Patents Represented by Attorney Bernard S. Leon
  • Patent number: 5036066
    Abstract: The compounds are of the class of bi- and tricyclic pyridone derivatives of the formula ##STR1## wherein the various substituent are as described in the specification, useful in the control of prevention of muscle tensions stress conditions, insomnia, anxiety states and/or convulsions.
    Type: Grant
    Filed: October 16, 1989
    Date of Patent: July 30, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Ulf Fischer, Fernand Schneider, Ulrich Widmer
  • Patent number: 5034402
    Abstract: Pyrrolidine derivatives of the formula ##STR1## wherein R.sup.1 is hydrogen or lower alkanoyl, R.sup.2 is hydrogen or lower alkyl and R.sup.3 is hydrogen, lower alkyl or a group of the formula --(CH.sub.2).sub.n --NR.sup.4 R.sup.5, wherein n is a whole number of 2 to 4 and R.sup.4 and R.sup.5 each, independently, are hydrogen or lower alkyl, or R.sup.4 and R.sup.5 taken together with the nitrogen atom are a pyrrolidinyl, piperidinyl, piperazinyl or morpholinyl group which is optionally substituted by one or two lower alkyl groups,enantiomers thereof, and acid addition salts of compounds of formula I and their enantiomers which are basic, are useful in the control or prevention of cerebral insufficiency or in the improvement of intellectual capacity. The compounds of formula I of the invention can be prepared starting from starting materials hereinafter described, and are useful as medicaments, for example, in the form of pharmaceutical preparations.
    Type: Grant
    Filed: April 12, 1990
    Date of Patent: July 23, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Werner Aschwanden, Emilio Kyburz
  • Patent number: 5034546
    Abstract: Novel methyl carbinol derivatives of Vitamin E and a method for their manufacture.
    Type: Grant
    Filed: October 9, 1990
    Date of Patent: July 23, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Richard Barner, Josef Hubscher
  • Patent number: 5030739
    Abstract: The invention is directed to a process for the catalytic oxidation of an isoprenoid containing at least one allylic hydrogen atom, which process comprises reacting the isoprenoid with oxygen or an oxygen-containing gas in an inert solvent in the presence of a N-hydroxydicarboxylic acid imide of the formula ##STR1## wherein A-B stands for CH.sub.2 -CH.sub.2, CH.dbd.CH, an aromatic hydrocarbon residue or a group derived from one of these groups in which one or more hydrogen atoms is/are replaced by alkyl or halogen,to produce a primary of secondary hydroperoxide.The process of the invention is suitable for the manufacture of steroids, vitamins, odorant substances, carotinoids and the like.
    Type: Grant
    Filed: August 31, 1990
    Date of Patent: July 9, 1991
    Assignee: Hoffman-La Roche Inc.
    Inventors: Joseph Foricher, Claude Furbringer, Karlheinz Pfoertner
  • Patent number: 5030765
    Abstract: The present invention is concerned with novel tetrahydronaphthalene and indane derivatives of the formula ##STR1## useful as for combatting dermatoses as well as neoplasmas.
    Type: Grant
    Filed: October 16, 1990
    Date of Patent: July 9, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Klaus, Peter Loeliger, Peter Mohr, Ekkehard Weiss
  • Patent number: 5030764
    Abstract: Novel styryl-tetrahydronaphthalene and indane derivatives useful for treating neoplasms and dermatoses.
    Type: Grant
    Filed: October 15, 1990
    Date of Patent: July 9, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Klaus, Peter Loeliger, Peter Mohr, Ekkehard Weiss
  • Patent number: 5028595
    Abstract: A method for treating a subject infected with the AIDS retrovirus without substantial neuropathy by administering 2',3'-dideoxycytidine to the subject at a dose of from 0.001 to 0.05 milligram per kilogram per day.
