9,10-seco- Cyclopentanohydrophenanthrene Ring System (e.g., Vitamin D, Etc.) Doai Patents (Class 514/167)
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Patent number: 8414910Abstract: The invention relates to a medical device for delivering a therapeutic agent to a tissue. The medical device has a layer overlying the exterior surface of the medical device. The layer contains a therapeutic agent, an antioxidant, and an additive. In certain embodiments, the additive has a hydrophilic part and a drug affinity part, wherein the drug affinity part is at least one of a hydrophobic part, a part that has an affinity to the therapeutic agent by hydrogen bonding, and a part that has an affinity to the therapeutic agent by van der Waals interactions. In some embodiments, the additive is a liquid. In other embodiments, the additive is at least one of a surfactant and a chemical compound, and the chemical compound has one or more hydroxyl, amino, carbonyl, carboxyl, acid, amide or ester groups.Type: GrantFiled: March 25, 2010Date of Patent: April 9, 2013Assignee: Lutonix, Inc.Inventor: Lixiao Wang
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Publication number: 20130085121Abstract: The present invention is an oral solid pharmaceutical compositions for the treatment of kidney diseases and mineral bone disorder including a phosphate binder, a calcium receptor-active compound and at least one pharmaceutically acceptable excipient, the invention further including a method for preparing the pharmaceutical compositions including the steps of granulating cinacalcet and/or sevelamer and/or vitamin D by one of a wet and a dry granulation process, each with at least one pharmaceutically acceptable excipient to form cinacalcet granules and/or sevelamer granules and/or vitamin D granules, mixing at least two of the cinacalcet granules, sevelamer granules and vitamin D granules to form a granules mixture and compressing the granules mixture to tablets or encapsulating the granules mixture into capsules or pulverizing the granules mixture into a dispersion powder.Type: ApplicationFiled: September 13, 2012Publication date: April 4, 2013Inventors: Jianguo Wang, Yuehua Sun
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Publication number: 20130084272Abstract: The present invention relates to compositions, kits and methods for the administration of compositions and kits for supplementation with twelve carbon chain fatty acids or twelve carbon chain acylglycerols; and specifically for the supplementation with twelve carbon chain fatty acids such as lauric acid and twelve carbon chain acylglycerols such as monolaurin; and specifically for the co-supplementation with other vitamins, minerals and nutrients.Type: ApplicationFiled: September 29, 2011Publication date: April 4, 2013Inventors: Philippe PERRIN, Guillaume HERRY, Cecile BOYER-JOUBERT
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Patent number: 8410080Abstract: 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: GrantFiled: October 11, 2012Date of Patent: April 2, 2013Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Lori A. Plum, Rafal R. Sicinski, Izabela Sibilska
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Publication number: 20130078318Abstract: Combined therapies and oral dosage forms based on genistein for the support of osteoporotic health.Type: ApplicationFiled: November 26, 2012Publication date: March 28, 2013Applicant: Primus Pharmaceuticals Inc.Inventors: Bruce P. Burnett, James D. Weir, Francesco Squadrito
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Patent number: 8404667Abstract: 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: GrantFiled: December 28, 2007Date of Patent: March 26, 2013Assignee: Wisconsin Alumni Research FoundationInventors: Margaret Clagett-Dame, Hector F. DeLuca, Nirca J. Nieves, Lori A. Plum, Mary E. Kaiser
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Patent number: 8404874Abstract: 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: GrantFiled: September 28, 2011Date of Patent: March 26, 2013Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Pawel Grzywacz, James B. Thoden, Hazel Holden
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Patent number: 8403910Abstract: The invention relates to a medical device for delivering a therapeutic agent to a tissue. The medical device has a layer overlying the exterior surface of the medical device. The layer contains a therapeutic agent and an additive. The additive has a hydrophilic part and a hydrophobic part and the therapeutic agent is not enclosed in micelles or encapsulated in particles or controlled release carriers.Type: GrantFiled: March 7, 2011Date of Patent: March 26, 2013Assignee: Lutonix, Inc.Inventor: Lixiao Wang
