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1. 发明申请

US20060084668A1 Isolated valacyclovir impurity, process for the preparation of valacyclovir impurity and use as a reference standard 失效
标题翻译：隔离的伐昔洛韦杂质，制备伐昔洛韦杂质的过程，并用作参考标准
公开(公告)号：US20060084668A1
公开(公告)日：2006-04-20
申请号：US11221124
申请日：2005-09-06
申请人： Amihai Eisenstadt , Michael Pesachovich
发明人： Amihai Eisenstadt , Michael Pesachovich
IPC分类号： A61K31/522 , C07D473/10
CPC分类号： C07D473/18 , Y10T436/147777
摘要： The present invention provides an isolated N-formyl valacyclovir, its preaparation and its use as a reference marker and/or reference standard.
摘要翻译：本发明提供分离的N-甲酰伐昔洛韦，其预制和其用作参考标记和/或参考标准。

2. 发明申请

US20060122271A1 Stable gabapentin having pH within a controlled range 审中-公开
公开(公告)号：US20060122271A1
公开(公告)日：2006-06-08
申请号：US11336552
申请日：2006-01-20
申请人： Claude Singer , Gideon Pilarski , Michael Pesachovich , Eduard Schwartz
发明人： Claude Singer , Gideon Pilarski , Michael Pesachovich , Eduard Schwartz
IPC分类号： A61K31/195 , A61K9/20
CPC分类号： A61K31/195 , A61K9/145 , A61K9/2013 , A61K9/2054 , A61K9/2059 , C07C227/40 , C07C227/44 , C07C2601/14 , C07D209/96 , C07C229/28
摘要： A pharmaceutical composition containing substantially pure and stable gabapentin are disclosed wherein gabapentin has a pH of between 6.8 to 7.3.

3. 发明申请

US20070199856A1 Methods of stabilizing azithromycin 审中-公开
标题翻译：稳定阿奇霉素的方法
公开(公告)号：US20070199856A1
公开(公告)日：2007-08-30
申请号：US11521594
申请日：2006-09-14
申请人： Michael Pesachovich , Sarah Isaacs , Claude Singer , Eduard Schwartz , Edit Berger , Ruth Tenengauzer , Joseph Schwarz , Julia Hrakovsky , Tania Lessen , Lev Khondo , Mathi Mathivanan
发明人： Michael Pesachovich , Sarah Isaacs , Claude Singer , Eduard Schwartz , Edit Berger , Ruth Tenengauzer , Joseph Schwarz , Julia Hrakovsky , Tania Lessen , Lev Khondo , Mathi Mathivanan
IPC分类号： B65D85/84
CPC分类号： A61K9/2009 , A61K9/2013 , A61K9/2027 , A61K9/2054
摘要： A method of packaging of azithromycin which provides improved stability of azithromycin upon storage. Additionally, compositions and methods of stabilizing azithromycin compositions are described. Stabilized azithromycin compositions comprise an intimate admixture of azithromycin and a stabilizing-effective amount of an antioxidant to improve the resistance of the azithromycin to degradation. Coprecipitation or co-milling of azithromycin and an antioxidant are particularly preferred means of achieving an intimate admixture. Pharmaceutical formulations comprising a stabilized azithromycin composition and methods of making such formulations are also described.
摘要翻译：包装阿奇霉素的方法，其提供阿奇霉素在储存时的改善的稳定性。另外，描述了稳定阿奇霉素组合物的组合物和方法。稳定的阿奇霉素组合物包含阿奇霉素和稳定有效量的抗氧化剂的紧密混合物，以改善阿奇霉素降解的抗性。阿奇霉素和抗氧化剂的共沉淀或共研磨是特别优选的实现紧密混合的方法。还描述了包含稳定的阿奇霉素组合物的药物制剂和制备这些制剂的方法。

4. 发明申请

US20060252803A1 Hydrogenation of precursors to thiazolidinedione antihyperglycemics 审中-公开
标题翻译：将前体氢化成噻唑烷二酮抗高血糖药
公开(公告)号：US20060252803A1
公开(公告)日：2006-11-09
申请号：US11341006
申请日：2006-01-26
申请人： Ben-Zion Dolitzky , Michael Pesachovich
发明人： Ben-Zion Dolitzky , Michael Pesachovich
IPC分类号： A61K31/4439 , C07D417/02
CPC分类号： C07D417/12 , C07D277/34
摘要： Provided is pioglitazone having a low level of impurities, especially a low level of the precursor PIE. Also provided is a method for making pioglitazone having a low level of impurities.
摘要翻译：提供具有低水平杂质的吡格列酮，特别是低水平的前体PIE。还提供了制备具有低水平杂质的吡格列酮的方法。

