1,3-thiazoles (including Hydrogenated) Patents (Class 548/146)
  • Patent number: 7595343
    Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
    Type: Grant
    Filed: September 12, 2002
    Date of Patent: September 29, 2009
    Assignee: MethylGene, Inc.
    Inventors: Daniel Delorme, Soon Hyung Woo, Arkadii Vaisburg, Oscar Moradei, Silvana Leit, Stephane Raeppel, Sylvie Frechette, Giliane Bouchain
  • Patent number: 7592337
    Abstract: Tetrazole compounds substituted directly, or by a bridge, with i) a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl and ii) another heteroaryl or aryl ring, with at least one of the rings being further substituted with another ring, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, panic, and bipolar disorder, as well as in the treatment of pain, Parkinson's disease, cognitive dysfunction, epilepsy, circadian rhythm disorders, drug addiction, drug abuse, drug withdrawal, obesity and other diseases.
    Type: Grant
    Filed: March 7, 2003
    Date of Patent: September 22, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Chixu Chen, Nicholas D. P. Cosford, Brian W. Eastman, Dehua Huang, Steve F. Poon, Thomas S. Reger, Jeffrey R. Roppe, Nicholas D. Smith
  • Patent number: 7585880
    Abstract: The present invention provides a novel compound having a GPR40 receptor function modulating action, which is useful as an insulin secretagogue, a drug for the prophylaxis or treatment of diabetes and the like. A compound represented by the formula (I) wherein each symbol is as defined in the specification, a salt thereof and a prodrug thereof have unexpectedly superior GPR40 receptor agonist activity and also show superior properties as a pharmaceutical product, such as stability and the like. Thus, they can be safe and useful drugs for the prophylaxis or treatment of GPR40 receptor related conditions or diseases in mammals.
    Type: Grant
    Filed: December 24, 2004
    Date of Patent: September 8, 2009
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Tsuneo Yasuma, Shinobu Sasaki, Nozomu Sakai
  • Patent number: 7582780
    Abstract: The invention relates to a method of separating and isolating an acylated derivative of 4-[(S)-4-dimethylamino-1-(4-fluorophenyl)-1-hydroxybutyl]-3-hydroxymethylbenzonitrile by reaction of a mixture of the 4-[(S)-4-dimethylamino-1-(4-fluorophenyl)-1-hydroxy-butyl]-3-hydroxymethylbenzonitrile and an acylated derivative thereof with a compound which form a derivative of the 4-[(S)-4-dimethylamino-1-(4-fluorophenyl)-1-hydroxy-butyl]-3-hydroxymethylbenzonitrile containing a carboxylic acid group. The acylated derivative containing a carboxylic acid group precipitates once it is formed and may easily be separated from the reaction mixture.
    Type: Grant
    Filed: February 2, 2005
    Date of Patent: September 1, 2009
    Assignee: H. Lundbeck A/S
    Inventor: Lars Ole Lyngso
  • Patent number: 7576110
    Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).
    Type: Grant
    Filed: September 8, 2006
    Date of Patent: August 18, 2009
    Assignee: Abbott Laboratories
    Inventors: Marlon D. Cowart, Minghua Sun, Chen Zhao, Guo Zhu Zheng
  • Publication number: 20090202920
    Abstract: The present invention provides an optical recording composition comprising at least one optical recording compound selected from the group consisting of cyanine compounds having specific structures and a holographic recording medium comprising a recording layer, wherein the recording layer comprises at least one optical recording compound selected from the group consisting of cyanine compounds having specific structures.
    Type: Application
    Filed: February 10, 2009
    Publication date: August 13, 2009
    Applicant: FUJIFILM Corporation
    Inventor: Hiroyuki SUZUKI
  • Publication number: 20090204336
    Abstract: The invention relates to compounds which bind to the PDZ domains of proteins with PDZ domains, the uses of such compounds and screening methods for identification of such compounds.
    Type: Application
    Filed: April 28, 2006
    Publication date: August 13, 2009
    Applicant: Forschungsverbund Berlin e. V.
