公开(公告)号：US20060014756A1

公开(公告)日：2006-01-19

申请号：US11029064

申请日：2005-01-04

Applicant: Michael Edwards ,  Paul Cox ,  Shelley Amendola ,  Stephanie Deprets ,  Timothy Gillespy ,  Christopher Edlin ,  Andrew Morley ,  Charles Gardner ,  Brian Pedgrift ,  Herve Bouchard ,  Didier Babin ,  Laurence Gauzy ,  Alain Le-Brun ,  Tahir Majid ,  John Reader ,  Lloyd Payne ,  Nawaz Khan ,  Michael Cherry

Inventor： Michael Edwards ,  Paul Cox ,  Shelley Amendola ,  Stephanie Deprets ,  Timothy Gillespy ,  Christopher Edlin ,  Andrew Morley ,  Charles Gardner ,  Brian Pedgrift ,  Herve Bouchard ,  Didier Babin ,  Laurence Gauzy ,  Alain Le-Brun ,  Tahir Majid ,  John Reader ,  Lloyd Payne ,  Nawaz Khan ,  Michael Cherry

IPC: A61K31/496 ,  A61K31/4184 ,  C07D43/02

CPC classification number: C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04

Abstract: The invention is directed to physiologically active compounds of the general formula (Ix) and compositions containing such compounds, and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (Ix), and to processes for their preparation. Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.

Abstract translation: 本发明涉及通式（Ix）的生理活性化合物和含有这些化合物及其前药以及这些化合物及其前药的药学上可接受的盐和溶剂合物的组合物，以及式（Ix）范围内的新化合物 Ix），以及它们的制备过程。 这些化合物和组合物具有有价值的药物特性，特别是抑制激酶的能力。

公开(公告)号：US06897207B2

公开(公告)日：2005-05-24

申请号：US10177804

申请日：2002-06-21

Applicant: Paul J. Cox ,  Tahir N. Majid ,  Justine Yeun Quai Lai ,  Andrew D. Morley ,  Shelley Amendola ,  Stephanie D. Deprets ,  Christopher Edlin ,  Charles J. Gardner ,  Dorothea Kominos ,  Brian L. Pedgrift ,  Frank Halley ,  Timothy A. Gillespy ,  Michael Edwards ,  Francois F. Clerc ,  Conception Nemecek ,  Olivier Houille ,  Dominique Damour ,  Herve Bouchard ,  Daniel N. A. Bezard ,  Chantal Carrez

Inventor： Paul J. Cox ,  Tahir N. Majid ,  Justine Yeun Quai Lai ,  Andrew D. Morley ,  Shelley Amendola ,  Stephanie D. Deprets ,  Christopher Edlin ,  Charles J. Gardner ,  Dorothea Kominos ,  Brian L. Pedgrift ,  Frank Halley ,  Timothy A. Gillespy ,  Michael Edwards ,  Francois F. Clerc ,  Conception Nemecek ,  Olivier Houille ,  Dominique Damour ,  Herve Bouchard ,  Daniel N. A. Bezard ,  Chantal Carrez

IPC: A61K20060101 ,  A61K31/437 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/5355 ,  A61K31/5377 ,  A61K31/541 ,  A61P20060101 ,  A61P9/00 ,  A61P11/00 ,  A61P11/02 ,  A61P11/06 ,  A61P13/08 ,  A61P17/00 ,  A61P17/02 ,  A61P17/06 ,  A61P19/02 ,  A61P27/14 ,  A61P29/00 ,  A61P35/00 ,  A61P37/08 ,  A61P43/00 ,  C07D20060101 ,  C07D209/00 ,  C07D221/00 ,  C07D241/00 ,  C07D471/04 ,  C07D487/04 ,  C07D519/00 ,  A61K31/33 ,  A61K31/66 ,  C07D417/02

CPC classification number: C07D519/00 ,  C07D471/04 ,  C07D487/04

Abstract: The invention is directed to physiologically active compounds of general formula (I): and compositions containing such compounds; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (I). Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.

