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31. 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

32. 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。

33. 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。

34. 发明授权

US5017599A Site specific alkylating agents 失效
标题翻译：现场特异性烷化剂
公开(公告)号：US5017599A
公开(公告)日：1991-05-21
申请号：US485847
申请日：1990-02-21
申请人： Ettore Lazzari , Federico Arcamone , Sergio Penco , Maria A. Verini , Nicola Mongelli
发明人： Ettore Lazzari , Federico Arcamone , Sergio Penco , Maria A. Verini , Nicola Mongelli
IPC分类号： A61K31/40 , A61K31/4025 , A61P35/00 , A61P35/02 , C07D207/34 , C07D403/12 , C07D409/12 , C07D417/12 , C07D207/14
CPC分类号： C07D409/12 , C07D207/34
摘要： The invention relates to distamycin A analogs of the following formula ##STR1## wherein n is 2, 3 or 4; A is an optionally substituted divalent radical chosen from ##STR2## and -Het- wherein Het is a pentatomic or hexatomic heteromonocyclic ring, except pyrrole; and wherein either one of R.sub.1 and R.sub.2 is hydrogen and the other is an acylating moiety or R.sub.1 and R.sub.2 are both hydrogen or both alkyl groups optionally substituted, including the pharmaceutically acceptable salts of the said compounds.The compounds of the invention can be useful antitumor and antiviral agents.

35. 发明授权

US4939282A The process for preparing 6-deoxynthracyclines 失效
标题翻译： 6-脱氧蒽环的制备方法
公开(公告)号：US4939282A
公开(公告)日：1990-07-03
申请号：US622177
申请日：1984-06-19
申请人： Francesco Angelucci , Sergio Penco , Ermes Vanotti , Federico Arcamone
发明人： Francesco Angelucci , Sergio Penco , Ermes Vanotti , Federico Arcamone
IPC分类号： C07C50/38 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07C45/00 , C07C46/00 , C07C50/36 , C07C67/00 , C07D407/04 , C07H15/252
CPC分类号： C07D407/04 , C07H15/252
摘要： A new process for the preparation of 6-deoxyanthracyclinones of general formula I: ##STR1## wherein R represents a hydrogen atom, a hydroxy group or a lower alkoxy group is described. The process provides a total synthesis of the 6-deoxyanthracyclinones of formula I using 1,2,3,6-tetrahydro-phthalate as starting material. The obtained racemic mixture of the compounds of formula I, if desired, can be submitted to optical resolution by the conventional method of conversion to diastereomeric derivatives using a chiral resolving agent. Alternatively, the racemic mixture can be used as such for the condensation with a suitably protected halosugar derivative to obtain alpha glycosidic derivatives of formula XV: ##STR2## wherein R.sub.1 represents a hydrogen atom or a hydroxy group, one of R.sub.2 and R.sub.3 represents a hydrogen atom, the other of R.sub.2 and R.sub.3 represents a hydrogen atom or a hydroxy group and X is a hydrogen atom or a trifluoro acetyl group. The N-trifluoroacetyl 7S:9S and 7R:9R derivatives of the .alpha.-glycosides of formula XV can be separated by chromatography on silica gel to obtain, after mild alkaline hydrolisis the wanted 7S:9S .alpha.-glycosides (R.sub.1 =H) as free bases and can eventually be transformed into their corresponding doxorubicin derivatives (R.sub.1 =OH) by known procedures.
摘要翻译：描述了制备通式I的6-脱氧尿嘧啶的新方法：其中R表示氢原子，羟基或低级烷氧基。该方法提供使用1,2,3,6-四氢邻苯二甲酸酯作为起始原料的式I的6-脱氧蒽环类的全合成。如果需要，所得到的式I化合物的外消旋混合物可以通过使用手性拆分剂转化成非对映体衍生物的常规方法进行光学拆分。或者，外消旋混合物可以直接用于与适当保护的卤糖衍生物的缩合，以获得式XV的α糖苷衍生物：其中R 1表示氢原子或羟基，R 2和R 3之一表示氢原子，R2和R3中的另一个表示氢原子或羟基，X是氢原子或三氟乙酰基。式XV的α-糖苷类的N-三氟乙酰基7S：9S和7R：9R衍生物可以通过硅胶色谱分离，得到在温和的碱性水解后，所需的7S：9Sα-糖苷（R1 = H）为游离碱，并且最终可以通过已知的方法转化成它们相应的多柔比星衍生物（R1 = OH）。

36. 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.

