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1. 发明授权

US08927771B2 Pharmaceutically acceptable cocrystals of N-[2-(7-methoxyl-1-naphtyl)ethyl]acetamide and methods of their preparation 有权
标题翻译： N- [2-（7-甲氧基-1-萘基）乙基]乙酰胺的药学上可接受的共晶体及其制备方法
公开(公告)号：US08927771B2
公开(公告)日：2015-01-06
申请号：US14114211
申请日：2012-04-25
申请人： Gary James Miller , Ludek Ridvan , Jindrich Richter , Ondrej Dammer , Tomas Chvojka , Tomas Pekarek , Winfried Heyse , Norbert Nagel
发明人： Gary James Miller , Ludek Ridvan , Jindrich Richter , Ondrej Dammer , Tomas Chvojka , Tomas Pekarek , Winfried Heyse , Norbert Nagel
IPC分类号： C07C233/25 , C07C309/20 , C07C231/22 , C07C309/29 , C07C233/18 , C07C57/145 , C07C59/265
CPC分类号： C07C233/25 , C07B2200/13 , C07C57/145 , C07C59/265 , C07C231/22 , C07C233/18 , C07C309/29
摘要： The present invention relates to novel solid forms of agomelatine (I), specifically novel phaamaceutically acceptable cocrystals thereof, as well as to methods of preparing them. Three pharmaceutically acceptable cocrystals of (I) that have physico-chemical properties acceptable for pharmaceutical development were obtained.
摘要翻译：本发明涉及agomelatine（I）的新型固体形式，特别是新颖的药物可接受的共晶体，以及其制备方法。获得具有药物开发可接受的物理化学性质的（I）的三种药学上可接受的共晶体。

2. 发明申请

US20140051887A1 PHARMACEUTICALLY ACCEPTABLE COCRYSTALS OF N-[2-(7-METHOXYL-1-NAPHTYL)ETHYL]ACETAMIDE AND METHODS OF THEIR PREPARATION 有权
标题翻译： N- [2-（7-甲氧基-1-萘基）乙基]乙酰胺的药学上可接受的结晶及其制备方法
公开(公告)号：US20140051887A1
公开(公告)日：2014-02-20
申请号：US14114211
申请日：2012-04-25
申请人： Gary James Miller , Ludek Ridvan , Jindrich Richter , Ondrej Dammer , Tomas Chvojka , Tomas Pekarek , Winfried Heyse , Norbert Nagel
发明人： Gary James Miller , Ludek Ridvan , Jindrich Richter , Ondrej Dammer , Tomas Chvojka , Tomas Pekarek , Winfried Heyse , Norbert Nagel
IPC分类号： C07C233/25 , C07C231/22
CPC分类号： C07C233/25 , C07B2200/13 , C07C57/145 , C07C59/265 , C07C231/22 , C07C233/18 , C07C309/29
摘要： The present invention relates to novel solid forms of agomelatine (I), specifically novel phaamaceutically acceptable cocrystals thereof, as well as to methods of preparing them. Three pharmaceutically acceptable cocrystals of (I) that have physico-chemical properties acceptable for pharmaceutical development were obtained.
摘要翻译：本发明涉及agomelatine（I）的新型固体形式，特别是新颖的药物可接受的共晶体，以及其制备方法。获得具有药物开发可接受的物理化学性质的（I）的三种药学上可接受的共晶体。

3. 发明授权

US08143417B2 Method for the preparation of zolmitriptan 有权
标题翻译：制备佐米曲坦的方法
公开(公告)号：US08143417B2
公开(公告)日：2012-03-27
申请号：US12526958
申请日：2008-02-25
申请人： Michal Voslar , Monika Zatopkova , Ludek Ridvan , Tomas Pekarek
发明人： Michal Voslar , Monika Zatopkova , Ludek Ridvan , Tomas Pekarek
IPC分类号： C07D263/04
CPC分类号： C07D413/06
摘要： In the preparation of zolmitriptan of formula III the reduction of the diazonium salt to (5)-4-(4-hydrazinobenzyl)-1,3-oxazolidin-2-one of formula IV is performed in a more concentrated mixture and by the effect on an alkali metal disulphite, preferably sodium disulphite. A zolmitriptan toluene solvate, characterized by a toluene content of 9 to 14% by weight according to the gas chromatography determination and by a maximum of the corresponding mass loss at temperatures of about 111° C. in the gravimetric analysis record. A zolmitriptan toluene solvate, showing strong Raman bands at the wave numbers of 1443 and 1354 cm−1, characteristic for the crystal lattice of zolmitriptan with built-in toluene, and further marked bands at 1004 and 786 cm−1, characteristic for toluene.
摘要翻译：在式III的佐米曲坦的制备中，将重氮盐还原成式IV的（5）-4-（4-肼基苄基）-1,3-恶唑烷-2-酮，以更浓缩的混合物和效果在碱金属亚硫酸盐上，优选二亚硫酸钠。唑来曲坦甲苯溶剂化物，其特征在于根据气相色谱测定的甲苯含量为9至14重量％，并且在重量分析记录中在约111℃的温度下达到最大的相应质量损失。唑来曲坦甲苯溶剂化物，在1443和1354cm -1的波数显示强拉曼带，具有内置甲苯的佐米曲坦的晶格特征，以及在1004和786cm -1处的进一步标记的带，其特征在于甲苯。

