2-imidazolines Patents (Class 514/401)
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Publication number: 20110097380Abstract: Antimicrobial clonidine compositions are provided. These antimicrobial clonidine compositions can be applied to medical devices or be part of a drug depot. Through the administration of an effective amount of clonidine at or near a target site, one can reduce, prevent, or treat infections. When appropriate clonidine compositions are provided within biodegradable polymers, the infection may be treated for extended periods of time.Type: ApplicationFiled: October 28, 2009Publication date: April 28, 2011Applicant: Warsaw Orthopedic, Inc.Inventors: Vanja Margareta King, Julie H. Block
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Publication number: 20110098331Abstract: The present invention relates to novel imidazoline derivatives and their use as insecticidal, acaricidal, mollus and nematocidal agents. The invention also extends to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising such imidazoline derivatives, and to methods of using such derivatives and/or compositions to combat and control insect, acarine, mollusc and nematode pests. A compound of formula (I): and the salts and N-oxides thereof.Type: ApplicationFiled: October 24, 2008Publication date: April 28, 2011Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Christoph Luethy, Anthony Cornelius O'Sullivan, Thomas Pitterna, Jurgen Harry Schaetzer
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Publication number: 20110092542Abstract: The present invention is directed to therapeutic compositions targeting the NCCa-ATP channel of an astrocyte, neuron or capillary endothelial cell and methods of using same. More specifically, antagonists of the NCCa-ATP channel are contemplated. The compositions are used to prevent cell death and to treat secondary damage associated with spinal cord injury.Type: ApplicationFiled: December 9, 2010Publication date: April 21, 2011Inventor: J. Marc Simard
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Patent number: 7923036Abstract: Compositions comprising a mixture of (a) a major amount of solid halogen-containing sanitizer material and (b) a minor amount of calcium oxide modified particulate boric acid, the amount of calcium oxide modified particulate boric acid being sufficient to enable the composition to be classified as a class 1 or class 2 NFPA oxidizer are described. Also described is particulate boric acid at least a portion of the particles thereof having on their surface at least a partial coating of calcium oxide, and a method for preparing such coated particulate boric acid.Type: GrantFiled: September 30, 2008Date of Patent: April 12, 2011Assignee: PPG Industries Ohio, Inc.Inventor: Stanley R. Pickens
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Publication number: 20110065766Abstract: The present invention relates, in part, to methods of treatment, prevention, and inhibition of viral disorders. In one aspect, the present invention relates to inhibition of the M2 proton channel of influenza viruses (e.g. influenza A virus) and other similar viroporins (e.g., VP24 of Ebola and Marburg viruses; and NS3 protein of Bluetongue). The present invention further relates, inter alia, to compounds which have been shown to possess antiviral activity, in particular, inhibiting the M2 proton channel of influenza viruses.Type: ApplicationFiled: September 13, 2010Publication date: March 17, 2011Inventors: Jizhou Wang, Xiaodong Fan, Lidia Cristian
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Publication number: 20110046120Abstract: The present disclosure provides methods and compositions for treating Impulse Control disorders including, for example, pathological gambling using ?2-adrenergic agonists, ?-adrenergic receptor antagonists, or both.Type: ApplicationFiled: October 25, 2007Publication date: February 24, 2011Inventor: Igor Elman
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Patent number: 7893097Abstract: The combination of any two of a polyol, a polyol ether, and a low carbon organic alcohol provides a synergistic effect on the solubility of azole compounds, such as metronidazole, in aqueous fluid.Type: GrantFiled: February 2, 2008Date of Patent: February 22, 2011Assignee: Dow Pharmaceutical Sciences, Inc.Inventors: Meidong Yang, Haigang Chen
