Chalcogen Bonded Directly To The Five-membered Hetero Ring By Nonionic Bonding Patents (Class 514/424)
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Publication number: 20130310423Abstract: The present invention relates to new diterpenoid derivatives of formula (I), processes for their preparation, and to pharmaceutical compositions containing them for the treatment of cardiovascular disorders, urinary incontinence, asthma, or Alzheimer's disease and/or to prevent obstructive vascular lesions consequently to arteriotomy and/or angioplasty, and to prevent organ damage in hypertensive patients.Type: ApplicationFiled: July 26, 2013Publication date: November 21, 2013Applicant: SIGMA-TAU Industrie Farmaceutiche Riunite S.p.A.Inventors: Alberto Cerri, Mauro Gobbini, Marco Torri, Patrizia Ferrari, Mara Ferrandi, Giuseppe Bianchi
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Publication number: 20130302377Abstract: Methods of treatment or prevention of a cancerous or pre-cancerous condition, of slowing or preventing growth of a cancerous condition, of stimulating a cell-mediated immune response, stimulating a Th1 helper T cell response against a pathogen in a mammal and of treating or preventing inflammatory diseases or disorders that involve administration of N-methyl pyrrolidone (NMP) or a physiologically acceptable salt, solvate, tautomer or prodrug thereof are provided. Also provided are formulations of an active agent.Type: ApplicationFiled: June 21, 2011Publication date: November 14, 2013Applicant: PETER MACCALLUM CANCER INSTITUTEInventors: Andy Kang-Wei Hsu, Jake Shortt, Paul Neeson, Ricky Wayne Johnstone, David Ritchie
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Publication number: 20130289019Abstract: One embodiment of an aspect of the present invention is a method for lessening the symptoms of depression, anxiety, and post-traumatic stress disorder comprising the step of administering a therapeutically effective quantity of a cholinergic M1 receptor antagonist and a therapeutically effective quantity of one or more cholinomimetic agents to lessen the symptoms of depression, anxiety, and post-traumatic stress disorder. Typically, the cholinergic M1 receptor antagonist is selected from the group consisting of telenzepine, amytriptyline, biperiden, trihexyphenidyl, darifenacin, dicyclomine, and tiotropium. Another aspect of the present invention is directed to methods and compositions employing other therapeutic agents and combinations of therapeutic agents for emulating the theoretical pharmacological effects of the non-selective mAChR antagonist scopolamine. The invention also encompasses pharmaceutical compositions incorporating one or more therapeutic agents and a pharmaceutically acceptable carrier.Type: ApplicationFiled: April 25, 2013Publication date: October 31, 2013Applicant: Amazing Grace, Inc.Inventor: David T. Chau
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Publication number: 20130289034Abstract: Methods of treating or suppressing mitochondrial diseases, such as Friedreich's ataxia (FRDA), Leber's Hereditary Optic Neuropathy (LHON), mitochondrial myopathy, encephalopathy, lactacidosis, and stroke (MELAS), Kearns-Sayre Syndrome (KSS), are disclosed, as well as compounds useful in the methods of the invention, such as 4-(p-quinolyl)-2-hydroxybutanamide derivatives. Methods and compounds useful in treating other disorders such as amyotrophic lateral sclerosis (ALS), Huntington's disease, Parkinson's disease, and pervasive developmental disorders such as autism are also disclosed. Energy biomarkers useful in assessing the metabolic state of a subject and the efficacy of treatment are also disclosed. Methods of modulating, normalizing, or enhancing energy biomarkers, as well as compounds useful for such methods, are also disclosed.Type: ApplicationFiled: June 21, 2013Publication date: October 31, 2013Inventors: Orion D. JANKOWSKI, Kieron E. WESSON, Paul MOLLARD, William D. SHRADER
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Patent number: 8568699Abstract: Soft anticholinergic zwitterions of the formulas: wherein R1 and R2 are both phenyl or one of R1 and R2 is phenyl and the other is cyclopentyl; and wherein each asterisk marks a chiral center; said compound having the R, S or RS stereoisomeric configuration at each chiral center unless specified otherwise, or being a mixture thereof.Type: GrantFiled: October 31, 2011Date of Patent: October 29, 2013Inventor: Nicholas S. Bodor
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Publication number: 20130274283Abstract: Premature termination codons readthrough compounds, composition thereof, and methods of making and using the same are provided.Type: ApplicationFiled: February 11, 2013Publication date: October 17, 2013Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Richard A. GATTI, Liutao DU, Robert DAMOISEAUX, Chih-Hung LAI, Michael JUNG, Jin-Mo KU, Carmen BERTONI
