Q Is Acyclic And Benzene Ring In A Substituent E Patents (Class 514/605)
  • Patent number: 7741520
    Abstract: Compounds and methods suppressing aromatase activity expression in cancer cells. Provided are compounds are those of formula I: wherein R1 may be alkyl, cycloalkyl, haloalkyl, aryl, substituted aryl, haloaryl, alkoxy, alkylaryl, and arylalkyl; R2 is H, alkyl, aryl, alkylaryl, arylalkyl, and cycloalkyl; R3, with the base nitrogen, forms an amide or sulfonamide; R4 is selected from nitro, amine, amide, and benzamide; or a pharmaceutically acceptable salts thereof. Also provided are small molecule selective aromatase inhibitors having a molecular weight of less 500 g/mol. In some embodiments, the small molecule selective aromatase inhibitors described herein have a molecular weight of less than 450 g/mol. Also provided are methods for suppressing aromatase activity expression in cancer cells comprising the step of administering a pharmaceutically effective amount of a small molecule aromatase inhibitor to a subject in need of such treatment. In one embodiment, the cancer cells are breast cancer cells.
    Type: Grant
    Filed: February 5, 2007
    Date of Patent: June 22, 2010
    Assignee: The Ohio State University Research Foundation
    Inventors: Robert W Brueggemeier, Bin Su, Edgar S Diaz-Cruz, Serena Landini
  • Publication number: 20100152297
    Abstract: The present invention relates to a composition for inhibiting cellular senescence, comprising N-[2-(cyclohexyloxyl)-4-nitrophenyl]-methanesulfonamide. During the progression of cellular senescence, the expression of COX-2 was decreased, whereas the enzymatic activity of COX-2 was increased, and the cellular senescence regulatory effects of the three selective COX-2 inhibitors had no connection with the concentration of intracellular reactive oxygen species, the activity of NF-?B and the amounts of p53 and p21 proteins. Rather, it was found that the three selective COX-2 inhibitors regulated the expression of caveolin-1 at the transcriptional level and regulated the intracellular total cholesterol concentration, and these results were closely connected with the cellular senescence regulatory effects of the three selective COX-2 inhibitors.
    Type: Application
    Filed: May 14, 2008
    Publication date: June 17, 2010
    Inventors: Sang Chul Park, Jeong A. Han
  • Publication number: 20100152296
    Abstract: The main goal of the present invention is the development of a polymerizable material for isolation and protection of the gums and generally the soft tissues of the oral cavity. For better protection during various procedures of the dental surfaces. The composition of the material can contain many other substances that strengthen its qualities and protective action. Such substances can be various substances that have antioxidative, sedative, anti-inflammatory, analgesic, anti-irritant action etc.
    Type: Application
    Filed: February 9, 2007
    Publication date: June 17, 2010
    Applicant: Klox Technologies Inc.
    Inventors: Vassilios Marmarinos, Paschalis Paschalakis, Irene Tseti
  • Publication number: 20100152256
    Abstract: The present invention relates to novel (2R)-2-phenylpropanamides bearing a 4-sulfonylamino substituent on the 4 position of the phenyl group and to pharmaceutical compositions containing them, which are used as inhibitors of the chemotaxis of polymorphonucleate and mononucleate cells, and which are useful in the treatment of various ELR+CXC chemokine-mediated disorders. In particular, the compounds of the invention are useful in the treatment and control of specific CXCR2 dependent pathologies such as BOS, COPD, angiogenesis and melanoma.
    Type: Application
    Filed: December 15, 2009
    Publication date: June 17, 2010
    Inventors: Marcello Allegretti, Riccardo Bertini, Cinzia Bizzarri, Maria Candida Cesta, Andrea Aramini, Alessio Moriconi
  • Publication number: 20100144681
    Abstract: The invention relates to substituted 1,2-ethylenediamines of general formula (I), wherein the radicals R1-R13, A, B, L and i are as defined in the description and the claims. The invention also relates to the use thereof for treating Alzheimer's disease (AD) and similar diseases.
