Three Or More Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 514/234.2)
  • Targeting Human Thymidylate Kinase Induces DNA Repair Toxicity in Malignant Tumor Cells
    Publication number: 20130252953
    Abstract: The present invention relates to novel TMPK inhibitor compositions and their methods of use. In particular, it relates to novel TMPK inhibitor compositions and therapeutics that lead to dUTP-mediated DNA repair in tumor cells and acts as a novel chemosensitizer, which are useful in methods for treating or preventing cancers.
    Type: Application
    Filed: November 29, 2011
    Publication date: September 26, 2013
    Inventors: Zee-Fen Chang, Jim-Min Fang, Chun-Mei Hu, Ming-Tyng Yeh
  • 6-(ETHYNYL)PYRIDO[2,3-D]PYRIMIDIN-7(8H)-ONES FOR THE TREATMENT OF CNS DISORDERS
    Publication number: 20130245012
    Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders.
    Type: Application
    Filed: June 10, 2011
    Publication date: September 19, 2013
    Applicant: AFRAXIS, INC.
    Inventors: David Campbell, Sergio G. Duron, Benedikt Vollrath, Warren Wade
  • STORAGE STABLE PERFUSION SOLUTION FOR DIHYDROPTERIDINONES
    Publication number: 20130245013
    Abstract: Disclosed are storage stable aqueous infusible or injectable solutions containing an active substance of general formula (I) wherein the groups L, R1, R2, R3, R4 and R5 have the meanings given in the claims and in the specification, and an amount of a physiologically acceptable acid or mixture of acids sufficient to dissolve the active substance and act as a stabiliser, optionally together with other formulating excipients suitable for parenteral administration, and a process for preparing the infusible or injectable solutions according to the invention.
    Type: Application
    Filed: April 23, 2013
    Publication date: September 19, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Detlef MOHR, Claus VEIT, Fridtjof TRAULSEN
  • Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents for the treatment of hematopoietic malignancies
    Patent number: 8536161
    Abstract: Combinations of PI3K inhibitor compounds having Formula I and chemotherapeutic agents, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for treating hematopoietic malignancies. Methods of using such combinations 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: Grant
    Filed: March 11, 2010
    Date of Patent: September 17, 2013
    Assignee: Genentech, Inc.
    Inventors: Allen J. Ebens, Jr., Lori Friedman
  • COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR
    Publication number: 20130237531
    Abstract: Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
    Type: Application
    Filed: April 19, 2013
    Publication date: September 12, 2013
    Inventors: Guoxian Wu, Jiazhong Zhang, Chao Zhang, Prabha N. Ibrahim, Songyuan Shi, Wayne Spevak, James Tsai
  • PHARMACEUTICAL COMPOUNDS
    Publication number: 20130230585
    Abstract: 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: Application
    Filed: November 5, 2012
    Publication date: September 5, 2013
    Applicant: F. HOFFMANN-LA ROCHE AG
    Inventors: Irina Chuckowree, Adrian Folkes, Tim Hancox, Stephen Shuttleworth
  • INHIBITORS OF POLO-LIKE KINASE
    Publication number: 20130231335
    Abstract: The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, X, R1, R2, R3, R4, R5 and R6, are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.
    Type: Application
    Filed: April 17, 2013
    Publication date: September 5, 2013
    Applicant: Elan Pharmaceuticals, Inc.
    Inventors: Robert A. Galemmo, Dean R. Artis, Xiaocong Michael Ye, Danielle Aubele, Anh Truong, Simeon Bowers, Roy K. Hom, Yong-Liang Zhu, R. Jeffrey Neitz, Jennifer Sealy, Marc Adler, Paul Beroza, John P. Anderson
  • PYRIDO[3,2-d]PYRIMIDINE PI3K DELTA INHIBITOR COMPOUNDS AND METHODS OF USE
    Publication number: 20130225557
    Abstract: Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. Methods of using compounds of Formula I 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 1, 2013
    Publication date: August 29, 2013
    Applicant: Genentech, Inc.
    Inventor: Genentech, Inc.
