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21. 发明授权

US4317904A 1,2-Epiminofortimicin B 失效
标题翻译： 1,2-二亚麻黄素B
公开(公告)号：US4317904A
公开(公告)日：1982-03-02
申请号：US131147
申请日：1979-04-27
申请人： Jerry R. Martin , John S. Tadanier , Paulette Collum
发明人： Jerry R. Martin , John S. Tadanier , Paulette Collum
IPC分类号： C07H15/224 , C07H15/22
CPC分类号： C07H15/224
摘要： A new fortimicin antibiotic, 2-deoxyfortimicin B, intermediates useful in the preparation of the compound, methods of making and using the compound and compositions containing 2-deoxyfortimicin B.
摘要翻译：一种新的fortimicin抗生素，2-脱氧好坏疽蛋白B，可用于制备化合物的中间体，制备和使用该化合物的方法和含有2-脱氧好坏疽蛋白B的组合物。

22. 发明授权

US4252972A Fortimicin B-1,2:4,5-bis-carbamates 失效
标题翻译： Fortimicin B-1,2：4,5-双 - 氨基甲酸酯
公开(公告)号：US4252972A
公开(公告)日：1981-02-24
申请号：US79136
申请日：1979-09-26
申请人： John S. Tadanier , Jerry R. Martin
发明人： John S. Tadanier , Jerry R. Martin
IPC分类号： C07H15/224
CPC分类号： C07H15/224
摘要： 2',6'-Di-N-benzyloxycarbonylfortimicin B-1,2:4,5-bis-carbamate and fortimicin B-1,2:4,5-bis-carbamate and its salt are provided by the present invention. The compound is represented by the formula ##STR1## wherein each R is either hydrogen or benzyloxycarbonyl The bis-carbamate is useful as in intermediate in the preparation of fortamine bis-carbamate, which in turn is useful as an intermediate in the preparation of aminoglycoside antibiotics via glycosidation with suitably protected sugar moieties.
摘要翻译： 2'，6'-二-N-苄氧基羰基有益霉素B-1,2：4,5-双 - 氨基甲酸酯和有害基因B-1,2：4,5-双氨基甲酸酯及其盐由本发明提供。该化合物由式“IMAGE”表示，其中每个R是氢或苄氧基羰基。双 - 氨基甲酸酯可用作制备二氨基甲酸苯胺甲酯的中间体，其又可用作制备氨基糖苷类抗生素的中间体通过具有适当保护的糖部分的糖基化。

23. 发明授权

US4232147A 4-N-Acylfortimicin B-1,5-carbamates 失效
标题翻译： 4-N-辛酰苦霉素B-1,5-氨基甲酸酯
公开(公告)号：US4232147A
公开(公告)日：1980-11-04
申请号：US79143
申请日：1979-09-26
申请人： John S. Tadanier , Jerry R. Martin
发明人： John S. Tadanier , Jerry R. Martin
IPC分类号： C07H15/224 , C07H17/00
CPC分类号： C07H15/224
摘要： 4-N-acylfortimicin B-1,5-carbamates represented by the formula ##STR1## wherein R is acyl and R.sub.1 is hydrogen or benzyloxycarbonyl.
摘要翻译：由式表示的4-N-酰基有益霉素B-1,5-氨基甲酸酯，其中R是酰基，R 1是氢或苄氧基羰基。