5. 发明授权

US06255526B1 Preparation of gabapentin 失效
标题翻译：加巴喷丁的制备
公开(公告)号：US06255526B1
公开(公告)日：2001-07-03
申请号：US09331555
申请日：1999-06-22
申请人： Michael Pesachovich , Claude Singer , Gideon Pilarski
发明人： Michael Pesachovich , Claude Singer , Gideon Pilarski
IPC分类号： C07C6106
CPC分类号： C07C227/42 , C07C229/28 , C07C2601/14
摘要： There is disclosed a method of converting gabapenting hydrochloride substantially free of inorganic salts to gabapenting form II. The method comprises the steps of: (1) obtaining gabapentin hydrochloride that is substantially free of inorganic salts; (2) mixing a solution of the gabapenting hydrochloride with an additional amine in a first solvent so as to obtain a precipitate comprising gabapenting; and then (3) recovering gabapentin form II from the precipitate. The precipitated gabapentin is a novel polymorphic form of gabapentin possessing a crystalline structure characterized by novel sets of peaks in the powder X-ray diffraction pattern and in the FTIR spectra. This newly disclosed polymorph of gabapentin is characterized herein as gabapentin form III. The recovery step may comprise, for example, one of two alternative methods, slurrying the gabapentin form II in methanol, and then filtering the suspension to obtain gabapentin form II, or solubilizing the gabapentin form III in methanol with heating by reflux, and then cooling the solution to obtain gabapentin form II by crystallization.
摘要翻译：公开了一种将基本上不含无机盐的盐酸氢化盐转化为耙状II的方法。该方法包括以下步骤：（1）获得基本上不含无机盐的盐酸加巴喷丁; （2）在第一溶剂中将加巴喷丁盐酸盐溶液与另外的胺混合，以获得包含加砂的沉淀物; 然后（3）从沉淀物中回收加巴喷丁II型。沉淀的加巴喷丁是一种具有特征在于粉末X射线衍射图和FTIR光谱中新颖的峰组的加巴喷丁的新型多晶型物。这种新公开的加巴喷丁多晶型物在本文中被表征为加巴喷丁形式III。回收步骤可以包括例如两种替代方法之一，将加巴喷丁II型在甲醇中制浆，然后过滤悬浮液以获得形式II的加巴喷丁，或者通过回流加热将加巴喷丁形式III溶解在甲醇中，然后冷却通过结晶获得形式II的加巴喷丁的溶液。

6. 发明申请

US20070082055A1 Stable micronized candesartan cilexetil and methods for preparing thereof 审中-公开
标题翻译：稳定的微粉化坎地沙坦碳酸酯及其制备方法
公开(公告)号：US20070082055A1
公开(公告)日：2007-04-12
申请号：US11432108
申请日：2006-05-10
申请人： Ziv Kurgan , Michael Pesachovich
发明人： Ziv Kurgan , Michael Pesachovich
IPC分类号： A61K31/4184 , A61K9/14
CPC分类号： C07D403/10 , A61K9/141 , A61K31/4184
摘要： The invention encompasses sable candesartan cilexetil of fine particle size, wherein desethyl-candesartan (desethyl-CNS) within the stable candesartan cilexetil does not increase to more than about 0.1% w/w by HPLC relative to the initial amount of candesartan cilexetil, when the stable candesartan cilexetil is maintained at a temperature of about 55° C. for at least 2 weeks, methods of making the same and pharmaceutical compositions thereof.
摘要翻译：本发明包括细粒度的稳定的坎地沙坦酯，其中稳定的坎地沙坦酯中的去甲基 - 坎地沙坦（去甲基 - 中枢神经系统）相对于初始量的坎地沙坦cilexetil，通过HPLC不会增加到超过约0.1％w / w，当将稳定的坎地沙坦片塞维持在约55℃的温度下至少2周，其制备方法及其药物组合物。

7. 发明申请

US20050192296A1 Process for the preparation of valacyclovir hydrochloride 审中-公开
标题翻译：盐酸伐昔洛韦制备方法
公开(公告)号：US20050192296A1
公开(公告)日：2005-09-01
申请号：US11040925
申请日：2005-01-21
申请人： Zvi Harel , Michael Pesachovich
发明人： Zvi Harel , Michael Pesachovich
IPC分类号： C07D473/00 , C07D473/10 , A61K31/522
CPC分类号： C07D473/00
摘要： Provided are HPLC methods for analyzing BOC-L-alanine in BOC-L-valine and alanine analogues in valacyclovir hydrochloride and a use and method of selecting valacyclovir compositions.
摘要翻译：提供了用于分析盐酸伐昔洛韦中的BOC-L-缬氨酸和丙氨酸类似物中的BOC-L-丙氨酸的HPLC方法和选择伐昔洛韦组合物的用途和方法。