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Patent number: 8404666Abstract: 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: GrantFiled: April 6, 2007Date of Patent: March 26, 2013Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Lori A. Plum, Margaret Clagett-Dame, Pawel Grzywacz
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Patent number: 8399439Abstract: 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: GrantFiled: July 10, 2008Date of Patent: March 19, 2013Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Grazia Chiellini, Pawel Grzywacz, Lori A. Plum, Margaret Clagett-Dame
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Patent number: 8399438Abstract: 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: GrantFiled: November 18, 2005Date of Patent: March 19, 2013Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Rafal R. Sicinski, Lori A. Plum, Margaret Clagett-Dame, Sumithra Gowlugari
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Publication number: 20130065867Abstract: This invention relates to methods for administering an effective amount of a dietary or nutritional supplement composition that effectively changes the quality of the meibum lipid composition of inflamed or dysfunctional meibomian glands so as to improve or increase tear break up time, reduce tear osmolarity, and elevate the omega-3 index, while reducing or eliminating the symptoms associated with dry eye or meibomianitis. The dietary or nutritional supplement composition administered to the patient suffering from inflamed or dysfunctional meibomian glands comprises an effective amount of omega-3 fatty acids.Type: ApplicationFiled: July 18, 2012Publication date: March 14, 2013Inventors: S. Gregory Smith, Michael B. Gross, Olav E. Sandnes
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Publication number: 20130059795Abstract: This invention describes a novel composition of matter describing a complex comprising leaf protein and a lipophilic substance(s), along with the method of producing it. Delivery of lipid-soluble materials into the body is challenging because they are generally highly insoluble in water and very subject to oxidative degradation. The inventors have found that leaf protein—the water-soluble proteins derived from plant leaves—can efficiently form a complex with lipophilic materials. This leaf protein—lipid-soluble material complex is an effective carrier of lipophilic substances. As such, the leaf protein—lipid-soluble material complex disclosed herein can be used for the delivery of lipophilic vitamins, fatty acids, caretenoids, lipophilic drugs, and other lipophilic materials. This complex can be used to deliver lipophiles in foods, nutritional and dietary supplements, topical compositions and in pharmaceutical products.Type: ApplicationFiled: March 7, 2011Publication date: March 7, 2013Inventors: Yangming Martin Lo, Ansu Elizabeth Cherian, Neil Allen Belson
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Publication number: 20130059825Abstract: Provided herein are antigenic molecules that can be used to generate antibodies capable of binding to a vitamin D derivative, such as 25-hydroxyvitamin D2 and/or 25-hydroxyvitamin D3, or a 25-hydroxyvitamin D analog, such as a vitamin D-C22 immunogenic molecule or compound. Antibodies produced using these antigenic molecules, and related antigenic compounds, are also described. In addition, disclosed herein are methods for detecting vitamin D deficiency in a subject, methods for treating a subject suspected of having a vitamin D deficiency, methods for monitoring progression of vitamin D deficiency in a subject, and methods for monitoring treatment of vitamin D deficiency in a subject in need thereof. Also provided are methods and reagents for the detection or quantification of 25-hydroxyvitamin D2 and D3, methods for stabilizing vitamin D analogs, and methods for separating 25-hydroxyvitamin D2 and D3 from vitamin D binding protein in a biological sample.Type: ApplicationFiled: April 27, 2012Publication date: March 7, 2013Applicant: Siemens Healthcare Diagnostics Inc.Inventors: Niver Panosian Sahakian, Bruce A. Campbell, Spencer Hsiang-Hsi Lin, James Vincent Freeman, Qimu Liao, Ramon A. Evangelista
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Patent number: 8389501Abstract: Azadirachta indica cell suspension culture is used to metabolize dianabol to yield potent anticarcinogenic 17?-hydroxy-17?-methyl-5?-androst-1-en-3-one, which can also be synthesized.Type: GrantFiled: July 17, 2011Date of Patent: March 5, 2013Inventors: Saifullah, Saifullah Khan, Azizuddin, Muhammad Kashif, Ahsana Dar, Muhammad Iqbal Choudhary
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Publication number: 20130053356Abstract: 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: ApplicationFiled: August 23, 2012Publication date: February 28, 2013Inventors: Hector F. DELUCA, Margaret Clagett-Dame, Lori A. Plum, Agnieszka Glebocka, Rafal Sicinski
