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1. 发明申请

US20060189594A1 Procedure for preparing a pharmaceutically active compound 有权
标题翻译：制备药物活性化合物的方法
公开(公告)号：US20060189594A1
公开(公告)日：2006-08-24
申请号：US10566413
申请日：2004-07-27
申请人： Salvador Puig , Reyes Herbera Espinal , Pere Dalmases Barjoan
发明人： Salvador Puig , Reyes Herbera Espinal , Pere Dalmases Barjoan
IPC分类号： A61K31/554 , C07D417/04
CPC分类号： C07D281/18 , Y02P20/55
摘要： The invention relates to a procedure for preparing quetiapine by reaction between a compound of formula (II) and a compound of formula (III), in which X means a leaving group and P a protective group of alcohols resistant to alkaline conditions, in the presence of a base, followed by a step of deprotection and, optionally, obtaining a pharmaceutically acceptable salt thereof. Said procedure permits the obtaining of quetiapine with a high degree of purity under soft temperature conditions, with short reaction times and avoiding the use of toxic solvents. (Graphic)
摘要翻译：本发明涉及通过式（II）化合物与式（III）化合物之间的反应制备喹硫平的方法，其中X表示离去基团，P表示对碱性条件有抗性的醇类保护基，的碱，随后是去保护步骤，和任选地获得其药学上可接受的盐。所述方法允许在软温条件下获得高纯度的喹硫平，反应时间短，避免使用有毒溶剂。（图）

2. 发明申请

US20100204264A1 POLYMORPHIC FORM OF GRANISETRON BASE, METHODS FOR OBTAINING IT AND FORMULATION CONTAINING IT 有权
标题翻译：遗传基础的多晶形式，其获取方法和包含其的配方
公开(公告)号：US20100204264A1
公开(公告)日：2010-08-12
申请号：US12664153
申请日：2007-12-20
申请人： Pere Dalmases Barjoan , Reyes Herbera Espinal , Angel Maria Alvarez Larena
发明人： Pere Dalmases Barjoan , Reyes Herbera Espinal , Angel Maria Alvarez Larena
IPC分类号： A61K31/439 , C07D451/14 , A61P1/08
CPC分类号： C07D451/14
摘要： Relates to a new polymorphic form of Granisetron base, Form I, to methods for obtaining thereof, to the method for obtaining Granisetron.HCl and its use for preparing pharmaceutical formulations. The Form I is characterized by the X-ray powder diffractogram shown in FIG. 1. Included in summarised form are the methods and solvents for obtaining the Form I: 1) Evaporation of hexane at atmospheric pressure; 2) Evaporation of acetone at atmospheric pressure; 3) Evaporation of toluene at atmospheric pressure; 4) Cooling of a saturated solution of diethyl ether to reflux temperature; 5) Evaporation of 2-propanol atmospheric pressure; 6) Evaporation of tetrahydrofuran at atmospheric pressure; and 7) Cooling of a saturated solution of acetonitrile to reflux temperature.
摘要翻译：关于Granisetron碱，形式I的新型多晶型物，其获得方法，获得格拉司琼HCl的方法及其在制备药物制剂中的用途。形式I的特征在于图1所示的X射线粉末衍射图。 1.总结形式是获得形式I的方法和溶剂：1）在大气压下蒸发己烷; 2）在大气压下蒸发丙酮; 3）在大气压下蒸发甲苯; 4）将乙醚饱和溶液冷却至回流温度; 5）蒸发2-丙醇大气压; 6）在大气压下蒸发四氢呋喃; 和7）将乙腈饱和溶液冷却至回流温度。

3. 发明授权

US08129522B2 Method for preparing a mixed solvate of olanzapine 有权
标题翻译：制备奥氮平混合溶剂化物的方法
公开(公告)号：US08129522B2
公开(公告)日：2012-03-06
申请号：US12160004
申请日：2006-12-20
申请人： Pere Dalmases Barjoan , Reyes Herbera Espinal
发明人： Pere Dalmases Barjoan , Reyes Herbera Espinal
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： An improved method is provided for preparing a mixed solvate of olanzapine/water/tetrahydrofuran in a proportion of 1:1:1/2. Said improvement is characterised in that said mixed solvate is basically prepared by means of methylation of the N-desmethylolanzapine with dimethyl sulphate, using tetrahydrofuran and water as solvents.
摘要翻译：提供了一种改进的方法，以1：1：1/2的比例制备奥氮平/水/四氢呋喃的混合溶剂合物。所述改进的特征在于，所述混合溶剂合物基本上通过使用四氢呋喃和水作为溶剂通过N-二甲基氯氮平与硫酸二甲酯的甲基化来制备。

