Patents by Inventor Ralph Mazitschek

Ralph Mazitschek has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Publication number: 20170096413
    Abstract: The present invention relates to pyrimidine hydroxy amide compounds, the use of such compounds in the inhibition of HDAC6, and the use of such compounds in the treatment of various diseases, disorders, or conditions related to HDAC6.
    Type: Application
    Filed: September 9, 2016
    Publication date: April 6, 2017
    Inventors: Ralph Mazitschek, John H. van Duzer
  • Patent number: 9572854
    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.
    Type: Grant
    Filed: April 6, 2015
    Date of Patent: February 21, 2017
    Assignees: President and Fellows of Harvard College, Dana-Farber Cancer Institute, Inc.
    Inventors: Kenneth C. Anderson, James E. Bradner, Edward Franklin Greenberg, Teru Hideshima, Nicholas Paul Kwiatkowski, Ralph Mazitschek, Stuart L. Schreiber, Jared Shaw, Stephen J. Haggarty
  • Publication number: 20170045521
    Abstract: A multiphoton fluorescence anisotropy microscopy live cell imaging system and method to measure and map drug-target interaction in real lime at subcellular resolution. Proposed modality enables a direct measurement of drug/target binding in vivo, high-resolution spatial and temporal snapping of bound and unbound drug distribution, and presents an versatile tool to enhance understanding of drug activity. Application of tire system to measurement of intracellular target engagement of the chemotherapeutic Olaparib, a poly(ADP-ribose) polymerase inhibitor, in live cells and within a tumor in vivo.
    Type: Application
    Filed: April 22, 2015
    Publication date: February 16, 2017
    Inventors: Claudio Vinegoni, Ralph Weissieder, Matt Dubach, Ralph Mazitschek
  • Publication number: 20170044144
    Abstract: Provided herein are compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with HDAC activity, particularly diseases or disorders that involve activity of HDAC1 and/or HDAC2. Such diseases include cancer, sickle-cell anemia, beta-thalassemia, and HIV.
    Type: Application
    Filed: July 19, 2016
    Publication date: February 16, 2017
    Inventors: John H. van Duzer, Ralph Mazitschek
  • Patent number: 9562013
    Abstract: Provided herein are HDAC3 inhibitors, as well as methods of treatment comprising administering these compounds to a subject in need thereof.
    Type: Grant
    Filed: June 29, 2015
    Date of Patent: February 7, 2017
    Assignee: Acetylon Pharmaceuticals, Inc.
    Inventors: John H. van Duzer, Ralph Mazitschek
  • Patent number: 9540317
    Abstract: The present invention is drawn to compounds of Formula (I) below: and the pharmaceutically acceptable salts thereof, wherein R and R? are defined herein. The compounds are useful inhibitors of histone deacetylases (HDAC).
    Type: Grant
    Filed: May 6, 2014
    Date of Patent: January 10, 2017
    Assignees: President and Fellows of Harvard College, Dana-Farber Cancer Institute, Inc.
    Inventors: Ralph Mazitschek, James E. Bradner
  • Publication number: 20160375021
    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.
    Type: Application
    Filed: September 12, 2016
    Publication date: December 29, 2016
    Inventors: John H. van Duzer, Ralph Mazitschek, Walter Ogier, James E. Bradner, Guoxiang Huang, Dejian Xie, Nan Yu
  • Patent number: 9505735
    Abstract: The present invention provides compounds of Formula I, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting fungal or parasitic growth. The compounds are useful as inhibitors of glycosylphosphatidylinositol (GPI)-anchor biosynthesis, in particular, as inhibitors of fungal Gwt1 activity. The present invention further provides methods of using the compounds described herein for treating fungal or parasitic infections. The compounds can also be used as biological probes to study the effects of inhibiting Gwt1 activity.
    Type: Grant
    Filed: June 21, 2013
    Date of Patent: November 29, 2016
    Assignees: Whitehead Institute for Biomedical Research, The General Hospital Corporation
    Inventors: Catherine McLellan, Ralph Mazitschek, Luke Whitesell, Susan L. Lindquist
  • Publication number: 20160317498
    Abstract: The present invention provides novel analogs and derivatives of halofuginone. The invention also provides pharmaceutical and cosmetic compositions thereof and methods for using halofuginone analogs in treating chronic inflammatory diseases, autoimmune diseases, dry eye syndrome, fibrosis, scar formation, angiogenesis, viral infections, ischemic damage, transplant and implant rejection, neurodegenerative diseases, and cosmetic applications.
    Type: Application
    Filed: March 8, 2016
    Publication date: November 3, 2016
    Applicants: President and Fellows of Harvard College, Children's Medical Center Corporation
    Inventors: Tracy Keller, Ralph Mazitschek, Malcolm Whitman, Jinbo Lee, Mark S. Sundrud, Anjana Rao
  • Patent number: 9464073
    Abstract: The present invention relates to pyrimidine hydroxy amide compounds, the use of such compounds in the inhibition of HDAC6, and the use of such compounds in the treatment of various diseases, disorders, or conditions related to HDAC6.
    Type: Grant
    Filed: February 26, 2015
    Date of Patent: October 11, 2016
    Assignee: Acetylon Pharmaceuticals, Inc.
