Additional Hetero Ring Attached Directly Or Indirectly To The Quinoline Ring System By Nonionic Bonding Patents (Class 514/314)
  • Patent number: 10351492
    Abstract: Novel selective synthesis route to introduce primary alkyl groups on aromatic compounds is disclosed. The synthesis route is based on electrophilic aromatic substitutions of thionium ion species that are generated in-situ from aldehydes and thiols, affording benzyl sulfide that can be reduced with triethylsilane.
    Type: Grant
    Filed: February 16, 2016
    Date of Patent: July 16, 2019
    Assignee: B. G. NEGEV TECHNOLOGIES AND APPLICATIONS
    Inventors: Doron Pappo, Regev Parnes
  • Patent number: 10251877
    Abstract: The present invention includes a method of reducing or inhibiting the kinase activity of C-KIT mutant tyrosine kinase activity in a cell or a subject, and the use of such compound for treating mutant C-KIT driven cell proliferative disorder(s) in a subject related to using a compound of the present invention: or pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: January 4, 2018
    Date of Patent: April 9, 2019
    Assignee: Arog Pharmaceuticals, Inc.
    Inventor: Vinay K. Jain
  • Patent number: 10092554
    Abstract: The present invention relates to compositions and methods for controlling glycemia in a mammalian in need thereof. The present invention relates to compositions and methods for the treatment of diabetes and related disorders. More specifically, the present invention relates to novel therapies or combinatorial therapies for diabetes and related disorders, based on compositions controlling the blood glucose level.
    Type: Grant
    Filed: April 29, 2015
    Date of Patent: October 9, 2018
    Assignee: PHARNEXT
    Inventors: Daniel Cohen, Ilya Chumakov, Serguei Nabirochkin, Rodolphe Hajj
  • Patent number: 10034854
    Abstract: The invention relates to solid dispersions of poorly water soluble compounds, in particular Compound A as disclosed herein, formed by solvent co-precipitation or spray drying, resulting in improved bioavailability, safety and tolerability of said compounds.
    Type: Grant
    Filed: July 1, 2016
    Date of Patent: July 31, 2018
    Assignee: HOFFMAN-LA ROCHE INC.
    Inventors: Steve Lomuscio, Hua Ma, Michael Allen Matchett, Harpreet K. Sandhu, Navnit Hargovindas Shah, Yu-E Zhang
  • Patent number: 10005744
    Abstract: It discloses compounds for the treatment and prevention of breast cancer, which are specifically 2-phenyl benzoselenazole compounds, pharmaceutically acceptable salts thereof and prodrugs thereof. The present invention further discloses pharmaceutical compositions containing the compounds and applications of the compounds in preparing medicines for the treatment and prevention of breast cancer in mammals. The compounds of the present invention can effectively inhibit or reduce the growth or proliferation of breast cancer cells in mammals, with no inhibition effect on the growth of part of the tested cell lines except for the breast cancer cell lines, and are highly selective.
    Type: Grant
    Filed: May 6, 2016
    Date of Patent: June 26, 2018
    Assignee: JIANGSU ATOM BIOSCIENCE AND PHARMACEUTICAL CO., LTD.
    Inventors: Dongfang Shi, Changjin Fu, Xi Cheng, Jianghua Zhu
  • Patent number: 10004734
    Abstract: The present disclosure provides methods and compositions for treating or preventing erythema, including rebound erythema associated with the use of topical alpha-adrenergic agonists. In certain embodiments, an effective amount of a capsaicinoid, such as capsaicin or a pharmaceutically acceptable salt or derivative thereof, is administered to a subject.
    Type: Grant
    Filed: January 25, 2017
    Date of Patent: June 26, 2018
    Inventor: Warren Scherer
  • Patent number: 9957274
    Abstract: Compounds having a structure of Formula (I): or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, wherein A1, A2, A3, A4, A5, n, and m are as defined herein and are provided. Pharmaceutical compositions comprising such compounds and methods for treating various EED-related conditions or diseases, including cancer, by administration of such compounds are also provided.
