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公开(公告)号：US20110201795A1
公开(公告)日：2011-08-18
申请号：US13093430
申请日：2011-04-25
申请人： Prashant P. Deshpande , Bruce A. Ellsworth , Janak Singh , Theodor W. Denzel , Chiajen Lai , Gerard Crispino , Michael E. Randazzo , Jack Z. Gougoutas
发明人： Prashant P. Deshpande , Bruce A. Ellsworth , Janak Singh , Theodor W. Denzel , Chiajen Lai , Gerard Crispino , Michael E. Randazzo , Jack Z. Gougoutas
CPC分类号： C07H23/00 , C07H5/04 , C07H5/06 , C07H7/00 , C07H15/207
摘要： Method for the production of C-aryl glucoside SGLT2 inhibitors useful for the treatment of diabetes and related diseases. and intermediates thereof. The C-aryl glucosides may be complexed with amino acid complex forming reagents.
摘要翻译： 生产用于治疗糖尿病和相关疾病的C-芳基葡萄糖苷SGLT2抑制剂的方法。 及其中间体。 C-芳基葡糖苷可以与形成氨基酸复合物的试剂络合。
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![Process for preparing novel crystalline forms of (2S)-1-[[(7R)-7-(3,4-dichlorophenyl)-4,7-dihydro-5-methylpyrazolo[1,5]pyrimidine-6-yl]carbonyl]-2-(4-fluorophenyl)pyrrolidine, novel stable forms produced therein and formulations](/abs-image/US/2006/06/15/US20060128726A1/abs.jpg.150x150.jpg)
2.发明申请Process for preparing novel crystalline forms of (2S)-1-[[(7R)-7-(3,4-dichlorophenyl)-4,7-dihydro-5-methylpyrazolo[1,5]pyrimidine-6-yl]carbonyl]-2-(4-fluorophenyl)pyrrolidine, novel stable forms produced therein and formulations 审中-公开制备（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]羰基的新结晶形式的方法 ] -2-（4-氟苯基）吡咯烷，其中制备的新型稳定形式和制剂公开(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。
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3.发明授权公开(公告)号：US08501698B2
公开(公告)日：2013-08-06
申请号：US13049712
申请日：2011-03-16
申请人： Jack Z. Gougoutas , Hildegard Lobinger , Srividya Ramakrishnan , Prashant P. Deshpande , Jeffrey T. Bien , Chiajen Lai , Chenchi Wang , Peter Riebel , John Anthony Grosso , Alexandra A. Nirschl , Janak Singh , John D. DiMarco
发明人： Jack Z. Gougoutas , Hildegard Lobinger , Srividya Ramakrishnan , Prashant P. Deshpande , Jeffrey T. Bien , Chiajen Lai , Chenchi Wang , Peter Riebel , John Anthony Grosso , Alexandra A. Nirschl , Janak Singh , John D. DiMarco
IPC分类号： A61K31/351 , C07D309/10 , C07H7/04
CPC分类号： C07H15/207 , A61K31/7034 , A61K45/06 , A61P3/10 , C07H7/04
摘要： The present invention relates to physical crystal structures of a compound of the formula I: wherein R1, R2, R2a, R3 and R4 are as defined herein, especially pharmaceutical compositions containing structures of compound I or II, processes for preparing same, intermediates used in preparing same, and methods of treating diseases such as diabetes using such structures.
摘要翻译： 本发明涉及式I化合物的物理结晶结构：其中R1，R2，R2a，R3和R4如本文所定义，特别是含有化合物I或II结构的药物组合物，其制备方法， 制备方法以及使用这种结构治疗糖尿病等疾病的方法。
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公开(公告)号：US07598380B2
公开(公告)日：2009-10-06
申请号：US11492750
申请日：2006-07-25
申请人： Wansheng Liu , Sunil S. Patel , Nicolas Cuniere , Yvonne Lear , Prashant P. Deshpande , Jeffrey N. Simon , Chiajen Lai , Annie J. Pullockaran , Nachimuthu Soundararajan , Jeffrey T. Bien
发明人： Wansheng Liu , Sunil S. Patel , Nicolas Cuniere , Yvonne Lear , Prashant P. Deshpande , Jeffrey N. Simon , Chiajen Lai , Annie J. Pullockaran , Nachimuthu Soundararajan , Jeffrey T. Bien
IPC分类号： C07D487/04 , C07D213/69 , C07D213/73
CPC分类号： C07D213/73 , C07D213/69 , C07D471/04
摘要： A method of preparing azaindole compounds for antiviral use having the formula
摘要翻译： 制备具有下式的用于抗病毒用途的唑烷醇化合物的方法
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![Formulations of 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione](/abs-image/US/2006/05/11/US20060100209A1/abs.jpg.150x150.jpg)
5.发明申请Formulations of 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione 审中-公开制备1-（4-苯甲酰基 - 哌嗪-1-基）-2- [4-甲氧基-7-（3-甲基 - [1,2,4]三唑-1-基）-1H-吡咯并[ 3-c]吡啶-3-基] - 乙烷-1,2-二酮公开(公告)号：US20060100209A1
公开(公告)日：2006-05-11
申请号：US11267441
申请日：2005-11-04
申请人： Chong-Hui Gu , Qi Gao , Shan-Ming Kuang , Chiajen Lai , Jaquan Levons , Feng Qian
发明人： Chong-Hui Gu , Qi Gao , Shan-Ming Kuang , Chiajen Lai , Jaquan Levons , Feng Qian
IPC分类号： A61K31/53
CPC分类号： A61K31/53 , A61K9/14 , A61K9/146 , A61K9/1635 , A61K31/496 , A61K47/32
摘要： The instant invention provides formulations of 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione; processes for the production of such formulations; and methods of treating HIV or AIDS with such crystalline materials or such formulations.
