Nitrogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/297)
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Publication number: 20140088159Abstract: Covalent conjugates of an ?,?-disubstituted glycine ester and a modulator of the activity of a target intracellular enzyme or receptor, wherein the ester group of the conjugate is hydrolysable by one or more intracellular carboxylesterase enzymes to the corresponding acid and the ?,?-disubstituted glycine ester is conjugated to the modulator at a position remote from the binding interface between the inhibitor and the target enzyme or receptor pass into cells and the active acid hydrolysis product accumulates within the cells.Type: ApplicationFiled: November 27, 2013Publication date: March 27, 2014Applicant: Chroma Therapeutics Ltd.Inventors: Alan Hastings Drummond, Alan Hornsby Davidson, David Festus Charles Moffat, Alastair David Graham Donald, Stephen John Davies
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Patent number: 8669209Abstract: Soluble granule formulations of amine salts of pyridine containing carboxylic acids with improved handling properties are provided by an improved process in which the pyridine containing carboxylic acid is partially neutralized with an amine.Type: GrantFiled: November 22, 2010Date of Patent: March 11, 2014Assignee: Dow AgroSciences, LLC.Inventors: Franklin N. Keeney, Neil A. Foster, Martin C. Logan, Maria G. Perry
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Publication number: 20140038963Abstract: The present disclosure provides methods for identifying therapeutic agents that are multifunctional radical quenchers. It also provides compounds of formula (I), (II), or (II-A): and pharmaceutically acceptable salts thereof, compositions comprising these compounds, and methods of using these compounds in a variety of applications, such as treatment or suppression of diseases associated with decreased mitochondrial function resulting in diminished ATP production and/or oxidative stress and/or lipid peroxidation.Type: ApplicationFiled: April 4, 2012Publication date: February 6, 2014Inventors: Sidney Hecht, Omar Khdour, Sandipan Roy Chowdhury, Poulami Talukder
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Publication number: 20140031395Abstract: The present invention relates to compounds useful in the positive modulation of the alpha 7 nicotinic acetylcholine receptor (?7nAChR). The invention also relates to the use of these compounds in the treatment or prevention of a broad range of diseases in which the positive modulation of ?7nAChR is advantageous, including neurodegenerative and neuropsychiatric diseases and also inflammatory diseases.Type: ApplicationFiled: February 2, 2012Publication date: January 30, 2014Applicant: Bionomics LimitedInventors: Andrew Harvey, Audrey Fluck, Bruno Giethlen, Dharam Paul, Laurent Schaeffer
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Publication number: 20140012007Abstract: Disclosed herein is a process for preparing a compound of Formula (I), comprising the steps of: (a) reacting an aniline compound of Formula (II) and an carboxylic acid compound of Formula (III) or an activated carboxylic acid compound thereof, to provide a compound of Formula (IV); and (b) converting said protected amine group attached to said compound of Formula (IV) to an amine group to provide said compound of Formula (I); wherein PAm is a protected amine group. Processes to prepare the compounds of Formulae (II), (III), and (IV) are also disclosed.Type: ApplicationFiled: September 13, 2013Publication date: January 9, 2014Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Robert C. Livingston, William P. Gallagher, Robert M. Borzilleri, Zhen-Wei Cai
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Publication number: 20140004044Abstract: The present disclosure provides novel compounds, including compounds that bind to potassium channels, methods for their manufacture, and methods for their use, including for the treatment of demyelinating diseases and/or in vivo imaging of the central nervous system to diagnose and/or assess the progression of MS or other diseases.Type: ApplicationFiled: May 17, 2013Publication date: January 2, 2014Applicant: The University of ChicagoInventors: Pedro Brugarolas, Brian Popko, Daniel Appelbaum
