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60 条记录 (耗时 0.023 秒)

    2'-deoxy-2'-epi-2'-fluorocoformycin
    43.
    发明授权
    2'-deoxy-2'-epi-2'-fluorocoformycin 失效
    2'-脱氧-2'-表2-fluorocoformycin

    公开(公告)号：US5886167A

    公开(公告)日：1999-03-23

    申请号：US990461

    申请日：1997-12-15

    申请人： Tomio Takeuchi ,  Sumio Umezawa ,  Tsutomu Tsuchiya ,  Yoshiaki Takahashi

    发明人： Tomio Takeuchi ,  Sumio Umezawa ,  Tsutomu Tsuchiya ,  Yoshiaki Takahashi

    IPC分类号： C07H19/04 ,  C07H19/052 ,  C07H19/16

    CPC分类号： C07H19/04 ,  C07H19/052

    摘要： 2'-Deoxy-2'-fluorocoformycin and 2'-deoxy-8-epi-2'-fluorocoformycin are synthesized in this invention through a multi-stage process via 3,5-di-O-benzoyl-2-deoxy-2-fluoro-.alpha.- and -.beta.-D-ribofuranosyl bromides. Further, according to this invention, 2'-deoxy-2'-epi-2'-fluorocoformycin and 2'-deoxy-8,2'-diepi-2'-fluorocoformycin are synthesized by a multi-stage process starting from 3,5-di-O-benzoyl-2-deoxy-2-fluoro-.alpha.-D-arabinofuranosyl bromide. These four 2'-fluoro derivatives of coformycin are novel compounds and have high enzyme-inhibitory activities against adenosine deaminase. In particular, these novel compounds are useful substances which exhibit therapeutic effects on acute lymphocytic leukemias due to their high enzyme-inhibitory activities above-mentioned. In addition, a variety of intermediates are obtained as novel compounds which are useful for the synthesis of the aforesaid novel 2'-fluoro derivatives of coformycin.

    摘要翻译： 2'-脱氧-2'-氟霉素和2'-脱氧-8-表2-fluorocoformycin在本发明中通过多步法通过3,5-二-O-苯甲酰基-2-脱氧-2 - 氟-α-和-β-D-呋喃核糖基溴。 此外，根据本发明，通过多阶段方法从3制备2'-脱氧-2'-表2-fluorocoformycin和2'-脱氧-8,2'-二哌啶-2'-氟霉素， 5-二-O-苯甲酰基-2-脱氧-2-氟-α-D-阿拉伯呋喃糖基溴。 这四种共转霉素的2'-氟衍生物是新型化合物，对腺苷脱氨酶具有较高的酶抑制活性。 特别地，这些新化合物是由于上述高酶抑制活性而对急性淋巴细胞性白血病具有治疗作用的有用物质。 此外，作为可用于合成上述新型共转霉素2'-氟衍生物的新型化合物，可获得多种中间体。

    Processes for preparing 2'-deoxy-2'-fluorocoformycin and stereoisomers thereof
    44.
    发明授权
    Processes for preparing 2'-deoxy-2'-fluorocoformycin and stereoisomers thereof 失效
    制备2'-脱氧-2'-氟霉素的方法及其立体异构体

    公开(公告)号：US5773607A

    公开(公告)日：1998-06-30

    申请号：US620396

    申请日：1996-03-22

    申请人： Tomio Takeuchi ,  Sumio Umezawa ,  Tsutomu Tsuchiya ,  Yoshiaki Takahashi

    发明人： Tomio Takeuchi ,  Sumio Umezawa ,  Tsutomu Tsuchiya ,  Yoshiaki Takahashi

    IPC分类号： C07H19/04 ,  C07H19/052 ,  C07H1/00 ,  C07H19/00

    CPC分类号： C07H19/04 ,  C07H19/052

    摘要： 2'-Deoxy-2'-fluorocoformycin and 2'-deoxy-8-epi-2'-fluorocoformycin are synthesized in this invention through a multi-stage process via 3,5-di-O-benzoyl-2-deoxy-2-fluoro-.alpha.- and -.beta.-D-ribofuranosyl bromides. Further, according to this invention, 2'-deoxy-2'-epi-2'-fluorocoformycin and 2'-deoxy-8,2'-diepi-2'-fluorocoformycin are synthesized by a multi-stage process starting from 3,5-di-O-benzoyl-2-deoxy-2-fluoro-.alpha.-D-arabinofuranosyl bromide. These four 2'-fluoro derivatives of coformycin are novel compounds and have high enzyme-inhibitory activities against adenosine deaminase. In particular, these novel compounds are useful substances which exhibit therapeutic effects on acute lymphocytic leukemias due to their high enzyme-inhibitory activities above-mentioned. In addition, a variety of intermediates are obtained as novel compounds which are useful for the synthesis of the aforesaid novel 2'-fluoro derivatives of coformycin.

    摘要翻译： 2'-脱氧-2'-氟霉素和2'-脱氧-8-表2-fluorocoformycin在本发明中通过多步法通过3,5-二-O-苯甲酰基-2-脱氧-2 - 氟-α-和-β-D-呋喃核糖基溴。 此外，根据本发明，通过多阶段方法从3制备2'-脱氧-2'-表2-fluorocoformycin和2'-脱氧-8,2'-二哌啶-2'-氟霉素， 5-二-O-苯甲酰基-2-脱氧-2-氟-α-D-阿拉伯呋喃糖基溴。 这四种共转霉素的2'-氟衍生物是新型化合物，对腺苷脱氨酶具有较高的酶抑制活性。 特别地，这些新化合物是由于上述高酶抑制活性而对急性淋巴细胞性白血病具有治疗作用的有用物质。 此外，作为可用于合成上述新型共转霉素2'-氟衍生物的新型化合物，可获得多种中间体。

    Tylosin derivatives
    47.
    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
    48.
    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。