1,2,4-triazoles (including Hydrogenated) Patents (Class 514/383)
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Patent number: 8895584Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.Type: GrantFiled: May 12, 2014Date of Patent: November 25, 2014Assignee: Janssen Pharmaceutica NVInventors: Carl R. Illig, Shelley K. Ballentine, Jinsheng Chen, Renee Louise Desjarlais, Sanath K. Meegalla, Mark Wall, Kenneth J. Wilson
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Patent number: 8895594Abstract: Synergistic microbicidal compositions containing N-methyl-1,2-benzisothiazolin-3-one.Type: GrantFiled: January 8, 2014Date of Patent: November 25, 2014Assignee: Rohm and Haas CompanyInventors: John W. Ashmore, Beverly J. El A'mma, Beat Heer, Kiran Pareek
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Patent number: 8895595Abstract: Synergistic microbicidal compositions containing N-methyl-1,2-benzisothiazolin-3-one.Type: GrantFiled: January 8, 2014Date of Patent: November 25, 2014Assignee: Rohm and Haas CompanyInventors: John W. Ashmore, Beverly J. El A'mma, Beat Heer, Kiran Pareek
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Publication number: 20140341850Abstract: A new class of haloalkyl heteroaryl benzamides is described. These compounds show strong activity against hepatitis viruses.Type: ApplicationFiled: August 5, 2014Publication date: November 20, 2014Applicant: Romark Laboratories, L.C.Inventors: Jean-Francois Rossignol, J. Edward Semple
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Publication number: 20140343347Abstract: A method of treatment and/or prevention of cancer comprises administering agents which cause increased intracellular granularity in cancer cells, at least in an amount sufficient to inhibit proliferation of such cells and preferably in an amount sufficient to lead to cancer cell death. The method is particularly directed to refractory cancer, particularly hormone refractory prostate cancer. The agents identified cause increased intracellular granularity in the cancer cells, and also convert adherent cancer cells to non-adherent cancer cells, leading to cancer cell death. Using the present invention, cancer cells undergo increased intracellular granularity at relatively low agent concentrations, while also inhibiting cell proliferation. Increased concentrations lead to conversion of adherent cancer cells to non-adherent cancer cells, then to cell death.Type: ApplicationFiled: August 1, 2014Publication date: November 20, 2014Inventors: Todd A. Thompson, Debra Mackenzie, Tudor I. Oprea, Larry A. Sklar, Bruce S. Edwards, Mark Haynes
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Publication number: 20140342912Abstract: This invention relates to the use of aromatic phosphate esters of formula (I) wherein R1, R2 and R2 are as defined within the description, as adjuvants in compositions, particularly for agrochemical use, as well to compositions comprising such an aromatic phosphate ester, in combination with at least one agrochemical and optionally at least one surfactant. The invention further extends to methods of making and using such compositions.Type: ApplicationFiled: November 23, 2012Publication date: November 20, 2014Applicant: SYNGENTA LIMITEDInventors: Gordon Alastair Bell, Philip Taylor
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Publication number: 20140343049Abstract: The present invention relates to compounds of formula (IA) wherein QA is QA1 or QA2 P is P1, heterocycyl or heterocyclyl substituted by one to five Z; and wherein A1, A2, A3, A4, G1, Z, R1, R2, R3 and R4 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 (IA), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (IA) and to methods of using the compounds of formula (IA) to control insect, acarine, nematode and mollusc pests.Type: ApplicationFiled: August 10, 2012Publication date: November 20, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Julie Clementine Toueg, Tomas Smejkal, Sebastian Volker Wendeborn, Jerome Yves Cassayre, Myriem El Qacemi, Bernhard Breit, Lisa Diab, Regis Jean Georges Mondiere, Nicolas Poirier
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Publication number: 20140343078Abstract: Methods of inhibiting cytochrome P450 2D6 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450 2D6. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 2D6 enzymes.Type: ApplicationFiled: July 29, 2014Publication date: November 20, 2014Inventors: Michael EISSENSTAT, Dehui DUAN, Ji-Hye KANG
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Publication number: 20140343077Abstract: A compound of formula (I) useful for the treatment or prevention of hepatitis C viral infection, (Formula (I)) wherein: X1 and X2 are each independently CRB or N; RB is H, (C1-6)alkyl, (C1-6)haloalkyl, halo.Type: ApplicationFiled: August 22, 2012Publication date: November 20, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Christian Brochu, Chantal Grand-Maitre, Lee Fader, Cyrille Kuhn, Megan Bertrand-Laperle, Marc Pesant