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Publication number: 20140005178Abstract: The present disclosure relates to new azabiphenylaminobenzoic acid derivatives of formula (I); as well as processes for their preparation, pharmaceutical compositions comprising them, and their use in therapy as inhibitors of the dehydroorotate dihydrogenase (DHODH).Type: ApplicationFiled: August 12, 2013Publication date: January 2, 2014Applicant: Almirall, S.A.Inventors: Julio Cesar CASTRO PALOMINO LARIA, Emma Terricabras Belart, Montserrat Erra Sola, Eloisa Navarro Romero, Siliva Fonquerna Pou, Aranzazu Cardus Figueras, Maria Estrella Lozoya Toribio
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Publication number: 20130345193Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: August 23, 2013Publication date: December 26, 2013Applicant: CALCIMEDICA, INC.Inventors: Jeffrey P. WHITTEN, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Publication number: 20130345240Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: August 16, 2013Publication date: December 26, 2013Applicant: CALCIMEDICA, INC.Inventors: Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Publication number: 20130338105Abstract: Compounds of the formula I in which the substituents are as defined in claim 1 are suitable for use as microbiocides.Type: ApplicationFiled: August 20, 2013Publication date: December 19, 2013Inventors: Paul Anthony Worthington, Daniel Stierli, Fredrik Cederbaum, Kurt Nebel, Antoine Daina
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Publication number: 20130327251Abstract: Novel tridentate-, bidentate-, and monodentate-based aromatic adsorbates including self-assembled monolayers (SAMs), especially, mixed multi-component SAMs, where the adsorbates comprise an aromatic ring including one head group or a plurality of dentate head groups and one tunable tail group or a plurality of tail groups and methods for making the same, and methods for using same, their use in the preparation of homogeneously mixed multi-component self-assembled monolayers (SAMs). The adsorbants and SAMs derived therefrom are ideally suited for biosensing, biosensing diagnostics, biological interfacial mimics, surface protections for nanoparticles, inert coatings for artificial implants, and corrosion-resistant coatings for microelectronics components.Type: ApplicationFiled: March 7, 2013Publication date: December 12, 2013Applicant: THE UNIVERSITY OF HOUSTON SYSTEMInventors: T. Randall Lee, Supachai Rittikulsittichai, Thomas Frank, Burapol Singhana
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Publication number: 20130267546Abstract: The present disclosure provides biologically active compounds of formula (I): and pharmaceutically acceptable salts thereof: compositions comprising these compounds, and methods of using these compounds in a variety of applications, such as treatment or suppression of diseases associated with decreased mitochondrial function resulting in diminished ATP production and/or oxidative stress and/or lipid peroxidation.Type: ApplicationFiled: April 2, 2013Publication date: October 10, 2013Applicant: Arizona Board of Regents, a body corporate of the State of Arizona acting for and on behalf of AriInventors: Sidney HECHT, Omar KHDOUR, Jun LU, Pablo ARCE
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Publication number: 20130267565Abstract: The present invention provides a novel compound having an excellent antitumor effect, stability and metabolic stability. The compound of the present invention is represented by the following general formula (1) wherein R1 represents a halogen atom, an aryl group, an aryloxy group or a lower alkyl group optionally substituted with one or more halogen atoms; R2 represents hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group; and; m represents an integer of 1 to 3; provided that when m represents 2 or 3, R1s are the same or different.Type: ApplicationFiled: October 3, 2011Publication date: October 10, 2013Inventors: Takashi Nakagawa, Makoto Sakamoto, Kazuya Yamaguchi, Yuki Terauchi, Masamichi Shirakura, Yasuo Harada, Yutaka Kojima, Takumi Sumida
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Patent number: 8552200Abstract: Substituted 6-amino-nicotinamides, pharmaceutical compositions containing these compounds and also use of these compounds in the treatment and/or prophylaxis of pain and further diseases and/or disorders.Type: GrantFiled: October 19, 2011Date of Patent: October 8, 2013Assignee: Gruenenthal GmbHInventors: Sven Kühnert, Gregor Bahrenberg, Achim Kless, Wolfgang Schröder, Simon Lucas
