C=x Bonded Directly Or Indirectly By An Acyclic Carbon Or Carbon Chain To Ring Carbon Of The Five-membered Hetero Ring (e.g., Tryptophan, Etc.) (x Is Chalcogen) Patents (Class 514/419)
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Patent number: 7713996Abstract: The invention is concerned with novel heterobicyclic derivatives of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, A, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.Type: GrantFiled: September 12, 2006Date of Patent: May 11, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Jean Ackermann, Konrad Bleicher, Simona M Ceccarelli Grenz, Odile Chomienne, Patrizio Mattei, Tanja Schulz-Gasch
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Patent number: 7714017Abstract: Peri-substituted, fused bicyclic ring carboxylic acids useful for the treatment or prophylaxis of a prostaglandin-mediated disease or condition are disclosed.Type: GrantFiled: October 11, 2005Date of Patent: May 11, 2010Assignee: Decode Genetics, EHFInventors: Jasbir Singh, Mark Gurney, Georgeta Hategan, Peng Yu, David Zembower, Nian Zhou, Alexandre Mikhaylovich Polozov, Wayne Edward Zeller
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Patent number: 7709521Abstract: The present invention relates to substituted indoles of formula (I) useful as pharmaceutical compounds for treating respiratory disorders.Type: GrantFiled: August 16, 2004Date of Patent: May 4, 2010Assignee: AstraZeneca ABInventors: Roger Victor Bonnert, Anthony Ronald Cook, Timothy Jon Luker, Rukhsana Tasneem Mohammed, Stephen Thom
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Publication number: 20100104624Abstract: Described here are compositions and methods for treating side-effects of vasodilator therapy. The compositions may include both a vasodilator and a side-effect alleviating agent in a single dosage form. Alternatively, the vasodilator and side-effect alleviating agent may be formulated separately, each in its own dosage form. The compositions may be packaged as kits for use with various medical conditions.Type: ApplicationFiled: June 11, 2009Publication date: April 29, 2010Inventors: Peter LANGECKER, Bryan T. Oronsky
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Patent number: 7705023Abstract: There is provided a compound of formula: (I), wherein X, R1, R2, R3, R4, R5 and R6 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of microsomal prostaglandin E synthase-1 is desired and/or required, and particularly in the treatment of inflammation.Type: GrantFiled: June 17, 2005Date of Patent: April 27, 2010Assignee: Biolipox ABInventors: Kristofer Olofsson, Benjamin Pelcman, Ivars Kalvins, Edgars Suna, Vita Ozola, Martins Katkevics
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Publication number: 20100099732Abstract: This invention relates to pharmaceutical compositions comprising phenylcarbamoyl-methyl-indole derivatives that are found to be potent modulators of potassium channels and, as such, are valuable candidates for the treatment of diseases or disorders as diverse as those which are responsive to the modulation of potassium channels.Type: ApplicationFiled: March 14, 2008Publication date: April 22, 2010Applicant: NeuroSearch A/SInventors: Antonio Nardi, Morten Grunnet, Palle Christophersen, David Spencer Jones, Elsebet Østergaard Nielsen, Dorte Strøbaek, Lars Siim Madsen
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Patent number: 7700642Abstract: The present invention provides a process for producing an aromatic unsaturated compound of the formula (4) wherein Ar represents an optionally substituted aromatic group or an optionally substituted heteroaromatic group, and Y represents an electron withdrawing group, which comprises reacting (a) a compound of the formula (1) Ar—H??(1) wherein Ar has the same meaning as defined above with (b) a compound of the formula (2) wherein Y has the same meaning as defined above, and Z represents a lower alkoxy, or a compound of the formula (3) wherein Y and Z have the same meanings as defined above, in the presence of (c) an acid or a compound which generates a mineral acid by its hydrolysis.Type: GrantFiled: August 25, 2004Date of Patent: April 20, 2010Assignee: Sumitomo Chemical Company, LimitedInventors: Weiqi Wang, Tetsuya Ikemoto