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Publication number: 20140341986Abstract: Provided herein are methods for treating certain conditions, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a biguanide or related heterocyclic compound, e.g., metformin. Also provided herein are biguanide or related heterocyclic compound compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use.Type: ApplicationFiled: August 4, 2014Publication date: November 20, 2014Inventors: Alain D. Baron, Mark S. Fineman, Nigel R.A. Beeley
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Patent number: 8889197Abstract: Combinations, compositions and methods of use for modulating plant pathogen infection using plant extracts containing anthraquinone derivatives which induce resistance to plant phytopathogens and an antimicrobial agent, a biological control agent and/or a surfactant having fungicidal activity.Type: GrantFiled: July 29, 2010Date of Patent: November 18, 2014Assignee: Marrone Bio Innovations, Inc.Inventors: Hai Su, Marja Koivunen, Pamela G Marrone
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Patent number: 8889594Abstract: There is provided an agent for improving the growth of seedlings, having effects of raising healthy rice seedlings, such as increase of the tillering number, increase of root weight, enhancement of greenness, and increase of stem thickness. An agent for improving the growth of rice seedlings containing, as active ingredients, 5-aminolevulinic acid represented by formula (1), a derivative thereof or a salt of the acid or the derivative, and a gibberellin biosynthesis inhibitor: R2R1NCH2COCH2CH2COR3??(1) wherein R1 and R2 each independently represent a hydrogen atom, an alkyl group, an acyl group, an alkoxycarbonyl group, an aryl group or an aralkyl group; and R3 represents a hydroxyl group, an alkoxy group, an acyloxy group, an alkoxycarbonyloxy group, an aryloxy group, an aralkyloxy group or an amino group.Type: GrantFiled: March 26, 2009Date of Patent: November 18, 2014Assignee: Cosmo Oil Co., Ltd.Inventors: Yasutomo Takeuchi, Shigeyuki Funada
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Publication number: 20140336154Abstract: Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: July 29, 2014Publication date: November 13, 2014Inventors: Steven Do, Richard Goldsmith, Tim Heffron, Aleksandr Kolesnikov, Steven Staben, Alan G. Olivero, Michael Siu, Daniel P. Sutherlin, Bing-Yan Zhu, Paul Goldsmith, Tracy Bayliss, Adrian Folkes, Neil Pegg
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Publication number: 20140336230Abstract: The present invention provides a method for increasing metabolism and/or energy expenditure in a subject, e.g., to treat or prevent obesity and/or a related condition and/or the reduce adiposity, the method comprising increasing the level and/or activity of Hypoxia Induced Factor 1? (HIF-1?) in a cell, tissue or organ of the subject, thereby increasing metabolism in the subject. The present invention also provides a method for increasing metabolism in a subject, the method comprising administering an iron chelating agent to the subject, thereby increasing metabolism in the subject.Type: ApplicationFiled: December 4, 2013Publication date: November 13, 2014Applicant: Garvan Institute of Medical ResearchInventor: Jenny Gunton
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Patent number: 8883835Abstract: There is provided a plant disease controlling composition comprising at least one compound (A) selected from the group consisting of metconazole, bromuconazole and epoxyconazole, as well as a compound represented by the formula (I): as active ingredients. Also provided is a method for controlling a plant disease, which comprises applying at least one compound (A) selected from the group consisting of metconazole, bromuconazole and epoxyconazole, as well as the compound represented by the formula (I) to a plant, a seed of a plant or a cropland.Type: GrantFiled: March 24, 2009Date of Patent: November 11, 2014Assignee: Sumitomo Chemical Company, LimitedInventor: Masato Soma
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Publication number: 20140329835Abstract: Oral dosage forms as a biodegradable, water soluble film for delivering pharmaceutically active agents, to patients through insertion into the mouth of patient and methods for administering pharmaceutically active agents to patients by insertion into the mouth to provide selective uptake of said agents through the mucosa and thus avoiding the gastrointestinal tract.Type: ApplicationFiled: June 19, 2014Publication date: November 6, 2014Inventors: Je Phil Ryoo, Chun Kwong Chu, Zheng Wang
