The Additional Hetero Ring Contains Ring Nitrogen Patents (Class 514/210.2)
  • Patent number: 10344020
    Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system.
    Type: Grant
    Filed: October 13, 2016
    Date of Patent: July 9, 2019
    Assignee: Bristol-Myers Squibb Company
    Inventors: Imadul Islam, Srinivasan Thangathirupathy, Jayakumar Sankara Warrier, Srinivas Cheruku, Poornima Shetty, Grandhi Venkat Ram Krishna Mohan Gupta, John E. Macor
  • Patent number: 10343992
    Abstract: The present invention relates to novel compounds and method for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase 30 (USP30). The invention further relates to the use of DUB inhibitors in the treatment of conditions involving mitochondrial dysfunction and cancer. Compounds of the invention include compounds having the formula (II) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R8, R9, R10, R12, Z, Y and m are as defined herein.
    Type: Grant
    Filed: March 24, 2016
    Date of Patent: July 9, 2019
    Assignee: Missions Therapeutics Limited
    Inventors: Alison Jones, Mark Kemp, Martin Stockley, Karl Gibson, Gavin Whitlock
  • Patent number: 10301289
    Abstract: The present invention relates to a process for preparing 1-[6-(morpholin-4-yl)pyrimidin-4-yl]-4-(1H-1,2,3-triazol-1-yl)-1H-pyrazol-5-ol (I—enol form) or 2-[6-(morpholin-4-yl)pyrimidin-4-yl]-4-(1H-1,2,3-triazol-1-yl)-1,2-dihydro-3H-pyrazol-3-one (I—keto form) and sodium 1-[6-(morpholin-4-yl)pyrimidin-4-yl]-4-(1H-1,2,3-triazol-1-yl)-1H-pyrazol-5-olate (II) from 1,2,3-triazole (III), methyl bromoacetate (IV-Me-Br) or ethyl bromoacetate (IV-Et-Br), 4,6-dichloropyrimidine (VIII), morpholine (IX) and hydrazine (XII).
    Type: Grant
    Filed: May 6, 2013
    Date of Patent: May 28, 2019
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Hans-Christian Militzer, Johannes Eggert
  • Patent number: 10280160
    Abstract: The invention relates to a compound of Formula I and methods of treating CFTR (cystic fibrosis transmembrane conductance regulator) mediated diseases, in particular cystic fibrosis, comprising the step of administering a therapeutically effective amount of a compound of Formula I to a patient in need thereof:
    Type: Grant
    Filed: June 6, 2017
    Date of Patent: May 7, 2019
    Assignee: FLATLEY DISCOVERY LAB, LLC
    Inventor: Bridget M. Cole
  • Patent number: 10258621
    Abstract: Certain adjunctive therapies comprising a kynurenine-3-monooxygenase inhibitor and an antiviral agent for treating HIV-related disorders are provided herein. These disorders include AIDS dementia complex, AIDS-induced encephalopathy, HIV-associated neurocognitive disorder, asymptomatic neurocognitive impairment, minor neurocognitive disorder, minor cognitive motor disorder, vacuolar myelopathy, peripheral neuropathies, and polymyositis. Also provided are pharmaceutical compositions comprising a kynurenine-3-monooxygenase inhibitor and an antiviral agent.
    Type: Grant
    Filed: July 17, 2015
    Date of Patent: April 16, 2019
    Assignee: CHDI Foundation, Inc.
    Inventors: Celia Dominguez, Ignacio Muñoz-Sanjuán, Leticia Toledo-Sherman
  • Patent number: 10174038
    Abstract: Compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections are provided. The compounds and compositions are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.
    Type: Grant
    Filed: June 9, 2017
    Date of Patent: January 8, 2019
    Assignee: Gilead Sciences, Inc.
