Polycyclo Ring System Having The Additional Hetero Ring As One Of The Cyclos Patents (Class 514/232.5)
  • Patent number: 10316033
    Abstract: Provided is a process of synthesizing a substituted pyridine and pyrimidine compound. Particularly, provided is a method for preparing a compound of formula III via a compound of formula II?, wherein the definition of each of groups is as described as the description. Compound with other methods, the method in the present invention has features of high yield and a result product being easier to separate.
    Type: Grant
    Filed: March 24, 2016
    Date of Patent: June 11, 2019
    Assignees: Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shandong Luoxin Pharmaceutical Group Stock Co., Ltd.
    Inventors: Jingkang Shen, Tao Meng, Ting Yu, Lanping Ma, Xin Wang, Lin Chen
  • Patent number: 9717736
    Abstract: There is provided a compound of formula I: or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.
    Type: Grant
    Filed: June 8, 2015
    Date of Patent: August 1, 2017
    Assignee: Kudos Pharmaceuticals Limited
    Inventors: Heather Mary Ellen Duggan, Frederic Georges Marie Leroux, Karine Fabienne Malagu, Niall Morrison Barr Martin, Keith Menear, Graeme Cameron Murray Smith
  • Patent number: 9585892
    Abstract: Solid forms comprising N-(5-tert-butyl-isoxazol-3-yl)-N?-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea, compositions comprising the solid forms, methods of making the solid forms and methods of their use for the treatment of various diseases and/or disorders are disclosed.
    Type: Grant
    Filed: October 7, 2014
    Date of Patent: March 7, 2017
    Assignee: Ambit Biosciences
    Inventors: Shripad S. Bhagwat, Wei Lai, Stephan D. Parent, Melanie J. Bevill, Alan Schwartz, Valeriya N. Smolenskaya
  • Patent number: 9499495
    Abstract: The present application provides novel quinazolines and azaquinazolines and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in for co-regulating RAS/RAF/MEK/ERK and PI3K/AKT/PTEN/mTOR pathways by administering a therapeutically effective amount of one or more of the compounds of formula (I), wherein X, Y, T and R4, and R6 to R8? are defined herein, to a patient. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the RAS/RAF/MEK/ERK and PI3K/AKT/PTEN/mTOR pathways. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment/the disease is cancer.
    Type: Grant
    Filed: April 11, 2014
    Date of Patent: November 22, 2016
    Assignee: Asana Biosciences, LLC
    Inventors: Scott K. Thompson, Roger A. Smith, Sanjeeva Reddy, Tyler M. John, Vijay Kumar Nyavanandi, Hosahalli Subramanya, Vijay Potluri, Sunil Kumar Panigrahi, Prabhakara Rao Nadipalli, Saumitra Sengupta
  • Patent number: 9434745
    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: Grant
    Filed: May 23, 2013
    Date of Patent: September 6, 2016
    Assignees: Savira pharmaceuticals GmbH, F. Hoffmann-La Roche AG, European Molecular Biology Laboratory
    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
  • Patent number: 9340536
    Abstract: Provided are a multicomponent crystalline system (co-crystal), use thereof, as well as a process for obtaining the same. The said multicomponent crystalline system (co-crystal) comprises Dasatinib and a second compound selected from methyM-hydrobenzoate, nicotinamide, ethyl gallate, methyl gallate, propyl gallate, ethyl maltol, vanillin, menthol, or (1R,2S,5R)-(?)-menthol.
    Type: Grant
    Filed: June 13, 2013
    Date of Patent: May 17, 2016
    Assignee: BASF SE
    Inventors: Tiziana Chiodo, Andreas Hafner, Tobias Hintermann, Beate Salvador, Martin Szelagiewicz, Fritz Blatter, Bernd Siebenhaar, Marcus Vossen
  • Patent number: 9334271
    Abstract: The invention relates to PI3K inhibitors of the formula (I)• in which all of the variables are as defined in the specification, to their preparation, to their medical use, in particular to their use in the treatment of cancer and neurodegenerative disorders, and to medicaments comprising them.
