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16 条记录 (耗时 0.017 秒)

    Ketolides from the class of 15-membered lactams
    11.
    发明授权
    Ketolides from the class of 15-membered lactams 失效
    来自15-元内酰胺类的酮内酯

    公开(公告)号：US6110965A

    公开(公告)日：2000-08-29

    申请号：US127764

    申请日：1998-07-31

    申请人： Gorjana Lazarevski ,  Gabrijela Kobrehel ,  Zeljko Kelneric

    发明人： Gorjana Lazarevski ,  Gabrijela Kobrehel ,  Zeljko Kelneric

    IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P31/04 ,  C07H17/08 ,  A61K31/35 ,  C07D267/00

    CPC分类号： C07H17/08

    摘要： The present invention relates to the new 15-membered ketoazalides from the class of 6-O-methyl-8a-aza-8a-homo-and 6-O-methyl-9a-aza-9a-homoerythromycin A with the general formula (I) ##STR1## wherein A represents NH group and B at the same time represents C.dbd.O group, orA represents C.dbd.O group and B at the same time represents NH group,R.sup.1 represents OH group, L-cladinosyl group of the formula (II) ##STR2## or together with R.sup.2 represents ketone, R.sup.2 represents hydrogen or together with R.sup.1 represents ketone,R.sup.3 represents hydrogen or C.sub.1 -C.sub.4 alkanoyl group,to intermediates and a process for their preparation, to their pharmaceutically acceptable addition salts with inorganic or organic acids, to the process for the preparation of pharmaceutical compositions, as well as to the use of pharmaceutical compositions for treating bacterial infections.

    摘要翻译： 本发明涉及一种具有通式（I）的6-O-甲基-8a-氮杂-8a-均聚物和6-O-甲基-9a-氮杂-9a-高红霉素A的新的15-元酮马来酸盐 ）其中A表示NH基团，B同时表示C = O基团，或A表示C = O基团，B同时表示NH基团，R1表示OH基团，式（II）所示L-赖壁糖苷酶基团， 或与R2一起表示酮，R 2表示氢或R 1表示酮，R 3表示氢或C 1 -C 4烷酰基，其中间体及其制备方法，其与无机或有机酸的药学上可接受的加成盐与该方法 用于制备药物组合物，以及用于治疗细菌感染的药物组合物。

    Derivatives of amino-ascorbic acid, the processes for their preparation and use
    12.
    发明授权
    Derivatives of amino-ascorbic acid, the processes for their preparation and use 失效
    氨基抗坏血酸的衍生物，其制备和使用的过程

    公开(公告)号：US5610181A

    公开(公告)日：1997-03-11

    申请号：US529394

    申请日：1995-09-18

    申请人： Bo zidar Su skovi c ,  Vanja Vela ,  Mira Bun ci c

    发明人： Bo zidar Su skovi c ,  Vanja Vela ,  Mira Bun ci c

    IPC分类号： C07D307/62 ,  A61K31/34

    CPC分类号： C07D307/62

    摘要： The invention relates to the process for the preparation of new derivatives of amino-ascorbic acid, their acid and alkali salts, processes for preparation and action.According to this invention derivatives of amino-ascorbic acid are prepared by three types of reactions: 1. reductive alkylation of amino-ascorbic acid; 2. alkylation of primary and secondary amines with halogen-ascorbic acid and 3. acylation of amino-ascorbic acid.

    摘要翻译： 本发明涉及制备氨基抗坏血酸，其酸和碱盐的新衍生物，制备方法和作用的方法。 根据本发明，氨基 - 抗坏血酸的衍生物通过三种类型的反应制备：1.氨基 - 抗坏血酸的还原性烷基化; 2.用卤素 - 抗坏血酸烷基化伯胺和仲胺，和3.酰化氨基 - 抗坏血酸。

    Certain 4H-�1!benzopyrano�3,4-b!pyridine derivatives and their corresponding �6,7-b! and �7,8-b! ring isomers
    15.
    发明授权
    Certain 4H-�1!benzopyrano�3,4-b!pyridine derivatives and their corresponding �6,7-b! and �7,8-b! ring isomers 失效
    某些4H- [1]苯并吡喃并[3,4-b]吡啶衍生物及其相应的[6,7-b]和[7,8-b]环异构体

