Carbocyclic Ring Bonded Directly To The Piperazine Ring Patents (Class 514/255.03)
  • Patent number: 10550090
    Abstract: The disclosure provides processes of preparing compounds of Formula (I) and Formula (IV), their salts, and intermediates thereof, wherein R1, R2, R3, and R7 are defined as set forth in the specification.
    Type: Grant
    Filed: March 17, 2017
    Date of Patent: February 4, 2020
    Assignee: Purdue Pharma L.P.
    Inventor: Laykea Tafesse
  • Patent number: 10501427
    Abstract: The present invention relates to deuterated 1-piperazino-3-phenyl-indanes and salts thereof with activity at dopamine receptors D1 and D2 as well as the 5HT2 receptors in the central nervous system, to medicaments comprising such compounds as active ingredients, to the use of such compounds in the treatment of diseases in the central nervous system, and to methods of treatment comprising administration of such compounds.
    Type: Grant
    Filed: September 28, 2018
    Date of Patent: December 10, 2019
    Assignee: H. LUNDBECK A/S
    Inventors: Morten Jorgensen, Peter Hongaard Andersen, Klaus Gjervig Jensen
  • Patent number: 10485799
    Abstract: The present invention relates to a solid oral pharmaceutical composition comprising vortioxetine hydrobromide in a matrix formed from at least one polyethylene oxide and optionally one or more further matrix forming polymers.
    Type: Grant
    Filed: December 21, 2016
    Date of Patent: November 26, 2019
    Assignee: Hexal AG
    Inventors: Andreas Krekeler, Dimitri Neumann, Michael Sedlmayr
  • Patent number: 10457642
    Abstract: Described herein is an alpha-emitting radionuclide, 211At, which has been incorporated into a selective sigma-2 ligand moiety to provide cytotoxic capabilities to a chemical compound. As described herein, a compound of formula (I), wherein R1-R4, m, and n are defined herein, was prepared and utilized in in vitro and in vivo tumor targeting of alpha-emitting sigma-2 ligand in a breast cancer model. In one embodiment, the compound is 5-(211At)—N-(4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)butyl)-2,3-dimethoxybenzamide.
    Type: Grant
    Filed: April 26, 2016
    Date of Patent: October 29, 2019
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: Daniel A. Pryma, Brian P. Lieberman, Mehran Makvandi, Robert H. Mach
  • Patent number: 10272080
    Abstract: Working memory deficits are treated and working memory is improved with a composition that comprises a therapeutically effective amount of one or more respective selective dopamine D4 receptor agonists and/or pharmaceutically acceptable analogs, salts or hydrates of the respective one or more selective dopamine D4 receptor agonists. This composition can be administered to a subject to improve the subject's working memory.
    Type: Grant
    Filed: September 12, 2014
    Date of Patent: April 30, 2019
    Assignees: Florida State University Research Foundation, Inc., The General Hospital Corporation
    Inventors: Pradeep G. Bhide, Jinmin Zhu, Joseph Biederman, Thomas J. Spencer
  • Patent number: 10071062
    Abstract: The present invention relates to method of treatment of hepatitis C using hexestrol or a derivative thereof. The methods of the present invention can be used in patients with hepatitis C administering hexestrol or a derivative thereof in combination with one or more anti-hepatitis C drugs.
    Type: Grant
    Filed: November 30, 2016
    Date of Patent: September 11, 2018
    Assignee: Cipla Limited
    Inventors: Geena Malhotra, Kalpana Joshi
  • Patent number: 9901827
    Abstract: In an aspect, a system for game play is provided, comprising a plurality of toy construction elements and a computer system. At least some of the toy construction elements include a first connector and a second connector. The computer system receives identification data relating to physical constructions made from at least two of the construction elements. For a first physical construction made from a first plurality of toy construction elements, the system generates a virtual representation of a first character, and generates a first set of properties for the virtual representation of the first character. For a second physical construction made from a second, larger, plurality of toy construction elements, the system generates a virtual representation of a second character based, and generates a second set of properties for the virtual representation of the second character. The system receives commands to operate the generated virtual representation in a virtual environment.
