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公开(公告)号：US20110077210A1
公开(公告)日：2011-03-31
申请号：US11916495
申请日：2006-06-02
CPC分类号： C07K14/4702 , A61K38/00 , C12N9/16 , C12N9/80 , C12Q1/34 , C12Y305/01098 , G01N33/573 , G01N33/6875 , G01N2333/98
摘要： This invention relates to the field of assays for compounds that interact with the binding of a PTB-containing protein, i.e. APPL (Adaptor protein containing PH domain, PTB domain and Leucine zipper motif) with histone deacetylase, in particular HDAC1. Compounds identified using said assays are useful in inhibiting HDAC activity and as a medicine, in particular in the manufacture of a medicament to inhibit proliferative conditions, such as cancer and psoriasis.
摘要翻译： 本发明涉及与含有PTB的蛋白质（即APPL（含适配蛋白的PH结构域，PTB结构域和亮氨酸拉链基序））与组蛋白脱乙酰酶（特别是HDAC1）的结合相互作用的化合物的测定领域。 使用所述测定法鉴定的化合物可用于抑制HDAC活性和用作药物，特别是在制备抑制增殖性疾病如癌症和牛皮癣的药物中。
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公开(公告)号：US20100168065A1
公开(公告)日：2010-07-01
申请号：US12529142
申请日：2008-03-07
申请人： Jorge Eduardo Vialard , Patrick René Angibaud , Laurence Anne Mevellec , Christophe Meyer , Eddy Jean Edgard Freyne , Isabelle Noëlle Pilatte , Bruno Roux , Elisabeth Thérèse Jeanne Pasquier , Xavier Marc Bourdrez , Christophe Denis Adelinet , Laurence Francoise Bernadette Marconnet-Decrane , Jacqueline Anne Macritchie , James Edward Stewart Duffy , Andrew Pate Owens , Pierre-Henri Storck , Virginie Sophie Poncelet
发明人： Jorge Eduardo Vialard , Patrick René Angibaud , Laurence Anne Mevellec , Christophe Meyer , Eddy Jean Edgard Freyne , Isabelle Noëlle Pilatte , Bruno Roux , Elisabeth Thérèse Jeanne Pasquier , Xavier Marc Bourdrez , Christophe Denis Adelinet , Laurence Francoise Bernadette Marconnet-Decrane , Jacqueline Anne Macritchie , James Edward Stewart Duffy , Andrew Pate Owens , Pierre-Henri Storck , Virginie Sophie Poncelet
IPC分类号： A61K31/675 , C07D215/227 , A61K31/4704 , C07D413/12 , A61K31/5377 , C07D401/12 , A61K31/496 , A61K31/506 , C07F9/38 , A61K31/502 , A61K31/498 , C07D471/04 , A61K31/437 , A61P35/00
CPC分类号： C07D215/227 , C07D401/06 , C07D401/12 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06
摘要： The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, n, m and X have defined meanings.
摘要翻译： 本发明提供式（I）化合物，它们作为PARP抑制剂的用途以及包含所述式（I）化合物的药物组合物，其中R1，R2，R3，R4，R5，R6，R7，n，m和X具有 定义含义。
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公开(公告)号：US08404713B2
公开(公告)日：2013-03-26
申请号：US12681790
申请日：2008-10-22
申请人： Patrick René Angibaud , Laurence Françoise Bernadette Marconnet-Decrane , Jorge Eduardo Vialard , Laurence Anne Mevellec , Christophe Meyer , Pierre-Henri Storck
发明人： Patrick René Angibaud , Laurence Françoise Bernadette Marconnet-Decrane , Jorge Eduardo Vialard , Laurence Anne Mevellec , Christophe Meyer , Pierre-Henri Storck
IPC分类号： A61K31/04 , C07D215/38
CPC分类号： C07D215/227 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D487/08
摘要： Compounds of formula (I): wherein R1, R2, R3, R4, R5, Z and n have defined meanings, the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary ammonium salts and the stereochemically isomeric forms thereof, and their use for the treatment of PARP-mediated disorders.
摘要翻译： 式（I）化合物：其中R1，R2，R3，R4，R5，Z和n具有定义的含义，N-氧化物形式，药学上可接受的加成盐，季铵盐及其立体化学异构形式，以及它们 用于治疗PARP介导的病症。
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公开(公告)号：US20110028433A1
公开(公告)日：2011-02-03
申请号：US12934733
申请日：2009-03-26
申请人： Eddy Jean Edgard Freyne , Laurence Anne Mevellec , Jorge Eduardo Vialard , Christophe Meyer , Elisabeth Thérèse Jeanne Pasquier , Xavier Marc Bourdrez , Patrick René Angibaud
发明人： Eddy Jean Edgard Freyne , Laurence Anne Mevellec , Jorge Eduardo Vialard , Christophe Meyer , Elisabeth Thérèse Jeanne Pasquier , Xavier Marc Bourdrez , Patrick René Angibaud
IPC分类号： A61K31/517 , C07D403/06 , C07D239/80 , C07F7/10 , C07D401/06 , A61K31/695 , C07D417/06 , A61P35/00
CPC分类号： C07D239/80 , C07D401/06 , C07D417/06
摘要： The present invention provides compounds of formula (I), their use as inhibitors of tubulin polymerization as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, n, m and X have defined meanings.
