Bicyclo Ring Having The Additional Six-membered Nitrogen Hetero Ring As One Of The Cyclos Patents (Class 514/253.04)
Isoquinolines (including hydrogenated) (Class 514/253.05)
Quinolines (including hydrogenated) (Class 514/253.06)
  • 1,6-Diazabicyclo [3,2,1] octan-7-one derivatives and their use in the treatment of bacterial infections
    Publication number: 20140088068
    Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infections are disclosed.
    Type: Application
    Filed: August 24, 2012
    Publication date: March 27, 2014
    Inventors: Sachin Bhagwat, Prasad Keshav Deshpande, Satish Bhawsar, Vijaykumar Jagdishwar Patil, Ravikumar Tadiparthi, Shivaji Sampatrao Pawar, Sunil Bhaginath Jadhav, Sanjay Kisan Dabhade, Vikas Vitthalrao Deshmukh, Bharat Dond, Satish Birajdar, Mohammad Usman Shaikh, Deepak Dekhane, Piyush Ambalal Patel
  • Fused pyridine derivatives
    Patent number: 8680089
    Abstract: Fused pyridine derivatives shown as the general formula (I), and their pharmaceutically acceptable salts, stereoisomers or solvates thereof are disclosed, which belong to the technical field of medicines. The R1, R2, R3, Q, X and Y substituents in formula (I) are defined as in the description. Also disclosed are the preparation methods, pharmaceutical compositions comprising the compounds and uses of the compounds in the manufacture of the medicine for the treatment and/or prevention of noninsulin-dependent diabetes, hyperglycemia, hyperlipidemia and insulin resistance.
    Type: Grant
    Filed: January 17, 2011
    Date of Patent: March 25, 2014
    Assignee: Xuanzhu Pharma Co., Ltd.
    Inventors: Zhenhua Huang, Yan Zhang, Yuntao Song
  • Substituted Imidazopyridinyl-Aminopyridine Compounds
    Publication number: 20140073635
    Abstract: The present invention relates to substituted imidazopyridinyl-aminopyridine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl-aminopyridine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Application
    Filed: November 8, 2013
    Publication date: March 13, 2014
    Inventors: Mark A. Ashwell, Chris Brassard, Anton Filikov, Jason Hill, Steffi Koerner, Jean-Marc Lapierre, Yanbin Liu, Nivedita Namdev, Robert Nicewonger, Rocio Palma, Manish Tandon, David Vensel, Akihisa Matsuda, Shin Iimura, Kenichi Yoshida, Takanori Yamazaki, Takahiro Kitamura, Takeshi Isoyama
  • ANTIVIRAL AND ANTIMICROBIAL COMPOUNDS
    Publication number: 20140073631
    Abstract: Disclosed are guanidine and biguanidine derivatives which have anti-viral and antibacterial activity. Also disclosed are pharmaceutical compositions containing such compounds as an active ingredient, and anti-viral and anti-bacterial methods utilizing such compounds. Methods of treating infections using the guanidine and biguanidine derivatives are also disclosed.
    Type: Application
    Filed: September 10, 2013
    Publication date: March 13, 2014
    Applicant: Vymed Corporation
    Inventor: B. Vithal SHETTY
  • Methods and Compositions for Treating Parkinson's Disease
    Publication number: 20140066434
    Abstract: The invention discloses methods and compositions for treating or preventing Parkinson's disease by administering a compound of Formula (I): or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the variables are defined as herein.
    Type: Application
    Filed: April 6, 2012
    Publication date: March 6, 2014
    Applicant: ARIAD PHARMACEUTICALS, INC.
    Inventor: William C. Shakespeare
  • SERINE/THREONINE KINASE INHIBITORS
    Publication number: 20140066453
    Abstract: Compounds having the formula I wherein R2, X and Z as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders.
    Type: Application
    Filed: August 27, 2013
    Publication date: March 6, 2014
    Applicants: Genentech, Inc., Array BioPharma Inc.