    Type: Grant
    Filed: August 21, 1989
    Date of Patent: July 2, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Whaijen Soo
  • Patent number: 5025036
    Abstract: The invention relates to catechol carboxylic acid derivatives of the formula ##STR1## wherein, R.sub.1 is ##STR2## acetyl, hydrogen, hydroxy or alkanoyloxy, R.sub.2 is ##STR3## hydroxy, hydrogen or alkanoyloxy, wherein R is hydrogen, lower alkyl or --(CH.sub.2).sub.n --N--(lower alkyl).sub.2,R.sub.3 is hydrogen, lower alkyl or amino,R.sub.4 is hydrogen, lower alkyl, halogen or aminoA is ##STR4## wherein, R.sub.5 is hydrogen or acyl, R.sub.6 is hydrogen, halogen, lower alkyl, aryl or cycloalkyl, and R.sub.7 and R.sub.8, independently, are hydrogen, lower alkyl or halogen, orA is ##STR5## wherein, R.sub.5 is hydrogen or acyl, R.sub.9 is hydrogen, lower alkyl, R.sub.10 is hydrogen, lower alkyl or halogen, R.sub.11 is hydrogen, lower alkyl, cycloalkyl or halogen, m is 0 or 1, n is an integer of 2-10, provided, that no more than one of R.sub.1 or R.sub.2 can be hydroxy, alkanoyloxy or ##STR6## and when R is hydrogen, salts thereof with pharmaceutically acceptable bases or when R is --(CH.sub.2).sub.
    Type: Grant
    Filed: May 3, 1989
    Date of Patent: June 18, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Matthew Carson, Ru-Jen L. Han, Ronald A. LeMahieu
  • Patent number: 5019351
    Abstract: A test element for agglutination tests, comprising a receiving and mixing region for a sample and reagents and a reaction capillary having an upstream region which produces a capillary effect causing the sample-reagents mixture to flow at a speed which is greater than along a downstream region of the reaction capillary. An intermediate region can be provided between the upstream capillary region and the downstream region. The downstream end of capillary is connected to a collecting region. The test element is characterized by continuous supply and movement of the sample-reagents mixture through the reaction capillary. More particularly the time needed for a sample-reagents mixture to flow from the upstream end to the downstream end of the reaction capillary fluctuates only slightly between tests. The test element is particularly suitable for detecting drugs of abuse such as cocaine metabolites in human body fluids.
    Type: Grant
    Filed: October 9, 1990
    Date of Patent: May 28, 1991
    Assignee: Hoffman-La Roche Inc.
    Inventor: Peter Schulz
  • Patent number: 5017487
    Abstract: New transcriptional regulatory sequences useful in the expression of pro- or eukaryotic proteins in eukaryotic organisms are provided comprising the 5' flanking region of the vaccinia virus late 11 kDa gene. Also described are recombinant vectors and recombinant infectious poxviruses containing such transcriptional regulatory sequences operatively linked to foreign genes, and live vaccines based upon these recombinant infectious poxviruses.
    Type: Grant
    Filed: March 27, 1986
    Date of Patent: May 21, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Hendrik G. Stunnenberg, Riccardo Wittek
  • Patent number: 5017608
    Abstract: Hydrocinnamic acid derivatives of the formula ##STR1## wherein one or two of the symbols R.sup.1 to R.sup.4 are halogen or methoxy and the others are hydrogen;R.sup.5 is hydrogen or phenyl;R.sup.6 is a residue of the formula ##STR2## R.sup.7 is (C.sub.1 -C.sub.4)-alkyl, (C.sub.2 -C.sub.5)-alkanoylamino-(C.sub.2 -C.sub.5)-alkyl, amino or (C.sub.1 -C.sub.4)-alkoxyphenyl;R.sup.8 and R.sup.9 each, independently, are hydrogen or (C.sub.1 -C.sub.4)-alkyl;R.sup.10 is hydrogen and R.sup.11 is hydroxy or R.sup.10 and R.sup.11 taken together are oxo;R.sup.12 is hydrogen, (C.sub.1 -C.sub.10)-alkyl, pyridylmethyl or carbamoylmethyl;R.sup.13 is hydrogen, (C.sub.1 -C.sub.4)-alkyl and R.sup.14 is hydrogen, (C.sub.1 -C.sub.4)-alkyl, pyridyl, phenyl-(C.sub.1 -C.sub.4)-alkyl, carboxy-(C.sub.1 -C.sub.4)-alkyl, carbamoyl-(C.sub.1 -C.sub.4)-alkyl, (C.sub.1 -C.sub.4)-alkoxycarbonyl-(C.sub.1 -C.sub.4)-alkyl, di-(C.sub.1 -C.sub.4)-alkoxycarbonyl-(C.sub.2 -C.sub.5)-alkyl, piperidino-(C.sub.2 -C.sub.
