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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: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: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:US20100152174A1
公开(公告)日:2010-06-17
申请号:US11720693
申请日:2005-12-08
申请人: Eddy Jean Edgard Freyne , Marc Willems , Peter Ten Holte , Alexandra Papanikos , Werner Constant John Embrechts , Pierre Henri Storck , Virginie Sophie Poncelet , Werner Constant Johan Embrechts , Pierre Henri Storck , Virginie Sophie Poncelet
发明人: Eddy Jean Edgard Freyne , Marc Willems , Peter Ten Holte , Alexandra Papanikos , Werner Constant John Embrechts , Pierre Henri Storck , Virginie Sophie Poncelet , Werner Constant Johan Embrechts , Pierre Henri Storck , Virginie Sophie Poncelet
IPC分类号: A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/517 , C07D498/04 , A61P35/00
CPC分类号: C07D498/06 , C07D498/08
摘要: The present invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z represents NH; Y represents —C3-9alkyl-, —C1-5alkyl-NR13—C1-5alkyl-, —C1-5alkyl-NR14—CO—C1-5alkyl-, —C1-2alkyl-NR21—H2—CO—NH—C1-3alkyl- or —C1-2alkyl-NR23—CO—CR16R17—NH—; X1 represents O or —O—C1-2alkyl-; X2 represents a direct bond, C1-2alkyl, —CO—C1-2alkyl or NR12—C1-2alkyl; R1 represents hydrogen or halo; R2 represents halo, acetylene or Het1; R3 represents hydrogen or cyano; R4 represents Ar4—C1-4alkyloxy-, C1-4alkyloxy- or C1-4alkyloxy substituted with one or where possible two or more substituents selected from Het2, NR7R8, hydroxy and C1-4alkyloxy-C1-4alkyloxy-; R7 represents hydrogen or C1-4alkyl; R8 represents C1-4alkyl substituted with NR25R26 or C1-4alkylsulfonyl; R12 represents hydrogen or C1-4alkyl-; R13 represents Ar6-sulfonyl or C1-6alkyloxycarbonyl optionally substituted with phenyl; R16 and R17 represents hydrogen, C1-4alkyl or R16 and R17 taken together with the carbon atom to which they are attached from a C3-6cycloalkyl; R23 represents C1-4alkyl and R23 represents hydrogen when R16 and R17 taken together with the carbon atom to which they are attached from a C3-6cycloalkyl; R25, R26, R27 and R28 each independently represent hydrogen or C1-4alkylcarbonyl; Het1 represents 2-bora-1,3-dioxolanyl; Het represents piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl or 1,1-dioxothiomorpholinyl wherein said Het2 is optionally substituted with C1-4alkyloxycarbonyl or NR27R28—C1-4alkyl; Ar4 and Ar5 represents phenyl; Ar6 represents phenyl optionally substituted with nitro.
摘要翻译: 本发明涉及式(I)化合物,N-氧化物形式,其药学上可接受的加成盐和立体化学异构形式,其中Z表示NH; Y表示-C3-9烷基,-C1-5烷基-NR13-C1-5烷基,-C1-5烷基-NR14-CO-C1-5烷基,-C1-2烷基-NR21-H2-CO-NH-C1-3烷基 - 或-C1-2烷基-NR23-CO-CR16R17-NH-; X 1表示O或-O-C 1-2烷基 - ; X2表示直接键,C1-2烷基,-CO-C1-2烷基或NR12-C1-2烷基; R1表示氢或卤素; R2代表卤代,乙炔或Het1; R3表示氢或氰基; R 4表示被一个或多个可能的两个或多个选自Het 2,NR 7 R 8,羟基和C 1-4烷氧基-C 1-4烷氧基 - 的取代基取代的Ar 4 -C 1-4烷氧基 - ,C 1-4烷氧基 - 或C 1-4烷氧基。 R7代表氢或C1-4烷基; R8表示被NR25R26或C1-4烷基磺酰基取代的C1-4烷基; R 12表示氢或C 1-4烷基 - ; R 13表示Ar 6 - 磺酰基或任选被苯基取代的C 1-6烷氧基羰基; R 16和R 17表示氢,C 1-4烷基或R 16和R 17与它们与C 3-6环烷基连接的碳原子一起; 当R 16和R 17与C 3-6环烷基连接的碳原子一起时,R 23表示C 1-4烷基,R 23表示氢; R 25,R 26,R 27和R 28各自独立地表示氢或C 1-4烷基羰基; Het1代表2-硼-1,3-二氧戊环基; Het表示哌啶基,哌嗪基,吗啉基,硫代吗啉基或1,1-二氧代硫代吗啉基,其中所述Het2任选被C 1-4烷氧基羰基或NR 27 R 28 -C 1-4烷基取代; Ar 4和Ar 5表示苯基; Ar 6表示任选被硝基取代的苯基。
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5.
