The Chalcogen Is Bonded Directly To Two Carbon Atoms Patents (Class 514/239.2)
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Publication number: 20110275616Abstract: Methods of utilizing an opioid agonist in a mammalian subject in a manner that inhibits peripheral effects of the opioid agonist are described. The methods comprise administering the opioid agonist in an amount sufficient to confer analgesia the subject and co-administering a neutral opioid antagonist or pharmaceutically acceptable isomorph or pharmaceutically acceptable salt thereof in an amount sufficient to substantially inhibit peripheral effects and insufficient to block substantial central effects of the opioid agonist in the subject.Type: ApplicationFiled: July 18, 2011Publication date: November 10, 2011Applicant: AIKO BIOTECHNOLOGYInventors: Wolfgang Sadée, Edward Bilsky, Janet Yancey-Wrona
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Publication number: 20110251198Abstract: Provided here are methods of manufacture of viloxazine and its various salts, as well as viloxazine-related compounds, such as novel intermediate reaction products and polymorphs thereof. In particular, the methods provide a substantially pure API of viloxazine HCl while avoiding undesirable impurities. The methods further provide for separating, identifying, and characterizing novel polymorphs of viloxazine. Further provided are methods for synthesis and identification and characterization of novel intermediates of viloxazine, as well as for some important metabolites and precursors of metabolites of viloxazine.Type: ApplicationFiled: April 12, 2011Publication date: October 13, 2011Applicant: Supernus Pharmaceuticals Inc.Inventors: Likan Liang, Padmanabh P. Bhatt, David Dain, Jean-Philippe Taquet, Aleksandr Pechenov, Alexei Tchesnokov, Reynold Mariaux
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Publication number: 20110237593Abstract: Topical anti-pruritic compositions and methods of using the same to treat pruritus. These anti-pruritic compositions are capable of temporarily or permanently reducing, inhibiting, treating, ameliorating, and/or preventing pruritic skin conditions, as well as other related skin conditions. In a particular aspect, the present formulations provide a quicker and more effective treatment of pruritus than do certain present pruritus-treating compositions.Type: ApplicationFiled: June 8, 2011Publication date: September 29, 2011Applicant: STIEFEL LABORATORIES, INC.Inventors: Kathleen L. CLARK, Joanne M. FRASER
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Publication number: 20110224179Abstract: We disclose a diagnostic test to determine suitable therapeutic intervention of subjects suffering from subclinical Cushing's syndrome [SCS] and also agents that antagonise the action of cortisol or inhibit excess cortisol production in the treatment of conditions such as SCS in the presence of an adrenal incidentaloma.Type: ApplicationFiled: November 7, 2008Publication date: September 15, 2011Inventor: John Newell-Price
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Publication number: 20110206780Abstract: The present invention relates to new morphinan modulators of NMDA receptors, ?1 receptors, ?2 receptors, and/or ?3?4 nicotinic receptors, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: January 5, 2011Publication date: August 25, 2011Applicant: Auspex Pharmaceuticals, Inc.Inventors: Thomas G. Gant, Sepehr Sarshar, Chengzhi Zhang
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Publication number: 20110189160Abstract: Methods and compositions for treating skin conditions in animals, which tend to have higher skin pH than humans, including wounds, ulcers, rashes, burns, abrasions, and other irritations and relevant injuries are provided. The invention contemplates the use of an aqueous or emollient medium having non-occlusive properties with one or more pH raising ingredients in a composition specifically designed to deliver oxygen to the skin's surface.Type: ApplicationFiled: September 10, 2010Publication date: August 4, 2011Inventor: Jennifer Bartels
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Publication number: 20110190301Abstract: Therapeutic compounds, methods, and compositions are disclosed herein for treating glaucoma and baldness in mammals. The specific compounds are described herein and are modified prostaglandin derivates.Type: ApplicationFiled: May 13, 2009Publication date: August 4, 2011Applicant: ALLERGAN, INC.Inventors: David W. Old, Vinh X. Ngo, Todd S. Gac
