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1. 发明申请

WO2012056458A2 INTERMEDIATE COMPOUNDS AND PROCESS FOR THE PREPARATION OF FINGOLIMOD 审中-公开
标题翻译：中间体化合物和制备FINGOLIMOD的方法
公开(公告)号：WO2012056458A2
公开(公告)日：2012-05-03
申请号：PCT/IL2011/000838
申请日：2011-10-27
申请人： MAPI PHARMA LTD. , MAROM, Ehud , MIZHIRITSKII, Michael , RUBNOV, Shai
发明人： MAROM, Ehud , MIZHIRITSKII, Michael , RUBNOV, Shai
IPC分类号： C07C209/34
CPC分类号： C07C213/02 , C07C201/12 , C07C205/02 , C07C205/31 , C07C205/40 , C07C205/45 , C07C231/02 , C07D319/06 , C07F9/4021 , C07F9/4056 , C07F9/5442 , C07F9/5456 , C07C215/28 , C07C205/16
摘要： The present invention relates to processes for the preparation of (2-Amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol hydrochloride (Fingolimod) and pharmaceutically acceptable salts thereof, and intermediates formed in such processes.
摘要翻译：本发明涉及（2-氨基-2- [2-（4-辛基苯基）乙基]丙烷-1,3-二醇盐酸盐（芬戈莫德）及其药学上可接受的盐的制备方法，以及在这些方法中形成的中间体。

2. 发明申请

WO2011099010A1 PREPARATION OF BENZOFURANS AND USE THEREOF AS SYNTHETIC INTERMEDIATES 审中-公开
标题翻译：苯并呋喃的制备及其作为合成中间体的应用
公开(公告)号：WO2011099010A1
公开(公告)日：2011-08-18
申请号：PCT/IL2011/000150
申请日：2011-02-10
申请人： MAPI PHARMA HOLDINGS (CYPRUS) LIMITED , MAROM, Ehud , MIZHIRITSKII, Michael , RUBNOV, Shai
发明人： MAROM, Ehud , MIZHIRITSKII, Michael , RUBNOV, Shai
IPC分类号： A01N43/08
CPC分类号： C07D307/79 , C07C311/48 , C07D307/80
摘要： The present invention provides several synthetic methods for preparing N-(2-butylbenzofuran-5-yl)-N-(methylsulfonyl)methanesulfonamide, a compound of formula (3), an intermediate in the preparation of Dronedarone. The present invention further provides a process for preparing Dronedarone, comprising the steps of converting 2-butyl-5-bis(methanesulfon)-amidobenzofuran of formula (3) to Dronedarone, wherein the 2-butyl-5-bis(methanesulfon)-amidobenzofuran of formula (3) is prepared by the processes of the present invention.
摘要翻译：本发明提供了几种制备N-（2-丁基苯并呋喃-5-基）-N-（甲基磺酰基）甲磺酰胺的合成方法，式（3）化合物是制备决奈达隆的中间体。本发明还提供了一种制备决奈达隆的方法，包括将式（3）的2-丁基-5-双（甲磺酰） - 氨基苯并呋喃转化成决奈达隆的步骤，其中2-丁基-5-双（甲磺酰） - 氨基苯并呋喃通过本发明的方法制备式（3）的化合物。

3. 发明申请

WO2012056458A3 INTERMEDIATE COMPOUNDS AND PROCESS FOR THE PREPARATION OF FINGOLIMOD 审中-公开
标题翻译：中间体化合物和制备FINGOLIMOD的方法
公开(公告)号：WO2012056458A3
公开(公告)日：2013-07-18
申请号：PCT/IL2011000838
申请日：2011-10-27
申请人： MAPI PHARMA LTD , MAROM EHUD , MIZHIRITSKII MICHAEL , RUBNOV SHAI
发明人： MAROM EHUD , MIZHIRITSKII MICHAEL , RUBNOV SHAI
IPC分类号： C07C211/27
CPC分类号： C07C213/02 , C07C201/12 , C07C205/02 , C07C205/31 , C07C205/40 , C07C205/45 , C07C231/02 , C07D319/06 , C07F9/4021 , C07F9/4056 , C07F9/5442 , C07F9/5456 , C07C215/28 , C07C205/16
摘要： The present invention relates to processes for the preparation of (2-Amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol hydrochloride (Fingolimod) and pharmaceutically acceptable salts thereof, and intermediates formed in such processes.
摘要翻译：本发明涉及（2-氨基-2- [2-（4-辛基苯基）乙基]丙烷-1,3-二醇盐酸盐（芬戈莫德）及其药学上可接受的盐的制备方法，以及在这些方法中形成的中间体。

4. 发明申请

WO2013014665A8 INTERMEDIATE COMPOUNDS AND PROCESS FOR THE PREPARATION OF LURASIDONE AND SALTS THEREOF 审中-公开
公开(公告)号：WO2013014665A8
公开(公告)日：2013-01-31
申请号：PCT/IL2012/050208
申请日：2012-06-13
申请人： MAPI PHARMA LTD. , MAROM, Ehud , MIZHIRITSKII, Michael , TCHILIBON, Susanna , RUBNOV, Shai
发明人： MAROM, Ehud , MIZHIRITSKII, Michael , TCHILIBON, Susanna , RUBNOV, Shai
IPC分类号： C07D417/12 , C07D209/44 , C07D209/48 , C07D275/06 , C07D417/14
摘要： The present invention relates to a process for the preparation of Lurasidone or a pharmaceutically acceptable salt thereof, a compound useful for the treatment of schizophrenia and bipolar disorder. The present invention further relates to processes for the preparation of Lurasidone intermediates, and to certain novel intermediates obtained by such processes.

