Patents Examined by D. Margaret M. Mach
  • Patent number: 6124344
    Abstract: The invention relates to the use of derivatives of F-type prostaglandins as ocular hypotensives. The compounds used in accordance with the invention are represented by the following formula I: ##STR1## wherein wavy line attachments indicate either the alpha (.alpha.) or beta (.beta.) configuration; hatched segments indicate a configuration; the solid triangle is used to indicate .beta. configuration; dashed bonds represent a double bond, or a single bond; R is a substituted heteroaryl radical having at least two pendant substituents selected from the group consisting of C.sub.1 to C.sub.6 alkyl; halogen; trifluoromethyl; COR.sup.1 ; COCF.sub.3 ; SO.sub.2 NR.sup.1 ; NO.sub.2 and CN or at least one cyano group; R.sup.1 is hydrogen or a lower alkyl radical having up to six carbon atoms, X is selected from the group consisting of --OR.sup.1 and --N(R.sup.1).sub.2 ; Y is .dbd.
    Type: Grant
    Filed: November 19, 1997
    Date of Patent: September 26, 2000
    Assignee: Allergan Sales, Inc.
    Inventor: Robert M. Burk
  • Patent number: 6103904
    Abstract: The present invention relates to an improved Skraup reaction process wherein pressure is applied during the reaction and the number of equivalents of sulfuric acid utilized is reduced.
    Type: Grant
    Filed: July 17, 1997
    Date of Patent: August 15, 2000
    Assignee: BASF Corporation
    Inventor: Ronald R. Eva
  • Patent number: 6048897
    Abstract: Compounds having the active site of natural lipoxins, but a longer tissue half-life are disclosed. In particular, 15-epi-lipoxins and their use in ameliorating undesired cell proliferation, which characterizes diseases such as cancer, are also disclosed.
    Type: Grant
    Filed: September 13, 1996
    Date of Patent: April 11, 2000
    Assignee: Brigham and Women's Hospital
    Inventor: Charles N. Serhan
  • Patent number: 6037350
    Abstract: This invention comprises the novel compounds of formula (I) ##STR1## wherein the dotted line represents an optional bond; X is oxygen or sulfur; R.sup.1 is hydrogen, C.sub.1-12 alkyl, Ar.sup.1, Ar.sup.2 C.sub.1-6 alkyl, quinolinylC.sub.1-6 alkyl, pyridylC.sub.1-6 alkyl, hydroxyC.sub.1-6 alkyl, C.sub.1-6 alkyloxyC.sub.1-6 alkyl, mono- or di(C.sub.1-6 alkyl)aminoC.sub.1-6 alkyl, aminoC.sub.1-6 alkyl, or a radical of formula -Alk.sup.1 -C(.dbd.O)--R.sup.9, -Alk.sup.1 -S(O)--R.sup.9 or -Alk.sup.1 -S(O).sub.2 --R.sup.9 ; R.sup.2, R.sup.3 and R.sup.16 each independently are hydrogen, hydroxy, halo, cyano, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, hydroxyC.sub.1-6 alkyloxy, C.sub.1-6 alkyloxyC.sub.1-6 alkyloxy, aminoC.sub.1-6 alkyloxy, mono- or di(C.sub.1-6 alkyl)aminoC.sub.1-6 alkyloxy, Ar.sup.1, Ar.sup.2 C.sub.1-6 alkyl, Ar.sup.2 oxy, Ar.sup.2 C.sub.1-6 alkyloxy, hydroxycarbonyl, C.sub.1-6 alkyloxycarbonyl, trihalomethyl, trihalomethoxy, C.sub.2-6 alkenyl; R.sup.4 and R.sup.5 each independently are hydrogen, halo, Ar.
    Type: Grant
    Filed: May 26, 1998
    Date of Patent: March 14, 2000
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Marc Gaston Venet, Patrick Rene Angibaud, Philippe Muller, Gerard Charles Sanz
  • Patent number: 6034129
    Abstract: A method for treating a microbial infection in a mammal, such as a human, comprising treating the mammal with a therapeutically effective amount of a polymer comprising an amino group or an ammonium group attached to the polymer backbone via an aliphatic spacer group. The polymer can be a homopolymer or a copolymer. In one embodiment, the polymer is a copolymer comprising a monomer having a pendant ammonium group and a hydrophobic monomer.