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Publication number: 20100092566Abstract: Highly concentrated drug particle formulations are described, wherein the drug comprises between about 25 wt % and 80 wt % of the particle formulation. The particle formulations of the present invention comprise, for example, macromolecules, such as proteins and/or small molecules (such as steroid hormones). The particle formulation typically further includes one or more additional component, for example, one or more stabilizer (e.g., carbohydrates, antioxidants, amino acids, and buffers). Such concentrated particle formulations can be combined with a suspension vehicle to form suspension formulations. The suspension formulation comprises (i) a non-aqueous, single-phase vehicle, comprising one or more polymer and one or more one solvent, wherein the vehicle exhibits viscous fluid characteristics, and (ii) a highly concentrated drug particle formulation. Devices for delivering the suspension formulations and methods of use are also described.Type: ApplicationFiled: October 14, 2009Publication date: April 15, 2010Inventors: Thomas R. Alessi, Ryan D. Mercer, Catherine M. Rohloff, Bing Yang
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Publication number: 20100092474Abstract: The invention provides combinations comprising (or consisting essentially of) one or more ancillary compound(s) and a compound of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxygType: ApplicationFiled: October 12, 2007Publication date: April 15, 2010Inventors: Neil James Gallagher, John Francis Lyons, Neil Thomas Thompson, Stephen Murray Yule, Christopher William Murray
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Patent number: 7696240Abstract: The invention is concerned with novel fused pyrrole derivatives of formula (I) wherein A, Ar, R1, R2, R2? and R2? and n are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit chymase and can be used as medicaments.Type: GrantFiled: December 5, 2006Date of Patent: April 13, 2010Assignee: Hoffmann-La Roche Inc.Inventors: David Banner, Hans Hilpert, Bernd Kuhn, Harald Mauser
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Publication number: 20100075963Abstract: 1-Benzenesulfonyl-1H-indoles, processes for their production and their use as pharmaceuticals, e.g. in the treatment of disorders which are mediated by CCR9, such as e.g. inflammatory bowel disease.Type: ApplicationFiled: February 4, 2008Publication date: March 25, 2010Applicant: NOVARTIS AGInventors: Philipp Lehr, Anthony Winiski
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Publication number: 20100074951Abstract: Disclosed herein is a lag time delayed-release combination pharmaceutical composition comprising of an angiotensin-II-receptor blocker and an HMG-CoA reductase inhibitor, as well as a preparation method thereof. The composition is designed based on chronotherapy in which active ingredients are administered to have different onset times, such that the release of each active ingredient of the composition in body can be lag time delayed to a specific rate. Also, the composition is very effective for the treatment of hypertension and the prevention of complications in patients having metabolic syndromes which show diabetes, obesity, hyperlipidemia, coronary artery diseases and the like. More specifically, the composition is a drug delivery system designed such that the release of each drug is controlled to a specific rate, and it can show the most ideal effect, when it is absorbed in body.Type: ApplicationFiled: October 30, 2007Publication date: March 25, 2010Applicant: HANALL PHARMACEUTICAL COMPANY, LTD.Inventors: Sung Wuk Kim, Sung Soo Jun, Young Gwan Jo, Ja Seong Koo, Jae Woon Son
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Publication number: 20100076052Abstract: Pharmaceutical formulations comprising perindopril or its salts, isomers, enantiomers, polymorphs, metabolites, solvates, hydrates, and mixtures thereof, and at least one surface stabilizer. Also disclosed are methods of stabilizing perindopril in the formulations, and polyoxyethylene-polyoxypropylene block copolymers as surface stabilizers.Type: ApplicationFiled: September 23, 2009Publication date: March 25, 2010Inventors: Janardhanan Anand Subramony, Jyotsna Rath, Prangya Paramita Pati
