The Additional Hetero Ring Is A Diazine Patents (Class 514/252.02)
  • Patent number: 11560390
    Abstract: Provided herein are compounds that inhibit the phosphorylation of MAPK and thus are useful in compositions and methods for treating cancer and inflammatory disease.
    Type: Grant
    Filed: September 16, 2020
    Date of Patent: January 24, 2023
    Assignee: SHY Therapeutics LLC
    Inventors: Yaron R. Hadari, Luca Carta, Michael Schmertzler, Theresa M. Williams, Charles H. Reynolds
  • Patent number: 11485740
    Abstract: The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts therefore, wherein R1 to R6, A, U, V, W, X, Y, and Z are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: February 13, 2019
    Date of Patent: November 1, 2022
    Assignees: Boehringer Ingelheim International GmbH, Hydra Biosciences, LLC
    Inventors: Steven Brunette, Jianwen Cui, Michael D. Lowe, Christopher Ronald Sarko, Simon Surprenant, Michael Robert Turner, Xinyuan Wu, Lana Louise Smith Keenan, Thierry Bouyssou, Paul Nicklin
  • Patent number: 11369603
    Abstract: The invention relates to the use of a H3R inverse agonist for the treatment of shift work disorder.
    Type: Grant
    Filed: April 17, 2018
    Date of Patent: June 28, 2022
    Assignee: NOVARTIS AG
    Inventors: Donald Johns, Klaus Kucher, Judit Sovago
  • Patent number: 11185590
    Abstract: A preserved liquid aqueous pharmaceutical composition includes one or more etherified cyclodextrin derivatives, at least one water-soluble preservative, and at least one pharmaceutically active compound which is poorly water-soluble, very poorly water-soluble or water-insoluble. The liquid aqueous pharmaceutical composition provides an acceptable solubility of the pharmaceutically active compound, such as pimobendan, in aqueous solution whereby the water-soluble preservatives retain their effectiveness in the presence of the etherified cyclodextrin derivatives allowing the use in an oral administration form.
    Type: Grant
    Filed: July 27, 2018
    Date of Patent: November 30, 2021
    Assignee: BOEHRINGER INGELHEIM VETMEDICA GMBH
    Inventors: Michael Aven, Tim Lukas
  • Patent number: 11180502
    Abstract: The invention provides azaspiro[4.5]decane derivatives of Formula (A): and pharmaceutically acceptable salts, solvates, hydrates, N-oxides, and diastereomers thereof, wherein A1, X, A2, Rr, R2?, W1, W2, R3?, R4?, a, and b are defined in the disclosure. The invention also provides compounds of Formulae I, and B-G, and pharmaceutically acceptable salts, solvates, hydrates, N-oxides, and diastereomers thereof. Further, the invention provides use of the compounds of Formulae A-G and I, and the pharmaceutically acceptable salts, solvates, hydrates, N-oxides, and diastereomers thereof, to treat pain. In certain embodiments, Compounds of the Disclosure are useful for treating a disorder responsive to blockade of one or more sodium channels.
    Type: Grant
    Filed: January 12, 2018
    Date of Patent: November 23, 2021
    Assignee: Purdue Pharma L.P.
    Inventors: Mark A. Youngman, Laykea Tafesse, Jae Hyun Park
  • Patent number: 11091464
    Abstract: Substituted pyridazinone compounds, conjugates, and pharmaceutical compositions for use in the treatment of neuromuscular diseases, such as Duchenne Muscular Dystrophy (DMD), are disclosed herein. The disclosed compounds are useful, among other things, in the treating of DMD and modulating inflammatory inhibitors IL-1, IL-6 or TNF-?.
    Type: Grant
    Filed: November 3, 2020
    Date of Patent: August 17, 2021
    Assignee: Edgewise Therapeutics, Inc.
