Ring Nitrogen Is Shared By The Two Cyclos Patents (Class 546/121)
  • Nematocidal sulfonamides
    Patent number: 8623890
    Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Z is O or S; and R1, R2, R3, Q and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling a parasitic nematode comprising contacting the parasitic nematode or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: May 4, 2010
    Date of Patent: January 7, 2014
    Assignee: E I du Pont de Nemours and Company
    Inventors: George Philip Lahm, Renee M. Lett, Brenton Todd Smith, Benjamin Kenneth Smith, C. Anne Daly
  • Glycine transporter inhibiting substances
    Patent number: 8623898
    Abstract: The present invention aims to provide novel compounds of formula [I] or pharmaceutically acceptable salts thereof that are based on a glycine uptake inhibiting action and which are useful in the prevention or treatment of such diseases as schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsory disorder, social anxiety disorder, posttraumatic stress disorder, specific phobia, acute stress disorder, etc.
    Type: Grant
    Filed: March 19, 2010
    Date of Patent: January 7, 2014
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Akito Yasuhara, Shuji Yamamoto, Hiroshi Ohta, Yoshihisa Shirasaki, Kazunari Sakagami, Masato Hayashi, Tsuyoshi Shibata, Youichi Shimazaki, Yuko Araki, Kumi Abe, Xiang-Min Sun
  • 5-phenylpyrazolopyridine derivatives, preparation and therapeutic use thereof
    Patent number: 8618301
    Abstract: The present invention relates to compounds of formula (I).
    Type: Grant
    Filed: September 17, 2010
    Date of Patent: December 31, 2013
    Assignee: Sanofi
    Inventors: Florian Auger, Danielle De Peretti, Luc Even
  • COMPOUNDS THAT MODULATE INTRACELLULAR CALCIUM
    Publication number: 20130345240
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: August 16, 2013
    Publication date: December 26, 2013
    Applicant: CALCIMEDICA, INC.
    Inventors: Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • ISOXAZOLE BETA-LACTAMASE INHIBITORS
    Publication number: 20130345190
    Abstract: ?-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D ?-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.
    Type: Application
    Filed: March 29, 2013
    Publication date: December 26, 2013
    Inventor: Cubist Pharmaceuticals, Inc.
  • FUSED RING ANALOGUES OF ANTI-FIBROTIC AGENTS
    Publication number: 20130338151
    Abstract: The present invention relates to arylcarbonyl and heteroarylcarbonyl anthranilate compounds that may be useful as anti-fibrotic agents. The present invention also relates to methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment disorders.
    Type: Application
    Filed: October 21, 2010
    Publication date: December 19, 2013
    Applicant: Fibrotech Therapeutics Pty Ltd
    Inventors: Spencer John Williams, Steven Zammit, Darren James Kelly
  • Pyrrolidine inhibitors of IAP
    Patent number: 8609845
    Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, Q, X1, X2, Y, R1, R2, R3, R4, R4?, R5, R6 and R6? are as described herein.
    Type: Grant
    Filed: August 10, 2009
    Date of Patent: December 17, 2013
    Assignee: Genentech, Inc.
    Inventors: Frederick Cohen, Vickie Hsiao-Wei Tsui, Cuong Ly, John A. Flygare
  • COMPOSITIONS AND METHODS FOR MODULATING FXR
    Publication number: 20130331349
    Abstract: The present invention relates to compounds of Formula (I), a stereoisomer, enantiomer, a pharmaceutically acceptable salt or an amino acid conjugate thereof; wherein variables are as defined herein; and their pharmaceutical compositions, which are useful as modulators of the activity of Farnesiod X receptors (FXR).
