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    1-N-(.alpha.-hydroxy-.omega.-aminoalkanoyl) derivatives of 3'-deoxykanamycin A and the production thereof
    31.
    发明授权
    1-N-(.alpha.-hydroxy-.omega.-aminoalkanoyl) derivatives of 3'-deoxykanamycin A and the production thereof 失效
    3 {40-脱氧卡那霉素A的1-N - （{60-羟基 - {107-氨基烷酰基）衍生物及其制备

    公开(公告)号：US4104372A

    公开(公告)日：1978-08-01

    申请号：US678560

    申请日：1976-04-20

    申请人： Hamao Umezawa ,  Sumio Umezawa ,  Tsutomu Tsuchiya

    发明人： Hamao Umezawa ,  Sumio Umezawa ,  Tsutomu Tsuchiya

    IPC分类号： C07H15/234 ,  A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/7036 ,  A61P31/04 ,  B01J23/00 ,  B01J25/00 ,  C07B61/00 ,  C07H15/236 ,  A61K31/71 ,  C07H15/22

    CPC分类号： C07H15/234 ,  Y02P20/55

    摘要： 1-N-(.alpha.-hydroxy-.omega.-aminoalkanoyl)-derivatives of 3'-deoxykanamycin A or 6'-N-methyl-3'-deoxykanamycin A are provided as new and useful compounds which are active against gram-negative and gram-positive bacteria, including drug-resistant strains of these bacteria. Examples of these compounds include 1-N-((SR)-.beta.-amino-.alpha.-hydroxypropionyl)-3'-deoxykanamycin A, 1-N-((S)-.gamma.-amino-.alpha.-hydroxybutyryl)-3'-deoxykanamycin A, 1-N-((S)-.delta.-amino-.alpha.-hydroxyvaleryl)-3'-deoxykanamycin A and 1-N-((S)-.gamma.-amino-.alpha.-hydroxybutyryl)-6'-N-methyl-3'-deoxykanamycin A. The compounds may be prepared by selective acylation of the 1-amino group of 3'-deoxykanamycin A or 6'-N-methyl-3'-deoxykanamycin A with a corresponding .alpha.-hydroxy-.omega.-amino-alkanoic acid.

    摘要翻译： 提供3'-脱氧卡那霉素A或6'-N-甲基-3'-脱氧卡那霉素A的1-N-（α-羟基 - ω-氨基烷酰基）衍生物作为对革兰氏阴性和革兰氏阴性菌具有活性的新的有用化合物 阳性细菌，包括这些细菌的耐药菌株。 这些化合物的实例包括1-N - （（SR）-β-氨基-α-羟基丙酰基）-3'-脱氧卡那霉素A，1-N - （（S）-γ-氨基-α-羟基丁酰基） 脱氧卡那霉素A，1-N - （（S）-δ-氨基-α-羟基戊酰基）-3'-脱氧卡那霉素A和1 -N（（S）-γ-氨基-α-羟基丁酰基）-6'-N- 甲基-3'-脱氧卡那霉素A.该化合物可以通过将3-脱氧卡那霉素A或6'- N-甲基-3'-脱氧卡那霉素A的1-氨基选择性酰化与相应的α-羟基 - 氨基 - 链烷酸。

    Process for the synthesis of 3',4'-dideoxykanamycin B and products
    34.
    发明授权
    Process for the synthesis of 3',4'-dideoxykanamycin B and products 失效
    合成3 {40,4（40-脱氧卡那霉素B和产物）的方法

    公开(公告)号：US4156078A

    公开(公告)日：1979-05-22

    申请号：US745015

    申请日：1976-11-26

    申请人： Hamao Umezawa ,  Sumio Umezawa ,  Tsutomu Tsuchiya

    发明人： Hamao Umezawa ,  Sumio Umezawa ,  Tsutomu Tsuchiya

    IPC分类号： C07H15/234 ,  B01J23/00 ,  B01J25/00 ,  C07B61/00 ,  C07H15/236 ,  C07H15/22

    CPC分类号： C07H15/234 ,  Y02P20/55

    摘要： A useful antibiotic, 3',4'-dideoxykanamycin B can be prepared in shortened steps and in an improved overall yield by a new process starting from kanamycin B via new intermediate derivatives of kanamycin B in which all the amino groups and possibly the 2"-hydroxyl group are protected with sulfonyl-type protecting groups selected from lower alkyl-, aryl- and aralkyl-sulfonyl groups.

