Patents Represented by Attorney Tom M. Moran
  • Patent number: 4670465
    Abstract: Long chain unsaturated hydrocarbon derivatives, having from 13 to 21 carbon atoms, which are substituted at the 1-position by a phenoxy, phenylthio or a phenyl that bear a carboxylic acid group at the ortho, meta or para positions, and up to 4 carbon-carbon triple bonds, methods of preparing them, and pharmaceutical preparations containing them. These compounds are useful as lipoxygenase inhibitors, and therefore as antiinflammatory agents.
    Type: Grant
    Filed: May 21, 1986
    Date of Patent: June 2, 1987
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Angel Guzman, Joseph M. Muchowski
  • Patent number: 4670434
    Abstract: This invention relates to compounds of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein the various substituents are defined herein. These compounds are cyclic AMP phosphodiesterase inhibitors useful as antithrombotic and inotropic agents in mammals.
    Type: Grant
    Filed: November 14, 1985
    Date of Patent: June 2, 1987
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Michael C. Venuti
  • Patent number: 4668703
    Abstract: This invention is for .gamma.-allenyl-.gamma.-aminobutyric acid derivatives which are .gamma.-aminobutyric acid transaminase inhibitors.
    Type: Grant
    Filed: July 1, 1985
    Date of Patent: May 26, 1987
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Alexander Krantz, Arlindo L. Castelhano, Diana H. Pliura
  • Patent number: 4667014
    Abstract: Synthetic nonpeptide and decapeptide LHRH antagonist analogs have a novel guanido-substituted, amidine, tertiary or quaternary amine water-soluble aminoacyl residue at position 6.
    Type: Grant
    Filed: May 20, 1983
    Date of Patent: May 19, 1987
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: John J. Nestor, Jr., Brian H. Vickery
  • Patent number: 4667038
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 and each independently --H or lower alkoxy; R.sub.3 and R.sub.4 are each independently lower alkyl; and R.sub.5 and R.sub.6 are each --OCH.sub.3, or together form --OCH.sub.2 O-- or --OCH.sub.2 CH.sub.2 O--, and pharmaceutically acceptable acid addition salts thereof are prepared by cyclizing, deoxygenating, coupling, or hydrogenating the intermediates disclosed herein.
    Type: Grant
    Filed: September 22, 1986
    Date of Patent: May 19, 1987
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Robin Clark, Joseph M. Muchowski, Fang-Ting Chiu, John O. Gardner, Jacob Berger
  • 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: 4659693
    Abstract: Peptides which promote the release of growth hormone by the pituitary gland or which inhibit the release of growth hormone by growth hormone releasing factor and which have an N,N'-dialkyl substituted guanidino amino acyl residue at position 1 or 2 are disclosed herein.
    Type: Grant
    Filed: February 28, 1985
    Date of Patent: April 21, 1987
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: John J. Nestor
  • 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: 4647580
    Abstract: A treatment for senile dementia of the Alzheimer's type comprising administering to the patient a tertiary amine of the formula ##STR1## wherein R.sup.1 is alkyl, alkoxy, alkylthio or dialkylamino hydroxyl, hydrogen, chlorine or fluorine;R.sup.2 is hydrogen, or when R.sup.1 is hydrogen, alkyl, alkoxy, alkylthio, alkylthioamino, hydroxyl, chlorine or fluorine;R.sup.3 is 1 to 2 carbon alkyl;R.sup.4 is 1 to 3 carbon alkyl;R.sup.5 is an optionally branched 3 to 12 carbon alkylene; X is oxygen or ethylene dioxy; andR.sup.6 is optionally branched or cyclic carbon group having less than eight carbons. The preferred compound is secoverine.The administration of secoverine may be used in conjunction with the coadministration of a cholinergic enhancer, for example, in a combination with acetylcholinesterase inhibitors, muscarinic agonists or choline supplement therapy.
