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1. 发明授权

US07579461B2 Processes for the preparation of rocuronium bromide and intermediates thereof 失效
标题翻译：罗库溴铵的制备方法及其中间体
公开(公告)号：US07579461B2
公开(公告)日：2009-08-25
申请号：US11034510
申请日：2005-01-13
申请人： Eliezer Adar , David Sondack , Oded Friedman , Iosef Manascu , Tamir Fizitzki , Boris Freger , Oded Arad , Alexander Weisman , Joseph Kaspi
发明人： Eliezer Adar , David Sondack , Oded Friedman , Iosef Manascu , Tamir Fizitzki , Boris Freger , Oded Arad , Alexander Weisman , Joseph Kaspi
IPC分类号： C07J43/00
CPC分类号： C07J43/00 , C07J11/00
摘要： A novel process for preparing (2β,3α,5α,16β,17β)-17-acetoxy-3-hydroxy-2-(4-morpholinyl)-16-(1-pyrrolidinyl) androstane, a known intermediate in the synthesis of the skeletal muscle relaxant rocuronium bromide, is disclosed.
摘要翻译：一种制备（2beta，3α，5α，16beta，17β）-17-乙酰氧基-3-羟基-2-（4-吗啉基）-16-（1-吡咯烷基）雄甾烷的新方法，公开了骨骼肌松弛剂罗库溴铵。

2. 发明申请

US20050159398A1 Processes for the preparation of rocuronium bromide and intermediates thereof 失效
标题翻译：罗库溴铵的制备方法及其中间体
公开(公告)号：US20050159398A1
公开(公告)日：2005-07-21
申请号：US11034510
申请日：2005-01-13
申请人： Eliezer Adar , David Sondack , Oded Friedman , Iosef Manascu , Tamir Fizitzki , Boris Freger , Oded Arad , Alexander Weisman , Joseph Kaspi
发明人： Eliezer Adar , David Sondack , Oded Friedman , Iosef Manascu , Tamir Fizitzki , Boris Freger , Oded Arad , Alexander Weisman , Joseph Kaspi
IPC分类号： A61K31/58 , C07J11/00 , C07J43/00
CPC分类号： C07J43/00 , C07J11/00
摘要： A novel process for preparing (2β,3α,5α,16β,17β)-17-acetoxy-3-hydroxy-2-(4-morpholinyl)-16-(1-pyrrolidinyl)androstane, a known intermediate in the synthesis of the skeletal muscle relaxant rocuronium bromide, is disclosed.
摘要翻译：一种制备（2beta，3α，5α，16beta，17β）-17-乙酰氧基-3-羟基-2-（4-吗啉基）-16-（1-吡咯烷基）雄甾烷的新方法，公开了骨骼肌松弛剂罗库溴铵。

3. 发明申请

US20060058276A1 Processes for the preparation and purification of rocuronium bromide 审中-公开
标题翻译：罗库溴铵的制备和纯化方法
公开(公告)号：US20060058276A1
公开(公告)日：2006-03-16
申请号：US11180716
申请日：2005-07-14
申请人： Oded Friedman , Oded Arad , Iosef Manascu , Tamir Fizitzki , Boris Freger , Joseph Kaspi
发明人： Oded Friedman , Oded Arad , Iosef Manascu , Tamir Fizitzki , Boris Freger , Joseph Kaspi
IPC分类号： A61K31/58
CPC分类号： A61K31/58
摘要： Processes are provided herein for the preparation of pure rocuronium bromide and for the purification of impure rocuronium bromide obviating the need for column chromatography and that can be easily, conveniently and inexpensively scaled-up.
摘要翻译：本文提供了用于制备纯罗库溴铵和用于纯化不纯的罗库溴铵溴化物的方法，从而避免了对柱色谱法的需要，并且可以容易地，方便和廉价地放大。

4. 发明申请

US20060004230A1 Process for the preparation of terbinafine and salts thereof 审中-公开
标题翻译：特比萘芬及其盐的制备方法
公开(公告)号：US20060004230A1
公开(公告)日：2006-01-05
申请号：US10879549
申请日：2004-06-30
申请人： Joseph Kaspi , Oded Arad , Oded Friedman , Iosef Manascu , Tamir Fizitzki , Edna Danon
发明人： Joseph Kaspi , Oded Arad , Oded Friedman , Iosef Manascu , Tamir Fizitzki , Edna Danon
IPC分类号： A61K31/137 , C07C29/10
CPC分类号： C07C209/08 , C07C17/00 , C07C21/22 , C07C29/40 , C07C211/30 , C07C33/048
摘要： A process for the preparation of Terbinafine and salts thereof by reacting 1-chloro-6,6-dimethylhept-2-en-4-yne and N-methyl-N-(1-naphthylmethyl)amine in a basic aqueous medium is disclosed. Also disclosed is a process for the preparation of 1-chloro-6,6-dimethylhept-2-en-4-yne.
摘要翻译：公开了通过使1-氯-6,6-二甲基庚-2-烯-4-炔和N-甲基-N-（1-萘基甲基）胺在碱性水性介质中的反应制备特比萘芬及其盐的方法。还公开了制备1-氯-6,6-二甲基庚-2-烯-4-基的方法。

