Polycyclo Ring System Having The Additional Oxygen Hetero Ring As One Of The Cyclos Patents (Class 514/254.11)
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Publication number: 20110287083Abstract: Bioabsorbable compositions of A) blends of bioabsorbable homopolymers and/or copolymers containing glycolide and lactide and B) salts of fatty acids and/or fatty acid esters are described. Processes for making the compositions and surgical articles made totally or in part therefrom, including suture coatings, are also described.Type: ApplicationFiled: July 21, 2011Publication date: November 24, 2011Applicant: Tyco Healthcare Group LPInventor: Ahmad R. Hadba
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Publication number: 20110280824Abstract: The present disclosure provides copolymers including a first monomer including at least one phospholipid possessing at least one vinyl group and a second monomer including a furanone possessing vinyl and/or acrylate groups. Compositions, medical devices, and coatings including such copolymers are also provided.Type: ApplicationFiled: July 26, 2011Publication date: November 17, 2011Applicant: Tyco Healthcare Group LPInventor: Joshua B. Stopek
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Publication number: 20110281811Abstract: The invention relates to the use of at least one leukotriene inhibitor for preparing a pharmaceutical composition for the prophylaxis and/or treatment of lung diseases, more particularly of bronchopulmonary dysplasia, in prematurely born infants. The invention further relates to a pharmaceutical composition for the prophylaxis and/or treatment of lung diseases, more particularly of bronchopulmonary dysplasia, in prematurely born infants, the pharmaceutical composition comprising at least one leukotriene inhibitor. The invention additionally relates to a method for the treatment and/or prophylaxis of a lung disease, more particularly of a bronchopulmonary dysplasia, in a prematurely born infant, where the prematurely born infant is administered a pharmacologically active amount of at least one leukotriene inhibitor.Type: ApplicationFiled: November 12, 2009Publication date: November 17, 2011Inventor: Sabine Rupprecht
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Publication number: 20110281890Abstract: Compounds of general formula (I) in which R1, m, X, n, Y and R3 have any of the meanings given in the specification, have affinity for sigma receptors and are useful in the treatment of disorders of the central nervous system.Type: ApplicationFiled: July 25, 2011Publication date: November 17, 2011Inventor: Connie L. Sun
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Publication number: 20110280921Abstract: The present invention relates to hydrogels endowed with antibacterial properties, to be used for injection in damaged bones or in the production of antibacterial coatings of prostheses for implant in the human or animal body, obtained by loading with antibacterial agents hydrogels formed by derivatives of hyaluronic acid; the invention also relates to a kit of parts for producing the antibacterial hydrogels.Type: ApplicationFiled: January 29, 2010Publication date: November 17, 2011Applicants: NOVAGENIT S.R.L., MERO S.R.LInventors: Gaetano Giammona, Giovanna Pitarresi, Fabio Palumbo, Carlo Luca Romano, Enzo Meani, Edgardo Cremascoli
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Publication number: 20110269775Abstract: Compounds of general formula (I) in which R1 and R0 have any of the meanings given in the specification have affinity for sigma receptors and are useful in the treatment of disorders of the central nervous system.Type: ApplicationFiled: July 12, 2011Publication date: November 3, 2011Inventor: Connie L. Sun
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Publication number: 20110262352Abstract: Compounds of formula (I), wherein X, Z, A, B, D, E, R1-R4 and m are as defined in the claims, exhibit alpha2C antagonistic activity and are thus useful as alpha2 antagonists.Type: ApplicationFiled: November 20, 2009Publication date: October 27, 2011Inventors: David Din Belle, Patrik Holm, Arto Tolvanen, Gerd Wohlfahrt
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Patent number: 8044057Abstract: Disclosed herein are methods for suppressing an immune response in a subject, treating a neoplasm in a subject, or treating a fibroproliferative vascular disease in a subject, that includes administering to the subject a therapeutically effective amount of a 2-(4-piperazinyl)-substituted 4H-1-benzopyran-4-one compound, or a pharmaceutically acceptable salt thereof, having the structure of wherein the presence of each of R1 and R2 is optional and R1 and R2 are each independently selected from alkyl, substituted alkyl, heteroalkyl, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, substituted heterocycloalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, alkoxy, halogen, hydroxy, or amino.Type: GrantFiled: December 9, 2004Date of Patent: October 25, 2011Assignee: The United States of America as represented by the Secretary of the Department of Health and Human ServicesInventors: Joel Moss, Arnold Kristof
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Patent number: 8017617Abstract: The invention relates to compounds of formula I: or a pharmaceutically acceptable salt thereof, where R1-3, R5, R7, a, b, Q, X, X?, X?, Y, Z, and Ar are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also relates to pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.Type: GrantFiled: December 12, 2008Date of Patent: September 13, 2011Assignee: Theravance, Inc.Inventors: YuHua Ji, Craig Husfeld, Rick Lee, YongQi Mu
