Ring Nitrogen In The Bicyclo Ring System Patents (Class 514/235.2)
  • 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
  • c-Met Modulators and Method of Use
    Publication number: 20140155378
    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: May 7, 2013
    Publication date: June 5, 2014
    Applicant: Exelixis, Inc.
    Inventors: Lynne Canne Bannen, Diva Sze-ming Chan, Jeff Chen, Timothy Patrick Forsyth, Tai Phat Huynh, Vasu Jammalamadaka, Richard George Khoury, James William Leahy, Morrison B. Mac, 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
  • MORPHOLINO COMPOUNDS, USES AND METHODS
    Publication number: 20140148452
    Abstract: The invention relates to morpholino-derivatives according to Formula (I) or stereoisomers or pharmaceutically acceptable salts or solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, m and n are as defined in the specification. The compounds are antagonists, reverse agonists or agonists of G-protein coupled receptors, such as dopamine D4 and 5HT1a. The inventions also relates to pharmaceutical compositions comprising the compounds and methods involving the compounds and compositions. The compounds and compositions of the invention may in particular be used in the treatment of diseases and disorders, such as neurological and neurodegenerative diseases; or as lead compounds for the design and selection of further therapeutic compounds.
    Type: Application
    Filed: November 20, 2013
    Publication date: May 29, 2014
    Applicant: University of Dundee
    Inventors: Jeremy Besnard, Andrew Lee Hopkins, Ian Gilbert, Gian Filippo Ruda, Keren Abecassis
  • Synthesis of functionalized octahydro-isoquinolin-1-one-8-carboxamides, octahydro-isoquinolin-1-one-8-carboxylic esters and analogs, and therapeutic methods
    Patent number: 8735391
    Abstract: A functionalized polycyclic compound can have a structure of Formula 1 or salt, prodrug, analog, or derivative thereof, which compound can be prepared by providing a diene; reacting the diene with a dienophile under sufficient conditions for a combined Diels-Alder/acylation reaction so as to provide a polycyclic compound having a carboxylic acid; and coupling the carboxylic acid with an amine-containing compound or a hydroxyl-containing compound so as to form an amide or an ester and producing a compound having a structure of Formula 1. The compound can be used for modulating an opioid receptor, which can be conducted by administering to an opioid receptor a functionalized polycyclic compound as described herein in an effective amount to modulate the functionality of the opioid receptor. Such opioid modulation can provide a biological benefit to a subject.
    Type: Grant
    Filed: September 25, 2009
    Date of Patent: May 27, 2014
    Assignee: University of Kansas
    Inventors: Jeffrey Aube, Bryan L. Roth, Partha Ghosh, Kevin J. Frankowski
  • COMPOUNDS FOR THE TREATMENT OF HIV
    Publication number: 20140142085
    Abstract: The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides 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: July 5, 2012
    Publication date: May 22, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Steven S. Bondy, Carina E. Cannizzaro, Chien-hung Chou, Randall L. Halcomb, Yunfeng Eric Hu, John O. Link, Qi Liu, Scott D. Schroeder, Winston C. Tse, Jennifer R. Zhang
  • Secondary 8-hydroxyquinoline-7-carboxamide derivatives
    Patent number: 8729076
    Abstract: The present invention provides new secondary 8-hydroxyquinoline-7-carboxamide derivatives of general formula (I) and pharmaceutically acceptable salts thereof. These compounds are useful as antifungal agents. Specifically, these compounds were tested against Tricophyton Rubrum, Tricophyton Mentagrophytes, Aspergillus Niger and Scopulariopsis Brevicaulis. Many of these compounds are active against Candida species such as Candida Albicans and Candida Glabrata.
    Type: Grant
    Filed: December 28, 2010
    Date of Patent: May 20, 2014
    Assignee: Polichem SA
    Inventors: Stefania Gagliardi, Simone Del Sordo, Federico Mailland, Michela Legora
  • METHOD OF TREATMENT OF AGGRESSION
    Publication number: 20140135326
    Abstract: The current invention offers a method of treatment of aggression in a human subject suffering from ADHD, comprising: (a) determining the weight of the human subject; (b) calculating a dose of molindone such to achieve a plasma concentration, based on body weight, that does not saturate the molindone receptors; (c) administering the dose of step (b) to the mammalian subject.