    Inventors: Kevin Hunt, Kevin Koch, Alan Russell, Stephen Schlachter, Paul Winship, Chris Steele
  • Patent number: 11066396
    Abstract: The present invention is directed to substituted 5-trifluoromethyl oxadiazole compounds of generic formula (I) or a pharmaceutically acceptable salt thereof. In particular, the invention is directed to a class of aryl and heteroaryl substituted 5-trifluoromethyl oxadiazole compounds of formula I which may be useful as HDAC6 inhibitors for treating cellular proliferative diseases, including cancer, neurodegenerative diseases, such as schizophrenia and stroke, as well as other diseases.
    Type: Grant
    Filed: June 19, 2017
    Date of Patent: July 20, 2021
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Abbas Walji, Richard Berger, Craig A. Stump, Kelly-Ann S. Schlegel, James J. Mulhearn, Thomas J. Greshock, Deping Wang, Mark E. Fraley, Kristen G. Jones
  • Patent number: 11045443
    Abstract: Disclosed herein are methods of treating a tumor or cancer in a subject whose tumor or cancer cells express low levels of asparagine synthetase (ASNS), and compounds and compositions useful in such treatment. Also disclosed herein are methods of evaluating whether to administer a compound that inhibits glutathione production or a glutaminase inhibitor to a subject with a tumor or cancer.
    Type: Grant
    Filed: June 3, 2020
    Date of Patent: June 29, 2021
    Assignee: Board of Regents, The University of Texas System
    Inventors: Timothy Heffernan, Jeffrey Kovacs, Nakia Spencer, Christopher Bristow
  • Patent number: 11020397
    Abstract: Bifunctional barbiturate-derivative compounds that increase uric acid excretion and reduce uric acid production, and monofunctional barbiturate-derivative compounds that either increase uric acid excretion or reduce uric acid production are provided. Methods of using these compounds for reducing uric acid levels in blood or serum, for treating disorders associated with excess uric acid, and for maintaining normal uric acid levels in blood or serum, or the whole body, are also provided. Pharmaceutical compositions comprising the bifunctional and monofunctional compounds are also provided.
    Type: Grant
    Filed: May 12, 2020
    Date of Patent: June 1, 2021
    Assignee: Acquist LLC
    Inventors: Raymond P. Warrell, Jr., John J. Piwinski, Alexandre Larivée, Arshad Siddiqui, Karen Thai
  • Patent number: 10973810
    Abstract: The present disclosure provides compounds and methods useful in the treatment of neurological disorders. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological disorders.
    Type: Grant
    Filed: January 5, 2018
    Date of Patent: April 13, 2021
    Assignee: Yumanity Therapeutics, Inc.
    Inventors: Benjamin Vincent, Daniel Tardiff, Jeff Piotrowski, Eric Solis, Robert Scannevin, Chee-Yeun Chung, Rebecca Aron, Bertrand Le Bourdonnec, Matthew Lucas, Kenneth Rhodes
  • Patent number: 10935526
    Abstract: A minimum peak is determined from analysis results, a correction wavelength at which an S/N ratio of the minimum peak is greatest is determined, and the determined correction wavelength is used to execute correction of the minimum peak. A plurality of detector output value correction method are registered in a processor, correction method is selected from default correction method or from among a plurality of preset correction methods according to an object to perform correction.
    Type: Grant
    Filed: December 16, 2019
    Date of Patent: March 2, 2021
    Assignee: HITACHI HIGH-TECH SCIENCE CORPORATION
    Inventors: Shuhei Yamamura, Daisuke Akieda, Ayumi Nakaogami, Katsutoshi Shimizu
  • Patent number: 10899744
    Abstract: Provided are a compound as represented by structural formula (I) ({5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-6-aminopyridazin-3-yl}-N-{4-[((3S,5R)-3,5-di methylpiperazinyl)carbonyl]phenyl}carboxamide hydrochloride) and a novel crystalline form of a hydrate or solvate of the compound. Further provided are a manufacturing method of the compound and crystalline form, a related intermediate, a pharmaceutical composition comprising the compound, an application using the compound or the crystalline form for preparing a pharmaceutical product for treating a disease, symptom, or disorder, and a therapeutic method for treating a disease, symptom, or disorder.
    Type: Grant
    Filed: June 1, 2017
    Date of Patent: January 26, 2021
    Assignee: XCOVERY HOLDINGS, INC.
