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51. 发明授权

US4985548A 4-demethoxy-4-amino-anthracyclines 失效
标题翻译： 4-脱甲氧基-4-氨基蒽环类
公开(公告)号：US4985548A
公开(公告)日：1991-01-15
申请号：US462549
申请日：1990-01-09
申请人： Michele Caruso , Antonino Suarato , Francesco Angelucci , Federico Arcamone
发明人： Michele Caruso , Antonino Suarato , Francesco Angelucci , Federico Arcamone
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07C46/00 , C07C50/22 , C07C50/38 , C07C225/34 , C07H15/252
CPC分类号： C07H15/252
摘要： Anthracycline glycosides of the general formula (I): ##STR1## wherein R.sub.1 represents a hydrogen atom or a hydroxyl group, one of R.sub.2 and R.sub.3 represents a hydrogen atom and the other of R.sub.2 and R.sub.3 represents a hydrogen atom or a hydroxyl group; and pharmaceutically acceptable acid addition salts thereof are antitumor agents. These glycosides may be prepared from a daunomycinone derivative of formula (II): ##STR2## in which the 4-amino group is protected. 4-Demethoxy-4-amino-daunomycinone (II) and an earlier intermediate in its preparation, 4-demethoxy-4-amino-7-deoxy-daunomycinone (IX), can be diazotised followed by mild reduction to form 4-demethoxy-daunomycinone or 4-demethoxy-7-deoxy-daunomycinone respectively. 4-Demethoxy-daunomycinone can be converted into another antitumor anthracycline glycoside, 4-demethoxy-daunorubicin.

52. 发明授权

US4331677A 7-Oxo-4-1-aza-bicyclo-[3,2,0]-heptane derivatives 失效
标题翻译： 7-氧代-4-氮杂 - 双环 - [3,2,0] - 庚烷衍生物
公开(公告)号：US4331677A
公开(公告)日：1982-05-25
申请号：US95790
申请日：1979-11-19
申请人： Maurizio Foglio , Giovanni Franceschi , Cosimo Scarafile , Federico Arcamone
发明人： Maurizio Foglio , Giovanni Franceschi , Cosimo Scarafile , Federico Arcamone
IPC分类号： C07D499/87 , A61K31/43 , A61P31/04 , C07D205/09 , C07D499/00 , C07D499/06 , C07D499/86 , C07D499/897 , C07F9/568 , A61K31/425
CPC分类号： C07F9/5683 , C07D205/09 , C07D499/00
摘要： This invention relates to 7-oxo-4-thia-1-aza-bicyclo-[3,2,0]-heptane derivatives, to processes for their synthesis from esters of penicillanic acid 1-oxide, and to intermediate compounds obtained in the synthesis.More particularly, the present invention relates to new and novel compounds of formula (1): ##STR1## wherein R is a hydrogen atom, an alkyl having from 1 to 5 carbon atoms, trichloroethyl, benzyl, p-nitrobenzyl, diphenylmethyl, acetoxymethyl, pivaloyloxymethyl, phthalidyl, trimethylsilyl or a group of formula ##STR2## and R.sup.1 is --CH.sub.2 OH, --CH.sub.2 OCOR.sup.2, --CH.sub.2 OR.sup.3, --COOR.sup.2, --CHO, --CH.sub.2 SH, --CH.sub.2 SR.sup.4, --CH.sub.2 NH.sub.2, --CH.sub.2 NHCOR.sup.2 in which R.sup.2 is an alkyl having from 1 to 5 carbon atoms, aryl, aralkyl or a five- or six-membered heterocyclic ring containing one or more heteroatoms; R.sup.3 is an alkyl having from 1 to 5 carbon atoms, benzyl, trityl, trialkylsilyl; and R.sup.4 is a five- or six-membered heterocyclic ring containing one or more heteroatoms, benzyl, trityl or trialkylsilyl;and to the synthesis of such compounds.Compounds of formula (1) (E+Z isomers) are endowed with antibacterial activity.
摘要翻译：本发明涉及7-氧代-4-硫杂-1-氮杂 - 双环[3,2,0] - 庚烷衍生物，用于由青霉酸1-氧化物的酯合成的方法，以及在合成。更具体地说，本发明涉及新的和新的式（1）化合物：其中R是氢原子，具有1至5个碳原子的烷基，三氯乙基，苄基，对硝基苄基，二苯基甲基，乙酰氧基甲基，新戊酰氧基甲基，邻苯二甲酰基，三甲基甲硅烷基或式的基团，并且R 1是-CH 2 OH，-CH 2 OCOR 2，-CH 2 OR 3，-COOR 2，-CHO，-CH 2 SH，-CH 2 SR 4，-CH 2 NH 2，-CH 2 NHCOR 2，其中R 2是具有1至5个碳原子的烷基，芳基，芳烷基或含有一个或多个杂原子的五元或六元杂环; R3是具有1至5个碳原子的烷基，苄基，三苯甲基，三烷基甲硅烷基; 并且R 4是含有一个或多个杂原子的五元或六元杂环，苄基，三苯甲基或三烷基甲硅烷基; 以及这些化合物的合成。式（1）化合物（E + Z异构体）具有抗菌活性。

