Polycyclo Ring System Having A 1,2- Or 1,4-diazine As One Of The Cyclos Patents (Class 514/248)
  • Publication number: 20140135323
    Abstract: The invention relates to novel inhibitors of kinases of the general formula (I): in which Q and R1 are defined in the claims, method for preparing such inhibitors, intermediates for preparing such inhibitors and uses of such inhibitors.
    Type: Application
    Filed: January 17, 2014
    Publication date: May 15, 2014
    Applicant: Bayer Intellectual Property GmbH
    Inventors: Olaf PRIEN, Knut EIS, Benjamin BADER, Judith GUENTHER, Arne VON BONIN
  • 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
  • Publication number: 20140134133
    Abstract: The present invention provides heteroaromatic derivatives and pharmaceutical acceptable salts and formulations thereof useful in modulating the protein kinase activity, especially phosphatidylinositol 3-kinases (PI3 kinases) and mTOR, and in modulating inter- and/or intra-cellular signaling activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
    Type: Application
    Filed: November 10, 2013
    Publication date: May 15, 2014
    Applicants: Calitor Sciences, LLC
    Inventor: Ning Xi
  • Publication number: 20140135336
    Abstract: Disclosed are compounds of general formula (I) wherein the groups R1 to R3 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.
    Type: Application
    Filed: November 11, 2013
    Publication date: May 15, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Harald ENGELHARDT, Davide GIANNI, Dirk KESSLER, Ulrich REISER, Christian SMETHURST, Andreas STEFFEN
  • Patent number: 8722675
    Abstract: The present invention is directed to methods and agents that are useful in the prevention and amelioration of signs and symptoms associated with neuropathic conditions. More particularly, the present invention discloses the use of angiotensin II receptor 2 (AT2 receptor) antagonists for the treatment, prophylaxis, reversal and/or symptomatic relief of neuropathic pain, including mechanical hyperalgesia, thermal or mechanical allodynia, diabetic pain and entrapment pain, in vertebrate animals and particularly in human subjects. The AT2 receptor antagonists may be provided alone or in combination with other compounds such as those that are useful in the control of neuropathic conditions.
    Type: Grant
    Filed: June 20, 2013
    Date of Patent: May 13, 2014
    Assignee: Spinifex Pharmaceuticals Pty Ltd
    Inventors: Maree Therese Smith, Bruce Douglas Wyse
  • Patent number: 8722676
    Abstract: Bicyclic piperazine compounds of Formula I 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: November 2, 2012
    Date of Patent: May 13, 2014
    Assignee: Genentech, Inc.
    Inventors: James John Crawford, Daniel Fred Ortwine, Wendy B. Young
  • Publication number: 20140128352
    Abstract: Compounds that modulate mitochondrial reactive oxygen species (ROS) production are provided. The compounds may modulate ROS production at defined sites without also altering energy production. Methods of using and identifying such compounds are also provided.
    Type: Application
    Filed: September 20, 2013
    Publication date: May 8, 2014
    Applicant: Buck Institute for Research on Aging
    Inventors: Martin D. Brand, Adam Orr
  • Publication number: 20140127157
    Abstract: Antiviral activity of Nilotinib against Hepatitis C virus.
    Type: Application
    Filed: November 4, 2013
    Publication date: May 8, 2014
    Inventors: Erica Canino, Adam Feire, Christopher Jones, Paul W. Manley
  • Publication number: 20140128401
    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: Application
    Filed: January 13, 2014
    Publication date: May 8, 2014
    Applicant: Genentech, Inc.
    Inventors: James John Crawford, Daniel Fred Ortwine, BinQing Wei, Wendy B. Young
  • Publication number: 20140128400
    Abstract: Bridged bicyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
    Type: Application
    Filed: January 8, 2014
    Publication date: May 8, 2014
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Sacha Holland, Joane Litvak, Dane Goff, Jing Zhang, Thilo J. Heckrodt
  • Patent number: 8716290
    Abstract: Substituted bicyclic heteroaryls and compositions containing them, 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, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lympho
    Type: Grant
    Filed: April 4, 2013
    Date of Patent: May 6, 2014
    Assignee: Amgen Inc.
