专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

71. 发明授权

EP1932522B1 Therapeutic agent for liver disease containing 2-amino-1,3-propanediol derivative as active ingredient 有权
标题翻译：肝脏疾病的治疗剂与作为活性成分的2-氨基-1,3-丙二醇衍生物
公开(公告)号：EP1932522B1
公开(公告)日：2012-05-23
申请号：EP06811299.4
申请日：2006-10-05
申请人： Kyorin Pharmaceutical Co., Ltd.
发明人： KANEKO, Takashi , KOBAYASHI, Eiji , YASUE, Tokutarou
IPC分类号： A61K31/137 , A61P1/16 , A61P3/10 , A61P37/06 , A61P43/00
CPC分类号： A61K31/137
摘要： It is intended to provide a novel therapeutic agent for an organ disease, particularly a therapeutic agent for a liver disease. It was found that a diaryl sulfide or diaryl ether derivative having a 2-amino-1,3-propanediol structure which is a sphingosine-1-phosphate receptor agonist represented by the general formula (1), a pharmaceutically acceptable salt or hydrate thereof is useful as the therapeutic agent for an organ disease, particularly the therapeutic agent for a liver disease.

72. 发明公开

EP2351748A1 ISOQUINOLINE DERIVATIVE, AND PDE INHIBITOR COMPRISING SAME AS ACTIVE INGREDIENT 审中-公开
标题翻译： ISOCHINOLINDERIVAT UND DIESES ALS WIRKSTOFF ENTHALTENDER PDE-HEMMER
公开(公告)号：EP2351748A1
公开(公告)日：2011-08-03
申请号：EP09819245.3
申请日：2009-10-08
申请人： Kyorin Pharmaceutical Co., Ltd.
发明人： KOHNO Yasushi , TAKITA Satoshi , KOJIMA Akihiko
IPC分类号： C07D401/04 , A61K31/4725 , A61P1/04 , A61P1/16 , A61P3/00 , A61P9/00 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/10 , A61P17/00 , A61P19/02 , A61P19/10 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , A61P27/14
CPC分类号： C07D401/04 , C07D471/04
摘要： The present invention provides a novel isoquinoline derivative which is useful as a pharmaceutical agent having a phosphodiesterase inhibitory activity.
The isoquinoline derivative of the present invention is represented by the following general formula (1):
摘要翻译：本发明提供了可用作具有磷酸二酯酶抑制活性的药剂的新型异喹啉衍生物。本发明的异喹啉衍生物由以下通式（1）表示：

73. 发明公开

EP2332908A1 METHOD FOR PURIFYING AMINOACETYLPYRROLIDINECARBONITRILE DERIVATIVE AND SALT THEREOF 审中-公开
标题翻译：净化氨基乙酰基吡咯烷酮腈衍生物及其盐的方法
公开(公告)号：EP2332908A1
公开(公告)日：2011-06-15
申请号：EP09814568.3
申请日：2009-09-15
申请人： Kyorin Pharmaceutical Co., Ltd.
发明人： SHIGA Futoshi
IPC分类号： C07D207/16
CPC分类号： C07D207/16 , C07B63/02
摘要： The present invention herein provides a simple, efficient and industrially useful method for purifying an aminoacetylpyrrolidinecarbonitrile derivative which is useful as a DPP-IV inhibitor. The method comprises the steps of acting an acid such as maleic acid on an aminoacetylpyrrolidinecarbonitrile derivative represented by the following Formula 1 to form a salt, isolating the salt and then regenerating the foregoing derivative from the salt:

(In the formula, A represents CH 2 , CHF or CF 2 ; R represents a C 1 to C 6 alkyl group which may have a substitutent, a C 3 to C 8 cycloalkyl group which may have a substitutent, an arylmethyl group which may have a substitutent, an arylethyl group which may have a substitutent, an aromatic hydrocarbon ring which may have a substitutent, an aromatic hetero ring which may have a substitutent, or an aliphatic hetero ring which may have a substitutent; and n represents 1 or 2).
摘要翻译：本发明提供了用于纯化可用作DPP-IV抑制剂的氨基乙酰基吡咯烷甲腈衍生物的简单，有效且工业上有用的方法。所述方法包括以下步骤：在由下式1表示的氨基乙酰基吡咯烷甲腈衍生物上使酸如马来酸形成盐，分离所述盐，然后从所述盐再生上述衍生物：（式中，A表示CH2， CHF或CF 2; R表示可以具有取代基的C1-C6烷基，可以具有取代基的C3-C8环烷基，可以具有取代基的芳基甲基，可以具有取代基的芳基乙基，芳香族可以具有取代基的烃环，可以具有取代基的芳香族杂环或可以具有取代基的脂肪族杂环，n表示1或2。

