Patents Examined by Anton H. Sutto
  • Patent number: 5017591
    Abstract: This invention relates to novel (aryl or heteroaromatic methyl)-2,2'-1H-biimidazoles; to a process for their production comprising of reacting an appropriate alpha-brominated or alpha-chlorinated, substituted or nonsubstituted, methylated monoaromatic ring compound with 2,2'-bi-1H-imidazole in a solvent such as ethanol in the presence of a base such as sodium hydroxide under reflux conditions; and to pharmaceutical compositions and methods of treating hypertension with such compounds.
    Type: Grant
    Filed: March 2, 1990
    Date of Patent: May 21, 1991
    Assignee: Merrell Dow Pharmaceuticals
    Inventors: Donald P. Matthews, Jeffrey P. Whitten, James B. McCarthy
  • Patent number: 5011947
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 each are independently hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or trifluoromethyl;R is C.sub.1-7 alkyl, C.sub.3-6 cycloalkyl, fluoromethyl, difluoromethyl, trifluoromethyl;A is ##STR2## R.sup.5 is hydrogen, a hydrolyzable ester group or a cation to form a non-toxic pharmaceutically acceptable salt,are novel antihypercholesterolemic agents which inhibit cholesterol biosynthesis. Intermediates and processes for their preparation are disclosed.
    Type: Grant
    Filed: June 12, 1990
    Date of Patent: April 30, 1991
    Assignee: Bristol-Myers
    Inventors: John D. Catt, John J. Wright
  • Patent number: 5011860
    Abstract: Aryl-substituted naphthyridines and pyridopyrazines are disclosed which are useful in treating allergic reactions, inflammation, peptic ulcers and/or hyperproliferative skin disease. Pharmaceutical compositions and methods of treatment employing such compounds are also disclosed.
    Type: Grant
    Filed: June 26, 1989
    Date of Patent: April 30, 1991
    Assignee: Schering Corporation
    Inventors: David J. Blythin, Ho-Jane Shue
  • Patent number: 5010198
    Abstract: Benzoxazol- and benzothiazolamine derivatives having anti-anoxic properties which compounds are useful in the treatment of anoxia. These compounds are produced from certain benzoxazol- and benzothizolamine intermediates.
    Type: Grant
    Filed: August 24, 1989
    Date of Patent: April 23, 1991
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Raymond A. Stokbroekx, Marcel G. M. Luyckx, Frans E. Janssens
  • Patent number: 5008391
    Abstract: A process and intermediates for the enantioselective synthesis of 5,10-dideaza-5,6,7,8-tetrahydrofolic acid are disclosed.
    Type: Grant
    Filed: July 7, 1989
    Date of Patent: April 16, 1991
    Assignee: Eli Lilly and Company
    Inventors: Charles J. Barnett, Thomas M. Wilson
  • Patent number: 5003066
    Abstract: The polyglycidamides are epoxy derivatives of cyclic ureas such as glycouril and aminotriazines such as melamine and guanamines. They are prepared from cyclic ureas and aminotriazines by methylolating with formaldehyde, etherifying with an alcohol, transetheramidizing with acrylamide and epoxidizing with hydrogen peroxide. They are used with polyamines and other epoxy reactive oligomers to provide crosslinkable coating systems which posses solvent, chemical and water resistance and UV stability.
    Type: Grant
    Filed: March 29, 1989
    Date of Patent: March 26, 1991
    Assignee: Monsanto Company
    Inventor: William F. Pfohl
  • Patent number: 5001249
    Abstract: The formation of dialkyl phosphorodithioic acids by reacting phosphorus pentasulfide with an alcohol is catalyzed by using an organosulfur halide catalyst for the reaction. Representative classes of organosulfur halide catalysts include the sulfonium halides, the sulfoxonium halides, and polymeric sulfur halide materials.
    Type: Grant
    Filed: March 16, 1988
    Date of Patent: March 19, 1991
    Assignee: ICI Americas Inc.
