Plural Ring Chalcogens In The Hetero Ring Patents (Class 514/360)
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Patent number: 10927086Abstract: Compounds of Formula I, or a pharmaceutically acceptable salt, solvate or hydrate thereof: (I). Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.Type: GrantFiled: February 19, 2018Date of Patent: February 23, 2021Assignee: Merck Sharp & Dohme Corp.Inventors: Kun Liu, Dane Clausen, Liangqin Guo, Yongxin Han, Shuwen He, Joseph Kozlowski, Derun Li, Qinglin Pu, Wensheng Yu, Hongjun Zhang
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Patent number: 10584120Abstract: Benzimidazole compounds of formula (I), shown below, are disclosed. The compounds are potent human glutaminyl cyclase inhibitors. Also disclosed is a pharmaceutical composition containing one of these compounds and a pharmaceutical acceptable carrier, as well as a method of treating Alzheimer's disease or Huntington's disease by administering to a subject in need thereof an effective amount of such a compound.Type: GrantFiled: August 27, 2019Date of Patent: March 10, 2020Assignees: National Health Research Institutes, Academia SinicaInventors: Chih-Hao Chen, Chuan Shih, Chiung-Tong Chen, Hwei-Jiung Wang, Kai-Fa Huang
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Patent number: 9988395Abstract: The present disclosure relates generally to systems, methods, and compounds for therapeutic use against parasitic infections. More particularly, the disclosure relates to anti-parasitic compounds, and methods for making and for using the anti-parasitic compounds, where the anti-parasitic compounds have the general formula: where X, R1, R2, R3, R4, R5, and R6 are defined more fully below.Type: GrantFiled: June 14, 2017Date of Patent: June 5, 2018Assignee: THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEMInventors: Rachid Skouta, Rosa A. Maldonado
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Patent number: 9943506Abstract: The invention provides compositions and methods for blocking the BCL6 BTB domain with small molecule, non-peptide compounds as disclosed and claimed herein. BCL6 is a transcriptional repressor of the BTB-POZ (brie a brae, tramtrack, broad complex/pox virus zincfinger) family of proteins. It is required for normal development of germinal center (GC) B-cells and is also the most commonly involvedoncogene in diffuse large B-celllymphomas (DLBCLs), and constitutive expression of BCL6 in GC B-cells causes DLBCL in mice.Type: GrantFiled: June 16, 2014Date of Patent: April 17, 2018Assignees: Cornell University, University of Maryland, BaltimoreInventors: Ari Melnick, Leandro Carlos A. Cerchietti, Mariano G. Cardenas, Fengtian Xue, Alexander D. MacKerell
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Patent number: 8962617Abstract: The present invention relates to the use of substituted dihydroimidazolones, particularly [1-(4-Chlorophenyl)-4-(4-morpholinyl)-2,5-dihydro-1H-imidazol-2-one] (AWD 131-138) or a physiologically acceptable salt thereof for the treatment of epilepsy in dogs.Type: GrantFiled: September 14, 2012Date of Patent: February 24, 2015Assignee: Boehringer Ingelheim Vetmedica GmbHInventors: Chris Rundfeldt, Rita Dost, Wolfgang Loscher, Andrea Tipold, Klaus Unverferth, Hans-Joachim Lankau
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Publication number: 20150030539Abstract: This invention relates to novel compounds suitable for labelling or already labelled by 18F, methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging by positron emission tomography (PET).Type: ApplicationFiled: July 21, 2014Publication date: January 29, 2015Applicant: PIRAMAL IMAGING SAInventors: Lutz LEHMANN, Andrea THIELE, Tobias HEINRICH, Thomas BRUMBY, Christer HALLDIN, Balazs GULYAS, Sangram NAG