    Inventors: Congxin Liang, Yongbin Ma, Wei He
  • Patent number: 10722487
    Abstract: Disclosed herein are methods of treating a tumor or cancer in a subject whose tumor or cancer cells express low levels of asparagine synthetase (ASNS), and compounds and compositions useful in such treatment. Also disclosed herein are methods of evaluating whether to administer a compound that inhibits glutathione production or a glutaminase inhibitor to a subject with a tumor or cancer.
    Type: Grant
    Filed: October 18, 2018
    Date of Patent: July 28, 2020
    Assignee: Board of Regents, The University of Texas System
    Inventors: Timothy Heffernan, Jeffrey Kovacs, Nakia Spencer, Christopher Bristow
  • Patent number: 10703752
    Abstract: The present invention relates to novel integrin antagonists of Formula I and their use as a medicament, in particular for inhibiting neovascularization.
    Type: Grant
    Filed: August 19, 2019
    Date of Patent: July 7, 2020
    Assignee: OXURION NV
    Inventors: Ove Pedersen, Elke Vermassen
  • Patent number: 10676538
    Abstract: Compounds inhibitory to Staphylococcus pseudintermedius Sortase A (SrtA) are identified. The compounds inhibit cell wall-associated protein anchoring to the bacterial cell wall, thus potentially reducing bacterial virulence.
    Type: Grant
    Filed: August 28, 2018
    Date of Patent: June 9, 2020
    Inventors: Stephen Anthony Kania, David Allen Bemis, Jerome Baudry, Manasi Balachandran
  • Patent number: 10624948
    Abstract: The present invention refers to the use of protein kinase inhibitors and more specifically to the use of inhibitors of the protein kinase c-Jun amino terminal kinase, JNK inhibitor sequences, chimeric peptides, or of nucleic acids encoding same as well as pharmaceutical compositions containing same, for the treatment of various diseases or disorders strongly related to JNK signaling.
    Type: Grant
    Filed: June 26, 2014
    Date of Patent: April 21, 2020
    Assignee: XIGEN INFLAMMATION LTD.
    Inventors: Jean-Marc Combette, Catherine Deloche
  • Patent number: 10414727
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.
    Type: Grant
    Filed: November 8, 2017
    Date of Patent: September 17, 2019
    Assignee: Navitor Pharmaceuticals, Inc.
    Inventors: David John O'Neill, Eddine Saiah, Seong Woo Anthony Kang, Andrew Brearley, Jonathan Bentley
  • Patent number: 10335416
    Abstract: The disclosure provides a method for treating NPM1-mutated acute myeloid leukemia (AML) by administration of a composition comprising dactinomycin.
    Type: Grant
    Filed: September 13, 2016
    Date of Patent: July 2, 2019
    Inventors: Brunangelo Falini, Maria Paola Martelli
  • Patent number: 10287269
    Abstract: The present invention is directed to pyrimidine carboxamide compounds of formula I which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Grant
    Filed: March 21, 2016
    Date of Patent: May 14, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Dong-Ming Shen, Jonathan E. Wilson, Meng Yang, Dann Parker, Zack Zhiqiang Guo, Alejandro Crespo, Deping Wang, Troy McCracken
  • Patent number: 10188666
    Abstract: Dendrogenin A and antineoplastic agents for the treatment of chemosensitive or chemoresistant tumors. The invention concerns a kit-of-parts comprising 5?-hydroxy-6?-[2-(1H-imidazol-4-yl)ethylamino]cholestan-3?-ol (Dendrogenin A) or a pharmaceutically acceptable salt thereof and an antineoplastic agent for use in the treatment of cancer. Furthermore, the invention concerns Dendrogenin A or a pharmaceutically acceptable salt thereof for use for treating a chemoresistant cancer.
    Type: Grant
    Filed: September 3, 2014
    Date of Patent: January 29, 2019
    Assignees: AFFICHEM, INSERM (INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE), CENTRE HOSPITALIER UNIVERSITAIRE DE TOULOUSE
    Inventors: Philippe de Medina, Michael Paillasse, Christian Recher, Marc Poirot, Sandrine Silvente Poirot
  • Patent number: 10149840
    Abstract: To provide an OCT3 activity inhibitor having a different basic skeleton than that of conventional OCT3 activity inhibitors. This inhibitor of organic cation transporter 3 (OCT3) contains, as an active component, an imidazo[1,2-a]pyridine derivative, a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof.
