The Bicyclo Ring System Consists Of The Five-membered Hetero Ring And A Benzene Ring (e.g., Indole, Etc.) Patents (Class 514/415)
  • Publication number: 20120190620
    Abstract: The present invention discloses methods to identify targets, pathways and molecules regulating purinosomes and their uses for treating pathophysiological disorders associated with purinosomes. Disclosed are methods related to both label-free cellular assays and fluorescence imaging to confirm the regulatory roles of various targets and molecules in purinosome dynamics. Disclosed are methods to classify molecules and the uses of these molecules for different indications. Specifically, the purinosome-disrupting molecules can be used for improved prevention and treatment of cancer development.
    Type: Application
    Filed: July 18, 2011
    Publication date: July 26, 2012
    Inventors: Stephen Benkovic, Ye Fang, Songon An, Florence Verrier
  • Publication number: 20120184591
    Abstract: It has been discovered that silodosin is effective in treating patients having symptoms associated with prostatitis with silodosin or a pharmaceutically acceptable salt thereof. In a preferred embodiment, patients are treated with 4 mg once daily.
    Type: Application
    Filed: February 23, 2011
    Publication date: July 19, 2012
    Applicant: WATSON PHARMACEUTICALS, INC.
    Inventors: Gary HOEL, Lawrence HILL, Kim CARAMELLI
  • Publication number: 20120184556
    Abstract: Disclosed are substituted benzoimidazolesulfonamides and substituted indolesulfonamides as mGluR4 potentiators.
    Type: Application
    Filed: July 23, 2010
    Publication date: July 19, 2012
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Charles David Weaver, Colleen M. Niswender, Yiu-Yin Cheung
  • Publication number: 20120178787
    Abstract: The invention relates to the use of melatonin, either alone or in combination with at least one compound selected from the group consisting of L-arginine, a physiologically acceptable salt thereof, one or more other physiologically acceptable compounds associated with the synthesis of nitric oxide and mixtures thereof, for the manufacture of a medicament for the therapeutic treatment, prophylactic treatment and/or prevention of postoperative infectious and/or non-infections complications induced by surgical interventions wherein the infectious complications may be pneumonia, wound infection (wound dehiscence), intra-abdominal abscess, and urinary tract infections (UTI) or wherein the non-infectious complication may be anastomotic leak, a pharmaceutical formulation comprising melatonin and at least one compound selected from the group consisting of L-arginine, a physiologically acceptable salt thereof, one or more other physiologically acceptable compounds associated with the synthesis of nitric oxide and mixt
    Type: Application
    Filed: August 12, 2011
    Publication date: July 12, 2012
    Inventor: Heinz Schneider
  • Publication number: 20120178780
    Abstract: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.
    Type: Application
    Filed: March 19, 2012
    Publication date: July 12, 2012
    Inventors: Jill E. WOOD, Hanno Wild, Daniel H. Rogers, John Lyons, Michael Katz, Yolanda Caringal, Robert Dally, Wendy Lee, Roger A. Smith, Cheri Blum
  • Publication number: 20120178757
    Abstract: A method is provided for the prevention of cancer metastasis in a patient comprising administering an adrenergic receptor antagonist to a patient in need thereof. The invention also includes an adrenergic receptor antagonist for use in the prevention of tumour recurrence in a patient. Also provided is a kit of parts for use in such methods comprising an adrenergic receptor antagonist, and an administration vehicle. A method is further included for identifying a patient at risk of developing cancer comprising the step of assaying for levels of expression of adrenergic receptor genes and proteins in said patient.
    Type: Application
    Filed: December 8, 2011
    Publication date: July 12, 2012
    Applicant: NOTTINGHAM UNIVERSITY HOSPITALS NHS TRUST
    Inventor: Desmond George Powe
  • Publication number: 20120171303
    Abstract: Compositions comprising melatonin and one or more carotenoids and methods for using such compositions for enhancing cognitive and related functions such as reducing or preventing a decline of social interaction, reducing or preventing age-related behavioral changes, increasing trainability, improving attention, maintaining optimal brain function, facilitating learning and memory, reducing memory loss, and preventing or treating cognitive decline caused by dementia in an animal. Preferably, the compositions are food compositions useful for enhancing cognitive function in humans and companion animals.