    Inventors: Hon Chung Hui, Jay P. Parrish, Michael Sangi, Dustin Siegel, David Sperandio, Hai Yang
  • Patent number: 10172952
    Abstract: The invention relates to inhibitory compounds of a p38 MAP kinase having a structure of type (I)-(VII) which can be used for the treatment or prophylaxis of adhesion. Pharmaceutical compositions are disclosed containing an effective amount of the substance SB203580 or one or more of the conjugated compounds of type (I)-(VII) or a combination thereof, and a pharmaceutically acceptable carrier, a diluent or an excipient. Also disclosed is the use of the substance SB203580 as an agent having anti-adhesion activity. Also disclosed is a method for the prophylaxis and/or treatment of a disease or a condition in which there is a possibility of the formation and/or growth of adhesions, which makes it possible to dispense with the additional administration of a preparation in the post-operative period.
    Type: Grant
    Filed: November 18, 2013
    Date of Patent: January 8, 2019
    Assignee: Joint Stock Company “Pharmasyntez”
    Inventors: Mikhail Gennadievich Shurygin, Irina Aleksandrovna Shurygina
  • Patent number: 10173995
    Abstract: The present invention is directed to novel pyridines, their derivatives, pharmaceutically acceptable salts, solvates and hydrates thereof. The present invention discloses compounds of Formulas I and II. The compounds and compositions of the present invention have protein kinases inhibitory activities and are expected to be useful for the treatment of protein kinases mediated diseases and conditions.
    Type: Grant
    Filed: January 11, 2014
    Date of Patent: January 8, 2019
    Assignee: Teligene Ltd.
    Inventor: Dawei Zhang
  • Patent number: 10174002
    Abstract: A compound having the structure of Formula II, or a stereoisomer, tautomer, or a pharmaceutically acceptable salt thereof that is useful as CFTR modulator. Further, a method of using the compound and pharmaceutical composition comprising the compound are provided for treating diseases in lungs, pancreas, gastrointestinal system, sinuses, reproductive system, and the sweat glands.
    Type: Grant
    Filed: October 6, 2016
    Date of Patent: January 8, 2019
    Assignee: NuBridge BioSciences
    Inventors: Lin Zhang, Yu Ge
  • Patent number: 10160744
    Abstract: The present invention relates to quinoline compounds of formula I wherein the variables are defined as in the claims and the description. The invention further relates to a pharmaceutical composition containing such compounds, to their use as modulators of the 5-HT6 receptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of the 5-HT6 receptor, and to methods for preventing or treating conditions and disorders which respond to the modulation of the 5-HT6 receptor.
    Type: Grant
    Filed: March 14, 2017
    Date of Patent: December 25, 2018
    Assignee: ABBVIE DEUTSCHLAND GMBH & CO. KG
    Inventors: Hervé Geneste, Andreas Haupt, Frauke Pohlki, Ana Lucia Relo, Liliane Unger, Karsten Wicke
  • Patent number: 10155777
    Abstract: A substituted trans-cycloheptene according to formula (I); wherein: a) Z and L are each selected from the group consisting of SiR1R2, CH2, CHOH, and CHR2; R1 is phenyl or CH3; R2 is phenyl, CH3, (CH2)nCN, or (CH2)nOH, wherein n is an integer from 1 to 5; Ra and Rb are each individually selected from the group consisting of H, OH, and CH3; and Z and L are not both SiR1R2; or b) Z is BocN, L is CH2, Ra is H, and Rb is H; or c) Z is C=0, L is CH2, Ra is H, and Rb is H.
    Type: Grant
    Filed: April 7, 2016
    Date of Patent: December 18, 2018
    Assignee: UNIVERSITY OF DELAWARE
    Inventors: Joseph Fox, Han Zhang, Yinzhi Fang
  • Patent number: 10125130
    Abstract: The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein A, L, D, R1-R15, w, x, y, and z are defined herein. The novel cycloalkyl-linked diheterocycle derivatives that are useful in the treatment of abnormal cell growth, such as cancer, in mammals. The present invention also relates to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in mammals.
    Type: Grant
    Filed: November 29, 2017
    Date of Patent: November 13, 2018
    Assignee: Pfizer Inc.