    Type: Application
    Filed: November 30, 2011
    Publication date: December 12, 2013
    Inventors: David C. Tully, Paul Vincent Rucker, Phillip B. Alper, Daniel Mutnick, Donatella Chianelli
  • PYRAZOLOPYRIDINE DERIVATIVE OR PHARMACOLOGICALLY ACCEPTABLE SALT THEREOF
    Publication number: 20130331378
    Abstract: A pyrazolopyridine derivative represented by the following formula (I) or a pharmacologically acceptable salt thereof exhibits a strong EP1 receptor antagonistic effect. Thus, the derivative or the pharmacologically acceptable salt is useful as a therapeutic agent for lower urinary tract symptoms (LUTS), particularly, overactive bladder syndrome (OABs), or a prophylactic agent therefor and furthermore, is also useful in the treatment, prevention, or suppression of various pathological conditions in which the EP1 receptor is involved, such as inflammatory disease, pain disease, osteoporosis, and cancer. [A is a benzene ring or the like, Y1 is C1-6 alkylene, R1 is —C(?O)—OZ1 or the like, Z1 is H or the like, R2 is a branched C3-6 alkyl group or the like, R3 is H or the like, R4 is a hydrogen atom or the like, and R5 is a hydrogen atom or the like].
    Type: Application
    Filed: January 25, 2012
    Publication date: December 12, 2013
    Applicants: KISSEI PHARMACEUTICAL CO., LTD., KYORIN PHARMACEUTICAL CO., LTD.
    Inventors: Shigeki Seto, Kentaro Umei, Yosuke Nishigaya, Asao Tanioka, Tatsuhiro Kondo, Atsushi Kondo, Kazuya Tatani, Naohiro Kawamura
  • CONDENSED HETEROCYCLIC COMPOUND
    Publication number: 20130331409
    Abstract: The present invention provides a compound having a superior PDE10A inhibitory action and use thereof. The compound is a compound represented by the following formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.
    Type: Application
    Filed: March 15, 2012
    Publication date: December 12, 2013
    Inventors: Takahiko Taniguchi, Jun Kunitomo, Masato Yoshikawa, Tomoaki Hasui, Eiji Honda, Keisuke Imamura, Haruhi Kamisaki, Shinkichi Suzuki, Kasei Miura
  • COMPOUNDS AND COMPOSITIONS AS TRK INHIBITORS
    Publication number: 20130331397
    Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated TRK kinase activity.
    Type: Application
    Filed: February 23, 2012
    Publication date: December 12, 2013
    Applicant: IRM LLC
    Inventors: Valentina Molteni, Yi Fan, Jon Loren, Jeffrey M. Smith, Brenton T. Flatt
  • COMPOUNDS USEFUL AS MODULATORS OF TRPM8
    Publication number: 20130324557
    Abstract: The present invention includes compounds useful as modulators of TRPM8, such as compounds of Formula (I) and the subgenus and species thereof; personal products containing those compounds; and the use of those compounds and the personal products, particularly the use of increasing or inducing chemesthetic sensations, such as cooling or cold sensations.
    Type: Application
    Filed: November 4, 2011
    Publication date: December 5, 2013
    Applicant: SENOMYX, INC.
    Inventors: Chad Priest, Alain Noncovich, Andrew Patron, Jane Ung
  • IMIDAZOPYRIDINES AS RESPIRATORY SYNCYTIAL VIRUS ANTIVIRAL AGENTS
    Publication number: 20130324527
    Abstract: A compound satisfying formula I, a prodrug, N-oxide, addition salt, quaternary amine, metal complex, or a stereochemically isomeric form thereof: compositions contain these compounds as active ingredient and processes for preparing these compounds and compositions.
    Type: Application
    Filed: December 16, 2011
    Publication date: December 5, 2013
    Applicant: Janssen R&D Ireland
    Inventors: Ludwig Paul Cooymans, Lili Hu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdella Tahri, Steven Maurice Paula Van Hoof, Sandrine Marie Helene Vendeville
  • Histone Deacetylase Inhibitors
    Publication number: 20130317003
    Abstract: This invention relates to generally inhibiting histone deacetylase (“HDAC”) enzymes (e.g., HDAC1, HDAC2, and HDAC3).
    Type: Application
    Filed: March 15, 2013
    Publication date: November 28, 2013
    Inventor: Repligen Corporation
  • Fused bicyclic imidazoles
    Patent number: 8592591
    Abstract: Compounds of formula (I) a tautomer or stereoisomer thereof, or a salt thereof, wherein ring B and the imidazole to which it is fused, R4, R6 and R7 have the meanings as given in the description and the claims, are effective inhibitors of the Pi3K/Akt pathway.
