Additional Hetero Ring Which Is Unsaturated Patents (Class 544/405)
  • Patent number: 10251867
    Abstract: The present invention relates to a dosing regimen for a selective S1P1 receptor agonist, whereby the selective S1P1 receptor agonist is administered to a subject in such a way that during the initial treatment phase the selective S1P1 receptor agonist is administered at a dose which induces desensitization of the heart wherein said dose is below the target dose, and at a dosing frequency that sustains desensitization of the heart, until no further acute heart rate reduction occurs, followed by dose up-titration to the target dose of the selective S1P1 receptor agonist.
    Type: Grant
    Filed: June 5, 2015
    Date of Patent: April 9, 2019
    Assignee: ACTELION PHARMACEUTICALS LTD.
    Inventors: Patrick Brossard, Jasper Dingemanse, Oliver Nayler, Michael Scherz, Beat Steiner
  • Patent number: 9845309
    Abstract: PKC inhibitors are disclosed. The PKC inhibitors are useful for treating PKC associated diseases, including certain cancers. The PKC inhibitors have improved efficacy at lower dosage amounts to achieve tumor regression, improved potency, PK profile, absorption, gastrointestinal tolerance and kinase selectivity.
    Type: Grant
    Filed: August 16, 2016
    Date of Patent: December 19, 2017
    Assignee: NOVARTIS AG
    Inventors: Michael Joseph Luzzio, Julien Papillon, Michael Scott Visser
  • Patent number: 9593128
    Abstract: Compounds of the formula V: or a pharmaceutically acceptable salt thereof, wherein, R2 is optionally substituted phenyl, optionally substituted pyridin-2-yl or optionally substituted thienyl, and R3, R4, R5, R6 and R13 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.
    Type: Grant
    Filed: January 9, 2014
    Date of Patent: March 14, 2017
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Patrick Dillon, Ronald Charles Hawley, Li Chen, Linchin Feng, Minmin Yang
  • Patent number: 9452998
    Abstract: PKC inhibitors are disclosed. The PKC inhibitors are useful for treating PKC associated diseases, including certain cancers. The PKC inhibitors have improved efficacy at lower dosage amounts to achieve tumor regression, improved potency, PK profile, absorption, gastrointestinal tolerance and kinase selectivity.
    Type: Grant
    Filed: August 5, 2015
    Date of Patent: September 27, 2016
    Assignee: NOVARTIS AG
    Inventors: Michael Scott Visser, Michael Joseph Luzzio, Julien Papillon
  • Patent number: 9388193
    Abstract: Dipicolylamine compounds of Formula (I) set forth herein. Also disclosed are pharmaceutical compositions containing metal ions and these compounds. Further disclosed is a method for treating a condition associated with cells containing inside-out phosphatidylserine, with these compounds.
    Type: Grant
    Filed: May 14, 2015
    Date of Patent: July 12, 2016
    Assignees: National Health Research Institutes, Molecular Targeting Technologies, Inc.
    Inventors: Chiung-Tong Chen, Kak-Shan Shia, Chien-Huang Wu, Lun-Kelvin Tsou, Yu-Sheng Chao
  • Patent number: 9372194
    Abstract: There are described novel fluorescent dyes, conjugates which include a radical of a dye and a biological or a synthetic moiety and diagnostic and in vivo assays utilizing such conjugates and other products including the dyes and conjugates.
    Type: Grant
    Filed: December 17, 2014
    Date of Patent: June 21, 2016
    Inventor: Ramdas Pai
  • Patent number: 9073954
    Abstract: The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.
    Type: Grant
    Filed: July 14, 2014
    Date of Patent: July 7, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Joerg Kley, Sara Frattini, Dieter Hamprecht, Armin Heckel
  • Patent number: 9040540
    Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain pyridyl-amino-pyrazine carbonitrile compounds that, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or thymidylate synthase (TS) inhibitor; (d) a microtubule targeted agent; and (e) ionizing radiation.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: May 26, 2015
    Assignee: Cancer Research Technology Limited
    Inventors: Ian Collins, Michael Lainchbury, Thomas Peter Matthews, John Charles Reader
  • Patent number: 9040534
    Abstract: The present invention is directed to a compound of Formula (I) and to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: May 26, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Michael K. Ameriks, Jason C. Rech, Brad M. Savall
  • Publication number: 20150141428
    Abstract: The present invention is directed to benzyl urea compounds, which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence may be useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor Trk-A, Trk-B and/or Trk-C.