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Publication number: 20100075923Abstract: The present invention is directed to a method of enhancing TGF-? signaling in a subject comprising administering to said subject a clathrin-dependent endocytosis inhibitor in an amount sufficient to enhance TGF-? signaling. In another aspect, the invention is directed to a method of treating a condition associated with decreased TGF-? signaling in a patient in need thereof comprising administering to said patient a clathrin-dependent endocytosis inhibitor in a therapeutically effective amount.Type: ApplicationFiled: September 15, 2009Publication date: March 25, 2010Inventors: Jung San Huang, Shuan Shian Huang
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Publication number: 20100076044Abstract: Disclosed is an agent for use in the treatment or prevention of inflammatory bowel disease. Also disclosed is an agent for inhibiting the production of TNF-?. A therapeutic or prophylactic agent for inflammatory bowel disease comprising at least one amino acid selected from the group consisting of lysine, histidine, phenylalanine, methionine, tryptophan, glutamine, glycine, cysteine, cystine and threonine, the amino acid being administered at a dose of 0.1 to 4000 mg/kg per day; and a TNF-? production inhibitor comprising an amino acid selected from the group consisting of histidine, phenylalanine and tryptophan, the amino acid being administered at a dose of 0.1 to 4000 mg/kg per day.Type: ApplicationFiled: June 25, 2009Publication date: March 25, 2010Applicant: Ajinomoto Co., Inc.Inventors: Hideki MATSUMOTO, Tomohisa Okutsu, Tomoko Takeda, Hideki Suzuki, Tetsuo Yano, Masaki Hashimoto, Miho Ono, Manabu Suzuki
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Patent number: 7683092Abstract: Novel crystalline forms of two indole compounds connected to phenoxyalkylcarboxylic acid groups are selective PPAR gamma partial agonists that are useful in the treatment of type 2 diabetes, hyperglycemia, obesity, dyslipidemia, and the metabolic syndrome. The novel crystal forms include a crystalline free acid dihydrate and crystalline free acid anhydrate of one compound and several crystalline forms of the free acid and the sodium salt of the second compound. The invention also relates to pharmaceutical compositions comprising these novel crystal forms, processes to prepare the crystal forms and their pharmaceutical compositions, and uses of the crystal forms in the treatment of type 2 diabetes and other PPAR gamma modulated diseases.Type: GrantFiled: March 10, 2006Date of Patent: March 23, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Dalian Zhao, Jean-Francois Marcoux, David Boardman, Aquiles E. Leyes
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Publication number: 20100069454Abstract: The present invention provides compounds, pharmaceutical compositions and methods for treating, immuno-allergical diseases, autoimmune diseases, and organ or tissue rejection following transplantation.Type: ApplicationFiled: August 21, 2009Publication date: March 18, 2010Applicant: Novaremed LimitedInventor: Eliahu Kaplan
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Publication number: 20100063068Abstract: The disclosure provides compounds of formula I, II, III, IV, and V, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.Type: ApplicationFiled: August 28, 2009Publication date: March 11, 2010Inventors: Richard Pracitto, John F. Kadow, John A. Bender, Brett R. Beno, Katharine A. Grant-Young, Ying Han, Piyasena Hewawasam, Andrew Nickel, Kyle E. Parcella, Kap-Sun Yeung, Louis S. Chupak
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Patent number: 7674818Abstract: Compounds of formula I are provided: wherein: R1, R2, and R3, are as defined herein, as well as pharmaceutical composition and methods using the compounds as inhibitors of plasminogen activator inhibitor (PAI-1) and as therapeutic composition for treating conditions resulting from fibrinolytic disorders, such as deep vein thrombosis, coronary heart disease and pulmonary fibrosis.Type: GrantFiled: July 11, 2007Date of Patent: March 9, 2010Assignee: Wyeth LLCInventors: Lee Dalton Jennings, Hassan Mahmoud Elokdah, Geraldine Ruth McFarlane
