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1. 发明申请

WO2004094368A2 NEW FORMS OF CABERGOLINE 审中-公开
标题翻译：新形态的碳酸氢钠
公开(公告)号：WO2004094368A2
公开(公告)日：2004-11-04
申请号：PCT/IB2004/002512
申请日：2004-04-20
申请人： FINETECH LABORATORIES, LTD. , GUTMAN, Arie , TISHIN, Boris , VILENSKI, Alex , AGAZADE, Albay , PERTZIKOV, Boris , NISNEVICH, Gennady
发明人： GUTMAN, Arie , TISHIN, Boris , VILENSKI, Alex , AGAZADE, Albay , PERTZIKOV, Boris , NISNEVICH, Gennady
IPC分类号： C07D
CPC分类号： C07D457/06
摘要： The invention provides methods for preparing amorphous physical form of cabergoline, and solvate form A of cabergoline useful in the preparation of the first mentioned physical form. A method for treating a prolactin disorder with medicaments prepared from amorphous physical form of cabergoline and solvate form A of cabergoline is also disclosed.
摘要翻译：本发明提供了制备卡麦角林的无定形物理形式的方法，以及用于制备第一种物理形式的卡麦角林的溶剂化物A. 还公开了用卡麦角林的无定形物理形式和卡麦角林的溶剂合物形式A制备的药物治疗催乳素障碍的方法。

2. 发明申请

WO2003097603A1 PROCESS FOR THE PREPARATION OF HIGHLY PURE TORSEMIDE 审中-公开
标题翻译：制备高纯度托泊霉素的方法
公开(公告)号：WO2003097603A1
公开(公告)日：2003-11-27
申请号：PCT/IL2003/000311
申请日：2003-04-15
申请人： FINETECH LABORATORIES LTD. , GUTMAN, Arie , ETINGER, Marina , GOLDRING, Dmitry , PERTSIKOV, Boris , YUDOVITCH, Lev , TISHIN, Boris , VILENSKY, Alexander , GLOZMAN, Alexander , NISNEVICH, Gennady
发明人： GUTMAN, Arie , ETINGER, Marina , GOLDRING, Dmitry , PERTSIKOV, Boris , YUDOVITCH, Lev , TISHIN, Boris , VILENSKY, Alexander , GLOZMAN, Alexander , NISNEVICH, Gennady
IPC分类号： C07D213/74
CPC分类号： C07D213/74
摘要： The present invention provides a novel process for the preparation of highly pure torsemide [1] by reacting of 4-m-tolylamino-3-pyridinesulfonamide [2] with phenyl isopropylcarbamate in the presence of lithium base (F I, II). The present invention also provides a novel intermediate - torsemide lithium, also in hydrate or solvate form - which is a stable, solid compound, and may be simply isolated from the reaction mixture to give after acidification practically pure torsemide [1] without further purification steps.
摘要翻译：本发明提供了一种通过在锂碱（F I，II）存在下使4-间甲苯基氨基-3-吡啶磺酰胺[2]与异丙基氨基甲酸苯基酯反应制备高纯度托塞米酸的新方法[1]。本发明还提供了也是水合物或溶剂合物形式的新型中间体 - 托塞米特锂，其是稳定的固体化合物，并且可以简单地从反应混合物中分离出来，在酸化后实际上是纯的托塞米[1]，无需进一步的纯化步骤。

