Spiro Ring System Patents (Class 514/462)
-
Patent number: 8101656Abstract: The present invention relates to the use of 2,2-dimethyl-3-(2,4-dichlorophenyl)-2-oxo-1-oxaspiro[4.5]dec-3-en-4-yl butanoate for controlling acarids in hops, kiwi fruit, soft fruit, nuts, coffee, tropical fruit, spices and conifers.Type: GrantFiled: July 2, 2004Date of Patent: January 24, 2012Assignee: Bayer CropScience AGInventors: Reiner Fischer, Ernst Brück
-
Publication number: 20120015910Abstract: Novel active compound combinations comprising a carboxamide of the general formula (I) (group 1) in which A, R1, R2 and R3 are as defined in the description, and the active compound groups (2) to (23) listed in the description have very good fungicidal properties.Type: ApplicationFiled: September 23, 2011Publication date: January 19, 2012Applicant: Bayer CropScience AGInventors: Ulrike Wachendorff-Neumann, Peter Dahmen, Ralf Dunkel, Hans-Ludwig Elbe, Anne Suty-Heinze, Heiko Rieck
-
Publication number: 20120010281Abstract: Infections caused by Mycobacterium tuberculosis kill more than 1.8 million people each year. While the persistence of this pathogenic bacterial species and the emergence of multidrug resistant strains have created an urgent need for new TB therapies, a new TB-specific drug has not been developed in over 40 years. The disclosure herein provides short and scalable syntheses of small molecules, and small molecules as new therapeutics for eradicating this life threatening pathogen.Type: ApplicationFiled: June 22, 2011Publication date: January 12, 2012Applicant: THE TRUSTEES OF PRINCETON UNIVERSITYInventors: Erik J. Sorensen, Stephen D. Lotesta, Junjia Liu, Emma V. Yates, Maurice A. Marsini
-
Publication number: 20120010227Abstract: The invention relates to a pharmaceutical composition with a content in active ingredient that can be an antimycotic, so that the composition is suitable for the treatment of onychomycoses, in particular severe onychomycoses. The inventive formulation is an ointment-like thermogel at body temperature and an inviscid thermogel at lower temperatures and facilitates the permeation of sufficient active ingredient quantities through human fingernails and toenails, in order to also treat severe onychomycoses.Type: ApplicationFiled: July 29, 2010Publication date: January 12, 2012Applicant: Technische Universitat BraunschweigInventors: Lusiana, Christel Müller-Goymann
-
Publication number: 20110312904Abstract: The present invention provides compounds of Formula (I), compositions comprising an effective amount of a compound of Formula (I), optionally with chemotherapeutic drugs such as a tubulin-binding drug, and methods of their use for reducing the toxicity of cytotoxic agents, treating or preventing cancer or a neuropathic disorder, inducing a chemoprotective phase II enzyme, DNA, or protein synthesis, enhancing the immune system, treating inflammation, improving and enhancing general health or well-being, and methods for making compounds of Formula (I).Type: ApplicationFiled: August 27, 2009Publication date: December 22, 2011Applicants: SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH, TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORKInventors: Samuel J. Danishefsky, Ting-Chao Chou, Xiaoguang Lei, Heedong Yun, Fay Ng, John Hartung, Dalibor Sames
-
Publication number: 20110313003Abstract: GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.Type: ApplicationFiled: June 16, 2010Publication date: December 22, 2011Inventors: Dong Fang Shi, Jiangao Song, Jingyuan Ma, Aaron Novack, Phuongly Pham, Imad Fayek Nashashibi, Christopher J. Rabbat, Xin Chen
-
Publication number: 20110306499Abstract: The invention relates to novel compounds of the formula (I) in which W, X, Y, Z and CKE have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides, and also to selective herbicidal compositions comprising, firstly, the compounds of the formula (I) and, secondly, at least one crop plant compatibility-improving compound. The invention further relates to the boosting of the action of crop protection compositions comprising compounds of the formula (I) through the additions of ammonium salts or phosphonium salts and optionally penetrants.Type: ApplicationFiled: November 22, 2007Publication date: December 15, 2011Applicant: Bayer CropScience AGInventors: Thomas Bretschneider, Reiner Fischer, Rolf Pontzen, Christian Arnold, Ulrich Görgens, Olga Malsam, Udo Reckmann, Erich Sanwald, Stefan Lehr, Jan Dittgen, Dieter Feucht, Martin Hills, Christopher Rosinger
