Plural Six-membered Hetero Rings Consisting Of One Nitrogen And Five Carbon Atoms Patents (Class 514/332)
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Patent number: 8946263Abstract: The present invention relates to a modulator of glucocorticoid biosynthesis, degradation and/or receptor activation for use in preventing or treating symptoms and/or diseases associated with jet lag. The compositions of the invention may be used as a lead compound for developing a drug for preventing or treating symptoms and/or diseases associated with jet lag. The invention relates to the discovery that administration of the modulator(s) to a subject results in a directional change of the time point of maximum amounts of glucocorticoids in the subject as compared to the time point of maximum amounts of glucocorticoids in a subject not treated with the modulator(s).Type: GrantFiled: March 7, 2012Date of Patent: February 3, 2015Assignee: Max-Planck-Gesellchaft zur Forderung der Wissenschaften E.V.Inventors: Gregor Eichele, Henrik Oster, Silke Kiessling
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Patent number: 8940324Abstract: The invention relates to octenidine or a pharmaceutical salt thereof, in particular octenidine dihydrochloride, which is intended for mutual therapeutic administration of the octenidine in solution with a polyalcohol of formula 1: (H—C—OH)a(HO—C—OH)b(H—C—H)c, where a, b, c are whole numbers, where a+b is at least 2, preferably at least 3, c is selected from 0, 1 or a number from 2 to a+b, optionally in addition to one or more aldehyde groups provided that they form (cyclic) acetals with one of the hydroxy groups or one or more keto groups optionally as acetal with one of the hydroxy groups, optionally in addition to one or more carboxylic acid groups if the polyalcohol is a cyclic acetal or acetal, preferably with ring sizes of 5 to 7 atoms, or a polymer, polyether or polyester thereof, provided that the polyalcohol exists as a polymer, polyether or polyester with at least two units of formula 1 if a+b is 2 or 3.Type: GrantFiled: November 13, 2009Date of Patent: January 27, 2015Assignee: Artan Holding AGInventor: Ahmet Melih Aydinoglu
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Publication number: 20150023950Abstract: The present invention relates to 2,6-diaminopyridine compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system.Type: ApplicationFiled: September 30, 2014Publication date: January 22, 2015Inventors: Heiko Kroth, Wolfgang Froestl, Andrea Pfeifer, Andreas Muhs
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Publication number: 20150018321Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.Type: ApplicationFiled: September 25, 2014Publication date: January 15, 2015Applicant: Chiesi Farmaceutici S.p.A.Inventors: Maurizio DELCANALE, Elisabetta ARMANI, Gabriele AMARI
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Patent number: 8933104Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.Type: GrantFiled: July 18, 2014Date of Patent: January 13, 2015Assignee: Pfizer Inc.Inventors: Gary Erik Aspnes, Mary Theresa Didiuk, Kevin James Filipski, Angel Guzman-Perez, Jeffrey Allen Pfefferkorn, Benjamin Dawson Stevens, Meihua Mike Tu
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Patent number: 8933103Abstract: Novel compounds or salts thereof, or crystals thereof, which inhibit Axl and are useful for treating diseases caused by Axl hyperfunction, diseases associated with Axl hyperfunction and/or diseases accompanied by Axl hyperfunction are provided. Pyridone derivatives represented by the formula (1) having various substituents or salts thereof, or crystals thereof (where R1, R2, R3, R5, R6, A, W, X and n in the formula (1) are as defined in the specification, respectively) are provided.Type: GrantFiled: January 30, 2013Date of Patent: January 13, 2015Assignee: Daiichi Sankyo Company, LimitedInventors: Hitoshi Ohki, Masahiro Ota, Kosuke Takeuchi, Hideaki Watanabe, Akitake Yamaguchi, Yoshihiro Shibata, Yuichi Tominaga, Takeshi Jimbo, Keijiro Kobayashi, Katsuhiro Kobayashi, Daisuke Fukatsu
