Polycyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 514/453)
  • Publication number: 20110034486
    Abstract: The invention relates to a cosmetic, dermatological or pharmaceutical preparation, containing one, two or more compounds of formula (I) and/or a pharmaceutically acceptable salt of a compound of this type, (i) for use in a method for preventing, treating or reducing cellulite, and/or (ii) in an adequate quantity to reduce the lipid quantity contained in subcutaneous fat tissue, and/or to inhibit the differentiation of preadipocytes, and/or to inhibit the lipogenesis in adipocytes, wherein the radicals R1 to R8, independently of one another, signify hydrogen, hydroxy or C1-C4-alkoxy, and/or two adjacent radicals together form a methylenedioxy group.
    Type: Application
    Filed: August 3, 2010
    Publication date: February 10, 2011
    Applicant: SYMRISE GmbH & Co., KG
    Inventors: Imke Meyer, Oskar Koch, Nadine Hillebrand, Martina Herrmann, Holger Joppe
  • Publication number: 20110027230
    Abstract: Oral compositions comprising an association of one or of a mixture of phytoestrogens, selective for the estrogen receptor-?, with dietary fibres are described. The compositions thereof can be profitably used for the prophylactic and therapeutic treatment in mammals, including humans, of health conditions characterised by a high risk of onset and recurrence of intestinal adenomas (adenopolyposis coli), and of adenoma's progression to colorectal carcinoma. In presence of pre-cancerous lesions in the colon, characterised by mutations of the APC tumor suppressor and defined as polyps or adenomas, the oral compositions disclosed can be in fact profitably used to reduce the number and volume of polyps, and to prevent their progression to neoplastic transformation, reducing their degree of dysplasia.
    Type: Application
    Filed: February 20, 2009
    Publication date: February 3, 2011
    Inventors: Alfredo Di Leo, Michele Barone
  • Publication number: 20110028416
    Abstract: Compositions and methods for maintenance of bone health or prevention, alleviation and/or treatment of bone disorders are presented. The present invention also provides the manufacture of a nutritional product, a supplement or a medicament for promoting bone growth or for the maintenance of bone health and methods regarding same. In an embodiment, the present invention provides a composition comprising an active ingredient having an effective amount of a plant or plant extract containing at least one phytochemical having the ability to induce bone morphogenic protein expression.
    Type: Application
    Filed: February 25, 2008
    Publication date: February 3, 2011
    Applicant: NESTEC S.A.
    Inventors: Elizabeth Offord Cavin, Gary Williamson, Didier Courtois, Bernard Lemaure, Andre Touche, Grace Ing Soon, Laurent Ameye
  • Publication number: 20110021615
    Abstract: The present invention relates to a method of treating plant(s) against larval pests by the use of terreulactone. It also relates to a process for producing meroterpenoid from fungus Aspergillus terreus strain MTCC5390.
    Type: Application
    Filed: March 3, 2009
    Publication date: January 27, 2011
    Applicant: INDIAN INSTITUTE OF SCIENCE
    Inventors: Ram Rajasekharan, Vivek Babu Shivegowda, Dodaghatta Krishnarao Venkata Rao
  • Publication number: 20110021613
    Abstract: Compounds obtainable from plants, e.g. of the genus Eucalyptus, or from microorganisms are shown to be useful as CNS activity modulators useful e.g. in the treatment of depression, for lifting mood and/or for increasing behavioural initiative and the like. This use and related aspects form embodiments of the invention. Also compounds as such are presented. The compounds useful are acylphloroglucine derivatives of the formula I, wherein the substituents are as defined in the description.
    Type: Application
    Filed: December 11, 2007
    Publication date: January 27, 2011
    Applicant: INTERMED DISCOVERY GMBH
    Inventors: Ernst Roemer, Torsten Grothe
  • Patent number: 7875607
    Abstract: 7,8-Bicyclic-chroman derivatives of Formula I: wherein the substituents are defined as in the specification or the pharmaceutically acceptable salts thereof, are disclosed. They are useful for the treatment of inflammatory disorders, neurodegenerative disorders and/or mitochondrial disorders. They are also useful in the manufacture of pharmaceutical formulations for the treatment of such conditions.
