Polycyclo Ring System Having The 1,3-thiazole Ring As One Of The Cyclos Patents (Class 546/270.1)
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Publication number: 20100305067Abstract: Compound of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; AIk is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical which may contain an ether (—O—), thioether (—S—) or amino (—NR)— link, wherein R is hydrogen, —CN or C1-C3 alkyl; X is —C(?O)NR6—, or —C(?O)O— wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl or C2-C6 alkynyl; Z1 is —N? or —CH?Z2 is —N? or —C(R1)?; R1 is hydrogen, methyl, ethyl, ethenyl, ethynyl, methoxy, mercapto, mercaptomethyl, halo, fully or partially fluorinated (C1-C2)alkyl, (C1-C2Jalkoxy or (C1-C2)alkylthio, nitro, or nitrile (—CN); R2 is a group Q1-[Alk1]q-Q2-, wherein q is 0 or 1; AIk1 is an optionally substituted, divalent, straight chain or branched C1-C6 alkylene, or C2-C6 alkenylene or C2-C6 alkynylene radical which may contain or terminate in an ether (—O—), thioether (—S—) or amino (—NR)— link; Q2 is an optionally substituted divalent monocyclic carbocyclic or heterocyclic raType: ApplicationFiled: December 12, 2008Publication date: December 2, 2010Applicant: BIOTA EUROPE LTDInventors: David John Haydon, Lloyd George Czaplewski
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Publication number: 20100298141Abstract: Disclosed are compounds of Formula 1, including N-oxides, and salts thereof, wherein W is O or NR7, n is 0 or 1, and R1, R2, R3, R4, R5, R6, R7 and m are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound or a composition of the invention. Also disclosed are mixtures and compositions comprising a herbicidally effective amount of a compound of Formula 1 and an effective amount of another herbicide or herbicide safener.Type: ApplicationFiled: February 8, 2008Publication date: November 25, 2010Applicant: E. I. DU PONT DE NEMOURS AND COMPANYInventors: Thomas Paul Selby, Brenton Todd Smith, Thomas Martin Stevenson
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Publication number: 20100298291Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands and methods for using such compounds and compositions.Type: ApplicationFiled: July 30, 2010Publication date: November 25, 2010Applicant: ABBOTT LABORATORIESInventors: Marlon D. Cowart, Yi-Yin Ku, Sou-Jen Chang, Dilinie P. Fernando, Timothy A. Grieme, Robert J. Altenbach
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Publication number: 20100292227Abstract: Compounds of formula I: wherein a, R1, R2, R3, R4, R5 and R6 are defined herein, are useful as inhibitors of HIV replication.Type: ApplicationFiled: May 11, 2010Publication date: November 18, 2010Applicant: BOEHRINGER INGLEHEIM INTERNATIONAL GMBHInventors: CHRISTIANE YOAKIM, MURRAY BAILEY, FRANCOIS BILODEAU, REBEKAH CARSON, LEE FADER, STEPHEN KAWAI, SEBASTIEN MORIN, CARL THIBEAULT, BRUNO SIMONEAU, SIMON SURPRENANT, YOULA TSANTRIZOS, STEVEN LAPLANTE
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Publication number: 20100286110Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof, are agonists of GPR119 and are useful for the treatment of diabetes and as peripheral regulators of satiety, e.g. for the treatment of obesity and metabolic syndrome.Type: ApplicationFiled: October 10, 2008Publication date: November 11, 2010Inventors: Matthew Colin Thor Fyfe, William Gattrell, Colin Peter Sambrook-Smith
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Publication number: 20100273830Abstract: An insecticidal compound of formula (I) in which G1, G2, and G3 together with the two carbon atoms to which G1 and G3 are attached, form a non-aromatic 4- or 5-membered ring system; wherein G1 is sulfur, SO, SO2, oxygen, a direct bond, NRa or CR5aR5b; G2 is sulfur, SO, SO2, oxygen, a direct bond, NRb or CR5cR5d; G3 is sulfur, SO, SO2, oxygen, a direct bond, NRc or CR5eR5f; with the provisos that a) not more than 1 group G can be a direct bond, b) not more than 2 G groups can be oxygen, sulfur, SO or SO2 and c) when 2 G groups are oxygen, SO, SO2 and/or sulfur the two groups are separated by a carbon atom; each of Z1 and Z2, which may be the same or different, represents oxygen or sulfur; D is phenyl or a 5- or 6-membered heteroaromatic ring and R1a, R1b, R5a, R5b, R5c, R5d, R5e, R5f, Ra, Rb Rc, R2, R3 and R20 are specified organic groups and agronomically acceptable salts/isomers/enantiomers/tautomers/N-oxides of those compounds.Type: ApplicationFiled: July 14, 2008Publication date: October 28, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Roger Graham Hall, Olivier Loiseleur, Jagadish Pabba, Sitaram Pal, Andre Jeanguenat, Andrew Edmunds, Andre Stoller
