Hetero Ring In The Polycyclo Ring System Patents (Class 514/320)
  • Publication number: 20140275020
    Abstract: This invention relates to compounds of Formula I having the following general structure: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.
    Type: Application
    Filed: October 25, 2012
    Publication date: September 18, 2014
    Inventors: Shawn P. Walsh, Alexander Pasternak, Zhi-Cai Shi, Brian Cato
  • Patent number: 8835413
    Abstract: Novel methods for treating or reducing the likelihood of acquiring vaginal dysfunctions, more particularly vaginal dryness and dyspareunia, leading to sexual dysfunction and low sexual desire and performance , in susceptible warm-blooded animals including humans involving administration of a sex steroid precursor. Further administration of estrogen or selective estrogen receptor modulator, particularly those selected from the group consisting of Raloxifene, Arzoxifene, Tamoxifen, Droloxifene, Toremifene, Iodoxifene, GW 5638, TSE-424, ERA-923, and lasofoxifene, and more particularly compounds having the general structure: is specifically disclosed for the medical treatment and/or inhibition of development of some of these above-mentioned diseases. Pharmaceutical compositions for delivery of active ingredient(s) and kit(s) useful to the invention are also disclosed.
    Type: Grant
    Filed: October 20, 2005
    Date of Patent: September 16, 2014
    Assignee: Endorecherche, Inc.
    Inventors: Mohamed El-Alfy, Fernand Labrie, Louise Berger
  • Patent number: 8815907
    Abstract: The invention provides compounds of the formula: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a, Z and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.
    Type: Grant
    Filed: June 19, 2013
    Date of Patent: August 26, 2014
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Craig Husfeld, YuHua Ji, Rick Lee, Li Li, YongQi Mu, Cameron Smith, Johnny Uy
  • Publication number: 20140235628
    Abstract: This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.
    Type: Application
    Filed: September 10, 2012
    Publication date: August 21, 2014
    Inventors: Shawn Walsh, Alexander Pasternak, Brian Cato, Paul E. Finke, Jessica Frie, Qinghong Fu, Dooseop Kim, Barbara Pio, Aurash Shahripour, Zhi-Cai Shi, Haifeng Tang
  • Publication number: 20140235649
    Abstract: A method of treating a mammalian subject afflicted with a disease characterized by a loss of protein function caused by a genetic abnormality associated with the disease comprising administering to the subject a therapeutically effective amount of a protein phosphatase 2A inhibitor or a histone deacetylase inhibitor.
    Type: Application
    Filed: May 24, 2012
    Publication date: August 21, 2014
    Applicant: LIXTE BIOTECHNOLOGY, INC.
    Inventors: John S. Kovach, Zhengping Zhuang, Jie Lu, Chunzhang Yang, Russell Lonser
  • Publication number: 20140221349
    Abstract: Compounds of general formula I wherein the group R1 is defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
    Type: Application
    Filed: February 3, 2014
    Publication date: August 7, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventor: Matthias ECKHARDT
  • Publication number: 20140221342
    Abstract: Provided herein is a method of treating an allergic inflammatory disease selected from asthma, dermatitis, allergic rhinitis, urticaria, anaphylaxis, angioedemea, allergies, contact hypersensitivity, drug hypersensitivity, and allergic conjunctivitis in a mammal, comprising administering a therapeutically effective amount of a compound of Formula I or a pharmaceutically acceptable salt thereof, to said mammal in need thereof, wherein A1, A2, W, L, G, R7a, R7b, R8, R9 and R10 are as defined herein.
    Type: Application
    Filed: March 31, 2014
    Publication date: August 7, 2014
    Applicant: Array BioPharma Inc.
    Inventors: Laurence E. Burgess, Christopher T. Clark, Adam Cook, Christopher P. Corrette, Robert Kirk DeLisle, George A. Doherty, Kevin W. Hunt, Todd T. Romoff, Ganghyeok Kim
  • Patent number: 8796254
    Abstract: Disclosed are uses of carboxamide, sulfonamide and amine compounds for the treatment and amelioration of disorders and conditions related to oxidative stress, mitochondrial dysfunction, free radical damage and metabolic inefficiency, among others. Also described are methods for increasing exercise endurance, exercise efficiency and aerobic workload using the compounds described herein.
