Nitrogen Containing Patents (Class 514/471)
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Patent number: 7795315Abstract: The present invention provides novel compounds of the general formula (I) and pharmaceutically acceptable salts thereof, processes for the manufacture of these novel compounds and medicaments containing such compounds. The compounds of the present invention show anti-proliferative and differentiation-inducing activity, which results in inhibition of tumor cell proliferation, induction of apoptosis and inhibition of invasion. The invention also covers the use of such compounds for the treatment of diseases such as cancer and for the manufacture of corresponding medicaments.Type: GrantFiled: January 23, 2009Date of Patent: September 14, 2010Assignee: Hoffman-La Roche Inc.Inventors: Li Chen, Yun He, Jason Christopher Wong
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Publication number: 20100222298Abstract: The invention relates to novel spill resistant formulations comprising either a weak base or a weak acid as the pharmaceutical ingredient, a liquid base, a clay and a water soluble cellulose ether. The clay and cellulose ether allow for a broader pH range into which the pharmaceutically active agent may be dispersed or dissolved, and therefore allows for easier preparation and formulation of the pharmaceutical composition.Type: ApplicationFiled: May 13, 2010Publication date: September 2, 2010Applicant: Taro Pharmaceuticals U.S.A., Inc.Inventors: Satish ASOTRA, Xiaoli WANG, Zoltan BODOR
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Publication number: 20100221337Abstract: Embodiments of the present invention provide methods of treating pain, arthritis and inflammation comprising administering naproxen 2(methanesulfonyl)ethyl ester and an H2 receptor antagonist. Further embodiments provide pharmaceutical compositions comprising naproxen 2(methanesulfonyl)ethyl ester and an H2 receptor antagonist.Type: ApplicationFiled: February 14, 2008Publication date: September 2, 2010Applicant: LOGICAL THERAPEUTICS, INC.Inventors: Mitchell P. Fink, Kathryn Lea Sewell
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Publication number: 20100216849Abstract: This invention relates to novel biphenylcarboxamides of the formula (I) in which R, Z, X, Y, m, n and A are as defined in the disclosure, to a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and to novel intermediates and their preparation.Type: ApplicationFiled: April 30, 2010Publication date: August 26, 2010Inventors: Ralf Dunkel, Hans-Ludwig Elbe, Heiko Rieck, Ulrike Wachendorff-Neumann, Peter Dahmen, Peter Lösel, Karl-Heinz Kuck, Astrid Mauler-Machnik, Jörg Nico Greul
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Publication number: 20100215774Abstract: The present invention is related to the composition and methods of manufacture of orally-dissolvable, edible films as a vehicle for the non-invasive administration of nitroglycerin and/or other active drugs through the mucosal tissues of the oral cavity. The films include a water soluble film-forming polymer such as pullulan. Methods for producing the films are also disclosed.Type: ApplicationFiled: February 8, 2008Publication date: August 26, 2010Inventor: Todd Maibach
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Publication number: 20100215643Abstract: Devices are provided which are functionalized to include surface regions having anti-infective agents. Methods are provided for functionalizing various material surfaces to include active surface regions for binding anti-infective agents. Methods are provided by which anti-infective moieties or agents are bonded to functionalized surfaces.Type: ApplicationFiled: February 24, 2010Publication date: August 26, 2010Applicant: ORTHOBOND CORP.Inventors: Randell Clevenger, Jeffrey Schwartz
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Publication number: 20100210608Abstract: The invention describes the use of betaine for treating and preventing arterites. The invention also describes an orally administered composition for treating arterites and, in particular, intermittent claudication, said composition containing, as an active ingredient, an active therapeutic quantity of betaine glycine by single dose. The invention particularly describes a medicament provided for treating a patient suffering from an intermittent claudication caused by peripheral circulatory disorders such as arteriosclerosis obliterans or by thromboangiitis obliterans.Type: ApplicationFiled: March 17, 2010Publication date: August 19, 2010Inventor: Jallal Messadek
