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公开(公告)号：US09079908B2
公开(公告)日：2015-07-14
申请号：US13543065
申请日：2012-07-06
申请人： Lee Honigberg , Erik J. Verner , Joseph J. Buggy , David J. Loury , Wei Chen
发明人： Lee Honigberg , Erik J. Verner , Joseph J. Buggy , David J. Loury , Wei Chen
IPC分类号： A01N43/58 , A01N43/60 , A61K31/50 , A61K31/495 , C07D471/00 , C07D487/00 , C07D487/04 , A61K31/4985 , A61K31/519
CPC分类号： C07D487/04 , A61K31/4985 , A61K31/519 , A61K45/06
摘要： Described herein are irreversible kinase inhibitor compounds exemplified by the following structure Formula (B2): methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of a B cell proliferative disorder or a mast cell proliferative disorder.
摘要翻译： 本文描述的是不可逆激酶抑制剂化合物，其通过以下结构式（B2）示例：用于合成这种不可逆抑制剂的方法，以及使用这种不可逆抑制剂治疗B细胞增殖性疾病或肥大细胞增殖性疾病的方法。
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公开(公告)号：US08603521B2
公开(公告)日：2013-12-10
申请号：US12761588
申请日：2010-04-16
申请人： David J. Loury , Joseph J. Buggy , Tarak D. Mody , Erik J. Verner , Norbert Purro , Sriram Balasubramanian
发明人： David J. Loury , Joseph J. Buggy , Tarak D. Mody , Erik J. Verner , Norbert Purro , Sriram Balasubramanian
IPC分类号： A61K9/22
CPC分类号： A61N5/10 , A61K9/205 , A61K9/2054 , A61K9/2826 , A61K9/2846 , A61K9/2866 , A61K9/4808 , A61K9/4858 , A61K9/4866 , A61K9/501 , A61K9/5026 , A61K31/166 , A61K31/343 , A61K31/35 , A61K31/381 , A61K31/40 , A61K31/4184 , A61K31/47 , A61K31/497 , A61K31/573 , A61K31/69 , A61K31/704 , A61K38/05 , A61K45/05 , A61K45/06 , A61K47/02 , A61K47/12 , C07D307/85
摘要： Dosing regimens, methods of treatment, controlled release formulations, and combination therapies that include an HDAC inhibitor, or a pharmaceutically acceptable salt thereof, are described.
摘要翻译： 描述了给药方案，治疗方法，控制释放制剂和包括HDAC抑制剂或其药学上可接受的盐的组合疗法。
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公开(公告)号：US20130195852A1
公开(公告)日：2013-08-01
申请号：US13747322
申请日：2013-01-22
申请人： Joseph J. Buggy , Laurence Elias , Gwen Fyfe , Eric Hedrick , David J. Loury , Tarak D. Mody
发明人： Joseph J. Buggy , Laurence Elias , Gwen Fyfe , Eric Hedrick , David J. Loury , Tarak D. Mody
IPC分类号： A61K31/519 , A61K31/7032 , A61K31/7076 , A61K31/4745 , A61K31/573 , A61K45/06 , A61K31/4184 , A61K39/395 , A61K31/675
CPC分类号： A61K31/519 , A61K9/0014 , A61K9/0031 , A61K9/0048 , A61K9/0056 , A61K9/007 , A61K9/06 , A61K31/195 , A61K31/337 , A61K31/4184 , A61K31/436 , A61K31/437 , A61K31/454 , A61K31/4745 , A61K31/475 , A61K31/573 , A61K31/606 , A61K31/664 , A61K31/675 , A61K31/69 , A61K31/7032 , A61K31/704 , A61K31/7076 , A61K39/395 , A61K39/39533 , A61K39/3955 , A61K45/06 , C07D487/04 , A61K2300/00
摘要： Disclosed herein are methods for treating a cancer comprising: a. administering a Btk inhibitor to a subject sufficient to result in an increase or appearance in the blood of a subpopulation of lymphocytes defined by immunophenotyping; b. determining the expression profile of one or more biomarkers from one or more subpopulation of lymphocytes; and c. administering a second agent based on the determined expression profile.
