The Additional Hetero Ring Is Five-membered Consisting Of Carbon And Plural Nitrogens As The Only Ring Members Patents (Class 514/266.23)
  • Patent number: 11014906
    Abstract: Disclosed herein are quinoline-based compounds and method for inhibiting CDK8 or CDK19 for the intervention in diseases, disorders, and conditions. The quinoline-based composition comprise substituents at quinoline ring positions 4 and 6, wherein the substituent at position 4 is selected from a substituted or unsubstituted arylalkylamine or a substituted or unsubstituted arylhetrocyclylamine. Pharmaceutical compositions comprising the substituted quinoline compositions, methods of inhibiting CDK8 or CDK19, and methods of treating CDK8/19-associated diseases, disorders, or conditions are also disclosed.
    Type: Grant
    Filed: August 21, 2019
    Date of Patent: May 25, 2021
    Assignees: University of South Carolina, Senex Biotechnology, Inc.
    Inventors: Igor Roninson, Campbell McInnes, Mengqian Chen, Li Zhang, Jing Li
  • Patent number: 10980804
    Abstract: Methods and compositions for treating cholangiocarcinoma.
    Type: Grant
    Filed: January 17, 2014
    Date of Patent: April 20, 2021
    Assignee: FOUNDATION MEDICINE, INC.
    Inventors: Siraj Mahamed Ali, Matthew J. Hawryluk, Jie He, Doron Lipson, Vincent A. Miller, Jeffrey S. Ross, Philip James Stephens
  • Patent number: 10570123
    Abstract: The present invention relates to inhibitors of ROCK1 and ROCK2 and methods of modulating the pharmacokinetic and/or pharmacodynamic properties of such compounds. Also provided are methods of inhibiting ROCK1 and or ROCK2 that are useful for the treatment of disease.
    Type: Grant
    Filed: July 19, 2018
    Date of Patent: February 25, 2020
    Assignee: SURFACE LOGIX, LLC
    Inventors: Alessandra Bartolozzi, Stewart Campbell, Hope Foudoulakis, Brian Kirk, Siya Ram, Paul Sweetnam, Hemalatha Seshadri
  • Patent number: 10194660
    Abstract: The present invention relates to compounds of Formula (I), or an agronomically acceptable salt of said compounds wherein A1a, A1b, R1, R2, R3 and R4 and R5 are as defined herein. The invention further relates to herbicidal compositions which comprise a compound of Formula (I), and to their use for controlling weeds, in particular in crops of useful plants.
    Type: Grant
    Filed: June 10, 2016
    Date of Patent: February 5, 2019
    Assignee: Syngenta Participations AG
    Inventors: Glynn Mitchell, Nicholas Phillip Mulholland, Yunas Bhonoah
  • Patent number: 9914754
    Abstract: The present invention features a compound having the formula A-X-B, where A is peptide vector capable of enhancing transport of the compound across the blood-brain barrier or into particular cell types, X is a linker, and B is a peptide therapeutic selected from the group consisting of neurotensin, a neurotensin analog, or a neurotensin receptor agonist. The compounds of the invention can be used to treat any disease in which increased neurotensin activity is useful and can be used to induce hypothermia or analgesia.
    Type: Grant
    Filed: December 7, 2009
    Date of Patent: March 13, 2018
    Assignee: Angiochem Inc.
    Inventors: Jean-Paul Castaigne, Michel Demeule, Christian Che, Carine Thiot, Catherine Gagnon
  • Patent number: 9815820
    Abstract: The invention relates to inhibitors of ROCK1 and/or ROCK2. Also provided are methods of treating diseases and disorders involving inhibiting ROCK1 and/or ROCK2.
    Type: Grant
    Filed: October 7, 2013
    Date of Patent: November 14, 2017
    Assignee: Kadmon Corporation, LLC
    Inventors: Masha Poyurovsky, Ji-In Kim, Kevin Liu, Alexandra Zanin-Zhorov
  • Patent number: 9802949
    Abstract: Provided are fused tricyclic compounds effective to inhibit the function of the NS5A protein of formula (I), wherein X, X?, Y, Y?, A, A?, Q1, Q2, R1-R4, X4, R5a, f and W are defined as in the description. Also provided herein are pharmaceutical compositions thereof, and uses in the manufacture of a medicament for treating HCV infection or a HCV disorder thereof.
