Patents Examined by Sabiha Qazi
  • Patent number: 8222235
    Abstract: Compounds of formula I are provided where X1 and X2 are independently selected from H or hydroxy protecting groups. Such compounds may be used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.
    Type: Grant
    Filed: November 18, 2005
    Date of Patent: July 17, 2012
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Lori A. Plum, Margaret Clagett-Dame
  • Patent number: 8222236
    Abstract: This invention discloses 2-methylene-(20E)-20(22)-dehydro-19-nor-vitamin D analogs, and specifically 2-methylene-(20E)-20(22)-dehydro-19-nor-1?,25-dihydroxyvitamin D3, and pharmaceutical uses therefore. This compound exhibits relatively high transcription activity as well as pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also shows lower activity in vivo on bone calcium mobilization and similar in vivo intestinal calcium transport activity compared to the native hormone 1?,25-dihydroxyvitamin D3, and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.
    Type: Grant
    Filed: July 10, 2008
    Date of Patent: July 17, 2012
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Bulli Padmaja Tadi, Lori A. Plum, Margaret Clagett-Dame
  • Patent number: 8217023
    Abstract: 19-nor-vitamin D analogs having an additional cyclopentene ring connecting carbon 1 and carbon 2, or connecting carbon 3 and carbon-2 of the A-ring of the analog, and pharmaceutical uses therefore, are described. These compounds exhibit selective in vitro activities, making them therapeutic agents for the treatment or prophylaxis of some types of cancers, particularly leukemia, colon cancer, breast cancer, skin cancer or prostate cancer.
    Type: Grant
    Filed: September 30, 2010
    Date of Patent: July 10, 2012
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Agnieszka Glebocka, Lori A. Plum, Margaret Clagett-Dame, Rafal R. Sicinski
  • Patent number: 8198263
    Abstract: 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: Grant
    Filed: September 26, 2006
    Date of Patent: June 12, 2012
    Assignees: Centre National de la Recherche Scientifique, Universite De Strasbourg, Universidad De Santiago De Compostela, Institut National de la Sante Et de la Recherche Medicale
    Inventors: Dino Moras, Antonio Mourino-Mosquera, Luis Cezar Rodrigues, Natacha Rochel, Jean-Marie Wurtz
  • Patent number: 8193169
    Abstract: 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: Grant
    Filed: July 10, 2008
    Date of Patent: June 5, 2012
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Pawel Grzywacz, Lori A. Plum, Margaret Clagett-Dame
  • Patent number: 8193170
    Abstract: 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: Grant
    Filed: July 10, 2008
    Date of Patent: June 5, 2012
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Grazia Chiellini, Pawel Grzywacz, Lori A. Plum, Margaret Clagett-Dame
  • Patent number: 8193171
    Abstract: 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: Grant
    Filed: January 22, 2009
    Date of Patent: June 5, 2012
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Margaret Clagett-Dame, Lori A. Plum, Rafal R. Sicinski, Katarzyna Plonska-Ocypa, Nirca J. Nieves, Pawel Grzywacz
  • Patent number: 8188133
    Abstract: The invention concerns novel imidazole derivatives of general formula (I), wherein Z? and Z represent different variable groups. Said products have an antitumoral activity. The invention also concerns pharmaceutical compositions containing said products and their use for preparing antitumoral medicine.
    Type: Grant
    Filed: April 26, 2007
    Date of Patent: May 29, 2012
    Assignee: Ipsen Pharma S.A.S.
    Inventors: Anne-Marie Liberatore, Dennis Bigg, Dominique Pons, Grégoire Prevost
  • Patent number: 8188064
    Abstract: 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: Grant
    Filed: November 24, 2004
    Date of Patent: May 29, 2012
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Margaret Clagett-Dame, Hector F. DeLuca, Jamie M. Ahrens, James M. Ntambi, Brian Thomson
  • Patent number: 8187575
    Abstract: The present invention relates to new compounds of formula (I), wherein R1, R2, R3, R4, R5, R6, R7, and R8 independently from each other are hydrogen; C1-C18alkyl; C2-C18alkenyl; C5-C7, cycloalkyl; C1-C6alkylene-C5-C7, cycloalkyl; R9 is hydrogen; C1-C18alkyl; C2-C18alkenyl; C5-C7cycloalkyl; C1-C6alkylene-C5-C7cycloalkyl; C6-C10aryl; A is —S—; —O— or —NR10—, wherein R10 has the same meanings as R9; X is COOR11; CONR12R13; SO3, R14; or SO2NR15R16, wherein R11, R12, R13, R14, R15, and R16, have independently from each other the same meanings as R9; to their preparation and to their use as UV absorbers in cosmetic and pharmaceutical formulations.
