Patents Represented by Attorney Bernard S. Leon
  • Patent number: 4772718
    Abstract: A process for the manufacture of 5-cyano-4-methyl-oxazole which comprises reacting a 5-(lower alkoxycarbonyl)-4-methyl-oxazole with ammonia in the gaseous phase, in the presence of a zirconium oxide or hafnium oxide catalyst.
    Type: Grant
    Filed: October 24, 1986
    Date of Patent: September 20, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Paul Nosberger
  • Patent number: 4772258
    Abstract: There is disclosed an angioplasty catheter having a drilling head disposed within its distal end. The drilling head having a rotatable drilling tool and means for temporary closing a blood vessel. A shaft position within the interior of the catheter is attached and drives the drilling tool. A pneumatic turbine is connected to the proximal end of the catheter and to the shaft for driving the shaft in drive tool and suctioning material removed by the drive tool.
    Type: Grant
    Filed: October 15, 1987
    Date of Patent: September 20, 1988
    Assignee: Kontron Holding A.G.
    Inventors: Daniele Marangoni, Corrado Vassanelli
  • Patent number: 4772254
    Abstract: A centrifuge having an interchangeable rotor provided with an information support means for machine-readable information, and a reader comprising detectors for scanning the information support means and an electronic circuit for processing the received information, the information support means comprising an array of permanent magnet pins distributed over the rotor and having in some cases their north poles and in other cases their south poles facing the detectors.
    Type: Grant
    Filed: December 3, 1986
    Date of Patent: September 20, 1988
    Assignee: Kontron Holding A.G.
    Inventors: Alfred Grassl, Erhard Knorr
  • Patent number: 4770503
    Abstract: Compounds of the formula ##STR1## wherein m stands for a whole number of 4-7 and n stands for 0 or a positive whole number; ring A represents trans-1,4-cyclohexylene or a 2,5-disubstituted pyrimidine ring; Z signifies a single covalent bond or, insofar as ring A represents trans-1,4-cyclohexylene, also the ethylene group --CH.sub.2 CH.sub.2 --; X denotes hydrogen or fluorine; and R represents the group --NCS or --CN,their manufacture, liquid crystalline mixtures which contain these compounds and the use of these compounds and mixtures for electro-optical purposes are described.
    Type: Grant
    Filed: May 27, 1987
    Date of Patent: September 13, 1988
    Assignee: Hoffmann-LaRoche Inc.
    Inventors: Richard Buchecker, Martin Schadt
  • Patent number: 4766133
    Abstract: (Benzimidazol-2-yl)-pyridinium compounds of the formula ##STR1## wherein A is --SR.sup.9, --SO.sub.3.sup.- or --S--SO.sub.3.sup.- ; R.sup.1 and R.sup.3 each is hydrogen or (C.sub.1 -C.sub.7)-alkyl; R.sup.2 is hydrogen, (C.sub.1 -C.sub.7)-alkyl, (C.sub.1 -C.sub.7)-alkoxy or a negatively charged oxygen atom; R.sup.4 is hydrogen or a negative charge; R.sup.5, R.sup.6, R.sup.7 and R.sup.8 each is hydrogen, (C.sub.1 -C.sub.7)-alkyl, aryl, halogen, cyano, nitro, formyl, (C.sub.2 -C.sub.7)-alkanoyl, arylcarbonyl, carboxy, carboxy-(C.sub.1 -C.sub.7)-alkyl, (C.sub.1 -C.sub.7)-alkoxycarbonyl, aryloxycarbonyl, aryl-(C.sub.1 -C.sub.7)-alkoxycarbonyl, (C.sub.1 -C.sub.7)-alkoxycarbonyl-(C.sub.1 -C.sub.7)-alkyl, carbamoyl, mono- or di-(C.sub.1 -C.sub.7)-alkylcarbamoyl, pyrrolidinocarbonyl, piperidinocarbonyl, carbamoyl-(C.sub.1 -C.sub.7)-alkyl, mono- or di-(C.sub.1 -C.sub.7)-alkylcarbamoyl-(C.sub.1 -C.sub.7)-alkyl, pyrrolidinocarbonyl-(C.sub.1 -C.sub.7)-alkyl, piperdinocarbonyl-(C.sub.1 -C.sub.7)-alkyl, hydroxy, (C.sub.
    Type: Grant
    Filed: August 6, 1986
    Date of Patent: August 23, 1988
    Assignee: Hoffman-La Roche Inc.
    Inventors: Albert Fischli, Anna Krasso, Andre Szente
  • Patent number: 4764522
    Abstract: Compounds of the formula ##STR1## wherein R is an aromatic, 5- or 6-membered heterocyclic residue, as described herein, and their pharmaceutically usable acid addition salts are described. These compounds have interesting monoamine oxidase inhibiting properties with low toxicity and can accordingly be used for the treatment of depressive states and parkinsonism.
