Patents by Inventor Leroy B. Townsend

Leroy B. Townsend 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).

  • Patent number: 5874413
    Abstract: The present invention relates to polysubstituted benzimidazoles, having the following formula: ##STR1## wherein Q is a substituted benzimidazole group attached at the benzimidazole 1-position; R is a halogen of atomic number 9 to 53, inclusive (i.e., --F, --Cl, --Br, or --I); azido (i.e., --N.sub.3); or --X--R.sub.1, wherein X is a chalcogen of atomic number 8 to 16, inclusive (i.e., --O-- or --S--), and R.sub.1 may be straight or branched chain alkyl of 1 to 8 carbon atoms; and R.sub.2 and R.sub.3 may be the same or different and are separately --O--C(.dbd.O)CH.sub.3 (i.e., --OAc) or hydroxy (i.e., --OH); and pharmaceutically acceptable salts and operative combinations thereof. Also provided by this invention are compositions comprising a polysubstituted benzimidazole as defined above and methods of use thereof.
    Type: Grant
    Filed: August 16, 1996
    Date of Patent: February 23, 1999
    Assignee: University of Michigan
    Inventors: Leroy B. Townsend, John C. Drach
  • Patent number: 5840743
    Abstract: This invention pertains to nucleoside analogs which have antiviral activity and improved metabolic stability. More specifically, this invention pertains to modified sugar benzimidazole nucleosides, as exemplified by compounds such as benzimidazole nucleosides possessing a fluorinated sugar-like moiety (for example, a 2'-fluoro-furanosyl moiety or a 3'-fluoro-furanosyl moiety), and may be represented by the following formula, ##STR1## wherein R.sup.1 is a fluorinated sugar-like moiety; and R.sup.2, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are benzimidazole substituents, such as --H, halogens (e.g., --F, --Cl, --Br, --I), --NO.sub.2, --NR.sub.2 (where R is independently --H or an alkyl group having 1-6 carbon atoms), --OR (where R is --H or an alkyl group having 1-6 carbon atoms), --SR (where R is --H or a hydrocarbyl of 1-10 carbon atoms), and --CF.sub.3. In one embodiment, R.sup.1 is 2'-fluoro-furanosyl or 3'-fluoro-furanosyl; R.sup.2 is --H, --F, --Cl, --Br, --I, or --NR.sub.
    Type: Grant
    Filed: January 22, 1997
    Date of Patent: November 24, 1998
    Assignees: The Regents of the University of Michigan, Glaxo Wellcome Inc.
    Inventors: Leroy B. Townsend, John C. Drach, George A. Freeman
  • Patent number: 5827833
    Abstract: Triciribine and analogs are effective antiviral agents.
    Type: Grant
    Filed: December 19, 1996
    Date of Patent: October 27, 1998
    Assignees: Regents of the University of Michigan, Wake Forest University
    Inventors: Leroy B. Townsend, John C. Drach, Louis S. Kucera
  • Patent number: 5712255
    Abstract: A method for treating a herpes viral infection comprising administering to the infected host a therapeutically effective amount of a compound, or a pharmaceutically acceptable salt or formulation thereof, selected from the group consisting of compounds having the following formula: ##STR1## wherein: R.sub.1 is H, R.sub.2 is Cl, R.sub.3 is Cl, R.sub.4 is H, R.sub.5 is Br and R.sub.6 is .beta.-D-ribofuranosyl (denoted compound 52 in the text);R.sub.1 is H, R.sub.2 is NO.sub.2, R.sub.3 is NO.sub.2, R.sub.4 is H, R.sub.5 is Cl and R.sub.6 is .beta.-D-ribofuranosyl (denoted compound 61 in the text);R.sub.1 is Cl, R.sub.2 is H, R.sub.3 is Cl, R.sub.4 is H, R.sub.5 is Cl and R.sub.6 is .beta.-D-ribofuranosyl (denoted compound 81 in the text);R.sub.1 is H, R.sub.2 is Cl, R.sub.3 is Cl, R.sub.4 is H, R.sub.5 is I and R.sub.6 is .beta.-D-ribofuranosyl (denoted compound 83a in the text);R.sub.1 is Br, R.sub.2 is Br, R.sub.3 is H, R.sub.4 is H, R.sub.5 is Cl and R.sub.6 is .beta.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: January 27, 1998
    Assignee: The Regents of the University of Michigan
    Inventors: Leroy B. Townsend, John C. Drach
  • Patent number: 5705490
    Abstract: This invention relates to novel polysubstituted benzimidazoles and compositions and their use in the treatment of viral infections. The polysubstituted benzimidazoles and compositions of the present invention exhibit antiviral properties against viruses of the herpes family, particularly human cytomegalovirus (HCMV) and herpes simplex viruses (HSV).
