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    3'-aziridino-anthracycline derivatives
    32.
    发明授权
    3'-aziridino-anthracycline derivatives 失效
    3'-氮丙啶基 - 蒽环类衍生物

    公开(公告)号：US5532218A

    公开(公告)日：1996-07-02

    申请号：US345450

    申请日：1994-11-21

    申请人： Alberto Bargiotti ,  Michele Caruso ,  Maria Grandi ,  Marina Ripamonti ,  Antonino Suarato

    发明人： Alberto Bargiotti ,  Michele Caruso ,  Maria Grandi ,  Marina Ripamonti ,  Antonino Suarato

    IPC分类号： A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/704 ,  A61P35/00 ,  C07H15/252 ,  C07H17/02 ,  C07H15/24

    CPC分类号： C07H15/252 ,  C07H17/02

    摘要： Anthracycline glycosides of general formula 1 and 2: ##STR1## wherein R.sub.1 is hydrogen or a methoxy group; R.sub.2 is hydrogen, a hydroxy group or represents an acyloxy residue of formula 3 --O--COR.sub.5 wherein R.sub.5 is a linear or branched C.sub.1 -C.sub.8 alkyl, an aryl group or a heterocyclic mono or bicyclic ring, each of which may be unsubstituted or substituted with (a) an amino group NR.sub.6 R.sub.7 in which R.sub.6 and R.sub.7 are independently hydrogen or C.sub.1 -C.sub.4 alkyl or (b) a carboxy group; R.sub.3 and R.sub.4 both represent hydrogen or one of R.sub.3 and R.sub.4 is hydrogen and the other is hydroxy group or a group of formula --OSO.sub.2 R.sub.8 in which R.sub.8 may be a linear or branched alkyl group containing from 1 to 6 carbon atoms or an aryl group unsubstituted or substituted by 1 to 3 substituents each of which may independently be a linear or branched alkyl or alkoxy group of from 1 to 6 carbon atoms, a halogen atom or a nitro group; and pharmaceutically acceptable salts thereof; are active as antitumor agents.

    摘要翻译： 通式1和2的蒽环酸苷：其中R 1是氢或甲氧基; R2是氢，羟基或代表式3-COR5的酰氧基残基，其中R5是直链或支链C1-C8烷基，芳基或杂环单环或双环，其各自可以是未取代或取代的 与（a）氨基NR 6 R 7，其中R 6和R 7独立地是氢或C 1 -C 4烷基或（b）羧基; R 3和R 4均代表氢或R 3和R 4之一是氢，另一个是羟基或式-OSO 2 R 8基团，其中R 8可以是含有1至6个碳原子的直链或支链烷基或未取代的芳基 或被1〜3个取代基取代，各自可以独立地为具有1-6个碳原子的直链或支链烷基或烷氧基，卤素原子或硝基; 及其药学上可接受的盐; 作为抗肿瘤剂有活性。

    Mono and bis alkylamino-anthracyclines
    33.
    发明授权
    Mono and bis alkylamino-anthracyclines 失效
    单和双烷基氨基蒽环类

    公开(公告)号：US5496808A

    公开(公告)日：1996-03-05

    申请号：US904650

    申请日：1992-06-26

    申请人： Alberto Bargiotti ,  Michele Caruso ,  Daniela Faiardi ,  Antonino Suarato ,  Nicola Mongelli

    发明人： Alberto Bargiotti ,  Michele Caruso ,  Daniela Faiardi ,  Antonino Suarato ,  Nicola Mongelli

    IPC分类号： A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/704 ,  A61P35/00 ,  C07H20060101 ,  C07H15/252 ,  C07H15/24

    CPC分类号： A61K31/70 ,  C07H15/252

    摘要： An anthracycline glycoside of general formula 1: ##STR1## wherein R.sub.1 is hydrogen or methoxy group; R.sub.2 is hydrogen or hydroxy group, A and B both represent hydrogen or one of A and B is hydrogen and the other is hydroxy or a group of formula --OSO.sub.2 R.sub.5 in which R.sub.5 is C1-C4 alkyl or aryl optionally substituted by C1-C4 alkyl, nitro, amino, methoxy or halogen; R.sub.3 is a hydrogen atom or a group of formula 2 and R.sub.4 is a group of formula 2--(CH.sub.2).sub.n --X 2in which n is 2 or 3 and X is hydroxy group, a halogen or a group of formula --OSO.sub.2 R.sub.5 in which R.sub.5 is as defined above and with the proviso that if R.sub.2, X and A are an hydroxy group and R.sub.3 .dbd.H, n must be 3; or a pharmaceutically acceptable salt thereof.Compounds of the invention have activity as antitumor agents. Processes for their preparation and pharmaceutical composition containing them are also disclosed.

