The Additional Hetero Ring Is A 1,3 Diazine (including Hydrogenated) Patents (Class 514/217.06)
  • Patent number: 10975062
    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: Grant
    Filed: April 1, 2019
    Date of Patent: April 13, 2021
    Inventors: Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan
  • Patent number: 10940132
    Abstract: Compounds, pharmaceutically acceptable salts, esters, prodrugs, and pharmaceutical compositions thereof are disclosed that are useful for inhibition of the biological activity of CCL5 on mammalian cells, as well as methods of treatment for diseases involving the increased biological activity of CCL5.
    Type: Grant
    Filed: December 21, 2019
    Date of Patent: March 9, 2021
    Assignee: AFECTA PHARMACEUTICALS, INC.
    Inventor: Bruce Kovacs
  • Patent number: 10695347
    Abstract: The present invention provides a pyrimidine derivative and a use thereof. The pyrimidine derivative is the compound shown in formula I or a pharmaceutically acceptable salt, hydrate, solvate, metabolite or prodrug thereof, wherein, R1, R2, R3, R4 and R5 are, for example, as defined in the specification. The compound can act as an ALK inhibitor, and is for preparing an anti-tumor medicament for suppressing an anaplastic lymphoma kinase.
    Type: Grant
    Filed: November 4, 2016
    Date of Patent: June 30, 2020
    Assignee: HUBEI BIO-PHARMACEUTICAL INDUSTRIAL TECHNOLOGICAL INSTITUTE, INC.
    Inventors: Xuehai Wang, Yong Xu, Xijun Sheng, Xiaolin Zhang, Hangui Xia, Zhongwen Yang, Yang Yue, Lu Huang, Qiang Xiao
  • Patent number: 10435364
    Abstract: A compound of formula (1), (1?), (1?) or (1??) or a pharmaceutically acceptable salt thereof, for use in the treatment of diseases or conditions for which a bromodomain inhibitor is indicated.
    Type: Grant
    Filed: April 15, 2014
    Date of Patent: October 8, 2019
    Assignee: Albert Ludwigs Universität Freiburg
    Inventors: Stefan Guenther, Xavier Lucas, Manfred Jung, Oliver Einsle, Daniel Wohlwend, Stefan Gerhardt
  • Patent number: 10414768
    Abstract: The present invention relates to compounds of Formula (I) or pharmaceutically acceptable enantiomers, salts, solvates or prodrugs thereof. The invention further relates to the use of the compounds of Formula (I) for the treatment of cystic fibrosis. The invention also relates to a process for manufacturing compounds of Formula (I).
    Type: Grant
    Filed: December 4, 2015
    Date of Patent: September 17, 2019
    Assignees: Centre National de la Recherche Scientifique (CNRS), Université Pierre et Marie Curie—Paris 6 (UPMC)
    Inventors: Isabelle Callebaut, Jean-Paul Mornon, Jean-Luc Decout, Frederic Becq, Pierre Lehn, Brice Hoffman, Benjamin Boucherle, Romain Haudecoeur, Antoine Fortune, Clement Boinot, Julien Alliot
  • Patent number: 10329292
    Abstract: The present invention relates to substituted xanthine derivatives, pharmaceutical compositions containing them and their use in therapy, particularly in the treatment of conditions having an association with TRPC5 containing ion channels.
    Type: Grant
    Filed: July 10, 2018
    Date of Patent: June 25, 2019
    Assignees: Boehringer Ingelheim International GmbH, Hydra Biosciences, Inc.
    Inventors: Kai Gerlach, Christian Eickmeier, Achim Sauer, Stefan Just, Bertrand L. Chenard
  • Patent number: 10280297
    Abstract: The present invention provides a particulate water-absorbing agent which has an excellent fluid retention capacity under pressure and an excellent liquid permeability. Each of the following values of the particulate water-absorbing agent of the present invention falls within a certain range: a ratio represented by “centrifuge retention capacity/Ln (water-soluble component amount)”; a molecular weight distribution of the water-soluble component; a weight average molecular weight after a hydrolysis treatment; and a branching density after the hydrolysis treatment.