    Type: Grant
    Filed: October 26, 2012
    Date of Patent: May 10, 2016
    Assignee: Novarits AG
    Inventors: Emmanuelle Briard, Pascal Furet, Andreas Lerchner, Peter Meier, Branko Radetich, David Andrew Sandham, Yanyi Zhu
  • Patent number: 9289475
    Abstract: This invention relates, e.g., to a method for treating a subject having a chronic inflammatory respiratory disorder, comprising administering to the subject an effective amount of an inhibitor of the expression of and/or the activity of VEGF-A and/or VEGFR1 and/or VEGFR2 and/or NP1, or a combination thereof. Also described are screening assays for agents for treating a subject having a chronic inflammatory respiratory disorder, and kits for performing one of the methods of the invention.
    Type: Grant
    Filed: November 6, 2009
    Date of Patent: March 22, 2016
    Assignee: The Johns Hopkins University
    Inventor: Jean Kim
  • Patent number: 9260531
    Abstract: The present invention relates to antibodies, or antigen-binding fragments thereof, that bind to the extracellular domain of human c-Met, compositions and kits comprising such c-Met antibodies, or antigen-binding fragments thereof, and methods of using the same for detection of human c-Met that aid in identifying patients with tumors expressing or overexpressing human Met and/or improving their treatment response with anti-c-Met therapeutics.
    Type: Grant
    Filed: May 1, 2013
    Date of Patent: February 16, 2016
    Assignee: Eli Lilly and Company
    Inventors: Gregory Beuerlein, Julian Davies, Irene Jennifer Denning, Ling Liu, Jirong Lu, Peter Edward Vaillancourt
  • Patent number: 9192162
    Abstract: The use of polyhexamethylene guanidine hydrochloride as preservative for preventing and controlling citrus sour rot and its application are disclosed by the present invention. The citrus preservative calculated by 100% total mass fraction comprises 0.05%-0.5% polyhexamethylene guanidine hydrochloride, 0.05%-0.2% of one or more selected from the group consisting of a mixture of several of the following: 0.05%-0.2% imidazole fungicidebactericide, benzimidazole fungicidebactericide, pyrimethanil, fludioxonil and azoxystrobin, and 0.02%-0.15% polyethenoxy ether emulsion or quaternary ammonium salt emulsion, and the rest is water. The citrus preservative can significantly inhibit the decay of citrus fruit such as Citrus microcarpa during storage, especially the incidence of sour rot. So the commercial value of citrus is obviously increased.
    Type: Grant
    Filed: November 15, 2010
    Date of Patent: November 24, 2015
    Assignee: SOUTH CHINA BOTANICAL GARDEN, CHINESE ACADEMY OF SCIENCES
    Inventors: Xuewu Duan, Yueming Jiang, Linyan Feng, Fuwang Wu
  • Patent number: 9187491
    Abstract: Gambogenic acid derivatives having a structure shown as Formula (I) or (II), salts, preparation method and application thereof in the treatment of tumor. Compared with gambogenic acid, the gambogenic acid derivatives exhibit more potent anti-tumor activities.
    Type: Grant
    Filed: September 28, 2012
    Date of Patent: November 17, 2015
    Assignee: Ninth People's Hospital, School Medicine Shanghai Jiao Tong University
    Inventors: Wantao Chen, Xu Wang, Zhiyuan Zhang, Chenping Zhang, Li Mao, Ping Zhang, Qin Xu, Ming Yan, Jianjun Zhang, Jinsong Pan, Yan Lv, Rongxin Deng, Weiliu Qiu
  • Patent number: 9145419
    Abstract: Disclosed are imidazopyridazinyl compounds of Formula (I): (I), or pharmaceutically salts and prodrugs thereof, wherein R3 is C2-4alkenyl or a cyclic group, and R1 and R2 are defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.
    Type: Grant
    Filed: April 27, 2011
    Date of Patent: September 29, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Upender Velaparthi, Peiying Liu, James Aaron Balog
  • Patent number: 9132102
    Abstract: Stilbene analogs and pharmaceutical compositions that are useful for the treatment of various cancers, including without limitation, colorectal cancer (CRC) and breast cancer are disclosed. The halogenated stilbene analogs include nitrogen heteroaryl groups and/or amino groups on the stilbene ring.