    Type: Application
    Filed: May 17, 2013
    Publication date: May 21, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Shawn J. Stachel, Melissa Egbertson, Edward Brnardic, Kristen G. Jones, John M. Sanders, Darrell Henze
  • Patent number: 9034879
    Abstract: The present invention provides pyridin-oxadiazole/thiadiazole derivatives of Formula I wherein A is N or CR 4a; and (ii) or (iii) which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: May 19, 2015
    Assignee: Novartis AG
    Inventors: Kamlesh Jagdis Bala, Rebecca Butler, Stephen Paul Collingwood, Edward Charles Hall, Lee Edwards, Darren Mark Legrand, Katrin Spiegel
  • Patent number: 9035053
    Abstract: The present invention relates to processes and intermediates for preparing compounds useful as inhibitors of ATR kinase, such as aminopyrazine-isoxazole derivatives and related molecules. The present invention also relates to compounds useful as inhibitors of ATR protein kinase. The invention relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and solid forms of the compounds of this invention. The compounds of this invention have formula I or II: wherein the variables are as defined herein.
    Type: Grant
    Filed: September 28, 2012
    Date of Patent: May 19, 2015
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, John Studley, Francoise Yvonne Theodora Marie Pierard, Steven John Durrant, Benjamin Joseph Littler, Robert Michael Hughes, David Andrew Siesel, Paul Angell, Armando Urbina, Yi Shi
  • Publication number: 20150133400
    Abstract: Heterocyclic compounds of formula (I), methods for their preparation, pharmaceutical compositions containing such a compound and their therapeutic uses.
    Type: Application
    Filed: September 15, 2014
    Publication date: May 14, 2015
    Inventors: Jiazhong Zhang, John Buell, Katrina Chan, Prabha N. Ibrahim, Jack Lin, Phuongly Pham, Songyuan Shi, Wayne Spevak, Guoxian Wu, Jeffrey Wu
  • Patent number: 9029392
    Abstract: Disclosed are a series of quinoline and quinoxaline derivatives comprising a fluorinated ethyl side-chain, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
    Type: Grant
    Filed: September 2, 2011
    Date of Patent: May 12, 2015
    Assignee: UCB Pharma S.A.
    Inventors: Andrew Harry Parton, Mezher Hussein Ali, Daniel Christopher Brookings, Julien Alistair Brown, Daniel James Ford, Richard Jeremy Franklin, Judi Charlotte Neuss, Joanna Rachel Quincey, Jackalyn Hinkins
  • Publication number: 20150125857
    Abstract: Disclosed are biomarkers, methods and assay for the identification of cancer patients who are predicted to benefit from the therapeutic administration of Wnt antagonist. The biomarkers include detection of RNF43 and ZNRF3 gene deletion, reduced RNF43 and ZNRF3 mRNA expression, reduced RNF43 and ZNRF3 protein expression, RNF43 and ZNRF3 inactivation mutation, phosphorylated LRP6, phophorylated Dishevelleds, and the expression of Frizzleds. These biomarkers can be associated with the better outcome for cancer patients treated with Wnt pathway inhibitors.
    Type: Application
    Filed: February 22, 2013
    Publication date: May 7, 2015
    Applicants: NOVARTIS AG, IRM LLC
    Inventors: Feng Cong, Huaixiang Hao, Mindy Hsin-I Hsieh, Xiaomo Jiang, Jun Liu, Nicholas Ng
  • Publication number: 20150126517
    Abstract: Novel aryl, heteroaryl, and non-aromatic heterocyle substituted tetrahydroisoquinolines are described in the present invention. These compounds are used in the treatment of various neurological and physiological disorders. Methods of making these compounds are also described in the present invention.
