Patents Examined by Brenda Coleman
  • Methods and compositions for preparing noribogaine from voacangine
    Patent number: 8859764
    Abstract: Disclosed are methods and compositions for preparing and purifying the non-addictive alkaloid noribogaine.
    Type: Grant
    Filed: January 23, 2012
    Date of Patent: October 14, 2014
    Assignee: DemeRx, Inc.
    Inventors: Deborah C. Mash, Robert M. Moriarty, Richard D. Gless, Jr.
  • Agents for treating disorders involving modulation of ryanodine receptors
    Patent number: 8853198
    Abstract: The present invention relates to 1,4-benzothiazepine derivatives and their use to treat conditions, disorders and diseases associated with ryanodine receptors (RyRs) that regulate calcium channel functioning in cells. The invention also discloses pharmaceutical compositions comprising the compounds and uses thereof to treat diseases and conditions associated with RyRs, in particular cardiac, musculoskeletal and central nervous system (CNS) disorders.
    Type: Grant
    Filed: November 11, 2013
    Date of Patent: October 7, 2014
    Assignees: Les Laboratoires Servier, ARMGO Pharma, Inc.
    Inventors: Jiaming Yan, Sandro Belvedere, Yael Webb, Marc Bertrand, Nicole Villeneuve
  • Sulfate esters of noribogaine
    Patent number: 8853201
    Abstract: Disclosed herein are sulfate esters of noribogaine or 9,17 dihydronoribogaine, and pharmaceutically acceptable salts of each thereof, pharmaceutical compositions comprising such compounds, and methods of their use, including in treating addiction and/or pain.
    Type: Grant
    Filed: December 7, 2012
    Date of Patent: October 7, 2014
    Assignee: DemeRx, Inc.
    Inventors: Richard D. Gless, Jr., Robert M. Moriarty
  • Sterol derivatives and their synthesis and use
    Patent number: 8853194
    Abstract: Sterol derivatives with structural formula I or II are disclosed, wherein R is defined as the description of the invention. Their synthesizing methods and anti-tumor use are also disclosed. Especially, the compound of formula I, in which R is O (i.e. the compound CL 168-6), has the anti-tumor therapeutic index of 49.3. The compound can be used to prepare a medicine for prevention or treatment of immunological diseases and cancers such as liver cancer and lung cancer.
    Type: Grant
    Filed: January 15, 2010
    Date of Patent: October 7, 2014
    Inventors: Dagang Chen, Haimin Lei
  • HIV integrase inhibitors
    Patent number: 8846659
    Abstract: The disclosure generally relates to the novel compounds of formula I, including their salts, which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.
    Type: Grant
    Filed: December 7, 2011
    Date of Patent: September 30, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Kevin Peese, B. Narasimhulu Naidu, Manoj Patel, Chen Li, Michael A. Walker
  • Compound having neurite-outgrowing activity
    Patent number: 8841284
    Abstract: There is provided a novel compound having neurite-outgrowing activity that is useful for the prevention or the treatment of a neurodegenerative disease. A compound of Formula (I) [where X is OR or NR1R2, Y is OH, NR3R4, —NHC(?NH)NHR5, or —NHC(?NH)R5, and Z is a hydrogen atom, a linear or branched C1-5 alkyl group, or a 5- or 6-membered ring aryl group optionally having 1 or 2 nitrogen atom(s), sulfur atom(s), or oxygen atom(s)], or a pharmaceutically or veterinary-medically acceptable salt of the compound.
    Type: Grant
    Filed: July 21, 2009
    Date of Patent: September 23, 2014
    Assignee: Lead Chemical Co., Ltd
    Inventors: Hideo Nemoto, Yuji Matsuya
  • Methods for the preparation of drospirenone and intermediates thereof
    Patent number: 8841283
    Abstract: The invention relates to a process for the preparation of Drospirenone in high yields and purity starting from a compound of formula 2 wherein R is a hydroxyl protective group as defined in the claims, through a sequence of oxidation, deprotection, lactonization and water elimination steps, and wherein the steps of oxidation and lactonization are performed with 1,3,5-trichloro1,3,5-triazine-2,4,6-(1H,3H,5H)-trione (trichloroisocyanuric acid, TCCA) or 1,3-dichloro-1,3,5-triazine-2,4,6-(1H,3H,5H)-trione (dichloroisocyanuric acid, DCCA) or an alkaline metal salt thereof such as the sodium salt dihydrate (DCCA sodium salt) or 1-hydroxy-1,2-benziodoxol-3(1H)-one 1-oxide (IBX). New synthetic intermediates useful for the synthesis of Drospirenone are disclosed, too.
