2-imidazolines Patents (Class 514/401)
-
Publication number: 20100034902Abstract: The present invention provides methods for measuring, detecting, diagnosing, treating, and researching salt sensitivity and related conditions. In particular, the present invention provides methods for measuring, detecting, diagnosing, treating, and researching salt sensitivity through measuring aberrant red blood cell based potassium efflux levels. In addition, the present invention provides methods for treating conditions involving salt sensitivity (e.g., hypertension), preventing the onset of conditions involving salt sensitivity, identifying individuals at risk for developing salt sensitivity and related conditions, identifying new types of treatment for salt sensitivity and related conditions, and evaluating the effectiveness of treatments for conditions involving salt sensitivity (e.g., hypertension).Type: ApplicationFiled: January 17, 2008Publication date: February 11, 2010Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Maria Carolina Delgado, Bertram Pitt
-
Publication number: 20100029618Abstract: Disclosed herein is a pharmaceutical composition comprising a pain-relieving anticonvulsant and an pan-alpha-2 adrenergic receptor agonist. The composition is effective for treating chronic pain, and methods of treating chronic pain using the composition and the compounds comprising it are also disclosed.Type: ApplicationFiled: December 14, 2007Publication date: February 4, 2010Inventors: Daniel W. Gil, John E. Donello
-
Publication number: 20100029662Abstract: 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.Type: ApplicationFiled: July 27, 2009Publication date: February 4, 2010Inventor: Gerald Horn
-
Publication number: 20100029660Abstract: 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.Type: ApplicationFiled: July 27, 2009Publication date: February 4, 2010Inventor: Gerald Horn
-
Publication number: 20100029663Abstract: 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.Type: ApplicationFiled: July 27, 2009Publication date: February 4, 2010Inventor: Gerald Horn
-
Publication number: 20100029654Abstract: Methods and compositions for the treatment of Alzheimer's Disease are described. More specifically, the invention demonstrates that administration of cardiovascular agents to a mammal suffering from the symptoms of Alzheimer's Disease causes an amelioration of those symptoms. The finding of the present invention can be used in treatment regimens designed to attenuate or prevent Alzheimer's Disease.Type: ApplicationFiled: March 22, 2007Publication date: February 4, 2010Inventor: Giulio Pasinetti
-
Publication number: 20100022574Abstract: The present invention relates, in general to treatment of pain comprising administering an alpha-2 adrenergic agonist and an endothelin antagonist, wherein administration of the agents acts as an analgesic and ameliorates pain in a subject.Type: ApplicationFiled: July 28, 2008Publication date: January 28, 2010Applicant: EndogenX, Inc.Inventor: Anil Gulati
-
Patent number: 7652055Abstract: The present invention relates to compounds of formula I wherein X—Y, R1, and n are as defined herein and to their pharmaceutically active salts. Compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1 and are useful for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), 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.Type: GrantFiled: June 25, 2008Date of Patent: January 26, 2010Assignee: Hoffman-La Roche Inc.Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
-
Patent number: 7652030Abstract: 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: September 18, 2002Date of Patent: January 26, 2010Assignee: Nycomed Danmark APSInventors: Hanne Anette Moesgaard, Karin Lowenstein Christensen
-
Patent number: 7652056Abstract: 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: GrantFiled: April 6, 2005Date of Patent: January 26, 2010Assignee: Board of Trustees of Michigan State UniversityInventors: Jetze J. Tepe, Satyamaheshwar Peddibhotla
-
