Bicyclo Ring System Having The Hetero Ring As One Of The Cyclos (e.g., Methylenedioxyphenyl Group, Etc.) Patents (Class 514/464)
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Publication number: 20120241532Abstract: Disclosed herein are insect repellant formulations and dispensing systems which avoid the need for synergists while still using highly effective pyrethrin repellant compounds. The formulations preferably are presented in aerosol form.Type: ApplicationFiled: March 24, 2011Publication date: September 27, 2012Inventors: Kent M. Palkki, Murthy S. Munagavalasa
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Publication number: 20120232071Abstract: The present invention relates to compounds of formula I wherein R1a to R1e, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.Type: ApplicationFiled: May 22, 2012Publication date: September 13, 2012Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
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Patent number: 8263647Abstract: The present invention provides a new composition for treating pain-associated sleep disturbances, especially shortened sleep duration, comprising ibuprofen and diphenhydramine. The composition is further prepared as a bilayer tablet or caplet, or alternatively as a soft gelatin capsule composition, to prevent interaction between the active ingredients.Type: GrantFiled: April 10, 2008Date of Patent: September 11, 2012Assignee: Wyeth LLCInventors: Graham D. Cook, Todd S. Koch, David H. Giamalva, Justin Bianco, James J. Fort, Geraldine Doyle, Steven Cooper
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Publication number: 20120208874Abstract: A composition comprising an alkynyl phenoxy compound of Formula (I) as a synergist and a pesticidal active ingredient is described, wherein R1 and R2, similar or different, are (C1-C4)alkyl or R1O— and R2O— together represent a group —O—CH2—O—, —O—CH(CH3)—O, —O—CH2—CH2—O—, —O—CH2—CH2—, R3 is (C1-C6)alkyl, (C3-C6)alkenyl or —B—(CH2-CH2—O)z-R6 where B is —CH2—O— or —O—, z is 0, 1 or 2 and R6 is (C1-C4)alkyl; R4 is hydrogen or methyl; R5 is hydrogen or methyl; x is an integer from 1 to 2; y is 0, 1 or 2; with the proviso that when R3 is —B—(CH2CH2—O)z-R6, y is 1 and 5-(propargyloxy)-benzo[1,3]dioxole is excluded.Type: ApplicationFiled: August 18, 2010Publication date: August 16, 2012Inventors: Valerio Borzatta, Elisa Capparella, Leni Moroni, Graham Moores, Despina Philippou
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Publication number: 20120190738Abstract: The present invention relates to compounds of general formula I for the treatment of malignancy by inhibition of PI3-Akt pathway and or induction of NO. The present invention also relates to the use of compound of general formula I for the treatment of malignancy by inhibition of PI3-Akt pathway and or induction of NO. The present invention further relates to a method of treating malignancy by inhibition of PI3-Akt pathway and or induction of NO by administration of compound or said composition to a mammal in need thereof.Type: ApplicationFiled: January 12, 2010Publication date: July 26, 2012Inventors: Santu Bandyopadhyay, Bikas Chandra Pal, Jaisankar Parasuraman, Siddhartha Roy, Jayashree Bagchi Chakrabotry, Indrani Choudhury Mukherjee, Sanjit Kumar Mahato, Aditya Konar, Srabanti Rakshit, Labanya Mandal, Dipyaman Ganguly, Kausik Paul, Anirban Manna, Jayaraman Vinayagam, Churala Pal
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Patent number: 8227512Abstract: The present invention relates to a pharmaceutical composition for the prevention and treatment of cancer comprising daurinol as an active ingredient, more precisely a pharmaceutical composition for the prevention and treatment of cancer comprising daurinol isolated from the medicinal plant of Mongolia, Haplophyllum dauricum or Haplophyllum cappadocicum, as an active ingredient. Daurinol can selectively block the S phase of cancer cell cycle to disturb the cycle and induce apoptosis stepwise, resulting in anticancer effect. Therefore, daurinol of the present invention can be used as a positive control chemical in the research and development field of cancer biology especially for cancer therapy and prevention. Daurinol also can be a promising candidate for a novel cell cycle blocker and a novel apoptosis inducer which could be effectively used for the prevention and treatment of cancer in the end.Type: GrantFiled: October 10, 2007Date of Patent: July 24, 2012Assignee: Korea Institute of Science and TechnologyInventors: Chu Won Nho, Kyung Su Kang, Saet Byoul Lee, Batsuren Dulamjav, Tunsag Jigjidsuren
