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。

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。