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Publication number: 20100197494Abstract: The present invention relates to novel active substance combinations which contain firstly at least one known compound of the formula (I) in which R1 and A have the meanings given in the description, and secondly at least one further known active substance from the class of the neonicotinoids, and which are highly suitable for controlling animal pests such as insects and undesired acarids.Type: ApplicationFiled: September 13, 2008Publication date: August 5, 2010Inventors: Heike Hungenberg, Peter Jeschke, Robert Velten, Wolfgang Thielert
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Publication number: 20100196430Abstract: An object of the present invention is to provide an agricultural chemical formulation which is able to control release of an agricultural chemical active ingredient. This agricultural chemical formulation includes a composition, containing an agricultural chemical active ingredient, styrene-maleic anhydride copolymer or mixture of styrene-maleic anhydride copolymer and polymer having repeating units derived from rosin or derivative thereof or salicylic acid or derivative thereof, and a release controller (a water-soluble polymer, a hydrophobically-treated silicon oxide, or a surfactant), forming a compatible state or matrix.Type: ApplicationFiled: April 6, 2010Publication date: August 5, 2010Applicant: NIPPON SODA CO., LTDInventors: Yuichi Maekawa, Yoshihisa Endo, Yoshihiro Enomoto
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Publication number: 20100197661Abstract: The present invention provides methods for treating neurological diseases and disorders. Compounds that replace or enhance the function of SMN or alleviate or reduce a phenotype of cells with low SMN protein levels are provided. Screening methods and kits for identifying such compounds also are provided.Type: ApplicationFiled: March 23, 2010Publication date: August 5, 2010Inventors: Gideon Dreyfuss, Jin Wang
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Patent number: 7763612Abstract: Therapeutic amine-arylsulfonamide conjugate compounds, of the general formula: wherein R? is [D-W-], hydroxyl, or alkoxyl; R? is independently [D-W?-], hydrogen, alkoxy, alkyl, cycloalkyl, alkenyl, alkynyl or aryl, or R? and R? together with the nitrogen atom to which they are attached form a 4-, 5-, 6-, 7- or 8-membered ring optionally containing one or two further heteroatoms independently selected from nitrogen, oxygen and sulfur; D is independently a therapeutic amine radical comprising at least one nitrogen atom and optionally at least one oxygen atom coupled to W or W? by a nitrogen or oxygen atom; W and W? are a chemical bond or linker; wherein either R? is [D-W-] or at least one R? is [D-W?-], and pharmaceutically acceptable esters, amides, salts or solvates thereof, pharmaceutical compositions containing same, methods for their preparation, and their use in treating psychiatric, neurologic and metabolic disorders are disclosed.Type: GrantFiled: January 3, 2007Date of Patent: July 27, 2010Assignee: Algebra, Inc.Inventors: Philip F. Morgan, James L. Kelley
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Publication number: 20100179218Abstract: Compounds of the following formula are disclosed: Methods of preparing the compounds, pharmaceutical compositions comprising the compounds, and methods of treating patients by administration of the pharmaceutical compositions are disclosed.Type: ApplicationFiled: February 5, 2010Publication date: July 15, 2010Applicant: QLT Inc.Inventors: WILLIAM L. MATIER, Ghanshyam Patil
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Publication number: 20100179168Abstract: The present invention therefore provides compounds of formula (I) or pharmaceutically acceptable salts thereof: (I) processes for their preparation, pharmaceutical compositions containing the same and to their use in the treatment of gastrointestinal and other disorders.Type: ApplicationFiled: April 13, 2007Publication date: July 15, 2010Inventors: Emma Louise Blaney, David Kenneth Dean, Alessandra Gaiba, Nigel Paul King, Jason Witherington
