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11. 发明申请

WO2003082857A3 LANSOPRAZOLE POLYMORPHS AND PROCESSES FOR PREPARATION THEREOF 审中-公开
公开(公告)号：WO2003082857A3
公开(公告)日：2003-10-09
申请号：PCT/US2003/009261
申请日：2003-03-27
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC. , FINKELSTEIN, Nina , WIZEL, Shlomit
发明人： FINKELSTEIN, Nina , WIZEL, Shlomit
IPC分类号： C07D401/12
摘要： The present invention relates to three crytalline solid forms of Iansoprazole Formula (I) denominated as forms D, E and F. Processes for preparing these crytalline solid forms of Iansoprazole are disclosed.

12. 发明申请

WO2002062790A1 PREPARATION OF N-METHYLPAROXETINE AND RELATED INTERMEDIATE COMPOUNDS 审中-公开
标题翻译： N-甲基戊二酸和相关中间体化合物的制备
公开(公告)号：WO2002062790A1
公开(公告)日：2002-08-15
申请号：PCT/US2002/003223
申请日：2002-02-04
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC. , FINKELSTEIN, Nina
发明人： FINKELSTEIN, Nina
IPC分类号： C07D405/12
CPC分类号： C07D405/12 , C07D317/64
摘要： The present invention provides a process for preparing N-methylparoxetine, an intermediate in the synthesis of paroxetine, by reacting sesamol-tetrabutylammonium salt with CIPMA. The synthesis of the intermediate in the prior are resulted in a particularly low yield. The use of the sesamol-tetrabutylammonium salt increases the yield by more than three folds over the prior art. The present invention is not limited to the synthesis of N-methylparoxetine, but also includes other similar compounds.
摘要翻译：本发明提供了通过使芝麻酚四丁基铵盐与CIPMA反应制备帕罗西汀合成中间体的N-甲基帕罗西汀的方法。先前的中间体的合成导致特别低的产率。与现有技术相比，使用芝麻酚四丁基铵盐的产量提高了三倍以上。本发明不限于N-甲基帕罗西汀的合成，还包括其它类似的化合物。

13. 发明申请

WO2009002552A1 RACEMIZATION PROCESS OF R-ZOPICLONE 审中-公开
标题翻译： R-ZOPICLONE的研究进展
公开(公告)号：WO2009002552A1
公开(公告)日：2008-12-31
申请号：PCT/US2008/008040
申请日：2008-06-25
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC. , FINKELSTEIN, Nina , MENDELOVICI, Marioara
发明人： FINKELSTEIN, Nina , MENDELOVICI, Marioara
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： In one of the embodiments, the present invention provides a racemization process comprising: removing the organic solvent from a mother liquor comprising R- zopiclone malate, eszopiclone malate and an organic solvent to obtain a mixture of R- zopiclone malate and eszopiclone malate; mixing the mixture with water to obtain a solution; neutralizing R-zopiclone malate and eszopiclone malate in the solution to obtain a precipitate of R-zopiclone and eszopiclone; filtering the precipitate; mixing the precipitate of R-zopiclone and eszopiclone with DBU and an organic inert solvent having a boiling point of at least 8O0C; heating; and cooling to obtain a zopiclone racemate.
摘要翻译：在一个实施方案中，本发明提供外消旋化方法，其包括：从包含R-佐匹克隆苹果酸酯，苹果酸佐佐匹克和有机溶剂的母液中除去有机溶剂，以获得苹果酸佐佐全隆和苹果酸佐佐匹克的混合物; 将混合物与水混合以获得溶液; 在溶液中中和R-佐匹克隆苹果酸盐和右佐剂丙二酸盐，得到R-佐匹克隆和依佐替普的沉淀物; 过滤沉淀物; 将R-佐匹克隆和左旋佐布隆的沉淀物与DBU和沸点至少为80℃的有机惰性溶剂混合; 加热; 并冷却以获得佐匹克隆外消旋物。

14. 发明申请

WO2007059307A2 CRYSTALLINE AND AMORPHOUS FORMS OF TELITHROMYCIN 审中-公开
标题翻译：结晶和非晶形态的紫杉醇
公开(公告)号：WO2007059307A2
公开(公告)日：2007-05-24
申请号：PCT/US2006/044657
申请日：2006-11-15
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC. , FINKELSTEIN, Nina , DOLITZKY, Ben-zion , ARONHIME, Judith , LEVI, Sigalit
发明人： FINKELSTEIN, Nina , DOLITZKY, Ben-zion , ARONHIME, Judith , LEVI, Sigalit
IPC分类号： C07H17/00 , C07H17/08
CPC分类号： C07H17/00 , A61K31/7052 , C07H17/08
摘要： Provided is telithromycin which melts at a range of 175 °C to 185 °C. Also provided are solid states of telithromycin and processes for the preparation thereof.
摘要翻译：提供的是在175℃至185℃的范围内熔化的泰利霉素。还提供了泰利霉素的固态及其制备方法。

