Nitrogen Attached Indirectly To The Diazole Ring By Acyclic Nonionic Bonding Patents (Class 548/375.1)
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Publication number: 20110294830Abstract: The present invention provides a nitrogen-containing compound represented by formula (I1) (in formula (I1), R0 represents a nitro group or the like, Z represents an optionally substituted aryl group or the like, R3 represents a hydrogen atom or the like, Y represents a nitro group or the like, n represents an integer of 0 to 3, D represents an optionally substituted 5-membered to 8-membered hydrocarbon ring group or heterocyclic group having or not having a substituent other than substituent X, X represents a group represented by formula (II-1) (in formula (II-1), R1 and R2 respectively and independently represent a hydrogen atom or the like), A represents a carbon atom or the like, n1 represents an integer of 0 to 2) or a salt thereof, and an insecticide, miticide, sanitary insect pest control agent, or harmful organism control agent including as an active ingredient thereof the nitrogen-containing compound or the salt thereof.Type: ApplicationFiled: February 5, 2010Publication date: December 1, 2011Applicant: Nippon Soda Co., Ltd.Inventors: Jyun Iwata, Masahiro Kawaguchi, Akiko Mizui
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Patent number: 8063055Abstract: The present invention comprises a new class of compounds capable of modulating the c-kit receptor and, accordingly, useful for treatment of c-kit mediated diseases, including various inflammatory, fibrotic and/or mast cell mediated diseases such as mastocytosis. The compounds have a general Formula I wherein A0-3 and R1-6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of c-kit mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.Type: GrantFiled: February 23, 2010Date of Patent: November 22, 2011Assignee: Amgen Inc.Inventors: Essa Hu, Jason Brooks Human, Roxanne Kunz, Andrew Tasker, Ryan White
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Patent number: 8063036Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: April 7, 2010Date of Patent: November 22, 2011Assignee: Millennium Pharmaceuticals, Inc.Inventors: Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song, Robert M. Scarborough
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Publication number: 20110275797Abstract: An N-acyl anthranilic acid derivative represented by general formula (1) or a salt thereof is useful for prevention or treatment of diseases associated with excessive production of collagen. (In the formula, R1 represents a carboxyl group or the like; R2 represents a hydrogen atom or the like; R3 represents an optionally substituted aryl group or the like; X1 represents a carbonyl group; X2 represents a bonding hand; X3 represents a bonding hand; X4 represents a bonding hand or the like; and A represents an optionally substituted phenyl group or the like.Type: ApplicationFiled: January 29, 2010Publication date: November 10, 2011Applicant: Toyama Chemical Co., Ltd.Inventors: Junichi Yokotani, Arihiro Takatori, Yukie Tada, Minori Yanai, Hiroshi Kato, Yoichi Taniguchi, Chiharu Tanabe
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Patent number: 8053439Abstract: Disclosed herein are novel benzophenone derivatives represented by formula I, a pharmaceutically acceptable salt thereof, a hydrate thereof or a solvate thereof, a pharmacological composition containing the same, and a use of the composition as therapeutic drugs. The benzophenone derivatives have an inhibition activity of microtubule formation and can be used to treat a normal proliferative state of a malignant tumor by killing the actively proliferating cells.Type: GrantFiled: September 21, 2007Date of Patent: November 8, 2011Assignee: Chong Kun Dang Pharmaceutical Corp.Inventors: Nam-Song Choi, Young-Mi Kim, Young-Hoon Kim, Jae-Kwang Lee, In-Taek Lim, Ho-Jin Choi, Hyun-Mo Yang, Seung-Kee Moon, Soo-Jin Kim, Hyun-Jung Yu, Jae-Su Shin, Young-Min Kwon, Sung-Sook Lee, Soon-Kil Ahn, Sun-Ju Kong
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Publication number: 20110251206Abstract: The present invention relates to compounds of formula (I) wherein X, R1, R2, R3, R4 and R5 are as defined herein, which are useful for treating diseases which respond to CXCR2 receptor mediators. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: ApplicationFiled: June 21, 2011Publication date: October 13, 2011Inventors: Urs Baettig, Anne-Marie D'Souza, Peter Hunt, Neil John Press, Simon James Watson