  • BICYCLIC DIAMINES AS JANUS KINASE INHIBITORS
    Publication number: 20130225577
    Abstract: The instant invention provides compounds of formula I which are Jak inhibitors, and as such are useful for the treatment of Jak-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
    Type: Application
    Filed: October 17, 2011
    Publication date: August 29, 2013
    Inventors: David Joseph Guerin, Jason D. Brubaker, Michelle Martinez, Joon O. Jung, Neville J. Anthony, Mark E. Scott, Carolyn Michele Cammarano, Dawn Marie Mampreian Hoffman, Hyun Chong Woo, Christopher J. Dinsmore, Philip Jones
  • HALOARYL SUBSTITUTED AMINOPURINES, COMPOSITIONS THEREOF,AND METHODS OF TREATMENT THEREWITH
    Publication number: 20130225564
    Abstract: Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing cancer, a cardiovascular disease, a renal disease, an autoimmune condition, an inflammatory condition, macular degeneration, ischemia-reperfusion injury, pain and related syndromes, disease-related wasting, an asbestos-related condition, pulmonary hypertension or a condition treatable or preventable by inhibition of the JNK pathway comprising administering an effective amount of an Aminopurine Compound to a patient in need thereof.
    Type: Application
    Filed: March 18, 2013
    Publication date: August 29, 2013
    Applicant: Signal Pharmaceuticals, LLC
    Inventor: Signal Pharmaceuticals, LLC
  • METHODS FOR TREATING NEUROLOGICAL CONDITIONS
    Publication number: 20130225575
    Abstract: Provided herein are PAK inhibitors. Also provided herein are compositions and methods for treating an individual suffering from certain neurological conditions.
    Type: Application
    Filed: June 16, 2011
    Publication date: August 29, 2013
    Applicant: AFRAXIS, INC.
    Inventors: Jay Lichter, David Campbell, Sergio G. Duron, Benedikt Vollrath
  • 1H-PYRAZOLO[3,4-B]PYRIDINES AND THERAPEUTIC USES THEREOF
    Publication number: 20130225576
    Abstract: Provided herein are compounds according to Formula I and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancers such as colon, ovarian, pancreatic, breast, liver, prostate and hematologic cancers:
    Type: Application
    Filed: April 3, 2013
    Publication date: August 29, 2013
    Applicant: Samumed, LLC
    Inventor: Samumed, LLC
  • HETEROBICYCLIC COMPOUNDS
    Publication number: 20130225552
    Abstract: Heterobicyclic compounds of Formula (I): or a pharmaceutically-acceptable salt, tautomer, or stereoisomer thereof, as defined in the specification, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, Huntington's Disease, and the like.
    Type: Application
    Filed: February 28, 2013
    Publication date: August 29, 2013
    Applicant: AMGEN INC.
    Inventor: Amgen Inc.
  • CRTH2 MODULATORS
    Publication number: 20130216552
    Abstract: Modulators of CRTH2, particularly antagonists of CRTH2, that are useful for treating various disorders, including asthma and respiratory disorders are disclosed herein.
    Type: Application
    Filed: June 24, 2011
    Publication date: August 22, 2013
    Applicant: Ironwood Pharmaceuticals, Inc.
    Inventors: Takashi Nakai, James Jia, Jason Rohde, Regina Graul, Ara Mermerian
  • BENZIMIDAZOLE AND AZABENZIMIDAZOLE COMPOUNDS THAT INHIBIT ANAPLASTIC LYMPHOMA KINASE
    Publication number: 20130217668
    Abstract: Compounds of Formula (I) are useful inhibitors of anaplastic lymphoma kinase. Compounds of Formula (I) have the following structure: where the definitions of the variables are provided herein.
    Type: Application
    Filed: July 28, 2011
    Publication date: August 22, 2013
    Applicant: AMGEN INC.
    Inventors: Christiane M. Boezio, Alan C. Cheng, Deborah Choquette, Richard T. Lewis, Michele H. Potashman, Karina Romero, John C. Stellwagen, Douglas A. Whittington
  • NOVEL COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES
    Publication number: 20130217664
    Abstract: Novel imidazolopyridines according to Formula I, able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic or inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons. Wherein R1, L1, R3, R4, Cy, L2 and R5 are as defined herein.
