Patents Represented by Attorney Tom M. Moran
  • Patent number: 4803271
    Abstract: Compounds useful as antiviral agents are defined by the following formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof whereinR.sup.1 is hydrogen or --C(O)R.sup.7 wherein R.sup.7 is hydrogen, alkyl of one to nineteen carbon atoms, hydroxyalkyl of one to eight carbon atoms, alkoxyalkyl of two to nine carbon atoms, alkenyl of two to nineteen carbon atoms, phenyl, 1-adamantyl or 2-carboxyethyl and the pharmaceutically acceptable alkali metal salts thereof;R.sup.2 is --C(O)R.sup.7 is as defined above;R.sup.3 is hydrogen, halo, thio, lower alkylthio of one to six carbon atoms, azido, NR.sup.9 R.sup.10 wherein R.sup.9 and R.sup.10 are independently hydrogen or lower alkyl of one to six carbon atoms or --NHC(O)R.sup.8 wherein R.sup.8 is hydrogen, alkyl of one to nineteen carbon atoms or 1-adamantyl; and(a) R.sup.6 is hydrogen, halo, lower alkoxy of one to six carbon atoms, azido, thio, lower alkylthio of one to six carbon atoms, --NR.sup.9 R.sup.10 and R.sup.9 and R.sup.
    Type: Grant
    Filed: June 8, 1987
    Date of Patent: February 7, 1989
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Julien P. H. Verheyden, John C. Martin
  • Patent number: 4803079
    Abstract: A controlled release tablet for once-daily oral administration of about 500-1200 mg of naproxen or naproxen sodium, said tablet comprising a homogeneous matrix comprising about 4-9 weight percent of hydroxypropyl methylcellulose having a number average molecular weight in the range of from about 80,000 to about 130,000, about 81-96 weight percent naproxen or naproxen sodium, and 0.1 to about 2 weight percent of a pharmaceutically acceptable lubricating agent, and optionally including a pharmaceutically acceptable coating.
    Type: Grant
    Filed: December 20, 1985
    Date of Patent: February 7, 1989
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Charles H. Hsiao, John S. Kent
  • Patent number: 4803269
    Abstract: 4-Monosubstituted and 4,6-disubstituted phenoxazines, methods of preparing them and pharmaceutical compositions containing them. These compounds are useful as anti-inflammatories.
    Type: Grant
    Filed: August 14, 1987
    Date of Patent: February 7, 1989
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Joseph M. Muchowski, Robert J. Greenhouse, Angel Guzman
  • Patent number: 4801577
    Abstract: Synthetic nona- and decapeptide LHRH antagonist analogs are disclosed, having a sterically hindered guanidino-substituted arginyl or homoarginyl residue at position 8, with no arginyl substituent at position 6.
    Type: Grant
    Filed: February 5, 1987
    Date of Patent: January 31, 1989
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: John J. Nestor, Jr., Brian H. Vickery
  • Patent number: 4792551
    Abstract: Compounds useful for treating inflammation, pain and swelling, represented by the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein: Y and Z are each independently halo, alkyl or alkoxy;l and m are each independently integers of 0-4;b is an integer of 2-12; andX is selected from the group consisting of:--NR.sup.1 R.sup.2, --NR.sup.1 (CH.sub.2 CH.sub.2 OH), ##STR2## in which R.sup.1 and R.sup.2 are independently H, alkyl or cycloalkyl;R.sup.3 is H, alkyl or CH.sub.2 CH.sub.2 OH; andn is an integer of 3-7.
    Type: Grant
    Filed: July 15, 1983
    Date of Patent: December 20, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Peter H. Nelson, Stefan H. Unger, Thomas R. Thieme
  • Patent number: 4792570
    Abstract: Compounds useful for treating inflammation, swelling and associated pain, represented by the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein: a is an integer of 0-3;b is an integer of 0-2;n is an integer of 3-12;each X and each Y are independently -halo, --R.sup.1, -alkoxy, or -phenyl; andB is selected from the group consisting of:--NR.sup.1 R.sup.2, --NR.sup.1 (CH.sub.2 CH.sub.2 OH), ##STR2## in which R.sup.1 and R.sup.2 are independently H, alkyl or cycloalkyl;R.sup.3 is H, alkyl or --CH.sub.2 CH.sub.2 OH; andm is an integer of 3-8.Novel compounds are those wherein n is at least 6 if both a and b are 0.
    Type: Grant
    Filed: April 6, 1984
    Date of Patent: December 20, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Peter H. Nelson, James P. Dunn, Stefan H. Unger, Thomas R. Thieme
  • Patent number: 4792561
    Abstract: The invention concerns a method of inhibiting both thromboxane synthetase and cyclic-AMP phosphodiesterase in a mammal having a disease characterized by elevated thromboxane levels or an imbalance of prostacyclin/thromboxane levels with a compound of the formula: ##STR1## or a pharmaceutically acceptable acid addition salt or ester thereof, wherein:X is chosen from the group consisting of: ##STR2## and a covalent bond in which R.sup.1 is H, alkyl having 1-6 carbon atoms, optionally substituted phenyl or optionally substituted phenyl lower alkyl, when R.sup.2 is H or OH, or R.sup.1 and R.sup.2 taken together represent oxo, alkylidene having 1-6 carbon atoms or optionally substituted benzylidene;R.sup.3 is H or alkyl having 1-6 carbon atoms, R.sup.4 is H and R.sup.3 and R.sup.4 are either cis or trans to each other, or R.sup.3 and R.sup.4 taken together represent a covalent bond;n is an integer from 0-3;Het is 1-imidazolyl or 3-pyridyl; and the dotted line represents an optional covalent bond.