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Patent number: 8546403Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: GrantFiled: April 12, 2011Date of Patent: October 1, 2013Assignee: Calcimedica, Inc.Inventors: Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Publication number: 20130252922Abstract: The present invention relates to substituted phenoxypyridine compounds of general formula (I) in which R1, R2 and R3 are as defined in the claims, to methods of preparing said compounds, to intermediates for the preparation of 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: October 27, 2011Publication date: September 26, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventor: Marion Hitchcock
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Publication number: 20130245063Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: April 26, 2013Publication date: September 19, 2013Applicant: CalciMedica, Inc.Inventors: Jeffrey P. Whitten, Jonathan Grey, Jianguo Cao, Zhijun Wang, Evan Rogers
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Patent number: 8530460Abstract: Azetidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.Type: GrantFiled: December 14, 2012Date of Patent: September 10, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Martin Fleck, Bernd Nosse, Niklas Heine, Gerald Juergen Roth
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Publication number: 20130178633Abstract: The use of compounds in the treatment of skin disorders is described. In particular, use of a compound of formula (I): or one of its pharmaceutically acceptable salts, solvates or hydrates in the preparation of a medicament to treat skin pathologies is described.Type: ApplicationFiled: December 22, 2010Publication date: July 11, 2013Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Cédric Poinsard, Pascale Mauvais, Jean-Michel Linget, Sandrine Rethore, Patrice Lucien Maurice Collette, Isabelle Marie Joëlle Martine Collette
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Publication number: 20130172564Abstract: The use of compounds in the treatment of skin disorders is described. In particular, use of a compound of formula (I): or one of its pharmaceutically acceptable salts, solvates or hydrates in the preparation of a medicament to treat skin pathologies is described.Type: ApplicationFiled: December 22, 2010Publication date: July 4, 2013Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Cédric Poinsard, Jean-Michel Rethore, Patrice Lucien Maurice Collette, Isabelle Marie Joëlle Collette
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Patent number: 8455654Abstract: A nanoscale pigment particle composition includes an organic benzimidazolone pigment, and a sterically bulky stabilizer compound, wherein the benzimidazolone pigment associates non-covalently with the sterically bulky stabilizer compound that is a substituted pyridine derivative; and the presence of the associated stabilizer limits the extent of particle growth and aggregation, to afford nanoscale pigment particles.Type: GrantFiled: July 18, 2011Date of Patent: June 4, 2013Assignees: Xerox Corporation, National Research Council of CanadaInventors: Rina Carlini, Darren Andrew Makeiff
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Patent number: 8455649Abstract: N-Azinyl-N?-aryl ureas and thioureas derivatives are effective at controlling insects.Type: GrantFiled: July 22, 2011Date of Patent: June 4, 2013Assignee: Dow AgroSciences, LLCInventors: Noormohamed M. Niyaz, Ricky Hunter, Timothy C. Johnson, Tony K. Trullinger, Annette V. Brown, Kristy Bryan
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Patent number: 8415350Abstract: The present invention relates to compounds of the general formula as dual modulators of the 5-HT2a and D3 receptors useful against CNS disorders, wherein A, R1, R2, n, p, q and r are as defined in the specification.Type: GrantFiled: September 15, 2011Date of Patent: April 9, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Luca Gobbi, Georg Jaeschke, Thomas Luebbers, Olivier Roche, Rosa Maria Rodriguez-Sarmiento, Lucinda Steward
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Publication number: 20130072449Abstract: Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.Type: ApplicationFiled: August 14, 2012Publication date: March 21, 2013Applicant: InterMune, Inc.Inventors: Brad O. Buckman, John B. Nicholas, Kumaraswamy Emayan, Scott D. Seiwert