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Publication number: 20110251196Abstract: The present disclosure is generally directed to compounds which can modulate G-protein coupled receptor 88, compositions comprising such compounds, and methods for modulating G-protein coupled receptor 88.Type: ApplicationFiled: October 5, 2010Publication date: October 13, 2011Inventors: Carolyn Diane Dzierba, Richard A. Hartz, Yingzhi Bi, Vijay T. Ahuja, Joanne J. Bronson, Kenneth Carson, Giovanni Cianchetta, Michael Green, David Kimball, S. Roy Kimura, Soojin Kwon, John E. Macor, Yulian Zhang, Greg Zipp
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Patent number: 8026195Abstract: The present invention relates to N-cycloalkyl-thiocarboxamide or N-cycloalkyl-N-substituted carboximidamide derivatives of formula (I) wherein A and B represent a 5-membered heterocyclyl groups, T represents an oxygen, sulphur or amino derivatives, Z1 represents a cycloalkyl group and Z2 and Z3 represent various substituents, their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: GrantFiled: July 30, 2007Date of Patent: September 27, 2011Assignee: Bayer Cropscience AGInventors: Ralf Dunkel, Stéphanie Gary, Marie-Claire Grosjean-Cournoyer, Philippe Rinolfi, Arounarith Tuch
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Publication number: 20110230350Abstract: Use of substituted sulfonamides of the formula (I) or salts thereof for enhancing stress tolerance in plants to abiotic stress, especially for enhancing plant growth and/or for increasing plant yield.Type: ApplicationFiled: March 17, 2011Publication date: September 22, 2011Applicant: BAYER CROPSCIENCE AGInventors: Jens Frackenpohl, Ines Heinemann, Thomas Müller, Pascal Von Koskull-Döring, Jan Dittgen, Dirk Schmutzler, Christopher Hugh Rosinger, Isolde Häuser-Hahn, Martin Jeffrey Hills
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Publication number: 20110223093Abstract: This invention relates to sulfur functionalized ionic liquid compounds that are useful in methods of carbon dioxide or sulfur dioxide removal to which they may be applied.Type: ApplicationFiled: March 11, 2011Publication date: September 15, 2011Applicant: E.I. DU PONT DE NEMOURS AND COMAPNYInventor: MARK A. SCIALDONE
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Patent number: 8017558Abstract: Novel carboxamides of the formula (I) The present application is further directed toward a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and also novel intermediates and their preparation.Type: GrantFiled: December 5, 2006Date of Patent: September 13, 2011Assignee: Bayer Cropscience AGInventors: Ralf Dunkel, Hans-Ludwig Elbe, Jörg Nico Greul, Herbert Gayer, Bernd-Wieland Krüger, Arnd Voerste, Ulrike Wachendorff-Neumann, Peter Dahmen
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Patent number: 8003654Abstract: The invention relates to novel sulfonamide compounds of the formula (I) and their use as orexin receptor antagonists.Type: GrantFiled: April 10, 2007Date of Patent: August 23, 2011Assignee: Actelion Pharmaceuticals Ltd.Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen, Cornelia Zumbrunn Acklin
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Patent number: 7989497Abstract: The present invention relates to compounds of formula (I) wherein X, R1, R2, R3, R4 and R5 are as defined herein, which are useful for treating diseases which respond to CXCR2 receptor mediators. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: GrantFiled: July 30, 2009Date of Patent: August 2, 2011Assignee: Novartis AGInventors: Urs Baettig, Anne-Marie D'Souza, Peter Hunt, Neil John Press, Simon James Watson
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Publication number: 20110178133Abstract: The present invention relates generally to novel calcimimetic compounds and pharmaceutical compositions comprising them. The invention also relates to methods of treating of diseases or disorders related to the function of the calcium sensing receptor using the compounds represented in Formula I.Type: ApplicationFiled: October 15, 2008Publication date: July 21, 2011Inventors: Thomas S. Coulter, Christopher H. Fotsch, Chiara Ghiron, Paul E. Harrington, Michael G. Kelly, Philip Miller, Gilbert M. Rishton, David J. St.Jean, JR., David J. Semin
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Patent number: 7977352Abstract: Novel triazolopyridine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, ECM degradation, joint degradation and/or inflammation, and others.Type: GrantFiled: November 30, 2007Date of Patent: July 12, 2011Assignee: Galapagos NVInventors: Paul John Edwards, Wolfgang Schmidt, Veronique Birault, Friedrich Erich Karl Kroll, Andrew Burritt, Xueliang Tao, Martin James Inglis Andrews, Sébastien Laurent Xavier Martina
