Bicyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos Patents (Class 546/112)
Plural ring hetero atoms in the bicyclo ring system (Class 546/113)
Tropanes (including nor and dehydro forms) (Class 546/124)
Quinuclidines (including unsaturated) (Class 546/133)
Quinolizines (including hydrogenated) (Class 546/138)
Isoquinolines (including hydrogenated) (Class 546/139)
Quinolines (including hydrogenated) (Class 546/152)
Chalcogen bonded directly to ring carbon of the bicyclo ring system (Class 546/183)
  • 2-aza-bicyclo[2.2.1]heptane derivatives
    Patent number: 8236801
    Abstract: The invention relates to novel 2-aza-bicyclo[2.2.1]heptane derivatives of formula (I), wherein A, B, n and R1 are as described in the description, and to the use of such compounds, or of pharmaceutically acceptable salts of such compounds, as medicaments, especially as orexin receptor antagonists.
    Type: Grant
    Filed: February 19, 2009
    Date of Patent: August 7, 2012
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Hamed Aissaoui, Christoph Boss, Ralf Koberstein, Thierry Sifferlen, Daniel Trachsel
  • Dihydro-[1H]-quinolin-2-one derivatives as RXR agonists for the treatment of dyslipidemia, hypercholesterolemia and diabetes
    Patent number: 8236819
    Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating RXR mediated disorders. More particularly, the compounds of the present invention are RXR agonists useful for treating RXR mediated disorders.
    Type: Grant
    Filed: November 13, 2009
    Date of Patent: August 7, 2012
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Bharat Lagu, Rimma Lebedev, Barbara Pio
  • Therapeutic isoxazole compounds
    Patent number: 8222243
    Abstract: The invention provides a compound of formula I: wherein A1, A2, A3, R1, X, Y, and B have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of monoamine oxidase B (MAO-B) enzyme function and are useful for improving cognitive function and for treating psychiatric disorders in animals.
    Type: Grant
    Filed: August 26, 2008
    Date of Patent: July 17, 2012
    Assignee: Dart NeuroScience (Cayman) Ltd
    Inventors: Alan P. Kaplan, Terence P. Keenan, Andrew J. McRiner
  • Method of producing aromatic compound
    Patent number: 8212048
    Abstract: A method of producing an aromatic compound of the following formula (3) comprising reacting a compound of the following formula (1) with an olefin compound of the following formula (2) in the presence of a transition metal complex: (wherein, an Ar1 ring represents an aromatic hydrocarbon ring or aromatic heterocyclic ring, an Ar2 ring represents a heterocyclic ring containing X1 and N*, and the X1 represents a nitrogen atom or carbon atom and the N represents a nitrogen atom connecting via a double bond to either one of two adjacent atoms in the Ar2 ring.) (wherein, R1, R2, R3 and R4 represent each independently a hydrogen atom, an alkyl group having 1 to 10 carbon atoms or an aryl group having 6 to 18 carbon atoms.) (wherein, Ar1, Ar2, X1, N*, R1, R2 and R3 represent the same meanings as described above.).
    Type: Grant
    Filed: February 2, 2007
    Date of Patent: July 3, 2012
    Assignees: Sumitomo Chemical Company, Limited, Osaka University
    Inventors: Fumitoshi Kakiuchi, Yusuke Matsuura, Masato Ueda
  • NEW HETEROCYCLIC DERIVATIVE AND ORGANIC LIGHT EMITTING DEVICE USING SAME
    Publication number: 20120161612
    Abstract: The present invention relates to a novel heterocyclic derivative and an organic light emitting device using the compound, and the heterocyclic derivative may largely improve a life span, efficiency, electrochemical stability and thermal stability of the organic light emitting device.
    Type: Application
    Filed: September 10, 2010
    Publication date: June 28, 2012
    Inventors: Ji-Eun Kim, Kong-Kyeom Kim, Se-Hwan Son, Jun-Gi Jang
  • LUMINOPHORES
    Publication number: 20120157681
    Abstract: There is described novel organo-platinum luminophores comprising a complex of formula I: The luminophores have application as the emissive component in organic light emitting diodes.
