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1. 发明授权

US07897793B2 Process for preparation of 13,14-dihydro-PGF2 alpha derivatives 有权
标题翻译： 13,14-二氢-PGF2α衍生物的制备方法
公开(公告)号：US07897793B2
公开(公告)日：2011-03-01
申请号：US11874218
申请日：2007-10-18
申请人： Jacek Martynow , Julita Szyc , Wieslaw Szelejewski , Osman Achmatowicz , Andrzej Kutner , Krzysztof Wiśniewski , Jerzy Winiarski , Oliwia Zegrocka-Stendel , Piotr Golebiewski
发明人： Jacek Martynow , Julita Szyc , Wieslaw Szelejewski , Osman Achmatowicz , Andrzej Kutner , Krzysztof Wiśniewski , Jerzy Winiarski , Oliwia Zegrocka-Stendel , Piotr Golebiewski
IPC分类号： C07D307/93 , C07D493/00 , C07C69/74
CPC分类号： C07C309/73 , C07B2200/07 , C07C405/00 , C07C405/0016 , C07C405/0033 , C07C2601/08 , C07D303/04 , C07D307/935 , C07D317/12 , C07D317/26 , C07D327/10 , C07D493/08 , C07D493/18 , C07F7/1804
摘要： The invention relates to a process for the preparation of 13,14-dihydro-PGF2α derivatives of R or S configuration at carbon 15, represented by the general formula (I), wherein the identity of the substituents is defined in the description. Compounds of the formula (I) are valuable biologically-active substances or intermediates in the preparation thereof. The invention especially relates to the process for preparation of 13,14-dihydro-15(R)-17-substituted-18,19,20-trinor-PGF2α, i.e., latanoprost.
摘要翻译：本发明涉及一种在通式（I）表示的碳15处制备R 1或R 2构型的13,14-二氢-PGF2α衍生物的方法，其中取代基的同一性在说明书中定义。式（I）的化合物在制备中是有价值的生物活性物质或中间体。本发明特别涉及制备13,14-二氢-15（R）-17-取代-18,19,20-三硝基-PGF2α（即拉坦前列素）的方法。

2. 发明申请

US20090093651A1 PROCESS FOR PREPARATION OF 13,14-DIHYDRO-PGF2 ALPHA DERIVATIVES 审中-公开
标题翻译：制备13,14-二氢-PGF2阿尔法衍生物的方法
公开(公告)号：US20090093651A1
公开(公告)日：2009-04-09
申请号：US11911813
申请日：2006-04-18
申请人： Jacek Martynow , Julita Szyc , Wieslaw Szelejewski , Osman Achmatowicz , Andrzej Kutner , Krzysztof Wisniewski , Jerzy Winiarski , Oliwia Zegrocka-Stendel , Piotr Golebiewski
发明人： Jacek Martynow , Julita Szyc , Wieslaw Szelejewski , Osman Achmatowicz , Andrzej Kutner , Krzysztof Wisniewski , Jerzy Winiarski , Oliwia Zegrocka-Stendel , Piotr Golebiewski
IPC分类号： C07C69/74
CPC分类号： C07C309/73 , C07B2200/07 , C07C405/00 , C07C405/0016 , C07C405/0033 , C07C2601/08 , C07D303/04 , C07D307/935 , C07D317/12 , C07D317/26 , C07D327/10 , C07D493/08 , C07D493/18 , C07F7/1804
摘要： The invention relates to a process for the preparation of 13,14-dihydro-PGF2α derivatives of R or S configuration at carbon 15, represented by the general formula (I), wherein the identity of the substituents is defined in the description. Compounds of the formula (I) are valuable biologically-active substances or intermediates in the preparation thereof. The invention especially relates to the process for preparation of 13,14-dihydro-15(R)-17-substituted-18,19,20-trinor-PGF2α, i.e., latanoprost.
摘要翻译：本发明涉及在通式（I）表示的碳15处制备R 14或S 4构型的13,14-二氢-PGF2α衍生物的方法，其中取代基的同一性在说明书中定义。式（I）的化合物在制备中是有价值的生物活性物质或中间体。本发明特别涉及制备13,14-二氢-15（R）-17-取代-18,19,20-三硝基-PGF2α，即拉坦前列素的方法。