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Publication number: 20100168068Abstract: The invention provides novel compounds of formulae I and II: that are monoamine oxidase-B inhibitors, which can be useful in treating obesity, diabetes, and/or cardiometabolic disorders (e.g., hypertension, dyslipidemias, high blood pressure, and insulin resistance).Type: ApplicationFiled: December 31, 2009Publication date: July 1, 2010Applicant: JENRIN DISCOVERYInventors: John Francis McElroy, Robert J. Chorvat, Parthasarathi Rajagopalan
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Publication number: 20100167936Abstract: The invention relates to the use of at least one ascorbic acid derivative for the functionalisation of matrices, and to specific ascorbic acid derivatives and processes for the preparation thereof.Type: ApplicationFiled: June 27, 2007Publication date: July 1, 2010Inventors: Thomas Rudolph, Philipp Buehle, Herwig Buchholz
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Patent number: 7745456Abstract: The present invention relates to novel 2,5-bis{[alkyl (or aryl) imino] aminophenyl}furans and thiophenes of the general formula in which R1, R2, R3 and R4 are each independently selected from the group consisting of H, alkyl, alkoxy, halide, and alkylhalide groups; R5 is H, alkyl or aryl; R6 is H, alkyl, aryl, or NR7R8, in which R7 and R8 are each independently selected from the group consisting of H, alkyl and aryl; and X is O, S or NR9, in which R9 is H or alkyl, and to the use of such compounds.Type: GrantFiled: July 9, 2007Date of Patent: June 29, 2010Assignees: The University of North Carolina at Chapel Hill, Duke University, Georgia State University Research Foundation, Inc.Inventors: David W. Boykin, Richard R. Tidwell, W. David Wilson, John R. Perfect, Chad F. Stephens
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Publication number: 20100160327Abstract: The present invention relates to a novel class of modified malonate derivatives. The modified malonate compounds can be used to treat cancer. The modified malonate compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: June 21, 2006Publication date: June 24, 2010Inventors: Jonathan Grimm, Paul Harrington, Richard Heidebrecht, JR., Thomas Miller, Karin Otte, Phieng Siliphaivanh, David Sloman, Matthew Stanton, Kevin Wilson, David Witter, Solomon Kattar, Paul Tempest
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Patent number: 7741323Abstract: An indene derivative for selectively modulating the activities of peroxisome proliferator activated receptors (PPARs) having the following formula (I): wherein, R1 is C1-6 alkyl, C1-6 alkenyl, or C3-6 cycloalkyl, each of which is unsubstituted or substituted with one or more phenyl groups; R2 is H, CN, CO2Ra, CH2CO2Ra, CONRbRc, or phenyl; R3 is C1-6 alkyl, C3-6 cycloalkyl, naphthyl, phenyl, being each unsubstituted or substituted with one or more substituents selected from the group consisting of halogen, CN, NH2, NO2, ORa, phenyloxy, C1-6 alkyl, and C3-6 cycloalkyl; and R4, R5, R6, and R7 are each independently H, OH, OSO2CH3, O(CH2)mRe, CH2Rf, OCOCH2ORg, OCH2CH2ORg, OCH2CH?CHRg, or pyridine-2-yloxy, or R5 and R6 together form OCH2O.Type: GrantFiled: April 13, 2005Date of Patent: June 22, 2010Assignees: Korea Research Institute of Chemical Technology, Jeil Pharm. Co., Ltd., Korea Research Institute of Bioscience and Biotechnology, CJ Corp.Inventors: Hyae Gyeong Cheon, Sung-Eun Yoo, Sung Soo Kim, Sung-Don Yang, Kwang-Rok Kim, Sang Dal Rhee, Jin Hee Ahn, Seung Kyu Kang, Won Hoon Jung, Sung Dae Park, Nam Gee Kim, Jang Hyuk Lee, Sun Chul Huh, Jae Mok Lee, Seog Beom Song, Soon Ji Kwon, Jong Hoon Kim, Jeong-Hyung Lee, Seung Jun Kim
