Bicyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos Patents (Class 514/299)
  • Patent number: 10342791
    Abstract: Methods of prevention of symptomatic malaria in a malaria-naïve, G6PD-normal human subject comprising administering to the human subject a compound of Formula (I), a pharmaceutically acceptable salt thereof, or pharmaceutical composition comprising a compound of Formula (I). A compound of Formula (I) can be administered prior to potential exposure of a species of Plasmodium, during potential exposure of a species of Plasmodium, and after potential exposure of a species of Plasmodium. The methods of the invention also pertains to kits comprising specific doses of Formula (I), a pharmaceutically acceptable salt thereof, or pharmaceutical composition comprising a compound of Formula (I), and instructions for administration of dosing quantity and frequency. The methods of the invention also pertain to determining doses of Formula (I) that meet the general regulatory requirement for a drug to be efficacious in the prevention of malaria in malaria-naïve subjects.
    Type: Grant
    Filed: December 2, 2015
    Date of Patent: July 9, 2019
    Assignees: 60 Degrees Pharmaceuticals LLC, The United States Of America As Represented By The Secretary Of The Army
    Inventors: Bryan L Smith, John P Jones, Moshe Shmuklarsky, Budda Balasubrahmanyam
  • Patent number: 10300053
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof, for use in the treatment of leukemia.
    Type: Grant
    Filed: November 5, 2015
    Date of Patent: May 28, 2019
    Assignee: ACTIVE BIOTECH AB
    Inventors: Helena Eriksson, Leif Svensson, Marie Törngren
  • Patent number: 10266530
    Abstract: Disclosed are compounds of Formula (I), methods of using the compounds for inhibiting HPK1 activity and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with HPK1 activity such as cancer.
    Type: Grant
    Filed: September 8, 2017
    Date of Patent: April 23, 2019
    Assignee: Incyte Corporation
    Inventors: Oleg Vechorkin, Jun Pan, Kai Liu, Alexander Sokolsky, Anlai Wang, Hai Fen Ye, Wenqing Yao
  • Patent number: 10100311
    Abstract: The present invention relates to a method for the treatment of fibrosis, in particular cardiac fibrosis, comprising the administration of an inhibitor of insulin-regulated aminopeptidase (IRAP). Preferable the IRAP inhibitor is chosen from the group including HFI-419, HA-08, AL-40, HFI-437, Val-Tyr-Ile-His-Pro-Phe (otherwise known as angiotensin IV or ANG IV), c[Cys-Tyr-Cys]-His-Pro-Phe, and c[Hcy-Tyr-Hcy]-His-Pro-Phe.
    Type: Grant
    Filed: July 29, 2016
    Date of Patent: October 16, 2018
    Assignee: MONASH UNIVERSITY
    Inventors: Siew Yeen Chai, Robert Widdop, Tracey Gaspari, Huey Wen Lee
  • Patent number: 10034947
    Abstract: The present invention provides compositions containing clopidogrel, present as a free base or a pharmaceutically acceptable salt thereof, and sulfoalkyl ether cyclodextrin (SAE-CD). The compositions can be liquid, suspension or solid compositions. They can be adapted for oral, peroral or parenteral administration. The SAE-CD serves to aid in dissolution and stabilization of the clopidogrel in aqueous media. The stability of clopidogrel against hydrolytic degradation, thermal degradation, and photolytic degradation are improved. SAE-CD provides improved results over other cyclodextrin derivatives. The SAE-CD-containing composition of clopidogrel can be provided in liquid form, solid form or as a reconstitutable powder. Both ready-to-use and concentrated liquid compositions can be prepared. The liquid composition is optionally available as a clear solution.
    Type: Grant
    Filed: March 9, 2017
    Date of Patent: July 31, 2018
    Assignee: Cydex Pharmaceuticals, Inc.
