Nitrogen Bonded Directly To The 1,3-diazine At 2-position By A Single Bond Patents (Class 514/275)
  • Materials and methods for suppressing and/or treating neurofibroma and related tumors
    Patent number: 8933082
    Abstract: Germline mutations in the NF1 tumor suppressor gene cause Von Recklinghausen's neurofibromatosis type 1 (NF1), a common genetic disorder of the nervous system characterized by plexiform neurofibroma development. Using adoptive transfer of hematopoietic cells, we establish that NF1 heterozygosity of bone marrow derived cells in the tumor microenvironment is sufficient to allow neurofibroma progression in the context of Schwann cell nullizygosity. Further, genetic or pharmacologic attenuation of the c-kit signaling pathway in hematopoietic cells greatly diminishes neurofibroma initiation and progression. These studies identify haploinsufficient hematopoietic cells and the c-kit receptor as therapeutic targets for preventing plexiform neurofibromas and implicate mast cells as critical mediators of tumor initiation.
    Type: Grant
    Filed: September 20, 2013
    Date of Patent: January 13, 2015
    Assignee: Indiana University Research and Technology Corp.
    Inventors: D Wade Clapp, David Ingram, Feng-Chun Yang
  • 1-aza-bicyclo[3.3.1]nonanes
    Patent number: 8933090
    Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I); wherein the substituents are as defined in the specification, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them. Formula (I), wherein A represents O or N(R1); Y represents a group of formula, or wherein the left bond is attached to the A group and the right bond is attached to the R group; R represents a substituted or unsubstituted C5-C10aryl, substituted or unsubstituted hetero-C5-C10aryl, a group N(R1)(R4), or a group N(R2)(CHP3R4); R represent a hydrogen, C1-C4alkyl, or CF3; R2 represents hydrogen, C1-C4alkyl, or CF3; R3 represents hydrogen, C1-C4alkyl, or CF3; R4 represents a substituted or unsubstituted C5-C10 aryl or a substituted or unsubstituted C5-C10heteroaryl; in free base or acid addition salt form.
    Type: Grant
    Filed: October 19, 2010
    Date of Patent: January 13, 2015
    Assignee: Novartis AG
    Inventors: Dominik Feuerbach, Werner Müller, Bernard Lucien Roy, Thomas J. Troxler, Konstanze Hurth, Mathias Frederiksen
  • Methods involving PDGFRBETA inhibitors
    Patent number: 8933037
    Abstract: The invention refers to PDGFRbeta inhibitor for use in the antiproliferative treatment of T-cell lymphoma, in particular NHL, ALCL and PTCL.
    Type: Grant
    Filed: September 28, 2010
    Date of Patent: January 13, 2015
    Assignee: Medizinische Universitat Wien
    Inventors: Lukas Kenner, Daniela Laimer
  • Inhibitors of Protein Kinases
    Publication number: 20150011576
    Abstract: The present invention relates to inhibitors of cyclin-dependent kinases and therapeutic applications thereof. Furthermore, the invention relates to methods of preventing and/or treating any type of pain, inflammatory disorders, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases and neurodegenerative diseases comprising the administration of an effective amount of at least one inhibitor of cyclin-dependent kinases.
    Type: Application
    Filed: September 22, 2014
    Publication date: January 8, 2015
    Inventors: Heike Schauerte, Hans Allgeier, Michael A. Pleiss, Martin Augustin, Gisela Peraus, Gabriele Stumm, Philipp Wabnitz
  • MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
    Publication number: 20150011546
    Abstract: Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
    Type: Application
    Filed: February 11, 2013
    Publication date: January 8, 2015
    Inventors: Brian K. Albrecht, James Edmund Audia, Andrew S. Cook, Les A. Dakin, Martin Duplessis, Victor S. Gehling, Jean-Christophe Harmange, Christopher G. Nasveschuk, Rishi G. Vaswani
  • PHENYLIMIDE-CONTAINING BENZOTHIAZOLE DERIVATIVE OF ITS SALT AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
    Publication number: 20150011528
    Abstract: Provided is a phenylimide-containing benzothiazole derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The phenylimide-containing benzothiazole derivative or its pharmaceutically acceptable salt can selectively inhibit the protein-protein interaction between KRS and a laminin receptor (LR), thereby inhibiting migration of cancer cells. Therefore, the phenylimide-containing benzothiazole derivative or its pharmaceutically acceptable salt may be usefully applied for preventing or treating the diseases associated with cancer cell metastasis.
