Patents Issued in April 17, 2018
  • Piperidine derivatives for GPR119 agonist
    Patent number: 9944600
    Abstract: The present invention relates to novel piperidine derivatives, stereoisomers thereof or pharmaceutically acceptable salts thereof; methods for preparing the compound; and pharmaceutical compositions comprising the compound. The novel piperidine derivatives, according to the present invention, having an effect as GPR119 agonist can be used for treatment of metabolic disorders, including diabetes mellitus (especially type II) and related disorders.
    Type: Grant
    Filed: June 11, 2013
    Date of Patent: April 17, 2018
    Assignee: CHONG KUN DANG PHARMACEUTICAL CORP.
    Inventors: ChangSik Lee, TaegSu Jang, DaeKyu Choi, MooSung Ko, DoHoon Kim, SoYoung Kim, JaeKi Min, WooSik Kim, YoungTae Lim
  • (Hetero)aryl cyclopropylamine compounds as LSD1 inhibitors
    Patent number: 9944601
    Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula I as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.
    Type: Grant
    Filed: September 21, 2016
    Date of Patent: April 17, 2018
    Assignee: ORYZON GENOMICS, S.A.
    Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Maria de los Àngeles Estiarte Martinez, Nuria Valls Vidal, Guido Kurz, Julio Cesar Castro Palomino Laria
  • Piperidinone herbicides
    Patent number: 9944602
    Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof: wherein R1, R2, R3, R2A, R3A, R4, R5, R6, Q1, Q2, Y1 and Y2 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: June 30, 2015
    Date of Patent: April 17, 2018
    Inventors: Andrew Duncan Satterfield, James Francis Bereznak, Matthew James Campbell
  • Compounds and methods for the treatment of cystic fibrosis
    Patent number: 9944603
    Abstract: The invention relates to a compound of Formula I and methods of treating cystic fibrosis comprising the step of administering a therapeutically effective amount of a compound of Formula I or IA to a patient in need thereof.
    Type: Grant
    Filed: April 10, 2017
    Date of Patent: April 17, 2018
    Assignee: FLATLEY DISCOVERY LAB, LLC
    Inventors: Michael P. Zawistoski, Yevgen Barsukov, Bridget M. Cole, Richard A. Nugent
  • Aminobenzamide derivatives as useful agents for controlling animal parasites
    Patent number: 9944604
    Abstract: The invention relates to a composition comprising at least one aminobenzamide compound or a salt thereof for controlling animal parasites, veterinary pharmaceutical compositions comprising at least one aminobenzamide of formula (I) for preventing infection with diseases transmitted through parasites, its use for the preparation of a veterinary pharmaceutical for controlling animal parasites, and a method for preventing infection with diseases transmitted through parasites.
    Type: Grant
    Filed: April 26, 2012
    Date of Patent: April 17, 2018
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Ulrich Görgens, Akihiko Yanagi, Kazue Yanagi, Keisuke Yanagi, Kasumi Yanagi, Katsuaki Wada, Tetsuya Murata, Yukiyoshi Watanabe, Jun Mihara, Koichi Araki
  • Farnesoid X receptor antagonists
    Patent number: 9944605
    Abstract: Provided herein are Farnesoid X receptor (FXR) antagonists having the structure of formula (I), and pharmaceutical compositions comprising the compound of formula (I) and a pharmaceutically acceptable excipient. Also provided are methods of antagonizing FXR, and methods of treating metabolic disease in a subject in need thereof, comprising administering an effective amount of the FXR antagonists of formula (I) to a subject.
