Patents by Inventor David A. Spiegel

David A. Spiegel 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: 20190209572
    Abstract: The present invention is directed to bifunctional compounds which are useful in the treatment of fungal infections. The present compounds contains at least one fungal binding moiety (FBM) which is linked to at least one antibody binding moiety (ABM or ABT group) through a linker group, which optionally comprises a connector group. Compounds according to the present invention are useful in the treatment of fungal infections as described herein.
    Type: Application
    Filed: August 18, 2017
    Publication date: July 11, 2019
    Inventors: DAVID A. SPIEGEL, EGOR CHIRKIN, TERRY ROEMER, PHILIPPE NANTERMET
  • Publication number: 20190209696
    Abstract: The present invention relates to compounds which function as antibody mimetic compounds. These compounds are bifunctional/multifunctional compounds which contain at least one cancer cell binding moiety which selectively binds to prostate specific membrane antigen (PSMA) and a FC receptor binding moiety which modulates an FC immune receptor, preferably a Fc?RI receptor. Compounds according to the present invention bind selectively to cancer cells which upregulate PSMA and through that interaction, place the Fc receptor binding moiety of the compound in proximity to a Fc receptor, preferably a Fc?RI receptor, which can modulate (preferably, upregulate) a humoral response in a patient to cancer cells. Through this biological action of the compounds according to the present invention, cancer cells, including metastatic cancer cells, especially prostate cancer cells can be immune regulated, resulting in the favorable therapy of cancer in a patient.
    Type: Application
    Filed: November 5, 2018
    Publication date: July 11, 2019
    Inventors: David A. Spiegel, Patrick McEnaney, Kelly Fitzgerald
  • Publication number: 20190192497
    Abstract: The present invention relates to chimeric (including bifunctional) compounds, compositions comprising those compounds and methods of treating cancer in a patient or subject, especially including metastatic and other cancers where cancer cells exhibit overexpression (heightened expression) of cell surface urokinase-type plasminogen activator receptor (urokinase receptor) compared to normal (non-cancerous) cells.
    Type: Application
    Filed: August 3, 2017
    Publication date: June 27, 2019
    Inventors: David Spiegel, H. Marie Loughran, Jeffrey C. Pelletier, Allen B. Reitz, Matthew Ernest Welsch
  • Publication number: 20190127487
    Abstract: The present invention relates to chimeric chemical compounds which are used to recruit antibodies to cancer cells, in particular, prostate cancer cells or metastasized prostate cancer cells. The compounds according to the present invention comprise an antibody binding terminus (ABT) moiety covalently bonded to a cell binding terminus (CBT) through a linker and optionally, a connector molecule.
    Type: Application
    Filed: July 26, 2018
    Publication date: May 2, 2019
    Inventors: David Spiegel, Ryan Murelli, Andrew Zhang
  • Patent number: 10188727
    Abstract: The present invention is directed to new bifunctional compounds and methods for treating HIV infections. The bifunctional small molecules, generally referred to as ARM-H's, function through orthogonal pathways, by inhibiting the gp120-CD4 interaction, and by recruiting anti-DNP antibodies to gp120-expressing cells, thereby preventing cell infection and spread of HIV. It has been shown that ARM-H's bind to gp120 and gp-120 expressing cells competitively with CD4, thereby decreasing viral infectivity as shown by an MT-2 cell assay, the binding leading to formation of a ternary complex by recruiting anti-DNP antibodies to bind thereto, the antibodies present in the ternary complex promoting the complement-dependent destruction of the gp120-expressing cells. Compounds and methods are described herein.
    Type: Grant
    Filed: October 15, 2015
    Date of Patent: January 29, 2019
    Assignee: YALE UNIVERSITY
    Inventors: David Spiegel, Christopher Parker
  • Publication number: 20190002447
    Abstract: The present invention is directed to new bifunctional compounds and methods for treating HIV infections. The bifunctional small molecules, generally referred to as ARM-HI's, function through orthogonal pathways, by inhibiting the gp120-CD4 interaction, and by recruiting anti-DNP antibodies to gp120-expressing cells, thereby preventing cell infection and spread of HIV. It has been shown that ARM-HI's bind to gp120 and gp-120 expressing cells competitively with CD4, thereby decreasing viral infectivity as shown by an MT-2 cell assay, the binding leading to formation of a ternary complex by recruiting anti-DNP antibodies to bind thereto, the antibodies present in the ternary complex promoting the complement-dependent destruction of the gp120-expressing cells. Compounds and methods are described herein.
    Type: Application
    Filed: July 17, 2018
    Publication date: January 3, 2019
    Inventors: David Spiegel, Christopher Parker
  • Patent number: 10117943
    Abstract: The present invention relates to compounds which function as antibody mimetic compounds. These compounds are bifunctional/multifunctional compounds which contain at least one cancer cell binding moiety which selectively binds to prostate specific membrane antigen (PSMA) and a FC receptor binding moiety which modulates an FC immune receptor, preferably a Fc?RI receptor. Compounds according to the present invention bind selectively to cancer cells which upregulate PSMA and through that interaction, place the Fc receptor binding moiety of the compound in proximity to a Fc receptor, preferably a Fc?RI receptor, which can modulate (preferably, upregulate) a humoral response in a patient to cancer cells. Through this biological action of the compounds according to the present invention, cancer cells, including metastatic cancer cells, especially prostate cancer cells can be immune regulated, resulting in the favorable therapy of cancer in a patient.
