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公开(公告)号：US4191755A
公开(公告)日：1980-03-04
申请号：US901358
申请日：1978-05-01
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。
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公开(公告)号：US4188377A
公开(公告)日：1980-02-12
申请号：US872626
申请日：1978-01-26
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。
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公开(公告)号：US4098798A
公开(公告)日：1978-07-04
申请号：US823581
申请日：1977-08-11
IPC分类号： C07H15/252 , C07D317/10
CPC分类号： C07H15/252
摘要： The known antibiotics adriamycin and its .beta.-anomer, and the novel compounds, 4'-epiadriamycin (both .alpha.- and .beta.-anomers) are prepared by condensing a novel, reactive protected derivative of adriamycinone with reactive intermediates which are 1-halo-2,3,6-trideoxy-3-trifluoroacetamido-4-trifluoroacetoxy-.alpha.-L-lyxo (or arabino) hexopyranoses.
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公开(公告)号：US4020270A
公开(公告)日：1977-04-26
申请号：US650519
申请日：1976-01-19
IPC分类号： C07D309/30 , C07H15/252 , C07H5/06
CPC分类号： C07H15/252 , C07D309/30 , Y02P20/55
摘要： Anthracyclinone glycoside antibiotics including the known antibiotics daunomycin and adriamycin, as well as other, novel glycoside antibiotics of the formula (VIII): ##STR1## wherein WHEN R.sub.1 is hydrogen, R.sub.2 and R.sub.3 are each independently hydrogen, methyl, methoxy, chloro, or bromo; and when R.sub.2 and R.sub.3 are hydrogen, R.sub.1 is methyl, chloro, or bromo and R.sub.4 and R.sub.5 are each independently hydrogen or hydroxy are prepared by an acid catalyzed addition reaction between (a) an anthracyclinone compound of the formula ##STR2## or a dioxolanyl protected derivative thereof (VI) having the formula: ##STR3## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as defined above, and R.sub.6, R.sub.7 and R.sub.8 are independently selected from the group consisting of hydrogen and C.sub.1 -C.sub.4 alkyl; or R.sub.7 and R.sub.8, together with the carbon atom to which they are bound may form a saturated or unsaturated ring of 3-8 carbon atoms and (b) a novel reactive, protected 1,2-unsaturated pyranoid sugar, preferably, 1,2,3,6-tetradeoxy-3-trifluoroacetamido-4-trifluoroacetoxy-L-lyxo-hex-1-enopyranose which forms protected derivatives of said glycoside antibiotics and then removing the protecting groups from said glycoside antibiotics. These antibiotics are useful in the treatment of various human cancers and leukemia such as sarcomas, breast cancer, bronchogenic carcinoma, malignant lymphomas, neuroblastomas, acute leukemia and bladder cancer.
摘要翻译： 蒽环类抗生素包括已知的抗生素道诺霉素和阿霉素，以及其它式（VIII）的新型糖苷抗生素：其中当R1是氢时，R2和R3各自独立地是氢，甲基，甲氧基， 氯或溴; 并且当R 2和R 3为氢时，R 1为甲基，氯或溴，并且R 4和R 5各自独立地为氢或羟基，是通过（a）式（III）的蒽环类化合物之间的酸催化加成反应制备的， 或其具有下式的二氧杂环戊烷基保护的衍生物（VI）：其中R 1，R 2，R 3，R 4和R 5如上所定义，并且R 6，R 7和R 8独立地选自氢 和C 1 -C 4烷基; 或R 7和R 8与它们所连接的碳原子一起可以形成3-8个碳原子的饱和或不饱和的环，和（b）新的反应性保护的1,2-不饱和吡喃糖，优选1,2 ，3,6-四脱氧-3-三氟乙酰氨基-4-三氟乙酰氧基-L-赖摩尔 - 己-1-吡喃糖，其形成所述糖苷抗生素的受保护的衍生物，然后从所述糖苷抗生素中除去保护基团。 这些抗生素可用于治疗各种人类癌症和白血病如肉瘤，乳腺癌，支气管癌，恶性淋巴瘤，神经母细胞瘤，急性白血病和膀胱癌。
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公开(公告)号：US5310752A
公开(公告)日：1994-05-10
申请号：US925408
申请日：1992-08-10
IPC分类号： C07D207/34 , C07D409/12 , A61K31/40 , C07D403/14
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.
摘要翻译： 本发明涉及下列式的分心霉素A类似物：其中n为2,3或4; A是选自以下的任选取代的二价基团：其中Het是五原子或六原子异单环，除了吡咯; 并且其中R 1和R 2中的任一个是氢，而另一个是酰化部分或R 1和R 2都是氢或任选被取代的两个烷基，包括所述化合物的药学上可接受的盐。 本发明的化合物可以是有用的抗肿瘤剂和抗病毒剂。
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公开(公告)号：US5049579A
公开(公告)日：1991-09-17
申请号：US607339
申请日：1990-10-31
IPC分类号： C07D207/34 , C07D409/12
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.