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Publication number: 20100261679Abstract: Disclosed herein are compounds and their oxides, esters, prodrugs, solvates, and pharmaceutically acceptable salts thereof, compositions of the compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier, and uses of the compounds, either alone or in combination with at least one additional therapeutic agent. The embodiments are useful for inhibiting cellular proliferation, inhibiting the growth and/or metathesis of tumors, treating or preventing cancer, treating or preventing degenerating bone diseases such as rheumatoid arthritis, and/or inhibiting molecules such as CSF-1R.Type: ApplicationFiled: October 16, 2008Publication date: October 14, 2010Inventors: James Sutton, Martin Sendzik, Weibo Wang
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Publication number: 20100240620Abstract: The present application relates to novel aryl-substituted 3-cyano-5-thiazolyl- and 3-cyano-5-thiadiazolyl-1,4-dihydropyridines, a process for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially cardiovascular disorders.Type: ApplicationFiled: September 8, 2007Publication date: September 23, 2010Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Lars Barfacker, Peter Kolkhof, Karl-Heinz Schlemmer, Rolf Grosser, Adam Nitsche
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Patent number: 7786125Abstract: The present application is directed to therapeutic compounds, compositions, and methods for culturing neuronal cells and for preventing and the treatment of neurodegenerative diseases, such as Parkinson's disease and amyotrophic lateral sclerosis (ALS).Type: GrantFiled: April 7, 2009Date of Patent: August 31, 2010Inventor: Leu-Fen H. Lin
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Patent number: 7786145Abstract: The present invention provides methods for the use of compounds as depicted by structure I, pharmaceutical compositions containing the same, and methods for the prophylaxis, management and treatment of metabolic diseases and diseases modulated by MCD inhibition. The compounds disclosed in this invention are useful for the prophylaxis, management and treatment of diseases involving in malonyl-CoA regulated glucose/fatty acid metabolism pathway. In particular, these compounds and pharmaceutical composition containing the same are indicated in the prophylaxis, management and treatment of cardiovascular diseases, diabetes, cancer and obesity.Type: GrantFiled: July 28, 2004Date of Patent: August 31, 2010Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Jie Fei Cheng, Bin Liu, Thomas Arrhenius, Mark E. Wilson, Alex M. Nadzan, Gary D. Lopaschuk, Jason R. Dyck, Rossy Serafimov
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Publication number: 20100216810Abstract: Provided is a fused heterocycle derivative showing a strong Raf inhibitory activity. A compound represented by the formula wherein each symbol is as defined in the present specification, or a salt thereof.Type: ApplicationFiled: December 1, 2009Publication date: August 26, 2010Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masanori OKANIWA, Terufumi TAKAGI
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Publication number: 20100216844Abstract: The present invention relates to novel carboxamide compounds and their use as a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity and to a method for the therapeutic and/or prophylactic treatment by administering an effective amount of at least one of these carboxamide compounds. The carboxamide compounds are compounds of the general formula I in which W—R2 is selected from and R1, R2, R3a, R3b, Y1, Y2, Y3, Y4, X, Q, m, k, Rw and Rw* have the meanings mentioned in the claims, the tautomers thereof and the pharmaceutically suitable salts thereof.Type: ApplicationFiled: February 19, 2010Publication date: August 26, 2010Inventors: Andreas Kling, Helmul Mack, Kaija Junios, Achim Mceller, Wllirled Hombarger, Charles W. Hulchins