摘要翻译： 本发明提供1-（4-苯甲酰基 - 哌嗪-1-基）-2- [4-甲氧基-7-（3-甲基 - [1,2,4]三唑-1-基） 吡咯并[2,3-c]吡啶-3-基] - 乙烷-1,2-二酮; 制备这种制剂的方法; 以及用这种结晶材料或这种制剂治疗HIV或AIDS的方法。
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6.发明授权公开(公告)号：US07919598B2
公开(公告)日：2011-04-05
申请号：US11765481
申请日：2007-06-20
申请人： Jack Z. Gougoutas , Hildegard Lobinger , Srividya Ramakrishnan , Prashant P. Deshpande , Jeffrey T. Bien , Chiajen Lai , Chenchi Wang , Peter Riebel , John Anthony Grosso , Alexandra A. Nirschl , Janak Singh , John D. DiMarco
发明人： Jack Z. Gougoutas , Hildegard Lobinger , Srividya Ramakrishnan , Prashant P. Deshpande , Jeffrey T. Bien , Chiajen Lai , Chenchi Wang , Peter Riebel , John Anthony Grosso , Alexandra A. Nirschl , Janak Singh , John D. DiMarco
CPC分类号： C07H15/207 , A61K31/7034 , A61K45/06 , A61P3/10 , C07H7/04
摘要： The present invention relates to physical crystal structures of a compound of the formula I: wherein R1, R2, R2a, R3 and R4 are as defined herein, especially pharmaceutical compositions containing structures of compound I or II, processes for preparing same, intermediates used in preparing same, and methods of treating diseases such as diabetes using such structures.
摘要翻译： 本发明涉及式I化合物的物理结晶结构：其中R1，R2，R2a，R3和R4如本文所定义，特别是含有化合物I或II结构的药物组合物，其制备方法， 制备方法以及使用这种结构治疗糖尿病等疾病的方法。
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公开(公告)号：US07820820B2
公开(公告)日：2010-10-26
申请号：US12546108
申请日：2009-08-24
申请人： Wansheng Liu , Sunil S. Patel , Nicolas Cuniere , Yvonne Lear , Prashant P. Deshpande , Jeffrey N. Simon , Chiajen Lai , Annie J. Pullockaran , Nachimuthu Soundararajan , Jeffrey T. Bien
发明人： Wansheng Liu , Sunil S. Patel , Nicolas Cuniere , Yvonne Lear , Prashant P. Deshpande , Jeffrey N. Simon , Chiajen Lai , Annie J. Pullockaran , Nachimuthu Soundararajan , Jeffrey T. Bien
IPC分类号： C07D487/04
CPC分类号： C07D213/73 , C07D213/69 , C07D471/04
摘要： A method of preparing azaindole compounds for antiviral use having the formula
摘要翻译： 制备具有下式的用于抗病毒用途的唑烷醇化合物的方法
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8.发明申请PROCESS FOR PREPARING TRIAZOLE SUBSTITUTED AZAINDOLEOXOACETIC PIPERAZINE DERIVATIVES AND NOVEL SALT FORMS PRODUCED THEREIN 有权制备三唑取代的氮杂双环氧哌嗪衍生物及其生产的新型盐形式的方法公开(公告)号：US20100076191A1
公开(公告)日：2010-03-25
申请号：US12548809
申请日：2009-08-27
申请人： NACHIMUTHU SOUNDARARAJAN , Yuping Qiu , Wenhao Hu , David R. Kronenthal , Pierre Sirard , Jean Lajeunesse , Robert Droghini , Ramakrishnan Chidambaram , Xinhua Qian , Kenneth J. Natalie , Shawn K. Pack , Nathan Reising , Erqing Tang , Michael G. Fakes , Qi Gao , Feng Qian , Blisse J. Vakkalagadda , Chiajen Lai , Shan-Ming Kuang
发明人： NACHIMUTHU SOUNDARARAJAN , Yuping Qiu , Wenhao Hu , David R. Kronenthal , Pierre Sirard , Jean Lajeunesse , Robert Droghini , Ramakrishnan Chidambaram , Xinhua Qian , Kenneth J. Natalie , Shawn K. Pack , Nathan Reising , Erqing Tang , Michael G. Fakes , Qi Gao , Feng Qian , Blisse J. Vakkalagadda , Chiajen Lai , Shan-Ming Kuang
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07C311/49 , C07D213/26
摘要： A process is provided for preparing triazole substituted azaindoleoxoacetic piperazine derivative. Novel intermediates produced in the above process, and novel N-1 and amorphous forms of a 1,2,3-triazole substituted azaindoloxoacetic piperazine derivatives and processes for producing such novel forms are also provided.