    Type: Application
    Filed: December 16, 2011
    Publication date: June 21, 2012
    Applicant: UNIVERSITY OF YORK
    Inventors: Duncan W. Bruce, Valery Kozhevnikov
  • USE OF AZABICYCLOALKYL DERIVATIVES OR PYRROLIDINE-2-ONE DERIVATIVES FOR THE TREATMENT OR PREVENTION OF ATAXIA
    Publication number: 20120157464
    Abstract: The invention concerns the use of azabicycloalkyl derivatives or pyrrolidine-2-one derivatives for the treatment, prevention or delay of progression of ataxia.
    Type: Application
    Filed: July 21, 2010
    Publication date: June 21, 2012
    Inventors: Dominik Feuerbach, Baltazar Gomez-Mancilla
  • NOVEL COMPOUNDS
    Publication number: 20120149676
    Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, L, M, W, R1, R2, R3, R4, R6, R7, R9, Ra, Rb have meanings given in the description.
    Type: Application
    Filed: December 8, 2011
    Publication date: June 14, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Henning PRIEPKE, Henri DOODS, Alexander HEIM-RIETHER, Raimund KUELZER, Roland PFAU, Klaus RUDOLF, Dirk STENKAMP
  • Sub-type selective azabicycloalkane derivatives
    Patent number: 8198296
    Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are amide, ketone, and ester compounds prepared from certain azabicycloalkane carboxylic acids. The resulting compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the ?4?2 subtype in the central nervous system (CNS). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, such as those disorders characterized by dysfunction of nicotinic cholinergic neurotransmission, including disorders involving neuromodulation of neurotransmitter release, such as dopamine release. CNS disorders, which are characterized by an alteration in normal neurotransmitter release, are another example of disorders that can be treated and/or prevented.
    Type: Grant
    Filed: March 27, 2008
    Date of Patent: June 12, 2012
    Assignee: Targacept, Inc.
    Inventors: Philip S. Hammond, Anatoly Mazurov, Yun-De Xiao, Srinivasa V. Murthy, Srinivisa Rao Akireddy
  • 3-substituted sulfonyl piperidine derivative
    Patent number: 8188280
    Abstract: [Problem] There is provided a compound useful as a preventive or remedy for cardiovascular disease, neurologic disease, metabolic disease, reproductive disease, and digestive disease. [Means for Resolution] A compound or a pharmaceutically acceptable salt thereof represented by the following Formula (I) wherein Z represents wherein n1, n2, and n3 are 0, 1, or 2, respectively; R1 represents C1-6 alkyl, C3-8 cycloalkyl, or the like; R2 represents aryl or heteroaryl; R3 represents a hydrogen atom, C1-6 alkyl, or the like; and M1, M2, M3, and M4 independently represent a hydrogen atom, C1-6 alkyl, or the like, or M1, together with M2, M3, or M4, forms —CH2— or the like.
    Type: Grant
    Filed: February 4, 2009
    Date of Patent: May 29, 2012
    Assignee: MSD K.K.
    Inventors: Tsuyoshi Nagase, Takahide Sasaki, Toshiyuki Takahashi
  • BENZENESULFONYL OR SULFONAMIDE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO THE MODULATION OFTHE SEROTONIN 5-HT6 RECEPTOR
    Publication number: 20120129883
    Abstract: The present invention relates to benzenesulfonyl or sulfonamide compounds of formulae IA and IB wherein the variables have the meanings given in the claims and the description, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT6 receptor.
    Type: Application
    Filed: November 1, 2011
    Publication date: May 24, 2012
    Applicants: Abbott Laboratories, Abbott GmbH & Co. KG
    Inventors: Andreas Haupt, Frauke Pohlki, Liliane Unger, Ana Lucia Relo, Karsten Wicke, Min Zhang
  • Pesticidal Arylpyrrolidines
    Publication number: 20120129854
    Abstract: The invention is directed to arylpyrrolidines compounds which exhibit excellent insecticidal efficacy and which may be used as in the agrochemical field or in the yield of veterinary medicine. The compounds are represented by formula (I): wherein the respective substituents are defined in the specification.
