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).

  • Publication number: 20090298800
    Abstract: The invention provides vitamin D3 analogs of cholecalciferol, substituted at carbons-26 and 27 with deuterated alkyl groups, e.g., trideuteromethyl, wherein carbon-16 is a single or double bond, and carbon-23 is a single, double, or triple bond. The invention provides pharmaceutically acceptable esters, salts, and prodrugs thereof. Methods for using the compounds to treat vitamin D3 associated states, and pharmaceutical compositions containing the compounds are also disclosed.
    Type: Application
    Filed: September 21, 2006
    Publication date: December 3, 2009
    Applicant: BioXell S.p.A.
    Inventors: Milan R. Uskokovic, Stanislaw Marczak, Pawel Jankowski, Luciano Adorini
  • Publication number: 20090298799
    Abstract: The invention provides for methods of using 20-methyl Gemini vitamin D3 compounds to treat osteoporosis and secondary hyperparathyroidism.
    Type: Application
    Filed: March 23, 2006
    Publication date: December 3, 2009
    Applicants: BioXell S.p.A., Galapagos SASU
    Inventors: Luciano Adorini, Milan R. Uskokovic, Michèle Resche-Rignon
  • Publication number: 20090137828
    Abstract: The invention provides a method of producing 20-methyl vitamin D3 compounds of formula (I). The method includes allylic and olefin oxidation, de-carbonylation, carbonyl reduction, fluoride substitution, epoxide deoxygenation, and Wittig-type couplings.
    Type: Application
    Filed: August 18, 2006
    Publication date: May 28, 2009
    Applicant: BIOXELL S.P.A.
    Inventors: Milan R. Uskokovic, Stanislaw Marczak, Ralf Loo, Marcel Van Der Sluis, Pawel Jankowski, Hubert Maehr
  • Publication number: 20090099140
    Abstract: The invention provides 20-alkyl Gemini vitamin D3 compounds, methods for using the compounds to treat vitamin D3 associated states and pharmaceutical compositions containing the compounds.
    Type: Application
    Filed: March 23, 2006
    Publication date: April 16, 2009
    Applicant: BioXell S.p.A.
    Inventors: Pawel Jankowski, Milan R. Uskokovic, Luciano Adorini
  • Publication number: 20080318911
    Abstract: The invention provides vitamin D3 analogs of cholecalciferol, substituted at carbon 20 with cycloalkyl, e.g., cyclopropyl, wherein carbon-16 is a double bond, and carbon-23 is a single, double, or triple bond. Various alkyl or haloalkyl substitutions are incorporated as carbon-25. The invention provides pharmaceutically acceptable esters, salts, and prodrugs thereof. Methods for using the compounds to treat vitamin D3 associated states, and pharmaceutical compositions containing the compounds are also disclosed.
    Type: Application
    Filed: September 23, 2005
    Publication date: December 25, 2008
    Applicant: BIOXELL S.P.A.
    Inventors: Milan R. Uskokovic, Luciano Adorini, Guiseppe Penna, Enrico Colli, Stanislaw Marczak
  • Publication number: 20080280859
    Abstract: The invention provides Gemini vitamin D3 compounds, methods for using the compounds to treat vitamin D3 associated states and pharmaceutical compositions containing the compounds.
    Type: Application
    Filed: October 19, 2005
    Publication date: November 13, 2008
    Applicant: BioXell S.p.A.
    Inventors: Luciano Adorini, Giuseppe Penna, Milan R. Uskokovic, Hubert Maehr
  • Publication number: 20080064668
    Abstract: The invention provides (1,3)di-acylated vitamin D3 analogs of cholecalciferol, substituted at carbon (20) with methyl or cyclopropyl wherein carbon (16) is a single or double bond, and carbon (23) is a single, double, or triple bond. Various alkyl or haloalkyl substitutions are incorporated at carbon (25). The invention provides pharmaceutically acceptable esters, salts, and pro-drugs thereof. Methods for using the compounds to treat vitamin D3 associated states, and pharmaceutical compositions containing the compounds are also disclosed.
