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11. 发明公开

EP3177295A4 USES OF SALT-INDUCIBLE KINASE (SIK) INHIBITORS 审中-公开
公开(公告)号：EP3177295A4
公开(公告)日：2018-06-13
申请号：EP15829427
申请日：2015-08-08
申请人： DANA FARBER CANCER INST INC , BROAD INST INC , THE GENERAL HOSPITAL CORP D/B/A MASSACHUSETTS GENERAL HOSPITAL , HARVARD COLLEGE
发明人： SHAMJI ALYKHAN , SUNDBERG THOMAS , GRAY NATHANAEL , XAVIER RAMNIK , SCHREIBER STUART L , CHOI HWAN GEUN , LIANG YANKE
IPC分类号： A61K31/519 , A61K31/5377 , C07D498/02
CPC分类号： A61K31/519 , A61K31/506 , A61K31/5377 , A61K45/06
摘要： The present disclosure provides methods of treating and/or preventing inflammatory bowel disease (IBD) and graft-versus-host disease (GVHD) using salt-inducible kinase (SIK) inhibitors, such as macrocyclic SIK inhibitors of Formula (I), imidazolyl SIK inhibitors of Formula (II), and urea and carbamate SIK inhibitors of Formula (III -A) (e.g., urea and carbamate SIK inhibitors of Formula (III)).

12. 发明公开

EP1994209A4 SMALL MOLECULE PRINTING 审中-公开
标题翻译：配用小分子
公开(公告)号：EP1994209A4
公开(公告)日：2013-11-13
申请号：EP07835647
申请日：2007-01-03
申请人： HARVARD COLLEGE , DANA FARBER CANCER INST INC
发明人： BARNES DAVID W , KOEHLER ANGELA N , BRADNER JAMES E , MAZITSCHEK RALPH , SCHREIBER STUART L
IPC分类号： C40B30/04 , B01J19/00 , C40B40/04 , C40B80/00 , G01N33/543 , 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

13. 发明专利

AU2015300782A1 Uses of salt-inducible kinase (SIK) inhibitors 未知
公开(公告)号：AU2015300782A1
公开(公告)日：2017-02-02
申请号：AU2015300782
申请日：2015-08-08
申请人： DANA FARBER CANCER INST INC , HARVARD COLLEGE , BROAD INST INC , THE GENERAL HOSPITAL CORP D/B/A MASSACHUSETTS GENERAL HOSPITAL
发明人： SHAMJI ALYKHAN , SUNDBERG THOMAS , GRAY NATHANAEL , XAVIER RAMNIK , SCHREIBER STUART L , CHOI HWAN GEUN , LIANG YANKE
IPC分类号： C07D498/02 , A61K31/519 , A61K31/5377
摘要： The present disclosure provides methods of treating and/or preventing inflammatory bowel disease (IBD) and graft-versus-host disease (GVHD) using salt-inducible kinase (SIK) inhibitors, such as macrocyclic SIK inhibitors of Formula (I), imidazolyl SIK inhibitors of Formula (II), and urea and carbamate SIK inhibitors of Formula (III -A) (e.g., urea and carbamate SIK inhibitors of Formula (III)).

14. 发明专利

CA2642273C BIFUNCTIONAL HISTONE DEACETYLASE INHIBITORS 未知
公开(公告)号：CA2642273C
公开(公告)日：2016-09-20
申请号：CA2642273
申请日：2007-02-14
申请人： HARVARD COLLEGE , DANA-FARBER CANCER INST INC
发明人： BRADNER JAMES ELLIOT , MAZITSCHEK RALPH , TANG WEIPING , SCHREIBER STUART L
IPC分类号： A61K38/00 , A61K31/19 , A61K31/44
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.

15. 发明专利

SG176453A1 SMALL MOLECULE PRINTING 未知
公开(公告)号：SG176453A1
公开(公告)日：2011-12-29
申请号：SG2011081163
申请日：2007-01-03
申请人： HARVARD COLLEGE , DANA FARBER CANCER INST INC
发明人： BARNES DAVID W , KOEHLER ANGELA N , BRADNER JAMES E , MAZITSCHEK RALPH , SCHREIBER STUART L
摘要： Abstract SMALL MOLECULE PRINTINGThe 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.Figure 2

16. 发明专利

CA2635929A1 SMALL MOLECULE PRINTING 未知
公开(公告)号：CA2635929A1
公开(公告)日：2008-01-31
申请号：CA2635929
申请日：2007-01-03
申请人： DANA FARBER CANCER INST INC , HARVARD COLLEGE
发明人： SCHREIBER STUART L , BARNES DAVID W , KOEHLER ANGELA N , MAZITSCHEK RALPH , BRADNER JAMES E
IPC分类号： C40B30/04
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.

17. 发明专利

AU2015300782B2 Uses of salt-inducible kinase (SIK) inhibitors 未知
公开(公告)号：AU2015300782B2
公开(公告)日：2020-04-16
申请号：AU2015300782
申请日：2015-08-08
申请人： DANA FARBER CANCER INST INC , HARVARD COLLEGE , BROAD INST INC , THE GENERAL HOSPITAL CORP D/B/A MASSACHUSETTS GENERAL HOSPITAL
发明人： SUNDBERG THOMAS , GRAY NATHANAEL , XAVIER RAMNIK , SCHREIBER STUART L , CHOI HWAN GEUN , LIANG YANKE , SHAMJI ALYKHAN
IPC分类号： A61K31/5377 , A61K31/519 , C07D498/02
摘要： The present disclosure provides methods of treating and/or preventing inflammatory bowel disease (IBD) and graft-versus-host disease (GVHD) using salt-inducible kinase (SIK) inhibitors, such as macrocyclic SIK inhibitors of Formula (I), imidazolyl SIK inhibitors of Formula (II), and urea and carbamate SIK inhibitors of Formula (III -A) (e.g., urea and carbamate SIK inhibitors of Formula (III)).

18. 发明专利

AU2009274549B2 Deacetylase inhibitors and uses thereof 未知
公开(公告)号：AU2009274549B2
公开(公告)日：2014-05-01
申请号：AU2009274549
申请日：2009-07-22
申请人： DANA FARBER CANCER INST INC , HARVARD COLLEGE
发明人： TANG WEIPING , BRADNER JAMES ELLIOT , SCHREIBER STUART L
IPC分类号： C07C251/86 , A61K31/15 , A61P29/00 , A61P35/00
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.

19. 发明专利

AU2006226861B2 Treatment of protein degradation disorders 未知
公开(公告)号：AU2006226861B2
公开(公告)日：2012-08-16
申请号：AU2006226861
申请日：2006-03-22
申请人： DANA FARBER CANCER INST INC , HARVARD COLLEGE
发明人： SHAW JARED , MAZITSCHEK RALPH , BRADNER JAMES ELLIOTT , HIDESHIMA TERU , KWIATKOWSKI NICHOLAS PAUL , SCHREIBER STUART L , ANDERSON KENNETH C , GREENBERG EDWARD FRANKLIN , HAGGARTY STEPHEN J
IPC分类号： A61K31/42 , A61K31/335
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.

20. 发明专利

AU2009274549A1 Deacetylase inhibitors and uses thereof 未知
公开(公告)号：AU2009274549A1
公开(公告)日：2010-01-28
申请号：AU2009274549
申请日：2009-07-22
申请人： DANA FARBER CANCER INST INC , HARVARD COLLEGE
发明人： TANG WEIPING , BRADNER JAMES ELLIOT , SCHREIBER STUART L
IPC分类号： C07C251/86 , A61K31/15 , A61P29/00 , A61P35/00

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