Patents Represented by Attorney Jon S. Saxe
  • Patent number: 4876369
    Abstract: The present invention is directed to a novel process for producing chromane derivatives, which are suitable as intermediates for the manufacture of d-.alpha.-tocopherol (natural vitamin E), and with a process for producing d-.alpha.-tocopherol itself.
    Type: Grant
    Filed: August 23, 1988
    Date of Patent: October 24, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Richard Barner, Josef Hubscher
  • Patent number: 4871755
    Abstract: 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: Grant
    Filed: February 5, 1988
    Date of Patent: October 3, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Marcel Muller
  • Patent number: 4871757
    Abstract: The invention is concerned with novel triazole derivatives of the formula ##STR1## wherein R.sup.1 is optionally substituted phenyl and R.sup.2 signifies substituted phenyl, as more precisely defined in the description, and R.sup.3 is halogen, methyl or halomethyl, and their acid addition salts, processes for their preparation, pest control compositions which contain these compounds as the active substance, as well as methods of use of such compounds or compositions for the control of pests.
    Type: Grant
    Filed: July 3, 1986
    Date of Patent: October 3, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Christoph Luthy, Rene Zurfluh
  • Patent number: 4870219
    Abstract: Novel styryl-tetrahydromaphythalene and indane derivatives useful for treating neoplasms and dermatoses.
    Type: Grant
    Filed: May 15, 1987
    Date of Patent: September 26, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Klaus, Peter Loeliger, Peter Mohr, Ekkehard Weiss
  • Patent number: 4869895
    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 vivo for detecting the presence of benzodiazepine receptor occupiers in a warmblooded animal.
    Type: Grant
    Filed: August 5, 1988
    Date of Patent: September 26, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Walter Burger, Arnold A. Liebman, Clark W. Berry
  • Patent number: 4867860
    Abstract: There is disclosed a process for producing a laminar electrode. The method comprises successive superposition of an insulating support, a conductive layer, a stable-potential internal reference element and an ion-selective diaphragm, all of which are protected by a mask which is impermeable to aqueous solutions. A completely tight seal between the mask and the ion-selective diaphragm is formed by casting the diaphragm in the form of a solution containing a binder which dissolves with and intimately mixes with the mask material.
    Type: Grant
    Filed: December 16, 1986
    Date of Patent: September 19, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Iqbal Siddiqi, Hans-Rudolf Wuhrmann
  • Patent number: 4868111
    Abstract: New gram-positive expression control DNA sequences useful in the expression of pro- or eukaryotic proteins in gram-positive organisms are provided having in the downstream direction of transcription a transcription initiation DNA sequence of gram-negative origin combined with a ribosome binding site-encoding DNA sequence, optionally a foreign gene and a transcription termination sequence. Also described are expression vectors containing these expression control DNA sequences and processes using same for the manufacture of pro- and eukaryotic polypeptides. In addition processes for the manufacture of such gram-positive expression control DNA sequences and such expression vectors are described.
    Type: Grant
    Filed: June 17, 1986
    Date of Patent: September 19, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Hermann Bujard, Stuart Le Grice
  • Patent number: 4865970
    Abstract: This invention provides methods for the diagnosis of systemic lupus erythematosus in patients, the sera of which contain antibodies reactive against ribosomal proteins P0, P1 and P2. A peptide containing an amino acid sequence corresponding to the carboxyl termini of the ribosomal proteins, which peptide is bound to a solid carrier, is also provided for use in such methods.
    Type: Grant
    Filed: February 28, 1986
    Date of Patent: September 12, 1989
    Assignees: Hoffmann-La Roche Inc., Cornell Research Foundation, Inc.
    Inventors: Nathan Brot, Keith Elkon, Susan M. Skelly, Herbert Weissbach
  • Patent number: 4866205
    Abstract: New optically active intermediates and processes thereto are provided for use in synthesizing therapeutically active prostaglandins of the formula: ##STR1## wherein R.sup.1 is hydrogen or lower alkyl; from a compound of the formula: ##STR2## wherein R.sup.1 is as above and R.sup.2 is hydrogen or a carboxy blocking group convertible to an acid by hydrolysis.
    Type: Grant
    Filed: July 11, 1988
    Date of Patent: September 12, 1989
    Assignees: Hoffman-La Roche Inc., Hoffman-La Roche Inc.
