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: 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: 8404666
    Abstract: Compounds of formula I, II or III are provided where X1, X2 and X3 are independently selected from H and hydroxy protecting groups and R1 and R2 are independently selected from H or straight or branched chain alkyl groups having from 1 to 8 carbon atoms, straight or branched chain alkenyl groups having from 2 to 8 carbon atoms, straight or branched chain hydroxy-substituted alkyl groups having from 1 to 8 carbon atoms, or straight and branched chain hydroxy-substituted alkenyl groups having from 2 to 8 carbon atoms; and R3 is independently selected from straight or branched chain alkyl groups having from 1 to 8 carbon atoms, straight or branched chain alkenyl groups having from 2 to 8 carbon atoms, straight or branched chain hydroxy-substituted alkyl groups having from 1 to 8 carbon atoms, or straight and branched chain hydroxy-substituted alkenyl groups having from 2 to 8 carbon atoms.
    Type: Grant
    Filed: April 6, 2007
    Date of Patent: March 26, 2013
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Lori A. Plum, Margaret Clagett-Dame, Pawel Grzywacz
  • Patent number: 8404874
    Abstract: A method of purifying (20R,25S)-2-methylene-19,26-dinor-1?,25-dihydroxyvitamin D3 to obtain (20R,25S)-2-methylene-19,26-dinor-1?,25-dihydroxyvitamin D3 in crystalline form. The method includes the steps of preparing a solvent of methanol and water, dissolving a product containing (20R,25S)-2-methylene-19,26-dinor-1?,25-dihydroxyvitamin 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 (20R,25S)-2-methylene-19,26-dinor-1?,25-dihydroxyvitamin D3 crystals, and recovering the (20R,25S)-2-methylene-19,26-dinor-1?,25-dihydroxyvitamin D3 crystals.
    Type: Grant
    Filed: September 28, 2011
    Date of Patent: March 26, 2013
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Pawel Grzywacz, James B. Thoden, Hazel Holden
  • Patent number: 8404667
    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: Grant
    Filed: December 28, 2007
    Date of Patent: March 26, 2013
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Margaret Clagett-Dame, Hector F. DeLuca, Nirca J. Nieves, Lori A. Plum, Mary E. Kaiser
  • Publication number: 20130073009
    Abstract: A method and computer program product for suppressing the symptoms of multiple sclerosis (MS) by irradiating a subject exhibiting the symptoms with a predetermined 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 3, 2011
    Publication date: March 21, 2013
    Inventors: Hector F. Deluca, Bryan R. Becklund
  • 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
  • Patent number: 8399439
    Abstract: This invention discloses 2-methylene-19,26-dinor-(20S,22E,25R)-vitamin D analogs, and specifically 2-methylene-19,26-dinor-(20S,22E,25R)-1?,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits 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 no activity in vivo on bone calcium mobilization and relatively low intestinal calcium transport activity 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 renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.
    Type: Grant
    Filed: July 10, 2008
    Date of Patent: March 19, 2013
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Grazia Chiellini, Pawel Grzywacz, Lori A. Plum, Margaret Clagett-Dame
  • Publication number: 20130053587
    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: Application
    Filed: August 17, 2012
    Publication date: February 28, 2013
    Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATION
    Inventors: Hector F. DeLuca, Agnieszka Glebocka, James B. Thoden, Hazel M. Holden
  • Publication number: 20130053356
    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: August 23, 2012
    Publication date: February 28, 2013
    Inventors: Hector F. DELUCA, Margaret Clagett-Dame, Lori A. Plum, Agnieszka Glebocka, Rafal Sicinski
  • Patent number: 8349818
    Abstract: The invention relates to novel methods of using 2?-methyl-19-nor-20(S)-1?,25-dihydroxyvitamin D3 or 2-methylene-19-nor-20(S)-1,25-dihydroxyvitamin D3 to prevent Type 1 diabetes in a subject at risk of developing Type 1 diabetes without causing hypercalcemia in the subject.
    Type: Grant
    Filed: October 21, 2010
    Date of Patent: January 8, 2013
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Jamie Nehring, Ehren N. Rudolph, Lori Plum
  • Publication number: 20130005686
    Abstract: This invention discloses 2-methylene-(22E)-25-hexanoyl-24-oxo-26,27-cyclo-22-dehydro-19-nor-vitamin D analogs, and specifically 2-methylene-(22E)-25-hexanoyl-24-oxo-26,27-cyclo-22-dehydro-19-nor-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 low activity in vivo on bone calcium mobilization, 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: June 26, 2012
    Publication date: January 3, 2013
    Applicant: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Margaret Clagett-Dame, Lori A. Plum, Rafal Barycki
  • 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
  • Publication number: 20120283228
    Abstract: This invention discloses 2?-methyl and 2?-methyl analogs of 19,26-dinor-1?,25-dihydroxyvitamin D3 and pharmaceutical uses therefor. These compounds exhibit in vitro biological activities 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 have little, if any, in vivo calcemic activity and therefore may be used to treat autoimmune disorders in humans as well as secondary hyperparathyroidism and renal osteodystrophy.
    Type: Application
    Filed: May 3, 2012
    Publication date: November 8, 2012
    Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATION
    Inventors: Hector F. DeLuca, Margaret Clagett-Dame, Pawel Grzywacz, Grazia Chiellini, Lori A. Plum
  • Publication number: 20120283227
    Abstract: This invention discloses (20S)-24(p-toluenesulfonyloxy)-25,26,27-trinorvitamin D3 analogs, and especially (20S)-25,26,27-trinor-24-(p-methylphenylsulfonate)-vitamin D3, its biological activities, and pharmaceutical uses therefor. This compound exhibits relatively little calcemic activity and does not promote cellular differentiation of 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, bone or ovarian 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: Application
    Filed: April 19, 2012
    Publication date: November 8, 2012
    Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATION
    Inventors: Hector F. DeLuca, Margaret Clagett-Dame, Lori A. Plum, Rafal Barycki
  • Patent number: 8232263
    Abstract: This invention discloses 17,20(Z)-dehydro vitamin D analogs, and specifically 17(Z)-1?,25-dihydroxy-17(20)-dehydro-2-methylene-19-nor-vitamin 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 may be used to treat autoimmune disorders and inflammatory diseases in humans as well as renal osteodystrophy and obesity. This compound also has significant calcemic activity making it a therapeutic agent for the treatment or prophylaxis of osteoporosis, osteomalacia, renal osteodystrophy and hypoparathyroidism.
    Type: Grant
    Filed: July 9, 2007
    Date of Patent: July 31, 2012
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Bulli Padmaja Tadi, Lori A. Plum, Margaret Clagett-Dame
  • Patent number: 8222236
    Abstract: This invention discloses 2-methylene-(20E)-20(22)-dehydro-19-nor-vitamin D analogs, and specifically 2-methylene-(20E)-20(22)-dehydro-19-nor-1?,25-dihydroxyvitamin D3, and pharmaceutical uses therefore. 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 similar in vivo intestinal calcium transport activity 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 renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.
    Type: Grant
    Filed: July 10, 2008
    Date of Patent: July 17, 2012
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Bulli Padmaja Tadi, Lori A. Plum, Margaret Clagett-Dame
  • Patent number: 8222235
    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: July 17, 2012
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Lori A. Plum, 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: 20120165300
    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: Application
    Filed: January 6, 2012
    Publication date: June 28, 2012
    Inventors: Hector F. DeLUCA, Agnieszka FLORES, Pawel GRZYWACZ, Lori A. PLUM, Margaret CLAGETT-DAME, James B. THODEN, Hazel M. HOLDEN
  • 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