Asymmetrical (e.g., 1, 2, 4-triazines, Etc.) Patents (Class 544/182)
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Publication number: 20130150358Abstract: This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.Type: ApplicationFiled: February 4, 2013Publication date: June 13, 2013Applicant: HMI MEDICAL INNOVATIONS, LLC.Inventor: HMI MEDICAL INNOVATIONS, LLC.
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Patent number: 8461080Abstract: The invention relates to aqueous, aluminum silicate-free, highly concentrated suspension concentrates, containing the active substance metribuzin, one or more surfactants based on nonionic polymers from the ‘acrylic grafted polymers’ group, one or more thickeners based on anionic heteropolysaccharides from the xanthan gum group, one or more wetting agents and optionally other components such as antifoaming agents, antifreeze agents and preservatives and other surfactants differing from the aforesaid components.Type: GrantFiled: August 11, 2010Date of Patent: June 11, 2013Assignee: Bayer Cropscience AGInventors: Frank Sixl, Udo Bickers, Harry Koppert, Juergen Hopert
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Publication number: 20130137661Abstract: Disclosed are compounds useful as gonadotrophin-releasing hormone (“GnRH”) receptor antagonist.Type: ApplicationFiled: November 19, 2010Publication date: May 30, 2013Applicant: SK CHEMICALS CO. LTD.Inventors: Seon Mi Kim, Min Hee Lee, Jae Sun Kim, Hoe Chul Jung, So Young Lee, Soo Min Lee, Eun Jeong Kim, Eui Sun Park, Sung Hoon Park, Bong Yong Lee, Key An Um
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Publication number: 20130123262Abstract: The present invention provides novel compounds of formula I wherein W1, W2, W3, W4, W5, B, X1, X2, X3, X4, X5, E and L are as defined herein; invention compounds are gamma amino butyrique acid receptor-subtype B (“GABAB”) positive allosteric modulators (enhancers), which are useful to provide methods of treating or preventing diseases or disorders, including treatment of anxiety, depression, epilepsy, schizophrenia, cognitive disorders, spasticity and skeletal muscle rigidity, spinal cord injury, multiple sclerosis, amyotrophic lateral sclerosis, cerebral palsy, neuropathic pain and craving associated with cocaine and nicotine, panic disorder, posttraumatic stress disorders, urge urinary incontinence, gastroesophageal reflux disease, transient lower oesophageal sphincter relaxations, functional gastrointestinal disorders and irritable bowel syndrome.Type: ApplicationFiled: December 14, 2012Publication date: May 16, 2013Applicant: Addex Pharma S.A.Inventor: Addex Pharma S.A.
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Publication number: 20130116235Abstract: Heteroaryl pyridone and aza-pyridone compounds of Formula I are provided, where one or two of X1, X2, and X3 are N, and including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: November 2, 2012Publication date: May 9, 2013Applicant: GENENTECH, INC.Inventor: Genentech, Inc.
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Patent number: 8435990Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, R1, R2, R3, R4, R5, Ra and Rb are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.Type: GrantFiled: July 30, 2010Date of Patent: May 7, 2013Assignee: Roche Palo Alto LLCInventors: Christine E. Brotherton-Pleiss, Joan Marie Caroon, Francisco Javier Lopez-Tapia, Keith Adrian Murray Walker
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Publication number: 20130102468Abstract: Disclosed are compounds exhibiting sufficient herbicidal activity at low application dosage when they are applied to soils and foliage, and an agrochemical composition using the same, in particular herbicides. The compounds are triazine derivatives represented by following Formula 1 or salts thereof, and the herbicides containing them: [Chem. 28] wherein in the formula, R1 represents a hydrogen atom; a C1-C12 alkyl group; a C2-C6 alkenyl group, etc., R2 represents a C1-C12 alkyl group, etc., Y and Z represent an oxygen atom or a sulfur atom, and A represents a 5- or 6-membered cyclic group which may contain a nitrogen atom, an oxygen atom, or a sulfur atom.Type: ApplicationFiled: May 26, 2011Publication date: April 25, 2013Applicants: IHARA CHEMICAL INDUSTRY CO., LTD., KUMIAI CHEMICAL INDUSTRY CO., LTD.Inventors: Atsushi Shibayama, Ryu Kajiki, Masami Kobayashi, Takashi Mitsunari, Atsushi Nagamatsu