    Inventors: Aaron Craig Burns, Michael Raymond Collins, Samantha Elizabeth Greasley, Robert Louis Hoffman, Peter Qinhua Huang, Robert Steven Kania, Pei-Pei Kung, Maria Angelica Linton, Lakshmi Sourirajan Narasimhan, Paul Francis Richardson, Daniel Tyler Richter, Graham Smith
  • Patent number: 10071957
    Abstract: The invention provides novel compounds having the general formula (I) and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, ring D, R1, and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
    Type: Grant
    Filed: July 5, 2013
    Date of Patent: September 11, 2018
    Assignees: GENENTECH, INC., XENON PHARMACEUTICALS INC.
    Inventors: Christoph Martin Dehnhardt, Sultan Chowdhury, Thilo Focken, Michael Edward Grimwood, Ivan William Hemeon, Brian Safina, Daniel P. Sutherlin
  • Patent number: 10059667
    Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
    Type: Grant
    Filed: February 3, 2015
    Date of Patent: August 28, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Harry Chobanian, Duane DeMong, Yan Guo, Zhiyong Hu, Michael Miller, Barbara Pio, Christopher W. Plummer, Dong Xiao, Cangming Yang
  • Patent number: 10059687
    Abstract: The present disclosure relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyridine derivative compounds, and compositions (including pharmaceutical compositions) that include these compounds. The subject compounds and compositions are useful for inhibition of at least one histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer or neoplastic disease, such as prostate cancer, breast cancer, bladder cancer, lung cancer, melanoma, retinoblastoma, or multiple endocrine neoplasia type 1.
    Type: Grant
    Filed: December 27, 2016
    Date of Patent: August 28, 2018
    Assignee: Celgene Quanticel Research, Inc.
    Inventors: Young K. Chen, Michael Brennan Wallace
  • Patent number: 10052308
    Abstract: Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
    Type: Grant
    Filed: October 28, 2016
    Date of Patent: August 21, 2018
    Assignee: Aptinyx Inc.
    Inventors: John A. Lowe, III, M. Amin Khan
  • Patent number: 10017477
    Abstract: The present invention provides kinase inhibitors, such as compounds of Formula (I) and Formula (II). The compounds may covalently or non-covalently bind a kinase (e.g., Janus kinase 3 (JAK3)). Also provided are pharmaceutical compositions, kits, methods, and uses that involve the compounds for reducing the activity of a kinase and/or treating and/or preventing a condition associated with aberrant activity of a kinase (e.g., a proliferative disease, inflammatory disorder, autoimmune disorder, painful condition, and/or viral infection).
    Type: Grant
    Filed: April 23, 2015
    Date of Patent: July 10, 2018
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Nathanael S. Gray, Li Tan
  • Patent number: 9981945
    Abstract: A compound having the structure of Formula II, or a stereoisomer, tautomer, or a pharmaceutically acceptable salt thereof: The compound is useful as CFTR modulator. Further, a method of using the compound and pharmaceutical composition comprising the compound are provided for treating diseases in lungs, pancreas, gastrointestinal system, sinuses, reproductive system, and the sweat glands.
    Type: Grant
    Filed: October 6, 2016
    Date of Patent: May 29, 2018
    Assignee: NuBridge BioSciences
    Inventors: Lin Zhang, Yu Ge
  • Patent number: 9938257
    Abstract: The present invention provides novel heteroaryl compounds, pharmaceutical acceptable salts and formulations thereof. They are useful in preventing, managing, treating or lessening the severity of a protein kinase-mediated disease. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of protein kinase-mediated disease.