Publication number: 20100003353Abstract: In a method for treating an affected skin region of a patient having a skin disorder, a vasodilation composition is applied to an affected skin region of a patient, the affected skin region exhibiting a skin disorder characterized by at least one abnormal blood vessel, and the affected skin region is then treated so as to non-invasively disrupt tissue architecture, e.g., by inducing ischemia, of the at least one abnormal blood vessel. A vasoconstriction composition can then be applied to the skin region to cause vasoconstriction of the at least one blood vessel in order to promote healing.Type: ApplicationFiled: June 11, 2009Publication date: January 7, 2010Applicant: BIOCHEMICS, INC.Inventors: Laura Stephens, John J. Masiz, Stephen G. Carter, Zhen Zhu, Kanu Patel
-
Publication number: 20090275603Abstract: A new class of imidazolines as 4-position 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. The compositions are also useful for treating autoimmune diseases and for inhibiting rejection of organ and tissue transplants.Type: ApplicationFiled: April 3, 2009Publication date: November 5, 2009Inventors: Jetze J. Tepe, Peddibhotla Satyamaheshwar
-
Publication number: 20090263441Abstract: Effective treatments of pain and/or inflammation are provided. Through the administration of an effective amount of at least analgesic and/or at least one anti-inflammatory agent at or near a target site, one can reduce, prevent or treat inflammation and pain.Type: ApplicationFiled: April 18, 2008Publication date: October 22, 2009Applicant: Warsaw Orthopedic, Inc.Inventor: William McKay
-
Publication number: 20090263451Abstract: Effective treatments of myofascial pain and/or inflammation are provided. Through the administration of an effective amount of at least one anti-inflammatory agent and/or analgesic at or near a target site, one can reduce, prevent or treat myofascial pain and/or inflammation.Type: ApplicationFiled: April 14, 2009Publication date: October 22, 2009Applicant: Warsaw Orthopedic, Inc.Inventor: Vanja M. King
-
Publication number: 20090263450Abstract: Effective treatments of pain and/or inflammation from tendonitis, carpal tunnel syndrome, tarsal tunnel syndrome, osteoarthritis, bursitis and/or an oral-facial disease 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 pain and/or inflammation from tendonitis, carpal tunnel syndrome, tarsal tunnel syndrome, osteoarthritis, bursitis and/or an oral-facial disease.Type: ApplicationFiled: April 13, 2009Publication date: October 22, 2009Applicants: Warsaw Orthopedic, Inc., Medtronic, Inc.Inventors: John Myers ZANELLA, William F. McKay, Vanja Margareta King, Christopher M. Hobot, Keith R. Hildebrand
-
Method for Treating Acute Pain with a Formulated Drug Depot in Combination with a Liquid Formulation
Publication number: 20090264489Abstract: Effective methods for treating pain are provided. Through the injection of liquid formulation comprising an active ingredient followed by the administration of drug depot comprising an active ingredient at or near a target site, one can effectively treat pain. This methodology is particularly effective to treat acute radicular pain.Type: ApplicationFiled: March 4, 2009Publication date: October 22, 2009Applicants: Warsaw Orthopedic, Inc., Medtronic, Inc., A Minnesota CorporationInventors: Keith R. HILDEBRAND, Christopher M. Hobot, John Myers Zanella, Vanja Margareta King -
Publication number: 20090263443Abstract: Effective treatments of spasticity and shivering that accompanies surgeries are provided. Through the administration of an effective amount of clonidine at or near a target site, one can relax muscle fibers. This administration of clonidine or a pharmaceutically acceptable salt thereof is particularly useful following the surgery.Type: ApplicationFiled: March 20, 2009Publication date: October 22, 2009Applicant: WARSAW ORTHOPEDICS, INC.Inventor: Vanja King
-
Publication number: 20090264491Abstract: The present invention is directed to an implantable drug depot useful for reducing, preventing or treating post-operative pain in a patient in need of such treatment, the implantable drug depot comprising a therapeutically effective amount of clonidine or pharmaceutically acceptable salt thereof and a polymer; wherein the depot is implantable at a site beneath the skin to reduce, prevent or treat post-operative pain, and the depot is capable of releasing (i) about 5% to about 45% of the clonidine or pharmaceutically acceptable salt thereof relative to a total amount of the clonidine or pharmaceutically acceptable salt thereof loaded in the drug depot over a first period of up to 48 hours and (ii) about 55% to about 95% of the clonidine or pharmaceutically acceptable salt thereof relative to a total amount of the clonidine or pharmaceutically acceptable salt thereof loaded in the drug depot over a subsequent period of at least 3 days.Type: ApplicationFiled: April 9, 2009Publication date: October 22, 2009Applicants: WARSAW ORTHOPEDIC, INC., MEDTRONIC, INC.Inventors: William F. MCKAY, Amira WOHABREBBI, Vanja Margareta KING, Phillip Edward MCDONALD, Christopher M. HOBOT, Troy CARTER