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Publication number: 20150011494Abstract: Curcumin analogues and methods are provided for treatment of disease.Type: ApplicationFiled: August 1, 2014Publication date: January 8, 2015Inventors: David L. Vander Jagt, Lorraine M. Deck, Steve F. Abcouwer, Robert A. Orlando, Robert E. Royer, Waylon M. Weber, Ekaterina V. Bobrovnikova-Marjon, Lucy A. Hunsaker
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Patent number: 8927580Abstract: The present invention relates to dipyridyl thiosemicarbazone compounds of formula (I): wherein R1 is cyclohexyl or ethyl; as well as pharmaceutical compositions containing those compounds, and the use of those compounds and compositions in the treatment of cancer.Type: GrantFiled: December 16, 2011Date of Patent: January 6, 2015Assignee: Oncochel Therapeutics LLCInventors: Des R. Richardson, David B. Lovejoy
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Publication number: 20150005308Abstract: The invention relates to novel heteroarylamide derivatives having formula (I) and N-oxides, stereoisomers and pharmaceutically acceptable salts thereof, where RA, RB, R1 1, R?, R?, z and X are as defined in the claims. The arylamide derivatives of formula (I) have antiandrogenic properties. The invention also relates to compounds of formula (I) for use as a medicament and to pharmaceutical compositions comprising them and to their preparation.Type: ApplicationFiled: January 11, 2013Publication date: January 1, 2015Inventors: Jari Ratilainen, Milla Koistinaho, Anu Muona
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Patent number: 8921370Abstract: The present invention provides bicyclo[3.2.1]octyl amide derivatives of formula (I): wherein L, R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.Type: GrantFiled: December 22, 2011Date of Patent: December 30, 2014Assignee: H. Lundbeck A/SInventors: Guiying Li, Hao Zhou, Jesse Weiss, Dario Doller, James Ford Burns
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Patent number: 8916590Abstract: The present invention relates to 2,6-diaminopyridine compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system.Type: GrantFiled: October 15, 2010Date of Patent: December 23, 2014Assignee: AC Immune SAInventors: Heiko Kroth, Wolfgang Froestl, Andrea Pfeifer, Andreas Muhs
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Patent number: 8916589Abstract: The present invention relates to compounds of general formula I wherein n, R1, R2, R3, R4, R5, R6, R7 and R8 are defined as stated hereinafter, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable properties, the preparation thereof, the pharmaceutical compositions containing the pharmacologically effective compounds, the preparation thereof and the use thereof.Type: GrantFiled: August 28, 2008Date of Patent: December 23, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Norbert Hauel, Angelo Ceci, Enzo Cereda, Henri Doods, Ingo Konetzki, Juergen Mack, Henning Priepke, Annette Schuler-Metz, Rainer Walter
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Publication number: 20140370067Abstract: The invention relates to means and methods for the disinfection of an insertion channel to prevent in particular catheter sepsis, which significantly reduces the carry-over of germs even out of deeper skin layers by means of medical instruments, such as catheters, to be introduced into non-natural openings and also permits the decontamination of perioperatively contaminated medical instruments. The disinfection of the insertion channel is achieved by means of a method for the perioperative coating of a medical instrument to be inserted into an invasively produced bodily opening before use, comprising the application of a preferably viscous or foam-like composition containing at least one anti-infective compound, preferably a gel having octenidine, by means of an applicator, such that when said gel is used, the composition is also specifically effective in the first millimeters of the insertion channel. Furthermore, an immediate disinfecting action is provided over the entire coated surface.Type: ApplicationFiled: January 22, 2013Publication date: December 18, 2014Inventors: Stefan Margraf, Jan Stange
