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11. 发明授权

US4250304A 2-Deoxy-2-substituted fortimicin A and B and derivatives 失效
标题翻译： 2-脱氧-2-取代的fortimicin A和B及其衍生物
公开(公告)号：US4250304A
公开(公告)日：1981-02-10
申请号：US79145
申请日：1979-09-26
申请人： Jerry R. Martin , John S. Tadanier , Paulette Johnson , Alex M. Nadzan
发明人： Jerry R. Martin , John S. Tadanier , Paulette Johnson , Alex M. Nadzan
IPC分类号： C07H15/224 , C07H15/22
CPC分类号： C07H15/224
摘要： Disclosed are 2-deoxy-2-substituted fortimicin A and B derivatives represented by the formula ##STR1## wherein R is hydrogen glycyl, .beta.-alanyl, acetyl, or .beta.-amino lower alkyl, R.sub.1 is hydrogen, amino, azido, halo, glycylamido, .beta.-alanyl amido or 2-O-methanesulfonyl and R.sub.2 is hydrogen or halo and their pharmaceutically acceptable salts. The compounds are active antibacterial agents.
摘要翻译：公开了由式“IMAGE”表示的2-脱氧-2-取代的fortimicin A和B衍生物，其中R是氢甘氨酰，β-丙氨酰基，乙酰基或β-氨基低级烷基，R 1是氢，氨基，叠氮基，卤素，甘氨酰胺基，β-丙氨酰氨基或2-O-甲磺酰基，R2是氢或卤素及其药学上可接受的盐。这些化合物是活性抗菌剂。

12. 发明授权

US4230846A 1,5-Carbamates of fortimicin B and derivatives 失效
标题翻译：富马汀B及其衍生物的1,5-氨基丁酸酯
公开(公告)号：US4230846A
公开(公告)日：1980-10-28
申请号：US79133
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： A 1,5-fortimicin B carbamate represented by the formula: ##STR1## wherein each R is hydrogen or monocyclicaryloxycarbonyl and R.sub.1 is selected from the group consisting of: loweralkyl, hydroxyloweralkyl, hydrogen, aminoloweralkyl, N-loweralkylaminoloweralkyl, N,N-diloweralkylaminoloweralkyl, trihaloalkoxycarbonyl, an amino acid residue and an N-protected amino acid residue and the pharmaceutically acceptable salts thereof.
摘要翻译：由下式表示的1,5-维霉素B氨基甲酸酯：其中每个R是氢或单环酰氧基羰基，R 1选自：低级烷基，羟基低级烷基，氢，氨基低级烷基，N-低级烷基氨基低级烷基，N，N-二低级烷基氨基低级烷基，三卤代烷氧基羰基，氨基酸残基和N-保护的氨基酸残基及其药学上可接受的盐。

13. 发明授权

US4214075A 6'-Epi-fortimicin A and B derivatives 失效
标题翻译： 6'-Epi-fortimicin A和B衍生物
公开(公告)号：US4214075A
公开(公告)日：1980-07-22
申请号：US863004
申请日：1977-12-21
申请人： John S. Tadanier , Jerry R. Martin
发明人： John S. Tadanier , Jerry R. Martin
IPC分类号： C07H15/224 , A61K31/71 , C07H15/22
CPC分类号： C07H15/224
摘要： 6'-Epi-fortimicin A and B derivatives represented by the formula ##STR1## wherein R.sub.1 is hydrogen or loweralkyl, R.sub.2 is hydrogen or loweralkyl and R.sub.3 is selected from the group consisting of hydrogen, loweralkyl, aminoloweralkyl, N-loweralkylaminoloweralkyl, N,N-diloweralkylaminoloweralkyl, aminohydroxyloweralkyl, N-loweralkylaminohydroxyloweralkyl, hydroxyloweralkyl, acyl, aminoacyl, hydroxyacyl, N-monoloweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl or an amino acid residue; the pharmaceutically acceptable salts thereof; intermediates useful in their preparation, compositions employing the compounds; and methods of using the compounds. The compounds are useful as antibiotics.
摘要翻译：其中R 1是氢或低级烷基，R 2是氢或低级烷基，R 3选自氢，低级烷基，氨基低级烷基，N-低级烷基氨基低级烷基，N，N-二烷基氨基低级烷基， N-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，羟基低级烷基，酰基，氨基酰基，羟基酰基，N-单低级烷基氨基酰基，N，N-二低级烷基氨基酰基，羟基取代的酰基或氨基酸残基。其药学上可接受的盐; 用于制备的中间体，使用该化合物的组合物; 和使用该化合物的方法。该化合物可用作抗生素。

