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1. 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。

2. 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。

3. 发明授权

US4134903A Anthracycline ethers and their preparation 失效
标题翻译：蒽环类醚及其制备方法
公开(公告)号：US4134903A
公开(公告)日：1979-01-16
申请号：US887782
申请日：1978-03-17
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： C07H15/252 , C07C49/72 , C07C49/73 , C07C97/26 , C09B1/30
CPC分类号： C07H15/252
摘要： Aglycones of the formula ##STR1## and Toslyhydrazones of the formula ##STR2## wherein R.sub.1, R.sub.2 and Ts have meanings described in the specification, and process for preparing a compound of formula (V).
摘要翻译：式（Ⅹ）的Ag con））of of hyd hyd V V V V））））））V V V V V V V V V V V V V V V V V V V V V V V V V V V V V V V V V V V V ）。

4. 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。

5. 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。

6. 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.

7. 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。

8. 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。

9. 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。

10. 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。

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