The Hetero Ring Is Three-membered Patents (Class 514/475)
  • Patent number: 8106075
    Abstract: Compounds of formula I wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula I can be used as agrochemical active ingredients and can be prepared in a manner known per se.
    Type: Grant
    Filed: October 10, 2005
    Date of Patent: January 31, 2012
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Anthony Cornelius O'Sullivan, David John Hughes, André Jeanguenat, Michel Muehlebach, Olivier Loiseleur
  • Publication number: 20120004162
    Abstract: The disclosure herein generally relates to methods of treating an over eight or obese condition, and overweight- or obesity-related conditions. In one embodiment, the disclosure provides a method of treating an overweight or obese condition involving administering to the subject in need thereof, an amount of a pharmaceutical composition including a MctAP-2 inhibitory compound, or a salt, ester, or prodrug thereof, effective to result in weight loss in the subject.
    Type: Application
    Filed: December 4, 2009
    Publication date: January 5, 2012
    Inventor: James E. Vath
  • Publication number: 20120004299
    Abstract: This invention relates to azeotrope-like compositions, methods and systems having utility in numerous applications, and in particular, uses for azeotrope-like compositions comprising effective amounts of the compound cis-1,1,1,4,4,4-hexafluoro-2-butene (Z-HFO-1336mzzm), which has the following structure: and another material selected from the group consisting of water, fluoroketones, alcohols, hydrochlorofluoroolefins, and combinations of two or more thereof. These compositions may be used in a wide variety of applications such as, blowing agents, refrigerants, heating agents, power cycle agents, cleaning agents, aerosol propellants, sterilization agents, lubricants, flavor and fragrance extractants, flammability reducing agents, and flame suppression agents.
    Type: Application
    Filed: December 14, 2010
    Publication date: January 5, 2012
    Applicant: Honeywell International Inc.
    Inventors: Ryan Hulse, Rajiv Ratna Singh, Martin R. Paonessa, Hang T. Pham, Mary Bogdan, Cliff Gittere, Martin Cheney, Linda L. Cheney
  • Patent number: 8080576
    Abstract: One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.
    Type: Grant
    Filed: February 19, 2010
    Date of Patent: December 20, 2011
    Assignee: Onyx Therapeutics, Inc.
    Inventors: Kevin D. Shenk, Francesco Parlati, Han-Jie Zhou, Catherine Sylvain, Mark S. Smyth, Mark K. Bennett, Guy J. Laidig
  • Patent number: 8075908
    Abstract: A method for inhibiting formation of adhesions following abdominal surgery which involves application of an anti-static fatty acid ethoxylated amide (Cocamide DEA) in a matrix that is placed in the peritoneal cavity at the conclusion of an abdominal surgery and which releases this anti-adhesive chemical over a predetermined time in a range from about five to seven days. Tests conducted on laboratory rats established that the method reduced the incidences of adhesions from 100 percent (100%) in a test model to near zero percent (0%) in the treated animals. In an alternative embodiment, Andrographalide was delivered through a drug pump with similar results. In still another embodiment, an effective amount of Rapamune was delivered, via a pump, into the abdominal cavity, again with similar results.
    Type: Grant
    Filed: July 15, 2008
    Date of Patent: December 13, 2011
    Assignee: Anhese LLC
    Inventor: John P. Delaney
  • Patent number: 8071645
    Abstract: Systems and methods for treating inflammatory and proliferative diseases, and wounds, using as a pharmacon a fatty acid metabolism inhibitor, a glycolytic inhibitor, and/or an agent able to alter cellular production of reactive oxygen, or combination thereof, optionally in combination with one or more chemotherpeutic agents. In preferred embodiments, the invention combines an oxirane carboxylic acid, represented by etomoxir, with a 2-deoxyglucose compound, represented by 2-deoxy-D-glucose, and/or an antibody against UCP and/or Fas antigen. The systems and methods of the invention can be used to treat drug-resistant or multi-drug resistant cancers.
    Type: Grant
    Filed: June 11, 2004
    Date of Patent: December 6, 2011
    Assignee: The Regents of the University of Colorado
    Inventors: M. Karen Newell, Evan Newell, Elizabeth Villalobos-Menuey
  • Publication number: 20110288168
    Abstract: Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, such as, for example, a hydroxamic acid group or a carboxylic acid group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, genetic disorders, e.g. Huntington's disease and spinal muscular atrophy and genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy.