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Publication number: 20130053355Abstract: This disclosure provides products, including pharmaceutical compositions and dietary supplements, which are useful for anti-inflammatory support.Type: ApplicationFiled: June 12, 2012Publication date: February 28, 2013Applicant: Rock Creek Pharmaceuticals, Inc.Inventor: Jonnie R. Williams
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Publication number: 20130045183Abstract: The present disclosure relates to non-acidic extracts or fractions selected from a Boswellia low polar gum resin extract fraction (BLPRE), a Boswellia volatile oil fraction (BVOIL), and a Boswellia oil fraction (BOIL) and their compositions. BLPRE, BOIL, and BVOIL are each derived from the gum resin of a Boswellia species. These compositions are useful for improving mental condition, enhancing brain functions such as cognition, memory, learning, communication and brain health, for treating impaired memory, and for preventing, control or treating memory and cognition related disorders/diseases. Additionally, BOIL, BVOIL, and mixtures of BOIL and BVOIL are useful for enhancing the bioavailability of a biological agent.Type: ApplicationFiled: September 14, 2012Publication date: February 21, 2013Applicant: LAILA NUTRACEUTICALSInventors: Ganga Raju GOKARAJU, Rama Raju GOKARAJU, Venkata Kanaka Ranga Raju GOKARAJU, Trimurtulu GOLAKOTI, Kiran BHUPATHIRAJU, Venkata Krishna Raju ALLURI
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Patent number: 8377913Abstract: The invention relates to compounds that are vitamin D receptor activators, compositions comprising such compounds, methods of using such compounds and compositions, processes for preparing such compounds, and intermediates obtained during such processes.Type: GrantFiled: September 8, 2008Date of Patent: February 19, 2013Assignee: AbbVie Inc.Inventors: Thomas W. Von Geldern, Jufang H. Barkalow, David M. Barnes, Anthony R. Haight, John E. Hengeveld, Xiaofeng Li, Maureen A. McLaughlin, William T. Noonan, Zhonghua Pei, Jinshyun Ruth Wu-Wong
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Patent number: 8377914Abstract: The current invention is directed to methods of inducing the negative chemotaxis of a migratory cell comprising contacting the cell with a compound selected from the group consisting of idebenone, benazepril, rolipram, moxonidine, lamivudine, loxoprofen, terbinafine, Synephrine, 6-aminoindazole, and a Vitamin D analog, or a pharmaceutically acceptable salt of any of thereof.Type: GrantFiled: October 9, 2009Date of Patent: February 19, 2013Assignee: Celtaxsys, Inc.Inventor: Erica Brook Goodhew
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Publication number: 20130039952Abstract: Calcipotriol monohydrate nanocrystals prepared by the process disclosed herein may be incorporated in a pharmaceutical composition for use in the prevention or treatment of dermal diseases and conditions.Type: ApplicationFiled: December 22, 2010Publication date: February 14, 2013Applicant: LEO PHARMA A/SInventor: Karsten Petersson
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Patent number: 8372808Abstract: Provided herein are methods of decreasing glial fibrillary acidic protein (GFAP) levels in a cell. Such methods include administering an effective amount of a GFAP lowering compound to the cell. Also provided are compounds useful for the treatment of Alexander disease in subjects at risk of or diagnosed with Alexander disease and methods for the identification of such compounds.Type: GrantFiled: October 26, 2009Date of Patent: February 12, 2013Assignee: Wisconsin Alumni Research FoundationInventors: Albee Messing, Woosung Cho, Jon Scott Thorson, Randal D. Goff
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Patent number: 8367116Abstract: The invention provides compositions and methods for treating a subject who has suffered from a central nervous system disorder. More particularly, the invention provides sustained polymeric drug delivery systems having a polymer particle, a therapeutic agent, and a buoyancy agent for direct delivery of therapeutic agents into the central nervous system.Type: GrantFiled: March 18, 2011Date of Patent: February 5, 2013Assignee: Seacoast Neuroscience, Inc.Inventors: Daniel Pratt, Samuel S. Macausland, Keith Baker
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Patent number: 8362287Abstract: The present invention relates to intermediates useful for the synthesis of calcipotriol or calcipotriol monohydrate, to methods of producing said intermediates, and to methods of stereoselectively reducing said intermediates.Type: GrantFiled: March 10, 2005Date of Patent: January 29, 2013Assignee: Leo Pharma A/SInventors: Thomas Peter Sabroe, Martin John Calverley