    Inventors: Gerold L. Mosher, Rebecca L. Wedel, Karen T. Johnson, Stephen G. Machatha, Jane A. Cowee, Daniel J. Cushing
  • Patent number: 10005762
    Abstract: The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically an agent for treating nocturia. The inventors have assumed that inhibition of nocturnal activity of placental leucine aminopeptidase (P-LAP), i.e. aminopeptidase that cleaves AVP, would maintain and/or increase an endogenous AVP level to enhance the antidiuretic effect, which would contribute to a decreased number of nocturnal voids, and have extensively studied compounds which inhibit P-LAP. As a result, the inventors have found that (2R)-3-amino-2-(pyridylmethyl)-2-hydroxy-propanoic acid derivatives have excellent P-LAP inhibitory activity. The inventors have evaluated antidiuretic effects in water-loaded rats and have found that the compounds increase endogenous AVP levels by inhibiting P-LAP and consequently reduce urine production. The present invention therefore provides compounds expected to be used as an agent for treating nocturia based on P-LAP inhibition.
    Type: Grant
    Filed: December 4, 2015
    Date of Patent: June 26, 2018
    Assignees: Astellas Pharma Inc., KOTOBUKI PHARMACEUTICAL CO., LTD.
    Inventors: Kenichi Kawaguchi, Akihiro Ishihata, Akira Kanai, Kazuyuki Tsuchiya, Yusuke Inagaki, Junichi Kazami, Hiroshi Morikawa, Masashi Hiramoto, Kentaro Enjo, Hajime Takamatsu
  • Patent number: 9933417
    Abstract: The presently-disclosed subject matter includes azetidine-substituted fluorescent compounds, where the compounds may be used as probes, dyes, tags, and the like. The presently-disclosed subject matter also includes kits comprising the same as well as methods for using the same to detect a target substance.
    Type: Grant
    Filed: April 1, 2015
    Date of Patent: April 3, 2018
    Assignee: HOWARD HUGHES MEDICAL INSTITUTE
    Inventors: Luke D. Lavis, Jonathan B. Grimm, Jiji Chen, Timothee Lionnet, Zhengjian Zhang, Andrey Revyakin, Joel Slaughter
  • Patent number: 9932338
    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: November 30, 2016
    Date of Patent: April 3, 2018
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Laura Carzaniga, Fabio Rancati, Andrea Rizzi, Ian Linney
  • Patent number: 9884043
    Abstract: The present invention relates to compounds according to Formula (I) or a pharmaceutically acceptable salt or solvate thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or condition.
    Type: Grant
    Filed: March 20, 2017
    Date of Patent: February 6, 2018
    Assignees: Merck Sharp & Dohme Corp., Merck Sharp & Dohme B.V.
    Inventors: Willem Frederik Johan Karstens, Mario Van Der Stelt, Jos Cals, Rita Corte Real Goncalves Azevedo, Kenneth Jay Barr, Hongjun Zhang, Richard Thomas Beresis, Dongshan Zhang, Xiaobang Duan
  • Patent number: 9795694
    Abstract: The present invention is in the field of pharmaceuticals and chemical industries. In particular, one aspect of the present invention relates to methods for labeling, imaging and detecting the beta-amyloid (A?) peptides, oligomers, and fibrils in vitro and in vivo via magnetic resonance and florescence imaging by using modified carbazole-based fluorophores. A further aspect of the present invention relates to a method of reducing and preventing aggregation of beta-amyloid peptides for Alzheimer's disease (AD) as well as of treating and/or preventing Alzheimer's disease by using the modified carbazole-based fluorophore. The modified carbazole-based fluorophore according to an embodiment of the present invention is prepared by conjugating a carbazole-based fluorophore with magnetic nanoparticles to form a conjugate which is permeable to blood brain barrier of a subject being introduced therewith.
    Type: Grant
    Filed: February 21, 2016
    Date of Patent: October 24, 2017
    Assignee: Hong Kong Baptist University
    Inventors: Yinhui Li, Di Xu, See-Lok Ho, Chung-Yan Poon, Hei-Nga Chan, Hung Wing Li, Ricky M. S. Wong
  • Patent number: 9775920
    Abstract: The present invention relates to a novel use of N-(4-isopropylphenyl)-5-amino-isoindoline for diagnosing Alzheimer's disease and quantifying amyloid in the brain.
    Type: Grant
    Filed: July 29, 2016
    Date of Patent: October 3, 2017
    Assignee: INSTITUTE OF NUCLEAR ENERGY RESEARCH, ATOMIC ENERGY COUNCIL, EXECUTIVE YUAN, R.O.C.
