Patents by Inventor Hector Deluca

Hector 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: 20060135493
    Abstract: This invention provides pharmaceutical uses for 2-methylene-19-nor-20(S)-1?,25-dihydroxyvitamin D3. This compound is characterized by high bone calcium mobilization activity demonstrating preferential activity on bone. This results in a novel therapeutic agent for the treatment of diseases where bone formation is desired, particularly osteoporosis. This compound also 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. This compound also increases both breaking strength and crushing strength of bones evidencing use in conjunction with bone replacement surgery such as hip and knee replacements.
    Type: Application
    Filed: February 9, 2006
    Publication date: June 22, 2006
    Applicant: Wisconsin Alumni Research Foundation
    Inventors: Hector DeLuca, Connie Smith
  • Publication number: 20060135799
    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: Application
    Filed: November 18, 2005
    Publication date: June 22, 2006
    Inventors: Hector DeLuca, Lori Plum, Margaret Clagett-Dame
  • Publication number: 20060122157
    Abstract: This invention discloses 2-methylene-18,19-dinor-vitamin D analogs, and specifically 2-methylene-18,19-dinor-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: Application
    Filed: November 18, 2005
    Publication date: June 8, 2006
    Inventors: Hector DeLuca, Rafal Barycki, Lori Plum, Margaret Clagett-Dame
  • Publication number: 20060116351
    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: Application
    Filed: November 18, 2005
    Publication date: June 1, 2006
    Inventors: Hector DeLuca, Bulli Tadi, Lori Plum, Margaret Clagett-Dame
  • Publication number: 20060116352
    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: Application
    Filed: November 18, 2005
    Publication date: June 1, 2006
    Inventors: Hector DeLuca, Lori Plum, Pawel Grzywacz, Margaret Clagett-Dame
  • Publication number: 20060111321
    Abstract: This invention discloses 2-methylene-19-nor-17-ene vitamin D analogs, and specifically 2-methylene-19-nor-?-hydroxy-17-ene-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 and 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 18, 2005
    Publication date: May 25, 2006
    Inventors: Hector DeLuca, Bulli Tadi, Lori Plum, Margaret Clagett-Dame
  • Publication number: 20060111330
    Abstract: This invention discloses 17,20(E)-dehydro vitamin D analogs, and specifically 17(E)-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 has little, if any, calcemic activity and therefore may be used to treat autoimmune disorders and inflammatory diseases in humans as well as renal osteodystrophy and obesity.
    Type: Application
    Filed: November 18, 2005
    Publication date: May 25, 2006
    Inventors: Hector DeLuca, Bulli Tadi, Lori Plum, Margaret Clagett-Dame
  • Publication number: 20060079692
    Abstract: A method of synthesizing aromatic ketone compositions of formula I comprising the step of introducing a double bond into the 5 membered ring of the 4,5-dihydro-1,3-azoles moiety of formula II is disclosed. A method of synthesizing aromatic ketone compositions of formula I comprising the step of ring synthesis of the tetrahydro-1,3-azoles of formula XI is also disclosed.
    Type: Application
    Filed: November 23, 2005
    Publication date: April 13, 2006
    Inventors: Hector DeLuca, Pawel Grzywacz, Rafal Sicinski
  • Publication number: 20060079490
    Abstract: A method of delaying the onset or reducing the severity of diabetes in a human patient is disclosed. In one embodiment, the invention comprises the step of orally administering to the human patient an effective amount of a vitamin D compound such as the onset of diabetes or diabetes symptoms is slowed.
    Type: Application
    Filed: September 20, 2005
    Publication date: April 13, 2006
    Inventors: Hector DeLuca, Ehren Rudolph, Laura Bloss, Julia Zella
  • Publication number: 20060003973
    Abstract: This invention provides pharmaceutical uses for 2?-methyl-19-nor-20(S)-1?,25-dihydroxyvitamin D3. This compound is characterized by high bone calcium mobilization activity demonstrating preferential activity on bone. This results in a novel therapeutic agent for the treatment of diseases where bone formation is desired, particularly osteoporosis. This compound also 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. This compound also increases both breaking strength and crushing strength of bones evidencing use in conjunction with bone replacement surgery such as hip and knee replacements.