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Publication number: 20110217335Abstract: Disclosed are macrocyclic compounds of formulae I, I?, II, II?, III, III?, IV, and V, which are analogs of the pochonin resorcylic acid lactones, pharmaceutical compositions comprising the compounds, and methods and uses comprising the compounds for the treatment of diseases mediated by kinases and Heat Shock Protein 90 HSP90.Type: ApplicationFiled: January 15, 2009Publication date: September 8, 2011Applicant: UNIVERSITE DE STRASBOURGInventors: Nicolas Winssinger, Sofia Barluenga, Martin Karplus
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Publication number: 20110212090Abstract: A method for the repair of a unit, by specific diagnosis of the undesired state, and its appropriate repair, using said specific diagnosis as a means to repair in an appropriate way said unit. The diagnosis and repair processes may involve chemical, physical, or mechanical means. The units being diagnosed and repaired include live matter (e.g. human beings, animals, plants) as well as non-live matter (e.g. buildings, electronic equipment, polymer materials).Type: ApplicationFiled: July 22, 2009Publication date: September 1, 2011Inventors: Henrik Pedersen, Liselotte Brix
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Patent number: 8008302Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof, in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.Type: GrantFiled: July 25, 2005Date of Patent: August 30, 2011Assignee: Merck Serono SAInventors: Dominique Swinnen, Agnes Bombrun, Jerome Gonzalez, Stefano Crosignani, Patrick Gerber, Catherine Jorand-Lebrun
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Publication number: 20110207729Abstract: An object of the present invention is to provide a novel and excellent agent for treating or preventing dementia, schizophrenia, and the like, based on the serotonin 5-HT5A receptor modulating action. It was confirmed that a bicyclic acylguanidine derivative which has a characteristic structure that guanidine is bonded to one ring of a bicyclic structure such as chromene and dihydronaphthalene through a carbonyl group and a cyclic group is bonded on the other ring, has a potent 5-HT5A receptor modulating action and an excellent pharmacological action based on this mechanism. The present invention is useful as an excellent agent for treating or preventing dementia, schizophrenia, bipolar disorder, or attention deficit hyperactivity disorder.Type: ApplicationFiled: August 7, 2008Publication date: August 25, 2011Applicant: ASTELLAS PHARMA INC.Inventors: Isao Kinoyama, Satoshi Miyamoto, Takehiro Miyazaki, Yohei Koganemaru, Yuichiro Kawamoto, Nobuyuki Shiraishi, Hiroaki Hoshii, Akio Kuroda, Mayako Yamazaki, Minoru Yasuda, Hiroaki Mizuno
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Publication number: 20110201583Abstract: The invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein R1-3, R5-7, a, X, Y, Y?, Y?, and Z are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.Type: ApplicationFiled: April 28, 2011Publication date: August 18, 2011Applicant: THERAVANCE, INC.Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
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Publication number: 20110195963Abstract: There is provided a novel carbamoyloxy arylalkanoyl arylpiperazine derivative compound having abundant racemic or enantiomeric characteristics, represented by the Formula 1, and pharmaceutically available salts or hydrates thereof. Also, there are provided a pharmaceutical composition for treating pain, anxiety or depression including an effective amount of the compound, and a method for treating pain, anxiety or depression in mammals by administering an effective amount of the compound to the mammals in need of treatment thereof.Type: ApplicationFiled: April 30, 2008Publication date: August 11, 2011Inventors: Byong Sung Kwak, Hong Sik Moon, Han Ju Yi, Young Soon Kang, Dae Joong Im, Eun Hee Chae, Sang Mi Chae, Ki Ho Lee
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Publication number: 20110195958Abstract: Disclosed are pyruvate kinase M2 activators, which are bis sulfonamide piperazinyl and piperidinyl compounds of Formula (I), 2,4-disubstituted 4H-thieno[3,2-c]pyrrole-2-(substituted benzyl)pyridazin-3(2H)-ones of Formula (II) and 6-(3,4-dimethylphenylaminosulfonyl)-3,4-dihydro-1H-quinolin-2-one of formula (III), wherein L, R1, R2, R11 to R16, R21 and R22 are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer and anemia.Type: ApplicationFiled: October 9, 2009Publication date: August 11, 2011Applicant: US Dept. of Health and Human ServicesInventors: Craig J. Thomas, Douglas S. Auld, James Inglese, Amanda P. Skoumbourdis, Jian-Kang Jiang, Matthew B. Boxer
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Publication number: 20110189256Abstract: Anti-infective articles capable of preventing infection associated with implantation of medical devices include low levels of anti-infective agents, may cover only a fraction of the portion of the medical device and be effective, or may rapidly elute anti-infective agent, without sustained elution, and still be effective.Type: ApplicationFiled: April 11, 2011Publication date: August 4, 2011Applicant: MEDTRONIC, INC.Inventors: Thomas C. Bischoff, William V. Ferris, JR.
