Abstract: The present invention is directed to novel opioid receptor modulators of Formula (I). The invention further relates to methods for preparing such compounds, pharmaceutical compositions containing them, and their use in the treatment of disorders that may be ameliorated or treated by the modulation of opioid receptors.
Type:
Grant
Filed:
March 14, 2005
Date of Patent:
June 22, 2010
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Henry J. Breslin, Chaozhong Cai, Wei He, Robert W. Kavash
Abstract: Compounds of formula (Ia): wherein R1, R2, R3, R4a, R4b, R5 and R6 are defined herein, as well as other indene derivatives are disclosed herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.
Type:
Application
Filed:
September 22, 2009
Publication date:
June 17, 2010
Applicant:
AQUINOX PHARMACEUTICALS INC.
Inventors:
Jeffery R. Raymond, Kang Han, Yuanlin Zhou, Yuehua He, Bradley Noren, James Gee Ken Yee
Abstract: The invention provides a method for the treatment of H4R modulated diseases and/or conditions comprising administering to the subject an effective amount of a H4R agonist. The invention also provides a method for treating COPD comprising administering to the subject an effective amount of a H4R agonist, a H1R antagonist and an anticholinergic drug. Further, the invention provides a pharmaceutical formulation comprising a H4R agonist, a second active agent and a pharmaceutically acceptable carrier.
Abstract: There is described an imidazole for the treatment of an infection caused or contributed to by microorganisms resistant to antibiotics. There is also described a method of treating a patient suffering from an infection caused or contributed to by microorganisms resistant to antibiotics, said method comprising the step of administering an effective amount of an imidazole.
Type:
Application
Filed:
November 15, 2007
Publication date:
June 10, 2010
Inventors:
Malcolm Philip Young, Catherine Mary Thomas, Olusola Clement Idowu, Julie Anne Charlton
Abstract: The invention provides methods for treating A? peptide related disorders such as Alzheimer's disease comprising administering a therapeutically effective amount of a CK1 modulator to a patient in need thereof.
Abstract: An antifungal composition is provided according to the present invention. The antifungal composition comprises an effective amount of an antifungal component to provide antifungal properties to skin tissue, an effective amount of a skin bonding polymer component to provide a sustained release of the antifungal component over a prolonged period of time after application of the antifungal treatment composition to skin tissue, and water. A method for using the antifungal composition is provided.
Abstract: Thiazole amides, imidazole amides and related analogues of the Formula: are provided, in which variables are as described herein. Such compounds may be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) and other disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).
Type:
Grant
Filed:
February 16, 2006
Date of Patent:
June 1, 2010
Assignee:
Neurogen Corporation
Inventors:
Wallace C. Pringle, John M. Peterson, Linghong Xie, Ping Ge, Yang Gao, Joseph W. Ochterski, Jiong Lan
Abstract: There is disclosed herein compounds of formula (I), wherein: R1, R2, R3, R4 and R5 are defined throughout the description and the claims. The compounds of formula (I) are useful for the treatment of neurological diseases and neurodegenerative diseases, e.g. anxiety, depression, Alzheimer's disease etc.
Type:
Grant
Filed:
April 12, 2007
Date of Patent:
June 1, 2010
Assignee:
Probiodrug AG
Inventors:
Michael Thormann, Michael Almstetter, Andreas Treml
Abstract: The present invention relates to 4,5-bis(4-methoxyphenyl)imidazole compound inducing differentiation of myoblasts or muscle fibers into neuron cells and a pharmaceutical composition including said compound. More specifically, it relates to 2-(2-fluorenyl)-4,5-bis(4-methoxyphenyl)imidazole that induces differentiation of myoblasts or muscle fibers, all pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug thereof, and a pharmaceutical composition including said compound.