4. 发明授权

US08304426B2 Polymorphic form of Granisetron base, methods for obtaining it and formulation containing it 有权
标题翻译：格拉司琼碱的多形态，其获得方法和含有它的制剂
公开(公告)号：US08304426B2
公开(公告)日：2012-11-06
申请号：US12664153
申请日：2007-12-20
申请人： Pere Dalmases Barjoan , Reyes Herbera Espinal , Angel Maria Alvarez Larena
发明人： Pere Dalmases Barjoan , Reyes Herbera Espinal , Angel Maria Alvarez Larena
IPC分类号： A61K31/439 , C07D451/14 , A61P1/08
CPC分类号： C07D451/14
摘要： Relates to a new polymorphic form of Granisetron base, Form I, to methods for obtaining thereof, to the method for obtaining Granisetron.HCl and its use for preparing pharmaceutical formulations. The Form I is characterized by the X-ray powder diffractogram shown in FIG. 1. Included in summarised form are the methods and solvents for obtaining the Form I: 1) Evaporation of hexane at atmospheric pressure; 2) Evaporation of acetone at atmospheric pressure; 3) Evaporation of toluene at atmospheric pressure; 4) Cooling of a saturated solution of diethyl ether to reflux temperature; 5) Evaporation of 2-propanol atmospheric pressure; 6) Evaporation of tetrahydrofuran at atmospheric pressure; and 7) Cooling of a saturated solution of acetonitrile to reflux temperature.
摘要翻译：关于Granisetron碱，形式I的新型多晶型物，其获得方法，获得格拉司琼HCl的方法及其在制备药物制剂中的用途。形式I的特征在于图1所示的X射线粉末衍射图。 1.总结形式是获得形式I的方法和溶剂：1）在大气压下蒸发己烷; 2）在大气压下蒸发丙酮; 3）在大气压下蒸发甲苯; 4）将乙醚饱和溶液冷却至回流温度; 5）蒸发2-丙醇大气压; 6）在大气压下蒸发四氢呋喃; 和7）将乙腈饱和溶液冷却至回流温度。

5. 发明授权

US07807827B2 Procedure for preparing 11-(4-[2-(2-hydroxyethoxy)ethyl]-1-piperazineyl)-dibenzo[b,f] [1,4]thiazepine 有权
标题翻译：制备11-（4- [2-（2-羟基乙氧基）乙基] -1-哌嗪基） - 二苯并[b，f] [1,4]
公开(公告)号：US07807827B2
公开(公告)日：2010-10-05
申请号：US10566413
申请日：2004-07-27
申请人： Salvador Puig Torres , Reyes Herbera Espinal , Pere Dalmases Barjoan
发明人： Salvador Puig Torres , Reyes Herbera Espinal , Pere Dalmases Barjoan
IPC分类号： C07D281/16
CPC分类号： C07D281/18 , Y02P20/55
摘要： The invention relates to a procedure for preparing quetiapine by reaction between a compound of formula (II) and a compound of formula (III), in which X means a leaving group and P a protective group of alcohols resistant to alkaline conditions, in the presence of a base, followed by a step of deprotection and, optionally, obtaining a pharmaceutically acceptable salt thereof.Said procedure permits the obtaining of quetiapine with a high degree of purity under soft temperature conditions, with short reaction times and avoiding the use of toxic solvents.(Graphic)
摘要翻译：本发明涉及通过式（II）化合物与式（III）化合物之间的反应制备喹硫平的方法，其中X表示离去基团，P表示对碱性条件有抗性的醇类保护基，的碱，随后是去保护步骤，和任选地获得其药学上可接受的盐。所述方法允许在软温条件下获得高纯度的喹硫平，反应时间短，避免使用有毒溶剂。（图）

6. 发明申请

US20090318683A1 METHOD FOR PREPARING A MIXED SOLVATE OF OLANZAPINE 有权
标题翻译：制备OLANZAPINE混合溶剂的方法
公开(公告)号：US20090318683A1
公开(公告)日：2009-12-24
申请号：US12160004
申请日：2006-12-20
申请人： Pere Dalmases Barjoan , Reyes Herbera Espinal
发明人： Pere Dalmases Barjoan , Reyes Herbera Espinal
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： An improved method is provided for preparing a mixed solvate of olanzapine/water/tetrahydrofuran in a proportion of 1:1:1/2. Said improvement is characterised in that said mixed solvate is basically prepared by means of methylation of the N-desmethylolanzapine with dimethyl sulphate, using tetrahydrofuran and water as solvents.
摘要翻译：提供了一种改进的方法，以1：1：1/2的比例制备奥氮平/水/四氢呋喃的混合溶剂合物。所述改进的特征在于，所述混合溶剂合物基本上通过使用四氢呋喃和水作为溶剂通过N-二甲基氯氮平与硫酸二甲酯的甲基化来制备。