    Inventors: Minna Bui, Timothy David Cushing, Felix Gonzalez Lopez De Turiso, Xiaolin Hao, Brian Lucas
  • Patent number: 8716289
    Abstract: Compound corresponding to general formula (I): in which R2 is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy or NR8R9 group; n is an integer equal to 1, 2 or 3 and m is an integer equal to 1 or 2; A is a covalent bond or a C1-8-alkylene group; R1 is a phenyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, triazinyl, naphthyl, quinolinyl, isoquinolinyl, phthalazinyl, quinazolinyl, quinoxalinyl, cinnolinyl or naphthyridinyl group, this group being optionally substituted; R3 is a hydrogen or fluorine atom, a C1-6-alkyl group or a tritluoromethyl group; R4 is a group selected from furanyl, pyrrolyl, thienyl, isothiazolyl, oxazolyl, isoxazolyl, pyrazolyl, oxadiazolyl, thiadiazolyl, imidazole, triazolyl, tetrazolyl, oxazolone, oxazolidinone, isoxazolone, isoxazolidinone, isothiazolone, isothiazolidinone, imidazolone, imidazolidinone, pyrazolone, pyrazolidinone, oxadiazolone, thiadiazolone and triazolone, this group being optionally substituted; in the form of a base or o
    Type: Grant
    Filed: November 13, 2009
    Date of Patent: May 6, 2014
    Assignee: Sanofi
    Inventors: Ahmed Abouabdellah, Nathalie Chereze, Aude Fayol, Mourad Saady, Julien Vache, Corinne Veronique, Philippe Yaiche
  • Patent number: 8716282
    Abstract: The present invention relates to novel imidazo[1,2-b]pyridazine derivatives which are inhibitors of the phosphodiesterase 10 enzyme (PDE10) and which are useful for the treatment or prevention of neurological, psychiatric and metabolic disorders in which the PDE10 enzyme is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, to the use of such compounds or pharmaceutical compositions for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases.
    Type: Grant
    Filed: April 28, 2011
    Date of Patent: May 6, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Joaquin Pastor-Fernández, José Manuel Bartolomé-Nebreda, Gregor James Macdonald, Susana Conde-Ceide, Óscar Delgado-González, Greta Constantia Peter Vanhoof, Michiel Luc Maria Van Gool, María Luz Martín-Martín, Sergio-Alvar Alonso-de Diego, Kelly Ann Swinney, Carina Leys, Johan Erwin Edmond Weerts, Stijn Wuyts
  • Publication number: 20140121240
    Abstract: Provided is a novel pharmaceutical composition (antipruritic agent) that is useful for prophylaxis or treatment of itch in conditions such as dermal pruritus. More specifically, provided is a pharmaceutical composition (antipruritic agent) for treatment of itch comprising as an active ingredient a naphthalene compound of the following formula (I): wherein the ring A is a heterocyclic group of the following formula: a hydrate thereof or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: June 26, 2012
    Publication date: May 1, 2014
    Applicants: MARUHO CO., LTD., MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Ryoko Oono, Hiroko Kido
  • Publication number: 20140121205
    Abstract: Compounds, compositions and methods for the treatment of retinal degenerative diseases, such as retinitis pigmentosa, Leber's congenital Amaurosis, Syndromic retinal degenerations, age-related macular degeneration and Usher Syndrome, and hearing loss associated with Usher Syndrome are described herein.
    Type: Application
    Filed: March 8, 2013
    Publication date: May 1, 2014
    Applicant: Usher III Initiative
    Inventors: Roland Werner Bürli, William Rameshchandra Krishna Esmieu, Christopher James Lock, Karine Fabienne Malagu, Andrew Pate Owens, William E. Harte
  • Publication number: 20140121197
    Abstract: Compounds, compositions and methods for the treatment of retinal degenerative diseases, such as retinitis pigmentosa, Leber's congenital Amaurosis, Syndromic retinal degenerations, age-related macular degeneration and Usher Syndrome, and hearing loss associated with Usher Syndrome are described herein.
