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公开(公告)号：EP1785415A4
公开(公告)日：2009-08-05
申请号：EP05781323
申请日：2005-08-31
发明人： KIKUCHI KAZUMI , FUJIYASU JIRO , WATANABE TOSHIHIRO , NAGAKURA YUKINORI , TOMIYAMA HIROSHI , SONEGAWA MOTOHARU , TOKUZAKI KAZUO , IWAI YOSHINORI
IPC分类号： C07D211/16 , A61K31/445 , C07D211/18 , C07D211/22 , C07D211/28 , C07D211/34 , C07D211/42 , C07D211/62 , C07D401/06 , C07D401/12 , C07D405/12 , C07D413/06 , C07D471/18 , C07D487/08 , C07D491/113
CPC分类号： C07D211/16 , C07D211/18 , C07D211/22 , C07D211/26 , C07D211/34 , C07D211/46 , C07D401/12 , C07D405/12 , C07D413/12 , C07D487/08 , C07D491/10
摘要： A piperidine derivative in which the piperidine ring is bonded in the 4-position to a monosubstituted or unsubstituted (-R1) benzene ring through vinylene and has an acyl group (-C(=O)-R4) in the 1-position; or a pharmaceutically acceptable salt of the derivative. The derivative and salt are excellent in sodium channel inhibitory activity and analgetic activity and have a high analgetic effect especially on neurogenic pains. The compounds are useful as a sodium channel inhibitor reduced in side effects.
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公开(公告)号：EP1716867A4
公开(公告)日：2009-09-23
申请号：EP05710598
申请日：2005-02-17
申请人： ASTELLAS PHARMA INC
IPC分类号： A61K45/00 , A61K31/166 , A61K31/454 , A61K31/505 , A61K45/06 , A61P25/06 , A61P43/00 , C07D239/42 , C07D339/06 , C07D401/06
CPC分类号： A61K31/166 , A61K31/454 , A61K31/505 , C07D339/06
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3.发明公开NITROGENOUS HETEROCYCLIC DERIVATIVE HAVING 2,6-DISUBSTITUTED STYRYL 审中-公开胶囊蛋白胶囊剂衍生物麻醉剂2,6-DISUBSTITUIERTEM STYRYLREST
公开(公告)号：EP1602645A4
公开(公告)日：2008-12-03
申请号：EP04717835
申请日：2004-03-05
发明人： KIKUCHI KAZUMI , OKU MAKOTO , FUJIYASU JIRO , ASAI NORIO , WATANABE TOSHIHIRO , NAGAKURA YUKINORI , TOMIYAMA HIROSHI , SONEGAWA MOTOHARU , TOKUZAKI KAZUO , IWAI YOSHINORI
IPC分类号： A61P25/02 , A61P25/04 , A61P43/00 , C07D211/12 , C07D207/06 , C07D211/14 , C07D211/16 , C07D211/18 , C07D211/22 , C07D211/26 , C07D211/30 , C07D211/34 , C07D211/38 , C07D211/42 , C07D211/46 , C07D211/56 , C07D211/60 , C07D211/62 , C07D213/16 , C07D215/06 , C07D223/04 , C07D401/06 , C07D451/02 , C07D453/02
CPC分类号： C07D211/12
摘要： A novel nitrogenous heterocyclic derivative having 2,6-disubstituted styryl or a pharmaceutically acceptable salt thereof; and a medicinal composition comprising the nitrogenous heterocyclic derivative or pharmaceutically acceptable salt and a pharmaceutically acceptable carrier, especially a medicinal composition for sodium channel inhibitors which has high analgetic activity against neurogenic pains and is reduced in side effects.
