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81. 发明申请

WO2007075838A3 PURE AND STABLE TIOTROPIUM BROMIDE 审中-公开
标题翻译：纯和稳定的生物化学品
公开(公告)号：WO2007075838A3
公开(公告)日：2007-08-16
申请号：PCT/US2006048690
申请日：2006-12-19
申请人： SICOR INC , VOLONTE ROBERTA , DIULGHEROFF NICOLA , SCARPITTA FRANCESCA , PONTIROLI ALESSANDRO , CASALONE ROBERTO
发明人： VOLONTE 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.
摘要翻译：本发明涉及纯度至少为99％的噻托溴铵的溶剂化物，制备这种纯溶剂化物的方法及其在药物制剂中的用途。本发明还提供了通过HPLC对2,2-二噻烷基乙醇酸含有小于约0.15％面积的噻托溴铵溶剂化物。

82. 发明申请

WO2007044950A2 CRYSTALLINE FORMS OF DOCETAXEL AND PROCESSES FOR THEIR PREPARATION 审中-公开
标题翻译： DOCETAXEL的结晶形式及其制备方法
公开(公告)号：WO2007044950A2
公开(公告)日：2007-04-19
申请号：PCT/US2006/040308
申请日：2006-10-12
申请人： SICOR, INC. , PONTIROLI, Alessandro , VILLA, Marco , ARONHIME, Judith , LEVI, Sigalit
发明人： PONTIROLI, Alessandro , VILLA, Marco , ARONHIME, Judith , LEVI, Sigalit
CPC分类号： C07D305/14
摘要： Novel forms of crystalline docetaxel are provided, as well as pharmaceutical compositions, and methods of treatment. Novel processes for making crystalline docetaxel are also provided.
摘要翻译：提供结晶多西他赛的新型形式，以及药物组合物和治疗方法。还提供了制备结晶多西紫杉醇的新方法。

83. 发明申请

WO2006108155A2 PROCESS FOR THE PREPARATION OF ANTICANCER DRUGS 审中-公开
标题翻译：制备抗生素药物的方法
公开(公告)号：WO2006108155A2
公开(公告)日：2006-10-12
申请号：PCT/US2006/013140
申请日：2006-04-06
申请人： SICOR, INC. , VILLA, Marco , FRETTA, Roberta , DIULGHEROFF, Nicola , PONTIROLI, Alessandro
发明人： VILLA, Marco , FRETTA, Roberta , DIULGHEROFF, Nicola , PONTIROLI, Alessandro
IPC分类号： C07D249/08 , A61K31/4196 , A61P35/00
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 l,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 l,3-benzendiacetonitrile-5- (bromomethyl)-α, 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）; 湾加热; 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，选自在低于-20℃的温度下进行由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）-a，a，¬-四甲基。

84. 发明申请

WO2006079090A3 PROCESS FOR THE PREPARATION OF FENOLDOPAM MESYLATE 审中-公开
公开(公告)号：WO2006079090A3
公开(公告)日：2006-07-27
申请号：PCT/US2006/002571
申请日：2006-01-24
申请人： SICOR INC. , BIGATTI, Ettore , ROSSETTO, Pierluigi , MACDONALD, Peter, Lindsay
发明人： BIGATTI, Ettore , ROSSETTO, Pierluigi , MACDONALD, Peter, Lindsay
IPC分类号： C07C213/00 , C07C221/00 , C07C225/06 , C07D223/16
摘要： Methods and inteπnediates for the preparation of Fenoldopam mesylate and ntermediates thereof are provided.

85. 发明申请

WO2006024016A2 SYNTHESIS OF IDARUBIN AGLYCONE 审中-公开
标题翻译： IDARUBIN AGLYCONE的合成
公开(公告)号：WO2006024016A2
公开(公告)日：2006-03-02
申请号：PCT/US2005/030298
申请日：2005-08-23
申请人： SICOR, INC. , VILLA, Marco , AROSIO, Roberto , FRETTA, Roberta , DIULGHEROFF, Nicola
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
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。

86. 发明申请

WO2006020885A1 PROCESS FOR THE PREPARATION OF 3-OXIMINO STEROIDS 审中-公开
标题翻译：制备3-OXIMINO STEROIDS的方法
公开(公告)号：WO2006020885A1
公开(公告)日：2006-02-23
申请号：PCT/US2005/028769
申请日：2005-08-12
申请人： SICOR, INC. , VILLA, Marco , FRETTA, Roberta , DIULGHEROFF, Nicola
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.
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/顺反比; 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。

