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81. 发明授权

US4067968A Daunosamine nucleosides 失效
标题翻译：丹诺胺类核苷
公开(公告)号：US4067968A
公开(公告)日：1978-01-10
申请号：US746851
申请日：1976-12-02
申请人： Ettore Lazzari , Federico Arcamone , Aurelio DI Marco
发明人： Ettore Lazzari , Federico Arcamone , Aurelio DI Marco
IPC分类号： C07D405/04 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61P35/00 , C07D239/36 , C07H17/02 , C07H19/06 , C07H19/16
CPC分类号： C07H19/06 , C07H19/16
摘要： The antitumor efficacy of the known antibiotics daunomycin (daunorubicin) and adriamycin (doxorubicin) is synergized by the use of said antibiotics together with a daunosamine nucleoside. The latter compounds are prepared by condensing a reactive protected daunosamine with a reactive protected heterocyclic base.
摘要翻译：已知的抗生素道诺霉素（柔红霉素）和阿霉素（多柔比星）的抗肿瘤功效通过使用所述抗生素与柔红霉素核苷进行协同作用。后一种化合物通过将反应性保护的柔红霉素与反应性保护的杂环碱缩合来制备。

82. 发明授权

US4035362A Methods for preparing cephalosporins 失效
标题翻译：头孢菌素的制备方法
公开(公告)号：US4035362A
公开(公告)日：1977-07-12
申请号：US672527
申请日：1976-03-31
申请人： Paolo Masi , Maurizio Foglio , Giovanni Franceschi , Antonino Suarato , Gianfranco Cainelli , Federico Arcamone
发明人： Paolo Masi , Maurizio Foglio , Giovanni Franceschi , Antonino Suarato , Gianfranco Cainelli , Federico Arcamone
IPC分类号： C07D205/08 , C07D205/095 , C07D501/08 , C07D501/10 , C07D501/20
CPC分类号： C07D501/08 , C07D205/095
摘要： A process for preparing cephalosporins of the structure: ##STR1## where R is any of hydrogen, C.sub.1 to C.sub.4 alkyl, t-butoxy, benzyloxy, cyano-methyl, thienyl-methyl, furyl-methyl, naphthyl-methyl, phenyl-methyl, phenoxy-methyl, phenoxy-isopropyl, pyridyl-4-thiomethyl and tetrazolyl-1-methyl;R.sub.1 is any of hydroxyl, C.sub.1 to C.sub.4 alkoxy, benzyloxy, p-methoxy- (or nitro-) benzyloxy, benzhydryloxy, triphenylmethoxy, phenacyloxy, p-halophenacyloxy and trichloroethoxy;Z is any of hydrogen, hydroxyl, --O--CO--C.sub.1 -C.sub.4 alkyl, --O--C.sub.1 -C.sub.4 alkyl, --Br, --I, --Cl, --N.sub.3, --NH.sub.2, --O--CO--CH.sub.3, --O--CO--NH.sub.2 and an -S-mononuclear nitrogen heterocyclic ring,By reacting compounds of the structure: ##STR2## IN WHICH R, R.sub.1, and Z are as above defined; R.sub.2 and R.sub.3 are the same or different and represent a C.sub.1 to C.sub.4 alkyl, a mononuclear aryl ring, --CN, a mononuclear heterocyclic ring or the radicals --COR.sub.4, COOR.sub.4, --PO(OR.sub.4).sub.2, --CO--NHR.sub.4 or R.sub.2 and R.sub.3 together may represent: ##STR3## where T represents >CH.sub.2, -N--R.sub.4 ; and R.sub.4 is lower alkyl, a mononuclear aryl ring or a mononuclear heterocyclic ring,Alone or as mixtures with each other in a suitable solvent at a temperature between -100 and +120.degree. C with a strong base to give compounds of formula I that are a mixture of .DELTA..sub.2 and .DELTA..sub.3 cephem-derivatives from which the .DELTA..sub.3 cephem derivatives can be obtained.
摘要翻译：一种制备结构式头孢菌素的方法：其中R是氢，C1-C4烷基，叔丁氧基，苄氧基，氰基 - 甲基，噻吩基 - 甲基，呋喃基 - 甲基，萘基 - 甲基，苯基 - 甲基，苯氧基甲基，苯氧基 - 异丙基，吡啶基-4-硫代甲基和四唑基-1-甲基; R1是羟基，C1〜C4烷氧基，苄氧基，对甲氧基 - （或硝基）苄氧基，二苯甲氧基，三苯基甲氧基，苯甲酰氧基，对卤代苯氧基和三氯乙氧基中的任一个。 Z是氢，羟基，-O-CO-C 1 -C 4烷基，-O-C 1 -C 4烷基，-Br，-I，-Cl，-N 3，-NH 2，-O-CO-CH 3，-O -CO-NH 2和-S-单核氮杂环，通过反应结构的化合物：其中R，R 1和Z如上所定义;其中R，R 1和Z如上所定义; R2和R3相同或不同，表示C1至C4烷基，单核芳基环，-CN，单核杂环或基团-COR4，COOR4，-PO（OR4）2，-CO-NHR4或R2和 R3一起可以表示：其中T表示> CH 2，-N-R 4; 并且R 4为低级烷基，单核芳基环或单核杂环，单独或混合于适宜溶剂中的温度为-100℃和+120℃之间的强碱，得到式I化合物可以获得DELTA 2和DELTA 3头孢烯衍生物的混合物，其中可以获得DELTA 3头孢烯衍生物。