    Type: Application
    Filed: September 24, 2004
    Publication date: March 13, 2008
    Applicant: BioXell S.p.A.
    Inventors: Milan R. Uskokovic, Luciano Adorini, Giuseppe Penna, Enrico Colli
  • Publication number: 20030083319
    Abstract: This invention relates to 1,3-dihydroxy-20,20-dialkyl-vitamin D3 analogs of Formula (I): 1
    Type: Application
    Filed: July 25, 2002
    Publication date: May 1, 2003
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Percy S. Manchand, Milan R. Uskokovic
  • Patent number: 5872113
    Abstract: Fluorinated Vitamin D.sub.3 analogs, intermediates for their preparation, compositions comprising the analogs and methods of treatment of osteoporosis and related conditions with these and related analogs are provided.
    Type: Grant
    Filed: May 16, 1997
    Date of Patent: February 16, 1999
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: John J. Nestor, Jr., Percy S. Manchand, Milan R. Uskokovic, Brian H. Vickery
  • Patent number: 5612328
    Abstract: Compounds of the formula ##STR1## wherein R is hydrogen, hydroxy, or fluorine, and X is H.sub.2 or .dbd.CH.sub.2 are useful as agents for the treatment of hyperproliferative disorders of the skin such as psoriasis, as agents for the treatment of cancer, such as, leukemia, and as agents for the treatment of sebaceous gland diseases, such as, acne and seborrheic dermatitis.
    Type: Grant
    Filed: February 1, 1996
    Date of Patent: March 18, 1997
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Barbara J. Baggiolini, Shian-Jan Shiuey, Milan R. Uskokovic
  • Patent number: 5547947
    Abstract: A method of inducing inhibition or loss of cell proliferation in solid tumors utilizing a Vitamin D.sub.3 analog, as well as a method of inducing loss of cell proliferation in solid tumors utilizing trans retinoic acid and a Vitamin D.sub.3 analog.In another aspect, a method of inducing inhibition or loss of cell proliferation in solid tumors utilizing a Vitamin D.sub.3 metabolite, as well as a method of inducing loss of cell proliferation in solid tumors utilizing trans retinoic acid and a Vitamin D.sub.3 metabolite.
    Type: Grant
    Filed: November 30, 1994
    Date of Patent: August 20, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Benoit T. Dore, Richard L. Momparler, Milan R. Uskokovic
  • Patent number: 5512554
    Abstract: Compounds of the formula ##STR1## wherein R is hydrogen, hydroxy, or fluorine, and X is H.sub.2 or .dbd.CH.sub.2 are useful as agents for the treatment of hyperproliferative disorders of the skin such as psoriasis, as agents for the treatment of cancer, such as, leukemia, and as agents for the treatment of sebaceous gland diseases, such as, acne and seborrheic dermatitis.
    Type: Grant
    Filed: April 11, 1995
    Date of Patent: April 30, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Enrico G. Baggiolini, deceased, Shian-Jan Shiuey, Milan R. Uskokovic
  • Patent number: 5451574
    Abstract: Compounds of the formula ##STR1## wherein R is hydrogen, hydroxy, or fluorine, and X is H.sub.2 are useful as agents for the treatment of hyperproliferative disorders of the skin such as psoriasis, as agents for the treatment of cancer, such as, leukemia, and as agents for the treatment of sebaceous gland diseases, such as, acne and seborrheic dermatitis.
    Type: Grant
    Filed: January 18, 1994
    Date of Patent: September 19, 1995
    Assignee: Hoffman-La Roche Inc.
    Inventors: Enrico G. Baggiolini, deceased, Barbara J. Baggiolini, Shian-Jan Shiuey, Milan R. Uskokovic
  • Patent number: 5428029
    Abstract: Compounds of the formula ##STR1## wherein R is hydrogen, hydroxy, or fluorine, X is H.sub.2 or .dbd.CH.sub.2, and the 23,24-double bond is E or Z, are useful as agents for the treatment of hyperproliferative disorders of the skin such as psoriasis, as agents for the treatment of tumors such as breast cancer, as agents for the treatment of neoplastic diseases such as leukemia, and as agents for the treatment of sebaceous gland diseases such as acne and seborrheic dermatitis.
