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1. 发明授权

US08754237B2 Bifunctional histone deacetylase inhibitors 有权
标题翻译：双功能组蛋白脱乙酰酶抑制剂
公开(公告)号：US08754237B2
公开(公告)日：2014-06-17
申请号：US13550110
申请日：2012-07-16
申请人： James Elliot Bradner , Ralph Mazitschek , Weiping Tang , Stuart L. Schreiber
发明人： James Elliot Bradner , Ralph Mazitschek , Weiping Tang , Stuart L. Schreiber
IPC分类号： A61K31/24 , C07C229/02
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.
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本发明化合物的方法。

2. 发明申请

US20130261023A1 SMALL MOLECULE PRINTING 审中-公开
公开(公告)号：US20130261023A1
公开(公告)日：2013-10-03
申请号：US13648667
申请日：2012-10-10
申请人： David W. Barnes , Angela N. Koehler , James Elliot Bradner , Ralph Mazitschek , Stuart L. Schreiber
发明人： David W. Barnes , Angela N. Koehler , James Elliot Bradner , Ralph Mazitschek , Stuart L. Schreiber
IPC分类号： G01N33/68
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 cm2. 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 cm2. In another aspect, the present invention provides methods for utilizing these arrays to identify small molecule partners for biological macromolecules of interest.

3. 发明申请

US20130018103A1 BIFUNCTIONAL HISTONE DEACETYLASE INHIBITORS 有权
公开(公告)号：US20130018103A1
公开(公告)日：2013-01-17
申请号：US13550110
申请日：2012-07-16
申请人： James Elliot Bradner , Ralph Mazitschek , Weiping Tang , Stuart S. Schreiber
发明人： James Elliot Bradner , Ralph Mazitschek , Weiping Tang , Stuart S. Schreiber
IPC分类号： A61K31/197 , C12N5/071 , C12N9/99 , C07C259/06 , A61P35/00
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.

4. 发明申请

US20150038581A1 HISTONE DEACETYLASE INHIBITORS 有权
标题翻译： HISTONE脱乙酰酶抑制剂
公开(公告)号：US20150038581A1
公开(公告)日：2015-02-05
申请号：US14198764
申请日：2014-03-06
申请人： James Elliot Bradner , Ralph Mazitschek
发明人： James Elliot Bradner , Ralph Mazitschek
IPC分类号： C07C259/06
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.
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例如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。

5. 发明授权

US08304451B2 Histone deacetylase and tubulin deacetylase inhibitors 有权
标题翻译：组蛋白脱乙酰酶和微管蛋白脱乙酰酶抑制剂
公开(公告)号：US08304451B2
公开(公告)日：2012-11-06
申请号：US12299430
申请日：2007-05-02
申请人： Ralph Mazitschek , Nicholas Paul Kwiatkowski , James Elliot Bradner
发明人： Ralph Mazitschek , Nicholas Paul Kwiatkowski , James Elliot Bradner
IPC分类号： A61K31/357 , C07D407/12
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—“isotubacin” 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：异豆豆素类和异倍他宁类，其中全部包括1,3-二恶烷核。本发明还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/或聚集体（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，蛋白质沉积病症等）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。

6. 发明申请

US20100056588A1 HISTONE DEACETYLASE INHIBITORS 有权
标题翻译： HISTONE脱乙酰酶抑制剂
公开(公告)号：US20100056588A1
公开(公告)日：2010-03-04
申请号：US12279398
申请日：2007-02-14
申请人： James Elliot Bradner , Ralph Mazitschek
发明人： James Elliot Bradner , Ralph Mazitschek
IPC分类号： A61K31/422 , C07D413/12 , A61K31/22 , C07C229/00 , C12N5/02 , C07D319/06
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.
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例如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。

7. 发明授权

US08716344B2 Class- and isoform-specific HDAC inhibitors and uses thereof 有权
标题翻译：类别和异构体特异性HDAC抑制剂及其用途
公开(公告)号：US08716344B2
公开(公告)日：2014-05-06
申请号：US13389814
申请日：2010-08-11
申请人： Ralph Mazitschek , James Elliot Bradner
发明人： Ralph Mazitschek , James Elliot Bradner
IPC分类号： A61K38/05 , A61K31/495 , C12Q1/48 , A61K45/06 , C07D239/42 , C07D401/04
CPC分类号： C07C243/38 , A61K31/175 , A61K31/495 , A61K38/05 , A61K45/06 , C07D239/42 , C07D401/04 , C12Q1/48
摘要： The present invention relates to compounds of the following formula wherein R3 is a fluorescent tag. 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 the above formula in the presence of a test compound; and determining the activity of the HDAC protein.
摘要翻译：本发明涉及下式的化合物，其中R3是荧光标记。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蛋白质与上式的底物一起孵育; 并测定HDAC蛋白的活性。

8. 发明申请

US20130040998A1 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：US20130040998A1
公开(公告)日：2013-02-14
申请号：US13520650
申请日：2011-01-05
申请人： James Elliot Bradner , Ralph Mazitschek
发明人： James Elliot Bradner , Ralph Mazitschek
IPC分类号： A61K31/165 , A61K31/4045 , C07C239/14 , A61P35/00 , A61K31/40 , C07D213/56 , A61K31/44 , C07D209/14 , C07D207/333
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）。

9. 发明申请

US20090312363A1 BIFUNCTIONAL HISTONE DEACETYLASE INHIBITORS 有权
标题翻译：双功能脱乙酰壳多糖酶抑制剂
公开(公告)号：US20090312363A1
公开(公告)日：2009-12-17
申请号：US12279440
申请日：2007-02-14
申请人： James Elliot Bradner , Ralph Mazitschek , Tang Weiping , Stuart S. Schreiber
发明人： James Elliot Bradner , Ralph Mazitschek , Tang Weiping , Stuart S. Schreiber
IPC分类号： A61K31/4353 , C07D263/04 , A61K31/421 , C07D319/06 , A61K31/351 , C07D221/04 , C07C237/02 , A61K31/16 , C07D209/04 , A61K31/40 , C07C243/00 , C07D249/04 , A61K31/4192 , C12N9/99 , C12Q1/37
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.
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本发明化合物的方法。

10. 发明申请

US20140213620A1 HISTONE DEACETYLASE INHIBITORS 审中-公开
标题翻译： HISTONE脱乙酰酶抑制剂
公开(公告)号：US20140213620A1
公开(公告)日：2014-07-31
申请号：US13944320
申请日：2013-07-17
申请人： James Elliot Bradner , Ralph Mazitschek
发明人： James Elliot Bradner , Ralph Mazitschek
IPC分类号： C07D413/12 , C07C235/78 , C07D319/06
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.
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例如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。

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