Quinuclidines (including Unsaturated) Patents (Class 546/133)
  • Patent number: 10604518
    Abstract: The invention relates to a method of preparing inhibitors of glucosylceramide synthase (GCS) useful for the treatment metabolic diseases, such as lysosomal storage diseases, either alone or in combination with enzyme replacement therapy, and for the treatment of cancer.
    Type: Grant
    Filed: August 1, 2018
    Date of Patent: March 31, 2020
    Assignee: GENZYME CORPORATION
    Inventors: Craig S. Siegel, Rayomand Gimi, Michael Reardon, Jin Zhao
  • Patent number: 10214524
    Abstract: The invention relates to novel 2-heteroaryl carboxamides and to the use thereof for producing medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning and/or memory.
    Type: Grant
    Filed: June 8, 2015
    Date of Patent: February 26, 2019
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Joachim Luithle, Frank-Gerhard Böβ, Christina Erb, Frank-Thorsten Hafner, Katrin Schnizler, Timo Flessner, Marja Van Kampen, Franz-Josef Van Der Staay
  • Patent number: 10065949
    Abstract: The invention relates to a method of preparing inhibitors of glucosylceramide synthase (GCS) useful for the treatment metabolic diseases, such as lysosomal storage diseases, either alone or in combination with enzyme replacement therapy, and for the treatment of cancer.
    Type: Grant
    Filed: May 12, 2017
    Date of Patent: September 4, 2018
    Assignee: GENZYME CORPORATION
    Inventors: Craig S. Siegel, Rayomand Gimi, Michael Reardon, Jin Zhao
  • Patent number: 9682975
    Abstract: The invention relates to a method of preparing inhibitors of glucosylceramide synthase (GCS) useful for the treatment metabolic diseases, such as lysosomal storage diseases, either alone or in combination with enzyme replacement therapy, and for the treatment of cancer.
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: June 20, 2017
    Assignee: Genzyme Corporation
    Inventors: Craig S. Siegel, Rayomand Gimi, Michael Reardon, Jin Zhao
  • Patent number: 9657011
    Abstract: The present invention relates to a process for the preparation of umeclidinium bromide, and to processes for preparing intermediates used in the preparation of umeclidinium bromide.
    Type: Grant
    Filed: January 15, 2016
    Date of Patent: May 23, 2017
    Assignee: Glaxo Group Limited
    Inventors: Frank Hossner, John Bryce Strachan
  • Patent number: 9518049
    Abstract: The present invention relates to novel salt forms of (S)-Quinuclidin-3-yl (2-(2-(4-fluorophenyl)thiazol-4-yl)propan-2-yl)carbamate useful as an inhibitor of glucosylceramide synthase (GCS) and for the treatment metabolic diseases, such as lysosomal storage diseases, either alone or in combination with enzyme replacement therapy, and for the treatment of cancer.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: December 13, 2016
    Assignee: GENZYME CORPORATION
    Inventors: Craig S. Siegel, Jin Zhao
  • Patent number: 9144571
    Abstract: Methods of using Muscarinic Acetylcholine Receptor Antagonists are provided.
    Type: Grant
    Filed: May 8, 2015
    Date of Patent: September 29, 2015
    Assignee: Glaxo Group Limited
    Inventors: Dramane Ibrahim Laine, Michael R. Palovich, Brent W. McCleland, Christopher E. Neipp, Sonia M. Thomas
  • Patent number: 9073922
    Abstract: Disclosed are compounds of Formula (IIIa), wherein R1, R2, R3, X1, X2, X3, X4, X5, have any of the values defined therefore in the specification, and pharmaceutically acceptable salts thereof. The compounds may be used as agents in the treatment of diseases, including cancer. Also provided are pharmaceutical compositions comprising one or more compounds of Formula (IIIa).
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: July 7, 2015
    Assignee: AbbVie, Inc.
    Inventors: Jianchun Gong, Zhi-Fu Tao, Thomas D. Penning, Andrew J. Souers, Yunsong Tong, Guidong Zhu
  • Patent number: 9045469
    Abstract: Muscarinic Acetylcholine Receptor Antagonists and methods of using them are provided.
    Type: Grant
    Filed: September 4, 2014
    Date of Patent: June 2, 2015
    Assignee: Glaxo Group Limited
    Inventors: Dramane Ibrahim Laine, Michael R. Palovich, Brent W. McCleland, Christopher E. Neipp, Sonia M. Thomas
  • Patent number: 9000008
    Abstract: The invention relates to novel amides of acetic and propionic acids, methods for production and use thereof for the production of medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning ability and memory.
