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1. 发明公开

EP2774926A1 MORPHINAN DERIVATIVE 有权转让
标题翻译： MORPHINANDERIVAT
公开(公告)号：EP2774926A1
公开(公告)日：2014-09-10
申请号：EP12829693.6
申请日：2012-09-07
申请人： The Kitasato Institute , Nippon Chemiphar Co., Ltd.
发明人： NAGASE, Hiroshi , FUJII, Hideaki , NAKATA, Eriko , WATANABE, Yoshikazu , TAKAHASHI, Toshihiro
IPC分类号： C07D491/18 , A61K31/485 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/5375 , A61K31/541 , A61K31/55 , A61P25/04 , A61P43/00 , C07D471/08
CPC分类号： C07D491/18 , C07D471/08 , C07D471/22 , C07D487/08 , C07D491/22 , C07F7/1856
摘要： A morphinan derivative represented by the following general formula (I):

(in the formula, R 1 represents hydrogen, C 1-6 alkyl, cycloalkylalkyl (the cycloalkyl moiety has 3 to 6 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms), aralkyl (the aryl moiety has 6 to 10 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms) and the like,
R 2 represents hydrogen, C 1-6 alkyl, C 3-6 cycloalkyl, C 6-10 aryl, aralkyl (the aryl moiety has 6 to 10 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms) and the like,
R 3 , R 4 and R 5 represent hydrogen, hydroxy, carbamoyl, C 1-6 alkoxy, C 6-10 aryloxy and the like,
R 6a , R 6b , R 7 , R 8 , R 9 , and R 10 represent hydrogen and the like,
X represents O or CH 2 , and
Y represents C=O, SO 2 , an atomic bond and the like), or an acid addition salt thereof is used as an analgesic.
摘要翻译：由以下通式（I）表示的吗啡喃衍生物：（式中，R 1表示氢，C 1-6烷基，环烷基烷基（环烷基部分具有3〜6个碳原子，亚烷基部分具有1〜5个碳原子原子），芳烷基（芳基部分具有6〜10个碳原子，亚烷基部分具有1〜5个碳原子）等，R 2表示氢，C 1-6烷基，C 3-6环烷基， 10芳基，芳烷基（芳基部分具有6至10个碳原子，亚烷基部分具有1至5个碳原子）等，R 3，R 4和R 5表示氢，羟基，氨基甲酰基，C 1-6烷氧基，C 6-10芳氧基等，R 6a，R 6b，R 7，R 8，R 9和R 10表示氢等，X表示O或CH 2，Y表示C = O，SO 2 ，原子键等）或其酸加成盐用作止痛剂。

2. 发明授权

EP2966074B1 MORPHINAN DERIVATIVE 有权
公开(公告)号：EP2966074B1
公开(公告)日：2018-07-25
申请号：EP13877360.1
申请日：2013-10-15
申请人： The Kitasato Institute , Nippon Chemiphar Co., Ltd.
发明人： NAGASE, Hiroshi , FUJII, Hideaki , NAKATA, Eriko , WATANABE, Yoshikazu , SAITO, Daisuke , TAKAHASHI, Toshihiro
IPC分类号： C07D471/08 , C07D471/10 , C07D491/20 , A61K31/439 , A61P25/04 , A61P25/22
CPC分类号： C07D471/08 , C07D471/10 , C07D491/20
摘要： The present invention relates to a morphinan derivative represented by the following general formula (I), wherein R 1 represents hydrogen, C 1-6 alkyl, C 6-10 aryl, etc., R 2 and R 3 , which are the same or different, represent hydrogen, hydroxy, ect., R 4 and R 5 represent hydrogen, C 1-6 alkyl, etc., R 6 represents hydrogen, hydroxy, C 1 - 6 alkyl, etc., X represents O or CH 2 , Y represents C=O, C(=O)O, etc., and m and n, which are the same or different, represent an integer of 0 to 2 (m and n are not 0 at the same time), a tautomer or stereoisomer of the compound, or a pharmaceutically acceptable salt thereof, or a solvate thereof, as well as an analgesic, antianxiety drug, etc. containing the same as an active ingredient.