    Type: Grant
    Filed: January 6, 2016
    Date of Patent: February 27, 2018
    Assignee: SPIN MASTER LTD.
    Inventor: Timothy Robert May
  • Patent number: 9889102
    Abstract: The present invention includes compounds useful in preventing, treating or ameliorating Sigma-related disorders or diseases. The compounds of the invention may modulate cellular protein homeostasis, which includes: translation initiation, folding, processing, transport, and degradation (including ubiquitin selective autophagy) of proteins. The present invention also includes methods of preventing, treating or ameliorating a Sigma-related disorder or disease in a subject in need thereof, the method comprising administering to the subject an effective amount of a Sigma-modulating compound. The present invention also includes methods of preventing, treating or ameliorating a Sigma-related disorder or disease in a subject in need thereof, the method comprising administering to the subject an effective amount of a Sigma-modulating compound, further comprising administering an effective amount of a compound that inhibits the ubiquitin proteasome system (UPS) and/or autophagic survival pathways.
    Type: Grant
    Filed: June 8, 2016
    Date of Patent: February 13, 2018
    Assignee: Drexel University
    Inventors: Felix J. Kim, Joseph M. Salvino
  • Patent number: 9884841
    Abstract: This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having benzoic acid structure which function as inhibitors of Mcl-1 protein, and their use as therapeutics for the treatment of cancer and other diseases.
    Type: Grant
    Filed: April 20, 2016
    Date of Patent: February 6, 2018
    Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Zaneta Nikolovska-Coleska, Jeanne A. Stuckey, Ahmed Mady, Lei Miao
  • Patent number: 9796676
    Abstract: The present specification discloses honeybee repellents exhibiting repellent properties similar to 2-heptanone, compositions comprising such repellents, uses to repel a honeybee from a mammal, location, plant, structure treated of such repellents, and methods of treating a mammal, location, plant, structure by applying such repellents.
    Type: Grant
    Filed: May 16, 2016
    Date of Patent: October 24, 2017
    Assignee: Inscent, Inc.
    Inventors: Daniel F. Woods, Spiros Dimitratos, Robin W. Justice
  • Patent number: 9763901
    Abstract: The present invention relates to method of treatment of hepatitis C using bufexamac or a derivative thereof. The methods of the present invention can be used in patients with hepatitis C administering bufexamac or a derivative thereof in combination with one or more anti-hepatitis C drugs.
    Type: Grant
    Filed: December 6, 2016
    Date of Patent: September 19, 2017
    Assignee: Cipla Limited
    Inventors: Geena Malhotra, Kalpana Joshi
  • Patent number: 9763957
    Abstract: The present invention relates to novel compounds that are autotaxin inhibitors, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in diseases and disorders mediated by autotaxin.
    Type: Grant
    Filed: July 16, 2014
    Date of Patent: September 19, 2017
    Assignee: Novartis AG
    Inventors: David Beattie, Urs Baettig, Darren Mark Legrand, Andrew Stuart Lister, Jeffrey McKenna, David William Pearce, David Andrew Sandham, Oliver Ross Steward, Christopher Thomson
  • Patent number: 9649332
    Abstract: The present invention provides a composition comprising a polymer of a ?-hydroxy short-medium chain fatty acid, which is used for delivering the ?-hydroxy short-medium chain fatty acid or an oligomer thereof to the large intestine. In case the composition is administrated orally, the composition will be delivered to the large intestine, without being degraded in the stomach or short intestine, and degraded by the large intestinal bacterial flora and release the short-medium chain fatty acid or an oligomer thereof. The released short-medium chain fatty acid or an oligomer thereof has useful physiological activities and is effective for treating or preventing inflammatory diseases or cancer in the large intestine.
