Tropanes (including Nor Or Dehydro Form) Patents (Class 514/304)
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Publication number: 20130315981Abstract: The present invention is a method of increasing lipolysis in an adipose tissue of a mammal comprising delivering to macrophages at the adipose tissue of the mammal an effective amount of an agent which reduces the concentration of macrophages at the adipose tissue of the mammal, thereby increasing lipolysis in the adipose tissue of the mammal.Type: ApplicationFiled: June 22, 2011Publication date: November 28, 2013Applicant: The Trustees of Columbia University in the City of New YorkInventors: Anthony W. Ferrante, JR., Aliki Kosteli
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Patent number: 8592395Abstract: The present invention relates to compounds of Formula (I) and (Ia) useful in the treatment of CCR5-related diseases and disorders, for example, the prevention or treatment of an HIV infection, and in the treatment of the resulting acquired immune deficiency syndrome (AIDS).Type: GrantFiled: July 23, 2010Date of Patent: November 26, 2013Assignee: GlaxoSmithKline LLCInventors: Maosheng Duan, Wieslaw Mieczyslaw Kazmierski, Matthew Tallant
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Publication number: 20130310379Abstract: Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.Type: ApplicationFiled: November 21, 2011Publication date: November 21, 2013Applicant: CONSTELLATION PHARMACEUTICALSInventors: Brian K. Albrecht, James Edmund Audia, Alexandre Gagnon, Jean-Christophe Harmange, Christopher G. Naveschuk
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Publication number: 20130309215Abstract: A pharmaceutical composition for application in human and animals, with at least one systemically and/or locally acting, topically applicable active ingredient and with at least one phospholipid, improving the transport of the active ingredient trough the cell membrane and containing a concentration of at least 60% by weight phosphatidylcholine, referring to the phospholipid, is described. The composition shows such a liquid consistency, that it is able to be sprayed as droplets or as a foam, whereas in the composition such a phospholipid is included, that additionally contains oil in a concentration of maximum 7.5% by weight besides the at least 60% by weight phosphatidylcholine.Type: ApplicationFiled: August 10, 2012Publication date: November 21, 2013Applicant: MIKA Pharma Gesellschaft fur die Entwicklung und Vermarktung pharmazeutischer Produkte mbHInventor: Bernd G. SEIGFRIED
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Patent number: 8586620Abstract: The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing conditions such as, for example, stroke, reperfusion injury, neurodegeneration, head trauma, CABG, migraine headache with and without aura, migraine with allodynia, central post-stroke pain (CPSP), neuropathic pain, morphine/opioid induced tolerance and hyperalgesia.Type: GrantFiled: May 6, 2011Date of Patent: November 19, 2013Assignee: NeurAxon, Inc.Inventors: Shawn Maddaford, Jailall Ramnauth, Suman Rakhit, Joanne Patman, Paul Renton, Subhash C. Annedi
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Publication number: 20130303570Abstract: The present invention relates to modulators of cystic fibrosis transmembrane conductance regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using modulators of CFTR.Type: ApplicationFiled: July 17, 2013Publication date: November 14, 2013Inventors: Hayley Binch, Lev T.D. Fanning, Dennis Hurley, Urvi Sheth, Alina Silina, Xiaoqing Yang, Martyn Botfield, Peter D.J. Grootenhuis, Fredrick Van Goor, Mehdi Michel Djamel Numa
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Publication number: 20130303512Abstract: This disclosure is directed, in part, to a method of determining whether a subject having cancer is at risk for developing metastasis of the cancer. In one embodiment, the method comprises (a) obtaining a biological sample from the subject having cancer; (b) determining CCR5 expression level and/or expression level of at least one of CCR5 ligands in the biological sample; and (c) if the expression level of CCR5 and/or of at least one of CCR5 ligands determined in step (b) is increased compared to CCR5 expression level and/or expression level of at least one of CCR5 ligands in a control sample, then the subject is identified as likely at risk for developing metastasis of the cancer.Type: ApplicationFiled: May 14, 2013Publication date: November 14, 2013Inventor: Richard G. PESTELL
