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1.发明专利Pyroglutamate salt and use of the same in optical resolution of intermediate for synthesis of dextrocetirizine and levocetirizine 审中-公开吡喃葡萄糖盐及其在中间体光合作用中的用途，用于合成去氧胆酸酯酶和左旋胆碱酯酶
公开(公告)号：JP2013032380A
公开(公告)日：2013-02-14
申请号：JP2012226914
申请日：2012-10-12
Applicant: Ucb Farchim Sa , ユセベ ファルシム ソシエテ アノニム
Inventor： PALACIO MAGALI , ATES CELAL
IPC: C07D295/08 , C07B57/00 , C07D207/28
CPC classification number: C07D295/088 , C07D207/28
Abstract: PROBLEM TO BE SOLVED: To provide a simpler preparation method for an enantiomerically and essentially pure compound like levocetirizine or the like by using a novel and enantiomerically and essentially pure intermediate.SOLUTION: There is provided a (S)-2-[4-(4-chlorobenzhydryl)piperazine-1-yl]-ethoxyacetamide-(S)-pyrrolidone-5-carboxylic acid salt, (R)-2-[4-(4-chlorobenzhydryl)piperazine-1-yl]-ethoxyacetamide-(S)-pyrrolidone-5-carboxylic acid salt, (S)-2-[4-(4-chlorobenzhydryl)piperazine-1-yl]-ethoxyacetamide-(R)-pyrrolidone-5-carboxylic acid salt, or (R)-2-[4-(4-chlorobenzhydryl)piperazine-1-yl]-ethoxyacetamide-(R)-pyrrolidone-5-carboxylic acid salt. There is also provided the preparation method for (S)-2-[4-(4-chlorobenzhydryl)piperazine-1-yl]-ethoxyacetamide (I) and (R)-2-[4-(4-chlorobenzhydryl)piperazine-1-yl]-ethoxyacetamide (II) by chemical resolution of a mixture.
Abstract translation: 要解决的问题：通过使用新型和对映体和基本上纯的中间体，为对映异构体和基本上纯的化合物如左西替利嗪等提供更简单的制备方法。 提供了（S）-2- [4-（4-氯二苯甲基）哌嗪-1-基] - 乙氧基乙酰胺 - （S） - 吡咯烷酮-5-羧酸盐，（R）-2- [（4-氯二苯甲基）哌嗪-1-基] - 乙氧基乙酰胺 - （S） - 吡咯烷酮-5-羧酸盐，（S）-2- [4-（4-氯二苯甲基）哌嗪-1-基] 乙氧基乙酰胺 - （R） - 吡咯烷酮-5-羧酸盐或（R）-2- [4-（4-氯二苯甲基）哌嗪-1-基] - 乙氧基乙酰胺 - （R） - 吡咯烷酮-5-羧酸盐。 还提供了（S）-2- [4-（4-氯二苯甲基）哌嗪-1-基] - 乙氧基乙酰胺（I）和（R）-2- [4-（4-氯二苯甲基）哌嗪-1-基] 吡啶-1-基] - 乙氧基乙酰胺（II）。 版权所有（C）2013，JPO＆INPIT
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公开(公告)号：JP2007176958A
公开(公告)日：2007-07-12
申请号：JP2007092969
申请日：2007-03-30
Applicant: Ucb Farchim Sa , ユセベ ファルシム ソシエテ アノニム
Inventor： FANARA DOMENICO , GUICHAUX ANTHONY , BERWAER MONIQUE , DELEERS MICHEL
IPC: A61J1/03 , A61K31/475 , A61K20060101 , A61K9/20 , A61K9/24 , A61K9/26 , A61K31/137 , A61K31/495 , A61K47/36 , A61K47/38 , A61P11/00 , A61P11/02 , A61P27/02 , A61P27/14 , A61P37/08 , A61P43/00 , C07D295/08
CPC classification number: A61K31/137 , A61K9/209 , A61K31/495 , A61K2300/00
Abstract: PROBLEM TO BE SOLVED: To provide a medicine having the practically same pharmacodynamic profiles of cetirizine and pseudoephedrine as those in a medicine administration type containing the same amount of cetirizine and pseudoephedrine discretely as the discrete active ingredients. SOLUTION: The tablet comprises at least two discrete segments, one of which mainly contains the cetirizine as the active ingredient and the other second segment mainly contains the pseudoephedrine as the active ingredient, wherein the pseudoephedrine segment and the cetirizine segment contact directly and their interfacial surface area is 2 . COPYRIGHT: (C)2007,JPO&INPIT