    Type: Grant
    Filed: November 28, 2013
    Date of Patent: October 31, 2017
    Assignee: SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Yingjun Zhang, Jiancun Zhang, Hongming Xie, Qingyun Ren, Shifeng Li, Changping Fu, Bailin Hu, Xiwei Wu, Changhua Tang
  • Patent number: 9597375
    Abstract: Methods for stopping or slowing bleeding from a wound are provided; these methods include the step of administering a composition comprising a polyphosphate (polyP) to blood from the wound at the site of the wound. Also provided are methods for slowing fibrinolysis and for blocking the action of Tissue Factor Pathway Inhibitor (TFPI) with the use of polyP.
    Type: Grant
    Filed: October 20, 2009
    Date of Patent: March 21, 2017
    Assignee: The Board of Trustees of the University of Illinios
    Inventors: James H. Morrissey, Stephanie A. Smith, Roberto Docampo, Nicola J. Mutch
  • Patent number: 9562052
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, A1, A2, A3, m, n and p are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Grant
    Filed: February 20, 2015
    Date of Patent: February 7, 2017
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bernd Buettelmann, Aurelia Conte, Holger Kuehne, Bernd Kuhn, Werner Neidhart, Ulrike Obst Sander, Hans Richter
  • Patent number: 9440961
    Abstract: The present invention relates to inhibitors of ROCK1 and ROCK2 and methods of modulating the pharmacokinetic and/or pharmacodynamic properties of such compounds. Also provided are methods of inhibiting ROCK1 and or ROCK2 that are useful for the treatment of disease.
    Type: Grant
    Filed: December 23, 2014
    Date of Patent: September 13, 2016
    Assignee: SURFACE LOGIX, INC.
    Inventors: Alessandra Bartolozzi, Stewart Campbell, Hope Foudoulakis, Brian Kirk, Siya Ram, Paul Sweetnam, Hemalatha Seshadri
  • Patent number: 9365550
    Abstract: The present invention relates to compounds of general formula wherein R1 hydrogen, lower alkyl, halogen or lower alkyl substituted by halogen; R2 is hydrogen or halogen; X1 is N or CH; X2 is N or CH; with the proviso that only one of X1 or X2 is N; X3 is C(R) or N; and R is hydrogen, lower alkyl, halogen, lower alkyl substituted by halogen, lower alkoxy or SO2-lower alkyl; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof.
    Type: Grant
    Filed: March 31, 2015
    Date of Patent: June 14, 2016
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Simona M. Ceccarelli, Ravi Jagasia, Roland Jakob-Roetne, Juergen Wichmann
  • Patent number: 9295672
    Abstract: Provided herein is an optically active pyrazolylaminoquinazoline, and pharmaceutical compositions thereof. Also provided herein is a method for treating, preventing, or ameliorating one or more symptoms of a JAK-mediated condition, disorder, or disease. Further provided herein is a method for treating, preventing, or ameliorating one or more symptoms of a proliferative disease, inflammatory disease, or renal disease.
    Type: Grant
    Filed: November 18, 2014
    Date of Patent: March 29, 2016
    Assignee: Ambit Biosciences Corporation
    Inventors: Mark W. Holladay, Eduardo Setti
  • Patent number: 9290460
    Abstract: Disclosed are 1-(arylmethyl)quinazoline-2,4(1H,3H)-diones thereof, represented by the Formula (I) wherein Ar, R1-R6 are defined herein. Compounds having Formula (I) are PARP inhibitors. Therefore, compounds of the invention may be used to treat clinical conditions that are responsive to the inhibition of PARP activity.
    Type: Grant
    Filed: March 31, 2012
    Date of Patent: March 22, 2016
    Assignee: IMPACT THERAPEUTICS, INC.
