Three Or More Ring Hetero Atoms In The Tricyclo Ring System Patents (Class 544/250)
  • Patent number: 10150766
    Abstract: The present invention is directed to compounds of Formula (I), which includes enantiomer and diasteromers thereof: The invention also relates 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: August 25, 2015
    Date of Patent: December 11, 2018
    Assignee: Janssen Pharmaceutica NV
    Inventors: Michael A. Letavic, Jason C. Rech, Jessica L. Wall
  • Patent number: 9920058
    Abstract: 7-(substituted) derivatives of 7H-pyrrolo[3,2-f]-quinazoline-1,3-diamines, derivative thereof, and methods of using them are provided. The pharmaceutical formulations prepared from the compounds can be used to treat a variety of conditions, which include, but are not limited to bacterial and fungal infections. The compounds can also be used as a sterilizing or disinfecting agent.
    Type: Grant
    Filed: May 5, 2014
    Date of Patent: March 20, 2018
    Assignee: Georgia Tech Research Corporation
    Inventors: Bharath Srinivasan, Jeffrey Skolnick, Hongyi Zhou
  • Patent number: 9505774
    Abstract: Provided are Icotinib maleate (the compound of Formula I) and polymorph forms thereof, and methods of preparing and using them.
    Type: Grant
    Filed: June 9, 2014
    Date of Patent: November 29, 2016
    Assignee: Betta Pharmaceuticals Co., Ltd.
    Inventors: Shaojing Hu, Wei Long, Fei Wang, Yinxiang Wang, Lieming Ding
  • Patent number: 9505768
    Abstract: Provided herein, inter alia, are methods and compositions for modulating TLR-4.
    Type: Grant
    Filed: March 27, 2015
    Date of Patent: November 29, 2016
    Assignee: The Regents Of The University Of California
    Inventors: Dennis A. Carson, Howard B. Cottam, Tomoko Hayashi, Michael Chan, Mary P. Corr
  • Patent number: 9458167
    Abstract: The present invention provides tricyclic compounds, pharmaceutically acceptable salts, prodrugs, solvates, or hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells.
    Type: Grant
    Filed: May 22, 2015
    Date of Patent: October 4, 2016
    Assignee: Duquesne University of the Holy Spirit
    Inventor: Aleem Gangjee
  • Patent number: 9440940
    Abstract: Methods for the synthesis of psoralen derivatives are provided.
    Type: Grant
    Filed: March 17, 2015
    Date of Patent: September 13, 2016
    Assignee: Macopharma, S.A.S.
    Inventor: Bernard Refouvelet
  • Patent number: 9382263
    Abstract: Compounds of formula (I) i.e. monocyclic or bicyclic diamine-substituted thieno[2,3-d]pyrimidine and isothiazolo[5,4-d]pyrimidine derivatives substituted by an optionally substituted oxazolin-2-yl moiety, are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases; and organ and cell transplant rejection.
    Type: Grant
    Filed: October 2, 2013
    Date of Patent: July 5, 2016
    Assignee: UCB Biopharma SPRL
    Inventors: Claire Louise Kulisa, Daniel Christopher Brookings, Daniel James Ford, Richard Jeremy Franklin, James Thomas Reuberson, Anant Ramrao Ghawalkar
  • Patent number: 9296757
    Abstract: The present invention relates to substituted benzothienopyrimidine compounds of general formula I: in which R1a, R1b, R2a, R2b, and R2c are as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: May 17, 2013
    Date of Patent: March 29, 2016
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Ulrich Klar, Georg Kettschau, Dirk Kosemund, Florian Pühler, Knut Eis, Philip Lienau, Ulf Bömer, Detlev Sülzle, Lars Wortmann
  • Patent number: 9284312
    Abstract: The present invention is directed to N-methyl tetrahydroquinoline compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Grant
    Filed: May 11, 2012
    Date of Patent: March 15, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Christina Ng DiMarco, Thomas J. Greshock
  • Patent number: 9175007
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.
    Type: Grant
    Filed: January 8, 2014
    Date of Patent: November 3, 2015
    Assignee: Nimbus Iris, Inc.