Abstract translation: 待解决的问题：提供具有与含有相同量的西替利嗪和伪麻黄碱作为离散活性成分的药物给药型相同的西替立嗪和伪麻黄碱具有实际相同的药效学特征的药物。 解决方案：片剂包含至少两个离散区段，其中一个主要含有西替利嗪作为活性成分，另一个第二部分主要含有伪麻黄碱作为活性成分，其中伪麻黄碱片段和西替立嗪片段直接接触， 它们的界面面积<180mm
2 。 版权所有（C）2007，JPO＆INPIT -
3.发明专利2-oxo-1-pyrrolidine derivatives, process for preparing them and their uses 有权2-氧代-1-吡咯烷衍生物，其制备方法及其用途
公开(公告)号：JP2007182459A
公开(公告)日：2007-07-19
申请号：JP2007102379
申请日：2007-04-10
Applicant: Ucb Farchim Sa (Ag-Ltd) , ユセベ ファルシム ソシエテ アノニム(アーゲー − リミテッド)
Inventor： SURTEES JOHN , MARMON VIOLETA , DIFFERDING EDMOND , VINCENT ZIMMERMANN
IPC: C07D207/27 , C07D401/04 , A61K31/4015 , A61K31/4025 , A61K31/41 , A61K31/4178 , A61K31/4188 , A61K31/4192 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/427 , A61K31/433 , A61K31/4439 , A61K31/497 , A61K31/506 , A61K31/541 , A61P9/00 , A61P9/06 , A61P9/10 , A61P11/00 , A61P11/06 , A61P21/00 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P27/16 , A61P37/08 , C07B61/00 , C07C237/06 , C07C237/12 , C07D207/26 , C07D207/273 , C07D207/277 , C07D307/33 , C07D401/06 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04 , C07D495/04
CPC classification number: C07D207/26 , A61K31/4015 , C07C237/12 , C07D207/27 , C07D207/273 , C07D207/277 , C07D307/33 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/12 , C07D409/04 , C07D413/04 , C07D417/04 , C07D495/04
Abstract: PROBLEM TO BE SOLVED: To provide a new intermediate in a method for preparing 2-oxo-1-pyrrolidine derivatives. SOLUTION: The compound having the general formula (A) (X is -CONR 5 R 6 , -COOR 7 , -CO-R 8 , or CN; R 1 is H or the like; R 2 and R 4 are each identically or differently independently H or the like; R 3 is H or the like; R 5 , R 6 and R 7 are each identically or differently independently H or the like; R 8 is H or the like), or a pharmaceutically acceptable salt thereof; the compound including methyl 2-[4R,S-isopropyl-2-oxo-pyrrolidin-1-yl]acrylate and methyl 2-[3R,S-chloro-4R,S-isopropyl-2-oxo-pyrrolidin-1-yl]acrylate. COPYRIGHT: (C)2007,JPO&INPIT
Abstract translation: 待解决的问题：在制备2-氧代-1-吡咯烷衍生物的方法中提供新的中间体。 解决方案：具有通式（A）的化合物（X为-CONR 5，R SP 6，-COOR 7，-CO， -R
8 或CN; R 1 是H等; R SP＆gt; 2＆lt; SP＆gt;和＆lt; SP＆gt; 4＆lt; / SP＆ 相同或不同的独立的H等; R 3是H等; R 6，R 6，R 6， / SP>各自相同或不同地独立地为H等; R 6为H等）或其药学上可接受的盐; 该化合物包括2- [4R，S-异丙基-2-氧代 - 吡咯烷-1-基]丙烯酸甲酯和2- [3R，S-氯-4R，S-异丙基-2-氧代 - 吡咯烷-1-基 ]丙烯酸甲酯。 版权所有（C）2007，JPO＆INPIT -
公开(公告)号：JP2014024866A
公开(公告)日：2014-02-06
申请号：JP2013228128
申请日：2013-11-01
Applicant: Ucb Farchim Sa , ユセベ ファルシム ソシエテ アノニム
