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    Substances having antibiotic activity, processes for their preparation, pharmaceutical compositions containing them, their use in medicaments and microorganisms
    4.
    发明公开
    Substances having antibiotic activity, processes for their preparation, pharmaceutical compositions containing them, their use in medicaments and microorganisms 失效
    具有物质的抗菌活性，它们的制备方法，药物组合物含有它们，它们在医药和微生物的用途。

    公开(公告)号：EP0029309A1

    公开(公告)日：1981-05-27

    申请号：EP80303807.4

    申请日：1980-10-27

    申请人： KYOWA HAKKO KOGYO CO., LTD

    发明人： Tomita, Fusao ,  Tamaoki, Tatsuya ,  Shirahata, Kunikatsu ,  Iida, Takao ,  Morimoto, Makoto ,  Fujimoto, Kazuhisa

    IPC分类号： A61K35/66 ,  C12P1/06 ,  C07G11/00

    CPC分类号： C12R1/465 ,  C12P1/06

    摘要： Substances having respectively an elemental analysis of C:55.11%; H:5.74%, a molecular weight of 864-958 a melting point of 180±3°C (decomp); an elemental analysis of C:54.20%; H:6.15%, a molecular weight of 826-1004 and a melting point of 193-194°C (decomp); and an elemental analysis of C:54.34%, H:6.03%, a molecular weight of 822-960 and a melting point of 181-182°C (decomp), have been found to possess antibiotic activity. These substances have been prepared by culturing microorganisms of the genus Streptomyces. A preferred strain is Streptomyces ochraceus DC-45 (FERM-P No. 5219 NRRL 12051). The substances have a pale yellowish colour, have activity against Bacillus subtilis No. 10707 and are soluble in methanol, ethanol and chloroform and insoluble in n-hexane. These substances are of potential interest as medicaments for use against bacteria such as Bacillus subtilis No.10707 and for use as anti-tumour agents.

    摘要翻译： 分别具有C个的元素分析的物质：55.11％; H：5.74％，的864-958的180 +/- 3℃（分解）的熔点的分子量; 的的C元素分析：54.20％; H：6.15％，826的分子量为1004和193-194℃（分解）的熔点 和至C的元素分析：54.34％，H：6.03％，的一个822-960分子量和181-182℃（分解）的熔点，已被发现具有抗菌活性。 这些物质已经制备通过培养链霉菌属的微生物。 优选的菌株是链霉菌赭DC-45（FERM-P 5219号NRRL 12051）。 该物质具有浅黄色颜色，具有对抗枯草芽孢杆菌活动号 10707和可溶于甲醇，乙醇和氯仿，不溶于正己烷。 这些物质是潜在的利益作为药物用于对抗细菌的使用：如枯草芽孢杆菌号 10707和用作抗肿瘤剂。

    7-n-aminomethylenemitomycin derivatives, process for production thereof and anti-tumor composition
    6.
    发明公开
    7-n-aminomethylenemitomycin derivatives, process for production thereof and anti-tumor composition 失效
    7-N-氨基亚甲基螺旋霉素，Verfahren zu ihrer Herstellung und Antitumorzubereitung。

    公开(公告)号：EP0191375A2

    公开(公告)日：1986-08-20

    申请号：EP86101214.4

    申请日：1986-01-30

    申请人： KYOWA HAKKO KOGYO CO., LTD.

    发明人： Shirahata, Kunikatsu ,  Kono, Motomichi ,  Kasai, Masaji ,  Ashizawa, Tadashi

    IPC分类号： C07D487/14 ,  A61K31/40

    CPC分类号： C07D487/14

    摘要： Mitomycin derivatives represented by the formula (I):

    wherein R 1 and R 2 may be the same or different, and represent a hydrogen atom or a lower alkyl group: R 3 and R 4 mean that when R 3 is a hydrogen atom, R 4 represents -CH 2 0CONH 2 or

    (wherein R 1 and R 2 have the same significances as defined above), or R 3 and R 4 are combined to form =CH 2 ; Y and Z may be the same or different, and represent a hydrogen atom for a methyl group; represents a- or β-bond, provided that
    Y represents a hydrogen atom when R 4 takes β-conflguration, have an excellent antitumor activity.

