Ring Nitrogen Shared By Two Of The Cyclos Patents (Class 514/233.2)
  • Patent number: 10849901
    Abstract: Disclosed herein are compounds and methods for inhibiting Arf6. Pharmaceutical compositions and methods for treating a subject with an inhibitor of Arf6 are also disclosed herein.
    Type: Grant
    Filed: May 27, 2015
    Date of Patent: December 1, 2020
    Assignees: Navigen, Inc., The University of Utah Research Foundation
    Inventors: Kirill Ostanin, Mark Shenderovich, Ashok Bajji, Christopher L. Cioffi, Neil Moss, Hariprasad Vankayalapati, Dean Li
  • Patent number: 10821103
    Abstract: The present invention includes substituted pyridinone-containing tricyclic compounds, and compositions comprising the same, that can be used to treat or prevent hepatitis B virus (HBV) infection in a patient. In certain embodiments, the compounds and compositions of the invention inhibit and/or reduce HBsAg secretion.
    Type: Grant
    Filed: November 3, 2017
    Date of Patent: November 3, 2020
    Assignee: Arbutus Biopharma Corporation
    Inventors: Laurèn Danielle Bailey, Yingzhi Bi, Shuai Chen, Bruce D. Dorsey, Dimitar B. Gotchev, Richard James Holland, Ramesh Kakarla, Duyan Nguyen, Mark Christopher Wood
  • Patent number: 10822352
    Abstract: Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an aryl, heteroaryl or heterocycle (R32) are provided. The inhibitors of Factor D described herein reduce the excessive activation of complement.
    Type: Grant
    Filed: March 12, 2019
    Date of Patent: November 3, 2020
    Assignee: Achillion Pharmaceuticals, Inc.
    Inventors: Jason Allan Wiles, Avinash S. Phadke, Milind Deshpande, Atul Agarwal, Dawei Chen, Venkat Rao Gadhachanda, Akihiro Hashimoto, Godwin Pais, Qiuping Wang, Xiangzhu Wang
  • Patent number: 10765687
    Abstract: A compound having an antiviral activity for inhibiting release of an enveloped virus from a cell is disclosed, including methods of inhibiting release of an enveloped virus from a cell. The antiviral activity of the compound includes inhibiting formation of an associative complex or disrupting formation of an associative complex. The associative complex comprises an L-domain motif of the enveloped virus and at least one cellular polypeptide, or fragment thereof, capable of binding the L-domain motif of the enveloped virus.
    Type: Grant
    Filed: March 22, 2019
    Date of Patent: September 8, 2020
    Assignees: Northwestern University, THE RESEARCH FOUNDATION FOR THE STATE UNIVERSITY OF NEW YORK
    Inventors: Jonathan Leis, Carol Carter
  • Patent number: 10759794
    Abstract: The present application relates to novel 2-phenyl-3-(piperazinomethyl)imidazo[1,2-a]pyridine derivatives, to processes for their preparation, to their use alone or in combinations 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 treatment and/or prevention of respiratory disorders including, sleep-related respiratory disorders such as obstructive sleep apnoeas and central sleep apnoeas and snoring.
    Type: Grant
    Filed: December 7, 2016
    Date of Patent: September 1, 2020
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Martina Delbeck, Michael Hahn, Thomas Müller, Heinrich Meier, Klemens Lustig, Johanna Mosig, Luisella Toschi, Udo Albus, Doris Gehring, Björn Rosenstein
  • Patent number: 10752622
    Abstract: The present invention relates to novel compounds of formula (I), process for preparation of the same and composition comprising these compounds.
    Type: Grant
    Filed: December 24, 2018
    Date of Patent: August 25, 2020
    Assignee: MANKIND PHARMA LTD.
    Inventors: Rakesh Ishwar Patil, Jeevan Verma, Puneet Kumar, Amol Pandurang Gunjal, Himanshu Rai, Santosh Kumar Rai, Anil Kumar
  • Patent number: 10738056
    Abstract: The present invention relates to pyrazolopyrimidinone compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating autoimmune, inflammatory, and neurodegenerative diseases by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
    Type: Grant
    Filed: September 14, 2018
    Date of Patent: August 11, 2020
    Assignee: Aduro BioTech Inc.