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Publication number: 20130023501Abstract: A substantially anhydrous, topical pharmaceutical composition comprising a non-alcoholic three-component solvent mixture and a biologically active vitamin D derivative or analogue dissolved therein as well as a pharmaceutically acceptable carrier may be used in the treatment of dermal conditions.Type: ApplicationFiled: December 22, 2010Publication date: January 24, 2013Applicant: LEO PHARMA A/SInventor: Karsten Petersson
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Publication number: 20130017234Abstract: An implant to be used as medical or dental implant, comprising a metallic or polymeric base which is covered by the vitamin D precursor cholecalciferol. The implant can be obtained by direct covering of the polymeric or metallic base with a solution comprising cholecalciferol or also covering the base with the 7-dehydrocholesterol (7-DHC), and subsequently irradiated with UV light to induce the formation of cholecalciferol. Optionally, the coating of the implant may include an antioxidant such as vitamin E. This implant enhances osseointegration in compromised patients by means of the endogenous synthesis and activity of vitamin D in hard and mineralized tissue regeneration. Furthermore, a method to obtain these implants which comprises coating the surface of the implant directly with cholecalciferol or with a specific concentration of 7-DHC and irradiated with UV light to induce the formation of cholecalciferol.Type: ApplicationFiled: July 26, 2012Publication date: January 17, 2013Applicant: Numat Biomedical S.L.Inventors: Ståle Petter Lyngstadaas, Marta Monjo, Christlane Petzold, Jan Erik Ellingsen
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Publication number: 20130018021Abstract: 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: ApplicationFiled: September 18, 2012Publication date: January 17, 2013Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATIONInventor: Wisconsin Alumni Research Foundation
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Publication number: 20130011342Abstract: A substantially surface active agent-free and foam adjuvant-free composition which includes a hydrophobic solvent, a wax and a propellant. A substantially surface active agent-free and foam adjuvant-free composition, further comprising, a tetracycline antibiotic, or one or More other active agents. A method of treatment, using a substantially surface active agent-free and substantially foam adjuvant-free composition.Type: ApplicationFiled: October 1, 2010Publication date: January 10, 2013Applicant: FOAMIX LTD.Inventors: Dov Tamarkin, Elana Gazal, Irakliy Papiashvili, Yohan Hazot, David Schuz, Rita Keynan, Nukzi Papiashvile
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Publication number: 20130012484Abstract: Novel compositions in petroleum jelly-free unguent form, in particular for topical application, contain a vitamin D compound and optionally an active agent of the family of steroidal anti-inflammatory agents.Type: ApplicationFiled: September 14, 2012Publication date: January 10, 2013Applicant: GALDERMA S.A.Inventors: Nathalie WILLCOX, Nathalie BARTHEZ, Karine NADAU-FOURCADE, Claire MALLARD
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Publication number: 20130012483Abstract: The present invention relates to a pharmaceutical composition comprising an NMDA receptor antagonist and vitamin D as active ingredients for the treatment of neurodegenerative or neurovascular diseases.Type: ApplicationFiled: March 4, 2011Publication date: January 10, 2013Inventors: Olivier Beauchet, Cédric Annweiler
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Patent number: 8349818Abstract: 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: GrantFiled: October 21, 2010Date of Patent: January 8, 2013Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Jamie Nehring, Ehren N. Rudolph, Lori Plum
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Publication number: 20130005680Abstract: A topical pharmaceutical composition which is an oil-in-water-oil emulsion comprising a vitamin D derivative or analogue dissolved in a mixture of a non-ionic surfactant and a lower alkanol. The topical pharmaceutical composition may be used in the treatment of dermal conditions, such as psoriasis.Type: ApplicationFiled: December 22, 2009Publication date: January 3, 2013Applicant: LEO PHARMA A/SInventor: Karsten Petersson
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Publication number: 20130005694Abstract: The present invention relates to a liquid composition comprising vitamin D, or a salt thereof. Specific embodiments employ 5000 IU to 250,000 IU, and include sorbate and benzoate as a preserving agent.Type: ApplicationFiled: December 2, 2010Publication date: January 3, 2013Inventors: Evan Hayes, Sean Michael Hall, Melissa Luke
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Publication number: 20130005686Abstract: 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: ApplicationFiled: June 26, 2012Publication date: January 3, 2013Applicant: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Margaret Clagett-Dame, Lori A. Plum, Rafal Barycki