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Publication number: 20110034463Abstract: The invention, in some aspects, relates to compounds and compositions useful for inhibiting Type III secretion systems in pathogenic bacteria, such as Yersinia Pestis. In some aspects, the invention relates to methods for discovering inhibitors of the Type III secretion system and uses of such inhibitors in the treatment and prevention of disease.Type: ApplicationFiled: April 1, 2009Publication date: February 10, 2011Inventors: Jon Goguen, Ning Pan, Kyungae Lee
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Patent number: 7884122Abstract: A composition and method of treating adrenergic dysregulation by administering the composition is disclosed, wherein the composition comprises a a2-adrenergic receptor agonist; a pharmaceutically acceptable hydrophilic matrix and a release-retardant of a metal alkyl sulfate. In embodiments, the composition provides a sustained release of the agonist, wherein after administration of the composition no more than once about every 12 hours to a subject having a steady state plasma concentration of the a2-adrenergic receptor agonist, the agonist's plasma concentration peak-to-trough ratio is no greater than about 1.9.Type: GrantFiled: November 10, 2009Date of Patent: February 8, 2011Assignee: Shionogi Pharma, Inc.Inventors: Henry Joseph Horacek, Min Michael He, Moise A. Khayrallah
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Publication number: 20110027201Abstract: The present invention is directed to the treatment of skin erythema as exhibited in rosacea and other conditions characterized by increased erythema (redness) of the skin. These conditions exhibit dilation of blood vessels due to a cutaneous vascular hyper-reactivity. In particular, the present invention is directed to a novel composition and method for the treatment of skin erythema using ?1-adrenergic receptor (?1-adrenoceptor) agonists incorporated into cosmetic, pharmacological or dermatological compositions for topical application to the skin.Type: ApplicationFiled: October 11, 2010Publication date: February 3, 2011Applicant: VICEPT THERAPEUTICS, INC.Inventors: Stuart D. Shanler, Andrew Ondo
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Publication number: 20110027340Abstract: The present invention is directed to an implantable drug depot for weight control. The drug depot includes at least one biodegradeable polymer and at least one biologically active agent. Through the administration of an effective amount of the biologically active agent at or near a target site, one can control weight gain and/or reduce, prevent or treat obesity. When appropriate formulations are provided within biodegradable polymers, weight control or treatment can be conducted for at least five days and up to one hundred and thirty-five days.Type: ApplicationFiled: July 31, 2009Publication date: February 3, 2011Applicant: Warsaw Orthopedic, Inc.Inventor: Vanja Margareta King
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Publication number: 20110021573Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the antagonists of PGD2 receptors described herein, as well as methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: ApplicationFiled: February 25, 2009Publication date: January 27, 2011Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: John Howard Hutchinson, Brian Andrew Stearns, Thomas Jonathan Seiders, Jill Melissa Scott, Jeannie M. Arruda, Bowei Wang
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Publication number: 20110021469Abstract: A high concentration baclofen solution is provided suitable for therapeutic use in a medical setting. A high concentration solution of baclofen in multivalent physiological ion solution such as artificial cerebrospinal fluid is provided with concentrations of baclofen of 10 mg/ml. Artificial cerebrospinal fluid is particularly advantageous as a baclofen solvent. A medical package is also provided for baclofen delivery to patients suffering from spasticity.Type: ApplicationFiled: June 13, 2008Publication date: January 27, 2011Inventors: Jay M. Meythaler, Stephen M. Tuel
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Publication number: 20110020362Abstract: The current invention provides mechanisms by which chronic stress induced hypersensitivity exacerbates the symptoms of irritable bowel syndrome. The invention includes methods of treating irritable bowel syndrome using agents which inhibit key molecules involved in the sensitization pathway.Type: ApplicationFiled: July 20, 2010Publication date: January 27, 2011Inventor: Sushil K. Sarna