    Type: Grant
    Filed: November 24, 2008
    Date of Patent: January 25, 2011
    Assignee: Ampere Life Sciences, Inc.
    Inventors: Bing Wang, Gail Walkinshaw
  • Publication number: 20110009372
    Abstract: The invention provides compositions comprising formula 1 steroids, e.g., 16?-bromo-3?-hydroxy-5?-androstan-17-one hemihydrate and one or more excipients, including compositions that comprise a liquid formulation comprising less than about 3% v/v water. The compositions are useful to make improved pharmaceutical formulations. The invention also provides methods of intermittent dosing of steroid compounds such as analogs of 16?-bromo-3?-hydroxy-5?-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using the compounds. The invention also provides methods to make and use these immunomodulatory compositions and formulations.
    Type: Application
    Filed: September 30, 2009
    Publication date: January 13, 2011
    Inventor: James M. Frincke
  • Patent number: 7868040
    Abstract: The present invention relates to synergistic combinations of the compound 5,6-dimethylxanthenone-4-acetic acid (DMXAA) and an alkylating agent, which has anti-tumour activity. Preferably, the present invention relates to synergistic combinations of the compound 5,6-dimethylxanthenone-4-acetic acid (DMXAA) and cyclophosphamide. More particularly, the invention is concerned with the use of such combinations in the treatment of cancer and pharmaceutical compositions containing such combinations. The invention further provides for methods of preparing the combinations of the invention.
    Type: Grant
    Filed: July 30, 2007
    Date of Patent: January 11, 2011
    Assignee: Cancer Research Technology Limited
    Inventors: William R. Wilson, Bronwyn G. Siim
  • Patent number: 7868039
    Abstract: The present invention relates to synergistic combinations of the compound 5,6-dimethylxanthenone-4-acetic acid (DMXAA) and vinca alkaloids, which have anti-tumour activity. Preferably, the present invention relates to synergistic combinations of the compound 5,6-dimethylxanthenone-4-acetic acid (DMXAA) and vincristine. More particularly, the invention is concerned with the use of such combinations in the treatment of cancer and pharmaceutical compositions containing such combinations. The invention further provides for methods of preparing the combinations of the invention.
    Type: Grant
    Filed: July 30, 2007
    Date of Patent: January 11, 2011
    Assignee: Cancer Research Technology Limited
    Inventors: William R. Wilson, Bronwyn G. Siim
  • Publication number: 20110003887
    Abstract: Oncogenic Ras-driven cancer is treated with agent by interrupting pathway comprising activation of Akt by oncogenic Ras, activated Akt causing phosphorylation of eNOS at S1177 site of eNOS to provide activated eNOS in cancer cells and activated eNOS causing activation of wildtype Ras by nitrosylation thereof at C118 to provide GTP-bound activated wildtype H and N Ras. L-NAME can be orally administered to interrupt this pathway. Wortmannin can be administered intravenously to interrupt this pathway. Novel siRNAs are disclosed useful to interrupt said pathway.
    Type: Application
    Filed: January 9, 2009
    Publication date: January 6, 2011
    Applicant: Duke University
    Inventors: Christopher M. Counter, Kian-Huat Lim, Brooke Ancrile, David F Kashatus
  • Publication number: 20110002995
    Abstract: Provided is a pharmaceutical composition for the treatment and prevention of cardiac diseases, containing (a) a therapeutically effective amount of a compound represented by Formula 1 or 2 or a pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, and (b) a pharmaceutically acceptable carrier, diluent or excipient or any combination thereof.