    摘要翻译： 通式1的蒽环类苷：oup; R2是氢或羟基，A和B都代表氢或A和B之一是氢，另一个是羟基或式-OSO 2 R 5基团，其中R 5是任选被C 1 -C 4烷基取代的C 1 -C 4烷基或芳基 ，硝基，氨基，甲氧基或卤素; R3是氢原子或式2的基团，R4是式2 - （CH2）nX2的基团，其中n是2或3，X是羟基，卤素或式-OSO2R5基团，其中R5 条件是如果R2，X和A是羟基，R3 = H，则n必须为3; 或其药学上可接受的盐。 本发明的化合物具有作为抗肿瘤剂的活性。 还公开了其制备方法和含有它们的药物组合物。

    Antracycline glycosides, pharmaceutical compositions and method of use
    36.
    发明授权
    Antracycline glycosides, pharmaceutical compositions and method of use 失效
    抗菌素苷，药物组合物和使用方法

    公开(公告)号：US4477444A

    公开(公告)日：1984-10-16

    申请号：US434509

    申请日：1982-10-15

    申请人： Antonino Suarato ,  Sergio Penco ,  Federico Arcamone

    发明人： Antonino Suarato ,  Sergio Penco ,  Federico Arcamone

    IPC分类号： C07H15/252 ,  A61K31/70 ,  C07H15/24

    CPC分类号： C07H15/252 ,  Y02P20/55

    摘要： Disclosed is a process for preparing the new antitumor glycosides: 4'-deoxy-3'-epi-daunorubicin and 4'-deoxy-3'-epi-doxorubicin starting from the known 3'-epi-4'-keto-N-trifluoroacetyl-daunorubicin.Reduction of the 4'-keto group with sodium borohydride to the corresponding 4'-hydroxy group, reacting the so obtained intermediate with trifluoromethanesulphonic anhydride followed by treatment with n-tetrabutylammonium iodide, dehalogenated reductively, by treatment with tributyl tin hydride to 4'-deoxy-3'-epi-N-trifluoroacetyl-daunorubicin.A mild alkaline hydrolysis removes the N-protecting group to give 4'-deoxy-3'-epi-daunorubicin which is successively transformed, via its 14-bromo derivative, in its doxorubicin analogue.

    摘要翻译： 公开了一种制备新型抗肿瘤糖苷的方法：从已知的3'-表面-4'-酮-n-三磷酸开始制备4'-脱氧-3'-表柔比星和4'-脱氧-3'-表阿霉素， 三氟乙酰柔红霉素。 将4'-酮基用硼氢化钠还原成相应的4'-羟基，使所得中间体与三氟甲磺酸酐反应，然后用正丁基碘化铵处理，还原脱卤，通过用三丁基锡氢化物处理至4'- 脱氧-3'-表N-N-三氟乙酰柔红霉素。 轻度碱性水解除去N-保护基，得到4'-脱氧-3'-表柔比星，其通过其14-溴衍生物在其多柔比星类似物中相继转化。

    Methyl-.alpha.[3'acetoxy-1'isopropenyl]-3 substituted 1.alpha.,5x-4-thia 2,6 diaza[3,2,0]2-heptene-6 acetate 7-one
    39.
    发明授权
    Methyl-.alpha.[3'acetoxy-1'isopropenyl]-3 substituted 1.alpha.,5x-4-thia 2,6 diaza[3,2,0]2-heptene-6 acetate 7-one 失效
    甲基 - {60 {8 3 {40乙酰氧基-1 {40异丙烯基{9,3取代的1 {60,5x-4-硫杂-2,6-二氮杂{8 3,2,0 {9 2-庚烯-6-乙酸酯7- 一

    公开(公告)号：US4077970A

    公开(公告)日：1978-03-07

    申请号：US603605

    申请日：1975-08-11

    申请人： Maurizio Foglio ,  Antonino Suarato ,  Paolo Masi ,  Giovanni Franceschi ,  Giorgio Palamidessi ,  Luigi Bernardi

    发明人： Maurizio Foglio ,  Antonino Suarato ,  Paolo Masi ,  Giovanni Franceschi ,  Giorgio Palamidessi ,  Luigi Bernardi