    Type: Application
    Filed: August 8, 2006
    Publication date: June 10, 2010
    Inventors: Klaus Fuchs, Christian Eickmeier, Niklas Heine, Stefan Peters, Cornelia Dorner-Ciossek, Sandra Handschuh, Herbert Nar, Klaus Klinder
  • Publication number: 20100136031
    Abstract: The present invention provides methods of treating cancer by administering an IL8-CXCR1 pathway inhibitor (e.g., an anti-CXCR1 antibody or Repertaxin) alone or in combination with an additional chemotherapeutic agent such that non-tumorigenic and tumorigenic cancer cells in a subject are killed. The present invention also provides compositions and methods for detecting the presence of and isolating solid tumor stem cells in a patient (e.g., based on the presence of CXCR1 or FBXO21).
    Type: Application
    Filed: November 11, 2009
    Publication date: June 3, 2010
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Max S. Wicha, Christophe Ginestier
  • Publication number: 20100113449
    Abstract: The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (IA) or (IB): as further described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: October 28, 2009
    Publication date: May 6, 2010
    Applicant: Gilead Palo Alto, Inc.
    Inventors: Matthew Abelman, Elfatih Elzein, Robert Jiang, Rao Kalla, Tetsuya Kobayashi, Xiaofen Li, Thao Perry, Jeff Zablocki
  • Publication number: 20100113539
    Abstract: Provided are compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
    Type: Application
    Filed: October 21, 2009
    Publication date: May 6, 2010
    Applicant: Acucela, Inc.
    Inventors: Ian L. Scott, Vladimir Aleksandrovich Kuksa, Feng Hong, Ryo Kubota, Jennifer Gage
  • Publication number: 20100099769
    Abstract: The benzylamine derivative represented by the formula below and a pharmaceutically acceptable acid addition salt thereof, and a pharmaceutical containing the derivative or the pharmaceutically acceptable acid addition salt thereof, and a therapeutic or prophylactic agent for pollakiuria or urinary incontinence containing the derivative or the pharmaceutically acceptable acid addition salt thereof are provided. The benzylamine derivative of the present invention and the pharmaceutically acceptable acid addition salt thereof have less possibility of occurrence of side effects than known compounds, and show a better therapeutic effect against pollakiuria or urinary incontinence, so that they can be used as excellent therapeutic or prophylactic agents for pollakiuria or urinary incontinence.
    Type: Application
    Filed: January 31, 2008
    Publication date: April 22, 2010
    Applicant: TORAY INDUSTRIES, INC.
    Inventors: Ryoji Hayashi, Tsukasa Kikuchi, Masaki Arai, Satoshi Kurosawa, Ko Hasebe, Sayoko Kanie, Seiichiro Ozono, Atsushi Otsuka
  • Patent number: 7700654
    Abstract: A process for isolating N-butylbenzenesulfonamide (NBBS) from biological material, the chemical synthesis of benzenesulfonamide derivatives, the use of NBBS and benzenesulfonamide derivatives for treating benign prostatic hyperplasia and/or prostate carcinoma, the production of medicaments for the treatment thereof, and the use of NBBS and benzenesulfonamide derivatives as a lead substance in the development of active substances for treating benign prostatic hyperplasia and/or prostate carcinoma are provided.
    Type: Grant
    Filed: January 28, 2006
    Date of Patent: April 20, 2010
    Assignee: LTS Lohmann Therapie-Systeme AG
    Inventors: Hans-Rainer Hoffmann, Rudolf Matusch, Aria Baniahmad
  • Publication number: 20100035868
    Abstract: A method of treating or preventing a pathological condition of the uterus in an individual the method comprising administering to the individual any one or more of an inhibitor of cyclooxygenase-2 (COX-2), an inhibitor of prostaglandin E synthase (PGES), or an EP2 or EP4 receptor antagonist. Typically, the pathological condition is uterine cancer, fibroids or endometriosis.