    Type: Application
    Filed: November 13, 2013
    Publication date: May 15, 2014
    Applicant: Supernus Pharmaceuticals, Inc.
    Inventor: Adam Kenneth Hamm
  • NOVEL BENZYLAMINE DERIVATIVES AND THEIR UTILITY AS CHOLESTEROL ESTER-TRANSFER PROTEIN INHIBITORS
    Publication number: 20140134235
    Abstract: The present invention provides, among other things, new benzylamine compounds, compositions comprising benzylamine compounds, methods of making benzylamine compounds, and methods of using benzylamine compounds for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism.
    Type: Application
    Filed: October 14, 2013
    Publication date: May 15, 2014
    Applicant: DR. REDDY'S LABORATORIES LTD.
    Inventors: Anima BARUAH, Dibyendu DE, Ish Kumar KHANNA, Sivaram PILLARISETTI, Santanu MAITRA, Christopher W. ALEXANDER, Jennepalli SREENU, Indu Dagar, Shanavas Alikunju
  • N- (2 -AMINOPHENYL) BENZAMIDE DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS
    Publication number: 20140135327
    Abstract: This invention relates to the discovery of novel compounds, or pharmaceutically acceptable salts thereof, which possess HDAC inhibitory activity. In particular, the compounds of the invention demonstrate selectivity towards Class I HDAC enzymes, and are accordingly expected to be useful for their anti-proliferative activity and in methods of treatment of the human or animal body, for example in preventing or inhibiting tumour growth and metastasis in cancers. The invention also relates to processes for the manufacture of the compounds defined herein, or pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an anti-proliferative effect in a warm-blooded animal such as man.
    Type: Application
    Filed: July 6, 2012
    Publication date: May 15, 2014
    Applicant: CANCER RESEARCH TECHNOLOGY LIMITED
    Inventors: Ronald Ernest Grigg, Martyn Inman, Graham Packham
  • SUBSTITUTED SULFONAMIDES USEFUL AS ANTIAPOPTOTIC BCL INHIBITORS
    Publication number: 20140135318
    Abstract: Disclosed are compounds of Formula (I), or a pharmaceutically acceptable salt thereof, wherein: W and Q and G are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bcl-2 family antiapoptotic proteins for the treatment of cancer; and pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: May 23, 2012
    Publication date: May 15, 2014
    Applicant: Bristol-Myers Squibb Company
    Inventors: Robert M. Borzilleri, Zhen-Wei Cai, Andrew J. Tebben, Heidi L. Perez, Liping Zhang, Gretchen M. Schroeder, Donna D. Wei
  • NOVEL EZRIN INHIBITORS AND METHODS OF MAKING AND USING
    Publication number: 20140135325
    Abstract: The invention encompasses compound and pharmaceutical composition comprising the compound of the following Formula (I): or pharmaceutically acceptable salts or prodrugs thereof, that are useful for inhibiting ezrin protein in a cell or for inhibiting the growth of a cancer cell.
    Type: Application
    Filed: October 7, 2013
    Publication date: May 15, 2014
    Applicant: GEORGETOWN UNIVERSITY
    Inventors: Milton L. Brown, Mikell Paige, Jeffrey A. Torestsky, Aykut Uren, George Kosturko, Gullay Bulut
  • Isoquinoline derivatives
    Patent number: 8722671
    Abstract: The invention relates to 6-piperidinyl-substituted isoquinoline derivatives of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.