    Inventors: Mangesh Joshi, Hartmut Oschkinat, Markus Schade, Carolyn Vargas
  • Patent number: 7572816
    Abstract: The present invention is directed to compounds having the structure wherein R1, R2, R3, R4, R5 and m are as defined herein. The compounds of this invention are novel therapeutic agents for the treatment of cancer, metabolic diseases and skin disorders in mammalian subjects. These compounds are also useful modulators of gene expression. They exert their activity by interfering with certain cellular signal transduction cascades. The compounds of the invention are thus also useful for regulating cell differentiation and cell cycle processes that are controlled or regulated by various hormones or cytokines. In particular, the invention relates to compounds that induce apoptosis of cancer cells and therefore may be used for the treatment or prevention of cancer, including advanced cancers and pre-cancerous cells.
    Type: Grant
    Filed: July 21, 2004
    Date of Patent: August 11, 2009
    Assignee: Auspex Pharmaceuticals, Inc.
    Inventors: Bruno Tse, Sepehr Sarshar
  • Patent number: 7569678
    Abstract: Activated haptens useful for generating immunogens to HIV protease inhibitors, immunogens useful for producing antibodies to HIV protease inhibitors, and antibodies and labeled conjugates useful in immunoassays for the HIV protease inhibitor saquinavir. The novel haptens feature an activated functionality at the central, non-terminal hydroxyl group. Also described are monoclonal antibodies specific for saquinavir having less than 10% cross-reactivity with lopinavir, nelfinavir, amprenavir, ritonavir, and indinavir, and a murine hybridoma producing said antibodies.
    Type: Grant
    Filed: January 31, 2007
    Date of Patent: August 4, 2009
    Assignee: Roche Diagnostics Operations, Inc.
    Inventors: Gerald F. Sigler, Raymond A. Hui, Ina Deras, Erasmus Huber, Herbert W. Von Der Eltz, Sigrun Metz, Peter Kern
  • Publication number: 20090192179
    Abstract: The invention relates to novel chroman derivatives, stereoisomers and pharmaceutically acceptable salts of Formula I wherein the substituents are as defined in the specification. They are useful in the treatment of disorders mediated by lipoxygenase, such as immune diseases, respiratory diseases and cardiovascular diseases, as well as in the treatment of neurodegenerative disorders and/or mitochondria) disorders. They are also useful in the manufacture of pharmaceutical formulations for the treatment of such conditions.
    Type: Application
    Filed: February 26, 2009
    Publication date: July 30, 2009
    Inventors: Bing Wang, Jian Chen
  • Patent number: 7566716
    Abstract: Compounds of Formula I are useful for inhibiting Raf kinase and for treating disorders mediated thereby. Methods of using compounds of Formula I, and stereoisomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
    Type: Grant
    Filed: May 18, 2006
    Date of Patent: July 28, 2009
    Assignee: Array Biopharma Inc.
    Inventors: Ellen Laird, George Topalov, Joseph P. Lyssikatos, Mike Welch, Jonas Grina, Josh Hansen, Brad Newhouse
  • Patent number: 7566787
    Abstract: Cyclin D1 ablative agents and methods of using these agents in the treatment of cancers, and particularly breast cancer. Also provided are methods of treating cancer, the method comprising administering a therapeutically effective amount of one of the cyclin D1 ablative agents described herein to a subject in need of such treatment. Also provided are methods of treating cancers comprising using the cyclin D1 ablative agents described herein in combination therapies with existing chemotherapeutic agents.
    Type: Grant
    Filed: December 22, 2005
    Date of Patent: July 28, 2009
    Assignee: The Ohio State University
    Inventor: Ching-Shih Chen
  • Patent number: 7566444
    Abstract: Dye-peptide conjugates useful for diagnostic imaging and therapy are disclosed. The dye-peptide conjugates include several cyanine dyes with a variety of bis- and tetrakis(carboxylic acid) homologues. The small size of the compounds allows more favorable delivery to tumor cells as compared to larger molecular weight imaging agents. The various dyes are useful over the range of 350-1300 nm, the exact range being dependent upon the particular dye. Use of dimethylsulfoxide helps to maintain the fluorescence of the compounds. The molecules of the invention are useful for diagnostic imaging and therapy, in endoscopic applications for the detection of tumors and other abnormalities and for localized therapy, for photoacoustic tumor imaging, detection and therapy, and for sonofluorescence tumor imaging, detection and therapy.
    Type: Grant
    Filed: May 10, 2005
    Date of Patent: July 28, 2009
    Assignee: Mallinckrodt Inc.