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公开(公告)号：EP1852129A4
公开(公告)日：2009-07-15
申请号：EP06713158
申请日：2006-02-07
申请人： ASTELLAS PHARMA INC
IPC分类号： A61K45/00 , A61K31/166 , A61K31/343 , A61K31/351 , A61K31/352 , A61K31/385 , A61K31/41 , A61K31/4168 , A61K31/4196 , A61K31/421 , A61K31/426 , A61K45/06 , A61P1/04 , C07D233/88 , C07D249/14 , C07D257/06 , C07D263/28 , C07D277/18 , C07D277/20 , C07D277/38 , C07D277/46
CPC分类号： A61K31/438 , A61K31/085 , A61K31/16 , A61K31/166 , A61K31/215 , A61K31/343 , A61K31/351 , A61K31/352 , A61K31/385 , A61K31/403 , A61K31/41 , A61K31/4168 , A61K31/4196 , A61K31/421 , A61K31/426 , A61K45/06 , C07D209/54 , C07D221/20 , C07D233/88 , C07D249/14 , C07D257/06 , C07D263/28 , C07D277/18 , C07D303/06 , C07D305/14 , C07D307/94 , C07D319/14 , C07D327/02 , C07D333/50 , C07D335/04 , A61K2300/00
摘要： A remedy for IBS comprising, as the active ingredient, a dual antagonist for 5-HT2B and 5-HT7 receptors which shows selective binding affinities to 5-HT2B and 5-HT7 receptors. The above-described medicinal composition is superior in the pharmacological effect to each of the cases of using an antagonist for 5-HT2B receptor which has a selective binding affinity for 5-HT2B receptor alone and using an antagonist for 5-HT7 receptor which has a selective binding affinity for 5-HT7 receptor alone. Thus, this medicinal composition is useful as a drug which is excellent in the therapeutic effect on IBS and shows lessened side effects occurring in the existing remedies for IBS.
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公开(公告)号：EP1632477A4
公开(公告)日：2008-07-16
申请号：EP04736576
申请日：2004-06-10
申请人： ASTELLAS PHARMA INC
发明人： KURAMOCHI TAKAHIRO , ASAI NORIO , IKEGAI KAZUHIRO , AKAMATSU SEIJIRO , HARADA HIRONORI , ISHIKAWA NORIKO , SHIRAKAMI SHOHEI , MIYAMOTO SATOSHI , WATANABE TOSHIHIRO , KISO TETSUO
IPC分类号： C07C237/40 , A61K31/167 , A61K31/428 , A61K31/4453 , A61K31/454 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/5377 , A61K31/538 , A61K31/55 , A61P1/04 , A61P11/00 , A61P11/06 , A61P13/10 , A61P17/04 , A61P25/06 , A61P29/00 , C07D209/08 , C07D209/34 , C07D209/36 , C07D213/75 , C07D215/38 , C07D217/04 , C07D223/16 , C07D231/56 , C07D235/06 , C07D241/42 , C07D249/18 , C07D263/58 , C07D265/36 , C07D277/62 , C07D277/64 , C07D277/82 , C07D279/16 , C07D295/155 , C07D307/79 , C07D317/64 , C07D317/66 , C07D333/54 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04
CPC分类号： C07C237/40 , A61K31/167 , A61K31/428 , A61K31/4453 , A61K31/454 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/5377 , A61K31/538 , A61K31/55 , C07D209/08 , C07D209/34 , C07D213/75 , C07D215/38 , C07D217/04 , C07D223/16 , C07D231/56 , C07D235/06 , C07D241/42 , C07D249/18 , C07D263/58 , C07D265/36 , C07D277/64 , C07D277/82 , C07D279/16 , C07D295/155 , C07D307/79 , C07D317/66 , C07D333/54 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04
摘要： A compound which functions to inhibit capsaicin receptor VR1 activation and is useful as a therapeutic agent for, e.g., various pains including inflammatory pain and neurogenic pain, migraine, cluster headache, and bladder diseases including overactive bladder. It is a benzamide derivative or salt thereof, the derivative being characterized by comprising: a benzene ring; a ring D (a mono- or dicyclic hydrocarbon ring or mono- or dicyclic heteroaromatic ring) bonded to the benzene ring through an amide bond; a ring E (a mono- or dicyclic hydrocarbon ring or mono- or dicyclic heteroaromatic ring) directly bonded to the benzene ring; and A (an amino moiety or a mono- or dicyclic heteroring) bonded to the benzene ring through L (a lower alkylene).