83. 发明授权

US4024224A 14-Aminodaunomycins, their preparation and use 失效
标题翻译： 14-氨基诺乃霉素，其制备和用途
公开(公告)号：US4024224A
公开(公告)日：1977-05-17
申请号：US637170
申请日：1975-12-03
申请人： Federico Arcamone , Luigi Bernardi , Bianca Patelli , Aurelio DI Marco
发明人： Federico Arcamone , Luigi Bernardi , Bianca Patelli , Aurelio DI Marco
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , C07H15/22 , A61K31/71
CPC分类号： C07H15/252
摘要： 14-Aminodaunomycins, which are prepared by reacting 14-bromodaunomycin with an amine in a solvent at about 20.degree.-60.degree. C. are useful in treating certain tumors such as ascites Sarcoma 180 and solid Sarcoma 180.
摘要翻译：通过使14-溴原子素霉素与胺在溶剂中在约20-60℃下反应制备的14-氨基诺乃霉素可用于治疗某些肿瘤如腹水肉瘤180和固体肉瘤180。

84. 发明授权

US4021601A Paromomycin derivatives and process for the preparation thereof 失效
标题翻译：巴罗霉素衍生物及其制备方法
公开(公告)号：US4021601A
公开(公告)日：1977-05-03
申请号：US565657
申请日：1975-04-07
申请人： Federico Arcamone , Giuseppe Cassinelli
发明人： Federico Arcamone , Giuseppe Cassinelli
IPC分类号： C07H15/232 , C07H15/22
CPC分类号： C07H15/232
摘要： A process is disclosed for preparing paromomycin derivatives N-substituted in the 2'-position and having the general formula: ##STR1## wherein R.sub.2 is an alkyl radical having from 1 to 10 carbon atoms or an arylalkyl radical having not more than 10 carbon atoms, wherein paromomycin is treated with a carboxylic acid anhydride in the presence of a strong acid to give an intermediate of formula II as shown in the accompanying specification, which then is reacted in the presence of sodium borohydride with the aldehyde whose radical is to be attached to the N-atom in the 2' position. Also as new compounds, 2'-N-alkylparomomycins of formula (I), wherein R.sub.2 is an alkyl radical having from 1 to 10 carbon atoms or an arylalkyl radical having not more than 10 carbon atoms, includingTetra-(N-1, N-3, N-2"', N-6"')-acetylparomomycin;2'-N-ethylparomomycin; and2'-N-(3-phenylpropyl)-paromomycin.The new compounds are useful as antibiotics.
摘要翻译：公开了制备在2'-位上N-取代的具有以下通式的巴龙霉素衍生物的方法：其中R 2是具有1至10个碳原子的烷基或具有不超过10个碳原子的芳基烷基其中在强酸存在下，用羧酸酐处理巴龙霉素，得到如所附说明书所示的式Ⅱ中间体，然后在硼氢化钠存在下与其基团所连接的醛反应到2'位的N原子。还有作为新化合物，式（I）的2'-N-烷基巴罗霉素，其中R2是具有1-10个碳原子的烷基或具有不多于10个碳原子的芳基烷基，包括TETRA-（N-1， N-3，N-2“'，N-6”'） - 乙酰丙霉素; 2-N-乙基巴霉素; 和2'-N-（3-苯基丙基） - 霉素霉素。

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