-
Publication number: 20110306662Abstract: The present invention relates to steroid-derived cyclopamine analogs and methods for using the same for inhibiting sonic hedgehog signaling and preventing or treating cancer. A method for synthesizing the analogs of the present invention from a steroid is also provided.Type: ApplicationFiled: June 15, 2011Publication date: December 15, 2011Applicant: The Wistar Institute and The Trustees of the University of PennsylvaniaInventors: Nadia Dahmane, Jeffrey D. Winkler
-
Publication number: 20110301233Abstract: Novel polyisoprenylated benzophenone derivatives isolated from the plant Garcinia paucinervis. Among these new compounds, paucinones A-C (Compounds 1-3) contains an unexpected cyclohexane-spiro-tetrahydrofuran moiety. A 1-methylene-3,3-dimethylcyclohexane group never reported before was found in the structure of paucinone D (Compound 4). Structures of these compounds were elucidated with spectroscopic evidence. The relative stereochemistry of 1-4 was determined by NOESY correlations. These compounds a potent ability to activate caspase-3 in HeLa-C3 cells within 72 hours at a low concentration and significant cytotoxicity against HeLa-C3 cells.Type: ApplicationFiled: June 4, 2010Publication date: December 8, 2011Inventors: XUE-MEI GAO, Ting Yu, Kathy Qian Luo, Hong Xi Xu
-
Publication number: 20110301099Abstract: A method and composition that allows for the penetration of lipid insoluble medicaments through cell membranes using small S-Allyl-containing molecules with phospholipid permeable molecules as carrier molecules. S-Allyl-containing compounds can include alliin, allicin, Allium sativum extract and DMSO. Lipid insoluble medicaments can include 1% xylocaine, curcumin, acyclovir, valacyclovir, famciclovir, terbenafin, griseofulvin, clotrimazole, ketoconazole, clindamycin, neomycin, polysporin, bactricin, among others. The lipid insoluble medicaments are mixed with the phospholipid permeable molecules and painted on the skin using a swab or other suitable tool, thereby allowing for penetration of the medicament and providing relief from pain potentially caused by a subsequent injection. The composition can also be administered through an inhaler or directly into mucous membranes.Type: ApplicationFiled: June 4, 2010Publication date: December 8, 2011Inventor: Madalene Choon Ying Heng
-
Publication number: 20110294783Abstract: The present invention concerns boosting the activity of crop protection materials comprising inhibitors of fatty acid biosynthesis (for example phenyl-substituted cyclic ketoenols) through the addition of ammonium salts and/or phosphonium salts or through the addition of ammonium salts and/or phosphonium salts and penetrants, the corresponding materials, processes for preparing them, and their use in crop protection.Type: ApplicationFiled: August 10, 2011Publication date: December 1, 2011Applicant: BAYER CROPSCIENCE AGInventors: Reiner FISCHER, Stefan LEHR, Peter MARCZOK, Udo Reckmann, Christian Arnold, Waltraud Hempel, Erich SANWALD, Rolf Pontzen
-
Patent number: 8067620Abstract: A means and method for treating malaria, schistosomiasis, and cancer using a spiro or dispiro 1,2,4-trioxolane is described. The preferred 1,2,4-trioxolanes include a spiroadamantane group on one side of the trioxolane group, and a spirocyclohexyl on the other side of the trioxolane group. In comparison to artemisinin semisynthetic derivatives, the compounds of this invention are structurally simple, easy to synthesize, non-toxic, and potent against malarial parasites. The compounds of the invention unexpectedly provide a single-dose cure for malaria, as well as prophylactic activity against the same. The compounds are also active against schistosomiasis and cancer.Type: GrantFiled: October 31, 2007Date of Patent: November 29, 2011Assignee: Medicines for Malaria Venture MMVInventors: Jonathan L. Vennerstrom, Yuxiang Dong, Susan A. Charman, Sergio Wittlin, Jacques Chollet, Darren J. Creek, Xiaofang Wang, Kamaraj Spiraghavan, Lin Zhou, Hugues Matile, William N. Charman
-
Publication number: 20110280921Abstract: The present invention relates to hydrogels endowed with antibacterial properties, to be used for injection in damaged bones or in the production of antibacterial coatings of prostheses for implant in the human or animal body, obtained by loading with antibacterial agents hydrogels formed by derivatives of hyaluronic acid; the invention also relates to a kit of parts for producing the antibacterial hydrogels.Type: ApplicationFiled: January 29, 2010Publication date: November 17, 2011Applicants: NOVAGENIT S.R.L., MERO S.R.LInventors: Gaetano Giammona, Giovanna Pitarresi, Fabio Palumbo, Carlo Luca Romano, Enzo Meani, Edgardo Cremascoli