摘要翻译： 一种起抑制辣椒素受体VR1激活作用的化合物，可用作例如各种疼痛的治疗剂，包括炎性疼痛和神经原性疼痛，偏头痛，丛集性头痛和膀胱疾病，包括膀胱过度活动症。 它是苯甲酰胺衍生物或其盐，所述衍生物的特征在于包含：苯环; 通过酰胺键与苯环键合的环D（单环或双环烃环或单环或双环杂芳环） 直接键合到苯环上的环E（单环或双环烃环或单环或双环杂芳环） 和通过L（低级亚烷基）与苯环键合的A（氨基部分或单环或双环杂环）。
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公开(公告)号：EP1728784A4
公开(公告)日：2008-02-20
申请号：EP05710602
申请日：2005-02-17
申请人： ASTELLAS PHARMA INC
发明人： YAMADA HIROYOSHI , ITAHANA HIROTSUNE , MORITOMO AYAKO , MATSUZAWA TAKAHO , HARADA KOICHIRO , FUJIYASU JIRO , KOGA YUJI , OKU MAKOTO , OKAZAKI TOSHIO , AKUZAWA SHINOBU , WATANABE TOSHIHIRO
IPC分类号： C07C279/22 , A61K31/166 , A61K31/343 , A61K31/351 , A61K31/352 , A61K31/357 , A61K31/385 , A61K31/41 , A61K31/4168 , A61K31/4196 , A61K31/421 , A61K31/426 , A61K31/438 , C07D207/20 , C07D209/54 , C07D209/96 , C07D211/70 , C07D221/20 , C07D233/50 , C07D249/14 , C07D257/06 , C07D263/28 , C07D277/18 , C07D303/06 , C07D305/14 , C07D307/94 , C07D309/06 , C07D309/20 , C07D311/96 , C07D317/12 , C07D319/14 , C07D327/04 , C07D335/04 , C07D339/06
CPC分类号： C07D311/96 , A61K31/166 , A61K31/343 , A61K31/351 , A61K31/352 , A61K31/357 , A61K31/385 , A61K31/41 , A61K31/4168 , A61K31/4196 , A61K31/421 , A61K31/426 , A61K31/438 , C07C279/22 , C07D207/20 , C07D209/54 , C07D209/96 , C07D211/70 , C07D221/20 , C07D233/50 , C07D249/14 , C07D257/06 , C07D263/28 , C07D277/18 , C07D303/06 , C07D305/14 , C07D307/94 , C07D309/06 , C07D309/20 , C07D317/12 , C07D319/14 , C07D327/04 , C07D335/04 , C07D339/06
摘要： A novel fluorene characterized by having a fluorene skeleton to which a functional group such as a guanidino group is attached via a carbonyl group, or its salt. This compound has such an advantage as showing a high affinity particularly for 5-HT2B receptor and 5-HT7 receptor, among serotonin receptor subtypes, and exhibiting an excellent pharmacological effect compared with a conventional compound having an antagonistic activity to only one of the 5-HT2B receptor and 5-HT7 receptor. Thus, it is useful as a highly efficacious and safe preventive for migraine.
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7.发明公开
公开(公告)号：EP1609788A4
公开(公告)日：2007-10-03
申请号：EP04725182
申请日：2004-04-01
申请人： ASTELLAS PHARMA INC
IPC分类号： A61K31/4725 , A61P9/10 , A61P43/00 , C07D211/60 , C07D401/06
CPC分类号： C07D211/60 , A61K31/4725 , C07D401/06
摘要： A novel crystal of (-)-N-{2-[(R)-3-(6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline-2-carbonyl)piperidino]ethyl}-4-fluorobenzamide monophosphate.
摘要翻译： （ - ） - N- {2 - [（R）-3-（6,7-二甲氧基-1,2,3,4-四氢异喹啉-2-羰基）哌啶子基]乙基} -4-氟苯甲酰胺单磷酸盐 。
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8.发明公开
公开(公告)号：EP1486501A4
公开(公告)日：2006-03-22
申请号：EP03710430
申请日：2003-03-19
申请人： ASTELLAS PHARMA INC
发明人： ITAHANA HIROTSUNE , FUJIYASU JIRO , HAYASHIBE SATOSHI , WATANABE TOSHIHIRO , OKADA MASAMICHI , TOYA TAKASHI
IPC分类号： A61K31/429 , A61K31/5377 , A61P9/10 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/16 , A61P25/28 , A61P43/00 , C07D513/04
CPC分类号： A61K31/429 , A61K31/5377 , C07D513/04
摘要： A novel aminomethyl-substituted thiazolobenzimidazole derivative represented by the following general formula (I) or a salt thereof. The derivative or salt has metabotropic glutamate receptor activity, has excellent oral activity, and is useful as a medicine. (I) (In the formula, R1 represents oxygenic saturated heterocycle, etc.; Alk1 represents lower alkylene; m is 0 or 1; Alk2 represents lower alkylene optionally substituted by oxo; n is 0 or 1; X represents a bond, oxygen, sulfur, or NR5; R3 represents hydrogen, etc.; and R2, R4, R5, R6, and R7 are the same or different and each represents hydrogen, etc.; provided that when X is a bond and n is 1, then R3 represents neither lower alkyl nor lower halogenoalkyl, and when m is 1, R1 is OH or OMe, Alk1 is C1-3 alkylene, and either 1) X is a bond, n is 1, and R3 is hydrogen or 2) X is a bond, n is 0, and R3 is cyclohexane, then R4 represents a group other than Me.)
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