Patents Examined by Joseph Paul Brust
  • Patent number: 5578639
    Abstract: Certain compounds have been synthesized and found to be effective inhibitors of phospholipase A.sub.2 (PLA.sub.2), and thereby useful in the treatment of intestinal cholesterol absorption and the disease states arising therefrom, such as hypercholesterolemia and coronary artery disease.
    Type: Grant
    Filed: May 30, 1995
    Date of Patent: November 26, 1996
    Assignee: Warner-Lambert Company
    Inventor: Reynold Homan
  • Patent number: 5543431
    Abstract: A compound having the formula ##STR1## which is an anti-fungal agent is described. The producing organism Colletotricum accutatum is also described, along with a method of production.
    Type: Grant
    Filed: May 24, 1995
    Date of Patent: August 6, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Evon A. Bolessa, Robert E. Schwartz, Gerald F. Bills, Robert A. Giacobbe, Fernando Pelaez Perez, Angeles Cabello Arroyo, Teresa Diez Matas, Isabel Martin Fernandez, Francisca Vicente Perez, Suzanne M. Mandala, Deborah L. Zink, Rosemary Thornton, John R. Thompson, James E. Curotto
  • Patent number: 5536866
    Abstract: Triarylamino-based dinitrile and dicarboxylic acid monomers as represented by the formula: ##STR1## wherein Z is --CN or --COOH and R is selected from the group consisting of --H, --CH.sub.3, --N(CH.sub.3).sub.2 and --OH.
    Type: Grant
    Filed: January 26, 1995
    Date of Patent: July 16, 1996
    Assignee: The United States of America as represented by the Secretary of the Air Force
    Inventors: Loon-Seng Tan, Kasturi R. Srinivasan
  • Patent number: 5527946
    Abstract: Aliphatic alpha, omega-aminonitriles are prepared by partial hydrogenation of aliphatic alpha, omega-dinitriles at elevated temperatures and superatmospheric pressure in the presence of a solvent and of a catalyst by a process which comprises using a catalyst which(a) contains a compound based on a metal selected from the group consisting of nickel, cobalt, iron, ruthenium and rhodium and(b) contains from 0.
    Type: Grant
    Filed: January 18, 1995
    Date of Patent: June 18, 1996
    Assignee: BASF Aktiengesellschaft
    Inventors: Klemens Flick, Johann-Peter Melder, Werner Schnurr, Klaus Ebel, Tom Witzel, Wolfgang Harder, Alwin Rehfinger, Rolf Fischer
  • Patent number: 5527923
    Abstract: The present invention relates to a new process for preparing enantiomerically pure diarylprolinols, especially (R)-(+)- or (S)-(-)-2-(diphenylhydroxymethyl)-pyrrolidine (R)-(+)- or (S)-(-)-.alpha.,.alpha.-diphenyl-(2-pyrrolidinyl)-methanol) starting from proline.
    Type: Grant
    Filed: May 4, 1995
    Date of Patent: June 18, 1996
    Assignee: Boehringer Ingelheim KG
    Inventors: Franz D. Klingler, Rainer Sobotta
  • Patent number: 5525734
    Abstract: Disclosed are methods for synthesizing very large collections of diverse pyrrolidine compounds on solid supports and synthetic compound libraries comprising pyrrolidine groups prepared by such methods.
    Type: Grant
    Filed: June 22, 1994
    Date of Patent: June 11, 1996
    Assignee: Affymax Technologies N.V.
    Inventors: Mark A. Gallop, Martin A. Murphy
  • Patent number: 5525735
    Abstract: Disclosed are methods for synthesizing very large collections of diverse pyrrolidine compounds and derivatives thereof on solid supports and synthetic compound libraries comprising pyrrolidine groups and derivatives thereof prepared by such methods.
    Type: Grant
    Filed: December 12, 1994
    Date of Patent: June 11, 1996
    Assignee: AFFYMAX Technologies NV
    Inventors: Mark A. Gallop, Martin A. Murphy
  • Patent number: 5523453
    Abstract: A process for hydrocyanation of certain ethylenically unsaturated compounds which uses a catalyst composition comprising certain bidentate phosphorous compounds and zero-valent nickel in the presence of a Lewis Acid promoter.
    Type: Grant
    Filed: March 22, 1995
    Date of Patent: June 4, 1996
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Anne I. Breikss
  • Patent number: 5521212
    Abstract: Compounds of the formula ##STR1## wherein A is C1 to C3 alkylene, Ar is phenyl or styryl, R is halosubstituted C1 to C3 alkyl, NHR' or ##STR2## R' is hydrogen or C2 to C8 alkytthioalkyl, n is an integer of from 1 to 4 and p is an integer of from 2 to 5, with the proviso that when R' is hydrogen then Ar is styryl, and the pharmaceutically acceptable salts thereof, inhibit the enzyme lipoxygenase and are useful in treating allergy and inflammatory and cardiovascular conditions for which the action of lipoxygenase has been implicated. These compounds form the active ingredient in pharmaceutical compositions for treating such conditions.