    Type: Application
    Filed: January 9, 2015
    Publication date: May 7, 2015
    Inventors: Shuang Liu, Bruce F. Molino, Kassoum Nacro
  • Patent number: 9023872
    Abstract: The present invention relates to substituted triazoles of formula (I), uses thereof, processes for the preparation thereof and compositions containing said compounds. These inhibitors have utility in a variety of therapeutic areas including sexual dysfunction.
    Type: Grant
    Filed: May 23, 2012
    Date of Patent: May 5, 2015
    Assignee: Ixchelsis Limited
    Inventors: Alan Daniel Brown, Andrew Antony Calabrese, David Ellis
  • Publication number: 20150119390
    Abstract: The present invention provides imidazothiadiazole compounds of Formula (I); Wherein W, Y, R0, R2, R4, Ra, Rb, X1, X2, X3 and X4 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments for treating or preventing thromboembolic disorders.
    Type: Application
    Filed: April 24, 2013
    Publication date: April 30, 2015
    Inventors: Alain Martel, François Tremblay, Anne Marinier, Eldon Scott Priestley, Shoshana L. Posy, R. Michael Lawrence, Michael M. Miller
  • Publication number: 20150118186
    Abstract: New pyrazole derivatives having the chemical structure of formula (I) are disclosed; as well as process for theft preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).
    Type: Application
    Filed: January 5, 2015
    Publication date: April 30, 2015
    Inventors: Jordi BACH TAÑA, Lluis Miquel PAGES SANTACANA, Joan TALTAVULL MOLL, Paul Robert EASTWOOD, Jacob GONZALEZ RODRIGUES, Victor GIULIO MATASSA
  • Publication number: 20150119387
    Abstract: The present invention relates to a compound having the structure of Formula I as inhibitor of WNT signal transduction pathways, as well as a composition comprising the compound. Further, the present invention relates to the use of the compound and the method of inhibiting the WNT signal transduction pathways.
    Type: Application
    Filed: June 15, 2012
    Publication date: April 30, 2015
    Applicant: Curegenix Inc.
    Inventor: Songzhou An
  • Publication number: 20150119385
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing said compound, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.
    Type: Application
    Filed: October 24, 2014
    Publication date: April 30, 2015
    Applicant: Novartis AG
    Inventors: Nicole Buschmann, Robin Alec Fairhurst, Pascal Furet, Thomas Knöpfel, Catherine Leblanc, Lv Liao, Robert Mah, Pierre Nimsgern, Sebastien Ripoche, Jing Xiong, Bo Han, Can Wang, Xianglin Zhao
  • Publication number: 20150119402
    Abstract: The present application is related to compounds represented by Formula I, which are novel positive allosteric modulators of al nAChRs. The application also discloses the treatment of disorders that are responsive to enhancement of acetylcholine action on al nAChRs in a mammal by administering an effective amount of a compound of Formula I.
    Type: Application
    Filed: May 8, 2013
    Publication date: April 30, 2015
    Inventor: Derk Hogenkamp
  • Patent number: 9018224
    Abstract: Substituted cyclopropyl compounds of the formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: April 28, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott Edmondson, Zhiyong Hu, Ping Liu, Gregori J. Morriello, Jason W. Szewczyk, Bowei Wang, Liping Wang, Harold B. Wood, Cheng Zhu, Yuping Zhu, Zhiqiang Guo
  • Patent number: 9018215
    Abstract: The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels and the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.
    Type: Grant
    Filed: April 28, 2014
    Date of Patent: April 28, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Joerg Kley, Armin Heckel
  • Publication number: 20150111893
    Abstract: The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the compounds of formula I, and methods of using said compounds, salts and compositions in the treatment of various disorders associated with CRM1 activity.
