Pyrazoles Patents (Class 514/406)
-
Publication number: 20150087682Abstract: The present invention provides a method for treating scleroderma by administering a therapeutically effective amount of a toll like receptor 4 inhibitor to a subject in need of such a treatment.Type: ApplicationFiled: April 17, 2013Publication date: March 26, 2015Applicant: The Regents of the University of Colorado, a body CorporateInventors: Hang Yin, John Varga, Swati Bhattacharyya
-
Publication number: 20150087510Abstract: Fungicidal mixtures, comprising as active components 1) at least one 1-methylpyrazol-4-ylcarboxanilide of the formula I where R1?C1-C4-alkyl or C1-C4-haloalkyl, R2=hydrogen or halogen, X=hydrogen or halogen, Q=direct bond, a cyclopropylene or an anellated bicyclo[2.2.Type: ApplicationFiled: September 29, 2014Publication date: March 26, 2015Inventors: Markus GEWEHR, Ulf GROEGER, Egon HADEN, Michael VONEND
-
Patent number: 8987317Abstract: A plant disease control composition comprising a carboxamide compound represented by following formula (I), wherein R1 represents a hydrogen atom or a methyl group, and R2 represents a methyl group, a difluoromethyl group or a trifiuoromethyl group, and one or more dithiocarbamate compounds selected from group (A) consisting of mancozeb, maneb, thiram and zineb is provided by the present invention, and this composition has an excellent effect for controlling a plan disease.Type: GrantFiled: April 25, 2011Date of Patent: March 24, 2015Assignee: Sumitomo Chemical Company, LimitedInventor: Yuichi Matsuzaki
-
Patent number: 8987471Abstract: The present invention relates to substituted dihydropyrazoles, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: GrantFiled: February 13, 2014Date of Patent: March 24, 2015Assignee: Allergan, Inc.Inventors: Janet A. Takeuchi, Ling Li, Wha Bin Im, Ken Chow
-
Patent number: 8987318Abstract: Described herein are liver X receptor (LXR) modulators and methods of utilizing LXR modulators in the treatment of dermal diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.Type: GrantFiled: September 2, 2014Date of Patent: March 24, 2015Assignee: Alexar Therapeutics, Inc.Inventor: Raju Mohan
-
Publication number: 20150080434Abstract: A compound of formula Ia: The present invention relates to novel indazolyl derivatives, to pharmaceutical compositions comprising such derivatives, to processes for preparing such novel derivatives and to the use of such derivatives as medicamentsType: ApplicationFiled: November 19, 2014Publication date: March 19, 2015Inventors: Markus Berger, Hartmut Rehwinkel, Jan Dahmen, Anders Eriksson, Thomas Hansson, Nafizal Hossain, Per Thomas Klingstedt, Matti Lepistö, Stinabritt Nilsson, Martin Hemmerling, Karl Edman
-
Publication number: 20150080446Abstract: The present invention provides a compound, that is a 1-[(2-{[(alkyl or aryl)methyl]oxy}halo or haloalkyl substituted-phenyl)alkyl]-5-hydrocarbyl or substituted hydrocarbyl-1H-pyrazole carboxylic acid or alkylenylcarboxylic acid or a hydrocarbyl or substituted hydrocarbyl sulfonamide of said carboxylic acid or said alkylenylcarboxylic acid, provided however said compound is not a 3-carboxylic acid, a sulfonamide thereof, or a 3-methylenylcarboxylic acid. The compound may be represented by the following formula Wherein R1, R2, R3, R4, R5, R6, X, W, X and Y are as defined in the specification. The compounds may be administered to treat DP1, FP, EP1, TP and/or EP4 receptor mediated diseases or conditions.Type: ApplicationFiled: September 16, 2014Publication date: March 19, 2015Inventors: David F. Woodward, William R. Carling, Jose L. Martos, Jenny W. Wang, Jussi J. Kangasmetsa
-
Publication number: 20150080349Abstract: The present invention provides compounds and methods for modulation of the quorum sensing of bacteria. In an embodiment, the compounds of the present invention are able to act as replacements for naturally occurring bacterial quorum sensing ligands in a ligand-protein binding system; that is, they imitate the effect of natural ligands and produce an agonistic effect. In another embodiment, the compounds of the present invention are able to act in a manner which disturbs or inhibits the naturally occurring ligand-protein binding system in quorum sensing bacteria; that is, they produce an antagonistic effect. The compounds of the present invention comprise N-acylated-homoserine lactones (AHLs) comprised of a wide range of acyl groups.Type: ApplicationFiled: July 10, 2014Publication date: March 19, 2015Inventors: Helen E. BLACKWELL, Grant D. GESKE, Jennifer C. CAMPBELL