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Publication number: 20110160165Abstract: The present invention provides compounds of Formula (I) and related methods and formulations: wherein: A represents a pyrazole ring optionally substituted by one or more R groups.Type: ApplicationFiled: March 1, 2011Publication date: June 30, 2011Applicant: Paratek Pharmaceuticals, Inc.Inventors: Sophie Huss, Jose M. Bueno, Jose M. Fiandor, Roger Frechette
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Patent number: 7968729Abstract: Methods useful for preparing compounds of formula I: and salts thereof are disclosed. Also disclosed are intermediates useful in the preparation of such compounds.Type: GrantFiled: March 26, 2010Date of Patent: June 28, 2011Assignee: Lexicon Pharmaceuticals, Inc.Inventors: Mark S. Bednarz, Hugh Alfred Burgoon, Jr., Shinya Iimura, Ramanaiah C. Kanamarlapudi, Qiuling Song, Wenxue Wu, Jie Yan, Haiming Zhang
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Publication number: 20110150873Abstract: The invention relates to the use of Broad-Spectrum Chemokine Inhibitors (BSCIs), and in particular members of the acylaminolactam class of pharmaceutical agents, for the prevention, prophylaxis, treatment or amelioration of symptoms of inflammatory diseases. In particular, improved compositions consisting of BSCI agents combined with one or more additional active pharmaceutical agents in order to achieve improved anti-inflammatory efficacy with a reduced side-effect profile are described and claimed.Type: ApplicationFiled: December 10, 2008Publication date: June 23, 2011Applicant: CAMBRIDGE ENTERPRISE LIMITEDInventor: David John Grainger
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Patent number: 7964732Abstract: This invention provides a compound of the formula These compounds are useful for the treatment of disease conditions caused by overactivation of the VR1 receptor such as pain, or the like in mammal. This invention also provides a pharmaceutical composition comprising the above compound.Type: GrantFiled: November 9, 2007Date of Patent: June 21, 2011Assignee: Pfizer Inc.Inventors: Koji Ando, Andrew Anthony Calabrese, Matthew Alexander James Duncton, Kentaro Futatsugi, Misato Hirano, Satochi Nagayama
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Publication number: 20110144080Abstract: The invention provides compounds of the formula: (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between R1 and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom a with respect to the NR2R3 group and provided that the oxo group when present is located at a carbon atom a with respect to the NR2R3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R1 is an aryl or heteroaryl group; and R2, R3, R4 and R5 are as defined in the claims.Type: ApplicationFiled: December 23, 2004Publication date: June 16, 2011Applicants: ASTEX THERAPEUTICS LIMITED, THE INSTITUTE OF CANCER RESEARCH ROYAL CANCER HOSPITALInventors: Valerio Berdini, Gordon Saxty, Marinus Leendert Verdonk, Steven John Woodhead, Paul Graham Wyatt, Robert George Boyle, Hanna Fiona Sore, David Winter Walker, Ian Collins, Robert Downham, Robin Arthur Ellis Carr
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Publication number: 20110143942Abstract: The present invention relates to novel pyrazolyl-substituted heterocycles of the formula (I) in which X, Y, Z and Het are as defined in the disclosure, to processes for their preparation, and to their use as pesticides, microbicides and herbicides.Type: ApplicationFiled: February 11, 2011Publication date: June 16, 2011Inventors: Reiner Fischer, Astrid Ullmann, Thomas Bretschneider, Axel Trautwein, Ralf Wischnat, Christoph Erdelen, Angelika Lubos-Erdelen, Dieter Feucht, Mark Wilhelm Drewes
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Publication number: 20110118303Abstract: The present invention relates to compounds derived from taurine with non-steroidal anti inflammatory activity. In a first embodiment, the present invention relates to compounds derived from taurine, in which taurine is bound directly by means of an amide bond or through an spacing group, to a compound selected from the group of non-steroidal anti inflammatory compounds, cited as derived from taurine presenting the Formula (I): in which R means the component with non-steroidal anti inflammatory activity. In a second embodiment, the invention provides a process for obtaining the compounds of Formula (I) by reaction of taurine with a compound belonging to the group of non-steroidal anti inflammatory (NSAIs), in order to obtain a compound derived from taurine by direct bond or through a spacing group of the taurine to the NSAI. The invention also relates to the pharmaceutical compositions comprising at least one compound derived from taurine presenting non-steroidal anti inflammatory activity.Type: ApplicationFiled: April 9, 2009Publication date: May 19, 2011Applicants: EMS S.A., Universidade Estadual Paulista Julio De Mesquita Filho - UNESPInventors: Ednir de Oliveira Vizioli, Chung Man Chin, Renato Farina Menegon, Lorena Blau, Jean Leandro Dos Santos, Maria do Carmo Longo