    Type: Application
    Filed: September 2, 2010
    Publication date: July 5, 2012
    Inventors: Brian Michael Zanghi, Ziad Saad Ramadan
  • Publication number: 20120172392
    Abstract: Compositions and methods are disclosed for inhibiting semicarbazide-sensitive amine oxidase (SSAO), also known as vascular adhesion protein-1 (VAP-1). The compounds disclosed are amine-containing and amide-containing compounds. The compounds and compositions are useful for treatment of diseases, including inflammation, inflammatory diseases and autoimmune disorders.
    Type: Application
    Filed: March 7, 2012
    Publication date: July 5, 2012
    Inventors: LUISA M. SALTER-CID, ERIC Y. WANG, MARY T. MACDONALD, JINGJING ZHAO
  • Patent number: 8211934
    Abstract: Novel compounds that have been found effective in inhibiting PDZ domain interactions, and particularly interactions of PDZ domains in MAGIs with the oncogenic (tumor suppressor) protein PTEN and interactions between the PDZ domain in the Dishevelled (Dvl) protein and other proteins such as the Frizzled (Fz) protein, have the general formula (I) or (III). The invention also includes combinatorial libraries, arrays and methods for screening and studying proteins using such compounds. Compounds of the invention have produced apoptosis in certain cell lines that overexpress the Dishevelled protein (Dvl), inhibiting Wnt signaling.
    Type: Grant
    Filed: August 4, 2010
    Date of Patent: July 3, 2012
    Assignee: The Regents of the University of California
    Inventors: Rodney Kiplin Guy, Naoaki Fujii, Liang You, David M. Jablons
  • Patent number: 8211923
    Abstract: The present invention relates to substituted arylsulphonylaminomethyl-phosphonic acid derivatives of general formula wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.
    Type: Grant
    Filed: July 25, 2008
    Date of Patent: July 3, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Holger Wagner, Elke Langkopf, Matthias Eckhardt, Ruediger Streicher, Corinna Schoelch, Annette Schuler-Metz, Alexander Pautsch
  • Patent number: 8211918
    Abstract: This invention provides compounds of formula I where the dashed line represents an optional double bond; where R1 is phenyl, naphthyl, pyridyl, pyrimidyl, pyrrolyl, imidazolyl, pyrazyl, furyl, thienyl, oxazolyl, isoxazolyl, thiazolyl, or isothiazolyl, optionally substituted, and other substituents are defined herein. Such compounds are potassium channel modulators.
    Type: Grant
    Filed: August 13, 2010
    Date of Patent: July 3, 2012
    Assignee: Valeant Pharmaceuticals International
    Inventors: Jean-Michel Vernier, Huanming Chen, Jianlan Song
  • Patent number: 8207208
    Abstract: A compound having the structure R—Y wherein R is, for example, Y is selected from the group consisting of 1) R5, 2) —C(R1R2)(C(R3R4))0-1Y1R5, and 3) —C(R1R2)—O—Y1R5; R1, R2, R3 and R4 are independently selected from the group consisting of hydrogen and C1-4 alkyl; R5 is Y1 is selected from the group consisting of —C(O)—O— and —P(O)(OR6)—O—; and R6 is hydrogen or CH3, or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.
    Type: Grant
    Filed: May 6, 2009
    Date of Patent: June 26, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Michael Man-chu Lo, Iyassu K. Sebhat, Chris Franklin, Nicoletta Almirante, Silvia Stefanini, Stefano Biondi, Ennio Ongini
  • Publication number: 20120156244
    Abstract: Pharmaceutical compositions for the treatment of nasal congestion, wherein the pharmaceutical compositions comprise low concentrations of a super-selective subclass of selective ?-2 adrenergic receptor agonists. Methods of using the compositions for the treatment of nasal congestion, cerebrovascular disease or systemic conditions, and as delivery vehicles to deliver other active agents to treat systemic or cerebrovascular diseases or conditions.
    Type: Application
    Filed: February 27, 2012
    Publication date: June 21, 2012
    Applicant: ALPHA SYNERGY DEVELOPMENT INC.
    Inventor: Gerald Horn
  • Publication number: 20120149693
    Abstract: The invention relates to protein binding interacting/binding compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating 5-HT2C and/or RSK disorders, including diseases and disorders mediated by GPCRs and/or RSKs.
    Type: Application
    Filed: May 5, 2010
    Publication date: June 14, 2012
    Applicant: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC.