    Type: Grant
    Filed: June 24, 1996
    Date of Patent: March 7, 2000
    Assignee: GelTex Pharmaceuticals, Inc.
    Inventors: W. Harry Mandeville, III, Thomas X. Neenan, Stephen Randall Holmes-Farley
  • Patent number: 6020500
    Abstract: Compositions comprising hydroxy-substituted monolactones, a process for reacting olefinic compounds with certain carboxylic reactants and products prepared by the process. The compositions containing the hydroxy-substituted lactones and the products of the process are useful as intermediates for the preparation of additives for lubricants and fuels.
    Type: Grant
    Filed: August 22, 1995
    Date of Patent: February 1, 2000
    Assignee: The Lubrizol Corporation
    Inventors: Mark R. Baker, Paul E. Adams, Jeffry G. Dietz
  • Patent number: 6017906
    Abstract: The present invention relates to methods of preventing or treating an infection or disease caused by an infectious agent. The present invention also relates to the augmentation of the efficacy of existing anti-infective agents by the co-administration of the compounds described herein.
    Type: Grant
    Filed: May 5, 1998
    Date of Patent: January 25, 2000
    Assignee: Intercardia, Inc.
    Inventors: Clifford S. Mintz, Natan A. Kogan, Ramesh Kakarla, Helena R. Axelrod, Michael J. Sofia
  • Patent number: 6004958
    Abstract: The present invention is based on the discovery of a metabolic pathway in which a specific kinase converts fructose-lysine into fructose-lysine-3-phosphate in an ATP dependent reaction. Fructose-lysine-3-phosphate (FL3P) is then broken down to form free lysine, inorganic phosphate and 3-deoxyglucosone (3DG), the latter being a reactive protein modifying agent. 3DG can be detoxified by reduction to 3-deoxyfructose (3DF), or it can react with endogenous proteins to form advanced glycation end-product modified proteins (AGE-proteins), which are believed to be a cause of diabetic complications. Disclosed is a class of compounds which inhibit the action of FL3P kinase in the above-mentioned pathway.
    Type: Grant
    Filed: February 5, 1997
    Date of Patent: December 21, 1999
    Assignee: Fox Chase Cancer Center
    Inventors: Truman R. Brown, Francis Kappler, Benjamin Szwergold, Sundeep Lal, Bangying Su
  • Patent number: 6005113
    Abstract: The invention relates to fluorescent dyes that are substituted or unsubstituted derivatives of 1-(isoindolyl)methylene-isoindole that are bound through both isoindole nitrogens to a boron difluoride moiety, forming a fluorescent dibenzopyrrometheneboron difluoride compound ##STR1## that is further substituted by bathochromic substituents that are aryl or heteroaryl moieties further substituted by an additional aryl or heteroaryl, that is itself optionally further substituted by an additional aryl or heteroaryl. These aryl and heteroaryl groups are separated by a covalent bond, or by an ethenyl, butadienyl or hexatrienyl linkage. The dyes of the invention are particularly useful as labels for carriers, particularly polymeric microparticles. The resulting microparticles have a long-wavelength fluorescence emission, and possess utility for tracing flow in biological systems, particularly in tracing blood flow.
    Type: Grant
    Filed: May 14, 1997
    Date of Patent: December 21, 1999
    Assignee: Molecular Probes, Inc.
    Inventors: Yexin Wu, Dieter H. Klaubert, Hee Chol Kang, Yu-Zhong Zhang
  • Patent number: 6005111
    Abstract: A method for forming a color image comprises the step of developing an image-wise exposed silver halide color photographic photosensitive material at the presence of a 6-aminotetrahydroquinoline color developing agent which is the following compound or its analoge. According to this method, the rapid process can be attained and an image of a low fog density can be obtained.
    Type: Grant
    Filed: January 30, 1998
    Date of Patent: December 21, 1999
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Masato Taniguchi, Kiyoshi Morimoto, Keizo Kimura, Kazumi Nii, Shigeo Hirano
  • Patent number: 6001843
    Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating COX-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. The invention also encompasses certain pharmaceutical compositions for treatment of COX-2 mediated diseases comprising compounds of Formula I.