-
Publication number: 20090264490Abstract: Effective treatments of pain for extended periods of time are provided. Through the administration of an effective amount of clonidine at or near a target site, one can relieve pain caused by diverse sources, including but not limited to spinal disc herniation (i.e. sciatica), spondilothesis, stenosis, discogenic back pain and joint pain, as well as pain that is incidental to surgery. When appropriate formulations are provided within biodegradable polymers, this relief can be continued for at least three days. In some embodiments, the relief can be for at least twenty-five days, at least fifty days, at least one hundred days, at least one hundred and thirty-five days or at least one hundred and eighty days.Type: ApplicationFiled: April 8, 2009Publication date: October 22, 2009Applicants: Warsaw Orthopedic, Inc., Medtronic, Inc.Inventors: John Myers ZANELLA, Christopher M. Hobot, Danielle L. Biggs, Katara Shaw, Phillip Edward McDonald, Vanja Margareta King, William F. McKay, Kathy L. Remsen
-
Publication number: 20090246256Abstract: The present invention provides for compositions and methods for accelerating the rate of delivery of lofexidine to the systemic circulation by transmucosal administration through the nasal, sublingual, or buccal routes to provide rapid response in the treatment of opiate addicts, migraine, neuropathic pain, and other therapeutic indications related to lofexidine, to a patient in need of such treatment. Compositions of lofexidine formulated for transmucosal delivery are provided. Also provided are methods for the treatment of opiate addicts, migraine, neuropathic pain, and other therapeutic indications related to lofexidine. The methods utilize lofexidine compositions formulated for transmucosal delivery through nasal, sublingual, or buccal routes of administration in an amount effective for the treatment of the drug indications.Type: ApplicationFiled: March 24, 2009Publication date: October 1, 2009Inventor: Abeer M. Al-Ghananeem
-
Publication number: 20090239918Abstract: The invention provides methods for treating pain in mammals. In particular, the invention provides well-defined aminoimidazolines, aminothiazolines, and aminooxazolines and pharmaceutical compositions thereof to treat pain.Type: ApplicationFiled: March 23, 2009Publication date: September 24, 2009Applicant: ALLERGAN, INC.Inventors: Janet A. Takeuchi, Ling Li, Todd M. Heidelbaugh, Ken Chow, Karen M. Kedzie, Daniel W. Gil, Wenkui K. Fang
-
Publication number: 20090232886Abstract: Pharmaceutical fixed dose combination products are formed by merging a fixed dose of a first pharmaceutical formulation from primary module, with a fixed dose of a second pharmaceutical formulation from a secondary module In a preferred embodiment the first and second pharmaceutical formulations are separated from one another in a three piece capsule, a capsule-in-a-capsule or a tablet-in-a-capsule, and the primary and secondary modules are interchangeable.Type: ApplicationFiled: May 22, 2009Publication date: September 17, 2009Inventor: Raymundo A. Sison
-
Publication number: 20090233943Abstract: This invention relates to novel compounds having the structural formula I below: and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.Type: ApplicationFiled: May 14, 2008Publication date: September 17, 2009Applicants: Astex Therapeutics Limited, AstraZeneca ABInventors: Jeremy Nicholas Burrows, Sven Hellberg, Katharina Hogdin, Sofia Karlstrom, Karin Kolmodin, Johan Lindstrom, Can Slivo
-
Publication number: 20090214504Abstract: A method for treating a patient suffering from a wound, ulcer, or inflammation includes providing a topical formulation comprising a carrier and a combination of active ingredients that includes at least one retinoid and at least one blood vessel dilator, and applying the topical formulation to the skin of the patient to cause healing, accelerated healing or prevention of the wound, ulcer or inflammation. Additional active ingredients may include a promoter of mitochondrial function or an antioxidant.Type: ApplicationFiled: January 22, 2009Publication date: August 27, 2009Applicant: BIOCHEMICS, INC.Inventors: Stephen G. Carter, Zhen Zhu, Kanu Patel, Diane L. Kozwich
