Abstract: Compounds of the formula: ##STR1## wherein R.sub.1 is phenyl substituted with 1 to 3 substituents selected from the group consisting of lower alkoxy and halogen; R.sub.2 is hydroxy, lower alkoxy, lower alkanoyloxy, lower cycloalkylcarbonyloxy; ##STR2## or ##STR3## R.sub.3 and R.sub.4 are independently lower alkyl, phenyl lower alkyl or together form a piperidine or pyrrolidine ring; n is 2 to 4; m is 1 to 2; or pharmaceutically acceptable acid addition salts thereof are described. The compounds of formula I have activity as calcium channel blockers and accordingly, are useful as agents for lowering blood pressure, and as agents for treating ischemia.
Abstract: In this process of the invention a compound of the formula ##STR1## wherein R is a leaving group, is reacted with a compound of the formula ##STR2## wherein R.sup.1 is an ether protecting group, and, if desired a thus-obtained compound of the formula ##STR3## is converted in a known manner into d-.alpha.-tocopherol.
Abstract: This invention is directed towards methods for treating patients having a psychotic illness such as schizophrenia and/or inhibiting the occurrence of movement disorders in patients receiving or having received a neuroleptic medication by administering to the patients a pharmaceutically effective amount of a retinoid, such as retinoic acid, and particularly isotretinoin.
Abstract: Compounds of the formula ##STR1## wherein R is lower-alkyl, R.sup.1 is halogen, R.sup.2 is C.sub.1 -C.sub.12 -alkyl, R.sup.3 is hydroxy, lower-alkoxy, lower-alkyl-carbonyloxy, lower-alkoxy-lower-alkylcarbonoyloxy, lower-alkylaminocarbonyloxy, arylaminocarbonyloxy or aryl-lower alkylaminocarbonyloxy, X is C.sub.1 -C.sub.18 -alkylene which optionally can be interrupted by 1,4-phenylene or interrupted or lengthened by 1,4-cyclohexylene, A is di- or tri-substituted 2-imidazolyl attached via an ethylene group or a substituted or unsubstituted heterocycle selected from the group consisting of benzimidazolyl, benzimidazolonyl, imidazo[4,5-c]pyridinyl, imidazo[4,5-c]pyridinonyl, benzthiazolyl, benzodiazepine-2,5-dion-1-yl and pyrrolo[2,1-c]-[1,4]benzodiazepine-5,11-dion-10-yl and n is the number 0 or 1, in the form of racemates and optical antipodes, as well as N-oxides and pharmaceutically usable acid addition salts thereof.
Type:
Grant
Filed:
November 10, 1987
Date of Patent:
February 28, 1989
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Quirico Branca, Roland Jaunin, Hans P. Maki, Franzi Marti, Henri Ramuz
Abstract: 16-Cycloalkyl-7-fluoro prostacyclins having a 16 lower alkyl or fluoro substituent useful as blood platelet anti-aggregating agent, vasodilators, cyto protective lowering agents, anti-ulcerogenic agent and for treating peripheral vascular diseases such as schleroderma.
Type:
Grant
Filed:
December 1, 1986
Date of Patent:
February 28, 1989
Assignee:
Hoffmann-La Roche Inc.
Inventors:
George W. Holland, Perry Rosen, Hans Maag, Ferdinand Lee
Abstract: The pharmaceutically acceptable salts corresponding to the imidazolium hydrogen carbonates of the formula ##STR1## wherein the symbol Q is arylene or heteroarylene, the group --NR.sup.1 R.sup.2 is a basic amino group, R.sup.3 is hydrogen, lower alkyl, lower hydroxyalkyl, lower alkoxyalkyl, lower haloalkyl, lower alkylthio, lower alkoxy or the group --(A).sub.n --Ra, R.sup.4 is a saturated or partially unsaturated lower hydrocarbon group, a basic amino group or the group --N.dbd.CRc--Rb, --CHRcRd, --NH--CHRcRd, --NH--CO--Re or --CHRc--CO--Re, R.sup.5 is hydrogen, lower alkyl, lower hydroxyalkyl, lower alkoxyalkyl, lower haloalkyl, aryl or a fused benzene ring, R.sup.
Abstract: Use of compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5, independently are hydrogen, alkyl, or C.sub.3-7 -cycloalkyl or two adjacent residues R.sup.1 to R.sup.5 taken together with adjacent carbons of the phenyl ring form a 5- to 7-membered ring optionally substituted by one or more lower alkyl groups; X is --NR.sup.7 --CO-- or --CO-NR.sup.7 --; R.sup.6 is hydroxy, lower-alkoxy or --NR.sup.8 R.sup.9 ; and R.sup.7, R.sup.8 and R.sup.9, independently, are hydrogen or lower-alkyl, and where R.sup.6 is hydroxy, their pharmaceutically usable salts, for the treatment of inflammatory and rheumatic diseases.