    Inventors: Chudi Obioma Ndubaku, George Edwin Katibah, Tucker Curran Roberts, Leonard Sung, Stephane Ciblat, Franck Raeppel, Vu Linh Ly, Yeeman K. Ramtohul, Taras Rybak, Mariam Zaky, Laura Gillard, Hossein Ismaili
  • Patent number: 10653695
    Abstract: Disclosed are oral pharmaceutical compositions of neflamapimod that exhibit suitable exposure for administration in humans and/or that maintain a desirable dissolution profile under standard storage conditions.
    Type: Grant
    Filed: March 12, 2019
    Date of Patent: May 19, 2020
    Assignee: EIP Pharma, LLC
    Inventors: John Jahangir Alam, Jeffrey Douglas Wilson
  • Patent number: 10568879
    Abstract: A compound according to Formula I: wherein R1, LA, CyA, RA, R2, R3, and R4 are as described herein. The present invention relates to novel compounds according to Formula I that antagonize GPR84, a G-protein-coupled receptor that is involved in inflammatory conditions, and methods for the production of these novel compounds, pharmaceutical compositions comprising these compounds, and methods for the prevention and/or treatment of inflammatory conditions, pain, neuroinflammatory conditions, neurodegenerative conditions, infectious diseases, autoimmune diseases, endocrine and/or metabolic diseases, cardiovascular diseases, leukemia, and/or diseases involving impairment of immune cell functions by administering a compound of the invention.
    Type: Grant
    Filed: April 19, 2016
    Date of Patent: February 25, 2020
    Assignee: GALAPAGOS NV
    Inventors: Christel Jeanne Marie Menet, Julien Georges Pierre-Olivier Doyon, Pieter Isabelle Roger Claes, Brigitte Allart, Maxim Maria Paul De Wachter, Giovanni Alessandro Tricarico
  • Patent number: 10556869
    Abstract: The present invention relates to a process for providing the compound of formula I, comprising the step of reacting a compound of formula VII with a base in the presence of an alkaline- or alkaline earth metal salt (MX), wherein LG is a leaving group. The presence of an alkaline- or alkaline earth metal salt was surprisingly found to render said reaction highly reliable in terms of the yield and purity of the compound of formula I obtained. In a further aspect, the present invention relates to the compound of formula I, having less than an amount of 1.50% or less than an amount of 1.25% or less than an amount of 1.00% or less than an amount of 0.75% or less than an amount of 0.50% or less than an amount of 0.25% or less than an amount of 0.10% of the compound of formula VIII.
    Type: Grant
    Filed: January 28, 2016
    Date of Patent: February 11, 2020
    Assignee: Novartis AG
    Inventors: Andreas Bertogg, Hanspeter Schilling
  • Patent number: 10457683
    Abstract: The disclosure relates to aryl hydrocarbon receptor antagonists, such as substituted imidazopyridines and imidazopyrazines, as well as methods of expanding hematopoietic stem cells by culturing hematopoietic stem or progenitor cells in the presence of these agents. Additionally, the disclosure provides methods of treating various pathologies in a patient by administration of expanded hematopoietic stem cells. The disclosure further provides methods of synthesizing aryl hydrocarbon receptor antagonists, such as substituted imidazopyridines and imidazopyrazines, as well as kits containing aryl hydrocarbon receptor antagonists that can be used for the expansion of hematopoietic stem cells.
    Type: Grant
    Filed: April 12, 2018
    Date of Patent: October 29, 2019
    Assignee: Magenta Therapeutics Inc.
    Inventor: Arthur Glenn Romero
  • Patent number: 10399995
    Abstract: The present invention provides a compound of Formula I: or a pharmaceutically acceptable salt thereof, useful as a BACE1 inhibitor.
    Type: Grant
    Filed: August 18, 2017
    Date of Patent: September 3, 2019
    Assignee: Eli Lilly and Company
    Inventors: Steven James Green, Erik James Hembre, II, Dustin James Mergott
  • Patent number: 10364245
    Abstract: Compounds of formula (I) defined herein are p38 MAPK inhibitors and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.
    Type: Grant
    Filed: May 23, 2018
    Date of Patent: July 30, 2019
    Assignee: CHIESI FARMACEUTICI S.p.A.
