Patents Represented by Attorney Bernard S. Leon
  • Patent number: 6063814
    Abstract: Phorbol esters and particularly phorbol-12-myristate-13-acetate (TPA) are described as effective in treating patients with neoplastic diseases such as leukemia as well as in increasing the white blood cell count.
    Type: Grant
    Filed: April 14, 1997
    Date of Patent: May 16, 2000
    Inventors: Richard L. Chang, Zheng Tao Han
  • Patent number: 5126347
    Abstract: Isomeric derivatives of 2',3'-dideoxyadenosine and 2',3'-dideoxyguanosine wherein the adenine or guanine base is attached to the 1' position of the iso-dideoxysugar residue by the 9-N position, the novel intermediates used in the synthesis of these compounds, and a method for treating a subject infected with a retrovirus by administering the compounds of the invention.
    Type: Grant
    Filed: February 13, 1989
    Date of Patent: June 30, 1992
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Donna M. Huryn, Steve Yik-Kai Tam, Manfred Weigele
  • Patent number: 5081036
    Abstract: Methods and apparatus are provided for growing both suspension type cells and anchorage dependent cells in airlift bioreactors. A packing means, such as stainless steel wool, is provided in the growth chamber of the bioreactor to increase cell density by trapping suspension cells or acting as a solid support for anchorage depended cells without interfering with gentle circulation of liquid growth medium in the bioreactor.
    Type: Grant
    Filed: September 28, 1990
    Date of Patent: January 14, 1992
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Philip C. Familletti
  • Patent number: 5073491
    Abstract: Method and apparatus are provided for immobilizing and growing cells in airlift bioreactors to obtain increased cell density. Cells are immobilized by forming alginate beads containing cells and gelatin particles, and dissolving the gelatin by heating to form cavities in the beads entrapping the cells. In a growth chamber of an airlift bioreactor, introduced oxygen-containing gas circulates growth medium in contact with the beads resulting in oxygen transfer to cells in the cavities of the beads where growth of the cells occurs. Preferably, bead formation is carried out in the growth chamber by dripping an alginate-cell gelatin suspension into a calcium solution contained in the growth chamber. Growth medium is then supplied to the chamber, and oxygen-containing gas is introduced to result in circulation of the growth medium and growth of the cells.
    Type: Grant
    Filed: December 23, 1988
    Date of Patent: December 17, 1991
    Assignee: Hoffman-La Roche Inc.
    Inventor: Philip C. Familletti
  • Patent number: 5073550
    Abstract: Antibacterial compounds of the formula ##STR1## wherein R is a mononuclear carbocyclic aromatic group, a 5-membered aromatic heterocyclic group which contains as the hetero (non-carbon) ring member(s) an oxygen or sulphur atom or an imino or lower alkylimino group and, optionally, one or two nitrogen atoms, or a 6-membered aromatic heterocyclic group which contains one to three nitrogen atoms as the hetero ring member(s); R.sup.1 is hydrogen or a 3-substituent which is usable in cephalosporin chemistry; A is lower alkylene or C.sub.3-7 cycloalkylene which is optionally substituted with carboxy, carbamoyl, lower alkylcarbamoyl or di-(lower alkyl)carbamoyl; Q is lower alkylene or C.sub.3-7 cycloalkylene which is optionally substituted with carboxy, carbamoyl, lower alkylcarbamoyl or di(lower alkyl)carbamoyl, or the group --NR.sup.2 -- or --NR.sup.2 NR.sup.3 --; R.sup.2 and R.sup.3 are independently hydrogen or lower alkyl; p and m are the zero or 1, n is zero, 1 or 2; R.sup.
    Type: Grant
    Filed: August 28, 1990
    Date of Patent: December 17, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Erwin Gotschi
  • Patent number: 5066800
    Abstract: A novel process and intermediates used therein for linking a cephalosporin compound to a quinolone are disclosed. According to the disclosed process, the 2-carboxylic acid moiety of the cephalosporin compound is treated with an organic base. The resulting salt is then reacted with a quinolone compound which has been activated using a haloformate. The reaction is run in a non-aqueous organic solvent. 4-Dimethylaminopyridine is used to promote the reaction between the cephalosporin salt and the activated quinolone.