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Publication number: 20130261045Abstract: The subject invention concerns materials and methods for treating or preventing a neurodegenerative condition or disease associated with ?-amyloid peptide deposition in neural tissue in a person or animal by administering a therapeutically effective amount of a polyphenol, or an analog, isomer, metabolite, or prodrug thereof, that increases expression or activity of a protein that exhibits ?-secretase activity. The subject invention also provides methods to increase ?-secretase expression and/or activity in cells by administering polyphenol flavonoids like (?)-epigallocatechin-3-gallate (EGCG) and epicatechin (EC), two polyphenols derived from green tea and other plants and that can be produced synthetically. Furthermore, there are provided methods to decrease or inhibit the production of A?1-40 or A?1-42 by administering the EGCG and EC compounds, their analogs, metabolites, and prodrugs.Type: ApplicationFiled: December 7, 2012Publication date: October 3, 2013Inventors: ROLAND DOUGLAS SHYTLE, JUN TAN
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Publication number: 20130259830Abstract: Modulators of CRTH2, particularly antagonists of CRTH2, that are useful for treating various disorders, including asthma and respiratory disorders are disclosed.Type: ApplicationFiled: June 24, 2011Publication date: October 3, 2013Applicant: Ironwood Pharmaceuticals, Inc.Inventors: Timothy Barden, Colleen Hudson, James Jia, Charles Kim, Regina Graul, Ara Mermerian, Joel Moore, Kevin Sprott, Yueh-tyng Chien
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Patent number: 8546493Abstract: Multi-armed, monofunctional, and hydrolytically stable polymers are described having the structure wherein Z is a moiety that can be activated for attachment to biologically active molecules such as proteins and wherein P and Q represent linkage fragments that join polymer arms polya and polyb, respectively, to central carbon atom, C, by hydrolytically stable linkages in the absence of aromatic rings in the linkage fragments. R typically is hydrogen or methyl, but can be a linkage fragment that includes another polymer arm. A specific example is an mPEG disubstituted lysine having the structure where mPEGa and mPEGb have the structure CH3O—(CH2CH2O)nCH2CH2— where n may be the same or different for polya- and polyb- and can be from 1 to about 1,150 to provide molecular weights of from about 100 to 100,000.Type: GrantFiled: December 14, 2012Date of Patent: October 1, 2013Assignee: Nektar TherapeuticsInventors: J. Milton Harris, Francesco M. Veronese, Paolo Caliceti, Oddone Schiavon
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Publication number: 20130251673Abstract: The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.Type: ApplicationFiled: December 21, 2012Publication date: September 26, 2013Applicant: Novira Therapeutics, INC.Inventors: George D. HARTMAN, Osvaldo A. FLORES
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Patent number: 8535717Abstract: The present invention relates to an oral controlled release pharmaceutical composition in the form of a unit dosage form comprising: (a) a highly soluble high dose active ingredient consisting essentially of therapeutically effective amount of levetiracetam or a pharmaceutically acceptable derivative thereof, and (b) a rate controlling means comprising a rate-controlling agent and/or a coating selected from (i) a active ingredient permeable coating surrounding the unit dosage form, and (ii) an active ingredient impermeable coating covering one or more surfaces but not all the surfaces of the unit dosage form, wherein the composition is in the form of a compact tablet and the levetiracetam or a pharmaceutically acceptable derivative thereof is present in an amount ranging from about 55% to about 90% by weight of the tablet.Type: GrantFiled: May 6, 2011Date of Patent: September 17, 2013Assignee: Sun Pharma Advanced Research Company LimitedInventors: Yashoraj Rupsinh Zala, Nitin Bhalachandra Dharmadhikari
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Publication number: 20130237583Abstract: The present invention provides stereoselective processes for the preparation of compounds of formula (I) wherein P is phenyl, naphthyl, a 6-membered heteroaryl group containing one or two nitrogen atoms as ring members, or a 10-membered bicyclic heteroaryl group containing one or two nitrogen atoms as ring members, and wherein the phenyl, naphthyl and heteroaryl groups are optionally substituted; R1 is chlorodifluoromethyl or trifluoromethyl; R2 is optionally substituted aryl or optionally substituted heteroaryl; n is 0 or 1; including the process comprising (a-i) reacting a compound of formula II wherein P, R1 and R2 are as defined for the compound of formula I; with nitromethane in the presence a chiral catalyst to give a compound of formula III Wherein P, R1 and R2 are as defined for the compound of formula I; and (a-ii) reductively cyclising the compound of formula III to give the compound of formula I.Type: ApplicationFiled: June 14, 2011Publication date: September 12, 2013Applicant: SYNGENTA CROP PROTECTION LLCInventors: Myriem El Qacemi, Helmars Smits, Jerome Yves Cassayre, Nicholas Phillip Mulholland, Peter Renold, Edouard Godineau, Thomas Pitterna
