Bicyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos Patents (Class 514/299)
  • Patent number: 11834663
    Abstract: The present invention relates to compositions, methods and kits for the treatment of fibrosis. In particular, the compositions, methods and kits are particularly useful, but not limited to, the treatment of cardiac fibrosis. The invention provides a method of treating fibrosis in an individual comprising administering an inhibitor of insulin-regulated aminopeptidase (IRAP), thereby treating fibrosis.
    Type: Grant
    Filed: July 1, 2021
    Date of Patent: December 5, 2023
    Assignee: MONASH UNIVERSITY
    Inventors: Siew Yeen Chai, Robert Widdop, Tracey Gaspari, Huey Wen Lee
  • Patent number: 11807640
    Abstract: The substituted indolizine dicarboxylates are antibacterial agents. The emergence of drug-resistant bacteria calls for constant development of new antibacterial agents with the aim of generating medicaments that are potent against drug sensitive and resistant bacteria and are well tolerated. The present compounds are not only new, but have very valuable antimicrobial properties. These compounds showed a broad spectrum of activity against tuberculosis mycobacteria. Based on their pharmacological profiles, the present compounds may find important clinical applications for severe infectious diseases and tuberculosis.
    Type: Grant
    Filed: March 28, 2023
    Date of Patent: November 7, 2023
    Assignee: KING FAISAL UNIVERSITY
    Inventors: Katharigatta N. Venugopala, Bandar Aldhubiab, Mohamed A. Morsy, Mahesh Attimarad, Anroop B. Nair, Nagaraja Sreeharsha, Christophe Tratrat, Sandeep Chandrashekharappa, Melendran Pillay, Pran Kishore Deb, Sheena Shashikanth
  • Patent number: 11793875
    Abstract: The present invention relates to the field of carrier and delivery systems for active molecular compounds. In particular, the present invention provides aqueous dispersions for delivery of active molecular compounds.
    Type: Grant
    Filed: May 17, 2022
    Date of Patent: October 24, 2023
    Inventors: Jai Supamahitorn, Lauren McMillan
  • Patent number: 11738004
    Abstract: Provided are compositions for inhibiting a biological activity of an aldo-keto reductase family 1, member C3 (AKR1C3) polypeptide. In some embodiments, the compositions are indomethacin derivatives that are AKR1C3-specific inhibitors. Also provided are methods for producing disclosed indomethacin derivatives that substantially lack cyclooxygenase inhibitory activity but that have AKR1C3 inhibitory activity, methods for inhibiting AKR1C3 polypeptide biological activities, and methods for treating prostate tumors in subjects.
    Type: Grant
    Filed: April 21, 2021
    Date of Patent: August 29, 2023
    Assignees: Vanderbilt University, The Trustees of the University of Pennsylvania
    Inventors: Lawrence J. Marnett, Andy J. Liedtke, Trevor M. Penning, Adegoke O. Adeniji, Michael C. Byrns
  • Patent number: 11697650
    Abstract: The present invention is generally directed to inhibitors of BCL-2 proteins useful in the treatment of diseases and disorders modulated by said enzyme and having the Formula (I):
    Type: Grant
    Filed: March 11, 2022
    Date of Patent: July 11, 2023
    Assignee: Eil Therapeutics, Inc.
    Inventors: Volodymyr Kysil, Vladislav Zenonovich Parchinsky, Alexei Pushechnikov, Alexandre Vasilievich Ivachtchenko, Ruben Abagyan, Andrew Orry, Polo Chun-Hung Lam, Nikolay Savchuk
  • Patent number: 11440884
    Abstract: The present disclosure relates to compounds according to Formulae (I), (II) and (VIII), useful for treating diseases.
    Type: Grant
    Filed: August 20, 2018
    Date of Patent: September 13, 2022
    Assignee: ACADIA PHARMACEUTICALS INC.
    Inventors: Ethan S. Burstein, Roger Olsson, Karl Erik Jansson, Niklas Patrik Sköld, Larisa Yudina Wahlström, Björn Gustav Borgström, Henrik Von Wachenfeldt, Magnus Gustav Wilhelm Bergner
  • Patent number: 11331389
    Abstract: The present invention relates to the field of carrier and delivery systems for active molecular compounds. In particular, the present invention provides aqueous dispersions for delivery of active molecular compounds.
    Type: Grant
    Filed: July 14, 2020
    Date of Patent: May 17, 2022
    Assignee: Austin Research Labs Corp.
    Inventors: Jai Supamahitorn, Lauren McMillan
  • Patent number: 11078488
    Abstract: The present invention relates to compositions, methods and kits for the treatment of fibrosis. In particular, the compositions, methods and kits are particularly useful, but not limited to, the treatment of cardiac fibrosis. The invention provides a method of treating fibrosis in an individual comprising administering an inhibitor of insulin-regulated aminopeptidase (IRAP), thereby treating fibrosis.
    Type: Grant
    Filed: August 4, 2020
    Date of Patent: August 3, 2021
    Assignee: MONASH UNIVERSITY
    Inventors: Siew Yeen Chai, Robert Widdop, Tracey Gaspari, Huey Wen Lee
  • Patent number: 10858321
    Abstract: The present invention relates to a composition for inducing cell reprogramming. The indazole derivative compound contained in the composition of the present invention shows an improved biological profile and at the same time can perform efficient cell reprogramming. In addition, unlike conventional compounds (e.g. riversine or BIO) for inducing low-molecular cell reprogramming, the indazole derivative compound of the present invention does not show cytotoxicity and thus is expected to have high growth in the market of cell therapy products when clinically applied. Conventional indazole derivative compounds have never known as a use for cell reprogramming. Compared with conventional indazole derivative compounds, the compound of the present invention has a great cell reprogramming ability while having no or little cytotoxicity.