    Type: Application
    Filed: February 7, 2013
    Publication date: August 22, 2013
    Inventors: Christel Jeanne Marie MENET, Benoit Antoine SCHMITT, Raphael Jean Joel GENEY, Kevin James DOYLE, Joanne PEACH, Nicholas John PALMER, Graham Peter JONES, David HARDY, James Edward Stewart DUFFY
  • ENHANCED TREATMENT REGIMENS USING MTOR INHIBITORS
    Publication number: 20130209543
    Abstract: The present invention provides for methods and pharmaceutical compositions comprising inhibitors of mTorC1 and/or mTorC2. In some aspects, the invention provides for treatment regimens resulting in enhanced treatment efficacy and better tolerability.
    Type: Application
    Filed: November 21, 2012
    Publication date: August 15, 2013
    Applicant: Intellikine LLC
    Inventor: Intellikine LLC
  • POSITIVE ALLOSTERIC MODULATORS OF MGLUR2
    Publication number: 20130210768
    Abstract: The present invention is directed to 5-substituted 1,3-dihydro-2H-imidazo[4,5-b]pyridine-2-one derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved, such as schizophrenia.
    Type: Application
    Filed: June 6, 2011
    Publication date: August 15, 2013
    Inventors: Kenneth L. Arrington, Vadim Dudkin, Mark E. Layton, Joseph E. Pero, Alexander J. Reif
  • Preventive and/or therapeutic agent for neutrophilic inflammatory diseases
    Patent number: 8507484
    Abstract: The present invention provides a preventive and/or therapeutic agent for neutrophilic inflammatory diseases which comprises, as an active ingredient, a bicyclic heterocyclic compound represented by formula (I): [wherein R1 represents a hydrogen atom, substituted or unsubstituted alkyl, or the like, A1-A2-A3-A4 represents N?CR3—CR4?CR5 (wherein R3, R4, and R5 are the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, and the like), Q represents substituted or unsubstituted phenylene, and the like, and T represents substituted or unsubstituted lower alkyl, substituted or unsubstituted aroyl, and the like].
    Type: Grant
    Filed: February 25, 2005
    Date of Patent: August 13, 2013
    Assignee: Kyowa Hakko Kirin Co., Ltd.
    Inventors: Kyoichiro Iida, Nobumasa Otsubo, Takeshi Kuboyama, Hitoshi Arai, Akihiko Watanabe, Mayumi Saki, Naoko Hiura, Haruhiko Manabe, Hidenori Takada, Jun Saito
  • Inhibitors of Human Immunodeficiency Virus Replication
    Publication number: 20130203748
    Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.
    Type: Application
    Filed: August 9, 2012
    Publication date: August 8, 2013
    Inventors: B. Narasimhulu Naidu, Manoj Patel
  • BICYCLIC HETEROARYL KINASE INHIBITORS AND METHODS OF USE
    Publication number: 20130203755
    Abstract: Provided are compounds having an inhibitory effect on kinases including Mixed Lineage Kinases. Also provided are pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions that are affected by Mixed Lineage Kinase inhibition. Also provided are methods of treatment of neuropsychiatric disorders that comprise the inhibition of Mixed Lineage Kinases.
    Type: Application
    Filed: May 24, 2011
    Publication date: August 8, 2013
    Applicant: UNIVERSITY OF ROCHESTER
    Inventors: Harris A. Gelbard, Stephen Dewhurst, Val S. Goodfellow, Torsten Wiemann, Satheesh Babu Ravula, Colin J. Loweth
  • Heterocyclic compound and use thereof
    Patent number: 8501750
    Abstract: Heterocyclic compounds, pharmaceutical agent and methods thereof, having superior pharmacological action and/or physicochemical properties, which are useful for the prophylaxis or treatment of circulatory diseases such as hypertension, cardiac diseases, arteriosclerosis, renal diseases and cerebral apoplexy and/or metabolic diseases such as hyperlipidemia, obesity and diabetes and/or central nervous disorders such as cerebral infarction, and/or mental diseases such as dementia depression and depression.
    Type: Grant
    Filed: May 20, 2008
    Date of Patent: August 6, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Takanobu Kuroita, Hideyuki Igawa, Hiroki Sakamoto, Kouhei Asano, Minoru Sasaki
  • BENZODIOXANE INHIBITORS OF LEUKOTRIENE PRODUCTION
    Publication number: 20130196973
    Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.