14. 发明授权

US4208407A 5-Deoxyfortimicin A, 2,5-dideoxyfortimicin A and the corresponding 4-N-acyl and alkyl fortimicin B derivatives thereof and intermediates therefor 失效
标题翻译： 5-脱氧有益霉素A，2,5-二脱氧有益霉素A及其相应的4-N-酰基和烷基苦味素B衍生物及其中间体
公开(公告)号：US4208407A
公开(公告)日：1980-06-17
申请号：US9638
申请日：1979-02-05
申请人： Ronald E. Carney , Jerry R. Martin , James B. McAlpine , John S. Tadanier
发明人： Ronald E. Carney , Jerry R. Martin , James B. McAlpine , John S. Tadanier
IPC分类号： C07H15/224 , A61K31/71 , C07H15/22
CPC分类号： C07H15/224
摘要： 5-Deoxyfortimicin A, 2,5-dideoxyfortimicin A and the corresponding 4-N-acyl and alkyl fortimicin B derivatives thereof, pharmaceutically acceptable salts thereof, intermediates therefor, and pharmaceutical compositions containing the compounds of this invention. The fortimicin derivatives are represented by the formula: ##STR1## wherein R is selected from the group consisting of acyl, hydroxyacyl, aminoacyl, N-monoloweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxyacyl, hydroxy-substituted aminoacyl or an amino acid residue other than glycyl, loweralkyl, aminoloweralkyl, hydroxyloweralkyl, N-monoloweralkylaminoloweralkyl, N-N-diloweralkylaminoloweralkyl or hydroxy-substituted aminoloweralkyl; R.sub.1 is hydrogen or hydroxy; and R.sub.2 is hydrogen or hydroxy with the limitation that either R.sub.1 and R.sub.2 each are hydrogen or when only one of R.sub.1 or R.sub.2 are hydrogen, R.sub.2 is hydrogen and R.sub.1 is hydroxy and R.sub.1 and R.sub.2 both cannot be hydroxy.
摘要翻译： 5-脱氧有益霉素A，2,5-双脱氧有益霉素A及其相应的4-N-酰基和烷基苦味素B衍生物，其药学上可接受的盐，其中间体和含有本发明化合物的药物组合物。所述有害基因衍生物由下式表示：其中R选自酰基，羟基酰基，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，羟基酰基，羟基取代的氨基酰基或除甘氨酰，低级烷基，氨基低级烷基，羟基低级烷基，N-单低级烷基氨基低级烷基，N，N'-二烯烷基氨基低级烷基或羟基取代的氨基低级烷基; R1是氢或羟基; 并且R 2是氢或羟基，限制在于R 1和R 2各自为氢或当R 1或R 2中只有一个为氢时，R 2为氢且R 1为羟基，且R 1和R 2均不能为羟基。

15. 发明授权

US4196197A 2'N-Acyl and alkyl-6'-N-alkyl- and 6',6'-di-N-alkyl derivatives of fortimicins A and B 失效
标题翻译：苦味素A和B的2'N-酰基和烷基-6'-N-烷基 - 和6'，6'-二-N-烷基衍生物
公开(公告)号：US4196197A
公开(公告)日：1980-04-01
申请号：US863008
申请日：1977-12-21
申请人： John S. Tadanier , Jerry R. Martin
发明人： John S. Tadanier , Jerry R. Martin
IPC分类号： A01N43/14 , C07H15/224 , A61K31/71 , C07H15/22
CPC分类号： C07H15/224
摘要： Novel fortimicin 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; R.sub.1 is loweralkyl, R.sub.2 is hydrogen or lower alkyl; and R.sub.3 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, N,N-diloweralkylaminohydroxyloweralkyl or hydrogen and the pharmaceutically acceptable salts thereof; pharmaceutical compositions containing the compounds; and methods of making and using the compounds. The compounds are useful as antibiotics.
摘要翻译：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，N-二低级烷基氨基羟基低级烷基; R1是低级烷基，R2是氢或低级烷基; 氨基酰基，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-低级烷基氨基羟基低级烷基，N，N-二低级烷基氨基羟基低级烷基或氢及其药学上可接受的盐; 含有这些化合物的药物组合物; 以及制备和使用该化合物的方法。该化合物可用作抗生素。