    Type: Application
    Filed: September 21, 2012
    Publication date: January 8, 2015
    Applicant: YUHAN CORPORATION
    Inventors: Youn Hur, Dong-Hyun Kim, Eun-Kyung Kim, Jin-Hwi Park, Jae-Eun Joo, Ho-Woong Kang, Se-Woong Oh, Dong-Kyun Kim, Kyoung-Kyu Ahn
  • METHODS AND COMPOSITIONS FOR MODULATING IRE1, SRC, AND ABL ACTIVITY
    Publication number: 20150011575
    Abstract: Disclosed herein are, inter alia, compositions for modulating Ire1, Src, or Abl, methods for identifying modulating activity in test compounds, and methods for treating diseases caused by the activity or inactivity of Ire1, Src, or Abl.
    Type: Application
    Filed: July 2, 2014
    Publication date: January 8, 2015
    Inventors: Peter Walter, Alexei Korennykh, Kevan M. Shokat, Chao Zhang, Janet Finer-Moore, Robert Stroud, Pascal Egea, Andrei Korostelev, Arvin Dar, Sebastian Bernales
  • Pesticidal Arylpyrrolidines
    Publication number: 20150011553
    Abstract: The invention is directed to arylpyrrolidines compounds which exhibit excellent insecticidal efficacy and which may be used as in the agrochemical field or in the field of veterinary medicine. The compounds are represented by formula (I): wherein the respective substituents are defined in the specification.
    Type: Application
    Filed: July 3, 2014
    Publication date: January 8, 2015
    Inventors: Ulrich GÖRGENS, Jun Mihara, Tetsuya Murata, Daiei Yamazaki, Yasushi Yoneta, Koichi Araki, Norio Sasaki, Kei Domon, Mamoru Hatazawa, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya
  • Method for Improving Water Solubility of Slightly Soluble Substance
    Publication number: 20150010638
    Abstract: It is an object of the present invention to provide a method for improving the solubility of a poorly-soluble substance, which is capable of increasing the solubility of substantially all poorly-soluble substances. This is a method comprising coating the surface of a poorly-soluble substance particle with microparticles of a calcium compound such as calcium phosphate or calcium carbonate, and at least one selected from a pH adjuster and a surfactant, by applying mechanical energy thereto.
    Type: Application
    Filed: February 21, 2013
    Publication date: January 8, 2015
    Inventors: Shuji Sakuma, Keiichiro Kikukawa, Ryosuke Miyasaka
  • Aqueous Suspensions of TMC278
    Publication number: 20150010637
    Abstract: This invention concerns pharmaceutical compositions for administration via intramuscular or subcutaneous injection, comprising micro- or nanoparticles of the NNRTI compound TMC278, suspended in an aqueous pharmaceutically acceptable carrier, and the use of such pharmaceutical compositions in the treatment and prophylaxis of HIV infection.
    Type: Application
    Filed: September 23, 2014
    Publication date: January 8, 2015
    Inventors: Lieven Elvire Colette Baert, Willie Albert Maria Carlo Dries, Laurent Bruno Schueller, Marc Karel Jozef Francois, Peter Jozef Maria Van Remoortere
  • COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF PARASITIC DISEASES
    Publication number: 20150011522
    Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a Plasmodium parasite, such as malaria.
    Type: Application
    Filed: September 22, 2014
    Publication date: January 8, 2015
    Applicants: IRM LLC, Novartis AG
    Inventors: Arnab Kumar Chatterjee, Advait Suresh Nagle, Prasuna Paraselli, Ravinder Reddy Kondreddi, Seh Yong Leong, Pranab Kumar Mishra, Robert Joseph Moreau, Jason Thomas Roland, Wei Lin Sandra Sim, Oliver Simon, Liying Jocelyn Tan, Bryan KS Yeung, Bin Zou, Venkatataiah Bollu
  • Aminopyrimidine kinase inhibitors
    Patent number: 8927525
    Abstract: Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of CK1, CK1?1, CK1?2, CK1?3, CK2, Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, the AKT 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 CK1, CK1?1, CK1?2, CK1?3, CK2, Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, the AKT pathway, and/or the mTOR pathway.
