9,10-seco- Cyclopentanohydrophenanthrene Ring System (e.g., Vitamin D, Etc.) Doai Patents (Class 514/167)
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Publication number: 20120277180Abstract: Provided herein are methods and systems for identifying one or more cofactors such as vitamins for individuals based on the genetic makeup of the individual by detecting the presence or absence of at least one genetic variant, determining a predisposition to cofactor remediable condition, generating a personalized nutritional advice plan based on the genetic variant. Also provided herein are formulations of cofactors determined by the genetic make-up of the individual and methods of determining and producing these formulations.Type: ApplicationFiled: September 30, 2010Publication date: November 1, 2012Applicants: VITAPATH GENETICS, INC, THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Nicholas Marini, Jasper Rine, Dennis Austin Gilbert, Bruce Cohen
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Publication number: 20120269868Abstract: Disclosed is a nutritional supplement composition including effective amounts of Coenzyme Q10, fish oil, vitamin D and a pharmaceutically acceptable excipient. Described is a method of promoting nutritional health comprising administering a nutritional supplement composition including Coenzyme Q10, fish oil, vitamin D and a pharmaceutically acceptable excipient to a subject. The nutritional supplement composition may further include flax seed oil, borage oil, evening primrose oil, vitamin E, resveratrol, vitamin B6, vitamin B12, folic acid, piperine and combinations. In some embodiments, administering Administering the nutritional supplement may ameliorate nutrient depletion, or promote cardiovascular health, liver health, or both. The nutritional supplement may be used to promote nutritional health taking a cholesterol lowering drug. The nutritional supplement may be used to ameliorate nutrient depletion taking a cholesterol lowering drug. The cholesterol lowering drug may be a statin.Type: ApplicationFiled: April 18, 2012Publication date: October 25, 2012Inventor: Paul Joseph FAERSTEIN
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Publication number: 20120270839Abstract: Bromoacetoxycalcidiol (B3CD), which is structurally related to calcidiol, exhibits cytotoxic and apoptotic activity toward cancer cells, including highly aggressive neuroblastoma cells. A series of small molecules designed around the structure of B3CD is expected to have growth inhibitory and apoptogenic activities toward a wide range of malignancies. B3CD shows no apparent toxicity in vivo, indicating potential value as a chemotherapeutic agent which will be particularly useful in treating highly aggressive tumors.Type: ApplicationFiled: February 22, 2012Publication date: October 25, 2012Applicant: WOMEN AND INFANTS HOSPITAL OF RIInventors: Narasimha Swamy, Hema Malini K. Sundaresha
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Publication number: 20120258938Abstract: Provided herein are steroidal compounds that are androsta-5,7-dienes or pregna-5,7-dienes and ultraviolet B (UVB) conversion products thereof and cholecalciferol derivatives hydroxylated at one or more of C1, C17, C20, C23, C24, C25, and C26 which includes pharmaceutical, cosmeceutical or nutraceutical compositions of the steroidal compounds as shown in Tables 1A, 2A and 3. Also provided is a method for producing hydroxylated metabolites of cholecalciferol via CYP11A1, CYP24, CYP27A1, or CYP27B1 enzyme systems where the hydroxylase has an activity to hydroxylate position C1 or C20 or other position of the sidechain of a secosteroid or its 5,7-dieneal precursor and the hydroxylated metabolites so produced.Type: ApplicationFiled: April 30, 2012Publication date: October 11, 2012Inventors: Andrej Slominski, Robert C. Tuckey, Edith Tang, Elaine Tieu, Minh Nguyen, Zorica Janjetovic, Jianjun Chen, Wei Li, Yan Lu, Duane D. Miller, Jordan K. Zjawiony, Arnold E. Postlethwaite