    Type: Grant
    Filed: July 22, 2011
    Date of Patent: September 23, 2014
    Assignee: Newchem S.p.A.
    Inventors: Mauro Montorsi, Edoardo Mariani, Luca Gambarin, Gianmauro Orru′, Romeo Scalaprice, Massimo Merlo, Erika Andriolo
  • Process for preparing fluticasone propionate/furoate
    Patent number: 8841442
    Abstract: The present invention relates to an improved process for the preparation of substituted Fluticasone derivatives. The invention also reveals the processes for the purification of Fluticasones and related intermediates to provide the highly pure product.
    Type: Grant
    Filed: September 2, 2011
    Date of Patent: September 23, 2014
    Assignee: Cadila Healthcare Limited
    Inventors: Kirtipalsinh Solanki, Ruchir Z Bavadia, Dhaval P Patel, Dhaval J Patel, Tejash C Shah, Manoj Kumar Singh
  • Selective agents for pain suppression
    Patent number: 8835424
    Abstract: In preferred embodiments, the present invention provides methods of treatment and pharmaceutical compositions for the suppression, alleviation and prevention of the often chronic, severe and debilitating pain that can accompany inflammatory diseases and neuropathic insults, pain that is often unresponsive to conventional analgesic treatment. The preferred embodiments of the present invention further relate to methods of treatment and pharmaceutical compositions using benzodiazepine derivatives that provide suppression, alleviation and prevention of neuropathic pain, migraine-related pain and inflammatory pain with reduced sedative and ataxic side effects.
    Type: Grant
    Filed: May 13, 2010
    Date of Patent: September 16, 2014
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: James Cook, Shengming Huang, Rahul Edwankar, Ojas A. Namjoshi, Zhi-Jian Wang
  • Substituted imidazoheterocycle derivatives
    Patent number: 8835422
    Abstract: The present invention provides substituted imidazoheterocycles having the general structure of formula I: wherein Y is chosen from —O—, —OCRgRh—, —CRgRhO—, —CRgRh—, —(CRgRh)2—, —NRi—, —CRgRhNRi— and —NRiCRgRh—. Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis and treatment of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.
    Type: Grant
    Filed: December 1, 2009
    Date of Patent: September 16, 2014
    Assignee: Cara Therapeutics, Inc.
    Inventors: Stephen J. O'Connor, Jason S. Newcom, Janet L. Ralbovsky, Gary R. Gustafson, R. Paul Beckett, Robert Zhiyong Luo
  • Benzimidazole linked pyrrolo[2,1-c[1,4] benzodiazepine hybrids as potential antitumour agents and process for the preparation thereof
    Patent number: 8835421
    Abstract: The present invention provides a compounds of general formula (8), (11) and (14), useful as potential antitumour agents against human cancer cell lines. The present invention further provides a process for the preparation of pyrrolo[2,1-c][1,4]benzodiazepine hybrids of general formula (8), (11) and (14).
    Type: Grant
    Filed: October 31, 2008
    Date of Patent: September 16, 2014
    Assignee: Council of Scientific and Industrial Research
    Inventors: Ahmen Kamal, Pogula Praveen Kumar, Bobburi Naga Seshadri, Kokkonda Sreekanth
  • Psychotropic agents having glutamate NMDA activity
    Patent number: 8828993
    Abstract: The invention provides novel compounds and pharmaceutical compositions for the treatment of psychological and/or psychiatric diseases or disorders.
    Type: Grant
    Filed: January 24, 2013
    Date of Patent: September 9, 2014
    Assignee: Ramot at Tel-Aviv University Ltd.
    Inventors: Moshe Portnoy, Irit Gil-Ad, Avraham Weizman
  • Oxy-cyclohexyl-4H,6H-5-oxa-2,3,10b-triaza-benzo[E]azulenes as V1A antagonists
    Patent number: 8828989
    Abstract: The present invention provides 4H,6H-5-oxa-2,3,10b-triaza-benzo[e]azulenes of the formula wherein R1 and R2 are as defined herein and which act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments.
    Type: Grant
    Filed: August 23, 2012
    Date of Patent: September 9, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Cosimo Dolente, Patrick Schnider
  • Gamma secretase modulators
    Patent number: 8809318
    Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more disease associated with the central nervous system using such compounds or pharmaceutical compostions.
