1,2-oxazoles (including Hydrogenated) Patents (Class 514/378)
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Publication number: 20140256700Abstract: The present invention is directed to carbazole compounds, pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.Type: ApplicationFiled: February 26, 2014Publication date: September 11, 2014Inventors: Michael A. Poss, David R. Tortolani, Dharmpal S. Dodd, Christopher P. Mussari, John S. Tokarski, Ashvinikumar V. Gavai, Yufen Zhao, George V. Delucca, Daniel O'Malley, Derek J. Norris, Patrice Gill, Claude A. Quesnelle, Wen-Ching Han
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Patent number: 8828992Abstract: Provided are a substituted azole derivative and pharmaceutically acceptable salts thereof, a pharmaceutical composition including an effective amount of the derivative, and a method for treating Parkinson's disease in a mammal including administering an effective amount of the compound to the mammal. The azole derivative of the following Formula (I) and pharmaceutically useful salts thereof have an efficacy against Parkinson's disease from inhibitory effects of the activity of MAO-B.Type: GrantFiled: February 25, 2010Date of Patent: September 9, 2014Assignee: SK Biopharmaceuticals Co., Ltd.Inventors: Cheol-Hyoung Park, Hye-Kyung Min, Mi-Jung Lim, Ji-Won Lee, Jin-Yong Chung, Choon-Ho Ryu, Yeo-Jin Yoon, Mi-Kyung Ji, Joo-Young Park
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Patent number: 8828908Abstract: Bicyclic dione compounds of formula (I), and derivatives thereof, which are suitable for use as herbicides.Type: GrantFiled: May 27, 2008Date of Patent: September 9, 2014Assignee: Syngenta LimitedInventors: Christopher John Mathews, Matthew Brian Hotson, Alan John Dowling, James Nicholas Scutt, Mangala Govenkar, Lee Challinor
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Patent number: 8822517Abstract: Arylsulphonamide derivatives of formula (I) and pharmaceutically acceptable salts thereof. The compounds may be useful for the treatment and/or prevention of disorders of the central nervous system.Type: GrantFiled: September 16, 2011Date of Patent: September 2, 2014Assignee: Adamed SP. Z O.O.Inventors: Marcin Kolaczkowski, Piotr Kowalski, Jolanta Jaśkowska, Monika Marcinkowska, Katarzyna Mitka, Adam Bucki, Anna Wesolowska, Maciej Pawlowski
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Patent number: 8822466Abstract: 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: GrantFiled: March 9, 2012Date of Patent: September 2, 2014Assignee: Novartis AGInventors: Noëlle Gauvry, Steve Nanchen
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Patent number: 8822502Abstract: A compound of formula (I): wherein A1, A2, A3, A4, A1?, A2?, A3?, A4?, A5?, A6?, G1, R1, R2, R3, R4, R5a and R5b 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) or compounds of formula (I?), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising compounds of formula (I) or compounds of formula (I?), and to methods of using compounds of formula (I) or compounds of formula (I?) to combat and control insect, acarine, nematode and mollusc pests.Type: GrantFiled: July 24, 2009Date of Patent: September 2, 2014Assignee: Syngenta Crop Protection LLCInventors: Thomas Pitterna, Myriem El Qacemi, Vladimir Bobosik, Peter Renold, Jérôme Yves Cassayre, Pierre Joseph Marcel Jung
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Publication number: 20140243322Abstract: Described herein are compounds capable of modulating one or more biomolecules substantially simultaneously, e.g., modulating two or more binding domains (e.g., bromodomains) on a protein or on different proteins.Type: ApplicationFiled: February 28, 2014Publication date: August 28, 2014Applicant: Coferon, Inc.Inventors: Lee Daniel Arnold, Kenneth W. Foreman, Douglas S. Werner
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Publication number: 20140242091Abstract: Methods are provided for treating pathologies associated with hypoxia with an MIF inhibitor. Methods are also provided for treating a subject having, or at risk for pulmonary hypertension, with an MIF inhibitor. Methods are also provided for reating a subject having, or at risk from, a CNS disorder associated with hypoxia, with an MIF inhibitor. Methods are also provided of treating severe chronic lung disease, hypoxia-induced right ventricular hypertrophy or hypoxia-induced pulmonary vascular remodeling with an MIF inhibitor. Methods of diagnosing a subject with pulmonary hypertension are also provided.Type: ApplicationFiled: May 13, 2014Publication date: August 28, 2014Applicant: The Feinstein Institute For Medical ResearchInventors: Edmund Miller, Yousef Al-Abed, Yinzhong Zhang, Kai Fan Cheng