    摘要翻译： 一种有用的抗生素，3'，4'-双脱氧卡那霉素B可以通过新的卡那霉素B通过卡那霉素B的新中间体衍生物从卡那霉素B开始的新方法以缩短的步骤和总产率提高，其中所有氨基和可能的2' ' - 羟基被选自低级烷基 - ，芳基 - 和芳烷基 - 磺酰基的磺酰基型保护基保护。

    Processes for the production of 3'-deoxykanamycin A and intermediates
    35.
    发明授权
    Processes for the production of 3'-deoxykanamycin A and intermediates 失效
    制备3'-脱氧卡那霉素A和中间体的方法

    公开(公告)号：US4357466A

    公开(公告)日：1982-11-02

    申请号：US198612

    申请日：1980-10-20

    申请人： Hamao Umezawa ,  Sumio Umezawa ,  Tsutomu Tsuchiya ,  Tomo Jikihara

    发明人： Hamao Umezawa ,  Sumio Umezawa ,  Tsutomu Tsuchiya ,  Tomo Jikihara

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

    CPC分类号： C07H15/234

    摘要： 3'-Deoxykanamycin A useful as antibacterial agent is produced from a protected kanamycin A derivative either by a process comprising imidazolylthiocarbonylation of the 3'- and 2"-hydroxyl groups of 4",6"-O-cyclohexylidene-4'-0:6'-N-carbonyl-5,2'-O-isopropylidene-1,3,3"-tri-N-tosylkanamycin A, preferential removal of the 3'-imidazolylthiocarbonyloxy group with tributyltin hydride for the 3'-deoxygenation, followed by removal of the 2"-O-imidazolylthiocarbonyl group with aqueous ammonia, removal of the N-tosyl groups with alkali or alkaline earth metal in liquid ammonia, hydrolytic fission of the 4',6'-cyclic carbamate ring and concurrent removal of the 5,2'-O-isopropylidene group and 4",6"-O-cyclohexylidene group, or by a process comprising selective acetylation of the 2"-hydroxyl group of said protected kanamycin A derivative with acetyl chloride in pyridine, trifluoromethanesulfonylation of the 3'-hydroxyl group, followed by concurrent removal of the 3'-trifluoromethanesulfonyloxy group and N-tosyl groups with alkali metal in liquid ammonia, removal of the 2"-O-acetyl group concurrently with hydrolytic fission of 4',6'-cyclic carbamate, and hydrolytic removal of the 5,2'-O-isopropylidene and 4",6"-O-cyclohexylidene groups.

    摘要翻译： 可用作抗菌剂的3'-脱氧卡那霉素A由受保护的卡那霉素A衍生物制备，其通过包含4'，6“-O-亚环己基-4'的3'和2” - 羟基的咪唑基硫代羰基化的方法制备， -0：6'-N-羰基-5,2'-O-异亚丙基-1,3,3“ - 三-N-甲苯磺酰基卡那霉素A，优选用三丁基氢化锡将3'-咪唑硫基羰基氧基除去3' 脱氧，然后用氨水除去2“-O-咪唑基硫代羰基，在液氨中用碱金属或碱土金属除去N-甲苯磺酰基，4'，6'-环状氨基甲酸酯环的水解裂变 并且同时去除5,2'-O-异亚丙基和4“，6”-O-亚环己基，或通过包括将所述受保护的卡那霉素A衍生物的2'-羟基选择性乙酰化的方法与 吡啶中的乙酰氯，3'-羟基的三氟甲磺酰化，然后同时除去3'-三氟甲磺酸 氧基和N-甲苯磺酰基与液氨中的碱金属反应，与4'，6'-环状氨基甲酸酯的水解裂解同时除去2'-乙酰基，并除去5,2'-O 异亚丙基和4“，6”-O-亚环己基。

    Tylosin derivatives
    37.
    发明授权
    Tylosin derivatives 失效
    泰乐菌素衍生物

    公开(公告)号：US4438109A

    公开(公告)日：1984-03-20

    申请号：US285747

    申请日：1981-07-22

    申请人： Hamao Umezawa ,  Sumio Umezawa ,  Tsutomu Tsuchiya ,  Akihiro Tanaka

    发明人： Hamao Umezawa ,  Sumio Umezawa ,  Tsutomu Tsuchiya ,  Akihiro Tanaka

    IPC分类号： C07H17/08 ,  A61K31/70

    CPC分类号： C07H17/08

    摘要： Tylosin derivatives shown by the general formula ##STR1## wherein R represents a hydrogen atom or a hydroxyl group; R.sub.1 represents a halogen atom, a hydroxyl group, a tetrahydrofuranyloxy group, a tetrahydropyranyloxy group, a tetrahydrothiofuranyloxy group, a tetrahydrothiopyranyloxy group, an alkanoyloxy group, an arylcarbonyloxy group, an aralkylcarbonyloxy group, a lower alkylthiomethyloxy group, a heterocyclic thio group which may have a substituent, a mono- or di- lower alkylamino lower alkylthio group or a group of ##STR2## (wherein R.sub.4 represents a hydroxyl group or an alkanoyloxy group); R.sub.2 represents a hydrogen atom, a hydroxyl group, or an alkanoyloxy group; R.sub.3 represents a hydroxyl group or an alkanoyloxy group; and represents a single bond or a double bond, but represents a double bond when R.sub.2 is a hydrogen atom.These compounds are useful as antibiotics.

