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1. 发明专利

JP2013018783A Bifunctional histone deacetylase inhibitor 审中-公开
标题翻译：双功能脱乙酰壳多糖酶抑制剂
公开(公告)号：JP2013018783A
公开(公告)日：2013-01-31
申请号：JP2012220357
申请日：2012-10-02
申请人： President & Fellows Of Harvard College , プレジデントアンドフェロウズオブハーバードカレッジPresident and Fellows of Harvard College , Dana-Farber Cancer Inst Inc , デイナファーバーキャンサーインスティチュート,インコーポレイテッド
发明人： BRADNER JAMES ELLIOT , MAZITSCHEK RALPH , TANG WEIPING , SCHREIBER STUART L
IPC分类号： C07C251/86 , A61K31/165 , A61K31/167 , A61K31/225 , A61K31/23 , A61K31/357 , A61K31/4045 , A61K31/422 , A61K31/435 , A61K45/00 , A61P29/00 , A61P35/00 , A61P43/00 , C07B61/00 , C07C249/16 , C07C259/06 , C07D209/14 , C07D221/14 , C07D319/06 , C07D413/12 , G01N33/15 , G01N33/50
CPC分类号： A61K31/19 , A61K31/44 , A61K47/55 , C07C259/06 , C07D249/04 , C07D249/06 , C07D413/12
摘要： PROBLEM TO BE SOLVED: To provide bifunctional histone deacetylase inhibitors.SOLUTION: 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.
摘要翻译：待解决的问题：提供双功能组蛋白脱乙酰酶抑制剂。解决方案：鉴于需要开发新的治疗剂及其有效的合成方法，本发明提供用于抑制组蛋白脱乙酰酶的新型双功能，三官能或多功能化合物及其药学上可接受的盐和衍生物。本发明还提供了治疗由组蛋白脱乙酰酶活性（例如增殖性疾病，癌症，炎性疾病，原生动物感染，脱发等）调节的病症的方法，包括向有需要的受试者施用治疗有效量的本发明化合物。本发明还提供了制备化合物的方法。版权所有（C）2013，JPO＆INPIT

2. 发明专利

JP2013100327A Histone deacetylase inhibitor 审中-公开
标题翻译： HISTONE脱乙酰基酶抑制剂
公开(公告)号：JP2013100327A
公开(公告)日：2013-05-23
申请号：JP2013008195
申请日：2013-01-21
申请人： President & Fellows Of Harvard College , プレジデントアンドフェロウズオブハーバードカレッジPresident and Fellows of Harvard College , Dana-Farber Cancer Inst Inc , デイナファーバーキャンサーインスティチュート,インコーポレイテッド
发明人： SCHREIBER STUART L , BRADNER JAMES ELLIOT , MAZITSCHEK RALPH
IPC分类号： C07C259/06 , A61K31/235 , A61K31/422 , A61P17/00 , A61P17/06 , A61P17/14 , A61P29/00 , A61P35/00 , A61P43/00 , C07B61/00 , C07D413/12
CPC分类号： A61K31/231 , A61K9/0014 , A61K31/165 , A61K31/337 , C07C235/78 , C07C259/06 , C07D319/06 , C07D413/12
摘要： PROBLEM TO BE SOLVED: To provide a compound serving as a histone deacetylase inhibitor particularly useful in treating cutaneous T-cell lymphoma, neurofibromatosis, psoriasis, hair loss, skin pigmentation, and dermatitis.SOLUTION: The compound represented by formula (I), and a pharmaceutically acceptable salt thereof are provided. In formula (I), A comprises a functional group inhibiting histone deacetylase; L is a linker moiety; and Ar is a substituted/unsubstituted aryl/heteroaryl moiety; a substituted/unsubstituted branched/unbranched aryl aliphatic/heteroaryl aliphatic moiety; a substituted/unsubstituted cyclic/heterocyclic moiety; or a substituted/unsubstituted branched/unbranched cyclic aliphatic/heterocyclic aliphatic moiety.
摘要翻译：要解决的问题：提供特别可用于治疗皮肤T细胞淋巴瘤，神经纤维瘤病，牛皮癣，脱发，皮肤色素沉着和皮炎的组蛋白脱乙酰酶抑制剂的化合物。解决方案：提供由式（I）表示的化合物及其药学上可接受的盐。在式（I）中，A包含抑制组蛋白脱乙酰酶的官能团; L是连接体部分; 并且Ar是取代/未取代的芳基/杂芳基部分; 取代/未取代的支链/非支链芳基脂族/杂芳基脂族部分; 取代/未取代的环/杂环部分; 或取代/未取代的支链/非支链环脂族/杂环脂族部分。版权所有（C）2013，JPO＆INPIT

