Chalcogen Or Nitrogen Bonded Directly To The Hetero Ring Patents (Class 514/470)
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Publication number: 20100144864Abstract: Disclosed herein are novel compositions and methods for treating or preventing a variety of disorders and conditions associated with lipid metabolism. The methods generally include administering to a patient in need thereof a therapeutically effective amount of a pharmaceutical composition comprising one or more sGC modulators alone or in combination with one or more lipid altering agents and/or PDE inhibitors.Type: ApplicationFiled: April 3, 2008Publication date: June 10, 2010Applicant: IRONWOOD PHARMACEUTICALS, INC.Inventors: Mark G. Currie, Daniel P. Zimmer
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Publication number: 20100137284Abstract: The combination of nitric oxide generating compounds which are not dependent upon aldehyde dehydrogenase for bioactivation, or are specifically targeted to nNOS or the sarcoplasmic reticulum of cardiac muscle cells, and xanthine oxidase inhibitors are effective in the treatment of heart disease, specifically congestive heart failure and ischemic coronary disease. This treatment is particularly effective in patients who have particularly heavy oxidative burdens, e.g. diabetics, patients with lung disorders, patients with sickle cell anemia and patients of Asian descent.Type: ApplicationFiled: June 25, 2009Publication date: June 3, 2010Inventors: Jonathan S. Stamler, Gregory T. Went
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Publication number: 20100137373Abstract: A composition comprising at least a strigolactone derivative (a) of general formula: and an insecticide compound (b) in a (a)/(b) weight ratio of from 1/1 to 1/1013; A composition further comprising an additional fungicidal compound; A method for preventively or curatively combating the pests and diseases of crops and increasing their yield by using this composition.Type: ApplicationFiled: June 12, 2008Publication date: June 3, 2010Inventors: Heike Hungenberg, Wolfgang Thielert, Jean-Pierre Vors
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Publication number: 20100130498Abstract: The present invention relates to agonists of the human bitter-taste receptors hTAS2R14, hTAS2R10 and hTAS2R4 and their role in bitter taste transduction. The invention also relates to methods for identifying molecules that modulate, e.g. suppress, or enhance hTAS2R14, hTAS2R10 and hTAS2R4 bitter taste transduction or bitter taste response.Type: ApplicationFiled: March 31, 2008Publication date: May 27, 2010Applicant: Deutshes Institut Fur Ernahrungsforschung Potsdam- RehbruckeInventors: Maik Behrens, Anne Brockhoff, Christina Kuhn, Wolfgang Meyerhof, Giovanni Appendino
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Patent number: 7723381Abstract: Compounds of formula 1 and hetero derivatives thereof and the pharmacologically acceptable salts, enantiomers, racemates, hydrates, or solvates thereof, which are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin, or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.Type: GrantFiled: April 21, 2006Date of Patent: May 25, 2010Assignee: Boehringer Ingelheim International GmbHInventors: Ralf Anderskewitz, Horst Dollinger, Rolf Goeggel, Birgit Jung, Joerg Kley, Juergen Mack, Peter Nickolaus, Rainer Walter
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Publication number: 20100125073Abstract: The present invention relates to benzofuran and benzothiophene derivatives and compositions containing such compounds for the production of medicaments for the treatment of cancers of the central nervous system as monotherapy or combination with other agents.Type: ApplicationFiled: August 28, 2007Publication date: May 20, 2010Inventors: Olaf Weber, Verena Voehringer, Hans-Georg Lerchen, Frank-Thorsten Hafner, Joerg Keldenich, Karl-Heinz Schlemmer, Ursula Krenz, Bernd Riedl
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Publication number: 20100119519Abstract: An ocular device comprising a delivery body configured for implanting within the capsular bag of a patient's eye, the delivery body containing an ocular therapeutic agent, the delivery body having a permeable exterior surface for delivering the therapeutic agent when implanted in the patient's eye.Type: ApplicationFiled: November 3, 2009Publication date: May 13, 2010Inventor: Gholam A. Peyman