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Mono Quaternary Ammonium Salts and Methods for Modulating Neuronal Nicotinic Acetylcholine Receptors
Publication number: 20140371266Abstract: Provided are monoquaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse, and gastrointestinal tract disorders.Type: ApplicationFiled: August 27, 2014Publication date: December 18, 2014Inventors: Peter CROOKS, Linda P. DWOSKIN, Guangrong ZHENG, Sangeetha SUMITHRAN, Zhenfa ZHENG -
Patent number: 8912184Abstract: The invention relates to methods of treating diseases, particularly cancers, that respond favorably to the inhibition of Nicotinamide phosphoribosyltransferase (Nampt); it also relates to therapeutic methods that utilize Nampt inhibitors in combination with NAD biosynthesis precursors to intentionally kill cancer cells while limiting or minimizing toxicity to normal host cells; and it relates to methods of identifying cancers that will be most responsive to treatment with Nampt inhibitors, particularly when administered in combination with nicotinic acid.Type: GrantFiled: September 16, 2011Date of Patent: December 16, 2014Assignee: Alzheimer's Institute of America, Inc.Inventors: Tracey C. Fleischer, Daniel M. Cimbora, Jeffrey S. Flick, Andrew D. Gassman, Vijay R. Baichwal, Damon I. Papac
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Patent number: 8906408Abstract: The invention relates to octenidine or a pharmaceutical salt thereof, in particular octenidine dihydrochloride, which is intended for mutual therapeutic administration of the octenidine in solution with a polyalcohol of formula 1: (H—C—OH)a(HO—C—OH)b(H—C—H)c, where a, b, c are whole numbers, where a+b is at least 2, preferably at least 3, c is selected from 0, 1 or a number from 2 to a+b, optionally in addition to one or more aldehyde groups provided that they form (cyclic) acetals with one of the hydroxy groups or one or more keto groups optionally as acetal with one of the hydroxy groups, optionally in addition to one or more carboxylic acid groups if the polyalcohol is a cyclic acetal or acetal, preferably with ring sizes of 5 to 7 atoms, or a polymer, polyether or polyester thereof, provided that the polyalcohol exists as a polymer, polyether or polyester with at least two units of formula 1 if a+b is 2 or 3.Type: GrantFiled: November 13, 2009Date of Patent: December 9, 2014Assignee: Artan Holding AGInventor: Ahmet Melih Aydinoglu
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Publication number: 20140350030Abstract: The present invention provides compounds of formula (I): where R1, R2, X, Y and n are as described herein, and pharmaceutical compositions, uses and methods comprising same.Type: ApplicationFiled: September 17, 2012Publication date: November 27, 2014Inventors: Dario Doller, Guiying Li
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Publication number: 20140350055Abstract: The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases.Type: ApplicationFiled: August 31, 2012Publication date: November 27, 2014Applicant: Amakem NVInventors: Jo Alen, Sandro Boland, Arnaud Pierre Jean Bourin, Olivier Defert, Dirk Leysen
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Publication number: 20140348880Abstract: A method for treating or preventing a microbial infection in a subject in need thereof, the method comprising administering to the subject, a therapeutically effective amount of a compound of Formula Ia, a compound of Formula IIa, one or more compounds of Formula Ia or Formula IIa complexed with a metal core, or a pharmaceutically acceptable salt, prodrug or hydrate thereof.Type: ApplicationFiled: May 23, 2014Publication date: November 27, 2014Inventors: Matthias Bierenstiel, Harshiny Muthukumar
