Patents Represented by Attorney Jon S. Saxe
  • 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: 4743687
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 represents hydroxy, alkyl, aralkyl, aralkoxy-alkyl, hydroxy-alkyl, amino-alkyl, acylamino-alkyl, monoalkylamino-alkyl, dialkylamino-alkyl, alkoxycarbonylamino-alkyl, halo-alkyl, carboxy-alkyl, alkoxycarbonyl-alkyl, alkoxy or aralkoxy; R.sup.2 and R.sup.3 each represent hydrogen, alkyl or aralkyl; R.sup.4 and R.sup.5 each represent hydrogen or R.sup.4 and R.sup.5 together represent oxo; and X represents an oxygen atom or the group --NR.sup.6 -- in which R.sup.6 represents hydrogen, alkyl or aralkyl or --(CH.sub.2).sub.n -- in which n stands for zero, 1 or 2,and racemates, enantiomers, diastereoisomers or pharmaceutically acceptable salts thereof have antihypertensive activity and can be used as medicaments in the form of pharmaceutical preparations. They can be prepared according to known methods.Compounds useful as starting materials for producing the compounds of formula I are also provided.
    Type: Grant
    Filed: June 23, 1986
    Date of Patent: May 10, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Geoffrey Lawton, Sally Redshaw
  • Patent number: 4743696
    Abstract: Compounds of the general formula ##STR1## wherein R represents an ether protecting group and R.sup.3 is a group of (f)-(i) useful as intermediates.
    Type: Grant
    Filed: March 5, 1987
    Date of Patent: May 10, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Richard Barner, Josef Hubscher
  • Patent number: 4743604
    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: November 1, 1984
    Date of Patent: May 10, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Marcel Muller
  • Patent number: 4741767
    Abstract: The invention is concerned with novel weed control compositions which contain herbicidally-active compounds of the formula ##STR1## wherein ring A, R.sup.1, R.sup.2, R.sup.3, Y and Z are as hereinafter set forth, and the use of these compounds and compositions for the control of weeds. The invention is also concerned with novel compounds of formula I as well as their preparation.
    Type: Grant
    Filed: November 6, 1985
    Date of Patent: May 3, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Jean-Pierre Obrecht
  • Patent number: 4742069
    Abstract: Dihydropyridine derivatives of the formula ##STR1## wherein the symbols A, R and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are as described herein.Compounds of formula I have a pronounced calcium-antagonistic activity and can accordingly be used as medicaments, especially for the control or prevention of angina pectoris, ischemia, high blood pressure and/or migraine.
    Type: Grant
    Filed: June 17, 1985
    Date of Patent: May 3, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Roland Jaunin, Henri Ramuz
  • 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: 4735940
    Abstract: Compounds of the formula ##STR1## or a pharmaceutically acceptable acid addition salt of a compound of formula I which has one or more basic substituents, are described.The compounds of formula I possess pronounced muscle relaxant, sedative-hypnotic, anticonvulsive and anxiolytic properties and have low toxicity.
    Type: Grant
    Filed: October 31, 1985
    Date of Patent: April 5, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Ulf Fischer, Fernand Schneider, Ulrich Widmer
  • 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: 4734400
    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: June 16, 1986
    Date of Patent: March 29, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: David R. Bolin, Johannes A. Meienhofer, Iou-Iou Sytwu
  • Patent number: 4734399
    Abstract: The invention is directed to analogs of GRF or fragments thereof wherein the fragment is reduced in number by one to fifteen amino acids from the carboxyl end wherein the analogs have the formula: ##STR1## wherein R is desNH.sub.2 -Tyr, Tyr, D-Tyr, Ac-Tyr, His or C.sup..alpha. -Methyl-Tyr; R.sub.1 is Ala, N-Methyl-D-Ala or D-Ala; R.sub.2 is Lys, Ala, Leu, Val or Ile; R.sub.3 is Ala, Leu, Val, Ile, Nle, Nval, .beta.-Ala or .alpha.-Aib; R.sub.4 is Lys, Ala, Leu, Val or Ile; R.sub.5 is Met, Leu, Nle or Ile; R.sub.6 is Asn or Ser; X is hydrogen or --COR.sub.7 ; R.sub.7 is hydrogen, C.sub.1-4 alkyl or halo(C.sub.1-4)alkyl; Y is --OR.sub.8 or --NR.sub.9 R.sub.10 ; R.sub.8 is hydrogen or C.sub.1-5 -alkyl; R.sub.9 and R.sub.10 independently equal hydrogen, C.sub.1-7 alkyl, C.sub.2-4 alkenyl or halo(C.sub.1-4)alkyl; and pharmaceutically acceptable acid or base addition salts thereof. The invention is further directed to pharmaceutical compositions and to methods for treating growth hormone deficiencies.
    Type: Grant
    Filed: October 23, 1986
    Date of Patent: March 29, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Arthur M. Felix, Edgar P. Heimer, Thomas F. Mowles
  • Patent number: 4732972
    Abstract: Polypeptides corresponding to growth hormone releasing factor in which methionine at position 27 has been replaced by a leucine residue retain full growth hormone releasing activity. In the case of the full length (44-amino acid) polypepitide, the leucine analog has full biological activity in the free acid form, unlike the natural growth releasing factor which requires carboxy terminal amidation for full biological activity.
