1,2-oxazoles (including Hydrogenated) Patents (Class 514/378)
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Patent number: 8623896Abstract: A compound of formula (I), wherein A1, A2, A3, A4, G1, L, R1, R2, R3, R4, Y1, Y2 and Y3 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control insect, acarine, mollusc and nematode pests.Type: GrantFiled: December 16, 2008Date of Patent: January 7, 2014Assignee: Syngenta Crop Protection, LLCInventors: Peter Renold, Werner Zambach, Peter Maienfisch, Michel Muehlebach
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Patent number: 8623875Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein A is a 6-membered aromatic ring containing carbon atoms and 0-3 nitrogen atoms as ring members, said ring optionally substituted with 1-5 substituents independently selected from R2; R1 is C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C4-C7 alkylcycloalkyl or C4-C7 cycloalkylalkyl, each optionally substituted with one or more substituents independently selected from R21; R21 is independently H, halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfonyl, CN or NO2; and Q is as defined in the disclosure.Type: GrantFiled: June 10, 2008Date of Patent: January 7, 2014Assignee: E.I. du Pont de Nemours and CompanyInventors: George Philip Lahm, Ty Wagerle, Ming Xu
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Publication number: 20140005221Abstract: The present invention relates to a compound that has URAT1 inhibitory action, and a URAT1 inhibitor, a blood uric acid level-reducing agent and a pharmaceutical composition comprising the compound. More specifically, the present invention relates to a compound represented by Formula (I) below.Type: ApplicationFiled: January 30, 2012Publication date: January 2, 2014Applicant: SATO PHARMACEUTICAL CO., LTD.Inventors: Keita Nagai, Koh Nagasawa, Hirobumi Takahashi, Motoaki Baba, Shinichi Fujioka, Eri Kondoh, Kenichi Tanaka, Yoshiki Itoh
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Patent number: 8618147Abstract: Provided are various compounds of Formula I (I). Also provided are various compounds of Formula II (II). Also provided are pharmaceutical compositions comprising the above compounds. Additionally, methods of inhibiting macrophage migration inhibitory factor (MIF) activity in a mammal are provided, as are methods of treating or preventing inflammation in a mammal. Further provided are methods of treating a mammal having sepsis, septicemia, and/or endotoxic shock. Also provided are methods of treating a mammal having an autoimmune disease, and methods of treating a mammal having a tumor.Type: GrantFiled: January 28, 2013Date of Patent: December 31, 2013Assignee: The Feinstein Institute for Medical ResearchInventor: Yousef Al-Abed
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Patent number: 8618138Abstract: This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterized by cytotoxic ?-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds.Type: GrantFiled: June 11, 2010Date of Patent: December 31, 2013Assignees: Katholieke Universiteit Leuven, K.U. Leuven R&D, reMYNDInventors: Gerard Griffioen, Tom Van Dooren, Veronica Rojas De La Parra, Arnaud Marchand, Sara Allasia, Amuri Kilonda, Patrick Chaltin
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Publication number: 20130345196Abstract: This invention relates generally to compounds that are glucuronidase inhibitors. The glucuronidase inhibitors include phenoxy thiophene sulfonamides, and other compounds such as pyridine sulfonyls, benzene sulfonyls, thiophene sulfonyls, thiazole sulfonyls, thiophene carbonyls, and thiazole carbonyls. These compounds include nialamide, isocarboxazid, phenelzine, amoxapine, loxapine and mefloquine. Also compositions including one or more of such compounds for use in inhibiting glucuronidase and methods of using one or more of such compounds for selective inhibition of bacterial ?-glucuronidase. These compounds may be used as a co-drug in combination with the anticancer drug CPT-11. Also a method for screening compounds to determine their usefulness in reducing diarrhea associated with irinotecan chemotherapy.Type: ApplicationFiled: May 24, 2012Publication date: December 26, 2013Inventors: Alfred L. WILLIAMS, John Scott, Li-An Yeh, Matthew Robert Redinbo
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Publication number: 20130345222Abstract: The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.Type: ApplicationFiled: May 17, 2013Publication date: December 26, 2013Inventors: Donald S. Karanewsky, Joseph R. Fotsing, Catherine Tachdjian, Melissa Arellano