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: January 6, 1998
    Assignee: The Regents of the University of Michigan
    Inventors: Leroy B. Townsend, John C. Drach
  • Patent number: 5665709
    Abstract: Polysubstituted benzimidazole nucleosides, pharmaceutical compositions thereof, and their use in the treatment of herpes viral infections.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: September 9, 1997
    Assignee: The Regents of the University of Michigan
    Inventors: Leroy B. Townsend, John C. Drach
  • Patent number: 5654283
    Abstract: This invention relates to novel polysubstituted benzimidazoles and compositions and their use in the treatment of viral infections. The polysubstituted benzimidazoles and compositions of the present invention exhibit antiviral properties against viruses of the herpes family, particularly human cytomegalovirus (HCMV) and herpes simplex viruses (HSV).
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: August 5, 1997
    Assignee: The Regents of the University of Michigan
    Inventors: Leroy B. Townsend, John C. Drach
  • Patent number: 5646125
    Abstract: This invention relates to novel polysubstituted benzimidazoles and compositions and their use in the treatment of viral infections. The polysubstituted benzimidazoles and compositions of the present invention exhibit antiviral properties against viruses of the herpes family, particularly human cytomegalovirus (HCMV) and herpes simplex viruses (HSV).
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: July 8, 1997
    Assignee: The Regents of the University of Michigan
    Inventors: Leroy B. Townsend, John C. Drach
  • Patent number: 5633235
    Abstract: Triciribine and analogs are effective antiviral agents.
    Type: Grant
    Filed: July 5, 1994
    Date of Patent: May 27, 1997
    Assignees: Regents of the University of Michigan, Wake Forest University
    Inventors: Leroy B. Townsend, John C. Drach, Louis S. Kucera
  • Patent number: 5574058
    Abstract: Polysubstituted benzimidazoles and pharmaceutical compositions containing them as the active ingredients. These compounds and compositions exhibit antiviral activity against viruse of the herpes family, particularly human cytomegalovirus and herpes simplex viruses (HSV).
    Type: Grant
    Filed: May 3, 1993
    Date of Patent: November 12, 1996
    Assignee: The Regents of the University of Michigan
    Inventors: Leroy B. Townsend, John C. Drach
  • Patent number: 5543413
    Abstract: This invention relates to a novel class of 4,5,6,7-substituted non-nucleoside, non-phosphorylatable pyrrolo[2,3-d]pyrimidines which exhibit both significantly lower levels of cytotoxicity and superior antiviral activity than known nucleoside, non-nucleoside, and non-nucleoside, non-phosphorylatable pyrrolo[2,3-d]pyrimidine derivatives, particularly against human DNA viruses such as cytomegalovirus (HCMV) and herpes simplex virus type 1 (HSV-1). These compounds are represented by the following formula: ##STR1## wherein R.sup.4 is -NH.sub.2 or -NHCH.sub.3 ;R.sup.5 is -CN,-CSNH.sub.2, or -CSeNH.sub.2 ;R.sup.6 is -H or -NH.sub.2 ; andR.sup.7 is selected from the group consisting ofaryls and aralkyls having 6 to 30 carbon atoms;aliphatic oxy-hydrocarbyls having 2 to 15 carbon atoms, lacking free hydroxyl groups and further lacking acyl or acyl derivatized groups; andoxy-hydrocarbyls having 6 to 30 carbon atoms, at least one aryl or aralkyl group, and only one oxy-group;with the proviso that if R.sup.
    Type: Grant
    Filed: December 15, 1994
    Date of Patent: August 6, 1996
    Assignee: Regents of the University of Michigan
    Inventors: Leroy B. Townsend, John C. Drach, Thomas E. Renau
  • Patent number: 5534535
    Abstract: Antiviral nucleoside analogues contain a substituted benzimidazole base attached to a carbocyclic ring in place of the conventional sugar residue. Particularly preferred compounds include those in which the 2-, 5- and 6- positions of the benzimidazole base are substituted by halogen. The compounds have activity against herpes virus especially cytomegalovirus and also hepatitis B virus infections.
    Type: Grant
    Filed: September 9, 1994
    Date of Patent: July 9, 1996
    Assignees: Burroughs Wellcome Co., The Regents of the University of Michigan
    Inventors: Leroy B. Townsend, John C. Drach, Steven S. Good, Susan M. Daluge, Michael T. Martin
  • Patent number: 5360795
    Abstract: This invention relates to novel polysubstituted benzimidazoles and compositions and their use in the treatment of viral infections. The polysubstituted benzimidazoles and compositions of the present invention exhibit antiviral properties against viruses of the herpes family, particularly human cytomegalovirus (HCMV) and herpes simplex viruses (HSV). Preferred polysubstituted benzimidazoles of the invention are 2,5,6-Trichloro-1-(.beta.-D-5-deoxyribofuranosyl)benzimidazole and 2-bromo-5,6-dichloro-1-(5-deoxy-.beta.-D-ribofuranosyl)benzimidazole.
