Patents Examined by Sabiha N. Qazi
  • Patent number: 7563783
    Abstract: 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: Grant
    Filed: February 10, 2006
    Date of Patent: July 21, 2009
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Lori A. Plum, Margaret Clagett-Dame
  • Patent number: 7553828
    Abstract: The present invention pertains, at least in part, to novel 9-substituted minocycline compounds. These minocycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and minocycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.
    Type: Grant
    Filed: February 24, 2004
    Date of Patent: June 30, 2009
    Assignee: Paratek Pharmaceuticals, Inc.
    Inventors: Mark L. Nelson, Roger Frechette, Mohamed Y. Ismail, Laura Honeyman, Todd Bowser, Beena Bhatia
  • Patent number: 7550487
    Abstract: The invention is concerned with novel pyrrolidine-3,4-dicarboxamide derivatives of formula (I) wherein R1 to R9 and X are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.
    Type: Grant
    Filed: March 9, 2005
    Date of Patent: June 23, 2009
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Lilli Anselm, Katrin Groebke Zbinden, Wolfgang Haap, Jacques Himber, Christoph Martin Stahl, Stefan Thomi
  • Patent number: 7541349
    Abstract: Compounds of formula 1A and 1B 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 disorders.
    Type: Grant
    Filed: June 22, 2007
    Date of Patent: June 2, 2009
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Lori A. Plum, Margaret Clagett-Dame, Grazia Chiellini, Pawel Grzywacz
  • Patent number: 7541348
    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: June 2, 2009
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Lori A. Plum, Margaret Clagett-Dame
  • Patent number: 7538098
    Abstract: 19-nor-vitamin D analogs having an additional heterocyclic ring connecting the 3?-oxygen and carbon-2 or the 1?-oxygen and carbon-2 of the A-ring of the analog, and pharmaceutical uses therefore, are described. These compounds exhibit significant activity in mobilization of bone, making them therapeutic agents for the treatment or prophylaxis of osteoporosis, osteomalacia, osteopenia, renal osteodystrophy and hypoparathyroidism.
    Type: Grant
    Filed: April 6, 2007
    Date of Patent: May 26, 2009
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Rafal R. Sicinski, Agnieszka Glebocka, Lori A. Plum, Margaret Clagett-Dame
  • Patent number: 7534777
    Abstract: Des-C,D 2-methylene-19-norvitamin D3 analogs are provided including compounds of formula 1, in which R1 is a straight or branched chain alkyl or alkylene group having from 8 to 27 carbons and bearing an OY3 group; and Y1, Y2 and Y3 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: August 30, 2006
    Date of Patent: May 19, 2009
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Katarzyna Plonska-Ocypa, Rafal Sicinski, Pawel Grzywacz, Lori A. Plum, Margaret Clagett-Dame
  • Patent number: 7531527
    Abstract: 2-propylidene-19-nor-vitamin D compounds are disclosed as well as pharmaceutical uses for these compounds and methods of synthesizing these compounds. These compounds are characterized by high 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: Grant
    Filed: May 17, 2007
    Date of Patent: May 12, 2009
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Rafal R. Sicinski, Agnieszka Glebocka, Lori A. Plum
  • Patent number: 7528122
    Abstract: 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: Grant
    Filed: January 30, 2007
    Date of Patent: May 5, 2009
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Grazia Chiellini, Pawel Grzywacz, Lori A. Plum, Margaret Clagett-Dame
  • Patent number: 7517911
    Abstract: The present invention relates to ester compounds derived from 3,4,5-trimethoxy phenyl acetate, 3,4,5-trimethoxy cinnamate or 3,4,5-trimethoxy hydrocinnamate that are represented by Formula (I), wherein R1 is CH2—, —CH?CH— or CH2—CH2, R2 is thymyl or carvacryl, to methods for preparing them, and to a whitening cosmetic composition containing the ester compounds. Because the ester compounds of the present invention inhibit the generation of melanin, the cosmetic composition can improve the skin pigmentation and can be used for whitening cosmetics.
    Type: Grant
    Filed: September 23, 2002
    Date of Patent: April 14, 2009
    Assignee: Amorepacific Corporation
    Inventors: Ho-Sik Rho, Jae-Sung Hwang, Hyun-Jung Choi, Hyun-Jung Shin, Bae-Hwan Kim, Eun-Young Lee, Byeong-Gon Lee, Duck-Hee Kim
  • Patent number: 7511030
    Abstract: 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: Grant
    Filed: February 10, 2006
    Date of Patent: March 31, 2009
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Lori A. Plum, Margaret Clagett-Dame
  • Patent number: 7432290
    Abstract: The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH-mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.