Type:
Grant
Filed:
January 20, 2006
Date of Patent:
May 18, 2010
Assignee:
Industry-Academic Cooperation Foundation, Yonsei University
Inventors:
In-Jae Shin, Myung-Ryul Lee, Darren Williams
Abstract: A modest (2-5 fold) increase in androgen receptor (AR) mRNA is the only expression change consistently associated with developing resistance to antiandrogen therapy. Increased levels of AR confer resistance to anti-androgens by amplifying signal output from low levels of residual ligand and altering the normal response to antagonists. This invention provides cell based assays for use in the examination of new therapeutic modalities and provides for the design of novel antiandrogen compounds.
Type:
Grant
Filed:
February 23, 2005
Date of Patent:
May 18, 2010
Assignee:
The Regents of the University of California
Inventors:
Michael E. Jung, Samedy Ouk, Charles L. Sawyers, Charlie D. Chen, Derek Welsbie
Abstract: This invention describes novel tricyclic-bis-enone derivatives (TBEs), such as TBE-31, TBE-34, TBE-45 and water-soluble TBEs. The methods of preparing these compounds are also disclosed. The inventors demonstrate the ability of these new TBEs to inhibit proliferation of human myeloma cells, inhibit the induction of iNOS in cells stimulated with interferon-?, induce heme oxygenase-1 (HO-1), induce CD11b expression—a leukemia differentiation marker, inhibit proliferation of leukemia cells, induce apoptosis in human lung cancer, and induce apoptosis in other cancerous cells. The TBEs of this invention are expected to be useful agents for the treatment and prevention of many diseases, including cancer, neurological disorders, inflammation, and pathologies involving oxidative stress.
Type:
Grant
Filed:
November 16, 2007
Date of Patent:
May 11, 2010
Assignee:
Trustees of Dartmouth University
Inventors:
Tadashi Honda, Chitra Sundararajan, Gordon W. Gribble, Michael B. Sporn, Karen T. Liby
Abstract: Methods and pharmaceutical compositions relating to selective antagonists of the 5-HT6 receptor and 5-HT2A receptor useful for the treatment of cognitive disorders are presented.
Type:
Grant
Filed:
September 30, 2005
Date of Patent:
May 11, 2010
Assignee:
Roche Palo Alto LLC
Inventors:
Douglas William Bonhaus, Renee Sharon Martin
Abstract: A gelled composition formulated to maintain an active ingredient in association with the nasal membrane for an extended period of time is provided. The gelled composition may be formulated as a decongestant or a sinus discomfort relieving agent. The invention further includes a system and method for applying the gelled composition to the nasal membrane.
Abstract: Disclosed are compounds having the ability to inhibit cytochrome P450 2A6, 2A13, and/or 2B6 and tobacco products comprising them. Also disclosed are pharmaceutical compositions comprising them.
Type:
Application
Filed:
March 20, 2008
Publication date:
May 6, 2010
Applicant:
Givaudan SA
Inventors:
Boris Schilling, Wolf D. Woggon, Antoinette Chougnet, Thierry Granier, Georg Frater, Andreas Hanhart
Abstract: Disclosed herein is a hydrophilic foam. The hydrophilic foam includes a polyurethane matrix having a plurality of cells. The cells are capable of retaining water in an amount of least about 8 grams of water per gram of the hydrophilic foam.
Abstract: A nasal spray composition for treating mucosal inflammation associated with rhinitis, sinusitis, or both can include a decongestant and at least one therapeutic agent. The therapeutic agent is selected from the group consisting of an anti-inflammatory agent and an anti-histamine agent. The nasal spray composition is non-habituating and is administered intranasally to a subject in need thereof.
Abstract: The present invention relates to compositions of submicron- to micron-size particles of antimicrobial agents. More particularly the invention relates to a composition of an antimicrobial agent that renders the agent potent against organisms normally considered to be resistant to the agent. The composition comprises an aqueous suspension of submicron- to micron-size particles containing the agent coated with at least one surfactant selected from the group consisting of: ionic surfactants, non-ionic surfactants, biologically derived surfactants, and amino acids and their derivatives. The particles have a volume-weighted mean particle size of less than 5 ?m as measured by laser diffractometry.
