Patents Examined by Catherine S. Kilby Scalzo
  • Patent number: 5106998
    Abstract: Disclosed is a compound represented by the following general formula(I): ##STR1## wherein R.sub.1 and R.sub.2, which may be the same or different, represent a hydrogen atom, an alkyl group, an aryl group, an aralkyl group or a substituted amino group, R.sub.3 and R.sub.4, which may be the same or different, represent an alkyl group, or R.sub.3 and R.sub.4 together form a nobornylidene group or bicyclo (3, 3, 1) 9-nonylidene group which may have a substituent, and ##STR2## represents a divalent aromatic hydrocarbon group or divalent unsaturated heterocyclic group which may have a substituent, with the proviso that when R.sub.3 and R.sub.4 represent an alkyl group, ##STR3## represents a bicyclic aromatic fused ring which is substituted with at least one substituent selected form the group consisting of a halgoen atom, an alkyl group, an alkoxy group, --R.sub.5 --S--R.sub.6 and ##STR4## (in which R.sub.5 represents an alkylene group or --O--R.sub.8).sub.n (in which R.sub.
    Type: Grant
    Filed: March 9, 1990
    Date of Patent: April 21, 1992
    Assignee: Tokuyama Soda Kabushiki Kaisha
    Inventors: Takashi Tanaka, Satoshi Imura, Kenji Tanaka, Yasuji Kida
  • Patent number: 5101048
    Abstract: The present invention relates, by way of novel industrial products, to the .beta.-D-phenylthioxyloside compounds of the formula ##STR1## in which: X represents a sulfur atom or an oxygen atom;R.sub.1, R.sub.2 and R.sub.3, which are identical or different, each represent a hydrogen atom, a nitro group, a cyano group, a group --CO--R (in which R represents a C.sub.1 -C.sub.4 alkyl group or a trifluoromethyl group), an amino group, an acetamido group (NHCOCH.sub.3), a C.sub.1 -C.sub.4 alkoxy group, a trifluoromethyl group or a phenyl group substituted by one or more cyano, nitro or trifluoromethyl groups, it being possible for R.sub.1 and R.sub.2, taken together, to form, with the phenyl group to which they are bonded, a .beta.-naphthalenyl group which is unsubstituted or substituted by one or more cyano, nitro or trifluoromethyl groups; andY represents the hydrogen atom or an aliphatic acyl group.These compounds are useful as therapeutic agents, especially as venous antithrombotics.
    Type: Grant
    Filed: October 18, 1989
    Date of Patent: March 31, 1992
    Assignee: Fournier Industrie et Sante
    Inventors: Jerzy Bajgrowicz, Patrice Renaut, Veronique Barberousse, Soth Samreth, Jean Millet, Francois Bellamy
  • Patent number: 5096920
    Abstract: The use of 5-phenyl-3H-1,2-dithiol-3-thion-S-oxides which are optionally substituted in the phenyl ring as active substances in hepato-protective medicaments and new 5-phenyl-3H-1,2-dithiol-3-thion-S-oxides which are substituted in the phenyl ring are described.
    Type: Grant
    Filed: May 26, 1989
    Date of Patent: March 17, 1992
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Dominique Biard, Marie-Odile Christen, Patrick Dansette, Daniel Jasserand, Daniel Mansuy, Amor Sassi
  • Patent number: 5093493
    Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof: ##STR1## wherein: R.sub.1 is hydrogen, C.sub.1-6 alkyl, phenyl or phenyl C.sub.1-4 alkyl wherein the phenyl moiety is optionally substituted by one or more C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, hydroxy, C.sub.2-7 alkanoyl, halo, trifluoromethyl, nitro, amino optionally substituted by one or two C.sub.1-6 alkyl groups or by C.sub.2-7 alkanoyl, cyano, carbamoyl or carboxy groups;R.sub.2, R.sub.3 and R.sub.4 are independently selected from hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 alkylthio, C.sub.2-7 alkanoyl, trifluoromethyl, cyano, carbamoyl and carboxy, and phenyl or phenyl C.sub.1-4 alkyl in which any phenyl moiety is optionally substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkoxy carbonyl, C.sub.1-6 alkylthio, hydroxy, C.sub.2-7 alkanoyl, chloro, fluoro, trifluoromethyl, nitro or amino optionally substituted by one or two C.sub.1-6 alkyl groups or by C.sub.
