9,10-seco-cyclopentanohydrophenanthrene Ring System Or 9,10-seco Cyclopentanohydrophenanthrene Ring System Having A Bond Between The 3- And 5-positions (e.g., Vitamin D Compounds, Cholecalciferols, Activated 7-dehydrocholesterols, Dihydrotachysterols, 3,5 Cyclovitamin D Compounds, Etc.) Patents (Class 552/653)
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Patent number: 7888339Abstract: This invention discloses 2-methylene-20(21)-dehydro-19-nor-vitamin D analogs, and specifically 2-methylene-20(21)-dehydro-19-nor-1?,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits relatively high transcription activity as well as pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also shows lower activity in vivo on bone calcium mobilization and 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: February 15, 2011Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Bulli Padmaja Tadi, Lori A. Plum, Margaret Clagett-Dame
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Patent number: 7888000Abstract: Salt sensitivity is measured as a function of the urinary 25-OHD binding activity, which may be evaluated by measuring 25-hydroxyvitamin D binding activity using radiolabeled 25-hydroxyvitamin D3. High binding activity is indicative of salt sensitivity and is an important predictor for development of salt-sensitivity related hypertension.Type: GrantFiled: July 11, 2003Date of Patent: February 15, 2011Assignee: Morehouse School of MedicineInventors: Myrtle Thierry-Palmer, Akins Doherty, Keri J. Griffin, Mohamed A. Bayorh
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Patent number: 7888338Abstract: The present invention relates to 7-(2-cyclohexylidene-ethylidene)-spiro[4.5]-decanes, compositions which comprise said 7-(2-cyclohexylidene-ethylidene)-spiro[4.5]-decanes, and methods for treating diseases, illnesses, and the like with said 7-(2-cyclohexylidene-ethylidene)-spiro[4.5]decanes.Type: GrantFiled: December 6, 2005Date of Patent: February 15, 2011Assignees: K.U. Leuven Research & Development, Universiteit GentInventors: Roger Bouillon, Pierre De Clercq, Wim Schepens, Maurits Vandewalle, Annemieke Verstuyf
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Patent number: 7879829Abstract: 19-nor-vitamin D analogs having an additional dihydrofuran ring connecting the 1?-oxygen and carbon-2 of the A-ring of the analog, and pharmaceutical uses therefore, are described. These compounds exhibit selective in vitro and in vivo activities, making them therapeutic agents for the treatment or prophylaxis of autoimmune diseases, some types of cancers, secondary hyperparathyroidism, psoriasis, or other skin diseases.Type: GrantFiled: July 10, 2008Date of Patent: February 1, 2011Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Agnieszka Glebocka, Katarzyna Sokolowska, Rafal R. Sicinski, Lori A. Plum, Margaret Clagett-Dame
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Publication number: 20100273748Abstract: Methods and compositions for modulating gene expression and the innate immune response by 1,25(OH)2 vitamin D3 (1,25D3) are provided. Also provided are methods and compositions for modulating histone acetylation using 1,25(OH)2 vitamin D3 (1,25D3).Type: ApplicationFiled: September 7, 2007Publication date: October 28, 2010Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Richard L. Gallo, Jurgen Schauber, Robert Modlin
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Patent number: 7803789Abstract: Compounds of formula IA or IB are provided where X1, X2 and X3 are independently selected from H or hydroxy protecting groups and R1 is 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; straight and branched chain hydroxy-substituted alkenyl groups having from 2 to 8 carbon atoms. Such compounds are used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.Type: GrantFiled: January 30, 2007Date of Patent: September 28, 2010Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. Deluca, Grazia Chiellini, Pawel Grzywacz, Lori A. Plum, Margaret Clagett-Dame
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Patent number: 7795459Abstract: Paricalcitol, a synthetic vitamin D analog, is purified to a purity greater than 99.7% by crystallization from solution in isopropyl acetate solvent, followed by filtration and vacuum drying. Isopropyl acetate appears to be unique among commonly available and pharmaceutically acceptable solvents in its ability to precipitate paricalcitol in this high purity, essentially free of isomers thereof.Type: GrantFiled: April 28, 2009Date of Patent: September 14, 2010Assignee: Alphora Research Inc.Inventors: Fabio Eduardo Silva e Souza, Ming Pan, Kathleen Da Silva Turcot