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Patent number: 8895585Abstract: An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. The present invention provides a nicotinamide derivative represented by the following formula (I) (wherein R1 represents a halogen atom; R2 represents a C1-12 alkyl group, a C2-12 alkenyl group, a C2-12 alkynyl group, a C3-8 cycloalkyl group, an aryl group, an ar-C1-6 alkyl group or a heterocyclic group, each optionally having at least one substituent; R3 represents an aryl group or a heterocyclic group each optionally having at least one substituent; and R4 and R5 each independently represent a hydrogen atom; and R2 and R4 may form a cyclic amino group optionally having at least one substituent together with the nitrogen atom to which they bind) or a salt thereof, and a pharmaceutical composition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.Type: GrantFiled: December 28, 2012Date of Patent: November 25, 2014Assignee: FUJIFILM CorporationInventors: Hideyasu Fujiwara, Kimihiko Sato, Shinsuke Mizumoto, Yuichiro Sato, Hideki Kurihara, Yohei Kubo, Hiyoku Nakata, Yasutaka Baba, Takashi Tamura, Hidenobu Kuniyoshi, Shinji Hagiwara, Mari Yamamoto
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Publication number: 20140343102Abstract: The present invention relates to novel crystalline forms of (4-{4-[5-(6-Trifluoromethyl-pyridin-3-ylamino)-pyridin-2-yl]-phenyl}-cyclohexyl)-acetic acid, sodium and their use in the treatment or prevention of a condition or a disorder associated with DGAT1 activity in animals, particularly humans. It also relates processes for making such novel crystalline forms.Type: ApplicationFiled: July 31, 2014Publication date: November 20, 2014Inventors: Paul Allen Sutton, Michael J. Girgis, Jessica Liang, Mahavir Prashad, Edwin Bernard Villhauer
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Publication number: 20140343101Abstract: Disclosed are methods and compositions for modulating the function of transcription factors, especially transcription factors that recruit epigenetic regulators (histone modifying enzymes) to specific DNA promoters. The targeted transcription factors include but are not limited to the myocyte enhancing factor (MEF2), the forkhead/winged helix transcription factor FOXP3 and the transcription factor GATA3.Type: ApplicationFiled: February 26, 2014Publication date: November 20, 2014Applicant: UNIVERSITY OF SOUTHERN CALIFORNIAInventors: Lin Chen, Nimanthi Jayathilaka, Aidong Han, Nicos A. Petasis
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Publication number: 20140341969Abstract: The invention relates to a sterile wound dressing having a backing and a nonabsorbent elastomer wound contact layer, wherein the elastomer matrix is formed by a synthetic three-block elastomer, preferably a copolymer of polystyrene block and polyolefin block (SEPS, SEBS, SEEPS, etc.) or mixtures thereof, wherein the total polymer content is less than 3.2 wt %, in particular 3.0 wt % or less, preferably 2.6 wt % or less, and is plasticized by an apolar oil and/or petroleum jelly.Type: ApplicationFiled: July 31, 2014Publication date: November 20, 2014Applicant: LOHMANN & RAUSCHER GMBH & CO. KGInventor: MARIUS-THOMAS GORKA
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Publication number: 20140329862Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.Type: ApplicationFiled: July 18, 2014Publication date: November 6, 2014Applicant: Pfizer Inc.Inventors: Gary Erik Aspnes, Mary Theresa Didiuk, Kevin James Filipski, Angel Guzman-Perez, Jeffrey Allen Pfefferkorn, Benjamin Dawson Stevens, Meihua Mike Tu
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Publication number: 20140323486Abstract: The present invention provides a compound of the following formula, racemates, enantiomers and salts thereof. Also provided is the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.Type: ApplicationFiled: December 21, 2012Publication date: October 30, 2014Inventors: Edward Malcolm Tyndall, Lloyd George Czaplewski, Colin William Gordon Fishwick, Andrew Ian Yule, Jeffrey Peter Mitchell, Kelly Helen Anderson, Gary Robert William Pitt
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Publication number: 20140315839Abstract: Provided is a pest control composition containing a novel iminopyridine derivative and other pest control agents. Provided is a pest control composition containing an iminopyridine derivative represented by the following Formula (I) and at least one of other pest control agents: [in the formula (I), Ar represents a 5- to 6-membered heterocycle which may be substituted, A represents a heterocycle having a 5- to 10-membered unsaturated bond including one or more nitrogen atoms, and has an imino group substituted with an R group at a position adjacent to the nitrogen atom present on the cycle, Y represents hydrogen, halogen and the like, and R represents any one of groups represented by the following Formulae (a) to (e), (y) or (z)].Type: ApplicationFiled: July 1, 2014Publication date: October 23, 2014Applicant: MEIJI SEIKA PHARMA CO., LTD.Inventors: Ryo HORIKOSHI, Yasumichi ONOZAKI, Satoshi NAKAMURA, Masahiro NOMURA, Makoto MATSUMURA, Masaaki MITOMI