    Inventor: Raymond G. Booth
  • Patent number: 8198274
    Abstract: This application discloses compounds of generic Formula I: or pharmaceutically acceptable salts thereof, wherein A, R1, R2, R3, R4, Q, X, Y, m, p, and q are defined as described herein, useful for treatment of diseases associated with monoamine reuptake inhibitors. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.
    Type: Grant
    Filed: July 15, 2009
    Date of Patent: June 12, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Eun Kyung Lee, Ryan Craig Schoenfeld, Robert James Weikert
  • Patent number: 8198314
    Abstract: The present invention provides indole derivatives that antagonize prostaglandin D2, and that can be used to treat inflammatory diseases mediated by prostaglandin D2.
    Type: Grant
    Filed: September 17, 2008
    Date of Patent: June 12, 2012
    Assignee: Oxagen Limited
    Inventors: David Middlemiss, Mark Richard Ashton, Edward Andrew Boyd, Frederick Arthur Brookfield, Michael George Hunter, Mark Whittaker, Chris Palmer, Eric R. Pettipher
  • Publication number: 20120142671
    Abstract: The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma.
    Type: Application
    Filed: November 1, 2011
    Publication date: June 7, 2012
    Applicant: Portola Pharmaceuticals, Inc.
    Inventors: Zhaozhong J. Jia, Yonghong Song, Qing Xu, Brian Kane, Shawn M. Bauer, Anjali Pandey
  • Publication number: 20120142668
    Abstract: Disclosed are 4-amino-2-butenamides of Formula (I) having pharmacological activity, pharmaceutical compositions containing them, and methods for the treatment of diseases mediated by the cathepsin C enzyme such as chronic obstructive pulmonary disease.
    Type: Application
    Filed: August 11, 2010
    Publication date: June 7, 2012
    Inventors: Niall Anderson, Ann M. Bullion, Neysa Nevins, Michael R. Palovich, Steven L. Sollis, Michael D. Wall, Jakob Busch-Petersen, Brian Evans, Huijie Li
  • Patent number: 8193194
    Abstract: In general, the invention relates to compounds useful as ion channel modulators. It has now been found that compounds of this invention, and pharmaceutically acceptable compositions thereof, are useful as inhibitors of voltage-gated sodium channels.
    Type: Grant
    Filed: May 21, 2008
    Date of Patent: June 5, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Esther Martinborough, Tim Neubert, Tara Whitney, Danielle Lehsten, Tara Hampton, Nicole Zimmermann, Andreas P. Termin
  • Patent number: 8193236
    Abstract: A compound of formula (I) wherein R denotes another heterocylic residue and wherein Ra, Rb, Rc, Rd and Re, are as defined in the specification, processes for their production, their uses, in particular in transplantation, and pharmaceutical compositions containing them.
    Type: Grant
    Filed: December 14, 2007
    Date of Patent: June 5, 2012
    Assignee: Novartis AG
    Inventors: Maurice van Eis, Peter von Matt, Jurgen Wagner
  • Publication number: 20120136006
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, L, Q, R1, R2, and R3 are defined herein.
    Type: Application
    Filed: February 6, 2012
    Publication date: May 31, 2012
    Inventors: Raymond W. Colburn, Scott L. Dax, Christopher M. Flores, Donald W. Ludovici, Jay M. Matthews, Mingde Xia, Xiaoqing Xu, Mark A. Youngman, Bin Zhu
  • Publication number: 20120122948
    Abstract: The invention relates to a compound of formula (Ia) wherein n is an integer between 2 and 10, R1 and R2 independently represent a substituent selected from the group consisting of hydrogen, C1-C10 alkyl, C3-C10 cycloalkyl and aminoalkyl, or R1 and R2 are taken together with the nitrogen atom to which they are attached to form a four to ten-membered heterocycle, R5 represents independently in each of the n units a substituent selected from the group consisting of hydrogen, C1-C10 alkyl, halogen, alkoxy, aminoalkyl and alkylamino; or a pharmaceutically acceptable salt thereof, with the proviso that the 5-fluorotryptamine is excluded, for the treatment or the prophylaxis of neuroinflammatory diseases or disorders. The invention also relates to a pharmaceutical composition, a method for inhibiting myeloperoxidase enzyme activity, to a method for inhibiting Low density lipoproteins oxidation.