    Type: Grant
    Filed: July 18, 1985
    Date of Patent: March 3, 1987
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Adolph P. Roszkowski
  • Patent number: 4642378
    Abstract: Intraocular hypertensive diseases such as glaucoma are treated with compounds represented by formula I ##STR1## or a pharmaceutically acceptable acid addition salt thereof, wherein R.sub.1 is alkyl of two to four carbon atoms;R.sub.2 is --(CH.sub.2).sub.n --C.sub.6 H.sub.4 --R.sub.5 ; wheren is an integer from 1 to 4; andR.sub.5 is --H, --OH, halo, lower alkyl, lower alkoxy, ureido, lower alkyl-ureido, lower alkyl-amido, or formamido;R.sub.3 is hydro or hydroxy; andR.sub.4 is hydro, lower alkyl, amino, or lower alkylamino.
    Type: Grant
    Filed: April 11, 1985
    Date of Patent: February 10, 1987
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Robin D. Clark, L. David Waterbury
  • Patent number: 4642346
    Abstract: Novel anhydrous crystalline 9-(1,3-dihydroxy-2-propoxymethyl)guanine useful as an antiviral agent.
    Type: Grant
    Filed: June 24, 1985
    Date of Patent: February 10, 1987
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Tai W. Chan, Huong T. Nguyen
  • Patent number: 4629730
    Abstract: Elevated intraocular pressure diseases such as glaucoma are treated with compounds represented by formula I ##STR1## or a pharmaceutically acceptable acid addition salt thereof, wherein R.sub.1 is alkyl of two to four carbon atoms; andR.sub.2 is alkyl of three or four carbon atoms; orR.sub.1 and R.sub.2 taken together with N form ##STR2## wherein n is 0, 1, or 2 and R.sub.5 and R.sub.6 are each independently lower alkyl or hydro;R.sub.3 is hydro or hydroxy;R.sub.4 is hydro, lower alkyl, amino, or lower alkylamino.
    Type: Grant
    Filed: April 11, 1985
    Date of Patent: December 16, 1986
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Robin D. Clark, L. David Waterbury
  • Patent number: 4629782
    Abstract: Crystalline N-acetylmuramyl-L-.alpha.-aminobutyryl-D-isoglutamine monohydrate useful as an adjuvant for vaccines and as an immunostimulant.
    Type: Grant
    Filed: December 21, 1984
    Date of Patent: December 16, 1986
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Tai W. Chan, Allyn R. Becker
  • Patent number: 4621140
    Abstract: Process and novel intermediates for preparing 9-(1,3-dihydroxy-2-propoxymethyl)guanine and 2,6-diamino-9-(1,3-dihydroxy-2-propoxymethyl)purine and certain esters thereof. The present process and intermediates reduce the number of reaction steps to prepare these compounds as compared to prior processes. The products are useful as antiviral agents.
    Type: Grant
    Filed: February 23, 1984
    Date of Patent: November 4, 1986
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Julien P. H. Verheyden, John C. Martin, Daniel P. C. McGee
  • Patent number: 4618696
    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; and X is hydrogen, halo, trifluoromethyl, lower alkyl or lower alkoxy; 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: July 31, 1984
    Date of Patent: October 21, 1986
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Gary F. Cooper, John A. Edwards, Albert R. Van Horn
  • Patent number: 4613606
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are each independently --H or lower alkoxy;R.sub.3 and R.sub.4 are each independently lower alkyl; andR.sub.5 and R.sub.6 are each --OCH.sub.3, or together form --OCH.sub.2 O-- or --OCH.sub.2 CH.sub.2 O--and pharmaceutically acceptable acid addition salts thereof are calcium channel blockers useful for treating cardiovascular disorders including angina, hypertension and congestive heart failure.
    Type: Grant
    Filed: December 2, 1985
    Date of Patent: September 23, 1986
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Robin Clark, Joseph M. Muchowski, Fang-Ting Chiu, John O. Gardner, Jacob Berger
  • Patent number: 4612314
    Abstract: Compounds useful as antiviral agents are defined by the following formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sup.1 and R.sup.2 are both --C(O)R.sup.7 wherein R.sup.7 is 1-adamantyl;R.sup.3 is amino;(a) R.sup.6 is hydrogen or amino and R.sup.4 together with R.sup.5 is a bond; or(b) R.sup.5 together with R.sup.6 is a keto group and R.sup.4 is hydrogen.
    Type: Grant
    Filed: June 13, 1985
    Date of Patent: September 16, 1986
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Julien P. H. Verheyden, John C. Martin