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1. 发明申请

WO2007062076A2 DEXRAZOXANE FORMULATIONS AND METHODS 审中-公开
标题翻译：异噻唑酮制剂和方法
公开(公告)号：WO2007062076A2
公开(公告)日：2007-05-31
申请号：PCT/US2006045125
申请日：2006-11-20
申请人： NOVARTIS AG , OKHAMAFE AUGUSTUS , HORA MININDER , FAKES DAVID , WEI REBECCA , DANI BHAS , HASHASH AHMAD
发明人： OKHAMAFE AUGUSTUS , HORA MININDER , FAKES DAVID , WEI REBECCA , DANI BHAS , HASHASH AHMAD
IPC分类号： A61K31/495 , A61K9/19 , A61P31/00
CPC分类号： A61K9/0019 , A61K9/19 , A61K31/495
摘要： Improved formulations of dexrazoxane for making injectable solutions in a clinical setting are provided. In some embodiments, high pH formulations are provided to reduce or eliminate pain upon injection. According to various embodiments, dexrazoxane may be formulated as a lyophilized or non-lyophilized acid salt or as a lyophilized or non-lyophilized free base. In some embodiments, dexrazoxane is provided as a sterile dry milled powder of a free base or an isolated acid salt crystal. Formulations that require significantly reduced clinical preparation time are provided. Single-container presentations of unit doses of dexrazoxane are also provided. The formulations of the present invention may be provided in a vial, infusion bottle or infusion bag. In some embodiments, the container may be directly attachable to a diluent-containing container for easy preparation. In other embodiments, diluent may be added directly to the container. Improved methods of manufacturing dexrazoxane that allow greater processing latitude are also provided.
摘要翻译：提供了用于在临床环境中制备可注射溶液的右旋唑烷的改进制剂。在一些实施方案中，提供高pH制剂以减少或消除注射时的疼痛。根据各种实施方案，地塞米松可以配制成冻干或非冻干的酸盐或冻干或非冻干的游离碱。在一些实施方案中，将脱甲硅烷作为游离碱或分离的酸盐晶体的无菌干研磨粉末提供。提供需要显着减少临床准备时间的制剂。还提供了单位剂量的地塞米松的单容器介绍。本发明的制剂可以提供在小瓶，输液瓶或输液袋中。在一些实施方案中，容器可以直接附接到含稀释剂的容器以便于制备。在其它实施方案中，可以将稀释剂直接加入到容器中。还提供了改进的允许更大加工纬度的地塞米松的制造方法。

2. 发明申请

WO2008011154A3 FORMULATIONS FOR BENZIMIDAZOLYL PYRIDYL ETHERS 审中-公开
标题翻译：苯并咪唑基吡啶类化合物的配方
公开(公告)号：WO2008011154A3
公开(公告)日：2008-06-26
申请号：PCT/US2007016469
申请日：2007-07-20
申请人： NOVARTIS AG , HASHASH AHMAD , RITCHIE SEAN , LIN KANGWEN , SHEN PENG , OKHAMAFE AUGUSTUS , GULLAPALLI RAMPURNA
发明人： HASHASH AHMAD , RITCHIE SEAN , LIN KANGWEN , SHEN PENG , OKHAMAFE AUGUSTUS , GULLAPALLI RAMPURNA
IPC分类号： A61K9/107 , A61K31/00 , C07D401/14
CPC分类号： A61K9/1075 , A61K9/107 , A61K9/143 , A61K9/4858
摘要： Formulations are provided, comprising: a compound of Formula (I), a pharmaceutically acceptable salt thereof, or a mixture of any two or more thereof; and an ingredient selected from a hydrophilic solvent, a lipophilic solvent, an emulsifier, or a mixture of any two or more thereof; wherein the compound of Formula (I) is: In some embodiments, the formulations are liquids. In other embodiments, the formulations are solids. Also provided are methods of preparing such formulations.
摘要翻译：提供制剂，其包含：式（I）的化合物，其药学上可接受的盐或其任何两种或多种的混合物; 和选自亲水性溶剂，亲脂性溶剂，乳化剂或其任何两种或更多种的混合物的成分; 其中式（I）的化合物是：在一些实施方案中，制剂是液体。在其它实施方案中，制剂是固体。还提供了制备这种制剂的方法。

