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121. 发明公开

EP2189446A4 NOVEL 4-{3-[4-(3-{4-[AMINO(BUTOXYCARBONYLIMINO)METHYL]PHENOXY}PROPYL)-1-PIPERIDINYL]PROPOXY]-N'-(BUTOXYCARBONYL)BENZAMIDINE CRYSTALS 有权
标题翻译： NEUE 4- {3- [4-（3- {4- [氨基（丁氧基羰基亚氨基）甲基]苯氧基}丙基）-1-哌啶基]丙氧基] -N' - （丁氧基羰基）苯甲酰胺基
公开(公告)号：EP2189446A4
公开(公告)日：2010-10-20
申请号：EP08790795
申请日：2008-07-02
申请人： TOYAMA CHEMICAL CO LTD
发明人： MITSUYAMA JUNICHI , AOKI NAOKATU
IPC分类号： C07D211/22 , A61K31/445 , A61P31/10
CPC分类号： C07D211/22

122. 发明公开

EP2022793A4 NOVEL HETEROCYCLIC COMPOUND OR SALT THEREOF AND INTERMEDIATE THEREOF 有权
标题翻译： NEW杂环化合物或其盐及其中间体
公开(公告)号：EP2022793A4
公开(公告)日：2010-09-08
申请号：EP07744040
申请日：2007-05-24
申请人： TOYAMA CHEMICAL CO LTD , TAISHO PHARMA CO LTD
发明人： KIYOTO TARO , ANDO JUNICHI , TANAKA TADASHI , TSUTSUI YASUHIRO , YOKOTANI MAI , NOGUCHI TOSHIYA , USHIYAMA FUMIHITO , URABE HIROKI , HORIKIRI HIROMASA
IPC分类号： C07D471/04 , A61K31/4375 , A61K31/4985 , A61K31/5365 , A61K31/542 , A61P31/04 , C07D519/00
CPC分类号： C07D471/04 , C07D491/056 , C07D519/00 , Y02P20/55

123. 发明公开

EP2192117A1 ORGANIC AMINE SALT OF 6-FLUORO-3-HYDROXY-2-PYRAZINECARBONITRILE AND METHOD FOR PRODUCING THE SAME 有权
标题翻译：有机物AMINSALZ AUS 6-氟-3-羟基-2-吡嗪酮在VERFAHREN ZU SEINER HERSTELLUNG
公开(公告)号：EP2192117A1
公开(公告)日：2010-06-02
申请号：EP08832816.6
申请日：2008-09-25
申请人： Toyama Chemical Co., Ltd.
发明人： TAKAMATSU, Tamotsu , YONEZAWA, Kenji
IPC分类号： C07D241/24
CPC分类号： C07D241/24
摘要： Disclosed is an organic amine salt of 6-fluoro-3-hydroxy-2-pyrazinecarbonitrile, which is excellent in crystallinity and useful as a production intermediate for 6-fluoro-3-hydroxy-2-pyrazinecarboxamide.
摘要翻译：公开了6-氟-3-羟基-2-吡嗪甲腈的有机胺盐，其结晶性优异，可用作6-氟-3-羟基-2-吡嗪甲酰胺的制备中间体。

124. 发明公开

EP2189446A1 NOVEL 4-{3-[4-(3-{4-[AMINO(BUTOXYCARBONYLIMINO)METHYL]PHENOXY}PROPYL)-1-PIPERIDINYL]PROPOXY]-N'-(BUTOXYCARBONYL)BENZAMIDINE CRYSTALS 有权
标题翻译： NEUE 4- {3- [4-（3- {4- [氨基（羧基苄基）甲基]苯氧基}丙基）-1-哌啶基]丙氧基] -N' - （丁氧羰基）苯并恶嗪
公开(公告)号：EP2189446A1
公开(公告)日：2010-05-26
申请号：EP08790795.2
申请日：2008-07-02
申请人： Toyama Chemical Co., Ltd.
发明人： MITSUYAMA, Junichi , AOKI, Naokatu
IPC分类号： C07D211/22 , A61K31/445 , A61P31/10
CPC分类号： C07D211/22
摘要： PROBLEMS
To provide novel crystals of 4-{3-[4-(3-{4-[amino(butoxycarbonylimino)methyl]phenoxy} propyl)-1-piperidinyl]propoxy}-N'-(butoxycarbonyl) benzamidine.
MEANS FOR SOLVING THE PROBLEMS
The type II crystal, the type III crystal and the type IV crystal of 4-{3-[4-(3-{4-[amino(butoxycarbonylimino)methyl]phenoxy} propyl)-1-piperidinyl]propoxy}-N'-(butoxycarbonyl) benzamidine are useful as excellent drug substances of antifungal agents.
摘要翻译：问题提供4- {3- [4-（3- {4- [氨基（丁氧基羰基亚氨基）甲基]苯氧基}丙基）-1-哌啶基]丙氧基} -N' - （丁氧基羰基）苄脒的新晶体。解决问题的手段4- {3- [4-（3- {4- [氨基（丁氧基羰基亚氨基）甲基]苯氧基}丙基）-1-哌啶基]的II型晶体，III型晶体和IV型晶体，丙氧基} -N' - （丁氧基羰基）苄脒可用作抗真菌剂的优异药物。