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Patent number: 7875645Abstract: The present invention relates a method for treating depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders which comprises administering to an individual a therapeutically effective amount of a compound of formula I wherein R, R1, R2, A and n are as defined in the specification and to their pharmaceutically active salts. The invention also relates to novel compounds of formula I, pharmaceutical compositions containing them, and methods for their preparation.Type: GrantFiled: January 19, 2007Date of Patent: January 25, 2011Assignee: Hoffman-La Roche Inc.Inventors: Guido Galley, Katrin Groebke Zbinden, Marius Hoener, Sabine Kolczewski, Roger Norcross, Henri Stalder
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Publication number: 20110014259Abstract: Effective treatments of hematomas, edema, or other fluid accumulation or deep vein thromboses are provided. Through the administration of an effective amount of at least one alpha adrenergic agonist at or near a target site, one can reduce, prevent or treat edema, or other fluid accumulation or deep vein thromboses.Type: ApplicationFiled: July 17, 2009Publication date: January 20, 2011Applicant: Warsaw Orthopedic, Inc.Inventor: Vanja Margareta KING
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Patent number: 7872048Abstract: The present invention is directed to therapeutic compositions targeting the NCCa-ATP channel of an astrocyte, neuron or capillary endothelial cell and methods of using same. More specifically, antagonists of the NCCa-ATP channel are contemplated. The compositions are used to prevent cell death and to treat secondary damage associated with spinal cord injury.Type: GrantFiled: September 16, 2005Date of Patent: January 18, 2011Assignee: University of Maryland, BaltimoreInventor: J. Marc Simard
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Publication number: 20100331384Abstract: The adrenergic receptors or adrenoceptors are a family of G-protein coupled receptors split into ? and ? subclasses. The adrenoceptors have important roles in regulating a myriad of physiological conditions and their malfunction has been implicated in the pathophysiology of a number of diseases. Disclosed herein are a series of novel guanidine and 2-aminoimidazoline compounds which are ligands of the alpha2-adrenoceptor (?2-ARs) subclass of adrenergic receptors. The invention also provides for pharmaceutical compositions comprising the novel compounds. The compounds are suitable for use in the manufacture of medicaments for the treatment of ?2-ARs associated disorders, such as depression, schizophrenia, glaucoma and analgesia.Type: ApplicationFiled: December 22, 2008Publication date: December 30, 2010Applicants: UNIVERSIDAD DEL PAIS VASCO/EUSKAL HERRIKO UNIBERTSITATEA, UNIDIVIDED TRINITY OF QUEEN ELIZABETHInventors: Maria Isabel Rozas Hernando, Fernando Rodriguez Royo, Javier Meana, Luis Callado
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Publication number: 20100316628Abstract: The present invention relates to a novel method of preventing and/or treating respiratory disorders and respiratory-related complications in a subject by inhibiting the release of nitric oxide from basal cells in the respiratory tract.Type: ApplicationFiled: December 9, 2009Publication date: December 16, 2010Applicant: THE GENERAL HOSPITAL CORPORATIONInventors: Sylvie Breton, Dennis Brown, Wai Chi Shum, Nicolas Da Silva
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Publication number: 20100311705Abstract: Solutions for perioperative intraocular application by continuous irrigation during ophthalmologic procedures are provided. These solutions include multiple agents that act to inhibit inflammation, inhibit pain, effect mydriasis (dilation of the pupil), and/or decrease intraocular pressure, wherein the multiple agents are selected to target multiple molecular targets to achieve multiple differing physiologic functions, and are included in dilute concentrations in a balanced salt solution carrier.Type: ApplicationFiled: May 5, 2010Publication date: December 9, 2010Inventors: Gregory A. Demopulos, Pamela Pierce Palmer, Jeffrey M. Herz
