Patents by Inventor William F. Huffman

William F. Huffman 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).

  • Polypeptide intermediates
    Patent number: 4658015
    Abstract: Certain vasopressin-like peptides, which have an acyclic unit at position 1 and which have an .omega.-amino- or guanidinoalkyl substituent attached to the cysteine in the 6-position of the ring, have V.sub.1 -vasopressin and oxytocin antagonist activity. A species of this series of new compounds is [1-desaminopenicillamine-2-(O-ethyl-D-tyrosine)-8-(1,4-diaminobutane)-9-de sglycinamide]-vasopressin.
    Type: Grant
    Filed: April 16, 1986
    Date of Patent: April 14, 1987
    Assignee: SmithKline Beckman Corporation
    Inventors: James F. Callahan, William F. Huffman, Michael L. Moore, Nelson C. Yim
  • Basic V.sub.1 -vasopressin antagonists
    Patent number: 4604378
    Abstract: Certain vasopressin-like peptides, which have an acyclic unit at position 1 and which have an .omega.-amino- or guanidinoalkyl substituent attached to the cysteine in the 6-position of the ring, have V.sub.1 -vasopressin and oxytocin antagonist activity. A species of this series of new compounds is [1-desaminopenicillamine-2-(O-ethyl-D-tyrosine)-8-(1,4-diaminobutane)-9-de sglycinamide]-vasopressin.
    Type: Grant
    Filed: November 21, 1984
    Date of Patent: August 5, 1986
    Assignee: SmithKline Beckman Corporation
    Inventors: James F. Callahan, William F. Huffman, Michael L. Moore, Nelson C. Yim
  • V1-vasopressin antagonists
    Patent number: 4599324
    Abstract: Vasopressin derivatives having V.sub.1 and oxytocin antagonist activity whose structures are characterized by a Mpa unit at position 1 and a des-Pro unit at position 7 are prepared by standard peptide synthetic methods also using an oxidative cyclization of a dimercaptan. Representative species are [1-deaminopenicillamine-2-(O-methyl)-tyrosine-7-desproline-8-arginine-9-de sglycine]vasopressin or [1-.beta.-mercaptopropionic acid-2-D-(O-ethyl)tyrosine-3-isoleucine-4-threonine-7-desproline-8-arginin e-9-desglycine]-vasopressin.
    Type: Grant
    Filed: November 21, 1984
    Date of Patent: July 8, 1986
    Assignee: SmithKline Beckman Corporation
    Inventors: Fadia E. Ali, William F. Huffman
  • Intermediates for preparing octapeptide vasopressin antagonists
    Patent number: 4587045
    Abstract: Certain octapeptides, which have structures characterized by being a six unit cyclic peptide ring with a dipeptide tail which lacks a glycine unit at position 9, have potent vasopressin antagonist activity. The compounds here claimed are in general characterized by having an amino acid unit at position 4 which is other than valine. An important species of the group is [1-(.beta.-mercapto-.beta.,.beta.-cyclopentamethylenepropionic acid)-2-(O-ethyl-D-tyrosine)-4-.alpha.-aminobutyric acid-8-arginine-9-desglycine]vasopressin.
    Type: Grant
    Filed: May 16, 1985
    Date of Patent: May 6, 1986
    Assignee: SmithKline Beckman Corporation
    Inventors: William F. Huffman, Michael L. Moore
  • Octapeptide vasopressin antagonists
    Patent number: 4542124
    Abstract: Certain octapeptides, which have structures characterized by being a six unit cyclic peptide ring with a dipeptide tail which lacks a glycine unit at position 9, have potent vasopressin antagonist activity. The compounds here claimed are in general characterized by having an amino acid unit at position 4 which is other than valine. An important species of the group is [1-(.beta.-mercapto-.beta.,.beta.-cyclopentamethylenepropionic acid)-2-(O-ethyl-D-tyrosine)-4-.alpha.-aminobutyric acid-8-arginine-9-desglycine]vasopressin.
