Patents Represented by Attorney Bernard S. Leon
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Patent number: 4772718Abstract: 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: GrantFiled: October 24, 1986Date of Patent: September 20, 1988Assignee: Hoffmann-La Roche Inc.Inventor: Paul Nosberger
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Patent number: 4772258Abstract: 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: GrantFiled: October 15, 1987Date of Patent: September 20, 1988Assignee: Kontron Holding A.G.Inventors: Daniele Marangoni, Corrado Vassanelli
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Patent number: 4772254Abstract: 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: GrantFiled: December 3, 1986Date of Patent: September 20, 1988Assignee: Kontron Holding A.G.Inventors: Alfred Grassl, Erhard Knorr
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Patent number: 4770503Abstract: 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: GrantFiled: May 27, 1987Date of Patent: September 13, 1988Assignee: Hoffmann-LaRoche Inc.Inventors: Richard Buchecker, Martin Schadt
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Patent number: 4766133Abstract: (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: GrantFiled: August 6, 1986Date of Patent: August 23, 1988Assignee: Hoffman-La Roche Inc.Inventors: Albert Fischli, Anna Krasso, Andre Szente
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Patent number: 4764522Abstract: 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: GrantFiled: August 16, 1985Date of Patent: August 16, 1988Assignee: Hoffmann-La Roche Inc.Inventors: Rene Imhof, Emilio Kyburz
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Patent number: 4762924Abstract: 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: GrantFiled: June 15, 1987Date of Patent: August 9, 1988Assignee: Hoffmann-La Roche Inc.Inventors: Cedric H. Hassall, Geoffrey Lawton, Sally Redshaw
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Patent number: 4760059Abstract: 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: GrantFiled: August 5, 1985Date of Patent: July 26, 1988Assignee: Hoffmann-La Roche Inc.Inventors: Charanjit Behl, Joel Unowsky
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Patent number: 4757824Abstract: 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: GrantFiled: August 15, 1986Date of Patent: July 19, 1988Assignee: Kontron Holding A.G.Inventor: Serge G. J. Chaumet
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Patent number: 4757069Abstract: 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: GrantFiled: November 24, 1987Date of Patent: July 12, 1988Assignee: Hoffmann-La Roche Inc.Inventors: Geoffrey Lawton, Sally Redshaw
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Patent number: 4751846Abstract: 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: GrantFiled: October 3, 1986Date of Patent: June 21, 1988Assignee: Kontron Holding A.G.Inventor: Bruno Dousse
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Patent number: 4749710Abstract: 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: GrantFiled: May 1, 1985Date of Patent: June 7, 1988Assignee: Hoffmann-La Roche Inc.Inventors: Gary A. Truitt, William R. Benjamin, Bruce H. Devens, Maurice K. Gately
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Patent number: 4749791Abstract: 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: GrantFiled: November 18, 1987Date of Patent: June 7, 1988Assignee: Hoffmann-La Roche Inc.Inventors: Werner Aschwanden, Rene Imhof, Roland Jakob, Emilio Kyburz
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Patent number: 4745076Abstract: 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: GrantFiled: September 9, 1985Date of Patent: May 17, 1988Assignee: Hoffmann-La Roche Inc.Inventors: Francis Muller, Dieter Schmidt
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Patent number: 4743687Abstract: 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: GrantFiled: June 23, 1986Date of Patent: May 10, 1988Assignee: Hoffmann-La Roche Inc.Inventors: Geoffrey Lawton, Sally Redshaw
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Patent number: 4743604Abstract: 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: GrantFiled: November 1, 1984Date of Patent: May 10, 1988Assignee: Hoffmann-La Roche Inc.Inventors: Leo Alig, Marcel Muller
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Patent number: 4742069Abstract: 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: GrantFiled: June 17, 1985Date of Patent: May 3, 1988Assignee: Hoffmann-La Roche Inc.Inventors: Roland Jaunin, Henri Ramuz
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Patent number: 4739049Abstract: 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: GrantFiled: August 15, 1986Date of Patent: April 19, 1988Assignee: Hoffmann-La Roche Inc.Inventors: Robert Y. Ning, Pradeep B. Madan
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Patent number: 4735940Abstract: 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: GrantFiled: October 31, 1985Date of Patent: April 5, 1988Assignee: Hoffmann-La Roche Inc.Inventors: Ulf Fischer, Fernand Schneider, Ulrich Widmer
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Patent number: 4734367Abstract: 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: GrantFiled: November 23, 1984Date of Patent: March 29, 1988Assignee: Hoffmann-La Roche Inc.Inventors: Hans G. W. Leuenberger, Peter K. Matzinger, Dieter Seebach, Max F. Zuger