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Publication number: 20140378415Abstract: The present invention provides compounds of formula (I) wherein P is P0, heterocyclyl or heterocyclyl substituted by one to five Z formula (II); Y1, Y2, Y3 and Y4 are independently of each other C—H, C—R5, or nitrogen; G1 is oxygen or sulfur; X4 is C1-C8 haloalkyl; R4 is aryl or aryl substituted by one to five R9, or heteroaryl or heteroaryl substituted by one to five R9; and R1, R2, R4, R5, R9 and Z are as defined in the claims. The invention also provides compositions comprising the compounds of formula (I), intermediates useful in the preparation of compounds of formula (I) and methods of using the compounds of formula (I) to control insects, acarines, nematodes or molluscs.Type: ApplicationFiled: August 27, 2012Publication date: December 25, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Jerome Yves Cassayre, Myriem El Qacemi
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Publication number: 20140364461Abstract: A method of treating a dermatological disorder in a subject includes the step of administering a therapeutically effective amount of at least one PPAR? agonist or derivative thereof to the subject.Type: ApplicationFiled: August 4, 2014Publication date: December 11, 2014Inventor: Pratima Karnik
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Patent number: 8859540Abstract: The present invention relates to the use of substituted dihydroimidazolones, particularly [1-(4-Chlorophenyl)-4-(4-morpholinyl)-2,5-dihydro-1H-imidazol-2-one] (AWD 131-138) or a physiologically acceptable salt thereof for the treatment of epilepsy in dogs.Type: GrantFiled: July 18, 2007Date of Patent: October 14, 2014Assignee: Boehringer Ingelheim Vetmedica GmbHInventors: Chris Rundfeldt, Rita Dost, Wolfgang Loscher, Andrea Tipold, Klaus Unverferth, Hans-Joachim Lankau
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Publication number: 20140296254Abstract: Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds are described that correspond to general formula (I). Also described, are pharmaceutical compositions that include these compounds and methods of using these compounds and compositions for the treatment of chemokine-mediated diseases.Type: ApplicationFiled: October 26, 2012Publication date: October 2, 2014Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Branislav Musicki, Jerôme Aubert, Jean-Guy Boiteaux, Laurence Clary, Patricia Rossio, Marlène Schuppli-Nollet
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Publication number: 20140296269Abstract: The present invention provides a composition for controlling plant diseases having an excellent control efficacy on plant diseases. A composition for controlling plant diseases comprising an amide compound represented by a formula (I); wherein each of symbols are the same as defined in the Description; or salts thereof and at least one kind of compounds selected from the group (A) consisting of kresoxim-methyl, azoxystrobin, pyraclostrobin, picoxystrobin, enestrobin, trifloxystrobin, dimoxystrobin, fluoxastrobin, orysastrobin, famoxadone, fenamidone, metominostrobin, a compound represented by a formula (II) and pyribencarb: shows an excellent controlling efficacy on plant diseases.Type: ApplicationFiled: October 26, 2012Publication date: October 2, 2014Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Atsushi Iwata, Makoto Kurahashi
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Patent number: 8846726Abstract: The present invention is directed to modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.Type: GrantFiled: January 4, 2013Date of Patent: September 30, 2014Assignee: Incyte CorporationInventors: Andrew P. Combs, Eddy W. Yue
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Patent number: 8841335Abstract: Provided is a pharmaceutical composition for inhibiting apoptosis of neurons or neurodegeneration. The pharmaceutical composition effectively prevents or treats diseases related to apoptosis of neurons or neurodegeneration.Type: GrantFiled: May 3, 2011Date of Patent: September 23, 2014Assignee: SK Biopharmaceuticals Co., Ltd.Inventors: Cheol Hyoung Park, Hye Kyung Min, In Suk Park, Mi Jung Lim, Ji Won Lee, Jin Yong Chung, Yeo Jin Yoon, Joo Young Park