    Inventor: Stanley B. Mirviss
  • Patent number: 4999429
    Abstract: Aryl difluoromethyl sulfone adds to aldehydes under phase transfer conditions to give novel substituted alcohols of the general formulaRCH(OH)CF.sub.2 SO.sub.2 Ar (I)wherein R is an aryl, cycloaliphatic, sec- or tert-aliphatic, or heterocyclic group and Ar is an aryl group. The substituted alcohols of formula I are of particular utility as intermediates in the synthesis of a variety of useful end products. For example, the products of formula I may be utilized in desulfonylation reactions, oxidation reactions and fluorination reactions.
    Type: Grant
    Filed: November 13, 1989
    Date of Patent: March 12, 1991
    Assignee: Ethyl Corporation
    Inventor: G. Patrick Stahly
  • Patent number: 4990674
    Abstract: Disclosed is a method of making an aliphatic aromatic phosphine oxide by reacting an aliphatic aromatic phosphinic acid with a halogenating agent to produce a phosphoryl halide, reducing the phosphoryl halide to a phosphinous halide, hydrolyzing the phosphinous halide with water to produce a mixture of a phosphine and a phosphine oxide, determining how much phosphine is present in said mixture, and adding sufficient oxidizing agent to oxidize the phosphine in the mixture to the corresponding phosphine oxide. Octylphenyl phosphine oxide is preferred. The phosphine oxides are useful in making extractants for extracting actimides and lanthanides.
    Type: Grant
    Filed: June 14, 1989
    Date of Patent: February 5, 1991
    Assignee: Occidental Chemical Corporation
    Inventor: Mohan S. Saran
  • Patent number: 4965391
    Abstract: Novel radioiodinated analogues of naturally occurring phospholipid ethers are tumor-specific to enable selective visualization of neoplastic lesions by gamma-camera scintigraphy. The novel compounds enable a physician to differentiate neoplastic lesions from non-neoplastic lesions in a manner not heretofore available.
    Type: Grant
    Filed: October 23, 1987
    Date of Patent: October 23, 1990
    Assignee: The University of Michigan
    Inventors: Raymond E. Counsell, Karen L. Meyer, Susan W. Schwendner
  • Patent number: 4956487
    Abstract: Thiophosphonate compounds having the formula ##STR1## in which R is alkyl, haloalkyl or aryl; X is chloro or SR.sub.2 ; R.sub.1 is alkyl or aryl; and when X is SR.sub.2 then R.sub.2 is a group identical to R.sub.1, or R.sub.1 and R.sub.2 taken together form an optionally alkyl-substituted polymethylene group, are prepared by reaction of a thiophosphonodichloride with a mercaptan in the presence of a catalytic amount of a quaternary ammonium or phosphonium salt, a tertiary amine or hydrohalide thereof or an alkali metal halide combined with a Crown ether, in the substantial absence of a base.
    Type: Grant
    Filed: December 12, 1988
    Date of Patent: September 11, 1990
    Assignee: ICI Americas Inc.
    Inventors: Jeffrey D. Robbins, Richard D. Gless, Jr.
  • Patent number: 4952740
    Abstract: New cyclic phosphonites, in which one of the oxygen atoms of the ring can be replaced by an atom of sulphur or nitrogen; the molecule has an asymmetry due to at least two carbon atoms, one or more nitrogen and/or oxygen atoms or several of these elements together.Preparation of these phosphonites by the reaction of a dihalogeno-phosphine with a compound having two active H atoms, in the presence of a hydracid acceptor.Application of the new phosphonites to the production of the corresponding phosphinates and phosphine oxides.
    Type: Grant
    Filed: September 12, 1989
    Date of Patent: August 28, 1990
    Assignee: Societe Nationale Elf Aquitaine
    Inventors: Sylvain Juge, Yvonne Legras
  • Patent number: 4952578
    Abstract: The object of the invention is a new cephem compound with antimicrobial activity used for the treatment of infectious diseases of the general formula: ##STR1## wherein R1 is amino or a protected aminoR2 is lower alkyl which may have 1 to 3 halogensR3 is COO.sup..crclbar., carboxy or a protected carboxyR4 is hydroxy(lower)alkyl or protected hydroxy(lower)alkylR5 is amino or a protected aminoR6 is hydrogen or lower alkylX.sup..crclbar. is an anion, andn is 0 or 1with proviso that(i) when R3 is COO.sup..crclbar., then n is 0, and(ii) when R3 is carboxy or a protected carboxy, then n is 1,and pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: September 7, 1988
    Date of Patent: August 28, 1990
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Kazuo Sakane, Kohji Kawabata, Kenzi Miyai, Yoshiko Inamoto
  • Patent number: 4950759
    Abstract: The invention relates to a group of new substituted 1,7-annelated 1H-indazole derivatives being strong and selective antagonists of "neuronal" 5-hydroxytryptamine (5-HT) receptors.