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Publication number: 20120244134Abstract: The present invention provides a process for preparing an aqueous dispersion containing a high concentration of nano/submicron, hydrophobic, functional compounds. The process is carried out by using a complex stabilizer having an HLB value of about 10 to about 17, comprising lecithin and at least one non-phospholipid selected from polysorbate, sucrose ester, and polyglycerol fatty acid ester; selecting a specific weight ratio of the hydrophobic functional compounds and the stabilizer; and using homogenization technique, media milling technique, and/or centrifugal technique. The aqueous dispersion containing a high concentration of nano/submicron, hydrophobic, functional compound produced by the process of the invention has stable dispersibility and improved bioavailability, and can be applied to the fields of foods and pharmaceuticals.Type: ApplicationFiled: July 19, 2011Publication date: September 27, 2012Inventors: Ru-Yin CHEN, Chung-Jen CHEN, Yi-Jie TSAI, Jia-Jiu WU, Chih-Ping HUANG, Chung-Liang CHU
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Patent number: 8273380Abstract: A beverage for minimizing or reducing jet lag symptoms preferably includes vitamin B3, vitamin B5, vitamin B6, vitamin B12, vitamin D, zinc, calcium, iodine, magnesium, manganese, ginseng, ginkgo biloba, grape seed extract, Echinacea extract and water. A method for minimizing or reducing jet lag symptoms including ingestion of the beverage by a traveler, one hour prior to a flight, and/or during the flight, and/or after a flight.Type: GrantFiled: May 19, 2009Date of Patent: September 25, 2012
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Publication number: 20120231010Abstract: The present invention provides a method of promoting bone growth in a subject in need thereof, by administering to the subject a therapeutically effective amount of a compound of Formula I. The compounds include the salts, hydrates and isomers thereof. The present invention also provides methods for the treatment of renal disease and cancer.Type: ApplicationFiled: May 17, 2012Publication date: September 13, 2012Applicant: OsteoGeneX Inc.Inventors: Debra Ellies, William Rosenberg
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Publication number: 20120232011Abstract: The present invention relates to a new use of rapamycin and rapamycin derivatives.Type: ApplicationFiled: May 18, 2012Publication date: September 13, 2012Inventors: Michaela Kneissel, Mira Susa Spring
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Patent number: 8263580Abstract: A pharmaceutical aerosol foam composition, comprising: an effective amount of a pharmaceutically active ingredient, wherein said pharmaceutically active ingredient is a vitamin or analogue thereof; an occlusive agent; an aqueous solvent; an organic cosolvent; wherein the pharmaceutically active ingredient is insoluble in both water and the occlusive agent; and the occlusive agent being present in an amount sufficient to form an occlusive layer on the skin, in use. In a second embodiment, an oil-in water emulsion having a vitamin, an occlusive agent; an aqueous solvent; and an organic cosolvent, wherein the occlusive agent is present in an amount sufficient to form an occlusive layer on the skin.Type: GrantFiled: May 26, 2006Date of Patent: September 11, 2012Assignee: Stiefel Research Australia Pty LtdInventors: Richard Buchta, Robert James Houlden, Rose Ye, Maria Graziella Larm, Leon Loupenok
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Patent number: 8263582Abstract: A method of administration of an oral pharmaceutical product to patients suffering from inflammatory disorders of the gastrointestinal tract comprises orally administering to the patient at least two different dosage forms of a therapeutically effective amount of a topically active corticosteroid, such as beclomethasone dipropionate (BDP).Type: GrantFiled: March 15, 2002Date of Patent: September 11, 2012Assignee: Soligenix, Inc.Inventors: Nicholas Stergis, George B. McDonald
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Patent number: 8263667Abstract: A nutritional supplement for use in physiologically stressful conditions is disclosed. The nutritional supplement may include one or more of vitamin A, vitamin E, vitamin D3, vitamin C, vitamin B1, riboflavin, niacin, folic acid, vitamin B6, biotin, pantothenic acid, vitamin B12, magnesium, zinc, selenium, chromium, copper, iron, alpha lipoic acid, lutein and lycopene.Type: GrantFiled: March 8, 2011Date of Patent: September 11, 2012Assignee: Vertical Pharmaceuticals, Inc.Inventors: Steven A. Squashic, Kevin M Hudy, David C. Purdy
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Publication number: 20120214773Abstract: The invention relates to pharmaceutical formulations of lipophilic therapeutic agents in which such agents are solubilized in largely aqueous vehicles, and processes for preparing and using the same.Type: ApplicationFiled: August 22, 2011Publication date: August 23, 2012Inventors: Richard B. Mazess, Jeffrey W. Driscoll, Creighton Reed Goldensoph, Leon W. LeVan