    Type: Grant
    Filed: August 14, 2008
    Date of Patent: November 26, 2013
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Swen Hölder, Armin Zülch, Thomas Bär, Thomas Maier, Astrid Zimmermann, Thomas Beckers, Volker Gekeler, Hemant Joshi, Yogesh Munot, Umesh Bhise, Sunil Chavan, Sachin Shivatare, Sarvesh Patel, Vikas Gore
  • OXYGEN-CONTAINING FUSED RING DERIVATIVE AND ORGANIC ELECTROLUMINESCENCE DEVICE COMPRISING THE SAME
    Publication number: 20130306958
    Abstract: An oxygen-containing fused ring derivative represented by the following formula (1) wherein Ar1 is an m-valent fused ring group in which four or more rings including one or more rings selected from a furan ring and a pyran ring are fused and HAr is any of the nitrogen-containing heterocyclic group represented by the following formulas (2) to (5):
    Type: Application
    Filed: November 22, 2011
    Publication date: November 21, 2013
    Applicant: IDEMITSU KOSAN CO., LTD.
    Inventors: Hirokatsu Ito, Masahiro Kawamura, Yuichiro Kawamura, Yumiko Mizuki, Hiroyuki Saito
  • Ethynyl compounds useful for treatment of CNS disorders
    Patent number: 8586581
    Abstract: The present invention relates to ethynyl compounds of formula wherein X, Y, Z, and R4 are as defined herein or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5) and they are therefore useful for the treatment of diseases related to this receptor.
    Type: Grant
    Filed: December 10, 2010
    Date of Patent: November 19, 2013
    Assignee: Hoffmann-La Roche Inc
    Inventors: Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Heinz Stadler, Eric Vieira
  • Aminotetraline derivatives
    Patent number: 8586603
    Abstract: The present application relates to compounds of formula (I): and pharmaceutically acceptable salts and solvates thereof, wherein the substituents are as defined herein, compositions containing such compounds and the uses of such compounds in producing medicaments for the treatment of various diseases and conditions, such as of the central nervous system.
    Type: Grant
    Filed: December 20, 2010
    Date of Patent: November 19, 2013
    Inventors: Peter Gmeiner, Miriam Ruberg, Harald Hüebner
  • 1,3,4-OXADIAZOLE AND 1,3,4-THIADIAZOLE BETA-LACTAMASE INHIBITORS
    Publication number: 20130303504
    Abstract: ?-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D ?-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.
    Type: Application
    Filed: March 29, 2013
    Publication date: November 14, 2013
    Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III, Robert Busch
  • NAMPT INHIBITORS
    Publication number: 20130303508
    Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.
    Type: Application
    Filed: May 10, 2013
    Publication date: November 14, 2013
    Applicant: ABBVIE INC.
    Inventors: Richard F. Clark, Bryan Sorensen, Augustine T. Osuma, Robin Frey, Kenton Longenecker, George Doherty, Michael L. Curtin, Michael R. Michaelides, Ramzi F. Sweis, Marina A. Pliushchev, Andy Judd, Todd M. Hansen, Howard R. Heyman
  • NAMPT INHIBITORS
    Publication number: 20130303511
    Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.
    Type: Application
    Filed: May 10, 2013
    Publication date: November 14, 2013
    Applicant: AbbVie Inc.
    Inventors: Richard F. Clark, Bryan Sorensen, Augustine T. Osuma, Robin Frey, Kenton Longenecker, George Doherty, Michael L. Curtin, Michael R. Michaelides, Ramzi F. Sweis, Marina A. Pliushchev, Andy Judd, Todd M. Hansen, Howard R. Heyman
  • NOVEL COMPOUNDS USEFUL FOR THE TREATMENT OF METABOLIC AND INFLAMMATORY DISEASES
    Publication number: 20130303515
    Abstract: Compounds are disclosed that have a formula represented by the following: These compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example inflammatory conditions, infectious diseases, autoimmune diseases, diseases involving impairment of immune cell functions, cardiometabolic diseases, and/or proliferative diseases.