    IPC分类号： C07D205/08 ,  C07D513/04 ,  C07D513/08

    CPC分类号： C07D513/04 ,  C07D205/08

    摘要： A process is disclosed for the preparation of a compound of the formula ##STR1## where R and R.sup.1 are defined herein below, wherein a compound of the structure; ##STR2## is reacted in a suitable solvent with a haloamide in the presence of a metal oxide or a haloamide in the presence of a free radical initiator under the influence of light or heat or alternatively with a halogen in the presence of a metal oxide, to give a compound of the structure; ##STR3## which compound, in a suitable solvent is reacted with a suitable nucleophilic reagent to obtain the compound; ##STR4## which compound is then subjected to allylic halogenation to give a compound of the structure; ##STR5## which is then reacted with a reducing agent to yield I.

    摘要翻译： 公开了用于制备下式化合物的方法，其中R和R 1如下文所定义，其中该结构的化合物; 在自由基引发剂的存在下，在光或热的作用下，或者在卤素存在下，在金属氧化物或卤代酰胺的存在下，在合适的溶剂中与卤代酰胺反应。 ，得到结构的化合物; 该化合物在合适的溶剂中与合适的亲核试剂反应得到化合物; 然后将该化合物进行烯丙基卤化，得到结构的化合物; 然后将其与还原剂反应以产生I.

    Process for preparing cephalosporins and certain novel 2.beta.-thiohydrazo-azetidinones as intermediates
    40.
    发明授权
    Process for preparing cephalosporins and certain novel 2.beta.-thiohydrazo-azetidinones as intermediates 失效

    公开(公告)号：US4067866A

    公开(公告)日：1978-01-10

    申请号：US700972

    申请日：1976-06-29

    申请人： Maurizio Foglio ,  Giovanni Franceschi ,  Paolo Masi ,  Antonino Suarato

    发明人： Maurizio Foglio ,  Giovanni Franceschi ,  Paolo Masi ,  Antonino Suarato

    IPC分类号： C07D501/08 ,  C07F9/24 ,  C07D205/08 ,  C07D409/12

    CPC分类号： C07F9/2458

    摘要： A process is disclosed for preparing cephalosporins of structure: ##STR1##where R is selected from the class consisting of hydrogen, alkyl having from 1 to 4 carbon atoms, cyano-methyl-, thienyl-methyl, furyl-methyl-, naphthyl-methyl-, phenyl-methyl-, phenoxy-methyl-, phenyl-isopropyl-, phenoxy-isopropyl-, pyridyl-4-thiomethyl-, and tetrazolyl-1-methyl;R.sup.1 is selected from the class consisting of hydroxyl, alkoxy with 1 to 4 carbon atoms, trichloroethoxy-, benzyloxy-, p-methoxy-benzyloxy-, p-nitrobenzyloxy-, benzhydryloxy-, triphenylmethoxy-, phenacyloxy-, and p-halophenacyloxy;Z is selected from the class consisting of hydrogen, hydroxyl, --O--alkyl, --O--CO--alkyl, --Br, --I, --N.sub.3, --NH.sub.2, --O--CO--CH.sub.3, --O--CO--NH.sub.2 and an --S--mononuclear nitrogen heterocyclic ring;Wherein a compound of structure: ##STR2## is reacted in a suitable solvent at a temperature between -20.degree. C and +80.degree. C, in the presence of an aqueous organic or inorganic acid with an azoderivative of the formula: ##STR3## where R.sup.2 and R.sup.3 are equal or different and represent lower alkyl, a mononuclear aryl ring, CN--, a mononuclear heterocyclic ring, or the radicals --COR.sup.4, --COOR.sup.4, ##STR4## --CONHR.sup.4, or R.sub.2 and R.sub.3 together may represent the residues; ##STR5## where T represents >CH.sub.2, >N -- R.sup.4, and R.sup.4 is lower alkyl, a mononuclear aryl ring or a mononuclear heterocyclic, ring to give a compound of structure: ##STR6## in which R, R.sup.1, R.sup.2, R.sup.3, and Z have the meanings given above, and said intermediate (II') is reacted in a suitable solvent at a temperature between -100.degree. C and +120.degree. C with a compound selected from the class consisting of inorganic basic or weakly acid oxides, and inorganic and organic bases, to finally give the desired compound (III) which is isolated and purified in known manner.