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Patent number: 8835469Abstract: The present invention relates to substituted benzamide derivatives of the Formula I and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, diastereomers, prodrugs, metabolites, and polymorphs and can be useful for treating disease states mediated by glucokinase. Compounds disclosed herein can be used for reducing blood glucose levels and for increasing insulin secretion for treating type II diabetes. The invention also relates to processes for the preparation of the compounds of invention, pharmaceutical compositions containing the compounds, and their use.Type: GrantFiled: July 22, 2010Date of Patent: September 16, 2014Assignee: Cadila Healthcare LimitedInventors: Rajendra Kharul, Mukul R. Jain, Pankaj R. Patel
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Patent number: 8785483Abstract: Embodiments of the invention include methods and compositions involving aldose reductase inhibitors for treating COPD.Type: GrantFiled: December 23, 2011Date of Patent: July 22, 2014Assignee: The Board of Regents of the University of Texas SystemInventors: Satish K. Srivastava, Kota V. Ramana, Umesh Yadav
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Patent number: 8778979Abstract: Methods of treating mental disorders, including anxiety disorders such as obsessive-compulsive disorder, are provided. The methods comprise administering an effective amount of a glutamate modulator to an individual in need thereof. Also provided are methods of enhancing the activity of a serotonin reuptake inhibitor (SRI) comprising co-administering a glutamate modulator and a serotonin reuptake inhibitor. Pharmaceutical composition comprising a serotonin reuptake inhibitor and a glutamate modulator are also provided.Type: GrantFiled: April 5, 2006Date of Patent: July 15, 2014Assignee: Yale UniversityInventors: Vladimir Coric, John H. Krystal, Gerard Sanacora
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Patent number: 8735362Abstract: The present invention relates to compounds of formula (I): Wherein A1, A2, A3, A4, G1, L, Y1, Y2, Y3, Y4, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to intermediates for preparing compounds of formula (I), to compositions comprising them and to methods of using them to combat and control insect, acarine, nematode and mollusc pests.Type: GrantFiled: December 1, 2010Date of Patent: May 27, 2014Assignee: Syngenta Crop Protection, LLCInventors: Jerome Yves Cassayre, Peter Renold, Myriem El Qacemi, Thomas Pitterna, Julie Clementine Toueg
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Publication number: 20140113884Abstract: Compounds and compositions comprising epoxyeicosatrienoic acid (EET) analogs that act as EET agonists and are useful as medications in the treatment of drug-induced nephrotoxicity, hypertension and other related conditions. Methods of making and using the compounds and compositions are further described.Type: ApplicationFiled: April 4, 2012Publication date: April 24, 2014Inventors: John David Imig, William B. Campell, John Russell Falck
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Patent number: 8658650Abstract: Compounds useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4) and methods of using the compounds.Type: GrantFiled: January 28, 2010Date of Patent: February 25, 2014Inventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Charles David Weaver, Colleen M. Niswender, Rocco D. Gogliotti, Darren W. Engers
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Patent number: 8637496Abstract: The invention relates to the use of compounds having a monogalactosyldiacylglycerol (MGDG) synthase inhibitory activity as herbicide or algaecide, and to herbicide and algaecide compositions containing at least one of these compounds.Type: GrantFiled: June 2, 2008Date of Patent: January 28, 2014Assignees: Commissariat a l'Energie Atomique, Centre National de la Recherche ScientifiqueInventors: Anne-Laure Bonneau, Cyrille Botte, Michael Deligny, Nadia Saidani, Hélène Hardre, Bernard Rousseau, Roman Lopez, Eric Marechal
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Patent number: 8618086Abstract: A method for treating hair loss in mammals uses compositions containing prostaglandin F analogs. The compositions can be applied topically to the skin. The compositions can arrest hair loss, reverse hair loss, and promote hair growth.Type: GrantFiled: June 13, 2008Date of Patent: December 31, 2013Assignee: Duke UniversityInventors: Mitchell Anthony deLong, John McMillan McIver, Robert Scott Youngquist
