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    Certain 4H-�1!benzopyrano�3,4-b!pyridine derivatives and their corresponding �6,7-b! and �7,8-b! ring isomers
    2.
    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。

    Ketolides from the class of 15-membered lactams
    3.
    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。

    9-N-ethenyl derivatives of 9(S)-erythromycylamine
    4.
    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。