    Type: Application
    Filed: November 29, 2010
    Publication date: November 24, 2011
    Inventors: Hsuan-Yin Lan-Hargest, Robert J. Kaufman, Norbert L. Wiech
  • Publication number: 20110281883
    Abstract: The present invention relates to the use of compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, R7, r, Y and G have the meanings given above as insecticides and/or acaricides and/or fungicides.
    Type: Application
    Filed: January 14, 2010
    Publication date: November 17, 2011
    Applicant: Bayer Cropscience AG
    Inventors: Reiner Fischer, Stefan Lehr, Arnd Voerste
  • Publication number: 20110275649
    Abstract: Novel combinations comprising HMG CoA reductase inhibitors, or statins, with partial fatty acid oxidation inhibitors (pFOXi), and methods for their use, are disclosed. These combinations are useful in preventing or reducing the risk of developing diabetes which results from therapy with a statin.
    Type: Application
    Filed: May 3, 2011
    Publication date: November 10, 2011
    Applicant: Palmetto Pharmaceuticals LLC
    Inventor: Wayne H. Kaesemeyer
  • Publication number: 20110269831
    Abstract: The invention provides uses and methods for reducing nephropathy in persons with diabetes mellitus (particularly Type 2 diabetes), in persons with metabolic syndrome, in persons with triglyceride levels over 215 mg/dL, and in persons with a cholesterol level over 200 mg/dL, by administering an inhibitor of soluble epoxide hydrolase (“sEH”). Optionally, a cis-epoxyeicosantrienoic acid (“EET”) can be administered with the sEH inhibitor. The invention further provides for using EETs in conjunction with one or more sEH inhibitors to reduce hypertension, and for compositions of EETs coated with a material insoluble in an acid of pH 3 but soluble in a solution with a pH of 7.4 or higher.
    Type: Application
    Filed: May 4, 2011
    Publication date: November 3, 2011
    Applicant: The Regents of the University of California
    Inventors: Bruce D. Hammock, Takaho Watanabe, Seung-Jin Ma, Susan E. Bennett, Judith S. Stern, Christophe Morisseau, In-Hae Kim
  • Publication number: 20110245206
    Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
    Type: Application
    Filed: February 23, 2011
    Publication date: October 6, 2011
    Inventors: XIN JIANG, XIAOFENG LIU, JACK GREINER, STEPHEN S. SZUCS, MELEAN VISNICK
  • Publication number: 20110230504
    Abstract: The present invention relates to compositions and methods for promoting and enhancing the analgesic, anesthetic and anticonvulsant properties of epoxygenated fatty acids, in particular, epoxy-eicosatrienoic acids (“EETs”) and inhibitors of soluble epoxide hydrolase (“sEH”) in the presence of elevated levels of cyclic adenosine monophosphate (“cAMP”) by combining or co-administering the epoxygenated fatty acid, EET and/or inhibitor of sEH with an agent that increases intracellular levels of cAMP, e.g., a phosphodiesterase inhibitor.
    Type: Application
    Filed: September 11, 2009
    Publication date: September 22, 2011
    Applicant: The Regents Of The University Of California Office Of Technology
    Inventors: Bruce D. Hammock, Ahmet Bora Inceoglu, Steven L. Jinks
  • Patent number: 8022103
    Abstract: Ester prodrugs of phorbol compounds for the treatment of viral infections, neoplastic diseases, inflammatory reactions, and use as analgesics, wherein the phorbol compounds are derivatized with a -x-o-c(o)-R? group linked to the 6-carbon of the phorbol residue.
    Type: Grant
    Filed: July 13, 2006
    Date of Patent: September 20, 2011
    Assignee: Salvia Sciences, Inc.
    Inventors: Rensheng Xu, Weimin Zhao, Chun Jiang
  • Publication number: 20110224179
    Abstract: We disclose a diagnostic test to determine suitable therapeutic intervention of subjects suffering from subclinical Cushing's syndrome [SCS] and also agents that antagonise the action of cortisol or inhibit excess cortisol production in the treatment of conditions such as SCS in the presence of an adrenal incidentaloma.