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Publication number: 20130231319Abstract: The invention relates to a method for preparing linear polymers having an amide end or having a star architecture comprising an amide core, by means of a ring opening using lactide and glycolide monomers or a lactide monomer ring in the presence of a catalyst, wherein the method includes the steps of: (i) reacting the excess monomer(s) with an initiator in a solvent, said initiator being selected from among an amine and an amino alcohol, given that the initiator has at least one primary or secondary amine function; (ii) adding a catalyst, said catalyst being a non-nucleophilic base and including at least one neutral sp2 nitrogen atom; and (iii) neutralizing the reaction mixture. Said novel method is particularly advantageous in that it can be easily monitored and enables better modulation of the polymers, and thus of the properties thereof, than the methods of the prior art. The invention also relates to novel polymers that are obtainable by means of said method.Type: ApplicationFiled: November 16, 2011Publication date: September 5, 2013Applicant: Actelion Pharmaceuticals Ltd.Inventors: Daniel Bur, Olivier Corminboeup, Sylvaine Gren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein, Davide Pozzi
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Publication number: 20130225619Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are substituted heterocyclic amine derivative compound and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.Type: ApplicationFiled: January 18, 2013Publication date: August 29, 2013Applicant: Acucela Inc.Inventors: Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Ryo Kubota
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Publication number: 20130225588Abstract: The invention is concerned with the compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and X are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are antagonists or partial agonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.Type: ApplicationFiled: February 14, 2013Publication date: August 29, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Patent number: 8518918Abstract: The invention relates to novel combinations based on anticholinergics, ?2-adrenoceptor agonists, PDE 4 Inhibitors, glucocorticoids, and leukotriene-receptor antagonists, process for their production and their use for the treatment of inflammatory diseases, preferably respiratory diseases as bronchial asthma and chronic obstructive pulmonary diseases (COPD) or rheumatic or autoimmune diseases.Type: GrantFiled: September 23, 2011Date of Patent: August 27, 2013Inventors: Joachim Maus, Kastrup Horst, Istvan Szelenyi, Peter Jurgen Cnota, Bauhofer Artur
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Publication number: 20130217732Abstract: This invention provides compounds of formula I, pharmaceutical compositions comprising a compound of formula I and a pharmaceutically acceptable excipient, methods of modulating the androgen receptor, methods of treating diseases beneficially treated by an androgen receptor modulator (e.g., sarcopenia, prostate cancer, contraception, type 2 diabetes related disorders or diseases, anemia, depression, and renal disease) and processes for making compounds and intermediates useful in the preparation of same.Type: ApplicationFiled: September 27, 2011Publication date: August 22, 2013Inventor: Chris P. Miller
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Publication number: 20130210769Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cannabinoid Receptor 1 (CB1).Type: ApplicationFiled: March 15, 2013Publication date: August 15, 2013Applicant: IRM LLCInventors: Hong Liu, Xiaohui He, Dean Paul Phillips, Xuefeng Zhu, Kunyong Yang, Thomas Lau, Baogen Wu, Yongping Xie, Truc Ngoc Nguyen, Xing Wang
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Patent number: 8507545Abstract: Disclosed is a substance which has a low molecular weight, can be applied in a simpler manner, and has an immunopotentiating activity against cancer and/or a microorganism-mediated infectious disease. An EP4 agonist exhibits an immunopotentiating activity through the activation of a cytotoxic T cell, and is therefore useful for the prevention and/or treatment of cancer or a microorganism-mediated infection disease.Type: GrantFiled: May 7, 2008Date of Patent: August 13, 2013Assignees: National University Corporation, Hamamatsu University School of Medicine, Ono Pharmaceutical Co., Ltd.Inventors: Masahiro Takigawa, Naohiro Seo, Kenji Kabashima, Takayuki Maruyama, Toshiya Kanaji