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Publication number: 20140243362Abstract: The present invention is directed to novel retinoid-related orphan receptor gamma (ROR?) modulators of formula (I), processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by ROR? wherein R1 to R7 are as defined in claim 35.Type: ApplicationFiled: September 25, 2012Publication date: August 28, 2014Inventors: Veronique Birault, Amanda Jennifer Campbell, Stephen Harrison, Joelle Le
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Publication number: 20140235622Abstract: The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.Type: ApplicationFiled: January 28, 2014Publication date: August 21, 2014Applicant: Arena Pharmaceuticals, Inc.Inventors: Bradley Teegarden, Dennis Chapman, Juyi Choi, Konrad Feichtinger, Sangdon Han, Honnappa Jayakumar, Thuy-Anh Tran, Jay Xu, Ning Zou
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Publication number: 20140235660Abstract: The present invention relates to compounds of formula I: in which n, m, X, Y1, R1, R2, R3, R4 and R5 are defined in the Summary of the Invention; capable of being both potent antagonists and degraders of estrogen receptors. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with aberrant estrogen receptor activity.Type: ApplicationFiled: February 12, 2014Publication date: August 21, 2014Applicant: NOVARTIS AGInventors: Heather Elizabeth BURKS, Michael A. DECHANTSREITER, Guo HE, Jill NUNEZ, Stefan PEUKERT, Clayton SPRINGER, Yingchuan SUN, Noel Marie-France THOMSEN, George Scott TRIA, Bing YU
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Publication number: 20140228416Abstract: 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: ApplicationFiled: September 12, 2013Publication date: August 14, 2014Applicant: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
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Patent number: 8796320Abstract: Provided is a 1,3,4-oxadiazole-2-carboxamide compound which has STAT3 inhibitory activity and is useful as an anticancer agent. Provided is a 1,3,4-oxadiazole-2-carboxamide compound represented by formula (I) or a pharmacologically acceptable salt thereof (in the formula, Ar represents a furyl group or the like; R1 represents a hydrogen atom or the like; and —X—Y represents a diaryl group such as a biphenyl group).Type: GrantFiled: December 28, 2010Date of Patent: August 5, 2014Assignees: General Incorporated Association Pharma Valley Project Supporting Organization, Pharma Design, Shizuoka Prefecture, Kumamoto Health Science University, Kabushiki Kaisha Yakult HonshaInventors: Akira Asai, Kenji Matsuno, Naohisa Ogo, Osamu Takahashi, Yoshiaki Masuda, Ayumu Muroya, Yasuto Akiyama, Tadashi Ashizawa, Tadashi Okawara
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Patent number: 8796273Abstract: The present invention relates to the treatment, alleviation, prevention or reduction in the incidence of symptoms, diseases or conditions resulting from or associated with enteroviruses, more particularly the enteroviral infections they cause.Type: GrantFiled: June 24, 2011Date of Patent: August 5, 2014Assignee: Biota Scientific Management Pty LtdInventors: Johan Neyts, Armando De Palma, Hendrik Jan Thibaut, Pieter Leyssen, Simon Tucker
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Publication number: 20140213611Abstract: The present invention provides compounds of formula (I): compositions comprising such compounds; the use of such compounds in therapy (for example in the treatment or prevention of a disease or condition in which plasma kallikrein activity is implicated); and methods of treating patients with such compounds; wherein R1 to R9 are as defined herein.Type: ApplicationFiled: July 6, 2012Publication date: July 31, 2014Applicant: KalVista Pharmaceuticals LimitedInventors: David Michael Evans, Rebecca Louise Davie, Hannah Joy Edwards, David Philip Rooker