15. 发明申请

WO2006034451A2 CRYSTALLINE CLOPIDOGREL HYDROBROMIDE AND PROCESSES FOR PREPARATION THEREOF 审中-公开
标题翻译：结晶氯吡格雷氢溴酸盐及其制备方法
公开(公告)号：WO2006034451A2
公开(公告)日：2006-03-30
申请号：PCT/US2005/034149
申请日：2005-09-21
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC. , FINKELSTEIN, Nina , ARONHIME, Judith , TESSLER, Limor
发明人： FINKELSTEIN, Nina , ARONHIME, Judith , TESSLER, Limor
IPC分类号： C07D495/04 , A61K31/4365 , A61P7/02
CPC分类号： C07D495/04
摘要： Provided are crystalline forms of clopidogrel hydrobromide and processes for their preparation.
摘要翻译：提供氢溴酸氯吡格雷的结晶形式及其制备方法。

16. 发明申请

WO2004011455A1 PREPARATION OF LANSOPRAZOLE AND RELATED COMPOUNDS 审中-公开
标题翻译：兰吡唑及其相关化合物的制备
公开(公告)号：WO2004011455A1
公开(公告)日：2004-02-05
申请号：PCT/US2003/023588
申请日：2003-07-28
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC. , FINKELSTEIN, Nina
发明人： FINKELSTEIN, Nina
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： The present invention provides a process for preparing lansoprazole (LNP) (I) and related compounds having a high yield and a low level of impurities by oxidation of corresponding sulfide (compound having formula (II)) with tert -butyl hydroperoxide (TBHP), catalyzed by a catalyst vanadium oxytrichloride in an organic solvent selected from the group consisting of a C 1 -C 5 alkanol, decane, nonane, toluene and a mixture of the organic solvent and water, preferably in the presence of a base.
摘要翻译：本发明提供了通过用叔丁基过氧化氢（TBHP）氧化相应的硫化物（具有式（II）的化合物）制备兰索拉唑（LNP）（I）和具有高产率和低水平杂质的相关化合物的方法，在选自C1-C5烷醇，癸烷，壬烷，甲苯以及有机溶剂和水的混合物的有机溶剂中，优选在碱的存在下催化催化剂三氯氧化钒。

17. 发明申请

WO2004056804A2 SOLID STATES OF PANTOPRAZOLE SODIUM, PROCESSES FOR PREPARING THEM AND PROCESSES FOR PREPARING KNOWN PANTOPRAZOLE SODIUM HYDRATES 审中-公开
标题翻译：泮托拉唑钠的固体状态，制备它们的方法以及制备已知泮托拉唑钠盐水合物的方法
公开(公告)号：WO2004056804A2
公开(公告)日：2004-07-08
申请号：PCT/US2003/040668
申请日：2003-12-19
申请人： EVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC. , FINKELSTEIN, Nina , WIZEL, Shlomit , KROCHMEL, Barnaba , BRAUDE, Viviana
发明人： FINKELSTEIN, Nina , WIZEL, Shlomit , KROCHMEL, Barnaba , BRAUDE, Viviana
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： Crystalline pantoprazole sodium Forms II, IV, V, VI, VIII, IX, X, XI, XII, XIII, XIV, XV, XVI, XVII, XVIII, XIX and XX; pantoprazole sodium solvates containing water, acetone, butanol, methylethylketone, dimethylcarbonate, propanol and 2-methylpropanol; and amorphous pantoprazole sodium are disclosed.
摘要翻译：结晶泮托拉唑钠晶型II，IV，V，VI，VIII，IX，X，XI，XII，XIII，XIV，XV，XVI，XVII，XVIII，XIX和XX; 包含水，丙酮，丁醇，甲基乙基酮，碳酸二甲酯，丙醇和2-甲基丙醇的泮托拉唑钠溶剂合物; 和无定形泮托拉唑钠。

18. 发明申请

WO2009149344A2 SOLID STATES OF ALISKIREN FREE BASE 审中-公开
标题翻译：阿里斯汀自由基的固体状态
公开(公告)号：WO2009149344A2
公开(公告)日：2009-12-10
申请号：PCT/US2009/046398
申请日：2009-06-05
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICAL USA, INC. , FINKELSTEIN, Nina , MITTELMAN, Ariel
发明人： FINKELSTEIN, Nina , MITTELMAN, Ariel
IPC分类号： C07C231/24 , C07C237/22 , A61P9/12 , A61K31/165
CPC分类号： C07C237/22 , C07C57/15 , C07C231/24
摘要： The present invention describes a solid state of aliskiren free base, and process for the preparation thereof.
摘要翻译：本发明描述了阿利吉仑游离碱的固态及其制备方法。