3. 发明申请

WO2004016589A2 PROCESS FOR PRODUCTION OF HIGHLY PURE DONEPEZIL HYDROCHLORIDE 审中-公开
标题翻译：生产高纯度盐酸厄替西仑的方法
公开(公告)号：WO2004016589A2
公开(公告)日：2004-02-26
申请号：PCT/IL2003/000665
申请日：2003-08-11
申请人： FINETECH LABORATORIES LTD. , GUTMAN, Arie, L. , NISNEVICH, Gennady , TISHIN, Boris , VILENSKY, Alexander , POTYABIN, Pavel
发明人： TISHIN, Boris , VILENSKY, Alexander , POTYABIN, Pavel
IPC分类号： C07D211/00
CPC分类号： C07D211/32
摘要： The present invention provides a process for the preparation of highly pure Donepezil hydrochloride having a liquid chromatography purity (relative area method) of more than 97%, with a content of each individual impurity not exceeding 0.02 area %, which process comprises forming Donepezil base in solution and treating the Donepezil base solution with HCl without prior isolation of Donepezil base; and optionally re-crystallizing the hydrochloride to give Donepezil hydrochloride of desired liquid chromatography purity. Donepezil base in solution may be obtained by intramolecular cyclization of 2-(3,4-dimethoxybenzyl)-3-(N-benzyl- 4-piperidine)propionic acid or a salt thereof.
摘要翻译：本发明提供一种制备液相色谱纯度（相对面积法）超过97％的高纯度盐酸多奈哌齐的方法，每种单独杂质的含量不超过0.02面积％该方法包括在溶液中形成多奈哌齐碱，并用HCl处理多奈哌齐碱溶液，而不事先分离多奈哌齐碱; 并任选重结晶盐酸盐，得到所需液相色谱纯度的盐酸多奈哌齐。溶液中的多奈哌齐碱可以通过2-（3,4-二甲氧基苄基）-3-（N-苄基-4-哌啶）丙酸或其盐的分子内环化而获得。

4. 发明申请

WO2006053766A1 METHODS FOR PURIFYING TRANS-(-)-Δ9-TETRAHYDROCANNABINOL AND TRANS-(+)-A9-TETRAHYDROCANNABINOL 审中-公开
标题翻译：用于纯化（ - ） - 9-四氢萘啶醇和转移 - （+） - A9-四氢萘啶醇的方法
公开(公告)号：WO2006053766A1
公开(公告)日：2006-05-26
申请号：PCT/EP2005/012378
申请日：2005-11-18
申请人： EURO-CELTIQUE S.A. , GUTMAN, Arie, L. , NISNEVICH, Gennady, A. , RUKHMAN, Igor , TISHIN, Boris , ETINGER, Marina , FEDOTEV, Irina , PERTSIKOV, Boris , KHANOLKAR, Ram
发明人： GUTMAN, Arie, L. , NISNEVICH, Gennady, A. , RUKHMAN, Igor , TISHIN, Boris , ETINGER, Marina , FEDOTEV, Irina , PERTSIKOV, Boris , KHANOLKAR, Ram
IPC分类号： A61K31/353 , C07D311/80 , A61P1/08 , A61P3/00 , A61P29/00
CPC分类号： A61K31/352 , A61K9/4875 , C07D311/80
摘要： Methods for making trans-(-)-Δ 9 -tetrahydrocannabinoI and trans-(+)-Δ 9 -tetrahydrocannabinol are disclosed herein. In one embodiment, a trans-(-)-Δ 9 -tetrahydrocannabinoI composition is prepared by allowing a composition comprising (±)-Δ 9 -tetrahydrocannabinol to separate on a chiral stationary phase to provide a trans-(-)-Δ 9 -tetrahydrocannabinoI composition comprising at least about 99% by weight of trans-(-)-Δ 9 -tetrahydrocannabinol based on the total amount of trans-(-)-Δ 9 -tetrahydrocannabinol and trans-(+)-Δ 9 -tetrahydrocannabinol. The invention also relates to methods for treating or preventing a condition such as pain comprising administering to a patient in need thereof an effective amount of a trans-(-)-Δ 9 -tetrahydrocannabinoI having a purity of at least about 98% based on the total weight of cannabinoids.
摘要翻译：制备反式 - （ - ） - 吗 - 四氢大麻丙醇和反 - （+） - α9-四氢大麻酚的方法在本文中公开。在一个实施方案中，通过使包含（±）-β9-四氢大麻酚的组合物在手性上分离来制备反式 - （ - ） - 吗 - 四氢大麻素组合物得到包含至少约99重量％反式 - （ - ） - 叔 - 四氢大麻酚的反 - （ - ） - 四氢大麻素组合物反式 - （ - ） - 四氢大麻酚和反 - （+） - α9-四氢大麻酚的总量。本发明还涉及用于治疗或预防诸如疼痛的病症的方法，其包括向有需要的患者施用有效量的具有纯度的反式 - （ - ） - 吗啡四氢大麻素I 至少约98％，基于大麻素的总重量。

