Having -c(=x)-, Wherein X Is Chalcogen, Attached Indirectly To Ring Carbon Of The Five-membered Hetero Ring By An Acyclic Carbon Or Acyclic Carbon Chain (e.g., Indole-3-acetic Acid, Etc.) Patents (Class 548/494)
  • Patent number: 9221812
    Abstract: The present invention relates to novel compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein, such as Alzheimer's disease, and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system. The present invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the preparation of medicaments for treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins. A method of treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins is also disclosed.
    Type: Grant
    Filed: April 18, 2011
    Date of Patent: December 29, 2015
    Assignee: AC Immune SA
    Inventors: Heiko Kroth, Cotinica Hamel, Pascal Benderitter, Wolfgang Froestl, Nampally Sreenivasachary, Andreas Muhs
  • Patent number: 9044463
    Abstract: The invention relates to FSH receptor antagonist according to general formula I or a pharmaceutically acceptable salt thereof and to a pharmaceutical composition containing the same. The compounds can be used for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, and for the treatment of uterine fibroids and other menstrual-related disorders.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: June 2, 2015
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Wesley Peter Blackaby, Martin De Kort, Mark Enthoven, Paul Stuart Hinchliffe, Cristian Bernard Matthijs Poulie, Cornelis Marius Timmers, Saskia Verkaik
  • Publication number: 20150133442
    Abstract: The invention features compositions and methods for inhibiting the Pin1 protein, and the treatment of disorders characterized by elevated Pin1 levels.
    Type: Application
    Filed: June 7, 2013
    Publication date: May 14, 2015
    Inventors: Kun Ping Lu, Matthew Brian Boxer, Mindy Irene Emily Davis, Rajan Pragani, Min Shen, Anton Momtchilov Simeonov, Shuo Wei, Xiao Zhen Zhou
  • Patent number: 8993611
    Abstract: The invention relates to a family of stable polyamine arylethylamide compounds, and to the use of these compounds as agents inhibiting DNA damages induced by by-products of the non-enzymatic glycosylation of skin tissues. The invention also relates to cosmetic or dermocosmetic compositions intended to fight skin disorders associated with said glycosylation by-products.
    Type: Grant
    Filed: July 1, 2013
    Date of Patent: March 31, 2015
    Assignee: Exsymol
    Inventor: Marie-Christine Seguin
  • Patent number: 8987321
    Abstract: The present invention provides analogs of a Lysofylline (LSF), and synthetic methods for the preparation of such analogs. The have the active side chain moiety (5-R-hydroxyhexyl) of LSF and can have greater potency and oral bioavailability than LSF.
    Type: Grant
    Filed: June 27, 2013
    Date of Patent: March 24, 2015
    Assignee: University of Virginia Patent Foundation
    Inventors: Timothy L. MacDonald, Jerry L. Nadler, Peng Cui
  • Patent number: 8962674
    Abstract: The present invention provides a novel compound that is structurally similar to curcumin and has a suppressive effect on A? aggregation, a degradative effect on A? aggregates, an inhibitory effect on ?-secretase, and a protective effect on neurons. The novel compound is a compound represented by the following general formula (Ia) or a salt thereof: wherein R1 represents a 4-hydroxy-3-methoxyphenyl group or the like, and R2 represents a 1H-indol-6-yl group or the like.
