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1. 发明申请

WO2009115334A2 PROCESS FOR THE MANUFACTURE OF MEMANTINE AND INTERMEDIATE PRODUCT 审中-公开
标题翻译：制造和中间产品的过程
公开(公告)号：WO2009115334A2
公开(公告)日：2009-09-24
申请号：PCT/EP2009002049
申请日：2009-03-19
申请人： MERZ PHARMA GMBH & CO KGAA , HUBER FLORIAN ANTON MARTIN , GALLO GIORGIO , DE FAVERI CARLA
发明人： HUBER FLORIAN ANTON MARTIN , GALLO GIORGIO , DE FAVERI CARLA
IPC分类号： C07C231/08 , C07C233/03
CPC分类号： C07C231/08 , C07C2603/74 , C07C233/03
摘要： The present invention relates to a process for manufacturing N-Formyl-1-amino-3,5-dimethyladamantane, an intermediate product in the overall process of producing 1-Amino-3,5-dimethyladamantane hydrochloride (Memantine). Therein, the process comprises the following steps: (a) reacting 1,3-dimethyladamantane with an acid mixture comprising concentrated sulfuric acid and concentrated nitric acid, wherein 1 to 6 volume parts of sulfuric acid (measured in ml) are used per weight part of 1,3-dimethyladamantane (measured in g); (b) reacting the solution from step (a) with an amount of formamide varying from 1 to 5 molar equivalents per mole of deprotonated 1,3-dimethyladamantane from step (a) to obtain N-Formyl-1-amino-3,5-dimethyladamantane. In step (b), the molar ratio of total acid, i.e. the molar amount of sulfuric acid and the molar amount of nitric acid taken together versus the molar amount of formamide is at least 1.5 and that the temperature is at least 5O0C. The present invention also relates to the overall process of manufacturing Memantine from 1,3-dimethyladamantane by means of hydrolyzing the intermediate NFORM.
摘要翻译：本发明涉及N-甲酰基-1-氨基-3,5-二甲基金刚烷的制备方法，该方法是制备1-氨基-3,5-二甲基金刚烷盐酸盐（美金刚）的总体方法中的中间产物。其中，该方法包括以下步骤：（a）使1,3-二甲基金刚烷与包含浓硫酸和浓硝酸的酸混合物反应，其中使用1至6体积份硫酸（以ml计）以重量份计的1,3-二甲基金刚烷（以g计）; （b）使来自步骤（a）的溶液与从步骤（a）中每摩尔脱质子化的1,3-二甲基金刚烷的1至5摩尔当量变化的甲酰胺反应得到N-甲酰基-1-氨基-3,5 -dimethyladamantane。在步骤（b）中，总酸的摩尔比，即硫酸的摩尔量和硝酸的摩尔量相对于甲酰胺的摩尔量的摩尔比为至少1.5，温度为至少50℃。本发明还涉及通过水解中间体NFORM从1,3-二甲基金刚烷制造美金刚的整个方法。

2. 发明申请

WO2011134724A2 METHOD FOR PREPARING RITODRINE HYDROCHLORIDE 审中-公开
标题翻译：制备盐酸氯吡格雷的方法
公开(公告)号：WO2011134724A2
公开(公告)日：2011-11-03
申请号：PCT/EP2011/054565
申请日：2011-03-24
申请人： LUNDBECK PHARMACEUTICALS ITALY S.P.A. , ZANON, Jacopo , LIBRALON, Giovanna , DE FAVERI, Carla , HUBER, Florian Anton Martin
发明人： ZANON, Jacopo , LIBRALON, Giovanna , DE FAVERI, Carla , HUBER, Florian Anton Martin
IPC分类号： C07C215/60
CPC分类号： C07C215/60 , C07C213/08 , C07C213/10
摘要： The present invention describes a new method for preparing Ritodrinehydrochloride.The invention also concerns non-hygroscopic crystalline polymorphic Ritodrine hydrochloride Form (I).
摘要翻译：本发明描述了一种制备盐酸利多替罗的新方法。本发明还涉及非吸湿结晶多晶型盐酸雷托方（I）。

3. 发明申请

WO2010063292A1 NALMEFENE HYDROCHLORIDE DIHYDRATE 审中-公开
标题翻译： NALMEFENE氢氯化物二水合物
公开(公告)号：WO2010063292A1
公开(公告)日：2010-06-10
申请号：PCT/DK2009/050320
申请日：2009-12-04
申请人： H. LUNDBECK A/S , BIOTIE THERAPIES CORP. , LOPEZ DE DIEGO, Heidi , DE FAVERI, Carla , HUBER, Florian Anton Martin
发明人： LOPEZ DE DIEGO, Heidi , DE FAVERI, Carla , HUBER, Florian Anton Martin
IPC分类号： C07D489/08 , A61K31/485 , A61P25/30
CPC分类号： C07D489/08
摘要： The present invention relates to the Nalmefene hydrochloride dihydrate, methods of manufacturing Nalmefene hydrochloride dihydrate, a pharmaceutical composition comprising Nalmefene hydrochloride dihydrate and a method of treatment comprising administering Nalmefene hydrochloride dehydrate.
摘要翻译：本发明涉及盐酸纳美芬，二水合盐酸纳美芬的制备方法，盐酸纳美芬酸二水合物的药物组合物及其制备方法，该方法包括给予盐酸纳美芬无水物。

