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51. 发明申请

US20080293970A1 Process for Synthesis of 4-4'-Diamino-Diphenyl-Sulfone 有权
标题翻译：合成4-4'-二氨基 - 二苯基砜的方法
公开(公告)号：US20080293970A1
公开(公告)日：2008-11-27
申请号：US11630760
申请日：2004-07-07
申请人： Marco Villa , Carla De Faveri , Riccardo Zanotti , Francesco Ciardella , Fabrizio Borin
发明人： Marco Villa , Carla De Faveri , Riccardo Zanotti , Francesco Ciardella , Fabrizio Borin
IPC分类号： C07C211/09
CPC分类号： C07C315/04 , C07C315/02 , C07C317/34
摘要： A new process for the preparation and purification of 4-4′-diamino-diphenyl-sulfone (dapsone) is described. The process described is a three step process comprising a condensation reaction with the synthesis of a thioeter intermediate and then steps of oxidation and reduction in suitable conditions in order to obtain a product with good yield and purity.
摘要翻译：描述了制备和纯化4-4'-二氨基 - 二苯基砜（氨苯砜）的新方法。所述方法是三步法，其包括与合成硫代特异中间体的缩合反应，然后在合适的条件下进行氧化和还原的步骤，以获得具有良好产率和纯度的产物。

52. 发明申请

US20080146799A1 Processes for preparing intermediates of pemetrexed 有权
标题翻译：制备培美曲塞中间体的方法
公开(公告)号：US20080146799A1
公开(公告)日：2008-06-19
申请号：US11893233
申请日：2007-08-14
申请人： Nicola Diulgheroff , Moran Pirkes , Alessandro Pontiroli , Marco Villa
发明人： Nicola Diulgheroff , Moran Pirkes , Alessandro Pontiroli , Marco Villa
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Provided are processes for preparing intermediates of pemetrexed.
摘要翻译：提供了制备培美曲塞中间体的方法。

53. 发明申请

US20060276657A1 Process for the preparation of anticancer drugs 失效
标题翻译：抗癌药物的制备工艺
公开(公告)号：US20060276657A1
公开(公告)日：2006-12-07
申请号：US11400639
申请日：2006-04-06
申请人： Marco Villa , Roberta Fretta , Nicola Diulgheroff , Alessandro Pontiroli
发明人： Marco Villa , Roberta Fretta , Nicola Diulgheroff , Alessandro Pontiroli
IPC分类号： C07D249/08
CPC分类号： C07D249/08
摘要： A process for preparing Anastrozole is provided. In the process the steps of a. combining 3,5-bis (2-cyanoisopropyl)toluene, a solvent selected from the group consisting of acetonitrile, dichloromethane and chlorobenzene, a brominating reagent selected from a group consisting of N-bromosuccinimide and 1,3-dibromo-5,5-dimethylhydantoin, and 2,2′-azobis(2-methylpropionitrile); b. heating; c. combining with 1,2,4-triazole, a solvent selected from a group consisting of N-methylpyrrolidine, dimethylformamide, mixtures of NMP and DMF, dimethylsulfoxide, mixtures of DMSO and toluene, acetone, ACN, and tetrahydrofuran, a base selected from a group consisting of NaOH, KOH, K2CO3, and Na2CO3, and 1,3-benzendiacetonitrile-5-(bromomethyl)-α,α,{acute over (α)},{acute over (α)}-tetramethyl, at a temperature below −20° C. are performed.
摘要翻译：提供了一种制备阿那曲唑的方法。在这个过程中，a。结合3,5-双（2-氰基异丙基）甲苯，选自乙腈，二氯甲烷和氯苯的溶剂，选自N-溴代琥珀酰亚胺和1,3-二溴-5,5-二氯苯的溴化试剂，二甲基乙内酰脲和2,2'-偶氮双（2-甲基丙腈）; b。加热; C。与1,2,4-三唑组合，选自N-甲基吡咯烷，二甲基甲酰胺，NMP和DMF的混合物，二甲基亚砜，DMSO和甲苯的混合物，丙酮，ACN和四氢呋喃的溶剂，选自由NaOH，KOH，K 2 CO 3 3和Na 2 CO 3 3组成的组和1,3 - 苄基乙腈-5-（溴甲基）-α，α，α，α-四甲基，在低于-20℃的温度下进行。