    Type: Application
    Filed: April 27, 2010
    Publication date: May 24, 2012
    Applicant: Bayer CropScience AG
    Inventors: Jun Mihara, Tetsuya Murata, Daiei Yamazaki, Yasushi Yoneta, Koichi Araki, Norio Sasaki, Kei Domon, Mamoru Hatazawa, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya, Ulrich Görgens
  • COMPOUND FOR INHIBITING ACTIVITY OF RIBONUCLEASE, AND CONTAINER FOR STORING NUCLEIC ACID CONTAINING THE SAME
    Publication number: 20120114535
    Abstract: Provided are an RNase activity inhibitory compound to effectively control the activity of the RNase promoting degradation of extracted RNAs and, in addition, a sample storage container including the same. The RNase activity inhibitory compound and the sample storage container according to the present invention may be effectively used to store RNAs during RNA extraction or the extracted RNAs.
    Type: Application
    Filed: June 12, 2009
    Publication date: May 10, 2012
    Applicant: BIONEER CORPORATION
    Inventors: Jong Hoon Kim, Hwangseo Park, Han Oh Park
  • 1-aza-bicycloalkyl derivatives
    Patent number: 8173667
    Abstract: The present invention provides a compound of formula (I) where X, R, Y, D, A and B are as defined herein.
    Type: Grant
    Filed: October 19, 2006
    Date of Patent: May 8, 2012
    Assignee: Novartis AG
    Inventors: Dominik Feuerbach, Mathias Frederiksen, Martin Marzi, Bernard Lucien Roy
  • Azabicycloalkane derivatives, preparation thereof and use thereof in therapy
    Patent number: 8173669
    Abstract: The invention relates to compounds of the general formula (I): Wherein R, m, n and o are as defined herein. The invention also relates to a method for preparing the same and to the application in therapy.
    Type: Grant
    Filed: August 4, 2009
    Date of Patent: May 8, 2012
    Assignee: Sanofi-Aventis
    Inventors: Omar Ben Ayad, Odile Leclerc, Alistair Lochead, Mourad Saady, Franck Slowinski, Julien Vache
  • Inhibitors of AKT activity
    Patent number: 8168652
    Abstract: The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
    Type: Grant
    Filed: March 3, 2010
    Date of Patent: May 1, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Philip E. Sanderson, Mark E. Layton, Kevin J. Rodzinak
  • Helix 12 directed non-steroidal antiandrogens
    Patent number: 8168627
    Abstract: Compounds having the structure (or their salts): are used to treat or reduce the likelihood of acquiring androgen-dependent diseases, such as prostate cancer, benign prostatic hyperplasia, polycystic ovarian syndrome, acne, hirsutism, seborrhea, androgenic alopecia and male baldness. The compounds can be formulated together with pharmaceutically acceptable diluents or carriers or otherwise made into any pharmaceutical dosage form. Combinations with other active pharmaceutical agents are also disclosed.
    Type: Grant
    Filed: March 16, 2010
    Date of Patent: May 1, 2012
    Assignee: Endorecherche, Inc.
    Inventors: Fernand Labrie, Rock Breton, Shankar Mohan Singh, Rene Maltais
  • THERAPEUTIC AGENT FOR MOTOR DISORDERS
    Publication number: 20120101101
    Abstract: Provided are an agent for the treatment and/or prophylaxis of a movement disorder, the agent for the treatment and/or prophylaxis wherein the movement disorder is extrapyramidal syndrome, the agent for the treatment and/or prophylaxis wherein the movement disorder is bradykinesia, gait disturbance, dystonia, dyskinesia or tardive dyskinesia, the agent for the treatment and/or prophylaxis wherein the movement disorder is a side effect of L-DOPA and/or dopamine agonist therapy, and the like, each containing a thiazole derivative represented by the formula (I) wherein R1 represents aryl and the like, and R2 represents pyridyl or the like, or a pharmaceutically acceptable salt thereof as an active ingredient.