    Type: Grant
    Filed: May 5, 2017
    Date of Patent: May 1, 2018
    Assignee: AbbVie Inc.
    Inventors: Michael R. Michaelides, Michael L. Curtin, Huan-Qiu Li, Marina A Pliushchev, Ying Wang, Hongyu H. Zhao, Richard F. Clark, Alan S. Florjancic, Zhiqin Ji, Mariazel Torrent, Ramzi F. Sweis, Anil Vasudevan, Justin D. Dietrich
  • Patent number: 9951057
    Abstract: The present inventions include a method of inhibiting COMT enzyme in a subject as well as compounds of formula I, or a pharmaceutically acceptable salt thereof, that are useful in the treatment of various disorders mediated by COMT, including Parkinson's disease and/or schizophrenia.
    Type: Grant
    Filed: January 29, 2016
    Date of Patent: April 24, 2018
    Assignee: LIEBER INSTITUTE FOR BRAIN DEVELOPMENT
    Inventors: James Barrow, Glen Ernst, Yifang Huang, Ingrid Price Buchler, Daniel Weinberger
  • Patent number: 9896420
    Abstract: The present invention relates to the NQBS class of molecules. It is based, at least in part, on the discovery that a representative group of compounds have been observed to inhibit nuclear translocation of NF-?B subunits. Without being bound by any particular theory, this inhibition of nuclear translocation may be mediated by either (i) binding of the NQBS or related compound to the C-terminus of the RHD, which specifically mediates the nuclear internalization; or (ii) NQBS-mediated stabilization of the dimer/I?B complex, disallowing dissociation of the active NF-?B monomers, and thus, inhibiting the generation of the subunits necessary to enter the nucleus. The NQBS class of molecules, and related molecules, may be used in therapeutic applications where inhibition of NF-?B translocation is beneficial, including but not limited to the treatment of cancer, autoimmune disorders, and inflammatory states.
    Type: Grant
    Filed: September 6, 2013
    Date of Patent: February 20, 2018
    Assignee: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK
    Inventors: Donald W. Landry, Owen O'Connor, Shi-Xian Deng, Matko Kalac, Kristen Alison Rinderspacher
  • Patent number: 9889127
    Abstract: The present invention includes a method of reducing or inhibiting the kinase activity of C-KIT mutant tyrosine kinase activity in a cell or a subject, and the use of such compound for treating mutant C-KIT driven cell proliferative disorder(s) in a subject related to using a compound of the present invention: or pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: September 2, 2016
    Date of Patent: February 13, 2018
    Assignee: AROG PHARMACEUTICALS, INC.
    Inventor: Vinay K. Jain
  • Patent number: 9834564
    Abstract: Provided herein are Cyclic Nucleotide Phosphodiesterase inhibitors, and pharmaceutical compositions thereof, useful for the treatment of, for example, central nervous system and metabolic diseases and disorder.
    Type: Grant
    Filed: February 20, 2015
    Date of Patent: December 5, 2017
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: John Emmerson Campbell, Michael Charles Hewitt, Philip Jones, Linghong Xie
  • Patent number: 9801869
    Abstract: The present invention includes a method of inhibiting or reducing deregulated FLT3 tyrosine kinase activity or FLT3 tyrosine kinase expression in a subject with a proliferative disease by administering to the subject having or suspected to have the proliferative disease, a therapeutically or prophylactically effective amount of the compound of Formula I: or pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 27, 2015
    Date of Patent: October 31, 2017
    Assignee: AROG PHARMACEUTICALS, INC.
    Inventor: Vinay K. Jain
  • Patent number: 9795599
    Abstract: Compounds of formula (I) are provided which are useful in the treatment of diseases or conditions modulated at least in part by CCR6:
    Type: Grant
    Filed: March 18, 2016
    Date of Patent: October 24, 2017
    Assignee: CHEMOCENTRYX, INC.