    Type: Application
    Filed: May 9, 2013
    Publication date: April 23, 2015
    Inventors: Vincent P. Sandanayaka, Sharon Shechter, Sharon Shacham, Dilara McCauley, Erkan Baloglu
  • Publication number: 20150111874
    Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
    Type: Application
    Filed: October 3, 2014
    Publication date: April 23, 2015
    Inventors: Alfredo C. Castro, Catherine A. Evans, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Tao LIU, Martin R. TREMBLAY
  • Publication number: 20150111750
    Abstract: N-(tetrazol-5-yl)- and N-(triazol-5-yl)hetarylcarboxamides of formula I and their use as herbicides. The invention relates to N-(tetrazol-5-yl)- and N-(triazol-5-yl)hetarylcarboxamides of formula I and their use as herbicides. In said formula I, B represents N or CH, whereas X1 is N or CR1, X2 is N or CR2, X3 is N or CR3 and X4 is N or CR4; provided that a least one of X1, X3 and X4 is N; R, R1, R2, R3, R4 and R5 represent groups such as hydrogen, halogen or organic groups such as alkyl or phenyl.
    Type: Application
    Filed: April 16, 2013
    Publication date: April 23, 2015
    Inventors: Helmut Kraus, Matthias Witschel, Thomas Seitz, Trevor William Newton, Liliana Parra Rapado, Klaus Kreuz, Johannes Hutzler, Maciej Pasternak, Jens Lerchl, Richard Roger Evans
  • Publication number: 20150111900
    Abstract: The present invention relates to compounds described herein Formula (I) and pharmaceutical acceptable salts thereof, which modulate the activity of calcium release-activated calcium (CRAC) channel. The invention also describes the compounds of Formula (I) and pharmaceutical compositions containing such compounds thereof for treating, managing, and/or lessening the severity of diseases, disorders, syndromes or conditions associated with the modulation of calcium release-activated calcium (CRAC) channel.
    Type: Application
    Filed: May 1, 2013
    Publication date: April 23, 2015
    Inventors: Nageswara Rao Irlapati, Zubair Abdul Wajid Shaikh, Vijay Pandurang Karche, Gokul Keruji Deshmukh, Neelima Sinha, Venkata P. Palle, Rajender Kumar Kamboj
  • Patent number: 9012445
    Abstract: In one aspect, the invention relates to substituted 4-(1H-pyrazol-4-yl)benzyl analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: January 12, 2013
    Date of Patent: April 21, 2015
    Assignee: Vanderbilt University
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, Michael S. Poslusney, James C. Tarr
  • Publication number: 20150105385
    Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
    Type: Application
    Filed: December 17, 2014
    Publication date: April 16, 2015
    Inventors: Alfredo C. CASTRO, Katrina CHAN, Catherine A. EVANS, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Liansheng LI, Tao LIU, Yi LIU, Pingda REN, Daniel A. SNYDER, Martin R. TREMBLAY
  • Publication number: 20150105378
    Abstract: The present invention provides compounds of Formula (I) or Formula (III): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Inventors: Lynn Abell, Leonard Adam, Cullen L. Cavallaro, Heather Finlay, Todd J. Friends, Jon J. Hangeland, Ji Jiang, R. Michael Lawrence, John Lloyd, Zulan Pi, George O. Tora, Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
  • Publication number: 20150105379
    Abstract: The following compound is provided as an agent for treating a disease induced by production, secretion and/or deposition of amyloid ? protein, for example, a compound represented by the formula (I): wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group, R1 is optionally substituted lower alkyl or the like, R2a and R2b are each independently hydrogen, optionally substituted lower alkyl or the like, R3a and R3c are each independently hydrogen, halogen, hydroxy, optionally substituted lower alkyl or the like, or a pharmaceutically acceptable salt thereof, or a solvate thereof.
    Type: Application
    Filed: July 26, 2013
    Publication date: April 16, 2015
    Applicant: Shionogi & Co., Ltd.
