Chalcogen Bonded Directly To Ring Carbon Of The Oxazole Ring Patents (Class 514/376)
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Publication number: 20120189623Abstract: The present invention relates to new substituted imidazole compounds have the following Formula (I) and to the pharmaceutically acceptable salts, esters, or prodrugs thereof, to compositions of the compounds together with pharmaceutically acceptable carriers, and to uses of the compounds:Type: ApplicationFiled: April 3, 2012Publication date: July 26, 2012Inventors: Rustum Boyce, Eric Martin, Weibo Wang, Hong Yang, Paul A. Barsanti
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Patent number: 8217063Abstract: The present application relates to novel lactam-substituted dicarboxylic acid derivatives, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.Type: GrantFiled: March 15, 2008Date of Patent: July 10, 2012Assignee: Bayer Intellectual Property GmbHInventors: Michael Hahn, Eva-Maria Becker, Andreas Knorr, Dirk Schneider, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Frank Wunder, Dieter Lang
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Publication number: 20120165320Abstract: The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof.Type: ApplicationFiled: June 22, 2010Publication date: June 28, 2012Applicant: PANACEA BIOTEC LTD.Inventors: Rajseh Jain, Sanjay Trehan, Jagattaran Das, Gurmeet Kaur, Sandeep Kanwar, Nishan Singh, Gurmeet Kaur Nanda, Sitaram Kumar Magadi, Sudhir Kumar Sharma
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Patent number: 8202895Abstract: The present application relates to new, substituted 2-acetamido-5-aryl-1,2,4-triazolones, to processes for preparing them, to their use alone or in combinations for the treatment and/or prevention of diseases and also to their use for the production of medicaments for the treatment and/or prevention of diseases, more particularly for the treatment and/or prevention of cardiovascular disorders.Type: GrantFiled: March 18, 2010Date of Patent: June 19, 2012Assignee: Bayer Pharma AktiengesellschaftInventors: Ulf Brüggemeier, Chantal Fürstner, Volker Geiβ, Joerg Keldenich, Armin Kern, Martina Delbeck, Peter Kolkhof, Axel Kretschmer, Elisabeth Pook, Carsten Schmeck, Hubert Trübel
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Publication number: 20120148656Abstract: The present invention provides a sheet-form preparation that can be easily dissolved intraorally, allows the dissolution time thereof to be easily controlled, and can stably contain a drug except an allergenic protein from cedar pollen. The sheet-form preparation contains water, gelatin, and a drug except an allergenic protein from cedar pollen.Type: ApplicationFiled: December 8, 2011Publication date: June 14, 2012Applicant: NITTO DENKO CORPORATIONInventors: Daisuke ASARI, Takuya SHISHIDO, Mitsuhiko HORI, Toshihiko OKAZAKI
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Publication number: 20120148689Abstract: 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 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 17, 2012Publication date: June 14, 2012Inventor: Todd Maibach
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Publication number: 20120149702Abstract: The present invention relates to compounds and pharmaceutical preparations and their use in therapy for preventing or treating trauma, ischemia, stroke and degenerative diseases associated with cell death. Methods and compositions of the invention are particularly useful for treating neurological disorders associated with cellular necrosis.Type: ApplicationFiled: February 21, 2012Publication date: June 14, 2012Applicants: The Brigham and Women's Hospital, Inc., President and Fellows of Harvard CollegeInventors: Gregory D. Cuny, Prakash Jagtap, Junying Yuan, Alexei Degterev
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Publication number: 20120142684Abstract: The disclosure provides compositions and methods for treating a skin blemish. The compositions comprise a therapeutically effective amount of a compound useful for treating skin blemishes such as wounds, scars and wrinkles.Type: ApplicationFiled: November 29, 2011Publication date: June 7, 2012Applicant: ALLERGAN, INC.Inventors: Robert M. Burk, Wha Bin Im, Scott M. Whitcup