    Type: Grant
    Filed: May 3, 2013
    Date of Patent: November 6, 2018
    Assignee: YALE UNIVERSITY
    Inventors: David A. Spiegel, Patrick McEnaney, Kelly Fitzgerald
  • Publication number: 20180311334
    Abstract: The invention provides a modified cell having an immunomodulatory molecule bound to the cell surface. In some aspects, the invention provides compositions and methods for the treatment and prevention of a microbial infection and microbial infection-related diseases and disorders. The present invention also provides methods of inducing an immune response against a pathogen.
    Type: Application
    Filed: April 27, 2018
    Publication date: November 1, 2018
    Inventors: Samir Gautam, Taehan Kim, David Spiegel
  • Publication number: 20180291031
    Abstract: Glucosepane is a structurally complex protein post-translational modification (PTM) believed to exist in all living organisms. Research in humans suggests that glucosepane plays a critical role in the pathophysiology of both diabetes and human aging; yet comprehensive biological investigations of this ‘metabolite have been’ greatly hindered by a scarcity of chemically homogeneous material available for study. Glucosepane possesses a unique chemical structure that incorporates a surprising, never-before-prepared non-aromatic tautomer of imidazole (hereafter termed an “iso-imidazole”), rendering it a challenging target for chemical synthesis. In this application, the inventors report the first total synthesis of glucosepane, enabled by the development of a novel one-pot method for preparation of the iso-imidazole core. The synthesis of the present invention is concise (8-steps starting from commercial materials), convergent, high-yielding (12% overall), and enantioselective.
    Type: Application
    Filed: September 23, 2016
    Publication date: October 11, 2018
    Applicant: Yale University
    Inventor: David SPIEGEL
  • Patent number: 10066026
    Abstract: The present invention relates to chimeric chemical compounds which are used to recruit antibodies to cancer cells, in particular, prostate cancer cells or metastasized prostate cancer cells. The compounds according to the present invention comprise an antibody binding terminus (ABT) moiety covalently bonded to a cell binding terminus (CBT) through a linker and optionally, a connector molecule.
    Type: Grant
    Filed: March 28, 2016
    Date of Patent: September 4, 2018
    Assignee: YALE UNIVERSITY
    Inventors: David Spiegel, Ryan Murelli, Andrew Zhang
  • Patent number: 10030008
    Abstract: The present invention is directed to new bifunctional compounds and methods for treating HIV infections. The bifunctional small molecules, generally referred to as ARM-HI's, function through orthogonal pathways, by inhibiting the gp120-CD4 interaction, and by recruiting anti-DNP antibodies to gp120-expressing cells, thereby preventing cell infection and spread of HIV. It has been shown that ARM-HI's bind to gp120 and gp-120 expressing cells competitively with CD4, thereby decreasing viral infectivity as shown by an MT-2 cell assay, the binding leading to formation of a ternary complex by recruiting anti-DNP antibodies to bind thereto, the antibodies present in the ternary complex promoting the complement-dependent destruction of the gp120-expressing cells. Compounds and methods are described herein.
    Type: Grant
    Filed: December 15, 2016
    Date of Patent: July 24, 2018
    Assignee: YALE UNIVERSITY
    Inventors: David Spiegel, Christopher Parker
  • Patent number: 10016412
    Abstract: The present invention relates to chimeric chemical compounds which are used to recruit antibodies to cancer cells, in particular, prostate cancer cells or metastasized prostate cancer cells. The compounds according to the present invention comprise an antibody binding terminus (ABT) moiety covalently bonded to a cell binding terminus (CBT) and Toll-like receptor agonist (TLR) through a linker and a multifunctional connector group or molecule.
    Type: Grant
    Filed: December 9, 2016
    Date of Patent: July 10, 2018
    Assignee: YALE UNIVERSITY
    Inventors: David Spiegel, Kelly Fitzgerald
  • Publication number: 20180155332
    Abstract: The present invention relates to chimeric (including bifunctional) compounds, compositions comprising those compounds and methods of treating cancer in a patient or subject, especially including metastatic cancer where cancer cells exhibit overexpression (heightened expression) of cell surface urokinase-type plasminogen activator receptor (urokinase receptor) compared to normal (non-cancerous) cells.