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Publication number: 20140206668Abstract: 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: March 25, 2014Publication date: July 24, 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: 20140206633Abstract: The present invention relates to processes for the preparation of compounds of formula IB wherein A1, A2, A3, A4, L, Y1, Y2, R1, R2, R3, R4 and R5 are as defined in the claims, comprising reacting a compound of formula (II) wherein Y1, Y2, L, A1, A2, R1, R2, R3, R4 and R5 are as defined for the compound of formula (I); with hydroxylamine in the presence of water, a base and a chiral phase transfer catalyst, which chiral phase transfer catalyst is a quinine derivative. The invention also relates to compounds of formula IB and enantiomerically enriched mixtures comprising compounds of formula IB.Type: ApplicationFiled: February 3, 2011Publication date: July 24, 2014Applicant: SYNGENTA CROP PROTECTION LLCInventors: Nicholas Phillip Mulholland, Edouard Godineau, Jérôme Yves Cassayre, Peter Renold, Myriem El Qacemi, Guillaume Revol
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Publication number: 20140206606Abstract: The present invention provides compounds of formula (I), wherein G1 is oxygen; R1 is hydrogen; R2 is group P (P) L is a bond, methylene or ethylene; one of A1 and A2 is S, SO or SO2 and the other is —C(R4)R4—R3 is hydrogen or methyl; each R4 is independently hydrogen or methyl; Y1 is C—R6, CH or nitrogen; Y2 and Y3 are independently CH or nitrogen; wherein no more than two of Y1, Y2 and Y3 are nitrogen and wherein Y2 and Y3 are not both nitrogen; R5 is hydrogen, halogen, cyano, nitro, NH2, C1-C2alkyl, C1-C2haloalkyl, C3-C5cycloalkyl, C3-C5halocycloalkyl, C1-C2alkoxy, C1-C2haloalkoxy; R6 together with R5 forms a —CH?CH—CH?CH— bridge; X2 is C—X6 or nitrogen; X1, X3 and X6 are independently hydrogen, halogen or trihalomethyl, wherein at least two of X1, X3 and X6 are not hydrogen; X4 is trifluoromethyl, difluoromethyl or chlorodifluoromethyl.Type: ApplicationFiled: August 24, 2012Publication date: July 24, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Jerome Yves Cassayre, Peter Renold, Thomas Pitterna, Myriem El Qacemi
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Publication number: 20140206676Abstract: In one aspect, the invention relates to substituted 4-(1H-pyrazol-4-yl)benzyl analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: January 12, 2013Publication date: July 24, 2014Applicant: Vanderbilt UniversityInventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, Michael S. Poslusney, James C. Tarr
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Patent number: 8785489Abstract: Disclosed are compounds and compositions of the formula I as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula I.Type: GrantFiled: October 13, 2009Date of Patent: July 22, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Asitha Abeywardane, Bennett Farmer, Neil Alexander Farrow, Donghong Amy Gao, Alexander Heim-Riether, Lana Louise Smith Keenan, Ingo Andreas Mugge, Steven John Taylor, Zhaoming Xiong, Yang Yu, Qiang Zhang
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Patent number: 8785485Abstract: The present invention provides an animal ectoparasite-controlling agent containing as an active ingredient a hydrazide compound represented by the formula (1) wherein R3 represents a fluorine atom, a chlorine atom, a bromine atom, a methyl group, an ethyl group or a hydrogen atom, R5 and R6 are the same or different each other and each represents a methyl group or a hydrogen atom, R4 represents a C1-C6 haloalkyl group, which shows excellent controlling effects on animal ectoparasites.Type: GrantFiled: July 29, 2011Date of Patent: July 22, 2014Assignee: Sumitomo Chemical Company, LimitedInventor: Kaori Ikari
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Publication number: 20140200189Abstract: Artonin I is reported to treat multi-drug resistant Staphlococcus infections.Type: ApplicationFiled: January 14, 2013Publication date: July 17, 2014Inventors: Muhammad Iqbal Choudhary, Saba Farooq, Atia-tul-Wahab, Christian D.A. Fozing
