Plural Ring Nitrogens In The Seven-membered Hetero Ring Patents (Class 514/211.08)
  • Patent number: 10048277
    Abstract: A polynucleotide, which is a novel causative gene for cancer, is elucidated, and, based on this finding, provided are a method for detecting the polynucleotide, or a polypeptide encoded by the polynucleotide; a kit and a primer set for the detection; a method for screening an inhibitor of the polypeptide; and a pharmaceutical composition for treating a cancer containing the inhibitor. In the detection method of the present invention, an FGFR3 fusion protein, or a fusion gene encoding the fusion protein, or a TACC3 fusion protein, or a fusion gene encoding the fusion protein, is detected in a sample derived from female genitalia obtained from a subject.
    Type: Grant
    Filed: January 23, 2015
    Date of Patent: August 14, 2018
    Assignee: JAPANESE FOUNDATION FOR CANCER RESEARCH
    Inventor: Kengo Takeuchi
  • Patent number: 9994585
    Abstract: Embodiments of the present invention are directed to methods and dosage forms for treating inflammation and rejection in transplantation injuries with Bryostatin-1, Bryostatin-1 analogs and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: September 30, 2014
    Date of Patent: June 12, 2018
    Assignee: Aphios Corporation
    Inventors: Jonathan Steven Alexander, April C. Carpenter, Trevor Percival Castor
  • Patent number: 9926529
    Abstract: The present invention is based in part on a chemically defined method of generating neural stem cells (NSCs) and dopaminergic (DA) neurons from human pluripotent stem cells (hPSCs). The DA neurons of the invention can be derived from hPSCs and NSCs. The present invention also provides reagents and kits useful for the derivation of neural stem cells and dopaminergic neurons from human pluripotent stem cells.
    Type: Grant
    Filed: April 23, 2013
    Date of Patent: March 27, 2018
    Assignee: International Stem Cell Corporation
    Inventors: Rodolfo Gonzalez, Ibon Garitaonandia, Ruslan Semechkin
  • Patent number: 9782418
    Abstract: The methods, compositions, and kits of the invention are related to the discovery that lestaurtinib reduces levels and pathway activity of an SPOP substrate. Accordingly, described herein are methods and compositions for the use of lestaurtinib in downregulating one or more SPOP substrates or signaling pathway activities thereof in a subject in need thereof.
    Type: Grant
    Filed: December 3, 2014
    Date of Patent: October 10, 2017
    Assignee: Celestra Life Science LLC
    Inventors: Allen J. Lee, Jason J. Lee, David M. Lu, Ruey-Min Lee
  • Patent number: 9738660
    Abstract: The present invention provides a compound of formula (I) or the salt thereof: wherein R is at least one selected from the group consisting of unsubstituted C1-4 alkyl, C1-4 alkyl substituted by C6-18 aryl or —OR1, and —C(?O)Z. The compound is a type-S protein kinase inhibitor, which binds to an ATP-binding site and a substrate-recognition site of a protein kinase simultaneously. The present invention further provides a pharmaceutical composition, which includes a compound of formula (I) or a salt and a pharmaceutically acceptable carrier thereof. The present invention further provides a use of a compound of formula (I) or a salt thereof, which is for the manufacture of a protein kinase inhibitor as a drug.
    Type: Grant
    Filed: January 16, 2015
    Date of Patent: August 22, 2017
    Assignee: National Chiao Tung University
    Inventors: Jinn-Moon Yang, Kai-Cheng Hsu, Tzu-Ying Sung, Shen Rong Lin, Yun-Ming Wang, Kuang-Mei Hsu, Hsin-Ping Lin, Wan-Chun Liu
  • Patent number: 9708347
    Abstract: Disclosed are compounds of Formula G1 (structurally represented): where “RG3” “Rd1” to “Rd4”, “n”, “m”, “p”, “W”, “X”, “Y”, and “Z” are defined herein which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2a receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.
    Type: Grant
    Filed: December 20, 2013
    Date of Patent: July 18, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Michael Man-Chu Lo, Yeon-Hee Lim
  • Patent number: 9682983
    Abstract: The present invention provides small molecule inhibitors of BMP signaling. These compounds may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation. These compounds may also be used to reduce circulating levels of ApoB-100 or LDL and treat or prevent acquired or congenital hypercholesterolemia or hyperlipoproteinemia; diseases, disorders, or syndromes associated with defects in lipid absorption or metabolism; or diseases, disorders, or syndromes caused by hyperlipidemia.