    Type: Application
    Filed: February 6, 2018
    Publication date: June 7, 2018
    Inventors: David Spiegel, Anthony Rullo
  • Patent number: 9745334
    Abstract: The present invention is directed to new bifunctional compounds and methods for treating HIV infections. The bifunctional small molecules, generally referred to as CDM-Hs, function through orthogonal pathways, by inhibiting the gp120-CD4 interaction, and by introducing cytotoxic moieties to gp120-expressing cells, thereby causing cell death and preventing cell infection and spread of HIV. It is shown that CDM-Hs bind to gp120 and gp-120 expressing cells competitively with CD4, and these compounds cause cell death of HIV-infected cells, thereby decreasing viral infectivity. Compounds and methods are described herein.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: August 29, 2017
    Assignee: YALE UNIVERSITY
    Inventors: David Spiegel, Christopher Parker
  • Patent number: 9622469
    Abstract: A preservative for body fluids, proteins, cells and tissues comprising an effective amount of an AGE crosslink breaker for preventing formation of advanced glycation end products. The AGE crosslink breaker comprises a compound of Structure (1): wherein V, W, X, Y and Z are any atom suitable for a heterocyclic carbene or carbene precursor framework, including B, C, O, N, S, Se, P, and As in any chemically-feasible oxidation state; wherein Q, R, M, T and U are any atom or substituent, including but not limited to, H, CLn, NLn, PLn, OLn, SLn, SeLn, LnCl, LnBr, LnI, wherein L is any atom, substituent or group, and n is any integer such that Q, R, M, T, and U can access all chemically-feasible oxidation states; and wherein G comprises any charged counter ion including, but not limited to those derived from C, O, N, B, Al, S, Se, Cl, Br, I in any chemically-feasible oxidation state.
    Type: Grant
    Filed: October 3, 2014
    Date of Patent: April 18, 2017
    Inventors: David Spiegel, Jeanne Hendrickson
  • Publication number: 20170096415
    Abstract: The present invention is directed to new bifunctional compounds and methods for treating HIV infections. The bifunctional small molecules, generally referred to as ARM-HI's, function through orthogonal pathways, by inhibiting the gp120-CD4 interaction, and by recruiting anti-DNP antibodies to gp120-expressing cells, thereby preventing cell infection and spread of HIV. It has been shown that ARM-HI's bind to gp120 and gp-120 expressing cells competitively with CD4, thereby decreasing viral infectivity as shown by an MT-2 cell assay, the binding leading to formation of a ternary complex by recruiting anti-DNP antibodies to bind thereto, the antibodies present in the ternary complex promoting the complement-dependent destruction of the gp120-expressing cells. Compounds and methods are described herein.
    Type: Application
    Filed: December 15, 2016
    Publication date: April 6, 2017
    Inventors: David Spiegel, Christopher Parker
  • Publication number: 20170087148
    Abstract: The present invention relates to chimeric chemical compounds which are used to recruit antibodies to cancer cells, in particular, prostate cancer cells or metastasized prostate cancer cells. The compounds according to the present invention comprise an antibody binding terminus (ABT) moiety covalently bonded to a cell binding terminus (CBT) and Toll-like receptor agonist (TLR) through a linker and a multifunctional connector group or molecule.
    Type: Application
    Filed: December 9, 2016
    Publication date: March 30, 2017
    Inventors: David Spiegel, Kelly Fitzgerald
  • Patent number: 9562038
    Abstract: The present invention is directed to new bifunctional compounds and methods for treating HIV infections. The bifunctional small molecules, generally referred to as ARM-HI's, function through orthogonal pathways, by inhibiting the gp120-CD4 interaction, and by recruiting anti-DNP antibodies to gp120-expressing cells, thereby preventing cell infection and spread of HIV. It has been shown that ARM-HI's bind to gp120 and gp-120 expressing cells competitively with CD4, thereby decreasing viral infectivity as shown by an MT-2 cell assay, the binding leading to formation of a ternary complex by recruiting anti-DNP antibodies to bind thereto, the antibodies present in the ternary complex promoting the complement-dependent destruction of the gp120-expressing cells. Compounds and methods are described herein.
    Type: Grant
    Filed: November 17, 2011
    Date of Patent: February 7, 2017
    Assignee: YALE UNIVERSITY
    Inventors: David Spiegel, Christopher Parker
  • Patent number: 9556167
    Abstract: The present invention relates to chimeric chemical compounds which are used to recruit antibodies to cancer cells, in particular, prostate cancer cells or metastasized prostate cancer cells. The compounds according to the present invention comprise an antibody binding terminus (ABT) moiety covalently bonded to a cell binding terminus (CBT) and Toll-like receptor agonist (TLR) through a linker and a multifunctional connector group or molecule.
    Type: Grant
    Filed: May 1, 2013
    Date of Patent: January 31, 2017
    Assignee: YALE UNIVERSITY
    Inventors: David Spiegel, Kelly Fitzgerald
  • Publication number: 20160347863
    Abstract: The present invention relates to chimeric chemical compounds which are used to recruit antibodies to cancer cells, in particular, prostate cancer cells or metastasized prostate cancer cells. The compounds according to the present invention comprise an antibody binding terminus (ABT) moiety covalently bonded to a cell binding terminus (CBT) through a linker and optionally, a connector molecule.
    Type: Application
    Filed: March 28, 2016
    Publication date: December 1, 2016
    Inventors: David Spiegel, Ryan Murelli, Andrew Zhang