Patents Represented by Attorney Jon S. Saxe

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  • Process for the preparation of 1.alpha.,23,25-trihydroxycholecalciferol-26-oic acid 23,26-lactone
    Patent number: 4632784
    Abstract: The invention is directed to a process and intermediates for the preparation of 1.alpha., 23,25-trihydroxycholecalciferol-26-oic acid 23,26-lactone.
    Type: Grant
    Filed: July 30, 1984
    Date of Patent: December 30, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Enrico G. Baggiolini, Milan R. Uskokovic, Peter M. Wovkulich
  • N-substituted diphenylpiperidines and antiobesity use thereof
    Patent number: 4632925
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is ##STR2## the asterisk denotes the specific bonding orientation to the piperidine moiety; R.sub.2 is alkylene or --CO--(CH.sub.2).sub.n -- wherein n is 0 to 11; R.sub.3 and R.sub.4, independently, are hydrogen, halogen or lower alkoxy; and HET is pyridinyl, pyrimidinyl or imidazolyl, and salts thereof with pharmaceutically acceptable acids, are described. The compounds of formula I exhibit insulin lowering activity and are useful as antiobesity agents.
    Type: Grant
    Filed: October 7, 1985
    Date of Patent: December 30, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: John G. Mullin, Jr., Richard W. Kierstead, Joseph Triscari
  • Blood particle analyzer
    Patent number: 4633169
    Abstract: A method for the analysis of particles in suspension in a fluid having a conductivity different from that of the particles, in particular a method for the analysis of blood particles is disclosed. The method includes the following steps: passing the fluid through an orifice, applying an electronic signal across the orifice, and producing electronic pulses corresponding to the changes in the signal level caused by the passage of the particles through the orifice. The invention is also concerned with a device for carrying out the method.
    Type: Grant
    Filed: June 28, 1984
    Date of Patent: December 30, 1986
    Assignee: Kontron Holding AG
    Inventors: Philippe L. Degrave, Jean P. Lepage
  • Carcinoembryonic antigen determination
    Patent number: 4631254
    Abstract: Process for the determination of carcinoembryonic antigen (CEA) in a sample of serum or plasma. The process comprises contacting a slightly acidic buffered sample of the serum or plasma with hydrophilic silica at room temperature, separating the silica from the sample and carrying out a radioimmunoassay for carcinoembryonic antigen on said sample.
    Type: Grant
    Filed: September 6, 1985
    Date of Patent: December 23, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Nicholas A. Giorgio, John Krupey, Leonard T. Wilson
  • Benzonitriles
    Patent number: 4630896
    Abstract: Compounds of the formula: ##STR1## wherein one of X.sup.1 and X.sup.2 is --CH.sub.2 CH.sub.2 -- and the other is --CH.sub.2 CH.sub.2 -- or a single covalent bond,ring A is 1,4-phenylene or trans-1,4-cyclohexylene, andR.sup.1 is straight-chain C.sub.1 -C.sub.12 -alkyl or when positioned on a 1,4-phenylene ring R.sup.1 may also be straight chain C.sub.1 -C.sub.12 -alkoxy.
    Type: Grant
    Filed: May 29, 1984
    Date of Patent: December 23, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Martin Petrzilka, Alois Villiger
  • Ultrasonic imaging device
    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
  • Cyclohexanecarbonitriles
    Patent number: 4629581
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or straight-chain alkyl; R.sup.2 is --CN, --R, --COR, --COOR or when R.sup.2 is positioned on an aromatic ring R.sup.2 also can be --OR, --OOCR or --F; R is alkyl; A is a group with 1 to 4 six-membered rings, these rings being linked directly with one another and with ring B in each case via a single covalent bond or being linked at one or two positions also via --COO--, --OOC-- or --CH.sub.2 CH.sub.