    Inventors: Jeremy Robert Greenwood, Geraldine C. Harriman, Rosana Kapeller-Libermann, Craig E. Masse, Shaughnessy Robinson, Donna L. Romero, Mee Shelley, Ronald T. Wester
  • Patent number: 9102592
    Abstract: The present invention relates to processes for the preparation of quinoline-3-carboxamide derivatives, such as sodium 5-chloro-3-(ethylphenylcarbamoyl)-1-methyl-2-oxo-1,2-dihydroquinolin-4-olate (Laquinimod sodium). The present invention further relates to intermediates formed in such processes.
    Type: Grant
    Filed: August 28, 2014
    Date of Patent: August 11, 2015
    Assignee: MAPI PHARMA LTD.
    Inventors: Ehud Marom, Michael Mizhiritskii, Shai Rubnov
  • Patent number: 9079916
    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: Grant
    Filed: June 25, 2014
    Date of Patent: July 14, 2015
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear
  • Patent number: 9056869
    Abstract: The present invention provides tricyclic compounds, pharmaceutically acceptable salts, prodrugs, solvates, or hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells.
    Type: Grant
    Filed: June 2, 2011
    Date of Patent: June 16, 2015
    Assignee: Duquesne University of the Holy Spirit
    Inventor: Aleem Gangjee
  • Publication number: 20150141415
    Abstract: The present invention relates to methods for treating an infectious disease in a subject in need thereof via administration of a therapeutically effective amount of compounds described herein. The methods may utilize particular compounds, for example, a quinoline, a hydrazone, a quinone, or a pyrimidine derivatives thereof or a pharmaceutical salts thereof.
    Type: Application
    Filed: November 7, 2014
    Publication date: May 21, 2015
    Inventors: Omonike Arike Olaleye, Sarah Finney John, Adaugo Chimzurum Isichei, Jun O Liu, Rosa Maldonado, Janice Endsley
  • Publication number: 20150140489
    Abstract: Disclosed and claimed herein is a composition of matter having a general structure chosen from (I), (II), (III) or (IV); wherein X and Y are the same or different, wherein at least one of X and Y comprises an acid labile group, wherein R1 is a saturated or unsaturated group having from 1-4 carbon atoms, R2 is chosen from hydrogen or a saturated or unsaturated group having from 1-4 carbon atoms, R3 is a saturated or unsaturated group having from 1-4 carbon atoms, and R4 is a saturated or unsaturated group having from 1-4 carbon atoms.
    Type: Application
    Filed: October 21, 2014
    Publication date: May 21, 2015
    Inventors: Alex Philip Graham Robinson, Dongxu Yang, Andreas Frommhold, Thomas Lada, John L. Roth, Xiang Xue
  • Publication number: 20150141445
    Abstract: The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders.
    Type: Application
    Filed: September 25, 2014
    Publication date: May 21, 2015
    Inventor: Aleem Gangjee
  • Publication number: 20150141408
    Abstract: The present invention relates to tricyclic pyrrolo derivatives which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.
    Type: Application
    Filed: January 30, 2015
    Publication date: May 21, 2015
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Marina Caldarelli, Mauro Angiolini, Italo Beria, Maria Gabriella Brasca, Francesco Casuscelli, Roberto D'Alessio, Andrea Lombardi Borgia
  • Publication number: 20150141444
    Abstract: The present invention is directed to N-methyl tetrahydroquinoline compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Application
    Filed: May 11, 2012
    Publication date: May 21, 2015
    Inventors: Scott D. Kuduk, Christina Ng DiMarco, Thomas J. Greshock
  • Publication number: 20150133426
    Abstract: The present invention relates to substituted pyrrolopyrimidine compounds general formula I: in which A, X, R1, R2, m and n are as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: May 17, 2013
    Publication date: May 14, 2015
    Inventors: Ulrich Klar, Georg Kettschau, Detlev Sülzle, Florian Puehler, Dirk Kosemund, Philip Lienau, Ulf Bömer, Lars Wortmann
  • Publication number: 20150133425
    Abstract: The present invention relates to substituted thienopyrimidine compounds of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: May 17, 2013
    Publication date: May 14, 2015
    Inventors: Georg Kettschau, Florian Puehler, Knut Eis, Ulrich Klar, Dirk Kosemund, Detlev Sülzle, Philip Lienau, Andrea Hägebarth, Ulf Bömer, Lars Wortmann, Keith Graham, Antje Margret Wengner
  • Publication number: 20150126449
    Abstract: The present application relates to novel substituted (aza)pyridopyrazolopyrimidinones and indazolopyrimidinones, to processes for their preparation, the compounds for use alone or in combinations in a method for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of acute and recurrent bleeding in patients with or without underlying hereditary or acquired bleeding disorders, wherein the bleeding is associated with a disease or medical intervention selected from the group consisting of menorrhagia, postpartum hemorrhage, hemorrhagic shock, trauma, surgery, transplantation, stroke, liver diseases, hereditary angioedema, nosebleed, and synovitis and cartilage damage following hemarthrosis.