    Type: Grant
    Filed: August 16, 2013
    Date of Patent: April 7, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Joachim Luithle, Frank-Gerhard Bob, Christina Erb, Katrin Schnizler, Timo Flessner, Marja V. Kampen, Christoph Methfessel
  • Patent number: 8993556
    Abstract: The present invention relates to substituted resorcinol derivatives which inhibit the activity of Heat Shock Protein HSP90. The compounds of the invention are therefore useful in treating proliferative diseases such as cancer and neurodegenerative diseases. The present invention also provides processes for preparing these compounds, pharmaceutical compositions comprising them, methods of treating diseases and the pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: April 16, 2010
    Date of Patent: March 31, 2015
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Maria Gabriella Brasca, Elena Casale, Ron Ferguson, Paolo Polucci, Fabio Zuccotto
  • Publication number: 20150087626
    Abstract: There is described a novel group of cyclic amine derivative compounds, having an EP4 receptor antagonistic activity and specifically pharmaceutical compounds which are useful for the treatment or alleviation of Prostaglandin E mediated diseases. The present invention therefore relates to novel compounds which are selective antagonists of the EP4 subtype of PGE2 receptors with analgesic and antinflammatory activity, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments, inter alia for the treatment or alleviation of Prostaglandin E mediated diseases such as acute and chronic pain, osteoarthritis, inflammation-associated disorder as arthritis, rheumatoid arthritis, cancer, migraine and endometriosis.
    Type: Application
    Filed: July 4, 2011
    Publication date: March 26, 2015
    Inventors: Manuela Borriello, Sabrina Pucci, Luigi Piero Stasi, Lucio Rovati
  • Patent number: 8987299
    Abstract: Compounds of formula (I) described herein act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for the prevention and/or treatment of broncho-obstructive or inflammatory diseases.
    Type: Grant
    Filed: December 6, 2013
    Date of Patent: March 24, 2015
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Fabio Rancati, Ian Linney
  • Patent number: 8980913
    Abstract: Compounds of formula (I) defined herein act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for the prevention and/or treatment of broncho-obstructive or inflammatory diseases.
    Type: Grant
    Filed: December 6, 2013
    Date of Patent: March 17, 2015
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Fabio Rancati, Ian Linney, Chris Knight, Wolfgang Schmidt
  • Publication number: 20150065537
    Abstract: The invention relates to novel benzothiophene-, benzofuran-, and indole ureas and to the use thereof for producing medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning, and/or memory.
    Type: Application
    Filed: June 9, 2014
    Publication date: March 5, 2015
    Inventors: Timo Flessner, Frank-Gerhard Boss, Christina Erb, Frank-Thorsten Hafner, Katrin Schnizler, Dieter Lang, Joachim Luithle, Marja Van Kampen, Franz-Josef Van Der Staay
  • Publication number: 20150057272
    Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
    Type: Application
    Filed: August 1, 2014
    Publication date: February 26, 2015
    Inventors: Chi B. Vu, Jeremy S. Disch, Pui Yee Ng, Charles A. Blum, Robert B. Perni
  • Patent number: 8952165
    Abstract: A pyridone derivative compound and a pharmaceutically acceptable salt, isomer, solvate or hydrate thereof, and a preventive or therapeutic pharmaceutical composition for cognitive disorders that includes the pyridone derivative compound or a pharmaceutically acceptable salt, isomer, solvate or hydrate thereof.
    Type: Grant
    Filed: January 30, 2012
    Date of Patent: February 10, 2015
    Assignee: SK Biopharmaceuticals Co., Ltd.
    Inventors: Cheol Young Maeng, Young Koo Jang, Su Bong Cha, Hye Won Shin, Chan Mi Joung, Eun Jung Yi
  • Publication number: 20150031891
    Abstract: The invention is directed to novel bis-quarternary cinchona alkaloid salts and the use of bis-quarternary cinchona alkaloid salts in asymmetric phase transfer catalysis. The present invention is directed to novel bis-quarternary cinchona alkaloid salts and the use of bis-quarternary cinchona alkaloid salts in asymmetric phase transfer catalysis. On certain substrates and under specific reaction conditions, the inventors have discovered that the use of bis-quarternary cinchona alkaloid salts in asymmetric phase transfer catalysis surprisingly provides for a more active and efficient process as compared to mono-quarternary catalysts.
