2-Deoxyfortimicin A, 4-N-alkyl and 4-N-acyl-2-deoxyfortimicin B
derivatives and intermediates therefor
    1.
    发明授权
    2-Deoxyfortimicin A, 4-N-alkyl and 4-N-acyl-2-deoxyfortimicin B derivatives and intermediates therefor 失效
    2-脱氧有益霉素A,4-N-烷基和4-N-酰基-2-脱氧有机霉素B衍生物及其中间体

    公开(公告)号:US4360666A

    公开(公告)日:1982-11-23

    申请号:US266030

    申请日:1981-05-22

    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。

    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
    2.
    发明授权
    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 失效
    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-N-烷基-2'- -acyl fortimicin B衍生物

    公开(公告)号:US4187298A

    公开(公告)日:1980-02-05

    申请号:US863012

    申请日:1977-12-21

    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。

    2-O-Methanesulfonylfortimicin B
    3.
    发明授权
    2-O-Methanesulfonylfortimicin B 失效
    2-O-甲磺酰基有益霉素B

    公开(公告)号:US4360668A

    公开(公告)日:1982-11-23

    申请号:US266266

    申请日:1981-05-22

    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。

    Fortimicin intermediates for producing 2-deoxyfortimicins
    4.
    发明授权
    Fortimicin intermediates for producing 2-deoxyfortimicins 失效
    用于生产2-脱氧舒缓素的富咪咪嗪中间体

    公开(公告)号:US4276413A

    公开(公告)日:1981-06-30

    申请号:US91864

    申请日:1979-11-06

    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。

    3-De-O-methyl-2-N-acyl and alkyl fortimicins A and B
    5.
    发明授权
    3-De-O-methyl-2-N-acyl and alkyl fortimicins A and B 失效
    3-脱-O-甲基-2-N-酰基和烷基fortimicins A和B

    公开(公告)号:US4187297A

    公开(公告)日:1980-02-05

    申请号:US863014

    申请日:1977-12-21

    CPC分类号: C07H15/224

    摘要: 3-De-O-methyl-2'-N-acyl and alkyl 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 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, hydrogen; the pharmaceutically acceptable salts thereof; pharmaceutical compositions containing the compounds; and methods of making and using the compounds. The compounds are 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,羟基取代的氨基酰基,羟基酰基,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,N,N-二烷基氨基羟基低级烷基。 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,氢; 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。 这些化合物是抗生素。

    2-Deoxy-2'-N-acyl and alkyl fortimicins A and B
    8.
    发明授权
    2-Deoxy-2'-N-acyl and alkyl fortimicins A and B 失效
    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

    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。

    (1,2',6'-Tri-N-(2-O-methanesulfonylsalicylidine)-4,5-(2-O-methanesulfonyl
salicylaldehyde) oxazolidine-2-O-methanesulfonylfortimicin B
    9.
    发明授权
    (1,2',6'-Tri-N-(2-O-methanesulfonylsalicylidine)-4,5-(2-O-methanesulfonyl salicylaldehyde) oxazolidine-2-O-methanesulfonylfortimicin B 失效
    (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

    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。