    Type: Application
    Filed: November 5, 2014
    Publication date: May 7, 2015
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Jorma Haßfeld, Tom KINZEL, Johannes Köbberling, Yolanda CANCHO GRANDE, Kristin BEYER, Susanne Röhrig, Maria Köllnberger, Michael SPERZEL, Nils BURKHARDT, Karl-Heinz SCHLEMMER, Christian STEGMANN, Joachim SCHUHMACHER, Matthias WERNER, Manuel ELLERMANN
  • Publication number: 20150105381
    Abstract: The present invention relates to the pyrazoloquinazolinone and pyrroloquinazolinone derivatives of the general formula (I), as well as pharmaceutical compositions containing them, and their use in the treatment and/or prophylaxis of conditions associated with altered glutamatergic signalling and/or functions, and/or conditions which can be affected by alteration of glutamate level or signalling in mammals, in particular their use in the treatment and/or prophylaxis of acute and chronic neurological and/or psychiatric disorders.
    Type: Application
    Filed: May 21, 2013
    Publication date: April 16, 2015
    Inventors: Stanislas Mayer, Stephan Schann
  • Patent number: 9006265
    Abstract: The use of substituted fused pyrimidinones and dihydropyrimidinones of the formula (I) or salts thereof where the radicals of the formula (I) are each as defined in the description, for enhancing stress tolerance in plants to abiotic stress, and for invigorating plant growth and/or for increasing plant yield.
    Type: Grant
    Filed: September 2, 2011
    Date of Patent: April 14, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Jens Frackenpohl, Hans-Joachim Zeiβ, Ines Heinemann, Lothar Willms, Thomas Müller, Marco Busch, Pascal Von Koskull-Döring, Isolde Häuser-Hahn, Christopher Hugh Rosinger, Jan Dittgen, Martin Jeffrey Hills, Monika H. Schmitt
  • Patent number: 8999988
    Abstract: Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following structure: including steroisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein A is a ring moiety selected from: and wherein R1, R2, R3, X, Z, L1, Cycl1, L2 and Cycl2 are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.
    Type: Grant
    Filed: July 22, 2013
    Date of Patent: April 7, 2015
    Assignees: Arizona Board of Regents on behalf of the University of Arizona, Astex Pharmaceuticals, Inc.
    Inventors: Laurence H. Hurley, Daruka Mahadevan, David J. Bearss, Hariprasad Vankayalapati, Steven L. Warner, James Welsh, Sridevi Bashyam
  • Publication number: 20150080374
    Abstract: This invention relates to novel 2,3-dihydroimidazo[1,2-c]quinazoline compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for phosphotidylinositol-3-kinase (PI3K) inhibition and treating diseases associated with phosphotidylinositol-3-kinase (PI3K) activity, in particular treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: November 25, 2014
    Publication date: March 19, 2015
    Inventors: William Scott, Ningshu LIU, Manfred MÖWES, Andrea HÄGEBARTH, Ursula MÖNNING, Ulf BÖMER
  • Patent number: 8980903
    Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of CDK4-mediated disorders, such as cancer. The subject compounds are fused pyridine, pyrimide and triazine derivatives.
    Type: Grant
    Filed: August 7, 2014
    Date of Patent: March 17, 2015
    Assignee: Amgen Inc.
    Inventors: Richard V. Connors, Kang Dai, John Eksterowicz, Pingchen Fan, Benjamin Fisher, Jiasheng Fu, Kexue Li, Zhihong Li, Lawrence R. McGee, Rajiv Sharma, Xiaodong Wang, Dustin L. McMinn, Jeffrey T. Mihalic, Jeffrey Deignan
  • Patent number: 8980902
    Abstract: Compounds of the following formula are provided for use with PARP: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits, and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds.