    Type: Grant
    Filed: October 21, 1985
    Date of Patent: March 22, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Arthur M. Felix, Edgar P. Heimer
  • Patent number: 4732902
    Abstract: The invention relates to long-acting depot producing antipsychotic pyrroloisoquinolinyl-dimethyloxoalkyl alkanoates of the formula ##STR1## wherein R.sub.1 and R.sub.2 independently, are hydrogen, alkyl of 1 to 4 carbon atoms, cycloalkyl or alkenyl, or taken together are alkylene of 3 to 6 carbon atoms; and R.sub.3 is hydrogen, alkyl, hydroxyalkyl, phenylhydroxyalkyl, halophenylhydroxyalkyl, alkylphenylhydroxyalkyl, alkoxyphenylhydroxyalkyl, alkoxyalkyl, aryloxyhydroxyalkyl, alkoxyhydroxyalkyl, acyloxyalkyl, arylcarbonylalkyl, alkoxycarbonylalkyl, aralkyl, alkenyl, alkylcycloalkyl, alkynyl, thienylalkyl, furylalkyl, arylcarboxamidoalkyl, acylalkyl, cyclic-alkyloxoalkyl, cyclic-alkylhydroxyalkyl, alkenyloxyalkyl, aralkenyl, aryloxyalkyl, or aryl-N-imidazolonylalkyl; R.sub.4 is alkyl; and n is the integer 2 or 3,their corresponding optical isomers, geometric isomers, and mixtures thereof, and the pharmaceutically acceptable acid additional salts.The compounds of formula I are useful as antipsychotic agents.
    Type: Grant
    Filed: May 23, 1986
    Date of Patent: March 22, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Berger, Gary L. Olson
  • Patent number: 4732753
    Abstract: Suppositories containing as the active substance a therapeutically effective amount of ceftriaxone, a pharmaceutically compatible salt thereof or a hydrate of one of these compounds, a stabilizer consisting of a mono-, di- or triglyceride of a C.sub.12 -C.sub.18 -fatty acid or of a mixture of such glycerides, a potentiator consisting of an aliphatic C.sub.2 -C.sub.18 -fatty acid, a mono-, di- or triglyceride of a C.sub.2 -C.sub.12 -fatty acid, a partial ester or complete ester of propylene glycol, polyethylene glycol or a carbohydrate with a C.sub.2 -C.sub.12 -fatty acid, a pharmaceutically compatible ester or ether thereof or of a mixutre of the said potentiators and, if desired, customary therapeutically inert adjuvants for suppositories, and their manufacture are described. These have valuable antimicrobial properties.
    Type: Grant
    Filed: February 11, 1985
    Date of Patent: March 22, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Walter Fuller
  • 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: 4731373
    Abstract: Glycerine derivatives of the formula ##STR1## wherein the residues R.sup.1, R.sup.2 and R.sup.3 have the significance given in the description,and their hydrates, which inhibit blood platelet activating factor (PAF), are descried.
    Type: Grant
    Filed: December 10, 1984
    Date of Patent: March 15, 1988
    Assignee: Hoffman-La Roche Inc.
    Inventors: Richard Barner, Kasper Burri, Jean-Marie Cassal, Paul Hadvary, Georges Hirth, Klaus Muller
  • Patent number: 4731363
    Abstract: The present disclosure relates to the use of thromboxane synthase inhibitors as antiobesity agents and insulin lowering agents. Such compounds fall into a variety of classes among which are 1-substituted imidazoles, 4-substituted imidazoles, 3-substituted pyridines, 3-substituted indoles, 4-substituted pyrimidines, 5-substituted tetrazoles, pyrazolidines, quinazolines, and substituted xanthene carboxylic acids.
    Type: Grant
    Filed: January 16, 1986
    Date of Patent: March 15, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: James G. Hamilton, Ann C. Sullivan, Lawrence D. Tobias, Joseph Triscari
  • Patent number: 4729903
    Abstract: The invention relates to a process for depositing I-125 on a substrate which comprises contacting a predetermined surface area of substrate with Xe-125 gas, whereby the Xe-125 decays to I-125 and the I-125 in turn deposits as a solid on the surface of the substrate, the contact being for a time sufficient to deposit at least about 1 microcurie of I-125. I-125 is thereby deposited in a relatively uniform amount over the surface area of the substrate. The substrate is then assayed to determine how much I-125 has been deposited. The substrate is then divided into pieces of measured surface area, each piece therefore containing a measured amount of deposited I-125, and each piece can then be used in the manufacture of an I-125 source.
    Type: Grant
    Filed: June 10, 1986
    Date of Patent: March 8, 1988
    Assignee: Midi-Physics, Inc.
    Inventors: James J. McGovern, Joseph M. Olynyk
  • Patent number: 4728609
    Abstract: Th preparation of a double-stranded polydeoxy ribonucleotide having cohesive termini each comprising one strand of a double-strand restriction endonuclease recognition site and, between the termini, a structural gene coating for the expression of recombinant growth hormone releasing factor, at least a majority of the codons and the coding strand of said gene being codons preferred for the expression of microbial genomes; a method of producing such DNA a recombinant microbial cloning vehicle comprising such DNA and the novel methods of producing said peptide are described.
    Type: Grant
    Filed: September 24, 1985
    Date of Patent: March 1, 1988
    Assignee: Hoffmann-La-Roche Inc.
    Inventors: Ram S. Bhatt, Kenneth J. Collier, Robert M. Crowl, Mohindar S. Poonian
  • Patent number: 4725554
    Abstract: Method for measuring the coagulation time of a blood sample in which a sample-reagent mixture is formed by introducing the sample and at least one reagent into a cuvette. To reduce the operating and material costs, the sample-reagent mixture is so moved in a stationary cuvette that the mixture flows back and forth around an edge projecting into the cuvette, whereby a clot forms on this edge.
    Type: Grant
    Filed: December 5, 1986
    Date of Patent: February 16, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Kurt Schildknecht