Patents Represented by Attorney George M. Gould
  • Patent number: 5482718
    Abstract: A novel delivery system for targeting drugs to the colon is disclosed. The delivery system is a tablet comprised of three parts: (1) an enteric coating to prevent penetration of gastric fluid into the delivery system, thereby preventing any drug release in the stomach; (2) an erodible polymer layer which is exposed and gradually erodes during transit through the upper intestinal tract, and (3) a core, which is a conventional tablet or beadlet containing an active ingredient(s), which readily disintegrates and subsequently releases the drug to the target site, the colon, after erosion of the erodible polymer layer. The erodible polymer layer prevents drug release in the upper portion of the intestinal tract for 4-6 hours after gastric emptying, representing the amount of time needed for the delivery system to reach the colon.
    Type: Grant
    Filed: March 23, 1994
    Date of Patent: January 9, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Navnit H. Shah, Wantanee Phuapradit, Aruna Railkar
  • Patent number: 5482866
    Abstract: The present invention provides novel reagent compositions incorporating chlorophosphonazo III and a chelating agent and methods utilizing such compositions for the determination of magnesium and magnesium concurrently with calcium in an analytical sample as well as diagnostic test kits for such determinations.
    Type: Grant
    Filed: July 28, 1994
    Date of Patent: January 9, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventors: James B. Denton, Diane J. Dixon, Richard A. Kaufman
  • Patent number: 5482863
    Abstract: An analytical device incorporating a system for suspending particles includes a conveying device for positioning a pipetting needle at a distance from the central longitudinal axis of the reaction vessel. Particles are suspended by delivering amounts of liquid reagent to two different positions at a predetermined distance from the central longitudinal axis of a reaction vessel, such delivery generates a flow in the reaction vessel which suspends particles exclusively by injection of liquid, thus avoiding the need for subsequent shaking.
    Type: Grant
    Filed: September 7, 1994
    Date of Patent: January 9, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Rolf Knobel
  • Patent number: 5482864
    Abstract: An analytical device incorporating a system for suspending particles includes a conveying device for positioning a pipetting needle at a distance from the central longitudinal axis of the reaction vessel. Particles are suspended by delivering amounts of liquid reagent to two different positions at a predetermined distance from the central longitudinal axis of a reaction vessel, such delivery generates a flow in the reaction vessel which suspends particles exclusively by injection of liquid, thus avoiding the need for subsequent shaking.
    Type: Grant
    Filed: April 24, 1995
    Date of Patent: January 9, 1996
    Assignee: Hoffman-La Roche Inc.
    Inventor: Rolf Knobel
  • Patent number: 5481001
    Abstract: Light screening compositions which contain a compound of the formula ##STR1## wherein R.sup.1 represents H, C.sub.1-19 -alkyl, C.sub.2-29 -alkenyl, C.sub.2-29 -alkynyl, optionally lower-alkyl or oxy-lower alkyl substituted phenyl,R.sup.2 represents H, C.sub.1-29 -alkyl, C.sub.2-29 -alkenyl, C.sub.2-29 -alkynyl, optionally lower-alkyl or oxy-lower alkyl substituted phenyl,R.sup.3 represents H, C.sub.1-19 -alkyl, C.sub.1-19 -hydroxyalkyl, C.sub.1-19 -polyhydroxyalkyl, C.sub.2-29 -alkenyl, C.sub.2-29 -alkynyl, optionally lower-alkyl or oxy-lower alkyl substituted phenyl or optionally lower-alkyl or oxy-lower alkyl substituted pyridyl, a polyether residue, a phenylsulphonic acid residue andR.sup.2 and R.sup.3 together with the N atom can also form a ring.
    Type: Grant
    Filed: December 22, 1994
    Date of Patent: January 2, 1996
    Assignee: Givaudan-Roure Corporation
    Inventor: Ulrich Huber
  • Patent number: 5481008
    Abstract: A catalytic process for the manufacture of optically active compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are alkyl, which is optionally interrupted by an O atom in a position other than the .alpha.-or .beta.-position, or optionally substituted benzyl,R.sup.3 is hydrogen, lower alkyl, optionally substituted benzyl, --CO--R.sup.4, --COOR.sup.4 or --CONR.sub.2.sup.4, andR.sup.4 is lower alkyl or aryl,comprising asymmetrically hydrogenating a compound of the formula ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 have the above significance, in the presence of a complex of an optically active, preferably atropisomeric, diphospine ligand with a metal of Group VIII.
