Bicyclo Ring System Patents (Class 514/657)
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Publication number: 20140057990Abstract: This invention provides a convenient method for converting oximes into enamides. The process does not require the use of metallic reagents. Accordingly, it produces the desired compounds without the concomitant production of a large volume of metallic waste. The enamides are useful precursors to amides and amines. The invention provides a process to convert a prochiral enamide into the corresponding chiral amide. In an exemplary process, a chiral amino center is introduced during hydrogenation through the use of a chiral hydrogenation catalyst. In selected embodiments, the invention provides methods of preparing amides and amines that include the 1,2,3,4-tetrahydro-N-alkyl-1-naphthalenamine or 1,2,3,4-tetrahydro-1-naphthalenamine substructure.Type: ApplicationFiled: August 1, 2013Publication date: February 27, 2014Applicant: SUNOVION PHARMACEUTICALS INC.Inventors: Hang Zhao, Stefan G. Koenig, Charles P. Vandenbossche, Surendra Singh, Harold Scott Wilkinson, Roger P. Bakale
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Publication number: 20140051768Abstract: The invention relates to a medicament containing (S)-2-N-propylamino-5-hydroxytetralin, the salts or prodrugs thereof. As a D3 agonist, (S)-2-N-propylamino-5-hydroxytetralin is suitable particularly for the treatment of dopa-sensitive movement disorders.Type: ApplicationFiled: October 25, 2013Publication date: February 20, 2014Applicant: UCB Pharma GmbHInventors: Dieter Scheller, Klaus Hansen
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Publication number: 20140051767Abstract: This application provides a method of preferentially inhibiting monoamine oxidase A (MAOA) in the brain of a subject relative to in the intestine of the subject comprising parenterally administering to the subject a controlled release formulation comprising a therapeutically effective amount of rasagiline or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: August 16, 2013Publication date: February 20, 2014Applicant: Teva Pharmaceutical Industries, Ltd.Inventors: Cheryl Fitzer-Attas, Rom E. Eliaz, Eran Blaugrund, Aviva Gross, Adi Mayk
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Publication number: 20130345310Abstract: The present invention relates to a solid composition containing at least one pharmaceutically compatible auxiliary ingredient and rasagiline or a pharmaceutically compatible salt thereof as an active ingredient. The invention further relates to a method for producing said solid composition and to a medicine comprising said solid composition.Type: ApplicationFiled: August 14, 2013Publication date: December 26, 2013Applicant: RATIOPHARM GMBHInventors: Katrin Rimkus, Sandra Brueck, Frank Muskulus, Jana Paetz
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Patent number: 8614252Abstract: The subject invention provides crystalline R(+)-N-propargyl-1-aminoindan, pharmaceutical compositions and methods of manufacture thereof.Type: GrantFiled: January 8, 2010Date of Patent: December 24, 2013Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Anton Frenkel, Tamas Koltai
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Patent number: 8609641Abstract: The invention relates to a medicament containing (S)-2-N-propylamino-5-hydroxytetralin, the salts or prodrugs thereof. As a D3 agonist, (S)-2-N-propylamino-5-hydroxytetralin is suitable particularly for the treatment of dopa-sensitive movement disorders.Type: GrantFiled: December 13, 2004Date of Patent: December 17, 2013Assignee: UCB Pharma GmbHInventors: Dieter Scheller, Klaus Hansen
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Publication number: 20130331429Abstract: The present application relates generally to amino tetraline derivative compounds and methods of use, specifically, embodiments including compounds of formula (I) described herein, pharmaceutically acceptable salts and solvates. More specifically, this application relates to amino tetraline derivative compounds and uses of such compounds producing medicaments for the treatment of various disease and conditions including movement disorders and disorders of the central nervous system.Type: ApplicationFiled: August 15, 2013Publication date: December 12, 2013Inventors: Peter Gmeiner, Miriam Ruberg, Harald Huebner