7. 发明申请

US20130045998A1 PROCESS FOR PREPARING RUFINAMIDE INTERMEDIATE 有权
标题翻译：制备联苯胺中间体的方法
公开(公告)号：US20130045998A1
公开(公告)日：2013-02-21
申请号：US13643717
申请日：2011-05-02
申请人： Antonio Abelino De Leon Martin , Jordi Bessa Bellmunt , Juan Huguet Clotet , Lluis Sola Carandell , Gloria Freixas Pascual , Jordi Ceron Bertran , Pere Dalmases Barjoan
发明人： Antonio Abelino De Leon Martin , Jordi Bessa Bellmunt , Juan Huguet Clotet , Lluis Sola Carandell , Gloria Freixas Pascual , Jordi Ceron Bertran , Pere Dalmases Barjoan
IPC分类号： C07D249/04 , A61P25/08 , A61K31/4192
CPC分类号： C07D249/04 , A61K31/4192
摘要： The present invention refers to an improved method for the preparation of compound 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxylic acid substantially free of its 3H-I isomer. The invention also refers to the use of said intermediate for the preparation of Rufinamide and for obtaining a new polymorphic form of Rufinamide, designed as Form R-5. The invention also refers to said new polymorph of Rufinamide, and to the composition containing it and its use as medicament. The new polymorph of Rufinamide shows good stability and appropriate physico-chemical properties for its manipulation on industrial scale. Polymorph Form R-5 will be suitable to use as pharmaceutical for the treatment of convulsions, especially for the treatment of epilepsy.
摘要翻译：本发明涉及一种制备基本上不含其3H-1异构体的化合物1-（2,6-二氟苄基）-1H-1,2,3-三唑-4-羧酸的改进方法。本发明还涉及所述中间体用于制备Rufinamide并用于获得设计为R-5型的新型多聚体形式的Rufinamide。本发明还涉及所述新型Rufinamide多晶型物及其含有的组合物及其作为药物的用途。 Rufinamide的新型多晶型物具有良好的稳定性和适用于工业规模操作的物理化学性质。多晶型R-5适合用作药物治疗惊厥，特别是治疗癫痫。

8. 发明授权

US07071209B2 Process for preparing a pharmaceutically active compound (granisetron) 失效
标题翻译：制备药物活性化合物（格拉司琼）的方法
公开(公告)号：US07071209B2
公开(公告)日：2006-07-04
申请号：US10508493
申请日：2003-03-21
申请人： Salvador Puig Torres , Pere Dalmases Barjoan
发明人： Salvador Puig Torres , Pere Dalmases Barjoan
IPC分类号： C07D421/12
CPC分类号： C07D471/08
摘要： The invention relates to a process for preparing granisetron, or a pharmaceutically acceptable salt thereof, which comprises: a) cyclisation of a compound of formula (I) in an inert solvent and at a temperature between 0–100° C., in the presence of a strong acid, in order to yield the compound of formula (II); b) methylation of the compound of formula (II), with an alkylating agent, in the presence of a base, in an inert solvent and at a temperature between 0° C.–160° C., and with optional formation of a pharmaceutically acceptable salt. The process of the invention yields a granisetron of high purity, preventing impurities due to demethylation, by carrying out the methylation after rather than before cyclisation and with a higher yield.
摘要翻译：本发明涉及一种制备格拉司琼或其药学上可接受的盐的方法，其包括：a）在惰性溶剂中和在0-100℃的温度下，在存在下使式（I）化合物在的强酸，以产生式（II）的化合物; b）式（II）化合物与烷基化剂在碱的存在下，在惰性溶剂中，在0℃至160℃之间的温度下甲基化，并任选地形成药学上可接受的盐本发明的方法产生高纯度的格拉司琼，通过在环化后而不是在环化之前进行甲基化并以较高的产率来防止由于去甲基化引起的杂质。