    Type: Grant
    Filed: February 27, 2014
    Date of Patent: September 15, 2015
    Assignee: UNIVERSITY OF KENTUCKY RESEARCH FOUNDATION
    Inventors: David Watt, Chunming Liu, Vitaliy M. Sviripa, Wen Zhang
  • Patent number: 9102670
    Abstract: There is provided a compound of formula I: or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.
    Type: Grant
    Filed: April 9, 2013
    Date of Patent: August 11, 2015
    Assignee: KUDOS PHARMACEUTICALS LIMITED
    Inventors: Heather Mary Ellen Duggan, Frederic Georges Marie Leroux, Karine Fabienne Malagu, Niall Morrison Barr Martin, Keith Menear, Graeme Cameron Murray Smith
  • Publication number: 20150148328
    Abstract: The invention relates to the novel products of formula (I) with p, q=0, 1 or 2; R1=phenyl, pyridyl; —(CH2)m—Ra; alkylene; cycloalkyl; heterocycloalkyl; alkyl; —SO2 —Rb; —CO—Re; m=1 or 2; Ra=aryl, heteroaryl, —CO-cycloalkyl, —CO-heterocycloalkyl, —CO—Rb, —C(Rb)?N—ORc, —CO 2 Rd, —CONRxRy; Rb=alkyl, aryl, heteroaryl; Rc=H, alkyl; Rd=alkyl, cycloalkyl; Re=alkyl, cycloalkyl, aryl, heteroaryl; NRxRy with Rx,Ry=H, alkyl, cycloalkyl, alkoxy, phenyl, or form with N a ring with optionally O, N; R2, R3=H, alkyl, CF 3, or form with C a ring with optionally O, S and N; R4=H, F, Cl, CH3 or CN; the morpholine is substituted with Me, and optionally substituted with F, OH; or is (Formula 1a) and the isomer of configuration R,R (Formula 1b) these products being in all the isomer forms and the salts, as medicaments, in particular as anticancer medicaments.
    Type: Application
    Filed: June 21, 2013
    Publication date: May 28, 2015
    Inventors: Youssef El-Ahmad, Bruno Filoche-Romme, Jean-Philippe Letallec, Gilbert Marciniak, Baptiste Ronan, Bertrand Vivet, Maurice Brollo
  • Patent number: 9040021
    Abstract: Heterocyclic compounds of formula (I) useful as imaging probes of Tau pathology in Alzheimer's disease are described. Compositions and methods of making such compounds are also described.
    Type: Grant
    Filed: November 7, 2011
    Date of Patent: May 26, 2015
    Assignee: GE Healthcare Limited
    Inventors: Clare Jones, Amanda Ewan, Duncan Wynn, Alessandra Gaeta, James Nairne
  • Patent number: 9035047
    Abstract: Compounds which inhibit the activity of anti-apoptotic Mcl-1 protein, compositions containing the compounds, and methods of treating diseases involving overexpressed or unregulated Mcl-1 protein are disclosed.
    Type: Grant
    Filed: April 23, 2013
    Date of Patent: May 19, 2015
    Assignee: AbbVie Inc.
    Inventors: Xilu Wang, Xiaohong Song, Steven W. Elmore, Milan Bruncko, David J. Madar, Andrew J. Souers, Lisa A. Hasvold, Le Wang, Zhi-Fu Tao, Aaron R. Kunzer
  • Publication number: 20150126505
    Abstract: Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.
    Type: Application
    Filed: October 31, 2014
    Publication date: May 7, 2015
    Inventors: Shripad Bhagwat, Qi Chao, Robert M. Grotzfeld, Hitesh K. Patel, Kelly G. Sprankle
  • Publication number: 20150105370
    Abstract: Embodiments of the disclosure relate to selectively substituted quinoline compounds that act as antagonists or inhibitors for Toll-like receptors 7 and/or 8, and their use in pharmaceutical compositions effective for treatment of systemic lupus erythematosus (SLE) and lupus nephritis.
    Type: Application
    Filed: October 14, 2014
    Publication date: April 16, 2015
    Inventors: ERIC CARLSON, HANS HANSEN, LYNN HAWKINS, SALLY ISHIZAKA, MATTHEW MACKEY, SHAWN SCHILLER, CHIKAKO OGAWA, HEATHER DAVIS
  • Publication number: 20150099735
    Abstract: The invention is concerned with triazolopyridine compounds of formula (I) wherein R1, R2 and R3 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used as medicaments.