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Publication number: 20110183995Abstract: This invention relates to the use of the drug Eltoprazine for combating dyskinesias arising from chronic Levodopa (L-DOPA) therapy in patients suffering from Parkinson's disease.Type: ApplicationFiled: June 23, 2009Publication date: July 28, 2011Applicant: Neurosearch A/SInventors: Anders Björklund, Munolo Carta, Jørgen Buus Lassen
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Publication number: 20110172225Abstract: Novel derivatives of enfumafungin are disclosed herein, along with their, pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antifungal agents and/or inhibitors of (1,3)-?-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.Type: ApplicationFiled: September 25, 2008Publication date: July 14, 2011Applicants: Merck Sharp & Dohme Corp., Scynexis, Inc.Inventors: James M. Balkovec, Phieng Siliphaivanh, Frances A. Bouffard, Roland A. Bouffard, Michael R. Peel, Weiming Fan, Ahmed Mamai, Sarah Dimick Gray
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Publication number: 20110171195Abstract: Methods and compositions are provided for treating a urinary tract infection (UTI). The methods involve administering to a subject in need thereof a cAMP elevator or agent that mimics cAMP, particularly a labdane diterpene such as forskolin or a derivative or analog thereof in a therapeutically effective amount to treat a UTI. The methods may further include administration of at least one cAMP elevator in combination with one or more additional active compounds from other classes of therapeutic agents, such as antimicrobial agents or cholesterol lowering drugs. Compositions of the invention include pharmaceutical compositions and kits for treating a UTI in a subject in need thereof that include therapeutically effective amounts of at least two cAMP elevators, particularly where one of the cAMP elevators is a labdane diterpene such as forskolin or a derivative or analog thereof.Type: ApplicationFiled: June 12, 2008Publication date: July 14, 2011Applicant: Duke UniversityInventors: Soman N. Abraham, Brian L. Bishop, Matthew J. Duncan, K. Ranga Rama Krishnan, Jeongmin Song, Guojie Li, David A. Zaas
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Publication number: 20110172244Abstract: The invention provides compounds, of Formula I: pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.Type: ApplicationFiled: February 20, 2009Publication date: July 14, 2011Applicant: IRM LLCInventors: Phillip B. Alper, Robert Epple, Pierre-Yves Michellys, Daniel Mutnick, Victor Nikulin
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Publication number: 20110165225Abstract: Drag derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drag derivatized with a weak-base moiety that facilitates active loading of the drag through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drag to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drag derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drags.Type: ApplicationFiled: May 26, 2009Publication date: July 7, 2011Inventors: Peter Cullis, Marcel Bally
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Publication number: 20110165259Abstract: [Problem to be Solved] The purpose of present invention is to provide a medicine which has low contamination with a fine-pulverizing medium, is safe and has improved bioavailability. [Solution] A method for producing a composite organic compound powder for medical use is used which comprises: mixing a poorly water-soluble and crystalline organic compound powder, a physiologically acceptable salt, a physiologically acceptable polyol, and a carboxyvinyl polymer and fine-pulverizing the organic compound powder; and removing at least the salt and the polyol during or after fine-pulverizing.Type: ApplicationFiled: September 15, 2009Publication date: July 7, 2011Applicant: ACTIVUS PHARMA CO., LTD.Inventors: Takashi Hirokawa, Takahiro Tada, Jun Nihira
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Patent number: 7973039Abstract: The present invention is related to derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.Type: GrantFiled: December 19, 2005Date of Patent: July 5, 2011Assignee: Merck Serono SAInventors: Dominique Swinnen, Agnes Bombrun, Patrick Gerber, Catherine Jorand-Lebrun
