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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。
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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.
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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.
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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。
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5.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：US08236847B2
公开(公告)日：2012-08-07
申请号：US13081341
申请日：2011-04-06
申请人： Jack Z. Gougoutas , Mary F. Malley , John D. DiMarco , Xiaotian S. Yin , Chenkou Wei , Jurong Yu , Truc Chi Vu , Gregory Scott Jones , Scott A. Savage
发明人： Jack Z. Gougoutas , Mary F. Malley , John D. DiMarco , Xiaotian S. Yin , Chenkou Wei , Jurong Yu , Truc Chi Vu , Gregory Scott Jones , Scott A. Savage
IPC分类号： A61K31/403 , C07D209/02
CPC分类号： C07D209/52 , A61K31/403 , A61K45/06 , A61K2300/00
摘要： Physical crystal structures of a compound of the formula I: are provided including the free base monohydrate thereof (form H-1) and the hydrochloric acid salt thereof, including hydrochloric acid salt containing 0.75 equivalent of H2O (form H0.75-3) and hydrochloric acid salt containing 2 equivalents of H2O (form H2-1), and hydrochloric acid salt Pattern P-5, preferably in substantially pure form, and other forms as described herein, pharmaceutical compositions containing structures of compound I or IA, processes for preparing same, intermediates used in preparing same, and methods of treating diseases such as diabetes using such structures.
摘要翻译： 提供式I化合物的物理晶体结构：包括其游离碱一水合物（形式H-1）及其盐酸盐，包括含有0.75当量H 2 O（H0.75-3）的盐酸盐和 含有2当量H 2 O（形式H2-1）的盐酸盐和盐酸盐图案P-5，优选基本上纯的形式，以及本文所述的其它形式，含有化合物I或IA的结构的药物组合物，制备方法 相同的，用于制备其的中间体，以及使用这种结构治疗疾病如糖尿病的方法。
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7.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：US06858644B2
公开(公告)日：2005-02-22
申请号：US10304615
申请日：2002-11-26
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。
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9.发明申请公开(公告)号：US20110172176A1
公开(公告)日：2011-07-14
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： A61K31/7034 , C07H15/207 , C07H1/00 , A61P3/04 , A61P3/10 , A61P17/02 , A61P3/06 , A61P9/10 , A61P9/12
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：US07943656B2
公开(公告)日：2011-05-17
申请号：US12105316
申请日：2008-04-18
申请人： Jack Z. Gougoutas , Mary F. Malley , John D. DiMarco , Xiaotian S. Yin , Chenkou Wei , Jurong Yu , Truc Chi Vu , Gregory Scott Jones , Scott A. Savage
发明人： Jack Z. Gougoutas , Mary F. Malley , John D. DiMarco , Xiaotian S. Yin , Chenkou Wei , Jurong Yu , Truc Chi Vu , Gregory Scott Jones , Scott A. Savage
IPC分类号： C07D209/02 , A61K31/403
CPC分类号： C07D209/52 , A61K31/403 , A61K45/06 , A61K2300/00
摘要： Physical crystal structures of a compound of the formula I: are provided including the free base monohydrate thereof (form H-1) and the hydrochloric acid salt thereof, including hydrochloric acid salt containing 0.75 equivalent of H2O (form H0.75-3) and hydrochloric acid salt containing 2 equivalents of H2O (form H2-1), and hydrochloric acid salt Pattern P-5, preferably in substantially pure form, and other forms as described herein, pharmaceutical compositions containing structures of compound I or IA, processes for preparing same, intermediates used in preparing same, and methods of treating diseases such as diabetes using such structures.
摘要翻译： 提供式I化合物的物理晶体结构：包括其游离碱一水合物（形式H-1）及其盐酸盐，包括含有0.75当量H 2 O（H0.75-3）的盐酸盐和 含有2当量H 2 O（形式H2-1）的盐酸盐和盐酸盐图案P-5，优选基本上纯的形式，以及本文所述的其它形式，含有化合物I或IA的结构的药物组合物，制备方法 相同的，用于制备其的中间体，以及使用这种结构治疗疾病如糖尿病的方法。
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