87. 发明申请

WO2006015081A2 A PROCESS FOR THE PREPARATION OF 7a-ALKYLATED 19-NORSTEROIDS 审中-公开
标题翻译：一种制备7a-烷基化的19-核黄素的方法
公开(公告)号：WO2006015081A2
公开(公告)日：2006-02-09
申请号：PCT/US2005026715
申请日：2005-07-27
申请人： SICOR INC , MACDONALD PETER LINDSAY , BIGATTI ETTORE , ROSSETTO PIERLUIGI
发明人： MACDONALD PETER LINDSAY , BIGATTI ETTORE , ROSSETTO PIERLUIGI
IPC分类号： C07J5/00
CPC分类号： C07J1/00 , C07J1/007 , C07J1/0074 , C07J31/006 , C07J41/0072
摘要： Processes useful in the preparation of pharmaceutical compounds such as fulvestrant and processes for the preparation of fulvestrant.
摘要翻译：可用于制备药物化合物如氟维司群的方法和用于制备氟维司群的方法。

88. 发明申请

WO2003099007A1 AQUEOUS FLUDARABINE PHOSPHATE COMPOSITION 审中-公开
标题翻译：水溶性磷酸氢盐组合物
公开(公告)号：WO2003099007A1
公开(公告)日：2003-12-04
申请号：PCT/US2003/016395
申请日：2003-05-23
申请人： SICOR INC. , MIREJOVSKY, Dorla , MACDONALD, Peter, Lindsay
发明人： MIREJOVSKY, Dorla , MACDONALD, Peter, Lindsay
IPC分类号： A01N43/04
CPC分类号： A61K9/0095 , A61K9/0019 , A61K9/0048 , A61K31/70 , A61K31/7076 , A61K47/02 , A61K47/26
摘要： This invention is directed towards a ready-to-use aqueous composition of fludarabine phosphate. In one embodiment, the invention is directed to an aqueous fludarabine phosphate composition which comprises fludarabine phosphate, a base, and water. The concentration of fludarabine phosphate in the composition may be between about 0.5 mg/mL and about 50 mg/mL. The pH of the composition may be between about 5.5 and about 7.1.
摘要翻译：本发明涉及磷酸氟达拉滨的即用型水性组合物。在一个实施方案中，本发明涉及磷酸氟阿拉伯磷酸盐组合物，其包含氟达拉滨磷酸盐，碱和水。组合物中氟达拉滨磷酸盐的浓度可以在约0.5mg / mL至约50mg / mL之间。组合物的pH可以在约5.5至约7.1之间。

89. 发明申请

WO2003051297A3 AQUEOUS IFOSFAMIDE COMPOSITION 审中-公开
公开(公告)号：WO2003051297A3
公开(公告)日：2003-06-26
申请号：PCT/US2002/039851
申请日：2002-12-13
申请人： SICOR INC. , MIREJOVSKY, Dorla , BURKHART, Michael
发明人： MIREJOVSKY, Dorla , BURKHART, Michael
IPC分类号： A61K31/535
摘要： ABSTRACTThis invention is directed towards a ready-to-use aqueous composition of ifosfamide. In one embodiment, the invention is directed to an aqueous ifosfamide composition which comprises ifosfamide, a pharmaceutically acceptable buffer, and water. The concentration of ifosfamide in the composition may be between about 40 mM and about 400 mM. The concentration of buffer in the composition may be between about 10 mM and about 260 mM. The molar ratio of ifosfamide to buffer may be between about 0.5:1 to about 20:1. The pH of the composition may be between about 4 and about 8.

90. 发明申请

WO2010017374A1 PROCESS FOR PREPARING AZACYTIDINE INTERMEDIATE 审中-公开
标题翻译：制备AZACYTIDINE中间体的方法
公开(公告)号：WO2010017374A1
公开(公告)日：2010-02-11
申请号：PCT/US2009/052983
申请日：2009-08-06
申请人： SICOR INC. , BIGATTI, Ettore , LUX, Giovanna , PAIOCCHI, Maurizio , GIOLITO, Andrea , TOSI, Simone
发明人： BIGATTI, Ettore , LUX, Giovanna , PAIOCCHI, Maurizio , GIOLITO, Andrea , TOSI, Simone
IPC分类号： C07H19/12 , C07H1/00 , A61K31/706
CPC分类号： C07H1/00 , C07H19/12 , Y10T436/147777
摘要： The present invention provides a processes for preparing 5 -Azacytidine, and intermediates thereof, said process Comprising reacting a silylated 5-azacytosine of the formula (II), a sugar moiety having of the formula (III): and a protic acid; wherein R is a substituted or non substituted C 1 -C 20 acyl moiety, R 1 , R 2 and R 3 are each independently H or an alkyl group, and X is a halogen. The present invention further provides an analytical method for determining the purity of 5-Azacytidine in a sample.
摘要翻译：本发明提供了制备5-氨基胞苷及其中间体的方法，所述方法包括使式（II）的甲硅烷基化5-氮杂胞嘧啶，具有式（III）的糖部分与质子酸反应; 其中R是取代或未取代的C 1 -C 20酰基部分，R 1，R 2和R 3各自独立地为H或烷基，X为卤素。本发明还提供了一种用于测定样品中5-氮杂胞苷的纯度的分析方法。

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