    Type: Application
    Filed: March 13, 2012
    Publication date: August 1, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Asitha Abeywardane, Michael J. Burke, Thomas Martin Kirrane, Matthew Russell Netherton, Anil Kumar Padyana, Lana Louise Smith Keenan, Hidenori Takahashi, Michael Robert Turner, Qiang Zhang, Qing Zhang
  • Dihydrothienopyrimidines
    Publication number: 20130196988
    Abstract: The present invention relates to dihydrothienopyrimidines, their use as modulators of ?-secretase and to pharmaceutical compositions containing said compounds. In particular, the present invention relates to compounds which interfere with ?-secretase and/or its substrate and therefore modulate the formation of A? peptides.
    Type: Application
    Filed: July 27, 2012
    Publication date: August 1, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Kia GERLACH, Niklas HEINE, Scott HOBSON, Christoph HOENKE, Alexander WEBER
  • COMPOSITIONS AND METHODS FOR INDUCING CELL DEDIFFERENTIATION
    Publication number: 20130196989
    Abstract: The present invention provides compounds, compositions and methods for dedifferentiating lineage committed mammalian cells into stem cells. The present invention also provides methods of inducing dedifferentiation of lineage committed mammalian cells into stem cells, which can be further differentiated into various lineage committed cells. Methods of identifying additional compounds useful for inducing dedifferentiation of lineage committed cells into stem cells are also provided.
    Type: Application
    Filed: August 24, 2012
    Publication date: August 1, 2013
    Applicant: The Scripps Research Institute
    Inventors: Shuibing Chen, Sheng Ding, Peter G. Schultz
  • Antiviral Activity of Novel Bicyclic Heterocycles
    Publication number: 20130190297
    Abstract: The present invention relates to compound of Formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, and R12 are as defined in the claim 1 or as described in detail in the description of the invention, and to the use of said compounds to treat or prevent viral infections and their use to manufacture a medicine to treat or prevent viral infections, particularly infections with RNA-viruses belonging to the family of the Retroviridae, the family of the Flaviviridae and the family of the Picornaviridae and more preferably infections with Human Immunodeficiency Virus 1 (HIV1), Human Immunodeficiency Virus 2 (HIV2), Hepatitis C virus (HCV), Dengue virus, and enteroviruses like Coxsackievirus, Rhinovirus and Poliovirus.
    Type: Application
    Filed: May 20, 2011
    Publication date: July 25, 2013
    Applicant: KATHOLIEKE UNIVERSITEIT LEUVEN, K.U.LEUVEN R&D
    Inventors: Steven De Jonghe, Ling-Jie Gao, Piet Herdewijn, Jean Herman, Miyeon Jang, Pieter Leyssen, Thierry Louat, Johan Neyts, Christophe Pannecouque, Bart Vanderhoydonck
  • HETEROCYCLYL PYRAZOLOPYRIMIDINE ANALOGUES AS SELECTIVE JAK INHIBITORS
    Publication number: 20130190292
    Abstract: The present invention relates to compounds of formula (I) wherein X1 to X5, Y, Z1 to Z3, and R have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
    Type: Application
    Filed: August 12, 2011
    Publication date: July 25, 2013
    Applicant: CELLZOME LIMITED
    Inventors: Kathryn Bell, Nelly Piton, Claudio Dagostin, Cyrille Boussard, Andrew Ratcliffe, Nigel Ramsden
  • AZAINDAZOLE COMPOUNDS
    Publication number: 20130184254
    Abstract: Disclosed are azaindazole compounds of Formula (I), or pharmaceutically acceptable salts thereof, wherein W is CR4 or N; and R1, R2, R3, and R4 are defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: July 14, 2011
    Publication date: July 18, 2013
    Inventors: Upender Velaparthi, David B. Frennesson, Mark G. Saulnier, Joel F. Austin, Audris Huang, James Aaron Balog, Dolatrai M. Vyas
  • Protein Kinase Inhibitors and Methods of Treatment
    Publication number: 20130184274
    Abstract: The present invention relates to chemical compounds of formula (I) and methods for their use and preparation. In particular, the invention relates to substituted pyrazolo[3,4-d]pyrimidine based compounds which can be used in treating proliferative disorders, use of these compounds in methods of therapy and the manufacture of medicaments as well as compositions containing these compounds.
