Patents Represented by Attorney Liza K. Toth
  • Patent number: 4665070
    Abstract: 2-Oxy-4H-3,1-benzoxazin-4-ones represented by the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein: a is an integer of 0-4;A is a bond, or alkylene having one to eight carbon atoms;R is hydrogen, phenyl, imidazolyl or cycloalkyl having three to six carbon atoms, wherein the phenyl, imidazolyl or cycloalkyl ring is optionally substituted with 1-3 substituents independently selected from the group consisting of lower alkyl having one to four carbon atoms, lower alkoxy having one to four carbon atoms, --N(R.sup.1).sub.2, --NO.sub.2, halo or lower alkylthio having one to four carbon atoms, and,each R' is independently selected from the group consisting of lower alkyl having one to six atoms, lower alkenyl having two to six carbon atoms, lower alkoxy having one to six carbon atoms,lower alkylthio or halo-lower alkyl having one to four carbon atoms, halo, --NO.sub.2, --N(R.sup.1).sub.2, ##STR2## --NR.sup.1 COR.sup.2, and ##STR3## in which each R.sup.
    Type: Grant
    Filed: June 25, 1985
    Date of Patent: May 12, 1987
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Alexander Krantz, Robin Spencer, Tim Tam, Teng J. Liak
  • Patent number: 4663320
    Abstract: Compounds according to the formula ##STR1## an optical isomer thereof, or a pharmaceutically acceptable acid addition salt thereof wherein:n is an integer of 1 to 6;R.sub.1 is hydrogen or alkyl of 1 to 4 carbons;R.sub.2 is hydrogen or R.sub.1 and R.sub.2 are combined to form an oxo group;R.sub.3 is hydrogen, alkyl of 1 to 6 carbons, phenyl, benzyl, hydroxy lower alkyl or an aliphatic acylate thereof of 1 to 6 carbon atoms or an aryl acylate thereof of 7 to 12 carbon atoms, carbamoyl alkyl, carboxyalkyl, alkoxycarbonylalkyl of an .alpha.-amino acid side chain;R.sub.4 is hydrogen, alkyl of 1 to 6 carbons, benzyl, or hydroxy lower alkyl;Y is hydrogen, alkyl of 1 to 4 carbon atoms, halo or lower alkoxy;A is NR.sub.5 R.sub.6 wherein R.sub.5 and R.sub.
    Type: Grant
    Filed: June 11, 1985
    Date of Patent: May 5, 1987
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Gordon H. Jones, Michael C. Venuti, Robert Alvarez, John J. Bruno, Jurg R. Pfister
  • Patent number: 4661510
    Abstract: Novel .alpha.-allenic-.alpha.-amino acids which are enzyme inhibitors of the suicide or k.sub.cat type are disclosed herein.
    Type: Grant
    Filed: October 21, 1985
    Date of Patent: April 28, 1987
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Alexander Krantz, Arlindo L. Castelhano
  • Patent number: 4657893
    Abstract: Novel 2-amino-4H-3,1-benzoxazin-4-ones represented by the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and X are defined herein are useful as enzyme inhibitors in animals.
    Type: Grant
    Filed: November 26, 1984
    Date of Patent: April 14, 1987
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Alexander Krantz, Robin Spencer, Tim Tam
  • Patent number: 4654360
    Abstract: Disclosed are compounds of the formula ##STR1## wherein the several groups are defined herein. These compounds are useful for treating inflammation.
    Type: Grant
    Filed: June 1, 1984
    Date of Patent: March 31, 1987
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Robert J. Greenhouse, Joseph M. Muchowski
  • Patent number: 4602006
    Abstract: Compounds of the formula ##STR1## wherein n is 1-3; R.sup.1, R.sup.2 and R.sup.3 are the same or different and are hydrogen, lower alkyl, lower alkenyl, lower alkynyl, aryl or aryl lower alkyl wherein when aryl is phenyl it is unsubstituted or independently substituted with one or more halo, lower alkyl or lower alkoxy groups; and R.sup.4 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, trialkylsilyl, aryl or aryl lower alkyl wherein when aryl is phenyl it is unsubstituted or independently substituted by one or more halo, lower alkyl or lower alkoxy groups; excluding those compounds wherein R.sup.1 and R.sup.2 are hydrogen and R.sup.4 is ethyl, propyl or butyl. These compounds are useful as protease inhibitors.
    Type: Grant
    Filed: May 9, 1984
    Date of Patent: July 22, 1986
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Alexander Krantz, Tim F. Tam, Robin W. Spencer