Chalcogen Bonded Directly To The 2-and 6- Positions Of The Purine Ring System (e.g., Theophylline, Etc.) Patents (Class 514/263.34)
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Publication number: 20130316024Abstract: A cosmetic kit and the use thereof for improving the appearance of the skin is described. Further described, is the prevention and/or controlling of cellulite or the orange peel syndrome and/or for slimming down the figure, through the increase of the elasticity and firmness of the skin by stepping up collagen synthesis, for increasing blood microcirculation and for improving thermoregulation of the skin.Type: ApplicationFiled: November 18, 2011Publication date: November 28, 2013Applicant: RHODIA POLIAMIDA E ESPECIALIDADES LTDAInventors: Gabriel Gorescu, Thomas Canova, Tarcis Cordeiro Bastos, Karla Laguens
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Publication number: 20130309200Abstract: New imidazo[1,2-b]pyridazine and imidazo[4,5-b]pyridine derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).Type: ApplicationFiled: November 24, 2011Publication date: November 21, 2013Applicant: ALMIRALL, S.A.Inventors: Jacob Gonzalez Rodriguez, Bernat Vidal Juan, Laura Vidal Gispert, Jordi Bach TaƱa
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Publication number: 20130310347Abstract: High throughput methods for identifying novel inhibitors of Hsp90 chaperone protein folding are disclosed. The inhibitors so identified disrupt the binding of p23 to either Hsp90? or Hsp90? and have selective activity against the proliferation of cancer cells. In particular are provided embodiments of therapeutic compositions that comprise at least one inhibitor of an Hsp90 chaperone activity, the inhibitor being any of the compounds designated as CP1-CP19 as shown in FIGS. 1A-1D or a 2-(trifluoromethyl)pyrimidin-2-yl)thio)acetamide derivatives.Type: ApplicationFiled: May 21, 2013Publication date: November 21, 2013Applicant: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Carmel Chan, Sanjiv S. Gambhir, David E. Solow-Cordero, Aileen Hoehne, Ramasamy Paulmurugan
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Publication number: 20130302264Abstract: Provided are indole alkaloid compounds of formula I, for example, pubescine, and the use of such compounds and compositions thereof to promote (e.g., enhance) melanogenesis and pigmentation. Also provided are plant extracts containing a compound of formula I, for example, pubescine, and the use of such a plant extract to promote (e.g., enhance) melanogenesis and pigmentation. The compound or plant extract may be prepared as pharmaceutical and cosmetic compositions, and may be used for the prevention and treatment of conditions that are related to aberrant melanogenesis activity.Type: ApplicationFiled: November 16, 2011Publication date: November 14, 2013Applicant: NEW YORK UNIVERSITYInventors: Seth J. Orlow, Li Ni Komatsu
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Patent number: 8580801Abstract: Methods and compositions are disclosed for the treatment of diseases or conditions produced by or associated with low cyclic nucleotide levels. The compositions comprise phosphodiesterase inhibitors and are formulated for intranasal and pulmonary administration.Type: GrantFiled: July 23, 2009Date of Patent: November 12, 2013Inventor: Robert I. Henkin
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Publication number: 20130289055Abstract: A powder of cold-soluble polysaccharide and polyol, which is highly viscous in water and suitable for direct compression, and a method for preparing the powder and uses thereof are described, the powder being notably intended for preparing solid forms with controlled release of an active principle.Type: ApplicationFiled: November 2, 2011Publication date: October 31, 2013Applicant: ROQUETTE FRERESInventors: Baptiste Boit, Fabrice Buquet, Gregory Le Bihan, Philippe Lefevre
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Patent number: 8563564Abstract: The present invention relates to a composition for external skin application having a skin-moisturizing effect, which comprises gallocatechin gallate as an active ingredient. More particularly, the composition for external skin application comprises gallocatechin gallate as an active ingredient to activate peroxisome proliferator activated receptor isoform alpha (PPAR-?), to stimulate expression of filaggrin and involucrin that are skin-moisturizing factors, and thus to provide excellent anti-drying and skin-moisturizing effects. More particularly, the composition for external skin application may further comprise theobromine and quercetin in addition to gallocatechin gallate to maximize such effects.Type: GrantFiled: June 22, 2011Date of Patent: October 22, 2013Assignee: Amorepacific CorporationInventors: Hyun Jung Shin, Jeong Ki Kim, Su Nam Kim, Sang Min Lee, Byeong Gon Lee, Ih Seop Chang