    Inventors: Jim Blake, Huifen Chen, Mark Chicarelli, John Gaudino, Lewis Gazzard, Sam Kintz, Pete Mohr, Kirk Robarge, Jacob Schwarz, Aihe Zhou
  • TRAZODONE AND TRAZODONE HYDROCHLORIDE IN PURIFIED FORM
    Publication number: 20140057922
    Abstract: A process of production of trazodone or trazodone hydrochloride that comprises: (a) preparing an organic phase comprising trazodone in at least one organic solvent; (b) preparing an aqueous phase comprising at least one basic compound; (c) mixing said aqueous phase with said organic phase; (d) heating at a temperature of at least 40° C. for at least 30 minutes; (e) recovering said trazodone; and, optionally, (f) treating said trazodone with hydrochloric acid to obtain trazodone hydrochloride. Trazodone or trazodone hydrochloride comprising less than 15 ppm of allylating substances, and a pharmaceutical composition comprising said trazodone hydrochloride.
    Type: Application
    Filed: November 6, 2013
    Publication date: February 27, 2014
    Applicant: AZIENDE CHIM. RIUN. ANG. FRANC. A.C.R.A.F. S.p.A.
    Inventors: Marcello MARCHETTI, Tommaso Iacoangeli, Giovanni Battista Ciottoli, Giuseppe Biondi
  • Substituted 6,5-Fused Bicyclic Heteroaryl Compounds
    Publication number: 20140057891
    Abstract: The present invention relates to substituted 6,5-fused bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Application
    Filed: November 4, 2013
    Publication date: February 27, 2014
    Applicant: Epizyme, Inc.
    Inventors: Kevin Wayne Kuntz, Edward James Olhava, Richard Chesworth, Kenneth William Duncan
  • METHODS OF TREATING A DISEASE OR CONDITION OF THE CENTRAL NERVOUS SYSTEM
    Publication number: 20140051701
    Abstract: The present invention provides methods of treating central nervous system disorders, such as mood disorders (e.g., depression) and neurodegenerative diseases using compounds of formula (I). The subject disclosure enables the manufacture of medicaments as well as compositions containing same for use in methods of therapy and prophylaxis of central nervous system disorders.
    Type: Application
    Filed: March 2, 2012
    Publication date: February 20, 2014
    Applicant: Bionomics Limited
    Inventors: Sue O'Connor, Andrew John Harvey, Stephanie Wagner, Emile Andriambeloson
  • NOVEL COMPOUND USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES
    Publication number: 20140051677
    Abstract: Novel pyrrazolopyridines according to Formula I, able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prophylaxis and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergy, inflammatory conditions, autoimmune diseases, proliferative diseases, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons.
    Type: Application
    Filed: April 26, 2012
    Publication date: February 20, 2014
    Inventors: Christel Jeanne Marie Menet, Alastair James Hodges, Huw David Vater
  • METHODS AND COMPOSITIONS FOR TREATING NEURODEGENERATIVE DISEASES
    Publication number: 20140045826
    Abstract: The invention discloses methods and compositions for treating or preventing neurodegenerative disease by administering a compound of Formula I: or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the variables are defined as herein.
    Type: Application
    Filed: April 6, 2012
    Publication date: February 13, 2014
    Applicant: ARIAD PHARMACEUTICALS, INC.
    Inventors: William C. Shakespeare, Frank G. Haluska
  • SUBSTITUTED 1,3-BENZOTHIAZOL-2(3H)-ONES AND [1,3]THIAZOLO[5,4-B]PYRIDIN-2(1H)-ONES AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2
    Publication number: 20140045829
    Abstract: The present invention is directed to benzothiazol-one and thiazolo pyridine-one derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
    Type: Application
    Filed: October 8, 2013
    Publication date: February 13, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: MARK E. LAYTON, Michael J. Kelly
  • NOVEL ANXIOLYTIC COMPOUNDS
    Publication number: 20140045839
    Abstract: The present invention relates to chemical compounds of general formula (I) which may possess useful therapeutic activity in a range of central nervous system disorders, and in particular, anxiety disorders.
    Type: Application
    Filed: September 18, 2013
    Publication date: February 13, 2014
    Applicant: Bionomics Limited
    Inventors: Jonathan Bayldon Baell, Brad Sleebs, Bernard Luke Flynn, Ian Phillip Street, Nurul Quazi, Chinh Thien Bui
  • TREATMENT REGIMENS
    Publication number: 20140038985
    Abstract: The invention further relates to compounds, pharmaceutical compositions and methods for treating sexual disorder (SD) in a subject.
    Type: Application
    Filed: October 3, 2013
    Publication date: February 6, 2014
    Applicant: S1 Pharmaceuticals, Inc.