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Publication number: 20130096128Abstract: This invention describes novel pyrazole compounds of formula III: wherein Z1, Z2, and Z3 are as described in the specification; Q is —S—, —O—, —N(R4)—, or —CH(R6)—; R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; and R2 and R2? are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.Type: ApplicationFiled: September 28, 2012Publication date: April 18, 2013Inventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Francoise Pierard
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Patent number: 8415368Abstract: The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein R1 is a nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle, the nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle optionally has substituent(s), R2 is an optionally substituted C6-14 aryl group, an optionally substituted thienyl group or an optionally substituted pyridyl group, R3 and R4 are each a hydrogen atom, or one of R3 and R4 is a hydrogen atom and the other is an optionally substituted lower alkyl group, an acyl group, a halogen atom, a cyano group or a nitro group, and R5 is an alkyl group or a salt thereof.Type: GrantFiled: January 26, 2009Date of Patent: April 9, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Masahiro Kajino, Atsushi Hasuoka, Haruyuki Nishida
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Publication number: 20130085276Abstract: The use of a complex of the form Z—M—OR in the carboxylation of a substrate is described. The group Z is a two-electron donor ligand, M is a metal and OR is selected from the group consisting of OH, alkoxy and aryloxy. The substrate may be carboxylated at a C—H or N—H bond. The metal M may be copper, silver or gold. The two-electron donor ligand may be a phosphine, a carbene or a phosphite ligand. Also described are methods of manufacture of the complexes and methods for preparing isotopically labelled caboxylic acids and carboxylic acid derivatives.Type: ApplicationFiled: June 9, 2011Publication date: April 4, 2013Inventors: Steven P. Nolan, Catherine Cazin
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Patent number: 8410098Abstract: Disclosed are N-{1-[3-(2-ethoxy-5-(4-ethylpiperazinyl)sulfonylphenyl)-4,5-dihydro-5-oxo-1,2,4-triazin-6-yl]ethyl}butyramide (which is represented by formula III and utilized for preparing vardenafil), its preparation method, intermediates during preparation procedure, preparation method for such intermediates and a method for preparing vardenafil from the compound.Type: GrantFiled: December 28, 2007Date of Patent: April 2, 2013Assignee: Topharman Shanghai Co., Ltd.Inventors: Guanghui Tian, Zheng Liu, Jin Zheng, Jingshan Shen
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Publication number: 20130064770Abstract: The present invention relates to radiodiagnostic compounds, methods of making those compounds, and methods of use thereof as imaging agents for preferably a HA serotonin 5-HT1A receptor for use in PET or SPECT, preferably PET. Compositions comprising an imaging-effective amount of radiolabeled compounds are also disclosed. The present invention also relates to non-radiolabeled compounds, methods of making those compounds, and methods of use thereof to treat various neurological and/or psychiatric disorders.Type: ApplicationFiled: May 26, 2011Publication date: March 14, 2013Applicant: GE HEALTHCARE LIMITEDInventors: Ian Martin Newington, Duncan George Wynn, Robert James Domett Nairne, Benedicte Guilbert, Subrata Mandal, Jinto Jose, Sunderaraman Varadarajan, Chitralekha Rangaswamy, Helen Betts, Rebecca Davis
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Publication number: 20130053559Abstract: A 1,2,4-triazine of formula (I): and its process of manufacture and use.Type: ApplicationFiled: October 8, 2010Publication date: February 28, 2013Applicants: Michelin Recherche et Technique S.A., Societe De Technologie MichelinInventors: Nicolas Seeboth, Sergey Ivanov, Sergey Molkov
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Publication number: 20130040928Abstract: The present invention relates to compounds having general formula I characterised in that wherein in particular: R1 represents one or a plurality of groups such as: trifluoromethyl, halogen such as F, Cl, Br, methyl, nitro. R represents nitrogen T-U represents C?C, V represents N, W represents C?O, R2 represents Cl or H, R3=H and R4=Me, A represents wherein n=m=1, X represents —CH2— and E represents —CH—, and D represents oxygen, along with the various isomers and mixtures thereof in any proportions, and the pharmaceutically acceptable salts thereof.Type: ApplicationFiled: April 15, 2011Publication date: February 14, 2013Applicant: PIERRE FABRE MEDICAMENTInventors: Isabelle Leroy, Elisabeth Dupont-Passelaigue, Samuel Mialhe, Didier Junquero, Karine Valeille