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Publication number: 20100210688Abstract: The present invention provides compounds of formula (I) wherein e, R1, R2, R3, R4, R5, R4, R5, R6, R7, R7a, R7b, A, D, m and n are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: April 27, 2010Publication date: August 19, 2010Inventors: Roger Bonnert, Alice Flaherty, Garry Pairaudeau, Michael Stocks
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Publication number: 20100210762Abstract: A compound represented by formula (I-1): wherein R21, R22, R23 and R24 each independently represent a hydrogen atom or a monovalent substituent, with the proviso that compounds, in which R21, R22, R23 and R24 each are an alkylthio group, are excluded; R21 and R22 and/or R23 and R24 each may bond to each other to form a ring, with the proviso that compounds, in which the formed ring is a dithiol ring or a dithiolane ring, are excluded; R25 and R26 each independently represent a hydrogen atom or a monovalent substituent; X21, X22, X23 and X24 each independently represent a hetero atom; compounds, wherein R21, R22, R23 and R24 each represent a cyan group; X21, X22, X23 and X24 each represent a sulfur atom; and R25 and R26 each represent a hydroxyl group or a hydrogen atom, are excluded; and compounds, wherein R21 and R23 each represent a hydrogen atom; R22 and R24 each represent an arylcarbonyl group; X21, X22, X23 and X24 each represent a sulfur atom; and R25 and R26 each represent a hydroxyl group, are eType: ApplicationFiled: August 15, 2008Publication date: August 19, 2010Applicant: FUJIFILM CORPORATIONInventors: Naoyuki Hanaki, Masuji Motoki, Toshihiko Yawata
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Patent number: 7776861Abstract: A compound of formula: where Ar1, Ar2, X, R3, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Cycloheteroalkenyl Compound”); compositions comprising an effective amount of a Cycloheteroalkenyl Compound; and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Cycloheteroalkenyl Compound are disclosed herein.Type: GrantFiled: January 23, 2006Date of Patent: August 17, 2010Assignee: Purdue Pharma L.P.Inventors: Qun Sun, Xin Wen
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Publication number: 20100200054Abstract: A compound for an organic photoelectric device, represented by the following Chemical Formula 1:Type: ApplicationFiled: April 19, 2010Publication date: August 12, 2010Inventors: Ho-Kuk Jung, Myeong-Soon Kang, Jin-Seong Park, Nam-Soo Kim, Kyu-Yeol In, Eiu-Su Kang, Mi-Young Chae
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Publication number: 20100197711Abstract: The present invention relates to benzothiazole compounds that mimic the activity of BH3 only proteins and are capable of binding to and neutralizing pro survival Bcl 2 proteins. The invention also relates to the use of such compounds in the regulation of cell death or cell survival and the treatment and/or prophylaxis of diseases or conditions associated with the deregulation of cell death or cell survival.Type: ApplicationFiled: September 27, 2007Publication date: August 5, 2010Inventors: Keith Geoffrey Watson, Guillaume Laurent Lessene, Jonathan Bayldon Baell, David Ching Siang Huang, Ian Philip Street, Jerry McKee Adams, Peter Malcolm Colman, Brad Edmund Sleebs, Brian John Smith, Peter Edward Czabotar
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Publication number: 20100196368Abstract: New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.Type: ApplicationFiled: March 12, 2010Publication date: August 5, 2010Applicant: NOVARTIS VACCINES AND DIAGNOSTICS, INC.Inventors: Payman Amiri, Wendy Fantl, Teresa Hansen, Barry Haskell Levine, Christopher McBride, Daniel J. Poon, Savithri Ramurthy, Paul A. Renhowe, Cynthia M. Shafer, Sharadha Subramanian, Leonard Sung
