Plural Ring Nitrogens In The Bicyclo Ring System Patents (Class 514/234.5)
Quinoxalines (including hydrogenated) (Class 514/234.8)
  • THERAPEUTIC COMPOUNDS
    Publication number: 20140221347
    Abstract: Compounds of formula I: or pharmaceutically acceptable salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.
    Type: Application
    Filed: January 9, 2014
    Publication date: August 7, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Gediminas BRIZGYS, Chien-Hung CHOU, Randall L. HALCOMB, Yunfeng Eric HU, Qi LIU, John R. SOMOZA, Winston C. TSE, Jennifer R. ZHANG
  • BIOMARKERS OF THERAPEUTIC RESPONSIVENESS
    Publication number: 20140221368
    Abstract: The present invention relates to methods of diagnosing breast cancer in a patient, as well as methods of monitoring the progression of breast cancer and/or methods of monitoring a treatment protocol of a therapeutic agent or a therapeutic regimen. The invention also relates to assay methods used in connection with the diagnostic methods described herein.
    Type: Application
    Filed: January 30, 2014
    Publication date: August 7, 2014
    Applicant: Meso Scale Technologies, LLC
    Inventors: Simone Barbero, Eli N. Glezer, Anu Mathew
  • PYRROLOPYRIDINES AS KINASE INHIBITORS
    Publication number: 20140221370
    Abstract: Compounds of Formula (I) are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula (I) and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
    Type: Application
    Filed: April 9, 2014
    Publication date: August 7, 2014
    Applicant: Array BioPharma Inc.
    Inventors: James F. Blake, Indrani W. Gunawardana, Yvan LeHuerou, Peter J. Mohr, Eli M. Wallace, Bin Wang
  • Heteroaryl substituted pyrazole derivatives useful for treating hyper-proliferative disorders and diseases associated with angiogenesis
    Patent number: 8796253
    Abstract: This invention relates to novel heteroaryl substituted pyrazole compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients or therapeutic measures.
    Type: Grant
    Filed: May 8, 2008
    Date of Patent: August 5, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Stephen Boyer, Michael Härter, Philip Wickens, Manoj Patel, Ellalahewage Sathyajith Kumarasinghe, Ajay Kumar Bhargava, Karl-Heinz Thierauch, Hartmut Beck, Susanne Greschat, Peter Ellinghaus, Patrick Paulus, Holger Hess-Stumpp
  • PYRIMIDINE-2-AMINE COMPOUNDS AND THEIR USE AS INHIBITORS OF JAK KINASES
    Publication number: 20140213585
    Abstract: This invention is directed to methods of treating diseases or conditions associated with JAK2 activity in a mammal comprising the administration of a compound of formula (I): where n, m, Y, R1, R2, R3, R4 and R5 are disclosed herein, or a pharmaceutically acceptable salt.
    Type: Application
    Filed: April 2, 2014
    Publication date: July 31, 2014
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Somasekhar Bhamidipati, Jeffrey Clough, Ankush Argade, Rajinder Singh, Vadim Markovtosov, Pingyu Ding, Jiaxin Yu, Andy Atuegbu, Hui Hong, Ihab Darwish, Sambaiah Thota
  • COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR
    Publication number: 20140213554
    Abstract: 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/or mutant c-kit protein kinases.
    Type: Application
    Filed: December 20, 2013
    Publication date: July 31, 2014
    Inventors: Guoxian Wu, Katrina Chan, Todd Ewing, Prabha N. Ibrahim, Jack Lin, Marika Nespi, Wayne Spevak, Ying Zhang
  • 2,4-diaryl-substituted [1,8] naphthyridines as kinase inhibitors for use against cancer
    Patent number: 8791113
    Abstract: The present invention relates to novel [1,8]naphthyridine derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors.