3. 发明公开

EP2966074A1 MORPHINAN DERIVATIVE 有权
标题翻译：吗啡喃衍生物
公开(公告)号：EP2966074A1
公开(公告)日：2016-01-13
申请号：EP13877360.1
申请日：2013-10-15
申请人： The Kitasato Institute , Nippon Chemiphar Co., Ltd.
发明人： NAGASE, Hiroshi , FUJII, Hideaki , NAKATA, Eriko , WATANABE, Yoshikazu , SAITO, Daisuke , TAKAHASHI, Toshihiro
IPC分类号： C07D471/08 , A61K31/439 , A61P25/04 , A61P25/22
CPC分类号： C07D471/08 , C07D471/10 , C07D491/20
摘要： The present invention relates to a morphinan derivative represented by the following general formula (I), wherein R 1 represents hydrogen, C 1-6 alkyl, C 6-10 aryl, etc., R 2 and R 3 , which are the same or different, represent hydrogen, hydroxy, ect., R 4 and R 5 represent hydrogen, C 1-6 alkyl, etc., R 6 represents hydrogen, hydroxy, C 1 - 6 alkyl, etc., X represents O or CH 2 , Y represents C=O, C(=O)O, etc., and m and n, which are the same or different, represent an integer of 0 to 2 (m and n are not 0 at the same time), a tautomer or stereoisomer of the compound, or a pharmaceutically acceptable salt thereof, or a solvate thereof, as well as an analgesic, antianxiety drug, etc. containing the same as an active ingredient.
摘要翻译：本发明涉及下述通式（I）表示的吗啡喃衍生物，其中R 1表示氢，C 1-6烷基，C 6-10芳基等，R 2和R 3相同或不同，表示氢，羟基等，R 4和R 5表示氢，C 1-6烷基等，R 6表示氢，羟基，C 1-6烷基等，X表示O或CH 2，Y表示C = O，C（= O） O等，m和n相同或不同，表示0〜2的整数（m和n同时不为0），该化合物的互变异构体或立体异构体或其药学上可接受的盐或其溶剂化物，以及含有该化合物作为活性成分的镇痛剂，抗焦虑药等。

4. 发明授权

EP2774926B1 MORPHINAN DERIVATIVE 有权转让
标题翻译：吗啡
公开(公告)号：EP2774926B1
公开(公告)日：2017-03-15
申请号：EP12829693.6
申请日：2012-09-07
申请人： The Kitasato Institute , Nippon Chemiphar Co., Ltd.
发明人： NAGASE, Hiroshi , FUJII, Hideaki , NAKATA, Eriko , WATANABE, Yoshikazu , TAKAHASHI, Toshihiro
IPC分类号： C07D491/18 , A61K31/485 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/5375 , A61K31/541 , A61K31/55 , A61P25/04 , A61P43/00 , C07D471/08
CPC分类号： C07D491/18 , C07D471/08 , C07D471/22 , C07D487/08 , C07D491/22 , C07F7/1856

5. 发明公开

EP2397480A1 DIAZEPINEDIONE DERIVATIVE 有权
标题翻译： DIAZEPINEDIONE派生物
公开(公告)号：EP2397480A1
公开(公告)日：2011-12-21
申请号：EP10741334.6
申请日：2010-02-15
申请人： Nippon Chemiphar Co., Ltd.
发明人： SAKUMA, Shogo , TAKAHASHI, Toshihiro , USHIODA, Masatoshi , IMAI, Toshiyasu , INOUE, Kazuhide
IPC分类号： C07D403/10 , A61K31/5513 , A61P25/04 , A61P43/00 , C07D413/10 , C07D417/10
CPC分类号： C07D243/10 , C07D403/10 , C07D413/10
摘要： A diazepinedione derivative represented by the formula (I) or a pharmacologically acceptable salt thereof is used as a P2X 4 receptor antagonist:

wherein R 1 represents a hydrogen atom, an alkyl group having' 1 to 8 carbon atoms, or the like, R 2 and R 3 represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, a halogen atom, or the like, R 4 and R 5 represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or the like, and W represents tetrazole or the like.
摘要翻译：作为P2X 4受体拮抗剂，使用式（I）所示的二氮杂二酮衍生物或其药理学上可接受的盐作为P2X 4受体拮抗剂，式中，R 1表示氢原子，碳原子数1〜8的烷基等，R 2和R 3表示氢原子，具有1至8个碳原子的烷基，卤素原子等，R 4和R 5表示氢原子，具有1至8个碳原子的烷基等，并且W表示四唑或喜欢。