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Publication number: 20120136011Abstract: The disclosure provides compositions and methods for treating a skin blemish. The compositions comprise a therapeutically effective amount of a compound useful for treating skin blemishes such as wounds, scars and wrinkles.Type: ApplicationFiled: July 29, 2011Publication date: May 31, 2012Applicant: ALLERGAN, INC.Inventors: Guang L. Jiang, Wha-Bin Im, Frederick C. Beddingfield, Larry A. Wheeler, Scott M. Whitcup, Robert M. Burk
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Publication number: 20120136034Abstract: Compounds of formula I and their metabolites are potent mediators of an inflammatory response: (I) where a, b, c, d, e, f, V, W, X, Y, Ra, Ra?, Rb, Rb?, Rc, and Rc? are defined herein. In particular, the compounds of the invention are candidate therapeutics for treating inflammatory conditions.Type: ApplicationFiled: August 2, 2010Publication date: May 31, 2012Applicant: University of Pittsburgh -Of the Commonwealth SystInventors: Bruce A. Freeman, Francisco J. Schopfer
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Publication number: 20120122940Abstract: The present disclosure relates to lipid compounds of the general formula (I): R1-O—C(R2)(R3)-X??(I) wherein R1 is a C10-C22 alkyl group, a C10-C22 alkenyl group having 1-6 double bonds, or a C10-C22 alkynyl group having 1-6 triple bonds; R2 and R3 are the same or different and may be chosen from different substituents; and X is a carboxylic acid or a derivative thereof, such as a carboxylic ester, a carboxylic anhydride, a phospholipid, triglyceride, or a carboxamide; or a pharmaceutically acceptable salt, solvate, solvate of such salt or a prodrug thereof. The present disclosure also relates to pharmaceutical compositions and lipid compositions comprising at least one compound according to the present disclosure, and to such compounds for use as medicaments or for use in therapy, in particular for the treatment of diseases related to the cardiovascular, metabolic, and inflammatory disease area.Type: ApplicationFiled: May 7, 2010Publication date: May 17, 2012Inventors: Ragnar Hovland, Anne Kristin Holmeide, Tore Skjæret, Morten Brændvang
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Publication number: 20120115916Abstract: The invention relates to oxazole and thiazole derivatives of formula (I), wherein A, E, X, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds.Type: ApplicationFiled: June 11, 2010Publication date: May 10, 2012Applicant: Actelion Pharmaceuticals Ltd.Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
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Publication number: 20120115912Abstract: A method of treating a PPAR? and/or RXR related disease or disorder in a subject includes adminstering to the subject an RXR agonist alone or in combination with a PPAR? agonist.Type: ApplicationFiled: July 12, 2010Publication date: May 10, 2012Inventors: Gary E. Landreth, Paige E. Cramer
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Patent number: 8173649Abstract: A compound represented by the following formula (1): (wherein the carbon atom denoted by * is in the R-configuration; R1 and R2 are each independently a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C1-C6 alkyl group, a C1-C6 alkoxy group, a C1-C6 alkylsulfanyl group, a C1-C6 alkylsulfinyl group or a C1-C6 alkylsulfonyl group; and A is a substituted or unsubstituted heteroaryl group), or a pharmaceutically acceptable salt thereof.Type: GrantFiled: December 21, 2007Date of Patent: May 8, 2012Assignees: Kyorin Pharmaceutical Co., Ltd., Teijin Pharma LimitedInventors: Yasumichi Fukuda, Yoshikazu Asahina, Ayako Nakamura, Kenji Fujita, Tomohiro Ide, Fumiyoshi Kobayashi, Shinji Kobayashi, Kanji Komatsu, Masanori Yamamoto
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Publication number: 20120108570Abstract: The present invention relates generally to pharmacological methods for the prevention of amelioration of sleep-related breathing disorders via administration of agents or combinations of agents that possess serotonin-related pharmacological activity.Type: ApplicationFiled: January 6, 2012Publication date: May 3, 2012Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOISInventors: Miodrag Radulovacki, David W. Carley