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Publication number: 20130273183Abstract: 2-Pyrimidine thioesters and thiocarbonates are disclosed as effective skin brightening agents. These compounds may be formulated with dermatologically acceptable carriers to form skin brightening compositions. Methods for brightening skin and for inhibiting melanogenesis using these agents are also disclosed.Type: ApplicationFiled: April 13, 2012Publication date: October 17, 2013Applicant: EASTMAN CHEMICAL COMPANYInventors: Stephanie Kay Clendennen, Liu Deng, Neil Warren Boaz
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Publication number: 20130267515Abstract: A method for treating an ATP analog-induced side effect in a subject comprises administering an effective amount of an adenosine receptor antagonist to the subject. A method for treating cancer in a subject comprises administering a nucleobase and/or nucleoside prior to administering an ATP analog.Type: ApplicationFiled: October 26, 2011Publication date: October 10, 2013Applicant: Alberta Health ServicesInventors: Michael Bruce Sawyer, Vijayalakshmi Damaraju
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Publication number: 20130261136Abstract: Embodiments are related to compositions of matter comprising a food, drug, cosmetic, dietary supplement, or biologic product, said product comprised of a phytochemical fraction recovered from a crude caffeine, said phytochemical fraction having a ratio of polyphenols to caffeine of about 20, 10-30 or 40, or greater than 10. In related embodiments, said phytochemical fraction is a retentate of a filtration process of a water suspension of crude caffeine, and wherein said crude caffeine is a product of a green coffee bean decaffeination process. In other related embodiments, said compositions of matter are useful for facilitating neuroprotection, inhibiting COX-2 or stimulating glucose uptake.Type: ApplicationFiled: October 12, 2011Publication date: October 3, 2013Inventors: Yi-Fang Chu, Yumin Chen, Peter H. Brown, Barbara J. Lyle
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Publication number: 20130224318Abstract: The present invention describes methods for improving the appearance of skin, particularly, treating, ameliorating, preventing, delaying, and/or improving one or more signs of excess accumulation and/or production of subcutaneous fat, such as cellulite, and conditions related thereto, by topically applying compositions comprising Carnitine Palmitoyl Transferase-1 (CPT-1) modulators, optionally with other anti-lipid agents; and also describes compositions and methods for treating, preventing and improving the appearance of skin, particularly, treating, preventing, ameliorating, reducing and/or eliminating loss of subcutaneous fat in the skin, wherein the compositions include natural plant constituents that stimulate lipid synthesis.Type: ApplicationFiled: February 26, 2013Publication date: August 29, 2013Applicant: Avon Products, Inc.Inventor: Avon Products, Inc.
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Publication number: 20130216634Abstract: An extraction method for extracts of Pelargonium citronellum with improved methylhexaneamine content is provided. The method involves separating the oil phase from the aqueous phase; concentrating the aqueous phase; purifying the oil phase; and recombining the resulting material. Additionally, extracts of Pelargonium citronellum prepared by the extraction method are provided. The extracts are useful in compositions, for example as dietary supplements, and for appetite suppression.Type: ApplicationFiled: March 12, 2013Publication date: August 22, 2013Inventors: James Akrong, Shawn Shirazi, Jason Peters, John Doherty
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Publication number: 20130210840Abstract: A cellulite-reducing topical composition comprising a lecithin organogel, an ethylene oxide-propylene oxide-ethylene oxide triblock copolymer, caffeine, a retinoid, and optionally at least one vitamin, vitamin derivative or vitamin precursor.Type: ApplicationFiled: June 13, 2011Publication date: August 15, 2013Applicant: IMPRIMIS PHARMACEUTICALS, INC.Inventors: Joseph Grasela, Joachim Schupp, Sergio Nacht
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Patent number: 8507506Abstract: The theophylline derivative disclosed in the present invention is characterized by having the pharmaceutical functions of osteoporosis. The theophylline derivative protects against bone resorption and inflammatory mediator infiltration.Type: GrantFiled: July 8, 2011Date of Patent: August 13, 2013Assignee: Kaohsiung Medical UniversityInventors: Jwu-Lai Yeh, Ing-Jun Chen