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Publication number: 20100113589Abstract: This invention relates to novel compounds that are hydroxyethylamino sulfonamide derivatives and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel hydroxyethylamino sulfonamide derivatives that are derivatives of darunavir. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering a human immunodeficiency virus (HIV) protease inhibitor, such as darunavir.Type: ApplicationFiled: April 28, 2009Publication date: May 6, 2010Applicant: CoNCERT Pharmaccuticals, Inc.Inventor: Scott L. Harbeson
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Patent number: 7700647Abstract: It is an object of the present invention to provide fluorinated bis(phthalic anhydride) which has less coloration and higher solubility in comparison with conventional compounds, and a method for producing the same. Further, it is also an object of the present invention to provide a method for producing a fluorinated bis(phthalonitrile) compound, which is an intermediate raw material compound of the method for producing the fluorinated bis(phthalic anhydride), and a polyamic acid and a polyimide, which are produced from the fluorinated bis(phthalic anhydride). A fluorinated bis(phthalic anhydride) of the present invention is the fluorinated bis(phthalic anhydride) represented by the following formula (I1), wherein its specific surface area is 3.0 m2/g or larger. It is also characterized in that its molar absorption coefficient is 0.6 L/mol·cm or less at a wavelength of 360 nm. [wherein, m and n independently represent integers of 1 to 3, and Z1 represents a single bond group or a bivalent organic group.Type: GrantFiled: January 7, 2008Date of Patent: April 20, 2010Assignee: Nippon Shokubai Co., Ltd.Inventors: Go Masuda, Yasunori Okumura, Shinji Nishimae
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Publication number: 20100093768Abstract: The present invention provides methods for discovering agents that are effective in reversing epigenetic silencing by inhibiting the interaction of methyl-binding (MBD) proteins with methylated genomic DNA. Also provided are methods for reactivating silenced genes having CpG island hypermethylation along with methods for treatment and prevention of diseases, such as cancer and sickle cell anemia, by administering an agent that modulates methyl-binding domain (MBD) protein-mediated transcriptional repression, thereby increasing gene transcription to prevent or treat disease. Additionally, compounds identified by the present invention useful for treatment and prevention of diseases, such as cancer and sickle cell anemia, are provided.Type: ApplicationFiled: December 21, 2007Publication date: April 15, 2010Inventors: William G. Nelson, Srinivasan Yegnasubramanian, Xiaohui Lin, Traci J. Speed, Zachery Reichert
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Publication number: 20100069392Abstract: The invention relates to the combined use of a PDE4 inhibitor with a HMG-CoA reductase inhibitor for the preventive and curative treatment of an inflammatory pulmonary disease.Type: ApplicationFiled: July 3, 2007Publication date: March 18, 2010Applicant: Nycomed GmbHInventor: Stefan-Lutz Wollin
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Publication number: 20100068301Abstract: Disclosed herein are compositions and compounds that combine an inhibitor of 5-lipoxygenase activating protein (FLAP) and a modulator of NO levels in a mammal. The NO modulator can be an agent that induces the production of NO in a mammal, or can be an agent that itself produces NO in the mammal. Further disclosed herein are strategies for synthesizing such compounds, and methods for testing whether the combination compounds and compositions provide a desired benefit. Also disclosed herein are pharmaceutical compositions and formulations that combine a FLAP inhibitor and an NO modulator. Further described herein are methods for using such compositions and compounds for the treatment of diseases, conditions, and disorders in a mammal, including a human. Such treatment methods include the separate administration of a FLAP inhibitor and a NO modulator to the mammal, and the simultaneous administration of a FLAP inhibitor and a NO modulator to the mammal.Type: ApplicationFiled: November 30, 2007Publication date: March 18, 2010Inventors: John H. Hutchinson, Mustapha Haddach, Mark Moran, Jillian Evans, Nicholas Simon Stock, Jeffrey Roger Roppe