5. 发明申请

WO2003041647A3 SYNTHESIS AND PURIFICATION OF VALACYCLOVIR 审中-公开
公开(公告)号：WO2003041647A3
公开(公告)日：2003-05-22
申请号：PCT/US2002/036269
申请日：2002-11-13
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC. , ETINGER, Marina, Yu , YUDOVICH, Lev, M. , YUZEFOVICH, Michael , NISNEVICH, Gennady, A. , DOLITZKI, Ben, Zion , PERTSIKOV, Boris , TISHIN, Boris , BLASBERGER, Dina
发明人： ETINGER, Marina, Yu , YUDOVICH, Lev, M. , YUZEFOVICH, Michael , NISNEVICH, Gennady, A. , DOLITZKI, Ben, Zion , PERTSIKOV, Boris , TISHIN, Boris , BLASBERGER, Dina
IPC分类号： C07D473/18
摘要： The present invention relates to protected valacyclovir, N-tert-butoxycarbonyl-L-valine 2-[(2-amino-1,6-dihydro-6-oxo-9H-purin-9-yl)methoxy] ethyl ester, and a method of making it. The present invention further relates to a method of making valacyclovir including the steps of coupling an amine protected valine selected from N-tbutoxycarbonyl valine and N-formyl valine with acyclovir using a coupling agent to form a protected valacyclovir, and deprotecting the protected valacyclovir to form valacyclovir or a pharmaceutically acceptable salt thereof. The present invention further relates to valacyclovir in pure form, a method of making pure valacyclovir, and to compositions containing pure valacyclovir.

6. 发明申请

WO2003022209A3 CRYSTALLINE FORMS OF VALACYCLOVIR HYDROCHLORIDE 审中-公开
公开(公告)号：WO2003022209A3
公开(公告)日：2003-03-20
申请号：PCT/US2002/028517
申请日：2002-09-06
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMCEUTICAL USA, INC. , WIZEL, Shlomit , ARONHIME, Judith , NIDDAM-HILDESHEIM, Valerie , DOLITZKY, Ben-Zion , ETINGER, Marina, Yu , YUZEFOVICH, Michael , NISNEVICH, Gennady, A. , PERTSIKOV, Boris , TISHIN, Boris , BLASBERGER, Dina
发明人： WIZEL, Shlomit , ARONHIME, Judith , NIDDAM-HILDESHEIM, Valerie , DOLITZKY, Ben-Zion , ETINGER, Marina, Yu , YUZEFOVICH, Michael , NISNEVICH, Gennady, A. , PERTSIKOV, Boris , TISHIN, Boris , BLASBERGER, Dina
IPC分类号： C07D473/18
摘要： Provided are novel polymorphs and pseudopolymorphs of valacyclovir hydrochloride and phamaceutical compositions containing these. Also provided are methods for making the novel polymorphs and pseudopolymorphs, which include valacyclovir hydrochloride monohydrate and valacyclovir hydrochloride dihydrate.