公开(公告)号:US20100173913A1
公开(公告)日:2010-07-08
申请号:US12724203
申请日:2010-03-15
申请人: Eddy Jean Edgard Freyne , Marc Willems , Pierre Henri Storck , Virginie Sophie Poncelet , Kristof Van Emelen , Peter Jacobus Johannes Antonius Buijnsters , Werner Constant Johan Embrechts , Timothy Pietro Suren Perera
发明人: Eddy Jean Edgard Freyne , Marc Willems , Pierre Henri Storck , Virginie Sophie Poncelet , Kristof Van Emelen , Peter Jacobus Johannes Antonius Buijnsters , Werner Constant Johan Embrechts , Timothy Pietro Suren Perera
IPC分类号: A61K31/529 , C07D498/18 , A61P35/00 , C07D487/18
CPC分类号: C07D498/16 , C07D471/04 , C07D487/04 , C07D487/16 , C07D487/22
摘要: The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein a1-a2=a3-a4 represents a divalent radical selected from N—CH═CH—CH, N—CH═N—CH or CH—CH═N—CH; Z represents NH; Y represents —C3-9alkyl-, —C1-5alkyl-NR13—C1-5alkyl-, —C1-6alkyl-NH—CO— or —CO—NH—C1-6alkyl-; X1 represents —O— or —NR11—; X2 represents —C1-2alkyl-, —O—C1-2alkyl, —O— or —O—CH2—; R1 represents hydrogen or halo; R2 represents hydrogen, cyano, halo, hydroxycarbonyl-, C1-4alkyloxycarbonyl-, Het16-carbonyl- or Ar5; R3 represents hydrogen; R4 represents hydroxy, C1-4alkyloxy-, Ar4—C1-4alkyloxy or R4 represents C1-4alkyloxy substituted with one or where possible two or more substituents selected from C1-4alkyloxy- or Het2-; R11 represents hydrogen; R12 represents hydrogen, C1-4alkyl- or C1-4alkyl-oxy-carbonyl-; R13 represents Het14-C1-4alkyl, in particular morpholinyl-C1-4alkyl; Het2 represents a heterocycle selected from morpholinyl or piperidinyl optionally substituted with C1-4alkyl-, preferably methyl; Het14 represents morpholinyl; Het16 represents a heterocycle selected from morpholinyl or pyrrolidinyl; Ar4 represents phenyl; Ar5 represents phenyl optionally substituted with cyano.
摘要翻译: 本发明涉及N-氧化物形式的化合物,其药学上可接受的加成盐和立体化学异构体,其中a1-a2 = a3-a4表示选自N-CH = CH-CH,N- CH = N-CH或CH-CH = N-CH; Z表示NH; Y表示-C3-9烷基 - ,-C1-5烷基-NR13-C1-5烷基 - ,C1-6烷基-NH-CO-或-CO-NH-C1-6烷基 - ; X1表示-O-或-NR11-; X2表示-C1-2烷基 - , - O-C1-2烷基,-O-或-O-CH2-; R1表示氢或卤素; R 2表示氢,氰基,卤素,羟基羰基 - ,C 1-4烷氧基羰基 - ,Het 16 - 羰基 - 或Ar 5; R3表示氢; R 4表示羟基,C 1-4烷氧基 - ,Ar 4 -C 1-4烷氧基或R 4表示被一个或多个可能的两个或多个选自C 1-4烷氧基或Het 2-的取代基取代的C 1-4烷氧基; R11表示氢; R 12表示氢,C 1-4烷基 - 或C 1-4烷基 - 氧基 - 羰基 - ; R13表示Het14-C1-4烷基,特别是吗啉基-C 1-4烷基; Het2表示选自任选被C 1-4烷基,优选甲基取代的吗啉基或哌啶基的杂环; Het14代表吗啉基; Het16表示选自吗啉基或吡咯烷基的杂环; Ar4表示苯基; Ar 5表示任选被氰基取代的苯基。
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6.
