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    Seco compounds from the class of tylosins
    1.
    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。

    2-bromo-and derivatives of 3-bromo-and 3,3-dibromo-4-oxo-azetidines, processes for the preparation thereof and use thereof
    5.
    发明授权
    2-bromo-and derivatives of 3-bromo-and 3,3-dibromo-4-oxo-azetidines, processes for the preparation thereof and use thereof 失效
    3-溴 - 和3,3-二溴-4-氧代 - 氮杂环丁烷的2-溴衍生物，其制备方法及其用途

    公开(公告)号：US5847119A

    公开(公告)日：1998-12-08

    申请号：US624919

    申请日：1996-03-27

    申请人： Irena Lukic

    发明人： Irena Lukic

    IPC分类号： A61K31/395 ,  A61K31/397 ,  A61P31/04 ,  A61P35/00 ,  C07D201/02 ,  C07D205/08

    CPC分类号： A61K31/395 ,  C07D205/08 ,  Y02P20/55

    摘要： Novel 2-bromo- and 2-nitroxy derivatives of 3-bromo- and 3-dibromo-4-oxo-azetidines, to processes for the preparation thereof and to the use thereof are provided. The azetidines of the present invention have the formula I ##STR1## wherein R.sup.1 is hydrogen or bromine, R.sup.2 is hydrogen or bromine, wherein at least one of R.sup.1 or R.sup.2 is bromine, R.sup.3 is hydrogen; Me.sub.2 --C.dbd.C--COOR.sup.4 wherein R.sup.4 is hydrogen, methyl, benzyl or some other carboxy-protective group, and X is bromine or nitroxy group (--ONO.sub.2). According to the invention 2-bromo- and 2-nitroxy derivatives of 3-bromo- and 3-dibromo-4-oxo-azetidines are prepared by reacting derivatives of protected penicillanic acid 1,1-dioxides with DBN reactant (1,5-diazabicyclo/3.4.0/non-5-ene) and then the obtained DBN salt of sulfinic acid or isolated sulfinic acid is treated with thionyl chloride and, after eliminating thionyl chloride by evaporation, the obtained residue is passed through a silica gel column with methylene chloride or some other solvent as eluant or the obtained residue is dissolved in tetrahydrofuran or some other suitable solvent and treated with tetrabutyl ammonium bromide and after the treatment a derivative of 2-bromo, 3-bromo or 2-bromo-3,3-dibromo-4-oxo-azetidine is isolated, which derivative may be subjected to a reaction with silver nitrate in 2-propanol and, after the treatment of the reaction mixture, derivatives of 2-nitroxy-,3-bromo- or 2-nitroxy-3,3-dibromo-4-oxo-azetidine are isolated. The obtained substances are useful intermediates in the syntheses of beta lactam analogons or as components in formulations having antibacterial, inhibitory, antitumour or antagonistic action.

    摘要翻译： 提供3-溴 - 和3-二溴-4-氧代 - 氮杂环丁烷的新型2-溴 - 和2-硝基氧基衍生物，其制备方法及其用途。 本发明的氮杂环丁烷具有式I其中R 1是氢或溴，R 2是氢或溴，其中R 1或R 2中的至少一个是溴，R 3是氢; Me2-C = C-COOR4，其中R4是氢，甲基，苄基或一些其它羧基保护基，X是溴或硝基氧基（-ONO 2）。 根据本发明，3-溴 - 和3-二溴-4-氧代 - 氮杂环丁烷的2-溴 - 和2-硝基氧基衍生物是通过将受保护的青霉烷酸1,1-二氧化物的衍生物与DBN反应物（1,5- 二氮杂双环/ 3.4.0 /非-5-烯），然后将得到的亚磺酸的DBN盐或分离的亚磺酸用亚硫酰氯处理，通过蒸发除去亚硫酰氯后，将所得残余物通过硅胶柱， 二氯甲烷或一些其它溶剂作为洗脱剂，或将所得残余物溶于四氢呋喃或其它合适的溶剂中，并用四丁基溴化铵处理，处理后，将2-溴，3-溴或2-溴-3,3- 分离出二溴-4-氧代 - 氮杂环丁烷，该衍生物可以与硝酸银在2-丙醇中进行反应，在处理反应混合物后，将2-硝基氧基，3-溴 - 或2-硝基氧基 分离出-3,3-二溴-4-氧代 - 氮杂环丁烷。 获得的物质是合成β-内酰胺类似物或作为具有抗菌，抑制，抗肿瘤或拮抗作用的制剂中的组分的有用中间体。

