Patents Assigned to Trega Biosciences, Inc.
  • 4-Substituted-quinoline derivatives and 4-substituted-quinoline combinatorial libraries
    Patent number: 6262269
    Abstract: The present invention relates to novel 4-substituted quinoline compounds of the following formula, libraries containing such compounds, and to the generation of such combinatorial libraries composed of such compounds: wherein R1, R2, R3, R4, R5, R6, R7, R9, and Y, have the meanings provided.
    Type: Grant
    Filed: February 3, 1998
    Date of Patent: July 17, 2001
    Assignee: Trega Biosciences, Inc.
    Inventors: Thomas K. Hayes, Behrouz Forood, John S. Kiely
  • Cytokine restraining agents
    Patent number: 6245738
    Abstract: The present invention provides novel cytokine restraining agents, which limit or control the biological activity of cytokines. The invention also provides pharmaceutical compositions comprising a cytokine restraining peptide and methods of administering the pharmaceutical composition to a subject. The invention further provides methods for using the novel peptides to restrain cytokine activity in a subject.
    Type: Grant
    Filed: November 9, 1994
    Date of Patent: June 12, 2001
    Assignee: Trega Biosciences, Inc.
    Inventors: Mark J. Suto, Beverly E. Girten, Richard A. Houghten, Costas C. Loullis, Ronald R. Tuttle
  • Selectively N-alkylated peptidomimetic combinatorial libraries and compounds therein
    Patent number: 6143932
    Abstract: The instant invention is directed to a single, selectively N-alkylated compound and libraries of such compounds as set forth in Formula I. Furthermore, the instant invention is directed to methods of effecting analgesia, a decrease in the postprandial rise in the blood glucose levels of a mammal after ingestion of a carbohydrate load by said mammal, and treating microbial infections, utilizing such a single compound of Formula I in conjunction with a pharmaceutically-acceptable carrier. Also, the instant invention is directed to methods for selective alkylation, positional scanning and iterative synthetic and screening technologies.
    Type: Grant
    Filed: July 1, 1999
    Date of Patent: November 7, 2000
    Assignee: Trega Biosciences, Inc.
    Inventors: Barbara Dorner, John M. Ostresh, Colette T. Dooley, Richard A. Houghten, Jutta Eichler
  • Quinoline derivatives and quinoline combinatorial libraries
    Patent number: 6143895
    Abstract: The present invention relates to novel tetrahydro-quinoline compounds of the following formula, libraries containing such compounds, and to the generation of such combinatorial libraries composed of such compounds: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8 and Y have the meanings provided.
    Type: Grant
    Filed: August 20, 1998
    Date of Patent: November 7, 2000
    Assignee: Trega Biosciences, Inc.
    Inventors: Yazhong Pei, John S. Kiely
  • Method for separation of liquid and solid phases for solid phase organic syntheses
    Patent number: 6121054
    Abstract: A simple, efficient apparatus and method for separation of solid and liquid phases useful in methods of high-throughput combinatorial organic synthesis of large libraries or megaarrays of organic compounds is disclosed. The apparatus and method are useful, whether as part of an automated, robotic or manual system for combinatorial organic synthesis. In a preferred embodiment, an apparatus and method of removal of liquid phase from solid phase compatible with microtiter plate type array(s) of reaction vessels is disclosed.
    Type: Grant
    Filed: November 19, 1997
    Date of Patent: September 19, 2000
    Assignee: Trega Biosciences, Inc.
    Inventor: Michal Lebl
  • Selectively N-alkylated peptidomimetic combinatorial libraries and compounds therein
    Patent number: 6121489
    Abstract: The instant invention is directed to a single, selectively N-alkylated compound and libraries of such compounds as set forth in Formula I. Furthermore, the instant invention is directed to methods of effecting analgesia, a decrease in the postprandial rise in the blood glucose levels of a mammal after ingestion of a carbohydrate load by said mammal, and treating microbial infections, utilizing such a single compound of Formula I in conjunction with a pharmaceutically-acceptable carrier. Also, the instant invention is directed to methods for selective alkylation, positional scanning and iterative synthetic and screening technologies.
    Type: Grant
    Filed: March 5, 1997
    Date of Patent: September 19, 2000
    Assignee: Trega Biosciences, Inc.