公开(公告)号:US08772272B2
公开(公告)日:2014-07-08
申请号:US12724203
申请日:2010-03-15
申请人: Eddy Jean Edgard Freyne , Marc Willems , Pierre Henri Storck , Virginie Sophie Poncelet , Kristof Van Emelen , Peter Jacobus Johnnes Antonius Buijnsters , Werner Constant Johan Embrechts , Timothy Pietro Suren Perera
发明人: Eddy Jean Edgard Freyne , Marc Willems , Pierre Henri Storck , Virginie Sophie Poncelet , Kristof Van Emelen , Peter Jacobus Johnnes Antonius Buijnsters , Werner Constant Johan Embrechts , Timothy Pietro Suren Perera
IPC分类号: A61K31/33 , A61K31/519 , C07D487/00 , C07D487/18
CPC分类号: C07D498/16 , C07D471/04 , C07D487/04 , C07D487/16 , C07D487/22
摘要: The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein a1-a2=a3-a4 represents a divalent radical selected from N—CH═CH—CH, N—CH═N—CH or CH—CH═N—CH; Z represents NH; Y represents —C3-9alkyl-, —C1-5alkyl-NR13—C1-5alkyl-, —C1-6alkyl-NH—CO— or —CO—NH—C1-6alkyl-; X1 represents —O— or —NR11—; X2 represents —C1-2alkyl-, —O—C1-2alkyl, —O— or —O—CH2—; R1 represents hydrogen or halo; R2 represents hydrogen, cyano, halo, hydroxycarbonyl-, C1-4alkyloxycarbonyl-, Het16-carbonyl- or Ar5; R3 represents hydrogen; R4 represents hydroxy, C1-4alkyloxy-, Ar4—C1-4alkyloxy or R4 represents C1-4alkyloxy substituted with one or where possible two or more substituents selected from C1-4alkyloxy- or Het2-; R11 represents hydrogen; R12 represents hydrogen, C1-4alkyl- or C1-4alkyl-oxy-carbonyl-; R13 represents Het14-C1-4alkyl, in particular morpholinyl-C1-4alkyl; Het2 represents a heterocycle selected from morpholinyl or piperidinyl optionally substituted with C1-4alkyl-, preferably methyl; Het14 represents morpholinyl; Het16 represents a heterocycle selected from morpholinyl or pyrrolidinyl; Ar4 represents phenyl; Ar5 represents phenyl optionally substituted with cyano.
摘要翻译: 本发明涉及N-氧化物形式的化合物,其药学上可接受的加成盐和立体化学异构体,其中a1-a2 = a3-a4表示选自N-CH = CH-CH,N- CH = N-CH或CH-CH = N-CH; Z表示NH; Y表示-C3-9烷基 - ,-C1-5烷基-NR13-C1-5烷基 - ,C1-6烷基-NH-CO-或-CO-NH-C1-6烷基 - ; X1表示-O-或-NR11-; X2表示-C1-2烷基 - , - O-C1-2烷基,-O-或-O-CH2-; R1表示氢或卤素; R 2表示氢,氰基,卤素,羟基羰基 - ,C 1-4烷氧基羰基 - ,Het 16 - 羰基 - 或Ar 5; R3表示氢; R 4表示羟基,C 1-4烷氧基 - ,Ar 4 -C 1-4烷氧基或R 4表示被一个或多个可能的两个或多个选自C 1-4烷氧基或Het 2-的取代基取代的C 1-4烷氧基; R11表示氢; R 12表示氢,C 1-4烷基 - 或C 1-4烷基 - 氧基 - 羰基 - ; R13表示Het14-C1-4烷基,特别是吗啉基-C 1-4烷基; Het2表示选自任选被C 1-4烷基,优选甲基取代的吗啉基或哌啶基的杂环; Het14代表吗啉基; Het16表示选自吗啉基或吡咯烷基的杂环; Ar4表示苯基; Ar 5表示任选被氰基取代的苯基。
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7.
