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：US07388096B2

公开(公告)日：2008-06-17

申请号：US11235519

申请日：2005-09-26

申请人： Margaret M. Gleeson ,  Gary McGeorge ,  Bang-Chi Chen ,  Huiping Zhang ,  Mary F. Malley ,  John D. DiMarco ,  Denette K. Murphy ,  Xiaotian Yin ,  Steven R. Fabian ,  Jasmine M. Gupta

发明人： Margaret M. Gleeson ,  Gary McGeorge ,  Bang-Chi Chen ,  Huiping Zhang ,  Mary F. Malley ,  John D. DiMarco ,  Denette K. Murphy ,  Xiaotian Yin ,  Steven R. Fabian ,  Jasmine M. Gupta

IPC分类号： C07D471/02 ,  C07D491/02 ,  C07D498/02 ,  C07D513/02 ,  C07D515/02

CPC分类号： C07D471/04

摘要： The instant invention provides crystalline forms of 1-(3-chlorophenyl)-7-oxo-6-[4-(2-oxo-1 (2H)pyridinyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide and its solvates thereof; processes for the production of such crystalline forms; pharmaceutical compositions comprising such crystalline forms; and methods of treating thromboembolic disorders with such crystalline forms or such pharmaceutical compositions.

摘要翻译： 本发明提供1-（3-氯苯基）-7-氧代-6- [4-（2-氧代-1（2H）吡啶基）苯基] -4,5,6,7-四氢-1H- 吡唑并[3,4-c]吡啶-3-甲酰胺及其溶剂化物; 生产这种结晶形式的方法; 包含这种结晶形式的药物组合物; 以及用这种结晶形式或这种药物组合物治疗血栓栓塞障碍的方法。

公开(公告)号：US20060140821A1

公开(公告)日：2006-06-29

申请号：US11300851

申请日：2005-12-15

申请人： Victor Rosso ,  Anne Song ,  John Venit ,  Xiaotian Yin

发明人： Victor Rosso ,  Anne Song ,  John Venit ,  Xiaotian Yin

IPC分类号： B01L9/00

CPC分类号： G01N23/20025 ,  B01L3/5085 ,  B01L2300/0829 ,  B01L2300/12

摘要： A laboratory sample plate for use in PXRD and other testing techniques includes a quartz body having substantially planar top and bottom surfaces that are parallel with each other. The quartz body includes a matrix of cylindrical apertures that are substantially perpendicular to the top and bottom surfaces. Each aperture has an upper opening at the top surface and a lower opening at the bottom surface of the plate body. A synthetic quartz bottom sheet is fused to the bottom surface of the quartz body. The quartz bottom sheet include respective portions that close the lower opening of each aperture in the quartz body, such that each aperture and respective portion of the bottom sheet together form a well for receiving a sample. Each aperture and respective portion of the bottom sheet are suitably dimensioned to perform a powder X-ray diffraction technique as well as microscopy and Raman spectroscopy on a sample contained in the well.

摘要翻译： 用于PXRD和其他测试技术的实验室样品板包括具有彼此平行的基本平坦的顶部和底部表面的石英体。 石英体包括基本上垂直于顶表面和底表面的圆柱形孔的矩阵。 每个孔在顶表面具有上开口和在板体的底表面处的下开口。 合成石英底片与石英体的底面融合。 石英底片包括关闭石英体中每个孔的下开口的相应部分，使得每个孔和底片的相应部分一起形成用于接收样品的孔。 每个孔和底部片的相应部分适当地确定尺寸以对包含在该孔中的样品进行粉末X射线衍射技术以及显微镜和拉曼光谱。

公开(公告)号：US20060069118A1

公开(公告)日：2006-03-30

申请号：US11235519

申请日：2005-09-26

申请人： Margaret Gleeson ,  Gary McGeorge ,  Bang-Chi Chen ,  Huiping Zhang ,  Mary Malley ,  John DiMarco ,  Denette Murphy ,  Xiaotian Yin ,  Steven Fabian ,  Jasmine Gupta

发明人： Margaret Gleeson ,  Gary McGeorge ,  Bang-Chi Chen ,  Huiping Zhang ,  Mary Malley ,  John DiMarco ,  Denette Murphy ,  Xiaotian Yin ,  Steven Fabian ,  Jasmine Gupta

IPC分类号： C07D471/02 ,  A61K31/4745

CPC分类号： C07D471/04

摘要： The instant invention provides crystalline forms of 1-(3-chlorophenyl)-7-oxo-6-[4-(2-oxo-1 (2H)pyridinyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide and its solvates thereof; processes for the production of such crystalline forms; pharmaceutical compositions comprising such crystalline forms; and methods of treating thromboembolic disorders with such crystalline forms or such pharmaceutical compositions.

摘要翻译： 本发明提供1-（3-氯苯基）-7-氧代-6- [4-（2-氧代-1（2H）吡啶基）苯基] -4,5,6,7-四氢-1H- 吡唑并[3,4-c]吡啶-3-甲酰胺及其溶剂化物; 生产这种结晶形式的方法; 包含这种结晶形式的药物组合物; 以及用这种结晶形式或这种药物组合物治疗血栓栓塞障碍的方法。

公开(公告)号：US20130039989A1

公开(公告)日：2013-02-14

申请号：US13643561

申请日：2011-04-29

申请人： Dilbir S. Bindra ,  Yeshwant Gokhale ,  Cletus John Nunes ,  Victor W. Rosso ,  Gretchen M. Schroeder ,  Ajit B. Thakur ,  Xiaotian Yin

发明人： Dilbir S. Bindra ,  Yeshwant Gokhale ,  Cletus John Nunes ,  Victor W. Rosso ,  Gretchen M. Schroeder ,  Ajit B. Thakur ,  Xiaotian Yin

IPC分类号： A61K31/444 ,  A61P35/00 ,  C07D401/12 ,  A61K9/14

CPC分类号： C07D401/12 ,  C07D213/82

摘要： Disclosed are salts and crystalline forms of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide and salts thereof. Also disclosed are at least one pharmaceutical composition comprising at least one crystalline form of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide, at least one method of using at least one crystalline form of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide to treat cancer and/or other proliferative diseases, and processes to prepare crystalline forms of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide and salts thereof.