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Patent number: 8168664Abstract: Disclosed herein are methods of using metaxalone. In one embodiment, the method comprises determining that a patient in need metaxalone therapy is taking a substance that is a n inhibitor or an inducer of a cytochrome p450 isozyme, wherein the cytochrome P450 is CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, or CYP3A4, and adjusting administration to the patient of metaxalone or the substance to avoid an adverse event associated with metaxalone. In another embodiment, the method comprises informing a user that metaxalone is metabolized by a cytochrome p450 isozyme, wherein the cytochrome P450 is CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, or CYP3A4. Also included are articles of manufacture comprising a container containing a dosage form of metaxalone, wherein the container is associated with published material informing that metaxalone affects activity of a cytochrome p450 isozyme. Also disclosed are a method of treatment and a method of manufacturing a metaxalone product.Type: GrantFiled: May 21, 2010Date of Patent: May 1, 2012Assignee: Mutual Pharmaceutical Company, Inc.Inventors: Richard H. Roberts, Jie Du, Matthew W. Davis
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Patent number: 8168797Abstract: Novel oxazolidinone derivatives with a difluorophenyl moiety, represented by Chemical Formula 1, pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition containing the same as an active ingredient are provided. Exhibiting potent inhibitory activity against Gram-positive bacteria including Haemophilus influenza and Coagulase negative staphylococci and resistant bacteria including vancomycin-resistant enterococci (VRE), the pharmaceutical composition is useful as an antibiotic (wherein, R is as defined in the specification).Type: GrantFiled: November 25, 2008Date of Patent: May 1, 2012Assignee: Korea Institute of Science and TechnologyInventors: Chang Hyun Oh, Jung Hyuck Cho
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Publication number: 20120101111Abstract: The present invention relates to oxazolidinone derivatives of formula (I) wherein Y, R3 and R4 are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as orexin receptor antagonists.Type: ApplicationFiled: May 11, 2010Publication date: April 26, 2012Inventors: Hamed Aissaoui, Christoph Boss, Christine Brotschi, Markus Gude, Romain Siegrist, Thierry Sifferlen, Jodi T. Williams
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Publication number: 20120101078Abstract: Disclosed are a series of neuropeptide Y Y5 receptor ligands, and as such are useful to treat disorders related to mood, stress, ADHD, cognition, stress and dementia.Type: ApplicationFiled: March 19, 2010Publication date: April 26, 2012Applicant: H. Lundbrck A/SInventors: Bin Chen, James Ford Burns, Dario Doller
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Patent number: 8163793Abstract: The invention relates to a compound of formula (I) wherein A, R1-R6 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: GrantFiled: April 16, 2010Date of Patent: April 24, 2012Assignee: Hoffman-La Roche Inc.Inventors: Rubén Alvarez Sánchez, David Banner, Simona M. Ceccarelli, Uwe Grether, Wolfgang Haap, Peter Hartman, Guido Hartmann, Hans Hilpert, Holger Kuehne, Harald Mauser, Jean-Marc Plancher
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Publication number: 20120093928Abstract: The present invention relates to a pharmaceutical composition comprising low-dose metaxalone and one or more pharmaceutically acceptable polymer, as well as methods of preparing them.Type: ApplicationFiled: August 6, 2008Publication date: April 19, 2012Applicant: RANBAXY LABORATORIES LIMITEDInventors: Rajesh S. Shear, Venkateshwaran Rathinasabapathy, Sumit Madan, Vinod Kumar Arora
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Publication number: 20120095003Abstract: Prodrugs of methyl hydrogen fumarate, pharmaceutical compositions comprising prodrugs of methyl hydrogen fumarate, and methods of using prodrugs of methyl hydrogen fumarate and pharmaceutical compositions thereof for treating diseases such as psoriasis, asthma, multiple sclerosis, inflammatory bowel disease, and arthritis are disclosed.Type: ApplicationFiled: October 14, 2011Publication date: April 19, 2012Applicant: XenoPort, Inc.Inventors: Archana Gangakhedkar, Xuedong Dai, Noa Zerangue, Peter A. Virsik