公开(公告)号:US07799772B2
公开(公告)日:2010-09-21
申请号:US10596512
申请日:2004-12-15
申请人: Eddy Jean Edgard Freyne , Pierre Henri Storck , Virginie Sophie Poncelet , Timothy Pietro Suren Perera
发明人: Eddy Jean Edgard Freyne , Pierre Henri Storck , Virginie Sophie Poncelet , Timothy Pietro Suren Perera
IPC分类号: A01N43/00 , A61K31/33 , C07D225/00 , C07D295/00
CPC分类号: C07D498/16 , C07D471/04 , C07D487/04 , C07D487/16 , C07D487/22
摘要: The present invention concerns the compounds of formula wherein a1-a2=a3-a4 represents a divalent radical selected from N—CH═CH—CH, N—CH═N—CH or CH—CH═N—CH; Z represents NH; Y represents —C3-9alkyl-, —C1-5alkyl-NR13—C1-5alkyl-, —C1-6alkyl-NH—CO— or —CO—NH—C1-6alkyl-; X1 represents —O— or —NR11—; X2 represents —C1-2alkyl-, —O—C1-2alkyl, —O— or —O—CH2—; R1 represents hydrogen or halo; R2 represents hydrogen, cyano, halo, hydroxycarbonyl-, C1-4alkyloxycarbonyl-, Het16-carbonyl- or Ar5; R3 represents hydrogen; R4 represents hydroxy, C1-4alkyloxy-, Ar4—C1-4alkyloxy or R4 represents C1-4alkyloxy substituted with one or where possible two or more substituents selected from C1-4alkyloxy- or Het2-; R11 represents hydrogen; R12 represents hydrogen, C1-4alkyl- or C1-4alkyl-oxy-carbonyl-; R13 represents Het14-C1-4alkyl, in particular morpholinyl-C1-4alkyl; Het2 represents a heterocycle selected from morpholinyl or piperidinyl optionally substituted with C1-4alkyl-, preferably methyl; Het14 represents morpholinyl; Het16 represents a heterocycle selected from morpholinyl or pyrrolidinyl; Ar4 represents phenyl; Ar5 represents phenyl optionally substituted with cyano.
摘要翻译: 本发明涉及下式的化合物:其中a 1-a 2 = a 3-a 4表示选自N-CH = CH,N-CH = N-CH或CH-CH = N-CH的二价基团; Z表示NH; Y表示-C3-9烷基 - ,-C1-5烷基-NR13-C1-5烷基 - ,C1-6烷基-NH-CO-或-CO-NH-C1-6烷基 - ; X1表示-O-或-NR11-; X2表示-C1-2烷基 - , - O-C1-2烷基,-O-或-O-CH2-; R1表示氢或卤素; R 2表示氢,氰基,卤素,羟基羰基 - ,C 1-4烷氧基羰基 - ,Het 16 - 羰基 - 或Ar 5; R3表示氢; R 4表示羟基,C 1-4烷氧基 - ,Ar 4 -C 1-4烷氧基或R 4表示被一个或多个可能的两个或多个选自C 1-4烷氧基或Het 2-的取代基取代的C 1-4烷氧基; R11表示氢; R 12表示氢,C 1-4烷基 - 或C 1-4烷基 - 氧基 - 羰基 - ; R13表示Het14-C1-4烷基,特别是吗啉基-C 1-4烷基; Het2表示选自任选被C 1-4烷基,优选甲基取代的吗啉基或哌啶基的杂环; Het14代表吗啉基; Het16表示选自吗啉基或吡咯烷基的杂环; Ar4表示苯基; Ar 5表示任选被氰基取代的苯基。
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公开(公告)号:US08097611B2
公开(公告)日:2012-01-17
申请号:US12759256
申请日:2010-04-13
申请人: Kristof Van Emelen , Janine Arts , Leo-Jacobus Jozef Backx , Hans Louis Jos De Winter , Sven Franciscus Anna Van Brandt , Marc Gustaaf Celine Verdonck , Lieven Meerpoel , Isabelle Noëlle Constance Pilatte , Virginie Sophie Poncelet , Alexey Borisovich Dyatkin , Jimmy Arnold Viviane Van heusden
发明人: Kristof Van Emelen , Janine Arts , Leo-Jacobus Jozef Backx , Hans Louis Jos De Winter , Sven Franciscus Anna Van Brandt , Marc Gustaaf Celine Verdonck , Lieven Meerpoel , Isabelle Noëlle Constance Pilatte , Virginie Sophie Poncelet , Alexey Borisovich Dyatkin , Jimmy Arnold Viviane Van heusden
IPC分类号: A61K31/551 , A61K31/5377 , A61K31/506 , A61K31/496 , C07D243/08 , C07D413/14 , C07D403/04 , C07D295/26