    Type: Grant
    Filed: November 30, 2007
    Date of Patent: February 24, 2015
    Assignees: Tokyo Institute of Technology, Kyoto University
    Inventors: Takashi Takahashi, Ichiro Hijikuro, Hachiro Sugimoto, Takeshi Kihara, Yoshiari Shimmyo, Tetsuhiro Niidome
  • Publication number: 20140315956
    Abstract: In one aspect, the invention relates to substituted 2-(1H-indol-3-yl)ethanol analogs and substituted 3,3a,8,8a-tetrahydro-2H-furo[2,3-b]indole analogs, derivatives thereof, and related compounds, which are useful as inhibitors of IL-6 mediated activation of the Jak2/STAT3 pathway; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a IL6 dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: July 29, 2012
    Publication date: October 23, 2014
    Applicants: NATIONWIDE CHILDREN'S HOSPITAL, OHIO STATE INNOVATION FOUNDATION
    Inventors: James Fuchs, Chenglong Li, Pui Kai Li, Jiayuh Lin
  • Publication number: 20140303186
    Abstract: The present application relates to nitrogen-containing fused ring compounds shown by general formula (I), a pharmaceutically acceptable salt thereof and a stereoisomer thereof as CRTH2 antagonist, wherein X1, X2, X3, X4, X5, W, X, Y, L1, L2, L3, A, B are as defined in the description; the present application further relates to a method for preparing the compounds, a pharmaceutical formulation and a pharmaceutical composition comprising the compounds, a use of the compounds for the manufacture of a medicament for the treatment and/or prevention of diseases related to activity of CRTH2.
    Type: Application
    Filed: November 16, 2012
    Publication date: October 9, 2014
    Inventors: Yan Zhang, Min Zhang, Hoyin Lo
  • Publication number: 20140296524
    Abstract: Halo-organic heterocyclic compounds are described, in which at least two halogen atoms are bound to a nitrogen-containing heterocyclic terminal moiety of the compound, with at least one of such halogen atoms being iodine or bromine. Also described are polymethine dyes based on these heterocyclic compounds, and dendrimeric compounds and conjugates of such polymethine dyes. The polymethine dyes are characterized by enhanced properties, e.g., brightness, photostability, sensitivity and/or selective affinity that make them useful to target cancer cells, pathogenic microorganisms, and/or other biological materials, in applications such as photodynamic therapy, photodynamic antimicrobial chemotherapy (PACT), cancer treatment, selective removal or attachment of biological materials, antimicrobial coating materials, and other diagnostic, theranostic, spectrum shifting, deposition/growth, and analytic applications.
    Type: Application
    Filed: May 5, 2014
    Publication date: October 2, 2014
    Applicant: Nanoquantum Sciences, Inc.
    Inventors: Gary W. Jones, Anatoliy L. Tatarets, Leonid D. Patsenker
  • Patent number: 8846748
    Abstract: Indolyl or indolinyl compounds of formula (I): wherein bond, n, R1, R2, R3, R4, R5, and R6, are defined herein. Also disclosed is a method for treating cancer with these compounds.
    Type: Grant
    Filed: March 29, 2011
    Date of Patent: September 30, 2014
    Assignees: Taipei Medical University, Ohio State University, National Taiwan University
    Inventors: Ching-Shih Chen, Jing-Ping Liou, Hsing-Jin Liu, Kuo-Sheng Hung, Pei-Wen Shan, Wen-Ta Chiu, Che-Ming Teng
  • Publication number: 20140249199
    Abstract: The disclosure relates to TAK1 inhibitors, compositions, and uses related thereto. In certain embodiments, the disclosure relates to compounds of formula (I), pharmaceutical compositions having a compound of formula (I), and methods of treating or preventing cancer by administering an effective amount of a pharmaceutical composition having a compound of formula (I) to a subject in need thereof.
    Type: Application
    Filed: July 19, 2012
    Publication date: September 4, 2014
    Applicants: HEALTH RESEARCH, INC., EMORY UNIVERSITY
    Inventors: Huw M. L. Davies, Spandan Chennamadhavuni, Andrei Bakin
  • Patent number: 8822525
    Abstract: Molecular mimics of Smac are capable of modulating apoptosis through their interaction with cellular IAPs (inhibitor of apoptosis proteins). The mimetics are based on a monomer or dimer of the N-terminal tetrapeptide of IAP-binding proteins, such as Smac/DIABLO, Hid, Grim and Reaper, which interact with a specific surface groove of IAP. Also disclosed are methods of using these peptidomimetics for therapeutic purposes. In various embodiments of the invention the Smac mimetics of the invention are combined with chemotherapeutic agents, including, but not limited to topoisomerase inhibitors, kinase inhibitors, NSAIDs, taxanes and platinum containing compounds use broader language.
