Patents by Inventor Rafal R. Sicinski

Rafal R. Sicinski 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: 20170253546
    Abstract: Disclosed are 2-methylene analogs of vitamin D3 and related compounds, their biological activities, and various pharmaceutical uses for these analogs. Particularly disclosed are 1?-hydroxy-2-methylene-vitamin D3, (20S)-1?-hydroxy-2-methylene-vitamin D3, and (5E)-1?,25-dihydroxy-2-methylene-vitamin D3, their biological activities, and various pharmaceutical uses for these compounds including methods of treating and/or preventing bone diseases and disorders.
    Type: Application
    Filed: May 18, 2017
    Publication date: September 7, 2017
    Applicant: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Izabela K. Sibilska, Rafal R. Sicinski, Lori A. Plum
  • Patent number: 9688596
    Abstract: Disclosed are 2-methylene analogs of vitamin D3 and related compounds, their biological activities, and various pharmaceutical uses for these analogs. Particularly disclosed are 1?-hydroxy-2-methylene-vitamin D3, (20S)-1?-hydroxy-2-methylene-vitamin D3, and (5E)-1?,25-dihydroxy-2-methylene-vitamin D3, their biological activities, and various pharmaceutical uses for these compounds including methods of treating and/or preventing bone diseases and disorders.
    Type: Grant
    Filed: July 26, 2016
    Date of Patent: June 27, 2017
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Izabela K. Sibilska, Rafal R. Sicinski, Lori A. Plum
  • Publication number: 20170036977
    Abstract: Disclosed are 2-methylene analogs of vitamin D3 and related compounds, their biological activities, and various pharmaceutical uses for these analogs. Particularly disclosed are 1?-hydroxy-2-methylene-vitamin D3, (20S)-1?-hydroxy-2-methylene-vitamin D3, and (5E)-1?,25-dihydroxy-2-methylene-vitamin D3, their biological activities, and various pharmaceutical uses for these compounds including methods of treating and/or preventing bone diseases and disorders.
    Type: Application
    Filed: July 26, 2016
    Publication date: February 9, 2017
    Applicant: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Izabela K. Sibilska, Rafal R. Sicinski, Lori A. Plum
  • Patent number: 8993547
    Abstract: This invention discloses 3-desoxy-2-methylene-19-nor-vitamin D analogs, and specifically (20S)-3-desoxy-2-methylene-1?,25-dihydroxy-19-nor-vitamin D3 and (20R)-3-desoxy-2-methylene-1?,25-dihydroxy-19-nor-vitamin D3 as well as pharmaceutical uses therefor. These compounds exhibit relatively high binding activity and pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to monocytes thus evidencing use as anti-cancer agents especially for the treatment or prevention of osteosarcoma, leukemia, colon cancer, breast cancer, skin cancer or prostate cancer. These compounds also exhibit relatively high calcemic activity evidencing use in the treatment of bone diseases.
    Type: Grant
    Filed: June 13, 2012
    Date of Patent: March 31, 2015
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Lori A. Plum, Rafal R. Sicinski, Izabela Sibilska, Margaret Clagett-Dame
  • Patent number: 8729054
    Abstract: This invention discloses 3-desoxy-2-methylene-vitamin D analogs, and specifically (20S)-3-desoxy-1?,25-dihydroxy-2-methylene-vitamin D3 and (20R)-3-desoxy-1?,25-dihydroxy-2-methylene-vitamin D3 as well as pharmaceutical uses therefor. These compounds exhibit relatively high binding activity and pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to monocytes thus evidencing use as anti-cancer agents especially for the treatment or prevention of osteosarcoma, leukemia, colon cancer, breast cancer, skin cancer or prostate cancer. These compounds also exhibit relatively high calcemic activity evidencing use in the treatment of bone diseases.