    Inventors: Samuel I. Achilefu, Raghavan Rajagopalan, Richard B. Dorshow, Joseph E. Bugaj
  • Publication number: 20090186790
    Abstract: The present invention relates to photo-labile pro-fragrance conjugates comprising: a) a photo-labile unit which upon exposure to electromagnetic radiation is capable of releasing a pro-fragrance unit; and b) a pro-fragrance unit, which when so released is either i) a pro-fragrance compound capable of releasing a fragrance raw material; or ii) a fragrance raw material. The present invention relates to systems for delivering fragrances to a situs, and to laundry detergent compositions, fine fragrances, personal care and hair care compositions comprising said systems.
    Type: Application
    Filed: March 26, 2009
    Publication date: July 23, 2009
    Inventors: Robert Richard Dykstra, Gregory Scot Miracle, Lon Montgomery Gray
  • Patent number: 7563901
    Abstract: The present invention relates to compounds represented by formula (1) and a process for producing the same. The use of these compounds can realize the production of carbapenem derivatives having potent antimicrobial activity and a wide antimicrobial spectrum in a safe and cost-effective manner.
    Type: Grant
    Filed: February 15, 2008
    Date of Patent: July 21, 2009
    Assignee: Meiji Seika Kaisha, Ltd.
    Inventors: Toshiro Sasaki, Takashi Ando, Yasuo Yamamoto, Takahiro Imai, Dai Kubota, Katsuhiko Noguchi, Nobuyuki Hori, Eiki Shitara, Kunio Atsumi, Shohei Yasuda
  • Patent number: 7563813
    Abstract: Compounds of Formula 1, or pharmaceutically acceptable salts thereof, are provided: which are inhibitors of secreted frizzled related protein-1. The compounds, and compositions containing the compounds, can be used to treat a variety of disorders, including osteoporosis.
    Type: Grant
    Filed: May 10, 2006
    Date of Patent: July 21, 2009
    Assignee: Wyeth
    Inventors: Ariamala Gopalsamy, Mengxiao Shi
  • Publication number: 20090163549
    Abstract: The present invention provides a novel modulator of the TRPV1-receptor function, comprising a compound of the formula; wherein ring A is an optionally substituted carbocycle or heterocycle, ring B is an optionally substituted benzene ring or an optionally substituted 6-membered heteroaromatic ring containing N atom, a dashed line means existence or absence of a bond, n is 1 or 2, R1 and R2 are hydrogen etc., R3 is lower alkyl, R4 is lower alkyl or aryloxy, or R3 and R4 taken together may form optionally substituted 5- or 6-membered non-aromatic heterocycle.
    Type: Application
    Filed: December 13, 2006
    Publication date: June 25, 2009
    Inventor: Hiroyuki Kai
  • Patent number: 7550491
    Abstract: The present invention relates to salts comprising bis(trifluoromethyl)imide anions and saturated, partially or fully unsaturated, heterocyclic cations, to a process for the preparation thereof, and to the use thereof as ionic liquids.
    Type: Grant
    Filed: November 17, 2003
    Date of Patent: June 23, 2009
    Assignee: Merck Patent GmbH
    Inventors: Nikolai Ignatyev, Urs Welz-Biermann, Michale Schmidt, Helge Willner, Andriy Kucheryna
  • Patent number: 7550493
    Abstract: A halogenated benzamide derivative characterized by greater specificity for viral pathogens and less disruptive to beneficial gut microflora, according to formula (III): in which R1 is a halogen atom, and R2-R6 are independently hydrogen, hydroxyl, C1-C4 alkyl, —C1-C4 alkoxy, acyloxy, nitro, halogen, —C(O)R7 where R7 is —C1-C4 alkyl, or, aromatic including salts and hydrates of these compounds and where at least two of R2-R6 are not hydrogen and where at least one of R2-R6 are hydroxy or acyloxy.
    Type: Grant
    Filed: October 1, 2007
    Date of Patent: June 23, 2009
    Assignee: Romark Laboratories, LC
    Inventor: Jean Francois Rossignol
  • Patent number: 7538228
    Abstract: A chiral ligand represented by the formula and its enantiomer: wherein A, X, Y and Z are as defined in the specification is provided. Also provided is a process of making the chiral ligands and catalysts prepared from these ligands and a transition metal, a salt thereof or a complex thereof. In addition, a method of preparing an asymmetric compound by a transition metal catalyzed asymmetric reaction, such as, hydrogenation, hydride transfer reaction, hydrosilylation, hydroboration, hydrovinylation, hydroformylation, hydrocarboxylation, allylic alkylation, epoxidation, cyclopropanation, Diels-Alder reaction, Aldol reaction, ene reaction, Heck reaction and Michael addition is provided.