    Type: Application
    Filed: October 6, 2009
    Publication date: February 11, 2010
    Applicant: MEDICAL RESEARCH COUNCIL
    Inventor: Henry Nicolas Jabbour
  • Publication number: 20100035880
    Abstract: This invention provides a compound of the formula (I): wherein A and B are independently CR12 or N; D and E are each independently CR9 or N; R1 represents (C1-C6)alkyl; R2 represents hydrogen, halogen, hydroxy, (C1-C6) alkyl, halo(C1-C6) alkyl, hydroxy(C1-C6)alkyl, (C1-C6)alkoxy or (C1-C6)alkoxy-(C1-C6)alkyl; R3, R4, R5, R6, R10 and R11 each independently represent hydrogen, halogen, (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkyl or (C1-C6)alkoxy-(C1-C6)alkyl; or R3 and R4 are taken together with the carbon atom to which they are attached to form a 3- to 7-membered carbocyclic ring or heterocyclic ring in which one or two non-adjacent carbon atoms are optionally replaced by an oxygen atom, a sulfur atom or NH; R7 and R9 each independently represent hydrogen, halogen, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkoxy, (C1-C6)alkylthio, (C1-C6)alkylsulfinyl, (C1-C6)alkylsulfonyl, NH2, [(C1-C6)
    Type: Application
    Filed: October 13, 2009
    Publication date: February 11, 2010
    Inventors: TAKESHI HANAZAWA, MISATO HIRANO, TADASHI INOUE, SATOSHI NAGAYAMA, KAZUNARI NAKAO, YUJI SHISHIDO, HIROTAKA TANAKA
  • Publication number: 20100015224
    Abstract: The present invention is concerned with a system for spatially and temporally programmable delivery of an active agent. When administered orally, the System can be retained in the gastric region for a prolonged period of time. It comprises of a core (I), one or more layers (II, IV, V) coated over the core and a preformed hollow space (III). The invention also concerns with a process for preparation of the System and a method for treating/preventing diseases, by administering to a subject in need thereof, the System of the invention.
    Type: Application
    Filed: September 3, 2007
    Publication date: January 21, 2010
    Inventors: Amarjit Singh, Sarabjit Singh, Shivanand Puthli, Rajendra Tandale
  • Patent number: 7645799
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, and ring B are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Grant
    Filed: November 7, 2008
    Date of Patent: January 12, 2010
    Assignee: Bristol-Myers Squibb Company
    Inventors: James R. Corte, Mimi L. Quan, Joanne M. Smallheer, Donald J. P. Pinto
  • Publication number: 20100004295
    Abstract: Disclosed is a novel compound having an NPY Y5 receptor antagonistic activity. A compound represented by the formula: a pharmaceutically acceptable salt or solvate thereof, wherein R1 is optionally substituted lower alkyl or the like, R2 and R8 are each independently hydrogen or lower alkyl, X is optionally substituted lower alkylene or the like, Y is —OCONR7— or the like, R7 is hydrogen, lower alkyl or the like, Z is optionally substituted carbocyclyl or the like, W is optionally substituted alkylene or the like.
    Type: Application
    Filed: August 28, 2007
    Publication date: January 7, 2010
    Inventor: Naoki Kouyama
  • Publication number: 20090281093
    Abstract: The present invention relates to novel non steroidal anti-inflammatory compounds (NSAIDs) that release hydrogen sulfide (H2S). The present invention also provides methods for treating, preventing and/or reducing inflammation-associated diseases by releasing H2S in the cardiovascular, connective tissue, pulmonary, gastrointestinal, respiratory, urogenital, nervous, or cutaneous systems as well as infective diseases employing said compounds.
    Type: Application
    Filed: July 29, 2005
    Publication date: November 12, 2009
    Applicant: C.T.G. PHARMA S.R.L.