    Type: Grant
    Filed: June 25, 2013
    Date of Patent: September 2, 2014
    Assignee: TetraLogic Pharmaceuticals Corporation
    Inventors: Stephen M. Condon, Matthew G. LaPorte, Yijun Deng, Susan R. Rippin
  • Patent number: 8809382
    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: Grant
    Filed: May 4, 2010
    Date of Patent: August 19, 2014
    Assignees: The Royal Institution for the Advancement of Learning/McGill University, Florida Institute of Technology
    Inventors: William S. Powell, Joshua Rokach
  • Patent number: 8802716
    Abstract: IAP binding molecules and compositions including these are disclosed. The IAP binding molecules interact with IAPB (inhibitor of apoptosis proteins) in cells and may be used to modify apoptosis in cells treated with such molecules. Embodiments of these compounds have a Kd of less than 0.1 micromolar. Methods of using these IAP binding molecules for therapeutic, diagnostic, and assay purposed are also disclosed.
    Type: Grant
    Filed: June 25, 2013
    Date of Patent: August 12, 2014
    Assignee: TetraLogic Pharmaceuticals Corporation
    Inventors: Stephen M. Condon, Matthew G. LaPorte, Yijun Deng, Susan R. Rippin
  • Publication number: 20140179723
    Abstract: Statin compositions are disclosed for stimulating neurite growth from spiral ganglion neurons in the inner ear and methods for preventing damage to or treating damage of auditory neurons and/or hair cells of the cochlea following acoustic or toxic insult.
    Type: Application
    Filed: December 13, 2013
    Publication date: June 26, 2014
    Inventors: Donna S. Whitlon, Claus-Peter Richter
  • Publication number: 20140142156
    Abstract: Compounds which modulate quorum sensing in quorum sensing bacteria. Compounds of the invention inhibit quorum sensing and/or activate quorum sensing in various bacteria. Compounds that inhibit quorum sensing are particularly useful for inhibition of detrimental bacterial biofilm formation. Compounds that activate quorum sensing are particularly useful for promoting growth and biofilm formation of beneficial bacterial.
    Type: Application
    Filed: December 12, 2013
    Publication date: May 22, 2014
    Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATION
    Inventors: Helen E. BLACKWELL, Christine E. McINNIS
  • Publication number: 20140128383
    Abstract: The present invention relates to compounds, their use in the treatment or the prevention of viral disorders, including HIV.
    Type: Application
    Filed: April 6, 2012
    Publication date: May 8, 2014
    Applicant: LABORATOIRE BIODIM
    Inventors: Sophie Chasset, Francis Chevreuil, Benoit Ledoussal, Frédéric Le Strat, Richard Benarous
  • Patent number: 8648208
    Abstract: A compound represented by the formula (I) or a pharmacologically acceptable salt thereof is used as an activator of PPAR wherein each of R1 and R2 is hydrogen, C1-8 alkyl, C1-8 alkyl substituted with halogen, or the like; each of R3, R4, R5, and R6 is hydrogen, C1-8 alkyl, or the like; X is sulfur or the like; Y is oxygen, a bond, or the like; p is 0 or 1; A is oxygen, CH2, N—NH2, or the like; when p is 1, B is phenyl, which can have a substituent; when p is 0, B is a condensed ring such as benzisoxazole, which can have a substituent; m is an integer of 1 to 4; and n is an integer of 0 to 5.
    Type: Grant
    Filed: April 15, 2009
    Date of Patent: February 11, 2014
    Assignee: Nippon Chemiphar Co. Ltd.
