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1. 发明授权

US4046878A Daunomycin analogues, their preparation and use 失效
标题翻译：道诺霉素类似物，其制备和用途
公开(公告)号：US4046878A
公开(公告)日：1977-09-06
申请号：US579901
申请日：1975-05-22
申请人： Bianca Patelli , Luigi Bernardi , Federico Arcamone , Aurelio Di Marco
发明人： Bianca Patelli , Luigi Bernardi , Federico Arcamone , Aurelio Di Marco
IPC分类号： A61K31/704 , C07H15/252 , A61K31/71 , C07H11/00
CPC分类号： C07H15/252 , Y10S514/908
摘要： Daunomycin analogues of the formula: ##STR1## wherein when each R.sub.1 is hydrogen, each R is hydrogen, chlorine, bromine, methyl or methoxy and when each R.sub.1 is chlorine, bromine or methyl, each R is hydrogen, are useful in treating various mammalian tumors and are prepared by reacting a daunomycinone derivative of the formula: ##STR2## wherein R and R.sub.1 are as defined above with 1-chloro-2,3,6-trideoxy-3-trifluoroacetamido-4-trifluoroacetoxy-.alpha.-L-lyxopyranose in an inert anhydrous organic solvent in the presence of a catalyst and a hydrogen chloride acceptor.
摘要翻译：道诺霉素类似物，具有下式：其中当每个R 1是氢时，每个R是氢，氯，溴，甲基或甲氧基，并且当每个R 1是氯，溴或甲基时，每个R是氢，可用于治疗各种哺乳动物肿瘤，并且通过使下式的道诺霉素酮衍生物：其中R和R 1如上所定义的道诺霉素酮衍生物与1-氯-2,3,6-三脱氧-3-三氟乙酰氨基-4-三氟乙酰氧基 α-L-吡喃葡萄糖在惰性无水有机溶剂中，在催化剂和氯化氢受体存在下。

2. 发明授权

US4024224A 14-Aminodaunomycins, their preparation and use 失效
标题翻译： 14-氨基诺乃霉素，其制备和用途
公开(公告)号：US4024224A
公开(公告)日：1977-05-17
申请号：US637170
申请日：1975-12-03
申请人： Federico Arcamone , Luigi Bernardi , Bianca Patelli , Aurelio DI Marco
发明人： Federico Arcamone , Luigi Bernardi , Bianca Patelli , Aurelio DI Marco
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , C07H15/22 , A61K31/71
CPC分类号： C07H15/252
摘要： 14-Aminodaunomycins, which are prepared by reacting 14-bromodaunomycin with an amine in a solvent at about 20.degree.-60.degree. C. are useful in treating certain tumors such as ascites Sarcoma 180 and solid Sarcoma 180.
摘要翻译：通过使14-溴原子素霉素与胺在溶剂中在约20-60℃下反应制备的14-氨基诺乃霉素可用于治疗某些肿瘤如腹水肉瘤180和固体肉瘤180。

3. 发明授权

US4031211A Adriamycin esters, their preparation and use 失效
标题翻译：阿霉素酯，其制备和用途
公开(公告)号：US4031211A
公开(公告)日：1977-06-21
申请号：US694656
申请日：1976-06-10
申请人： Bianca Patelli , Luigi Bernardi , Federico Arcamone , Aurelio DI Marco
发明人： Bianca Patelli , Luigi Bernardi , Federico Arcamone , Aurelio DI Marco
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , A61P35/02 , C07H15/252 , C07H15/24
CPC分类号： C07H15/252 , Y10S514/908
摘要： Disclosed are novel C-14 adriamycin esters which are useful in the treatment of certain tumors.
摘要翻译：公开了可用于治疗某些肿瘤的新型C-14阿霉素酯。

4. 发明授权

US4125607A Daunosaminyl anthracyclinones and their use 失效
标题翻译：氨基甲酰基蒽环霉素及其用途
公开(公告)号：US4125607A
公开(公告)日：1978-11-14
申请号：US737473
申请日：1976-11-01
申请人： Federico Arcamone , Luigi Bernardi , Pietro Giardino , Aurelio DI Marco
发明人： Federico Arcamone , Luigi Bernardi , Pietro Giardino , Aurelio DI Marco
IPC分类号： A61K31/65 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , C07H15/24
CPC分类号： C07H15/252
摘要： Disclosed is a class of novel daunosaminyl anthracyclinones which are useful in treating Sarcoma 180 ascites.
摘要翻译：公开了一类可用于治疗肉瘤180腹水的新型氨基甲酰基蒽环类抗生素。