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Publication number: 20130035304Abstract: This invention relates to compounds which selectively bind to the survival protein MCL-1 with high affinity and selectivity, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for modulating MCL-1 activity and for treating hyperproliferative disorders, angiogenesis disorders, cell cycle regulation disorders, autophagy regulation disorders, inflammatory disorders, and/or infectious disorders and/or for enhancing cellular engraftment and/or wound repair, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: January 31, 2011Publication date: February 7, 2013Inventors: Loren D. Walensky, Michelle L. Stewart, Nicole Cohen
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Publication number: 20130029963Abstract: According to the invention there is provided a compound of formula A1 which may be useful in the treatment of a condition or disorder ameliorated by the inhibition of the A1-A2b or, particularly, the A2a receptor wherein the compound of formula A1 has the structure, wherein, A represents Cy1 or HetA; Cy1 represents a 5- to 14-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one, two or three rings, which Cy1 group is optionally substituted by one or more R4a substituents; HetA represents a 5- to 14-membered heterocyclic group that may be aromatic, fully saturated or partially unsaturated, and which contains one or more heteroatoms selected from O, S and N, which heterocyclic group may comprise one, two or three rings and which HetA group is optionally substituted by one or more R4b substituents; B represents a Cy2 or HetB; Cy2 represents a 3- to 10-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one or two rings, whicType: ApplicationFiled: February 7, 2011Publication date: January 31, 2013Applicant: HEPTARES THERAPEUTICS LIMITEDInventors: Miles Stuart Congreve, Stephen Philippe Andrews, Jonathan Stephen Mason, Christine Mary Richardson, Giles Albert Brown
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METHODS AND SYSTEM FOR INTERFERING WITH VIABILITY OF BACTERIA AND RELATED COMPOUNDS AND COMPOSITIONS
Publication number: 20130022578Abstract: Provided herein are methods and systems for interfering with viability of bacteria and related compounds and compositions.Type: ApplicationFiled: April 25, 2012Publication date: January 24, 2013Inventors: Dianne K. NEWMAN, Ryan C. HUNTER -
Publication number: 20130018046Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: ApplicationFiled: September 13, 2012Publication date: January 17, 2013Applicant: ARIAD Pharmaceuticals, Inc.Inventors: Yihan Wang, Xiaotian Zhu, Rajeswari Sundaramoorthi, Wei-Sheng Huang, Dong Zou, R. Mathew Thomas, Jiwei Qi, Jan Antoinette C. Romero, David C. Dalgarno, William C. Shakespeare, Tomi K. Sawyer, Chester A. Metcalf, III
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Publication number: 20130005732Abstract: Compounds of formula (I): especially where R1 is an optionally substituted alkyl, aralkyl or heterocyclyl-alkyl group, are shown to have activity as sodium channel blockers or as antifolates. Some novel compounds where R1 is an aralkyl or heterocyclyl-alkyl are disclosed.Type: ApplicationFiled: September 13, 2012Publication date: January 3, 2013Applicant: University of GreenwichInventors: Michael LEACH, Laurence HARBIGE, Dieter RIDDALL, Paul BARRACLOUGH
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Publication number: 20130005967Abstract: Provided are a method for preparing (R)-3-(3-fluoro-4-(1-methyl-5,6-dihydro-1,2,4-triazin-4(1H)-yl)phenyl)-5-(substituted methyl)oxazolidin-2-one derivatives, which are oxazolidinone antibiotic compounds having a cyclic amidrazone group, represented by Chemical Formula 1, and intermediates thereof, and uses 3,4-difluoro-4-nitrobenzen as a starting material. According to the preparation method of the present invention, (R)-3-(3-fluoro-4-(1-methyl-5,6-dihydro-1,2,4-triazin-4(1H)-yl)phenyl)-5-(substituted methyl)oxazolidin-2-one derivatives, which are useful as oxazolidinone antibiotics, can be prepared in high purity and high yield in a simpler manner than conventional methods.Type: ApplicationFiled: March 8, 2011Publication date: January 3, 2013Applicant: LEGOCHEM BIOSCIENCES, INC.Inventors: Young Lag Cho, Sung Yoon Baek, Sang Eun Chae, Hong Bum Lee, Tae Kyo Park, Sung Ho Woo, Yong Zu Kim