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Publication number: 20110105447Abstract: Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer.Type: ApplicationFiled: October 6, 2010Publication date: May 5, 2011Applicants: Incozen Therapeutics Pvt. Ltd., Rhizen Pharmaceuticals SAInventors: Meyyappan Muthuppalaniappan, Srikant Viswanadha, Gayatri S. Merikapudi, Swaroop Kumar V.S. Vakkalanka
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Patent number: 7932283Abstract: The present invention relates to N-cyclopropyl-sulfonylamide derivatives of formula (I) wherein the substituents are cyclic groups, their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions:Type: GrantFiled: April 5, 2007Date of Patent: April 26, 2011Assignee: Bayer Cropscience AGInventors: Hans-Georg Schwarz, Sandra Gassmann, Karl-Heinz Kuck, Peter Dahmen, Ulrike Wachendorff-Neumann, Stéphane Carbonne, Stéphanie Gary, Christopher Steele, Alain Villier, Jean-Pierre Vors
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Publication number: 20110081297Abstract: The present invention relates to novel amyloid binding compounds and methods for measuring effects of the compounds, by measuring changes of amyloid plaque level in living patients. More specifically, the present invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET) imaging to study amyloid deposits in brain in vivo to allow diagnosis of Alzheimer's disease. Thus, the present invention relates to use of the novel amyloid binding compounds as a diagnostic. The invention further relates to a method of measuring clinical efficacy of Alzheimer's disease therapeutic agents. Specifically, the present invention relates to novel aryl or heteroaryl substituted pyrazole derivatives, compositions, and therapeutic uses and processes for making such compounds.Type: ApplicationFiled: May 28, 2009Publication date: April 7, 2011Inventors: James C. Barrow, Scott Harrison, James Mulhearn, Cyrille Sur, David L. Williams, Scott Wolkenberg
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Publication number: 20110077409Abstract: Cyano-substituted sulfilimines are produced efficiently and in high yield from the corresponding sulfides by reaction with cyanamide and hypochlorite.Type: ApplicationFiled: November 18, 2010Publication date: March 31, 2011Inventors: David E. Podhorez, Ronald Ross, JR., James R. McConnell
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Patent number: 7915286Abstract: The present invention relates to phosphodiesterase (PDE) type IV selective inhibitors. Processes for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds and their use as PDE type IV selective inhibitors are provided. Prepared compounds correspond to structure XIV Formula (XIV).Type: GrantFiled: September 11, 2006Date of Patent: March 29, 2011Assignee: Ranbaxy Laboratories LimitedInventors: Venkata P. Palle, Sarala Balachandran, Nidhi Gupta, Vinayak Vasantrao Khairnar, Mandadapu Raghuramaiah, Abhijit Ray, Sunanda Ghose Dastidar
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Patent number: 7910747Abstract: Pyrazoloamides are provided which are phosphonate and phosphinate glucokinase activators that are useful in treating diabetes and related diseases and have the structure wherein is a pyrazoyl ring; R4 is —(CH2)n—Z—(CH2)m—PO(OR7)(OR8), —(CH2)nZ—(CH2)m—PO(OR7)R9, or —(CH2)nZ—(CH2)m—PO(R9)(R10); R5 and R6 are independently selected from H, alkyl and halogen; Y is R3(CH2)s, wherein R3 is aryl , s is 0, X is a bond; and n, Z, m, R4, R5, R6, and R7 are as defined herein; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: June 28, 2007Date of Patent: March 22, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Denis E. Ryono, Peter T. W. Cheng, Scott A. Bolton, Sean Chen, Yan Shi, Wei Meng, Joseph A. Tino