    Type: Grant
    Filed: October 21, 1992
    Date of Patent: November 1, 1994
    Assignee: The Regents of the University of Michigan
    Inventors: Leroy B. Townsend, John C. Drach
  • Patent number: 5278181
    Abstract: Soluble alkyl [5-(amino (phenyl)methyl)-2H-benzimidazol-2-yl]carbamates, their enantiomorphic forms, and acid addition salts thereof are well absorbed and possess curative anthelmintic activity, especially against filarial worms, when administered orally or parenterally. Pharmaceutical compositions containing the compounds and methods of employing the compounds in methods of treating helminth infections in mammals are also disclosed, together with methods of synthesis.
    Type: Grant
    Filed: May 12, 1992
    Date of Patent: January 11, 1994
    Assignee: Board of Regents Acting on Behalf of the University of Michigan
    Inventors: Leroy B. Townsend, Dean S. Wise, Siya Ram
  • Patent number: 5248672
    Abstract: This invention relates to novel polysubstituted benzimidazole nucleosides and compositions and their use in the treatment of viral infections, particulary those caused by human cytomegalovirus and herpes simplex virus. Such substituted compounds exhibit antiviral properties superior to their parent compounds and low leveSPONSORSHIPThis invention was made with government support under Contract No. NO1 Al 42554 and NO1 Al 72641 awarded by the National Institute of Allergy and Infectious Diseases of the National Institutes of Health. The government has certain rights in this invention.
    Type: Grant
    Filed: November 1, 1990
    Date of Patent: September 28, 1993
    Assignee: The Regents of the University of Michigan
    Inventors: Leroy B. Townsend, John C. Drach
  • Patent number: 4968686
    Abstract: This invention relates to the use of acyclic substituted pyrrolo[2,3-d]pyrimidine nucleoside analogs in the treatment of viral infections. Such substituted compounds retain antiviral properties present in their parent compounds, yet exhibit significantly decreased levels of cytotoxicity, thereby having therapeutic potential as antiviral agents.
    Type: Grant
    Filed: June 21, 1989
    Date of Patent: November 6, 1990
    Assignee: The Regents of The University of Michigan
    Inventors: Leroy B. Townsend, John G. Drach, Charles Shipman, Jr., Jeffrey S. Pudlo
  • Patent number: 4935505
    Abstract: Novel azolo [1,3] diazepine compounds of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are either H or OH and R.sup.1 and R.sup.2 are not the same and X is either CH or N. Such compounds are active as adenosine deaminase inhibitors.
    Type: Grant
    Filed: February 4, 1988
    Date of Patent: June 19, 1990
    Inventors: Leroy B. Townsend, Oscar L. Acevedo
  • Patent number: 4927830
    Type: Grant
    Filed: April 8, 1988
    Date of Patent: May 22, 1990
    Assignee: The Regents of the University of Michigan
    Inventors: Leroy B. Townsend, John C. Drach
  • Patent number: 4892865
    Abstract: This invention relates to the use of certain substituted pyrrolo[2,3-d]-pyrimidine nucleosides in the treatment of viral infections, in particular those caused by human immunodeficiency virus type 1, herpes simplex virus type 1 and human cytomegalovirus. These substituted compounds retain antiviral properties present in their parent compounds yet exhibit significantly decreased levels of cytotoxicity.
    Type: Grant
    Filed: December 1, 1987
    Date of Patent: January 9, 1990
    Assignee: The Regents of the University of Michigan
    Inventors: Leroy B. Townsend, John C. Drach, Steven H. Krawczyk
  • Patent number: 4140851
    Abstract: Certain trisubstituted pyrrolopyrimidine nucleosides are prepared from toyocamycin and have shown antitumor activity against L1210 and P388 murine leukemia. The particular compounds of interest are selected from the following structural formula: ##STR1## where X is haloY is halo; --NH.sub.2 ; --SH, --SR (where R is lower alkyl, benzyl); --OR (where OR is methoxy or alkoxy or where alk is C1-C6); amino (where the amino is --NH.sub.2, -alkyl amino or -dialkyl amino and alkyl is C1-C6); gamma gamma dimethyl allyl amino; benzyl amino; phenyl amino; selenoZ is CN; CXNH.sub.2 where X is .dbd.0, .dbd.S, or .dbd.Se, .dbd.NH, .dbd.NHNH.sub.2, .dbd.NOH. OR Z is = --CH.sub.2 NH.sub.2, --COR.dbd.NHRib.dbd..beta.-D-ribofuranosylPreferred members of this group of compounds are shown by the following structural formula: ##STR2## where X is ClY is Cl or NH.sub.2Z is CN, CONH.sub.2, or C.dbd.NOH--NH.sub.
    Type: Grant
    Filed: November 21, 1977
    Date of Patent: February 20, 1979
    Assignee: The United States of America as represented by the Department of Health, Education and Welfare
    Inventor: Leroy B. Townsend