    Inventor: Nicolas G. Sitchon
  • HUMAN PAPILLOMA VIRUS AS PREDICTOR OF CANCER PROGNOSIS
    Publication number: 20140037622
    Abstract: Methods of treating a head and neck cancer are disclosed.
    Type: Application
    Filed: August 2, 2013
    Publication date: February 6, 2014
    Applicants: UCL BUSINESS PLC, FOUNDATION MEDICINE, INC.
    Inventors: Chris Hendrik Boshoff, Timothy Robert Fenton, Matthias Alexander Lechner, Philip James Stephens, Matthew J. Hawryluk, Roman Yelensky, Garrett Michael Frampton
  • TRIAZOLOPYRIDINE JAK INHIBITOR COMPOUNDS AND METHODS
    Publication number: 20140038939
    Abstract: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined herein, are useful as JAK kinase inhibitors. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of JAK kinase activity in a patient are disclosed.
    Type: Application
    Filed: October 9, 2013
    Publication date: February 6, 2014
    Applicant: Genentech, Inc.
    Inventors: Bing-Yan Zhu, Michael Siu, Steven R. Magnuson, Richard Pastor, He Haiying, Xiao Yisong, Zheng Jifu, Xu Xing, Zhao Junping, Christopher Hurley, Jun Liang, Wendy Liu, Joseph P. Lyssikatos
  • ISOINDOLINONE INHIBITORS OF PHOSPHATIDYLINOSITOL 3-KINASE
    Publication number: 20140038936
    Abstract: The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3K?. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Application
    Filed: May 7, 2013
    Publication date: February 6, 2014
    Inventors: Alex Aronov, Jon H. Come, Robert J. Davies, Albert Charles Pierce, Philip N. Collier, Ronald Lee Grey, Hardwin O'Dowd, James A. Henderson, Elaine B. Krueger, Anne-Laure Grillot, Arnaud Le Tiran, Yusheng Liao, David Messersmith, Jian Wang, Jingrong Cao, Upul Keerthi Bandarage, Suganthini S. Nanthakumar
  • HETEROARYL AMIDE ANALOGUES AS P2X7 ANTAGONISTS
    Publication number: 20140038955
    Abstract: Heteroaryl amide analogues are provided, of the Formula: 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: Application
    Filed: October 2, 2013
    Publication date: February 6, 2014
    Applicant: H. Lundbeck A/S
    Inventors: David C. IHLE, Qin GUO, Kevin HODGETTS, Jun YUAN
  • Hetaryl-[1,8]naphthyridine derivatives
    Publication number: 20140038960
    Abstract: Novel hetaryl-[1,8]naphthyridine derivatives of formula (I) wherein R1, R2, W1, W3, W5 and W6 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.
    Type: Application
    Filed: October 4, 2013
    Publication date: February 6, 2014
    Applicant: MERCK PATENT GMBH
    Inventors: Alfred Jonczyk, Dieter Dorsch, Guenter Hoelzemann, Christiane Amendt, Frank Zenke
  • NOVEL (HETEROCYCLE/CONDENSED PIPERIDINE)-(PIPERAZINYL)-1-ALKANONE OR (HETEROCYCLE/CONDENSED PYRROLIDINE)-(PIPERAZINYL)-1-ALKANONE DERIVATIVES AND USE THEREOF AS p75 INHIBITORS
    Publication number: 20140038946
    Abstract: The disclosure relates to (heterocycle-fused piperidine)-(piperazinyl)-1-alkanone derivatives and (heterocycle-fused pyrrolidine)-(piperazinyl)-1-alkanone derivatives of formula (I): wherein A, W, R2 and n are as defined in the disclosure, to the method of preparation thereof and the therapeutic use thereof.
    Type: Application
    Filed: October 8, 2013
    Publication date: February 6, 2014
    Applicant: SANOFI
    Inventors: Marco BARONI, Francoise BONO, Sandrine DELBARY-GOSSART, Valentina VERCESI
  • 1,4-DISUBSTITUTED 1,2,3-TRIAZOLES, METHODS FOR PREPARING SAME, AND DIAGNOSTIC AND THERAPEUTIC USES THEREOF
    Publication number: 20140030191
    Abstract: A compound having the following general formula (I): wherein: X is a nitrogen atom and Y is a carbon atom; or X is a carbon atom and Y is a nitrogen atom; the Ar group is an aryl or heteroaryl group; and the RN and RN? groups, together with the carbon atoms to which they are bound, form a monocyclic or bicyclic azacycloalkane group. The pharmaceutically acceptable salts thereof, the hydrates or polymorphic crystalline structures thereof, and to the racemates, diastereoisomers, or enantiomers thereof are also described.