    Type: Application
    Filed: May 27, 2010
    Publication date: May 17, 2012
    Applicant: UNIVERSITE LIBRE DE BEUXELLES
    Inventors: Jalal Soubhye, François Dufrasne, Pierre Van Antwerpen
  • Publication number: 20120122920
    Abstract: New compounds are continually being sought for the treatment and prevention of disorders. The invention relates to N-substituted-N-phenylethylsulfonamides libraries which can be used in the search for, and identification of, new lead compounds that could modulate the functional activity of a biological target.
    Type: Application
    Filed: December 22, 2011
    Publication date: May 17, 2012
    Inventors: JOSEP CASTELLS BOLIART, David Enrique MIGUEL CENTENO, Marta PASCUAL GILABERT
  • Publication number: 20120122870
    Abstract: Ischemia-reperfusion injury remains a primary cause of morbidity and mortality in individuals who experience disruption of normal blood flow to one or more major organs. For example, there are no clinically proven strategies that prevent acute renal failure following cardiac surgery. The present invention provides a variety of methods for the treatment or prevention of ischemia-reperfusion injury. In one aspect of the invention, a method for treating or preventing ischemia-reperfusion injury includes administering to a subject an effective amount of a sphingosine kinase inhibitor. Sphingosine kinase inhibitors are very effective in the protection against IR-induced acute renal failure and liver failure. Moreover, the effects occur very early after administration, requiring only a very short time of treatment. Toxicology studies with sphingosine kinase inhibitors demonstrate that they have low toxicity, even in long-term treatment.
    Type: Application
    Filed: May 10, 2010
    Publication date: May 17, 2012
    Applicants: MUSC FOUNDATION FOR RESEARCH DEVELOPMENT, APOGEE BIOTECHNOLOGY CORPORATION
    Inventors: Charles D. Smith, Zhi Zhong, Lynn W. Maines
  • Publication number: 20120122942
    Abstract: The present invention relates to novel pharmaceutically-useful compounds which are antagonists of the 5-oxo-ETE receptors, such as the OXE receptor. These compounds have use as therapeutic and/or prophylactic agents for diseases characterized by tissue eosinophilia, such as inflammatory conditions including respiratory diseases. The invention also relates to pharmaceutical compositions, to the use of such compounds and compositions as medicaments, and to therapeutic methods.
    Type: Application
    Filed: May 4, 2010
    Publication date: May 17, 2012
    Inventors: William S. Powell, Joshua Rokach
  • Publication number: 20120122931
    Abstract: A compound represented by the general formula (I) of the present invention, which has an EP1 receptor antagonism: [wherein A represents a benzene ring or the like; Y represents a C1-6 alkylene group or the like; RN represents a hydrogen atom or a C1-6 alkyl group; R1 represents a hydrogen atom, a C1-6 alkyl group or the like; R2 represents a phenyl group which may have a substituent, a 5-membered aromatic heterocyclic group which may have a substituent, a 6-membered aromatic heterocyclic group which may have a substituent or the like; R3 represents a halogen atom, a C1-6 alkoxy group or the like; R4 represents a hydrogen atom or the like; and R5 represents a hydrogen atom or the like] or a pharmaceutically acceptable salt thereof is provided. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.
    Type: Application
    Filed: July 26, 2010
    Publication date: May 17, 2012
    Applicant: KISSEI PHARMACEUTICAL CO., LTD.
    Inventors: Tatsuhiro Kondo, Atsushi Kondo, Kazuya Tatani, Naohiro Kawamura
  • Publication number: 20120115778
    Abstract: Methods for treating eating disorders associated with excessive weight gain, suppressing appetite, reducing body weight, or treating obesity in an animal by administering one or more antagonists of the serotonin Htr1a or Htr2b receptor, or a Tph2 inhibitor are provided, or combinations thereof.
    Type: Application
    Filed: July 15, 2010
    Publication date: May 10, 2012
    Applicant: The Trustees of Columbia University in the City of New York
    Inventors: Gerard Karsenty, Vijay Yadav, Franck Oury
  • Publication number: 20120114663
    Abstract: Disclosed are methods to treat allergic conditions, including pulmonary and non-pulmonary conditions, in a subject by administering a composition that inhibits Pim kinase. Also disclosed are methods to treat allergic conditions in a subject by administering a composition that induces expression of Runx3.