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: June 20, 2017
    Assignees: The Brigham and Women's Hospital, Inc., Dept. of Health and Human Services, National Institutes of Health
    Inventors: Asaf Alimardanov, Gregory D. Cuny, Gurmit Singh Grewal, Arthur Lee, John C. McKew, Agustin H. Mohedas, Min Shen, Xin Xu, Paul B. Yu
  • Patent number: 9630945
    Abstract: The present invention relates to novel compounds of formula (I) (I) that are autotaxin inhibitors, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in the treatment of an ATX-dependent or ATX-mediated disease or condition.
    Type: Grant
    Filed: December 17, 2013
    Date of Patent: April 25, 2017
    Assignee: Novartis AG
    Inventors: Vikki Furminger, Owen Rhys Hughes, Darren Mark Le Grand, Emily Stanley, Christopher Thomson
  • Patent number: 9617230
    Abstract: The invention describes membrane permeable creatine prodrugs, pharmaceutical compositions comprising membrane permeable creatine prodrugs, and methods of treating diseases such as ischemia, heart failure, neurodegenerative disorders and genetic disorders affecting the creatine kinase system comprising administering creatine prodrugs or pharmaceutical compositions thereof. The invention also describes treating a genetic disease affecting the creatine kinase system, such as, for example, a creatine transporter disorder or a creatine synthesis disorder comprising administering creatine prodrugs or pharmaceutical compositions thereof.
    Type: Grant
    Filed: December 21, 2015
    Date of Patent: April 11, 2017
    Assignee: FARMINGTON PHARMA DEVELOPMENT
    Inventor: William F. Brubaker
  • Patent number: 9517238
    Abstract: The invention provides methods of treating allergic inflammatory conditions using an anti-neurotrophin tyrosine kinase receptor 1 (NTRK1)-based therapeutic agent, and related compositions and methods.
    Type: Grant
    Filed: November 6, 2015
    Date of Patent: December 13, 2016
    Assignee: CHILDREN'S HOSPITAL MEDICAL CENTER
    Inventors: Mark Rochman, Marc E. Rothenberg
  • Patent number: 9486440
    Abstract: The present invention provides a method of using indole-ketone or indolidone such as SU4312, SU5416, SU11248 (Sunitinib), or indirubin-3-oxime to treat a neurodegenerative disease or disorder such as Parkinson's disease which is associated with excessive neuronal Nitric Oxide Synthase (nNOS) activity.
    Type: Grant
    Filed: October 25, 2012
    Date of Patent: November 8, 2016
    Assignees: UNIVERSITY OF MACAU, THE HONG KONG POLYTECHNIC UNIVERSITY
    Inventors: Ming Yuen Lee, Yifan Han, Chung Lit Choi, Zaijun Zhang, Wei Cui
  • Patent number: 9255087
    Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.
    Type: Grant
    Filed: November 6, 2014
    Date of Patent: February 9, 2016
    Assignee: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
  • Patent number: 9241941
    Abstract: The present disclosure identifies a novel subtype of follicular lymphoma (FL) characterized by dysregulation of the cyclin/CDK/RB proliferative pathway. This subtype of FL is associated with increased malignancy and mortality, relative to FL which is not associated with cell cycle dysregulation. Accordingly, this disclosure presents novel methods to subtype FL and stratify patient risk by detection of biomarkers associated with RB inactivation. This disclosure further presents novel therapies for the treatment of FL subtyped by inactivation of RB.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: January 26, 2016
    Assignee: MEMORIAL SLOAN-KETTERING CANCER CENTER
    Inventors: Hans Guido Wendel, Elisa Oricchio
  • Patent number: 9150589
    Abstract: The present invention relates to a crystalline form III and a crystalline form IV of N-benzoyl staurosporine. N-benzoyl staurosporine is also known as Midostaurin or PKC412.
    Type: Grant
    Filed: November 29, 2010
    Date of Patent: October 6, 2015
    Assignee: NOVARTIS AG
    Inventor: Ranjit Thakur
  • Patent number: 9101567
    Abstract: Disclosed is a composition comprising a derivative of NDGA and 7-hydroxystaurosporine. The composition can be in a unit dose form or kit. Also disclosed are methods for achieving cytotoxicity, particularly of rapidly dividing cells such as cancer, by administering a composition of the invention. In various embodiments of the invention subjects with cancer achieve prolonged survival and/or diminution in the size of their malignancies and cancer metastasis.