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Publication number: 20120213713Abstract: The present invention discloses compositions of omega polyunsaturated fatty acids for controlling and preventing dental caries resulting from oral infections. The compositions of fatty acids include omega-3 fatty acids, omega-6 fatty acids, and other fatty acids, for their synergistic bioactivity against cariogenic pathogens. The application of this composition can be used for the preparation of drugs, nutritional supplements, food and daily necessities with oral health care and therapeutic effects.Type: ApplicationFiled: February 18, 2011Publication date: August 23, 2012Inventors: Chifu Huang, Jeffrey Lee Ebersole
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Publication number: 20120207707Abstract: Methods of increasing production, stability or activity of a target polypeptide are provided herein. The method includes increasing the level of an antioxidant in a cell comprising a polynucleotide encoding the target polypeptide. Also provided are cells and transgenic organisms produced using the methods described herein. Methods of treating a subject with a condition treatable by administration of the target polypeptide are also disclosed. Finally methods and compositions for transiently increasing antioxidants in plant cells are provided.Type: ApplicationFiled: October 22, 2010Publication date: August 16, 2012Inventors: Maureen C. Dolan, Argelia Lorence, Giuliana Medrano
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Publication number: 20120195981Abstract: A bolus dose supplement, foodstuff, beverage and beverage concentrate with calcium and vitamin D for the treatment and prevention of PMS, panic attacks, and postpartum depression. The combination of adequate calcium and vitamin D is provided as a multi-vitamin and mineral supplement. The bolus dose is comprised of 2 main ingredients calcium and vitamin D at 1000-1500 mg of elemental calcium in the form of carbonate or citrate or gluconate or citrate maleate and 400-20,000 I.U.Type: ApplicationFiled: April 4, 2012Publication date: August 2, 2012Inventor: Susan THYS-JACOBS
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Publication number: 20120196837Abstract: Disclosed is a method of treatment or prevention of frailty in an elderly patient, particularly having an age of 60 or older. The method provides the concomitant parenteral administration of a combination of an anabolic steroid and a vitamin D compound. A preferred combination comprises nandrolone decanoate and cholecalciferol (vitamin D3). The invention, in a further preference, provides a booster therapy to support frail elderly that have undergone hospitalization or surgery to retain independence and regain their regular physical and mental activities.Type: ApplicationFiled: August 23, 2010Publication date: August 2, 2012Inventors: Marjanna Prins, Helenius Jan Kloosterboer
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Patent number: 8232263Abstract: 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: GrantFiled: July 9, 2007Date of Patent: July 31, 2012Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Bulli Padmaja Tadi, Lori A. Plum, Margaret Clagett-Dame
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Publication number: 20120190656Abstract: Disclosed herein are diagnostic methods for determining whether subjects will be responsive to vitamin D therapy. The methods involve the detection of one or more single nucleotide polymorphisms in a test sample, in combination with other clinical factors. The tests are suitable for diagnosing and determining a treatment regime for patients having or suspected of having a cardiovascular disease, including hyperlipidemia or hypertriglyceridemia.Type: ApplicationFiled: December 20, 2011Publication date: July 26, 2012Inventors: Brian H. Shirts, Steven C. Hunt, Paul N. Hopkins
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Publication number: 20120184514Abstract: An air-stable, high-melt 1a-hydroxy-vitamin D3 compound, methods for preparing an animal feed composition, methods of preparing 1?-hydroxy-vitamin D3, methods of enhancing phytate phosphorus and calcium utilization, and an animal feed regime are provided.Type: ApplicationFiled: June 29, 2010Publication date: July 19, 2012Applicant: Vitamin Derivatives Inc.Inventors: Hardy M. Edwards, George Majetich, Richard Hill, Dezhi Sha, George Yiannikouros
