Bicyclo Ring System Having The Diazole Ring As One Of The Cyclos Patents (Class 548/302.7)
  • Patent number: 8354434
    Abstract: The invention relates to cyclourea compounds of Formula I: or a pharmaceutically acceptable salt or solvate thereof, wherein R1-R3 and Z are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Grant
    Filed: January 15, 2007
    Date of Patent: January 15, 2013
    Assignee: Purdue Pharma L.P.
    Inventor: Xiaoming Zhou
  • Patent number: 8354542
    Abstract: Objects of the present invention are to provide the following: a novel heterocyclic compound which can be used as a material in which a light-emitting substance of a light-emitting layer in a light-emitting element is dispersed; a novel heterocyclic compound having a high electron-transport property; a light-emitting element having high current efficiency; and a light-emitting device, an electronic device and a lighting device each having reduced power consumption. Provided are a heterocyclic compound represented by General Formula (G1-1) or (G1-2) below, and a light-emitting element, a light-emitting device, an electronic device and a lighting device each including the heterocyclic compound. Such use of the heterocyclic compound represented by General Formula (G1-1) or (G1-2) makes it possible to provide a light-emitting element having high current efficiency, and a light-emitting device, an electronic device and a lighting device each having reduced power consumption.
    Type: Grant
    Filed: December 20, 2010
    Date of Patent: January 15, 2013
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Yuko Kawata, Hiroshi Kadoma, Harue Osaka, Nobuharu Ohsawa, Satoshi Seo
  • Publication number: 20120322830
    Abstract: The invention relates to cyclourea compounds of Formula I: or a pharmaceutically acceptable salt or solvate thereof, wherein R1-R3 and Z are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Application
    Filed: June 11, 2012
    Publication date: December 20, 2012
    Applicant: Purdue Pharma L.P.
    Inventor: Xiaoming ZHOU
  • Publication number: 20120316150
    Abstract: A compound of Formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein, R1, R2, R3, R4, R5 and R6 are as defined herein: and compositions, processes for the preparation, and uses thereof, e.g. in the treatment of endometriosis or uterine fibroids.
    Type: Application
    Filed: June 18, 2012
    Publication date: December 13, 2012
    Inventors: KARL RICHARD GIBSON, Martin Peter Green, Toby James Underwood, Florian Wakenhut
  • Patent number: 8329140
    Abstract: A method and system for storing and evolving hydrogen (H2) employ chemical compounds that can be hydrogenated to store hydrogen and dehydrogenated to evolve hydrogen. A catalyst lowers the energy required for storing and evolving hydrogen. The method and system can provide hydrogen for devices that consume hydrogen as fuel.
    Type: Grant
    Filed: September 11, 2008
    Date of Patent: December 11, 2012
    Assignee: Los Alamos National Security, LLC
    Inventors: David L. Thorn, William Tumas, P. Jeffrey Hay, Daniel E. Schwarz, Thomas M. Cameron
  • Publication number: 20120295888
    Abstract: The present invention relates to a method of treating a disease or disorder characterised by increased stress hormone levels and/or decreased androgen hormone levels in a subject, comprising administering to the subject a therapeutically effective amount of a compound represented by formula (I): wherein n is 1 or 3; R is hydrogen or —C(O)N(Ra)(Rb) wherein Ra and Rb are independently —(C1-C4)alkyl, or —(C1-C4)alkyl-(C5-C7)aryl, wherein each of Ra and Rb is optionally substituted by —(C1-C4)alkoxy; R1, R2, and R3, are independently hydrogen, halogen, cyano or —(C6-C10) aryl, wherein said —(C6-C10)aryl is optionally substituted by halogen, with the proviso that no more than one of R1, R2, and R3 is hydrogen; and R4 and R5 are hydrogen; or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: January 13, 2011
    Publication date: November 22, 2012
    Inventors: Qi-Ying Hu, Gary Michael Ksander, Erik Meredith, Lauren G. Monovich, Julien Papillon, Christoph Schumacher
  • Patent number: 8314097
    Abstract: The present invention provides a compound of formula I: Said compound is inhibitor of aldosterone synthase and aromatase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase or aromatase. Accordingly, the compound of formula I can be used in treatment of hypokalemia, hypertension, congestive heart failure, atrial fibrillation, renal failure, in particular, chronic renal failure, restenosis, atherosclerosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, inflammation, increased formation of collagen, fibrosis such as cardiac or myocardiac fibrosis and remodeling following hypertension and endothelial dysfunction, gynecomastia, osteoporosis, prostate cancer, endometriosis, uterine fibroids, dysfunctional uterine bleeding, endometrial hyperplasia, polycystic ovarian disease, infertility, fibrocystic breast disease, breast cancer and fibrocystic mastopathy.