74. 发明公开

EP2327406A1 STABILIZED PHARMACEUTICAL COMPOSITION 审中-公开
标题翻译： STABILISIERTE PHARMAZEUTISCHE ZUSAMMENSETZUNG
公开(公告)号：EP2327406A1
公开(公告)日：2011-06-01
申请号：EP09806757.2
申请日：2009-08-14
申请人： Kyorin Pharmaceutical Co., Ltd.
发明人： UCHIDA Hiroshi , FUKUDA Mamoru , ARITOMI Seigo
IPC分类号： A61K31/40 , A61K47/02 , A61K47/10 , A61K47/12
CPC分类号： A61K31/40 , A61K9/2018 , A61K9/2081 , A61K9/2866 , A61K9/5015
摘要： A pharmaceutical composition is provided which can easily be prepared and which can prevent decomposition of an aminoacetylpyrrolidine carbonitrile derivative, as an effective component, which derivative is in general instable in a pharmaceutical composition.
More specifically, the pharmaceutical composition comprises an aminoacetyl pyrrolidine carbonitrile derivative represented by the following general formula (1):

(in the formula (1), A represents CH 2 , CHF or CF 2 ; and R 1 represents a secondary amino group which may have a substituent), and the following components blended with the derivative: (1) a sugar alcohols (2) calcium carbonate, sodium citrate or sodium sulfate; and (3) a neutral low melting point oily and/or fatty substance.
摘要翻译：提供了一种药物组合物，其可以容易地制备并且可以防止作为有效成分的氨基乙酰基吡咯烷腈衍生物的分解，该衍生物通常在药物组合物中不稳定。更具体地说，药物组合物包含由以下通式（1）表示的氨基乙酰基吡咯烷腈衍生物：（式（1）中，A表示CH 2，CHF或CF 2; R 1表示可以具有取代基），并且以下组分与衍生物共混：（1）糖醇（2）碳酸钙，柠檬酸钠或硫酸钠; 和（3）中性低熔点油性和/或脂肪物质。

75. 发明公开

EP2325183A1 4-(2-Furoyl) Aminopiperidine compound useful as therapeutic agent for itching 审中-公开
标题翻译： 4-（2-糠酰基）氨基哌啶嘌呤üich s s iz iz iz iz
公开(公告)号：EP2325183A1
公开(公告)日：2011-05-25
申请号：EP11156179.1
申请日：2004-05-06
申请人： Kyorin Pharmaceutical Co., Ltd. , Nisshin Seifun Group Inc.
发明人： Muraki, Yukiko , Fujimoto, Tomokazu , Kishimoto, Takuya
IPC分类号： C07D405/12 , C07D405/14 , A61K31/4525 , A61K31/5377 , A61K31/4545 , A61K31/454 , A61P17/04
CPC分类号： C07F9/65586 , C07D405/12 , C07D405/14
摘要： There are provided compounds represented by the following general formula (I):

where R 1 is 5-methylpyridin-2-yl, p-tolyl or mesityl, R 2 is

where R 3 is C1-C4 alkyl, R 4 is H or C1-C4 alkyl,
and pharmaceutically acceptable salts thereof. The compounds exhibit pruritus-inhibiting action, and are useful for prevention or treatment of itching and pruritus caused by reaction against insect-inflicted wounds, reaction against environmental allergens, skin infections or external parasite infections, or caused to renal dialysis patient.
摘要翻译：提供由以下通式（I）表示的化合物：其中R 1是5-甲基吡啶-2-基，对甲苯基或者间二甲基，R 2是其中R 3是C 1 -C 4烷基，R 4是H或C 1 -C4烷基及其药学上可接受的盐。该化合物显示出瘙痒抑制作用，并且可用于预防或治疗由于对昆虫造成的伤口的反应，对环境变应原的反应，皮肤感染或外部寄生虫感染引起的瘙痒和瘙痒或引起肾透析患者。

