Patents by Inventor Ethan R. Signer

Ethan R. Signer 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: 20110009343
    Abstract: Compounds that modulate the aggregation of amyloidogenic proteins or peptides are disclosed. The modulators of the invention can promote amyloid aggregation or, more preferably, can inhibit natural amyloid aggregation. In a preferred embodiment, the compounds modulate the aggregation of natural ? amyloid peptides (?-AP). In a preferred embodiment, the ? amyloid modulator compounds of the invention are comprised of an A? aggregation core domain and a modifying group coupled thereto such that the compound alters the aggregation or inhibits the neurotoxicity of natural ? amyloid peptides when contacted with the peptides. Furthermore, the modulators are capable of altering natural ?-AP aggregation when the natural ?-APs are in a molar excess amount relative to the modulators. Pharmaceutical compositions comprising the compounds of the invention, and diagnostic and treatment methods for amyloidogenic diseases using the compounds of the invention, are also disclosed.
    Type: Application
    Filed: December 21, 2009
    Publication date: January 13, 2011
    Applicant: Praecis Pharmaceuticals, Inc.
    Inventors: Mark A. Findeis, Howard Benjamin, Marc B. Garnick, Malcolm L. Gefter, Arvind Hundal, Laura Kasman, Gary Musso, Ethan R. Signer, James Wakefield, Michael J. Reed
  • Patent number: 7658917
    Abstract: Compounds that modulate the aggregation of amyloidogenic proteins or peptides are disclosed. The modulators of the invention can promote amyloid aggregation or, more preferably, can inhibit natural amyloid aggregation. In a preferred embodiment, the compounds modulate the aggregation of natural ? amyloid peptides (?-AP). In a preferred embodiment, the ? amyloid modulator compounds of the invention are comprised of an A? aggregation core domain and a modifying group coupled thereto such that the compound alters the aggregation or inhibits the neurotoxicity of natural ? amyloid peptides when contacted with the peptides. Furthermore, the modulators are capable of altering natural ?-AP aggregation when the natural ?-APs are in a molar excess amount relative to the modulators. Pharmaceutical compositions comprising the compounds of the invention, and diagnostic and treatment methods for amyloidogenic diseases using the compounds of the invention, are also disclosed.
    Type: Grant
    Filed: June 17, 2003
    Date of Patent: February 9, 2010
    Assignee: Praecis Pharmaceuticals, Inc.
    Inventors: Mark A. Findeis, Howard Benjamin, Marc B. Garnick, Malcolm L. Gefter, Arvind Hundal, Ethan R. Signer, James Wakefield, Laura Kasman, Gary Musso, Michael J. Reed
  • Patent number: 7175828
    Abstract: Compounds that modulate natural ? amyloid peptide aggregation are provided. The modulators of the invention comprise a peptide, preferably based on a ? amyloid peptide, that is comprised entirely of D-amino acids. Preferably, the peptide comprises 3–5 D-amino acid residues and includes at least two D-amino acid residues independently selected from the group consisting of D-leucine, D-phenylalanine and D-valine. In a particularly preferred embodiment, the peptide is a retro-inverso isomer of a ? amyloid peptide, preferably a retro-inverso isomer of A?17-21. In certain embodiments, the peptide is modified at the amino-terminus, the carboxy-terminus, or both. Preferred amino-terminal modifying groups include cyclic, heterocyclic, polycyclic and branched alkyl groups. Preferred carboxy-terminal modifying groups include an amide group, an alkyl amide group, an aryl amide group or a hydroxy group.
    Type: Grant
    Filed: September 30, 2003
    Date of Patent: February 13, 2007
    Assignee: Praecis Pharmaceuticals, Inc.
    Inventors: Mark A. Findeis, Malcolm L. Gefter, Gary F. Musso, Ethan R. Signer, James Wakefield, Susan Molineaux, Joseph Chin, Jung-Ja Lee, Michael Kelley, Sonja Komar, Christopher C. Arico-Muendel, Kathryn Phillips, Neil J. Hayward
  • Publication number: 20040091904
    Abstract: Methods for identifying a compound that binds to a target are described. In general, the methods involve forming a first library comprising a multiplicity of peptides, identifying one or more peptides that bind to the target and determining a peptide motif therefrom, forming a second library comprising a multiplicity of compounds designed based on the peptide motif, selecting from the second library at least one compound that binds to the target, and determining the structure or structures of the at least one compound that binds to the target. Libraries of compounds based on a peptide motif and compounds identified by the methods of the invention are also disclosed.