    Type: Grant
    Filed: May 29, 1986
    Date of Patent: December 20, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Keith A. M. Walker, John J. Bruno, Gregory R. Martinez
  • Patent number: 4792556
    Abstract: Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are the same and are lower alkoxy or optionally substituted phenoxy,R.sup.3 is lower alkyl, lower alkoxy, or halo and m is 0, 1 or 2 or R.sup.3 is optionally substituted phenyl, optionally substituted phenyl lower alkyl, optionally substituted phenyl lower alkoxy, amino, lower alkylamino, lower dialkylamino, cyano, or S(O).sub.n R wherein R is lower alkyl; optionally substituted phenyl; optionally substituted phenyl lower alkyl; or optionally substituted heterocyclic aryl of three to nine ring atoms containing one or two heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, and the pharmaceutically acceptable acid addition salts thereof; and m is 1 and n is 0, 1 or 2;at least one of X or Y is C(O)W and the other X or Y is different and is hydrogen, C(O)W or R.sup.
    Type: Grant
    Filed: April 28, 1986
    Date of Patent: December 20, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: D. V. K. Murthy, Michael C. Venuti, John M. Young
  • Patent number: 4792617
    Abstract: This invention covers a compound of the formula ##STR1## wherein R is hydrogen, lower alkyl or a pharmaceutically acceptable, non-toxic salt of a compound wherein R is hydrogen; X is hydrogen, halo, trifluoromethyl, lower alkyl or lower alkoxy, Y is lower alkyl or ##STR2## wherein Z is hydrogen, halo, methyl, methoxy or trifluoromethyl; and the wavy lines represent the .alpha. or .beta. configuration with the proviso that when one wavy line is .alpha. the other is .beta..
    Type: Grant
    Filed: February 27, 1987
    Date of Patent: December 20, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Gary F. Cooper, John H. Fried, L. David Waterbury
  • Patent number: 4791108
    Abstract: Compounds of formulas (1) and (2): ##STR1## in which: X and Y are independently hydrogen, hydroxy, lower alkyl, lower alkoxy or halo, or X and Y taken together is methylenendioxy or ethylene-1,2-dioxy, andR is lower alkyl, optionally substituted phenyl, --(CH.sub.2).sub.m OR.sup.1 or --NR.sup.1 R.sup.2 wherein m is an integer of 1 to 6 and R.sup.1 and R.sup.2 are independently hydrogen or lower alkyl, or --NR.sup.1 R.sup.2 taken together is a heterocycle of the formula: ##STR2## wherein A is --CH.sub.2 --, --NR.sup.1 -- or oxygen, or a pharmaceutically acceptable salt thereof, are useful as .alpha..sub.2 -blockers, especially as antidepressants.
    Type: Grant
    Filed: April 13, 1987
    Date of Patent: December 13, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Robin D. Clark
  • Patent number: 4786637
    Abstract: The compounds and pharmaceutical compositions of Formula A, wherein Z is hydrogen or --C(O)R, Y is hydrogen or morpholinoethyl, and where R is lower alkyl or aryl, and the pharmaceutically acceptable salts thereof, are useful as immunosuppressive agents, particularly for treatment of allograft rejection, especially including cardiac allograft rejection, pancreatic allograft rejection and renal allograft rejection, and for treating autoimmune diabetes.
    Type: Grant
    Filed: January 22, 1988
    Date of Patent: November 22, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Anthony C. Allison, Elsie M. Eugui, Peter H. Nelson, Chee-Liang L. Gu, William A. Lee
  • Patent number: 4786652
    Abstract: Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 is lower alkoxy or optionally substituted phenoxy,R.sup.2 is the same as R.sup.1, or R.sup.2 is hydrogen, lower alkyl, optionally substituted phenyl or optionally substituted phenylalkyl,R.sup.3 is hydrogen, lower alkyl, lower alkoxy, halo, optionally substituted phenyl, optionally substituted phenyl-lower-alkyl or optionally substituted phenyl-lower-alkoxy, and m is 1 or 2;X is the same and is either --C(O)OR.sup.4 or --C(O)NR.sup.5 R.sup.6,whereinR.sup.4 is alkyl, phenyl or benzyl optionally substituted with one or two lower alkyl groups, lower alkoxy groups or halo; andR.sup.5 and R.sup.6 are independently hydrogen, lower alkyl, cycloalkyl or phenyl optionally substituted with one or two lower alkyl groups, lower alkoxy groups or halo.