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Publication number: 20100056621Abstract: The present invention relates to agonists of the hTAS2R14 bitter taste receptor and its role in bitter taste transduction. The invention also relates to assays for screening molecules that modulate, e.g. suppress or block hTAS2R14 bitter taste transduction or bitter taste response.Type: ApplicationFiled: April 20, 2005Publication date: March 4, 2010Applicant: Deutsches Institut fur ErnahrungsforschungInventors: Maik Behrens, Anne Brockhoff, Bernd Bufe, Christina Kuhn, Wolfgang Meyerhof, Marcel Winnig
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Patent number: 7655688Abstract: Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.Type: GrantFiled: December 19, 2005Date of Patent: February 2, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Mark E. Salvati, Ricardo M. Attar, Marco M. Gottardis, James Aaron Balog, Dacia A. Pickering, Rogelio L. Martinez, Chongqing Sun
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Publication number: 20100022638Abstract: The present invention relates to new 3-substituted 6-nitrooxy-hexahydrofuro[3,2-b]furane derivatives possessing a superior pharmacological activity in thrombosis and in coronary ischemia models.Type: ApplicationFiled: December 15, 2008Publication date: January 28, 2010Applicant: Lacer, S. A.Inventors: Juan Carlos DEL CASTILLO NIETO, Marisabel Mourelle Mancini, Francisco Pubill Coy, Lydia Cabeza Llorente, Jose Repolles Moliner
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Patent number: 7649015Abstract: Phosphonate substituted compounds with HIV protease inhibitory properties having use as therapeutics and for other industrial purposes are disclosed. The compositions inhibit HIV protease activity and/or are useful therapeutically for the treatment of AIDS and other antiviral infections, as well as in assays for the detection of HIV protease.Type: GrantFiled: April 25, 2003Date of Patent: January 19, 2010Assignee: Gilead Sciences, Inc.Inventors: Murty N. Arimili, Xiaowu Chen, Maria Fardis, Gong-Xin He, Haolun Jin, Choung U. Kim, William A. Lee, Kuei-Ying Lin, Hongtao Liu, Richard L. Mackman, Michael L. Mitchell, Hyung-Jung Pyun, Mark Sparacino, Sundaramoorthi Swaminathan, Jianying Wang, Matthew A. Williams, Lianhong Xu, Zheng-Yu Yang, Richard H. Yu, Jiancun Zhang, Lijun Zhang
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Publication number: 20100010082Abstract: The present disclosure relates to ophthalmic solutions and methods of using the solutions to treat ocular disordersType: ApplicationFiled: July 9, 2009Publication date: January 14, 2010Applicant: Aspreva International Ltd.Inventors: Eddie CHONG, Clive BURGE, Lee MIZZEN
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Publication number: 20100004208Abstract: The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerisation inhibitors.Type: ApplicationFiled: February 2, 2007Publication date: January 7, 2010Applicant: BIONOMICS LIMITEDInventors: Jason Hugh Chaplin, Gurmit Singh Gill, Damian Wojciech Grobelny, Bernard Luke Flynn, Gabriel Kremmidiotis
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Publication number: 20090312318Abstract: The present invention provides compounds of Formula (I): wherein A, X, Q, R2-R6, m, and W have the values described herein, as well as compositions comprising such compounds. The compounds are protease inhibitors and are useful for inhibiting the development of drug resistance in animals.Type: ApplicationFiled: July 24, 2007Publication date: December 17, 2009Inventors: Manoj C. Desai, Christopher P. Lee, Hongtao Liu, Sundaramoorthi Swaminathan, Lianhong Xu
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Publication number: 20090306201Abstract: A pharmaceutical composition comprising a compound of formula I or II and a pharmaceutically acceptable carrier. Methods for treating a proliferative disorder mediated by a methyl transferase comprising administering an anti-proliferative effective amount of the compound of formula I or II are also presented.Type: ApplicationFiled: June 15, 2007Publication date: December 10, 2009Applicant: University of Medicine and Dentistry of New JerseyInventors: Danny Reinberg, Patrick Trojer, Gianluca Sbardella