摘要翻译： 本发明涉及下列式的分心霉素A类似物：其中n为2,3或4; A是选自以下的任选取代的二价基团：其中Het是五原子或六原子异单环，除了吡咯; 并且其中R 1和R 2中的任一个是氢，而另一个是酰化部分或R 1和R 2都是氢或任选被取代的两个烷基，包括所述化合物的药学上可接受的盐。 本发明的化合物可以是有用的抗肿瘤剂和抗病毒剂。
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公开(公告)号：US5037970A
公开(公告)日：1991-08-06
申请号：US501869
申请日：1990-03-28
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 compound of the formula ##STR1## 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 hydrolysis 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.
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公开(公告)号：US4965351A
公开(公告)日：1990-10-23
申请号：US430149
申请日：1989-11-01
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 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.
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69.发明授权.beta.-Lactam-containing antibacterial agents and .beta.-lactamase inhibitors 失效含β-内酰胺的抗菌剂和β-内酰胺酶抑制剂
公开(公告)号：US4558042A
公开(公告)日：1985-12-10
申请号：US595336
申请日：1984-03-30
申请人： Maurizio Foglio , Giovanni Franceschi , Cosimo Scarafile , Federico Arcamone , Aurora Sanfilippo
发明人： Maurizio Foglio , Giovanni Franceschi , Cosimo Scarafile , Federico Arcamone , Aurora Sanfilippo
IPC分类号： C07D499/88 , C07D499/00 , A61K31/425
CPC分类号： C07D499/88
摘要： There are disclosed .beta.-lactam-containing compounds of the formula: ##STR1## where R is hydrogen, lower alkyl, trichloroethyl, acetonyl, benzyl, substituted benzyl, phenyl, substituted phenyl, benzidryl or a residue that will undergo metabolic activation "in vivo" and have favorable pharmacokinetic properties; R.sup.1 is a hydrogen atom, lower alkyl, lower alkoxy, cycloalkyl, or hydroxyalkyl, with the alcoholic function of the hydroxyalkyl being free or protected; Z is hydrogen, halogen, hydroxy, amino, carbamoyloxy, mercapto, pyridinium, OR.sup.2, OCOR.sup.2, NHCOR.sup.2, or SR.sup.3 wherein each of R.sup.2 and R.sup.3 is any of lower alkyl, aryl, or a heterocyclic ring, each of which may be substituted or unsubstituted, and n is 0 or 1. The compounds have broad spectrum antibacterial activity and .beta.-lactamase inhibiting activity. Processes for the production of the .beta.-lactam-containing compounds and various intermediates in the production of those compounds are also disclosed.
摘要翻译： 公开了含有β-内酰胺的化合物，其中R为氢，低级烷基，三氯乙基，丙酰基，苄基，取代的苄基，苯基，取代的苯基，苯并或将经历代谢活化的残基。 “并具有有利的药代动力学性质; R1是氢原子，低级烷基，低级烷氧基，环烷基或羟基烷基，其羟基烷基的醇官能团是游离或保护的; Z是氢，卤素，羟基，氨基，氨基甲酰氧基，巯基，吡啶鎓，OR2，OCOR2，NHCOR2或SR3，其中R2和R3各自为低级烷基，芳基或杂环， 未取代的，n为0或1.该化合物具有广谱抗菌活性和β-内酰胺酶抑制活性。 还公开了用于生产含有β-内酰胺的化合物和这些化合物生产中的各种中间体的方法。
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公开(公告)号：US4477444A
公开(公告)日：1984-10-16
申请号：US434509
申请日：1982-10-15
IPC分类号： C07H15/252 , A61K31/70 , C07H15/24
CPC分类号： C07H15/252 , Y02P20/55
摘要： Disclosed is a process for preparing the new antitumor glycosides: 4'-deoxy-3'-epi-daunorubicin and 4'-deoxy-3'-epi-doxorubicin starting from the known 3'-epi-4'-keto-N-trifluoroacetyl-daunorubicin.Reduction of the 4'-keto group with sodium borohydride to the corresponding 4'-hydroxy group, reacting the so obtained intermediate with trifluoromethanesulphonic anhydride followed by treatment with n-tetrabutylammonium iodide, dehalogenated reductively, by treatment with tributyl tin hydride to 4'-deoxy-3'-epi-N-trifluoroacetyl-daunorubicin.A mild alkaline hydrolysis removes the N-protecting group to give 4'-deoxy-3'-epi-daunorubicin which is successively transformed, via its 14-bromo derivative, in its doxorubicin analogue.
摘要翻译： 公开了一种制备新型抗肿瘤糖苷的方法：从已知的3'-表面-4'-酮-n-三磷酸开始制备4'-脱氧-3'-表柔比星和4'-脱氧-3'-表阿霉素， 三氟乙酰柔红霉素。 将4'-酮基用硼氢化钠还原成相应的4'-羟基，使所得中间体与三氟甲磺酸酐反应，然后用正丁基碘化铵处理，还原脱卤，通过用三丁基锡氢化物处理至4'- 脱氧-3'-表N-N-三氟乙酰柔红霉素。 轻度碱性水解除去N-保护基，得到4'-脱氧-3'-表柔比星，其通过其14-溴衍生物在其多柔比星类似物中相继转化。
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