Patents by Inventor Milan Radoje Uskokovic

Milan Radoje 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: 7491711
    Abstract: The present invention provides a method for treating osteoporosis, hyperparathyroidism or an autoimmune disease in a patient by administering to the patient a 3-desoxy vitamin D3 analog of the formula: a prodrug or a salt thereof, where the dotted line, R1, R2, R3, R4 and L are those defined herein. The present invention also provides methods for producing 3-desoxy vitamin D3 analog of Formula I.
    Type: Grant
    Filed: September 18, 2002
    Date of Patent: February 17, 2009
    Assignee: Roche Palo Alto LLC
    Inventor: Milan Radoje Uskokovic
  • Publication number: 20040214803
    Abstract: The present invention is concerned with the use of 1,25-dihydroxy-16,23Z-diene-26,27-hexafluoro-19-nor vitamin D3 for the manufacture of a medicament for the prevention and/or treatment of autoimmune diabetes as well as for the manufacture of a medicament for preventing and/or treating allograft rejection, it is further concerned with a method for preventing and/or treating such diseases by administering 1,25-dihydroxy-16,23Z-diene-26,27-hexafluoro-19-nor vitamin D3 in an amount effective to prevent and/or to treat such diseases alone or in combination with other immunosuppressive agents.
    Type: Application
    Filed: June 1, 2004
    Publication date: October 28, 2004
    Inventors: Luciano Adorini, Nadia Giarratana, Silvia Gregori, Simona Smiroldo, Milan Radoje Uskokovic
  • Publication number: 20040167105
    Abstract: This invention relates to 1,3-dihydroxy-20,20-dialkyl-vitamin D3 analogs of Formula (I): 1
    Type: Application
    Filed: February 18, 2004
    Publication date: August 26, 2004
    Inventors: Percy Sarwood Manchand, Milan Radoje Uskokovic
  • Publication number: 20030130241
    Abstract: The present invention provides a method for treating osteoporosis, hyperparathyroidism or an autoimmune disease in a patient by administering to the patient a 3-desoxy vitamin D3 analog of the formula: 1
    Type: Application
    Filed: September 18, 2002
    Publication date: July 10, 2003
    Inventor: Milan Radoje Uskokovic
  • Patent number: 6559138
    Abstract: The present invention provides 3-desoxy vitamin D3 analog esters of the formula: and methods for use and preparation of the same, wherein the dotted line, R1, R2, R3, R4 and L are those defined herein.
    Type: Grant
    Filed: September 18, 2002
    Date of Patent: May 6, 2003
    Assignee: Syntex (U.S.A.) LLC
    Inventor: Milan Radoje Uskokovic
  • Patent number: 6492353
    Abstract: This invention relates to 1,3-dihydroxy-20,20-dialkyl-vitamin D3 analogs of Formula (I): compositions comprising the analogs, methods of preparing the analogs and methods of treatment of osteoporosis, secondary hyperparathyroidism, cancer and autoimmune diseases using such analogs.
    Type: Grant
    Filed: September 3, 1998
    Date of Patent: December 10, 2002
    Assignees: Syntex LLC, Hoffmann-La Roche Inc.
    Inventors: Percy Sarwood Manchand, Milan Radoje Uskokovic
  • Patent number: 6452028
    Abstract: A compound of the formula wherein R is hydrogen or hydroxy, each R1 is ethyl, propyl, butyl, isopropyl or t-butyl, X is ═CH2, or when R is hydroxy, X is hydrogen or ═CH2, and A is —C≡C—, or —CH2—CH2—. These compounds are useful for the treatment of hyperproliferative disorders, skin diseases, and sebaceous gland diseases.
    Type: Grant
    Filed: August 25, 2000
    Date of Patent: September 17, 2002
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Andrew David Batcho, Bernard Michael Hennessy, Jerome Anthony Iacobelli, Milan Radoje Uskokovic
  • Patent number: 6331642
    Abstract: Compounds of the formula wherein R1 is hydrogen or an alkyl group; R2 is hydrogen or an alkyl group; or R1, R2 and C20 together are cyclopropyl; R3 is alkyl, hydroxy-alkyl or fluoroalkyl; and R4 is alkyl, hydroxy-alkyl or fluoroalkyl which are useful in the treatment of breast cancer, prostate cancer, myeloid leukemia benign prostate growth, baldness and osteoporosis.