    Type: Application
    Filed: December 16, 2014
    Publication date: April 9, 2015
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Alexander Flohr, Katrin Groebke Zbinden, Matthias Koerner
  • Patent number: 8987257
    Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, to their preparation, to their medical use, in particular to their use in the treatment of cancer and neurodegenerative disorders, and to medicaments comprising them.
    Type: Grant
    Filed: January 30, 2012
    Date of Patent: March 24, 2015
    Assignee: Novartis AG
    Inventors: Branko Radetich, Bing Yu, Yanyi Zhu
  • Publication number: 20150051202
    Abstract: Compounds of the formula I in which R1, R2 and R4 have the meanings indicated in Claim 1, are inhibitors of GCN2, and can be employed, inter alia, for the treatment of cancer.
    Type: Application
    Filed: February 14, 2013
    Publication date: February 19, 2015
    Applicant: Merck Patent GmbH
    Inventors: Kai Schiemann, Carl Deutsch, Guenter Hoelzemann, Daniel Kuhn, Ansgar Wegener, Dominique Swinnen, Horacio Comas
  • Publication number: 20150051203
    Abstract: A compound of structural formula (I) or (II): as HSP90 inhibitors that possess significantly improved bioavailability over comparative compounds, which are suitable for the treatment of hyperproliferative diseases such as cancer, infections, immune disorders, inflammation, and CNS related disorders.
    Type: Application
    Filed: March 27, 2013
    Publication date: February 19, 2015
    Inventors: Dinesh Chimmanamada, Zachary Demko, Weiwen Ying
  • Patent number: 8957071
    Abstract: The disclosure provides methods and compositions for treating a vascular, autoimmune, and/or inflammatory disease, or a condition associated therewith, with a dose of an inosine monophosphate dehydrogenase (IMPDH) inhibitor effective to treat the vascular, autoimmune and/or inflammatory disease, or associated condition but that does not produce immunosuppression sufficient to reduce the risk of allograft rejection. These lower doses of the immunosuppressant avoid the adverse consequences of severe immunosuppression while providing effective treatment of the vascular, autoimmune and/or inflammatory disease.
    Type: Grant
    Filed: May 5, 2008
    Date of Patent: February 17, 2015
    Assignees: Aspreva Pharmaceuticals S.A., Aspreva Pharmaceuticals Corp.
    Inventors: Richard Glickman, Michael R. Hayden, Noel Hall
  • Publication number: 20150038486
    Abstract: Provided herein are pyrimidinyl and 1,3,5-triazinyl benzimidazole sulfonamides, e.g., compounds of Formulae IA, IB, and IC, and their pharmaceutical compositions, preparation, and use as agents or drugs for cancer therapy, either alone or in combination with radiation and/or other anticancer drugs.
    Type: Application
    Filed: July 7, 2014
    Publication date: February 5, 2015
    Inventors: Gordon William Rewcastle, Swarnalatha Akuratiya Gamage, Jack Urquhart Flanagan, Anna Claire Giddens, Kit Yee Tsang
  • Publication number: 20150031669
    Abstract: The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Application
    Filed: October 26, 2012
    Publication date: January 29, 2015
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventors: Steven John Woodhead, Christopher William Murray, Valerio Berdini, Gordon Saxty, Gilbert Ebai Besong, Lieven Meerpoel, Olivier Alexis Georges Querolle, Virginie Sophie Poncelet
  • Patent number: 8940736
    Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazotriazines inhibit protein kinase activity thereby making them useful as anticancer agents.
    Type: Grant
    Filed: July 12, 2013
    Date of Patent: January 27, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ashok Vinayak Purandare, Brian E. Fink, Ashvinikumar V. Gavai, Walter Lewis Johnson, Amy C. Hart, Liqi He, Tram N. Huynh, Jennifer Inghrim, Harold Mastalerz, Xiaopeng Sang, Christine M. Tarby, Honghe Wan, Wayne Vaccaro, Guifen Zhang, Yufen Zhao, Kurt Zimmermann
  • Patent number: 8940724
    Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjogren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphob
    Type: Grant
    Filed: June 25, 2010
    Date of Patent: January 27, 2015
    Assignee: Amgen Inc.