125. 发明公开

EP2128162A1 NOVEL CRYSTAL OF PIPERACILLIN SODIUM 审中-公开
标题翻译： NEUER KRISTALL VON PIPERACILIN-NATRIUM
公开(公告)号：EP2128162A1
公开(公告)日：2009-12-02
申请号：EP08704041.6
申请日：2008-01-29
申请人： Toyama Chemical Co., Ltd.
发明人： MOURI, Masaru , NISHIKAWA, Dai
IPC分类号： C07D499/68 , A61K9/14 , B01D9/00 , B01D9/02
CPC分类号： C07D499/68 , A61K9/0019
摘要： Disclosed are a novel crystal of piperacillin sodium which has diffraction angles of 3.7°, 5.5°, 7.3°, 11.6°, 14.5° and 18.0° and a novel crystal of piperacillin sodium which has diffraction angles of 5.6°, 7.8°, 12.3°, 15.5°, 17.5°, 23.3°, 24.8° and 28.5° expressed by 2θ in the powder X-ray diffraction analysis. The crystals have excellent stability and solubility and a low water-absorbing property, is extremely easy to be handled in the manufacturing process for a medicinal substance and in the packing during the preparation process for a pharmaceutical product. A pharmaceutical preparation for injection comprising any one of the crystals is useful.
摘要翻译：公开了一种新颖的哌拉西林钠结晶，其衍射角为3.7°，5.5°，7.3°，11.6°，14.5°和18.0°，新颖的哌拉西林钠晶体为衍射角为5.6°，7.8°，12.3° ，15.5°，17.5°，23.3°，24.8°和28.5°，在粉末X射线衍射分析中用2？表示。该晶体具有优异的稳定性和溶解性以及低吸水性，在药物制品的制造过程中以及在药物制备过程中的包装中极易处理。可以使用包含任何一种晶体的用于注射的药物制剂。

126. 发明公开

EP2022788A4 NOVEL CRYSTAL OF 3-Ý5-Ý4-(CYCLOPENTYLOXY)-2- HYDROXYBENZOYL¨-2-Ý(3-HYDROXY-1,2-BENZISOXAZOL-6- YL)METHOXY¨PHENYL¨PROPIONIC ACID 有权
标题翻译：新的晶体形式的3- [5- [4-（环戊氧基）-2-羟基苯甲酰基] -2 - [（3-羟基-1,2-苯并异唑-6-基）甲氧基]苯基]丙酸
公开(公告)号：EP2022788A4
公开(公告)日：2009-06-24
申请号：EP07744104
申请日：2007-05-25
申请人： TOYAMA CHEMICAL CO LTD
发明人： YONEZAWA KENJI , KOTSUBO HIRONORI , BABA YASUTAKA , TADA YUKIE
IPC分类号： C07D261/12 , A61K31/42 , A61P19/02
CPC分类号： C07D261/20
摘要： Disclosed is a crystal of 3-[5-[4-(cyclopentyloxy)-2- hydroxybenzoyl]-2-[(3-hydroxy-1,2-benzisoxazol-6- yl)methoxy]phenyl]propionic acid having refraction angles of 14.0, 16.0, 23.3, 23.7 and 26.3˚ as measured in terms of 2ϑ in powder X-ray diffraction pattern. Also disclosed is a crystal of 3-[5-[4-(cyclopentyloxy)-2-hydroxybenzoyl]-2-[(3- hydroxy-1,2-benzisoxazol-6-yl)methoxy]phenyl]propionic acid having refraction angles of 14.6, 23.1, 24.7, 25.6 and 26.0˚ as measured in terms of 2ϑ in powder X-ray diffraction pattern. These crystals have small specific volumes, are hardly charged electrically, can be handled easily, and are useful as excellent active ingredients for anti-rheumatic drugs.

127. 发明公开

EP1514542A4 MEDICINAL COMPOSITIONS IMPROVING BRAIN FUNCTION AND METHOD FOR IMPROVING BRAIN FUNCTION 有权
标题翻译：脑功能改善和方法医学组合物改善脑功能
公开(公告)号：EP1514542A4
公开(公告)日：2009-06-03
申请号：EP03760132
申请日：2003-04-03
申请人： TOYAMA CHEMICAL CO LTD
发明人： NAKADA YASUSHI , NAKAGAWA MASAYA , ONO SATOSHI
IPC分类号： A61K31/122 , A61K31/21 , A61K31/381 , A61K31/397 , A61K31/445 , A61K31/473 , A61K31/55 , A61K45/06 , A61P25/28 , A61P43/00 , A61K45/00
CPC分类号： A61K45/06 , A61K31/122 , A61K31/21 , A61K31/381 , A61K31/397 , A61K31/445 , A61K31/473 , A61K31/55 , A61K2300/00
摘要： When combined with a compound having an acetylcholine esterase inhibitory effect, an alkyl ether derivative represented by the following general formula [1] or its salt: [1] wherein R , R , R , R , m and n are each as defined in the description; synergistically enhances an anti-hypoxia effect. Thus, this combination is useful as a method of improving brain function. A medicinal composition containing the combination of the compounds as described above is useful in treating and preventing dysmnesia caused by intracerebral acetylcholine nerve hypofunction or selective cell death occurring in cerebrovascular dementia, senile dementia, Alzheimer's disease, after effect of ischemic encephalopathy and cerebral stroke.

