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1. 发明授权

US4155902A 4-N-acylfortimicin B derivatives and the chemical conversion of fortimicin B to fortimicin A 失效
公开(公告)号：US4155902A
公开(公告)日：1979-05-22
申请号：US888085
申请日：1978-03-20
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： C07D309/14 , A61K31/35 , A61K31/351 , A61K31/415 , A61P31/04 , C07D405/12 , C07H15/224 , C07C103/52
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.

2. 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。

3. 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。

4. 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.

5. 发明授权

US4231924A 4-N-Acylfortimicin B derivatives and the chemical conversion of fortimicin B to fortimicin A 失效
标题翻译： 4-N-酰基苦霉素B衍生物和fortimicin B对fortimicin A的化学转化
公开(公告)号：US4231924A
公开(公告)日：1980-11-04
申请号：US2436
申请日：1979-01-10
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 , C07H15/22
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-monoloweralkylminoacyl, 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：本发明提供了结构式为“IMAGE”的4-N-酰基苦味霉素B衍生物，其中R为酰基，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，羟基取代的酰基酰基或下式的取代的酰基酰基，其中R 1为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。

6. 发明授权

US4188319A 4-N-Acylfortimicin B derivatives and the chemical conversion of fortimicin B to fortimicin A 失效
标题翻译： 4-N-酰基苦霉素B衍生物和fortimicin B对fortimicin A的化学转化
公开(公告)号：US4188319A
公开(公告)日：1980-02-12
申请号：US3053
申请日：1979-01-12
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
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。

7. 发明授权

US4338308A 4-N-.beta.-Lysyl-2'-N-des-.beta.-lysyl antibiotic AX-127B-1 and the pharmaceutically acceptable salts thereof 失效
标题翻译： 4-N-β-赖氨酰-2'-N-des-β-赖氨酰基抗生素AX-127B-1及其药学上可接受的盐
公开(公告)号：US4338308A
公开(公告)日：1982-07-06
申请号：US205814
申请日：1980-11-10
申请人： Paul Kurath , Earl E. C. Fager
发明人： Paul Kurath , Earl E. C. Fager
IPC分类号： C07H15/224 , C12P19/48 , A61K31/71 , C07H15/22
CPC分类号： C07H15/224 , C12P19/48
摘要： 4-N-Lysyl-2'-N-des-.beta.-lysyl antibiotic AX-127B-1 and the pharmaceutically acceptable salts thereof. The compounds are useful as intermediates in the preparation of 3-O-demethyl 4-N-lysyl-2'-N-des-.beta.-lysyl antibiotic AX-127B-1 and as a broad spectrum antibacterial agents.
摘要翻译： 4-N-赖氨酰-2'-N-des-β-lysyl抗生素AX-127B-1及其药学上可接受的盐。该化合物可用作制备3-O-去甲基4-N-赖氨酰-2'-N-des-β-lysyl抗生素AX-127B-1和广谱抗菌剂的中间体。

8. 发明授权

US4091032A 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：US4091032A
公开(公告)日：1978-05-23
申请号：US725829
申请日：1976-09-23
申请人： John Soloman Tadanier , Jerry Roy Martin , Paul Kurath
发明人： John Soloman Tadanier , Jerry Roy Martin , Paul Kurath
IPC分类号： C07D309/14 , A61K31/35 , A61K31/351 , A61K31/415 , A61P31/04 , C07D405/12 , C07H15/224 , 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。

9. 发明授权

US4338309A 4',5'-Dihydro-antibiotic AX-127B-1; 2'-N-des-.beta.-lysyl-4',5'-dihydro-antibiotic AX-127B-1; and 4-N-derivatives thereof 失效
标题翻译： 4'，5'-二氢抗菌素AX-127B-1; 2-N-des-β-lysyl-4'，5'-二氢抗生素AX-127B-1; 及其4-N-衍生物
公开(公告)号：US4338309A
公开(公告)日：1982-07-06
申请号：US205815
申请日：1980-11-10
申请人： Paul Kurath
发明人： Paul Kurath
IPC分类号： C07H15/224 , C12P19/48 , A61K31/71 , C07H15/22
CPC分类号： C07H15/224 , C12P19/48
摘要： 4',5'-Dihydro-antibiotic AX-127B-1, 2'-N-des-.beta.-lysyl-4',5'-dihydro-antibiotic AX-127B-1, the 4-N-acyl and alkyl derivatives thereof and their pharmaceutically acceptable salts. The compounds are useful as antibiotics and as intermediates for preparing the corresponding 3-O-demethyl derivatives of antibiotic AX-127B-1.
摘要翻译： 4'，5'-二氢抗生素AX-127B-1,2-N-des-β-lysyl-4'，5'-二氢抗生素AX-127B-1，4-N-酰基和烷基衍生物及其药学上可接受的盐。该化合物可用作抗生素，也可用作制备抗生素AX-127B-1的相应3-O-去甲基衍生物的中间体。

10. 发明授权

US4338307A 2'-N-Des-.beta.-lysyl antibiotic AX-127B-1 and 4-N-acyl and alkyl derivatives thereof 失效
标题翻译： 2-N-Des-β-lysyl抗生素AX-127B-1和4-N-酰基及其烷基衍生物
公开(公告)号：US4338307A
公开(公告)日：1982-07-06
申请号：US205813
申请日：1980-11-10
申请人： Paul Kurath
发明人： Paul Kurath
IPC分类号： C07H15/224 , C12P19/48 , A61K31/71 , C07H15/22
CPC分类号： C07H15/224 , C12P19/48
摘要： 2'-N-Des-.beta.-lysyl antibiotic AX-127B-1 and the 4-N-acyl and alkyl derivatives thereof. The compounds are useful as intermediates in the preparation of 3-O-demethyl antibiotic AX-127B-1 and its derivatives. 2'-N-des-.beta.-lysyl antibiotic AX-127B-1 is also useful as a broad spectrum antibacterial agent.
摘要翻译： 2-N-Des-β-赖氨酰基抗生素AX-127B-1及其4-N-酰基及其烷基衍生物。该化合物可用作制备3-O-脱甲基抗生素AX-127B-1及其衍生物的中间体。 2'-N-去β-赖氨酸抗生素AX-127B-1也可用作广谱抗菌剂。

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