Patents Represented by Attorney Jon S. Saxe
  • Patent number: 4614723
    Abstract: There are described novel porphyrin derivatives of the general formula ##STR1## wherein either R.sup.1 signifies the group ##STR2## and R.sup.2 signifies the group ##STR3## or R.sup.1 signifies the group ##STR4## and R.sup.2 signifies the group ##STR5## whereby X.sup.- signifies a halogen ion, an arylsulphonate ion, an alkylsulphonate ion or an alkyl sulphate ion, A signifies (C.sub.1-8)-alkylene and R.sup.3 signifies (C.sub.1-4)-alkyl,and sulphonic acid salts of compounds of formula I in which R.sup.1 signifies the group ##STR6## as well as a process for their manufacture and intermediates used in this process.Because of their water-solubility the novel porphyrin derivatives are suitable as label molecules for highly sensitive fluorescence immuno-assays, especially for time-resolving fluorescence immuno-assays. The coupling of the novel porphyrin derivatives to immunologically-active materials is carried out in the customary manner, for example with a water-soluble carbodiimide derivative.
    Type: Grant
    Filed: May 23, 1984
    Date of Patent: September 30, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Dieter Schmidt, Hans Steffen
  • Patent number: 4613208
    Abstract: A liquid crystalline mixture comprising(a) at least one compound of the formula: ##STR1## wherein R.sup.1 is alkyl, alkoxy, p-alkylphenyl, p-alkoxyphenyl, trans-4-alkylcyclohexyl, 4'-alkyl-4-biphenylyl, p-(trans-4-alkylcyclohexyl)phenyl, 2-(trans-4-alkylcyclohexyl)ethyl or p-[2-(trans-4-alkylcyclohexyl)ethyl]phenyl and R.sup.2 is trans-4-alkylcyclohexyl; or R.sup.1 is trans-4-alkylcyclohexyl and R.sup.2 is p-(trans-4-alkylcyclohexyl)phenyl, p-[2-(trans-4-alkylcyclohexyl)ethyl]phenyl or 4'-(trans-4-alkylcyclohexyl)-4-biphenylyl; or R.sup.1 is p-alkylphenyl and R.sup.2 is p-[2-(trans-4-alkylcyclohexyl)ethyl]phenyl; and the alkyl and alkoxy groups in the substituents R.sup.1 and R.sup.2 are straight-chain groups of 1 to 7 carbon atoms, and;(b) at least one dichroic coloring substance selected from the group of compounds consisting of: ##STR2## wherein R.sup.3 is straight-chain C.sub.1 -C.sub.12 -alkyl and R.sup.4 is straight-chain C.sub.1 -C.sub.4 -alkyl, Z.sup.1 is hydrogen or chlorine, one of the symbols Z.
    Type: Grant
    Filed: November 18, 1983
    Date of Patent: September 23, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Arthur Boller, Alfred Germann, Martin Petrzilka, Martin Schadt
  • Patent number: 4613594
    Abstract: Novel hexafluoro-cholecalciferol compounds and processes for preparing such compounds are disclosed. Intermediates utilized in the preparation of such compounds and pharmaceutical preparations containing these compounds are also disclosed.
    Type: Grant
    Filed: November 16, 1984
    Date of Patent: September 23, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Enrico Baggiolini, Giacomo Pizzolato, Milan Uskokovic, Gary Truitt
  • Patent number: 4612324
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 each individually is hydrogen, or lower alkyl and R.sup.4 is hydroxy, lower alkoxy, aryl-(lower alkoxy), amino, mono(lower alkyl)amino or di(lower alkyl) amino,and pharmaceutically acceptable salts thereof which are useful in the treatment of degenerative joint diseases and of Wilson's disease are described.
    Type: Grant
    Filed: February 1, 1984
    Date of Patent: September 16, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Colin H. Cashin, Noel A. Roberts, Brian P. Tong
  • Patent number: 4612380
    Abstract: The prostacyclins 7-fluoro-6,9-epoxy-16-substituted-15-hydroxyprost-[4 or 5,13]-dienoic acids and esters useful as anti-secretory agents, blood pressure lowering agents, anti-ulcerogenic agents, anti-hypertensive agents, bronchodilation agents and for combating gastro-hyperacidity and as anti-blood platelet aggregating agents.
    Type: Grant
    Filed: September 9, 1985
    Date of Patent: September 16, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: George W. Holland, Perry Rosen, Hans Maag
  • Patent number: 4612308
    Abstract: The syntheses of 25,26-dehydro-1.alpha.,23S-dihydroxycholecalciferol, 25,26-dehydro-1.alpha.,23R-dihydroxycholecalciferol, and the epimeric mixture thereof which are useful as differentiation inducing agents and anti-proliferation agents are described, 25,26-dehydro-1.alpha.,23S-dihydroxycholecalciferol 25,26-dehydro-1.alpha.,23R-dihydroxycholecalciferol and the epimeric mixture thereof are useful for treating tumors and leukemia, and osteoporosis.