    Type: Grant
    Filed: September 6, 1989
    Date of Patent: May 21, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Werner Aschwanden, Rene Imhof, Roland Jakob-Roetne, Emilio Kyburz
  • Patent number: 5015661
    Abstract: Racemic Compounds of the formula ##STR1## A is --C.tbd.C--R.sub.6, --CH.sub.2 --CH.sub.2 --R.sub.7 or ##STR2## R.sub.1 is hydrogen or lower alkanoyl, R.sub.2, R.sub.3, and R.sub.4 independently are hydrogen or lower alkyl,R.sub.5 is lower alkyl,R.sub.6 is a heteroaromatic radical or an aromatic radical selected from phenyl, naphthyl or phenanthryl, which aromatic radical may optionally be substituted by one or more substituents selected from chlorine, fluorine, lower alkyl, lower alkoxy, phenyl lower alkoxy, lower alkanoyl, lower alkanoyloxy, hydroxy-lower alkyl, carboxy, lower alkoxycarbonyl, hydroxyimino lower alkyl, amino, amino lower alkyl, mono- or di-lower alkylamino, mono- or di-lower alkylamino-lower alkyl, lower alkanoylamino, aminocarbonyl, lower alkylaminocarbonyl, lower dialkylaminocarbonyl, trifluoroacetylamino, trifluoromethyl, hydroxy, pyridyl, or on adjacent carbons can be ##STR3## wherein R' is hydrogen, lower alkanoyl, trifluoroacetyl and R" hydrogen or lower alkyl,R.sub.
    Type: Grant
    Filed: June 16, 1989
    Date of Patent: May 14, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Armin Walser
  • Patent number: 5013476
    Abstract: A ferroelectric liquid crystal mixture containing at least one compound of the formula ##STR1## wherein n stands for the number 0 or 1; X.sup.1 represents a single covalent bond, --COO-- or --OOC-- and X.sup.2 represents a single covalent bond, --COO--, --OOC--, --CH.sub.2 CH.sub.2 --, --OCH.sub.2 -- or --CH.sub.2 O--; rings A.sup.1, A.sup.2 and A.sup.3 each independently signify 1,4-phenylene optionally substituted with cyano, halogen or lower alkyl or pyrimidin-2,5-diyl, pyrazin-2,5-diyl, when n is 1, trans-1,4-cyclohexylene or trans-m-dioxan-2,5-diyl; with the proviso that one of the rings present stands for pyrimidin-2,5-diyl or pyrazin-2,5-diyl when a further ring signifies trans-1,4-cyclohexylene or when n stands for the number 0 and X.sup.1 stands for a single covalent bond; and R.sup.1 signifies an optionally halogen-substituted alkenyl group with up to 18 carbon atoms in which optionally 1 or 2 non-adjacent CH.sub.2 groups are replaced by --O-- and/or a C.dbd.C double bond; with the proviso that R.
    Type: Grant
    Filed: November 17, 1987
    Date of Patent: May 7, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Arthur Boller, Richard Buchecker, Hans-Jurgen Fromm, Stephen Kelly, Martin Schadt, Alois Villiger
  • Patent number: 5013478
    Abstract: Compounds of the formula ##STR1## wherein, inter alia, R.sup.1 is hydrogen or straight-chain alkyl; R.sup.2 is --CN, --R, --COR, --COOR; R is alkyl; A is a group with 1 to 4 six-membered rings, these rings being linked directly with one another and with ring B in each case via a single covalent bond or being linked at one or two positions also via ester or ether groups; the six-membered rings in A and ring B each are 1,4-phenylene or trans-1,4-cyclohexylene or one of these rings also is trans-2,5-disubstituted m-dioxane; m can be 0 when ring B is trans-1,4-cyclohexylene or trans-2,5-disubstituted m-dioxane,liquid crystalline mixtures which contain these compounds as well as their use for electro-optical purposes are described.
    Type: Grant
    Filed: August 31, 1988
    Date of Patent: May 7, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Martin Petrzilka
  • Patent number: 5013477
    Abstract: Compounds of the formula ##STR1## wherein Z represents a single covalent bond or --CH.sub.2 CH.sub.2 --, R.sup.1 denotes 1E-alkenyl with 2-10 carbon atoms or 3E-alkenyl with 4-10 carbon atoms and R.sup.2 is alkyl with 1-10 carbon atoms, 2E-alkenyl with 3-10 carbon atoms or 3-alkenyl with 4-10 carbon atoms,as well as their use in liquid crystalline mixtures and for electro-optical purposes.