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Publication number: 20130203751Abstract: The present application relates to novel substituted 8-alkoxy-2-aminotetraline derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular disorders.Type: ApplicationFiled: May 9, 2011Publication date: August 8, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Walter Hübsch, Michael Hahn, Alexandros Vakalopoulos, Volkhart Min-Jian Li, Frank Wunder, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Friederike Stoll, Niels Lindner
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Publication number: 20130202705Abstract: This disclosure relates to an extended release oral dosage form comprising a matrix containing a viscosity modifier (but no lipid) and coated granules containing a high water-soluble, high dose drug. The dosage form has alcohol resistance and may also have crush resistance.Type: ApplicationFiled: May 9, 2011Publication date: August 8, 2013Applicant: Cima Labs Inc.Inventor: Ehab Hamed
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Publication number: 20130202667Abstract: The present invention relates to hydrogel particles coated with lipid, which are made from dispersing hydrogel particles in an organic solvent in which lipids are dissolved, and to a method for manufacturing same. Unlike the existing method for manufacturing hydrogel core vesicles, the present invention can effectively manufacture same by using an emulsification method, without involving the steps of chemical treatment of the surface of hydrogels or dilution, thereby facilitating mass production and preventing the decrease of drug encapsulation efficiency.Type: ApplicationFiled: October 12, 2011Publication date: August 8, 2013Applicant: AMOREPACIFIC CORPORATIONInventors: Eun Jung An, Do Hoon Kim, Hyung Jun Lim, Jong Won Shim, Choon Bok Jeong, Lee Kyoung Kwon, Jun Oh Kim
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Publication number: 20130196978Abstract: Alkaloid aminoester compounds which act as muscarinic receptor antagonists are useful for the prevention and/or treatment of a broncho-obstructive or inflammatory diseases.Type: ApplicationFiled: March 14, 2013Publication date: August 1, 2013Applicant: Chiesi Farmaceutici S.p.A.Inventor: Chiesi Farmaceutici S.p.A.
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Patent number: 8497263Abstract: The present invention provides a compound represented by the formula (I): wherein R1, R2, R3, Z1, Z2, Ra, Rb, q, A and n are as defined in the description, a pharmaceutically acceptable salt or solvate thereof. The compound is useful as P2X3 and/or P2X2/3 receptor antagonist.Type: GrantFiled: September 23, 2011Date of Patent: July 30, 2013Assignee: Shionogi & Co., Ltd.Inventors: Hiroyuki Kai, Shunji Shinohara, Takayuki Kameyama
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Patent number: 8497282Abstract: Methods of preparing (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid are disclosed. Also provided are pharmaceutical compositions comprising (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid, and methods of treatment using such compositions.Type: GrantFiled: December 30, 2009Date of Patent: July 30, 2013Assignee: Sunesis Pharmaceuticals, Inc.Inventors: Anantha Sudhakar, Tamilarasan Subramani, Mohamed Sheik Mohamed Mujeebur Rahuman, Ramar Subbiah
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Patent number: 8497381Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the antagonists of PGD2 receptors described herein, as well as methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: GrantFiled: February 25, 2009Date of Patent: July 30, 2013Assignee: Panmira Pharmaceuticals, LLCInventors: John Howard Hutchinson, Brian Andrew Stearns, Thomas Jonathan Seiders, Jill Melissa Scott, Jeannie M. Arruda, Bowei Wang
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Publication number: 20130190377Abstract: The present invention relates to novel lactams of formulae (I) and (II). The present invention further relates to the use of these compounds in the treatment of microbial infections and microbial contamination of surfaces, particularly infections and surface contaminations characterised by biofilm formation. Further provided are compounds of formula (I) and (II) substituted with acrylate or methacrylate groups and their attachment to surfaces or polymers to inhibit microbial contamination.Type: ApplicationFiled: January 24, 2007Publication date: July 25, 2013Applicant: BIOSIGNAL LIMITEDInventors: Naresh Kumar, George Iskander
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Publication number: 20130190338Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: ApplicationFiled: March 11, 2013Publication date: July 25, 2013Applicant: ALLERGAN, INC.Inventor: ALLERGAN, INC.
