Patents Represented by Attorney Jon S. Saxe
  • Patent number: 4914095
    Abstract: A compound of the formula ##STR1## is useful to treat psychotic disorders in humans, especially schizophrenia, and to prevent exacerbations thereof. The compound can be used as a single therapeutic agent or in combination with neuroleptics such as haloperidol.
    Type: Grant
    Filed: January 13, 1989
    Date of Patent: April 3, 1990
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Walter Merz
  • Patent number: 4898861
    Abstract: A method of inhibiting the proliferation of tumor cells is disclosed which comprises the treatment of such tumor cells with a benzodiazepine having a selective affinity to bind peripheral binding sites on the tumor cell in order to induce non-proliferation of said tumor cells.
    Type: Grant
    Filed: August 29, 1988
    Date of Patent: February 6, 1990
    Assignee: Hoffmann-La Roche Inc.
    Inventors: James I. Morgan, Sydney Spector, James K. T. Wang
  • Patent number: 4888429
    Abstract: There is described a process for the manufacture of a compound of the formula ##STR1## wherein R.sup.1 is lower alkyl, lower alkanoyl, lower alkenyl or the group --CH.sub.2 COOR.sup.2 or --C(CH.sub.3).sub.2 COOR.sup.2 and R.sup.2 is a readily cleavable group, by reacting a compound of the formula ##STR2## wherein R is lower alkyl, with an alkali metal allylate and reacting the resulting compound of the formula ##STR3## wherein M is an alkali metal atom, with a compound of the formula R.sup.1 -X, wherein X is a leaving group. This process can be used to manufacture antimicrobially active mono-.beta.-lactam, cephalosporin and penicillin derivatives.
    Type: Grant
    Filed: October 17, 1988
    Date of Patent: December 19, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Paul Hebeisen
  • Patent number: 4886499
    Abstract: The portable appliance is of use for the subcutaneous or intradermal injection of a liquid formulation of an active principle and it comprises in combination: a supply vessel for the formulation; an injection needle adapted to communicate with the vessel; pump means for emptying the vessel through the injection needle; securing means for securing the appliance to an appropriate part of the patient's body; and needle-driving means for shooting the injection needle into the patient's skin.
    Type: Grant
    Filed: December 4, 1987
    Date of Patent: December 12, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Giorgio Cirelli, Hans Steffen, Christian Surber
  • Patent number: 4885283
    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: December 1, 1987
    Date of Patent: December 5, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael J. Broadhurst, Balraj K. Handa, William H. Johnson, Geoffrey Lawton, Peter J. Machin
  • Patent number: 4885361
    Abstract: Novel compounds with anti-proliferative and mucosaprotective activity are obtained by sulfating trestatins.
    Type: Grant
    Filed: July 20, 1988
    Date of Patent: December 5, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Hans P. Wessel
  • Patent number: 4885309
    Abstract: The compound 6-acetyl-7-[5-(4-acetyl-3-hydroxy-2-propylphenoxy)pentyloxy]-3,4-dihydro-2 4-1-benzopyran-2-carboxylic acid, as well as its enantiomers, salts and lower alkyl esters, are useful in topically administrable dosage forms for the treatment of leukotriene-mediated dermal inflammations, such as psoriasis. These compounds can be formulated into creams, ointments, lotions, gels and other types of compositions suitable for applying on the skin.
    Type: Grant
    Filed: August 1, 1986
    Date of Patent: December 5, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Ann F. Welton
  • Patent number: 4883613
    Abstract: The compounds 9-phenyl-3,7-dimethyl-2,4,6,8 nonatetraenoic acids wherein the phenyl group is substituted with an alkyl, aminoalkyl, hydroxyalkyl, alkoxy, hydroxyalkylamino, and a hydroxy alkoxy group, and derivatives thereof which are used as disease modifying anti-rheumatic agents and as immunosuppressants.
    Type: Grant
    Filed: July 31, 1987
    Date of Patent: November 28, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Edward R. Aig, John W. Coffey, Allen J. Lovey, Michael Rosenberger
  • Patent number: 4883815
    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)-alkoxy carbonyl-(C.sub.1 -C.sub.4)-alkyl, di-(C.sub.1 -C.sub.4)-alkoxy carbonyl-C.sub.2 -C.sub.5)-alky, piperidino-C.sub.2 -C.sub.
    Type: Grant
    Filed: July 5, 1988
    Date of Patent: November 28, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Werner Aschwenden, Rene Imhof, Roland Jakob-Roetne, Emilio Kyburz
  • Patent number: 4883614
    Abstract: The compounds 9-phenyl-3,7-dimethyl-2,4,6,8 nonatetraenoic acids wherein the phenyl group is substituted with an alkyl, aminoalkyl, hydroxyalkyl, alkoxy, hydroxyalkylamino, and a hydroxy alkoxy group, and derivatives thereof which are used as disease modifying anti-rheumatic agents and as immunosuppressants.
    Type: Grant
    Filed: October 24, 1986
    Date of Patent: November 28, 1989
    Assignee: Hoffman-La Roche Inc.
    Inventors: Edward R. Aig, John W. Coffey, Allen J. Lovey, Michael Rosenberger
  • Patent number: 4883887
    Abstract: A process for producing carotenoids and carotenoid intermediates via reduction of sulfonyl polyenes with a dithionite in the presence of ammonia or an aliphatic amine, including novel intermediates in this process, which carotenoids are known coloring agents for foodstuffs, animal feeds, pharmaceuticals, etc.
