专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

81. 发明申请

US20070093542A1 Process for the preparation of valsartan and intermediates thereof 审中-公开
标题翻译：制备缬沙坦及其中间体的方法
公开(公告)号：US20070093542A1
公开(公告)日：2007-04-26
申请号：US11639502
申请日：2006-12-14
申请人： Igor Rukhman , Ben-Zion Dolitzky , Evgeni Flyaks
发明人： Igor Rukhman , Ben-Zion Dolitzky , Evgeni Flyaks
IPC分类号： A61K31/41 , C07D257/02
CPC分类号： C07D257/04
摘要： Provided are process for the preparation of valsartan and the precursors thereof.
摘要翻译：提供制备缬沙坦及其前体的方法。

82. 发明授权

US07199144B2 Process for the preparation of valsartan and intermediates thereof 失效
公开(公告)号：US07199144B2
公开(公告)日：2007-04-03
申请号：US10829873
申请日：2004-04-21
申请人： Igor Rukhman , Ben-Zion Dolitzky , Evgeni Flyaks
发明人： Igor Rukhman , Ben-Zion Dolitzky , Evgeni Flyaks
IPC分类号： A61K31/41 , C07D257/00
CPC分类号： C07D257/04
摘要： Provided are process for the preparation of valsartan and the precursors thereof.

83. 发明申请

US20070072868A1 Novel synthesis of gatifloxacin 审中-公开
标题翻译：加替沙星的新型合成
公开(公告)号：US20070072868A1
公开(公告)日：2007-03-29
申请号：US11605565
申请日：2006-11-28
申请人： Valerie Niddam-Hildesheim , Ben-Zion Dolitzky , Gideon Pilarski , Greta Sterimbaum
发明人： Valerie Niddam-Hildesheim , Ben-Zion Dolitzky , Gideon Pilarski , Greta Sterimbaum
IPC分类号： A61K31/496 , C07D403/02
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。

84. 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。

85. 发明授权

US07102026B2 Process for preparing and isolating rac-bicalutamide and its intermediates 失效
标题翻译：制备和分离外加酯和其中间体的方法
公开(公告)号：US07102026B2
公开(公告)日：2006-09-05
申请号：US10606403
申请日：2003-06-25
申请人： Ben-Zion Dolitzky , Ofer Reany , Jenny Shammai
发明人： Ben-Zion Dolitzky , Ofer Reany , Jenny Shammai
IPC分类号： C07C255/50 , A61K31/275
CPC分类号： C07C255/58 , C07C315/04 , C07C317/14 , C07C319/14 , C07D301/14 , C07C317/46 , C07C323/52
摘要： The present invention relates to a new process for the synthesis of racemic and optically active bicalutamide starting from ethyl pyruvate and methyl methacrylate. The present invention discloses processes of preparing bicalutamide intermediates including ethyl-[2-{4-fluorophenyl sulfone}]-2-hydroxy propionate, 1,2-epoxy-2-methyl propionate and 2-hydrox-2-methyl-3-(4-fluorophenylthio) propionic acid. The present invention further discloses micronized rac-bicalutamide and the preparation thereof. The present invention further discloses a new process for the isolation and purification of racemic and optically active bicalutamide.
摘要翻译：本发明涉及从丙酮酸乙酯和甲基丙烯酸甲酯开始合成外消旋和光学活性比卡鲁胺的新方法。本发明公开了制备比卡鲁胺中间体的方法，包括乙基 - [2- {4-氟苯基砜}] - 2-羟基丙酸酯，1,2-环氧-2-甲基丙酸酯和2-羟基-2-甲基-3-（ 4-氟苯硫基）丙酸。本发明还公开了微粉化的外消旋 - 比卡鲁胺及其制备方法。本发明还公开了用于分离和纯化外消旋和光学活性比卡鲁胺的新方法。

86. 发明申请

US20060172942A1 Process for producing polypeptide mixtures using hydrogenolysis 审中-公开
标题翻译：使用氢解制备多肽混合物的方法
公开(公告)号：US20060172942A1
公开(公告)日：2006-08-03
申请号：US11336251
申请日：2006-01-20
申请人： Ben-Zion Dolitzky
发明人： Ben-Zion Dolitzky
IPC分类号： A61K38/17 , C07K1/02 , C07K14/00
CPC分类号： C07K14/001 , A61K38/00 , C07K1/061 , C07K1/12 , Y02P20/55
摘要： The subject invention provides for a process for making a mixture of acetate salts of polypeptides, each of which consisting of glutamic acid, alanine, tyrosine and lysine, wherein the mixture has a desired peak molecular weight, comprising: a) polymerizing N-carboxyanhydrides of tyrosine, alanine, γ-benzyl glutamate and trifluoroacetyllysine with an initiator in an amount of 0.01% to 20% by weight for a suitable period of time and at a suitable temperature to form a mixture of protected polypeptides, which mixture of polypeptides in unprotected form having a first peak molecular weight; b) removing the benzyl protecting group from the mixture of protected polypeptides by contacting the polypeptides with a hydrogenolysis catalyst and hydrogen to produce a mixture of trifluoroacetyl protected polypeptides, which mixture of polypeptides in unprotected form having the first peak molecular weight; c) removing the trifluoroacetyl protecting group from the trifluoroacetyl protected polypeptides by contacting the polypeptides with an organic base solution to form a mixture of polypeptides, which mixtures of polypeptides in unprotected form having the first peak molecular weight; d) removing the free trifluoroacetyl groups and low molecular weight impurities by ultrafiltration to obtain the mixture of polypeptides each of which consisting of glutamic acid, alanine, tyrosine and lysine; and e) contacting the mixture of polypeptides each of which consisting of glutamic acid, alanine, tyrosine and lysine with an aqueous solution of acetic acid to form the mixture of acetate salts of polypeptides each of which consisting of glutamic acid, alanine, tyrosine and lysine and having the desired peak molecular weight.
摘要翻译：本发明提供了制备多肽的乙酸盐的混合物的方法，其中每一种由谷氨酸，丙氨酸，酪氨酸和赖氨酸组成，其中所述混合物具有所需的峰分子量，其包括：a）使N-羧酸酐酪氨酸，丙氨酸，γ-苄基谷氨酸和三氟乙酰赖氨酸，其引发剂的量为0.01重量％至20重量％，持续适宜的时间和温度，以形成受保护的多肽的混合物，多肽的未受保护的形式具有第一峰分子量; b）通过使多肽与氢解催化剂和氢气接触来除去保护的多肽的混合物中的苄基保护基团，以产生三氟乙酰基保护的多肽的混合物，该多肽的未保护形式的混合物具有第一峰分子量; c）通过使多肽与有机碱溶液接触以形成多肽的混合物，从三氟乙酰保护的多肽中除去三氟乙酰基保护基，多肽的混合物以未保护形式具有第一峰分子量; d）通过超滤除去游离的三氟乙酰基和低分子量杂质，得到各自由谷氨酸，丙氨酸，酪氨酸和赖氨酸组成的多肽的混合物; 和e）将由谷氨酸，丙氨酸，酪氨酸和赖氨酸组成的各自的多肽混合物与乙酸的水溶液接触，形成各自由谷氨酸，丙氨酸，酪氨酸和赖氨酸组成的多肽的乙酸盐的混合物并具有所需的峰分子量。