    Coumarin derivatives, and processes for their preparation
    6.
    发明授权
    Coumarin derivatives, and processes for their preparation 失效
    香豆素衍生物及其制备方法

    公开(公告)号：US5840922A

    公开(公告)日：1998-11-24

    申请号：US887217

    申请日：1997-07-02

    申请人： Mladen Trkovnik ,  Zrinka Ivezic ,  Ljerka Polak

    发明人： Mladen Trkovnik ,  Zrinka Ivezic ,  Ljerka Polak

    IPC分类号： C07D311/08 ,  A61K31/37 ,  C07D311/06 ,  C07D311/14 ,  C07D311/16 ,  C07D311/18 ,  C07D311/74 ,  C07D311/12

    CPC分类号： C07D311/14 ,  C07D311/16 ,  C07D311/18

    摘要： The present invention relates to new coumarin derivatives represented by the general formula I ##STR1## wherein R.sup.1 =NH.sub.2 or --NHCH.dbd.C(CO.sub.2 C.sub.2 H.sub.5).sub.2, R.sup.2 =R.sup.3 =R.sup.4 =H, R.sup.5 =F, R.sup.1 =R.sup.3 =NHCH.dbd.C(CO.sub.2 C.sub.2 H.sub.5).sub.2, R.sup.2 =R.sup.4 =R.sup.5 =H, R.sup.1 =H or OH, R.sup.3 =NHCH.dbd.C(CO.sub.2 C.sub.2 H.sub.5).sub.2, R.sup.2 =R.sup.4 =R.sup.5 =H, R.sup.1 =OH, R.sup.2 =R.sup.3 =R.sup.4 =H, R.sup.5 =--NHCH.dbd.C(CO.sub.2 C.sub.2 H.sub.5).sub.2, R.sup.1 =R.sup.3 =R.sup.5 =H, R.sup.2 =CH.sub.3 or CF.sub.3, R.sup.4 =--NHCH.dbd.C(CO.sub.2 C.sub.2 H.sub.5).sub.2, processes for the preparation thereof and their use as intermediates for the synthesis of new coumarin derivatives with potential biological action.

    摘要翻译： 本发明涉及通式Ⅰ的化合物，其中R1 = NH2或-NHCH = C（CO2C2H5）2，R2 = R3 = R4 = H，R5 = F，R1 = R3 = NHCH = C（CO2C2H5）2，R2 = R4 = R5 = H，R1 = H或OH，R3 = NHCH = C（CO2C2H5）2，R2 = R4 = R5 = H，R1 = OH，R2 = R3 = R4 = R5 = -NHCH = C（CO2C2H5）2，R1 = R3 = R5 = H，R2 = CH3或CF3，R4 = -NHCH = C（CO2C2H5）2，其制备方法及其作为合成 新的香豆素衍生物具有潜在的生物学作用。

    Secomacrolides from class of erythromycins and process for their preparation
    7.
    发明授权
    Secomacrolides from class of erythromycins and process for their preparation 失效
    来自红霉素类的重庆霉素及其制备方法

    公开(公告)号：US6077944A

    公开(公告)日：2000-06-20

    申请号：US38901

    申请日：1998-03-12

    申请人： Gorjana Lazarevski ,  Gabrijela Kobrehel ,  Amalija Narandja ,  Zrinka Banic-Tomisic

    发明人： Gorjana Lazarevski ,  Gabrijela Kobrehel ,  Amalija Narandja ,  Zrinka Banic-Tomisic

