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1. 发明公开

EP1957497A2 PROCESSES FOR PREPARING INTERMEDIATES OF PEMETREXED 有权
标题翻译：用于生产中间产品从培美曲塞
公开(公告)号：EP1957497A2
公开(公告)日：2008-08-20
申请号：EP07811336.2
申请日：2007-08-14
申请人： Sicor, Inc.
发明人： DIULGHEROFF, Nicola , PIRKES, Moran , PONTIROLI, Alessandro , VILLA, Marco
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The invention provides intermediates of pemetrexed of formula VI and processes for the preparation thereof.

2. 发明公开

EP1934226A2 HIGHLY PURE PEMETREXED DIACID AND PROCESSES FOR THE PREPARATION THEREOF 审中-公开
标题翻译：高纯度和方法，培美曲塞二酸及其
公开(公告)号：EP1934226A2
公开(公告)日：2008-06-25
申请号：EP07836878.4
申请日：2007-08-14
申请人： Sicor, Inc.
发明人： DIULGHEROFF, Nicola , PIRKES, Moran , PONTIROLI, Alessandro , VILLA, Marco , BUSOLLI, Jonathan , CASALONE, Roberto
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , C07B2200/13
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]ben-zoyl]-L-glutamic acid, pemetrexed diacid, and processes for the preparation thereof.

3. 发明公开

EP1778716A1 PROCESS FOR THE PREPARATION OF 3-OXIMINO STEROIDS 审中-公开
标题翻译：工艺制备3-肟类固醇
公开(公告)号：EP1778716A1
公开(公告)日：2007-05-02
申请号：EP05788984.2
申请日：2005-08-12
申请人： Sicor Inc.
发明人： VILLA, Marco , FRETTA, Roberta , DIULGHEROFF, Nicola
IPC分类号： 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.

4. 发明授权

EP1957497B1 PROCESSES FOR PREPARING INTERMEDIATES OF PEMETREXED 有权
标题翻译：用于生产中间产品从培美曲塞
公开(公告)号：EP1957497B1
公开(公告)日：2015-09-30
申请号：EP07811336.2
申请日：2007-08-14
申请人： Sicor, Inc.
发明人： DIULGHEROFF, Nicola , PIRKES, Moran , PONTIROLI, Alessandro , VILLA, Marco
IPC分类号： C07D487/04
CPC分类号： C07D487/04

5. 发明授权

EP1943252B1 PROCESSES FOR THE PREPARATION OF LYOPHILIZED PHARMACEUTICALLY ACCEPTABLE SALTS OF PEMETREXED DIACID 有权
标题翻译： PROCESS FOR产生亲脂性的药学上可接受的盐OFF培美曲塞二酸
公开(公告)号：EP1943252B1
公开(公告)日：2010-12-22
申请号：EP07836879.2
申请日：2007-08-14
申请人： Sicor, Inc.
发明人： BUSOLLI, Jonathan , DIULGHEROFF, Nicola , NEMETHNE RACZ, Csilla , PIRKES, Moran , PONTIROLI, Alessandro , VILLA, Marco , HAREL, Zvi
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.

6. 发明公开

EP2057182A2 A PROCESS FOR PREPARING DROSPIRENONE AND INTERMEDIATE THEREOF 审中-公开
标题翻译：用于生产屈螺酮及其中间体
公开(公告)号：EP2057182A2
公开(公告)日：2009-05-13
申请号：EP08767495.8
申请日：2008-05-01
申请人： Sicor, Inc.
发明人： PONTIROLI, Alessandro , DIULGHEROFF, Nicola , SCARPITTA, Francesca , AROSIO, Roberto , VILLA, Marco , POGGIALI, Andrea
IPC分类号： C07J53/00
CPC分类号： C07J53/008
摘要： The present invention encompasses processes for preparing drospirenone and intermediates thereof.

7. 发明授权

EP1869035B2 NOVEL CRYSTALLINE FORM OF TIOTROPIUM BROMIDE AND PROCESS FOR PREPARATION THEREOF 有权
标题翻译：新的结晶噻托溴铵形式和方法及其
公开(公告)号：EP1869035B2
公开(公告)日：2015-08-12
申请号：EP06847887.4
申请日：2006-12-19
申请人： Sicor, Inc.
发明人： DIULGHEROFF, Nicola , SCARPITTA, Francesca , PONTIROLI, Alessandro , KOVACSNE-MEZEI, Adrienne , ARONHIME, Judith , JEGOROV, Alexandr
IPC分类号： C07D451/10 , A61K31/46 , A61P11/06
CPC分类号： C07D451/12 , C07D451/10

8. 发明授权

EP1945645B1 CRYSTALLINE FORMS OF PEMETREXED DIACID AND PROCESSES FOR THE PREPARATION THEREOF 有权
标题翻译：培美曲塞二酸及其方法晶形
公开(公告)号：EP1945645B1
公开(公告)日：2010-12-01
申请号：EP07836867.7
申请日：2007-08-14
申请人： Sicor, Inc.
发明人： BUSOLLI, Jonathan , DIULGHEROFF, Nicola , NEMETHNE, RACZ, Csilla , PIRKES, Moran , PONTIROLI, Alessandro , VILLA, Marco , ARONHIME, Judith
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.

9. 发明公开

EP1966196A2 PURE AND STABLE TIOTROPIUM BROMIDE 审中-公开
标题翻译： PURE和安全的噻托溴铵
公开(公告)号：EP1966196A2
公开(公告)日：2008-09-10
申请号：EP06845924.7
申请日：2006-12-19
申请人： Sicor, Inc.
发明人： VOLONTÈ, Roberta , DIULGHEROFF, Nicola , SCARPITTA, Francesca , PONTIROLI, Alessandro , CASALONE, Roberto
IPC分类号： C07D451/10 , A61K31/46 , A61P11/06
CPC分类号： C07D451/10
摘要： This invention relates to solvates of tiotropium bromide having a purity of at least 99%, process for preparing such pure solvates, and their use in pharmaceutical, formulations. This invention also provides tiotropium bromide solvates containing less than about 0.15% area by HPLC of 2,2-dithienyl glycolic acid.

10. 发明授权

EP1781589B1 SYNTHESIS OF IDARUBIN AGLYCONE 有权
标题翻译： SYNTHESE VON IDARUBIN-AGLYCON
公开(公告)号：EP1781589B1
公开(公告)日：2010-04-14
申请号：EP05791316.2
申请日：2005-08-23
申请人： Sicor Inc.
发明人： VILLA, Marco , AROSIO, Roberto , FRETTA, Roberta , DIULGHEROFF, Nicola
IPC分类号： C07C46/00 , C07C50/38
CPC分类号： C07C50/38 , C07C46/00 , C07C2603/44

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