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Patent number: 7829596Abstract: A method of treating weight loss due to underlying disease in a patient, the method comprising administering to the patient an effective amount of an agent which reduces sympathetic nervous system activity. A method of treating weight loss due to underlying disease in a patient, the method comprising administering to the patient an effective amount of any one or more of the following: a compound which inhibits the effect of aldosterone such as an aldosterone antagonist; a chymase inhibitor; a cathepsin B inhibitor; a ? receptor blocker; an imidazoline receptor antagonist; a centrally acting ? receptor antagonist; a peripherally acting ? receptor antagonist; a ganglion blocking agent; a drug that has an effect on cardiovascular reflexes and thereby reduces SNS activity such as an opiate; scopolamine; an endothelin receptor antagonist; and a xanthine oxidize inhibitor. The methods are particularly useful in treating cardiac cachexia.Type: GrantFiled: August 15, 2008Date of Patent: November 9, 2010Assignee: Imperial Innovations LimitedInventors: Stefan Dietmar Anker, Andrew Justin Stewart Coats
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Publication number: 20100280088Abstract: The present invention relates to novel imidazoline derivatives and their use as insecticidal, acaricidal, molluscicidal and nematocidal agents. The invention also extends to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising such imidazoline derivatives, and to methods of using such derivatives and/or compositions to combat and control insect, acarine, mollusc and nematode pests.Type: ApplicationFiled: September 9, 2008Publication date: November 4, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Christoph Luethy, Anthony Cornelius O'Sullivan, Thomas Pitterna, Jurgen Harry Schaetzer
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Publication number: 20100267795Abstract: The present invention relates to imidazoline derivatives and their use as insecticidal and acaricidal agents. The invention also extends to insecticidal and acaricidal compositions comprising such imidazoline derivatives, and to methods of using such derivatives and/or compositions to combat and control insect and acarine pests. In particular the present invention relates to phenoxy-imidazoline derivatives wherein the phenoxy moiety is substituted with a nitro group. A method of combating and/or controlling an insect or acarid pest, which comprises applying to said pest, or to the locus of said pest, or to a plant susceptible to attack by said pest, a compound of formula (I): or salt or N-oxide thereof.Type: ApplicationFiled: October 24, 2008Publication date: October 21, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Christoph Luethy, Anthony Cornelius O'Sullivan, Thomas Pitterna, Jurgen Harry Schaetzer
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Publication number: 20100260813Abstract: A rodenticidal mixture comprising a) 0.0015 to 99.89% by weight of at least one rodenticide, b) 10?8 to 95% by weight of at least one painkiller and c) 0.01 to 99.9984% by weight of at least one biocide, where the percentages by weight are based on the total of components (a), (b) and (c), is suitable for the preparation of rodenticidal bait formulations which are employed for controlling rodent pests.Type: ApplicationFiled: September 30, 2008Publication date: October 14, 2010Applicant: BASF SEInventors: Gerhard Schnabel, Michael Ishaque, Dieter Zeller, Lars Weichel, Andrej Brejc
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Patent number: 7812049Abstract: The present invention is directed to the treatment of skin erythema as exhibited in rosacea and other conditions characterized by increased erythema (redness) of the skin. These conditions exhibit dilation of blood vessels due to a cutaneous vascular hyper-reactivity. In particular, the present invention is directed to a novel composition and method for the treatment of skin erythema using ?1-adrenergic receptor (?1-adrenoceptor) agonists incorporated into cosmetic, pharmacological or dermatological compositions for topical application to the skin.Type: GrantFiled: January 22, 2004Date of Patent: October 12, 2010Assignee: Vicept Therapeutics, Inc.Inventors: Stuart D. Shanler, Andrew Ondo
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Publication number: 20100255051Abstract: Polyketal polymers, and methods of making and using such polyketal polymers are disclosed herein. The polyketal poylmers can be useful for applications including, for example, medical devices and pharmaceutical compositions. In a preferred embodiment, the polyketal polymers are biodegradable.Type: ApplicationFiled: June 18, 2010Publication date: October 7, 2010Inventors: Michael Eric Benz, Lian Leon Luo