    Type: Grant
    Filed: December 17, 2004
    Date of Patent: May 26, 2009
    Assignee: The Penn State Research Foundation
    Inventors: Xumu Zhang, Duan Liu
  • Patent number: 7534790
    Abstract: Ion channel modulating compounds are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the treatment of arrhythmia and the production of analgesia and local anesthesia.
    Type: Grant
    Filed: November 21, 2007
    Date of Patent: May 19, 2009
    Assignee: Cardiome Pharma Corp.
    Inventors: Allen I. Bain, Gregory N. Beatch, Cindy J. Longley, Bertrand M. C. Plouvier, Tao Sheng, Michael J. A. Walker, Richard A. Wall, Sandro L. Yong, Jeff Jiqun Zhu, Alexander B. Zolotoy
  • Publication number: 20090124625
    Abstract: The present invention relates to novel compounds of formula (I) wherein W, n, X and W? are defined in the description; invention compounds are modulators of metabotropic glutamate receptors—subtype 5 (“mGluR5”) which are useful for the treatment of central nervous system disorders as well as other disorders modulated by mGluR5 receptors.
    Type: Application
    Filed: June 17, 2005
    Publication date: May 14, 2009
    Applicant: Addex Pharmaceuticals SA
    Inventors: Anne-Sophie Bessis, Christelle Bolea, Beatrice Bonnet, Mark Epping-Jordan, Nicolas Poirier, Sonia-Maria Poli, Jean-Philippe Rocher, Yves Thollon
  • Patent number: 7531563
    Abstract: The present invention relates to novel thiazoline acids and derivatives thereof useful as chelators of trivalent metals in therapeutic applications. For example, the thiazoline acid derivatives are useful in diagnosing and treating pathological conditions associated with an excess of trivalent metals in humans and animals.
    Type: Grant
    Filed: September 15, 2006
    Date of Patent: May 12, 2009
    Assignee: University of Florida Research Foundation, Inc.
    Inventor: Raymond J. Bergeron
  • Patent number: 7524876
    Abstract: A compound represented by the following general formula (I) or a salt thereof: [wherein R1 and R2 represent hydrogen atom, a C1-6 alkyl group, or a group represented by the following formula (A): [wherein X1 and X2 represent hydrogen atom, or a group represented as —N(R3)(R4) (R3 and R4 represent hydrogen atom, a C1-6 alkyl group, a C1-6 alkylcarbonyl group, or a C1-6 alkyloxycarbonyl group); and n represents an integer of 1 to 6 ], provided that R1 and R2 do not simultaneously represent hydrogen atom), which is a novel luciferin derivative that serves as a luciferase substrate.
    Type: Grant
    Filed: July 27, 2006
    Date of Patent: April 28, 2009
    Assignee: The University of Tokyo
    Inventors: Hideo Takakura, Yasuteru Urano, Tetsuo Nagano
  • Patent number: 7524870
    Abstract: The present invention relates to compounds of formula (I) wherein Ar, Ar2, R2, R3, R4, m, p and s are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases that are associated with the activation of the glycogen synthase enzyme, such as diabetes.
    Type: Grant
    Filed: November 21, 2005
    Date of Patent: April 28, 2009
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Paul Gillespie, Robert Alan Goodnow, Jr., Jefferson Wright Tilley
  • Patent number: 7521563
    Abstract: A compound which inhibits the production of IL-6 and/or TNF? by inflammatory cytokines and is useful in the prevention of or treatments for diseases such as various inflammatory diseases in which these cytokines participate and autoimmune diseases. It is a hydroxamic acid derivative represented by the following formula (1): (1) (wherein A and B each represents phenyl, etc.; n is an integer of 1 to 8; and Y represents oxygen or sulfur). This compound has excellent interleukin-6 and/or TNF? production inhibitory activity and is useful as a therapeutic agent for various inflammatory diseases, autoimmune diseases, etc.
    Type: Grant
    Filed: August 10, 2004
    Date of Patent: April 21, 2009
    Assignee: Shizuoka Coffein Co., Ltd.