    Type: Grant
    Filed: February 22, 2011
    Date of Patent: August 11, 2015
    Assignee: The Johns Hopkins University
    Inventors: Ru Chih C. Huang, Kotohiko Kimura
  • Patent number: 9085558
    Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.
    Type: Grant
    Filed: November 6, 2014
    Date of Patent: July 21, 2015
    Assignee: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
  • Publication number: 20150073036
    Abstract: Novel NTRK1 fusion molecules, detection reagents, and uses and kits for evaluating, identifying, assessing and/or treating a subject having a cancer are disclosed.
    Type: Application
    Filed: August 29, 2014
    Publication date: March 12, 2015
    Inventors: Matthew J. Hawryluk, Doron Lipson, Vincent A. Miller, Philip James Stephens
  • Publication number: 20150065485
    Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.
    Type: Application
    Filed: November 7, 2014
    Publication date: March 5, 2015
    Inventors: Toshiyuki Akiyama, Kenji Takaya, Makoto Kawai, Yoshiyuki Taoda, Minako Mikamiyama, Kenji Morimoto, Chika Kageyama, Kenji Tomita, Hidenori Mikamiyama, Naoyuki Suzuki
  • Publication number: 20150057267
    Abstract: The invention provides a method for treating viral infections and coinfections through the use of inhibitory agents that prevent a unique viral structural protein motifs from binding to host proteins from the clathrin adaptor proteins family and subsequently preventing viral replication.
    Type: Application
    Filed: December 6, 2012
    Publication date: February 26, 2015
    Applicant: The Board of Trustees of the Leland Stanford Junior university
    Inventors: Shirit Einav, Rina Barouch-Bentov, Gregory Neveu, Amotz Zivav
  • Publication number: 20150050274
    Abstract: The present invention relates to methods and biomarkers for detection and characterization of mature T-cell neoplasias/leukemias (e.g., T-cell prolymphocytic leukemia, Sezary syndrome) in biological samples (e.g., tissue samples, blood samples, plasma samples, cell samples, serum samples).
    Type: Application
    Filed: August 14, 2014
    Publication date: February 19, 2015
    Inventors: Kojo Elenitoba-Johnson, Mark J. Kiel, Thirunavukkarasu Velusamy, Anagh Sahasrabuddhe, Delphine Rolland, Megan Lim
  • Publication number: 20150030572
    Abstract: Drug targets, pathways, kits and methods for treating conditions related to neurodegeneration or ocular disease, are disclosed.
    Type: Application
    Filed: March 11, 2013
    Publication date: January 29, 2015
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Donald J. Zack, Derek S. Welsbie
  • Publication number: 20150017264
    Abstract: The invention provides compositions and methods for the induction of cell death, for example, cancer cell death. Combinations of compounds and related methods of use are disclosed, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells. The disclosed drug combinations can have lower neurotoxicity effects than other compounds and combinations of compounds.
    Type: Application
    Filed: March 6, 2013
    Publication date: January 15, 2015
    Applicants: Vanquish Oncology, Inc., TheBoard of Trustees of the University of Illinois
    Inventors: Paul J. Hergenrother, Rachel C. Botham, Timothy M. Fan, Mark J. Gilbert, Michael K. Handley, Howard S. Roth, Theodore M. Tarasow
  • Publication number: 20150018294
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides for methods and pharmaceutical agents to modulate the activity of Tousled-like kinase (TLK). The invention also provides for methods and pharmaceutical agents to inhibit the activity of Tousled-like kinase to provide increased sensitivity to irradiation (IR) and chemotherapeutic agents. The invention also provides for methods and pharmaceutical agents to increase the activity of Tousled-like kinase to provide increased protection against DNA damaging agents including to irradiation (IR) and chemotherapeutic agents.
    Type: Application
    Filed: February 7, 2013
    Publication date: January 15, 2015
    Inventors: Arrigo DE BENEDETTI, Gulshan SUNAVALA
  • Publication number: 20140356416
    Abstract: Provided herein are novel methods of making liposomally encapsulated drugs using reverse pH gradients and optimizing internal buffer compositions. Further provided herein are liposome compositions including an active pharmaceutical ingredient and uses thereof to treat a variety of diseases (e.g. cancer, inflammatory, neurological and cardiovascular diseases).