    Type: Application
    Filed: March 13, 2013
    Publication date: January 29, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Bangping Xiang, Nobuyoshi Yasuda
  • Publication number: 20150031681
    Abstract: A medicament for treating diseases associated with cholinergic properties in the central nervous system (CNS) and/or peripheral nervous system (PNS), diseases associated with smooth muscle contraction, endocrine disorders, neurodegenerative disorders and the like, which comprises a compound of Formula (I): wherein A is CR1E or a nitrogen atom, X—Y—Z is N—CO—NR3AR3B and the like, R1A to R1E are each independently a hydrogen atom and the like, R2A to R2D are each independently a hydrogen atom and the like, R3A and R3B are each independently an optionally-substituted C3-10 cycloalkyl and the like, and n is 1 or 2 or a pharmaceutically acceptable salt thereof, which exhibits potent modulatory-effects on the activity of ?7 nicotinic acetylcholine receptor (?7 nAChR).
    Type: Application
    Filed: April 9, 2013
    Publication date: January 29, 2015
    Inventors: Shinya Usui, Hiroki Yamaguchi, Yoko Nakai
  • Publication number: 20150025222
    Abstract: The invention discloses new substituted anthraquinone dyes that may be useful as cellular stains. In some aspect of the invention, the nuclear stains are useful for staining the nuclei of dead or fixed cells. Another aspect of the invention relates to substituted anthraquinone dyes comprising an enzyme substrate moiety that is transformable or cleavable by an enzyme such that the transformation or cleavage of the substrate moiety causes a detectable change in the functionality or spectral properties of the dye.
    Type: Application
    Filed: April 9, 2014
    Publication date: January 22, 2015
    Applicant: Biotium, Inc.
    Inventors: Fei MAO, Wai-Yee LEUNG, Ching-Ying CHEUNG, Lori Michelle ROBERTS
  • Patent number: 8921544
    Abstract: The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2 are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.
    Type: Grant
    Filed: June 3, 2014
    Date of Patent: December 30, 2014
    Assignee: Sareum Limited
    Inventors: John Charles Reader, John Mark Ellard, Helen Boffey, Susanne Taylor, Andrew David Carr, Michael Cherry, Michelle Wilson, Richard Boakye Owoare
  • Publication number: 20140378668
    Abstract: A new and versatile class of cyclic diazodicarboxamides that reacts efficiently and selectively with phenols and the phenolic side chain of tyrosine through an Ene-like reaction is reported. This mild aqueous tyrosine ligation reaction works over a broad pH range and expands the repertoire of aqueous chemistries available for small molecule, peptide, and protein modification. The tyrosine ligation reactions are shown to be compatible with the labeling of native enzymes and antibodies in buffered aqueous solution. This reaction provides a novel synthetic approach to bispecific antibodies. This reaction will find broad utility in peptide and protein chemistry and in the chemistry of phenol-containing compounds.
    Type: Application
    Filed: June 25, 2014
    Publication date: December 25, 2014
    Inventors: Carlos F. Barbas, III, Hitoshi Ban, Julia Gavrilyuk
  • Publication number: 20140336378
    Abstract: Disclosed are a novel benzamide derivative and pharmaceutical use thereof, and more particularly, a novel benzamide derivative having a structure of Formula 1 or pharmaceutically acceptable salts thereof, and a composition for prevention or treatment of pain or itching including the above material. The novel benzamide derivative and pharmaceutically acceptable salt thereof according to the present invention exhibit excellent pain-suppressive effect and, in particular, pain-suppressive effect in not only a neuropathic animal model but also other models such as a formalin model, and therefore, may be used in suppression of different pains such as nociceptive pain, chronic pain, etc.
    Type: Application
    Filed: November 29, 2012
    Publication date: November 13, 2014
    Inventor: Doo Hyun Lee
  • Patent number: 8884017
    Abstract: The invention relates to novel 2-heteroarylcarboxamides, processes for their preparation, and their use for producing medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning and/or memory.
    Type: Grant
    Filed: November 4, 2011
    Date of Patent: November 11, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Martin Hendrix, Frank-Gerhard Böβ, Christina Erb, Timo Fleβner, Marja van Kampen, Joachim Luithle, Christoph Methfessel, Welf-Burkhard Wiese
  • Patent number: 8877774
    Abstract: Compounds of formula(I) act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for the prevention and/or treatment of broncho-obstructive and inflammatory diseases.
