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.
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
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.
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
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.
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
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
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
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
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
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
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.
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.
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.
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.
Abstract: The present invention is directed to a novel process for producing chromane derivatives, which are suitable as intermediates for the manufacture of d-.alpha.-tocopherol (natural vitamin E), and with a process for producing d-.alpha.-tocopherol itself.