Plural Ring Nitrogens In The Bicyclo Ring System Patents (Class 514/234.5)
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Publication number: 20140134130Abstract: Compounds of Formula I, including pharmaceutically acceptable salts thereof, as well as compositions containing these compounds, have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV:Type: ApplicationFiled: November 7, 2013Publication date: May 15, 2014Inventors: Tao Wang, Zhiwei Yin, Paul Michael Scola
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Publication number: 20140134161Abstract: The present invention relates to compositions and methods for treatment of neurological disorders. In particular, the present invention relates to EGFR as a clinical target for treatment of neurological disorders.Type: ApplicationFiled: July 5, 2012Publication date: May 15, 2014Applicant: SYKEHUSET SØRLANDET HFInventors: Christian Kersten, Marte Grønlie Cameron, Svein Mjåland
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Publication number: 20140128373Abstract: Compounds active on protein kinases are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.Type: ApplicationFiled: February 1, 2012Publication date: May 8, 2014Inventors: Prabha N. Ibrahim, Chao Zhang, Wayne Spevak, Jiazhong Zhang, Guoxian Wu, Jack Lin, Hanna Cho, Marika Nespi, Songyuan Shi, Todd Ewing, Ying Zhang
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Publication number: 20140127157Abstract: Antiviral activity of Nilotinib against Hepatitis C virus.Type: ApplicationFiled: November 4, 2013Publication date: May 8, 2014Inventors: Erica Canino, Adam Feire, Christopher Jones, Paul W. Manley
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Publication number: 20140128390Abstract: Compounds active on c-kit protein kinases or mutant c-kit protein kinases having any mutations are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of the c-kit protein kinases and mutant c-kit protein kinases.Type: ApplicationFiled: September 5, 2013Publication date: May 8, 2014Inventors: JACK LIN, JOHN BUELL, KATRINA CHAN, TODD EWING, PRABHA IBRAHIM, MARIKA NESPI, PHUONGLY PHAM, SONGYUAN SHI, WAYNE SPEVAK, GUOXIAN WU, JIAZHONG ZHANG, YING ZHANG
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Publication number: 20140128391Abstract: Provided herein are compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with HDAC activity, particularly diseases or disorders that involve activity of HDAC1 and/or HDAC2. Such diseases include cancer, sickle-cell anemia, beta-thalassemia, and HIV.Type: ApplicationFiled: November 1, 2013Publication date: May 8, 2014Inventors: John H. van Duzer, Ralph Mazitschek
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Publication number: 20140121206Abstract: The present invention relates to spirocarbamate compounds of Formula (I) in which R1, (R2)Y, R3, R4, X and A have the meanings given in the specification. The invention further provides pharmaceutical compositions containing the compounds or pharmaceutically acceptable salts thereof and relates to their use of these compounds as TRPV4 antagonists in treating or preventing conditions associated with TRPV4 imbalance.Type: ApplicationFiled: June 15, 2012Publication date: May 1, 2014Applicant: GlaxoSmithKliine, LLCInventors: Carl Brooks, Mui Cheung, Hilary Schenck Eidam, Krista B. Goodman, Marlys Hammond, Mark A. Hilfiker, Tram H. Hoang, Jaclyn R. Patterson, Patrick Stoy, Guosen Ye
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Publication number: 20140107119Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein.Type: ApplicationFiled: November 15, 2013Publication date: April 17, 2014Applicant: AbbVie Inc.Inventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura A. Hexamer, Aaron R. Kunzer, Robert A. Mantei, William J. McClellan, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt, Todd M. Hansen
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Publication number: 20140107123Abstract: The invention relates to the treatment and prevention of type I diabetes. More specifically, the invention relates to compounds that treat or prevent the body's immune system from destroying ?-cells (i.e., insulin-producing cells in the pancreatic islets of Langerhans) by inhibition of JNK2, selective inhibition of JNK2, or inhibition of the expression of the MAPK9 gene or gene product. In one embodiment, the present invention contemplates the diagnosis, identification, production, and use of compounds which modulate MAPK9 gene expression or the activity of the MAPK9 gene product including but not limited to, JNK2, the nucleic acid encoding MAPK9 and homologues, analogues, and deletions thereof, as well as antisense, ribozyme, triple helix, antibody, and polypeptide molecules as well as small inorganic molecules. The present invention contemplates a variety of pharmaceutical formulations and routes of administration for such compounds.Type: ApplicationFiled: August 5, 2013Publication date: April 17, 2014Applicant: University of MassachusettsInventors: Roger J. Davis, Anja Jaeschke