    Type: Grant
    Filed: March 29, 2016
    Date of Patent: May 7, 2019
    Assignee: NIPPON SHOKUBAI CO., LTD.
    Inventors: Nobuya Tanaka, Kohei Omori, Kazushi Torii
  • Patent number: 10253023
    Abstract: The present invention relates to imidazo pyridine compounds, and pharmaceutically acceptable compositions thereof, useful as BTK inhibitors.
    Type: Grant
    Filed: October 6, 2015
    Date of Patent: April 9, 2019
    Assignee: Merck Patent GmbH
    Inventors: Pascale Gaillard, Jeyaprakashnarayanan Seenisamy, Lesley Liu-Bujalski, Richard D. Caldwell, Justin Potnick, Hui Qiu, Constantin Neagu, Reinaldo Jones, Annie Cho Won, Andreas Goutopoulos, Brian A. Sherer, Theresa L. Johnson, Anna Gardberg
  • Patent number: 10246442
    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: Grant
    Filed: February 17, 2017
    Date of Patent: April 2, 2019
    Assignee: JANSSEN PHARMACEUTICA NV
    Inventors: Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan
  • Patent number: 10117871
    Abstract: Various embodiments described herein are directed to compounds of formula (I), (II), (III) or (IV) for use as potent inhibitors of HIV integrase and for treatment of patients afflicted with AIDS. A major challenge of human immunodeficiency virus (HIV) chemotherapy continues to be the inevitable selection of resistance by the virus towards known drug regimens. Treating resistant HIV strains calls for novel antivirals with unique structural cores. Some embodiments are directed to compounds featuring a 3-hydroxypyrimidine-2,4-dione-5-carboxamide core that consistently confers low nanomolar potencies against HIV-1 in cell culture. Biochemical testing and molecular modeling results corroborate an antiviral mechanism of action of inhibiting integrase strand transfer (INST). Preliminary testing against raltegravir-resistant HIVs showed marginal cross resistance, suggesting that the chemotypes of the various embodiments described herein could fit an inhibitory profile of second generation INSTIs.
    Type: Grant
    Filed: March 3, 2016
    Date of Patent: November 6, 2018
    Assignee: Regents of the University of Minnesota
    Inventor: Zhengqiang Wang
  • Patent number: 9951056
    Abstract: Compounds of Formula I, as shown below and defined herein: and pharmaceutically acceptable salts, syntheses, intermediates, formulations, and methods of treating diseases including cancer, inflammation, and autoimmune disease mediated at least in part by Bruton's Tyrosine Kinase (BTK).
    Type: Grant
    Filed: September 29, 2014
    Date of Patent: April 24, 2018
    Assignee: BEIJING INNOCARE PHARMA TECH CO., LTD.
    Inventors: Xiangyang Chen, Yingxiang Gao, Chong Liu, Haihong Ni, Mark Mulvihill
  • Patent number: 9943075
    Abstract: The present invention provides compositions (i.e., preservation solutions) for preserving biologies comprising at least one membrane penetrable sugar, at least one membrane impenetrable sugar, at least one anti-microbial agent, at least one anti-oxidant, adenosine, albumin, a salt, a buffer, and a chelating agent, and to methods of using such preservation solutions to preserve biologies.
    Type: Grant
    Filed: February 16, 2011
    Date of Patent: April 17, 2018
    Assignee: HEMEMICS BIOTECHNOLOGIES, INC.
    Inventors: David Ho, Stephen P. Bruttig
  • Patent number: 9840491
    Abstract: The present disclosure relates to inhibitors of USP7 inhibitors useful in the treatment of cancers, neurodegenerative diseases, immunological disorders, inflammatory disorders, cardiovascular diseases, ischemic diseases, viral infections and diseases, and bacterial infections and diseases, having the Formula: where R1, R2, R3, R4, R4?, X1, Y1, Y2, Y3, Y4, n, and m are described herein.
    Type: Grant
    Filed: February 4, 2016
    Date of Patent: December 12, 2017
    Assignee: FORMA Therapeutics, Inc.