    Type: Application
    Filed: June 9, 2014
    Publication date: December 4, 2014
    Inventors: Santosh Kesari, Rajesh Mukthavaram, Milan Makale, Wolf Wrasidlo
  • Publication number: 20140323412
    Abstract: Provided herein are methods of treating or ameliorating hypercholemia or a cholestatic liver disease by administering to an individual in need thereof a therapeutically effective amount of an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating a liver disease, decreasing the levels of serum bile acids or hepatic bile acids, treating or ameliorating pruritis, reducing liver enzymes, or reducing bilirubin comprising administering to an individual in need thereof a therapeutically effective amount of ASBTI or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 30, 2014
    Inventors: Bronislava Gedulin, Michael Grey, Niall O'Donnell
  • Publication number: 20140314882
    Abstract: Combinations of compounds are provided that produce a synergistic effect when administered.
    Type: Application
    Filed: June 27, 2014
    Publication date: October 23, 2014
    Inventors: Frederick P. ROTH, Murat COKOL, Hon Nian CHUA
  • Publication number: 20140314791
    Abstract: The present invention provides methods of treating cancer, particularly cancers that are null or have decreased expression or activity of the Lkb1 gene. Also included are methods of identifying therapeutic targets for the treatment of cancer.
    Type: Application
    Filed: January 4, 2013
    Publication date: October 23, 2014
    Inventors: Kwok-Kin Wong, Yan Liu
  • Patent number: 8865700
    Abstract: Methods for preventing, ameliorating, or reducing dermatological signs of aging are provided which employ cosmetic composition comprising novel active agents that enhance collagen production in the skin.
    Type: Grant
    Filed: December 20, 2012
    Date of Patent: October 21, 2014
    Assignee: Avon Products, Inc.
    Inventors: Uma Santhanam, Permanan Raaj Khusial
  • Publication number: 20140303145
    Abstract: Solid composition comprising (a) an anionic surfactant in combination with a water-soluble and basic polymer, or (b) a cationic surfactant in combination with a water-soluble and acidic polymer, and (c) at least one poorly water-soluble pharmaceutically active ingredient, and solid or liquid dosage forms, especially tablets, coated tablets, capsules or suppositories or aqueous solutions comprising the solid composition. The surfactant/polymer system is soluble in water and solubilises the active ingredient so that good bioavailability with therapeutical quantities may be attained. Aqueous solutions are suitable for nasal, parenteral or ophthalmic treatments.
    Type: Application
    Filed: June 19, 2014
    Publication date: October 9, 2014
    Applicant: NOVARTIS AG
    Inventors: Andreas Ebner, Bruno Galli
  • Publication number: 20140302022
    Abstract: The invention relates to the use of compounds of formula (I) in the treatment of warm-blooded animal target of VEGF-driven angiogenic diseases, methods of use of said compounds in the treatment of said diseases in a warm-blooded animal, especially a human, pharmaceutical compositions comprising said compounds for the treatment of said diseases and said compounds for use in the treatment of said diseases.
    Type: Application
    Filed: October 31, 2012
    Publication date: October 9, 2014
    Applicant: NOVARTIS AG
    Inventor: Christian Rene Schnell
  • Publication number: 20140303146
    Abstract: The present invention relates to a method of treating a warm-blooded animal, especially a human, having Mixed Lineage Leukemia (MLL rearranged ALL) comprising administering to said animal a therapeutically effective amount of a staurosporine derivative, especially PKC412 or a pharmaceutically acceptable salt thereof, alone or in combination with further therapeutic measures, for example, those defined herein; to the use of a staurosporine derivative for the preparation of a medicament for the treatment of MLL rearranged ALL; and to a commercial package comprising a staurosporine derivative together with instructions for its use in the treatment of MLL rearranged ALL.
    Type: Application
    Filed: June 23, 2014
    Publication date: October 9, 2014
    Applicants: DANA-FARBER CANCER INSTITUTE INC., NOVARTIS AG
    Inventors: James Douglas Griffin, Doriano Fabbro
  • Publication number: 20140302988
    Abstract: The invention relates to novel compounds of the formula (I) in which X, Y and CKE have the meanings given above, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides. The invention also relates to selective herbicidal compositions comprising, firstly, the 1,2,4-triazolyl-substituted ketoenols and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to the boosting of the action of crop protection compositions comprising, in particular, 1,2,4-triazolyl-substituted ketoenols, through the addition of ammonium salts or phosphonium salts and optionally penetrants, to the corresponding compositions, to processes for producing them and to their application in crop protection as insecticides and/or acaricides and/or for preventing unwanted plant growth.