    Type: Grant
    Filed: November 12, 2009
    Date of Patent: May 16, 2017
    Assignee: EARTHUS, INC.
    Inventors: Kazunari Ushida, Masaki Kuriyama
  • Patent number: 9572820
    Abstract: The invention provides methods of treating autophagy mediated diseases and disorders and related pharmaceutical compositions, diagnostics, screening techniques and kits. In one embodiment, the invention provides a method of determining whether a subject suffers from, or is at risk of developing, and autophagy mediated disease state and/or condition by evaluating LC3 levels.
    Type: Grant
    Filed: May 10, 2012
    Date of Patent: February 21, 2017
    Assignee: STC.UNM
    Inventors: Vojo Deretic, Eliseo Castillo, Steven Bradfute, Larry A. Sklar
  • Patent number: 9357781
    Abstract: The present specification discloses honeybee repellents exhibiting repellent properties similar to 2-heptanone, compositions comprising such repellents, uses to repel a honeybee from a mammal, location, plant, structure treated of such repellents, and methods of treating a mammal, location, plant, structure by applying such repellents.
    Type: Grant
    Filed: May 3, 2014
    Date of Patent: June 7, 2016
    Assignee: Inscent, Inc.
    Inventors: Daniel F. Woods, Spiros Dimitratos, Robin W. Justice
  • Patent number: 9150560
    Abstract: This invention comprises the novel compounds of formula (I) wherein n, R1, R2, R3, R4, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
    Type: Grant
    Filed: February 21, 2014
    Date of Patent: October 6, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Kristof Van Emelen, Marc Gustaaf Celine Verdonck, Sven Franciscus Anna Van Brandt, Patrick Rene Angibaud, Lieven Meerpoel, Alexey Borisovich Dyatkin
  • Patent number: 9120810
    Abstract: The invention relates to compounds of Formula I or a pharmaceutically acceptable salt, ester or prodrug thereof:
    Type: Grant
    Filed: September 26, 2013
    Date of Patent: September 1, 2015
    Assignees: THE BOARD INSTITUTE, INC., PRESIDENT & FELLOWS OF HARVARD COLLEGE
    Inventors: Mahmud Hussain, Daisuke Ito, Jason Law, Matthias Leiendecker, Ke Liu, Benito Munoz, Stuart Schreiber, Alykhan Shamji, Andrew Stern
  • Patent number: 9095588
    Abstract: This disclosure relates to a process for the preparation of 1-[2-(2,4-dimethylphenylsulfanyl)-phenyl]piperazine or a salt thereof. The process includes reacting compound II with compound III and compound IV in the presence of a solvent, a base and a palladium catalyst. R, R?, X1, and X2 in the formulas above are defined in the Specification.
    Type: Grant
    Filed: August 29, 2014
    Date of Patent: August 4, 2015
    Assignee: H. Lundbeck A/S
    Inventors: Andre Faldt, Lone Munch Ringgaard, Michael J. Mealy, Michael Harold Rock, Jorgen Brodersen, Morten Jorgensen
  • Patent number: 9090575
    Abstract: The invention provides compounds represented by the general formula I wherein the substituents are defined in the application. The compounds are useful in the treatment of an affective disorder, including depression, anxiety disorders including general anxiety disorder and panic disorder and obsessive compulsive disorder.
    Type: Grant
    Filed: June 26, 2013
    Date of Patent: July 28, 2015
    Assignee: H. Lundbeck A/S
    Inventors: Thomas Ruhland, Garrick P. Smith, Benny Bang-Andersen, Ask Puschl, Ejner K. Moltzen, Kim Andersen
  • Patent number: 9056846
    Abstract: The present invention relates to stable and bioavailable immediate release formulations comprising dopamine receptor ligands. Methods of treating various disorders by administering the formulations are also described.
    Type: Grant
    Filed: October 17, 2012
    Date of Patent: June 16, 2015
    Assignee: Richter Gedeon Nyrt.
