Patents by Inventor Milan R. Uskokovic

Milan R. Uskokovic has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 4595776
    Abstract: The invention is directed to a process and intermediates for the preparation of 1.alpha.,25-dihydroxyergocalciferol as well as substantially pure and crystalline 1.alpha.,25-dihydroxyergocolciferol. The end-product 1.alpha.,25-dihydroxyergocalciferol is useful in the treatment of disease states which are characterized by insufficient amounts of 1.alpha., 25-dihydroxycholecalciferol.
    Type: Grant
    Filed: December 17, 1984
    Date of Patent: June 17, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Enrico G. Baggiolini, Andrew D. Batcho, Alfred Boris, Milan R. Uskokovic
  • Patent number: 4594432
    Abstract: The invention is directed to a process and intermediates for the preparation of 1.alpha.,23(S),25-trihydroxycholecalciferol and 1.alpha.,23(R),25-trihydroxycholecalciferol. The end-products, 1.alpha.,23(S),25-trihydroxycholecalciferol and 1.alpha.,23(R),25-trihydroxycholecalciferol, are useful for the treatment of disease states which are characterized by insufficient amounts of 1,25 dihydroxycholecalciferol.
    Type: Grant
    Filed: December 27, 1983
    Date of Patent: June 10, 1986
    Assignee: Hoffman-La Roche Inc.
    Inventors: Enrico G. Baggiolini, Milan R. Uskokovic, Peter M. Wovkulich
  • Patent number: 4594340
    Abstract: The syntheses of 25,26-dehydro-1.alpha.,24R-dihydroxycholecalciferol and 25,26-dehydro-1.alpha.,24S-dihydroxycholecalciferol and the epimeric mixture which are useful as differentiation inducing agent and anti-proliferation agents are described. 25,26-dehydro-1.alpha.,24R-dihydroxycholecalciferol, 25,26-dehydro-1.alpha.,24S-dihydroxycholecalciferol, and the epimeric mixture are useful in treating osteoporosis, tumors and leukemia.
    Type: Grant
    Filed: November 29, 1984
    Date of Patent: June 10, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: John J. Partridge, Shian-Jan Shiuey, Gary A. Truitt, Milan R. Uskokovic
  • Patent number: 4508651
    Abstract: The invention is directed to a process and intermediates for the preparation of 1.alpha.,25-dihydroxyergocalciferol as well as substantially pure and crystalline 1.alpha.,25-dihydroxyergocolciferol. The end-product 1.alpha.,25-dihydroxyergocalciferol is useful in the treatment of disease states which are characterized by insufficient amounts of 1.alpha.,25-dihydroxycholecalciferol.
    Type: Grant
    Filed: March 21, 1983
    Date of Patent: April 2, 1985
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Enrico G. Baggiolini, Andrew D. Batcho, Alfred Boris, Milan R. Uskokovic
  • Patent number: 4428963
    Abstract: Thiophene derivatives having utility as blood lipid lowering agents and as antiobesity agents are disclosed.
    Type: Grant
    Filed: March 10, 1983
    Date of Patent: January 31, 1984
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Pasquale N. Confalone, Giacomo Pizzolato, Milan R. Uskokovic, Marianne Rouge
  • Patent number: 4421690
    Abstract: The present invention relates to a process and intermediates for the preparation of 24,24-difluoro-1.alpha.,25-dihydroxycholecalciferol from the readily-available 1.alpha.,3.beta.-dihydroxyandrost-5-en-17-one which is made by a known microbiological process from 3.beta.-hydroxyandrost-5-en-17-one [R. M. Dodson, A. H. Goldkamp and R. D. Muir, J. Amer. Chem. Soc. 82 4026 (1960)].
    Type: Grant
    Filed: May 17, 1982
    Date of Patent: December 20, 1983
    Assignee: Hoffmann-La Roche Inc.
    Inventors: John J. Partridge, Shian-Jan Shiuey, Milan R. Uskokovic
  • Patent number: 4415742
    Abstract: A simple and economic chiral synthesis of optically active methyl L-acosaminide and methyl L-daunosaminide from propenyl acetate, said methyl L-acosaminide and methyl L-daunosaminide being coupling agents for the production of known antitumor agents.
    Type: Grant
    Filed: September 27, 1982
    Date of Patent: November 15, 1983
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Milan R. Uskokovic, Peter M. Wovkulich
  • Patent number: 4414402
    Abstract: A simple and economic chiral synthesis of optically active methyl L-acosaminide and methyl L-daunosaminide from propenyl acetate, said methyl L-acosaminide and methyl L-daunosaminide being coupling agents for the production of known antitumor agents.
    Type: Grant
    Filed: September 27, 1982
    Date of Patent: November 8, 1983
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Milan R. Uskokovic, Peter M. Wovkulich
  • Patent number: 4397847
    Abstract: The present invention relates to a method of treating osteoporosis by administering to a host suffering from osteoporosis an effective amount of 24,24-difluoro-1.alpha.,25-dihydroxycholecalciferol.