    Type: Application
    Filed: August 10, 2012
    Publication date: October 9, 2014
    Applicant: Bayer Intellectual Property GMBH
    Inventors: Wolfgang Gienckle, Stefan Lehr, Reiner Fischer, David Stephen Lindell, Isolde Haeuser-Hahn, Ines Heinemann, Elmar Gatzweiler, Christopher Hugh Rosinger, Angela Becker, Arnd Voerste, Ulrich D.I. Goergens
  • Publication number: 20140286938
    Abstract: The present invention relates to spiroketal compounds that are useful in methods of treating or preventing protozoal infections, parasitic infections, bacterial infections, cell proliferative disorders and anti inflammatory disorders. The spiroketal compounds are also useful as immunosuppressive agents, and also in methods of controlling pests.
    Type: Application
    Filed: March 21, 2014
    Publication date: September 25, 2014
    Applicant: EcoBiotics Ltd
    Inventors: Paul Warren Reddell, Victoria Anne Gordon
  • Patent number: 8840923
    Abstract: Slow-release excipients which comprise an association of at least one glycogen and at least one alginate with an alkaline-earth metal salt are useful for the preparation of slow-release pharmaceutical formulations.
    Type: Grant
    Filed: December 23, 2008
    Date of Patent: September 23, 2014
    Assignee: Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
    Inventors: Vincenzo Russo, Elisa Liberati, Nicola Cazzolla, Leonardo Marchitto, Lorella Ragni
  • Publication number: 20140275032
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, A, X1, X2, X3, X4, X5, X6, Y, Z, G, R1a, R2a, R1b, R2b, R3, R4, R5 and R6 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: Genentech, Inc.
    Inventors: Benjamin Fauber, Olivier Rene, Monique Bodil van Niel, Stuart Ward
  • Patent number: 8809318
    Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more disease associated with the central nervous system using such compounds or pharmaceutical compostions.
    Type: Grant
    Filed: November 11, 2009
    Date of Patent: August 19, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Zhaoning Zhu, William J. Greenlee, Hongmei Li, Monica L. Vicarel, Jun Qin, Pawan Kumar Dhondi, Xianhai Huang, Anandan Palani, Xiaoxiang Liu, Zhong-Yue Sun, Hubert B. Josien, Ruo Xu, David James Cole, Duane A. Burnett, Chad E. Bennett, Troy McCracken, Malcolm MacCoss
  • Patent number: 8802099
    Abstract: Disclosed are methods to treat allergic conditions, including pulmonary and non-pulmonary conditions, in a subject by administering a composition that inhibits Pim kinase. Also disclosed are methods to treat allergic conditions in a subject by administering a composition that induces expression of Runx3.
    Type: Grant
    Filed: November 10, 2011
    Date of Patent: August 12, 2014
    Assignee: National Jewish Health
    Inventors: Erwin W. Gelfand, Meiqin Wang
  • Patent number: 8778927
    Abstract: The invention provides methods for modulating, e.g., antagonizing, the activity of the Hedgehog signaling pathway, and for treating Hedgehog related disorders such as cancers (e.g., medulloblastoma). In particular, the invention provides methods for inhibiting aberrant growth states resulting from phenotypes such as Ptch loss-of-function, Hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function by administering to a mammal combinations of Smoothened inhibitors (e.g., a compound of Formula I, Formula II, or Formula III, or any of the compounds listed herein or incorporated by reference) and cholesterol biosynthesis pathway inhibitors (e.g., statins), Gli inhibitors, and/or Phosphatidylinositol 3-kinase (PI3K) inhibitors.