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Publication number: 20130316906Abstract: The invention relates to novel compounds of the formula (I) in which R1, R2, R3, R4, R5, Y, Q and G have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as herbicides and/or pesticides. Moreover, the invention relates to selective herbicidal compositions comprising, firstly, the phenyl-substituted bicyclooctane-1,3-dione derivates and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to increasing the activity of crop protection compositions comprising in particular phenyl-substituted bicyclooctane-1,3-dione derivates by adding ammonium salts or phosphonium salts and, if appropriate, penetrants, to the corresponding compositions, to processes for their preparation and to their use in crop protection as pesticides and/or for preventing unwanted plant growth.Type: ApplicationFiled: October 28, 2011Publication date: November 28, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Alfred Angermann, Stefan Lehr, Guido Bojack, Reiner Fischer, Isolde Häuser-hahn, Ines Heinemann, Elmar Gatzweiler, Christopher Hugh Rosinger, Arnd Voerste, Dieter Feucht
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Publication number: 20130302441Abstract: Methods of treating skin neoplasms using a monoamine oxidase inhibitor, e.g., a propynylaminoindan (such as rasagiline) are provided. Pharmaceutical compositions and kits comprising monoamine oxidase inhibitors are also provided.Type: ApplicationFiled: November 2, 2012Publication date: November 14, 2013Inventors: Susan Meier-Davis, Jianye Wen, Richard D. Hamlin
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Patent number: 8575139Abstract: The invention relates to the field of male and/or female sexual dysfunction. The invention specifically relates to the use of testosterone and a 5-HT1A agonist.Type: GrantFiled: November 2, 2007Date of Patent: November 5, 2013Assignee: Emotional Brain B.V.Inventors: Jan Johan Adriaan Tuiten, Johannes Martinus Maria Bloemers, Robertus Petrus Johannes De Lange
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Patent number: 8569356Abstract: The invention relates to cyclin dependent kinase inhibitor compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions for treating cell proliferative disorders, especially cancer.Type: GrantFiled: October 25, 2006Date of Patent: October 29, 2013Assignee: University of Florida Research Foundation, Inc.Inventors: David A. Ostrov, Brian K. Law, Patrick Corsino
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Patent number: 8569379Abstract: Disclosed are methods of treating olfactory dysfunction by periodically administering a therapeutically effective amount of rasagiline or a pharmaceutically acceptable salt of rasagiline to a subject.Type: GrantFiled: July 27, 2011Date of Patent: October 29, 2013Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Geraldine Petit, Patrik Brundin
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Publication number: 20130253005Abstract: Provided are small molecule inhibitors of ubiquitin specific protease 1 (USP1) activity and methods for their use in treating and characterizing cancers. The small molecule USP1 inhibitors of the invention are particularly useful in the treatment of cancers that are resistant to DNA cross-linking agents.Type: ApplicationFiled: April 29, 2011Publication date: September 26, 2013Applicants: The Brigham and Women's Hospital, Inc., Dana-Farber Cancer Institute, Inc.Inventors: Alan D. D'Andrea, Gregory D. Cuny, Ross L. Stein, Marcie Glicksman, April Case, Jun Xian, David Wilson, Min Huang
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Publication number: 20130251654Abstract: The present invention relates to a pharmaceutical composition for preventing or treating autophagy-related diseases, angiogenic diseases or hypermelanosis, comprising: (a) a pharmaceutically effective amount of an indatraline derivative or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier. The composition of the present invention effectively induces autophagy of cells, and thus is very effective for preventing or treating autophagy-related diseases. In addition, the composition of the present invention inhibits angiogenesis through the mechanism of inhibiting angiogenesis, invasion and metastasis and inhibits melanogenesis, and thus can also be effective for preventing or treating angiogenic diseases or melanin-related diseases.Type: ApplicationFiled: September 6, 2011Publication date: September 26, 2013Inventors: Ho Jeong Kwon, Yoon Sun Cho
