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。

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：US4251516A

公开(公告)日：1981-02-17

申请号：US79132

申请日：1979-09-26

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： A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/7036 ,  A61P31/04 ,  C07H15/224 ,  A61K31/71 ,  C07H15/22

CPC分类号： C07H15/224

摘要： The present invention provides 2-deoxy-3-O-demethyl-fortimcins A and B and the 4-N-acyl and alkyl derivatives thereof, represented by the formula: ##STR1## wherein R is selected from the group consisting of hydrogen, acyl, aminoacyl,diaminoacyl,N-monoloweralkylaminoalkyl,N,N-diloweralkylaminoalkyl, hydroxy-substituted aminoacyl,loweralkyl, aminoloweralkyl, N-monoloweralkylaminoloweralkyl, N,N-diloweralkylaminoloweralkyl and hydroxy-substituted aminoloweralkyl and the pharmaceutically acceptable salts thereof.

公开(公告)号：US4273925A

公开(公告)日：1981-06-16

申请号：US79135

申请日：1979-09-26

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： A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/7036 ,  A61P31/04 ,  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.

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。

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：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。