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Publication number: 20130202667Abstract: The present invention relates to hydrogel particles coated with lipid, which are made from dispersing hydrogel particles in an organic solvent in which lipids are dissolved, and to a method for manufacturing same. Unlike the existing method for manufacturing hydrogel core vesicles, the present invention can effectively manufacture same by using an emulsification method, without involving the steps of chemical treatment of the surface of hydrogels or dilution, thereby facilitating mass production and preventing the decrease of drug encapsulation efficiency.Type: ApplicationFiled: October 12, 2011Publication date: August 8, 2013Applicant: AMOREPACIFIC CORPORATIONInventors: Eun Jung An, Do Hoon Kim, Hyung Jun Lim, Jong Won Shim, Choon Bok Jeong, Lee Kyoung Kwon, Jun Oh Kim
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Patent number: 8481060Abstract: The present invention relates to a process for producing a solid, coated pharmaceutical composition by a melt coating process. The process is adapted to provide a solid, coated pharmaceutical composition by melt coating, which has a fast release.Type: GrantFiled: December 17, 2009Date of Patent: July 9, 2013Assignee: Losan Pharma GmbHInventors: Peter Kraahs, Stefanie Bold, Lars Fahsel
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Publication number: 20130165427Abstract: Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein.Type: ApplicationFiled: August 24, 2012Publication date: June 27, 2013Applicant: HYDRA BIOSCIENCES, INC.Inventor: Jayhong A. Chong
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Publication number: 20130165418Abstract: The invention is directed in part to oral dosage forms comprising a combination of an opioid agonist, acetaminophen and an orally active opioid antagonist, the opioid antagonist being included in a ratio to the opioid agonist to provide a combination product which is analgesically effective when the combination is administered orally, but which is aversive in a physically dependent subject. Preferably, the amount of opioid antagonist included in the combination product provides at least a mildly negative, āaversiveā experience in physically dependent addicts (e.g., precipitated abstinence syndrome).Type: ApplicationFiled: December 7, 2012Publication date: June 27, 2013Applicant: Purdue Pharma L.P.Inventor: Purdue Pharma L.P.
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Publication number: 20130150384Abstract: A method for preventing and/or treating brain tumor, including administering caffeine and/or its analog, and/or their pharmaceutically acceptable salt, as an active ingredient, to a patient in need thereof, is provided. The method for preventing or treating brain tumor has an activity to inhibit invasion, migration, and proliferation of brain tumor cells, and thereby very effective for the prevention and treatment of brain tumor.Type: ApplicationFiled: February 15, 2013Publication date: June 13, 2013Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGYInventor: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY
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Publication number: 20130150383Abstract: The present invention relates to therapeutically active xanthine derivative compounds of Formula (I): corresponding processes for manufacture of said derivatives, pharmaceutical formulations containing and uses of such compounds in therapy, particularly in treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficial.Type: ApplicationFiled: February 6, 2013Publication date: June 13, 2013Applicant: GlaxoSmithKline LLCInventors: Ivan Leo PINTO, Shahzad Sharooq Rahman, Neville Hubert Nicholson
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Publication number: 20130143903Abstract: A medicated formulation and method of use for treating migraine having a combination of active ingredients including: nicotine, and tryptophan alone and also with phenylalanine and/or, tyrosine, and/or caffeine in an aqueous solution.Type: ApplicationFiled: January 26, 2012Publication date: June 6, 2013Applicant: NICO WORLDWIDE, INC.Inventor: Joseph Robert Knight
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Publication number: 20130143904Abstract: An agent for inhibiting the activity of inositol-1,4,5-triphospate receptor subtype 3 (IP3R3), containing caffeine and/or its analogs, and/or their pharmaceutically acceptable salts, as an active ingredient, is provided. A composition for preventing and/or treating a disease associated with Ca2+ release through IP3R3, containing the IP3R3 inhibiting agent, is also provided.Type: ApplicationFiled: September 21, 2012Publication date: June 6, 2013Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGYInventor: KOREA INSTITUTE OF SCIENCE AND TECHNOL
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Publication number: 20130137710Abstract: The present invention relates to the cosmetic, dermatological or therapeutic use of certain cyclohexyl carbamate compounds of formula (I) given below, preferably as anti-cellulite actives.Type: ApplicationFiled: May 25, 2010Publication date: May 30, 2013Applicant: SYMRISE AGInventors: Imke Meyer, Heiko Oertling, Nadine Hillebrand, Claudia Gƶmann, Rahim Brodhage