摘要翻译： 提供制备三唑取代的氮杂糊精乙酸哌嗪衍生物的方法。 还提供了在上述方法中制备的新型中间体和新的N-1和无定形形式的1,2,3-三唑取代的氮杂寡脱氧乙酸哌嗪衍生物及其制备方法。
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![PROCESS FOR THE PREPARATION OF [(1R), 2S]-2-AMINOPROPIONIC ACID 2-[4-(4-FLUORO-2-METHYL-1H-INDOL-5-YLOXY)-5-METHYLPYRROLO[2,1-f][1,2,4]TRIAZIN-6-YLOXY]-1-METHYLETHYL ESTER](/abs-image/US/2007/10/25/US20070249610A1/abs.jpg.150x150.jpg)
9.发明申请PROCESS FOR THE PREPARATION OF [(1R), 2S]-2-AMINOPROPIONIC ACID 2-[4-(4-FLUORO-2-METHYL-1H-INDOL-5-YLOXY)-5-METHYLPYRROLO[2,1-f][1,2,4]TRIAZIN-6-YLOXY]-1-METHYLETHYL ESTER 有权制备[（1R），2S] -2-氨基丙酸2- [4-（4-氟-2-甲基-1H-吲哚-5-基）-5-甲基吡咯并[2,1-f] [1,2,4]三嗪-6-基锂] -1-甲基乙基酯公开(公告)号：US20070249610A1
公开(公告)日：2007-10-25
申请号：US11737787
申请日：2007-04-20
申请人： Gerard Crispino , Mourad Hamedi , Thomas LaPorte , John Thornton , Jaan Pesti , Zhongmin Xu , Paul Lobben , David Leahy , Jale Muslehiddinoglu , Chiajen Lai , Lori Spangler , Robert Discordia
发明人： Gerard Crispino , Mourad Hamedi , Thomas LaPorte , John Thornton , Jaan Pesti , Zhongmin Xu , Paul Lobben , David Leahy , Jale Muslehiddinoglu , Chiajen Lai , Lori Spangler , Robert Discordia
IPC分类号： A61K31/53 , C07D487/04
CPC分类号： C07D487/04
摘要： The invention relates to an improved process for preparing [(1R),2S]-2-aminopropionic acid 2-[4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy]-1-methylethyl ester of the formula: Compound I has been shown to be useful for the treatment of certain types of cancer.
摘要翻译： 本发明涉及制备[（1R），2S] -2-氨基丙酸2- [4-（4-氟-2-甲基-1H-吲哚-5-基氧基）-5-甲基吡咯并[2， 1-f] [1,2,4]三嗪-6-基氧基] -1-甲基乙基酯：化合物I已经显示可用于治疗某些类型的癌症。
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公开(公告)号：US20060293304A1
公开(公告)日：2006-12-28
申请号：US11455338
申请日：2006-06-19
申请人： Nachimuthu Soundararajan , Yuping Qiu , Wenhao Hu , David Kronenthal , Pierre Sirard , Jean Lajeunesse , Robert Droghini , Ramakrishnan Chidambaram , Xinhua Qian , Kenneth Natalie , Shawn Pack , Nathan Reising , Erqing Tang , Michael Fakes , Qi Gao , Feng Qian , Blisse Vakkalagadda , Chiajen Lai , Shan-Ming Kuang
发明人： Nachimuthu Soundararajan , Yuping Qiu , Wenhao Hu , David Kronenthal , Pierre Sirard , Jean Lajeunesse , Robert Droghini , Ramakrishnan Chidambaram , Xinhua Qian , Kenneth Natalie , Shawn Pack , Nathan Reising , Erqing Tang , Michael Fakes , Qi Gao , Feng Qian , Blisse Vakkalagadda , Chiajen Lai , Shan-Ming Kuang
IPC分类号： C07D471/02 , A61K31/55 , A61K31/5377 , A61K31/496 , A61K31/4745
CPC分类号： C07D471/04 , C07C311/49 , C07D213/26
摘要： A process is provided for preparing triazole substituted azaindoleoxoacetic piperazine derivative. Novel intermediates produced in the above process, and novel N-1 and amorphous forms of a 1,2,3-triazole substituted azaindoloxoacetic piperazine derivatives and processes for producing such novel forms are also provided.
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