9. 发明申请

US20050148778A1 Process for preparing a rizatriptan 有权
标题翻译：制备利扎曲坦的方法
公开(公告)号：US20050148778A1
公开(公告)日：2005-07-07
申请号：US10509918
申请日：2003-08-05
申请人： Montserrat Armengol Asparo , Pere Dalmases Barjoan
发明人： Montserrat Armengol Asparo , Pere Dalmases Barjoan
IPC分类号： C07D249/08 , C07D403/06 , C07D405/12 , C07D491/052 , C07D521/00 , C07D43/02
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56
摘要： In particular, rizatriptan or a pharmaceutically acceptable salt thereof, which includes a) Preparation of the diazonium salt of aniline hydrochloride (II); followed by reduction and acidification to give the hydrazine (III); b) reaction in situ of the hydrazine hydrochloride (III) with α-keto-δ-valerolactone, to give the hydrazone (IV); c) Fischer indole reaction of the hydrazone (IV), to give the pyranoindolone (V), optionally followed by a hydrolysis reaction to give (VI); d) Transesterification of (V) or esterification of its hydrolysis product (VI), to give (VII), where R means straight or branched C1-C4 alkyl chain; e) Conversion of the hydroxyl group of (VII) into dimethylamino, to give the indolecarboxylate (VIII), where R has the meaning defined above; f) Saponification of the 2-carboalkoxy group of (VIII) to give indolecarboxylic acid (IX); and g) Decarboxylaton of the indolecarboxylic acid (IX) to give rizatriptan and, eventually, to obtain a pharmaceutically acceptable salt thereof. The invention also relates to synthesis intermediates to obtain rizatriptan.
摘要翻译：特别是利扎曲坦或其药学上可接受的盐，其包括a）苯胺盐酸盐（II）的重氮盐的制备; 然后还原和酸化得到肼（III）; b）将肼盐酸盐（III）与α-酮-δ-戊内酯原位反应，得到腙（IV）; c）腙（IV）的费 - 托吲哚反应，得到吡喃兰多酮（V），任选地随后进行水解反应得到（VI）; d）（V）的酯交换或其水解产物（VI）的酯化，得到（VII），其中R表示直链或支链C 1 -C 4烷基链; e）（Ⅶ）的羟基转化为二甲基氨基，得到吲哚羧酸酯（Ⅷ），其中R具有上述定义; f）（VIII）的2-烷氧羰基的皂化得到吲哚羧酸（IX）; 和g）吲哚羧酸（IX）的脱羧作用，得到利扎曲坦，最后得到其药学上可接受的盐。本发明还涉及获得利扎曲普坦的合成中间体。

10. 发明授权

US08884026B2 Process for preparing rufinamide intermediate 有权
标题翻译： Rufinamide中间体的制备方法
公开(公告)号：US08884026B2
公开(公告)日：2014-11-11
申请号：US13643717
申请日：2011-05-02
申请人： Antonio Abelino De Leon Martin , Jordi Bessa Bellmunt , Juan Huguet Clotet , Lluis Sola Carandell , Gloria Freixas Pascual , Jordi Ceron Bertran , Pere Dalmases Barjoan
发明人： Antonio Abelino De Leon Martin , Jordi Bessa Bellmunt , Juan Huguet Clotet , Lluis Sola Carandell , Gloria Freixas Pascual , Jordi Ceron Bertran , Pere Dalmases Barjoan
IPC分类号： C07D249/04 , A61K31/4192
CPC分类号： C07D249/04 , A61K31/4192
摘要： The present invention refers to an improved method for the preparation of compound 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxylic acid substantially free of its 3H-I isomer. The invention also refers to the use of said intermediate for the preparation of Rufinamide and for obtaining a new polymorphic form of Rufinamide, designed as Form R-5. The invention also refers to said new polymorph of Rufinamide, and to the composition containing it and its use as medicament. The new polymorph of Rufinamide shows good stability and appropriate physico-chemical properties for its manipulation on industrial scale. Polymorph Form R-5 will be suitable to use as pharmaceutical for the treatment of convulsions, especially for the treatment of epilepsy.
摘要翻译：本发明涉及一种制备基本上不含其3H-1异构体的化合物1-（2,6-二氟苄基）-1H-1,2,3-三唑-4-羧酸的改进方法。本发明还涉及所述中间体用于制备Rufinamide并用于获得设计为R-5型的新型多聚体形式的Rufinamide。本发明还涉及所述新型Rufinamide多晶型物及其含有的组合物及其作为药物的用途。 Rufinamide的新型多晶型物具有良好的稳定性和适用于工业规模操作的物理化学性质。多晶型R-5适合用作药物治疗惊厥，特别是治疗癫痫。

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