5. 发明申请

US20060058275A1 Processes for preparing stabilized, highly pure rocuronium bromide 审中-公开
标题翻译：制备稳定，高纯度罗库溴铵的方法
公开(公告)号：US20060058275A1
公开(公告)日：2006-03-16
申请号：US11180715
申请日：2005-07-14
申请人： Oded Friedman , Oded Arad , Iosef Manascu , Tamir Fizitzki , Joseph Kaspi
发明人： Oded Friedman , Oded Arad , Iosef Manascu , Tamir Fizitzki , Joseph Kaspi
IPC分类号： A61K31/58
CPC分类号： A61K31/58
摘要： Processes are provided herein for the preparation and purification of stable, powdered solids comprising substantially pure rocuronium bromide.
摘要翻译：本文提供了用于制备和纯化包含基本上纯的罗库溴铵的稳定的粉末状固体的方法。

6. 发明申请

US20060009485A1 Method of reprocessing quaternary ammonium-containing neuromuscular blocking agents 审中-公开
标题翻译：含季铵盐的神经肌肉阻滞剂的再加工方法
公开(公告)号：US20060009485A1
公开(公告)日：2006-01-12
申请号：US11159891
申请日：2005-06-23
申请人： Oded Friedman , Oded Arad , Tamir Fizitzki , Josef Manasku , Joseph Kaspi
发明人： Oded Friedman , Oded Arad , Tamir Fizitzki , Josef Manasku , Joseph Kaspi
IPC分类号： A01N43/42 , A61K31/47
CPC分类号： C07J43/003
摘要： Provided is a method for reprocessing neuromuscular blocking agents containing a quaternary ammonium salt, e.g., Rocuronium bromide, using a novel dealkylation method. The process is effective in obtaining a highly pure product from a contaminated starting material by heating, optionally in the presence of an organic solvent, to produce a dealkyated product. The dealkylated product is purified, e.g., by crystallization, and converted by any known method to a stable, highly-pure neuromuscular blocking agent.
摘要翻译：提供了一种使用新的脱烷基方法再次处理含有季铵盐（例如溴溴氰菊酯）的神经肌肉阻滞剂的方法。该方法有效地通过加热，任选在有机溶剂的存在下从受污染的原料获得高纯度产物，以产生脱烷基化的产物。脱烷基化产物例如通过结晶纯化，并通过任何已知的方法转化成稳定的，高纯度的神经肌肉阻滞剂。

7. 发明申请

US20070112202A1 Letrozole production process 失效
标题翻译：来曲唑生产过程
公开(公告)号：US20070112202A1
公开(公告)日：2007-05-17
申请号：US11273276
申请日：2005-11-14
申请人： Oded Friedman , Boris Freger , Olga Etlin , Julia Ditkovitch , Edna Danon , Yana Seryi , Guy Davidi , Oded Arad , Joseph Kaspi
发明人： Oded Friedman , Boris Freger , Olga Etlin , Julia Ditkovitch , Edna Danon , Yana Seryi , Guy Davidi , Oded Arad , Joseph Kaspi
IPC分类号： C07D249/08
CPC分类号： C07D249/08
摘要： Provided is a method for preparing letrozole, which includes reacting an activated bis-(4-cyanophenyl)-methane with a triazole to produce letrozole, and, optionally, purifying the letrozole. Also provided are highly pure letrozole, and a method of purifying letrozole, which method includes precipitating letrozole, e.g., by selective precipitation from a reaction mixture and/or by subjecting the letrozole to one or more crystallizations.
摘要翻译：提供了一种制备来曲唑的方法，其包括使活化的双 - （4-氰基苯基） - 甲烷与三唑反应以产生来曲唑，并且任选地纯化来曲唑。还提供了高纯度的来曲唑和纯化来曲唑的方法，该方法包括例如通过从反应混合物中选择性沉淀和/或使来曲唑进行一次或多次结晶来沉淀来曲唑。