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Publication number: 20130295049Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: October 30, 2012Publication date: November 7, 2013Applicant: ENANTA PHARMACEUTICALS, INCInventor: ENANTA PHARMACEUTICALS, INC
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Patent number: 8575192Abstract: The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.Type: GrantFiled: March 1, 2012Date of Patent: November 5, 2013Assignee: Theravance, Inc.Inventors: Daniel Marquess, Paul R. Fatheree, S. Derek Turner, Daniel D. Long
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Publication number: 20130281428Abstract: Novel compounds or salts thereof, or crystals thereof, which inhibit Axl and are useful for treating diseases caused by Axl hyperfunction, diseases associated with Axl hyperfunction and/or diseases accompanied by Axl hyperfunction are provided. Pyridone derivatives represented by the formula (1) having various substituents or salts thereof, or crystals thereof (where R1, R2, R3, R5, R6, A, W, X and n in the formula (1) are as defined in the specification, respectively) are provided.Type: ApplicationFiled: January 30, 2013Publication date: October 24, 2013Inventors: Hitoshi Ohki, Masahiro Ota, Kosuke Takeuchi, Hideaki Watanabe, Akitake Yamaguchi, Yoshihiro Shibata, Yuichi Tominaga, Takeshi Jimbo, Keijiro Kobayashi, Katsuhiro Kobayashi, Daisuke Fukatsu
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Publication number: 20130281485Abstract: The present invention is directed to synthetic bridged bicyclic compounds that are inhibitors of rho-associated protein kinase. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with cytoskeletal reorganization. The method comprises administering to a subject a therapeutically effective amount of a Rho kinase inhibitory compound of Formula I, wherein said amount is effective to influence the actomyosin interactions, for example, by leading to cellular relaxation and alterations in cell-substratum adhesions. In one embodiment, the method treats increased intraocular pressure, such as primary open-angle glaucoma.Type: ApplicationFiled: June 14, 2013Publication date: October 24, 2013Inventors: John W. Lampe, Paul S. Watson, David J. Slade
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Patent number: 8557842Abstract: The invention provides novel cocaine analogs. The invention also provides a method of preparing cocaine analogs with control over the substituents installed at the C-1, C-2, C-3, C-4 and N-8 positions of the tropane bicyclic scaffold. The invention further provides methods of providing anesthesia, blocking reuptake of a monoamine neurotransmitter, and treating depression, by administering to a subject in need of such treatment a pharmaceutical composition comprising a compound of the invention.Type: GrantFiled: May 18, 2012Date of Patent: October 15, 2013Assignee: Temple University—Of the Commonwealth System of Higher EducationInventors: Franklin A. Davis, Naresh Theddu, Maarten E. A. Reith
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Publication number: 20130267506Abstract: Compositions for therapy of a diabetic symmetrical polyneuropathy a subject in need thereof, the compositions comprising: an effective amount of a muscarinic acetylcholine receptor antagonist exemplified by pirenzepine, telenzepine, atropine, or derivatives thereof or salts thereof or analogs thereof or derivatives thereof, and a pharmacologically acceptable carrier. The composition may be injectable or alternatively, may be applied topically or alternatively, may be delivered orally. A suitable topical composition may comprise a lotion, a cream, a gel, or a viscous fluid. The muscarinic acetylcholine receptor antagonist may be a muscarinic acetylcholine receptor antagonist salt or a muscarinic acetylcholine receptor antagonist derivative or a muscarinic acetylcholine receptor antagonist analog.Type: ApplicationFiled: October 24, 2011Publication date: October 10, 2013Applicant: UNIVERSITY OF MANITOBAInventors: Paul Fernyhough, Nigel A. Calcutt, Lakshmi Kotra