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Publication number: 20140329674Abstract: The present specification discloses honeybee repellents exhibiting repellent properties similar to 2-heptanone, compositions comprising such repellents, uses to repel a honeybee from a mammal, location, plant, structure treated of such repellents, and methods of treating a mammal, location, plant, structure by applying such repellents.Type: ApplicationFiled: May 3, 2014Publication date: November 6, 2014Applicant: INSCENT, INC.Inventors: Daniel F. Woods, Spiros Dimitratos, Robin W. Justice
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Publication number: 20140322293Abstract: The biodegradable drug delivery systems described here are formulated for implantation into the nail unit and its surrounding tissues for the treatment of various nail unit conditions. The systems include non-temperature dependent phase change compositions that may be formulated as solutions, solids, semisolids, microparticles, or crystals.Type: ApplicationFiled: April 29, 2014Publication date: October 30, 2014Applicant: Hallux, Inc.Inventors: Frank Kochinke, Corinne Bright
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Publication number: 20140322247Abstract: Disclosed herein are immunoconjugates comprising an inhibitor of Eg5 linked to an antigen binding moiety such as an antibody, that are useful for treating cell proliferative disorders. Also disclosed are novel inhibitors of Eg5 that can be used either alone or as part of an immunoconjugate to treat cell proliferation disorders. The Eg5 inhibitors include compounds of this formula as described herein: The invention further provides pharmaceutical compositions comprising these compounds and immunoconjugates, and compositions comprising the immunoconjugates or compounds with a therapeutic co-agent, and methods to use these compounds, conjugates and compositions for treating cell proliferation disorders.Type: ApplicationFiled: March 13, 2014Publication date: October 30, 2014Applicant: NOVARTIS AGInventors: Paul A. Barsanti, Sylvie Chamoin, Lionel Doumampouom-Metoul, Stephanie Guerro-Lagasse, Robert Martin Grotzfeld, Alexei Karpov, Marc Lafrance, Cristina Montserrat Nieto-Oberhuber, Grazia Piizzi
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Publication number: 20140323305Abstract: The present invention relates to the use of strobilurine type compounds of formula I and the N-oxides and the salts thereof for combating phytopathogenic fungi containing a mutation in the mitochondrial cytochrome b gene conferring resistance to Qo inhibitors, and to methods for combating such fungi. The invention also relates to novel compounds, processes for preparing these compounds, to compositions comprising at least one such compound, to plant health applications, and to seeds coated with at least one such compound.Type: ApplicationFiled: December 6, 2012Publication date: October 30, 2014Applicant: BASF SEInventors: Joachim Rheinheimer, Violeta Terteryan, Stefan Redlich, Doris Kremzow, Claudia Rosenbaum, Sebastian Georgios Rohrer, Wassilios Grammenos, Christian Pilger, Franz Roehl, Markus Gewehr, Gerd Stammler, Jurith Montag, Hubert Sauter
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Patent number: 8871792Abstract: 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: GrantFiled: June 6, 2013Date of Patent: October 28, 2014Assignee: Theravance Biopharma R&D IP, LLCInventors: Adam D. Hughes, Melissa Fleury
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Publication number: 20140315721Abstract: This document discloses molecules having the following formulas (“Formula One” & “Formula Two” and “Formula Three”) The Ar1, Het, Ar2, R1, R2, R3, R4, and R5 are further described herein.Type: ApplicationFiled: June 25, 2014Publication date: October 23, 2014Applicant: DOW AGROSCIENCES LLCInventors: Gary D. Crouse, Thomas C. Sparks, William H. Dent, III, CaSandra L. McLeod, Lawrence C. Creemer, David A. Demeter, Amanda E. Fritz, Lindsey G. Fischer, Erich W. Baum
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Publication number: 20140315953Abstract: A method for treating migraines is disclosed. The method utilizes a rapid drug delivery system which prevents deactivation or degradation of the active agent, including small molecules and peptides being administered to a patient in need of treatment. In particular, the drug delivery system is designed for inhalation for delivery of drugs to the pulmonary circulation in a rapid and therapeutically effective manner.Type: ApplicationFiled: June 16, 2014Publication date: October 23, 2014Inventors: Andrea Leone-Bay, Grayson W. Stowell, Joseph J. Guarneri, Dawn M. Carlson, Marshall Grant, Chad C. Smutney
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Publication number: 20140315967Abstract: In order to provide a compound which exhibits a high controlling effect against plant diseases and is able to reduce phytotoxicity, the present invention is a triazole derivative represented by General Formula (I), the azole derivative being a (?)-enantiomer or (+)-enantiomer having an —R1 group, hydroxy group, and substituted or unsubstituted benzyl group bonded to a cyclopentane ring in cis-form.Type: ApplicationFiled: November 16, 2012Publication date: October 23, 2014Inventors: Nobuyuki Araki, Taiji Miyake, Emiko Obata