    Type: Grant
    Filed: April 27, 1990
    Date of Patent: November 19, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Masami Okabe
  • Patent number: 5064863
    Abstract: Tertiary and secondary amines of the formulas ##STR1## wherein n is the integer 1 or 2, p0 R is hydrogen, lower-alkanoyl or phenyl-lower-alkanoyl,X.sup.1 is phenoxymethyl optionally mono-fluorinated or mono-chlorinated in the ortho-position,X.sup.2 is lower-alkyl, phenoxymethyl optionally mono-fluorinated or mono-chlorinated in the ortho-position or phenyl optionally monosubstituted by fluorine, chlorine, trifluoromethyl or lower-alkoxy,Y is hydrogen or methyl, andZ is a phenyl or thienyl residue substituted as hereinafter described,and the physiologically and pharmaceutically compatible salts are described. The compounds of formulas I and V-1 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. The compounds of formulas I and V-1 can be prepared starting from corresponding primary amines.
    Type: Grant
    Filed: December 10, 1987
    Date of Patent: November 12, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Marcel Muller
  • Patent number: 5063219
    Abstract: Compositions comprising a mixture of a 2,4-diamino-5-(trisubstituted)benzyl-pyrimidine potentiated sulfonamide antibiotic with an ionophorous polyether anticoccidial agent are useful for the treatment and prevention of coccidiosis in animals.
    Type: Grant
    Filed: October 9, 1990
    Date of Patent: November 5, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Eugene G. Schildknecht, Govind G. Untawale
  • Patent number: 5061629
    Abstract: Enantiomerically pure (2R)-2-hydroxy arylalkanoic acid esters and (2S)-2-hydroxy arylalkanoic acids are prepared by the Pseudomonas lipase-catalyzed selective hydrolyxis of racemic (2RS)-2-hydroxy arylalkanoic acid esters in solution or suspension in an aqueous medium at a controlled pH of from about 5 to about 9.
    Type: Grant
    Filed: October 29, 1990
    Date of Patent: October 29, 1991
    Assignee: Hoffman-La Roche Inc.
    Inventors: David L. Coffen, Panayiotis Kalaritis, John J. Patridge
  • Patent number: 5057530
    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: May 19, 1989
    Date of Patent: October 15, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Richard Barner, Kaspar Burri, Jean-Marie Cassal, Paul Hadvary, Georges Hirth, Klaus Muller
  • Patent number: 5057614
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, X and Y have the signficance given in the description, are useful in the control or prevention of inflammatory, immunological, bronchopulmonary or cardiovascular disorders.
    Type: Grant
    Filed: February 6, 1989
    Date of Patent: October 15, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Peter D. Davis, Christopher H. Hill, Geoffrey Lawton
  • Patent number: 5055572
    Abstract: Acyl derivatives of the formula ##STR1## in which R is an acyl group, excluding those acyl groups of the formula ##STR2## in which A is a group of the formulae --NHCO--, --NHCONHCO--, --NHCOCH.dbd.CH--, ##STR3## wherein R.sup.6 is hydrogen or lower alkyl; R.sup.1 and R.sup.2 are hydrogen or a protecting group, X is hydrogen, halogen, lower alkoxy, nitro or --OR.sup.2, n is 1 or 2, R.sup.4 and R.sup.5 are hydrogen or together represent an additional bond and Z is a direct bond or carbonyl (where R.sup.4 and R.sup.5 both represent hydrogen) or a group of the formula --O--B-- (where R.sup.4 and R.sup.5 together represent an additional bond) in which B is a straight-chain, branched or cyclic lower alkylene;and wherein R.sup.3 is a substituted bicyclic group of the formulae ##STR4## wherein R.sup.7 and R.sup.
    Type: Grant
    Filed: April 8, 1988
    Date of Patent: October 8, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Andre Furlenmeier, Erwin Gotschi, Paul Hebeisen, Werner Hofheinz, Helmut Link
  • Patent number: 5055622
    Abstract: Novel Styryl-tetrahydromaphthalene and indane derivatives useful for treating neoplasms and dermatoses.
    Type: Grant
    Filed: September 12, 1990
    Date of Patent: October 8, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Klaus, Peter Loeliger, Peter Mohr, Ekkehard Weiss
  • Patent number: 5045567
    Abstract: Propanolamine derivatives of the formula ##STR1## wherein R.sup.1 is hydrogen or a group of formula ##STR2## n is the number 0 or 1; R.sup.2 and R.sup.5 are phenyl, m-halophenyl, m-trifluoromethylphenyl, thienyl or pyridyl;R.sup.3 is hydrogen or methyl;R.sup.4 is hydrogen, --CH.sub.2 COOH, --CH.sub.2 COO--C.sub.1-4 -alkyl, --(CH.sub.2).sub.2 O--C.sub.1-4 -alkyl or --(CH.sub.2).sub.2 O(CH.sub.2).sub.1-4 --C.sub.6 H.sub.5 ;and a physiologically compatible salt thereof.The invention also relates to processes for the preparation of these propanolamine derivatives, pharmaceutical preparations and feedstuffs containing them, and methods of using the propanolamine derivatives.