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Patent number: 7968538Abstract: The invention relates to 5-HT6 receptor antagonists. Novel arylamine compounds and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with serotonin action, such as in treating obesity, and obesity-related disorders, e.g., cardiovascular disease, digestive disease, respiratory disease, cancer and type II diabetes; and psychological disorders such as schizophrenia, are disclosed.Type: GrantFiled: January 25, 2006Date of Patent: June 28, 2011Assignee: Galenea Corp.Inventors: Oren Becker, Rosa Melendez, Yael Marantz, Anurag Sharadendu, Merav Fichman, Mercedes Lobera, Hanoch Senderowitz, Srinivasa Rao Cheruku, Silvia Noiman, Xiang Y. Yu, Sharon Shacham, Laurence Wu, Ashis Saha, Pini Orbach, Dale S. Dhanoa
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Publication number: 20110152289Abstract: The present invention relates to dimeric derivatives of 10-trifluoromethylated artemisinin of formula (I) below: Formula (I) and the pharmaceutically acceptable salts thereof, and also to the preparation method thereof and to the uses thereof, especially in the treatment of cancer.Type: ApplicationFiled: July 29, 2009Publication date: June 23, 2011Applicants: PIERRE FABRE MEDICAMENT, UNIVERSITE PARIS-SUDInventors: Jean-Pierre Begue, Daniele Bonnet-Delpon, Benoit Crousse, Anais Fournial, Celine Mordant, Jacques Fahy
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Publication number: 20110144094Abstract: This invention concerns novel substituted heterocyclic tetracyclic tetrahydrofuran derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.Type: ApplicationFiled: February 16, 2011Publication date: June 16, 2011Inventors: José Maria Cid-Núñez, Antonius Adrianus Hendrikus Petrus Megens, Andrés Avelino Trabanco-Suárez
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Patent number: 7960385Abstract: The invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein R1-3, R5-7, a, X, Y, Y?, Y?, and Z are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.Type: GrantFiled: September 5, 2008Date of Patent: June 14, 2011Assignee: Theravance, Inc.Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
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Publication number: 20110118272Abstract: Novel 3?-deoxy-3?-acylaminospectinomycin compounds are described. Also described are methods of using the 3?-deoxy-3-acylaminospectinomycin compounds and other spectinomycin analogs in treating tuberculosis and in treating microbial infections.Type: ApplicationFiled: July 26, 2010Publication date: May 19, 2011Inventors: Richard E. Lee, Jianjun Qi, Juilian G. Hurdle, Bernd Meibohm, Vnr Pavan Kumar Vaddady, Rakesh, Jiuyu Liu
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Publication number: 20110112090Abstract: A Compound of structure (IX) or (X) or a pharmaceutically acceptable salt thereof, wherein: X is —C(?O)N(R10)— or —CH(OPr3)—; R7, R9 and R10 are the same or different and represent hydrogen or an amino acid side chain moiety from either a natural or an unnatural amino acid; Pr1 and Pr2 are the same or different and represent hydrogen or a thiol protecting group; Pr3 is hydrogen or an alcohol protecting group; R1, R2, R5 and R6 are the same or different and represent hydrogen or an amino acid side chain moiety from either a natural or an unnatural amino acid, or R1 and R2 and/or R5 and R6, taken together with the carbon atom to which they are attached, form a spirocyclic moiety, with the proviso that: each of R1 and R2 is not hydrogen, or each of R5 and R6 is not hydrogen.Type: ApplicationFiled: May 22, 2009Publication date: May 12, 2011Inventors: Stephen Joseph Shuttleworth, Franck Alexandre Silva, Cyrille Davy Tomassi, Alexander Richard Liam Cecil, Thomas James Hill
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Publication number: 20110105475Abstract: The present invention relates to compounds of formula (I) wherein the substituents are as defined in the claims, including pharmaceutical compositions thereof and for their use in the treatment and/or prevention and/or amelioration of one or more symptoms of disease or disorders related to the activity of FXR. The invention is also directed to intermediates and to a method of preparation of compounds of formula (I).Type: ApplicationFiled: March 30, 2009Publication date: May 5, 2011Applicant: MERXCK PATENT GESELLSCHAFTInventors: Didier Roche, Giséle Mautino, Ingo Kober, Francis Contard, Serge Christmann-Franck, Saumitra Sengupta, Ramesh Sistla, Gummadi Venkateshwar Rao
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Patent number: 7935705Abstract: Compounds of the formula: where X and Y are each independently H, halo, or C1-C6 straight or branched chain substituted or unsubstituted alkyl.Type: GrantFiled: August 12, 2010Date of Patent: May 3, 2011Assignee: Medtronic, Inc.Inventor: William V. Ferris, Jr.