Type:
Application
Filed:
March 30, 2009
Publication date:
April 8, 2010
Applicants:
BAXTER INTERNATIONAL INC., BAXTER HEALTHCARE S.A.
Inventors:
Barrett Rabinow, Randy White, Chong-Son Sun, Joseph Chung Tak Wong, James E. Kipp, Mark J. Doty, Christine Rebbeck, Pavlos George Papadopoulos
Abstract: The present invention relates to compounds of the general formula (I): wherein A, B, C and D each independently are a methine group or a nitrogen atom, said methine group optionally having a substituent(s) with at least one of them meaning the methine group; E means a group represented by the following formulae (E1): R1 means a lower alkyl group or an aryl group optionally having a substituent(s) or means a lower alkylene group linked to arbitrary, linkable position(s) of E, and others. The compounds of the present invention are useful as an agent for the treatment of a variety of diseases related to NPY.
Abstract: The present invention relates to a process for preparing a compound of formula (6a): wherein Ar1 represents an imidazolyl group which may be substituted with 1 to 3 substituents shown below; Ar2 represents a pyridinyl group, a pyrimidinyl group or a phenyl group which may be substituted with 1 to 3 substituents; and R11 represents a group selected from certain substituents.
Abstract: A foaming gelled composition in the form of a stable oil-in-water microemulsion comprising a fatty phase of microdroplets dispersed in an aqueous phase and a dermatological active ingredient, characterized in that it comprises a surfactant system comprising:—at least one ethoxylated nonionic surfactant;—at least one cosurfactant for stabilizing the ethoxylated nonionic surfactant;—at least one nonethoxylated hydrophilic nonionic surfactant;—at least one foaming agent chosen from the group of anionic surfactants.
Abstract: The present invention relates to diphenylmethyl imidazole mineralocorticoid receptor modulators compounds having the structure and their use in treating cardiovascular events.
Type:
Application
Filed:
March 19, 2008
Publication date:
March 18, 2010
Inventors:
Philip E. Brandish, James C. Hershey, Mark E. Fraley, Justin T. Steen
Abstract: This invention is directed to vanilloid receptor VR1 ligands. More particularly, this invention relates to ?-aminotetralin-derived ureas that are potent antagonists or agonists of VR1 which are useful for the treatment and prevention of inflammatory and other pain conditions in mammals.
Type:
Grant
Filed:
October 23, 2007
Date of Patent:
March 16, 2010
Assignee:
Janssen Pharmaceutica NV
Inventors:
Ellen Codd, Scott L. Dax, Michele Jetter, Mark McDonnell, James J. McNally, Mark Youngman
Abstract: In its several embodiments, this invention discloses a pharmaceutical formulation comprising at least one antineoplastic agent or a pharmaceutically acceptable salt thereof, and at least one dissolution enhancing agent sufficient to substantially dissolve said at least one antineoplastic agent in at least one aqueous diluent, wherein said dissolution enhancing agent is urea, L-histidine, L-threonine, L-asparagine, L-serine, L-glutamine or mixtures thereof; a lyophilized powder comprising said pharmaceutical formulation, and articles of manufacture thereof.
Type:
Grant
Filed:
January 13, 2006
Date of Patent:
March 9, 2010
Assignee:
Schering Corporation
Inventors:
Sydney Ugwu, Vinay Radhakrishnan, Peter M. Ihnat, Leonore C. Witchey-Lakshmanan
Abstract: The present invention includes methods and compositions for the treatment and prevention of protozoal parasitic infections utilizing Diindolylmethane-related indoles. Additive and synergistic interaction of Diindolylmethane-related indoles with other known anti-parasitic and pro-apoptotic agents is believed to permit more effective therapy and prevention of protozoal parasitic infections. The methods and compositions described provide new treatment of protozoal parasitic diseases of mammals and birds including malaria, leishmaniasis, trypanosomiasis, trichomoniasis, neosporosis and coccidiosis.