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Patent number: 8486992Abstract: The invention relates to compounds of formula processes and intermediates for their preparation, their use as muscarinic antagonists and pharmaceutical composition containing them.Type: GrantFiled: July 1, 2010Date of Patent: July 16, 2013Assignee: Pfizer LimitedInventors: Paul Alan Glossop, Simon John Mantell, Anthony Wood, Christine Anne Louise Watson
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Publication number: 20130172319Abstract: The invention relates to the generation of a library of compounds enriched in agonist and antagonists for members of the G-protein coupled class of receptors (GPCRs). The library contains compounds of general formula (II) wherein: y is any integer from 1 to 8; X is —CO—R1 or —SO2—R1; each R1 is independently selected from an alkyl, haloalkyl, alkenyl, alkynyl, alkylaminoalkyl, alkylaminodialkyl, or charged alkylaminotrialkyl, radical of 1 to 20 carbon atoms; or each R1 is independently selected from oxyalkyl, aminoalkyl, aminodialkyl, or charged aminotrialkyl radical; and wherein the R1 radical has a “key” carbon next to the carbonyl of the carbon amide or the sulfonyl group of the sulfonamide which is di-substituted with the same or different groups selected from: alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, alkynyl and alkylamino radicals.Type: ApplicationFiled: February 26, 2013Publication date: July 4, 2013Applicants: CAMBRIDGE ENTERPRISE LIMITEDInventors: Cambridge Enterprise Limited, David J. Grainger, David John Fox
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Publication number: 20130172398Abstract: A method administers quaternary ammonium anti-cholinergic muscarinic receptor antagonists in combination with acetyl-cholinesterase inhibitors to treat either cognitive impairment or acute delirium. This therapy results in a modification of a cognitive disorder or disease, namely a slow down in the disease progression. In one preferred embodiment, the disease is dementia with Lewy Bodies. New formulations for quaternary ammonium anti-cholinergic muscarinic receptor antagonists are also disclosed.Type: ApplicationFiled: February 27, 2013Publication date: July 4, 2013Inventor: Steven A. Rich
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Publication number: 20130171077Abstract: Ion channel modulating compounds are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the treatment of arrhythmia and the production of analgesia and local anesthesia.Type: ApplicationFiled: November 15, 2012Publication date: July 4, 2013Applicant: CARDIOME PHARMA CORP.Inventor: Cardiome Pharma Corp.
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Publication number: 20130172379Abstract: A method administers quaternary ammonium anti-cholinergic muscarinic receptor antagonists in combination with acetyl-cholinesterase inhibitors to treat either cognitive impairment or acute delirium. This therapy results in a modification of a cognitive disorder or disease, namely a slow down in the disease progression. In one preferred embodiment, the disease is dementia with Lewy Bodies. New formulations for quaternary ammonium anti-cholinergic muscarinic receptor antagonists are also disclosed.Type: ApplicationFiled: February 27, 2013Publication date: July 4, 2013Inventor: Steven A. Rich
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Publication number: 20130158035Abstract: Screening methods for identifying compounds and compounds and pharmaceutical compositions for treating and preventing cancer are disclosed. The compounds affect signal transduction downstream of the MET receptor.Type: ApplicationFiled: August 23, 2011Publication date: June 20, 2013Applicant: Brigham Young UniversityInventor: Marc Hansen