    Inventors: Shogo Sakuma, Rie Takahashi, Hideki Nakamura
  • Publication number: 20140005412
    Abstract: The present invention relates to a pharmaceutical combination composition comprising at least one HMG-CoA reductase inhibitor in a subtherapeutic dose and which is designed to prevent and/or to reduce the ageing of the body, particularly for use in prevention, reduction or reversal of arterial ageing in apparently healthy subjects.
    Type: Application
    Filed: February 28, 2012
    Publication date: January 2, 2014
    Applicant: FARMICOM PHARMACEUTICAL COMPANY D.O.O.
    Inventor: Miso Sabovic
  • Publication number: 20140005409
    Abstract: A compound represented by the following formula (I): wherein in formula (I), R1 represents a hydrogen atom, an alkyl group, an alkenyl group, an alkoxy group, an alkoxycarbonyl group, an acyl group, a carbamoyl group, a sulfamoyl group, a sulfo group, a cyano group, an aryl group or a heteroaryl group; R2 represents an alkyl group or an aryl group; each of R3 and R4 independently represents a hydrogen atom, an alkyl group, an alkenyl group, an alkoxy group, an alkoxycarbonyl group, a carbonyl group or an aryl group; X represents —O—, —S—, —NH—, —NR5—, —CH2—, —CR6H— or —CR6R7—; each of R5 to R7 independently represents an alkyl group or an aryl group; and R1 and any one of R5 to R7, or R3 and R4, may be bonded to each other to form a ring.
    Type: Application
    Filed: September 5, 2013
    Publication date: January 2, 2014
    Applicant: FUJIFILM CORPORATION
    Inventors: Youhei ISHIJI, Masanori HIKITA
  • Publication number: 20130296281
    Abstract: The invention relates to aryl and heteroaryl substituted compounds of Formula (I), and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein G, R1, and Z1-Z5 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Application
    Filed: June 16, 2011
    Publication date: November 7, 2013
    Applicant: Purdue Pharma L.P.
    Inventors: Donald J. Kyle, Chiyou Ni, Laykea Tafesse, Jiangchao Yao
  • Publication number: 20130267469
    Abstract: Indole-3-propionic acid as a marker and for treatment for Huntington Disease.
    Type: Application
    Filed: March 14, 2013
    Publication date: October 10, 2013
    Applicant: COUNTERPOINT HEALTH SOLUTIONS, INC.
    Inventor: Wayne Matson
  • Publication number: 20130231604
    Abstract: Halo-organic heterocyclic compounds are described, in which at least two halogen atoms are bound to a nitrogen-containing heterocyclic terminal moiety of the compound, with at least one of such halogen atoms being iodine or bromine. Also described are polymethine dyes based on these heterocyclic compounds, and dendrimeric compounds and conjugates of such polymethine dyes. The polymethine dyes are characterized by enhanced properties, e.g., brightness, photostability, sensitivity and/or selective affinity that make them useful to target cancer cells, pathogenic microorganisms, and/or other biological materials, in applications such as photodynamic therapy, photodynamic antimicrobial chemotherapy (PACT), cancer treatment, selective removal or attachment of biological materials, antimicrobial coating materials, and other diagnostic, theranostic, spectrum shifting, deposition/growth, and analytic applications.
    Type: Application
    Filed: March 3, 2012
    Publication date: September 5, 2013
    Applicant: NANOQUANTUM SCIENCES, INC.
    Inventors: Gary W. Jones, Anatoliy L. Tatarets, Leonid D. Patsenker
  • Patent number: 8497297
    Abstract: Molecular mimics of Smac are capable of modulating apoptosis through their interaction with cellular IAPs (inhibitor of apoptosis proteins). The mimetics are based on a monomer or dimer of the N-terminal tetrapeptide of IAP-binding proteins, such as Smac/DIABLO, Hid, Grim and Reaper, which interact with a specific surface groove of IAP. Also disclosed are methods of using these peptidomimetics for therapeutic purposes. In various embodiments of the invention the Smac mimetics of the invention are combined with chemotherapeutic agents, including, but not limited to topoisomerase inhibitors, kinase inhibitors, NSAIDs, taxanes and platinum containing compounds use broader language.
