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1.
公开(公告)号:US07709487B2
公开(公告)日:2010-05-04
申请号:US11668906
申请日:2007-01-30
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 Noelle 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 Noelle Constance Pilatte , Virginie Sophie Poncelet , Alexey Borisovich Dyatkin , Jimmy Arnold Viviane Van heusden
IPC分类号: A61K31/506 , C07D403/04
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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2.
公开(公告)号:US08865720B2
公开(公告)日:2014-10-21
申请号:US14053119
申请日:2013-10-14
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 Noelle 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 Noelle Constance Pilatte , Virginie Sophie Poncelet , Alexey Borisovich Dyatkin , Jimmy Arnold Viviane Van Heusden
IPC分类号: C07D207/28 , C07D409/04 , C07D213/82 , C07D233/90 , C07D413/14 , C07D307/79 , C07D213/81 , C07D243/08 , G01N33/573 , C07D333/34 , A61K31/495 , C07D295/22 , A61K45/06 , C07D241/24 , C07D403/04 , C07D239/42 , A61K31/496 , C07D241/04 , C07D295/26 , C07D207/277 , C07D261/10
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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3.
公开(公告)号:US07704998B2
公开(公告)日:2010-04-27
申请号:US11926759
申请日:2007-10-29
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 Noelle 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 Noelle Constance Pilatte , Virginie Sophie Poncelet , Alexey Borisovich Dyatkin , Jimmy Arnold Viviane Van heusden
IPC分类号: A61K31/551 , A61K31/495 , C07D241/04 , C07D403/04 , C07D413/14
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: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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5.
公开(公告)号:US07205304B2
公开(公告)日:2007-04-17
申请号:US10507708
申请日:2003-03-11
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: A61K31/497 , C07D403/04 , C07D239/69
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: 本发明包括新的式(I)化合物,其中n,m,t,R 1,R 2,R 3,R 3, 具有组氨酸脱乙酰酶抑制酶活性的含义; 其制剂,含有它们的组合物及其作为药物的用途
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6.
公开(公告)号:US20140038979A1
公开(公告)日:2014-02-06
申请号:US14053119
申请日:2013-10-14
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 Noelle Constance Pilatte , Virginie Sophie Poncelet , Alexey Borisovich Dyatkin , Jimmy Arnold Viviene 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 Noelle Constance Pilatte , Virginie Sophie Poncelet , Alexey Borisovich Dyatkin , Jimmy Arnold Viviene Van Heusden
IPC分类号: C07D295/26 , A61K31/496 , A61K31/495 , C07D241/24 , C07D409/04 , A61K45/06 , C07D261/10 , C07D233/90 , C07D207/277 , C07D307/79 , C07D333/34 , G01N33/573 , C07D213/81
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: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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8.
公开(公告)号:US08557825B2
公开(公告)日:2013-10-15
申请号:US13325330
申请日:2011-12-14
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 Viviene 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 Viviene Van heusden
IPC分类号: A61K31/496 , 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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9.
公开(公告)号:US20120088754A1
公开(公告)日:2012-04-12
申请号:US13325330
申请日:2011-12-14
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 Viviene 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 Viviene Van heusden
IPC分类号: A61K31/551 , C07D295/26 , A61K31/495 , C07D403/12 , A61K31/496 , C07D403/04 , A61K31/506 , C07D413/14 , A61K31/5377 , A61K31/501 , A61K31/497 , C07D403/14 , C07D409/14 , C07D405/14 , G01N33/573 , A61P35/00 , A61P17/06 , C07D243/08
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: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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