    Type: Grant
    Filed: June 8, 2012
    Date of Patent: November 4, 2014
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Fabio Rancati, Andrea Rizzi, Gabriele Amari, Matteo Biagetti, Ian Linney
  • Patent number: 8859535
    Abstract: The invention relates to compounds of formula (I): as defined in the application. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof.
    Type: Grant
    Filed: June 19, 2012
    Date of Patent: October 14, 2014
    Assignee: Novartis AG
    Inventors: Nicole Buschmann, Pascal Furet, Philipp Holzer, Joerg Kallen, Keiichi Masuya, Stefan Stutz
  • Publication number: 20140303231
    Abstract: The invention features therapeutic compositions comprising agents useful for the treatment or prevention of pruritis, and methods useful for identifying such agents.
    Type: Application
    Filed: January 24, 2014
    Publication date: October 9, 2014
    Applicant: The Johns Hopkins University
    Inventors: Xinzhong Dong, Qin Liu, David J. Anderson
  • Patent number: 8853404
    Abstract: Muscarinic Acetylcholine Receptor Antagonists and methods of using them are provided.
    Type: Grant
    Filed: October 14, 2013
    Date of Patent: October 7, 2014
    Assignee: Glaxo Group Limited
    Inventors: Dramane Ibrahim Laine, Michael R. Palovich, Brent W. McCleland, Christopher E. Neipp, Sonia M. Thomas
  • Patent number: 8846655
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, R2, R3, Ra, and Y are defined herein.
    Type: Grant
    Filed: October 28, 2010
    Date of Patent: September 30, 2014
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Steven J. Coats, Haiyan Bian, Chaozhong Cai, Bart L. DeCorte, Li Liu, Mark J. Macielag, Scott L. Dax, Philip M. Pitis, Peter J. Connolly, Wei He
  • Patent number: 8846947
    Abstract: Provided herein are sirtuin-modulating compounds of formula (II). The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders relating to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
    Type: Grant
    Filed: July 2, 2009
    Date of Patent: September 30, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Chi B. Vu, Jeremy S. Disch, Pui Yee Ng, Charles A. Blum, Robert B. Perni
  • Patent number: 8846715
    Abstract: The present invention relates to (2S,3R)—N-(2-((3-pyridinyl)methyl)-1-azabicyclo[2.2.2]oct-3-yl)benzofuran-2-carboxamide, novel salt forms thereof, methods for its preparation, novel intermediates, and methods for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central and autonomic nervous systems.
    Type: Grant
    Filed: July 22, 2013
    Date of Patent: September 30, 2014
    Assignee: Targacept, Inc.
    Inventors: Merouane Bencherif, Lisa Benson, Gary Maurice Dull, Nikolai Federov, Gregory J. Gatto, Kristen G. Jordan, Anatoly A. Mazurov, Lan Miao, Julio A. Munoz, Inigo Pfeiffer, Sondra Pfeiffer, Teresa Phillips
  • Publication number: 20140288118
    Abstract: The invention relates to N-biarylamides, methods for production and use thereof for the production of medicaments for the treatment and/or prophylaxis of diseases and for improvement in cognition, concentration power, learning power and/or memory.
    Type: Application
    Filed: February 21, 2014
    Publication date: September 25, 2014
    Inventors: Timo Flebner, Frank-Gerhard Boss, Frank-Thorsten Hafner, Joachim Luithle, Christoph Methfessel, Leila Telan
  • Publication number: 20140275011
    Abstract: Disclosed are compound of Formula (Ia), wherein R2, R12, R16, J, Q, X, Y and Z are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds may be used as agents in the treatment of diseases, including cancer. Also provided are pharmaceutical compositions comprising one or more compounds of Formula (Ia).
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Applicant: AbbVie Inc.
    Inventors: Anthony Mastracchio, Milan Bruncko, Chunqiu Lai, Julie M. Miyashiro, Zhi-Fu Tao, Keith W. Woods, Thomas D. Penning, Andrew J. Souers
  • Patent number: 8796256
    Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalac
    Type: Grant
    Filed: May 24, 2011
    Date of Patent: August 5, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Gilles Bignan, Wing Cheung, Micheal Gaul, Hui Huang, Xun Li, Raymond Patch, Sharmila Patel, Mark Player, Guozhang Xu, Bao-Ping Zhao, Jian Liu
  • Patent number: 8772511
    Abstract: The invention relates to novel benzothiophene-, benzofuran-, and indole ureas and to the use thereof for producing medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning, and/or memory.