    Type: Grant
    Filed: June 26, 1985
    Date of Patent: December 16, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Arthur Boller, Martin Petrzilka, Martin Schadt
  • Substituted 4-acetyl-3-hydroxyphenoxy alkanoic acids
    Patent number: 4628115
    Abstract: The invention relates to compounds of the formula ##STR1## wherein R is hydrogen or lower alkyl, Z is alkylene of 1 to 10 carbon atoms, --(C*H.sub.2).sub.3 --C.tbd.C--, --C*H.sub.2 --C.tbd.C--(CH.sub.2).sub.3 --, and --(CH.sub.2).sub.2 O].sub.n (CH.sub.2).sub.2 -- wherein n is an integer of 1 to 3, the carbon atom marked with an asterisk is linked to the phenoxy moiety,and salts thereof with pharmaceutically acceptable bases. The compounds of formula I are antagonists of slow reacting substance of anaphylaxis (SRS-A; leukotrienes C.sub.4, D.sub.4 and E.sub.4), which renders them useful as agents for the treatment of allergic conditions.
    Type: Grant
    Filed: March 25, 1985
    Date of Patent: December 9, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Matthew Carson, Ronald A. LeMahieu, William C. Nason
  • Carbamic acid esters
    Patent number: 4625048
    Abstract: Carbamic acid esters of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, X, and Y are as defined hereinafter, process for their preparation, as well as pesticidal compositions containing these compounds as the active ingredient and methods for using the pesticidal compositions for the control of pests are described.
    Type: Grant
    Filed: December 20, 1984
    Date of Patent: November 25, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Rene Zurfluh
  • Immunoassay for peptide and protein oligomers
    Patent number: 4623621
    Abstract: A convenient immunoassay for detecting the presence of oligomeric forms of peptides and proteins is described. The assay employs the sandwich technique with a monoclonal antibody selective for a single epitope on the peptide or protein bound to a solid phase and the same monoclonal antibody labeled with a detectable label in the solution phase.
    Type: Grant
    Filed: September 24, 1984
    Date of Patent: November 18, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Sidney Pestka
  • Peptide derivatives
    Patent number: 4623639
    Abstract: The present invention provides for peptide derivatives, a process for their manufacture and pharmaceutical preparations containing the same. The invention is also concerned with novel intermediates used in the manufacture of said derivatives.
    Type: Grant
    Filed: July 5, 1984
    Date of Patent: November 18, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Cedric H. Hassall, William H. Johnson, Noel A. Roberts
  • Novel liquid crystal mixtures
    Patent number: 4621901
    Abstract: Liquid crystalline mixtures containing compounds of the formula ##STR1## wherein n stands for the number 0 or 1; X.sup.1 and X.sup.2 denote single covalent bonds or one of the symbols X.sup.1 and X.sup.2 also denotes --COO--, --OOC-- or --CH.sub.2 CH.sub.2 --; the rings A.sup.1, A.sup.2, and A.sup.3 represent 1,4-phenylene, 2-fluoro-1,4-phenylene or trans-1,4-cyclohexylene or one of these rings also represents a 2,5-disubstituted pyrimidine ring or a trans-2,5-disubstituted m-dioxane ring; R.sup.1 signifies 4-alkenyl or on a cyclohexyl ring also 2Z-alkenyl; and R.sup.2 denotes alkyl, alkoxy, --CN or --NCS,as well as the manufacture of these compounds and the use for electro-optical purposes are described.
    Type: Grant
    Filed: June 26, 1985
    Date of Patent: November 11, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Martin Petrzilka, Martin Schadt
  • Growth hormone releasing factor analogs
    Patent number: 4622312
    Abstract: Novel growth hormone releasing factor analogs in which glycine at position 15 is replaced by appropriately selected amino acids demonstrate enhanced potency for the release of growth hormone and the analogs can be administered to a subject having a deficiency of growth hormone.