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Patent number: 8222235Abstract: 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: GrantFiled: November 18, 2005Date of Patent: July 17, 2012Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Lori A. Plum, Margaret Clagett-Dame
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Patent number: 8222236Abstract: 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: GrantFiled: July 10, 2008Date of Patent: July 17, 2012Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Bulli Padmaja Tadi, Lori A. Plum, Margaret Clagett-Dame
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Publication number: 20120177744Abstract: Disclosed are methods of treating an individual having a condition characterized by an imbalance in type 1 and type 2 cytokine production, wherein the method comprises administering to the individual an amount of ?-hydroxy-?-methylbutyrate (HMB) effective to modulate or otherwise cause an increase in the ratio of type 1 to type 2 cytokines, including an increase in the ratio of type 1 to type 2 cytokines without a corresponding increase in type 2 cytokine levels. Also disclosed are methods of using HMB to treat asthma and allergies. The methods of the present invention are based upon the discovery that HMB modulates cytokine production, most typically by increasing type 1 cytokines without a corresponding increase in type 2 cytokines.Type: ApplicationFiled: January 11, 2012Publication date: July 12, 2012Applicant: ABBOTT LABORATORIESInventors: Debra L. Thomas, Pradip Mukerji
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Publication number: 20120177699Abstract: A preparation method of drug loaded emulsion is disclosed. The method comprises the steps of: preparing a non-self emulsifying O/W blank emulsion having no active ingredients; then, adding therapeutically effective amount of active ingredients to the 0/W blank emulsion, adjusting pH to distribute the active ingredients through the membrane to obtain the desired emulsion.Type: ApplicationFiled: June 3, 2010Publication date: July 12, 2012Applicants: SHANGHAI HENGRUI PHARMACEUTICAL CO., LTD., JIANGSU HENGRUI MEDICINE CO., LTD.Inventors: Xinyong Tong, Haifeng Wang, Li Lu, Liang Chen, Yuan Shi
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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: 20120171307Abstract: A composition for administration to a subject, such as oral administration to a subject, for example, has been provided. Such a composition may comprise at least one magnesium-counter ion compound. A magnesium-counter ion composition described herein may be useful for any of a variety of applications provided herein, such as maintaining, enhancing, and/or improving health, nutrition, and/or another condition of a subject, and/or cognitive, learning, and/or memory function. A magnesium-counter ion composition provided herein may be useful for administration to a subject presenting magnesium deficiency, mild cognitive impairment, Alzheimer's disease, attention deficit hyperactivity disorder, ALS, Parkinson's disease, diabetes, migraine, anxiety disorder, mood disorder, and/or hypertension. A kit, method, and other associated technology are also provided.Type: ApplicationFiled: February 22, 2012Publication date: July 5, 2012Applicant: Magceutics, Inc.Inventors: Guosong Liu, Fei Mao
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Publication number: 20120165300Abstract: 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: ApplicationFiled: January 6, 2012Publication date: June 28, 2012Inventors: Hector F. DeLUCA, Agnieszka FLORES, Pawel GRZYWACZ, Lori A. PLUM, Margaret CLAGETT-DAME, James B. THODEN, Hazel M. HOLDEN
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Publication number: 20120165301Abstract: The present invention provides, for example, pharmaceutical compositions comprising a benzodiazepine compound and an agent selected from the group consisting of a topical steroid, a keratolytic agent, a topical retinoid, a coal tar, and a vitamin D-3 analog. The pharmaceutical compositions are useful for treating medical disorders, such as epidermal hyperplasia.Type: ApplicationFiled: February 13, 2012Publication date: June 28, 2012Applicant: The Regents of the University of MichiganInventor: Gary D. Glick