    Inventors: Daniel Dairaghi, Dean R. Dragoli, Jaroslaw Kalisiak, Christopher W. Lange, Manmohan Reddy Leleti, Yandong Li, Rebecca M. Lui, Venkat Reddy Mali, Viengkham Malathong, Jay P. Powers, Hiroko Tanaka, Joanne Tan, Matthew J. Walters, Ju Yang, Penglie Zhang
  • Patent number: 9730449
    Abstract: A thiazole compound represented by Formula (1): wherein R1 represents a C1-C4 alkyl group optionally having one or more fluorine atoms, R2 represents a hydrogen atom etc., R3 and R4 are the same or different and each represents a hydrogen atom etc., Ar represents a phenyl group optionally having one or more atoms or groups selected from the group A etc., and n represents 1 or 2 has excellent control activity against pests.
    Type: Grant
    Filed: December 25, 2014
    Date of Patent: August 15, 2017
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Hideki Uneme, Yasser Samir Abdelhalek Sokeirik
  • Patent number: 9656989
    Abstract: Provided herein are pentafluorosulfanyl (SF5) mefloquine derivatives, formulations, methods of making the SF5 derivatives, and uses thereof.
    Type: Grant
    Filed: May 12, 2016
    Date of Patent: May 23, 2017
    Assignee: University of Florida Research Foundation, Inc.
    Inventors: William R. Dolbier, Jr., Oleksandr S. Kanishchev
  • Patent number: 9636337
    Abstract: The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) wherein ring A, RQ, -L-, R1, n, R2, and R3 are as defined herein. The compounds of the invention are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and in methods of treating a patient (preferably a human) for diseases or disorders in which the mGluR2-NAM receptor is involved, including potentially Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: February 18, 2016
    Date of Patent: May 2, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher James Bungard, Antonella Converso, Pablo De Leon, Barbara Hanney, Timothy John Hartingh, Jesse Josef Manikowski, Peter J. Manley, Robert Meissner, Zhaoyang Meng, James J. Perkins, Michael T. Rudd, Youheng Shu
  • Patent number: 9623118
    Abstract: The present disclosure provides various molecular constructs having a targeting element and an effector element. Methods for treating various diseases using such molecular constructs are also disclosed.
    Type: Grant
    Filed: July 18, 2016
    Date of Patent: April 18, 2017
    Inventors: Tse-Wen Chang, Hsing-Mao Chu, Chun-Yu Lin
  • Patent number: 9597315
    Abstract: The invention provides novel 1-heteroaryl-3-azabicyclo[3.1.0]hexanes, and related processes and intermediates for preparing these compounds, as well as compositions and methods employing these compounds for the treatment and/or prevention of central nervous system (CNS) disorders, including but not limited to depression and anxiety.
    Type: Grant
    Filed: July 17, 2015
    Date of Patent: March 21, 2017
    Assignee: EUTHYMICS BIOSCIENCE, INC.
    Inventors: Phil Skolnick, Zhengming Chen
  • Patent number: 9591855
    Abstract: The present invention provides high potency 3,3?-diindolylmethane (DIM) and analogue compounds as antifouling agents. The present invention further provides methods of preventing or reducing settlement and/or fouling of marine fouling organisms on surfaces of submerged objects by coating the surfaces with the 3,3?-diindolylmethane (DIM) and analogue compounds provided.
    Type: Grant
    Filed: July 31, 2015
    Date of Patent: March 14, 2017
    Assignees: THE HONG KONG UNIVERSITY OF SCIENCE AND TECHNOLOGY, CHINA OCEAN MINERAL RESOURCES R&D ASSOCIATION
    Inventors: Peiyuan Qian, Ying Xu, Kailing Wang, Changyun Wang
  • Patent number: 9546159
    Abstract: The present invention relates to a compound of formula (I) in which: -m is an integer from 0 to 3, preferably from 0 to 2; n is an integer from 0 to 3, preferably from 0 to 2; m+n?1; EAG is an electro-attractive group chosen independently from among a halogen atom, an NO2, CF3, CCI3, CN, CO2H, (C?O)NR2, CH?NR, (C?S)OR, (C?O)SR, CS2R, SO2R, SO2NR2, SO3R, P(O)(OR)2, P(O)(R)2, B(OR)2 group where R is a (C1-C6) alkyl radical, a phenyl group or a hydrogen atom; A is a saturated or unsaturated, linear or branched hydrocarbon chain including 1 to 10 atoms of carbon; and R1 and R2 each represent independently from one another a hydrogen atom, a CO-(Ci-C6)-alkyl, (C1-C6) alkyl, phenyl or phenyl-(C1-C6)-alkyl group, in which R1 and R2 form, together with the nitrogen atom they carry, a 5- to 15-member heterocycle, optionally substituted by a (C1-C6) alkyl group; including its stereoisomers and the mixtures thereof, or a pharmaceutically acceptable salt of same.