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Publication number: 20140199320Abstract: The invention provides inhibitors capable of binding to a member of the inflammasome group comprised of IL-1?, IL-1 receptor type 1, NLRP3, ASC, Caspase-1 and cathepsin B with a dissociation constant of 10-8 mol/l or smaller for the prevention and treatment of acne, specifically an antibody, an antibody fragment, an antibody-like molecule, an oligopeptide of 6 to 30 amino acid residues, a nucleic acid aptamer molecule of 10 to 75 nucleotides in length or a soluble polypeptide comprising a contiguous amino acid sequence of at least 30 amino acids comprised within the protein sequence of a member of the group comprised of IL-1?, IL-1 receptor type 1, IL-1 receptor type 2, NLRP3, ASC and Caspase-1. Similarly, an interfering RNA or an antisense modulator of gene expression of IL-1?, I L-1? receptor type 1, NLRP3, ASC, Caspase-1 and cathepsin B are provided for the prevention or treatment of acne.Type: ApplicationFiled: July 11, 2012Publication date: July 17, 2014Applicant: UNIVERSITAT ZURICHInventors: Dragana Jankovic, Magdalena Kistowiska, Emmanuel Contassot, Lars E. French, Samuel Gehrke
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Patent number: 8778983Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.Type: GrantFiled: September 29, 2010Date of Patent: July 15, 2014Assignee: Amira Pharmaceuticals, Inc.Inventors: Ryan Clark, Brian Andrew Stearns, Lucy Zhao, Thomas Jon Seiders, Deborah Volkots, Jeannie M. Arruda, David Nathan Zalatan
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Patent number: 8778940Abstract: The present invention relates to compounds and methods for inducing neuronal differentiation in normal neural stem cells and brain cancer stem cells. The methods may take place in vitro, such as in isolates from the adult mammalian brain, or in vivo. Compounds and methods described herein may find use in the treatment of neurodegenerative and psychiatric diseases, the repair and regeneration of the nervous system, and in treatment of neurologic malignancy.Type: GrantFiled: June 4, 2012Date of Patent: July 15, 2014Assignee: The Board of Regents of the University of Texas SystemInventors: Jay Schneider, Jenny Hsieh, Douglas Frantz, Steven L. McKnight, Joseph M. Ready
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Publication number: 20140194376Abstract: The present invention provides compounds of formula (I) wherein G1 is oxygen; R1 is hydrogen; R2 is group (P) L is a bond, methylene or ethylene; one of A1 and A2 is S, SO or SO2 and the other is —C(R4)R4—; R3 is hydrogen or methyl; each R4 is independently hydrogen or methyl; Y2 and Y3 are independently CH or nitrogen, wherein Y2 and Y3 are not both nitrogen; X2 is C—X6 or nitrogen; X1, X3 and X6 are independently hydrogen, halogen or trihalomethyl, wherein at least two of X1, X3 and X6 are not hydrogen; X4 is trifluoromethyl, difluoromethyl or chlorodifluoromethyl. The invention also provides intermediates useful for the preparation of compounds of formula (I), as well as methods of controlling insects, acarines, nematodes or molluscs using the compounds of formula (I).Type: ApplicationFiled: August 24, 2012Publication date: July 10, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Jerome Yves Cassayre, Peter Renold, Thomas Pitterna, Myriem El Qacemi
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Publication number: 20140194425Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.Type: ApplicationFiled: March 11, 2014Publication date: July 10, 2014Applicant: N30 Pharmaceuticals, Inc.Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
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Publication number: 20140194480Abstract: The present invention provides a method for controlling termites comprising applying a liquid formulation comprising a compound of formula I to a location where termite control is needed or is expected to be needed, wherein the compound of formula (I) is wherein X is optionally substituted aryl, optionally substituted heterocyclyl, or a group selected from X1 to X5 cycle A is aryl or heteroaryl; cycle B is a saturated or partially unsaturated heterocyclyl; cycle C is aryl or heteroaryl; R1, R2, R3, R4, R5, R6 and R8 are independently hydrogen or an organic radical; R7 is haloalkyl; G is oxygen or sulfur; L is O, NH, NR1, CR3R4; n is 0, 1, 2, 3, 4 or 5; o is 0, 1, 2, 3, 4 or 5; p is 1, 2, 3, 4 or 5. The invention also relates to methods for protecting man-made structures from termites using the compounds of formula I as well as termite baits comprising the compound of formula I.Type: ApplicationFiled: August 27, 2012Publication date: July 10, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Mark Hoppe, Myriem El Qacemi, Jerome Yves Cassayre