    公开(公告)号：US5908933A

    公开(公告)日：1999-06-01

    申请号：US897057

    申请日：1997-07-18

    申请人： Mladen Trkovnik ,  Zrinka Ivezic ,  Zeljko Kelneric ,  Ljerka Polak

    发明人： Mladen Trkovnik ,  Zrinka Ivezic ,  Zeljko Kelneric ,  Ljerka Polak

    IPC分类号： C07D491/02 ,  A61K31/435 ,  A61K31/436 ,  A61K31/47 ,  A61P31/04 ,  A61P31/12 ,  A61P35/00 ,  C07D411/04 ,  C07D491/052 ,  C07D491/12 ,  C07D491/14 ,  C07D491/147 ,  A61K31/44 ,  C07D471/02 ,  C07D471/04

    CPC分类号： C07D411/04 ,  C07D491/14

    摘要： The present invention relates to novel coumarin quinolone carboxylic acids wherein the pyridone system is fused in 3,4-, 6,7- and 7,8-positions of the coumarin system, of the general formula I ##STR1## wherein R.sup.1 R.sup.2 =--NHCH=C(CO.sub.2 R.sup.6)CO, R.sup.3 =NO.sub.2 or NH.sub.2, R.sup.4 =R.sup.5 =H, R.sup.6 =H or C.sub.2 H.sub.5 ;R.sup.1 R.sup.2 =--NHCH=C(CO.sub.2 R.sup.6)CO, R.sup.3 =R.sup.4 =H, R.sup.5 =F, R.sup.6 =H or C.sub.2 H.sub.5 ;R.sup.1 R.sup.2 =--CO(CO.sub.2 R.sup.6)C=CHNH, R.sup.3 =R.sup.4 =R.sup.5 =H, R.sup.6 =H or C.sub.2 H.sub.5 ;R.sup.1 R.sup.2 =R.sup.3 R.sup.4 =--NHCH=C(CO.sub.2 R.sup.6)CO, R.sup.5 =H, R.sup.6 =H or C.sub.2 H.sub.5 ;R.sup.1 =H or OH, R.sup.2 =R.sup.5 =H, R.sup.3 R.sup.4 =--NHCH (CO.sub.2 R.sup.6)CO, R.sup.6 =H or C.sub.2 H.sub.5 ;R.sup.1 =OH, R.sup.2 =R.sup.3 =H, R.sup.4 R.sup.5 =--CO(CO.sub.2 R.sup.6) C=CHNH, R.sup.6 =H or C.sub.2 H.sub.5 ;R.sup.1 =R.sup.5 =H, R.sup.2 =CH.sub.3 or CF.sub.3, R.sup.3 R.sup.4 =--CO(CO.sub.2 R.sup.6)C=CHNH, R.sup.6 =H or C.sub.2 H.sub.5,as well as pharmaceutically acceptable salts thereof.The object of the invention are also processes for the preparation of novel coumarin quinolone carboxylic acids and the biological action thereof.

    摘要翻译： 本发明涉及新颖的香豆素喹诺酮羧酸，其中吡啶酮体系在香豆素体系的3,4,6,7和7,8位融合，通式Ⅰ其中R1R2 = -NHCH = C（ CO 2 R 6）CO，R 3 = NO 2或NH 2，R 4 = R 5 = H，R 6 = H或C 2 H 5; R1R2 = -NHCH = C（CO2R6）CO，R3 = R4 = H，R5 = F，R6 = H或C2H5; R1R2 = -CO（CO2R6）C = CHNH，R3 = R4 = R5 = H，R6 = H或C2H5; R1R2 = R3R4 = -NHCH = C（CO2R6）CO，R5 = H，R6 = H或C2H5; R1 = H或OH，R2 = R5 = H，R3R4 = -NHCH（CO2R6）CO，R6 = H或C2H5; R1 = OH，R2 = R3 = H，R4R5 = -CO（CO2R6）C = CHNH，R6 = H或C2H5; R1 = R5 = H，R2 = CH3或CF3，R3R4 = -CO（CO2R6）C = CHNH，R6 = H或C2H5，以及其药学上可接受的盐。 本发明的目的还在于制备新型香豆素喹诺酮羧酸及其生物学作用。