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Publication number: 20100183743Abstract: Inhibitors of poly(ADP-ribose)polymerase having a structure of Formula (I), ways to make them and methods of treating patients using them are disclosed.Type: ApplicationFiled: January 19, 2010Publication date: July 22, 2010Applicant: ABBOTT LABORATORIESInventors: Magdalena K. Przytulinska, Thomas D. Penning, Yunsong Tong
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Publication number: 20100183852Abstract: 1. A compound of Formula (1) and salts thereof: wherein: R1 and R2 are independently H or optionally substituted alkyl; X and Y are independently CO2H or COSH; Q and T are independent substituents; a+n is 0 to 4; b+m is 0 to 4; and n+m are at least 1; also ink-jet compositions, processes and printed material.Type: ApplicationFiled: May 12, 2008Publication date: July 22, 2010Inventor: Gavin Wright
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Publication number: 20100179190Abstract: The present invention provides novel bicyclic pyrazolo kinase modulators and methods of using the novel bicyclic pyrazolo kinase modulators to treat diseases mediated by kinase activity.Type: ApplicationFiled: November 14, 2008Publication date: July 15, 2010Applicant: SGX PHARMACEUTICALS, INC.Inventors: Pierre-Yves Bounaud, Andrew Vaino
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Publication number: 20100179141Abstract: Disclosed are compounds of the formula (I) wherein X is N or CH, and Y is N or CR5. Also disclosed are methods of treating JNK and ERK mediated diseases using the compounds of formula 1.0.Type: ApplicationFiled: December 17, 2007Publication date: July 15, 2010Inventors: David B. Belanger, M. Arshad Siddiqui, Patrick J. Curran, Blake Hamann, Lianyun Zhao, Panduranga Adulla P. Reddy, Praveen K. Tadikonda, Gerald W. Shipps, JR., Umar Faruk Mansoor
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Publication number: 20100152195Abstract: The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl, indazolyl; p is an integer ranging from 0 to 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl; or corresponds to a group R5; R2 is hydrogen or C1-4alkyl; R3 is C1-4alkyl; R4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; R5 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 a group is optionally substituted by one or two substituentType: ApplicationFiled: December 16, 2009Publication date: June 17, 2010Inventors: Luca Arista, Giorgio Bonanomi, Anna Maria Capelli, Federica Damiani, Romano Di Fabio, Gabriella Gentile, Dieter Hamprecht, Fabrizio Micheli, Luca Tarsi, Giovanna Tedesco, Silvia Terreni
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Publication number: 20100152185Abstract: The instant invention provides compounds of formula I which are 5-lipoxygenase activating protein inhibitors. Compounds of formula I are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.Type: ApplicationFiled: December 7, 2009Publication date: June 17, 2010Inventors: Lin Chu, Mark T. Goulet, Feroze Ujjainwalla, Linda Chang, Richard Frenette, Yves Girard, Michel Therien, Dwight MacDonald, John H. Hutchinson
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Patent number: 7737281Abstract: The present invention provides novel purine-based fluorescent dyes that may be used for staining, localizing and otherwise labeling target molecules, such as nucleic acids, for detection, amplification and quantification.Type: GrantFiled: July 7, 2005Date of Patent: June 15, 2010Assignee: Enzo Life Sciences, Inc. c/o Enzo Biochem, Inc.Inventor: Maciej Szczepanik
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Publication number: 20100137317Abstract: 1,2-disubstituted heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described. Also described are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Among the disorders which may be treated are neurological, neurodegenerative and psychiatric disorders including, but not limited to, those associated with cognitive deficits or schizophrenic symptoms.Type: ApplicationFiled: June 24, 2009Publication date: June 3, 2010Applicant: EnVivo Pharmaceuticals, Inc.Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
