Patents Represented by Attorney, Agent or Law Firm Richard J. Mazza
  • 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: 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: 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: 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
  • Patent number: 4732979
    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: January 21, 1987
    Date of Patent: March 22, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Werner Aschwanden, Rene Imhof, Roland Jakob, Emilio Kyburz
  • Patent number: 4721137
    Abstract: An apparatus for withdrawing liquid from a receptacle which is closed with a penetrable cover, which comprises a puncturing tool for creating an aperture in the receptacle cover, a cannula for entering the receptacle through the aperture and withdrawing liquid from the receptacle, a holding arm to which the puncturing tool and cannula are affixed in parallel and at a certain distance apart, and a motor drive for effecting horizontal and vertical movements of the holding arm relative to the covered receptacle to align, lower and raise the puncturing tool and cannula in succession through the cover.
    Type: Grant
    Filed: October 7, 1986
    Date of Patent: January 26, 1988
    Assignee: Kontron Holding A.G.
    Inventor: Paul Muller
  • Patent number: 4700009
    Abstract: The present disclosure is concerned with a novel process for the manufacture of substituted benzaldehydes, namely of benzaldehydes of the formula ##STR1## wherein R represents a methoxy or tert.butyl group. The compounds of formula I are known substances, useful as, e.g. intermediates.
    Type: Grant
    Filed: January 28, 1986
    Date of Patent: October 13, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Nosberger, Paul
  • Patent number: 4699986
    Abstract: There is presented optically uniform .beta.-lactams of the formulae ##STR1## wherein Z is a readily cleavable acyl group, R.sup.1 is amino or a group convertible into amino, R.sup.2 is hydrogen or a readily cleavable protecting group and R.sup.3 and R.sup.4 each are a lower hydrocarbon group which optionally contains oxygen and which is attached via a carbon atom, whereby these groups can also be joined with one another to form a ring, with the proviso that R.sup.1 is a readily cleavable acylamino when R.sup.2 is hydrogen,and the corresponding optical antipodes, their manufacture and use in the manufacture of antimicrobially-active .beta.-lactams as well as novel intermediates usable in their manufacture.
    Type: Grant
    Filed: August 26, 1985
    Date of Patent: October 13, 1987
    Assignee: Hofmann-La Roche Inc.
    Inventors: Christian N. Hubschwerlen, Gerard Schmid
  • Patent number: 4689227
    Abstract: The antibacterially-active substance composition consisting of mecillinam and (2S,3S)-3-((Z)-2-(2-amino-4-thiazolyl)-2-((carboxymethoxy)imino)acetamido) -2-((carbamoyloxy)methyl-4-oxo-1-azetidinesulphonic acid (compound A), or pro-drugs and/or pharmaceutically usable salts thereof, has a pronounced synergism against Enterobacter strains which are resistant to mecillinam and which are only moderately sensitive to compound A.
    Type: Grant
    Filed: July 24, 1986
    Date of Patent: August 25, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Peter Angehrn
  • Patent number: 4680408
    Abstract: There are presented compounds of the formula ##STR1## wherein R.sup.1 is one of the 3-substituents usable in cephalosporin chemistry, R.sup.2 is hydrogen, lower alkyl or COOR.sup.3 -lower alkyl, wherein R.sup.3 is hydrogen, a cation of a base or a readily hydrolyzable ester group, and X is sulphur, oxygen or one of the groups --SO-- and --SO.sub.2 --, and the readily hydrolyzable esters, readily hydrolyzable ethers and salts of these compounds and hydrates of the compounds of formula I or of their esters, ethers and salts, also presented are methods for the manufacture of these compounds as well as compounds used in their manufacture.
    Type: Grant
    Filed: June 9, 1986
    Date of Patent: July 14, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Roland Reiner, Urs Weiss
  • Patent number: 4672033
    Abstract: There is presented antibiotic compounds designated as Antibiotics X-14889 A, C and D of the formulas ##STR1## wherein (for X-14889A) R.sub.1 is methyl, R.sub.2 is methyl, R.sub.3 is hydrogen, R.sub.4 is methyl and R.sub.5 is hydrogen or (for X-14889C) R.sub.1 is hydrogen, R.sub.2 is methyl, R.sub.3 is hydrogen, R.sub.4 is methyl and R.sub.5 is CO.sub.2 H or ##STR2## and the pharmaceutically acceptable salts thereof. The compounds exhibit antimicrobial activity and one of the compounds X-14889C also exhibits activity against Treponema hyodysenteriae (in vitro), Plasmodium berghei and as food efficiency enhancers in ruminants.Also presented is a process to produce the above compounds and another known component Antibiotic X-14889B.