-
Patent number: 7579481Abstract: A method of 4-substituted imidazole-2-ones and thiones which comprises reacting a methylene urea or methylene thiourea wherein said methylene is substituted with the 4-subsituent and a cyano or alkycarboxylate group to provide said 4-substituted imidazole 2-one or thione.Type: GrantFiled: August 25, 2006Date of Patent: August 25, 2009Assignee: Allergan, Inc.Inventors: Michael E. Garst, Lloyd Dolby, Shervin Esfandiari
-
Publication number: 20090209422Abstract: Certain substituted aminoalkyl heteroaryl and heterocyclyl derivatives have provided unexpected insecticidal and acaricidal activity. These compounds are represented by formula I: wherein R, R1, R2, R3 and R4 are folly described herein. 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 an additional compound, with at least one insecticidally compatible 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: ApplicationFiled: May 2, 2006Publication date: August 20, 2009Applicant: Bayer CropScience AGInventors: John A. Dixson, George Theodoridis, Zeinab M. Elshenawy, Benjamin J. Dugan, Manorama M. Patel, John W. Lyga, Stephen F. Donovan, Ping Ding
-
Patent number: 7575757Abstract: The present invention provides compositions and stable liquid formulations comprising alpha adrenergic receptor antagonists and use thereof for increasing blood flow. In one embodiment, the stable liquid formulations of this invention are useful for reversing the effects of an anesthetic agent, preferably a long-lasting local anesthetic agent administered in conjunction with an alpha adrenergic receptor agonist.Type: GrantFiled: March 18, 2005Date of Patent: August 18, 2009Assignee: Novalar Pharmaceuticals, Inc.Inventors: Andrew X. Chen, Julius Knowles, Eckard Weber
-
Publication number: 20090197932Abstract: This invention relates to an alpha-1A 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: ApplicationFiled: February 4, 2009Publication date: August 6, 2009Inventors: Counde O'Yang, Dennis Mitsugu Yasuda
-
Publication number: 20090197934Abstract: This invention relates to an alpha-1A 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: ApplicationFiled: February 4, 2009Publication date: August 6, 2009Inventors: Counde O'Yang, Robert Greenhouse
-
Publication number: 20090197933Abstract: 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: ApplicationFiled: February 4, 2009Publication date: August 6, 2009Inventors: Counde O'Yang, Dennis Mitsugu Yasuda
-
Publication number: 20090197931Abstract: 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: ApplicationFiled: February 4, 2009Publication date: August 6, 2009Inventors: Counde O'Yang, Robert Greenhouse
-
Patent number: 7569230Abstract: The present invention provides compositions and stable liquid formulations comprising alpha adrenergic receptor antagonists and use thereof for increasing blood flow. In one embodiment, the stable liquid formulations of this invention are useful for reversing the effects of an anesthetic agent, preferably a long-lasting local anesthetic agent administered in conjunction with an alpha adrenergic receptor agonist.Type: GrantFiled: December 15, 2006Date of Patent: August 4, 2009Assignee: Novalar Pharmaceuticals, Inc.Inventors: Andrew X Chen, Julius Knowles, Eckard Weber
-
Publication number: 20090169621Abstract: A microcrystalline cellulose-based excipient having improved compressibility, whether utilized in direct compression, dry granulation or wet granulation formulations, is disclosed. The excipient is an agglomerate of microcrystalline cellulose particles and from about 0.1% to about 20% silicon dioxide particles, by weight of the microcrystalline cellulose, wherein the microcrystalline cellulose and silicon dioxide are in intimate association with each other. The silicon dioxide utilized in the novel excipient has a particle size from about 1 nanometer to about 100 microns. Most preferably, the silicon dioxide is a grade of colloidal silicon dioxide.Type: ApplicationFiled: December 15, 2008Publication date: July 2, 2009Applicant: J. Rettenmaier & Soehne GmbH + Co. KGInventors: Bob Sherwood, John H. Staniforth, Edward Hunter
-