    Type: Grant
    Filed: May 17, 1982
    Date of Patent: August 9, 1983
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alfred Boris, John J. Partridge, Milan R. Uskokovic
  • Patent number: 4382031
    Abstract: A process is disclosed for producing d-biotin from L or DL-cystine ester via novel intermediates.
    Type: Grant
    Filed: November 23, 1981
    Date of Patent: May 3, 1983
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Enrico G. Baggiolini, Hsi L. Lee, Milan R. Uskokovic
  • Patent number: 4376207
    Abstract: A simple and economic chiral synthesis of optically active methyl L-acosaminide and methyl L-daunosaminide from propenyl acetate, said methyl L-acosaminide and methyl L-daunosaminide being coupling agents for the production of known antitumor agents.
    Type: Grant
    Filed: December 2, 1981
    Date of Patent: March 8, 1983
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Milan R. Uskokovic, Peter M. Wovkulich
  • Patent number: 4360470
    Abstract: The present disclosure is directed to a process for the synthesis of chenodeoxychloic acid, 25-hydroxycholesterol and 1.alpha.,25-dihydroxycholesterol from 17-keto steroids. A cholic acid side chain is stereospecifically introduced by reaction of the appropriate 17-keto steroid with ethyltriphenylphosphonium halides to produce the 17-ethylidene derivative which is allowed to react with acrylic acid esters or propiolic acid esters followed by hydrogenation.
    Type: Grant
    Filed: October 22, 1980
    Date of Patent: November 23, 1982
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Andrew D. Batcho, Milan R. Uskokovic, Peter M. Wovkulich
  • Patent number: 4360681
    Abstract: Novel thiophene compounds having utility as biotin intermediates and blood lipid lowering agents, as well as related processes and intermediates, are disclosed.
    Type: Grant
    Filed: June 25, 1981
    Date of Patent: November 23, 1982
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Pasquale N. Confalone, Giacomo Pizzolato, Milan R. Uskokovic
  • Patent number: 4337345
    Abstract: A process is disclosed for producing d-biotin from L cysteine via substituted thiens [3,2c] isoxazoles.
    Type: Grant
    Filed: June 25, 1981
    Date of Patent: June 29, 1982
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Enrico G. Baggiolini, Hsi L. Lee, Milan R. Uskokovic
  • Patent number: 4335120
    Abstract: A process for administering biologically active vitamin D.sub.3 and vitamin D.sub.2 materials into the blood system of a subject by providing the biologically active vitamin D.sub.3 or D.sub.2 material to the skin whereby the skin releases the biologically active vitamin D.sub.3 or D.sub.2 material into the blood system in a controlled and prolonged manner.
    Type: Grant
    Filed: November 3, 1980
    Date of Patent: June 15, 1982
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael F. Holick, Milan R. Uskokovic
  • Patent number: 4324726
    Abstract: A simple and economic chiral synthesis of optically active methyl L-acosaminide and methyl L-daunosaminide from propenyl acetate, said methyl L-acosaminide and methyl L-daunosaminide being coupling agents for the production of known antitumor agents.
    Type: Grant
    Filed: August 18, 1980
    Date of Patent: April 13, 1982
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Milan R. Uskokovic, Peter M. Wovkulich
  • Patent number: 4320056
    Abstract: A process is disclosed for producing d-biotin from L or DL-cystine ester via novel intermediates.
    Type: Grant
    Filed: March 12, 1981
    Date of Patent: March 16, 1982
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Enrico G. Baggiolini, Hsi L. Lee, Milan R. Uskokovic
  • Patent number: 4317915
    Abstract: Thiophene derivatives having utility as blood lipid lowering agents and as antiobesity agents are disclosed.
    Type: Grant
    Filed: January 14, 1980
    Date of Patent: March 2, 1982
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Pasquale N. Confalone, Giacomo Pizzolato, Milan R. Uskokovic, Marianne Rouge
  • Patent number: 4310467
    Abstract: The present disclosure is directed to a process and intermediates for the synthesis of Vitamin D.sub.3 metabolites such as 1,25-dihydroxycholecalciferol, 25-hydroxycholecalciferol and 24R,25-dihydroxycholecalciferol from 17-keto steroids via intermediates having the natural steroid configuration at the 20-position. These novel intermediates are prepared from 17-keto steroids by reaction with ethyltriphenylphosphonium halides followed by reaction with formaldehyde to form comounds having the natural steroid configuration at the 20-position and which are suitable substrates for the preparation of the aforementioned Vitamin D.sub.3 metabolites.
    Type: Grant
    Filed: October 22, 1980
    Date of Patent: January 12, 1982
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Andrew D. Batcho, Donald E. Berger, Jr., Milan R. Uskokovic
  • Patent number: 4310462
    Abstract: A process to produce methyl 3,4-anhydro-2,6-dideoxy-L-ribohexopyranoside, its enantiomer and racemate thereof.The compound is useful as an intermediate in the production of daunosamine which in turn is a prime constituent in the anti-cancer agents Daunomycin and Adriamycin. Also disclosed are novel intermediates in the process.
    Type: Grant
    Filed: October 17, 1980
    Date of Patent: January 12, 1982
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Guenter Grethe, Milan R. Uskokovic, John Sereno