-
Publication number: 20150080381Abstract: Method of treating alopecia and acne with are disclosed.Type: ApplicationFiled: April 12, 2013Publication date: March 19, 2015Inventors: Mark G. Currie, Yueh-tyng Chien
-
Patent number: 8980934Abstract: The present teachings provide a compound represented by structural formula (I): or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof.Type: GrantFiled: June 21, 2013Date of Patent: March 17, 2015Assignee: University Health NetworkInventors: Heinz W. Pauls, Radoslaw Laufer, Sze-Wan Li, Grace Ng
-
Patent number: 8981131Abstract: The present invention provides compounds represented by formula I: 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: GrantFiled: July 25, 2008Date of Patent: March 17, 2015Assignee: Piramal Enterprises LimitedInventors: Dilip Narayanrao Bhedi, Ram Asrey Vishwakarma, Vaishali Deka, Dattatray Maruti More, Manivannan Ramalingam, Ashish Suthar, Roda Dalal, Sapna Parikh, Aditi Amol Tannu
-
Patent number: 8980792Abstract: The present invention relates to methods comprising applying to a useful plant, the locus thereof or propagation material thereof a combination of abscisic acid and a fungicidally active compound, which fungicidally active compound is a succinate dehydrogenase inhibitor, in particular for increasing the potency of a fungicidally active compound. The invention also relates to compositions comprising abscisic acid and the fungicidally active compounds as well as seeds comprising the combinations.Type: GrantFiled: October 21, 2011Date of Patent: March 17, 2015Assignees: Syngenta Participations AG, Syngenta LimitedInventors: Elizabeth Pearson, Jose Luis Calvo, Robin Wesley, Jeremy R. Godwin, Ryan Jon Langs Ramsey, Timothy Robert Hawkes
-
Publication number: 20150073029Abstract: The present invention relates to fungicidal 1-(pyrazolylcarbonyl)piperidines or pyrrolidines, and their thiocarbonyl derivatives, their process of preparation and intermediate compounds for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions.Type: ApplicationFiled: April 11, 2013Publication date: March 12, 2015Inventors: Christoph Braun, Pierre Cristau, Philippe Desbordes
-
Patent number: 8975254Abstract: The present disclosure relates to compounds of formula (I), and pharmaceutically acceptable salts thereof. The present disclosure also relates to compositions and methods of treating comprising compounds of formula (I), and pharmaceutically acceptable salts thereof.Type: GrantFiled: October 27, 2010Date of Patent: March 10, 2015Assignee: Orion CorporationInventors: Gerd Wohlfahrt, Olli Törmäkangas, Harri Salo, Iisa Höglund, Arja Karjalainen, Pia Knuuttila, Patrik Holm, Sirpa Rasku, Anniina Vesalainen
-
Patent number: 8974827Abstract: A pharmaceutical composition comprises nanoparticles comprising a poorly water-soluble drug, a poorly aqueous soluble non-ionizable cellulosic polymer, and a poorly aqueous soluble polymeric amphiphilic non-ionizable block copolymer.Type: GrantFiled: May 26, 2008Date of Patent: March 10, 2015Assignee: Bend Research, Inc.Inventors: Corey Jay Bloom, Marshall David Crew, Warren Kenyon Miller, Michael Mark Morgen, Daniel Tod Smithey
-
Publication number: 20150065445Abstract: The present invention relates to viral polymerase inhibitors of formula (I) or salts, N-oxides, solvates, hydrates, racemates, enantiomers or isomers thereof, processes for their preparation and their use in the treatment of Flaviviridae viral infections such as Hepatitis C virus (HCV) infections.Type: ApplicationFiled: April 11, 2013Publication date: March 5, 2015Inventors: Tyrone Pieter Jeynes, Alistair George Draffan, Michael Harding, Silas Bond, Rosliana Halim
-