    Type: Grant
    Filed: March 31, 2011
    Date of Patent: August 5, 2014
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Donald Payan, Yasumichi Hitoshi, Todd Kinsella
  • Patent number: 8790691
    Abstract: Drag derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drag derivatized with a weak-base moiety that facilitates active loading of the drag through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drag to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drag derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drags.
    Type: Grant
    Filed: May 26, 2009
    Date of Patent: July 29, 2014
    Assignee: The University of British Columbia
    Inventors: Pieter Cullis, Marcel Bally, Marco Ciufolini, Norbert Maurer, Igor Jigaltsev
  • Publication number: 20140206722
    Abstract: Disclosed herein are compositions and methods for treating depression using compositions comprising a compound of formula I. Disclosed herein are compositions and methods for treating depression using compositions comprising phenoxypropylamine compounds and derivatives having selective affinity for and antagonistic activity against the 5-HT1A receptor, as well as 5-HT reuptake inhibitory activity. In addition, compositions and methods for treating depression using compositions comprising a compound of formula II are disclosed. Methods of treating or diminishing at least one symptom of depression in a human subject with a composition comprising a compound of the formula (I) or formula (II), or a pharmaceutically acceptable salt, hydrate, or solvate thereof, are also disclosed.
    Type: Application
    Filed: January 24, 2014
    Publication date: July 24, 2014
    Applicant: MINERVA NEUROSCIENCES, INC.
    Inventors: Lorenzo Pellegrini, Argeris Karabelas, Remy Luthringer
  • Publication number: 20140205688
    Abstract: The present invention relates to a stimulating agent comprising a pungent component having astringency, a stimulating composition including the agent, as well as a flavor or fragrance composition, a food, a drink, an oral care product and an external skin preparation containing the agent or the composition, and also relates to the use of a pungent component having astringency as a stimulating agent. Examples of the pungent component having astringency include a plant extract of Asteraceae Spilanthes, Rutaceae Zanthoxyium, Rutaceae Fagara, or Piperaceae Piper, or an amide derivative represented by general formula (1) (where R1 represents an alkenyl group having 2 to 12 carbon atoms which may be substituted by a methylenedioxyphenyl at the end, R2 and R3 may be the same or different from each other and each are a hydrogen atom or a lower alkyl group in which a hydroxyl group may be substituted, and R2 and R3, together with the nitrogen atom adjacent thereto, may form a heterocyclic ring).
    Type: Application
    Filed: May 29, 2012
    Publication date: July 24, 2014
    Applicant: TAKASAGO INTERNATIONAL CORPORATION
    Inventors: Kaori Takahashi, Miyuki Takayanagi
  • Patent number: 8778970
    Abstract: Provided is a new serotonin-reuptake inhibitor that exhibits affinity for serotonin-1A receptors. Said serotonin-reuptake inhibitor is a compound represented by formula (1) or a pharmacologically acceptable salt thereof. In the formula, R1 represents a hydrogen atom, a 2-hydroxyethyl group, or a 2-methoxyethyl group. R2 represents one of the following bonded to a methylene group which is bonded to a piperidine ring: a chlorine atom bonded in a p-position; a bromine atom bonded in a p-position; a methyl group bonded in a p-position; a chlorine atom bonded in an m-position; or a bromine atom bonded in an m-position. Either Y1 represents a hydrogen atom and Y2 represents a hydrogen atom or a hydroxyl group, or Y1 and Y2 together represent an oxo group. Z represents a group represented by one of the following formulas: formula (3-1-1), formula (3-1-2), formula (3-2-1), formula (3-2-2), formula (3-3-1), formula (3-3-2), formula (3-4-1), or formula (3-4-2).
