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1. 发明申请

WO2013189847A1 BENDAMUSTINE DERIVATIVES AND RELATED COMPOUNDS, AND MEDICAL USE THEREOF CANCER THERAPY 审中-公开
标题翻译： BENDAMUSTINE衍生物及相关化合物，以及癌症治疗的医疗用途
公开(公告)号：WO2013189847A1
公开(公告)日：2013-12-27
申请号：PCT/EP2013/062347
申请日：2013-06-14
申请人： SCHICKANEDER, Helmut , SCHICKANEDER, Christian , BUSCHAUER, Armin , BERNHARDT, Günther , HUBER, Stefan , LIMMERT, Michael
发明人： SCHICKANEDER, Helmut , SCHICKANEDER, Christian , BUSCHAUER, Armin , BERNHARDT, Günther , HUBER, Stefan , LIMMERT, Michael , LUBBE, Mathias , HOFMEIER, Harald
IPC分类号： C07D235/12 , A61K31/4184 , A61P35/00
CPC分类号： C07D235/16 , C07C231/02
摘要： The present invention relates to bendamustine derivatives and related compounds of formula (VII), (VIII) and (IX), and medical uses thereof in particular in cancer therapy.
摘要翻译：本发明涉及苯达莫司汀衍生物和式（VII），（VIII）和（IX）的相关化合物及其医疗用途，特别是癌症治疗。

2. 发明申请

WO2010061366A1 MANUFACTURE OF BISOPROLOL AND INTERMEDIATES THEREFOR 审中-公开
标题翻译：双酚A及其中间体的制备
公开(公告)号：WO2010061366A1
公开(公告)日：2010-06-03
申请号：PCT/IE2009/000082
申请日：2009-11-26
申请人： CORDEN PHARMA IP LIMITED , O'NEILL, John, A. , SCHICKANEDER, Helmut , NIKOLOPOULOS, Aggelos , JAS, Gerhard
发明人： O'NEILL, John, A. , SCHICKANEDER, Helmut , NIKOLOPOULOS, Aggelos , JAS, Gerhard
IPC分类号： C07C217/32 , C07D263/14
CPC分类号： C07C217/32 , C07D263/18
摘要： A process for preparing bisoprolol comprises reacting oxazolidinone sulphonate with 4-hydroxybenzylaldehyde to form oxazolidinone benzaldehyde, forming oxazolidone benzylalcohol from oxazolidone benzaldehyde, and subsequently reacting oxazolidinone benzylalcohol with isopropyl oxitol to form bisoprolol base. Oxazolidone sulphonate and oxazolidone benzaldehyde are novel intermediates.
摘要翻译：制备比索洛韦的方法包括使恶唑烷酮磺酸盐与4-羟基苄基醛反应形成恶唑烷酮苯甲醛，由恶唑烷酮苯甲醛形成恶唑烷酮苄醇，随后使恶唑烷酮苄醇与异丙基氧基醇反应形成比索洛尔碱。恶唑烷酮磺酸盐和恶唑烷酮苯甲醛是新的中间体。