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Publication number: 20120129818Abstract: Ortho methoxy phenolic compounds are provided that include methylenedioxyphenyl ferulate and ferulylproline and derivatives thereof. Pharmaceutical compositions comprising the compounds and methods of using the compounds for treating cardiovascular diseases, including hypertension, atherosclerosis, coronary heart disease, angina, stroke, and myocardial infarction, are further provided. The compounds are also useful in reducing low-density lipoprotein oxidation, improving or increasing vasodilation, and reducing plaque destabilization in a subject.Type: ApplicationFiled: April 23, 2010Publication date: May 24, 2012Inventor: Desikan Rajagopal
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Publication number: 20120121681Abstract: An insecticidal polymer matrix containing Piperonyl Butoxide (PBO) and deltamethrin (DM), wherein the ratio between the content of PBO and the content of DM in terms of weight is higher than 3.Type: ApplicationFiled: July 23, 2009Publication date: May 17, 2012Inventors: Mikkel Vestergaard Frandsen, Michael Stanley Pedersen, Matthieu Zellweger, Sebastien Gouin, Sicco Dirk Roorda, Thi Quynh chi Phan
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Publication number: 20120122970Abstract: The present invention includes insecticidal carbamates that are useful, for example, for the control of insects, such as mosquitoes, which can be used in applications where exposure to and/or contact with humans is likely. The insecticides of the present invention include phenyl N-methyl carbamates and compositions comprising them that exhibit species-selective inhibition of acetylcholinesterase (AChE) and are preferably toxic to mosquitoes but not humans. Of particular interest are compounds of Formula (I) and Formula (II): Compounds of Formula (I) and Formula (II) are especially suitable for insecticide treated nets and indoor residual spraying for mosquito control.Type: ApplicationFiled: January 26, 2012Publication date: May 17, 2012Inventors: Paul Carlier, Jeffrey Bloomquist, Sally Paulson, Eric Wong
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Publication number: 20120095092Abstract: The invention provides a compound of formula (I), a pharmaceutical composition thereof, a method of preparing a medicament for the treatment of a cancer, and a method of treating cancers. The invention exhibits merits against cancers such as significantly higher potency and effectiveness over a broader range of cancers. In formula (I), Ra is a benzyl group with alkyl and/or alkoxy; Rb is selected from H and alkyl groups; Rf is an alkyl; and R3 is selected from a substituted phenyl, a heterocyclic group, and wherein Rc is selected from a fused ring, fused rings, and any bivalent cyclic group.Type: ApplicationFiled: October 18, 2010Publication date: April 19, 2012Inventors: Bin Su, Aimin Zhou, Yan Xu
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Patent number: 8158664Abstract: The present invention relates to a method of treatment and/or prophylaxis of a microbial infection, comprising the step of administering an effective amount of a compound of formula (I), in which X and Y are either the same or different and selected from a heteroatom; is a double or single bond depending on the heteroatoms X and Y; R1 to R5 are either the same or different and selected from hydrogen or a non-deleterious substituent; and R6 and R7 are either the same or different and selected from hydrogen and a non-deleterious substituent or one of R6 and R7 are absent when there is a double bond present, pharmaceutically acceptable salts or derivatives, pro-drugs, tautomers and/or isomers thereof. The present invention also relates to a method for protecting a subject from radiation damage, a method of cancer radiotherapy and use as an antimicrobial or radioprotective agent of the compound of formula (I) defined above.Type: GrantFiled: May 10, 2010Date of Patent: April 17, 2012Assignee: Biodiem Ltd.Inventors: Peter Prokofievich Denisenko, Nikolay Sergeevich Sapronov, Alexander Alexandrovich Tarasenko