    Type: Grant
    Filed: October 29, 1998
    Date of Patent: December 14, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Daniel Dube, Rejean Fortin, Richard Friesen, Zhaoyin Wang, Jacques Yves Gauthier
  • Patent number: 6002008
    Abstract: This invention provides compounds having the formula: ##STR1## wherein: X is cycloalkyl which may be optionally substituted; or is a pyridinyl, pyrimidinyl, or phenyl ring; wherein the pyridinyl, pyrimidinyl, or phenyl ring may be optionally substituted;n is 0-1;Y is --NH--, --O--, --S--, or --NR--;R is alkyl of 1-6 carbon atoms;R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are each, independently, hydrogen, halogen, alkyl, alkenyl, alkynyl, alkenyloxy, alkynyloxy, hydroxymethyl, halomethyl, alkanoyloxy, alkenoyloxy, alkynoyloxy, alkanoyloxymethyl, alkenoyloxymethyl, alkynoyloxymethyl, alkoxymethyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkylsulfonamido, alkenylsulfonamido, alkynylsulfonamido, hydroxy, trifluoromethyl, cyano, nitro, carboxy, carboalkoxy, carboalkyl, phenoxy, phenyl, thiophenoxy, benzyl, amino, hydroxyamino, alkoxyamino, alkylamino, dialkylamino, aminoalkyl, N-alkylaminoalkyl, N,N-dialkylaminoalkyl, phenylamino, benzylamino, ##STR2## R.sub.
    Type: Grant
    Filed: March 27, 1998
    Date of Patent: December 14, 1999
    Assignee: American Cyanamid Company
    Inventors: Allan Wissner, Bernard D. Johnson, Marvin F. Reich, Middleton B. Floyd, Jr., Douglas B. Kitchen, Hwei-Ru Tsou
  • Patent number: 5994545
    Abstract: The present invention provides a process for producing decahydro(4as, 8aS)isoquinoline-3(S)-carboxamides which are useful as intermediates of Saquinavir (EP 432694). Saquinavir is an anti-AIDS agent. The comprises reacting tetrahydroisoquinoline-3(S)-carboxylic acid with at least one of phosgene, phosgene dimer and triphosgene to form N-carboxy anhydride (NCA), then reacting NCA with an amine to produce a tetrahydroisoquinoline-3(S)-carboxamide derivative, and further reducing this derivative in the presence of a metal catalyst.
    Type: Grant
    Filed: February 3, 1998
    Date of Patent: November 30, 1999
    Assignee: Ajinomoto Co., Inc.
    Inventors: Takahiro Sato, Kunisuke Izawa
  • Patent number: 5990122
    Abstract: The invention relates to new quinolone- and naphthyridonecarboxylic acid derivatives which are substituted in the 7-position by a tricyclic amine radical, their salts, processes for their preparation and antibacterial compositions comprising these compounds.
    Type: Grant
    Filed: January 7, 1998
    Date of Patent: November 23, 1999
    Assignee: Bayer Aktiengesellschaft
    Inventors: Uwe Petersen, Thomas Schenke, Thomas Jaetsch, Stephan Bartel, Klaus Dieter Bremm, Rainer Endermann, Karl Georg Metzger
  • Patent number: 5985789
    Abstract: Improved hydrogenation catalysts consisting essentially of reduced or at least partially reduced ruthenium and tin on a refractory oxide support which is insoluble in aqueous acid. Such catalysts are very durable and exhibit high conversion rates in aqueous acidic solution hydrogenation of hydrogenatable precursors (e.g. maleic acid, succinic acid, gamma-butyrolactone etc.) and high selectivity for their conversion to 1,4-butanediol and gamma-butyrolactone and their mixtures.
    Type: Grant
    Filed: March 27, 1997
    Date of Patent: November 16, 1999
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Patricia Ann Tooley, Jesse Raymond Black
  • Patent number: 5985887
    Abstract: Compounds of formula I ##STR1## wherein X.sub.1 and X.sub.2 are C.dbd.O, C.dbd.NH or CH.sub.2, X.sub.3 is CH.sub.2, CO, CHOH, ##STR2## wherein n=2 or, 3 or C.dbd.N(R.sub.9) wherein R.sub.9 is hydroxy or amino-aryl, and each of R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are hydrogen, halogen or an organic residue, are useful in the treatment of amyloidosis. A process for their preparation and pharmaceutical compositions containing them are also described.