    Inventors: Sae Matsumoto, Yuuji Kooriyama
  • Publication number: 20150105403
    Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
    Type: Application
    Filed: March 14, 2013
    Publication date: April 16, 2015
    Inventors: Nicholas D. Smith, Steven P. Govek, Mehmet Kahraman, Jackaline D. Julien, Johnny Y. Nagasawa, Karensa L. Douglas, Celine Bonnefous, Andiliy G. Lai
  • Publication number: 20150105391
    Abstract: Certain embodiments of the present invention provide selected compounds having a molecular structure according to Formula 1: In Formula 1, Z is —CO—, —SO—, or —SO2—; Ar is phenyl, heteroaryl, or heterocycloalkyl; Het is heteroaryl; R is R?, X, or NR1R2; R? is R3, or OR3; R? is R4, or OR4; R1 and R2 are each independently H, alkyl, or acyl; R3 is H, heteroaryl, or alkyl; R4 is H, heteroaryl, or CnH2n+1 (n>2); and X is F, Br, I, CN, or NO2. In some embodiments, compounds having a molecular structure according to Formula 1 have the property of inhibiting a growth of a cell line selected from HeLa and MB468 with a sub-micromolar IC50.
    Type: Application
    Filed: July 19, 2014
    Publication date: April 16, 2015
    Inventors: Wen-Hwa Lee, Jiewen Zhu, Chun-Mei Hu
  • Patent number: 9006454
    Abstract: The invention relates to compounds of formula (I) wherein R1, R2, X1, X2, Y, Ra, Rb, Q have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis and also in the treatment of cancer disorders.
    Type: Grant
    Filed: March 26, 2010
    Date of Patent: April 14, 2015
    Assignee: Merck Serono S.A.
    Inventors: Siva Sanjeeva Rao Thunuguntla, Hosahalli Subramanya, Satish Reddy Kunnam, Sekhar Reddy Sanivaru Vijay, Chakrapani Bingi, Raviraj Kusanur, Matthias Schwarz, Michael Arlt
  • Patent number: 9006437
    Abstract: The present invention relates to fluorescent dyes in general. The present invention provides a wide range of fluorescent dyes and kits containing the same, which are applicable for labeling a variety of biomolecules, cells and microorganisms. The present invention also provides various methods of using the fluorescent dyes for research and development, forensic identification, environmental studies, diagnosis, prognosis, and/or treatment of disease conditions.
    Type: Grant
    Filed: April 9, 2013
    Date of Patent: April 14, 2015
    Assignee: Biotium, Inc.
    Inventors: Fei Mao, Wai-Yee Leung, Ching-Ying Cheung
  • Patent number: 9006429
    Abstract: Pyrandione, thiopyrandione and cyclohexanetrione compounds, which are suitable for use as herbicides.
    Type: Grant
    Filed: August 30, 2013
    Date of Patent: April 14, 2015
    Assignee: Syngenta Crop Protection, LLC
    Inventors: Christopher John Mathews, James Nicholas Scutt, Michel Muehlebach
  • Publication number: 20150099758
    Abstract: The present application is related to compounds represented by Formula I, which are novel positive allosteric modulators of al nAChRs. The application also discloses the treatment of disorders that are responsive to enhancement of acetylcholine action on al nAChRs in a mammal by administering an effective amount of a compound of Formula I.
    Type: Application
    Filed: May 8, 2013
    Publication date: April 9, 2015
    Applicant: Anvyl LLC
    Inventors: David Putnam, Olivier Dasse
  • Patent number: 8999996
    Abstract: The invention generally relates to nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to a compound represented by structural formula I: or a pharmaceutically acceptable salt thereof, wherein the values and alternative values for the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.
    Type: Grant
    Filed: March 19, 2014
    Date of Patent: April 7, 2015
    Assignee: Karyopharm Therapeutics Inc.
    Inventors: Vincent P. Sandanayaka, Sharon Shacham, Dilara McCauley, Sharon Shechter
  • Publication number: 20150094306
    Abstract: The present invention relates to pyrrolopyridinone derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.
    Type: Application
    Filed: April 25, 2013
    Publication date: April 2, 2015
    Inventors: Kiyoshi Kawamura, Mikio Morita, Tatsuya Yamagishi
  • Publication number: 20150094297
    Abstract: The present invention provides thiazole compounds of Formula I wherein W, Y, R0, R2, R4, R5, R6, R7, X1, X2, X3 and X4 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments for treating or preventing thromboembolic disorders.