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Publication number: 20140314676Abstract: The current application is directed to methods of treating or ameliorating myocardial ischemia, an acute coronary event, and a myocardial reperfusion injury comprising administering a therapeutically effective amount of deferiprone or a pharmaceutically acceptable salt thereof to a patient in need thereof. The application is also directed to reducing the risk for myocardial reperfusion injury as well as promoting the beneficial remodeling of cardiac tissue in a patient, comprising administering a therapeutically effective amount of deferiprone or a pharmaceutically acceptable salt thereof to a patient before, during or after reperfusion therapy. The application also includes methods of selecting a patient for treatment of reperfusion injury and subsequently treating the selected patient.Type: ApplicationFiled: November 16, 2012Publication date: October 23, 2014Inventors: Michael Spino, John Chalmers Connelly, John Charles Wood, Graham Arnold Wright, Nilesh Ramesh Ghugre
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Patent number: 8865755Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, r, Z, X, R3, and R5-7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: GrantFiled: November 20, 2012Date of Patent: October 21, 2014Assignee: Theravance Biopharma R&D IP, LLCInventors: Seok-Ki Choi, Paul R. Fatheree, Roland Gendron, Robert Murray McKinnell, Brooke Blair
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Patent number: 8865910Abstract: Invention provides antitubercular compounds selected from propargylated 1,2,3 triazoles of Formula I, wherein, X is sulfur(S) or a sulphone (A), n, m represent independently an integer O or 1, with the provision that when ‘n’ is 1, ‘m’ is 1; R1 is hydrogen; C1-C6 linear or branched alkyl group optionally substituted with aryl group; halogen; or aryl group optionally substituted with —OCH3, halogen, and nitro; R2 and R3 are selected from the group consisting of hydrogen, C1-C6 alkyl optionally substituted with heterocyclic ring of 5 to 6 ring atoms containing one to three hetero atoms selected from oxygen, sulfur, nitrogen, which may be substituted with alkyl, arylalkyl, linear or branched alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, or allyl or propargyl groups consisting of 1 to 6 carbon atoms; Z is C1-C6 alkyl optionally substituted with heterocyclic ring of 1 to 6 ring atoms, containing one to three hetero atoms selected from oxygen, sulfur, nitrogen, which may be substituted with arylalkyl,Type: GrantFiled: March 14, 2011Date of Patent: October 21, 2014Assignee: Council of Scientific & Industrial ResearchInventors: Dhiman Sarkar, Sunita Ranjan Deshpande, Shailaja Pramod Maybhate, Anjali Prabhakar Likhite, Sampa Sarkar, Arshad Khan, Preeti Madhukar Chaudhary, Sayalee Ramchandra Chavan
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Publication number: 20140308243Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, esters, or prodrugs thereof: Q-G-A-L-B—Z—W??(I), which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: April 16, 2014Publication date: October 16, 2014Applicant: ENANTA PHARMACEUTICALS, INC.Inventors: Yao-Ling Qiu, Hui Cao, Xiaowen Peng, Zhigang Chen, Yat Sun Or
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Publication number: 20140309267Abstract: The aromatase inhibitor 4,4?-[fluoro-(1-H-1,2,4-triazol-1-yl)methylene]bisbenzonitrile increases testosterone levels and treats hypogonadism and related diseases. A particular dosing regimen is disclosed as well as pharmaceutical compositions comprising said of 4,4?-[fluoro-(1-H-1,2,4-triazol-1-yl)methylene]bisbenzonitrile, optionally in combination with other active ingredients and kits comprising the pharmaceutical compositions.Type: ApplicationFiled: September 6, 2012Publication date: October 16, 2014Inventors: Ann Taylor, Lloyd B. Klickstein
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Patent number: 8859607Abstract: The present invention relates to crystalline complexes comprising at least one agriculturally active organic compound A having at least one functional moiety which is capable as serving as a hydrogen acceptor in a hydrogen bond and thiophanate-methyl.Type: GrantFiled: February 8, 2008Date of Patent: October 14, 2014Assignee: BASF SEInventors: Rafel Israels, Heidi Emilia Saxell, Matthias Bratz, Marco Kuhns, Peter Erk
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Patent number: 8859599Abstract: The present invention concerns compounds of general formula (I): Method of preparation and uses thereof.Type: GrantFiled: February 11, 2010Date of Patent: October 14, 2014Assignees: CNR—Consiglio Nazionale delle Ricerche, Istituto Scientifico Romagnolo per lo Studio e la Cura dei Tumori (I.R.S.T.) S.r.l.Inventors: Greta Varchi, Andrea Guerrini, Anna Tesei, Giovanni Brigliadori