    Type: Application
    Filed: August 31, 2005
    Publication date: January 5, 2006
    Inventors: Hector DeLuca, Connie Smith
  • Publication number: 20050282789
    Abstract: Biologically active 19-nor vitamin D analogs substituted at C-2 in the A-ring with an ethylidene or an ethyl group. These compounds have preferential activity on mobilizing calcium from bone and either high or normal intestinal calcium transport activity which allows their in vivo administration for the treatment of metabolic bone diseases where bone loss is a major concern. These compounds are also characterized by high cell differentiation activity.
    Type: Application
    Filed: July 28, 2005
    Publication date: December 22, 2005
    Applicant: Wisconsin Alumni Research Foundation
    Inventors: Hector DeLuca, Rafal Sicinski
  • Publication number: 20050227950
    Abstract: 2-alkylidene-18,19-dinor-vitamin D compounds are disclosed as well as pharmaceutical uses for these compounds and methods of synthesizing these compounds. These compounds are characterized by low bone calcium mobilization activity and high intestinal calcium transport activity. This results in novel therapeutic agents for the treatment and prophylaxis of diseases where bone formation is desired, particularly osteoporosis, as well as autoimmune diseases such as multiple sclerosis, diabetes mellitus and lupus. These compounds also 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. These compounds also increase both breaking strength and crushing strength of bones evidencing use in conjunction with bone replacement surgery such as hip and knee replacements.
    Type: Application
    Filed: April 9, 2004
    Publication date: October 13, 2005
    Inventors: Hector DeLuca, Rafal Barycki, Pawel Grzywacz, Lori Plum, Rafal Sicinski
  • Publication number: 20050203071
    Abstract: It has been discovered that the 2-carbon-modified derivatives of 1?,25-dihydroxyvitamin D3 specifically stimulate osteoblasts to form new bone. The ability of the 2-carbon-modified vitamin D analogs to stimulate new bone formation suggest that these compounds can be used where synthesis of new bone is required. Thus, these compounds can be used either systemically or locally to stimulate the growth of bone transplants, to increase the rate of fracture healing and thereby reduce the time required for the healing of fractures, the stimulation of bone growth when required for replacement surgery, and also for the growth of bone to implants or other devices required to maintain the skeleton or teeth in the proper positions.
    Type: Application
    Filed: March 12, 2003
    Publication date: September 15, 2005
    Inventors: Hector Deluca, J. Pike, Nirupama Shevde
  • Publication number: 20050187201
    Abstract: This invention provides pharmaceutical uses for 2-methylene-19-nor-20(S)-1?,25-dihydroxyvitamin D3. This compound is characterized by high bone calcium mobilization activity demonstrating preferential activity on bone. This results in a novel therapeutic agent for the treatment and prophylaxis of diseases where bone formation is desired, particularly osteoporosis. This compound also increases both breaking strength and crushing strength of bones evidencing use in conjunction with bone replacement surgery such as hip and knee replacements, as well as use by normal subjects when high bone mass is desired.