    Type: Grant
    Filed: July 19, 2016
    Date of Patent: April 17, 2018
    Assignee: City of Hope
    Inventors: Barry Forman, Donna Yu
  • Cannabinoid receptor modulators
    Patent number: 9944606
    Abstract: The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor. The present invention further relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activities of both the CB1 receptor and the CB2 receptor.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: April 17, 2018
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Robert M Jones, Sangdon Han, Lars Thoresen, Jae-Kyu Jung, Sonja Strah-Pleynet, Xiuwen Zhu, Yifeng Xiong, Dawei Yue
  • Thiohydantoin derivatives and uses thereof
    Patent number: 9944607
    Abstract: The present invention provides novel compounds (e.g., compounds of Formula (I)), and pharmaceutically acceptable salts, solvates, hydrate, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits comprising the inventive Compounds, or compositions thereof, for treating and/or preventing a fungal or protozoan infection, inhibiting the activity of a fungal or protozoan enzyme, killing a fungus or protozoan, or inhibiting the growth of a fungus or protozoan. The fungus may be a Candida species, Sacchawmyces species, or other pathogenic fungal species. The compounds of the invention may inhibit the activity of fungal or protozoan mitochondrial phosphate carrier protein.
    Type: Grant
    Filed: October 16, 2013
    Date of Patent: April 17, 2018
    Assignees: Whitehead Institute for Biomedical Research, Massachusetts Institute of Technology, The Broad Institute, Inc.
    Inventors: Benjamin Vincent, Luke Whitesell, Susan L. Lindquist, Willmen Youngsaye, Stephen L. Buchwald, Jean-Baptiste Langlois, Jun Pu, Benito Munoz, Sivaraman Dandapani
  • Herbicidal pyridazinone derivatives
    Patent number: 9944608
    Abstract: The present invention relates to herbicidal benzyloxy-substituted phenyl-diones and benzyloxy substituted phenyl-dioxo-thiazinone derivatives of formula (I), as well as to processes and intermediates used for the preparation of such derivatives. The invention further extends to herbicidal compositions comprising such derivatives, as well as to the use of such compounds and compositions in controlling undesirable plant growth: in particular the use in controlling weeds, such as broad-leaved dicotyledonous weeds, in crops of useful plants.
    Type: Grant
    Filed: July 10, 2015
    Date of Patent: April 17, 2018
    Assignee: Syngenta Participations AG
    Inventors: Stephen Edward Shanahan, Paul Matthew Burton, Benjamin Andrew Egan, Timothy Jeremiah Cornelius O'Riordan
  • Formation of N-protected bis-3,6-(4-aminobutyl)-2, 5-diketopiperazine through a cyclic alpha-N-protected amino ester
    Patent number: 9944609
    Abstract: A method for the synthesis of N-protected 3,6-aminoalkyl-2,5-diketopiperazines is provided. The method includes obtaining a cyclic ?-N protected active amino ester and adding it to a mixture of an amine catalyst in an organic solvent.
    Type: Grant
    Filed: November 16, 2015
    Date of Patent: April 17, 2018
    Assignee: MannKind Corporation
    Inventors: John J. Freeman, Otto Phanstiel, William Elliot Bay, Kelly Sullivan Kraft
  • Preparation and method for use in the treatment of respiratory diseases
    Patent number: 9944610
    Abstract: The present disclosure relates to a novel active compound having the formula Ia: solid preparations, uses and methods for the treatment or prevention of respiratory diseases comprising said compound as well as process of preparation thereof.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: April 17, 2018
    Assignee: UNIVERSITÉ LAVAL
    Inventors: Evelyne Israel-Assayag, Pierre Lavallee, Yvon Cormier, Bildad Nyambura
  • Polymerizable resins containing a 1,3,5-hexahydro-1,3,5-triazine moiety, methods of making, and dental compositions containing the same
    Patent number: 9944611
    Abstract: Disclosed herein are methods of making polymerizable resins containing a 1,3,5-hexahydro-1,3,5-triazine moiety and dental compositions comprising such novel hydrolytically-stable, polymerizable resins derived from a 1,3,5-hexahydro-1,3,5-triazine.
    Type: Grant
    Filed: November 16, 2016
    Date of Patent: April 17, 2018
    Assignee: Dentsply Sirona Inc.
    Inventor: Xiaoming Jin
  • 1-phenyl-2-pyridinyl alkyl alcohol derivatives as phosphodiesterase inhibitors
    Patent number: 9944612
    Abstract: Compounds of formula (I) described herein are inhibitors of the phosphodiesterase 4 (PDE4) enzyme and are useful for the prevention and/or treatment of an allergic disease state or a disease of the respiratory tract characterized by airway obstruction.