3. 发明申请

WO2011019393A3 CLASS- AND ISOFORM-SPECIFIC HDAC INHIBITORS AND USES THEREOF 审中-公开
标题翻译：类别和ISOFORM-SPECIFIC HDAC抑制剂及其用途
公开(公告)号：WO2011019393A3
公开(公告)日：2011-06-16
申请号：PCT/US2010002220
申请日：2010-08-11
申请人： HARVARD COLLEGE , DANA FARBER CANCER INST INC , MAZITSCHEK RALPH , BRADNER JAMES ELLIOT
发明人： MAZITSCHEK RALPH , BRADNER JAMES ELLIOT
IPC分类号： C07C243/38 , A61K31/175 , A61P35/00 , C07C237/04 , C07C241/04
CPC分类号： C07C243/38 , A61K31/175 , A61K31/495 , A61K38/05 , A61K45/06 , C07D239/42 , C07D401/04 , C12Q1/48
摘要： HDAC inhibitors of the general formula (I) and (II) 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/deacetylase activity as described herein (e.g., cancer). In certain embodiments, the compounds of the invention selectively target either a class or isoform of the HDAC family. Another aspect of the invention provides an assay for determining the inhibitory effect of a test compound on an HDAC protein comprising: incubating the HDAC protein with a substrate of general formula (IIIc) in the presence of a test compound; and determining the activity of the HDAC protein.
摘要翻译：如本文所述的通式（I）和（II）的HDAC抑制剂及其药学上可接受的盐可用作组蛋白脱乙酰酶或其它脱乙酰酶的抑制剂，因此可用于治疗与乙酰酶/ 如本文所述的脱乙酰酶活性（例如，癌症）。在某些实施方案中，本发明的化合物选择性地靶向HDAC家族的类别或同种型。本发明的另一方面提供了一种用于测定测试化合物对HDAC蛋白质的抑制作用的测定法，包括：在测试化合物存在下，将HDAC蛋白质与通式（IIIc）的底物一起培养; 并测定HDAC蛋白的活性。

4. 发明公开

EP2321264A4 DEACETYLASE INHIBITORS AND USES THEREOF 有权
标题翻译： DEACETYLASEINHIBITOREN UND ANWENDUNGEN DAVON
公开(公告)号：EP2321264A4
公开(公告)日：2011-09-21
申请号：EP09800666
申请日：2009-07-22
申请人： HARVARD COLLEGE , DANA FARBER CANCER INST INC
发明人： TANG WEIPING , BRADNER JAMES ELLIOT , SCHREIBER STUART L
IPC分类号： C07C251/86 , A61K9/00 , A61K31/15 , A61P29/00 , A61P35/00
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。

5. 发明申请

WO2011084991A3 FLUORINATED HDAC INHIBITORS AND USES THEREOF 审中-公开
标题翻译：氟化HDAC抑制剂及其用途
公开(公告)号：WO2011084991A3
公开(公告)日：2013-08-29
申请号：PCT/US2011020206
申请日：2011-01-05
申请人： HARVARD COLLEGE , DANA FARBER CANCER INST INC , BRADNER JAMES ELLIOT , MAZITSCHEK RALPH
发明人： BRADNER JAMES ELLIOT , MAZITSCHEK RALPH
IPC分类号： C07D207/327 , A61K31/145 , A61P35/00 , C07C311/21
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).
摘要翻译：如本文所述的通式（I），（II）和（III）的氟化脱乙酰酶抑制剂及其药学上可接受的盐可用作组蛋白脱乙酰酶或其它脱乙酰酶的抑制剂，因此可用于治疗各种与本文所述的乙酰酶活性相关的疾病和病症（例如，癌症，神经变性疾病，炎性疾病）。

6. 发明申请

WO2010011296A3 DEACETYLASE INHIBITORS AND USES THEREOF 审中-公开
标题翻译： DEACETYLASE抑制剂及其用途
公开(公告)号：WO2010011296A3
公开(公告)日：2010-04-22
申请号：PCT/US2009004235
申请日：2009-07-22
申请人： HARVARD COLLEGE , DANA FARBER CANCER INST INC , TANG WEIPING , BRADNER JAMES ELLIOT , SCHREIBER STUART L
发明人： TANG WEIPING , BRADNER JAMES ELLIOT , SCHREIBER STUART L
IPC分类号： C07C251/86 , A61K31/15 , A61P29/00 , A61P35/00
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。

