Patents Represented by Attorney George M. Gould
  • Patent number: 5449823
    Abstract: Two optically active forms of 4-hydroxy-3-methyl-2-keto-pentanoic acid of the formula ##STR1## wherein carbon atom 4 has the (S)-configuration, and carbon atom 3 can have the (R)-configuration or the (S)-configuration (compound I) are made using a biotransformation process. Compound I may be manufactured by reacting 4-hydroxy-isoleucine (2S, 3R, 4S) of the formula: ##STR2## with microorganisms which have L-amino acid oxidase activity or with an L-amino acid oxidase. Compound I is a flavor precursor and may also be used as an intermediate for the production of the optically active (5S)-3-hydroxy-4,5-dimethyl-2(5H)-furanone: ##STR3## which is useful as a flavorant.
    Type: Grant
    Filed: April 28, 1994
    Date of Patent: September 12, 1995
    Assignee: Givaudan-Roure Corporation
    Inventor: Konrad Lerch
  • Patent number: 5447839
    Abstract: The presence of human papillomavirus (HPV) in a sample can be detected and the HPV typed by a method that involves the amplification of HPV DNA sequences by the polymerase chain reaction (PCR). The primers used in the method are consensus primers that can be used to amplify a particular region of the genome of any HPV. The presence of HPV in a sample is indicated by the formation of amplified DNA. The HPV nucleic acid is detected by consensus probes that may be short oligonucleotide probes or long genetic probes. The HPV is typed by the use of type-specific DNA probes specific for the amplified region of DNA.
    Type: Grant
    Filed: April 20, 1993
    Date of Patent: September 5, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: M. Michele Manos, Heidi M. Bauer, Catherine E. Greer, Robert M. Resnick, Yi Ting
  • Patent number: 5447919
    Abstract: The use of compounds of the formula ##STR1## wherein R is hydrogen or a residue --SO.sub.3 M; M is a cation; and R' and R" are hydrogen or an .alpha.-glycosidically linked sulfated mono- or disaccharide residue; and at least one --SO.sub.3 M group is present per monosaccharide unit,as pharmaceutical compositions for the prevention and/or treatment of arteriosclerotic disorders and for the prevention of restenosis after invasive vascular surgery and after organ transplants.
    Type: Grant
    Filed: March 17, 1994
    Date of Patent: September 5, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Markus Hosang, Niggi Iberg, Thomas B. Tschopp, Hans P. Wessel
  • Patent number: 5447953
    Abstract: The use of biomasses obtained in the fermentative production of lipase inhibitors, especially lipstatin, for the preparation of foodstuffs, feedstuffs, food additives, feed additives, feed supplements, medicinal feed premixes or medicaments for oral administration, are described.
    Type: Grant
    Filed: June 17, 1994
    Date of Patent: September 5, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Dorothea Isler, Walter Rehm, Erich Widmer
  • Patent number: 5447929
    Abstract: Hydroxamic acid derivatives of the fdrrnula ##STR1## and pharmaceutically acceptable salts thereof, which are collagenase inhibitors useful for the control or prevention of degenerative joint diseases, such as, rheumatoid arthritis and ostecarthritis or for the treatment of invasive tumours, atherosclerosis or multiple sclerosis, are described. Said compounds can be prepared either by hyclroxamidating a corresponding carboxylic acid or deprotecting a corresponding benzyloxycarbamoyl compound.
    Type: Grant
    Filed: March 17, 1994
    Date of Patent: September 5, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael J. Broadhurst, Paul A. Brown, William H. Johnson, Geoffrey Lawton
  • Patent number: 5447658
    Abstract: Compounds of the general formula ##STR1## wherein R.sup.1 represents vinyl or straight-chain alkenyl with 3 to 7 carbon atoms,the manufacture of such compounds, liquid crystalline mixtures which contain such compounds as well as the use of such compounds for electro-optical purposes.