Inventor： FANARA DOMENICO , BERWAER MONIQUE , GUICHAUX ANTHONY , DELEERS MICHEL
IPC: A61K9/10 , A61K31/495 , A61K9/00 , A61K9/08 , A61K9/14 , A61K9/16 , A61K9/20 , A61K9/24 , A61K9/28 , A61K9/68 , A61K47/04 , A61K47/10 , A61K47/12 , A61K47/16 , A61K47/22 , A61K47/26 , A61K47/36 , A61K47/38 , A61K47/40 , A61K47/42 , G01N33/53
CPC classification number: A61K9/0095 , A61K9/0056 , A61K9/0058 , A61K9/2086 , A61K9/2826 , A61K31/495
Abstract: PROBLEM TO BE SOLVED: To provide a stable pharmaceutical composition for oral administration of an active compound.SOLUTION: The pharmaceutical composition for oral administration contains at least two separate formulations. A first formulation, which contains the active compound selected from 2-[4-(diphenylmethyl)-1-piperazinyl]-acetic acids and their amides, does not contain polyols having a molecular weight of less than 950 in a molar ratio between the polyols and the active compound represented by formula I above 10. Lactose is an exception. A second formulation contains one or more solid polyols of a molecular weight of less than 3,000 and is free of any drug. The composition is a dry syrup composition.
Abstract translation: 要解决的问题：提供用于口服给予活性化合物的稳定的药物组合物。溶液：用于口服给药的药物组合物含有至少两种分开的制剂。 包含选自2- [4-（二苯基甲基）-1-哌嗪基] - 乙酸及其酰胺的活性化合物的第一制剂不含多元醇，其分子量小于950，多元醇 和上述式I表示的活性化合物。乳糖是例外。 第二种制剂含有一种或多种分子量小于3,000的固体多元醇，并且不含任何药物。 组合物是干糖浆组合物。
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公开(公告)号：JP2012121917A
公开(公告)日：2012-06-28
申请号：JP2012051259
申请日：2012-03-08
Applicant: Ucb Farchim Sa , ユセベ ファルシム ソシエテ アノニム
Inventor： FANARA DOMENICO , BERWAER MONIQUE , GUICHAUX ANTHONY , DELEERS MICHEL
IPC: A61K9/10 , A61K31/495 , A61K9/00 , A61K9/08 , A61K9/14 , A61K9/16 , A61K9/20 , A61K9/24 , A61K9/28 , A61K9/68 , A61K47/02 , A61K47/04 , A61K47/10 , A61K47/12 , A61K47/16 , A61K47/22 , A61K47/26 , A61K47/34 , A61K47/36 , A61K47/38 , A61K47/40 , A61K47/42 , A61K47/44 , A61P11/02 , A61P29/00 , A61P37/08 , A61P43/00 , G01N33/53
CPC classification number: A61K9/0095 , A61K9/0056 , A61K9/0058 , A61K9/2086 , A61K9/2826 , A61K31/495
Abstract: PROBLEM TO BE SOLVED: To provide a stable pharmaceutical composition for oral administration of an active compound.SOLUTION: The oral drug composition includes at least two different formulations, or a first formulation including an active compound selected from 2-[4-(diphenylmethyl)-1-pyperadinyl]-acetic acid and amides thereof, the first formulation not including, except lactose, a polyol having a molecular weight of less than 950 in a mole ratio exceeding 10 of the active compound of formula I; and a second formulation including one or more solid polyols having a molecular weight of less than 3,000, the second formulation including no medicinal substances. The composition has a form of dry syrup.