    IPC分类号： C07H17/08 ,  A61K31/70 ,  A61K31/7048 ,  C07H15/04 ,  C07H15/26 ,  C07H1/00 ,  C07H15/00

    CPC分类号： C07H15/04 ,  C07H15/26

    摘要： The invention relates to novel secomacrolides from the class of erythromycin A, potential intermediates for preparation of novel macrolide antibiotics general formula ##STR1## and its pharmaceuticaly acceptable addition salts with inorganic or organic acids, wherein R.sub.1 represents hydrogen, C.sub.1 -C.sub.4 alkanoyl group, arylcarbonyl group and together with R.sub.2 and carbon atoms to which they are bound, cyclic carbonyl or thiocarbonyl group, R.sub.2 represents hydrogen or together with R.sub.1 and carbon atoms to which they are bound, cyclic carbonyl or thiocarbonyl group, R.sub.3 represents hydrogen, C.sub.1 -C.sub.4 alkanoyl or arylcarbonyl group,Z is hydrogen or L-cladinosyl group represented by formula (i) ##STR2## wherein R.sub.4 represents hydrogen or C.sub.1 -C.sub.4 alkanoyl group, W is hydrogen or D-desosaminyl group represented by formula (ii) ##STR3## wherein R.sub.5 represents hydrogen or C.sub.1 -C.sub.4 alkanoyl or arylcarbonyl group,X and Y together represent a lactone, or X is CH.sub.2 OR.sub.6, wherein R.sub.6 represents hydrogen or C.sub.1 -C.sub.4 alkanoyl group and Y is hydroxyl group.

    摘要翻译： 本发明涉及来自红霉素A类的新型次氯氰菊酯，用于制备新型大环内酯类抗生素通用型的潜在中间体及其与无机或有机酸的药学上可接受的加成盐，其中R1表示氢，C1-C4烷酰基，芳基羰基和一起 R 2和它们所连接的碳原子，环状羰基或硫代羰基，R 2表示氢或与它们所连接的R 1和碳原子一起，环状羰基或硫代羰基，R 3表示氢，C 1 -C 4烷酰基或芳基羰基 Z为氢或由式（ⅰ）表示的L-克拉糖糖基，其中R 4表示氢或C 1 -C 4烷酰基，W为氢或式（ⅱ）表示的D-脱氨基甲酰基，其中R 5表示氢或C 1 -C 4烷酰基或 芳基羰基，X和Y一起表示内酯，或X是CH 2 OR 6，其中R 6表示氢或C 1 -C 4烷酰基，Y是羟基。

    9-N-ethenyl derivatives of 9(S)-erythromycylamine
    8.
    发明授权
    9-N-ethenyl derivatives of 9(S)-erythromycylamine 失效
    9（S） - 红霉素胺的9-N-乙烯基衍生物

    公开(公告)号：US5854219A

    公开(公告)日：1998-12-29

    申请号：US956352

    申请日：1997-10-23

    申请人： Nedjeljko Kujundzic ,  Dina Pavlovic ,  Gabrijela Kobrehel ,  Gorjana Lazarevski ,  Zeljko Kelneric

    发明人： Nedjeljko Kujundzic ,  Dina Pavlovic ,  Gabrijela Kobrehel ,  Gorjana Lazarevski ,  Zeljko Kelneric

    IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P31/04 ,  C07H17/08 ,  C07D315/00 ,  C07G11/00

    CPC分类号： A61K31/7048 ,  C07H17/08

    摘要： The invention relates to 9-N-ethenyl derivatives of 9 (S)-erythromycylamine, new semisynthetic antibiotics of the macrolide class of the general formula (I) ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and represent nitryl, a carboxyl group of the formula COOR.sup.3, wherein R.sup.3 represents a C.sub.1 -C.sub.4 alkyl group, or a keto group of the formula COR.sup.4, wherein R.sup.4 represents a C.sub.1 -C.sub.4 alkyl group, to their pharmaceutically acceptable addition salts with inorganic or organic acids, to a process for their preparation, to a process for the preparation of the pharmaceutical compositions as well as to the use of the obtained pharmaceutical compositions in the treatment of bacterial infections.