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Publication number: 20140107120Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, n, X, R2-3 and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: December 18, 2013Publication date: April 17, 2014Applicant: THERAVANCE, INC.Inventors: Paul Allegretti, Seok-Ki Choi, Paul R. Fatheree, Roland Gendron, Ryan Hudson, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson
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Publication number: 20140107118Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of Alzheimer's Disease or diabetes via inhibition of BACE-1 or BACE-2.Type: ApplicationFiled: December 20, 2013Publication date: April 17, 2014Applicant: NOVARTIS AGInventors: Sangamesh BADIGER, Murali CHEBROLU, Konstanze HURTH, Sebastien JACQUIER, Rainer Martin LUEOEND, Rainer MACHAUER, Heinrich RUEEGER, Marina TINTELNOT-BLOMLEY, Siem Jacob VEENSTRA, Markus VOEGTLE
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Publication number: 20140105886Abstract: Glioblastoma multiforme (GBM) is an aggressive form of brain cancer. Biomarkers for GBM that provide prognostic and predictive information are useful because they provide the physician valuable information regarding treatment options for GBM. The present invention provides a method to quantify such biomarkers. Thus, the method relates to the quantification of GSK3?, S6, CREB, PTEN, AKT and mTOR biomarkers and the use of AQUA® analysis to estimate a patient's risk and benefit to treatment using an inhibitor of the AGC-family kinase. Unlike traditional IHC, the AQUA® system is objective and produces quantitative in situ protein expression data on a continuous scale. The present invention uses the AQUA system to provide a robust and standardized diagnostic assay that can be used in a clinical setting to provide prognostic and predictive information.Type: ApplicationFiled: July 9, 2013Publication date: April 17, 2014Inventors: Waldron Donald E., Pinard Robert, Gustavson Mark
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Publication number: 20140107073Abstract: Described are GCF-8 inhibitors of the formula (I), and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R5, R6, X and Z are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for inhibiting GDF-8 in a cell and methods for treating a patient suffering from a disease or disorder, wherein the patient would therapeutically benefit from an increase in mass or strength of muscle tissue.Type: ApplicationFiled: October 4, 2013Publication date: April 17, 2014Applicant: Rigel Pharmaceuticals, Inc.Inventors: Somasekhar Bhamidipati, Marina Gelman, Pingyu Ding, Rajinder Singh, Jeffrey Clough, Todd Kinsella, Donald Payan
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Patent number: 8697692Abstract: The present invention relates to pyrrolo[3,2-c]pyridine-4-one 2-indolinone compounds of Formula (I) and their pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8 X, Y and have the meaning cited in the specification. Also disclosed are the pharmaceutical compositions containing the foregoing compounds, methods for the preparation and pharmaceutical use thereof, particularly as protein kinase inhibitors. Formula (I).Type: GrantFiled: August 2, 2011Date of Patent: April 15, 2014Assignee: Shanghai Hengrui Pharmaceutical Co., Ltd.Inventors: Peng Cho Tang, Yidong Su, Lei Zhang, Lu Xiao
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Patent number: 8697693Abstract: Thienopyrimidines of formula (Ia) or (Ib): wherein R1-R3 have any of the values described herein, and the pharmaceutically acceptable salt thereof have activity as inhibitors of PI3K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behavior associated with PI3 kinase, in particular the p110 delta subtype, such as immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. Processes for synthesizing the compounds are also described.Type: GrantFiled: July 19, 2012Date of Patent: April 15, 2014Assignee: F. Hoffmann LaRoche AGInventors: Stewart James Baker, Paul John Goldsmith, Timothy Colin Hancox, Neil Anthony Pegg, Stephen Price, Stephen Joseph Shuttleworth, Sukhjit Sohai
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Patent number: 8697667Abstract: The present invention is directed to drug delivery vehicles comprising one or more cyclodextrin moieties conjugated to a dendritic polyamine for the delivery of small molecule and protein therapeutic molecules and nucleic acid therapeutic molecules, and methods of making and using the delivery vehicles.Type: GrantFiled: October 11, 2011Date of Patent: April 15, 2014Assignee: Rutgers, The State University of New JerseyInventors: Ki-Bum Lee, Birju Shah, Prasad Subramaniam, Cheoljin Kim