54. 发明授权

US06271375B1 Ortho-metalation process for the synthesis of 2-substituted-1-(tetrazol-5-yl)benzenes 失效
标题翻译：用于合成2-取代-1-（四唑-5-基）苯的正金属化方法
公开(公告)号：US06271375B1
公开(公告)日：2001-08-07
申请号：US09445470
申请日：2000-04-27
申请人： Marco Villa , Pietro Allegrini , Katiuscia Arrighi , Maurizio Paiocchi
发明人： Marco Villa , Pietro Allegrini , Katiuscia Arrighi , Maurizio Paiocchi
IPC分类号： C07D47100
CPC分类号： C07D471/04 , C07F3/02
摘要： A process of direct metalation of phenyltetrazoles useful for preparing compounds of formula (II) intermediates for the synthesis of angiotensin II antagonists is described.
摘要翻译：描述了可用于制备式（II）化合物用于合成血管紧张素II拮抗剂的中间体的苯基四唑的直接金属化方法。

55. 发明授权

US06187936B1 Process for the enzymatic kinetic resolution of 3-phenylglycidates by transesterification with aminoalcohols 失效
标题翻译：通过与氨基醇进行酯交换的3-苯基缩水甘油酯的酶动力学拆分方法
公开(公告)号：US06187936B1
公开(公告)日：2001-02-13
申请号：US09399962
申请日：1999-09-20
申请人： Marco Villa , Dario Tentorio , Angelo Restelli , Sergio Riva
发明人： Marco Villa , Dario Tentorio , Angelo Restelli , Sergio Riva
IPC分类号： C07D30340
CPC分类号： C12P41/005 , C12P17/02
摘要： A process for the preparation of I: in which R and R1 have the meanings reported in the description, that comprises the enzymatic kinetic resolution by transesterification with aminoalcohols of 3-phenylglycidates of formula I: is described.
摘要翻译：描述了制备I的方法：其中R和R 1具有在描述中报道的含义，其包括通过与式I的3-苯基缩水甘油的氨基醇进行酯交换的酶动力学拆分。

56. 发明授权

US6100425A Process for the preparation of an intermediate useful in the synthesis of iodinated contrast media 失效
标题翻译：用于制备可用于合成碘化造影剂的中间体的方法
公开(公告)号：US6100425A
公开(公告)日：2000-08-08
申请号：US995153
申请日：1997-12-19
申请人： Marco Villa , Maurizio Paiocchi
发明人： Marco Villa , Maurizio Paiocchi
IPC分类号： C07C231/02 , C07C67/02
CPC分类号： C07C231/02
摘要： A process for the preparation of the compound L-5-(2-acetoxypropionylamino)-2,4,6-triiodoisophthaloyl dichloride by reacting 5-amino-2,4,6-triiodoisophthaloyl dichloride with L-2-acetoxypropionyl chloride in N,N-dimethylacetamide as a solvent, characterized in that a catalytic amount of a lower alcohol is added to the reaction mixture.
摘要翻译：通过使5-氨基-2,4,6-三碘邻苯二甲酰氯与N-1中的L-2-乙酰氧基丙酰氯反应制备化合物L-5-（2-乙酰氧基丙酰基氨基）-2,4,6-三碘间苯二酰氯的方法， N-二甲基乙酰胺作为溶剂，其特征在于向反应混合物中加入催化量的低级醇。