37. 发明授权

US4604381A 4-demethoxy-13-dihydrodaunorubicin and use thereof 失效
标题翻译： 4-脱甲氧基-13-二氢阿柔比星及其用途
公开(公告)号：US4604381A
公开(公告)日：1986-08-05
申请号：US668178
申请日：1984-11-05
申请人： Sergio Penco , Federico Arcamone , Anna Maria Casazza
发明人： Sergio Penco , Federico Arcamone , Anna Maria Casazza
IPC分类号： C07H15/252 , A61K31/71 , C07H15/24
CPC分类号： C07H15/252
摘要： A new antitumor anthracycline glycoside, 4-demethoxy-13-dihydrodaunorubicin, is disclosed.The new compound is prepared by reduction of the side-chain ketone function of the known 4-demethoxydaunorubicin, with sodium borohydride in aqueous solution at room temperature.
摘要翻译：公开了一种新的抗肿瘤蒽环苷类4-脱甲氧基-13-二氢阿柔比星。通过在室温下将硼氢化钠在水溶液中还原已知的4-脱甲氧基二柔比星的侧链酮官能团制备新化合物。

38. 发明授权

US4465671A Anthracycline glycosides use and compositions containing same 失效
标题翻译：蒽环类苷用途及其含有的组合物
公开(公告)号：US4465671A
公开(公告)日：1984-08-14
申请号：US382144
申请日：1982-05-26
申请人： Francesco Angelucci , Sergio Penco , Federico Arcamone
发明人： Francesco Angelucci , Sergio Penco , Federico Arcamone
IPC分类号： C07C50/38 , C07H15/252 , A61K31/71 , C07H15/24
CPC分类号： C07H15/252 , C07C50/38 , Y02P20/55
摘要： Anthracycline glycosides of the formula (I) ##STR1## wherein one of R.sub.1 and R.sub.2 is hydrogen and the other of R.sub.1 and R.sub.2 is hydroxy, each of R.sub.3, R.sub.4 and R.sub.5 is independently selected from the group consisting of hydrogen and hydroxy and X is hydrogen or trifluoroacetyl, with the provisos that R.sub.4 and R.sub.5 are not simultaneously hydroxy and that if R.sub.3 is hydroxy, then X is hydrogen, which are useful in treating certain mammalian tumors are prepared by condensing an aglycone of the formula (II) ##STR2## wherein R.sub.1 and R.sub.2 are defined as above, with a suitable protected halosugar, after which the protecting groups are removed.
摘要翻译：式（I）的蒽环酸糖苷其中R 1和R 2之一是氢，R 1和R 2中的另一个是羟基，R 3，R 4和R 5各自独立地选自氢和羟基，X 是氢或三氟乙酰基，条件是R 4和R 5不同时为羟基，如果R 3为羟基，则X为氢，其可用于治疗某些哺乳动物肿瘤通过将式（II）的糖苷配基缩合制备其中R 1和R 2如上所定义，具有合适的受保护的卤糖，之后除去保护基。

39. 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。

40. 发明授权

US4393052A Antitumor anthracycline glycosides, their preparation, intermediates therefor, and compositions and use thereof 失效
标题翻译：抗癌蒽环类苷，其制备方法，其中间体及其组合物和用途
公开(公告)号：US4393052A
公开(公告)日：1983-07-12
申请号：US316058
申请日：1981-10-29
申请人： Alberto Bargiotti , Giuseppe Cassinelli , Sergio Penco , Federico Arcamone , Annamaria Casazza
发明人： Alberto Bargiotti , Giuseppe Cassinelli , Sergio Penco , Federico Arcamone , Annamaria Casazza
IPC分类号： A61K31/70 , A61K31/7024 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , A61P35/02 , C07D309/30 , C07H13/04 , C07H13/06 , C07H15/04 , C07H15/252 , A61K31/71 , C07H15/22
CPC分类号： C07H15/04 , C07D309/30 , C07H13/04 , C07H15/252 , Y10S514/908
摘要： Novel antitumor anthracycline glycosides are prepared by condensing daunomycinone with 2,3,4,6-tetradeoxy-4-C-methylene-3-trifluoroacetamido-L-threo-hexopyranosyl chloride; 2,3,4,6-tetradeoxy-4-C-methylene-3-trifluoroacetamido-L-arabino-hexopyranosyl chloride or 2,3,6-trideoxy-4-C-trifluoroacetamidomethyl-3-trifluoroacetamido-3-O-trifluoroacetyl-L-lyxo-hexopyranosyl chloride.
摘要翻译：通过将道诺霉素与2,3,4,6-四脱氧-4-C-亚甲基-3-三氟乙酰氨基-L-苏 - 己酰氯氯化物缩合制备新型抗肿瘤蒽环类苷; 2,3,4,6-四脱氧-4-C-亚甲基-3-三氟乙酰氨基-L-阿拉伯 - 己酸乳酸酰氯或2,3,6-三脱氧-4-C-三氟乙酰氨基甲基-3-三氟乙酰胺基-3-羟基乙酰氨基 -L-胞嘧啶 - 六吡喃葡糖酰氯。

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