Patents by Inventor Wayne C. Guida

Wayne C. Guida 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).

  • 5?,-substituted adenosynes preparation thereof and use as inhibitors of S-adenosylmethionine decarboxylase
    Patent number: 8637485
    Abstract: The crystal structure of the complex of S-adenosylmethionine methyl ester with h?doMetDC F223A, a mutant where the stacking of the aromatic rings of F7, adenine and F223 would be eliminated. The structure of this mutant with the ester shows that the ligand still maintains a syn conformation aided by pi-pi interactions to F7, hydrogen bonds to the backbone of Glu67, and electrostatic interactions. Several series of AdoMet substrate analogues with a variety of substituents at the 8 position of adenine were synthesized and analyzed for their ability to inhibit hAdoMetDC. To understand these results, virtual modeling of the enzyme inhibitor complexes and the crystal structures of human AdoMetDC with 5?-deoxy-5?-[N-methyl-N-[2-(aminooxy)ethyl]amino-8-methyl]adenosine (MAOEMA) and 5?-deoxy-5?-[N-methyl-N-[4-(aminooxy)butyl]amino-8-ethyl]adenosine (MAOBEA) at the active site have been determined experimentally.
    Type: Grant
    Filed: August 1, 2008
    Date of Patent: January 28, 2014
    Assignees: Southern Research Institute, Cornell University, H. Lee Moffitt Cancer and Research Institute, The Penn State Research Foundation
    Inventors: John A. Secrist, III, Steven Ealick, Shridhar Bale, Anthony E. Pegg, Diane E. McCloskey, Wayne C. Guida
  • 5',-SUBSTITUTED ADENOSYNES PREPARATION THEREOF AND USE AS INHIBITORS OF S-ADENOSYLMETHIONINE DECARBOXYLASE
    Publication number: 20110009354
    Abstract: The crystal structure of the complex of S-adenosylmethionine methyl ester with h?doMetDC F223A, a mutant where the stacking of the aromatic rings of F7, adenine and F223 would be eliminated. The structure of this mutant with the ester shows that the ligand still maintains a syn conformation aided by pi-pi interactions to F7, hydrogen bonds to the backbone of Glu67, and electrostatic interactions. Several series of AdoMet substrate analogues with a variety of substituents at the 8 position of adenine were synthesized and analyzed for their ability to inhibit hAdoMetDC. To understand these results, virtual modeling of the enzyme inhibitor complexes and the crystal structures of human AdoMetDC with 5?-deoxy-5?-[N-methyl-N-[2-(aminooxy)ethyl]amino-8-methyl]adenosine (MAOEMA) and 5?-deoxy-5?-[N-methyl-N-[4-(aminooxy)butyl]amino-8-ethyl]adenosine (MAOBEA) at the active site have been determined experimentally.
    Type: Application
    Filed: August 1, 2008
    Publication date: January 13, 2011
    Inventors: John A. Secrist, III, Steve Ealick, Shridhar Bale, Anthony E. Pegg, Diane E. McCloskey, Wayne C. Guida
  • 7-disubstituted-methyl-4-oxo-3H,5H-pyrrolo?3,2-d!pyrimidine and pharmaceutical uses and compositions containing the same
    Patent number: 5726311
    Abstract: Disclosed is a compound of the formula ##STR1## wherein R.sup.1 is H, NH.sub.2, or OCH.sub.3, R.sup.2 is an optionally substituted cyclic group optionally containing one or more heteroatoms, R.sup.3 and R.sup.4 are independently H or C.sub.1-4 alkyl, m is 0-4, n is 0-6, p is 0.1, X is CN, CSNH.sub.2, PO(OH).sub.2, COOH, SO.sub.2 NH.sub.2, NH.sub.2, OH, CNHNH.sub.2, tetrazole, triazole, or COR.sup.5 where R.sup.5 is C.sub.1-4 alkyl, CF.sub.3, NH.sub.2, or OC.sub.1-4 alkyl, and Y is O or NH that is useful as a pharmaceutical.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: March 10, 1998
    Assignee: BioCryst Pharmaceuticals, Inc.