    Type: Application
    Filed: June 30, 2003
    Publication date: May 13, 2004
    Inventors: Howard Benjamin, Mark A. Findeis, Malcolm L. Gefter, Gary Musso, Ethan R. Signer
  • Patent number: 6689752
    Abstract: Compounds that modulate natural &bgr; amyloid peptide aggregation are provided. The modulators of the invention comprise a peptide, preferably based on a &bgr; amyloid peptide, that is comprised entirely of D-amino acids. Preferably, the peptide comprises 3-5 D-amino acid residues and includes at least two D-amino acid residues independently selected from the group consisting of D-leucine, D-phenylalanine and D-valine. In a particularly preferred embodiment, the peptide is a retro-inverso isomer of a &bgr; amyloid peptide, preferably a retro-inverso isomer of A&bgr;17-21. In certain embodiments, the peptide is modified at the amino-terminus, the carboxy-terminus, or both. Preferred amino-terminal modifying groups include cyclic, heterocyclic, polycyclic and branched alkyl groups. Preferred carboxy-terminal modifying groups include an amide group, an alkyl amide group, an aryl amide group or a hydroxy group.
    Type: Grant
    Filed: June 29, 2001
    Date of Patent: February 10, 2004
    Assignee: Praecis Pharmaceuticals, Incorporated
    Inventors: Mark A. Findeis, Malcolm L. Gefter, Gary Musso, Ethan R. Signer, James Wakefield, Susan Molineaux, Joseph Chin, Jung-Ja Lee, Michael Kelley, Sonja Komar-Panicucci, Christopher C. Arico-Muendel, Kathryn Phillips, Neil J. Hayward
  • Publication number: 20040005307
    Abstract: Compounds that modulate the aggregation of amyloidogenic proteins or peptides are disclosed. The modulators of the invention can promote amyloid aggregation or, more preferably, can inhibit natural amyloid aggregation. In a preferred embodiment, the compounds modulate the aggregation of natural &bgr; amyloid peptides (&bgr;-AP). In a preferred embodiment, the &bgr; amyloid modulator compounds of the invention are comprised of an A&bgr; aggregation core domain and a modifying group coupled thereto such that the compound alters the aggregation or inhibits the neurotoxicity of natural &bgr; amyloid peptides when contacted with the peptides. Furthermore, the modulators are capable of altering natural &bgr;-AP aggregation when the natural &bgr;-APs are in a molar excess amount relative to the modulators. Pharmaceutical compositions comprising the compounds of the invention, and diagnostic and treatment methods for amyloidogenic diseases using the compounds of the invention, are also disclosed.
    Type: Application
    Filed: June 17, 2003
    Publication date: January 8, 2004
    Applicant: Praecis Pharmaceuticals, Inc.
    Inventors: Mark A. Findeis, Howard Benjamin, Marc B. Garnick, Malcolm L. Gefter, Arvind Hundal, Laura Kasman, Gary Musso, Ethan R. Signer, James Wakefield, Michael J. Reed
  • Publication number: 20030154518
    Abstract: The subject application provides methods and materials useful for the transformation of eukaryotic cells, particularly plant cells. More specifically, the subject invention provides materials and methods for eliminating selectable marker genes from transformed cells. In a preferred embodiment the subject invention provides methods for removing both positive and negative selectable marker genes from plant cells after a gene of interest has been introduced into the plant cells. The methods of the subject invention are applicable to any gene of interest, in any plant species that can be transformed.
    Type: Application
    Filed: June 12, 2001
    Publication date: August 14, 2003
    Inventors: Ethan R. Signer, J. Ranjan Perera
  • Publication number: 20030100007
    Abstract: Methods for identifying a compound that binds to a target are described. In general, the methods involve forming a first library comprising a multiplicity of peptides, identifying one or more peptides that bind to the target and determining a peptide motif therefrom, forming a second library comprising a multiplicity of compounds designed based on the peptide motif, selecting from the second library at least one compound that binds to the target, and determining the structure or structures of the at least one compound that binds to the target. Libraries of compounds based on a peptide motif and compounds identified by the methods of the invention are also disclosed.