    Type: Grant
    Filed: October 24, 2012
    Date of Patent: January 6, 2015
    Assignee: Jasco Pharmaceuticals, LLC
    Inventors: Carmen M. Baldino, Justin L. Caserta, Chee-Seng Lee, Stephane A. Dumas, Yvonne L. Flanders
  • Pyrimidine derivatives
    Patent number: 8927547
    Abstract: The invention provides novel pyrimidine derivatives of formula I, to methods of preparing such compounds, to pharmaceutical compositions containing such compounds, and to methods for using such compounds in treatment of diseases including cancer; wherein R1, R2, R3, R4, R5, L, A, D, E, Z, and Y are as defined in the specification.
    Type: Grant
    Filed: May 20, 2011
    Date of Patent: January 6, 2015
    Assignee: Noviga Research AB
    Inventors: Marita Högberg, Tommy Johansson, Emma Dahlstedt, Olof Smitt
  • Adamantyl benzamide derivatives
    Patent number: 8927549
    Abstract: Embodiments of the present invention provide adamantyl benzamide derivatives and pharmaceutical compositions comprising adamantyl benzamide derivatives. Methods of use of such compounds and compositions to modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) in a subject are also provided.
    Type: Grant
    Filed: November 17, 2009
    Date of Patent: January 6, 2015
    Assignee: High Point Pharmaceuticals, LLC
    Inventors: Dharma Rao Polisetti, Suparna Gupta, Soren Ebdrup
  • PYRIMIDINE-2,4-DIAMINE DERIVATIVES AS KINASE INHIBITORS
    Publication number: 20150005281
    Abstract: The present invention relates to compounds of formula (I) wherein X, R, Y0, T0A, T0B 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 and their use as medicaments.
    Type: Application
    Filed: December 20, 2012
    Publication date: January 1, 2015
    Inventors: Andrew Hobson, Glynn Addison, Nigel Ramsden, John Harrison
  • QUINOLONE COMPOUND
    Publication number: 20150005287
    Abstract: The present invention provides a compound represented by the formula (I) wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R1 is (1) cyclopropyl optionally substituted by to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R2 is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R3 is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infection such as Clostridium difficile-associated diarrhea.
    Type: Application
    Filed: February 28, 2014
    Publication date: January 1, 2015
    Inventors: Mamuti ABUDUSAIMI, Fangguo YE, Jiangqin SUN, Hisashi MIYAMOTO, Jay-Fei CHENG, Daisuke OKA
  • 1,5-NAPHTHYRIDINE DERIVATIVES AND MELK INHIBITORS CONTAINING THE SAME
    Publication number: 20150005302
    Abstract: The present invention directs a compound represented by formula (I).
    Type: Application
    Filed: December 21, 2012
    Publication date: January 1, 2015
    Inventors: Yo Matsuo, Shoji Hisada, Yusuke Nakamura, Feryan Ahmed, Joel R. Walker, Raymond Huntley
  • DISUBSTITUTED 5-FLUORO PYRIMIDINE DERIVATIVES CONTAINING A SULFOXIMINE GROUP
    Publication number: 20150005329
    Abstract: The present invention relates to disubstituted 5-fluoro pyrimidine derivatives containing a sulfoximine group of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).
    Type: Application
    Filed: September 13, 2012
    Publication date: January 1, 2015
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Ulrich Lücking, Dirk Kosemund, Arne Scholz, Philip Lienau, Gerhard Siemeister, Ulf Bömer, Rolf Bohlmann
  • INTERVENTIONAL MEDICAL DEVICE AND MANUFACTURING METHOD THEREOF
    Publication number: 20150004207
    Abstract: An interventional medical device and manufacturing method thereof, the interventional medical device comprising a stent body (1); the stent body (1) is provided with a drug releasing structure on the surface, the drug in the drug releasing structure being a drug for inhibiting adventitial fibroblast proliferation. When the interventional medical device is implanted into a human body, the drug for inhibiting the adventitial fibroblast proliferation can be slowly released into vessel wall cells in contact with the stent body (1), thus inhibiting the proliferation of the adventitial fibroblasts, promoting vascular compensatory expansion, and reducing the incidence rate of instent restenosis.
    Type: Application
    Filed: January 17, 2012
    Publication date: January 1, 2015
    Applicant: SHANGHAI MICROPORT MEDICAL (GROUP) CO., LTD.