    摘要翻译： 由通式表示的泰乐菌素衍生物，其中R表示氢原子或羟基; R 1表示卤素原子，羟基，四氢呋喃氧基，四氢吡喃氧基，四氢噻喃氧基，四氢噻喃氧基，烷酰氧基，芳基羰基氧基，芳烷基羰基氧基，低级烷基硫代甲氧基，可具有的杂环硫基 取代基，单 - 或二 - 低级烷基氨基低级烷硫基或一组（其中R 4表示羟基或烷酰氧基）。 R2表示氢原子，羟基或烷酰氧基; R3表示羟基或烷酰氧基; 并且表示单键或双键，但当R 2为氢原子时，表示双键。 这些化合物可用作抗生素。

    3',4'-Dideoxykanamycin A and 1-N-(S)-.alpha.-hydroxy-.omega.-aminoalkanoyl) derivatives thereof
    38.
    发明授权
    3',4'-Dideoxykanamycin A and 1-N-(S)-.alpha.-hydroxy-.omega.-aminoalkanoyl) derivatives thereof 失效
    3'，4'-双脱氧卡那霉素A和1-N-（S）-α-羟基-ω-氨基烷酰基）衍生物

    公开(公告)号：US4298727A

    公开(公告)日：1981-11-03

    申请号：US114779

    申请日：1980-01-23

    申请人： Hamao Umezawa ,  Sumio Umezawa ,  Tsutomu Tsuchiya ,  Tomo Jikahara ,  Toshiaki Miyake

    发明人： Hamao Umezawa ,  Sumio Umezawa ,  Tsutomu Tsuchiya ,  Tomo Jikahara ,  Toshiaki Miyake

    IPC分类号： C07H15/234 ,  A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/7036 ,  A61P31/04 ,  C07H15/236 ,  C07H15/22

    CPC分类号： C07H15/234 ,  Y02P20/55

    摘要： 3',4'-Dideoxy derivative and 1-N-((S)-.alpha.-hydroxy-.omega.-aminoalkanoyl)-3',4'-dideoxy derivative of kanamycin A are now synthetized from kanamycin A and show a wider and/or higher antibacterial activity than the parent kanamycin A so that they are useful in therapeutic treatment of infections by gram-negative and gram-positive bacteria, including drug-resistant strains thereof. The production of these new derivatives may be made by preparing a protected kanamycin A derivative having its 3'- and 4'-hydroxyl groups unprotected and having its all or substantially all other functional groups protected from the initial material, kanamycin A, sulfonylating the 3'- and 4'-hydroxyl groups, removing the 3'- and 4'-sulfonyloxy groups from the resulting 3',4'-di-sulfonic acid ester product to give a 3'-eno-kanamycin A derivative, hydrogenating the 3'-eno-kanamycin A derivative to saturate the 3',4'-unsaturated bond and to yield a protected 3',4'-dideoxykanamycin A product, followed by removal of the remainiing protective groups, and optionally further followed by 1-N-acylation of the 1-amino group of the resulting 3',4'-dideoxykanamycin A with an (S)-.alpha.-hydroxy-.omega.-aminoalkanoic acid or its reactive equivalent.

    摘要翻译： 卡那霉素A的3'，4'-二脱氧衍生物和1-N - （（S）-α-羟基-ω-氨基烷酰基）-3'，4'-二脱氧衍生物现在从卡那霉素A合成并显示出更宽和/ 或更高的抗菌活性，使得它们可用于革兰氏阴性和革兰氏阳性细菌（包括其耐药菌株）的感染的治疗性治疗。 这些新衍生物的生产可以通过制备其未被保护的3'和4'-羟基的保护的卡那霉素A衍生物和其全部或基本上所有其它保护起始材料的卡那霉素A的其他官能团来制备，磺酰化3 '和4'-羟基，从所得的3'，4'-二磺酸酯产物中除去3'-和4'-磺酰氧基，得到3'-烯 - 卡那霉素A衍生物，将3 ' - 卡那霉素A衍生物使3'，4'-不饱和键饱和并产生受保护的3'，4'-二脱氧卡那霉素A产物，然后除去剩余的保护基，并且任选地进一步加入1-N 所得的3'，4'-二脱氧卡那霉素A的1-氨基酸与（S）-α-羟基-ω-氨基链烷酸或其反应性等同物的酰基化。