    Type: Grant
    Filed: August 31, 1994
    Date of Patent: January 2, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Emil A. Broger, Martin Karpf, Ulrich Zutter
  • Patent number: 5479260
    Abstract: The optical process for analyzing substances is based on the measurement of the propagation properties of optical surface waves on sensor surfaces. In a wave guide layer structure in contact with a sample, guided light waves are decoupled with a grating coupler. The decoupling region of the grating coupler is imaged onto a position resolving detector so that the plane of the wave guide layer structure forms the object plane and the detection plane lies in the image plane of the optical imaging. The light distribution of the decoupled wave field in the image plane is measured with the detector and used to determine the analytical quantity to be measured. The device for carrying out the process consists of a suitable wave guide sensor with grating coupler, an imaging lens system and an optical detector (10).
    Type: Grant
    Filed: April 24, 1995
    Date of Patent: December 26, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Christof Fattinger
  • Patent number: 5478569
    Abstract: Stable, cold water-dispersible, liquid or pulverous compositions of fat-soluble substances which contain fish gelatin as the protective colloid and a method of making same are described.
    Type: Grant
    Filed: November 28, 1994
    Date of Patent: December 26, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Kurt Berneis, Peter Schuler
  • Patent number: 5478497
    Abstract: Compounds of the formula ##STR1## wherein rings A, B and C, Z.sup.1, Z.sup.2, Z.sup.3, R.sup.1, R.sup.2 and R.sup.3 are defined in the specification, their manufacture, liquid crystalline mixtures which contain such compounds and the use of these compounds for electro-optical purposes.
    Type: Grant
    Filed: February 1, 1995
    Date of Patent: December 26, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Richard Buchecker, Martin Schadt, Alois Villiger
  • Patent number: 5476875
    Abstract: Catechol derivatives of the formula ##STR1## wherein Ra, Rb and Rc have the significance given herein, the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adenosylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuronal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure.
    Type: Grant
    Filed: October 21, 1994
    Date of Patent: December 19, 1995
    Assignee: Hoffman-La Roche Inc.
    Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mose Da Prada, Gerhard Zurcher
  • Patent number: 5476774
    Abstract: The present invention provides a method for determining the amount of a target acid segment in a sample by polymerase chain reaction. The method involves the simultaneous amplification or the target nucleic acid segment and an internal standard nucleic acid segment. The amount of amplified DNA from each segment is determined and compared to standard curves to determine the amount of the target nucleic acid segment present in the sample prior to amplification. The method is especially preferred for determining the quantity of a specific mRNA species in a biological sample. Additionally, an internal standard is provided useful for quantitation of multiple mRNA species.
    Type: Grant
    Filed: March 9, 1993
    Date of Patent: December 19, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alice M. Wang, Michael V. Doyle, David F. Mark
  • Patent number: 5476932
    Abstract: A process for preparing N4-acyl-5'-deoxy-5-fluorocytidine derivatives of formula III: ##STR1## by selective deacylation, wherein R is alkyl, cycloalkyl, alkenyl, aralkyl or aryl,which comprises reacting a compound of formula II, ##STR2## wherein R is as defined above, with a base in an aqueous or inert organic solvent.
    Type: Grant
    Filed: August 26, 1994
    Date of Patent: December 19, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Herbert R. Brinkman, Panayiotis Kalaritis, John F. Morrissey
  • Patent number: 5474744
    Abstract: An automatic pipetting device comprising only one pipetting needle having a tip end and an open end. The device comprises a metering syringe having an outlet. The device also comprises a mechanism for cleaning the pipetting needle with a cleaning fluid when the pipetting needle is positioned in a cleaning position. The mechanism comprises a plunger pump, a second tube having a first end and a second end, a first valve, a second valve, and a third tube having a first end and a second end, the second end of the tubing immersed in a cleaning fluid. The second end of the first tube is in fluid communication with both the outlet of the metering syringe and the first valve. The first end of the second tube is in fluid communication with the first valve. The second end of the second tube is in fluid communication with both the plunger pump and the second valve. The first end of the third tube is in fluid communication with the second valve.