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Publication number: 20130261129Abstract: Disclosed herein are chemokine receptor antagonists of formula (I) wherein R1, R2, and R3 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.Type: ApplicationFiled: March 29, 2013Publication date: October 3, 2013Applicant: AbbVie Inc.Inventors: Michael D. Meyer, Xueqing Wang, Tao Guo, Robert Wei, Lijuan Jane Wang
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Publication number: 20130252945Abstract: An amorphous formulations of a pharmaceutical includes a composition of the formula [A]x[MpClq]y, the composition being an ionic liquid with a melting temperature below 150° C., wherein [MpClq] is a metal chloride, x is 1, 2, 3, or 4, p is 1, 2, 3, or 4, q is 1, 2, 3, 4, 5, 6, 7, 8, or 9, and y is 1 or 2, wherein each A is a cation that is a pharmaceutical or a cation precursor that is a pharmaceutical.Type: ApplicationFiled: March 25, 2013Publication date: September 26, 2013Inventors: Katherine Lovejoy, Rico Del Sesto, Andrew Koppisch
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Publication number: 20130231311Abstract: Systems and methods are described for treating un-met medical needs in migraine and related conditions such as cluster headache. Included are treatments that are both rapid onset and long acting, which include sustained release formulations, and combination products. Also included are treatments for multiple symptoms of migraine, especially headache and nausea and vomiting. Systems that are self contained, portable, prefilled, and simple to self administer at the onset of a migraine attack are disclosed, and preferably include a needle-free injector and a high viscosity formulation, to eliminate such issues as fear of self administration with needles, and needle stick and cross contamination.Type: ApplicationFiled: April 16, 2013Publication date: September 5, 2013Inventors: Stephen J. FARR, John TURANIN, Roger HAWLEY, Jeffrey A. SCHUSTER
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Publication number: 20130224291Abstract: Methods and compositions for reducing the frequency of urination are disclosed. One method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising an analgesic agent formulated in a delayed-release formulation. Another method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising multiple active ingredients. Yet another method comprises administering to a subject in need thereof an effective amount of a diuretic followed with another administration of an pharmaceutical composition comprising an analgesic agent.Type: ApplicationFiled: March 20, 2013Publication date: August 29, 2013Applicant: WELLESLEY PHARMACEUTICALS, LLCInventor: Wellesley Pharmaceuticals, LLC
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Patent number: 8518966Abstract: The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula wherein R1, R2, R3, and a 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: GrantFiled: January 31, 2011Date of Patent: August 27, 2013Assignee: Theravance, Inc.Inventors: Daniel D. Long, Daisuke Roland Saito, Priscilla M. Van Dyke, Lan Jiang, Timothy J. Church, John R. Jacobsen
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Publication number: 20130217620Abstract: The present invention relates to ionic silicone hydrogel contact lenses which comprise at least one pharmaceutical or nutriceutical component and are formed from reaction mixtures comprising a mixture of slow-reacting hydrophilic monomers, including at least one slow-reacting ionic monomer, at least one silicone-containing component and at least one hydroxyl-containing component, wherein the ratio of the slow-reacting hydrophilic component half lives to the silicone-containing component half life is at least 2.Type: ApplicationFiled: March 14, 2013Publication date: August 22, 2013Applicant: Johnson & Johnson Vision Care, Inc.Inventor: Johnson & Johnson Vision Care, Inc.
