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).
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Publication number: 20170253546Abstract: 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: ApplicationFiled: May 18, 2017Publication date: September 7, 2017Applicant: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Izabela K. Sibilska, Rafal R. Sicinski, Lori A. Plum
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Patent number: 9688596Abstract: 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: GrantFiled: July 26, 2016Date of Patent: June 27, 2017Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Izabela K. Sibilska, Rafal R. Sicinski, Lori A. Plum
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Publication number: 20170036977Abstract: 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: ApplicationFiled: July 26, 2016Publication date: February 9, 2017Applicant: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Izabela K. Sibilska, Rafal R. Sicinski, Lori A. Plum
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Patent number: 8993547Abstract: 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: GrantFiled: June 13, 2012Date of Patent: March 31, 2015Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Lori A. Plum, Rafal R. Sicinski, Izabela Sibilska, Margaret Clagett-Dame
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Patent number: 8729054Abstract: 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: GrantFiled: October 3, 2012Date of Patent: May 20, 2014Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Lori A. Plum, Rafal R. Sicinski, Izabela Sibilska
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Patent number: 8642579Abstract: 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: GrantFiled: September 30, 2010Date of Patent: February 4, 2014Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Katarzyna M. Barycka, Izabela Sibilska, Lori A. Plum, Margaret Clagett-Dame, Rafal Barycki, Rafal R. Sicinski, Katarzyna Plonska-Ocypa
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Patent number: 8518917Abstract: 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: GrantFiled: October 21, 2011Date of Patent: August 27, 2013Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Izabela Sibliska, Lori A. Plum, Margaret Clagett-Dame, Rafal R. Sicinski, Katarzyna M. Barycka, Katarzyna Plonska-Ocypa, Rafal Barycki
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Publication number: 20130178449Abstract: 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: ApplicationFiled: July 12, 2012Publication date: July 11, 2013Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATIONInventors: Hector F. DeLuca, Margaret Clagett-Dame, Lori A. Plum, Agnieska Glebocka, Rafal R. Sicinski
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Patent number: 8410080Abstract: 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: GrantFiled: October 11, 2012Date of Patent: April 2, 2013Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Lori A. Plum, Rafal R. Sicinski, Izabela Sibilska
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Patent number: 8399438Abstract: 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: GrantFiled: November 18, 2005Date of Patent: March 19, 2013Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Rafal R. Sicinski, Lori A. Plum, Margaret Clagett-Dame, Sumithra Gowlugari
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Publication number: 20120322775Abstract: 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: ApplicationFiled: June 13, 2012Publication date: December 20, 2012Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATIONInventors: Hector F. DeLuca, Lori A. Plum, Rafal R. Sicinski, Izabela Sibilska, Margaret Clagett-Dame
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Patent number: 8217023Abstract: 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: GrantFiled: September 30, 2010Date of Patent: July 10, 2012Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Agnieszka Glebocka, Lori A. Plum, Margaret Clagett-Dame, Rafal R. Sicinski
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Publication number: 20120157418Abstract: 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: ApplicationFiled: October 21, 2011Publication date: June 21, 2012Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATIONInventors: Hector F. DeLuca, Izabela Sibilska, Lori A. Plum, Margaret Clagett-Dame, Rafal R. Sicinski, Katarzyna M. Barycka, Katarzyna Plonska-Ocypa, Rafal Barycki
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Patent number: 8193171Abstract: 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: GrantFiled: January 22, 2009Date of Patent: June 5, 2012Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Margaret Clagett-Dame, Lori A. Plum, Rafal R. Sicinski, Katarzyna Plonska-Ocypa, Nirca J. Nieves, Pawel Grzywacz
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Patent number: 8178517Abstract: 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: GrantFiled: September 30, 2010Date of Patent: May 15, 2012Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Katarzyna Sokolowska, Lori A. Plum, Margaret Clagett-Dame, Rafal R. Sicinski, Antonio Mouriño
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Publication number: 20120071562Abstract: 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: ApplicationFiled: November 22, 2011Publication date: March 22, 2012Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATIONInventors: Hector F. DeLuca, Rafal R. Sicinski, Lori A. Plum, Margaret Clagett-Dame
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Patent number: 8093232Abstract: 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: GrantFiled: July 9, 2007Date of Patent: January 10, 2012Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Rafal R. Sicinski, Lori A. Plum, Margaret Clagett-Dame
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Patent number: 8058265Abstract: 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: GrantFiled: April 5, 2007Date of Patent: November 15, 2011Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. Deluca, Rafal R. Sicinski, Lori A. Plum, Margaret Clagett-Dame, Agnieszka Glebocka
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Patent number: 7943601Abstract: 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: GrantFiled: December 24, 2008Date of Patent: May 17, 2011Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Margaret Clagett-Dame, Lori A. Plum, Agnieszka Glebocka, Rafal R. Sicinski
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Publication number: 20110082123Abstract: 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: ApplicationFiled: September 30, 2010Publication date: April 7, 2011Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATIONInventors: Hector F. DeLuca, Katarzyna Sokolowska, Lori A. Plum, Margaret Clagett-Dame, Rafal R. Sicinski, Antonio Mouriño