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Publication number: 20130045869Abstract: Complexes of herbicidal carboxylic acids and amine-containing polymers or oligomers are provided. These herbicidal complexes are useful for controlling unwanted plant growth. The herbicidal complexes have low solubility in water, low volatility relative to commercial compositions of the corresponding herbicidal carboxylic acids, and offer similar or improved herbicidal performance when compared to existing salts of the herbicidal carboxylic acids.Type: ApplicationFiled: August 15, 2012Publication date: February 21, 2013Applicant: Dow AgroSciences LLCInventors: Lei Liu, Hong Zhang, Alex Kennedy, Holger Tank, David G. Ouse, James M. Gifford, Min Zhao
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Publication number: 20130040997Abstract: Provided are a novel pyridine carboxylic acid based compound used as a P2X1 and P2X3 receptor antagonist, a production method for the same and a composition comprising the same. The compound according to the present invention is a powerful antagonist of P2X1 and P2X3 receptors, and hence can be used as a drug for treating or preventing diseases involving neurological pain or chronic inflammatory diseases which are diseases caused by P2X1 and P2X3 receptor activity.Type: ApplicationFiled: December 20, 2010Publication date: February 14, 2013Applicant: GWANGJU INSTITUTE OF SCIENCE AND TECHNOLOGYInventors: Yong-Chul Kim, Kwan-Young Jung, Joong Heui Cho
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Patent number: 8372981Abstract: Compounds represented by the following general formula: wherein Ag is an optionally substituted 5- to 14-membered heterocyclic group, etc.; Xg is —O—, —S—, etc.; Yg is an optionally substituted C6-14 aryl group, an optionally substituted 5- to 14-membered heterocyclic group, etc.; and Tg1 is a group represented by the following general formula: (wherein Eg is a single bond or —N(Rg2)—), Rg1 and Rg2 each independently represent a hydrogen atom, an optionally substituted C1-6 alkyl group, etc. and Zg represents a C1-8 alkyl group, a C3-8 alicyclic hydrocarbon group, a C6-14 aryl group, etc.), salts thereof or hydrates of the foregoing.Type: GrantFiled: January 7, 2011Date of Patent: February 12, 2013Assignee: Eisai R&D Management Co., Ltd.Inventors: Yasuhiro Funahashi, Masayuki Matsukura, Tatsuo Watanabe, Hiroshi Obaishi, Junji Matsui
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Publication number: 20130035351Abstract: The present invention relates to non-charged oxime compounds which are acetyl cholinesterase (AChE) reactivators of inhibited AChE and which protect against organophosphate poisoning both peripherally and in the central nervous system. Also disclosed are pharmaceutical compositions and methods for preparing the reactivator compounds and associated intermediates.Type: ApplicationFiled: August 3, 2011Publication date: February 7, 2013Applicant: SOUTHWEST RESEARCH INSTITUTEInventors: Stanton F. MCHARDY, Richard M. CORBETT, Donald M. MAXWELL, Michael W. TIDWELL, Bismarck CAMPOS, Christopher J. BEMBEN
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Patent number: 8362043Abstract: The present invention provides a compound of formula I: wherein R1, R2, R3, R4, and R5 are as defined herein. The present invention also provides pharmaceutical compositions and methods using such compositions for treating a caspase-mediated diseases and processes for preparing the compounds of the invention.Type: GrantFiled: November 21, 2005Date of Patent: January 29, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Ronald Knegtel, Michael Mortimore, John R. Studley
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Publication number: 20130022629Abstract: Disclosed are an assay to identify modulators of the PD-1:PD-L pathway and PD-1:PD-L pathway modulators, e.g., compounds and pharmaceutical compositions thereof. Methods for treating diseases influenced by modulation of the PD-1:PD-L pathway such as, for example, autoimmune diseases, inflammatory disorders, allergies, transplant rejection, cancer, immune deficiency, and other immune system-related disorders, are also disclosed.Type: ApplicationFiled: January 3, 2011Publication date: January 24, 2013Inventors: Arlene H. Sharpe, Manish J. Butte, Shinji Oyama