    Type: Application
    Filed: March 8, 2013
    Publication date: May 1, 2014
    Inventors: Roland Werner BÜRLI, William Rameshchandra Krishna ESMIEU, Christopher James LOCK, Karine Fabienne MALAGU, Andrew Pate OWENS, William E. HARTE
  • Patent number: 8710057
    Abstract: The present invention provides protein kinase inhibitors comprising imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine compounds of the following structure (I) and (II): or a stereoisomer, prodrug or pharmaceutically acceptable salt thereof, wherein R, R1, R2 and X are as defined herein. Compositions and methods for using the same in the treatment of cancer and other Pim kinase-associated conditions are also disclosed.
    Type: Grant
    Filed: July 21, 2011
    Date of Patent: April 29, 2014
    Assignee: Tolero Pharmaceuticals, Inc.
    Inventors: David J. Bearss, Xiao-Hui Liu, Hariprasad Vankayalapati, Yong Xu
  • Publication number: 20140113900
    Abstract: The present application relates to novel substituted imidazopyridazines, to processes for their preparation, to their use, alone or in combinations, for the treatment and/or prophylaxis of diseases and to their use for production of medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Application
    Filed: May 2, 2012
    Publication date: April 24, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Alexander Straub, Jens Ackerstaff, Nils Griebenow, Andreas Knorr, Frank Wunder, Volkhart Min-Jian Li
  • Publication number: 20140113902
    Abstract: A method for preparing 5-amino-2,3-dihydrophthalazine-1,4-dione salts with alkali metals of the formula II, pharmaceutical compositions including such salts, and their application in medicine. The sodium salt may be used for treatment of heart diseases, pancreas diseases and diabetes as well as optionally in combination with lithium salt for treatment of the nervous system diseases.
    Type: Application
    Filed: September 16, 2013
    Publication date: April 24, 2014
    Applicant: ABIDOPHARMA PL SP. Z.O.O.
    Inventors: Admir Musaevich ABIDOV, Irina Georgievna DANILOVA
  • Publication number: 20140112945
    Abstract: The compounds of formula (1) in which R1, R7, R8, R9, R10, R17, R18, R19, R20 and m have the meanings as given in the description, are novel effective inhibitors of type 4 and type 5 phosphodiesterase.
    Type: Application
    Filed: June 12, 2012
    Publication date: April 24, 2014
    Applicant: TAKEDA GmbH
    Inventors: Thomas Stengel, Thomas Maier, Alexander Mann, Josef Stadlwieser, Dieter Flockerzi, Andreas Pahl, Ewald Benediktus, Manuela Hessmann, Tobias Kanacher, Ragna Hussong, Christof Zitt, Hans Christof Holst, Rolf-Peter Hummel, Martin Viertelhaus, Hermann Tenor, Torsten Dunkern, Armin Hatzelmann, Christian Hesslinger
  • Publication number: 20140113901
    Abstract: Imidazopyridazines of formula (I) a process for their production and the use thereof.
    Type: Application
    Filed: April 7, 2011
    Publication date: April 24, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Lars Bärfacker, William Sott, Andrea Hägebarth, Stuart Ince, Hartmut Rehwinkel, Oliver Politz, Roland Neuhaus, Hans Briem, Ulf Bömer
  • Patent number: 8703760
    Abstract: The present invention relates to a novel antiplatelet agent and a novel compound which is an active ingredient for the agent. The present invention provides the antiplatelet agent comprising a compound represented by the formula I: wherein, X is N, or CR1d, Xb1-Xb5 are the same or different, and are nitrogen or carbon, R1a-R1d are the same or different, and are hydrogen, an optionally substituted alkyl, an optionally substituted alkoxy, an optionally substituted alkylthio, an alkenyl, a cycloalkyl, a halogen, cyano, or hydroxyl or optionally substituted by 1 or 2 alkylamino, R2 is an optionally substituted aryl or an optionally substituted heteroaryl, R3 is an optionally substituted aryl or an optionally substituted heteroaryl, or pharmaceutically acceptable salt thereof as an active ingredient.