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Patent number: 8697685Abstract: The invention is directed to 6-(4-pyrimidinyl)-1H-indazole derivatives. Specifically, the invention is directed to compounds according to Formula (I) wherein R1-R4 are defined herein. The compounds of the invention axe inhibitors of PDK1 and can be useful in the treatment of immune and metabolic diseases and disorders characterized by constitutively activated ACG kinases such as cancer and more specifically cancers of the breast, colon, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PDK1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: GrantFiled: November 18, 2009Date of Patent: April 15, 2014Assignee: GlaxoSmithKline LLCInventors: Jeffrey Michael Axten, Charles William Blackledge, Jr., Gerald Patrick Brady, Jr., Yanhong Feng, Seth W. Grant, Jesus Raul Medina, William H. Miller, Stuart P. Romeril
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Publication number: 20140100221Abstract: 1H-Pyrrolo[2,3-b]pyridine compounds are inhibitors of cell proliferation/cell vitality and can be employed for the treatment of tumours.Type: ApplicationFiled: October 2, 2013Publication date: April 10, 2014Applicant: MERCK PATENT GMBHInventors: Timo HEINRICH, Margarita WUCHERER-PLIETKER, Hans-Peter BUCHSTALLER
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Patent number: 8691810Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A, B, R1, R2, R3, R4a, R5, and Z are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as aurora.Type: GrantFiled: May 12, 2011Date of Patent: April 8, 2014Assignee: AbbVie Inc.Inventors: Michael R. Michaelides, Andrew S. Judd, Shannon R. Fix-Stenzel, Richard F. Clark, Bryan K. Sorensen, Zhiqin Ji
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Publication number: 20140094471Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.Type: ApplicationFiled: September 26, 2013Publication date: April 3, 2014Applicants: AbbVie Inc., The Walter and Eliza Hall Institute of Medical Research, Genentech, Inc.Inventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa A. Hasvold, Laura Hexamer, Aaron R. Kunzer, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt, Robert A. Mantei, Todd M. Hansen
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Publication number: 20140094450Abstract: The present invention relates to benzoimidazole-carboxylic acid amide compounds of the formula I, in which R?, R?, R??, R1, R2, R3, R4, R5, R6 and Z are defined as indicated below. The compounds of the formula I are APJ receptor modulators, and are useful for the treatment of diseases associated with increased blood pressure for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.Type: ApplicationFiled: September 19, 2013Publication date: April 3, 2014Applicant: SANOFIInventors: Stephanie HACHTEL, Paulus WOHLFART, John WESTON, Marco MUELLER, Elisabeth DEFOSSA, Katharina MERTSCH, Jian-Hui WENG, Robert Alan BINNIE, Farid ABDUL-LATIF, William Jerome BOCK, Armin WALSER
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Patent number: 8685968Abstract: Provided herein is a pharmaceutical composition that comprises a pharmaceutically acceptable carrier or diluent and, as an active ingredient, the compound 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine bismesylate.Type: GrantFiled: November 5, 2012Date of Patent: April 1, 2014Assignee: F. Hoffmann-La Roche AGInventors: Irina Chuckowree, Adrian Folkes, Tim Hancox, Stephen Shuttleworth
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Patent number: 8685969Abstract: Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof, formula (I) are useful as kinase modulators, including Btk modulation.Type: GrantFiled: June 16, 2011Date of Patent: April 1, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Chunjian Liu, James Lin, George V. DeLucca, Douglas G. Batt, Qingjie Liu
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Publication number: 20140088102Abstract: Provided herein are (alpha-substituted cycloalkylamino or heterocyclylamino) pyrimidinyl and 1,3,5-triazinyl benzimidazoles, e.g., a compound of Formula I, and their pharmaceutical compositions, preparation, and use as agents or drugs for treating proliferative diseases.Type: ApplicationFiled: March 27, 2012Publication date: March 27, 2014Applicant: MEI PHARMA, INC.Inventors: S. David Brown, David J. Matthews
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Publication number: 20140086995Abstract: Compositions and methods for localized delivery of a therapeutic agent to a biological tissue over time. The composition includes a temperature-responsive polymer and one or more microspheres, each having degradation rate different from the other, and each comprising a therapeutic agent. In the method, the composition is applied to a biological tissue and forms a gel that adheres to the tissue.Type: ApplicationFiled: April 12, 2012Publication date: March 27, 2014Inventors: Buddy D. Ratner, Julee Floyd, Rohan Ramakrishna, Anna Galperin