    Type: Grant
    Filed: May 24, 2000
    Date of Patent: December 18, 2001
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Andrew David Batcho, Bernard Michael Hennessy, Milan Radoje Uskokovic
  • Patent number: 6329538
    Abstract: A compound of the formula wherein R is hydrogen or hydroxy, each R2 is independently H or halogen, X is ═CH2, or when R is hydroxy, X is hydrogen or ═CH2, and A is —C≡C—, or —CH2—CH2—, provided that when A is —CH2—CH2—, R2 is H.
    Type: Grant
    Filed: August 25, 2000
    Date of Patent: December 11, 2001
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Andrew David Batcho, Bernard Michael Hennessy, Jerome Anthony Iacobelli, Milan Radoje Uskokovic
  • Patent number: 6040461
    Abstract: The invention relates to a process for the preparation of vitamin D.sub.3 compounds of formula I. ##STR1## Wherein A is a single or a double bond; B is a single, cis-double, trans double or a triple bond; R.sub.1 and R.sub.2 are independently hydrogen, a lower alkyl, e.g., a C.sub.1 -C.sub.4 alkyl; R.sub.3 and R.sub.4 are independently a lower alkyl, e.g., C.sub.1 -C.sub.4 alkyl, a hydroxyalkyl, and a haloalkyl, e.g., a fluoroalkyl; and X and Y are independently hydrogen or hydroxy in the case when B is a single or a double bond.
    Type: Grant
    Filed: May 11, 1999
    Date of Patent: March 21, 2000
    Assignees: Hoffmann-La Roche Inc., Syntex (U.S.A.)
    Inventors: Andrew David Batcho, Percy Sarwood Manchand, Milan Radoje Uskokovic
  • Patent number: 6030963
    Abstract: The invention relates to a compound of the formula ##STR1## wherein A is ##STR2## Et is ethyl, and R is hydroxy and R.sup.1 is hydrogen or .dbd.CH.sub.2 or R is hydrogen or fluoro and R.sup.1 is .dbd.CH.sub.2. Compounds of formula I stimulate HL-60 cell differentiation. Accordingly, the compounds of formula I are useful as agents for the treatment of neoplastic diseases, such as leukemia.
    Type: Grant
    Filed: July 31, 1998
    Date of Patent: February 29, 2000
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jerome Anthony Iacobelli, Milan Radoje Uskokovic
  • Patent number: 6030962
    Abstract: This invention provides Vitamin D.sub.3 analogs of the Formula I ##STR1## wherein: X is H.sub.2 or CH.sub.2 ;Y is hydrogen, hydroxy or fluorine;Z is hydroxy;R.sub.1 and R.sub.2 are a (C.sub.1 -C.sub.4) alkyl or fluoroalkyl, or R.sub.1 and R.sub.2 together with C.sub.25 form a (C.sub.3 -C.sub.6) cycloalkyl or cyclofluoroalkyl;R.sub.3 and R.sub.4 are a (C.sub.1 -C.sub.4) alkyl or fluoroalkyl, or R.sub.3 and R.sub.4 together with C.sub.25, form a (C.sub.3 -C.sub.6)cycloalkyl or cyclofluoroalkyl;A is a single bond or a double bond;B.sub.1 is a single bond, an E-double bond, a Z-double bond or a triple bond; andB.sub.2 is a single bond, an E-double bond, a Z-double bond or a triple bond; and prodrugs thereof, intermediates and methods for preparation of these analogs, pharmaceutical compositions containing such analogs and methods for treatment of osteoporosis, hyperparathyroidism and autoimmune diseases.
    Type: Grant
    Filed: April 16, 1998
    Date of Patent: February 29, 2000
    Assignee: Synttex (U.S.A.) Inc.
    Inventors: Percy Sarwood Manchand, Milan Radoje Uskokovic
  • Patent number: 6008209
    Abstract: This invention provides a method of treating or preventing neoplastic diseases. The method comprises adminstering to a host in need of such treatment or prevention an effective amount of a Vitamin D.sub.3 analog of the Formula I wherein:X is H.sub.2 or CH.sub.2 ;Y is hydrogen, hydroxy or fluorine;Z is hydroxy;R.sub.1 and R.sub.2 are a (C.sub.1 -C.sub.4) alkyl or fluoroalkyl, or R.sub.1 and R.sub.2 together with C.sub.25 form a (C.sub.3 -C.sub.6) cycloalkyl or cyclofluoroalkyl;R.sub.3 and R.sub.4 are a (C.sub.1 -C.sub.4) alkyl or fluoroalkyl, or R.sub.3 and R.sub.4 together with C.sub.25' form a (C.sub.3 -C.sub.6)cycloalkyl or cyclofluoroalkyl;A is a single bond or a double bond;B.sub.1 is a single bond, an E-double bond, a Z-double bond or a triple bond; andB.sub.2 is a single bond, an E-double bond, a Z-double bond or a triple bond; or a prodrug thereof.