    Inventors: Anna Sparatore, Piero Del Soldato
  • Publication number: 20090270508
    Abstract: The present invention provides for compositions and methods for modulating the GluR2 receptor. It is based, at least in part, on the discovery, by X-ray crystallography, that a known GluR2 agonist binds to the receptor in two different orientations, thereby diminishing its potency. The present invention provides for structural alternatives in which alternative binding possibilities are substantially eliminated.
    Type: Application
    Filed: January 30, 2009
    Publication date: October 29, 2009
    Inventors: James Eric Gouaux, Langzhou Song, Yuli Xie, Donald W. Landry
  • Publication number: 20090253739
    Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
    Type: Application
    Filed: June 10, 2009
    Publication date: October 8, 2009
    Inventors: Kim James, Lyn Howard Jones, David Anthony Price
  • Publication number: 20090215775
    Abstract: Compounds of formula (I) are disclosed for treatment of cancer.
    Type: Application
    Filed: May 16, 2006
    Publication date: August 27, 2009
    Inventors: Huw David Lewis, Timothy Harrison, Mark Steven Shearman
  • Publication number: 20090209619
    Abstract: The use of an HERG channel inhibitor for controlling the proliferation of cancer cells. Examples of such HERG channel inhibitors include dofetilide, cisapride, E-4031 and a siRNA molecule targeting a sequence involved in the expression of an HERG channel. Other ERG channels are also targets for these inhibitors.
    Type: Application
    Filed: October 14, 2005
    Publication date: August 20, 2009
    Inventors: Zhiguo Wang, Baofeng Yang
  • Patent number: 7572833
    Abstract: The present invention provides a preparation containing a compound of the formula (I) wherein R1 is an alkyl group having 1 to 4 carbon atoms or an optionally substituted aryl group having 6 to 10 carbon atoms; R2 and R3 are the same or different and each is hydrogen or an alkyl group having 1 to 4 carbon atoms, or R2 and R3 in combination form a ring having 3 to 7 carbon atoms; and R4 is a lower alkyl group optionally substituted by aryl, cycloalkyl or aromatic heterocyclic residue, or a pharmaceutically acceptable salt thereof together with a lipid. The preparation shows improved stability and improved absorption and penetration into tissue.
    Type: Grant
    Filed: September 27, 2001
    Date of Patent: August 11, 2009
    Assignee: Senju Pharmaceutical Co., Ltd.
    Inventors: Jun Inoue, Masazumi Yamaguchi
  • Publication number: 20090197912
    Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
    Type: Application
    Filed: April 8, 2009
    Publication date: August 6, 2009
    Inventors: Alan Daniel Brown, Mark Edward Bunnage, Paul Alan Glossop, Kim James, Charlotte Alice Louise Lane, Russel Andrew Lewthwaite, Ian Brian Moses, David Anthony Price, Nicholas Murray Thomson
  • Patent number: 7566739
    Abstract: This invention provides compounds of the formula (I) useful for the treatment of disease conditions caused by over activation of Vr1 receptors such as pain or the like in mammals as well as compositions comprising them.
    Type: Grant
    Filed: March 10, 2006
    Date of Patent: July 28, 2009
    Assignee: Pfizer Inc.
    Inventors: Takeshi Hanazawa, Misato Hirano, Tadashi Inoue, Satoshi Nagayama, Kazunari Nakao, Yuji Shishido, Hirotaka Tanaka
  • Patent number: 7560459
    Abstract: The present invention is directed to novel compounds of the formula (I) wherein X, R1, R2, R3, R4, R5 and R6 are as described in the specification, processes for the preparation of and pharmaceutical compositions comprising said derivatives. The compounds of the present invention are useful for the treatment of epilepsy. The invention is further directed to a process for the preparation of compounds of formula (XX), wherein X, R3, R4, R5 and R6 are as described in the specification.
    Type: Grant
    Filed: November 2, 2005
    Date of Patent: July 14, 2009
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Ahmed Abdel-Magid, Cynthia Maryanoff, Steven Mehrman, Allen B. Reitz, Bruce Maryanoff
  • Patent number: 7544717
    Abstract: Disclosed are compounds of the formula: where variables Q, Z, X, R15, R2, R3, and Rc are defined herein. Compounds disclosed herein are inhibitors of the beta-secretase enzyme and are therefore useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal.
