公开(公告)号：US06689802B2

公开(公告)日：2004-02-10

申请号：US09925112

申请日：2001-08-09

申请人： John D. DiMarco ,  Jack Z. Gougoutas ,  Imre M. Vitez ,  Martha Davidovich ,  Michael A. Galella ,  Timothy M. Malloy ,  Zhenrong Guo ,  Denis Favreau

发明人： John D. DiMarco ,  Jack Z. Gougoutas ,  Imre M. Vitez ,  Martha Davidovich ,  Michael A. Galella ,  Timothy M. Malloy ,  Zhenrong Guo ,  Denis Favreau

IPC分类号： C07D49304

CPC分类号： C07D491/04 ,  C07D417/06

摘要： There are provided in accordance with the present invention two crystalline polymorphs, designated Form A and Form B, respectively, as well as mixtures thereof, of an epothilone analog represented by the formula Also provided are methods of forming the novel polymorphs, therapeutic methods utilizing them and pharmaceutical dosage forms containing them.

摘要翻译： 根据本发明，提供了分别由式表示的埃坡霉素类似物的分别称为A型和B型的两种结晶多晶型物及其混合物，还提供形成新型多晶型物的方法，利用它们的治疗方法和 含有它们的药物剂型。

公开(公告)号：US07153879B2

公开(公告)日：2006-12-26

申请号：US11271456

申请日：2005-11-10

申请人： John D. DiMarco ,  Jack Z. Gougoutas ,  Imre M. Vitez ,  Martha Davidovich ,  Michael A. Galella ,  Timothy M. Malloy ,  Zhenrong Guo ,  Denis Favreau

发明人： John D. DiMarco ,  Jack Z. Gougoutas ,  Imre M. Vitez ,  Martha Davidovich ,  Michael A. Galella ,  Timothy M. Malloy ,  Zhenrong Guo ,  Denis Favreau

IPC分类号： C07D493/04 ,  A61K31/42 ,  A61P35/00

CPC分类号： C07D491/04 ,  C07D417/06

摘要： There are provided in accordance with the present invention two crystalline polymorphs, designated Form A and Form B, respectively, as well as mixtures thereof, of an epothilone analog represented by the formula Also provided are methods of forming the novel polymorphs, therapeutic methods utilizing them and pharmaceutical dosage forms containing them.

公开(公告)号：US06982276B2

公开(公告)日：2006-01-03

申请号：US10773819

申请日：2004-02-06

申请人： John D. DiMarco ,  Jack Z. Gougoutas ,  Imre M. Vitez ,  Martha Davidovich ,  Michael A. Galella ,  Timothy M. Malloy ,  Zhenrong Guo ,  Denis Favreau

发明人： John D. DiMarco ,  Jack Z. Gougoutas ,  Imre M. Vitez ,  Martha Davidovich ,  Michael A. Galella ,  Timothy M. Malloy ,  Zhenrong Guo ,  Denis Favreau

IPC分类号： C07D493/04 ,  A61K31/42

CPC分类号： C07D491/04 ,  C07D417/06

摘要： There are provided in accordance with the present invention two crystalline polymorphs, designated Form A and Form B, respectively, as well as mixtures thereof, of an epothilone analog represented by the formula Also provided are methods of forming the novel polymorphs, therapeutic methods utilizing them and pharmaceutical dosage forms containing them.

公开(公告)号：US06413969B1

公开(公告)日：2002-07-02

申请号：US09932045

申请日：2001-08-17

申请人： Krishnaswamy S. Raghavan ,  Sunanda A. Ranadive ,  Jack Z. Gougoutas ,  John D. DiMarco ,  William L. Parker ,  Martha Davidovich ,  Ann Newman

发明人： Krishnaswamy S. Raghavan ,  Sunanda A. Ranadive ,  Jack Z. Gougoutas ,  John D. DiMarco ,  William L. Parker ,  Martha Davidovich ,  Ann Newman

IPC分类号： A61K31496

CPC分类号： C07D215/56

摘要： There are provided in accordance with the present invention crystalline gatifloxacin pentahydrate represented by the formula in a highly homogeneous form with respect to other crystalline forms thereof.

摘要翻译： 根据本发明，提供了结晶加替沙星五水合物，其以相对于其它结晶形式的高度均匀形式的形式表示。

公开(公告)号：US20110124689A1

公开(公告)日：2011-05-26

申请号：US12900588

申请日：2010-10-08

申请人： Soojin Kim ,  Bruce T. Lotz ,  Mary F. Malley ,  Jack Z. Gougoutas ,  Martha Davidovich ,  Sushil K. Srivastava

发明人： Soojin Kim ,  Bruce T. Lotz ,  Mary F. Malley ,  Jack Z. Gougoutas ,  Martha Davidovich ,  Sushil K. Srivastava

IPC分类号： A61K31/4418 ,  C07D213/42 ,  A61P31/12

CPC分类号： C07D213/42

摘要： A process is provided for preparing the HIV protease inhibitor atazanavir bisulfate wherein a solution of atazanavir free base is reacted with concentrated sulfuric acid in an amount to react with less than about 15% by weight of the free base, seeds of Form A crystals of atazanavir bisulfate are added to the reaction mixture, and as crystals of the bisulfate form, additional concentrated sulfuric acid is added in multiple stages at increasing rates according to a cubic equation, to effect formation of Form A crystals of atazanavir bisulfate.A process is also provided for preparing atazanavir bisulfate as Pattern C material. A novel form of atazanavir bisulfate is also provided which is Form E3 which is a highly crystalline triethanolate solvate of the bisulfate salt from ethanol.