    Type: Grant
    Filed: September 7, 2016
    Date of Patent: April 10, 2018
    Assignees: CALITOR SCIENCES, LLC, SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Ning Xi, Minxiong Li, Xiaobo Li, Wuhong Chen, Tao Zhang, Haiyang Hu, Weilong Dai, Yanjun Wu
  • Patent number: 9908875
    Abstract: The present application relates to compounds having the inhibitory activity to apoptosis signal-regulating kinase (ASK1), thus are thus useful in treating ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases, diabetes, diabetic nephropathy, cardio-renal diseases, including kidney disease, fibrotic diseases, respiratory diseases, COPD, idiopathic pulmonary fibrosis, acute lung injury, acute and chronic liver diseases, and neurodegenerative diseases.
    Type: Grant
    Filed: December 15, 2014
    Date of Patent: March 6, 2018
    Assignee: GILEAD SCIENCES, INC.
    Inventor: Gregory Notte
  • Patent number: 9895308
    Abstract: Provided are certain pharmaceutical formulations of omecamtiv mecarbil and methods for their preparation and use.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: February 20, 2018
    Assignee: AMGEN INC.
    Inventor: William Brett Caldwell
  • Patent number: 9896445
    Abstract: The present application provides novel heterocyclic compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful for inhibiting ERK1/2. By administering to a patient in need a therapeutically effective amount of one or more of the compounds of formula (I), wherein X, Y, Z, J, M, and R1 to R8 are defined herein, these compounds are effective in treating conditions associated with dysregulation of the RAS/RAF/MEK/ERK pathway. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer.
    Type: Grant
    Filed: June 15, 2016
    Date of Patent: February 20, 2018
    Assignee: Ansana BioSciences, LLC
    Inventors: Aranapakam M. Venkatesan, Scott K. Thompson, Roger A. Smith, Sanjeeva P. Reddy, Raghava Reddy Kethiri, Purushottam M. Dewang, Gurulingappa Hallur, Chandrika Mulakala, Ramesh Mullangi, Mohd Zainuddin
  • Patent number: 9879001
    Abstract: Compounds of formula (I) wherein X1, X2, W, R1 to R5, L and m have the meaning according to the claims, are glucosidase inhibitors, and can be employed, inter alia, for the treatment of Alzheimer's disease.
    Type: Grant
    Filed: March 10, 2014
    Date of Patent: January 30, 2018
    Assignee: Merck Patent GmbH
    Inventors: Henry Yu, Lesley Liu-Bujalski, Theresa L. Johnson
  • Patent number: 9868700
    Abstract: The present invention relates to carbamoyl hydrazine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the FPR receptor.
    Type: Grant
    Filed: March 13, 2017
    Date of Patent: January 16, 2018
    Assignee: Allergan, Inc.
    Inventors: Vidyasagar Vuligonda, Thong Vu, Veena Viswanath, John E. Donello, Richard L. Beard
  • Patent number: 9868723
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Grant
    Filed: July 29, 2016
    Date of Patent: January 16, 2018
    Assignee: Celgene CAR LLC
    Inventors: Kwangho Lee, Deqiang Niu, Matthew Frank Baevsky
  • Patent number: 9862688
    Abstract: The present invention provides Janus kinase inhibitors, such as compounds of Formula (I) and Formula (II) wherein RY1 and RY2 comprise a tagged hydrophobic moiety RH. The compounds may covalently or non-covalently bind a kinase (e.g., Janus kinase 3 (JAK3)). The hydrophobic moiety RH may signal to the intracellular protein homeostasis machinery to induce degradation of the targeted kinase. Also provided are pharmaceutical compositions, kits, methods, and uses that involve the compounds for reducing the activity of a kinase and/or treating and/or preventing a condition associated with aberrant activity of a kinase (e.g., a proliferative disease, inflammatory disorder, autoimmune disorder, painful condition, and/or viral infection).
    Type: Grant
    Filed: April 23, 2015
    Date of Patent: January 9, 2018
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Nathanael S. Gray, Li Tan
  • Patent number: 9809573
    Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, antagonists of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system.
