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1. 发明申请

WO2011091213A3 REVERSE AMIDE COMPOUNDS AS PROTEIN DEACETYLASE INHIBITORS AND METHODS OF USE THEREOF 审中-公开
标题翻译：反式酰胺化合物作为蛋白质脱乙酰酶抑制剂及其使用方法
公开(公告)号：WO2011091213A3
公开(公告)日：2011-12-01
申请号：PCT/US2011021982
申请日：2011-01-21
申请人： ACETYLON PHARMACEUTICALS , VAN DUZER JOHN H , MAZITSCHEK RALPH , OGIER WALTER , BRADNER JAMES ELLIOTT , HUANG GUOXIANG , XIE DEJIAN , YU NAN
发明人： VAN DUZER JOHN H , MAZITSCHEK RALPH , OGIER WALTER , BRADNER JAMES ELLIOTT , HUANG GUOXIANG , XIE DEJIAN , YU NAN
IPC分类号： C07D239/42 , A61K31/505 , A61P25/00 , A61P35/00 , C07C233/78
CPC分类号： A61K31/505 , A61K31/164 , A61K31/337 , A61K45/06 , C07C237/36 , C07C259/06 , C07D209/46 , C07D209/48 , C07D213/30 , C07D213/74 , C07D213/81 , C07D235/30 , C07D239/42 , C07D241/20 , C07D263/58 , C07D277/24 , C07D277/82 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D413/04 , C07D417/06
摘要： The present invention relates to novel "reverse amide" compounds comprising a zinc chelator group, and the use of such compounds in the inhibition of HDAC6 and in the treatment of various diseases, disorders or conditions related to HDAC6.
摘要翻译：本发明涉及包含锌螯合剂基团的新型“反向酰胺”化合物，以及这些化合物在抑制HDAC6和治疗与HDAC6相关的各种疾病，病症或病症中的用途。

2. 发明申请

WO2012068109A3 PYRIMIDINE HYDROXY AMIDE COMPOUNDS AS PROTEIN DEACETYLASE INHIBITORS AND METHODS OF USE THEREOF 审中-公开
标题翻译：作为蛋白脱乙酰酶抑制剂的吡咯烷酮羟化物化合物及其使用方法
公开(公告)号：WO2012068109A3
公开(公告)日：2012-08-02
申请号：PCT/US2011060791
申请日：2011-11-15
申请人： ACETYLON PHARMACEUTICALS , VAN DUZER JOHN H , MAZITSCHEK RALPH , DING YANBING , YU NAN , CAO YUN , LIU YONG
发明人： VAN DUZER JOHN H , MAZITSCHEK RALPH , DING YANBING , YU NAN , CAO YUN , LIU YONG
IPC分类号： C07D239/12 , A61K31/495 , A61P25/00 , C07D239/16 , C07D409/12
CPC分类号： C07D239/42 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12
摘要： The present invention relates to novel pyrimidine hydroxy amide compounds, and the use of such compounds in the inhibition of HDAC6 and in the treatment of various diseases, disorders or conditions related to HDAC6.
摘要翻译：本发明涉及新颖的嘧啶羟基酰胺化合物，以及这些化合物在抑制HDAC6和治疗与HDAC6相关的各种疾病，病症或病症中的用途。

