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    3-deoxy-desmycosin derivatives and process for their preparation
    1.
    发明授权
    3-deoxy-desmycosin derivatives and process for their preparation 失效
    3-脱氧 - 去霉霉素衍生物及其制备方法

    公开(公告)号：US06504035B1

    公开(公告)日：2003-01-07

    申请号：US09959692

    申请日：2002-01-28

    申请人： Amalija Narandja ,  Nevenka Lopotar ,  Marko Djerek ,  Dra{haeck over (z)}en Pavlović

    发明人： Amalija Narandja ,  Nevenka Lopotar ,  Marko Djerek ,  Dra{haeck over (z)}en Pavlović

    IPC分类号： C07D32100

    CPC分类号： C07H17/08

    摘要： The present invention relates to derivatives of 3-deoxy desmycosin of the formula I, wherein, starting from triply protected desmycosin, there are performed an oxidation at C-3 in the first step and then, optionally, a hydrogenation of double bonds and an epoxidation followed by a reductive opening of the oxirane ring. The present invention also relates to derivatives of 3-deoxy-desmycosin of the formula II, wherein in the first step triacetyl desmycosin is hydrogenated and then, via an intermediate mesylate, it is converted to a 2,3-didehydro derivative; or 2,3-didehydro-desmycosin is subjected to epoxidation reactions followed by a reductive opening of the oxirane ring.

    摘要翻译： 本发明涉及式I的3-脱氧去糖霉素衍生物，其中，从三重保护的脱沙霉素开始，在第一步中在C-3进行氧化，然后任选地进行双键氢化和环氧化 随后是环氧乙烷环的还原开口。 本发明还涉及式II的3-脱氧 - 去霉霉素的衍生物，其中在第一步中，将三乙酰基脱沙霉素氢化，然后经由甲磺酸中间体转化为2,3-二脱水衍生物; 或2,3-二脱氢脱硫霉素进行环氧化反应，然后进行环氧乙烷环的还原开口。

    Derivatives of 12,13-Epoxy-tylosin and processes of manufacture thereof
    2.
    发明授权
    Derivatives of 12,13-Epoxy-tylosin and processes of manufacture thereof 失效
    12,13-环氧 - 泰乐菌素的衍生物及其制备方法

    公开(公告)号：US5688924A

    公开(公告)日：1997-11-18

    申请号：US696178

    申请日：1996-08-13

    申请人： Amalija Narandja ,  Nevenka Lopotar

    发明人： Amalija Narandja ,  Nevenka Lopotar

    IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P31/04 ,  B01J23/42 ,  B01J23/44 ,  C07B61/00 ,  C07H17/08 ,  C07D313/00 ,  C07H5/06

    CPC分类号： C07H17/08

    摘要： The invention relates to derivatives of 12,13-epoxy-tylosin, the novel seynthetic antibiotics from tylosin group and the methods of their preparation. According to this invention hydrogenation followed by oximation of 12,13-epoxy-tylosin derivatives yields the following tylosin derivatives: 10,11-dihydro-12,13-epoxy, respectively 10,11-dihydro-12,13-epoxy oxime. Direct oximation of 12,13-epoxy tylosin derivative gives 12,13-epoxy oxime derivatives of tylosin.

    摘要翻译： 本发明涉及12,13-环氧 - 泰乐菌素衍生物，泰乐菌素组合的新型半合成抗生素及其制备方法。 根据本发明，12,13-环氧 - 泰乐菌素衍生物的氢化反应产生以下泰乐菌素衍生物：10,11-二氢-12,13-环氧基，分别为10,11-二氢-12,13-环氧肟。 12,13-环氧泰乐菌素衍生物的直接肟化得到泰乐菌素的12,13-环氧肟衍生物。

    Hydroxy derivatives of tylosin and process for their preparation
    3.
    发明授权
    Hydroxy derivatives of tylosin and process for their preparation 失效
    泰乐菌素的羟基衍生物及其制备方法