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Patent number: 8153685Abstract: The present invention provides new salts and/or addition compounds and/or complex compounds of guanidinoacetic acid with malic acid, aspartic acid, ascorbic acid, succinic acid, pyruvic acid, fumaric acid, gluconic acid, ?-ketoglutaric acid, oxalic acid, pyroglutamic acid, 3-nicotinic acid, lactic acid, citric acid, maleic acid, sulfuric acid, acetic acid, formic acid, 2-hydroxybenzoic acid, L-carnitine, acetyl-L-carnitine, taurine, betaine, choline, methionine and lipoic acid as well as in the form of sodium, potassium or calcium guanidinoacetate. These salts have improved physiological and therapeutic properties and are particularly suitable for use as dietary supplements, as animal feeds and in cosmetic or dermatological preparations in which especially the marked stability and good bioavailability of the salts come to the fore.Type: GrantFiled: March 2, 2006Date of Patent: April 10, 2012Assignee: Alzchem Trostberg GmbHInventors: Thomas Gastner, Hans-Peter Krimmer
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Publication number: 20120077875Abstract: The present invention relates to a composition, in particular an antibacterial drug, including trans-cinnamaldehyde, a pharmaceutical composition including trans-cinnamaldehyde for treatment or prevention, in particular, of a nosocomial infection, specifically caused by a bacteria resistant to anti-bacterial drugs, the use of trans-cinnamaldehyde as an anti-bacterial agent and a method for preparing a surface including the application of a composition according to the invention.Type: ApplicationFiled: June 7, 2010Publication date: March 29, 2012Applicant: SEPTEOSInventor: Nicolas Tesse
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Publication number: 20120071523Abstract: The instant invention provides novel benzofuran-4,5-diones and pharmaceutical compositions thereof useful for inhibiting PDF and for treating proliferative and infectious diseases. Compounds may be selective for eukaryotic (e.g., human) PDF or prokaryotic PDF.Type: ApplicationFiled: May 5, 2010Publication date: March 22, 2012Applicant: Sloan-Kettering Institute for Cancer ResearchInventors: Hakim Djaballah, Christophe Antczak
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Publication number: 20120045531Abstract: Provided are methods of treating cellulite, the methods comprising applying to skin in need of cellulite treatment a composition comprising paulownin or an extract of Paulownia wood.Type: ApplicationFiled: August 17, 2011Publication date: February 23, 2012Inventors: Khalid Mahmood, Thierry Oddos
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Patent number: 8114905Abstract: The present invention provides an essentially pure compacted 2,2-Dibromo-3-nitrilopropionamide (DBNPA) in a granular and/or tablet and/or briquette and/or pellet form. The present invention further provides a process for preparing the same essentially pure compacted DBNPA.Type: GrantFiled: March 17, 2009Date of Patent: February 14, 2012Assignee: Bromine Compounds LimitedInventors: Michael Lupin, Ayala Lupin, legal representative, David Feldman
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Publication number: 20120029069Abstract: This invention relates to a novel compound extracted from antrodia Cinnamomea and related compounds of formula (1), and pharmaceutical compositions comprising the compound of formula (1) and a pharmaceutically acceptable carrier or excipient. The invention further comprises the method of inhibit cancer cells by administering an effective amount of the compound of formula (1).Type: ApplicationFiled: May 6, 2011Publication date: February 2, 2012Inventors: Ching-Kuo Lee, Pi-Yu Chen, Jir-Mehng Lo, Wen-Bin Zhong, Tien-Wang Chiu, Chieh-Chou YU
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Patent number: 8088820Abstract: This invention provides a method for treating or preventing malaria in a subject. The method includes administering to the subject an effective amount of a substituted tetracycline compound, such that malaria is treated or prevented. In one aspect, the invention relates to pharmaceutical compositions which include an effective amount of a tetracycline compound to treat malaria in a subject and a pharmaceutically acceptable carrier. The substituted tetracycline compounds of the invention can be used to in combination with one or more anti-malarial compounds or can be used to treat or prevent malaria which is resistant to one or more other anti-malarial compounds.Type: GrantFiled: October 24, 2003Date of Patent: January 3, 2012Assignee: Paratek Pharmaceuticals, Inc.Inventors: Michael Draper, Mark L. Nelson