    Type: Grant
    Filed: March 12, 1990
    Date of Patent: March 3, 1992
    Assignee: Beecham Group p.l.c.
    Inventors: Mervyn Thompson, Ian T. Forbes, Christopher N. Johnson
  • Patent number: 5087638
    Abstract: Benzofuran derivatives, pharmaceutical compositions and methods of treatment are disclosed. These compounds are useful as inhibitors of mammalian leukotriene biosynthesis. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders, inflammation. The compounds are also useful as analgesics and as cytoprotective agents.
    Type: Grant
    Filed: June 28, 1989
    Date of Patent: February 11, 1992
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Patrice C. Belanger, John Scheigetz, Joshua Rokach
  • Patent number: 5086180
    Abstract: Sulphamoylathiophenes of the formula ##STR1## in which Y denotes O or S,A denotes a single bond or a straight-chain or branched alkylene group having 1-5 carbon atoms,R.sub.1 denotes methyl or trifluoromethyl andR.sub.2 denotes hydrogen or a group COOH or COOR.sub.3, in whichR.sub.3 represents (C.sub.1 -C.sub.4)-alkyl,and, in the case in which R.sub.2 denotes a group COOH, their pharmaceutically tolerable salts, a process for their preparation, pharmaceutical preparations which contain these compounds and their use in medicaments as leukotriene antagonists for the treatment of asthma and allergies.
    Type: Grant
    Filed: June 15, 1990
    Date of Patent: February 4, 1992
    Assignee: Chemisch Pharmazeutische Forschungsgesellschaft m.b.H.
    Inventors: Dieter Binder, Franz Rovenszky, Norman Brunner, Hubert P. Ferber
  • Patent number: 5084207
    Abstract: Liquid composition for controlling dust migration which comprises an emulsion of liquid asphalt, a lignosulfonic acid salt solution and water. The emulsion is spread on a dusty surface to penetrate the same before the emulsion breaks.
    Type: Grant
    Filed: February 16, 1990
    Date of Patent: January 28, 1992
    Inventors: Jeffrey Reed, Wendell Reed
  • Patent number: 5082859
    Abstract: Derivatives of benzocycloalkenyldihydroxyalkanoic acids, inhibitors of HMG CoA reductase, antagonists of thromoboxane A.sub.2 receptors and antifungals, denoted by the formula I ##STR1## in which X=CH.sub.2, O or S; R.sub.1 and R.sub.2, identical or different, =H, C.sub.1-3 alkyl or together from a --(CH.sub.2).sub.n -- chain (n=4,5) optionally substituted symmetrically by one or two C.sub.1-3 alkyl radicals.R.sub.3 and R.sub.4, identical or different, =H, CF.sub.3, halogen (Cl, F, Br), C.sub.1-5 N,N-dialkylamino, C.sub.1-4 alkyl, C.sub.1-5 -alkoxy, C.sub.1-3 alkylthio, or phenyl optionally substituted by at most two substitutents which may be identical or different and may denote C.sub.1-3 alkyl or C.sub.1-3 alkoxy radicals or halogens (F, Cl), it being understood that when one of R.sub.3 and R.sub.4 denotes the radicals: CF.sub.3, N,N-dialkylamino, C.sub.6 H.sub.5 or substituted phenyl, it is present at the vertices 3', 4'or 5' according to formula 1 and the other denotes a hydrogen atom.R.sub.5 and R.sub.
    Type: Grant
    Filed: January 24, 1990
    Date of Patent: January 21, 1992
    Assignee: Lipha, Lyonnaise Industrielle Pharmaceutique
    Inventors: Didier Festal, Jean-Yves Nioche, Denis Descours, Robert Bellemin, Jacques Decerprit
  • Patent number: 5081266
    Abstract: A new process for preparing [1S-[1.alpha.,2.alpha.(Z),-3.alpha.,4.alpha.]]-7-[3-[[[[(1-oxoheptyl)-amin o]acetyl]amino]methyl]-7-oxabicyclo [2.2.1]-hept-2-yl]-5-heptenoic acid. New intermediates are also described. [1S-(1.alpha.,2.alpha.(9Z),3.alpha.,4.alpha.]]-7-[3-[[[[(1-oxoheptyl)-amin o]acetyl]amino]methyl]-7-oxabicyclo[2.2.1]hept-2-yl]-5-heptenoic acid is useful in the treatment of thrombotic disease.