    Inventors: Stephanos Ioannidis, Adam Charles Talbot, Bruce Follows, Alexandre Joseph Buckmelter, Minghua Wang, Ann-Marie Campbell, David R. Lancia, Jr.
  • Patent number: 9771351
    Abstract: A Wnt signaling inhibitor which comprises, as an active ingredient, a fused-ring heterocyclic compound represented by the following formula (IA) or a pharmaceutically acceptable salt thereof, and the like are provided: (wherein, n1A represents 0 or 1; n2A and n3A may be the same or different, and each represents 1 or 2; ROA represents optionally substituted aryl or the like; R2A represents a hydrogen atom or the like; R3A represents an optionally substituted aromatic heterocyclic group or the like; X1A, X2A, X3A and X4A each represent CH or the like; Y1A represents CH2 or the like; Y2A represents N or the like; and LA represents CH2 or the like).
    Type: Grant
    Filed: July 29, 2014
    Date of Patent: September 26, 2017
    Assignee: KYOWA HAKKO KIRIN CO., LTD.
    Inventors: Hiroshi Ishida, Keiichi Motosawa, Yusuke Miura, Ryuichiro Nakai, Ryoko Okada, Yuichi Takahashi
  • Patent number: 9701691
    Abstract: The present invention relates to the use of novel compounds of Formula I: wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.
    Type: Grant
    Filed: January 10, 2013
    Date of Patent: July 11, 2017
    Assignee: Hoffman-La Roche Inc.
    Inventors: Shaoqing Chen, Johannes Cornelius Hermann, Nam T. Le, Matthew C. Lucas, Fernando Padilla
  • Patent number: 9661853
    Abstract: This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”).
    Type: Grant
    Filed: August 25, 2016
    Date of Patent: May 30, 2017
    Assignee: Dow AgroSciences LLC
    Inventors: Natalie C. Giampietro, Gary D. Crouse, Thomas C. Sparks, David A Demeter
  • Patent number: 9623021
    Abstract: The present invention relates to methods for prevention and/or treatment of metabolic disorders, post-menopausal obesity and conditions associated with high fat diet consumption including, obesity, body weight gain, fat mass formation, bone mineral content reduction, white adipose tissue weight gain, increased cholesterol levels, increased leptin levels, insulin resistance, type II diabetes, increased blood glucose levels, inflammatory diseases, cardiovascular diseases, fatty liver condition (accumulation of fat in the liver), decreased uncoupling protein-1 (UCP-1) levels and increased lipogenesis.
    Type: Grant
    Filed: May 4, 2010
    Date of Patent: April 18, 2017
    Assignee: GTX, Inc.
    Inventors: Ramesh Narayanan, Muralimohan Yepuru, James T. Dalton
  • Patent number: 9573940
    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: Grant
    Filed: March 26, 2015
    Date of Patent: February 21, 2017
    Assignee: JANSSEN PHARMACEUTICA NV
    Inventors: Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan
  • Patent number: 9550738
    Abstract: The present invention is directed to novel bicyclic compounds, their derivatives, pharmaceutically acceptable salts, solvates and hydrates thereof. The compounds and compositions of the present invention have protein kinases inhibitory activities and are useful for the treatment of protein kinases mediated diseases and conditions. Novel bicyclic compounds disclosed herein include quinazolines shown in Formula I (X?N).
    Type: Grant
    Filed: May 13, 2013
    Date of Patent: January 24, 2017
    Inventor: Dawei Zhang
  • Patent number: 9493426
    Abstract: The invention relates to new quinazolinone 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: Grant
    Filed: April 25, 2014
    Date of Patent: November 15, 2016
    Assignee: ASTEX THERAPEUTICS LIMITED
    Inventors: Patrick René Angibaud, Olivier Alexis Georges Querolle, Isabelle Noëlle Constance Pilatte, Lieven Meerpoel, Virginie Sophie Poncelet
  • Patent number: 9395369
    Abstract: The present disclosure provides an isolated or purified guinea pig cytomegalovirus (GPCMV) Strain CIDMTR, glycoproteins from GPCMV Strain CIDMTR, and methods of use thereof.