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Publication number: 20100217020Abstract: There are provided a novel process for producing [{(5Z,7E)-(1S,3R,20S)-1,3-dihydroxy-9,10-secopregna-5,7,10(19),16-tetraen-20-yl}oxy]-N-(2,2,3,3,3-pentafluoropropyl)acetamide, which process is shown in the following reaction scheme: an intermediate useful for carrying out the process, and a process for producing the intermediate.Type: ApplicationFiled: December 4, 2006Publication date: August 26, 2010Inventors: Kunio Ogasawara, Takashi Emura, Akira Kawase, Koji Takano, Keisuke Yamamoto, Yoshiaki Kato
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Publication number: 20100210569Abstract: The instant invention constitutes an unique subject matter as a whole which has four individual aspects: (1) a class of chiral, non-racemic, synthetic carnitinoid analog carrier molecules which constitute biocompatible transport compounds not found in nature; (2) a subsequently formed, mitochondria-targeting, coupled antioxidant-carrier complex comprising an antioxidant reversibly attached to and releasable from the synthetic carrier molecule; (3) a method for introducing a biologically active antioxidant into the interior of mitochondria of a living cell for subsequent reaction with such reactive oxygen species may then be present; and (4) a system for delivering a biologically active antioxidant to the interior of mitochondria within a living cell.Type: ApplicationFiled: February 12, 2010Publication date: August 19, 2010Inventor: Kosta Steliou
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Publication number: 20100209536Abstract: This invention provides methods of treating and preventing diseases or conditions of the immune system or infectious disease, involving administration of vitamin D and/or one or more antioxidants (e.g., vitamin E and/or zinc).Type: ApplicationFiled: September 24, 2007Publication date: August 19, 2010Applicant: The Brigham and Women's Hospital, Inc.Inventors: Scott T. Weiss, Augusto A. Litonjua, Benjamin Raby
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Patent number: 7763599Abstract: A method of minimizing or reducing the toxicity of a retinoid having a free carboxyl group and the resulting modified retinoids are described. The method comprises the step of esterifying the carboxyl group of the retinoid with a highly sterically hindered compound, which is preferably a secondary or tertiary alcohol. The resulting retinoid esters are rendered much less toxic than the starting or parent retinoid. This process provides a retinoid ester analog of reduced toxicity so that it may be administered orally with minimal side effects and with a much greater therapeutic window. The modified retinoid compounds are useful in the treatment and prophylaxis of all diseases and disorders where retinoid compounds have been shown effective.Type: GrantFiled: April 2, 2008Date of Patent: July 27, 2010Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Margaret Clagett-Dame, Sumithra Gowlugari
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1?-hydroxy-2-(3?-hydroxypropylidene)-19-nor-vitamin D compounds with a 1,1-dimethylpropyl side chain
Patent number: 7763598Abstract: This invention discloses 1?-hydroxy-2-(3?-hydroxypropylidene)-19-nor-vitamin D compounds with a 1,1-dimethylpropyl side chain, 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: GrantFiled: April 6, 2007Date of Patent: July 27, 2010Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Agnieszka Glebocka, Rafal R. Sicinski, Lori A. Plum, Margaret Clagett-Dame -
Patent number: 7741314Abstract: This invention discloses 2-methylene-(20R,25S)-19,27-dinor-(22E)-vitamin D analogs, and specifically 2-methylene-(20R,25S)-19,27-dinor-(22E)-1?,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also has little, if any, calcemic activity and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.Type: GrantFiled: September 25, 2007Date of Patent: June 22, 2010Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Margaret Clagett-Dame, Lori A. Plum, Grazia Chiellini, Pawel Grzywacz
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Patent number: 7741313Abstract: 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: GrantFiled: July 9, 2007Date of Patent: June 22, 2010Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Bulli Padmaja Tadi, Lori A. Plum, Margaret Clagett-Dame
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Publication number: 20100144683Abstract: The present invention concerns a method for generating a human atopic disease-like phenotype, preferably an atopic dermatitis (AD)-like phenotype in a mammal comprising administering to said mammal at least one compound selected in the group comprising the physiologically active vitamin D3 (1?,25(OH)2D3) and agonistic analogs thereof. The present invention also concerns a method for treating and/or preventing an atopic disease in a patient in a patent comprising administrating to said patient an effective amount of at least one vitamin D3 antagonist.Type: ApplicationFiled: July 24, 2007Publication date: June 10, 2010Applicant: ASSOCIATION POUR LA RECHERCHE A L'IGBMC (ARI)Inventors: Pierre Chambon, Daniel Metzger, Mei Li