    Type: Grant
    Filed: November 3, 2014
    Date of Patent: November 7, 2017
    Assignee: Bristol-Myers Squibb Company
    Inventors: Guanglin Luo, Ling Chen, Gene M. Dubowchik, Swanee E. Jacutin-Porte, Prasanna Sivaprakasam, John E. Macor
  • Patent number: 9771332
    Abstract: Myeloperoxidase inhibitor, pharmaceutical compositions containing the inhibitor and the use of the inhibitor to treat, for example, cardiovascular conditions.
    Type: Grant
    Filed: May 2, 2016
    Date of Patent: September 26, 2017
    Assignee: Pfizer Inc.
    Inventor: Roger Ruggeri
  • Patent number: 9751863
    Abstract: Provided are compounds useful for treating cancer and methods of making the compounds and intermediates described herein.
    Type: Grant
    Filed: August 4, 2016
    Date of Patent: September 5, 2017
    Assignee: Agios Pharmaceuticals, Inc.
    Inventor: Shijie Zhang
  • Patent number: 9738625
    Abstract: Provided are isocitrate dehydrogenase 2 (IDH2) inhibitor compounds useful for treating cancer and methods of treating cancer, comprising administering to a subject in need thereof a compound described herein. Also provided are polymorphic forms of the IDH2 inhibitor compounds characterized by X Ray powder diffraction patterns, having improved physicochemical properties that influence in vivo dissolution rate for formulation purposes.
    Type: Grant
    Filed: August 1, 2014
    Date of Patent: August 22, 2017
    Assignee: Agios Pharmaceuticals, Inc.
    Inventors: Samuel V. Agresta, Chong-Hui Gu, David Schenkein, Hua Yang, Liting Guo, Zhen Tang, Jianming Wang, Yanfeng Zhang, Yan Zhou
  • Patent number: 9732087
    Abstract: Diamino-pyridine, pyrimidine and pyridazine compounds which may be used as H4 receptor modulators, and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.
    Type: Grant
    Filed: August 14, 2014
    Date of Patent: August 15, 2017
    Assignee: JANSSEN PHARMACEUTICA N.V.
    Inventors: Hui Cai, Frank Chavez, Paul J. Dunford, Andrew J. Greenspan, Steven P. Meduna, Jorge A. Quiroz, Brad M. Savall, Kevin L. Tays, Robin L. Thurmond, Jianmei Wei, Ronald L. Wolin, Xiaohu Zhang
  • Patent number: 9701659
    Abstract: Insecticidally active amide derivatives with sulfur-substituted phenyl- and pyridine groups of formula (I), wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.
    Type: Grant
    Filed: May 18, 2015
    Date of Patent: July 11, 2017
    Assignee: Syngenta Participations AG
    Inventors: Andrew Edmunds, Roger Graham Hall, Michel Muehlebach, Daniel Emery, Pierre Joseph Marcel Jung, Andre Stoller
  • Patent number: 9695169
    Abstract: Provided herein are intermediates and processes useful for facile synthesis of biologically active molecules.
    Type: Grant
    Filed: August 28, 2015
    Date of Patent: July 4, 2017
    Assignee: Plexxikon Inc.
    Inventor: Prabha N. Ibrahim
  • Patent number: 9687485
    Abstract: The invention relates to methods of treating cancer, myeloproliferative diseases, or immunological or neurological diseases with a combination of a glutaminase inhibitor and an anticancer agent such as an enzyme inhibitor (such as a kinase inhibitor), a mitotic inhibitor, a DNA-modifying agent, or a cytidine analog. The invention further relates to methods of treating cancer, myeloproliferative diseases, or immunological or neurological diseases that are resistant to one or more anticancer agents.
    Type: Grant
    Filed: June 12, 2015
    Date of Patent: June 27, 2017
    Assignee: Calithera Biosciences, Inc.