    Type: Grant
    Filed: December 5, 2013
    Date of Patent: April 17, 2018
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Elisabetta Armani, Gabriele Amari, Oriana Esposito, Laura Carzaniga, Carmelida Capaldi
  • Fumagillol spirocyclic compounds and fused bicyclic compounds and methods of making and using same
    Patent number: 9944613
    Abstract: Disclosed herein, in part, are fumagillol compounds and methods of use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making fumagillol compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.
    Type: Grant
    Filed: November 30, 2017
    Date of Patent: April 17, 2018
    Assignee: Zafgen, Inc.
    Inventors: Robert Zahler, Zhenwei Cai, Zhixing Wu, James E. Vath
  • Production of furfural from xylose
    Patent number: 9944614
    Abstract: Described is a method for producing furfural from one or more substances selected from the group consisting of xylose, oligosaccharides comprising xylose units and polysaccha-rides comprising xylose units.
    Type: Grant
    Filed: December 10, 2014
    Date of Patent: April 17, 2018
    Assignee: BASF SE
    Inventors: Stefan Koch, Alois Kindler
  • Purifying crude furan 2,5-dicarboxylic acid by hydrogenation and a purge zone
    Patent number: 9944615
    Abstract: A process for purifying a crude furan 2,5-dicarboxylic acid composition (cFDCA) by hydrogenation of a FDCA composition dissolved in a hydrogenation solvent such as water, and hydrogenating under mild conditions, such as at a temperature within a range of 130° C. to 225° C. by contacting the solvated FDCA composition with hydrogen in the presence of a hydrogenation catalyst under a hydrogen partial pressure within a range of 10 psi to 900 psi. A product FDCA composition is produced having a low amount of tetrahydrofuran dicarboxylic acid, a low b*, and a low amount of 5-formyl furan-2-carboxylic acid (FFCA).
    Type: Grant
    Filed: July 1, 2016
    Date of Patent: April 17, 2018
    Assignee: EASTMAN CHEMICAL COMPANY
    Inventors: Mesfin Ejerssa Janka, Kenny Randolph Parker, Ashfaq Shahanawaz Shaikh, Lee Reynolds Partin, Charles Edwan Sumner, Jr., Shane Kipley Kirk
  • Processes for the preparation of Tasimelteon and intermediates thereof
    Patent number: 9944616
    Abstract: The present invention provides processes for the preparation of Tasimelteon (1), as well as processes for the preparation of intermediates of Formulas (2), (3) and (4) useful in the preparation of Tasimelteon (1).
    Type: Grant
    Filed: June 6, 2017
    Date of Patent: April 17, 2018
    Assignee: Apotex Inc.
    Inventors: Yajun Zhao, Murali Kondamreddy, Peter Garth Blazecka, Gamini Weeratunga, Craig Stewart, Nalini Nagireddy, Michael B. Johansen, Uma Kotipalli
  • Selective aerobic oxidations using carbon nitride nanotubes
    Patent number: 9944617
    Abstract: The present invention discloses an improved oxidation process using carbon nitride nanotubes as metal free catalyst and molecular O2 as the oxidant to obtain desired adipic acid and other oxygenated hydrocarbons with improved conversion and selectivity.
    Type: Grant
    Filed: December 2, 2014
    Date of Patent: April 17, 2018
    Assignee: COUNCIL OF SCIENTIFIC AND INDUSTIAL RESEARCH
    Inventors: Satyanarayana Vera Venkata Chilukuri, Narasimharao Kanna, Lakshmiprasad Gurrala
  • Inhibiting neurotransmitter reuptake
    Patent number: 9944618
    Abstract: This document relates to compounds as well as methods and materials involved in modulating neurotransmitter reuptake. For example, compounds, methods for synthesizing compounds, and methods for inhibiting neurotransmitter reuptake are provided. Specifically gamma-amino alcohol derivatives that inhibit the reuptake of neurotransmitters such as dopamine, serotonin, epinephrine or norepinephrine are provided as therapeutic agents for the treatment of depression or anxiety in a mammalian subject.