3. 发明申请

WO1998005674A1 PROCESS FOR THE PRODUCTION OF SALTS OF ERYTHROMYCIN, ROXITHROMYCIN, CLARITHROMYCIN AND AZITHROMYCIN 审中-公开
标题翻译：生产红霉素，罗红霉素，克拉霉素和阿奇霉素的方法
公开(公告)号：WO1998005674A1
公开(公告)日：1998-02-12
申请号：PCT/IE1997000056
申请日：1997-08-07
申请人： RUSSINSKY LIMITED , SCHICKANEDER, Helmut , NIKOLOPOULOS, Aggelos
发明人： RUSSINSKY LIMITED
IPC分类号： C07H17/08
CPC分类号： C07H17/08 , C07H17/00
摘要： N-acetylcysteine, carboxymethylcysteine and thiazolidincarboxylic acid salts of erythromycin-2-propionate are produced by charging erythromycin-2-propionate and the sulphur-containing acid into a reactor. The reactants are homogenised and milled under nitrogen for 1 - 2 hours at 10 - 20 DEG C. To this mixture purified water is added under nitrogen and the resultant aqueous mixture is further homogenised and milled for 1 to 2 hours at 10 - 30 DEG C under nitrogen to produce a suspension of the desired salt. The suspension is dried under vacuum to produce a high yield of the desired salt at high levels of purity. Carboxymethylcysteine, N-acetylcysteine and thiazolidin-carboxylic acid salt of erythromycin, clarithromycin, roxithromycin and azithromycin may be produced in a similar manner.
摘要翻译：通过将红霉素-2-丙酸酯和含硫酸装入反应器中制备红霉素-2-丙酸的N-乙酰半胱氨酸，羧甲基半胱氨酸和噻唑烷羧酸盐。将反应物均化并在10-20℃下在氮气下研磨1-2小时。向该混合物中加入纯化水，并将所得含水混合物进一步均化并在10-30℃下研磨1至2小时在氮气下产生所需盐的悬浮液。将悬浮液在真空下干燥以产生高纯度的所需盐的高产率。红霉素，克拉霉素，罗红霉素和阿奇霉素的羧甲基半胱氨酸，N-乙酰半胱氨酸和噻唑烷 - 羧酸盐可以以类似的方式制备。

4. 发明申请

WO1996019489A1 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：WO1996019489A1
公开(公告)日：1996-06-27
申请号：PCT/IE1995000065
申请日：1995-12-19
申请人： RUSSINSKY LIMITED , SCHICKANEDER, Helmut , NIKOLOPOULOS, Aggelos , KELLY, Declan
发明人： RUSSINSKY LIMITED
IPC分类号： C07H17/08
CPC分类号： C07H17/08 , C07H17/00
摘要： Antibiotic and mucolytic salts of roxithromycin, clarithromycin and azithromycin are described. Particularly described is roxithromycin stinoprate which was found to be more potent than erythromycin stinoprate.
摘要翻译：描述了罗红霉素，克拉霉素和阿奇霉素的抗生素和粘液溶解盐。特别描述的是硫酸罗红霉素，被发现比雄激素红霉素更有效。

5. 发明申请

WO2015091827A1 BENDAMUSTINE DERIVATIVES AND RELATED COMPOUNDS 审中-公开
标题翻译： BENDAMUSTINE衍生物及相关化合物
公开(公告)号：WO2015091827A1
公开(公告)日：2015-06-25
申请号：PCT/EP2014/078509
申请日：2014-12-18
申请人： SCHICKANEDER, Helmut
发明人： SCHICKANEDER, Helmut , SCHICKANEDER, Christian , BUSCHAUER, Armin , BERNHARDT, Günther , HUBER, Stefan , ANTONI, Frauke
IPC分类号： C07D235/16 , A61K31/4184
CPC分类号： C07D235/16
摘要： The present invention relates to bendamustine derivatives and related compounds as well as their medical application.
摘要翻译：本发明涉及苯达莫司汀衍生物及其相关化合物及其医疗应用。

6. 发明申请

WO0066174A3 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：WO0066174A3
公开(公告)日：2001-03-15
申请号：PCT/IE0000041
申请日：2000-04-04
申请人： RUSSINSKY LTD , SCHICKANEDER HELMUT , KIKOLOPOULOS AGGELOS , HERMANN GESINE
发明人： SCHICKANEDER HELMUT , KIKOLOPOULOS AGGELOS , HERMANN GESINE
IPC分类号： A61K31/00 , A61K31/341 , A61K31/7048 , A61K47/48 , A61P1/04 , A61P31/04
CPC分类号： A61K47/552
摘要： An adduct contains Clarithromycin and Ranitidine either in the form of a base or a base hydrate in which the molar ratio of Clarithromycin to Ranitidine in the adduct is at least 2:1. The adduct has high stability and is particularly useful in a single dose formulation for the treatment of gastrointestinal disorders.
摘要翻译：加合物含有克拉霉素和雷尼替丁，其形式为碱或水合物，其中加合物中克拉霉素与雷尼替丁的摩尔比至少为2:1。加合物具有高稳定性，并且在用于治疗胃肠道疾病的单剂量制剂中特别有用。