    Type: Application
    Filed: December 18, 1996
    Publication date: May 29, 2003
    Inventors: HOWARD BENJAMIN, MARK A. FINDEIS, MALCOLM L. GEFTER, GARY MUSSO, ETHAN R. SIGNER
  • Publication number: 20020103134
    Abstract: Compounds that modulate natural &bgr; amyloid peptide aggregation are provided. The modulators of the invention comprise a peptide, preferably based on a &bgr; amyloid peptide, that is comprised entirely of D-amino acids. Preferably, the peptide comprises 3-5 D-amino acid residues and includes at least two D-amino acid residues independently selected from the group consisting of D-leucine, D-phenylalanine and D-valine. In a particularly preferred embodiment, the peptide is a retro-inverso isomer of a &bgr; amyloid peptide, preferably a retro-inverso isomer of A&bgr;17-21. In certain embodiments, the peptide is modified at the amino-terminus, the carboxy-terminus, or both. Preferred amino-terminal modifying groups include cyclic, heterocyclic, polycyclic and branched alkyl groups. Preferred carboxy-terminal modifying groups include an amide group, an alkyl amide group, an aryl amide group or a hydroxy group.
    Type: Application
    Filed: June 29, 2001
    Publication date: August 1, 2002
    Applicant: Praecis Pharmaceuticals Inc.
    Inventors: Mark A. Findeis, Malcolm L. Gefter, Gary Musso, Ethan R. Signer, James Wakefield, Susan Molineaux, Joseph Chin, Jung-Ja Lee, Michael Kelley, Sonja Komar-Panicucci, Christopher C. Arico-Muendel, Kathryn Phillips, Neil J. Hayward
  • Publication number: 20020098173
    Abstract: Compounds that modulate the aggregation of amyloidogenic proteins or peptides are disclosed. The modulators of the invention can promote amyloid aggregation or, more preferably, can inhibit natural amyloid aggregation. In a preferred embodiment, the compounds modulate the aggregation of natural &bgr; amyloid peptides (&bgr;-AP). In a preferred embodiment, the &bgr; amyloid modulator compounds of the invention are comprised of an A&bgr; aggregation core domain and a modifying group coupled thereto such that the compound alters the aggregation or inhibits the neurotoxicity of natural &bgr; amyloid peptides when contacted with the peptides. Furthermore, the modulators are capable of altering natural &bgr;-AP aggregation when the natural &bgr;-APs are in a molar excess amount relative to the modulators. Pharmaceutical compositions comprising the compounds of the invention, and diagnostic and treatment methods for amyloidogenic diseases using the compounds of the invention, are also disclosed.
    Type: Application
    Filed: October 4, 2001
    Publication date: July 25, 2002
    Applicant: Praecis Pharmaceuticals, Inc.
    Inventors: Mark A. Findeis, Howard Benjamin, Marc B. Garnick, Malcolm L. Gefter, Arvind Hundal, Laura Kasman, Gary Musso, Ethan R. Signer, James Wakefield, Michael J. Reed
  • Patent number: 6319498
    Abstract: Compounds that modulate the aggregation of amyloidogenic proteins or peptides are disclosed. The modulators of the invention can promote amyloid aggregation or, more preferably, can inhibit natural amyloid aggregation. In a preferred embodiment, the compounds modulate the aggregation of natural &bgr; amyloid peptides (&bgr;-AP). In a preferred embodiment, the &bgr; amyloid modulator compounds of the invention are comprised of an A&bgr; aggregation core domain and a modifying group coupled thereto such that the compound alters the aggregation or inhibits the neurotoxicity of natural &bgr; amyloid peptides when contacted with the peptides. Furthermore, the modulators are capable of altering natural &bgr;-AP aggregation when the natural &bgr;-APs are in a molar excess amount relative to the modulators. Pharmaceutical compositions comprising the compounds of the invention, and diagnostic and treatment methods for amyloidogenic diseases using the compounds of the invention, are also disclosed.
    Type: Grant
    Filed: March 14, 1996
    Date of Patent: November 20, 2001
    Assignee: Praecis Pharmaceuticals Incorporated
    Inventors: Mark A. Findeis, Howard Benjamin, Marc B. Garnick, Malcolm L. Gefter, Arvind Hundal, Laura Kasman, Gary Musso, Ethan R. Signer, James Wakefield, Michael J. Reed
  • Patent number: 6303567
    Abstract: Compounds that modulate natural &bgr; amyloid peptide aggregation are provided. The modulators of the invention comprise a peptide, preferably based on a &bgr; amyloid peptide, that is comprised entirely of D-amino acids. Preferably, the peptide comprises 3-5 D-amino acid residues and includes at least two D-amino acid residues independently selected from the group consisting of D-leucine, D-phenylalanine and D-valine. In a particularly preferred embodiment, the peptide is a retro-inverso isomer of a &bgr; amyloid peptide, preferably a retro-inverso isomer of A&bgr;17-21. In certain embodiments, the peptide is modified at the amino-terminus, the carboxy-terminus, or both. Preferred amino-terminal modifying groups include cyclic, heterocyclic, polycyclic and branched alkyl groups. Preferred carboxy-terminal modifying groups include an amide group, an alkyl amide group, an aryl amide group or a hydroxy group.