    Inventors: Shri Niwas, John A. Secrist, III, John A. Montgomery, Mark David Erion, Wayne C. Guida, Steve E. Ealick
  • 7-disubstituted-methyl-4-oxo-3H,5H-pyrrolo[3,2d]pyrimidine and pharmaceutical uses and compositions containing the same
    Patent number: 5189039
    Abstract: Disclosed is a compound of the formula ##STR1## wherein R.sup.1 is H, NH.sub.2, or OCH.sub.3, R.sup.2 is an optionally substituted cyclic group optionally containing one or more heteroatoms, R.sup.3 and R.sup.4 are independently H or C.sub.1-4 alkyl, m is 0-4, n is 0-6, p is 0.1, X is CN, CSNH.sub.2, PO(OH).sub.2, COOH, SO.sub.2 NH.sub.2, NH.sub.2, OH, CNHNH.sub.2, tetrazole, triazole, or COR.sup.5 where R.sup.5 is C.sub.1-4 alkyl, CF.sub.3, NH.sub.2, or OC.sub.1-4 alkyl, and Y is O or NH that is useful as a pharmaceutical.
    Type: Grant
    Filed: May 14, 1991
    Date of Patent: February 23, 1993
    Assignee: BioCryst, Inc.
    Inventors: Shri Niwas, John A. Secrist, III, John A. Montgomery, Mark D. Erion, Wayne C. Guida, Steve E. Ealick
  • 2-amino-7-(alicyclomethyl)-3H,5H,-pyrrolo[3,2-d]pyrimidin-4-ones and pharmaceutical uses and compositions containing the same
    Patent number: 5008265
    Abstract: Disclosed is a compound containing a 2-amino-7-(substituted methyl)-3H,5H-pyrrolo[3,2-d]pyrimidin-4-one wherein substituted methyl is --CH.sub.2 --R wherein R is an optionally substituted alicyclic group, a pharmaceutical composition containing the compound, and a method for the selective suppression of mammalian T-cell function without diminished effect on humoral immunity which involves administering the composition to a mammal.
    Type: Grant
    Filed: October 31, 1989
    Date of Patent: April 16, 1991
    Assignee: BioCryst, Inc.
    Inventors: John A. Secrist, III, John A. Montgomery, Steve E. Ealick, Mark D. Erion, Wayne C. Guida
  • 2-amino-7-(heterocyclomethyl)-3H,5H-pyrrolo[3,2-d]pyrimidin-4-ones and pharmaceutical uses and compositions containing the same
    Patent number: 5008270
    Abstract: Disclosed is a compound containing a 2-amino-7-(substituted methyl)-3H,5H-pyrrolo[3,2-d]pyrimidin-4-one wherein substituted methyl is --CH.sub.2 --R wherein R is an optionally substituted heteroalicyclic group, a pharmaceutical composition containing the compound, and a method for the selective suppression of mammalian T-cell function without diminished effect on humoral immunity which involves administering the composition to a mammal.
    Type: Grant
    Filed: October 31, 1989
    Date of Patent: April 16, 1991
    Assignee: BioCryst, Inc.
    Inventors: John A. Secrist, III, John A. Montgomery, Steve E. Ealick, Mark D. Erion, Wayne C. Guida
  • 2-amino-7-(pyridinylmethyl)-3H,5H-pyrrolo[3,2-d]pyrimidin-4-ones and pharmaceutical uses and compositions containing the same
    Patent number: 4985433
    Abstract: Disclosed is a compound containing a 2-amino-7-(substituted methyl)-3H,5H-pyrrolo[3,2-d]pyrimidin-4-one wherein substituted methyl is --CH.sub.2 --R wherein R is optionally substituted pyridinyl, a pharmaceutical composition containing the compound, and a method for the selective suppression of mammalian T-cell function without diminished effect on humoral immunity which involves administering the composition to a mammal.
    Type: Grant
    Filed: October 31, 1989
    Date of Patent: January 15, 1991
    Assignee: BioCryst, Inc.
    Inventors: John A. Secrist, III, John A. Montgomery, Steve E. Ealick, Mark D. Erion, Wayne C. Guida
  • 7-substituted derivatives of 2-amino-3H,5H-pyrrolo(3,2-d)pyrimidin-4-ones and pharamceutical uses and compositions containing the same
    Patent number: 4985434
    Abstract: Disclosed is a compound containing 2-amino-7-(R)-3H,5H-pyrrolo[3,2-d]pyrimidin-4-one wherein R is optionally substituted cyclohexenyl or cyclohexyl, a pharmaceutical composition containing the compound, and a method for the selective suppresion of mammalian T-cell function without diminished effect on humoral immunity which involves administering the composition to a mammal.
    Type: Grant
    Filed: October 31, 1989
    Date of Patent: January 15, 1991
    Assignee: Biocryst, Inc.
    Inventors: John A. Secrist, III, John A. Montgomery, Steve E. Ealick, Mark D. Erion, Wayne C. Guida