    Type: Grant
    Filed: June 26, 1984
    Date of Patent: September 17, 1985
    Assignee: Smithkline Beckman Corporation
    Inventors: William F. Huffman, Michael L. Moore
  • Des-proline vasopressin antagonists
    Patent number: 4481193
    Abstract: Certain octapeptides, which have structures characterized by being a six unit cyclic peptide ring with a dipeptide tail with no proline unit, have vasopressin antagonist activity. An important species of the group is [1-(.beta.-mercapto-.beta.,.beta.-cyclopentamethylenepropionic acid)-2-(O-ethyl-D-tyrosine)-4-valine]-7-desproline-8-arginine-vasopressin .
    Type: Grant
    Filed: March 7, 1984
    Date of Patent: November 6, 1984
    Assignee: SmithKline Beckman Corporation
    Inventors: Fadia E. Ali, William F. Huffman
  • Des-proline-des-glycine vasopressin antagonists
    Patent number: 4481194
    Abstract: Certain heptapeptides which have structures characterized by being a six unit cyclic peptide ring with an arginine or lysine tail have vasopressin antagonist activity. An important species of the group is [1-(.beta.-mercapto-.beta.,.beta.-cyclopentamethylenepropionic acid)-2-(O-ethyl-D-tyrosine)-4-valine-7-desproline-8-arginine-9-desglycine ]-vasopressin.
    Type: Grant
    Filed: March 7, 1984
    Date of Patent: November 6, 1984
    Assignee: SmithKline Beckman Corporation
    Inventors: Fadia E. Ali, William F. Huffman
  • Iodinated vasopressin antagonists
    Patent number: 4469680
    Abstract: A series of vasopressin antagonists which have a 3'-iodo-tyrosine unit at position 2 are prepared by iodination of the tyrosine congeners. The compounds have antagonist activity manifested by an aquaretic effect and, also, are useful in studying various biological reactions.
    Type: Grant
    Filed: July 6, 1983
    Date of Patent: September 4, 1984
    Assignee: SmithKline Beckman Corporation
    Inventors: William F. Huffman, Michael L. Moore
  • Octapeptide vasopressin antagonists
    Patent number: 4469679
    Abstract: Certain octapeptides which have structures characterized by being a six unit cyclic peptide ring with a dipeptide tail have vasopressin antagonist activity. An important species of the group is [1-(.beta.-mercapto-.beta.,.beta.-cyclopentamethylenepropionic acid)-2-(O-ethyl-D-tyrosine)-4-valine-8-arginine-9-desglycine]vasopressin.
    Type: Grant
    Filed: February 16, 1983
    Date of Patent: September 4, 1984
    Assignee: SmithKline Beckman Corporation
    Inventors: William F. Huffman, Michael L. Moore
  • Pharmaceutical composition and methods for producing dopamine agonist activity
    Patent number: 4414224
    Abstract: Methods and compositions using as active ingredients 2-(3H)-indolones whose structures having an aminoalkyl substituent at position 4 and a hydroxy group at position 7 of the indolone nucleus are used to produce selective dopaminergic activity resulting in improved kidney function, relief of the symptoms of congestive heart failure, long lasting anti-hypertensive activity and anti-anginal activity. A species of the active ingredients is 4-di-n-propylaminoethyl-7-hydroxy-2(3H)-indolone or its salts.
    Type: Grant
    Filed: January 22, 1982
    Date of Patent: November 8, 1983
    Assignee: SmithKline Beckman Corporation
    Inventors: William F. Huffman, James W. Wilson
  • 4-Aminoalkyl-7-hydroxy-2(3H)-indolones
    Patent number: 4314944
    Abstract: A new group of 2(3H)-indolones whose structures are characterized by having an aminoalkyl substituent at position 4 and a hydroxy group at position 7 of the indolone nucleus have beneficial activity on the cardiovascular system. A typical species of the group is 4-di-n-propylaminoethyl-7-hydroxy-2(3H)-indolone and its acid addition salts.
    Type: Grant
    Filed: August 22, 1980
    Date of Patent: February 9, 1982
    Assignee: SmithKline Corporation
    Inventors: William F. Huffman, James W. Wilson
  • Method for preparing lower alkyl .beta.-(S-benzylmercapto)-.beta.,.beta.-pentamethylenepropionates
    Patent number: 4299969
    Abstract: Lower alkyl .beta.-(S-benzylmercapto)-.beta.,.beta.-pentamethylenepropionates are prepared in improved yields by reacting lower alkyl cyclohexylideneacetates with benzylmercaptan in the presence of an alkali metal mercaptide.