    Type: Grant
    Filed: May 31, 2011
    Date of Patent: July 29, 2014
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Alfred Jonczyk, Guenter Hoelzemann, Christiane Amendt, Frank Zenke
  • QUINAZOLINE DERIVATIVE, PREPARATION METHOD THEREFOR, INTERMEDIATE, COMPOSITION AND APPLICATION THEREOF
    Publication number: 20140206687
    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: Application
    Filed: July 27, 2012
    Publication date: July 24, 2014
    Applicants: ZHEJIANG UNIVERSITY, SHANGHAI PHARMACEUTICALS HOLDING CO., LTD.
    Inventors: Guangxin Xia, Jingkang Shen, Yongping Yu, Wenteng Chen, Chunchun Zhang, Yu Hao, Jing Zhang, Bojun Li, Xuejun Liu
  • AMINO QUINAZOLINES AS KINASE INHIBITORS
    Publication number: 20140206688
    Abstract: Disclosed are compounds having the formula (Formula I)): wherein R1, R2, R3 and Z are as defined herein, and methods of making and using the same.
    Type: Application
    Filed: August 17, 2012
    Publication date: July 24, 2014
    Inventors: Michael Jonathan Bury, Linda N. Casillas, Adam K. Charnley, Michael P. Demartino, Xiaoyang Dong, Patrick M. Eidam, Pamela A. Haile, Robert W. Marquis, JR., Joshi M. Ramanjulu, Joseph J. Romano, Ami Lakdawala Shah, Robert R. Singhaus, JR., Gren Wang
  • PHTHALAZINONES AND ISOQUINOLINONES AS ROCK INHIBITORS
    Publication number: 20140206686
    Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.
    Type: Application
    Filed: January 17, 2014
    Publication date: July 24, 2014
    Inventors: Peter W. Glunz, Yan Zou, Mimi L. Quan
  • Substituted Fused Imidazole Derivatives, Pharmaceutical Compositions, and Methods of Use Thereof
    Publication number: 20140200212
    Abstract: Substituted fused imidazole derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted fused imidazole derivative, and methods of use in treating inflammation are provided. The substituted fused imidazole derivatives may control the activity or the amount or both the activity and the amount of heme-oxygenase.
    Type: Application
    Filed: March 17, 2014
    Publication date: July 17, 2014
    Applicant: High Point Pharmaceuticals, LLC
    Inventors: Adnan M.M. Mjalli, Dharma Rao Polisetti, Jareer Nabeel Kassis, Matthew J. Kostura, Mustafa Guzel, Otis Clinton Attucks, Robert Carl Andrews, Samuel Victory, Suparna Gupta
  • Pyrazole compounds that modulate the activity of CDK, GSK and aurora kinases
    Patent number: 8778936
    Abstract: The invention provides a compound of the formula (I): or a salt, solvate, tautomer or N-oxide thereof, wherein M is selected from a group D1 and a group D2: and R?, E, A and X are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, processes for making the compounds and the use of the compounds in the prophylaxis or treatment of a disease state mediated by a CDK kinase, GSK-3 kinase or Aurora kinase.
    Type: Grant
    Filed: December 19, 2011
    Date of Patent: July 15, 2014
    Assignee: Astex Therapeutics Limited
    Inventors: Valerio Berdini, Maria Grazia Carr, Adrian Liam Gill, Steven Howard, Eva Figueroa Navarro, Gary Trewartha, David Charles Rees, Mladen Vinkovic, Paul Graham Wyatt
  • Benzimidazole boronic acid derivatives as PI3 kinase inhibitors
    Patent number: 8778937
    Abstract: This invention relates to the use of benzimidazole boronic acid derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3? OH kinase family (hereinafter PI3 kinases), suitably, PI3K?, PI3K?, PI3K?, and/or PI3K?. Suitably, the present invention relates to the use of benzimidazole boronic acids in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3K? selective benzimidazole boronic acid compounds for treating cancer.
    Type: Grant
    Filed: November 12, 2012
    Date of Patent: July 15, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Ralph A. Rivero, Rosanna Tedesco, Juan Ignacio Luengo
  • NOVEL BENZIMIDAZOLE DERIVATIVES
    Publication number: 20140193363
    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: January 15, 2014
    Publication date: July 10, 2014
    Applicant: ENANTA PHARMACEUTICALS, INC.
    Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
  • HETEROCYCLIC GLUTAMINASE INHIBITORS
    Publication number: 20140194421
    Abstract: The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treatment using the novel heterocyclic compounds of the invention.
    Type: Application
    Filed: November 15, 2013
    Publication date: July 10, 2014
    Applicant: CALITHERA BIOSCIENCES, INC.
    Inventors: Jim Li, Lijing Chen, Bindu Goyal, Guy Laidig, Timothy Friend Stanton, Eric Brian Sjogren
  • Pyrimidinyl and 1,3,5-triazinyl benzimidazole sulfonamides and their use in cancer therapy
    Patent number: 8772287
    Abstract: Provided herein are pyrimidinyl and 1,3,5-triazinyl benzimidazole sulfonamides, e.g., compounds of Formulae IA, IB, and IC, and their pharmaceutical compositions, preparation, and use as agents or drugs for cancer therapy, either alone or in combination with radiation and/or other anticancer drugs.
    Type: Grant
    Filed: June 10, 2013
    Date of Patent: July 8, 2014
    Assignee: VetDC, Inc.
    Inventors: Gordon William Rewcastle, Swarnalatha Akuratiya Gamage, Jack Urquhart Flanagan, Anna Claire Giddens, Kit Yee Tsang
  • Substituted spiro[cycloalkyl-1,3?-indo]-2?(1?H)-one derivatives and their use as P38 mitogen-activated kinase inhibitors
    Patent number: 8772288
    Abstract: The present disclosure is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I), processes for preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Grant
    Filed: April 3, 2009
    Date of Patent: July 8, 2014
    Assignee: Almirall, S.A.
    Inventors: Paul Robert Eastwood, Jacob Gonzalez Rodriguez, Bernet Vidal Juan, Nuria Aguilar Izquierdo
  • MK2 inhibitors
    Patent number: 8772286
    Abstract: The present invention relates to compounds of general Formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used in the treatment of immune, autoimmune, inflammatory diseases, cardiovascular diseases, infectious diseases, bone resorption disorders, neurodegenerative diseases or proliferative diseases.
    Type: Grant
    Filed: December 13, 2010
    Date of Patent: July 8, 2014
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Tjeerd Andries Barf, Arthur Oubrie, Carsten Schultz-Fademrecht, Eduard Willem Zwart, Niels Hoogenboom, Sander Martijn De Wilde, Allard Kaptein
  • MOLECULAR ACTIVATORS OF THE WNT/BETA-CATENIN PATHWAY
    Publication number: 20140187510
    Abstract: The present invention is directed toward a method of treating a subject for a condition mediated by aberrant Wnt/?-catenin signaling by selecting a subject with a condition mediated by aberrant Wnt/?-catenin signaling and administering to the selected subject a compound selected from the group consisting of those set forth in Table 1, Table 2, and a pharmaceutically acceptable salt thereof. A method of similarly modulating the Wnt/?-catenin pathway in a subject is also discussed.
    Type: Application
    Filed: July 11, 2013
    Publication date: July 3, 2014
    Applicants: THE GENERAL HOSPITAL CORPORATION, MASSACHUSETTS INSTITUTE OF TECHNOLOGY, UNIVERSITY OF WASHINGTON THROUGH ITS CENTER FOR CENTER FOR COMMERCIALIZATION
    Inventors: Randall T. Moon, Travis L. Biechele, Nathan D. Camp, Stephen Haggarty, Daniel Fass
  • 7-AZAINDOLE DERIVATIVES SUITABLE FOR TREATMENT OF CANCERS
    Publication number: 20140187551
    Abstract: Compounds of the formula (I) in which R1, R2 and R3 have the meanings indicated in Claim 1, are inhibitors of PDK1 and cell proliferation/cell vitality and can be employed treatment of tumours.