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Publication number: 20110178088Abstract: This invention relates to tetrahydro-naphthalene derivatives and salts thereof which are useful as an active ingredient of pharmaceutical preparations. The tetrahydro-naphthalene derivatives of the present invention have excellent activity as VR1 antagonist and useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, overactive bladder, urge urinary incontinence, chronic pain, neuropathic pain, post-operative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD.Type: ApplicationFiled: March 21, 2011Publication date: July 21, 2011Applicant: XENTION LIMITEDInventors: Masaomi Tajimi, Toshio Kokubo, Masahiro Shiroo, Yasuhiro Tsukimi, Takeshi Yura, Klaus Urbahns, Noriyuki Yamamoto, Muneto Mogi, Hiroshi Fujishima, Tsutomu Masuda, Nagahiro Yoshida, Toshiya Moriwaki
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Publication number: 20110178084Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof are disclosed, wherein a dashed line represents the presence or absence of a bond; and, wherein Y, A, R, D, and n are as described. Methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: May 13, 2009Publication date: July 21, 2011Applicant: ALLERGAN, INC.Inventors: David W. Old, Vinh X. Ngo
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Publication number: 20110150766Abstract: A transdermal patch having a top region containing an antagonist followed by a bottom region containing an agonist, whereby the bottommost end of the bottom region is secured to the skin of the patient for delivering a prescribed dosage of agonist to the patient over a predetermined period of time, the antagonist will be released by migrating or moving from the top region through the bottom region to the patient to prevent overdose. Visual indicators are provided in the patch for changing color to separately indicate the operation of the patch, delivery of prescribed dosage, and/or overdosage.Type: ApplicationFiled: February 23, 2011Publication date: June 23, 2011Inventor: Robert B. Royds
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Publication number: 20110152268Abstract: The present invention relates to a pharmaceutical composition for treating nociceptive pain, containing a morpholine derivative or a pharmaceutically acceptable salt thereof, as an active ingredient. The present invention is useful in providing an excellent pharmaceutical composition for treating nociceptive pain. In addition, the present invention is particularly useful in providing a pharmaceutical composition for treating pain accompanying a disease selected from the group consisting of rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, spondylosis deformans, gouty arthritis, juvenile arthritis, scapulohumeral periarthritis, and cervical syndrome, lumbago, lumbago accompanying spondylosis deformans, menalgia, pain and tumentia after inflammation, operation or injury, pain after odontectomy, and cancer pain. In addition, the present invention is particularly useful for alleviating pain in a damaged cartilage region, and is particularly useful for osteoarthritis in which NSAIDs are not effective.Type: ApplicationFiled: September 10, 2009Publication date: June 23, 2011Applicant: ASTELLAS PHARMA INC.Inventors: Nobuaki Takeshita, Fusako Nishigaki, Toshiaki Aoki, Seiji Tamura, Kazumi Kikuchi, Akio Kuroda
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Publication number: 20110152255Abstract: Compounds comprising formula (I) or a pharmaceutically acceptable salt thereof, are disclosed, wherein J, B, Y, and A are as described in claims 1-13. Methods, compositions, and medicaments related thereto are also disclosed, for treating baldness, glaucoma or inflammatory bowel diseases.Type: ApplicationFiled: April 21, 2009Publication date: June 23, 2011Inventors: Yariv Donde, Jeremiah H. Nguyen
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Patent number: 7964599Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein J, B, Y, and A are as described. Methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: May 1, 2009Date of Patent: June 21, 2011Assignee: Allergan, Inc.Inventors: Yariv Donde, Jeremiah H. Nguyen
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Publication number: 20110136742Abstract: The invention provides antidepressant prodrugs comprising an antidepressant conjugated to one or more amino acids. The invention also relates to pharmaceutical compositions comprising an antidepressant prodrug, and to methods of preparing and using the same.Type: ApplicationFiled: February 22, 2007Publication date: June 9, 2011Inventors: Travis Mickle, Wendy Hirschelman Severs
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Publication number: 20110117055Abstract: Provided herein are hepatitis C virus entry inhibitor oxoacetamide compounds, pharmaceutical compositions thereof, and methods for their use in treatment or prevention of hepatitis C virus infection in a subject in need thereof.Type: ApplicationFiled: November 18, 2010Publication date: May 19, 2011Inventors: James E. MacDonald, McKelvy F. Jeffrey, Flossie Wong-Staal