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Publication number: 20130345221Abstract: The invention relates to new isoxazoline compounds of formula wherein the variables have the meaning as indicated in the claims; in free form and in salt form; and optionally the enantiomers and geometrical isomers thereof. The compounds of formula (I) are useful in the control of parasites, in particular ectoparasites, in and on vertebrates.Type: ApplicationFiled: March 9, 2012Publication date: December 26, 2013Applicant: NOVARTIS AGInventors: Noëlle Gauvry, Steve Nanchen
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Publication number: 20130338158Abstract: The invention provides compounds represented by the formula I, each of which compounds may have sphingosine-1-phosphate receptor agonist and or antagonist biological activity: and wherein the variables Y, R4, n, o, A, A1, A2, X, Z, R1, R3, R2, p, q and r are as defined in the specification.Type: ApplicationFiled: July 19, 2013Publication date: December 19, 2013Applicant: Allergan, Inc.Inventors: Richard L. Beard, John E. Donello, Tien T. Duong, Xiaoxia Liu, Haiging Yuan
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Publication number: 20130338104Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain 3-substituted-4-oxo-3,4-dihydro-imidazo[5,1-d][1,2,3,5]tetrazine-8-carboxylic acid amide (collectively referred to herein as 3TM compounds). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit cell proliferation, and in the treatment of proliferative disorders such as cancer, etc., and methods of preparing such compounds.Type: ApplicationFiled: May 24, 2013Publication date: December 19, 2013Applicant: Pharminox LimitedInventors: Malcolm Francis Graham Stevens, David Cousin, Sharon Jennings, Andrew James McCarroll, John Gareth Williams, Marc Geoffery Hummersone, Jihong Zhang
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Publication number: 20130338197Abstract: There is provided a novel agent for controlling harmful arthropods or nematodes that are parasites and hygienic pests for animals. An ecto- or endo-parasiticide for mammals or the like comprising as active ingredient, one or more selected from substituted benzamide compounds of formula (1) or salts thereof: wherein A1 is C—X3 or nitrogen atom, etc., A2 and A3 are C—H, etc., A4 is C—H or nitrogen atom, etc., G is G-2a, etc., W is oxygen atom or sulfur atom, X1 is halogen atom, trifluoromethyl, etc., X2 is hydrogen atom, halogen atom, trifluoromethyl, etc., X3 is hydrogen atom, halogen atom, etc., Y1 is hydrogen atom, halogen atom, methyl, etc., R1 is trifluoromethyl, etc., R2 is E-3a, etc., R3 is hydrogen atom, etc., p is an integer of 0 to 2.Type: ApplicationFiled: November 18, 2011Publication date: December 19, 2013Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.Inventors: Takeshi Mita, Yukihiro Maizuru, Ken-ichi Toyama, Motoyoshi Iwasa, Hotaka Imanaka, Hiroto Matsui
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Publication number: 20130338117Abstract: This invention provides methods of inhibiting replication of a poxvirus by contacting a poxvirus with a compound having formula I, formula XXI, formula XXXII, or formula XLI which in turn reduce, inhibit, or abrogate poxvirus DNA polymerase activity and/or its interaction with its processivity factor. Formula I, formula XXI, formula XXXII, or formula XLI can be utilized to treat humans and animals suffering from a poxvirus infection. Pharmaceutical compositions for treating poxvirus infected subjects are also provided.Type: ApplicationFiled: August 27, 2013Publication date: December 19, 2013Applicant: The Trustees of the University of PennsylvaniaInventor: Robert P. RICCIARDI
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Patent number: 8609706Abstract: The invention relates to isoxazolidine containing compounds that bind to bcl proteins and inhibit Bcl function. The compounds may be used for treating and modulating disorders associated with hyperproliferation, such as cancer.Type: GrantFiled: May 15, 2012Date of Patent: December 17, 2013Assignee: Infinity Discovery, Inc.Inventors: Alfredo C. Castro, Kristopher M. Depew, Michael J. Grogan, Charles W. Johannes, Edward B. Holson, Brian T. Hopkins, Gregg F. Keaney, Nii O. Koney, Tao Liu, David A. Mann, Marta Nevalainen, Stephane Peluso, Lawrence Blas Perez, Daniel A. Snyder, Thomas T. Tibbitts