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Patent number: 7928138Abstract: The invention is the discovery of an actinomycete genus, given the name Salinospora gen. nov., that displays an obligate requirement of seawater (Na+) for growth and unique 16S rRNA signature nucleotides. The invention is also the use of the genus for the production and discovery of active biomolecules such as pharmaceutical agents, agrichemicals, immunomodifiers, enzymes and enzyme inhibitors.Type: GrantFiled: December 28, 2007Date of Patent: April 19, 2011Assignee: Regents of the University of CaliforniaInventors: Robert H. R. Feling, William Fenical, Paul R. Jensen, Tracy J. Mincer
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Publication number: 20110086863Abstract: The present invention relates to novel benzenesulfonanilide compounds of the formulae I and I? and physiologically tolerated acid addition salts and the N-oxides thereof. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT6 receptor. wherein R1 is hydrogen or methyl R2 is hydrogen or methyl R3 hydrogen, fluorine C1-C2 alkoxy or fluorinated C1-C2 alkoxy; R4 is hydrogen, C1-C4 alkyl or fluorinated C1-C4 alkyl; R5 is hydrogen, fluorine, C1-C2 alkyl, fluorinated C1-C2 alkyl, C1-C2 alkoxy or fluorinated C1-C2 alkoxy; and R6 is hydrogen, fluorine and chlorine.Type: ApplicationFiled: August 5, 2010Publication date: April 14, 2011Applicants: Abbott GmbH & Co. KG, Abbott LaboratoriesInventors: Wilfried Martin Braje, Sean Colm Turner, Andreas Haupt, Udo Lange, Karla Drescher, Karsten Wicke, Liliane Unger, Mario Mezler, Wolfgang Wernet, Matthias Mayrer, Ana Jongen-Relo, Anton Bespalov, Min Zhang
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Patent number: 7910135Abstract: The present invention relates to a method of forming shape-retentive and shape-conforming aggregate wound dressings and biomaterials composed of gel nanoparticles and wound or bodily fluid in which the aggregates are held together by non-covalent bond physical forces such as, without limitation, hydrophobic-hydrophilic interactions and hydrogen bonds. The method comprises introducing a dry powder of gel nanoparticles to a wound site in which the nanoparticles absorb some of the blood or wound exudate and coalesce in situ into the claimed shape-retentive aggregate dressing. The method also comprises introducing the dry nanoparticle powder in or on a wet bodily tissue in vivo to form the claimed shape-retentive biomaterial. In addition, the method also comprises incorporating biomedical agents to produce medicated aggregate dressings or biomaterials for a variety of medical applications. This invention also relates to uses of the method of formation of the shape-retentive aggregates of gel nanoparticles.Type: GrantFiled: October 13, 2006Date of Patent: March 22, 2011Assignee: ULURU Inc.Inventors: John St. John, Daniel G. Moro
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Publication number: 20110065689Abstract: The invention includes a compound of formula I: wherein R1, X, Z, n, and m have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of PDE4 function and are useful for improving cognitive function in animals.Type: ApplicationFiled: September 1, 2010Publication date: March 17, 2011Inventors: Terence P. Keenan, Alan P. Kaplan
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Publication number: 20110065723Abstract: The present invention relates to compositions of N-benzyl-3-(4-chlorophenyl)-2-[methyl-[2-oxo-2-(3,4,5-trimethoxyphenyl)acetyl]amino]-N-[3-(4-pyridyl)-1-[2-(4-pyridyl)ethyl]propyl]propanamide (Timcodar) useful for the treatment of patients with mycobacterium infections such as Mycobacterium tuberculosis. The invention also provides methods of treating patients with tuberculosis.Type: ApplicationFiled: September 10, 2010Publication date: March 17, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Trudy H. Grossman, Christopher Locher
