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).

  • Patent number: 9884850
    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: September 9, 2016
    Date of Patent: February 6, 2018
    Assignee: ACETYLON PHARMACEUTICALS, INC.
    Inventors: Ralph Mazitschek, John H. van Duzer
  • Publication number: 20180030040
    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 15, 2017
    Publication date: February 1, 2018
    Inventors: John H. van Duzer, Ralph Mazitschek
  • Publication number: 20180022702
    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: September 29, 2017
    Publication date: January 25, 2018
    Inventors: John H. van Duzer, Ralph Mazitschek
  • Publication number: 20170369441
    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: September 11, 2017
    Publication date: December 28, 2017
    Inventors: John H. van Duzer, Ralph Mazitschek
  • Publication number: 20170360740
    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.
    Type: Application
    Filed: June 29, 2017
    Publication date: December 21, 2017
    Inventors: James Elliot Bradner, Ralph Mazitschek
  • Publication number: 20170304245
    Abstract: Pentacyclic triterpene weight loss agents are provided herein. Also provided are pharmaceutical formulations containing a therapeutically effective amount of one or more of the weight loss agents, or pharmaceutically acceptable salts or prodrugs thereof, in combination with one or more pharmaceutically acceptable excipients. The pharmaceutical formulations can be administered to a pre-obese, obese, or morbidly obese patient to induce weight loss, reduce body fat, reduce food intake, improve glucose homeostasis, prevent obesity, or a combination thereof. The weight loss agents can also be co-administered with leptin or a leptin analog.
    Type: Application
    Filed: July 7, 2017
    Publication date: October 26, 2017
    Inventors: Umut Ozcan, Joseph Majzoub, Ralph Mazitschek, Isin Cakir, Serkan Cabi
  • Patent number: 9790180
    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: Grant
    Filed: December 11, 2015
    Date of Patent: October 17, 2017
    Assignee: REGENACY PHARMACEUTICALS, LLC
    Inventors: John H. van Duzer, Ralph Mazitschek
  • Publication number: 20170267630
    Abstract: HDAC inhibitors of the general formula (I) and (II) and pharmaceutically acceptable salts thereof, as described herein, are useful as inhibitors of histone deacetylases or other deacetylases, and thus are useful for the treatment of various diseases and disorders associated with acetylase/deacetylase activity as described herein (e.g., cancer). In certain embodiments, the compounds of the invention selectively target either a class or isoform of the HDAC family. Another aspect of the invention provides an assay for determining the inhibitory effect of a test compound on an HDAC protein comprising: incubating the HDAC protein with a substrate of general formula (IIIc) in the presence of a test compound; and determining the activity of the HDAC protein.
    Type: Application
    Filed: January 5, 2017
    Publication date: September 21, 2017
    Applicants: President and Fellows of Harvard College, Dana-Farber Cancer Institute, Inc.
    Inventors: Ralph Mazitschek, James E. Bradner
  • Patent number: 9765066
    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: July 19, 2016
    Date of Patent: September 19, 2017
    Assignee: REGENACY PHARMACEUTICALS, LLC
    Inventors: John H. van Duzer, Ralph Mazitschek
  • Patent number: 9724321
    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.
    Type: Grant
    Filed: September 23, 2015
    Date of Patent: August 8, 2017
    Assignees: President & Fellows of Harvard College, Dana-Farber Cancer Institute, Inc.
    Inventors: James Elliot Bradner, Ralph Mazitschek
  • Publication number: 20170204094
    Abstract: Provided herein are HDAC3 inhibitors, as well as methods of treatment comprising administering these compounds to a subject in need thereof.
    Type: Application
    Filed: December 23, 2016
    Publication date: July 20, 2017
    Inventors: John H. van Duzer, Ralph Mazitschek
  • 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
  • Publication number: 20170096403
    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: Application
    Filed: July 6, 2016
    Publication date: April 6, 2017
    Inventors: John H. van Duzer, Ralph Mazitschek, Yanbing Ding, Nan Yu, Yun Cao, Yong Liu
  • 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: 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
  • 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
  • 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