    Type: Grant
    Filed: August 8, 1980
    Date of Patent: November 10, 1981
    Assignee: SmithKline Corporation
    Inventors: William F. Huffman, Nelson C. Yim
  • 3-Amino-2-hydroxy, halo or mercaptomethyl-4-oxoazetidines
    Patent number: 4257947
    Abstract: The stereospecific cycloaddition of nitrogen containing acetic acid halides or anhydrides with Schiff bases having a carbalkoxy group substituted on the methine carbon atom offers new intermediates and methods for preparing synthetic cephalosporin congeners having antibacterial activity.
    Type: Grant
    Filed: March 14, 1979
    Date of Patent: March 24, 1981
    Assignee: SmithKline Corporation
    Inventors: John G. Gleason, Kenneth G. Holden, William F. Huffman
  • Substituted azetidinones
    Patent number: 4200572
    Abstract: Substituted azetidine intermediates for preparing novel bicyclic .beta.-lactam penicillin analogs which have antibacterial activity are disclosed.
    Type: Grant
    Filed: May 1, 1978
    Date of Patent: April 29, 1980
    Assignee: SmithKline Corporation
    Inventors: John G. Gleason, Kenneth G. Holden, William F. Huffman
  • Methods and intermediates for preparing cis-4-oxoazetidine intermediates
    Patent number: 4166816
    Abstract: The stereospecific cycloaddition of nitrogen containing acetic acid halides or anhydrides with Schiff bases having a carbalkoxy group substituted on the methine carbon atom offers new intermediates and methods for preparing synthetic cephalosporin congeners having antibacterial activity.
    Type: Grant
    Filed: August 3, 1977
    Date of Patent: September 4, 1979
    Assignee: SmithKline Corporation
    Inventors: John G. Gleason, Kenneth G. Holden, William F. Huffman
  • Monocyclic beta-lactams with antibacterial activity
    Patent number: 4144333
    Abstract: A monocyclic .beta.-lactam containing a cis-.beta.-acylamino moiety as in the penicillin and cephalosporin antibacterials is disclosed. These compounds have antibacterial activity against a variety of Gram-positive and Gram-negative organisms. Intermediates useful for the preparation of these antibacterials are also disclosed.
    Type: Grant
    Filed: November 15, 1976
    Date of Patent: March 13, 1979
    Assignee: SmithKline Corporation
    Inventors: Ralph F. Hall, William F. Huffman
  • 8-Oxo-4-thia-1-azabicyclo (4.2.0)-oct-2-ene derivatives
    Patent number: 4103086
    Abstract: Novel bicyclic .beta.-lactams and intermediates useful in their preparation are disclosed. In particular, 7.beta.-acyl-amino- and 7.beta.-amino-8-oxo-4-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acids are prepared. The acylated compounds are antibacterial agents.
    Type: Grant
    Filed: June 8, 1976
    Date of Patent: July 25, 1978
    Assignee: SmithKline Corporation
    Inventors: John G. Gleason, Kenneth G. Holden, William F. Huffman
  • Cis-4-oxoazetidine intermediates and methods of preparing them
    Patent number: 4072674
    Abstract: The stereospecific cycloaddition of nitrogen containing acetic acid halides or anhydrides with Schiff bases having a carbalkoxy group substituted on the methine carbon atom offers new intermediates and methods for preparing synthetic cephalosporin congeners having antibacterial activity.
    Type: Grant
    Filed: June 14, 1976
    Date of Patent: February 7, 1978
    Assignee: SmithKline Corporation
    Inventors: John G. Gleason, Kenneth G. Holden, William F. Huffman
  • 3-Substituted-6.beta.-(amino- and acylamino)-7-oxo-1,3-diazabicyclo[3.2.0]- h
    Patent number: 4000154
    Abstract: Novel bicyclic .beta.-lactam penicillin analogs which have antibacterial activity and intermediates for the synthesis thereof are disclosed. In particular, 3-acetyl-7-oxo-6.beta.-phenoxyacetylamino-1,3-diazabicyclo[3.2.0]heptane-2 -carboxylic acid and derivatives thereof are prepared.
    Type: Grant
    Filed: September 3, 1975
    Date of Patent: December 28, 1976
    Assignee: SmithKline Corporation
    Inventors: John G. Gleason, Kenneth G. Holden, William F. Huffman