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Publication number: 20090304815Abstract: The invention relates to a method of treatment for muscular dystrophies, including Duchenne, Becker, limb-girdle, facioscapulohumeral, congenital muscular dystrophies and the like using a combination of nitric oxide-releasing and anti-inflammatory compounds.Type: ApplicationFiled: February 1, 2007Publication date: December 10, 2009Inventors: Giulio Cossu, Emilio Clementi, Silvia Brunelli
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Publication number: 20090306027Abstract: The invention provides methods for treating various indications and diseases in a patient in need thereof, wherein the patient has a C825T polymorphism in the G protein beta3 subunit (GNB3), comprising administering to the patient (i) at least one antioxidant compound or a pharmaceutically acceptable salt thereof; (ii) at least one nitric oxide enhancing compound; and (iii) optionally the best current therapy for the treatment of cardiovascular diseases. In one embodiment the antioxidant is a hydralazine compound or a pharmaceutically acceptable salt thereof and the nitric oxide enhancing compound is isosorbide dinitrate and/or isosorbide mononitrate.Type: ApplicationFiled: April 4, 2007Publication date: December 10, 2009Applicants: NitoMed, Inc., Unversity of Pittsburgh of the Commonwealth System of the Higher EducationInventors: Manuel Worcel, Michael Sabolinski, Sang W. Tam, Dennis M. McNamara
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Patent number: 7622465Abstract: Disclosed are methods for inhibiting TNF? expression, IL-1? expression, iNOS expression, and NF-?B activity and methods for treating autoimmune disease, cancer, or atherosclerosis with a compound of the following formula:Type: GrantFiled: December 16, 2008Date of Patent: November 24, 2009Assignee: Hutchison Medipharma Enterprises LimitedInventors: Wei-Guo Su, Hong Jia, Xiaoqiang Yan, Jifeng Duan, Tao Wang, Yu Cai, Weihan Zhang
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Publication number: 20090285797Abstract: The invention relates to methods and compositions for regulating nicotine metabolism. Also provided are methods for screening and assessing substances for regulating nicotine metabolism. Methods are provided for assessing nicotine metabolism.Type: ApplicationFiled: September 25, 2008Publication date: November 19, 2009Applicant: Nicogen Inc.Inventors: Edward M. Sellers, Rachel F. Tyndale
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Publication number: 20090281177Abstract: The present invention discloses a butylphthalide intravenous emulsion for intravenous injection or infusion, containing butylphthalide or derivatives thereof as an active ingredient in an amount of 0.01˜50 wt % and an excipient in an amount of 50˜99.99 wt %, based on the total weight of the emulsion.Type: ApplicationFiled: December 15, 2006Publication date: November 12, 2009Applicant: SHIJIAZHUAN PHARMA GROUP NBP PHARMACEUTICAL CO., LTD.Inventors: Chunshun Zhao, Zhanqi Niu, Zhen Chen, Haibo Guo
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Publication number: 20090274650Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.Type: ApplicationFiled: February 12, 2009Publication date: November 5, 2009Inventors: Michael R. Hale, Roger Tung, Stephen Price, Robin David Wilkes, Wayne Carl Schairer, Ashley Nicholas Jarvis, Andrew Spaltenstein, Eric Steven Furfine, Vicente Samano, Istvan Kaldor, John Franklin Miller, Michael Stephen Brieger, Ronald George Sherrill
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Patent number: 7605158Abstract: The present invention provides a carbamoyl-type benzofuran derivative of the formula [1]: wherein Ring Z is a group of the formula: etc.; A is a single bond, and the like; Y is a cycloalkanediyl group, etc.; R4 and R5 are the same or different and each is an optionally substituted lower alkyl group, etc.; R1 is a halogen atom, etc.; Ring B of the formula: is an optionally substituted benzene ring; and R3 is a hydrogen atom. etc., or a pharmaceutically acceptable salt thereof, which is useful as an FXa inhibitor.Type: GrantFiled: September 24, 2004Date of Patent: October 20, 2009Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Takayuki Kawaguchi, Hidenori Akatsuka, Masamichi Morimoto, Tatsuya Watanabe, Toru Iijima, Jun Murakami