    Type: Grant
    Filed: August 2, 2011
    Date of Patent: July 30, 2013
    Assignee: TetraLogic Pharmaceuticals Corporation
    Inventors: Stephen M. Condon, Matthew G. LaPorte, Yijun Deng, Susan R. Rippen
  • Publication number: 20130184222
    Abstract: Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1 comprising administering to a subject in need thereof a compound described here.
    Type: Application
    Filed: July 15, 2011
    Publication date: July 18, 2013
    Applicant: AGIOS PHARMACEUTICALS, INC
    Inventors: Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey Saunders, Jeremy Travins, Shunqi Yan
  • Patent number: 8481587
    Abstract: The present invention relates to novel substituted 2-(5-hydroxy-2-methyl-1H-indol-3-yl)acetic acids, to novel antiviral active ingredients, pharmaceutical compositions, antiviral medicaments, methods for prophylaxis and treatment of viral diseases particularly caused by influenza viruses and infectious hepatisis C (HCV) viruses.
    Type: Grant
    Filed: November 27, 2009
    Date of Patent: July 9, 2013
    Inventors: Andrey Alexandrovich Ivashchenko, Nikolay Filippovich Savchuk, Alexander Vasilievich Ivashchenko, Pavel Mikhailovich Yamanushkin, Oleg Dmitrievich Mitkin, Vladimir Yurievich Vvedensky, Vadim Vasilievich Bichko
  • Patent number: 8445697
    Abstract: The present invention relates to squarylium dyes including an anchoring group, to a method of synthesis of such dye, to an electronic device comprising such dye, and to uses of such dye.
    Type: Grant
    Filed: October 27, 2008
    Date of Patent: May 21, 2013
    Assignee: Sony Corporation
    Inventors: Gerda Fuhrmann, Gabriele Nelles, Ameneh Bamedi Zilai, Akio Yasuda
  • Patent number: 8440840
    Abstract: A dye including an anchoring group in its molecular structure, said anchoring group allowing a covalent coupling of said dye to a surface, for example a surface of a nanoporous semiconductor layer, said anchoring group being represented by formula 1 wherein attachment of said anchoring group within said molecular structure of said dye is at the terminal carbon marked with an asterisk in above formula, wherein G is selected from —COOH, —SO3H, —PO3H2, —BO2H2, —SH, —OH, —NH2, preferably —COOH, wherein A is selected from the group comprising H, —CN, —NO2, —COOR, —COSR, —COR, —CSR, —NCS, —CF3, —CONR2-OCF3, C6H5-mFm, wherein m=1-5, R being H or any straight or branched alkyl chain of general formula —CnH2n+I, n=O-12, preferably 0-4, or any substituted or non-substituted phenyl or biphenyl.
    Type: Grant
    Filed: October 27, 2008
    Date of Patent: May 14, 2013
    Assignee: Sony Corporation
    Inventors: Gerda Fuhrmann, Gabriele Nelles, Ameneh Bamedi Zilai, Akio Yasuda
  • Patent number: 8436040
    Abstract: Indole compounds corresponding to the formula (I): as defined in the claims, pharmaceutically acceptable addition salts of such compounds, pharmaceutical compositions containing such compounds, the process for their preparation, and their use as pharmacologically active substances, especially in the treatment of hypertriglyceridemia, hyperlipidemia, hypercholesterolemia, diabetes, endothelial dysfunction, cardiovascular disease, inflammatory disease and neurodegeneration.
    Type: Grant
    Filed: June 7, 2010
    Date of Patent: May 7, 2013
    Assignee: Laboratoires Fournier S.A.