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Patent number: 7943612Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are activators of PPAR? and should be useful for treating conditions mediated by the same.Type: GrantFiled: March 7, 2007Date of Patent: May 17, 2011Assignee: High Point Pharmaceuticals, LLCInventor: Per Sauerberg
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Publication number: 20110110870Abstract: Skin care compositions comprising certain phenoxyalkylamines, which are particularly beneficial for skin lightening and achieving evenness of color, especially for face and underarm skin.Type: ApplicationFiled: November 9, 2009Publication date: May 12, 2011Applicant: CONOPCO, INC., D/B/A UNILEVERInventors: Jose Guillermo ROSA, Bijan HARICHIAN, John Steven BAJOR, Carol Annette BOSKO, Diana Jean DRENNAN, John Chun-Sing NIP
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Publication number: 20110105506Abstract: Diaminoalkanes of Formula I have now been found which are orally active and bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with elevated levels of aspartic protease activity. The invention also relates to a method for the use of the compounds of Formula I in ameliorating or treating aspartic protease related disorders in a subject in need thereof comprising administering to said subject an effective amount of a compound of Formula I.Type: ApplicationFiled: May 28, 2010Publication date: May 5, 2011Inventors: John J. Baldwin, David A. Claremon, Colin M. Tice, Salvacion Cacatian, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wei Zhao, Robert D. Simpson, Suresh B. Singh, Patrick T. Flaherty, Jean-Pierre Wery
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Publication number: 20110105507Abstract: Provided are new functionalized surfactants and methods of their preparation and use. The surfactants are compounds of formula I: wherein R1, R2, and R3 are as defined herein.Type: ApplicationFiled: October 21, 2010Publication date: May 5, 2011Inventors: Matthias S. Ober, Edward D. Daugs, Wanglin Yu, Cynthia L. Rand
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Publication number: 20110086845Abstract: This invention provides agents, compositions, pharmaceutical compositions and methods for treating or slowing the progression of a neurodegenerating disease, such as Alzheimer's disease and a demyelinating disease.Type: ApplicationFiled: October 18, 2010Publication date: April 14, 2011Applicant: The Board of Trustees of the University of IllinoisInventors: Douglas L. Feinstein, Maria Vittoria Simonini, Sergey Kalinin, Paul E. Polak
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Patent number: 7919617Abstract: The present invention provides low molecular weight compounds useful as cytokine inhibitors, and compositions thereof. In particular, compounds of the invention are useful as anti-inflammatory agents. There are further provided methods for the preparation of such agents and their use in preventing or treating conditions mediated by cytokines such as arthritis.Type: GrantFiled: December 14, 2009Date of Patent: April 5, 2011Assignee: iTherX Pharmaceuticals Inc.Inventors: Erik Boman, Susana Conde Ceide, Russell Dahl, Nancy G. J. Delaet, Justin Ernst, Antonio Garrido Montalban, Jeffrey Kahl, Christopher Larson, Stephen Miller, Hiroshi Nakanishi, Edward Roberts, Eddine Saiah, Robert Sullivan, Zhinjun Wang
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Publication number: 20110059967Abstract: Compounds comprising Formula (I) or a pharmaceutically acceptable salt thereof, are disclosed, wherein J1, J2, U1, B, Y, and A are as described in claims 1-16. Methods, compositions, and medicaments related thereto are also disclosed, for treating glaucoma, inflammatory bowel disease and baldness.Type: ApplicationFiled: May 4, 2009Publication date: March 10, 2011Applicant: Allergan Inc.Inventors: David W. Old, Vinh X. Ngo
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Publication number: 20110039813Abstract: Disclosed are use of a benzophenone derivative represented by general formula (I) or a salt thereof and one or more immunosuppressing agents in combination, and a pharmaceutical composition containing the benzophenone derivative or a salt thereof and one or more immunosuppressing agents. The use and the composition are useful for treatment or prevention of autoimmune diseases and the like. (In the formula, R1 represents an optionally substituted heterocyclic group, a substituted phenyl group or the like; Z represents an alkylene group or the like; R2 represents a carboxyl group, which may be protected by an alkyl group, or the like; R3 represents an optionally protected hydroxyl group or the like; R4 represents an optionally substituted cycloalkyloxy group or the like; and R5 represents a hydrogen atom or the like.Type: ApplicationFiled: April 20, 2009Publication date: February 17, 2011Applicant: Toyama Chemical Co., Ltd.Inventors: Yukihiko Aikawa, Shunichi Shiozawa