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Publication number: 20140302010Abstract: The present invention relates to substituted benzimidazole compounds of general formula (I) in which R3, R5 and A are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: March 28, 2012Publication date: October 9, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Ulrich Klar, Marcus Koppitz, Duy Nguyen, Dirk Kosemund, Roland Neuhaus, Gerhard Siemeister
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Publication number: 20140302988Abstract: The invention relates to novel compounds of the formula (I) in which X, Y and CKE have the meanings given above, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides. The invention also relates to selective herbicidal compositions comprising, firstly, the 1,2,4-triazolyl-substituted ketoenols and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to the boosting of the action of crop protection compositions comprising, in particular, 1,2,4-triazolyl-substituted ketoenols, through the addition of ammonium salts or phosphonium salts and optionally penetrants, to the corresponding compositions, to processes for producing them and to their application in crop protection as insecticides and/or acaricides and/or for preventing unwanted plant growth.Type: ApplicationFiled: August 10, 2012Publication date: October 9, 2014Applicant: Bayer Intellectual Property GMBHInventors: Wolfgang Gienckle, Stefan Lehr, Reiner Fischer, David Stephen Lindell, Isolde Haeuser-Hahn, Ines Heinemann, Elmar Gatzweiler, Christopher Hugh Rosinger, Angela Becker, Arnd Voerste, Ulrich D.I. Goergens
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Publication number: 20140296198Abstract: Biomarkers associated with anti-estrogen sensitivity in cancers, methods for detecting and quantitating the biomarkers, and methods for treating cancer patients that exhibit the biomarkers are provided. The biomarkers are activated estrogen receptor foci (AEF) found in the nuclei of certain tumor cells. The methods provide new information to guide the intention to treat patients with anti-estrogens, allowing selection of individual patients and patient populations that are likely to respond to treatment. Also provided are methods for screening an antitumor drug or antitumor drug candidate for AEF inactivating activity. Such methods are useful to identify additional AEF-active drugs, including anti-estrogens, which may be candidates for use in treating AEF-positive tumors according to the methods of the invention.Type: ApplicationFiled: November 1, 2012Publication date: October 2, 2014Inventor: Erard Gilles
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Publication number: 20140296177Abstract: A new class of biotin protein ligase (BPL) inhibitors that have antibacterial activity against multiple Staphylococcus aureus isolates, including clinically important methicillin-resistant S. aureus (MRSA) are disclosed that are non-toxic.Type: ApplicationFiled: September 21, 2012Publication date: October 2, 2014Inventors: Andrew Abel, Steven Polyak, Grant Booker, John Wallace, Tatiana Soares Da Costa, Angie Jarrad, William Tieu, Kelly Lee Keeling, Daniel Sejer Pederson, Nicole Pendini, Matthew Wilce, Min Yin Yap
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Publication number: 20140294808Abstract: Methods of treating cancer with a compound of formulae (I) or (Ia) are disclosed. Also provided are methods of treating a cancer with a mutation in ALK or a c-MET mutation with a compound of formulae (I) or (Ia). Further provided are methods of treating non-small cell lung cancer with a mutation in ALK with a compound of formulae (I) or (Ia); a tautomer, or a pharmaceutically acceptable salt thereof, wherein the variables structural formulae are defined herein.Type: ApplicationFiled: July 9, 2012Publication date: October 2, 2014Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: Iman El-Hariry, David Proia, Vojo Vukovic
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Patent number: 8846739Abstract: TGR5 agonists of structural formula VIII(Q), wherein X, R1, R2, and R5 are defined in the specification, pharmaceutically acceptable salts thereof, compositions thereof, and use of the compounds and compositions for treating diseases. The invention also comprises use of the compounds in and for the manufacture of medicaments, particularly for treating diseases.Type: GrantFiled: August 11, 2010Date of Patent: September 30, 2014Assignee: Exelixis Patent Company LLCInventors: Venkataiah Bollu, Brant Clayton Boren, Jackaline Dalgard Julien, Brenton T. Flatt, Nadia Haq, Sarah Hudson, Raju Mohan, Michael Morrissey, Benjamin Pratt