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Publication number: 20140088103Abstract: Provided herein are (fused ring arylamino and heterocyclylamino) pyrimidinyl and 1,3,5-triazinyl benzimidazoles, e.g., a compound of Formula (I), and their pharmaceutical compositions, preparation, and use as agents or drugs for treating proliferative diseases.Type: ApplicationFiled: March 27, 2012Publication date: March 27, 2014Applicant: MEI PHARMA, INC.Inventors: S. David Brown, David J. Matthews
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Publication number: 20140088100Abstract: Described herein are inhibitors of FGFR, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of tyrosine kinases.Type: ApplicationFiled: July 11, 2013Publication date: March 27, 2014Applicant: BLUEPRINT MEDICINESInventors: Neil Bifulco, JR., Natasja Brooijmans, Brian L. Hodous, Joseph L. Kim, Chandrasekhar V. Miduturu
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Publication number: 20140088101Abstract: The present disclosure relates to novel compounds, methods, and compositions capable of inhibiting HIF hydroxylase enzyme activity, thereby increasing the stability and/or activity of hypoxia inducible factor (HIF).Type: ApplicationFiled: February 1, 2012Publication date: March 27, 2014Applicant: FibroGen, Inc.Inventors: Danny Ng, Michael P. Arend, Lee A. Flippin
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Publication number: 20140088094Abstract: The invention provides tetrahydroquinoline and related compounds, pharmaceutical compositions, methods of inhibiting ROR? activity, reducing the amount of IL-17 in a subject, and treating immune disorders and inflammatory disorders using such tetrahydroquinoline and related compounds are provided.Type: ApplicationFiled: November 8, 2011Publication date: March 27, 2014Applicants: Merck Sharp & Dohme Corp., Lycera CorporationInventors: Gary D. Glick, Peter L. Toogood, Arthur Glenn Romero, Chad A. Van Huis, Thomas Daniel Aicher, Carl Kaub, Matthew N. Mattson, William David Thomas, Karin Ann Sttein, Erik Krogh-Jespersen, Zhan Wang
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Publication number: 20140088075Abstract: The invention relates to dihydronaphthyridines and related compounds; compositions comprising an effective amount of a dihydronaphthyridine or a related compound; and methods for treating or preventing proliferative diseases comprising the administration of an effective amount of a dihydronaphthyridine or a related compound.Type: ApplicationFiled: March 13, 2013Publication date: March 27, 2014Applicant: DECIPHERA PHARMACEUTICALS, INC.Inventor: Deciphera Pharmaceuticals, Inc.
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Publication number: 20140080829Abstract: The present invention provides compounds of Formula I, including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.Type: ApplicationFiled: November 21, 2013Publication date: March 20, 2014Applicants: Genentech, Inc., Array BioPharma Inc.Inventors: Josef Bencsik, James F. Blake, James M. Graham, Martin F. Hentemann, Nicholas C. Kallan, Ian S. Mitchell, Stephen T. Schlachter, Keith L. Spencer, Dengming Xiao, Rui Xu, Mike Welch, Jun Liang, Brian S. Safina
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Publication number: 20140080828Abstract: This disclosure relates to antiviral compounds disclosed herein and uses related thereto. In certain embodiments, the disclosure relates to pharmaceutical compositions comprising 2-((benzo[d]imidazol-2-yl)thio)-N-phenylpropanamide derivatives, N-phenyl-2-((1-phenyl-benzo[d]imidazol-2-yl)thio)propanamide derivatives, or 2-((benzo[d]imidazol-2-yl)thio)-N-(2-chloro-4-methylphenyl)propanamide derivatives. The derivatives may be substituted with one or more substituents. Typically, the pharmaceutical composition comprises a compound of Formula (I), or salt, prodrug, or ester thereof wherein X, Y, and R1 to R7 are described herein.Type: ApplicationFiled: March 28, 2012Publication date: March 20, 2014Applicants: CHILDREN'S HEATLHCARE OF ATLANTA, INC., EMORY UNIVERSITYInventors: Richard K. Plemper, James P. Snyder, Aiming Sun, John M. Ndungu, Jeong-Joong Yoon
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Publication number: 20140080807Abstract: The present invention relates to substituted indazole compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by degulated protein kinase activity, like cancer. 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: ApplicationFiled: May 7, 2012Publication date: March 20, 2014Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Andrea Lombardi Borgia, Marina Ciomei, Daniele Donati, Marcella Nesi