Abstract translation: 待解决的问题：提供用于口服给予活性化合物的稳定的药物组合物。 口服药物组合物包含至少两种不同的制剂，或包含选自2- [4-（二苯基甲基）-1-芘二乙烯基] - 乙酸及其酰胺的活性化合物的第一制剂，第一制剂不 包括除乳糖外，分子量小于950的摩尔比超过10的式I的活性化合物的多元醇; 以及包含分子量小于3,000的一种或多种固体多元醇的第二种制剂，所述第二制剂不包括药物。 该组合物具有干糖浆的形式。 版权所有（C）2012，JPO＆INPIT
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Patent Agency Ranking
公开(公告)号：JP2010120963A
公开(公告)日：2010-06-03
申请号：JP2010035633
申请日：2010-02-22
Applicant: Ucb Farchim Sa , ユセベ ファルシム ソシエテ アノニム
Inventor： FANARA DOMENICO , BERWAER MONIQUE , GUICHAUX ANTHONY , DELEERS MICHEL
IPC: A61K9/10 , A61K31/495 , A61K9/00 , A61K9/14 , A61K9/16 , A61K9/20 , A61K9/28 , A61K9/68 , A61K47/02 , A61K47/04 , A61K47/10 , A61K47/12 , A61K47/16 , A61K47/22 , A61K47/36 , A61K47/38 , A61K47/40 , A61K47/42 , A61P29/00 , A61P43/00 , G01N33/53
CPC classification number: A61K9/0095 , A61K9/0056 , A61K9/0058 , A61K9/2086 , A61K9/2826 , A61K31/495
Abstract: PROBLEM TO BE SOLVED: To provide a stable pharmaceutical composition for oral administration of an active compound.
SOLUTION: The pharmaceutical composition for oral administration contains at least two separate formulations. A first formulation, which contains the active component selected from 2-[4-(diphenylmethyl)-1-piperazinyl]-acetic acids and their amides, does not contain polyols having a molecular weight of less than 950 in a molar ratio between the polyols and the active compound represented by formula I above 10. Lactose is an exception. A second formulation contains one or more solid polyols of a molecular weight of less than 3,000 and is free of any drug. The composition is a dry syrup composition.
COPYRIGHT: (C)2010,JPO&INPITAbstract translation: 待解决的问题：提供用于口服给予活性化合物的稳定的药物组合物。 解决方案：用于口服给药的药物组合物含有至少两种分开的制剂。 含有选自2- [4-（二苯基甲基）-1-哌嗪基] - 乙酸及其酰胺的活性成分的第一制剂不含多元醇，其分子量小于950，多元醇 和上述式I表示的活性化合物。乳糖是例外。 第二种制剂含有一种或多种分子量小于3,000的固体多元醇，并且不含任何药物。 组合物是干糖浆组合物。 版权所有（C）2010，JPO＆INPIT
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7.发明专利2-氧基-1-咯啶衍生物之製法 PROCESS FOR PREPARING 2-OXO-1-PYRROLIDINE DERIVATIVES 失效2-氧基-1-咯啶衍生物之制法 PROCESS FOR PREPARING 2-OXO-1-PYRROLIDINE DERIVATIVES
公开(公告)号：TWI308912B
公开(公告)日：2009-04-21
申请号：TW090107984
申请日：2001-04-03
Applicant: 優稀美法契姆股份有限公司 UCB FARCHIM SA
Inventor： 約翰蘇帝斯 JOHN SURTEES , 維爾利特瑪孟 VIOLETA MARMON , 艾德蒙迪弗丁 EDMOND DIFFERDING , 文生齊麥曼 VINCENT ZIMMERMANN
IPC: C07D
Abstract: 本發明係有關2-氧-1-咯啶衍生物及其製法及其用途。本發明亦係關於由未飽和2-氧基-1-咯啶衍生物製備���-乙基-2-氧基-1-咯啶乙醯胺衍生物之方法。