19. 发明申请

WO2009143423A1 ALISKIREN MONOFUMARATE AND PROCESSES FOR PREPARATION THEREOF 审中-公开
标题翻译： ALISKIREN MONOFUMARATE及其制备方法
公开(公告)号：WO2009143423A1
公开(公告)日：2009-11-26
申请号：PCT/US2009/044975
申请日：2009-05-22
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICAL USA, INC. , FINKELSTEIN, Nina , MITTELMAN, Ariel
发明人： FINKELSTEIN, Nina , MITTELMAN, Ariel
IPC分类号： C07C237/22 , C07C57/15
CPC分类号： C07C237/22 , C07C57/15
摘要： The present invention provides a novel fumarate compound of aliskiren monofiimarate, and process for preparation thereof. The present invention also provides pharmaceutical compositions comprising aliskiren monofumarate, and methods of using aliskiren monofumarate for treating hypertension.
摘要翻译：本发明提供了阿利吉仑单富马酸的富马酸酯化合物及其制备方法。本发明还提供了包含阿利吉仑单富马酸盐的药物组合物，以及使用阿利吉仑单富马酸盐治疗高血压的方法。

20. 发明公开

EP1178805A1 NOVEL SYNTHESIS AND CRYSTALLIZATION OF PIPERAZINE RING-CONTAINING COMPOUNDS 审中-公开
标题翻译：克里斯蒂安·冯·皮纳
公开(公告)号：EP1178805A1
公开(公告)日：2002-02-13
申请号：EP00923457.6
申请日：2000-04-18
申请人： Teva Pharmaceutical Industries Limited , Teva Pharmaceuticals USA, Inc. , Singer, Claude , Liberman, Anita
发明人： SINGER, Claude , LIBERMAN, Anita , FINKELSTEIN, Nina
IPC分类号： A61K31/55 , A61P25/24 , C07D401/04 , C07D487/12
CPC分类号： C07D401/04 , C07D471/14
摘要： The present invention is directed to methods for the preparation of piperazine ring-containing compounds, particularly mirtazapine. According to the present invention, the mirtazapine intermediate 1-(3-carboxypyridyl-2)-4-methyl-2-phenyl-piperazine is made by hydrolyzing 1-(3-cyanopyridyl-2)-4-methyl-2-phenyl-piperazine with a base where the base is present in a ratio of up to about 12 moles of the base per one mole of 1-(3-cyanopyridyl-2)-4-methyl-2-phenyl-piperazine. The mirtazapine intermediate 1-(3-carboxypyridly-2)-4-methyl-2-phenyl-piperazine may be made by hydrolyzing 1-(3-cyanopyridyl-2)-4-methyl-2-phenyl-piperazine with potassium hydroxide at a temperature of at least about 130 °C. The method of the present invention also includes reacting 2-amino-3-hydroxymethyl pyridine with N-methyl-1-phenyl-2, 2'-iminodiethyl chloride to form 1-(3-hydroxymethylpyridyl-2)-4-methyl-2-phenyl piperazine, and adding sulfuric acid to the 1-(3-hydroxymethylpyridyl-2)-phenyl-4-methylpiperazine to form mirtazapine. The present invention also relates to new processes for recrystallization of mirtazapine form crude mirtazapine.
摘要翻译：本发明涉及制备含哌嗪环化合物，特别是米氮平的方法。根据本发明，米氮平中间体1-（3-羧基吡啶-2）-4-甲基-2-苯基 - 哌嗪是通过水解1-（3-氰基吡啶基-2）-4-甲基-2-苯基 - 哌嗪与碱相比，每1摩尔1-（3-氰基吡啶基-2）-4-甲基-2-苯基 - 哌嗪，碱的含量最多为约12摩尔碱。米氮平中间体1-（3-羧基吡啶-2）-4-甲基-2-苯基 - 哌嗪可以通过用氢氧化钾水解1-（3-氰基吡啶基-2）-4-甲基-2-苯基 - 哌嗪来制备温度至少约130℃。本发明的方法还包括使2-氨基-3-羟甲基吡啶与N-甲基-1-苯基-2,2'-亚氨基二乙基氯反应形成1-（3- 羟甲基吡啶-2）-4-甲基-2-苯基哌嗪，并向1-（3-羟甲基吡啶-2） - 苯基-4-甲基哌嗪中加入硫酸以形成米氮平。本发明还涉及来自粗米氮平的米氮平重结晶的新方法。

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