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Patent number: 8541475Abstract: The invention provides novel compounds of formulae I and II: that are monoamine oxidase-B inhibitors, which can be useful in treating obesity, diabetes, and/or cardiometabolic disorders (e.g., hypertension, dyslipidemias, high blood pressure, and insulin resistance).Type: GrantFiled: December 31, 2009Date of Patent: September 24, 2013Assignee: Jenrin Discovery, Inc.Inventors: John Francis McElroy, Robert J. Chorvat, Parthasarathi Rajagopalan
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Patent number: 8529928Abstract: Biodegradable polymers incorporating biomolecules and methods of their use are provided. Certain aspects provide biomolecules crosslinked with diglycidyl esters. The disclosed compositions have numerous applications including cellular regeneration, wound healing, and cellular differentiation.Type: GrantFiled: July 6, 2007Date of Patent: September 10, 2013Assignee: Georgia Tech Research CorporationInventors: Yadong Wang, Blaine Zern, Christiane Gumera
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Publication number: 20130225679Abstract: Provided are analgesic compounds, and salts thereof, of formula: (I) wherein A is: (A) Additionally, pharmaceutical formulations and methods of use employing the above compounds are provided.Type: ApplicationFiled: January 13, 2012Publication date: August 29, 2013Applicant: ELI LILLY AND COMPANYInventors: Jean Marie Defauw, Scott Dale Holmstrom, Shuhui Chen, Yang Zhang, Wentao Wu, Xian Peng, Yujuan Ma, Lun Lu
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Publication number: 20130197091Abstract: A method for treating an cancer disease is disclosed comprising administering to a subject a pharmaceutical composition comprising an adrenergic beta-3-receptor blocker.Type: ApplicationFiled: January 30, 2013Publication date: August 1, 2013Inventors: Shuguang LIN, Meng ZHENG
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Publication number: 20130197074Abstract: A method for treating an aging-related disease is disclosed comprising administering to a subject a pharmaceutical composition comprising an adrenergic beta-3-receptor agonist.Type: ApplicationFiled: January 30, 2013Publication date: August 1, 2013Inventors: Shuguang LIN, Meng ZHENG
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Publication number: 20130183278Abstract: The present invention relates to method of identifying whether or not an individual has Parkinson's disease (PD). In particular, the invention relates to a method for identifying whether or not an individual has PD as opposed to another neurodegenerative disease. The method of the invention comprises measuring the concentration of ?-synuclein (?-syn) and the concentration of unphosphorylated tau (tau) and/or phosphorylated tau (p-tau) in a cerebrospinal fluid sample taken from an individual. The method also comprises calculating the ratio of the concentration of tau and/or p-tau to the concentration of ?-syn, and thereby determining whether or not the individual has PD.Type: ApplicationFiled: July 6, 2011Publication date: July 18, 2013Applicant: United Arab Emirates UniversityInventors: Omar El-Agnaf, Lucilla Parnetti, Paolo Calabresi
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Patent number: 8475804Abstract: The invention features compositions, methods, and kits useful for the treatment of filovirus-mediated diseases, e.g., hemorrhagic fever caused by Ebola virus, in an animal.Type: GrantFiled: February 22, 2010Date of Patent: July 2, 2013Assignees: U.S. Army Medical Research and Material Command, Zalicus, Inc.Inventors: Lisa M. Johansen, Joseph Lehár, Benjamin G. Hoffstrom, Gene G. Olinger, Andrea R. Stossel
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Publication number: 20130158125Abstract: Treatment of CNS disorders with (1R,4S)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine; and (1S,4R)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is disclosed. A process for preparing 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is also disclosed. The process includes the preparation of all four isomers of N-[4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydronaphthalen-1-yl]formamide, which are also useful.Type: ApplicationFiled: December 4, 2012Publication date: June 20, 2013Applicant: SUNOVION PHARMACEUTICALS INC.Inventor: SUNOVION PHARMACEUTICALS INC.