摘要翻译： 本发明提供式（I）化合物，其作为微管蛋白聚合抑制剂的用途以及包含所述式（I）化合物的药物组合物，其中R1，R2，R3，R4，R5，R6，n，m和X具有 定义含义。
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公开(公告)号：US08168644B2
公开(公告)日：2012-05-01
申请号：US12934733
申请日：2009-03-26
申请人： Eddy Jean Edgard Freyne , Laurence Anne Mevellec , Jorge Eduardo Vialard , Christophe Meyer , Elisabeth Thérèse Jeanne Pasquier , Xavier Marc Bourdrez , Patrick René Angibaud
发明人： Eddy Jean Edgard Freyne , Laurence Anne Mevellec , Jorge Eduardo Vialard , Christophe Meyer , Elisabeth Thérèse Jeanne Pasquier , Xavier Marc Bourdrez , Patrick René Angibaud
IPC分类号： A01N43/54 , A61K31/517 , C07D239/72
CPC分类号： C07D239/80 , C07D401/06 , C07D417/06
摘要： The present invention provides compounds of formula (I), their use as inhibitors of tubulin polymerization as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, n, m and X have defined meanings.
摘要翻译： 本发明提供式（I）化合物，其作为微管蛋白聚合抑制剂的用途以及包含所述式（I）化合物的药物组合物，其中R1，R2，R3，R4，R5，R6，n，m和X具有 定义含义。
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6.发明申请TETRAHYDROPHENANTHRIDINONES AND TETRAHYDROCYCLOPENTAQUINOLINONES AS PARP AND TUBULIN POLYMERIZATION INHIBITORS 有权四氢萘二酮和四氢环戊二烯作为PARP和TUBULIN聚合抑制剂公开(公告)号：US20110263622A1
公开(公告)日：2011-10-27
申请号：US12934753
申请日：2009-03-26
申请人： Patrick René Angibaud , Laurence Anne Mevellec , Bruno Roux , Pierre-Henri Storck , Christophe Meyer , Jorge Eduardo Vialard
发明人： Patrick René Angibaud , Laurence Anne Mevellec , Bruno Roux , Pierre-Henri Storck , Christophe Meyer , Jorge Eduardo Vialard
IPC分类号： A61K31/506 , A61P35/00 , C07D401/10 , C07D221/12 , A61K31/473
CPC分类号： C07D401/06 , A61K31/4353 , C07D221/12
摘要： The present invention provides compounds of formula (I), their use as inhibitors of tubulin polymerization and their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7 and Y have defined meanings.
摘要翻译： 本发明提供式（I）化合物，其作为微管蛋白聚合抑制剂及其作为PARP抑制剂的用途以及包含所述式（I）化合物的药物组合物，其中R1，R2，R3，R4，R5，R6， R7和Y定义含义。
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7.发明授权Tetrahydrophenanthridinones and tetrahydrocyclopentaquinolinones as PARP and tubulin polymerization inhibitors 有权四氢苯并蒽醌和四氢环戊基喹啉酮作为PARP和微管蛋白聚合抑制剂公开(公告)号：US08889866B2
公开(公告)日：2014-11-18
申请号：US12934753
申请日：2009-03-26
申请人： Patrick René Angibaud , Laurence Anne Mevellec , Bruno Roux , Pierre-Henri Storck , Christophe Meyer , Jorge Eduardo Vialard
发明人： Patrick René Angibaud , Laurence Anne Mevellec , Bruno Roux , Pierre-Henri Storck , Christophe Meyer , Jorge Eduardo Vialard
IPC分类号： C07D221/12 , C07D401/06 , A61K31/4353
CPC分类号： C07D401/06 , A61K31/4353 , C07D221/12
摘要： The present invention provides compounds of formula (I), their use as inhibitors of tubulin polymerization and their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7 and Y have defined meanings.