    Type: Grant
    Filed: October 3, 2012
    Date of Patent: May 20, 2014
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Lori A. Plum, Rafal R. Sicinski, Izabela Sibilska
  • Patent number: 8642579
    Abstract: This invention discloses 1-desoxy-2-methylene-19-nor-vitamin D analogs, and specifically (20S)-25-hydroxy-1-desoxy-2-methylene-19-nor-vitamin D3 and pharmaceutical uses therefor. This compound exhibits relatively high binding activity and pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent especially for the treatment or prevention of leukemia, colon cancer, breast cancer, skin cancer or prostate cancer.
    Type: Grant
    Filed: September 30, 2010
    Date of Patent: February 4, 2014
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Katarzyna M. Barycka, Izabela Sibilska, Lori A. Plum, Margaret Clagett-Dame, Rafal Barycki, Rafal R. Sicinski, Katarzyna Plonska-Ocypa
  • Patent number: 8518917
    Abstract: This invention discloses 2-methylene-19-nor-vitamin D analogs, and specifically (20S)-25-hydroxy-2-methylene-19-nor-vitamin D3 and (20R)-25-hydroxy-2-methylene-19-nor-vitamin D3, as well as pharmaceutical uses therefor. These compounds exhibit relatively high binding activity and pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent especially for the treatment or prevention of osteosarcoma, leukemia, colon cancer, breast cancer, skin cancer or prostate cancer. Although these compounds have relatively low calcemic activities they may also be useful in the treatment of bone diseases due to their ability to act as prodrugs in vivo.
    Type: Grant
    Filed: October 21, 2011
    Date of Patent: August 27, 2013
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Izabela Sibliska, Lori A. Plum, Margaret Clagett-Dame, Rafal R. Sicinski, Katarzyna M. Barycka, Katarzyna Plonska-Ocypa, Rafal Barycki
  • Publication number: 20130178449
    Abstract: This invention discloses 2-methylene-20(21)-dehydro-19,24,25,26,27-pentanor-vitamin D analogs, and specifically 2-methylene-20(21)-dehydro-19,24,25,26,27-pentanor-1?-hydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits relatively high transcription activity as well as pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also shows lower activity in vivo on bone calcium mobilization and lower in vivo intestinal calcium transport activity as compared to the native hormone 1?,25-dihydroxyvitamin D3, and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as secondary hyperparathyroidism and renal osteodystrophy.
    Type: Application
    Filed: July 12, 2012
    Publication date: July 11, 2013
    Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATION
    Inventors: Hector F. DeLuca, Margaret Clagett-Dame, Lori A. Plum, Agnieska Glebocka, Rafal R. Sicinski
  • Patent number: 8410080
    Abstract: This invention discloses 2-methylene-vitamin D analogs, and specifically (20S)-1?,25 -dihydroxy-2-methylene-vitamin D3 as well as (5E)-(20S)-1?,25-dihydroxy-2 -methylene-vitamin D3 and (20R)-1?,25-dihydroxy-2-methylene-vitamin D3, as well as pharmaceutical uses therefor. These compounds exhibit relatively high binding activity and pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent especially for the treatment or prevention of osteosarcoma, leukemia, colon cancer, breast cancer, skin cancer or prostate cancer. These compounds also have relatively high calcemic activities evidencing use in the treatment of bone diseases.
    Type: Grant
    Filed: October 11, 2012
    Date of Patent: April 2, 2013
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Lori A. Plum, Rafal R. Sicinski, Izabela Sibilska
  • Patent number: 8399438
    Abstract: This invention discloses 2?-methyl-19-nor-vitamin D analogs, and specifically 2?-methyl-19-nor-1?-hydroxy-homopregnacalciferol and pharmaceutical uses therefor. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also has little, if any, calcemic activity and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.