    Type: Grant
    Filed: October 21, 2013
    Date of Patent: July 19, 2016
    Assignee: REGENTS OF THE UNIVERSITY OF MINNESOTA
    Inventor: Mark Schleiss
  • Patent number: 9371292
    Abstract: Disclosed are as represented by Formula (I) a quinazoline derivative and a pharmaceutical acceptable salt thereof, or, an enantiomer, a non-enantiomer, a tautomer, a racemate, a solvate, a metabolic precursor, or a prodrug of both. Also disclosed are a preparation method therefor, an intermediate, a pharmaceutical composition having the quinazoline derivative, and an application thereof. The quinazoline derivative of the present invention is provided with improved anti-tumor activity.
    Type: Grant
    Filed: July 27, 2012
    Date of Patent: June 21, 2016
    Assignees: SHANGHAI PHARMACEUTICALS HOLDINGS CO., LTD., ZHEJIANG UNIVERSITY
    Inventors: Guangxin Xia, Jingkang Shen, Yongping Yu, Wenteng Chen, Chunchun Zhang, Yu Hao, Jing Zhang, Bojun Li, Xuejun Liu
  • Patent number: 9321760
    Abstract: The invention provides novel heterocyclic amine compounds according to Formula (I) and their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
    Type: Grant
    Filed: September 12, 2012
    Date of Patent: April 26, 2016
    Assignee: Merck Patent GmbH
    Inventors: Ruoxi Lan, Bayard R. Huck, Xiaoling Chen, Lizbeth Celeste Deselm, Hui Qiu, Yufang Xiao, Constantin Neagu, Igor Mochalkin, Theresa L. Johnson
  • Patent number: 9212190
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.
    Type: Grant
    Filed: January 10, 2013
    Date of Patent: December 15, 2015
    Assignee: Nimbus Iris, Inc.
    Inventors: Geraldine C. Harriman, Ronald T. Wester, Donna L. Romero, Shaughnessy Robinson, Mee Shelley, Matthew David Wessel, Jeremy Robert Greenwood, Craig E. Masse, Rosana Kapeller-Libermann
  • Patent number: 9157084
    Abstract: Compositions and methods to attenuate the immunosuppressive activity of TGF-? through the use of bi-functional shRNAs was substituted therefor described herein. The bi-functional shRNAs of the present invention knocks down the expression of furin in cancer cells to augment tumor antigen expression, presentation, and processing through expression of the GM-CSF transgene.
    Type: Grant
    Filed: December 20, 2010
    Date of Patent: October 13, 2015
    Assignee: GRADALIS, INC.
    Inventors: John J. Nemunaitis, Neil Senzer, Phillip B. Maples, Donald Rao
  • Patent number: 9067963
    Abstract: The present invention provides N-alkyl 2-(disubstituted)alkynyladenosine-5?-uronamides and derivatives thereof and pharmaceutical compositions containing the same that are selective agonists of A2A adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.
    Type: Grant
    Filed: July 31, 2013
    Date of Patent: June 30, 2015
    Assignee: Lewis and Clark Pharmaceuticals, LLC
    Inventors: Robert D Thompson, Anthony Beauglehole, Guoquan Wang
  • Patent number: 9062029
    Abstract: Compounds selected from the group according to Claim 1 are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumours.
    Type: Grant
    Filed: January 7, 2014
    Date of Patent: June 23, 2015
    Assignee: Merck Patent GmbH
    Inventors: Oliver Schadt, Dieter Dorsch, Frank Stieber, Andree Blaukat
  • Publication number: 20150148327
    Abstract: The invention provides certain substituted pyridines of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, Cy, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
    Type: Application
    Filed: June 17, 2013
    Publication date: May 28, 2015
    Applicant: Merck Canada Inc.
    Inventors: Andrew M. Haidle, Sandra Lee Knowles, Solomon D. Kattar, Denis Deschenes, Jason Burch, Joel Robichaud, Matthew Christopher, Michael D. Altman, James P. Jewell, Alan B. Northrup, Marc Blouin, John Michael Ellis, Hua Zhou, Christian Fischer, Adam J. Schell, Michael H. Reutershan, Brandon M. Taoka, Anthony Donofrio, Joel Robichaud
  • Publication number: 20150141408
    Abstract: The present invention relates to tricyclic pyrrolo derivatives which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.