-
Patent number: 8058288Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.Type: GrantFiled: June 17, 2010Date of Patent: November 15, 2011Assignee: Incyte CorporationInventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Colin Zhang, Brian W. Metcalf, Chunhong He, Ding-Quan Qian
-
Publication number: 20110275708Abstract: The invention relates to a novel compound of formula I or pharmaceutically acceptable salts thereof as well as pharmaceutical, nutraceutical, and botanical drug compositions and therapeutic methods related thereto. In certain embodiments, the compounds are used for the treatment of abnormal cell growth, hyperproliferative disorders, and inflammatory diseases in mammals. In other embodiments, the invention encompasses methods to isolate and synthesize the compounds.Type: ApplicationFiled: October 22, 2009Publication date: November 10, 2011Applicant: CORNELL UNIVERSITYInventors: Kathryn J. Chavez, Eloy Rodriguez, Frank Schroeder, James A. Flanders
-
Publication number: 20110275709Abstract: Use of tellurium-containing compounds for maintaining and/or augmenting fertility in a male subject following chemotherapy and/or radiotherapy is disclosed. The tellurium-containing compound is utilized in combination with a chemotherapeutic agent and/or radiation, such that the male subject treated by the chemotherapeutic agent and/or radiation and by the tellurium-containing compound is instructed to refrain from conceptive sex for a pre-determined time period, following the chemotherapy and/or radiotherapy, during which conception is undesired.Type: ApplicationFiled: January 7, 2010Publication date: November 10, 2011Applicant: BIOMAS LTD.Inventors: Benjamin Sredni, Michael Albeck, Benjamin Ron
-
Publication number: 20110263424Abstract: The present invention relates to novel oxaspirocyclic spirophenyl-substituted tetramic acid and tetronic acid derivatives of the formula (I) in which W, X, Y, Z, A, B, D, Q1, Q2, and G have the meanings given above, to a plurality of processes for their preparation and to their use as pesticides and/or herbicides. The invention also provides selective herbicidal compositions comprising, firstly, oxaspirocyclic spirophenyl-substituted tetramic acid and tetronic acid derivatives and, secondly, a crop plant compatibility-improving compound. The invention furthermore relates to increasing the activity of crop protection compositions comprising compounds of the formula (I) by addition of ammonium salts or phosphonium salts and, if appropriate, penetrants.Type: ApplicationFiled: July 22, 2008Publication date: October 27, 2011Applicant: Bayer CropScience AGInventors: Thomas Bretschneider, Reiner Fischer, Gudrun Lange, Stefan Lehr, Christian Arnold, Dieter Feucht, Eva-Maria Franken, Martin Jeffrey Hills, Heinz Kehne, Olga Malsam, Christopher Hugh Rosinger, Jan Dittgen, Ulrich Gorgens, Isolde Hauser-Hahn
-
Patent number: 8039013Abstract: The present invention relates to novel active substance combinations which contain spiroxamine, which is known, a known azole and a known carboxamide and which are very suitable for controlling undesired phytopathogenic fungi.Type: GrantFiled: September 3, 2005Date of Patent: October 18, 2011Assignee: Bayer CropScience AGInventors: Peter Dahmen, Ulrike Wachendorff-Neumann, Ralf Dunkel
-
Publication number: 20110251146Abstract: A topical, foamable composition is provided that includes at least one antifungal agent that is able to penetrate the upper layers of skin and is retained in or on an area to be treated for a prolonged period of time, and that has a residual non-volatile component content less than 25%. In addition, a method of treating fungal diseases including jock itch, tinea, dandruff and sebborheic dermatitis is provided, and includes applying to the affected area of patient requiring such treatment an antifungal composition.Type: ApplicationFiled: June 21, 2011Publication date: October 13, 2011Applicant: STIEFEL RESEARCH AUSTRALIA PTY LTDInventors: Greg DAVEY, Albert Zorko ABRAM
-
Patent number: 8008346Abstract: The present invention relates to a anti-proliferative target for designing chemotherapeutic agents, which comprises a EIF4A protein having an amino acid sequence, as defined in claim 1.Type: GrantFiled: July 24, 2006Date of Patent: August 30, 2011Assignee: The Royal University for the Advancement of Learning/McGill UniversityInventors: Jerry Pelletier, Marie-Ève Bordeleau, Lisa Lindqvist, Robert Francis, Junichi Tanaka