    Inventors: Wan-I Kuo, Jian-Hua Zhao, Kang-Wei Chang, Tsai-Yueh Luo, Wei-Hsi Chen
  • Patent number: 9688615
    Abstract: The invention relates to compounds useful in treating conditions associated with voltage-gated ion channel function, particularly conditions associated with sodium channel activity. More specifically, the invention concerns compounds (e.g., compounds according to any of Formulas (I)-(XIII) or Compounds (1)-(236) of Table 1) that are useful in treatment of a variety of diseases and conditions.
    Type: Grant
    Filed: August 24, 2015
    Date of Patent: June 27, 2017
    Assignee: DEGIACOMO, INTERIM TRUSTEE, MARK G.
    Inventors: Hassan Pajouhesh, Richard Holland, Lingyun Zhang, Hossein Pajouhesh, Jason Lamontagne, Brendan Whelan
  • Patent number: 9629830
    Abstract: Provided is the discovery of the role of EphA4 signaling in neurodegenerative disorders involving ?-amyloid induced neurotoxicity such as Alzheimer's Disease. New therapeutic methods, therapeutic agents, and kits for treating diseases caused or exacerbated by overactivated EphA4 signaling are provided. Also provided are methods for identifying additional compounds as therapeutic agents useful for treating conditions involving overly active EphA4 signaling.
    Type: Grant
    Filed: July 17, 2014
    Date of Patent: April 25, 2017
    Assignee: The Hong Kong University of Science and Technology
    Inventors: Nancy Yuk Yu Ip, Kit Yu Fu, Fanny Chui Fun Ip, Wing Yu Fu, Shuo Gu, Xuhui Huang, Kwok Wang Hung
  • Patent number: 9623045
    Abstract: The present invention provides compositions containing clopidogrel, present as a free base or a pharmaceutically acceptable salt thereof, and sulfoalkyl ether cyclodextrin (SAE-CD). The compositions can be liquid, suspension or solid compositions. They can be adapted for oral, peroral or parenteral administration. The SAE-CD serves to aid in dissolution and stabilization of the clopidogrel in aqueous media. The stability of clopidogrel against hydrolytic degradation, thermal degradation, and photolytic degradation are improved. SAE-CD provides improved results over other cyclodextrin derivatives. The SAE-CD-containing composition of clopidogrel can be provided in liquid form, solid form or as a reconstitutable powder. Both ready-to-use and concentrated liquid compositions can be prepared. The liquid composition is optionally available as a clear solution.
    Type: Grant
    Filed: September 4, 2015
    Date of Patent: April 18, 2017
    Assignee: CyDex Pharmaceuticals, Inc.
    Inventors: Gerold L. Mosher, Rebecca L. Wedel, Karen T. Johnson, Stephen G. Machatha, Jane A. Cowee, Daniel J. Cushing
  • Patent number: 9546166
    Abstract: The present invention relates to indolizine compounds, and pharmaceutically acceptable compositions thereof, useful as antagonists of P2X7, and for the treatment of P2X7-related disorders.
    Type: Grant
    Filed: July 31, 2015
    Date of Patent: January 17, 2017
    Assignee: Merck Patent GmbH
    Inventors: Srinivasa R. Karra, Andreas Goutopoulos
  • Patent number: 9512097
    Abstract: The present invention relates to a process for the preparation of 3-aroyl-5-aminobenzofuran derivatives useful as antiarrhythmic drugs which avoids the use of nitro intermediates.
    Type: Grant
    Filed: November 11, 2011
    Date of Patent: December 6, 2016
    Assignee: Lek Pharmaceuticals D.D.
    Inventors: Frank Richter, Erwin Schreiner, Samo Pirc, Anton Copar
  • Patent number: 9403794
    Abstract: The present invention is in the field of pharmaceuticals and chemical industries. In particular, the present invention relates to methods for labeling, imaging and detecting the beta-amyloid (A?) peptides, oligomers, and fibrils in vitro by using carbazole-based fluorophores. A further aspect of the present invention relates to a method of reducing and preventing aggregation of beta-amyloid peptides for Alzheimer's disease (AD) as well as of treating and/or preventing Alzheimer's disease by using carbazole-based fluorophores.