    Type: Grant
    Filed: April 6, 2012
    Date of Patent: July 8, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Timo Fleβner, Frank-Gerhard Böβ, Christina Erb, Frank-Thorsten Hafner, Katrin Schnizler, Dieter Lang, Joachim Luithle, Marja Van Kampen, Franz-Josef Van der Staay
  • Patent number: 8759524
    Abstract: A process is provided for efficiently producing an optically active 3-quinuclidinol derivative of high optical purity using a readily available ruthenium compound as an asymmetric reduction catalyst. This process is a process for producing an optically active 3-quinuclidinol derivative represented by the following formula (III) comprising asymmetrically hydrogenating a 3-quinuclidinone derivative represented by the following formula (I) in the presence of a ruthenium compound (II) represented by formula (II): Ru(X)(Y)(Px)n[R1R2C*(NR3R4)-A-R5R6C*(NR7R8)] (in the formulas, R represents a hydrogen atom or C7 to C18 aralkyl group and the like, X and Y represent hydrogen atoms or halogen atoms and the like, Px represents a phosphine ligand, n represents 1 or 2, R1 to R8 represent hydrogen atoms or C1 to C20 alkyl groups and the like, * represents an optically active carbon atom and A represents an ethylene group and the like).
    Type: Grant
    Filed: April 8, 2013
    Date of Patent: June 24, 2014
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Takeshi Ohkuma, Noriyoshi Arai, Masaya Akashi, Hirohito Oooka, Tsutomu Inoue
  • Patent number: 8754074
    Abstract: The present invention relates to the use of the vinyl quinuclidine enantiomer (R) of the following formula 2 as a synthesis intermediate in the preparation of (R)-mequitazine.
    Type: Grant
    Filed: January 10, 2012
    Date of Patent: June 17, 2014
    Assignees: Pierre Fabre Medicament, Commissariat a l'Energie Atomique et aux Energies Alternatives
    Inventors: Marc Nicolas, Laurent Larquetoux, Sébastien Leroux, Eric Doris
  • Patent number: 8748613
    Abstract: Compounds of formula (I): wherein A, R1, R2, X, m, and n are as defined in the specification, are selective M3 receptor antagonists and may be used in the treatment of, inter alia, a respiratory disease such as asthma and COPD.
    Type: Grant
    Filed: December 28, 2012
    Date of Patent: June 10, 2014
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Gabriele Amari, Cristina Pesenti, Stefano Bossolo
  • Publication number: 20140135306
    Abstract: The invention relates to compounds of formula (I): as defined in the application. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof.
    Type: Application
    Filed: June 19, 2012
    Publication date: May 15, 2014
    Applicant: Novartis AG
    Inventors: Nicole Buschmann, Pascal Furet, Philipp Holzer, Joerg Kallen, Keiichi Masuya, Stefan Stutz
  • Patent number: 8716309
    Abstract: A pyridone derivative compound and a pharmaceutically acceptable salt, isomer, solvate or hydrate thereof, and a preventive or therapeutic pharmaceutical composition for cognitive disorders that includes the pyridone derivative compound or a pharmaceutically acceptable salt, isomer, solvate or hydrate thereof.
    Type: Grant
    Filed: January 30, 2012
    Date of Patent: May 6, 2014
    Assignee: SK Biopharmaceuticals Co., Ltd.
    Inventors: Cheol Young Maeng, Young Koo Jang, Su Bong Cha, Hye Won Shin, Chan Mi Joung, Hwa Ryun Cha, Eun Jung Yi
  • Publication number: 20140116434
    Abstract: Dry powder inhalers comprising a muscarinic acetylcholine receptor antagonist and optionally a beta 2 agonist and/or a corticosteroid for use in the treatment of inflammatory or respiratory tract diseases, such as asthma or COPD.
    Type: Application
    Filed: June 1, 2012
    Publication date: May 1, 2014
    Applicant: GLAXO GROUP LIMITED
    Inventor: Glenn Crater
  • Patent number: 8710227
    Abstract: Crystalline Forms I and II of (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide hydrochloride monohydrate and compositions, methods of manufacture and therapeutic uses thereof are described.
    Type: Grant
    Filed: May 17, 2011
    Date of Patent: April 29, 2014
    Assignee: EnVivo Pharmaceuticals, Inc.
    Inventors: Patricia Oliver-Shaffer, Gideon Shapiro, Richard Chesworth, Muneki Kishida, Takayuki Ishige
  • Publication number: 20140107027
    Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.
