公开(公告)号：US4207415A

公开(公告)日：1980-06-10

申请号：US9637

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 ,  C07H15/22

CPC分类号： C07H15/224

摘要： An improved method for producing the antibiotic 2-deoxyfortimicin A, the method comprising the process of producing said antibiotic directly from fortimicin A in a four step process which results in a 50-60 percent yield of product.

摘要翻译： 一种用于生产抗生素2-脱氧好霉素A的改进方法，该方法包括以四步法直接生产所述抗生素的方法，其导致产物产率为50-60％。

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。

公开(公告)号：US4360666A

公开(公告)日：1982-11-23

申请号：US266030

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

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。

公开(公告)号：US4340727A

公开(公告)日：1982-07-20

申请号：US201651

申请日：1980-10-28

申请人： Jerry R. Martin ,  John S. Tadanier ,  Paulette Johnson

发明人： Jerry R. Martin ,  John S. Tadanier ,  Paulette Johnson

IPC分类号： C07H15/224 ,  C07H15/22

CPC分类号： C07H15/224

摘要： A 1,2-modified fortimicin A or B represented by the formulae I, II and III: ##STR1## wherein R is hydrogen or loweralkyl; and R.sub.1 is selected from the group consisting of hydrogen, loweralkyl, aminoloweralkyl, diaminoloweralkyl, N-lower-alkylaminoloweralkyl, N,N-diloweralkylaminoloweralkyl, hydroxyloweralkyl, amino hydroxyloweralkyl, N-loweralkylaminohydroxyloweralkyl, N-N-diloweralkylaminohydroxyloweralkyl, acyl, aminoacyl, hydroxy-substituted aminoacyl, diaminoacyl, hydroxyacyl, hydroxy-substituted diaminoacyl, N-loweralkylaminoacyl, N, N-diloweralkylaminoacyl, hydroxysubstituted-N-loweralkylaminoacyl and hydroxy-substituted-N, N-diloweralkylaminoacyl, and the pharmaceutically acceptable salts thereof. The compounds are broad spectrum antibiotics.

摘要翻译： 由式I，II和III表示的1,2-改性的fortimicin A或B：其中R是氢或低级烷基; 其中R 1选自氢，低级烷基，氨基低级烷基，二氨基低级烷基，N-低级烷基氨基低级烷基，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， ，二氨基酰基，羟基酰基，羟基取代的二氨基酰基，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N-低级烷基氨基酰基和羟基取代的N，N-二低级烷基氨基酰基及其药学上可接受的盐。 这些化合物是广谱抗生素。

公开(公告)号：US4187298A

公开(公告)日：1980-02-05

申请号：US863012

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'-N-Acyl and alkyl fortimicin B and fortimicin B derivatives, 4,2'-N,N'-diacyl and dialkyl 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, an amino acid residue, hydroxyacyl, 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, intermediates, and are further useful in making moth proofing agents and pickling inhibitors.

摘要翻译： 2-N-酰基和烷基维生素B和fortimicin B衍生物，4,2'-N，N'-二酰基和二烷基衍生物，4-N-酰基-2'-N-烷基和4-N-烷基-2 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，N-二烷基氨基低级烷基，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， 氨基酸残基，羟基酰基，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，N-低级烷基氨基低级烷基氨基甲酰基， ，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。 这些化合物可用作抗生素，中间体，并且还可用于制备防蛀剂和酸洗抑制剂。

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.

公开(公告)号：US4431799A

公开(公告)日：1984-02-14

申请号：US79129

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： A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/7036 ,  A61K31/7042 ,  A61P31/04 ,  C07H15/224 ,  C07H17/00 ,  A61K31/71 ,  C07H17/04

CPC分类号： C07H15/224

摘要： Described is a method for the preparation of 6'-modified fortimicin compounds including 6'-epi fortimicin by converting 1,2-di-N-protected fortimicin B into 4,6'-di-N-substituted alkoxycarbonyl-1,2'-di-N-protected fortimicin B which is further converted to 1,2'-di-substituted fortimicin B-4,5-carbamate, a compound whose substitution pattern is particularly suited to modification at the 6'-amino group and novel compounds thereof.

摘要翻译： 描述了通过将1,2-二-N-保护的fortimicin B转化成4,6'-二-N-取代的烷氧基羰基-1,2'的6'-改性的fortimicin化合物，包括6'-epi fortimicin的方法， -di-N-保护的fortimicin B，其进一步转化为1,2'-二取代的fortimicin B-4,5-氨基甲酸酯，其取代模式特别适于在6'-氨基改性的化合物和新化合物 其中。

公开(公告)号：US4360668A

公开(公告)日：1982-11-23

申请号：US266266

申请日：1981-05-22

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： 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： 由式“IMAGE”表示的2-脱氧有机霉素，A，2-脱氧-4-N-烷基苦味蛋白和2-脱氧-4-N-酰基苦味霉素，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。

公开(公告)号：US4276413A

公开(公告)日：1981-06-30

申请号：US91864

申请日：1979-11-06

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 ,  C07H15/20

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 hydroxysubstituted 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'-二低级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。

公开(公告)号：US4269970A

公开(公告)日：1981-05-26

申请号：US79138

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 ,  C07D413/02

CPC分类号： C07H15/224

摘要： A 1,2-carbamate of fortimicin B and derivatives represented by the formula: ##STR1## wherein: R is hydrogen or monocyclicaryloxycarbonyl, R.sub.1 is hydrogen or monocyclicaryloxycarbonyl; and R.sub.2 is selected from the group consisting of loweralkyl, loweralkoxycarbonyl aminoloweralkyl, hydroxyloweralkyl, hydroxy-substituted aminolowerakyl, an amino acid residue, and N-protected amino acid residue, or when R and R.sub.1 are hydrogen, R.sub.2 can also be hydrogen; and the acid addition salts thereof when R,R.sub.1 or R.sub.2 are hydrogen or an unprotected aminoacid residue.

摘要翻译： 苦味霉素B的1,2-氨基甲酸酯和由下式表示的衍生物：其中：R为氢或单环酰氧基羰基，R 1为氢或单环酰氧基羰基; 并且R 2选自低级烷基，低级烷氧基羰基氨基低级烷基，羟基低级烷基，羟基取代的氨基低官能基，氨基酸残基和N-保护的氨基酸残基，或当R和R 1为氢时，R 2也可为氢; 当R 1，R 2或R 2为氢或未被保护的氨基酸残基时，其酸加成盐。