    Type: Grant
    Filed: August 26, 1994
    Date of Patent: May 28, 1996
    Assignee: Pfizer Inc.
    Inventors: Takafumi Ikeda, Akiyoshi Kawai, Takashi Mano, Yoshiyuki Okumura, Rodney W. Stevens
  • Patent number: 5519162
    Abstract: A method for removing hydrogen cyanide from a hydrogen cyanide-contaminated organic liquid includes the steps of contacting the hydrogen cyanide-contaminated organic liquid with a metal alkoxide to generate a metal cyanide salt and an alkanol and then separating the organic liquid from the metal cyanide salt and the alkanol.
    Type: Grant
    Filed: August 23, 1994
    Date of Patent: May 21, 1996
    Assignee: Rohm and Haas Company
    Inventors: Sudhir K. Agarwal, Rajiv M. Banavali, Bharati D. Chheda, Samuel F. Reed, Jr.
  • Patent number: 5519052
    Abstract: Carbonarins A, B, C, D, E, F, G, and H have been isolated from the sclerotia of the fungus Aspergillus carbonarius. The carbonarins are effective for controlling Coleopteran and Lepidopteran insects. The carbonarins have the structure: ##STR1## wherein: R.sub.1 is a hydrogen atom or a hydroxy group; R.sub.2 is a hydrogen atom or a methoxy group; R.sub.3 is a hydrogen atom or a naphthopyrone group; and X is an oxygen atom or an NH group.
    Type: Grant
    Filed: July 29, 1994
    Date of Patent: May 21, 1996
    Assignees: The United States of America as represented by the Secretary of Agriculture, University of Iowa Research Foundation and Biotechnology Research and Development Corp.
    Inventors: Ali A. Alfatafta, Patrick F. Dowd, James B. Gloer, Donald T. Wicklow
  • Patent number: 5519146
    Abstract: A process for crystallizing N.sup.2 -((S)-1-ethoxycarbonyl-3-phenylpropyl)-N.sup.6 -trifluoroacetyl-L-lysyl-L-proline using one or a mixture of at least two kinds of compound having the general formula: CR.sup.1 R.sup.2 R.sup.3 R.sup.4 as a crystallizing solvent, optionally with an auxiliary solvent which controls crystallization condition.
    Type: Grant
    Filed: August 26, 1994
    Date of Patent: May 21, 1996
    Assignee: Kanegafuchi Kagaku Kogyo Kabushiki Kaisha
    Inventors: Yasuyoshi Ueda, Hajime Manabe
  • Patent number: 5516928
    Abstract: A process for the preparation of 3-cyano-3,5,5-trimethylcyclohexanone by the reaction of isophorone with hydrogen cyanide in the presence of quaternary ammonium catalysts at temperatures ranging from 80.degree. to 180.degree. C. and pressures ranging from 0.5 to 20 bar, in which the ammonium catalysts used are salts of the general formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 denote C.sub.1 -C.sub.18 alkyl, C.sub.5 -C.sub.8 cycloalkyl, aryl, C.sub.7 -C.sub.18 aralkyl or C.sub.2 -C.sub.18 hydroxyalkyl andX denotes HCO.sub.3 or ##STR2## with the proviso that R.sup.4 stands for C.sub.1 -C.sub.
    Type: Grant
    Filed: February 28, 1995
    Date of Patent: May 14, 1996
    Assignee: BASF Aktiengesellschaft
    Inventors: Klaus Mundinger, Gerhard Laqua, Tom Witzel, Franz Merger
  • Patent number: 5516788
    Abstract: The invention concerns compounds and their enantiomers of the formula IA or IB ##STR1## and pharmaceutically acceptable salts thereof wherein each of R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11 and R.sup.12 is independently selected from hydrogen or an alkyl group containing 1-6 carbon atoms and R.sup.5 is an alkoxy group containing 1-6 carbon atoms. The invention further concerns pharmaceutical compositions comprising the active compounds and methods employing the compounds for the treatment of conditions associated with free radical formation.