Publication number: 20150065431Abstract: The present invention provides methods of reducing cutaneous scar formation by treating a cutaneous wound with a composition comprising a therapeutic agent that is a sodium channel blocker and/or an inhibitor of the Nax/SCN7A pathway. The present invention also provides wound cover components impregnated with such compositions, kits composed of such compositions with a wound dressing or sterile wipe, and mixtures of such compositions with a topical component (e.g., cream, ointment, or gel) suitable for application to a cutaneous wound. The present invention also provides compositions, kits, devices, and methods for treating skin conditions (e.g., dermatitis, psoriasis, or other skin conditions) with such compositions and devices. Examples of such therapeutic agents include, but are not limited to, an inhibitor of a gene or protein selected from: ENac, COX-2, PGE2, PI3K, PKB, Nax Prss8, IL-1?, IL-8, SAPK, Erk gene, p38 gene, PAR2, S100A8, S100A9, S100A12.Type: ApplicationFiled: August 27, 2014Publication date: March 5, 2015Inventors: Wei Xu, Seok Jong Hong, Robert D. Galiano, Thomas A. Mustoe
-
Publication number: 20150065543Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, Y, Z, Q, W, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: October 23, 2014Publication date: March 5, 2015Applicant: THERAVANCE BIOPHARMA R&D IP, LLCInventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson
-
Patent number: 8969371Abstract: The present disclosure relates to compositions, kits, uses, systems and methods related to naltrexone plus bupropion for treating an overweight or obese subject at increased risk of adverse cardiovascular outcomes. Preferably, the subject has had type-two diabetes for a period of less than 6 years or is a current smoker, optionally that does not have type-two diabetes.Type: GrantFiled: July 2, 2014Date of Patent: March 3, 2015Assignee: Orexigen Therapeutics, Inc.Inventors: Preston Klassen, Kristin Taylor
-
Patent number: 8969399Abstract: A plant disease control composition comprising a carboxamide compound represented by following formula (I), wherein R1 represents a hydrogen atom or a methyl group, and R2 represents a methyl group, a difluoromethyl group or a trifluoromethyl group, and chlorothalonil is provided by the present invention, and this composition has an excellent effect for controlling a plan disease.Type: GrantFiled: April 25, 2011Date of Patent: March 3, 2015Assignee: Sumitomo Chemical Company, LimitedInventor: Yuichi Matsuzaki
-
Patent number: 8969246Abstract: Pesticidal mixtures comprising, as active components, 1) an anthranilamid compound of the formula I wherein the variables are defined according to the description, and 2) at least one fungicidal compound II selected from the following groups: strobilurins, carboxamides, heterocylic compounds and other active compounds according to the description, in a synergistically effective amount, methods for controlling pests, and harmful fungi, methods of protecting plants from attack or infestation by insects, acarids or nematodes, methods for treating, controlling, preventing or protecting an animal against infestation or infection by parasites, compositions containing these mixtures, and methods for their preparation.Type: GrantFiled: March 13, 2013Date of Patent: March 3, 2015Assignee: BASF SEInventors: Jürgen Langewald, Reinhard Stierl
-
Patent number: 8969341Abstract: The invention relates to compounds of formula (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.Type: GrantFiled: November 28, 2012Date of Patent: March 3, 2015Assignee: Novartis AGInventors: Pascal Furet, Vito Guagnano, Philipp Holzer, Robert Mah, Keiichi Masuya, Achim Schlapbach, Stefan Stutz, Andrea Vaupel
-
Publication number: 20150057247Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of degenerative diseases and disorders.Type: ApplicationFiled: October 29, 2014Publication date: February 26, 2015Inventors: Craig C. Beeson, Christopher C. Lindsey, Yuri K. Peterson, Baerbel Rohrer
-
Publication number: 20150057318Abstract: The invention relates to the use of succinate dehydrogenase SDH inhibitors (SDHIs), in particular bixafen, penflufen or fluopyram for controlling wood diseases in grape, to a method for treating plants or plant parts for controlling wood diseases in grape and to a method for controlling wood diseases in grape plants and plant parts, and in plants which grow from the seedlings, grafts and cuttings, by treating them with SDHIs.Type: ApplicationFiled: February 19, 2013Publication date: February 26, 2015Applicants: BAYER CROPSCIENCE AG, BAYER INTELLECTUAL PROPERTY GmbHInventors: Lucien Meunier, Gilbert Labourdette, Helene Lachaise
-
Publication number: 20150057301Abstract: This invention relates generally to stimulating neurogenesis (e.g., post-natal neurogenesis, e.g., post-natal hippocampal neurogenesis) and protectiong from neuron cell death.Type: ApplicationFiled: July 24, 2014Publication date: February 26, 2015Inventors: Steven L. McKnight, Joseph M. Ready, Andew A. Pieper, Jef K. De Brabander