    Type: Grant
    Filed: March 10, 2014
    Date of Patent: April 17, 2018
    Assignees: Mayo Foundation for Medical Education and Research, Virginia Tech Intellectual Properties, Inc.
    Inventors: Elliott Richelson, Abdul H. Fauq, Paul Carlier, Christopher J. Monceaux
  • Compounds for the treatment of HIV
    Patent number: 9944619
    Abstract: The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I), processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.
    Type: Grant
    Filed: February 3, 2017
    Date of Patent: April 17, 2018
    Assignee: Gilead Sciences, Inc.
    Inventors: Steven S. Bondy, Carina E. Cannizzaro, Chien-Hung Chou, Randall L. Halcomb, Yunfeng Eric Hu, John O. Link, Qi Liu, Scott D. Schroeder, Winston C. Tse, Jennifer R. Zhang
  • Indolizine compounds, a process for their preparation and pharmaceutical compositions containing them
    Patent number: 9944620
    Abstract: Compounds of formula (I) wherein Ra, Rb, Rc, Rd, T, R3, R4, R5, X, Y and Het are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.
    Type: Grant
    Filed: July 22, 2014
    Date of Patent: April 17, 2018
    Assignees: LES LABORATOIRES SERVIER, VERNALIS (R&D) LTD
    Inventors: Arnaud Le Tiran, Thierry Le Diguarher, Jéròme-Benoît Starck, Jean-Michel Henlin, Guillaume De Nanteuil, Olivier Geneste, James Edward Paul Davidson, James Brooke Murray, I-Jen Chen
  • Substituted piperidinyl tetrahydroquinolines
    Patent number: 9944621
    Abstract: The present application relates to novel substituted piperidinyltetrahydroquinolines, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of diabetic microangiopathies, diabetic ulcers on the extremities, in particular for promoting wound healing of diabetic foot ulcers, diabetic heart failure, diabetic coronary microvascular heart disorders, peripheral and cardial vascular disorders, thromboembolic disorders and ischaemias, peripheral circulatory disturbances, Raynaud's phenomenon, CREST syndrome, microcirculatory disturbances, intermittent claudication, and peripheral and autonomous neuropathies.
    Type: Grant
    Filed: December 16, 2014
    Date of Patent: April 17, 2018
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Eva Maria Becker-Pelster, Philipp Buchgraber, Anja Buchmüller, Karen Engel, Volker Geiss, Andreas Göller, Herbert Himmel, Raimund Kast, Andreas Knorr, Dieter Lang, Gorden Redlich, Carsten Schmeck, Hanna Tinel, Frank Wunder
  • Pyrimidinyl tyrosine kinase inhibitors
    Patent number: 9944622
    Abstract: The present invention provides compounds and compositions thereof which are useful as inhibitors of Bruton's tyrosine kinase and which exhibit desirable characteristics for the same.
    Type: Grant
    Filed: June 29, 2016
    Date of Patent: April 17, 2018
    Assignees: Biogen MA Inc., Sunesis Pharmaceuticals, Inc.
    Inventors: Brian T. Hopkins, Timothy R. Chan, Tracy J. Jenkins, Patrick Conlon, Xiongwei Cai, Michael Humora, Xianglin Shi, Ross A. Miller, Andrew Thompson
  • Sterically hindered amine stabilizer
    Patent number: 9944623
    Abstract: The present invention relates to oxygen-substituted sterically hindered amines of the formulae I or II: (II), wherein, for example, F2, R3, R5, R6, R8, R9, R11, R12, R13, R14 are n-butyl: Z1 to Z10 are propoxy and R1, R4, R7, R10, R13 are 2,2,6,6-tetramethyl-1-propoxy-piperidin-4-yl. Compositions comprising compounds of formulae I or II and an organic material, which is susceptible to oxidative, thermal or light-induced degradation, are further disclosed. Optionally, further additives are contained.