    Type: Grant
    Filed: December 17, 2010
    Date of Patent: April 22, 2014
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Hiroshi Sato, Kazutoshi Yokoyama, Kazushi Sato
  • Patent number: 8703769
    Abstract: Methods of treating or preventing obesity or obesity related disorders in a subject are provided, comprising administering to the subject a treatment effective in reducing one or more activities of an epidermal growth factor receptor (EGFR) in the subject. Methods of screening for compositions that can modulate one or more EGFR activities are also provided.
    Type: Grant
    Filed: July 14, 2006
    Date of Patent: April 22, 2014
    Assignee: The University of North Carolina at Chapel Hill
    Inventors: David Threadgill, Cordelia Johnson Barrick
  • Publication number: 20140105898
    Abstract: This invention relates generally to methods and agents for modulating adiposity-related conditions. More particularly, the present invention relates to the use of TRAIL death receptor agonists, including nucleic acids such as TRAIL polynucleotides, peptides and polypeptides including TRAIL polypeptides, TRAIL DR agonist antigen-binding molecules, TRAIL DR peptide agonists as well as small molecule TRAIL DR agonists in compositions and methods for treating or preventing adiposity-related conditions such as obesity, diabetes mellitus and metabolic syndrome.
    Type: Application
    Filed: February 27, 2012
    Publication date: April 17, 2014
    Applicant: Istituto Di Ricovero E Cura A Carattere Scientific Materno-Infantile Burlo Garo
    Inventors: Merlin C. Thomas, Giorgio Zauli, Paola Secchiero, Bruno Fabris, Stella Bernardi
  • Patent number: 8697627
    Abstract: The present invention provides compositions for reducing amyloid plaque burden associated with Alzheimer's disease and methods of using the same.
    Type: Grant
    Filed: May 9, 2012
    Date of Patent: April 15, 2014
    Assignee: EIP Pharma, LLC
    Inventor: John Jahangir Alam
  • Patent number: 8697875
    Abstract: The invention provides for compounds that are phosphodiesterase inhibitors. The invention further provides for a method for screening compounds that bind to and modulate a phosphosdiesterase protein. The invention also provides methods for treating conditions associated with accumulated amyloid-beta peptide deposit accumulations by administering a phosphodiesterase-binding compound to a subject.
    Type: Grant
    Filed: June 23, 2011
    Date of Patent: April 15, 2014
    Assignee: The Trustees of Columbia University in the City of New York
    Inventors: Yan Feng, Ottavio Arancio, Shixian Deng, Donald W. Landry
  • Publication number: 20140100231
    Abstract: Compounds of Formula I: are HIV reverse transcriptase inhibitors, wherein R1, R2, RE, L, M and Z are defined herein. The compounds of Formula I and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Application
    Filed: October 7, 2013
    Publication date: April 10, 2014
    Inventors: Kenneth L. Arrington, Christopher Burgey, Robert Gilfillan, Yongxin Han, Mehul Patel, Chun Sing Li, Yaozong Li, Yunfu Luo, Zhiyu Lei
  • Publication number: 20140094466
    Abstract: In alternative embodiments, the invention provides compositions that inhibit the polypeptide SSH-2, or SlingSHot-2, a phosphatase enzyme that regulates actin filaments, and methods for making and using them, including methods comprising administering compositions of the invention to regulate or modify actin filament polymerization by inhibiting SSH-2, where in one embodiment compositions of the invention slow or inhibit F-actin depolymerization and severing. In alternative embodiments, compositions and methods of the invention are used to slow or inhibit cell motility and/or internal remodeling. In alternative embodiments, compositions and methods of the invention are used to slow or inhibit, or reverse, or ameliorate the progression of a cancer or a metastasis or other uncontrolled or unregulated cell growth, and/or Alzheimer's disease.