    Type: Grant
    Filed: August 4, 2010
    Date of Patent: July 15, 2014
    Assignee: Dainippon Sumitomo Pharma Co., Ltd
    Inventors: Tomohiro Toyoda, Tomoaki Nishida, Hidefumi Yoshinaga
  • Patent number: 8778926
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, LP, LQ, X1, X2, X3, A, n and m are as defined in the application. The compounds of formula I have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
    Type: Grant
    Filed: January 20, 2012
    Date of Patent: July 15, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Frank Himmelsbach, Elke Langkopf, Bernd Nosse
  • Publication number: 20140171442
    Abstract: Disclosed are alicyclic[c]benzopyrone derivatives and use thereof. The alicyclic[c]benzopyrone derivatives are compounds represented by formula I or their salts. The present compounds not only significantly improve high activity induced by MK-801, but also effectively improve clambering symptom induced by Apomorphine and do not cause EPS within effective dose. These in vitro targets and in vivo pharmacological models are closely related to diseases of the nervous system caused by dopamine dysfunction, especially schizophrenia. Therefore the present compounds can be used for the treatment of central nervous system diseases, especially schizophrenia. ED50 is lower and effect is stronger in two animal models i.e. high activity induced by MK-801 and clambering symptom induced by Apomorphine, while ED50 is higher and therapeutic index is greater in animal models of catalepsy.
    Type: Application
    Filed: July 31, 2012
    Publication date: June 19, 2014
    Inventors: Guisen Zhang, Yin Chen, Xiangqing Xu, Xin Liu, Song Zhao, Bifeng Liu, Miquan Yu, Yinli Qiu
  • Patent number: 8741928
    Abstract: Provided are protected antimicrobial compounds which are useful for controlling microorganisms in aqueous or water-containing systems, such as oil or gas field fluids, at elevated temperature. The antimicrobial compounds are of the formula I: wherein R, R1, R2, X and Y are as defined herein.
    Type: Grant
    Filed: December 2, 2011
    Date of Patent: June 3, 2014
    Assignees: Dow Global Technologies LLC, ANGUS Chemical Company
    Inventors: Charles E. Coburn, Michael V. Enzien, Heather R. Mcginley, David W. Moore
  • Patent number: 8735391
    Abstract: A functionalized polycyclic compound can have a structure of Formula 1 or salt, prodrug, analog, or derivative thereof, which compound can be prepared by providing a diene; reacting the diene with a dienophile under sufficient conditions for a combined Diels-Alder/acylation reaction so as to provide a polycyclic compound having a carboxylic acid; and coupling the carboxylic acid with an amine-containing compound or a hydroxyl-containing compound so as to form an amide or an ester and producing a compound having a structure of Formula 1. The compound can be used for modulating an opioid receptor, which can be conducted by administering to an opioid receptor a functionalized polycyclic compound as described herein in an effective amount to modulate the functionality of the opioid receptor. Such opioid modulation can provide a biological benefit to a subject.
    Type: Grant
    Filed: September 25, 2009
    Date of Patent: May 27, 2014
    Assignee: University of Kansas
    Inventors: Jeffrey Aube, Bryan L. Roth, Partha Ghosh, Kevin J. Frankowski
  • Publication number: 20140135298
    Abstract: This invention is in the fields of cancer therapy. More particularly it concerns compounds which are useful agents for treating cell proliferative disorders, especially those disorders characterized by over activity and/or inappropriate activity of a EGFR, including EGFR-related cancers, particularly for expanding the efficacy of drugs previously developed for this purpose, and for methods of treatments using the compounds for this purpose.
    Type: Application
    Filed: March 16, 2012
    Publication date: May 15, 2014
    Applicant: THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA
    Inventors: Alan Berezov, Mark I. Greene, Natalie Minkovsky, Zheng Cai, Hongtao Zhang
  • Patent number: 8722578
    Abstract: Herbicidal compositions containing as active ingredients spiroheterocyclic pyrrolidine dione compounds.
    Type: Grant
    Filed: October 28, 2009
    Date of Patent: May 13, 2014
    Assignee: Syngenta Participations AG
    Inventors: Werner Zambach, Ottmar Franz Hueter, Jean Wenger, Marcela Goeghova, Thomas Pitterna, Peter Maienfisch, Stephane André´Marie Jeanmart, Michel Muehlebach
  • Patent number: 8716314
    Abstract: Provided herein are thalidomide, which is enriched with isotopes such as deuterium. Pharmaceutical compositions comprising the isotopes-enriched compounds, and methods of using such compounds are also provided.
    Type: Grant
    Filed: February 9, 2010
    Date of Patent: May 6, 2014
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Hon-Wah Man
  • Patent number: 8703957
    Abstract: The present invention is directed to phosphonic acid compounds useful as serine protease inhibitors, compositions thereof and methods for treating inflammatory and serine protease mediated disorders.