57. 发明授权

US5580993A Process for the preparation of iopamidol and 5-amino-2,2-dialkyl-1,3-dioxanes 失效
标题翻译：碘帕醇和5-氨基-2,2-二烷基-1,3-二恶烷的制备方法
公开(公告)号：US5580993A
公开(公告)日：1996-12-03
申请号：US304178
申请日：1994-09-12
申请人： Marco Villa , Antonio Nardi
发明人： Marco Villa , Antonio Nardi
IPC分类号： C07D233/66 , C07D319/06 , C07D319/08 , C07D233/67
CPC分类号： C07D319/06
摘要： A process for the preparation of Iopamidol and 5-amino-2,2-dialkyl-1,3-dioxanes of formula ##STR1## wherein R and R.sub.1 are the same or different and represent a straight or branched C.sub.1 and C.sub.2 alkyl group or together with the carbon atom to which they are bonded, form a C.sub.5 -C.sub.6 cycloaliphatic ring; comprising the transformation of a 2,2-dialkyl-1,3-dioxane-5-carboxylic acid ester of formula ##STR2## wherein R.sub.2 represents a straight or branched C.sub.1 -C.sub.2 alkyl group, a phenyl optionally substituted by nitro groups or a benzyl; by treatment with ammonia into the corresponding amides and the subsequent rearrangement of the latter into the compounds of formula I, by treatment with a hypohalogenite. The resultant ketals may be used as is, or be converted to 2-amino-1,3-propanediol, and reacted with 5-amino-2,4,6-triiodo-isophthalic acid dichloride or, alternatively,L-5-(2-acetoxy-propionylamino)-2,4,6-triido-isophthalic acid dichloride, to produce Iopamidol.
摘要翻译：制备式I（I）的Iopamidol和5-氨基-2,2-二烷基-1,3-二恶烷的方法，其中R和R 1相同或不同并且表示直链或支链C 1和C 2烷基或与它们所键合的碳原子一起形成C5-C6脂环族环; 包括转化式（II）的2,2-二烷基-1,3-二恶烷-5-羧酸酯，其中R 2表示直链或支链C 1 -C 2烷基，任选被硝基取代的苯基或苄基; 通过用氨处理成相应的酰胺，随后通过用次卤酸盐处理将后者重排成式I化合物。所得的缩酮可原样使用，或转化为2-氨基-1,3-丙二醇，并与5-氨基-2,4,6-三碘 - 间苯二甲酸二氯化物反应，或与L-5- 2-乙酰氧基 - 丙酰基氨基）-2,4,6-三苯基间苯二甲酸二氯化物，以制备Iopamidol。

58. 发明申请

US20130306848A1 Assembly for Monitoring Output Characteristics of a Modulator 有权
标题翻译：监控调制器输出特性的组件
公开(公告)号：US20130306848A1
公开(公告)日：2013-11-21
申请号：US13991868
申请日：2011-12-06
申请人： Flavio Dell'Orto , Giuseppe Cusmai , Stefano Balsamo , Marco Villa
发明人： Flavio Dell'Orto , Giuseppe Cusmai , Stefano Balsamo , Marco Villa
IPC分类号： G02F1/225
CPC分类号： G02F1/225 , G02F1/2255 , G02F2001/212 , G02F2201/122
摘要： A photonic assembly is described. The assembly comprises a substrate. An optical modulator (100) in or on the substrate has an output port coupled to an output waveguide (106) mounted in or on the substrate. A spiller waveguide (107, 108) is mounted in or on the substrate. The spiller waveguide (107, 108) has an input end (109, 110) physically separated from but proximate to the output waveguide (106) so as to collect light spilt from the output port or output waveguide (106). The modulator (106) may be a MZI modulator.
摘要翻译：描述了光子组件。组件包括基底。衬底中或衬底上的光学调制器（100）具有耦合到安装在衬底中或衬底上的输出波导（106）的输出端口。垃圾波导（107,108）安装在基板中或基板上。垃圾波导（107,108）具有与输出波导（106）物理分离但接近输出波导（106）的输入端（109,110），以便收集从输出端口或输出波导（106）溢出的光。调制器（106）可以是MZI调制器。