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Publication number: 20090253662Abstract: The invention provides methods for (a) reducing mortality associated with heart failure; (b) improving oxygen consumption; (c) treating heart failure; (d) treating hypertension; (e) improving the quality of life in a heart failure patient; (f) inhibiting left ventricular remodeling; (g) reducing hospitalizations related to heart failure; (h) improving exercise tolerance; (j) increasing left ventricular ejection fraction; (Ic) decreasing levels of B-type natriuretic protein; (l) treating renovascular diseases; (m) treating end-stage renal diseases; (n) reducing cardiomegaly; (o) treating diseases resulting from oxidative stress; (p) treating endothelial dysfunctions; (q) treating diseases caused by endothelial dysfunctions; or (r) treating cardiovascular diseases; in a patient in need thereof, wherein the patient has a ?344 (T/T) polymorphism or a ?344 (C/C) polymorphism in an aldosterone synthase CYP11B2 gene, comprising administering to the patient (i) at least one antioxidant compound or a pharmaceuticallyType: ApplicationFiled: October 4, 2006Publication date: October 8, 2009Applicants: NitroMed, Inc., University of Pittsburgh of the Commonwealth System of Higher EducationInventors: Manuel Worcel, Michael Sabolinski, Sang W. Tam, Dennis M. McNamara
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Patent number: 7595064Abstract: A method for isolating the bioactive component of the water-soluble extract of Uncaria tomentosa known as C-MED-100®, comprising (i) precipitating the spray drying carrier from C-MED-100®; (ii) using the resulting C-MED-100® to obtain a spotting mixture for thin layer chromatography (TLC); (iii) spotting the C-MED-100® spotting mixture on pre-run TLC plates and eluting the plates to obtain the fluorescing band with Rf=0.2-0.3; (iv) scraping off the Rf=0.2-0.3 band, eluting it in ammonia and freeze drying the eluted band to form a powder; and (v) extracting the powder with methanol to remove solubilized silica gel, concentrating the methanol solution and crystallizing the concentrated solution to obtain the bioactive component. The isolated bioactive component in vitro is a quinic acid analog, preferably quinic acid lactone. By contrast, the isolated bioactive component in vivo is quinic acid, whether as free acid or as a quinic acid salt, including quinic acid ammonium salt.Type: GrantFiled: October 21, 2004Date of Patent: September 29, 2009Inventor: Ronald W. Pero
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Publication number: 20090239791Abstract: A pharmaceutical composition comprising a lipophilic substance which inhibits IL-2 production, and a base capable of inhibiting blood exposure of the substance and delivering the substance to lymph following oral administration, is disclosed. The pharmaceutical composition can inhibit blood exposure of the substance to reduce its adverse effects, and can develop desired pharmacological effects.Type: ApplicationFiled: October 23, 2008Publication date: September 24, 2009Applicant: Astellas Pharma Inc.Inventors: Takayuki Yoshida, Kiyo Nakanishi, Atsushi Maeda, Kazuhiro Sako, Yuki Kasashima, Hiromu Kondo, Tatsunobu Yoshioka, Yuuki Tsutsui
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Patent number: 7585888Abstract: This invention relates to novel benzofuran and benzothiophene derivatives of the general formula and their use for the treatment of hyper-proliferative disorders.Type: GrantFiled: March 31, 2008Date of Patent: September 8, 2009Assignee: Bayer Pharmaceuticals CorporationInventors: Chengzhi Zhang, Michael J. Burke, Zhi Chen, Jacques P. Dumas, Dongping Fan, Jianmei Fan, Holia Hatoum-Mokdad, Benjamin D. Jones, Gaetan Ladouceur, Wendy Lee, Barton Phillips