    Type: Application
    Filed: April 20, 2012
    Publication date: January 30, 2014
    Applicant: Centre National de la Recherche Scientifique (C.N.R.S.)
    Inventors: Sylvain Routier, Franck Suzenet, Frederic Pin, Sylvie Chalon, Johnny Vercouillie, Denis Guilloteau
  • Azaindazoles
    Patent number: 8637509
    Abstract: Herein are disclosed azaindazoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.
    Type: Grant
    Filed: May 5, 2011
    Date of Patent: January 28, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Joelle Lorraine Burgess, Neil Johnson, Steven D. Knight, Louis LaFrance, William H. Miller, Kenneth Newlander, Stuart Romeril, Meagan B. Rouse, Xinrong Tian, Sharad Kumar Verma, Dominic Suarez
  • PATCH PREPARATION
    Publication number: 20140023695
    Abstract: A patch preparation containing a support and an adhesive layer formed on one surface of the support, wherein the adhesive layer contains 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine or a physiologically acceptable acid addition salt thereof, an acrylic polymer, lactic acid, sesame oil and one or more kinds of stabilizers selected from 2-mercaptobenzimidazole, 2,6-di-tert-butyl-4-methylphenol and propyl gallate. A patch preparation containing a support and an adhesive layer containing lactic acid and magnesium aluminometasilicate and formed on at least one surface of the support, which preparation is superior in both skin permeability and adhesiveness in the presence of water.
    Type: Application
    Filed: February 1, 2012
    Publication date: January 23, 2014
    Inventors: Yasuaki Okada, Katsuhiro OKada, Masato Nishimura, Yuji Kawaharada, Hiroo Maeda, Kazumitsu Yamamoto, Masayasu Tanaka
  • JANUS KINASE 2 (JAK2) INHIBITOR FOR THE TREATMENT OF LUPUS
    Publication number: 20140024655
    Abstract: The present invention provides a method for treating lupus in a subject, comprising the step of administering to the subject COMPOUND A
    Type: Application
    Filed: June 6, 2013
    Publication date: January 23, 2014
    Applicant: Cephalon, Inc.
    Inventors: Pawel T. Dobrzanski, Matthew M. Seavey
  • Benzenesulfonamide compounds, method for synthesizing same, and use thereof in medicine as well as in cosmetics
    Patent number: 8633196
    Abstract: Benzenesulfonamide compounds having a structure of formula (I) are described. Also described, are methods for synthesizing the compounds and to the use thereof in pharmaceutical compositions for human or veterinary medicine and in cosmetic compositions.
    Type: Grant
    Filed: February 22, 2013
    Date of Patent: January 21, 2014
    Assignee: Galderma Research & Development
    Inventors: Laurence Clary, Sandrine Chambon, Laurent Chantalat, Carine Rosignoli, Olivier Roye, Jean-Claude Pascal, Marlène Schuppli-Nollet
  • Preparation and uses of 1,2,4-triazolo [1,5a] pyridine derivatives
    Patent number: 8633173
    Abstract: This application relates, in part, to compounds of the general Formula I and/or salts thereof, wherein X, R1A, R1B, R2, R3, R4, and R5 are as defined herein. The application also relates to compositions and methods of inhibiting at least JAK2 in subjects in recognized need thereof for the treatment of diseases or disorders for which inhibition of at least JAK2 is indicated.
    Type: Grant
    Filed: June 18, 2013
    Date of Patent: January 21, 2014
    Assignee: Cephalon, Inc
    Inventors: Matthew A. Curry, Bruce D. Dorsey, Benjamin J. Dugan, Diane E. Gingrich, Eugen F. Mesaros, Karen L. Milkiewicz
  • INHIBITION OF ENZYMES
    Publication number: 20140018345
    Abstract: Compounds of formula (I): wherein R1, R2, R3, R5, R6, A1, A2, A3, A4 assume meanings as defined in formula (I) are inhibitors of neutrophil elastase.