    Inventors: Jean Binet, Benaiessa Boubia, Pierre Dodey, Christiane Legendre, Martine Barth, Olivia Poupardin-Olivier
  • Publication number: 20130095040
    Abstract: The present invention relates to sulfonated unsymmetrical pentamethine optical dye compositions, especially dyes suitable for biological applications in vitro, and for in vivo imaging. Improved dye compositions and intermediates are provided, which enable the suppression of undesirable newly-identified impurities. Also provided is the use of the improved dye compositions in the preparation of conjugates with biological targeting molecules.
    Type: Application
    Filed: June 29, 2011
    Publication date: April 18, 2013
    Applicant: GE HEALTHCARE AS
    Inventor: Umamaheshwar P. Mokkapati
  • Publication number: 20130090482
    Abstract: The present invention provides type C crystal of compound I, type B crystal of compound II, or type C crystal of compound III set forth in this specification.
    Type: Application
    Filed: June 20, 2011
    Publication date: April 11, 2013
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Jun Takeuchi, Satoshi Itadani, Junya Ueda, Shizuka Ono, Takahiro Nekado, Manabu Fujita
  • Patent number: 8394970
    Abstract: Glutamic acid derivatives, in particular monatin, may be conveniently prepared by alkylating a 4-protected hydroxyl pyroglutamic acid derivative with an alkylating agent to prepare a 4-protected hydroxyl-4-alkylglutamic acid derivative, followed by the steps of hydrolysis and deprotection. The 4-protected hydroxyl pyroglutamic acid derivative is easy to produce from hydroxyproline. The 4-protected hydroxyl pyroglutamic acid derivative is particularly suitable for use in the efficient manufacture of monatin of high optical purity, since it can be alkylated selectively at the 4-position and stereoselectively and after its alkylation, it can easily be converted to a glutamic acid derivative.
    Type: Grant
    Filed: July 9, 2009
    Date of Patent: March 12, 2013
    Assignee: Ajinomoto Co., Inc.
    Inventor: Yusuke Amino
  • Patent number: 8367847
    Abstract: Methods for the preparation of the high intensity sweetener, monatin, 3-(1-amino-1,3-dicarboxy-3-hydroxy-but-4-yl)indole, its salts and internal condensation products thereof, including methods applicable to the large-scale production of monatin are described.
    Type: Grant
    Filed: October 1, 2007
    Date of Patent: February 5, 2013
    Assignee: Cargill, Incorporated
    Inventors: Subash Buddoo, Amanda Louise Rousseau, Gregory E. R. Gordon
  • Publication number: 20120322769
    Abstract: A method of reducing virulence in a bacterium comprising at least one of a GacS/GacA-type system, a HrpX/HrpY-type system, a T3SS-type system, and a Rsm-type system, the method comprising contacting the bacterium with an effective amount of a compound described herein.
    Type: Application
    Filed: February 16, 2011
    Publication date: December 20, 2012
    Applicants: DUKE UNIVERSITY, UWM RESEARCH FOUNDATION
    Inventors: Ching-Hong Yang, Xin Chen, Eric J. Toone
  • Patent number: 8314257
    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: November 20, 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: 20120245213
    Abstract: Methods and compositions are provided for modulating the activity of human type I taste receptor subunit 3 (hT1R3). Such materials and methods are useful for the screening and preparation of compositions and methods for the treatment of carbohydrate and lipid metabolic diseases and disorders.