    Inventors: David L. Coffen, George W. Holland, W. Harry Mandeville, Perry Rosen, Frederick Wong
  • Patent number: 4863920
    Abstract: A compound for treating disorders of the central nervous system, which is of the formulawherein A taken together with the two carbon atoms denoted by .alpha. and .beta. is one of the following groups: ##STR1## R.sup.1 is one of the following groups:--CH.dbd.CH--R.sup.6 (d)and--C.tbd.C--R.sup.6, (e)R.sup.2 is hydrogen, R.sup.3 is lower alkyl, or R.sup.2 and R.sup.3 together are dimethylene or trimethylene, R.sup.4 and R.sup.5 are independently hydrogen, halogen, trifluoromethyl or lower alkyl, and R.sup.6 is hydrogen, halogen, aryl or a saturated lower hydrocarbon group which is optionally mono- or di-substituted by hydroxy, lower alkoxy, (C.sub.3 -C.sub.7)-cycloalkyl or oxo, wherein the compound has the (S)- or (R,S)-configuration with reference to the carbon atom denoted by .gamma. when R.sup.2 and R.sup.3 together are dimethylene or trimethylene and, further, the double bond present in group (d) has the E- and/or Z-configuration when R.sup.6 is different from hydrogen.
    Type: Grant
    Filed: March 3, 1988
    Date of Patent: September 5, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Walter Hunkeler, Emilio Kyburz, Marc Meier
  • Patent number: 4864023
    Abstract: The invention is concerned with tricyclic compounds of the formula ##STR1## wherein R.sup.1 is a hydrogen atom or a carboxy-protecting radical; R.sup.2 is a hydrogen atom or a lower alkyl radical which may be substituted with a halogen atom; R.sup.3 and R.sup.4 independently are a hydrogen atom or a lower alkyl radical which may be substituted with a hydroxy radical or a substituted or unsubstituted amino radical; X is a halogen atom; and R.sup.5 and R.sup.6 are independently a hydrogen atom or a lower alkyl radical which may be substituted with a hydroxy radical, a lower alkoxy radical or a substituted or unsubstituted amino radical; or R.sup.5 and R.sup.6, taken together with the adjacent nitrogen atom, may form a 5 to 7 membered heterocyclic ring which may be substituted with one or more substituents at the carbon atom(s), and the heterocyclic ring may further contain --NR.sup.7 --, --O--, --S--, --SO--, --SO.sub.2 -- or --NR.sup.7 --CO--, and also R.sup.
    Type: Grant
    Filed: August 26, 1988
    Date of Patent: September 5, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Kazuteru Yokose, Nobuo Shimma, Mikayo Kamata, Masahiro Aoki, Tatsuo Ohtsuka
  • Patent number: 4864058
    Abstract: A process for preparing optically active naphtho[1,2-b][1,4]thiazepin-4(5H)-ones comprising resolution of rac-.beta.-[(2-amino-1-naphthalenyl)thio]-.alpha.-hydroxy-4-methoxybenzene propanoic acid and converting the optically active acids so obtained into final products is described. The end product naphtho[1,2-b][1,4]thiazepin-4(5H)-ones have activity as calcium channel blockers and accordingly are useful as agents for lowering blood pressure, and as agents for treating ischemia.
    Type: Grant
    Filed: May 10, 1988
    Date of Patent: September 5, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Erno Mohacsi
  • Patent number: 4863941
    Abstract: Glycerol derivatives of the formula ##STR1## wherein one of the residues R.sup.1, R.sup.2 and R.sup.3 is a group U of the formula OY.sup.1 or --X.sup.1 --CO--(A.sup.1).sub.n --Z.sup.1, another residue is a group V of the formula OY.sup.2 or --X.sup.2 --CO--(A.sup.2).sub.p --Z.sup.2, and the remaining residue is a group W of the formula --X.sup.3 T--(C.sub.2-6 -alkylene)-N.sup.+ R A.sup.- in which one of X.sup.1, X.sup.2 and X.sup.3 is oxygen or NQ.sup.1 and the other two are oxygen and the remaining symbols have the significance given below, and their hydrates are described and are prepared by introducing or generating the residues R.sup.1, R.sup.2 and R.sup.3 in corresponding glycerol derivatives.The compounds of formula I are active as inhibitors of blood platelet activating factor or as inhibitors of the growth of tumors.