    Type: Application
    Filed: January 10, 2012
    Publication date: November 14, 2013
    Inventors: Laurent Raymond Maurice Sanière, Mathieu Rafaël Pizzonero, Nicolas Triballeau, Nick Ernest René Vandeghinste, Steve Irma Joel De Vos, Reginald Christophe Xavier Brys, Christelle Dominique Bénédicte Pourbaix-L'ebraly
  • Heteroaryl amide analogues as P2Xantagonists
    Patent number: 8580812
    Abstract: Heteroaryl amide analogues are provided, of Formula (I), wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
    Type: Grant
    Filed: April 9, 2008
    Date of Patent: November 12, 2013
    Assignee: H. Lundbeck A/S
    Inventors: David C. Ihle, Qin Guo, Kevin Hodgetts, Jun Yuan
  • BETA-LACTAMASE INHIBITORS
    Publication number: 20130296555
    Abstract: Aryl substituted diazabicyclooctanes (DBO) compounds that inhibit ?-lactamases of class A, class C or class D and potentiate ?-lactam antibiotics are disclosed. In particular, this disclosure provides DBO compounds that, when used in the disclosed Synergy MIC Assay with a ?-lactam antibiotic at a fixed concentration have an MIC of 8 ?g/mL or less against one or more isogenic ?-lactamase expressing bacterial strains.
    Type: Application
    Filed: March 29, 2013
    Publication date: November 7, 2013
    Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Robert Busch, Roland E. Dolle, Chester A. Metcalf, III
  • 1,3,4-OXADIAZOLE AND 1,3,4-THIADIAZOLE BETA-LACTAMASE INHIBITORS
    Publication number: 20130296291
    Abstract: ?-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D ?-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.
    Type: Application
    Filed: March 29, 2013
    Publication date: November 7, 2013
    Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III, Robert Busch
  • LIPOPROTEIN LIPASE-ACTIVATING COMPOSITIONS COMPRISING BENZENE DERIVATES
    Publication number: 20130296342
    Abstract: The present invention provides pharmaceutical compositions containing benzene compound(s) represented by General Formula (1) below and, particularly, LPL-activating compositions for use in hyperlipidemia therapeutic and preventive agents, anti-obesity agents, and the like: wherein R1, R2, R3 and R4 are as defined in the specification.
    Type: Application
    Filed: June 28, 2013
    Publication date: November 7, 2013
    Applicant: OTSUKA PHARMACEUTICAL FACTORY, INC.
    Inventors: Irina NEAGU, Michael OHLMEYER, Vidyadhar M. PARADKAR, Kurt W. SAIONZ, Koushi IWATA, Takashi OKAMURA, Tadao SHIBUTANI
  • 1,3,4-OXADIAZOLE AND 1,3,4-THIADIAZOLE BETA-LACTAMASE INHIBITORS
    Publication number: 20130296293
    Abstract: ?-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D ?-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.
    Type: Application
    Filed: March 29, 2013
    Publication date: November 7, 2013
    Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III, Robert Busch
  • 1,3,4-OXADIAZOLE AND 1,3,4-THIADIAZOLE BETA-LACTAMASE INHIBITORS
    Publication number: 20130296290
    Abstract: ?-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D ?-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.
    Type: Application
    Filed: March 29, 2013
    Publication date: November 7, 2013
    Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III, Robert Busch
  • 1,3,4-OXADIAZOLE AND 1,3,4-THIADIAZOLE BETA-LACTAMASE INHIBITORS
    Publication number: 20130296292
    Abstract: ?-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D ?-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.
    Type: Application
    Filed: March 29, 2013
    Publication date: November 7, 2013
    Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III, Robert Busch
  • NOVEL COMPOUNDS AND COMPOSITIONS FOR THE INHIBITION OF NAMPT
    Publication number: 20130295051
    Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below.
    Type: Application
    Filed: September 2, 2011
    Publication date: November 7, 2013
    Inventors: Kenneth W. Bair, Alexandre J. Buckmelter, Bingsong Han, Jian Lin, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Xiaozhang Zheng
  • 1,2,4-OXADIAZOLE AND 1,2,4-THIADIAZOLE BETA-LACTAMASE INHIBITORS
    Publication number: 20130289012
    Abstract: ?-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D ?-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.