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Patent number: 8344138Abstract: The present invention provides novel compounds of formula I wherein W1, W2, W3, W4, W5, B, X1, X2, X3, X4, X5, E and L are as defined herein; invention compounds are gamma amino butyrique acid receptor-subtype B (“GABAB”) positive allosteric modulators (enhancers), which are useful to provide methods of treating or preventing diseases or disorders, including treatment of anxiety, depression, epilepsy, schizophrenia, cognitive disorders, spasticity and skeletal muscle rigidity, spinal cord injury, multiple sclerosis, amyotrophic lateral sclerosis, cerebral palsy, neuropathic pain and craving associated with cocaine and nicotine, panic disorder, posttraumatic stress disorders, urge urinary incontinence, gastroesophageal reflux disease, transient lower oesophageal sphincter relaxations, functional gastrointestinal disorders and irritable bowel syndrome.Type: GrantFiled: November 9, 2007Date of Patent: January 1, 2013Assignee: Addex Pharma S.A.Inventors: Eric Riguet, Brice Campo, Antoine Gibelin, Karim Mhalla
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Publication number: 20120289403Abstract: The invention relates to alkylsulfide derivatives compounds of formula I as hereunder depicted or the enantiomers or veterinarily acceptable salts thereof which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to methods for controlling invertebrate pests by using these compounds and to plant propagation material and to agricultural and veterinary compositions comprising said compounds. wherein U, R1, R2, R3U, X, n and p are defined as in the description.Type: ApplicationFiled: November 11, 2010Publication date: November 15, 2012Inventors: Sebastian Soergel, Ralph Paulini, Steffen Gross, Carsten Beyer, Matthias Pohlman, Henricus Maria Martinus Bastiaans, Michael Rack, Deborah L. Culbertson, Douglas D. Anspaugh, Sarah Thompson, Vincent Salgado
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Patent number: 8309740Abstract: The present invention relates to a method for one-pot synthesis of ionic liquid with fluoroalkyl group, more particularly to a method for one-pot synthesis of ionic liquid with fluoroalkyl group represented by the following Chemical Formula 1 by adding and reacting a nitrogen-containing compound, a Brønsted acid of the formula YH and a fluoroolefin compound of the formula CFR1?CR2R3 in a single reactor: wherein represents a nitrogen-containing compound; Y? represents an anion of the Brønsted acid; and R1, R2 and R3, which may be same or different, represent hydrogen, fluorine, C1-C10 alkyl or C1-C10 fluoroalkyl having from 1 to 23 fluorine atoms.Type: GrantFiled: August 15, 2008Date of Patent: November 13, 2012Assignee: Korea Institute of Science and TechnologyInventors: Hyun Joo Lee, Dong Jin Suh, Byoung Sung Ahn, Hong Gon Kim, Chang Soo Kim, Hoon Sik Kim
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Patent number: 8293898Abstract: There is described novel organo-platinum luminophores comprising a complex of formula I: The luminophores have application as the emissive component in organic light emitting diodes.Type: GrantFiled: December 16, 2011Date of Patent: October 23, 2012Assignee: University of YorkInventors: Duncan W. Bruce, Valery Kozhevnikov
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Patent number: 8258130Abstract: This invention is directed to a compound of formula (I): wherein R1, R2, R3, R4 and L1 are as defined herein, a pharmaceutical composition comprising the compound, and the use of the compound to treat allergic and/or inflammatory disorders, particularly disorders such as allergic rhinitis, asthma and/or chronic obstructive pulmonary disease (COPD).Type: GrantFiled: September 30, 2009Date of Patent: September 4, 2012Assignee: SanofiInventors: Suzanne C Aldous, Michael W Fennie, John Z Jiang, Stanly John, Lan Mu, Brian Pedgrift, James R Pribish, Barbara S Rauckman, Jeffrey S Sabol, Grzegorz T Stoklosa, Sukanthini Thurairatnam, Christopher Loren Vandeusen
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Publication number: 20120208791Abstract: The invention relates to new bicyclic heterocyclic derivative compounds, to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.Type: ApplicationFiled: June 12, 2009Publication date: August 16, 2012Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Valerio Berdini, Maria Grazia Carr, Miles Stuart Congreve, Martyn Frederickson, Charlotte Mary Griffiths-Jones, Christopher Charles Frederick Hamlett, Andrew Madin, Christopher William Murray, Rajdeep Kaur Benning, Gordon Saxty, Emma Vickerstaffe, Brian John Williams, Marian Williams, Andrew James Woodhead, Steven John Woodhead, Eddy Jean Edgard Freyne, Tom Cornelis Hortense Govaerts, Patrick René Angibaud