    Type: Grant
    Filed: June 30, 2015
    Date of Patent: December 8, 2020
    Assignee: GWANGJU INSTITUTE OF SCIENCE AND TECHNOLOGY
    Inventors: Yong Chul Kim, Darren R. Williams, Da Woon Jung, Jung Eun Lee, Shin Ae Seo, Ji Yeon Park
  • Patent number: 10851051
    Abstract: In one aspect, the present invention provides a method of inhibiting proliferation of a multiple myeloma cell, the method comprising contacting the cell with BRD9647, thereby inhibiting proliferation of the cell. In another aspect, the present invention provides a method of treating multiple myeloma in a pre-selected subject, the method comprising administering an effective amount of BRD9647 to the subject, wherein the subject is pre-selected by detecting a mutation in an AZIN1 polynucleotide or polypeptide relative to a reference in a biological sample obtained from the subject. In another aspect, the present invention provides a method of modulating benzoylation of an agent in a cell, the method comprising contacting the cell with BRD9647, thereby modulating benzoylation of an agent in the cell.
    Type: Grant
    Filed: August 12, 2016
    Date of Patent: December 1, 2020
    Assignees: THE BROAD INSTITUTE, INC., THE GENERAL HOSPITAL CORPORATION, PRESIDENT AND FELLOWS OF HARVARD COLLEGE
    Inventors: Shrikanta Chattopadhyay, Stuart L. Schreiber, Zarko Boskovic
  • Patent number: 10787668
    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: September 6, 2018
    Date of Patent: September 29, 2020
    Assignee: MONASH UNIVERSITY
    Inventors: Siew Yeen Chai, Robert Widdop, Tracey Gaspari, Huey Wen Lee
  • Patent number: 10729689
    Abstract: A series of novel EHop-016 derivatives is presented herein via designing and synthesizing compounds that mimics its more favorable “U-shaped” conformation that appears to be critical for inhibitory activity against Rac. Based on modeling studies on EHop-016, compounds with a more rigid structural conformation can mimic this “U-shaped” conformation would improve the anti-migration activity against metastatic cells. Compounds are disclosed that inhibit RhoGTPases that are useful for inhibiting hyperprofilerative and neoplastic diseases, for instance compounds of formula (I) Specifically, the compounds inhibit the GTPases Rac and Cdc42 that are overactive or overexpressed in signaling pathways in cancer and metastasis. Methods for treatment of cancer and hyperproliferative diseases are disclosed.
    Type: Grant
    Filed: October 23, 2018
    Date of Patent: August 4, 2020
    Assignee: UNIVERSITY OF PUERTO RICO
    Inventors: Eliud Hernandez-O'Farrill, Cornelis P. Vlaar, Suranganie Dharmawardhane Flanagan, Linette Castillo-Pichardo
  • Patent number: 10723705
    Abstract: The present disclosure relates to heterocyclic compounds, and pharmaceutical compositions of the same, that are modulators/inhibitors of HDACs, such as HDAC8 and are useful in the treatment of HDAC-associated diseases.
    Type: Grant
    Filed: August 12, 2016
    Date of Patent: July 28, 2020
    Assignee: Incyte Corporation
    Inventors: Jun Pan, Xiaozhao Wang, Joseph Barbosa, Wenqing Yao, Yingda Ye
  • Patent number: 10688103
    Abstract: Provided herein are methods, formulations and dosing regimens for treating hypersomnia in a subject. For instance, methods provided herein comprise administering a GABAA chloride channel blocker. In certain embodiments, the GABAA chloride channel blocker is pentylenetetrazol (PTZ).
    Type: Grant
    Filed: April 14, 2015
    Date of Patent: June 23, 2020
    Assignee: BALANCE THERAPEUTICS, INC.
    Inventor: Lyndon Lien
  • Patent number: 10688048
    Abstract: Symmetrically and asymmetrically branched homopolymers are modified at the surface level with functional groups that enable forming aggregates with water insoluble or poorly water soluble pharmaceutically active agents (PAA). The aggregates formed are specifically induced by interaction of PAA and homopolymer and are different from aggregates that are formed by the polymer alone in the absence of the PAA or by the PAA alone in the absence of the polymer. Such aggregates can be used to improve drug solubility, stability, delivery and efficacy.
    Type: Grant
    Filed: November 21, 2017
    Date of Patent: June 23, 2020
    Assignee: ANP Technologies, Inc.
    Inventors: Dujie Qin, Ray Yin, Jing Pan, Yubei Zhang
  • Patent number: 10370369
    Abstract: A novel acid addition salt of 3-aminoquinuclidine, which is an industrially useful compound as an intermediate of medicines and does not exhibit deliquescence, is provided. In particular, an acid addition salt of 3-aminoquinuclidine selected from the group consisting of racemic 3-aminoquinuclidine, (R)-3-aminoquinuclidine, and (S)-3-aminoquinuclidine, and acid selected from the group consisting of phosphoric acid, sulfuric acid, fumaric acid, terephthalic acid, oxalic acid, p-toluenesulfonic acid, (±)-10-camphorsulfonic acid, and (?)-10-camphorsulfonic acid, is provided.
    Type: Grant
    Filed: March 31, 2016
    Date of Patent: August 6, 2019
    Assignee: YUKI GOSEI KOGYO CO. LTD.
    Inventors: Yukiko Takeda, Tetsuji Noda
  • 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: 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: 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: 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: 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: 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