    Type: Grant
    Filed: August 23, 2006
    Date of Patent: November 20, 2012
    Assignee: Novartis AG
    Inventors: Gary Michael Ksander, Erik Meredith, Lauren G. Monovich, Julien Papillon, Fariborz Firooznia, Qi-Ying Hu
  • Publication number: 20120289549
    Abstract: The invention provides novel compounds having the general formula (I), wherein R1, R2, R3 and A are as described herein, compositions including the compounds and methods of using the compounds. These compounds are useful as inhibitors of hormone sensitive lipase (HSL) and may be used in the treatment of diabetes, metabolic syndrome, dyslipidemia, atherosclerosis, obesity, cardiovascular diseases, myocardial dysfunction, inflammation, non-alcoholic fatty liver disease and non-alcoholic steatohepatitis.
    Type: Application
    Filed: May 2, 2012
    Publication date: November 15, 2012
    Inventors: Aurelia Conte, Daniel Hunziker, Werner Neidhart, Matthias Nettekoven, Tanja Schulz-Gasch
  • Publication number: 20120277215
    Abstract: The present invention provides a compound of formula I: Said compound is inhibitor of aldosterone synthase and aromatase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase or aromatase. Accordingly, the compound of formula I can be used in treatment of hypokalemia, hypertension, congestive heart failure, atrial fibrillation, renal failure, in particular, chronic renal failure, restenosis, atherosclerosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, inflammation, increased formation of collagen, fibrosis such as cardiac or myocardiac fibrosis and remodeling following hypertension and endothelial dysfunction, gynecomastia, osteoporosis, prostate cancer, endometriosis, uterine fibroids, dysfunctional uterine bleeding, endometrial hyperplasia, polycystic ovarian disease, infertility, fibrocystic breast disease, breast cancer and fibrocystic mastopathy.
    Type: Application
    Filed: July 2, 2012
    Publication date: November 1, 2012
    Inventors: Gary Michael Ksander, Erik Meredith, Lauren G. Monovich, Julien Papillon, Fariborz Firooznia, Qi-Ying Hu
  • Patent number: 8273769
    Abstract: The present invention provides phenoxyacetic acid derivatives of Formula (I) for the treatment of CRTH2 related disorders and disease selected from asthma, atopic dermatitis and inflammatory dermatoses.
    Type: Grant
    Filed: February 9, 2010
    Date of Patent: September 25, 2012
    Assignee: Merck Serono SA
    Inventors: Stefano Crosignani, Catherine Jorand-Lebrun, Christophe Cleva, Adeline Pretre
  • Patent number: 8242156
    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.
    Type: Grant
    Filed: February 9, 2010
    Date of Patent: August 14, 2012
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
  • Patent number: 8232269
    Abstract: A compound of Formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein, R1 and R2 each independently represent H, halogen, CF3, C1-3 alkyl or C1-3 alkoxy; R3 represents C1-6 alkyl, C3-6 cycloalkyl, phenyl (optionally substituted by one or more substituents each independently selected from Ra) or Het (optionally substituted by one or more substituents each independently selected from OH, oxo, or C1-4 alkyl); R4 represents H or C1-3 alkyl; R5 represents C1-6 alkyl (optionally substituted by one or more substituents each independently selected from Rb), C3-6 cycloalkyl (optionally substituted by one or more substituents each independently selected from oxo or OH), or Het2 (optionally substituted by one or more substituents each independently selected from Rd); oxygen atom or 1 sulphur atom, or (c) 1 oxygen atom or 1 sulphur atom, (optionally substituted by one or more substituents each independently selected from OH, oxo or C1-4 alkyl); and R6 represents C1-3 alkyl (optionally substitu
    Type: Grant
    Filed: September 17, 2009
    Date of Patent: July 31, 2012
    Assignee: Pfizer Inc.
