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1. 发明申请

WO2008013569A2 SMALL MOLECULE PRINTING 审中-公开
标题翻译：小分子印刷
公开(公告)号：WO2008013569A2
公开(公告)日：2008-01-31
申请号：PCT/US2007000003
申请日：2007-01-03
申请人： HARVARD COLLEGE , DANA FARBER CANCER INST INC , BARNES DAVID W , KOEHLER ANGELA N , BRADNER JAMES E , MAZITSCHEK RALPH , SCHREIBER STUART L
发明人： BARNES DAVID W , KOEHLER ANGELA N , BRADNER JAMES E , MAZITSCHEK RALPH , SCHREIBER STUART L
IPC分类号： C40B40/04
CPC分类号： G01N33/6803 , B01J19/0046 , B01J2219/00527 , B01J2219/00605 , B01J2219/00626 , B01J2219/00659 , B01J2219/0072 , B01J2219/0074 , C40B30/04 , C40B40/04 , C40B80/00 , G01N33/50 , G01N33/53 , G01N33/543 , G01N33/54353 , G01N33/547 , G01N33/552 , G01N33/553
摘要： The present invention provides compositions and methods to facilitate the identification of compounds that are capable of interacting with a biological macromolecule of interest. In one aspect, a composition is provided that comprises an array of one or more types of chemical compounds attached to a solid support using isocyanate or isothiocyanate chemistry, wherein the density of the array of compounds is at least 1000 spots per cm 2 . In general, these inventive arrays are generated by: (1) providing a solid support, wherein said solid support is functionalized with an isocyanate or isothiocyanate moiety capable of interacting with a desired chemical compound to form a covalent attachment; (2) providing one or more solutions of one or more types of compounds to be attached to the solid support; (3) delivering said one or more types of compounds to the solid support; and (4) catalyzing the attachment of the compound to the solid support, whereby an array is formed and the array of compounds has a density of at least 1000 spots per cm 2 . In another aspect, the present invention provides methods for utilizing these arrays to identify small molecule partners for biological macromolecules of interest.
摘要翻译：本发明提供了有助于鉴定能够与感兴趣的生物大分子相互作用的化合物的组合物和方法。在一个方面，提供了一种组合物，其包含使用异氰酸酯或异硫氰酸酯化学连接到固体支持物上的一种或多种类型的化合物的阵列，其中化合物阵列的密度为至少1000个点/ cm 2 。通常，这些本发明的阵列通过以下方式产生：（1）提供固体支持物，其中所述固体支持物用能够与所需化学化合物相互作用以形成共价连接的异氰酸酯或异硫氰酸酯部分官能化; （2）提供待连接到固体支持物上的一种或多种类型化合物的一种或多种溶液; （3）将所述一种或多种类型的化合物递送至固体支持物; 和（4）催化化合物与固体支持物的连接，从而形成阵列，化合物阵列的密度至少为1000个/ cm 2。在另一方面，本发明提供了利用这些阵列鉴定感兴趣的生物大分子的小分子伴侣的方法。

2. 发明申请

WO2006102557A2 TREATMENT OF PROTEIN DEGRADATION DISORDERS 审中-公开
标题翻译：治疗蛋白质降解病
公开(公告)号：WO2006102557A2
公开(公告)日：2006-09-28
申请号：PCT/US2006010676
申请日：2006-03-22
申请人： HARVARD COLLEGE , DANA FARBER CANCER INST INC , ANDERSON KENNETH C , BRADNER JAMES ELLIOTT , GREENBERG EDWARD FRANKLIN , HIDESHIMA TERU , KWIATKOWSKI NICHOLAS PAUL , MAZITSCHEK RALPH , SCHREIBER STUART L , SHAW JARED
发明人： ANDERSON KENNETH C , BRADNER JAMES ELLIOTT , GREENBERG EDWARD FRANKLIN , HIDESHIMA TERU , KWIATKOWSKI NICHOLAS PAUL , MAZITSCHEK RALPH , SCHREIBER STUART L , SHAW JARED
IPC分类号： A61K51/00 , A61K33/36 , A61K39/395
CPC分类号： A61K38/05 , A61K31/35 , A61K31/357 , A61K31/422 , A61K31/4965 , A61K31/69 , A61K38/50 , A61K45/06 , A61K49/0008 , G01N33/5011 , A61K2300/00
摘要： The invention relates to methods of treating protein degradation disorders, such cellular proliferative disorders (e.g., cancer) and protein deposition disorders (e.g., neurodegenerative disorders). The invention provides methods and pharmaceutical compositions for treating these diseases using aggresome inhibitors or combinations of aggresome inhibitors and proteasome inhibitors. The invention further relates to methods and pharmaceutical compositions for treating multiple myeloma. New HDAC/TDAC inhibitors and aggresome inhibitors are also provided as well as synthetic methodologies for preparing these compounds.
摘要翻译：本发明涉及治疗蛋白质降解病症，细胞增殖性疾病（例如癌症）和蛋白沉积病症（例如神经变性疾病）的方法。本发明提供了使用聚集抑制剂或聚集抑制剂和蛋白酶体抑制剂的组合治疗这些疾病的方法和药物组合物。本发明还涉及用于治疗多发性骨髓瘤的方法和药物组合物。还提供了新的HDAC / TDAC抑制剂和聚集抑制剂以及制备这些化合物的合成方法。