    Type: Grant
    Filed: March 25, 2005
    Date of Patent: June 9, 2009
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: Roy Hom, John Tucker, Varghese John, Neerav Shah
  • Patent number: 7541383
    Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of inflammatory and immune-related diseases and conditions. In particular, the invention provides compounds which modulate the function and/or expression of proteins involved in atopic diseases, inflammatory conditions and cancer. The subject compounds are carboxylic acid derivatives.
    Type: Grant
    Filed: November 26, 2007
    Date of Patent: June 2, 2009
    Assignee: Amgen Inc.
    Inventors: Zice Fu, Xi Alan Huang, Jiwen Liu, Julio C. Medina, Michael J. Schmitt, H. Lucy Tang, Yingcai Wang, Qingge Xu
  • Publication number: 20090124664
    Abstract: The present invention relates to selected (R)-arylalkylamino derivatives of formula (I), in which R, R1 and Ar are as defined in the claims. These compounds show a surprising potent inhibitory effect on C5a induced human PMN chemotaxis. The compounds of the invention absolutely lack of CXCL8 inhibitory activity. Said compounds are useful in the treatment of pathologies depending on the chemotactic activation of neutrophils and monocytes induced by the fraction C5a of the complement. In particular, the compounds of the invention are useful in the treatment of sepsis, psoriasis, rheumatoid arthritis, ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of injury caused by ischemia and reperfusion.
    Type: Application
    Filed: November 24, 2006
    Publication date: May 14, 2009
    Inventors: Marcello Allegretti, Alessio Moriconi, Andrea Aramini, Maria Candida Cesta, Andrea Beccari, Riccardo Bertini
  • Patent number: 7528170
    Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
    Type: Grant
    Filed: July 3, 2007
    Date of Patent: May 5, 2009
    Assignee: Pfizer Inc.
    Inventors: Alan Daniel Brown, Mark Edward Bunnage, Paul Alan Glossop, Kim James, Charlotte Alice Louise Lane, Russel Andrew Lewthwaite, Ian Brian Moses, David Anthony Price, Nicholas Murray Thomson
  • Publication number: 20090082456
    Abstract: Disclosed are amide, thioamide, urea and thiourea compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, and diabetic-related diseases.
    Type: Application
    Filed: September 9, 2008
    Publication date: March 26, 2009
    Inventor: Richard D. Gless, JR.
  • Publication number: 20090062244
    Abstract: Topical composition for enhanced local and systemic delivery of poorly soluble biologically active compounds, comprises of non-volatile solvent or mixture of solvents to dissolve active component, and moisture absorbent or mixture of sorbents to prevent precipitation or crystallization of insoluble material after application
    Type: Application
    Filed: September 4, 2007
    Publication date: March 5, 2009
    Inventors: Joseph Schwarz, Michael Weisspapir
  • Publication number: 20090047346
    Abstract: Sustained release compositions of sotalol, or a pharmaceutically acceptable salt thereof, are provided. In certain examples, sotalol, or a pharmaceutically acceptable salt thereof, may be administered in an effective amount to provide a therapeutic effect to a patient, such as, for example, a patient suffering from a cardiac disorder. In some examples, sotalol combined with a sustained release system may be administered to provide a sustained release of sotalol for a desired period, e.g., at least about 24 hours.
    Type: Application
    Filed: September 5, 2008
    Publication date: February 19, 2009
    Inventor: Bramah N. Singh
  • Publication number: 20090047243
    Abstract: The invention features compositions and methods employing combinations of an A2A receptor agonist and a PDE inhibitor for the treatment of a B-cell proliferative disorder, e.g., multiple myeloma.
    Type: Application
    Filed: July 17, 2008
    Publication date: February 19, 2009
    Inventors: Richard Rickles, Laura Pierce, Margaret S. Lee
  • Publication number: 20090035315
    Abstract: Improved treatments of joint diseases, such as, e.g.