摘要翻译： 本发明提供式（I）化合物，其作为微管蛋白聚合抑制剂及其作为PARP抑制剂的用途，以及包含所述式（I）化合物的药物组合物，其中R1，R2，R3，R4，R5，R6， R7和Y定义含义。
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公开(公告)号：US08778966B2
公开(公告)日：2014-07-15
申请号：US13617686
申请日：2012-09-14
申请人： Jorge Eduardo Vialard , Patrick René Angibaud , Laurence Anne Mevellec , Christophe Meyer , Eddy Jean Edgard Freyne , Isabelle Noëlle Constance Pilatte , Bruno Roux , Elisabeth Thèrése Jeanne Pasquier , Xavier Marc Bourdrez , Christophe Denis Adelinet , Laurence Françoise Bernadette Marconnet-Decrane , Jacqueline Anne Macritchie , James Edward Stewart Duffy , Andrew Pate Owens , Pierre-Henri Storck , Virginie Sophie Poncelet
发明人： Jorge Eduardo Vialard , Patrick René Angibaud , Laurence Anne Mevellec , Christophe Meyer , Eddy Jean Edgard Freyne , Isabelle Noëlle Constance Pilatte , Bruno Roux , Elisabeth Thèrése Jeanne Pasquier , Xavier Marc Bourdrez , Christophe Denis Adelinet , Laurence Françoise Bernadette Marconnet-Decrane , Jacqueline Anne Macritchie , James Edward Stewart Duffy , Andrew Pate Owens , Pierre-Henri Storck , Virginie Sophie Poncelet
IPC分类号： A61K31/04 , C07D413/06 , C07D401/06 , C07D401/12 , C07D405/06 , C07D409/06 , C07D215/227 , C07D417/06
CPC分类号： C07D215/227 , C07D401/06 , C07D401/12 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06
摘要： The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, n, m and X have defined meanings.
摘要翻译： 本发明提供式（I）化合物，它们作为PARP抑制剂的用途以及包含所述式（I）化合物的药物组合物，其中R1，R2，R3，R4，R5，R6，R7，n，m和X具有 定义含义。
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公开(公告)号：US08299256B2
公开(公告)日：2012-10-30
申请号：US12529142
申请日：2008-03-07
申请人： Jorge Eduardo Vialard , Patrick René Angibaud , Laurence Anne Mevellec , Christophe Meyer , Eddy Jean Edgard Freyne , Isabelle Noëlle Constance Pilatte , Bruno Roux , Elisabeth Thérèse Jeanne Pasquier , Xavier Marc Bourdrez , Christophe Denis Adelinet , Laurence Françoise Bernadette Marconnet-Decrane , Jacqueline Anne Macritchie , James Edward Stewart Duffy , Andrew Pate Owens , Pierre-Henri Storck , Virginie Sophie Poncelet
发明人： Jorge Eduardo Vialard , Patrick René Angibaud , Laurence Anne Mevellec , Christophe Meyer , Eddy Jean Edgard Freyne , Isabelle Noëlle Constance Pilatte , Bruno Roux , Elisabeth Thérèse Jeanne Pasquier , Xavier Marc Bourdrez , Christophe Denis Adelinet , Laurence Françoise Bernadette Marconnet-Decrane , Jacqueline Anne Macritchie , James Edward Stewart Duffy , Andrew Pate Owens , Pierre-Henri Storck , Virginie Sophie Poncelet
IPC分类号： C07D215/38
CPC分类号： C07D215/227 , C07D401/06 , C07D401/12 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06
摘要： The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, n, m and X have defined meanings.
摘要翻译： 本发明提供式（I）化合物，它们作为PARP抑制剂的用途以及包含所述式（I）化合物的药物组合物，其中R1，R2，R3，R4，R5，R6，R7，n，m和X具有 定义含义。
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公开(公告)号：US20100222348A1
公开(公告)日：2010-09-02
申请号：US12681790
申请日：2008-10-22
申请人： Patrick René Angibaud , Laurence Francoise Bernadette Marconnet-Decrane , Jorge Eduardo Vialard , Laurence Anne Mevellec , Christophe Meyer , Pierre-Henri Storck
发明人： Patrick René Angibaud , Laurence Francoise Bernadette Marconnet-Decrane , Jorge Eduardo Vialard , Laurence Anne Mevellec , Christophe Meyer , Pierre-Henri Storck
IPC分类号： A61K31/5377 , C07D215/227 , A61K31/4709 , C07D401/14 , A61K31/497 , C07D413/10 , C07D403/14 , A61K31/506 , A61P35/00 , A61P25/00 , A61P1/02 , A61P29/00 , A61P19/02 , A61P3/10 , A61P9/00 , A61P21/00 , A61P37/00 , A61P31/18
CPC分类号： C07D215/227 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D487/08
摘要： Compounds of formula (I): wherein R1, R2, R3, R4, R5, Z and n have defined meanings, the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary ammonium salts and the stereochemically isomeric forms thereof, and their use for the treatment of PARP-mediated disorders.
摘要翻译： 式（I）化合物：其中R1，R2，R3，R4，R5，Z和n具有定义的含义，N-氧化物形式，药学上可接受的加成盐，季铵盐及其立体化学异构形式，以及它们 用于治疗PARP介导的病症。
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