    Type: Application
    Filed: March 15, 2012
    Publication date: April 3, 2014
    Inventors: Jason H. Haga, Shu Chien, Matt Mui, Marshall J. Levesque, Phillip D. Pham
  • 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
  • Publication number: 20140088110
    Abstract: Compounds of formula (I) a tautomer or stereoisomer thereof, or a salt thereof, wherein ring B and the imidazole to which it is fused, R4, R6 and R7 have the meanings as given in the description and the claims, are effective inhibitors of the Pi3K/Akt pathway.
    Type: Application
    Filed: November 26, 2013
    Publication date: March 27, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GmbH
    Inventors: Swen HÖLDER, Armin ZÜLCH, Thomas BÄR, Thomas MAIER, Astrid ZIMMERMANN, Thomas BECKERS, Volker GEKELER, Hemant JOSHI, Yogesh MUNOT, Umesh BHISE, Sunil CHAVAN, Sachin SHIVATARE, Sarvesh PATEL, Vikas GORE
  • Publication number: 20140080835
    Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2, R3, L, X, Y and Z have defined meanings.
    Type: Application
    Filed: November 12, 2013
    Publication date: March 20, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Jerome Emile Jorges Guillemont, Ludo Edmond Josephine Kennis, Josephus Carolus Mertens, Jacobus Alphonsus Josephus Van Dun, Maria Victorina Francisca Somers, Walter Boudewijn Leopold Wouters
  • Publication number: 20140080834
    Abstract: This invention is directed to the treatment of pain by inhibiting adaptor associated kinase 1 (AAK1). Numerous AAK1 inhibitors are disclosed.
    Type: Application
    Filed: March 6, 2013
    Publication date: March 20, 2014
    Inventors: Thomas Herbert LANTHORN, Katerina SAVELIEVA, Brian ZAMBROWICZ
  • Publication number: 20140080799
    Abstract: Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of casein kinase 1 (e.g., CK1?), casein kinase 2 (CK2), Pim1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of casein kinase 1 (e.g., CK1?), casein kinase 2 (CK2), Pim1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway.
    Type: Application
    Filed: September 20, 2013
    Publication date: March 20, 2014
    Applicant: Jasco Pharmaceuticals, LLC
    Inventors: Carmen M. Baldino, Justin L. Caserta, Chee-Seng Lee, Robert B. Nicewonger, Yvonne L. Flanders, Stephane A. Dumas
  • Patent number: 8674113
    Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, L, M, W, R1, R2, R3, R4, R6, R7, R9, Ra, Rb have meanings given in the description.
    Type: Grant
    Filed: December 8, 2011
    Date of Patent: March 18, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Henning Priepke, Henri Doods, Alexander Heim-Riether, Raimund Kuelzer, Roland Pfau, Klaus Rudolf, Dirk Stenkamp
  • Publication number: 20140073640
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-xL protein.
    Type: Application
    Filed: August 12, 2013
    Publication date: March 13, 2014
    Inventors: Andrew S. Judd, Andrew J. Souers, Zhi-Fu Tao
  • Patent number: 8669289
    Abstract: Methods of treating a subject having, or at risk of having, a myeloproliferative disorder are provided according to embodiments of the present invention which include administering a therapeutically effective amount of an arachidonate 5-lipoxygenase (5-LO) inhibitor to the subject. Combinations of therapeutic agents are administered according to embodiments of the present invention. In some embodiments, two or more 5-LO inhibitors are administered to a subject to treat a myeloproliferative disorder. In further embodiments, at least one 5-LO inhibitor and at least one additional therapeutic agent are administered to a subject to treat a myeloproliferative disorder. Methods of inhibiting leukemia stem cells are provided according to embodiments of the present invention which include contacting leukemia stem cells with an effective amount of an arachidonate 5-lipoxygenase inhibitor.