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Publication number: 20100137262Abstract: The disclosure provides compounds, compositions and methods using these compounds and compositions to stimulate the differentiation of cells and inhibit excessive cell proliferation of certain cells, including cancer cells and skin cells, which may be useful in the treatment of diseases characterized by abnormal cell proliferation and/or cell differentiation such as leukemia, myelofibrosis and psoriasis without the well known effect on calcium metabolism, which gives rise to hypercalcemia.Type: ApplicationFiled: April 18, 2008Publication date: June 3, 2010Inventors: Gary H. Posner, Kimberly S. Petersen, Lindsey C. Hess, Douglas T. Genna, Scott Borella
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Publication number: 20100130454Abstract: A novel useful vitamin D3 derivative which is reduced in influence on systemic calcium metabolism while retaining excellent vitamin D3 activity. The derivative is a 9,10-secopregnane derivative represented by the following general formula [1]. Also provided is a medicinal composition containing the derivative as an active ingredient. In the general formula [1], Y represents (1) a single bond, (2) alkylene (3) alkenylene, or (4) phenylene; R1 and R2 are the same or different and each represents (1) hydrogen, (2) alkyl, or (3) cycloalkyl, or R1 and R2 in combination represent cycloalkyl in cooperation with the adjacent carbon atom; R3 represents hydrogen or methyl; and Z represents (1) hydrogen, (2) hydroxy, or (3) —NR11R12.Type: ApplicationFiled: December 5, 2005Publication date: May 27, 2010Applicant: NIPPON SHINYAKU CO., LTD.Inventors: Hiroki Fujieda, Hironori Otsu, Shoji Yasufuku
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Patent number: 7718637Abstract: This invention discloses (20S)-23,23-difluoro-2-methylene-19-nor-bishomopregnacalciferol-vitamin D analogs, and specifically (20S)-23,23-difluoro-1?-hydroxy-2-methylene-19-nor-bishomopregnacalciferol, 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: December 24, 2008Date of Patent: May 18, 2010Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Margaret Clagett-Dame, Lori A. Plum, Rafal Barycki
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Patent number: 7718638Abstract: This invention discloses (20R)-23,23-difluoro-2-methylene-19-nor-bishomopregnacalciferol-vitamin D analogs, and specifically (20R)-23,23-difluoro-1?-hydroxy-2-methylene-19-nor-bishomopregnacalciferol, 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: December 24, 2008Date of Patent: May 18, 2010Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Margaret Clagett-Dame, Lori A. Plum, Rafal Barycki
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Patent number: 7718636Abstract: This invention provides pharmaceutical uses for 2-methylene-19-nor-20(S)-1?,25-dihydroxyvitamin D3. Administration of this compound increases the life expectancy of human beings, especially elderly human beings. In particular, it increases the survival rate of females lacking estrogen, especially post-menopausal females, and reduces mortality resulting from spontaneous development of malignant tumors in both males and females.Type: GrantFiled: June 21, 2006Date of Patent: May 18, 2010Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Lori A. Plum, Margaret Clagette-Dame
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Patent number: 7713953Abstract: This invention discloses 2-methylene-(22E)-25-(1-methylene-hexyl)-26,27-cyclo-22-dehydro-19-nor-vitamin D analogs, and specifically 2-methylene-(22E)-25-(1-methylene-hexyl)-26,27-cyclo-22-dehydro-19-nor-1?,24(R)-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits relatively high transcription activity as well as pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also shows lower activity in vivo on bone calcium mobilization and 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.Type: GrantFiled: July 10, 2008Date of Patent: May 11, 2010Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Rafal Barycki, Lori A. Plum, Margaret Clagett-Dame
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Patent number: 7713951Abstract: 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: GrantFiled: April 9, 2004Date of Patent: May 11, 2010Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Rafal Barycki, Pawel K. Grzywacz, Lori A. Plum, Rafal R. Sicinski
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Patent number: 7713952Abstract: This invention discloses 2-methylene-19,26,27-trinor-(20S)-vitamin D analogs, and specifically 2-methylene-19,26,27-trinor-(20S)-1?-hydroxyvitamin D3 and pharmaceutical uses therefor. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also has little, if any, calcemic activity and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.Type: GrantFiled: July 9, 2007Date of Patent: May 11, 2010Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Lori A. Plum, Pawel K. Grzywacz, Margaret Clagett-Dame