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Publication number: 20130131028Abstract: Described herein are methods for modulation of the activity of the carotid body that afford therapeutic benefit for sleep-related breathing disorders and related conditions.Type: ApplicationFiled: April 11, 2011Publication date: May 23, 2013Applicants: JOHNS HOPKINS UNIVERSITY, SOVA PHARMACEUTICALS, INC., THE UNIVERSITY OF CHICAGOInventors: Solomon H. Snyder, Moataz M. Gadalla, Nanduri R. Prabhakar, Gregory Stein, Gary Pace
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Publication number: 20130131026Abstract: The present invention relates to compositions containing stimulant and anti-histamine compounds, to methods for treating symptoms related to inflammation using the combination compounds, and to a method for preparing the compositions.Type: ApplicationFiled: May 6, 2012Publication date: May 23, 2013Inventor: Mlchael LEIGHTON
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Publication number: 20130123345Abstract: Described herein is a method of treating a viral infection such as an influenza infection, in a subject comprising administering an effective amount of a pharmaceutical composition to disrupt a adenosine receptor pathway, such as the Aradenosine receptor pathway, in a subject. The adenosine receptor pathway includes the steps of 1) producing the adenosine precursor adenosine triphosphate (ATP), 2) releasing ATP into the extracel lular space, 3) enzymatic conversion of ATP to adenosine, 4) activation of the adenosine receptor and the adenosine receptor cascade, and 5) clearance of adenosine from the extracellular space by degradation or uptake into a cell. The method includes affecting at least one of these steps so as to decrease the activation of the adenosine receptor pathway. This may be accomplished by decreasing the production, release, or conversion of ATP to adenosine, decreasing the expression of the adenosine receptor, antagonizing adenosine receptor activation, and/or increasing adenosine clearance.Type: ApplicationFiled: July 22, 2011Publication date: May 16, 2013Applicant: THE OHIO STATE UNIVERSITYInventor: Ian C. Davis
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Patent number: 8440678Abstract: The present invention provides pharmaceutical compositions, which are useful for treatment of depression and the like, and which comprises a compound having an adenosine A2A receptor antagonistic activity such as (E)-8-(3,4-dimethoxystyryl)-1,3-diethyl-7-methyl-3,7-dihydro-1H-purine-2,6-dione or a pharmaceutically acceptable salt thereof and an antidepressant drug (for example, a tricyclic antidepressant, a tetracyclic antidepressant, a selective serotonin reuptake inhibitor, a selective noradrenalin reuptake inhibitor, a dopamine reuptake inhibitor, a serotonin-noradrenalin reuptake inhibitor, monoamine oxidase inhibitor, a 5-HT2 antagonist or the like), and the like.Type: GrantFiled: September 16, 2011Date of Patent: May 14, 2013Assignee: Kyowa Hakko Kirin Co., Ltd.Inventors: Hiroshi Kase, Minoru Kobayashi, Shizuo Shiozaki, Akihisa Mori, Naoki Seno
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Publication number: 20130116221Abstract: Theobromine for use in the treatment of increasing HDL-cholesterol and/or increasing the ratio HDL-cholesterol:LDL-cholesterol in humans and the use of theobromine for increasing HDL-cholesterol in humans, and/or for increasing the ratio HDL-C/LDL-C, and compositions comprising theobromine.Type: ApplicationFiled: May 16, 2011Publication date: May 9, 2013Inventors: Richard Draijer, Bert-Jan Hendrik Van Den Born
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Publication number: 20130095156Abstract: The invention provides disintegratable films containing a mixture of high molecular weight and low molecular weight water soluble components; and a pharmaceutically or cosmetically active ingredient. Optionally, the films contain a starch component, a glucose component, a filler, a plasticizer and/or humectant. The films are preferably in the form of a mucoadhesive monolayer having a thickness sufficient to rapidly disintegrate in the oral environment and release the active ingredient without undue discomfort to the oral mucosa. The monolayer can be cut to any desired size or shape to provide conveniently useable unit dosage forms for administration to oral or other mucosal surfaces for human pharmaceutical, cosmetic, or veterinary applications. The invention further provides methods of administering the film compositions by placing the composition into, for example, the oral cavity for a sufficient period of time to permit the film to disintegrate and release the active ingredient.Type: ApplicationFiled: December 10, 2012Publication date: April 18, 2013Applicant: Adhesives Research, Inc.Inventor: Adhesives Research, Inc.