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Publication number: 20130150346Abstract: The present disclosure relates to methods of using fatty acid amide hydrolase (FAAH) inhibitors to treat aspects of Parkinson's disease (PD), restless legs syndrome (RLS) and periodic limb movement disorder (PLMD), the use of FAAH inhibitors for the manufacture of medicaments for use in the treatment of PD, RLS and PLMD, as well as pharmaceutically acceptable compositions comprising FAAH inhibitors for use in the treatment of PD, RLS and PLMD.Type: ApplicationFiled: January 7, 2011Publication date: June 13, 2013Applicants: Ironwood Pharmaceutical, Inc.Inventors: James Philip Pearson, Todd G. Milne, Thomas Henry Johnston, Jonathan Michael Brotchie
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Publication number: 20130115264Abstract: A method of treating the symptoms of Parkinson's disease comprises implanting a reservoir-based drug delivery composition into a subject to systemically deliver a therapeutically effective amount of rasagiline to the subject for a long period of time (e.g., one month or one year). The drug delivery composition may include a rate-controlling excipient (e.g., an elastomeric polymer) defining a reservoir containing at least one discrete solid dosage form (e.g., one or more pellets), which includes rasagiline hemitartrate and optionally, a sorption enhancer.Type: ApplicationFiled: October 24, 2012Publication date: May 9, 2013Applicant: Endo Pharmaceuticals Solutions Inc.Inventor: Endo Pharmaceuticals Solutions Inc.
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Publication number: 20130102650Abstract: The present invention relates to a compound having formula (I) wherein: R1 is chosen from the group consisting of: phenyl group, possibly substituted, —CH2—C6H4—R?1 group, R?1 being chosen from the group consisting of: H, —OH, halogen, alkyl, aryl, CHO, —CN, —NO2, —SR?, —OR?, —NR?R?, —CONR?R?, —COOR?, and —NHCOR?, R? and R? representing independently from each other H, an alkyl group or an aryl group, R?1 being preferably in para position, and —CH2—CO—R? group, R? representing an aryl or heteroaryl group, said aryl and heteroaryl groups being possibly substituted, R2 is chosen from the group consisting of: —OH and halogen, and R3, R4, R5 and R6 are in particular H, for its use for the prevention and/or the treatment of bacterial infections.Type: ApplicationFiled: April 8, 2011Publication date: April 25, 2013Inventors: Yap Jean-Bertrand Boum, II, Tamara Basta-Le-Berre, Ursula Liebl, Hannu Myllykallio
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Publication number: 20130089610Abstract: The subject invention provides R(+)-N-methyl-propargyl-aminoindan or a pharmaceutically acceptable salt thereof and a composition containing R(+)-N-propargyl-1(R)-aminoindan or a pharmaceutically acceptable salt thereof, and a compound of R(+)-N-methyl-propargyl-aminoindan or a salt thereof.Type: ApplicationFiled: October 9, 2012Publication date: April 11, 2013Applicant: Teva Pharmaceutical Industries, Ltd.Inventor: Teva Pharmaceutical Industries, Ltd.
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Publication number: 20130089612Abstract: The subject invention provides R(+)-N-formyl-propargyl-aminoindan and a composition containing N-propargyl-1(R)-aminoindan or a pharmaceutically acceptable salt thereof, and a compound of R(+)-N-formyl-propargyl-aminoindan.Type: ApplicationFiled: October 9, 2012Publication date: April 11, 2013Applicant: TEVA PHARMACEUTICAL INDUSTRIES, LTD.Inventor: TEVA PHARMACEUTICAL INDUSTRIES, LTD.