7. 发明申请

WO2005085247A1 CRYSTALLINE FORMS OF VALACYCLOVIR HYDROCHLORIDE 审中-公开
标题翻译： VALACYCLOVIR氢氯化物的结晶形式
公开(公告)号：WO2005085247A1
公开(公告)日：2005-09-15
申请号：PCT/US2005/005916
申请日：2005-02-25
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC. , WIZEL, Shlomit , ARONHIME, Judith , NIDDAM-HILDESHEIM, Valerie , DOLITZKY, Ben-Zion , ETINGER, Marina, Yu , YUZEFOVICH, Michael , NISNEVICH, Gennady, A. , PERTSIKOV, Boris , TISHIN, Boris , BLASBERGER, Dina
发明人： WIZEL, Shlomit , ARONHIME, Judith , NIDDAM-HILDESHEIM, Valerie , DOLITZKY, Ben-Zion , ETINGER, Marina, Yu , YUZEFOVICH, Michael , NISNEVICH, Gennady, A. , PERTSIKOV, Boris , TISHIN, Boris , BLASBERGER, Dina
IPC分类号： C07D473/18
CPC分类号： A61K31/522 , C07D473/00 , C07D473/18
摘要： Provided are novel polymorphs and pseudopolymorphs of valacyclovir hydrochloride and pharmaceutical compositions containing these. Also provided are methods for making the novel polymorphs and pseudopolymorphs, which include valacyclovir hydrochloride monohydrate and valacyclovir hydrochloride dihydrate.
摘要翻译：提供了盐酸伐昔洛韦的新型多晶型物和假多晶型物，以及含有它们的药物组合物。还提供了制备新型多晶型物和假多晶型物的方法，其包括盐酸伐昔洛韦一水合物和盐酸伐昔洛韦二水合物。

8. 发明申请

WO2003041647A2 SYNTHESIS AND PURIFICATION OF VALACYCLOVIR 审中-公开
标题翻译： VALACYCLOVIR的合成和纯化
公开(公告)号：WO2003041647A2
公开(公告)日：2003-05-22
申请号：PCT/US2002/036269
申请日：2002-11-13
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC. , ETINGER, Marina, Yu , YUDOVICH, Lev, M. , YUZEFOVICH, Michael , NISNEVICH, Gennady, A. , DOLITZKI, Ben, Zion , PERTSIKOV, Boris , TISHIN, Boris , BLASBERGER, Dina
发明人： ETINGER, Marina, Yu , YUDOVICH, Lev, M. , YUZEFOVICH, Michael , NISNEVICH, Gennady, A. , DOLITZKI, Ben, Zion , PERTSIKOV, Boris , TISHIN, Boris , BLASBERGER, Dina
IPC分类号： A61K
CPC分类号： C07D473/00
摘要： The present invention relates to protected valacyclovir, N-tert-butoxycarbonyl-L-valine 2-[(2-amino-1,6-dihydro-6-oxo-9H-purin-9-yl)methoxy] ethyl ester, and a method of making it. The present invention further relates to a method of making valacyclovir including the steps of coupling an amine protected valine selected from N-tbutoxycarbonyl valine and N-formyl valine with acyclovir using a coupling agent to form a protected valacyclovir, and deprotecting the protected valacyclovir to form valacyclovir or a pharmaceutically acceptable salt thereof. The present invention further relates to valacyclovir in pure form, a method of making pure valacyclovir, and to compositions containing pure valacyclovir.
摘要翻译： N-叔丁氧基羰基-L-缬氨酸-2 - [（2-氨基-1,6-二氢-6-氧代-9H-嘌呤-9-基）甲氧基]乙酯（I）是新的。独立权利要求包括以下内容：（1）（I）的制备（P1），其包括在偶联剂存在下将N-叔丁氧羰基缬氨酸与阿昔洛韦偶联; （2）将伐昔洛韦（II）或其盐的制备（P2）涉及（a1）将胺保护的缬氨酸（优选N-叔丁氧基羰基缬氨酸（a）或N-甲酰缬氨酸（b），特别是（a））与阿昔洛韦（c）在偶联剂存在下形成受保护的伐昔洛韦，和（a2）使受保护的伐昔洛韦脱保护; （3）包括进行步骤（a1）的盐酸伐昔洛韦（III）的制备（P3），和用盐酸脱保护的伐昔洛韦; 方法A：在低级烷基醇（优选乙醇）中形成（III）的浆液，回流浆料，并从浆料中分离出（III）;（4）制备（III）或方法B：在水中形成（III）的溶液，将溶液与异丙醇混合以形成浆料，并从浆料中分离（III）。