    Type: Grant
    Filed: June 17, 1994
    Date of Patent: September 5, 1995
    Assignees: Hoffman-La Roche Inc., Dainipppon Ink and Chemicals, Inc.
    Inventors: Richard Buchecker, Teodor Lukac, Martin Schadt, Haruyoshi Takatsu, Alois Villiger
  • Patent number: 5447662
    Abstract: Polymeric coatings having optically non-linear or optically anisotropic properties in selected areas and of any arbitrary shape including a pattern. These zones are sharply defined from surfaces having centro-symmetrical or isotropic configurations or from surfaces with different optically non-linear or anisotropic properties. The polymeric coating has optically non-linear and/or mesogenic side chains, selected surface areas of which are cross-linked by the action of light, the zones which have optically non-linear or anisotropic properties being subjected to the influence or orienting fields or forces during the cross-linking process. The distances between optically different zones are limited to typically about 1 .mu.m.
    Type: Grant
    Filed: December 18, 1991
    Date of Patent: September 5, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Rolf-Peter Herr, Martin Schadt, Klaus Schmitt
  • Patent number: 5447657
    Abstract: The present invention provides compounds of the general formula: ##STR1## wherein R is an alkyl group with 1 to 12 carbon atoms or a group of the formula ##STR2## Ring A.sup.1 is 1,4-phenylene, which is unsubstituted or substituted with fluorine, pyridine-2,5-diyl or pyrimidine-2,5-diyl;Ring A.sup.2 is trans-1,4-cyclohexylene or trans-1,3-dioxane-2,5-diyl;R.sup.1 is an alkyl, alkenyl or alkoxyalkyl group with 1 to 12 and, respectively, 2 to 12 carbon atoms;X.sup.1 is fluorine, chlorine, bromine, trifluoromethyl, trifluoromethoxy or difluoromethoxy; andX.sup.2, X.sup.3 each independently are hydrogen or fluorine.The invention is also concerned with liquid crystal mixtures which contain these compounds and with the use of these compounds and mixtures for electro-optical purposes.
    Type: Grant
    Filed: March 8, 1994
    Date of Patent: September 5, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Martin Schadt, Alois Villiger
  • Patent number: 5446189
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, n, m, o, p, and q are as hereinafter set forth,and, when R.sub.2 is hydrogen, pharmaceutically acceptable salts thereof with bases, are described. The compounds of formula 1 are potent inhibitors of phospholipases A.sub.2 (PLA.sub.2 's) and are therefore useful in the treatment of inflammatory diseases, such as psosiasis, inflammatory bowel disease, asthma, allergy, arthritis, dermatitis, gout, pulmonary disease, myocardial ischemia/reperfusion, and trauma induced inflammation, such as spinal cord injury.
    Type: Grant
    Filed: March 22, 1994
    Date of Patent: August 29, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Mathew Carson, Ru-Jen L. Han, Ronald A. LeMahieu, Vincent S. Madison
  • Patent number: 5446161
    Abstract: Compounds of the formula ##STR1## wherein and their pharmaceutically acceptable acid addition salts inhibit proteases of vital origin and can be used as medicaments for the treatment or prophylaxis of viral infections. They can be manufactured according to generally known procedures.
    Type: Grant
    Filed: July 20, 1992
    Date of Patent: August 29, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Balraj K. Handa, Peter J. Machin, Joseph A. Martin, Sally Redshaw, Gareth J. Thomas
  • Patent number: 5443792
    Abstract: A pipetting device contains a pipetting needle connected to metering device for transferring a volume of liquid from a primary vessel to a secondary vessel. Primary vessel and secondary vessels are disposed on the same or different vessel carrier units, and each vessel has a clearly defined position relative to the vessel carrier unit. Additionally, a device is provided for controlling conveyance of the pipetting needle in three directions. The controlling device controls the metering device and the conveyance device. The pipetting device independently determines coordinates of the pipetting positions for each vessel carrier unit. For each vessel carrier unit at least one reference member, which is part of the vessel carrying unit or is directly and permanently connected thereto, may be provided. These vessel carrier units have flat surfaces which are accessible to sensing the pipetting needle.