    Type: Grant
    Filed: November 18, 2005
    Date of Patent: March 19, 2013
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Rafal R. Sicinski, Lori A. Plum, Margaret Clagett-Dame, Sumithra Gowlugari
  • Publication number: 20120322775
    Abstract: This invention discloses 3-desoxy-2-methylene-19-nor-vitamin D analogs, and specifically (20S)-3-desoxy-2-methylene-1?,25-dihydroxy-19-nor-vitamin D3 and (20R)-3-desoxy-2-methylene-1?,25-dihydroxy-19-nor-vitamin D3 as well as pharmaceutical uses therefor. These compounds exhibit relatively high binding activity and pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to monocytes thus evidencing use as anti-cancer agents especially for the treatment or prevention of osteosarcoma, leukemia, colon cancer, breast cancer, skin cancer or prostate cancer. These compounds also exhibit relatively high calcemic activity evidencing use in the treatment of bone diseases.
    Type: Application
    Filed: June 13, 2012
    Publication date: December 20, 2012
    Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATION
    Inventors: Hector F. DeLuca, Lori A. Plum, Rafal R. Sicinski, Izabela Sibilska, Margaret Clagett-Dame
  • Patent number: 8217023
    Abstract: 19-nor-vitamin D analogs having an additional cyclopentene ring connecting carbon 1 and carbon 2, or connecting carbon 3 and carbon-2 of the A-ring of the analog, and pharmaceutical uses therefore, are described. These compounds exhibit selective in vitro activities, making them therapeutic agents for the treatment or prophylaxis of some types of cancers, particularly leukemia, colon cancer, breast cancer, skin cancer or prostate cancer.
    Type: Grant
    Filed: September 30, 2010
    Date of Patent: July 10, 2012
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Agnieszka Glebocka, Lori A. Plum, Margaret Clagett-Dame, Rafal R. Sicinski
  • Publication number: 20120157418
    Abstract: This invention discloses 2-methylene-19-nor-vitamin D analogs, and specifically (20S)-25-hydroxy-2-methylene-19-nor-vitamin D3 and (20R)-25-hydroxy-2-methylene-19-nor-vitamin D3, as well as pharmaceutical uses therefor. These compounds exhibit relatively high binding activity and pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent especially for the treatment or prevention of osteosarcoma, leukemia, colon cancer, breast cancer, skin cancer or prostate cancer. Although these compounds have relatively low calcemic activities they may also be useful in the treatment of bone diseases due to their ability to act as prodrugs in vivo.
    Type: Application
    Filed: October 21, 2011
    Publication date: June 21, 2012
    Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATION
    Inventors: Hector F. DeLuca, Izabela Sibilska, Lori A. Plum, Margaret Clagett-Dame, Rafal R. Sicinski, Katarzyna M. Barycka, Katarzyna Plonska-Ocypa, Rafal Barycki
  • Patent number: 8193171
    Abstract: 13,13-Dimethyl-des-C,D analogs of 1?,25-dihydroxy-19-nor-vitamin D3 compounds and topical composition dosage forms thereof, and methods of treating skin conditions thereof. Exemplary active pharmaceutical ingredients include (1R,3R)-5-[(E)-(S)-11?-hydroxy-5?,5?,7?,11?-tetramethyl-dodec-2?-enylidene]-2-methylene-cyclohexane-1,3-diol, (1R,3R)-5-[(Z)-(S)-11?-hydroxy-5?,5?,7?,11?-tetramethyl-dodec-2?-enylidene]-2-methylene-cyclohexane-1,3-diol, (1R,3R)-5-[(E)-(R)-11?-hydroxy-5?,5?,7?,11?-tetramethyl-dodec-2?-enylidene]-2-methylene-cyclohexane-1,3-diol, and (1R,3R)-5-[(Z)-(R)-11?-hydroxy-5?,5?,7?,11?-tetramethyl-dodec-2?-enylidene]-2-methylene-cyclohexane-1,3-diol.
