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    4'-Epi-6'-hydroxyadriamycin and method of use
    4.
    发明授权
    4'-Epi-6'-hydroxyadriamycin and method of use 失效
    4 {40-Epi-6 {40-羟基阿霉素及其使用方法

    公开(公告)号：US4025623A

    公开(公告)日：1977-05-24

    申请号：US621582

    申请日：1975-10-10

    申请人： Federico Arcamone ,  Alberto Bargiotti ,  Giuseppe Cassinelli ,  Aurelio DIMarco

    发明人： Federico Arcamone ,  Alberto Bargiotti ,  Giuseppe Cassinelli ,  Aurelio DIMarco

    IPC分类号： C07H15/24 ,  A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/704 ,  A61P35/00 ,  C07D309/30 ,  C07H15/252 ,  A61K31/71

    CPC分类号： C07H15/252 ,  C07D309/30 ,  Y02P20/55 ,  Y10S514/908

    摘要： The novel glycoside antibiotic: 4'-epi-6'-hydroxydaunomycin is prepared by condensing daunomycin with a novel protected, reactive derivative, which is 1,2,3-trideoxy-4,6-di-O-(p-nitrobenzoyl)-3-trifluoroacetamido-L-arabino-hex-1-enepyranose and thereafter removing the protecting groups. A further novel glycoside antibiotic: 4'-epi-6'-hydroxyadriamycin is prepared by reacting 4'-epi-6'-hydroxydaunomycin with bromine to form an intermediate bromo derivative which is then mildly hydrolyzed to form 4'-epi-6'-hydroxyadriamycin. These novel glycoside antibiotics, while not as effective as the parent compounds daunomycin and adriamycin in the treatment of tumors, are considerably less toxic than the parent compounds.

    摘要翻译： 新型糖苷抗生素：4'-表 - 6'-羟基多柔比星霉素通过将道诺霉素与新型受保护的活性衍生物（其为1,2,3-三脱氧-4,6-二-O-（对硝基苯甲酰基） -3-三氟乙酰氨基-L-阿拉伯邻 - 己-1-烯并吡喃并除去保护基。 另外新的糖苷抗生素：4'-epi-6'-羟基阿霉素是通过使4'-表 - 6'-羟基天然霉素与溴反应形成一种中间体溴衍生物，然后轻度水解形成4'-表 - 6' - 羟基阿霉素。 这些新型糖苷类抗生素虽然不如母体化合物道诺霉素和阿霉素在治疗肿瘤方面效果好，但比母体化合物毒性好。

    Antitumor glycosides, their preparation and use
    5.
    发明授权
    Antitumor glycosides, their preparation and use 失效
    抗肿瘤糖苷，其制备及用途

    公开(公告)号：US4276289A

    公开(公告)日：1981-06-30

    申请号：US131035

    申请日：1980-03-17

    申请人： Giuseppe Cassinelli ,  Daniela Ruggieri ,  Federico Arcamone ,  Aurelio di Marco

    发明人： Giuseppe Cassinelli ,  Daniela Ruggieri ,  Federico Arcamone ,  Aurelio di Marco

    IPC分类号： A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/704 ,  A61P35/00 ,  C07H15/252 ,  C07H15/24

    CPC分类号： C07H15/252

    摘要： Anthracycline glycosides of the formula I ##STR1## wherein R is hydrogen or hydroxyl and the hydrochlorides thereof, and which are useful in treating certain mammalian tumors, are prepared by condensing daunomycinone with the novel sugar, 4-O-methyl-2,3,6-trideoxy-3trifluoroacetamidoribohexopyranosyl chloride in an inert organic solvent and in the presence of a soluble silver salt and a dehydrating agent to form 3', 4' -diepi-4'-O-methyl-N-trifluoroacetyl daunorubicin, and removing the N-trifluoroacetyl group therefrom. This gives the compound wherein R is hydrogen. The former is converted to the corresponding hydroxyl compound by conventional means.

    摘要翻译： 通过将道诺霉素酮与新的糖4-O-甲基-2,3,3-四氢呋喃缩合来制备其中R为氢或羟基的式I的蒽环酸苷及其盐酸盐，其可用于治疗某些哺乳动物肿瘤 ，6-三脱氧-3-三氟乙酰胺六溴代吡喃葡萄糖氯化物在惰性有机溶剂中，在可溶性银盐和脱水剂存在下反应形成3'，4'-二甲基-4'-O-甲基-N-三氟乙酰柔红霉素，并除去 N-三氟乙酰基。 这得到其中R是氢的化合物。 前者通过常规方法转化成相应的羟基化合物。

    L-lyxohex-1-enopyranose derivative
    7.
    发明授权
    L-lyxohex-1-enopyranose derivative 失效
    L-赖索昔-1-吡喃葡萄糖衍生物

