Abstract: The compounds of the formula ##STR1## wherein Ra,R.sub.b,R.sub.c R.sub.d are defined in the specification and pharmaceutically acceptable addition salts are disclosed.The compounds of formula I have valuable pharmacological properties and can be used for the control or prevention of illnesses. In particular, they have muscle relevant, seditive-hypnotic, anxiolytic and/or anticonvulsive activity and can accordingly be used in the control or prevention of muscle tensions, stress conditions, isomnia, anxiety states and/or convulsions.
Abstract: An asymmetric synthesis for Vitamin E in an optically active pure form for 4-(2,5-diloweralkanoyloxy)-3,4,6-trimethylphenyl-butan-2-one and intermediates therein.
Abstract: A novel process for the manufacture of quinone derivatives is described.In this process a compound of the formula ##STR1## is reacted with a compound of the formula ##STR2## and the resulting compound of the formula ##STR3## is subjected to a retro-Diels-Alder reaction. The substituents R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the significance given in the description.
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,Z 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:
July 31, 1987
Date of Patent:
July 25, 1989
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Robert W. Lambert, Joseph A. Martin, Gareth J. Thomas
Abstract: Lactic acid produced by cells in culture is detected and used in a bioassay to determine cell growth and vitality. Lactic acid is detected by coupling the lactate dehydrogenase conversion of lactic acid to pyruvic acid to a reaction using micotinamide adenine dinucleotide in reduced form (NADH) to reduce a tetrazolium dye. The process can be used to serve as a bioassay for measuring biologically active compounds, particularly lymphokines.
Type:
Grant
Filed:
November 29, 1984
Date of Patent:
July 18, 1989
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Philip C. Familletti, Judith W. Swanson
Abstract: Dihydropyridine derivatives of the formula ##STR1## wherein the symbols R and R.sup.1 to R.sup.6 have the significance given in claim 1, have a pronounced calcium-antagonist activity and can accordingly be used as medicaments, especially in the control or prevention of angina pectoris, ischemia, high blood pressure and/or migraine.
Abstract: A method and a device for measuring mechanical property parameters of the pulmonary system of a patient which comprises;inflating and deflating the lung with a predetermined gas volume with a pump;measuring the pressure changes generated in the lung during inflation and deflation with a pressure sensor;transforming the volume and the measured pressure data into digital form;calculating typical or clinically significant volume to pressure ratios in a data processor and;displaying the result of the calculation.
Abstract: A new process for the stereospecific synthesis of alkaloids of the vinblastine and vincristine type including the synthesis of vinblastine and vincristine as well novel alkaloids which are active as anti-tumor agents.
Type:
Grant
Filed:
May 18, 1987
Date of Patent:
June 20, 1989
Assignee:
University of Vermont & State Agricultural College
Abstract: The novel 5,6-sulfinyl-L-ascorbic acid and its stereoisomers, their manufacture by sulfinylating L-ascorbic acid or corresponding stereoisomers, compositions having oxidation-inhibiting properties which contain 5,6-sulfinyl-L-ascorbic acid or a stereoisomer thereof as well as the use of 5,6-sulfinyl-L-ascorbic acid or a stereoisomer thereof as an antioxidant are described.
Abstract: Compositions comprising a mixture of the antibiotic frenolicin B with one of the ionophorous polyether anticoccidial agents, useful for the treatment and prevention of coccidiosis in animals and methods of treating coccidiosis ar disclosed.
Type:
Grant
Filed:
May 11, 1987
Date of Patent:
June 13, 1989
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Gianpaolo Maestrone, Eugene G. Schildknecht, Govind G. Untawale
Abstract: A-B-C wherein A and C are each independently 2',3' dideoxynucleosides and B is a linking group; and a method of treating or preventing a retroviral injection in a subject by administering the compounds of the invention.
Type:
Grant
Filed:
June 22, 1987
Date of Patent:
June 6, 1989
Assignees:
Hoffman-La Roche Inc., United States of America
Inventors:
Steve Tam, Manfred Weigele, Samuel Broger, Hiroaki Mitsuya
Abstract: A flow cell for high performance chromatography, in which the measuring chamber is formed by a bore (12) in a plate (11) and the supply and discharge ducts are formed by bores (13, 14) in the plate (11) communicating with grooves (16, 18) in the plate surfaces (15, 17), the grooves being covered by transparent plates (19, 20) bonded on the plate surfaces, and thus forming closed ducts.
Abstract: A transparent disk with a round periphery is produced, for example, by a grinding operation, and a mark is placed at the geometric center of the disk. A coil is then wound about the periphery of the disk. As a consequence, the mark at the geometric center of the disk coincides with the electrical center point of the coil, thus obviating the need for a bobbin, or coil former, on which the coil can be wound.The transparent disk is first ground into a round shape, and a metallic film is deposited on a surface of the disk. The film is coated with a photosensitive resist material, and then exposed through a mask to define an image of a mark at the geometric center of the disk. The film is then etched to remove all but the mark from the disk.In manufacturing the coil, the disk, is concentrically clamped between two plates of a winding jig, each plate having annular peripheral flanges that are radially larger than the disk and thus project beyond the periphery of the disk.
Abstract: Novel cannabinol derivatives are provided which can be used in improved immunoassays for the detection in blood or urine samples of cannabinol metabolites.
Type:
Grant
Filed:
January 27, 1987
Date of Patent:
May 23, 1989
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Alan J. McNally, Alan Schwartz, Magdalena Usategui
Abstract: The invention is concerned with novel heterocyclic compounds of the formula ##STR1## wherein R is C.sub.1-12 -alkyl, C.sub.3-12 -alkenyl, C.sub.3-12 -alkynyl or C.sub.3-8 -cycloalkyl and X signifies oxygen or sulfur, and none of the possible multiple bonds of R is present in the .alpha.-position of X, and their acid addition salts, processes for their manufacture, pest control compositions which contain these compounds as the active substance as well as the use of such compounds or compositions for the control of pests. Moreover, the invention is concerned with starting materials used for the preparation of such compounds.
Abstract: The novel sunscreen agents which are esters, namely esters of p-methoxy-cinnamic acid with d,1-.alpha.-tocopherol, pantolactone or panthenol.
Type:
Grant
Filed:
August 24, 1987
Date of Patent:
May 23, 1989
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Gustav Erlemann, Christian Fizet, Horst Pauling
Abstract: An asymmetric synthesis for Vitamin E in an optically active pure form for 4-(2,5-diloweralkanoyloxy)-3,4,6-trimethylphenyl-butan-2-one and intermediates therein.
Abstract: Compounds of the formula ##STR1## wherein A is one of the following: ##STR2## in which R.sub.1, is acyl, R.sub.2 is hydrogen, lower alkyl, lower alkoxycarbonyl or aminocarbonyl, R.sub.3 is hydrogen or lower alkyl and R.sub.4 and R.sub.4 ' are hydrogen, lower alkyl, lower alkoxy, acyl or aralkyl, as well as pharmaceutically acceptable salts of such compounds, are useful as antibacterial agents.
Type:
Grant
Filed:
July 10, 1987
Date of Patent:
May 16, 1989
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Harry A. Albrecht, Frederick M. Konzelmann, Dennis D. Keith