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Patent number: 8242113Abstract: Disclosed is a novel oxazolidinone derivative, particularly a novel oxazolidinone compound with a cyclic amidoxime or cyclic amidrazone group. Also disclosed is a pharmaceutical antibiotic composition including a novel oxazolidinone derivative, in vivo hydrolysable ester thereof, in vivo hydrolysable phosphate ester thereof, an isomer thereof or a pharmaceutically acceptable salt thereof as an effective ingredient. Because the novel oxazolidinone derivative, in vivo hydrolysable ester thereof, in vivo hydrolysable phosphate ester thereof, an isomer thereof or a pharmaceutically acceptable salt thereof exhibits a wide antibacterial spectrum against resistant bacteria, a low toxicity, and a strong antibacterial activity against Gram-positive and Gram-negative bacteria, it can be usefully used as an antibiotic.Type: GrantFiled: September 22, 2009Date of Patent: August 14, 2012Assignee: Legochem Biosciences, Inc.Inventors: Young Lag Cho, Sang Eun Chae, Sung Yoon Baek, Yeon Ok Kim, Seong Jin Kim, Hyang Sook Lee, Ju Hyun Park, Tae Kyo Park, Sung Ho Woo, Yong Zu Kim
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Publication number: 20120202763Abstract: Compounds that selectively inhibit pathological production of human vascular endothelial growth factor (VEGF) and compositions comprising such Compounds are described. Compounds that inhibit viral replication or the production of viral RNA or DNA or viral protein and compositions comprising such Compounds are described. Also described are methods of reducing VEGF using such Compounds and methods for treating cancer and non-neoplastic conditions involving the administration of such Compounds. Further described are methods of inhibiting viral replication or the production of viral RNA or DNA or viral protein using such Compounds and methods for treating viral infections involving the administration of such Compounds. The Compounds may be administered as a single agent therapy or in combination with one or more additional therapies to a human in need of such treatments.Type: ApplicationFiled: May 27, 2010Publication date: August 9, 2012Applicant: PTC THERAPEUTICS, INCInventors: Neil Almstead, Tamil Arasu, Soongyu Choi, Liangxian Cao, Jeffrey Allen Campbelll, Donald Corson, Thomas W. Davis, Jason D. Graci, Zhengxian Gu, Peter Seong Woo Hwang, William Lennox, Harry H. Miao, Langdon Miller, Young-Choon Moon, Hongyan Qi, Christopher Trotta, Marla L. Weetall
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Patent number: 8232275Abstract: Compounds which are active against viruses have the following formulas: wherein B is a purine or pyrimidine heterocyclic ring or base. In a preferred embodiment, the purine include 6-aminopurine (adenine), 6-hydroxypurine (hypoxanthine), 2-amino-6-hydroxypurine (guanine), 2,6-diamino-purine, 2-amino-6-azidopurine, 2-amino-6-halo substituted purines such as 2-amino-6-chloropurine, 2-amino-6-fluoropurine, 2-amino-6-alkoxypurines such as 2-amino-6-methoxypurine, 2-amino-6-cyclopropylaminopurine, 2-amino-6-alkylamino or 2-amino-6-dialkylamino substituted purines, 2-amino-6-thiopurine, 2-amino-6-alkylthio substituted purines, 3-deazapurines, 7-deazapurines and 8-azapurines. The pyrimidine incorporates cytosine, uracil and thymine, 5-halo substituted cytosines and uracils, 5-alkyl substituted cytosines and uracils including derivatives with a saturated or unsaturated alkyl group and 6-azapyrimidines.Type: GrantFiled: July 15, 2011Date of Patent: July 31, 2012Assignees: Wayne State University, The Regents of the University of MichiganInventors: Jiri Zemlicka, Shaoman Zhou, John C. Drach
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Patent number: 8217168Abstract: The present invention relates to novel compounds of formula (I) or a salt thereof: wherein G is selected from a group consisting of: phenyl, a 5- or 6-membered monocyclic heteroaryl group, or a 8- to 11-membered heteroaryl bicyclic group; p is an integer ranging from 0 to 5; R1 is halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; or corresponds to a group R6; and when p is an integer ranging from 2 to 5, each R1 may be the same or different; R2 is hydrogen or C1-4alkyl; n is 3, 4, 5 or 6; R6 is a moiety selected from the group consisting of: isoxazolyl, —CH2—N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl, 2-pyrrolidinonyl, and such R6 group is optionally substituted by one or two substituents selected from: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; R4 is selected in the group consisting of: hydrogen, halogen, hydroxy, cyano, C1-4alkyl, C3-7 cycloalkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanType: GrantFiled: October 1, 2008Date of Patent: July 10, 2012Assignee: Glaxo Group LimitedInventors: Barbara Bertani, Susanna Cremonesi, Stefano Fontana, Alessandra Pasquarello