    Type: Grant
    Filed: January 13, 2004
    Date of Patent: May 29, 2012
    Assignee: BASF SE Ludwigshafen
    Inventors: Thomas Ehlis, Dietmar Hüglin, Elek Borsos
  • Patent number: 8183401
    Abstract: A method is provided for preparing an aromatase inhibitor of formula (I) wherein each of R1, R2, R3, R4, independently, is hydrogen, halogen or C1-C6 alkyl. In one form, the aromatase inhibitor is exemestane wherein each of R1, R2, R3, R4 is hydrogen. In the method, a compound of formula (II) wherein R1, R2, R3, R4 are as defined above and R is alkylene, is reacted with a deprotonating agent and a compound of the formula R5SO2X wherein R5 is C1-C5 alkyl and X is halogen so as to obtain a compound of formula (III) wherein R1, R2, R3, R4, R5 are as defined above. The compound of Formula (III) is then reacted with a base to form an aromatase inhibitor of formula (I).
    Type: Grant
    Filed: January 14, 2005
    Date of Patent: May 22, 2012
    Assignee: Cedarburg Pharmaceuticals, Inc.
    Inventors: Kevin Kunnen, Nathan W. Stehle, Scot W. Weis, John M. Pascone, Richard J Pariza, Scott G. Van Ornum, Paul Zizelman
  • Patent number: 8178517
    Abstract: 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: Grant
    Filed: September 30, 2010
    Date of Patent: May 15, 2012
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Katarzyna Sokolowska, Lori A. Plum, Margaret Clagett-Dame, Rafal R. Sicinski, Antonio Mouriño
  • Patent number: 8168619
    Abstract: A method of preventing estrogen deficiencies and osteoporosis in menopausal women by continuously orally administering without interruption to menopausal women in need thereof an amount of 0.3 to 3 mg of 17?-estradiol or esters thereof and 0.3 to 1.25 mg of nomegestrol or esters thereof in an amount sufficient to prevent said problems.
    Type: Grant
    Filed: October 29, 1999
    Date of Patent: May 1, 2012
    Assignee: Laboratoire Theramex
    Inventors: Jacques Paris, Jean-Louis Thomas
  • Patent number: 8163742
    Abstract: The present invention comprises a new class of compounds capable of modulating the c-kit receptor and, accordingly, useful for treatment of c-kit mediated diseases, including various fibrotic and mast cell related diseases such as mastocytosis. The compounds have a general Formula I wherein R1-6, X and Y are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of c-kit mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.
    Type: Grant
    Filed: July 18, 2007
    Date of Patent: April 24, 2012
    Assignee: Amgen Inc.
    Inventors: Ning Chen, Essa Hu
  • Patent number: 8158558
    Abstract: Herbicide combinations comprising an amount of components (A) and (B) have improved herbicidal action: (A) one or more herbicides of the formula (I) or salts thereof in which R1 is (C1-C8)-alkyl, (C3-C4)-alkenyl, (C3-C4)-alkynyl or (C1-C4)-alkyl which is mono- to tetrasubstituted by radicals selected from the group consisting of halogen and/or (C1-C2)-alkoxy, R2 is I or CH2NHSO2CH3, R3 is methyl or methoxy and Z is N or CH; and (B) denotes one or more herbicides which act selectively in some monocotyledonous crops against monocotyledonous and/or dicotyledonous harmful plants, which herbicides are selected from the group of compounds consisting of (B1) flucarbazone, (B2) BAY MKH 6561 (procarbazone), (B3) florasulam, (B4) halosulfuron, (B5) tritosulfuron, (B6) picolinafen, (B7) cinidon-ethyl, (B8) mesotrione, (B9) metosulam, (B10) clopyralid, (B11) flufenacet, (B12) flumetsulam, (B13) flupoxam, (B14) prosulfocarb, (B15) flurtamone, (B16) aclonifen, (B17) hexazinone, (B18) asulam, (B19) diuron, (B20)
    Type: Grant
    Filed: July 18, 2002
    Date of Patent: April 17, 2012
    Assignee: Bayer CropScience GmbH
    Inventors: Hermann Bieringer, Hans Philipp Huff, Erwin Hacker
  • Patent number: 8158802
    Abstract: This invention provides compounds of Formula 1, their N-oxides and agriculturally suitable salts wherein R1, R2, R3, R4a, R4b and R5 are as defined in the disclosure. Also disclosed are methods for controlling invertebrate pests comprising contacting the invertebrate pests or their environment with a biologically effective amount of a compound of Formula 1 or a composition comprising a compound of Formula 1.