53. 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 ）。

54. 发明授权

US4132721A Optically active anthracyclinones and process therefor 失效
标题翻译：光学活性炭疽菌素及其制备方法
公开(公告)号：US4132721A
公开(公告)日：1979-01-02
申请号：US802789
申请日：1977-06-02
申请人： Luigi Bernardi , Pietro Giardino , Bianca Patelli , Federico Arcamone
发明人： Luigi Bernardi , Pietro Giardino , Bianca Patelli , Federico Arcamone
IPC分类号： C07C50/38 , C07C45/00 , C07C46/00 , C07C49/84 , C07C50/36 , C07C67/00 , C07H15/252 , C07C49/70
CPC分类号： C07C50/36 , C07C49/84 , C07H15/252
摘要： Optically active anthracyclinones are prepared by reacting an optically active (-) 1,4-dimethoxy-6-hydroxy-6-acetyl-tetralin with a phthalic anhydride in the presence of AlCl.sub.3 or AlBr.sub.3 and an alkali metal chloride at 130-180.degree. C. for 1 to 10 minutes.
摘要翻译：在AlCl 3或AlBr 3和碱金属氯化物的存在下，在130-180℃下使光学活性（ - ）1,4-二甲氧基-6-羟基-6-乙酰基 - 四氢化萘与邻苯二甲酸酐反应制备光学活性蒽环类 1至10分钟。

55. 发明授权

US4098884A Doxorubicin thioesters 失效
标题翻译： DOXORUBICIN THIOESTERS
公开(公告)号：US4098884A
公开(公告)日：1978-07-04
申请号：US776821
申请日：1977-03-10
申请人： Federico Arcamone , Luigi Bernardi , Bianca Patelli
发明人： Federico Arcamone , Luigi Bernardi , Bianca Patelli
IPC分类号： A61K31/095 , A61K31/65 , A61P35/00 , C07H15/252 , C07H15/24
CPC分类号： C07H15/252 , Y10S514/908
摘要： Doxorubicin thioesters of the formula ##STR1## wherein R is acyl and which are useful in treating animal tumors, are prepared by reacting 14-bromo-daunomycin with a salt of a thioacid of the formula RSM wherein R is as defined above and M is an alkali metal atom or a quaternary ammonium salt in an inert polar solvent. The invention described herein was made in the course of work under a grant from the Department of Health, Education, and Welfare.

56. 发明授权

US4085113A Process for the preparation of azetidinone-thiazoline precursors for cephalosporin synthesis 失效
标题翻译：制备用于头孢菌素合成的氮杂环丁酮 - 噻唑啉前体的方法
公开(公告)号：US4085113A
公开(公告)日：1978-04-18
申请号：US598260
申请日：1975-07-23
申请人： Maurizio Foglio , Ugo Scarponi , Federico Arcamone
发明人： Maurizio Foglio , Ugo Scarponi , Federico Arcamone
IPC分类号： C07D513/04
CPC分类号： C07D513/04
摘要： A process for the preparation of azetidinone-thiazoline precursors for cephalosporin synthesis. Said precursors are obtained by reducing by means of zinc dust in the presence of aqueous acetic acid a compound of formula ##STR1##
摘要翻译：用于制备头孢菌素合成的氮杂环丁酮 - 噻唑啉前体的方法。所述前体是通过在乙酸水溶液存在下通过锌粉，通式（IMAGE）化合物进行还原获得的

57. 发明授权

US4077988A Optically active anthracyclinones 失效
标题翻译：光学活性蒽环类
公开(公告)号：US4077988A
公开(公告)日：1978-03-07
申请号：US649825
申请日：1976-01-16
申请人： Federico Arcamone , Luigi Bernardi , Bianca Patelli , Aurelia Di Marco
发明人： Federico Arcamone , Luigi Bernardi , Bianca Patelli , Aurelia Di Marco
IPC分类号： C07C49/577 , A61K31/122 , A61K31/65 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07B31/00 , C07B57/00 , C07C13/48 , C07C39/12 , C07C45/00 , C07C45/85 , C07C49/215 , C07C50/22 , C07C50/38 , C07C67/00 , C07H15/24 , C07H15/252 , C07C49/68 , A61K31/12 , C07C49/72
CPC分类号： C07H15/252 , Y10S514/908
摘要： Disclosed are optically active anthracyclinones and their daunosaminyl derivatives, which are useful for the treatment of malignant diseases, particularly sarcomas, breast cancer, bronchogenic carcinoma, malignant lymphomas, neuroblastomas, acute leukemia and bladder cancer.
摘要翻译：公开了光学活性蒽环类和它们的柔红色氨基衍生物，其可用于治疗恶性疾病，特别是肉瘤，乳腺癌，支气管癌，恶性淋巴瘤，成神经细胞瘤，急性白血病和膀胱癌。

58. 发明授权

US4906743A 4-demethoxy-4-amino-anthracyclines 失效
公开(公告)号：US4906743A
公开(公告)日：1990-03-06
申请号：US181506
申请日：1988-04-14
申请人： Michele Caruso , Antonino Suarato , Francesco Angelucci , Federico Arcamone
发明人： Michele Caruso , Antonino Suarato , Francesco Angelucci , Federico Arcamone
摘要： Anthracycline glycosides of the general formula (I): ##STR1## wherein R.sub.1 represents a hydrogen atom or a hydroxyl group, one of R.sub.2 and R.sub.3 represents a hydrogen atom and the other of R.sub.2 and R.sub.3 represents a hydrogen atom or a hydroxyl group; and pharmaceutically acceptable acid addition salts thereof are antitumor agents. These glycosides may be prepared from a daunomycinone derivative of formula (II): ##STR2## in which the 4-amino group is protected. 4-Demethoxy-4-amino-daunomycinone (II) and an earlier intermediate in its preparation, 4-demethoxy-4-amino-7-deoxy-daunomycinone (IX), can be diazotized followed by mild reduction to form 4-demethoxy-daunomycinone or 4-demethoxy-7-deoxy-daunomycinone respectively. 4-Demethoxy-daunomycinone can be converted into another antitumor anthracycline glycoside, 4-demethoxy-daunorubicin.

59. 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。

60. 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。

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