    Type: Grant
    Filed: January 6, 1995
    Date of Patent: May 14, 1996
    Assignees: University of Bath, University of Cincinnati, School of Medicine
    Inventors: Malcolm Sainsbury, Howard G. Shertzer
  • Patent number: 5514830
    Abstract: The present invention provides a process for producing a nitrile represented by the general formula (1):RC.ident.N (1)wherein R is alkyl, alkenyl, aralkyl or aryl, each may have a substituent, characterized by heating an aldoxime represented by the general formula (2):RCH.dbd.NOH (2)wherein R is as defined above, in the presence of one or more catalysts selected from hydroxides of alkali metals, alcoholates of alkali metals, hydroxides of alkaline earth metals and alcoholates of alkaline earth metals, and distilling off water formed in the course of the reaction from the reaction system. The process according to the present invention can produce a nitrile which is useful as a perfume or as a starting material for the organic synthesis of perfumes, medicines and so on in high yields and advantageously from the viewpoint of production economy.
    Type: Grant
    Filed: April 21, 1995
    Date of Patent: May 7, 1996
    Assignee: Kao Corporation
    Inventors: Masayuki Oku, Yoshiaki Fujikura
  • Patent number: 5514711
    Abstract: Styrene derivatives of the following general formula (I): ##STR1## or pharmaceutically acceptable salts thereof. A pharmaceutical composition useful as anticancer agent, which comprises the above compound as an essential component, is also provided.
    Type: Grant
    Filed: January 5, 1995
    Date of Patent: May 7, 1996
    Assignee: Mitsubishi Chemical Corporation
    Inventors: Yasunori Kitano, Hisao Takayanagi, Koichi Sugawara, Hiroto Hara, Hideo Nakamura, Toshiko Oshino
  • Patent number: 5514825
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or alkyl of 1 to 10 carbons; R.sub.2 and R.sub.3 are hydrogen, or alkyl of 1 to 6 carbons and the substituted ethynyl group occupies either the 2 or the 3 position of the tetrahydronaphthalene nucleus; m is an integer having the value of 0-3; o is an integer having the value 0-4; Y is a phenyl group, or heteroaryl selected from a group consisting of pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl, oxazolyl, and imidazolyl, said groups being optionally substituted with one or two R.sub.2 groups; A is (CH.sub.2).sub.n where n is 0-5, lower branched chain alkyl having 3-6 carbons, cycloalkyl having 3-6 carbons, alkenyl having 2-6 carbons and 1 or 2 double bonds, alkynyl having 2-6 carbons and 1 or 2 triple bonds; B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.13 O, --COR.sub.7, CR.sub.
    Type: Grant
    Filed: December 29, 1994
    Date of Patent: May 7, 1996
    Assignee: Allergan, Inc.
    Inventors: Vidyasagar Vuligonda, Min Teng, Richard L. Beard, Alan T. Johnson, Tien T. Duong, Yuan Lin, Roshantha A. Chandraratna
  • Patent number: 5512696
    Abstract: A process for hydrocyanation of an aliphatic monoethylenically unsaturated compound, in which the ethylenic double bond is not conjugated to any other unsaturated group in the molecule, or a monoethylenically unsaturated compound in which the ethylenic double bond is conjugated to an ester group, which process uses a catalyst composition comprising a zero-valent and a multidentate phosphite ligand in the presence of a Lewis acid promoter.
    Type: Grant
    Filed: July 21, 1995
    Date of Patent: April 30, 1996
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Kristina A. Kreutzer, Wilson Tam
  • Patent number: 5512680
    Abstract: A process is described for the preparation of (+)-2-(3,4-dichlorophenyl)-4-hydroxybutylamine (I) by reaction of 3,4-dichlorophenylacetonitrile (II) with an alkali metal halogenoacetate, treatment of the 3-cyano-3-(3,4-dichlorophenyl)propionic acid (III) with D-(-)-N-methylglucamine, with second-order asymmetric conversion, hydrolysis of the D-(-)-N-methylglucamine salt of (-)-3-cyano-3-(3,4-dichlorophenyl)propionic acid and enantioconservative reduction of the resulting levorotatory cyanoacid with a borane.
    Type: Grant
    Filed: August 24, 1994
    Date of Patent: April 30, 1996
    Assignee: Sanofi
    Inventors: Marcel Descamps, Joel Radisson, Gilles Anne-Archard
  • Patent number: RE35230
    Abstract: A method of enantiomerically enriching chiral cyanohydrins is disclosed that involves selective cleavage of the unwanted enantiomer into its cleavage products HCN and the corresponding aldehyde or ketone by use of an enantioselective dehydrocyanation catalyst, coupled with simultaneous removal of at least one of the dehydrocyanation products.
    Type: Grant
    Filed: February 7, 1994
    Date of Patent: May 7, 1996
    Assignee: Bend Research, Inc.
    Inventor: Paul van Eikeren