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Patent number: 7674815Abstract: Compounds of formula I processes for their preparation, their use as pharmaceuticals and to pharmaceutical compositions comprising them.Type: GrantFiled: January 29, 2007Date of Patent: March 9, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Christoph Faeh, Holger Kuehne, Thomas Luebbers, Patrizio Mattei, Cyrille Maugeais, Philippe Pflieger
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Publication number: 20100055073Abstract: An orally administrable nutritional formulation for use in the treatment of Pervasive Developmental Disorders (e.g. Autism, Asperger disorder or Retts disorder) contains free amino acids as the sole source of protein.Type: ApplicationFiled: June 12, 2009Publication date: March 4, 2010Inventors: Andrew Sean Lynch, Kerry Louisa Hambleton, Stephen Leyland Smith
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Publication number: 20100055173Abstract: The present invention provides a controlled absorption formulation in which modified release of the active ingredient preferentially occurs in the lower gastrointestinal tract, including the colon. The formulation supports a significantly higher bioavailability of the active ingredient in the body of the subject than that can be achieved from the currently used conventional formulation, such that therapeutically significant plasma levels of statin are maintained for an extended period after administration. The formulation preferably features a core, a subcoat surrounding the core comprising at least one water soluble hydrophilic carrier and an outer coating. The core is optionally and preferably in the form of a tablet.Type: ApplicationFiled: October 9, 2007Publication date: March 4, 2010Inventors: Adel Penhasi, Maxim Gomberg
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Publication number: 20100056520Abstract: The present invention is directed to formulations of inhibitors of phospholipase enzymes, such as cytosolic PLA2, compositions containing the same and processes for manufacture thereof.Type: ApplicationFiled: October 30, 2007Publication date: March 4, 2010Inventors: Frances Anne Donahue, Marc Sadler Tesconi, Mannching Sherry Ku
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Publication number: 20100048589Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, L, Q, R1, R2, and R3 are defined herein.Type: ApplicationFiled: August 11, 2009Publication date: February 25, 2010Inventors: Raymond W. Colburn, Scott L. Dax, Christopher M. Flores, Donald W. Ludovici, Jay M. Matthews, Mingde Xia, Xiaoqing Xu, Mark A. Youngman, Bin Zhu
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Patent number: 7662848Abstract: The present invention is directed to a process for preparing Fluvastatin Sodium salt by basic hydrolysis of its alkyl ester. The reaction is performed in conditions suitable to allow a selective hydrolysis of the desired syn isomer, while the unwanted anti isomer is removed by extraction, thus reducing its content in the final product; this diastereomer is the main impurity of Fluvastatin sodium salt and its ester precursor.Type: GrantFiled: April 19, 2007Date of Patent: February 16, 2010Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.Inventor: Marco Fachini
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Patent number: 7659304Abstract: A compound represented by the following formula (I) or a salt thereof is provided: wherein X represents a halogen atom; R1 represents a hydrogen atom, substituted or unsubstituted C1-6 alkyl group, substituted or unsubstituted C2-6 alkenyl group, substituted or unsubstituted C2-6 alkynyl group, substituted or unsubstituted aromatic group, substituted or unsubstituted aralkyl group, substituted or unsubstituted acyl group, substituted or unsubstituted arylsulfonyl group, substituted or unsubstituted C1-6 alkylsulfonyl group, substituted or unsubstituted C2-7 alkoxycarbonyl group, or hydroxyl group; R2 represents a substituted or unsubstituted C1-21 alkyl group; R3, R5, and R6 are the same or different and represent a hydrogen atom or halogen atom; R4 represents a hydrogen atom or substituted or unsubstituted C1-6 alkyl group; and R7 represents a hydrogen atom or substituted or unsubstituted C1-21 hydrocarbon group.Type: GrantFiled: January 17, 2008Date of Patent: February 9, 2010Inventors: Masanori Somei, Atsuhiko Hattori, Nobuo Suzuki
