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公开(公告)号：US20060217557A1
公开(公告)日：2006-09-28
申请号：US11243496
申请日：2005-10-03
申请人： Barnaba Krochmal , Dov Diller , Ben-Zion Dolitzky , Judith Aronhime , Shlomit Wizel , Boaz Gome , Igor Lifshitz
发明人： Barnaba Krochmal , Dov Diller , Ben-Zion Dolitzky , Judith Aronhime , Shlomit Wizel , Boaz Gome , Igor Lifshitz
IPC分类号： C07D211/34
CPC分类号： C07D211/22
摘要： Provided is a crystalline (polymorphic) form of fexofenadine hydrochloride, denominated fexofenadine hydrochloride Form XVI.
摘要翻译： 提供盐酸非索非那定的结晶（多晶型）形式，称为盐酸非索非那定形式XVI。
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公开(公告)号：US07098342B2
公开(公告)日：2006-08-29
申请号：US10968710
申请日：2004-10-18
IPC分类号： C07D403/08 , C07D257/04
CPC分类号： C07D403/10
摘要： The invention encompasses processes for the synthesis of cilexetil trityl candesartan from the reaction of trityl candesartan with cilexetil halide in the presence of a base and a low boiling organic solvent. Optionally, the reaction may be conducted in the presence of a phase transfer catalyst.
摘要翻译： 本发明包括在碱和低沸点有机溶剂的存在下，从三苯甲基坎地沙坦与碳酸吡哩啶卤化物的反应合成曲塞沙星三苯甲基坎地沙坦的方法。 任选地，反应可以在相转移催化剂的存在下进行。
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![Novel synthesis of 2-Butyl-3-(1-trityl-1H-tetrazol-5-YL)biphenyl-4-YL)-1,3-diazaspiro[4,4]- non-ene-4-one](/abs-image/US/2006/06/15/US20060128967A1/abs.jpg.150x150.jpg)
83.发明申请Novel synthesis of 2-Butyl-3-(1-trityl-1H-tetrazol-5-YL)biphenyl-4-YL)-1,3-diazaspiro[4,4]- non-ene-4-one 失效2-丁基-3-（1-三苯甲基-1H-四唑-5-基）联苯-4-YL）-1,3-二氮杂螺[4,4] - 壬-4-酮的新合成公开(公告)号：US20060128967A1
公开(公告)日：2006-06-15
申请号：US11328966
申请日：2006-01-09
IPC分类号： C07D403/02
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。
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公开(公告)号：US07041832B2
公开(公告)日：2006-05-09
申请号：US10426612
申请日：2003-04-29
申请人： Ben-Zion Dolitzky
发明人： Ben-Zion Dolitzky
IPC分类号： C07D257/00
CPC分类号： C07D403/10
摘要： Losartan is prepared by acid catalyzed cleavage of a triarylmethyl group from a triarylmethyl-substituted losartan derivative in a diluent comprising liquid ketone. The reaction mixture is basified and liquid ketone is evaporated from the mixture leaving a residue from which a triarylmethyl alcohol and losartan are each obtained in high yield and high purity. In addition, losartan potassium is prepared by a process that is more convenient that those previously known in the art in which losartan is contacted with potassium ions in substantially pure liquid alcohol and losartan potassium is precipitated from the alcohol.
摘要翻译： 氯沙坦通过在包含液体酮的稀释剂中由三芳基甲基取代的氯沙坦衍生物进行酸催化裂解三芳基甲基来制备。 将反应混合物碱化，并从混合物中蒸发出液体酮，留下残余物，从中以高产率和高纯度各自获得三芳基甲醇和氯沙坦。 此外，氯沙坦钾通过以下方法制备，该方法比本领域已知的氯沙坦与基本上纯的液体醇中的钾离子和氯沙坦钾从醇中沉淀出来的方法更为方便。
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![Synthesis of 2-butyl-3-(2′-(1-trityl-1H-tetrazol-5-yl)biphenyl-4-yl)-1,3-diazaspiro[4.4]-non-ene-4-one](/abs-image/US/2006/05/02/US07038060B2/abs.jpg.150x150.jpg)
85.发明授权Synthesis of 2-butyl-3-(2′-(1-trityl-1H-tetrazol-5-yl)biphenyl-4-yl)-1,3-diazaspiro[4.4]-non-ene-4-one 失效2-丁基-3-（2' - （1-三苯甲基-1H-四唑-5-基）联苯-4-基）-1,3-二氮杂螺[4.4]壬烯-4-酮的合成公开(公告)号：US07038060B2
公开(公告)日：2006-05-02
申请号：US10773414
申请日：2004-02-05
IPC分类号： C07D257/04 , C07D403/10 , C07D487/10 , C07C69/74
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]壬-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。
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公开(公告)号：US20060052586A1
公开(公告)日：2006-03-09
申请号：US11223072
申请日：2005-09-09
申请人： Ben-Zion Dolitzky
发明人： Ben-Zion Dolitzky
IPC分类号： C07K14/00
CPC分类号： C07K14/00 , C07K14/001 , C07K14/4713
摘要： The subject invention provides an improved process for obtaining a mixture of polypeptides having nonuniform amino acid sequences, where each polypeptide consists essentially of alanine, glutamic acid, tyrosine and lysine where the resulting mixture of polypeptides comprises less than 0.3% brominated tyrosine and less than 1000 ppm metal ion impurities.