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Patent number: 8076324Abstract: The present invention relates to di(hetero)arylcyclohexane derivatives of the formula I, in which Ar1, Ar2, R1 and R2 have the meanings indicated in the claims. The compounds of the formula I are valuable pharmaceutical active compounds which inhibit ATP-sensitive potassium channels in the heart muscle and are suitable, for example, for the treatment of disorders of the cardiovascular system such as arrhythmias or a decreased contractility of the heart, such as can occur, for example, in coronary heart disease, cardiac insufficiency or cardiomyopathies. In particular, they are suitable for the prevention of sudden cardiac death. The invention furthermore relates to processes and intermediates for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: GrantFiled: December 3, 2009Date of Patent: December 13, 2011Assignee: Sanofi-AventisInventors: Thomas Bohme, Uwe Gerlach, Dirk Gretzke, Heinz-Werner Kleemann, Stefania Pfeiffer-Marek, Henning Vollert, Jean-Michel Altenburger, Sergio Mallart
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Patent number: 8058309Abstract: The present invention provides new tyrphostin derivatives acting as substrate competitive protein tyrosine kinase (PTK) inhibitors and receptor tyrosine kinase (RTK) inhibitors, methods of their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds and compositions, especially as chemotherapeutic agents for preventions and treatments of PTK and RTK related disorders such as metabolic, fibrotic, and cell proliferative disorders, in particular psoriasis and cancer.Type: GrantFiled: December 4, 2007Date of Patent: November 15, 2011Assignee: Novotyr Therapeutics Ltd.Inventors: Hadas Reuveni, Alexander Levitzki, Lilach Steiner, Revital Sasson, Iris Ben-David, Avi Weissberg
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Publication number: 20110274677Abstract: An organic pest control product comprising nutmeg oil and D-limonene is disclosed. In some embodiments the organic pest control product further comprises a miscibility enhancer to enhance the effectiveness of the product. In some embodiments the miscibility enhancer can comprise a liquid soap or detergent. Additional formulations that comprise cassia oil and/or eucalyptus oil are also disclosed. A method of use of an organic pest control product is also disclosed, in which the organic pest control product is effective to control a wide range of biological pests including fungi, bacteria, and insects, including those responsible for Dutch Elm Disease, fire blight, and Colony Collapse Disorder.Type: ApplicationFiled: October 31, 2008Publication date: November 10, 2011Inventors: Bob Mullen, Linda Louise Mullen
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Publication number: 20110263567Abstract: The present invention relates to compounds of general formula (i) having an oxime moiety or a pharmaceutically acceptable salt, hydrate or solvate thereof and its use for inhibiting semicarbazide-sensitive amine oxidase (SSAO), also known as vascular adhesion protein-1 (VAP-1), a pharmaceutical composition comprising the compound or a salt, hydrate or solvate thereof as an active ingredient, a method for the prevention or the treatment of a SSAO/VAP-1 related disease, said diseases including acute or chronic inflammatory diseases, diseases related to carbohydrate metabolism, diabetes-associated complications, diabetic retinopathy and macular oedema, diseases related to adipocyte or smooth muscle dysfunctions, neurodegenerative diseases and vascular diseases.Type: ApplicationFiled: September 11, 2009Publication date: October 27, 2011Applicant: Semmelweis EgyetemInventors: Péter Mátyus, Kálmán Magyar, Marjo Pihlavisto, Klára Gyires, Norbert Haider, Yinghua Wang, Patrick Woda, Petra Dunkel, Éva Tóth-Sarudy, Gÿorgy Túrós
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Patent number: 8039491Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: GrantFiled: January 7, 2010Date of Patent: October 18, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara S. Hadida Ruah, Mark T. Miller, Brian Bear, Jason McCartney, Peter D. J. Grootenhuis
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Publication number: 20110250166Abstract: The present invention relates to a combined preparation comprising at least one rocaglamide derivative and at least one apoptosis inducing agent, preferably from the group of substances comprising agents inducing the extrinsic apoptotic pathway, antiproliferative agents and agents which induce apoptosis in T-cells by activation induced cell death (AICD) for the treatment of cancer.Type: ApplicationFiled: November 20, 2009Publication date: October 13, 2011Applicant: DKFZ DEUTSCHES KREBSFORSCHUNGSZENTRUMInventors: Min Li-Weber, Peter H. Krammer