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Publication number: 20110039853Abstract: Novel substituted benzamide based inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.Type: ApplicationFiled: February 19, 2008Publication date: February 17, 2011Inventor: Soren Ebdrup
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Publication number: 20110021499Abstract: Urethral suppositories containing a mixed-activity anti-cholinergic drug and methods of use for treatment of over-active bladder are provided. Buffering drugs to pH near their pKas can result in a desired proportion of uncharged drug and can enhance absorption of the agents into urethral tissues.Type: ApplicationFiled: July 22, 2009Publication date: January 27, 2011Inventors: Amie Ellen Franklin, Dennis H. Giesing
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Publication number: 20110009351Abstract: The present invention relates to a novel assay or screen for identifying compounds with potential therapeutic value for the treatment of protein trafficking diseases such as Cystic Fibrosis (CF) and nephrogenic diabetes insipidus (NDI). The usual approach involves expressing the mutant form of the gene in cells and assaying function in a multiwell format when cells are exposed to libraries of compounds. Although such functional assays are useful, they do not directly test the ability of a compound to correct defective trafficking of the protein. To address this a novel corrector screening assay for CF has been developed in which the appearance of the mutant protein at the cell surface is measured as the assay output. This assay was used to screen more than 3100 compounds. This novel screening approach to protein trafficking diseases is robust and general, and may enable the selection of molecules that can be translated rapidly to a clinical setting.Type: ApplicationFiled: May 9, 2008Publication date: January 13, 2011Inventors: David Y. Thomas, John Hanrahan, Graeme Carlile, Renaud Robert
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Publication number: 20100311754Abstract: Naphthalene-based compounds having linked heterocyclic and aromatic rings capable of inhibiting P38, methods for inhibiting P38 in vivo or in vitro, diagnostics for determining activity in the treatment of P38 and/or cytokine-associated conditions and methods for treating conditions associated with P38 activity or cytokine activity; more particularly naphthalene-based compounds of Formula (I) having a morpholine heterocyclic ring, and methods of use thereof.Type: ApplicationFiled: August 11, 2010Publication date: December 9, 2010Applicant: ARQULE, INC.Inventors: Mark A. Ashwell, Yanbin Liu, Syed Ali, Jason Hill, Woj Wrona
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Publication number: 20100305131Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, B1, X and n are defined herein. The invention also relates a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: May 27, 2010Publication date: December 2, 2010Inventors: Gary Mark Coppola, Yuki Iwaki, Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi, Robert Sun
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Publication number: 20100305130Abstract: A single-use sprayer for nasal anesthesia is disclosed. The single-use sprayer includes a single dose of anesthetic and a delivery system adapted to dispense the single dose of anesthetic into a nostril. The single-use sprayer prevents patient-to-patient contamination, is easy to use and allows for self-administration, and has a simple, disposable configuration so as to lower the production cost.Type: ApplicationFiled: June 1, 2009Publication date: December 2, 2010Inventor: Thomas PHILLIPS
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Publication number: 20100297077Abstract: The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.Type: ApplicationFiled: October 3, 2008Publication date: November 25, 2010Applicant: BIONOMICS LIMITEDInventors: Bernard Luke Flynn, Jonathan Bayldon Baell, Jason Hugh Chaplin, Girmit Singh Gill, Damian Wojciech Grobelny, Andrew John Harvey, Jorgen Alvar Mould, Dharam Paul
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Patent number: 7829560Abstract: 1,4 disubstituted napthylenes, of formula (I), are disclosed. These compounds may be useful in treating cell-proliferative diseases.Type: GrantFiled: July 8, 2005Date of Patent: November 9, 2010Assignee: Arqule, Inc.Inventors: Mark A. Ashwell, Yanbin Liu, Syed Ali, Jason Hill, Woj Wrona
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Publication number: 20100279997Abstract: A compound, composition and method are disclosed that can provide analgesia. A contemplated compound has a structure that corresponds to Formula A, wherein A, B, X, R1, R2, R7 and R8, and the dashed lines are defined within.Type: ApplicationFiled: October 28, 2009Publication date: November 4, 2010Inventors: Lindsay Burns Barbier, Hoau-Yan Wang, Nan-Horng Lin, Andrei Blasko