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Publication number: 20100113378Abstract: Disclosed are compositions and methods used to treat and/or prevent cancer and metabolic diseases, such as psoriasis. In one aspect, the present invention pertains to the use of cross-linking analogs of vitamin D and its metabolites employed for the treatment of prostate cancer.Type: ApplicationFiled: December 23, 2009Publication date: May 6, 2010Inventors: Rahul Ray, Narashima Swamy
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Patent number: 7704982Abstract: This invention discloses 2-methylene-19-nor-17-ene vitamin D analogs, and specifically 2-methylene-19-nor-1?-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: GrantFiled: July 9, 2007Date of Patent: April 27, 2010Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Bulli Padmaja Tadi, Lori A. Plum, Margaret Clagett-Dame
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Patent number: 7704981Abstract: Compounds of formula I are provided where X1, X2 and X3 are independently selected from H or hydroxy protecting groups. Such compounds are used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.Type: GrantFiled: April 6, 2007Date of Patent: April 27, 2010Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Lori A. Plum, Margaret Clagett-Dame, Rafal Barycki
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Publication number: 20100087405Abstract: Use of one or more vitamin D3 compounds chosen from the group 1-?-hydroxy vitamin D3, 25-hydroxy vitamin D3, 1-?-,25-dihydroxy vitamin D3, in combination with one or more magnesium salts to prevent milk fever in animals.Type: ApplicationFiled: September 14, 2007Publication date: April 8, 2010Inventors: Robert Elliott, Gilbert Weber
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Publication number: 20100069339Abstract: There is provided a method of treatment of male sub-fertility by using a vitamin D compound. Compositions and uses are also provided.Type: ApplicationFiled: October 12, 2007Publication date: March 18, 2010Applicant: BIOXELL S.P.A.Inventors: Luciano Adorini, Giuseppe Penna, Enrico Colli
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Publication number: 20100063307Abstract: Paricalcitol, a synthetic vitamin D analog, is purified to a purity greater than 99.7% by crystallization from solution in isopropyl acetate solvent, followed by filtration and vacuum drying. Isopropyl acetate appears to be unique among commonly available and pharmaceutically acceptable solvents in its ability to precipitate paricalcitol in this high purity, essentially free of isomers thereof. In addition, paricalcitol of purity of at least 99.9% has been shown to have exceptional storage stability.Type: ApplicationFiled: August 19, 2009Publication date: March 11, 2010Applicant: ALPHORA RESEARCH INC.Inventors: Fabio Eduardo Silva e SOUZA, Ming PAN, Kathleen Da Silva TURCOT
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Publication number: 20100041631Abstract: The present invention relates to the treatment of tuberculosis (mycobacterial infections) by the use of KshAB complex inhibitors, or a KstD molecule, or a HsaAB complex, or a HsaC molecule, or a HsaD molecule. The application also includes a method for identifying an inhibitor or modulator of the previously mentioned molecules and complexes.Type: ApplicationFiled: April 17, 2007Publication date: February 18, 2010Applicants: THE UNIVERSITY OF BRITISH COLUMBIA, QUEEN'S UNIVERSITY AT KINGSTONInventors: Lindsay D. Eltis, Victor A. Snieckus
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Publication number: 20100036140Abstract: The invention provides sterols modified by polyethylene glycol represented by the following formula, the preparation and the use thereof, wherein each symbol is defined as in the description.Type: ApplicationFiled: December 13, 2007Publication date: February 11, 2010Inventor: Wenfang Zhang
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Publication number: 20100016263Abstract: A main object of the invention is to provide a novel useful vitamin D3 derivative, which has an excellent vitamin D3 activity and, as compared with conventional vitamin D3 derivatives, has a relatively small amount of influence on the systemic calcium metabolism. The invention includes a 9,10-secopregnane derivative of the following general formula [1] and a pharmaceutical composition containing it as active ingredient. In the general formula [1], the following partial structure between the 16-position and the 17-position means a single bond or a double bond: Y is a single bond, an alkylene, an alkenylene or phenylene; R1 and R2 are the same or different, each represents hydrogen, an alkyl or a cycloalkyl; or R1 and R2, taken together with the adjacent carbon atom, form a cycloalkyl; R3 is hydrogen or methyl; Z is hydrogen, hydroxy or —NR11R12.Type: ApplicationFiled: June 1, 2007Publication date: January 21, 2010Applicant: NIPPON SHINYAKU CO., LTD.Inventors: Hiroki Fujieda, Hironori Otsu, Shoji Yasufuku, Masaaki Shirai