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Publication number: 20140315893Abstract: The invention provides 1,4-dihydropyridine derivatives of formula (I) wherein R1 is optionally substituted C6-24aryl group or 5 to 6 membered heteroaryl group comprising 1 to 3 nitrogen atoms or other heteroatoms like oxygen and sulphur, and combinations thereof; R2 and R3 are independently hydrogen or C1-6alkyl group; R4 and R5 are independently hydrogen, C1-6alkyl group optionally substituted with amino, mono- or di(C1-6alkyl)amino, or with 5 to 24 membered optionally fused heterocyclic ring attached by nitrogen and optionally comprising additional 1 to 3 N, O, S heteroatoms and optionally substituted with C1-6alkyl group or C1-6 alkoxy group; R6 is C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-6alkyl or arylC1-6alkyl group; and stereoisomers including enantiomers, diastereomers, racemic mixtures, mixture of enantiomers and combination thereof, as well as polymorphs, pharmaceutically acceptable salts, solvates, esters and prodrugs thereof for use in the therapeutic or prophylactic treatment of a disorder mediType: ApplicationFiled: November 22, 2012Publication date: October 23, 2014Inventors: Ferenc Fülöp, László Vígh, Zsolt Török, Botond Penke, Ibolya Horváth, Gábor Balogh, Sándor Bernáth, Ákos Hunya
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Publication number: 20140309244Abstract: The present invention provides compounds of formula (I) wherein R1, R2, A, X, D1, D2 and Y3 are as defined in the claims. The invention further provides intermediates used in the preparation of these compounds, to compositions which comprise these compounds and to their use in agriculture or horticulture for controlling or preventing infestation of plants by phytopathogenic microorganisms, preferably fungi.Type: ApplicationFiled: September 23, 2011Publication date: October 16, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Werner Zambach, Daniel Stierli, Kurt Nebel, Andrea Bortolato, Clara Massol
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Publication number: 20140303206Abstract: The invention provides certain 3-pyridyl carboxamide-containing compounds of the Formula (I) (I) or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.Type: ApplicationFiled: October 1, 2012Publication date: October 9, 2014Inventors: Michael D. Altman, Kaleen Konrad Childers, Anthony Donofrio, John Michael Ellis, Sandra Lee Knowles, Alan B. Northrup
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Publication number: 20140296067Abstract: A compound of formula (I) wherein R1 to R4 are, for example, each hydrogen, R5 is pyridyl, which has two or more substituents selected, for example, from halogen, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, and cyano; R6 is, for example, hydrogen; R7 is, for example, hydrogen, cyano, hydroxyl, formyl, C1-C4-alkyl, C1-C4-alkoxy, C2-C4-alkenyl, or C2-C4-alkynyl; and A1 to A5 are, independently selected, from, for example, N, and C—H; and its use as a pesticidal agent.Type: ApplicationFiled: October 31, 2012Publication date: October 2, 2014Applicants: SYNGENTA PARTICIPATIONS AG, University of ExeterInventors: Thomas Pitterna, Olivier Loiseleur, Paul Anthony Worthington, Anthony Cornelius O'Sullivan, Torsten Luksch, Vladimir Bobosik