    Type: Application
    Filed: January 30, 2015
    Publication date: May 21, 2015
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Marina Caldarelli, Mauro Angiolini, Italo Beria, Maria Gabriella Brasca, Francesco Casuscelli, Roberto D'Alessio, Andrea Lombardi Borgia
  • Patent number: 9006232
    Abstract: A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: wherein Z represents nitrogen atom or C—X; X represents hydrogen atom or fluorine atom; R1 is hydrogen atom or a C1-C3 alkyl group; L represents single bond or a C1-C6 alkylene group which may be substituted; Y represents single bond, sulfur atom, oxygen atom, NH, or the like; R2 represents hydrogen atom or a cyclic group which may be substituted, which is used for preventive and/or therapeutic treatment of a disease caused by abnormal activity of tau protein kinase 1 such as a neurodegenerative diseases (e.g. Alzheimer disease).
    Type: Grant
    Filed: August 11, 2010
    Date of Patent: April 14, 2015
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Kazuki Nakayama, Daiki Sakai, Kazutoshi Watanabe, Toshiyuki Kohara, Keiichi Aritomo
  • Publication number: 20150065478
    Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
    Type: Application
    Filed: November 11, 2014
    Publication date: March 5, 2015
    Inventors: Patrick Rene Angibaud, Kristof Van Emelen, Virginie Sophie Poncelet, Bruno Roux
  • Publication number: 20150057263
    Abstract: This invention relates to quinazoline compounds of Formula (I) which are inhibitors of the histone lysine methyltransferase (HKMTase) EZH2, and to uses of such compounds as medicaments, in particular in the treatment of a disease or disorder in which inhibition of EZH2 provides a therapeutic or prophylactic effect.
    Type: Application
    Filed: March 19, 2013
    Publication date: February 26, 2015
    Inventors: Robert Brown, Matthew John Fuchter, Nadine Chapman-Rothe, Nitipol Srimongkolpithak, Joachim Caron, James Synder, Thota Ganesh, Jin Liu, Aiming Sun
  • Publication number: 20150051195
    Abstract: The present invention relates to a series of novel compounds having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to novel intermediates useful in one or more steps of such syntheses. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutical amount of such compounds, optionally combined with one or more other drugs having antiviral activity.
    Type: Application
    Filed: October 30, 2014
    Publication date: February 19, 2015
    Inventors: Patrick Chaltin, Zeger Debyser, Marc De Maeyer, Arnaud Marchand, Damien Marchand, Wim Smets, Arnout Voet, Frauke Christ
  • Publication number: 20150045339
    Abstract: The object is to provide an Fms-like tyrosine kinase 3 (FLT3) inhibitor useful as a therapeutic agent for acute myeloid leukemia (AML). A novel nitrogen-containing heterocyclic compound represented by the general formula [1] or a salt thereof is provided. The compound or a salt thereof of the present invention can be used as an active ingredient of a pharmaceutical composition for a treatment of a disease or condition relating to FLT3, such as acute myeloid leukemia (AML) and acute promyelocytic leukemia (APL).
    Type: Application
    Filed: October 16, 2014
    Publication date: February 12, 2015
    Applicant: FUJIFILM CORPORATION
    Inventors: Masaru TAKASAKI, Toshiaki TSUJINO, Shintarou TANABE, Megumi OOKUBO, Kimihiko SATO, Atsushi HIRAI, Daisuke TERADA, Shinsuke INUKI, Shinsuke MIZUMOTO
  • Publication number: 20150011534
    Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, R4? have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.
    Type: Application
    Filed: September 25, 2014
    Publication date: January 8, 2015
    Applicant: MERCK PATENT GMBH
    Inventors: Dieter DORSCH, Frank STIEBER, Oliver SCHADT, Andree BLAUKAT
  • Patent number: 8921357
    Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, R4? have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumors.