    Type: Grant
    Filed: September 26, 1990
    Date of Patent: January 14, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: David Kronenthal
  • Patent number: 5081118
    Abstract: A series of novel oxyethyl derivatives of certain selected enolic oxicam compounds are disclosed, including certain novel oxyethyl derivatives of 4-hydroxy-2-methyl-N-(2-pyridinyl)-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide (piroxicam). These particular compounds are useful in therapy as prodrug forms of the known anti-inflammatory and analgesic oxicams. Said oxyethyl derivatives of enoic oxicam compounds like piroxicam are of the formulae: ##STR1## wherein R.sub.1 is hydrogen, methyl, fluorine or chlorine, and R.sub.2 is hydrogen or --COOR.sub.3 wherein R.sub.3 is alkyl having from one to eight carbon atoms.
    Type: Grant
    Filed: April 26, 1990
    Date of Patent: January 14, 1992
    Assignee: Pfizer Inc.
    Inventors: Andrew C. Braisted, Philip D. Hammen
  • Patent number: 5077302
    Abstract: Urea derivatives of the following formula: ##STR1## wherein R.sub.2 indicates a piperidino or pyrrolidino group which may be substituted with a hydroxy group or a lower alkyl group having 1 to 13 carbon atoms; A indicates an ethylene group, propylene group, butylene group or butenylene group; R.sub.2 indicates a straight or branched alkyl group having 1 to 20 carbon atoms, a benzyl group, or a phenyl group which may have 1 to 3 substituents such as a lower alkyl group having 1 to 6 carbon atoms, a lower alkoxy group having 1 to 3 carbon atoms, a halogen atom, a trifluoromethyl group, an amino group, a nitro group or a methylenedioxy group; and X indicates an oxygen or sulfur atom, as well as the hydrates and pharmaceutically acceptable salts thereof are useful antiulcer agents.
    Type: Grant
    Filed: May 15, 1990
    Date of Patent: December 31, 1991
    Assignee: Kyorin Pharmaceutical Co., Ltd.
    Inventors: Hiroshi Matsukubo, Toyomi Matsumoto, Mitsutomo Miyashita, Kyuya Okamura, Fukutaro Taga, Haruo Sekiguchi, Katsuhiro Hamada
  • Patent number: 5077293
    Abstract: Certain 1-indolylalkyl-4-(alkoxypyrimidinyl)piperazines of Formula I are useful antidepressant agents. The ##STR1## substituents R.sup.1, R.sup.2 and R.sup.5 are hydrogen or lower alkyl; R.sup.3 and R.sup.4 are hydrogen, alkyl, alkoxy, alkythio, carboxamido, halo, or trifluoromethyl; R.sup.6 is alkoxy; and n is the integer 2 or 3.
    Type: Grant
    Filed: June 29, 1990
    Date of Patent: December 31, 1991
    Assignee: Bristol-Myers Squibb Co.
    Inventors: David W. Smith, Frank D. Yocca, Joseph P. Yevich, Ronald J. Mattson
  • Patent number: 5075303
    Abstract: Pyridine derivatives of formula ##STR1## their heteroaromatic N-oxides and their pharmaceutically acceptable acid addition salts are disclosed. In the formula z is 0, 1 and 2 and R, R.sup.1, R.sup.2 and R.sup.2 have specified meanings. The compounds exhibit activity as 5-HT.sub.1A agonists, antagonists or partial agonists and are useful for the treatment of CNS disorders e.g. anxiety, as antihypertensives and in treating anorexia.
    Type: Grant
    Filed: April 6, 1990
    Date of Patent: December 24, 1991
    Assignee: John Wyeth & Brother Limited
    Inventors: Ian A. Cliffe, Howard L. Mansell, Richard S. Todd, Alan C. White
  • Patent number: 5075460
    Abstract: A compound of the formula ##STR1## wherein: one of R.sub.1 and R.sub.2 is hydrogen or C.sub.1-4 alkyl and the other is C.sub.1-4 alkyl or R.sub.1 and R.sub.2 together are C.sub.2-5 polymethylene; and R'.sub.4 is ethyl, isopropyl, t-butyl or cyclopentyl.