16. 发明授权

US4183920A 4-N-Acyl, 2'-N-acyl and 4,2'-N,N'-diacylfortimicin E derivatives 失效
标题翻译： 4-N-酰基，2'-N-酰基和4,2'-N，N'-二酰基有益霉素E衍生物
公开(公告)号：US4183920A
公开(公告)日：1980-01-15
申请号：US863010
申请日：1977-12-21
申请人： Paul Kurath , John S. Tadanier , Jerry R. Martin
发明人： Paul Kurath , John S. Tadanier , Jerry R. Martin
IPC分类号： C07H15/224 , A61K31/71 , C07H15/22
CPC分类号： C07H15/224
摘要： 4-N-Acyl, 2'-N-acyl and 4,2' -N,N' -diacylfortimicin E derivatives represented by the formula ##STR1## wherein R is hydrogen, acyl, aminoacyl, N-lower alkylamino acyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl or an amino acid residue; R.sub.1 is hydrogen, acyl, aminoacyl, N-loweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl or an amino acid residue, with the limitation that R cannot be hydrogen when R.sub.1 is hydrogen, and R.sub.1 cannot be hydrogen when R is hydrogen; the pharmaceutically acceptable salts thereof; intermediates therefor; pharmaceutical compositions; and methods of making and using the compounds. The compounds are useful as antibiotics.
摘要翻译：其中R是氢，酰基，氨基酰基，N-低级烷基氨基酰基，N，N-二乙酰基，N，N-二乙酰基和4,2'-N，N' - 二酰基有益霉素E衍生物， N-二卤代烷基氨基酰基，羟基取代的氨基酰基或氨基酸残基; R1是氢，酰基，氨基酰基，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氨基酸残基，但是当R 1为氢时，R不能为氢，当R为氢时，R 1不能为氢 ; 其药学上可接受的盐; 中间体药物组合物; 以及制备和使用该化合物的方法。该化合物可用作抗生素。

17. 发明授权

US4124756A 3-DE-O-Methylfortimicins 失效
标题翻译： 3-DE-O-甲基有益霉素
公开(公告)号：US4124756A
公开(公告)日：1978-11-07
申请号：US754670
申请日：1976-12-27
申请人： Jerry R. Martin , John S. Tadanier
发明人： Jerry R. Martin , John S. Tadanier
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/7036 , A61P31/04 , C07H15/224 , C07H15/22
CPC分类号： C07H15/224
摘要： Described are 3-de-O-methylfortimicins A and B and 4-N-acyl and 4-N-alkyl-3-de-O-methylfortimicin B derivatives, and their preparation, which compounds are useful as antibiotics or as intermediates for preparing other useful derivatives having antibacterial activity. The compounds have the following structural formula ##STR1## wherein R is hydrogen, acyl, aminoacyl, N-monoloweralkylaminoacyl, N.N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl, alkyl, aminoalkyl, N-monoloweralkylaminoalkyl, N.N-diloweralkylaminoalkyl or hydroxy-substituted aminoalkyl and the pharmaceutically acceptable salts thereof, for example, salts formed from hydrochloric, sulfuric, and phosphoric acids.
摘要翻译：描述了3-de-O-甲基有益霉素A和B以及4-N-酰基和4-N-烷基-3-脱-O-甲基有益霉素B衍生物及其制备方法，该化合物可用作抗生素或作为制备中间体其他有用的衍生物具有抗菌活性。该化合物具有以下结构式：其中R是氢，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，羟基取代的氨基酰基，烷基，氨基烷基，N-单低级烷基氨基烷基，NN-二低烷基氨基烷基或羟基取代的氨基烷基其药学上可接受的盐，例如由盐酸，硫酸和磷酸形成的盐。

18. 发明授权

US4319022A 2-O-Substituted sulfonyl derivatives of fortimicin B 失效
标题翻译： fortimicin B的2-O-取代磺酰基衍生物
公开(公告)号：US4319022A
公开(公告)日：1982-03-09
申请号：US131468
申请日：1980-04-27
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 , A61K31/71 , 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。

19. 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。

20. 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。

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