    Type: Grant
    Filed: June 15, 2011
    Date of Patent: May 13, 2014
    Assignee: Sanofi
    Inventors: Oliver Plettenburg, Armin Hofmeister, Dieter Kadereit, Stefan Peukert, Sven Ruf, Kurt Ritter, Matthias Loehn, Yuri Ivashchenko, Peter Monecke, Matthias Dreyer, Aimo Kannt
  • SELECTIVE HDAC1 AND HDAC2 INHIBITORS
    Publication number: 20140128391
    Abstract: 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: Application
    Filed: November 1, 2013
    Publication date: May 8, 2014
    Inventors: John H. van Duzer, Ralph Mazitschek
  • DISPIROPYRROLIDINE DERIVATIVES
    Publication number: 20140121196
    Abstract: A compound that inhibits interaction between, murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity is provided. The present invention provides a dispiropyrrolidine derivative represented by the following formula (1), which has various substituents, inhibits interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity, wherein R1, R2, R3, ring A, and ring B in formula (1) respectively have the same meanings as defined in the specification.
    Type: Application
    Filed: November 14, 2013
    Publication date: May 1, 2014
    Applicant: Daiichi Sankyo Company, Limited
    Inventors: Yuuichi Sugimoto, Kouichi Uoto, Takanori Wakabayashi, Masaki Miyazaki, Masaki Setoguchi, Toru Taniguchi, Keisuke Yoshida, Akitake Yamaguchi, Shoko Yoshida
  • QUINOLONE COMPOUND AND PHARMACEUTICAL COMPOSITION
    Publication number: 20140121207
    Abstract: The present invention provides a quinolone compound represented by General Formula (1) or a salt thereof, wherein R1 represents a hydrogen atom, etc.; R2 represents a hydrogen atom, etc.; R3 represents a phenyl group optionally being substituted with one or more substituents, etc.; R4 represents a halogen atom; R5 represents a hydrogen atom or halogen atom; R6 represents a hydrogen atom; and R7 represents a hydroxyl group, etc. The quinolone compound have a functional improvement effect, which suppresses progression of neurological dysfunction by inhibiting the chronic progression of Parkinson's disease or protecting dopamine neurons from the disease etiology, thereby prolonging the period before first administration begins.
    Type: Application
    Filed: January 3, 2014
    Publication date: May 1, 2014
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Kenji OTSUBO, Yuji OCHI, Masami NAKAI, Atsushi MORI
  • NEW 4-AMINO-4-OXOBUTANOYL PEPTIDES AS INHIBITORS OF VIRAL REPLICATION
    Publication number: 20140113890
    Abstract: The invention provides 4-amino-4-oxobutanoyl peptides of Formula I and the pharmaceutically salts and hydrates thereof. The variables R, R1, R6-R8, R16, R18, R19, M, n, T, Y, and Z are defined herein. Certain compounds of Formula I are useful as antiviral agents. The 4-amino-4-oxobutanoyl peptides disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more 4-amino-4-oxobutanoyl peptides and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain a 4-amino-4-oxobutanoyl peptides as the only active agent or may contain a combination of a 4-amino-4-oxobutanoyl peptides and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections.
    Type: Application
    Filed: December 23, 2013
    Publication date: April 24, 2014
    Applicant: ACHILLION PHARMACEUTICALS, INC.
    Inventors: Avinash Phadke, Dawei Chen, Venkat Gadhachanda, Akihiro Hashimoto, Godwin Pais, Xiangzhu Wang, Atul Agarwal, Ha Young Kim, Shuoming Li, Cuixian Liu, Suoming Zhang, Milind Deshpande
  • HETEROARYL LINKED QUINOLINYL MODULATORS OF RORyt
    Publication number: 20140107097
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Application
    Filed: October 15, 2013
    Publication date: April 17, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Anne Fourie, Xiaohua Xue, Taraneh Mirzadegan, Kelly Ganamet
  • OLOPATADINE COMPOSITIONS AND USES THEREOF
    Publication number: 20140107121
    Abstract: The invention provides solution compositions comprising olopatadine and a PDE4 inhibitor compound of Formula I: The invention also provides methods for treating allergic and inflammatory diseases. More particularly, the present invention relates to formulations of olopatadine and their use for treating and/or preventing allergic or inflammatory disorders of the eye, nose, skin, and ear.
    Type: Application
    Filed: December 17, 2013
    Publication date: April 17, 2014
    Applicant: Alcon Research, Ltd.