    摘要翻译： 本发明涉及9（S） - 红霉素胺的9-N-乙烯基衍生物，通式（I）的大环内酯类的新的半合成抗生素：其中R1和R2相同或不同，代表硝基 ，式COOR 3的羧基，其中R 3表示C 1 -C 4烷基，或式COR 4的酮基（其中R 4表示C 1 -C 4烷基）与其与无机或有机酸的药学上可接受的加成盐， 制备方法，制备药物组合物的方法以及所获得的药物组合物在细菌感染治疗中的用途。

    Derivatives of 3-bromo- and 3,3-dibromo-4-oxo-1-azetidines, processes for the preparation thereof and their use
    9.
    发明授权
    Derivatives of 3-bromo- and 3,3-dibromo-4-oxo-1-azetidines, processes for the preparation thereof and their use 失效
    3-溴 - 和3,3-二溴-4-氧代-1-氮杂环丁烷的衍生物，其制备方法及其用途

    公开(公告)号：US5843939A

    公开(公告)日：1998-12-01

    申请号：US796708

    申请日：1997-02-06

    申请人： Irena Lukic

    发明人： Irena Lukic

    IPC分类号： A61K31/395 ,  A61K31/397 ,  A61P31/04 ,  A61P35/00 ,  C07D205/08 ,  C07D405/04

    CPC分类号： C07D405/04 ,  C07D205/08 ,  Y02P20/55

    摘要： 3-Bromo- and 3,3-dibromo-4-oxo-1-azetidines of the formula I ##STR1## wherein R.sub.1 is hydrogen or bromo, R.sub.2 is hydrogen or bromo, R.sub.3 is hydrogen, ##STR2## wherein R.sub.4 is hydrogen, methyl, benzyl or some other protective group, R.sub.5 is hydrogen, alkyl, alkylaryl, a heterocyclic ring, Y is a halo atom, X is a halo atom, alkoxy group, nitroxy group are provided along with processes for the preparation thereof and the use thereof. The 3-bromo- and 3,3-dibromo-4-oxo-1-azetidines can be prepared by reacting 2-sulfinic acid derivatives, with various halogenating agents, and after treating the reaction mixture, 2-halo derivatives of 3-bromo- and 2,2-dibromo-4-oxo-azetidines are isolated and are subjected to a reaction with silver tetrafluoroborate and alcohols to give the corresponding 2-alkoxy derivatives of 3-bromo- and 3,3-dibromo-4-oxo azetidines, or 2-halo derivatives of 3-bromo- and 3-3-dibromo-4-oxo azetidines are subjected to a reaction with silver nitrate in 2-propanol to give, after treating the reaction mixture, 2-nitroxy derivatives of 3-bromo and 3,3-dibromo-4-oxo-1-azetidines. Some newly prepared compounds are deprotected and derivatives having a free carboxy group are obtained. The prepared compounds are components in pharmaceutical compositions effective in antibacterial or antirumour therapy.

    摘要翻译： 其中R 1是氢或溴，R 2是氢或溴，R 3是氢，氢，甲基，苄基或一些式 其它保护基，R5是氢，烷基，烷基芳基，杂环，Y是卤素原子，X是卤素原子，烷氧基，硝酰基以及其制备方法及其用途。 3-溴 - 和3,3-二溴-4-氧代-1-氮杂环丁烷可以通过使2-亚磺酸衍生物与各种卤化剂反应制备，在处理反应混合物后，将3-溴 - 和2,2-二溴-4-氧代 - 氮杂环丁烷，并与四氟硼酸银和醇反应，得到3-溴 - 和3,3-二溴-4-氧代氮杂环丁烷的相应2-烷氧基衍生物 或3-溴 - 和3-3-二溴-4-氧代氮杂环丁烷的2-卤代衍生物与硝酸银在2-丙醇中进行反应，在处理反应混合物后，得到3- 溴和3,3-二溴-4-氧代-1-氮杂环丁烷。 一些新制备的化合物脱保护，得到具有游离羧基的衍生物。 制备的化合物是有效抗菌或抗肿瘤治疗的药物组合物中的成分。