    Type: Application
    Filed: December 18, 2013
    Publication date: April 17, 2014
    Applicant: BHI LIMITED PARTNERSHIP
    Inventors: Xianqi Kong, David Migneault, Isabelle Valade, Xinfu Wu, Francine Gervais
  • Patent number: 8697722
    Abstract: The disclosure provides compounds capable of selectively or non-selectively modulating nicotinic acetylcholine receptors. The compounds, compositions, and methods described herein are useful, for example, in treating patients suffering from various medical conditions including pain, chemical addictions, Parkinson's disease, Alzheimer's disease, and neurodegenerative disorders. In one embodiment, the compounds comprise a 7- to 11-membered azabicyclo ring.
    Type: Grant
    Filed: November 2, 2007
    Date of Patent: April 15, 2014
    Assignee: SRI International
    Inventors: Faming Jiang, Taline Khroyan, Cris M. Olsen, Willma E. Polgar, Lawrence R. Toll, Nurulain T. Zaveri
  • Publication number: 20140088078
    Abstract: The invention provides tricyclic compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tricyclic compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.
    Type: Application
    Filed: May 7, 2012
    Publication date: March 27, 2014
    Applicant: ZAFGEN, Inc.
    Inventors: Susan Mary Cramp, Hazel Joan Dyke, Thomas David Pallin, Robert Zahler
  • Publication number: 20140080863
    Abstract: Muscarinic Acetylcholine Receptor Antagonists and methods of using them are provided.
    Type: Application
    Filed: October 14, 2013
    Publication date: March 20, 2014
    Applicant: Glaxo Group Limited
    Inventors: Dramane Ibrahim LAINE, Michael R. Palovich, Brent W. McCleland, Christopher E. Neipp, Sonia M. Thomas
  • Publication number: 20140058100
    Abstract: To provide a pharmaceutical, in particular a compound which can be used as a therapeutic agent for irritable bowel syndrome (IBS). It was found that a tetrahydroisoquinolin-1-one derivative having an amide group at the 4-position or a pharmaceutically acceptable salt thereof has an excellent bombesin 2 (BB2) receptor antagonistic action. It is also found that the tetrahydroisoquinolin-1-one derivative is highly effective on bowel movement disorders. From the above, the tetrahydroisoquinolin-1-one derivative of the present invention is useful as a therapeutic agent for diseases associated with a BB2 receptor, in particular IBS.
    Type: Application
    Filed: July 15, 2013
    Publication date: February 27, 2014
    Applicant: Seldar Pharma Inc.
    Inventors: Hiroyuki Hisamichi, Itsuro Shimada, Tsukasa Ishihara, Tomofumi Takuwa, Takafumi Shimizu, Noriko Ishikawa, Kyoichi Maeno, Norio Seki
  • Publication number: 20140045779
    Abstract: This invention relates with anti-tumor activities of new compounds containing an adamantyl group or analogs thereof.
    Type: Application
    Filed: August 29, 2011
    Publication date: February 13, 2014
    Inventor: Lifeng Xu
  • Publication number: 20140030191
    Abstract: A compound having the following general formula (I): wherein: X is a nitrogen atom and Y is a carbon atom; or X is a carbon atom and Y is a nitrogen atom; the Ar group is an aryl or heteroaryl group; and the RN and RN? groups, together with the carbon atoms to which they are bound, form a monocyclic or bicyclic azacycloalkane group. The pharmaceutically acceptable salts thereof, the hydrates or polymorphic crystalline structures thereof, and to the racemates, diastereoisomers, or enantiomers thereof are also described.
    Type: Application
    Filed: April 20, 2012
    Publication date: January 30, 2014
    Applicant: Centre National de la Recherche Scientifique (C.N.R.S.)
    Inventors: Sylvain Routier, Franck Suzenet, Frederic Pin, Sylvie Chalon, Johnny Vercouillie, Denis Guilloteau
  • Publication number: 20130338186
    Abstract: The invention relates to novel amides of acetic and propionic acids, methods for production and use thereof for the production of medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning ability and memory.
    Type: Application
    Filed: August 16, 2013
    Publication date: December 19, 2013
    Applicant: BAYER HEALTHCARE AG
    Inventors: Joachim Luithle, Frank-Gerhard Bob, Christina Erb, Katrin Schnizler, Timo Flessner, Marja Van Kampen, Christoph Methfessel