    Type: Application
    Filed: May 29, 2012
    Publication date: July 3, 2014
    Applicant: MERCK PATENT GMBH
    Inventors: Timo Heinrich, Margarita Wucherer-Plietker, Hans-Peter Buchstaller
  • BICYCLIC ORGANIC COMPOUNDS SUITABLE FOR THE TREATMENT OF INFLAMMATORY OR ALLERGIC CONDITIONS
    Publication number: 20140187550
    Abstract: A compound of formula (I): in free or salt form, wherein R1, R3, Qa, Qb and Q are as defined herein, for the treatment of a disease mediated by the S1P2 or S1P3 receptor, such as inflammatory or obstructive airways disease.
    Type: Application
    Filed: December 16, 2013
    Publication date: July 3, 2014
    Applicant: Novartis AG
    Inventor: Roger John Taylor
  • Compounds
    Patent number: 8765743
    Abstract: The invention is directed to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.
    Type: Grant
    Filed: June 3, 2009
    Date of Patent: July 1, 2014
    Assignee: Glaxosmithkline Intellectual Property Development Limited
    Inventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, Juliet Kay Simpson, Christian Alan Paul Smethurst
  • Indazolyl, benzimidazolyl, benzotriazolyl substituted indolinone derivatives as kinase inhibitors useful in the treatment of cancer
    Patent number: 8765748
    Abstract: The present invention is directed to a compound is represented by Structural Formula (A): or a pharmaceutically acceptable salt thereof. The present invention is also directed to a pharmaceutical composition comprising a compound represented by Structural Formula (A) described above or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or diluent. Also disclosed is a method of treating a subject having cancer, wherein the method comprises administering a therapeutically effective amount of a compound represented by Structural Formula (A) described above or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 19, 2008
    Date of Patent: July 1, 2014
    Assignee: University Health Network
    Inventors: Heinz W. Pauls, Bryan T. Forrest, Radoslaw Laufer, Miklos Feher, Peter Brent Sampson, Guohua Pan, Sze-Wan Li, Yong Liu
  • NOVEL PYRIMIDINE COMPOUNDS AS mTOR AND PI3K INHIBITORS
    Publication number: 20140178360
    Abstract: The present invention relates to pyrimidine compounds of formula (I): which are useful in treating mTOR kinase- or PI3K kinase-related diseases.
    Type: Application
    Filed: February 27, 2014
    Publication date: June 26, 2014
    Applicants: DCB-USA LLC, DEVELOPMENT CENTER FOR BIOTECHNOLOGY
    Inventors: Mann-Yan KUO, Ying-Shuan Lee, Paonien Chen, Li Jung Chen, Yann Yu Lu, Yi-Ting Huang, Hung-Yi Hsu, Ping-Kuei Tsai
  • PHOSPHATIDYLINOSITOL 3-KINASE INHIBITORS
    Publication number: 20140179673
    Abstract: The present disclosure provides phosphatidylinositol 3-kinase (PI3K) inhibitors of formula (I), or pharmaceutically acceptable salts thereof, in which R1, R2, n, R3, R4, R5 and R6 are as defined herein. These compounds are useful for treatment of conditions mediated by one or more PI3K isoforms, such as PI3K?. The present disclosure further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by one or more PI3K isoforms, such as PI3K?.