Abstract translation: 本发明涉及通式（I）的生理活性化合物：和含有这些化合物的组合物; 及其前药，以及这些化合物及其前药的药学上可接受的盐和溶剂合物，以及式（I）范围内的新化合物。 这些化合物和组合物具有有价值的药物特性，特别是抑制激酶的能力。

公开(公告)号：US5959125A

公开(公告)日：1999-09-28

申请号：US930561

申请日：1997-10-02

Applicant: Herve Bouchard ,  Jean-Dominique Bourzat ,  Alain Commer.cedilla.on

Inventor： Herve Bouchard ,  Jean-Dominique Bourzat ,  Alain Commer.cedilla.on

IPC: A61K31/335 ,  A61K31/337 ,  A61P35/00 ,  C07D305/14 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07D413/12

CPC classification number: C07D405/12 ,  C07D305/14 ,  C07D407/12 ,  C07D409/12 ,  Y02P20/55

Abstract: Novel taxoids of general formula (I), wherein R is a substituted alkyl radical or an alkenyl, alkynyl, cycloalkyl, optionally substituted cycloalkenyl or phenyl radical, or an aromatic 5- or 6-membered heterocyclic radical; and Z is a hydrogen atom or a radical of general formula (II), wherein R.sub.1 is an optionally substituted benzoyl, thenoyl or furoyl radical or a radical R.sub.2 --O--CO, where R.sub.2 is an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, optionally substituted phenyl, or heterocycl radical, and R.sub.3 is an aromatic heterocyclic, alkyl, alkenyl, alkynyl cycloalkyl, phenyl or naphthyl radical. The novel products of general formula (I), wherein Z is a radical of general formula (II), have remarkable antitumoral activity. ##STR1##

Abstract translation: PCT No.PCT / FR96 / 00487 Sec。 371 1997年10月2日第 102（e）日期1997年10月2日PCT提交1996年4月1日PCT公布。 WO96 / 31493 PCT出版物 日期1996年10月10日通式（I）的新型紫杉烷类，其中R是取代的烷基或链烯基，炔基，环烷基，任选取代的环烯基或苯基，或芳族5-或6-元杂环基; 并且Z是氢原子或通式（II）的基团，其中R 1是任选取代的苯甲酰基，噻吩甲酰基或糠基或基团R 2 -O-CO，其中R 2是烷基，烯基，炔基，环烷基，环烯基 ，双环烷基，任选取代的苯基或杂环基，并且R 3是芳族杂环，烷基，烯基，炔基环烷基，苯基或萘基。 通式（I）的新产物（其中Z为通式（II）的基团）具有显着的抗肿瘤活性。

公开(公告)号：US5654449A

公开(公告)日：1997-08-05

申请号：US607854

申请日：1996-02-27

Applicant: Herve Bouchard ,  Jean-Dominique Bourzat ,  Alain Commercon ,  Jean-Pierre Pulicani

Inventor： Herve Bouchard ,  Jean-Dominique Bourzat ,  Alain Commercon ,  Jean-Pierre Pulicani

IPC: A61K31/335 ,  A61K31/337 ,  A61P35/00 ,  C07D305/14

CPC classification number: C07D305/14 ,  Y02P20/55

Abstract: This invention relates to a process for preparing taxoid derivatives of formulae II and XI: ##STR1## in which Ar represents an aryl radical; R.sub.1 represents a benzoyl radical or a radical R.sub.2 --O--CO-- in which R.sub.2 represents an unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl, or saturated or unsaturated heterocyclic radical; R.sub.3 represents an unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, saturated or unsaturated heterocyclic, or aryl radial, but not a phenyl radical; R.sub.4 represents a hydrogen atom and R.sub.5 represents a hydroxyl-protecting group or R.sub.4 and R.sub.5 together form a heterocyclic group; G.sub.1 represents a hydroxyl-protecting group; and G.sub.2 represents an acetyl radical or hydroxyl-protecting group;by electrolytically reducing a protected taxoid compound in an electrolyte comprising a quaternary ammonium salt which is soluble in an organic solvent or in an aqueous/organic mixture at a controlled potential.

Abstract translation: 本发明涉及制备式II和XI的类固醇衍生物的方法：其中Ar表示芳基;其中Ar表示芳基; R 1表示苯甲酰基或基团R 2 -O-CO-，其中R 2表示未取代或取代的烷基，烯基，炔基，环烷基，环烯基，双环烷基，苯基或饱和或不饱和杂环基; R 3表示未取代或取代的烷基，烯基，炔基，环烷基，环烯基，双环烷基，饱和或不饱和杂环，或芳基，但不是苯基; R4表示氢原子，R5表示羟基保护基，或R4和R5一起形成杂环基; G1表示羟基保护基; G 2代表乙酰基或羟基保护基; 通过在包含可溶于有机溶剂的季铵盐或在受控电位的水/有机混合物中的电解质中电解还原受保护的紫杉烷化合物。