    Type: Grant
    Filed: August 27, 1996
    Date of Patent: October 16, 2001
    Assignee: Praecis Pharmaceuticals, Inc .
    Inventors: Mark A. Findeis, Malcolm L. Gefter, Gary Musso, Ethan R. Signer, James Wakefield, Susan Molineaux, Joseph Chin, Jung-Ja Lee, Michael Kelley, Sonja Komar-Panicucci, Christopher C. Arico-Muendel, Kathryn Phillips, Neil J. Hayward
  • Patent number: 6277826
    Abstract: Compounds that modulate natural &bgr; amyloid peptide aggregation are provided. The modulators of the invention comprise a peptide, preferably based on a &bgr; amyloid peptide, that is comprised entirely of D-amino acids. Preferably, the peptide comprises 3-5 D-amino acid residues and includes at least two D-amino acid residues independently selected from the group consisting of D-leucine, D-phenylalanine and D-valine. In a particularly preferred embodiment, the peptide is a retro-inverso isomer of a &bgr; amyloid peptide, preferably a retro-inverso isomer of A&bgr;17-21. In certain embodiments, the peptide is modified at the amino-terminus, the carboxy-terminus, or both. Preferred amino-terminal modifying groups include cyclic, heterocyclic, polycyclic and branched alkyl groups. Preferred carboxy-terminal modifying groups include an amide group, an alkyl amide group, an aryl amide group or a hydroxy group.
    Type: Grant
    Filed: July 19, 1999
    Date of Patent: August 21, 2001
    Assignee: Praecis Pharmaceuticals, Inc.
    Inventors: Mark A. Findeis, Malcolm L. Gefter, Gary Musso, Ethan R. Signer, James Wakefield, Susan Molineaux, Joseph Chin, Jung-Ja Lee, Michael Kelley, Sonja Komar-Panicucci, Christopher C. Arico-Muendel, Kathryn Phillips, Neil J. Hayward
  • Publication number: 20010006778
    Abstract: Methods for identifying a compound that binds to a target are described. In general, the methods involve forming a first library comprising a multiplicity of peptides, identifying one or more peptides that bind to the target and determining a peptide motif therefrom, forming a second library comprising a multiplicity of compounds designed based on the peptide motif, selecting from the second library at least one compound that binds to the target, and determining the structure or structures of the at least one compound that binds to the target. Libraries of compounds based on a peptide motif and compounds identified by the methods of the invention are also disclosed.
    Type: Application
    Filed: January 26, 2001
    Publication date: July 5, 2001
    Applicant: Praecis Pharmaceuticals Incorporated
    Inventors: Howard Benjamin, Mark A. Findeis, Malcolm L. Gefter, Gary Musso, Ethan R. Signer
  • Patent number: 6214795
    Abstract: This invention provides peptide compounds that bind to either a fibroblast growth factor (FGF) or a fibroblast growth factor receptor (FGFR) and, accordingly, are useful for modulating FGFR activity. Preferably, the FGFR is FGFR2-IIIC. Preferably, the FGF is basic FGF. Preferably the peptide compound comprises an amino acid sequence: (Y/F)-(L/F/I)-(R/D/E/S/Y/G)-(Q/L/Y)-Y-(M/L/K/R)-(L/M/D/E/N/S)-(R/L/S/T)-(L/F/M/V) (SEQ ID NO: 1). The invention further comprises pharmaceutical compositions comprising the peptide compounds of the invention and a pharmaceutically acceptable carrier. The invention still further provides methods of modulating FGFR activity using the peptide compounds of the invention.
    Type: Grant
    Filed: November 12, 1996
    Date of Patent: April 10, 2001
    Assignee: Praecis Pharmaceuticals, Inc.
    Inventors: Howard Benjamin, Ling Chai, Mark A. Findeis, William Goodwin, Arvind Hundal, David I. Israel, Michael Kelley, Martin P. Keough, Kuanghui Lu, Farah Natoli, Alicia Peticolas, Ethan R. Signer, Malcolm L. Gefter
  • Patent number: 5985242
    Abstract: Compounds that modulate natural .beta. amyloid peptide aggregation are provided. The modulators of the invention comprise a peptide, preferably based on a .beta. amyloid peptide, that is comprised entirely of D-amino acids. Preferably, the peptide comprises 3-5 D-amino acid residues and includes at least two D-amino acid residues independently selected from the group consisting of D-leucine, D-phenylalanine and D-valine. In a particularly preferred embodiment, the peptide is a retro-inverso isomer of a .beta. amyloid peptide, preferably a retro-inverso isomer of A.beta..sub.17-21. In certain embodiments, the peptide is modified at the amino-terminus, the carboxy-terminus, or both. Preferred amino-terminal modifying groups include cyclic, heterocyclic, polycyclic and branched alkyl groups. Preferred carboxy-terminal modifying groups include an amide group, an alkyl amide group, an aryl amide group or a hydroxy group.