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Patent number: 8618134Abstract: A method and composition for treating serotonin receptor-mediated conditions.Type: GrantFiled: December 13, 2008Date of Patent: December 31, 2013Assignee: Vanda Pharmaceuticals Inc.Inventors: Mihael H. Polymeropoulos, Paolo Baroldi, Curt Wolfgang
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Patent number: 8614168Abstract: The invention relates to the use of at least one compound, selected from the group consisting of tebuconazole, epoxiconazole, metconazole, cyproconazole, prothioconazole and any mixtures thereof, for increasing the resistance of plants to abiotic stress factors.Type: GrantFiled: July 24, 2009Date of Patent: December 24, 2013Assignee: MonheimInventors: Jan Dittgen, Isolde Häuser-Hahn, Heinz Kehne, Stefan Lehr, Jörg Tiebes, Marco Busch
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Patent number: 8592420Abstract: Anxiety disorders, such as panic disorder, agoraphobia, obsessive-compulsive disorder, social phobia, post-traumatic stress disorder, generalized anxiety disorder, specific phobia, or the like, are treated by administering an effective amount of at least one adenosine A2A receptor antagonist to a patient in need thereof, optionally in combination with an anxiolytic(s) other than the adenosine A2A receptor antagonist.Type: GrantFiled: April 16, 2012Date of Patent: November 26, 2013Assignee: Kyowa Hakko Kirin Co., Ltd.Inventors: Hiroshi Kase, Naoki Seno, Shizuo Shiozaki, Minoru Kobayashi, Junya Kase
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Publication number: 20130303525Abstract: The present invention relates to a series of substituted compounds having the general formula (I), including their stereoisomers and/or their pharmaceutically acceptable salts. (I) Wherein A, m, R1s, R2, R3, R4 are as defined herein. This invention also relates to methods of making these compounds including intermediates. The compounds of this invention are effective at the kappa (?) opioid receptor (KOR) site. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic pain, and associated disorders, particularly functioning peripherally at the CNS.Type: ApplicationFiled: July 19, 2011Publication date: November 14, 2013Applicants: DR. REDDY'S LABORATORIES, INC., DR. REDDY;S LABORATORIES LTD.Inventors: Pradip Kumar Sasmal, Vamsee Krishna Chintakunta, Vijay Potluri, Ish Kumar Khanna, Ashok Tehim, Mahaboobi Jaleel, Thomas Hogberg, Oystein Rist, Lisbeth Elster, Thomas Michael Frimurer, Lars-Ole Gerlach
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Patent number: 8569346Abstract: Compositions and methods for inhibiting BoNT protease activity are presented. In most preferred aspects, inhibitors comprise a thiol reactive group, a zinc binding group, a redox active group, an alkylating group, and/or an electrophilic Michael addition acceptor group. Particularly preferred inhibitors include an isothiazolone ring, a thiadiazolidine dione ring, a (hydro)quinone ring, an iminophenol group, and/or a hydrazonophenol group, and inhibit BoNT/A at ?M and sub-?M concentrations.Type: GrantFiled: October 14, 2010Date of Patent: October 29, 2013Assignee: Biomadison, Inc.Inventors: Füsûn N. Zeytin, Ward Tucker
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Patent number: 8541466Abstract: A method for treating hair loss in mammals uses compositions containing prostaglandin F analogs. The compositions can be applied topically to the skin. The compositions can arrest hair loss, reverse hair loss, and promote hair growth.Type: GrantFiled: August 4, 2009Date of Patent: September 24, 2013Assignee: Duke UniversityInventors: Mitchell Anthony DeLong, John McMillan McIver, Robert Scott Youngquist