    Type: Grant
    Filed: March 31, 2014
    Date of Patent: August 2, 2016
    Assignee: HONG KONG BAPTIST UNIVERSITY
    Inventors: Lei Guo, Di Xu, See-Lok Ho, Chung-Yan Poon, Olivia T. W. Ng, Hung Wing Li, Ken K. L. Yung, Daniel W. J. Kwong, Ricky M. S. Wong
  • Patent number: 9382223
    Abstract: The invention relates to a novel process for the preparation of dronedarone (I) and pharmaceutically acceptable salts thereof (formula I), which comprises oxidizing a compound of formula (VI), or a salt thereof and the obtained product is isolated and, if desired, converted into a pharmaceutically acceptable salt thereof. Further aspects of the invention include the novel intermediary compound of formula (VI) and process for the preparation thereof.
    Type: Grant
    Filed: February 14, 2013
    Date of Patent: July 5, 2016
    Assignee: SANOFI
    Inventors: Csaba Huszár, Adrienn Hegedus, Zsolt Dombrády
  • Patent number: 9242953
    Abstract: The present disclosure relates to processes for preparing dronedarone or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: August 26, 2014
    Date of Patent: January 26, 2016
    Assignee: Gilead Sciences, Inc.
    Inventors: Johann Chan, Justin Vitale
  • Patent number: 9179304
    Abstract: Embodiments described herein may help to protect users' privacy when storing and/or utilizing location data that is provided by the users' mobile devices. An example method may involve: (a) determining a location history associated with a first client device, wherein the location history comprises a plurality of time-stamped location reports associated with the first client device, (b) before the location history is exported: (i) identifying at least one stop in the location history, wherein the at least one stop corresponds to a plurality of location reports that indicate a substantial lack of movement by the first client device, and (ii) scrubbing the location history in order to obscure at least one location report that corresponds to the at least one stop, and (c) exporting the scrubbed location history to long-term data storage.
    Type: Grant
    Filed: September 18, 2013
    Date of Patent: November 3, 2015
    Assignee: Google Inc.
    Inventors: Stephen David Zelinka, Eli Brandt
  • Patent number: 9156814
    Abstract: The present invention relates to methods of detecting and monitoring aggregation of beta-amyloid peptides which are associated with neurodegenerative diseases as well as treating and/or preventing the neurodegenerative diseases by using carbazole-based fluorophores. In particular, the present invention provides methods for labeling and imaging the beta-amyloid (A?) peptides, oligomers, and fibrils in vitro and/or in vivo, as well as treating and/or preventing Alzheimer's disease by using the carbazole-based fluorophores of the present invention.
    Type: Grant
    Filed: April 13, 2012
    Date of Patent: October 13, 2015
    Assignee: HONG KONG BAPTIST UNIVERSITY
    Inventors: Wanggui Yang, Yi Wong, Olivia T. W. Ng, Hung Wing Li, Ken K. L. Yung, Daniel W. J. Kwong, Ricky M. S. Wong
  • Patent number: 9125945
    Abstract: The present invention provides compositions containing clopidogrel, present as a free base or a pharmaceutically acceptable salt thereof, and sulfoalkyl ether cyclodextrin (SAE-CD). The compositions can be liquid, suspension or solid compositions. They can be adapted for oral, peroral or parenteral administration. The SAE-CD serves to aid in dissolution and stabilization of the clopidogrel in aqueous media. The stability of clopidogrel against hydrolytic degradation, thermal degradation, and photolytic degradation are improved. SAE-CD provides improved results over other cyclodextrin derivatives. The SAE-CD-containing composition of clopidogrel can be provided in liquid form, solid form or as a reconstitutable powder. Both ready-to-use and concentrated liquid compositions can be prepared. The liquid composition is optionally available as a clear solution.
    Type: Grant
    Filed: October 6, 2014
    Date of Patent: September 8, 2015
    Assignee: Cydex Pharmaceuticals, Inc.
    Inventors: Gerold L. Mosher, Rebecca L. Wedel, Karen T. Johnson, Stephen G. Machatha, Jane A. Cowee, Daniel J. Cushing
  • Patent number: 9120819
    Abstract: FGF receptor agonist compounds corresponding to the general formula: M1-L-M2 are disclosed in which M1 and M2, which may be identical or different, each represent, independently of one another, a monomer unit M, and L represents a linker group, wherein the monomer unit is of the general formula I.