    Type: Grant
    Filed: July 1, 1988
    Date of Patent: November 28, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Kurt Bernhard, Stephan Jaggli, Paul Kreienbuhl, Ulrich Schwieter
  • Patent number: 4882441
    Abstract: A process for producing natural vitamin E and intermediates in this process.
    Type: Grant
    Filed: September 9, 1988
    Date of Patent: November 21, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: David L. Coffen, Rudolf Schmid, Mark J. Sebastian
  • Patent number: 4882164
    Abstract: Aqueous mixed micelle solutions comprising cholanic acid salts and lipids used for the solubilization of non-steroidal anti-inflammatories and for the preparation of locally tolerable pharmaceutical administration forms for such medicaments, are described.
    Type: Grant
    Filed: January 19, 1988
    Date of Patent: November 21, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alberto Ferro, Hans Steffen
  • Patent number: 4881993
    Abstract: The carbonyl compounds 5,6-carbonyl-ascorbic acid and 5,6-carbonyl-erythorbic acid been found useful for the preparation of explosive and propellant materials by admixing them with nitrate-containing oxidation agents and optionally further ingredients.
    Type: Grant
    Filed: June 29, 1989
    Date of Patent: November 21, 1989
    Assignee: Hoffman-LA Roche Inc.
    Inventors: Claude Furbringer, Horst Pauling
  • Patent number: 4882316
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is halogen, C.sub.1-4 -alkyl or halo-(C.sub.1-4 - alkyl), R.sup.2 is hydrogen, hydroxy or acyloxy, R.sup.3 and R.sup.4 each are hydrogen or C.sub.1-4 -alkyl, R.sup.5 is aryl or aryloxy, X is O or NH and Y is --CO--CH.sub.2 --, --CH(OH)--CH.sub.2 --, --CH.sub.2 --CH.sub.2 --, --S--, --SO-- or --SO.sub.2 --,and tautomers thereof are described. Compounds of formula I and their tautomers possess antiviral activity and can be used in the form of medicaments for the control and prevention of viral infections.
    Type: Grant
    Filed: July 30, 1987
    Date of Patent: November 21, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Robert W. Lambert, Joseph A. Martin, Gareth J. Thomas
  • Patent number: 4879395
    Abstract: A process for producing natural vitamin E and intermediates in this process.
    Type: Grant
    Filed: September 9, 1988
    Date of Patent: November 7, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: David L. Coffen, Rudolf Schmid, Mark J. Sebastian
  • Patent number: 4877830
    Abstract: Metal chelate resins whose complexed nitrilotriacetic acid residues are bound to a carrier matrix via a spacer and which are suitable for metal chelate chromatography of proteins, especially those which contain neighboring histidines.
    Type: Grant
    Filed: July 13, 1987
    Date of Patent: October 31, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Heinz Dobeli, Frich Hochuli
  • Patent number: 4877890
    Abstract: A process for producing alpha-tocopherol and intermediates in this process.
    Type: Grant
    Filed: October 17, 1988
    Date of Patent: October 31, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Noal Cohen
  • Patent number: 4876340
    Abstract: Benzazecinediones of the formula ##STR1## where R.sup.1 and R.sup.2 are independently hydrogen or chlorine, R.sup.3 is hydrogen, fluorine, chlorine, bromine or methoxy, R.sup.4 is hydrogen, chlorine or methoxy and R.sup.5 is hydrogen, acetyl, propionyl, benzoyl, chlorobenzoyl, methoxybenzoyl or phenylacetyl, with the proviso that 2 or 3 of the groups R.sup.1 to R.sup.4 are hydrogen, as well as many of the corresponding benzo[f]quinolines from which these benzazecinediones can be prepared by oxidation are suitable for the control or prevention of cerebral insufficiency or for the improvement of cognitive functions in mammals. They can be produced according to various processes and can be prepared into pharmaceutical compositions.
    Type: Grant
    Filed: February 11, 1988
    Date of Patent: October 24, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Werner Aschwanden, Rene Imhof, Roland Jakob, Emilio Kyburz
  • Patent number: 4876349
    Abstract: The compounds of the formula ##STR1## wherein X and Y are independently --CH.sub.2 -- or >C(CH.sub.3).sub.2 ; Z is --CHR.sup.8 --, >Co, >CR.sup.8 OR.sup.7 , --CHR.sup.8 --CHR.sup.8 --, --CHOR.sup.7 --CH.sub.2 --, --CO--CHOR.sup.7 or --CHOR.sup.7 --CHOR.sup.7 --R.sup.1 is a 5- or 6-membered, monocyclic heterocyclic group which optionally can be C-substituted by halogen, lower-alkyl, lower-alkoxy, acyloxy, nitro, hydroxy, amino, lower-alkylamino or di-lower-alkylamino and/or which can be substituted on a ring --NH-- group by lower-alkyl; R.sup.2 and R.sup.3 are independently hydrogen, lower-alkyl, trifluoromethyl or halogen and one of R.sup.2 and R.sup.3 always is trifluoromethyl or lower-alkyl; R.sup.4 and R.sup.5 are independently hydrogen, alkyl, alkoxy or halogen; R.sup.6 is hydrogen, lower-alkyl or --OR.sup.7 ; R.sup.7 is hydrogen, lower-alkyl or acyl; R.sup.8 is hydrogen or lower-alkyl; and R.sup.7 and R.sup.8 can be the same or different from one another.
    Type: Grant
    Filed: July 10, 1987
    Date of Patent: October 24, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Klaus, Ekkehard Weiss