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Patent number: 7737288Abstract: Non-steroidal androgen receptor modulating compounds of the general formula (I), their pharmaceutically acceptable salts, preparation process and pharmaceutically compositions containing the said compounds are disclosed. Such compounds of the general formula (I) or their pharmaceutically acceptable salts can be used for preparing non-steroidal medicines to treat and/or prevent conditions or diseases such as prostatic hyperplasia, prostate cancer, hirsutism, severe hormone-dependent alopecia or acne, etc. as a result of androgen receptor antagonistic activities.Type: GrantFiled: May 26, 2006Date of Patent: June 15, 2010Assignees: Shanghai Institute of Materia Medica Chinese Academy of Sciences, Sichuan UniversityInventors: Mingwei Wang, Caihong Zhou, Xin Hui, Haoran Su, Jie Gao, Yong Deng, Dacheng Yang
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Publication number: 20100144785Abstract: The present invention relates N-(aromatic, 6-membered, fused, (hetero)aryl-methylene)-N-cycloalkyl carboxamide derivatives, their thiocarboxamide or N-substituted carboximidamide analogues, all of formula (I) wherein A represents a carbo-linked 5-membered heterocyclyl group; T represents O, S, N—Rc, N—ORd, N—NRcRd or N—CN; Z1 to Z3 and B represents an aromatic, 6-membered, fused, (hetero)aryl; their process of preparation; their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: ApplicationFiled: July 31, 2008Publication date: June 10, 2010Applicant: Bayer SASInventors: Philippe Desbordes, Stephanie Gary, Marie-Claire Grosjean-Cournoyer, Benoit Hartmann, Philippe Rinolfi, Arounarith Tuch
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Publication number: 20100144817Abstract: The present invention relates to N-cycloalkyl-benzyl-thiocarboxamide or N-cycloalkyl-benzyl-N-substituted-carboximidamide amide derivatives of formula (I) wherein A represents a carbo-linked, unsaturated or partially saturated, 5-membered heterocyclyl; T represents S, N—Ra, N—ORa, N—NRaRb or N—CN; Z1 represents a C3-C7-cycloalkyl and Z2; Z3, X and n represent various substituents; their process of preparation; their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: ApplicationFiled: July 31, 2008Publication date: June 10, 2010Applicant: Bayer SASInventors: Philippe Desbordes, Stephanie Gary, Marie-Claire Grosjean-Cournoyer, Benoit Hartmann, Philippe Rinolfi, Jean-Pierre Vors
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NOVEL AROMATIC HETEROCYCLIC CARBOXYLIC ACID AMIDE DERIVATIVES USEFUL AS POTASSIUM CHANNEL MODULATORS
Publication number: 20100137312Abstract: This invention relates to novel aromatic heterocyclic carboxylic acid amide derivatives of formula (I) 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: May 13, 2008Publication date: June 3, 2010Applicant: neuroSearch A/SInventors: Antonio Nardi, Jeppe Kejser Christensen, Palle Christophersen, David Spencer Jones, Elsebet Østergaard Nielsen, Dorte Strøbæk, Lars Siim Madsen -
Publication number: 20100130556Abstract: A compound of formula (III): or a salt, solvate and chemically protected form thereof, wherein: R5 is an optionally substituted C5-20 aryl or C4-20alkyl group; L? is a single bond, —O— or —C(?O)—; A is selected from the group consisting of: formulae (i) (ii) (iii) wherein X and Y are selected from the group consisting of: O and CR3; S and CR3; NH and CR3; NH and N; O and N; S and N; N and S; and N and O, and where the dotted lines indicate a double bond in the appropriate location, and where Q is either N or CH; D is selected from: formulae (i) (ii) (iii) (iv) (v) (vii) (viii) (ix) B is selected from the group consisting of: formulae (A) (B) where RP6 is selected from fluoro and chloro; and R2 is either: (i) —CO2H; (ii) —CONH2; (iii) —CH2—OH; or (iv) tetrazol-5-yl.Type: ApplicationFiled: August 9, 2006Publication date: May 27, 2010Applicant: ASTERAND UK LIMITEDInventors: Alexander William Oxford, Richard Jon Davis, Robert Alexander Coleman, Kenneth Lyle Clark, David Edward Clark, Shirley Ann Brunton, Neil Victor Harris, Garry Fenton, George Hynd, Keith Alfred James Stuttle, Jonathan Mark Sutton, Mark Richard Ashton, Edward Andrew Boyd
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Publication number: 20100129311Abstract: The present invention relates to new phenylalanine amide inhibitors of ATP-sensitive potassium channels, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: November 23, 2009Publication date: May 27, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventor: Thomas G. Gant
