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41. 发明授权

US4438105A 4'-Iododerivatives of anthracycline glycosides 失效
标题翻译：蒽环类苷的4'-碘代衍生物
公开(公告)号：US4438105A
公开(公告)日：1984-03-20
申请号：US368415
申请日：1982-04-14
申请人： Antonino Suarato , Sergio Penco , Federico Arcamone , Anna M. Casazza
发明人： Antonino Suarato , Sergio Penco , Federico Arcamone , Anna M. Casazza
IPC分类号： C07H15/24 , A61K31/35 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , A61K31/71
CPC分类号： C07H15/252 , Y10S514/908
摘要： Starting from the known 4'-deoxy-4'-iodo-N-trifluoroacetyldaunorubicin, two new anthracycline glycosidic antibiotics, the 4'-deoxy-4'-iodo-daunorubicin and 4'-deoxy-4'-iodo-doxorubicin, have been prepared by known procedures. Both the new glycosides have been found to be endowed with outstanding antitumoral activity.
摘要翻译：从已知的4'-脱氧-4'-碘-N-三氟乙酰基柔红霉素开始，两种新的蒽环类抗生素，4'-脱氧-4'-碘柔红霉素和4'-脱氧-4'-碘 - 多柔比星，具有通过已知程序制备。这些新的糖苷都被发现具有突出的抗肿瘤活性。

42. 发明授权

US4327029A Anthracycline derivatives, their preparation and use 失效
标题翻译：蒽环类衍生物，其制备和用途
公开(公告)号：US4327029A
公开(公告)日：1982-04-27
申请号：US2072
申请日：1979-01-08
申请人： Luigi Bernardi , Paolo Masi , Antonino Suarato , Federico Arcamone
发明人： Luigi Bernardi , Paolo Masi , Antonino Suarato , Federico Arcamone
IPC分类号： A61K31/65 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , C07C39/40
CPC分类号： C07H15/252 , Y10S514/908
摘要： Compounds of the formula: ##STR1## wherein R.sub.1 is a C.sub.2 -C.sub.4 alkyl; a C.sub.3 -C.sub.6 cycloalkyl or benzyl; A and B are OH or A and B are OCOOR.sub.4 or B is OH and A is OCOOR.sub.4 ; and R.sub.4 is alkyl which are intermediates for the preparation of antitumor compounds of the formula: ##STR2## wherein R.sub.1 is a C.sub.2 -C.sub.4 alkyl; a C.sub.3 -C.sub.6 cycloalkyl; a C.sub.3 -C.sub.6 cycloalkyl substituted by a halogen, hydroxy, methoxy, amino or dimethylamino group; phenyl or phenyl substituted with nitro, chlorine or methoxy thiazyl, pyridyl, pyrazyl; or a phenyl-alkyl group of the formula X--Phe--(CH.sub.2).sub.n --, in which X is hydrogen, halogen, hydroxyl, amino, or nitro and n is an integer from 1 to 2; R.sub.2 is hydrogen, hydroxyl or acyloxy (R--COO--); where R is an alkyl having from 1 to 11 carbon atoms; and R.sub.3 is hydrogen or trifluoroacetyl and salts thereof with pharmaceutically acceptable acids.
摘要翻译：下式的化合物：其中R 1是C 2 -C 4烷基; C3-C6环烷基或苄基; A和B是OH或A，B是OCOOR4或B是OH，A是OCOOR4; 和R4是作为制备下式的抗肿瘤化合物的中间体的烷基：其中R 1是C 2 -C 4烷基; C3-C6环烷基; 被卤素，羟基，甲氧基，氨基或二甲氨基取代的C3-C6环烷基; 苯基或被硝基，氯或甲氧基噻唑取代的苯基，吡啶基，吡嗪基; 或式X-Phe-（CH2）n-的苯基 - 烷基，其中X是氢，卤素，羟基，氨基或硝基，n是1至2的整数; R2是氢，羟基或酰氧基（R-COO-）; 其中R是具有1至11个碳原子的烷基; 并且R 3是氢或三氟乙酰基及其盐与药学上可接受的酸。

43. 发明授权

US4268451A Daunomycin derivatives, their aglycones and the use thereof 失效
标题翻译：道诺霉素衍生物，其糖苷配基及其用途
公开(公告)号：US4268451A
公开(公告)日：1981-05-19
申请号：US038688
申请日：1979-05-14
申请人： Paolo Masi , Antonino Suarato , Luigi Bernardi , Federico Arcamone
发明人： Paolo Masi , Antonino Suarato , Luigi Bernardi , Federico Arcamone
IPC分类号： C07C50/38 , A61K31/65 , A61P31/04 , A61P35/00 , C07C45/00 , C07C67/00 , C07H15/252 , C07C50/16
CPC分类号： C07H15/252 , Y10S514/908
摘要： Daunomycin derivatives of the formula: ##STR1## wherein R.sub.1 is a lower alkyl having from 1 to 4 carbon atoms and R is a hydrogen atom or a trifluoroacetyl group are useful in treating certain mammalian tumors.
摘要翻译：下式的道诺霉素衍生物：其中R1是具有1至4个碳原子的低级烷基，R是氢原子或三氟乙酰基可用于治疗某些哺乳动物肿瘤。