    Inventors: Ranajoy Sarkar, Mahendra G. Dedhiya, Anil Chhettry
  • Patent number: 9056845
    Abstract: The present invention relates to stable and bioavailable immediate release formulations comprising dopamine receptor ligands. Methods of treating various disorders by administering the formulations are also described.
    Type: Grant
    Filed: July 16, 2009
    Date of Patent: June 16, 2015
    Assignee: Richter Gedeon Nyrt.
    Inventors: Ranajoy Sarkar, Mahendra G. Dedhiya, Anil Chhettry
  • Publication number: 20150141437
    Abstract: The use of compounds of formula wherein R2, R3, R4, R5, R6 and R7 have several meanings, for the treatment of disorders mediated by protozoan organisms, novel compounds of the above formula and intermediates for the preparation of such compounds, pharmaceutical compositions comprising such novel compounds, a method of treating disorders mediated by protozoan organisms comprising administering such compounds, optionally together with a second drug substance, to a subject in need thereof and the use of such compounds, whenever comprising a photoaffinity label, for the identification of the molecular target(s) of arylamino alcohol antimalarials.
    Type: Application
    Filed: June 10, 2013
    Publication date: May 21, 2015
    Inventors: Hubert Gstach, Peter Chiba, Matthias Mastalir
  • Publication number: 20150141397
    Abstract: Aniline compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.
    Type: Application
    Filed: August 5, 2014
    Publication date: May 21, 2015
    Inventors: Trevor T. Charvat, Junfa Fan, Christopher W. Lange, Manmohan Reddy Leleti, Yandong Li, Venkat Reddy Mali, Jeffrey P. McMahon, Jay Powers, Sreenivas Punna, Ju Yang
  • Patent number: 9029379
    Abstract: Methods for treating Down syndrome and improving cognitive function of a patient with an intellectual disability are disclosed. 5-hydroxytryptamine sub-receptor six (5-HT6) receptor antagonists are provided for improving the cognition of a Down syndrome patient.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: May 12, 2015
    Assignee: The University of Utah Research Foundation
    Inventors: Julie Ruth Korenberg, Karen Sue Wilcox, Peter Jeffrey West, Raymond Pierre Kesner
  • Publication number: 20150110873
    Abstract: The present invention relates to an enteric tablet with improved bioavailability, which is rapidly disintegrated after reaching the intestine to allow dissolution of the active ingredient, and which characteristically reduces the amount of talc to be used and is free of an alkali component.
    Type: Application
    Filed: December 26, 2014
    Publication date: April 23, 2015
    Inventors: Masafumi MISAKI, Yuki TSUSHIMA, Masahiro NIWA
  • Patent number: 9012460
    Abstract: The invention relates to compounds of formula I: where a, and R1 through R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: June 5, 2014
    Date of Patent: April 21, 2015
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Eric L. Stangeland, Lori Jean Patterson
  • Publication number: 20150105399
    Abstract: Disclosed in the present invention is a 3-cyanoanilinoalkylarylpiperazine derivatives and use thereof in preparing drugs; the 3-cyanoanilinoalkylarylpiperazine derivatives disclosed by the present invention has very useful pharmaceutical properties and good tolerance, especially the use as novel analgesic drugs, novel antidepressants, and novel analgesic and antidepressive drugs. This class of compounds are central analgesics regulating 5-hydroxytrptamine, and also are novel antidepressants regulating 5-hydroxytrptamine. This class of compounds also has less toxic and side effects and a higher safety range.
    Type: Application
    Filed: April 9, 2013
    Publication date: April 16, 2015
    Inventors: Jianqi Li, Guan Wang, Guisen Zhang, Yali Li, Xiangqing Xu, Xiaowen Chen, Shicheng Liu, Song Zhao, Minquan Yu
  • Publication number: 20150094316
    Abstract: Liquid formulations of lactic acid addition salts of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine are provided
    Type: Application
    Filed: December 11, 2014
    Publication date: April 2, 2015
    Inventors: Svend Treppendahl, Heidi Lopez De Diego
  • Publication number: 20150080400
    Abstract: The compounds of formula (1) in which R1, R4, A and X have the meanings as given in the description, are novel effective EP2 agonists.