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Patent number: 8772336Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.Type: GrantFiled: October 11, 2012Date of Patent: July 8, 2014Assignees: Merck Frosst Canada Ltd., Axys Pharmaceuticals, Inc.Inventors: Christopher I. Bayly, Cameron Black, Serge Leger, Chun Sing Li, Dan McKay, Christophe Mellon, Jacques Yves Gauthier, Vouy-Linh Truong, Cheuk Lau, Michel Therien, Michael J. Green, Bernard L. Hirschbein, James William Janc, James T. Palmer, Chitra I. Baskaran
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Patent number: 8772296Abstract: Benzamide derivatives of formula I are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders: wherein R1, R2, R3, R4, R5, R6, R7, R8, and n are as defined herein.Type: GrantFiled: May 31, 2007Date of Patent: July 8, 2014Assignee: Amgen Inc.Inventors: Jay P. Powers, Michael Degraffenreid, Lisa Julian, Jacob Kaizerman, Dustin McMinn, Yosup Rew, Daqing Sun, Xuelei Yan, Zhulun Wang, Felix Gonzalez Lopez De Turiso
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Publication number: 20140187592Abstract: The present invention provides a compound having excellent regulating action on blood lipid level. The present invention provides a compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, etc., wherein A represents a 5-membered nitrogen-containing aromatic heterocyclyl group; R1 represents COOH or the like; each R2 represents an alkyl or the like; each R3 represents an optionally substituted phenyl, an optionally substituted phenylalkyl, or the like; m represents 0, 1, 2, or 3; n represents 0 or 1; each of R4, R5, R6, and R7 represents H, an alkyl, or the like; and B represents an optionally substituted naphthyl, an optionally substituted aromatic heterocyclyl, or a group represented by the following formula (II) wherein each of B1 and B2 represents an optionally substituted phenyl or an optionally substituted aromatic heterocyclyl.Type: ApplicationFiled: February 10, 2014Publication date: July 3, 2014Applicant: Daiichi Sankyo Company, LimitedInventors: Keiko Suzuki, Takahiro Yamaguchi, Akihiro Tamura, Tomohiro Nishizawa, Mitsuhiro Yamaguchi
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Patent number: 8765735Abstract: The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient. The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof.Type: GrantFiled: May 18, 2010Date of Patent: July 1, 2014Assignee: Infinity Pharmaceuticals, Inc.Inventors: Mark L. Behnke, Alfredo C. Castro, Lawrence K. Chan, Catherine A. Evans, Louis Grenier, Michael J. Grogan, Yves Leblanc, Tao Liu, Stephane Peluso, Daniel A. Snyder, Thomas T. Tibbitts
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Patent number: 8765812Abstract: Substituted cinnamoyl anthranilate compounds exhibiting anti-fibrotic activity; or derivatives thereof, analogues thereof, pharmaceutically acceptable salts thereof, and metabolites thereof; with the proviso that the compound is not Tranilast.Type: GrantFiled: July 5, 2007Date of Patent: July 1, 2014Assignee: Fibrotech Therapeutics Pty LtdInventors: Spencer John Willams, David Stapleton, Steven Zammit, Darren James Kelly, Richard Ernest Gilbert, Henry Krum
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Patent number: 8765788Abstract: The present invention provides tricyclic compounds according to formula (I): (I) where R1, R2, R3, W, X, Y, Z, m, n, and p are as defined in the description; as well as pharmaceutical compositions comprising the same, methods of use of the compounds and compositions of the invention for the treatment of conditions associated with hydroxysteroid dehydrogenases (e.g., 11-HSD1), and the use of the compounds of the invention in the preparation of medicaments for the treatment of hydroxysteroid dehydrogenase-associated conditions.Type: GrantFiled: June 11, 2008Date of Patent: July 1, 2014Assignee: Amgen Inc.Inventors: Jay P. Powers, Daqing Sun, Xuelei Yan, Lisa Julian, Felix Gonzalez Lopez De Turiso
