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Ralph Mazitschek Phones & Addresses

  • Weston, MA
  • Belmont, MA
  • 46 Egerton Rd, Arlington, MA 02474
  • Somerville, MA
  • 28 Colborne Rd, Brighton, MA 02135
  • Boston, MA
  • Waban, MA

Publications

Us Patents

Bifunctional Histone Deacetylase Inhibitors

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US Patent:
8222423, Jul 17, 2012
Filed:
Feb 14, 2007
Appl. No.:
12/279440
Inventors:
James Elliot Bradner - Cambridge MA, US
Ralph Mazitschek - Arlington MA, US
Tang Weiping - Cambridge MA, US
Stuart S. Schreiber - Boston MA, US
Assignee:
Dana-Farber Cancer Institute, Inc. - Boston MA
President and Fellows of Harvard College - Cambridge MA
Howard Hughes Medical Institute - Chevy Chase MD
International Classification:
C07D 249/00
C07C 303/00
US Classification:
548255, 564 80, 564 84
Abstract:
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.

Histone Deacetylase And Tubulin Deacetylase Inhibitors

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US Patent:
8304451, Nov 6, 2012
Filed:
May 2, 2007
Appl. No.:
12/299430
Inventors:
Ralph Mazitschek - Arlington MA, US
Nicholas Paul Kwiatkowski - Auburn MA, US
James Elliot Bradner - Cambridge MA, US
Assignee:
President and Fellows of Harvard College - Cambridge MA
Dana-Farber Cancer Institute, Inc. - Boston MA
International Classification:
A61K 31/357
C07D 407/12
US Classification:
514452, 549370
Abstract:
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.

Kinase Inhibitors And The Use Thereof

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US Patent:
8324267, Dec 4, 2012
Filed:
Jul 12, 2002
Appl. No.:
10/483687
Inventors:
Vladimir Chirchin - Frankfurt am Main, DE
Giannis Athanassios - Leipzig, DE
Ralph Mazitschek - Boston MA, US
Jonathan Sleemann - Bruchsal, DE
Assignee:
Forschungzentrum Karlsruhe GmbH - Karlsruhe
International Classification:
A61K 31/405
C07D 209/00
US Classification:
514415, 548469
Abstract:
The present invention relates to protein kinase inhibitors and to the use thereof for the treatment of diseases induced by pathological signal transduction cascades.

Histone Deacetylase Inhibitors

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US Patent:
8383855, Feb 26, 2013
Filed:
Feb 14, 2007
Appl. No.:
12/279398
Inventors:
James Elliot Bradner - Cambridge MA, US
Ralph Mazitschek - Arlington MA, US
Assignee:
President and Fellows of Harvard College - Cambridge MA
Dana-Farber Cancer Institute, Inc. - Boston MA
International Classification:
C07C 259/04
A61K 31/47
A61K 31/19
US Classification:
562621, 514307, 514449, 514575
Abstract:
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.

Reverse Amide Compounds As Protein Deacetylase Inhibitors And Methods Of Use Thereof

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US Patent:
8394810, Mar 12, 2013
Filed:
Jan 21, 2011
Appl. No.:
13/010974
Inventors:
John H. van Duzer - Georgetown MA, US
Ralph Mazitschek - Arlington MA, US
Walter Ogier - Winchester MA, US
James E. Bradner - Cambridge MA, US
Guoxiang Huang - Kernersville NC, US
Dejian Xie - Shanghai, CN
Nan Yu - Shanghai, CN
Assignee:
Acetylon Pharmaceuticals - Boston MA
International Classification:
A61K 31/505
US Classification:
514275
Abstract:
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.

Reverse Amide Compounds As Protein Deacetylase Inhibitors And Methods Of Use Thereof

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US Patent:
8609678, Dec 17, 2013
Filed:
Apr 2, 2012
Appl. No.:
13/437672
Inventors:
John H. Van Duzer - Georgetown MA, US
Ralph Mazitschek - Belmont MA, US
Walter Ogier - Winchester MA, US
James E. Bradner - Cambridge MA, US
Guoxiang Huang - Kernersville NC, US
Dejian Xie - Shanghai, CN
Nan Yu - Shanghai, CN
Assignee:
Acetylon Pharmaceuticals - Boston MA
International Classification:
A01N 43/54
A61K 31/505
C07D 239/42
C07D 401/04
C07D 239/02
US Classification:
514275, 514256, 544332
Abstract:
The present invention relates to “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.

Pyrimidine Hydroxy Amide Compounds As Protein Deacetylase Inhibitors And Methods Of Use Thereof

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US Patent:
8614223, Dec 24, 2013
Filed:
Nov 15, 2011
Appl. No.:
13/296748
Inventors:
John H. van Duzer - Georgetown MA, US
Ralph Mazitschek - Belmont MA, US
Yanbing Ding - Richmond, CA
Nan Yu - Shanghai, CN
Yun Cao - Shanghai, CN
Yong Liu - Shanghai, CN
Assignee:
Acetylon Pharmaceuticals, Inc. - Boston MA
International Classification:
C07D 239/42
A61K 31/505
A61K 31/506
A61P 35/00
US Classification:
514275, 544330, 544331, 544332
Abstract:
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.

Treatment Of Protein Degradation Disorders

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US Patent:
20060239909, Oct 26, 2006
Filed:
Mar 22, 2006
Appl. No.:
11/386959
Inventors:
Kenneth Anderson - Wellesley MA, US
James Bradner - Cambridge MA, US
Edward Greenberg - Newton MA, US
Teru Hideshima - Brookline MA, US
Nicholas Kwiatkowski - Auburn MA, US
Ralph Mazitschek - Boston MA, US
Stuart Schreiber - Boston MA, US
Jared Shaw - Cambridge MA, US
Stephen Haggarty - Boston MA, US
International Classification:
A61K 51/00
A61K 39/395
A61K 33/36
US Classification:
424001490, 424155100, 424623000
Abstract:
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.
Ralph Mazitschek from Weston, MA, age ~53 Get Report