    Type: Grant
    Filed: June 19, 2013
    Date of Patent: April 22, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Michael N. Greco, Harold R. Almond, Jr., Michael J. Hawkins, Eugene Powell
  • Publication number: 20140107095
    Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
    Type: Application
    Filed: December 20, 2013
    Publication date: April 17, 2014
    Applicant: SERAGON PHARMACEUTICALS, INC.
    Inventors: Mehmet Kahraman, Steven P. Govek, Johnny Y. Nagasawa, Nicholas D. Smith
  • Patent number: 8686021
    Abstract: Use of a benzoyl derivative of 3-aminocarbazole to produce a drug for the preventive or therapeutic treatment of a disorder selected form the group comprising inflammatory processes, pain, fever, tumors, Alzheimer's disease and atherosclerosis. Method for the preventive or therapeutic treatment of a disorder selected from the group comprising inflammatory processes, pain, fever, tumors, Alzheimer's disease and atherosclerosis in which a therapeutically effective quantity of a benzoyl derivative of 3-aminocarbazole according to the invention is administered to an individual.
    Type: Grant
    Filed: May 3, 2006
    Date of Patent: April 1, 2014
    Assignee: Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
    Inventors: Lorenzo Polenzani, Giorgina Mangano, Isabella Coletta, Maria Alessandra Alisi, Nicola Cazzolla, Guido Furlotti, Caterina Maugeri
  • Publication number: 20140088078
    Abstract: The invention provides tricyclic compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tricyclic compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.
    Type: Application
    Filed: May 7, 2012
    Publication date: March 27, 2014
    Applicant: ZAFGEN, Inc.
    Inventors: Susan Mary Cramp, Hazel Joan Dyke, Thomas David Pallin, Robert Zahler
  • Publication number: 20140073595
    Abstract: The present invention relates to an aromatic substituted pentadienoic acid amides and there use in combination of specific amounts of aromatic amides i.e. 4-alkyl-5-(substituted phenyl)-2(E),4(E)-pentadienoic acid amides, its geometrical isomers or their dihydro or tetrahydro derivatives and an anti-infective drug useful in potentiating the bioefficacy of antiinfective drug. The combination of the present invention is useful in the treatment of certain infections and disease at lower concentration of anti-infectives necessary to inhibit the growth of microbial strains and may also find applications in reducing the resistance in microorganisms.
    Type: Application
    Filed: October 11, 2013
    Publication date: March 13, 2014
    Applicant: Council Of Scientific and Industrial Research
    Inventors: Surrinder KOUL, Jawahir Lal KOUL, Subhash Chandra TANEJA, Pankaj GUPTA, Inshad Ali KHAN, Zahid Mehmood MIRZA, Ashwani KUMAR, Rakesh Kamal JOHRI, Monika PANDITA, Anita KHOSA, Ashok Kumar TIKOO, Subhash Chander Sharma, Vijeshwar VERMA, Ghulam Nabi QAZI
  • Publication number: 20140045813
    Abstract: The present invention encompasses compounds of the formula (I) wherein the groups A, Cy, X1 and Y are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.
    Type: Application
    Filed: August 8, 2013
    Publication date: February 13, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Joerg Martin BENTZIEN, Angela Kay BERRY, Todd BOSANAC, Michael Jason BURKE, Darren Todd DISALVO, Joshua Courtney HORAN, Shuang LIANG, Can MAO, Wang MAO, Yue SHEN, Fariba SOLEYMANZADEH, Renee M. ZINDELL
  • Patent number: 8642769
    Abstract: This invention provides the methods of separation and identification of a novel type of piperidine flavan alkaloids from an African herbal tea, the leaves of Combretum micranthum commonly known as kinkeliba, and the procedures for preparing the total piperidine flavan alkaloids (TPFA). In particular, this invention relates to the use of the plant extract that may contain TPFA as anti-diabetic agents in treatment of metabolic disorders and other applications related to this new chemical structure and derivatives thereof.
    Type: Grant
    Filed: May 3, 2011
    Date of Patent: February 4, 2014
    Inventors: James E. Simon, Qingli Wu, Cara Welch
  • Publication number: 20140031302
    Abstract: The present invention includes novel derivatives, analogs, and intermediates of the natural products radicicol, pochonins, pochoximes, and their syntheses. The present invention also provides a pharmaceutical composition comprising the present compound and the use of the compound as inhibitors of kinases and of the enzyme family known as heat shock protein 90 (HSP90).