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Patent number: 8846566Abstract: PROBLEM There are provided a composition for controlling plant diseases and a method for controlling plant diseases having excellent control effect for plant diseases. SOLUTION A composition for controlling plant diseases comprising, as active ingredients, a compound represented by formula (1), wherein X1 represents a methyl group, a difluoromethyl group or an ethyl group; X2 represents a methoxy group or a methylamino group; and X3 represents a phenyl group, a 2-methylphenyl group or a 2,5-dimethylphenyl group, and at least one azole compound selected from the group consisting of bromuconazole, cyproconazole, difenoconazole, fenbuconazole, fluquinconazole, hexaconazole, imibenconazole, ipconazole, myclobutanil, prothioconazole, simeconazole, tetraconazole, triticonazole and metconazole.Type: GrantFiled: November 20, 2009Date of Patent: September 30, 2014Assignee: Sumitomo Chemical Company, LimitedInventors: Masanao Takaishi, Masato Soma
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Patent number: 8846737Abstract: There is provided a compound of formula I wherein Z is selected from N and CR22, wherein R22 is H or a bond with D; wherein D is selected from a bond, C?O, and linear or branched hydrocarbon groups having a carbon chain of from 1 to 6 carbon atoms, wherein the carbon chain optionally contains an oxy group (?O), an ether (—O—) or thioether (—S—) link, wherein R1 is selected from: triazolyl, imidazolyl, pyrimidinyl radical wherein each of R2 to R6 is independently selected from —H, NO2, halo, —CN, —N[(C?O)0-1R12][(C?O)0-1R13] and —(CH2)0-1R14, or two adjacent groups of R2 to R6, together with the carbon atoms to which they are attached, form a ring, wherein at least one of R2 to R6 is —CN, wherein (i) at least one of R2 to R6 is —(CH2)0-1R14, or (ii) at least one of R2 to R6 is —N[(C?O)0-1R12][(C?O)0-1R13], or (iii) at least two adjacent groups of R2 to R6 together with the carbon atoms to which they are attached, form a ring, or (iv) at least one of R2 to R6 is —(CH2)0-1—O—R?14, wherein R12 and R13Type: GrantFiled: August 23, 2010Date of Patent: September 30, 2014Assignee: Sterix LimitedInventors: Lok Wai Lawrence Woo, Christian Bubert, Paul Michael Wood, Aurélien Putey, Atul Purohit, Barry Victor Lloyd Potter
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Patent number: 8846738Abstract: The novel active compound combinations comprising 2-[2-(1-chlorocyclopropyl)-3-(2-chlorophenyl)-2-hydroxypropyl]-2,4-dihydro-[1,2,4]-triazole-3-thione of the formula and the active compound of groups (1) to (24) listed in the description have very good fungicidal properties.Type: GrantFiled: January 15, 2013Date of Patent: September 30, 2014Assignee: Bayer Intellectual Property GmbHInventors: Stefan Dutzmann, Klaus Stenzel, Manfred Jautelat
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Publication number: 20140288050Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as pain, neurological disorders, psychiatric disorders, and neuromuscular disorders. Compounds provided herein modulate the activity of opioid receptor (e.g., ?-opioid receptor) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.Type: ApplicationFiled: November 7, 2012Publication date: September 25, 2014Inventors: Scott Malcolm, Carrie Bowen, Laurence Melnick, Linghong Xie
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Publication number: 20140288136Abstract: Methods are provided for treating or preventing chronic obstructive pulmonary diseases such as emphysema, and fibrotic diseases including heart, liver, kidney and vascular diseases, by administering to a subject a pharmaceutical composition comprising a compound that inhibits cytochrome P450RA or CYP26.Type: ApplicationFiled: February 23, 2014Publication date: September 25, 2014Inventors: Lambertus J.W.M Oehlen, Bijoy Panicker
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Publication number: 20140274688Abstract: This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Nematoda, Arthropoda, and/or Mollusca, processes to produce such molecules and intermediates used in such processes, compositions containing such molecules, and processes of using such molecules against such pests. These molecules may be used, for example, as nematicides, acaricides, insecticides, miticides, and/or molluscicides. This document discloses molecules having the following formula (“Formula One”).Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Applicant: DOW AGROSCIENCES LLCInventors: Lindsey G. Fischer, Erich W. Baum, Gary D. Crouse, Carl DeAmicis, Beth Lorsbach, Jeff Petkus, Thomas C. Sparks, Gregory T. Whiteker
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Publication number: 20140271825Abstract: The present invention provides liposomes loaded with chelating agents, pharmaceutical formulations including these liposomes and methods of making chelating agent liposomes. Because the chelating agents are loaded in the liposome with high efficiencies, the liposomes are of use in treatment of metal ion overload in subjects. The liposomes can include two or more different chelating agents of different structures and affinities for metal ions.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Inventors: Mark E. HAYES, Charles O. NOBLE, Francis C. SZOKA, JR.