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Patent number: 8846932Abstract: Disclosed are methods and compositions for modulating the function of transcription factors, especially transcription factors that recruit epigenetic regulators (histone modifying enzymes) to specific DNA promoters. The targeted transcription factors include but are not limited to the myocyte enhancing factor (MEF2), the forkhead/winged helix transcription factor FOXP3 and the transcription factor GATA3. Also disclosed are small molecule modulators of MEF2 and its associated factors that include but not limited to histone deacetylases (HDACs), p300/CBP and Cabin1 and the therapeutic applications thereof.Type: GrantFiled: March 13, 2013Date of Patent: September 30, 2014Assignee: University of Southern CaliforniaInventors: Lin Chen, Nimanthi Jayathilaka, Aidong Han, Nicos A. Petasis
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Patent number: 8841457Abstract: The present invention describes a process for preparing a cyclooxygenase-2 selective inhibitor. It provides a synthetic procedure for the said substance namely 5-chloro-3-(4-methylsulphonyl)phenyl-2-(2-methyl-5-pyridinyl)pyridine of formula (I). The invention also relates to preparation of a new intermediate of formula (IV) and a process to prepare it. Furthermore, the invention describes a process for preparing another key intermediate of formula (II). Compounds of formula (IV) and formula (II) are useful intermediates in synthesis of the said cyclooxygenase-2 inhibitor.Type: GrantFiled: November 15, 2011Date of Patent: September 23, 2014Assignee: Virdev Intermediates Pvt. Ltd.Inventors: Dharmesh Mahendra Shah, Sanjay Amratlal Solanki, Viral Narendra Jariwala, Ashok Vasantray Vyas, Ashokkumar Bhikhubhai Mistry
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Patent number: 8841326Abstract: Curcumin analogs and methods are provided for treatment of disease.Type: GrantFiled: June 29, 2006Date of Patent: September 23, 2014Assignee: STC.UNMInventors: David L. Vander Jagt, Lorraine M Deck, Steve F. Abcouwer, Robert A. Orlando, Robert E. Royer, Waylon M. Weber, Ekaterina V. Bobrovnikova-Marjon, Lucy A. Hunsaker
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Publication number: 20140261454Abstract: An antiseptic solution including, a cationic antiseptic agent, a film forming polymer, an anionic tinting agent, and a solvent, wherein the cationic antiseptic agent, the film forming polymer and the anionic tinting agent each remain solubilized within the solution for greater than about 1 hour at 25° C. and 60% relative humidity. The antiseptic agent is preferably octenidine dihydrochloride or chlorhexadine gluconate. The film forming polymer is preferably an acrylate polymer. The solvent is preferably ethanol, isopropanol, and n-propanol. When a drape is adhered to a dried surgical film via the antiseptic solution, the force required to peel the drape from the surgical film is at least about 105 g/25 mm.Type: ApplicationFiled: March 15, 2013Publication date: September 18, 2014Applicant: CAREFUSION 2200, INC.Inventors: Kenneth M. DOKKEN, Tenoch BENITEZ, James BARDWELL
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Publication number: 20140256728Abstract: The present invention relates to the use of predominantly known pyridyl carboxamide derivatives as nematicides, compositions containing such compounds and methods for the control of nematodes.Type: ApplicationFiled: October 29, 2012Publication date: September 11, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Jörg Nico Greul, Heiko Rieck, Christian Paulitz, Matthias Riedrich, Ralf Dunkel, Arianna Martelletti, Alexander Sudau, Peter Lösel, Olga Malsam, Arnd Voerste, Hans-Georg Schwarz, Ulrich Görgens, Kerstin Ilg, Michael Maue, Pierre-Yves Coqueron, Philippe Desbordes, Philippe Meresse, Stephanie Gary, Pierre Cristau, David Bernier
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Patent number: 8829194Abstract: The present invention relates to novel crystalline forms of (4-{4-[5-(6-Trifluoromethyl-pyridin-3-ylamino)-pyridin-2-yl]-phenyl}-cyclohexyl)-acetic acid, sodium and their use in the treatment or prevention of a condition or a disorder associated with DGAT1 activity in animals, particularly humans. It also relates to processes for making such novel crystalline forms.Type: GrantFiled: October 5, 2011Date of Patent: September 9, 2014Assignee: Novartis AGInventors: Paul Allen Sutton, Michael J. Girgis, Jessica Liang, Mahavir Prashad, Edwin Bernard Villhauer