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Patent number: 8609655Abstract: This invention relates generally to the field of medicine and, more specifically, to methods for treating epithelial injury, in particular, due to ischemia, hypoxia, trauma, chemolytics or radiation exposure.Type: GrantFiled: March 27, 2009Date of Patent: December 17, 2013Assignee: Amgen Inc.Inventors: John Peter Geibel, David Martin, Gordon Ng, William G. Richards, Joanne L. Viney, Patricia R. Hebert
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Patent number: 8609628Abstract: Disclosed are polycyclic polyether compounds of formula I and pharmaceutical compositions comprising such compounds. wherein R, OR1, and R2 are as defined herein. Also disclosed are methods of regulating mucus clearance in a cell, and methods of treating decreased mucus clearance or mucociliary dysfunction.Type: GrantFiled: January 23, 2012Date of Patent: December 17, 2013Assignee: University of North Carolina at WilmingtonInventors: Daniel G. Baden, William M. Abraham, Andrea J. Bourdelais, Sophie Michelliza
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Publication number: 20130330366Abstract: In one aspect, the invention relates to compounds having the formula XII: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.Type: ApplicationFiled: June 6, 2013Publication date: December 12, 2013Inventors: Adam D. Hughes, Melissa Fleury
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Publication number: 20130330365Abstract: In one aspect, the invention relates to compounds having the formula X: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.Type: ApplicationFiled: June 6, 2013Publication date: December 12, 2013Inventors: Adam D. Hughes, Melissa Fleury
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Patent number: 8604069Abstract: A compound of formula [I-W]: wherein each symbol is as defined in the description, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: April 27, 2012Date of Patent: December 10, 2013Assignee: Japan Tobacco Inc.Inventors: Takaki Maeba, Katsuya Maeda, Masayuki Kotoku, Kazayuki Hirata, Noriyoshi Seki, Hiroshi Yamanaka, Takayuki Sakai, Shintaro Hirashima, Shingo Obika, Makoto Shiozaki, Masahiro Yokota
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Patent number: 8604038Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.Type: GrantFiled: August 24, 2010Date of Patent: December 10, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Scott D. Edmondson, Lehua Chang, Nam Fung Kar, Gergori J. Morriello, Christopher R. Moyes, Dong-Ming Shen, Cheng Zhu, Neville J. Anthony, Philip Jones, Graham F. Smith, Mark E. Scott, Christopher F. Thompson, Joon Jung, Carolyn Cammarano, Dawn Marie Hoffman
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Publication number: 20130324503Abstract: The present invention relates to methods of treatment for Parkinson Disease (PD) in a person by identifying gene variants which may indicate a more favorable response to specific medicaments, thereby allowing for personalized or individualized treatment. The present invention relates to a method of screening for a genetic predisposition to PD in a person. The present invention is also directed to a method of testing a person for the presence of particular gene variants, wherein the presence of a gene variant indicates a higher predisposition to PD, and the absence of a gene variant indicates a lower predisposition to PD, compared to a control sample. The present invention further relates to methods and kits for treating, or inhibiting the development of, PD in a person. The present invention is also directed to a method of identifying the heritage of an individual based on the genetic profile of the individual.Type: ApplicationFiled: October 19, 2012Publication date: December 5, 2013Applicants: Health Research Inc., Emory University School of Medicine, National Institute of Environmental Health Sciences, Veterans Affairs Puget Sound Health Care System, Oregon Health & Science UniversityInventors: Haydeh Payami, Taye H. Hamza, Stewart A. Factor, John Nutt, Cyrus Zabetian, Honglei Chen, Erin Hill Burns
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Publication number: 20130324538Abstract: The invention relates to new isoxazoline compounds of formula wherein the variables have the meaning as indicated in the claims; in free form and in salt form; and optionally the enantiomers and geometrical isomers thereof. The compounds of formula (I) are useful in the control of parasites, in particular ectoparasites, in and on warm-blooded animals.Type: ApplicationFiled: February 9, 2012Publication date: December 5, 2013Inventors: Noëlle Gauvry, Steve Nanchen