    Type: Grant
    Filed: July 11, 2008
    Date of Patent: September 1, 2015
    Assignee: SANOFI
    Inventors: Francoise Bono, Nathalie Guillo, Jean-Pierre Maffrand, Pierre Fons, Jacob-Alsboek Olsen, Gilles Anne-Archard
  • Patent number: 9078934
    Abstract: A method for sterilizing an antiseptic solution includes providing a container containing the antiseptic solution, the antiseptic solution having an initial purity, selecting a sterilization temperature from about 85° C. to about 135° C. and an sterilization time from about 1 minute to about 19 hours, heating the antiseptic solution to the selected sterilization temperature, maintaining the temperature for the selected sterilization time, and terminating the heating of the antiseptic solution when the sterilization time expires. After terminating the heating, the antiseptic solution has a post-sterilization purity. The sterilization temperature and the sterilization time are selected such that after terminating the heating, the antiseptic solution is sterile and has a post-sterilization purity of at least about 92% and the percentage point change in purity from the initial purity to the post-sterilization purity is at most about 5%.
    Type: Grant
    Filed: March 5, 2014
    Date of Patent: July 14, 2015
    Assignee: CAREFUSION 2200, INC.
    Inventors: Satish Degala, Christopher Matthew McGinley, Kenneth Bruce Thurmond, II
  • Patent number: 9062042
    Abstract: Provided herein are novel and selective high affinity ?3?4 nicotinic acetylcholine receptor ligands and pharmaceutical compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, drug addiction or pain using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods for modulating a nicotinic acetylcholine receptor (nAChR). In still other embodiments, provided herein are methods of selectively antagonizing receptors such as, for example, the ?3?4 nicotinic acetylcholine receptor using the compounds and compositions disclosed herein.
    Type: Grant
    Filed: January 11, 2011
    Date of Patent: June 23, 2015
    Assignee: Astraea Therapeutics, LLC
    Inventors: Nurulain T. Zaveri, Faming Jiang
  • Patent number: 9040508
    Abstract: The present invention relates to novel synthetic substituted heterocyclic compounds and pharmaceutical compositions containing the same that are capable of inhibiting or antagonizing a family of receptor tyrosine kinases, Tropomysosin Related Kinases (Trk), in particular the nerve growth factor (NGF) receptor, TrkA. The invention further concerns the use of such compounds in the treatment and/or prevention of pain, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, or a disease, disorder or injury relating to dysmyelination or demyelination or the disease or disorder associated with abnormal activities of NGF receptor TrkA.
    Type: Grant
    Filed: December 8, 2009
    Date of Patent: May 26, 2015
    Assignee: VM Pharma LLC
    Inventors: Jay Jie-Qiang Wu, Ling Wang
  • Patent number: 9040532
    Abstract: Compounds are described herein useful for treating diseases and conditions by modulation of one or more alpha adrenergic receptor. The compounds can include a naphthalene, a quinoline, a benzoimidazole or an isoquinoline as a core structure. Methods of making, using and formulating these compounds are described.
    Type: Grant
    Filed: October 6, 2010
    Date of Patent: May 26, 2015
    Assignee: Allergan, Inc.
    Inventors: Ken Chow, Liming Wang, Wenkui K. Fang, Evelyn G. Corpuz, Santosh C. Sinha, Daniel W. Gil, Mohammad I. Dibas, John E. Donello
  • Patent number: 9029378
    Abstract: Substituted bicyclic aromatic carboxamide and urea compounds as vanilloid receptor ligands, pharmaceutical compositions containing these compounds, and a method of using these compounds in the treatment and/or inhibition of pain and further diseases and/or disorders mediated at least in part via the vanilloid receptor 1 (VR1/TRPV1).
    Type: Grant
    Filed: July 25, 2012
    Date of Patent: May 12, 2015
    Assignee: Gruenenthal GmbH
    Inventors: Robert Frank, Thomas Christoph, Bernhard Lesch, Jeewoo Lee
  • Publication number: 20150119362
    Abstract: The present invention relates to compounds and methods useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of disease.