8. 发明申请

US20050106239A1 Stabilized azithromycin compositions 审中-公开
标题翻译：稳定的阿奇霉素组合物
公开(公告)号：US20050106239A1
公开(公告)日：2005-05-19
申请号：US10936075
申请日：2004-09-07
申请人： Ruth Tenengauzer , Joseph Schwarz , Julia Hrakovsky , Tania Lessen , Lev Khondo , Mathi Mathivanan , Claude Singer , Michael Pesachovich
发明人： Ruth Tenengauzer , Joseph Schwarz , Julia Hrakovsky , Tania Lessen , Lev Khondo , Mathi Mathivanan , Claude Singer , Michael Pesachovich
IPC分类号： A61K9/00 , A61K9/14 , A61K9/16 , A61K9/20 , A61K31/353 , A61K31/375 , A61K31/70 , A61K31/7048 , A61K31/7052 , A61K47/10
CPC分类号： A61K9/1617 , A61K9/0095 , A61K9/145 , A61K9/2077 , A61K31/7052
摘要： Compositions and methods of stabilizing azithromycin compositions are described. Stabilized azithromycin compositions comprise an intimate admixture of azithromycin and a stabilizing-effective amount of an antioxidant to improve the resistance of the azithromycin to degradation. Coprecipitation or co-milling of azithromycin and an antioxidant are particularly preferred means of achieving an intimate admixture. Pharmaceutical formulations comprising a stabilized azithromycin composition and methods of making such formulations are also described.
摘要翻译：描述了稳定阿奇霉素组合物的组合物和方法。稳定的阿奇霉素组合物包含阿奇霉素和稳定有效量的抗氧化剂的紧密混合物，以改善阿奇霉素降解的抗性。阿奇霉素和抗氧化剂的共沉淀或共研磨是特别优选的实现紧密混合的方法。还描述了包含稳定的阿奇霉素组合物的药物制剂和制备这些制剂的方法。

9. 发明授权

US06586576B2 Preparation method of azithromycin hydrates 失效
标题翻译：阿奇霉素水合物的制备方法
公开(公告)号：US06586576B2
公开(公告)日：2003-07-01
申请号：US09755829
申请日：2001-01-04
申请人： Judith Aronhime , Claude Singer , Michael Pesachovich
发明人： Judith Aronhime , Claude Singer , Michael Pesachovich
IPC分类号： C07H1708
CPC分类号： C07H17/08 , C07H17/00
摘要： This invention relates to a method for preparing azithromycin dihydrate from crude azithromycin by the gradual crystallization of azithromycin from acetone by the addition of a minimal amount of water to effect crystal formation is disclosed. This invention also relates to a method of making azithromycin from desmethyl-azithromycin by dissolving desmethyl-azithromycin in acetone, adding activated carbon, adding formaldehyde, adding formic acid; refluxing the desmethyl-azithromycin acetone solution, adding sodium hydroxide to induce precipitation of azithromycin, and isolating azithromycin.
摘要翻译：本发明涉及从阿奇霉素制备阿奇霉素二水合物的方法，其通过加入最少量的水来实现晶体形成，由阿奇霉素从丙酮中逐渐结晶。本发明还涉及通过将去甲基 - 阿奇霉素溶解在丙酮中，加入活性炭，加入甲醛，加入甲酸，由去甲基 - 阿奇霉素制备阿奇霉素的方法。回流脱甲基阿奇霉素丙酮溶液，加入氢氧化钠诱导阿奇霉素沉淀，分离阿奇霉素。

10. 发明授权

US07629461B2 Isolated valacyclovir impurity, process for the preparation of valacyclovir impurity and use as a reference standard 失效
标题翻译：隔离的伐昔洛韦杂质，制备伐昔洛韦杂质的过程，并用作参考标准
公开(公告)号：US07629461B2
公开(公告)日：2009-12-08
申请号：US11221124
申请日：2005-09-06
申请人： Amihai Eisenstadt , Michael Pesachovich
发明人： Amihai Eisenstadt , Michael Pesachovich
IPC分类号： C07D473/18 , G01N33/15
CPC分类号： C07D473/18 , Y10T436/147777
摘要： The present invention provides an isolated N-formyl valacyclovir, its preparation and its use as a reference marker and/or reference standard.
摘要翻译：本发明提供了一种分离的N-甲酰伐昔洛韦，其制备及其用作参考标记和/或参考标准。

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