3. 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

4. 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

5. 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。

6. 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）。

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. 发明专利

JP2013053157A Treatment of protein degradation disorder 审中-公开
标题翻译：蛋白质降解异常的治疗
公开(公告)号：JP2013053157A
公开(公告)日：2013-03-21
申请号：JP2012266681
申请日：2012-12-05
申请人： President & Fellows Of Harvard College , プレジデントアンドフェローズオブハーバードカレッジ , 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： ANDERSON KENNETH C , BRADNER JAMES ELLIOTT , GREENBERG EDWARD FRANKLIN , HIDESHIMA TERU , KWIATKOWSKI NICHOLAS PAUL , MAZITSCHEK RALPH , SCHREIBER STUART L , SHAW JARED , HAGGARTY STEPHEN J
IPC分类号： A61K45/00 , A61K31/357 , A61K31/422 , A61K31/428 , A61K31/4433 , A61K31/69 , A61K45/06 , A61P1/16 , A61P11/00 , A61P15/00 , A61P21/00 , A61P25/00 , A61P25/14 , A61P25/28 , A61P35/00 , A61P35/02 , A61P43/00 , C07D319/06 , C07D405/12 , C07D413/12 , C07D417/12 , C12N9/48 , C12N15/09 , C12Q1/02 , G01N33/15 , G01N33/50
CPC分类号： A61K38/05 , A61K31/35 , A61K31/357 , A61K31/422 , A61K31/4965 , A61K31/69 , A61K38/50 , A61K45/06 , A61K49/0008 , G01N33/5011 , A61K2300/00
摘要： PROBLEM TO BE SOLVED: To provide treatments for protein degradation disorders.SOLUTION: The invention relates to methods for treating protein degradation disorders, such cellular proliferative disorders (e.g. cancer) and protein deposition disorders (e.g. neurodegenerative disorders). The invention provides methods and pharmaceutical compositions for treating these diseases using aggresome inhibitors or combinations of aggresome inhibitors and proteasome inhibitors. The invention further relates to methods and pharmaceutical compositions for treating multiple myeloma. New HDAC/TDAC inhibitors and aggresome inhibitors are also provided as well as synthetic methodologies for preparing these compounds.
摘要翻译：要解决的问题：提供蛋白质降解障碍的治疗。解决方案：本发明涉及治疗蛋白质降解病症，例如细胞增殖性疾病（例如癌症）和蛋白沉积病症（例如神经变性疾病）的方法。本发明提供了使用聚集抑制剂或聚集抑制剂和蛋白酶体抑制剂的组合来治疗这些疾病的方法和药物组合物。本发明还涉及用于治疗多发性骨髓瘤的方法和药物组合物。还提供了新的HDAC / TDAC抑制剂和聚集抑制剂以及用于制备这些化合物的合成方法。版权所有（C）2013，JPO＆INPIT

9. 发明申请

WO2012112447A3 HISTONE DEACETYLASE INHIBITORS AND METHODS OF USE THEREOF 审中-公开
标题翻译： HISTONE DEACETYLASE抑制剂及其使用方法
公开(公告)号：WO2012112447A3
公开(公告)日：2012-12-27
申请号：PCT/US2012024868
申请日：2012-02-13
申请人： DANA FARBER CANCER INST INC , MAZITSCHEK RALPH , BRADNER JAMES ELLIOTT , GRACHAN MELISSA
发明人： MAZITSCHEK RALPH , BRADNER JAMES ELLIOTT , GRACHAN MELISSA
IPC分类号： C07C69/76 , A61K31/165 , A61P29/00 , C07C215/28
CPC分类号： C07C259/10 , A61K31/165 , C07C69/732 , C07C69/734 , C07C259/06 , C07D213/81 , C07D333/38
摘要： The present invention provides novel 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 a compound of the invention to a subject in need thereof. The present invention also provides methods for preparing compounds of the invention.
摘要翻译：本发明提供了用于抑制组蛋白脱乙酰酶的新化合物及其药学上可接受的盐和衍生物。本发明进一步提供了用于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，其包括向受试者施用治疗有效量的本发明化合物需要它。本发明还提供了制备本发明化合物的方法。

10. 发明申请

WO2012112447A9 HISTONE DEACETYLASE INHIBITORS AND METHODS OF USE THEREOF 审中-公开
标题翻译：组织脱乙酰酶抑制剂及其使用方法
公开(公告)号：WO2012112447A9
公开(公告)日：2012-10-18
申请号：PCT/US2012024868
申请日：2012-02-13
申请人： DANA FARBER CANCER INST INC , MAZITSCHEK RALPH , BRADNER JAMES ELLIOTT , GRACHAN MELISSA
发明人： MAZITSCHEK RALPH , BRADNER JAMES ELLIOTT , GRACHAN MELISSA
IPC分类号： C07C69/76 , A61K31/165 , A61P29/00 , C07C215/28
CPC分类号： C07C259/10 , A61K31/165 , C07C69/732 , C07C69/734 , C07C259/06 , C07D213/81 , C07D333/38
摘要： The present invention provides novel 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 a compound of the invention to a subject in need thereof. The present invention also provides methods for preparing compounds of the invention.
摘要翻译：本发明提供抑制组蛋白脱乙酰酶的新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，其包括向受治疗者施用治疗有效量的本发明化合物需要。本发明还提供了制备本发明化合物的方法。

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