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Publication number: 20140080783Abstract: The present invention relates to the field of oncology and provides compositions and methods for treating specific cancers, including non small cell lung cancer, breast cancer, thyroid cancer, pancreatic cancer, colon cancer, melanoma, hepatoma and adenocarcinoma. Particularly, compositions and methods involving administration, either simultaneously or sequentially, of pharmaceutical combinations comprising (S)—N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide with other compounds, to patients suffering from cancer are described.Type: ApplicationFiled: November 18, 2013Publication date: March 20, 2014Applicant: ARDEA BIOSCIENCES, INC.Inventor: Mark CHAPMAN
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Publication number: 20140080830Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): And salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3-kinase activity.Type: ApplicationFiled: November 25, 2013Publication date: March 20, 2014Applicant: GlaxoSmithKline Intellectual Property Development LimitedInventors: Julie Nicole Hamblin, Paul Spencer Jones, Suzanne Elaine Keeling, Joelle Le, Charlotte Jane Mitchell, Nigel James Parr
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Patent number: 8673893Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.Type: GrantFiled: September 12, 2012Date of Patent: March 18, 2014Assignee: Nerviano Medical Sciences S.r.l.Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
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Patent number: 8674113Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, L, M, W, R1, R2, R3, R4, R6, R7, R9, Ra, Rb have meanings given in the description.Type: GrantFiled: December 8, 2011Date of Patent: March 18, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Henning Priepke, Henri Doods, Alexander Heim-Riether, Raimund Kuelzer, Roland Pfau, Klaus Rudolf, Dirk Stenkamp
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Publication number: 20140073639Abstract: The application describes targets and methods that can inhibit bacterial growth in Gram-positive and Gram-negative bacteria. A bacterial enzyme, 2-epimerase, is common to both Gram-positive and Gram-negative bacteria and contains an allosteric site that can be targeted to disrupt the enzyme. The allosteric site is present on the bacterial 2-epimerase, but the analogous mammalian enzyme does not contain the allosteric site, providing a route for attacking bacterial infections without affecting the mammalian enzyme.Type: ApplicationFiled: August 8, 2013Publication date: March 13, 2014Applicants: The Rockefeller University, Avacyn Pharmaceuticals, Inc.Inventors: Vincent A. FISCHETTI, Allan R. GOLDBERG, Raymond SCHUCH
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Publication number: 20140073642Abstract: This invention relates to quinazoline derivatives, processes for their preparation, pharmaceutical compositions, and their use in therapy of disorders in which the modulation of toll-like-receptors is involved.Type: ApplicationFiled: May 18, 2012Publication date: March 13, 2014Applicant: Janssen R&D IrelandInventors: David McGowan, Pierre Jean-Marie Bernard Raboisson, Tim Hugo Maria Jonckers, Stefaan Julien Last, Werner Embrechts, Serge Maria Aloysius Pieters
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Patent number: 8669251Abstract: 8-Fluorophthalazin-1(2h)-one compounds of Formula II where one or two of X1, X2, and X3 are N, are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula II for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: GrantFiled: November 2, 2012Date of Patent: March 11, 2014Assignee: Genentech, Inc.Inventors: James John Crawford, Daniel Fred Ortwine, BinQing Wei, Wendy B. Young
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Publication number: 20140065095Abstract: The invention relates to novel pyrrolidine derivatives of formula (I): wherein R1, R2 and R3 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.Type: ApplicationFiled: June 5, 2013Publication date: March 6, 2014Inventors: Ulrich Heiser, Daniel Ramsbeck, Robert Sommer, Antje Meyer, Torsten Hoffmann, Livia Boehme, Hans-Ulrich Demuth
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Publication number: 20140066430Abstract: The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating Aurora kinase protein activity, thereby influencing various disease states and conditions related to the activities of Aurora kinase proteins. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, processes of preparing compounds of the invention, synthetic intermediates and methods of treatment of conditions related to the activity of Aurora kinase.Type: ApplicationFiled: October 3, 2013Publication date: March 6, 2014Applicant: Amgen Inc.Inventors: Victor J. CEE, Holly L. DEAK, Bingfan DU, Stephanie D. GEUNS-MEYER, Brian L. HODOUS, Hanh Nho NGUYEN, Philip R. Olivieri, Vinod F. Patel, Karina ROMERO, Laurie Schenkel