    Type: Grant
    Filed: August 10, 2016
    Date of Patent: April 17, 2018
    Assignee: BASF SE
    Inventors: Edoardo Menozzi, Massimiliano Sala, Anna Bassi, Holger Hoppe, Björn Ludolph, Gérard Lips
  • Substituted amino triazoles useful as human chitinase inhibitors
    Patent number: 9944624
    Abstract: Disclosed are amino triazole compounds substituted with a piperidinyl ring that is itself substituted with a heterocyclic ring. These compounds are inhibitors of acidic mammalian chitinase and chitotriosidase. Also disclosed are methods of using the compounds to treat asthma reactions caused by allergens, as well as acute and chronic inflammatory diseases, autoimmune diseases, dental diseases, neurologic diseases, metabolic diseases, liver diseases, polycystic ovary syndrome, endometriosis, and cancer.
    Type: Grant
    Filed: September 2, 2016
    Date of Patent: April 17, 2018
    Assignee: OncoArendi Therapeutics S.A.
    Inventors: Marzena Mazur, Robert Koralewski, Bartlomiej Borek, Sylwia Olejniczak, Wojciech J. Czestkowski, Michał C. Piotrowicz, Jacek P. Olczak, Adam A. Golebiowski, Agnieszka Bartoszewicz, Elżbieta Maziarz, Michał Łukasz Kowalski
  • Substituted tetrahydroisoquinoline compounds as factor XIa inhibitors
    Patent number: 9944625
    Abstract: The present invention provides compounds of Formula (I): or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa and/or plasma kallikrein which may be used as medicaments.
    Type: Grant
    Filed: November 28, 2016
    Date of Patent: April 17, 2018
    Assignee: Bristol-Myers Squibb Company
    Inventors: Michael J. Orwat, Donald J. P. Pinto, Leon M. Smith, II, Shefali Srivastava
  • 6-(5-hydroxy-1H-pyrazol-1-YL)nicotinamide inhibitors of PHD
    Patent number: 9944626
    Abstract: The present invention provides compounds of the formula: which are useful as inhibitors of PHD, pharmaceutical compositions thereof, methods for treatment of conditions associated with HIF, processes for making the compounds and intermediates thereof.
    Type: Grant
    Filed: June 12, 2017
    Date of Patent: April 17, 2018
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Jason W. Brown, Melinda Davis, Anthony Ivetac, Benjamin Jones, Andre A. Kiryanov, Jon Kuehler, Marion Lanier, Joanne Miura, Sean Murphy, Xiaolun Wang
  • Spiroacridine-triazine hybrids and applications for electroluminescent devices
    Patent number: 9944627
    Abstract: The present invention relates to compounds of the formula (1), to the use thereof in electroluminescent devices, and particularly organic electroluminescence devices, comprising said compounds according to the invention.
    Type: Grant
    Filed: May 9, 2017
    Date of Patent: April 17, 2018
    Assignee: NATIONAL TAIWAN UNIVERSITY
    Inventors: Ken-Tsung Wong, Chung-Chih Wu, Tanmay Chatterjee, Ting-An Lin, Wei-Lung Tsai, Meng-Jung Wu
  • Inhibitors of cellular necrosis and related methods
    Patent number: 9944628
    Abstract: A compound having the following structure (I): or a pharmaceutically acceptable salt, prodrug, stereoisomer or tautomer thereof, is provided. Related compounds, methods for preparation of the same and uses of the compounds for treatment of various indications, including treatment of necrotic cell diseases and/or inflammation, are also provided.
    Type: Grant
    Filed: December 11, 2015
    Date of Patent: April 17, 2018
    Assignees: President and Fellows of Harvard College, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences
    Inventors: Junying Yuan, Yijun Zhou, Shan Qian, Dawei Ma
  • Material for organic electroluminescent element, organic electroluminescent element, illumination device, and display device
    Patent number: 9944629
    Abstract: A material for an organic electroluminescent element contains a compound represented by Formula (1): where R1 to R3 independently represent a group such as a deuterium atom and a halogen atom; at least one of R1 to R3 is a group represented by Formula (2); if pluralities of R1 to R3 are present, these substituents may be the same or different or may be bonded to each other to form a ring; n1 represents an integer of 0 to 8; n2 represents an integer of 0 to 3; n3 represents an integer of 0 to 4; n1+n2+n3 is 1 or more; Cbz represents a carbazolyl group; X represents an oxygen atom or a sulfur atom; and L1 represents a single bond or a divalent linking group.