128. 发明公开

EP1767526A4 NOVEL ARYLAMIDINE DERIVATIVE, SALT THEREOF, AND ANTIFUNGAL CONTAINING THESE 有权转让
标题翻译：新ARYLAMIDINDERIVAT，盐，和那些含有杀菌剂
公开(公告)号：EP1767526A4
公开(公告)日：2009-05-06
申请号：EP05765373
申请日：2005-06-28
申请人： TOYAMA CHEMICAL CO LTD
发明人： HAYASHI KAZUYA , KUNITANI KAZUTO , UEHARA SAYURI , MORITA TEIICHI
IPC分类号： C07D211/22 , A61K31/445 , A61P31/10
CPC分类号： C07D211/22
摘要： An arylamidine derivative represented by the general formula (wherein R1 represents optionally protected or substituted amidino; and R2 and R3 are the same or different and each represents hydrogen or halogeno) or a salt of the derivative. The derivative and salt have potent activity against fungi including ones having tolerance to azole type drugs and further have high safety and excellent properties in a repeated dose toxicity test. They are hence useful as an excellent antifungal.

129. 发明公开

EP2011796A1 NEUROGENESIS INDUCER OR NEUROPATHY THERAPEUTIC AGENT COMPRISING ALKYL ETHER DERIVATIVE OR SALT THEREOF 有权
标题翻译：神经源性神经营养因子口服神经病理疗法治疗胃肠病学
公开(公告)号：EP2011796A1
公开(公告)日：2009-01-07
申请号：EP07742276.4
申请日：2007-04-24
申请人： TOYAMA CHEMICAL CO., LTD.
发明人： IWAKAMI, Noboru , MARUBUCHI, Shigeki , OKUDA, Tomohiro
IPC分类号： C07D409/12 , A61K31/397 , A61P25/00 , A61P25/18 , A61P43/00
CPC分类号： C07D409/12
摘要： Disclosed is an agent comprising a benzothiophene alkyl ether derivative represented by the general formula below or a salt thereof:

wherein R 1 and R 2 independently represent at least one group selected from a hydrogen atom, a halogen atom, an alkyl group, an aryl group, an aralkyl group, an alkoxy group, an aryloxy group, an alkylthio group, an arylthio group, an alkenyl group, an alkenyloxy group, an amino group, an alkylsulfonyl group, an arylsulfonyl group, a carbamoyl group, a heterocyclic group, an amino group, a hydroxyl group, a carboxyl group, a nitro group, an oxo group and the like; R 3 represents an alkylamino group which may be substituted or an amino or hydroxyl group which may be protected; and m and n independently represent an integer ranging from 1 to 6. The agent is useful as a neurogenesis inducer or a therapeutic agent for neuropathy.
摘要翻译：本发明涉及下述通式所示的苯并噻吩烷基醚衍生物或其盐：其中R 1和R 2独立地表示选自氢原子，卤原子，烷基，芳基中的至少一个基团芳烷基，烷氧基，芳氧基，烷硫基，芳硫基，烯基，烯氧基，氨基，烷基磺酰基，芳基磺酰基，氨基甲酰基，杂环基，氨基，羟基，羧基，硝基，氧代基等; R 3表示可被取代的烷基氨基或可被保护的氨基或羟基; m和n独立地表示1〜6的整数。该试剂可用作神经发生诱导剂或神经病的治疗剂。

130. 发明公开

EP1967190A1 NOVEL ARYLAMIDINE DERIVATIVE, SALT THEREOF AND ANTIFUNGAL AGENT CONTAINING THOSE 有权
标题翻译：新品ARYLAMID-DERIVAT，SALZ DAVON UND DIESE强制性抗生素MITTEL
公开(公告)号：EP1967190A1
公开(公告)日：2008-09-10
申请号：EP06843443.0
申请日：2006-12-27
申请人： TOYAMA CHEMICAL CO., LTD.
发明人： HAYASHI, Kazuya c/o TOYAMA CHEMICAL CO., LTD.
IPC分类号： A61K31/445 , A61P31/10 , C07D211/22
CPC分类号： C07D211/22
摘要： Disclosed is an arylamidine derivative represented by the following general formula:

(wherein R 1 and R 2 independently represent an optionally substituted C 3-4 alkyl group) or a salt thereof, which is useful as an antifungal agent.
摘要翻译：公开了用作抗真菌剂的由以下通式表示的芳脒衍生物或其盐，其中R 1和R 2独立地表示任选取代的C 3-4烷基。

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