    Type: Application
    Filed: October 24, 2013
    Publication date: April 30, 2015
    Inventors: Mark E. Gurney, Timothy J. Hagen, Joel R. Walker, Xuesheng Mo, A. Samuel Vellekoop, Robert Campbell, Lei Zhu, Donna L. Romero
  • Patent number: 9012447
    Abstract: The present invention provides 5-HT3 receptor antagonists of Formula (I): which are useful for the treatment of diseases treatable by inhibition of 5-HT3 receptor such as emesis, pain, drug addiction, neurodegenerative and psychiatric disorders, and GI disorders. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
    Type: Grant
    Filed: July 16, 2013
    Date of Patent: April 21, 2015
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Stephen Hitchcock, Holger Monenschein, Holly Reichard, Huikai Sun, Shota Kikuchi, Todd Macklin, Maria Hopkins
  • Publication number: 20150105378
    Abstract: The present invention provides compounds of Formula (I) or Formula (III): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Inventors: Lynn Abell, Leonard Adam, Cullen L. Cavallaro, Heather Finlay, Todd J. Friends, Jon J. Hangeland, Ji Jiang, R. Michael Lawrence, John Lloyd, Zulan Pi, George O. Tora, Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
  • Patent number: 8993595
    Abstract: Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula Ia or Ib, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
    Type: Grant
    Filed: January 10, 2013
    Date of Patent: March 31, 2015
    Assignee: Idenix Pharmaceuticals, Inc.
    Inventors: Christophe Claude Parsy, Francois-Rene Alexandre, Michel Derock, Frederic Leroy, Jean-Christophe Meillon, Thierry Convard, Dominique Surleraux
  • 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
  • Publication number: 20150087650
    Abstract: The present invention relates to 1-aza-bicy-cloalkyl derivatives of Formula (I); wherein the substituents are as defined in the specification, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them. Formula (I), wherein A represents O or N(R?); Y represents a group of formula, or wherein the left bond is attached to the A group and the right bond is attached to the R group; R represents a substituted or unsubstituted C5-C10aryl, substituted or unsubstituted hetero-C5-C10aryl, a group N(R1)(R4), or a group N(R2)(CHP3R4); R represent a hydrogen, C1-C4alkyl, or CF3; R2 represents hydrogen, C1-C4alkyl, or CF3; R3 represents hydrogen, C1-C4alkyl, or CF3; R4 represents a substituted or unsubstituted C5-C10 aryl or a substituted or unsubstituted C5-C10heteroaryl; in free base or acid addition salt form.
    Type: Application
    Filed: December 3, 2014
    Publication date: March 26, 2015
    Applicant: NOVARTIS AG
    Inventors: Dominik FEUERBACH, Werner Müller, Bernard Lucien ROY, Thomas TROXLER, Konstanze HURTH, Mathias FREDERIKSEN
  • Publication number: 20150065523
    Abstract: The present invention provides compounds of formula (I) including stereoisomers or a racemate or a mixture or a pharmaceutically acceptable salt thereof: wherein X is NH, or O; Q is 5-6 membered heteroaryl group, which may be substituted by one or more substituents independently selected from a group consisting of: C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN; A is phenyl or a 5-6 heteroaryl group, which may be substituted by one or more substituents independently selected from a group consisting of: C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN; B may assume different meanings from A and is phenyl or a 5-6 membered heteroaryl group, which may be substituted by one or more substituents independently selected from a group consisting of: C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN; and processes for their preparation, pharmaceutical compositions containing them and their use as dual antagonists of the Orexin 1 and Orexin 2 receptors.
    Type: Application
    Filed: March 18, 2013
    Publication date: March 5, 2015
    Inventors: Luigi Piero Stasi, Lucio Claudio Rovati
  • Publication number: 20150065501
    Abstract: The invention relates to N-substituted hetero-bicyclic furanone compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to methods and uses of these N-substituted hetero-bicyclic furanone compounds, and of compositions comprising thereof, for combating and controlling animal pests. Furthermore the invention relates also to pesticidal methods of applying such N-substituted hetero-bicyclic furanone compounds. The N-substituted hetero-bicyclic furanone compounds of the present invention are defined by the following formula I: wherein A, X, Het, W1, W2, W3, R1, R2 and R4 are defined as in the description.