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Patent number: 8207149Abstract: A stable, controlled release formulation for oral dosing of vitamin D compounds is disclosed. The formulation is prepared by incorporating one or more vitamin D compounds into a solid or semi-solid mixture of waxy materials. Oral dosage forms can be prepared by melt-blending the components described herein and filling gelatin capsules with the formulation.Type: GrantFiled: September 26, 2011Date of Patent: June 26, 2012Assignees: Cytochroma, Inc., Proventiv Therapeutics, LLCInventors: Samir P. Tabash, Jay A. White, Charles W. Bishop, Sammy A. Agudoawu, Eric J. Messner, P. Martin Petkovich
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Publication number: 20120156216Abstract: The various embodiments of the present invention are directed to methods and compositions for treatment, inhibition or reduction of metastasis in cancers. In particular, the invention is related to compositions and methods affecting connective tissue growth factor (CTGF). An aspect of the present invention comprises a method for interfering with the activity of connective tissue growth factor, comprising, administering to a subject an effective amount of a composition that inhibits production of or activity of connective tissue growth factor (CTGF), wherein the composition interferes with the activity of CTGF or prevents the transcription of CTGF genes or translation of CTGF mRNA. For example, the composition can comprises at least one HMG-CoA reductase inhibitor compound, such as a statin.Type: ApplicationFiled: March 2, 2010Publication date: June 21, 2012Inventor: Youngman OH
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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: 8202546Abstract: In one embodiment of the present invention, a pharmaceutically-acceptable single-dosage formulation consists essentially of about 300 mg of vitamin C; about 1200 IUs of vitamin D3; about 125 IUs of vitamin E; about 25 mg of vitamin B1; about 3.4 mg of vitamin B2; about 35 mg of niacin; about 35 mg of vitamin B6; about 1.25 mg of folate; about 70 mcg of vitamin B12; about 5 mg of pantothenic acid; about 300 mcg of biotin; about 50 mg of calcium; about 35 mg of magnesium; about 35 mg of zinc; about 1 mg of copper; about 125 mcg of selenium; about 150 mcg of chromium; about 25 mg of alpha lipoic acid; about 35 mg of co-enzyme Q-10; about 2 mg of lutein; about 500 mcg of lycopene; about 5 mg of pepper extract; and at least one or more excipients.Type: GrantFiled: February 2, 2010Date of Patent: June 19, 2012Assignee: Vertical Pharmaceuticals, Inc.Inventors: Steven A. Squashic, Kevin M. Hudy, David C. Purdy
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Publication number: 20120149669Abstract: 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: ApplicationFiled: November 11, 2011Publication date: June 14, 2012Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATIONInventors: Hector F. DeLuca, Rafal Barycki, Lori A. Plum
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Publication number: 20120148636Abstract: A process for producing micronized dispersed micro-particles and to micro-particles produced by this process.Type: ApplicationFiled: June 24, 2010Publication date: June 14, 2012Inventors: Colin Berrido, Peter Rabke, Hans-Jurgen Huppert
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Patent number: 8198263Abstract: The invention relates to vitamin D derivatives and their uses, particularly in the pharmaceutical industry. The invention discloses compounds having different interesting biological properties, including vitamin D nuclear receptor (VDR) agonist activity, as well as therapeutics methods by administering said compounds, in particular for treating cancer, psoriasis, autoimmune diseases, osteodistrophy and osteoporosis. It further relates to pharmaceutical compositions comprising said compounds and methods for preparing the same.Type: GrantFiled: September 26, 2006Date of Patent: June 12, 2012Assignees: Centre National de la Recherche Scientifique, Universite De Strasbourg, Universidad De Santiago De Compostela, Institut National de la Sante Et de la Recherche MedicaleInventors: Dino Moras, Antonio Mourino-Mosquera, Luis Cezar Rodrigues, Natacha Rochel, Jean-Marie Wurtz