    Type: Application
    Filed: July 12, 2013
    Publication date: January 16, 2014
    Applicant: CHIESI FARMACEUTICI S.p.A
    Inventors: Carmelida Capaldi, Robert Andrew Heald, Nicholas Charles Ray, Jonathan Mark Sutton
  • PYRAZOLE DERIVATIVES AS ERK INHIBITORS
    Publication number: 20140011806
    Abstract: This invention describes substituted pyrazole derivatives of Formula I and methods of making and using the compounds. These compounds have utility in the treatment of conditions or diseases in which modification of the activity of ERK would have a positive therapeutic outcome, for instance various cancers, psoriasis and actinic keratosis.
    Type: Application
    Filed: January 3, 2012
    Publication date: January 9, 2014
    Applicant: KINENTIA BIOSCIENCES LLC
    Inventors: David Fairfax, Russell Joseph Deorazio
  • WNT PATHWAY ANTAGONISTS
    Publication number: 20140005164
    Abstract: The present invention relates to novel compounds of formula (I): as herein described and pharmaceutical compositions thereof. The compounds of formula (I) have inhibitory effect on the Wnt pathway and are therefore useful in the preparation of a medicament, in particular for the treatment of cancer.
    Type: Application
    Filed: March 23, 2012
    Publication date: January 2, 2014
    Applicant: Siena Biotech S.p.A.
    Inventors: Maurizio Varrone, Massimiliano Travagli, Giacomo Minetto, Lucia Cesari, Simone Galeazzi, Andrea Caricasole, Antonio Chiumiento, Massimiliano Salerno
  • INDAZOLE INHIBITORS OF THE WNT SIGNAL PATHWAY AND THERAPEUTIC USES THEREOF
    Publication number: 20140005170
    Abstract: Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Application
    Filed: September 6, 2013
    Publication date: January 2, 2014
    Applicant: Samumed, LLC
    Inventors: John Hood, David Mark Wallace, Sunil Kumar KC
  • 5-AZAINDAZOLE COMPOUNDS AND METHODS OF USE
    Publication number: 20140005168
    Abstract: 5-Azaindazole compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: June 26, 2013
    Publication date: January 2, 2014
    Inventors: Steven Do, Huiyong Hu, Aleksandr Kolesnikov, Vickie H. Tsui, Xiaojing Wang
  • Compositions and methods for apoptosis modulators
    Patent number: 8618110
    Abstract: The present invention includes and relates generally to compounds of structural Formula (I), or a salt, solvate, or prodrug thereof, which modulate apoptosis in cells. The present invention also provides pharmaceutical compositions containing these compounds, methods of making these compounds, and methods of using these compounds and pharmaceutical compositions for treatment of diseases associated with irregular apoptosis in cells.
    Type: Grant
    Filed: February 9, 2010
    Date of Patent: December 31, 2013
    Assignee: VM Discovery Inc.
    Inventors: Jay Jie-Qiang Wu, Ling Wang
  • PYRROLOPYRIDINEAMINO DERIVATIVES AS MPS1 INHIBITORS
    Publication number: 20130345181
    Abstract: The present invention relates to the use of certain pyrrolopyridineamino derivatives (hereinafter referred to as “PPA derivatives”), particularly 1H-pyrrolo[3,2-c]pyridine-6-amino derivatives, to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps kinase itself. In particular, the present invention relates to PPA derivatives for use as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of the PPA derivatives, and pharmaceutical compositions comprising them.
    Type: Application
    Filed: March 14, 2012
    Publication date: December 26, 2013
    Applicant: CANCER RESEARCH TECHNOLOGY LIMITED
    Inventors: Vassilios Bavetsias, Butrus Atrash, Sébastien Gaston André Naud, Peter William Sheldrake, Julian Blagg
  • AZAINDOLES USEFUL AS INHIBITORS OF JAK AND OTHER PROTEIN KINASES
    Publication number: 20130345197
    Abstract: The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Application
    Filed: June 3, 2013
    Publication date: December 26, 2013
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Francesco Salituro, Luc Farmer, Randy Bethiel, Edmund Harrington, Jeremy Green, John Court, Jon Come, David Lauffer, Alex Aronov, Hayley Binch, Dean Boyall, Jean-Damien Charrier, Simon Everitt, Damien Fraysse, Michael Mortimore, Francoise Pierard, Daniel Robinson, Jian Wang, Joanne Pinder, Tiansheng Wang, Albert Pierce
  • PYRAZOLOPYRIMIDONE AND PYRAZOLOPYRIDONE INHIBITORS OF TANKYRASE
    Publication number: 20130345215
    Abstract: There are provided compounds of the formula or a pharmaceutically acceptable salt thereof, wherein Q, R1 and R2 are as defined herein. The compounds of formula I are useful in the treatment of cancer.