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Publication number: 20110065667Abstract: The present invention provides a prophylactic or therapeutic agent for dementia, Alzheimer's disease, attention-deficit hyperactivity disorder, schizophrenia, eating disorders, obesity, diabetes, hyperlipidemia, sleep disorders, narcolepsy, sleep apnea syndrome, circadian rhythm disorder, depression, allergic rhinitis or other diseases. A phenylpyrazole derivative represented by formula (1) or a pharmaceutically acceptable salt thereof: {wherein R1 and R2, which may be the same or different, each represent C1-C6 alkyl or C3-C8 cycloalkyl, or R1 and R2 are attached to each other together with their adjacent nitrogen atom to form a 4- to 7-membered saturated heterocyclic ring (wherein said saturated heterocyclic ring may be substituted with halogen or C1-C6 alkyl), n represents an integer of 0 to 2, T represents a hydrogen atom, halogen or C1-C6 alkyl, and R represents formula (I): or the like}.Type: ApplicationFiled: November 22, 2010Publication date: March 17, 2011Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Toshio NAKAMURA, Makoto Tatsuzuki, Dai Nozawa, Tomoko Tamita, Seiji Masuda, Hiroshi Ohta, Shuhei Kashiwa, Aya Fujino, Shigeyuki Chaki, Toshiharu Shimazaki
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Patent number: 7906556Abstract: The invention relates to novel compounds and methods of treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.Type: GrantFiled: October 12, 2006Date of Patent: March 15, 2011Assignee: Elan Pharmaceuticals, Inc.Inventors: R. Jeffrey Neitz, Eric Tisdale, Barbara Jagodzinska, Anh Truong, Jay Tung
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Publication number: 20110059964Abstract: The present invention relates to the orexin receptor antagonists compounds of the general formula (I) as well as to their isomers, salts and solvates, to the pharmaceutical compositions containing them and to the therapeutic application thereof.Type: ApplicationFiled: February 3, 2010Publication date: March 10, 2011Applicant: sanofi-aventisInventors: Michel Aletru, Peter Aranyi, Maria Balogh, Sandor Batori, Judit Bence, Philippe Bovy, Zoltan Kapui, Endre Mikus, Claudie Namane, Christophe Philippo, Tibor Szabo, Zsuzsanna Tomoskozi, Katalin Urban-Szabo
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Publication number: 20110046129Abstract: 2-Phenylethylamino substituted carboxamide derivatives and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies are presented.Type: ApplicationFiled: September 9, 2010Publication date: February 24, 2011Applicant: Newron Pharmaceuticals S.p.A.Inventors: Florian Thaler, Mauro Napoletano, Cibele Sabido-David, Ermanno Moriggi, Carla Caccia, Laura Faravelli, Alessandra Restivo, Patricia Salvati
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Publication number: 20110046137Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: The pyrazole derivatives of formula (I) or salts thereof modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor (P2X7 receptor antagonists). The invention also relates to the use of such compounds or salts, or pharmaceutical compositions thereof, in the treatment or prevention of disorders/diseases mediated by the P2X7 receptor, for example pain, inflammation or a neurodegenerative disease.Type: ApplicationFiled: May 8, 2008Publication date: February 24, 2011Inventors: Paul John Beswick, Laura Jane Chambers, Iain Patrick Chessell, David John Davies, Emmanuel Hubert Demont, Robert James Gleave, David George Hubert Livermore, Pamela Joan Theobald, Mythily Vimal, Daryl Simon Walter
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Patent number: 7888289Abstract: A compound of general formula (I): A process for preparing this compound. A fungicide composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.Type: GrantFiled: April 6, 2006Date of Patent: February 15, 2011Assignee: Bayer Cropscience AGInventors: Darren Mansfield, Pierre-Yves Coqueron, Philippe Desbordes, Heiko Rieck, Alain Villier, Pierre Genix, Marie-Claire Grosjean-Cournoyer
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Publication number: 20110034691Abstract: The present invention provides methods, i.e., scalable or large-scale processes for the production of fused, tricyclic sulfonamido analogs, such as substituted or unsubstituted 5-(aryl-sulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinolines and 5-(heteroaryl-sulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinolines. Exemplary methods of the invention include an intra-molecular cyclization step, in which a carbon-nitrogen bond is formed, and which employs a copper-based catalyst that contains at least one organic ligand, such as DMEDA. The invention further provides compounds, which are useful as intermediates in the methods of the invention.Type: ApplicationFiled: March 24, 2010Publication date: February 10, 2011Inventors: Michael S. Dappen, Jacek J. Jagodzinski, Lee H. Latimer, Jing Wu, Jollie Duaine Godfrey, JR., Robert Michael Matunas, Thomas W. Drabb, Gary Probst