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公开(公告)号：US20130035334A1
公开(公告)日：2013-02-07
申请号：US13606949
申请日：2012-09-07
申请人： Lee HONIGBERG , Erik J. Verner , Joseph J. Buggy , David J. Loury , Wei Chen
发明人： Lee HONIGBERG , Erik J. Verner , Joseph J. Buggy , David J. Loury , Wei Chen
IPC分类号： A61K31/519 , A61K31/5377 , A61P37/00 , A61P19/02 , A61P35/00 , C12Q1/02 , A61P19/10 , A61P29/00 , C12Q1/48 , G01N27/62 , G01N21/64 , C07D487/04 , A61P35/02
CPC分类号： C07D487/04 , A61K31/4985 , A61K31/519 , A61K45/06
摘要： Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase.
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公开(公告)号：US20120329130A1
公开(公告)日：2012-12-27
申请号：US13607036
申请日：2012-09-07
申请人： Lee Honigberg , Erik J. Verner , Joseph J. Buggy , David J. Loury , Wei Chen
发明人： Lee Honigberg , Erik J. Verner , Joseph J. Buggy , David J. Loury , Wei Chen
IPC分类号： C12N9/96
CPC分类号： C07D487/04 , A61K31/4985 , A61K31/519 , A61K45/06
摘要： Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase.
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公开(公告)号：US20120178753A1
公开(公告)日：2012-07-12
申请号：US13340276
申请日：2011-12-29
申请人： Lee Honigberg , Erik J. Verner , Joseph J. Buggy , David J. Loury , Wei Chen
发明人： Lee Honigberg , Erik J. Verner , Joseph J. Buggy , David J. Loury , Wei Chen
IPC分类号： A61K31/5377 , A61P35/04 , A61P19/10 , A61P35/00 , A61K31/519 , A61P19/08
CPC分类号： C07D487/04 , A61K31/4985 , A61K31/519 , A61K45/06
摘要： Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase.
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公开(公告)号：US20120065201A1
公开(公告)日：2012-03-15
申请号：US13232784
申请日：2011-09-14
申请人： Lee Honigberg , Erik J. Verner , Joseph J. Buggy , David J. Loury , Wei Chen
发明人： Lee Honigberg , Erik J. Verner , Joseph J. Buggy , David J. Loury , Wei Chen
IPC分类号： A61K31/5377 , A61K31/519 , A61P35/02 , A61P19/02 , A61P35/00 , C07D487/04 , A61P29/00
CPC分类号： C07D487/04
摘要： Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase.
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公开(公告)号：US08026371B2
公开(公告)日：2011-09-27
申请号：US12896535
申请日：2010-10-01
IPC分类号： C07D263/54 , A61K31/42
CPC分类号： A61K31/343 , A61K31/18 , A61K31/33 , A61K31/34 , A61K31/4015 , A61K31/4415 , A61K41/00 , A61K45/06 , A61N5/10 , C07C259/10 , C07C2601/02 , C07D207/12 , C07D207/327 , C07D207/34 , C07D209/08 , C07D209/18 , C07D209/42 , C07D209/44 , C07D211/46 , C07D213/56 , C07D213/74 , C07D213/81 , C07D213/82 , C07D215/08 , C07D215/18 , C07D215/48 , C07D215/54 , C07D217/04 , C07D217/06 , C07D217/26 , C07D231/56 , C07D235/06 , C07D235/24 , C07D241/52 , C07D249/18 , C07D261/18 , C07D263/58 , C07D277/30 , C07D277/42 , C07D277/56 , C07D277/68 , C07D307/54 , C07D307/68 , C07D307/79 , C07D307/81 , C07D307/85 , C07D307/86 , C07D317/60 , C07D333/16 , C07D333/24 , C07D333/28 , C07D333/38 , C07D333/70 , C07D405/06 , C07D405/12 , C07D409/04 , C07D413/12 , C07D417/04 , C07D417/12 , A61K2300/00
摘要： The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.