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Publication number: 20130324544Abstract: Compounds of the formula I Formula (I) wherein the substituents are as defined in claim 1, are useful as active ingredients, which have microbiocidal activity, in particular fungicidal activity.Type: ApplicationFiled: November 25, 2011Publication date: December 5, 2013Applicant: SYNGENTA PARTICIPATIONS AGInventors: Sarah Sulzer-Mosse, Clemens Lamberth, Mathias Stephan Respondek, Laura Quaranta, Fredrik Cederbaum, Guillaume Berthon
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Publication number: 20130324560Abstract: 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: ApplicationFiled: August 7, 2013Publication date: December 5, 2013Applicant: 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
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Publication number: 20130317007Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.Type: ApplicationFiled: April 11, 2013Publication date: November 28, 2013Applicant: Reata Pharmaceuticals, Inc.Inventors: Eric ANDERSON, Xin JIANG, Melean VISNICK
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Publication number: 20130317073Abstract: The present invention provides methods comprising applying to a crop of soybean plants, the locus thereof, or propagation material thereof, a compound a compound of formula III wherein A3, A4, A4? and A5? are independently C—H, or nitrogen and wherein #1 indicates the bond to X and #2 indicates the bond to cycle B; cycle B is selected from B1 to B6 wherein #1 indicates the bond to cycle A, #2 indicates the bond to R7 and #3 indicates the bond to cycle C; cycle C is phenyl; R5 is chloro, bromo, CF3 or methyl; R7 is chlorodifluoromethyl or trifluoromethyl; each R8 is independently bromo, chloro, fluoro or trifluoromethyl; p is 2 or 3; and wherein X is defined in the claims. The methods are preferably for the control of stinkbugs, in particular Euschistus.Type: ApplicationFiled: February 1, 2012Publication date: November 28, 2013Applicants: SYNGENTA LIMITED, SYNGENTA PARTICIPATIONS AGInventors: Christoph Vock, Jerome Yves Cassayre, Myriem El Qacemi
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Patent number: 8592418Abstract: The present invention relates to new isoxazoline compounds of formula wherein the variables have the meaning as indicated in the claims; in free form and in salt form; and optionally the enantiomers and geometrical isomers thereof. The compounds of formula (I) are useful in the control of parasites, in particular ectoparasites, in and on vertebrates.Type: GrantFiled: June 11, 2011Date of Patent: November 26, 2013Assignee: Novartis AGInventors: Steve Nanchen, Noelle Gauvry, Thomas Goebel
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Patent number: 8592456Abstract: The present invention relates to compounds of the general formula (I), and the pharmaceutically acceptable salt or solvate thereof, as anti-inflammatory and immunomodulatory agents.Type: GrantFiled: January 27, 2012Date of Patent: November 26, 2013Assignee: 4SC Discovery GmbHInventors: Johann Leban, Stefan Tasler, Roland Baumgartner, Wael Saeb, Carine Chevrier
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Publication number: 20130310386Abstract: Methods for treating eye diseases associated with inflammation and/or vascular proliferation in subjects are disclosed. The methods include administering therapeutically effective amounts of a tranilast compound, in particular (E)-2-[[3-(3-Methoxy-4-propargyloxy)phenyl)-1-oxo-2-propenyl]amino]benzoic acid or (E)-2-[[3,4-Bis(difluoromethoxy)phenyl)-1-oxo-2-propenyl]amino]benzoic acid or pharmaceutically acceptable salts or solvates thereof.Type: ApplicationFiled: November 10, 2011Publication date: November 21, 2013Applicant: Fibrotech Therapeutics Pty LtdInventors: Darren James Kelly, David Stapleton
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Publication number: 20130310377Abstract: Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer.Type: ApplicationFiled: December 20, 2012Publication date: November 21, 2013Applicant: Rhizen Phamaceuticals SAInventor: Rhizen Phamaceuticals SA
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Publication number: 20130296355Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.Type: ApplicationFiled: July 3, 2013Publication date: November 7, 2013Inventors: Gary Erik Aspnes, Mary Theresa Didiuk, Kevin James Filipski, Angel Guzman-Perez, Esther Cheng Yin Lee, Jeffrey Allen Pfefferkorn, Benjamin Dawson Stevens, Meihua Mike Tu