    Type: Grant
    Filed: September 18, 2013
    Date of Patent: March 17, 2015
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Jason W. Brown, Anthony R. Gangloff, Andre K. Kiryanov
  • Patent number: 8975269
    Abstract: The present invention provides a catalyst complex or ligand, and compositions thereof, for use in a variety of organic reactions having high reactivity and enantioselectivity. The catalyst is a N-heterocyclic carbene having three fused rings with first and second rings being six-membered rings and the third being a five-membered ring. The first ring is fused to the second and has four substituents. The second ring has two nitrogens flanking a carbene atom with one nitrogen bound to a substituent. The carbene atom may optionally be bonded to a metal. The third ring is fused to the second ring and contains two nitrogens. The third ring of the catalyst has a double bond and two substituents on adjacent non-fused carbons. A non-fused nitrogen of the third ring is partially bonded to another substituent. Methods for the synthesis and use of the catalyst embodiments of the present invention are also provided.
    Type: Grant
    Filed: July 29, 2014
    Date of Patent: March 10, 2015
    Assignee: Florida State University Research Foundation
    Inventors: D. Tyler McQuade, Jin Kyoon Park, Matthew D. Rexford, Hershel H. Lackey
  • Patent number: 8975267
    Abstract: The present invention relates to tricyclic pyrrolo derivatives of Formula (I), which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.
    Type: Grant
    Filed: January 19, 2012
    Date of Patent: March 10, 2015
    Assignee: Nerviano Medical Sciences S.r.l.
    Inventors: Marina Caldarelli, Mauro Angiolini, Italo Beria, Maria Gabriella Brasca, Francesco Casuscelli, Roberto D'Alessio, Andrea Lombardi Borgia
  • Publication number: 20150065505
    Abstract: The present invention provides compounds of Formula (I), 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: March 29, 2013
    Publication date: March 5, 2015
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang, Ji Jiang
  • 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
  • Patent number: 8969590
    Abstract: Classes of compounds that exhibit effective inhibition of autotaxin enzymes are provided. Such classes include thioureas, diphenyldiazerenes, xanthenes, and isoindoles and exhibit reactivity with autotaxin to ultimately reduce the size of the reactive sites thereon to prevent conversion of lysophosphatidyl choline to lysophophatidic acid. Furthermore, such compounds can be incorporated within delivery forms for human ingestion. As such, these compounds accord an excellent manner of potentially reducing generation of certain cancers attributable to the presence of naturally occurring autotaxin within the human body. Methods of inactivating autotaxin to certain degrees therewith such compounds are encompassed within invention as well.
    Type: Grant
    Filed: September 18, 2012
    Date of Patent: March 3, 2015
    Inventors: Abby Louise Parrill-Baker, Daniel Lee Baker
  • Publication number: 20150057263
    Abstract: This invention relates to quinazoline compounds of Formula (I) which are inhibitors of the histone lysine methyltransferase (HKMTase) EZH2, and to uses of such compounds as medicaments, in particular in the treatment of a disease or disorder in which inhibition of EZH2 provides a therapeutic or prophylactic effect.
    Type: Application
    Filed: March 19, 2013
    Publication date: February 26, 2015
    Inventors: Robert Brown, Matthew John Fuchter, Nadine Chapman-Rothe, Nitipol Srimongkolpithak, Joachim Caron, James Synder, Thota Ganesh, Jin Liu, Aiming Sun
  • Patent number: 8962607
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.
    Type: Grant
    Filed: April 22, 2013
    Date of Patent: February 24, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Haiyan Bian, Kristen Chevalier, Jose Clemente, Peter J Connolly, Christopher Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark Macielag, Mark M McDonnell, Philip M Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
  • Publication number: 20150031876
    Abstract: The present invention provides a pyrone derivative and a pyridone derivative, which are novel intermediates for synthesizing an anti-influenza drug, a method of producing the same, and a method of using the same.
    Type: Application
    Filed: September 5, 2014
    Publication date: January 29, 2015
    Applicant: Shionogi & Co., Ltd.
    Inventors: Yukihito Sumino, Kazuya Okamoto, Moriyasu Masui, Toshiyuki Akiyama
  • Publication number: 20150021555
    Abstract: Luminescent materials including donor-acceptor compounds with a high triplet energy heteropolyaromatic system, namely, dibenzofuran, dibenzothiophene and dibenzoselenophene with one or multiple nitrogens in the ring as the electron acceptor for use as emitters in organic light emitting diodes is disclosed.