    Inventors: L. Wayne Schneider, Wesley Wehsin Han, Masood A. Chowhan
  • BCL-2-SELECTIVE APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE DISEASES
    Publication number: 20140107119
    Abstract: 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: Application
    Filed: November 15, 2013
    Publication date: April 17, 2014
    Applicant: 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
  • METHODS FOR PREDICTING AND IMPROVING THE SURVIVAL OF GASTRIC CANCER PATIENTS
    Publication number: 20140099300
    Abstract: The present invention provides assays and methods for predicting the post-operative survival of a subject having an early stage gastric cancer after tumor surgery. The present invention also provides methods for treating a subject having an early stage gastric cancer by administering a combination therapy tailored to the signal transduction biomarkers that are activated in the cancer. In particular embodiments, the methods of the invention rely on the detection of the activation state or level of a specific combination of signal transducer analytes in a cancer cell obtained from the subject. Thus, the methods of the invention are particularly useful for predicting the survival or prognosis of a subject having an early stage gastric cancer and for guiding both pre- and post-operative treatment decisions by identifying subjects who would benefit from combination therapy as opposed to monotherapy.
    Type: Application
    Filed: October 2, 2013
    Publication date: April 10, 2014
    Applicant: NESTEC S.A.
    Inventors: Phillip Kim, Sharat Singh
  • HETEROCYCLIC COMPOUNDS AND USES THEREOF
    Publication number: 20140100214
    Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein.
    Type: Application
    Filed: December 6, 2013
    Publication date: April 10, 2014
    Applicant: Infinity Pharmaceuticals, Inc.
    Inventors: Alfredo C. CASTRO, Catherine A. Evans, Somarajannair Janardanannair, Andre Lescarbeau, Tao Liu, Daniel A. Snyder, Martin R. Tremblay, Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan
  • Substituted oxindole derivatives, drugs containing said derivatives and the use thereof
    Patent number: 8691815
    Abstract: The invention relates to novel oxindol derivative of general formula (I), wherein substituents R1, R2, A, B and Y are such as defined in a claim 1. Drugs containing said derivatives and the use thereof for preventing and/or treating vassopress-and/or oxytocin-dependent-diseases are also disclosed.
    Type: Grant
    Filed: July 30, 2010
    Date of Patent: April 8, 2014
    Assignee: AbbVie Deutschland GmbH & Co. KG
    Inventors: Thorsten Oost, Wilfried Lubisch, Wilfried Hornberger, Liliane Unger, Andrea Hager-Wernet
  • FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS
    Publication number: 20140094460
    Abstract: The present invention relates to sodium channel inhibitors of Formula I: in which R1, R2, R3, R4, R5, R6, and R7 are as defined above, and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes.
    Type: Application
    Filed: December 10, 2013
    Publication date: April 3, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Matthew Abelman, Nancy Chu, Robert H. Jiang, Kwan Leung, Jeff Zablocki
  • Carboline carboxamide compounds useful as kinase inhibitors
    Patent number: 8685969
    Abstract: Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof, formula (I) are useful as kinase modulators, including Btk modulation.
    Type: Grant
    Filed: June 16, 2011
    Date of Patent: April 1, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Chunjian Liu, James Lin, George V. DeLucca, Douglas G. Batt, Qingjie Liu
  • Quinolines and related analogs as sirtuin modulators
    Patent number: 8685970
    Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
    Type: Grant
    Filed: April 30, 2009
    Date of Patent: April 1, 2014
    Assignee: GlaxoSmithKline, LLC
    Inventors: Chi B. Vu, Jeremy S. Disch, Stephanic K. Springer, Charles A. Blum, Robert B. Perni
  • Cyclic compound having hetero atom
    Patent number: 8685981
    Abstract: Compounds exhibiting an osteogenesis-promoting action having the general formula (I) or a pharmacologically acceptable salt thereof: wherein A is selected from among a 3- to 10-membered heterocyclyl group, B is selected from among an amino group, and X is selected from N and CH.