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Publication number: 20100239523Abstract: The invention provides Toll-like receptor (TLR) modulators, compositions comprising the same, and methods for using the same.Type: ApplicationFiled: October 30, 2008Publication date: September 23, 2010Applicant: The Regents of the University of ColoradoInventors: Linda May Rothblum Watkins, Mark Rowland Hutchinson
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Patent number: 7799816Abstract: This invention relates to an alpha-1 A receptor partial agonist, which is represented by Formula I: and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing formula I, methods for their use as therapeutic agents, and methods of preparation thereof.Type: GrantFiled: February 4, 2009Date of Patent: September 21, 2010Assignee: Roche Palo Alto LLCInventors: Counde O'Yang, Robert Greenhouse
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Publication number: 20100233109Abstract: The present invention is directed to the treatment of skin erythema as exhibited in rosacea and other conditions characterized by increased erythema (redness) of the skin. These conditions exhibit dilation of blood vessels due to a cutaneous vascular hyper-reactivity. In particular, the present invention is directed to a novel composition and method for the treatment of skin erythema using ?1-adrenergic receptor (?1-adrenoceptor) agonists incorporated into cosmetic, pharmacological or dermatological compositions for topical application to the skin.Type: ApplicationFiled: May 27, 2010Publication date: September 16, 2010Applicant: VICEPT THERAPEUTICS, INC.Inventors: Stuart D. Shanler, Andrew Ondo
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Publication number: 20100227867Abstract: In methods, compounds, and topical formulations for treatment of inflammatory skin disorders incorporating compounds represented by the formulas below: wherein each of R1, R2, and R3 is independently hydrogen, hologen, alkyl, or alkoxy; each of R4 and R5 is independently hydrogen, alkyl, or alkoxy; and each of R6 and R7 is independently hydrogen, nitro, alkyl, or alkoxy; wherein each of A1, A3, and A4 is independently hydrogen or alkyl; and A2 is independently hydrogen or hydroxy; and wherein each of B1, B2, and B3 is independently hydrogen, hydroxy, or alkoxy; and each of B4 and B5 is independently hydrogen or alkyl, applying such compounds topically as sprays, mists, aerosols, solutions, lotions, gels, creams, ointments, pastes, unguents, emulsions, and suspensions to treat inflammatory skin disorders and the symptoms associated therewith.Type: ApplicationFiled: August 21, 2009Publication date: September 9, 2010Applicant: Galderma Laboratories Inc.Inventors: Jack A. DeJovin, Isabelle Jean DeJovin, Thomas M. Rossi
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Publication number: 20100222257Abstract: Disclosed herein are substituted phenethylamine alpha adrenergic receptor modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: May 17, 2010Publication date: September 2, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20100209510Abstract: A composition and method of treating adrenergic dysregulation by administering the composition is disclosed, wherein the composition comprises a ?2-adrenergic receptor agonist; a pharmaceutically acceptable hydrophilic matrix and a release-retardant of a metal alkyl sulfate. In embodiments, the composition provides a sustained release of the agonist, wherein after administration of the composition no more than once about every 12 hours to a subject having a steady state plasma concentration of the ?2-adrenergic receptor agonist, the agonist's plasma concentration peak-to-trough ratio is no greater than about 1.9.Type: ApplicationFiled: September 16, 2009Publication date: August 19, 2010Inventors: Henry Joseph Horacek, Min Michael He, Moise A. Khayrallah
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Publication number: 20100204260Abstract: A new class of imidazolines as 4-position acids or esters with very potent anti-inflammatory as well as antimicrobial activity is described. The synthesis of these imidazolines includes a multicomponent reaction applicable to a combinatorial synthetic approach. The combination of these two key characteristics provides an effective therapeutic drug in the treatment of septic shock as well as many other inflammatory (arthritis and asthma) and infectious disorders. The use of this novel class of non-steroidal agents as anti-inflammatory agents (for the treatment of asthma etc.), antibacterial agents and antiseptic agents is described. The compounds are also useful in the treatment of tumors (such as cancers). The imidazolines are potent inhibitors of the transcription factor NF-?B as well as potent activity against the Gram (+) bacterium B. subtillus and B. cereus with MIC values in the range of 50 ?m/mL.Type: ApplicationFiled: January 26, 2010Publication date: August 12, 2010Inventors: Jetze J. Tepe, Satyamaheshwar Peddibhotla