-
Patent number: 8003690Abstract: The invention relates to a topical nanoparticulate spironolactone formulation comprising nanoparticles having a mean diameter, measured by a photon correlation spectroscopy, in the range of from about 300 nm to about 900 nm. The nanoparticles are incorporated into a crystalline network system comprising a dispersion of solid crystals of polar lipids, said lipids exposing their hydrophilic side outwards and their hydrophobic side inwards towards the spironolactone nanoparticles.Type: GrantFiled: December 13, 2002Date of Patent: August 23, 2011Assignee: Jagotec AGInventors: Guy Vergnault, Pascal Grenier, Alain Nhamias, Dieter Scherer, Petra Beck, Patricia Cancade
-
Publication number: 20110201661Abstract: The present invention relates to novel spiro derivatives of parthenin prepared by the dipolar cycloaddition of various dipoles viz, benzonitrile oxides, nitrones, azides, nitrile ylide diazoalkane, nitrile imide, ozone, azomethine imides, azomethine ylides etc. with exocyclic double bond of C ring (?-methylene-?-butyrolactone). Representative compounds have been screened for their anticancer activity against different cancer cell lines. ICs0 value of these analogues varies between 4.3 ?M to 93 ?M. A mechanistic correlation of their anticancer activity has been described. The results of the cytotoxicity test of the compounds studies indicated that the ?,?-unsaturated ketonic moiety in parthenin plays an important role in the maintenance of the high level of cytotoxicity.Type: ApplicationFiled: March 5, 2009Publication date: August 18, 2011Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCHInventors: Mahabalarao Sampath Kumar Halmuthur, Ajit Kumar Saxena, Subhash Chandra Taneja, Shashank Kumar Singh, Vijay Kumar Sethi, Naveed Ahmed Qazi, Sanghapal Damodhar Sawant, Mahendhar Reddy Doma, Abid Hussain Banday, Monika Verma, Ghularn Nabi Qazi
-
Publication number: 20110195842Abstract: The invention relates to novel 2,4,6-phenyl-substituted cyclic ketoenols of the formula (I), in which CKE, W, X and Y are as defined above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides, and also to selective herbicidal compositions comprising firstly the 2,4,6-phenyl-substituted cyclic ketoenols and secondly at least one compound which improves crop plant tolerance.Type: ApplicationFiled: April 15, 2011Publication date: August 11, 2011Applicant: BAYER CROPSCIENCE AGInventors: Thomas BRETSCHNEIDER, Reiner FISCHER, Oliver GAERTZEN, Klaus KUNZ, Stefan LEHR, Dieter FEUCHT, Peter LÖSEL, Olga MALSAM, Guido BOJACK, Christian ARNOLD, Thomas AULER, Martin Jeffrey HILLS, Heinz KEHNE, Chris ROSINGER
-
Publication number: 20110178170Abstract: The present invention relates to uses of compounds having a structure as shown by formula (I) for the manufacture of a pharmaceutical composition for the treatment of cancer. Moreover, the present invention encompasses methods of treatment for said diseases.Type: ApplicationFiled: June 30, 2008Publication date: July 21, 2011Applicants: DKFZ Deutsches Krebsforschungszentrum, TECHNICAL UNIVERSITY OF DENMARKInventors: Mads Hartvig Clausen, Alwin Kramer, Thomas Ostenfeld Larsen, Blanka Leber
-
Publication number: 20110165259Abstract: [Problem to be Solved] The purpose of present invention is to provide a medicine which has low contamination with a fine-pulverizing medium, is safe and has improved bioavailability. [Solution] A method for producing a composite organic compound powder for medical use is used which comprises: mixing a poorly water-soluble and crystalline organic compound powder, a physiologically acceptable salt, a physiologically acceptable polyol, and a carboxyvinyl polymer and fine-pulverizing the organic compound powder; and removing at least the salt and the polyol during or after fine-pulverizing.Type: ApplicationFiled: September 15, 2009Publication date: July 7, 2011Applicant: ACTIVUS PHARMA CO., LTD.Inventors: Takashi Hirokawa, Takahiro Tada, Jun Nihira
-