    N-substituted derivatives of N-methyl-3-(p-trifluoromethylphenoxy)-3-phenylpropylamine and the procedure for their preparation
    16.
    发明授权
    N-substituted derivatives of N-methyl-3-(p-trifluoromethylphenoxy)-3-phenylpropylamine and the procedure for their preparation 失效
    N-甲基-3-（对三氟甲基苯氧基）-3-苯基丙胺的N-取代衍生物及其制备方法

    公开(公告)号：US5618968A

    公开(公告)日：1997-04-08

    申请号：US145141

    申请日：1993-11-03

    申请人： Zdravko Crnic ,  Srecko I. Kirin

    发明人： Zdravko Crnic ,  Srecko I. Kirin

    IPC分类号： A61K31/00 ,  C07C213/06 ,  C07C217/48 ,  C07C269/06 ,  C07C271/16 ,  C07C271/48 ,  C07C271/36

    CPC分类号： C07C269/06 ,  C07C213/06 ,  C07C217/48 ,  C07C271/16 ,  C07C271/48

    摘要： The invention provides the preparation procedure for N-substituted derivatives of N-methyl-3-(p-trifluoromethylphenoxy)-3 -phenylpropylamine having the general formula (I), where R is hydrogen and the group of the general formula (II), in which R.sub.1 is aryl, alkylaryl and alkyl group with C.sub.1 to C.sub.4 atoms, and n is 0 and 1, and also covers the compounds of the general formula (I), where R is the group of the formula (II), in which R.sub.1 is aryl and alkylaryl group, and n is 0 and 1.According to this invention by condensation of N-substituted derivatives of N-methyl-3-phenyl-3-hydroxypropylamine (XV), where R.sub.1 is benzyl and p-nitrobenzyl group and n is 0, and p-trifluoromethylchlorbenzene (XVI) prepared N-substituted derivatives of N-methyl-3-(p-trifluoromethylphenoxy)-3 -phenylpropylamine (I), where R is the group of the formula (II), in which n and R are the same as in the compound (XV), which by the reaction with chloroformic acid esther (XVII), where R.sub.1 aryl, alkylaryl and alkyl group with C.sub.1 to C.sub.4 atoms, are converted to N-substituted derivatives of N-methyl-3-(p -trifluoromethylphenoxy)-3-phenylpropylamine (I), where R is the group of the formula (II), in which R.sub.1 is the same as in the compound (XVII), and n is 1, from which is prepared the compound of the formula (I), in which R is hydrogen (Fluoxetin), by basic hydrolysis and/or catalytic hydrogenolysis, when R is the group of the formula (II), in which R.sub.1 is benzyl and p-nitrobenzyl group, and n is 0 and 1.

    摘要翻译： 本发明提供了具有通式（I）的N-甲基-3-（对三氟甲基苯氧基）-3-苯基丙胺的N-取代衍生物的制备方法，其中R是氢，通式（II）的基团， 其中R1是芳基，烷基芳基和具有C1至C4原子的烷基，n是0和1，并且还包括通式（I）的化合物，其中R是式（II）的基团，其中 R1是芳基和烷基芳基，n是0和1.根据本发明，通过N-甲基-3-苯基-3-羟基丙基胺（XV）的N-取代衍生物的缩合，其中R1是苄基和对硝基苄基 并且n为0，对三氟甲基氯苯（XVI）制备N-甲基-3-（对三氟甲基苯氧基）-3-苯基丙胺（I）的N-取代衍生物，其中R为式（II）基团， 其中n和R与化合物（XV）中的相同，其通过与氯甲酸esther（XVII）反应，其中R 1芳基，烷芳基和烷基基团与 h C1至C4原子转化为N-甲基-3-（对三氟甲基苯氧基）-3-苯基丙胺（I）的N-取代衍生物，其中R是式（II）的基团，其中R1是 与化合物（XVII）中相同，n为1，当R为基团时，通过碱性水解和/或催化氢解制备式（I）化合物，其中R为氢（氟西汀）） 其中R1是苄基和对硝基苄基，n是0和1。