4. 发明申请

WO2010136039A1 PREPARATION OF NALMEFENE HYDROCHLORIDE FROM NALTREXONE 审中-公开
标题翻译：从NALTREXONE制备NALMEFENE HYDROCHLORIDE
公开(公告)号：WO2010136039A1
公开(公告)日：2010-12-02
申请号：PCT/DK2010/050110
申请日：2010-05-21
申请人： H. LUNDBECK A/S , DE FAVERI, Carla , CASARIN, Mauro , BRUSEGAN, Michele
发明人： DE FAVERI, Carla , CASARIN, Mauro , BRUSEGAN, Michele
IPC分类号： C07D489/08
CPC分类号： C07D489/08
摘要： Method for producing nalmefene hydrochloride from naltrexone, which method is particular well adapted for large-scale industrial application, and has been found to be efficient, to give a high yield and to afford highly pure nalmefene hydrochloride salt.
摘要翻译：从纳曲酮生产盐酸纳美芬的方法，该方法特别适用于大规模工业应用，已被发现是有效的，以获得高产率并提供高纯度的纳美芬盐酸盐。

5. 发明申请

WO2009115334A3 PROCESS FOR THE MANUFACTURE OF MEMANTINE AND INTERMEDIATE PRODUCT 审中-公开
公开(公告)号：WO2009115334A3
公开(公告)日：2009-09-24
申请号：PCT/EP2009/002049
申请日：2009-03-19
申请人： MERZ PHARMA GMBH & CO. KGAA , HUBER, Florian, Anton, Martin , GALLO, Giorgio , DE FAVERI, Carla
发明人： HUBER, Florian, Anton, Martin , GALLO, Giorgio , DE FAVERI, Carla
IPC分类号： C07C231/08 , C07C233/03
摘要： The present invention relates to a process for manufacturing N-Formyl-1-amino-3,5-dimethyladamantane, an intermediate product in the overall process of producing 1-Amino-3,5-dimethyladamantane hydrochloride (Memantine). Therein, the process comprises the following steps: (a) reacting 1,3-dimethyladamantane with an acid mixture comprising concentrated sulfuric acid and concentrated nitric acid, wherein 1 to 6 volume parts of sulfuric acid (measured in ml) are used per weight part of 1,3-dimethyladamantane (measured in g); (b) reacting the solution from step (a) with an amount of formamide varying from 1 to 5 molar equivalents per mole of deprotonated 1,3-dimethyladamantane from step (a) to obtain N-Formyl-1-amino-3,5-dimethyladamantane. In step (b), the molar ratio of total acid, i.e. the molar amount of sulfuric acid and the molar amount of nitric acid taken together versus the molar amount of formamide is at least 1.5 and that the temperature is at least 5O0C. The present invention also relates to the overall process of manufacturing Memantine from 1,3-dimethyladamantane by means of hydrolyzing the intermediate NFORM.

6. 发明申请

WO2012059103A1 METHOD FOR THE MANUFACTURING OF NALTREXONE 审中-公开
标题翻译：制备NALTREXONE的方法
公开(公告)号：WO2012059103A1
公开(公告)日：2012-05-10
申请号：PCT/DK2011/000128
申请日：2011-11-04
申请人： H. LUNDBECK A/S , DE FAVERI, Carla , HUBER, Florian, Anton, Martin , STIVANELLO, Mariano
发明人： DE FAVERI, Carla , HUBER, Florian, Anton, Martin , STIVANELLO, Mariano
IPC分类号： C07D489/12 , C07D489/08
CPC分类号： C07D489/08
摘要： The present invention relates to an improved process for producing naltrexone [17- (cyclopropylmethyl)-4,5α-epoxy-3,14-dihydroxy-morphinan-6-one] from noroxymorphone [4,5- α-epoxy-3,14-dihydroxy-morphinan-6-one] by alkylation with a cyclopropylmethyl halide.
摘要翻译：本发明涉及一种从诺羟吗啡酮[4,5- a-环氧-3,14]制备纳曲酮[17-（环丙基甲基）-4,5a-环氧-3,14-二羟基吗啡喃-6-酮]的改进方法 - 二羟基吗啡喃-6-酮]通过用环丙基甲基卤化物烷基化。