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Publication number: 20110217397Abstract: The present invention comprises compositions, methods and cell lines related to controlling insects. An embodiment of a composition comprises a plant essential oil and targets at least one receptor of insects chosen from tyramine receptor, Or83b olfactory receptor, and Or43a olfactory receptor, resulting in a change in the intracellular levels of cAMP, Ca2+, or both in the insects.Type: ApplicationFiled: February 3, 2011Publication date: September 8, 2011Applicant: Tyra Tech, Inc.Inventor: Essam Enan
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Patent number: 8013012Abstract: The present invention relates to spiroketal compounds that are useful in methods of treating or preventing protozoal infections, parasitic infections, bacterial infections, cell proliferative disorders and anti inflammatory disorders. The spiroketal compounds are also useful as immunosuppressive agents, and also in methods of controlling pests.Type: GrantFiled: December 22, 2006Date of Patent: September 6, 2011Assignee: EcoBiotics LtdInventors: Paul Warren Reddell, Victoria Anne Gordon
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Publication number: 20110190325Abstract: Embodiments of the present invention provide compounds (such as Formula (I) compounds, Formula (II) compounds, and various embodiments thereof). Compositions comprising those compounds are also provided. Methods for their preparation are included. Also, uses of the compounds are included, such as administering and treating diseases (e.g., cancer and infections).Type: ApplicationFiled: August 14, 2009Publication date: August 4, 2011Inventors: Gerald B. Hammond, Jose C. Aponte, Robert H. Gilman, Michel Henri Auguste Sauvain, Abraham Caisberg
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Publication number: 20110178171Abstract: A method of inhibiting the cellular proliferation of at least one selected from the group consisting of androgen dependent prostate cancer cells, androgen independent prostate cancer cells, oral cancer cells, liver cancer cells (hepatoma), and gastric cancer cells in a subject is provided, wherein the method comprises administrating to the subject an effective amount of an active component selected from the group consisting of Z form isochaihulactone (Z-K8) of the following formula (I), E form isochaihulactone (E-K8) of the following formula (II), a pharmaceutically acceptable salt of Z-K8 or E-K8, a pharmaceutically acceptable ester of Z-K8 or E-K8, and combinations thereof: and R is H, alkoxy, or aryl. Also provided is a method for manufacturing Z-K8 and E-K8.Type: ApplicationFiled: January 18, 2011Publication date: July 21, 2011Applicant: China Medical UniversityInventors: Yi-Lin CHEN, Horng-Jyh Harn, Shinn-Zong Lin, Tzyy-Wen Chiou, Cheng-Tung Lin
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Publication number: 20110160276Abstract: A compound has Formula VIII where, X is —C(O)R, —C(O)OR, —CN, —NO2, —S(O)2R?, —P(O)(OR)2; each R is individually H, alkyl, or alkenyl; R? is alkyl or akenyl; R1 is aryl, alkenyl, arylalkenyl, heterocyclyl, or heteroaryl; and R2, R3, R4, R5, R6, R7, R8, R9, R10, and R11 are individually H, alkoxy, or hydroxy. In some cases, X is NO2. Pharmaceutical compositions of the compound of Formula VIII with a pharmaceutically acceptable carrier may be prepared. The compounds may be used for inhibition of cyclooxygenase-2.Type: ApplicationFiled: March 4, 2010Publication date: June 30, 2011Inventors: Irishi N.N. Namboothiri, Narasimham Ayyagari, Deena Jose
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Publication number: 20110159061Abstract: A wipe article comprising a lotion composition comprising omega-6 fatty acid. A method of improving skin barrier function of vulvar skin comprising the step of contacting the vulvar skin with a wipe article, wherein omega-6 fatty acid is disposed on the surface of the wipe article.Type: ApplicationFiled: December 21, 2010Publication date: June 30, 2011Inventor: Raphael WARREN