Abstract: A nasal delivery device for and method of delivering substance to the middle meatus in a nasal cavity of a subject in the treatment of a condition, in particular an inflammatory or infectious condition, thereof, the delivery device comprising: a nosepiece unit (17) including a nosepiece (20) for fitting to a nostril of a subject and a nozzle (25) through which substance is in use delivered to the respective nasal cavity; and a delivery unit (29) for delivering substance through the nozzle of the nosepiece; wherein the delivery device is configured to provide for deposition of a significant fraction of the delivered dose on, around and in the vicinity of the middle meatus.
Type:
Application
Filed:
February 14, 2007
Publication date:
March 4, 2010
Applicant:
OptiNose AS
Inventors:
Per Gisle Djupesland, Colin David Sheldrake, Roderick Peter Hafner
Abstract: A combination of selected substances in paint to prevent the settlement and growth of different bio-fouling organisms with a reduced negative effect on the ecosystems compared to present methods. Useful substances include medetomidine with various copper and zinc formulations, tolylfluanide, diclofluanide, DIURON™ and IRGAROL™, or more general biocides such as SEANINE™ (4,5-dichloro-2-n-octyl-3(2H)-isothiazolone) or ECONEA™ (2-(p-chlorophenyl)-3-cyano-4-bromo-5-trifluoromethyl pyrrole).
Abstract: A method for treatment of multiple sclerosis and other neurodegenerative diseases, disorders or conditions. An alkyl ester of imidazole carboxylic acid, preferably methyl 4-imidazolecarboxylate, is administered in a therapeutic amount. It is hypothesized that the alkyl ester of imidazole carboxylic acid serves to restore and/or maintain the intracellular/extracellular osmolyte gradient in the central nervous system (CNS). The methyl 4-imidazolecarboxylate may be administered transdermally, using PLO gel or other suitable transdermal carrier. The compound may also be administered orally, inhaler or by injection. The treatment is advantageously performed on a three day cycle, with a period of two days intervening between each day on which the compound is administered. Dosage ranges may be from about 0.01 mcg to about 3.0 mcg, with dosages in the range from about 0.1 mcg to about 0.2 mcg in generally preferred when using transdermal administration.
Abstract: This invention relates to a composition comprising a combination of a) an alpha substituted 2-benzyl substituted imidazole and b) a 1-N-arylpyrazole, and optionally c) an insect growth regulator, and their use as a parasiticide in mammals.
Abstract: This invention relates to the use of a combination of selected substances in paint to prevent the settlement and growth of different biofouling organisms with a reduced negative effect on the ecosystems compared to present methods.
Abstract: The invention generally relates to anesthetic compositions comprising low doses of a selective a-2 adrenergic receptor agonists in combination with anesthetic agents. The invention also relates to methods of using these compositions; in particular, the use of these compositions in humans to enhance the efficacy of a local peripheral anesthetic injection. The compositions and the methods are particularly useful in regional block anesthetic injections, and more particularly, in dental anesthetic injections.
Abstract: The invention generally relates to compositions and methods for reducing activation of a-1 adrenergic receptors. The compositions comprise highly selective a-2 adrenergic receptor agonists, at low concentrations, such as below 0.05% weight by volume. The compositions preferably comprise brimonidine. The compositions preferably have pH between about 5.5 and about 6.5.
Abstract: The invention generally relates to compositions for inducing vasoconstriction. The compositions comprise highly selective alpha-2 adrenergic receptor agonists, at low concentrations, such as below 0.05% weight by volume. The compositions preferably comprise brimonidine. The compositions preferably have pH between about 5.5 and about 6.5.
Abstract: The invention generally relates to compositions and methods for inducing vasoconstriction with low incidence of rebound hyperemia. The compositions comprise highly selective alpha-2 adrenergic receptor agonists, at low concentrations, such as below 0.05% weight by volume. The compositions preferably comprise brimonidine. The compositions preferably have pH between about 5.5 and about 6.5.