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Publication number: 20100196286Abstract: Methods, devices and kits for treating sleep disorders, anxiety disorders, and developmental disorders, and/or for inducing an arousable state of sedation in a subject, are described. For example, inhalation methods, devices and kits for treating insomnia, anxiety and/or ADHD using one or more ?2-adrenergic agonists such as dexmedetomidine or clonidine are described.Type: ApplicationFiled: December 1, 2009Publication date: August 5, 2010Inventors: Thomas A. ARMER, Robert O. Cook, Terry Alfredson, Anthony Sun
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Patent number: 7767667Abstract: It has now been found that certain novel heterocyclic derivitives have provided unexpected insecticidal activity. These compounds are represented by formula (I): R Preferred are those compounds of formula (I) where R2 and R3 taken together is ?NCH(R6)CH(R7)N(R8)—, ?NC(R6)?C(R7)N(R8)—, or ?CHN?C(R7)N(R8)—, and tautomers thereof, and where R4 and R5 taken together is —C(R11)?C(R12)C(R13)?C(R14) 1 12, -, where R,R,R6, R7, R8, RI1, R R13, R14, and X are described. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula (I), and optionally, an effective amount of at least one of a second compound with at least one insecticidally compatable carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.Type: GrantFiled: August 22, 2008Date of Patent: August 3, 2010Assignee: FMC CorporationInventors: John A. Dixson, Zeinab M. Elshenawy, Harvey R. Wendt, Saroj Sehgel, Robert H. Henrie, II, David M. Roush, Ping Ding, John W. Lyga, Stephen F. Donovan
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Publication number: 20100184817Abstract: Methods and compositions for the topical or transdermal treatment of neuropathy. More particularly, transdermal or topical compositions including a combination of ingredients that provide a surprising degree of effective relief from the symptoms of peripheral neuropathy and methods for administering the compositions to treat various neuropathies.Type: ApplicationFiled: March 29, 2010Publication date: July 22, 2010Applicant: TARAXOS INC.Inventor: Richard Wolicki
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Publication number: 20100159015Abstract: Disclosed herein are systems and methods for contributing to the local treatment of pain. More specifically, the disclosed systems and methods contribute to the local treatment pain by inhibiting the NF?B family of transcription factors.Type: ApplicationFiled: February 5, 2010Publication date: June 24, 2010Applicant: WARSAW ORTHOPEDIC, INC.Inventors: Eric N. Burright, Lisa L. Shafer, Bill McKay, John Zanella
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Publication number: 20100160332Abstract: The adrenergic receptors or adrenoceptors are a family of G-protein coupled receptors split into ? and ? subclasses. The adrenoceptors have important roles in regulating a myriad of physiological conditions and their malfunction has been implicated in the pathophysiology of a number of diseases. Disclosed herein are a series of novel compounds which are ligands of the alpha2-adrenoceptor (?2-ARs) subclass of adrenergic receptors. The invention also provides for pharmaceutical compositions comprising the novel compounds. The compounds are suitable for use in the manufacture of medicaments for the treatment of ?2-ARs associated disorders, such as depression and schizophrenia.Type: ApplicationFiled: December 22, 2009Publication date: June 24, 2010Applicant: The Provost, Fellows and Scholars of the College of the Holy and Undivided Trinity of Queen ElizabeInventors: Maria Isabel Rozas Hernando, Fernando Rodriguez Royo