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Publication number: 20100279996Abstract: A compound, composition and method are disclosed that can provide analgesia. A contemplated compound has a structure that corresponds to Formula I, wherein R1 and R2 are substituents, and W is a ring structure that are defined within.Type: ApplicationFiled: May 4, 2009Publication date: November 4, 2010Inventors: Lindsay Burns Barbier, Hoau-Yan Wang, Nan-Horng Lin, Andrei Blasko
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Publication number: 20100273797Abstract: The present invention provides low molecular weight compounds useful as cytokine inhibitors, and compositions thereof. In particular, compounds of the invention are useful as anti-inflammatory agents. There are further provided methods for the preparation of such agents and their use in preventing or treating conditions medicated by cytokines such as arthritis.Type: ApplicationFiled: July 2, 2010Publication date: October 28, 2010Inventors: Erik Boman, Susana Conde Ceide, Russell Dahl, Nancy G. J. Delaet, Justin Ernst, Antonio Garrido Montalban, Jeffrey Kahl, Christopher Larson, Stephen Miller, Hiroshi Nakanishi, Edward Roberts, Eddine Saiah, Robert Sullivan, Zhijun Wang
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Publication number: 20100247453Abstract: A composition comprising an antacid, and a local, topical anesthetic. The composition is used to relieve pain or discomfort associated with a sore throat, and therefore, the invention is also directed to a method of alleviating the pain or discomfort associated with a sore throat comprising instructing a human to orally administer the composition.Type: ApplicationFiled: May 12, 2010Publication date: September 30, 2010Inventor: Thomas L. Jones
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Publication number: 20100240644Abstract: The present invention provides a morpholine derivative of the formula [I]; wherein R1 is a substituted alkyl group, an optionally substituted aryl group, an optionally substituted heterocyclo group, a cycloalkyl group or an alkyl group; R2 is a substituted alkyl group, an optionally substituted aryl group, an optionally substituted heterocyclo group, an optionally substituted alkylcarbonyl group, an optionally substituted arylcarbonyl group, an optionally substituted heterocyclo-substituted carbonyl group or a cycloalkylcarbonyl group; T is a methylene group or a carbonyl group; R3, R4, R5 and R6 are the same or different and a hydrogen atom, an optionally substituted carbamoyl group or an optionally substituted alkyl group; or pharmaceutically acceptable salts thereof. These compounds are useful as a renin inhibitor.Type: ApplicationFiled: June 16, 2008Publication date: September 23, 2010Inventors: Hidenori Akatsuka, Hiroshi Sugama, Nobumasa Awai, Takayuki Kawaguchi, Yoichi Takahashi, Toru Iijima, Jingkang Shen, Guangxin Xia, Jianshu Xie
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Publication number: 20100233244Abstract: The present invention relates to a quickly decomposing oral drug preparation, for the application of active ingredient combinations for smoking withdrawal, which contains nicotine, a nicotine salt, a nicotine derivative, or a substance that reacts to nicotine, in combination with another active ingredient, and the use of such a drug preparation for the treatment of smoking withdrawal, and the use of nicotine, and/or nicotine salts or derivatives, for the production of medications for the treatment of smoking withdrawal. The active ingredient that is to be administered, in combination, for this purpose is a centrally active ingredient, preferably an antidepressant for the fighting of psychic dependency in terms of a smoking withdrawal therapy. The administration of the active ingredient combination to the patient should be handled in a simple and reliable way and should exclude side effects to a large extent.Type: ApplicationFiled: June 4, 2007Publication date: September 16, 2010Applicant: LTS Lohmann Therapie-Systeme AGInventors: Hans-Rainer Hoffmann, Reto Brändli, Frank Theobald
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Publication number: 20100210653Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome proliferator-activated receptors (PPAR), in particular the PPAR? suptype.Type: ApplicationFiled: April 30, 2010Publication date: August 19, 2010Applicant: HIGH POINT PHARMACEUTICALS, LLCInventors: Miroslav Havranek, Per Sauerberg, Ingrid Pettersson
