公开(公告)号：US20060128726A1

公开(公告)日：2006-06-15

申请号：US11283651

申请日：2005-11-21

申请人： Xuebao Wang ,  Chiajen Lai ,  Nachimuthu Soundararajan ,  Nina Nguyen ,  Weiming Ying ,  Lori Burton ,  Rajesh Gandhi ,  Krishnaswamy Raghavan ,  Ronald West ,  Yuji Zhou ,  Lin Yan ,  Xiaotian Yin ,  John DiMarco ,  Jack Gougoutas

发明人： Xuebao Wang ,  Chiajen Lai ,  Nachimuthu Soundararajan ,  Nina Nguyen ,  Weiming Ying ,  Lori Burton ,  Rajesh Gandhi ,  Krishnaswamy Raghavan ,  Ronald West ,  Yuji Zhou ,  Lin Yan ,  Xiaotian Yin ,  John DiMarco ,  Jack Gougoutas

IPC分类号： A61K31/519 ,  C07D487/04

CPC分类号： C07D487/04

摘要： A process is provided for preparing novel crystalline forms, namely selectively and consistently preparing the H2-1 dihydrate crystalline form, the H2-2 dihydrate crystalline form, the N-3 anhydrate crystalline form and the MTBE solvate crystalline form of the IKur compound (2S)-1-[[(7R)-7-(3,4-dichlorophenyl)-4,7-dihydro-5-methylpyrazolo[1,5]pyrimidine-6-yl]carbonyl]-2-(4-fluorophenyl)pyrrolidine. The process includes preparation of the H2-1 and H2-2 forms which are used in preparing the N-3 anhydrate form which is particularly stable and has suitable flow properties and desired particle size. Novel H2-1 dihydrate and H2-2 dihydrate forms, the N-3 anhydrate form and the MTBE solvate form of the above IKur compound, pharmaceutical compositions containing such novel forms and a method for preventing or treating arrhythmias including atrial fibrillation and IKur related conditions employing such novel forms are also provided.

摘要翻译： 提供了一种制备新型结晶形式的方法，即选择性和一致地制备H 2 - II二水合物结晶形式，H2-2二水合物结晶形式，N-3无水物结晶形式和IKEA化合物（2S ）-1 - [[（7R）-7-（3,4-二氯苯基）-4,7-二氢-5-甲基吡唑并[1,5]嘧啶-6-基]羰基] -2-（4-氟苯基） 吡咯烷。 该方法包括制备用于制备N-3无水物形式的H2-1和H2-2形式，其特别稳定并具有合适的流动性能和所需的粒度。 新型H2-1二水合物和H2-2二水合物形成上述IKur化合物的N-3无水物形式和MTBE溶剂化物形式，含有这种新型形式的药物组合物和用于预防或治疗包括心房颤动和IKur相关病症的心律失常的方法 也提供了这种新颖的形式。

公开(公告)号：US20060013836A1

公开(公告)日：2006-01-19

申请号：US11226017

申请日：2005-09-14

申请人： Rebanta Bandyopadhyay ,  Timothy Malloy ,  Andrea Panaggio ,  Krishnaswamy Raghavan ,  Sailesh Varia

发明人： Rebanta Bandyopadhyay ,  Timothy Malloy ,  Andrea Panaggio ,  Krishnaswamy Raghavan ,  Sailesh Varia

IPC分类号： A61K31/427 ,  A61K9/00

CPC分类号： C07D491/044 ,  A61K9/0019 ,  A61K9/0095 ,  A61K9/19 ,  A61K31/395 ,  A61K31/425 ,  A61K31/427 ,  A61K47/10 ,  A61K47/44 ,  A61K2300/00

摘要： A process for formulating certain epothilone analogs for parenteral administration is disclosed wherein the analog is dissolved in a mixture of at least 50% by volume tertiary-butanol in water, the mixture is lyophilized, the resulting lyophilized product is packaged in one vial with a sufficient amount of solvent comprising anhydrous ethanol and a suitable nonionic surfactant in a second vial. All steps are carried out with protection from light. In use, the contents of the second or diluent vial are added to the lyophilized product and mixed to constitute the epothilone analog and the resulting solution is diluted with a suitable diluent to produce a solution for intravenous injection containing the epothilone analog in a concentration of from about 0.1 mg/mL to about 0.9 mg/mL. A preferred surfactant is polyethoxylated castor oil and a preferred diluent is Lactated Ringer's Injection.

公开(公告)号：US20050054716A1

公开(公告)日：2005-03-10

申请号：US10704401

申请日：2003-11-07

申请人： Uday Gogate ,  Deborah Piperno ,  Robert Perrone ,  Krishnaswamy Raghavan

发明人： Uday Gogate ,  Deborah Piperno ,  Robert Perrone ,  Krishnaswamy Raghavan

IPC分类号： A61K9/00 ,  A61K31/337 ,  A61K47/10 ,  A61K47/44

CPC分类号： A61K31/337 ,  A61K9/0019 ,  A61K47/10 ,  A61K47/44

摘要： The present invention relates to a novel intravenous formulation for a taxane chemotherapeutic agent. The agent is formulated with ethanol, polyoxyethylated castor oil and a mixture of antioxidants to prevent oxidation of the drug substance caused by the polyoxyethylated castor oil.

摘要翻译： 本发明涉及紫杉烷化疗剂的新型静脉内制剂。 该试剂与乙醇，聚氧乙烯蓖麻油和抗氧化剂的混合物配制，以防止由聚氧乙基蓖麻油引起的药物物质的氧化。