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Publication number: 20130018054Abstract: The present invention provides organic compounds of the following structure; A-L1-B—C-D-L2-E that are useful for treating or preventing conditions or disorders associated with DGAT1 activity in animals, particularly humans.Type: ApplicationFiled: September 13, 2012Publication date: January 17, 2013Applicant: NOVARTIS AGInventors: Michael H. SERRANO-WU, Young-shin KWAK, Wenming Liu
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Publication number: 20130005574Abstract: 3-alkoxy, thioalkyl and amino-4-amino-6-(substituted)picolinic acids having a halogen, alkyl or mono-, di- tri- and tetra-substituted aryl substituents in the 6-position, and their acid derivatives, are herbicides demonstrating a broad spectrum of weed control.Type: ApplicationFiled: June 29, 2012Publication date: January 3, 2013Inventors: Jeffrey B. Epp, Christian T. Lowe, James M. Renga, Paul R. Schmitzer, Joseph D. Eckelbarger, Katherine A. Guenthenspberger, Thomas L. Siddall, Carla N. Yerkes, Lindsey G. Fischer, Natalie C. Giampietro, Jeremy Kister, Joshua Roth
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Publication number: 20120322834Abstract: The disclosed compounds are useful in the treatment of mammalian cancers and especially human cancers. Compounds, pharmaceutical compositions, and methods of Formula I are disclosed: or a pharmaceutically acceptable salt, hydrate, solvate, enantiomer, stereoisomer, or tautomer thereof.Type: ApplicationFiled: July 26, 2012Publication date: December 20, 2012Applicant: DECIPHERA PHARMACEUTICALS, LLCInventors: Daniel L. Flynn, Michael D. Kaufman
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Patent number: 8334307Abstract: Provided herein are hydroxypyridone derivatives, for example, a compound of Formula I, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a proliferative disease.Type: GrantFiled: October 7, 2011Date of Patent: December 18, 2012Assignee: Biotheryx Inc.Inventors: Frank Mercurio, Kyle W. H. Chan
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Publication number: 20120316147Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: ApplicationFiled: June 1, 2012Publication date: December 13, 2012Inventors: Caterina Bissantz, Uwe Grether, Paul Hebeisen, Atsushi Kimbara, Qingping Liu, Matthias Nettekoven, Marco Prunotto, Stephan Roever, Mark Rogers-Evans, Tanja Schulz-Gasch, Christoph Ullmer, Zhiwei Wang, Wulun Yang
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Publication number: 20120302551Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, and R6 are as described in the specification. The compounds are inhibitors of PLK and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: August 9, 2012Publication date: November 29, 2012Applicant: Millennium Pharmaceuticals, Inc.Inventors: Indu T. Bharathan, Matthew Duffey, Amy Elder, Jianping Guo, Gang Li, Dominic Reynolds, Francois Soucy, Tricia J. Vos
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Publication number: 20120263706Abstract: Enantiomerically pure compound of formula 1 are provided, as well as methods for their synthesis and use. Preferred compounds are potent inhibitors of the c-Met protein kinase, and are useful in the treatment of abnormal cell growth disorders, such as cancers.Type: ApplicationFiled: June 29, 2012Publication date: October 18, 2012Inventors: Jingrong Jean Cui, Lee Andrew Funk, Lei Jia, Pei-Pei Kung, Jerry Jialun Meng, Mitchell David Nambu, Mason Alan Pairish, Hong Shen, Michelle Tran-Dube
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Publication number: 20120259094Abstract: The present invention relates generally to affinity ligands and chemical affinity ligand-matrix conjugates for use as chromatographic adsorbents and methods which utilise the adsorbents in the purification of proteins by affinity chromatography. The affinity ligand-matrix conjugates of the present invention comprise ligands of general formula (I): wherein m represents an integer from 0-2, n represents an integer from 0-6, p represents an integer from 0-4, R1 represents H or C1-3 alkyl, R2 is an optional substituent, and X is the position at which the ligand is immobilized, optionally via a linker.Type: ApplicationFiled: October 15, 2010Publication date: October 11, 2012Inventors: Milton TW Hearn, Anjali Makarand Bhagwat, William Roy Jackson, Simon John Mountford