    Type: Grant
    Filed: October 31, 1990
    Date of Patent: September 3, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Frank Kienzle
  • Patent number: 5043170
    Abstract: Poultry feed premixes and finished poultry feeds which contain particles comprising a Vitamin D.sub.3 metabolite and Vitamin D.sub.3 in a weight ratio ranging from about 1:2.5 to about 1:125 are described. These premixes and feeds are useful for promoting egg shell strength and bone strength in older egg laying hens as well as to provide to such hens the usual benefits of Vitamin D.sub.3 in a diet. The invention also relates to methods for improving egg shell strength in older egg laying hens which comprise administering to hens such particles.
    Type: Grant
    Filed: February 14, 1989
    Date of Patent: August 27, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Benjamin Borenstein, William J. Mergens, Govind G. Untawale
  • Patent number: 5041266
    Abstract: A microtiter plate containing a plurality of reaction wells for conducting immunogenic reactions wherein the bottom wall of the reaction well has an inner surface which is substantially hydrophilic, and the side wall of the reaction well has an inner surface which is substantially hydrophobic and a process for producing said trays.
    Type: Grant
    Filed: December 21, 1989
    Date of Patent: August 20, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventor: William A. Fox
  • Patent number: 5039671
    Abstract: 26, 26, 26-Trifluoro-1.alpha., 25-dihydroxy-cholecalciferol, and the 25R or 25S epimer thereof, are described, as well as processes and intermediates utilized to prepare the same, as well as pharmaceutical compositions containing the same. 26,26,26-trifluoro 1.alpha., 25-dihydroxycholecalciferol and the 25R or 25S epimer thereof are useful agents in the treatment of disease states such as osteoporosis, oseodystrophy and leukemia.
    Type: Grant
    Filed: November 16, 1989
    Date of Patent: August 13, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Enrico G. Baggiolini, Giacomo Pizzolato, Gary A. Truitt, Milan R. Uskokovic
  • Patent number: 5037825
    Abstract: The invention relates to compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, acyl, lower-alkyl or --CHO, --CH.sub.2 OR.sup.10, --COR.sup.7 or OR.sup.13 ; R.sup.2, R.sup.3 and R.sup.4 are, independently, hydrogen, lower-alkyl, lower-alkoxy or halogen; R.sup.5 and R.sup.6 are, independently, hydrogen or lower-alkyl; R.sup.7 is hydroxy, lower-alkoxy or NR.sup.8 R.sup.9 ; R.sup.8 and R.sup.9 are, independently, hydrogen or lower-alkyl; X and Y are, independently, >CR.sup.14 R.sup.15, --O--, --S--, >SO, >SO.sub.2 or >NR.sup.18 ; R.sup.10 and R.sup.18 are, independently, hydrogen, lower-alkyl or acyl; M is --C(R.sup.11).dbd.C(R.sup.12)--, --CONH-- or --NH--CO--; R.sup.11, R.sup.12, R.sup.14 and R.sup.15 are, independently, hydrogen or lower-alkyl, R.sup.
    Type: Grant
    Filed: July 10, 1989
    Date of Patent: August 6, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Klaus, Peter Mohr, Ekkehard Weiss
  • Patent number: 5037747
    Abstract: Enantiomerically pure (2R)-hydroxy-substituted benzopyran-2-carboxylic acid esters and (2S)-hydroxy-substituted benzopyran-2-carboxylic acids, are prepared by the Pseudomonas lipase-catalyzed selective hydrolysis of racemic (2RS)-hydroxy-substituted benzopyran-2-carboxylic acid esters in solution or suspension in an aqueous or aqueous/organic medium, at a pH of from about 5 to about 10.
    Type: Grant
    Filed: January 26, 1988
    Date of Patent: August 6, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventors: David L. Coffen, Panayiotis Kalaritis, John J. Partridge
  • Patent number: 5036066
    Abstract: The compounds are of the class of bi- and tricyclic pyridone derivatives of the formula ##STR1## wherein the various substituent are as described in the specification, useful in the control of prevention of muscle tensions stress conditions, insomnia, anxiety states and/or convulsions.
    Type: Grant
    Filed: October 16, 1989
    Date of Patent: July 30, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Ulf Fischer, Fernand Schneider, Ulrich Widmer