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Patent number: 7579023Abstract: A method for isolating the bioactive component of the water-soluble extract of Uncaria tomentosa known as C-MED-100®, comprising (i) precipitating the spray drying carrier from C-MED-100®; (ii) using the resulting C-MED-100® to obtain a spotting mixture for thin layer chromatography (TLC); (iii) spotting the C-MED-100® spotting mixture on pre-run TLC plates and eluting the plates to obtain the fluorescing band with Rf=0.2-0.3; (iv) scraping off the Rf=0.2-0.3 band, eluting it in ammonia and freeze drying the eluted band to form a powder; and (v) extracting the powder with methanol to remove solubilized silica gel, concentrating the methanol solution and crystalizing the concentrated solution to obtain the bioactive component. The isolated bioactive component is a quinic acid analog, preferably quinic acid lactone. A pharmaceutical composition comprising a pharmaceutically effective amount of the bioactive component and a nontoxic inert carrier or diluent.Type: GrantFiled: November 9, 2005Date of Patent: August 25, 2009Assignee: Optigenex, Inc.Inventor: Ronald W. Pero
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Publication number: 20090209639Abstract: A process for modifying the crystal habit of acicular drug substances, crystals obtained by such a process, and particular crystal forms or modifications of mycophenolic acid or mycophenolate sodium are provided, as well as pharmaceutical compositions comprising the crystals, methods of treatment and uses thereof.Type: ApplicationFiled: December 18, 2008Publication date: August 20, 2009Inventors: Sabine Pfeffer, Dierk Wieckhusen
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Publication number: 20090209532Abstract: Compounds of formula (I) exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors.Type: ApplicationFiled: July 17, 2006Publication date: August 20, 2009Inventors: Marko Ahlmark, Reijo Backstrom, Anne Luiro, Jarmo Pystynen, Eija Tiainen
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Publication number: 20090203653Abstract: The invention describes novel compositions comprising at least one apocynin compound or a pharmaceutically acceptable salt thereof, and at least one nitric oxide donor, and, optionally, at least one therapeutic agent. The invention also provides novel kits comprising at least one apocynin compound or a pharmaceutically acceptable salt thereof, and at least one nitric oxide donor compound, and, optionally, at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating gastrointestinal disorders; (h) treating inflammatory disorders; and (j) treating respiratory disorders. The apocynin compound may preferably be apocynin. The nitric oxide donor compound may preferably be isosorbide dinitrate and/or isosorbide mononitrate.Type: ApplicationFiled: October 3, 2005Publication date: August 13, 2009Applicant: NITROMED, INC.Inventor: David S. Garvey
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Publication number: 20090192218Abstract: The present invention relates to the use of a compound as effective agent for the prevention or treatment of diabetes mellitus in a mammal. Said compounds being selected from the group of phthalide derivatives and exhibit excellent blood glucose lowering effects and thus are effective agents in the prevention or treatment of diabetes mellitus in mammals.Type: ApplicationFiled: March 27, 2009Publication date: July 30, 2009Inventors: Daniel D'Orazio, Antoine De Saizieu, Goede Schueler, Daniel Raederstorff, Sandra Renata Teixeira, Ying Wang Schmidt, Peter Weber, Swen Wolfram
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Publication number: 20090192128Abstract: The invention provides methods for (a) reducing mortality associated with heart failure; (b) improving oxygen consumption; (c) treating heart failure; (d) treating hypertension; (e) improving the quality of life in a heart failure patient; (f) inhibiting left ventricular remodeling; (g) reducing hospitalizations related to heart failure; (h) improving exercise tolerance; (j) increasing left ventricular ejection fraction; (k) decreasing levels of B-type natriuretic protein; (l) treating renovascular diseases; (m) treating end-stage renal diseases; (n) reducing cardiomegaly; (o) treating diseases resulting from oxidative stress; (p) treating endothelial dysfunctions; (q) treating diseases caused by endothelial dysfunctions; or (r) treating cardiovascular diseases; in a patient in need thereof, wherein the patient has a Arg389Arg polymorphism and/or a Gly389Gly polymorphism in the beta 1 adrenergic receptor gene, comprising administering to the patient (i) at least one antioxidant compound or a pharmaceuticallyType: ApplicationFiled: October 4, 2006Publication date: July 30, 2009Applicants: NitroMed Inc., University of Pittsburgh of the Commonwealth System of Higher EducationInventors: Manuel Worcel, Michael L. Sabolinski, Sang W. Tam, Dennis M. McNamara
