Patents by Inventor William W. Bachovchin

William W. Bachovchin 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: 20190275064
    Abstract: Disclosed are prodrugs of anthracyclines (such as doxorubicin) and derivatives thereof that are selectively cleaved and activated by fibroblast activating protein (FAP). The prodrugs are useful for targeted delivery of “warhead” anthracycline or anthracycline derivative to FAP-expressing tissues, including cancer (e.g., solid tumors). Also provided are pharmaceutical compounds comprising the prodrugs, as well as methods of using the prodrugs to treat a disorder characterized by FAP upregulation, e.g., cancer, undesirable fibrosis, and undesirable inflammation.
    Type: Application
    Filed: October 16, 2018
    Publication date: September 12, 2019
    Inventors: William W. Bachovchin, Hung-sen Lai, David G. Sanford, Sarah E. Poplawski, Wengen Wu
  • Publication number: 20190209525
    Abstract: Disclosed are potent immuno-DASH inhibitors, and their use in the treatment of cell proliferative diseases.
    Type: Application
    Filed: September 7, 2017
    Publication date: July 11, 2019
    Inventors: William W. Bachovchin, Hung-sen Lai, Wengen Wu
  • Patent number: 10245248
    Abstract: Disclosed are prodrugs of therapeutic or imaging agents, which prodrugs are selectively cleaved by fibroblast activating protein (FAP) to release the agents. Upon cleavage by FAP of the FAP substrate, the prodrug releases the agent in its active form or in a form that is readily metabolized to its active form. Pharmaceutical compositions comprising the prodrugs, as well as methods of using the prodrugs to treat a disorder characterized by FAP upregulation are also disclosed.
    Type: Grant
    Filed: June 15, 2015
    Date of Patent: April 2, 2019
    Assignee: BACH BIOSCIENCES, LLC
    Inventors: William W. Bachovchin, Hung-sen Lai, David G. Sanford, Sarah E. Poplawski, Wengen Wu
  • Publication number: 20190054181
    Abstract: Disclosed are proteasome inhibitors, fibroblast activation protein (FAP)-activated prodrugs of proteasome inhibitors, and pharmaceutically acceptable salts of the inhibitors and prodrugs. Also disclosed are related pharmaceutical compositions, and methods of using the inhibitors and prodrugs and compositions thereof, for example, in treating cancer or other cell proliferative diseases. In vitro and in vivo methods of quantifying the expression of FAP in a biopsy sample and a mammal, respectively, are also disclosed.
    Type: Application
    Filed: April 13, 2018
    Publication date: February 21, 2019
    Inventors: William W. Bachovchin, Hung-sen Lai, Sarah E. Poplawski
  • Patent number: 10117887
    Abstract: Disclosed are prodrugs of anthracyclines (such as doxorubicin) and derivatives thereof that are selectively cleaved and activated by fibroblast activating protein (FAP). The prodrugs are useful for targeted delivery of “warhead” anthracycline or anthracycline derivative to FAP-expressing tissues, including cancer (e.g., solid tumors). Also provided are pharmaceutical compositions comprising the prodrugs, as well as methods of using the prodrugs to treat a disorder characterized by FAP upregulation, e.g., cancer, undesirable fibrosis, and undesirable inflammation.
    Type: Grant
    Filed: July 20, 2017
    Date of Patent: November 6, 2018
    Assignee: BACH BIOSCIENCES, LLC
    Inventors: William W. Bachovchin, Hung-sen Lai, David G. Sanford, Sarah E. Poplawski, Wengen Wu
  • Patent number: 9956297
    Abstract: Disclosed are proteasome inhibitors, fibroblast activation protein (FAP)-activated prodrugs of proteasome inhibitors, and pharmaceutically acceptable salts of the inhibitors and prodrugs. Also disclosed are related pharmaceutical compositions, and methods of using the inhibitors and prodrugs and compositions thereof, for example, in treating cancer or other cell proliferative diseases. In vitro and in vivo methods of quantifying the expression of FAP in a biopsy sample and a mammal, respectively, are also disclosed.
    Type: Grant
    Filed: May 27, 2016
    Date of Patent: May 1, 2018
    Assignee: Trustees of Tufts College
    Inventors: William W. Bachovchin, Hung-sen Lai, Sarah E. Poplawski
  • Publication number: 20180092933
    Abstract: Disclosed is a method of treating cancer, comprising administering to a mammal in need thereof a therapeutically effective amount of a compound that inhibits a plurality of mammalian DASH serine proteases. Also disclosed is a method of (a) increasing antitumor immunity, (b) stimulating or enhancing an immune response, (c) treating a condition characterized by abnormal cell proliferation, (d) increasing cytokine and/or chemokine production, or (e) stimulating or enhancing production of T-cells, in a mammal, comprising administering to a mammal in need thereof an effective amount of a compound that inhibits a plurality of mammalian DASH serine proteases. For example, the compound that inhibits a plurality of mammalian DASH serine proteases may be t-butylGly-boroPro.