    Type: Application
    Filed: April 30, 2013
    Publication date: March 19, 2015
    Applicant: TAKEDA GMBH
    Inventors: Angelika Hoffmeyer, Rainer Boer, Manuela Hessmann, Andreas Pahl, Torsten Dunkern, Simone Hartung, Christof Zitt, Jurgen Volz, Christiane Praechter, Mahindra Makhija, Hiteshkumar Jain, Sandip Gavade, Arati Prabhu, Manojkumar Tiwari, Ashish Keche, Sarvesh Patel
  • Publication number: 20150072995
    Abstract: A composition comprising a selective oxytocin antagonist for use in the treatment and/or prevention of a male ejaculatory disorder; which selective oxytocin antagonist is optionally admixed with a pharmaceutically acceptable carrier, diluent or excipient.
    Type: Application
    Filed: September 24, 2014
    Publication date: March 12, 2015
    Applicant: Ixchelsis Limited
    Inventors: Alasdair Mark Naylor, Rachel Jane Russell, Stephen Derek Albert Street, Kim-Wah Tang, Pieter Hadewijn Van Der Graaf, Christopher Peter Wayman
  • Publication number: 20150072980
    Abstract: The present invention is directed to compounds, their synthesis, and their use as antagonists, inverse agonists, modulators and or inhibitors of the Retinoic acid-related orphan nuclear receptor ?t (ROR?t)/ROR?. The compounds of the present invention are useful for modulating ROR?t)/ROR? activity and for treating diseases or conditions mediated by ROR?t)/ROR? such as for example, disease states associated with immunopathology of human autoimmune diseases such as Multiple Sclerosis (MS), Rheumatoid Arthritis (RA), Inflammatory Colitis, Psoriasis, COPD, Pain, Obesity, Diabetes, Dyslipidemia, Osteoporosis, Asthma, Neurodegenerative diseases and Cancer.
    Type: Application
    Filed: August 27, 2014
    Publication date: March 12, 2015
    Inventors: Hariprasad Vankayalapati, Venkatakrishnareddy Yerramreddy
  • Patent number: 8969355
    Abstract: This disclosure relates to a method of treating a disease selected from the group consisting of affective disorders, depression, major depressive disorder, anxiety, general anxiety disorder, social anxiety disorder, obsessive compulsive disorder, panic disorder, and panic attacks. The method includes administering a therapeutically effective amount of Compound I or a pharmaceutically acceptable salt thereof to a patient in need thereof, in which Compound I is 1-[2-(2,4-dimethylphenylsulfanyl)-phenyl]piperazine.
    Type: Grant
    Filed: September 9, 2014
    Date of Patent: March 3, 2015
    Assignee: H. Lundbeck A/S
    Inventors: Benny Bang-Andersen, Andre Faldt, Rene Holm, Heidi Lopez de Diego
  • Publication number: 20150038515
    Abstract: Pharmaceutical compositions of the invention comprise covalently closed circular DNA formation inhibitors having a disease-modifying action in the treatment of diseases associated with the formation of covalently closed circular DNA that include hepatitis B infection, and any disease involving formation of covalently closed circular DNA.
    Type: Application
    Filed: February 28, 2013
    Publication date: February 5, 2015
    Inventors: Andrea Cuconati, Haitao Guo, Timothy M. Block, Ju-Tao Guo, Xiaodong Xu, Huagang Lu, Dawei Cai
  • Patent number: 8946228
    Abstract: The invention relates to a DGAT inhibitor of formula (I), including any stereochemically isomeric form thereof, a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof, and methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine, as a DGAT inhibitor, of said compounds.