    Inventors: Timothy D. Cushing, Paul John Dransfield, Felix Gonzalez Lopez de Turiso, Michael G. Johnson, Todd Kohn, Vatee Pattaropong, Jillian L. Simard
  • Publication number: 20150025058
    Abstract: Compounds of the formula I in which R1, R2 and R4 have the meanings indicated in Claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment of cancer, rheumatoid arthritis and/or systemic lupus
    Type: Application
    Filed: January 22, 2013
    Publication date: January 22, 2015
    Applicant: MERCK PATENT GMBH
    Inventors: Carl Deutsch, Daniel Kuhn, Tatjana Ross, Lars Burgdorf
  • Publication number: 20140349918
    Abstract: The present invention relates to xanthone analogs. Such compounds may be used in the treatment of bacterial infections.
    Type: Application
    Filed: September 10, 2012
    Publication date: November 27, 2014
    Applicants: Singapore Health Services Pte Ltd., Agency for Science, Technology and Research
    Inventors: Hanxun Zou, Lakshminiarayan Rajanmani, Lei Zhou, Chang Chui Charles Tang, Jun Jie Koh, Tiang Hwee Donald Tan, Chandra Verma, Roger W. Beuerman, Shouping Liu, Saraswathi Padmanabhan
  • Publication number: 20140343050
    Abstract: Provided are carboxylic ester derivatives of formula (I), methods of preparing them, and methods for using them. These compounds are prodrugs of D-isoglutamyl-[D/L]-tryptophan. The in vitro bioconversion of some of the prodrugs to the parent drug D-isoglutamyl-D-tryptophan (or thymodepressin) was tested in human hepatocytes and in human blood. In vivo pharmacokinetic studies following oral administration of some of the prodrugs to rats are also reported.
    Type: Application
    Filed: March 30, 2012
    Publication date: November 20, 2014
    Applicant: APTOEX TECHNOLOGIES, INC.
    Inventors: Tim Fat Tam, Regis Leung-Toung, Yingsheng Wang, Yanqing Zhao, Tao Xin, Wanren Li, Jolanta Maria Wodzinska, Vrajlal S. Rabadia, Christopher John Feeney
  • Publication number: 20140341851
    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: Application
    Filed: April 4, 2014
    Publication date: November 20, 2014
    Applicant: ENANTA PHARMACEUTICALS, INC.
    Inventors: YAO-LING QIU, Ce Wang, Xiaowen Peng, Hui Cao, Lu Ying, Xuri Gao, Bin Wang, Yat Sun Or
  • Publication number: 20140336166
    Abstract: The invention relates to PI3K inhibitors of the formula (I) • in which all of the variables are as defined in the specification, to their preparation, to their medical use, in particular to their use in the treatment of cancer and neurodegenerative disorders, and to medicaments comprising them.
    Type: Application
    Filed: October 26, 2012
    Publication date: November 13, 2014
    Applicant: NOVARTIS AG
    Inventors: Emmanuelle Briard, Pascal Furet, Andreas Lerchner, Peter Meier, Branko Radetich, David Andrew Sandham, Yanyi Zhu
  • Publication number: 20140336169
    Abstract: Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
    Type: Application
    Filed: May 9, 2014
    Publication date: November 13, 2014
    Applicant: GILEAD CONNECTICUT, INC.
    Inventors: Scott A. MITCHELL, Kevin S. CURRIE, Peter A. BLOMGREN, Jeffrey E. KROPF, Seung H. LEE, Jianjun XU, Douglas G. STAFFORD, James P. HARDING, Antonio J. M. BARBOSA, JR., Zhongdong ZHAO, David M. ARMISTEAD, Soumya MITRA
  • Publication number: 20140323470
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: wherein R2, W, A, Y and R1 are as defined in the specification, are p38 MAPK inhibitors, and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.
    Type: Application
    Filed: July 14, 2014
    Publication date: October 30, 2014
    Applicant: CHIESI FARMACEUTICI S.p.A.