    Type: Application
    Filed: November 10, 2011
    Publication date: May 10, 2012
    Applicant: NATIONAL JEWISH HEALTH
    Inventors: Erwin W. Gelfand, Meiqin Wang
  • Patent number: 8173693
    Abstract: The present invention is related to derivatives of benzenesulfonamide represented by formula (I), and the pharmaceutical composition thereof. In addition, the benzenesulfonamide derivatives disclosed in the present invention can serve as potential cell cycle inhibitors, and thereby these benzenesulfonamide derivatives and the pharmaceutical composition thereof can be antitumor drug candidates, which might aim at cell cycle. Particularly, the benzenesulfonamide derivatives disclosed in the present invention may function as antitumor drugs to treat solid cancers.
    Type: Grant
    Filed: February 23, 2011
    Date of Patent: May 8, 2012
    Assignee: Purzer Pharmaceutical Co., Ltd.
    Inventors: Ji-Wang Chern, Grace Shiahuy Chen, Pei-Teh Chang, Kuan-Yu Chen, Meng-Ling Chen, Hsueh-Yun Lee, Chiung Hua Huang, Chun-Tang Chiou
  • Publication number: 20120107383
    Abstract: Osteoconductive matrices and methods are provided that have one or more statins disposed in calcium phosphate particles. The matrices may be injected into a fracture site. The osteoconductive matrices provided allow for sustained release of the statin and facilitate bone formation and repair of the fracture site.
    Type: Application
    Filed: October 27, 2010
    Publication date: May 3, 2012
    Applicant: WARSAW ORTHOPEDIC, INC.
    Inventor: William F. McKay
  • Publication number: 20120108592
    Abstract: A new class of salicylanilides is described. These compounds show strong activity against hepatitis viruses.
    Type: Application
    Filed: October 28, 2011
    Publication date: May 3, 2012
    Inventors: J. Edward Semple, Jean-Francois Rossignol
  • Publication number: 20120108617
    Abstract: Disclosed is bucindolol substantially free of its R-stereoisomer. Also disclosed are pharmaceutical compositions that include bucindolol substantially free of its R-stereoisomer or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. Also disclosed are methods of treating a patient that involve administering to the patient a therapeutically effective amount of a composition of the present invention. Formula (I).
    Type: Application
    Filed: January 27, 2009
    Publication date: May 3, 2012
    Applicant: Arca Biopharma, Inc.
    Inventors: Michael R. Bristow, Jonathan D. Port
  • Publication number: 20120108522
    Abstract: The present invention relates to the methods of treating endocrine-regulated cancers, including hormone resistant cancers, for example. More specifically, the present invention relates to a method of increasing the sensitivity of hormone resistant cancers to hormonal therapeutic agents. In particular embodiments, the present invention concerns delivery of a histone deacetylase inhibitor and a hormone targeted drug to an individual with cancer. In specific embodiments, the histone deacetylase inhibitor and the hormone targeted drug act synergistically to treat the cancer, including by overcoming resistance to a cancer therapy.
    Type: Application
    Filed: January 4, 2012
    Publication date: May 3, 2012
    Inventors: Angela Brodie, Vincent Njar, Gauri Sabnis, Lalji Gediya
  • Publication number: 20120108631
    Abstract: The invention relates to sulfonamide compounds and methods for activating PKM2. The compounds and methods are useful in treating or preventing a disease or disorder selected from cancer, cell proliferative disorder, inflammatory disorder, metabolic disorder, and immune system disorder.
    Type: Application
    Filed: October 26, 2011
    Publication date: May 3, 2012
    Inventors: Oren M. Becker, Alina Shitrit, Nili Schutz, Efrat Ben-Zeev, Avihai Yacovan, Rachel Ozeri, Tzofit Kehat, Sima Mirilashvili, Alex Aizikovich, Daniel Sherman, Vered Behar, Osnat Kashtan
  • Publication number: 20120107401
    Abstract: Osteoconductive matrices and methods are provided that have one or more statins disposed therein. The matrices may be injected into a fracture site. The osteoconductive matrices provided allow for sustain release of the statin and facilitate bone formation and repair of the fracture site.
    Type: Application
    Filed: October 27, 2010
    Publication date: May 3, 2012
    Applicant: WARSAW ORTHOPEDIC, INC.
