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1. 发明申请

WO2003048135A1 AMORPHOUS AND CRYSTALLINE FORMS OF LOSARTAN POTASSIUM AND PROCESS FOR THEIR PREPARATION 审中-公开
标题翻译：洛沙坦钾的非晶态和晶体形态及其制备方法
公开(公告)号：WO2003048135A1
公开(公告)日：2003-06-12
申请号：PCT/US2002/036550
申请日：2002-11-13
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC. , DOLITZKY, Ben, Zion , WEIZEL, Shlomit , NISNEVICH, Gennady , RUKHMAN, Igor , KAFTANOV, Julia
发明人： DOLITZKY, Ben, Zion , WEIZEL, Shlomit , NISNEVICH, Gennady , RUKHMAN, Igor , KAFTANOV, Julia
IPC分类号： C07D257/04
CPC分类号： C07D403/10
摘要： This invention relates to novel amorphous losartan potassium, novel losartan potassium in a crystalline form that is a hydrate, novel crystalline losartan potassium Form IV and solvates thereof, novel crystalline losartan potassium Form V and solvates thereof, to processes for their preparation, to compositions containing them and to their use in medicine. This invention further relates to a novel process for preparing crystalline losartan potassium Form I and Form II.
摘要翻译：本发明涉及新型无定形洛沙坦钾，结晶形式的新型氯沙坦钾，其为水合物，新型结晶氯沙坦钾形式IV及其溶剂合物，新型结晶氯沙坦钾V型及其溶剂化物，其制备方法，含有他们和他们在医学中的使用。本发明还涉及一种制备结晶氯沙坦钾I型和II型的新方法。

2. 发明申请

WO2004007482A2 NOVEL SYNTHESIS OF IRBESARTAN 审中-公开
标题翻译：新型的IRBESARTAN合成
公开(公告)号：WO2004007482A2
公开(公告)日：2004-01-22
申请号：PCT/US2003/022479
申请日：2003-07-16
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC , NISNEVICH, Gennady , RUKHMAN, Igor , PERTSIKOV, Boris , KAFTANOV, Julia , DOLITZKY, Ben-Zion , SHAPIRO, Eugeny , YAHALOMI, Bonit
发明人： NISNEVICH, Gennady , RUKHMAN, Igor , PERTSIKOV, Boris , KAFTANOV, Julia , DOLITZKY, Ben-Zion , SHAPIRO, Eugeny , YAHALOMI, Bonit
IPC分类号： C07D403/00
CPC分类号： C07D403/10
摘要： Provided is a novel synthesis of irbesartan employing a phase transfer catalyst. Also provided is irbesartan having a fine particle size.
摘要翻译：提供了采用相转移催化剂的厄贝沙坦的新合成。还提供了具有精细颗粒大小的厄贝沙坦。

3. 发明申请

WO2004065383A3 NOVEL SYNTHESIS OF IRBESARTAN 审中-公开
公开(公告)号：WO2004065383A3
公开(公告)日：2004-08-05
申请号：PCT/US2004/001135
申请日：2004-01-16
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC. , NISNEVICH, Gennady , RUKHMAN, Igor , PERTSIKOV, Boris , KAFTANOV, Julia , DOLITZKY, Ben-Zion
发明人： NISNEVICH, Gennady , RUKHMAN, Igor , PERTSIKOV, Boris , KAFTANOV, Julia , DOLITZKY, Ben-Zion
IPC分类号： C07D403/10
摘要： Provided are a method of making irbesartan via a Suzuki coupling reaction and a novel intermediate, 2-butyl-3-(4'-bromobenzyl)-1,3-diazaspiro[4.4]non-1-ene-4-one, for such process. The novel process includes the step of reacting such intermediate with a protected imidazolephenylboronic acid.

4. 发明申请

WO2004072064A1 SYNTHESIS OF 2-BUTYL-3-(2'-(1-TRITYL-1H-TETRAZOL-5-YL)BIPHENYL-4-YL)-1,3-DIAZASPIROL[4,4]-NON-ENE-4-ONE 审中-公开
标题翻译：合成2-丁基-3-（2' - （1-三乙基-1H-四唑-5-基）联苯-4-基）-1,3-DIAZASPIROL [4,4] -NON-ENE-4-
公开(公告)号：WO2004072064A1
公开(公告)日：2004-08-26
申请号：PCT/US2004/003604
申请日：2004-02-05
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC. , NISNEVICH, Gennady , RUKHMAN, Igor , PERTSIKOV, Boris , KAFTANOV, Julia , DOLITZKY, Ben-Zion
发明人： NISNEVICH, Gennady , RUKHMAN, Igor , PERTSIKOV, Boris , KAFTANOV, Julia , DOLITZKY, Ben-Zion
IPC分类号： C07D403/10
CPC分类号： C07D403/10
摘要： Provided is a novel method of making 2-butyl-3-[[2'(1-trityl-1H-tetrazol-5-yl)biphen-4-yl]methyl]1,3-diazaspiro[4,4]non-1-ene-4-one, which can be converted to irbesartan. Also provided are methods of making irbesartan.
摘要翻译：提供了制备2-丁基-3 - [[2'（1-三苯甲基-1H-四唑-5-基）联苯-4-基]甲基] -1,3-二氮杂螺[4,4] 1-烯-4-酮，可以转化成厄贝沙坦。还提供了制备厄贝沙坦的方法。

5. 发明公开

EP1620100A2 NEW FORMS OF CABERGOLINE 审中-公开
标题翻译：卡麦角林的新形式
公开(公告)号：EP1620100A2
公开(公告)日：2006-02-01
申请号：EP04744162.1
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： A61K31/48 , C07D457/06
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.