    Type: Grant
    Filed: December 6, 1989
    Date of Patent: December 24, 1991
    Assignee: Beecham Group plc
    Inventors: John M. Evans, Geoffrey Stemp, Frederick Cassidy
  • Patent number: 5073298
    Abstract: A defoamer composition including a primary antifoam agent which includes a particulate-type material having a high surface area such as silica, a secondary antifoam agent for acting synergistically with the primary antifoam agent such as polydimethylsiloxane, a water carrier, and a quaternary ammonium salt silane compound which functions as an antimicrobial agent, fixed and adhered to the surface of the particulate material, in order that the defoamer composition be resistant to biological degradation due to the presence in the system of microorganisms. Methods of defoaming cationic, anionic, and nonionic surfactant produced foams are disclosed, as is a method of rendering silica hydrophobic.
    Type: Grant
    Filed: July 7, 1989
    Date of Patent: December 17, 1991
    Assignee: Dow Corning Corporation
    Inventors: Thomas M. Gentle, William C. White
  • Patent number: 5073560
    Abstract: Compounds of general formula I, ##STR1## wherein: A represents (CH.sub.2).sub.m optionally substituted by R.sub.3,B represents (CH.sub.2).sub.n optionally substituted by R.sub.4,R.sub.1 represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1-6 alkenyl or C.sub.1-6 alkynyl,R.sub.2 represents hydrogen, C.sub.1 -C.sub.6 alkyl or COOR.sub.5, in which R.sub.5 represents C.sub.1 -C.sub.6 alkyl,R.sub.3 and R.sub.4 independently represent hydrogen or C.sub.1 -C.sub.6 alkyl,in addition, any two of R.sub.2, R.sub.3 and R.sub.4 may together form a C.sub.1-3 alkylene chain,n and m independently represent an integer from 1-3 inclusive,Y represents O or S,and pharmaceutically acceptable acid addition salts thereof are useful as pharmaceuticals, in particular as central muscarinic acetylcholine receptor agonists. The compounds are therefore useful in the treatment of diseases such as presenile and senile dementia, Huntington's chorea, tardive dyskinesia, hyperkinesia, mania and Tourette Syndrome.
    Type: Grant
    Filed: July 20, 1990
    Date of Patent: December 17, 1991
    Assignee: Fisons Corporation
    Inventors: Edwin S. Wu, Alexander Kover
  • Patent number: 5073557
    Abstract: The compound (R)-3-[2-(6-chloropyrazin)yl]-1-azabicyclo[2.2.2]octane and its salts behave as M.sub.1, M.sub.3 muscarinic agonists and are useful in the treatment of neurological and mental disorders, preferably in a pharmaceutical formulation comprising the active compound in association with a pharmaceutically acceptable carrier. The compound can be prepared by via methods analogous to those known in the art and a chiral acid resolution.
    Type: Grant
    Filed: August 8, 1990
    Date of Patent: December 17, 1991
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Raymond Baker, Leslie J. Street, John Saunders
  • Patent number: 5071990
    Abstract: A process for the preparation of N-(2-hydroxyethyl)-2-hydroxymethyl-3,4,5-trihydroxypiperidines of the formula ##STR1## which comprises reacting a compound of the formula ##STR2## with glyoxal of the formula ##STR3## in a solvent to give the addition product ##STR4## and reducing such addition product (II) with a hydrogen donor reducing agent to produce the intermediates of the formula and then the end product (I).
    Type: Grant
    Filed: October 4, 1990
    Date of Patent: December 10, 1991
    Assignee: Bayer Aktiengesellschaft
    Inventor: Werner Hinsken
  • Patent number: 5070094
    Abstract: N-benzyl tropane amides, which have activity as Class III antiarrhythmic agents, acting by prolonging cardiac action potential repolarization. The invention further provides for compositions incorporating the compounds and methods of their use, as well as providing for pharmaceutically acceptable salts of the compounds.
    Type: Grant
    Filed: September 5, 1989
    Date of Patent: December 3, 1991
    Assignee: G. D. Searle & Co.
    Inventor: Kerry W. Fowler
  • Patent number: 5068332
    Abstract: This invention relates to alkylidene analogs of 1'-aminospiro[isoquinoline-4(1H),3'-pyrrolidine]-1,2',3,5'(2H)-tetrones, represented by formula (I): ##STR1## to processes for the preparation, to methods for using the compounds, and to pharmaceutical preparations thereof. The compounds have pharmaceutical properties which render them beneficial for the prevention or treatment of diabetes mellitus associated complications.
    Type: Grant
    Filed: October 11, 1990
    Date of Patent: November 26, 1991
    Assignee: American Home Products Corporation
    Inventor: Michael S. Malamas