    Inventors: Kiyoshi Nakatogawa, Masamichi Takagi, Makoto Akashima
  • Publication number: 20090099243
    Abstract: The invention relates to compound of the formula (I) in which the substituents are as defined in the specification; in free base form or in acid addition salt form; to its preparation, to its use as medicament and to medicaments comprising it.
    Type: Application
    Filed: October 15, 2008
    Publication date: April 16, 2009
    Inventors: Joachim Nozulak, David Orain
  • Patent number: 7517368
    Abstract: The present invention has for an object agents for coloring keratin fibers and containing at least one indolylthiazoliumazo dye of general formula (I)
    Type: Grant
    Filed: November 26, 2004
    Date of Patent: April 14, 2009
    Assignee: Wella AG
    Inventors: Cecile Pasquier, Veronique Buclin, Nadia Duc-Reichlin, Caroline Kiener, Hans-Juergen Braun
  • Publication number: 20090088457
    Abstract: The invention relates to novel primary amine derivatives and the use thereof as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as inhibitors of renin.
    Type: Application
    Filed: March 1, 2007
    Publication date: April 2, 2009
    Applicant: Actelion Pharmaceuticals, Ltd.
    Inventors: Olivier Bezencon, Daniel Bur, Olivier Corminboeuf, Corinna Grisostomi, Lubos Remen, Sylvia Richard-Bildstein, Thomas Weller
  • Patent number: 7511034
    Abstract: Novel dialkylhydroxybenzoic acid derivatives containing metal chelating groups are disclosed. The novel compounds are used as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactive oxygen species and/or excess Zn ions, in particular stroke, Parkinson's disease, Alzheimer's disease. The compounds have not only low toxicity but also similar or superior LPO inhibition activity to references. They also effectively inhibit the cerebral neuronal cell death by ROS and/or zinc ion, and show neuroprotective effects against ischemic neuronal degeneration.
    Type: Grant
    Filed: January 11, 2006
    Date of Patent: March 31, 2009
    Assignee: Samsung Electronics Co., Ltd.
    Inventors: Eu-Gene Oh, Sung-Bo Ko, Kyung-Hwa Kim, In-Kyu Chang, Dennis W. Choi, Laura L. Dugan, Jae-Young Koh, In-Jae Shin, Moo-Ho Won
  • Patent number: 7504520
    Abstract: The present invention is directed to compounds of formula (I) wherein variables W, X, Y, D, A, n, R1, R2 and R9 are as defined in the description.
    Type: Grant
    Filed: May 10, 2006
    Date of Patent: March 17, 2009
    Assignee: Abbott Laboratories
    Inventors: Arthur Gomtsyan, Richard J. Perner, John R. Koenig, Margaret Chi-Ping Hsu, Dilinie P. Fernando, Chih-Hung Lee
  • Patent number: 7504423
    Abstract: Compounds represented by the ?-amino acid derivative or a pharmaceutically acceptable salt thereof of the present invention have a therapeutic effect due to a DPP-IV inhibitory action and useful as pharmaceutical agents for the treatment and/or prophylaxis of diseases relating to a DPP-IV inhibitor.
    Type: Grant
    Filed: December 10, 2004
    Date of Patent: March 17, 2009
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Fumihiko Akahoshi, Yoshiharu Hayashi
  • Publication number: 20090054435
    Abstract: The present invention provides a compound represented by the formula: wherein each symbol is as defined in the specification. Since the compound of the present invention has superior hypoglycemic action and superior hypolipidemic action, it is useful as an agent for the prophylaxis or treatment of diabetes, hyperlipidemia, impaired glucose tolerance and the like.
    Type: Application
    Filed: July 28, 2006
    Publication date: February 26, 2009
    Inventor: Hiroshi Imoto
  • Publication number: 20090054420
    Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).
    Type: Application
    Filed: August 21, 2008
    Publication date: February 26, 2009
    Applicant: ABBOTT LABORATORIES
    Inventors: Robert J. Altenbach, Lawrence A. Black, Sou-Jen Chang, Marlon D. Cowart, Ramin Faghih, Gregory A. Gfesser, Yi-Yin Ku, Huaqing Liu, Kirill A. Lukin, Diana L. Nersesian, Yu-ming Pu, Padam N. Sharma, Youssef L. Bennani, Michael P. Curtis
  • Publication number: 20090053175
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.