    Type: Grant
    Filed: October 19, 1994
    Date of Patent: August 22, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Jurg Buhler
  • Patent number: 5440050
    Abstract: A process for the production of ambergris-type labdane spiroketals of general formulae I and II ##STR1## where R represents oxygen or sulphur, useful in the perfumery industry, the said process being characterized by the intramolecular cyclisation of the epoxyketone or its thio analog of general formula III ##STR2## where R.sub.1 represents COCH.sub.3 and R.sub.2 oxygen or sulphur.
    Type: Grant
    Filed: October 18, 1994
    Date of Patent: August 8, 1995
    Assignee: Givaudan-Roure Corporation
    Inventors: Maria do Ceu Goncalves da Costa, Maria J. V. de Oliveira Baptista Marcelo Curto, Maria R. de Loureiro da Silva Tavares da Rosa, William B. Motherwell
  • Patent number: 5438052
    Abstract: Cephalosporin derivatives have the formula ##STR1## wherein Z.sup.1, Z.sup.2, X, Y, P, Q, m, n and p are as defined in the following text. Also described are the readily hydrolyzable esters and pharmaceutically compatible salts of these compounds, and hydrates of compounds of formula I, their esters and salts. Processes are provided for manufacture and pharmaceutical preparations which contain these compounds. Intermediates from the manufacture of these compounds are described, as is the use of the compounds in the control of illnesses and for the manufacture of the aforementioned preparations.
    Type: Grant
    Filed: November 20, 1992
    Date of Patent: August 1, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Peter Angehrn, Andre Furlenmeier, Paul Hebeisen, Werner Hofheinz, Helmut Link
  • Patent number: 5437841
    Abstract: A cell for performing optical measurements in a automatic analyzer includes a cell having a tubular body. The body has two plane-parallel walls, and is open at one end and closed at the opposite end by a bottom wall. At the open end of the body, tongues extend perpendicularly outward from each plane-parallel wall. Each tongue includes a recess, with each tongue and its recess being symmetrically placed relative to another tongue and its recess with respect to the longitudinal axis of the cell.
    Type: Grant
    Filed: January 21, 1994
    Date of Patent: August 1, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Alfons Balmer
  • Patent number: 5437989
    Abstract: A homogeneous alcohol/aldehyde dehydrogenase isolated from Gluconobacter oxydans DSM 4025 FERM BP-3812 is disclosed. The enzyme is capable in the presence of an electron acceptor, of catalyzing the conversion of L-sorbose to 2-keto-L-gulonic acid via L-sorbosone. The enzyme has a molecular weight of 130,000-140,000 daltons as determined by gel filtration column chromatography, a pyrroloquinoline quinone prosthetic group, an optimum pH for enzyme activity of 7.0 to 9.0, an optimum temperature for enzyme activity from about 20.degree. C. to 40.degree. C. and an isoelectric point of about 4.4. Also disclosed is a process for producing the enzyme and a process for producing aldehydes, carboxylic acids and ketones, especially 2-keto-L-gulonic acid utilizing the enzyme.
    Type: Grant
    Filed: December 3, 1993
    Date of Patent: August 1, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Akira Asakura, Tatsuo Hoshino
  • Patent number: 5436338
    Abstract: Novel substituted heterocyclic formamidines are useful as ultraviolet light absorbers, the formamidines having the formula ##STR1## wherein: Ar represents a 2-thiazolyl, 2-pyridyl, 2- 4,6-dimethyl) pyrmidyl or a 4-(2-methyl)quinolyl group, and,R represents a phenyl group or an alkyl group of from one to eight carbon atoms.
