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1. 发明授权

US06897339B2 Process for the production of high purity iohexol 有权
标题翻译：生产高纯度碘海醇的方法
公开(公告)号：US06897339B2
公开(公告)日：2005-05-24
申请号：US10474535
申请日：2002-04-09
申请人： Stefano Turchetta , Pietro Massardo , Valentina Aromatario
发明人： Stefano Turchetta , Pietro Massardo , Valentina Aromatario
IPC分类号： C07C231/16 , C07C231/24 , C07C237/46 , C07C233/05 , C07C233/64
CPC分类号： C07C231/24 , C07C237/46
摘要： Purification process of iohexol comprising the treatment of said product with 1-methoxy-2-propanol either alone or mixed with other solvents.
摘要翻译：包括用1-甲氧基-2-丙醇单独处理所述产物或与其它溶剂混合的碘海醇的纯化方法。

2. 发明授权

US08236817B2 Polymorphs of 1-cyclopropy1-7-([s,s])-2,8-diazadicyclo[4.3.0]non-8-yl)-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinoline carboxylic acid hydrochloride and methods for the preparation thereof 有权
标题翻译： 1-环丙基] -7 - （[s，s]）-2,8-二氮杂双环[4.3.0]壬-8-基）-6-氟-1,4-二氢-8-甲氧基-4-氧代 -3-喹啉羧酸盐酸盐及其制备方法
公开(公告)号：US08236817B2
公开(公告)日：2012-08-07
申请号：US10580173
申请日：2004-10-28
申请人： Stefano Turchetta , Pietro Massardo , Valentina Aromatario
发明人： Stefano Turchetta , Pietro Massardo , Valentina Aromatario
IPC分类号： A61K31/47 , C07D471/04
CPC分类号： C07D471/04
摘要： Two novel crystalline forms, designated form A and form B of the antibacterial agent 1-cyclopropyl-7-(S,S)-2,8-diazabicyclo[4.3.0]non-8-yl)-6-fluoro-1,4-dihydro-8-methoxy -4-oxo-3-quinoline carboxylic acid hydrochloride of formula, the preparation thereof, and their pharmaceutical compositions are described. These crystalline forms, which are characterized by greater ability and ease of preparation and of formulation, can be produced by industrially applicable methods which comprises the steps of: a) suspending 1-cyclopropyl-7-(S,S)-2,8-diazabicyclo-[4.3.0]non-8-yl)-6-fluoro-1,4-dihydro -8-methoxy-4-oxo-3-quinoline carboxylic acid hydrochloride in a solvent selected from an alcohol and a polyalcohol, b) heating the mixture under reflux, c) cooling, d) isolating the product which is separated, (form A) and, additionally, e), reslurrying the solid at reflux in a solvent selected from alcohols and polyols or mixtures thereof, in which the resulting mixture has an overall water content of between 2.5% and 0.01% by weight, f) isolating the product (form B).
摘要翻译：两种新颖的结晶形式，称为抗菌剂1-环丙基-7-（S，S）-2,8-二氮杂双环[4.3.0]壬-8-基）-6-氟-1,2-的形式A和形式B，描述了下式的4-二氢-8-甲氧基-4-氧代-3-喹啉羧酸盐酸盐及其药物组合物。其特征在于具有更大的制备能力和制备容易性的结晶形式可以通过工业上可应用的方法制备，其包括以下步骤：a）将1-环丙基-7-（S，S）-2,8- 二氮杂双环[4.3.0]壬-8-基）-6-氟-1,4-二氢-8-甲氧基-4-氧代-3-喹啉羧酸盐酸盐在选自醇和多元醇的溶剂中，b ）在回流下加热混合物，c）冷却，d）分离分离的产物（形式A），另外e）分离固体，在选自醇和多元醇或其混合物的溶剂中回流固化，其中所得混合物的总含水量为2.5重量％至0.01重量％，f）分离产物（B型）。