    Type: Grant
    Filed: September 15, 2017
    Date of Patent: December 11, 2018
    Assignee: SHIN NIPPON BIOMEDICAL LABORATORIES, LTD.
    Inventors: Hidetoshi Yamashita, Nobuyuki Suzuki
  • Patent number: 10071162
    Abstract: The present invention is directed to a preserved liquid aqueous pharmaceutical composition comprising one or more etherified cyclodextrin derivatives; one or more water-soluble preservatives; preferably selected from the group consisting of sorbic acid or salts thereof, preferably sodium sorbate, potassium sorbate, calcium sorbate; benzoic acid or salts thereof, preferably sodium benzoate; benzalkonium chloride; benzethonium chloride; cetylpyridinium chloride; sodium metabisulfite; sodium acetate; parabenes and salts thereof, preferably methylparabene, ethylparabene, propylparabene, butylparabene, butylparabene sodium; or combinations thereof; and at least one pharmaceutically active compound which is poorly water-soluble, very poorly water-soluble or water-insoluble.
    Type: Grant
    Filed: July 18, 2014
    Date of Patent: September 11, 2018
    Assignee: BOEHRINGER INGELHEIM VETMEDICA GMBH
    Inventors: Michael Aven, Tim Lukas
  • Patent number: 9938265
    Abstract: A compound of Formula (I): or a pharmaceutically acceptable salt thereof, where: Q can be 5-methylpyridazin-3-yl,5-chloropyridazin-3-yl, 6-methylpyridazin-3-yl, or 6-fluoropyridazin-3-yl; R can be hydrogen, fluoro, or methoxy; R1 can be hydrogen, methoxy, difluoromethoxy, or trifluoromethoxy; and R2 can be methyl or ethyl. The compound of formula (I) can inhibit glutaminase, e.g., GLS1.
    Type: Grant
    Filed: November 29, 2016
    Date of Patent: April 10, 2018
    Assignees: AstraZeneca AB, Cancer Research Technology Limited
    Inventors: Johannes Wilhelmus Maria Nissink, Maurice Raymond Verschoyle Finlay, Mark David Charles, Matt Wood
  • Patent number: 9839636
    Abstract: Disclosed herein are analogues of itraconazole that are both angiogenesis and hedgehog signaling pathway inhibitors. The compounds are expected to be useful in the treatment of cancer, particularly cancers that are dependent upon the hedgehog signaling pathway such as basal cell carcinoma and medulloblastoma.
    Type: Grant
    Filed: April 7, 2017
    Date of Patent: December 12, 2017
    Assignee: UNIVERSITY OF CONNECTICUT
    Inventors: Matthew Kyle Hadden, Upasana Banerjee
  • Patent number: 9708290
    Abstract: Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
    Type: Grant
    Filed: January 12, 2016
    Date of Patent: July 18, 2017
    Assignees: Array BioPharma Inc., Genentech, Inc.
    Inventors: James F. Blake, Mark Joseph Chicarelli, Rustam Ferdinand Garrey, John Gaudino, Jonas Grina, David A. Moreno, Peter J. Mohr, Li Ren, Jacob Schwarz, Huifen Chen, Kirk Robarge, Aihe Zhou
  • Patent number: 9682083
    Abstract: The present invention relates to 6-amino-7-deaza-purine derivatives which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular RET family kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions containing these compounds.
    Type: Grant
    Filed: May 7, 2014
    Date of Patent: June 20, 2017
    Assignee: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Mauro Angiolini, Laura Buffa, Maria Menichincheri, Ilaria Motto, Paolo Polucci, Gabriella Traquandi, Fabio Zuccotto
  • Patent number: 9611262
    Abstract: The present invention is directed to compounds of Formula I: Methods of making the compounds of Formula I are also described. The invention also relates to pharmaceutical compositions comprising compounds of Formula I. Methods of using the compounds of the invention are also within the scope of the invention.