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Publication number: 20120252849Abstract: The disclosed compounds are useful in the treatment of mammalian cancers and especially human cancers. Compounds, pharmaceutical compositions, and methods of Formula I are disclosed: or a pharmaceutically acceptable salt, hydrate, solvate, enantiomer, stereoisomer, or tautomer thereof.Type: ApplicationFiled: May 24, 2012Publication date: October 4, 2012Applicant: DECIPHERA PHAMACEUTICALS, LLCInventors: Daniel L. Flynn, Michael D. Kaufman
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Publication number: 20120214808Abstract: A method of treating a condition associated with the CB-1 receptor, in particular obesity, by administering an effective amount of an aryl urea CB-1 receptor modulating compound to a subject in need of such treatment.Type: ApplicationFiled: February 17, 2012Publication date: August 23, 2012Applicant: Prosidion LimitedInventors: Jason Bloxham, Matthew Colin Thor Fyfe, James Horswill, Revathy Perpetua Jeevaratnam, John Keily, Martin James Procter, Karen Lesley Schofield, Salam Shaaban, Simon Andrew Swain, Philippe Wong-Kai-In
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Patent number: 8247573Abstract: The invention relates to substituted N-(2-mercaptopyridin-3-yl)amides, methods for the preparation thereof, medicaments containing these compounds and the use of these compounds for the preparation of medicaments.Type: GrantFiled: March 10, 2010Date of Patent: August 21, 2012Assignee: Gruenenthal GmbHInventors: Sven Kühnert, Beatrix Merla, Achim Kless, Gregor Bahrenberg, Wolfgang Schröder
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Patent number: 8236826Abstract: An object of the present invention is to provide a medicinal drug much improved in anti tumor activity and excellent in safety. According to the present invention, there is provided a medicinal drug containing a compound represented by the following general formula (1) or a salt thereof as an active ingredient: [Formula 1] wherein X1 represents a nitrogen atom or a group —CH?, R1 represents a group —Z—R6, in which Z represents a group —CO—, a group —CH(OH)— or the like, R6 represents a 5- to 15-membered monocyclic, dicyclic or tricyclic saturated or unsaturated heterocyclic group having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms, R2 represents a hydrogen atom or a halogen atom, Y represents a group —O—, a group —CO—, a group —CH(OH)— or a lower alkylene group, and A represents [Formula 2] wherein R3 represents a hydrogen atom, a lower alkoxy group or the like, p represents 1 or 2, R4 represents an imidazolyl lower alkyl group or the like.Type: GrantFiled: December 4, 2006Date of Patent: August 7, 2012Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hironori Matsuyama, Kenji Ohnishi, Takashi Nakagawa, Hideki Takasu, Makoto Sakamoto, Kumi Higuchi, Keisuke Miyajima, Satoshi Yamada, Masaaki Motoyama, Yutaka Kojima, Koichi Yasumura, Takeshi Kodama, Shun Otsuji, Keizo Kan, Takumi Sumida
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Publication number: 20120190684Abstract: N-Azinyl-N?-aryl ureas and thioureas derivatives are effective at controlling insects.Type: ApplicationFiled: July 22, 2011Publication date: July 26, 2012Applicant: DOW AGROSCIENCES LLCInventors: Noormohamed M. Niyaz, Ricky Hunter, Timothy C. Johnson, Tony K. Trullinger, Annette V. Brown, Kristy Bryan
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Patent number: 8211920Abstract: Disclosed are compounds of the Formula V and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8 and R9, and W are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, and inflammatory conditions in mammals. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases and inflammatory conditions in mammals and pharmaceutical compositions containing such compounds.Type: GrantFiled: August 5, 2008Date of Patent: July 3, 2012Assignee: Array BioPharma Inc.Inventors: Allison L. Marlow, Eli M. Wallace, Jeongbeob Seo, Joseph P. Lyssikatos, Hong Woon Yang, James Blake
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Patent number: 8211921Abstract: Disclosed are compounds of the Formula and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9, W, and X are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.Type: GrantFiled: January 20, 2009Date of Patent: July 3, 2012Assignee: Array BioPharma Inc.Inventors: James F. Blake, Joseph P. Lyssikatos, Allison L. Marlow, Jeongbeob Seo, Eli M. Wallace, Hong-Woon Yang