    Type: Grant
    Filed: January 22, 2009
    Date of Patent: June 5, 2012
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Margaret Clagett-Dame, Lori A. Plum, Rafal R. Sicinski, Katarzyna Plonska-Ocypa, Nirca J. Nieves, Pawel Grzywacz
  • Patent number: 8178517
    Abstract: This invention discloses 6-methylvitamin D3 analogs, and specifically 1?,25-dihydroxy-6-methylvitamin D3, and pharmaceutical uses therefor. This compound exhibits vitamin D receptor binding activity and transcription activity as well as activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent, especially for the treatment or prevention of leukemia, colon cancer, breast cancer, skin cancer or prostate cancer. This compound also exhibits low in vivo calcemic activity, but because it binds the receptor with the same affinity as the native hormone calcitriol, it may act as an antagonist to inhibit development of hypercalcemia.
    Type: Grant
    Filed: September 30, 2010
    Date of Patent: May 15, 2012
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Katarzyna Sokolowska, Lori A. Plum, Margaret Clagett-Dame, Rafal R. Sicinski, Antonio MouriƱo
  • Publication number: 20120071562
    Abstract: This invention discloses 2?-methyl-19-nor-(20S)-vitamin D analogs, and specifically 2?-methyl-19-nor-(20S)-1?-hydroxy-bishomopregnacalciferol and pharmaceutical uses therefor. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also has little, if any, calcemic activity and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.
    Type: Application
    Filed: November 22, 2011
    Publication date: March 22, 2012
    Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATION
    Inventors: Hector F. DeLuca, Rafal R. Sicinski, Lori A. Plum, Margaret Clagett-Dame
  • Patent number: 8093232
    Abstract: This invention discloses 2?-methyl-19-nor-(20S)-vitamin D analogs, and specifically 2?-methyl-19-nor-(20S)-1?-hydroxy-bishomopregnacalciferol and pharmaceutical uses therefor. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also has little, if any, calcemic activity and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.
    Type: Grant
    Filed: July 9, 2007
    Date of Patent: January 10, 2012
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Rafal R. Sicinski, Lori A. Plum, Margaret Clagett-Dame
  • Patent number: 8058265
    Abstract: Disclosed are 1?-hydroxy-2-(3?-hydroxypropylidene)-19-nor-vitamin D compounds, pharmaceutical compositions, and methods of making and treatment thereof. The compounds are generally directed to biologically active 2-alkylidene-19-nor-vitamin D compounds and analogs thereof characterized by the presence of a 3?-hydroxypropylidene moiety at C-2 and the presence of an abbreviated alkyl side-chain free of any hydroxyl moiety.
    Type: Grant
    Filed: April 5, 2007
    Date of Patent: November 15, 2011
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. Deluca, Rafal R. Sicinski, Lori A. Plum, Margaret Clagett-Dame, Agnieszka Glebocka
  • Patent number: 7943601
    Abstract: This invention discloses 2-methylene-20-methyl-19,24,25,26,27-pentanor-vitamin D analogs, and specifically 2-methylene-20-methyl-1?-hydroxy-19,24,25,26,27-pentanor-vitamin D3, and pharmaceutical uses therefore. This compound exhibits activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also has little, if any, calcemic activity and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.
    Type: Grant
    Filed: December 24, 2008
    Date of Patent: May 17, 2011
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Margaret Clagett-Dame, Lori A. Plum, Agnieszka Glebocka, Rafal R. Sicinski
  • Publication number: 20110082122
    Abstract: 19-nor-vitamin D analogs having an additional cyclopentene ring connecting carbon 1 and carbon 2, or connecting carbon 3 and carbon-2 of the A-ring of the analog, and pharmaceutical uses therefore, are described. These compounds exhibit selective in vitro activities, making them therapeutic agents for the treatment or prophylaxis of some types of cancers, particularly leukemia, colon cancer, breast cancer, skin cancer or prostate cancer.
    Type: Application
    Filed: September 30, 2010
    Publication date: April 7, 2011
    Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATION
    Inventors: Hector F. DeLuca, Agnieszka Glebocka, Lori A. Plum, Margaret Clagett-Dame, Rafal R. Sicinski