    Type: Grant
    Filed: October 14, 2013
    Date of Patent: January 17, 2017
    Assignee: Centre National de la Recherche Scientifique (CNRS)
    Inventors: Pascal Collin, Maxim Egorov, Bernard Delpech, Joanna Bakala, Maria Achab, Jérome Bignon, Odile Thoison, Michel Benechie
  • Patent number: 9475795
    Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof: (I) in which m, n, W, X, Y, Z, R1, R2, R3 and R4 are as defined in the specification, for use in the treatment or prevention of a diseases o conition mediated by a prokineticin, such as psychiatric and neurological conditions.
    Type: Grant
    Filed: May 29, 2013
    Date of Patent: October 25, 2016
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Colm Carroll, Anne Goldby, Martin Teall
  • Patent number: 9427427
    Abstract: The invention relates to solid dispersions of poorly water soluble compounds, in particular Compound A as disclosed herein, formed by solvent co-precipitation or spray drying, resulting in improved bioavailability, safety and tolerability of said compounds.
    Type: Grant
    Filed: January 21, 2014
    Date of Patent: August 30, 2016
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Steve Lomuscio, Hua Ma, Michael Allen Matchett, Harpreet K. Sandhu, Navnit Hargovindas Shah, Yu-E Zhang
  • Patent number: 9365545
    Abstract: Compounds of general formula I: and compositions comprising compounds of general formula I that modulate pyruvate kinase are described herein. Also described herein are methods of using the compounds that modulate pyruvate kinase in the treatment of diseases.
    Type: Grant
    Filed: July 31, 2015
    Date of Patent: June 14, 2016
    Assignee: AGIOS PHARMACEUTICALS, INC
    Inventors: Giovanni Cianchetta, Janeta Popovici-Muller, Robert Zahler, Sheldon Cao, Xiaolei Wang, Zhixiong Ye
  • Patent number: 9308201
    Abstract: The present invention relates to a method for treating skin diseases and skin conditions in a patient in need thereof which comprises of administering a therapeutically effective amount of a pharmaceutical composition comprising a therapeutically effective amount of 7-(1H-Imidazol-4-ylmethyl)-5,6,7,8-tetrahydro-quinoline, or its individual enantiomers or the tautomers thereof, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 1, 2015
    Date of Patent: April 12, 2016
    Assignee: Allergan, Inc.
    Inventors: Mohammed I. Dibas, Edward C. Hsia, John E. Donello, Daniel W. Gil
  • Patent number: 9302993
    Abstract: The present invention describes a method for the treatment of a neurological condition in a subject which comprises administering to a subject in need thereof a therapeutically effect amount of a compound of the formula or pharmaceutically acceptable salts, hydrates, or solvates thereof.
    Type: Grant
    Filed: October 9, 2014
    Date of Patent: April 5, 2016
    Assignee: PRANA BIOTECHNOLOGY LIMITED
    Inventors: Kevin Jeffrey Barnham, Elisabeth Colette Louise Gautier, Gaik Beng Kok, Guy Krippner
  • Patent number: 9273254
    Abstract: The present invention generally relates to compositions and methods for scavenging hydrogen sulfide and/or mercaptans from fluids. More particularly, the invention relates to the use of amino acetal and ketal compounds as a hydrogen sulfide or a mercaptan scavenger for hydrocarbon fluids, particularly for natural gas, crude oil, field oil, fuel oil, naphtha, gasoline, kerosene, diesel, refinery gas, coal gas, tar, asphalt, coke gas, ammonia synthesis gas, gas from a sulfurization plant, or industrial gas streams.