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Publication number: 20110059913Abstract: The present invention relates to identification of Oroxylum indicum, Indian medicinal plant as a rich source for flavanoid compounds. Mucoprotective and antigastric ulcer properties in the flavone class of compounds isolated therefrom have been identified along with a flavanoids mixture in substantial yields from hexane and acetone extracts. The hexane extract was fractionated, purified and the compounds identified as Oroxylin A, Chrysin and Baicalein. The acetone extract was purified and the compounds obtained identified as methoxy chrysin, Oroxyloside methyl ester and chrysin-7-O-methyl glycoside.Type: ApplicationFiled: November 12, 2010Publication date: March 10, 2011Applicant: COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCHInventors: Janaswamy Madusudana RAO, Suresh Babu KATRAGADDA, Hari Babu TATIPAKA, Manjulatha KHANAPUR, Muralidhar Gurachar PUROHIT, Venkata Srinivas PULLELA, Jhillu Singh YADAV
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Publication number: 20110059960Abstract: The invention is directed to a method of treating severe neutropenia, and in particular, cyclic neutropenia (CN) or severe congenital neutropenia (SCN), in a patient in need of such treatment comprising: administering a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: September 5, 2008Publication date: March 10, 2011Inventors: David C. Dale, Paul E. Finke, Richard A. Munford, Andranik Andrew Aprikyan
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Publication number: 20110053956Abstract: Methods for treating neurological or mental disorders in humans and the symptoms associated therewith are provided by administering eltoprazine and/or related compounds. In some embodiments, specific symptoms are treated by administering eltoprazine and/or a related compound in an effective amount to ameliorate the symptoms. Of particular significance are symptoms that are associated with cognitive dysfunction where eltoprazine will improve the symptoms and the disorder associated with that symptom. Of particular interest are non-ADHD-associated inattention, hyperactivity and impulsiveness. The methods provided herein are especially useful for improving functional recovery after CNS injury such as stroke where improved cognitive function will facilitate the acquisition of learning and memory of rehabilitative tasks.Type: ApplicationFiled: November 9, 2010Publication date: March 3, 2011Applicant: Psychogenics, Inc.Inventors: Emer Leahy, Mark Day
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Publication number: 20110046142Abstract: Methods for identifying prodrug antibiotic compounds and direct inhibitory antibiotic compounds utilizing various screens are provided. Also provided are methods for treating infections using these compounds.Type: ApplicationFiled: June 11, 2008Publication date: February 24, 2011Applicant: Northeastern UniversityInventors: Kim Lewis, Gabriele Casadei
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Publication number: 20110033550Abstract: The invention provides a process for the production of nanoparticle carriers for drug delivery, said nanoparticles being produced by preparing a double emulsion of water-oil-water including one or more polymer which forms the basis of the nanoparticle carrier, blending the drug to be delivered into one of the emulsion phases, doping either the oil-phase or the outer-water phase with a carbohydrate, and spray drying the emulsion to form nanoparticles of a narrow particle size distribution of 100 nm to 1000 nm, which nanoparticles are substantially spherical.Type: ApplicationFiled: August 17, 2010Publication date: February 10, 2011Applicant: CSIRInventor: Lonji Kalombo
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Publication number: 20110015185Abstract: The present invention relates to compounds of formula (I): wherein P, R3, W1, and W2 are as described herein, to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds for the preparation of a medicament against 5-HT6 receptor-related disorders.Type: ApplicationFiled: September 28, 2010Publication date: January 20, 2011Applicant: BIOVITRUM ABInventors: Gary Johansson, Peter Brandt, Björn M. Nilsson
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Publication number: 20110008425Abstract: A method for treating Attention Deficit/Hyperactivity Disorder (ADHD) in humans and the symptoms associated therewith, inattentiveness, and hyperactivity with impulsivity, using eltoprazine and related compounds is provided.Type: ApplicationFiled: September 20, 2010Publication date: January 13, 2011Applicant: Psychogenics, Inc.Inventors: Daniela Brunner, Daniel W. Goodman
