Patents Represented by Attorney Tom M. Moran
  • Patent number: 5198226
    Abstract: A long acting sustained release pharmaceutical composition for dihydropyridine calcium channel blockers wherein the calcium channel blocker and a pH-dependent binder are intimately admixed in essentially spherically shaped non-rugose particles of up to 1.2 mm in diameter.
    Type: Grant
    Filed: November 12, 1991
    Date of Patent: March 30, 1993
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Calum B. MacFarlane, Alastair B. Selkirk, Michael J. Dey
  • Patent number: 5192770
    Abstract: .alpha.-Oxoacetamides of the formula R.sup.1 C(O)C(O)NR.sup.2 R.sup.3 in which R.sup.1 is optionally substituted phenyl, 1-indolyl, 2,3-dihydro-1-indolyl, 1-benzimidazolidinonyl, 3-benzofuranyl, 3-benzothiophenyl, 3-indolyl, and 1,2-alkano-3-indolyl; R.sup.2 is selected from: ##STR1## and R.sup.3 is selected from hydrogen or lower alkyl; and the pharmaceutically acceptable salts, individual isomers, mixtures of isomers, processes for preparation, compositions, and methods of use thereof.
    Type: Grant
    Filed: December 7, 1990
    Date of Patent: March 9, 1993
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Robin D. Clark, Richard M. Eglen, Joseph M. Muchowski, William L. Smith, Klaus K. Weinhardt
  • Patent number: 5189041
    Abstract: 5-HT.sub.3 receptor antagonist compounds of the formula ##STR1## in which Z is --O--, --S-- or --N(R.sup.2)--; R.sup.1 and R.sup.2 are independently selected from hydrogen and lower alkyl or are together --(CH.sub.2).sub.n -- wherein n is 2 to 4; and R.sup.3 is selected from ##STR2## and the pharmaceutically acceptable salts, individual isomers, compositions, and methods of use thereof.
    Type: Grant
    Filed: November 16, 1990
    Date of Patent: February 23, 1993
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Jacob Berger, Robin D. Clark
  • Patent number: 5177072
    Abstract: Heterocyclic aminoalkyl esters of mycophenolic acid, and the derivatives and pharmaceutically acceptable salts thereof, are useful as immunosuppressive agents, anti-inflammatory agents, anti-tumor agents, anti-viral agents, and anti-psoriatic agents.
    Type: Grant
    Filed: December 9, 1991
    Date of Patent: January 5, 1993
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Peter H. Nelson, Chee-Liang L. Gu, Anthony C. Allison, Elsie M. Eugui, William A. Lee
  • Patent number: 5164405
    Abstract: There is disclosed a stable pharmaceutical composition containing nicardipine hydrochloride, a non-chloride isotonicity agent, a buffering agent and a pharmaceutically acceptable aqueous vehicle for parenteral administration.
    Type: Grant
    Filed: October 22, 1990
    Date of Patent: November 17, 1992
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Calum B. McFarlane, Alistair B. Selkirk, Michael J. Dey
  • Patent number: 5158936
    Abstract: Thiol protease inhibitors are disclosed having the formula: ##STR1## or an optical isomer thereof, or a pharmaceutically acceptable salt thereof, wherein:n is 0 or 1;m is 0, 1 or 2;X is H or an N-protecting group;each Y is independently an optionally protected .alpha.-amino acid residue;R is an optionally protected .alpha.-amino acid side chain that is H or CH.sub.3 or that is bonded to the .alpha.-carbon atom to which it is attached by a methylene, methine or phenyl radial; andR' is optionally substituted aryl.
    Type: Grant
    Filed: May 15, 1991
    Date of Patent: October 27, 1992
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Alexander Krantz, Heinz W. Pauls, Roger A. Smith, Robin W. Spencer
  • Patent number: 5158949
    Abstract: Compounds of formula (I): ##STR1## wherein n is 2 or 3;p is 0, 1 or 2;q is 0, 1 or 2;X is oxygen or S(O).sub.t where t is 0, 1 or 2;each R.sup.1 is independently halo, lower alkyl, lower alkoxy, or trifluoromethyl;each R.sup.2 is independently halo or lower alkyl;R.sup.3 is nitro or --N(R.sup.5)R.sup.6 whereR.sup.5 is hydrogen or lower alkyl;R.sup.6 is hydrogen lower alkyl, lower alkylsulfonyl or --C(Y)R.sup.7 where Y is oxygen or sulfur and R.sup.7 is hydrogen, lower alkyl, lower alkoxy or --N(R.sup.8)R.sup.9 where R.sup.8 is hydrogen or lower alkyl and R.sup.9 is hydrogen, lower alkyl or lower alkoxycarbonyl; orR.sup.5 and R.sup.6 together with N is pyrrolidino, piperidino, morpholino, thiomorpholino or piperazino, wherein the piperazino is optionally substituted at the 4-position by --N(O)R.sup.10 where R.sup.10 is hydrogen, lower alkyl, lower alkoxy or amino; andR.sup.