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Publication number: 20130216620Abstract: Methods and compositions for reducing the frequency of urination are disclosed. One method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising an analgesic agent formulated in an extended-release formulation. Another method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising multiple active ingredients formulated for extended-release. Yet another method comprises administering to a subject in need thereof an effective amount of a diuretic followed with another administration of a pharmaceutical composition comprising an analgesic agent formulated for extended-release.Type: ApplicationFiled: March 20, 2013Publication date: August 22, 2013Applicant: WELLESLEY PHARMACEUTICALS, LLCInventor: Wellesley Pharmaceuticals, LLC
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Patent number: 8513282Abstract: The present invention relates to modulators of cystic fibrosis transmembrane conductance regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using modulators of CFTR.Type: GrantFiled: October 23, 2009Date of Patent: August 20, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Hayley Binch, Lev T. D. Fanning, Dennis Hurley, Urvi Sheth, Alina Silina, Xiaoqing Yang, Martyn Botfield, Peter D. J. Grootenhuis, Fredrick Van Goor, Mehdi Michel Djamel Numa
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Publication number: 20130202529Abstract: Disclosed are benztropine analogs having the formula (I) in which Ar is a C6-C20 monocyclic aryl group or a C10-C20 bicyclic aryl group or a heteroaryl, heterocyclic, or arylheterocyclic group having 2 to 12 carbon atoms and one or more heteroatoms selected from the group consisting of N, O, S, P, and any combination thereof; m=1 to 5; n=1 to 3; and R1 to R4 are as described in the specification; or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical compositions and use thereof, e.g., in treating mental disorders.Type: ApplicationFiled: January 11, 2013Publication date: August 8, 2013Applicant: The United States of America, as represented by the Secretary, Department of Health and HumanInventor: The United States of America, as represented by the Secretary, Department of Health and Human Services
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Publication number: 20130197027Abstract: In one aspect, the invention relates to compounds which are useful as allosteric or bitopic agonists of the M1 muscarinic receptor; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurodegenerative diseases, including Alzheimer's Disease. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: March 10, 2011Publication date: August 1, 2013Inventors: Craig Lindsley, P. Jeffrey Conn, Colleen M. Niswender, Michael R. Wood, Brian Chauder, Evan P. Lebois
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Publication number: 20130196952Abstract: The invention relates to compounds of Formula (1) and to processes for the preparation of intermediates used in the preparation of compositions containing and the uses of such derivatives. The compounds according to the present invention are useful in numerous diseases in which ALK protein is involved or in which inhibition of ALK activity may induce benefit, especially for the treatment of cancer mediated by a mutated EML4-ALK fusion protein.Type: ApplicationFiled: May 4, 2011Publication date: August 1, 2013Applicant: PFIZER INC.Inventors: Mark Edward Bunnage, Andrew Simon Cook, Jingrong Jean Cui, Kevin Nell Dack, Judith Gail Deal, Danlin Gu, Mingying He, Patrick Stephen Johnson, Ted William Johnson, Phuong Thi Quy Le, Cynthia Louise Palmer, Hong Shen
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Publication number: 20130190351Abstract: This invention relates to bicyclic amide compounds, pharmaceutical compositions and methods for use in the prevention and treatment of a variety of conditions and/or disease states including cerebral insufficiency, through the enhancement of receptor functioning in synapses in brain networks responsible for basic and higher order behaviors as defined herein. These brain networks, which are involved in regulation of breathing, and cognitive abilities related to memory impairment, such as is observed in a variety of dementias, in imbalances in neuronal activity between different brain regions, as is suggested in disorders such as Parkinson's disease, schizophrenia, respiratory depression, sleep apneas, attention deficit hyperactivity disorder and affective or mood disorders, and in other disorders wherein a deficiency in neurotrophic factors is implicated, as well as other disorders as described herein.Type: ApplicationFiled: July 25, 2012Publication date: July 25, 2013Applicant: CORTEX PHARMACEUTICALS, INC.Inventors: Rudolf Mueller, Leslie Street