Patent number: 7968601Abstract: the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n represents an integer being 1 or 2; R1 and R2 each independently represents hydrogen C1-4alkyl, NR9R10, C1-4alkyloxy; or R1 and R2 taken together with the carbon atom with which they are attached form a C3-6cycloalkyl; and where n is 2, either R1 or R2 may be absent to form an unsaturated bond; R3 represents a C6-12cycloalkyl, preferably selected from cylo-octanyl and cyclohexyl or R3 represents a monovalent radical having one of the following formulae ?wherein said C6-12cycloalkyl or monovalent radical may optionally be substituted with one, or where possible two, three or more substituents selected from the group consisting of C1-4alkyl, C1-4alkyloxy, halo or hydroxy; Q represents Het1 or Ar2 wherein said C3-8cycloalkyl, Het1 or Ar2 are optionally substituted with one or where possible two or more substituents selected from halo, C1-4alkyl, C1-4alkyloxy, hydroxy, nitro, NR5RType: GrantFiled: December 18, 2007Date of Patent: June 28, 2011Assignee: Janssen Pharmaceutica N.V.Inventors: Joannes Theodorus Maria Linders, Gustaaf Henri Maria Willemsens, Ronaldus Arnodus Hendrika Joseph Gilissen, Christophe Francis Robert Nester Buyck, Greta Constantia Peter Vanhoof, Louis Jozef Elisabeth Van Der Veken, Libuse Jaroskova
-
Patent number: 7964637Abstract: A simplified production method of stereoisomer of theaspiran having high optical purity has been desired. An alcohol compound having a specific skeleton is enantioselectively esterified with an enzyme, or an ester compound having a specific skeleton is enantioselectively hydrolyzed with an enzyme. The resultant optically active ester or optically active alcohol is used. Thus, optically active theaspiran having a desired configuration and having a high optical purity is obtained in a satisfactory yield.Type: GrantFiled: September 8, 2006Date of Patent: June 21, 2011Assignee: Takasago International CorporationInventors: Makoto Harada, Hiroyuki Matsuda, Kenya Ishida, Yuichiro Yamazaki
-
Publication number: 20110143943Abstract: The present invention relates to novel C2-phenyl-substituted cyclic ketoenols of the formula (I) in which W, X, Y, Z and CKE are as defined in the description, to processes for their preparation and to their use as pesticides and herbicides.Type: ApplicationFiled: February 17, 2011Publication date: June 16, 2011Applicant: Bayer AktiengesellschaftInventors: Michael RUTHER, Hermann Hagemann, Udo Schneider, Markus Dollinger, Peter Dahmen, Ulrike Wachendorff-Neumann, Reiner Fischer, Alan Graff, Thomas Bretschneider, Christoph Erdelen, Mark Wilhelm Drewes, Dieter Feucht, Folker Lieb
-
Patent number: 7960402Abstract: A compound represented by, e.g. the formula (I): [wherein X, Y, Z, and W each independently represent optionally substituted methine; A, B, and D each independently represent —C(O)—, etc.; Q represents a methine or a nitrogen; and R represents the formula (II-1), optionally substituted with lower alkyl, etc.; (wherein R6 represents a lower alkyl, etc; and R7 and R8 each independently represents a lower alkyl, etc.)] or a pharmaceutically acceptable salt of the compound. The compounds and salt have antagonistic activity against a histamine H3 receptor or inverse agonistic activity against a histamine H3 receptor. They are useful in the prevention or treatment of metabolic diseases, circulatory diseases, or neurotic diseases.Type: GrantFiled: September 6, 2005Date of Patent: June 14, 2011Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Makoto Jitsuoka, Norikazu Ohtake, Nagaaki Sato, Shigeru Tokita, Daisuke Tsukahara
-
Publication number: 20110124656Abstract: The present invention relates to methods for the treatment or prevention of symptoms associated with post-traumatic stress disorder, and related pharmaceutical compositions. Of particular interest are pharmaceutical compositions comprising a very low dose of cyclobenzaprine, alone, or in combination with an alpha-1-adrenergic receptor antagonist, a beta-adrenergic antagonist, an anticonvulsant, a selective serotonin reuptake inhibitor or a serotonin-norepinephrine reuptake inhibitor.Type: ApplicationFiled: November 18, 2010Publication date: May 26, 2011Applicant: TONIX PHARMACEUTICALS, INC.Inventors: Lederman Seth, Harris Herbert
-
Publication number: 20110124502Abstract: Embodiments of the present invention provide compositions for controlling a target pest including a first agent and a second agent comprising a pest control product or a signal cascade modulator, wherein the first agent and the second agent act synergistically to control the target pest. The first agent can be capable of interacting with a receptor in the target pest. The pest control product can have a first activity against the target pest when applied without the active agent and the compositions can have a second activity against the target pest; and the second activity can be greater than the first activity. Embodiments of the invention can include compositions that modulate the signal cascade initiated by the binding of ligands to, for example, cell surface receptors. Methods of screening such compositions are also disclosed.Type: ApplicationFiled: March 19, 2009Publication date: May 26, 2011Inventor: Essam Enan