    Type: Grant
    Filed: April 26, 2010
    Date of Patent: March 11, 2014
    Assignee: The Jackson Laboratory
    Inventor: Shaoguang Li
  • Patent number: 8669251
    Abstract: 8-Fluorophthalazin-1(2h)-one compounds of Formula II where one or two of X1, X2, and X3 are N, are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula II for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Grant
    Filed: November 2, 2012
    Date of Patent: March 11, 2014
    Assignee: Genentech, Inc.
    Inventors: James John Crawford, Daniel Fred Ortwine, BinQing Wei, Wendy B. Young
  • Publication number: 20140066447
    Abstract: The present invention relates to a pharmaceutical formulation comprising the drug 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one in a solid dispersion with a matrix polymer that exhibits low hygroscopicity and high softening temperature, such as copovidone. The invention also relates to a daily pharmaceutical dose of the drug provided by such a formulation. In addition, the invention relates to the use of a matrix polymer that exhibits low hygroscopicity and high softening temperature in solid dispersion with 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one for increasing the bioavailability of the drug.
    Type: Application
    Filed: June 6, 2013
    Publication date: March 6, 2014
    Applicant: Astrazeneca UK, Ltd.
    Inventors: Michael Karl BECHTOLD, Julie Kay CAHILL, Katja Maren FASTNACHT, Kieran James LENNON, Bernd Harald LIEPOLD, Claudia Bettina PACKHAEUSER, Benedikt STEITZ
  • Publication number: 20140066430
    Abstract: The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating Aurora kinase protein activity, thereby influencing various disease states and conditions related to the activities of Aurora kinase proteins. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, processes of preparing compounds of the invention, synthetic intermediates and methods of treatment of conditions related to the activity of Aurora kinase.
    Type: Application
    Filed: October 3, 2013
    Publication date: March 6, 2014
    Applicant: Amgen Inc.
    Inventors: Victor J. CEE, Holly L. DEAK, Bingfan DU, Stephanie D. GEUNS-MEYER, Brian L. HODOUS, Hanh Nho NGUYEN, Philip R. Olivieri, Vinod F. Patel, Karina ROMERO, Laurie Schenkel
  • Publication number: 20140066448
    Abstract: The present invention provides substituted diamino-pyrimidine and substituted diamino-pyridine derivatives of Formula I; wherein X, Y, R1, R2, and Ar are defined herein, that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
    Type: Application
    Filed: March 13, 2012
    Publication date: March 6, 2014
    Applicant: INCYTE CORPORATION
    Inventors: Andrew P. Combs, Yun-Long Li, Song Mei, Eddy W. Yue
  • Publication number: 20140066412
    Abstract: Certain heteroaryl-substituted piperidinyl and piperazinyl urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis).
    Type: Application
    Filed: November 6, 2013
    Publication date: March 6, 2014
    Inventors: J. Guy Breitenbucher, John M. Keith, Mark S. Tichenor, Alison L. Chambers, William M. Jones, Natalie A. Hawryluk, Amy K. Timmons, Jeffrey E. Merit, Mark J. Selerstad
  • Publication number: 20140066434
    Abstract: The invention discloses methods and compositions for treating or preventing Parkinson's disease by administering a compound of Formula (I): or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the variables are defined as herein.
    Type: Application
    Filed: April 6, 2012
    Publication date: March 6, 2014
    Applicant: ARIAD PHARMACEUTICALS, INC.
    Inventor: William C. Shakespeare
  • Publication number: 20140066429
    Abstract: A compound having the structure set forth in Formula (I) and Formula (II): wherein the substituents Y, Z, A, B, R1, R2, R3, R4 and R5 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions associated with a PTEN deficiency that are ameliorated by the inhibition of PARP activity.
    Type: Application
    Filed: August 21, 2013
    Publication date: March 6, 2014
    Applicant: BIOMARIN PHARMACEUTICAL INC.