    摘要翻译： 由式（I）表示的丝裂霉素衍生物：其中R 1和R 2可以相同或不同，表示氢原子或低级烷基; R 3和R 4表示当R 3是氢原子时，R 4表示-CH 2 OCONH 2或者其中R 1和R 2具有与上述相同的含义，或者R 3和R 4组合形成= CH 2; Y和Z可以相同或不同，表示氢原子或甲基; 表示α或β键，条件是当R4取β构型时，Y表示氢原子，具有优异的抗肿瘤活性。

    Antibiotic compounds, pharmaceutical compositions containing such compounds, process for production thereof
    8.
    发明公开
    Antibiotic compounds, pharmaceutical compositions containing such compounds, process for production thereof 失效
    抗生素化合物，它们的药物组合物和它们的制备方法。

    公开(公告)号：EP0042172A1

    公开(公告)日：1981-12-23

    申请号：EP81104619.2

    申请日：1981-06-15

    申请人： KYOWA HAKKO KOGYO CO., LTD

    发明人： Tomita, Fusao ,  Tamaoki, Tatsuya ,  Shirahata, Kunikatsu ,  Kasai, Masaji ,  Hirayama, Noriaki ,  Morimoto, Makoto ,  Fukui, Masanori

    IPC分类号： C07D407/12 ,  C12P17/16 ,  C12P19/60 ,  C07H17/04 ,  A61K31/365

    CPC分类号： C07H17/08 ,  C07D307/60 ,  C07H15/26 ,  C12P17/162 ,  C12P19/60 ,  C12R1/30

    摘要： Antibacterial tetronolide compounds F-1 and F-2 are produced by fermentation of a microorganism belonging to the genus Micromonospora. The antibiotics F-1 and F-2 are accumulated in the culture liquor and are isolated therefrom, respectively. The acyl derivatives of F-1 and F-2, that is F-1-21-0 acetate, F-1-21-0 propionate, F-1-21-0-n butylate, F-1 diacetate, F-1 dipropionate, F-2 triacetate, F-2 tripropionate and F-2 tri-n-butylate, etc., are chemically synthesized from F-1 and F-2, respectively (Fig. 1).
    Their formula :
    wherein R 1 and R 2 may be the same or different substituents and represent a hydrogen atom or an acyl group and R 3 represents a hydrogen atom, an acyl group or a tetronitrose represented by the formula (2)
    and the pharmaceutically acceptable salts thereof.

    摘要翻译： Antibacteriai tetronolide化合物F-1和F-2是由属于埃希孢微生物的发酵生产。 抗生素的F-1和F-2被累积在培养液和从分别分离在那里。 F-1和F-2的酰基衍生物F-确实是1-21-0乙酸，丙酸F-1-21-0，1-21-0 F-Ñ丁醇，F-1二乙酸，F- 1个二丙酸酯，F-2三乙酸酯，F-2和F-2三丙三正丁醇等，从化学F-1和F-2分别合成。 ... 他们的公式：... ...

    New mitomycins and processes for production thereof
    9.
    发明公开
    New mitomycins and processes for production thereof 失效
    丝裂霉素和Verfahren zu ihrer Herstellung。

    公开(公告)号：EP0008021A1

    公开(公告)日：1980-02-20

    申请号：EP79102497.9

    申请日：1979-07-17

    申请人： KYOWA HAKKO KOGYO CO., LTD

    发明人： Kasai, Masaji ,  Kono, Motomichi ,  Shirahata, Kunikatsu ,  Urakawa, Chikahiro ,  Tsuchiya, Haruko ,  Nakano, Kinichi ,  Takahashi, Itaru ,  Mineura, Kazuyuki