    Inventors: Karl Richard Gibson, Martin Peter Green, Toby James Underwood, Florian Wakenhut
  • Patent number: 8217070
    Abstract: Compounds of Formula (I) inhibit the PARP enzyme and are useful for treating a disease or a disorder associated with PARP. Also disclosed are pharmaceutical compositions comprising compounds of Formula (I), methods of treatment comprising compounds of Formula (I), and methods of inhibiting the PARP enzyme comprising compounds of Formula (I).
    Type: Grant
    Filed: April 22, 2010
    Date of Patent: July 10, 2012
    Assignee: Abbott Laboratories
    Inventors: Gui-Dong Zhu, Virajkumar B. Gandhi, Jianchun Gong, Thomas D. Penning, Vincent L. Giranda, Sheela Thomas
  • Patent number: 8188132
    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.
    Type: Grant
    Filed: February 9, 2010
    Date of Patent: May 29, 2012
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yat Sun Or, Ce Wang, Xiaowen Peng, Lu Ying, Yao-Ling Qiu
  • Patent number: 8168668
    Abstract: The present invention relates to new compounds or salts, solvates or solvated salts thereof, processes for their preparation and to new intermediates used in the preparation thereof, pharmaceutical compositions containing said compounds and to the use of said compounds in therapy.
    Type: Grant
    Filed: October 14, 2009
    Date of Patent: May 1, 2012
    Assignee: AstraZeneca AB
    Inventors: Yevgeni Besidski, Martin Nylof, Inger Kers, Karin Skogholm, Shawn Johnstone, Paul Jones, Denis Labrecque, Andrew Griffin
  • Patent number: 8147987
    Abstract: An organic electroluminescent element comprises: a pair of electrodes; and one or more organic compound layers at least one of which is a light-emitting layer, the one or more organic compound layers being provided between the pair of electrodes, wherein at least one of the one or more organic compound layers comprises a compound represented by general formula (Z): wherein R31 and R32 each represents a hydrogen atom or a substituent, R3A represents a substituent other than an aromatic hetero ring connected through a nitrogen atom, or a hydrogen atom, X31 to X38 each represents a substituted or unsubstituted carbon atom or a nitrogen atom, and Y31 to Y33 each represents a nitrogen atom or C—R3B (wherein R3B represents a substituent other than an aromatic hetero ring connected through a nitrogen atom, or a hydrogen atom).
    Type: Grant
    Filed: February 23, 2007
    Date of Patent: April 3, 2012
    Assignee: Fujifilm Corporation
    Inventors: Itaru Osaka, Tatsuya Igarashi, Toshihiko Ise, Eiji Fukuzaki, Satoshi Sano
  • Publication number: 20120077985
    Abstract: The present invention provides an industrially advantageous process for producing a steroid C17,20 lyase inhibitor represented by the general formula (I); and a Reformatsky reagent in a stable form suitable for the process. In the present invention, a compound represented by the general formula (I) is produced by reducing a specific ?-hydroxy ester compound derivative or a salt thereof obtained from a specific carbonyl compound in a Reformatsky reaction in the presence of a metal hydride complex and a metal halide, and then subjecting it to a ring-closing reaction. In the above Reformatsky reaction, it is useful to use a stable solution of a compound represented by the general formula BrZnCH2COOC2H5 or a crystal of the compound which is represented by the formula (BrZnCH2COOC2H5.THF)2.
    Type: Application
    Filed: November 28, 2011
    Publication date: March 29, 2012
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Jun-ichi Kawakami, Shigeru Nuwa, Shokyo Miki
  • Patent number: 8143420
    Abstract: Methods and compositions for detecting free radicals, the compositions being spin trapping compounds comprising a nitrone having a detecting moiety and optionally having a targeting moiety for targeting the nitrone to an organ, a cell, an organelle or a molecule of interest for directly detecting free radicals, especially free radicals in biological samples.