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Publication number: 20130190381Abstract: The present invention provides methods and compounds for treating viral infections using modulators of host cell enzymes relating to long chain fatty acid and lipid droplet metabolism. It includes a method of treating viral infections using triacsin C and its relatives, analogues and derivatives as well as other inhibitors of long chain fatty acid metabolism and lipid droplet metabolism.Type: ApplicationFiled: February 18, 2011Publication date: July 25, 2013Applicant: THE TRUSTEES OF PRINCETON UNIVERSITYInventors: Emre Koyuncu, Joshua D. Rabinowitz, Thomas Shenk
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Patent number: 8481563Abstract: The invention provides 8-azabicyclo[3.2.1]octyl-2-hydroxybenzamide compounds of formula (I): wherein R2, R7, and m 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: GrantFiled: January 26, 2011Date of Patent: July 9, 2013Assignee: Theravance, Inc.Inventors: Daisuke Roland Saito, Daniel D. Long, Priscilla Van Dyke, Timothy J. Church, Lan Jiang, Bryan Frieman
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Publication number: 20130172327Abstract: Disclosed are N-1-cyano-2-(phenyl)ethyl)-2-azabicyclo[2.2.1]heptane-3-carboxamides of formula I and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of respiratory diseases.Type: ApplicationFiled: September 14, 2012Publication date: July 4, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Marc GRUNDL, Thorsten OOST, Alexander PAUTSCH, Stefan PETERS, Doris RIETHER, Wolfgang WIENEN
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Patent number: 8476295Abstract: The present invention is directed to synthetic bridged bicyclic compounds that are inhibitors of rho-associated protein kinase. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with cytoskeletal reorganization. The method comprises administering to a subject a therapeutically effective amount of a Rho kinase inhibitory compound of Formula I, wherein said amount is effective to influence the actomyosin interactions, for example, by leading to cellular relaxation and alterations in cell-substratum adhesions. In one embodiment, the method treats increased intraocular pressure, such as primary open-angle glaucoma.Type: GrantFiled: December 10, 2010Date of Patent: July 2, 2013Assignee: InspireInventors: John W. Lampe, Paul S. Watson, David J. Slade
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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: 20130158060Abstract: The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I): wherein R1, R2, R3, A, and G are defined in the specification, or a pharmaceutically-acceptable salt or solvate 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: June 20, 2012Publication date: June 20, 2013Applicant: THERAVANCE, INC.Inventors: Daniel D. Long, John R. Jacobsen, Lan Jiang
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Publication number: 20130158071Abstract: The present invention relates to pharmaceutical compositions comprising a compound of Formula I in combination with one or both of a Compound of Formula II and/or a Compound of Formula III. The invention also relates to solid forms and to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis.Type: ApplicationFiled: October 22, 2012Publication date: June 20, 2013Applicant: Vertex Pharmaceuticals IncorporatedInventor: Vertex Pharmaceuticals Incorporated
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Publication number: 20130150377Abstract: The invention relates to tetrahydropyridinyl and dihydropyrrolyl compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein X, Y, Z, R1, R2, m, and n are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.Type: ApplicationFiled: November 13, 2012Publication date: June 13, 2013Applicants: SHIONOGI & CO., LTD., PURDUE PHARMA, L.P.Inventors: PURDUE PHARMA, L.P., SHIONOGI & CO., LTD.
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Publication number: 20130149388Abstract: Chronic obstructive pulmonary disease (COPD), characterized by chronic airflow limitation, is a serious and growing public health concern. The major environmental risk factor for COPD is cigarette smoking, but the biological mechanisms underlying COPD are not well understood. Herein, proton nuclear magnetic resonance (1H-NMR) spectroscopy is used in methods to identify metabolites and biomarkers associated with lung function in COPD.Type: ApplicationFiled: July 3, 2012Publication date: June 13, 2013Inventors: Joseph Louie MCCLAY, Barbara K. ZEDLER, Edward Lenn MURRELLE, Edwin J.C.G. VAN DEN OORD, Thomas O'CONNELL, Daniel ADKINS