    Type: Grant
    Filed: October 21, 1994
    Date of Patent: December 12, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Erich Lerch
  • Patent number: 5472949
    Abstract: The invention relates to N.sup.4 -(substituted-oxycarbonyl)-5'-deoxy-5-fluorocytidine derivatives which are useful as an agent for treating tumors, pharmaceutical compositions including the same, a method of treating tumors and a method of preparing N.sup.4 -(substituted-oxycarbonyl)-5'-deoxy-5-fluorocytidine derivatives for treating tumors.Compounds of formula (I), ##STR1## wherein R.sup.1 is a saturated or unsaturated, straight or branched hydrocarbon radical wherein the number of carbon atoms in the longest straight chain of this hydrocarbon radical ranges from three to seven, or is a radical of the formula --(CH.sub.2)n--.sup.Y wherein Y is a cyclohexyl radical, a C.sub.1 -C.sub.4 alkoxy radical or a phenyl radical and wherein when Y is a cyclohexyl radical n is an integer from 0 to 4, and when Y is C.sub.1 -C.sub.4 alkoxy radical or a phenyl radical n is an integer from 2 to 4, and R.sup.2 is a hydrogen atom or a radical easily hydrolyzable under physiological conditions,or a hydrate or solvate thereof.
    Type: Grant
    Filed: December 14, 1993
    Date of Patent: December 5, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Motohiro Arasaki, Hideo Ishitsuka, Isami Kuruma, Masanori Miwa, Chikako Murasaki, Nobuo Shimma, Isao Umeda
  • Patent number: 5470991
    Abstract: The invention is concerned with a process for the manufacture of substituted furans which are, in particular, flavorants; thereby 4-hydroxy-2-yn-1-ones or acetals or ketals thereof are cyclized with nucleophilic S-compounds to 3-S-furans, whereby this 3-S atom can be optionally substituted, and the acetylene derivatives, the 4-hydroxy-2-yn-1-ones, can be optionally 1- and/or 4-alkyl or alkenyl substituted.
    Type: Grant
    Filed: June 3, 1993
    Date of Patent: November 28, 1995
    Assignee: Givaudan-Roure Corporation
    Inventor: Ulrich Huber
  • Patent number: 5470861
    Abstract: The use of the compound 2-(6-cyano-3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-4-yl)pyridine-1-oxide represented by the formula ##STR1## as well as pharmaceutically acceptable salts, as topical agents to promote hair growth is disclosed.
    Type: Grant
    Filed: August 4, 1994
    Date of Patent: November 28, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Charles S. Harmon
  • Patent number: 5468613
    Abstract: Single or multiple nucleotide variations in nucleic acid sequence can be detected in nucleic acids by a process whereby the sample suspected of containing the relevant nucleic acid is repeatedly treated with primers, nucleotide triphosphates, and an agent for polymerization of the triphosphates and then denatured, in a process which amplifies the sequence containing the nucleotide variation if it is present. In one embodiment, the sample is spotted on a membrane and treated with a labeled sequence-specific oligonucleotide probe. Hybridization of the probe to the sample is detected by the label on the probe.
    Type: Grant
    Filed: March 9, 1990
    Date of Patent: November 21, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Henry A. Erlich, Glenn Horn, Randall K. Saiki, Kary B. Mullis
  • Patent number: 5466708
    Abstract: Novel compounds of the formula ##STR1## wherein Q, R.sup.1 and R.sup.2 are described herein, are disclosed along with pharmaceutical compositions, methods of use, and process for producing compounds of formula I which starts from the corresponding .beta.-hydroxycarboxylic acids.
    Type: Grant
    Filed: September 19, 1994
    Date of Patent: November 14, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Romano Derungs, Hans P. Marki, Henri Stalder, Andre Szente
  • Patent number: 5466591
    Abstract: The present invention relates to thermostable DNA polymerases which have been mutated such that a lesser amount of 5' to 3' exonuclease activity is exhibited from that which is exhibited by the native enzyme.
    Type: Grant
    Filed: February 23, 1993
    Date of Patent: November 14, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Richard D. Abramson, David H. Gelfand
  • Patent number: 5464617
    Abstract: Compounds of the formula ##STR1## where Z, A, and R are as disclosed herein and pharmaceutically compatible, readily hydrolyzable esters and salts of these compounds are disclosed.The compounds have .beta.-lactamase inhibiting properties and are useful in the control of .beta.-lactamase-forming pathogens in combination with .beta.-lactam antibiotics. They also exhibit antibacterial activity of their own and can accordingly be used themselves in the control or treatment of infectious diseases.
    Type: Grant
    Filed: March 3, 1995
    Date of Patent: November 7, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Markus Bohringer, Christian Hubschwerlen, Philippe Pflieger, Jean-Luc Specklin