    Type: Grant
    Filed: August 16, 1985
    Date of Patent: August 16, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Rene Imhof, Emilio Kyburz
  • Patent number: 4762924
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, alkanoyl or aroyl; R.sup.2 is hydrogen or alkyl; R.sup.3 is hydrogen or aryl; R.sup.4 and R.sup.5 each are hydrogen or R.sup.4 and R.sup.5 taken together are oxo; and Y is --CH.sub.2 --, --CH.sub.2 CH.sub.2 -- or --N(R.sup.6)-- in which R.sup.6 is hydrogen, alkyl or aralkyl,as well as pharmaceutically acceptable salts thereof with bases when R.sup.2 is hydrogen and pharmaceutically acceptable salts thereof with acids when Y is --N(R.sup.6)--, which have antihypertensive activity and can be used as medicaments in the form of pharmaceutical preparations, are described.The compounds of formula I contain at least one asymmetric carbon atom. Therefore, the invention comprises not only the optically uniform forms of these compounds, but also the various diastereoisomeric racemates and mixtures of different diastereoisomeric racemates.
    Type: Grant
    Filed: June 15, 1987
    Date of Patent: August 9, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Cedric H. Hassall, Geoffrey Lawton, Sally Redshaw
  • Patent number: 4760059
    Abstract: The rectal absorption of the beta-lactam antibiotic ceftriaxone in a solid dosage form is enhanced with chenodeoxycholic acid or its sodium salt, in the presence of a carrier consisting of a mixture of two or more glycerides of C.sub.12 to C.sub.18 fatty acids.
    Type: Grant
    Filed: August 5, 1985
    Date of Patent: July 26, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Charanjit Behl, Joel Unowsky
  • Patent number: 4757824
    Abstract: A method and an apparatus are provided for monitoring waveforms representing the respiration of a patient and for detecting waveforms having characteristics indicative of apnea. The method comprises processing a first electrical signal having a waveform representing the respiration of the patient and a second electrical signal representing the electrocardiogram of the patient.
    Type: Grant
    Filed: August 15, 1986
    Date of Patent: July 19, 1988
    Assignee: Kontron Holding A.G.
    Inventor: Serge G. J. Chaumet
  • Patent number: 4757069
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently represent hydrogen, C.sub.1 -C.sub.10 -alkyl, adamantyl-(C.sub.1 -C.sub.4 -alkyl) or (C.sub.2 -C.sub.6 -alkanoyloxy)-(C.sub.1 -C.sub.4 -alkyl), and pharmaceutically acceptable salts thereof possess antihypertensive activity and can be used as theraputic or prophylactic agents in pharmaceutical preparations. Intermediates for the production of such compounds are also provided.
    Type: Grant
    Filed: November 24, 1987
    Date of Patent: July 12, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Geoffrey Lawton, Sally Redshaw
  • Patent number: 4751846
    Abstract: Techniques are disclosed for producing improved ultrasonic cross-sectional images of a body subject to a number of consecutive and at least partly overlapping scans by the pulse echo method to produce digital image signals corresponding to the received echoes. The illustrated systems includes an ultrasonic transducer scanner energized by a transmitter, and a receiver configuration which processes the received echo signals for display on a TV monitor. To reduce the image-quality-limiting noise while retaining a satisfactory representation of moving parts in the zone under examination, image signals corresponding to corresponding scanning dots of consecutive scans are combined in the receiver circuit which utilizes time-discrete non-linear filtering with filter coefficients which vary as a function of the filter input signal. This arrangement and the related process produce improved images.
    Type: Grant
    Filed: October 3, 1986
    Date of Patent: June 21, 1988
    Assignee: Kontron Holding A.G.
    Inventor: Bruno Dousse
  • Patent number: 4749710
    Abstract: The invention relates to pharmaceutical compositions comprising at least one Vitamin D derivative and a method of using the pharmaceutical compositions in suppressing immune responses.
    Type: Grant
    Filed: May 1, 1985
    Date of Patent: June 7, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Gary A. Truitt, William R. Benjamin, Bruce H. Devens, Maurice K. Gately
  • Patent number: 4749791
    Abstract: Benzazecinediones of the formula ##STR1## wherein 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: November 18, 1987
    Date of Patent: June 7, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Werner Aschwanden, Rene Imhof, Roland Jakob, Emilio Kyburz
  • Patent number: 4745076
    Abstract: The invention relates to a ruthenium complex having the formulaRu.sup.2+ L.sub.1 L.sub.2 L.sub.3 Iwherein L.sub.1, L.sub.2 and L.sub.3 are the same or different are equal to a bi- or polycyclic ligand with at least two nitrogen-containing heterocycles, whereby at least one of these ligands is substituted with at least one group conferring water-solubility, and whereby at least one of these ligands is substituted, optionally via a spacer group, with at least one reactive group, and whereby the ligands L.sub.1, L.sub.2 and L.sub.3 are attached to the ruthenium via nitrogen atoms.The invention is further related to such ruthenium complexes having coupled thereto an immunologically active material, for example, antigens, haptens or antibodies and to the use of said ruthenium complexes in fluorescence spectroscopy. Specific ligands L.sub.1, L.sub.2 and L.sub.3 which are useful in the ruthenium complexes of the invention are, e.g.