8. 发明授权

US07538230B2 Letrozole production process 失效
标题翻译：来曲唑生产过程
公开(公告)号：US07538230B2
公开(公告)日：2009-05-26
申请号：US11273276
申请日：2005-11-14
申请人： Oded Friedman , Boris Freger , Olga Etlin , Julia Ditkovitch , Edna Danon , Yana Seryi , Guy Davidi , Oded Arad , Joseph Kaspi
发明人： Oded Friedman , Boris Freger , Olga Etlin , Julia Ditkovitch , Edna Danon , Yana Seryi , Guy Davidi , Oded Arad , Joseph Kaspi
IPC分类号： C07D249/08
CPC分类号： C07D249/08
摘要： Provided is a method for preparing letrozole, which includes reacting an activated bis-(4-cyanophenyl)-methane with a triazole to produce letrozole, and, optionally, purifying the letrozole. Also provided are highly pure letrozole, and a method of purifying letrozole, which method includes precipitating letrozole, e.g., by selective precipitation from a reaction mixture and/or by subjecting the letrozole to one or more crystallizations.
摘要翻译：提供了一种制备来曲唑的方法，其包括使活化的双 - （4-氰基苯基） - 甲烷与三唑反应以产生来曲唑，并且任选地纯化来曲唑。还提供了高纯度的来曲唑和纯化来曲唑的方法，该方法包括例如通过从反应混合物中选择性沉淀和/或使来曲唑进行一次或多次结晶来沉淀来曲唑。

9. 发明授权

US06570044B2 Process for the preparation of 6,6-dimethylhept-1-en-4-yn-3-ol 失效
公开(公告)号：US06570044B2
公开(公告)日：2003-05-27
申请号：US09906105
申请日：2001-07-17
申请人： Joseph Kaspi , Oded Friedman , Edna Danon
发明人： Joseph Kaspi , Oded Friedman , Edna Danon
IPC分类号： C07C3304
CPC分类号： C07C29/42 , C07C33/048 , C07C33/30
摘要： The invention provides a process for the preparation of 6,6-dimethylhept-1-en-4-yn-3-ol comprising of reacting t-butylacetylene with a proton-extracting agent selected from the group consisting of an organometallic compound and metallic lithium to form a t-butylacetylide, reacting the acetylide with acrolein at temperatures between −40° C. to +20° C., quenching the reaction mixture and isolating the product.

10. 发明授权

US06270803B1 Controlled-release garlic formulations 失效
标题翻译：控释大蒜制剂
公开(公告)号：US06270803B1
公开(公告)日：2001-08-07
申请号：US09392754
申请日：1998-10-07
申请人： Yoav Blatt , David Cohen , Eugene Kimmelman , Oded Friedman , Avner Rotman
发明人： Yoav Blatt , David Cohen , Eugene Kimmelman , Oded Friedman , Avner Rotman
IPC分类号： A61K914
CPC分类号： A61K9/5073 , A61K9/2081 , A61K9/5042 , A61K9/5047 , A61K36/8962 , A61K2300/00
摘要： There are provided orally-administrable formulations for the controlled release of granulated garlic, comprising particles of granulated garlic coated with a film comprising a mixture of at least one water soluble polymer and at least one water insoluble polymer, said at least one water soluble polymer and at least one water insoluble polymer being present in a ratio that produces a substantially zero order linear release pattern of at least one active ingredient. Preferably, the formulations are characterized in that the total in vitro dissolution time of said formulations required for release of 75% of the Allicin available from said formulations based upon the total amount of alliin initially present in said formulations is between about 4 and about 12 hours, as determined by U.S.P. XXIII paddle method at a paddle speed of 150 rpm, using simulated intestinal fluid without the digestive enzymes normally found in intestinal fluid, containing 0.1% w/w sodium dodecyl sulfate (SDS), at pH 6.8, and a temperature of 37° C. A process for preparing the formulations of the invention is also disclosed.
摘要翻译：提供了用于受控释放造粒大蒜的口服给药制剂，其包括用包含至少一种水溶性聚合物和至少一种水不溶性聚合物的混合物的膜的粒状大蒜颗粒，所述至少一种水溶性聚合物和至少一种水不溶性聚合物以一定比例存在，其产生至少一种活性成分的基本零级线性释放模式。优选地，制剂的特征在于，基于最初存在于所述制剂中的蒜素的总量，从所述制剂释放75％的大蒜素所需的所述制剂的总体外溶出时间为约4至约12小时，由USP确定 XXIII桨法以150rpm的桨叶速度，使用模拟肠液，不含肠液中通常存在的消化酶，含有0.1％w / w十二烷基硫酸钠（SDS），pH 6.8，温度为37℃。还公开了制备本发明制剂的方法。

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