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Patent number: 8217063Abstract: The present application relates to novel lactam-substituted dicarboxylic acid derivatives, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.Type: GrantFiled: March 15, 2008Date of Patent: July 10, 2012Assignee: Bayer Intellectual Property GmbHInventors: Michael Hahn, Eva-Maria Becker, Andreas Knorr, Dirk Schneider, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Frank Wunder, Dieter Lang
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Publication number: 20120157681Abstract: There is described novel organo-platinum luminophores comprising a complex of formula I: The luminophores have application as the emissive component in organic light emitting diodes.Type: ApplicationFiled: December 16, 2011Publication date: June 21, 2012Applicant: UNIVERSITY OF YORKInventors: Duncan W. Bruce, Valery Kozhevnikov
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Publication number: 20120142919Abstract: The invention relates, in general, to an improved process for preparing lamotrigine, Formule (I). Processes for preparing and purifying lamotrigine, including lamotrigine hydrate, lamotrigine monohydrate and anhydrous lamotrigine, are described.Type: ApplicationFiled: August 2, 2005Publication date: June 7, 2012Applicant: MEDICHEM, S.A.Inventor: Carmen Arnalot Aguilar
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Publication number: 20120135993Abstract: The present invention relates to triazine compounds having sodium channel blocking properties, and to use of the compounds for preparation of medicaments for treatment of associated disorders. The triazine compounds are of formula (I) wherein: R1 is hydrogen or a substituent group; R2 is amino or a substituent group; N* is amino when R1 is hydrogen or ?NH when R1 is a substituent group; R3 and R4 are both carbocyclic, heterocyclic or alkyl groups and may be same or different; and R5 is hydrogen, alkyl or a cyclic aryl group, with the proviso that: when R3 and R4 are both alkyl they are linked to form a cycloalkyl group, and R5 is a cyclic aromatic group; and when R3 and R4 are both carbocyclic or heterocyclic groups, R5 is hydrogen or an alkyl group; or a salt thereof.Type: ApplicationFiled: July 8, 2010Publication date: May 31, 2012Applicant: University of GreenwichInventors: Michael Leach, Karl Franzmann, Dieter Riddall, Laurence Harbige
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Publication number: 20120136149Abstract: Disclosed are: a method for preparing a 5-chloro-N-({(5S)-2-oxo-3-[4-(5,6-dihydro-4H-[1,2,4]triazin-1-yl)phenyl]-1,3-oxazolidin-5-yl}-methyl)thiophene-2-carboxamide derivative, which is a inhibitor of blood coagulation factor Xa, in a high purity and yield; and a novel intermedicate used therein.Type: ApplicationFiled: July 7, 2010Publication date: May 31, 2012Applicants: LEGOCHEM BIOSCIENCE LTD., GREEN CROSS CORPORATIONInventors: Young Lag Cho, Sang Eun Chae, Seong Jin Kim, Ho Young Song, Tae Kyo Park, Sung Ho Woo, Yong Zu Kim, Jinhwa Lee, Suk Ho Lee
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Publication number: 20120135992Abstract: The present invention relates to triazine compounds having sodium channel blocking properties, and to use of the compounds for preparation of medicaments for treatment of associated disorders. The compounds are of formula (I): in which z is a single bond or an optionally substituted linking group, R1 is a halo-alkyl group; and A is an optionally substituted aromatic heterocyclic or carbocyclic ring system; or a salt thereof.Type: ApplicationFiled: July 8, 2010Publication date: May 31, 2012Applicant: University of GreenwichInventors: Michael Leach, Karl Franzmann, Dieter Riddall, Laurence Harbige
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Patent number: 8188269Abstract: The present invention relates to improved covalent coupling of two or more entities such as biomolecules, polymer compositions, organic/inorganic molecules/materials, and the like, including their combinations, through one or more novel reactive groups attached to linker groups of 2-1000 atoms length. The present invention also contemplates the use of bifunctional bridge molecules to link two or more entities, wherein the functional groups of the bridge molecules are the novel reactive groups of the present invention.Type: GrantFiled: May 12, 2008Date of Patent: May 29, 2012Assignee: Luminex CorporationInventors: Ananda G. Lugade, Kurt D. Hoffacker, Adam J. Jenkins, Karri L. Michael-Ballard, Leonid Patsenker, Ewald Terpetschnig, Veronica D. Thomason, Ralph McDade