    Type: Grant
    Filed: June 6, 2008
    Date of Patent: February 3, 2015
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jean-Pierre André Marc Bongartz, Joannes Theodorus Maria Linders, Lieven Meerpoel, Guy Rosalia Eugeen Van Lommen, Erwin Coesemans, Mirielle Braeken, Christophe Francis Robert Nestor Buyck, Monique Jenny Marie Berwaer, Katharina Antonia Germania J. M. De Waepenaert, Peter Walter Maria Roevens, Petr Vladimirivich Davidenko
  • Patent number: 8940746
    Abstract: Liquid formulations of lactic acid addition salts of 1-[2-(2,4-dimethylphenylsulfanyl)-phenyl]piper-azine are provided.
    Type: Grant
    Filed: April 16, 2010
    Date of Patent: January 27, 2015
    Assignee: H. Lundbeck A/S
    Inventors: Svend Treppendahl, Heidi Lopez De Diego
  • Publication number: 20150018371
    Abstract: Positive allosteric modulators of melanocortin receptors, especially allosteric potentiators of the receptors MC3R and MC4R are described herein. Also provided are pharmaceutical compositions containing the positive allosteric modulators and methods of treating obesity or an obesity-related disorder such as type 2 diabetes, comprising administering an effective amount of the positive allosteric modulator.
    Type: Application
    Filed: March 6, 2013
    Publication date: January 15, 2015
    Inventors: Roger D. Cone, Julien A. Sebag, Jacques Pantel, Savannah Y. Williams, David C. Weaver, Gary A. Sulikowski, Craig W. Lindsley, Padma S. Portonova, Chao Zhang
  • Publication number: 20150011566
    Abstract: The present invention provides N-phenylpiperazine derivatives for use as multiple binders and/or antagonists of ?1A adrenoceptors, ?1D adrenoceptors and 5-HT1A serotonin receptors. These substances are candidates to prototypes for the treatment of benign prostate hyperplasia and lower urinary tract symptoms, and are useful in pharmaceutical compositions.
    Type: Application
    Filed: January 4, 2013
    Publication date: January 8, 2015
    Inventors: Claudia Lucia Martins Da Silva, Fernanda Chagas Da Silva, Luana Chaves Barberato, Luciana De Camargo Nascente, Jessica Barbosa Do Nascimento Viana, Renata Oliveira Silva, Laís Flávia Nunes Lemes, François German Noël, Luís Antônio Soares Romeiro
  • Patent number: 8927546
    Abstract: The invention includes a compound of formula I: wherein R1, Y, A, n, R4 and Z have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of PDE4 function and are useful for improving cognitive function and/or treating cognitive disorders or impairment, traumatic and/or ischemic injuries of the central and peripheral nervous system and/or psychiatric disorders in animals, especially humans.
    Type: Grant
    Filed: September 22, 2010
    Date of Patent: January 6, 2015
    Assignee: Dart Neuroscience (Cayman) Ltd.
    Inventors: Alan P. Kaplan, Terence P. Keenan, Michael I. Weinhouse, Mark E. Wilson, Andrew K. Lindstrom, William C. Ripka, Mi Chen
  • Patent number: 8927553
    Abstract: The present invention is concerned with deuterium-enriched sulfonamides of formula 1, their pharmaceutically acceptable salts and methods of use thereof for the treatment of anxiety disorders including, General Anxiety Disorder (GAD), Panic Disorder (PD), Post-Traumatic Stress Disorder (PTSD), Social Phobia (SP), Health Anxiety (Hypochondriasis), depression, major depressive disorders, unipolar depression, bipolar I depression disorder, bipolar II depression disorder, treatment-resistant depression, single episodic and recurrent major depressive disorders, depression in the medically ill, attention deficit hyperactivity disorder (ADHD), attention deficit disorder (ADD), Obsessive-Compulsive Disorder (OCD), Obsessive-Compulsive Personality Disorder (OCPD), Autism Spectrum Disorder (ASD), schizophrenia, psychosis, epilepsy, seizures, hot flashes due to menopause, age-related macular degeneration (AMD), premature ejaculation, male erectile dysfunction, sexual dysfunction, obesity, eating disorders, bulimia nervo
    Type: Grant
    Filed: July 30, 2013
    Date of Patent: January 6, 2015
    Inventor: Daljit Singh Dhanoa
  • Publication number: 20150005318
    Abstract: This disclosure relates to a method of treating a disease selected from the group consisting of Alzheimer's disease, cognitive impairment, and attention deficit hyperactivity disorder (ADHD). The method includes administering a therapeutically effective amount of Compound I or a pharmaceutically acceptable salt thereof to patient in need thereof, in which Compound I is 1-[2-(2,4-dimethylphenylsulfanyl)-phenyl]piperazine.