    Type: Grant
    Filed: December 24, 2008
    Date of Patent: March 27, 2012
    Assignees: Medical Collage of Wisconsin, Inc., Université de Provence
    Inventors: Micael Joel Hardy, Marcos Lopez, Balaraman Kalyanaraman, Neil Hogg, Olivier Ouari, Paul Tordo
  • Patent number: 8138182
    Abstract: The present invention relates to a diketohydrazine derivative of formula (I) and a pharmaceutically acceptable salt thereof (the symbols in the formula have the same meaning as described in the specification). The compound of formula (I) has an inhibitory activity against cysteine protease, and it is useful for the treatment of inflammatory diseases, immune diseases, ischemic diseases, respiratory diseases, circulatory diseases, blood diseases, neuronal diseases, hepatic or biliary diseases, osseous or articular diseases, metabolic diseases, etc. And the compound has inhibitory activity against elastase and it is also useful for the treatment of COPD (chronic obstacle pulmonary diseases).
    Type: Grant
    Filed: September 24, 2009
    Date of Patent: March 20, 2012
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Akira Hatayama, Hiroshi Tsuruta, Yasuo Ochi, Haruo Imawaka, Kazuyuki Ohmoto
  • Publication number: 20120065210
    Abstract: There are provided compounds of formula I or a pharmaceutically acceptable salt thereof, wherein X, Y, R1, R1?, R2, R2?, R3, R4, R5 are as defined herein. The compounds exhibit activity as anticancer agents.
    Type: Application
    Filed: September 7, 2011
    Publication date: March 15, 2012
    Inventors: Xin-Jie Chu, Qingjie Ding, Nan Jiang, Jin-Jun Liu, Tina Morgan Ross, Zhuming Zhang
  • Patent number: 8124636
    Abstract: Compounds of formula as well as pharmaceutically acceptable salts and esters thereof, wherein A and R1 to R4 have the significance given in claim 1 can be used in the form of pharmaceutical compositions.
    Type: Grant
    Filed: April 16, 2009
    Date of Patent: February 28, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean Ackermann, Kurt Amrein, Bernd Kuhn, Alexander V. Mayweg, Werner Neidhart
  • Patent number: 8119675
    Abstract: Novel compounds of the formula I (I), in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R, Q, W, X and Z have the meanings indicated in Patent Claim 1, are suitable as antidiabetics.
    Type: Grant
    Filed: January 28, 2008
    Date of Patent: February 21, 2012
    Assignee: Merck Patent GmbH
    Inventors: Lars Thore Burgdorf, Bertram Cezanne, Markus Klein, Rolf Gericke, Christos Tsaklakidis, Werner Mederski, Norbert Beier
  • Patent number: 8110575
    Abstract: The present invention relates to new CGRP-antagonists of general formula I wherein U, V, X, Y, R1, R2, R3 and R4 are defined as in the description, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates, the mixtures thereof and the salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, medicaments containing these compounds, their use and processes for preparing them.
    Type: Grant
    Filed: November 21, 2008
    Date of Patent: February 7, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Dirk Gottschling, Georg Dahmann, Henri Doods, Annekatrin Heimann, Stephan Georg Mueller, Klaus Rudolf, Gerhard Georg Schaenzle, Dirk Stenkamp
  • Patent number: 8101637
    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: Grant
    Filed: June 17, 2005
    Date of Patent: January 24, 2012
    Assignee: Addex Pharma SA
    Inventors: Anne-Sophie Bessis, Christelle Bolea, Béatrice Bonnet, Mark Epping-Jordan, Nicholas Poirier, Sonia-Maria Poli, Jean-Philippe Rocher, Yves Thollon
  • Patent number: 8067457
    Abstract: The present invention provides compounds of general formula I: or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R1 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR2 and accordingly are useful for the treatment of a variety of inflammatory, allergic, and autoimmune diseases, disorders, or conditions.