-
Publication number: 20150051183Abstract: The conformationally restricted, spatially defined macrocyclic ring system of formula (I) is constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. Macrocycles described by this ring system I are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), inhibitory activity on enzymes or antimicrobial activity. In particular, these macrocycles show inhibitory activity on endothelin converting enzyme of subtype 1 (ECE-1) and/or the cysteine protease cathepsin S (CatS), and/or act as antagonists of the oxytocin (OT) receptor, thyrotropin-releasing hormone (TRH) receptor and/or leukotriene B4 (LTB4) receptor, and/or as agonists of the bombesin 3 (BB3) receptor, and/or show antimicrobial activity against at least one bacterial strain.Type: ApplicationFiled: March 15, 2013Publication date: February 19, 2015Inventors: Daniel Obrecht, Philipp Ermert, Said Oumouch, Arnaud Piettre, Jean-François Gosalbes, Marc Thommen
-
Patent number: 8957066Abstract: This invention relates to generally inhibiting histone deacetylase (“HDAC”) enzymes (e.g., HDAC1, HDAC2, and HDAC3) using compounds of formula (I), wherein the substituents are as defined herein.Type: GrantFiled: March 15, 2013Date of Patent: February 17, 2015Assignee: Biomarin Pharmaceutical Inc.Inventors: Vincent Jacques, James R Rusche, Norton P. Peet, Jasbir Singh
-
Patent number: 8957094Abstract: A therapeutic agent or prophylactic agent has an analgesic effect on both nociceptive pain and neuropathic pain and is effective in treatment of fibromyalgia. The agent includes as an effective ingredient a cyclohexane derivative or a pharmaceutically acceptable salt thereof or a prodrug thereof.Type: GrantFiled: March 31, 2011Date of Patent: February 17, 2015Assignee: Toray Industries, Inc.Inventors: Chihiro Yoshida, Kaoru Nakao
-
Publication number: 20150045389Abstract: The present invention is a screening assay for identifying inhibitors of Pseudomonas aeruginosa CFTR Inhibitory Factor as well as compounds identified by the screening assay for use in compositions and methods for ameliorating or treating a respiratory disease such as cystic fibrosis or secondary infection thereof.Type: ApplicationFiled: April 9, 2013Publication date: February 12, 2015Inventors: Dean R. Madden, Christopher D. Bahl, Bruce D. Hammock, Christophe Morisseau
-
Publication number: 20150045398Abstract: The present invention provides a compound of formula (I): said compound is inhibitor of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12, and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.Type: ApplicationFiled: October 7, 2014Publication date: February 12, 2015Applicant: NOVARTIS AGInventors: Claus EHRHARDT, Leslie Wighton MCQUIRE, Pascal RIGOLLIER, Olivier ROGEL, Michael David SHULTZ, Ruben Alberto TOMMASI
-
Publication number: 20150045404Abstract: The invention provides a compound of formula (I): wherein R1-R5 have any of the values defined in the specification. The compounds are useful for the treatment of cancer and other diseases.Type: ApplicationFiled: March 25, 2013Publication date: February 12, 2015Inventors: John Kodet, Jeffrey D. Neighbors, David F. Wiemer
-
Publication number: 20150045405Abstract: An improved AKT inhibiting compound, crystalline N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide hydrochloride.Type: ApplicationFiled: October 23, 2014Publication date: February 12, 2015Inventors: Pingyun Y. CHEN, Jeffrey GAULDING
-
Publication number: 20150045327Abstract: The present invention discloses compounds according to Formula I: wherein R1 is as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment cystic fibrosis by administering a compound of the invention.Type: ApplicationFiled: August 5, 2014Publication date: February 12, 2015Inventors: Steven Emiel VAN DER PLAS, Hans KELGTERMANS, Sébastien Jean Jacques Cédric DROPSIT MONTOVER, Sébastien Laurent Xavier MARTINA, Martin James Inglis ANDREWS
-
Publication number: 20150045300Abstract: The subject invention is directed to a pharmaceutical composition comprising an open matrix network carrying a pharmaceutically active ingredient, wherein the open matrix network comprises both the polysaccharides levan and inulin.Type: ApplicationFiled: September 7, 2012Publication date: February 12, 2015Applicant: FERRING B.V.Inventors: Varinder Ahuja, Tejas Gunjikar, Balachendar Gundu