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Publication number: 20100029742Abstract: The present invention relates to crystalline forms of the mono-sodium salt of D-isoglutamyl-D-tryptophan, pharmaceutical compositions comprising them, their use in the treatment of various diseases and conditions, and processes for their preparation. In particular, the present invention relates the crystal modification 1 (polymorphic form F), the crystal modification 2 (polymorphic form I), and the crystal modification 3 (polymorphic form X) of the mono-sodium salt of D-isoglutamyl-D-tryptophan.Type: ApplicationFiled: February 11, 2008Publication date: February 4, 2010Applicant: Apotex Technologies Inc.Inventors: Tim Fat Tam, Blaise N'Zemba, Regis Leung-Tuong, Yingsheng Wang, Yanqing Zhao, Lily Yu
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Publication number: 20100029598Abstract: The present invention relates to extended benzamide derivatives of the general formula I, to processes for preparation thereof and to use thereof for production of pharmaceutical compositions for treatment of disorders and indications associated with the EP2 receptor.Type: ApplicationFiled: July 24, 2009Publication date: February 4, 2010Applicant: Bayer Schering Pharma AGInventors: Marcus Kopitz, Bernhard Lindenthal, Antonius Ter Laak, Tim Wintermantel, Olaf Peters, Gernot Langer, Nico Braeuer, Bernd Buchmann
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Publication number: 20100016295Abstract: This invention relates to certain biphenyl amino acid compounds, compositions, and methods for treating or preventing obesity and related diseases.Type: ApplicationFiled: July 31, 2006Publication date: January 21, 2010Applicant: Bayer Healthcare LLCInventors: Roger A. Smith, Derek Lowe, Tatiana Shelekhin, Georgiy Bondar, Philip Coish, Stephen J. O'Connor
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Publication number: 20100008976Abstract: The invention relates to compounds having the general structural formula (formula I) for use in a diagnostic method or a method for treatment of the human or animal body by surgery or therapy.Type: ApplicationFiled: July 16, 2007Publication date: January 14, 2010Applicant: Westfallsche Wilheims Universitat MunsterInventors: Andreas Hensel, Thomas Hofmann, Alexandra Deters, Timo Stark
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Publication number: 20100010026Abstract: Methods of utilizing a combined administration or a unit dosage of a combination of an HMG-CoA inhibitor and omega-3 fatty acids for the reduction of apolipoprotein-B levels. The methods are especially useful in the treatment of patients with hypertriglyceridemia or hypercholesterolemia or mixed dyslipidemia, coronary heart disease (CHD), vascular disease, atherosclerotic disease and related conditions, and for the prevention or reduction of cardiovascular, cardiac, and vascular events.Type: ApplicationFiled: September 17, 2009Publication date: January 14, 2010Inventors: Roelof M.L. RONGEN, Robert A. SHALWITZ, Douglas KLING, Ralph T. DOYLE, JR.
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Publication number: 20100009970Abstract: The present invention features compositions, methods, and kits useful in the treatment of viral diseases. In certain embodiments, the viral disease is caused by a single stranded RNA virus, a flaviviridae virus, or a hepatic virus. In particular embodiments, the viral disease is viral hepatitis (e.g., hepatitis A, hepatitis B, hepatitis C, hepatitis D, hepatitis E) and the agent or combination of agents includes sertraline, a sertraline analog, UK-416244, or a UK-416244 analog. Also featured are screening methods for identification of novel compounds that may be used to treat a viral disease.Type: ApplicationFiled: March 18, 2009Publication date: January 14, 2010Applicant: Combinatorx (Singapore) Pte. Ltd.Inventors: Lisa M. Johansen, Christopher M. Owens, Christina Mawhinney, Todd W. Chappell, Alexander T. Brown, Michael G. Frank, Michael A. Foley, Ralf Altmeyer, Yu Chen