6. 发明公开

EP1310494A1 PPAR (delta) ACTIVATORS 有权
标题翻译： PPAR（DELTA）AKTIVATOREN
公开(公告)号：EP1310494A1
公开(公告)日：2003-05-14
申请号：EP01955606.7
申请日：2001-08-09
申请人： NIPPON CHEMIPHAR CO., LTD.
发明人： SAKUMA, Shogo , ENDO, Tsuyoshi , TENDO, Atsushi , TAKAHASHI, Toshihiro , YOSHIDA, Shinichi , KOBAYASHI, Kunio , MOCHIZUKI, Nobutaka , YAMAKAWA, Tomio , KANDA, Takashi , MASUI, Seiichiro
IPC分类号： C07D263/32 , C07D277/24 , C07D413/04 , C07D263/48 , C07D263/34 , C07D277/28 , C07D417/04 , C07D233/64 , C07D233/70 , C07D233/88 , C07D233/90 , A61K31/421 , A61K31/4439 , A61K31/426 , A61K31/4164 , A61K31/4709 , A61K31/506 , A61K31/422 , A61K31/427
CPC分类号： C07D413/04 , C07D263/32 , C07D277/24
摘要： Compounds of the general formula (I) or salts thereof and activators of PPARδ (peroxisome proliferator activated receptor δ) containing the compounds or the salts as the active ingredient: wherein R 1 and R 2 each are hydrogen, C 1-8 alkyl, an aryl or heterocyclic group which may be substituted, or the like; A is oxygen, sulfur, or the like; X 1 and X 2 are each a free valency, oxygen, S(O) p (wherein p is an integer of 0 to 2), C(=O), C(=O)NH, NHC(=O), CH=CH, or the like; Y is optionally substituted C 1-8 alkylene; Z is oxygen or sulfur; R 3 and R 4 are each optionally substituted C 1-8 alkyl; and R 8 is hydrogen or C 1-8 alkyl, with the proviso that when X 1 is a free valency, X 2 is not O or S(O) p , while when X 1 is C(=O)NH, X 2 is not a free valency.
摘要翻译：通式（I）化合物或其盐和含有化合物或其盐作为活性成分的PPARδ（过氧化物酶体增殖物激活受体δ）的活化剂：其中R 1和R 2各自为氢，C1- 8烷基，可被取代的芳基或杂环基等; A是氧，硫等; X 1和X 2各自为自由价，氧，S（O）p（其中p为0至2的整数），C（= O），C（= O）NH，NHC O），CH = CH等; Y为任选取代的C 1-8亚烷基; Z是氧或硫; R 3和R 4各自为任选取代的C 1-8烷基; 并且R 8是氢或C 1-8烷基，条件是当X 1是自由价时，X 2不是O或S（O）p，而当X 1是C（O） = O）NH，X 2不是自由价。

7. 发明公开

EP0794178A1 QUINAZOLINE DERIVATIVE 失效
标题翻译： CHINAZOLIN衍
公开(公告)号：EP0794178A1
公开(公告)日：1997-09-10
申请号：EP95932948.3
申请日：1995-09-29
申请人： NIPPON CHEMIPHAR CO., LTD.
发明人： NISHIOKA, Koichiro , TAKAHASHI, Toshihiro , NOMURA, Yutaka
IPC分类号： C07D239/95 , A61K31/505
CPC分类号： C07D239/95
摘要： The present invention provides a new compound which shows slow and continuous blood pressure reducing action and is useful as an antihypertensive agent.
The invention resides in a quinazoline derivative of the following formula (I) and its pharmaceutically acceptable salt:
in which, each of R 1 and R 2 is H or an alkyl group of 1 to 6 carbon atoms, or R 1 and R 2 are combined to form an ethylene group; each of R 3 and R 4 is an alkyl group of 1 to 6 carbon atoms; R 5 is a hydrogen atom, a hydroxyl group, an alkyl group of 1 to 6 carbon atoms, or an alkoxy group of 1 to 6 carbon atoms; each of R 6 and R 7 is a hydrogen atom or an alkyl group of 1 to 6 carbon atoms; and n is 2 or 3. The invention further resides in an antihypertensive agent containing the above compound.
摘要翻译：本发明提供了一种新的化合物，其显示缓慢且持续的减压作用，并且可用作抗高血压药。本发明涉及下式（I）的喹唑啉衍生物及其药学上可接受的盐：其中R 1和R 2各自为H或1至6个碳原子的烷基，或R 1和R 2结合形成亚乙基; R 3和R 4各自为1至6个碳原子的烷基; R 5为氢原子，羟基，碳原子数为1〜6的烷基或碳原子数1〜6的烷氧基。 R 6和R 7各自为氢原子或1〜6个碳原子的烷基; 并且n为2或3.本发明还涉及含有上述化合物的抗高血压药。