    Type: Grant
    Filed: August 27, 1997
    Date of Patent: November 16, 1999
    Assignee: Praecis Pharmaceuticals, Inc.
    Inventors: Mark A. Findeis, Malcolm L. Gefter, Gary Musso, Ethan R. Signer, James Wakefield, Susan Molineaux, Joseph Chin, Jung-Ja Lee, Michael Kelley, Sonja Komar-Panicucci, Christopher C. Arico-Muendel, Kathryn Phillips, Neil J. Hayward
  • Patent number: 5854204
    Abstract: Compounds that modulate the aggregation of amyloidogenic proteins or peptides are disclosed. The modulators of the invention can promote amyloid aggregation or, more preferably, can inhibit natural amyloid aggregation. In a preferred embodiment, the compounds modulate the aggregation of natural .beta. amyloid peptides (.beta.-AP). In a preferred embodiment, the .beta. amyloid modulator compounds of the invention are comprised of an A.beta. aggregation core domain and a modifying group coupled thereto such that the compound alters the aggregation or inhibits the neurotoxicity of natural .beta. amyloid peptides when contacted with the peptides. Furthermore, the modulators are capable of altering natural .beta.-AP aggregation when the natural .beta.-APs are in a molar excess amount relative to the modulators. Pharmaceutical compositions comprising the compounds of the invention, and diagnostic and treatment methods for amyloidogenic diseases using the compounds of the invention, are also disclosed.
    Type: Grant
    Filed: March 14, 1996
    Date of Patent: December 29, 1998
    Assignee: Praecis Pharmaceuticals, Inc.
    Inventors: Mark A. Findeis, Howard Benjamin, Marc B. Garnick, Malcolm L. Gefter, Arvind Hundal, Laura Kasman, Gary Musso, Ethan R. Signer, James Wakefield, Michael Reed, Susan Molineaux, William Kubasek, Joseph Chin, Jung-Ja Lee, Michael Kelley
  • Patent number: 5854215
    Abstract: Compounds that act to modulate the aggregation of natural .beta. amyloid peptides (.beta.-AP) are disclosed. The .beta. amyloid modulators of the invention can promote .beta.-AP aggregation or, more preferably, can inhibit natural .beta.-AP aggregation. Furthermore, the modulators are capable of altering natural .beta.-AP aggregation when the natural .beta.-APs are in a molar excess amount relative to the modulators. Pharmaceutical compositions comprising the compounds of the invention, and methods of altering natural .beta.-AP aggregation using the compounds of the invention, are also disclosed.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: December 29, 1998
    Assignee: Praecis Pharmaceuticals Incorporated
    Inventors: Mark A. Findeis, Howard Benjamin, Marc B. Garnick, Malcolm L. Gefter, Arvind Hundal, Laura Kasman, Gary Musso, Ethan R. Signer, James Wakefield, Michael J. Reed
  • Patent number: 5817626
    Abstract: Compounds that act to modulate the aggregation of natural .beta. amyloid peptides (.beta.-AP) are disclosed. The .beta. amyloid modulators of the invention can promote .beta.-AP aggregation or, more preferably, can inhibit natural .beta.-AP aggregation. Furthermore, the modulators are capable of altering natural .beta.-AP aggregation when the natural .beta.-APs are in a molar excess amount relative to the modulators. Preferred .beta. amyloid modulators comprise amino-terminally biotinylated .beta. amyloid peptide compounds. Pharmaceutical compositions comprising the compounds of the invention, and methods of altering natural .beta.-AP aggregation using the compounds of the invention, are also disclosed.
    Type: Grant
    Filed: March 14, 1995
    Date of Patent: October 6, 1998
    Assignee: Praecis Pharmaceuticals Incorporated
    Inventors: Mark A. Findeis, Howard Benjamin, Marc B. Garnick, Malcolm L. Gefter, Arvind Hundal, Laura Kasman, Gary Musso, Ethan R. Signer, James Wakefield, Michael J. Reed