    Type: Application
    Filed: August 22, 2008
    Publication date: February 26, 2009
    Inventors: Yat Sun Or, Ce Wang, Jiang Long, Lu Ying, Yao-Ling Qiu
  • Publication number: 20090047247
    Abstract: The present invention discloses compounds of formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.
    Type: Application
    Filed: August 12, 2008
    Publication date: February 19, 2009
    Inventors: Yao-Ling Qiu, Ce Wang, Lu Ying, Yat Sun Or
  • Publication number: 20090048228
    Abstract: The present invention relates to compounds of formula I: or pharmaceutically acceptable salts or tautomers thereof, which are inhibitors of histone deacetylase (HDAC). The compounds of the present invention are useful for treating cellular proliferative diseases, including cancer. Further, the compounds of the present invention are useful for treating neurodegenerative diseases, schizophrenia and stroke among other diseases.
    Type: Application
    Filed: December 9, 2005
    Publication date: February 19, 2009
    Inventors: Barbara Attenni, Federica Ferrigno, Philip Jones, Raffaele Ingenito, Olaf Kinzel, Laura Llauger Bufi, Jesus Maria Ontoria, Giovanna Pescatore, Michael Rowley, Rita Scarpelli, Carsten Schultz
  • Publication number: 20090030018
    Abstract: This invention relates to novel benzimidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex, and in particular for combating anxiety and related diseases.
    Type: Application
    Filed: April 18, 2006
    Publication date: January 29, 2009
    Inventors: Lene Teuber, Janus S. Larsen, Philip K. Ahring, Elsebet Ostergaard Nielsen, Naheed Mirza
  • Publication number: 20090030038
    Abstract: The present invention relates to new compounds of formula I. (I) wherein R1 to R12, X, Q and n are as defined as in formula I, or salts, solvates or solvated salts thereof, processes for their preparation and to new intermediates used in the preparation thereof, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.
    Type: Application
    Filed: May 22, 2006
    Publication date: January 29, 2009
    Applicant: ASTRAZENECA AB
    Inventors: Chester Chu, Andrew Lister, Gunnar Nordvall, Carl Petersson, Didier Rotticci, Daniel Sohn, Stefan Von Berg
  • Publication number: 20090023928
    Abstract: The present invention provides luminescent lanthanide metal chelates comprising a metal ion of the lanthanide series and a complexing agent comprising at least one phthalamidyl moiety. Also provided are probes incorporating the phthalamidyl ligands of the invention and methods utilizing the ligands of the invention and probes comprising the ligands of the invention.
    Type: Application
    Filed: September 1, 2008
    Publication date: January 22, 2009
    Applicant: The Regents of the Univeristy of California
    Inventors: Kenneth N. Raymond, Stephane Petoud, Seth Cohen, Jide Xu
  • Publication number: 20090018139
    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: Application
    Filed: September 17, 2008
    Publication date: January 15, 2009
    Applicant: Oxagen Limited
    Inventors: David Middlemiss, Mark Richard Ashton, Edward Andrew Boyd, Frederick Arthur Brookfield, Michael George Hunter, Mark Whittaker, Chris Palmer, Eric R. Pettipher
  • Patent number: 7476686
    Abstract: The invention provides compounds and pharmaceutically acceptable salts of Formula I wherein the variables A1, A2, R1, R2, V, W, X, Y, and Z are defined herein. Certain compounds of Formula I described herein which possess potent antiviral activity. The invention particularly provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These infectious diseases include viral infections, particularly HCV infections.
    Type: Grant
    Filed: December 17, 2004
    Date of Patent: January 13, 2009
    Assignee: Achillion Pharmaceuticals, Inc.
    Inventors: Dawei Chen, Milind Deshpande, Andrew Thurkauf, Avinash Phadke, Xiangzhu Wang, Yiping Shen, Cuixian Liu, Jesse Quinn, Junko Ohkanda, Shouming Li
  • Publication number: 20090012070
    Abstract: It has now been found that certain novel heterocyclic derivatives have provided unexpected insecticidal activity. These compounds are represented by formula (I): R Preferred are those compounds of formula (I) where R2 and R3 taken together is ?NCH(R6)CH(R7)N(R8)—, ?NC(R6)=C(R7)N(R8)-, or ?CHN?C(R7)N(R8)—, and tautomers thereof, and where R4 and R5 taken together is —C(R11)=C(R12)C(R13)=C(R14) 112, -, where R, R, R6, R7, R8, R11, R R13, R14, and X are described. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula (I), and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.