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Publication number: 20140275173Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR120 G protein-coupled receptor modulators which may be used as medicaments.Type: ApplicationFiled: March 12, 2014Publication date: September 18, 2014Inventors: Hao Zhang, Peter T.W. Cheng, Sean Chen, Shiwei Tao, Shung C. Wu, Lidet A. Negash
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Publication number: 20140275047Abstract: This disclosure relates to the field of molecules having pesticidal utility against pests in phyla Nematoda, Arthropoda, and/or Mollusca, processes to produce such molecules and intermediates used in such processes, compositions containing such molecules, and processes of using such molecules against such pests. These molecules may be used, for example, as nematicides, acaricides, insecticides, miticides, and/or molluscicides. This document discloses molecules having the following formula (“Formula One”).Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Applicant: DOW AGROSCIENCES LLCInventors: Lindsey G. Fischer, Erich W. Baum, Gary D. Crouse, Jeff Petkus, Andrew L. Ward, Thomas C. Sparks
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Publication number: 20140275194Abstract: The invention relates to film products including a polymer component and a therapeutically effective amount of rizatriptan or a pharmaceutically acceptable salt thereof. The invention further relates to film products including a polymer component and a therapeutically effective amount of rizatriptan benzoate.Type: ApplicationFiled: March 15, 2013Publication date: September 18, 2014Inventors: Eric Dadey, Alexander Mark Schobel, Daniel R. Barber, Garry L. Myers
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Publication number: 20140271923Abstract: Patients inflicted with various clustering chronic diseases require treatment with multiple drugs having distinct mechanisms of action. Accordingly, patients with multiple conditions suffer from cumulative side effects of multiple drugs as well as drug-drug interactions. Embodiments, agents, compounds or drugs of the present invention, such as sesquiterpenes, e.g., Zerumbone, replace an equal or larger number of approved drugs during patient treatment. Examples of disorders prevented or ameliorated by administration of the formulations of this invention include but are not limited to inflammatory diseases that may be, oncological, genetic, ischemic, infectious, neurological, hematological, ophthalmological, rheumatoid, orthopedic, neurological, hematological, kidney, vascular, dermatological, gynecological, or obstetric.Type: ApplicationFiled: March 14, 2013Publication date: September 18, 2014Inventor: Christopher Brian Reid
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Publication number: 20140255386Abstract: The present invention is a method for identifying agents which modulate microRNA activity. The invention involves contacting a cell harboring a microRNA and a microRNA binding sequence, which is operably linked to a nucleic acid molecule encoding a reporter protein, with a test agent and determining whether the test agent increases or decreases the expression of the reporter protein thereby identifying a microRNA modulator. Antagonists identified by this screening assay are provided, as are methods for using the same to inhibit microRNA activity and prevent or treat disease.Type: ApplicationFiled: July 24, 2012Publication date: September 11, 2014Applicants: NORTH CAROLINA STATE UNIVERSITY, THE WISTAR INSTITUTEInventors: Qihong Huang, Alexander Deiters, Kiranmai Gumireddy
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Publication number: 20140256716Abstract: The invention relates to the use of C16-C18-carboxylic acid dibutylamides in agrochemical formulations, agrochemical formulations which comprise such compounds and the use as tank mix additives.Type: ApplicationFiled: August 10, 2012Publication date: September 11, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Peter Baur, Martin Steinbeck, Ingo Wetcholowsky, Thomas Auler, Alison Daniels, Rolf Pontzen