Abstract: Compounds that act as inhibitors of QC including those represented by the general formulae 1 to 9: and combinations thereof for the treatment of neuronal disorders, especially Alzheimer's disease, Down Syndrome, Parkinson disease, Corea Huntington, pathogenic psychotic conditions, schizophrenia, impaired food intake, sleep-wakefulness, impaired homeostatic regulation of energy metabolism, impaired autonomic function, impaired hormonal balance, impaired regulation, body fluids, hypertension, fever, sleep dysregulation, anorexia, anxiety related disorders including depression, seizures including epilepsy, drug withdrawal and alcoholism, neurodegenerative disorders including cognitive dysfunction and dementia.
Type:
Grant
Filed:
March 12, 2008
Date of Patent:
February 2, 2010
Assignee:
Probiodrug AG
Inventors:
Stephan Schilling, Andre Johannes Niestroj, Ulrich Heiser, Hans-Ulrich Demuth, Mirko Buchholz
Abstract: Methods of screening and designing compounds as inhibitors of glutamine synthetase are provided herein. Compounds, e.g., serine protease inhibitors, and compositions comprising the same, that are useful for the treatment, prevention, and/or amelioration of bacterial infections, including Mycobacterium tuberculosis, are also provided.
Type:
Application
Filed:
March 15, 2006
Publication date:
January 28, 2010
Inventors:
Colin Peter Kenyon, Lyndon Carey Oldfield
Abstract: There is provided compounds of formula (I), wherein X1, X2, X3, Y4, Y1, Y2, Y3, Y4, Z1, Z2, R4 and R5 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful as selective agonists of the AT2 receptor, and thus, in particular, in the treatment of inter alia gastrointestinal conditions, such as dyspepsia, IBS and MOF, and cardiovascular disorders.
Type:
Grant
Filed:
November 26, 2003
Date of Patent:
January 26, 2010
Assignee:
Vicore Pharma AB
Inventors:
Mathias Alterman, Anders Rudolf Hallberg
Abstract: Disclosed herein is a pharmaceutical composition comprising a serotonin-norepinephrine reuptake inhibitor and an alpha-2B receptor agonist. The composition is effective for treating chronic pain, and methods of treating pain using the composition and compounds comprising it are also disclosed.
Abstract: It is now recognized that chronic inflammation is an important risk factor for the development of cancer. The proinflammatory cytokine IL-6 is implicated in cancer because it is important for the activation of STAT, a key regulator of cancer growth, survival, metastasis, immune evasion and angiogenesis. Increased IL-6 and Stat-3 exists in vitro in pancreatic cancer, malignant melanoma, papillary thyroid cancer, breast cancer, colon cancer, and prostate cancer cells with high basal expression of Toll-like receptor 3 (TLR3) and Wnt5a. IL6/STAT3 activation, mediated by overexpressed TLR3 signaling, appears important in the tumor growth process, it may increase Wnt5a signaling, and be associated with increased cellular growth and migration.
Type:
Application
Filed:
October 1, 2008
Publication date:
January 7, 2010
Inventors:
Leonard D. Kohn, Douglas J. Goetz, Kelly D. McCall, Anthony Schwartz, Frank Schwartz, Ramiro Malgor, Glorglo Napolitano, Cesidio Giullant
Abstract: The present invention relates to S1P analogs that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds have the general structure (I) wherein R11 is C5-C18 alkyl or C5-C18 alkenyl; Q is selected from the group consisting of C3-C6 optionally substituted cycloalkyl, C3-C6 optionally substituted heterocyclic, C3-C6 optionally substituted aryl C3-C6 optionally substituted heteroaryl and; R2 is selected from the group consisting of H, C1-C4 alkyl, (C1-C4 alkyl)OH and (C1-C4 alkyl)NH2; R23 is H or C1-C4 alkyl, and R15 is a phosphonate ester or a phosphate ester or a pharmaceutically acceptable salt or tautomer thereof.