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Publication number: 20100124543Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.Type: ApplicationFiled: July 16, 2009Publication date: May 20, 2010Applicant: Vertex Pharmaceuticals IncorporatedInventors: Roger Dennis Tung, Michael Robin Hale, Christopher Todd Baker, Eric Steven Furfine, Istvan Kaldor, Wieslaw Mieczylaw Kazmierski, Andrew Spaltenstein
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Publication number: 20100113512Abstract: A method of treatment using pharmaceutical compositions containing novel antagonists or inverse agonists at opioid receptors for the treatment of binge eating disorder, anorexia nervosa, bulimia nervosa, excess drug or alcohol use, or eating disorder not otherwise specified.Type: ApplicationFiled: October 29, 2009Publication date: May 6, 2010Inventor: DIANE MICHELE IGNAR
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Publication number: 20100113268Abstract: The invention relates to active compound combinations of chloronicotinyls with oxamyl and to the use of these mixtures for controlling animal pests.Type: ApplicationFiled: December 12, 2007Publication date: May 6, 2010Applicant: Bayer CropScience AGInventors: Wolfram Andersch, Heike Hungenberg, Roland Gallow
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Publication number: 20100099682Abstract: The invention provides compounds of formula (I) wherein R1 represents hydrogen or alkyl; R2 represents an unsubstituted or substituted heterocycle or R2 represents an unsubstituted or substituted aryl; R3 represents alkyl or halogen; X represents a single bond or an alkandiyl-group, optionally interrupted by one or more oxygen atoms or carbonyl groups or carbonyloxy groups in free base or acid addition salt form, processes for their preparation and their use as pharmaceuticals.Type: ApplicationFiled: September 17, 2009Publication date: April 22, 2010Inventors: Ralf GLATTHAR, Thomas J. Troxler, Thomas Zoller, Joachim Nozulak
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Patent number: 7700648Abstract: (5-Benzyl-3-furyl)methyl 2,2-dimethyl-3-((E)-2-cayano-3-methoxy-3-oxo-1-propenyl)cyclopropanecarboxylate has an excellent pesticidal activity, and a pesticidal composition comprising it as an active ingredient is useful for controlling pests.Type: GrantFiled: February 8, 2005Date of Patent: April 20, 2010Assignee: Sumitomo Chemical Company LimitedInventor: Tatsuya Mori
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Publication number: 20100092545Abstract: The invention relates to the film products and methods of their preparation that demonstrate a non-self-aggregating uniform heterogeneity. Desirably, the films disintegrate in water and may be formed by a controlled drying process, or other process that maintains the required uniformity of the film. The films contain a polymer component, which includes polyethylene oxide optionally blended with hydrophilic cellulosic polymers. Desirably, the films also contain a pharmaceutical and/or cosmetic active agent with no more than a 10% variance of the active agent pharmaceutical and/or cosmetic active agent per unit area of the film.Type: ApplicationFiled: November 9, 2009Publication date: April 15, 2010Applicant: MonoSol RX, LLCInventors: Robert K. Yang, Richard C. Fuisz, Garry L. Myers, Joseph M. Fuisz
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Publication number: 20100093828Abstract: Disclosed are compounds of formula (IA), formula (IV) or formula (V), and pharmaceutical compositions containing them which are useful for treating a subject with a proliferative disorder, such as cancer. The disclosed compounds and pharmaceutical compositions are also useful for treating disorders responsive to Hsp70 induction and/or natural killer induction.Type: ApplicationFiled: August 20, 2007Publication date: April 15, 2010Inventors: Keizo Koya, Lijun Sun, Shoujun Chen, Jun Jiang
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Publication number: 20100075914Abstract: The present invention relates to methods for treating, killing, and/or inhibiting the growth of Herpes viruses in human subjects comprising topically administering to a human subject in need thereof a nanoemulsion composition having antiviral properties.Type: ApplicationFiled: April 17, 2009Publication date: March 25, 2010Inventors: Mary R. FLACK, Susan Marie CIOTTI, Tarek HAMOUDA, Joyce A. SUTCLIFFE, James R. Baker, JR.