    Inventors: Ralph Mazitschek, John H. van Duzer
  • Publication number: 20160279128
    Abstract: Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat or prevent diseases or disorders associated with HDAC activity, particularly diseases or disorders that involve activity of HDAC1, HDAC2, and/or HDAC6. Also provided herein are methods for inhibiting migration of a neuroblastoma cell, inducing maturation of a neuroblastoma cell, and altering cell cycle progression of a neuroblastoma cell comprising administering to the cell a therapeutically effective amount of a HDAC1, HDAC2, and/or HDAC6 selective inhibitor or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: January 20, 2016
    Publication date: September 29, 2016
    Inventors: John H. van Duzer, Ralph Mazitschek, Simon Stewart Jones, Min Yang, David Lee Tamang
  • Publication number: 20160272579
    Abstract: The present invention relates to compounds which inhibit histone deacetylase activity and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing these compounds. The present invention also relates to methods of treating and preventing hematological cell proliferative disorders, such as multiple myeloma, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Application
    Filed: November 5, 2014
    Publication date: September 22, 2016
    Inventors: Ralph Mazitschek, Teru Hideshima, Kenneth C. Anderson, Stephen J. Haggarty, Balaram Ghosh
  • Patent number: 9421212
    Abstract: Provided herein are compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with HDAC activity, particularly diseases or disorders that involve activity of HDAC1 and/or HDAC2. Such diseases include cancer, sickle-cell anemia, beta-thalassemia, and HIV.
    Type: Grant
    Filed: August 12, 2015
    Date of Patent: August 23, 2016
    Assignee: ACETYLON PHARMACEUTICALS, INC.
    Inventors: John H. van Duzer, Ralph Mazitschek
  • Patent number: 9409890
    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.
    Type: Grant
    Filed: November 18, 2013
    Date of Patent: August 9, 2016
    Assignee: ACETYLON PHARAMCEUTICALS, INC.
    Inventors: John H. van Duzer, Ralph Mazitschek, Yanbing Ding, Nan Yu, Yun Cao, Yong Liu
  • Publication number: 20160168093
    Abstract: Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat diseases or disorders associated with HDAC1 and/or HDAC2 activity.
    Type: Application
    Filed: December 11, 2015
    Publication date: June 16, 2016
    Inventors: John H. van Duzer, Ralph Mazitschek
  • Publication number: 20160143874
    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 exmaple. The present invention also provides methods for preparing compounds of the invention and intermediates thereto.
    Type: Application
    Filed: September 23, 2015
    Publication date: May 26, 2016
    Inventors: James Elliot Bradner, Ralph Mazitschek
  • Patent number: 9284297
    Abstract: The present invention provides novel analogs and derivatives of halofuginone. The invention also provides pharmaceutical and cosmetic compositions thereof and methods for using halofuginone analogs in treating chronic inflammatory diseases, autoimmune diseases, dry eye syndrome, fibrosis, scar formation, angiogenesis, viral infections, ischemic damage, transplant and implant rejection, neurodegenerative diseases, and cosmetic applications.
    Type: Grant
    Filed: August 11, 2009
    Date of Patent: March 15, 2016
    Assignees: President and Fellows of Harvard College, Children's Medical Center Corporation
    Inventors: Tracy Keller, Ralph Mazitschek, Malcolm Whitman, Jinbo Lee, Mark S. Sundrud, Anjana Rao
  • Publication number: 20160067259
    Abstract: Provided herein are compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with HDAC activity, particularly diseases or disorders that involve activity of HDAC1 and/or HDAC2. Such diseases include cancer, sickle-cell anemia, beta-thalassemia, and HIV.
    Type: Application
    Filed: August 12, 2015
    Publication date: March 10, 2016
    Applicant: Acetylon Pharmaceuticals, Inc.
    Inventors: John H. van Duzer, Ralph Mazitschek
  • Patent number: 9278963
    Abstract: Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat or prevent diseases or disorders associated with HDAC activity, particularly diseases or disorders that involve activity of HDAC1, HDAC2, and/or HDAC6. Also provided herein are methods for inhibiting migration of a neuroblastoma cell, inducing maturation of a neuroblastoma cell, and altering cell cycle progression of a neuroblastoma cell comprising administering to the cell a therapeutically effective amount of a HDAC1, HDAC2, and/or HDAC6 selective inhibitor or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: October 9, 2014
    Date of Patent: March 8, 2016
    Assignee: Acetylon Pharmaceuticals, Inc.
    Inventors: John H. van Duzer, Ralph Mazitschek, Simon Stewart Jones, Min Yang, David Lee Tamang
  • Publication number: 20160051619
    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.
    Type: Application
    Filed: April 6, 2015
    Publication date: February 25, 2016
    Applicants: President and Fellows of Harvard College, Dana-Farber Cancer Institute, Inc.
    Inventors: Kenneth C. Anderson, James E. Bradner, Edward Franklin Greenberg, Teru Hideshima, Nicholas Paul Kwiatkowski, Ralph Mazitschek, Stuart L. Schreiber, Jared Shaw, Stephen J. Haggarty