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Patent number: 7879897Abstract: The invention relates to 5-sub-stituted-oxyalkylaminopyrazole derivatives of the formula or salts thereof wherein the various symbols are as defined in the description, to processes for their preparation, to compositions thereof, and to their use for the control of pests including arthropods and helminths.Type: GrantFiled: August 21, 2004Date of Patent: February 1, 2011Assignee: Merial LimitedInventors: David Teh-Wei Chou, Stefan Schnatterer, Werner Knauf, Karl Seeger
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Publication number: 20110021771Abstract: This invention relates to compounds and methods for the inhibition of HDAC enzymatic activity. More particularly, the invention provides for compounds of formula (I), (I) and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, and racemic and scalemic mixtures, diastereomers and enantiomers thereof, wherein L, M, n, R, W, X and Y are as defined in the specification.Type: ApplicationFiled: November 3, 2008Publication date: January 27, 2011Applicant: METHYLGENE INC.Inventors: Tammy Mallais, Oscar Moradei, Alain Ajamian, Pierre Tessier, David Smil, Sylvie Frechette, Roger Machaalani, Silvana Leit, Patrick Beaulieu, Robert Déziel, John Mancuso
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Patent number: 7875646Abstract: The present invention relates to compounds corresponding to the formula (I): In which R1, R2, R3, R4 and R5 are as described herein. The invention also relates to the method of preparation of said compounds and their application in therapeutics.Type: GrantFiled: September 21, 2007Date of Patent: January 25, 2011Assignee: Sanofi-AventisInventors: Francis Barth, Christian Congy, Serge Martinez, Philippe Pointeau, Murielle Rinaldi-Carmona
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Publication number: 20110015065Abstract: The present invention relates to the use of substituted sulfonic acid amide compounds of formula I wherein Ra, n, Het, A, Y and D are as defined in the claims and the N-oxides and the salts thereof for combating phytopathogenic harmful fungi, and to compositions and seeds comprising at least one such compound. The invention also relates to novel substituted sulfonic acid amide compounds and processes for preparing these compounds.Type: ApplicationFiled: February 10, 2009Publication date: January 20, 2011Applicant: BASF SEInventors: Jochen Dietz, Wassilios Grammenos, Bernd Mueller, Jan Klaas Lohmann, Jens Renner, Sarah Ulmschneider, Marianna Vrettou, Michael Puhl
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Publication number: 20110009638Abstract: Disclosed is a method for preparing a compound of Formula 1 wherein Q and Z are as defined in the disclosure comprising distilling water from a mixture comprising a compound of Formula 2, a compound of Formula 3, a base comprising at least one compound selected from the group consisting of alkaline earth metal hydroxides of Formula 4 wherein M is Ca, Sr or Ba, alkali metal carbonates of Formula 4a wherein M1 is Li, Na or K, 1,5-diazabicyclo[4.3.0]non-5-ene and 1,8-diazabicyclo[5.4.0]undec-7-ene, and an aprotic solvent capable of forming a low-boiling azeotrope with water.Type: ApplicationFiled: April 8, 2009Publication date: January 13, 2011Applicant: E.I. DU PONT DE NEMOURS AND COMPANYInventor: Gary David Annis
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Publication number: 20110003795Abstract: The invention relates to substituted aromatic carboxamide and urea derivatives, to processes for the preparation thereof, to pharmaceutical compositions containing these compounds and also to the use of these compounds for preparing pharmaceutical compositions.Type: ApplicationFiled: May 6, 2010Publication date: January 6, 2011Applicant: Gruenenthal GmbHInventors: Robert FRANK, Gregor BAHRENBERG, Thomas CHRISTOPH, Klaus SCHIENE, Jean DE VRY, Nils DAMANN, Sven FRORMANN, Bernhard LESCH, Jeewoo LEE, Yong-Soo KIM, Myeong-Seop KIM
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Publication number: 20100331302Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: July 8, 2010Publication date: December 30, 2010Applicant: Chemocentryx, Inc.Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M.K. Pennell, Edward J. Sullivan, William D. Thomas, Solomon Ungashe, Penglie Zhang, Jay Powers, Sreenivas Punna
