公开(公告)号：US4711956A

公开(公告)日：1987-12-08

申请号：US756018

申请日：1985-07-17

申请人： Ivanka A. Atanassova ,  Marieta A. Haimova ,  Vesselina B Chavdarova ,  Anton I. Nakov ,  Nedelcho G. Petkov ,  Ruska S. Avramova

发明人： Ivanka A. Atanassova ,  Marieta A. Haimova ,  Vesselina B Chavdarova ,  Anton I. Nakov ,  Nedelcho G. Petkov ,  Ruska S. Avramova

IPC分类号： A61K31/43 ,  A61P31/04 ,  C07D499/00 ,  C07D499/04 ,  C07D499/10 ,  C07D499/68 ,  C07D499/70 ,  C07D499/76 ,  C07D499/46

CPC分类号： C07D499/00 ,  Y02P20/55

摘要： The invention relates to penicillin derivatives of Formula I, and a method of synthesis; the derivatives having high antimicrobial activity against gram-positive and gram-negative microorganisms. ##STR1## R is selected from the group consisting of ##STR2## R.sub.1 is selected from the group consisting of hydrogen and a hydroxyl group;R.sub.2 is selected from the group consisting of hydrogen, an alkaline metal, and a carboxy protective group;R.sub.3 is selected from the group consisting of hydrogen, a lower alkyl, and a phenyl residue;R.sub.4, R.sub.5, and R.sub.6 are each selected from the group consisting of hydrogen, a halogen, a lower alkyd, and a lower alkoxy group;A is selected from the group consisting of oxygen and a N-(lower alkyl) residue; andn is 0 or 1.

摘要翻译： 本发明涉及式I的青霉素衍生物及其合成方法。 该衍生物对革兰氏阳性和革兰氏阴性微生物具有高抗微生物活性。 R 1选自由氢和羟基组成的组，其中R 1选自氢原子和羟基。 R2选自氢，碱金属和羧基保护基; R3选自氢，低级烷基和苯基残基; R4，R5和R6各自选自氢，卤素，低级醇酸和低级烷氧基; A选自氧和N-（低级烷基）残基; n为0或1。

公开(公告)号：US4933454A

公开(公告)日：1990-06-12

申请号：US341092

申请日：1989-04-20

申请人： Tashka K. Atanassova ,  Anton I. Nakov ,  Lyudmila V. Petkova ,  Zoya T. Ivanova ,  Donka M. Mondeshka

发明人： Tashka K. Atanassova ,  Anton I. Nakov ,  Lyudmila V. Petkova ,  Zoya T. Ivanova ,  Donka M. Mondeshka

IPC分类号： A61K31/425 ,  A61K31/427 ,  A61P29/00 ,  A61P37/02 ,  C07D233/32 ,  C07D241/08 ,  C07D277/46 ,  C07D417/12

CPC分类号： C07D417/12

摘要： The invention concernes acylureidoaminothiazolyl derivatives possessing pharmacological activity and a method for preparing them.2-aminothiazolyl derivatives having an allyl radical with 1-4 carbon atoms are known in the pharmaceutical practice as immunomodulators, active against immune failure diseases.The aim of the invention is to synthesize new 2-aminothiazolyl derivatives possessing pharmacological activity and describe a new method for their preparation.

摘要翻译： 本发明涉及具有药理活性的酰基脲基氨基噻唑衍生物及其制备方法。 具有1-4个碳原子的烯丙基的2-氨基噻唑基衍生物在药物实践中是已知的，其针对免疫功能衰竭疾病是有效的免疫调节剂。 本发明的目的是合成具有药理活性的新的2-氨基噻唑衍生物，并描述了其制备方法。