    Type: Grant
    Filed: March 9, 1987
    Date of Patent: November 22, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Michael C. Venuti
  • Patent number: 4782047
    Abstract: A non-stinging aqueous anti-inflammatory steroid formulation suitable for intranasal administration comprises: an anti-inflammatory steroid in an amount between about 0.01% and about 0.05% (w/v); propylene glycol in an amount between about 2% and about 10% (w/v); PEG 400 in an amount between about 10% and about 25% (w/v); polysorbate 20 in an amount between about 1% and about 4% (w/v); an effective amount of a preservative; an effective amount of a stabilizer; an effective amount of an antioxidant; water; and pH buffering agent sufficient to adjust the pH of the resulting solution to between about 3.5 and about 7.
    Type: Grant
    Filed: May 22, 1986
    Date of Patent: November 1, 1988
    Assignee: Syntex Pharmaceuticals International Ltd.
    Inventors: Eric Benjamin, Shabbir Anik, Ya-Yun T. Lin
  • Patent number: 4780480
    Abstract: Novel aroyl-substituted benzofuran and benzothiophene acetic and proprionic acids are disclosed herein. These compounds are useful as analgesic, anti-inflammatory, and antipyretic agents.
    Type: Grant
    Filed: April 20, 1987
    Date of Patent: October 25, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: James P. Dunn
  • Patent number: 4772466
    Abstract: A vaccine contains an immunologically effective amount of an antigen, a polyoxypropylene-polyoxyethylene block polymer, a glycol ether-based surfactant, an immunopotentiating amount of an immunostimulating glycopeptide, and, optionally, a metabolizable non-toxic oil.
    Type: Grant
    Filed: February 21, 1985
    Date of Patent: September 20, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Anthony C. Allison, Noelene E. Byars
  • Patent number: 4770874
    Abstract: An adjuvant composition contains an immunopotentiating amount of an immunostimulating glycopeptide, a polyoxypropylene-polyoxyethylene block polymer, a glycol ether-based surfactant, and, optionally, a metabolizable non-toxic oil.
    Type: Grant
    Filed: May 5, 1986
    Date of Patent: September 13, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Anthony C. Allison, Noelene E. Byars
  • Patent number: 4761420
    Abstract: Compound of formula 1 are calcium entry antagonists useful for treating hypertension, congestive heart failure, angina, and vasospastic disorders: ##STR1## wherein n is an integer from 1 to 4;R.sub.1 and R.sub.2 are lower alkyl;R.sub.3 is lower alkyl or alkoxyalkyl;A is alkylene of two to eight carbon atoms;X.sub.1 and X.sub.2 are each independently --NO.sub.2, --CF.sub.3, CH.sub.3 O--, --CN, --H, lower alkyl or halo;Y is --O--, --S--, --S(O)--, or --S(O).sub.2 --; andR is H, lower alkyl, cycloalkyl, alkoxyalkyl, cycloalkyloxy-alkyl, alkoxycycloalkyl, acyl, or saturated or unsaturated 5- or 6-membered heterocyclyl optionally substituted with lower alkyl or alkoxy, wherein the heteroatom is one oxygen atom.
    Type: Grant
    Filed: June 13, 1986
    Date of Patent: August 2, 1988
    Assignee: Laboratoires Syntex S.A.
    Inventor: Gilles Genain
  • Patent number: 4761416
    Abstract: Pharmaceutical compositions comprising, or compositions consisting essentially of, compounds according to the formula ##STR1## or an optical isomer thereof are disclosed, wherein the substituents A, Z and R.sup.1 are defined herein. The invention is also directed to certain compounds of the above class. The compounds of Formula I are cyclic AMP phosphodiesterase inhibitors useful as antithrombotic and inotropic agents and the like in mammals.
    Type: Grant
    Filed: July 25, 1986
    Date of Patent: August 2, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: John H. Fried, Michael C. Venuti
  • Patent number: 4758587
    Abstract: Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 is lower alkoxy or optionally substituted phenoxy;R.sup.2 is hydrogen, lower alkyl, optionally substituted phenyl or optionally substituted phenylalkyl;R.sup.3 is hydrogen, lower alkyl, lower alkoxy, halo, optionally substituted phenyl, optionally substituted phenyl-lower-alkyl or optionally substituted phenyl-lower-alkoxy, and m is 1 or 2;X and Y are different and are either R.sup.4 or --C(O)W whereinR.sup.4 is lower alkyl or optionally substituted phenyl-lower-alkyl;W is --OR.sup.5 or --NR.sup.6 R.sup.7,whereinR.sup.5 is alkyl, optionally substituted phenyl or optionally substituted benzyl; andR.sup.6 and R.sup.7 are independently hydrogen, lower alkyl, cycloalkyl or optionally substituted phenyl.
    Type: Grant
    Filed: March 9, 1987
    Date of Patent: July 19, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Michael C. Venuti
  • Patent number: 4755531
    Abstract: Thiol esters of 4,5-allenyl prostaglandins, methods of making them, and pharmaceutical compositions containing them. These compounds are useful as gastric acid secretion inhibitors.
    Type: Grant
    Filed: August 11, 1986
    Date of Patent: July 5, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Joseph M. Muchowski, Angel Guzman