特別本發明係有關新穎中間及其用於製備S-���-乙基-2-氧基-1-咯啶乙醯胺之方法。Abstract in simplified Chinese: 本发明系有关2-氧-1-咯啶衍生物及其制法及其用途。本发明亦系关于由未饱和2-氧基-1-咯啶衍生物制备���-乙基-2-氧基-1-咯啶乙酰胺衍生物之方法。 特别本发明系有关新颖中间及其用于制备S-���-乙基-2-氧基-1-咯啶乙酰胺之方法。
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8.发明专利2-氧基-1-咯啶衍生物,其製法及用途 2-OXO-1-PYRROLIDINE DERIVATIVES, PROCESS FOR PREPARING THEM AND THEIR USES 审中-公开2-氧基-1-咯啶衍生物,其制法及用途 2-OXO-1-PYRROLIDINE DERIVATIVES, PROCESS FOR PREPARING THEM AND THEIR USES
公开(公告)号：TW200536828A
公开(公告)日：2005-11-16
申请号：TW094125252
申请日：2001-04-03
Applicant: 優稀美法契姆股份有限公司 UCB FARCHIM SA
Inventor： 約翰蘇帝斯 SURTEES, JOHN , 維爾利特瑪孟 MARMON, VIOLETA , 艾德蒙迪弗丁 DIFFERDING, EDMOND , 文生齊麥曼 ZIMMERMANN, VINCENT
Abstract: 本發明係有關2–氧–1–咯啶衍生物及其製法及其用途。本發明亦係關於由未飽和2–氧基–1–咯啶衍生物製備α–乙基–2–氧基–1–咯啶乙醯胺衍生物之方法。特別本發明係有關新穎中間及其用於製備S–α–乙基–2–氧基–1–咯啶乙醯胺之方法。094125252-p01.bmp
Abstract in simplified Chinese: 本发明系有关2–氧–1–咯啶衍生物及其制法及其用途。本发明亦系关于由未饱和2–氧基–1–咯啶衍生物制备α–乙基–2–氧基–1–咯啶乙酰胺衍生物之方法。特别本发明系有关新颖中间及其用于制备S–α–乙基–2–氧基–1–咯啶乙酰胺之方法。094125252-p01.bmp
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公开(公告)号：WO2006005507A3
公开(公告)日：2006-04-27
申请号：PCT/EP2005007340
申请日：2005-07-07
Applicant: UCB FARCHIM SA , FANARA DOMENICO , SCOUVART JEAN , POULAIN CLAIRE , DEELERS MICHEL
Inventor： FANARA DOMENICO , SCOUVART JEAN , POULAIN CLAIRE , DEELERS MICHEL
IPC: A61K9/08 , A61K31/495
CPC classification number: A61K47/14 , A61K9/0043 , A61K9/0048 , A61K9/0095 , A61K31/495
Abstract: The present invention relates to a liquid composition containing an active substance belonging to the family of substituted benzhydryl piperazines with reduced amounts of preservatives.
Abstract translation: 本发明涉及含有具有减少量的防腐剂的取代的二苯甲基哌嗪类的活性物质的液体组合物。
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公开(公告)号：WO2006005507A2
公开(公告)日：2006-01-19
申请号：PCT/EP2005/007340
申请日：2005-07-07
Applicant: UCB FARCHIM SA , FANARA, Domenico , SCOUVART, Jean , POULAIN, Claire , DEELERS, Michel
Inventor： FANARA, Domenico , SCOUVART, Jean , POULAIN, Claire , DEELERS, Michel
IPC: C07D487/04
CPC classification number: A61K47/14 , A61K9/0043 , A61K9/0048 , A61K9/0095 , A61K31/495
Abstract: The present invention relates to a liquid composition containing an active substance belonging to the family of substituted benzhydryl piperazines with reduced amounts of preservatives.
Abstract translation: 本发明涉及一种液体组合物，其含有属于取代的二苯甲基哌嗪类的活性物质，其中防腐剂的量降低。
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