    Type: Grant
    Filed: September 11, 2015
    Date of Patent: April 4, 2017
    Assignee: Janssen Pharmaceutica NV
    Inventors: Brock T. Shireman, Terry P. Lebold, Curt A. Dvorak, Heather R. Coate, Jeannie M. Ziff, Cathy Preville, Christine Gelin, Gang Chen
  • Patent number: 9604962
    Abstract: Disclosed are compounds of Formulae 1, 1A, 1B and 1C including all geometric and stereoisomers, N-oxides, and salts thereof, wherein R1, R2, R4a1, R4a2, A, Aa, G, M, W, Z1, Z3, X, J, J1 and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: June 24, 2015
    Date of Patent: March 28, 2017
    Assignee: E I DU PONT DE NEMOURS AND COMPANY
    Inventors: Robert James Pasteris, Rafael Shapiro
  • Patent number: 9505752
    Abstract: Compounds of Formula I, including pharmaceutically acceptable salts thereof: formula (I): wherein A is selected from the group consisting of: formula (II) and wherein Z is selected from the group consisting of: formula (III): and. are useful as HIV attachment inhibitors.
    Type: Grant
    Filed: August 7, 2013
    Date of Patent: November 29, 2016
    Assignee: ViiV Healthcare UK (No. 5) Limited
    Inventors: Tao Wang, Zhongxing Zhang, John F. Kadow, Nicholas A. Meanwell, Edward H. Ruediger, Clint A. James, Daniel H. Deon, David J. Carini, Barry L. Johnson
  • Patent number: 9499567
    Abstract: The invention further relates to a DGAT inhibitor of formula including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —NRx—C(?O)—; —Z—C(?O)—; —Z—NRx—C(?O)—; —S(?O)p-; —C(?S)—; —NRx—C(?S)—; —Z—C(?S)—; —Z—NRx—C(?S)—; —O—C(?O)—; —C(?O)—C(?O)—; R1 represents a 5-membered monocyclic heterocycle containing at least 2 heteroatoms; a 6-membered aromatic monocyclic heterocycle; or a 5-membered heterocycle containing at least 2 heteroatoms fused with phenyl, cyclohexyl or a 5- or 6-membered heterocycle; wherein each of said heterocycles may optionally be substituted; R2 represents R3; R3 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or 6-
    Type: Grant
    Filed: July 20, 2015
    Date of Patent: November 22, 2016
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jean-Pierre Andre Marc Bongartz, Lieven Meerpoel, Gustaaf Maria Boeckx, Guy Rosalia Eugeen Van Lommen, Christophe Francis Robert Nestor Buyck, Daniel Obrecht, Philipp Ermert, Anatol Luther
  • Patent number: 9463199
    Abstract: The invention relates to the use of a phosphodiesterase type III (PDE III) inhibitor or Ca2+-sensitizing agent or a pharmaceutically acceptable derivative thereof for the preparation of a medication for the reduction of the heart size of a patient suffering from heart failure.
    Type: Grant
    Filed: March 23, 2005
    Date of Patent: October 11, 2016
    Assignee: Boehringer Ingelheim Vetmedica GmbH
    Inventors: Juergen Daemmgen, Olaf Joens, Rainer Kleemann
  • Patent number: 9434721
    Abstract: A compound of formula: wherein Ar1, A, R3, x, and m are as disclosed herein and Ar2 is a benzothiazolyl, benzooxazolyl, or benzoimidazolyl group or a pharmaceutically acceptable salt thereof (a “Benzoazolylpiperazine Compound”), compositions comprising a Benzoazolylpiperazine Compound, and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Benzoazolylpiperazine Compound are disclosed.
    Type: Grant
    Filed: December 6, 2013
    Date of Patent: September 6, 2016
    Assignee: Purdue Pharma L.P.
    Inventors: Qun Sun, Laykea Tafesse, Sam Victory
  • Patent number: 9422296
    Abstract: The present invention relates to 4-aryl-6-piperazin-1-yl-3-substituted-pyridazines that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.