    Type: Grant
    Filed: May 23, 1985
    Date of Patent: June 9, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Chao-Min Liu, John Westley
  • Patent number: 4659735
    Abstract: Heterocyclic compounds of the formula ##STR1## wherein X is --CH.dbd.CH--, --O--or --S--; R.sup.1 is a group Ar--R.sup.2 or --CH.dbd.CH--C(CH.sub.3).dbd.CH--R.sup.21 ; Ar is phenyl, pyridyl, furyl or thienyl; R.sup.2 is a group --CO.sub.2 R.sup.3, --C(O)R.sup.4, --CH.sub.2 OR.sup.3, lower-alkylsulphonyl or formyl; R.sup.21 is a group --CO.sub.2 R.sup.3, --C(O)R.sup.4, --CH.sub.2 OR.sup.3 or formyl; R.sup.3 is hydrogen or lower-alkyl and R.sup.4 is hydrogen, hydroxy, amino, lower alkylamino, di-(lower alkyl)amino or lower-alkyl; at least one ring of the molecule being heterocyclic, salts thereof, processes for their preparation, rodenticidal compositions containing these compounds as the active ingredient and methods of use of the rodenticidal compositions are disclosed.
    Type: Grant
    Filed: April 19, 1985
    Date of Patent: April 21, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Klaus, Peter Loeliger, Harald Weiser
  • Patent number: 4652651
    Abstract: The manufacture of 1-sulpho-2-oxazetidine derivatives of the formula ##STR1## in which Het is an optionally amino-substituted, 5- or 6-membered, aromatic heterocycle containing 1 or 2 nitrogen atoms and optionally also an oxygen or sulphur atom, R.sup.1 is hydrogen, lower alkyl, phenyl-lower alkyl, lower alkanoyl, lower alkoxycarbonyl, lower alkenyl-lower alkyl, lower alkoxycarbonyl-lower alkyl, phenyl-lower-alkoxycarbonyl-lower alkyl, nitrophenyl-lower-alkoxycarbonyl-lower alkyl or carboxy-lower alkyl and R.sup.2 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower alkoxycarbonyl, lower alkanoyloxy-lower alkyl, lower alkoxycarbonyl-lower alkenyl, hydroxyiminomethyl, lower alkoxyiminomethyl, carbamoyl, carbamoyl-lower alkenyl or carbamoyloxy-lower alkyl, the group .dbd.NOR.sup.
    Type: Grant
    Filed: April 14, 1986
    Date of Patent: March 24, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Andre Furlenmeier, Werner Hofheinz, Christian N. Hubschwerlen, Hans P. Isenring
  • Patent number: 4642318
    Abstract: The total radiation load on a subject being treated for psoriasis with a psoralen in conjunction with ultraviolet A radiation (PUVA) can be substantially reduced by at least pretreating said subject with an anti-psoriatic effective polyene compound such as a retinoid, .beta.-carotene or phytoene.
    Type: Grant
    Filed: June 21, 1985
    Date of Patent: February 10, 1987
    Inventor: Klaus Wolff
  • Patent number: 4639135
    Abstract: A cuvette arrangement for use in a chemical analysis system, which cuvette arrangement comprises an integrally constructed unit which defines separate chambers, for the receipt of sample-reagent mixtures.
    Type: Grant
    Filed: February 19, 1985
    Date of Patent: January 27, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Claude Borer, Andreas Greter
  • Patent number: 4628738
    Abstract: An ultrasonic imaging apparatus for operation in either or both linear and sector scan modes is disclosed which employs a common array of transducers. Circuitry is provided for controlling the order and timing of pulse echo transmission and reception, which further include control circuitry to operate variable delay and switching circuitry to generate transmission signals to be applied to the transducers, and to direct echo signals received by the transducers for processing to provide the image of the structures being inspected. Suitable interconnection/switching circuitry is provided so as to minimize prior art requirements for use of different elements for the separate scanning modes, with concomitant expenses associated with the larger number of components being reduced.
    Type: Grant
    Filed: February 19, 1986
    Date of Patent: December 16, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Christoph B. Burckhardt, Rainer Fehr, Peter Krummenacher
  • Patent number: 4617150
    Abstract: There is presented optically uniform .beta.-lactams of the formulae ##STR1## wherein Z is a readily cleavable acyl group, R.sup.1 is amino or a group convertible into amino, R.sup.2 is hydrogen or a readily cleavable protecting group and R.sup.3 and R.sup.4 each are a lower hydrocarbon group which optionally contains oxygen and which is attached via a carbon atom, whereby these groups can also be joined with one another to form a ring, with the proviso that R.sup.1 is a readily cleavable acylamino when R.sup.2 is hydrogen,and the corresponding optical antipodes, their manufacture and use in the manufacture of antimicrobially-active .beta.-lactams as well as novel intermediates usable in their manufacture.
    Type: Grant
    Filed: August 26, 1985
    Date of Patent: October 14, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Christian N. Hubschwerlen, Gerard Schmid