Patents by Inventor Hector F. DeLuca

Hector F. DeLuca 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: 9212137
    Abstract: Disclosed are methods of purifying the compound (20R,22R)-2-methylene-19-nor-22-methyl-1?,25-dihydroxyvitamin D3 to obtain the compound in crystalline form. The methods typically include the steps of dissolving a product containing the compound in a solvent comprising hexane and 2-propanol, cooling the solvent and dissolved product below ambient temperature for a sufficient amount of time to form a precipitate of crystals, and recovering the crystals. Certain diol precursors formed during the synthesis of the compound and its diasteromers also may be obtained in crystalline form using ethyl acetate as a solvent.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: December 15, 2015
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Pawel Grzywacz, Lori A. Plum, Agnieszka Flores, James B. Thoden, Hazel M. Holden
  • Patent number: 9205096
    Abstract: Disclosed are methods of administering 2-methylene-19-nor-(20S)-1?,25-dihydroxyvitamin D3 to treat and/or prevent secondary hyperparathyroidism and/or its accompanying symptoms in a subject having or at risk for developing secondary hyperparathyroidism.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: December 8, 2015
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Lori A. Plum, Julia B. Zella, Margaret Clagett-Dame
  • Patent number: 9040728
    Abstract: Disclosed are methods of purifying the compound (20R)-19-nor-24-difluoro-1?,25-dihydroxyvitamin D3 to obtain the compound in crystalline form. The methods typically include the steps of dissolving a product containing the compound in a solvent comprising hexane and 2-propanol, cooling the solvent and dissolved product below ambient temperature for a sufficient amount of time to form a precipitate of crystals, and recovering the crystals.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: May 26, 2015
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Agnieszka Flores, James B. Thoden, Hazel M. Holden
  • Patent number: 9034853
    Abstract: Disclosed are methods of administering 2-methylene-19-nor-(20S)-1?,25-dihydroxyvitamin D3 to treat and/or prevent secondary hyperparathyroidism and/or its accompanying symptoms in a subject having or at risk for developing secondary hyperparathyroidism.
    Type: Grant
    Filed: March 7, 2014
    Date of Patent: May 19, 2015
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Julia B. Zella, Lori A. Plum, Margaret Clagett-Dame
  • 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: 8987235
    Abstract: This invention discloses N-cyclopropyl-(20R)-2-methylene-19,26,27-trinor-25-aza-vitamin D analogs, and specifically N-cyclopropyl-(20R)-2-methylene-19,26,27-trinor-25-aza-1?-hydroxyvitamin 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: May 16, 2012
    Date of Patent: March 24, 2015
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Margaret Clagett-Dame, Lori A. Plum, Grazia Chiellini
  • Patent number: 8940916
    Abstract: Disclosed are methods of purifying the compound (20R)-2-methylene-19-nor-24-difluoro-1?,25-dihydroxyvitamin D3 to obtain the compound in crystalline form. The methods typically include the steps of dissolving a product containing the compound in a solvent comprising hexane and 2-propanol, cooling the solvent and dissolved product below ambient temperature for a sufficient amount of time to form a precipitate of crystals, and recovering the crystals.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: January 27, 2015
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Agnieszka Flores, James B. Thoden, Hazel M. Holden
  • Patent number: 8884039
    Abstract: Disclosed are methods of purifying (20R) and (20S) analogs of 2-methylene-19-nor-22-dimethyl-1?,25-dihydroxyvitamin D3 to obtain the (20R) and (20S) analogs in crystalline form. The method includes the steps of preparing a solvent of either diethyl ether or a mixture of 2-propanol and hexane, dissolving a product containing the (20R) and (20S) analog to be purified in the solvent, cooling the solvent and dissolved product below ambient temperature for a sufficient amount of time to form a precipitate of crystals, and recovering the crystals.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: November 11, 2014
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Agnieszka Flores, James B. Thoden, Hazel M. Holden
  • Publication number: 20140206655
    Abstract: Disclosed are (22E)-2-methylene-22-dehydro-1,24,25-trihydroxy-19-nor-vitamin D3 compounds, their biological activities, and various pharmaceutical uses for these compounds. Particularly disclosed are (22E)-(24R)-2-methylene-22-dehydro-1?,24,25-trihydroxy-19-nor-vitamin D3 and (22E)-(24S)-2-methylene-22-dehydro-1?,24,25-trihydroxy-19-nor-vitamin D3, their biological activities, and various pharmaceutical uses for these compounds.