24. 发明授权

US4176178A 2-Deoxy-2'-N-acyl and alkyl fortimicins A and B 失效
标题翻译： 2-脱氧-2'-N-酰基和烷基苦味素A和B
公开(公告)号：US4176178A
公开(公告)日：1979-11-27
申请号：US863011
申请日：1977-12-21
申请人： Jerry R. Martin , John S. Tadanier , Paulette Collum
发明人： Jerry R. Martin , John S. Tadanier , Paulette Collum
IPC分类号： C07H15/224 , A61K31/71 , C07H15/22
CPC分类号： C07H15/224
摘要： 2-Deoxy-2'-N-acyl and alkyl fortimicin B and derivatives, 4,2'-N,N'-diacyl and dialkyl fortimicin B derivatives, 4-N-acyl-2'-N-alkyl- and 4-N-alkyl-2'-N-acyl fortimicin B derivatives represented by the formula ##STR1## wherein R is acyl, aminoacyl, N-monoloweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl, hydroxyacyl, an amino acid residue, loweralkyl, aminoloweralkyl, hydroxyloweralkyl, N-loweralkylaminoloweralkyl, N,N-diloweralkylaminoloweralkyl, aminohydroxyloweralkyl, N-loweralkylaminohydroxyloweralkyl or N,N-diloweralkylaminohydroxyloweralkyl; and R.sub.1 is acyl, aminoacyl, N-monoloweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl, hydroxyacyl, an amino acid residue, loweralkylaminoloweralkyl, hydroxyloweralkyl, N-loweralkylaminoloweralkyl, N,N-diloweralkylaminoloweralkyl, aminohydroxyloweralkyl, N-loweralkylaminohydroxyloweralkyl, N,N-diloweralkylaminohydroxyloweralkyl, hydrogen; and the pharmaceutically acceptable salts therefor, pharmaceutical compositions containing the compounds and methods of making and using the compounds. The compounds of this invention are useful as antibiotics.
摘要翻译： 2-脱氧-2'-N-酰基和烷基苦味蛋白B及其衍生物，4,2'-N，N'-二酰基和二烷基苦味蛋白B衍生物，4-N-酰基-2'-N-烷基 - 和4- 其中R是酰基，氨基酰基，N-单低级烷基氨基酰基，N，N-二低级烷基氨基酰基，羟基取代的酰基酰基，羟基酰基，氨基酸残基，低级烷基，氨基低级烷基，羟基低级烷基，N-低级烷基氨基低级烷基，N，N-二低级烷基氨基低级烷基，氨基羟基低级烷基，N-低级烷基氨基羟基低级烷基或N，并且R 1是酰基，氨基酰基，N-单低级烷基氨基酰基，N，N-二低级烷基氨基酰基，羟基取代的酰基酰基，羟基酰基，氨基酸残基，低级烷基氨基低级烷基，羟基低级烷基，N-低级烷基氨基低级烷基，N，N-二烷基氨基低级烷基，氨基羟基低级烷基，N-低级烷基氨基羟基低级烷基，N-二烷基氨基羟基低级烷基，氢; 及其药学上可接受的盐，含有该化合物的药物组合物和制备和使用该化合物的方法。本发明的化合物可用作抗生素。

25. 发明授权

US4174312A 4-N-acylfortimicin B derivatives and the chemical conversion of fortimicin B to fortimicin A 失效
标题翻译： 4-N-酰基福替霉素B衍生物和fortimicin B对fortimicin A的化学转化
公开(公告)号：US4174312A
公开(公告)日：1979-11-13
申请号：US956752
申请日：1978-11-01
申请人： John S. Tadanier , Jerry R. Martin , Paul Kurath
发明人： John S. Tadanier , Jerry R. Martin , Paul Kurath
IPC分类号： C07H15/224 , C07C103/52 , A61K37/00 , C07D309/22
CPC分类号： C07H15/224
摘要： This invention provides 4-N-acylfortimicin B derivatives of the structure ##STR1## wherein R is acyl, aminoacyl, N-monoloweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl, or substituted aminoacyl of the formula ##STR2## where R.sup.1 is an acyl radical derived from an amino acid or a short peptide, and the pharmaceutically acceptable salts thereof.The compounds are useful as intermediates for preparing 4-N-alkyl or substituted alkylfortimicin B derivatives. In addition to their utility as intermediates, some of the compounds of this invention are also useful as antimicrobial agents.
摘要翻译：本发明提供了结构为“IMAGE”的4-N-酰基苦味霉素B衍生物，其中R是酰基，氨基酰基，N-单低级烷基氨基酰基，N，N-二低级烷基氨基酰基，羟基取代的酰基酰基或下式的取代的酰基酰基，其中R1是衍生自氨基酸或短肽的酰基及其药学上可接受的盐。该化合物可用作制备4-N-烷基或取代的烷基富霉菌素B衍生物的中间体。除了作为中间体的作用外，本发明的一些化合物也可用作抗微生物剂。