    Type: Application
    Filed: June 17, 2005
    Publication date: February 5, 2009
    Inventors: Stephan Christgau, Christian Hansen, Henrik Nilsson
  • Publication number: 20090030083
    Abstract: N-(2-aryl-propionyl)-sulfonamides of general formula (I): are useful in the treatment of spinal cord injury.
    Type: Application
    Filed: March 17, 2005
    Publication date: January 29, 2009
    Applicant: Dompe' pha.r.ma S.p.A
    Inventors: Riccardo Bertini, Francesco Colotta
  • Publication number: 20090023791
    Abstract: NMDA receptor blockers, including pH-sensitive NMDA receptor blockers, are provided as neurprotective drugs that are useful in stroke, traumatic brain injury, epilepsy, and other neurologic events that involve acidification of brain or spinal cord tissue. Compositions and methods of this invention are used for treating neurodegeneration resulting from NMDA receptor activation. The compounds described herein have enhanced activity in brain tissue having lower than normal pH due to pathological conditions such as hypoxia resulting from stroke, traumatic brain injury, global ischemia that may occur during cardiac surgery, hypoxia that may occur following cessation of breathing, pre-eclampsia, spinal cord trauma, epilepsy, chrounic pain, vascular dementia and glioma rumors.
    Type: Application
    Filed: May 8, 2008
    Publication date: January 22, 2009
    Applicant: Emory University
    Inventors: Stephen F. Traynelis, Dennis C. Liotta, James P. Snyder, Yesim Altas, David D. Mott, James J. Doherty, JR., Raymond J. Dingledine
  • Patent number: 7479508
    Abstract: This invention relates to compositions of nimesulide for topical application.
    Type: Grant
    Filed: August 25, 2004
    Date of Patent: January 20, 2009
    Assignee: EDKO Trading and Representation Company Limited
    Inventors: Koral Embil, Ray Figueroa
  • Publication number: 20090018057
    Abstract: Oil-in-water emulsion comprising a non-steroidal anti-inflammatory drug and a quaternary ammonium halide useful for the prevention and treatment of inflammation in the eye, and process for manufacturing thereof.
    Type: Application
    Filed: July 9, 2007
    Publication date: January 15, 2009
    Inventors: Gregory LAMBERT, Laura RABINOVICH-GUILATT, Frederic LALLEMAND, Jean-Sebastien GARRIGUE
  • Publication number: 20080312286
    Abstract: The present invention is directed to compounds which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
    Type: Application
    Filed: July 26, 2005
    Publication date: December 18, 2008
    Inventors: Anthony B. Pinkerton, Jean-Michel Vernier, Rowena Cube, John Hutchinson, Celine Bonnefous, Theodore Kamenecka
  • Patent number: 7453010
    Abstract: The invention relates to compounds of general formula (I): where R1 represents H or a (C1-C4)alkyl, —CO(C1-C4)alkyl, (C1-C4)alkylphenyl or —CO-phenyl group, said phenyl optionally being substituted; R2 represents H, a halogen atom, an —S(O)z(C1-C4)alkyl group, where z is equal to 0, 1 or 2, an —NHSO2(C1-C4)alkyl group, an —NHSO2-phenyl group or an —NHSO2—(C1-C4)alkylphenyl group, said phenyl optionally being substituted; R3 represents an —X—R4 group—in which X represents a bond, an oxygen atom or a —CH2— group and R4 represents H or a —CR5R6—COOR7 group, where R5, R6 and R7 independently represent H or a (C1-C4)alkyl group—a phenyl group optionally substituted or fused with a dioxolane group, a —CO—NR8R9 group—where R8 represents H, a (C1-C4)alkyl group or a (C1-C4)alkyl(C1-C4)alkoxy group and R9 represents a (C1-C4)alkyl(C1-C4)alkoxy group, a —(CH2)n-A group, where n is equal to 0, 1, 2, 3 or 4 and where A represents an indolyl group, a fluorenyl group or a phenyl group which is substituted, an optiona
    Type: Grant
    Filed: May 26, 2003
    Date of Patent: November 18, 2008
    Assignee: Sanofi Aventis
    Inventors: Philippe R. Bovy, Roberto Cecchi, Tiziano Croci, Olivier Venier
  • Publication number: 20080267970
    Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
    Type: Application
    Filed: July 3, 2007
    Publication date: October 30, 2008
    Inventors: Alan Daniel Brown, Mark Edward Bunnage, Paul Alan Glossop, Kim James, Charlotte Alice Louise Lane, Russel Andrew Lewthwaite, Ian Brian Moses, David Anthony Price, Nicholas Murray Thomson
  • Publication number: 20080262048
    Abstract: Novel trifluoromethanesulfonanilide oxime ether compounds useful for controlling endo and/or ectoparasites in the environment are provided, together with methods of making the same, and methods of using the inventive compounds to treat parasite infestations in vivo or ex vivo.