76. 发明公开

EP2292594A1 METHOD FOR PRODUCING OPTICALLY ACTIVE AMINOALCOHOL DERIVATIVE 审中-公开
标题翻译： VERFAHREN ZUR HERSTELLUNG EINES OPTISCH AKTIVEN AMINOALKOHOLDERIVATS
公开(公告)号：EP2292594A1
公开(公告)日：2011-03-09
申请号：EP09750556.4
申请日：2009-05-19
申请人： Kyorin Pharmaceutical Co., Ltd.
发明人： TSUBUKI Takeshi , ARAYA Ichiro , KANDA Takahiro , KANAZAWA Shintaro
IPC分类号： C07C319/20 , C07B57/00 , C07C323/32 , C07C323/63
CPC分类号： C07B57/00 , C07B2200/07 , C07C319/20 , C07C323/32
摘要： Disclosed is a preparation method which makes it possible to produce an aminoalcohol derivative having a high optical purity and to enable the large scale synthesis thereof at a low price.
For instance, a compound represented by the following general formula (8) is recrystallized in the course of the production process thereof

In this case, R 1 represents, for instance, a trihalomethyl group; R 2 represents, for instance, a hydrogen atom; R 3 represents, for instance, a halogen atom; R 4 represents, for instance, a lower alkyl group; X represents, for instance, a sulfur atom; n represents an integer ranging from 1 to 4; and W represents hydrogen chloride or hydrogen bromine.
摘要翻译：公开了一种制备方法，其可以生产具有高光学纯度的氨基醇衍生物，并且能够以低价格进行大规模合成。例如，由以下通式（8）表示的化合物在制造过程中重结晶。在这种情况下，R 1表示例如三卤代甲基; R 2表示例如氢原子; R 3表示例如卤素原子; R 4表示例如低级烷基; X表示例如硫原子; n表示1〜4的整数， W表示氯化氢或氢溴。

77. 发明授权

EP1431275B1 DIARYL ETHER DERIVATIVE, ADDITION SALT THEREOF, AND IMMUNOSUPPRESSANT 有权
标题翻译：二芳基醚衍生物，添加盐和免疫抑制剂
公开(公告)号：EP1431275B1
公开(公告)日：2010-04-07
申请号：EP02768056.0
申请日：2002-09-25
申请人： Kyorin Pharmaceutical Co., Ltd.
发明人： KOHNO, Yasushi , ANDO, Naoki , TANASE, Takahiro , KURIYAMA, Kazuhiko , IWANAMI, Satoru , KUDOU, Shinji
IPC分类号： C07C217/34 , C07C217/56 , C07C217/64 , C07C255/54 , C07C317/22 , C07C323/20 , C07D213/30 , A61K31/137 , A61K31/138 , A61K31/277 , A61K31/4409 , A61P11/02 , A61P11/06 , A61P17/00 , A61P17/16 , A61P27/14 , A61P29/00 , A61P37/06 , A61P37/08
CPC分类号： C07D319/06 , C07C217/64
摘要： A diaryl ether derivative having excellent immunosuppressive activity and reduced in side effects. The diaryl ether derivative is represented by the general formula (1): (1) {e.g., 2-amino-2-[4-(3-benzyloxyphenoxy)-2-chlorophenyl]propyl-1,3-propanediol}.

78. 发明公开

EP2116535A1 GLUCOKINASE-ACTIVATING SUBSTANCE 有权
标题翻译：葡萄糖激酶活化物质
公开(公告)号：EP2116535A1
公开(公告)日：2009-11-11
申请号：EP07851044.3
申请日：2007-12-21
申请人： Kyorin Pharmaceutical Co., Ltd. , Teijin Pharma Limited
发明人： FUKUDA, Yasumichi , ASAHINA, Yoshikazu , NAKAMURA, Ayako , FUJITA, Kenji , IDE, Tomohiro , KOBAYASHI, Fumiyoshi , KOBAYASHI, Shinji , KOMATSU, Kanji , YAMAMOTO, Masanori
IPC分类号： C07D213/80 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/426 , A61K31/428 , A61K31/433 , A61K31/437 , A61K31/4375 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4439 , A61K31/455 , A61K31/47 , A61K31/472 , A61K31/4965 , A61K31/50 , A61K31/505
CPC分类号： C07C317/44 , C07C2601/08 , C07D213/75 , C07D213/80 , C07D215/38 , C07D217/22 , C07D231/40 , C07D237/20 , C07D239/42 , C07D241/20 , C07D241/28 , C07D241/44 , C07D261/14 , C07D263/48 , C07D275/02 , C07D277/20 , C07D277/46 , C07D277/82 , C07D285/08 , C07D417/04 , C07D471/04 , C07D487/04 , C07D498/04 , C07D513/04
摘要： A compound represented by the following formula (1):