    Type: Application
    Filed: October 24, 2011
    Publication date: January 30, 2014
    Applicant: UNIVERSITE DE STRASBOURG
    Inventors: Nicolas Winssinger, Sofia Barluenga
  • Publication number: 20140005250
    Abstract: A method of (a) treating a lymphoproliferative disease in a subject in need thereof; (b) slowing the progression of lymphoproliferative disease in a subject who has been diagnosed with a lymphoproliferative disease; or (c) preventing or delaying development of a lymphoproliferative disease in a subject who is at risk of developing a lymphoproliferative disease. The method generally comprises administering to the individual an effective amount of a combination therapy comprising: i) at least one autophagy modulating agent, or a derivative, pharmaceutically acceptable salt thereof, or prodrug thereof; and ii) at least one CDK inhibitor agent, or a derivative, pharmaceutically acceptable salt thereof, or prodrug thereof, wherein the i) agent and the ii) agents are administered in amounts sufficient to enhance the cytotoxicity of the combination relative to the CDK inhibitor agent treatment alone.
    Type: Application
    Filed: November 7, 2011
    Publication date: January 2, 2014
    Applicant: THE OHIO STATE UNIVERSITY
    Inventors: John C. Byrd, Amy J. Johnson, Emilia Mahoney, David M. Lucas, Michael R. Grever
  • Publication number: 20130345199
    Abstract: The present invention relates to 1-[m-Carboxamido(hetero)aryl-methyl]-piperidine-4-carboxamide derivatives of formula (I) wherein X, Ar1, R1, R2, R3, R4, R5 and p are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as CXCR7 receptor modulators.
    Type: Application
    Filed: June 21, 2013
    Publication date: December 26, 2013
    Applicant: Actelion Pharmaceuticals Ltd.
    Inventors: Heinz FRETZ, Markus Gude, Philippe Guerry, Thierry Kimmerlin, Francois Lehembre, Thomas Pfeifer, Anja Valdenaire
  • Patent number: 8614232
    Abstract: An injectable depot formulation comprising crystals having structure (I) wherein R is (FII) and the X50 value of the crystals is from 1 to 200 microns. Depot formulations containing crystals of iloperidone or its metabolites have the following advantages: (i) release of the crystals in plasma can be correlated with the size of the crystals; (ii) absorption of the crystals in plasma can be correlated with the size of the crystals; (iii) the particle size of the crystals can be controlled by crystal engineering and/or milling; and (iv) the crystals are stable upon storage, and stable to sterilization procedures, such as gamma irradiation.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: December 24, 2013
    Assignee: Novartis AG
    Inventors: Dierk Wieckhusen, Alexandra Glausch, Markus Ahlheim
  • Patent number: 8614231
    Abstract: The present invention relates to a compound of structural formula (I) and its derivatives for use as medicinal drugs. They are preferably immunosuppressive agents, with mechanism of action based on the blockage of TCR-Nck interaction.
    Type: Grant
    Filed: June 18, 2009
    Date of Patent: December 24, 2013
    Assignee: Consejo Superior de Investigaciones Cientificas
    Inventors: Balbino Alarcon Sanchez, Aldo Borroto Revuelta, Antonio Morreale de Leon, María del Carmen Fábregas Cleveria, Maria Luz Ortiz
  • Publication number: 20130337148
    Abstract: The invention relates to film products containing desired levels of active components and methods of their preparation. Desirably, the films disintegrate in water and may be formed by a controlled drying process, or other process that maintains the required uniformity of the film. Desirably, the films may be exposed to temperatures above that at which the active components typically degrade without concern for loss of the desired activity.
    Type: Application
    Filed: March 29, 2013
    Publication date: December 19, 2013
    Applicant: MONOSOL RX, LLC
    Inventors: Robert K. Yang, Richard C. Fuisz, Garry L. Myers, Joseph M. Fuisz
  • Patent number: 8609695
    Abstract: Novel methods for the medical treatment and/or prevention of obesity, abdominal fat, and insulin resistance in susceptible warm-blooded animals including humans involves the administration of selective estrogen receptor modulators (SERMs). A combination of a SERM with an amount of estrogen or a sex steroid precursor selected from the group consisting of dehydroepiandrosterone, dehydroepiandrosterone sulfate, androst-5-ene-3b,17b-diol and compounds converted in vivo to one of the foregoing precursors or estrogen is also disclosed.