    Type: Grant
    Filed: November 29, 1984
    Date of Patent: September 16, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Enrico G. Baggiolini, Gary A. Truitt, Milan R. Uskokovic, Peter M. Wovkulich
  • Patent number: 4610989
    Abstract: A method of producing analgesia by administering an opiate alkaloid such as morphine, codeine, oxycodone or a pharmaceutically acceptable acid addition salt thereof together with a carbazole compound, 6-chloro-.alpha.-methyl-carbazole-2-acetic acid, or a salt thereof with a pharmaceutically acceptable base and composition therefor.
    Type: Grant
    Filed: July 31, 1985
    Date of Patent: September 9, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Herman W. Baruth, Jr., Leo Berger, Alfred J. Corraz, Jerry Sepinwall
  • Patent number: 4608372
    Abstract: A process for the preparation of the .beta.' form of the copper chelate of 8-hydroxyquinoline (copper oxinate), stabilized compositions containing said chelate, fungicidal compositions containing said chelate, and the methods for using said .beta.' form chelate or compositions for combatting fungi are disclosed.
    Type: Grant
    Filed: February 12, 1985
    Date of Patent: August 26, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bernard Muller, Rene Piat, Cornelis Rensing, Jean-Paul Trajin
  • Patent number: 4607051
    Abstract: Carbamic acid compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, X and Y are as hereinafter set forth, processes for their preparation, pesticidal compositions containing one or more of the carbamic acid compounds as the active ingredient and methods for using the pesticidal compositions for the control of pests, particularly insects, mites and nematodes, are described.
    Type: Grant
    Filed: August 4, 1983
    Date of Patent: August 19, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Rene Zurfluh
  • Patent number: 4605641
    Abstract: Novel vasoactive intestinal peptide analogs containing substitutions of appropriately selected amino acids at specific positions of the VIP molecule, with potent sustained bronchodilatory activity without cardiovascular side effects.
    Type: Grant
    Filed: October 9, 1984
    Date of Patent: August 12, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: David R. Bolin, Johannes A. Meienhofer, Iou-Iou Sytwu
  • Patent number: 4605656
    Abstract: Pyridine and pyrazine compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as hereinafter set forth and acid addition salts of these compounds, processes for their preparation, fungicidal compositions containing these compounds as the active ingredients and methods for the use of such compounds or compositions for combating fungi in agriculture and horticulture are disclosed.
    Type: Grant
    Filed: October 21, 1983
    Date of Patent: August 12, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Franz Dorn
  • Patent number: 4605744
    Abstract: 6-Amidinopenicillanic acid derivatives wherein one of the nitrogen atoms of the amidino group is part of a heterocyclic ring having on a side chain an unsubstituted heterocyclic ring containing 2 to 3 nitrogen atoms, and being useful as an antibiotic.
    Type: Grant
    Filed: May 20, 1985
    Date of Patent: August 12, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Chung-Chen Wei, Manfred Weigele
  • Patent number: 4605674
    Abstract: Antivirally active compounds of the formula ##STR1## wherein R.sup.1 represents hydroxy, acyloxy derived from an aliphatic acid having 2-18 carbon atoms or a heterocyclic carboxylic acid containing nitrogen atom(s), lower alkoxycarbonyloxy, aminoacyloxy or carboxyalkanoyloxy;R.sup.2 represents lower alkoxy;R.sup.3 represents hydrogen or lower alkoxy; andR.sup.4 represents phenyl which may be substituted by one or more substituents selected from the group consisting of lower alkyl, lower alkoxy, benzyloxy, allyloxy, alkylthio, dialkylamino, amino, cyano, hydroxy, halo and alkylenedioxy; or pyridyl, furyl, thienyl or pyrrolyl which may be substituted by lower alkyl,pharmaceutical compositions containing them and a process for the preparation of those compounds of formula I which are novel.
    Type: Grant
    Filed: April 24, 1984
    Date of Patent: August 12, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Morio Fujiu, Yasuji Suhara, Hideo Ishitsuka
  • Patent number: 4604284
    Abstract: An active fragment of human immune interferon and a method for the extraction and purification of this protein fragment is disclosed. This method permits the purification to homogenity of the active fragment of recombinant human immune interferon.
    Type: Grant
    Filed: September 20, 1983
    Date of Patent: August 5, 1986
    Assignees: Hoffmann-La Roche Inc., Takeda Chemical Industries Ltd.