    Type: Application
    Filed: October 1, 2010
    Publication date: September 27, 2012
    Inventors: Bedrich Mosinger, Emeline Maillet, Robert Margolskee
  • Patent number: 8268803
    Abstract: The present invention relates to 5,6-ring annulated indole derivatives of the formula (I), compositions comprising at least one 5,6-ring annulated indole derivatives, and methods of using the 5,6-ring annulated indole derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Grant
    Filed: December 17, 2007
    Date of Patent: September 18, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Frank Bennett, Srikanth Venkatraman, F. George Njoroge, Kevin X. Chen, Neng-Yang Shih, Stuart B. Rosenblum, Joseph A. Kozlowski
  • Patent number: 8232310
    Abstract: Peptides and compounds are provided that function as EWS-FLI1 protein inhibitors. The peptides and compounds have utility in the treatment of Ewing's sarcoma family of tumors. Also provided are methods of preparing the compounds and assays for identifying inhibitors of EWS-FLI1 protein.
    Type: Grant
    Filed: June 29, 2009
    Date of Patent: July 31, 2012
    Assignee: Georgetown University
    Inventors: Jeffrey A. Toretsky, Aykut Üren, Milton Lang Brown, Yali Kong
  • Patent number: 8227502
    Abstract: There are described Compounds of formula (I) in which R3 to R8 are independently selected from hydrogen, halogen, trihaloalkyl, alkyl having 1, 2, 3, 4 or 5 carbon atoms, electron donor groups selected from alkoxy having 1, 2, 3, 4 or 5 carbon atoms, trihaloalkoxy, hydroxy or amino, electron acceptor groups selected from cyano, sulphonic, nitro, or amide; R1 is an optionally substituted phenyl, benzyl or cyclohexyl group; R2 is selected from amino, substituted amino or guanidino groups, Z is a saturated or unsaturated C1-5 hydrocarbon chain, and salts thereof. A process for their preparation and compositions containing them are also described. The Compounds are either agonists or antagonists of a specific adenosine receptor or a number of adenosine receptors and have usefulness for the treatment of inflammation, arthritic conditions, rheumatoid arthritis, osteoarthritis, mental disorders, or for inducing central nerve regeneration.
    Type: Grant
    Filed: November 9, 2007
    Date of Patent: July 24, 2012
    Assignee: Anamar AB
    Inventors: Torbjorn Lundstedt, Elisabeth Seifert, Per Lek, Arne Boman
  • Publication number: 20120156255
    Abstract: A polymeric matrix for delivery of an HMG CoA reductase inhibitor such as a statin to tissue such as cardiac tissue in need thereof for the treatment or prevention of a disease or defect such as atrial fibrillation has been developed. In the preferred embodiment, a statin is delivered by means of a patch sutured to cardiac tissue at the time of cardiothoracic surgery. In the most preferred embodiment, the patch is a biodegradable material providing controlled or sustained release over a prolonged period of time, such as a week. Suitable materials include extracellular matrix, or other biodegradable hydrogels or polymeric materials providing sustained or controlled release of statin at the site of application.
    Type: Application
    Filed: December 16, 2011
    Publication date: June 21, 2012
    Inventors: Jaipal Singh, Nicolas Chronos
  • Publication number: 20120122792
    Abstract: S-t-butyl protected cysteine di-peptide analogs and related compounds and methods of using these compounds for the treatment of diseases and/or conditions, including but not limited to diseases and/or conditions of Central Nervous System (CNS).
    Type: Application
    Filed: November 11, 2011
    Publication date: May 17, 2012
    Applicant: PROMENTIS PHARMACEUTICALS, INC.
    Inventors: Edward M. Johnson, II, Daniel G. Lawton
  • Patent number: 8163936
    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: April 24, 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: 20120095071
    Abstract: Substantially pure 3-(3-indolyl)propionic acid free acid is synthesized by converting the free acid to 3-(3-indolyl)propionic acid calcium salt (3-IPA calcium), precipitating and washing, and then reconverting the 3-IPA calcium to the free acid. 3-IPA calcium is suitable for use in pharmaceutical compositions in tablet and sustained-release dosage forms. 3-IPA calcium can be used to inhibit the cytotoxic effects of amyloid beta protein on cells, to treat fibrillogenic diseases in a mammal, and to treat diseases or conditions in which free radicals or oxidative stress plays a role.