    Type: Application
    Filed: March 29, 2013
    Publication date: October 31, 2013
    Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III, Robert Busch
  • IMIDAZO[1,2-a]PYRIDINE COMPOUNDS
    Publication number: 20130289013
    Abstract: Imidazo[1,2-a]pyridines are disclosed. Compounds of the invention are useful therapeutic agents and their inclusion in pharmaceutical formulations and use in methods of treatment are disclosed.
    Type: Application
    Filed: June 24, 2013
    Publication date: October 31, 2013
    Inventors: Qun Kevin FANG, Frank Xinhe Wu, Paul T. Grover, Seth C. Hopkins, Una Campbell, Milan Chytil, Kerry L. Spear
  • Compounds and compositions as c-Kit kinase inhibitors
    Patent number: 8569283
    Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit or c-kit and PDGFR (PDGFR?, PDGFR?) kinases.
    Type: Grant
    Filed: August 29, 2012
    Date of Patent: October 29, 2013
    Inventors: Valentina Molteni, Hank Michael James Petrassi, Xiaolin Li, Xiaodong Liu, Jon Loren, Juliet Nabakka, Bao Nguyen, Vince Yeh
  • Imidazopyridine compound
    Patent number: 8569504
    Abstract: For the prevention and/or treatment of chymase-mediated diseases such as skin diseases, circulatory diseases, digestive system diseases, respiratory diseases, liver diseases, ocular diseases or the like, a drug is provided having as an active ingredient a compound having extremely strong chymase inhibitory activity, high safety, and high metabolic stability. The compound represented by the formula (I): wherein all symbols have the same meanings as in the description, a salt thereof, an N-oxide thereof or a solvate thereof, or a prodrug thereof, is useful as a pharmaceutical ingredient having chymase inhibitory activity for preventing and/or treating of chymase-mediated disease, such as skin diseases, circulatory diseases, digestive system diseases, respiratory diseases, liver diseases, ocular diseases or the like.
    Type: Grant
    Filed: June 16, 2010
    Date of Patent: October 29, 2013
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Jun Takeuchi, Takayuki Inukai, Masaru Sakai
  • NEW BICYCLIC COMPOUNDS AND THEIR USE AS ANTIBACTERIAL AGENTS AND BETA-LACTAMASE INHIBITORS
    Publication number: 20130281359
    Abstract: A compound of formula (I): wherein: M is hydrogen or a pharmaceutically acceptable salt-forming cation; and R1 and M are as defined herein. Also, methods of treating bacterial infection, pharmaceutical compositions, molecular complexes and processes for preparing compounds.
    Type: Application
    Filed: June 14, 2013
    Publication date: October 24, 2013
    Inventors: Samarendra N. MAITI, Dai Nguyen, Jehangir Khan, Rong Ling
  • ANTI-ABUSE GELLED PHARMACEUTICAL COMPOSITIONS
    Publication number: 20130274280
    Abstract: This invention provides an oral pharmaceutical composition comprising a physiologically tolerable gelled oil-in-water emulsion containing a drug of abuse.
    Type: Application
    Filed: April 11, 2011
    Publication date: October 17, 2013
    Applicant: AYANDA GROUP AS
    Inventors: Kurt Ingar Draget, Ingvild Johanne Haug, Steinar Johan Engelsen, Tore Seternes, Magnus N. Hattrem
  • Chemical Compounds
    Publication number: 20130274243
    Abstract: The invention relates to benzimidazole and imidazopyridine derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new Nav1.8 modulators of formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, X and Y are as defined in the description. Nav1.8 modulators are potentially useful in the treatment of a wide range of disorders, particularly pain.