    Type: Application
    Filed: April 28, 2010
    Publication date: April 26, 2012
    Applicant: KYOWA HAKKO KIRIN CO., LTD.
    Inventors: Noriaki Uesaka, Takashi Sawada, Tomoyuki Kanda
  • N-(amino-heteroaryl)-1H-pyrrolopyridine-2-carboxamides derivatives preparation thereof and their use in therapy
    Patent number: 8153650
    Abstract: The invention relates to compounds of the general formula (I): Wherein X, Y, Z, Z1, Z2, Z3, Z4 and n are as defined herein. The invention also relates to a method for making the same and to the use thereof in therapy.
    Type: Grant
    Filed: June 23, 2009
    Date of Patent: April 10, 2012
    Assignee: Sanofi-Aventis
    Inventors: Laurent Dubois, Yannick Evanno, Catherine Gille, David Machnik, André Malanda
  • Chromen-2-one derivatives and their use as monoamine neurotransmitter re-uptake inhibitors
    Patent number: 8153797
    Abstract: This invention relates to novel chromen-2-one derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Grant
    Filed: February 13, 2007
    Date of Patent: April 10, 2012
    Assignee: Neurosearch A/S
    Inventors: Dan Peters, John Paul Redrobe, Elsebet Østergaard Nielsen
  • Azaindoles having serotonin receptor affinity
    Patent number: 8148394
    Abstract: Described herein are compounds with affinity for the 5-HT6 receptor, which have the general formula I: wherein A, B, D, E, R1 to R3 and n are described herein. Also described is the use of these compounds as pharmaceuticals to treat indications where inhibition of the 5-HT6 receptor is implicated, such as schizophrenia.
    Type: Grant
    Filed: August 7, 2007
    Date of Patent: April 3, 2012
    Assignee: NPS Pharmaceuticals, Inc.
    Inventors: Louise Edwards, Abdelmalik Slassi, Ashok Tehim, Tao Xin
  • Heteroaryl derivatives of N-{[(1S,4S,6S)-3-(2-pyridinylcarbonyl)-3-azabicyclo[4.1.0]hept-4-yl]methyl}-2-amine
    Patent number: 8133908
    Abstract: Disclosed are N-{[(1S,4S,6S)-3-(2-pyridinylcarbonyl)-3-azabicyclo[4.1.0]hept-4-yl]methyl}-2-heteroarylamine derivatives having the following formula: wherein m, n, Het, R1, R2 and R3 are as defined herein, and their use as orexin antagonists.
    Type: Grant
    Filed: November 30, 2009
    Date of Patent: March 13, 2012
    Assignee: Glaxo Group Limited
    Inventors: Giuseppe Alvaro, David Amantini, Emiliano Castiglioni, Romano Di Fabio, Francesca Pavone
  • BACE 2 INHIBITORS
    Publication number: 20120053200
    Abstract: The present invention relates to N-1-Benzyl-2-hydroxy-3-(hetero)arylamino-propyl)-isophthalamides of formula I having BACE2 inhibitory activity and their use as therapeutically active substances, their manufacture and pharmaceutical compositions. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. type 2 diabetes.
    Type: Application
    Filed: August 23, 2011
    Publication date: March 1, 2012
    Inventors: Harald Mauser, Matthias Nettekoven, Sébastien Schmitt
  • Intermediate products for producing oxazolidinone-quinolone hybrids
    Patent number: 8124772
    Abstract: The present invention describes intermediates (ZP) for a novel and efficient synthesis of compounds in which the pharmacophores of quinolone and oxazolidinone are linked to one another by way of a chemically stable linker.