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Publication number: 20130157990Abstract: A method of detoxifying a patient addicted to at least one drug comprises the step of administering a first-medication component to the patient for mitigating drug withdrawal symptoms of the patient. The method further comprises the step of administering an anesthetic component to the patient for putting the patient in a sedated state. The method further comprises the step of administering a detoxification component to the patient for detoxifying the patient of the drug(s) while the patient is in the sedated state. The detoxification component can comprise naloxone. The method further comprises the step of administering a second-medication component to the patient for further mitigating drug withdrawal symptoms of the patient while the patient is in the sedated state. The second-medication component can comprise naltrexone. The method further comprises the step of terminating administration of the anesthetic component to the patient for reviving the patient from the sedated state.Type: ApplicationFiled: February 20, 2013Publication date: June 20, 2013Applicant: EAGLE ADVANCEMENT INSTITUTE LLCInventor: EAGLE ADVANCEMENT INSTITUTE LLC
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Publication number: 20130150311Abstract: In one aspect, the present invention is directed to a dry, flowable and compressible composition, useful as a pharmaceutical excipient, which composition comprises a mixture of hydrophobic and hydrophilic poly(ethylene oxide)-polypropylene oxide)-poly(ethylene oxide) block copolymers, and which possesses a Carr index of less than about 20. In other aspects, the present invention is directed a pharmaceutical composition comprising such adjuvant and a pharmaceutically active ingredient; as well as to a method of making the compositions.Type: ApplicationFiled: December 13, 2011Publication date: June 13, 2013Inventors: Grzegorz Pietrzynski, Valery Alakhov, Kishore Patel
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Publication number: 20130143858Abstract: The invention relates to compounds according to Formula I: or a pharmaceutically acceptable salt thereof, wherein m, n, R1, R2, R3, R4, R5, x and y are as defined herein. Compounds according to Formula I are pharmacologically effective as potassium channel inhibitors, in particular inhibitors of the acetylcholine operated inward rectifying potassium channel current (i.e. IKACh blockers), and are believed to be useful in the treatment of cardiac arrhythmias, in particular supraventricular tacharrhythmias, such as atrial fibrillation and atrial flutter.Type: ApplicationFiled: January 28, 2013Publication date: June 6, 2013Applicant: ASTRAZENECA ABInventor: AstraZeneca AB
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Publication number: 20130143924Abstract: The present invention is directed to a non-therapeutical process for deterring vermin, which is based on the usage of the largely known beta amino-alcohol derivatives of formula (I) as described herein. Further, the present invention is directed to corresponding vermin-deterring compositions which contain these substances as the active ingredient, compounds of the formula (I) for the preparation of vermin-deterring compositions, and the use of compounds of formula (I) in the defense against vermin.Type: ApplicationFiled: November 16, 2012Publication date: June 6, 2013Inventors: Pierre DUCRAY, Tania Cavaliero, Maike Lohrmann, Jacques Bouvier
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Patent number: 8455538Abstract: The present invention provides methods of therapy of cognitive deficits associated with a central nervous system disorder or condition, methods of enhancing cognitive performance and methods for repeated stimulation of neuronal activity or a pattern of neuronal activity, such as that underlying a specific neuronal circuit(s). The methods comprise combining cognitive training protocols and a general administration of CREB pathway-enhancing agents.Type: GrantFiled: May 23, 2011Date of Patent: June 4, 2013Assignee: Cold Spring Harbor LaboratoryInventors: Timothy P. Tully, Filippo Cavalieri
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Publication number: 20130137744Abstract: In various embodiments, the present invention provides cycloalkyl pyrrolidine compounds and methods for their use in the treatment and/or prevention of various diseases, conditions and syndromes, including central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.Type: ApplicationFiled: January 28, 2013Publication date: May 30, 2013Applicant: Sunovion Pharmaceutical Inc.Inventor: Sunovion Pharmaceutical Inc.