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Patent number: 8518978Abstract: There is provided a pharmaceutical composition for prevention and treatment of restenosis comprising isoxazole derivatives. The pharmaceutical composition includes a therapeutic effective amount of isoxazole derivatives represented by Formula 1 or pharmaceutically available salts thereof. The pharmaceutical composition may be useful to prevent and treat vascular restenosis since the pharmaceutical composition shows an anti-restenosis activity and accelerates the re-endothelization.Type: GrantFiled: June 30, 2008Date of Patent: August 27, 2013Assignee: SK Biopharmaceuticals Co., Ltd.Inventors: Sun Gwan Hwang, Sang Rak Choi, Jeong Woo Cho, Sung Jin Bae, Tae Sung Koo, So Young Lee, Kyung Chul Cho, Hyeon Cheol Gwon
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Publication number: 20130165485Abstract: A compound of formula (I): where A, B, C, G, m, n, o, p, R1, R2, R3, R4, R5, R6, X, R7, R8, R9, R10 and R11 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, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.Type: ApplicationFiled: February 20, 2013Publication date: June 27, 2013Applicant: Syngenta Crop Protection LLCInventors: Jerome Yves Cassayre, Peter Renold, Vladimir Bobosik, Myriem El Qacemi, Anne Jacqueline Dalencon, Werner Zambach, Christopher Richard Godfrey, Thomas Pitterna, Pierre Joseph Jung, Jagadish Pabba
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Patent number: 8466166Abstract: This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein: R1, R2, R3, R4, A and E are each as described herein or a pharmaceutically acceptable salt, and compositions containing such compounds and the method of treatment and the use, comprising such compounds for the treatment of a condition mediated by acid pump antagonistic activity such as, but not limited to, as gastrointestinal disease, gastroesophageal disease, gastroesophageal reflux disease (GERD), laryngopharyngeal reflux disease, peptic ulcer, gastric ulcer, duodenal ulcer, NSAID-induced ulcers, gastritis, infection of Helicobacter pylori, dyspepsia, functional dyspepsia, Zolli?ger-Ellison syndrome, non-erosive reflux disease (NERD), visceral pain, cancer, heartburn, nausea, esophagitis, dysphagia, hypersalivation, airway disorders or asthma.Type: GrantFiled: September 17, 2007Date of Patent: June 18, 2013Assignee: Raqualia Pharma Inc.Inventors: Hiroki Koike, Mikio Morita
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Patent number: 8399495Abstract: Novel metabolites of talarazole of formula (I) have been isolated and characterized, wherein R?H, OH, OSO3H or O-gly; R1, ?H, OH, OSO3H, O-gly or =0; and gly=a glucuronate, or a pharmaceutically acceptable salt thereof. These compounds are targeted for the treatment of various skin-, hair- and nail-associated disorders.Type: GrantFiled: May 21, 2012Date of Patent: March 19, 2013Assignee: Stiefel Laboratories, Inc.Inventor: Debra Barrett
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Patent number: 8383579Abstract: Generally the method involves identifying the concentration of each of two or more active therapeutics tailored to treat a particular patient's unique metabolism and one or more diseases, communicating that information to a producer who has multiple fixed or variable concentrations of each active available, where the producer then combines the individual concentrations of each active into single units such as a tablets or pills, and distributes those indirectly or directly to the patient.Type: GrantFiled: August 3, 2011Date of Patent: February 26, 2013Assignee: Glaxosmithkline, LLCInventors: Richard L. Kirsh, Steven D. Finkelmeier, Robert Glinecke, Luigi Martini
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Patent number: 8372870Abstract: The present invention is directed to modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.Type: GrantFiled: August 29, 2011Date of Patent: February 12, 2013Assignee: Incyte CorporationInventors: Andrew P. Combs, Eddy W. Yue
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Patent number: 8367645Abstract: The invention relates to a composition that includes a first agent selected including an agent that possesses anti-inflammatory activity or acetaminophen, phenacetin, tramadol and the like; a second agent selected from the group consisting of an oxidative phosphorylation inhibitor, an ionophore, and an adenosine 5-monophosphate-activated Protein kinase (AMPK) activator; a third agent that possesses or maintains serotonin activity.Type: GrantFiled: May 18, 2009Date of Patent: February 5, 2013Inventor: Chien-Hung Chen