    IPC分类号： C07D487/14 ,  C12P17/18

    CPC分类号： C07D487/14 ,  A01N43/90 ,  C12P17/182 ,  C12R1/465

    摘要： New mitomycins and processes for production thereof.
    Mytomycin represented by general formula:
    Wherein X is amino, substituted amino, hydroxyl or alkoxy; Y is hydrogen, methyl, -COR' wherein R' is hydrogen, alkyl, substituted alkyl, aryl or substituted aryl, or -CH 2 CH 2 Z wherein Z is alkyloxycarbonyl, acyl or cyano; R A is hydrogen and R B is -CH 2 OH or -CH 2 OSO 2 R 2 wherein R 2 is alkyl or aryl, or R A and R B combine to form = CH 2 ; and Rc is hydrogen or alkyl. In spite of the above definition, when R A is hydrogen and R B is -CH 2 OH, Y is -CH 2 CH 2 Z and when R A is hydrogen and R B is -CH 2 OSO 2 R 2 , Y is hydrogen or -CH 2 CH 2 Z, and processes for production thereof.
    The compounds are useful for sterilization of equipment, as washing agent with detergent or as medicament.

    摘要翻译： 新的丝裂霉素及其生产方法。 由通式表示的霉菌素：其中X为氨基，取代氨基，羟基或烷氧基; Y是氢，甲基，-COR 1，其中R 1是氢，烷基，取代的烷基，芳基或取代的芳基或-CH 2 CH 2 Z，其中Z是烷氧基羰基，酰基或氰基; RA是氢，RB是-CH 2 OH或-CH 2 OSO 2 R 2，其中R 2是烷基或芳基，或RA和RB结合形成= CH 2; 和RC是氢或烷基。 尽管上述定义，当RA为氢且RB为-CH2OH时，Y为-CH2CH2Z，当RA为氢，RB为-CH2OSO2R2时，Y为氢或-CH2CH2Z，其制备方法为。 该化合物可用于灭菌设备，作为洗涤剂与洗涤剂或作为药物。

    7-n,8-n-ethylenemitomycin 8-imines, pharmaceutical compositions and use
    10.
    发明公开
    7-n,8-n-ethylenemitomycin 8-imines, pharmaceutical compositions and use 失效
    7-N，8-N-乙基美丝霉素-8-亚胺，药物Zubereitungen和Verwendung。

    公开(公告)号：EP0287855A2

    公开(公告)日：1988-10-26

    申请号：EP88105055.3

    申请日：1988-03-29

    申请人： KYOWA HAKKO KOGYO CO., LTD.

    发明人： Saito, Yutaka ,  Kasai, Masaji ,  Shirahata, Kunikatsu ,  Kono, Motomichi ,  Morimoto, Makoto ,  Ashizawa, Tadashi

    IPC分类号： C07D487/22 ,  A61K31/495

    CPC分类号： C07D487/22

    摘要： 7-N,8-N-ethylenemitomycin 8-imines represented by the formula
    wherein one of R₁ and R₂ represents carbamoyloxymethyl and another represents hydrogen or both are combined together to form methylene; R₃, R₄, R₅ and R₆ each independently represent hydrogen or C₁₋₄ alkyl, or R₃ and R₄ may be combined together to represent -(CH₂) n -, wherein n is 3 or 4; and Y and Z represent hydrogen or methyl, provided that when R₁ represents carbamoyloxymethyl and Y represents methyl, R₂, R₃, R₄, R₅, R₆ and Z are not hydrogen simultaneously, has an excellent antitumor activity.

    摘要翻译： 由式表示的7-N，8-N-亚乙基霉素8-亚胺，其中R 1和R 2之一表示氨基甲酰氧基甲基，另一个表示氢或两者结合在一起形成亚甲基; R 3，R 4，R 5和R 6各自独立地表示氢或C 1-4烷基，或者R 3和R 4可以组合在一起表示 - （CH 2）n - ，其中n为3或4; 并且Y和Z表示氢或甲基，条件是当R 1表示氨基甲酰氧基甲基且Y表示甲基时，R 2，R 3，R 4，R 5，R 6和Z不同时为氢，具有优异的抗肿瘤活性。