Patents Represented by Attorney, Agent or Law Firm Wayne W. Montgomery
  • Patent number: 8206695
    Abstract: Effective enhancement of eyelash length and density can be obtained by topical applications of an active agent selected from a class of compounds consisting of synthetic prostaglandin agonists, polymers thereof and mixtures thereof preferably having the chemical formula of C24H35NO5, such as 7-[3.5-dihydroxy-2-(3-hydroxy-4phenoxy-but-1-enyl)-cyclopentyl]-hept-5-enoic acid ethylamide. Such active agents having a molecular weight of 417.54 can be employed in concentrations from 0.00075% to 0.03% by weight in mixtures with inactive ingredients, such as gels, oils, etc. Results are obtained by daily topical applications of active agent in such liquid mixtures (tinctures) at the roots of the lashes and/or lash follicles.
    Type: Grant
    Filed: October 10, 2007
    Date of Patent: June 26, 2012
    Assignee: La Canada Ventures, Inc.
    Inventor: Suan Lin
  • Patent number: 6492362
    Abstract: The present invention relates to novel selective cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.
    Type: Grant
    Filed: September 15, 2000
    Date of Patent: December 10, 2002
    Assignee: Axys Pharmaceuticals, Inc.
    Inventors: Michael Graupe, John O. Link, John W. Patterson, Sheila Zipfel
  • Patent number: 6465503
    Abstract: The present invention provides novel compounds of Formula I: its prodrug forms, or pharmaceutically acceptable salts thereof. The compounds of this invention are inhibitors of uPA, and have utility as cancer treating agents.
    Type: Grant
    Filed: August 10, 2001
    Date of Patent: October 15, 2002
    Assignee: Axys Pharmaceuticals, Inc.
    Inventor: Richard Laurence Mackman
  • Patent number: 6150379
    Abstract: The present invention relates to novel biheterocyclic derivatives which are factor Xa inhibitors; the pharmaceutically acceptable salts and N-oxides thereof; their uses as therapeutic agents and the methods of their making.
    Type: Grant
    Filed: November 17, 1998
    Date of Patent: November 21, 2000
    Assignee: Axys Pharmaceuticals, Inc.
    Inventors: Paul R. Fatheree, Thomas E. Jenkins, Martin S. Linsell, Sean G. Trapp, Erik J. Verner, Wendy B. Young
  • Patent number: 6103879
    Abstract: Antibodies and Bivalent molecules which activate erythropoietins and induce the proliferation or differentiation of erythroid progenitor cells are provided. Also provided are methods of using such bivalent molecules for drug discovery, diagnosis and treatment of disorders related to the activation of an erythropoietin receptor.
    Type: Grant
    Filed: June 16, 1997
    Date of Patent: August 15, 2000
    Assignee: Axys Pharmaceuticals, Inc.
    Inventors: Warak Lee Chaovapong, Lutz B. Giebel, Cyrus Karkaria, Michael J. Ross, Helmut H. Schneider, Kevin Shoemaker
  • Patent number: 5693515
    Abstract: Serine protease inhibitors are provided comprising compounds having a P site binding moiety and a divalent cation(s) chelating moiety which are pre-prepared as divalent cation(s) complexes or combined with the serine protease in the presence of divalent cation(s). The compounds are shown to have high inhibitory activity when complexed to divalent cation(s) and find use in various processes associated with serine protease isolation and inhibition.
    Type: Grant
    Filed: April 28, 1995
    Date of Patent: December 2, 1997
    Assignee: Arris Pharmaceutical Corporation
    Inventors: James M. Clark, Thomas E. Jenkins, Bradley A. Katz, Robert M. Stroud
  • Patent number: 5510486
    Abstract: This invention relates to a process for preparing 2-(1-azabicyclo 2.2.2!oct-3-yl)-2,3,3a,4,5,6-tetrahydro-1H-benz de!isoquin olin-1-one, particularly 2-(1-azabicyclo 2.2.2!oct-3S-yl)-2,3,3aS,4,5,6-tetrahydro-1H-benz de!isoqu inolin-1-one, and to intermediates useful in such process.
    Type: Grant
    Filed: July 26, 1994
    Date of Patent: April 23, 1996
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: James Robinson, III, John C. Rohloff, Bruce A. Kowalczyk
  • Patent number: 5492914
    Abstract: This invention relates to 2-(1'-azabicyclo[2.2.2]oct-3'S-yl)-6-hydroxy-2,4,5,6-tetrahydro-1H-benz[de ]isoquinolin-1-one and 2-(1'-azabicyclo[2.2.2]oct-3'S-yl)-6-hydroxy-2,3,3a,4,5,6-hexahydro-1H-ben z[de]isoquinolin-1-one and their individual stereoisomers and uses and the processes for their making.