    Type: Grant
    Filed: July 14, 2011
    Date of Patent: April 1, 2014
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Osamu Kanno, Katsuyoshi Nakajima, Kazumasa Aoki, Ryoichi Tanaka, Shimpei Hirano, Kiyoshi Oizumi, Daigo Asano
  • Quinolinyloxyphenylsulfonamides
    Patent number: 8685971
    Abstract: The present invention relates to quinolinyloxyphenylsulfonamides and stereoisomeric forms, solvates, hydrates and/or pharmaceutically acceptable salts of these quinolinyloxyphenylsulfonamide compounds as well as pharmaceutical compositions containing at least one of these compounds together with at least one pharmaceutically acceptable carrier, excipient and/or diluent. Said quinolinyloxyphenylsulfonamides are useful for prophylaxsis, treatment and/or after-treatment of hyperproliferative disorders, such as cancer, tumors and particularly cancer metastases.
    Type: Grant
    Filed: October 16, 2010
    Date of Patent: April 1, 2014
    Assignee: Max-Planck-Gesellschaft zur Forderung der Wissenschaften E.V.
    Inventors: Axel Ullrich, Robert Torka, Yixiang Zhang, György Kéri, László Örfi, István Szabadkai
  • Method of treating cancer with substituted amide derivatives
    Patent number: 8685983
    Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Grant
    Filed: November 30, 2011
    Date of Patent: April 1, 2014
    Assignee: Amgen Inc.
    Inventors: Tae-Seong Kim, David Bauer, Steven Bellon, Alessadro Boezio, Shon Booker, Deborah Choquette, Derin C. D'Amico, Noel D'Angelo, Celia Dominguez, Ingrid M. Fellows, Julie Germain, Russell Graceffa, Jean-Christophe Harmange, Satoko Hirai, Daniel La, Matthew Lee, Longbin Liu, Mark H. Norman, Michele Potashman, Philip Roveto, Aaron C. Siegmund, Ning Xi, Kevin Yang
  • Heterocyclic compounds and their uses
    Patent number: 8686137
    Abstract: Compounds having the structure which are selective inhibitors of P13K (phosphatidylinositol 3-kinase-delta), for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions.
    Type: Grant
    Filed: June 30, 2011
    Date of Patent: April 1, 2014
    Assignee: Amgen Inc.
    Inventor: Paul John Dransfield
  • SUBSTITUTED 6,6-FUSED NITROGENOUS HETEROCYCLIC COMPOUNDS AND USES THEREOF
    Publication number: 20140088076
    Abstract: The invention provides novel compounds having the general formula: wherein X1 is N or N+O?, and one of X2, X3 and X4 is N or N+—O? and the remainder of X2, X3 and X4 is C. R2, R3, R4, R5, R6. A, B and Y are as described herein. Additionally compositions compounds of Formula I and methods of use are further described herein.
    Type: Application
    Filed: October 31, 2013
    Publication date: March 27, 2014
    Applicant: Genentech, Inc.
    Inventors: Joseph P. Lyssikatos, Lewis J. Gazzard, Emily Hanan, Samuel S. Kintz, Hans Edward Purkey
  • NOVEL SMALL-MOLECULES AS THERAPEUTICS
    Publication number: 20140088104
    Abstract: The present invention provides compounds of formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful in treating central nervous system disorders, such as anxiety disorders or depression.
    Type: Application
    Filed: March 2, 2012
    Publication date: March 27, 2014
    Applicant: Bionomics Limited
    Inventors: Bernard Luke Flynn, Dharam Paul, Andrew John Harvey, Damian Wojciech, Sue O'Connor, Jonathan Bayldon Baell, Brad Sleebs, Ian Phillip Street
  • NOVEL PYRAZOLE DERIVATIVE
    Publication number: 20140088029
    Abstract: Provided is a novel therapeutic means for Alzheimer's disease. In particular, provided is a compound represented by the following general formula (I): [wherein Ar1 represents 2-methoxy-4-(2-pyridylmethoxy)phenyl etc. and Ar2 represents a 1H-indol-6-yl group etc.] or a salt thereof.
    Type: Application
    Filed: April 11, 2012
    Publication date: March 27, 2014
    Applicant: PHARMA EIGHT CO., LTD.