    Type: Grant
    Filed: October 26, 1988
    Date of Patent: May 7, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Richard Buchecker, Martin Schadt
  • Patent number: 5011849
    Abstract: Ethylenediamine monoamides of the formulaR--CO--NH--CH.sub.2 --CH.sub.2 --NH.sub.2 Iwherein R is one of groups ##STR1## in which R.sup.1 is phenyl monohalophenyl, monolower-alkylphenyl, monolower-alkoxypheynl, monotrifluoromethylphenyl, monocyanophenyl or monoaryl-lower-alkoxyphenyl, dihalophenyl, furyl, thienyl or monohalothienyl, R.sup.2 is hydrogen, halogen or amino, R.sup.3, R.sup.5 and R.sup.7 each are phenyl, monohalophenyl, dihalophenyl, thienyl, furyl or monohalofuryl, R.sup.4 and R.sup.6 each are hydrogen or amino and R.sup.8 is hydrogen or lower-alkyl, as well as their pharmaceutically usable acid addition salts are disclosed. The compounds have monoamine oxidase inhibiting properties with low toxicity and are useful for the treatment of depressive states and cognitive disorders.
    Type: Grant
    Filed: July 21, 1989
    Date of Patent: April 30, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Walter Gassner, Rene Imhof, Emilio Kyburz
  • Patent number: 5010060
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is halogen, C.sub.1-4 -alkyl, halo-(C.sub.1-4 -alkyl) or C.sub.2-4 -alkanoyl,R.sup.2 is hydrogen, hydroxy, C.sub.1-4 -alkoxy, C.sub.1-4 -alkylthio or phenyl-(C.sub.1-4 -alkoxy) or, when X is O, also acyloxy,R.sup.3 is hydrogen or C.sub.1-4 -alkyl,R.sup.4 is a carbocyclic group or a heterocyclic group,R.sup.5 is hydrogen or fluorine,m stands for zero, 1 or 2,X is O or NH and Y is a direct bond, --CH.dbd.CH--, --C.tbd.C-- or a group of the formula of--(Z).sub.n --A-- (a)in which A is a C.sub.1-8 -alkylene group which is optionally substituted by one or two phenyl groups, is O, S, SO or SO.sub.2 and n stands for zero or 1, with the proviso that R.sup.1 is different from iodine, when R.sup.2 is hydroxy or benzoyloxy, R.sup.3 is hydrogen, R.sup.4 is unsubstituted phenyl, R.sup.
    Type: Grant
    Filed: April 24, 1989
    Date of Patent: April 23, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Robert W. Lambert, Joseph A. Martin, Gareth J. Thomas
  • Patent number: 5008411
    Abstract: A process for the preparing a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are each independently hydrogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, halogen, trifluoromethyl or nitro; or R.sub.1 and R.sub.2 taken together with the benzene ring to which they are attached are naphthalene, and Ar is p-lower alkoxy phenyl.which comprises reacting ##STR2## wherein R.sub.1 and R.sub.2 are as described above with the compound of the formula ##STR3## wherein Ar is as described above, in an aromatic organic compound. The intermediates formed by the process of the invention are useful in the production of thiazepin-4(5H)-ones which have activity as calcium channel blockers and accordingly are useful as agents for lowering blood pressure and agents for treating ischemia.
    Type: Grant
    Filed: October 2, 1989
    Date of Patent: April 16, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventors: David L. Coffen, Pradeep B. Madan, Alan Schwartz
  • Patent number: 5006651
    Abstract: The invention relates compounds of the formula ##STR1## wherein R.sup.1 -R.sup.5 and X have the significance given in the description, and their pharmaceutically acceptable salts. The compounds of formula I inhibit the enzyme collagenase and can be used in the form of medicaments for the control or prevention of degenerative joint diseases such as rheumatoid arthritis and osteoarthritis.
    Type: Grant
    Filed: September 22, 1989
    Date of Patent: April 9, 1991
    Assignee: Hoffman-La Roche Inc.
    Inventors: Michael J. Broadhurst, Balraj K. Handa, William H. Johnson, Geoffrey Lawton, Peter J. Machin
  • Patent number: 5004324
    Abstract: A liquid crystal display (LCD) cell comprising a highly twisted nematic liquid crystal disposed between two electrode plates and polarizers and having a positive dielectric anisotropy. The optical path difference .DELTA.n.d is 0.2 to 0.7 .mu.m and the ratio d/p of thickness to pitch is 0.2 to 0.6. The absolute value of the twist angle .phi. can be between 120.degree. and 260.degree. for a right-hand twist or left-hand twist, the angle .psi. between the polarizers can be between 0.degree. and 180.degree. and the angle .beta. between the surface orientation direction and the polarization direction on the screen on the light incidence side can be between 0.degree. and 360.degree..
    Type: Grant
    Filed: January 18, 1990
    Date of Patent: April 2, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Frans Leenhouts, Martin Schadt