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公开(公告)号：EP2321264A2
公开(公告)日：2011-05-18
申请号：EP09800666.1
申请日：2009-07-22
IPC分类号： C07C251/86 , A61K31/15 , A61P35/00 , A61P29/00
CPC分类号： C07C259/06 , C07C251/86
摘要： The present invention provides novel compounds of formula (I) and pharmaceutical compositions thereof. The inventive compounds are useful as deacetylase inhibitors (e.g., histone deacetylase inhibitors) and may be useful in the treatment of proliferative diseases such as cancer. In particular, the inventive compounds are HDAC6 inhibitors. The invention also provide synthetic methods for preparing the inventive compounds.
摘要翻译： 本发明提供了新的式（I）化合物及其药物组合物。 本发明的化合物可用作脱乙酰酶抑制剂（例如组蛋白脱乙酰酶抑制剂）并可用于治疗增殖性疾病如癌症。 特别地，本发明的化合物是HDAC6抑制剂。 本发明还提供了用于制备本发明化合物的合成方法。
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公开(公告)号：EP1991247A1
公开(公告)日：2008-11-19
申请号：EP07872648.6
申请日：2007-02-14
CPC分类号： A61K31/19 , A61K31/44 , A61K47/55 , C07C259/06 , C07D249/04 , C07D249/06 , C07D413/12
摘要： In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel bifunctional, trifunctional, or multifunctional compounds for inhibiting histone deacetylases, and pharmaceutically acceptable salts and derivatives thereof. The present invention further provides methods for treating disorders regulated by histone deacetylase activity (e.g., proliferative diseases, cancer, inflammatory diseases, protozoal infections, hair loss, etc.) comprising administering a therapeutically effective amount of an inventive compound to a subject in need thereof. The present invention also provides methods for preparing compounds of the invention.
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公开(公告)号：EP1991247B1
公开(公告)日：2015-10-14
申请号：EP07872648.6
申请日：2007-02-14
IPC分类号： C07C259/06 , C07D413/12 , C07D249/04 , C07D249/06
CPC分类号： A61K31/19 , A61K31/44 , A61K47/55 , C07C259/06 , C07D249/04 , C07D249/06 , C07D413/12
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公开(公告)号：EP2321264B1
公开(公告)日：2016-05-04
申请号：EP09800666.1
申请日：2009-07-22
IPC分类号： C07C259/06 , C07C251/86
CPC分类号： C07C259/06 , C07C251/86
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公开(公告)号：EP2638009A2
公开(公告)日：2013-09-18
申请号：EP11732077.0
申请日：2011-01-05
IPC分类号： C07D207/327
CPC分类号： C07C259/06 , C07C259/10 , C07C271/28 , C07D207/323 , C07D209/14 , C07D213/75 , C07D221/14 , C07D413/12
摘要： Fluorinated deacetylase inhibitors of the general formulae (I), (II), and (III): and pharmaceutically acceptable salts thereof, as described herein, are useful as inhibitors of histone deacetylases or other deacetylases, and thus are useful for the treatment of various diseases and disorders associated with acetylase activity as described herein (
e.g. , cancer, neurodegenerative diseases, inflammatory diseases).-
公开(公告)号：EP2010168B1
公开(公告)日：2014-04-16
申请号：EP07757000.0
申请日：2007-02-14
IPC分类号： C07C259/06 , C07D413/12
CPC分类号： A61K31/231 , A61K9/0014 , A61K31/165 , A61K31/337 , C07C235/78 , C07C259/06 , C07D319/06 , C07D413/12
摘要： In recognition of the need to develop novel therapeutic agents, the present invention provides novel histone deacetylase inhibitors. These compounds include an ester bond making them sensitive to deactivation by esterases. Therefore, these compounds are particularly useful in the treatment of skin disorders. When the compounds reaches the bloodstream, an esterase or an enzyme with esterase activity cleaves the compound into biologically inactive fragments or fragments with greatly reduced activity Ideally these degradation products exhibit a short serum and/or systemic half-life and are eliminated rapidly. These compounds and pharmaceutical compositions thereof are particularly useful in treating cutaneous T-cell lymphoma, neurofibromatosis, psoriasis, hair loss, skin pigmentation, and dermatitis, for example. The present invention also provides methods for preparing compounds of the invention and intermediates thereto.
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公开(公告)号：EP2010168A2
公开(公告)日：2009-01-07
申请号：EP07757000.0
申请日：2007-02-14
IPC分类号： A61K31/19
CPC分类号： A61K31/231 , A61K9/0014 , A61K31/165 , A61K31/337 , C07C235/78 , C07C259/06 , C07D319/06 , C07D413/12
摘要： In recognition of the need to develop novel therapeutic agents, the present invention provides novel histone deacetylase inhibitors. These compounds include an ester bond making them sensitive to deactivation by esterases. Therefore, these compounds are particularly useful in the treatment of skin disorders. When the compounds reaches the bloodstream, an esterase or an enzyme with esterase activity cleaves the compound into biologically inactive fragments or fragments with greatly reduced activity Ideally these degradation products exhibit a short serum and/or systemic half-life and are eliminated rapidly. These compounds and pharmaceutical compositions thereof are particularly useful in treating cutaneous T-cell lymphoma, neurofibromatosis, psoriasis, hair loss, skin pigmentation, and dermatitis, for example. The present invention also provides methods for preparing compounds of the invention and intermediates thereto.
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