    Type: Grant
    Filed: October 26, 2006
    Date of Patent: November 29, 2011
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Shomir Ghosh, Prakash Raman, Kevin Sprott, Amy M. Elder, Sian Griffiths, Francois Soucy, Qing Ye
  • Publication number: 20110245310
    Abstract: The present invention relates to compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, processes for their preparation, pharmaceutical compositions containing these compounds, and their use in the treatment of allergic disorders, such as allergic rhinitis and asthma.
    Type: Application
    Filed: December 16, 2009
    Publication date: October 6, 2011
    Inventors: Ian Baxter Campbell, Simon Peace, John Martin Pritchard, Daniel Tape, Robert Charles Wheeler
  • Patent number: 8030328
    Abstract: Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof wherein the variables A, n, R5, R21-R24 and Q are defined herein. These compounds bind VLA-4. Certain of these compound also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
    Type: Grant
    Filed: May 22, 2006
    Date of Patent: October 4, 2011
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: Frank Stappenbeck, Andrei Konradi, Jacek Jagodzinski, Christopher M. Semko, Ying-zi Xu, Jenifer L. Smith, Kassandra Rossiter
  • Patent number: 8008334
    Abstract: The patent application relates to new heterocyclic compounds of the general formula (I) in which R, R1, R2, R3, R4 and n have the definitions elucidated in more detail in the description, to a process for preparing them and to the use of these compounds as medicaments, particularly as aldosterone synthase inhibitors.
    Type: Grant
    Filed: December 8, 2006
    Date of Patent: August 30, 2011
    Assignee: Novartis AG
    Inventors: Peter Herold, Robert Mah, Vincenzo Tschinke, Michael Quirmbach, Christiane Marti, Aleksandar Stojanovic, Stefan Stutz
  • Patent number: 7989472
    Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: March 19, 2007
    Date of Patent: August 2, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ronald M. Kim, Emma R. Parmee, Qiang Tan, Ashley Rouse Lins, Jiang Chang, Cangming Yang
  • Patent number: 7977334
    Abstract: The present invention relates to new beta-agonists of general formula (I) wherein the groups R1 to R7 have the meanings given in the claims and specification, the tautomers, the enantiomers, the diastereomers, the mixtures thereof, the prodrugs thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, processes for preparing these compounds and their use as pharmaceutical compositions.
    Type: Grant
    Filed: May 1, 2008
    Date of Patent: July 12, 2011
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Thomas Trieselmann, Bradford S. Hamilton
  • Patent number: 7973066
    Abstract: The use of a compound of formula (I), is disclosed in treating and/or preventing 5 chemotherapy-induced peripheral neurotoxicity (CIPN). The invention includes pharmaceutical compositions wherein the compound of formula (I) is present in a mixture with anticancer agents. An improved anticancer treatment with reduced CIPN-related side effects is also provided.
    Type: Grant
    Filed: November 14, 2007
    Date of Patent: July 5, 2011
    Assignee: Neurotune AG
    Inventors: Carlo Farina, Carla Ghelardini, Paola Petrillo
  • Publication number: 20110158930
    Abstract: A method for treatment of a patient suffering from irritable bowel syndrome with diarrhea or mixed irritable bowel syndrome, which comprises administering to the patient a therapeutically effective amount of ramosetron or a pharmaceutically acceptable salt thereof in combination with a therapeutically effective amount of polycarbophil or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: August 27, 2009
    Publication date: June 30, 2011
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Takuya Hirata, Toshiyuki Funatsu, Yoshihiro Keto, Shinobu Akuzawa
  • Publication number: 20110112303
    Abstract: A process for preparing the S or R enantiomer of a compound of formula A, the process comprising subjecting a compound of formula B to asymmetric hydrogenation in the presence of a chiral transition metal catalyst and a source of hydrogen, wherein X is CH2, oxygen, or sulphur; R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, alkyloxy, hydroxy, nitro, alkylcarbonylamino, alkylamino, or dialkylamino group; and R4 is alkyl or aryl, wherein the transition metal catalyst comprises a chiral ligand having the formula wherein p is from 1 to 6, and Ar means aryl group; wherein the term alkyl means hydrocarbon chains, straight or branched, containing from one to six carbon atoms, optionally substituted by aryl, alkoxy, halogen, alkoxycarbonyl or hydroxycarbonyl groups; the term aryl means an aromatic or heteroaromatic group, optionally substituted by alkyloxy, halogen, or nitro group; and the term halogen means fluorine, chlorine, bromine, or iodine.