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Publication number: 20120094995Abstract: This invention relates to 2-aza-bicyclo[2.2.1]heptane compounds (and salts thereof), the process for making such a compound and pharmaceutical compositions comprising such a compound. The invention also relates to the use of the compounds for modulating the glycine transporter 1 (GlyT1) and for the treatment of psychosis, cognitive disorders, bipolar disorders, depression disorders, anxiety disorders, post-traumatic stress disorders and pain.Type: ApplicationFiled: January 27, 2010Publication date: April 19, 2012Applicant: ASTRAZENECA ABInventors: Jeffrey Scott Albert, Donald Andisik, Cristobal Alhambra, Todd Andrew Brugel, Glen E Ernst, William Frietze, Lindsay Hinkley, Jeffrey Gilbert Varnes, Xia Wang, Hui Xiong
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Publication number: 20120083500Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, X, Y, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.Type: ApplicationFiled: December 8, 2011Publication date: April 5, 2012Inventors: Li CHEN, Michael Patrick DILLON, Lichun FENG, Minmin YANG
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Patent number: 8148363Abstract: The present invention relates to novel heterocyclic compounds of Formulae I-III; as disclosed herein or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are pharmaceutical compositions comprising said compounds, and methods for using said compounds for treating or preventing a thromboembolic disorder.Type: GrantFiled: May 18, 2009Date of Patent: April 3, 2012Assignee: Schering CorporationInventors: Martin C. Clasby, William J. Greenlee, Yan Xia, Tin-Yau Chan, Mariappan V. Chelliah, Samuel Chackalamannil, Haiyan Pu, Keith A. Eagen, Henry Vaccaro, Brian A. McKittrick, Liyuan Wang, Xiaobang Gao
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Patent number: 8148414Abstract: Prodrugs of methyl hydrogen fumarate, pharmaceutical compositions comprising prodrugs of methyl hydrogen fumarate, and methods of using prodrugs of methyl hydrogen fumarate and pharmaceutical compositions thereof for treating diseases such as psoriasis, asthma, multiple sclerosis, inflammatory bowel disease, and arthritis are disclosed.Type: GrantFiled: August 19, 2009Date of Patent: April 3, 2012Assignee: XenoPort, Inc.Inventors: Archana Gangakhedkar, Xuedong Dai, Noa Zerangue, Peter A. Virsik
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Publication number: 20120071510Abstract: A method for treating migraines is disclosed. The method utilizes a rapid drug delivery system which prevents deactivation or degradation of the active agent, including small molecules and peptides being administered to a patient in need of treatment. In particular, the drug delivery system is designed for inhalation for delivery of drugs to the pulmonary circulation in a rapid and therapeutically effective manner.Type: ApplicationFiled: November 9, 2011Publication date: March 22, 2012Applicant: MANNKIND CORPORATIONInventors: Andrea Leone-Bay, Grayson W. Stowell, Joseph J. Guarneri, Dawn M. Carlson, Marshall Grant, Chad C. Smutney
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Patent number: 8133889Abstract: Compounds of formula (I): wherein: m and n represent 1 or 2, A represents a pyrrolyl group, X represents a C(O), S(O) or SO2 group, R1 and R2 represent an alkyl group or, together with the nitrogen atom carrying them, form a heterocyclic group, R3 and R4, together with the atoms carrying them, form a heterocyclic group, R5 represents a hydrogen atom or an alkyl group, R6 represents a hydrogen atom or a halogen atom. Medicinal products containing the same which are useful in treating cancer.Type: GrantFiled: August 4, 2010Date of Patent: March 13, 2012Assignee: Les Laboratoires ServierInventors: Jean-Claude Ortuno, Alexis Cordi, Jean-Michel Lacoste, Vincent Lacoste, legal representative, Pauline Lacoste, legal representative, Imre Fejes, Michael Burbridge, John Hickman, Alain Pierre
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Patent number: 8129369Abstract: The present invention discloses novel compounds of the Formula (1), comprising benzothiazinone, benzoxazinone or benzoxazolinone moieties having antifungal activity, method for preparing these compounds and the use of these compounds as antifungal agents in prevention and treatment of fungal infections, and pharmaceutical preparations containing these novel compounds.Type: GrantFiled: October 16, 2009Date of Patent: March 6, 2012Assignees: Council of Scientific & Industrial Research;, FDC Ltd.Inventors: Hanumant Bapurao Borate, Suleman Riyasaheb Maujan, Sangmeshwer Prabhakar Sawargave, Ramesh Ganesh Kelkar, Radhika Dilip Wakharkar, Mohan Anand Chandavarkar, Sharangi Ravinda Vaiude, Vinay Anant Joshi