    Inventors: Monique Bodil VAN NIEL, Nicholas Charles Ray, Lilian Alcaraz, Terry Aaron Panchal, Andrew Stephen Robert Jennings, Elisabetta Armani, Andrew Peter Cridland, Christopher Hurley
  • Publication number: 20140309216
    Abstract: Compounds of Formulae Ia, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia 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, 2014
    Publication date: October 16, 2014
    Inventors: Adrian Folkes, Stephen Shuttleworth, Irina Chuckowree, Sally Oxenford, Nan Chi Wan, Georgette Castanedo, Richard Goldsmith, Janet Gunzer-Toste, Tim Heffron, Simon Mathieu, Alan Olivero, Daniel P. Sutherlin, Bing-Yan Zhu
  • Publication number: 20140303141
    Abstract: The invention is concerned with triazolopyridine compounds of formula (I) wherein R1, R2 and R3 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used as medicaments.
    Type: Application
    Filed: March 18, 2014
    Publication date: October 9, 2014
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Alexander Flohr, Katrin Groebke Zbinden, Matthias Koerner
  • Publication number: 20140275063
    Abstract: Compounds of formula (I) are inhibitors of Semicarbazide-sensitive amine oxidase R1—X—R2??(I) wherein R1, X and R2 are as defined in the claims.
    Type: Application
    Filed: September 13, 2012
    Publication date: September 18, 2014
    Applicant: PROXIMAGEN LIMITED
    Inventors: Allison Carley, Iain Simpson
  • Publication number: 20140275024
    Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. 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: March 12, 2014
    Publication date: September 18, 2014
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: John Patrick Maxwell, Paul S. Charifson, Qing Tang, Steven M. Ronkin, Katrina Lee Jackson, Albert Charles Pierce, David J. Lauffer, Pan Li, Simon Giroux
  • Publication number: 20140275062
    Abstract: The invention relates to novel compounds which are naphthalene diimides of general formula (I): The compounds are used in therapy, particularly in cancer treatment.
    Type: Application
    Filed: March 13, 2013
    Publication date: September 18, 2014
    Inventors: Stephen NEIDLE, Stephan A. OHNMACHT, Mekala GUNARATNAM, Aaron Grainger DALE, Marialuisa MICCO, Gavin William COLLIE
  • Publication number: 20140256713
    Abstract: The present invention features compounds that are HIV integrase inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.
    Type: Application
    Filed: February 21, 2014
    Publication date: September 11, 2014
    Applicants: Shionogi & Co., Ltd., ViiV Healthcare Company
    Inventors: Brian Alvin JOHNS, Eric Eugene BOROS, Takashi KAWASUJI, Cecilia S. KOBLE, Noriyuki KUROSE, Hitoshi MURAI, Ronald George SHERRILL, Jason Gordon WEATHERHEAD
  • Publication number: 20140256706
    Abstract: Inhibitors of BET bromodomains and compositions containing the same are disclosed. Methods of using the BET bromodomain inhibitors in the treatment of diseases and conditions wherein inhibition of BET bromodomain provides a benefit, like cancers, also are disclosed.
    Type: Application
    Filed: March 11, 2014
    Publication date: September 11, 2014
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Shaomeng Wang, Xu Ran, Yujun Zhao, Chao-Yie Yang, Liu Liu, Longchuan Bai, Donna McEachern, Jeanne Stuckey, Jennifer Lynn Meagher, Duxin Sun, Xiaoqin Li, Bing Zhou, Hacer Karatas, Ruijuan Luo, Arul Chinnaiyan, Irfan A. Asangani
  • Publication number: 20140249144
    Abstract: Disclosed is a compound which has a low molecular weight and has an activity of enhancing the production of EPO and/or an activity of enhancing the production of hemoglobin.
    Type: Application
    Filed: May 12, 2014
    Publication date: September 4, 2014
    Applicant: KOWA COMPANY, LTD.
    Inventors: Masanori Ashikawa, Junya Tagashira, Akiyasu Koketsu, Toshiharu Morimoto, Takahiro Kitamura, Syunji Takemura, Gen Watanabe, Tatsuaki Nishiyama, Satoshi Goda, Masaki Yamabi, Takeshi Doi, Hiroyuki Ishiwata
  • Publication number: 20140243324
    Abstract: The present invention relates to uses of small molecule mimetics of hematopoietic growth factors. In particular the present invention relates to uses of small molecule mimetics of erythropoietin.