Patent number: 7553862Abstract: The present invention relates to compounds of formula I wherein R1, R2, R3, and R4 are as defined herein and to pharmaceutically acceptable acid addition salts thereof. Compounds of formula I or their tautomeric forms are good inhibitors of the glycine transporter 1 (GlyT-1), and have a good selectivity to glycine transporter 2 (GlyT-2) inhibitors. Such compounds are useful for the treatment of schizophrenia.Type: GrantFiled: March 1, 2007Date of Patent: June 30, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Synese Jolidon, Robert Narquizian, Roger Norcross, Emmanuel Pinard
-
Publication number: 20090143364Abstract: and the pharmaceutically acceptable salts and esters thereof, wherein X1, X2, X3, Y1, Y2 and R are described herein inhibit the interaction of MDM2 protein with a p53-like peptide and hence have anti proliferative activity.Type: ApplicationFiled: February 5, 2009Publication date: June 4, 2009Inventors: Nader Fotouhi, Gregory Jay Haley, Klaus B. Simonsen, Binh Thanh Vu, Stephen Evan Webber
-
Publication number: 20090130178Abstract: Formulations have been developed which assist individuals having an addiction such as smoking to reduce or quit engaging in the addictive behavior. Representative behaviors include smoking, excessive alcohol or food ingestion, drug addiction, and ingestion of caffeine or junk food providing quick “highs”. The formulations assist the smoker to become dissatisfied with smoking, until he or she willingly gives up the habit or at least cuts down on the number of cigarettes smoked per day as an initial step towards quitting in the future. The formulations can also be used in conjunction with other known formulations, such as nicotine gum or patch. The formulations contain hydrophilic polymers, for example, polyethylene glycol (PEG) alone or in combination or polyvinyl pyrrolidone (PVP) (also known as povidone or polyvidone alone or in combination.), sweeteners and/or flavorings, viscosity modifiers/binders, and pH or buffering agents.Type: ApplicationFiled: November 19, 2007Publication date: May 21, 2009Applicant: Xvasive, Inc.Inventors: Bryan T. Oronsky, Neil C. Oronsky, Arnold L. Oronsky
-
Patent number: 7528161Abstract: A new class of imidazolines as 4-position 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. The compositions are also useful for treating autoimmune diseases and for inhibiting rejection of organ and tissue transplants.Type: GrantFiled: December 3, 2003Date of Patent: May 5, 2009Assignee: Michigan State UniversityInventor: Jetze J. Tepe
-
Publication number: 20090105222Abstract: Methods for the prevention or treatment of stress-related disorders by administering a therapeutically effective amount of a dual serotonin/norepinephrine reuptake inhibitor to an individual under stress are described. A triple monoamine reuptake inhibitor for serotonin/noradrenaline/dopamine may also be administered to an individual at risk for a stress-related disorder. In a preferred embodiment the compound is milnacipran and is prophylactically administered at an effective amount to delay or prevent stress-related disorders in an individual at risk.Type: ApplicationFiled: September 19, 2008Publication date: April 23, 2009Applicant: Cypress Bioscience, Inc.Inventors: Jay D. Kranzler, Srinivas G. Rao
-
Publication number: 20090087490Abstract: 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: June 6, 2008Publication date: April 2, 2009Applicant: Addrenex Pharmaceuticals, Inc.Inventors: Henry Joseph Horacek, Min Michael He, Moise A. Khayrallah
-
Patent number: 7495108Abstract: The present invention relates to 1,2,4-tri-substituted imidazoline derivatives, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said imidazoline derivatives, to methods for the preparation of these intermediates, to pharmaceutical compositions containing one or more of these imidazoline derivatives as active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification.Type: GrantFiled: January 12, 2007Date of Patent: February 24, 2009Inventors: Josephus H. M. Lange, Cornelis G. Kruse, Herman H. Van Stuivenberg
-
Publication number: 20090048323Abstract: 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: ApplicationFiled: June 20, 2008Publication date: February 19, 2009Applicant: Gruenenthal GMBHInventors: Beatrix Merla, Stefan Oberboersch, Bernd Sundermann, Werner Englberger, Hagen-Heinrich Hennies, Heinz Graubaum
-