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Patent number: 8129378Abstract: The invention relates to the field of blood coagulation. Novel oxazolidinone derivatives of the general formula (I) processes for their preparation and their use as medicinally active compounds for the prophylaxis and/or treatment of disorders are described.Type: GrantFiled: June 30, 2009Date of Patent: March 6, 2012Assignee: Bayer Pharma AktiengesellschaftInventors: Alexander Straub, Thomas Lampe, Jens Pohlmann, Susanne Röhrig, Elisabeth Perzborn, Karl-Heinz Schlemmer, Joseph Pernerstorfer
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Patent number: 8124633Abstract: The present invention is directed to certain hydroxymethyl ether hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, LUTS, depression, and anxiety.Type: GrantFiled: April 7, 2008Date of Patent: February 28, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Robert J. DeVita, Sander G. Mills, Jinlong Jiang, Andrew J. Kassick, Jianming Bao
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Publication number: 20120046287Abstract: Compounds of formula (I): wherein: m and n represent 1 or 2, A represents a pyrrolyl group, X represents a C(O), S(O) or SO2 group, R1 and R2 represent an alkyl group or, together with the nitrogen atom carrying them, form a heterocyclic group, R3 and R4, together with the atoms carrying them, form a heterocyclic group, R5 represents a hydrogen atom or an alkyl group, R6 represents a hydrogen atom or a halogen atom. Medicinal products containing the same which are useful in treating cancer.Type: ApplicationFiled: November 2, 2011Publication date: February 23, 2012Applicant: LES LABORATOIRES SERVIERInventors: Jean-Claude Ortuno, Alexis Cordi, Jean-Michel Lacoste, Vincent Lacoste, Pauline Lacoste, Imre Fejes
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Patent number: 8119669Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: GrantFiled: March 6, 2008Date of Patent: February 21, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Michael Gaul, Lily Lee Searle, Dionisios Rentzeperis
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Patent number: 8114914Abstract: Vasoconstrictors are administered topically to provide protection against the adverse effects, e.g., alopecia, mucositis or dermatitis, induced by chemotherapy or radiotherapy. Appropriate dosages and formulations of topical vasoconstrictors are provided. Methods for the use of such compositions are also provided.Type: GrantFiled: June 19, 2006Date of Patent: February 14, 2012Assignee: Wisconsin Alumni Research FoundationInventors: William E. Fahl, Arnold E. Ruoho, Minesh Mehta
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Publication number: 20120035124Abstract: The present invention is directed to the use of nifuratel, or a physiologically acceptable salt thereof, to treat' infections caused by Atopobium species. The invention is further directed to the use of nifuratel to treat bacteriuria, urinary tract infections, infections of external genitalia in both sexes, as well as bacterial vaginosis, or mixed vaginal infections in women, when one or more species of the genus Atopobium are among the causative pathogens of those infections.Type: ApplicationFiled: April 19, 2010Publication date: February 9, 2012Applicant: POLICHEM SAInventor: Federico Mailland
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Publication number: 20120010200Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.Type: ApplicationFiled: September 22, 2011Publication date: January 12, 2012Inventors: Jiacheng Zhou, Ashoke Bhattacharjee, Shili Chen, Yi Chen, Jay J. Farmer, Joel A. Goldberg, Roger Hanselmann, Rongliang Lou, Alia Orbin, Adegboyega K. Oyelere, Joseph M. Salvino, Dane M. Springer, Jennifer Tran, Deping Wang, Yusheng Wu
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Publication number: 20120004272Abstract: Provided are compositions comprising 2,6-dimethyl-m-dioxane-4-ol acetate and a biocidal compound selected from the group consisting of: a biocidal oxazolidine; 1-(3-chloroallyl)-3,5,7-triaza-1-azoniaadamantane; and tris(hydroxymethyl)-nitromethane. The compositions are useful for controlling microorganisms in aqueous or water containing systems.Type: ApplicationFiled: March 26, 2009Publication date: January 5, 2012Inventors: Kathy J. Ji, Donald J. Love, Jon B. Raymond