    Type: Grant
    Filed: December 20, 1990
    Date of Patent: October 27, 1992
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Keith A. Walker, Pamela M. Burton, David C. Swinney
  • Patent number: 5155132
    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; and R.sup.6 and R.sup.7 are independently hydrogen, lower alkyl, cycloalkyl or optionally substituted phenyl.The compounds of this invention are also useful for the treatment of disease-states caused by lipoxygenase activity in mammals, particularly 5-lipoxygenase activity, when administered systemically.
    Type: Grant
    Filed: March 21, 1988
    Date of Patent: October 13, 1992
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Michael C. Venuti, John M. Young
  • Patent number: 5152995
    Abstract: Acid-sensitive antibiotic esters for oral administration to livestock are stabilized by incorporation in premix formulations comprising a carrier, a base, a protective coating, and optionally a sealant film.
    Type: Grant
    Filed: October 12, 1989
    Date of Patent: October 6, 1992
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Richard A. Runkel, Stephen A. Berry, Mahmood M. Ghani
  • Patent number: 5142052
    Abstract: Aryl- and heterocyclic-methanamines are prepared by reacting a hydroxy-aryl carbinol or a heterocyclic carbinol with a primary or a secondary amine in the presence of a cationic effect reagent.
    Type: Grant
    Filed: October 21, 1988
    Date of Patent: August 25, 1992
    Assignee: Laboratoires Syntex
    Inventors: Serge Beranger, Bruno Francois
  • Patent number: 5135944
    Abstract: Compounds of Formula I ##STR1## in which: R.sub.1 is hydrogen, lower alkyl, --C(O)R.sub.3, or --C(O)NR.sub.3 R.sub.4, where R.sub.3 and R.sub.4 are independently lower alkyl, phenyl, or phenyl lower alkyl;R.sub.2 is hydrogen or lower alkyl; andX is --(CH.sub.2).sub.m -- where m is an integer of 1 to 10, or --(CH.sub.2).sub.n Y(CH.sub.2).sub.n -- where n is an integer of 1 to 3 and Y is oxygen or sulfur,their individual R,R-; R,S-; and S,S-stereoisomers, and racemic or non-racemic mixtures of stereoisomers, and their pharmaceutically acceptable salts are dopamine agonist compounds useful in the treatment of hypertension and congestive heart failure in mammals.
    Type: Grant
    Filed: December 3, 1991
    Date of Patent: August 4, 1992
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Lawrence E. Fisher, Joseph M. Muchowski, Edvige Galeazzi, Roberto P. Rosenkranz, Deborah L. McClelland
  • Patent number: 5134161
    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;both X groups are the same and X 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: April 15, 1988
    Date of Patent: July 28, 1992
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Michael C. Venuti, John M. Young
  • Patent number: 5130432
    Abstract: A process for preparing a cyclic amine of Formula I ##STR1## in which R.sup.1 is phenyl, optionally substituted by 1 to 3 lower alkoxy groups;R.sup.2, R.sup.3 and R.sup.4 are independently hydrogen or lower alkyl; andn is 1 or 2,comprises(1) converting an aminoalcohol of Formula III ##STR2## to a dioxooxathiazolidine of Formula II ##STR3## in which R.sup.2, R.sup.3, R.sup.4 and n are as defined above; and (2) reacting the dioxooxathiazolidine of Formula II with an organometallic nucleophile, R.sup.1 M*, wherein R.sup.1 is as defined above, and hydrolyzing the resulting sulfamate salt.
    Type: Grant
    Filed: December 21, 1990
    Date of Patent: July 14, 1992
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Gary F. Cooper, Michael G. Martin
  • Patent number: 5116817
    Abstract: The present invention relates to a novel nasal composition comprising a nona- or decapeptide having LHRH agonist or antagonist activity and a surfactant which is a bile acid or a pharmaceutically acceptable salt thereof in a buffered aqueous solution.