    公开(公告)号：US06211348B1

    公开(公告)日：2001-04-03

    申请号：US09393322

    申请日：1999-09-10

    申请人： Amalija Narandja ,  Nevenka Lopotar ,  Zoran Mandić

    发明人： Amalija Narandja ,  Nevenka Lopotar ,  Zoran Mandić

    IPC分类号： C07H1708

    CPC分类号： C07H17/08

    摘要： The present invention relates to 12,13-dihydroxy derivatives of tylosin, new semisynthetic compounds of the macrolide class, and to a process for their preparation. According to the present invention by the oxidation of 13-hydroxy derivative a 12,13-dihydroxy compound is obtained, which can be subsequently subjected to a series of reactions such as oximation, reduction (catalytic, electrochemical) or hydrolysis yielding corresponding dihydro or tetrahydro 12,13-dihydroxy derivatives.

    摘要翻译： 本发明涉及泰乐菌素的12,13-二羟基衍生物，大环内酯类的新的半合成化合物及其制备方法。 根据本发明，通过氧化13-羟基衍生物，得到12,13-二羟基化合物，其随后可进行一系列反应，如肟化，还原（催化，电化学）或水解，产生相应的二氢或四氢 12,13-二羟基衍生物。

    Seco compounds from the class of tylosins
    4.
    发明授权
    Seco compounds from the class of tylosins 失效
    山梨醇化合物来自泰乐菌素类

    公开(公告)号：US5962661A

    公开(公告)日：1999-10-05

    申请号：US114514

    申请日：1998-07-14

    申请人： Nevenka Lopotar ,  Amalija Narandja ,  Zoran Mandic

    发明人： Nevenka Lopotar ,  Amalija Narandja ,  Zoran Mandic

    IPC分类号： C07H17/08 ,  A61K31/70 ,  C07H15/04 ,  C07H17/00 ,  C07H15/00

    CPC分类号： C07H15/04 ,  C07H17/00

    摘要： Seco compounds from a class of tylosins represented by the formula I whereinR stands for H or CH.sub.3,R.sup.1 stands for H, CH.sub.3, C.sub.1 -C.sub.3 acyl or aryl sulfonyl,R.sup.2 stands for H and R.sup.3 stands for NH.sub.2 or OH, or R.sup.2 and R.sup.3 together stand for .dbd.O or .dbd.NOH,R.sup.4 stands for H or C.sub.1 -C.sub.3 acyl,and the line - - - stands for a double or a single bond,and to a process for their preparation are provided.Oximation of 4'-demicarosyl-8a-aza-8a-homorelymycin causes breaking of the lactam to obtain a seco compound. The seco compound can be subjected to reductive N-alkylation or to conversion of the hydroxyimino group into a keto group and then optionally to N- or N,O-acylation, a catalytical hydrogenation of the double bond or a reduction of the ketone or a reduction of the hydroxyimino group into an amino group.

    摘要翻译： 由式I表示的一类泰乐菌素的Seco化合物，其中R代表H或CH3，R1代表H，CH3，C1-C3酰基或芳基磺酰基，R2代表H，R3代表NH2或OH或R2和 R3一起代表= O或= NOH，R4代表H或C1-C3酰基，线 - - 代表双键或单键，并提供其制备方法。 4'-二去甲酰基-8a-氮杂-8a-茂霉霉素的肟化引起内酰胺的破坏以获得seco化合物。 可以对仲式化合物进行还原N-烷基化或将羟基亚氨基转化为酮基，然后任选地进行N-或N，O-酰化，双键的催化氢化或酮的还原或 将羟基亚氨基还原成氨基。

    Polyhydro derivatives of tylosine and process for their preparation
    5.
    发明授权
    Polyhydro derivatives of tylosine and process for their preparation 失效
    泰乐菌素的多羟基衍生物及其制备方法

    公开(公告)号：US5922684A

    公开(公告)日：1999-07-13

    申请号：US959306

    申请日：1997-10-28

    申请人： Amalija Narandja ,  Nevenka Lopotar

    发明人： Amalija Narandja ,  Nevenka Lopotar

    IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P31/04 ,  C07H17/08 ,  A61K71/31

    CPC分类号： C07H17/08

    摘要： The invention relates to 13-hydroxy-tylosine derivatives, novel semisynthetic antibiotics from the class of macrolides, and to a process for the preparation thereof. According to the present invention by a reductive opening of the oxirane ring of tylosine 13-hydroxy compounds are obtained, which are then subjected to a hydrogenation of the double bond and then 13-hydroxy dihydro or tetrahydro compounds are subjected to an oximation reaction or 13-hydroxy oximes are subjected to the hydrogenation of the double bond.