3. 发明申请

US20180244714A1 PROTOESCIGENIN DERIVATIVE, PROCESS OF ITS PREPARATION, USE OF SAID COMPOUND AND PHARMACEUTICAL COMPOSITION COMPRISING THAT COMPOUND 审中-公开
公开(公告)号：US20180244714A1
公开(公告)日：2018-08-30
申请号：US15553301
申请日：2016-02-26
申请人： Katarzyna KOZIAK , Krzysztof BOJAKOWSKI , Magdalena KOWALEWSKA , Dorota MACIEJKO , Oliwia ZEGROCKA-STENDEL , Iwona GRABOWSKA , Grzegorz GRYNKIEWICZ , Mariusz Marek GRUZA , Kamil JATCZAK , Katarzyna FILIP , Piotr CMOCH , Marta LASZCZ , Instytut Farmaceutyczny
发明人： Katarzyna Koziak , Krzysztof Bojakowski , Magdalena Kowalewska , Dorota Maciejko , Oliwia Zegrocka-Stendel , Iwona Grabowska , Grzegorz Grynkiewicz , Mariusz Marek Gruza , Kamil Jatczak , Katarzyna Filip , Piotr Cmoch , Marta Laszcz
IPC分类号： C07J63/00 , A61K31/58
CPC分类号： C07J63/008 , A61K31/58
摘要： Described herein is compound including a protoescigenin derivative having pharmacological properties. Also described are a process of its preparation, and the use of such a compound as a medicament, especially for treating vascular disorders. A pharmaceutical composition comprising such compound is further described.

4. 发明申请

US20110077405A1 PROCESS FOR PREPARATION OF ENANTIOMERICALLY PURE (S)-1-PHENYI-1,2,3,4- TETRAHYDROISOQUINOLINE 审中-公开
标题翻译：制备纯度（S）-1-苯基-1,2,3,4-四氢喹啉的方法
公开(公告)号：US20110077405A1
公开(公告)日：2011-03-31
申请号：US12993874
申请日：2009-05-22
申请人： Oliwia Zegrocka-Stendel , Joanna Zagrodzka , Marta Laszcz
发明人： Oliwia Zegrocka-Stendel , Joanna Zagrodzka , Marta Laszcz
IPC分类号： C07D453/02 , C07D217/02
CPC分类号： C07D217/02
摘要： Process for preparation of (S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline wherein 1-phenyl-1,2,3,4-tetrahydroisoquinoline is reacted with D-(−)-tartaric acid in a solvent system comprising of methanol and water, preferably at 3.3:1 to 1:1 volume ratio, the crystallization mixture is left for crystallization and (S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline is released from obtained crystalline diastereoisomeric salt according to standard procedures. (S)-1-Phenyl-1,2,3,4-tetrahydroisoquinoline is the intermediate in enantiomeric synthesis of solifenacin.
摘要翻译：（S）-1-苯基-1,2,3,4-四氢异喹啉的制备方法，其中1-苯基-1,2,3,4-四氢异喹啉与D - （ - ） - 酒石酸在溶剂体系中反应包括甲醇和水，优选以3.3:1至1:1的体积比，结晶混合物留下结晶，（S）-1-苯基-1,2,3,4-四氢异喹啉从得到的结晶非对映异构体盐按照标准程序。（S）-1-苯基-1,2,3,4-四氢异喹啉是solifenacin对映体合成中的中间体。