    Inventors: Sui Xiong Cai, Ye Edward Tian, Xiuhua Hu
  • Patent number: 9096541
    Abstract: Proteases such as memapsin-1 are import enzymes, playing roles in a variety of diseases including diabetes. The inventors have developed inhibitors of memapsin 1 and methods of use therefore in the treatment of disease.
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: August 4, 2015
    Assignees: Oklahoma Medical Research Foundation, Purdue Research Foundation
    Inventors: Jordan Tang, Xiangping Huang, Deborah Downs, Arun K. Ghosh
  • Publication number: 20150141442
    Abstract: Certain chemical entities that modulate PI3 kinase activity, and chemical entities, pharmaceutical compositions, and methods of treatments of diseases and conditions associated with PB kinase activity are described.
    Type: Application
    Filed: September 19, 2014
    Publication date: May 21, 2015
    Inventors: Pingda Ren, Yi Liu, Troy Edward Wilson
  • Publication number: 20150141443
    Abstract: Provided herein is an optically active pyrazolylaminoquinazoline, and pharmaceutical compositions thereof. Also provided herein is a method for treating, preventing, or ameliorating one or more symptoms of a JAK-mediated condition, disorder, or disease. Further provided herein is a method for treating, preventing, or ameliorating one or more symptoms of a proliferative disease, inflammatory disease, or renal disease.
    Type: Application
    Filed: November 18, 2014
    Publication date: May 21, 2015
    Inventors: Mark W. HOLLADAY, Eduardo SETTI
  • Publication number: 20150140104
    Abstract: Described herein are polymeric nanoparticles that include a therapeutic agent which is 2-(3-((7-(3-(ethyl(2-hydroxyethyl)amino)propoxy)quinazolin-4-yl)amino)-1H-pyrazol-5-yl)-N-(3-fluorophenyl)acetamide (also known as AZD1152 hqpa) or a pharmaceutically acceptable salt thereof, and methods of making and using such therapeutic nanoparticles.
    Type: Application
    Filed: September 15, 2014
    Publication date: May 21, 2015
    Applicant: ASTRAZENECA AB
    Inventors: Marianne Bernice ASHFORD, James Martin NOLAN III, Eyoung SHIN, Young-Ho SONG, Greg TROIANO, Hong WANG
  • Patent number: 9023859
    Abstract: A compound in combination with a pharmaceutically acceptable carrier, the compound having a formula: wherein: R1 is a member of the group consisting of hydrogen, halogen, nitro, benzo, lower alkyl, phenyl, and lower alkoxy; R2 is a member of the group consisting of hydroxy, acetoxy, and lower alkoxy; and R3 is a member of the group consisting of hydrogen and lower alkenoxy-carbonyl; and n is either 1 or 2; and pharmaceutically acceptable salts thereof; for use in treatment of or prevention of skeletal muscle fibrosis and/or for inducing skeletal muscle regeneration.
    Type: Grant
    Filed: March 1, 2013
    Date of Patent: May 5, 2015
    Assignees: State of Israel, Ministry of Agriculture, Agricultural Research Organization, Hadasit Medical Research Services and Development Company
    Inventors: Mark Pines, Arnon Nagler
  • Patent number: 9018191
    Abstract: Quinazoline derivatives of formula (I): wherein A is 5-membered heteroaryl containing a nitrogen atom and one or two further nitrogen atoms; compositions containing them, processes for their preparation and their use in therapy.
    Type: Grant
    Filed: August 21, 2012
    Date of Patent: April 28, 2015
    Assignee: AstraZeneca AB
    Inventors: Nicola Murdoch Heron, Andrew Austen Mortlock, Frederic Henri Jung, Georges Rene Pasquet
  • Publication number: 20150110723
    Abstract: The disclosure relates to quinazoline derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to inhibitors of NADPH-oxidases (Nox enzymes) and/or myeloperoxidase.