    Type: Grant
    Filed: December 20, 2013
    Date of Patent: March 1, 2016
    Assignee: Ecolab USA Inc.
    Inventors: Dennis R. Compton, Kekeli Ekoue-Kovi
  • Patent number: 9259419
    Abstract: Provided herein are piperidine alkaloids and uses thereof in neurological disorders and physical enhancement applications.
    Type: Grant
    Filed: August 15, 2013
    Date of Patent: February 16, 2016
    Assignee: SYNAPSIN PHARMACEUTICALS, INC.
    Inventors: Denis Dorsey, Mark S. Kindy
  • Patent number: 9259415
    Abstract: The present disclosure relates to molecules which function as selective modulators (i.e., inhibitors and agonists) of the Ras-homologous (Rho) family of small GTPases and, in particular, CDC42 GTPase, and their use to treat bacterial infection including systemic infection from sources such as Staphylococcus aureus.
    Type: Grant
    Filed: February 22, 2013
    Date of Patent: February 16, 2016
    Assignees: Ball State Innovation Corporation, STC.UNM
    Inventors: Susan A. McDowell, Robert E. Sammelson, Larry A. Sklar, Mark K. Haynes
  • Patent number: 9257658
    Abstract: A method of making ligands for producing novel heteroleptic iridium complexes is provided. The method includes reacting the condensation product of an aryl 1,2-diamine and an aryl aldehyde with manganese dioxide in a solvent. The novel iridium complexes produced using the ligands are useful compounds in OLED devices.
    Type: Grant
    Filed: June 20, 2014
    Date of Patent: February 9, 2016
    Assignee: UNIVERSAL DISPLAY CORPORATION
    Inventors: Gregg Kottas, Chuanjun Xia, Zeinab Elshenawy, Nasrin Ansari
  • Patent number: 9233941
    Abstract: The present invention relates to methods for reducing body weight in an animal in need thereof via administration of a therapeutically effective amount of a compound having a general tripartite structure A-B-C. In the tripartite structure A, B, and C are identical or non-identical structures, for example, but not limited to, heterocyclic, phenyl or benzyl ring structures with or without substitutions and are described in detail herein. The methods may utilize particular compounds, for example, having a piperidinyl, a pyrrolinyl or pyridinyl A ring, a thiazole B ring, and a phenyl C ring which may be further substituted independently. Also provided are methods for increasing thermogenesis without reducing lean body mass during weight loss in an animal by administering of a therapeutically effective amount of the compounds described.
    Type: Grant
    Filed: May 5, 2014
    Date of Patent: January 12, 2016
    Assignee: Baylor College of Medicine
    Inventors: Motonari Uesugi, Salih J. Wakil, Lutfi Abu-Elheiga, Mizuki Watanabe
  • Patent number: 9187485
    Abstract: The present invention relates to methods of treating a disease related to cell hyper-proliferation via administration of a therapeutically effective amount of a compound having a general tripartite structure A-B-C. In the tripartite structure A, B, and C are identical or non-identical structures, for example, but not limited to, heterocyclic, phenyl or benzyl ring structures with or without substitutions and are described in detail herein. The methods may utilize particular compounds, for example, having a piperidinyl, a pyrrolinyl or pyridinyl A ring, a thiazole B ring, and a phenyl C ring which may be further substituted independently.
    Type: Grant
    Filed: October 11, 2013
    Date of Patent: November 17, 2015
    Assignee: Baylor College of Medicine
    Inventors: Motonari Uesugi, Salih J. Wakil, Lutfi Abu-Elheiga, Mizuki Watanabe
  • Patent number: 9180200
    Abstract: The invention provides pharmaceutical stable semisolid topical compositions comprising between 0.2 to 5% of a des-fluoroquinolone compound, and a suitable carrier to manufacture an ointment or a cream.
    Type: Grant
    Filed: October 16, 2009
    Date of Patent: November 10, 2015
    Assignee: FERRER INTERNATIONAL, S.A.