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Publication number: 20130296310Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is a group of formula A or formula B, and X, R2, R3, R4, R5, R6, Ra and Rb are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist and methods of making the subject compounds.Type: ApplicationFiled: July 1, 2013Publication date: November 7, 2013Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
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Patent number: 8575197Abstract: The present invention provides a novel P2X3 and/or P2X2/3 receptor antagonist. A compound represented by the formula (I): wherein Z1 is optionally protected hydroxy, etc.; Z2 is —C(?O)—, etc.; Z3a and Z3b are taken together ?O or ?S; t is an integer of 0 to 4; R4a and R4b are each independently, hydrogen or substituted or unsubstituted lower alkyl, etc.; m and n are each independently an integer of 0 to 2; k is an integer of 0 or 1; Ring A is an aromatic carbocyclic ring or a heterocyclic ring, etc.; B is aromatic carbocyclic ring-diyl or heterocyclic ring-diyl, etc.; R1a and R1b are each independently halogen, hydroxy, substituted or unsubstituted lower alkyl, etc.; R2 is substituted or unsubstituted alkyl, etc.; R3 is substituted or unsubstituted alkyl, substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group, etc.; or its pharmaceutically acceptable salt, or a solvate thereof is provided.Type: GrantFiled: September 24, 2009Date of Patent: November 5, 2013Assignee: Shionogi & Co., Ltd.Inventors: Hiroyuki Kai, Yoshiyuki Taoda, Takeshi Endoh, Kentaro Asahi, Hiroyuki Tobinaga
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Publication number: 20130289026Abstract: Isoxazoles of formula (A) or (B) are inhibitors of HSP90 activity, and useful for treatment of, for example cancers: wherein R1, is a group of formula (IA): —Ar1-(Alk1)p-(Z)r-(Alk2)s-Q, wherein in any compatible combination Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1 and Alk2 are optionally substituted divalent C1-C6 alkylene or C2-C6 alkenylene radicals, p, r and s are independently 0 or 1, Z is -0-, —S—, —(C?O)—, —(C?S)—, —SO.sub.Type: ApplicationFiled: June 27, 2013Publication date: October 31, 2013Inventors: Martin James Drysdale, Brian William Dymock, Harry Finch, Paul Webb, Edward McDonald, Karen Elizabeth James, Kwai Ming Cheung, Thomas Peter Matthews
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Patent number: 8569376Abstract: Provided are methods of reducing body fat in a subject, comprising locally (e.g., topically) administering one or more compounds of the Formula (I) and/or (V): or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, polymorph, tautomer, isotopically enriched derivative, or prodrug thereof, wherein X is —OR1, —SR2, or —NR3R4, and R1, R2, R3, R4, R5, R6, R7, R7?, Z, Y, n, y, and x, are as defined herein.Type: GrantFiled: March 1, 2013Date of Patent: October 29, 2013Assignee: Topokine Therapeutics, Inc.Inventors: Murat V. Kalayoglu, Michael S. Singer
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Patent number: 8569312Abstract: In its many embodiments, the present invention provides a novel class of biaryl spiroaminooxazoline analogues as modulators of ?2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ?2C adrenergic receptors using such compounds or pharmaceutical compositions.Type: GrantFiled: April 4, 2013Date of Patent: October 29, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Kevin D. McCormick, Li Dong, Christopher W. Boyce, Manuel de Lera Ruiz, Salem Fevrier, Jie Wu, Junying Zheng, Younong Yu, Jianhua Chao, Walter S. Won, Ashwin U. Rao, Rongze Kuang, Pauline C. Ting, Xianhai Huang, Ning Shao, Anandan Palani, Michael Y. Berlin, Robert G. Aslanian
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Publication number: 20130281387Abstract: Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administering a composition comprising a chemosensory receptor ligand. Also provided herein are chemosensory receptor ligand compositions and methods for the preparation thereof for use in the methods of the present invention.Type: ApplicationFiled: October 18, 2011Publication date: October 24, 2013Applicant: ELCELYX THERAPEUTICS, INC.Inventors: Alain D. Baron, Martin R. Brown, Christopher R.G. Jones, Nigel R.A. Beeley
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Publication number: 20130281501Abstract: This invention provides topical localized formulations comprising an isoxazoline compound and a pharmaceutically or veterinary acceptable liquid carrier vehicle comprising N,N-diethyl-3-methylbenzamide as a solvent and an improved method for controlling, and preventing parasite infestation in animals.Type: ApplicationFiled: December 22, 2011Publication date: October 24, 2013Inventors: Stefan Fuchs, Anja Regina Heckeroth, Ramona Müller, Heike Williams