5. 发明申请

WO2011141903A1 POLYMORPHS OF ALOGLIPTIN BENZOATE 审中-公开
标题翻译：苯甲酸甲酯的聚合物
公开(公告)号：WO2011141903A1
公开(公告)日：2011-11-17
申请号：PCT/IL2010/000974
申请日：2010-11-22
申请人： MAPI PHARMA HOLDINGS (CYPRUS) LIMITED , MAROM, Ehud , RUBNOV, Shai
发明人： MAROM, Ehud , RUBNOV, Shai
IPC分类号： A61K31/513 , C07D213/84
CPC分类号： A61K31/513 , C07D401/04
摘要： The present invention provides new amorphous forms of alogliptin benzoate, pharmaceutical compositions comprising same, methods for their preparation and use thereof in treating conditions mediated by DPP-IV, in particular, type 2 diabetes.
摘要翻译：本发明提供了新型无定形形式的苯丙酸阿曲肽，包含其的药物组合物，其制备方法和用于治疗由DPP-IV介导的病症，特别是2型糖尿病。

6. 发明申请

WO2013050996A3 PROCESS AND INTERMEDIATES FOR THE PREPARATION OF SUBSTITUTED 2-ARYLTHIAZOLE CARBOXYLIC ACIDS 审中-公开
标题翻译：制备取代的2-芳基羧基羧酸的方法和中间体
公开(公告)号：WO2013050996A3
公开(公告)日：2015-06-18
申请号：PCT/IL2012050018
申请日：2012-01-23
申请人： MAPI PHARMA LTD , MIZHIRITSKII MICHAEL , MAROM EHUD , RUBNOV SHAI
发明人： MIZHIRITSKII MICHAEL , MAROM EHUD , RUBNOV SHAI
IPC分类号： A01N43/78 , A61K31/425
CPC分类号： C07D275/03 , A61K31/426 , C07D277/56
摘要： The present invention relates to processes and intermediates for the preparation of derivatives of 2-arylthiazole such as Febuxostat and its analogs. Febuxostat which is an inhibitor of xanthine oxidase, is used for the treatment of chronic hyperuricaemia in conditions in which urate deposition has occurred, such as gouty arthritis.
摘要翻译：本发明涉及制备2-芳基噻唑衍生物如异丙酚钠及其类似物的方法和中间体。作为黄嘌呤氧化酶抑制剂的非索非司他钠，用于在发生尿酸盐沉积的病症中治疗慢性高尿酸血症，例如痛风性关节炎。

7. 发明申请

WO2013014665A1 INTERMEDIATE COMPOUNDS AND PROCESS FOR THE PREPARATION OF LURASIDONE AND SALTS THEREOF 审中-公开
标题翻译：中间体化合物及其制备方法及其制备方法
公开(公告)号：WO2013014665A1
公开(公告)日：2013-01-31
申请号：PCT/IL2012050208
申请日：2012-06-13
申请人： MAPI PHARMA LTD , MARON EHUD , MIZHIRITSKII MICHAEL , TCHILIBON SUSANNA , RUBNOV SHAI
发明人： MARON EHUD , MIZHIRITSKII MICHAEL , TCHILIBON SUSANNA , RUBNOV SHAI
IPC分类号： C07D417/12 , C07D209/44 , C07D209/48 , C07D275/06 , C07D417/14
CPC分类号： C07D417/14 , C07C309/04 , C07D209/44 , C07D209/48 , C07D209/72 , C07D275/04 , C07D417/12
摘要： The present invention relates to a process for the preparation of Lurasidone or a pharmaceutically acceptable salt thereof, a compound useful for the treatment of schizophrenia and bipolar disorder. The present invention further relates to processes for the preparation of Lurasidone intermediates, and to certain novel intermediates obtained by such processes.
摘要翻译：本发明涉及一种制备卢拉西酮或其药学上可接受的盐，可用于治疗精神分裂症和双相情感障碍的化合物的方法。本发明还涉及制备紫罗兰酮中间体的方法，以及通过这些方法获得的某些新型中间体。

