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1. 发明申请

WO2003059898A2 EPONEMYCIN AND EPOXOMICIN ANALOGS AND USES THEREOF 审中-公开
标题翻译： EPONEMYCIN和EPOXOMICIN类似物及其用途
公开(公告)号：WO2003059898A2
公开(公告)日：2003-07-24
申请号：PCT/US2003/000390
申请日：2003-01-08
申请人： EISAI CO. LTD. , AGOULNIK, Sergei , AKASAKA, Kozo , FANG, Frank , HARMANGE, Jean-Christophe , HAWKINS, Lynn , JIANG, Yimin , JOHANNES, Charles , LI, Xiang-Yi , MCGUINNESS, Pamela , MURPHY, Erin , SCHILLER, Shawn , VERMEULEN, Mary , WU, Jiayi
发明人： AGOULNIK, Sergei , AKASAKA, Kozo , FANG, Frank , HARMANGE, Jean-Christophe , HAWKINS, Lynn , JIANG, Yimin , JOHANNES, Charles , LI, Xiang-Yi , MCGUINNESS, Pamela , MURPHY, Erin , SCHILLER, Shawn , VERMEULEN, Mary , WU, Jiayi
IPC分类号： C07D303/36
CPC分类号： C07D209/48 , A61K38/00 , C07D303/36 , C07D405/12 , C07D407/12 , C07F5/025 , C07F9/65502 , C07K5/06139
摘要： The present invention provides compounds having formula (I) : wherein R 1 -R 6 , A, J, D, E, G, Q, w, x, y, and z are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof in the treatment of cancer and/or inflammatory disorders, and more generally as proteasome inhibitors.
摘要翻译：本发明提供具有式（I）的化合物：其中R 1 -R 6，A，J，D，E，G，Q，w，x，y和z如本文中所述的一般和类别和亚类所述，其药物组合物及其用于治疗癌症和/或炎症性疾病的方法，更一般地，作为蛋白酶体抑制剂。

2. 发明申请

WO2003059898A3 EPONEMYCIN AND EPOXOMICIN ANALOGS AND USES THEREOF 审中-公开
公开(公告)号：WO2003059898A3
公开(公告)日：2003-07-24
申请号：PCT/US2003/000390
申请日：2003-01-08
申请人： EISAI CO. LTD. , AGOULNIK, Sergei , AKASAKA, Kozo , FANG, Frank , HARMANGE, Jean-Christophe , HAWKINS, Lynn , JIANG, Yimin , JOHANNES, Charles , LI, Xiang-Yi , MCGUINNESS, Pamela , MURPHY, Erin, A. , SCHILLER, Shawn , VERMEULEN, Mary , WU, Jiayi
发明人： AGOULNIK, Sergei , AKASAKA, Kozo , FANG, Frank , HARMANGE, Jean-Christophe , HAWKINS, Lynn , JIANG, Yimin , JOHANNES, Charles , LI, Xiang-Yi , MCGUINNESS, Pamela , MURPHY, Erin, A. , SCHILLER, Shawn , VERMEULEN, Mary , WU, Jiayi
IPC分类号： C07D303/36
摘要： The present invention provides compounds having formula (I) : wherein R 1 -R 6 , A, J, D, E, G, Q, w, x, y, and z are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof in the treatment of cancer and/or inflammatory disorders, and more generally as proteasome inhibitors.

3. 发明申请

WO2005030779A2 LAULIMALIDE ANALOGS AND USES THEREOF 审中-公开
标题翻译：赖氨酸类似物及其用途
公开(公告)号：WO2005030779A2
公开(公告)日：2005-04-07
申请号：PCT/US2004/031076
申请日：2004-09-22
申请人： EISAI CO. LTD. , GALLAGHER, Brian , JOHANNES, Charles , LI, Xiang-Yi , PESANT, Marc , ZHAO, Hongjuan , AKASAKA, Kozo , FANG, Francis, G.
发明人： GALLAGHER, Brian , JOHANNES, Charles , LI, Xiang-Yi , PESANT, Marc , ZHAO, Hongjuan , AKASAKA, Kozo , FANG, Francis, G.
IPC分类号： C07D493/18
CPC分类号： C07D493/08
摘要： The present invention provides compounds having formula 1: (I) and pharmaceutically acceptable derivatives thereof, wherein R 1 -R 10 , q, t, X 0 , X 1 , A, B, D, E, G, J, K, L, M and Z are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of disorders associated with cellular hyperproliferation.
摘要翻译：本发明提供具有式1的化合物及其药学上可接受的衍生物，其中R1-R10，q，t，X0，X1，A，B，D，E，G，J，K，L，如本文所述的一般类型和亚类，并且另外提供其药物组合物，以及其用于治疗与细胞过度增殖相关的病症的用途的方法。