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Patent number: 8338464Abstract: Provided are methods of inhibiting BCL6 repression in a mammalian cell. Also provided are methods of treating cancer in a mammal.Type: GrantFiled: November 29, 2007Date of Patent: December 25, 2012Assignees: Albert Einstein College of Medicine of Yeshiva University, University Health Network, University of Maryland, BaltimoreInventors: Ari Matthew Melnick, Alexander D. MacKerell, Jr., Gilbert Gerard Privé
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Patent number: 8287631Abstract: The invention relates to compounds from the groups of (A) electrophiles, (B) nucleophiles, (C) alkylating agents, (D) antioxidants and (E) oxidizing agents as odor preventatives for reducing so-called ghost odor which is induced by 2-methyl-4-isothiazolin-3-one and/or octyl-4-isothiazolin-3-one. The invention further relates to biocide compositions which comprise 2-methyl-4-isothiazolin-3-one and/or octyl-4-isothiazolin-3-one and also one or more odor preventatives, and to the use of odor preventatives for preventing ghost odor.Type: GrantFiled: January 28, 2010Date of Patent: October 16, 2012Assignee: THOR GmbHInventors: Rudiger Baum, Hans-Jurgen Schmidt, Thomas Wunder, Christos Savides
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Publication number: 20120238517Abstract: The present invention relates to compounds of formula (I): Wherein A1, A2, A3, A4, G1, L, Y1, Y2, Y3, Y4, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to intermediates for preparing compounds of formula (I), to compositions comprising them and to methods of using them to combat and control insect, acarine, nematode and mollusc pests.Type: ApplicationFiled: December 1, 2010Publication date: September 20, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Jerome Yves Cassayre, Peter Renold, Myriem El Qacemi, Thomas Pitterna, Julie Clementine Toueg
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Publication number: 20120232104Abstract: The invention is concerned with novel sulfonamide derivatives of formula (I) wherein R2, R3, R4, A, X, Y1, Y2, Y3, Y4 and Z1 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.Type: ApplicationFiled: May 22, 2012Publication date: September 13, 2012Inventors: Konrad Bleicher, Simona Maria Ceccarelli, Odile Chomienne, Patrizio Mattei, Tanja Schulz-Gasch, Christoph Martin Stahl
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Patent number: 8247398Abstract: The present invention relates to the use of zinc complexes of natural amino acids, especially L-arginine, L-lysine, L-ornithine, and other natural amino acids, in a molar ratio of about 1:2 (metal:amino acid), and formulations thereof. These pharmaceutical compositions offer better tolerated and faster acting regimens than common zinc salts (i.e., acetate, sulfate, etc.) for long term maintenance therapy of diseases caused by abnormal elevated copper levels, such as in Wilson's disease, inflammatory and fibrotic diseases and Alzheimer's disease.Type: GrantFiled: February 17, 2007Date of Patent: August 21, 2012Assignee: SSV Therapeutics, Inc.Inventor: Om P. Goel
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Patent number: 8231721Abstract: The invention relates to stable antifungal liquid formulations for protecting material, containing 3-iodopropynyl butyl carbamate (IPBC) and n-octylisothiazolinone (n-OIT).Type: GrantFiled: July 28, 2009Date of Patent: July 31, 2012Assignee: LANXESS Deutschland GmbHInventors: Hermann Uhr, Tanja Gerharz, Frank Sauer
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Patent number: 8217063Abstract: The present application relates to novel lactam-substituted dicarboxylic acid derivatives, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.Type: GrantFiled: March 15, 2008Date of Patent: July 10, 2012Assignee: Bayer Intellectual Property GmbHInventors: Michael Hahn, Eva-Maria Becker, Andreas Knorr, Dirk Schneider, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Frank Wunder, Dieter Lang