    Type: Application
    Filed: December 18, 2008
    Publication date: January 6, 2011
    Applicants: MAZENCE INC., KT & G CORPORATION
    Inventors: Taehwan Kwak, Myung-Gyu Park
  • Patent number: 7863320
    Abstract: The present invention relates to synergistic combinations of the compound 5,6-dimethylxanthenone-4-acetic acid (DMXAA) and a platinum compound which has anti-tumour activity. Preferably, the present invention relates to synergistic combinations of the compound 5,6-dimethylxanthenone-4-acetic acid (DMXAA) and carboplatin. More particularly, the invention is concerned with the use of such combinations in the treatment of cancer and pharmaceutical compositions containing such combinations. The invention further provides for methods of preparing the combinations of the invention.
    Type: Grant
    Filed: July 30, 2007
    Date of Patent: January 4, 2011
    Assignee: Cancer Research Technology Limited
    Inventors: William R. Wilson, Bronwyn G. Siim
  • Patent number: 7863321
    Abstract: The present invention relates to synergistic combinations of the compound 5, 6-dimethylxanthenone-4-acetic acid (DMXAA) and a compound selected from anthracyclines and topisomerase II inhibitors, which have anti-tumor activity. Preferably, the present invention relates to synergistic combinations of the compound 5,6-dimethylxanthenone-4-acetic acid (DMXAA) and a compound selected from etoposide, and doxorubicin. More particularly, the invention is concerned with the use of such combinations in the treatment of cancer and pharmaceutical compositions containing such combinations. The invention further provides for methods of preparing the combinations of the invention.
    Type: Grant
    Filed: July 30, 2007
    Date of Patent: January 4, 2011
    Assignee: Cancer Research Technology Limited
    Inventors: William R. Wilson, Bronwyn G. Siim
  • Publication number: 20100331398
    Abstract: Gossypol and apogossypol derivatives of general formula (1), preparation thereof and use thereof.
    Type: Application
    Filed: December 5, 2008
    Publication date: December 30, 2010
    Applicant: UNIVERSITE DU MAINE (LE MANS)
    Inventors: Jacques Mortier, Anne-Sophie Castanet, Nguyet Trang Thanh Chau
  • Publication number: 20100331325
    Abstract: This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.
    Type: Application
    Filed: August 5, 2010
    Publication date: December 30, 2010
    Inventors: José Maria CID-NÚÑEZ, Antonius Adrianus Hendrikus Petrus MEGENS, Andrés Avelino TRABANCO-SUÁREZ, Mohamed KOUKNI, Georges Joseph Cornelius HOORNAERT, Frans Josef Cornelius COMPERNOLLE, Tomasz KOZLECKI, Hua MAO, Sushil Chandra JHA, Francisco Javier FERNÁNDEZ-GADEA
  • Patent number: 7858657
    Abstract: Novel wortmannin analogs and their use in inhibiting PI-3-kinase activity in mammals and the treatment or prevention of cancer and tumor formation in a subject are described herein. Preferably, the wortmannin analogs may be administered with other chemotherapeutic agents in the treatment of cancer.