    Type: Grant
    Filed: July 3, 1989
    Date of Patent: August 21, 1990
    Assignee: Duphar International Research B.V.
    Inventors: Ineke van Wijngaarden, Derk Hamminga, Hans H. Haeck, Wouter Wouters
  • Patent number: 4950784
    Abstract: The O-alkyl S,S-dialkylphosphorodithioates, e.g., ethoprophos, are facilely prepared, in improved yields and having great purity, by reacting an alkylphosphate dihalogenide, e.g., a dichloride, with a 1.5 to 8 mol excess of a thiol, in the presence of a 0.1 to 5 mol excess of an acid acceptor, with both molar excesses being per mole of said dihalogenide.
    Type: Grant
    Filed: July 24, 1987
    Date of Patent: August 21, 1990
    Assignee: Rhone-Poulenc Agrochimie
    Inventors: Jean-Michel Brochard, Francois Frisou, Pierre Le Roy
  • Patent number: 4950819
    Abstract: A process for the preparation of alkali metal salts of phosphonic acid monoalkyl esters of formula ##STR1## by reacting 1 mole of a phosphonic acid ester of formula ##STR2## with 1 mole of a finely particulate alkali metal halide of formula XY. In these formulae, R is straight chain or branched C.sub.1 -C.sub.20 alkyl, R.sub.1 is C.sub.1 -C.sub.4 alkyl, X is an alkali metal cation and Y is a halogen anion.
    Type: Grant
    Filed: September 19, 1988
    Date of Patent: August 21, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Claus D. Weis, Peter Sutter
  • Patent number: 4948895
    Abstract: A 6-tertiary amino-2-(Z.dbd.CH--)benzofuran dye is disclosed, where Z represents the atoms providing an electron withdrawing group and a conjugated methine linkage completing a resonant dye chromophore including the 6-tertiary amino group as an electron donor and the electron withdrawing group as an electron acceptor. The dyes are formed by condensing a 6-tertiary amino-2-formylbenzofuran with an electron withdrawing dye nucleus precursor containing an active methyl or methylene site. The dyes exhibit bathochromically shifted absorption peaks.
    Type: Grant
    Filed: October 13, 1989
    Date of Patent: August 14, 1990
    Assignee: Eastman Kodak Company
    Inventors: Chin H. Chen, John L. Fox
  • Patent number: 4948582
    Abstract: Disclosed are pharmaceutical compositions containing naphthoic acid derivatives and method of use for enhancing oxygen availability to mammailian tissue.
    Type: Grant
    Filed: May 11, 1989
    Date of Patent: August 14, 1990
    Assignee: Rorer Pharmaceutical Corporation
    Inventors: John T. Suh, Robert G. Pendleton, Charles E. Pendley, II, Kin T. Yu, Paul R. Menard, Alain B. Schreiber
  • Patent number: 4948905
    Abstract: Synthesis of vinyl lactones by means of palladium catalyzed coupling of vinylic halides or triflates and certain unsaturated carboxylic acids.
    Type: Grant
    Filed: September 18, 1989
    Date of Patent: August 14, 1990
    Assignee: Iowa State University Reasearch Foundation, Inc.
    Inventor: Richard C. Larock
  • Patent number: 4946863
    Abstract: The present invention relates to 3-aminomethyl derivatives of indane, dihydrobenzofurane, dihydrobenzothiophene, and indoline, acid addition salts thereof, isomers thereof, methods of preparation, pharmaceutical compositions and method of treating CNS-disorders such as schizophrenia, Parkinson's disease, depression, anxiety, migraine and senile dementia, or in the cure of cardiovascular diseases, by administering such a derivative.
    Type: Grant
    Filed: January 18, 1989
    Date of Patent: August 7, 1990
    Assignee: H. Lundbeck A/S
    Inventors: Klaus P. Boegesoe, Jens K. Perregaard