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Publication number: 20100068282Abstract: A process for the production of a composition comprising a water-insoluble paracetamol or NSAID which comprises the steps of: a) providing a mixture comprising: i) a water-insoluble paracetamol or NSAID, ii) a water soluble carrier, and iii) a solvent for each of the paracetamol or NSAID and the carrier, and b) spray-drying the mixture to remove the or each solvent and obtain a substantially solvent-free nano-dispersion of the paracetamol or NSAID in the carrier.Type: ApplicationFiled: July 13, 2007Publication date: March 18, 2010Inventor: Andrew James Elphick
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Publication number: 20100068291Abstract: The invention relates to oral medicaments having a modified release of proton pump inhibitors (PPI's) that are, in particular, useful in preventing and treating gastrointestinal disorders. The aim of the invention is to provide a novel oral medicament based on PPI's ideally having all or some of the following characteristics: a) quickly providing relief to the patient by increasing the gastric pH after oral administration of the medicament; b) accelerating the recovery of patients while maintaining this increase in the gastric pH for as long as possible after oral administration of the medicament and, in particular, during the night; c) improving the observance of the treatment and the comfort of the patient by taking the medicament once daily.Type: ApplicationFiled: May 15, 2006Publication date: March 18, 2010Applicant: FLAMEL TECHNOLOGIES, S.A.Inventors: Philippe CAISSE, Catherine CASTAN, Rémi MEYRUEIX, Gérard SOULA
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Publication number: 20100069483Abstract: Compounds of Formula I potently inhibit both cyclooxygenase-2 and carbonic anhydrases. Inhibition of carbonic anhydrases by a cyclooxygenase-2 inhibitor may affect significantly the safety and efficacy profiles of such a dual inhibitor in the treatment of cyclooxygenase-2 mediated disorders, compared to a cyclooxygenase-2 inhibitor without carbonic anhydrase inhibitory activity.Type: ApplicationFiled: November 23, 2009Publication date: March 18, 2010Applicant: AMOREPACIFIC CORPORATIONInventors: Mi-Young PARK, Kyung-Min LIM, Song-Seok SHIN, Jun-Yong HA, Shin CHUNG
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Publication number: 20100068280Abstract: Pharmaceutical compositions comprising phenylephrine in a sustained release oral dosage formulation. Compositions can comprise phenylephrine alone or phenylephrine in combination additional pharmaceutically active substances such as an antihistamine and/or an analgesic.Type: ApplicationFiled: June 1, 2007Publication date: March 18, 2010Inventor: John W. PATTON
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Publication number: 20100057047Abstract: A nasal delivery device for and method of delivering substance to the middle meatus in a nasal cavity of a subject in the treatment of a condition, in particular an inflammatory or infectious condition, thereof, the delivery device comprising: a nosepiece unit (17) including a nosepiece (20) for fitting to a nostril of a subject and a nozzle (25) through which substance is in use delivered to the respective nasal cavity; and a delivery unit (29) for delivering substance through the nozzle of the nosepiece; wherein the delivery device is configured to provide for deposition of a significant fraction of the delivered dose on, around and in the vicinity of the middle meatus.Type: ApplicationFiled: February 14, 2007Publication date: March 4, 2010Applicant: OptiNose ASInventors: Per Gisle Djupesland, Colin David Sheldrake, Roderick Peter Hafner
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Publication number: 20100056528Abstract: The invention provides sulfonamide compounds of formula (I) as defined herein, pharmaceutical compositions containing the same and methods of treatment using such compounds and pharmaceutical compositions. These compounds have a common wide range of beneficial therapeutic indications, in particular as analgesic and anti-inflammatory agents.Type: ApplicationFiled: December 19, 2007Publication date: March 4, 2010Inventors: Avihai Yacovan, Iris Alroy, Alexander Aizikovich, Sima Mirilashvili, Flavio Gryszpan