    Type: Grant
    Filed: June 5, 2009
    Date of Patent: February 28, 2012
    Assignee: Morphochem Aktiengesellschaft für Kombinatorische Chemie
    Inventors: Christian Hubschwerlen, Jean-Luc Specklin, Jean Phillippe Surivet, Daniel Baeschlin
  • Substituted disulfonamide compounds
    Patent number: 8119805
    Abstract: Substituted disulfonamide compounds corresponding to formula I: In which R1, R2, R3, R4a, R4b, R5a, R5b, R8, R9a, R9b, R10, R11, a, b, s, t and A have defined meanings, pharmaceutical compositions containing one or more such compounds, processes for preparing such compounds, and a method of using such compounds for the treatment or inhibition of pain and/or other conditions mediated by the bradykinin receptor 1 (BR1).
    Type: Grant
    Filed: November 6, 2009
    Date of Patent: February 21, 2012
    Assignee: Gruenenthal GmbH
    Inventors: Melanie Reich, Stefan Schunk, Ruth Jostock, Sabine Hees, Tieno Germann, Michael Franz-Martin Engels
  • 3-AZABICYCLO [4.1.0] HEPTANES USED AS OREXIN ANTAGONISTS
    Publication number: 20120040991
    Abstract: Disclosed are 3-azabicyclo[4.1.0]heptane derivatives of formula (I) and their use as orexin receptor antagonists.
    Type: Application
    Filed: April 23, 2010
    Publication date: February 16, 2012
    Applicant: Glaxo Group Limited
    Inventors: David Amantini, Romano Di Fabio, Massimo Gianotti, Francesca Pavone, Francesco Ferroni
  • Compounds comprising heterocyclic-substituted piperidine for treating pain
    Patent number: 8110602
    Abstract: The invention relates to Heterocyclic-Substituted Piperidine Compounds, compositions comprising an effective amount of a Heterocyclic-Substituted Piperidine Compound and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Heterocyclic-Substituted Piperidine Compound.
    Type: Grant
    Filed: July 15, 2009
    Date of Patent: February 7, 2012
    Assignee: Purdue Pharma L.P.
    Inventors: Kevin C. Brown, R. Richard Goehring, Yoshiyasu Baba, Naoki Tsuno
  • Indazoles, benzothiazoles, benzoisothiazoles, benzisoxazoles, pyrazolopyridines, isothiazolopyridines, and preparation and uses thereof
    Patent number: 8106066
    Abstract: The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (e.g., indazoles and benzothiazoles), which act as ligands for the ?7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
    Type: Grant
    Filed: September 22, 2006
    Date of Patent: January 31, 2012
    Assignee: Memory Pharmaceuticals Corporation
    Inventors: Richard Schumacher, Mihaela Diana Danca, Jianguo Ma, Brian Herbert, True Minh Nguyen, Wenge Xie, Ashok Tehim
  • Indolizine derivatives and the use thereof as antidiabetics
    Patent number: 8106067
    Abstract: Novel compounds of the formula (I), in which X, Y, R, R1, R1, R1?, R2, R2?, R3, R4, R4?, R5 and n have the meanings indicated in patent claim 1, are suitable as antidiabetics.
    Type: Grant
    Filed: November 17, 2007
    Date of Patent: January 31, 2012
    Assignee: Merck Patent GmbH
    Inventors: Werner Mederski, Norbert Beier, Lars Thore Burgdorf, Rolf Gericke, Markus Klein, Christos Tsaklakidis
  • N[S(4-aryl-triazol-3-yl)?-mercaptoacetyl]-amino benzoic acids as HIV reverse transcriptase inhibitors
    Patent number: 8106205
    Abstract: A series of S-triazolyl ?-mercaptoacetanilides having N-(?-mercaptoacetyl) p amino benzoic acid derivatives. are provided, where Q is CO2H, or a salt or ester thereof, or a C(O) N-linked amino acid. The compounds inhibit several variants of the reverse transcriptase of HIV, and are useful in the treatment of HIV infections.
    Type: Grant
    Filed: February 2, 2010
    Date of Patent: January 31, 2012
    Assignee: Ardea Biosciences, Inc.