Type:
Grant
Filed:
November 3, 2004
Date of Patent:
December 29, 2009
Assignee:
University of Virginia Patent Foundation
Abstract: The present invention provides various biomarkers of Alzheimer's Disease (AD). The present invention also provides various methods of using the biomarkers, including methods for diagnosis of AD, methods of determining predisposition to AD, methods of monitoring progression/regression of AD, methods of assessing efficacy of compositions for treating AD, methods of screening compositions for activity in modulating biomarkers of AD, methods of treating AD, as well as other methods based on biomarkers of AD.
Type:
Application
Filed:
August 15, 2008
Publication date:
December 24, 2009
Inventors:
Lisa A. Paige, Matthew W. Mitchell, Anne Evans, Don Harvan
Abstract: Described herein are transdermal delivery devices composed of at least one resealable injection port and at least one local anesthetic reservoir. The device effectively delivers anesthetic to the skin of the subject prior to puncturing the skin by syringes, needle sticks, or other instruments intended to be inserted into the skin. In addition, this device can be used to deliver various therapeutic agents for either locally or systemically.
Abstract: This invention relates to a range of alpha substituted 2-benzyl substituted imidazole compounds and pharmaceutically acceptable salts and solvates thereof, to compositions comprising such compounds, processes for their synthesis and their use as parasiticides.
Type:
Application
Filed:
August 4, 2009
Publication date:
December 17, 2009
Applicant:
PFIZER LIMITED
Inventors:
Nathan Anthony Logan Chubb, Mark Roger Cox, Jerome Sebastien Dauvergne, Richard Andrew Ewin, Christelle Lauret
Abstract: The present invention relates to the antimicrobial mixture comprising or consisting of: (a) one, two or more tropolone derivatives of the formula (1) wherein the substituents R1, R2, R3, R4, R5 independently of one another have the following meaning: H; linear or branched, saturated or unsaturated, aliphatic hydrocarbon radical having up to 30 C atoms; OH; OR6, wherein R6 is a linear or branched, saturated or unsaturated, aliphatic hydrocarbon radical having up to 30 C atoms; COOH; COOR7, wherein R7 is a linear or branched, saturated or unsaturated, aliphatic hydrocarbon radical having up to 30 C atoms; NO2, NH2, F, Cl, Br or I or salts or solvates thereof and (b) one or more compounds selected from the group consisting of: chlorphenesin, imidazolidinyl urea, DMDM hydantoin, ethylhexylglycerin, diazolidinyl urea, sodium hydroxymethylglycinate and polyaminopropyl biguanide or salts or solvates thereof.
Abstract: This invention comprises a composition and the process of using the composition for removing and preventing mold, mildew, and fungal growth. The composition comprises at least one alkali metal perborate, at least one inhibiting compound selected from the group consisting of alkali metal silicates, triazoles and mixtures thereof in any ratio, at least one corrosion inhibitor, and effective amounts of surfactant.
Type:
Grant
Filed:
January 31, 2007
Date of Patent:
December 8, 2009
Assignee:
The United States of America as represented by the Secretary of the Navy
Inventors:
El Sayed S. Arafat, Craig A. Matzdorf, Stephen J. Spadafora, David L. Gauntt, Paul R. Roser, James A. Whitfield
Abstract: It has now been found that the p53 pathway is inactivated in ocular cancers such as retinoblastoma. As such, the present invention is a method for inducing ocular cancer cell death using a p53 activator. In particular embodiments, the p53 activator blocks the interaction between DM2 or DMX and p53. As the p53 activator induces ocular cancer cell death, a method for preventing or treating ocular cancer is also provided.
Type:
Application
Filed:
July 24, 2007
Publication date:
December 3, 2009
Inventors:
Michael A. Dyer, Jean-Christophe Marine, Aart Gerrit Jochemsen
Abstract: Novel compounds having the general formula (I) below: are useful in a wide variety of applications in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively are formulated into cosmetic compositions.
Type:
Grant
Filed:
December 20, 2005
Date of Patent:
December 1, 2009
Assignee:
Galderma Research & Development
Inventors:
Laurence Clary, Etienne Thoreau, Michel Rivier, Jerome Aubert, Laurent Chantalat, Johannes Voegel