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Patent number: 8563714Abstract: The present invention relates to bridged spiro[2.4]heptane derivatives of formula (I), wherein W, Y, Z, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds as ALX receptor and/or FPRL2 agonists for the treatment of inflammatory and obstructive airways diseases.Type: GrantFiled: May 17, 2010Date of Patent: October 22, 2013Assignee: Actelion Pharmaceuticals Ltd.Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
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Publication number: 20130274212Abstract: The present invention relates to sesterterpene compounds, to the precursors thereof that are hydrolysable in a living body, or to the pharmaceutically acceptable salts thereof, and also relates to the prevention and treatment efficacy of the sesterterpene compounds with respect to non-insulin dependent diabetes mellitus, diabetic complications (renal failure and foot ulcers caused by diabetes), alcoholic, non-alcoholic, and viral fatty liver diseases, obesity, hyperlipidemia, atherosclerosis, cardiovascular diseases such as atherosclerotic stroke, and cerebropathies (Parkinsonism, schizophrenia and Alzheimer's disease). In addition, the present invention relates to compositions for functional foods, functional beverages, functional cosmetics, and functional feed.Type: ApplicationFiled: September 7, 2011Publication date: October 17, 2013Applicant: SNU R&DB FOUNDATIONInventors: Heon Joong Kang, Dong Hwan Won, In Ho Yang, Eun Oh Kim, Jung Ah Kim, Awadut Gajendra Giri, Venkat Reddy Mallepally
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Publication number: 20130274301Abstract: The invention relates to the use of polycycloolefins in electronic devices and more specifically to the use of such polycycloolefins as interlayers applied to insulating layers used in electronic devices, the electronic devices that encompass such polycycloolefin interlayers and processes for preparing such polycycloolefin interlayers and electronic devices.Type: ApplicationFiled: August 23, 2011Publication date: October 17, 2013Applicant: AL-GIAX PHARMACEUTICALS GMBHInventors: Guido Koopmans, Birgit Hasse, Stefan Mullner
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Publication number: 20130274302Abstract: This invention provides topical localized formulations comprising an isoxazoline compound and a pharmaceutically or veterinary acceptable liquid carrier vehicle comprising glycofurol and an improved method for controlling, and preventing parasite infestation in animals.Type: ApplicationFiled: December 22, 2011Publication date: October 17, 2013Inventors: Stefan Fuchs, Anja Regina Heckeroth, Ramona Müller, Heike Williams
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Publication number: 20130267501Abstract: The present disclosure provides compounds that function as modulators of aldehyde dehydrogenase (ALDH) enzymatic activity, as well as compositions and formulations comprising the compounds. The present disclosure provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition.Type: ApplicationFiled: January 22, 2013Publication date: October 10, 2013Applicant: The Board of Trustees of the Leland Stanford Junior UniversityInventor: The Board of Trustees of the Leland Stanford Junior University
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Patent number: 8552040Abstract: Methods of use and pharmaceutical compositions for a genus of low molecular weight compounds comprising optionally substituted isoxazoline ring systems that act as inhibitors of MIF (macrophage migration inhibitory factor) are disclosed. Specifically, the compounds are useful for treating a variety of diseases involving inflammatory activity or pro-inflammatory cytokine responses, such as autoimmune diseases (including rheumatoid arthritis, insulin-dependent diabetes, multiple sclerosis, graft versus host disease, lupus syndromes), asthma, arthritis, ARDS, psoriasis, interleukin-2 toxicity, proliferative vascular disease, and various forms of sepsis and septic shock, and other conditions characterized by underlying MIF responses including, for instance, tumor growth and neovascularization (angiogenesis).Type: GrantFiled: April 14, 2011Date of Patent: October 8, 2013Assignee: CPSI Stockholder TrustInventor: Yousef Al-Abed