    Type: Grant
    Filed: July 28, 2014
    Date of Patent: August 23, 2016
    Assignee: JANSSEN PHARMACEUTICA NV
    Inventors: Gregor James Macdonald, Xavier Jean Michel Langlois, José Manuel Bartolomé-Nebreda, Michiel Luc Maria Van Gool
  • Patent number: 9409871
    Abstract: The present invention relates to compounds of formula I: in which L, W, X, Y, Z, m, p, R1, R2, R3, R4 and R7 are defined in the Summary of the Invention; capable of inhibiting the Hedgehog and Smo signaling pathway. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the diagnosis and treatment of pathologies relating to the Hedgehog and Smo signaling pathway, for example, tumor formation, cancer, neoplasia and non-malignant hyperproliferative disorders.
    Type: Grant
    Filed: May 30, 2013
    Date of Patent: August 9, 2016
    Assignee: NOVARTIS AG
    Inventors: Feng He, Stefan Peukert, Karen Marie Miller-Moslin, Naeem Yusuff, Zhuoliang Chen, Bharat Lagu
  • Patent number: 9353104
    Abstract: The present invention is directed to substituted pyridizinone compounds of formula I which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Grant
    Filed: March 10, 2014
    Date of Patent: May 31, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Casey C. McComas, Thomas S. Reger, Changhe Qi
  • Patent number: 9315381
    Abstract: To provide a catalyst for dehydrogenation of formic acid which allows hydrogen, heavy hydrogen gas or heavy-hydrogenated hydrogen containing no carbon monoxide to be produced through dehydrogenation of formic acid in a highly efficient manner. A catalyst for dehydrogenation of formic acid, including: a multinuclear metal complex represented by the following Formula (1), a tautomer or stereoisomer thereof, or a salt thereof, where M1 and M2 denote transition metals and may be the same as or different from each other; Q1 to Q6 each independently denote carbon or nitrogen; R1 to R6 each independently denote, for example, a hydrogen atom, an alkyl group, a phenyl group, a nitro group, a halogen group, a sulfonate group (sulfo group); L1 and L2 each independently denote an aromatic anionic ligand or an aromatic ligand, and may be substituted by one or more substituents; Y1 and Y2 each independently denote any ligand or are absent; and m denotes a positive integer, 0, or a negative integer.
    Type: Grant
    Filed: January 25, 2013
    Date of Patent: April 19, 2016
    Assignee: NATIONAL INSTITUTE OF ADVANCED INDUSTRIAL SCIENCE AND TECHNOLOGY
    Inventors: Yuichiro Himeda, Wan-Hui Wang
  • Patent number: 9289427
    Abstract: The present invention relates to 3-(1-{3-[5-(1-methyl-piperidin-4-ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile hydrochloride solvates and crystalline modifications thereof. The present invention further relates to processes of manufacturing these crystalline modifications as well as their use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by the inhibition, regulation and/or modulation of signal transduction of kinases, in particular by the inhibition of tyrosine kinases, e.g. pathophysiological conditions such as cancer.
    Type: Grant
    Filed: January 17, 2014
    Date of Patent: March 22, 2016
    Assignee: MERCK PATENT GMBH
    Inventors: Axel Becker, Clemens Kuehn, Christoph Saal, Oliver Schadt, Dieter Dorsch, Heinz-Hermann Bokel, Frank Stieber, Cristina Donini
  • Patent number: 9283208
    Abstract: Medicaments and methods for treating cancer are disclosed.
    Type: Grant
    Filed: May 17, 2012
    Date of Patent: March 15, 2016
    Assignee: NIIKI PHARMA INC.
    Inventor: Hooshmand Sheshbaradaran
  • Patent number: 9095846
    Abstract: The invention relates to a ligand that may be used to create a catalyst including a coordination complex is formed by the addition of two metals; Cp, Cp* or an unsubstituted or substituted ?-arene; and two coordinating solvent species or solvent molecules. The bimetallic catalyst may be used in the hydrogenation of CO2 to form formic acid and/or salts thereof, and in the dehydrogenation of formic acid and/or salts thereof to form H2 and CO2.