    Type: Grant
    Filed: September 23, 2008
    Date of Patent: December 28, 2010
    Assignees: Proix Pharmaceutical Corp., Arizona Board of Regents, Acting on Behalf of The University of Arizona, University of Pittsburgh - Of the Commonwealth System of Higher Education
    Inventors: Lynn D. Kirkpatrick, Garth Powis, Peter Wipf
  • Patent number: 7858662
    Abstract: The invention relates to a medicament containing a compound of general formula (1), where R1=independently, a straight or branched, saturated, singly- or multiply-unsaturated, optionally substituted C11-C21 alkyl, alkylene or alkynyl group, preferably a C11-C15 alkyl, alkylene or alkynyl group, particularly a C11-C13 alkyl, alkylene or alkynyl group, most preferably a C13 alkyl group, R2=independently, a straight or branched C1-C8 alkyl, alkylene or alkynyl group, preferably a C1-C6 alkyl, alkylene or alkynyl group, in particular a C2-C4 alkyl, alkylene or alkynyl group, most preferably a C3 alkyl group, a —[CH2—(CH2)m—O]nH group with n=1 to 10, preferably n=1 to 5, m=1 to 5, preferably m=1 to 3, a —CH2—[CH—(OH)]p[CH2—(R3)]— group, where R3=independent H or OH, p=1 to 7, preferably p=1 to 4, a pentose group or a hexose group, as therapeutically active agent, alone or in combination with one or several further pharmaceutical agents as a combination preparation for the treatment of viral skin diseases and/or tu
    Type: Grant
    Filed: November 18, 2002
    Date of Patent: December 28, 2010
    Assignee: MediGene AG
    Inventors: Yunik Chang, Robert Lathrop, Erwin Böhm, Irene Gander-Meisterernst, Regina Greger, Johanna Holldack, Ulrich Moebius
  • Publication number: 20100324067
    Abstract: The present invention relates to tetracyclodipyrano-coumarin compounds of general formula (I), wherein the substituents are defined herein. These compounds exihibit dual biological activities of anti human immunodeficiency virus type 1 (HIV-1) infection and anti-Mycobacterium Tuberculosis (TB) infection.
    Type: Application
    Filed: November 5, 2007
    Publication date: December 23, 2010
    Inventors: Gang Liu, Hai Xue, Tao Ma, Ziwei Chen, Lin Wang
  • Publication number: 20100317727
    Abstract: The present invention refers to rosemary extracts for use as medicament for the treatment of a disorder connected to reduced neurotransmission, as well as to dietary and pharmaceutical compositions containing such rosemary extracts and their uses.
    Type: Application
    Filed: November 22, 2007
    Publication date: December 16, 2010
    Inventors: Antoine De Saizieu, Ann Fowler, Regina Goralczyk, Claus Kilpert, Goede Schueler
  • Publication number: 20100317728
    Abstract: The present invention refers to a sage extract containing a mixture of tricyclic diterpene (derivative)s of the formulae I to III, preferably to a sage extract containing a mixture of tricyclic diterpene (derivative)s of the formulae I to IV, more preferably to a sage extract containing a mixture of tricyclic diterpene (derivative)s of the formulae I to V, for use as medicaments for the treatment of a disorder connected to reduced neurotransmission, as well as to dietary and pharmaceutical compositions and their uses.
    Type: Application
    Filed: November 22, 2007
    Publication date: December 16, 2010
    Inventors: Ann Fowler, Claus Kilpert, Goede Schueler, Christof Wehrli, Adrian Wyss
  • Publication number: 20100311826
    Abstract: The present invention relates to xanthone compounds isolated from the plant Psorospermum molluscum Hochr. (Clusiaceae), a Madagascar plant, which are potent cytotoxic agents.
    Type: Application
    Filed: September 11, 2008
    Publication date: December 9, 2010
    Inventors: John E. Leet, Craig R. Fairchild, Stephen W. Mamber, Xiaohong Liu
  • Publication number: 20100310657
    Abstract: Provided is a pharmaceutical composition for the treatment and prevention of kidney diseases, containing (a) a therapeutically effective amount of a compound represented by Formulae 1 or 2 or a pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, and (b) a pharmaceutically acceptable carrier, diluent or excipient or any combination thereof.
    Type: Application
    Filed: December 18, 2008
    Publication date: December 9, 2010
    Applicants: MAZENCE INC., KT & G CORPORATION
    Inventors: Taehwan Kwak, Myung-Gyu Park, Kyoung Hoon Jung
  • Publication number: 20100298280
    Abstract: The present invention relates to tetranortriterpenoid compounds and pharmaceutical compositions thereof, which are provided for use in the treatment, diagnosis and/or prevention of trinucleotide repeat disorders (like a polyglutamine diseases, e.g Huntingdon's disease), amyloid diseases, neurodegenerative disease, protein misfolding diseases or tumors. The tetranortriterpenoid compounds of the present invention are further provided for the reduction and/or inhibition of the aggregation of amyloidogenic proteins, preferably of polyglutamine proteins (such as huntingtin) as well as for increasing proteasome activity. The present invention furthermore relates to nucleic acids, comprising the nucleotide sequences of two huntingtin fragments, as well as to cells and kits, which are useful in methods for assessing the aggregation of huntingtin and in methods for identifying compounds, which modulate the aggregation of huntingtin.