    Type: Application
    Filed: January 29, 2013
    Publication date: October 17, 2013
    Inventors: Sharanjeet Kaur Bagal, Alan Daniel Brown, Mark Ian Kemp, Wolfgang Klute, Laia Malet Sanz, Brian Edward Marron, Duncan Charles Miller, Sarah Elizabeth Skerratt, Mark J. Suto, Christopher William West
  • BETA-LACTAMASE INHIBITORS
    Publication number: 20130274475
    Abstract: Substituted bicyclic beta-lactams of Formula I: are ?-lactamase inhibitors, wherein a, X, R1 and R2 are defined herein. The compounds and pharmaceutically acceptable salts thereof are useful in the treatment of bacterial infections in combination with ?-lactam antibiotics. In particular, the compounds can be employed with a ?-lactam antibiotics (e.g., imipenem, piperacillin, or ceftazidime) against microorganisms resistant to ?-lactam antibiotics due to the presence of the ?-lactamases.
    Type: Application
    Filed: June 6, 2013
    Publication date: October 17, 2013
    Inventors: Ian MANGION, Nelo Rivera, Rebecca T. Ruck, Michael Shelvin
  • NOVEL COMPOUNDS AND COMPOSITIONS FOR THE INHIBITION OF NAMPT
    Publication number: 20130273034
    Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes.
    Type: Application
    Filed: September 2, 2011
    Publication date: October 17, 2013
    Inventors: Kenneth W. Bair, Timm R. Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Bingsong Han, Jian Lin, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Xiaozhang Zheng, Po-Wai Yuen
  • COMPOUNDS AND METHODS FOR ANTIVIRAL TREATMENT
    Publication number: 20130273037
    Abstract: Compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections are provided. The compounds and compositions are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.
    Type: Application
    Filed: April 17, 2013
    Publication date: October 17, 2013
    Inventors: Dustin Siegel, David Sperandio, Hai Yang, Michael Sangi, Jay P. Parrish, Hon Chung Hui
  • NOVEL CRYSTALLINE FORMS OF TRANS-7-OXO-6-(SULPHOOXY)-1,6-DIAZABICYCLO[3,2,1]OCTANE-2-CARBOXAMIDE SODIUM SALT
    Publication number: 20130267480
    Abstract: The present invention relates to novel crystalline forms of sodium salt of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide (e.g., NXL-104) thereof. The present invention relates to compositions comprising a crystalline form of sodium salt of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide (e.g., NXL-104) alone or in combination with an antibacterial agent (e.g., ceftaroline fosamil). Processes for the preparation of the crystalline forms and methods of treating bacterial infections by administering the crystalline forms alone or in combination with an antibacterial agent (e.g., ceftaroline fosamil) are also described.
    Type: Application
    Filed: May 24, 2013
    Publication date: October 10, 2013
    Inventors: Mahendra G. Dedhiya, Sisir Bhattacharya, Véronique Ducandas, Alexandre Giuliani, Valérie Ravaux, Alain Bonnet, Alain Priour, Peter Spargo
  • INDAZOLE DERIVATIVES USEFUL AS ERK INHIBITORS
    Publication number: 20130261125
    Abstract: The present invention provides a compound of the Formula I, or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R1, R2, R3, m and are as defined herein. The compounds are ERK inhibitors. Also disclosed are pharmaceutical compositions that comprise the above compounds, and methods of treating cancer using the same.
    Type: Application
    Filed: December 16, 2011
    Publication date: October 3, 2013
    Inventors: Gerald W. Shipps, JR., Xiaohua Huang, Yongqi Deng, Liang Zhu, Alan B. Cooper, Binyuan Sun, Abdelghani Achab, Sie-Mun Lo
  • Compounds that modulate intracellular calcium
    Patent number: 8546403
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Grant
    Filed: April 12, 2011
    Date of Patent: October 1, 2013
    Assignee: Calcimedica, Inc.
    Inventors: Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • Acetylene derivatives of 5-phenyl-pyrazolopyridine, preparation thereof, and therapeutic use thereof
    Patent number: 8546424
    Abstract: Compounds of formula (I): in which: R1 and R2 represent, independently of one another, a hydrogen atom or a (C1-C6)alkyl group, R3 represents one or more hydrogen or halogen atoms, X represents from 1 to 4 substituents, identical to or different from one another, chosen from hydrogen, halogen or (C1-C6)alkyl, in the form of the base or of an addition salt with an acid. Therapeutic use and synthetic process.
