公开(公告)号：EP1357123A1

公开(公告)日：2003-10-29

申请号：EP01272847.3

申请日：2001-12-25

申请人： Sumitomo Pharmaceuticals Company, Limited

发明人： SUNAGAWA, Makoto ,  SASAKI, Akira

IPC分类号： C07D477/14 ,  A61K31/407 ,  A61P31/04

CPC分类号： C07D477/14

摘要： Carbapenem compounds having a substituted phenyl or a substituted thienyl directly attached to the 3-position of carbapenem nucleus as represented by the formula:
wherein Ring E is benzene ring or thiophene ring; R 1 is optionally OH-substituted C 1-3 alkyl; R 2 and R 3 represent each H, optionally substituted lower alkyl, etc.; R is H, or a group which is hydrolyzed in the living body to regenerate a carboxyl group, etc.; X is O or S; and Y represents H, lower alkyl, etc., or pharmaceutically acceptable salts thereof and medicaments containing said compound as the active ingredient. These compounds exhibit an excellent antibacterial activity over a broad range of Gram-positive and Gram-negative bacteria, in particular, penicillin-resistant Staphylococcus pneumoniae (PRSP) which has been isolated at an elevated frequency in recent years and thus causes a serious clinical problem, and Haemophilus influenzae which has acquired resistance against the existing β-lactam antibiotics over a wide scope due to penicillin-binding protein (PBP) mutations such as β-lactamase non-producing ampicillin-resistant (BLNAR) Haemophihis influenzae.

摘要翻译： 具有substituiertem苯基或直接附接至所表示由式碳代青霉烯核的3位上的噻吩基碳青霉烯substituiertem化合物： worin环E为苯环或噻吩环; [R <1>任选OH substituiertem C 1-3烷基; [R <2>和R <3>表示每一个是H，任选substituiertem低级烷基等; R是H，或一个组中的所有其在活体中水解以再生羧基等; X是O或S; 以及它们的ÿdarstellt H，低级烷基等，或药学上可接受的盐和包含所述化合物作为活性成分的药物。 这些化合物表现出优异的抗菌活性在宽范围的革兰氏阳性和革兰氏阴性细菌，特别是，青霉素耐药的肺炎（PRSP），其具有在近几年在分离在升高的频率，从而导致严重的临床problem- 如β-内酰胺酶非产生氨苄青霉素抗性（BLNAR）Haemophihis流感：其中已由于青霉素结合蛋白（PBP）的突变获取针对存在β-内酰胺类抗生素的抗性在很宽的范围，和流感嗜血杆菌。

公开(公告)号：EP1357123B1

公开(公告)日：2005-11-30

申请号：EP01272847.3

申请日：2001-12-25

申请人： SUMITOMO PHARMACEUTICALS COMPANY, LIMITED

发明人： SUNAGAWA, Makoto ,  SASAKI, Akira

IPC分类号： C07D477/14 ,  A61K31/407 ,  A61P31/04

CPC分类号： C07D477/14

摘要： Carbapenem compounds having substituted phenyl or substituted thienyl directly attached to the 3-position of carbapenem compounds as represented by the following formula (1): (1) wherein the ring E represents a benzene or thiophene ring; R1 represents optionally OH-substituted C¿1-3? alkyl; R?2 and R3¿ represent each H, optionally substituted lower alkyl, etc.; R represents H, a group which is hydrolyzed in vivo to regenerate carboxyl, etc.; X represents O or S; and Y represents H, lower alkyl, etc.; pharmaceutically acceptable salts thereof and drugs containing these compounds as the active ingredient. These compounds exhibit an excellent antibacterial activity over a broad range of gram-positive and gram-negative bacteria, in particular, penicillin-resistant Staphylococcus pneumoniae(PRSP) which has been isolated at an elevated frequency in recent years and thus causes a serious clinical problem, and Haemophilus influenza which have acquired resistance against the existing βlactam agents over a wide scope due to penicillin-binding protein (PBP) mutations such as β-lactamase non-producing ampicillin-resistant (BLNAR) H. influenza.

公开(公告)号：EP0827951A1

公开(公告)日：1998-03-11

申请号：EP96910192.2

申请日：1996-04-18

申请人： SUMITOMO PHARMACEUTICALS COMPANY, LIMITED

发明人： YAMAMOTO, Michihiro ,  SASAKI, Akira ,  KATSUMATA, Takashi ,  TSUSHIMA, Naomi ,  HARADA, Hideyuki

IPC分类号： C07C233/46 ,  C07C233/63 ,  C07C237/22 ,  C07C271/40 ,  C07C275/34 ,  C07C311/04 ,  C07C311/22 ,  C07C311/30 ,  C07C323/50

CPC分类号： C07F9/3869

摘要： A novel estrogen derivative represented by the formula:
is useful for treating or preventing diseases caused by estrogen deficiency.