3. 发明申请

WO2011028979A1 STABLE SNS-595 COMPOSITIONS AND METHODS OF PREPARATION 审中-公开
标题翻译：稳定的SNS-595组合物和制备方法
公开(公告)号：WO2011028979A1
公开(公告)日：2011-03-10
申请号：PCT/US2010/047776
申请日：2010-09-03
申请人： SUNESIS PHARMACEUTICALS, INC. , SUDHAKAR, Anantha , JACOBS, Jeff , HASHASH, Ahmad , RITCHIE, Sean , CHENG, Hengqin
发明人： SUDHAKAR, Anantha , JACOBS, Jeff , HASHASH, Ahmad , RITCHIE, Sean , CHENG, Hengqin
IPC分类号： C07D417/04 , C07D417/14
CPC分类号： C07D471/04 , A61K31/4375 , C07D417/04 , C07D417/14
摘要： Methods of preparing substantially pure SNS-595 substance are disclosed. Also provided are compositions comprising SNS-595 substance that are substantially pure and essentially free of visible particles.
摘要翻译：公开了制备基本上纯的SNS-595物质的方法。还提供了包含基本上纯的且基本上不含可见颗粒的SNS-595物质的组合物。

4. 发明申请

WO2008027523A3 SALTS OF BENZIMIDAZOLYL PYRIDYL ETHERS AND FORMULATIONS THEREOF 审中-公开
标题翻译：苯并咪唑基吡啶类盐的盐及其制剂
公开(公告)号：WO2008027523A3
公开(公告)日：2008-04-10
申请号：PCT/US2007019152
申请日：2007-08-30
申请人： NOVARTIS AG , GULLAPALLI RAMPURNA , HASHASH AHMAD , KARPINSKI PIOTR H , LIN KANGWEN L , LOESER ERIC M , OKHAMAFE AUGUSTUS O , SUTTON PAUL ALLEN , SY EDUARDO
发明人： GULLAPALLI RAMPURNA , HASHASH AHMAD , KARPINSKI PIOTR H , LIN KANGWEN L , LOESER ERIC M , OKHAMAFE AUGUSTUS O , SUTTON PAUL ALLEN , SY EDUARDO
IPC分类号： C07D401/14 , A61K31/4439 , A61P35/00
CPC分类号： C07D401/14
摘要： Salts of benzimidazolyl pyridyl ethers are provided, particularly salts of { 1 -methyl-5- [2-(5-trifluoromethyl- 1 H-imidazol-2-yl)-pyridin-4-yloxy] - 1 H-benzoimidazol-2-yl } -(4- trifluoromethyl-phenyl)amine. Compositions and formulations including such salts and surfactants as well as methods of preparing such compositions and formulations are provided.
摘要翻译：提供苯并咪唑基吡啶基醚的盐，特别是{1-甲基-5- [2-（5-三氟甲基-1H-咪唑-2-基） - 吡啶-4-基氧基] -1H-苯并咪唑-2-基] 嘧啶-4-基} - （4-三氟甲基 - 苯基）胺。提供了包含此类盐和表面活性剂的组合物和制剂以及制备这种组合物和制剂的方法。

5. 发明申请

WO2007062076A3 DEXRAZOXANE FORMULATIONS AND METHODS 审中-公开
公开(公告)号：WO2007062076A3
公开(公告)日：2007-05-31
申请号：PCT/US2006/045125
申请日：2006-11-20
申请人： NOVARTIS AG , OKHAMAFE, Augustus , HORA, Mininder , FAKES, David , WEI, Rebecca , DANI, Bhas , HASHASH, Ahmad
发明人： OKHAMAFE, Augustus , HORA, Mininder , FAKES, David , WEI, Rebecca , DANI, Bhas , HASHASH, Ahmad
IPC分类号： A61K31/495 , A61K9/19 , A61P31/00
摘要： Improved formulations of dexrazoxane for making injectable solutions in a clinical setting are provided. In some embodiments, high pH formulations are provided to reduce or eliminate pain upon injection. According to various embodiments, dexrazoxane may be formulated as a lyophilized or non-lyophilized acid salt or as a lyophilized or non-lyophilized free base. In some embodiments, dexrazoxane is provided as a sterile dry milled powder of a free base or an isolated acid salt crystal. Formulations that require significantly reduced clinical preparation time are provided. Single-container presentations of unit doses of dexrazoxane are also provided. The formulations of the present invention may be provided in a vial, infusion bottle or infusion bag. In some embodiments, the container may be directly attachable to a diluent-containing container for easy preparation. In other embodiments, diluent may be added directly to the container. Improved methods of manufacturing dexrazoxane that allow greater processing latitude are also provided.