    Inventors: Hachiro Sugimoto, Michiaki Okuda, Takashi Takahashi, Ichiro Hijikuro, Hidetaka Suzuki, Shinichi Nakayama
  • Heterocycle compounds and uses thereof for the prevention or treatment of diseases involving formation of amyloid plaques and/or where a dysfunction of the APP metabolism occurs
    Patent number: 8680095
    Abstract: The present invention relates to compounds having the following Formula (I) for use in the prevention and/or the treatment of diseases involving formation of amyloid plaques and/or where a dysfunction of the APP metabolism occurs.
    Type: Grant
    Filed: December 16, 2010
    Date of Patent: March 25, 2014
    Assignees: Institut National de la Sante et de la Recherche Medicale (INSERM), Universite Lille 2 Droit et Sante, Centre National de la Recherche Scientifique (C.N.R.S.), Universite Lille 1—Sciences et Technologies
    Inventors: Andre Delacourte, Patricia Melnyk, Stephane Burlet, Nicolas Lefur
  • COMPOUNDS USEFUL FOR TREATING CANCER
    Publication number: 20140080831
    Abstract: A method of preventing, inhibiting, or treating cancer that includes contacting a cell with at least one compound of formula (Ia) or a pharmaceutically acceptable salt thereof: where: R independently represents a hydrogen atom, a halogen atom, a (C1-C3)alkyl group, a —CN group, a hydroxyl group, a —COOR1 group, a (C1-C3)fluoroalkyl group, a —NO2 group, a —NR1R2 group, or a (C1-C3)alkoxy group; R? is a hydrogen atom, a halogen atom, a (C1-C3)alkyl group, a —NO2 group, a (C1-C3)alkoxy group, or a —NR1R2 group; and R1 and R2 are a hydrogen atom or a (C1-C3)alkyl group.
    Type: Application
    Filed: November 22, 2013
    Publication date: March 20, 2014
    Applicants: CENTRE NATIONALE DE RECHERCHE SCIENTIFIQUE, UNIVERSITE MONTPELLIER 2, SOCIETE SPLICOS, INSTITUT CURIE
    Inventors: Pierre ROUX, Florence MAHUTEAU, Romain NAJMAN, Jamal TAZI, Gilles GADEA, Didier SCHERRER, Carsten BROCK, Nathalie CAHUZAC
  • Indole compounds and methods for treating visceral pain
    Patent number: 8673909
    Abstract: The invention features methods of treating visceral pain or a condition in a mammal caused by the action of nitric oxide synthase (NOS) or by the action of serotonin 5HT1D/1B receptors, by administering to a patient in need thereof a therapeutically effective amount of an indole compound of Formula (I), or a pharmaceutically acceptable salt or prodrug thereof. The methods of the invention may further comprise the administration of additional therapeutic agent. The invention also features new compounds of Formula (I), pharmaceutical compositions thereof, and methods of resolving enantiomeric mixtures.
    Type: Grant
    Filed: November 17, 2008
    Date of Patent: March 18, 2014
    Assignee: NeurAxon, Inc.
    Inventors: Shawn Maddaford, Jailall Ramnauth, Suman Rakhit, Joanne Patman, Paul Renton, Subhash C. Annedi, John S. Andrews, Gabriela Mladenova
  • ANTIVIRAL AND ANTIMICROBIAL COMPOUNDS
    Publication number: 20140073631
    Abstract: Disclosed are guanidine and biguanidine derivatives which have anti-viral and antibacterial activity. Also disclosed are pharmaceutical compositions containing such compounds as an active ingredient, and anti-viral and anti-bacterial methods utilizing such compounds. Methods of treating infections using the guanidine and biguanidine derivatives are also disclosed.
    Type: Application
    Filed: September 10, 2013
    Publication date: March 13, 2014
    Applicant: Vymed Corporation
    Inventor: B. Vithal SHETTY
  • Method of Treating Cancer
    Publication number: 20140066444
    Abstract: This invention is directed to the treatment of cancer, particularly castration-resistant prostate cancer and osteoblastic bone metastases, with a dual inhibitor of MET and VEGF.