    Type: Application
    Filed: December 20, 2013
    Publication date: June 26, 2014
    Applicant: GILEAD CALISTOGA LLC
    Inventors: Jerry EVARTS, Leena PATEL, Jennifer A. TREIBERG, Stephane PERREAULT, Arthur YEUNG, Lafe J. PURVIS, II, Musong KIM
  • BICYCLIC HETEROCYCLE COMPOUNDS AND THEIR USES IN THERAPY
    Publication number: 20140179666
    Abstract: The invention relates to bicyclic heterocycle compounds of formula (I): or tautomeric or stereochemically isomeric forms, N-oxides, pharmaceutically acceptable salts or the solvates thereof; wherein R1, R2a, R2b, R3a, R3b, R5, R6, R7, R8, R9, p and E are as defined herein; to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Application
    Filed: April 20, 2012
    Publication date: June 26, 2014
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventors: Alison Jo-Anne Woolford, Steven Howard, Ildiko Maria Buck, Gianni Chessari, Christopher Norbert Johnson, Emiliano Tamanini, James Edward Harvey Day, Elisabetta Chiarparin, Thomas Daniel Heightman, Martyn Frederickson, Charlotte Mary Griffiths-Jones
  • FUSED PYRIMIDINE COMPOUNDS AND USE THEREOF
    Publication number: 20140179668
    Abstract: Fused pyrimidine compounds as kinase inhibitors, such as multi-kinase inhibitors, are provided. Fused pyrimidine compounds as IGF-IR inhibitors are provided. The compounds may be used in a method of treating cancer. Pharmaceutical compositions containing a fused pyrimidine compound and a pharmaceutically acceptable carrier are also provided, as are kits containing a fused pyrimidine compound or salt thereof and instructions for use, e.g., in a method of treating cancer.
    Type: Application
    Filed: December 26, 2013
    Publication date: June 26, 2014
    Applicant: MEDIVATION TECHNOLOGIES, INC.
    Inventors: Sarvajit CHAKRAVARTY, Roopa RAI, Michael John GREEN
  • DISUBSTITUTED OCTAHYDROPYRROLO[3,4-c]PYRROLES AS OREXIN RECEPTOR MODULATORS
    Publication number: 20140179697
    Abstract: Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.
    Type: Application
    Filed: December 23, 2013
    Publication date: June 26, 2014
    Applicant: JANSSEN PHARMACEUTICA NV
    Inventors: Wenying Chai, Michael A. Letavic, Kiev S. Ly, Daniel J. Pippel, Dale A. Rudolph, Kathleen C. Sappey, Brad M. Savall, Chandravadan R. Shah, Brock T. Shireman, Akinola Soyode Johnson, Emily M. Stocking, Devin M. Swanson
  • Benzoimidazoles as prolyl hydroxylase inhibitors
    Patent number: 8759345
    Abstract: The present invention is directed to benzoimidazole compounds of the formula (1) and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.
    Type: Grant
    Filed: April 28, 2009
    Date of Patent: June 24, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Frances Meredith Hocutt, Barry Eastman Leonard, Jr., Hillary M Peltier, Victor K. Phuong, Michael H. Rabinowitz, Mark D Rosen, Kyle T. Tarantino, Hariharan Venkatesan, Lucy Xiumin Zhao
  • ENHANCEMENT OF CELLULAR TRANSPLANTATION USING SMALL MOLECULE MODULATORS HEPATOCYTE GROWTH FACTOR (SCATTER FACTOR) ACTIVITY
    Publication number: 20140171419
    Abstract: The present invention provides methods for enhancing cellular transplantation by exposing cells in vitro or ex vivo, or a recipient of cells, to a small molecule hepatocyte growth factor/scatter factor mimetic. Exemplary compounds are described.
    Type: Application
    Filed: February 21, 2014
    Publication date: June 19, 2014
    Applicant: ANGION BIOMEDICA CORP
    Inventors: Lambertus J.W.M Oehlen, Itzhak D. Goldberg
  • DISUBSTITUTED OCTAHYDROPYRROLO [3,4-C] PYRROLES AS OREXIN RECEPTOR MODULATORS
    Publication number: 20140171430
    Abstract: Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.
    Type: Application
    Filed: April 20, 2012
    Publication date: June 19, 2014
    Applicant: JANSSEN PHARMACEUTICA NV
    Inventors: Michael A. Letavic, Rudolph A. Dale, Brad M. Savall, Brock T. Shireman, Devin Swanson
  • AZOLE HETEROCYCLIC COMPOUND, PREPARATION METHOD, PHARMACEUTICAL COMPOSITION AND USE
    Publication number: 20140171431
    Abstract: The present invention relates to the field of pharmaceutical chemistry, and in particular, to a novel class of azole compounds represented by general formula (I), (II) or (III) and a preparation method thereof, a pharmaceutical composition with the compounds as active components, and a use of the azole compounds and the pharmaceutical composition in the preparation of a medicament for treatment of diseases associated with Lp-PLA2 enzyme activities, wherein each substituent is as defined in the specification.
