衍生物的3'，4'-环硫化物衍生物，其在3'，4' 含有黄原酸酯的环氧衍生物也用作制备3'，4'-双脱氧卡那霉素B的中间体。

    Derivative of kanamycin A and a process for the preparation thereof
    9.
    发明授权
    Derivative of kanamycin A and a process for the preparation thereof 失效
    卡那霉素A的衍生物及其制备方法

    公开(公告)号：US4337336A

    公开(公告)日：1982-06-29

    申请号：US235576

    申请日：1981-02-18

    申请人： Hamao Umezawa ,  Sumio Umezawa ,  Shunzo Fukatsu ,  Toshio Yoneta ,  Tadashi Wakazawa

    发明人： Hamao Umezawa ,  Sumio Umezawa ,  Shunzo Fukatsu ,  Toshio Yoneta ,  Tadashi Wakazawa

    IPC分类号： C07H15/234 ,  C07H15/236 ,  A61K31/71 ,  C07H15/22

    CPC分类号： C07H15/234

    摘要： There are provided new compounds, 3',4'-anhydro-4'-epi derivatives of kanamycin A of the formula: ##STR1## wherein R represents an alkyl, aralkyl or aryl group and Y represents an alkylidene, aralkylidene, cycloalkylidene or tetrahydropyranylidene group which are useful as an intermediate for the synthesis of 3',4'-dideoxykanamycin A and 4'-deoxykanamycin A from kanamycin A. The compounds of formula (I) can be prepared by treating the corresponding 4'-O-sulfonyl derivative with an alkali metal alcoholate in a lower alkanol under an alkaline condition.

    摘要翻译： 提供了下式的卡那霉素A的新化合物3'，4'-脱水-4'-表面衍生物：其中R表示烷基，芳烷基或芳基，Y表示亚烷基，亚烷基， 可用作合成来自卡那霉素A的3'，4'-二脱氧卡那霉素A和4'-脱氧卡那霉素A的中间体的环亚烷基或四氢吡喃亚基。式（I）化合物可以通过将相应的4'- 磺酰基衍生物与碱金属醇化物在低级烷醇中在碱性条件下反应。

    3',4'-Diedeoxykanamycin B derivatives
    10.
    发明授权
    3',4'-Diedeoxykanamycin B derivatives 失效
    3'，4'-脱氧卡那霉素B衍生物

    公开(公告)号：US4357465A

    公开(公告)日：1982-11-02

    申请号：US187014

    申请日：1980-09-15

    申请人： Hamao Umezawa ,  Sumio Umezawa ,  Shigeo Seki ,  Shunzo Fukatsu ,  Shuntaro Yasuda

    发明人： Hamao Umezawa ,  Sumio Umezawa ,  Shigeo Seki ,  Shunzo Fukatsu ,  Shuntaro Yasuda

    IPC分类号： C07H15/236 ,  A61K31/71 ,  C07H15/22

    CPC分类号： C07H15/234 ,  Y02P20/55

    摘要： New routes are provided for the synthesis of 3',4'-dideoxykanamycin B which is effective in inhibiting kanamycin-resistant organisms from kanamycin B through new intermediate, of which a fundamental process comprises a new reaction of a 3',4'-epoxy derivative of amino- and hydroxyl-protected kanamycin B with a xanthate to form a corresponding 3',4'-dideoxy-3'-eno derivative followed by removal of the amino- and hydroxyl-protecting groups thereof and by hydrogenation of the resulting 3',4'-dideoxy-3'-eno-kanamycin B. A 3',4'-episulfide derivative corresponding to the 3',4'-epoxy derivative which is formed as second product in the reaction of 3',4'-epoxy derivative with xanthate is also used as intermediate for the preparation of 3',4'-dideoxykanamycin B.

    摘要翻译： 提供了用于合成3'，4'-双脱氧卡那霉素B的新途径，其通过新的中间体有效抑制卡那霉素B的卡那霉素抗性生物，其中基本方法包括3'，4'-环氧基 氨基和羟基保护的卡那霉素B与黄原酸酯的衍生物形成相应的3'，4'-二脱氧-3'-烯衍生物，然后除去其氨基和羟基保护基团，并通过氢化得到的3 '，4'-二脱氧-3'-烯 - 卡那霉素B.对应于3'，4'-环氧衍生物的3'，4'-环硫化物衍生物，其在3'，4' 含有黄原酸酯的环氧衍生物也用作制备3'，4'-双脱氧卡那霉素B的中间体。