    Type: Application
    Filed: October 31, 2007
    Publication date: October 23, 2008
    Inventors: Adam Gerhard Meyer, Kevin Norman Winzenberg, David G. Sawutz, Andris Juris Liepa
  • Publication number: 20080261956
    Abstract: The present invention relates to methods, compounds, and compositions for inhibiting angiogenesis. More particularly, the present invention relates to methods, compounds, and compositions for inhibiting VEGF production.
    Type: Application
    Filed: November 23, 2005
    Publication date: October 23, 2008
    Inventors: Soongyu Choi, Young-Choon Moon, Nadarajan Tamilarasu
  • Publication number: 20080249102
    Abstract: Compounds of the formula I: wherein R1, R2, X and N are as defined in the specification; E is N, CH; A? and A? are terminal groups as defined in the specification. The compounds have utility as HIV-1 protease inhibitors.
    Type: Application
    Filed: February 9, 2006
    Publication date: October 9, 2008
    Inventors: Jenny Ekegren, Anders Hallberg, Hans Wallberg, Bertil Samuelsson, Mahalingam Kannan
  • Publication number: 20080234383
    Abstract: This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receotor 1; VR1; TRPV1) antagonist; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, and heart disease.
    Type: Application
    Filed: March 17, 2006
    Publication date: September 25, 2008
    Inventors: Young-Ger Suh, Hee-Doo Kim, Hyeung-Geun Park, Uh Taek Oh, Yong-Sil Lee, Seol Rin Park, Chong Hyon Ryu, Young-Ho Park, Song Seok Shin, Sun-Young Kim, Jin Kwan Kim, Yeon Su Jeong, Ki-Wha Lee, Jin Kyu Choi, Kyung Min Lim, Hyun Ju Koh, Joo Hyun Moh, Sung-II Kim, Joon Ho Bae
  • Patent number: 7417169
    Abstract: The present invention provides compounds represented by general formula (I): a prodrug thereof, or pharmaceutical acceptable salts thereof, wherein R1 is hydrogen or lower alkyl; each of R2 and R3 is independently hydrogen or lower alkyl; each of R4, R5 and R6 is independently hydrogen, halogen, lower alkyl or lower alkoxy; R7 is hydrogen or lower alkyl; R8 is hydrogen, halogen, lower alkyl, lower alkoxy, etc; R9 is —COR10, -A1-COR10, —O-A2-COR10, etc; Ar is optionally substituted phenyl or heteroaryl; and A is a bond, —OCH2—, etc, which exhibit potent and selective ?3-adrenoceptor stimulating activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.
    Type: Grant
    Filed: October 5, 2004
    Date of Patent: August 26, 2008
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Junichi Kobayashi, Tetsuya Nakamura, Hideyuki Muranaka, Takehiro Ishikawa, Tetsuro Tamai, Satoshi Akahane
  • Publication number: 20080167351
    Abstract: This invention relates to potentiation of the glutamate receptor by novel compounds of formula (I): The invention also relates to the use of the derivatives in treating diseases and conditions mediated by potentiation of the glutamate receptor, compositions containing the derivatives and processes for their preparation.