-
Publication number: 20110112112Abstract: The disclosure provides compounds and methods of using Apogossypolone derivatives for treating diseases and disorders. In particular, the disclosure provides compounds of Formula I: or a pharmaceutically acceptable salt, hydrate, or solvate thereof, and provides methods for the preparation of compounds of Formula I; and methods for treating cancer, autoimmune diseases, and inflammation by administering a compound of Formula I.Type: ApplicationFiled: October 7, 2010Publication date: May 12, 2011Applicant: Sanford-Burnham Medical Research InstituteInventors: Maurizio Pellecchia, Jun Wei
-
Publication number: 20110104235Abstract: The biodegradable drug delivery systems described here are formulated for implantation into the nail unit and its surrounding tissues for the treatment of various nail unit conditions. The systems include non-temperature dependent phase change compositions that may be formulated as solutions, solids, semisolids, microparticles, or crystals.Type: ApplicationFiled: January 6, 2011Publication date: May 5, 2011Inventors: Frank Kochinke, Corinne Bright
-
Patent number: 7928139Abstract: Compounds of Formula I and Formula II are useful as inhibitors of HIF prolyl hydroxylases. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.Type: GrantFiled: November 4, 2009Date of Patent: April 19, 2011Assignee: Amgen Inc.Inventors: Jennifer R. Allen, Kaustav Biswas, Marian C. Bryan, Roland Burli, Guo-Qiang Cao, Michael J. Frohn, Jennifer E. Golden, Stephanie Mercede, Susana Neira, Tanya Peterkin, Alexander J. Pickrell, Anthony Reed, Christopher M. Tegley, Xiang Wang
-
Patent number: 7919528Abstract: Novel PDF inhibitors and novel methods for their use are provided.Type: GrantFiled: May 30, 2003Date of Patent: April 5, 2011Assignee: GlaxoSmithKline LLCInventors: Kelly M. Aubart, Andrew B. Benowitz, Siegfried B. Christensen, IV, Joseph M. Karpinski, Jinhwa Lee, Domingos J. Silva
-
Publication number: 20110071220Abstract: Compounds of the formula (II) in which A, B, G, W, X, Y and Z may have the meanings given in the description are highly suitable for controlling animal pests such as insects and/or spider mites by treating the soil/growth substrate by watering or droplet application or dip application. In soil applications, the activity of crop protection compositions comprising active compounds of the formula (II) can be improved by adjuvants. The present invention describes corresponding processes and suitable compositions.Type: ApplicationFiled: March 27, 2008Publication date: March 24, 2011Applicant: Bayer CropScience AGInventors: Heike Hungenberg, Peter Baur, Ralf Nauen, Reiner Fischer, Udo Reckmann, Wolfgang Thielert
-
Publication number: 20110065766Abstract: The present invention relates, in part, to methods of treatment, prevention, and inhibition of viral disorders. In one aspect, the present invention relates to inhibition of the M2 proton channel of influenza viruses (e.g. influenza A virus) and other similar viroporins (e.g., VP24 of Ebola and Marburg viruses; and NS3 protein of Bluetongue). The present invention further relates, inter alia, to compounds which have been shown to possess antiviral activity, in particular, inhibiting the M2 proton channel of influenza viruses.Type: ApplicationFiled: September 13, 2010Publication date: March 17, 2011Inventors: Jizhou Wang, Xiaodong Fan, Lidia Cristian
-
Publication number: 20110059907Abstract: This invention relates to certain complexes of ascorbic acid and its derivatives with certain natural antioxidant and anti-inflammatory ketones for topical or oral application; said complexes having general chemical formula (I), its isomers, and salts thereof, including their optically active or racemic forms.Type: ApplicationFiled: November 16, 2010Publication date: March 10, 2011Applicant: Island Kinetics Inc.Inventors: SHYAM K. GUPTA, Linda Walker
-