    Inventors: Carmelida Capaldi, Elisabetta Armani, Christopher Hurley, Barbara Giuseppina Avitabile-Woo, Roberta Lanaro, Neil Stuart Jennings
  • Patent number: 10351572
    Abstract: The disclosure relates to aryl hydrocarbon receptor antagonists, such as substituted imidazopyridines and imidazopyrazines, as well as methods of expanding hematopoietic stem cells by culturing hematopoietic stem or progenitor cells in the presence of these agents. Additionally, the disclosure provides methods of treating various pathologies in a patient by administration of expanded hematopoietic stem cells. The disclosure further provides methods of synthesizing aryl hydrocarbon receptor antagonists, such as substituted imidazopyridines and imidazopyrazines, as well as kits containing aryl hydrocarbon receptor antagonists that can be used for the expansion of hematopoietic stem cells.
    Type: Grant
    Filed: February 8, 2019
    Date of Patent: July 16, 2019
    Assignee: Magenta Therapeutics Inc.
    Inventor: Arthur Glenn Romero
  • Patent number: 10342795
    Abstract: The present invention relates to substituted 4,5,6,7-tetrahydro-pyrazolo[1,5-a]pyrimidine derivatives and 2,3-dihydro-1H-imidazo[1,2-b]pyrazole derivatives of formula (I) and also compounds of formula (I?) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as ROS1 inhibitors. The invention further relates to processes for preparing novel compounds of the present invention, pharmaceutical compositions comprising compounds of the present invention as an active ingredient as well as the use of compounds of the present invention as a medicament.
    Type: Grant
    Filed: March 26, 2015
    Date of Patent: July 9, 2019
    Assignee: Janssen Pharmaceutica NV
    Inventors: Laurence Anne Mevellec, Matthieu Ludovic Jeanty, Thierry Francois Alain Jean Jousseaume
  • Patent number: 10335411
    Abstract: Disclosed are methods for the treatment of cancer in patients in need of such treatment. The methods comprise administering to such a patient an ubiquitin-activating enzyme (UAE) inhibitor such as ((1R,2R,3S,4R)-2,3-dihydroxy-4-(2-(3-(trifluoromethylthio) phenyl)pyrazolo[1,5-a]pyrimidin-7-ylamino)cyclopentyl)methyl sulfamate (Compound 1) or a pharmaceutically acceptable salt in combination with radiation. Also disclosed are medicaments for use in the treatment of cancer.
    Type: Grant
    Filed: October 23, 2015
    Date of Patent: July 2, 2019
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Neil Bence, Marc Hyer, Michael Milhollen, Vivek Samnotra, Sergio Luis Santillana Soto, Darshan Sappal
  • Patent number: 10328066
    Abstract: The present disclosure pertains to a pharmaceutical combination comprising (a) an alpha-isoform specific PI3K inhibitor, (b) a cyclin dependent kinase 4/6 (CDK4/6) inhibitor, and (c) an antimetabolite antineoplastic agent; combined preparations and pharmaceutical compositions thereof; the uses of such a combination in the treatment or prevention of cancer; and methods of treating or preventing cancer in a subject comprising administering a therapeutically effective amount of such combination.
    Type: Grant
    Filed: August 24, 2016
    Date of Patent: June 25, 2019
    Assignee: Novartis AG
    Inventors: Giordano Caponigro, Thomas Horn-Spirohn, Joseph Lehar
  • Patent number: 10258615
    Abstract: The present invention provides a method of treating or ameliorating a neurodegenerative disease in a mammal, the method comprising administering to the mammal a therapeutically effective amount of a neurodegenerative disease drug, wherein the drug is a substrate of an ABC transporter inhibitor, wherein the mammal is further administered a therapeutically effective amount of an ABC transporter inhibitor, whereby the neurodegenerative disease is treated in the mammal. In certain embodiments, the neurodegenerative disease comprises at least one selected from the group consisting of spinal cord injury, Alzheimer's disease, Parkinson's disease, Huntington's disease, prion disease, amyotrophic lateral sclerosis, a tauopathy, and chronic traumatic encephalopathy.
