Patents Represented by Attorney George M. Gould
  • Patent number: 5502236
    Abstract: Novel processes and intermediates useful for the manufacture of the Wittig ester salts are disclosed. The Wittig ester salts are known as important CS building blocks for the manufacture of various polyenecarboxylic acid esters in the field of carotenoid chemistry.
    Type: Grant
    Filed: March 17, 1995
    Date of Patent: March 26, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bruno Burdet, August Ru/ ttimann, Jean-Marie Santer, Theodor Siegfried
  • Patent number: 5500752
    Abstract: A liquid crystal cell comprising a cholesteric liquid crystal (3) between parallel plates (1, 2) as used e.g. for optical filters. The previously unavoidable interference through faulty disinclination is eliminated in that the cholesteric liquid crystal is mixed with a nematic or smectic liquid crystal material having negative dielectric anisotropy and the cell is subjected to an electric field directed at right angles to the plates.
    Type: Grant
    Filed: January 17, 1995
    Date of Patent: March 19, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Martin Schadt, Hubert Seiberle
  • Patent number: 5498367
    Abstract: A chiral dopant of the formula ##STR1## wherein ring A is 1,4-phenylene which is optionally substituted with one or more fluorine atoms, chlorine atoms, bromine atoms, cyano groups, or methyl groups, and in which one or two CH groups can be replaced by nitrogen, or is trans-1,4-cyclohexylene;Z is a single covalent bond, --CH.sub.2 CH.sub.2 --, --CH.sub.2 O-- or --OCH.sub.2 --;X.sup.1,X.sup.2,X.sup.3,X.sup.4 each independently are hydrogen or fluorine;R.sup.1 is hydrogen, is alkyl with 1 to 12 carbon atoms which is optionally substituted with one or more fluorine or chlorine atoms and in which one or two non-adjacent CH.sub.2 groups can be replaced by --O--, is alkenyl with 2 to 12 carbon atoms, which is optionally substituted with one or more fluorine or chlorine atoms and in which one or two non-adjacent CH.sub.2 groups can be replaced by --O--, is a group of the formula ##STR2## and when R.sup.1 is bonded to an aromatic ring, can also be fluorine, chlorine, cyano, CF.sub.3, OCHF.sub.2 or --OCF.sub.3 ;R.sup.
    Type: Grant
    Filed: February 17, 1995
    Date of Patent: March 12, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Richard Buchecker, Guy Marck, Martin Schadt
  • Patent number: 5496519
    Abstract: A processing station for making a fluorescence polarization measurement on a sample in a cell under examination in a device for chemical and biochemical analysis, the analytical device containing a conveyor for conveying cells. In order to make fluorescence polarization measurements outside the conveyor, the processing station is separated from the conveyor and contains a measuring device means for making fluorescence polarization measurements on a sample in a cell, and an automatically controlled change-over and positioning device for removing individual cells from the conveyor, transferring a removed cell to a measuring position in the measuring device, and returning the cell to its original position on the conveyor after the measurement.
    Type: Grant
    Filed: July 21, 1994
    Date of Patent: March 5, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Gottlieb Schacher
  • Patent number: 5494666
    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: June 9, 1995
    Date of Patent: February 27, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Markus Bohringer, Christian Hubschwerlen, Philippe Pflieger, Jean-Luc Specklin
  • Patent number: 5495039
    Abstract: Novel organosiloxane compounds have at least one unit ##STR1## any other units being present in this organosiloxane are ##STR2## wherein R is a C.sub.1-8 alkyl or aryl, R.sup.1 is H or a C.sub.1-5 alkyl, R.sup.2 is H, C.sub.1-5 alkyl or OR.sup.1, R.sup.3 is a C.sub.1-5 alkyl, R" is H, a monovalent C.sub.1-8 hydrocarbon or halogenated hydrocarbon group, a is 0, 1 or 2, b 0, 1, 2 or 3 and n 1 to 6, provided the--C(R.sup.1).dbd.CH--(CR.sub.2.sup.1).sub.n --O--group and the two R.sup.2 groups are linked to the aromatic ring at the para- and meta-positions in relation to the group --CH.dbd.C[C(O)OR.sup.3 ].sub.2.The compounds are useful as UV sunscreens. Compositions containing them are also included.