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Publication number: 20110009396Abstract: The present invention provides compounds represented by formula 1: wherein, R1 R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13 and X are as defined in the specification, in all its stereoisomeric and tautomeric forms and mixtures thereof in all ratios, and its pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable polymorphs and prodrugs. These compounds are useful for treatment of inflammatory disorders including those caused by elevated levels of proinflammatory cytokines such as Tumor Necrosis Factor (TNF-? and/or interleukins (IL-1?, IL-6, IL-8). The invention also relates to processes for the manufacture of compounds of formula 1 and pharmaceutical compositions containing them.Type: ApplicationFiled: July 25, 2008Publication date: January 13, 2011Inventors: Dilip Narayanrao Bhedi, Ram Asrey Vishwakarma, Vaishali Deka, Dattatray Maruti More, Manivannan Ramalingam, Ashish Suthar, Rada Dalal, Sapna Parikh, Aditi Amol Tannu
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Publication number: 20110003776Abstract: This invention relates to tetrahydropyranonaphthyridines derivatives having formula (III) or IV: and analogues of the tetrahydropyranonaphthyridines derivatives. The invention also relates to pharmaceutical compositions comprising these compounds and methods for treatment of tuberculosis using these compounds.Type: ApplicationFiled: June 3, 2010Publication date: January 6, 2011Applicant: TRUSTEES OF BOSTON UNIVERSITYInventors: John K. Snyder, John A. Porco, JR., Ya Zhou
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Publication number: 20110003830Abstract: The invention relates to a novel process for the preparation of 3-amino-8-(1-piperazinyl)-2H-1-benzopyran-2-one, a broad spectrum 5-HT receptor binding ligand having potent 5-HT1A-agonistic as well as 5-HT1D-antagonistic activity. The invention also relates to novel salts and solvates, in particular hydrates of salts of said compound, as well as to their use as medicaments.Type: ApplicationFiled: July 2, 2010Publication date: January 6, 2011Applicant: Solvay Pharmaceuticals B.V.Inventor: Cornelis BAKKER
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TETRACYCLIC DIPYRANO-COUMARIN COMPOUNDS WITH ANTI-HIV AND ANTI-MYCOBACTERIUM TUBERCULOSIS ACTIVITIES
Publication number: 20100324067Abstract: The present invention relates to tetracyclodipyrano-coumarin compounds of general formula (I), wherein the substituents are defined herein. These compounds exihibit dual biological activities of anti human immunodeficiency virus type 1 (HIV-1) infection and anti-Mycobacterium Tuberculosis (TB) infection.Type: ApplicationFiled: November 5, 2007Publication date: December 23, 2010Inventors: Gang Liu, Hai Xue, Tao Ma, Ziwei Chen, Lin Wang -
Publication number: 20100324026Abstract: Compounds of formula 1: are disclosed, wherein V is CH2; W is S(O)m; m is the integer 0, 1 or 2; U is O, C(O), CR13R14 or NR15; where R13 is H, alkyl; R14 is H, OH, OR13 or OCOR13; R15 is H, alkyl, cycloalkyl, alkenyl, C(O)R13, C(O)OR13 or alkylaminocarbonyl; R1, R2, R3, R4, R5, R6, R7 and R5 are as defined herein. These compounds are inhibitors of tumor necrosis factor-alpha (TNF-?) and are useful as medicaments for the treatment and prevention of disorders caused by increased TNF-? activity, in particular inflammations.Type: ApplicationFiled: August 11, 2010Publication date: December 23, 2010Applicant: Piramal Life Sciences LimitedInventors: Bansi LAL, Somesh Sharma, Usha Ghosh, Swati Bal-Tembe, Tulsidas More, Pravin Gagare, Sunil Jadhav, Shashikant Patil, Asha Kulkarni-Almeida, Sapna Parikh, Radha Panicker, Anagha Damre, Ravindra Gupte
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Patent number: 7855200Abstract: The present invention relates to methods of using Oroxylum indicum as a rich source for flavanoid compounds having mucoprotective and antigastric ulcer properties, and containing Oroxylin A, Chrysin and Baicalein.Type: GrantFiled: January 9, 2007Date of Patent: December 21, 2010Assignee: Council of Scientific and Industrial ResearchInventors: Janaswamy Madusudana Rao, Suresh Babu Katragadda, Hari Babu Tatipaka, Manjulatha Khanapur, Muralidhar Gurachar Purohit, Venkata Srinivas Pullela, Jhillu Singh Yadav