-
Publication number: 20150045399Abstract: Described herein are liver X receptor (LXR) modulators and methods of utilizing LXR modulators in the treatment of dermal diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.Type: ApplicationFiled: September 2, 2014Publication date: February 12, 2015Applicant: Alexar Therapeutics, Inc.Inventor: Raju Mohan
-
Patent number: 8952042Abstract: The present invention relates to compounds of formula (1): where R, A, Q and Z are defined herein, or an enantiomer, diastereomer, tautomer, solvate, prodrug or pharmaceutical acceptable salt thereof. These compounds bind to the NR1H4 receptor (FXR) and act as agonists of the NR1H4 receptor (FXR). The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds, and to a process for the synthesis of said compounds.Type: GrantFiled: August 19, 2010Date of Patent: February 10, 2015Assignee: Phenex Pharmaceuticals AGInventors: Claus Kremoser, Ulrich Abel, Christoph Steeneck, Olaf Kinzel
-
Patent number: 8952026Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting PRMT1 activity. Methods of using the compounds for treating PRMT1-mediated disorders are also described.Type: GrantFiled: March 14, 2014Date of Patent: February 10, 2015Assignee: Epizyme, Inc.Inventors: Lorna Helen Mitchell, Gideon Shapiro, Richard Chesworth, Paula Ann Boriack-Sjodin, Oscar Miguel Moradei
-
Patent number: 8946267Abstract: A therapeutic agent or a prophylactic agent for neuropathic pain provides a synergistically-enhanced analgesic effect at a dose at which a calcium channel ?2? ligand does not produce any side effects as well as which agent does not produce any new side effects on the central nervous system. The therapeutic agent or a prophylactic agent for neuropathic pain includes as effective ingredients a cyclohexane derivative, represented by the following formula, or a pharmaceutically acceptable salt thereof or a prodrug thereof, and a calcium channel ?2? ligand.Type: GrantFiled: July 29, 2011Date of Patent: February 3, 2015Assignee: Toray Industries, Inc.Inventors: Naoki Izumimoto, Hidenori Mochizuki
-
Patent number: 8946231Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.Type: GrantFiled: March 15, 2010Date of Patent: February 3, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Christopher S. Burgey, Craig M. Potteiger
-
Patent number: 8946236Abstract: The present invention relates to new insecticides of the formula (I) in which R1, R2, R3, R4, R5, R6, A, Q and n can have the definitions stated in the description, to a number of processes for preparing them and to their use as active compounds, more particularly to their use as pest control compositions.Type: GrantFiled: August 7, 2013Date of Patent: February 3, 2015Assignee: Bayer Cropscience AGInventors: Bernd Alig, Ruediger Fischer, Christian Funke, Rudolf F. Ernst Gesing, Achim Hense, Olga Malsam, Mark Wilhelm Drewes, Ulrich Goergens, Tetsuya Murata, Katsuaki Wada, Christian Arnold, Erich Sanwald
-
Patent number: 8946278Abstract: Invented are novel heterocyclic carboxamide compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.Type: GrantFiled: February 22, 2013Date of Patent: February 3, 2015Assignee: GlaxoSmithKline LLCInventors: Mark A. Seefeld, Meagan B. Rouse, Dirk A. Heerding, Dennis S. Yamashita, Kenneth C. McNulty
-
Patent number: 8946204Abstract: Substituted phenylureas and phenylamides, processes for their preparation, pharmaceutical compositions containing these compounds, and the use of these compounds for preparing pharmaceutical compositions.Type: GrantFiled: November 9, 2011Date of Patent: February 3, 2015Assignee: Gruenenthal GmbHInventors: Robert Frank, Gregor Bahrenberg, Thomas Christoph, Klaus Schiene, Jean De Vry, Nils Damann, Sven Frormann, Bernhard Lesch, Derek John Saunders, Jeewoo Lee, Yong-Soo Kim, Myeong-Seop Kim, Hannelore Stockhausen
-