    Type: Application
    Filed: June 13, 2008
    Publication date: November 25, 2010
    Inventors: Petra Kioschis-Schneider, Mathias Hafner, Manuel Ammer-Schläger, Sandra Ritz, Andreas Holloschi, Erich E. Wanker
  • Publication number: 20100298422
    Abstract: Novel polyspirane compounds used in the treatment of diseases involving parasites that belong to the phylum of apicomplexae, and a method for preparing the same.
    Type: Application
    Filed: October 2, 2008
    Publication date: November 25, 2010
    Applicants: UNIVERSITE JOSEPH FOURIER, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Yung-Sing Wong, Marine Aimee Peuchmaur, Eric Marechal, Cyrille Botte, Henri Joseph Vial, Nadia Saidani
  • Publication number: 20100286141
    Abstract: Methods are provided for the identification, biochemical characterization and therapeutic use of agents which impact PTEN, p53, PI-kinase and AKT mediated cellular signaling.
    Type: Application
    Filed: June 29, 2010
    Publication date: November 11, 2010
    Inventor: Donald L. Durden
  • Publication number: 20100284925
    Abstract: Methods and compositions for activating PLTP gene expression include administering an effective amount of a limonoid.
    Type: Application
    Filed: October 17, 2007
    Publication date: November 11, 2010
    Inventor: Khew-Voon Chin
  • Patent number: 7820713
    Abstract: Disclosed and claimed are cocoa extracts such as polyphenols or procyanidins, methods for preparing such extracts, as well as uses for them, especially as antineoplastic agents and antioxidants. Disclosed and claimed are antineoplastic compositions containing cocoa polyphenols or procyanidins and methods for treating patients employing the compositions. Additionally disclosed and claimed is a kit for treating a patient in need of treatment with an antineoplastic agent containing cocoa polyphenols or procyanidins as well as a lyophilized antineoplastic composition containing cocoa polyphenols or procyanidins. Further, disclosed and claimed is the use of the invention in antioxidant, preservative and topoisomerase-inhibiting compositions and methods.
    Type: Grant
    Filed: May 8, 2007
    Date of Patent: October 26, 2010
    Assignee: Mars, Incorporated
    Inventors: Leo J. Romanczyk, Jr., John F. Hammerstone, Jr., Margaret M. Buck
  • Publication number: 20100267643
    Abstract: Provided herein are compositions and methods for treating diabetes, obesity, and other metabolic diseases, disorders or conditions with chemosensory receptor ligands. Also provided herein are pharmaceutical compositions useful for the methods of the present invention.
    Type: Application
    Filed: April 20, 2010
    Publication date: October 21, 2010
    Applicant: ELCELYX THERAPEUTICS, INC.
    Inventors: Alain BARON, Martin R. BROWN, Christopher R.G. JONES
  • Publication number: 20100255054
    Abstract: Provided is a pharmaceutical composition for the treatment and/or prevention of restenosis including (a) a therapeutically effective amount of a particular compound represented by Formula 1 and 2, or a pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, and (b) a pharmaceutically acceptable carrier, a diluent or an excipient, or any combination thereof.
    Type: Application
    Filed: November 26, 2007
    Publication date: October 7, 2010
    Inventors: Taehwan Kwak, Sang-ku Yoo, Myung-gyu Park
  • Publication number: 20100249205
    Abstract: Novel metabolites of wortmannin and wortmannin analogs and their use in inhibiting PI-3 kinase activity in mammals and the treatment and prevention of cancer or tumor formation in a subject are described herein.