    Type: Grant
    Filed: September 28, 2009
    Date of Patent: July 15, 2014
    Assignee: Novartis AG
    Inventors: Marion Dorsch, John E. Monahan, Michael Patrick Morrissey, Shifeng Pan, Juliet Williams
  • Patent number: 8771682
    Abstract: The present invention relates generally to methods and compositions for reducing Interleukin-4 or Interleukin-13 signaling, in particular to treat asthma and atopic dermatitis. The inventors have found that Rac/PAK mediated endocytosis of the ligand bound type I (IL-4R with the chains IL-4Ra and IL-2-Rg) and/or type II receptor (IL-13R with the chains IL-4Ra and IL-13Ra1) is needed for the IL-4 and/or IL-13 mediated activation of downstream signalling events including phosphorylation of Stat family transcrition factors. These discoveries enable new methods of screening compounds that modulate Interleukin-4 and Interleukin-13 signalling, as well as new methods for treating conditions characterized by increased Interleukin-4 and Interleukin-13 levels. These conditions include inflammatory conditions, asthma bronchiale, atopic dermatitis, allergies, atopic syndromes, allergic rhinitis, and th2-induced conditions.
    Type: Grant
    Filed: April 26, 2012
    Date of Patent: July 8, 2014
    Assignee: Technische Universtität Dresden
    Inventors: Christian Bökel, Thomas Weidemann
  • Publication number: 20140186417
    Abstract: An aliphatic polyester polymer for stent coating is described.
    Type: Application
    Filed: February 20, 2014
    Publication date: July 3, 2014
    Applicant: Abbott Cardiovascular Systems Inc.
    Inventors: O. Mikael Trollsas, Lothar W. Kleiner, Syed F.A. Hossainy
  • Publication number: 20140187510
    Abstract: The present invention is directed toward a method of treating a subject for a condition mediated by aberrant Wnt/?-catenin signaling by selecting a subject with a condition mediated by aberrant Wnt/?-catenin signaling and administering to the selected subject a compound selected from the group consisting of those set forth in Table 1, Table 2, and a pharmaceutically acceptable salt thereof. A method of similarly modulating the Wnt/?-catenin pathway in a subject is also discussed.
    Type: Application
    Filed: July 11, 2013
    Publication date: July 3, 2014
    Applicants: THE GENERAL HOSPITAL CORPORATION, MASSACHUSETTS INSTITUTE OF TECHNOLOGY, UNIVERSITY OF WASHINGTON THROUGH ITS CENTER FOR CENTER FOR COMMERCIALIZATION
    Inventors: Randall T. Moon, Travis L. Biechele, Nathan D. Camp, Stephen Haggarty, Daniel Fass
  • Publication number: 20140179677
    Abstract: A novel therapeutic agent for ectopic pregnancy having a therapeutic effect for ectopic pregnancy, especially unruptured ectopic pregnancy, and a novel method of screening a therapeutic agent for ectopic pregnancy are disclosed. The therapeutic agent for ectopic pregnancy contains as an effective ingredient a suppressor of brain-derived neurotrophic factor (BDNF) and/or of brain-derived neurotrophic factor receptor (TrkB). The method of screening a therapeutic agent for ectopic pregnancy includes measuring the kinase activity of TrkB in the presence of a test substance and the kinase activity of TrkB in the absence of the test substance; and selecting the test substance which decreases the kinase activity of TrkB.
    Type: Application
    Filed: December 28, 2011
    Publication date: June 26, 2014
    Applicant: AKITA UNIVERSITY
    Inventor: Kazuhiro Kawamura
  • Publication number: 20140147415
    Abstract: The present invention relates to the treatment of mastocytosis, and in particular indolent forms of mastocytosis (including smoldering systemic, indolent systemic and cutaneous mastocytosis), comprising administration of a tyrosine kinase inhibitor or a mast cell inhibitor, especially masitinib or a pharmaceutically acceptable salt thereof, in particular in an appropriate dosage regimen.
    Type: Application
    Filed: November 3, 2011
    Publication date: May 29, 2014
    Applicant: AB SCIENCE
    Inventors: Alain Moussy, Jean-Pierre Kinet
  • Patent number: 8729065
    Abstract: Described are crystalline forms of the pharmaceutical compound “[9S-(9?,10?,12?)]-5,16-Bis[(ethylthio)methyl]-2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-9,12-epoxy-1H-diindolo[1,2,3-fg:3?,2?,1?-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid methyl ester”, as well as methods for their use and preparation.
    Type: Grant
    Filed: January 3, 2011
    Date of Patent: May 20, 2014
    Assignee: Cephalon, Inc.