    Type: Application
    Filed: May 28, 2013
    Publication date: April 23, 2015
    Applicant: EMORY UNIVERSITY
    Inventors: John David Lambeth, Thota Ganesh, Susan M. Smith, Aiming Sun
  • Patent number: 9012445
    Abstract: In one aspect, the invention relates to substituted 4-(1H-pyrazol-4-yl)benzyl analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: January 12, 2013
    Date of Patent: April 21, 2015
    Assignee: Vanderbilt University
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, Michael S. Poslusney, James C. Tarr
  • Publication number: 20150099730
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including those mediated by inhibition of fatty acid synthase (FASN) enzyme, such as, cancer, obesity or related discorders, and liver related disorders. Such compounds are represented by formula (I) as follows: wherein L1, a, b, m, n, R1, R2, R3, R4, and R5 are defined herein.
    Type: Application
    Filed: September 6, 2013
    Publication date: April 9, 2015
    Applicant: Janssen Pharmaceutica, NV
    Inventor: Peter J. Connolly
  • Publication number: 20150087664
    Abstract: Compounds having the formula (I) wherein R1, R2, R3 and Ar as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders.
    Type: Application
    Filed: August 3, 2012
    Publication date: March 26, 2015
    Applicants: GENENTECH, INC., ARRAY BIOPHARMA INC.
    Inventors: James F. Blake, Huifen Chen, Mark Joseph Chicarelli, Jason Demeese, Rustam Ferdinand Garrey, John Gaudino, Lewis Gazzard, Robert J. Kaus, Samuel Kintz, Peter J. Mohr, David A. Moreno, Jacob Schwartz, Christopher S. Siedem, Eli M. Wallace
  • Publication number: 20150087663
    Abstract: The invention relates to the preparation and use of new aminopyrimidine derivatives as drug candidates in free form or in pharmaceutically acceptable salt form and formulations thereof for the modulation of a disorder or disease which is mediated by the activity of the PI3K enzymes. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of disorders or diseases, such as disorders of immunity and inflammation in which PI3K enzymes play a role in leukocyte function, and hyperproliferative disorders associated with PI3K activity, including but not limited to leukemias and solid tumors, in mammals, especially humans.
    Type: Application
    Filed: September 17, 2014
    Publication date: March 26, 2015
    Applicants: SUNSHINE LAKE PHARMA CO., LTD., CALITOR SCIENCES, LLC
    Inventors: Ning Xi, Liang Wang, Zuping Wu, Xuejin Feng, Yanjun Wu
  • Publication number: 20150057218
    Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.
    Type: Application
    Filed: November 3, 2014
    Publication date: February 26, 2015
    Inventors: Min ZHONG, Leping LI
  • Patent number: 8952020
    Abstract: Provided herein is an optically active pyrozolylaminoquinazaline, and pharmaceutical compositions thereof. Also provided herein is a method for treating, preventing, or ameliorating one or more symptoms of a JAK-mediated condition, disorder, or disease. Further provided herein is a method for treating, preventing, or ameliorating one or more symptoms of a proliferative disease, inflammatory disease, or renal disease.
    Type: Grant
    Filed: March 11, 2014
    Date of Patent: February 10, 2015
    Assignee: Ambit Biosciences Corp.
    Inventors: Mark W. Holladay, Eduardo Setti
  • Patent number: 8946121
    Abstract: The present invention relates to new antifungal compositions and their use in the treatment of agricultural products.
    Type: Grant
    Filed: March 1, 2012
    Date of Patent: February 3, 2015
    Assignee: DSM IP Assets B.V.
    Inventors: Jacobus Stark, Angelique De Rijk
  • Patent number: 8940735
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Grant
    Filed: June 20, 2012
    Date of Patent: January 27, 2015
    Assignee: Viamet Pharmaceuticals, Inc.
    Inventors: William J. Hoekstra, Robert J. Schotzinger, Gary D. Gustafson
  • Publication number: 20150025092
    Abstract: Solid forms comprising pyrazolylaminoquinazoline, 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: Application
    Filed: February 27, 2013
    Publication date: January 22, 2015
    Inventor: Timothy David Gross
  • Patent number: 8937078
    Abstract: Quinazolinone compounds of formula (I) are described, which are useful as prolyl hydroxylase inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by prolyl hydroxylase activity. Thus, the compounds may be administered to treat, e.g., anemia, vascular disorders, metabolic disorders, and wound healing.