    Type: Grant
    Filed: January 31, 2011
    Date of Patent: April 17, 2012
    Assignee: E.I. du Pont de Nemours and Company
    Inventors: George Philip Lahm, Thomas Paul Selby, Thomas Martin Stevenson
  • Patent number: 8148521
    Abstract: This invention provides compounds of Formula 1, their N-oxides and agriculturally suitable salts wherein R1, R2, R3, R4a, R4b and R5 are as defined in the disclosure. Also disclosed are methods for controlling invertebrate pests comprising contacting the invertebrate pests or their environment with a biologically effective amount of a compound of Formula 1 or a composition comprising a compound of Formula 1.
    Type: Grant
    Filed: January 31, 2011
    Date of Patent: April 3, 2012
    Assignee: E.I. du Pont de Nemours and Company
    Inventors: George Philip Lahm, Thomas Paul Selby, Thomas Martin Stevenson
  • Patent number: 8147821
    Abstract: The present invention provides a means to concentrate, dry and formulate biomaterials such as polysaccharides, gums and related biopolymers, and microorganisms such as cells, spores, and the like from dilute solutions using spent germ and other oil bearing residues. In addition, the spent germ can serve as a carrier for such biomaterials. The sorbed materials are useful in animal feeds.
    Type: Grant
    Filed: February 21, 2003
    Date of Patent: April 3, 2012
    Assignee: Grain Processing Corporation
    Inventor: Serge Johal
  • Patent number: 8143238
    Abstract: Methods of increasing the thickness of the epidermal layer in the skin of a human comprising topically administering a therapeutically effective dose of an active pharmaceutical ingredient comprising a vitamin D analog including 2-methylene-19-nor-20(S)-1?-hydroxy-bishomopregnacalciferol, 19-nor-26,27-dimethylene-20(S)-2-methylene-1?,25-dihydroxyvitamin D3, 2-methylene-19-nor-(24R)-1?,25-dihydroxyvitamin D2, 2-methylene-1?,25-dihydroxy-(17E)-17(20)-dehydro-19-nor-vitamin D3, 2-methylene-(20R,25S)-19,26-dinor-1?,25-dihydroxyvitamin D3, 2-methylene-18,19-dinor-(20S)-1?,25-dihydroxyvitamin D3, 2-methylene-19-nor-1?-hydroxy-pregnacalciferol, 1?-hydroxy-2-methylene-19-nor-homopregnacalciferol, (20R)-1?-hydroxy-2-methylene-19-nor-bishomopregnacalciferol, 2-methylene-(20S)-19-nor-1?-hydroxy-trishomopregnacalciferol, 2-methylene-(20R)-23,23-difluoro-1?-hydroxy-19-nor-bishomopregnacalciferol, 2-methylene-(20S)-23,23-difluoro-1?-hydroxy-19-nor-bishomopregnacalciferol, 2-(3?hydroxypropyl-1?,2?-idene)-19,23,24-trinor-(20
    Type: Grant
    Filed: March 6, 2009
    Date of Patent: March 27, 2012
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Margaret Clagett-Dame, Lori A. Plum, Nirca J. Nieves, Jamie Ahrens
  • Patent number: 8114859
    Abstract: This invention discloses 2-methylene-(20S,25S)-19,27-dinor-(22E)-vitamin D analogs, and specifically 2-methylene-(20S,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: Grant
    Filed: September 25, 2007
    Date of Patent: February 14, 2012
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Margaret Clagett-Dame, Lori A. Plum, Grazia Chiellini, Pawel Grzywacz