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Publication number: 20130064789Abstract: The present invention relates to hairy cell leukemia biomarkers and methods of utilizing these biomarkers to diagnose and/or treat hairy cell leukemia.Type: ApplicationFiled: May 10, 2012Publication date: March 14, 2013Inventors: Brunangelo Falini, Raul Rabadan, Enrico Tiacci
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Patent number: 8394808Abstract: The present invention relates to therapeutically active xanthine derivative compounds of Formula (I): corresponding processes for manufacture of said derivatives, pharmaceutical formulations containing and uses of such compounds in therapy, particularly in treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficial.Type: GrantFiled: September 2, 2009Date of Patent: March 12, 2013Assignee: Glaxosmithkline LLCInventors: Ivan Leo Pinto, Shahzad Sharooq Rahman, Neville Hubert Nicholson
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Publication number: 20130053350Abstract: The present invention relates to thiazolidinedione analogues and pharmaceutical compositions that are useful for treating and/or preventing neurodegenerative disorders.Type: ApplicationFiled: December 15, 2010Publication date: February 28, 2013Applicant: Metabolic Solutions Development Company, LLCInventors: Gerard R. Colca, Rolf F. Kletzien, Steve P. Tanis, Scott D. Larsen
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Publication number: 20130052234Abstract: An edible oral strip composition includes a therapeutically effective amount of active agent(s) to provide at least one effect selected from a stimulating effect, an increased physical endurance, alleviate temporary fatigue, improve nervous system functions, and combinations of any of the foregoing. In additional embodiments, the edible strip composition includes a therapeutically effective amount of active agent(s) to provide sleep aid.Type: ApplicationFiled: August 3, 2012Publication date: February 28, 2013Applicant: Purebrands LLCInventors: Michael Goldberg, Ehud Arbit
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Publication number: 20130052280Abstract: The use of theobromine for lowering central blood pressure and/or lowering central pulse pressure in humans and derived benefits, and compositions comprising theobromine.Type: ApplicationFiled: January 18, 2011Publication date: February 28, 2013Inventors: Richard Draijer, Bas Van Den Bogaard
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Publication number: 20130045175Abstract: The present invention relates to the use of a compound of general formula: wherein X is a CiO-24 carbon chain with ānā unsaturations wherein ānā is an integer from zero to 3 for the preparation of a cosmetic composition and a pharmaceutical composition to increase the skin permeation and retention of active ingredients. The present invention is suitable for cosmetic and pharmaceutical products the activity of which is enhanced with increased permeation and retention of active ingredients in the skin as a treatment for cellulite and fat accumulation, acne treatment, skin whitening amongst others.Type: ApplicationFiled: January 6, 2011Publication date: February 21, 2013Applicant: NATURA COSMETICOS S.A.Inventors: Rosa Maria Teixeira Tagae Biaggio, Ana Paula Pedroso De Oliveira, Leda Fernanda Jesus, Mary Sanae Nakamura, Philip Leite Ribeiro
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Patent number: 8372872Abstract: Co-administration of febuxostat and theophylline to a hyperuricemic patient suffering from gout is disclosed.Type: GrantFiled: November 14, 2011Date of Patent: February 12, 2013Assignee: Takeda Pharmaceuticals U.S.A., Inc.Inventors: Lhanoo Gunawardhana, Himanshu Naik, Max Tsai
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Publication number: 20120309677Abstract: The invention relates to methods and compositions for reducing blood glucose levels in hyperglycaemic subjects. The methods and compositions may therefore be suitable for treating a disease or condition associated with hyperglycaemia such as, for example, obesity (particularly diet induced obesity (DIO)), weight gain, Type II diabetes mellitus, insulin sensitivity, impaired glucose tolerance and inflammation. In some embodiments, the methods comprise administering a melanocortin-5 receptor (MC5R) agonist to one or more skeletal muscle cells of the subject. Preferred MC5R agonists are those that specifically activate MC5R and/or enhance expression of MC5R, such as the melanocortin analogue, Ac-Nle-c[Asp-Pro-D-Nal(2?)-Arg-Trp-Lys]-NH2.Type: ApplicationFiled: January 25, 2011Publication date: December 6, 2012Applicant: Monash UniversityInventors: Michael Alexander Cowley, Pablo Jose Enriori, Russell Deputy Brown, Iain James Clarke, Belinda Anne Henry, Maria Cecilia Garcia-Rudaz