    Inventors: Barbara Dorner, John M. Ostresh, Colette T. Dooley, Richard A. Houghten, Jutta Eichler
  • Apparatus and method for combinatorial chemistry synthesis
    Patent number: 6045755
    Abstract: In a first embodiment, this invention includes an integrated robot apparatus for performing combinatorial chemistry synthesis protocols and having interchangeable work-stations, robot arm tools, and reaction vessels and reaction vessel arrays. The work-stations and tools are specialized to perform tasks necessary for the synthesis in a plurality of the reaction vessels grouped in a plurality of the reaction vessel arrays. Preferably, these elements function interchangeably because they have standardized sizes and conformation. The work-stations and tools include those for fluid dispensing or aspirating from individual reaction vessels or from all the reaction vessels in an array simultaneously. The reaction vessels can include, alternatively, stackable, ball-sealed reaction vessels, microtitre-like reaction vessel arrays, arrays of independent reaction vessels, valve-sealed reaction vessels, septum-sealed reaction vessels, and syringe reaction vessels.
    Type: Grant
    Filed: March 10, 1997
    Date of Patent: April 4, 2000
    Assignee: Trega Biosciences,, Inc.
    Inventors: Michael Lebl, Vit Pokorny, Viktor Krchnak
  • Tricyclic Tetrahydroquinoline derivatives and tricyclic tetrahydroquinoline combinatorial libraries
    Patent number: 5925527
    Abstract: The present invention relates to novel tricyclic tetrahydroquinoline compounds of the following formula, libraries containing such compounds, and to the generation of such combinatorial libraries composed of such compounds: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, n, and Y have the meanings provided.
    Type: Grant
    Filed: February 5, 1997
    Date of Patent: July 20, 1999
    Assignee: Trega Biosciences, Inc.
    Inventors: Thomas K. Hayes, John S. Kiely
  • Isoquinoline derivatives and isoquinoline combinatorial libraries
    Patent number: 5916899
    Abstract: The present invention provides the synthesis of heterocyclic compounds based on the isoquinoline ring. More specifically, the invention provides novel isoquinolines as well as novel libraries comprised of many such compounds, and methods of synthesizing the libraries.
    Type: Grant
    Filed: October 18, 1996
    Date of Patent: June 29, 1999
    Assignee: Trega Biosciences, Inc.
    Inventors: John S. Kiely, Michael C. Griffith
  • Use of cytokine restraining agents to treat inflammatory bowel disease
    Patent number: 5888969
    Abstract: The present invention relates to the use of cytokine restraining agents to treat inflammatory bowel disease.
    Type: Grant
    Filed: July 14, 1997
    Date of Patent: March 30, 1999
    Assignee: Trega Biosciences, Inc.
    Inventors: Beverly E. Girten, Ronald R. Tuttle
  • Method for reducing the severity of gastro-intestinal damage
    Patent number: 5888978
    Abstract: The present invention provides methods for reducing the severity of GI damage in an individual by administering a cytokine regulatory agent to an individual that is susceptible to developing such damage.
    Type: Grant
    Filed: September 12, 1995
    Date of Patent: March 30, 1999
    Assignee: Trega Biosciences, Inc.
    Inventors: Beverly E. Girten, Paul Omholt, Ronald R. Tuttle
  • Isoquinoline derivatives and isoquinoline combinatorial libraries
    Patent number: 5874443
    Abstract: The present invention provides the synthesis of heterocyclic compounds based on the isoquinoline ring. More specifically, the invention provides novel isoquinolines as well as novel libraries comprised of many such compounds, and methods of synthesizing the libraries.
    Type: Grant
    Filed: October 18, 1996
    Date of Patent: February 23, 1999
    Assignee: Trega Biosciences, Inc.
    Inventors: John S. Kiely, Michael C. Griffith
  • Combinatorial libraries of hydantoin and thiohydantoin derivatives, methods of making the libraries and compounds therein
    Patent number: 5859190
    Abstract: The invention provides a rapid approach for combinatorial synthesis and screening of libraries of hydantoin and thiohydantoin compounds. The present invention further provides the compounds made by the combinatorial synthesis.
    Type: Grant
    Filed: February 4, 1997
    Date of Patent: January 12, 1999
    Assignee: Trega Biosciences, Inc.
    Inventors: Jean-Philippe Meyer, John M. Ostresh, Richard A. Houghten
  • Combinatorial libraries of imidazol-pyrido-indole and imidazol-pyrido-benzothiophene derivatives, methods of making the libraries and compounds therein
    Patent number: 5856107
    Abstract: The invention provides a rapid approach for combinatorial synthesis and screening of libraries of imidazol-pyrido-indole and imidazol-pyrido-benzothiophene compounds. The present invention further provides methods of preparing the libraries and the individual compounds made by the combinatorial synthesis.