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Patent number: 8193228Abstract: Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.Type: GrantFiled: October 16, 2007Date of Patent: June 5, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: David Chen, Christopher L. Franklin, Peter R. Guzzo, Linus S. Lin, Michael M. C. Lo, Ravi P. Nargund, Iyassu K. Sebhat
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Patent number: 8188124Abstract: Novel metabolites of talarazole of formula (I) have been isolated and characterized, wherein R?H, OH, OSO3H or O-gly; R1, ?H, OH, OSO3H, O-gly or =0; and gly=a glucuronate, or a pharmaceutically acceptable salt thereof. These compounds are targeted for the treatment of various skin-, hair- and nail-associated disorders.Type: GrantFiled: October 17, 2007Date of Patent: May 29, 2012Assignee: Stiefel Laboratories, Inc.Inventor: Debra Barrett
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Patent number: 8183275Abstract: Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.Type: GrantFiled: October 16, 2007Date of Patent: May 22, 2012Assignees: Merck Sharp & Dohme Corp., Albany Molecular Research, Inc.Inventors: Peter H. Dobbelaar, Christopher L. Franklin, Allan Goodman, Cheng Guo, Peter R. Guzzo, Mark Hadden, Shuwen He, Alan J. Henderson, Tianying Jian, Linus S. Lin, Jian Liu, Ravi P. Nargund, Megan Ruenz, Bruce J. Sargent, Iyassu K. Sebhat, Larry Yet
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Publication number: 20120115912Abstract: A method of treating a PPAR? and/or RXR related disease or disorder in a subject includes adminstering to the subject an RXR agonist alone or in combination with a PPAR? agonist.Type: ApplicationFiled: July 12, 2010Publication date: May 10, 2012Inventors: Gary E. Landreth, Paige E. Cramer
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Patent number: 8153667Abstract: The present invention provides compounds of the structure: wherein the constituent members are defined herein, including pharmaceutical compositions thereof and methods of treating diseases therewith.Type: GrantFiled: September 14, 2007Date of Patent: April 10, 2012Assignee: Cephalon, Inc.Inventors: Edward R. Bacon, Sankar Chatterjee, Derek Dunn, Rabindranath Tripathy
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Patent number: 8153682Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, G, Y, R1, R2, R3, and R4 are defined herein.Type: GrantFiled: July 18, 2008Date of Patent: April 10, 2012Assignee: Janssen Pharmaceutica, NVInventors: Shawn T. Branum, Raymond W. Colburn, Scott L. Dax, Christopher M. Flores, Michele C. Jetter, Yi Liu, Donald Ludovici, Mark J. Macielag, Jay M. Matthews, James J. McNally, Laura M. Reaney, Ronald K. Russell, Ning Qin, Christopher Teleha, Kenneth M. Wells, Scott C. Youells, Mark A. Youngman
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Patent number: 8110589Abstract: An ectoparasiticide composition for animals including etoxazole as an active ingredient, a UV absorber and a phenol antioxidant, and a method for exterminating ectoparasites using the composition. The preferable blending ratio between etoxazole, a UV absorber and a phenol antioxidant in terms of mass ratio is 1: from 0.05 to 5: from 0.05 to 5.Type: GrantFiled: June 17, 2008Date of Patent: February 7, 2012Assignee: Kyoyu Agri Co., Ltd.Inventors: Yosuke Hashimoto, Yoshiko Tamura, Mamoru Takiuchi, Hidenobu Yanase
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Publication number: 20110319429Abstract: Compounds useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4) and methods of using the compounds.Type: ApplicationFiled: January 28, 2010Publication date: December 29, 2011Inventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Charles David Weaver, Colleen M. Niswender, Rocco D. Gogliotti, Darren W. Engers
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Publication number: 20110294780Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: ApplicationFiled: May 24, 2011Publication date: December 1, 2011Inventors: Gilles Bignan, Wing Cheung, Micheal Gaul, Hui Huang, Xun Li, Raymond Patch, Sharmila Patel, Mark Player, Guozhang Xu, Bao-Ping Zhao, Jian Liu