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Publication number: 20110160228Abstract: The present invention relates to compounds of formula (I) below in which: —R1 and R3 represent, independently of one another, a methoxy group optionally substituted by one or more fluorine atoms, —R2 and R4 represent, independently of one another, a hydrogen atom or a methoxy group optionally substituted by one or more fluorine atoms, —A represents a ring chosen from the group comprising aryl and heteroaryl groups, said ring possibly being substituted by or fused to a heterocycle, —X represents a nitrogen atom or a CH group, and —Z1 represents a hydrogen atom or a halogen atom, preferably fluorine, and —Z2 represents a hydrogen atom, a halogen atom, preferably fluorine, a C1 to C4 alkyl group, an aryl group or a —CN, —SO2NR12R13, —SO2R9, —COOR15 or —COR15 group, and also to the pharmaceutically acceptable salts thereof, the isomers thereof and the prodrugs thereof.Type: ApplicationFiled: June 4, 2009Publication date: June 30, 2011Inventors: Mouâd Alami, Samir Messaoudi, Abdallah Hamze, Olivier Provot, Jean-Daniel Brion, Jian-Miao Liu, Jérôme Bignon, Joanna Bakala
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Publication number: 20110135764Abstract: Embodiments of the invention relate to a composition for controlling a target pest, wherein the composition includes at least two active ingredients selected from the group consisting of thymyl acetate, linalyl acetate, amyl butyrate, anise star oil, black seed oil, p-cymene, geraniol, isopropyl myristate, d-limonene, linalool, lilac flower oil, methyl salicylate, alpha-pinene, piperonal, piperonyl alcohol, tetrahydrolinalool, thyme oil white, thyme oil red, thymol, vanillin, and winter-green oil, wherein the composition causes synergistic control of the target pest.Type: ApplicationFiled: March 19, 2009Publication date: June 9, 2011Applicant: TyraTech, Inc.Inventor: Essam Enan
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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
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Publication number: 20110118346Abstract: The present invention relates to a new use of lignan-type compounds or an extract of nutmeg or aril of nutmeg comprising the same. More particularly, the present invention relates to a composition for skin whitening comprising a lignan-type compound or an extract of nutmeg or aril of nutmeg comprising the same. Because the lignan compound represented by Chemical Formulas 1 to 3 or the extract of nutmeg or aril of nutmeg has superior skin whitening activity by inhibiting melanin production and tyrosinase activity, it can be used for the preparation of a cosmetic composition, food composition or pharmaceutical composition for skin whitening.Type: ApplicationFiled: October 17, 2008Publication date: May 19, 2011Applicants: BIOCARE CO., LTD., NEWTREE CO., LTD.Inventors: Jae Kwan Hwang, Yu-Mi Cho, Gyu Hoi Kim, Jeong Hwan Kim, Hae Ji Lee, Do Un Kim, Hee Chul Chung, Jae Youn Chung, Hyun In Oh
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Patent number: 7943663Abstract: To provide a process and an apparatus by means of which a composition that contains episesamin in a concentration greater than 50 wt % on the basis of the sum weight of sesamin and episesamin can be produced conveniently and at high yield. There are provided a process and an apparatus which comprise the step of applying epimerization to sesamin or a sesamin-containing composition so that at least part of the sesamin is converted to episesamin and the step of selectively crystallizing episesamin by recrystallization and by means of which a composition that contains episesamin in a concentration greater than 50 wt % can be produced conveniently and at high yield.Type: GrantFiled: September 29, 2006Date of Patent: May 17, 2011Assignee: Suntory Holdings LimitedInventors: Yukihiro Aoshima, Masaaki Nakai, Kenji Katano, Asako Okada
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Patent number: 7939528Abstract: The present invention relates to novel compounds which are antagonist or inverse agonists at an opioid receptor. Such compounds are useful in the treatment of obesity and related diseases and/or conditions in mammals, particularly humans. Methods of making and using such compounds are also disclosed.Type: GrantFiled: October 12, 2006Date of Patent: May 10, 2011Assignee: GlaxoSmithKline LLCInventors: Kevin Karl Barvian, Jason Daniel Speake, David John Cowan, Andrew Lamont Larkin, Jerzy Ryszard Szewczyk
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Patent number: 7928137Abstract: Compounds of formula I in which R1, R2, R3, each X, L, Y, Cy, Lp, D and n have the meanings as set out in the specification, and corresponding compounds in which the unsubstituted or substituted amidine group is replaced with an unsubstituted or substituted aminomethyl group, are useful as serine protease inhibitors.Type: GrantFiled: March 2, 2007Date of Patent: April 19, 2011Assignee: Tularik LimitedInventors: John Walter Liebeschuetz, William Alexander Wylie, Bohdan Waszkowycz, Christopher William Murray, Andrew David Rimmer, Pauline Mary Welsh, Stuart Donald Jones, Jonathan Michael Ernest Roscoe, Stephen Clinton Young, Phillip John Morgan