    Inventors: Cristina Tarragó, Benjamin Santos, Manuel Raga, Antonio Guglietta
  • Patent number: 9181219
    Abstract: The present application relates to compounds and methods for treating pain and other conditions related to TRPV3.
    Type: Grant
    Filed: January 29, 2013
    Date of Patent: November 10, 2015
    Assignee: HYDRA BIOSCIENCES, INC.
    Inventors: Magdalene M. Moran, Jayhong A. Chong, Christopher Fanger, Amy S. Ripka, Glenn R. Larsen, Xiaoguang Zhen, Dennis John Underwood, Manfred Weigele
  • Patent number: 9125904
    Abstract: Biphenyl imidazoles and related compounds of Formula I, useful as antiviral agents, are provided herein. Pharmaceutical compositions containing a compound of Formula I, together with a second active agent, such as an NS3a protease inhibitor are provided herein. Methods for treating viral infections, including Hepatitis C infections, are included herein by providing a compound of Formula I together with an additional active agent. In certain embodiments the additional active agent is an NS3a protease inhibitor.
    Type: Grant
    Filed: May 11, 2011
    Date of Patent: September 8, 2015
    Assignee: ACHILLION PHARMACEUTICALS, INC.
    Inventors: Jason Allan Wiles, Venkat Gadhachanda, Dawei Chen, Qiuping Wang, Akihiro Hashimoto, Godwin Pais, Xiangzhu Wang, Milind Deshpande, Avinash Phadke
  • Patent number: 9090559
    Abstract: The present invention provides compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Grant
    Filed: February 21, 2013
    Date of Patent: July 28, 2015
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Adrian Wai-Hing Cheung, Ryan Craig Schoenfeld, Weiya Yun, Shu-Hai Zhao
  • Patent number: 9067928
    Abstract: In one aspect, the present invention provides for a compound of Formula I in which in Formula I, the variables X1, X2a, X2b, X2c, R1, B, L, E, A and the subscript n are as defined herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xL proteins.
    Type: Grant
    Filed: June 27, 2013
    Date of Patent: June 30, 2015
    Assignees: AbbVie Inc., Genentech, Inc., The Walter and Eliza Hall Institute of Medical Research
    Inventors: Jonathan Bayldon Baell, Chinh Thien Bui, Peter Colman, Danette A. Dudley, Wayne J. Fairbrother, John A. Flygare, Guillaume Laurent Lessene, Chudi Ndubaku, George Nikolakopoulos, Carl Steven Rye, Brad Edmund Sleebs, Brian John Smith, Keith Geoffrey Watson, Steven W. Elmore, Andrew M. Petros, Andrew J. Souers, Peter Czabotar
  • Patent number: 9051299
    Abstract: The present invention is directed to imidazolyl methyl piperidine compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are 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 T-type calcium channels are involved.
    Type: Grant
    Filed: March 26, 2013
    Date of Patent: June 9, 2015
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Craig W. Lindsley, William D. Shipe
  • Publication number: 20150148377
    Abstract: The invention relates to quinoline compounds of the formula (I) and/or pharmaceutically acceptable salts and/or solvates thereof, wherein Y, W, U, Q, R1, R5 R7 and R30 are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.
    Type: Application
    Filed: December 20, 2012
    Publication date: May 28, 2015
    Applicant: NOVARTIS AG
    Inventors: Klemens Hogenauer, Konstanze Hurth, Christoph Kalis, Henrik Moebitz, Nicolas Soldermann, Frederic Zecri
  • Publication number: 20150148344
    Abstract: This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula I wherein R1, R2, R3, R4, R7, W, X, and Z are as described herein.
    Type: Application
    Filed: November 21, 2014
    Publication date: May 28, 2015
    Inventors: Kerim Babaoglu, Britton K. Corkey, Robert H. Jiang, David Sperandio, Hai Yang
  • Patent number: 9040532
    Abstract: Compounds are described herein useful for treating diseases and conditions by modulation of one or more alpha adrenergic receptor. The compounds can include a naphthalene, a quinoline, a benzoimidazole or an isoquinoline as a core structure. Methods of making, using and formulating these compounds are described.