Publication number: 20110059175Abstract: The present invention relates generally to use of a polyvinyl alcohol-polyethylene glycol graft copolymer (PVA-PEG graft co-polymer), such as Kollicoat IR, in the formulation of solid dispersions of low aqueous solubility and dissolution rate bioactive compound and, more particularly to a system and method for improving the solubility and dissolution rate of such low aqueous solubility and dissolution rate bioactive compound, in particular the drug of low aqueous solubility, such as a BCS Class II or Class IV drug compounds.Type: ApplicationFiled: April 10, 2007Publication date: March 10, 2011Applicant: K.U.LEUVEN RESEARCH AND DEVELOPMENTInventors: Sandrien Janssens, Guy Van Den Mooter
-
Publication number: 20110053883Abstract: The present invention provides an agent that modulates physiological condition of pests, wherein the agent has an ability to modulate the activity of an insect c-Jun NH2-terminal kinase; a method for assaying pesticidal activity of a test substance, which comprises a step of measuring the activity of a c-Jun NH2-terminal kinase in a reaction system in which the c-Jun NH2-terminal kinase contacts with a test substance, and the like.Type: ApplicationFiled: June 23, 2006Publication date: March 3, 2011Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Yasutaka Shimokawatoko, Mar Van De Craen, Irene Nooren, Sandra Turconi, Annelies Roobrouck, Wendy Maddelein
-
Publication number: 20110039700Abstract: The Invention discloses novel uses and methods for TSD directed to increasing the production potential of transgenic plants as well as methods for controlling unwanted animal pests on transgenic plants by application of the compounds to the transgenic plants or to propagation material of these plants.Type: ApplicationFiled: April 17, 2009Publication date: February 17, 2011Inventor: Reiner FISCHER
-
Publication number: 20110039701Abstract: The invention relates to novel compounds of the formula (I) in which X, Y, Z, A, B and G have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides. Moreover, the invention relates to selective herbicidal compositions comprising, firstly, the phenyl-substituted bicyclooctane-1,3-dione derivates 33 and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to increasing the activity of crop protection compositions comprising in particular phenyl-substituted bicyclooctane-1,3-dione derivates by adding ammonium salts or phosphonium salts and, if appropriate, penetrants, to the corresponding compositions, to processes for their preparation and to their use in crop protection as insecticides and/or acaricides and/or for preventing unwanted plant growth.Type: ApplicationFiled: March 30, 2010Publication date: February 17, 2011Applicant: Bayer CropScience AGInventors: Alfred ANGERMANN, Guido Bojack, Reiner Fischer, Stefan Lehr, Jan Dittgen, Dieter Feucht, Isolde Häuser-Hahn, Christopher Hugh Rosinger, Arnd Voerste
-
Publication number: 20110021549Abstract: The present invention relates to substituted benzofused derivatives, which can he used as vanilloid receptor ligands, method of treating diseases, conditions and/or disorders modulated by vanilloid receptors with them, and processes for preparing them.Type: ApplicationFiled: July 21, 2010Publication date: January 27, 2011Applicant: Glenmark Pharmaceuticals S.A.Inventors: Laxmikant Atmaram GHARAT, Uday Mukund JOSHI, Neelima KHAIRATKAR JOSHI
-
Publication number: 20110021624Abstract: Disclosed are a series of ?-amino-N-substituted amide compounds having a structure of the following formula, the pharmaceutically acceptable salts thereof, and the pharmaceutical composition comprising the same. The ?-amino-N-substituted amide compounds or the pharmaceutically acceptable salts thereof according to the present invention have anti-tumor and/or anti-cancer activities in vivo and in vitro, can effectively depress the growth of various tumor cells and/or cancer cells, and thus can be used in preparing drugs for treating tumors and/or cancers.Type: ApplicationFiled: December 11, 2008Publication date: January 27, 2011Inventors: Fajun Nan, Jia Li, Jian Ding, Gang Liu, Chuanming Xie, Zehong Miao, Wanyi Tai
-