    Inventors: Michael Harold Rock, Heidi Lopez De Diego, Kim Lasse Christensen, Ole Nielsen, Anders Buur, Mark Howells
  • Patent number: 8722663
    Abstract: The present invention provides a novel compound having an excellent antitumor effect. The compound of the present invention is represented by the following general formula (1) wherein R1 and R2 are aryl or the like; A is lower alkylene; Ring X is optionally substituted arylene; E is bond or lower alkenylene; Ring Y is optionally substituted heterocycloalkylene containing one or more nitrogen atoms, one of which is attached to the adjacent carbonyl group; G is —NH-G2-, —N(lower alkyl)-G2-, —NH—CH2-G2-, —N(lower alkyl)-CH2-G2- or —CH2-G2-, [wherein G2 binds to R2, G2-R2 is bond-R2, phenylene-G3-R2, phenylene-G4-O—R2, phenylene-G5-NH—R2, phenylene-G6-N(lower alkyl)-R2 or quinolinediyl-O—R2, the phenylene of said phenylene-containing groups being optionally substituted with one or more substituents; G3-R2 is —O-lower alkylene-R2 or the like; G4-O— is lower alkylene-O— or the like; G5 is lower alkylene; G6 is lower alkylene].
    Type: Grant
    Filed: January 28, 2011
    Date of Patent: May 13, 2014
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Hideki Takasu, Shigekazu Fujita, Shinya Ohtsuka, Toshiyuki Hirose, Yosuke Sato, Satoshi Yamada, Keisuke Miyajima, Koji Sakai, Yutaka Kojima, Kazuo Sekiguchi, Yasuo Yanagihara, Takashi Suzuki, Hideo Tanaka, Kazuhisa Sugiyama, Mitsuhiro Okuno, Takumi Sumida
  • Patent number: 8722664
    Abstract: Spontaneously dispersible N-benzoyl-staurosporine compositions are disclosed for oral administration having high bioavailability levels and reduced variability of bioavailability levels of N-benzoyl-staurosporine, as well as their preparation and use in medical treatment.
    Type: Grant
    Filed: October 15, 2013
    Date of Patent: May 13, 2014
    Assignee: Novartis AG
    Inventors: Graham Paul Matthews, Barbara Haeberlin
  • Patent number: 8710216
    Abstract: The invention relates to a new crystalline form II of N-benzoyl-staurosporine; compositions containing the same; processes for the preparation thereof; and the use of crystalline form II of of N-benzoyl-staurosporine in diagnostic methods or therapeutic treatment of warm-blooded animals, especially humans. The invention relates to the amorphous forms of N-benzoyl-staurosporine; compositions containing the same; processes for the preparation thereof; and the use of amorphous N-benzoyl-staurosporine in diagnostic methods or therapeutic treatment of warm-blooded animals, especially humans.
    Type: Grant
    Filed: May 15, 2012
    Date of Patent: April 29, 2014
    Assignee: Novartis AG
    Inventors: Pascale Hoehn, Bernd Koch, Michael Mutz
  • Patent number: 8685960
    Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and the use of these compounds and other heteroaryl substituted quinolinone derivatives for the treatment of hyperaldosteronism and/or disorders or diseases that are mediated by 11 ?-hydroxylase (CYP11 B1).
    Type: Grant
    Filed: May 5, 2009
    Date of Patent: April 1, 2014
    Assignee: Elexopharm GmbH
    Inventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
  • Patent number: 8685433
    Abstract: The present invention provides an absorbable coating for an implantable device and the methods of making and using the same.
    Type: Grant
    Filed: March 31, 2010
    Date of Patent: April 1, 2014
    Assignee: Abbott Cardiovascular Systems Inc.
    Inventors: Lothar W. Kleiner, Syed F. A. Hossainy, Mikael Trollsas, Stephen D. Pacetti
  • Publication number: 20140057897
    Abstract: The present invention relates to a method of treating a warm-blooded animal, especially a human, having Mixed Lineage Leukemia (MLL rearranged ALL) comprising administering to said animal a therapeutically effective amount of a staurosporine derivative, especially PKC412 or a pharmaceutically acceptable salt thereof, alone or in combination with further therapeutic measures, for example, those defined herein; to the use of a staurosporine derivative for the preparation of a medicament for the treatment of MLL rearranged ALL; and to a commercial package comprising a staurosporine derivative together with instructions for its use in the treatment of MLL rearranged ALL.
    Type: Application
    Filed: October 31, 2013
    Publication date: February 27, 2014
    Inventors: James Douglas Griffin, Doriano Fabbro