    Type: Grant
    Filed: September 21, 1994
    Date of Patent: February 27, 1996
    Assignee: Givaudan-Roure Corporation
    Inventors: Georg Frater, Rolf Schwarzenbach, Stephane F. M. Van Oycke
  • Patent number: 5495025
    Abstract: The compound of the formula, ##STR1## wherein R.sup.4 is hydrogen, lower-alkanoyl or benzyloxycarbonyl and R.sup.2 is lower-alkyl or acid-addition salts thereof, useful as intermediates in the production of beta-aminoalcohols.
    Type: Grant
    Filed: March 9, 1995
    Date of Patent: February 27, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Hans Hilpert
  • Patent number: 5495048
    Abstract: A method of lowering cholesterol which comprises administering to a host requiring such treatment an effective amount of a compound of the formula ##STR1## wherein one of R.sup.1 and R.sup.2 is C.sub.1-7 -alkyl and the other is C.sub.1-7 -alkyl or C.sub.2-6 -alkenyl-methyl;L is C.sub.1-11 -alkylene or C.sub.2-11 -alkenylene optionally bonded to the phenyl group via an O atom or L is 1,4-phenylene;n is 0 or, when L contains an O atom, n is 0 or 1;Q is C.sub.1-7 -alkyl, C.sub.2-10 -alkenyl or a group of formula ##STR2## wherein R is H, halogen, CF.sub.3, CN or NO.sub.2 ; R.sup.3 and R.sup.4 are H, C.sub.1-4 -alkyl or halogen; andR.sup.5 is H or, when R is H, R.sup.5 is H or halogen;or a pharmaceutically acceptable acid addition salt thereof, as well as certain compounds of formula I, are described.
    Type: Grant
    Filed: June 17, 1994
    Date of Patent: February 27, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Johannes Aebi, Philipe Guerry, Synese Jolidon, Olivier Morand
  • Patent number: 5494928
    Abstract: The invention releates to indole derivatives of the formula ##STR1## wherein R.sup.1 to R.sup.4 are, independently, hydrogen, halogen, lower-alkyl, cycloalkyl or trifluoromethyl, R.sup.5 and R.sup.6 are, independently, hydrogen, halogen, lower-alkyl, cycloalkyl, trifluoromethyl, hydroxy or lower-alkoxy and R.sup.7 is hydrogen or lower-alkyl, andpharmaceutically acceptable acid addition salts thereof.The compounds of formula I bind to serotonin receptors and are therefore useful in the treatment and/or prevention of central nervous system disorders, such as depression.
    Type: Grant
    Filed: October 3, 1994
    Date of Patent: February 27, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Michael Bos
  • Patent number: 5491086
    Abstract: Recombinant DNA sequences encoding the DNA polymerase activity of Pyrodictium species can be used to construct recombinant vectors and transformed host cells for production of the activity. Pyrodictium enzymes for catalyzing 3'.fwdarw.5' exonuclease activity, i.e., proofreading enzymes, are also provided. The Pyrodictium enzymes are useful in DNA amplification procedures and are not irreversibly inactivated by exposure to 100.degree. C. in a polymerase chain reaction.
    Type: Grant
    Filed: May 14, 1993
    Date of Patent: February 13, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventors: David H. Gelfand, Alice M. Wang
  • Patent number: 5491063
    Abstract: The present invention is directed to methods for controlling the light emission of an oligonucleotide labeled with a light-emitting label that are useful in nucleic acid detection assays. A reaction that results in the cleavage of single-stranded oligonucleotide probes labeled with a light-emitting label is carried out in the presence of a DNA binding compound that interacts with the label to modify the light emission of the label. The methods utilize the change in light emission of the labeled probe that results from degradation of the probe. The methods are applicable in general to assays that utilize a reaction that results in cleavage of oligonucleotide probes, and, in particular, to homogeneous amplification/detection assays wherein hybridized probe is cleaved concomitant with palmer extension. A homogeneous amplification/detection assay is provided which allows the simultaneous detection of the accumulation of amplified target and the sequence-specific detection of the target sequence.