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Publication number: 20130072884Abstract: Transdermal compositions are provided. Aspects of the transdermal compositions include: an active agent layer and a conversion layer, where the conversion layer includes a weak base and, optionally, a carboxylated component. Also provided are methods of using the transdermal compositions and kits containing the transdermal compositions.Type: ApplicationFiled: March 22, 2012Publication date: March 21, 2013Inventors: Richard Hamlin, Jianye Wen
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Publication number: 20130046023Abstract: A pharmaceutical composition, comprising a GluR2-lacking AMPAR antagonist as an active ingredient, is effective for preventing or treating mental diseases selected from the group consisting of posttraumatic stress disorder (PTSD), drug addiction, and phobia.Type: ApplicationFiled: October 24, 2012Publication date: February 21, 2013Applicant: SNU R&DB FOUNDATIONInventor: SNU R&DB Foundation
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Patent number: 8377992Abstract: The present invention embraces compounds selected for interacting with the T-pocket of telomerase and use thereof for modulating the activity of telomerase and preventing or treating diseases or conditions associated with telomerase.Type: GrantFiled: February 8, 2010Date of Patent: February 19, 2013Assignee: The Wistar InstituteInventor: Emmanuel Skordalakes
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Patent number: 8354451Abstract: Methods of inhibiting phagolysosomal fusion in patients infected with a microorganism involve the administration of a 4-hydroxyphenylpyruvate dioxygenase (HPPD)-inhibiting compound, such as 2-(2-nitro-4-trifluoromethylbenzoyl)-1,3-cyclohexanedione (NTBC) to the patient. A HPPD-inhibiting compound administered in an amount effective to enhance phagolysosomal fusion in the macrophages or neutrophils of the patient reduces or treats the infection. Methods for treating bacterial infections by administering a HPPD-inhibiting compound and reducing the production of pyomelanin or melanin in microorganisms are disclosed.Type: GrantFiled: March 9, 2010Date of Patent: January 15, 2013Assignee: The UWM Research Foundation, Inc.Inventors: Graham R. Moran, Panqing He
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Publication number: 20120329789Abstract: Pharmaceutical compositions for treating Alzheimer's disease are disclosed. The pharmaceutical compositions include a compound having the general formula: and a pharmaceutically acceptable carrier. Methods for treating Alzheimer's disease, inhibiting ATase I and/or ATase 2, reducing the activity of BACE1, reducing the level of amyloid ?-peptide (A?), and/or reducing the level of APP intracellular domain peptide (AICD) by administering such compositions are also disclosed.Type: ApplicationFiled: May 31, 2012Publication date: December 27, 2012Applicant: Wisconsin Alumni Research FoundationInventor: Luigi Puglielli
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Publication number: 20120329800Abstract: Administration of a monoamine oxidase inhibitor is useful in the prevention and treatment of muscle dystrophy. Methods and compositions for inhibiting the production of reactive oxygen species in a muscle cell overproducing reactive oxygen species are provided herein.Type: ApplicationFiled: June 22, 2011Publication date: December 27, 2012Inventors: Paolo Bonaldo, Marcella Canton, Fabio DiLisa, Sara Menazza
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Patent number: 8338489Abstract: The present disclosure relates the use of a beta blocker for the manufacture of a medicament for the treatment of hemangiomas, for example of infantile hemangiomas. The beta blocker may be a non-selective beta-blocker, for example propranolol. The present disclosure provides an alternative to the known compounds, e.g. corticosteroids, interferon or vincristine, generally used for the treatment of hemangiomas.Type: GrantFiled: October 16, 2008Date of Patent: December 25, 2012Assignee: Université Victor Segalen—Bordeaux 2Inventors: Christine Léauté-Labrèze, Éric Dumas De La Roque, Alain Taieb, Jean-Benoît Thambo
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Publication number: 20120301542Abstract: The present invention provides various pharmaceutical compositions, in particular for oral administration, formulated for extended release of active compounds useful in the treatment of neurodegenerative diseases, in particular Parkinson's disease, and injuries to the nervous system. The active compound comprised within these compositions is preferably selected from N-propargyl-1-aminoindan, an enantiomer thereof, or a pharmaceutically acceptable salt thereof, more preferably rasagiline or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: February 3, 2011Publication date: November 29, 2012Applicant: Pharma Two B Ltd.Inventors: Yoram Sela, Nurit Livnah, Itschak Lamensdorf, Tomer Madmon
