Patents Represented by Attorney Jon S. Saxe
  • Patent number: 4831185
    Abstract: An asymmetric synthesis for Vitamin E in an optically active pure form for 4-(2,5-diloweralkanoyloxy)-3,4,6-trimethylphenyl-butan-2-one and intermediates therein.
    Type: Grant
    Filed: December 18, 1987
    Date of Patent: May 16, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Ka-kong Chan, Gabriel G. Saucy
  • Patent number: 4831151
    Abstract: Compounds of the formula ##STR1## wherein the various substituents are defined hereinbelow and the pharmaceutically acceptable acid addition salts thereof, possess pharmacological properties. In particular, they possess antibacterial, antimycotic, protozoacidal and/or anthelmintic properties.
    Type: Grant
    Filed: April 21, 1986
    Date of Patent: May 16, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Helmut Link, Marc Montavon, Eva M. Karpitschka, Wilhelm Klotzer, Renate Mussner
  • Patent number: 4826773
    Abstract: A reagent for determining quantitatively the amount of phosphorous in bodily fluids which comprises a surface active agent, a strong acid, ammonium molybdate, a heavy metal chelating compound, and anti-oxidant, and deionized water is described. A method of using such a reagent is also described.
    Type: Grant
    Filed: July 18, 1988
    Date of Patent: May 2, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Richard A. Kaufman, Henry J. Rosenfeld, Denise Zaunczkowski
  • Patent number: 4827004
    Abstract: Novel Isoprene Derivatives which have mucosa-protective and gastric acid secretion-inhibiting properties and are useful for combatting ulcers both by treating and as a prophylaxis against gastric and/or duodenal ulcers.
    Type: Grant
    Filed: August 24, 1987
    Date of Patent: May 2, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Albert Fischli, Max Schmid, Rudolf Schmid
  • Patent number: 4826980
    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: July 12, 1988
    Date of Patent: May 2, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Cedric H. Hassall, Geoffrey Lawton, Sally Redshaw
  • Patent number: 4826830
    Abstract: Topical application of glyciphosphoramide for treatment of cancerous ulcerations and tumor conditions are disclosed.
    Type: Grant
    Filed: July 31, 1985
    Date of Patent: May 2, 1989
    Inventors: Jui Han, Yan Sun
  • Patent number: 4824972
    Abstract: Compounds of the general formula ##STR1## wherein R represents an ether protecting group and R.sup.1 is a group of (a)-(d) useful as intermediates.
    Type: Grant
    Filed: January 19, 1988
    Date of Patent: April 25, 1989
    Assignee: Hoffmann-LaRoche Inc.
    Inventors: Richard Barner, Josef Hubscher
  • Patent number: 4824971
    Abstract: Novel 2-halochromans and their coupling to various nucleophiles to produce Vitamin E and as well as novel intermediates for Vitamin E.
    Type: Grant
    Filed: January 21, 1988
    Date of Patent: April 25, 1989
    Assignee: Hoffman-La Roche Inc.
    Inventor: Noal Cohen
  • Patent number: 4822890
    Abstract: A method for the production of substantially 100% pure N.alpha.-urethane protected amino acids is disclosed. This method eliminates the formation of di-peptide and tri-peptide contaminants. Reaction of blocking reagents at the carboxylate site on a protected peptide is prevented by the application of labile amino acid esters. Subsequent removal of the ester yields, in ultra-high purity, the N.alpha.-protected amino acid. The substantially 100% pure N.alpha.-urethane protected amino acid are also disclosed.
    Type: Grant
    Filed: June 24, 1986
    Date of Patent: April 18, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventor: David R. Bolin
  • Patent number: 4820835
    Abstract: A compound of the formula: ##STR1## wherein T is tritium; is described as well as intermediates for its preparation. The compound of formula I is useful in an assay for detecting the presence of benzodiazepine receptor occupiers in a warmblooded animal.
    Type: Grant
    Filed: June 30, 1986
    Date of Patent: April 11, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Walter Burger, Arnold A. Liebman, Clark W. Perry
  • Patent number: 4820734
    Abstract: The novel phenethylamine derivatives of the general formula ##STR1## wherein R.sup.1 and R.sup.2 each signify hydrogen, halogen, trifluoromethyl, lower alkoxy, lower alkyl, hydroxy or nitro, with the proviso that at least one of R.sup.1 and R.sup.2 is different from hydrogen, R.sup.3 and R.sup.4 each signify lower alkyl, n signifies the number 1, 2, 3 or 4 and B signifies the group --CO-- or --CHOH--, and their pharmaceutically acceptable acid addition salts have interesting analgesic and antidepressant properties. These substances can be manufactured according to various methods which are known per se and can be used as medicaments in the form of pharmaceutical preparation.
    Type: Grant
    Filed: November 4, 1987
    Date of Patent: April 11, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Karl Bernauer, Hans Bruderer
  • Patent number: 4816582
    Abstract: Antimicrobial 2-oxo-1-azetidinesulphonic acids of the formula ##STR1## in which H.sub.2 N ##STR2## represents an amino-substituted thiazolyl group, R.sup.1 is lower alkyl which is substituted by carbamoyl, lower alkylsuphonyl, azido, piperidine-carbonyl, (hexahydro-1H-azepin-1-yl)carbonyl or lower alkynyl, and R.sup.2 is hydrogen or a lower organic group, typically, carbamoyloxymethyl.