    Type: Application
    Filed: March 17, 2009
    Publication date: May 12, 2011
    Applicant: BIAL - PORTELA & CA, S.A.
    Inventors: David Alexander Learmonth, Alexander Beliaev, Wenge Li
  • Patent number: 7939528
    Abstract: The present invention relates to novel compounds which are antagonist or inverse agonists at an opioid receptor. Such compounds are useful in the treatment of obesity and related diseases and/or conditions in mammals, particularly humans. Methods of making and using such compounds are also disclosed.
    Type: Grant
    Filed: October 12, 2006
    Date of Patent: May 10, 2011
    Assignee: GlaxoSmithKline LLC
    Inventors: Kevin Karl Barvian, Jason Daniel Speake, David John Cowan, Andrew Lamont Larkin, Jerzy Ryszard Szewczyk
  • Patent number: 7923464
    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: Grant
    Filed: December 4, 2006
    Date of Patent: April 12, 2011
    Assignee: Neurosearch A/S
    Inventors: Janus S. Larsen, Lene Teuber, Philip K. Ahring, Elsebet Østergaard Nielsen, Naheed Mirza
  • Patent number: 7897619
    Abstract: The invention relates to heterocyclic compounds of Formula I and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein. The invention also relates to the therapeutic use of such compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.
    Type: Grant
    Filed: July 16, 2008
    Date of Patent: March 1, 2011
    Assignee: Amgen Inc.
    Inventors: Qingping Zeng, Dawei Zhang, Guomin Yao, George E. Wohlhieter, Xianghong Wang, James Rider, Andreas Reichelt, Holger Monenschein, Fang-Tsao Hong, James R. Falsey, Celia Dominguez, Matthew P. Bourbeau, John G. Allen
  • Patent number: 7883574
    Abstract: Nanoscale particles of benzimidazolone pigments are made by providing one or more organic pigment precursor(s) to a benzimidazolone pigment, providing a solution or suspension of a sterically bulky stabilizer compound that associates non-covalently with a benzimidazolone moiety on one of the pigment precursors, wherein the sterically bulky stabilizer compound is selected from the group consisting of substituted pyridine derivatives, alkylated benzimidazolone compounds, alkylated derivatives of aromatic acids, and mixtures thereof, and carrying out a coupling reaction to form a benzimidazolone pigment composition, whereby one or more functional moieties on the benzimidazolone pigment is non-covalently associated with the sterically bulky stabilizer, so as to limit an extent of particle growth and aggregation and results in nanoscale pigment particles.
    Type: Grant
    Filed: July 24, 2009
    Date of Patent: February 8, 2011
    Assignee: Xerox Corporation
    Inventors: Rina Carlini, Darren Andrew Makeiff
  • Publication number: 20110028512
    Abstract: Heterocyclic compounds of the general formula (I) are provided in which R, R1, R2, R3, R4 and n have the definitions elucidated in more detail in the description, to a process for preparing them and to the use of these compounds as medicaments, particularly as aldostereone synthase inhibitors,
    Type: Application
    Filed: October 8, 2010
    Publication date: February 3, 2011
    Inventors: Peter Herold, Robert Mah, Vincenzo Tschinke, Michael Quirmbach, Christiane Marti, Aleksandar Stojanovic, Stefan Stutz
  • Publication number: 20110021772
    Abstract: The invention relates to new heterocyclic compounds of general formula (I), and their salts with a base or an acid: The invention also relates to a process for the preparation of these compounds as well as their use as medicaments, in particular as anti-bacterial agents.