7. 发明申请

WO2007095584A3 Histone Deacetylase Inhibitors 审中-公开
标题翻译：组蛋白脱乙酰酶抑制剂
公开(公告)号：WO2007095584A3
公开(公告)日：2009-05-22
申请号：PCT/US2007062152
申请日：2007-02-14
申请人： HARVARD COLLEGE , DANA FARBER CANCER INST INC , BRADNER JAMES ELLIOT , MAZITSCHEK RALPH
发明人： BRADNER JAMES ELLIOT , MAZITSCHEK RALPH
IPC分类号： C07C309/00 , C07C233/00 , C07C235/00 , C07C327/00
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 exmaple. The present invention also provides methods for preparing compounds of the invention and intermediates thereto.
摘要翻译：鉴于需要开发新的治疗剂，本发明提供了新的组蛋白脱乙酰酶抑制剂。这些化合物包括酯键，使它们对酯酶的失活敏感。因此，这些化合物特别可用于治疗皮肤病。当化合物达到血流时，酯酶或具有酯酶活性的酶将化合物切割成具有大大降低的活性的生物活性片段或片段。理想地，这些降解产物表现出短的血清和/或全身半衰期并被快速消除。这些化合物及其药物组合物特别可用于治疗皮肤T细胞淋巴瘤，神经纤维瘤病，牛皮癣，脱发，皮肤色素沉着和皮炎。本发明还提供了制备本发明化合物及其中间体的方法。

8. 发明公开

EP3122181A4 COMPOSITIONS AND METHODS FOR EX VIVO EXPANSION OF HUMAN HEMATOPOIETIC STEM/PROGENITOR CELLS 审中-公开
公开(公告)号：EP3122181A4
公开(公告)日：2018-04-25
申请号：EP15769962
申请日：2015-03-25
申请人： THE BRIGHAM AND WOMENS HOSPITAL INC , DANA FARBER CANCER INST INC , NAT UNIV SINGAPORE
发明人： CHAI LI , TATETSU HIRO , TENEN DANIEL GEOFFREY , BRADNER JAMES ELLIOT , FEDERATION ALEXANDER
IPC分类号： A01N1/02 , A01N63/00 , A61K35/28 , A61K38/47 , C12N5/00 , C12N5/071 , C12N15/00
CPC分类号： A61K35/28 , C12N5/0647 , C12N2501/065
摘要： Described herein are methods and compositions which lead to the efficient ex vivo expansion of hematopoietic cells, such as hematopoietic stem cells (HSCs) and hematopoietic stem and progenitor cells HSPCs. Using combinations of small molecule drugs and cytokines/growth factors/grown factors targeting epigenetic status in cells, significant improvements in the expansion of cells was observed, including cells isolated from human cord blood or peripheral mobilized stem/progenitor cells. Multiple genes implicated in HSPC function were unperturbed, and efficiency of genomic editing using lentivirus was greatly enhanced following treatment. These novel approaches could be used therapeutically in a variety of hematopoietic transplantation settings, in addition to benefiting gene therapy techniques.

9. 发明公开

EP2638009A4 FLUORINATED HDAC INHIBITORS AND USES THEREOF 审中-公开
标题翻译：氟化HDAC抑制剂及其用途
公开(公告)号：EP2638009A4
公开(公告)日：2014-06-11
申请号：EP11732077
申请日：2011-01-05
申请人： HARVARD COLLEGE , DANA FARBER CANCER INST INC
发明人： BRADNER JAMES ELLIOT , MAZITSCHEK RALPH
IPC分类号： C07D207/327 , A61K31/16 , A61K31/401 , A61K31/4353 , A61K31/44 , A61P9/00 , A61P25/00 , A61P29/00 , A61P35/00 , A61P37/00 , C07C259/06 , C07C259/10 , C07C271/28 , C07D213/75 , C07D221/14 , C07D413/12
CPC分类号： C07C259/06 , C07C259/10 , C07C271/28 , C07D207/323 , C07D209/14 , C07D213/75 , C07D221/14 , C07D413/12

10. 发明公开

EP1991247A4 BIFUNCTIONAL HISTONE DEACETYLASE INHIBITORS 有权
标题翻译：双功能的组蛋白去乙酰化酶抑制剂
公开(公告)号：EP1991247A4
公开(公告)日：2011-05-11
申请号：EP07872648
申请日：2007-02-14
申请人： HARVARD COLLEGE , DANA FARBER CANCER INST INC
发明人： BRADNER JAMES ELLIOT , MAZITSCHEK RALPH , TANG WEIPING , SCHREIBER STUART L
IPC分类号： A61K38/00 , A61K31/19 , A61K31/44
CPC分类号： A61K31/19 , A61K31/44 , A61K47/55 , C07C259/06 , C07D249/04 , C07D249/06 , C07D413/12

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