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Patent number: 8197854Abstract: A nutritional supplement for use in physiologically stressful conditions is disclosed. The nutritional supplement may include one or more of vitamin A, vitamin E, vitamin D3, vitamin C, vitamin B1, riboflavin, niacin, folic acid, vitamin B6, biotin, pantothenic acid, vitamin B12, magnesium, zinc, selenium, chromium, copper, iron, alpha lipoic acid, lutein and lycopene.Type: GrantFiled: March 7, 2011Date of Patent: June 12, 2012Assignee: Vertical Pharmaceuticals, Inc.Inventors: Steven A. Squashic, Kevin M Hudy, David C. Purdy
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Publication number: 20120141446Abstract: A composition for increasing the bioavailability of nutrients in humans and animals comprising an oil base emulsion into which nutrients selected from the group comprising omega fatty acids, vitamin D, Co Q10, green tea extract, and policosanol are added.Type: ApplicationFiled: December 2, 2010Publication date: June 7, 2012Inventor: Bhiku Patel
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Publication number: 20120141483Abstract: The present invention provides indane acetic acids and their derivatives and methods for the treatment and/or prevention of psoriasis and/or Alzheimer's diseases using the same.Type: ApplicationFiled: June 3, 2010Publication date: June 7, 2012Inventor: Mary Katherine Delmedico
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Patent number: 8193169Abstract: This invention discloses (20R)-2?-methyl-19,26,27-trinor-vitamin D analogs, and specifically (20R)-2?-methyl-19,26,27-trinor-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 very low activity in vivo on bone calcium mobilization and 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: GrantFiled: July 10, 2008Date of Patent: June 5, 2012Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Pawel Grzywacz, Lori A. Plum, Margaret Clagett-Dame
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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: 8193170Abstract: This invention discloses 2-methylene-19,26-dinor-(20R,22E,25R)-vitamin D analogs, and specifically 2-methylene-19,26-dinor-(20R,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 very low activity in vivo on bone calcium mobilization and relatively high 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: GrantFiled: July 10, 2008Date of Patent: June 5, 2012Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Grazia Chiellini, Pawel Grzywacz, Lori A. Plum, Margaret Clagett-Dame
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Publication number: 20120135002Abstract: The present invention relates to a pharmaceutical composition comprising: a) at least one iron uptake inhibitor, and b) at least one vitamin D and/or at least one analog thereof and/or at least one vitamin D receptor modulator, and optionally a pharmaceutically acceptable carrier.Type: ApplicationFiled: July 16, 2009Publication date: May 31, 2012Inventors: Ivan Cruz Moura, Olivier Hermine, Celine Callens, Severine Coulon
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Patent number: 8188065Abstract: The present invention provides a method of promoting bone growth in a subject in need thereof, by administering to the subject a therapeutically effective amount of a compound of Formula I. The present invention also provides methods for the treatment of renal disease and cancer.Type: GrantFiled: October 1, 2009Date of Patent: May 29, 2012Assignee: OsteoGeneX Inc.Inventors: Debra Ellies, William Rosenberg
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Patent number: 8188064Abstract: Methods for treating and preventing obesity, inhibiting adipocyte differentiation, inhibiting increased SCD-1 gene transcription, and/or reducing body fat in a subject include administering at least one analog of 1?,25-dihydroxyvitamin D3 or 1?,25-dihydroxyvitamin D2 or a pharmaceutical composition that includes such an analog to a subject in need thereof. The analog may be a 19-nor vitamin D analog such as a compound of formula IA, a compound of formula IB, or a mixture thereof where the variables R1, R2, and R3 have the values described herein.Type: GrantFiled: November 24, 2004Date of Patent: May 29, 2012Assignee: Wisconsin Alumni Research FoundationInventors: Margaret Clagett-Dame, Hector F. DeLuca, Jamie M. Ahrens, James M. Ntambi, Brian Thomson
