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11. 发明申请

WO2004094368A3 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：WO2004094368A3
公开(公告)日：2005-05-19
申请号：PCT/IB2004002512
申请日：2004-04-20
申请人： FINETECH LAB 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： C07D457/06 , A61K31/48
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。

12. 发明申请

WO2002096868A3 PREPARATION OF 17-PHENYL- 18, 19, 20- TRINOR-PGF2A AND ITS DERIVATIVES 审中-公开
公开(公告)号：WO2002096868A3
公开(公告)日：2002-12-05
申请号：PCT/IL2002/000422
申请日：2002-05-30
申请人： FINETECH LABORATORIES LTD. , GUTMAN, Arie, L. , NISNEVICH, Gennady , ETINGER, Marina , ZALTZMAN, Igor , YUDOVITCH, Lev , PERTSIKOV, Boris
发明人： GUTMAN, Arie, L. , NISNEVICH, Gennady , ETINGER, Marina , ZALTZMAN, Igor , YUDOVITCH, Lev , PERTSIKOV, Boris
IPC分类号： C07C405/00
摘要： The present invention provides a new and effective process for the synthesis of 17-phenyl-18,19,20-trinor-PGF 2α and its derivatives, including the anti-glaucoma drugs Bimatoprost and Latanoprost. The benefit of the present invention rises inter alia from the fact that a major intermediate involved in the synthesis of the above compounds may be isolated from a mixture containing also an undesired isomer, by crystallization. In addition, the undesired isomer may be oxidized to give the starting compound, which is then recycled.

13. 发明申请

WO0246153A2 PROCESS FOR THE PREPARATION OF ZAFIRLUKAST 审中-公开
标题翻译：制备ZAFIRLUKAST的方法
公开(公告)号：WO0246153A2
公开(公告)日：2002-06-13
申请号：PCT/IB0102268
申请日：2001-11-30
申请人： ISP FINETECH LTD , GUTMAN ARIE , NISNEVICH GENNADY , ZALTZMAN IGOR , PONOMAREV VICTOR , SOTRIHIN MAXIM
发明人： GUTMAN ARIE , NISNEVICH GENNADY , ZALTZMAN IGOR , PONOMAREV VICTOR , SOTRIHIN MAXIM
IPC分类号： C07D209/18 , C07D209/24 , C07D209/00
CPC分类号： C07D209/18 , C07D209/24 , Y02P20/582
摘要： The present invention provides a novel process for the preparation of alkyl (1-alkylindol-3-ylmethyl)benzoate derivatives which process comprises the steps of: (a) reacting of an alkyl (halomethyl)benzoate with excess of an indole, said indole being unsubstituted at positions 1-, 2- and 3-, under conditions promoting alkylation at the 3-position of the indole to yield a mixture comprising alkyl (indol-3-ylmethyl)benzoate and unreacted starting indole,(b) treating the mixture obtained in step (a) with base to yield a mixture, comprising the salt of (indol-3-ylmethyl)benzoic acid and the unreacted indole, (c) recovering the unreacted indole from the mixture obtained in step (b), and recycling the indole as starting material to step (a),(d) isolating the salt of (indol-3-ylmethyl)benzoic acid and/or acidifying the salt to form (indol-3-ylmethyl)benzoic acid, (e) reacting the (indol-3-ylmethyl)benzoic acid or it's salt with alkylating agent in the presence of base to form the desired alkyl (1-alkylindol-3-ylmethyl)benzoate. The above process affords also the preparation of the anti-asthmatic leukotriene antagonist zafirlukast. In such case, methyl 3-methoxy-4-(1-methyl-5-nitroindol-3-ylmethyl)benzoate [1a] is formed in step (e) of the process and this compound is subsequently converted into zafirlukast by known methods.
摘要翻译：本发明提供了一种制备烷基（1-烷基吲哚-3-基甲基）苯甲酸酯衍生物的新方法，该方法包括以下步骤：（a）使（卤代甲基）烷基烷基酯与过量的吲哚反应，所述吲哚为在吲哚的3位上促进烷基化的条件下，在位置1-，2-和3-未被取代，得到包含烷基（吲哚-3-基甲基）苯甲酸酯和未反应的起始吲哚的混合物，（b）处理得到的混合物在步骤（a）中与碱反应以产生包含（吲哚-3-基甲基）苯甲酸的盐和未反应的吲哚的混合物，（c）从步骤（b）中获得的混合物中回收未反应的吲哚，并将吲哚作为步骤（a）的起始原料，（d）分离（吲哚-3-基甲基）苯甲酸的盐和/或酸化盐以形成（吲哚-3-基甲基）苯甲酸，（e）使吲哚-3-基甲基）苯甲酸或其与烷基化剂的盐在碱的存在下形成所需的烷基（1-alkylindol -3-基甲基）苯甲酸甲酯。上述方法还提供了抗哮喘白三烯拮抗剂扎非司酮的制备。在这种情况下，在该方法的步骤（e）中形成3-甲氧基-4-（1-甲基-5-硝基吲哚-3-基甲基）苯甲酸甲酯[1a]，该化合物随后通过已知方法转化成扎非司酮。