8. 发明公开

EP1619190A1 SALT OF (2S,3S)-3- (1S)-1-ISOBUTOXYMETHYL-3-METHYLBUTYL CARBAMOYLOXIRANE-2-CARBOXYLIC ACID 有权
标题翻译： SALZE VON（2S，3S）-3 - [[（1S）-1-异丙氧基甲基-3-甲基丁基]羰基]氧基-2-碳
公开(公告)号：EP1619190A1
公开(公告)日：2006-01-25
申请号：EP04728921.0
申请日：2004-04-22
申请人： NIPPON CHEMIPHAR CO., LTD.
发明人： TENDO, Atsushi , TAKAHASHI, Toshihiro , YAMAKAWA, Tomio , OKAI, Kazuki , NIHASHI, Susumu
IPC分类号： C07D303/48
CPC分类号： C07D303/48
摘要： The invention relates to purification of (2S,3S)-3-[[(1S)-1-isobutoxymethyl-3-methylbutyl]carbamoyl]oxirane-2-carboxylic acid [hereinafter, referred to as the carboxylic acid] using the salt of the carboxylic acid with an organic amine selected from the group consisting of piperazine, adamantane amines and others. The invention also relates to providing crystalline sodium salt of the carboxylic acid. The sodium salt is usable as a material for preparing medicaments and improved in storage stability, and has the following characteristics:

DSC: exothermic peak observed at a temperature in the range of 170 to 175°C with weight decrease; and
characteristic absorption bands of infrared absorption spectrum (KBr tablet): 3255, 2950, 2860, 1670, 1630, 1550, 1460, 1435, 1395, 1365, 1310, 1260, 1110, 890 cm -1 .
摘要翻译：本发明涉及（2S，3S）-3 - [[（1S）-1-异丁氧基甲基-3-甲基丁基]氨基甲酰基]环氧乙烷-2-羧酸[以下称为羧酸] 所述羧酸与选自哌嗪，金刚烷胺等的有机胺反应。本发明还涉及提供羧酸的结晶钠盐。钠盐可用作制备药物的材料并提高储存稳定性，具有以下特征：DSC：在170至175℃的温度范围内观察到的放热峰，重量减少; 和红外吸收光谱的特征吸收带（KBr片剂）：3255,2950,2860,1670,1630,1550,1460,1435,1395,1365,1310,1260,1110,890cm -1。

9. 发明授权

EP2397480B1 DIAZEPINEDIONE DERIVATIVE 有权
标题翻译： DIAZEPINEDIONE派生物
公开(公告)号：EP2397480B1
公开(公告)日：2013-08-14
申请号：EP10741334.6
申请日：2010-02-15
申请人： Nippon Chemiphar Co., Ltd.
发明人： SAKUMA, Shogo , TAKAHASHI, Toshihiro , USHIODA, Masatoshi , IMAI, Toshiyasu , INOUE, Kazuhide
IPC分类号： C07D403/10 , A61K31/5513 , A61P25/04 , A61P43/00 , C07D413/10 , C07D417/10
CPC分类号： C07D243/10 , C07D403/10 , C07D413/10

10. 发明公开

EP2058304A1 P2X4 RECEPTOR ANTAGONIST 审中-公开
标题翻译： P2X4-REZEPTORANTAGONIST
公开(公告)号：EP2058304A1
公开(公告)日：2009-05-13
申请号：EP07806431.8
申请日：2007-08-24
申请人： Nippon Chemiphar Co., Ltd.
发明人： SAKUMA, Shogo , ENDO, Tsuyoshi , IMAI, Toshiyasu , KANAKUBO, Noriko , ARAI, Masahiko , TAKAHASHI, Toshihiro , YAMAKAWA, Tomio , TSUDA, Makoto, Kyushu University , INOUE, Kazuhide, Kyushu University
IPC分类号： C07D243/24 , A61K31/5513 , A61P25/04 , A61P43/00
CPC分类号： C07D243/20 , C07D243/22 , C07D243/24
摘要： A compound having the following formula (II) or its pharmacologically acceptable salt is used as a P2X 4 receptor antagonist:

in which
R 11 represents hydrogen or an alkyl group having 1-8 carbon atoms;
R 21 represents an alkyl group having 1-8 carbon atoms, an alkoxy group having 1-8 carbon atoms, an alkyl group having 1-8 carbon atoms and having 1-3 halogen substituents, or hydroxyl; and
R 31 is hydrogen or a halogen atom.
摘要翻译：使用具有下式（II）的化合物或其药理学上可接受的盐作为P2X 4受体拮抗剂：其中R 11表示氢或具有1-8个碳原子的烷基; R 21表示具有1-8个碳原子的烷基，具有1-8个碳原子的烷氧基，具有1-8个碳原子并具有1-3个卤素取代基的烷基或羟基; 和R 31是氢或卤素原子。

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