9. 发明申请

WO2002085902A1 PROCESS AND INTERMEDIATES FOR PRODUCTION OF CABERGOLINE AND RELATED COMPOUNDS 审中-公开
标题翻译：生产咖啡因及相关化合物的方法和中间体
公开(公告)号：WO2002085902A1
公开(公告)日：2002-10-31
申请号：PCT/IL2001/000344
申请日：2001-04-16
申请人： FINETECH LTD. , GUTMAN, Arie, L. , NISNEVICH, Gennadiy , RUKHMAN, Igor , TISHIN, Boris , VILENSKY, Alex , PERTSIKOV, Boris
发明人： GUTMAN, Arie, L. , NISNEVICH, Gennadiy , RUKHMAN, Igor , TISHIN, Boris , VILENSKY, Alex , PERTSIKOV, Boris
IPC分类号： C07D457/06
CPC分类号： C07D457/06
摘要： A process for preparation of N -(ergoline-8β-carbonyl)ureas of the formula [I] their stereoisomers as well as acid addition salts thereof which process comprises silylating an ergoline -8β-carboxamide of the formula [2], their stereoisomers as well as metal or ammonium salts or acid addition salts thereof and reacting the resultant product with an isocyanates R 1 N=C=O [5] wherein R 1 is selected from alkyl having from 1 to 4 carbon atoms, cyclohexyl, phenyl, and dimethylamino alkyl group -(CH 2 ) n NMe 2 in which n is an integer, R 2 is selected from hydrogen, alkyl having from 1 to 4 carbon atoms, cyclohexyl, phenyl, dimethylamino alkyl group -(CH 2 ) n NMe 2 in which n is an integer, pyridyl, pyrimidyl, pyrazinyl, pyridazinyl, thiazolyl or thiadiazolyl , R 3 represents a hydrocarbon group having from 1 to 4 carbon atoms, and R 4 is selected from hydrogen, halogen, methylthio and phenylthio group; followed by desilylation. This novel approach provides an efficient method for preparation of N -(ergoline-8β-carbonyl)ureas of the formula [I] which can be useful as anty-Parkinson drugs and prolactin inhibitors. One of the most potent antiprolactinic agent of the class of compounds prepared according to the present invention is Cabergoline. Silylated ergolines, which are obtained as intermediates in the process of the present invention, are novel compounds and represent a further aspect of the invention.
摘要翻译：制备式[I]的N-（麦角灵-8β-羰基）脲的方法及其酸加成盐，其方法包括使麦角灵-8β-甲酰胺甲硅烷基化式[2]，其立体异构体以及金属或铵盐或其酸加成盐，并使所得产物与异氰酸酯R 1 = C = O [5]反应，其中R 1选自具有 1至4个碳原子，环己基，苯基和二甲基氨基烷基 - （CH 2）n NMe 2，其中n是整数，R 2选自氢，具有1至4个碳原子的烷基，环己基，苯基，二甲基氨基烷基 - （CH 2）n NMe 2，其中n是整数，吡啶基，嘧啶基，吡嗪基，哒嗪基，噻唑基或噻二唑基，R 3表示具有1至4个碳原子的烃基，R 4选自氢，卤素，甲硫基和苯硫基; 然后脱甲硅烷基化。这种新方法提供了一种制备式[I]的N - （麦角灵-8β-羰基）脲的有效方法，其可用作非帕特森帕金森药物和催乳素抑制剂。根据本发明制备的化合物类别中最有效的促乳素剂之一是卡麦角林。在本发明的方法中作为中间体获得的甲硅烷基化的麦角糖是新的化合物，代表本发明的另一方面。

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