    Type: Grant
    Filed: September 9, 1985
    Date of Patent: May 17, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Francis Muller, Dieter Schmidt
  • Patent number: 4743687
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 represents hydroxy, alkyl, aralkyl, aralkoxy-alkyl, hydroxy-alkyl, amino-alkyl, acylamino-alkyl, monoalkylamino-alkyl, dialkylamino-alkyl, alkoxycarbonylamino-alkyl, halo-alkyl, carboxy-alkyl, alkoxycarbonyl-alkyl, alkoxy or aralkoxy; R.sup.2 and R.sup.3 each represent hydrogen, alkyl or aralkyl; R.sup.4 and R.sup.5 each represent hydrogen or R.sup.4 and R.sup.5 together represent oxo; and X represents an oxygen atom or the group --NR.sup.6 -- in which R.sup.6 represents hydrogen, alkyl or aralkyl or --(CH.sub.2).sub.n -- in which n stands for zero, 1 or 2,and racemates, enantiomers, diastereoisomers or pharmaceutically acceptable salts thereof have antihypertensive activity and can be used as medicaments in the form of pharmaceutical preparations. They can be prepared according to known methods.Compounds useful as starting materials for producing the compounds of formula I are also provided.
    Type: Grant
    Filed: June 23, 1986
    Date of Patent: May 10, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Geoffrey Lawton, Sally Redshaw
  • Patent number: 4743604
    Abstract: The oxazolidines of the formula ##STR1## wherein n signifies the number 1 or 2,T signifies lower carbalkoxy,X signifies phenoxymethyl optionally mono-fluorinated or mono-chlorinated in the ortho-position or phenyl optionally monosubstituted by fluorine, chlorine, trifluoromethyl or lower-alkoxy,Y signifies hydrogen or methyl, andZ signifies a phenyl or thienyl residue substituted in a defined manner,and the physiologically compatible salts thereof have catabolic activity and can be used for the treatment of obesity and diabetes mellitus or for the treatment of conditions which are associated with an increased protein breakdown, or as feed additives for fattening animals. They are manufactured starting from corresponding primary amines.
    Type: Grant
    Filed: November 1, 1984
    Date of Patent: May 10, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Marcel Muller
  • Patent number: 4742069
    Abstract: Dihydropyridine derivatives of the formula ##STR1## wherein the symbols A, R and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are as described herein.Compounds of formula I have a pronounced calcium-antagonistic activity and can accordingly be used as medicaments, especially for the control or prevention of angina pectoris, ischemia, high blood pressure and/or migraine.
    Type: Grant
    Filed: June 17, 1985
    Date of Patent: May 3, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Roland Jaunin, Henri Ramuz
  • Patent number: 4739049
    Abstract: Compounds of the general formula ##STR1## are reacted with a strong base followed by a phosphorylating agent, such as dicyclicaminophosphinic halide or bis-di-lower alkylaminophosphinic halide to produce an imine of the formula ##STR2## wherein R is dicyclicaminophosphinyloxy or bis-di-lower alkylaminophosphinyloxy.R represents a leaving group which will undergo nucleophilic displacement with nitrogen, oxygen, sulfur and carbon containing nucleophiles, that is, nucleophiles which have, as a reactive site, a nitrogen, oxygen, sulfur or carbon atom, such that, when the cyclic imine undergoes nucleophilic displacement, there is formed C--N, C--O, C--S and C--C bonds between the carbon atom of the cyclic imine and the nucleophilic group.The end products may be utilized as intermediates in the production of pharmaceutically valuable compounds and, in some instances, are pharmaceutically valuable compounds per se.
    Type: Grant
    Filed: August 15, 1986
    Date of Patent: April 19, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Robert Y. Ning, Pradeep B. Madan
  • Patent number: 4735940
    Abstract: Compounds of the formula ##STR1## or a pharmaceutically acceptable acid addition salt of a compound of formula I which has one or more basic substituents, are described.The compounds of formula I possess pronounced muscle relaxant, sedative-hypnotic, anticonvulsive and anxiolytic properties and have low toxicity.
    Type: Grant
    Filed: October 31, 1985
    Date of Patent: April 5, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Ulf Fischer, Fernand Schneider, Ulrich Widmer
  • Patent number: 4734367
    Abstract: The manufacture of optically active compounds of the formula ##STR1## wherein R.sup.1 signifies alkyl, phenyl or benzyl and R.sup.2 signifies hydrogen or a customary ester residue,by the fermentative reduction of compounds of the formula ##STR2## wherein R.sup.1 and R.sup.2 have the above significance. The compounds obtained are valuable intermediates in organic syntheses.
    Type: Grant
    Filed: November 23, 1984
    Date of Patent: March 29, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Hans G. W. Leuenberger, Peter K. Matzinger, Dieter Seebach, Max F. Zuger