    Type: Application
    Filed: November 7, 2008
    Publication date: September 15, 2011
    Inventor: John Newell-Price
  • Patent number: 8017795
    Abstract: Disclosed are coating formulations that include a copolyester and a vinyl ether in which the copolyester is produced by copolymerizing a monomer composition that includes a fused aromatic diacid monomer, an unsaturated diacid monomer, and a polyol. Also disclosed are methods for producing a laser-ablatable film on a surface of a substrate. The method includes coating the substrate with a coating formulation that includes a copolyester and a vinyl ether and polymerizing the coating formulation. The copolyester includes a fused aromatic moiety covalently bonded therein. Novel radiation curable sensitizers that can be used in the preparation of radiation curable polymer films having improved laser ablation properties are also described.
    Type: Grant
    Filed: April 21, 2006
    Date of Patent: September 13, 2011
    Assignee: NDSU Research Foundation
    Inventors: Dean C. Webster, Zhigang Chen, Neena Ravindran
  • Patent number: 8013014
    Abstract: Methods for treatment and/or prevention of nerve degeneration in mammals using aza-peptide epoxide caspase inhibitors are provided. Aspects of the present disclosure include aza-peptide epoxide compositions to treat or prevent diseases, for example stroke, Alzheimer's disease, Parkinson's disease, multiple sclerosis, neuropathies, Huntington's disease, dentatorubropallidoluysian atrophy, spinocerebellar atrophies, spinal bulbar muscular atrophy, diabetes, amyotrophic lateral sclerosis and other motor neuron diseases. The disclosed methods can be used in combination with calpain inhibitors to treat disease or pathological conditions related to the activity of caspases and calpain associated with a specific disease or condition.
    Type: Grant
    Filed: January 24, 2006
    Date of Patent: September 6, 2011
    Assignee: Georgia Tech Research Corporation
    Inventors: James C. Powers, Jonathan D. Glass
  • Publication number: 20110212161
    Abstract: Disclosed are a composition and a method for treating skin disorders, including rosacea, pityriasis rosea, erythema, rhinophyma, and rosacea-associated disorders including pimples, papules, pustules, and telangiectasia.
    Type: Application
    Filed: February 4, 2011
    Publication date: September 1, 2011
    Applicant: Asan Laboratories Company (Cayman), Limited
    Inventors: Yih-Lin Chung, Nam-Mew Pui, Wei-Wei Chang
  • Publication number: 20110212072
    Abstract: Described are a method and a composition for preventing and/or treating a disease related to mitochondrial dysfunction by inhibiting the fatty acid oxidation of one or more cells of an organism. Particularly, the fatty acid oxidation is inhibited by inhibiting the expression and/or activity of the enzyme Camitin-Palmitoyl-Transferase-1 (CPT-1) by means of an arylalkyl- or arlyoxyalkyl-substitued oxirane carboxylic acid or pharmaceutically acceptable salts and derivatives of the arylalkyl-substituted oxirane carboxylic acid.
    Type: Application
    Filed: April 19, 2011
    Publication date: September 1, 2011
    Applicant: MediGene AG
    Inventors: Thomas Henkel, Christoph Rehfuess
  • Publication number: 20110190302
    Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-phenyl-sulfonamido-phenylene compounds of the following formula (I) (collectively referred to herein as “APSAP compounds”).
    Type: Application
    Filed: September 18, 2009
    Publication date: August 4, 2011
    Applicant: PIMCO 2664 LIMITED
    Inventors: Iain Robert Greig, Rose Mary Sheridan, Raymond Fisher, Matthew John Tozer, Juha Andrew Clase, Andrew Smith, Andrew Robert Tuffnell, Robert Jurgen Van 't Hof
  • Publication number: 20110190389
    Abstract: Disclosed are novel oxylipins, referred to herein as docosanoids and eicosanoids, that are derived from C22 polyunsaturated fatty acids and from C20 polyunsaturated fatty acids, respectively, and methods of making and using such oxylipins. Also disclosed is the use of docosapentaenoic acid (C22:5n-6) (DPAn-6), docosapentaenoic acid (C22:5n-3) (DPAn-3), and docosatetraenoic acid (DTAn-6: C22:4n-6), docosatrienoic acid (C22:3n-3) (DTrAn-3), docosadienoic acid (C22:2n-6) (DDAn-6), eicosatrienoic acid (C20:3n-3) (ETrAn-3) eicosapentaenoic acid and arachidonic acid as substrates for the production of novel oxylipins, and to the oxylipins produced thereby. Also disclosed is the use of DPAn-6, DPAn-3, DTAn-6, and/or the oxylipins derived therefrom, and/or novel docosanoids derived from the structures of C22 fatty acids in therapeutic and nutritional or cosmetic applications, and particularly as anti-inflammatory or anti-neurodegenerative compounds.