87. 发明申请

US20060135780A1 Novel synthesis of irbesartan 失效
公开(公告)号：US20060135780A1
公开(公告)日：2006-06-22
申请号：US11349360
申请日：2006-02-06
申请人： Gennady Nisnevich , Igor Rukhman , Boris Pertsikov , Julia Kaftanov , Ben-Zion Dolitzky
发明人： Gennady Nisnevich , Igor Rukhman , Boris Pertsikov , Julia Kaftanov , Ben-Zion Dolitzky
IPC分类号： C07F5/02
CPC分类号： C07D235/02 , 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.

88. 发明申请

US20050215585A1 Method of making 7-(4-bromobutoxy)-3,4-dihydrocarbostyril 失效
标题翻译：制备7-（4-溴丁氧基）-3,4-二氢喹诺酮的方法
公开(公告)号：US20050215585A1
公开(公告)日：2005-09-29
申请号：US11053072
申请日：2005-02-07
申请人： Ben-Zion Dolitzky , Jean Hildesheim , Alisa Berlin
发明人： Ben-Zion Dolitzky , Jean Hildesheim , Alisa Berlin
IPC分类号： A61K31/4706 , C07D215/22 , C07D215/227
CPC分类号： C07D215/22 , C07D215/227
摘要： The invention encompasses synthesizing 7-(4-bromobutoxy)-3,4-dihydrocarbostyril by mixing 7-hydroxy-tetrahydroquinolinone, dibromobutane, and at least one base to form a reaction mixture; heating the reaction mixture; cooling the reaction mixture; and isolating the 7-(4-bromobutoxy)-3,4-dihydrocarbostyril from the reaction mixture. The invention also encompasses using phase transfer catalysts during the reaction.
摘要翻译：本发明包括通过混合7-羟基 - 四氢喹啉酮，二溴丁烷和至少一个碱来合成7-（4-溴丁氧基）-3,4-二氢喹诺酮，形成反应混合物; 加热反应混合物; 冷却反应混合物; 并从反应混合物中分离7-（4-溴丁氧基）-3,4-二氢喹诺酮。本发明还包括在反应期间使用相转移催化剂。

89. 发明申请

US20050176794A1 Novel synthesis of irbesartan 审中-公开
标题翻译：厄贝沙坦的新型合成
公开(公告)号：US20050176794A1
公开(公告)日：2005-08-11
申请号：US10621623
申请日：2003-07-16
申请人： Ben-Zion Dolitzky , Gennady Nisnevich , Igor Rukhman , Boris Pertsikov , Julia Kaftanov
发明人： Ben-Zion Dolitzky , Gennady Nisnevich , Igor Rukhman , Boris Pertsikov , Julia Kaftanov
IPC分类号： C07D403/10 , A61K31/41
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：提供使用相转移催化剂的厄贝沙坦的新型合成。还提供了具有细粒度的厄贝沙坦。

90. 发明申请

US20050131027A1 Fine particle size pioglitazone 审中-公开
标题翻译：精细粒径吡格列酮
公开(公告)号：US20050131027A1
公开(公告)日：2005-06-16
申请号：US10508741
申请日：2003-03-21
申请人： Guy Samburski , Ben-Zion Dolitzky
发明人： Guy Samburski , Ben-Zion Dolitzky
IPC分类号： A61K9/00 , A61K9/14 , A61K9/20 , A61K9/48 , A61K31/427 , A61K31/4439 , A61K47/10 , A61K47/12 , A61K47/18 , A61K47/22 , A61K47/26 , A61K47/32 , A61K47/34 , A61K47/36 , A61K47/38 , A61K47/42 , A61K47/44 , A61P3/10 , C07D417/02
CPC分类号： A61K9/0053 , A61K9/0095 , A61K9/14 , A61K9/146 , A61K9/2054 , A61K9/2095 , A61K31/4439
摘要： The present invention provides pioglitazone of defined particle size distribution. The Pioglitazone of defined particle size can be formulated into a wide variety of dosage forms.
摘要翻译：本发明提供了定义的粒度分布的吡格列酮。具有规定粒径的吡格列酮可配制成多种剂型。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式