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Publication number: 20140179687Abstract: The present invention relates to a compound of formula (I): wherein: n is 0, 1 or 2; A is in particular CH or N; X is in particular CO, SO2, CS, and R1 is in particular H, R2 is a group of formula NR3R4 or OR5, R3 and R4 being in particular H, and R5 an alkyl group, R6 is in particular H or an alkyl group, and R7 is in particular an aryl group, for its use in the prevention and/or the treatment of viral pathologies or infections.Type: ApplicationFiled: February 21, 2014Publication date: June 26, 2014Applicant: Institut National de la Sante et de la Recherche Medicale (INSERM)Inventors: Jean-Francois Guichou, Lionel Colliandre, Hakim Ahmed-Belkacem, Jean-Michael Pawlotsky
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Patent number: 8759537Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, M, W, R1, R2, R6, R7, R8 have meanings given in the description.Type: GrantFiled: August 17, 2011Date of Patent: June 24, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Henning Priepke, Henri Doods, Raimund Kuelzer, Roland Pfau, Dirk Stenkamp, Benjamin Pelcman, Robert Roenn
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Publication number: 20140171475Abstract: An animal ectoparasite-controlling agent comprising a benzylamide compound represented by the formula (1): wherein R3 represents a hydrogen atom; a halogen atom; a cyano group; a C1-C6 alkyl group; a C1-C6 haloalkyl group; a C1-C6 alkoxy group or a C1-C6 haloalkoxy group; and R4 represents a C1-C6 alkyl group substituted with one or more C1-C6 alkoxy group(s); a C1-C6 alkyl group substituted with one or more cyano group(s); a C1-C6 alkyl group; a C1-C6 haloalkyl group or a C3-C6 cycloalkyl group, as an active ingredient and an inert carrier, has an excellent controlling effect on animal ectoparasites.Type: ApplicationFiled: May 15, 2012Publication date: June 19, 2014Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventor: Kaori Ikari
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Patent number: 8754053Abstract: The present invention relates to compounds formula (I), wherein P is P1, P2, heterocyclyl or heterocyclyl substituted by one to five Z; and wherein A1, A2, A3, A4, G1, R1, R2, R3, R4, R5, R6, R17, R18, R19 and R20 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: GrantFiled: February 17, 2011Date of Patent: June 17, 2014Assignee: Syngenta Crop Protection LLCInventors: Thomas Pitterna, Myriem El Qacemi, Jerome Yves Cassayre, Peter Renold, Vladimir Bobosik
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Publication number: 20140163032Abstract: The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.Type: ApplicationFiled: February 18, 2014Publication date: June 12, 2014Applicant: ARENA PHARMACEUTICALS, INC.Inventors: BRADLEY TEEGARDEN, Dennis Chapman, Marc Decaire, Peter I. Dosa, Konrad Feichtinger, HONNAPPA JAYAKUMAR, THUY-ANH Tran, Sonja Strah-Pleynet, Jay Xu
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Patent number: 8748466Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors and, more specifically, their use to treat bacterial infections.Type: GrantFiled: March 23, 2012Date of Patent: June 10, 2014Assignee: Pfizer Inc.Inventors: Joseph Alan Abramite, Matthew Frank Brown, Jinshan Michael Chen, Michael Joseph Melnick, Justin Ian Montgomery, Usa Reilly
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Patent number: 8748627Abstract: The present invention relates to compounds of formula (I), which inhibit acetyl-CoA carboxylase (ACC) and are useful for the prevention or treatment of metabolic syndrome, type II diabetes, obesity, atherosclerosis and cardiovascular diseases in humans.Type: GrantFiled: February 15, 2007Date of Patent: June 10, 2014Assignee: AbbVie Inc.Inventors: Yu Gui Gu, Moshe Weitzberg, Xiangdong Xu, Richard F. Clark, Tianyuan Zhang, Qun Li, Todd M. Hansen, Hing Sham, Bruce A. Beutel, Heidi S. Camp, Xiaojun Wang
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Patent number: 8748431Abstract: 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: GrantFiled: November 25, 2011Date of Patent: June 10, 2014Assignee: Syngenta Participations AGInventors: Sarah Sulzer-Mosse, Clemens Lamberth, Mathias Stephan Respondek, Laura Quaranta, Fredrik Cederbaum, Guillaume Berthon