Publication number: 20110021625Abstract: There is provided a neuronal cell death inhibitor having a high efficacy. A neuronal cell death inhibitor comprising a compound of general formula (1) below: (where R1 is a hydrogen atom or an optionally substituted hydroxy group; R2 is a hydrogen atom; R3 is a hydrogen atom or an optionally substituted hydroxy group; R4 is a hydrogen atom or an optionally substituted hydroxy group, R3 together with R4 is optionally an oxo group or a group of —O—(CH2)n—O— (where n is an integer of 2 to 4), or R2 together with R4 optionally forms an unsaturated bond between carbon atoms, the respective carbon atoms being attached to R2 and R4; R5 is a hydrogen atom or an optionally substituted lower alkyl group; each of R6, R7, and R8 is the same as or different from each other and is a hydrogen atom, an optionally substituted hydroxy group, an optionally substituted alkyl group, an optionally substituted aryl group, or an optionally substituted heteroaryl group); or a salt thereof.Type: ApplicationFiled: January 23, 2009Publication date: January 27, 2011Applicant: LEAD CHEMICAL CO., LTD.Inventors: Hideo Nemoto, Chihiro Tohda, Yuji Matsuya
-
Publication number: 20100330212Abstract: A skin-sensitizing formulation is provided in an edible, softgel pill. A person engaged in a sexual activity bites down on the pill, thereby effectuating the oral release of the skin-sensitizing formulation. This allows the skin-sensitizing formulation to be spread to a sexual partner, on any part of the skin or sexual region of the body preferably through oral contact with the partner. The skin-sensitizing substance is spread to the partner directly on the skin or through oral contact or beneath a condom worn by the partner. The skin-sensitizing formulation may include an essential mint oil, analog or derivative, and may further includes an enhancer, rubefacient, counterirritant, anesthetic, K-Opoid Receptor activator, or TRPM8 activator. Various inactive ingredients are also disclosed.Type: ApplicationFiled: June 29, 2010Publication date: December 30, 2010Inventor: Amy Grosso-Piacentino
-
Publication number: 20100297256Abstract: Compositions and methods for inhibiting integrin and treating integrin-related conditions, utilizing tellurium-containing compounds, are disclosed. The tellurium-containing compounds comprise at least one tellurium dioxo moiety and may have any one of Formulae I to IV as defined in the specification. Further disclosed are compositions and methods for treating a neoplastic condition characterized by a resistance to an anti-neoplastic agent and by a high level of expression of an integrin by neoplastic cells.Type: ApplicationFiled: November 23, 2008Publication date: November 25, 2010Inventors: Benjamin Sredni, Michael Albeck
-
Publication number: 20100297251Abstract: The present invention provides a system for delivery of an enteric coated active agent generally resistant to disintegration in an neutral environment having one or more active agents encapsulated by a polymer coating formed by chemical vapor deposition of one or more monomers on the one or more active agents to form a chemical vapor deposition polymer coating that controls the release of the one or more active agents in the gastrointestinal tract.Type: ApplicationFiled: May 21, 2010Publication date: November 25, 2010Applicants: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM, AEONCLAD COATINGS, LLCInventors: Richard B. Timmons, Ceren Susut, Donald E. Owens, III, J. Brian Windsor, Rachel Kennedy Khorzad
-
Publication number: 20100291231Abstract: The present invention relates to compositions which, in sprayable or form, are suitable as wound sealants for woody plants. The invention also relates to a method of protecting woody plants from infection with phytopathogenic fungi, in particular ESCA infection, using such wound sealants. These compositions comprise: a) a water-insoluble sealing agent in dissolved or dispersed form, which is selected among film-forming water-insoluble polymers, waxes and their mixtures; b) at least one plant protectant, c) at least one volatile diluent, in particular an aqueous diluent, and, if appropriate, d) at least one nonionic surface-active substance in an amount of from 10 to 100% by weight, in particular 10 to 80% by weight, based on the sealing agent.Type: ApplicationFiled: September 23, 2008Publication date: November 18, 2010Applicant: BASF SEInventors: Reinhold Stadler, Michael Vonend, Erich Birner, Heike Pfistner, Steffen Henkes, Michael Merk, Sven Harmsen, Egon Haden
-
Patent number: RE41998Abstract: Sympathetically maintained pain is treated topically by administering to the site where sympathetically maintained pain is present an ?-1-adrenergic antagonist, ?-2-adrenergic agonist, or other drug that depletes or blocks synthesis of sympathetic norepinephrine, known collectively as sympatholytic agents. Chemical formulas for several sympatholytic agents are given.Type: GrantFiled: May 5, 2005Date of Patent: December 14, 2010Assignee: Arclon Therapeutics, Inc.Inventor: James N. Campbell