    Type: Application
    Filed: February 13, 2006
    Publication date: July 10, 2008
    Inventors: Daniele Andreotti, Luca Arista, Francesca Cardullo, Simone Spada, Kevin Michael Thewlis, Simon Edward Ward
  • Publication number: 20080160082
    Abstract: A controlled release pharmaceutical composition for peroral administration including a single unit fast release fraction and a single unit extended release fraction which includes nimesulide as an active drug upto 99% w/w of the composition, one or more release controlling materials from 0.1% to 99% w/w of the composition and pharmaceutical excipients from 0% to 90% w/w of the composition. The nimesulide is present in the fast release fraction and in the extended release fraction.
    Type: Application
    Filed: October 26, 2007
    Publication date: July 3, 2008
    Inventors: Amarjit Singh, Rajesh Jain
  • Patent number: 7388031
    Abstract: The present invention relates to the compounds of formula (I): in which A is a group of formula (a) or (b) in which R represents a hydrogen or halogen atom, an —S(O)z(C1–C4)alkyl group, an —NHSO2(C1–C4)alkyl group, an —SO2NH(C1–C4)alkyl group, an —NHSO2phenyl-(C1–C4)alkyl group or an —NHSO2phenyl group, said phenyl possibly being substituted with a halogen atom, with a (C1–C4)alkyl group or with a (C1–C4)alkoxy group; R1 represents a hydrogen atom or a (C1–C4)alkyl group, a —CO(C1–C4)alkyl group, a phenyl-(C1–C4)alkyl group or a —COphenyl group, said phenyl also possibly being substituted with a halogen atom or with a (C1–C4)alkoxy group; R2 is a hydrogen atom or an —SO2(C1–C4)alkyl group, an —SO2phenyl-(C1–C4)alkyl group or an —SO2phenyl group; X completes a ring of 5 to 8 atoms, said ring being saturated or unsaturated, possibly being substituted with one or two (C1–C4)alkyl groups and bearing one or two carbonyl groups; n, m and z are, independently, 0, 1 or 2; R3 represents a hydrogen or halogen
    Type: Grant
    Filed: November 30, 2001
    Date of Patent: June 17, 2008
    Assignee: Sanofi-Aventis
    Inventors: Philippe R. Bovy, Roberto Cecchi, Gilles Courtemanche, Tiziano Croci, Ambrogio Oliva, Nunzia Viviani
  • Patent number: 7375136
    Abstract: NMDA receptor blockers, including pH-sensitive NMDA receptor blockers, are provided as neuroprotective drugs that are useful in stroke, traumatic brain injury, epilepsy, and other neurologic events that involve acidification of brain or spinal cord tissue. Compositions and methods of this invention are used for treating neurodegeneration resulting from NMDA receptor activation. The compounds described herein have enhanced activity in brain tissue having lower-than normal pH due to pathological conditions such as hypoxia resulting from stroke, traumatic brain injury, global ischemia that may occur during cardiac surgery, hypoxia that may occur following cessation of breathing, pre-eclampsia, spinal cord trauma, epilepsy, chronic pain, vascular dementia and glioma tumors.
    Type: Grant
    Filed: March 8, 2002
    Date of Patent: May 20, 2008
    Assignee: Emory University
    Inventors: Stephen F. Traynelis, Dennis C. Liotta, James P. Snyder, Yesim Altas, David D. Mott, James J. Doherty, Jr., Raymond J. Dingledine
  • Patent number: 7375120
    Abstract: Novel PDF inhibitors and novel methods for their use are provided.
    Type: Grant
    Filed: April 16, 2003
    Date of Patent: May 20, 2008
    Assignee: Smithkline Beecham Corporation
    Inventors: Siegfried B. Christensen, IV, Maxwell D. Cummings, Jinhwa Lee, Jia-ning Xiang