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Patent number: 8343557Abstract: The present invention relates to synergic compositions incorporating agents for reducing cellulite and unaesthetic appearance associated therewith which comprise a base matrix constituted by conjugated linoleic acid (CLA), grape seed extract, beta-glucan, organic calcium and dry extract of pine bark together with complementary synergic agents of the matrix. The invention also relates to the use of such compositions and formulations containing said compositions.Type: GrantFiled: October 27, 2009Date of Patent: January 1, 2013Assignee: STARGATE—Produtos Farmacêuticos, Dietéticos e Nutricionais, Lda.Inventor: Edoardo Messora
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Publication number: 20120329764Abstract: The present invention is related to compositions and methods for treating or reducing the likelihood of a migraine, reducing the severity of migraine, reducing the frequency of migraines, reducing the duration of migraine, and ameliorating the symptoms of a migraine. The methods and compositions of the present invention may also be used to treat or prevent condition characterized by increased cardiovascular risk or endothelial dysfunction and musculoskeletal symptoms.Type: ApplicationFiled: January 10, 2011Publication date: December 27, 2012Applicant: BETH ISRAEL DEACONESS MEDICAL CENTER, INC.Inventors: Rami Burstein, Catherine Buettner
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Patent number: 8338393Abstract: Combined therapies and oral dosage forms based on genistein for the support of osteoporotic health.Type: GrantFiled: March 23, 2009Date of Patent: December 25, 2012Assignee: Primus Pharmaceuticals, Inc.Inventors: Bruce P. Burnett, James D. Weir, Francesco Squadrito
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Publication number: 20120322776Abstract: A pharmaceutical composition comprising a vitamin D derivative or analogue as the active ingredient dissolved in a three-component surfactant-solvent mixture is useful in the treatment of dermal disorders or conditions.Type: ApplicationFiled: December 22, 2010Publication date: December 20, 2012Applicant: LEO PHARMA A/SInventor: Karsten Petersson
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Publication number: 20120322775Abstract: 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: ApplicationFiled: June 13, 2012Publication date: December 20, 2012Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATIONInventors: Hector F. DeLuca, Lori A. Plum, Rafal R. Sicinski, Izabela Sibilska, Margaret Clagett-Dame
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Publication number: 20120322774Abstract: A method for forming chocolate having cholecalciferol is provided. The method includes mixing cholecalciferol into an oil to produce a cholecalciferol-oil mixture. The temperature of a chocolate base is raised to a melting point, and the cholecalciferol-oil mixture is blended into the chocolate base to form a cholecalciferol-chocolate.Type: ApplicationFiled: December 27, 2011Publication date: December 20, 2012Applicant: ENTERAL HEALTH AND NUTRITION, LLCInventors: Dustin Garth James, Helen Kim-James
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Patent number: 8329678Abstract: Azadirachta indica cell suspension culture was used for the biotransformation of dianabol to yield a metabolite 17?-hydroxy-17?-methyl-5?-androstan-3-one, which can also be synthesized, as a potent antiinflammatory agent.Type: GrantFiled: July 17, 2011Date of Patent: December 11, 2012Inventors: Saif Ullah, Saifullah Khan, Muhammed Ahmed Mesaik, Zaheerul Haq, Almas Jabeen, Sobia Ahsan Halim, Muhammad Iqbal Choudhary
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Patent number: 8329677Abstract: The a method of treating elevated blood levels of iPTH by increasing or maintaining blood concentrations of both 25-hydroxyvitamin D and 1,25-dihydroxyvitamin D in a patient by administering, as necessary, both Vitamin D repletion and Vitamin D hormone replacement therapies, is disclosed. The blood concentrations of 25-hydroxyvitamin D are increased to and maintained at or above 30 ng/mL, and blood concentrations of 1,25-dihydroxyvitamin D are increased to or maintained within a patient's normal historical physiological range for 1,25-dihydroxyvitamin D without causing substantially increased risk of hypercalcemia, hyperphosphatemia or over suppression of plasma iPTH in the patient. The blood levels of 25-hydroxyvitamin D are maintained at or above 30 ng/mL between doses of Vitamin D repletion therapies, and the blood levels of 1,25-dihydroxyvitamin D are maintained in the patient's normal historical physiological range between doses of Vitamin D hormone replacement therapies.Type: GrantFiled: June 21, 2007Date of Patent: December 11, 2012Assignees: Cytochroma, Inc., Proventiv Therapeutics, LLCInventors: Charles W. Bishop, Keith H. Crawford, Eric J. Messner, Martin P. Petkovich, Christian F. Helvig