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Publication number: 20120129846Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.Type: ApplicationFiled: November 5, 2009Publication date: May 24, 2012Inventors: Zhaoning Zhu, William J. Greenlee, Mihir Baran Mandal, Duane A. Burnett, Chad E. Bennett, Troy McCracken
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Publication number: 20120129812Abstract: Provided is a heterocyclic derivative showing a thyroid hormone ? receptor agonist action, which is effective for the prophylaxis or treatment of the diseases relating to the action. A compound represented by the formula [I]: wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, and a medicament containing the compound as an active ingredient.Type: ApplicationFiled: April 19, 2010Publication date: May 24, 2012Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Shinji Kawata, Koji Matsumoto, Maki Nijima, Taichi Takahashi
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Publication number: 20120122871Abstract: The invention relates to (among other things) oligomer-containing substituted aromatic triazine compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits one or more advantages over corresponding compounds lacking the oligomer.Type: ApplicationFiled: May 13, 2010Publication date: May 17, 2012Applicant: Nektar TherapeuticsInventors: Jennifer Riggs-Sauthier, Bo-Liang Deng
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Patent number: 8178525Abstract: Disclosed are novel oxazolidinone derivatives with cyclic amidoxime or cyclic amidrazone group, pharmaceutically acceptable salts thereof, methods for preparing the same and pharmaceutical compositions containing the same. The oxazolidinone derivatives with cyclic amidoxime or cyclic amidrazone group or the pharmaceutically acceptable salts thereof can be effectively used for the treatment of thromboembolism and tumor as an anticoagulant based on the inhibition of factor Xa.Type: GrantFiled: June 5, 2009Date of Patent: May 15, 2012Assignee: Legochem Bioscience Ltd.Inventors: Ho Young Song, Young Lag Cho, Dae Yon Lee, Hee Sock Park, Sung Yoon Baek, Sang Eun Chae, Sang Hui Jo, Yeon Ok Kim, Hyang Sook Lee, Ju Hyun Park, Tae Kyo Park, Sung Ho Woo, Yong Zu Kim
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Publication number: 20120108812Abstract: Processes including preparation of trans-4-[(3-amino-5-oxo-4,5-dihydro-[1,2,4]triazin-6-ylmethyl)-carbamoyl]-cyclohexanecarboxylic acid methyl ester, and its conversion to trans-4-(4-amino-5-substituted-imidazo[5,1-f][1,2,4]triazin-7-yl)-cyclohexanecarboxylic acid compounds.Type: ApplicationFiled: July 8, 2010Publication date: May 3, 2012Inventors: Hanqing Dong, Yunyu Mao, Kristen Michelle Mulvhill, Josef A. Rechka, Douglas S. Werner
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Patent number: 8168786Abstract: The present invention relates to Radiolabeled Compounds and methods of use thereof for treating or preventing a psychiatric disorder in a subject, for stabilizing the mood of a subject having a mood disorder, or as imaging agents for a serotonin receptor. Compositions comprising an imaging-effective amount of a Radiolabeled Compound are also disclosed.Type: GrantFiled: June 28, 2007Date of Patent: May 1, 2012Assignee: The Trustees of Columbia University in the City of New YorkInventors: Joseph John Mann, J. S. Dileep Kumar
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Publication number: 20120094999Abstract: The present invention relates to novel pyrimidine, pyrrolo-pyrimidine, pyrrolo-pyridine, pyridine, purine and triazine compounds which are able to modulate epidermal growth factor receptor (EGFR), including Her-kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.Type: ApplicationFiled: May 5, 2010Publication date: April 19, 2012Applicant: Dana-Farber Cancer Institute, Inc.Inventors: Nathanael S. Gray, Pasi Janne, Michael J. Eck, Wenjun Zhou