    Type: Application
    Filed: August 22, 2008
    Publication date: January 8, 2009
    Applicant: Bayer Cropscience AG
    Inventors: John A. Dixson, Zeinab M. Elshenawy, Harvey R. Wendt, Saroj Sehgel, Robert H. Henrie, II, David M. Roush, Ping Ding, John W. Lyga, Stephen F. Donovan
  • Patent number: 7473281
    Abstract: Colorant for keratin fibers containing cationic indazoline thiazolazo dyes of the general formula (I).
    Type: Grant
    Filed: March 27, 2007
    Date of Patent: January 6, 2009
    Assignee: The Procter & Gamble Company
    Inventors: Markus Speckbacher, Hans-Jürgen Braun
  • Publication number: 20090004140
    Abstract: The present invention discloses compounds of Formulae (I) and (II), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.
    Type: Application
    Filed: June 25, 2008
    Publication date: January 1, 2009
    Inventors: YAO-LING QIU, Lu Ying, Yat Sun Or, Ce Wang, Jiang Long
  • Patent number: 7465752
    Abstract: Compounds of the formula (I): in which R, R1, R2 and R3 are as defined in the description, to their use for the treatment of dyslipidaemia, atherosclerosis and diabetes, to pharmaceutical compositions comprising them and to the processes for the preparation of these compounds.
    Type: Grant
    Filed: April 6, 2005
    Date of Patent: December 16, 2008
    Assignee: Merck Patent GmbH
    Inventors: Jean Jacques Zeiller, Hervè Dumas, Valérie Guyard-Dangremont, Isabelle Berard, Francis Contard, Daniel Guerrier, Gérard Ferrand, Yves Bonhomme
  • Publication number: 20080293747
    Abstract: A highly active synthetic epothilone compound whose activity exceeds that of either epothilone EpoA or EpoB when assayed as a cytotoxic agent against a cancer cell line is disclosed as is a pharmaceutical composition containing the synthetic epothilone.
    Type: Application
    Filed: November 9, 2006
    Publication date: November 27, 2008
    Inventors: Kyriacos C. Nicolaou, Benjamin Pratt, Stellios Arseniyadis
  • Patent number: 7438894
    Abstract: Highly hydrophilic indole and benzoindole derivatives that absorb and fluoresce in the visible region of light are disclosed. These compounds are useful for physiological and organ function monitoring. Particularly, the molecules of the invention are useful for optical diagnosis of renal and cardiac diseases and for estimation of blood volume in vivo.
    Type: Grant
    Filed: October 7, 2003
    Date of Patent: October 21, 2008
    Assignee: Mallinckrodt, Inc.
    Inventors: Samuel Achilefu, Raghavan Rajagopalan, Richard B. Dorshow, Joseph E. Bugaj, Muthunadar P. Periasamy
  • Patent number: 7439260
    Abstract: The instant invention provides compounds of Formula (I) which are leukotriene biosynthesis inhibitors. Compounds of formula (I) are useful as anti-asthmatic, anti-allergic, anti-inflammatory, cytoprotective and anti-artherosclerotic agents.
    Type: Grant
    Filed: June 8, 2004
    Date of Patent: October 21, 2008
    Assignee: Merck Forsst Canada & Co.
    Inventors: Yves Gareau, Helene Juteau, D. Bruce MacKay, Richard Friesen, Erich L. Grimm, Marc Blouin, Sebastien Laliberte
  • Patent number: RE40558
    Abstract: The use of diaryl acid derivatives of formula (I) or pharmaceutically acceptable salts, N-oxides, hydrates or solvates thereof, wherein the variables shown are defined in the disclosure, and their pharmaceutical compositions as PPAR ligand receptor binders. The PPAR ligand receptor binders of this invention are useful as agonists or antagonists of the PPAR receptor.
    Type: Grant
    Filed: October 20, 2005
    Date of Patent: October 28, 2008
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Zaid Jayyosi, Gerard M. McGeehan, Michael F. Kelley, Richard F. Labaudiniere, Litao Zhang, Robert D. Groneberg, Daniel G. McGarry, Thomas J. Caulfield, Anne Minnich, Mark Bobko