    Type: Grant
    Filed: December 9, 2014
    Date of Patent: April 16, 2019
    Assignee: Thomas Jefferson University
    Inventors: Davide Trotti, Piera Pasinelli, Michael R. Jablonski
  • Patent number: 10253043
    Abstract: The invention relates to the novel products of formula (I) with p, q=0, 1 or 2; R1=phenyl, pyridyl; —(CH2)m—Ra; alkylene; cycloalkyl; heterocycloalkyl; alkyl; —SO2 —Rb; —CO—Re; m=1 or 2; Ra=aryl, heteroaryl, —CO-cycloalkyl, —CO-heterocycloalkyl, —CO—Rb, —C(Rb)?N—ORc, —CO 2 Rd, —CONRxRy; Rb=alkyl, aryl, heteroaryl; Rc=H, alkyl; Rd=alkyl, cycloalkyl; Re=alkyl, cycloalkyl, aryl, heteroaryl; NRxRy with Rx,Ry=H, alkyl, cycloalkyl, alkoxy, phenyl, or form with N a ring with optionally O, N; R2, R3=H, alkyl, CF 3, or form with C a ring with optionally O, S and N; R4=H, F, Cl, CH3 or CN; the morpholine is substituted with Me, and optionally substituted with F, OH; or is (Formula 1a) and the isomer of configuration R,R (Formula 1b) these products being in all the isomer forms and the salts, as medicaments, in particular as anticancer medicaments.
    Type: Grant
    Filed: June 21, 2013
    Date of Patent: April 9, 2019
    Assignee: SANOFI
    Inventors: Youssef El-Ahmad, Bruno Filoche-Romme, Jean-Philippe Letallec, Gilbert Marciniak, Baptiste Ronan, Bertrand Vivet, Maurice Brollo
  • Patent number: 10208030
    Abstract: The present invention relates to novel compounds of formula (I), process for preparation of the same and composition comprising these compounds.
    Type: Grant
    Filed: April 4, 2017
    Date of Patent: February 19, 2019
    Assignee: Mankind Pharma Ltd.
    Inventors: Rakesh Ishwar Patil, Jeevan Verma, Puneet Kumar, Amol Pandurang Gunjal, Himanshu Rai, Santosh Kumar Rai, Anil Kumar
  • Patent number: 10189840
    Abstract: Disclosed are compounds of Formula (I) or a salt thereof, wherein: X is N; W is: (i) —(CR3R3)1-4—; (ii) —(CR3R3)x—Y—(CR3R3)y—; Or (iii) —Y—(CR3R3)2—Y—; and Y, R1, R2, R3, R5, R6, R8, x, and y are defined herein. Also disclosed are methods of using such compounds as modulators of TNF?, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.
    Type: Grant
    Filed: March 17, 2016
    Date of Patent: January 29, 2019
    Assignee: Bristol-Myers Squibb Company
    Inventors: Hai-Yun Xiao, Murali T. G. Dhar, Jingwu Duan, Bin Jiang, Andrew J. Tebben
  • Patent number: 10160991
    Abstract: Disclosed herein are methods determining susceptibility of bacteria in a sample from a subject suspected of having an infection to a plurality of antibiotics simultaneously, wherein the sample is tested without first isolating the bacteria from the sample.
    Type: Grant
    Filed: April 19, 2018
    Date of Patent: December 25, 2018
    Assignee: CAP DIAGNOSTICS, LLC
    Inventors: David A. Baunoch, Miguel F. R. Penaranda, Michael L. Opel, Maher Badir
  • Patent number: 10131673
    Abstract: The invention concerns novel substituted tricyclic pyrazolo pyrimidine compounds of formula (I-a) or (I-b) having antiviral activity, in particular, having an inhibitory activity on the replication of the respiratory syncytial virus (RSV). The invention further concerns the preparation of such novel compounds, compositions comprising these compounds, and the compounds for use in the treatment of respiratory syncytial virus infection.
    Type: Grant
    Filed: December 7, 2015
    Date of Patent: November 20, 2018
    Assignee: Janssen Sciences Ireland UC
    Inventors: Abdellah Tahari, Sandrine Marie Helene Vendeville, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Samuël Dominique Demin, Lili Hu
  • Patent number: 10125123
    Abstract: Described herein are IRE1? inhibitors, compositions containing such inhibitors, and methods of treatment that include administration of such compounds. Exemplary compounds are provided throughout the application.
