Patents Represented by Attorney George M. Gould
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Patent number: 5502236Abstract: 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: GrantFiled: March 17, 1995Date of Patent: March 26, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Bruno Burdet, August Ru/ ttimann, Jean-Marie Santer, Theodor Siegfried
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Patent number: 5500752Abstract: 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: GrantFiled: January 17, 1995Date of Patent: March 19, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Martin Schadt, Hubert Seiberle
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Patent number: 5498367Abstract: 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: GrantFiled: February 17, 1995Date of Patent: March 12, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Richard Buchecker, Guy Marck, Martin Schadt
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Patent number: 5496519Abstract: 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: GrantFiled: July 21, 1994Date of Patent: March 5, 1996Assignee: Hoffmann-La Roche Inc.Inventor: Gottlieb Schacher
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Patent number: 5494666Abstract: 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: GrantFiled: June 9, 1995Date of Patent: February 27, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Markus Bohringer, Christian Hubschwerlen, Philippe Pflieger, Jean-Luc Specklin
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Patent number: 5495039Abstract: 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: GrantFiled: September 21, 1994Date of Patent: February 27, 1996Assignee: Givaudan-Roure CorporationInventors: Georg Frater, Rolf Schwarzenbach, Stephane F. M. Van Oycke
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Patent number: 5495025Abstract: 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: GrantFiled: March 9, 1995Date of Patent: February 27, 1996Assignee: Hoffmann-La Roche Inc.Inventor: Hans Hilpert
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Patent number: 5495048Abstract: 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: GrantFiled: June 17, 1994Date of Patent: February 27, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Johannes Aebi, Philipe Guerry, Synese Jolidon, Olivier Morand
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Patent number: 5494928Abstract: 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: GrantFiled: October 3, 1994Date of Patent: February 27, 1996Assignee: Hoffmann-La Roche Inc.Inventor: Michael Bos
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Patent number: 5491086Abstract: 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: GrantFiled: May 14, 1993Date of Patent: February 13, 1996Assignee: Hoffmann-La Roche Inc.Inventors: David H. Gelfand, Alice M. Wang
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Patent number: 5491063Abstract: 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: GrantFiled: September 1, 1994Date of Patent: February 13, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Mary E. Fisher, Robert M. Watson
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Patent number: 5491225Abstract: 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: GrantFiled: May 27, 1993Date of Patent: February 13, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Teresa K. H. Picone, Theresa M. McCallum, Michael A. Zoccoli
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Patent number: 5487972Abstract: 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: GrantFiled: January 5, 1993Date of Patent: January 30, 1996Assignee: Hoffmann-La Roche Inc.Inventors: David H. Gelfand, Pamela M. Holland, Randall K. Saiki, Robert M. Watson
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Patent number: 5488115Abstract: 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: GrantFiled: May 12, 1995Date of Patent: January 30, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Kevin E. B. Parkes, Sally Redshaw, Gareth J. Thomas
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Patent number: 5487817Abstract: 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: GrantFiled: January 21, 1994Date of Patent: January 30, 1996Assignee: Hoffmann-La Roche Inc.Inventor: Christian Fizet
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Patent number: 5488172Abstract: 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: GrantFiled: August 23, 1994Date of Patent: January 30, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Marco Cereghetti, Joseph Foricher, Bernd Heiser, Rudolf Schmid
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Patent number: 5486463Abstract: 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: GrantFiled: April 1, 1993Date of Patent: January 23, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Werner Lesslauer, Hansruedi Lotscher, Dietrich Stuber
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Patent number: 5486310Abstract: 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: GrantFiled: February 18, 1994Date of Patent: January 23, 1996Assignees: Hoffmann-La Roche Inc., Niopic Moscow Research and Production AssociationInventors: Richard Buchecker, Nina I. Chernova, Alexander V. Ivaschenko, Marina V. Loseva, Olga S. Petrashevich, Evgeniy P. Pozhidaev, Arnold Z. Rabinovich, Martin Schadt
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Patent number: 5486466Abstract: 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: GrantFiled: November 14, 1994Date of Patent: January 23, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Mikio Arisawa, Erwin Gotschi, Paul Hebeisen, Tsutomu Kamiyama, Helmut Link, Raffaello Masciadri, Hisao Shimada, Junko Watanabe
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Patent number: 5484551Abstract: 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: GrantFiled: May 12, 1995Date of Patent: January 16, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Stephen Kelly, Martin Schadt