    Type: Application
    Filed: May 15, 2012
    Publication date: June 19, 2014
    Inventors: Jianhua Shen, Yiping Wang, Kai Wang
  • HISTONE DEMETHYLASE INHIBITORS
    Publication number: 20140171432
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted 3-aminopyridine derivative compounds, substituted 3-aminopyridazine derivative compounds, and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
    Type: Application
    Filed: December 19, 2013
    Publication date: June 19, 2014
    Applicant: Quanticel Pharmaceuticals, Inc.
    Inventors: Toufike Kanouni, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennen Wallace
  • BICYCLIC INHIBITORS OF ALK
    Publication number: 20140171429
    Abstract: The present invention relates to compounds of formula (1) or pharmaceutical acceptable salts, Formula (1) wherein R1, R2, R3, X, Y, Z, A, B, G1, m, and n are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as ALK and methods of treating diseases such as cancer.
    Type: Application
    Filed: January 20, 2012
    Publication date: June 19, 2014
    Applicant: ABBVIE INC.
    Inventors: Anil Vasudevan, Thomas Dale Penning, Huanming Chen, Bo Liang, Shaohui Wang, Zhongqiang Zhao, Dikun Chai, Leifu Yang, Yingxiang Gao, Marina Pliushchev
  • Pyrimidine substituted purine compounds as kinase (S) inhibitors
    Patent number: 8754080
    Abstract: The present invention relates to a purine compound useful as a kinase inhibitor. The compound has the structure (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: April 3, 2009
    Date of Patent: June 17, 2014
    Assignee: Verastem, Inc.
    Inventors: DiZhong Chen, Meredith Williams
  • 8-fluorophthalazin-1(2H)-one compounds
    Patent number: 8754077
    Abstract: 8-Fluorophthalazin-1(2h)-one compounds of Formula I 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 I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Grant
    Filed: January 13, 2014
    Date of Patent: June 17, 2014
    Assignee: F. Hoffmann-La Roche AG
    Inventors: James J. Crawford, Daniel F. Ortwine, BinQing Wei, Wendy B. Young
  • INHIBITION OF ACTIVATED CDC42-ASSOCIATED KINASE 1
    Publication number: 20140163028
    Abstract: Compounds, compositions, and methods for specific inhibition of activated cdc42-associated kinase 1 (Ack1) are provided.
    Type: Application
    Filed: January 24, 2014
    Publication date: June 12, 2014
    Applicant: Institute for Cancer Research d/b/a The Research Institute of Fox Chase Cancer Center
    Inventors: Jeffrey R. Peterson, Haiching Ma, Sean Deacon
  • BROMODOMAIN INHIBITORS
    Publication number: 20140162971
    Abstract: The present invention provides for compounds of formula (I) wherein A1, A2, A3, A4, X1, X2, Y1, L1, G1, Rx, and Ry have any of the values defined thereof in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).
    Type: Application
    Filed: March 14, 2013
    Publication date: June 12, 2014
    Inventors: Le WANG, John K PRATT, Keith F. McDANIEL, Yujia DAI, Steven D FIDANZE, Lisa HASVOLD, John H. Holms, Warren M. KATI, Dachun LIU, Robert A Mantei, William J. McCLELLAN, George S. SHEPPARD, Carol K. Wada
  • C-Met Modulators and Method of Use
    Publication number: 20140155396
    Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.