    Type: Application
    Filed: July 16, 2013
    Publication date: January 22, 2015
    Inventors: Raymond Kwong, Chuanjun Xia, Scott Joseph, Siu Tung Lam, Chi Hang Lee
  • Publication number: 20150021556
    Abstract: The present disclosure generally relates to novel compounds containing carbazole and triazine with different number of phenyl units attached to its core. In particular, the disclosure relates to compositions and/or devices comprising these compounds as hosts for PHOLEDs.
    Type: Application
    Filed: July 16, 2013
    Publication date: January 22, 2015
    Applicant: Universal Display Corporation
    Inventors: Chuanjun Xia, Scott Joseph
  • Publication number: 20150025093
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.
    Type: Application
    Filed: February 25, 2014
    Publication date: January 22, 2015
    Applicant: Nimbus Iris, Inc.
    Inventors: Donna L. Romero, Matthew David Wessel, Shaughnessy Robinson, Jeremy Robert Greenwood, Karl Shawn Watts, Leah Lynn Frye, Geraldine C. Harriman, Alan Franklin Corin, Craig E. Masse, Mee Shelley
  • Patent number: 8933087
    Abstract: Proteinopathies result from the proteasome not acting efficiently enough to eliminate harmful proteins and prevent the formation of the pathogenic aggregates. As described herein, inhibition of proteasome-associated deubiquitinase Usp14 results in increased proteasome efficiency. The present invention therefore provides novel compositions and methods for inhibition of Usp14, enhancement of proteasome activity and treatment of proteinopathies.
    Type: Grant
    Filed: July 22, 2011
    Date of Patent: January 13, 2015
    Assignee: President and Fellows of Harvard College
    Inventors: Daniel J. Finley, Randall W. King, Byung-Hoon Lee, Min J. Lee, Timothy C. Gahman
  • Publication number: 20150011543
    Abstract: Pyrimido[4,5-b]indole derivatives are provided. These compounds are useful to expand hematopoietic stem cell populations, particularly, human hematopoietic stem cell populations. The compounds are also useful in the medical treatment of diseases that involve hematopoietic stem cells.
    Type: Application
    Filed: January 25, 2013
    Publication date: January 8, 2015
    Applicant: UNIVERSITE DE MONTREAL
    Inventors: Guy Sauvageau, Yves Gareau
  • Publication number: 20150011531
    Abstract: Compounds of formula (I) and pharmaceutical compositions thereof: wherein A1 A2 and A3 are each independently selected from the group consisting of N and CR3, wherein R1 is an optionally substituted heterocyclyl or an optionally substituted —(C1-6)alkyl-heterocyclyl, R2 is an optionally substituted aryl or an optionally subsisted heteroaryl, R4 is an optionally substituted aryl, an optionally substituted heterocyclyl or an optionally substituted heteroaryl, useful as an inhibitor of HIV replication.
    Type: Application
    Filed: December 19, 2012
    Publication date: January 8, 2015
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Claudio Sturino, Pierre Beaulieu, Patrick Deroy, Martin Duplessis, Clint James, Jean-Eric Lacoste, Joannie Minville, Louis Morency, Sébastien Morin, Bruno Simoneau, Martin Tremblay
  • Patent number: 8927561
    Abstract: Disclosed herein are compounds and related compositions for the treatment of viral infection, including RNA viral infection, and compounds that can modulate the RIG-I pathway in vertebrate cells, including compounds that can activate the RIG-I pathway.
    Type: Grant
    Filed: April 20, 2011
    Date of Patent: January 6, 2015
    Assignee: Kineta, Inc.
    Inventors: Shawn P. Iadonato, Kristin Bedard
  • Patent number: 8927560
    Abstract: The present invention provides 4-Aza-2,3-didehydropodophyllotoxin compound of general formula A (4a-4z and 4aa-4ae) as useful potential antitumour agents against human cancer cell lines. The present invention further provides a process for the synthesis of 4-Aza-2,3-didehydropodophyllotoxin compounds (4a-4z and 4aa-4ae).