    Type: Grant
    Filed: September 12, 2012
    Date of Patent: August 4, 2015
    Assignees: Brookhaven Science Associates, LLC, National Institute of Advanced Industrial Science and Technology (AIST)
    Inventors: Jonathan F. Hull, Yuichiro Himeda, Etsuko Fujita, James T. Muckeman
  • Publication number: 20150148351
    Abstract: The present invention relates to 3-(1-{3-[5-(1-methyl-piperidin-4-ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile hydrochloride solvates and crystalline modifications thereof. The present invention further relates to processes of manufacturing these crystalline modifications as well as their use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by the inhibition, regulation and/or modulation of signal transduction of kinases, in particular by the inhibition of tyrosine kinases, e.g. pathophysiological conditions such as cancer.
    Type: Application
    Filed: January 29, 2015
    Publication date: May 28, 2015
    Applicant: MERCK PATENT GMBH
    Inventors: Axel BECKER, Clemens KUEHN, Christoph SAAL, Oliver SCHADT, Dieter DORSCH, Heinz-Hermann BOKEL, Frank STIEBER, Cristina DONINI
  • Patent number: 9040537
    Abstract: The present invention relates to pyridazine compounds of formulae I or II and the salts thereof, the N-oxides thereof and the salts of the N-oxides thereof, where the radical A is of the formula A, wherein # denotes the point of attachment to the remainder of formulae I or II, and wherein A1 is N or C—RA1, A2 is N or C—RA2, A3 is N or C—RA3, A4 is N or C—RA4 and A5 is N or C—RA5, provided that one or two of the variables A1, A2, A3, A4 or A5 is N; RA1, RA5, if present, are H, halogen, CN, NO2, C1-C6-alkyl, C1-C6-haloalkyl and the like; RA2, RA4, if present, are H, halogen, CN, NO2, C1-C10-alkyl, C1-C10-haloalkyl and the like; RA3, if present, is H, halogen, CN, NO2, C1-C10-alkyl, C1-C10-haloalkyl and the like; where W is N or C—RW and V is N or C—RV, provided that one of the variables W or V is N; Rt and Rw, if present, are H, halogen, methyl, C1-haloalkyl and the like; Ru and Rv, if present, are H, halogen, C1-C4-alkyl, C1-C3-haloalkyl and the like; X1 is S, O or NR1a, wherein R1a is H, C1-C10-alkyl
    Type: Grant
    Filed: March 23, 2011
    Date of Patent: May 26, 2015
    Assignee: BASF SE
    Inventors: Ronan Le Vezouet, Sebastian Soergel, Christian Defieber, Steffen Gross, Karsten Koerber, Wolfgang Von Deyn, Douglas D. Anspaugh, Deborah L. Culbertson
  • Patent number: 9040568
    Abstract: This invention discloses a method of treatment of osteoarthritis pain by administration of a composition containing a nicotinic acetylcholine receptor ligand and a nicotinic acetylcholine receptor subtype ?4?2 allosteric modulator. The present application also relates to compositions comprising such compounds for use in treating pain and related disorders mediated by controlling neurotransmitter release in a subject.
    Type: Grant
    Filed: May 26, 2010
    Date of Patent: May 26, 2015
    Assignee: AbbVie Inc.
    Inventors: Murali Gopalakrishnan, Chih-Hung Lee, Jianguo Ji, Tao Li, Kevin B. Sippy
  • Patent number: 9034873
    Abstract: The present disclosure describes compounds of the following formula in which: the groups A, which may be identical or different, represent a group n is an integer equal to 1 or 2, Y represents an oxygen or sulfur atom, a methylene, hydroxymethylene, carbonyl or thiocarbonyl group, or a group of formula the groups R, which may be identical or different, represent a hydrogen, an alkyl, alkylamine, hydroxyl-alkyl or alkyloxy chain containing from 1 to 6 carbons, or a —COOH, —CONH2, —COOR2 or —CONHR2 group in which R2 is an alkyl chain containing from 1 to 6 carbons, or, when the substituents R are identical in the 2-pyridinyl groups, the substituents R2 may together form an ethereal cyclic alkyl chain, with the exception of the compounds: 2,6-di[5-(2-pyridyl)pyrrol-2-yl]pyridine and bis[5-(6-methyl-2-pyridyl)pyrrol-2-yl]methane.