    Type: Application
    Filed: June 27, 2013
    Publication date: June 5, 2014
    Inventors: Lynne Canne Bannen, Diva Sze-Ming Chan, Jeff Chen, Lisa Esther Dalrymple, Timothy Patrick Forsyth, Tai Phat Huynh, Vasu Jammalamadaka, Richard George Khoury, James William Leahy, Morrison B. Mac, Grace Mann, Larry W. Mann, John M. Nuss, Jason Jevious Parks, Craig Stacy Takeuchi, Yong Wang, Wei Xu
  • BRAF Mutations Conferring Resistance to BRAF Inhibitors
    Publication number: 20140155399
    Abstract: The present invention relates to methods, compositions and kits concerning resistance to treatment with an anti-cancer agent, specifically an inhibitor of BRAF. In particular embodiments, the invention concerns mutations in a BRAF sequence that confer resistance to a BRAF inhibitor. Identification of such mutations in a BRAF sequence allows the identification and design of second-generation BRAF inhibitors. Methods and kits for detecting the presence of a mutant BRAF sequence in a sample are also provided.
    Type: Application
    Filed: December 4, 2013
    Publication date: June 5, 2014
    Applicant: DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Levi Garraway, Caroline Emery
  • NOVEL COMPOUNDS
    Publication number: 20140155375
    Abstract: The present invention relates to novel NADPH oxidase II inhibitors and their use in the treatment of diseases mediated by the NADPH oxidase enzymes.
    Type: Application
    Filed: June 8, 2012
    Publication date: June 5, 2014
    Applicant: GlaxoSmithKline Interllectual Property Limited
    Inventors: Deborah W. Chen, Sarah Duncan, Nigel Paul King, Kiew Ching Lee, Sing Yeung Mak, Dean Andrew Rivers
  • HETEROCYCLIC COMPOUNDS AS PROTEIN KINASE INHIBITORS
    Publication number: 20140155398
    Abstract: The present invention provides a heterocyclic compound of formula (I), a pharmaceutically acceptable salt thereof, a prodrug thereof or a hydrate thereof, wherein A, A? B, D, R1, R2 and R3 are as defined herein, a pharmaceutical composition comprising a compound of formula (I) as an active ingredient, methods of production, and methods of use thereof. Particularly, the present invention provides a compound of formula (I) useful for treating or preventing a disease, condition or disorder associated with protein kinases, preferably Janus Kinase family.
    Type: Application
    Filed: November 22, 2013
    Publication date: June 5, 2014
    Applicant: Daiichi Sankyo Company, Limited
    Inventors: Ashwani Kumar Verma, Kumaragurubaran Nagaswamy, Lalima Sharma, Soma Ghosh, Balkrishna Ramchandra Kale, Aniruddha Mondal, Punit Kumar Srivastava, Sunanda Ghosh Dastidar, Rijwan Jaffer Momin, Pradip Balu Wagh, Sonali Nanasaheb Pansare, Pramod Raosaheb Markad, Yogesh Balasaheb Khairnar, Rie Miyauchi, Takeshi Murata, Masayuki Ishizaki, Masatoshi Nagamochi, Shin Iimura
  • EMT SIGNATURES AND PREDICTIVE MARKERS AND METHOD OF USING THE SAME
    Publication number: 20140155397
    Abstract: EMT signatures and markers useful for characterizing the status of epithelial cancers and for predicting drug responses in patients having non-small cell lung cancer are provided together with methods of using the same.
    Type: Application
    Filed: April 2, 2012
    Publication date: June 5, 2014
    Applicant: Board of Regents
    Inventors: John V Heymach, Jing Wang, Lauren Averett Byers, Kevin R. Coombes, John D. Minna, Luc Girard
  • Glucocorticoid mimetics, methods of making them, pharmaceutical compositions and uses thereof
    Patent number: 8741897
    Abstract: Compounds of Formula (IA), (IB), (IC), and (ID) wherein R1, R2, R3, R4, R5, and R6 are as respectively defined herein for Formula (IA), (IB), (IC), and (ID), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
    Type: Grant
    Filed: September 22, 2004
    Date of Patent: June 3, 2014
    Assignee: Boehringer Ingelheim Pharmaceuticals Inc.