6. 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。

7. 发明申请

WO2003040120A1 PROCESS FOR THE PREPARATION OF DRONEDARONE 审中-公开
标题翻译：制备红霉素的方法
公开(公告)号：WO2003040120A1
公开(公告)日：2003-05-15
申请号：PCT/IL2002/000881
申请日：2002-11-06
申请人： ISP INVESTMENTS INC. , GUTMAN, Arie, L. , NISNEVICH, Gennady , YUDOVITCH, Lev
发明人： GUTMAN, Arie, L. , NISNEVICH, Gennady , YUDOVITCH, Lev
IPC分类号： C07D307/80
CPC分类号： C07D307/79 , C07D307/80
摘要： The present invention provides, according to an aspect thereof, a novel process for the preparation of dronedarone [1] and pharmaceutically acceptable salts thereof. According to a preferred embodiment, the process comprises N-acetylating of p-anisidine or p-phenetidine with acetic anhydride, reacting of the obtained N-(4-alkoxyphenyl)acetamide with 2-bromohexanoyl chloride or bromide in the presence of aluminum chloride or bromide to obtain N-[3-(2-bromohexanoyl)-4-hydroxyphenyl]acetamide [6a], converting the compound [6a] into 2-butyl-5-benzofuranamine hydrochloride [12a] and subsequently converting [12a] into [1] or pharmaceutically acceptable salts thereof. In accordance with another aspect of this invention, there are provided novel intermediates, inter alia the novel compounds [6a] and [12a]. The novel intermediates of the present invention are stable, solid compounds, obtainable in high yields, which can be easily purified by crystallization and stored for long periods of time.
摘要翻译：根据本发明的一个方面，本发明提供了制备决奈达隆[1]及其药学上可接受的盐的新方法。根据优选的实施方案，该方法包括对乙氧基苯胺或对苯乙胺与乙酸酐的N-乙酰化反应，所得的N-（4-烷氧基苯基）乙酰胺与氯化2-氯己酰氯在溴化铝存在下反应得到N- [3-（2-溴己酰基）-4-羟基苯基]乙酰胺[6a]，将化合物[6a]转化为2-丁基-5-苯并呋喃胺盐酸盐[12a]，随后将[12a]转化为[1 ]或其药学上可接受的盐。根据本发明的另一方面，提供了新的中间体，特别是新化合物[6a]和[12a]。本发明的新型中间体是稳定的固体化合物，其可以高产率获得，其可以通过结晶容易地纯化并长时间储存。

8. 发明申请

WO2002096868A2 A NEW PROCESS FOR THE PREPARATION OF 17-PHENYL- 18,19,20- TRINOR-PGF2A AND ITS DERIVATIVES 审中-公开
标题翻译：制备17-苯基-18,19,20-三氢生物-PGF2A及其衍生物的新方法
公开(公告)号：WO2002096868A2
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
CPC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.
摘要翻译：本发明提供了一种新的有效的合成17-苯基-18,19,20-三硝基-PGF2α及其衍生物的方法，包括抗青光眼药物比马前列素和拉坦前列素。本发明的优点尤其在于通过结晶从参与合成上述化合物的主要中间体也可以从含有不想要的异构体的混合物中分离出来。此外，不需要的异构体可被氧化，得到起始化合物，然后再循环。

9. 发明申请

WO2002046153A3 PROCESS FOR THE PREPARATION OF ZAFIRLUKAST 审中-公开
公开(公告)号：WO2002046153A3
公开(公告)日：2002-06-13
申请号：PCT/IB2001/002268
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
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 its 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.

10. 发明申请

WO2011154953A1 PROCESS FOR THE PREPARATION OF IODIDES 审中-公开
标题翻译：制备碘化物的方法
公开(公告)号：WO2011154953A1
公开(公告)日：2011-12-15
申请号：PCT/IL2011/000458
申请日：2011-06-09
申请人： TECHNION R&D FOUNDATION LTD. , NISNEVICH, Gennady , GANDELMAN, Mark , KULBITSKI, Kseniya
发明人： NISNEVICH, Gennady , GANDELMAN, Mark , KULBITSKI, Kseniya
IPC分类号： C07C67/32 , C07C17/093 , C07C41/22 , C07J9/00 , C07C22/04 , C07C22/00 , C07C23/46 , C07C19/07 , C07C19/075 , C07D205/04 , C07D211/38 , C07C25/02 , C07C25/22 , C07C25/18 , C07C69/74
CPC分类号： C07C17/093 , C07C41/22 , C07C67/32 , C07C201/12 , C07C269/06 , C07C2601/02 , C07C2601/04 , C07C2603/62 , C07C2603/90 , C07D205/04 , C07D211/38 , C07J9/00 , C07J9/005 , C07C19/075 , C07C22/04 , C07C25/22 , C07C25/18 , C07C22/00 , C07C19/07 , C07C25/02 , C07C23/46 , C07C43/225 , C07C69/753 , C07C69/74 , C07C69/76 , C07C205/11 , C07C271/22
摘要： This invention is directed to a process for the preparation of high yield alkyl or aryl iodide from its corresponding carboxylic acid using N-iodo amides.
摘要翻译：本发明涉及使用N-碘酰胺从其相应的羧酸制备高产率烷基或芳基碘的方法。

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