    Type: Application
    Filed: May 24, 2011
    Publication date: April 19, 2012
    Applicant: INTELLECT NEUROSCIENCES INC.
    Inventor: Norman H. Rogers
  • Patent number: 8148550
    Abstract: The present invention relates to a process for the production of statins, which are known as HMG-CoA reductase inhibitors. A few of the intermediate compounds for use in the process in accordance with the invention are novel compounds and the invention also relates to these novel intermediate compounds.
    Type: Grant
    Filed: April 28, 2006
    Date of Patent: April 3, 2012
    Assignee: Ratiopharm GmbH
    Inventors: Vitali Tararov, Armin Boerner, Gerd Koenig, Andrei Korostylev
  • Patent number: 8143426
    Abstract: Smac mimetics that inhibit IAPs.
    Type: Grant
    Filed: July 24, 2007
    Date of Patent: March 27, 2012
    Assignee: TetraLogic Pharmaceuticals Corporation
    Inventors: Stephen M. Condon, Matthew G. LaPorte, Yijun Deng, Susan R. Rippin
  • Publication number: 20120035374
    Abstract: The present invention relates to an improved process for the preparation of fluvastatin or pharmaceutical acceptable salts or derivatives thereof, in particular to a one-pot process for large scale production of Fluvastatin and salts thereof in high yield and high purity and pharmaceutical preparations containing said compounds.
    Type: Application
    Filed: April 15, 2009
    Publication date: February 9, 2012
    Applicant: PHARMATHEN S.A.
    Inventors: Theoharis V. Koftis, Thoedoros Panagiotidis, Rohit Ravikant Soni, Alexandra Lithadioti
  • Patent number: 8101649
    Abstract: This invention relates to N-acylhydrazone derivatives, which are found to be useful as modulators of the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
    Type: Grant
    Filed: November 19, 2008
    Date of Patent: January 24, 2012
    Assignee: Neurosearch A/S
    Inventors: Antonio Nardi, Jeppe Kejser Christensen, Dan Peters, Tino Dyhring
  • Patent number: 8101775
    Abstract: The invention relates to compounds of formula (I) wherein one of R5 and R6 is hydrogen or R2 and the other is (a) pharmaceutical compositions containing them and their use in the treatment of conditions or disorders which are mediated via the S1P1 receptor.
    Type: Grant
    Filed: December 19, 2007
    Date of Patent: January 24, 2012
    Assignee: Glaxo Group Limited
    Inventors: Mahmood Ahmed, James Myatt, David Norton, Dean Andrew Rivers
  • Publication number: 20120015966
    Abstract: Compounds are described that are active on at least one of PPAR?, PPAR?, and PPAR?, which are useful for therapeutic and/or prophylactic methods involving modulation of at least one of PPAR?, PPAR?, and PPAR?.
    Type: Application
    Filed: September 23, 2011
    Publication date: January 19, 2012
    Inventors: Jack Lin, Byunghun Lee, Shenghua Shi, Chao Zhang, Dean R. Artis, Prabha N. Ibrahim, Weiru Wang, Rebecca Zuckerman
  • Publication number: 20110306498
    Abstract: The present invention provides a method and a composition for restoring pollen fertility by suppressing formation insufficiency in a pollen formation process due to a high-temperature or low-temperature stress. The present invention provides a fertility restorative agent comprising an auxin as an active ingredient, and a method for restoring the fertility of a plants of the family Poaceae, comprising spreading an auxin. Moreover, the present invention provides a fertility restorative agent containing as an active ingredient a substance which inhibits auxin action, and a method for restoring the fertility of rice plant, including spreading a substance which inhibits auxin action.
    Type: Application
    Filed: July 8, 2011
    Publication date: December 15, 2011
    Inventors: Atsushi Higashitani, Masao Watanabe, Tadashi Sakata