    Inventors: Susanne M. Steggerda, Andrew L. MacKinnon, Mirna L. Rodriguez, Dong Zhang, Francesco Parlati
  • Patent number: 9688930
    Abstract: A method for marking a petroleum hydrocarbon or a liquid biologically derived fuel by adding to the petroleum hydrocarbon or liquid biologically derived fuel at least one compound having formula Ar(R2)m(OR1)n, wherein Ar is an aromatic ring system having from six to twenty carbon atoms, R1 is C1-C12 alkyl or C2-C12 alkenyl, R2 is C1-C12 alkyl or C3-C12 alkenyl, m is an integer from zero to five and n is an integer from one to three; wherein each compound of formula Ar(R2)m(OR1)n is present at a level from 0.01 ppm to 100 ppm.
    Type: Grant
    Filed: November 5, 2013
    Date of Patent: June 27, 2017
    Assignee: Dow Global Technologies LLC
    Inventors: George David Green, Raymond J. Swedo, Ronda L. Gras, Jim C. Luong
  • Patent number: 9663454
    Abstract: The present invention relates to a process for labeling compounds comprising thiol moieties with 3-arylpropiolonitrile compounds, to 3-arylpropiolonitrile compounds substituted with tag moieties and to specific 3-arylpropiolonitrile linkers.
    Type: Grant
    Filed: July 4, 2014
    Date of Patent: May 30, 2017
    Assignees: Universite De Strasbourg, Centre National De La Recherche Scientifique
    Inventors: Alain Wagner, Oleksandr Koniev
  • Patent number: 9663457
    Abstract: The present invention relates to carbamoyl hydrazine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the FPR receptor.
    Type: Grant
    Filed: April 6, 2015
    Date of Patent: May 30, 2017
    Assignee: Allergan, Inc.
    Inventors: Richard L. Beard, Vidyasagar Vuligonda, Thong Vu, Veena Viswanath, John E. Donello
  • Patent number: 9663504
    Abstract: The present disclosure relates to salts of heterocyclic compounds and methods that inhibit HIF pathway activity. The compounds are designed to treat or prevent cancer and other hypoxia-mediated diseases.
    Type: Grant
    Filed: February 25, 2015
    Date of Patent: May 30, 2017
    Assignee: Board of Regents, The University of Texas System
    Inventors: Philip Jones, Maria Emilia Di Francesco, Timothy McAfoos
  • Patent number: 9624199
    Abstract: The invention relates to novel substituted bipiperidinyl derivatives, 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 18, 2017
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventors: Eva Maria Becker-Pelster, Philipp Buchgraber, Anja Buchmüller, Karen Engel, Andreas Göller, Herbert Himmel, Raimund Kast, Joerg Keldenich, Carsten Schmeck, Hanna Tinel, Frank Wunder
  • Patent number: 9604967
    Abstract: The invention provides certain azetidinyloxyphenylpyrrolidine compounds, particularly compounds of formula I wherein R is hydrogen or methyl, and pharmaceutical compositions thereof. The invention further provides methods of using a compound of formula I to treat overactive bladder.
    Type: Grant
    Filed: January 15, 2016
    Date of Patent: March 28, 2017
    Assignee: Eli Lilly and Company
    Inventors: Danwen Huang, Joshua O. Odingo
  • Patent number: 9604946
    Abstract: The present invention relates to compounds and methods for the treatment of bacterial infections. The compounds and methods involve the disruption of the QseC signaling pathway which modulates the virulence of some bacteria. This methodology for treatment of bacterial infections reduces evolutionary pressure to develop resistance because the bacteria are not killed in the process.
    Type: Grant
    Filed: March 10, 2014
    Date of Patent: March 28, 2017
    Assignee: The Board of Regents of the University of Texas System
    Inventors: Vanessa Sperandio, John R. Falck
  • Patent number: 9585882
    Abstract: In one aspect, the invention relates to compounds having the formula I: where R1, R2a, R2b, and R3-R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
    Type: Grant
    Filed: January 29, 2015
    Date of Patent: March 7, 2017
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Melissa Fleury, Anne-Marie Beausoliel, Adam D. Hughes, Daniel D. Long, Donna A. A. Wilton
  • Patent number: 9579304
    Abstract: Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
    Type: Grant
    Filed: February 22, 2016
    Date of Patent: February 28, 2017
    Assignee: Aptinyx, Inc.