    Type: Grant
    Filed: February 10, 2010
    Date of Patent: January 20, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Scott D. Bembenek, Frances M. Hocutt, Barry Eastman Leonard, Jr., Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan
  • Publication number: 20150011513
    Abstract: A triazole bridged flavonoid dimer compound library was efficiently constructed via the cycloaddition reaction of a series of flavonoid-containing azides (Az 1-15) and alkynes (Ac 1-17). These triazole bridged flavonoid dimers and their precursor alkyne- and azide-containing flavonoids were screened for their ability to modulate multidrug resistance (MDR) in P-gp-overexpressed cell line (LCC6MDR), MRP1-overexpressed cell line (2008/MRP1) and BCRP-overexpressed cell line (HEK293/R2 and MCF7-MX100). Generally, they displayed very promising MDR reversal activity against P-gp-, MRP1- and BCRP-mediated drug resistance. Moreover, they showed different levels of selectivity for various transporters. Overall, they can be divided into mono-selective, dual-selective and multi-selective modulators for the P-gp, MRP1 and BCRP transporters.
    Type: Application
    Filed: March 1, 2013
    Publication date: January 8, 2015
    Inventors: Larry Ming Cheung Chow, Tak Hang Chan, Kin Fai Chan, Iris Lai King Wong, Man Chun Law
  • Patent number: 8927530
    Abstract: The present invention provides a combination comprising (a) a compound of formula (I) and (b) one or more antineoplastic agents selected from the group consisting of an antimetabolite agent, analkylating or alkylating-like agent, an intercalating agent, a topoisomerase I or II inhibitor, an antimitotic agent, a kinase inhibitor, a proteasome inhibitor and an antibody inhibiting a growth factor or its receptor, wherein active ingredients of the combination are present in each case in free form or in the form of a pharmaceutically acceptable salt or any hydrate or solvate thereof, useful in the treatment of tumors.
    Type: Grant
    Filed: May 21, 2010
    Date of Patent: January 6, 2015
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Barbara Valsasina, Italo Beria, Antonella Ciavolella, Dario Ballinari, Enrico Pesenti, Juergen Moll, Mara Emanuela Casnaghi, Alessandro Luciano Croci
  • Publication number: 20150005278
    Abstract: This invention relates to novel sulfoximine substituted quinazoline derivatives of formula I wherein Ar, R1 and R2 are as defined in the description and claims, and their use as MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) kinase inhibitors, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment or amelioration of MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) mediated disorders.
    Type: Application
    Filed: June 26, 2014
    Publication date: January 1, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Andreas BLUM, Dirk GOTTSCHLING, Armin HECKEL, Joerg P. HEHN, Bernhard SCHMID, Dieter WIEDENMAYER
  • Publication number: 20150005279
    Abstract: The invention provides compounds of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.
    Type: Application
    Filed: June 26, 2014
    Publication date: January 1, 2015
    Applicant: ABBVIE INC.
    Inventors: Dominique Bonafoux, Heather M. Davis, Kristine E. Frank, Michael M. Friedman, J. Martin Herold, Michael Z. Hoemann, Raymond Huntley, Augustine Osuma, George Sheppard, Gagandeep K. Somal, Jennifer Van Camp, Stacy A. Van Epps, Anil Vasudevan, Grier A. Wallace, Lu Wang, Lu Wang, Zhi Wang, Noel S. Wilson, Xiangdong Xu
  • Publication number: 20140378485
    Abstract: Inhibitors of HCV replication of formula (I) including stereochemically isomeric forms, salts, and solvates thereof, wherein R and R? have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.