44. 发明授权

US4166848A Anthracycline derivatives, their preparation and use 失效
标题翻译：蒽环类衍生物，其制备和用途
公开(公告)号：US4166848A
公开(公告)日：1979-09-04
申请号：US850933
申请日：1977-11-14
申请人： Luigi Bernardi , Paolo Masi , Antonino Suarato , Federico Arcamone
发明人： Luigi Bernardi , Paolo Masi , Antonino Suarato , Federico Arcamone
IPC分类号： A61K31/65 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , C07G3/00 , C07G11/00
CPC分类号： C07H15/252 , Y10S514/908
摘要： Disclosed are antitumor compounds of the formula: ##STR1## wherein R.sub.1 is a C.sub.2 -C.sub.4 alkyl; a C.sub.3 -C.sub.6 cycloalkyl; a C.sub.3 -C.sub.6 cycloalkyl substituted by a halogen, hydroxy, methoxy, amino or dimethylamino group; phenyl or phenyl substituted with nitro, chlorine or methoxy; thiazyl, pyridyl, pyrazyl; or a phenyl-alkyl group of the formula X--Phe--(CH.sub.2).sub.n --, in which X is hydrogen, halogen, hydroxyl, amino, or nitro and n is an integer from 1 to 2; R.sub.2 is hydrogen, hydroxyl or acyloxy (R--COO--), where R is an alkyl having from 1 to 11 carbon atoms; and R.sub.3 is hydrogen or trifluoroacetyl and salts thereof with pharmaceutically acceptable acids. Compounds I are prepared by condensing the aglycones thereof with 2,3,6-trideoxy-3-trifluoroacetamido-4-O-trifluoro-acetyl-.alpha.-L-lyxopyranosyl chloride according to a conventional technique.
摘要翻译：公开了下式的抗肿瘤化合物：其中R 1是C 2 -C 4烷基; C3-C6环烷基; 被卤素，羟基，甲氧基，氨基或二甲氨基取代的C3-C6环烷基; 苯基或被硝基，氯或甲氧基取代的苯基; 噻嗪基，吡啶基，吡嗪基; 或式X-Phe-（CH2）n-的苯基 - 烷基，其中X是氢，卤素，羟基，氨基或硝基，n是1至2的整数; R2是氢，羟基或酰氧基（R-COO-），其中R是具有1至11个碳原子的烷基; 并且R 3是氢或三氟乙酰基及其盐与药学上可接受的酸。通过根据常规技术将其糖苷配基与2,3,6-三脱氧-3-三氟乙酰氨基-4-O-三氟乙酰基-β-L-吡喃葡糖酰氯缩合制备化合物I.

45. 发明授权

US4133877A Anthracycline ethers and use therefor 失效
标题翻译：蒽环类醚类及其用途
公开(公告)号：US4133877A
公开(公告)日：1979-01-09
申请号：US817972
申请日：1977-07-22
申请人： Paolo Masi , Antonino Suarato , Pietro Giardino , Luigi Bernardi , Federico Arcamone
发明人： Paolo Masi , Antonino Suarato , Pietro Giardino , Luigi Bernardi , Federico Arcamone
IPC分类号： A61K31/65 , A61P35/00 , C07H15/252 , A61K31/71 , C07H15/24
CPC分类号： C07H15/252 , Y10S514/908
摘要： Novel antitumor antibiotics, which are daunomycin analogues of the formula: ##STR1## wherein R.sub.1 is hydrogen or a C.sub.1 -C.sub.4 lower alkyl, R.sub.2 is a C.sub.1 -C.sub.4 lower alkyl, a C.sub.3 -C.sub.6 cycloalkyl, phenyl, lower alkyl phenyl, lower alkoxy phenyl or halophenyl, and R.sub.3 is hydrogen or trifluoroacetyl are prepared by condensing 2,3,6-trideoxy-3-trifluoroacetamido-4-0-trifluoroacetyl-.alpha.-L-lyxopyranosyl chloride with novel aglycones of the formula: ##STR2## which are in turn prepared by a novel method from 14-bromodaunomycinone through a series of novel intermediates.
摘要翻译：新型抗肿瘤抗生素，其为下式的道诺霉素类似物：其中R 1为氢或C 1 -C 4低级烷基，R 2为C 1 -C 4低级烷基，C 3 -C 6环烷基，苯基，低级烷基苯基，低级烷氧基苯基或卤代苯基，R 3是氢或三氟乙酰基是通过将2,3,6-三脱氧-3-三氟乙酰胺基-4-0-三氟乙酰基-α-L-吡喃半乳糖酰氯与下式的新型糖苷配基缩合制备的：，其又通过一系列新型中间体通过来自14-溴代新霉素酮的新方法制备。