    Type: Application
    Filed: September 9, 2014
    Publication date: January 1, 2015
    Inventors: Benny Bang-Andersen, Arne Mork, Nicholas Moore, Tine Bryan Stensbol
  • Publication number: 20150005317
    Abstract: Some embodiments are based on the discovery that proliferative diseases (e.g., neoplastic diseases, for example, tumors or cancers) having an FBW7 mutation or other FBW7 deficiency are sensitive to Mcl1 inhibiting agents, but resistant to pro-apoptotic drugs that do not inhibit Mcl1. Some embodiments provide methods of treating a proliferative disease based on an assessment of FBW7 expression level or mutation status. Some embodiments provide methods of classifying a hyperproliferative cell or cell population, for example, a malignant cell or cell population based on an assessment of FBW7 expression level or mutation status. Some embodiments provide methods of selecting a treatment regimen for treating a proliferative disease, for example, a malignant disorder, based on an assessment of FBW7 expression level or mutation status.
    Type: Application
    Filed: March 2, 2012
    Publication date: January 1, 2015
    Applicant: Beth Israel Deaconess Medical Center, Inc.
    Inventor: Wenyi Wei
  • Publication number: 20140378460
    Abstract: This invention relates to the use sigma-2 receptor antagonists, and of pharmaceutical compositions comprising such compounds, in methods for inhibiting Abeta-associated synapse loss or synaptic dysfunction in neuronal cells, modulating an Abeta-associated membrane trafficking change in neuronal cells, and treating cognitive decline associated with Abeta pathology and more broadly treating with such compounds and compositions neurodegenerative diseases and disorders associated with Abeta pathology. This invention also relates to methods for screening compounds for activity in inhibiting cognitive decline on the basis of their ability to bind to a sigma-2 receptor.
    Type: Application
    Filed: August 27, 2012
    Publication date: December 25, 2014
    Applicant: COGNITION THERAPEUTICS, INC.
    Inventors: Susan M. Catalano, Gilbert Rishton, Nicholas J. Izzo
  • Publication number: 20140378473
    Abstract: This invention relates to novel diarylamino compounds that bind to the sigma-2 receptor, to pharmaceutical compositions comprising such compounds, and to methods for inhibiting or restoring synapse loss in neuronal cells, modulating a membrane trafficking change in neuronal cells, and treating cognitive decline and neurodegenerative diseases and disorders therewith.
    Type: Application
    Filed: August 27, 2012
    Publication date: December 25, 2014
    Applicant: COGNITION THERAPEUTICS, INC.
    Inventors: Susan M. Catalano, Gilbert Rishton, Nicholas J. Izzo
  • Publication number: 20140377363
    Abstract: This disclosure relates to a method of treating a disease selected from the group consisting of affective disorders, depression, major depressive disorder, anxiety, general anxiety disorder, social anxiety disorder, obsessive compulsive disorder, panic disorder, and panic attacks. The method includes administering a therapeutically effective amount of Compound I or a pharmaceutically acceptable salt thereof to a patient in need thereof, in which Compound I is 1-[2-(2,4-dimethylphenylsulfanyl)-phenyl]piperazine.