    Type: Grant
    Filed: March 3, 2017
    Date of Patent: November 13, 2018
    Assignee: CORNELL UNIVERSITY
    Inventors: Laurie H. Glimcher, Sarah Elizabeth Bettigole, Juan Rodrigo Cubillos Ruiz, Joseph P. Vacca
  • Patent number: 10112944
    Abstract: Disclosed are compounds of Formula (I) or a salt thereof, wherein: X is CR6 or N; W is: (i) —(CR3R3)1-4— or (ii) —(CR3R3)x-Y—(CR3R3)y-; and Y, R1, R2, R3, R5, R6, R7, x, and y are define herein. Also disclosed are methods of using such compounds as modulators of TNF?, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.
    Type: Grant
    Filed: March 17, 2016
    Date of Patent: October 30, 2018
    Assignee: Bristol-Myers Squibb Company
    Inventors: Lawrence R. Marcin, Stephen T. Wrobleski, T.G. Murali Dhar
  • Patent number: 10100059
    Abstract: This disclosure is directed to agonists of the apelin receptor (APJ) and uses of such agonists.
    Type: Grant
    Filed: December 9, 2016
    Date of Patent: October 16, 2018
    Assignee: Research Triangle Institute
    Inventors: Scott P. Runyon, Rangan Maitra, Sanju Narayanan, James Barnwell Thomas, Kenneth S. Rehder, Srinivas Olepu
  • Patent number: 10085992
    Abstract: This invention is in the area of improved compounds, compositions and methods of transiently protecting healthy cells, and in particular hematopoietic stem and progenitor cells (HSPC) as well as renal cells, from damage associated with DNA damaging chemotherapeutic agents. In one aspect, improved protection of healthy cells is disclosed using disclosed compounds that act as highly selective and short, transiently-acting cyclin-dependent kinase 4/6 (CDK 4/6) inhibitors when administered to subjects undergoing DNA damaging chemotherapeutic regimens for the treatment of proliferative disorders.
    Type: Grant
    Filed: November 3, 2016
    Date of Patent: October 2, 2018
    Assignee: G1 Therapeutics, Inc.
    Inventors: Jay Copeland Strum, John Emerson Bisi, Patrick Joseph Roberts, Francis Xavier Tavares
  • Patent number: 10076523
    Abstract: This invention is in the area of improved compounds for and methods of treating selected RB-positive cancers and other Rb-positive abnormal cellular proliferative disorders while minimizing the deleterious effects on healthy cells, for example healthy Hematopoietic Stem Cells and Progenitor Cells (HSPCs), associated with current treatment modalities. In one aspect, improved treatment of select RB-positive cancers is disclosed using specific compounds disclosed herein. In certain embodiments, the compounds described herein act as highly selective and, in certain embodiments, short, transiently-acting cyclin-dependent kinase 4/6 (CDK 4/6) inhibitors when administered to subjects.
    Type: Grant
    Filed: December 21, 2016
    Date of Patent: September 18, 2018
    Assignee: G1 Therapeutics, Inc.
    Inventors: Jay Copeland Strum, John Emerson Bisi, Patrick Joseph Roberts, Francis Xavier Tavares
  • Patent number: 10053464
    Abstract: A series of substituted [1,2,4]triazolo[4,3-b]pyridazine derivatives of formula (I), being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
    Type: Grant
    Filed: December 8, 2014
    Date of Patent: August 21, 2018
    Assignee: UCB BIOPHARMA SPRL
    Inventor: Daniel Christopher Brookings
  • Patent number: 9988365
    Abstract: Provided herein are 2-(2,4-difluorophenyl)-1,1-difluoro-1-(5-substituted-pyridin-2-yl)-3-(1H-tetrazol-1-yl)propan-2-ols and 1-(2,4-difluorophenyl)-2,2-difluoro-2-(5-substituted-pyridin-2-yl)ethanones and processes for their preparation.
    Type: Grant
    Filed: March 19, 2015
    Date of Patent: June 5, 2018
    Assignee: VPS-3, Inc.
    Inventors: William J. Hoekstra, Nakyen Choy, Carl DeAmicis, Daniel Knueppel, Jim Renga, Michael T. Sullenberger, Gregory Whiteker, Yuanming Zhu, Gary D. Gustafson
  • Patent number: 9980982
    Abstract: The invention provides compositions and methods for utilizing human epididymal secretion protein E4 (HE4) in the prevention and treatment of cancer and other human diseases.