    Type: Application
    Filed: July 8, 2011
    Publication date: July 18, 2013
    Inventors: Guillaume Laurent Lessene, Jonathan Bayldon Baell, Antony Wilks Burgess, Hiroshi Maruta
  • TETRAHYDROPYRIDO-PYRIDINE AND TETRAHYDROPYRIDO-PYRIMIDINE COMPOUNDS AND USE THEREOF AS C5A RECEPTOR MODULATORS
    Publication number: 20130184253
    Abstract: The present invention provides a compound of formula I: (I) a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: July 19, 2012
    Publication date: July 18, 2013
    Applicant: NOVARTIS AG
    Inventors: Christopher Michael ADAMS, Veronique DARSIGNY, Alec Nathanson FLYER, Christine Fang GELIN, Timothy Brian Hurley, Nan JI, Rajeshri Ganesh KARKI, Toshio KAWANAMI, Erik MEREDITH, Chang RAO, Michael H. SERRANO-WU, Catherine Fooks SOLOVAY
  • HETERO RING-FUSED IMIDAZOLE DERIVATIVE HAVING AMPK ACTIVATING EFFECT
    Publication number: 20130184240
    Abstract: Disclosed is a compound which is useful as an AMPK activator. A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein a group represented by the formula: is a group represented by the formula: R1 is each independently halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like; m is an integer of 0 to 3; R2 is hydrogen, or substituted or unsubstituted alkyl; X is —O—; and Y is substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.
    Type: Application
    Filed: September 8, 2011
    Publication date: July 18, 2013
    Applicant: Shionogi & Co., Ltd.
    Inventors: Keisuke Tonogaki, Akira Ino, Eiichi Kojima, Manabu Katou, Masafumi Iwatsu, Nobuyuki Tanaka, Masahiko Fujioka
  • Compounds for the reduction of ?-amyloid production
    Patent number: 8486952
    Abstract: The present disclosure provides a series of compounds of the formula (I) which modulate ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by ?-amyloid peptide (?-AP) production.
    Type: Grant
    Filed: July 28, 2010
    Date of Patent: July 16, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Kenneth M. Boy, Jason M. Guernon, John E. Macor, Richard E. Olson, Jianliang Shi, Lorin A. Thompson, III, Yong-Jin Wu, Li Xu, Yunhui Zhang, Dmitry S. Zuev
  • COMPOUNDS FOR THE REDUCTION OF BETA-AMYLOID PRODUCTION
    Publication number: 20130178462
    Abstract: The present disclosure provides a series of compounds of the formula (I) which modulate ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by ?-amyloid peptide (?-AP) production.
    Type: Application
    Filed: March 5, 2013
    Publication date: July 11, 2013
    Applicant: Bristol-Myers Squibb Company
    Inventor: Bristol-Myers Squibb Company
  • PYRAZOLO[3,4-d]PYRIMIDINE AND PYRROLO[2,3-d]PYRIMIDINE COMPOUNDS AS KINASE INHIBITORS
    Publication number: 20130172314
    Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
    Type: Application
    Filed: September 14, 2012
    Publication date: July 4, 2013
    Applicant: Pharmacyclics, Inc.
    Inventors: Wei CHEN, David J. Loury
  • SUBSTITUTED 2-(9H-PURIN-9-YL) ACETIC ACID ANALOGUES AS INHIBITORS OF STAT3
    Publication number: 20130172340
    Abstract: In one aspect, the invention relates to substituted purine analogs, derivatives thereof, and related compounds, which are useful as inhibitors of STAT protein activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a STAT protein activity dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: June 22, 2011
    Publication date: July 4, 2013
    Applicant: University of Central Flordia Research Foundation,
    Inventors: James Turkson, Patrick Gunning
  • FUSED PYRAZOLE DERIVATIVES AS NOVEL ERK INHIBITORS
    Publication number: 20130172341
    Abstract: Disclosed are the ERK inhibitors of Formula (I): (Formula (I)) and the pharmaceutically acceptable salts thereof. All substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of Formula (I).