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Publication number: 20140249135Abstract: New compounds, compositions and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.Type: ApplicationFiled: May 9, 2014Publication date: September 4, 2014Applicant: NOVARTIS AGInventors: Matthew Burger, Mika Lindvall, Wooseok Han, Jiong Lan, Gisele Nishiguchi, Cynthia Shafer, Cornelia Bellamacina, Kay Huh, Gordana Atallah, Christopher McBride, William Antonios-McCrea, JR., Tatiana Zavorotinskaya, Annette Walter, Pablo Dominguez Garcia
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Publication number: 20140248236Abstract: The disclosure provides methods of use of certain compounds that are useful for treating certain symptoms of endocrine disturbances, and in particular those associated with hot flashes.Type: ApplicationFiled: November 7, 2012Publication date: September 4, 2014Inventors: Michael G. Natchus, Richard Arrendale
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Publication number: 20140243336Abstract: The invention provides certain 2-pyridyl carboxamide-containing compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.Type: ApplicationFiled: October 1, 2012Publication date: August 28, 2014Inventors: Michael D. Altman, Corey E. Bienstock, John W. Butcher, Kaleen Konrad Childers, Maria Emilia Di Francesco, Anthony Donofrio, John Michael Ellis, Christian Fischer, Andrew M. Haidle, James P. Jewell, Sandra Lee Knowles, Alan B. Northrup, Ryan D. Otte, Scott L. Peterson, Graham Frank Smith
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Patent number: 8815912Abstract: The invention relates to an antimicrobially effective composition which comprises a) 0.001 to 1% by weight of bispyridiniumalkane, b) humectant and c) water. The composition has an osmolality of from 230 to 350 mOsmol/kg and is free from surfactant. It is used as wound and mucosa antiseptic.Type: GrantFiled: October 14, 2010Date of Patent: August 26, 2014Assignee: L'Air Liquide Société Anonyme pour l'Etude et l'Exploitation des Procédés Georges ClaudeInventors: Boris Baur, Sabine Behrends, Jörg Siebert, Andreas Dettmann, Mona Golombiewski
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Publication number: 20140235671Abstract: Compounds of the invention are of the formula wherein: is a double bond and X is C; or is a single bond and X is N, CH or CQR1; and wherein: n is 1 to 10; R is H or QR1; each R? is independently selected from H and QR1; each Q is independently selected from a bond, CO, NH, S, SO, SO2 or O; each R1 is independently selected from C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, substituted or unsubstituted aryl or heteroaryl, acyl, C1-C10 cycloalkyl, halogen, C1-C10 alkylaryl or C1-C10 heterocycloalkyl; L is a nitrogen-containing heteroaryl; and W is a zinc-chelating residue; or a pharmaceutically acceptable salt thereof. The compounds are useful in therapy.Type: ApplicationFiled: April 30, 2014Publication date: August 21, 2014Applicant: Karus Therapeutics LimitedInventors: Stephen Joseph SHUTTLEWORTH, Cyrille Davy TOMASSI
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Publication number: 20140235652Abstract: The present application provides novel pyridine compounds and pharmaceutically acceptable salts or prodrugs thereof. Also provided are methods for preparing these compounds. These compounds are useful in inhibiting CYP17 activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with CPY17 activity. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer, such as prostate cancer.Type: ApplicationFiled: November 13, 2013Publication date: August 21, 2014Applicant: Endo Pharmaceuticals Inc.Inventors: Roger A. Smith, Nicholas James Laping, Aranapakam M. Venkatesan, Raghava Reddy Kethiri, Chandregowda Venkateshappa, Bheemashankar Kulkarni, Purushottam Dewang, Rajendra Kristam, Rajesh Devraj
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Publication number: 20140235642Abstract: Compounds of Formula I are useful as antagonists of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.Type: ApplicationFiled: April 28, 2014Publication date: August 21, 2014Applicant: AMGEN INC.Inventors: James Brown, Jian J. Chen, Vijay Keshav Gore, Scott Harried, Daniel B. Horne, Matthew R. Kaller, Qingyian Liu, Holger Monenschein, Thomas T. Nguyen, Nobuko Nishimura, Wenge Zhong