    Type: Grant
    Filed: November 11, 2009
    Date of Patent: August 19, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Zhaoning Zhu, William J. Greenlee, Hongmei Li, Monica L. Vicarel, Jun Qin, Pawan Kumar Dhondi, Xianhai Huang, Anandan Palani, Xiaoxiang Liu, Zhong-Yue Sun, Hubert B. Josien, Ruo Xu, David James Cole, Duane A. Burnett, Chad E. Bennett, Troy McCracken, Malcolm MacCoss
  • Processes for the preparation of 8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine and intermediates related thereto
    Patent number: 8802845
    Abstract: The present invention provides processes, methods and intermediates for the preparation of 8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine, salts, hydrates and crystal forms thereof which are useful as serotonin (5-HT) receptor agonists for the treatment of, for example, central nervous system disorders such as obesity.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: August 12, 2014
    Assignee: Arena Phamaceuticals, Inc.
    Inventors: Ulrich Weigl, Frank Porstmann, Christoph Straessler, Lars Ulmer, Ulf Koetz
  • Bromodomain inhibitors and uses thereof
    Patent number: 8796261
    Abstract: The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.
    Type: Grant
    Filed: December 2, 2011
    Date of Patent: August 5, 2014
    Assignee: Constellation Pharmaceuticals, Inc.
    Inventors: Brian K. Albrecht, James E. Audia, Alexandre Côté, Victor S. Gehling, Jean-Christophe Harmange, Michael C. Hewitt, Yves Leblanc, Christopher G. Nasveschuk, Alexander M. Taylor, Rishi G. Vaswani
  • Imidazobenzazepine CGRP receptor antagonists
    Patent number: 8796260
    Abstract: Compounds of Formula I: I (where variables R1A, R1B, R2, R3, R4, A, and Z are as defined herein) useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP receptors are involved.
    Type: Grant
    Filed: February 6, 2009
    Date of Patent: August 5, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Howard G. Selnick, Ian M. Bell
  • Aryl- and heteroaryl-substituted tetrahydrobenzazepines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin
    Patent number: 8791101
    Abstract: The compounds of the present invention are represented by the following aryl- and heteroaryl-substituted tetrahydrobenzazepine and dihydrobenzazapine derivatives having formulae I(A-E) and formula (II): where the carbon atom designated * is in the R or S configuration, and the substituents X and R1-R9 are as defined herein.
    Type: Grant
    Filed: November 1, 2010
    Date of Patent: July 29, 2014
    Assignees: Albany Molecular Research, Inc., Bristol-Myers Squibb Company
    Inventors: Bruce F. Molino, Shuang Liu, Aruna Sambandam, Peter R. Guzzo, Min Hu, Congxiang Zha, Kassoum Nacro, David D. Manning, Matthew L. Isherwood, Kristen N. Fleming, Wenge Cui, Richard E. Olson
  • Prodrugs of (1S,9S)-9-[[(1S)-1-carboxy-3-phenylpropyl]amino]octahydro-10-oxo-6H-pyridazino[1,2-a][1,2]diazepine-1-carboxylic acid and their use in transdermal therapeutic systems
    Patent number: 8785431
    Abstract: The present invention relates to diester prodrugs of cilazaprilate which undergo enzymatic cleavage to release the active metabolite cilazaprilate that is used for the treatment of hypertension and congestive heart failure. Furthermore the diester prodrugs of cilazaprilate possess all the properties necessary to be topically administered, preferably via transdermal therapeutic systems.
    Type: Grant
    Filed: June 20, 2012
    Date of Patent: July 22, 2014
    Assignee: Hexal AG
    Inventors: Günther Bernhardt, Miriam Ertel, Armin Buschauer, Jörg Nink
  • Cephalotaxane derivatives and their processes of preparation and purification
    Patent number: RE45128
    Abstract: The present invention concerns a new general process for asymmetric hemisynthesis of harringtonines and their analogs, that are alkaloids used in chemotherapy. This process comprises direct esterification of a natural cephalotaxine with an acylating compound constituted of a side chain precursor which backbone and functionalization are entirely preformed. The invention also concerns a natural, synthetic or semi-synthetic harringtonines including their tautomeric forms and their salts of the following formula: wherein n=2 (i.e. harringtonine) or n=3 (i.e. homoharringtonine), in which the total content of impurities, possibly including enantiomeric forms, is lower than 1%, and/or the content of the major impurity is lower than 0.9%, and/or the chromatographic assay exhibits a harringtonines content higher than 97.5%.
    Type: Grant
    Filed: October 26, 2012
    Date of Patent: September 9, 2014
    Assignee: IVAX International GmbH
    Inventors: Jean-Pierre Robin, Julie Blanchard, Jean-Pierre Marie, Nina Radosevic