    Type: Application
    Filed: February 20, 2008
    Publication date: August 4, 2011
    Inventors: Linda Arterburn, William Barclay, Bindi Dangi, James Flatt, Jung Lee, Dutt Vinjamoori, Mary Van Elswyk
  • Publication number: 20110190242
    Abstract: The invention relates to methods of treating inflammatory disease comprising administering a compound of formula A, a compound of any one of formulae 1-49 or I-III, a lipoxin compound, or an oxylipin compound.
    Type: Application
    Filed: September 23, 2009
    Publication date: August 4, 2011
    Applicant: Resolvyx Pharmaceuticals, Inc.
    Inventor: Per Gjorstrup
  • Publication number: 20110178172
    Abstract: Carnitin-Palmitoyl-Transferase-1 (CPT-1) inhibitor for use in treating and/or preventing disorders caused by delipidation of neural tissue.
    Type: Application
    Filed: June 25, 2009
    Publication date: July 21, 2011
    Applicant: META-IQ APS
    Inventor: Josephus Dirk Nieland
  • Publication number: 20110172271
    Abstract: The present invention describes a method for determination of urinary globotriaosylceramide (Gb3) levels in non-Fabry disease cardiac patients. Determination of Gb3 levels provides a screening method for determining cardiac risk and may offer an alternative therapeutic option for cardiac disease management or cardiac disease risk mitigation by lowering Gb3 levels by the use of pharmacological chaperones or other agents.
    Type: Application
    Filed: November 17, 2010
    Publication date: July 14, 2011
    Applicant: Baylor Research Institute
    Inventors: Raphael Schiffmann, Fanny Mochel, Lawrence Sweetman, Sabrina Forni
  • Publication number: 20110150981
    Abstract: A compound of formula (I) for use in the treatment of a disease of the immune system; wherein R is an optionally-substituted alkyl, alkenyl, alkynyl, aryl, arylalkyl or alkylaryl moiety having from 1 to 50 carbon atoms; R1 is an optionally-substituted alkyl, alkenyl, alkynyl, aryl, arylalkyl or alkylaryl moiety having from 1 to 40 carbon atoms; each of R2, Wand R4 is independently selected from an optionally-substituted alkylene, alkenylene, alkynylene, arylene, arylalkylene or alkylarylene moiety having from 1 to 40 carbon atoms; each of X, Y and Z is independently selected from an optionally-substituted alkylene, alkenylene, alkenylene, arylene, alkylarylene, cycloalkylene, ketone, ester, amide, imide, imine, thioether, ether, thioester and thioketone; and P is selected from hydrogen, an alkyl group, a sugar residue, or a metal, phosphonium or ammonium species; wherein at least one of X, Y and Z includes a moiety selected from cyclopropyl, C=A, C-AH and C-OR5; wherein R5 is alkyl or haloalkyl, and A is O, S
    Type: Application
    Filed: April 22, 2009
    Publication date: June 23, 2011
    Applicant: Bangor University
    Inventors: Mark Stephen Baird, Juma' a Raheem Najeem Al-Dulayymi, Cornelias Theunissen, Gani Koza, Seppe Vander Beken, Johan Adriann March Grooten
  • Publication number: 20110144170
    Abstract: The present invention provides compounds capable of binding to an Fc receptor and modulating Fc receptor activity comprising a core lipophilic group in the form of an Aryl zing substituted with a group rich in p-electrons. The invention further provides for a method of treating an autoimmune disease involving Fc receptor activity using such compounds. A method for obtaining a compound which modulates Fc receptor activity is also provided, the method comprising: (a) providing or designing compounds having structural characteristics to fit in the groove of the Fc?RIIa structure; and (b) screening the compounds for modulating activity on the Fc receptor.