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Publication number: 20100130490Abstract: Benzoxazole and benzothiazole compounds and their oxides, esters, prodrugs, solvates, and pharmaceutically acceptable salts thereof are disclosed. Compositions of the compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier, and uses of the compounds, either alone or in combination with at least one additional therapeutic agent are also disclosed. The embodiments are useful for inhibiting cellular proliferation, inhibiting the growth and/or metathesis of tumors, treating or preventing cancer, treating or preventing degenerating bone diseases such as rheumatoid arthritis, and/or inhibiting molecules such as CSF 1R.Type: ApplicationFiled: May 20, 2008Publication date: May 27, 2010Inventors: Simon C. Ng, Keith B. Pfister, Martin Sendzik, James Sutton, Allan S. Wagman, Marion Wiesmann
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Publication number: 20100120802Abstract: Heterocyclic amidines with anti-inflammatory and analgesic activity that inhibit nitrogen oxide production, of formula (I): in which: G1 and G2 are hydrogen, halogen, hydroxyl, C1-C4 alkoxy, C1-C4 alkyl, and an amidino substituent of formula Q, provided that, for each compound of formula (I), only one of the two substituents G1 or G2 is an amidino substituent of formula Q: and in which the substituents W, Y and X are combined to form 9- or 10-membered bicyclic heteroaromatic derivatives containing up to 2 hetero atoms in the same ring; and Z is an aryl or heteroaryl group, a linear or branched C1-C6 alkyl or alkenyl chain, a C1-C4 alkyl-aryl group or a C1-C4 alkyl-heteroaryl group.Type: ApplicationFiled: January 15, 2010Publication date: May 13, 2010Inventors: Francesco MAKOVEC, Antonio Giordani, Roberto Artusi, Stefano Mandelli, Ilario Verpiliq, Simona Zanzola, Lucio Claudio Rovati
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Publication number: 20100113789Abstract: The present invention is to provide a medicinal composition for preventing or treating parasitic protozoan infections, having a high selective toxicity against parasitic protozoan infection, and a superior preventive or treating effect.Type: ApplicationFiled: September 30, 2005Publication date: May 6, 2010Applicants: FUJIFILM CORPORATIONInventors: Masataka Ihara, Kiyosei Takasu, Khanitha Pudhom, Hiroshi Kitaguchi, Masayuki Kawakami, Kozo Sato
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Publication number: 20100113414Abstract: The present invention encompasses compounds of the general formula (1) in which R1 to R3 are defined as in claim 1, which are suitable for treating diseases which are characterized by excessive or anomalous cell proliferation, and their use for producing a pharmaceutical having the abovementioned properties.Type: ApplicationFiled: January 11, 2010Publication date: May 6, 2010Applicant: Boehringer Ingelheim International GmbHInventors: Bodo BETZEMEIER, Trixi BRANDL, Steffen BREITFELDER, Ralph BRUECKNER, Thomas GERSTBERGER, Michael GMACHL, Matthias GRAUERT, Frank HILBERG, Christoph HOENKE, Matthias HOFFMANN, Maria IMPAGNATIELLO, Dirk KESSLER, Christian KLEIN, Bernd KRIST, Udo MAIER, Darryl McCONNELL, Charlotte REITHER, Stefan SCHEUERER, Andreas SCHOOP, Norbert SCHWEIFER, Oliver SIMON, Martin STEEGMAIER, Steffen STEURER, Irene WAIZENEGGER, Ulrike WEYER-CZERNILOFSKY, Andreas ZOEPHEL
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Publication number: 20100098634Abstract: Provided herein are compounds and compositions which comprise the formulae as disclosed herein, wherein the compound is an amyloid binding compound. An amyloid binding compound according to the invention may be administered to a patient in amounts suitable for in vivo imaging of amyloid deposits, and distinguish between neurological tissue with amyloid deposits and normal neurological tissue. Amyloid probes of the invention may be used to detect and quantitate amyloid deposits in diseases including, for example, Down's syndrome, familial Alzheimer's Disease. In another embodiment, the compounds may be used in the treatment or prophylaxis of neurodegenerative disorders. Also provided herein are methods of allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing a neurodegenerative disease.Type: ApplicationFiled: July 24, 2009Publication date: April 22, 2010Inventors: Hartmuth C. Kolb, Joseph C. Walsh, Wei Zhang, Umesh B. Gangadharmath, Dhanalakshmi Kasi, Kai Chen, Anjana Sinha, Eric Wang, Gang Chen, Peter J.H. Scott, Henry Clifton Padgett, Qianwa Liang, Zhiyong Gao, Tieming Zhao, Chunfang Xia