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Publication number: 20120309719Abstract: Cyclopropane-containing vitamin D analogs of formulas I and IV are provided. Such compounds may be used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.Type: ApplicationFiled: May 31, 2012Publication date: December 6, 2012Inventors: Hector DeLuca, Rafal Barycki, Lori Plum, Margaret Clagett-Dame
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Publication number: 20120309713Abstract: 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: ApplicationFiled: May 16, 2012Publication date: December 6, 2012Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATIONInventors: DeLuca F. Hector, Clagett-Dame Margaret, Plum A. Lori, Chiellini Grazia
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Patent number: 8324191Abstract: The present invention relates to oral nutritional and therapeutic products which are useful for providing vitamins and minerals required for bone health. The present invention is an oral nutritional and therapeutic composition of calcium succinate, magnesium R-(+)-alpha-lipoate, and Vitamin D for use in the maintenance of bone health, the optimization of bone growth, reducing the risk of bone fracture, and the prevention and treatment of osteoporosis. The pharmaceutical products and methods of the present invention are particularly useful in building bone mass, quality, and density during growth, maintaining bone mass, quality, and density over time, reducing bone fracture risk, and treating osteoporosis in men and women.Type: GrantFiled: July 11, 2008Date of Patent: December 4, 2012Assignee: Biolink Life Sciences, IncInventors: Deanna Jean Nelson, Walter C. Holberg, III
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Patent number: 8318708Abstract: This application relates to methods of treating and ameliorating fibrosis, such as fibrosis of the pancreas. In particular, the application relates to methods of using a vitamin D receptor agonist (such as vitamin D, vitamin D analogs, vitamin D precursors, and vitamin D receptor agonists precursors) for the treatment of pancreatic fibrosis.Type: GrantFiled: May 3, 2010Date of Patent: November 27, 2012Assignees: Salk Institute for Biological Studies, University of SydneyInventors: Ronald M. Evans, Michael Downes, Christopher Liddle, Nanthakumar Subramaniam, Caroline Flora Samer
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Publication number: 20120289474Abstract: The compounds of Formula (1), in which A, R1, R2, R3 and R5 have the meanings as given in the description, are novel effective inhibitors of type 4 and 5 phosphodiesterase.Type: ApplicationFiled: December 15, 2010Publication date: November 15, 2012Applicant: NYCOMED GMBHInventors: Dieter Flockerzi, Thomas Stengel, Alexander Mann, Harald Ohmer, Ulrich Kautz, Steffen Weinbrenner, Stefan Fischer, Christof Zitt, Armin Hatzelmann, Torsten Dunkern, Christian Hesslinger, Thomas Maier, Hermann Tenor, Clemens Braun, Raimund Külzer, Degenhard Marx
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Publication number: 20120288533Abstract: The present invention provides protein (or peptide)-polysaccharide (or oligosaccharide) conjugates (PPC) as nanocapsular vehicles for nanoencapsulation of biologically active compounds, particularly nutraceuticals. The PPCs efficiently protect both hydrophobic (i.e., water insoluble) and hydrophilic (i.e., water soluble) nutraceuticals, to provide a composition which, when added to a beverage, disperses so as to provide a clear or transparent solution. In some embodiments, the PPCs are Maillard reaction based PPCs. Advantageously, the conjugates of the present invention protect the nutraceuticals from degradation, both during shelf life and upon gastric digestion.Type: ApplicationFiled: March 1, 2012Publication date: November 15, 2012Applicant: Technion Research and Development Foundation Ltd.Inventor: Yoav D. Livney
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Publication number: 20120283227Abstract: 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: ApplicationFiled: April 19, 2012Publication date: November 8, 2012Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATIONInventors: Hector F. DeLuca, Margaret Clagett-Dame, Lori A. Plum, Rafal Barycki
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Publication number: 20120283228Abstract: 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: ApplicationFiled: May 3, 2012Publication date: November 8, 2012Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATIONInventors: Hector F. DeLuca, Margaret Clagett-Dame, Pawel Grzywacz, Grazia Chiellini, Lori A. Plum