    Inventor: William F. McKay
  • Publication number: 20120108570
    Abstract: The present invention relates generally to pharmacological methods for the prevention of amelioration of sleep-related breathing disorders via administration of agents or combinations of agents that possess serotonin-related pharmacological activity.
    Type: Application
    Filed: January 6, 2012
    Publication date: May 3, 2012
    Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
    Inventors: Miodrag Radulovacki, David W. Carley
  • Patent number: 8168673
    Abstract: Compounds of general formula (I) wherein W is chloro or fluoro; Z is a group SO2R1; wherein R1 is —C3-C8 cycloalkyl or heterocyclyl optionally substituted with one or more substituents chosen from halo, —CN, —C1-C6 alkyl, —SOR3, —SO2R3, —SO2N(R2)2, —N(R2)2, —NR2C(O)R3, —CO2R2, —CONR2R3, —NO2, —OR2, —SR2, —O(CH2)pOR2, and —O(CH2)pO(CH2)qOR2 wherein each R2 is independently hydrogen, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; each R3 is independently, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; p and q are each independently an integer from 1 to 3; and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.
    Type: Grant
    Filed: January 22, 2009
    Date of Patent: May 1, 2012
    Assignee: Oxagen Limited
    Inventors: Richard Edward Armer, Carole Eliane Andree Maillol, Colin Richard Dorgan, Graham Michael Wynne, Julia Vile
  • Publication number: 20120100223
    Abstract: Lipid compositions comprising nuts, seeds, oils, legumes, fruits, grains, and dairy useful in specified amounts as dietary supplements and diet plans designed around and including the aforementioned for the prophylaxis and treatment of numerous diseases are disclosed. The compositions include omega-6 and omega-3 fatty acids where the ratio of the omega-6 to the omega-3 fatty acids and their amounts are controlled based on one or more factors including age of the subject, sex of the subject, diet of the subject, the body weight of the subject, medical conditions of the subject, and climate of the subject's living area.
    Type: Application
    Filed: December 20, 2011
    Publication date: April 26, 2012
    Applicant: ASHA NUTRITION SCIENCES, INC.
    Inventor: Urvashi BHAGAT
  • Patent number: 8163787
    Abstract: A compound represented by the following general formula (1) or salts thereof or hydrates of the foregoing: wherein R1a, R1b, R1c and R1d each independently represent hydrogen, etc.; R2 represents optionally substituted phenyl, etc.; R3 represents optionally substituted C6-10 aryl, etc.; and Z1 and Z2 each independently represent hydrogen.
    Type: Grant
    Filed: January 13, 2011
    Date of Patent: April 24, 2012
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Richard Clark, Fumiyoshi Matsuura, Kazunobu Kira, Shinsuke Hirota, Hiroshi Azuma, Tadashi Nagakura, Tatsuo Horizoe, Kimiyo Tabata, Kazutomi Kusano, Takao Omae, Atsushi Inoue
  • Patent number: 8163764
    Abstract: Disclosed are compositions and methods for skincare, e.g., reducing skin wrinkles and for treating skin disorders.
    Type: Grant
    Filed: February 5, 2010
    Date of Patent: April 24, 2012
    Assignee: Asan Laboratories Company (Cayman) Limited
    Inventors: Yih-Lin Chung, Nam-Mew Pui, Wei-Wei Chang
  • Publication number: 20120095070
    Abstract: The present invention provides a means for prevention and treatment of sarcopenia by administration of a substance that both reduces the sensibility of beta-adrenergic receptors and of 5-HT1a receptors. (S)-pindolol, (S)-propanol, tertalol, or bopindolol are preferred for this purpose.
    Type: Application
    Filed: April 29, 2010
    Publication date: April 19, 2012
    Applicant: PSIOXUS THERAPEUTICS LIMITED
    Inventors: Jochen Springer, Stefan Anker, Andrew Coats, John Beadle
  • Publication number: 20120095004
    Abstract: The invention relates to substituted adamantane compounds, pharmaceutical compositions thereof, processes for their preparation, and methods for inhibiting sphingosine kinase and for treating or preventing hyperproliferative disease, inflammatory disease, or angiogenic disease.