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Patent number: 8809371Abstract: An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. The present invention provides a nicotinamide derivative represented by the following formula (I) (wherein R1 represents a halogen atom; R2 represents a C1-12 alkyl group, a C2-12 alkenyl group, a C2-12 alkynyl group, a C3-8 cycloalkyl group, an aryl group, an ar-C1-6 alkyl group or a heterocyclic group, each optionally having at least one substituent; R3 represents an aryl group or a heterocyclic group each optionally having at least one substituent; and R4 and R5 each independently represent a hydrogen atom; and R2 and R4 may form a cyclic amino group optionally having at least one substituent together with the nitrogen atom to which they bind) or a salt thereof, and a pharmaceutical composition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.Type: GrantFiled: December 28, 2012Date of Patent: August 19, 2014Assignee: FUJIFILM CorporationInventors: Hideyasu Fujiwara, Kimihiko Sato, Shinsuke Mizumoto, Yuichiro Sato, Hideki Kurihara, Yohei Kubo, Hiyoku Nakata, Yasutaka Baba, Takashi Tamura, Hidenobu Kuniyoshi, Shinji Hagiwara, Mari Yamamoto
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Patent number: 8809342Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.Type: GrantFiled: December 22, 2011Date of Patent: August 19, 2014Assignee: Pfizer Inc.Inventors: Gary Erik Aspnes, Mary Theresa Didiuk, Kevin James Filipski, Angel Guzman-Perez, Jeffrey Allen Pfefferkorn, Benjamin Dawson Stevens, Meihua Mike Tu
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Publication number: 20140228407Abstract: The invention provides a novel tetra-pyridine compound and a composition containing this compound for protecting and preserving cells, tissues and organs against ischemia-reperfusion injury. A method and use of the tetra-pyridine compound for preventing or treating ischemia-reperfusion injury or for protecting and preserving excorporeal tissue or organ from ischemia and oxygen radical-related damage are also provided.Type: ApplicationFiled: June 27, 2012Publication date: August 14, 2014Applicants: YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY, LTD., ATHENA CARDIONET LTD.Inventors: Jerachmiel Y. Appelbaum, Edit Tshuva Goldberg
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Publication number: 20140228363Abstract: The present invention provides a compound of formula (I): as further described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula I, and pharmaceutical compositions comprising such compounds.Type: ApplicationFiled: April 22, 2014Publication date: August 14, 2014Applicant: NOVARTIS AGInventors: Matthew Burger, Yu Ding, Wooseok Han, Gisele Nishiguchi, Alice Rico, Robert Lowell Simons, Aaron R. Smith, Victoriano Tamez, JR., Huw Tanner, Lifeng Wan
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Publication number: 20140228408Abstract: The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and respiratory diseases.Type: ApplicationFiled: August 31, 2012Publication date: August 14, 2014Applicant: AMAKEM NVInventors: Jo Alen, Sandro Boland, Arnaud Pierre, Jean Bourin, Olivier Defert, Dirk Leysen
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Publication number: 20140221429Abstract: The invention provides that heterocyclic Schiff bases posses protein antiglycation potential in hyperglycemia. The novel antiglycation agents 3-6 showed a moderate to potent antiglycation activity.Type: ApplicationFiled: February 4, 2013Publication date: August 7, 2014Inventors: Saud Ibrahim Al-Resayes, Ismail Warad, Mohammed A. Al-Nuri, Muhammad Iqbal Choudhary, Atia-tul Wahab, Saima Rasheed
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Publication number: 20140221334Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: ApplicationFiled: April 10, 2014Publication date: August 7, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Juan-Miguel Jimenez, Guy William Bemis, Francois Maltais, Tiansheng Wang, Ronald Marcellus Alphonsus Knegtel, Christopher John Davis, Damien Fraysse, Dean Boyall, Luca Settimo, Stephen Young, Michael Paul Mortimore