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Publication number: 20100190793Abstract: Disclosed are compositions for affecting weight loss comprising a first compound and a second compound, where the first compound is an opioid antagonist and the second compound causes increased agonism of a melanocortin 3 receptor (MC3-R) or a melanocortin 4 receptor (MC4-R) compared to normal physiological conditions. Also disclosed are methods of affecting weight loss, increasing energy expenditure, increasing satiety in an individual, or suppressing the appetite of an individual, comprising identifying an individual in need thereof and treating that individual to antagonize opioid receptor activity and to enhance ?-MSH activity.Type: ApplicationFiled: March 31, 2010Publication date: July 29, 2010Applicant: Orexigen Therapeutics, Inc.Inventors: Eckard Weber, Michael Alexander Cowley
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Patent number: 7750012Abstract: The present invention relates to a chemical genus of biaryl nitrogen-attached heterocycles that are inhibitors of LTA4H (leukotriene A4 hydrolase). The compounds have the general formula They are useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders.Type: GrantFiled: August 3, 2006Date of Patent: July 6, 2010Assignee: deCODE genetics ehfInventors: Vincent Sandanayaka, Jasbir Singh, Li-Ming Zhou, Mark E. Gurney
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Patent number: 7750004Abstract: Compounds which inhibit the activity of anti-apoptotic Mcl-1 protein, compositions containing the compounds and methods of treating diseases during which are expressed the Mcl-1 protein are disclosed.Type: GrantFiled: July 7, 2006Date of Patent: July 6, 2010Assignee: Abbott LaboratoriesInventors: Michael D. Wendt, Hong Ding, Sheela A. Thomas, Steven W. Elmore, Wang Shen, Daniel A. Dickman, David Augeri
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Publication number: 20100166889Abstract: The invention provides methods of treating depressive disorders, in particular major depression but other depressive orders also, with prodrug stimulants or analogs including amphetamine prodrugs, methylphenidate prodrugs, and methylphenidate analogs, Such methods of treatment may utilize the prodrug stimulant or analog as monotherapy or, more commonly, as an adjunct to antidepressant medication treatment to augment their effect. The invention includes combination methods of treatment in which an amphetamine prodrug, methylphenidate prodrug, or methylphenidate analog is administered to an individual in need with one or more other active agents, either in separate forms or as a single pharmaceutical formulation. Packaged pharmaceutical compositions containing an amphetamine or methylphenidate prodrug, instructions for using the prodrug to treat certain disorders, and optionally one or more other active agents are provided by the invention.Type: ApplicationFiled: December 23, 2009Publication date: July 1, 2010Applicant: LCS GROUP, LLCInventor: Louis Sanfilippo
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Patent number: 7745439Abstract: The inventive indene derivatives of formula (I) are capable of selectively modulating the activities of peroxisome proliferator activated receptors (PPARs), causing no adverse side effects, and thus, they are useful for the treatment and prevention of disorders modulated by PPARs, i.e., metabolic syndromes such as diabetes, obesity, arteriosclerosis, hyperlipidemia, hyperinsulinism and hypertension, inflammatory diseases such as osteoporosis, liver cirrhosis and asthma, and cancer.Type: GrantFiled: April 12, 2005Date of Patent: June 29, 2010Assignees: Korea Research Institute of Chemical Technology, Jeil Pharm. Co., Ltd., Korea Research Institute of Bioscience and Biotechnology, CJ Corp.Inventors: Hyae Gyeong Cheon, Sung-Eun Yoo, Sung Soo Kim, Sung-Don Yang, Kwang-Rok Kim, Sang Dal Rhee, Jin Hee Ahn, Seung Kyu Kang, Won Hoon Jung, Sung Dae Park, Nam Gee Kim, Sun Mee Kim, Kil Woong Mo, Jae Mok Lee, Hye Jung Kang, Koun Ho Lee, Jong Hoon Kim, Jeong-Hyung Lee, Seung Jun Kim
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Publication number: 20100160294Abstract: A reduction in the side effects of treating with an agent having combined 5HT2/5HT3 and alpha-2 antagonistic activity is obtained by administering an agent having selective norepinephrine reuptake inhibitory or histamine H1 agonist activity. A combined dosage form comprising an agent having 5HT2/5HT3 and alpha-2 antagonistic activity and an agent having selective norepinephrine reuptake inhibitory or histamine H1 agonist activity is presented. Some embodiments of the combined dosage form comprise an immediate release component comprising an agent having 5HT2/5HT3 and alpha-2 antagonistic activity and a delayed release component comprising an agent having selective norepinephrine reuptake inhibitor or histamine H1 agonist activity.Type: ApplicationFiled: December 14, 2009Publication date: June 24, 2010Inventors: Srinivas Rao, Jay Kranzler, Jeffery J. Anderson