CPC分类号: C07D413/12 , A61K31/40 , A61K31/402 , A61K31/435 , A61K31/4427 , A61K31/454 , A61K31/4545 , A61K31/472 , A61K31/495 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D207/09 , C07D207/14 , C07D207/277 , C07D207/28 , C07D211/14 , C07D211/58 , C07D213/78 , C07D213/81 , C07D213/82 , C07D217/02 , C07D217/04 , C07D217/16 , C07D233/90 , C07D239/42 , C07D241/04 , C07D241/24 , C07D243/08 , C07D261/10 , C07D295/155 , C07D295/22 , C07D295/26 , C07D307/68 , C07D307/79 , C07D333/34 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/06 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/14 , C07D471/04 , C07D471/10 , C07D513/04 , C12Q1/34 , C12Q1/48 , G01N33/573 , G01N2333/91
摘要: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
摘要翻译: 本发明包括式(I)的新化合物,其中n,m,t,R 1,R 2,R 3,R 4,L,Q,X,Y,Z具有定义的含义,具有组蛋白脱乙酰酶抑制酶活性; 其制剂,含有它们的组合物及其作为药物的用途。
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公开(公告)号:US08524711B2
公开(公告)日:2013-09-03
申请号:US13471579
申请日:2012-05-15
IPC分类号: A61P35/00 , A61K31/535 , C07D413/00
CPC分类号: C07D413/12 , A61K31/40 , A61K31/402 , A61K31/435 , A61K31/4427 , A61K31/454 , A61K31/4545 , A61K31/472 , A61K31/495 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D207/09 , C07D207/14 , C07D211/14 , C07D211/58 , C07D213/78 , C07D217/02 , C07D217/04 , C07D217/16 , C07D239/42 , C07D295/155 , C07D295/26 , C07D307/68 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/06 , C07D409/12 , C07D409/14 , C07D413/04 , C07D471/04 , C07D471/10 , C07D513/04 , C12Q1/34 , C12Q1/48
摘要: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
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公开(公告)号:US20100240639A1
公开(公告)日:2010-09-23
申请号:US12759256
申请日:2010-04-13
申请人: Kristof Van Emelen , Janine Arts , Leo-Jacobus Jozef Backx , Hans Louis Jos De Winter , Sven Franciscus Anna Van Brandt , Mac Gustaaf Celine Verdonck , Lieven Meerpoel , Isabelle Noëlle Constance Pilatte , Virginie Sophie Poncelet , Alexey Borisovich Dyatkin , Jimmy Arnold Viviane Van heusden
发明人: Kristof Van Emelen , Janine Arts , Leo-Jacobus Jozef Backx , Hans Louis Jos De Winter , Sven Franciscus Anna Van Brandt , Mac Gustaaf Celine Verdonck , Lieven Meerpoel , Isabelle Noëlle Constance Pilatte , Virginie Sophie Poncelet , Alexey Borisovich Dyatkin , Jimmy Arnold Viviane Van heusden
IPC分类号: A61K31/551 , C12Q1/34 , A61K31/5377 , A61K31/506 , A61K31/501 , A61K31/496 , A61K31/495 , C07D243/08 , C07D413/14 , C07D403/04 , C07D403/12 , C07D295/26
CPC分类号: C07D413/12 , A61K31/40 , A61K31/402 , A61K31/435 , A61K31/4427 , A61K31/454 , A61K31/4545 , A61K31/472 , A61K31/495 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D207/09 , C07D207/14 , C07D207/277 , C07D207/28 , C07D211/14 , C07D211/58 , C07D213/78 , C07D213/81 , C07D213/82 , C07D217/02 , C07D217/04 , C07D217/16 , C07D233/90 , C07D239/42 , C07D241/04 , C07D241/24 , C07D243/08 , C07D261/10 , C07D295/155 , C07D295/22 , C07D295/26 , C07D307/68 , C07D307/79 , C07D333/34 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/06 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/14 , C07D471/04 , C07D471/10 , C07D513/04 , C12Q1/34 , C12Q1/48 , G01N33/573 , G01N2333/91
摘要: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
摘要翻译: 本发明包括式(I)的新化合物,其中n,m,t,R 1,R 2,R 3,R 4,L,Q,X,Y,Z具有定义的含义,具有组蛋白脱乙酰酶抑制酶活性; 其制剂,含有它们的组合物及其作为药物的用途。
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