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Publication number: 20120128612Abstract: The present invention relates generally to antifugal compositions. In an embodiment, the antifungal compositions are effective for application to nails and surrounding skin, and comprise at least one volatile solvent, at least one film forming substance, and at least one pyrimidone derivative of formula I, such as albaconazole. These compositions are capable of treating an infection caused by fungi, such as onychomychosis.Type: ApplicationFiled: May 27, 2010Publication date: May 24, 2012Applicant: PALAU PHARMA, S.A.Inventors: Jon Lenn, Hans Hofland, Edward Hsia
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Publication number: 20120122784Abstract: The invention relates to novel calcium-sensing receptor (CaSR) modulating substituted cyclopentylene compounds represented in formula I and derivatives thereof, to said compounds for use as a medicament, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases with said compounds, and to the use of said compounds in the manufacture of medicaments.Type: ApplicationFiled: May 26, 2010Publication date: May 17, 2012Applicant: LEO PHARMA A/SInventors: Bjarne Nørremark, Lars Kristian Albert Blæhr, Anne Eeg Knapp, Kristoffer Månsson
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Patent number: 8178099Abstract: The present invention provides a method of promoting local bone growth by administering a therapeutic amount of a Sost antagonist to a mammalian patient in need thereof. Preferably, the Sost antagonist is an antibody or FAB fragment selectively recognizing any one of SEQ ID NOS: 1-23. The Sost antagonist may be coadministered together or sequentially with a matrix conducive to anchoring new bone growth. Orthopedic and Periodontal devices comprising an implantable portion adapted to be permanently implanted within a mammalian body and bearing an external coating of a Sost antagonist are also disclosed, as it a method of increasing bone density by administering to a mammalian patient a therapeutic amount of a Sost antagonist together with an antiresorptive drug.Type: GrantFiled: December 21, 2007Date of Patent: May 15, 2012Assignee: OsteoGeneX Inc.Inventor: Debra L. Ellies
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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: 20120115804Abstract: The invention features compositions and methods for characterizing the methylation status of the Vitamin D Receptor (VDR) in neoplasia (e.g., breast carcinoma), selecting an appropriate therapy, and treating the neoplasia (e.g., breast carcinoma).Type: ApplicationFiled: March 10, 2010Publication date: May 10, 2012Applicant: The John Hopkins UniversityInventors: Radharani Marik, Christopher B. Umbricht, Martha A. Zeiger
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Publication number: 20120115824Abstract: Disclosed is a compound of Formula (I) in which R1, R2, R3, R4, R5, R6, X, and a are defined herein, or a pharmaceutically acceptable salt thereof. Also disclosed are a pharmaceutical composition comprising a compound or salt thereof of Formula (I) and a method of treating a disease which benefits from the modulation of the vitamin D receptor, such as a bone disorder, cardiovascular disease, a cardiovascular complication associated with renal disease, endothelial dysfunction, hyperparathyroidism, hypocalcemia, an immune disorder, left ventricular hypertrophy, a proliferative disease, proteinuria, renal disease, and thrombosis.Type: ApplicationFiled: April 12, 2010Publication date: May 10, 2012Applicant: VIDASYM, LLCInventor: Megumi Kawai
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Patent number: 8173160Abstract: The invention provides compositions for an administration to a mammal orally or in a suppository that include one or more edible oils (preferably including one or more omega-3 fatty acids), one or more plant stanols, phytosterols, or esters thereof, and admixed in the one or more edible oils one or more water-soluble vitamins and/or minerals, for example, vitamins B6, B9 and/or B12. The invention also provides a method of making the compositions comprising mixing the foregoing components to form a suspension or emulsion of the vitamins and/or minerals in the edible oils. The mixture can be inserted into hollow soft or hard capsules, gelcaps or caplets. The edible oils can coat particles of the water-soluble vitamins and/or minerals, which may provide them with an improved absorption in the body due to an increased resistance to degradation in the acidic environment of the stomach.Type: GrantFiled: May 18, 2005Date of Patent: May 8, 2012Assignee: PBM Pharmaceuticals, Inc.Inventors: Jack H. Schramm, James W. McGrath, Jr.