    Type: Grant
    Filed: December 2, 2013
    Date of Patent: April 17, 2018
    Assignee: KONICA MINOLTA, INC.
    Inventors: Takamune Hattori, Norio Miura, Kaori Ono
  • Dithiolane carbonate monomers and polymers thereof
    Patent number: 9944630
    Abstract: 1,2-Diothiolane monomers are disclosed, as are polymers and hydrogels comprising the polymers. Processes for preparing the monomers, polymers and compositions are also disclosed.
    Type: Grant
    Filed: January 27, 2017
    Date of Patent: April 17, 2018
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Robert M. Waymouth, Gregg Barcan, Xiangyi Zhang
  • Modulators of calcium release-activated calcium channel
    Patent number: 9944631
    Abstract: Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer.
    Type: Grant
    Filed: June 28, 2017
    Date of Patent: April 17, 2018
    Assignee: RHIZEN PHARMACEUTICALS SA
    Inventors: Meyyappan Muthuppalaniappan, Srikant Viswanadha, Gayatri S. Merikapudi, Swaroop K. Vakkalanka
  • Compounds having estrogen receptor alpha degradation activity and uses thereof
    Patent number: 9944632
    Abstract: The present disclosure relates to novel compounds, pharmaceutical compositions containing such compounds, and their use in prevention and treatment of estrogen-related diseases and conditions.
    Type: Grant
    Filed: July 11, 2017
    Date of Patent: April 17, 2018
    Assignee: Accutar Biotechnology Inc.
    Inventors: Jie Fan, Ke Liu
  • Compounds and methods for the treatment of isocitrate dehydrogenase related diseases
    Patent number: 9944633
    Abstract: The invention relates to compounds of Formula I or a pharmaceutically acceptable salt, ester or prodrug thereof:
    Type: Grant
    Filed: August 4, 2015
    Date of Patent: April 17, 2018
    Assignees: The Broad Institute, Inc., PRESIDENT & FELLOWS OF HARVARD COLLEGE
    Inventors: Mahmud Hussain, Daisuke Ito, Jason Law, Matthias Leiendecker, Ke Liu, Benito Munoz, Stuart Schreiber, Alykhan Shamji, Andrew Stern
  • Pyrazolopyridine derivatives as TTX-S blockers
    Patent number: 9944634
    Abstract: The present invention relates to pyrazolopyridine 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: Grant
    Filed: October 31, 2013
    Date of Patent: April 17, 2018
    Assignee: RaQualia Pharma Inc.
    Inventors: Kiyoshi Kawamura, Tatsuya Yamagishi, Yoshimasa Arano, Mikio Morita
  • Deuterated pyrazino[2,1-a]isoquinoline compounds and methods of treatment using the same
    Patent number: 9944635
    Abstract: This invention in one embodiment is directed to a compound of Formula Ia; where the designation (R) indicates that the designated carbon has the (R) stereochemistry; and wherein Z1 is hydrogen or fluorine; Z2 is hydrogen, deuterium, or fluorine; Z3 is deuterium; Z4 is fluorine; m is an integer from 0 to 10; n is an integer from 0 to 2; provided that: the sum of m+n does not exceed 10; and when both Z1 and Z2 are hydrogen, the sum of m+n is greater than 0, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering an antihelminthic agent, such as praziquantel.
    Type: Grant
    Filed: December 3, 2015
    Date of Patent: April 17, 2018
    Assignee: Concert Pharmaceuticals, Inc.
    Inventors: Julie F. Liu, Scott L. Harbeson, Roger D. Tung
  • Inhibitors of lysine specific demethylase-1
    Patent number: 9944636
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
    Type: Grant
    Filed: December 10, 2014
    Date of Patent: April 17, 2018
    Assignee: Celgene Quanticel Research, Inc.