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Publication number: 20100159033Abstract: The present invention relates to new benzisoxazole modulators of D2 receptors and/or 5-HT2A receptors, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: September 25, 2009Publication date: June 24, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Manoucherhr M. Shahbaz
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Publication number: 20100137316Abstract: The present invention provides compounds of Formula I wherein R1, R2, R3, and n have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of conditions including urinary disorders, pain, premature ejaculation, ADHD and fibromyalgia. Also provided are pharmaceutical compositions comprising one or more compounds of Formula I.Type: ApplicationFiled: February 9, 2010Publication date: June 3, 2010Inventors: Paul Vincent Fish, Malcolm Christian MacKenny, Alan Stobie, Florian Wakenhut, Gavin Alistair Whitlock
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Patent number: 7723334Abstract: Methods and compositions for treating humans suffering from, or preventing a human from suffering, a physiological or psychiatric disease, disorder, or a condition where inhibiting reuptake of norepinephrine is a benefit are disclosed. The compositions comprise a compound having a pharmacological selectivity of serotonin (Ki)/norepinephrine (Ki) of at least about 5000. Examples of such compounds include reboxetine, and more preferably optically pure (S,S) enantiomer of reboxetine. The methods generally include administration of a therapeutic amount of such compositions. Also disclosed are preparations of a medicament from the composition, and uses of the composition in a manufacture of the medicament to treat a human suffering from, or preventing a human from suffering, a physiological or psychiatric disease, disorder, or condition.Type: GrantFiled: October 30, 2007Date of Patent: May 25, 2010Assignee: Pfizer Inc.Inventors: Erik H. F. Wong, Saeeduddin Ahmed, Robert C. Marshall, Robert McArthur, Duncan P. Taylor, Lars Birgerson, Pasquale Cetera
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Publication number: 20100119622Abstract: The present invention relates to new 3H-benzooxazol-2-one modulators of D2 receptors and/or 5-HT1A receptors, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: September 15, 2009Publication date: May 13, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20100113451Abstract: The present invention relates to an agent for preventing and/or treating diabetic neuropathy comprising a 2-[(substituted-inden-7-yloxy)methyl]morpholine of the formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient. The invention is useful for providing an excellent agent for preventing and/or treating diabetic neuropathy, and particularly useful for providing an agent for preventing and/or treating diabetic motor neuropathy (such as muscle weakness disorder (such as muscle weakness disorder with inability to walk independently)), diabetic sensory neuropathy (such as paresthesia (such as vibration perception abnormality), allodynia, hypoesthesia (such as numbness of extremities or cold sensation), or pain), or diabetic autonomic neuropathy (such as stool abnormality (such as constipation or diarrhea), urination disorder, impotence, orthostatic hypotension, sudomotor dysfunction, abnormal heart rate variability, or delayed gastric emptying).Type: ApplicationFiled: March 14, 2008Publication date: May 6, 2010Applicant: Astellas Pharma Inc.Inventors: Toshiaki Aoki, Nobuhito Murai, Seiji Tamura, Hiroko Yamamoto, Nozomu Hamakawa
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Publication number: 20100105631Abstract: Inositol derivatives are described that are represented by the structural formula I wherein X is a radical of scyllo-inositol wherein one or more of R1, R2, R3, R4, R5, and R6 are independently alkyl, alkenyl, alkynyl, alkylene, alkenylene, alkoxy, alkenyloxy, cycloalkyl, cycloalkenyl, cycloalkoxy, aryl, aryloxy, arylalkoxy, aroyl, heteroaryl, heterocyclic, acyl, acyloxy, sulfoxide, sulfate, sulfonyl, sulfenyl, sulfonate, sulfinyl, amino, imino, azido, thiol, thioalkyl, thioalkoxy, thioaryl, nitro, cyano, halo, seleno, silyl, silyloxy, silylthio, carboxyl, carbonyl, carbamoyl, or carboxamide and the other of R1, R2, R3, R4, R5, or R6 are hydroxyl, or pharmaceutically acceptable salts thereof. The compounds, compositions comprising same and methods using same are described for use in the prevention and/or treatment of diseases characterized by abnormal protein folding or aggregation or amyloid formation, desposition, accumulation or persistence.Type: ApplicationFiled: November 11, 2009Publication date: April 29, 2010Inventors: Antonio Curz, Linda Kurdydyk