    Type: Grant
    Filed: October 22, 1987
    Date of Patent: March 28, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Andre Furlenmeier, Werner Hofheinz, Christian N. Hubschwerlen, Hans P. Isenring
  • Patent number: 4816476
    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: December 12, 1986
    Date of Patent: March 28, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Klaus, Peter Loeliger, Harald Weiser
  • Patent number: 4816566
    Abstract: A polypeptide having interferon activity which has an amino acid sequence corresponding to an amino acid sequence of an interferon selected from rIFN-.alpha., hybrid rIFN-.alpha., rIFN-.beta. and rIFN-.gamma. interferons in which at least one cysteine residue in the amino acid sequence has been replaced by an amino acid residue which is incapable of forming intermolecular disulfide bonds is provided. There are also provided a dsDNA sequence encoding the novel polypeptide; a replicable plasmidic expression vehicle containing the dsDNA encoding the novel polypeptides of the invention; a microorganism which has been transformed with the replicable plasmidic expression vehicle; and a method of preparing the dsDNA which encodes the novel polypeptides of the invention.
    Type: Grant
    Filed: February 10, 1986
    Date of Patent: March 28, 1989
    Assignee: Hoffmann-La Roche, Inc.
    Inventors: Thomas M. DeChiara, Stanley J. Tarnowski, Jr.
  • Patent number: 4816581
    Abstract: The novel compounds of the formula ##STR1## wherein R.sup.11 signifies hydrogen, acyl or tri(lower alkyl)silyl, R.sup.2 signifies a phenyl group which is substituted in the o- and/or the p-position by halogen, lower alkyl, lower alkylthio or lower alkoxy and n signifies the number 0 or 2, and mixtures thereof with the corresponding optical antipodes are valuable intermediates for the manufacture of antimicrobially active penems and carbapenems which have as a common structural element a (R)-1-hydroxyethyl group in the 6-position. They can be manufactured by reacting a compound of the formula ##STR2## wherein R.sup.12 signifies acyl, tri(lower alkyl)silyl or a group of the formula --BR.sup.3 R.sup.4 and R.sup.3 and R.sup.4 have the same significance and each signify a branched-open chain, cyclic or bicyclic hydrocarbon residue with 5-10 carbon atoms or together signify an open chain or cyclic hydrocarbon residue with 5-10 carbon atoms and two free valencies and R.sup.
    Type: Grant
    Filed: September 28, 1987
    Date of Patent: March 28, 1989
    Assignee: Hoffman-La Roche Inc.
    Inventor: Gerard Schmid
  • Patent number: 4814332
    Abstract: The imidazolium compounds of the formula ##STR1## wherein the various substituents are defined hereinbelow and their pharmaceutically acceptable acid addition salts, which possess valuable pharmacological properties are described. In particular, they possess antibacterial, antimycotic, protozoacidal and/or anthelmintic properties and are especially active against parasitic protozoa and worms. The compounds of formula I can be prepared according to known methods.
    Type: Grant
    Filed: May 4, 1987
    Date of Patent: March 21, 1989
    Assignee: Hoffman-La Roche Inc.
    Inventors: Wilhelm Klotzer, Helmut Link, Renate Mussner, Werner Schiestl, Nicolas Singewald
  • Patent number: 4812164
    Abstract: The invention is concerned with novel C.sub.1-4 -alkyl, C.sub.2-4 -alkenyl and C.sub.3 or 4 -alkynyl enol ethers of 3-aryluracils of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and X are as defined in the specification, their manufacture, weed control compositions which contain such enol ethers as the active substance and the use of the active substances or compositions for the control of weeds. The invention is also concerned with certain novel intermediates, some of which possess herbicidal activity, and with weed control compositions containing such active substances.
    Type: Grant
    Filed: September 15, 1987
    Date of Patent: March 14, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean Wenger, Paul Winternitz
  • Patent number: 4810645
    Abstract: This invention relates to the microbial production, via recombinant DNA technology, of new human leukocyte interferons, Le IF-K and Le IF-L for use in the treatment of viral and neoplastic diseases, and to the means and end products of such production.
    Type: Grant
    Filed: January 27, 1986
    Date of Patent: March 7, 1989
    Assignees: Hoffmann-La Roche Inc., Genentech, Inc.
    Inventors: David V. Goeddel, Sidney Pestka
  • Patent number: 4808605
    Abstract: Compounds of the formula ##STR1## wherein R is lower-alkyl, R.sup.1 is halogen, R.sup.2 is C.sub.1 -C.sub.12 -alkyl, R.sup.3 is hydroxy, lower-alkoxy, lower-alkyl-carbonyloxy, lower-alkoxy-lower-alkylcarbonoyloxy, lower-alkylaminocarbonyloxy, arylaminocarbonyloxy or aryl-lower alkylaminocarbonyloxy, X is C.sub.1 -C.sub.18 -alkylene which optionally can be interrupted by 1,4-phenylene or interrupted or lengthened by 1,4-cyclohexylene, A is di- or tri-substituted 2-imidazolyl attached via an ethylene group or a substituted or unsubstituted heterocycle selected from the group consisting of benzimidazolyl, benzimidazolonyl, imidazo[4,5-c]pyridinyl, imidazo[4,5-c]pyridinonyl, benzthiazolyl, benzodiazepine-2,5-dion-1-yl and pyrrolo[2,1-c]-[1,4]benzodiazepine-5,11-dion-10-yl and n is the number 0 or 1, in the form of racemates and optical antipodes, as well as N-oxides and pharmaceutically usable acid addition salts thereof.
    Type: Grant
    Filed: November 10, 1987
    Date of Patent: February 28, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Quirico Branca, Roland Jaunin, Hans P. Maki, Franzi Marti, Henri Ramuz
  • Patent number: 4808701
    Abstract: Cyclic peptides with appetite regulating activity.
    Type: Grant
    Filed: March 30, 1987
    Date of Patent: February 28, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Waleed Danho, Joseph Triscari, Vincent S. Madison