    Inventors: Young K. Chen, Toufike Kanouni, Stephen W. Kaldor, Jeffrey Alan Stafford, James Marvin Veal
  • P2Xand/or P2Xcompounds and methods
    Patent number: 9944637
    Abstract: The present application provides novel compounds and methods for preparing and using these compounds. In one embodiment, the compounds are of the structure of formula (I), wherein R1-R4 are defined herein. In a further embodiment, these compounds are useful in method for regulating one or both of the P2X3 or P2X2/3 receptors. In another embodiment, these compounds are useful for treating pain in patients by administering one or more of the compounds to a patient.
    Type: Grant
    Filed: December 16, 2014
    Date of Patent: April 17, 2018
    Assignee: Asana Biosciences, LLC
    Inventors: Scott K. Thompson, Aranapakam Venkatesan, Tony Priestley, Mrinal Kundu, Ashis Saha
  • Indoles as respiratory syncytial virus antiviral agents
    Patent number: 9944638
    Abstract: Indoles having inhibitory activity on RSV replication and having the formula I the prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof; compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.
    Type: Grant
    Filed: April 22, 2016
    Date of Patent: April 17, 2018
    Assignee: JANSSEN SCIENCES IRELAND US
    Inventors: Ludwig Paul Cooymans, Samuël Dominique Demin, Lili Hu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri, Sandrine Marie Helene Vendeville
  • Quinolizinone derivatives as PI3K inhibitors
    Patent number: 9944639
    Abstract: Disclosed are compounds of formula (I), their tautomeric forms, stereoisomers, and pharmaceutically acceptable salts thereof, wherein R1-R4, and n are as defined in the specification, pharmaceutical compositions including a compound, tautomer, stereoisomer, or salt thereof, and methods of treating or preventing diseases or disorders, for example, cancer, that are amenable to treatment or prevention by inhibiting the PI3K enzyme of a subject.
    Type: Grant
    Filed: July 1, 2015
    Date of Patent: April 17, 2018
    Assignee: Lupin Limited
    Inventors: Manojkumar Ramprasad Shukla, Nirmal Kumar Jana, Sachin Jaysing Mahangare, Prashant Popatrao Vidhate, Dipak Raychand Lagad, Anand Jagannath Tarage, Sanjeev Anant Kulkarni, Venkata P. Palle, Rajender Kumar Kamboj
  • Pyrimidine-2,4-diamine derivatives for treatment of cancer
    Patent number: 9944640
    Abstract: A compound of formula I, or a pharmaceutically-acceptable salt thereof. The compound is useful in the treatment of cancer or other diseases that may benefit from inhibition of MTH1.
    Type: Grant
    Filed: March 2, 2017
    Date of Patent: April 17, 2018
    Assignee: THOMAS HELLEDAYS STIFTELSE FOR MEDICINSK FORSKNING
    Inventors: Martin Scobie, Thomas Helleday, Tobias Koolmeister, Sylvain Jacques, Matthieu Desroses, Marie-Caroline Jacques-Cordonnier
  • Isoquinolinone derivatives useful in the treatment of cancer
    Patent number: 9944641
    Abstract: The present invention relates to a compound of the following formula (I) or a pharmaceutically acceptable salt and/or solvate thereof, notably for use as a drug, notably in the treatment of cancer, as well as pharmaceutical compositions containing such a compound and processes to prepare such a compound.
    Type: Grant
    Filed: September 2, 2015
    Date of Patent: April 17, 2018
    Assignee: PIERRE FABRE MEDICAMENT
    Inventors: El Bachir Kaloun, Philippe Schmitt, Anna Kruczynski
  • Factor XIa inhibitors
    Patent number: 9944643
    Abstract: The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
    Type: Grant
    Filed: February 6, 2015
    Date of Patent: April 17, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Santhosh F. Neelamkavil, Scott D. Edmondson, Alan W. Hruza, Zahid Hussain, Charles Lesburg, Remond Moningka
  • Octahydropyrrolopyrroles their preparation and use
    Patent number: 9944644
    Abstract: The present invention provides compounds comprising variously substituted octahydropyrrolopyrroles, their synthesis, methods of making, methods of using, compositions and formulations thereof.