    Type: Grant
    Filed: July 26, 2007
    Date of Patent: May 19, 2015
    Assignee: Centre National de la Recherche Scientifique (C.N.R.S.)
    Inventors: Didier Max Dubreuil, Muriel Genevieve Pipelier, Jean-Paul Pradere, Hicham Bakkali, Patrice Lepape, Thierry Delaunay, Alexandra Tabatchnik
  • Patent number: 9034874
    Abstract: The invention relates to compound of the formula I or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it.
    Type: Grant
    Filed: July 17, 2013
    Date of Patent: May 19, 2015
    Assignee: NOVARTIS AG
    Inventors: Yves Auberson, Mark Gary Bock, Dario Braga, Marco Curzi, Stephanie Kay Dodd, Stefano Luca Giaffreda, Haiyang Jiang, Piotr Karpinski, Thomas J. Troxler, Tielin Wang, Xiaoyang Wang, Xuechun Zhang
  • Publication number: 20150133425
    Abstract: The present invention relates to substituted thienopyrimidine compounds of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: May 17, 2013
    Publication date: May 14, 2015
    Inventors: Georg Kettschau, Florian Puehler, Knut Eis, Ulrich Klar, Dirk Kosemund, Detlev Sülzle, Philip Lienau, Andrea Hägebarth, Ulf Bömer, Lars Wortmann, Keith Graham, Antje Margret Wengner
  • Publication number: 20150133452
    Abstract: Compounds selected from the group according to claim 1 are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumours.
    Type: Application
    Filed: January 22, 2015
    Publication date: May 14, 2015
    Applicant: MERCK PATENT GMBH
    Inventors: Oliver SCHADT, Dieter DORSCH, Frank STIEBER, Andree BLAUKAT
  • Publication number: 20150133429
    Abstract: Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.
    Type: Application
    Filed: January 14, 2015
    Publication date: May 14, 2015
    Inventors: Julia Haas, Steven W. Andrews, Yutong Jiang, Gan Zhang
  • Publication number: 20150126506
    Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
    Type: Application
    Filed: January 8, 2015
    Publication date: May 7, 2015
    Inventors: Alfredo C. CASTRO, Catherine A. EVANS, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Tao LIU, Daniel A. SNYDER, Martin R. TREMBLAY, Pingda REN, Yi LIU, Liansheng LI, Katrina CHAN
  • Patent number: 9018214
    Abstract: The invention relates to bicyclic heterocycle compounds of formula (I): or tautomeric or stereochemically isomeric forms, N-oxides, pharmaceutically acceptable salts or the solvates thereof; wherein R1, R2a, R2b, R3a, R3b, R5, R6, R7, R8, R9, p and E are as defined herein; to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Grant
    Filed: April 20, 2012
    Date of Patent: April 28, 2015
    Assignee: Astex Therapeutics Limited
    Inventors: Alison Jo-Anne Woolford, Steven Howard, Ildiko Maria Buck, Gianni Chessari, Christopher Norbert Johnson, Emiliano Tamanini, James Edward Harvey Day, Elisabetta Chiarparin, Thomas Daniel Heightman, Martyn Frederickson, Charlotte Mary Griffiths-Jones
  • Patent number: RE48622
    Abstract: A series of pyrazolo[3,4-d]pyrimidine derivatives that are substituted at the 4-position by a diaza monocyclic, bridged bicyclic or spirocyclic moiety, are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases and malaria; and organ and cell transplant rejection.
    Type: Grant
    Filed: July 22, 2019
    Date of Patent: July 6, 2021
    Assignees: UCB Biopharma SRL, Katholieke Universiteit Leuven, K.U. Leuven R&D
    Inventors: Daniel James Ford, Richard Jeremy Franklin, Anant Ramrao Ghawalkar, Helen Tracey Horsley, Qiuya Huang, James Thomas Reuberson, Bart Vanderhoydonck