    Type: Grant
    Filed: June 6, 2012
    Date of Patent: May 29, 2018
    Assignee: Women & Infants Hospital of Rhode Island
    Inventors: Richard G. Moore, Rakesh K. Singh
  • Patent number: 9931345
    Abstract: This invention is in the area of improved compounds, compositions and methods of transiently protecting healthy cells, and in particular hematopoietic stem and progenitor cells (HSPC) as well as renal cells, from damage associated with DNA damaging chemotherapeutic agents. In one aspect, improved protection of healthy cells is disclosed using disclosed compounds that act as highly selective and short, transiently-acting cyclin-dependent kinase 4/6 (CDK 4/6) inhibitors when administered to subjects undergoing DNA damaging chemotherapeutic regimens for the treatment of proliferative disorders.
    Type: Grant
    Filed: October 7, 2016
    Date of Patent: April 3, 2018
    Assignee: Presidents and Fellows of Harvard College
    Inventors: Jay Copeland Strum, John Emerson Bisi, Patrick Joseph Roberts, Francis Xavier Tavares
  • Patent number: 9932334
    Abstract: A series of substituted 4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine derivatives, being potent treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
    Type: Grant
    Filed: December 8, 2014
    Date of Patent: April 3, 2018
    Assignee: UCB BIOPHARMA SPRL
    Inventors: Victoria Elizabeth Jackson, Boris Kroeplien, Martin Alexander Lowe, John Robert Porter
  • Patent number: 9902727
    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: Grant
    Filed: November 25, 2014
    Date of Patent: February 27, 2018
    Assignee: Bayer Intellectual Property GmbH
    Inventors: William Scott, Ningshu Liu, Manfred Möwes, Andrea Hägebarth, Ursula Mönning, Ulf Bömer
  • Patent number: 9902723
    Abstract: The present invention provides a method for manufacturing a compound represented by formula (I). With this method, provided is a method for manufacturing a 4-substituted-N-(2-phenyl-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-1H-pyrazole-5-carboxylic acid amide derivative; or an intermediate for this manufacturing method.
    Type: Grant
    Filed: July 29, 2015
    Date of Patent: February 27, 2018
    Assignee: MOCHIDA PHARMACEUTICAL CO., LTD.
    Inventors: Tsutomu Satoh, Takashi Kudoh, Tetsuo Iwama
  • Patent number: 9896459
    Abstract: Azaindoles having inhibitory activity on RSV replication and having the formula I compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.
    Type: Grant
    Filed: May 12, 2016
    Date of Patent: February 20, 2018
    Assignee: Janssen Sciences Ireland UC
    Inventors: Ludwig Paul Cooymans, Samuël Dominique Demin, Lili Hu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri, Sandrine Marie Helene Vendeville
  • Patent number: 9879009
    Abstract: The present invention provides a method for manufacturing a compound represented by formula (I). With this method, provided are a method for manufacturing a 4-heteroaryl-N-(2-phenyl-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-1H-pyrazole-5-carboxylic acid amide derivative; and an intermediate for this manufacturing method.
    Type: Grant
    Filed: July 29, 2015
    Date of Patent: January 30, 2018
    Assignee: MOCHIDA PHARMACEUTICAL CO., LTD.
    Inventors: Tsutomu Satoh, Takashi Kudoh, Tetsuo Iwama
  • Patent number: 9850240
    Abstract: A series of substituted [1,2,4]triazolo[4,3-a]pyridine derivatives, being potent modulators of human TNF activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
    Type: Grant
    Filed: December 8, 2014
    Date of Patent: December 26, 2017
    Assignee: UCB BIOPHARMA SPRL
    Inventors: Daniel Christopher Brookings, Victoria Elizabeth Jackson
  • Patent number: 9828350
    Abstract: The present invention relates to novel 5,6-dihydro-2H-[1,4]oxazin-3-ylamine derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease and dementia associated with beta-amyloid.