    Type: Grant
    Filed: March 5, 2013
    Date of Patent: December 30, 2014
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Frank Stieber, Oliver Schadt, Andree Blaukat
  • Patent number: 8906906
    Abstract: The present invention relates to a series of novel compounds having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to novel intermediates useful in one or more steps of such syntheses. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutical amount of such compounds, optionally combined with one or more other drugs having antiviral activity.
    Type: Grant
    Filed: August 5, 2010
    Date of Patent: December 9, 2014
    Assignee: Katholieke Universiteit Leuven
    Inventors: Patrick Chaltin, Zeger Debyser, Marc De Maeyer, Arnaud Marchand, Damien Marchand, Wim Smets, Arnout Voet, Frauke Christ
  • Publication number: 20140336175
    Abstract: The present invention relates to compounds of formula (I): wherein R1 is C1-6alkylamino, C1-6alkoxy, or C3-7cycloalkyloxy; m is an integer having a value of 3 to 6; n is an integer having a value of 0 to 4; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.
    Type: Application
    Filed: May 16, 2014
    Publication date: November 13, 2014
    Applicant: GlaxoSmithKline LLC
    Inventors: Keith Biggadike, Diane Mary Coe, Xiao Qing Lewell, Charlotte Jane Mitchell, Stephen Allan Smith, Naimisha Trivedi
  • Publication number: 20140328805
    Abstract: The present invention provides for compounds of Formula I and embodiments and salts thereof for the treatment of diseases (e.g., neurodegenerative diseases). R1, R2, R3, X1, X2, A and Cy variable in Formula all have the meaning as defined herein.
    Type: Application
    Filed: May 1, 2014
    Publication date: November 6, 2014
    Applicant: GENENTECH, INC.
    Inventors: Anthony Estrada, Alan G. Olivero, Snahel Patel, Michael Siu
  • Publication number: 20140323466
    Abstract: Disclosed are new thienyl[3,2-d]pyrimidin-4-one compounds shown as the general formula (I), preparation method, pharmaceutical compositions and pharmacological use thereof. The compounds are strong DPPIV (dipeptide peptidase IV) inhibitors and can treat type II diabetes through well inhibiting DPPIV indirectly increasing the content of GLP-1 in vivo and inducing a series of physiological actions in vivo. Therefore, the compounds could be developed as new promising drugs for treating diabetes.
    Type: Application
    Filed: October 23, 2012
    Publication date: October 30, 2014
    Inventors: Hong Liu, Jia Li, Jian Li, Jingya Li, Jiang Wang, Mingbo Su, Jie Lian, Hualiang Jiang, Kaixian Chen
  • 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: 20140303149
    Abstract: Compounds of the formula I or II: wherein X, m, Ar, R1 and R2 are as defined herein. The subject compounds are useful for treatment of IRAK-mediated conditions.
    Type: Application
    Filed: April 2, 2014
    Publication date: October 9, 2014
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Nidhi Arora, Shaoqing Chen, Johannes Cornelius Hermann, Andreas Kuglstatter, Sharada Shenvi Labadie, Clara Jeou Jen Lin, Matthew C. Lucas, Amy Geraldine Moore, Eva Papp, Francisco Xavier Talamas, Jutta Wanner, Yansheng Zhai
  • Publication number: 20140294764
    Abstract: This disclosure relates to compounds, compositions and methods of epigenetically transforming cells. In certain embodiments, the disclosure relates to methods of generating epigenetically altered cells comprising mixing isolated cells with compositions disclosed herein under conditions such that epigenetically altered cells are formed. In certain embodiments, the disclosure contemplates inducing cells, such as adult somatic cells or cells that are not naturally pluripotent, into cells with chemically induce pluripotency. In certain embodiments, the disclosure contemplates certain compounds disclosed herein, compounds disclosed herein optionally substituted with one or more substituents, derivatives, or salts thereof, for these purposes.
    Type: Application
    Filed: November 8, 2012
    Publication date: October 2, 2014
    Applicants: ISTITUTO PASTEUR - FONDAZIONE CENCI BOLOGNETTI, EMORY UNIVERSITY
    Inventors: Young-Sup Yoon, Xiaodong Cheng, Ji Woong Han, Antonello Mai
  • Publication number: 20140296201
    Abstract: Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A compound is represented by Structural Formula (IA) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.