    Type: Grant
    Filed: February 4, 1997
    Date of Patent: January 5, 1999
    Assignee: Trega Biosciences, Inc.
    Inventors: John M. Ostresh, Richard A. Houghten
  • Protected biopolymers for oral administration and methods of using same
    Patent number: 5846525
    Abstract: The present invention provides a composition comprising an ion exchange resin and a therapeutically active biopolymer in a form for oral administration. The present invention also provides a composition comprising Amberlite.RTM. IRP-64 and a cytokine regulatory agent having the amino acid sequence:Ac-Nle-Gln-His-(D)Phe-Arg-(D)Trp-Gly-NH.sub.2,in a form for oral administration. The present invention further provides a method of protecting a therapeutically active biopolymer from degradation by forming a complex of the biopolymer and an ion exchange resin. In addition, the present invention provides a method of reducing or inhibiting the severity of a pathological condition by orally administering a therapeutically effective dose of the composition.
    Type: Grant
    Filed: December 19, 1995
    Date of Patent: December 8, 1998
    Assignee: Trega Biosciences, Inc.
    Inventors: Manoj Maniar, Steven Mauch
  • Quinoline derivatives and quinoline combinatorial libraries
    Patent number: 5840500
    Abstract: The present invention relates to novel tetrahydro-quinoline compounds of the following formula, libraries containing such compounds, and to the generation of such combinatorial libraries composed of such compounds: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8 and Y have the meanings provided.
    Type: Grant
    Filed: July 11, 1996
    Date of Patent: November 24, 1998
    Assignee: Trega Biosciences, Inc.
    Inventors: Yazhong Pei, John S. Kiely
  • Cytokine restraining agents and methods of use in pathologies and conditions associated with altered cytokine levels
    Patent number: 5786332
    Abstract: The present invention relates to novel peptides that are potent cytokine restraining agents. In addition, the present invention relates to pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a cytokine restraining agent. Administration of such a cytokine restraining agent to a subject restrains, but does not necessarily suppress, cytokine activity completely. Thus, the present invention provides a method of restraining pathologically elevated cytokine activity in a subject. The invention also provides methods of treating disuse deconditioning and diseases mediated by nitric oxide and cytokines, such as diabetes and glomerulonephritis, a method of organ protection, a method of organ protection, and a method of reducing the negative side effects of cancer chemotherapy, such as nephrotoxicity.
    Type: Grant
    Filed: March 6, 1995
    Date of Patent: July 28, 1998
    Assignee: Trega Biosciences, Inc.
    Inventors: Beverly E. Girten, Richard A. Houghten, Costas C. Loullis, Mark J. Suto, Ronald R. Tuttle
  • Combinatorial libraries of cyclic urea and cyclic thiourea derivatives and compounds therein
    Patent number: 5786448
    Abstract: The invention provides a rapid approach for combinatorial synthesis and screening of libraries of cyclic urea and cyclic thiourea compounds. The present invention further provides the compounds made by the combinatorial synthesis.
    Type: Grant
    Filed: November 7, 1996
    Date of Patent: July 28, 1998
    Assignee: Trega Biosciences, Inc.
    Inventors: Adel Nefzi, John M. Ostresh, Richard Houghten
  • Synthesis of quinazolinone libraries and derivatives thereof
    Patent number: 5783577
    Abstract: The present invention provides synthetic combinatorial libraries of organic compounds based on the quinazolinone ring.
    Type: Grant
    Filed: September 13, 1996
    Date of Patent: July 21, 1998
    Assignee: Trega Biosciences, Inc.
    Inventors: Richard A. Houghten, John M. Ostresh
  • Cytokine restraining agents and methods of use in pathologies and conditions associated with altered cytokine levels
    Patent number: 5760001
    Abstract: The present invention relates to novel peptides that are potent cytokine restraining agents. In addition, the present invention relates to pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a cytokine restraining agent. Administration of such a cytokine restraining agent to a subject restrains, but does not necessarily suppress, cytokine activity completely. Thus, the present invention provides a method of restraining pathologically elevated cytokine activity in a subject. The invention also provides methods of treating disuse deconditioning and diseases mediated by nitric oxide and cytokines, such as diabetes and glomerulonephritis, a method of organ protection, a method of organ protection, and a method of reducing the negative side effects of cancer chemotherapy, such as nephrotoxicity.
    Type: Grant
    Filed: May 22, 1995
    Date of Patent: June 2, 1998
    Assignee: Trega Biosciences, Inc.
    Inventors: Beverly E. Girten, Richard A. Houghten, Costas C. Loullis, Mark J. Suto, Ronald R. Tuttle