摘要翻译： 提供了一种制备HIV蛋白酶抑制剂阿扎那韦硫酸氢盐的方法，其中阿扎那韦游离碱的溶液与浓硫酸反应的量与小于约15重量％的游离碱反应，阿扎那韦的A型晶体种子 将硫酸氢盐加入到反应混合物中，并且以硫酸氢盐形式的结晶，按照立方式以增加的速率以多个阶段多次加入另外的浓硫酸，以实现阿扎那韦硫酸氢盐的形式A晶体的形成。 还提供了制备作为图案C材料的阿扎那韦硫酸氢盐的方法。 还提供了一种新型形式的阿扎那韦硫酸氢盐，其为E3型，其是来自乙醇的硫酸氢盐的高度结晶的三乙醇盐溶剂合物。

公开(公告)号：US07838678B2

公开(公告)日：2010-11-23

申请号：US12360468

申请日：2009-01-27

申请人： Soojin Kim ,  Bruce T. Lotz ,  Mary F. Malley ,  Jack Z. Gougoutas ,  Martha Davidovich ,  Sushil K. Srivastava

发明人： Soojin Kim ,  Bruce T. Lotz ,  Mary F. Malley ,  Jack Z. Gougoutas ,  Martha Davidovich ,  Sushil K. Srivastava

IPC分类号： C07D213/56

CPC分类号： C07D213/42

摘要： A process is provided for preparing the HIV protease inhibitor atazanavir bisulfate wherein a solution of atazanavir free base is reacted with concentrated sulfuric acid in an amount to react with less than about 15% by weight of the free base, seeds of Form A crystals of atazanavir bisulfate are added to the reaction mixture, and as crystals of the bisulfate form, additional concentrated sulfuric acid is added in multiple stages at increasing rates according to a cubic equation, to effect formation of Form A crystals of atazanavir bisulfate.A process is also provided for preparing atazanavir bisulfate as Pattern C material. A novel form of atazanavir bisulfate is also provided which is Form E3 which is a highly crystalline triethanolate solvate of the bisulfate salt from ethanol.

公开(公告)号：US20090203630A1

公开(公告)日：2009-08-13

申请号：US12360468

申请日：2009-01-27

申请人： Soojin Kim ,  Bruce T. Lotz ,  Mary F. Malley ,  Jack Z. Gougoutas ,  Martha Davidovich ,  Sushil K. Srivastava

发明人： Soojin Kim ,  Bruce T. Lotz ,  Mary F. Malley ,  Jack Z. Gougoutas ,  Martha Davidovich ,  Sushil K. Srivastava

IPC分类号： A61K38/05 ,  C07C243/18 ,  A61P31/12

CPC分类号： C07D213/42

摘要： A process is provided for preparing the HIV protease inhibitor atazanavir bisulfate wherein a solution of atazanavir free base is reacted with concentrated sulfuric acid in an amount to react with less than about 15% by weight of the free base, seeds of Form A crystals of atazanavir bisulfate are added to the reaction mixture, and as crystals of the bisulfate form, additional concentrated sulfuric acid is added in multiple stages at increasing rates according to a cubic equation, to effect formation of Form A crystals of atazanavir bisulfate.A process is also provided for preparing atazanavir bisulfate as Pattern C material. A novel form of atazanavir bisulfate is also provided which is Form E3 which is a highly crystalline triethanolate solvate of the bisulfate salt from ethanol.

摘要翻译： 提供了一种制备HIV蛋白酶抑制剂阿扎那韦硫酸氢盐的方法，其中阿扎那韦游离碱的溶液与浓硫酸反应的量与小于约15重量％的游离碱反应，阿扎那韦的A型晶体种子 将硫酸氢盐加入到反应混合物中，并且以硫酸氢盐形式的结晶，按照立方式以增加的速率以多个阶段多次加入另外的浓硫酸，以实现阿扎那韦硫酸氢盐的形式A晶体的形成。 还提供了制备作为图案C材料的阿扎那韦硫酸氢盐的方法。 还提供了一种新型形式的阿扎那韦硫酸氢盐，其为E3型，其是来自乙醇的硫酸氢盐的高度结晶的三乙醇盐溶剂合物。

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

IPC分类号： C07H7/04 ,  C07H1/00 ,  A61K31/70

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。

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。

公开(公告)号：US06858644B2

公开(公告)日：2005-02-22

申请号：US10304615

申请日：2002-11-26

申请人： Daniel A. Benigni ,  Jack Z. Gougoutas ,  John D. DiMarco

发明人： Daniel A. Benigni ,  Jack Z. Gougoutas ,  John D. DiMarco

IPC分类号： A61K31/337 ,  A61P35/00 ,  C07C233/03 ,  C07C233/05 ,  C07C255/03 ,  C07C317/04 ,  C07D305/14 ,  C07D409/12 ,  A61K31/335

CPC分类号： C07D409/12 ,  A61K31/337 ,  C07D305/14

摘要： Biologically active crystalline solvates of paclitaxel are precipitated using polar, aprotic, organic solvents. A pharmaceutical composition is also disclosed, as well as the preparation of the novel solvates and their uses as anti-tumor agents.

摘要翻译： 使用极性，非质子，有机溶剂沉淀紫杉醇的生物活性结晶溶剂合物。 还公开了药物组合物，以及新溶剂合物的制备及其作为抗肿瘤剂的用途。