Publication number: 20090023639Abstract: 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 oxidase inhibitor. The methods are particularly useful in treating cardiac cachexia.Type: ApplicationFiled: August 15, 2008Publication date: January 22, 2009Inventors: Stefan Dietmar Anker, Andrew Justin Stewart Coats
-
Publication number: 20090018180Abstract: The present invention relates to compounds of formula I wherein X—Y, R1, and n are as defined herein and to their pharmaceutically active salts. Compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1 and are useful for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), 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.Type: ApplicationFiled: June 25, 2008Publication date: January 15, 2009Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
-
Publication number: 20090012070Abstract: It has now been found that certain novel heterocyclic derivatives 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) 112, -, where R, R, R6, R7, R8, R11, 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 compatible 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: ApplicationFiled: August 22, 2008Publication date: January 8, 2009Applicant: Bayer Cropscience AGInventors: 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
-
Publication number: 20080319041Abstract: The invention relates to methods for treatment of CNS disease and pathologies using non-racemic mixtures of lofexidine enantiomers. The invention also relates to processes for the manufacture of chirally pure enantiomers of lofexidine.Type: ApplicationFiled: March 14, 2006Publication date: December 25, 2008Inventors: George Digenis, Peter A. Crooks, Abeer Al-Ghananeem
-
Patent number: 7459473Abstract: This invention relates to novel N-linked sulfonamides of N-heterocyclic carboxylic acid and carboxylic acid isosteres, their preparation, and use for treating neurological disorders including physically damaged nerves and neurodegenerative diseases, and for treating alopecia and promoting hair growth.Type: GrantFiled: December 3, 1998Date of Patent: December 2, 2008Assignee: Glia Med, Inc.Inventors: Gregory S. Hamilton, Mark H. Norman, Yong-Qian Wu
-
Publication number: 20080287460Abstract: This invention relates to novel compounds having the structural formula I below: and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.Type: ApplicationFiled: May 14, 2008Publication date: November 20, 2008Applicants: Astex Therapeutics Limited, AstraZeneca ABInventors: Jeremy Nicholas Burrows, Sven Hellberg, Katharina Hogdin, Sofia Karlstrom, Karin Kolmodin, Johan Lindstrom, Can Slivo
-
Publication number: 20080261873Abstract: Disclosed are methods of treating a disorder of the stomach, intestine or duodenum in a human subject. The method includes administering to the subject, a pharmaceutical composition comprising a compound that increases gastrointestinal motility (e.g., by modulating myenteric nerve activity) and/or induces the secretion or production of growth hormone.Type: ApplicationFiled: August 18, 2005Publication date: October 23, 2008Applicant: ELIXIR PHARMACEUTICALS, INC.Inventor: Bard J. Geesaman
-
Patent number: 7439241Abstract: In methods, compounds, and topical formulations for treatment of rosacea 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 rosacea and its symptoms.Type: GrantFiled: May 25, 2004Date of Patent: October 21, 2008Assignee: Galderma Laboratories, Inc.Inventors: Jack A. DeJovin, Isabelle Jean DeJovin
-
Publication number: 20080200335Abstract: The present invention relates to 1-(imidazolin-2-yl)amino-1,2-diphenylethane compounds of the formula I and their agriculturally acceptable salts, wherein A is a radical of the formula A1 or A2. The invention relates also to agricultural compositions and to seed comprising at least one compound I and/or a salt thereof, as well as a method of combating animal pests, a method for protecting crops from attack or infestation by animal pests and a method for protecting non-living materials from attack or infestation by animal pests, a method for the protection of seeds from animal pests and of the seedlings' roots and shoots from animal pests by applying a pesticidally effective amount of at least one 1-(imidazolin-2-yl)amino-1,2-diphenylethane compound I and/or a salt thereof.Type: ApplicationFiled: May 18, 2006Publication date: August 21, 2008Inventors: Markus Kordes, Norbert Gotz, Michael Rack, Christopher Koradin, Livio Tedeschi, Deborah L. Culbertson