    Type: Application
    Filed: February 19, 2004
    Publication date: August 25, 2005
    Inventors: Hector DeLuca, Lori Plum, Margaret Clagette-Dame
  • Publication number: 20050182033
    Abstract: Various compounds such as those having the formula I and XIV where the variables have the values described herein antagonize the vitamin D receptor and are useful in treating conditions such as asthma and in preparing medicaments for use in antagonizing the vitamin D receptor or treating conditions such as asthma
    Type: Application
    Filed: February 16, 2005
    Publication date: August 18, 2005
    Inventors: Hector DeLuca, Rafal Barycki, Moises Rivera-Bermudez, Lori Plum, Margaret Clagett-Dame
  • Publication number: 20050182034
    Abstract: A method of modifying or altering the structure of a 1?-hydroxylated vitamin D compound to increase its biological activity by altering the conformational equilibrium of the A-ring to favor a chair conformation that presents the 1?-hydroxyl in the axial orientation. This is accomplished by either locking the A-ring chair conformation in a geometry having an axially orientated 1?-hydroxyl, or by the addition of one or more substituents to the A-ring which interact with other substituents in the molecule or on the A-ring to provide a driving force to the A-ring to adopt a chair conformation which presents the 1?-hydroxyl in the axial orientation.
    Type: Application
    Filed: March 18, 2005
    Publication date: August 18, 2005
    Applicant: Wisconsin Alumni Research Foundation
    Inventors: Hector DeLuca, Rafal Sicinski
  • Publication number: 20050182035
    Abstract: A method of modifying or altering the structure of a 1?-hydroxylated vitamin D compound to increase its biological activity by altering the conformational equilibrium of the A-ring to favor a chair conformation that presents the 1?-hydroxyl in the axial orientation. This is accomplished by either locking the A-ring chair conformation in a geometry having an axially orientated 1?-hydroxyl, or by the addition of one or more substituents to the A-ring which interact with other substituents in the molecule or on the A-ring to provide a driving force to the A-ring to adopt a chair conformation which presents the 1?-hydroxyl in the axial orientation.
    Type: Application
    Filed: March 18, 2005
    Publication date: August 18, 2005
    Applicant: Wisconsin Alumni Research Foundation
    Inventors: Hector DeLuca, Rafal Sicinski
  • Publication number: 20050164995
    Abstract: A method of modifying or altering the structure of a 1?-hydroxylated vitamin D compound to increase its biological activity by altering the conformational equilibrium of the A-ring to favor a chair conformation that presents the 1?-hydroxyl in the axial orientation. This is accomplished by either locking the A-ring chair conformation in a geometry having an axially orientated 1?-hydroxyl, or by the addition of one or more substituents to the A-ring which interact with other substituents in the molecule or on the A-ring to provide a driving force to the A-ring to adopt a chair conformation which presents the 1?-hydroxyl in the axial orientation.
    Type: Application
    Filed: March 18, 2005
    Publication date: July 28, 2005
    Applicant: Wisconsin Alumni Research Foundation
    Inventors: Hector DeLuca, Rafal Sicinski
  • Publication number: 20050159397
    Abstract: This invention discloses (20S)-1?-hydroxy-2?-methyl-19-nor-vitamin D3 and (20S)-1?-hydroxy-2?-methyl-19-nor-vitamin 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 very significant calcemic activity and therefore may be used to treat immune disorders in humans as well as metabolic bone diseases such as osteoporosis.
    Type: Application
    Filed: January 18, 2005
    Publication date: July 21, 2005
    Inventors: Hector DeLuca, Rafal Sicinski, Pawel Grzywacz
  • Publication number: 20050143358
    Abstract: A treatment for obesity and overweight comprises administering a vitamin D analog. The analog effectively inhibits an increase in body fat to animals at risk and decreases the basal fat content of animals. The treatment has a positive effect on the lean body component such that while there is an overall decrease in body weight, there is also a decrease in percent body fat. This decrease can be proportionally greater than the overall decrease in body weight. In addition, the treatment has a positive effect on bone turnover and osteogenesis making the vitamin D analog a beneficial treatment for the symptoms of menopause. Various exemplary embodiments of the treatment use the 2-alkylidene derivatives of vitamin D3, such as the 2-alkylidene-19-nor derivatives in both the R and S configurations at carbon-20.
    Type: Application
    Filed: November 24, 2004
    Publication date: June 30, 2005
    Inventors: Hector DeLuca, Lori Plum, Hau Ke, Thomas Brown