    Type: Grant
    Filed: September 1, 1994
    Date of Patent: February 13, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Mary E. Fisher, Robert M. Watson
  • Patent number: 5491225
    Abstract: This invention provides for superior nucleic acid primers for amplification of select target regions of the genome of the genus Legionella. The invention facilitates detection of pathogenic and nonpathogenic forms of this genus. The invention further provides for processes for using the primers in template dependent nucleic acid polymerase extension reactions to amplify select target regions. Kits for the use of these primers are also provided. This invention further provides for methods of controlling the intensity of visual signal for detection of duplex formation in nucleic acid hybridization assays under high stringent conditions. This method involves the blending of different capture probes onto a solid support.
    Type: Grant
    Filed: May 27, 1993
    Date of Patent: February 13, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Teresa K. H. Picone, Theresa M. McCallum, Michael A. Zoccoli
  • Patent number: 5487972
    Abstract: A process of detecting a target nucleic acid using labeled oligonucleotides which uses the 5' to 3' nuclease activity of a nucleic acid polymerase to cleave annealed labeled oligonucleotide from hybridized duplexes and thus releasing labeled oligonucleotide fragments for detection. This process is easily incorporated into a PCR amplification assay.
    Type: Grant
    Filed: January 5, 1993
    Date of Patent: January 30, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventors: David H. Gelfand, Pamela M. Holland, Randall K. Saiki, Robert M. Watson
  • Patent number: 5488115
    Abstract: Novel alcohols of the formula ##STR1## wherein R.sup.a is azido or phthalimido, R.sup.4 is alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, R.sup.7 and R.sup.8 together are a trimethylene or tetramethylene group which is optionally substituted by hydroxy, alkoxycarbonylamino or acylamino or in which one --CH.sub.2 -- group is replaced by --NH--, --N(alkoxycarbonyl)--, --N(acyl)-- or --S-- or which carries a fused cycloalkane, aromatic or heteroaromatic ring, and R.sup.9 is alkoxycarbonyl, monoalkylcarbamoyl, monoaralkylcarbamoyl, monoarylcarbamoyl or a group of the formula ##STR2## in which R.sup.10 and R.sup.11 each is alkyl, are described along with a process for their manufacture. These alcohols are useful as intermediates, for example in the manufacture of amino acid derivatives having antiviral activity.
    Type: Grant
    Filed: May 12, 1995
    Date of Patent: January 30, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Kevin E. B. Parkes, Sally Redshaw, Gareth J. Thomas
  • Patent number: 5487817
    Abstract: A novel process for the recovery of tocopherols and sterols from natural, especially vegetable, sources. This process is especially a process for the separation of tocopherols and sterols from deodorizer sludges by distillation of these deodorizer sludges, in that prior to the distillation the sterols present in the deodorizer sludge are esterified with the fatty acids which are also present, the resulting mixture is distilled to obtain residual fatty acids and subsequently to obtain tocopherols, whereby the sterol esters formed in the esterification remain in the residue of this distillation, and then the tocopherols are isolated from the distillate and the sterols, after cleavage of their esters, are isolated from the distillation residue.
    Type: Grant
    Filed: January 21, 1994
    Date of Patent: January 30, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Christian Fizet
  • Patent number: 5488172
    Abstract: Novel chiral phosphorus compounds of the formula ##STR1## wherein R signifies lower alkyl, R.sup.1 signifies phenyl and R.sup.2 and R.sup.3 signify hydrogen or lower alkoxy,which are suitable in the form of complexes with a metal of Group VIII as catalysts for asymmetric hydrogenations and for enantioselective hydrogen displacements in prochiral allylic systems.