    Type: Application
    Filed: October 19, 2011
    Publication date: April 19, 2012
    Applicant: APOGEE BIOTECHNOLOGY CORPORATION
    Inventors: Charles D. Smith, Kevin J. French, Yan Zhuang
  • Publication number: 20120095042
    Abstract: Provided are compounds of formula (I) wherein m is 0, 1 or 2; RI is a mono- or bicyclic heterocyclic ring system including one, two or three heteroatoms selected from nitrogen, sulphur and oxygen; R2 is selected from hydrogen, methyl and ethyl; I) R3 is hydrogen, methyl, or ethyl; and R4 and R5 are independently selected from ethyl and isopropyl; and R3, R4 and R5 together have at least 6 carbon atoms: or II) any two or all of R3, R4 and R5 form together with the carbon atom to which they are attached 3-para-menthyl, bornyl, or adamantyl; having cooling properties, their use as cooling agent and compositions including them.
    Type: Application
    Filed: May 4, 2010
    Publication date: April 19, 2012
    Inventor: Stefan Michael Furrer
  • Publication number: 20120095048
    Abstract: The present invention relates to allosteric binding compounds of formula (I), especially for the treatment of CNS disorders, together with pharmaceutical compositions and methods of treatment including these compounds.
    Type: Application
    Filed: February 19, 2010
    Publication date: April 19, 2012
    Applicants: REGION MIDT JYLLAND, AARHUS UNIVERSITET
    Inventors: Henrik Amtoft Neubauer, Ove Kjaer Wiborg, Henrik Helligsø Jensen
  • Publication number: 20120094977
    Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.
    Type: Application
    Filed: May 25, 2011
    Publication date: April 19, 2012
    Applicant: Dendreon Corporation
    Inventors: Sateesh K. Natarajan, Ofir Moreno, Thomas J. Graddis, David F. Duncan, Reiner Laus, Feng Chen
  • Patent number: 8158825
    Abstract: The present invention relates to a novel class of modified malonate derivatives. The modified malonate compounds can be used to treat cancer. The modified malonate compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Grant
    Filed: June 21, 2006
    Date of Patent: April 17, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jonathan Grimm, Paul Harrington, Richard Heidebrecht, Jr., Thomas Miller, Karin Otte, Phieng Siliphaivanh, David Sloman, Matthew Stanton, Kevin Wilson, David Witter, Solomon Kattar, Paul Tempest
  • Patent number: 8158671
    Abstract: The invention is directed to indole and indoline cyclopropyl amide derivatives as EP4 receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer. Pharmaceutical compositions and methods of use are also included.
    Type: Grant
    Filed: February 22, 2008
    Date of Patent: April 17, 2012
    Assignee: Merck Canada Inc.
    Inventors: Michael Boyd, John Colucci, Yongxin Han
  • Patent number: 8153680
    Abstract: Compounds and methods for treating cancer or inducing apoptosis in proliferating cells. The compounds are shown in formula I: wherein X is selected from hydroxyl, thiol, and amino; Y is selected from carboxyl and sulfonyl; R1, R2, R3, and R4 are selected from hydrogen, lower alkyl, and combinations thereof; R5, R6, and R7 are selected from hydrogen, halo, nitro, amino, methoxy, and combinations thereof; and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: August 25, 2009
    Date of Patent: April 10, 2012
    Assignee: The Ohio State University Research Foundation
    Inventors: Ching-Shih Chen, Jing-Ru Weng
  • Patent number: 8148547
    Abstract: The present embodiment of the invention is generally directed to compositions comprising suspensions of poorly water soluble compounds recrystallized in nanoparticulate sizes ranging from 0.1 to 5 ?m. In addition, the embodiment of the invention is directed to methods for preparation and administration of these compositions to a patient for prevention and treatment of disease states. In particular, the embodiment of the invention is directed to compositions comprising suspensions of poorly water-soluble compounds, such as antimitotics and antibiotics, in nanoparticulates and methods of prevention and treatment of chronic disease states, such as cancer, by intraperitoneal and intravenous administration of such compositions.
    Type: Grant
    Filed: February 2, 2010
    Date of Patent: April 3, 2012
    Assignee: The Texas A&M University System
    Inventor: Stephen S. Safe
  • Publication number: 20120077818
    Abstract: Provided herein are methods of and compositions for, treating, preventing and managing various neurological disorders. The methods comprise administering a transnorsertraline in combination with a serotonin receptor IA agonist, antagonist or modulator.
    Type: Application
    Filed: May 12, 2010
    Publication date: March 29, 2012
    Applicant: Sunovion Pharmaceuticals Inc.
    Inventors: Una Campbell, Judith Dunn