    Type: Application
    Filed: April 1, 2010
    Publication date: September 30, 2010
    Applicant: ARIZONA BOARD OF REGENTS
    Inventor: Garth Powis
  • Publication number: 20100249122
    Abstract: The present invention provides compositions and methods of use thereof to prevent and/or treat pathogenic infection. In particular, the present invention provides the use of kinase inhibitors to inhibit kinases that involve in pathogen-host cell interactions that are associated with or cause pathogenic infections, therefore, to effectively prevent and/or treat pathogenic infections with far less likely to engender resistance as compared to conventional antibiotics and anti-viral drugs. The present invention further provides the use of kinase inhibitors for the treatment of acute pathogenic infections for a short period of time to avoid toxicities that may caused by long term use of these kinase inhibitors.
    Type: Application
    Filed: September 5, 2007
    Publication date: September 30, 2010
    Applicant: Emory University
    Inventor: Daniel Kalman
  • Publication number: 20100239685
    Abstract: Provided is a naphthoquinone-based compound represented by Formula 1 or 2 having therapeutic effect on the treatment and/or prevention of prostate and/or testicle (seminal glands)-related diseases, and to a pharmaceutical composition of intestinal delivery system containing the same.
    Type: Application
    Filed: November 26, 2007
    Publication date: September 23, 2010
    Inventors: Taehwan Kwak, Sang-Ku Yoo, Myung-gyu Park
  • Patent number: 7799785
    Abstract: This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.
    Type: Grant
    Filed: December 6, 2005
    Date of Patent: September 21, 2010
    Assignee: Janssen Pharmaceutica NV
    Inventors: José Maria Cid-Núñez, Antonius Andrianus Hendrikus Petrus Megens, Andrés Avelino Trabanco-Suárez, Mohamed Koukni, Georges Joseph Cornelius Hoornaert, Frans Josef Cornelius Compernolle, Tomasz Kozlecki, Hua Mao, Sushil Chandra Jha, Francisco Javier Fernández-Gadea
  • Publication number: 20100234453
    Abstract: Provided is an oral pharmaceutical composition with improved bioavailability and pharmacokinetic properties of a drug, by increasing a bioabsorption rate and an in vivo retention time of an active ingredient via intestine-targeted formulation of a particular phenanthrenequinone-based compound, or a pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, as an active ingredient.
    Type: Application
    Filed: November 26, 2007
    Publication date: September 16, 2010
    Inventors: In Geun Jo, Sang-Ku Yoo, Myung-gyu Park, Taehwan Kwak
  • Patent number: 7795299
    Abstract: Compounds of Formulas I-II are described, along with methods of using such compounds for the treatment of cancer and pharmaceutical formulations thereof.
    Type: Grant
    Filed: January 16, 2009
    Date of Patent: September 14, 2010
    Assignee: The University of North Carolina at Chapel Hill
    Inventors: Kuo-Hsiung Lee, Xihong Wang, Kenneth F. Bastow, Tian-Shung Wu
  • Publication number: 20100227918
    Abstract: The present invention relates to a novel antimicrobial compound of lactoquinomycin that is highly effective against many antibiotic-resistant gram-positive bacteria; namely, methicillin-resistant and vancomycin-resistance Staphylococcus aureus, vancomycin-resistant Enterococcus faecilis and Mycobacteria. The present invention also relates to a fermentation process of culturing a Streptomyces strain to prepare the antimicrobial compound and its use in killing the antibiotic-resistant bacteria.
    Type: Application
    Filed: April 26, 2007
    Publication date: September 9, 2010
    Applicant: Taro Pharmaceuticals North America, Inc.
    Inventors: Albert Fliss, Arthur Bailey, Avraham Yacobi
  • Publication number: 20100222338
    Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A, B, W, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.