    Inventors: Jean-Luc Girardet, Yung-hyo Koh, Martha De La Rosa, Zhi Hong, Stanley Lang
  • NOVEL SUBSTITUTED INDANES, METHOD FOR THE PRODUCTION THEREOF, AND USE THEREOF AS DRUGS
    Publication number: 20120022039
    Abstract: The invention relates to substituted indanes and derivatives thereof, to physiologically acceptable salts and physiologically functional derivatives thereof, to the production thereof, to drugs containing at least one substituted indane according to the invention or derivative thereof, and to the use of the substituted indanes according to the invention and to derivatives thereof as MCH antagonists.
    Type: Application
    Filed: February 12, 2010
    Publication date: January 26, 2012
    Applicant: SANOFI
    Inventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Klaus Wirth
  • ORGANIC COMPOUNDS
    Publication number: 20120022074
    Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I) wherein the substituents are as defined in the specification and to processes for their production to pharmaceutical compositions comprising them and to their use in the manufacture of a medicament for the treatment and/or delay of progression of psychotic and nemodegenerative disorders.
    Type: Application
    Filed: October 4, 2011
    Publication date: January 26, 2012
    Inventors: Dominik FEUERBACH, Mathias Frederiksen, Konstanze Hurth, Bernard Lucien Roy, Beatrix Wagner
  • INDOLIZINE DERIVATIVE AND USE THEREOF FOR MEDICAL PURPOSES
    Publication number: 20120015972
    Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level and the like. That is, the present invention relates to indolizine derivatives represented by the following formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, salts thereof or the like. In the formula, ring U represents aryl or heteroaryl; R1 represents halogen, a hydroxy group or the like; R2 represents halogen, a hydroxy group, alkyl, alkoxy, alkyl substituted by fluorine, alkoxy substituted by fluorine or the like; m represents a number from 0 to 2; n represents a number from 0 to 3; and R3 represents hydrogen, fluorine or the like.
    Type: Application
    Filed: March 30, 2010
    Publication date: January 19, 2012
    Applicant: KISSEI PHARMACEUTICAL CO., LTD.
    Inventors: Kazuo Shimizu, Masato Iizuka, Yasushi Takigawa
  • N-SUBSTITUTED PYRROLIDINES
    Publication number: 20120010235
    Abstract: Compounds of formula and enantiomers and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositions for the treatment, control, amelioration or prevention of cancer.
    Type: Application
    Filed: June 30, 2011
    Publication date: January 12, 2012
    Inventors: Xin-Jie Chu, Qingjie Ding, Nan Jiang, Jin-Jun Liu, Tina Morgan Ross, Zhuming Zhang
  • Antiviral compounds
    Patent number: 8088368
    Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: May 12, 2010
    Date of Patent: January 3, 2012
    Assignee: Gilead Sciences, Inc.
    Inventors: Hongyan Guo, Darryl Kato, Thorsten A. Kirschberg, Hongtao Liu, John O. Link, Michael L. Mitchell, Jay P. Parrish, Jianyu Sun, James Taylor, Elizabeth M. Bacon, Eda Canales, Aesop Cho, Choung U. Kim, Jeromy J. Cottell, Manoj C. Desai, Randall L. Halcomb, Scott E. Lazerwith, Richard L. Mackman, Hyung-Jung Pyun, Joseph H. Saugier, James D. Trenkle, Winston C. Tse, William J. Watkins, Lianhong Xu
  • NOVEL INHIBITORS OF HEPATITIS C VIRUS REPLICATION
    Publication number: 20110312996
    Abstract: The embodiments provide compounds of the general Formulae VI, VII, VIII, IX, X, XI, XII, XIII, XIV, and XV as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.
    Type: Application
    Filed: May 16, 2011
    Publication date: December 22, 2011
    Applicant: InterMune, Inc.
    Inventors: Brad Buckman, John B. Nicholas, Vladimir Serebryany, Scott D. Seiwert
  • QUINOLIZIDINE AND INDOLIZIDINE DERIVATIVES
    Publication number: 20110313165
    Abstract: The present invention relates to a compound of formula I-A or I-B wherein X, R1, R2 and R3 are defined herein; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer thereof. The compounds of formulas I-A and I-B are good inhibitors of the glycine transporter 1 (GlyT-1), and have a good selectivity to glycine transporter 2 (GlyT-2) inhibitors, suitable in the treatment of neurological and neuropsychiatric disorders.