6. 发明申请

WO2008140850A1 SOLID FORMS OF A RAF KINASE INHIBITOR 审中-公开
标题翻译： RAF激酶抑制剂的固体形式
公开(公告)号：WO2008140850A1
公开(公告)日：2008-11-20
申请号：PCT/US2008/055227
申请日：2008-02-28
申请人： NOVARTIS AG , HASHASH, Ahmad , LIN, Kangwen, L. , OKHAMAFE, Augustus, O.
发明人： HASHASH, Ahmad , LIN, Kangwen, L. , OKHAMAFE, Augustus, O.
IPC分类号： C07D401/14 , A61P35/00 , A61K31/4439
CPC分类号： C07D401/14
摘要： The present invention is directed to solid forms of the Raf kinase inhibitor 1-methyl-5-(2-(5-(trifluoromethyl)-1H-imidazol-2-yl)pyridin-4-yloxy)-N-(4-(trifluoromethyl)phenyl)-1H-benzo[d]imidazol-2-amine, as well as compositions thereof and uses of the same.
摘要翻译：本发明涉及Raf激酶抑制剂1-甲基-5-（2-（5-（三氟甲基）-1H-咪唑-2-基）吡啶-4-基氧基）-N-（4-（三氟甲基）苯基）-1H-苯并[d]咪唑-2-胺，及其组合物及其用途。

7. 发明申请

WO2008027523A2 SALTS OF BENZIMIDAZOLYL PYRIDYL ETHERS AND FORMULATIONS THEREOF 审中-公开
标题翻译：苯并咪唑类吡咯烷酮及其制剂的盐
公开(公告)号：WO2008027523A2
公开(公告)日：2008-03-06
申请号：PCT/US2007/019152
申请日：2007-08-30
申请人： NOVARTIS AG , GULLAPALLI, Rampurna , HASHASH, Ahmad , KARPINSKI, Piotr, H. , LIN, Kangwen, L. , LOESER, Eric, M. , OKHAMAFE, Augustus, O. , SUTTON, Paul, Allen , SY, Eduardo
发明人： GULLAPALLI, Rampurna , HASHASH, Ahmad , KARPINSKI, Piotr, H. , LIN, Kangwen, L. , LOESER, Eric, M. , OKHAMAFE, Augustus, O. , SUTTON, Paul, Allen , SY, Eduardo
IPC分类号： C07D401/14 , A61K31/4439 , A61P35/00
CPC分类号： C07D401/14
摘要： Salts of benzimidazolyl pyridyl ethers are provided, particularly salts of { 1 -methyl-5- [2-(5-trifluoromethyl- 1 H-imidazol-2-yl)-pyridin-4-yloxy] - 1 H-benzoimidazol-2-yl } -(4- trifluoromethyl-phenyl)amine. Compositions and formulations including such salts and surfactants as well as methods of preparing such compositions and formulations are provided.
摘要翻译：提供苯并咪唑基吡啶基醚的盐，特别是{1-甲基-5- [2-（5-三氟甲基-1H-咪唑-2-基） - 吡啶-4-基氧基] -1H-苯并咪唑-2-基] （4-三氟甲基 - 苯基）胺。提供了包括这些盐和表面活性剂的组合物和制剂以及制备这种组合物和制剂的方法。

8. 发明申请

WO2008011154A2 FORMULATIONS FOR BENZIMIDAZOLYL PYRIDYL ETHERS 审中-公开
标题翻译： BENZIMIDAZOLYL PYRIDYL ETHERS的制剂
公开(公告)号：WO2008011154A2
公开(公告)日：2008-01-24
申请号：PCT/US2007/016469
申请日：2007-07-20
申请人： NOVARTIS AG , HASHASH, Ahmad , RITCHIE, Sean , LIN, Kangwen , SHEN, Peng , OKHAMAFE, Augustus , GULLAPALLI, Rampurna
发明人： HASHASH, Ahmad , RITCHIE, Sean , LIN, Kangwen , SHEN, Peng , OKHAMAFE, Augustus , GULLAPALLI, Rampurna
IPC分类号： A61K9/107 , A61K31/00
CPC分类号： A61K9/1075 , A61K9/107 , A61K9/143 , A61K9/4858
摘要： Formulations are provided, comprising: a compound of Formula (I), a pharmaceutically acceptable salt thereof, or a mixture of any two or more thereof; and an ingredient selected from a hydrophilic solvent, a lipophilic solvent, an emulsifier, or a mixture of any two or more thereof; wherein the compound of Formula (I) is: In some embodiments, the formulations are liquids. In other embodiments, the formulations are solids. Also provided are methods of preparing such formulations.
摘要翻译：提供制剂，其包含：式（I）的化合物，其药学上可接受的盐或其任何两种或更多种的混合物; 和选自亲水性溶剂，亲脂性溶剂，乳化剂或其任何两种或更多种的混合物的成分; 其中式（I）化合物是：在一些实施方案中，所述制剂是液体。在其他实施方案中，制剂是固体。还提供了制备这种制剂的方法。

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