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Patent number: 8450339Abstract: New stable compositions comprising the combination of a topically active vasoconstrictor and a topically active anticholinergic drug are disclosed. Preferably, the composition comprises ipratropium or a salt thereof in combination with xylometazoline hydrochloride and a salt thereof. Upon topically administering such compositions to a nasal mucosa in individuals suffering from the common cold the symptoms of rhinorrhea are significantly reduced.Type: GrantFiled: December 11, 2009Date of Patent: May 28, 2013Assignee: Takeda Pharma A/SInventors: Hanne Anette Moesgaard, Karin Lowenstein Christensen
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Patent number: 8449863Abstract: Uncoated particles of reversed cubic phase or reversed hexagonal phase material containing an active disposed within are provided. The uncoated particles have an ionic charge that is sufficient to stabilize them in dispersion in a liquid, e.g. a polar solvent. The active that is disposed within the particles may be, for example, a pharmaceutical or nutriceutical compound.Type: GrantFiled: March 25, 2010Date of Patent: May 28, 2013Assignee: Lyotropic Therapeutics, Inc.Inventor: David Anderson
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Patent number: 8445015Abstract: Methods and compositions for reducing the frequency of urination are disclosed. One method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising an analgesic agent formulated in an extended-release formulation. Another method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising multiple active ingredients formulated for extended-release. Yet another method comprises administering to a subject in need thereof an effective amount of a diuretic followed with another administration of a pharmaceutical composition comprising an analgesic agent formulated for extended-release.Type: GrantFiled: July 27, 2012Date of Patent: May 21, 2013Assignee: Wellesley Pharmaceuticals, LLCInventor: David A. Dill
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Patent number: 8445011Abstract: Methods and compositions for reducing the frequency of urination are disclosed. One method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising an analgesic agent formulated in a delayed-release formulation. Another method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising multiple active ingredients. Yet another method comprises administering to a subject in need thereof an effective amount of a diuretic followed with another administration of an pharmaceutical composition comprising an analgesic agent.Type: GrantFiled: July 27, 2012Date of Patent: May 21, 2013Assignee: Wellesley Pharmaceuticals, LLCInventor: David A. Dill
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Patent number: 8445690Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: GrantFiled: February 16, 2011Date of Patent: May 21, 2013Assignee: Janssen Pharmaceutica NVInventors: Gilles Bignan, Micheal Gaul, Guozhang Xu, Bao-Ping Zhao
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Publication number: 20130123268Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3,3-disubstituted-(8-aza-bicyclo[3.2.1]oct-8-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone, 3,3-disubstituted-(6-aza-bicyclo[3.1.1]hept-6-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone, and 4,4-disubstituted piperidin-1-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone compounds of the following formula that, inter alia, inhibit 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1).Type: ApplicationFiled: March 10, 2011Publication date: May 16, 2013Applicant: THE UNIVERSITY OF EDINBURGHInventors: Scott Peter Webster, Jonathan Robert Seckl, Brian Robert Walker, Peter Ward, Thomas David Pallin, Hazel Joan Dyke, Trevor Robert Perrior
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Publication number: 20130123298Abstract: Pharmaceutical composition for the prevention of perioperative arterial hypotension in humans comprising noradrenaline for intravenous administration.Type: ApplicationFiled: July 27, 2011Publication date: May 16, 2013Applicant: LABORATOIRE AGUETTANTInventor: Jean-Michel Julia
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Publication number: 20130123243Abstract: This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.Type: ApplicationFiled: October 18, 2012Publication date: May 16, 2013Inventor: Celtaxsys, Inc.