    Type: Application
    Filed: June 6, 2013
    Publication date: December 26, 2013
    Inventors: Jianwen Feng, Nancy-Ellen Haynes, Johannes Cornelius Hermann, Kyungjin Kim, Jin-Jun Liu, Nathan Robert Scott, Lin Yi, Mark Edward Zak, Guiling Zhao
  • HETEROCYCLIC TYROSINE KINASE INHIBITORS
    Publication number: 20130345192
    Abstract: The present invention provides compounds useful as inhibitors of Tec family kinases, compositions thereof, and methods of using the same.
    Type: Application
    Filed: October 28, 2011
    Publication date: December 26, 2013
    Applicants: SUNESIS PHARMACEUTICALS, INC., BIOGEN IDEC MA INC.
    Inventors: Brian T. Hopkins, Daniel Scott, Patrick Conlon, Tracy J. Jenkins, Noel Powell, Bing Guan, Julio H. Cuervo, Deping Wang, Art Taveras
  • IMIDAZOPYRIDIN-2-ONE DERIVATIVES
    Publication number: 20130338156
    Abstract: A compound represented by formula (I) having mTOR inhibitory activity or a pharmacologically acceptable salt thereof.
    Type: Application
    Filed: March 13, 2013
    Publication date: December 19, 2013
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventor: DAIICHI SANKYO COMPANY, LIMITED
  • AZAINDAZOLE COMPOUNDS AND METHODS OF USE
    Publication number: 20130338157
    Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.
    Type: Application
    Filed: February 22, 2013
    Publication date: December 19, 2013
    Applicant: Chemocentryx, Inc.
    Inventors: Penglie Zhang, Andrew M.K. Pennell, John J. Kim Wright, Wei Chen, Manmohan R. Leleti, Yandong Li, Lianfa Li, Yuan Xu, Mark M. Gleason, Yibin Zeng, Kevin Lloyd Greenman
  • Hepatitis C virus inhibitors
    Patent number: 8609648
    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: June 15, 2010
    Date of Patent: December 17, 2013
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yat Sun Or, Lu Ying, Xiaowen Peng, Datong Tang, Ce Wang, Yao-Ling Qiu
  • 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
  • PYRROLOPYRIMIDONE AND PYRROLOPYRIDONE INHIBITORS OF TANKYRASE
    Publication number: 20130331375
    Abstract: There are provided compounds of the formula (I) wherein Q, R1 and R2 are defined herein. The compounds have activity as anticancer agents.
    Type: Application
    Filed: June 6, 2013
    Publication date: December 12, 2013
    Inventors: Nancy-Ellen Haynes, Johannes Hermann, Kyungjin Kim, Nathan Robert Scott, Lin Yi, Mark Zak
  • 2-[(2-substituted)-indolizin-3-yl]-2-oxo-acetamide derivatives as antifungal agents
    Patent number: 8604029
    Abstract: The invention provides compounds of formula (I), and pharmaceutically acceptable salts thereof wherein: R1, R2, R3, R4, R5, R6, R7, X and X1 are as defined herein. These compounds are useful in the manufacture of medicaments for use in the prevention or treatment of a fungal disease. Compounds of formula (I), and agriculturally acceptable salts thereof, may also be used as agricultural fungicides.
    Type: Grant
    Filed: November 21, 2007
    Date of Patent: December 10, 2013
    Assignee: F2G Ltd British Body Corporate
    Inventors: Robert Downham, Graham Edward Morris Sibley, Lloyd James Payne, Philip Edwards, Gareth Morse Davies
  • HETEROCYCLIC PYRIMIDINE CARBONIC ACID DERIVATIVES WHICH ARE USEFUL IN THE TREATMENT, AMELIORATION OR PREVENTION OF A VIRAL DISEASE
    Publication number: 20130317021
    Abstract: The present invention relates to a compound having the general formula (C), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameliorating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.