5. 发明授权

US4107423A Process for preparing daunomycin and analogues thereof 失效
标题翻译：道诺霉素及其类似物的制备方法
公开(公告)号：US4107423A
公开(公告)日：1978-08-15
申请号：US695434
申请日：1976-08-14
申请人： Federico Arcamone , Luigi Bernardi , Bianca Patelli , Sergio Penco
发明人： Federico Arcamone , Luigi Bernardi , Bianca Patelli , Sergio Penco
IPC分类号： C07H15/252 , C07H15/24
CPC分类号： C07H15/252
摘要： Racemic anthracyclinones of the general formula II ##STR1## when condensed with 2,3,6-trideoxy-3-trifluoroacetamido-4-0-trifluoroacetyl-.alpha.-L-lyxo-pyranosyl chloride in the presence of silver trifluoromethane sulphonate yield an easily separable mixture of equimolar amounts of exclusively the .alpha.-glycoside of the 7S : 9S diastereomer and the .beta.-glycoside of the 7R : 9R diastereomer. In this way the biologically important .alpha.-glycosides of the 7S : 9S diastereomer of the general formula I (below) are easily prepared from a racemic anthracyclinone.
摘要翻译：在三氟甲磺酸银存在下与2,3,6-三脱氧-3-三氟乙酰胺基-4-0-三氟乙酰-α-L-吡唑并吡喃二氯甲烷缩合时，通式II II的外消旋蒽环类产生容易 7S：9S非对映异构体的α-糖苷和7R：9R非对映异构体的β-糖苷的等摩尔量的可分离混合物。以这种方式，通式I（下文）的7S：9S非对映异构体的生物学上重要的α-糖苷类可以容易地由外消旋蒽环类抗生素制备。

6. 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。

7. 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.

8. 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。

9. 发明授权

US3963760A Selective demethylation of anthracycline derivatives 失效
标题翻译：蒽环类衍生物的选择性去甲基化
公开(公告)号：US3963760A
公开(公告)日：1976-06-15
申请号：US613423
申请日：1975-09-15
申请人： Luigi Bernardi , Bianca Patelli
发明人： Luigi Bernardi , Bianca Patelli
IPC分类号： C07C69/95 , C07C87/10
CPC分类号： C07C69/95
摘要： Anthracycline derivatives of the formula ##SPC1##Wherein R.sub.1, R.sub.2, R.sub. 3 and R.sub.4 are independently selected from the group consisting of hydrogen, chlorine, bromine and methoxy, with the proviso that at least one of the substituents is methoxy, and wherein R.sub.5 is selected from the group consisting of hydrogen, OH OR and OCOR; R being an alkyl group of 1 to 4 carbon atoms are prepared, in a single step, by selectively demethylating a compound of the formula: ##SPC2##Wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as defined above by treating same with an aluminum halide in the presence of a suitable solvent at a temperature of 0.degree. to 50.degree.C.
摘要翻译：式WHEREIN R 1，R 2，R 3和R 4的蒽环类衍生物独立地选自氢，氯，溴和甲氧基，条件是至少一个取代基是甲氧基，其中R 5选自由氢，OH OR和OCOR组成的组; 在一个步骤中，通过选择性地使下式化合物去甲基化制备R 1为1至4个碳原子的烷基：

10. 发明授权

US4196288A Ergoline derivatives and a process for their preparation 失效
标题翻译：艾尔莫林衍生物及其制备方法
公开(公告)号：US4196288A
公开(公告)日：1980-04-01
申请号：US856536
申请日：1977-12-01
申请人： Enzo Beacco , Luigi Bernardi , Enrico Di Salle , Giovanni Falconi , Bianca Patelli
发明人： Enzo Beacco , Luigi Bernardi , Enrico Di Salle , Giovanni Falconi , Bianca Patelli
IPC分类号： A61K31/48 , A61K31/495 , A61K31/505 , C07D457/02
CPC分类号： C07D457/02
摘要： New ergoline derivatives are disclosed which are compounds of formula (I) having the structure: ##STR1## wherein R.sub.1 is hydrogen or methoxy; R.sub.2 is hydrogen or methyl; andX is hydroxy, R.sub.3 COO, S--R.sub.4 or NR.sub.5 R.sub.6 in which R.sub.3 is a straight or branched alkyl having from 1 to 6 carbon atoms, unsubstituted- or substituted-phenyl, the substituents being selected from the class consisting of chlorine, bromine, alkyl or alkoxy having from 1 to 4 carbon atoms, cycloalkyl containing from 3 to 6 carbon atoms, or a heterocycle;R.sub.4 is phenyl or a heterocycle, andR.sub.5 and R.sub.6 are alkyl having from 1 to 4 carbon atoms, or together with the N atom to which they are attached, forming a heterocycle. The heterocycle may be a 5- or 6-membered ring which contains from 1 to 3 hetero atoms selected from the class consisting of nitrogen, oxygen and sulphur, and may be saturated or unsaturated, and unsubstituted or substituted by halogen, alkyl having from 1 to 3 carbon atoms, hydroxy, nitro, amino, CONHNH.sub.2 and COOH.
摘要翻译：公开了新的麦角灵衍生物，其是具有以下结构的式（I）的化合物：其中R 1是氢或甲氧基; R2是氢或甲基; 并且X是羟基，R 3 COO，S-R 4或NR 5 R 6，其中R 3是具有1至6个碳原子的直链或支链烷基，未取代或取代的苯基，所述取代基选自氯，溴，烷基或具有1至4个碳原子的烷氧基，含3至6个碳原子的环烷基或杂环; R 4是苯基或杂环，R 5和R 6是具有1至4个碳原子的烷基，或与它们相连的N原子一起形成杂环。杂环可以是含有1至3个选自氮，氧和硫的杂原子的5或6元环，并且可以是饱和或不饱和的，未取代的或被卤素取代的烷基，具有1个至3个碳原子，羟基，硝基，氨基，CONHNH 2和COOH。

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