    公开(公告)号：US4020270A

    公开(公告)日：1977-04-26

    申请号：US650519

    申请日：1976-01-19

    申请人： Federico Arcamone ,  Giuseppe Cassinelli

    发明人： Federico Arcamone ,  Giuseppe Cassinelli

    IPC分类号： C07D309/30 ,  C07H15/252 ,  C07H5/06

    CPC分类号： C07H15/252 ,  C07D309/30 ,  Y02P20/55

    摘要： Anthracyclinone glycoside antibiotics including the known antibiotics daunomycin and adriamycin, as well as other, novel glycoside antibiotics of the formula (VIII): ##STR1## wherein WHEN R.sub.1 is hydrogen, R.sub.2 and R.sub.3 are each independently hydrogen, methyl, methoxy, chloro, or bromo; and when R.sub.2 and R.sub.3 are hydrogen, R.sub.1 is methyl, chloro, or bromo and R.sub.4 and R.sub.5 are each independently hydrogen or hydroxy are prepared by an acid catalyzed addition reaction between (a) an anthracyclinone compound of the formula ##STR2## or a dioxolanyl protected derivative thereof (VI) having the formula: ##STR3## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as defined above, and R.sub.6, R.sub.7 and R.sub.8 are independently selected from the group consisting of hydrogen and C.sub.1 -C.sub.4 alkyl; or R.sub.7 and R.sub.8, together with the carbon atom to which they are bound may form a saturated or unsaturated ring of 3-8 carbon atoms and (b) a novel reactive, protected 1,2-unsaturated pyranoid sugar, preferably, 1,2,3,6-tetradeoxy-3-trifluoroacetamido-4-trifluoroacetoxy-L-lyxo-hex-1-enopyranose which forms protected derivatives of said glycoside antibiotics and then removing the protecting groups from said glycoside antibiotics. These antibiotics are useful in the treatment of various human cancers and leukemia such as sarcomas, breast cancer, bronchogenic carcinoma, malignant lymphomas, neuroblastomas, acute leukemia and bladder cancer.

    摘要翻译： 蒽环类抗生素包括已知的抗生素道诺霉素和阿霉素，以及其它式（VIII）的新型糖苷抗生素：其中当R1是氢时，R2和R3各自独立地是氢，甲基，甲氧基， 氯或溴; 并且当R 2和R 3为氢时，R 1为甲基，氯或溴，并且R 4和R 5各自独立地为氢或羟基，是通过（a）式（III）的蒽环类化合物之间的酸催化加成反应制备的， 或其具有下式的二氧杂环戊烷基保护的衍生物（VI）：其中R 1，R 2，R 3，R 4和R 5如上所定义，并且R 6，R 7和R 8独立地选自氢 和C 1 -C 4烷基; 或R 7和R 8与它们所连接的碳原子一起可以形成3-8个碳原子的饱和或不饱和的环，和（b）新的反应性保护的1,2-不饱和吡喃糖，优选1,2 ，3,6-四脱氧-3-三氟乙酰氨基-4-三氟乙酰氧基-L-赖摩尔 - 己-1-吡喃糖，其形成所述糖苷抗生素的受保护的衍生物，然后从所述糖苷抗生素中除去保护基团。 这些抗生素可用于治疗各种人类癌症和白血病如肉瘤，乳腺癌，支气管癌，恶性淋巴瘤，神经母细胞瘤，急性白血病和膀胱癌。

    Paromomycin containing compounds and method of use
    8.
    发明授权
    Paromomycin containing compounds and method of use 失效
    含有溴霉素的化合物及其使用方法

    公开(公告)号：US4337248A

    公开(公告)日：1982-06-29

    申请号：US156478

    申请日：1980-06-04

    申请人： Carlo Battistini ,  Giuseppe Cassinelli ,  Giovanni Franceschi ,  Rosanna Mazzoleni ,  Federico Arcamone

    发明人： Carlo Battistini ,  Giuseppe Cassinelli ,  Giovanni Franceschi ,  Rosanna Mazzoleni ,  Federico Arcamone

    IPC分类号： C07H5/06 ,  A61K31/70 ,  A61K31/702 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/7036 ,  A61P31/04 ,  C07H15/232 ,  A61K31/71 ,  C07H15/22

    CPC分类号： C07H15/232

    摘要： Compounds are disclosed of the formula ##STR1## wherein R.sub.1 represents a hydrogen or chlorine atom, as well as intermediates. These include 4'-deoxy-paromomycin; 4'-deoxy-4'-epi-chloro-paromomycin; 4'-deoxy-4'-epi-chloro-penta-N-benzyloxycarbonylparomomycin; 4'-deoxy-penta-N-benzyloxycarbonylparomomycin; 6,3',2",5",3"',4"'-hexa-O-acetyl-6'-O-benzoyl-4'-deoxy-penta-N-benzyloxycarbonylparomomycin; 6,3',2",5",3"',4"'-hexa-O-acetyl-6'-O-benzoyl-4'-epi-chloro-4'-deoxy-penta-N-benzyloxycarbonylparomomycin; 6,3',2",5",3"',4"'-hexa-O-acetyl-6'-O-benzyl-penta-N-benzyloxycarbonylparomomycin; 6,3',2",5",3"',4"'-hexa-O-acetyl-6'-O-benzoyl-4'-O-[(methylthio)-thiocarbonyl]-penta-N-benzyloxycarbonylparomomycin; and 6,3',2",5",3"',4"'-hexa-O-acetyl-6'-O-benzoyl-4'-O-[(phenylthio)-thiocarbonyl]-penta-N-benzyloxycarbonylparomomycin. The compounds illustrated by the structural formula are useful in treating amoebic dysentery in man and animals.