    Type: Grant
    Filed: November 24, 1993
    Date of Patent: June 27, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Thomas I. Doran, Bernard M. Hennessy, John A. McLane, Giacomo Pizzolato, Farhad Sedarati, Milan R. Uskokovic
  • Patent number: 5401733
    Abstract: The invention relates to the compounds 1,25-dihydroxy-16-ene-24-oxo-cholecalciferol and 1,24,25-trihydroxy-16-ene-cholecalciferol which stimulate differentiation of HL-60 cells, rendering them useful as an agent for the treatment of neoplastic diseases such as leukemia, and also decrease proliferation of human keratinocytes, rendering them useful as an agent for the treatment of hyperproliferative disorders of the skin such as psoriasis.
    Type: Grant
    Filed: October 1, 1993
    Date of Patent: March 28, 1995
    Assignees: Hoffmann-La Roche Inc., Satyanarayama G. Reddy
    Inventors: John A. McLane, Satyanarayama G. Reddy, Milan R. Uskokovic
  • Patent number: 5393900
    Abstract: The invention comprises compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen or acyl; provided that only one of R.sup.1 or R.sup.2 is hydrogen, useful in the treatment of hyperproliferative skin diseases and sebaceous gland diseases. The invention also includes a process for making these compounds and steroid intermediates of the process.
    Type: Grant
    Filed: June 7, 1994
    Date of Patent: February 28, 1995
    Assignee: Hoffmann-La Roche inc.
    Inventors: Thomas I. Doran, John A. McLane, Masami Okabe, Michelangelo Scalone, Milan R. Uskokovic
  • Patent number: 5384314
    Abstract: This invention is for 1.alpha.-fluoro-25-hydroxy-16-ene-23-yne-cholecalciferol, which can be further characterized by the formula: ##STR1## and which is useful as an agent for the treatment of sebaceous gland diseases such as acne and sebhorreic dermatitis.
    Type: Grant
    Filed: March 11, 1994
    Date of Patent: January 24, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Thomas I. Doran, Shian-Jan Shiuey, Milan R. Uskokovic
  • Patent number: 5342833
    Abstract: The invention is drawn to compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen or acyl; provided that only one of R.sup.1 or R.sup.2 is hydrogen, useful in the treatment of hyperproliferative skin diseases and sebaceous gland diseases.
    Type: Grant
    Filed: November 22, 1993
    Date of Patent: August 30, 1994
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Thomas I. Doran, John A. McLane, Masami Okabe, Michelangelo Scalone, Milan R. Uskokovic
  • Patent number: 5258559
    Abstract: A process for the preparation of [1R-(1.beta.(R*),3a.alpha.,4.alpha.,7a.beta.)]octahydro-1-(5-hydroxy-1,5-d imethyl(hexyl)-7a-methyl-4H-inden-4-one which comprises reacting [1R-(1.beta.(R*)3a.alpha.,7a.beta.)]octahydro-1-(1,5-dimethylhexyl)-7a-met hyl-4H-inden-4-ol or [1R-(1.beta.(R*) 3a.alpha.,7a.beta.)]octahydro-1-(1,5-dimethylhexyl)-7a-methyl-4H-inden-4-o ne with sodium metaperiodate and ruthenium chloride hydrate.
    Type: Grant
    Filed: May 26, 1992
    Date of Patent: November 2, 1993
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Milan R. Uskokovic
  • Patent number: 5247123
    Abstract: The invention is directed to deuterated vitamin D analogs, and processes and intermediates for their preparation. The end products, that is the deuterated vitamin D analogs, are useful for the treatment osteoporosis and cutaneous inflammations such as psoriasis, and contact dermatitis.
    Type: Grant
    Filed: July 2, 1992
    Date of Patent: September 21, 1993
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Enrico G. Baggiolini, Bernard M. Hennessy, Milan R. Uskokovic