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).
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Patent number: 7491711Abstract: 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: GrantFiled: September 18, 2002Date of Patent: February 17, 2009Assignee: Roche Palo Alto LLCInventor: Milan Radoje Uskokovic
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Publication number: 20040214803Abstract: 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: ApplicationFiled: June 1, 2004Publication date: October 28, 2004Inventors: Luciano Adorini, Nadia Giarratana, Silvia Gregori, Simona Smiroldo, Milan Radoje Uskokovic
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Publication number: 20040167105Abstract: This invention relates to 1,3-dihydroxy-20,20-dialkyl-vitamin D3 analogs of Formula (I): 1Type: ApplicationFiled: February 18, 2004Publication date: August 26, 2004Inventors: Percy Sarwood Manchand, Milan Radoje Uskokovic
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Publication number: 20030130241Abstract: 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: 1Type: ApplicationFiled: September 18, 2002Publication date: July 10, 2003Inventor: Milan Radoje Uskokovic
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Patent number: 6559138Abstract: 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: GrantFiled: September 18, 2002Date of Patent: May 6, 2003Assignee: Syntex (U.S.A.) LLCInventor: Milan Radoje Uskokovic
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Patent number: 6492353Abstract: 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: GrantFiled: September 3, 1998Date of Patent: December 10, 2002Assignees: Syntex LLC, Hoffmann-La Roche Inc.Inventors: Percy Sarwood Manchand, Milan Radoje Uskokovic
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Patent number: 6452028Abstract: 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: GrantFiled: August 25, 2000Date of Patent: September 17, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Andrew David Batcho, Bernard Michael Hennessy, Jerome Anthony Iacobelli, Milan Radoje Uskokovic
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Patent number: 6331642Abstract: 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: GrantFiled: May 24, 2000Date of Patent: December 18, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Andrew David Batcho, Bernard Michael Hennessy, Milan Radoje Uskokovic
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Patent number: 6329538Abstract: 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: GrantFiled: August 25, 2000Date of Patent: December 11, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Andrew David Batcho, Bernard Michael Hennessy, Jerome Anthony Iacobelli, Milan Radoje Uskokovic
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Patent number: 6040461Abstract: 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: GrantFiled: May 11, 1999Date of Patent: March 21, 2000Assignees: Hoffmann-La Roche Inc., Syntex (U.S.A.)Inventors: Andrew David Batcho, Percy Sarwood Manchand, Milan Radoje Uskokovic
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Patent number: 6030963Abstract: 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: GrantFiled: July 31, 1998Date of Patent: February 29, 2000Assignee: Hoffmann-La Roche Inc.Inventors: Jerome Anthony Iacobelli, Milan Radoje Uskokovic
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Patent number: 6030962Abstract: 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: GrantFiled: April 16, 1998Date of Patent: February 29, 2000Assignee: Synttex (U.S.A.) Inc.Inventors: Percy Sarwood Manchand, Milan Radoje Uskokovic
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Patent number: 6008209Abstract: 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: GrantFiled: April 16, 1998Date of Patent: December 28, 1999Assignees: Hoffmann-La Roche Inc., Syntex (U.S.A.)Inventors: Percy Sarwood Manchand, Milan Radoje Uskokovic
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Patent number: 5939408Abstract: 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: GrantFiled: September 29, 1998Date of Patent: August 17, 1999Assignee: Hoffman-La Roche Inc.Inventors: Andrew David Batcho, Bernard Michael Hennessy, Jerome Anthony Iacobelli, Milan Radoje Uskokovic
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Patent number: 5891866Abstract: 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: GrantFiled: April 18, 1995Date of Patent: April 6, 1999Assignee: Hoffman-La Roche Inc.Inventors: Benoit Thomas Dore, Richard Lewis Momparler, Milan Radoje Uskokovic
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Patent number: 5888994Abstract: 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: GrantFiled: May 16, 1997Date of Patent: March 30, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Bernard Michael Hennessy, Milan Radoje Uskokovic
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Patent number: 5856317Abstract: 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: GrantFiled: May 24, 1996Date of Patent: January 5, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Benoit Thomas Dore, Richard Lewis Momparler, Milan Radoje Uskokovic
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Patent number: 5840718Abstract: 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: GrantFiled: March 6, 1997Date of Patent: November 24, 1998Assignee: Hoffmann-La Roche Inc.Inventors: Bernard Michael Hennessy, Jerome Anthony Iacobelli, Milan Radoje Uskokovic
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Patent number: 5811414Abstract: 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: GrantFiled: May 16, 1997Date of Patent: September 22, 1998Assignee: Hoffmann-La Roche Inc.Inventors: Graeme Findlay Bryce, Milan Radoje Uskokovic
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Patent number: 5804574Abstract: 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: GrantFiled: September 17, 1997Date of Patent: September 8, 1998Assignee: Hoffmann-La Roche Inc.Inventors: Graeme Findlay Bryce, Milan Radoje Uskokovic