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Publication number: 20100041708Abstract: An N-phenylarylsulfonylamide compound of formula (I) (R1 is COOH etc.; R2 is hydrogen, methyl, etc.; R3 and R4 are a combination of methyl and methyl, etc.; R5 is isopropyl etc.; Ar is thiazolyl, pyridyl, 5-methyl-2-furyl each optionally substituted with methyl; n is zero or 1), a synthetic intermediate for the compound and a process for its preparation. The compound of formula (I) binds to a prostaglandin E2 receptor, especially an EP1 subtype receptor, and antagonizes it. It is less affected by protein binding, so it has a satisfactory in vivo activity. Therefore, it is considered to be useful as an analgesic, an antipyretic agent, an agent for the treatment of pollakiuria (frequent urination) and/or lower urinary tract disease syndrome or an antineoplastic agent.Type: ApplicationFiled: October 21, 2009Publication date: February 18, 2010Applicant: ONO PHARMACEUTICAL Co., Ltd.Inventors: Atsushi NAGANAWA, Tetsuji Saito, Kaoru Kobayashi, Takayuki Maruyama, Yoshihiko Nakai, Shinsuke Hashimoto
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Publication number: 20100035854Abstract: A dry powder suitable for inhalation in a dry powder inhaler, the powder comprising a carrier, an active agent and at least 0.5% by weight of magnesium stearate, the powder being further characterized in that the less than 10% of the surface of the carrier material is covered with particles of magnesium stearate. The invention is also directed to a method of making dry powders by blending together the ingredients mentioned in a diffusion blender for a period time that is less than 60 minutes.Type: ApplicationFiled: August 6, 2009Publication date: February 11, 2010Inventors: Rudi Mueller-Walz, Roland Steiner
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Publication number: 20100029670Abstract: The present invention relates to compounds of formula (I) wherein X, R1, R2, R3, R4 and R5 are as defined herein, which are useful for treating diseases which respond to CXCR2 receptor mediators. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: ApplicationFiled: July 30, 2009Publication date: February 4, 2010Inventors: Urs Baettig, Anne-Marie D'Souza, Peter Hunt, Neil John Press, Simon James Watson
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Publication number: 20100029689Abstract: PDE4 inhibition is achieved by novel compounds, e.g., N-substituted aniline and diphenylamine analogs. The compounds of the present invention are of Formula I: wherein R1, R2, R3, and R4 are as defined herein.Type: ApplicationFiled: July 2, 2009Publication date: February 4, 2010Applicants: MEMORY PHARMACEUTICALS CORPORATION, ROCHE PALO ALTO LLCInventors: Allen T. HOPPER, Joan Marie CAROON, Elbert CHIN, Robert F. DUNN, Sharada Shenvi LABADIE, Jim LI, Richard Allen SCHUMACHER, Francisco Xavier TALAMAS
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Publication number: 20100022594Abstract: Compounds of Formula (I), wherein R1, R2, R3, R4, R5, R6, T, W, X, Y and Z are as defined herein are provided, together with pharmaceutically acceptable salt, hydrates and/or prodrugs thereof. Methods of using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's disease and Down's syndrome are described.Type: ApplicationFiled: October 9, 2009Publication date: January 28, 2010Applicants: Wyeth, ArQule, Inc.Inventors: Anthony F. Kreft, Derek Cecil Cole, Kevin R. Woller, Joseph R. Stock, George Diamantidis, Dennis M. Kubrak, Kristina M. Kutterer, William J. Moore, David S. Casebier
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Publication number: 20100022605Abstract: Described herein are N-hydroxyamlde antibacterial compounds, methods for making the compounds, pharmaceutical compositions containing the compounds and methods of treating bacterial infections utilizing the compounds and pharmaceutical compositions compound of Formula (I): or a salt, solvate ti hydrate thereof, wherein A is (a) eachindicates a point of attachment.Type: ApplicationFiled: December 4, 2006Publication date: January 28, 2010Inventors: Rakesh Kumar Jain, Mikhail Fedorovich Gordeev, Jason Gustaf Lewis, Charles Francavilla