5. 发明授权

US08436182B2 Process for preparation of solifenacin and/or the pharmaceutically acceptable salts thereof of high pharmaceutical purity 有权
标题翻译：制备高度药物纯度的索非那新和/或其药学上可接受的盐的方法
公开(公告)号：US08436182B2
公开(公告)日：2013-05-07
申请号：US12993988
申请日：2009-05-22
申请人： Oliwia Zegrocka-Stendel , Joanna Zagrodzka , Marta Laszcz
发明人： Oliwia Zegrocka-Stendel , Joanna Zagrodzka , Marta Laszcz
IPC分类号： C07D217/02
CPC分类号： C07D453/02
摘要： A process for the preparation of solifenacin and/or the pharmaceutically acceptable salts thereof of high pharmaceutical purity is characterized in that 3-(R)-quinuclidinoloxy anion generated in situ from 3-(R)-quinuclidinol in a presence of strong base in polar organic solvent is subject to acylation with (S)-1-phenyl-1,2,3,4-tetrahydroisoquinolinecarbonyl chloride of chemical purity at least 98%, while maintaining constant anion excess in a reaction mixture, and after reaction completion solifenacin base is optionally transformed into solifenacin salt according to standard procedures. (S)-1-Phenyl-1,2,3,4-tetrahydroisoquinolinecarbonyl chloride of chemical purity at least 98% is obtained in a reaction of (S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline and molar excess of phosgene in a presence of tertiary aromatic amine in aromatic hydrocarbon, and isolated in a crystalline form.
摘要翻译：制备索非那嗪和/或其药学上可接受的高度药学上可接受的盐的方法的特征在于3-（R） - 奎宁环氧基阴离子在极性强碱存在下由3-（R） - 奎宁环醇原位产生有机溶剂用化学纯度至少为98％的（S）-1-苯基-1,2,3,4-四氢异喹啉碳酰氯进行酰化，同时在反应混合物中保持恒定的阴离子过量，反应完成后，solifenacin碱为任选地根据标准程序转化为索非那新盐。在（S）-1-苯基-1,2,3,4-四氢异喹啉和摩尔（R）的反应中获得化学纯度至少98％的（S）-1-苯基-1,2,3,4-四氢异喹啉碳酰氯在芳族烃中存在叔芳族胺的过量的光气，并以结晶形式分离。

6. 发明申请

US20110065922A1 Process for Preparation Of Solifenacin and/or the Pharmaceutically Acceptable Salts Thereof of High Pharmaceutical Purity 有权
标题翻译： Solifenacin和/或其高药物纯度的药学上可接受的盐的制备方法
公开(公告)号：US20110065922A1
公开(公告)日：2011-03-17
申请号：US12993988
申请日：2009-05-22
申请人： Oliwia Zegrocka-Stendel , Joanna Zagrodzka , Marta Laszcz
发明人： Oliwia Zegrocka-Stendel , Joanna Zagrodzka , Marta Laszcz
IPC分类号： C07D453/02
CPC分类号： C07D453/02
摘要： A process for the preparation of solifenacin and/or the pharmaceutically acceptable salts thereof of high pharmaceutical purity is characterized in that 3-(R)-quinuclidinoloxy anion generated in situ from 3-(R)-quinuclidinol in a presence of strong base in polar organic solvent is subject to acylation with (S)-1-phenyl-1,2,3,4-tetrahydroisoquinolinecarbonyl chloride of chemical purity at least 98%, while maintaining constant anion excess in a reaction mixture, and after reaction completion solifenacin base is optionally transformed into solifenacin salt according to standard procedures. (S)-1-Phenyl-1,2,3,4-tetrahydroisoquinolinecarbonyl chloride of chemical purity at least 98% is obtained in a reaction of (S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline and molar excess of phosgene in a presence of tertiary aromatic amine in aromatic hydrocarbon, and isolated in a crystalline form.
摘要翻译：制备索非那嗪和/或其药学上可接受的高度药学上可接受的盐的方法的特征在于3-（R） - 奎宁环氧基阴离子在极性强碱存在下由3-（R） - 奎宁环醇原位产生有机溶剂用化学纯度至少为98％的（S）-1-苯基-1,2,3,4-四氢异喹啉碳酰氯进行酰化，同时在反应混合物中保持恒定的阴离子过量，反应完成后，solifenacin碱为任选地根据标准程序转化为索非那新盐。在（S）-1-苯基-1,2,3,4-四氢异喹啉和摩尔（R）的反应中获得化学纯度至少98％的（S）-1-苯基-1,2,3,4-四氢异喹啉碳酰氯在芳族烃中存在叔芳族胺的过量的光气，并以结晶形式分离。

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