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Patent number: 7648974Abstract: 19-nor-vitamin D analogs having an additional dihydrofuran ring connecting the 3?-oxygen and carbon-2 of the A-ring of the analog, and pharmaceutical uses therefore, are described. These compounds exhibit selective in vitro and in vivo activities, making them therapeutic agents for the treatment or prophylaxis of autoimmune diseases, some types of cancers, metabolic bone diseases, osteomalacia, osteopenia, secondary hyperparathyroidism, psoriasis, or other skin diseases.Type: GrantFiled: July 10, 2008Date of Patent: January 19, 2010Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Agnieszka Glebocka, Katarzyna Sokolowska, Rafal R. Sicinski, Lori A. Plum, Margaret Clagett-Dame
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Patent number: 7648973Abstract: Compounds of formula I are provided where X1, X2 and X3 are independently selected from H or hydroxy protecting groups. Such compounds are used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.Type: GrantFiled: April 6, 2007Date of Patent: January 19, 2010Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Lori A. Plum, Margaret Clagett-Dame, Rafal Barycki
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Patent number: 7648972Abstract: Compounds of formula I are provided where X1 and X2 are independently selected from H or hydroxy protecting groups. Such compounds are used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.Type: GrantFiled: April 6, 2007Date of Patent: January 19, 2010Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Lori A. Plum, Margaret Clagett-Dame, Rafal Barycki
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Publication number: 20100009942Abstract: This invention discloses 2-methylene-(17Z)-17(20)-dehydro-19,21-dinor-vitamin D analogs, and specifically 2-methylene-(17Z)-17(20)-dehydro-19,21-dinor-1?, 25-dihydroxyvitamin 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 has significant calcemic activity in vivo having about the same bone calcium mobilization activity and intestinal calcium transport activity as 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: ApplicationFiled: July 10, 2008Publication date: January 14, 2010Inventors: Hector F. DeLuca, Bulli Padmaja Tadi, Lori A. Plum, Margaret Clagett-Dame
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Publication number: 20100009946Abstract: 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: ApplicationFiled: July 10, 2008Publication date: January 14, 2010Inventors: Hector F. DeLuca, Grazia Chiellini, Pawel Grzywacz, Lori A. Plum, Margaret Clagett-Dame
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Publication number: 20100009941Abstract: This invention discloses 2-methylene-20(21)-dehydro-19-nor-vitamin D analogs, and specifically 2-methylene-20(21)-dehydro-19-nor-1?,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits relatively high transcription activity as well as pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also shows lower activity in vivo on bone calcium mobilization and similar in vivo intestinal calcium transport activity compared to the native hormone 1?a,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: ApplicationFiled: July 10, 2008Publication date: January 14, 2010Inventors: Hector F. DeLuca, Bulli Padmaja Tadi, Lori A. Plum, Margaret Clagett-Dame
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Publication number: 20100009940Abstract: 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 therefor. This compound exhibits relatively high transcription activity as well as pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also shows lower activity in vivo on bone calcium mobilization and 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: ApplicationFiled: July 10, 2008Publication date: January 14, 2010Inventors: Hector F. DeLuca, Bulli Padmaja Tadi, Lori A. Plum, Margaret Clagett-Dame
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Publication number: 20100009947Abstract: 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: ApplicationFiled: July 10, 2008Publication date: January 14, 2010Inventors: Hector F. DeLuca, Grazia Chiellini, Pawel Grzywacz, Lori A. Plum, Margaret Clagett-Dame
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Publication number: 20100009943Abstract: This invention discloses 2-methylene-(22E)-25-(1-methylene-hexyl)-26,27-cyclo-22-dehydro-19-nor-vitamin D analogs, and specifically 2-methylene-(22E)-25-(1-methylene-hexyl)-26,27-cyclo-22-dehydro-19-nor-1?,24(R)-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits relatively high transcription activity as well as pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also shows lower activity in vivo on bone calcium mobilization and 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.Type: ApplicationFiled: July 10, 2008Publication date: January 14, 2010Inventors: Hector F. DeLuca, Rafal Barycki, Lori A. Plum, Margaret Clagett-Dame