    Type: Application
    Filed: April 16, 2010
    Publication date: January 27, 2011
    Inventors: Maxime Lampilas, Jozsef Aszodi, David Alan Rowlands, Claude Fromentin
  • Patent number: 7867629
    Abstract: A specific derivative of heterocyclic compound having nitrogen atom and an organic electroluminescence device comprising the compound. An organic electroluminescence device comprising at least one of organic compound layers including a light emitting layer sandwiched between an anode and a cathode, wherein said at least one of the organic compound layers comprises the derivative of the heterocyclic compound having nitrogen atom as a sole component or as mixed component. The organic electroluminescence device achieves elevation of luminance and excellent efficiency of light emission, and also achieves long lifetime by an improvement of an electrode adhesion.
    Type: Grant
    Filed: September 26, 2003
    Date of Patent: January 11, 2011
    Assignee: Idemitsu Kosan Co., Ltd.
    Inventors: Hiroshi Yamamoto, Masahide Matsuura, Hidetsugu Ikeda, Mineyuki Kubota, Masahiro Kawamura
  • Patent number: 7863305
    Abstract: Compounds of formula I: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein p, Ar, R1, R2, R3, Ra, Rb, Rc, Rd and Re are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.
    Type: Grant
    Filed: June 1, 2005
    Date of Patent: January 4, 2011
    Assignee: Roche Palo Alto LLC
    Inventors: Robert Greenhouse, Saul Jaime-Figueroa, Lubica Raptova, Deborah Carol Reuter, Karin Ann Stein, Robert Weikert
  • Publication number: 20100279991
    Abstract: This invention is directed to a tetrahydro-cyclopentyl pyrazole cannabinoid modulator compound of formula (I): and a method for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease.
    Type: Application
    Filed: July 15, 2010
    Publication date: November 4, 2010
    Inventors: Fina Liotta, Mingde Xia, Michael P. Wachter, Scott A. Beers
  • Patent number: 7816388
    Abstract: Formula (I) compounds are described: Formula (I) where the radicals are as defined in the description, processes for their preparation, and their uses for the preparation of conjugates with radionuclides for use in human and animal therapy and diagnostics, particularly for the diagnosis and therapy of pathological conditions such as tumors.
    Type: Grant
    Filed: September 18, 2006
    Date of Patent: October 19, 2010
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Paolo Carminati, Mauro Ginanneschi, Giovanni Paganelli, Marco Chinol
  • Publication number: 20100249091
    Abstract: A compound of Formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein, R1 and R2 each independently represent H, halogen, CF3, C1-3 alkyl or C1-3 alkoxy; R3 represents C1-6 alkyl, C3-6 cycloalkyl, phenyl (optionally substituted by one or more substituents each independently selected from Ra) or Het (optionally substituted by one or more substituents each independently selected from OH, oxo, or C1-4 alkyl); R4 represents H or C1-3 alkyl; R5 represents C1-6 alkyl (optionally substituted by one or more substituents each independently selected from Rb), C3-6 cycloalkyl (optionally substituted by one or more substituents each independently selected from oxo or OH), or Het2 (optionally substituted by one or more substituents each independently selected from Rd); oxygen atom or 1 sulphur atom, or (c) 1 oxygen atom or 1 sulphur atom, (optionally substituted by one or more substituents each independently selected from OH, oxo or C1-4 alkyl); and R6 represents C1-3 alkyl (optionally subs
    Type: Application
    Filed: September 17, 2009
    Publication date: September 30, 2010
    Inventors: Karl Richard Gibson, Martin Peter Green, Toby James Underwood, Florian Wakenhut
  • Patent number: 7799927
    Abstract: An indolestyryl compound. The indolestyryl compound has formula (I): wherein Z1 comprises benzene, naphthalene, or heterocyclic ring containing O, S, or N, R2 comprises H, halogen atoms, C1-5 alkyl, nitro, ester, carboxyl, sulfo, sulfonamide, sulfuric ester, amide, C1-3 alkoxy, amino, alkylamino, cyano, C1-6 alkylsulfonyl, or C2-7 alkoxy carbonyl, R3, R4, R5, and R6 comprise H, alkyl, aralkyl, or heterocyclic ring containing O, S, or N, R7 and R8 comprise H or alkyl, R10 comprises H, alkyl, halogen atoms, nitro, hydroxyl, amino, ester, or substituted or non-substituted sulfonyl, W comprises carbon or nitrogen, Y comprises carbon, oxygen, sulfur, selenium, —NR, or —C(CH3)2, m is 1˜3, and X1 comprises an anionic group or an anionic organometallic complex, wherein R3 and R4 are joined to a nitrogen atom or R5 and R6 are joined together to form a ring, and R bonded to nitrogen is C1-5 alkyl.
