公开(公告)号：USRE39356E1

公开(公告)日：2006-10-17

申请号：US11056606

申请日：2005-02-11

申请人： Wen Sen Li ,  John E. Thornton ,  Zhenrong Guo ,  Shankar Swaminathan ,  Robert M. Borzilleri ,  Soong-Hoon Kim ,  Denis Favreau

发明人： Wen Sen Li ,  John E. Thornton ,  Zhenrong Guo ,  Shankar Swaminathan ,  Robert M. Borzilleri ,  Soong-Hoon Kim ,  Denis Favreau

IPC分类号： C07D491/00 ,  C07D417/00

摘要： The present invention relates to a process for the preparation of epothilone analogs by initially forming novel ring-opened epothilones and carrying out a macrolactamization reaction thereon. The subject process is amenable to being carried out in a single reaction vessel without isolation of the intermediate compound and provides at least about a three-fold increase in yield over prior processes for preparing the desired epothilone analogs.

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：US20060063815A1

公开(公告)日：2006-03-23

申请号：US11271456

申请日：2005-11-10

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

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

IPC分类号： A61K31/427

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，提供分别由式（I）和式（B）表示的两个结晶多晶型物及其混合物，其由式

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：US08357806B2

公开(公告)日：2013-01-22

申请号：US13468812

申请日：2012-05-10

申请人： Shawn A. Springfield ,  Wendel W. Doubleday ,  Frederic Buono ,  Michel A. Couturier ,  Yvonne Lear ,  Denis Favreau ,  Kathia Levesque ,  Percy Sarwood Manchand ,  Markus Frieser ,  Anthony J. Cocuzza

发明人： Shawn A. Springfield ,  Wendel W. Doubleday ,  Frederic Buono ,  Michel A. Couturier ,  Yvonne Lear ,  Denis Favreau ,  Kathia Levesque ,  Percy Sarwood Manchand ,  Markus Frieser ,  Anthony J. Cocuzza

IPC分类号： C07D217/24

CPC分类号： C07D217/24

摘要： The present disclosure generally relates to a process for synthesizing optionally substituted 1-chloro-4-methoxyisoquinolines. The present disclosure also relates to intermediates useful in this process.

摘要翻译： 本公开内容一般涉及合成任选取代的1-氯-4-甲氧基异喹啉的方法。 本公开还涉及在该方法中有用的中间体。

公开(公告)号：US20120220774A1

公开(公告)日：2012-08-30

申请号：US13468812

申请日：2012-05-10

申请人： Shawn A. Springfield ,  Wendel W. Doubleday ,  Frederic Buono ,  Michel A. Couturier ,  Yvonne Lear ,  Denis Favreau ,  Kathia Levesque ,  Percy Sarwood Manchand ,  Markus Frieser ,  Anthony J. Cocuzza

发明人： Shawn A. Springfield ,  Wendel W. Doubleday ,  Frederic Buono ,  Michel A. Couturier ,  Yvonne Lear ,  Denis Favreau ,  Kathia Levesque ,  Percy Sarwood Manchand ,  Markus Frieser ,  Anthony J. Cocuzza

IPC分类号： C07D217/24

CPC分类号： C07D217/24

摘要： The present disclosure generally relates to a process for synthesizing optionally substituted 1-chloro-4-methoxyisoquinolines. The present disclosure also relates to intermediates useful in this process.

摘要翻译： 本公开内容一般涉及合成任选取代的1-氯-4-甲氧基异喹啉的方法。 本公开还涉及在该方法中有用的中间体。

公开(公告)号：US20100056792A1

公开(公告)日：2010-03-04

申请号：US12547158

申请日：2009-08-25

申请人： Shawn A. Springfield ,  Wendel W. Doubleday ,  Frederic Buono ,  Michel A. Couturier ,  Yvonne Lear ,  Denis Favreau ,  Kathia Levesque ,  Percy Sarwood Manchand ,  Markus Frieser ,  Anthony J. Cocuzza ,  Hyungcheol Kim ,  Sangsoo Lee ,  Chunyoung Kim ,  Soonha Yang ,  Eunhee Choi

发明人： Shawn A. Springfield ,  Wendel W. Doubleday ,  Frederic Buono ,  Michel A. Couturier ,  Yvonne Lear ,  Denis Favreau ,  Kathia Levesque ,  Percy Sarwood Manchand ,  Markus Frieser ,  Anthony J. Cocuzza ,  Hyungcheol Kim ,  Sangsoo Lee ,  Chunyoung Kim ,  Soonha Yang ,  Eunhee Choi

IPC分类号： C07D217/24 ,  A61P31/14

CPC分类号： C07D217/24

摘要： The present disclosure generally relates to a process for synthesizing optionally substituted 1-chloro-4-methoxyisoquinolines. The present disclosure also relates to intermediates useful in this process.

摘要翻译： 本公开内容一般涉及合成任选取代的1-氯-4-甲氧基异喹啉的方法。 本公开还涉及在该方法中有用的中间体。

公开(公告)号：US06930187B2

公开(公告)日：2005-08-16

申请号：US10365892

申请日：2003-02-13

申请人： Denis Favreau ,  Joydeep Kant ,  Kathia Levesque ,  Shaopeng Wang ,  Zhengrong Guo ,  Brian Leslie James

发明人： Denis Favreau ,  Joydeep Kant ,  Kathia Levesque ,  Shaopeng Wang ,  Zhengrong Guo ,  Brian Leslie James

IPC分类号： C07D493/04 ,  C07D417/06

CPC分类号： C07D493/04

摘要： An improved method of synthesis of 21-amino epothilone derivatives which provides a one-pot conversion of 21-hydroxy epothilones to highly desirable 21-amino epothilones in high yield.

摘要翻译： 一种改进的21-氨基埃坡霉素衍生物的合成方法，其以高收率提供21-羟基埃坡霉素一高效转化为高度期望的21-氨基埃坡霉素。

公开(公告)号：US5648474A

公开(公告)日：1997-07-15

申请号：US773056

申请日：1991-10-08

申请人： Denis Favreau

发明人： Denis Favreau

IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P35/00 ,  C07H15/24 ,  C07H17/00 ,  C07H17/04

CPC分类号： C07H17/04

摘要： The present invention provides temperature stable crystalline etoposide 4'-phosphate diethanol solvate, and a process for its preparation.

摘要翻译： 本发明提供温度稳定的依托泊苷4'-磷酸二乙醇溶剂化物及其制备方法。