    Type: Application
    Filed: November 20, 2017
    Publication date: April 5, 2018
    Inventor: William W. Bachovchin
  • Patent number: 9839646
    Abstract: Disclosed is a method of treating cancer, comprising administering to a mammal in need thereof a therapeutically effective amount of a compound that inhibits a plurality of mammalian DASH serine proteases. Also disclosed is a method of (a) increasing antitumor immunity, (b) stimulating or enhancing an immune response, (c) treating a condition characterized by abnormal cell proliferation, (d) increasing cytokine and/or chemokine production, or (e) stimulating or enhancing production of T-cells, in a mammal, comprising administering to a mammal in need thereof an effective amount of a compound that inhibits a plurality of mammalian DASH serine proteases. For example, the compound that inhibits a plurality of mammalian DASH serine proteases may be t-butylGly-boroPro.
    Type: Grant
    Filed: November 23, 2015
    Date of Patent: December 12, 2017
    Assignee: Trustees of Tufts College
    Inventor: William W. Bachovchin
  • Publication number: 20170333461
    Abstract: Disclosed are inhibitors of post-proline cleavage enzymes, such as inhibitors of dipeptidyl peptidase IV, as well as pharmaceutical compositions thereof, and methods for using such inhibitors. In particular, the inhibitors are improved over those in the prior art by selection of particular classes of side chains in the P1 and/or P2 position of the inhibitor. The inhibitors can have a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease.
    Type: Application
    Filed: June 19, 2017
    Publication date: November 23, 2017
    Inventor: William W. Bachovchin
  • Publication number: 20170319609
    Abstract: Disclosed are prodrugs of anthracyclines (such as doxorubicin) and derivatives thereof that are selectively cleaved and activated by fibroblast activating protein (FAP). The prodrugs are useful for targeted delivery of “warhead” anthracycline or anthracycline derivative to FAP-expressing tissues, including cancer (e.g., solid tumors). Also provided are pharmaceutical compositions comprising the prodrugs, as well as methods of using the prodrugs to treat a disorder characterized by FAP upregulation, e.g., cancer, undesirable fibrosis, and undesirable inflammation.
    Type: Application
    Filed: July 20, 2017
    Publication date: November 9, 2017
    Inventors: William W. Bachovchin, Hung-sen Lai, David G. Sanford, Sarah E. Poplawski, Wengen Wu
  • Patent number: 9757400
    Abstract: Disclosed are inhibitors of post-proline cleavage enzymes, such as inhibitors of dipeptidyl peptidase IV, as well as pharmaceutical compositions thereof, and methods for using such inhibitors. In particular, the inhibitors are improved over those in the prior art by selection of particular classes of side chains in the P1 and/or P2 position of the inhibitor. The inhibitors can have a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease.
    Type: Grant
    Filed: February 12, 2016
    Date of Patent: September 12, 2017
    Assignee: Trustees of Tufts College
    Inventor: William W. Bachovchin
  • Publication number: 20170246255
    Abstract: The present invention relates to compositions of peptide and polypeptide analogs that are resistant to proteolysis, pharmaceutical uses thereof, and methods of preparation thereof.
    Type: Application
    Filed: July 24, 2015
    Publication date: August 31, 2017
    Inventors: William W. Bachovchin, Hung-sen Lai, David G. Sanford
  • Patent number: 9737556
    Abstract: Disclosed are prodrugs of anthracyclines (such as doxorubicin) and derivatives thereof that are selectively cleaved and activated by fibroblast activating protein (FAP). The prodrugs are useful for targeted delivery of “warhead” anthracycline or anthracycline derivative to FAP-expressing tissues, including cancer (e.g., solid tumors). Also provided are pharmaceutical compositions comprising the prodrugs, as well as methods of using the prodrugs to treat a disorder characterized by FAP upregulation, e.g., cancer, undesirable fibrosis, and undesirable inflammation.
    Type: Grant
    Filed: June 15, 2015
    Date of Patent: August 22, 2017
    Assignee: Trustees of Tufts College
    Inventors: William W. Bachovchin, Hung-sen Lai, David G. Sanford, Sarah E. Poplawski, Wengen Wu
  • Publication number: 20170226155
    Abstract: The present invention relates to prodrugs of protease inhibitors, such as inhibitors of the proteosome, DPP IV, FAP? and the like. These“pro-inhibitors” are activated, i.e., cleaved, by an “activated protease” to release an active inhibitor moiety in proximity to a “target protease”. The identity of activating protease and target protease can be the same (such as pro-inhibitors being referred to as “Target-Activated Smart Protease Inhibitors” or “TASPI”) or different (e.g., “Target-Directed Smart Protease Inhibitors” or “TDSPI”). After activation of the pro-inhibitor, the active inhibitor moiety can self-inactivate by, e.g., intramolecular-cyclization or cis-trans isomerization.