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Publication number: 20110319398Abstract: The disclosure relates to compounds and methods of inhibiting type three secretion system effector molecules, to methods of detecting compounds that inhibit Yops translocation, and to methods of treating or preventing infections by administering compounds described herein to a subject in need thereof.Type: ApplicationFiled: June 1, 2011Publication date: December 29, 2011Applicant: TUFTS UNIVERSITYInventor: Joan Mecsas
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Publication number: 20110319359Abstract: Compounds exhibiting calcium receptor antagonist activity that are safe and orally administrable having Formula (I) or pharmaceutically acceptable salts thereof:Type: ApplicationFiled: June 23, 2011Publication date: December 29, 2011Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Akira Nakao, Kentoku Gotanda, Kazumasa Aoki, Shimpei Hirano, Yoshiharu Hiruma, Takeshi Shiiki
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Publication number: 20110318321Abstract: The present invention relates to a controlled release pharmaceutical or food formulation comprising at least one active pharmaceutical or food ingredient dispersed in a mixture of a glycogen with a polysaccharide, and the process for its preparation. The invention also relates to a slow release system represented by a mixture of a glycogen with a polysaccharide, and its use for the preparation of slow release pharmaceutical or food formulations.Type: ApplicationFiled: January 8, 2010Publication date: December 29, 2011Applicant: AZIENDE CHIM.RIUN.ANG.FRANC.A.C.R.A.F. S.p.A.Inventors: Stefano Selva, Leonardo Marchitto, Giovanni Battista Ciottoli, Lorella Ragni, Vincenzo Russo, Elisa Liberati
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Publication number: 20110312967Abstract: This invention provides for certain bridged and fused compounds of the formula G-L-A I or a pharmaceutically acceptable salt, ester of solvate thereof wherein: A is: (I) and the other variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.Type: ApplicationFiled: January 21, 2010Publication date: December 22, 2011Applicant: Schering CorporationInventors: Hubert B. Josien, John W. Clader, William J. Greenlee, Michael John Mayer, Jason L. Davis, Shuangyi Wan
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Publication number: 20110305640Abstract: Soluble adenylyl cyclase (sAC) is implicated in proliferation of keratinocytes. Inhibitors of sAC are useful for the treatment and/or prevention of psoriasis and other hyperproliferative skin disorders. Assays to identify such compounds are also described.Type: ApplicationFiled: February 23, 2010Publication date: December 15, 2011Applicant: CORNELL UNIVERSITYInventors: Jochen Buck, Lonny Levin, Jonathan Zippin
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Publication number: 20110294813Abstract: Disclosed is a compound which is useful as an 11?-hydroxysteroid dehydrogenase type 1 inhibitor. A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein R1 is optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted heterocycle or optionally substituted heterocyclealkyl, X is —O—, —NR3—, —NR3C(?O)— or —NR3S(?O)2—, R2 is optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl, R3 is hydrogen or optionally substituted alkyl.Type: ApplicationFiled: June 30, 2011Publication date: December 1, 2011Applicants: SHIONOGI & CO., LTD., INSTITUTE OF MEDICINAL MOLECULAR DESIGN, INC.Inventors: Akiko Itai, Susumu Muto, Ryuko Tokuyama, Hiroshi Fukasawa, Takeshi Yanase
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Publication number: 20110294840Abstract: There is provided a hydrazide compound having a controlling effect on pests represented by the formula (1): wherein, G is a 5-membered heterocyclic group, M is an oxygen atom or a sulfur atom, Q1, Q2, Q3 and Q4 is independently a nitrogen atom, etc., m is an integer of 0 to 5, R2 is an optionally halogenated C1-C6 alkyl group, etc., R5 and R6 are independently an optionally substituted C1-C12 chain hydrocarbon group, etc., and R4 is an optionally substituted C1-C12 chain hydrocarbon group, etc.Type: ApplicationFiled: February 5, 2010Publication date: December 1, 2011Inventors: Hideki Ihara, Koji Kumamoto