    Type: Grant
    Filed: September 17, 2010
    Date of Patent: October 1, 2013
    Assignee: Sanofi
    Inventors: Florian Auger, Luc Even
  • Imidazoisoindole neuropeptide S receptor antagonists
    Patent number: 8541595
    Abstract: The present invention is directed to imidazoisoindole compounds which are antagonists of neuropeptide S receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which the neuropeptide S receptor is 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 the neuropeptide S receptor is involved.
    Type: Grant
    Filed: November 3, 2009
    Date of Patent: September 24, 2013
    Assignee: Merch Sharp & Dohme Corp.
    Inventors: Peter J. Manley, Kausik K Nanda, B. Wesley Trotter
  • Compounds that modulate intracellular calcium
    Publication number: 20130245025
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: January 3, 2013
    Publication date: September 19, 2013
    Applicant: CalciMedica, Inc.
    Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • Positive Allosteric Modulators of MGLUR2
    Publication number: 20130245042
    Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds modulate the mGluR2 receptor and may be useful for the treatment of various disorders of the central nervous system.
    Type: Application
    Filed: March 14, 2013
    Publication date: September 19, 2013
    Inventors: Ronald J. Mattson, Zhaoxing Meng
  • AZA-indoles and related compounds having sphingosine-1-phosphate (S1P) receptor antagonist biological activity
    Patent number: 8536339
    Abstract: The present invention provides compounds are disclosed herein having the formula: Wherein n is 1 or 2; m is 0 or 1; p is 0, 1 or 2; R1 is aryl, heteroaryl or alkyl; R2 is C1-6 hydrocarbyl, alkylacyl or hydroxyalkyl; R3 is aryl, heteroaryl, or alkyl; R4 is H, OH, —O—(C1-6 alkyl), —NH—(C1-6 alkyl), or oxide; R5 is H, halogen, C1-6 alkyl, O—(C1-6 alkyl), aryl, heteroaryl, —C(?O)(C1-6 alkyl), substituted or un-substituted oxazolin-2-yl; X?O, NH, —C(?O)— or —N?CH—; and Each L is independently alkylene and carbonyl. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: August 1, 2011
    Date of Patent: September 17, 2013
    Assignee: Allergan, Inc.
    Inventors: Haiqing Yuan, Richard L. Beard
  • NOVEL COMPOUNDS THAT ARE ERK INHIBITORS
    Publication number: 20130237518
    Abstract: Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof, wherein: A is a five membered monocyclic heteroaryl ring; and B is a monocyclic heterocycloalkyl ring, or a monocyclic heterocycloalkenyl ring, or a bridged monocyclic heterocycloalkyl ring, or a fused (monocyclic heterocycloalkyl ring) cyclopropyl ring. Also disclosed are methods of treating cancer using the compounds of formula (1).
    Type: Application
    Filed: October 24, 2011
    Publication date: September 12, 2013
    Inventors: Sobhana Babu Boga, Joseph M. Kelly, Hugh Y. Zhu, Abdul-Basit Alhassan, Xin Yao, Xiaolei Gao, James J-S Wang, Jagdish A. Desai, Subrahmanyam Gudipati, Sie-Mun Lo, Liang Zhu, Alan B. Cooper, Yongqi Deng, Gerald W. Shipps, JR.
  • BICYCLIC HETEROCYCLE DERIVATIVES FOR THE TREATMENT OF PULMONARY ARTERIAL HYPERTENSION
    Publication number: 20130237519
    Abstract: Bicyclic heterocyclic derivatives of formula I useful in inhibiting PDGF receptor mediated biological activity. wherein A is and R1, R1a, R2, R3, R4, R5, R6 and X are as defined herein.
    Type: Application
    Filed: August 30, 2012
    Publication date: September 12, 2013
    Inventors: Ian Bruce, Sylvie Chamoin, Stephen Paul Collingwood, Pascal Furet, Vikki Furminger, Diana Janus, Sarah Lewis, Jon Christopher Loren, Valentina Molteni, Alex Michael Saunders, Duncan Shaw, Lilya Sviridenko, Christopher Thomson, Ryan West, Vince Yeh