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Publication number: 20130261158Abstract: The present invention relates to fungicide N-(2-phenoxyethyl)carboxamide derivatives of formula (I), their aza, thia and sila analogues, their process of 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. Formula (1) wherein A, T, W, X, n and Z3 to Z7 represent various substituents.Type: ApplicationFiled: July 30, 2009Publication date: October 3, 2013Inventors: Samir Bennabi, Jurgen Benting, Stephane Brunet, Philippe Desbordes, Peter Dahmen, Stephanie Gary, Marie-Claire Grosjean-Cournoyer, Rachel Rama, Philippe Rinolfi, Valerie Toquin, Arnd Voerste, Ulrike Wachendorff-Neumann
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Publication number: 20130261069Abstract: The present invention provides pesticidal mixtures comprising a component A, a component B and a component C, wherein component A is a compound of formula (I) wherein one of Y1 and Y2 is S, SO or SO2 and the other is CH2; L is a direct bond or methylene; A1 and A2 are C—H, or one of A1 and A2 is C—H and the other is N; R1 is hydrogen or methyl; R2 is chlorodifluoromethyl or trifluoromethyl; R3 is 3,5-dibromo-phenyl, 3,5-dichloro-phenyl, 3,4-dichloro-phenyl, or 3,4,5-trichloro-phenyl; R4 is methyl; R5 is hydrogen; or R4 and R5 together form a bridging 1,3-butadiene group; component B is a compound selected from Sedaxane, Fludioxonil, Metalaxyl, Mefenoxam, Cyprodinil, Azoxystrobin, Tebuconazole, Difenoconazole, Thiabendazole, Fluopyram, Penflufen, N-[9-(dichloromethylene)-1,2,3,4-tetrahydro-1,4-methanonaphthalen-5-yl]-3-(difluoromethyl)-1-methyl-1H-pyrazole-4-carboxamide and Fuxapyroxad; or component B is a compound selected from Tefluthrin, Lambda-cyhalothrin, Abamectin, Spinosad, Spinetoram, Chlorpyrifos, ThiType: ApplicationFiled: June 9, 2011Publication date: October 3, 2013Applicant: SYNGENTA CROP PROTECTION LLCInventors: Ana Dutton, Jerome Yves Cassayre, Ulrich Johannes Haas
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Publication number: 20130261133Abstract: The compounds of the invention exhibit antiprotozoal, antimicrobial, and anticancer properties that are useful for the treatment or prevention of infections or cancer in a patient (e.g., a human). For example, the compounds and methods described herein can be used for the treatment or prevention of protozoal infections such as leishmaniasis, malaria, and trypanosoma infections, bacterial infections such as S. aureus and C. albicans, and cancers such as breast, colon, lung, or prostate cancer. The invention further provides methods of synthesizing such compounds as well as kits useful for administering the compounds.Type: ApplicationFiled: March 14, 2013Publication date: October 3, 2013Applicant: The University of MontanaInventors: John Howard Hoody, David Brian Bolstad
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Patent number: 8546376Abstract: The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.Type: GrantFiled: September 17, 2010Date of Patent: October 1, 2013Assignee: Almac Discovery LimitedInventors: Mark Peter Bell, Timothy Harrison, Sumita Bhattacharyya, James Samuel Shane Rountree, Frank Burkamp, Stephen Price, Calum MacLeod, Richard Leonard Elliott, Phillip Smith, Toby Jonathan Blench, Colin Roderick O'Dowd, Lixin Zhang, Graham Peter Trevitt, Hazel Joan Dyke
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Patent number: 8546389Abstract: The present invention relates to viral polymerase inhibitors of formula (I), 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: GrantFiled: October 20, 2011Date of Patent: October 1, 2013Assignee: Biota Scientific Management Pty Ltd.Inventors: Rosliana Halim, Michael Harding, Richard Hufton, Craig James Morton, Saba Jahangiri, Brett Raymond Pool, Tyrone Pieter Jeynes, Alistair George Draffan, Barbara Frey, Michael John Lilly
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Patent number: 8546588Abstract: This invention provides compounds of formula (I): wherein X1, X2, X3, R2, R4b, R1, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: GrantFiled: February 25, 2011Date of Patent: October 1, 2013Assignee: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
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Patent number: 8546357Abstract: This invention provides novel compounds, methods of using the compounds, and pharmaceutical compositions containing the compounds.Type: GrantFiled: November 16, 2012Date of Patent: October 1, 2013Assignees: Eli Lilly and Company, Anacor Pharmaceuticals, Inc.Inventors: Tsutomu Akama, Terry William Balko, Jean Marie Defauw, Jacob J. Plattner, William Hunter White, Joseph Raymond Winkle, Yong-Kang Zhang, Yasheen Zhou