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Publication number: 20120136002Abstract: A compound of formula (I) wherein R1 to R15, P1, P2, A, B and Q are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as matriptase inhibitors and are useful in the treatment of matriptase dependent conditions, particularly cancer.Type: ApplicationFiled: May 18, 2010Publication date: May 31, 2012Inventors: Rajeev Goswami, Anil Kumar Vuppala, Ramesh Veludandi, Ramesh Sistla, Chakshusmathi Ghadiyaram, Muralidhara Ramachandra
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Patent number: 8188277Abstract: The present invention provides a novel compound, which has an excellent effect of suppressing the generation of collagen and less side effects, with being excellent in terms of safety. The compound of the present invention is represented by the following general formula (1): [wherein X1 represents a nitrogen atom or a group —CH?; R1 represents a group —Z—R6, wherein Z represents a group —CO—, a group —CH(OH)—, or the like, and R6 represents a 5- to 15-membered monocyclic, dicyclic, or tricyclic, saturated or unsaturated heterocyclic group having 1 to 4 nitrogen atoms, oxygen atoms, or sulfur atoms; R2 represents a hydrogen atom, a halogen atom or a lower alkylene group; Y represents a group —O—, a group —CO—, a group —CH(OH)—, a lower alkylene group, or the like; and A represents a group or the like, wherein R3 represents a hydrogen atom, a lower alkoxy group, or the like, p represents 1 or 2, and R4 represents an imidazolyl lower alkyl group or the like.Type: GrantFiled: August 3, 2005Date of Patent: May 29, 2012Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Tae Fukushima, Shuji Matsumura, Noriaki Takemura, Hideaki Satou, Nobuaki Ito, Takuya Shitsuta, Hironori Tsutsui, Michinori Tanaka, Keizo Kan, Hitoshi Nagao, Kenji Watanabe, Kuninori Tai, Takashi Nakagawa, Hideki Takasu, Makoto Sakamoto, Keisuke Miyajima, Satoshi Yamada, Yutaka Kojima, Koichi Yasumura, Naoto Ohi, Mitsuhiro Okuno, Kazuhisa Sugiyama, Kunihiko Kiyono, Takashi Suzuki, Seiji Akamatsu, Takeshi Kodama, Yasuo Yanagihara, Takumi Sumida
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Patent number: 8183266Abstract: The invention relates to the novel chemical compounds of the formula (I): (I) in free or salt form, its use in the treatment of NET and/or SERT mediated conditions, e.g., depression, vasomotor symptoms, e.g., hot flashes and other diseases or conditions mediated by NET and/or SERT.Type: GrantFiled: June 4, 2008Date of Patent: May 22, 2012Assignee: Intra-Cellular Therapies, Inc.Inventors: Lawrence P. Wennogle, Peng Li, Jun Zhao
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Publication number: 20120122819Abstract: The present invention includes novel compounds and pharmaceutically acceptable formulations of said compounds which exhibit antibiotic activity against microorganisms bearing a guanine riboswitch that controls the expression of the guaA gene, including organisms which are resistant to certain antibiotic families, and which are useful as antibacterial agents for treatment or prophylaxis of bacterial infections in animals or in humans, in particular but not limited to infections of the mammary gland, or their use as antiseptics, agents for sterilization or disinfection.Type: ApplicationFiled: June 14, 2010Publication date: May 17, 2012Applicant: SOCPRA - SCIENCES ET GENIE S.E.C.Inventors: Jérôme Mulhbacher, Daniel Lafontaine, François Malouin, Marianne Allard, Eric Marsault
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Patent number: 8173684Abstract: A compound represented by the formula (I): wherein R1 is lower alkyl, cycloalkyl or aromatic hydrocarbon ring, each of which is optionally substituted with one or more substituents; R2 is hydrogen atom, halogen atom, lower alkyl, halo(lower)alkyl or lower alkoxy; and R3 is (1) a group represented by the formula: wherein R4 is lower alkyl, etc.; (2) a group represented by the formula: wherein R5 is lower alkyl, etc.; (3) a group represented by the formula: wherein R6 is lower alkyl, etc.; or (4) a group selected from halogen atom, carboxy, hydroxy and lower alkoxy, or a salt thereof.Type: GrantFiled: May 2, 2008Date of Patent: May 8, 2012Assignees: Astellas Pharma Inc., Wakunaga Pharmaceutical Co., Ltd.Inventors: Chiyoshi Kasahara, Hitoshi Yamazaki