4. 发明授权

US08779005B2 Salts of desvenlafaxine and a method of their preparation 有权
标题翻译：去甲文拉法辛盐及其制备方法
公开(公告)号：US08779005B2
公开(公告)日：2014-07-15
申请号：US13146467
申请日：2010-02-03
申请人： Ludek Ridvan , Petr Hruby , Stanislav Radl , Hana Brusova , Lukas Krejcik , Tomas Pekarek , Natalia Csokova , Anna Zerzanova
发明人： Ludek Ridvan , Petr Hruby , Stanislav Radl , Hana Brusova , Lukas Krejcik , Tomas Pekarek , Natalia Csokova , Anna Zerzanova
IPC分类号： A61K31/205 , C07C215/52
CPC分类号： A61K31/205 , C07B2200/13 , C07C51/412 , C07C55/07 , C07C213/08 , C07C213/10 , C07C215/52 , C07C215/64 , C07C2601/14
摘要： The invention deals with new salts of the desvenlafaxine base of formula (I) with oxalic acid, the new salts being the hydrogen oxalate of formula (II) in the proportion of desvenlafaxine:oxalic acid of 1:1 and hemioxalate of formula (III) in the proportion of desvenlafaxine:oxalic acid of 2:1.
摘要翻译：本发明涉及式（I）的去甲文拉法辛碱与草酸的新盐，新盐是式（II）的草酸氢盐，其中去甲文拉法辛：草酸为1:1，式（III）的次氯酸盐以去甲文拉法辛：草酸为2：1的比例。

5. 发明申请

US20120041227A1 NEW SALTS OF DESVENLAFAXINE AND A METHOD OF THEIR PREPARATION 有权
标题翻译：维生素D的新盐及其制备方法
公开(公告)号：US20120041227A1
公开(公告)日：2012-02-16
申请号：US13146467
申请日：2010-02-03
申请人： Ludek Ridvan , Petr Hruby , Stanislav Radl , Hana Brusova , Lukas Krejcik , Tomas Pekarek , Natalia Csokova , Anna Zerzanova
发明人： Ludek Ridvan , Petr Hruby , Stanislav Radl , Hana Brusova , Lukas Krejcik , Tomas Pekarek , Natalia Csokova , Anna Zerzanova
IPC分类号： C07C229/34
CPC分类号： A61K31/205 , C07B2200/13 , C07C51/412 , C07C55/07 , C07C213/08 , C07C213/10 , C07C215/52 , C07C215/64 , C07C2601/14
摘要： The invention deals with new salts of the desvenlafaxine base of formula (I) with oxalic acid, the new salts being the hydrogen oxalate of formula (II) in the proportion of desvenlafaxine:oxalic acid of 1:1 and hemioxalate of formula (III) in the proportion of desvenlafaxine:oxalic acid of 2:1.
摘要翻译：本发明涉及式（I）的去甲文拉法辛碱与草酸的新盐，新盐是式（II）的草酸氢盐，其中去甲文拉法辛：草酸为1:1，式（III）的次氯酸盐以去甲文拉法辛：草酸为2：1的比例。

6. 发明申请

US20100105919A1 METHOD FOR THE PREPARATION OF ZOLMITRIPTAN 有权
标题翻译：制备ZOLMITRIPTAN的方法
公开(公告)号：US20100105919A1
公开(公告)日：2010-04-29
申请号：US12526958
申请日：2008-02-25
申请人： Michal Voslar , Monika Zatopkova , Ludek Ridvan , Tomas Pekarek
发明人： Michal Voslar , Monika Zatopkova , Ludek Ridvan , Tomas Pekarek
IPC分类号： C07D263/04
CPC分类号： C07D413/06
摘要： In the preparation of zolmitriptan of formula III the reduction of the diazonium salt to (5)-4-(4-hydrazinobenzyl)-1,3-oxazolidin-2-one of formula IV is performed in a more concentrated mixture and by the effect on an alkali metal disulphite, preferably sodium disulphite. A zolmitriptan toluene solvate, characterized by a toluene content of 9 to 14% by weight according to the gas chromatography determination and by a maximum of the corresponding mass loss at temperatures of about 111° C. in the gravimetric analysis record. A zolmitriptan toluene solvate, showing strong Raman bands at the wave numbers of 1443 and 1354 cm−1, characteristic for the crystal lattice of zolmitriptan with built-in toluene, and further marked bands at 1004 and 786 cm−1, characteristic for toluene.
摘要翻译：在式III的佐米曲坦的制备中，将重氮盐还原成式IV的（5）-4-（4-肼基苄基）-1,3-恶唑烷-2-酮，以更浓缩的混合物和效果在碱金属亚硫酸盐上，优选二亚硫酸钠。唑来曲坦甲苯溶剂化物，其特征在于根据气相色谱测定的甲苯含量为9至14重量％，并且在重量分析记录中在约111℃的温度下达到最大的相应质量损失。唑来曲坦甲苯溶剂化物，在1443和1354厘米-1的波数显示强拉曼带，具有内置甲苯的佐米曲坦的晶格特征，以及在1004和786厘米-1处的进一步标记的带，特征在于甲苯。

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