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1. 发明授权

US4155911A Process for the production of substituted 4-thia-2,6-diaza[3.2.0]-2-heptene-7-one 失效
标题翻译：制备取代的4-硫杂-2,6-二氮杂{8 3.2.0 {9,2-庚烯-7-酮
公开(公告)号：US4155911A
公开(公告)日：1979-05-22
申请号：US820895
申请日：1977-08-01
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
CPC分类号： C07D513/04 , C07D205/08
摘要： A new process is disclosed for the preparation of compounds of structure: ##STR1## and are as defined herein characterized in that a compound of structure ##STR2## where R and R.sup.1 have the meanings given herein, 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 structure: ##STR3## where R and R.sup.1 have the meanings given herein, Hal is a halogen atom; THE INTERMEDIATE COMPOUND (III) in a suitable solvent is then reacted with an appropriate nucleophilic reagent to obtain the compound IV where Z replaces Hal, where Z is defined herein;The compound (IV) is then subjected to an allylic halogenation in a suitable solvent by reacting it with a haloamide either under the influence of light alone or by heating it in the presence of a free radical initiator, to give a compound of structure: ##STR4## where R, R.sup.1 and Hal and Z have the above meanings; THE INTERMEDIATE COMPOUND (V) is then reacted with a reducing agent to give finally the desired compound (I).
摘要翻译：公开了用于制备结构式（I）的化合物的新方法，其定义如下，其特征在于其中R和R 1具有本文给出的含义的结构式（II）的化合物在在金属氧化物或卤代酰胺的存在下，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，在金属氧化物的存在下，与卤代酰胺合适的溶剂，得到结构化合物（III）其中R和R1具有本文给出的含义，Hal是卤素原子; 然后将合适的溶剂中的中间体化合物（III）与合适的亲核试剂反应，得到Z代替Hal的化合物IV，其中Z在本文中定义; 然后使化合物（IV）在合适的溶剂中通过与单独的光的影响下的卤代酰胺反应或通过在自由基引发剂的存在下加热使其与卤代酰胺反应，得到结构式（V）其中R，R1，Hal和Z具有上述含义; 然后将中间体化合物（V）与还原剂反应，最终得到所需化合物（I）。

2. 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.

3. 发明授权

US4191755A 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：US4191755A
公开(公告)日：1980-03-04
申请号：US901358
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 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。

4. 发明授权

US4188377A Carminomycin derivatives, their preparation and use 失效
标题翻译：卡门霉素衍生物，其制备和用途
公开(公告)号：US4188377A
公开(公告)日：1980-02-12
申请号：US872626
申请日：1978-01-26
申请人： Antonino Suarato , Paolo Masi , Luigi Bernardi , Federico Arcamone
发明人： Antonino Suarato , Paolo Masi , Luigi Bernardi , Federico Arcamone
IPC分类号： C07H15/252 , A61K31/70 , C07H15/24
CPC分类号： C07H15/252 , Y10S514/908
摘要： N-acyl derivatives of the known antitumor antibiotic carminomycin, particularly N-trifluoroacetyl carminomycin, have a much lower toxicity than carminomycin.
摘要翻译：已知抗肿瘤抗生素卡明霉素的N-酰基衍生物，特别是N-三氟乙酰卡明霉素，毒性低于卡培霉素。

5. 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。

6. 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。

7. 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。

8. 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。

9. 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.

10. 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。

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