    Type: Grant
    Filed: April 9, 1993
    Date of Patent: July 25, 1995
    Assignee: Givaudan-Roure Corporation
    Inventors: Joseph A. Virgilio, Emanuel Heilweil, Isaac D. Cohen
  • Patent number: 5434186
    Abstract: Compounds of the formula ##STR1## wherein X is O or CH.sub.2 ; Y is O, --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, or --OCH.sub.2 C.sub.6 H.sub.4 --;Z is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH-- or --C.tbd.C--;f, h, k, m and t, independently, are 0 or 1;n is an integer from 1 to 12;R.sup.1 is hydrogen, lower alkyl, lower alkenyl, cycloalkyl, or aralkyl; and A is B or --O--B, wherein B is a mono-, di- or tricyclic aromatic or heteroaromatic moiety substituted by the group --COR.sup.2, --(O).sub.t --(W).sub.s --COR.sup.2 or --(CH.dbd.CH).sub.p COR.sup.2 and which may also contain up to 4 additional substituents selected, independently, from the group consisting of halogen, cyano, lower alkyl, lower alkoxy, sulfonamido, alkanoyl, aroyl, --(Q).sub.k --(W).sub.s' --E or --(Q).sub.k --(W).sub.s" --C.sub.6 H.sub.4 --(W).sub.s'" --E, provided that no more than one of said substituents is --(Q).sub.k --(W).sub.s' --E or --(Q).sub.k --(W).sub.s" --C.sub.6 H.sub.4 --(W).sub.s'" --E, and wherein E is COR.sup.
    Type: Grant
    Filed: September 28, 1993
    Date of Patent: July 18, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Noal Cohen, Ferdinand K. Lee, Keith A. Yagaloff
  • Patent number: 5432069
    Abstract: A tocopherol cyclase is produced in homogenous form which acts on phytyl benzoquinol derivatives to produce R', R', R'-tocopherols enantioselectively. The cyclase has a molecular weight of from about 48 kD to about 50 kD as determined by SDS-PAGE. The cyclase is isolated from Chlorella protothecoides, Dunaliella salina and wheat leaves of the Fidel variety.
    Type: Grant
    Filed: July 17, 1992
    Date of Patent: July 11, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Fiona Gruninger, Erich Hochuli, Peter K. Matzinger
  • Patent number: 5430024
    Abstract: Acetic acid derivatives of formulaH.sub.2 N(NH)C--X--Y--CO--Z--CH(Q.sup.1)COOQ.sup.2 Iand hydrates, solvates and physiologically acceptable salts thereof are useful to inhibit the binding of adhesive proteins to blood platelets and also to inhibit blood platelet aggregation and cell-cell adhesion.
    Type: Grant
    Filed: September 20, 1993
    Date of Patent: July 4, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Albrecht Edenhofer, Marcel Muller, Arnold Trzeciak, Thomas Weller
  • Patent number: 5430041
    Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 is alkoxycarbonyl, aralkoxycarbonyl, alkanoyl, aralkanoyl, heterocyclylcarbonyl or a group of the formula: ##STR2## R.sup.2 is alkyl, cycloalkylalkyl or aralkyl; R.sup.3 is hydrogen and R.sup.4 is hydroxy or R.sup.3 and R.sup.4 together are oxo; R.sup.5 is alkoxycarbonyl or alkylcarbamoyl; R.sup.6 and R.sup.7 together are trimethylene or tetramethylene optionally substituted by alkyl or on adjacent carbon atoms by tetramethylene; R.sup.8 is alkoxycarbonyl, aralkoxycarbonyl, alkanoyl, aroyl, aralkanoyl or heterocyclylcarbonyl; and R.sup.9 is alkyl, cycloalkyl, cycloalkylalkyl, aralkyl, cyanoalkyl, carbamoyl-alkyl, alkylthioalkyl, alkoxyalkyl or alkoxycarbonylalkyl: and pharmaceutically acceptable acid addition salts of those compounds of formula I which are basic, inhibit aspartyl proteases of viral origin and can be used in the form of medicaments for the prophylaxis or treatment of viral infections.
    Type: Grant
    Filed: April 21, 1992
    Date of Patent: July 4, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Joseph A. Martin, Gareth J. Thomas