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Publication number: 20110071221Abstract: Disclosed is a method for treating PPAR (peroxisome proliferator activated receptor)mediated diseases, such as diabetes mellitus and diabetic complications, which includes administering to a subject an effective amount of macelignan represented by the following Formula (I): or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: June 27, 2006Publication date: March 24, 2011Inventors: Jae-Kwan Hwang, Kyu-Lee Han, Jong-Hee Sohn, Ah-Jin Kim, Jeong-Han Choo, Jae-Young Lee, Jeong-Hwan Kim, Do Un Kim, Heechul Chung, Jae Youn Chung
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Patent number: 7902254Abstract: Disclosed is a method for treating PPAR (peroxisome proliferator activated receptor)-mediated diseases, such as diabetes mellitus, which includes administering to a subject an effective amount of macelignan represented by the following Formula (I): or a pharmaceutically acceptable salt thereof.Type: GrantFiled: June 27, 2006Date of Patent: March 8, 2011Assignee: Newtree Co., Ltd.Inventors: Jae-Kwan Hwang, Kyu-Lee Han, Jong-Hee Sohn, Ah-Jin Kim, Jeong-Han Choo, Jae-Young Lee, Jeong-Hwan Kim, Do Un Kim, Heechul Chung, Jae Youn Chung
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Publication number: 20110046138Abstract: A series of novel compounds showing anticonvulsant activity is described. Such pharmaceutically active compounds may also show utility in the treatment of other central nervous system (“CNS”) diseases and disorders, such as anxiety, depression, insomnia, migraine headaches, schizophrenia, Parkinson's disease, spasticity, Alzheimer's disease, and bipolar disorder. Furthermore, such compounds may additionally find utility as analgesics (e.g., for the treatment of chronic or neuropathic pain) and as neuroprotective agents useful in the treatment of stroke(s), chronic neurodegenerative diseases (such as Alzheimer's disease and Huntington's disease), and/or traumatic brain and/or spinal cord injuries. Moreover, these/such compounds may also be useful in the treatment of status epilepticus and/or as chemical countermeasures.Type: ApplicationFiled: March 18, 2009Publication date: February 24, 2011Inventors: Amir Pesyan, Manuel M. Balandrin
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Patent number: 7893282Abstract: 7-substituted fused ring tetracycline compounds, methods of treating tetracycline responsive states, and pharmaceutical compositions containing the 7-substituted fused ring tetracycline compounds are described.Type: GrantFiled: October 10, 2007Date of Patent: February 22, 2011Assignee: Paratek Pharmaceuticals, Inc.Inventors: Mark L. Nelson, Laura Honeyman
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Patent number: 7868204Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.Type: GrantFiled: March 25, 2005Date of Patent: January 11, 2011Assignee: MethylGene Inc.Inventors: Daniel Delorme, Soon Hyung Woo, Arkadii Vaisburg, Oscar Moradei, Silvana Leit, Stephane Raeppel, Sylvie Frechette, Giliane Bouchain
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Patent number: 7868004Abstract: A compound of the formula I in which X and Y are selected as follows: (i) X is H and Y is selected from the group consisting of (ii) X and Y together form a bivalent radical selected from the group consisting of —O—CH2—O—, —N?CH—O— and —N?CH—S— thus forming together with the carbon atoms to which the radical is attached a 5-membered ring. The compounds have cooling properties and are useful in, for example, foodstuffs, dentifrices and cosmetics.Type: GrantFiled: February 23, 2006Date of Patent: January 11, 2011Assignee: Givaudan S.A.Inventors: Lucienne Cole, Stefan Michael Furrer, Christophe C. Galopin, Pablo Victor Krawec, Adam Mazur, Jay Patrick Slack
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Publication number: 20110002866Abstract: The described invention relates to delivery of compositions comprising at least one prostaglandin analog to prevent or reduce hair loss (e.g. brittle hair growth, thin hair growth, short hair growth, sparse hair growth) or alopecia associated with chemotherapy.Type: ApplicationFiled: September 14, 2010Publication date: January 6, 2011Inventors: Beverly W. Lubit, Pamela R. Lipkin