    Type: Application
    Filed: February 18, 2011
    Publication date: June 16, 2011
    Inventors: Mark Phillip Hogarth, Geoffrey Allan Pietersz, Gerard Peter Moloney
  • Publication number: 20110144045
    Abstract: A method for increasing the bioavailability of antiparasitic active ingredients, and therefore to potentiate the effects thereof, including combining antiparasitic active ingredients with an adjuvant, wherein, the antiparasitic active ingredients are capable of being recognized and binding to cellular transporters in order to be transported out of cells without being able to reach an intracellular therapeutic target, the transporters being present in the cells of the human or animal organism to which the antiparasitic active ingredients are administered, and, optionally, in the cells of parasites against which the antiparasitic active ingredients are administered, the adjuvant is a compound corresponding to fumagillin of the following formula (II):
    Type: Application
    Filed: December 22, 2010
    Publication date: June 16, 2011
    Applicant: INSTITUT NATIONAL DE LA RECHERCHE AGRONOMIQUE
    Inventors: Michel ALVINERIE, Jacques DUPUY, Anne LESPINE, Jean Francois SUTRA
  • Publication number: 20110144200
    Abstract: The invention describes the preparation and use of carotenoid and epi-lutein compositions to treat various ocular diseases.
    Type: Application
    Filed: December 8, 2010
    Publication date: June 16, 2011
    Inventor: Thomas Eidenberger
  • Publication number: 20110135764
    Abstract: Embodiments of the invention relate to a composition for controlling a target pest, wherein the composition includes at least two active ingredients selected from the group consisting of thymyl acetate, linalyl acetate, amyl butyrate, anise star oil, black seed oil, p-cymene, geraniol, isopropyl myristate, d-limonene, linalool, lilac flower oil, methyl salicylate, alpha-pinene, piperonal, piperonyl alcohol, tetrahydrolinalool, thyme oil white, thyme oil red, thymol, vanillin, and winter-green oil, wherein the composition causes synergistic control of the target pest.
    Type: Application
    Filed: March 19, 2009
    Publication date: June 9, 2011
    Applicant: TyraTech, Inc.
    Inventor: Essam Enan
  • Publication number: 20110136901
    Abstract: The present invention discloses 4-nerolidylcatechol and its derivatives isolated from South American/Amazon plants (Pothomorphe species) and their potential use as therapeutical agent for treatment of malarial symptoms, including malarial patients resistant to traditional drugs. The present invention also discloses a method for producing 4-nerolidylcatechol and their derivatives.
    Type: Application
    Filed: December 28, 2007
    Publication date: June 9, 2011
    Inventors: Ana Cristina Da Silva Pinto, Màrcia Rùbia Silva Melo, Valter Ferreira De Andrade Neto, Francisco Célio Maia Chaves, Pedro Paulo Ribeiro Vieira, Adrian Martin Pohlit
  • Publication number: 20110136902
    Abstract: There provided a 12-membered-ring macrolactam derivative having antitumor activity: A compound represented by Formula (1) or a salt thereof. In this Formula, R1 is a hydrogen atom, a C1-6 alkyl group, a C1-6 alkylcarbonyl group or a C6-14 arylcarbonyl group; R2 is a hydrogen atom or a C1-6 alkyl group; R3 is a hydrogen atom or a hydroxyl group; R4 is a hydrogen atom or a hydroxyl group; R5 is a hydrogen atom or a C1-6 alkyl group; R6 is a hydrogen atom or a hydroxyl group; and R7 is an acetyl group or the like.
    Type: Application
    Filed: February 15, 2011
    Publication date: June 9, 2011
    Inventors: Masayuki MIYANO, Daisuke ITO, Norio MURAI
  • Publication number: 20110129433
    Abstract: Disclosed herein are novel compositions and methods for treating or preventing GI tract disorders and/or GERD-related respiratory disorders as well as protecting stratified squamous epithelium against injury by a noxious substance. The methods generally include administering to a patient in need thereof a therapeutically effective amount of a pharmaceutical composition comprising at least one bile acid sequestrant, alone or in combination with at least one proton pump inhibitor, and optionally one or more agent chosen from antacids, histamine H2-receptor antagonists, ?-aminobutyricacid-b (GABA-B) agonists, prodrugs of GABA-B agonists, and protease inhibitors.
    Type: Application
    Filed: June 26, 2009
    Publication date: June 2, 2011
    Applicant: IRONWOOD PHARMACEUTICALS, INC.