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4,5-RING ANNULATED INDOLE DERIVATIVES FOR TREATING OR PREVENTING OF HCV AND RELATED VIRAL INFECTIONS
Publication number: 20100098661Abstract: The present invention relates to 4,5-ring annulated indole derivatives, compositions comprising at least one 4,5-ring annulated indole derivatives, and methods of using the 4,5-ring annulated indole derivatives for treating or preventing a viral infection or a virus-related disorder in a patient. Wherein ring Z, of formula (I), is a cyclopentyl, cyclopentenyl, 5-membered heterocycloalkyl, 5-membered heterocycloalkenyl or 5-membered heteroaryl ring.Type: ApplicationFiled: December 17, 2007Publication date: April 22, 2010Inventors: Kevin X. Chen, Srikanth Venkatraman, F. George Njoroge, Stuart B. Rosenblum, Charles A. Lesburg, Jose S. Duca, Neng-Yang Shih, Francisco Velazquez, Gopinadhan N. Anilkumar, Qingbei Zeng, Joseph A. Kozlowski -
Publication number: 20100063045Abstract: Objects of the present invention are to study the synthesis of a novel pyridinecarboxylic acid (2-aminophenyl)amide derivative having a novel urea structure and to find a pharmacological effect of the derivative. The invention provides a compound represented by the formula (1) or a salt thereof.Type: ApplicationFiled: March 28, 2008Publication date: March 11, 2010Applicant: Santen Pharmaceutical Co., Ltd.Inventors: Hiroyuki Mogi, Hasashi Tajima, Noriko Mishina, Yusuke Yamazaki, Shinji Yoneda, Katsuhiko Watanabe, Junko Fujikawa, Minoru Yamamoto
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Patent number: 7674801Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.Type: GrantFiled: December 4, 2007Date of Patent: March 9, 2010Assignee: AstraZeneca ABInventors: Gregory Steven Basarab, Shanta Bist, John Irvin Manchester, Brian Sherer
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Patent number: 7671077Abstract: The present application is directed to therapeutic compounds, compositions, and methods for culturing neuronal cells and for preventing and the treatment of neurodegenerative diseases, such as Parkinson's disease and amyotrophic lateral sclerosis (ALS).Type: GrantFiled: July 19, 2004Date of Patent: March 2, 2010Inventor: Leu-Fen Hou Lin
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Patent number: 7655767Abstract: The present invention relates to the use of thiazolyl-pyridinium based dyes in optical layers for optical data recording, preferably for optical data recording using a laser with a wavelength up to 450 nm. The invention further relates to a write only read many (WORM) type optical data recording medium capable of recording and reproducing information with radiation of blue laser, which employs a thiazolyl-pyridinium based type dye in the optical layer. The present invention further relates to new thiazolyl-pyridinium based dyes, of formula (V), (VI) or (VIII).Type: GrantFiled: August 31, 2005Date of Patent: February 2, 2010Assignee: Clariant Finance (BVI) LimitedInventor: Andre Weiss
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Patent number: 7655676Abstract: Use of the compound of formula (I) and the pharmaceutically acceptable addition salts thereof for the manufacture of a medicament for topical treatment or 5 prevention of acne formula (I) wherein: R represents methoxymethyl, R1 represents methyl, Rz represents methyl, Y represents the group formula (II) The compound of formula (I) and the pharmaceutically acid addition salts thereof show selective activity against propionibacterium acne and are suitable for use in a method of treatment or prevention of acne.Type: GrantFiled: June 6, 2003Date of Patent: February 2, 2010Assignee: Naicons S.C.A.R.L.Inventors: Adriano Malabarba, Marco Cavaleri, Giorgio Mosconi, Daniela Jabes, Gabriela Romano