3. 发明申请

WO2007130429A2 HISTONE DEACETYLASE AND TUBULIN DEACETYLASE INHIBITORS 审中-公开
标题翻译： HISTONE脱乙酰壳多糖酶和管状体脱乙酰酶抑制剂
公开(公告)号：WO2007130429A2
公开(公告)日：2007-11-15
申请号：PCT/US2007010587
申请日：2007-05-02
申请人： HARVARD COLLEGE , MAZITSCHEK RALPH , KWIATKOWSKI NICHOLAS PAUL , BRADNER JAMES ELLIOTT
发明人： MAZITSCHEK RALPH , KWIATKOWSKI NICHOLAS PAUL , BRADNER JAMES ELLIOTT
IPC分类号： A61K31/357
CPC分类号： C07D413/12 , C07D319/06 , C07D405/12 , C07D417/12
摘要： In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel inhibitors of histone deacetylases, tubulin deacetylases, and/or aggresome inhibitors, and pharmaceutically acceptable salts and derivatives thereof. The inventive compounds fall into two classes - "isorubacin" class and "isoisotubacin" class- - all of which include a 1,3-dioxane core. The present invention further provides methods for treating disorders regulated by histone deacetylase activity, tubulin deacetylase activity, and/or the aggresome (e.g., proliferative diseases, cancer, inflammatory diseases, protozoal infections, protein degradation disorders, protein deposition disorders, 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.
摘要翻译：鉴于需要开发新的治疗剂及其有效的合成方法，本发明提供组蛋白脱乙酰酶，微管蛋白脱乙酰酶和/或聚集抑制剂的新型抑制剂及其药学上可接受的盐和衍生物。本发明的化合物分为两类 - “异霍巴康”类和“异倍他康”类，其中全部包括1,3-二恶烷核。本发明进一步提供了用于治疗由组蛋白脱乙酰酶活性，微管蛋白脱乙酰酶活性和/或聚集物（例如增殖性疾病，癌症，炎性疾病，原生动物感染，蛋白质降解紊乱，蛋白沉积病症等）调节的病症的方法，其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本发明化合物的方法。

4. 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。

5. 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。

6. 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。

7. 发明申请

WO2006074293A2 BICYCLIC DIHYDROPYRIMIDINES AND USES THEREOF 审中-公开
标题翻译：双相二氢吡啶并嘧啶及其用途
公开(公告)号：WO2006074293A2
公开(公告)日：2006-07-13
申请号：PCT/US2006000300
申请日：2006-01-06
申请人： HARVARD COLLEGE , MAZITSCHEK RALPH , TALLARICO JOHN A , MALIGA ZOLTAN , MITCHISON TIMOTHY J
发明人： MAZITSCHEK RALPH , TALLARICO JOHN A , MALIGA ZOLTAN , MITCHISON TIMOTHY J
CPC分类号： C07D471/04 , C07D487/04 , C07D491/04
摘要： The present invention provides compounds having formula (I): (I) and pharmaceutically acceptable derivatives thereof; as described generally and in subclasses herein, which compounds are useful as kinesin inhibitors (e.g., Eg5 inhibitors), and thus are useful, for example, for the treatment of proliferative disorders e.g., cancer. The invention additionally provides methods for preparing compounds of the invention, compositions comprising them, and methods for the use thereof in the treatment of various disorders where Eg5 is involved. In certain embodiments, the present invention provides for compounds, compositions, methods and systems for inhibiting cell growth. More specifically, the present invention provides for methods, compounds and compositions which are capable of inhibiting mitosis in metabolically active cells. Compounds, compositions and methods of the present invention inhibit the activity of a protein involved in the assembly and maintenance of the mitotic spindle. One class of proteins which acts on the mitotic spindle is the family of mitotic kinesins, a subset of the kinesin superfamily.
摘要翻译：本发明提供具有式（I）的化合物：（I）及其药学上可接受的衍生物; 如本文中通常和在本文中所述的那样，哪些化合物可用作驱动蛋白抑制剂（例如Eg5抑制剂），因此可用于例如治疗增殖性疾病例如癌症。本发明另外提供了制备本发明化合物的方法，包含它们的组合物，以及用于治疗其中涉及Eg5的各种疾病的方法。在某些实施方案中，本发明提供了用于抑制细胞生长的化合物，组合物，方法和系统。更具体地，本发明提供能够抑制代谢活性细胞中有丝分裂的方法，化合物和组合物。本发明的化合物，组合物和方法抑制参与有丝分裂纺锤体的组装和维持的蛋白质的活性。作用于有丝分裂纺锤体的一类蛋白质是有丝分裂驱动蛋白家族，是驱动蛋白超家族的一个子集。

8. 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。

9. 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。

10. 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）。

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