    Type: Application
    Filed: March 27, 2013
    Publication date: March 5, 2015
    Inventors: Nina Gertrud Bandur, Ralph Paulini, Florian Kaiser, Arun Narine, Joachim Dickhaut, Karsten Körber
  • Publication number: 20150051243
    Abstract: The invention provides 8-azabicyclo[3.2.1]octyl-2-hydroxybenzamide compounds of formula (I): wherein R2, R7, and m are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Application
    Filed: June 26, 2014
    Publication date: February 19, 2015
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Daisuke Roland Saito, Daniel D. Long, Lan Jiang, Bryan Frieman
  • Patent number: 8952180
    Abstract: The present invention provides compounds of Formula (I) or Formula (III): [INSERT CHEMICAL STRUCTURE HERE] (I) [INSERT CHEMICAL STRUCTURE HERE] (III) as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Grant
    Filed: September 25, 2012
    Date of Patent: February 10, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Lynn Abell, Leonard Adam, Cullen L. Cavallaro, Heather Finlay, Todd J. Friends, Jon J. Hangeland, Ji Jiang, R. Michael Lawrence, John Lloyd, Zulan Pi, George O. Tora, Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
  • Patent number: 8952034
    Abstract: The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein W1, W2, W3, R1, Q, X1, X2 and X3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Grant
    Filed: July 26, 2010
    Date of Patent: February 10, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Britton Corkey, Elfatih Elzein, Robert Jiang, Rao Kalla, Tetsuya Kobayashi, Dmitry Koltun, Xiaofen Li, Gregory Notte, Eric Parkhill, Thao Perry, Jeff Zablocki
  • Publication number: 20150038509
    Abstract: The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and optionally contains additional rings. The compounds bind to chemokine receptors, including CXCR4 and CCR5, and demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).
    Type: Application
    Filed: June 12, 2014
    Publication date: February 5, 2015
    Inventors: Gary J. Bridger, Renato T. Skerlj, Al Kaller, Curtis Harwig, David Earl Bogucki, Trevor R. Wilson, Jason B. Crawford, Ernest J. McEachern, Bem Atsma, Siqiao Nan, Yuanxi Zhou, Dominique Schols, Christopher Dennis Smith, Maria Rosario DiFluri
  • Patent number: 8940762
    Abstract: The present invention is directed to methods of treating pain by administering a therapeutically effective amount of an ?7 nAChR ligand or a pharmaceutically acceptable salt thereof, to a mammal in need of treatment thereof and to pharmaceutical compositions comprising such a compound or salt.
    Type: Grant
    Filed: December 22, 2010
    Date of Patent: January 27, 2015
    Assignee: AbbVie Inc.
    Inventors: Chih-Hung Lee, Michael R. Schrimpf, Timothy A. Esbenshade, Chang Z. Zhu
  • Publication number: 20150025105
    Abstract: Disclosed herein are indolizine compounds of general formula I, wherein R1-R7, X and Y are as disclosed in the application, useful as inhibitors of lipoprotein associated phospholipase A2 (Lp-PLA2) and/or 15-lipoxygenase (15-LOX), as well as methods of preparation and use thereof, and compositions thereof Advantageously, certain compounds disclosed herein are capable of inhibiting both Lp-PLA2 and 15-LOX. Accordingly, provided herein are methods of inhibiting one or both of Lp-PLA2 and 15-LOX, and methods of treating diseases or conditions associated with Lp-PLA2 and/or 15-LOX.
    Type: Application
    Filed: February 8, 2013
    Publication date: January 22, 2015
    Inventors: Praveen Rao PERAMPALLI NEKKAR, Saad NAMBIL KABIR
  • Publication number: 20150018332
    Abstract: The invention generally relates to nuclear transport modulators, e.g CRM1 inhibitors, and more particularly to a compound represented by formula (I): or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula (I), or a pharmaceutically acceptable salt or composition thereof, e.g, in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.
    Type: Application
    Filed: July 26, 2012
    Publication date: January 15, 2015
    Applicant: KARYOPHARM THERAPEUTICS INC.
    Inventors: Vincent P. Sandanayaka, Sharon Shacham, Michael Kauffman, Sharon Shechter, Dilara McCauley, Yosef Landesman, William Senapedis, Jean-Richard Saint-Martin
  • Patent number: 8933229
    Abstract: Disclosed is a compound represented by formula (1) or a pharmacologically acceptable salt thereof (In the formula, A represents a group that is represented by formula (A-1); R1a and R1b may be the same or different and each independently represents a C1-6 alkyl group which may be substituted by one to three halogen atoms; m and n each independently represents an integer of 0-5; X1 represents a hydroxyl group or an aminocarbonyl group; Z1 represents a single bond or the like; and R2 represents an optionally substituted C1-6 alkyl group, an optionally substituted C6-10 aryl group or the like).