    Type: Grant
    Filed: March 10, 2003
    Date of Patent: December 17, 2013
    Assignee: Endorecherche, Inc.
    Inventors: Fernand Labrie, Yves Deshaies, Denis Richard, Celine Martel, Andre Marette
  • Patent number: 8603521
    Abstract: Dosing regimens, methods of treatment, controlled release formulations, and combination therapies that include an HDAC inhibitor, or a pharmaceutically acceptable salt thereof, are described.
    Type: Grant
    Filed: April 16, 2010
    Date of Patent: December 10, 2013
    Assignee: Pharmacyclics, Inc.
    Inventors: David J. Loury, Joseph J. Buggy, Tarak D. Mody, Erik J. Verner, Norbert Purro, Sriram Balasubramanian
  • Patent number: 8604059
    Abstract: The claimed subject matter is directed to certain thioxanthene derivatives and phenothiazine derivatives suitable for use as anti-infective agents, in particular, for the treatment of infectious diseases. The claimed subject matter furthermore relates to compositions including said anti-infective agents.
    Type: Grant
    Filed: April 20, 2010
    Date of Patent: December 10, 2013
    Assignee: BKG Pharma APS
    Inventor: Birgit Kjældgaard Giwercman
  • Patent number: 8586610
    Abstract: The present invention relates to methods for the identification of genetic polymorphisms that may be associated with a risk for QT prolongation after treatment with iloperidone and related methods of administering iloperidone to patients with such polymorphisms.
    Type: Grant
    Filed: September 30, 2005
    Date of Patent: November 19, 2013
    Assignee: Vanda Pharmaceuticals, Inc.
    Inventors: Curt D. Wolfgang, Mihael H. Polymeropoulos
  • Patent number: 8586589
    Abstract: The present invention relates to piperidine and piperazine phenyl sulfonamides useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including for example the treatment of pain.
    Type: Grant
    Filed: October 2, 2012
    Date of Patent: November 19, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Esther Martinborough, Lev T. D. Fanning, Urvi Sheth, Dean Wilson, Andreas P. Termin, Timothy D. Neubert, Nicole Hilgraf, Tara Leanne Hampton, Tara Whitney, Aarti Sameer Kawatkar, Danielle Lehsten, Dean Stamos, Jinglan Zhou, Vijayalaksmi Arumugam, Corey Anderson
  • Publication number: 20130303489
    Abstract: The present invention provides compounds, pharmaceutical compositions and methods for the treatment of specific cancers. Such compositions may generally comprise a compound of formula (I): wherein R1-R3 are as defined herein, or pharmaceutically acceptable salts or esters thereof; and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: March 11, 2013
    Publication date: November 14, 2013
    Applicant: Eisai R&D Management Co., Ltd.
    Inventors: Sergei Agoulnik, Bruce Decosta, Hong Du, Yimin Jiang, Xiang-Yi Li, Kenichi Nomoto, John (Yuan) Wang, Huiming Zhang
  • Publication number: 20130296288
    Abstract: The present invention relates to a salt in which at least one cation and at least one anion is in each case an emitter compound or a dye compound, characterised in that at least one of the emitter compounds is a fluorescent emitter compound. In addition, the present invention also relates to a process for the preparation of the salt according to the invention, to the use of the salt in an electronic device, and to a formulation and an electronic device which comprises the salt.
    Type: Application
    Filed: November 24, 2011
    Publication date: November 7, 2013
    Applicant: Merck Patent GmbH
    Inventors: Junyou Pan, Philipp Stoessel
  • Patent number: 8569282
    Abstract: Chemokine receptor antagonists, in particular, compounds of Formula (I-A) that act as antagonists of the chemokine CCR2 receptor, including pharmaceutical compositions and uses thereof to treat or prevent diseases associated with monocyte accumulation, lymphocyte accumulation or leukocyte accumulation are described herein.
    Type: Grant
    Filed: December 11, 2008
    Date of Patent: October 29, 2013
    Assignee: CytoPathfinder, Inc.