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Publication number: 20120077806Abstract: Disclosed herein are methods of inhibiting a deubiquitinase (DUB), methods of treating pathogenic infections (e.g., viral, bacterial, and/or parasitic), methods of inhibiting cell proliferation, methods of treating a neurodegenerative disease, methods of treating one or more symptoms of a neurodegenerative disease or a genetic disorder, and compounds.Type: ApplicationFiled: September 23, 2011Publication date: March 29, 2012Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Nicholas J. Donato, Christiane Wobus, Hollis D. Showalter, Moshe Talpaz, Jeffrey W. Perry, Roderick J. Sorenson, Mary X. O'Riordan, Yafei Jin
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Publication number: 20120071513Abstract: The present invention provides novel compounds and pharmaceutical compositions thereof, as well as methods for using the compounds and pharmaceutical compositions for treating tumors. Examples of specific tumor types that the compounds may be used to treat include, but are not limited to sarcomas, melanomas, neuroblastomas, carcinomas (including but not limited to lung, renal cell, ovarian, liver, bladder, and pancreatic carcinomas), and mesotheliomas.Type: ApplicationFiled: November 28, 2011Publication date: March 22, 2012Applicant: COMPASS PHARMACEUTICALS LLCInventors: David Kanne, John Ward, Gary Look, X. Michael Wang, Diva Chan, Tina Lee, Donald R. James, Richard Gless, John Schullek, Charles Vacin
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Publication number: 20120028983Abstract: Disclosed is a compound which has both an angiotensin-II receptor antagonistic activity and a PPAR? activation activity and is useful as a prophylactic and/or therapeutic agent for hypertension, heart diseases, angina pectoris, cerebrovascular disorders, cerebral circulatory disorders, ischemic peripheral circulatory disorders, renal diseases, arteriosclerosis, inflammatory diseases, type-2 diabetes, diabetic complications, insulin resistance syndrome, syndrome X, metabolic syndrome and hyperinsulinemia. [In the formula, A represents a 5- to 10-membered heteroaryl group; R1 and R2 independently represent a C1-6 alkyl group; and each of R3 to R5 is absent or represents H, a halogen atom, OH, NO2, a halo-C1-6 alkyl group, a (substituted) C1-6 alkoxy group, a (substituted) C3-6 cycloalkyloxy group, or a 5- to 10-membered heteroaryl group.Type: ApplicationFiled: April 16, 2010Publication date: February 2, 2012Applicant: KOWA COMPANY, LTD.Inventors: Toru Miura, Kazuhiro Onogi, Seiichi Sato, Junya Tagashira, Gen Watanabe, Ryohei Sekimoto, Rie Ishida, Hitomi Aoki, Tadaaki Ohgiya
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Patent number: 8106193Abstract: There is described novel organo-platinum luminophores comprising a complex of formula (I). The luminophores have application as the emissive component in organic light emitting diodes.Type: GrantFiled: September 29, 2008Date of Patent: January 31, 2012Assignee: University of YorkInventors: Duncan W. Bruce, Valery Kozhevnikov
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Patent number: 8106048Abstract: The present invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, (I) wherein R1 is independently hydrogen, alkyl, cycloalkyl, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, arylalkyl or substituted arylalkyl; R2 is independently —NR3R4, (II) or (III) R3 is independently alkyl, cycloalkyl, alkoxy, alkylamine, —OH, —SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl, R4 is independently alkyl, cycloalkyl, alkoxy, alkylamine, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R5 is independently H, COR6, CO2R6, SOR6, SO2R6, SO3R6, alkyl, cycloalkyl, alkoxy, —NH2, alkylamine, —NR7COR6, halogen, —OH, —SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R6 is independently H, alkyl, cycloalkyl, —NH2, alkylamine, aryl or heteroaryl; R7 is independently H, alkyl, cycloalkyl, alkoxy, —OH, —SH, alkylthio, hydroxyalkyl, aryl, or heteroaryl;Type: GrantFiled: July 29, 2005Date of Patent: January 31, 2012Assignee: 4SC AGInventors: Johann Leban, Harald Schmitt, Kristina Wolf, Stefano Pegoraro, Andreas Wuzík
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Patent number: RE43748Abstract: Nitrogen-containing heterocyclic carboxamide derivatives represented by the following general formula: wherein ring A is a substituted or unsubstituted pyrazine, pyrimidine, pyridazine or triazine ring; R1 is O or OH; R2 is a hydrogen atom, an acyl group or a substituted or unsubstituted carbamoylalkyl or carboxyalkyl group; and the broken line represents a single bond or a double bond; or salts thereof are useful for preventing and treating virus infections and especially influenza virus infections.Type: GrantFiled: August 26, 2010Date of Patent: October 16, 2012Assignee: Toyama Chemical Co., Ltd.Inventors: Yousuke Furuta, Hiroyuki Egawa, Nobuhiko Nomura