    Type: Application
    Filed: May 13, 2010
    Publication date: September 2, 2010
    Inventors: Wenge Zhong, Stephen Hitchcock, Brian K. Albrecht, Michael D. Bartberger, James Brown, Ryan Brown, Stuart C. Chaffee, Yuan Cheng, Michael Croghan, Russell Graceffa, Scott Harried, Dean Hickman, Daniel Horne, Randall Hungate, Ted Judd, Matthew Kaller, Charles Kreiman, Daniel La, Patricia Lopez, Craig E. Masse, Thomas Nixey, Vinod F. Patel, Lewis Pennington, Matthew Weiss, Qiufen Xue, Bryant Yang, Holger Monenschein, Thomas Nguyen
  • Publication number: 20100222313
    Abstract: The invention provides compositions comprising formula 1 steroids, e.g., 16?-bromo-3?-hydroxy-5?-androstan-17-one hemihydrate and one or more excipients, typically wherein the composition comprises less than about 3% water. The compositions are useful to make improved pharmaceutical formulations. The invention also provides methods of intermittent dosing of steroid compounds such as analogs of 16?-bromo-3?-hydroxy-5?-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen (viral) replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using certain steroids and steroid analogs. The invention also provides methods to make and use these immunomodulatory compositions and formulations.
    Type: Application
    Filed: December 9, 2009
    Publication date: September 2, 2010
    Inventor: James M. Frincke
  • Patent number: 7776908
    Abstract: Novel Wortmannin analogs and their use in inhibiting inhibiting PI-3-kinase activity in mammals as well, as tumor formation in a subject are described herein.
    Type: Grant
    Filed: September 20, 2007
    Date of Patent: August 17, 2010
    Assignees: Arizona Board of Regents, The University of Pittsburgh
    Inventors: Garth Powis, Peter Wipf
  • Patent number: 7776911
    Abstract: A pharmaceutical composition for the treatment of malaria in mammals is disclosed. The composition comprises of a synergistic combination of curcumin and artemisinin.
    Type: Grant
    Filed: November 7, 2005
    Date of Patent: August 17, 2010
    Assignee: Indian Institute of Science
    Inventors: Govindarajan Padmanaban, Pundi Narasimhan Rangarajan, Vathsala Palakkod Govindan, Dalavaikodihalli Nanjiah Nandakumar, Viswanathan Arun Nagaraj
  • Publication number: 20100204204
    Abstract: Co-crystals comprising at least one nutraceutical compound and at least one co-crystal former with or without impurities. These co-crystals may be included in compositions (optionally also including other components such as pharmaceutically acceptable excipients, other nutritional supplements, etc.) having utility as pharmaceuticals, nutraceuticals, nutritional supplements, and foodstuffs.
    Type: Application
    Filed: June 6, 2008
    Publication date: August 12, 2010
    Applicant: UNIVERSITY OF SOUTH FLORIDA
    Inventors: Michael Zaworotko, Heather Clarke, Arora Kapildev, Padmini Kavuru, Roland Douglas Shytle, Twarita Pujari, Lissette Marshall, Tien Teng Ong
  • Publication number: 20100204186
    Abstract: Aromatized A-ring derivatives of tetracycline compounds are described.
    Type: Application
    Filed: April 22, 2010
    Publication date: August 12, 2010
    Applicant: Paratek Pharmaceuticals, Inc.
    Inventor: Mark L. Nelson
  • Patent number: 7763648
    Abstract: The present invention is directed to 7 oxa-estra-4,9-diene-3,17-dione derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by at least one progesterone or glucocorticoid receptor.
    Type: Grant
    Filed: February 16, 2007
    Date of Patent: July 27, 2010
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Fu-An Kang, Nareshkumar F. Jain, Zhihua Sui
  • Publication number: 20100184650
    Abstract: Patients are subject to a post-seizure treatment regime to separately inhibitor consecutive targets of an epileptogenic cascade comprising neurotransmitter receptor signaling, kinase/phosphatase activity, protein translation, and apoptosis or inflammation.