    Inventors: Xu Cai, Dadong Zhang, Yan Hu, Peng Huang, Junfei Li, Chengyun Yue, Zhirong Tang, Qiyi Luo
  • INDAZOLE DERIVATIVES
    Publication number: 20150005232
    Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, and R6 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating obesity and related diseases, disorders, and conditions associated with MetAP2.
    Type: Application
    Filed: February 28, 2013
    Publication date: January 1, 2015
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Zacharia Cheruvallath, Philip Erickson, Jun Feng, Mallareddy Komandla, John David Lawson, Christopher McBride, Joanne Miura, Sean Murphy, Mingnam Tang, Huong-Thu Ton-Nu
  • 2,4-Pyrimidinediamine Compounds and Their Uses
    Publication number: 20150005297
    Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
    Type: Application
    Filed: September 12, 2014
    Publication date: January 1, 2015
    Applicant: RIGEL PHARMACEUTICALS, INC.
    Inventors: Rajinder Singh, Ankush Argade, Donald Payan, Susan Molineaux, Sacha Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander Rossi
  • 5-Membered Heterocyclic Amides And Related Compounds
    Publication number: 20150005293
    Abstract: 5-Membered heterocyclic amides and related compounds are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
    Type: Application
    Filed: September 9, 2014
    Publication date: January 1, 2015
    Inventors: Hongbin Li, Jun Yuan, Rajagopal Bakthavatchalam, Kevin J. Hodgetts, Qin Guo, Scott M. Capitosti, Jianmin Mao, David J. Wustrow
  • Substituted-1,3,8-triazaspiro[4.5]decane-2,4-diones
    Patent number: 8921555
    Abstract: The present invention relates to substituted 1,3,8-triazaspiro[4.5]decame-2,4-diones useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
    Type: Grant
    Filed: June 7, 2010
    Date of Patent: December 30, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joan M. Pierce, Jeffrey J. Hale, Shouwu Miao, Petr Vachal
  • NOVEL METHODS
    Publication number: 20140378454
    Abstract: The present invention relates to the field of methods for providing components of pharmaceutical compositions comprising poorly water-soluble drugs. In particular the present invention relates to methods for providing stable, amorphous hybrid nanoparticles, comprising at least one protein kinase inhibitor and at least one polymeric stabilizing and matrix-forming component, useful in pharmaceutical compositions.
    Type: Application
    Filed: January 11, 2013
    Publication date: December 25, 2014
    Applicant: XSPRAY MICROPARTICLES AB
    Inventors: Magnus Brisander, Mustafa Demirbüker, Gérald Jesson, Martin Malmsten, Helene Dérand
  • Fused Bicyclic Oxazolidinone CETP Inhibitor
    Publication number: 20140378493
    Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
    Type: Application
    Filed: September 8, 2014
    Publication date: December 25, 2014
    Inventors: Pengcheng Patrick Shao, Wanying Sun, Revathi Reddy Katipally, Petr Vachal, Feng Ye, Jian Liu, Deyou Sha
  • 4-SUBSTITUTED-(3-SUBSTITUTED-1H-PYRAZOLE-5-AMINO)-PYRIMIDINE DERIVATIVES HAVING ACTIVITY OF INHIBITING PROTEIN KINASE AND USE THEREOF
    Publication number: 20140378488
    Abstract: Provided are derivatives substituted by urea associated with 4-substituted-(3-substituted-1H-pyrazole-5-amino)-pyrimidine-2-amino of formula (I), wherein these compounds may selectively regulate or inhibit an information transmission process controlled by natural or variant tyrosine kinase. Also provided are preparation methods and uses of the compounds.
    Type: Application
    Filed: September 5, 2011
    Publication date: December 25, 2014
    Applicant: ZHEJIANG HISUN PHARMACEUTICAL CO., LTD.
    Inventors: Yili Ding, Xuan Yang, Qingyan Yan, Hua Bai, Lifeng Cai, Kenneth Smith, Jian Chai
  • Compositions and Method for Hair Loss Prevention
    Publication number: 20140377384
    Abstract: The invention encompasses a formulation for hair loss prevention comprising a mixture of water and at least one nonpolar aprotic organic solvent and at least one hair loss preventive ingredient known to inhibit the hormonal mechanism underlying androgenetic hair loss and methods of using the same.
    Type: Application
    Filed: September 14, 2014
    Publication date: December 25, 2014
    Inventor: Giuseppe Trigiante
  • Histone Deacetylase 6 Selective Inhibitors for the Treatment of Bone Disease
    Publication number: 20140378385
    Abstract: This invention relates to methods for treating bone disease associated with osteoclast activation using HDAC6 selective inhibitors, e.g., small molecule inhibitors such as reverse amide compounds.