3. 发明申请

US20050014798A1 Polymorphous forms of rosiglitazone maleate 审中-公开
标题翻译：马来酸罗格列酮的多形态
公开(公告)号：US20050014798A1
公开(公告)日：2005-01-20
申请号：US10826868
申请日：2004-04-16
申请人： Stefano Turchetta , Pietro Massardo , Valentina Aromatario
发明人： Stefano Turchetta , Pietro Massardo , Valentina Aromatario
IPC分类号： A61P43/00 , C07D417/12 , C07D417/02 , A61K31/4439
CPC分类号： C07D417/12
摘要： Two new polymorphous crystalline forms of rosiglitazone maleate, termed respectively form I and II, and the methods for selectively obtaining each form are described and characterized. Rosiglitazone maleate may be obtained in the form of the single polymorph I by blending an approximately equimolar mixture of rosiglitazone base and maleic acid in a series of solvents and mixtures thereof which comprises isopropanol, acetone, ethyl acetate, isopropyl acetate, followed by cooling of the mixture to ambient temperature; the form II may on the other hand be obtained by means of treatment of the approximately equimolar mixture of rosiglitazone base and maleic acid in water under reflux, followed by cooling of the mixture to ambient temperature
摘要翻译：描述和表征了两种称为分别形成I和II的罗格列酮马来酸盐的新型多形态结晶形式和选择性地获得各种形式的方法。马来酸罗格列酮可以通过在一系列溶剂及其混合物中混合罗格列酮碱和马来酸的近似等摩尔混合物，其中包括异丙醇，丙酮，乙酸乙酯，乙酸异丙酯，然后冷却混合至环境温度; 另一方面，形式II可以通过在回流下处理罗格列酮碱和马来酸的大约等摩尔混合物在水中，然后将混合物冷却至环境温度

4. 发明申请

US20070072895A1 Polymorphs of 1-cyclopropyl-7-([s,s])-2,8-diazadicyclo[4.3.0]non-8-yl)-6-fluoro-1,4-dihydro -8-methoxy-4-oxo-3-quinoline carboxylic acid hydrochloride and methods for the preparation thereof 有权
标题翻译： 1-环丙基-7 - （[s，s]）-2,8-二氮杂双环[4.3.0]壬-8-基）-6-氟-1,4-二氢-8-甲氧基-4-氧代 -3-喹啉羧酸盐酸盐及其制备方法
公开(公告)号：US20070072895A1
公开(公告)日：2007-03-29
申请号：US10580173
申请日：2004-10-28
申请人： Stefano Turchetta , Pietro Massardo , Valentina Aromatario
发明人： Stefano Turchetta , Pietro Massardo , Valentina Aromatario
IPC分类号： C07D471/02 , A61K31/4745
CPC分类号： C07D471/04
摘要： Two novel crystalline forms, designated form A and form B of the antibacterial agent 1-cyclopropyl-7-([S,S])-2,8-diazadicyclo[4.3.0]non-8-yl)-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinoline carboxylic acid hydrochloride of formula, the preparation thereof, and their pharmaceutical compositions are described. These crystalline forms, which are characterized by greater stability and ease of preparation and of formulation, can be produced by industrially applicable methods which comprises the steps of: a) suspending 1-cyclopropyl-7-([S,S])-2,8-diazadicyclo-[4.3.0]non-8-yl)-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinoline carboxylic acid hydrochloride in a solvent selected from an alcohol and a polyalcohol, b) heating the mixture under reflux, p1 c) cooling, d) isolating the product which is separated, (form A) and, additionally, e) reslurrying the solid at reflux in a solvent selected from alcohols and polyols or mixtures thereof, in which the resulting mixture has an overall water content of between 2.5% and 0.01% by weight, f) isolating the product (form B).
摘要翻译：抗菌剂1-环丙基-7-（[S，S]）-2,8-二氮杂双环[4.3.0]壬-8-基）-6-氟 - 异喹啉的两种新型结晶形式A和B形式描述了式的1,4-二氢-8-甲氧基-4-氧代-3-喹啉羧酸盐酸盐及其药物组合物。其特征在于具有更好的稳定性和易于制备和配制的这些结晶形式可以通过工业上可应用的方法制备，其包括以下步骤：a）将1-环丙基-7 - （[S，S]） - -8-氮杂-8-氮杂-8-氮杂-8-甲氧基-4-氧代-3-喹啉羧酸盐酸盐在选自醇和多元醇的溶剂中反应 b）在回流下加热混合物，p1 c）冷却，d）分离分离的产物（形式A），另外e）在选自醇和多元醇或其混合物的溶剂中回流下将固体再浆化，其中所得混合物的总含水量为2.5重量％至0.01重量％，f）分离产物（B型）。

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