    Type: Grant
    Filed: October 6, 2010
    Date of Patent: May 26, 2015
    Assignee: Allergan, Inc.
    Inventors: Ken Chow, Liming Wang, Wenkui K. Fang, Evelyn G. Corpuz, Santosh C. Sinha, Daniel W. Gil, Mohammad I. Dibas, John E. Donello
  • Patent number: 9040021
    Abstract: Heterocyclic compounds of formula (I) useful as imaging probes of Tau pathology in Alzheimer's disease are described. Compositions and methods of making such compounds are also described.
    Type: Grant
    Filed: November 7, 2011
    Date of Patent: May 26, 2015
    Assignee: GE Healthcare Limited
    Inventors: Clare Jones, Amanda Ewan, Duncan Wynn, Alessandra Gaeta, James Nairne
  • Patent number: 9040558
    Abstract: The invention is directed to novel substituted benzylamino quinolines, compounds comprising substituted benzylamino quinolines, methods of making substituted benzylamino quinolines, the use of substituted benzylamino quinolines for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism, and the use of substituted benzylamino quinolines as cholesterol ester-transfer protein inhibitors.
    Type: Grant
    Filed: December 28, 2005
    Date of Patent: May 26, 2015
    Assignee: DR. REDDY'S LABORATORIES LTD.
    Inventors: Anima Baruah, Dibyendu De, Ish Kumar Khanna, Sivaram Pillarisetti, Santanu Maitra, Christopher W. Alexander, Jennepalli Sreenu, Indu Dager, Shanavas Alikunju
  • Patent number: 9040561
    Abstract: Cyanine dye compounds having a substituted methine moiety that are nucleic acid stains, particularly for fluorescent staining of RNA, including compounds having the formula where R1 is a C1-C6 alkyl, sulfoalkyl, carboxyalkyl or C1-C6 alkoxy; each R2 is independently selected from the group consisting of H, C1-C6 alkyl, C1-C6 alkoxy, fused benzo, trifluoromethyl, amino, sulfo, carboxy and halogen, that is optionally further substituted; at least one of R3, R4, and R5 is an alkyl, aryl, heteroaryl, cyclic, or heterocyclic moiety that is optionally substituted by alkyl, amino, aminoalkyl, carboxy, nitro, or halogen; and the remaining R3, R4 or R5 are hydrogen; X is S, O, or Se; and D is a substituted or unsubstituted pyridinium, quinolinium or benzazolium moiety.
    Type: Grant
    Filed: May 24, 2013
    Date of Patent: May 26, 2015
    Assignee: Life Technologies Corporation
    Inventors: Jason Dallwig, David Hagen, Ching-Ying Cheung, Gerald Thomas, Stephen Yue
  • Patent number: 9040562
    Abstract: Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers, wherein each dashed line represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR7, —NH—SO2R8; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, C3-7cycloalkyl; R4 is aryl or Het; n is 3, 4, 5, or 6; R5 is halo, C1-6alkyl, hydroxy, C1-6alkoxy, phenyl, or Het; R6 is C1-6alkoxy, or dimethylamino; R7 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R8 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; aryl is phenyl optionally substituted with one, two or three substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms selected from nitroge
    Type: Grant
    Filed: May 23, 2014
    Date of Patent: May 26, 2015
    Assignees: Janssen R&D Ireland, Medivir AB
    Inventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Raboisson, Karl Magnus Nilsson, Bengt Bertil Samuelsson, Asa Annica Kristina Rosenquist
  • Publication number: 20150141423
    Abstract: Disclosed are pesticidally active pyridyl- and pyrimidyl-substituted thiazole derivatives, processes for their preparation, compositions comprising those compounds, and their use for controlling insects.