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Patent number: 8436208Abstract: A process for the preparation of a substituted 2,2?-dithiophene is described, which process comprises the steps (a), (c) and optional steps (b) and (d): a reaction of a compound of the formula: with a suitable lithium organic compound, preferably Li-alkyl or Li-alkylamide; b) optional exchange of lithium against another metal selected from Mg1 Zn and Cu; c) reaction of the metallated intermediate obtained in step (a) or (b) with a suitable electrophil, which is CO2 or an aldehyde (addition reaction), or a compound Y?—R17 or Y?—R18-Z (substitution reaction), where R17 and R18 are as defined in claim 1; and optionally d) modification of the product obtained in step (c), e.g. by introducing one or more conjugating moieties Y ring closure between suitable monovalent residues R17, exchange or extension of functional groups or substituents such as addition to carbonyl or substitution of carbonyl in R17 or R18.Type: GrantFiled: March 6, 2009Date of Patent: May 7, 2013Assignee: BASF SEInventors: Hans Jürg Kirner, Frank Bienewald, Jean-Charles Flores, Olivier Frédéric Aebischer
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Patent number: 8410094Abstract: The present invention pertains to the field of pharmaceutical chemistry and discloses 8-(3-aminopropyl)-3-exo-8-azabicyclo[3.2.1]octane-3-amino amide compounds represented by formula I, the pharmaceutical compositions, the preparation method and the use thereof. Such compounds or pharmaceutically acceptable salts thereof can be used as an antagonist of CCR5 in preparing medicaments for treating diseases mediated by CCR5, particularly HIV infection, asthma, rheumatoid arthritis, autoimmune diseases and chronic obstructive pulmonary diseases (COPD).Type: GrantFiled: September 18, 2009Date of Patent: April 2, 2013Assignees: Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai Targetdrug Co., Ltd.Inventors: Yaqiu Long, Xing Fan, Dongzhi Feng, Li Chen, Renhai Chen
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Patent number: 8404711Abstract: The invention provides methods for the treatment of cognitive disorders utilizing specific 5-HT4 receptor agonist compounds, in particular, methods utilizing these compounds in combination with other agents, specifically acetylcholinesterase inhibitors, for the treatment of Alzheimer's disease and other cognitive disorders.Type: GrantFiled: April 12, 2010Date of Patent: March 26, 2013Assignee: Theravance, Inc.Inventors: David Beattie, Fei Shen, Jacqueline A. M. Smith
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Publication number: 20130071319Abstract: Certain embodiments disclosed herein relate to compositions, methods, devices, systems, and products regarding frozen particles. In certain embodiments, the frozen particles include materials at low temperatures. In certain embodiments, the frozen particles provide vehicles for delivery of particular agents. In certain embodiments, the frozen particles are administered to at least one biological tissue.Type: ApplicationFiled: October 8, 2012Publication date: March 21, 2013Applicant: Searete LLCInventor: Searete LLC
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Publication number: 20130072467Abstract: The present invention provides a novel compound having a superior activity as an ERR-? modulator and useful as an agent for the prophylaxis or treatment of ERR-? associated diseases. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.Type: ApplicationFiled: August 3, 2012Publication date: March 21, 2013Inventors: Shigemitsu MATSUMOTO, Koji Ono, Yusuke Tominari, Taisuke Katoh, Kazuhiro Miwa, Atsushi Hasuoka, Shinichi Imamura
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Publication number: 20130058880Abstract: Compositions, kits and methods of preparing a biocompatible film for cosmetic or medical uses are disclosed. The compositions or kits contain polyvinyl acetal (PVA), siloxane and a solvent. The siloxane can have a hydrophilic group. Once the solvent content is reduced, for instance, by evaporation, the mixture of PVA and siloxane is solidified, forming a film. The compositions and kits, optionally, further include one or more of an antimicrobial agent, a pigment, an anti-inflammatory agent, an anesthetic agent or a hemostatic agent. Such a film can be used, for example, in the form of an antimicrobial sealant, a liquid bandage, body paints, scar camouflage, water-proof sun block, makeup sealer, or antimicrobial wipe or spray.Type: ApplicationFiled: May 9, 2011Publication date: March 7, 2013Inventor: Shaosheng Dong
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Publication number: 20130052190Abstract: The present invention provides a method for the treatment of allergic and inflammatory diseases or conditions by administering a compound of Formula (I). The invention provides a method of treatment that is particularly suited for patients with a high degree of airway eosinophilia in contrast to those with a lower degree of airway eosinophilia. The invention also provides a method of treatment that is particularly suited for patients with a high atopic status in contrast to those patients with a lower atopic status.Type: ApplicationFiled: February 22, 2012Publication date: February 28, 2013Applicant: Oxagen LimitedInventors: Lisa Pearce Collins, Colin Michael Perkins, Michael Hunter, Eric Roy Pettipher
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Publication number: 20130053364Abstract: The invention provides sulphone compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various sulphone compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.Type: ApplicationFiled: April 23, 2012Publication date: February 28, 2013Inventors: Hazel J. Dyke, Susan M. Cramp, Thomas D. Pallin, Janusz J. Kulagowski, John G. Montana, Robert Zahler