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Publication number: 20110293673Abstract: The present invention provides a film-form base having one or more sugars or sugar alcohols dispersed as fine particles therein, and also provides a film-form preparation containing the base and a drug. The base is produced by dispersing, in an organic solvent having a solubility parameter of 9.7 or higher, an edible polymer soluble in water and the organic solvent, and particles of one or two or more compounds selected from the group consisting of mono- to hexasaccharide sugars and sugar alcohols thereof which have an average particle size of 0.1 ?m to 60 ?m and are insoluble in an organic solvent. The present invention can therefore provide oral film-form base and preparation which have a rapid dissolution profile in the mouth and sufficient film strength, and provide a reduced sticky sensation attributed to the water-soluble polymer in the mouth and an improved feel when handled with the fingers.Type: ApplicationFiled: March 6, 2009Publication date: December 1, 2011Applicant: NITTO DENKO CORPORATIONInventors: Daisuke Asari, Mitsuhiko Hori, Keiko Ogawa
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Publication number: 20110294857Abstract: There is provided an inhibitor that inhibits casein kinase 1? and casein kinase 1?, and thus, there is also provided a pharmaceutical agent useful for the treatment and/or prevention of a disease, with the pathological condition of which the mechanism of activation of casein kinase 1? or casein kinase 1? is associated. Particularly, the above-described inhibitor is used to provide a pharmaceutical agent useful for the treatment of circadian rhythm disorder (including sleep disorder), central neurodegenerative disease, and cancer.Type: ApplicationFiled: December 28, 2009Publication date: December 1, 2011Applicants: NB HEALTH LABORATORY CO. LTD., PHARMADESIGN, INC.Inventors: Masako Okamoto, Kiyoshi Takayama
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Publication number: 20110288080Abstract: The invention is directed to the synthesis and use of nitrofuran compounds, especially Nifurtimox, as medicaments to treat cancer, especially neuroblastoma, and to inhibit angiogenesis. The invention also provides compositions, unit dosage forms, and kits comprising the compounds.Type: ApplicationFiled: March 7, 2007Publication date: November 24, 2011Inventors: Giselle L Saulnier Sholler, Narasimha Swamy, Henna Swamy, Satyan Kalkunte, Rakesh K. Singh, Laurent Brard, Kyu Kwang Kim
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Publication number: 20110288138Abstract: Silicon dioxide free orally disintegrating tablet formulations of zolmitriptan or a pharmaceutically acceptable salt thereof having magnesium carbonate heavy and sodium stearyl fumarate with one or more pharmaceutically acceptable excipients and a process for preparing such a formulation and its use in the treatment of migraines.Type: ApplicationFiled: May 20, 2011Publication date: November 24, 2011Applicant: Sanovel llac Sanayi Ve Ticaret Anonim SirketiInventors: Umit Cifter, Ali Turkyilmaz, Gulay Yelken
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Patent number: 8048901Abstract: The invention relates to 1,3-substituted cycloalkyl derivatives having acidic, mostly heterocyclic groups and to their physiologically acceptable salts and physiologically functional derivatives. What is described are compounds of the formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparation. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved.Type: GrantFiled: July 10, 2007Date of Patent: November 1, 2011Assignee: Aventis Pharma Deutschland GmbHInventors: Jochen Goerlitzer, Heiner Glombik, Eugen Falk, Dirk Gretzke, Stefanie Keil, Hans-Ludwig Schaefer, Christian Stapper, Wolfgang Wendler
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Publication number: 20110257228Abstract: The present disclosure relates to aqueous liquid pharmaceutical compositions comprising a) at least one triptan compound, pharmaceutically acceptable salts or hydrates thereof, and b) xylitol.Type: ApplicationFiled: December 15, 2009Publication date: October 20, 2011Inventors: Begoña Duarte Lopez, Pere Guiro Coll, Antoni Masso Carbonell