    Type: Application
    Filed: April 24, 2013
    Publication date: April 2, 2015
    Inventors: Jacques Banville, Roger Rèmillard, Edward H. Ruediger, Daniel H. Deon, Marc Gagnon, Laurence Dubé, Julia Guy, Eldon Scott Priestley, Shoshana L. Posy, Brad D. Maxwell, Pancras C. Wong, R. Michael Lawrence, Michael M. Miller
  • Patent number: 8993554
    Abstract: Tetrahydroquinoline compounds, pharmaceutical compositions containing such compounds and their use in therapy.
    Type: Grant
    Filed: April 19, 2012
    Date of Patent: March 31, 2015
    Assignee: GlaxoSmithKline LLC
    Inventors: Dominique Amans, Emmanuel Hubert Demont, Darren Jason Mitchell, Jonathan Thomas Seal
  • Patent number: 8993779
    Abstract: The present invention is directed to benzimidazolone derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved, such as schizophrenia.
    Type: Grant
    Filed: August 5, 2011
    Date of Patent: March 31, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Vadim Y. Dudkin, Mark E. Fraley, Kenneth L. Arrington, Mark E. Layton, Alexander J. Reif, Kevin J. Rodzinak, Joseph E. Pero
  • Patent number: 8993752
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, R4, and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: July 8, 2013
    Date of Patent: March 31, 2015
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Roland Gendron, Adam D. Hughes
  • Publication number: 20150087644
    Abstract: The invention relates to compounds of formula I wherein A1, A2, A3, B, R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used as medicaments.
    Type: Application
    Filed: November 26, 2014
    Publication date: March 26, 2015
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Alexander Flohr, Katrin Groebke Zbinden, Matthias Koerner, Christian Lerner
  • Patent number: 8987288
    Abstract: The present invention relates to a novel berbamine derivative of formula I or a pharmaceutically acceptable salt thereof, a process for preparation of the same, a pharmaceutical composition comprising said compound and its use in manufacture of an antitumor medicament.
    Type: Grant
    Filed: September 9, 2011
    Date of Patent: March 24, 2015
    Assignee: Hangzhou Bensheng Pharmaceutical Co., Ltd.
    Inventors: Rongzhen Xu, Fuwen Xie, Hongxi Lai, Frank Rong
  • Patent number: 8987258
    Abstract: The present invention relates to novel chromenone analog sirtuin modulator compounds of Formula (I): or pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions and treatment methods and combination therapies thereof for use in increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity.
    Type: Grant
    Filed: September 29, 2009
    Date of Patent: March 24, 2015
    Inventors: Christopher Oalmann, Robert B. Perni, Chi B. Vu
  • Patent number: 8987449
    Abstract: Disclosed in the present invention are a compound of the general structure formula LQC-T as shown below, wherein R represents an aromatic organic acid or phenol or the structural analog thereof, such as protocatechuic acid, protocatechuic aldehyde, vanillic acid, gallic acid, caffeic acid, ferulic acid etc., and the synthesis and use of the compound. The compounds promote new blood vessel growth in the chick embryo chorioallantoic membrane, wherein LQC-T4 can be used to prepare a medicine for treating ischemic brain injury (stroke) and its sequelae.
    Type: Grant
    Filed: September 4, 2013
    Date of Patent: March 24, 2015
    Assignee: Haimin Lei
    Inventors: Haimin Lei, Ying Hong
  • Patent number: 8987250
    Abstract: Compounds disclosed herein including compounds of formula I?: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.
    Type: Grant
    Filed: April 19, 2013
    Date of Patent: March 24, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Kerim Babaoglu, Gediminas Brizgys, Jake Cha, Xiaowu Chen, Hongyan Guo, Randall L. Halcomb, Xiaochun Han, Richard Huang, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu, Hong Yang
  • Publication number: 20150080372
    Abstract: Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on each of B-Raf, B-Raf V600E and c-Raf-1 protein kinase. In certain aspects and embodiments, the described compounds are active in inhibiting proliferation of a Ras mutant cell line.
    Type: Application
    Filed: October 14, 2014
    Publication date: March 19, 2015
    Inventors: Prabha N. Ibrahim, Guoxian Wu, Jack Lin, Wayne Spevak, Hanna Cho, Todd Ewing, Chao Zhang