Patents Represented by Attorney, Agent or Law Firm Wayne W. Montgomery
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Patent number: 8206695Abstract: 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: GrantFiled: October 10, 2007Date of Patent: June 26, 2012Assignee: La Canada Ventures, Inc.Inventor: Suan Lin
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Patent number: 6492362Abstract: 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: GrantFiled: September 15, 2000Date of Patent: December 10, 2002Assignee: Axys Pharmaceuticals, Inc.Inventors: Michael Graupe, John O. Link, John W. Patterson, Sheila Zipfel
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Patent number: 6465503Abstract: 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: GrantFiled: August 10, 2001Date of Patent: October 15, 2002Assignee: Axys Pharmaceuticals, Inc.Inventor: Richard Laurence Mackman
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Patent number: 6150379Abstract: 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: GrantFiled: November 17, 1998Date of Patent: November 21, 2000Assignee: Axys Pharmaceuticals, Inc.Inventors: Paul R. Fatheree, Thomas E. Jenkins, Martin S. Linsell, Sean G. Trapp, Erik J. Verner, Wendy B. Young
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Patent number: 6103879Abstract: 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: GrantFiled: June 16, 1997Date of Patent: August 15, 2000Assignee: Axys Pharmaceuticals, Inc.Inventors: Warak Lee Chaovapong, Lutz B. Giebel, Cyrus Karkaria, Michael J. Ross, Helmut H. Schneider, Kevin Shoemaker
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Patent number: 5693515Abstract: 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: GrantFiled: April 28, 1995Date of Patent: December 2, 1997Assignee: Arris Pharmaceutical CorporationInventors: James M. Clark, Thomas E. Jenkins, Bradley A. Katz, Robert M. Stroud
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Patent number: 5510486Abstract: 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: GrantFiled: July 26, 1994Date of Patent: April 23, 1996Assignee: Syntex (U.S.A.) Inc.Inventors: James Robinson, III, John C. Rohloff, Bruce A. Kowalczyk
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Patent number: 5492914Abstract: 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: GrantFiled: July 28, 1994Date of Patent: February 20, 1996Assignee: Syntex (U.S.A.) Inc.Inventors: Jacob Berger, Robin D. Clark, Paul E. Weller, Douglas L. Wren
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Patent number: 5491148Abstract: 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: GrantFiled: April 26, 1991Date of Patent: February 13, 1996Assignee: Syntex (U.S.A.) Inc.Inventors: Jacob Berger, Robin D. Clark
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Patent number: 5470580Abstract: 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: GrantFiled: July 6, 1994Date of Patent: November 28, 1995Assignee: Syntex Pharmaceuticals International LimitedInventors: Roy Kuramoto, Zakauddin T. Chowhan, Ranal O. Pendleton, Hafez Hafezzadeh
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Patent number: 5468867Abstract: 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: GrantFiled: May 27, 1994Date of Patent: November 21, 1995Assignee: Syntex (U.S.A.) Inc.Inventors: Lawrence E. Fisher, Lee A. Flippin, Michael G. Martin
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Patent number: 5446121Abstract: 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: GrantFiled: January 17, 1995Date of Patent: August 29, 1995Assignee: Syntex (U.S.A.) Inc.Inventors: Robin D. Clark, Lawrence E. Fisher, Lee A. Flippin, Michael G. Martin, Stephen R. Stabler
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Patent number: 5438150Abstract: 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: GrantFiled: April 26, 1994Date of Patent: August 1, 1995Assignee: Syntex (U.S.A.) Inc.Inventors: Rekha P. Bansal, Owen W. Gooding, Alexander V. Muehldorf, Counde O-Yang
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Patent number: 5436264Abstract: 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: GrantFiled: August 19, 1993Date of Patent: July 25, 1995Assignee: Syntex (U.S.A.) Inc.Inventors: Jurg R. Pfister, David E. Clarke
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Patent number: 5412102Abstract: 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: GrantFiled: May 27, 1994Date of Patent: May 2, 1995Assignee: Syntex (U.S.A.) Inc.Inventors: Robin D. Clark, Lawrence E. Fisher, Lee A. Flippin, Michael G. Martin, Stephen R. Stabler
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Patent number: 5358717Abstract: 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: GrantFiled: May 4, 1992Date of Patent: October 25, 1994Assignee: Syntex (U.S.A.) Inc.Inventors: Roy Kuramoto, Zakauddin T. Chowhan, Randal O. Pendleton, Hafez Hafezzadeh
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Patent number: 5202318Abstract: 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: GrantFiled: May 28, 1991Date of Patent: April 13, 1993Assignee: Syntex (U.S.A.) Inc.Inventors: Jacob Berger, Robin D. Clark, Richard M. Eglen, William L. Smith, Klaus K. Weinhardt
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Patent number: 5202333Abstract: 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: GrantFiled: May 22, 1991Date of Patent: April 13, 1993Assignee: Syntex (U.S.A.) Inc.Inventors: Jacob Berger, Robin D. Clark, Richard M. Eglen, William L. Smith, Klaus K. Weinhardt
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Patent number: 5192770Abstract: .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: GrantFiled: December 7, 1990Date of Patent: March 9, 1993Assignee: Syntex (U.S.A.) Inc.Inventors: Robin D. Clark, Richard M. Eglen, Joseph M. Muchowski, William L. Smith, Klaus K. Weinhardt
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Patent number: 5189041Abstract: 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: GrantFiled: November 16, 1990Date of Patent: February 23, 1993Assignee: Syntex (U.S.A.) Inc.Inventors: Jacob Berger, Robin D. Clark