    Type: Grant
    Filed: June 5, 1986
    Date of Patent: September 5, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Richard Barner, Kaspar Burri, Jean-Marie Cassal, Paul Hadvary, Georges Hirth, Klaus Muller
  • Patent number: 4861890
    Abstract: A process for producing chiral enamines by isomerizing a beta, gamma unsaturated amine with a rhodium-diphosphine complex with the addition of an achiral triarylphosphine and, if desired, hydrolyzing the compound of the enamine I obtained to the corresponding aldehyde.
    Type: Grant
    Filed: August 10, 1987
    Date of Patent: August 29, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bernd Heiser, Hansjorg Stoller
  • Patent number: 4861772
    Abstract: The known compound, t-butyl (S)-8-bromo-11,12,13,13a-tetrahydro-9-oxo-9H-imidazo[1,5-a]pyrrolo[2,1-c][ 1,4]benzodiazepine-1-carboxylate of the formula ##STR1## is effective in the prevention or interruption in a human being of panic states, accompanying phobias and the associated social consequences such as anticipatory anxiety and avoidance behavior. In particular, it is effective in the discontinuous, purely attack-based prevention or interruption of panic states.
    Type: Grant
    Filed: April 7, 1988
    Date of Patent: August 29, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Walter Merz
  • Patent number: 4859306
    Abstract: The electrode comprises an internal reference half-cell at stable potential comprising a conductive sheet, e.g. of metal of carbon, covered by a redox system. The redox system comprises a thin dehydrated layer of Prussian blue deposited by contact between the sheet and a mixture of alkaline ferrocyanide and a ferric salt.
    Type: Grant
    Filed: May 31, 1988
    Date of Patent: August 22, 1989
    Assignee: Hoffman-La Roche Inc.
    Inventors: Iqbal Siddiqi, Hans-Rudolf Wuhrmann
  • Patent number: 4859665
    Abstract: Compositions for treating hypertension comprising an effective amount of a dihydropyridine of the formula ##STR1## in which X is 1 or 2 identical or different substituents from the group consisting of nitro, chlorine and trifluoromethyl, or together with the phenyl ring, the group ##STR2## R.sup.1 is alkyl of 1 to 4 C atoms, which is optionally substituted by alkoxy of 1 to 4 C atoms,R.sup.2 is alkyl of 1 to 12 C atoms, which is optionally substituted by alkoxy of 1 to 3 C atoms, fluorine or N-methyl-N-benzylamino andR.sup.3 is alkyl of 1 to 4 C atoms, cyano or hydroxymethyl, and a pyridazodiazepine of the formula ##STR3## in which R.sup.4 is aralkyl,R.sup.5 is hydrogen or alkyl of 1 to 8 C atoms,R.sup.6 is hydrogen or alkyl of 1 to 8 C atoms andR.sup.7 and R.sup.8 are hydrogen, or together, an oxo group, are described.
    Type: Grant
    Filed: December 2, 1986
    Date of Patent: August 22, 1989
    Assignees: Hoffmann-LaRoche Inc., Bayer Akt.
    Inventors: Bernward Garthoff, Marcel Gerold, Fridolin Hefti, Stanislav Kazda, Andreas Knorr
  • Patent number: 4859229
    Abstract: The invention is concerned with 3-aryluracils of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are as described herein, as well as salts thereof and their manufacture, weed control compositions which contain such compounds as the active substance and the use of the active substances or compositions for weed control. The invention is also concerned with herbicidally-active starting materials and weed control compositions containing these.
    Type: Grant
    Filed: July 21, 1987
    Date of Patent: August 22, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean Wenger, Paul Winternitz
  • Patent number: 4857648
    Abstract: The invention is concerned with novel isoquinoline derivatives of the formula ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, lower alkoxy, aryl, aryloxy, aryl-lower alkyl or aryl-lower alkoxy andR.sup.2 is phenyl or substituted phenyl.These novel isoquinoline derivatives are valuable intermediates in the manufacture of morphinan derivatives.
    Type: Grant
    Filed: November 8, 1988
    Date of Patent: August 15, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Emil A. Broger, Yvo Crameri, Bernd Heiser
  • Patent number: 4855085
    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: January 30, 1989
    Date of Patent: August 8, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Ka-Kong Chan, Gabriel G. Saucy