26. 发明授权

US4173564A 4-N-acylfortimicin B derivatives and the chemical conversion of fortimicin B to fortimicin A 失效
公开(公告)号：US4173564A
公开(公告)日：1979-11-06
申请号：US956751
申请日：1978-11-01
申请人： John S. Tadanier , Jerry R. Martin , Paul Kurath
发明人： John S. Tadanier , Jerry R. Martin , Paul Kurath
IPC分类号： C07H15/224 , C07C103/52 , A61K37/00 , C07D309/22
CPC分类号： C07H15/224
摘要： This invention provides 4-N-acylfortimicin B derivatives of the structure ##STR1## wherein R is acyl, aminoacyl, N-monoloweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl, or substituted aminoacyl of the formula ##STR2## where R.sup.1 is an acyl radical derived from an amino acid or a short peptide, and the pharmaceutically acceptable salts thereof.The compounds are useful as intermediates for preparing 4-N-alkyl or substituted alkylfortimicin B derivatives. In addition to their utility as intermediates, some of the compounds of this invention are also useful as antimicrobial agents.

27. 发明授权

US4360667A (1,2',6'-Tri-N-(2-O-methanesulfonylsalicylidine)-4,5-(2-O-methanesulfonyl salicylaldehyde) oxazolidine-2-O-methanesulfonylfortimicin B 失效
标题翻译：（1,2'，6'-三-N-（2-O-甲磺酰基水杨基）-4,5-（2-O-甲磺酰水杨醛）恶唑烷-2-基 - 甲磺酰基有益霉素B
公开(公告)号：US4360667A
公开(公告)日：1982-11-23
申请号：US266031
申请日：1981-05-22
申请人： John S. Tadanier , Jerry R. Martin , Paulette Collum
发明人： John S. Tadanier , Jerry R. Martin , Paulette Collum
IPC分类号： C07H15/224 , C07H15/22 , A61K31/71
CPC分类号： C07H15/224
摘要： 2-Deoxyfortimicin A, 2-deoxy-4-N-alkyl fortimicins and 2-deoxy-4-N-acyl fortimicins represented by the formula ##STR1## wherein R is selected from the group consisting of acyl, aminoacyl, N-monoloweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl, an amino acid residue, hydroxyacyl, loweralkyl, aminoloweralkyl, N-monoloweralkylaminoloweralkyl, hydroxyloweralkyl, N-N-diloweralkylaminoloweralkyl or hydroxy-substituted aminoloweralkyl, and the pharmaceutically acceptable salts thereof; intermediates therefor; and pharmaceutical compositions containing the compounds of this invention.
摘要翻译： 2-脱氧有益霉素A，2-脱氧-4-N-烷基苦味蛋白和由式“IMAGE”表示的2-脱氧-4-N-酰基酪氨酸，其中R选自酰基，氨基酰基，N-单低级烷基氨基酰基， N，N-二烷基氨基酰基，羟基取代的酰基酰基，氨基酸残基，羟基酰基，低级烷基，氨基低级烷基，N-单低级烷基氨基低级烷基，羟基低级烷基，N，N-二烷基氨基低级烷基或羟基取代的氨基低级烷基。中间体和含有本发明化合物的药物组合物。