7. 发明申请

WO9903821A3 PROCESS FOR ISOMERISATION OF TILIDINE 审中-公开
标题翻译：酪氨酸异构化方法
公开(公告)号：WO9903821A3
公开(公告)日：1999-05-20
申请号：PCT/IE9800052
申请日：1998-06-26
申请人： RUSSINSKY LTD , NIKOLOPOULOS ANGELO , SCHICKANEDER HELMUT , MULCAHY DAVID
发明人： NIKOLOPOULOS ANGELO , SCHICKANEDER HELMUT , MULCAHY DAVID
IPC分类号： C07C227/36 , C07C229/48
CPC分类号： C07C227/36 , C07B2200/07 , C07C2601/16 , C07C229/48
摘要： Cis/trans Tilidine base with an enhanced content of the trans isomer is prepared by mixing a substantially pure cis Tilidine base with water under acidic conditions, preferably using phosphoric acid, at pH values between 2 to 6. Alternatively the substantially pure cis Tilidine base is mixed with a solvent, especially diisopropylethylamine or dimethylformamide under basic conditions at pH values of from 8 to 14. The reaction mixtures thus formed are heated to yield isomerised cis/trans Tilidine base with an enhanced content of the trans isomer.
摘要翻译：通过在酸性条件下，优选使用磷酸，在2至6的pH值下，将基本上纯的顺式替利陆碱与水混合来制备具有增强的反式异构体含量的顺式/反式替利陆碱。或者，基本上纯的顺式替赖啶碱是在碱性条件下在8至14的pH值下与溶剂，特别是二异丙基乙胺或二甲基甲酰胺混合。将由此形成的反应混合物加热，得到具有增强的反式异构体含量的异构化顺式/反式替利啶碱。

8. 发明申请

WO1996019232A1 COMBINATIONS OF RANITIDINE HYDROCHLORIDE-FORM 1 AND BISMUTH COMPOUNDS 审中-公开
标题翻译： RANITIDINE HYDROCHLORIDE-FORM 1和BISMUTH化合物的组合
公开(公告)号：WO1996019232A1
公开(公告)日：1996-06-27
申请号：PCT/IE1995000015
申请日：1995-02-03
申请人： LAUTERAL LIMITED , SCHICKANEDER, Helmut , NIKOLOPOULOS, Aggelos
发明人： LAUTERAL LIMITED
IPC分类号： A61K33/24
CPC分类号： A61K31/426 , A61K2300/00
摘要： Combination products of Ranitidine hydrochloride - Form 1 and bismuth compounds for the treatment of gastro-intestinal disorders are described. The products may also be used in association with antibiotics such as nitazoxanide.
摘要翻译：描述了雷尼替丁盐酸盐 - 形式1和铋化合物用于治疗胃肠道疾病的组合产物。这些产品也可以与抗生素例如硝唑尼特一起使用。

9. 发明申请

WO1996019220A1 A COMBINATION PRODUCT COMPRISING NITAZOXANIDE AND AN ANTI-ULCER AGENT 审中-公开
标题翻译：包含NITAZOXANIDE和ANTI-ULCER代理的组合产品
公开(公告)号：WO1996019220A1
公开(公告)日：1996-06-27
申请号：PCT/IE1995000064
申请日：1995-12-19
申请人： LAUTERAL LIMITED , SCHICKANEDER, Helmut , NIKOLOPOULOS, Aggelos
发明人： LAUTERAL LIMITED
IPC分类号： A61K31/425
CPC分类号： A61K31/426 , A61K2300/00
摘要： A combination of nitazoxanide with an anti-ulcer agent, especially ranitidine has a synergistic therapeutic profile in prophylaxis or treatment of H. pylori related infections. The product may also contain, as an antibacterial agent, bismuth salts such as bismuth subsalicylate or bismuth citrate.
摘要翻译：硝唑尼特与抗溃疡剂的组合，特别是雷尼替丁在预防或治疗幽门螺杆菌相关感染方面具有协同的治疗特征。该产品还可以含有作为抗菌剂的铋盐，例如二水杨酸铋或柠檬酸铋。

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