    Type: Application
    Filed: September 12, 2011
    Publication date: July 4, 2013
    Inventors: Gerald W. Shipps, JR., Yongqi Deng, Alan B. Cooper, Xiaolei Gao, Binyuan Sun, James Wang, Liang Zhu
  • Purine-core inhibitors of HSP90 and their use in treating cancer
    Patent number: 8476285
    Abstract: The invention relates to compounds of Formulae I-III: and therapeutic uses thereof, wherein A is chosen from a substituted or unsubstituted aryl, heteroaryl, heterocyclic, or carbocyclic group; B is chosen from a substituted or unsubstituted piperidine, homopiperidine, piperazine, pyrrolidine or azetidine group; R1 is chosen from hydro, alkyl, aryl, heteroaryl, amino, or halo; and L1, L2, are as defined herein.
    Type: Grant
    Filed: June 30, 2009
    Date of Patent: July 2, 2013
    Assignee: Myrexis, Inc.
    Inventors: Ashok C. Bajji, Se-Ho Kim, Benjamin Markovitz, Richard Trovato, Rajendra Tangallapally, Mark B. Anderson, Daniel Wettstein, Mark Shenderovich, John A. Vanecko
  • CHEMICAL COMPOUNDS
    Publication number: 20130165439
    Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R1 to R5 are defined as in claim 1, which are suitable for treating diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a medicament having the above-mentioned properties.
    Type: Application
    Filed: February 25, 2013
    Publication date: June 27, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Darryl MCCONNELL, Lars van der VEEN, Tobias WUNBERG
  • IMIDAZOPYRIDINE, IMIDAZOPYRIMIDINE AND IMIDAZOPYRAZINE DERIVATIVES AS MELANOCORTIN-4 RECEPTOR MODULATORS
    Publication number: 20130165426
    Abstract: Disclosed is a compound of Formula I or a salt thereof, in which X, X1, X2, R1, R2, and R3 are described herein. Also disclosed are pharmaceutical compositions and methods of using the compounds of Formula I to treat disorders mediated by melanocortin-4 receptors.
    Type: Application
    Filed: July 5, 2011
    Publication date: June 27, 2013
    Applicant: UNIVERSITÉ DE MONTRÉAL
    Inventors: Réjean Ruel, Yves Chantigny, Anne Marinier, Patricia Rene, Michel Bouvier
  • COMPOUNDS AND COMPOSITIONS FOR TREATING CHEMICAL WARFARE AGENT-INDUCED INJURIES
    Publication number: 20130165427
    Abstract: Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein.
    Type: Application
    Filed: August 24, 2012
    Publication date: June 27, 2013
    Applicant: HYDRA BIOSCIENCES, INC.
    Inventor: Jayhong A. Chong
  • Episomal fusion gene
    Patent number: 8470826
    Abstract: The present invention relates to an episomal structure expressing a functional oncogene, whereby said oncogene is a fusion gene of two chromosomal gene fragments. More specifically, the invention relates to a NUP214-ABL1 fusion product, important in the development of T-cell acute lymphoblastic leukemia, to methods to detect the fusion and to methods to prevent the oncogenic activity of said fusion product.
    Type: Grant
    Filed: June 15, 2010
    Date of Patent: June 25, 2013
    Assignees: VIB VZW, K.U. Leuven Research and Development
    Inventors: Jan Cools, Anne Hagemeijer, Peter Marynen
  • NOVEL PYRIDOPYRAZINES AND THEIR USE AS MODULATORS OF KINASES
    Publication number: 20130157976
    Abstract: The invention relates to novel pyrido[2,3-b]pyrazine derivatives of the general formulae (I) and (II), and to their preparation and use as medicaments, especially for the treatment of malignant disorders and other disorders based on pathological cell proliferations.
    Type: Application
    Filed: February 19, 2013
    Publication date: June 20, 2013
    Inventors: Eckhard CLAUS, Irene Seipelt, Eckhard Guenther, Emmanuel Polymeropoulos, Michael Czech, Tilmann Schuster
  • AZOLOPYRIDIN-3-ONE DERIVATIVES AS INHIBITORS OF LIPASES AND PHOSPHOLIPASES
    Publication number: 20130157941
    Abstract: The present invention relates to azolopyridin-3-one derivatives of the general formula (I) with the meanings specified in the description, to their pharmaceutically usable salts and to their use as drug substances.