    Type: Grant
    Filed: April 16, 1998
    Date of Patent: December 28, 1999
    Assignees: Hoffmann-La Roche Inc., Syntex (U.S.A.)
    Inventors: Percy Sarwood Manchand, Milan Radoje Uskokovic
  • Patent number: 5939408
    Abstract: Compounds of the formula ##STR1## wherein R is hydrogen, fluorine, or hydroxyl, each R.sub.2 is lower alkyl or C(R.sub.3).sub.3 and R.sub.3 is halogen, X is .dbd.CH.sub.2 or when R is hydroxy, X is hydrogen or .dbd.CH.sub.2, and A is --C.tbd.C-- ##STR2## or --CH.sub.2 --CH.sub.2 --, which are useful in the treatment of hyperproliferative skin disorders, neoplastic diseases, and sebaceous gland diseases.
    Type: Grant
    Filed: September 29, 1998
    Date of Patent: August 17, 1999
    Assignee: Hoffman-La Roche Inc.
    Inventors: Andrew David Batcho, Bernard Michael Hennessy, Jerome Anthony Iacobelli, Milan Radoje Uskokovic
  • Patent number: 5891866
    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: April 18, 1995
    Date of Patent: April 6, 1999
    Assignee: Hoffman-La Roche Inc.
    Inventors: Benoit Thomas Dore, Richard Lewis Momparler, Milan Radoje Uskokovic
  • Patent number: 5888994
    Abstract: A compound of formula I ##STR1## wherein R is hydrogen, fluorine or hydroxy, and X is .dbd.CH.sub.2 or when R is hydroxy, X is hydrogen or .dbd.CH.sub.2 which are useful in the treatment of hyperproliferative disorders, neoplastic diseases and sebaceous gland diseases.
    Type: Grant
    Filed: May 16, 1997
    Date of Patent: March 30, 1999
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bernard Michael Hennessy, Milan Radoje Uskokovic
  • Patent number: 5856317
    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: May 24, 1996
    Date of Patent: January 5, 1999
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Benoit Thomas Dore, Richard Lewis Momparler, Milan Radoje Uskokovic
  • Patent number: 5840718
    Abstract: The invention relates to a compound of the formula ##STR1## wherein R is hydroxy and R.sup.1 is H.sub.2 or .dbd.CH.sub.2 or R is hydrogen or fluoro and R.sup.1 is .dbd.CH.sub.2 and (b) an inert carrier.Compounds of formula I are useful as agents for the treatment of hyperproliferative skin diseases, such as psoriasis, neoplastic diseases, such as leukemia, and sebaceous gland diseases, such as acne and sebhorreic dermatitis.
    Type: Grant
    Filed: March 6, 1997
    Date of Patent: November 24, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bernard Michael Hennessy, Jerome Anthony Iacobelli, Milan Radoje Uskokovic
  • Patent number: 5811414
    Abstract: The use of compounds of formula I as topical agents to combat the disorders of the skin, produced by photodamage, which disorders include wrinkling, elastosis and premature aging is described. Compounds of formula I are ##STR1## wherein R is hydrogen, fluorine, or hydroxy, R.sub.2 is hydrogen, lower alkyl or halogen, X is .dbd.CH.sub.2 or when R is hydroxy X is hydrogen or .dbd.CH.sub.2, ##STR2## --CH.sub.2 --CH.sub.2 --, provided that when A is --CH.sub.2 --CH.sub.2 --, R.sub.2 is hydrogen or lower alkyl.
    Type: Grant
    Filed: May 16, 1997
    Date of Patent: September 22, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Graeme Findlay Bryce, Milan Radoje Uskokovic
  • Patent number: 5804574
    Abstract: The use of compounds of formula I as topical agents to combat the disorders of the skin, produced by photodamage, which disorders include wrinkling, elastosis and premature aging is described. Compounds of formula I are ##STR1## wherein R.sub.1 is hydrogen, hydroxy or fluorine, R.sub.2 is hydrogen or halogen and A is --C.tbd.C--, --C.dbd.C-- or --CH.sub.2 --CH.sub.2 --, provided that when A is --CH.sub.2 --CH.sub.2 --, R.sub.2 is hydrogen.
    Type: Grant
    Filed: September 17, 1997
    Date of Patent: September 8, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Graeme Findlay Bryce, Milan Radoje Uskokovic