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Patent number: 8324224Abstract: Disclosed are novel compounds that are A2B adenosine receptor antagonists, useful for treating various disease states, including asthma and diarrhea.Type: GrantFiled: June 27, 2011Date of Patent: December 4, 2012Assignee: Gilead Sciences, Inc.Inventors: Rao Kalla, Thao Perry, Elfatih Elzein, Vaibhav Varkhedkar, Xiaofen Li, Prabha Ibrahim, Venkata Palle, Dengming Xiao, Jeff Zablocki
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Publication number: 20120275998Abstract: A biodegradable stent comprising a biodegradable material having dissolved therein an acid scavenging agent. The biodegradable material may be PLLA or PLGA. The acid scavenging agent may be also a pharmaceutical agent, for example an antiproliferative agent, coronary vasodilator agent and/or a bronchodilator. Preferably the acid scavenging agent is dipyridamole and/or mopidamol. The invention also provides a method of preparing a biodegradable material for use in the stent of the invention comprising: (i) preparing a formulation of the biodegradable material and the acid scavenging agent; (ii) heating the formulation to melt the biodegradable material and the acid scavenging agent so as to dissolve the agent in the material; and (iii) collecting and cooling the formulation of step (ii).Type: ApplicationFiled: December 2, 2010Publication date: November 1, 2012Inventor: Kadem Gayad Al-Lamee
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Publication number: 20120258087Abstract: The subject of the invention is an isotonic beverage with chelates containing carbohydrates, mineral amino acid chelates, L-carnitine, sweeteners, flavouring substances, and a diluent, the essential feature of the beverage being the content of up to 0.1 wt % of mineral components in the form of mineral amino acid chelates, preferably bisglycinates and glycinates, from 0.1 to 50 wt % of isomaltulose, up to 15 wt % of L-carnitine and/or its derivatives, from 5 to 84% of carbohydrates, up to 50 wt % of bioactive substances, up to 50 wt % of flavouring substances, up to 80 wt % of polyalcohols, diluents, tableting aids, stabilizers, antioxidants, dyes, and 0.013-25 wt % of sweeteners, whereby its osmolarity is 275-295 mOsm/kg and pH is 2-5.Type: ApplicationFiled: January 4, 2010Publication date: October 11, 2012Applicant: OLIMP LABORATORIES SP. Z O.O.Inventors: Marcin Jedlinski, Rafal Jedlinski, Piotr Kula, Justyna Widlak-Kargul, Gertruda Birus-Marszalek
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Publication number: 20120252783Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R4 are as defined herein, the tautomers and the stereoisomers thereof, mixtures thereof, the prodrugs and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: ApplicationFiled: June 15, 2012Publication date: October 4, 2012Applicant: BOEHRINGER INGELHEIM PHARMA & CO. KGInventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf LOTZ
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Publication number: 20120252782Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R4 are defined as in claim 1, the tautomers and the stereoisomers thereof, mixtures thereof, the prodrugs and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: ApplicationFiled: June 15, 2012Publication date: October 4, 2012Applicant: BOEHRINGER INGELHEIM PHARMA GMBH AND CO. KGInventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf R.H. LOTZ
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Patent number: 8268839Abstract: The present invention relates to therapeutically active xanthine derivative compounds of Formula (I): corresponding processes for manufacture of said derivatives, pharmaceutical formulations containing and uses of such compounds in therapy, particularly in treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficial.Type: GrantFiled: March 4, 2010Date of Patent: September 18, 2012Assignee: Glaxosmithkline LLCInventors: Ivan Leo Pinto, Shahzad Sharooq Rahman, Neville Hubert Nicholson
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Publication number: 20120232089Abstract: Anxiety disorders, such as panic disorder, agoraphobia, obsessive-compulsive disorder, social phobia, post-traumatic stress disorder, generalized anxiety disorder, specific phobia, or the like, are treated by administering an effective amount of at least one adenosine A2A receptor antagonist to a patient in need thereof, optionally in combination with an anxiolytic(s) other than the adenosine A2A receptor antagonist.Type: ApplicationFiled: April 16, 2012Publication date: September 13, 2012Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Hiroshi Kase, Naoki Seno, Shizuo Shiozaki, Minoru Kobayashi, Junya Kase