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Publication number: 20090192213Abstract: The present invention relates to benzo[b]furane and benzo[b]thiophene derivatives of the general formula IV as the free base or salts thereof and their use.Type: ApplicationFiled: February 20, 2009Publication date: July 30, 2009Applicant: H. Lundbeck A/SInventors: Jan Kehler, Karsten Juhl, Morten Bang Norgaard
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Publication number: 20090191283Abstract: The formulation provides a method of treating headaches, neck, joint and inflammatory-type pain in a mammalian subject by administering to the subject a therapeutically effective amount of a nitrate-containing compound and a therapeutically effective amount of a selenium-containing compound. The formulation also provides kits and systems for practicing the subject methods.Type: ApplicationFiled: January 24, 2008Publication date: July 30, 2009Inventors: Bryan Todd Oronsky, Neil Charles Oronsky
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Publication number: 20090186916Abstract: Provided is a compound that is an NMDA receptor antagonist having a broader safety margin, and is useful as an agent for treating or preventing Alzheimer's disease, cerebrovascular dementia, Parkinson's disease, ischemic apoplexy, or pain. A novel compound or a salt thereof, which is characterized in that it has an amino group and R1 (lower alkyl, cycloalkyl, -lower alkylene-aryl, aryl which may be substituted, and the like) on carbon atoms of indane, cyclopenta[b]thiophene, cyclopenta[b]furan, cyclopenta[b]pyridine, or cyclopenta[c]pyridine ring, or 2,3-dihydrdo-1-benzofuran, 2,3-dihydrdo-1-benzothiophene, indoline ring, or the like, and has R2 and R3 (the same or different, each lower alkyl or aryl) on carbon atoms beside them, and an NMDA receptor antagonist comprising the same as an active component.Type: ApplicationFiled: July 17, 2007Publication date: July 23, 2009Applicant: ASTELLAS PHARMA INC.Inventors: Satoshi Hayashibe, Shingo Yamasaki, Kazushi Watanabe, Nobuyuki Shiraishi, Daisuke Suzuki, Hiroaki Hoshii, Junya Ohmori, Takatoshi Kanayama
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Publication number: 20090176873Abstract: The present invention relates to the use of compounds of the formula (I) wherein the clotted line is an optional bond; R1 is butyl or butyryl if R2 is hydroxyl but is butyl if R2 is hydrogen; or R1 and R2 taken together are 1-butylidene optionally substituted by hydroxyl, methyl, or 3-(?,?-dimethylacrylyloxy)-pentylidenyl; X is a residue selected from the group consisting of X1, X2, X3, X4, and X5; wherein X is X2, X3 or X5 if the dotted line in formula (I) is absent; and X is X1, X4 or X5 if the dotted line signifies a bond in formula (I) above; R3 is hydroxyl or butyryl; and n is 1 or 2, as agents for the prevention, control and treatment of conditions requiring modulation of inflammation in mammals. In another aspect, the present invention relates to the use of compounds of the formula (I) as active ingredients in the manufacture of medicaments/compositions for the prevention, control and treatment of conditions requiring modulation of inflammation.Type: ApplicationFiled: May 24, 2006Publication date: July 9, 2009Applicant: DSM IP ASSETS B.V.Inventors: Ann Fowler, Daniel Raederstorff, Goede Schuler, Joseph Schwager
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Publication number: 20090169560Abstract: In the present invention there are disclosed new derivatives of dianhydrohexite mononitrate corresponding to formula (I), tautomers, pharmaceutically acceptable salts, prodrugs and solvates thereof: as well as pharmaceutical compositions comprising these compounds and uses thereof.Type: ApplicationFiled: March 9, 2009Publication date: July 2, 2009Applicant: LACER S.A.Inventors: Jose Repolles Moliner, Eduardo Salas Perez-Rasilla, Francisco Pubill Coy