    Type: Application
    Filed: September 26, 2011
    Publication date: March 6, 2014
    Applicant: Exelixis, Inc.
    Inventors: David C. Smith, Maha Hussain
  • Pharmaceutical compounds
    Patent number: 8664218
    Abstract: The invention provides a compound of the formula (1): or a salt, solvate, N-oxide or tautomer thereof.
    Type: Grant
    Filed: January 30, 2013
    Date of Patent: March 4, 2014
    Assignee: Astex Therapeutics Ltd.
    Inventors: Brian John Williams, Martyn Frederickson
  • Method of Treating Cancer
    Publication number: 20140057908
    Abstract: This invention is directed to the treatment of cancer, particularly castration-resistant prostate cancer and osteoblastic bone metastases, with a dual inhibitor of MET and VEGF.
    Type: Application
    Filed: September 26, 2011
    Publication date: February 27, 2014
    Applicant: Exelixis, Inc.
    Inventors: David C. Smith, Maha Hussain
  • Pharmaceutical composition, use of 2-iminopyrrolidine derivative for production of pharmaceutical composition, and kit for treatment or amelioration of heart diseases
    Patent number: 8658620
    Abstract: One embodiment of the present invention is a pharmaceutical composition comprising at least one specific 2-iminopyrrolidine derivative and at least one other compound (B). Another embodiment of the present invention is a pharmaceutical composition comprising at least one specific 2-iminopyrrolidine derivative, which is to be used in combination with at least one other compound (B). According to the present invention, there are provided pharmaceutical compositions capable of treating or ameliorating diseases, such as heart diseases, effectively.
    Type: Grant
    Filed: January 9, 2009
    Date of Patent: February 25, 2014
    Assignee: Eisai R&D Management Co., Ltd.
    Inventor: Motoji Kogushi
  • TRPV4 antagonists
    Patent number: 8658636
    Abstract: The present invention relates to quinoline analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.
    Type: Grant
    Filed: March 23, 2011
    Date of Patent: February 25, 2014
    Assignee: GlaxoSmithKline, LLC
    Inventors: Carl A. Brooks, Mui Cheung, Hilary S. Eidam, Ryan M. Fox, Mark A. Hilfiker, Eric S. Manas, Guosen Ye
  • 7-SUBSTITUTED INDOLE MCL-1 INHIBITORS
    Publication number: 20140051683
    Abstract: Compounds which inhibit the activity of anti-apoptotic Mcl-1 protein, compositions containing the compounds, and methods of treating diseases involving overexpressed or unregulated Mcl-1 protein are disclosed.
    Type: Application
    Filed: April 23, 2013
    Publication date: February 20, 2014
    Applicant: AbbVie Inc.
    Inventors: Xilu WANG, Xiaohong Song, Steven W. Elmore, Milan Bruncko, David J. Madar, Andrew J. Souers, Lisa A. Hasvold, Le Wang, Zhi-Fu Tao, Aaron R. Kunzer
  • SUBSTITUTED INDOLE COMPOUNDS HAVING NOS INHIBITORY ACTIVITY
    Publication number: 20140051687
    Abstract: The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing conditions such as, for example, stroke, reperfusion injury, neurodegeneration, head trauma, CABG, migraine headache with and without aura, migraine with allodynia, central post-stroke pain (CPSP), neuropathic pain, morphine/opioid induced tolerance and hyperalgesia.
    Type: Application
    Filed: October 21, 2013
    Publication date: February 20, 2014
    Applicant: NeurAxon, Inc.
    Inventors: Shawn Maddaford, Jailall Ramnauth, Suman Rakhit, Joanne Patman, Paul Renton, Subhash C. Annedi
  • Dihydroindolone compounds, a process for their preparation and pharmaceutical compositions containing them
    Patent number: 8653073
    Abstract: Compounds of formula (I): wherein: m and n represent 1 or 2, A represents a pyrrolyl group, X represents a C(O), S(O) or SO2 group, R1 and R2 represent an alkyl group or, together with the nitrogen atom carrying them, form a heterocyclic group, R3 and R4, together with the atoms carrying them, form a heterocyclic group, R5 represents a hydrogen atom or an alkyl group, R6 represents a hydrogen atom or a halogen atom. Medicinal products containing the same which are useful in treating cancer.