    Type: Grant
    Filed: April 26, 2006
    Date of Patent: September 21, 2010
    Assignee: Industrial Technology Research Institute
    Inventors: Shin-Shin Wang, Chien-Wen Chen, Jong-Lieh Yang, Chii-Chang Lai, Hui-Ping Tsai, Wen-Ping Chu, Wen-Yih Liao, Chien-Liang Huang, Tzuan-Ren Jeng, Ching-Yu Hsieh, An-Tse Lee
  • Patent number: 7781431
    Abstract: The present invention relates to thienopyrrole compounds of formula (I); wherein A, B, Y, Ar, n, Z and X1 are as defined herein, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C infections.
    Type: Grant
    Filed: September 7, 2004
    Date of Patent: August 24, 2010
    Assignee: Istituto di Ricerche di Biologia Molecolare P Angeletti SpA
    Inventors: Barbara Attenni, Jose Ignacio Martin Hernando, Savina Malancona, Frank Narjes, Jesus Maria Ontoria Ontoria, Michael Rowley
  • Patent number: 7776900
    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: Grant
    Filed: April 18, 2006
    Date of Patent: August 17, 2010
    Assignee: Neurosearch A/S
    Inventors: Lene Teuber, Janus S. Larsen, Philip K. Ahring, Elsebet Østergaard Nielsen, Naheed Mirza
  • Patent number: 7772267
    Abstract: There are provided compounds according to formula I wherein the substitutents are as described herein. Further provided are methods of using such compounds for the treatment of nuclear hormone receptor-associated conditions, such as age related diseases, for example sarcopenia. Also provided are pharmaceutical compositions containing such compounds and processes for preparing some of the compounds of the invention. Other embodiments are also disclosed.
    Type: Grant
    Filed: October 31, 2007
    Date of Patent: August 10, 2010
    Assignee: Bristol-Myers Squibb Company
    Inventors: Chong-qing Sun, Lawrence Hamann, David Augeri, Yingzhi Bi, Jeffrey Robl, Yan-Ting Huang, Tammy Wang, Alexandra Holubec, Ligaya Simpkins, James C. Sutton, James J. Li
  • Patent number: 7772248
    Abstract: The present disclosure is directed to modulators of GABAA receptors and pharmaceutically acceptable salts and prodrugs thereof, the chemical synthesis thereof, and the medical use of such compounds for the treatment and/or management of sleep disorders and/or for providing a patient in need with a hypnotic, anxiolytic or anti-convulsive effect are described.
    Type: Grant
    Filed: May 30, 2007
    Date of Patent: August 10, 2010
    Assignee: Auspex Pharmaceuticals, Inc.
    Inventors: Thomas G. Gant, Sepehr Sarshar
  • Publication number: 20100184982
    Abstract: Provided is a detergent-dispersant for a lubricant having excellent detergency and dispersibility effects. Specifically provided are: a detergent-dispersant including a heterocyclic compound having a heterocyclic skeleton derived from a compound selected from the group consisting of pyridines, pyrroles, pyrimidines, pyrazoles, pyridazines, imidazoles, pyrazines, triazines, triazoles, tetrazoles, oxazoles, oxadiazoles, thiazoles, thiadiazoles, furans, dioxanes, pyrans, and thiophenes; and an additive composition for a lubricant and a lubricant composition, each containing the detergent-dispersant.
    Type: Application
    Filed: June 10, 2008
    Publication date: July 22, 2010
    Applicant: IDEMITSU KOSAN CO., LTD
    Inventors: Junya Iwasaki, Izumi Terada, Hiroaki Koshima