    Inventors: Younes Bekkali, Rajashekhar Betageri, Michel J. Emmanuel, Abdelhakim Hammach, Christian Hanke Justus Joachim Harcken, Thomas Martin Kirrane, Jr., Daniel Kuzmich, Thomas Wai-Ho Lee, Pingrong Liu, Usha R. Patel, John Robert Proudfoot, Hossein Razavi, Doris Riether, Hidenori Takahashi, David S. Thomson, Ji Wang, Renee Zindell
  • Inhibitors of Bruton's tyrosine kinase
    Patent number: 8742098
    Abstract: This application discloses compounds according to generic Formula I: wherein the variables are defined as described herein, and which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation, such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.
    Type: Grant
    Filed: December 6, 2012
    Date of Patent: June 3, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Christine E. Brotherton-Pleiss, Francisco Javier Lopez-Tapia, Yan Lou
  • Polymorphs and salts
    Patent number: 8735390
    Abstract: The present invention is directed to novel polymorphs and salts of a compound which is an inhibitor of kinase activity.
    Type: Grant
    Filed: September 6, 2011
    Date of Patent: May 27, 2014
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Julie Nicole Hamblin, Paul Spencer Jones, Suzanne Elaine Keeling, Joelle Le, Charlotte Jane Mitchell, Nigel James Parr, Robert David Willacy
  • CORRELATION OF MOLECULAR MARKERS WITH CLINICAL OUTCOME IN GBM PATIENTS RADIATION TREATED WITH OR WITHOUT GEFITINIB
    Publication number: 20140142101
    Abstract: Interestingly, for prognosis, the significant biomarkers for Gefitinib-treated GBM patients (RTOG 0211) appeared to differ compared to historical, RT and non-Gefitinib-treated GBM patients. In Gefitinib-treated patients, those with higher levels of nuclear pAKT driven by PTEN loss, higher levels of nuclear pMAPK, and lower levels of nuclear pmTOR had significantly worse clinical outcomes. In contrast, in non-Gefitinib-treated patients, patients with PTEN-deficiency, and higher levels of EGFRvIII, total EGFR, IGFR1, NFkB and lower levels of nuclear Survivin appeared to have adverse clinical outcomes, highlighting the treatment-dependency of these biomarkers.
    Type: Application
    Filed: October 14, 2013
    Publication date: May 22, 2014
    Applicants: Radiation Therapy Oncology Group of the Americal College of Radiology, HistoRx, Inc.
    Inventors: Arnab CHAKRAVARTI, Robert Pinard, Donald Waldron, Agnes Ang, Marisa P. Dolled-Filhart, Annette Molinaro
  • BIARYL DERIVATIVES AS BROMODOMAIN INHIBITORS
    Publication number: 20140140956
    Abstract: The present disclosure relates to compounds, which are useful for inhibition of BET protein function by binding to bromodomains, and their use in therapy.
    Type: Application
    Filed: November 20, 2013
    Publication date: May 22, 2014
    Applicant: RVX Therapeutics Inc.
    Inventors: David John Fairfax, Gregory Scott Martin, John Frederick Quinn, Bryan Cordell Duffy, Gregory Steven Wagner, Peter Ronald Young
  • CYCLIC AMINES AS BROMODOMAIN INHIBITORS
    Publication number: 20140142102
    Abstract: The present disclosure relates to compounds, which are useful for inhibition of BET protein function by binding to bromodomains, and their use in therapy.
    Type: Application
    Filed: November 20, 2013
    Publication date: May 22, 2014
    Applicant: RVX Therapeutics Inc.
    Inventors: David John Fairfax, Bryan Cordell Duffy, Gregory Scott Martin, John Frederick Quinn, Shuang Liu, Gregory Steven Wagner, Peter Ronald Young
  • COMBINATION THERAPY WITH MDM2 AND EFGR INHIBITORS
    Publication number: 20140134163
    Abstract: 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: Application
    Filed: January 16, 2014
    Publication date: May 15, 2014
    Inventor: Joseph P. Errico