    Type: Application
    Filed: June 4, 2013
    Publication date: May 21, 2015
    Applicant: Syngenta Participations AG
    Inventors: Ruifang Chen, Laura Quaranta, Andrew Edmunds, Andre Jeanguenat, Aurelien Bigot, Sebastian Rendler, Roger Graham Hall, Long Lu, Peter Renold
  • Publication number: 20150141407
    Abstract: The present invention relates to a compound of Formula I or a pharmaceutically acceptable salt thereof, its preparation method, a pharmaceutical composition comprising the compound, and its use in manufacture of a medicament for treatment of a disease or disorder, wherein R1, R2, R5, R6, X, Y, Q, W, n1 and n2 are defined as those stated in the description.
    Type: Application
    Filed: May 30, 2013
    Publication date: May 21, 2015
    Applicant: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
    Inventors: Lan Xie, Xiaofeng Wang, Kuo-Hsiung Lee
  • Patent number: 9034888
    Abstract: Compounds of formula (I): wherein R1, R2, R3, R4, R7, R6, R7, R8, R9, A, X and Y as defined herein are provided as useful for the treatment of cancer or for the manufacture of anti-cancer agents.
    Type: Grant
    Filed: February 16, 2011
    Date of Patent: May 19, 2015
    Assignee: Universite Laval
    Inventors: René C. Gaudreault, Sébastien Fortin
  • Patent number: 9034871
    Abstract: The invention provides novel compounds useful for the treatment of neurodegenerative disorders including Alzheimer's disease and dementia. The compounds have a substituents chosen from -L-C(?O)OH, -L-CH?CHC(?O)OH, -L-C(?O)NH2, -L-C(?O)NH(C1-3 alkyl), -L-C(?O)N(C1-3 alkyl)2, -L-S(?O)2(C1-3alkyl), -L-S(?O)2NH2, -L-S(?O)2N(C1-3 alkyl)2, -L-S(?O)2NH(C1-3 alkyl), -L-C(?O)NHOH, -L-C(?O)CH2NH2, -L-C(?O)CH2OH, -L-C(?O)CH2SH, -L-C(?O)NHCN, -L-NHC(?O)ORo, -L-C(?O)NHRo, -L-NH(C?O)NHRo, -L-C(?O)N(Ro)2, -L-NH(C?O)N(Ro)2, -L-sulfo, -L-(2,6 difluorophenol), -L-phosphono, and -L-tetrazolyl, where L is a linker.
    Type: Grant
    Filed: April 13, 2012
    Date of Patent: May 19, 2015
    Inventors: Rachel Slade, Yevgeniya Klimova, Robert J. Halter, Ashantai J. Yungai, Warren S. Weiner, Ruth J. Walton, Jon Adam Willardsen, Mark B. Anderson, Kenton Zavitz
  • Publication number: 20150133495
    Abstract: Disclosed herein is a compound of Formula I or a pharmaceutically acceptable salt thereof, in which A, G, R1 and R2 are as defined herein. The compounds and pharmaceutical compositions of the compounds are suitable for the treatment of HCV infection in mammals and are also useful to modulate or inhibit NS3/4 dimerization.
    Type: Application
    Filed: November 13, 2014
    Publication date: May 14, 2015
    Inventor: Daniel Lamarre
  • Publication number: 20150133450
    Abstract: The present invention relates to compositions and methods for cancer treatment comprising compounds of Formulae I, II, and III. In some aspects, the invention relates to the treatment of B-cell Lymphoma or other hematopoietic cancers. In other aspects, the invention provides methods for treating particular types of hematopoietic cancers, such as, for example, B-cell lymphoma, using a combination of one or more compounds of Formulae I, II, and III. Combination therapy with, for example, 26S proteasome inhibitors, such as, for example, Bortezomib, are also included. In another aspect the present invention relates to autoimmune treatment with compounds of Formulae I, II, and III. In another aspect, this invention relates to methods for identifying compounds, for example, compounds of the BH3 mimic class, that have in vitro properties that predict in vivo efficacy against B-cell lymphoma tumors and other cancers as well as autoimmune disease.
    Type: Application
    Filed: June 20, 2013
    Publication date: May 14, 2015
    Inventors: Michael H. Cardone, David Richard