7. 发明申请

WO2011134724A3 METHOD FOR PREPARING RITODRINE HYDROCHLORIDE 审中-公开
标题翻译：制备盐酸氯吡格雷的方法
公开(公告)号：WO2011134724A3
公开(公告)日：2012-03-15
申请号：PCT/EP2011054565
申请日：2011-03-24
申请人： LUNDBECK PHARMACEUTICALS ITALY S P A , ZANON JACOPO , LIBRALON GIOVANNA , DE FAVERI CARLA , HUBER FLORIAN ANTON MARTIN
发明人： ZANON JACOPO , LIBRALON GIOVANNA , DE FAVERI CARLA , HUBER FLORIAN ANTON MARTIN
IPC分类号： C07C215/60 , C07C213/08 , C07C213/10
CPC分类号： C07C215/60 , C07C213/08 , C07C213/10
摘要： The present invention describes a new method for preparing Ritodrinehydrochloride.The invention also concerns non-hygroscopic crystalline polymorphic Ritodrine hydrochloride Form (I).
摘要翻译：本发明描述了一种制备盐酸利多替罗的新方法。本发明还涉及非吸湿结晶多晶型盐酸雷托方（I）。

8. 发明申请

WO2009033488A1 METHOD FOR MANUFACTURE OF ESCITALOPRAM 审中-公开
标题翻译：制造方法
公开(公告)号：WO2009033488A1
公开(公告)日：2009-03-19
申请号：PCT/DK2008/050222
申请日：2008-09-10
申请人： H. LUNDBECK A/S , DE FAVERI, Carla , HUBER, Florian Anton Martin , DANCER, Robert James
发明人： DE FAVERI, Carla , HUBER, Florian Anton Martin , DANCER, Robert James
IPC分类号： C07C253/34 , C07C255/53 , C07D307/87
CPC分类号： C07D307/87 , C07C253/34 , C07C255/59
摘要： This patent discloses a method for resolution of 4-[4-(dimethylamino)-1-(4´-fluorophenyl)-1-hydroxybutyl]-3-(hydroxymethyl)-benzonitrile as a racemic or non-racemic enantiomer mixture into its isolated enantiomers, said method comprising the step of fractionally crystallising 4-[4-(dimethylamino)-1-(4´-fluoro-phenyl)-1-hydroxybutyl]-3-(hydroxymethyl)-benzonitrile as a salt with the (+)-(S,S)- or (-)-(R,R)-enantiomer of O,O'-di- p -toluoyl-tartaric acid in a solvent system comprising 1-propanol, ethanol or acetonitrile.
摘要翻译：该专利公开了将4- [4-（二甲基氨基）-1-（4'-氟苯基）-1-羟基丁基] -3-（羟基甲基） - 苄腈作为外消旋或非外消旋对映异构体混合物分离成其分离的方法所述方法包括将4- [4-（二甲基氨基）-1-（4'-氟 - 苯基）-1-羟基丁基] -3-（羟甲基） - 苄腈以（+） - - 在包含1-丙醇，乙醇或乙腈的溶剂体系中的O，O-二对甲苯酰 - 酒石酸的（S，S） - 或（ - ） - （R，R） - 对映异构体。

9. 发明申请

WO2006002690A1 PROCESS FOR SYNTHESIS OF 4-4'-DIAMINO-DIPHENYL-SULFONE 审中-公开
标题翻译：合成4-4'-二氨基 - 二苯基硫醚的方法
公开(公告)号：WO2006002690A1
公开(公告)日：2006-01-12
申请号：PCT/EP2004/051389
申请日：2004-07-07
申请人： LUNDBECK PHARMACEUTICALS ITALY S.P.A. , VILLA, Marco , DE FAVERI, Carla , ZANOTTI, Riccardo , CIARDELLA, Francesco , BORIN, Fabrizio
发明人： VILLA, Marco , DE FAVERI, Carla , ZANOTTI, Riccardo , CIARDELLA, Francesco , BORIN, Fabrizio
IPC分类号： C07C315/02
CPC分类号： C07C315/04 , C07C315/02 , C07C317/34
摘要： A new process for the preparation and purification of 4-4'-diamino-diphenyl-sulfone (dapsone) is described. The process described is a three step process comprising a condensation reaction with the synthesis of a thioeter intermediate and then steps of oxidation and reduction in suitable conditions in order to obtain a product with good yield and purity.
摘要翻译：描述了制备和纯化4-4'-二氨基 - 二苯基砜（氨苯砜）的新方法。所述方法是三步法，其包括与合成硫代特异中间体的缩合反应，然后在合适的条件下进行氧化和还原的步骤，以获得具有良好产率和纯度的产物。

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