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Publication number: 20120269906Abstract: The invention concerns methods of treating suicidal ideation or behavior in a subject in need thereof, comprising decreasing endogenous nicotinic acetylcholine receptor (nAChR) activity in the subject; therapeutic packages for treating suicidal ideation or behavior; and methods for determining the efficacy of a treatment for suicidal ideation or behavior. In some embodiments, the treatment methods comprise administering to the subject an effective amount of an inhibitor of a nAChR, such as a lithium compound, mecamylamine, clozapine, or asenapine.Type: ApplicationFiled: October 15, 2010Publication date: October 25, 2012Applicant: University of South FloridaInventors: David Vincent Sheehan, Roland Douglas Shytle
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Publication number: 20120263789Abstract: Disclosed are formulations which are designed to delay release of rasagiline while maintaining specific pharmacokinetic properties.Type: ApplicationFiled: June 29, 2012Publication date: October 18, 2012Inventors: Muhammad Safadi, Daniella Licht, Rachel Cohen, Anton Frenkel, Marina Zholkovsky
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Publication number: 20120265158Abstract: A method for preparing a transdermal patch comprising a substrate layer is provided, the method comprising the steps of contacting an active pharmaceutical ingredient with a retaining means to provide a composition, applying the composition obtained in step (a) to a carrier material to form a substrate layer of the transdermal patch, wherein the retaining means remain within the final transdermal patch.Type: ApplicationFiled: September 9, 2010Publication date: October 18, 2012Applicant: LABTEC GMBHInventors: Sebastian Braun, Armin Breitenbach, Ulrich Becker
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Publication number: 20120238636Abstract: This invention provides a solid pharmaceutical composition comprising rasagiline or a pharmaceutically acceptable salt of rasagiline, and particles having a non-filamentous microstructure of at least two sugar alcohols. This invention also provides a solid pharmaceutical composition comprising rasagiline or a pharmaceutically acceptable salt of rasagiline, a mixture of a disintegrant, a flow agent and particles having a non-filamentous microstructure of at least two sugar alcohols, a supplemental sugar alcohol, a supplemental flow agent, and a supplemental disintegrant. This invention further provides a method of treating a subject afflicted with Parkinson's disease comprising administering to the subject a therapeutically effective amount of the solid pharmaceutical composition, thereby treating the subject. Finally, this invention provides a process of making such solid pharmaceutical compositions.Type: ApplicationFiled: October 21, 2011Publication date: September 20, 2012Inventors: Shulamit Patashnik, Daniella Licht, Adrian Gilbert
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Publication number: 20120214877Abstract: The present invention provides a stable composition of rasagiline comprising an effective dosage of rasagiline or its pharmaceutically acceptable salts and an antioxidant used as a stabilizer. The dosage forms of the composition are pharmaceutically common transdermal-drug delivery dosage form and mucoadhesive delivery dosage form, such as patch, gel, ointment, cream, cataplasm, film, spray and solution, etc. The composition can be used to prevent or treat mental disorders.Type: ApplicationFiled: October 28, 2010Publication date: August 23, 2012Applicant: Chongqing Pharmaceutical Research Institute Co., Ltd.Inventors: Jialiang Lin, Jie Deng, Hao Chen, Tao Zhang
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Publication number: 20120208892Abstract: A method of treating or preventing emesis through the administration of an effective dosage of a 2-(amino) tetralin compound in which one of the S or R enantiomers of the 2-(amino) tetralin compound is present in the composition in excess of the other enantiomer, and compositions comprising such a 2-(amino) tetralin compound in which the ratio of the S and R enantiomers is at least 2:1.Type: ApplicationFiled: October 15, 2010Publication date: August 16, 2012Applicant: EPIOMED THERAPEUTICS, INC.Inventors: David Helton, James Lucot
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Patent number: 8236845Abstract: The present invention relates to heterocyclyl-substituted-tetrahydro-naphthalen-amine compounds of general formula (I) and compositions thereof, methods for their preparation, and the use of said compounds for the treatment or prophylaxis of various disorders of humans or animals.Type: GrantFiled: March 28, 2008Date of Patent: August 7, 2012Assignee: Laboratorios del Dr. Esteve, S.A.Inventors: Monica Garcia-Lopez, Antonio Torrens-Jover, Helmut H. Buschmann
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Publication number: 20120196852Abstract: The invention is directed towards novel naphthoquinone and naphthothiazole compounds, and methods of treating disorders related to MetAP, including tuberculosis and bacterial infection, using various naphthoquinone, hydroxyquinonline, and naphthothiazole compounds.Type: ApplicationFiled: August 5, 2010Publication date: August 2, 2012Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: Jun O. Liu, Omonike Arike Olaleye, Shridhar Bhat