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Publication number: 20120225840Abstract: Hydroxytyrosol or olive juice containing hydroxytyrosol in combination with at least one of the compounds selected from the group consisting of: creatine, coenzyme Q10, resveratrol, caffeine, carnitine, B vitamins (B1, B2, B3, B5, B6, and/or B12) and ginseng (preferably: root) extract can be used to maintain or increase mitochondrial biogenesis in cardiac muscle, skeletal muscles, and liver tissue.Type: ApplicationFiled: October 15, 2009Publication date: September 6, 2012Inventors: Ann Fowler, Angelika Friedel, Darko Knutti, Karin Kuratli, Daniel Raederstorff, Ying Wang-Schmidt, Karin Wertz
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Publication number: 20120225812Abstract: The present invention provides substituted fused pyrimidine compounds of formula (I), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by adenosine receptor (AR) activity. The present invention also provides process of preparation of compounds of formula (I).Type: ApplicationFiled: November 9, 2010Publication date: September 6, 2012Applicant: Advinus Therapeutics LimitedInventors: Vidya Ramdas, Summon Koul, Sujay Basu, Yogesh Waman, Yogesh Shejul, Dinesh Barawkar, Ventaka Poornapragnacharyulu Palle
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Publication number: 20120225142Abstract: An extraction method for extracts of Pelargonium citronellum with improved methylhexaneamine content is provided. The method involves separating the oil phase from the aqueous phase; concentrating the aqueous phase; purifying the oil phase; and recombining the resulting material. Additionally, extracts of Pelargonium citronellum prepared by the extraction method are provided. The extracts are useful in compositions, for example as dietary supplements, and for appetite suppression.Type: ApplicationFiled: August 8, 2011Publication date: September 6, 2012Inventors: James Akrong, Shawn Shirazi, Jason Peters, John Doherty
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Publication number: 20120208829Abstract: 2-Phenoxy pyrimidinone analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.Type: ApplicationFiled: August 22, 2011Publication date: August 16, 2012Applicant: Neurogen CorporationInventors: Rajagopal Bakthavatchalam, Scott M. Capitosti, Jianjun Xu, Bertrand L. Chenard, Manuka Ghosh, Charles A. Blum
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Publication number: 20120208832Abstract: The present invention provides a process for converting a solid (meth)acrylate copolymer into a dispersed form by preparing an aqueous dispersion comprising the components (a) a (meth)acrylate copolymer which is composed of free-radical polymerized methyl methacrylate, ethylacrylate and a salt of 2-trimethylammoniumethyl methacrylate, present in solid form as a powder or as a granulate, (b) up to 50% by weight calculated on the (meth)acrylate copolymer (a) of a dispersing agent selected from the groups of (b) i) plasticizers in combination with emulsifiers and/or (b) ii) pharmaceutically acceptable carbohydrates having 6 to 18 carbon atoms with a functional group and (c) water by mixing the components (a), (b) and (c) to give a suspension which becomes an aqueous dispersion during the conversion of the solid (meth)acrylate copolymer into the dispersed form, characterized in that, the (meth)acrylate copolymer is converted into the dispersed form by means of the presence of the dispersing agent at a temperatureType: ApplicationFiled: November 16, 2009Publication date: August 16, 2012Applicant: Evonik Roehm GmbHInventors: Erna Roth, Ruediger Alexowsky, Hans-Ulrich Petereit, Kathrin Nollenberger, Christian Meier
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Publication number: 20120203147Abstract: A method for increasing blood flow to vital organs during cardiopulmonary resuscitation of a person experiencing a cardiac arrest may include performing standard or active compression decompression cardiopulmonary resuscitation on a person to create artificial circulation by repetitively compressing the person's chest such that the person's chest is subject to a compression phase and a relaxation or decompression phase. The method may also include administering one or more vasodilator drugs to the person to improve the artificial circulation created by the cardiopulmonary resuscitation. The method may also include binding at least a portion of the person's abdomen, either manually or with an abdominal compression device. Performing cardiopulmonary resuscitation on a person may include ventilating the person with either an impedance threshold device or a intrathoracic pressure regulator.Type: ApplicationFiled: July 1, 2011Publication date: August 9, 2012Applicant: ResQSystems, Inc.Inventors: Keith Lurie, Demetris Yannopoulos