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。

公开(公告)号：US6071886A

公开(公告)日：2000-06-06

申请号：US223978

申请日：1998-12-31

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： C07H17/00 ,  A61K31/00 ,  A61K31/04 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61K31/7052 ,  A61P31/00 ,  A61P31/04 ,  C07H17/08

CPC分类号： C07H17/08

摘要： The present invention relates to .beta.,.beta.-disubstituted derivatives of 9-deoxo-9a-N-ethenyl-9a-aza-9a-homoerythromycin A, new semisynthetic antibiotics of macrolide class of the general formula (I) ##STR1## wherein R.sup.1 and R.sup.2 are mutually the same or different and represent nitrile, carboxy group of the formula COOR.sup.3, wherein R.sup.3 represents C.sub.1 -C.sub.4 alkyl group, or keto group of the formula COR.sup.4, wherein R.sup.4 represents C.sub.1 -C.sub.4 alkyl group, to their pharmaceutically acceptable addition salts with inorganic or organic acids, to a process for the preparation thereof, to a process for the preparation of 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-脱氧-9a-N-乙烯基-9a-氮杂-9a-高红霉素A的β，β-二取代衍生物，通式（I）的大环内酯类的新的半合成抗生素，其中R1和R2相互 表示腈，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）与其药学上可接受的加成盐与无机或 有机酸，其制备方法，制备药物组合物的方法，以及所用药物组合物在细菌感染治疗中的用途。