(wherein the carbon atom denoted by * is in the R-configuration; R 1 and R 2 are each independently a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C 1 -C 6 alkyl group, a C 1 -C 6 alkoxy group, a C 1 -C 6 alkylsulfanyl group, a C 1 -C 6 alkylsulfinyl group or a C 1 -C 6 alkylsulfonyl group; andA is a substituted or unsubstituted heteroaryl group), or a pharmaceutically acceptable salt thereof.

79. 发明授权

EP1486500B1 10-(3-CYCLOPROPYLAMINOMETHYL-1-PYRROLIDINYL)PYRIDOBENZOXAZINECARBOXYLIC ACID DERIVATIVE EFFECTIVE AGAINST RESISTANT BACTERIA 有权
标题翻译： 10-（3 - 丙基氨基CYCLO甲基-1-吡咯烷基）吡啶并苯并恶羧酸衍生物，对抗耐药菌有效
公开(公告)号：EP1486500B1
公开(公告)日：2009-09-16
申请号：EP03708575.0
申请日：2003-03-13
申请人： Kyorin Pharmaceutical Co., Ltd.
发明人： ASAHINA, Yoshikazu , TAKEI, Masaya
IPC分类号： C07D498/06 , A61K31/5383 , A61P31/04
CPC分类号： C07D498/06
摘要： A compound represented by the general formula (I): (I) wherein R1 represents methyl, fluoromethyl, methoxymethyl, acetoxymethyl, hydroxymethyl, or methylene; R2 represents hydrogen, C1-3 alkyl, or a pharmaceutically acceptable ester group of a cation and a prodrug; R3 represents hydrogen or halogeno; R4 represents hydrogen, C1-3 alkyl, fluoromethyl, trifluoromethyl, or fluorine; and R5 represents hydrogen or fluorine. It has excellent antibacterial activity against gram-positive bacteria, in particular, resistant bacteria such as MRSA, PRSP, and VRE.

80. 发明公开

EP2078526A1 AQUEOUS LIQUID PREPARATION HAVING IMPROVED INTRAOCULAR GATIFLOXACIN PENETRATION 审中-公开
标题翻译： WÄSSRIGEFLÜSSIGEZUBEREITUNG MIT VERBESSERTER INTRAOKULARER GATIFLOXACIN-PENETRATION
公开(公告)号：EP2078526A1
公开(公告)日：2009-07-15
申请号：EP07829584.7
申请日：2007-10-11
申请人： Kyorin Pharmaceutical Co., Ltd. , Senju Pharmaceutical Co., Ltd.
发明人： SAWA, Shirou
IPC分类号： A61K31/496 , A61K9/08 , A61K47/02 , A61K47/36 , A61P27/02 , A61P31/04
CPC分类号： A61K31/496 , A61K9/0048 , A61K47/36
摘要： An object is to provide an ophthalmic aqueous preparation excellent in the retention of gatifloxacin in a tear fluid and the preparation of gatifloxacin into an aqueous humor and a conjunctiva. Another object is to prevent the formation of any precipitate and the reduction in viscosity in the aqueous liquid preparation. An aqueous liquid preparation comprising gatifloxacin, a pharmacologically acceptable salt thereof or a hydrate of gatifloxacin or the salt and at least 0.15 w/v% of xanthan gum enables to improve the retention and penetration of gatifloxacin. When at least 0.2 w/v% of sodium chloride is added to the aqueous liquid preparation, the formation of any precipitate and the reduction in viscosity in the aqueous liquid preparation can be prevented.
摘要翻译：本发明的目的是提供在泪液中保留加替沙星和将加替沙星制备成房水和结膜中优异的眼用水制剂。另一个目的是防止水性液体制剂中任何沉淀的形成和粘度降低。包含加替沙星，其药理学上可接受的盐或加替沙星或其盐的水合物和至少0.15w / v％的黄原胶的含水液体制剂能够改善加替沙星的保留和渗透。当向水性液体制剂中加入至少0.2w / v％的氯化钠时，可以防止水性液体制剂中任何沉淀的形成和粘度降低。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式