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Publication number: 20120196894Abstract: The present invention relates to compositions and methods that modulate at least one TRP family member. Specifically, the present invention relates to novel TRPA1 antagonists and their use in the treatment of pain such as chronic inflammatory and neuropathic pain. Compounds that can modulate one or more TRPA1 functions are useful in many aspects including, but not limited to, maintaining calcium homeostasis; maintaining sodium homeostasis; modulating intracellular calcium levels; modulating membrane polarization (membrane potential); modulating cation levels; and/or treating or preventing diseases, disorders, or conditions associated with calcium homeostasis, sodium homeostasis, calcium or sodium dyshomeostasis, or membrane polarization/hyperpolarization (including hypo and hyperexcitability), and/or treating or preventing diseases, disorders, or conditions associated with regulation or misregulation of TRPA1 expression or function.Type: ApplicationFiled: September 28, 2010Publication date: August 2, 2012Inventors: Mark T. Bilodeau, Melissa Egbertson, Ahren Green, John C. Hartnett, Yiwei Li
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Publication number: 20120190652Abstract: The present invention relates to method of identifying whether or not an individual has Parkinson's disease (PD). In particular, the invention relates to a method for identifying whether or not an individual has PD in the pre-symptomatic phase of the disease or to distinguishing PD from another neurological disorder. The method of the invention comprises measuring the amount of soluble ?-synuclein oligomers in a cerebrospinal fluid sample taken from an individual. The method optionally also comprises measuring the total amount of ?-synuclein in the CSF sample, calculating the ratio of the amount of ?-synuclein oligomers to the total amount of ?-synuclein, and thereby determining whether or not the individual has PD. The method of the invention can be used in clinical trials to measure the effect of drugs in both PD animal models and human PD patients.Type: ApplicationFiled: September 13, 2010Publication date: July 26, 2012Applicant: United Arab Emirates UniversityInventor: Omar El-Agnaf
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Publication number: 20120165360Abstract: The invention provides amino- and amido-aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, and n are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: March 5, 2012Publication date: June 28, 2012Applicant: THERAVANCE, INC.Inventors: Sean G. Trapp, Michael R. Leadbetter, Daniel D. Long, Lan Jiang, Sabine Axt
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Publication number: 20120149693Abstract: The invention relates to protein binding interacting/binding compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating 5-HT2C and/or RSK disorders, including diseases and disorders mediated by GPCRs and/or RSKs.Type: ApplicationFiled: May 5, 2010Publication date: June 14, 2012Applicant: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC.Inventor: Raymond G. Booth
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Publication number: 20120136065Abstract: Treatment of CNS disorders with (1R,4S)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine; and (1S,4R)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is disclosed. A process for preparing 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is also disclosed. The process includes the preparation of all four isomers of N-[4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydronaphthalen-1-yl]formamide, which are also useful.Type: ApplicationFiled: February 3, 2012Publication date: May 31, 2012Applicant: SUNOVION PHARMACEUTICALS INC.Inventors: Thomas P. JERUSSI, Qun Kevin FANG, Mark G. CURRIE
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Publication number: 20120129798Abstract: The present invention is directed to a crosslinked or non-crosslinked polymer particle, wherein the crosslinked polymer particle comprises a copolymer of poly(alklyene glycol-graft-acrylate) that is crosslinked by at least one hydrolysable monomer or crosslinking agent. The present invention is also directed to a polymer particle comprising a crosslinked polymer particle that is a product of starting materials comprising (a) a hydrophilic monomer, (b) a hydrophobic monomer, and (c) a hydrolysable crosslinking agent (the crosslinking agent may be absent in the case of non-crosslinked particles). The present invention is still further directed to a polymer particle comprising a crosslinked copolymer, where the crosslinked copolymer includes structures represented by Formulas (I), (II), and (III), as defined in the specification. Other embodiments of the present invention also include methods of manufacturing polymer particles.Type: ApplicationFiled: November 23, 2010Publication date: May 24, 2012Inventors: Emmanuel AKALA, Oluyomi Okunola
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Publication number: 20120129775Abstract: Methods of inhibiting undesired angiogenesis are provided, which methods include administering to a subject a therapeutically effective amount of at least one of the compounds described herein, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: July 30, 2010Publication date: May 24, 2012Inventors: Enrique Zudaire, Marta Aparicio, Frank Cuttitta