    Type: Grant
    Filed: February 9, 1998
    Date of Patent: November 16, 1999
    Assignee: Pharmacia & UpJohn S.p.A.
    Inventors: Michele Caruso, Daniela Faiardi, Tiziano Bandiera, Jacqueline Lansen, Antonino Suarato
  • Patent number: 5981544
    Abstract: Invention concerning the therapeutic use of tetracyclic derivatives and their pharmaceutically acceptable salts having the following general formula: ##STR1## in which, independently of the other: X is a carbon or nitrogen atom,T is a carbon or nitrogen atom,L is an oxygen atom or ketone functional protective group,R.sub.1 is an atom of hydrogen, an atom of halogen, or a C.sub.1 to C.sub.5 alkyl radical,R.sub.2 is a hydrogen atom, a halogen atom, a nitro radical, or a C.sub.1 to C.sub.5 alkyl radical,n and m are equal to 0 or to 1, but not independently of the other, so that if n is equal to 1, then m is equal to 0, and if n is equal to 0, then m is equal to 1.
    Type: Grant
    Filed: September 21, 1998
    Date of Patent: November 9, 1999
    Assignee: Laboratoire Innothera
    Inventors: Odile Boutherin-Falson, Stephanie Desquand-Billiald, Anita Favrou, Michel Finet, Olivier Tembo, Jean-Luc Torregrosa, Sylvie Yannic-Arnoult, Cecile Joubert
  • Patent number: 5977125
    Abstract: Compounds of the formula ##STR1## and compounds of the formula ##STR2## or their salts have the potent ability to bind to retinoic acid receptors thus useful in treating psoriasis and rheumatoid arthritis.
    Type: Grant
    Filed: May 6, 1997
    Date of Patent: November 2, 1999
    Assignee: Eisai Co., Ltd.
    Inventors: Shigeki Hibi, Kouichi Kikuchi, Hiroyuki Yoshimura, Mitsuo Nagai, Katsuya Tagami, Shinya Abe, Ieharu Hishinuma, Junichi Nagakawa, Norimasa Miyamoto, Takayuki Hida, Aichi Ogasawara, Seiko Higashi, Kenji Tai, Takashi Yamanaka, Makoto Asada
  • Patent number: 5977359
    Abstract: The invention relates to compounds of the formula ##STR1## in which: A is a divalent radical selected from:A.sub.1) --O--CO--A.sub.2) --CH.sub.2 --O--CO--A.sub.3) --O--CH.sub.2 --CO--A.sub.4) --O--CH.sub.2 --CH.sub.2 --A.sub.5) --N(R.sub.1)--CO--A.sub.6) --N(R.sub.1)--CO--CO--A.sub.7) --N(R.sub.1)--CH.sub.2 --CH.sub.2 --A.sub.8) --O--CH.sub.2 --in which:R.sub.1 is a hydrogen or a (C.sub.1 -C.sub.4)-alkyl; andAm is a nitrogen-containing heterocycle.
    Type: Grant
    Filed: October 20, 1998
    Date of Patent: November 2, 1999
    Assignee: Sanofi
    Inventors: Xavier Emonds-Alt, Isabelle Grossriether, Patrick Gueule, Vincenzo Proietto, Didier Van Broeck
  • Patent number: 5972976
    Abstract: The invention relates to an aminostilbazole derivative of the following formula or a hydrate thereof, and a salt thereof. ##STR1## wherein R.sup.1 and R.sup.2 each represents hydrogen etc.; R.sup.3, R.sup.4, R.sup.13, and R.sup.14 each represents hydrogen, C.sub.1-3 acyl, halogen, hydroxy etc.; R.sup.5 represents hydrogen or hydroxy-substituted C.sub.1-3 alkyl etc.; R.sup.6 represents benzenesulfonyl substituted by C.sub.1-3 alkoxy etc.; ring Y represents phenyl etc.; ring Z represents 4-pyridyl, its oxide etc. The compound is useful or the treatment of various malignant tumors.
    Type: Grant
    Filed: October 2, 1996
    Date of Patent: October 26, 1999
    Assignee: Nippon Shinyaku Company, Limited
    Inventors: Hiroyoshi Hidaka, Akira Matsuura, Masato Matsuda