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公开(公告)号：US20060030614A1
公开(公告)日：2006-02-09
申请号：US11217643
申请日：2005-08-31
申请人： Jean Hildesheim , Sergey Finogueev , Judith Aronhime , Ben-Zion Dolitzky , Shoshana Ben-Valid , Iian Kor
发明人： Jean Hildesheim , Sergey Finogueev , Judith Aronhime , Ben-Zion Dolitzky , Shoshana Ben-Valid , Iian Kor
IPC分类号： A61K31/403 , C07D209/82
CPC分类号： C07D209/88
摘要： This invention relates to an improved process of preparing carvedilol, as well as a new crystalline hydrate and solvate and forms of carvedilol, processes for the manufacture thereof, and pharmaceutical compositions thereof.
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公开(公告)号：US06992191B2
公开(公告)日：2006-01-31
申请号：US10324928
申请日：2002-12-20
申请人： Ben-Zion Dolitzky
发明人： Ben-Zion Dolitzky
IPC分类号： C07D417/10 , C07D277/34 , A61K31/4439 , A61K31/427
CPC分类号： C07D277/20 , C07D277/34 , C07D417/12
摘要： Provided is a method of hydrogenating the exocyclic double bond of a thiazolidinedione precursor in a method of making a thiazolidinedione antihyperglycemic, for example pioglitazone, including work-up steps to afford pure thiazolidinedione antihyperglycemic.
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公开(公告)号：US20050143400A1
公开(公告)日：2005-06-30
申请号：US10932120
申请日：2004-09-02
申请人： Genny Shamai , Shlomo Antebi , David Ioffe , Ben-Zion Dolitzky , Batia Kauffmann
发明人： Genny Shamai , Shlomo Antebi , David Ioffe , Ben-Zion Dolitzky , Batia Kauffmann
IPC分类号： A61K31/522 , C07D473/14 , C07D473/32
CPC分类号： C07D473/32
摘要： The invention provides a process for making famciclovir, comprising reacting 9-[4-acetoxy-3-(acetoxymethyl)but-1-yl]-2-amino-6-chloropurine (Cl-FMC) with a palladium on charcoal catalyst in water and ammonium formate. The invention also provides methods of treating viral diseases by administering the famciclovir prepared according to the above process.
摘要翻译： 本发明提供了制备泛昔洛韦的方法，其包括使9- [4-乙酰氧基-3-（乙酰氧基甲基）丁-1-基] -2-氨基-6-氯嘌呤（Cl-FMC）与钯/炭催化剂在水 和甲酸铵。 本发明还提供了通过施用根据上述方法制备的泛昔洛韦来治疗病毒性疾病的方法。
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公开(公告)号：US20050080264A1
公开(公告)日：2005-04-14
申请号：US10641750
申请日：2003-08-14
IPC分类号： C07D215/56 , C07D43/02
CPC分类号： C07D215/56 , C07D401/04
摘要： Provided are a method for making (±)-1-Cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolenecarboxylic acid, commonly known as gatifloxacin, in high purity, in a suspension in a dipolar aprotic solvent.
摘要翻译： 提供了制备（±）-1-环丙基-6-氟-1,4-二氢-8-甲氧基-7-（3-甲基-1-哌嗪基）-4-氧代-3-喹啉羧酸的方法，通常 称为加替沙星，高纯度，在偶极非质子溶剂中的悬浮液中。
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