    Inventor: Mark G. Currie
  • Publication number: 20110118347
    Abstract: A compound of the formula CH3(CH2)n—RA—(CH2)m-(CH?CH)q—(CH2)p—X wherein RA=(a); q=0 or 1; m and p are independently selected integers of at least 1; n=0 or an integer of at least 1; X is a polar group selected from —CO2RS, where Rs?H, Na, K, —NHRI, —NRIRII or RIII; —CH3OH; —CH3NH2; —CH3NHRI; or —CH3NRIRII; wherein RI, RII and RIII are independently selected from C1-C6 alkyl or an aryl group, preferably a hydrophilically substituted C1-C6 alkyl or aryl group, or RIII is an esterified glycol; and wherein 20>m+n+p+2q?2; is useful for the treatment of ringworm infection caused by Trichophyton tonsurans.
    Type: Application
    Filed: May 29, 2009
    Publication date: May 19, 2011
    Applicant: Vernolix Limited
    Inventor: Michael William Fowler
  • Publication number: 20110117106
    Abstract: Calpains target junctional components that normally seal the epithelium, forming tight junctions. This selective targeting by calpains facilitates the transmigration of leukocytes across the epithelium and into tissue spaces where they can cause inflammation. The present disclosure provides methods of using calpain inhibitors to prevent epithelial junction reorganization such that leukocyte transmigration is inhibited and accordingly, inflammation reduced or prevented. These methods can at least be used to reduce respiratory inflammation by preventing leukocyte accumulation in pulmonary airways.
    Type: Application
    Filed: March 6, 2009
    Publication date: May 19, 2011
    Inventor: Alice Prince
  • Patent number: 7943795
    Abstract: The present invention relates to novel, non-secosteroidal, phenyl-naphthalene compounds of Formula (I): wherein R, R1, RP, ZP, LP1, LP2 LNP, RP3, RN, and ZNP are defined herein, their preparation, pharmaceutical compositions, and methods of use.
    Type: Grant
    Filed: December 19, 2005
    Date of Patent: May 17, 2011
    Assignee: Eli Lilly and Company
    Inventors: Lynn Stacy Gossett, Jose Eduardo Lopez, Alan M. Warshawsky, Ying Kwong Yee
  • Publication number: 20110111038
    Abstract: A stable concentrated dietary supplement containing fucoxanthin as the main active component. The dietary supplement is made by a process including grinding crude freeze-dried flakes of wakame seaweed (Undaria pinnatifida) with desirable characteristics into a powder, extracting the active fucoxanthin from the powder with use of an aliphatic or aromatic organic solvent, then filtering and distilling the extract to form a thick syrupy fucoxanthin-containing mass having a solids content of from about 10-99% by wt. The mass is then purified by dissolving it in an organic non-polar solvent having a Polarity Index of <6, wherein the resultant solution is filtered to remove any solid material therefrom and the remaining liquid is then concentrated to a dried mass by removing substantially all of the solvent, which mass is thereafter ground and sifted to obtain a plurality of particles measuring approximately 60-100 mesh in size.
    Type: Application
    Filed: January 17, 2011
    Publication date: May 12, 2011
    Inventor: Achyut Padmawar
  • Publication number: 20110105458
    Abstract: Fatty acid inhibitors, pharmaceutical compositions including fatty acid inhibitors, methods for using fatty acid inhibitors to treat a variety of diseases, and methods for preparing fatty acid inhibitors are provided herein.
    Type: Application
    Filed: November 2, 2010
    Publication date: May 5, 2011
    Applicant: COMPLEXA, INC.
    Inventor: Bruce Branchaud
  • Publication number: 20110105603
    Abstract: In alternative embodiments the invention provides compositions and methods for ameliorating diseases and conditions having a beta-amyloid component, including Alzheimer's disease (AD), Vascular Dementia (VD), dementia, pre-dementia, Cognitive Dysfunction Syndrome (CDS) and loss of cognition in humans and in non-human animal. In alternative embodiment the invention provides analogs of AB-007 and its acid form E64c (loxistatin), their preparation, and pharmaceutical compositions thereof and methods of making and using same. In alternative embodiments compositions of the invention are deuterated analogs of AB-007 (or E64d) and E64c (or loxistatin). In alternative embodiments compositions of the invention are metabolically blocked forms as compared to AB-007 and loxistatin. In alternative embodiments compositions of the invention are used to ameliorate (including treat, slow, reverse or prevent) a disease or condition which can be ameliorated by partial or complete inhibition of a cysteine protease, e.g.
    Type: Application
    Filed: October 22, 2010
    Publication date: May 5, 2011
    Applicant: AMERICAN LIFE SCIENCE PHARMACEUTICALS, INC.