    Type: Grant
    Filed: February 21, 2013
    Date of Patent: February 18, 2014
    Assignee: Les Laboratoires Servier
    Inventors: Jean-Claude Ortuno, Alexis Cordi, Jean-Michel Lacoste, Imre Fejes, Michael Burnbridge, John Hickman, Alain Pierre
  • ??neuronal nicotinic acetylcholine receptor ligands
    Patent number: 8653071
    Abstract: The present invention relates to novel ?4?2 neuronal nicotinic acetylcholine receptor ligand compounds of the formula (I), and their derivatives, stereoisomers, pharmaceutically acceptable salts and compositions containing them. The present invention relates to novel ?4?2 neuronal nicotinic acetylcholine receptor ligand compounds of the formula (I), and their derivatives, stereoisomers, pharmaceutically acceptable salts and compositions containing them.
    Type: Grant
    Filed: May 3, 2010
    Date of Patent: February 18, 2014
    Assignee: Suven Life Sciences Limited
    Inventors: Ramakrishna Nirogi, Abdul Rasheed Mohammed, Kana Ram Kumawat, Ishtiyaque Ahmad, Pradeep Jayarajan, Anil Karbhari Shinde, Nagaraj Vishwottam Kandikere, Koteshwara Mudigonda, Venkateswarlu Jasti
  • Estrogen receptor ligands
    Patent number: 8653072
    Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, carbamate, solvate or salt thereof, including a salt of such an ester, amide or carbamate, and a solvate of such an ester, amide, carbamate or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity, wherein R1, R2, R3, R5 and R6 are as defined in the specification.
    Type: Grant
    Filed: January 11, 2013
    Date of Patent: February 18, 2014
    Assignee: Karo Bio AB
    Inventors: Patrik Rhonnstad, Elisabet Kallin, Theresa Apelqvist, Mattias Wennerstal, Aiping Cheng
  • Insulin-Like Growth Factor-1 Receptor Inhibitors
    Publication number: 20140045832
    Abstract: The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating Insulin-Like-Growth Factor I Receptor and Insulin Receptor. The compounds of the instant invention possess a core structure that comprises a sulfonyl indole moiety. The present invention is also related to the pharmaceutically acceptable salts, hydrates and stereoisomers of these compounds.
    Type: Application
    Filed: April 19, 2012
    Publication date: February 13, 2014
    Applicants: PIRAMAL ENTERPRISES LIMITED, MERCK SHARP & DOHME CORP.
    Inventors: Sarala Balachandran, Christopher J. Dinsmore, Abhijit Roychowdhury, Rajiv Sharma, Ram Asrey Vishwakarma
  • ISOQUINOLIN-1(2H)-ONE DERIVATIVES AS PARP-1 INHIBITORS
    Publication number: 20140045846
    Abstract: There are provided substituted isoquinolin-1(2H)-one derivatives which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of the present invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds. A screening method for the identification of compounds capable of binding several PARP proteins, as well the probes used in such method, are further objects of the invention.
    Type: Application
    Filed: October 23, 2013
    Publication date: February 13, 2014
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Gianluca Mariano Enrico Papeo, Jay Aaron Bertrand, Giovanni Cervi, Barbara Forte, Rosita Lupi, Alessia Montagnoli, Alessandra Scolaro, Fabio Zuccotto, Paolo Orsini, Helena Posteri
  • NOVEL PYRIMIDINE DERIVATIVES
    Publication number: 20140045845
    Abstract: The invention provides novel pyrimidine derivatives of formula (I), methods of preparing such compounds, pharmaceutical compositions containing such compounds, and methods for using such compounds in treatment of diseases including cancer; wherein R1-R11, Z, and Y are as defined in the specification.
    Type: Application
    Filed: March 23, 2012
    Publication date: February 13, 2014
    Applicant: CHEMILIA AB
    Inventors: Marita Högberg, Emma Dahlstedt, Olof Smitt, Tommy Johansson