    Type: Application
    Filed: May 23, 2013
    Publication date: November 28, 2013
    Inventors: Andrea WOLKERSTORFER, Oliver Szolar, Norbert Handler, Stephen Cusack, Thibault Sauvaitre, Céline Simon, Christophe Morice, Bruno Giethlen, Thierry Langer, Mark Smith, Sung-Sau So, Dirk Classen-Houben, Helmut Buschmann
  • TRANSDERMAL PATCH
    Publication number: 20130315977
    Abstract: The present invention relates to an external preparation for transdermal administration, which remarkably enhances the skin permeability of 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine (compound A). The adhesive preparation of the present invention has an adhesive layer formed on one surface of a support, and the adhesive layer contains (i) compound A or a physiologically acceptable acid addition salt thereof, (ii) an adhesive, (iii) lactic acid, and (iv) an additive containing a particular permeation enhancer, whereby remarkably superior skin permeability is provided.
    Type: Application
    Filed: February 1, 2012
    Publication date: November 28, 2013
    Inventors: Hiroo Maeda, Kazumitsu Yamamoto, Masayasu Tanaka
  • 7-OXO-THIAZOLOPYRIDINE CARBONIC ACID DERIVATIVES AND THEIR USE IN THE TREATMENT, AMELIORATION OR PREVENTION OF A VIRAL DISEASE
    Publication number: 20130317022
    Abstract: The present invention relates to a compound having the general formula (A), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.
    Type: Application
    Filed: May 23, 2013
    Publication date: November 28, 2013
    Applicants: European Molecular Biology Laboratory, F. Hoffmann-La Roche AG
    Inventors: Andrea WOLKERSTORFER, Oliver SZOLAR, Norbert HANDLER, Stephen CUSACK, Thibault SAUVAITRE, Céline SIMON, Christophe MORICE, Bruno GIETHLEN, Thierry LANGER, Mark SMITH, Sung-Sau SO, Dirk CLASSEN-HOUBEN, Helmut BUSCHMANN
  • Anellated pyridine compounds
    Patent number: 8586579
    Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein X, Y, A, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as therapeutics.
    Type: Grant
    Filed: June 16, 2011
    Date of Patent: November 19, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Luca Gobbi, Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
  • COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR
    Publication number: 20130303534
    Abstract: Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
    Type: Application
    Filed: March 5, 2013
    Publication date: November 14, 2013
    Inventors: PRABHA N. IBRAHIM, DEAN R. ARTIS, RYAN BREMER, GASTON HABETS, SHUMEYE MAMO, MARIKA NESPI, CHAO ZHANG, JIAZHONG ZHANG, YONG-LIANG ZHU, REBECCA ZUCKERMAN, BRIAN WEST, YOSHISA SUZUKI, JIANMING TSAI, KLAUS-PETER HIRTH, GIDEON BOLLAG, WAYNE SPEVAK, HANNA CHO, SAMUEL J. GILLETTE, GUOXIAN WU, HONGYAO ZHU, SHENGHUA SHI
  • 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
  • Inhibitor compounds and cancer treatment methods
    Patent number: 8580792
    Abstract: A synergistically effective combination of an anti-cancer agent and a therapeutic compound, such as an mTOR-Rictor complex inhibitor, a Serine 473 phosphorylation inhibitor, an AKT2 inhibitor, or a combination thereof, for use in the treatment of cancer, and methods and uses thereof. Also included are methods and uses of a thiosemicarbazone for treating a cancer in a mammal in need thereof characterized by over-expression of RAS, by an EGFR mutation, and/or by over-expression of AKT2.
    Type: Grant
    Filed: February 1, 2012
    Date of Patent: November 12, 2013
    Assignee: Critical Outcome Technologies Inc.
    Inventor: Wayne R. Danter
  • 1H-PYRAZOLO[3,4-B]PYRIDINES AND THERAPEUTIC USES THEREOF
    Publication number: 20130296307
    Abstract: Provided herein are compounds according to Formula I and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancers such as colon, ovarian, pancreatic, breast, liver, prostate and hematologic cancers:
    Type: Application
    Filed: July 10, 2013
    Publication date: November 7, 2013
    Inventors: John Hood, Sunil Kumar KC, David Mark Wallace