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31. 发明申请

US20120053191A1 OXIDATED DERIVATIVES OF TRIAZOLYLPURINES USEFUL AS LIGANDS OF THE ADENOSINE A2A RECEPTOR AND THEIR USE AS MEDICAMENTS 有权
标题翻译：作为腺苷A2A受体的配体及其作为药物使用的三唑来膦的氧化衍生物有用
公开(公告)号：US20120053191A1
公开(公告)日：2012-03-01
申请号：US13257750
申请日：2010-03-18
申请人： Walter Cabri , Patrizia Minetti , Giovanni Piersanti , Giorgio Tarzia
发明人： Walter Cabri , Patrizia Minetti , Giovanni Piersanti , Giorgio Tarzia
IPC分类号： A61K31/52 , A61P3/00 , A61P25/28 , A61P25/14 , C07D473/34 , A61P25/16
CPC分类号： C07D473/34 , A61K31/198 , A61K31/52
摘要： The present invention relates to new triazolyl purine derivatives of formula (I), processes for their preparation, and to pharmaceutical compositions containing them for the treatment of neurological disorders or cerebral ischaemia for which inhibition of adenosine A2A receptor will result at improving the health state of a patient.
摘要翻译：本发明涉及式（I）的新的三唑基嘌呤衍生物，其制备方法和含有它们的药物组合物，用于治疗神经障碍或脑缺血，其中腺苷A2A受体的抑制将导致改善健康状态病人。

32. 发明申请

US20110137026A1 Crystalline (6r,7r)-7--3- [(R)-1'-Tert-Butoxycarbonyl-2-Oxo-[1,3']Bipyrrolidinyl-(3e)-Ylidenemethyl]-8-Oxo-5-Thia-1-Aza-Bicyclo[4.2.0] Oct-2-Ene-2-Carboxylic Acid Benzhydryl Ester; Its Manufacture and Use 有权
标题翻译：结晶（6r，7r）-7- 3 - [（R）-1'-叔丁氧羰基-2-氧代 - [1,3']联吡咯烷基 - （3e） - 亚甲基甲基] -8-氧代-5-硫杂 -1-氮杂 - 双环[4.2.0]十二-2-烯-2-羧酸二苯甲酯; 其制造和使用
公开(公告)号：US20110137026A1
公开(公告)日：2011-06-09
申请号：US12937607
申请日：2009-04-14
申请人： Marco Alpegiani , Walter Cabri , Markus Heubes , Davide Longoni , Michael Schleimer
发明人： Marco Alpegiani , Walter Cabri , Markus Heubes , Davide Longoni , Michael Schleimer
IPC分类号： C07D501/60 , C07D501/12
CPC分类号： C07D501/12 , C07D501/54
摘要： A solid DMSO solvate of a compound of formula (I) is described, which is a useful intermediate for preparing the broad spectrum antibiotics Ceftobiprole and Ceftobiprole Medocaril.
摘要翻译：描述了式（I）化合物的固体DMSO溶剂化物，其是制备广谱抗生素头孢匹双和头孢匹双酸甲酯的有用中间体。

33. 发明申请

US20100324003A1 AMINOOXIME DERIVATIVES OF 2- AND/OR 4-SUBSTITUTED ANDROSTANES AND ANDROSTENES AS MEDICAMENTS FOR CARDIOVASCULAR DISORDERS 失效
标题翻译： 2-和/或4-取代的安慰剂和安慰剂作为心血管疾病药物的氨基酸衍生物
公开(公告)号：US20100324003A1
公开(公告)日：2010-12-23
申请号：US12680988
申请日：2008-09-18
申请人： Alberto Cerri , Giuseppe Bianchi , Giorgio Fedrizzi , Patrizia Ferrari , Mauro Gobbini , Giuseppe Marazzi , Marco Torri , Walter Cabri
发明人： Alberto Cerri , Giuseppe Bianchi , Giorgio Fedrizzi , Patrizia Ferrari , Mauro Gobbini , Giuseppe Marazzi , Marco Torri , Walter Cabri
IPC分类号： A61K31/58 , C07J41/00 , C07J43/00 , C07J71/00 , C07J53/00 , A61K31/5685 , A61P9/12 , A61P9/00
CPC分类号： C07J41/0016 , C07J43/003
摘要： New aminooxime derivatives at position 3 of 2- and/or 4-substituted androstanes and androstenes, processes for their preparation, and to pharmaceutical compositions containing them for the treatment of cardiovascular disorders, such as heart failure and hypertension. In particular compounds having the general formula (I) are described, where the radicals have the meanings described in detail in the application.
摘要翻译： 2-和/或4-取代的雄甾烷和雄甾烯-3的位置3上的新的氨基肟衍生物，其制备方法以及含有它们用于治疗心力衰竭和高血压的心血管疾病的药物组合物。特别地描述了具有通式（I）的化合物，其中基团具有本申请中详细描述的含义。