    Inventors: Efrat Ben-Zeev, Dongli Chen, Merav Fichman, Shomir Ghosh, Steffi Koerner, Jian Lin, Yael Marantz, Rosa E. Melendez, Pradyumna Mohanty, Sharon Shacham, Zhaoda Zhang
  • Publication number: 20130281489
    Abstract: The invention provides compounds of the formula: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a, Z and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.
    Type: Application
    Filed: June 19, 2013
    Publication date: October 24, 2013
    Applicant: THERAVANCE, INC.
    Inventors: Craig Husfeld, YuHua Ji, Rick Lee, Li Li, YongQi Mu, Cameron Smith, Johnny Uy
  • Patent number: 8552032
    Abstract: The present invention is directed to novel bicyclic derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by DPP-1.
    Type: Grant
    Filed: December 16, 2010
    Date of Patent: October 8, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: Edward C. Lawson, Dennis J. Hlasta, Shyamali Ghosh, Renee L. DesJarlais, Carsten Schubert
  • Patent number: 8545877
    Abstract: Drug derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drug derivatized with a weak-base moiety that facilitates active loading of the drug through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drug to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drug derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drugs.
    Type: Grant
    Filed: April 19, 2013
    Date of Patent: October 1, 2013
    Assignee: University of British Columbia
    Inventors: Pieter Cullis, Marcel Bally, Marco Ciufolini, Norbert Maurer, Igor Jigaltsev
  • Publication number: 20130252937
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
    Type: Application
    Filed: March 14, 2013
    Publication date: September 26, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Matthias ECKHARDT, Sara FRATTINI, Dieter HAMPRECHT, Frank HIMMELSBACH, Elke LANGKOPF, Iain LINGARD, Stefan PETERS, Holger WAGNER
  • Publication number: 20130237566
    Abstract: Disclosed are compounds of Formula (I) or stereoisomers, salts, or prodrugs thereof, wherein: W is CH2 or O; Q is Formula (II), Formula (III) or Formula (IV); and R1, R2, R3, R4, n, and G are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
    Type: Application
    Filed: November 2, 2011
    Publication date: September 12, 2013
    Inventors: Robert J. Cherney, Zhongyu Wang
  • Publication number: 20130237536
    Abstract: Heterocyclic compounds which modulate cannabinoid receptors are presented. Pharmaceutical compositions containing these compounds, methods of using these compounds as modulators of cannabinoid receptors and processes for synthesizing these compounds are also described herein.
    Type: Application
    Filed: April 26, 2013
    Publication date: September 12, 2013
    Applicant: The Cleveland Clinic Foundation
    Inventors: Mohamed Naguib Attala, Philippe Diaz
  • Patent number: 8530498
    Abstract: Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of an immunomodulatory compound alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of an immunomodulatory compound. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.
    Type: Grant
    Filed: April 8, 2013
    Date of Patent: September 10, 2013
    Assignee: Celgene Corporation
    Inventor: Jerome B. Zeldis
  • Publication number: 20130231325
    Abstract: Disclosed are novel isoflavone derivatives having the structure of Formula I: which are ALDH-2 inhibitors, useful for treating a patient in need thereof, for dependence upon drugs of addiction, for example addiction to dopamine-producing agent such as cocaine, morphine, amphetamines, nicotine, and alcohol.
    Type: Application
    Filed: August 30, 2012
    Publication date: September 5, 2013
    Applicant: Gilead Sciences. Inc.
    Inventors: Michael Graupe, Chandrasekar Venkataramani, Jeff Zablocki
  • Publication number: 20130230583
    Abstract: Drug derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drug derivatized with a weak-base moiety that facilitates active loading of the drug through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drug to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drug derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drugs.
    Type: Application
    Filed: April 19, 2013
    Publication date: September 5, 2013
    Inventors: Pieter Cullis, Marcel Bally, Marco Ciufolini, Norbert Maurer, Igor Jigaltsev
  • Publication number: 20130231338
    Abstract: The present invention relates to novel benzofuran-2-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: March 1, 2013
    Publication date: September 5, 2013
    Applicant: ALLERGAN, INC.
    Inventors: HAIQING YUAN, RICHARD L. BEARD, XIAOXIA LIU, JOHN E. DONELLO, VEENA VISWANATH, MICHAEL E. GARST