    Type: Grant
    Filed: November 24, 2004
    Date of Patent: October 7, 2008
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Dean Stamos, Martin Trudeau, Randy S. Bethiel, Steven M. Ronkin, Michael C. Badia, Jeffrey O. Saunders
  • Patent number: 7432227
    Abstract: 4-Aminopicolinic acids having alkyl or alkenyl substituents in the 6-position and their amine and acid derivatives are potent herbicides demonstrating a broad spectrum of weed control.
    Type: Grant
    Filed: April 2, 2004
    Date of Patent: October 7, 2008
    Assignee: Dow AgroSciences LLC
    Inventors: Terry William Balko, Ann Marie Buysse, Stephen Craig Fields, Nicholas Martin Irvine, William Chi-Leung Lo, Christian Thomas Lowe, John Sanders Richburg, Paul Richard Schmitzer
  • Patent number: 7402688
    Abstract: A novel 2,2-di-substituted 19-norvitamin D derivative. It is a compound represented by the general formula (I) wherein R1 and R2 are the same or different and each represents hydroxy and A represents hydrogen, or an unsubstituted linear or branched alkyl.
    Type: Grant
    Filed: October 10, 2003
    Date of Patent: July 22, 2008
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Sachiko Yamada, Masato Shimizu, Yukiko Miyamoto
  • Patent number: 7371746
    Abstract: The present invention relates to a 1,2,4-thiadiazole compound of the formula (I) represented by the formula (1): wherein R1? represents C3-C7 alkynyl and X represents C4-C7 straight alkylene optionally substituted with one to four of R2?, C4-C7 straight alkenylene optionally substituted with one to four of R2?, ethylene-oxy-ethylene optionally substituted with one to four of R4?, or ethylene-thio-ethylene optionally substituted with one to four of R4?, R2? represents a halogen atom, trifluoromethyl or C1-C4 alkyl, and R4 represents a fluorine atom or C1-C3 alkyl.
    Type: Grant
    Filed: September 27, 2004
    Date of Patent: May 13, 2008
    Assignee: Sumitomo Chemical Company Limited
    Inventors: Hideki Ihara, Daisuke Takaoka, Hajime Mizuno
  • Patent number: 7332482
    Abstract: The use of 1-alpha-fluoro-25-hydroxy-16,23E-diene-26,27-bishomo-20-epi-cholecalciferol, or a pharmaceutically acceptable salt or ester thereof, for the manufacture of a medicament for the prevention and/or treatment of benign prostatic hyperplasia (BPH) and associated symptoms.
    Type: Grant
    Filed: July 29, 2004
    Date of Patent: February 19, 2008
    Assignee: BioXell S.p.A.
    Inventors: Luciano Adorini, Enrico Colli
  • Patent number: 7312179
    Abstract: A fungicidally active compound of formula (I): where X is (X1), (X2) or (X3); Het is a 5- or 6-membered heterocyclic ring containing one to three heteroatoms, each independently selected from oxygen, nitrogen and sulphur, provided that the ring is not 1,2,3-triazole, the ring being substituted by groups R4, R5 and R6; R1 and R2 are each, independently, hydrogen, halo or methyl; R3 is optionally substituted C2-12 alkyl, optionally substituted C2-12 alkenyl, optionally substituted C2-12 alkynyl, optionally substituted C3?12 cycloalkyl, optionally substituted phenyl or optionally substituted heterocyclyl; R4, R5 and R6 are each, independently, selected from hydrogen, halo, cyano, nitro, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy(C1-4)alkylene and C 1-4 haloalkoxy(C1-4)alkylene, provided that at least one of R4, R5 and R6 is not hydrogen; and R7 and R8 are each, independently, hydrogen, halogen, C1-4 alkyl or Clue haloalkyl; the invention also relates to the preparation of these compounds, to novel intermediates use
    Type: Grant
    Filed: October 24, 2003
    Date of Patent: December 25, 2007
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Josef Ehrenfreund, Hans Tobler, Harald Walter
  • Patent number: 7244719
    Abstract: 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: Grant
    Filed: November 18, 2005
    Date of Patent: July 17, 2007
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Lori A. Plum, Pawel K. Grzywacz, Margaret Clagett-Dame
  • Patent number: 7241747
    Abstract: 2-propylidene-19-nor-vitamin D compounds are disclosed as well as pharmaceutical uses for these compounds and methods of synthesizing these compounds. These compounds are characterized by high 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: Grant
    Filed: April 9, 2004
    Date of Patent: July 10, 2007
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Rafal R. Sicinski, Agnieszka Glebocka, Lori A. Plum
  • Patent number: 7241750
    Abstract: 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: Grant
    Filed: November 18, 2005
    Date of Patent: July 10, 2007
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Bulli Padmaja Tadi, Lori A. Plum, Margaret Clagett-Dame