59. 发明申请

US20100099888A1 Process for the preparation of anticancer drugs 审中-公开
标题翻译：抗癌药物的制备工艺
公开(公告)号：US20100099888A1
公开(公告)日：2010-04-22
申请号：US12592066
申请日：2009-11-17
申请人： Marco Villa , Roberta Fretta , Nicola Diulgheroff , Alessandro Pontiroli
发明人： Marco Villa , Roberta Fretta , Nicola Diulgheroff , Alessandro Pontiroli
IPC分类号： C07D249/08
CPC分类号： C07D249/08
摘要： A process for preparing Anastrozole is provided. In the process the steps of a. combining 3,5-bis(2-cyanoisopropyl)toluene, a solvent selected from the group consisting of acetonitrile, dichloromethane and chlorobenzene, a brominating reagent selected from a group consisting of N-bromosuccinimide and 1,3-dibromo-5,5-dimethylhydantoin, and 2,2′-azobis(2-methylpropionitrile); b. heating; c. combining with 1,2,4-triazole, a solvent selected from a group consisting of N-methylpyrrolidine, dimethylformamide, mixtures of NMP and DMF, dimethylsulfoxide, mixtures of DMSO and toluene, acetone, ACN, and tetrahydrofuran, a base selected from a group consisting of NaOH, KOH, K2CO3, and Na2CO3, and 1,3-benzendiacetonitrile-5-(bromomethyl)-α,α,{acute over (α)},{acute over (α)}-tetramethyl, at a temperature below −20° C. are performed.
摘要翻译：提供了一种制备阿那曲唑的方法。在这个过程中，a。结合3,5-双（2-氰基异丙基）甲苯，选自乙腈，二氯甲烷和氯苯的溶剂，选自N-溴代琥珀酰亚胺和1,3-二溴-5,5-二氯苯的溴化试剂，二甲基乙内酰脲和2,2'-偶氮双（2-甲基丙腈）; b。加热; C。与1,2,4-三唑结合，选自N-甲基吡咯烷，二甲基甲酰胺，NMP和DMF的混合物，二甲基亚砜，DMSO和甲苯的混合物，丙酮，ACN和四氢呋喃的溶剂，选自由NaOH，KOH，K 2 CO 3和Na 2 CO 3组成的组，和1,3-苯撑二乙腈-5-（溴甲基）-α，α，（急性（α）}，{急（α）} - 低于-20℃。

60. 发明申请

US20070004653A1 Stable lyophilized anthracycline glycosides 审中-公开
标题翻译：稳定的冻干蒽环类苷
公开(公告)号：US20070004653A1
公开(公告)日：2007-01-04
申请号：US11433026
申请日：2006-05-11
申请人： Roberto Arosio , Marco Villa , Simonetta Amati
发明人： Roberto Arosio , Marco Villa , Simonetta Amati
IPC分类号： A61K31/7048
CPC分类号： A61K9/19 , A61K31/704 , A61K31/7048 , A61K47/12 , A61K47/34
摘要： The present invention provides lyophilized and stable lyophilized anthracycline glycoside salts, in particular, the hydrochloride salt. Also, the present invention provides methods of stabilizing these anthracycline glycoside salts, and methods for producing stable lyophilized anthracycline glycoside salts, such as for example the antineoplastic compound idarubicin hydrochloride, or the compounds doxorubicin hydrochloride, and epirubicin hydrochloride.
摘要翻译：本发明提供冻干和稳定的冻干蒽环苷糖苷盐，特别是盐酸盐。此外，本发明提供了稳定这些蒽环苷类糖苷盐的方法，以及用于制备稳定的冻干蒽环苷类糖苷盐的方法，例如抗肿瘤化合物盐酸伊多比星，或盐酸多柔比星化合物和盐酸表柔比星。

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