摘要翻译： 本发明涉及可用于治疗丙型肝炎的某些异羟肟酸衍生物。这些化合物也是组蛋白脱乙酰酶的抑制剂，因此可用于治疗与组蛋白脱乙酰酶活性相关的疾病。 还公开了制备这些化合物的药物组合物和方法。
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公开(公告)号：US20120183535A1
公开(公告)日：2012-07-19
申请号：US13340522
申请日：2011-12-29
申请人： Joseph J. Buggy , Laurence Elias , Gwen Fyfe , Eric Hedrick , David J. Loury , Tarak D. Mody
发明人： Joseph J. Buggy , Laurence Elias , Gwen Fyfe , Eric Hedrick , David J. Loury , Tarak D. Mody
IPC分类号： A61K31/519 , A61K39/395 , A61K31/7068 , A61K31/7076 , A61P35/00 , A61K31/704 , A61K31/69 , A61K31/664
CPC分类号： A61K31/519 , A61K9/0014 , A61K9/0031 , A61K9/0048 , A61K9/0056 , A61K9/007 , A61K9/06 , A61K31/195 , A61K31/337 , A61K31/4184 , A61K31/436 , A61K31/437 , A61K31/454 , A61K31/4745 , A61K31/475 , A61K31/573 , A61K31/606 , A61K31/664 , A61K31/675 , A61K31/69 , A61K31/7032 , A61K31/704 , A61K31/7076 , A61K39/395 , A61K39/39533 , A61K39/3955 , A61K45/06 , C07D487/04 , A61K2300/00
摘要： Disclosed herein are methods for treating a cancer comprising: a. administering a Btk inhibitor to a subject sufficient to result in an increase or appearance in the blood of a subpopulation of lymphocytes defined by immunophenotyping; b. determining the expression profile of one or more biomarkers from one or more subpopulation of lymphocytes; and c. administering a second agent based on the determined expression profile.
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10.发明申请USES OF SELECTIVE INHIBITORS OF HDAC8 FOR TREATMENT OF INFLAMMATORY CONDITIONS 审中-公开HDAC8选择性抑制剂用于治疗炎症病症的用途公开(公告)号：US20110150825A1
公开(公告)日：2011-06-23
申请号：US11940232
申请日：2007-11-14
IPC分类号： A61K38/20 , A61K31/405 , A61K31/4045 , A61K31/423 , A61K31/454 , A61K31/573 , A61K31/42 , A61K31/7135 , A61K31/28 , A61K31/655 , A61K39/395 , A61K38/21 , A61K39/35 , A61P17/00 , A61P29/00 , A61P19/02 , A61P37/04 , A61K38/00
CPC分类号： C07D209/12 , A61K31/404 , A61K31/4045 , A61K31/405 , A61K31/4245 , A61K31/454 , A61K31/5377 , A61K45/06 , C07D209/08 , C07D209/10 , C07D401/06 , C07D403/06 , C07D413/06
摘要： Described herein are methods for treating a subject suffering from an inflammatory, autoimmune, or heteroimmune condition by administering to the subject a pharmaceutical composition containing a therapeutically effective amount of a compound that is a selective inhibitor of histone deacetylase 8. Also described herein are methods for decreasing secretion of pro-inflammatory cytokines by administering an HDAC8-selective inhibitor compound. Further described herein are methods for predicting responsiveness to treatments for inflammatory conditions. Methods for predicting efficacy of treatments for inflammatory conditions are also described.
摘要翻译： 本文描述了通过向受试者施用含有治疗有效量的作为组蛋白脱乙酰酶8的选择性抑制剂的化合物的药物组合物来治疗患有炎症，自身免疫或异种免疫病症的受试者的方法。本文还描述了用于 通过施用HDAC8选择性抑制剂化合物来减少促炎细胞因子的分泌。 本文进一步描述了用于预测对炎症病症治疗的反应性的方法。 还描述了用于预测炎症病症治疗功效的方法。
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