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Patent number: 7645852Abstract: An aliphatic polyester copolymer comprising an aliphatic carbonate unit (a) and an aliphatic polyester unit (b), and a molded body composed of said aliphatic polyester copolymer. The aliphatic polyester copolymer is excellent in heat resistance while having adequate mechanical properties and properties in the molten state.Type: GrantFiled: May 25, 2005Date of Patent: January 12, 2010Assignee: Mitsui Chemicals, Inc.Inventors: Yuji Terado, Masaru Wada, Tatsuhiro Urakami
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Patent number: 7642285Abstract: The present invention provides compositions and methods for modulating the communication and virulence of quorum sensing bacteria. In various exemplary embodiments, the invention provides a combinatorial library of quorum sensing compounds including synthetic analogs of naturally occurring and non-naturally occurring acyl-homoserine lactone (AHL) analogs, and methods of synthesizing and using these compounds.Type: GrantFiled: February 2, 2006Date of Patent: January 5, 2010Assignee: Wisconsin Alumni Research FoundationInventors: Helen E. Blackwell, Grant D. Geske, Rachel W. Wezeman
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Publication number: 20090326018Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity. Formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and R12 are as defined in the specification, and wherein either the bond between the C1 and C2 carbon atoms is a double bond or the bond between the C2 and C3 carbon atoms is a double bond, R2 being absent when the bond between the C1 and C2 carbon atoms is a double bond.Type: ApplicationFiled: October 12, 2007Publication date: December 31, 2009Inventors: Henrik Jernstedt, Lars Krüger, Patrik Rhönnstad, Daniel Nöteberg
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Publication number: 20090318391Abstract: The present invention relates to the treatment of a mammal with a pharmaceutical composition comprising an H2-blocker, at least one anti-inflammatory agent, a cytotoxic agent and, optionally, levamisole, a retinoid, an NFkB inhibitor, a redox quinone, an agent that enhances the intracellular accumulation of NADH+H+, a poly-alcohol, an inhibitor of pro-angiogenic growth factor(s) and an MMP inhibitor, such pharmaceutical composition allowing for the enhanced therapy and/or prevention of neoplastic diseases and disorders.Type: ApplicationFiled: July 4, 2007Publication date: December 24, 2009Applicant: TILTAN PHARMA LTD.Inventor: Shmuel A. Ben-Sasson
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Publication number: 20090311327Abstract: The present, invention provides an oral delivery system for a therapeutic compound that is an acid, a salt of an acid or an unionized compound or a proactive form thereof with pharmacological, physiological or biochemical activity. The present invention particularly provides a swallow formulation comprising a therapeutic compound that is an acid, a salt of an acid or an unionized compound or a proactive form thereof which facilitates the rapid delivery of the therapeutic compound to the circulatory system.Type: ApplicationFiled: November 28, 2006Publication date: December 17, 2009Applicant: IMAGINOT PTY LTDInventors: Michael Stephen Roberts, George Alexander Davidson, Ruoying Jiang, Geraldine Ann Elliott, Keivan Bezanehtak, Stephen Douglas Chandler, Greg Davey, Mantu Sarkar
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Publication number: 20090311235Abstract: Methods of enabling or improving the ability of a hydrogel to swell in the stomach of an animal and/or increasing the amount of time said hydrogel remains swollen in the stomach are described herein. In one embodiment, a polymer is administered in combination with one or more pH modifying agents which raise and maintain the pH of the micro environment of the polymer and/or the stomach in order inducing swelling in the polymer. The polymer can be a homopolymer, a copolymer, or a polymer blend or composite. In one embodiment, the polymer is a superabsorbent polymer (“SAP”). The polymers can also be administered with one or more active agents, such as appetite suppressants. The pH modifying agent and/or the active agent can be administered simultaneously with the polymer in the same dosage form, simultaneously with the polymer in separate dosage forms, or sequentially. The compositions are formulated for oral administration.Type: ApplicationFiled: March 13, 2009Publication date: December 17, 2009Inventors: Eric Elenko, Eyal S. Ron, Yishai Zohar