    Type: Application
    Filed: June 16, 2014
    Publication date: October 2, 2014
    Inventors: Paul S. Charifson, Michael P. Clark, Upul K. Bandarage, Randy S. Bethiel, John J. Court, Hongbo Deng, Ioana Davies, John P. Duffy, Luc J. Farmer, Huai Gao, Wenxin Gu, Dylan H. Jacobs, Joseph M. Kennedy, Mark W. Ledeboer, Brian Ledford, Francois Maltais, Emanuele Perola, Tiansheng Wang, M. Woods Wannamaker, Randal Byrn, Yi Zhou, Chao Lin, Min Jiang, Steven Jones, Ursula A. Germann, Francesco G. Salituro, Ann Dak-Yee Kwong
  • Patent number: 8822451
    Abstract: 4-amido-pyrimidine compounds, derivatives and compositions thereof, and synthetic methods described herein are useful for modulating ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Grant
    Filed: May 22, 2006
    Date of Patent: September 2, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara S. Hadida Ruah, Anna R. Hazlewood, Peter D. J. Grootenhuis, Ashvani Kumar Singh, Thomas Cleveland, Frederick F. Van-Goor
  • Publication number: 20140243290
    Abstract: The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.
    Type: Application
    Filed: April 17, 2014
    Publication date: August 28, 2014
    Inventors: Michael D. Altman, Brian M. Andresen, Kenneth L. Arrington, Sathesh Bhat, Jason Burch, Kaleen Konrad Childers, Bernard Cote, Maria Emilia Di Francesco, Anthony Donofrio, Kristina Dupont-Gaudet, John Michael Ellis, Christian Fischer, Jean-Francois Fournier, Jacques Yves Gauthier, Jonathan Grimm, Daniel Guay, David Joseph Guerin, Andrew M. Haidle, Solomon D. Kattar, Sandra Lee Knowles, Chaomin Li, Jongwon Lim, Michelle R. Machacek, Matthew L. Maddess, Alan B. Northrup, Brendan M. O'Boyle, Ryan D. Otte, Alessia Petrocchi, Michael H. Reutershan, Joel S. Robichaud, Eric T. Romeo, Adam J. Schell, Tony Siu, Kerrie B. Spencer, Brandon M. Taoka, B. Wesley Trotter, Hyun Chong Woo, Hua Zhou
  • Publication number: 20140235615
    Abstract: Provided is a compound useful for the prophylaxis or treatment of cancer. The present invention relates to a compound represented by formula (I): wherein each symbol in the formula is as defined in the specification, or a salt thereof or a prodrug thereof, which is useful for the prophylaxis or treatment of cancer.
    Type: Application
    Filed: March 24, 2014
    Publication date: August 21, 2014
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Misaki HOMMA, Toru MIYAZAKI, Yuya OGURO, Osamu KURASAWA
  • Publication number: 20140228352
    Abstract: Provided is a compound useful for the prophylaxis or treatment of cancer. The present invention relates to a compound represented by formula (I): wherein each symbol in the formula is as defined in the specification, or a salt thereof or a prodrug thereof, which is useful for the prophylaxis or treatment of cancer.
    Type: Application
    Filed: March 24, 2014
    Publication date: August 14, 2014
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Misaki HOMMA, Toru MIYAZAKI, Yuya OGURO, Osamu KURASAWA
  • Publication number: 20140221315
    Abstract: The present application provides novel pyrimido-pyridazinone compounds and methods for preparing and using these compounds. These compounds are useful in treating inflammation in patients by administering one or more of the compounds to a patient. In one embodiment, the novel pyrimido-pyridazinone compound is of Formula (I) and R1 and R2 are defined herein.
    Type: Application
    Filed: April 3, 2014
    Publication date: August 7, 2014
    Applicant: Endo Pharmaceuticals Inc.
    Inventors: Aranapakam Venkatesan, Roger Astbury Smith, Subramanya Hosahalli, Vijay Potluri, Sunil Kumar Panigrahi, Vishnu Basetti, Karunasree Kunta