    Type: Application
    Filed: January 17, 2010
    Publication date: July 22, 2010
    Inventors: Frances E. Jensen, Sanjay N. Rakhade
  • Publication number: 20100173860
    Abstract: Compositions of purified and biologically active ellagitannins are provided by separation from pomegranate husk using a method of extraction and purification using a solid polymeric adsorbent and the uses of the said compounds
    Type: Application
    Filed: December 24, 2009
    Publication date: July 8, 2010
    Inventors: Navindra P. Seeram, David Heber
  • Publication number: 20100168219
    Abstract: Neutrophils (PMN) can migrate along gradients of chemoattractants across endothelial monolayers to sites of inflammation and infection. This chemotaxis through endothelial cell borders is involved in several acute and chronic inflammatory diseases, however our understanding of the role of endothelial second messengers in the regulation of leukocyte emigration is still incomplete. We investigated this using an in vitro model of neutrophil migration across human umbilical vein endothelial cells (HUVECs) and human microvascular endothelial cells (HMECs) on cell culture inserts. We report that activation of endothelial protein kinase C (PKC) by both phorbol myristate acetate (PMA) and Bryostatin-1 (a potent PKC? and c activator) can completely abolish neutrophil migration mediated by both endothelial TNF-? stimulation and a leukotriene B4 (LTB4) gradient. PMA protected against LTB4 induced PMN transmigration for at least 24 hours in HMECs and HUVECs.
    Type: Application
    Filed: December 31, 2008
    Publication date: July 1, 2010
    Inventor: Jonathan Steven Alexander
  • Publication number: 20100168160
    Abstract: Genipin derivatives and pharmaceutical compositions thereof that inhibit the activity of uncoupling protein-2 (UCP2) and are useful in treating deficient first-phase insulin secretion, non-insulin dependent diabetes mellitus, and ischemia in a mammal are disclosed.
    Type: Application
    Filed: November 19, 2009
    Publication date: July 1, 2010
    Applicant: Beth Israel Deaconess Medical Center , Inc. And Trustees of Boston University
    Inventors: Chen-Yu Zhang, Bradford B. Lowell, John A. Porco, JR., Ruichao Shen, Cheng T. Lin, Stefan Krauss
  • Publication number: 20100143440
    Abstract: Methods and compositions related to treating or preventing a proliferative disease in a subject comprising administering an inhibitor of a UL97 or a UL97 homolog to the subject are described.
    Type: Application
    Filed: March 4, 2008
    Publication date: June 10, 2010
    Applicant: The UAB Research Foundation
    Inventor: Mark N. Prichard
  • Publication number: 20100137420
    Abstract: Biological markers for multiple sclerosis, and their use in the diagnosis and prognosis of the disease, are described. Also described are methods for treating multiple sclerosis by administering an inhibitor of cathepsin B activity or a neuroprotective composition comprising a modified terpenoid compound. Also described are isolated polypeptide biomarkers, polynucleotides encoding the polypeptide biomarkers, and antibodies that bind specifically to the polypeptide biomarkers. Further described are kits that include the above-mentioned isolated polypeptide biomarkers, the polynucleotides encoding them, or specific antibodies against the polypeptide biomarkers.
    Type: Application
    Filed: September 19, 2007
    Publication date: June 3, 2010
    Inventors: Avindra Nath, Caroline F. Anderson, David Irani, Robert J. Cotter, Joseph P. Steiner, Norman Haughey
  • Publication number: 20100137421
    Abstract: Provided herein are compounds that are inducers of apoptosis activators of caspases and pharmaceutically acceptable derivatives thereof. Also provided are methods of synthesis of the compounds and methods for treatment of diseases in which there is uncontrolled cell growth and spread of abnormal cells, such as cancers, by administering the compounds.
    Type: Application
    Filed: November 8, 2007
    Publication date: June 3, 2010
    Inventors: Emmanuel Theodorakis, Ayse Batova