    摘要翻译： 本发明涉及13-羟基 - 泰乐菌素衍生物，大环内酯类的新型半合成抗生素及其制备方法。 根据本发明，得到泰乐菌素13-羟基化合物的环氧乙烷环的还原开口，然后进行双键氢化，然后使13-羟基二氢或四氢化合物进行肟化反应或13 - 羟基肟进行双键的氢化。

    Metal complexes of N-methyl-11-aza-10-deoxo-10-dihydro-erythromycin A or 11-aza-10-deoxo-10-dihydro-erythromycin A, method for the manufacture thereof and their use in the manufacture of pharmaceuticals
    8.
    发明授权
    Metal complexes of N-methyl-11-aza-10-deoxo-10-dihydro-erythromycin A or 11-aza-10-deoxo-10-dihydro-erythromycin A, method for the manufacture thereof and their use in the manufacture of pharmaceuticals 失效
    N-甲基-11-氮杂-10-脱氧-10-二氢 - 红霉素A或11-氮杂-10-脱氧-10-二氢 - 红霉素A的金属络合物，其制造方法及其在药物制造中的应用

    公开(公告)号：US4963528A

    公开(公告)日：1990-10-16

    申请号：US94555

    申请日：1987-09-09

    申请人： Zlatko Vajtner ,  Nevenka Lopotar ,  Slobodan Djokic

    发明人： Zlatko Vajtner ,  Nevenka Lopotar ,  Slobodan Djokic

    IPC分类号： C07F1/08 ,  A61K31/295 ,  A61K31/315 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P31/04 ,  C07H17/00 ,  C07H17/08

    CPC分类号： C07H17/00

    摘要： New 2:1 complexes of N-methyl-11-aza-10-deoxo-10-dihydroerythromycin A or 11-aza-10-deoxo-10-dihydroerythromycin A with bivalent metals chosen form the group comprising Cu.sup.+2, Zn.sup.+2, Co.sup.+2, Ni.sup.+2 and Ca.sup.+2, a process for their manufacture and their use in the manufacture of antibiotically active pharmaceuticals.New 2:1 complexes of N-methyl-11-aza-10-deoxo-10-dihydroerythromycin A or 11-aza-10-deoxo-10-dihydroerythromycin A with bivalent metals chosen from the group comprising Cu.sup.+2, Zn.sup.+2, Co.sup.+2, Ni.sup.+2 and Ca.sup.+2 are made by reacting N-methyl-11-aza-10-deoxo-10-dihydroerythromycin A or 11-aza-10-deoxo-10-dihydroerythromycin A in its free base form or in its water-soluble salt form with salts of said bivalent metals. The compounds possess antibiotic activity.

    摘要翻译： 新型的2:1配合物的N-甲基-11-氮杂-10-脱氧-10-二氢红霉素A或11-氮杂-10-脱氧-10-二氢红霉素A与二价金属组成，选自Cu +2，Zn + 2 ，Co + 2，Ni + 2和Ca + 2，其制造方法及其在制备抗生物活性药物中的应用。 新的2:1络合物的N-甲基-11-氮杂-10-脱氧-10-二氢红霉素A或11-氮杂-10-脱氧-10-二氢红霉素A与选自Cu +2，Zn + 2的二价金属 通过N-甲基-11-氮杂-10-脱氧-10-二氢红霉素A或11-氮杂-10-脱氧-10-二氢红霉素A以游离碱形式反应制备Co + 2，Ni + 2和Ca + 或以其所述二价金属的盐的水溶性盐形式。 该化合物具有抗生素活性。