14. 发明申请

WO0155101A2 A NEW PROCESS FOR THE PREPARATION OF LATANOPROST 审中-公开
标题翻译：一种制备LATANOPROST的新工艺
公开(公告)号：WO0155101A2
公开(公告)日：2001-08-02
申请号：PCT/IL0100076
申请日：2001-01-26
申请人： FINETECH LTD , GUTMAN ARIE , NISNEVICH GENNADIY , ETINGER MARINA , ZALTZMAN IGOR , JUDOVICH LEV , PERTSIKOV BORIS
发明人： GUTMAN ARIE , NISNEVICH GENNADIY , ETINGER MARINA , ZALTZMAN IGOR , JUDOVICH LEV , PERTSIKOV BORIS
IPC分类号： C07D307/935 , A61K31/5575 , A61P43/00 , C07B61/00 , C07C405/00 , C07D309/12 , C07D407/12
CPC分类号： C07C405/00
摘要： Disclosed is a novel process for the preparation of the anti-glaucoma drug Latanoprost, in good yield, in large amounts and with desired purity. Also disclosed are novel intermediates for the above process.
摘要翻译：本发明公开了一种制备抗青光眼药物拉坦前列素的新方法，其产率高，产率高，纯度高。还公开了用于上述方法的新型中间体。

15. 发明专利

IL279168A Process for the preparation of eribulin 未知
公开(公告)号：IL279168A
公开(公告)日：2022-04-01
申请号：IL27916820
申请日：2020-12-02
申请人： FINETECH PHARMACEUTICAL LTD , GUTMAN ARIE , FEDOTEV IRINA , RUKHMAN IGOR , GROSSMAN OLGA , ZALTSMAN IGOR , YUDOVICH LEV
发明人： GUTMAN ARIE , FEDOTEV IRINA , RUKHMAN IGOR , GROSSMAN OLGA , ZALTSMAN IGOR , YUDOVICH LEV
摘要： The present invention relates to a process for the preparation of Eribulin.

16. 发明专利

AU2003249565A8 Process for production of highly pure donepezil hydrochloride 未知
公开(公告)号：AU2003249565A8
公开(公告)日：2004-03-03
申请号：AU2003249565
申请日：2003-08-11
申请人： FINETECH LAB LTD , GUTMAN ARIE L , NISNEVICH GENNADY
发明人： TISHIN BORIS , VILENSKY ALEXANDER , POTYABIN PAVEL
IPC分类号： C07D211/32 , C07D211/00

17. 发明专利

IL264851A Pure heptasulfated disaccharides having improved oral bioavailability 未知
公开(公告)号：IL264851A
公开(公告)日：2021-12-01
申请号：IL26485119
申请日：2019-02-14
申请人： OPKO PHARMACEUTICALS LLC , AHMED TAHIR , GUTMAN ARIE , FEDOTEV IRINA , RUKHMAN IGOR , GROSSMAN OLGA
发明人： AHMED TAHIR , GUTMAN ARIE , FEDOTEV IRINA , RUKHMAN IGOR , GROSSMAN OLGA
IPC分类号： A61K31/7024 , A61P37/08 , C07H11/00
摘要： Hypersulfated disaccharides with utility in asthma or asthma related disorders are disclosed. The heptasulfated disaccharides administered orally have comparable bioavailability to the intravenous administered dosage form.

18. 发明申请

WO2006053766A8 METHODS FOR PURIFYING TRANS-(-)-?9-TETRAHYDROCANNABINOL AND TRANS-(+)-?9-TETRAHYDROCANNABINOL 审中-公开
标题翻译：用于纯化（ - ） - β-四氢萘啶醇和转移 - （+） - β-9-四氢萘啶醇的方法
公开(公告)号：WO2006053766A8
公开(公告)日：2006-12-14
申请号：PCT/EP2005012378
申请日：2005-11-18
申请人： EURO CELTIQUE SA , 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 , A61P1/08 , A61P3/00 , A61P29/00 , C07D311/80
CPC分类号： A61K31/352 , A61K9/4875 , C07D311/80
摘要： Methods for making trans-(-)-? 9 -tetrahydrocannabinoI and trans-(+)-? 9 -tetrahydrocannabinol are disclosed herein. In one embodiment, a trans-(-)-? 9 -tetrahydrocannabinoI composition is prepared by allowing a composition comprising (±)-? 9 -tetrahydrocannabinol to separate on a chiral stationary phase to provide a trans-(-)-? 9 -tetrahydrocannabinoI composition comprising at least about 99% by weight of trans-(-)-? 9 -tetrahydrocannabinol based on the total amount of trans-(-)-? 9 -tetrahydrocannabinol and trans-(+)-? 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-(-)-? 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分离上来制备反式 - （ - ） - 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。

19. 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。

20. 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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