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Publication number: 20100324046Abstract: The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: June 24, 2008Publication date: December 23, 2010Inventors: Paul Harrington, Richard W. Heidebrecht, JR., Solomon Kattar, Thomas A. Miller, Karin M. Otte, Phieng Siliphaivanh, Paul Tempest, Kevin J. Wilson, David J. Witter
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Patent number: 7846956Abstract: The present invention provides a malononitrile compound represented by the formula (I): wherein any one of X1, X2, X3 and X4 is CR100, wherein R100 is a group represented by the formula: the other three of X1, X2, X3 and X4 each represent nitrogen or CR5, provided that 1 to 3 of X1, X2, X3 and X4 represent nitrogen, and Z represents oxygen, sulfur or NR6, which has pest-controlling activity.Type: GrantFiled: January 13, 2005Date of Patent: December 7, 2010Assignee: Sumitomo Chemical Company, LimitedInventors: Hiromasa Mitsudera, Ken Otaka, Jun Fujiwara
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Publication number: 20100304966Abstract: Compounds of the formula I in which the substituents have the meaning given in the description, processes for preparing these compounds, compositions comprising them and their use for controlling harmful fungi.Type: ApplicationFiled: October 9, 2008Publication date: December 2, 2010Applicant: BASF SEInventors: Joachim Rheinheimer, Barbara Nave, Doris Kremzow, Stefan Redlich, Christian Pilger, Claudia Rosenbaum, Wassilios Grammenos
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Publication number: 20100292157Abstract: The invention relates generally to novel compositions and methods comprising a cyclohexanehexol and a secretase inhibitor. The compositions and methods provide beneficial effects, in particular sustained beneficial effects, in the treatment of diseases involving a disorder in protein folding and/or aggregation, and/or amyloid formation, deposition, accumulation, or persistence, such as Alzheimer's disease and related neurodegenerative disorders.Type: ApplicationFiled: November 22, 2007Publication date: November 18, 2010Inventor: Antonio Cruz
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Publication number: 20100291151Abstract: The present invention relates to new 1-methylpyrazole modulators of substance P release, calcitonin gene-related peptide activity, adrenergic receptor activity, and/or 5-HT receptor activity, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: April 21, 2010Publication date: November 18, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20100267769Abstract: This invention provides a compound of the formula These compounds are useful for the treatment of disease conditions caused by overactivation of the VR1 receptor such as pain, or the like in mammal. This invention also provides a pharmaceutical composition comprising the above compound.Type: ApplicationFiled: November 9, 2007Publication date: October 21, 2010Inventors: Koji Ando, Andrew Anthony Calabrese, Matthew Alexander James Duncton, Kentaro Futatsugi, Misato Hirano, Satochi Nagayama
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Publication number: 20100249424Abstract: Disclosed is a method for preparing a compound of Formula 1 wherein R1 is CHX2, CX3, CX2CHX2 or CX2CX3; each X is independently Cl or F; Z is optionally substituted phenyl; and Q is phenyl or 1-naphthalenyl, each optionally substituted as defined in the disclosure; comprising contacting a compound of Formula 2 with hydroxylamine in the presence of a base. The present invention also relates to novel compounds of Formula 2, useful as starting materials for the aforedescribed method.Type: ApplicationFiled: August 4, 2008Publication date: September 30, 2010Applicant: E.I.DuPont De Nemours and CompanyInventors: Gary David Annis, Brenton Todd Smith
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Patent number: 7799820Abstract: Disclosed is a compound represented by the formula (I) below, which has a glucokinase-activating effect and is thus useful for treatment of diabetes or obesity, or a pharmaceutically acceptable salt thereof. In the formula, R1 represents an aryl or the like; R11 represents an aryl or the like; R2 represents a formyl or the like, R3 represents a C1-6 alkyl or the like; R3 represents a hydrogen atom or the like; Z1 represents —O— or the like; Z2 represents —O— or the like; Y1-Y4 respectively represent a carbon atom or a nitrogen atom; ring A represents a heteroaryl group; X represents a carbon atom or the like; m represents an integer of 0-2; and q represents an integer of 0-2.Type: GrantFiled: September 29, 2006Date of Patent: September 21, 2010Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Keiji Takahashi, Yoshio Ogino, Teruyuki Nishimura