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).

  • Publication number: 20140005152
    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 14, 2013
    Publication date: January 2, 2014
    Applicant: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Lori A. Plum, Julia B. Zella, Wendy Bedale, Margaret Clagett-Dame
  • Patent number: 8614202
    Abstract: This invention discloses 2?-methyl and 2?-methyl analogs of 19,26,27-trinor-(20S)-1?-hydroxyvitamin D3 and pharmaceutical uses therefor. These compounds exhibit 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. These compounds also have little, if any, calcemic activity and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. These compounds may also be used for the treatment or prevention of obesity.
    Type: Grant
    Filed: September 18, 2012
    Date of Patent: December 24, 2013
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Lori A. Plum, Pawel K. Grzywacz, Margaret Clagett-Dame
  • Patent number: 8609643
    Abstract: This invention discloses 2-methylene-(20S,25R)-19,26-dinor-vitamin D analogs, and specifically 2-methylene-(20S,25R)-19,26-dinor-1?,25-dihydroxyvitamin D3, 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: December 24, 2008
    Date of Patent: December 17, 2013
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Margaret Clagett-Dame, Lori A. Plum, Grazia Chiellini, Pawel Grzywacz
  • Publication number: 20130331459
    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: Application
    Filed: March 14, 2013
    Publication date: December 12, 2013
    Applicant: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Margaret Clagett-Dame, Lori A. Plum, Agnieszka Glebocka
  • Patent number: 8604009
    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: March 22, 2011
    Date of Patent: December 10, 2013
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Agnieszka Flores, Pawel Grzywacz, Lori A. Plum, Margaret Clagett-Dame
  • Patent number: 8604008
    Abstract: Compounds of formula I are provided where X1 and X2 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: November 18, 2005
    Date of Patent: December 10, 2013
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Lori A. Plum, Margaret Clagett-Dame
  • Publication number: 20130324751
    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: Application
    Filed: March 14, 2013
    Publication date: December 5, 2013
    Applicant: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Agnieszka Flores, James B. Thoden, Hazel M. Holden
  • Publication number: 20130324750
    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: Application
    Filed: March 14, 2013
    Publication date: December 5, 2013
    Applicant: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Agnieszka Flores, James B. Thoden, Hazel M. Holden
  • Publication number: 20130324752
    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: Application
    Filed: March 14, 2013
    Publication date: December 5, 2013
    Inventors: Hector F. DeLuca, Pawel Grzywacz, Lori A. Plum, Agnieszka Flores, James B. Thoden, Hazel M. Holden
  • Publication number: 20130324749
    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: Application
    Filed: March 14, 2013
    Publication date: December 5, 2013
    Applicant: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Agnieszka Flores, James B. Thoden, Hazel M. Holden
  • Publication number: 20130295083
    Abstract: A method of treating islet cell transplant patients is described herein. The method comprises the steps of a) identifying an islet cell transplant patient, b) treating the patient with 2AMD or 2AMD analog and c) observing a prolonged period of normal glycemia is disclosed. A composition for treatment of islet cell transplant patient is disclosed as well, wherein the composition comprises 50-400 ng/day of 2AMD or 2AMD analog.
    Type: Application
    Filed: February 20, 2013
    Publication date: November 7, 2013
    Applicant: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Carol M. Kiekhaefer
  • Patent number: 8575136
    Abstract: Compounds of formula I are provided where X1 and X2 are independently selected from H or hydroxy protecting groups. Such compounds are used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.
    Type: Grant
    Filed: April 6, 2007
    Date of Patent: November 5, 2013
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Lori A. Plum, Margaret Clagett-Dame, Rafal Barycki
  • Publication number: 20130253621
    Abstract: Methods and devices for suppressing clinical symptoms of multiple sclerosis (MS) by irradiating a subject exhibiting the symptoms with an effective dose of UV-containing light from a light source and detecting a suppression of the clinical symptoms of MS. In particular, the detected suppression of the clinical symptoms is disassociated from the vitamin D production within the subject.
    Type: Application
    Filed: February 21, 2013
    Publication date: September 26, 2013
    Inventors: Hector F. DeLuca, Yanping Wang, Steven Marling
  • 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
  • Patent number: 8519169
    Abstract: A method of purifying 1?-hydroxy-20-methyl-2-methylene-19,24,25,26,27-pentanorvitamin D3 to obtain 1?-hydroxy-20-methyl-2-methylene-19,24,25,26,27-pentanorvitamin D3 in crystalline form. The method includes the steps of preparing a solvent of either ethyl formate or a mixture of ethyl formate and hexane, dissolving a product containing 1?-hydroxy-20-methyl-2-methylene-19,24,25,26,27-pentanorvitamin D3 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 1?-hydroxy-20-methyl-2-methylene-19,24,25,26,27-pentanorvitamin D3 crystals, and recovering the 1?-hydroxy-20-methyl-2-methylene-19,24,25,26,27-pentanorvitamin D3 crystals.
    Type: Grant
    Filed: August 17, 2012
    Date of Patent: August 27, 2013
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Agnieszka Glebocka, James B. Thoden, Hazel M. Holden
  • 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: 8455467
    Abstract: This invention discloses 2-methylene-vitamin D analogs, and specifically (20S)-25-hydroxy-2-methylene-vitamin D3 and (20R)-25-hydroxy-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 9, 2012
    Date of Patent: June 4, 2013
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Lori A. Plum, Rafal Sicinski, Izabela Sibilska
  • Patent number: 8445468
    Abstract: This invention discloses (20S,22E)-2-methylene-19-nor-22-ene-1?,25-dihydroxyvitamin D3 analogs, and specifically(20S,22E)-2-methylene-19-nor-22-ene-1?,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits significant vitamin D receptor binding activity and 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, 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: May 21, 2013
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Pawel Grzywacz, Lori A. Plum, Margaret Clagett-Dame
  • Patent number: 8440647
    Abstract: This invention discloses 2?-methyl and 2?-methyl analogs of 19,26,27-trinor-(20S)-1?-hydroxyvitamin D3 and pharmaceutical uses therefor. These compounds exhibit 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. These compounds also have little, if any, calcemic activity and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. These compounds may also be used for the treatment or prevention of obesity.
    Type: Grant
    Filed: July 9, 2007
    Date of Patent: May 14, 2013
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Lori A. Plum, Pawel K. Grzywacz, Margaret Clagett-Dame
  • Patent number: 8420839
    Abstract: A method of purifying 1?-hydroxy-2-methylene-18,19-dinor-homopregnacalciferol to obtain 1?-hydroxy-2-methylene-18,19-dinor-homopregnacalciferol in crystalline form using precipitation with hexane from ethyl acetate. A method of preparing 1?-hydroxy-2-methylene-18,19-dinor-homopregnacalciferol crystals acceptable for X-ray experiment using precipitation with hexane from benzene by diffusive exchange of the solvents is also described.
    Type: Grant
    Filed: October 1, 2012
    Date of Patent: April 16, 2013
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Rafal Barycki, James B. Thoden, Hazel M. Holden