    Type: Application
    Filed: March 14, 2017
    Publication date: August 10, 2017
    Applicant: Trustees of Tufts College
    Inventor: William W. Bachovchin
  • Publication number: 20170128476
    Abstract: Disclosed are prodrugs of anthracyclines (such as doxorubicin) and derivatives thereof that are selectively cleaved and activated by fibroblast activating protein (FAP). The prodrugs are useful for targeted delivery of “warhead” anthracycline or anthracycline derivative to FAP-expressing tissues, including cancer (e.g., solid tumors). Also provided are pharmaceutical compositions comprising the prodrugs, as well as methods of using the prodrugs to treat a disorder characterized by FAP upregulation, e.g., cancer, undesirable fibrosis, and undesirable inflammation.
    Type: Application
    Filed: June 15, 2015
    Publication date: May 11, 2017
    Inventors: William W. Bachovchin, Hung-sen Lai, David G. Sanford, Sarah E. Poplawski, Wengen Wu
  • Publication number: 20170119901
    Abstract: Disclosed are prodrugs of therapeutic or imaging agents, which prodrugs are selectively cleaved by fibroblast activating protein (FAP) to release the agents. Upon cleavage by FAP of the FAP substrate, the prodrug releases the agent in its active form or in a form that is readily metabolized to its active form. Pharmaceutical compositions comprising the prodrugs, as well as methods of using the prodrugs to treat a disorder characterized by FAP upregulation are also disclosed.
    Type: Application
    Filed: June 15, 2015
    Publication date: May 4, 2017
    Inventors: William W. Bachovchin, Hung-sen Lai, David G. Sanford, Sarah E. Poplawski, Wengen Wu
  • Patent number: 9629921
    Abstract: The present invention relates to prodrugs of protease inhibitors, such as inhibitors of the proteosome, DPP IV, FAP? and the like. These“pro-inhibitors” are activated, i.e., cleaved, by an “activated protease” to release an active inhibitor moiety in proximity to a “target protease”. The identity of activating protease and target protease can be the same (such as pro-inhibitors being referred to as “Target-Activated Smart Protease Inhibitors” or “TASPI”) or different (e.g., “Target-Directed Smart Protease Inhibitors” or “TDSPI”). After activation of the pro-inhibitor, the active inhibitor moiety can self-inactivate by, e.g., intramolecular-cyclization or cis-trans isomerization.
    Type: Grant
    Filed: March 4, 2013
    Date of Patent: April 25, 2017
    Assignee: Trustees of Tufts College
    Inventor: William W. Bachovchin
  • Patent number: 9597410
    Abstract: Disclosed are proteasome inhibitors, fibroblast activation protein (FAP)-activated prodrugs of proteasome inhibitors, and pharmaceutically acceptable salts of the inhibitors and prodrugs. Also disclosed are related pharmaceutical compositions, and methods of using the inhibitors and prodrugs and compositions thereof, for example, in treating cancer or other cell proliferative diseases. In vitro and in vivo methods of quantifying the expression of FAP in a biopsy sample and a mammal, respectively, are also disclosed.
    Type: Grant
    Filed: August 30, 2012
    Date of Patent: March 21, 2017
    Assignee: Trustees of Tufts College
    Inventors: William W. Bachovchin, Hung-sen Lai, Sarah E. Poplawski
  • Patent number: 9511060
    Abstract: One aspect of the present invention relates to substituted pyridines and pharmaceutically acceptable salts thereof that are active against a range of mammalian maladies. Another aspect of the invention relates to a pharmaceutical composition, comprising a compound of the present invention or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable excipient. The present invention also relates to methods of treating a range of mammalian maladies or conditions, including but not limited to hyperlipidemia, hypercholesterolemia, atherosclerosis, coronary artery disease, congestive heart failure, cardiovascular disease, hypertension, coronary heart disease, angina, pellagra, Hartnup's syndrome, carcinoid syndrome, arterial occlusive disease, obesity, hypothyroidism, vasoconstriction, osteoarthritis, rheumatoid arthritis, diabetes, Alzheimer's disease, lipodystrophy, or dyslipidemia, raising serum high-density lipoprotein (HDL) levels, and lowering serum low-density lipoprotein (LDL) levels.
    Type: Grant
    Filed: November 4, 2015
    Date of Patent: December 6, 2016
    Assignee: Trustees of Tufts College
    Inventors: William W. Bachovchin, Hung-sen Lai
  • Publication number: 20160346401
    Abstract: Disclosed are proteasome inhibitors, fibroblast activation protein (FAP)-activated prodrugs of proteasome inhibitors, and pharmaceutically acceptable salts of the inhibitors and prodrugs. Also disclosed are related pharmaceutical compositions, and methods of using the inhibitors and prodrugs and compositions thereof, for example, in treating cancer or other cell proliferative diseases. In vitro and in vivo methods of quantifying the expression of FAP in a biopsy sample and a mammal, respectively, are also disclosed.
    Type: Application
    Filed: May 27, 2016
    Publication date: December 1, 2016
    Inventors: William W. Bachovchin, Hung-sen Lai, Sarah E. Poplawski