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Publication number: 20090318722Abstract: The present invention relates to a compound and a novel process for the preparation of Paricalcitol intermediates.Type: ApplicationFiled: June 20, 2008Publication date: December 24, 2009Applicant: FORMOSA LABORATORIES INC.Inventors: Chze-Siong Ng, Ching-Peng Wei
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Publication number: 20090311316Abstract: Methods and compositions for treating 25-hydroxyvitamin D insufficiency and deficiency in a patient are described herein. The method includes orally administering to the patient a delayed, sustained release formulation including a first ingredient selected from the group consisting of 25-hydroxyvitamin D2, 25-hydroxyvitamin D3, or a combination of 25-hydroxyvitamin D2 and 25-hydroxyvitamin D3, or it includes gradually administering to the patient a sterile intravenous formulation including a first ingredient selected from the group consisting of 25-hydroxyvitamin D2, 25-hydroxyvitamin D3, or a combination of 25-hydroxyvitamin D2 and 25-hydroxyvitamin D3.Type: ApplicationFiled: February 2, 2007Publication date: December 17, 2009Applicant: PROVENTIV THEREAPEUTICS, LLCInventors: Charles W. Bishop, Keith H. Crawford, Eric J. Messner
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Publication number: 20090298800Abstract: The invention provides vitamin D3 analogs of cholecalciferol, substituted at carbons-26 and 27 with deuterated alkyl groups, e.g., trideuteromethyl, wherein carbon-16 is a single or double bond, and carbon-23 is a single, double, or triple bond. The invention provides pharmaceutically acceptable esters, salts, and prodrugs thereof. Methods for using the compounds to treat vitamin D3 associated states, and pharmaceutical compositions containing the compounds are also disclosed.Type: ApplicationFiled: September 21, 2006Publication date: December 3, 2009Applicant: BioXell S.p.A.Inventors: Milan R. Uskokovic, Stanislaw Marczak, Pawel Jankowski, Luciano Adorini
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Publication number: 20090281340Abstract: Disclosed are 1?-hydroxy-2-(3?-hydroxypropylidene)-19-nor-vitamin D compounds, pharmaceutical compositions, and methods of making and treatment thereof. The compounds are generally directed to biologically active 2-alkylidene-19-nor-vitamin D compounds and analogs thereof characterized by the presence of a 3?-hydroxypropylidene moiety at C-2 and the presence of an abbreviated alkyl side-chain free of any hydroxyl moiety.Type: ApplicationFiled: May 8, 2009Publication date: November 12, 2009Inventors: Hector F. DeLuca, Rafal R. Sicinski, Lori A. Plum, Margaret Clagett-Dame, Agnieszka Glebocka
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Publication number: 20090275768Abstract: This invention relates to a method for purifying Paricalcitol by reverse phase chromatography. This invention also relates to a purified Paricalcitol prepared by said method. This invention further relates to a method for purifying Paricalcitol by crystallization.Type: ApplicationFiled: April 30, 2008Publication date: November 5, 2009Applicant: FORMOSA LABORATORIES, INC.Inventors: Chze-Siong Ng, Ching-Peng Wei
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Publication number: 20090233889Abstract: A stabilized 1,25-dihydroxyvitamin D2 composition which is particularly well suited for pharmaceutical formulations, pharmaceutical formulations of the 1,25-dihydroxyvitamin D2 composition, and a method of making the purified composition by purifying a crude 1,25-dihydroxyvitamin D2 from acetone/water, are disclosed.Type: ApplicationFiled: March 12, 2009Publication date: September 17, 2009Inventor: Uttam Saha
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Patent number: 7563783Abstract: 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: GrantFiled: February 10, 2006Date of Patent: July 21, 2009Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Lori A. Plum, Margaret Clagett-Dame
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Patent number: RE41474Abstract: This invention discloses (20S)-1?-hydroxy-2-methylene-19-nor-bishomopregnacalciferol 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 immune disorders in humans as well as renal osteodystrophy.Type: GrantFiled: May 6, 2008Date of Patent: August 3, 2010Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Lori A. Plum, Margaret Clagett-Dame
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Patent number: RE41491Abstract: This invention discloses (20S)-1?-hydroxy-2-methylene-19-nor-bishomopregnacalciferol 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 immune disorders in humans as well as renal osteodystrophy.Type: GrantFiled: May 6, 2008Date of Patent: August 10, 2010Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Lori A. Plum, Margaret Clagett-Dame