Patent number: 8946279Abstract: The present invention belongs to the technical field of medicine, relating in particular to: a fused ring compound as represented by Formula (I) for use as a mineralocorticoid receptor antagonist, a pharmaceutically acceptable salt thereof, and an isomer thereof; a preparation method for these compounds; a pharmaceutical preparation containing these compounds; and an application of these compounds, the pharmaceutically acceptable salt thereof, or the isomers thereof in the preparation of medicants for the treatment and/or prevention of kidney injury, cardiovascular diseases such as hypertension, and/or endocrine disease. The definitions of X, Y1, Y2, Y3, R1, R2a, R2b, R3a, R3b, R4, Cy and n are as presented in the description.Type: GrantFiled: August 18, 2011Date of Patent: February 3, 2015Assignee: KBP Biosciences Co., Ltd.Inventors: Zhenhua Huang, Jinyuan Wang, Dedong Zhang
-
Patent number: 8946234Abstract: The invention relates to compounds of the general formula (I), in which the radicals A1, A2, A3, A4, Lm, Q, R1, T and U have the meaning given in the description and to the use of the compounds for controlling animal pests. In addition, the invention relates to processes and intermediates for the preparation of the compounds according to formula (I).Type: GrantFiled: October 27, 2009Date of Patent: February 3, 2015Assignee: Bayer CropScience AGInventors: Michael Maue, Isabelle Adelt, Wolfgang Giencke, Markus Heil, Peter Jeschke, Bernd-Wieland Krüger, Friedrich August Mühlthau, Alexander Sudau, Klaus Raming, Ulrich Ebbinghaus-Kintscher, Martin Adamczewski, Arnd Voerste, Ulrich Görgens, Tobias Kapferer, Mark Wilhelm Drewes, Angela Becker, Eva-Maria Franken
-
Publication number: 20150030673Abstract: Provided herein is a hydrogen chloride salt of 1-(3-/t?r/-butyl-1-p-tolyl-1H-pyrazol-5-yl)-3-(5-fluoro-2-(1-(2-hydroxyethyl)-1H-indazol-5-yloxy)benzyl)urea, crystalline forms of 1-(3-½?butyl-1?-tolyl-1H-pyrazol-5-yl)-3-(5-fluoro-2-(1-(2-hydroxyethyl)-1H-indazol-5-yloxy)benzyl)urea hydrochloride, processes for the preparation of said crystalline forms, pharmaceutical compositions containing a crystalline form of 1-(3-r<i/-r-butyl-1-p-tolyl-1H-pyrazol-5-yl)-3-(5-fluoro-2-(1-(2-hydroxyethyl)-1H-indazol-5-yloxy)benzyl)urea hydrochloride Form B, processes for the preparation of said compositions, pharmaceutical compositions prepared by said methods, and the use of said compositions in the treatment of various diseases and disorders.Type: ApplicationFiled: February 27, 2013Publication date: January 29, 2015Applicant: Array BioPharma Inc.Inventors: Alisha B. Arrigo, Donald T. Corson, Coralee G. Mannila
-
Publication number: 20150031697Abstract: Provided herein are methods of preventing skin cancer, where the methods comprise the step of administering an effective amount of at least one Hsp90 inhibitor to a subject at the risk of developing skin cancer, whereby the skin cancer is prevented in the subject.Type: ApplicationFiled: July 25, 2014Publication date: January 29, 2015Inventor: Ajit K. Verma
-
Patent number: 8940781Abstract: A composition comprising a carboxamide compound represented by following formula (I), wherein R1 represents a hydrogen atom or a methyl group, and R2 represents a methyl group, a difluoromethyl group or a trifluoromethyl group, and one or more pyrethroid compounds selected from group (A) consisting of tefluthrin, lambda-cyhalothrin, cypermethrin, beta-cyfluthrin, permethrin, deltamethrin and bifenthrin is provided by the present invention, and this composition has an excellent pesticidal effect.Type: GrantFiled: April 25, 2011Date of Patent: January 27, 2015Assignee: Sumitomo Chemical Company, LimitedInventor: Yuichi Matsuzaki
-
Patent number: 8940774Abstract: Provided are tris-quaternary 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/or gastrointestinal tract disorders.Type: GrantFiled: November 26, 2013Date of Patent: January 27, 2015Inventors: Peter Crooks, Linda Dwoskin, Roger Papke, Guangrong Zheng, Sangeetha Sumithran
-
Publication number: 20150023921Abstract: The present invention relates to novel compositions having anti-viral activity and in particular it relates to synergistic compositions active against Hepatitis C virus (HCV). The invention also relates to methods for retarding, reducing or otherwise inhibiting HCV growth and/or functional activity.Type: ApplicationFiled: April 3, 2014Publication date: January 22, 2015Applicant: BIOTRON LIMITEDInventors: Gary Dinneen EWART, Carolyn Anne LUSCOMBE, Michelle MILLER
-
Publication number: 20150025120Abstract: A compound represented by the following formula: or a pharmaceutically acceptable salt thereof, and pharmaceutical use thereof.Type: ApplicationFiled: June 30, 2014Publication date: January 22, 2015Inventors: Takahisa MOTOMURA, Takuya MATSUO, Gakujun SHOMI, Masafumi INOUE