28. 发明授权

US4331804A 2-Epi-fortimicin A and derivatives 失效
标题翻译： 2-Epi-fortimicin A及其衍生物
公开(公告)号：US4331804A
公开(公告)日：1982-05-25
申请号：US079130
申请日：1979-09-26
申请人： John S. Tadanier , Robert Hallas , Jerry R. Martin
发明人： John S. Tadanier , Robert Hallas , Jerry R. Martin
IPC分类号： C07H15/224 , A61K31/71 , C07H15/22
CPC分类号： C07H15/224
摘要： What is described is 2-epi-fortimicin A, 2-epi-fortimicin B or a 2-epi-fortimicin B derivative represented by the formula: ##STR1## wherein R.sub.1 is hydrogen or loweralkyl; R.sub.2 is hydrogen or hydroxy; R.sub.3 is methyl or hydrogen; and R.sub.4 is selected from the group consisting of hydrogen, loweralkyl, aminoloweralkyl, diaminoloweralkyl, N-loweralkylaminoalkyl, N,N-diloweralkylaminoloweralkyl, hydroxyloweralkyl, aminohydroxyloweralkyl, N-loweralkylaminohydroxyloweralkyl, N,N-diloweralkylaminohydroxyloweralkyl, acyl of the formula ##STR2## wherein R.sub.5 is loweralkyl, aminoacyl, diaminoacyl, hydroxyacyl, N-loweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl or an amino acid residue other than those defined above and the pharmaceutically acceptable salts thereof useful in the treatment of infections.
摘要翻译：描述的是2-epi-fortimicin A，2-epi-fortimicin B或由下式表示的2-epi-fortimicin B衍生物：其中R 1是氢或低级烷基; R2是氢或羟基; R3是甲基或氢; 并且R 4选自氢，低级烷基，氨基低级烷基，二氨基低级烷基，N-低级烷基氨基烷基，N，N-二低级烷基氨基低级烷基，羟基低级烷基，氨基羟基低级烷基，N-低级烷基氨基羟基低级烷基，N，N-二烷基氨基羟基低级烷基，式是低级烷基，氨基酰基，二氨基酰基，羟基酰基，N-低级烷基氨基酰基，N，N-二低级烷基氨基酰基，羟基取代的氨基酰基或除上述定义之外的氨基酸残基及其可用于治疗感染的药学上可接受的盐。

29. 发明授权

US4273924A 2-O-Hydrocarbonsulfonyl-4,5-oxazolidine fortimicin B derivatives 失效
标题翻译： 2-O-烃基磺酰基-4,5-恶唑烷fortimicin B衍生物
公开(公告)号：US4273924A
公开(公告)日：1981-06-16
申请号：US71344
申请日：1979-04-27
申请人： Jerry R. Martin , John S. Tadanier , Paulette Collum
发明人： Jerry R. Martin , John S. Tadanier , Paulette Collum
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/7036 , A61P31/04 , C07H15/224 , C07H15/22
CPC分类号： C07H15/224 , Y02P20/55
摘要： A new fortimicin antibiotic, 2-deoxyfortimicin B, intermediates useful in the preparation of the compound, methods of making and using the compound and compositions containing 2-deoxyfortimicin B.
摘要翻译：一种新的fortimicin抗生素，2-脱氧好坏疽蛋白B，可用于制备化合物的中间体，制备和使用该化合物的方法和含有2-脱氧好坏疽蛋白B的组合物。

30. 发明授权

US4263429A 1,2,6-Tri-N-benzyloxycarbonylfortimicin B-4,5-carbamate and 1,2,6-tri-N-acetylfortimicin B-4,5-carbamate 失效
标题翻译： 1,2,6-三-N-苄氧基羰基有益霉素B-4,5-氨基甲酸酯和1,2,6-三-N-乙酰有益霉素B-4,5-氨基甲酸酯
公开(公告)号：US4263429A
公开(公告)日：1981-04-21
申请号：US79137
申请日：1979-09-26
申请人： John S. Tadanier , Jerry R. Martin
发明人： John S. Tadanier , Jerry R. Martin
IPC分类号： C07H15/224 , C07H15/22
CPC分类号： C07H15/224
摘要： A fortimicin intermediate selected from the group consisting of 1,2',6'-tri-N-benzyloxycarbonylfortimicin B-4,5-carbamate and 1,2',6'-tri-N-acetylfortimicin A-4,5-carbamate. The compounds are useful as intermediates in the preparation of 2-epi-fortimicin B.
摘要翻译：选自1,2'，6'-三-N-苄氧基羰基有益霉素B-4,5-氨基甲酸酯和1,2'，6'-三-N-乙酰有益霉素A-4,5-氨基甲酸酯的迷迭香碱中间体。该化合物可用作制备2-epi-fortimicin B的中间体。

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