    Inventors: Daniel Chu, Bing Wang, Ying Feng, Yuqiao Shen, Leonard Edwin Post
  • Publication number: 20140057873
    Abstract: There is provided amino acid ester compounds comprising at least one nitric oxide releasing group, pharmaceutically acceptable salts thereof and compositions thereof. These compounds involve an amino acid side-chain or an amino acid derivative thereof and a nitric oxide releasing group as depicted in the following structures: wherein R1 is either an ethyl or an amino acid side-chain group or an amino acid derivative thereof and R2 is an amino acid side-chain group or an amino acid derivative thereof and n is an integer from 1 to 10.
    Type: Application
    Filed: November 1, 2013
    Publication date: February 27, 2014
    Inventor: Michael Farber
  • Patent number: 8658569
    Abstract: Substituted quinolinones of the formula I in which the variables are defined according to the description, their agriculturally suitable salts, processes and intermediates for preparing the compounds of the formula I, compositions comprising them and their use as herbicides, i.e. for controlling harmful plants, and also a method for controlling unwanted vegetation which comprises allowing a herbicidally effective amount of at least one compound of the formula I to act on plants, their seed and/or their habitat.
    Type: Grant
    Filed: August 22, 2012
    Date of Patent: February 25, 2014
    Assignee: BASF SE
    Inventors: Dschun Song, Julia Major, Johannes Hutzler, Trevor William Newton, Matthias Witschel, William Karl Moberg, Liliana Parra Rapado, Tao Qu, Frank Stelzer, Andree Van Der Kloet, Thomas Seitz, Thomas Ehrhardt, Klaus Kreuz, Klaus Grossmann, Anna Aleksandra Michrowska, Anja Simon, Richard Roger Evans
  • Publication number: 20140051694
    Abstract: Oxazole derivatives are described. The inventive compounds are useful as kinase inhibitors, and may be used in the treatment of cancer, such as prostate cancer, lung cancer, breast cancer, colon cancer, leukemia, CNS cancer, melanoma, ovarian cancer, and renal cancer.
    Type: Application
    Filed: September 24, 2013
    Publication date: February 20, 2014
    Applicant: NEOSOME LIFE SCIENCES, LLC
    Inventors: Laxman S. Desai, Srinivas Chittaboina
  • Publication number: 20140051672
    Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; 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: August 7, 2013
    Publication date: February 20, 2014
    Inventors: Atwood Kim CHEUNG, Donovan Noel CHIN, Natalie DALES, Aleem FAZAL, Timothy Brian HURLEY, John KERRIGAN, Gary O'BRIEN, Lei SHU, Robert SUN, Moo Je SUNG
  • Publication number: 20140051695
    Abstract: The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof where in formula I the variables R1, R2, R3, R4 and R5 are as defined in the claims and where X is C—R6 or N, Y is C—R7 or N, where R6 and R7 are, inter alia, hydrogen, halogen, alkoxy, haloalkoxy and the like. The compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.
    Type: Application
    Filed: August 15, 2013
    Publication date: February 20, 2014
    Inventors: Hervé GENESTE, Michael OCHSE, Karla DRESCHER, Clarissa JAKOB
  • Patent number: 8653076
    Abstract: The invention relates to novel inhibitors of kinases of the general formula (I): in which Q and R1 are defined in the claims, method for preparing such inhibitors, intermediates for preparing such inhibitors and uses of such inhibitors.
    Type: Grant
    Filed: June 20, 2007
    Date of Patent: February 18, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Olaf Prien, Knut Eis, Benjamin Bader, Judith Guenther, Arne Von Bonin
  • Publication number: 20140045826
    Abstract: The invention discloses methods and compositions for treating or preventing neurodegenerative disease by administering a compound of Formula I: or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the variables are defined as herein.
    Type: Application
    Filed: April 6, 2012
    Publication date: February 13, 2014
    Applicant: ARIAD PHARMACEUTICALS, INC.
    Inventors: William C. Shakespeare, Frank G. Haluska