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公开(公告)号：EP2321264B1
公开(公告)日：2016-05-04
申请号：EP09800666.1
申请日：2009-07-22
IPC分类号： C07C259/06 , C07C251/86
CPC分类号： C07C259/06 , C07C251/86
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公开(公告)号：EP1994209A2
公开(公告)日：2008-11-26
申请号：EP07835647.4
申请日：2007-01-03
发明人： BARNES, David, W. , KOEHLER, Angela, N. , BRADNER, James, E. , MAZITSCHEK, Ralph , SCHREIBER, Stuart, L.
IPC分类号： C40B30/04
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 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.
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公开(公告)号：EP3354265A1
公开(公告)日：2018-08-01
申请号：EP18157889.9
申请日：2006-03-22
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： A61K31/357 , A61K31/42 , A61K31/335 , A61K31/4965 , A61K45/06 , A61K31/35 , A61K31/39 , A61K31/69 , A61K38/55 , A61K49/00 , G01N33/50 , A61K31/422 , A61K38/50 , A61K38/05
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 as cellular proliferative disorders (e.g., cancer). 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 solid tumors. New HDAC/TDAC inhibitors and aggresome inhibitors are also provided as well as synthetic methodologies for preparing these compounds.
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公开(公告)号：EP1991247B1
公开(公告)日：2015-10-14
申请号：EP07872648.6
申请日：2007-02-14
IPC分类号： C07C259/06 , C07D413/12 , C07D249/04 , C07D249/06
CPC分类号： A61K31/19 , A61K31/44 , A61K47/55 , C07C259/06 , C07D249/04 , C07D249/06 , C07D413/12
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公开(公告)号：EP1861126A2
公开(公告)日：2007-12-05
申请号：EP06748614.2
申请日：2006-03-22
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 , A61K39/395 , A61K33/36
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.
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公开(公告)号：EP2321264A2
公开(公告)日：2011-05-18
申请号：EP09800666.1
申请日：2009-07-22
IPC分类号： C07C251/86 , A61K31/15 , A61P35/00 , A61P29/00
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。
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公开(公告)号：EP1991247A1
公开(公告)日：2008-11-19
申请号：EP07872648.6
申请日：2007-02-14
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.
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公开(公告)号：EP0820283A1
公开(公告)日：1998-01-28
申请号：EP96912710.0
申请日：1996-04-12
IPC分类号： A61K31 , A61P25 , A61P29 , A61P35 , A61P37 , A61P43 , C07D207 , C07D487 , C07D491 , C07D495 , C07D498 , C12N9
CPC分类号： C07D487/04 , A61K31/4015 , A61K31/407 , C07D491/10 , C07D495/10 , C12N9/6421
摘要： Compounds related to lactacystin and lactacystin β-lactone, pharmaceutical compositions containing the compounds, and methods of use.
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公开(公告)号：EP1127140A2
公开(公告)日：2001-08-29
申请号：EP99958742.1
申请日：1999-11-05
IPC分类号： C12N15/62 , C12N15/52 , C12N9/16 , C12N15/86 , A01K67/027 , G01N33/566
CPC分类号： C07D498/18 , A01K67/0271 , A61K48/00 , C07K14/005 , C07K2319/00 , C07K2319/09 , C07K2319/43 , C07K2319/71 , C07K2319/715 , C12N9/16 , C12N9/90 , C12N15/62 , C12N2710/16622
摘要： This invention provides methods and materials for making and using genetically engineered cells which are responsive to the presence of an FKBP/CAB ligand or a cyclophilin/CAB ligand. The invention relies upon the introduction into cells of recombinant DNAs encoding fusion proteins which are capable of forming a complex with each other in the presence of ligand. One of the fusion proteins contains a calcineurin A/calcineurin B domain (CAB) and at least one heterologous protein domain. The second fusion protein contains a domain derived from an FKBP protein which is capable of binding to an FKBP/CAB ligand and forming a complex with a CAB-containing protein. The second fusion protein may alternatively contain a cyclophilin domain which is capable of binding cyclosporin or other cyclophilin/CAB ligand and forming a complex with a CAB-containing protein. The second fusion protein also contains at least one heterologous domain.
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公开(公告)号：EP0820283B1
公开(公告)日：2007-02-14
申请号：EP96912710.9
申请日：1996-04-12
IPC分类号： A61K31/395 , A61K38/00
CPC分类号： C07D487/04 , A61K31/4015 , A61K31/407 , C07D491/10 , C07D495/10 , C12N9/6421
摘要： Compounds related to lactacystin and lactacystin β-lactone, pharmaceutical compositions containing the compounds, and methods of use.
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