    Type: Application
    Filed: July 20, 2012
    Publication date: December 25, 2014
    Applicant: THE GENERAL HOSPITAL CORPORATION
    Inventors: Noopur Raje, Loredana Santo
  • METHODS FOR TREATING VASCULAR LEAK SYNDROME
    Publication number: 20140378445
    Abstract: Disclosed are methods for treating Vascular Leak Syndrome. Further disclosed are methods for treating vascular leakage due to inflammatory diseases, inter alia, sepsis, lupus, inflammatory bowel disease. Yet further disclosed are methods for treating renal cell carcinoma and melanoma. Still further disclosed are methods for reducing metastasis of malignant cells and/or preventing the proliferation of carcinoma cells via spreading due to vascular leakage.
    Type: Application
    Filed: December 21, 2012
    Publication date: December 25, 2014
    Inventors: Robert Shalwitz, Kevin G. Peters
  • Amino-derivatives as novel inhibitors of histone deacetylase
    Patent number: 8916554
    Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
    Type: Grant
    Filed: July 22, 2013
    Date of Patent: December 23, 2014
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Patrick René´ Angibaud, Kristof Van Emelen, Virginie Sophie Poncelet, Bruno Roux
  • BICYCLIC SULFONAMIDE COMPOUNDS AS SODIUM CHANNEL INHIBITORS
    Publication number: 20140371201
    Abstract: The present invention provides compounds of Formula I, and pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav1.7. The compounds are useful for the treatment of diseases associated with the activity of sodium channels such as pain disorders and itch. Also provided are pharmaceutical compositions containing compounds of the present invention.
    Type: Application
    Filed: June 11, 2014
    Publication date: December 18, 2014
    Inventors: Matthew WEISS, Alessandro BOEZIO, Christiane BOEZIO, John R. BUTLER, Margaret Yuhua CHU-MOYER, Erin F. DIMAURO, Thomas DINEEN, Russell GRACEFFA, Angel GUZMAN-PEREZ, Hongbing HUANG, Charles KREIMAN, Daniel LA, Isaac E. MARX, Benjamin Charles MILGRIM, Hanh Nho NGUYEN, Emily PETERSON, Karina ROMERO, Brian SPARLING
  • Tear Film Stability
    Publication number: 20140370060
    Abstract: The present invention relates to a method of stabilising a tear film in an individual having an ocular surface inflammatory disorder by providing a compound to an ocular surface of the individual to reduce the synthesis of a cholesterol by a meibum-producing tissue.
    Type: Application
    Filed: February 1, 2013
    Publication date: December 18, 2014
    Inventors: Kenneth Gek-Jin Ooi, Stephanie Louise Watson
  • METHOD OF INHIBITING DYRK1B
    Publication number: 20140371251
    Abstract: The present invention relates to a DYRK1B inhibitor for use in the treatment of cancer, wherein in said cancer and/or in cells of said cancer the hedgehog signaling pathway is activated, and in particular the activation of the hedgehog signaling pathway is independent of signaling by the G protein-coupled receptor Smoothened.
    Type: Application
    Filed: June 18, 2014
    Publication date: December 18, 2014
    Applicant: 4SC DISCOVERY GMBH
    Inventors: Fritz ABERGER, Wolfgang GRUBER, Johann LEBAN, Hella KOHLHOF, Daniel VITT, Roland BAUMGARTNER
  • 1-H-Pyrrolo[2,3-b]Pyridine Derivatives
    Publication number: 20140371215
    Abstract: 1H-Pyrrolo[2,3-b]pyridine compounds are inhibitors of cell proliferation/cell vitality and can be employed for the treatment of tumours.
    Type: Application
    Filed: August 13, 2014
    Publication date: December 18, 2014
    Applicant: MERCK PATENT GMBH
    Inventors: Timo HEINRICH, Margarita WUCHERER-PLIETKER, Hans-Peter BUCHSTALLER
  • Methods Of Treating Dyskinesia And Related Disorders
    Publication number: 20140371231
    Abstract: The present disclosure describes compounds and pharmaceutically acceptable salts thereof and compositions and formulations comprising the same that are useful in methods of treating dyskinesia or related disorders, and methods for treating dyskinesia or related disorders.