    Type: Grant
    Filed: February 5, 2016
    Date of Patent: November 28, 2017
    Assignee: Janssen Pharmaceutica NV
    Inventors: Andrés Avelino Trabanco-Suárez, Frederik Jan Rita Rombouts, Gary John Tresadern, Michiel Luc Maria Van Gool, Gregor James Macdonald, Carolina Martinez Lamenca, Henricus Jacobus Maria Gijsen
  • Patent number: 9801961
    Abstract: The present invention relates to compounds of general formula wherein R1 is (a) phenyl, optionally substituted by one or two substituents selected from 3H, halogen, lower alkyl, di-methyl-amino, NHC(O)-lower alkyl, C(O)O-lower alkyl, lower alkoxy, OC(3H)3, O11CH3, OCH2CH218F, lower alkoxy substituted by halogen, hydroxy, lower alkyl substituted by hydroxy, S-lower alkyl, (b) heterocyclyl group, (c) benzo[d][1,3]dioxol-5-yl, (d) 2,3-dihydrobenzo[b][1,4]dioxin-6-yl, (e) indolin-2-one, or (f) heteroaryl, selected from the group consisting of thiophenyl, benzofuranyl, benzothiophenyl, pyrazinyl, and benzothiazolyl; R2 is hydrogen, lower alkyl or lower alkyl substituted by halogen; R3 is lower alkyl, C(3H)3, 11CH3, lower alkyl substituted by halogen, —(CH2)2—O-lower alkyl substituted by halogen or cycloalkyl; or R2 and R3 form together with the N-atom to which they are attach a ring containing —CH2CH2CHRCH2CH2—, —CH2CH2CHRCH2—, —CH2CHRCH2—, —CH2CH2—NR—CH2CH2—, —CH2CH2—O—CH2CH2—, or, R is hydrogen, halog
    Type: Grant
    Filed: November 19, 2015
    Date of Patent: October 31, 2017
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Luca Gobbi, Henner Knust, Matthias Koerner, Dieter Muri
  • Patent number: 9789087
    Abstract: Disclosed herein are methods for determining whether a PAR4 inhibitor should be administered to a human subject, the methods comprising administering a PAR4 inhibitor to a subject determined to have a “G” allele for a single-nucleotide polymorphism (SNP) at rs773902, and not administering a PAR4 inhibitor to a subject determined to have an “A” allele for the SNP at rs773902. A genotyping assay can be used to determine the SNP.
    Type: Grant
    Filed: August 2, 2016
    Date of Patent: October 17, 2017
    Assignee: THOMAS JEFFERSON UNIVERSITY
    Inventors: Paul Bray, Michael Holinstat, Leonard Edelstein
  • Patent number: 9783543
    Abstract: The present invention relates to amino-substituted imidazopyridazine compounds of general formula (I), in which A, R1, R2, R3, R4 and n are as defined in the claims, 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: November 14, 2013
    Date of Patent: October 10, 2017
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Ludwig Zorn, Knut Eis, Volker Schulze, Detlev Sülzle, Florian Puehler, Philip Lienau, Ulf Bömer, Kirstin Petersen, Andrea Hägebarth
  • Patent number: 9745304
    Abstract: The present invention relates to amido-substituted imidazopyridazine compounds of general formula (I): in which A, R1, R2, R3, R4 and n are as defined in the claims, 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: January 28, 2014
    Date of Patent: August 29, 2017
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Ludwig Zorn, Knut Eis, Volker Schulze, Detlev Sülzle, Florian Puehler, Philip Lienau, Ulf Bömer, Kirstin Petersen, Andrea Hägebarth
  • Patent number: 9708312
    Abstract: A compound according to Formula (Ia), wherein Cy, L1, G, and R1 are as described herein. The present invention relates to novel compounds according to Formula (I) that antagonize GPR84, a G-protein-coupled receptor that is involved in inflammatory conditions, and methods for the production of these novel compounds, pharmaceutical compositions comprising these compounds, and methods for the prevention and/or treatment of inflammatory conditions (for example inflammatory bowel diseases (IBD), rheumatoid arthritis, vasculitis), lung diseases (e.g. chronic obstructive pulmonary disease (COPD) and lung interstitial diseases (e.g. idiopathic pulmonary fibrosis (IPF))), neuroinflammatory conditions, infectious diseases, autoimmune diseases, endocrine and/or metabolic diseases, and/or diseases involving impairment of immune cell functions by administering a compound of the invention.
    Type: Grant
    Filed: December 17, 2013
    Date of Patent: July 18, 2017
    Assignee: GALAPAGOS NV
    Inventors: Frédéric Gilbert Labéguère, Gregory John Robert Newsome, Luke Jonathan Alvey, Laurent Raymond Maurice Sanière, Stephen Robert Fletcher
  • Patent number: 9682992
    Abstract: The subject of the present invention are water-soluble derivatives of camptothecin, their synthesis and use. These compounds exhibit preferable biological properties for use in anti-neoplasm therapy.