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Publication number: 20100316631Abstract: The present disclosure describes the design and synthesis of a novel class of water soluble curcumin-based compounds. These water soluble curcumin-based compounds are shown to provide superior cell killing activity and exhibit increased and cell internalization solubility in aqueous solutions as compared to the free (unconjugated) curcumin. The present disclosure provides compositions for the treatment or prevention of a variety of disease states or conditions, such as but not limited to, cancer, other cell hyperproliferative disorders and chronic inflammatory conditions, said compositions comprising a water soluble curcumin-based compound.Type: ApplicationFiled: October 19, 2007Publication date: December 16, 2010Applicant: THE UAB RESEARCH FOUNDATIONInventor: Ahmad Safavy
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Publication number: 20100311665Abstract: Composition and methods of treating pain and reducing or reversing tolerance to opiate analgesics are disclosed. The composition and method utilize an opiate analgesic and an endothelin antagonist as active agents to treat pain in mammals, including humans.Type: ApplicationFiled: August 2, 2010Publication date: December 9, 2010Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOISInventor: Anil Gulati
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Publication number: 20100303940Abstract: Pest control compositions, blends, and formulations are disclosed. The blends contain, in a synergistic combinations, at least two ingredients such as Lilac Flower Oil, D-Limonene, Thyme Oil, Lime Oil, Black Seed Oil, Wintergreen Oil, Linalool, Tetrahydrolinalool, Vanillin, Isopropyl myristate, Piperonal (aldehyde), Geraniol, Geraniol 60, Triethyl Citrate, and Methyl Salicylate.Type: ApplicationFiled: March 21, 2008Publication date: December 2, 2010Applicant: TYRATECH, INC.Inventor: Essam Enan
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Publication number: 20100298347Abstract: Substituted 2-naphthoic acids of structural formula are effective as antagonists of the biological activity of GPR105 protein. They are useful for the treatment, control or prevention of disorders responsive to antagonism of this receptor, such as diabetes, particularly, Type 2 diabetes, insulin resistance, hyperglycemia, lipid disorders, obesity, atherosclerosis, and conditions associated with the Metabolic Syndrome.Type: ApplicationFiled: December 1, 2008Publication date: November 25, 2010Applicant: MERCK FROSST CANADA LTDInventors: Michel Belley, Denis Deschenes, Rejean Fortin, Jean-Francois Fournier, Sebastien Gagne, Yves Gareau, Jacques Yves Gauthier, Lianhai Li, Joel Robichaud, Michel Therien, Geoffrey K. Tranmer, Zhaoyin Wang
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Publication number: 20100285154Abstract: The present invention relates to the use of lignan compounds for treating or preventing an inflammatory disease. More particularly, it relates to a method for preventing or treating an inflammatory disease, comprising administering to a subject in need thereof an effective amount of macelignan represented by Chemical Formula I or a pharmaceutically acceptable salt thereof. The lignan compound has the effect of inhibiting inflammatory reactions by inhibiting the production or expression of inflammation mediators NO, iNOS, PGE2, COX-2 and TNF-? and by treating or preventing inflammatory disease in vivo. Accordingly, the lignan compound or a Myristica fragrans extract will be highly useful for the treatment or prevention of an inflammatory disease.Type: ApplicationFiled: April 23, 2010Publication date: November 11, 2010Applicants: NEWTREE INDUSTRY CO., LTD., Jae-KwanInventors: Jae-Kwan Hwang, Do-Un Kim, Jae-Youn Chung, Hee-Chul Chung, Kyu-Lee Han
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Publication number: 20100285960Abstract: A method for regulating the release rate of microencapsulated actives comprising: 1a) addition or subtraction of piperonylbutoxide (PBO), component B) to 2a) formulations A) comprising at least one microencapsulated active having agrochemical activity, optionally PBO outside the microcapsule, 3a) dilution by water of component A) and/or component B) until the active application dose, the ratio by weight PBO/active ranges from 0.1 to 80, the PBO subtraction being feasible only when the PBO is present outside the microcapsule of the formulation A).Type: ApplicationFiled: December 23, 2008Publication date: November 11, 2010Applicant: ENDURA S.p.A.Inventors: Carlotta Gobbi, Lucio Bassetti, Valerio Borzatta