    Type: Grant
    Filed: July 28, 1994
    Date of Patent: February 20, 1996
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Jacob Berger, Robin D. Clark, Paul E. Weller, Douglas L. Wren
  • Patent number: 5491148
    Abstract: 5-HT.sub.3 receptor antagonist compounds of Formula I: ##STR1## in which X and Y are independently selected from hydrogen, halogen, hydroxy, lower alkoxy, lower alkyl, nitro, amino, aminocarbonyl, (lower alkyl)amino, di(lower alkyl)amino and (lower alkanoyl)amino;R.sup.1 is hydrogen, lower alkyl, phenyl or halogen;R.sup.
    Type: Grant
    Filed: April 26, 1991
    Date of Patent: February 13, 1996
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Jacob Berger, Robin D. Clark
  • Patent number: 5470580
    Abstract: The present invention relates to directly-compressible naproxen or naproxen sodium compositions comprising spray-dried naproxen or naproxen sodium. The present invention further relates the processes for preparing the directly-compressible naproxen or naproxen sodium compositions, to aqueous mixtures containing naproxen or sodium naproxen suitable for spray-drying and useful in the processes for preparing the directly-compressible compositions, to naproxen or naproxen sodium tablets prepared from the directly-compressible compositions, and to the processes for preparing the naproxen or naproxen sodium tablets.
    Type: Grant
    Filed: July 6, 1994
    Date of Patent: November 28, 1995
    Assignee: Syntex Pharmaceuticals International Limited
    Inventors: Roy Kuramoto, Zakauddin T. Chowhan, Ranal O. Pendleton, Hafez Hafezzadeh
  • Patent number: 5468867
    Abstract: The present invention relates to a process for preparing 1-butyl-2-[2'-(2H-tetrazol-5-yl)biphenyl-4-ylmethyl]-1H-indole-3-carboxyli c acid and to intermediates useful in such process.
    Type: Grant
    Filed: May 27, 1994
    Date of Patent: November 21, 1995
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Lawrence E. Fisher, Lee A. Flippin, Michael G. Martin
  • Patent number: 5446121
    Abstract: The present invention relates to processes for preparing 1-butyl-2-[2'-(2H-tetrazol-5-yl)biphenyl-4-ylmethyl]-1H-indole-3-carboxyli c acid and to intermediates useful in such processes. The present invention also relates to a process for deprotecting compounds containing a protected 2H-tetrazolyl group, which process comprises reacting a the protected compound with a Lewis acid in the presence of a thiol.
    Type: Grant
    Filed: January 17, 1995
    Date of Patent: August 29, 1995
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Robin D. Clark, Lawrence E. Fisher, Lee A. Flippin, Michael G. Martin, Stephen R. Stabler
  • Patent number: 5438150
    Abstract: The present invention relates to a process for preparing a 5-(N-substituted)aminomethyl-1-benzocycloalkyl-1,3-dihydroimidazole-2-thio ne (wherein the N-substituent is selected from formyl, aminocarbonyl, (C.sub.1-4)alkylcarbonyl or trifluoro (C.sub.1-4)alkylcarbonyl), which process comprises reacting a benzocycloalkylamine with thiocyanic acid and dihydroxyacetone to give a corresponding 5-hydroxymethyl-1-benzocycloalkyl-1,3-dihydroimidazole-2-thione and then reacting the 5-hydroxymethyl-1-benzocycloalkyl-1,3-dihydroimidazole-2-thione with a compound of the formula H.sub.2 NC(0)R.sup.2 in which R.sup.2 is hydrogen, amino, (C.sub.1-4)alkyl or trifluoro(C.sub.1-4)alkyl or with an ammonium salt of the formula NH.sub.4.sup.+ - OC(0)R.sup.3 in which R.sup.3 is hydrogen, (C.sub.1-4)alkyl or trifluoro(C.sub.1-4)alkyl.
    Type: Grant
    Filed: April 26, 1994
    Date of Patent: August 1, 1995
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Rekha P. Bansal, Owen W. Gooding, Alexander V. Muehldorf, Counde O-Yang
  • Patent number: 5436264
    Abstract: The present invention relates to novel N-aryloxyalkyl tryptamine .alpha..sub.1 -adrenergic receptor antagonists of the formula I: ##STR1## in which n is 2, 3 or 4; q is 1, 2 or 3; t is 0, 1, 2 or 3; z is 0, 1, 2 or 3; each R.sup.1 and R.sup.2 are independently hydroxy, halogen, cyano, (C.sub.1-8)alkyl, (C.sub.1-8)alkyloxy or trifluoromethyl; and R.sup.2 is hydrogen, (C.sub.1-4)alkyl, fluoro(C.sub.1-4)alkyl, difluoro(C.sub.1-4)alkyl, trifluoro(C.sub.1-4)alkyl, (C.sub.1-4)alkyloxy(C.sub.1-4)alkyl, oxo(C.sub.1-4)alkyl, (C.sub.1-8)cycloalkyl, (C.sub.1-8)cycloalkylmethyl or allyl or phenyl(C.sub.1-4)alkyl or heterocyclo(C.sub.1-8)alkyl (optionally substituted with one to two substituents independently selected from (C.sub.1-4)alkyl, (C.sub.1-4)alkyloxy, trifluoromethyl and halogen); R.sup.3 and R.sup.4 are independently hydrogen, (C.sub.1-4)alkyl, (C.sub.1-8)cycloalkyl, (C.sub.1-8)cycloalkylmethyl or allyl; and R.sup.5 is hydrogen, (C.sub.1-4)alkyl, (C.sub.1-8)cycloalkyl, (C.sub.1-8)cycloalkylmethyl, allyl, (C.
