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公开(公告)号:EP1333025A4
公开(公告)日:2004-03-24
申请号:EP01981047
申请日:2001-11-09
申请人: TAISHO PHARMA CO LTD
IPC分类号: A61P3/10 , A61P29/00 , A61P31/18 , A61P35/04 , A61P37/02 , A61P43/00 , C07D207/16 , C07D401/06 , A61K31/40 , C07D401/12
CPC分类号: C07D401/06 , C07D207/16 , Y02P20/55
摘要: Cyanopyrrolidine derivatives represented by the general formula (1) or pharmaceutically acceptable salts thereof: (1) wherein R1 is halogeno, hydroxyl, or the like, and R2 is hydrogen, halogeno, or the like, or alternatively R?1 and R2¿ are united to form oxo, hydroxyimino, or the like; R?3 and R4¿ are each hydrogen, halogeno, or the like, or alternatively R?3 and R4¿ are united to form oxo, hydroxyimino, or the like; X is oxygen or sulfur; Y is CR5R6- (wherein R?5 and R6¿ are each independently hydrogen, halogeno, or the like) or CR?7R8-CR9R10¿- (wherein R?7, R8, R9, and R10¿ are each independently hydrogen, halogeno, or the like, or alternatively R?7 and R9¿ together with the carbon atoms adjacent thereto form C¿3-8? cycloalkyl or the like); and Z is hydrogen, C1-10 alkyl, or the like, or alternatively Y and Z together with the nitrogen atom adjacent thereto form cyclic C2-10 amino or the like.
摘要翻译: (1)代表的氰基吡咯烷衍生物或其药学上可接受的盐:(1)其中R1是卤代,羟基等,R2是氢,卤素等,或者R1和R2是 结合形成氧代,羟基亚氨基等; R 3和R 4各自为氢,卤素等,或者R 3和R 4结合形成氧代,羟基亚氨基等; X是氧或硫; Y是CR 5 R 6 - (其中R 5和R 6各自独立地是氢,卤素等)或CR 7 R 8 -CR 9 R 10 - (其中R 7,R 8,R 9和R 10各自独立地是氢,卤素 或者类似的,或者R7和R9与其相邻的碳原子一起形成C8-8环烷基等)。 并且Z是氢,C1-10烷基等,或者Y和Z与其相邻的氮原子一起形成环状的C2-10氨基或类似基团。
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公开(公告)号:EP2103607A4
公开(公告)日:2011-01-05
申请号:EP07850604
申请日:2007-12-14
申请人: TAISHO PHARMA CO LTD
发明人: KAKINUMA HIROYUKI , OI TAKAHIRO , HASHIMOTO YUKO , TAKAHASHI HITOMI , KOBAYASHI YOHEI , IWATA YUKI , KAWABE KENICHI , TAKAHASHI MASATO
IPC分类号: C07D335/02 , A61K31/382 , A61P3/04 , A61P3/06 , A61P3/08 , A61P3/10 , A61P7/10 , A61P9/04 , A61P9/10 , A61P9/12 , A61P13/12 , A61P19/06 , A61P25/00 , A61P27/02 , A61P31/04 , A61P43/00
CPC分类号: C07D335/02
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公开(公告)号:EP2562155A4
公开(公告)日:2014-09-10
申请号:EP11772045
申请日:2011-04-20
发明人: TAKASHIMA HAJIME , TSURUTA RISA , YABUUCHI TETSUYA , OKA YUSUKE , URABE HIROKI , SUGA YOICHIRO , TAKAHASHI MASATO , UNEUCHI FUMITO , KOTSUBO HIRONORI , SHOJI MUNEO , KAWAGUCHI YASUKO
IPC分类号: C07C259/06 , A61K31/166 , A61K31/337 , A61K31/341 , A61K31/343 , A61K31/351 , A61K31/357 , A61K31/36 , A61K31/381 , A61K31/397 , A61K31/40 , A61K31/4015 , A61K31/402 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/4045 , A61K31/407 , A61K31/415 , A61K31/416
CPC分类号: C07C233/83 , C07C235/84 , C07C237/36 , C07C259/06 , C07C271/22 , C07C271/28 , C07C309/30 , C07C311/08 , C07C317/28 , C07C317/44 , C07C323/41 , C07C323/62 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2602/08 , C07D205/04 , C07D205/12 , C07D207/10 , C07D207/12 , C07D207/27 , C07D207/327 , C07D209/08 , C07D209/12 , C07D209/14 , C07D209/44 , C07D209/52 , C07D211/14 , C07D211/18 , C07D211/38 , C07D211/46 , C07D211/56 , C07D211/70 , C07D213/38 , C07D213/40 , C07D213/54 , C07D213/61 , C07D213/64 , C07D213/65 , C07D213/70 , C07D213/74 , C07D213/81 , C07D215/14 , C07D217/04 , C07D217/12 , C07D231/12 , C07D231/56 , C07D233/61 , C07D235/04 , C07D257/04 , C07D261/08 , C07D263/14 , C07D263/32 , C07D263/56 , C07D265/30 , C07D265/36 , C07D265/38 , C07D267/10 , C07D271/12 , C07D277/20 , C07D277/30 , C07D277/62 , C07D277/66 , C07D285/12 , C07D295/08 , C07D295/12 , C07D295/14 , C07D295/16 , C07D305/06 , C07D305/08 , C07D307/14 , C07D307/18 , C07D307/52 , C07D307/54 , C07D307/78 , C07D307/81 , C07D307/82 , C07D307/87 , C07D309/04 , C07D309/14 , C07D317/30 , C07D317/60 , C07D319/18 , C07D319/20 , C07D333/24 , C07D405/06 , C07D413/06 , C07D471/04 , C07D471/10 , C07D487/08 , C07D491/20 , C07D498/04 , C07D498/08 , C07F9/091
摘要: Provided is a novel compound which is useful as a pharmaceutical composition by inhibiting an LpxC activity, thereby exhibiting potent antimicrobial activity against gram-negative bacteria including Pseudomonas aeruginosa and its drug resistant bacteria. Provided is a hydroxamic acid derivative represented by the following general formula [1] or a pharmaceutically acceptable salt thereof:
摘要翻译: 提供了通过抑制LpxC活性作为药物组合物有用的新型化合物,从而对包括铜绿假单胞菌及其耐药细菌在内的革兰氏阴性细菌表现出有效的抗微生物活性。 提供由以下通式[1]表示的异羟肟酸衍生物或其药学上可接受的盐:
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公开(公告)号:EP2881384A4
公开(公告)日:2015-12-23
申请号:EP13825784
申请日:2013-07-29
申请人: TAISHO PHARMA CO LTD
发明人: TAKAYAMA TETSUO , SHIBATA TSUYOSHI , SHIOZAWA FUMIYASU , KAWABE KENICHI , SHIMIZU YUKI , HAMADA MAKOTO , HIRATATE AKIRA , TAKAHASHI MASATO , USHIYAMA FUMIHITO , OI TAKAHIRO , SHIRASAKI YOSHIHISA , MATSUDA DAISUKE , KOIZUMI CHIE , KATO SOTA
IPC分类号: C07D207/36 , A61K31/4015 , A61K31/4412 , A61K31/4418 , A61K31/443 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/4704 , A61K31/4709 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/55 , A61P7/06 , A61P43/00
CPC分类号: C07D211/90 , C07D207/36 , C07D209/54 , C07D215/56 , C07D221/20 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/06 , C07D409/06 , C07D409/10 , C07D413/06 , C07D413/10 , C07D413/12 , C07D417/06 , C07D417/10 , C07D417/12 , C07D471/10 , C07D491/107 , C07D498/04
摘要: There are provided compounds having a superior PHD2 inhibitory effect that are represented by general formula (I'): (in the above-mentioned general formula (I'), W, Y, R 2 , R 3 , R 4 , and Y 4 are as described hereinabove), or pharmaceutically acceptable salts thereof.
摘要翻译: 提供由通式(I')表示的具有优异PHD2抑制作用的化合物:(在上述通式(I')中,W,Y,R 2,R 3,R 4和Y 4 如上所述)或其药学上可接受的盐。
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公开(公告)号:EP1535907A4
公开(公告)日:2006-11-29
申请号:EP03791325
申请日:2003-08-27
申请人: TAISHO PHARMA CO LTD
IPC分类号: A61K31/40 , A61P3/04 , A61P3/10 , A61P13/08 , A61P19/02 , A61P19/10 , A61P37/00 , A61P43/00 , C07D207/16
CPC分类号: A61K31/40 , C07D207/16
摘要: (2S,4S)-2-cyano-4-fluoro-1-[(2-hydroxy-1,1-dimethyl)ethylamino]acetylpyrrolidine benzenesulfonate which shows an excellent DPPIV inhibitory activity and has properties required as a medicine, for example, a high stability. This compound can be easily obtained in the form of highly stable crystals having a uniform shape and has a high solid stability.
摘要翻译: (2S,4S)-2-氰基-4-氟-1 - [(2-羟基-1,1-二甲基)乙氨基]乙酰基吡咯烷苯磺酸盐,其具有优异的DPPIV抑制活性并且具有作为药物所需的性质,例如, 高稳定性。 该化合物可以容易地以具有均匀形状并且具有高固体稳定性的高度稳定晶体的形式获得。
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