4. 发明授权

EP0609441B1 Oxazolidone derivatives as monoamine oxidase inhibitors 失效
标题翻译：恶唑烷酮衍生物单胺氧化酶抑制剂
公开(公告)号：EP0609441B1
公开(公告)日：1999-07-21
申请号：EP92920700.9
申请日：1992-09-30
申请人： Eisai Co., Ltd.
发明人： AKASAKA, Kozo , KAJIWARA, Akiharu , NAGATO, Satoshi , IIMURA, Youichi , YOSHIDA, Ichirou , SASAKI, Atsushi , MIZUNO, Masanori , KUBOTA, Atsuhiko , KAGAYA, Takaki , KOMATSU, Mariko
IPC分类号： C07D263/56 , C07D417/14 , A61K31/42 , A61K31/425 , C07D417/04
CPC分类号： C07D263/57 , C07D417/04 , C07D417/14
摘要： An oxazolidone derivative represented by general formula (I) and having a monoamine oxidase inhibitory activity, a pharmacologically acceptable salt thereof, and a drug containing the same as the active ingredient for preventing or treating diseases for which a monoamine oxidase inhibitory activity is efficacious. In formula (I) A and B represent each nitrogen, sulfur or oxygen provided that either A or B represents nitrogen; R1 represents a group of formula (a) wherein n and m represent each an integer of 0, 1 to 4; and R?3 and R4¿ represent each hydrogen, hydroxy, lower alkyl, etc.; a group of formula (b) wherein p and q represent each an integer of 0, 1 to 4; and X represents oxygen, sulfur, etc.; a group of formula (c) wherein R?5 and R6¿ represent each hydrogen, cyanoalkyl, etc., or alternatively R?5 and R6¿ are bonded to each other to represent a ring together with the nitrogen atom to which they are bonded; and so forth; R2 represents hydrogen or lower alkyl; and the bond --- represents either a single or a double bond.

5. 发明公开

EP1463719A2 EPONEMYCIN AND EPOXOMICIN ANALOGS AND USES THEREOF 审中-公开
标题翻译： Eponemycin以及模拟和其用途环氧酶素
公开(公告)号：EP1463719A2
公开(公告)日：2004-10-06
申请号：EP03715921.7
申请日：2003-01-08
申请人： Eisai Co., Ltd
发明人： AGOULNIK, Sergei , AKASAKA, Kozo , FANG, Frank , HARMANGE, Jean-Christophe , HAWKINS, Lynn , JIANG, Yimin , JOHANNES, Charles , LI, Xiang-Yi , MCGUINNESS, Pamela , MURPHY, Erin, A. , SCHILLER, Shawn , VERMEULEN, Mary , WU, Jiayi
IPC分类号： C07D303/36 , C07D405/12 , C07D407/12 , C07D209/48 , A61K31/336 , A61K31/16 , A61K38/05 , A61P35/00 , A61P29/00 , C07K5/06 , C07C235/08 , C07C235/06 , C07C233/76 , C07C235/82 , C07C271/22 , C07F5/02 , C07F9/655 , A61K31/665 , A61K31/69
CPC分类号： C07D209/48 , A61K38/00 , C07D303/36 , C07D405/12 , C07D407/12 , C07F5/025 , C07F9/65502 , C07K5/06139
摘要： The present invention provides compounds having formula (I) : wherein R1-R6, A, J, D, E, G, Q, w, x, y, and z are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof in the treatment of cancer and/or inflammatory disorders, and more generally as proteasome inhibitors.

6. 发明公开

EP0609441A1 OXAZOLIDONE DERIVATIVE 失效
标题翻译： OXAZOLIDONE DERIVAT。
公开(公告)号：EP0609441A1
公开(公告)日：1994-08-10
申请号：EP92920700.9
申请日：1992-09-30
申请人： Eisai Co., Ltd.
发明人： AKASAKA, Kozo , KAJIWARA, Akiharu , NAGATO, Satoshi , IIMURA, Youichi , YOSHIDA, Ichirou , SASAKI, Atsushi , MIZUNO, Masanori , KUBOTA, Atsuhiko , KAGAYA, Takaki , KOMATSU, Mariko
IPC分类号： C07D263/56 , C07D417/14 , A61K31/42 , A61K31/425 , C07D417/04
CPC分类号： C07D263/57 , C07D417/04 , C07D417/14
摘要： An oxazolidone derivative represented by general formula (I) and having a monoamine oxidase inhibitory activity, a pharmacologically acceptable salt thereof, and a drug containing the same as the active ingredient for preventing or treating diseases for which a monoamine oxidase inhibitory activity is efficacious. In formula (I) A and B represent each nitrogen, sulfur or oxygen provided that either A or B represents nitrogen; R¹ represents a group of formula (a) wherein n and m represent each an integer of 0, 1 to 4; and R³ and R⁴ represent each hydrogen, hydroxy, lower alkyl, etc.; a group of formula (b) wherein p and q represent each an integer of 0, 1 to 4; and X represents oxygen, sulfur, etc., a group of formula (c) wherein R⁵ and R⁶ represent each hydrogen, cyanoalkyl, etc., or alternatively R⁵ and R⁶ are bonded to each other to represent a ring together with the nitrogen atom to which they are bonded; and so forth; R² represents hydrogen or lower alkyl; and the bond ---- ¯ represents either a single or a double bond.
摘要翻译：具有通式（I）表示的具有单胺氧化酶抑制活性的恶唑烷酮衍生物及其药理学上可接受的盐，以及含有与用于预防或治疗单胺氧化酶抑制活性有效的疾病的活性成分相同的药物。在式（I）中，A和B各自表示氮，硫或氧，只要A或B表示氮; R 1表示式（a）的基团，其中n和m各自表示0,1或4的整数; R 3和R 4各自代表氢，羟基，低级烷基等; 式（b）的基团，其中p和q各自表示0,1或4的整数; X表示氧，硫等，其中R 5和R 6各自代表氢，氰基烷基等，或者R 5和R 6与式（c）的基团键合到彼此表示与它们所键合的氮原子一起形成的环; 等等; R 2表示氢或低级烷基; 债券----表示单一或双重债券。

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