    Type: Application
    Filed: June 17, 2011
    Publication date: June 20, 2013
    Applicant: Sanofi
    Inventors: Stefan Petry, Norbert Tennagels, Karl-Heinz Baringhaus
  • POSITIVE ALLOSTERIC MODULATORS OF MGLUR2
    Publication number: 20130158002
    Abstract: The present invention is directed to 5-substituted 1,3-dihydro-2,1,3-benzothiadiazole 2,2-dioxide and 1,3-dihydro[1,2,5]thiadiazolo[3,4-b]pyridine 2,2,-dioxide derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
    Type: Application
    Filed: February 28, 2011
    Publication date: June 20, 2013
    Inventors: Mark E. Layton, Michael J. Kelly, Timothy J. Hartingh
  • USE OF STIMULATORS AND ACTIVATORS OF SOLUBLE GUANYLATE CYCLASE FOR TREATING SICKLE-CELL ANEMIA AND CONSERVING BLOOD SUBSTITUTES
    Publication number: 20130158028
    Abstract: The present invention relates to the novel use of stimulators and activators of soluble guanylate cyclase for the treatment of sickle cell anemia and for the preservation of blood substitutes. The present invention furthermore relates to the use of stimulators and activators of soluble guanylate cyclase in combination with PDE5 inhibitors for the treatment of sickle cell anemia and for the preservation of blood substitutes.
    Type: Application
    Filed: June 21, 2011
    Publication date: June 20, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Johannes-Peter Stasch, Eva-Maria Becker, Hubert Trübel, Herbert Himmel
  • PYRAZOLO PYRIDINE DERIVATIVES AS NADPH OXIDASE INHIBITORS
    Publication number: 20130158027
    Abstract: The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).
    Type: Application
    Filed: January 31, 2013
    Publication date: June 20, 2013
    Applicant: GENKYOTEX SA
    Inventor: GENKYOTEX SA
  • IDENTIFICATION OF GENE EXPRESSION AS A PREDICTIVE BIOMARKER FOR LKB1 STATUS
    Publication number: 20130158023
    Abstract: Provided herein are methods for predicting the LKB1 status of a patient or a biological sample, comprising the measurement of particular gene expression levels relative to a set of reference levels that represent the gene expression level of a biological wild-type sample without LKB1 gene or protein loss or mutation and the gene expression level of a reference sample with LKB1 gene or protein loss or mutation. Further provided herein are methods for treating and/or preventing a cancer or a tumor syndrome in a patient, comprising administering an effective amount of a TOR kinase inhibitor to a patient having cancer or a tumor syndrome, characterized by particular gene expression levels.
    Type: Application
    Filed: August 2, 2012
    Publication date: June 20, 2013
    Applicant: SIGNAL PHARMACEUTICALS, LLC
    Inventors: Yuhong L. Ning, Weiming Xu, Rajesh Chopra, Peter Worland, Shuichan Xu
  • Use of reversine and analogs for treatment of cancer
    Patent number: 8466147
    Abstract: Herein is provided methods and compositions for treating cancer. In one embodiment, a method is provided for treating a patient suffering from cancer, the method comprising administering to the patient an effective amount of reversine, reversine analog or reversine containing agent. In another embodiment, compositions comprising reversine are provided. Such compositions may further comprise additional active agents and other additives. The compositions and methods provided herein are useful, for example, in the area of medicine.
    Type: Grant
    Filed: November 12, 2007
    Date of Patent: June 18, 2013
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Kenneth C. Anderson, Nicholas Mitsiades, Joseph Negri, Douglas W. McMillin, Constantine S. Mitsiades
  • 6-(4-Hydroxy-phenyl)-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
    Publication number: 20130150340
    Abstract: The present invention relates to 1H-pyrazolo[3,4-b]pyridine compounds of the formula I, in which R1, R2, R3 and R4 are defined as indicated below. The compounds of the formula I are kinase inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, 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: Application
    Filed: October 25, 2012
    Publication date: June 13, 2013
    Applicant: SANOFI
    Inventor: SANOFI
  • Phosphoinositide 3-kinase inhibitors with a zinc binding moiety
    Patent number: 8461157
    Abstract: The instant application relates to deazapurines, thienopyrimidines and furopyrimidines with zinc-binding moiety based derivatives and their use in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.
    Type: Grant
    Filed: April 1, 2011
    Date of Patent: June 11, 2013
    Assignee: Curis, Inc.
    Inventors: Xiong Cai, Haixiao Zhai, Chengjung Lai, Changgeng Qian