    Type: Application
    Filed: August 29, 2014
    Publication date: December 18, 2014
    Inventors: John Ciallella, John Gruner, Andrew G. Reaume, Michael S. Saporito
  • HETEROARYL DERIVATIVES AS CFTR MODULATORS
    Publication number: 20140371230
    Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Application
    Filed: June 25, 2014
    Publication date: December 18, 2014
    Inventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear
  • Alkynyl substituted pyrimidinyl-pyrroles active as kinases inhibitors
    Patent number: 8912200
    Abstract: The present invention relates to alkynyl substituted pyrimidinyl-pyrrole compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular Jak and/or Src family kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such compounds or the pharmaceutical compositions containing them.
    Type: Grant
    Filed: July 18, 2012
    Date of Patent: December 16, 2014
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Maria Gabriella Brasca, Jay Aaron Bertrand, Paola Gnocchi, Ilaria Motto, Marcella Nesi, Achille Panzeri, Paola Vianello
  • Protein Kinase Inhibitors
    Publication number: 20140364436
    Abstract: The present invention relates to compounds of Formula VIII with absolute configuration R or S: as well as pharmaceutically acceptable salts, hydrates, or solvates thereof, wherein the variables are described herein. The present invention further relates to pharmaceutical compositions which comprise the compounds of Formula VIII, and to methods for inhibiting protein kinase and methods of treating diseases, such as cancers, inflammation.
    Type: Application
    Filed: August 26, 2014
    Publication date: December 11, 2014
    Applicant: ASTAR BIOTECH LLC
    Inventors: Chunrong YU, Haihong HUANG, Dongfeng ZHANG, Peng LI
  • Compositions and methods for treating extracellular parasitic infections
    Publication number: 20140363479
    Abstract: There is disclosed herein a composition for treating extracellular parasitic infections, the composition comprising one or more of the following combinations: at least one quinolone or fluoroquinolone together with at least one tetracycline, iodoquinol, an azole or imidazole; or at least two agents selected from the group consisting of iodoquinol, thiazolidones, tetracycline, nitroimidazoles, cotrimoxazole and diloxanide furoate.
    Type: Application
    Filed: August 21, 2014
    Publication date: December 11, 2014
    Inventors: Thomas Julius BORODY, Soledad CARSULA
  • TRICYCLIC CARBAMATE JAK INHIBITORS
    Publication number: 20140363443
    Abstract: The present disclosure relates to 2,4-pyrimidinediamines substituted with tricyclic carbamates and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, such as JAK2 or JAK3, is therapeutically useful.
    Type: Application
    Filed: August 22, 2014
    Publication date: December 11, 2014
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Somasekhar Bhamidipati, Vadim Markovtsov
  • SUBSTITUTED PROLINES / PIPERIDINES AS OREXIN RECEPTOR ANTAGONISTS
    Publication number: 20140364432
    Abstract: The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention.
    Type: Application
    Filed: February 12, 2014
    Publication date: December 11, 2014
    Inventors: Theodore M. KAMENECKA, Yuanjun HE, William NGUYEN, Rong Jiang, Xinyi Song
  • SUBSTITUTED PROLINES / PIPERIDINES AS OREXIN RECEPTOR ANTAGONISTS
    Publication number: 20140364433
    Abstract: The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention.
    Type: Application
    Filed: August 14, 2014
    Publication date: December 11, 2014
    Inventors: Theodore M. KAMENECKA, Yuanjun HE, Rong JIANG, William NGUYEN, Xinyi SONG
  • Pyrimidine derivatives as FAK inhibitors
    Patent number: 8906916
    Abstract: Compounds of the formula (I), in which R1, R2 and R3 have the meanings indicated in Claim 1, are kinase inhibitors and can be employed, inter alia, for the treatment of tumors.
    Type: Grant
    Filed: July 19, 2011
    Date of Patent: December 9, 2014
    Assignee: Merck Patent GmbH
    Inventors: Timo Heinrich, Christina Esdar, Hartmut Greiner
  • Viral replication inhibitors
    Patent number: 8906906
    Abstract: The present invention relates to a series of novel compounds having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to novel intermediates useful in one or more steps of such syntheses. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutical amount of such compounds, optionally combined with one or more other drugs having antiviral activity.