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Publication number: 20090326222Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).Type: ApplicationFiled: June 22, 2009Publication date: December 31, 2009Applicant: ABBOTT LABORATORIESInventors: Marlon D. Cowart, Minghua Sun, Chen Zhao, Guo Zhu Zheng
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Publication number: 20090275588Abstract: The invention relates to novel sulfonamide compounds and their use as orexin receptor antagonists.Type: ApplicationFiled: April 10, 2007Publication date: November 5, 2009Applicant: Actelion Pharmaceuticals Ltd.Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen, Cornella Zumbrunn Acklin
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Publication number: 20090270407Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein A, B, D, R1, R2, R3, X and m are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.Type: ApplicationFiled: April 23, 2009Publication date: October 29, 2009Applicant: E. I. DU PONT DE NEMOURS AND COMPANYInventors: CHI-PING TSENG, Brenton Todd Smith
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Publication number: 20090258907Abstract: Disclosed herein are compounds of formula (I) or pharmaceutical acceptable salts thereof, wherein X, R1, R2, R3, R4, L1, and m, are defined in the specification. Compositions comprising said compounds which can be useful for inhibiting Rho kinase (ROCK) and methods for using said compositions are also described.Type: ApplicationFiled: April 7, 2009Publication date: October 15, 2009Applicant: ABBOTT LABORATORIESInventors: Steven L. Swann, Anil Vasudevan
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Publication number: 20090221645Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof, exhibit 5-HT1A agonism in addition to noradrenaline reuptake inhibition and optionally also 5-HT reuptake inhibition are useful for the treatment of obesity.Type: ApplicationFiled: February 8, 2006Publication date: September 3, 2009Inventors: Oscar Barba, Graham John Dawson, Thomas Martin Krulle, Robert John Rowley, Donald Smyth, Gerard Hugh Thomas
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Publication number: 20090221587Abstract: Compounds of formula (I), wherein the substituents are as defined in claim (1), and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula (I) can be used as agrochemical active ingredients and can be prepared in a manner known per se.Type: ApplicationFiled: August 14, 2006Publication date: September 3, 2009Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Andre Jeanguenat, Roger Graham Hall, Olivier Loiseleur, Stephan Trah, Patricia Durieux, Andrew Edmunds, Andrew Edmunds, Andre Stoller
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Publication number: 20090209532Abstract: Compounds of formula (I) exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors.Type: ApplicationFiled: July 17, 2006Publication date: August 20, 2009Inventors: Marko Ahlmark, Reijo Backstrom, Anne Luiro, Jarmo Pystynen, Eija Tiainen
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Publication number: 20090197883Abstract: The instant invention provides compounds of Formula (I) which are 5-lipoxygenase activating protein inhibitors. Compounds of Formula (I) are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.Type: ApplicationFiled: March 3, 2006Publication date: August 6, 2009Inventors: Helen M. Armstrong, Linda L. Chang, Richard Frenette, Dwight MacDonald, Hyun O. Ok, Michel Therien, Feroze Ujjainwalla
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Publication number: 20090197877Abstract: Compounds of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; AIk is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical which may contain an ether (—O—), thioether (—S—) or amino (—NR)— link, wherein R is hydrogen, —CN or C1-C3 alkyl; X is —C(?O)NR6—, —S(O)NR6—, —C(?O)O— or —S(?O)O— wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, -Cyc, or —(C1-C3 alkyl)-Cyc wherein Cyc is optionally substituted monocyclic carbocyclic or heterocyclic having 3-7 ring atoms; Z is N or CH, or CF; R2 and R3 are as defined in the description.Type: ApplicationFiled: June 21, 2007Publication date: August 6, 2009Applicant: Prolysis LTD.Inventors: David John Haydon, Lloyd George Czaplewski, Nicholas John Palmer, Dale Robert Mitchell, John Frederick Atherall, Christopher Richard Steele, Tamara Ladduwahetty