    Inventors: John A. Lowe, III, M. Amin Khan
  • Patent number: 9546139
    Abstract: Provided are a novel pyridine carboxylic acid based compound used as a P2X1 and P2X3 receptor antagonist, a production method for the same and a composition comprising the same. The compound according to the present invention is a powerful antagonist of P2X1 and P2X3 receptors, and hence can be used as a drug for treating or preventing diseases involving neurological pain or chronic inflammatory diseases which are diseases caused by P2X1 and P2X3 receptor activity.
    Type: Grant
    Filed: December 20, 2010
    Date of Patent: January 17, 2017
    Assignee: GWANGJU INSTITUTE OF SCIENCE AND TECHNOLOGY
    Inventors: Yong-Chul Kim, Kwan-Young Jung, Joong Heui Cho
  • Patent number: 9512134
    Abstract: Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
    Type: Grant
    Filed: January 29, 2014
    Date of Patent: December 6, 2016
    Assignee: Aptinyx, Inc.
    Inventors: John A. Lowe, III, M. Amin Khan
  • Patent number: 9512141
    Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) is a CB2 receptor agonist for use in the treatment of several disorders, such as pain, atherosclerosis and glaucoma.
    Type: Grant
    Filed: December 4, 2013
    Date of Patent: December 6, 2016
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Baledi Dhurwasulu, Uwe Grether, Matthias Nettekoven, Stephan Roever, Mark Rogers-Evans, Tanja Schulz-Gasch
  • Patent number: 9511058
    Abstract: Disclosed are uses of carboxamide, sulfonamide and amine compounds for the treatment and amelioration of disorders and conditions related to oxidative stress, mitochondrial dysfunction, free radical damage and metabolic inefficiency, among others. Also described are methods for increasing exercise endurance, exercise efficiency and aerobic workload using the compounds described herein.
    Type: Grant
    Filed: July 7, 2014
    Date of Patent: December 6, 2016
    Assignee: Rigel Pharmaceuticals Inc.
    Inventors: Donald Payan, Yasumichi Hitoshi, Todd Kinsella
  • Patent number: 9504670
    Abstract: Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
    Type: Grant
    Filed: November 4, 2015
    Date of Patent: November 29, 2016
    Assignee: Aptinyx, Inc.
    Inventors: John A. Lowe, III, M. Amin Khan
  • Patent number: 9499539
    Abstract: The invention relates generally to the creation and use of cyclic sulfonamide containing derivatives to inhibit the hedgehog signaling pathway and to the use of those compounds for the treatment of hyperproliferative diseases and angiogenesis mediated diseases.
    Type: Grant
    Filed: November 4, 2013
    Date of Patent: November 22, 2016
    Assignee: NantBioScience, Inc.
    Inventors: Chunlin Tao, Chengzhi Yu, Forrest Arp, Paul Weingarten, Patrick Soon-Shiong
  • Patent number: 9487491
    Abstract: Provided is a compound useful as an inhibitor against the kinase activity of EML4-ALK fusion protein. As a result of intensive and extensive studies on compounds having inhibitory activity against the kinase activity of EML4-ALK fusion protein, the present inventors found that the diamino heterocyclic carboxamide compounds of the present invention had inhibitory activity against the kinase activity of EML4-ALK fusion protein. By this finding, the present invention was completed. The compounds of the present invention can be used as a pharmaceutical composition for preventing and/or treating cancer, such as lung cancer, non-small cell lung cancer, and small cell lung cancer.
    Type: Grant
    Filed: August 29, 2014
    Date of Patent: November 8, 2016
    Assignees: ASTELLAS PHARMA INC., KOTOBUKI PHARMACEUTICAL CO., LTD.
    Inventors: Itsuro Shimada, Kazuo Kurosawa, Takahiro Matsuya, Kazuhiko Iikubo, Yutaka Kondoh, Akio Kamikawa, Hiroshi Tomiyama, Yoshinori Iwai