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Patent number: 7645752Abstract: The present invention is directed to compounds of Formula I: which are modulators of the 5-hydroxtryptamine-6 and 5-hydroxytryptamine-2A receptors and which are inhibitors of norepinephrine reuptake. The compounds of the invention, and pharmaceutical composition thereof, are useful in the treatment of disorders related to or associated with the 5-hydroxytryptamine-6 and 5-hydroxtryptamine-2A receptors or with norepinephrine reuptake inhibition.Type: GrantFiled: January 12, 2007Date of Patent: January 12, 2010Assignee: Wyeth LLCInventors: Robert E. McDevitt, Yanfang Li, Albert J. Robichaud, Gavin D. Heffernan, Richard D. Coghlan, Ronald C. Bernotas
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Publication number: 20100004309Abstract: The present invention relates to dietary compositions comprising reduced level of methionine, tryptophan, all amino acids, or protein, dietary compositions comprising glycerol as a substitute for monosaccharides, disaccharides, and polysaccharides, and hypocaloric or calorie free diets with reduced level of energy, carbohydrates, or protein. Also disclosed are methods of using these compositions and diets, as well as fasting, to protect subjects against chemotherapy, radiotherapy, oxidative stress, or aging.Type: ApplicationFiled: April 24, 2009Publication date: January 7, 2010Applicant: University of Southern CaliforniaInventor: Valter Longo
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Publication number: 20090324741Abstract: An injectable polymer-lipid blend is provided. The blend may provide a localized drug delivery system for a pharmaceutically active agent. The blend may be prepared from a chitosan-based material, fatty acid and phospholipid. The chitosan-based material may be a water soluble chitosan derivative. The fatty acid may be a fatty acid or a fatty aldehyde, such as laurinaldehyde, having an acyl chain length of C8-C16. The rheological properties of the blend relates to the ratio of the components and to the acyl chain length of the fatty acid. The injectable system is well suited for the delayed release of pharmaceutically active agents in the treatment of cancer and other diseases requiring localized drug delivery.Type: ApplicationFiled: August 28, 2008Publication date: December 31, 2009Inventors: Christine ALLEN, Justin GRANT, Jaepyoung CHO, Patrick LIM SOO, Micheline PIQUETTE-MILLER
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Publication number: 20090326037Abstract: The invention relates to medicine, in particular to searching and developing novel medicinal agents for treating and preventing viral infections, mainly influenza viruses. The aim of said invention is to develop more efficient and low toxic medicinal agents by combining arbidol and the analogs thereof with a preparation exhibiting another mechanism of action. Said combinations enhances the efficiency of the preparation small doses and makes it possible to reduce the probability of side effects and appearance of virus resistant strain by reducing the dose. The result is attained by the combined use of arbidol and the analogies thereof with at least one type of preparation selected from the following group of antiviral preparations: ribavirin, zanamivirin, oseltavirin, peramirin, amantadin or remantadin.Type: ApplicationFiled: December 28, 2005Publication date: December 31, 2009Inventor: Irina Anatolievna Leneva
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Publication number: 20090318492Abstract: Indole and indole-related compounds, compositions and methods are disclosed. The compounds of the invention are useful as phospholipase inhibitors. The compounds and compositions of the invention are useful for treatment of phospholipase-related conditions, such as insulin-related, weight-related and/or cholesterol-related conditions in an animal subject.Type: ApplicationFiled: November 3, 2006Publication date: December 24, 2009Inventors: Han-Ting Chang, Dominique Charmot, Tomasz Glinka, Michael James Cope, Elizabeth Goka, Jun Shao, Shiah-yun Chen, Jerry M. Buysse
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Publication number: 20090317377Abstract: The present invention relates to methods for the treatment or prevention of trigeminal nerve-associated pain, in particular chronic, acute and procedural-related pain. The methods comprise administration of analgesic agents to the trigeminal nerve system which results in analgesia to the facial or head region.Type: ApplicationFiled: August 28, 2006Publication date: December 24, 2009Inventors: David C. Yeomans, William H. Frey, Daniel I. Jacobs