    Type: Application
    Filed: December 27, 2012
    Publication date: December 25, 2014
    Inventors: Koen Vandyck, Pierre Jean-Marie Bernard Raboisson
  • Patent number: 8916576
    Abstract: The present invention relates to inhibitors of ROCK1 and ROCK2 and methods of modulating the pharmacokinetic and/or pharmacodynamic properties of such compounds. Also provided are methods of inhibiting ROCK1 and or ROCK2 that are useful for the treatment of disease.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: December 23, 2014
    Assignee: Surface Logix, Inc.
    Inventors: Alessandra Bartolozzi, Stewart Campbell, Hope Foudoulakis, Brian Kirk, Siya Ram, Paul Sweetnam, Hemalatha Seshadri
  • Patent number: 8912181
    Abstract: A novel bicyclic compound having an HSP90 inhibitory effect and a carcinostatic effect. A pharmaceutical agent based on the HSP90 inhibitory effect and useful in the prevention and/or treatment of a disease involving HSP90, particularly cancer. The compound has a general formula (I) or is a salt thereof wherein at least one of X1, X2, X3, and X4 represents N or N-oxide and the rest thereof are each independently C—R2; any one or two of Y1, Y2, Y3, and Y4 represent C—R4 and the rest thereof are each independently CH or N; R1 represents an optionally substituted monocyclic or bicyclic unsaturated heterocyclic group having 1 to 4 heteroatoms selected from N, S, and O; R2 represents a hydrogen atom, an optionally substituted alkyl group having 1 to 6 carbon atoms etc.; R3 represents a hydrogen atom, —CO—R5 etc.
    Type: Grant
    Filed: January 6, 2012
    Date of Patent: December 16, 2014
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventors: Makoto Kitade, Satoshi Yamashita, Shuichi Ohkubo
  • Publication number: 20140357626
    Abstract: Inhibitors of HCV replication of formula I, including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R and R? have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.
    Type: Application
    Filed: December 27, 2012
    Publication date: December 4, 2014
    Inventors: Koen Vandyck, Wim Gaston Verschueren, Pierre Jean-Marie Bernard Raboisson
  • Publication number: 20140350003
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Application
    Filed: August 12, 2014
    Publication date: November 27, 2014
    Inventors: William J. Hoekstra, Stephen W. Rafferty, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Michael T. Sullenberger, Gary D. Gustafson
  • 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
  • Patent number: 8865709
    Abstract: Oxazole derivatives are described. The inventive compounds are useful as kinase inhibitors, and may be used in the treatment of cancer, such as prostate cancer, lung cancer, breast cancer, colon cancer, leukemia, CNS cancer, melanoma, ovarian cancer, and renal cancer.
    Type: Grant
    Filed: September 24, 2013
    Date of Patent: October 21, 2014
    Assignee: Neosome Life Sciences, LLC
    Inventors: Laxman S. Desai, Srinivas Chittaboina
  • Patent number: 8865704
    Abstract: The present invention relates to known and 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: Grant
    Filed: October 6, 2010
    Date of Patent: October 21, 2014
    Assignee: Siena Biotech S.p.A.
    Inventors: Maurizio Varrone, Arianna Nencini, Joanna Margaret Quinn, Andrea Caricasole, Annette Cornelia Bakker, Giovanni Gaviraghi, Massimilano Salerno
  • Publication number: 20140309246
    Abstract: This invention is in the fields of cancer therapy. More particularly it concerns compounds which are useful agents for inhibiting cell proliferative disorders, especially those disorders characterized by over activity and/or inappropriate activity of a EGFR, including EGFR-related cancers, and methods for treating these disorders.
    Type: Application
    Filed: March 16, 2012
    Publication date: October 16, 2014
    Applicant: THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA
    Inventors: Mark I. Greene, Hongtao Zhang, Alan Berezov, Zheng Cai
  • Publication number: 20140309215
    Abstract: Aminoquinazolinyl compounds of formula (I) are described, which are useful as prolyl hydroxylase inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by prolyl hydroxylase activity. Thus, the compounds may be administered to treat, e.g., anemia, vascular disorders, metabolic disorders, and wound healing.