    Inventors: Robert J. TERNANSKY, Amy ALLAN, Gregory HOOK
  • Publication number: 20110098350
    Abstract: Novel substituted cyclohexylidene-ethylidene-octahydro-indene compounds and compositions comprising the same are described. The compounds exhibit profound anti-proliferative effects, in comparison to other compounds known for their anti-cancer and anti-hyperproliferative ability. Methods of use of such compounds and compositions are described for treating a variety of cancers, inflammatory and other hyperproliferative diseases and disorders.
    Type: Application
    Filed: June 16, 2009
    Publication date: April 28, 2011
    Inventors: Shimon Ben Shabat, Amnou Sintov
  • Publication number: 20110092484
    Abstract: [Problems] To provide a medicament which is effective for treatment and prophylaxis of cerebral aneurysms [Means for Solving the Problems] The invention provides a medicament for treatment and prophylaxis of cerebral aneurysms, wherein the medicament contains a cysteine protease inhibitor as an active ingredient. The cysteine protease inhibitor preferably is an epoxysuccinamide derivative or its salt.
    Type: Application
    Filed: June 6, 2008
    Publication date: April 21, 2011
    Applicant: NIPPON CHEMIPHAR CO., LTD.
    Inventors: Nobuo Hashimoto, Hiroharu Kataoka, Tomohiro Aoki
  • Publication number: 20110092447
    Abstract: Compounds can be used to act as inhibitors of enzymes having histone deacetylase activity for the medical therapy of conditions which predispose a person for the development of a disease, such as but not limited to cancer, inflammatory or metabolic diseases. Such conditions are linked to genetically inherited mutations of crucial genes which predispose a person with this condition to develop the disease phenotype. Thus, such compounds can be used for a suppressive therapeutic approach—the SUPPRESSION THERAPY—in order to inhibit or delay the onset or progression of the genetically predisposed disorder. Furthermore, a clinically used medicament can be manufactured for the SUPPRESSION THERAPY of such inherited predisposing conditions.
    Type: Application
    Filed: December 22, 2010
    Publication date: April 21, 2011
    Inventors: Bernd Hentsch, Alexander B. Maurer, Sascha Hovelmann, Monika Raab, Elke Martin
  • Patent number: 7928127
    Abstract: The present invention provides novel compounds of formulas I-IX, as described herein. Also provided are compositions of compounds of formulas I-IX, methods of making compounds of formulas I-IX, and methods of using compounds of formulas I-IX. The compounds of the invention can be used to inhibit matrix metalloproteinases, and are useful to treat conditions and diseases associated therewith.
    Type: Grant
    Filed: May 19, 2006
    Date of Patent: April 19, 2011
    Assignees: Notre Dame University, Wayne State University
    Inventors: Mijoon Lee, Masahiro Ikejiri, Mayland Chang, Rafael Fridman, Shahriar Mobashery
  • Publication number: 20110081423
    Abstract: Methods and devices for the stabilization of heart tissue to treat congestive heart failure using a therapeutic composition are discussed. The therapeutic composition can comprise an elastin stabilization agent, a collagen stabilization agent, or a combination thereof and be applied to the pericardium, to the outer surface of the myocardium, or a combination thereof using a catheter type of device with an attached reservoir. Controlled placement and release of the therapeutic composition can be achieved using a delivery vehicle to formulate the composition.
    Type: Application
    Filed: July 28, 2010
    Publication date: April 7, 2011
    Inventors: Norman R. Weldon, Matthew F. Ogle
  • Publication number: 20110070258
    Abstract: The fucoxanthin/pomegranate seed oil composition describes a method of slowing the aging process in a mammalian subject by activating at least one member of the sirtuin family of proteins, wherein the activating step includes administering to the subject a synergistic combination of fucoxanthin and punicic acid. Sirtuin enzymes exert their function by removing acetyl groups from proteins. The deacetylation results in inactivation of the proteins' role in cell metabolism and prevents genes from over-expression, thereby putting a cell into a state of hibernation and increasing its lifespan.
    Type: Application
    Filed: September 17, 2010
    Publication date: March 24, 2011
    Applicant: Polifenoles Naturales, S.L.