8. 发明申请

WO2012143924A1 RANDOM PENTAPOLYMER FOR TREATMENT OF AUTOIMMUNE DISEASES 审中-公开
标题翻译：随机PENTAPOLYMER治疗自身免疫性疾病
公开(公告)号：WO2012143924A1
公开(公告)日：2012-10-26
申请号：PCT/IL2012/050138
申请日：2012-04-16
申请人： MAPI PHARMA LTD. , MAROM, Ehud , RUBNOV, Shai
发明人： MAROM, Ehud , RUBNOV, Shai
IPC分类号： A61P25/28
CPC分类号： C08G69/10 , A61K31/785 , A61K38/00 , A61K45/06 , C07K14/001 , A61K2300/00
摘要： The present invention provides a synthetic polypeptide which is a random pentapolymer or a salt thereof, comprising alanine, glutamic acid, lysine, tyrosine and phenylalanine, useful for the treatment of autoimmune diseases and, in particular multiple sclerosis (MS). The pentapolymer is a copolymer of alanine, glutamic acid, lysine, tyrosine and phenylalanine, which are randomly polymerized into a polypeptide, thereby forming a random copolymer, or a salt thereof The present invention is based in part on the unexpected finding that the novel pentapolymer shows unexpected oral bioavailability, an advantageous release profile when formulated into a depot drug delivery system and advantageous synergistic activity in autoimmune diseases when combined with an additional therapeutic agent. According to a first aspect, the present invention provides a pentapolymer or a salt thereof, which is a linear random copolymer of alanine, glutamic acid, lysine, tyrosine and phenylalanine.
摘要翻译：本发明提供了一种合成多肽，其是无机五聚物或其盐，其包含丙氨酸，谷氨酸，赖氨酸，酪氨酸和苯丙氨酸，其可用于治疗自身免疫疾病，特别是多发性硬化（MS）。五元共聚物是丙氨酸，谷氨酸，赖氨酸，酪氨酸和苯丙氨酸的共聚物，其随机聚合成多肽，从而形成无规共聚物或其盐。本发明部分基于意想不到的发现，即新的五元共聚物显示出意想不到的口服生物利用度，当配制成贮库药物递送系统时的有利的释放特征，以及当与另外的治疗剂组合时，在自身免疫性疾病中的有利的协同活性。根据第一方面，本发明提供了一种五聚物或其盐，它是丙氨酸，谷氨酸，赖氨酸，酪氨酸和苯丙氨酸的线性无规共聚物。

9. 发明申请

WO2012001673A1 AMORPHOUS FORM OF DRONEDARONE 审中-公开
标题翻译：龙胆无机形式
公开(公告)号：WO2012001673A1
公开(公告)日：2012-01-05
申请号：PCT/IL2010/000961
申请日：2010-11-17
申请人： MAPI PHARMA HOLDINGS (CYPRUS) LIMITED , MAROM, Ehud , RUBNOV, Shai
发明人： MAROM, Ehud , RUBNOV, Shai
IPC分类号： A01N43/08 , A61K31/34
CPC分类号： A61K31/34 , C07D307/80
摘要： The present invention provides an amorphous form of dronedarone or salt thereof, particularly amorphous dronedarone HCl, pharmaceutical compositions comprising same, methods for its preparation and use thereof in treating cardiac arrhythmias. The amorphous dronedarone HCl has superior aqueous solubility and density characteristics as compared with crystalline dronedarone HCl.
摘要翻译：本发明提供无限形式的决奈达隆或其盐，特别是无定形决奈达隆HCl，包含其的药物组合物，其制备方法和用于治疗心律失常的方法。与结晶决奈达隆HCl相比，无定形决奈达隆HCl具有优异的水溶性和密度特性。

10. 发明申请

WO2010109468A1 PROCESS FOR THE PREPARATION OF ALOGLIPTIN 审中-公开
标题翻译：制备阿德列酮的方法
公开(公告)号：WO2010109468A1
公开(公告)日：2010-09-30
申请号：PCT/IL2010/000260
申请日：2010-03-25
申请人： MAPI PHARMA HK LIMITED , MAROM, Ehud , MIZHIRITSKII, Michael , RUBNOV, Shai
发明人： MAROM, Ehud , MIZHIRITSKII, Michael , RUBNOV, Shai
IPC分类号： A01N43/54
CPC分类号： A61K31/513 , C07C275/24 , C07C275/50 , C07D239/545 , C07D239/62 , C07D403/04
摘要： The present invention is based on the discovery of a process for preparing pyrimidin- dione compounds, especially alogliptin and its derivatives, which comprises the reaction of a urea derivative of formula (VIII) with a malonic acid or its derivatives to form intermediates of formulae (VII) or (VII-A), which are subsequently converted to a compound of formula (II) upon introduction of a leaving group X. Compound (II) then reacts with an amine to form compound (I), which is optionally converted to its salts of formula (IV).
摘要翻译：本发明基于发现制备嘧啶二酮化合物，特别是奥曲肽及其衍生物的方法，其包括式（VIII）的脲衍生物与丙二酸或其衍生物的反应，形成式 VII）或（VII-A），其随后在引入离去基团X时转化为式（II）化合物。然后化合物（II）与胺反应以形成化合物（I），其可任选地转化为其式（Ⅳ）的盐。

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