Patents Represented by Attorney Grant D. Green
  • Patent number: 4593029
    Abstract: Novel compound of the formula ##STR1## wherein n is an integer of 1 to 8;R.sub.1 is hydrogen or alkyl of 1-6 carbons;R.sub.2 is hydrogen;R.sub.3 is hydrogen, alkyl of 1-6 carbons, phenyl, benzyl, hydroxy lower alkyl, carbamoyl alkyl, carboxyalkyl, alkoxycarbonylalkyl;R.sub.4 is hydrogen, alkyl of 1-6 carbons, benzyl, or hydroxy lower alkyl;Y is hydrogen, alkyl of 1 to 4 carbon atoms, halo or lower alkoxy;any of its optical isomers, the mixture thereof, or the pharmaceutically acceptable acid addition salt.These compounds are inhibitors of thromboxane synthetase and cyclic AMP phosphodiesterase and are therefore potential cardiovascular agents particularly useful as platelet aggregation inhibitors and anti-thrombotic agents. Accordingly, these compounds will preferably be useful in treating cardiovascular disorders with thrombotic complications. However, they also possess vasodilatory, antisecretory, antihypertensive, inotropic and antimetastatic activities.
    Type: Grant
    Filed: February 15, 1984
    Date of Patent: June 3, 1986
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Michael C. Venuti, John J. Bruno
  • Patent number: 4558129
    Abstract: Novel compounds of the general formula: ##STR1## and the pharmaceutically acceptable esters and acid addition salts thereof, 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 R.sup.9 are each independently hydrogen, lower alkyl, lower alkoxy, trifluoromethyl, halo, lower alkylthio, lower alkyl sulfinyl, lower alkyl sulfonyl; orR.sup.2 and R.sup.3 together form --OCH.sub.2 O--; andR.sup.10 and R.sup.11 are each independently hydrogen or lower alkyl.These compounds combine .beta.-blockade and calcium entry blockade properties in the same compound and therefore are useful in therapy in the treatment of cardiovascular diseases, including hypertension, arrhythmias and variant and exercise induced angina.
    Type: Grant
    Filed: May 18, 1983
    Date of Patent: December 10, 1985
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Arthur F. Kluge, Robin D. Clark, Arthur M. Strosberg
  • Patent number: 4552898
    Abstract: Compounds useful in treating cardiovascular disorders are the carboxylic acids depicted in formulas (1) and (2) ##STR1## as well as their pharmaceutically acceptable, non-toxic salts and esters, wherein:n is an integer from one to four;R.sub.1 is hydroxy;R.sub.2 is hydrogen; orR.sub.1 and R.sub.2 together are an oxo group;R.sub.3 is ##STR2## wherein A is --CH.sub.2 --CH.sub.2 --; trans--CH.dbd.CH--; --C.tbd.C--; andR.sub.4 is linear or branched alkyl of one to twelve carbons, preferably 1-10 carbons, most preferably 3-8 carbons, cycloalkyl of three to eight carbons; phenyl optionally substituted with one or two identical substituents selected from the group consisting of lower alkyl, lower alkoxy, hydroxy, trifluoromethyl, and halo; or phenylloweralkyl optionally substituted with one or two identical substituents selected from the group consisting of lower alkyl, lower alkoxy, hydroxy, trifluoromethyl, and halo.
    Type: Grant
    Filed: August 19, 1983
    Date of Patent: November 12, 1985
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Tsung-Tee Li, Michael Marx
  • Patent number: 4542027
    Abstract: A compound represented by the formula ##STR1## wherein R.sup.1 is an alkali metal cation or hydrogen and which useful for increasing the feed efficiency of ruminants and for treating coccidiosis in domestic animals, especially chickens.
    Type: Grant
    Filed: February 23, 1984
    Date of Patent: September 17, 1985
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Robin D. Clark
  • Patent number: 4522811
    Abstract: Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides.
    Type: Grant
    Filed: July 8, 1982
    Date of Patent: June 11, 1985
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Deborah A. Eppstein, Elizabeth B. Fraser-Smith, Thomas R. Matthews
  • Patent number: 4499100
    Abstract: Novel compounds of the general formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein: R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each independently hydrogen, lower alkyl, lower alkoxy, trifluoromethyl, halo, lower alkylthio, lower alkyl sulfinyl or lower alkyl sulfonyl;R.sup.5 is hydrogen or lower alkyl;m is 0 or 1;W is alkylene, --CH.dbd.CH--, --O--, or --N(R.sup.6)--, where R.sup.6 is lower alkyl or hydrogen;n is 0 or 1; andQ is lower alkyl, cycloalkyl or optionally substituted phenyl.These compounds combine .beta.-blockade and calcium entry blockade properties in the same compound and therefore are useful in therapy in the treatment of cardiovascular diseases, including myocardial infarction, hypertension, arrhythmia and variant and exercise induced angina. The compounds are also useful in immunosuppressant therapy for immune diseases, such as rheumatoid arthritis.
    Type: Grant
    Filed: May 18, 1983
    Date of Patent: February 12, 1985
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Arthur F. Kluge, Robin D. Clark