    Type: Application
    Filed: September 9, 2014
    Publication date: December 25, 2014
    Inventors: Benny Bang-Andersen, Arne Mork, Nicholas Moore, Tine Bryan Stensbol
  • Patent number: 8912196
    Abstract: Novel piperazine, piperidine and tetrahydropyridine derivatives comprising a dibenzofurane moiety are provided herein, as well as pharmaceutical compositions comprising same and therapeutic uses thereof.
    Type: Grant
    Filed: May 26, 2010
    Date of Patent: December 16, 2014
    Assignee: ATIR Holding S.A.
    Inventors: Vladimir Kogan, Lev Tabachnik
  • Patent number: 8912197
    Abstract: The present invention relates to novel crystalline forms of carbamoyl-cyclohexane derivatives and, more particularly, to novel co-crystalline forms of trans-1{4-[2-[4-(2,3-dichlorophenyl-piperazin-1-yl]-ethyl]-cyclohexyl}-3,3-dimethyl urea hydrochloride and an acid such as fumaric acid. Processes for preparing these forms, compositions containing these forms, and methods of use thereof are also described.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: December 16, 2014
    Inventors: Xiangmin Liao, Hiajian (Jim) Zhu, Andreas Grill
  • Publication number: 20140364441
    Abstract: Novel [1,2,4]triazolo[1,5-a]pyridinyl-6-yl-substituted tetrahydroisoquinolines are described in the present invention. These compounds and crystalline forms SA1 and N-2 are used in the treatment of various neurological and physiological disorders. Methods of making these compounds and crystalline forms SA-1 and N-2 are also described in the present invention.
    Type: Application
    Filed: August 22, 2014
    Publication date: December 11, 2014
    Inventors: Chenkou Wei, Victor W. Rosso, Qi Gao
  • Patent number: 8901116
    Abstract: There is provided a novel carbamoyloxy arylalkanoyl arylpiperazine derivative compound having abundant racemic or enantiomeric characteristics, represented by the Formula 1, and pharmaceutically available salts or hydrates thereof. Also, there are provided a pharmaceutical composition for treating pain, anxiety or depression including an effective amount of the compound, and a method for treating pain, anxiety or depression in mammals by administering an effective amount of the compound to the mammals in need of treatment thereof.
    Type: Grant
    Filed: September 16, 2013
    Date of Patent: December 2, 2014
    Assignee: SK Biopharmaceuticals Co., Ltd.
    Inventors: Byong Sung Kwak, Hong Sik Moon, Han-Ju Yi, Young Soon Kang, Dae Joong Im, Eun Hee Chae, Sang Mi Chae, Ki Ho Lee
  • Publication number: 20140336185
    Abstract: Compounds that bind the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, methods of their therapeutic and/or prophylactic use, and methods of their use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor are provided. Certain compounds may have activity as modulators or potentiators with respect to glucagon receptor, GIP receptor, GLP-1 and GLP-2 receptors, and PTH receptor on their own or in the presence of receptor ligands such as GIP (1-42), PTH (1-34), Glucagon (1-29), GLP-2 (1-33), GLP-1 (7-36), GLP-1 (9-36), oxyntomodulin and exendin variants.
    Type: Application
    Filed: May 31, 2012
    Publication date: November 13, 2014
    Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Junko Tamiya, Liming Huang, Thomas Fowler, Andrew Novak, Premji Meghani, Enugurthi Brahmachary, Adam Richard Yeager
  • Patent number: 8883796
    Abstract: Provided are biphenyl derivatives exhibiting activity towards central nervous system diseases by acting on the 5-HT7 receptor, pharmaceutically acceptable salts thereof, a method for preparing the compounds and pharmaceutical compositions including the compounds as an active ingredient.
    Type: Grant
    Filed: February 8, 2013
    Date of Patent: November 11, 2014
    Assignee: Korea Institute of Science and Technology
    Inventors: Hyunah Choo, Young-Jae Kim, Jeeyeon Kim, Mi Young Yeom