    Type: Application
    Filed: November 17, 2011
    Publication date: August 28, 2014
    Applicant: LIGAND PHARMACEUTICALS INCORPORATED
    Inventors: Reid P. Bissonnette, Andrew R. Hudson, Keith B. Marschke, Deepa Rungta, Lin Zhi
  • Patent number: 8791090
    Abstract: Disclosed is a compound which has a low molecular weight and has an activity of enhancing the production of EPO and/or an activity of enhancing the production of hemoglobin.
    Type: Grant
    Filed: March 31, 2010
    Date of Patent: July 29, 2014
    Assignee: Kowa Company, Ltd.
    Inventors: Masanori Ashikawa, Junya Tagashira, Akiyasu Koketsu, Toshiharu Morimoto, Takahiro Kitamura, Syunji Takemura, Gen Watanabe, Tatsuaki Nishiyama, Satoshi Goda, Masaki Yamabi, Takeshi Doi, Hiroyuki Ishiwata
  • Publication number: 20140187545
    Abstract: PI3K? selective compounds having the structure
    Type: Application
    Filed: June 29, 2012
    Publication date: July 3, 2014
    Applicant: GlaxoSmithKline LLC
    Inventors: Hong Lin, Juan Luengo, Michael Lee Moore, Junya Qu, Ralph A. Rivero, Rosanna Tedesco, Hongyi Yu
  • Patent number: 8765731
    Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein A, B, B?, X, Y, R1, R1?, R2, R2?, R3, R3?, R5, R5?, R6, m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.
    Type: Grant
    Filed: November 16, 2012
    Date of Patent: July 1, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: James A. Henderson, John Maxwell, Louis Vaillancourt, Mark Morris, Ronald Grey, Jr., Simon Giroux, Laval Chan Chun Kong, Sanjoy Kumar Das, Bingan Liu, Carl Poisson, Caroline Cadilhac, Monica Bubenik, T. Jagadeeswar Reddy, Guy Falardeau, Constantin Yannopoulos, Jian Wang, Oswy Z. Pereira, Youssef L. Bennani, Albert C. Pierce, Govinda Rao Bhisetti, Kevin M. Cottrell, Valerie Marone
  • Publication number: 20140161731
    Abstract: Described are a compound of formula (II) or (III): The compounds are effective in the treatment of disease, including a tauopathy condition or a disease of tau protein aggregation.
    Type: Application
    Filed: February 14, 2014
    Publication date: June 12, 2014
    Applicant: WisTa Laboratories Ltd.
    Inventors: Scott Clunas, John Mervyn David Storey, Janet Elizabeth Rickard, David Horsley, Charles Robert Harrington, Claude Michel Wischik
  • Publication number: 20140163023
    Abstract: The invention relates to compounds of formula (I) wherein X, R1, R2, T0, o have the meaning as cited in the description and the claims. The compounds of formula I are useful as inhibitors of mTOR for the treatment or prophylaxis of mTOR related diseases and disorders. The invention also relates to pharmaceutical compositions including the compounds of formula I, the preparation of such compounds as well as the use as medicaments.
    Type: Application
    Filed: April 2, 2012
    Publication date: June 12, 2014
    Applicant: Cellzome Limited
    Inventors: Rosemary Lynch, Andrew David Cansfield, Daniel Paul Hardy, Jane Elizabeth Scanlon, Rita Joana Rodrigues Adrego
  • Publication number: 20140154232
    Abstract: The first aspect of the invention relates to a phosphoinositide 3-kinase inhibitor for use in the treatment or prevention of a disease or condition associated with the expression of peroxisome proliferator-activated receptor gamma coactivator 1-? (Pgd1?) and/or uncoupling protein 1 (Thermogenin/Ucp1) in brown adipocytes. The disease or condition may be positive energy imbalance-associated, for example, obesity, an obesity-associated disease or condition, steatosis and biological aging (performance aging). Another aspect of the invention provides the use of a phosphoinositide 3-kinase inhibitor for promoting weight loss in an individual.
    Type: Application
    Filed: June 1, 2011
    Publication date: June 5, 2014
    Applicant: Centro Nacional De Investigaciones Oncologicas (CNIO)
    Inventors: Manuel Serrano Marugan, Joaquin Pastor Fernández, Sonia Martínez González, Ana Ortega Molina, James R. Bischoff, Julen Oyarzabal Santamarina