    Type: Grant
    Filed: September 20, 1990
    Date of Patent: May 26, 1992
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Shabbir T. Anik
  • Patent number: 5108999
    Abstract: This invention is directed to compounds of the formula (I): ##STR1## wherein R.sup.1 is --OR.sup.4 (where R.sup.4 is hydrogen, lower alkyl, lower hydroxyalkyl, phenyl, phenyl-lower-alkyl, or --(CH.sub.2).sub.n Y where n is an integer from 1 to 4 and Y is morpholino, --SR.sup.5, --C(O)OR.sup.5, --C(O)N(R.sup.6).sub.2, --N(R.sup.6).sub.2, or --N.sup.+ (R.sup.6).sub.3 X.sup.-, in which R.sup.5 is lower alkyl, each R.sup.6 is independently selected from hydrogen or lower alkyl, and X is halogen)or --SR.sup.7 (where R.sup.7 is lower alkyl, phenyl-lower-alkyl, or --(CH.sub.2).sub.n W where W is --N(R.sup.6).sub.2 or --N.sup.+ (R.sup.6).sub.3 X.sup.-, and n, R.sup.6 and X are as previously defined);R.sup.2 is lower alkyl, phenyl or phenyl-lower-alkyl;R.sup.3 is halo, hydroxy, lower alkyl, lower alkoxy, lower haloalkyl, lower haloalkoxy, or --C(O)OR.sup.5 where R.sup.5 is as previously defined; andZ is a bond, 2,5-thienyl or 2,5-furanyl; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 19, 1990
    Date of Patent: April 28, 1992
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: John W. Patterson, Bruce H. Devens
  • Patent number: 5091428
    Abstract: Substituted imidazolyl-alkyl-piperazine and diazepine derivatives of Formula A: ##STR1## wherein: R.sup.1 is aryl, lower alkyl, cycloalkyl or hydrogen;R.sup.2 is aryl, lower alkyl or hydrogen;R.sup.3 is lower alkyl, hydroxy, or hydrogen;R.sup.4 is aryl or hydrogen;R.sup.5 is aryl or hydrogen;m is two or three;n is zero, one or two, provided that when R.sup.3 is hydroxy, n is one or two; andq is zero, one, two, or three;and the pharmaceutically acceptable salts thereof, are calcium channel antagonists useful for treating mammals having a variety of disease states, such as stroke, epilepsy, hypertension, angina, migraine, arrhythmia, thrombosis, embolism and also for treatment of spinal injuries.
    Type: Grant
    Filed: February 7, 1991
    Date of Patent: February 25, 1992
    Assignee: Syntex Pharmaceuticals, Ltd.
    Inventors: Jean C. Pascal, Chi-Ho Lee, Brian J. Alps, Henri Pinhas, Roger L. Whiting
  • Patent number: 5091182
    Abstract: A dispensing unit for a ketorolac topical gel formulation is disclosed, wherein the dispensing unit comprises a ketorolac topical gel formulation and a gas-impermeable multi-layered container wherein the container is comprised of a polyolefin inner layer and a metal foil outer layer.
    Type: Grant
    Filed: July 23, 1990
    Date of Patent: February 25, 1992
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: John T. H. Ong, Jean S. Fujiki, Wei-Cheng Liaw
  • Patent number: 5091558
    Abstract: Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 is alkoxy, alkylthio, optionally substituted phenoxy or optionally substituted phenylthio;R.sup.2 is hydrogen, lower alkyl, optionally substituted phenyl or optionally substituted phenylalkyl;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(0).sub.
    Type: Grant
    Filed: March 6, 1987
    Date of Patent: February 25, 1992
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Gordon H. Jones, Michael C. Venuti, John M. Young
  • Patent number: 5089657
    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 phenyl-lower-alkyl;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 selected from the group consisting of hydrogen, R.sup.4 and -C(O)W, whereinW is alkyl of one to seven carbon atoms, optionally substituted phenyl or optionally substituted benzyl; andR.sup.4 is lower alkyl or optionally substituted phenyl-lower-alkyl.
    Type: Grant
    Filed: March 11, 1987
    Date of Patent: February 18, 1992
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Michael C. Venuti
  • Patent number: 5082847
    Abstract: Carbostyril derivatives of Formula I: ##STR1## wherein: m is 0, 1, or 2;n is 0, 1, or 2;R.sup.1 is hydrogen or lower alkyl;R.sup.2 is hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy, aralkoxy, or acyloxy;R.sup.3 is hydrogen, halogen, lower alkyl, or lower alkoxy;R.sup.4 is hydrogen, hydroxy, lower alkyl, acyloxy, provided that when R.sup.4 is hydroxy or acyloxy, m and n are both 1;R.sup.5 is hydrogen or lower alkyl; andR.sup.6 is alkyl, hydroxyalkyl, alkoxyalkyl, or (dialkylamino)alkyl;and the pharmaceutically acceptable acid addition salts and N-oxides (at the carbostyril nitrogen) thereof, and compositions containing them, are useful in treating cardiovascular diseases, particularly arrhythmias. Methods of preparing intermediates, the compounds, their formulations and methods of treatment therewith are also disclosed.
    Type: Grant
    Filed: July 18, 1990
    Date of Patent: January 21, 1992
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Jean-Claude Pascal, Leslie Patmore, Jurg Pfister, Dominique Blondet, John M. Armstrong