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Publication number: 20100137369Abstract: Flowable pharmaceutical depots are described. The flowable pharmaceutical depot includes a polyester, such as a polylactic acid or a poly(trimethylene carbonate) endcapped with a primary alcohol and a pain relieving therapeutic agent, such as a post operative pain relieving therapeutic agent. Method of making and using the same are also described.Type: ApplicationFiled: December 1, 2008Publication date: June 3, 2010Applicant: Medtronic, Inc.Inventors: Michael Eric BENZ, Christopher M. Hobot, Phillip Edward McDonald, Lian Leon Luo, John Kramer
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Patent number: 7728028Abstract: Substituted imidazoline derivatives corresponding to Formula I: a method for producing them from substituted aldehyde compounds of Formula B: and the use of such imidazoline derivatives and aldehyde compounds to treat pain, depression, urinary incontinence, diarrhea, pruritus, alcohol and drug misuse, drug dependency, lethargy and/or anxiety.Type: GrantFiled: June 20, 2008Date of Patent: June 1, 2010Assignee: Gruenenthal GmbHInventors: Beatrix Merla, Stefan Oberboersch, Bernd Sundermann, Werner Englberger, Hagen-Heinrich Hennies, Heinz Graubaum
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Methods and materials for determining pain sensitivity and predicting and treating related disorders
Publication number: 20100132058Abstract: Methods of treating somatosensory disorders and modulating production of proinflammatory cytokines by administering to a subject an effective amount of a COMT modulator, ADRB2 modulator, ADRB3 modulator or combinations thereof are provided. Methods of predicting effective pharmacological therapies for a subject afflicted with a somatosensory disorder by determining a genotype of the subject with regard to a gene selected from the group consisting of COMT, ADRB2, ADRB3, and combinations thereof are further provided. Methods of determining pain responses or pain perception and predicting susceptibility of a subject to develop related disorders, such as somatosensory disorders and somatization, by determining a genotype of the subject with regard to a gene selected from the group consisting of COMT, ADRB2, ADRB3, and combinations thereof are further provided.Type: ApplicationFiled: July 25, 2005Publication date: May 27, 2010Inventors: Luda B. Diatchenko, William Maixner, Gary Slade, Andrea Gail Neeley -
Publication number: 20100130502Abstract: In methods, compounds, and topical formulations for treatment of inflammatory skin disorders incorporating compounds represented by the formulas below: wherein each of R1, R2, and R3 is independently hydrogen, hologen, alkyl, or alkoxy; each of R4 and R5 is independently hydrogen, alkyl, or alkoxy; and each of R6 and R7 is independently hydrogen, nitro, alkyl, or alkoxy; wherein each of A1, A3, and A4 is independently hydrogen or alkyl; and A2 is independently hydrogen or hydroxy; and wherein each of B1, B2, and B3 is independently hydrogen, hydroxy, or alkoxy; and each of B4 and B5 is independently hydrogen or alkyl, applying such compounds topically as sprays, mists, aerosols, solutions, lotions, gels, creams, ointments, pastes, unguents, emulsions, and suspensions to treat inflammatory skin disorders and the symptoms associated therewith.Type: ApplicationFiled: November 18, 2009Publication date: May 27, 2010Applicant: GALDERMA LABORATORIES, INC.Inventors: Jack A. DeJovin, Isabelle Jean DeJovin
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Publication number: 20100125076Abstract: Substituted sulphonamides having the general formula (I) and salts, hydrates and solvates thereof were prepared and described, wherein R1 is CO or SO2 and R2 is NH or O and where R represents linear or cyclic aliphatic chain and n represents number of linking aliphatic chain carbons (n can be 0, 1, 2 or 3), which are useful in the manufacture of the medicaments due to the carboanhydrase inhibition. These compounds are prepared by nucleophilic reaction of an amine with 4-sulfamoylbenzenesulphonyl chloride in the presence of triethylamine excess in tetrahydrofurane or in ether at temperature 0 to 20° C. The compounds show an antiglaucomatic activity.Type: ApplicationFiled: April 20, 2008Publication date: May 20, 2010Applicant: Unimed Pharma, Spol. S R.O.Inventors: Fridrich Gregan, Milan Remko, Elena Sluciakova, Jarmila Knapikova