    摘要翻译： 公开了下式的化合物：其中R 1表示氢或氯原子，以及中间体。 这些包括4'-脱氧巴马霉素; 4'-脱氧-4'-表 - 氯 - 巴龙霉素; 4'-脱氧-4'-表 - 氯 - 五-N-苄氧羰基巴霉素; 4'-脱氧 - 五-N-苄氧羰基巴霉素; 6,3'，2“，5”，3“，4”' - 六-O-乙酰基-6'-O-苯甲酰基-4'-脱氧-5-N-苄氧基羰基巴霉素; 6,3'，2“，5”，3“，4” - 六-O-乙酰基-6'-O-苯甲酰基-4'-表氯 - 4'-脱甲基 - 五 -N-苄氧羰基巴霉素; 6,3'，2“，5”，3“，4”' - 六-O-乙酰基-6'-O-苄基 - 五-N-苄氧基氨基辛基巴霉素; 6,3'，2“，5”，3“，4” - 六-O-乙酰基-6'-O-苯甲酰基-4'-O - [（甲硫基） - 噻吩基] 五-N-苄氧羰基巴霉素; 和6,3'，2“，5”，3“，4” - 六-O-乙酰基-6'-O-苯甲酰基-4'-O - [（苯硫基） - 噻吩基] - 五-N-苄氧羰基巴霉素。 由结构式表示的化合物可用于治疗人和动物中的阿米巴痢疾。

    Pentofuranosyl anthracyclines, intermediates in and method for their preparation and compositions and use thereof
    9.
    发明授权
    Pentofuranosyl anthracyclines, intermediates in and method for their preparation and compositions and use thereof 失效
    戊糖醛酸蒽环类抗生素，其中间体及其制备方法及其组合物和用途

    公开(公告)号：US4254110A

    公开(公告)日：1981-03-03

    申请号：US115725

    申请日：1980-01-28

    申请人： Giuseppe Cassinelli ,  Federico Arcamone ,  Aurelio di Marco

    发明人： Giuseppe Cassinelli ,  Federico Arcamone ,  Aurelio di Marco

    IPC分类号： C07D307/20 ,  A61K31/34 ,  A61K31/341 ,  A61P35/00 ,  C07H15/252 ,  A61K31/71 ,  C07H15/24

    CPC分类号： C07H15/252

    摘要： Antitumor anthracycline glycosides of the formula: ##STR1## wherein one of R.sub.1 and R.sub.2 is hydrogen and the other is formyl, hydroxymethyl or aminomethyl, and R.sub.3 is hydrogen, hydroxy or an acyloxy group; and pharmaceutically acceptable acid addition salts of said compounds in which one of R.sub.1 and R.sub. 2 is aminomethyl are prepared from daunorubicin, doxorubicin or 14-O-acyl derivatives of doxorubicin by deamination and C-3' epimerization effected with NaNO.sub.2 in a cold aqueous acidic medium, such as 1N aqueous acetic acid at 0.degree. C., to give compounds wherein one of R.sub.1 and R.sub.2 is formyl and the optional further steps of selective reduction, e.g., with NaCNBH.sub.3 in 4:1 dioxan:aqueous acetate buffer at pH 4.6 or with Na(CH.sub.3 COO).sub.3 BH in benzene under reflux, to form compounds in which one of R.sub.1 and R.sub.2 hydroxymethyl, or selective reductive amination, e.g., with NaCNBH.sub.3 in the presence of methanolic CH.sub.3 COONH.sub.4 and a dehydrating agent, to form compounds in which one of R.sub.1 and R.sub.2 is aminomethyl.

    摘要翻译： 下式的抗肿瘤蒽环酸苷：其中R1和R2之一是氢，另一个是甲酰基，羟甲基或氨基甲基，R3是氢，羟基或酰氧基; 和其中R 1和R 2之一是氨基甲基的所述化合物的药学上可接受的酸加成盐通过脱氨基的柔红霉素，多柔比星的多柔比星或14-O-酰基衍生物和用NaNO 2在冷酸水溶液中进行的C-3'差向异构体 培养基，如1N乙酸水溶液在0℃下反应，得到其中R1和R2之一为甲酰基的化合物，以及选择性还原步骤的任选的其他步骤，例如在pH4.6的4:1二恶烷：乙酸水溶液缓冲液中的NaCNBH 3 或与Na（CH 3 COO）3·3HH）反应，生成其中R1和R2羟甲基之一或选择性还原胺化的化合物，例如与NaCNBH 3在甲醇CH 3 COONH 4和脱水剂存在下形成化合物，其中一个 的R 1和R 2是氨基甲基。