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Patent number: 8450362Abstract: The invention relates to compounds of formula I: or a pharmaceutically acceptable salt thereof, where R1-3, R5, R7, a, b, Q, X, X?, X?, Y, Z, and Ar are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also relates to 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: GrantFiled: July 11, 2012Date of Patent: May 28, 2013Assignee: Theravance, Inc.Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Cameron Smith
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Patent number: 8450345Abstract: Provided are methods of treating or preventing viral infections caused by or associated with a Dengue virus using iminosugars.Type: GrantFiled: February 22, 2010Date of Patent: May 28, 2013Assignees: The Chancellor, Masters and Scholars of the University of Oxford, United Therapeutics CorporationInventors: Urban Ramstedt, Brennan Klose, Nicole Zitzmann, Raymond A. Dwek, Terry D. Butters
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Publication number: 20130116230Abstract: The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.Type: ApplicationFiled: December 20, 2012Publication date: May 9, 2013Applicant: INCYTE CORPORATIONInventor: Incyte Corporation
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Patent number: 8435564Abstract: The present invention relates to a pharmaceutical composition comprising brivaracetam as active ingredient, the invention relates specifically to a prolonged release formulation.Type: GrantFiled: May 28, 2009Date of Patent: May 7, 2013Assignee: UCB Pharma, S.A.Inventors: Frederic Eeckman, Monique Berwaer, Domenico Fanara
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Publication number: 20130109684Abstract: The present disclosure provides a series of compounds which exhibit isoform selective inhibition of GRP94, a homologue of Hsp90 that is localized to the endoplasmic recticulum. Through GRP94 inhibition, these compounds are likely to manifest anti-cancer, anti-inflammatory, anti-metastasis, and immunosuppressive activities, as well as utility in the treatment of neurodegenerative diseases, and diabetes.Type: ApplicationFiled: April 6, 2012Publication date: May 2, 2013Applicant: University of KansasInventors: Brian S.J. Blagg, Adam S. Duerfeldt
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Patent number: 8431156Abstract: The present invention relates to an oral controlled release pharmaceutical composition in the form of a unit dosage form comprising: (a) a highly soluble high dose active ingredient consisting essentially of therapeutically effective amount of levetiracetam or a pharmaceutically acceptable derivative thereof, and (b) a rate controlling means comprising a rate-controlling agent and/or a coating selected from (i) a active ingredient permeable coating surrounding the unit dosage form, and (ii) an active ingredient impermeable coating covering one or more surfaces but not all the surfaces of the unit dosage form, wherein the composition is in the form of a compact tablet and the levetiracetam or a pharmaceutically acceptable derivative thereof is present in an amount ranging from about 55% to about 90% by weight of the tablet.Type: GrantFiled: February 22, 2006Date of Patent: April 30, 2013Assignee: Sun Pharma Advanced Research Company Ltd.Inventors: Yashoraj Rupsinh Zala, Nitin Bhalachandra Dharmadhikari
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Publication number: 20130102591Abstract: The invention provides compositions and methods for prevention, treatment, or management of pulmonary hypertension using piperidine, pyrrolidine, or azepane derivatives comprising one to four nitric oxide (NO) donor groups and a reactive oxygen species (ROS) degradation catalyst. The invention further provides a water dispersible powder comprising nanoparticles comprising said derivatives, as well as pharmaceutical compositions thereof and methods of use.Type: ApplicationFiled: January 26, 2011Publication date: April 25, 2013Inventors: Andrew Lurie Salzman, Shlomo Magdassi, Katrin Margulis-Goshen
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Patent number: 8425938Abstract: The present invention relates to an oral controlled release pharmaceutical composition in the form of a unit dosage form comprising: (a) a highly soluble high dose active ingredient consisting essentially of therapeutically effective amount of levetiracetam or a pharmaceutically acceptable derivative thereof, and (b) a rate controlling means comprising a rate-controlling agent and/or a coating selected from (i) a active ingredient permeable coating surrounding the unit dosage form, and (ii) an active ingredient impermeable coating covering one or more surfaces but not all the surfaces of the unit dosage form, wherein the composition is in the form of a compact tablet and the levetiracetam or a pharmaceutically acceptable derivative thereof is present in an amount ranging from about 55% to about 90% by weight of the tablet.Type: GrantFiled: May 6, 2011Date of Patent: April 23, 2013Assignee: Sun Pharma Advanced Research Company Ltd.Inventors: Yashoraj Rupsinh Zala, Nitin Bhalachandra Dharmadhikari
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Patent number: 8420693Abstract: The present invention relates to novel Dipyrrole Compounds, compositions comprising a Dipyrrole Compound, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering a Dipyrrole Compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or neoplastic cell, treating or preventing a viral infection, or inhibiting the replication and/or infectivity of a virus. The invention also provides screening assays for compounds that can be used in combination with Dipyrrole Compounds for the treatment of cancer or neoplastic disease, inhibition of cancer cell growth, or treatment of viral infections.Type: GrantFiled: December 22, 2005Date of Patent: April 16, 2013Assignee: Gemin X Pharmaceuticals Canada Inc.Inventors: Giorgio Attardo, Sasmita Triparthy, Elise Rioux, Gerson Gonzalez
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Patent number: 8420694Abstract: A compound represented by the formula (I?): or a salt thereof, has a superior androgen modulating action, wherein R1, R2, R4 to R8, R10 and R11 are defined in the claim.Type: GrantFiled: August 6, 2008Date of Patent: April 16, 2013Assignee: Takeda Pharmaceutical Company LimitedInventor: Atsushi Hasuoka