    Type: Application
    Filed: November 19, 2013
    Publication date: July 24, 2014
    Applicant: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Lori A. Plum, Rafal Barycki, Margaret Clagett-Dame
  • Patent number: 8785422
    Abstract: Disclosed are 19-nor-vitamin D compounds, and specifically seco-A-2,19-dinor-1,25-dihydroxyvitamin D3 as well as pharmaceutical uses therefor. These compounds exhibit relatively high activity in vivo, specifically in intestinal tissues, but relatively low VDR binding activity, cell differentiation activity and gene transcription activity. There is thus potential for these compounds to have strong cell selectivity for use as therapeutic agents against some cancers, such as colon cancer or polyps, as well as hyperplastic intestinal disorders, such as Crohn's disease, ulcerative colitis and celiac disease. These compounds also have relatively high intestinal calcium transport activity evidencing potential in the treatment of bone diseases.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: July 22, 2014
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Margaret Clagett-Dame, Lori A. Plum, Agnieszka Glebocka
  • Publication number: 20140187522
    Abstract: Disclosed are methods of administering 2-methylene-19-nor-(20S)-1?,25-dihydroxyvitamin D3 to treat and/or prevent secondary hyperparathyroidism and/or its accompanying symptoms in a subject having or at risk for developing secondary hyperparathyroidism.
    Type: Application
    Filed: March 7, 2014
    Publication date: July 3, 2014
    Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATION
    Inventors: Hector F. DeLuca, Julia B. Zella, Lori A. Plum, Margaret Clagett-Dame, Wendy Bedale
  • Patent number: 8759328
    Abstract: An oral dosage form comprising a single dose of 25-hydroxy-vitamin D3 sufficient to elevate the serum level in a human to a concentration in the range of 30 ng/ml to 200 ng/ml for at least 7 days and a pharmaceutically suitable oral carrier system, wherein subsequent single doses at least every 7 days are sufficient to sustain the serum level in a human to a concentration in the range of 30 ng/ml to 200 ng/ml at steady-state pharmacokinetics is disclosed.
    Type: Grant
    Filed: July 24, 2009
    Date of Patent: June 24, 2014
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. Deluca, Lori A. Plum, Margaret Clagett-Dame
  • Patent number: 8754067
    Abstract: This invention discloses 22-haloacetoxy-homopregnacalciferol analogs and specifically 22-bromoacetoxy-homopregnacalciferol and pharmaceutical uses therefor. This compound exhibits relatively little calcemic activity and does not promote cellular differentiation off HL-60 leukemia cells, but rather kills the cells. This cell death activity is found in small cell lung carcinoma also, but not in prostate cancer cells. This compound thus causes specific cell death in the absence of changes in calcium levels and without general toxicity in an animal. Therefore it might serve as a useful therapy for treatment of some forms of cancer, such as leukemia and lung cancer.
    Type: Grant
    Filed: November 11, 2011
    Date of Patent: June 17, 2014
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Rafal Barycki, Lori A. Plum
  • Publication number: 20140155360
    Abstract: A calcium formate composition for oral administration to an individual for the purpose of supplementary dietary calcium is disclosed.
    Type: Application
    Filed: February 4, 2014
    Publication date: June 5, 2014
    Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATION
    Inventor: Hector F. DeLuca
  • 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
  • Publication number: 20140100203
    Abstract: An oral dosage form comprising a single dose of 25-hydroxy-vitamin D3 sufficient to elevate the serum level in a human to a concentration in the range of 30 ng/ml to 200 ng/ml for at least 7 days and a pharmaceutically suitable oral carrier system, wherein subsequent single doses at least every 7 days are sufficient to sustain the serum level in a human to a concentration in the range of 30 ng/ml to 200 ng/ml at steady-state pharmacokinetics is disclosed.
    Type: Application
    Filed: March 11, 2013
    Publication date: April 10, 2014
    Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATION
    Inventors: Hector F. DeLuca, Lori A. Plum, Margaret Clagett-Dame
  • Patent number: 8664206
    Abstract: Compounds of formula I are provided where X1, X2, and X3 are independently selected from H or hydroxy protecting groups. Such compounds may be used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.
    Type: Grant
    Filed: January 6, 2012
    Date of Patent: March 4, 2014
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Agnieszka Flores, Pawel Grzywacz, Lori A. Plum, Margaret Clagett-Dame, James B. Thoden, Hazel M. Holden
  • 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
  • Publication number: 20140018332
    Abstract: Oral and topical pharmaceutical compositions, kits and methods of treatment thereof for treating various skin disorder including acne, psoriasis, ichthyosis, photoaging, photodamaged skin, and, skin cancer.
    Type: Application
    Filed: September 23, 2013
    Publication date: January 16, 2014
    Applicant: Wisconsin Alumni Research Foundation
    Inventors: Margaret Clagett-Dame, Hector F. DeLuca, Nircaq J. Nieves, Lori A. Plum, Mary E. Kaiser
  • Publication number: 20140011778
    Abstract: Compounds of Formula I are provided where R1 and R2 are independently selected from H or hydroxy protecting groups. Such compounds may be used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.
    Type: Application
    Filed: September 12, 2013
    Publication date: January 9, 2014
    Applicant: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLUCA, Margaret Clagett-Dame, Lori A. Plum, Agnieszka Glebocka, Rafal Sicinski