    Type: Application
    Filed: June 24, 2014
    Publication date: October 16, 2014
    Inventors: Michael H. RABINOWITZ, Mark D. ROSEN, Kyle T. TARANTINO, Hariharan VENKATESAN
  • Publication number: 20140309184
    Abstract: Embodiments of the present disclosure relate to methods and compositions for treating a subject with ovarian cancer. Some embodiments include treating a subject with a particular combination of chemotherapeutic agents.
    Type: Application
    Filed: July 20, 2012
    Publication date: October 16, 2014
    Applicant: UNIVERSITY OF SOUTH ALABAMA
    Inventors: Rodney P. Rocconi, Lalita Samant
  • Publication number: 20140296268
    Abstract: The present invention is directed to methods and compositions for suppressing lymphangiogenesis, angiogenesis and/or tumor growth. The methods comprise contacting the tumor with a compound that (i) stabilizes a protein kinase in the inactive state and (ii) is not an ATP competitive inhibitor of the protein kinase in the active state.
    Type: Application
    Filed: February 7, 2011
    Publication date: October 2, 2014
    Inventors: Eric A. Murphy, David A. Cheresh, Lee Daniel Arnold
  • Patent number: 8846566
    Abstract: PROBLEM There are provided a composition for controlling plant diseases and a method for controlling plant diseases having excellent control effect for plant diseases. SOLUTION A composition for controlling plant diseases comprising, as active ingredients, a compound represented by formula (1), wherein X1 represents a methyl group, a difluoromethyl group or an ethyl group; X2 represents a methoxy group or a methylamino group; and X3 represents a phenyl group, a 2-methylphenyl group or a 2,5-dimethylphenyl group, and at least one azole compound selected from the group consisting of bromuconazole, cyproconazole, difenoconazole, fenbuconazole, fluquinconazole, hexaconazole, imibenconazole, ipconazole, myclobutanil, prothioconazole, simeconazole, tetraconazole, triticonazole and metconazole.
    Type: Grant
    Filed: November 20, 2009
    Date of Patent: September 30, 2014
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Masanao Takaishi, Masato Soma
  • Publication number: 20140288100
    Abstract: Disclosed are inhibitors of human galactokinase of formula (1) that are useful in treating or preventing a galactokinase mediated disease or disorder, e.g., galactosemia. Also disclosed are a composition comprising a pharmaceutically acceptable carrier and at least one inhibitor of the invention, and a method of treating or preventing such disease or disorder in a mammal.
    Type: Application
    Filed: September 23, 2011
    Publication date: September 25, 2014
    Applicants: University of Utah Research Foundation, The United States of American, as Represented by the Decretary, Department of Health and Human
    Inventors: Matthew B. Boxer, Martin J. Walsh, Li Liu, Cordelle D. Tanega, Min Shen, Kent Lai, Manshu Tang, Douglas S. Auld
  • Patent number: 8841311
    Abstract: The present invention relates to sulphone-substituted quinazoline derivatives of the formula (I), processes for their preparation and their use as a medicament for the treatment of various diseases.
    Type: Grant
    Filed: July 18, 2009
    Date of Patent: September 23, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Bernd Buchmann, Dirk Kosemund, Duy Nguyen, Arne Von Bonin
  • Patent number: 8835458
    Abstract: Provided is a pharmaceutical composition comprising, as an active ingredient, a quinoline or quinazoline derivative of formula (I), a pharmaceutically acceptable salt, an isomer, a hydrate, and a solvate thereof, which is effective in the prevention and treatment of a cancer, inflammation, autoimmune diseases or neurodegenerative disorders which are induced by the overexpression of inhibitor of apoptosis proteins (IAPs).
    Type: Grant
    Filed: August 31, 2011
    Date of Patent: September 16, 2014
    Assignee: Hanmi Science Co., Ltd
    Inventors: In Hwan Bae, Eun Young Byun, Hae Kyoung Ju, Ji Young Song, Seung Hyun Jung, Seung Ah Jun, Ho Seok Kim, Young Hee Jung, Mi Yon Shim, Young Gil Ahn, Maeng Sup Kim