    Type: Grant
    Filed: August 23, 1994
    Date of Patent: January 30, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Marco Cereghetti, Joseph Foricher, Bernd Heiser, Rudolf Schmid
  • Patent number: 5486463
    Abstract: The present invention is directed to a human Tumor Necrosis Factor mutein or a pharmaceutically acceptable salt thereof having selective binding affinity for the human p55-Tumor-Necrosis-Factor-Receptor characterized in that the amino acid sequence of human Tumor Necrosis Factor is changed at least at position 86 having a threonine instead of a serine residue, a DNA sequence coding for such a mutein, a vector comprising such a DNA sequence, and a host cell transformed by such a vector.
    Type: Grant
    Filed: April 1, 1993
    Date of Patent: January 23, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Werner Lesslauer, Hansruedi Lotscher, Dietrich Stuber
  • Patent number: 5486310
    Abstract: Optically active compounds of the formula ##STR1## wherein rings A, B and C each independently are unsubstituted or each are 1,4-phenylene substituted with at least one of halogen-, cyano-, methyl- or methoxy in which optionally 1 CH group or 2 CH groups is/are replaced by nitrogen; R.sup.1 is a radical of an optically active terpene alcohol after cleavage of the hydroxy group or a group --(CH.sub.2).sub.m --C*HX.sup.1 --R.sup.3 ; R.sup.2 is a radical of an optically active terpene alcohol after cleavage of the hydroxy group or a group --(CH.sub.2).sub.n --C*HX.sup.2 --R.sup.4 ; m and n each independently stand for the number 0 or 1: C* denotes a chiral carbon atom; X.sup.1 and X.sup.2 each independently are fluorine, chlorine, cyano, methyl or methoxy; R.sup.3 and R.sup.4 each independently denote a group R, phenyl or phenyl substituted with R, with the proviso that R.sup.3 is different from X.sup.1 and R.sup.4 is different from X.sup.
    Type: Grant
    Filed: February 18, 1994
    Date of Patent: January 23, 1996
    Assignees: Hoffmann-La Roche Inc., Niopic Moscow Research and Production Association
    Inventors: Richard Buchecker, Nina I. Chernova, Alexander V. Ivaschenko, Marina V. Loseva, Olga S. Petrashevich, Evgeniy P. Pozhidaev, Arnold Z. Rabinovich, Martin Schadt
  • Patent number: 5486466
    Abstract: Bicyclic derivatives of the general formula ##STR1## wherein X.sup.1 is --S-- or --SO--;X.sup.2 is --CO-- or --CS--;R.sup.1 is hydrogen, halogen or lower alkyl optionally substituted by halogen or lower alkoxy;R.sup.2 and R.sup.3 are each independently hydrogen, lower alkyl, halogen, amino, lower alkylamino, di-lower alkylamino, acylamino, lower alkexy, lower alkoxymethoxy or a group OR.sup.4 ;R.sup.4 is hydrogen or an easily hydrolyzable group;R.sup.5 is hydrogen, optionally esterified carboxy or amidated (thio)carboxy, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted acyl or heterocyclyl;R.sup.6 and R.sup.7a are each independently hydrogen or lower alkyl;R.sup.7b is hydrogen, optionally substituted hydroxy, --NR--A or --N.dbd.B, in which R is hydrogen or lower alkyl, A is hydrogen, optionally substituted alkyl, lower cycloalkyl, iminoyl, (thio)acyl, esterified carboxy or amidated (thio)carboxy and B is lower alkylidene;R.sup.7a and R.sup.
    Type: Grant
    Filed: November 14, 1994
    Date of Patent: January 23, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Mikio Arisawa, Erwin Gotschi, Paul Hebeisen, Tsutomu Kamiyama, Helmut Link, Raffaello Masciadri, Hisao Shimada, Junko Watanabe
  • Patent number: 5484551
    Abstract: Compounds containing a 4-[(E)-alk-2-enoyloxy]benzoate group and liquid crystalline mixtures which contain such compounds and the use of such compounds and, respectively, mixtures in electro-optical indicating devices.The compounds are of the formula ##STR1## wherein R.sup.1 is alkyl with 1 to 12 carbon atoms;X.sup.1, X.sup.3 each independently are halogen or hydrogen; andX.sup.2 is halogen or cyano.
    Type: Grant
    Filed: May 12, 1995
    Date of Patent: January 16, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Stephen Kelly, Martin Schadt