    Inventors: Hsiang-Fu Kung, Hiromu Sugino, Susumu Honda
  • Patent number: 4603223
    Abstract: A novel process for the manufacture of quinone derivatives is described.In this process a compound of the formula ##STR1## is reacted with a compound of the formula ##STR2## and the resulting compound of the formula ##STR3## is subjected to a retro-Diels-Alder reaction. The substituents R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the significance given in the description.
    Type: Grant
    Filed: July 24, 1984
    Date of Patent: July 29, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: August Ruttimann, George H. Buchi
  • Patent number: 4601984
    Abstract: There are provided antibiotics X-14873 A, G and H of the formulas ##STR1## wherein for X-14873A, R.sub.1 is CO.sub.2 H and R.sub.2 is ##STR2## for X-14873G, R.sub.1 is hydrogen and R.sub.2 is ##STR3## and for X-14873H, R.sub.1 is hydrogen and R.sub.2 is ##STR4## The compounds exhibit antibiotic activity. Also disclosed is a process to produce the above compounds.
    Type: Grant
    Filed: June 30, 1983
    Date of Patent: July 22, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Chao-Min Liu, Homer D. Tresner, John Westley
  • Patent number: 4602036
    Abstract: Aluminium panthenolate and zinc panthenolate, their manufacture and use as topical medicaments are described.
    Type: Grant
    Filed: January 14, 1985
    Date of Patent: July 22, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alfred Hanck, Horst Pauling
  • Patent number: 4599316
    Abstract: An improved photometric method for the determination of inorganic phosphate in fluids is disclosed.The method makes use of two reagents, an acid reagent and an ammonium molybdate reagent. Utilizing these reagents, the method comprises the following steps:(a) forming a first mixture consisting of a sample fluid and acid reagent;(b) measuring the light absorbance of said first mixture;(c) forming a second mixture consisting of said first mixture and ammonium molybdate reagent;(d) measuring the light absorbance of said second mixture;(e) calculating the difference in light absorbance (.DELTA.A sample) between the light absorbances measured for said first and second mixtures; and,(f) determining the concentration of inorganic phosphate in said sample fluid by comparing the difference in light absorbance (.DELTA.A sample) for said sample fluid to the difference in light absorbance (.DELTA.A standard) for a standard fluid having a known concentration of inorganic phosphate, .DELTA.
    Type: Grant
    Filed: December 2, 1983
    Date of Patent: July 8, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Benjamin A. Hahn, Richard A. Kaufman, Alexander F. Wesolowski
  • Patent number: 4599336
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, lower cycloalkyl, lower alkoxy, hydroxy, halo, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, di-(C.sub.1 -C.sub.7) alkyl-N(CH.sub.2).sub.n O-- or 2-hydroxyethoxy; n is 2 to 7; R.sub.2 is hydrogen, lower alkyl or lower alkoxy; R.sub.3 is hydrogen or methyl; R.sub.4 is hydrogen or lower alkyl; R.sub.5 is hydrogen or lower alkyl provided however if R.sub.2 is other than hydrogen R.sub.5 is hydrogen; m is 1 to 7; Y is ##STR2## --O-- or --S--; w is zero or one; and A is an unsubstituted or substituted aromatic 5- or 6-membered heterocyclic radical;or pharmaceutically acceptable addition salts thereof are described. The compounds of formula I are useful for treating allergic conditions and vascular disorders.
    Type: Grant
    Filed: August 8, 1983
    Date of Patent: July 8, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Matthew Carson, Ronald A. Le Mahieu, William C. Nason, Jefferson W. Tilley
  • Patent number: 4599347
    Abstract: Tricyclic imidazole derivatives of the formula ##STR1## wherein R.sup.1 is 2-pyridyl optionally substituted by lower alkyl or lower alkoxy, n is the integer 0 to 1, R.sup.2 is hydrogen or lower alkyl, R.sup.3 and R.sup.4, independently, are hydrogen or lower alkyl, A is a group of the formula ##STR2## m is the integer 2 or 3, R.sup.5, R.sup.6, R.sup.7 and R.sup.8, independently, are hydrogen or lower alkyl, and R.sup.9 is hydrogen and R.sup.10 is hydrogen or lower alkyl or R.sup.9 and R.sup.10 taken together are oxo, provided that at least one of R.sup.3 and R.sup.4 is lower alkyl when A is a group of the formula--CH.dbd.CH--CH.dbd.CH-- or --(CH.sub.2).sub.4 --,and their pharmaceutically acceptable acid addition salts. The compounds of formula I inhibit gastric acid secretion and prevent the formation of gastric ulcers.
    Type: Grant
    Filed: December 12, 1983
    Date of Patent: July 8, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Anna Krasso, Henri Ramuz