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Patent number: 7569695Abstract: The present invention provides dyes, reactive dyes and labeled reagents that may be used in the detection or quantification of desirable target molecules, such as proteins and nucleic acids. Dyes are provided that may be used free in solution where the binding of the dye to the target molecule provides signal generation. Dyes are also provided that comprise reactive groups that may be used to attach the dyes to probes that will bind to desirable target molecules. The novel dyes of the present invention have been modified by the addition of charged and polar groups to provide beneficial properties.Type: GrantFiled: May 24, 2005Date of Patent: August 4, 2009Assignee: Enzo Life Sciences, Inc.Inventors: Yuejun Xiang, Praveen Pande, Rajesh Khazanchi, Elazar Rabbani, Dakai Liu, Wei Cheng
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Novel 3-Bicyclocarbonylaminopyridine-2-Carboxamides or 3-Bicyclocarbonylaminopyrazine-2-Carboxamides
Publication number: 20090181968Abstract: The present invention relates to compounds of formula (I) [Chemical formula should be inserted here. Please see paper copy] as well as pharmaceutically acceptable salts and pharmaceutical compositions including the compounds are prepared or thereof: wherein, A1, A2, R1, R2, R3, R4, and R5 and n are as defined in the specification. The compounds of formula (I) are useful in therapy.Type: ApplicationFiled: November 22, 2006Publication date: July 16, 2009Applicant: ASTRAZENECA ABInventors: Kosrat Amin, Johan Broddefalk, Yantao Chen, Karolina Nilsson, Claire Milburn, Helene Desfosses, Ziping Liu, Maxime Tremblay, Christopher Walpole, Zhong-yong Wei, Hua Yang -
Patent number: 7553854Abstract: Benzoxazole and benzothiazole compounds and the stereoisomers, tautomers, solvates, oxides, esters, and prodrugs thereof and pharmaceutically acceptable salts thereof are disclosed. Compositions of the compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier, and uses of the compounds, either alone or in combination with at least one additional therapeutic agent are also disclosed. The embodiments are useful for inhibiting cellular proliferation, inhibiting the growth and/or metathesis of tumors, treating or preventing cancer, treating or preventing degenerating bone diseases such as rheumatoid arthritis, and/or inhibiting molecules such as CSF-1R.Type: GrantFiled: April 18, 2007Date of Patent: June 30, 2009Assignee: Novartis Vaccines and Diagnostics, Inc.Inventors: James C Sutton, Marion Wiesmann, Weibo Wang, Mika Lindvall, Jiong Lan, Savithri Ramurthy, Anu Sharma, Elizabeth J. Mieuli, Liana M. Klivansky, William Lenahan, Susan Kaufman, Hong Yang, Simon C. Ng, Keith Pfister, Allan S. Wagman, Victoria Sung, Martin Sendzik
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Publication number: 20090162283Abstract: To provide a diagnostic drug which binds specifically to an amyloid aggregate and/or an amyloid deposit, to thereby realize imaging and quantification of a disease caused by amyloid aggregation and/or deposition. The invention provides a compound represented by formula (1): (wherein X1 represents an optionally substituted bicyclic heterocyclic group; X2 represents a hydrogen atom, a halogen atom, or a chelate-forming group; ring A represents a benzene ring or a pyridine ring; and ring B represents an optionally substituted 5-membered aromatic heterocyclic group which is bonded to the benzene ring or the pyridine ring via a carbon atom of ring B), a salt thereof, a solvate of any of these, or a transition metal coordination compound of any of these, and a diagnostic, preventive, or therapeutic drug containing the same.Type: ApplicationFiled: November 30, 2006Publication date: June 25, 2009Applicants: Fujifilm RI Pharma Co., Ltd., Daiichi Sankyo Company, LimitedInventors: Kazunori Bando, Kazumi Taguchi