    Type: Grant
    Filed: October 25, 2013
    Date of Patent: June 20, 2017
    Assignees: INSTYTUT CHEMII ORGANICZNEJ POLSKIEJ AKADE, NARODOWY INSTYTUT LEKÓW
    Inventors: Lech Kozerski, Robert Kawęcki, Beata Naumczuk, Karolina Hyz, Wojciech Bocian, Jerzy Sitkowski, Elżbieta Bednarek, Katarzyna Wiktorska, Katarzyna Lubelska
  • Patent number: 9675549
    Abstract: Provided herein is a tablet comprising, as a drug, N-(5-tert-butyl-isoxazol-3-yl)-N?-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea or a pharmaceutically acceptable salt thereof, which is a medicament for treating acute myeloid leukemia (AML), the tablet characterized by comprising a composite of N-(5-tert-butyl-isoxazol-3-yl)-N?-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea or a pharmaceutically acceptable salt thereof and hydroxypropyl-?-cyclodextrin in a ratio ranging from 1:8 to 1:20.
    Type: Grant
    Filed: September 30, 2013
    Date of Patent: June 13, 2017
    Assignee: Ambit Biosciences Corporation
    Inventors: Shinsuke Oba, Hiroyasu Toyota, Satomi Ikeuchi, Takumi Hara, Emiko Murayama, Kei Motonaga
  • Patent number: 9669035
    Abstract: The present invention relates to combinations of phosphodiesterase 2 (PDE2) inhibitors with inhibitors of phosphodiesterase 10 (PDE10). In particular, the invention relates to combinations of 1-aryl-4-methyl-[1,2,4]triazolo[4,3-a]-quinoxaline derivatives which have been found to inhibit phosphodiesterase 2 (PDE2), with inhibitors of phosphodiesterase 10 (PDE10). Particular PDE10 inhibitors are selected from the group of MP-10, PQ-10, TP-10, papaverine, and the compounds disclosed in WO 2011/051324 and in WO 2011/110545.
    Type: Grant
    Filed: June 25, 2013
    Date of Patent: June 6, 2017
    Assignee: JANSSEN PHARMACEUTICA NV
    Inventors: Antonius Adrianus Hendrikus Petrus Megens, Xavier Jean Michel Langlois, José Ignacio Andrés-Gil
  • Patent number: 9649317
    Abstract: The present invention is directed to triazolopyrimidine, phenylpyrimidine, pyridopyridazine, and pyridotriazine compounds which are microtubule-stabilizing compounds and their use in the treatment of neurodegenerative disorders, in particular, tauopathies, such as for example, Alzheimer's disease, frontotemporal lobar degeneration, Pick's disease, progressive supranuclear palsy (PSP), and corticobasal degeneration. In addition, the compounds of the invention may be useful for other diseases where tau pathology is a comorbidity or where microtubule function is compromised, for example, schizophrenia, Parkinson's disease (PD), PD with dementia, Lewy body disease with dementia, and amyotrophic lateral sclerosis.
    Type: Grant
    Filed: September 19, 2013
    Date of Patent: May 16, 2017
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: Carlo Ballatore, Kurt R. Brunden, Adam T. Hoye, Virginia M. Y. Lee, Amos B. Smith, John Q. Trojanowski
  • Patent number: 9550771
    Abstract: Compounds of the formula I or II: or pharmaceutically acceptable salts thereof, wherein R1 is a group of formula (a), (b), (c); (d) or (e): and m, n, X, Y, R1, R2, R3, R4, Rb and Rc are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Grant
    Filed: September 10, 2014
    Date of Patent: January 24, 2017
    Assignee: Genentech, Inc.
    Inventors: Benjamin Fauber, Alberto Gobbi
  • Patent number: 9518240
    Abstract: A method for treating liquefied hydrocarbons including acid gases to remove said acid gases while minimizing loss of amine species, he method comprising the step of contacting he liquefied hydrocarbons with an absorbent aqeuous solution of a first amine compound, the first amine compound having the structure: wherein R1 is hydrogen or propane-2,3-diol and R2 is propane-2,3-diol, or mixtures thereof.
    Type: Grant
    Filed: June 11, 2013
    Date of Patent: December 13, 2016
    Assignee: Dow Global Technologies LLC
    Inventors: Christophe R. Laroche, James M. Hill