    Type: Grant
    Filed: March 25, 2011
    Date of Patent: January 6, 2015
    Assignee: Council of Scientific & Industrial Research
    Inventors: Kamal Ahmed, Suresh Paidakula, Ashwini Kumar Banala, Mallareddy Adla, Venkat Reddy Papagari, Rasheed Tamboli Jaki
  • Patent number: 8920944
    Abstract: Use of a precursor of an n-dopant for doping an organic semiconductive material, as a blocking layer, as a charge injection layer, as an electrode material, as a storage material or as a semiconductor material itself in electronic or optoelectronic components, the precursor being selected from the following formulae 1-3c:
    Type: Grant
    Filed: June 20, 2008
    Date of Patent: December 30, 2014
    Assignee: Novaled AG
    Inventors: Michael Limmert, Andrea Lux, Horst Hartmann
  • Patent number: 8921549
    Abstract: Provided are a light-emitting element including a novel organometallic complex as an emission center, the organometallic complex, a light-emitting device, an electronic device, and a lighting device each using the light-emitting element. One embodiment of the present invention is a light-emitting element including, as an emission center, an organometallic complex in which a benzofuropyrimidine derivative is coordinated to a metal. In particular, another embodiment is a light-emitting element including, as an emission center, an organometallic complex in which a benzofuropyrimidine derivative having an aryl group at the 4-position is coordinated to a metal. Another embodiment is a light-emitting element including, as an emission center, an organometallic complex in which nitrogen at the 3-position of a benzofuropyrimidine derivative having an aryl group at the 4-position is coordinated to a metal and the aryl group is bonded to the metal.
    Type: Grant
    Filed: May 30, 2013
    Date of Patent: December 30, 2014
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Hideko Inoue, Tomoya Yamaguchi, Hiromi Seo, Satoshi Seo
  • Publication number: 20140378486
    Abstract: Disclosed herein are acylated derivatives of 7H-pyrrolo[3,2-f]quinazoline-1,3-diamine and pharmaceutical compositions comprising said derivatives.
    Type: Application
    Filed: June 19, 2014
    Publication date: December 25, 2014
    Applicant: OREGON HEALTH & SCIENCE UNIVERSITY
    Inventors: Xiangshu Xiao, Jingjin Chen, Bingbing Li
  • Patent number: 8916577
    Abstract: New substituted tricyclic compounds of formula (I) are described, wherein R1, R2, X, Y, Z are herein defined, having protein kinase inhibiting activity. The invention includes methods to prepare the compounds of formula (I), pharmaceutical compositions containing them, and their use in therapy, in particular for the treatment of diseases caused by and/or associated with dysregulated activity of protein kinase.
    Type: Grant
    Filed: January 19, 2012
    Date of Patent: December 23, 2014
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Marina Caldarelli, Francesco Casuscelli, Daniele Donati, Danilo Mirizzi, Francesca Quartieri, Marco Silvagni
  • 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
  • Patent number: 8901141
    Abstract: There is provided a compound of the formula (I?): wherein X is a nitrogen or CRx, Rx is a hydrogen, etc., R1 is an optionally substituted hydrocarbon group, etc., R2 is an optionally substituted hydrocarbon group, etc., ring A is 5- to -8-membered heterocyclic ring, etc., and each of Y1, Y2 and Y3 is an optionally substituted carbon or a nitrogen, etc.; or ‘a salt thereof or a prodrug thereof, which have CRF receptor antagonistic activity and use thereof.
    Type: Grant
    Filed: January 21, 2009
    Date of Patent: December 2, 2014
    Assignee: Takeda Pharmaceutical Company, Limited
    Inventors: Kazuyoshi Aso, Katsumi Kobayashi, Takafumi Takai, Takuto Kojima, Kazuyuki Tokumaru, Michiyo Mochizuki
  • Publication number: 20140350244
    Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of CDK4-mediated disorders, such as cancer. The subject compounds are fused pyridine, pyrimide and triazine derivatives.
    Type: Application
    Filed: August 7, 2014
    Publication date: November 27, 2014
    Inventors: Richard V. Connors, Kang DAI, John EKSTEROWICZ, Pingchen FAN, Benjamin FISHER, Jiasheng FU, Kexue LI, Zhihong LI, Lawrence R. MCGEE, Rajiv SHARMA, Xiaodong WANG, Dustin L. MCMINN, Jeffrey T. MIHALIC, Jeffrey DEIGNAN