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1. 发明申请

US20060035872A1 Process for the preparation of 3-oximino steroids 审中-公开
标题翻译： 3-肟基类固醇的制备方法
公开(公告)号：US20060035872A1
公开(公告)日：2006-02-16
申请号：US11202191
申请日：2005-08-12
申请人： Marco Villa , Roberta Fretta , Nicola Diulgheroff
发明人： Marco Villa , Roberta Fretta , Nicola Diulgheroff
IPC分类号： A61K31/56 , C07J41/00
CPC分类号： C07J41/00 , C07J41/0016
摘要： The present invention provides a method of preparing norelgestromin or norgestimate by reacting the corresponding 3-oxosteroid precursor with hydroxylamine HCl and a base to obtain a reaction mixture forming norelgestromin or norgestimate; monitoring the anti/syn ratio of the norelgestromin or norgestimate produced in the reaction mixture; adding a base to the reaction mixture to neutralize acidity in the reaction mixture when a desired anti/syn ratio is detected; and isolating the norelgestromin or norgestimate. The present invention also provides a process allowing a control of the formation of the anti isomer and syn isomer of norelgestromin or norgestimate by reacting the corresponding 3-oxosteroid precursor with hydroxylamine HCl and a base to obtain a reaction mixture forming norelgestromin or norgestimate; regulating the acidity of the reaction mixture to adjust the anti/syn ratio of the norelgestromin or norgestimate produced in the reaction mixture; adding a base to the reaction mixture to neutralize acidity in the reaction mixture when a desired anti/syn ratio is detected; and isolating the norelgestromin or norgestimate.
摘要翻译：本发明提供了通过使相应的3-氧代甾体前体与羟胺HCl和碱反应来制备诺美孕酮或诺孕酯的方法，以获得形成诺美孕酮或诺孕酯的反应混合物; 监测反应混合物中产生的去甲孕酮或诺孕酯的抗/顺应比; 当检测到所需的抗/顺式比时，向反应混合物中加入碱以中和反应混合物中的酸度; 并分离去甲孕酮或诺孕酯。本发明还提供一种方法，其通过使相应的3-氧代甾体前体与羟胺HCl和碱反应以获得形成去甲孕激素或诺孕酯的反应混合物，从而控制去甲孕酮或诺孕酯的抗异构体和顺式异构体的形成; 调节反应混合物的酸度以调节反应混合物中产生的诺美辛溴或诺孕酯的抗/顺比; 当检测到所需的抗/顺式比时，向反应混合物中加入碱以中和反应混合物中的酸度; 并分离去甲孕酮或诺孕酯。

2. 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℃。

3. 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。

4. 发明授权

US07692025B2 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：US07692025B2
公开(公告)日：2010-04-06
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-methylpyrrolidinone, 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-甲基吡咯烷酮，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℃。

5. 发明申请

US20060047108A1 Synthesis of idarubicin aglycone 审中-公开
标题翻译：伊达比星糖苷配基的合成
公开(公告)号：US20060047108A1
公开(公告)日：2006-03-02
申请号：US11210605
申请日：2005-08-23
申请人： Marco Villa , Roberto Arosio , Roberta Fretta , Nicola Diulgheroff
发明人： Marco Villa , Roberto Arosio , Roberta Fretta , Nicola Diulgheroff
IPC分类号： C07H15/24 , C07C46/00
CPC分类号： C07C50/38 , C07C46/00 , C07C2603/44
摘要： The present invention provides a new method of producing high quality idarubicin aglycone from 4-protected demethoxydaunomycinones such as 4-demethoxydaunomycinone-4-triflate.
摘要翻译：本发明提供了一种从4-保护的脱甲氧基多霉素酮如4-脱氧山梨醇酮-4-三氟甲磺酸盐生产高品质伊达比星苷元的新方法。