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Publication number: 20090318528Abstract: New (2R,4R) monatin monosodium salt hydrate crystals characterized by having specific characteristic X-ray diffraction peaks provide general-purpose, stable, and safe monatin sodium salt crystals incorporating no organic solvent. These crystal may be prepared by a method that requires no organic solvent in the crystallization, separation, and drying steps. These crystal are useful as sweeteners and for the preparation of orally consumed products, such as foods, beverages, pharmaceutical products, topical pharmaceutical products, and feeds containing general-purpose, stable, and safe monatin sodium salt crystals.Type: ApplicationFiled: March 11, 2009Publication date: December 24, 2009Applicant: AJINOMOTO CO., INCInventors: Kenichi MORI, Eriko ONO
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Publication number: 20090312391Abstract: The present invention relates to methods for preventing the development of cancer or neurodegenerative diseases by administering N-Acetylcysteine (NAC), melatonin, or a combination thereof. The present invention also relates to methods for diagnosing cancer and/or neurdegenerative disease by detecting or determining the amount of dopamine metabolites, 4-CE, 2-CE, methylation of CE or CE-Q conjugates.Type: ApplicationFiled: July 31, 2009Publication date: December 17, 2009Applicant: Prevention, L.L.C.Inventors: Ercole L. Cavalieri, Eleanor Rogan
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Publication number: 20090312366Abstract: The present application is directed to novel P2X7R antagonists that are indol-3-carboxamide or azaindole-3-carboxamide compounds, pharmaceutical compositions comprising the same and their use for the prophylactic or therapeutic treatment of diseases mediated by P2X7R activity.Type: ApplicationFiled: March 25, 2009Publication date: December 17, 2009Applicant: AFFECTIS PHARMACEUTICALS AGInventor: Michael Bös
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Publication number: 20090305995Abstract: The invention relates to substituted F3-Phe-trp-F 3-Lys-beta-tri-peptides and derivatives thereof, a process for their preparation, pharmaceutical preparations which contain these compounds which are agonists/antagonists of somatostatin receptors, as active agents for the treatment of disorders which can be influenced by a modulation of somatostatin receptor activity, in particular somatostatin receptor sst4 activity, by the compounds of the invention.Type: ApplicationFiled: November 14, 2005Publication date: December 10, 2009Applicant: Novartis AGInventors: Karl Heinz Krawinkler, Peter Meier, Bernard Faller
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Publication number: 20090306171Abstract: Indole and indole-related compounds according to the formula (I) or (II) optionally having additional heteroatoms, compositions and methods are disclosed. The compounds of the invention are useful as phospholipase inhibitors. The compounds and compositions of the invention are useful for treatment of phospholipase-related conditions, such as insulin-related, weight-related and/or cholesterol-related conditions in an animal subject. Formula (I), formula (II). R4 being a moiety represented by formula (C4-II-C), R3 being a moiety represented by formula (C3-I or C3-II).Type: ApplicationFiled: November 3, 2006Publication date: December 10, 2009Inventors: Han-Ting Chang, Dominique Charmot, Tomasz Glinka, Michael James Cope, Elizabeth Goka, Jun Shao, Shiah-yun Chen, Jerry M. Buysse
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Patent number: 7625944Abstract: The present invention provides compounds that inhibit the activity of plasma kallikrein (PK) and methods of preventing and treating the formation of thrombin during or after a PK dependent disease or condition, for example, after fibrinolysis treatment.Type: GrantFiled: July 30, 2007Date of Patent: December 1, 2009Assignee: Activesite Pharmaceuticals, Inc.Inventors: Sukanto Sinha, Tamie Jo Chilcote