    Inventors: Miguel JIMENEZ DEL RIO, Paul Flowerman, Vladimir Badmaev
  • Publication number: 20110034550
    Abstract: The present invention relates to an inclusion compound of fumagillol derivative or its salt with hydroxypropyl-?-cyclodextrin or sulfobutylether-7-?-cyclodextrin, and pharmaceutical compositions comprising the same. The inclusion compound according to the present invention has superior water solubility and stability while exhibiting low toxicity, rendering it valuable as an anticancer agent or inhibitor of tumor metastasis.
    Type: Application
    Filed: April 8, 2010
    Publication date: February 10, 2011
    Inventors: Jae Hyun Kim, Su Kyung Lee, Won Kyu Choi, Jong Lae Lim, Soon Kil Ahn, Hee Jong Shin, Chung Il Hong
  • Publication number: 20110021627
    Abstract: There is provided a nitrile compound having an excellent controlling effect on arthropod pests represented by the formula (I): wherein m represents in integer of 0 to 4; n represents an integer of 1 to 4; q represents an integer of 0 to 4; Q represents a C1-C4 fluoroalkyl group; Z represents an optionally substituted C2-C6 alkynyl group or a ?N—OR3 group; R1 and R2 independently represent a monovalent C1-C4 chain hydrocarbon group optionally substituted with a halogen atom, etc.; and A represents an optionally substituted monovalent C1-C6 chain hydrocarbon group, etc.
    Type: Application
    Filed: March 18, 2009
    Publication date: January 27, 2011
    Applicant: Sumitomo Chemical Company, Limited
    Inventor: Hiromasa Mitsudera
  • Publication number: 20110015262
    Abstract: Methods and compositions for treating inflammatory and proliferative diseases, enabling treatment of MDR tumor cells by using combination of compounds, or a bifunctional compound, that inhibits both fatty acid metabolism and glycolysis. In particular, the invention combines or links a glycolysis inhibitor that is, or that is derived from, hypoglycin A (also referred to as hypoglycine A) and a fatty acid metabolism inhibitor. Preferably, the invention provides bifunctional compounds that link a moiety having the functionality of an oxirane carboxylic acid compound to a moiety having the functionality a hypoglycin A derivative. In specific embodiments, the invention provides a bifunctional compound that links a moiety having the functionality of etomoxir to a moiety having the functionality of hypoglycin A.
    Type: Application
    Filed: April 20, 2006
    Publication date: January 20, 2011
    Inventors: Martha Karen Newell, Evan Newell
  • Publication number: 20110014124
    Abstract: This invention relates generally to methods for ameliorating at least one symptom or aspect of atherosclerosis. The methods include administration of targeted carrier compositions comprising a therapeutic agent effective in ameliorating at least one aspect of atherosclerosis coupled to a targeting ligand effective is targeting the therapeutic agent to tissue associated with atherosclerotic plaque.
    Type: Application
    Filed: September 24, 2010
    Publication date: January 20, 2011
    Inventors: Gregory M. LANZA, Samuel A. WICKLINE
  • Publication number: 20110009387
    Abstract: The present invention relates e.g., to methods for predicting cellular sensitivity to farnesyl protein transferase inhibitors, such as lonafarnib; manumycin A; FTI-276; L-744832; BMS-214662; tipifarnib; BMS-316810K. The methods involve determining if malignant cells exhibit increased expression. of phosphorylated histone H2Ax following contact of one or more of said cells with said inhibitor.
    Type: Application
    Filed: June 11, 2008
    Publication date: January 13, 2011
    Inventor: Andrea Dawn Basso-Porcaro
  • Publication number: 20110009370
    Abstract: The present invention provides for compositions and methods for modulating tissue growth using tissue growth modulators, which are agents that either enhance or inhibit tissue growth as desired by a particular indication by modulating the PG or Wnt signaling pathways, or employing modulators of both PG and Wnt signaling pathways for a synergistic effect or highly selective effect.
    Type: Application
    Filed: October 22, 2007
    Publication date: January 13, 2011
    Applicant: CHILDREN'S MEDICAL CENTER CORPORATION
    Inventors: Leonard I. Zon, Trista E. North, Wolfram Goessling
  • Publication number: 20100331187
    Abstract: The present invention relates to physically stable oil dispersions. It also relates to a method for activating bentones that are designed for use with a low polarity organic systems. It also relates to physically stable oil dispersions comprising said activated bentone.
    Type: Application
    Filed: June 9, 2008
    Publication date: December 30, 2010
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Kirsty Jane Williams, Johathan Mark Richards