    Type: Grant
    Filed: September 24, 1984
    Date of Patent: November 11, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Arthur M. Felix, Edgar P. Heimer, Thomas F. Mowles
  • Beta lactams
    Patent number: 4619787
    Abstract: The novel compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, a residue readily removable by reduction, lower 1-hydroxyalkyl or lower alkanoyl andR.sup.2 is hydrogen, or each of R.sup.1 and R.sup.2 is a residue readily removable by reduction;R.sup.3 is hydrogen or lower alkyl;R.sup.4 is hydrogen or a readily removable protecting group; andA is lower alkylidene or (C.sub.5-7)-cycloalkylidene,are valuable intermediates for the manufacture of antimicrobially-active .beta.-lactams.
    Type: Grant
    Filed: November 13, 1984
    Date of Patent: October 28, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Erwin Gotschi, Christian Hubschwerlen
  • Chiral phosphines
    Patent number: 4620013
    Abstract: Novel chiral phosphines are disclosed which when complexed with rhodium provide catalyst compositions for asymmetric hydrogenations.
    Type: Grant
    Filed: June 14, 1985
    Date of Patent: October 28, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Emil A. Broger, Yvo Crameri
  • Method of treating disease states by the administration of 1.alpha.,25,26-trihydroxycholecalciferol
    Patent number: 4617297
    Abstract: The present invention relates to the method of treating disease states characterized by higher than normal levels of endogenously produced 1.alpha.,25 dihydroxy-cholecalciferol or conditions where there is an increased sensitivity to 1.alpha., 25 dihydroxy-cholecalciferol by administering to an organism suffering from such a disease state a pharmaceutically effective amount of the R or S epimer of 1.alpha.,25,26 trihydroxy-cholecalciferol.
    Type: Grant
    Filed: April 3, 1984
    Date of Patent: October 14, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alfred Boris, John J. Partridge, Milan R. Uskokovic
  • .beta.-lactams
    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
  • Imidazodiazepine derivatives
    Patent number: 4616010
    Abstract: Compounds which are imidazodiazepine derivatives of the formula ##STR1## wherein A together with the carbon atoms denoted by .alpha. and .beta. signifies the group ##STR2## one of R.sup.1 and R.sup.2 signifies hydrogen and the other signifies hydrogen, halogen or trifluoromethyl, R.sup.3 and R.sup.4 each signify hydrogen or halogen and n signifies the number 2 or 3, the compounds having the (S)- or (R,S)-configuration with reference to the carbon atom denoted by .gamma., and their pharmaceutically acceptable acid addition salts have been discovered which possess anxiolytic, anticonvulsant, muscle relaxant and sedative-hypnotic properties. They can be prepared into compositions, including pharmaceutically acceptable ones, using suitable inert carriers.
    Type: Grant
    Filed: February 20, 1986
    Date of Patent: October 7, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Walter Hunkeler, Emilio Kyburz
  • Naphthalenyloxy carboxylic acids
    Patent number: 4616091
    Abstract: Naphthalenyloxy carboxylic acids of the formula ##STR1## wherein X, R, m and n are as hereinafter set forth, are described. The compounds of formula I are antagonists of slow reacting substance of anaphylaxis (SRS-A), which renders them useful as agents for the treatment of allergic conditions.
    Type: Grant
    Filed: January 8, 1986
    Date of Patent: October 7, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Ronald A. LeMahieu
  • Peptide having immunopotentiating activity similar to thymosin alpha.sub.1
    Patent number: 4614731
    Abstract: A new biologically active polypeptide hormone has been isolated from calf thymosin fraction 5 and has been given the designation thymosin alpha.sub.11. The peptide contains seven additional amino acid residues at the carboxy terminus when compared to thymosin alpha.sub.1. Thymosin alpha.sub.11 is one of several peptides present in thymosin fraction 5 which participate in the regulation, differentiation and function of thymic dependent lymphocytes (T cells). The new peptide is approxomately 16 times as potent in the protection of subject animals against opportunistic infections as thymosin fraction 5 and approximately equal in potency to thymosin alpha.sub.1.
    Type: Grant
    Filed: June 10, 1985
    Date of Patent: September 30, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Bernard L. Horecker