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Publication number: 20090291978Abstract: Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers, wherein R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxyesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; Y is a bond, C(?O)—, —S(?O)2—, —C(—O)O—, —C(O)NR3—, —C(?S)—NR3, —C(?NH)NR3 or —S(?O)2NR3— wherein R3 is hydrogen or optionally substituted C1-C6 alkyl; L is a divalent radical of formula -(Alk1)m(O)n(Alk2)p— wherein m, n and p are independently 0 or 1, Q is (i) an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5-13 ring members, or (ii), in the case where both m and p are 0, a divalent radical of formula —X2-Q1- or -Q1-X2— wherein X2 is —O—, S— or NRA— wherein RA is hydrogen or optionally substituted C1-C3 alkyl, and Q1 is an optionally substituted divalent mono- or bicyclic carbocyclic or hetero-cyclic rType: ApplicationFiled: May 4, 2006Publication date: November 26, 2009Applicant: CHROMA THERAPEUTICS LTD.Inventors: Alan Hornsby Davidson, Sanjay Ratilal Patel, Francesca Ann Mazzei, Stephen John Davies, Alan Hastings Drummond, David Festus Moffat, Kenneth William John Baker, Alistair David Graham Donald
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Patent number: 7618650Abstract: The invention concerns the combination of a short-acting hypnotic agent and a compound of formula (I): Wherein X, Y, Z, A, B, D, Ar, R1 and R2 are as defined herein. The combination of this invention is useful in treating a variety of sleep disorders.Type: GrantFiled: February 6, 2008Date of Patent: November 17, 2009Assignee: Aventis Pharmaceuticals IncInventors: Gary Emmons, Sathapana Kongsamut, Craig N. Karson, Corrine M. Legoff
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Publication number: 20090281160Abstract: This invention relates to a process for the synthesis of ketomethylene derivatives of the tripeptide Phe-Gly-Pro (“keto-ACE”, compound 5a) and analogues thereof. The synthesis process proceeds via an ?,?-unsaturated keto intermediate. A key feature of the process involves a Horner-Emmons olefination of the, -unsaturated keto-phosphonate with ethyl glyoxylate. Keto-ACE analogues produced by the process of the invention display C-domain selectivity.Type: ApplicationFiled: May 29, 2006Publication date: November 12, 2009Inventors: Edward Sturrock, Aloysius Nchinda, Kelly Chibale
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Patent number: 7615572Abstract: Methods for increasing D-Serine concentration and reducing concentration of the toxic products of D-Serine oxidation, for enhancing learning, memory and/or cognition, or for treating schizophrenia, Alzheimer's disease, ataxia or neuropathic pain, or preventing loss in neuronal function characteristic of neurodegenerative diseases involve administering to a subject in need of treatment a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt or solvate thereof: wherein R1 and R2 are independently selected from hydrogen, halo, nitro, alkyl, acyl, alkylaryl, and XYR5; or R1 and R2, taken together, form a 5, 6, 7 or 8-membered substituted or unsubstituted carbocyclic or heterocyclic group; X and Y are independently selected from O, S, NH, and (CR6R7)n; R3 is hydrogen, alkyl or M+; M is aluminum, calcium, lithium, magnesium, potassium, sodium, zinc ion or a mixture thereof; Z is N or CR4; R4 is from selected from hydrogen, halo, nitro, alkyl, alkylaryl, and XYR5;Type: GrantFiled: December 15, 2008Date of Patent: November 10, 2009Assignee: Sepracor Inc.Inventors: Q. Kevin Fang, Seth Hopkins, Michele Heffernan, Milan Chytil
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Publication number: 20090275551Abstract: The present disclosure relates to method of using fluvastatin, alone or in combination with ezetimibe, be used to (1) lower cholesterol level, (2) treat hypercholesterolemia, (3) treat mixed dyslipidemia and/or (4) inhibit cholesterol biosynthesis in patients who experienced muscle-related side effects (MRSE). The present disclosure also relates to a pharmaceutical composition comprising ezetimibe and fluvastatin.Type: ApplicationFiled: October 22, 2008Publication date: November 5, 2009Inventors: Evan A. Stein, Claudio Ruben Gimpelewicz
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Publication number: 20090275572Abstract: Compounds of the formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment of bacterial infections.Type: ApplicationFiled: March 12, 2009Publication date: November 5, 2009Inventors: William H. Miller, Kenneth A. Newlander, Mark A. Seefeld, Irene N. Uzinskas, Walter E. Dewolf, JR., Dalia R. Jakas