    Type: Application
    Filed: June 16, 2011
    Publication date: December 22, 2011
    Inventors: Sabine Kolczewski, Emmanuel Pinard
  • Methods for One-Pot N-Demethylation/N-Functionalization of Morphine and Tropane Alkaloids
    Publication number: 20110313163
    Abstract: The present invention provides a method for the N-demethylation and N-functionalization of an N-methylated heterocycle such as a morphine alkaloid or tropane alkaloid. The method comprises reacting the heterocycle with an functionalization agent in the presence of a transition metal catalyst in air or in the presence of an oxidant.
    Type: Application
    Filed: July 8, 2011
    Publication date: December 22, 2011
    Inventors: Tomas Hudlicky, Robert James Carroll, Hemes Lalush, Ales Machara, Lukas Werner, Mary Ann Endoma-Arias
  • Carbazole Compounds and Therapeutic Uses of the Compounds
    Publication number: 20110305661
    Abstract: Compounds of the general structural formula (I) and (II) and use of the compounds and salts and hydrates thereof, as therapeutic agents are disclosed. Treatable diseases and conditions include cancers, inflammatory diseases and conditions, and immunodeficiency diseases.
    Type: Application
    Filed: October 5, 2009
    Publication date: December 15, 2011
    Inventors: John Tucker, Sergey Sviridov, Leonid Brodsky, Catherine Burkhart, Andrei Purmal, Katerina Gurova, Andrei Gudkov
  • 4-(substituted cycloalkylmethyl) imidazole-2-thiones, 4-(substituted cycloalkenylmethyl) imidazole-2-thiones, 4-(substituted cycloalkylmethyl) imidazol-2-ones and 4-(substituted cycloalkenylmethyl) imidazole-2-ones and related compounds
    Patent number: 8071635
    Abstract: Compounds of Formula 1 where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors, and as such have no or only minimal cardiovascular and/or sedatory activity. These compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors. Compounds of Formula 1 where X is O also have the advantageous property that they have no or only minimal cardiovascular and/or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardiovascular and/or sedatory activity.
    Type: Grant
    Filed: February 16, 2008
    Date of Patent: December 6, 2011
    Assignee: Allergan, Inc.
    Inventors: Ken Chow, Todd Heidelbaugh, Daniel Gil, Michael Garst, Larry A. Wheeler, Phong X. Nguyen, Dario G. Gomez
  • TROPANE UREA DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC APPLICATION THEREOF AS MODULATORS OF THE ACTIVITY OF 11BETAHSD1
    Publication number: 20110294809
    Abstract: The invention relates to tropane urea derivatives of general formula (I) and to the application thereof as modulators of the activity of 11?-hydroxysteroid dehydrogenose type 1 (11?HSD1).
    Type: Application
    Filed: October 27, 2009
    Publication date: December 1, 2011
    Applicant: SANOFI-AVENTIS
    Inventors: Alain Jean Braun, Olivier Crespin, Eric Nicolai, Cecile Pascal, Olivier Venier
  • INDOLE DERIVATIVES AS ANTICANCER AGENTS
    Publication number: 20110294846
    Abstract: The present invention provides compounds of formula (I), their use for the treatment of cancer as well as pharmaceutical compositions comprising said compounds of formula (I).
    Type: Application
    Filed: February 3, 2010
    Publication date: December 1, 2011
    Inventors: Bruno Schoentjes, Sophie Descamps, Nathalie Claudie Isabelle Amblard
  • Novel Polymorphs Of Azabicyclohexane
    Publication number: 20110294847
    Abstract: The invention provides polymorphic crystalline forms of acid addition salts of (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane designated as polymorph form A, polymorph form B and polymorph form C, where polymorph form A is more thermodynamically stable than the other forms, methods for preparing and using such polymorph forms and pharmaceutical compositions containing such polymorph forms.