34. 发明申请

US20090239893A1 STEREOSELECTIVE PROCESS AND CRYSTALLINE FORMS OF A CAMPTOTHECIN 有权
标题翻译：角蛋白的选择性方法和结晶形式
公开(公告)号：US20090239893A1
公开(公告)日：2009-09-24
申请号：US11721282
申请日：2005-12-16
申请人： Paolo Carminati , Maria Ornella Tinti , Mauro Marzi , Fabrizio Giorgi , Walter Cabri , Marco Alpegiani , Domenico Vergani , Paolo Ghetti
发明人： Paolo Carminati , Maria Ornella Tinti , Mauro Marzi , Fabrizio Giorgi , Walter Cabri , Marco Alpegiani , Domenico Vergani , Paolo Ghetti
IPC分类号： A61K31/4375 , C07D491/22 , A61P35/00
CPC分类号： C07D491/22
摘要： A stereoselective process for preparing 7-[(E)-t-butyloxyiminomethyl]-camptothecin (also known as gimatecan) is herein disclosed. With the addition of further dissolution and precipitation steps carried out in appropriate different solvent mixtures, four new crystalline forms of gimatecan are also obtainable by using the same stereoselective process.
摘要翻译：本文公开了制备7 - [（E） - 叔丁氧基亚氨基甲基] - 喜树碱（也称为gimatecan）的立体选择性方法。随着在合适的不同溶剂混合物中进一步溶解和沉淀步骤的添加，也可以通过使用相同的立体选择性方法获得四种新的结晶形式的gimatecan。

35. 发明申请

US20080160586A1 Process for the Purification of Tacrolimus 审中-公开
标题翻译：他克莫司净化方法
公开(公告)号：US20080160586A1
公开(公告)日：2008-07-03
申请号：US11718415
申请日：2005-10-24
申请人： Walter Cabri , Paolo Paissoni , Jacopo Roletto , Luca Morra
发明人： Walter Cabri , Paolo Paissoni , Jacopo Roletto , Luca Morra
IPC分类号： C12P17/16
CPC分类号： C07D498/18 , B01D15/322 , B01D15/325 , G01N30/461
摘要： A process for the purification and recovery of Tacrolimus (I) (17-allyl-1,14-dihydroxy-12-[2-(4-hydroxy-3-methoxycyclohexyl)-1-methyvinyl]-23,25- dimethoxy-13,19,21,27-tetramethyl-11,28-dioxi-4-azatricyclo-[22.3.1.04.9]octacos-18-en-2,3,10,16-tetraone), starting from Streptomyces sp fermentation broth. The process is particularly advantageous in terms of productivity and selectivity of the separation of impurities.
摘要翻译：一种纯化和回收他克莫司（I）（17-烯丙基-1,14-二羟基-12- [2-（4-羟基-3-甲氧基环己基）-1-甲基乙烯基] -23,25-二甲氧基-13 ，19,21,27-四甲基-11,28-二氧杂-4-氮杂三环[22.3.1.0]二十八-18-烯-2,3,10,16-四酮），起始来自链霉菌sp发酵液。该方法在分离杂质的生产率和选择性方面是特别有利的。

36. 发明申请

US20080033169A1 Crystalline Form Of Cefdinir Ammonium Salt As An Intermediate For The Preparation Of Pure Cefdinir 审中-公开
标题翻译：头孢地尼铵盐作为纯头孢地尼的制备中间体的结晶形式
公开(公告)号：US20080033169A1
公开(公告)日：2008-02-07
申请号：US11719599
申请日：2005-10-24
申请人： Giovanni Pozzi , Paolo Ghetti , Gaetano Balsamo , Marco Alpegiani , Walter Cabri
发明人： Giovanni Pozzi , Paolo Ghetti , Gaetano Balsamo , Marco Alpegiani , Walter Cabri
IPC分类号： C07D279/04
CPC分类号： C07D501/00
摘要： The invention relates to crystalline Cefdinir ammonium salt of formula (I) and to a process for the preparation thereof. This salt is particularly advantageous in that it allows to prepare highly pure Cefdinir.
摘要翻译：本发明涉及式（I）的结晶头孢地尼铵盐及其制备方法。这种盐是特别有利的，因为它允许制备高纯度的头孢地尼。