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Publication number: 20100120881Abstract: The present invention relates to imidazoline derivatives and their use as insecticidal, acaricidal, molluscicidal and nematocidal agents. The invention also extends to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising such imidazoline derivatives, and to methods of using such derivatives and/or compositions to combat and control insect, acarine, mollusc and nematode pests. In particular the present invention relates to imidazolines with alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl, heteroaryl or heterocyclyl substituents.Type: ApplicationFiled: January 18, 2008Publication date: May 13, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Anthony Cornelius O'Sullivan, Christoph Luethy, Jurgen Harry Schaetzer
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Publication number: 20100120882Abstract: The present invention relates to imidazoline derivatives and their use as insecticidal, acaricidal, molluscicidal and nematocidal agents. The invention also extends to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising such imidazoline derivatives, and to methods of using such derivatives and/or compositions to combat and control insect, acarine, mollusc and nematode pests. In particular the present invention relates to imidazolines with alkyl and fluoro substituents.Type: ApplicationFiled: January 28, 2008Publication date: May 13, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Christoph Luethy, Anthony Cornelius O'Sullivan, Jürgen Harry Schaetzer
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Publication number: 20100112027Abstract: A method for causing a permanent increase in the length and girth of a male subject's penis, the method comprising treatment comprising the step of (a) administering to the male an effective amount of a vasodilator selected from the group consisting of a vasodilator per se and compositions thereof comprising a pharmaceutically-acceptable diluent or carrier, to induce a cumulative prolonged engorgement of the subject's penis; and (b) repeating step (a) as necessary to cause the increase during the treatment. A potentiator which enhances the effect of the vasodilator may also be used.Type: ApplicationFiled: January 14, 2010Publication date: May 6, 2010Inventor: Kenneth W. Adams
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Publication number: 20100113379Abstract: The present invention relates to the induction of autophagy via mTOR independent pathways which modulated intracytosolic cAMP levels. In some embodiments, autophagy may be induced in a cell by reducing intracytosolic cAMP levels, for example using a cAMP antagonist, such as clonidine. This may be useful, for example in the treatment of neurodegenerative disorders or pathogen infections.Type: ApplicationFiled: February 14, 2008Publication date: May 6, 2010Inventors: David Rubinsztein, Sovan Sarkar, Andrea Williams
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Publication number: 20100093783Abstract: 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: ApplicationFiled: December 11, 2009Publication date: April 15, 2010Inventors: Hanne Anette Moesgaard, Karin Lowenstein Christensen
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Publication number: 20100063123Abstract: A composition and method of treating adrenergic dysregulation by administering the composition is disclosed, wherein the composition comprises a a2-adrenergic receptor agonist; a pharmaceutically acceptable hydrophilic matrix and a release-retardant of a metal alkyl sulfate. In embodiments, the composition provides a sustained release of the agonist, wherein after administration of the composition no more than once about every 12 hours to a subject having a steady state plasma concentration of the a2-adrenergic receptor agonist, the agonist's plasma concentration peak-to-trough ratio is no greater than about 1.9.Type: ApplicationFiled: November 10, 2009Publication date: March 11, 2010Inventors: Henry Joseph Horacek, Min Michael He, Moise A. Khayrallah
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Publication number: 20100035854Abstract: A dry powder suitable for inhalation in a dry powder inhaler, the powder comprising a carrier, an active agent and at least 0.5% by weight of magnesium stearate, the powder being further characterized in that the less than 10% of the surface of the carrier material is covered with particles of magnesium stearate. The invention is also directed to a method of making dry powders by blending together the ingredients mentioned in a diffusion blender for a period time that is less than 60 minutes.Type: ApplicationFiled: August 6, 2009Publication date: February 11, 2010Inventors: Rudi Mueller-Walz, Roland Steiner