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Publication number: 20140056910Abstract: Provided are a pharmaceutical composition which enhances the sensitivity of a cancer to a molecular target drug, such as gefitinib and erlotinib, wherein the cancer has resistance to the molecular target drug, and a cancer therapeutic agent effective against a cancer having resistance to a molecular target drug, such as gefitinib and erlotinib. The pharmaceutical composition comprising an HGF-MET receptor pathway inhibitor enhances the sensitivity of a cancer to a molecular target drug, such as gefitinib and erlotinib, even though the cancer has resistance to the molecular target drug. The cancer therapeutic agent comprising a molecular target drug in combination with an HGF-MET receptor pathway inhibitor is effective against a cancer having resistance to the molecular target drug.Type: ApplicationFiled: October 18, 2013Publication date: February 27, 2014Applicant: Kringle Pharma Inc.Inventors: Seiji YANO, Kunio MATSUMOTO
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Publication number: 20140057895Abstract: The present invention relates to a novel indazole- or pyrrolopyridine-derivative comprising a 5 membered heterocyclic substituent at 1 position thereof which has an agonistic action or a partial agonistic action against serotonin-4 receptor, and a pharmaceutical composition comprising the same.Type: ApplicationFiled: June 6, 2012Publication date: February 27, 2014Inventors: Kazuhiro Mizuno, Junya Ikeda, Takanori Nakamura, Masato Iwata, Hiromichi Otaka, Nana Goto
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Publication number: 20140057891Abstract: The present invention relates to substituted 6,5-fused bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: ApplicationFiled: November 4, 2013Publication date: February 27, 2014Applicant: Epizyme, Inc.Inventors: Kevin Wayne Kuntz, Edward James Olhava, Richard Chesworth, Kenneth William Duncan
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Patent number: 8658170Abstract: Provided is a method of treating a proliferative disease, condition, or disorder in a subject by administering a combination of an inhibitor of p53 and MDM2 binding and an EGFR inhibitor. Various embodiments of the disclosed methods provide a synergistic anti-proliferative or anti-apoptotic effect compared to administration of one agent alone.Type: GrantFiled: July 21, 2011Date of Patent: February 25, 2014Inventors: Joseph P. Errico, Benjamin Mugrage, Ignatius Turchi, Matthew Sills, Jane Ong, John Allocco, Pam Wines
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Patent number: 8658635Abstract: The invention is directed to certain novel compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.Type: GrantFiled: June 3, 2009Date of Patent: February 25, 2014Assignee: GlaxoSmithKline Intellectual Property Development LimitedInventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, John Edward Robinson, Juliet Kay Simpson, Christian Alan Paul Smethurst
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Publication number: 20140051700Abstract: Methods and compositions for agonizing a type-2 orexin receptor (OX2R) in a cell determined to be in need thereof, including the general method of (a) administering to a subject a cyclic guanidinyl OX2R agonist and (b) detecting a resultant enhanced wakefulness or increased resistance to diet-induced accumulation of body fat, or abbreviated recovery from general anesthesia or jet lag.Type: ApplicationFiled: August 20, 2012Publication date: February 20, 2014Inventor: Masashi Yanagisawa
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Publication number: 20140051701Abstract: The present invention provides methods of treating central nervous system disorders, such as mood disorders (e.g., depression) and neurodegenerative diseases using compounds of formula (I). The subject disclosure enables the manufacture of medicaments as well as compositions containing same for use in methods of therapy and prophylaxis of central nervous system disorders.Type: ApplicationFiled: March 2, 2012Publication date: February 20, 2014Applicant: Bionomics LimitedInventors: Sue O'Connor, Andrew John Harvey, Stephanie Wagner, Emile Andriambeloson
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Publication number: 20140051679Abstract: The present teachings provide a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof.Type: ApplicationFiled: October 12, 2012Publication date: February 20, 2014Applicant: UNIVERISTY HEALTH NETWORKSInventors: Heinz W. Pauls, Radoslaw Laufer, Yong Liu, Sze-Wan Li, Bryan T. Forrest, Yunhui Lang, Narendra Kumar B. Patel, Louise G. Edwards, Grace Ng, Peter B. Sampson, Miklos Feher, Donald E. Awrey