37. 发明授权

US07252965B2 Method of production of β-carotene by fermentation in mixed culture using (+) and (−) strains of Blakeslea trispora 有权
标题翻译：（+）和（ - ）菌株的混合培养中通过发酵生产β-胡萝卜素的方法
公开(公告)号：US07252965B2
公开(公告)日：2007-08-07
申请号：US10469190
申请日：2003-01-23
申请人： Javier Costa Perez , Ana Teresa Marcos Rodríguez , Juan Luis De La Fuente Moreno , Marta Rodríguez Saiz , Bruno Diez Garcia , Enrique Peiro Cezon , Walter Cabri , José Luis Barredo Fuente
发明人： Javier Costa Perez , Ana Teresa Marcos Rodríguez , Juan Luis De La Fuente Moreno , Marta Rodríguez Saiz , Bruno Diez Garcia , Enrique Peiro Cezon , Walter Cabri , José Luis Barredo Fuente
IPC分类号： C12P23/00
CPC分类号： C12P23/00
摘要： The invention consists of fermenting selected strains of Blakeslea trispora in conditions such that β-carotene is produced in the form of stabilized preparations with residual contents of other carotenoids (γ-carotene and β-zeacarotene). The fermentation conditions chosen include the programmed addition of oxygen and/or β-ionone during fermentation, and control of the age of the vegetative growth phases of the strains employed. The β-carotene obtained can be used in the pharmaceutical and food sectors.
摘要翻译：本发明包括在使β-胡萝卜素以其它类胡萝卜素（γ-胡萝卜素和β-玉米胡萝卜素）的残留物含量稳定的制剂形式产生的条件下发酵所选择的三倍体布鲁氏菌菌株。选择的发酵条件包括在发酵过程中编程加入氧和/或β-紫罗兰酮，并控制所用菌株的营养生长期的年龄。获得的β-胡萝卜素可用于制药和食品行业。

38. 发明授权

US07173126B2 Crystalline cefdinir salts 失效
标题翻译：结晶头孢地尼盐
公开(公告)号：US07173126B2
公开(公告)日：2007-02-06
申请号：US10539122
申请日：2003-12-01
申请人： Giovanni Pozzi , Patricio Martin Gomez , Marco Alpegiani , Walter Cabri
发明人： Giovanni Pozzi , Patricio Martin Gomez , Marco Alpegiani , Walter Cabri
IPC分类号： C07D501/22
CPC分类号： C07D501/22
摘要： Cefdinir crystalline salts of formula (I), in which n ranges from 1 to 3, the preparation and use thereof for the preparation and purification of cefdinir are herein disclosed. The salts of formula (I) can be obtained from cefdinir intermediates or crude cefdinir by treatment with phosphoric acid.
摘要翻译：本文公开了其中n为1至3的式（I）的头孢地尼结晶盐，其制备和用于头孢地尼的制备和纯化的制备和用途。式（I）的盐可以通过用磷酸处理从头孢地尼中间体或粗头孢地尼得到。

39. 发明申请

US20060111566A1 Intermediate cefdinir salts 失效
标题翻译：中间头孢地尼盐
公开(公告)号：US20060111566A1
公开(公告)日：2006-05-25
申请号：US10529649
申请日：2003-09-26
申请人： Giovanni Pozzi , Patricio Martinez Gomez , Marco Alpegiani , Walter Cabri
发明人： Giovanni Pozzi , Patricio Martinez Gomez , Marco Alpegiani , Walter Cabri
IPC分类号： C07D501/00
CPC分类号： C07D501/00 , Y02P20/55
摘要： Disclosed are salts of the general formula (I) wherein R1, R2 and as defined in the description and a process for the preparation thereof. These salts are useful intermediates for the preparation of cefdinir.
摘要翻译：公开了通式（I）的盐，其中R 1，R 2和如说明书中所定义的盐及其制备方法。这些盐是制备头孢地尼的有用中间体。

40. 发明授权

US06458558B1 Process for the preparation of &bgr;-lactam derivatives 失效
标题翻译：制备β-内酰胺衍生物的方法
公开(公告)号：US06458558B1
公开(公告)日：2002-10-01
申请号：US09979164
申请日：2002-02-11
申请人： Enrico Siviero , Walter Cabri , Daniele Mario Terrassan
发明人： Enrico Siviero , Walter Cabri , Daniele Mario Terrassan
IPC分类号： C12P3500
CPC分类号： C12P35/02 , C07D501/00
摘要： A process for the preparation of Cefuroxime acid (I), which comprises the following steps: (1) Extraction of deacetyl 7-glutaryl ACA (II) aqueous solution at acid pH with organic solvents (for example according to the procedures disclosed in U.S. Pat. No. 5,801,241); (2) drying the resulting solution while preventing lactonization of the intermediate; (3) carbamoylation of the hydroxymethyl group at the 3-position by reaction with chlorosulfonyl isocyanate or similar products; (7) extraction of the carbamoyl derivative from step 3 with water at neutral pH; (8) enzymatic hydrolysis of the amide at the 7-position of the cephalosporanic ring with glutaryl acylase; (6) acylation of the amnino group by condensation with 2-furanyl(sin-methoxyimino)acetic acid chloride or mixed anhydride.
摘要翻译：一种制备头孢呋辛酸（I）的方法，其包括以下步骤：（1）在酸性pH下用有机溶剂萃取脱乙酰基-7-戊二酰ACA（II）水溶液（例如根据US Pat 。5,801,241号）; （2）干燥所得溶液同时防止中间体的内酯化; （3）通过与氯磺酰基异氰酸酯或类似产物的反应在3-位羟基甲基的氨基甲酰基化; （7）在中性pH下用水萃取步骤3的氨基甲酰基衍生物; （8）用戊二酰基酰化酶在头孢菌素环的7-位酶水解酰胺; （6）通过与2-呋喃基（正 - 甲氧基亚氨基）乙酰氯或混合酸酐缩合来酰胺化氨基。

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