    Type: Grant
    Filed: November 11, 2010
    Date of Patent: January 13, 2015
    Assignee: Sumitomo Dainippon Pharma Co., Ltd.
    Inventors: Yoshihiro Horiuchi, Kiyoto Sawamura, Hiroaki Fujiwara
  • Publication number: 20150005292
    Abstract: There is described a method for increasing the maximal tolerated close and thus the efficacy of an acetyl choline esterase inhibitor (AChEI) in a patient suffering from an Alzheimer type dementia by decreasing concomitant adverse effects by administration of said AChEI in combination with a non-anticholinergic antiemetic agent, whereby an enhanced acetyl choline esterase inhibition in the CNS of said patient is achieved and alleviation of the symptoms of Alzheimer type dementia in said patient is thereby improved to a greater extent. The use of a non-anticholinergic antiemetic agent for the preparation of a pharmaceutical composition for the treatment of Alzheimer type dementia in combination with an acetyl choline esterase inhibitor (AChEI) and pharmaceutical compositions comprising (a) a 5HT3 receptor antagonist, a dopamine antagonist, a H1-receptor antagonist, a cannabinoid agonist, aprepitant or casopitant as an antiemetic agent and (b) an acetylcholine esterase inhibitor are also described.
    Type: Application
    Filed: September 18, 2014
    Publication date: January 1, 2015
    Applicant: CHASE PHARMACEUTICALS CORPORATION
    Inventors: Thomas N. CHASE, Kathleen E. CLARENCE-SMITH
  • Patent number: 8921390
    Abstract: A Medicaments for inhibiting thrombus formation contains active ingredients which are triflusal and clopidogrel bisulfate, wherein a mass ratio of triflusal to clopidogrel bisulfate is (100-650):(30-150), preferably (1-20):1, more preferably (3-6):1, and even more preferably 3:1 or 6:1.
    Type: Grant
    Filed: March 17, 2010
    Date of Patent: December 30, 2014
    Assignee: Guizhou Liansheng Pharmaceutical Co. Ltd.
    Inventor: Chunhua Su
  • Patent number: 8921369
    Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.
    Type: Grant
    Filed: December 2, 2009
    Date of Patent: December 30, 2014
    Assignee: Presidio Pharmaceuticals, Inc.
    Inventors: Min Zhong, Leping Li
  • Publication number: 20140378504
    Abstract: This invention relates to 2-Aza-bicyclo[2.2.2]octane-3-carboxylic acid (benzyl-cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
    Type: Application
    Filed: September 11, 2014
    Publication date: December 25, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Ralf ANDERSKEWITZ, Matthias GRAUERT, Marc GRUNDL, Thorsten OOST, Alexander PAUTSCH, Stefan PETERS
  • Publication number: 20140377223
    Abstract: The present invention relates to novel Substituted Biphenylene Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein Y1, Y2, R1, R2, R4, Ra and Rb are as defined herein. The present invention also relates to compositions comprising at least one Substituted Biphenylene Compound, and methods of using the Substituted Biphenylene Compounds for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: July 21, 2011
    Publication date: December 25, 2014
    Inventors: Joseph A. Kozlowski, Bandarpalle B. Shankar
  • Patent number: RE45364
    Abstract: A chemical compound represented by the formula [I]: (wherein R1 represents a hydroxyl group or the like, m represents 0 or an integer of 1 to 5, R2 represents a halogen atom or the like, k represents 0 or an integer of 1 to 4, R3, R31, R4, R41, R5, R51, R6, R61, and R7 each independently represents a hydrogen atom or the like, X represents an oxygen atom or the like, and n represents 1), a salt, an N-oxide of the chemical compound represented by formula [I], and a pest control agent containing the formula [I] as its active constituent.
    Type: Grant
    Filed: January 21, 2014
    Date of Patent: February 3, 2015
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Isami Hamamoto, Jun Takahashi, Makio Yano, Daisuke Hanai, Takao Iwasa