46. 发明授权

US4012381A Process for preparing cephalosporins and intermediates 失效
标题翻译：制备头孢菌素和中间体的方法
公开(公告)号：US4012381A
公开(公告)日：1977-03-15
申请号：US586376
申请日：1975-06-12
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： C07D205/095 , C07D501/08 , C07D501/18 , C07D501/20
CPC分类号： C07D205/095
摘要： A process is disclosed for preparing derivatives of 7-amino-cephalosporanic acid and 7-amino-desacetoxycephalosporanic acid of structure: starting from a 3-acylamino-2.beta.-thiohydrazoazetidinone of structure: ##STR1## wherein the compound (II') is reacted with a phosphorous halide in the presence of a tertiary amine, the corresponding imino chloride is reacted with a lower aliphatic alcohol, the iminoether so formed is hydrolyzed with water in an acid medium, and the resultant 3-amino-2.beta.-thiohydrazoazetidinone of structure: ##STR2## is reacted in a suitable solvent and at a temperature between -100.degree. 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 (V) which is isolated and purified in known manner.2.beta.-thiohydrazoazetidinones are also disclosed as intermediates.
摘要翻译：公开了一种制备以下结构的3-氨基 - 头孢烷酸和7-氨基 - 脱乙酰氧基头孢烷酸的衍生物的方法，其结构如下：起始于结构如下的3-酰基氨基-2β-硫代代氮杂环丁酮：（II' ），其中化合物（II'）在叔胺存在下与卤化磷反应，相应的亚氨基氯与低级脂族醇反应，所形成的亚氨基醚在酸性介质中用水水解，得到的将结构如下的3-氨基-2β-硫代代代氮杂环丁酮在合适的溶剂中，在-100至+ 120℃的温度下与选自无机碱性或弱碱性的化合物反应酸性氧化物和无机和有机碱，最终得到所需的化合物（V），其以已知方式分离和纯化。

47. 发明授权

US4477444A Antracycline glycosides, pharmaceutical compositions and method of use 失效
标题翻译：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。

48. 发明授权

US4267116A Novel daunomycin derivatives, their aglycones and the use thereof 失效
标题翻译：新型道诺霉素衍生物，其糖苷配基及其用途
公开(公告)号：US4267116A
公开(公告)日：1981-05-12
申请号：US38689
申请日：1979-05-14
申请人： Paolo Masi , Antonino Suarato , Luigi Bernardi , Federico Arcamone
发明人： Paolo Masi , Antonino Suarato , Luigi Bernardi , Federico Arcamone
IPC分类号： C07C50/38 , A61K31/65 , A61P31/04 , A61P35/00 , C07C45/00 , C07C67/00 , C07H15/252 , C07C50/16
CPC分类号： C07H15/252 , Y10S514/908
摘要： Daunomycin derivatives of the formula: ##STR1## wherein R.sub.1 is a lower alkyl having from 1 to 4 carbon atoms and R is hydrogen or a trifluoroacetyl group are useful in treating certain mammalian tumors.
摘要翻译：下式的道诺霉素衍生物：其中R1是具有1至4个碳原子的低级烷基，R是氢或三氟乙酰基可用于治疗某些哺乳动物肿瘤。

49. 发明授权

US4191756A Daunomycin derivatives, their aglycones and the use thereof 失效
标题翻译：道诺霉素衍生物，其糖苷配基及其用途
公开(公告)号：US4191756A
公开(公告)日：1980-03-04
申请号：US901359
申请日：1978-05-01
申请人： Paolo Masi , Antonino Suarato , Luigi Bernardi , Federico Arcamone
发明人： Paolo Masi , Antonino Suarato , Luigi Bernardi , Federico Arcamone
IPC分类号： C07C50/38 , A61K31/65 , A61P31/04 , A61P35/00 , C07C45/00 , C07C67/00 , C07H15/252 , A61K31/71 , C07H15/24
CPC分类号： C07H15/252 , Y10S514/908
摘要： Daunomycin derivatives of the formula: ##STR1## wherein R.sub.1 is a lower alkyl having from 1 to 4 carbon atoms and R is a hydrogen atom or a trifluoroacetyl group are useful in treating certain mammalian tumors.
摘要翻译：下式的道诺霉素衍生物：其中R1是具有1至4个碳原子的低级烷基，R是氢原子或三氟乙酰基可用于治疗某些哺乳动物肿瘤。

50. 发明授权

US4077970A 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
标题翻译：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.

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