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Publication number: 20140155381Abstract: The present invention relates to novel retinoid-related orphan receptor gamma (ROR?) modulators and their use in the treatment of diseases mediated by ROR?.Type: ApplicationFiled: July 27, 2012Publication date: June 5, 2014Inventors: Erkan Baloglu, Gary J. Bohnert, Shomir Ghosh, Mercedes Lobera, Darby R. Schmidt, Leonard Sung
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Publication number: 20140155377Abstract: The present invention relates to 3-cycloalkylaminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, Y and Z are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as modulators of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.Type: ApplicationFiled: February 6, 2014Publication date: June 5, 2014Applicant: Incyte CorporationInventors: Chu-Biao Xue, Brian W. Metcalf, Amy Qi Han, Darius J. Robinson, Changsheng Zheng, Anlai Wang, Yingxin Zhang
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Patent number: 8741299Abstract: Methods are provided for treating pathologies associated with hypoxia with an MIF inhibitor. Methods are also provided for treating a subject having, or at risk for pulmonary hypertension, with an MIF inhibitor. Methods are also provided for treating a subject having, or at risk from, a CNS disorder associated with hypoxia, with an MIF inhibitor. Methods are also provided of treating severe chronic lung disease, hypoxia-induced right ventricular hypertrophy or hypoxia-induced pulmonary vascular remodeling with an MIF inhibitor. Methods of diagnosing a subject with pulmonary hypertension are also provided.Type: GrantFiled: June 20, 2012Date of Patent: June 3, 2014Assignee: The Feinstein Institute for Medical ResearchInventors: Edmund Miller, Yousef Al-Abed, Yinzhong Zhang, Kai Fan Cheng
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Publication number: 20140148398Abstract: Compounds useful for the treatment of giardiasis are described.Type: ApplicationFiled: October 12, 2011Publication date: May 29, 2014Applicants: The United States of America, as represented by the Secretary, Dept. of Health and Human Service, UNIVERSITY OF MARYLAND, COLLEGE PARKInventors: Wei Zheng, Catherine Chen, Juan Jose Marugan, Noel Southall, Christopher P. Austin, Andrey Galkin, Liudmila Kulakova, Osnat Herzberg
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Patent number: 8735385Abstract: The present disclosure relates to a series of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and formula (Ib). wherein R1, R2, R3, R4, X, m, l, n, p and s are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure relates to methods of preparation of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and (Ib), and intermediates therefor.Type: GrantFiled: November 6, 2012Date of Patent: May 27, 2014Assignee: SanofiInventor: Zhongli Gao
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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: 20140141055Abstract: A process for the manufacture of semi-plastic pharmaceutical unit doses using a rotary moulding machine and semi-plastic pharmaceutical dosage units obtained by this process.Type: ApplicationFiled: November 18, 2013Publication date: May 22, 2014Inventors: Dominique Kluger, Carsten Schmidt, Albin Hauler, David Schroeckenfuchs, Niki Waldron
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Publication number: 20140135322Abstract: The present invention relates to novel chemical compounds formula (I) (C)n—B-(A)m-B—(C)n (I) wherein m is 0 or 1, and n is independently 0, 1, 2 or 3, A, each B and each C are independently selected from phenylene and five- and six-membered heteroaromatic rings, and for a terminal ring B or C also from bicyclic heteroaromatic fused rings having seven to ten ring members, wherein the bond between at least two of the rings A to C may be replaced by a carbonyl group (—CO—), wherein at least two of the rings A to C are substituted with one or two groups R, and wherein each ring A to C further optionally is substituted with one or two groups R1. The compounds are useful in therapy, especially therapy of a mammal suffering from a disease involving misfolded or aggregated forms of proteins.Type: ApplicationFiled: July 13, 2012Publication date: May 15, 2014Inventors: Peter Asberg, Kristin Hammer, Johan Olsson, Martin Henriksson