    Type: Application
    Filed: August 10, 2011
    Publication date: December 1, 2011
    Inventors: Eric J. Hagen, Kevin Halloran
  • MAPK/ERK kinase inhibitors
    Patent number: 8063066
    Abstract: Compounds are provided for use with MEK that comprise: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.
    Type: Grant
    Filed: March 17, 2008
    Date of Patent: November 22, 2011
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Qing Dong, Toufiko Kanounl, Michael B. Wallace
  • Polymerizable dichroic azo dyes
    Patent number: 8053039
    Abstract: The present invention is directed towards polymerizable dichroic azo dyes comprising azo-chromophores having at least one standard mesogenic ring system attached to said chromophores and at least one polymerizable group leading to dyes having sufficient solubilty and a very high order parameter.
    Type: Grant
    Filed: March 23, 2004
    Date of Patent: November 8, 2011
    Assignee: Rolic AG
    Inventors: Thomas Peglow, Franco Moia, Zoubair Mohammed Cherkaoui, Mario Schwab
  • Quinolones and azaquinolones that inhibit prolyl hydroxylase
    Patent number: 8048894
    Abstract: Compounds of Formula I are useful inhibitors of HIF prolyl hydroxylases. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.
    Type: Grant
    Filed: April 16, 2008
    Date of Patent: November 1, 2011
    Assignee: Amgen Inc.
    Inventors: Jennifer R. Allen, Roland Burli, Marian C. Bryan, Guo-Qiang Cao, Susana C. Neira, Anthony B. Reed
  • COMPOUNDS AND COMPOSITIONS FOR COGNITION-ENHANCEMENT, METHODS OF MAKING, AND METHODS OF TREATING
    Publication number: 20110263613
    Abstract: Disclosed are muscarinic agonist compounds including oxadiazole derivatives, compositions and preparations thereof. Also disclosed are methods of synthesizing such oxadiazole compounds. Further disclosed are methods for treating a subject with said muscarinic agonists or a pharmaceutically suitable form thereof to enhance cognitive function.
    Type: Application
    Filed: January 11, 2011
    Publication date: October 27, 2011
    Inventors: Michael L. Hendrickson, Jeffrey C. Ockuly, Trevor M. Twose, Melinda L. Verdone, Brent D. Abraham, Richard R. Copp, James G. Farnham, Seth A. Hanson
  • Derivatives of pyrrolopyridine-2-carboxamides, preparation thereof and therapeutic application thereof
    Patent number: 8044066
    Abstract: The invention relates to compounds of formula (I): Wherein n, the pyrrolopyridine core, X, Y and W are as described herein. The invention also relates to a preparation method and to a therapeutic application.
    Type: Grant
    Filed: July 17, 2009
    Date of Patent: October 25, 2011
    Assignee: Sanofi-Aventis
    Inventors: Laurent Dubois, Yannick Evanno, Andrè Malanda
  • Sulfonamide substituted pyrazoline compounds, their preparation and use as CB1 modulators
    Patent number: 8044053
    Abstract: The present invention relates to substituted pyrazoline compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.
    Type: Grant
    Filed: October 10, 2007
    Date of Patent: October 25, 2011
    Assignee: Laboratories del Dr. Esteve, S.A.
    Inventors: Helmut Buschmann, Antonio Torrens-Jover, Josef Mas-Prio, Susana Yenes-Minguez
  • Pleuromutilin derivatives as antimicrobials
    Patent number: RE43390
    Abstract: The present invention relates to pleuromutilin derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medical therapy, particularly antibacterial therapy.
    Type: Grant
    Filed: October 27, 1998
    Date of Patent: May 15, 2012
    Assignees: GlaxoSmithKline LLC, SmithKline Beecham Limited
    Inventors: Valerie Joan Berry, Steven Dabbs, Colin Henry Frydrych, Eric Hunt, Francis Dominic Sanderson, Gary Woodnutt