Abstract: An ampule opener is provided for automatically opening ampules. The ampule opener is especially suitable for use in a robotic sterility test system and is provided with a pneumatic actuator means releasably connected to an ampule opener arm. The head of an ampule is positioned with its neck on a knife edge so that when the ampule opener arm is rotated by the actuator means, the arm applies a pressure on the head of the ampule and the ampule head drops away.
Abstract: Tetracyclic compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, X, Y, Z and n are as herein described, and salts thereof, are described. The compounds of formula III have antibacterial activity, and are therefore useful as antibacterial agents.
Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or hydroxy and R.sub.2 is hydrogen or fluorine are described. The compounds of formula I are useful as agents in the treatment of disease states characterized by metabolic calcium deficiencies. Examplary of such disease states are osteoporosis and renal osteodystrophy.
Type:
Grant
Filed:
January 20, 1988
Date of Patent:
February 14, 1989
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Enrico G. Baggiolini, John J. Partridge, Shian-Jan Shiuey, Gary A. Truitt, Milan R. Uskokovic
Abstract: This invention relates to the microbial production, via recombinant DNA technology, of new human leukocyte interferons, Le IF-K and Le IF-L for use in the treatment of viral and neoplastic diseases, and to the means and end products of such production.
Type:
Grant
Filed:
June 1, 1987
Date of Patent:
January 31, 1989
Assignees:
Hoffmann-La Roche Inc., Genentech, Inc.
Abstract: The invention is concerned with tricyclic compounds of the formula ##STR1## wherein R.sup.1 is a hydrogen atom or a carboxy-protecting radical; R.sup.2 is a hydrogen atom or a lower alkyl radical which may be substituted with a halogen atom; R.sup.3 and R.sup.4 independently are a hydrogen atom or a lower alkyl radical which may be substituted with a hydroxy radical or a substituted or unsubstituted amino radical; X is a halogen atom; and R.sup.5 and R.sup.6 are independently a hydrogen atom or a lower alkyl radical which may be substituted with a hydroxy radical, a lower alkoxy radical or a substituted or unsubstituted amino radical; or R.sup.5 and R.sup.6, taken together with the adjacent nitrogen atom, may form a 5 to 7 membered heterocyclic ring which may be substituted with one or more substituents at the carbon atom(s), and the heterocyclic ring may further contain --NR.sup.7 --, --O--, --S--, --SO--, --SO.sub.2 -- or --NR.sup.7 --CO--, and also R.sup.
Abstract: A method for measuring chloride ion concentration in a sample of body fluid, e.g., serum or plasma is described in which a sample blank is made in the same cuvette after the test measurement has been made.
Abstract: Pyridine-ethanolamines of the formula ##STR1## wherein n, X, Y, R.sup.1, R.sup.2 and R.sup.3 have the significances given in the description, their corresponding enantiomers, diastereomers, and racemates as well as the pysiologically compatible salts thereof are describe. The compounds of formula I have catabolic activity and can be used for the treatment of obesity and of diabetes mellitus or of conditions which are associated with an increased protein breakdown, or as feed additives for fattening animals. The compounds of formula I can be prepared by alkylating the primary or secondary amines corresponding to the secondary or tertiary amines of formula I.
Abstract: Novel diaryl ethers of the formula ##STR1## wherein A is CR.sup.3 or N and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, n and R.sup.6 are as defined hereinafter, processes for their preparation, herbicidal compositions which contain these compounds as the active ingredient as well as the use of these compounds or compositions for the control of weeds is disclosed.
Abstract: 2,4-Diamino-5-benzylpyrimidines of the formula ##STR1## wherein R.sup.1, R.sup.2, A, Z and n are as hereinafter set forth, are described. The 2,4-diamino-5-benzylpyrimidines of the invention have useful antibacterial activity. More particularly, they inhibit bacterial dihydrofolate reductase and potentiate the antibacterial activity of sulfonamides.
Type:
Grant
Filed:
January 14, 1987
Date of Patent:
December 20, 1988
Assignee:
Hoffman-La Roche Inc.
Inventors:
Ivan Kompis, G/e/ rald Rey-Bellet, Guido Zanetti
Abstract: A combined sensor for sensing partial O.sub.2 pressure and partial CO.sub.2 pressure and comprising measuring electrodes, a reference electrode, a diaphragm covering the electrodes and an electrolyte layer between the electrodes and the diaphragm wherein the reference electrode has disposed around it a screening of gold which is at the same potential as the reference electrode and the electrolyte contains a defined concentration of a soluble silver compound or of a silver complex.
Type:
Grant
Filed:
January 25, 1988
Date of Patent:
December 6, 1988
Assignee:
Kontron Holding A.G.
Inventors:
Patrick Eberhard, Wolfgang Mindt, Jean-Pierre Palma