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: April 17, 2018
    Assignee: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK
    Inventors: Konstantin Petrukhin, Christopher Cioffi, Graham Johnson, Nicoleta Dobri, Emily Freeman, Ping Chen, Michael Conlon, Lei Zhu
  • Imidazotriazines and imidazopyrimidines as kinase inhibitors
    Patent number: 9944645
    Abstract: The present invention is directed to imidazo[1,2-b][1,2,4]triazines and imidazo[1,2-a]pyrimidines, and pharmaceutical compositions thereof, which are inhibitors of kinases such as c-Met and are useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways.
    Type: Grant
    Filed: February 5, 2016
    Date of Patent: April 17, 2018
    Assignees: Incyte Corporation, Incyte Holdings Corporation
    Inventors: Jincong Zhuo, Meizhong Xu, Chunhong He, Colin Zhang, Ding-Quan Qian, David M. Burns, Yun-Long Li, Brian Metcalf, Wenqing Yao
  • Bicyclic azaheterocyclobenzylamines as PI3K inhibitors
    Patent number: 9944646
    Abstract: The present invention provides bicyclic azaheterocyclobenzylamines of Formula I: wherein the variables are defined herein, that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
    Type: Grant
    Filed: March 9, 2016
    Date of Patent: April 17, 2018
    Assignees: Incyte Holdings Corporation, Incyte Corporation
    Inventors: Andrew P. Combs, Richard B. Sparks, Thomas P. Maduskuie, Jr.
  • Heterocyclic compounds as LSD1 inhibitors
    Patent number: 9944647
    Abstract: The present invention is directed to compounds of Formula I which are LSD1 inhibitors useful in the treatment of diseases such as cancer.
    Type: Grant
    Filed: April 1, 2016
    Date of Patent: April 17, 2018
    Assignee: Incyte Corporation
    Inventors: Chunhong He, Zhenwu Li, Liangxing Wu, Wenqing Yao, Fenglei Zhang
  • Organic compounds
    Patent number: 9944648
    Abstract: The invention provides novel compounds, composition comprising said compounds and methods for inhibiting CK1 as well as methods of treating CK1 related disorders such as Alzheimer's disease comprising administering a therapeutically effective amount of a CK1 inhibitor to a patient in need thereof.
    Type: Grant
    Filed: January 9, 2015
    Date of Patent: April 17, 2018
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Qiang Zhang, Youyi Peng, Peng Li, J. David Beard, Lawrence P. Wennogle, John Tomesch
  • Compounds and compositions as toll-like receptor 7 agonists
    Patent number: 9944649
    Abstract: The invention provides a compounds, immunogenic compositions and pharmaceutical compositions comprising such compounds and methods of using such compounds to treat diseases or disorders associated with Toll-Like Receptor 7 activity.
    Type: Grant
    Filed: April 29, 2015
    Date of Patent: April 17, 2018
    Assignee: Novartis Ag
    Inventors: Alex Cortez, Timothy Hoffman, Yongkai Li, Tom Yao-Hsiang Wu, Xiaoyue Zhang
  • [1,2,4]triazolo[4,3-B]pyridazines for use in the treatment of proliferative diseases
    Patent number: 9944650
    Abstract: The invention concerns compounds of Formula (I) (Formula (I)) or pharmaceutically-acceptable salts thereof, wherein R1, R2 and n have any of the meanings defined herein before in the description; processes for their preparation, pharmaceutical compositions containing them and their use as anti-proliferative and/or cell-killing agents.
    Type: Grant
    Filed: July 24, 2015
    Date of Patent: April 17, 2018
    Assignee: AstraZeneca AB
    Inventors: Robert Hugh Bradbury, Alfred Arthur Rabow, Michael James Waring, James Francis McCabe, Steven Christopher Glossop, Arshed Mahmood, Zoe Ann Cotter