6. 发明申请

US20080139810A1 Processes for the preparation of lyophilized pharmaceutically acceptable salts of pemetrexed diacid 有权
标题翻译：制备培美曲塞二酸的冻干药学上可接受的盐的方法
公开(公告)号：US20080139810A1
公开(公告)日：2008-06-12
申请号：US11893234
申请日：2007-08-14
申请人： Jonathan Busolli , Nicola Diulgheroff , Moran Pirkes , Alessandro Pontiroli , Marco Villa
发明人： Jonathan Busolli , 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 the preparation of lyophilized pharmaceutically acceptable salts of pemetrexed diacid, in particular, pemetrexed disodium salt, directly from pemetrexed diacid or salts thereof, i.e., without isolating the obtained pemetrexed salt prior to lyophilizing it.
摘要翻译：本发明提供了培美曲塞二酸的冻干药学上可接受的盐，特别是培美曲塞二钠盐的制备方法，其直接来自培美曲塞二酸或其盐，即在将其冻干之前不分离得到的培美曲塞盐。

7. 发明授权

US08088919B2 Crystalline forms of pemetrexed diacid and processes for the preparation thereof 有权
标题翻译：培美曲塞二酸的结晶形式及其制备方法
公开(公告)号：US08088919B2
公开(公告)日：2012-01-03
申请号：US11893212
申请日：2007-08-14
申请人： Jonathan Busolli , Nicola Diulgheroff , Csilla Nemethne Racz , Moran Pirkes , Alessandro Pontiroli , Marco Villa , Judith Aronhime
发明人： Jonathan Busolli , Nicola Diulgheroff , Csilla Nemethne Racz , Moran Pirkes , Alessandro Pontiroli , Marco Villa , Judith Aronhime
IPC分类号： C07D487/04 , A61K31/519
CPC分类号： C07D487/04
摘要： Provided are crystalline forms of N-[4-[2-(2-amino-4,7-dihydro-4-oxo-1H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-L-glutamic acid, pemetrexed diacid, and processes for the preparation thereof.
摘要翻译：提供的是N- [4- [2-（2-氨基-4,7-二氢-4-氧代-1H-吡咯并[2,3-d]嘧啶-5-基）乙基]苯甲酰基] -L- 谷氨酸，培美曲塞二酸及其制备方法。

8. 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。

9. 发明授权

US09156841B2 Crystalline forms of pemetrexed diacid and processes for the preparation thereof 有权
标题翻译：培美曲塞二酸的结晶形式及其制备方法
公开(公告)号：US09156841B2
公开(公告)日：2015-10-13
申请号：US13070432
申请日：2011-03-23
申请人： Jonathan Busolli , Nicola Diulgheroff , Csilla Nemethne Racz , Moran Pirkes , Alessandro Pontiroli , Marco Villa , Judith Aronhime
发明人： Jonathan Busolli , Nicola Diulgheroff , Csilla Nemethne Racz , Moran Pirkes , Alessandro Pontiroli , Marco Villa , Judith Aronhime
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Provided are crystalline forms of N-[4-[2-(2-amino-4,7-dihydro-4-oxo-1H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-L-glutamic acid, pemetrexed diacid, and processes for the preparation thereof.
摘要翻译：提供的是N- [4- [2-（2-氨基-4,7-二氢-4-氧代-1H-吡咯并[2,3-d]嘧啶-5-基）乙基]苯甲酰基] -L- 谷氨酸，培美曲塞二酸及其制备方法。

10. 发明授权

US08629152B2 Processes for the preparation of lyophilized pharmaceutically acceptable salts of pemetrexed diacid 有权
标题翻译：制备培美曲塞二酸的冻干药学上可接受的盐的方法
公开(公告)号：US08629152B2
公开(公告)日：2014-01-14
申请号：US11893234
申请日：2007-08-14
申请人： Jonathan Busolli , Nicola Diulgheroff , Moran Pirkes , Alessandro Pontiroli , Marco Villa , Zvi Harel
发明人： Jonathan Busolli , Nicola Diulgheroff , Moran Pirkes , Alessandro Pontiroli , Marco Villa , Zvi Harel
IPC分类号： A61K31/519 , C07D487/04
CPC分类号： C07D487/04
摘要： Provided are processes for the preparation of lyophilized pharmaceutically acceptable salts of pemetrexed diacid, in particular, pemetrexed disodium salt, directly from pemetrexed diacid or salts thereof, i.e., without isolating the obtained pemetrexed salt prior to lyophilizing it.
摘要翻译：本发明提供了培美曲塞二酸的冻干药学上可接受的盐，特别是培美曲塞二钠盐的制备方法，其直接来自培美曲塞二酸或其盐，即在将其冻干之前不分离得到的培美曲塞盐。

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