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Patent number: 7544676Abstract: Novel sulfamoyl benzamide compounds, pharmaceutical compositions containing the sulfamoyl benzamide compounds, and methods of their pharmaceutical use are disclosed. In certain embodiments, the sulfamoyl benzamide compounds are agonists and/or ligands of cannabinoid receptors and may be useful, inter alia, for treating and/or preventing pain, gastrointestinal disorders, inflammation, auto-immune diseases, ischemic conditions, immune-related disorders, hypertension, neurological disorders, and neurodegenerative diseases, for providing cardioprotection against ischemic and reperfusion effects, for inducing apoptosis in malignant cells, for inhibiting mechanical hyperalgesia associated with nerve injury, and as an appetite stimulant.Type: GrantFiled: November 9, 2006Date of Patent: June 9, 2009Assignee: Adolor CorporationInventors: Roland E. Dolle, Karin Worm
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Patent number: 7538137Abstract: A novel natural compound having various therapeutically effects is provided. The compound is obtainable from Sibiraea leaves by aqueous extraction and is represented by a formula (1) as follows.Type: GrantFiled: May 22, 2006Date of Patent: May 26, 2009Assignee: Iskra Industry Co., Ltd.Inventors: Yasuo Sei, Yoshihiro Kano, Ryotarou Takabori
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Patent number: 7538138Abstract: Compounds of formula (I) or a pharmaceutically acceptable salts or prodrug thereof which are useful for the modulation of the histamine-3 receptors in mammals and which are useful for the treatment of disorders ameliorated by histamine-3 receptor ligands.Type: GrantFiled: April 8, 2005Date of Patent: May 26, 2009Assignee: Abbott LaboratoriesInventors: Marlon D. Cowart, Youssef L. Bennani, Ramin Faghih, Gregory A. Gfesser, Lawrence A. Black
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Publication number: 20090131363Abstract: This invention relates to novel compounds that are hydroxyethylamino sulfonamide derivatives and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel hydroxyethylamino sulfonamide derivatives that are derivatives of darunavir. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering a human immunodeficiency virus (HIV) protease inhibitor, such as darunavir.Type: ApplicationFiled: October 24, 2008Publication date: May 21, 2009Inventor: Scott L. Harbeson
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Publication number: 20090131427Abstract: Disclosed are methods for inhibiting TNF? expression, IL-1? expression, iNOS expression, and NF-?B activity and methods for treating autoimmune disease, cancer, or atherosclerosis with a compound of the following formula:Type: ApplicationFiled: December 16, 2008Publication date: May 21, 2009Applicant: HUTCHISON MEDIPHARMA ENTERPRISES LIMITEDInventors: Weiguo Su, Hong Jia, Weihan Zhang, Xiaoqiang Yan, Jifeng Duan, Tao Wang, Yu Cai
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Patent number: 7534903Abstract: The use of compounds corresponding to formula I: in which R1, R2, R3, R4, R5 and R6 have the meanings given in the description for treating cardiac arrhythmias and other disease states.Type: GrantFiled: January 18, 2008Date of Patent: May 19, 2009Assignee: Solvay Pharmaceuticals GmbHInventors: David Sykes, Brian Moloney, Lester Marrison, Dieter Ziegler, Michael Mlinaric, Christiane Boecker, Reinhard Brueckner, Michael Weske, Klaus Witte, Yvan Fischer
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Publication number: 20090105279Abstract: The invention is related to compounds of Formula I: or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.Type: ApplicationFiled: July 19, 2007Publication date: April 23, 2009Inventors: Carina E. Cannizzaro, James M. Chen, Manoj C. Desai, Michael L. Mitchell, Sundaramoorthi Swaminathan, Lianhong Xu, Zheng-Yu Yang
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Publication number: 20090088469Abstract: Method for the preparation of citalopram comprising reaction of a compound of Formula (IV) wherein R is halogen, or CF3—(CF2)n—SO2—, n being 0 to 8, with a cyanide source in the presence of a palladium catalyst and a catalytic amount of Cu+ or Zn2+, or with Zn(CN)2 in the presence of a palladium catalyst.Type: ApplicationFiled: December 8, 2008Publication date: April 2, 2009Applicant: H. Lundbeck A/SInventors: Hans Petersen, Michael Harold Rock, Henrik Svane