    Type: Grant
    Filed: August 5, 2010
    Date of Patent: December 9, 2014
    Assignee: Katholieke Universiteit Leuven
    Inventors: Patrick Chaltin, Zeger Debyser, Marc De Maeyer, Arnaud Marchand, Damien Marchand, Wim Smets, Arnout Voet, Frauke Christ
  • Pyridyl-and pyrimidinyl-substituted pyrrole-, thiophene-and furane-derivatives as kinase inhibitors
    Patent number: 8906934
    Abstract: The present invention provides compounds of the formula (I), or the pharmaceutically acceptable salts thereof, wherein G, W, R2, R3, R4, R5 and R6 are as defined in the specification. Further objects of the invention are processes and intermediates for the preparation of the compounds of the formula (I), pharmaceutical compositions comprising them and methods for treating cell proliferative disorders. As a matter of fact, the compounds of the formula (I) are useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.
    Type: Grant
    Filed: July 27, 2012
    Date of Patent: December 9, 2014
    Assignee: Nerviano Medical Science S.R.L.
    Inventors: Ermes Vanotti, Marina Caldarelli, Alessandra Cirla, Barbara Forte, Antonella Ermoli, Maria Menichincheri, Antonio Pillan, Alessandra Scolaro
  • Chemokine receptor antagonists
    Patent number: 8906911
    Abstract: Disclosed herein are chemokine receptor antagonists of formula (I) wherein R1, R2, and R3 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.
    Type: Grant
    Filed: March 29, 2013
    Date of Patent: December 9, 2014
    Assignee: AbbVie Inc.
    Inventors: Michael D. Meyer, Xueqing Wang, Tao Guo, Robert Guo Ping Wei, Lijuan Jane Wang
  • COMPOUNDS FOR KINASE MODULATION, AND INDICATIONS THEREFOR
    Publication number: 20140357612
    Abstract: Compounds active on protein kinases and methods for regulating protein kinase pathways 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: May 29, 2014
    Publication date: December 4, 2014
    Inventors: Chao Zhang, Klaus-Peter Hirth, Prabha N. Ibrahim, Marika Nespi, Songyuan Shi, Wayne Spevak, Gaston G. Habets, Betsy Burton
  • Diamino-Pyridine, Pyrimidine, and Pyrazine Modulators of the Histamine H4 Receptor
    Publication number: 20140357614
    Abstract: Diamino-pyridine, pyrimidine and pyridazine compounds which may be used as H4 receptor modulators, and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.
    Type: Application
    Filed: August 14, 2014
    Publication date: December 4, 2014
    Inventors: Hui Cai, Frank Chavez, Paul J. Dunford, Andrew J. Greenspan, Steven P. Meduna, Jorge A. Quiroz, Brad M. Savall, Kevin L. Tays, Robin L. Thurmond, Jianmei Wei, Ronald L. Wolin, Xioahu Zhang
  • DIAMINOPYRIMIDINES AS P2X3 AND P2X2/3 ANTAGONISTS
    Publication number: 20140357629
    Abstract: Compounds and methods for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a compound of formula (I): or a pharmaceutically acceptable salt, solvate or prodrug thereof, wherein D, X, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein.
    Type: Application
    Filed: August 6, 2014
    Publication date: December 4, 2014
    Applicant: ROCHE PALO ALTO LLC
    Inventors: Chris Allen Broka, David Scott Carter, Michael Patrick Dillon, Ronald Charles Hawley, Alam Jahangir, Clara Jeou Jen Lin, Daniel Warren Parish
  • PHARMACEUTICAL COMPOSITION COMPRISING STABLE, AMORPHOUS, HYBRID NANOPARTICLES OF AT LEAST ONE PROTEIN KINASE INHIBITOR AND AT LEAST ONE POLYMERIC STABILIZING AND MATRIX-FORMING COMPONENT
    Publication number: 20140356443
    Abstract: The present invention relates to the field of methods for providing pharmaceutical compositions comprising poorly water-soluble drugs. In particular the present invention relates to compositions comprising stable, amorphous hybrid nanoparticles, comprising at least one protein kinase inhibitor and at least one polymeric stabilizing and matrix-forming component, useful in pharmaceutical compositions and in therapy.
    Type: Application
    Filed: January 11, 2013
    Publication date: December 4, 2014
    Applicant: XSPRAY MICROPARTICLES AB
    Inventors: Magnus Brisander, Mustafa Demirbüker, Gérald Jesson, Martin Malmsten, Helene Dérand