    Type: Grant
    Filed: August 19, 1993
    Date of Patent: July 25, 1995
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Jurg R. Pfister, David E. Clarke
  • Patent number: 5412102
    Abstract: The present invention relates to processes for preparing 1-butyl-2-[2'-(2H-tetrazol-5-yl)biphenyl-4-ylmethyl]-1H-indole-3-carboxyli c acid and to intermediates useful in such processes. The present invention also relates to a process for deprotecting compounds containing a protected 2H-tetrazolyl group, which process comprises reacting a the protected compound with a Lewis acid in the presence of a thiol.
    Type: Grant
    Filed: May 27, 1994
    Date of Patent: May 2, 1995
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Robin D. Clark, Lawrence E. Fisher, Lee A. Flippin, Michael G. Martin, Stephen R. Stabler
  • Patent number: 5358717
    Abstract: The present invention relates to directly-compressible naproxen or naproxen sodium compositions comprising spray-dried naproxen or naproxen sodium. The present invention further relates the processes for preparing the directly-compressible naproxen or naproxen sodium compositions, to aqueous mixtures containing naproxen or sodium naproxen suitable for spray-drying and useful in the processes for preparing the directly-compressible compositions, to naproxen or naproxen sodium tablets prepared from the directly-compressible compositions, and to the processes for preparing the naproxen or naproxen sodium tablets.
    Type: Grant
    Filed: May 4, 1992
    Date of Patent: October 25, 1994
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Roy Kuramoto, Zakauddin T. Chowhan, Randal O. Pendleton, Hafez Hafezzadeh
  • Patent number: 5202318
    Abstract: Compounds of Formula I: ##STR1## in which Z is CH.sub.2 or C.dbd.O;X and Y are independently selected from hydrogen, halogen, hydroxy, lower alkoxy, lower alkyl, nitro, amino, aminocarbonyl, (lower alkyl)amino, di(lower alkyl)amino and (lower alkanoyl)amino; and R.sup.1 is a group selected from Formulae (a), (b), (c) (d) and (e): ##STR2## in which p is 0 or 1;n is 1, 2 or 3;R.sup.2 is hydrogen, lower alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl-C.sub.12 alkyl, or a group R.sup.6 -C.sub.1-2 alkyl in which R.sup.6 is thienyl, pyrrolyl or furyl optionally substituted by one or two substituents selected from lower alkyl, lower alkoxy, trifluoromethyl or halogen, or is phenyl optionally substituted by one or two substituents selected from C.sub.1-4 alkoxy, trifluoromethyl, halogen, nitro, carboxy, esterified carboxy, and C.sub.1-4 alkyl optionally further substituted by hydroxy, C.sub.1-4 alkoxy, carboxy, esterified carboxy or in vivo hydrolyzable acyloxy;each R.sup.
    Type: Grant
    Filed: May 28, 1991
    Date of Patent: April 13, 1993
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Jacob Berger, Robin D. Clark, Richard M. Eglen, William L. Smith, Klaus K. Weinhardt
  • Patent number: 5202333
    Abstract: The present invention is directed to 5-HT.sub.3 receptor antagonist compounds of formula I: ##STR1## in which the dashed line denotes an optional double bond;n is 1, 2 or 3;p is 0, 1, 2 or 3;q is 0, 1 or 2;each R.sup.1 is independently selected from halogen, hydroxy, lower alkoxy, lower alkyl, nitro, amino, amino carbonyl, (lower alkyl)amino, di(lower alkyl)amino, and (lower alkanoyl)amino;each R.sup.2 is lower alkyl; andR.sup.3 is a group selected from Formulae (a), (b), (c) and (d): ##STR2## in which u is 0 or 1;z is 1, 2 or 3; andR.sup.4 is C.sub.1-7 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl-C.sub.1-2 alkyl, or a group (CH.sub.2).sub.t R.sup.5 where t is 1 or 2 and R.sup.5 is thienyl, pyrrolyl, or furyl, each optionally further substituted by one or two substituents selected from C.sub.1-6 alkyl, C.sub.1-6 alkoxy, trifluoromethyl or halogen, or is phenyl optionally substituted by one or two substituents selected from C.sub.
    Type: Grant
    Filed: May 22, 1991
    Date of Patent: April 13, 1993
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Jacob Berger, Robin D. Clark, Richard M. Eglen, William L. Smith, Klaus K. Weinhardt
  • 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