Polycyclo Ring System Having The Five-membered Hetero Ring As One Of The Cyclos Patents (Class 548/126)
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Publication number: 20130109019Abstract: Embodiments of hapten conjugates including a hapten, an optional linker, and a peroxidase-activatable aryl moiety are disclosed. In some embodiments, the peroxidase-activatable aryl moiety is tyramine or a tyramine derivative. Embodiments of methods for making and using the hapten conjugates also are disclosed. In particular embodiments, the hapten conjugates are used in a signal amplification assay. In certain embodiments, the hapten is an oxazole, a pyrazole, a thiazole, a benzofurazan, a triterpene, a urea, a thiourea other than a rhodamine thiourea, a nitroaryl other than dinitrophenyl or trinitrophenyl, a rotenoid, a cyclolignan, a heterobiaryl, an azoaryl, a benzodiazepine, or 7-diethylamino-3-carboxycoumarin. The hapten is coupled to the peroxidase-activatable aryl moiety directly or indirectly via a linker. In certain embodiments, the hapten conjugates are used in multiplexed assays.Type: ApplicationFiled: July 1, 2011Publication date: May 2, 2013Inventors: Adrian E. Murillo, Jerome W. Kosmeder, Eric May, William Day, Mark Lefever, Anne M. Pedata, Christopher Bieniarz, Phillip Miller
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Publication number: 20130102609Abstract: The present invention provides biaryl oxyacetic acid compounds which may be useful for treating inflammatory disorders, including disorders affecting the respiratory system and skin.Type: ApplicationFiled: December 14, 2012Publication date: April 25, 2013Applicant: LIGAND PHARMACEUTICALS INC.Inventor: Ligand Pharmaceuticals Inc.
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Publication number: 20130085256Abstract: Described herein are compositions including heterocyclic organic compounds based on fused thiophene compounds, polymers based on fused thiophene compounds, and methods for making the monomers and polymer along with uses in thin film-based and other devices.Type: ApplicationFiled: October 31, 2012Publication date: April 4, 2013Inventors: Mingqian He, Jianfeng Li, James Robert Matthews, Weijun Niu, Arthur L. Wallace
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Publication number: 20130074927Abstract: The invention provides highly fluorescent materials comprising a single (n=0) or a series (n=1, 2, etc.) of benzo heterocyclic systems. The photo-stable highly luminescent chromophores are useful in various applications, including in wavelength conversion films. Wavelength conversion films have the potential to significantly enhance the solar harvesting efficiency of photovoltaic or solar cell devices.Type: ApplicationFiled: September 25, 2012Publication date: March 28, 2013Applicant: NITTO DENKO CORPORATIONInventor: NITTO DENKO CORPORATION
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Publication number: 20130052138Abstract: The presently disclosed subject matter provides compositions that selectively bind cyclooxygenase-2 and comprise a therapeutic and/or diagnostic moiety. Also provided are methods for using the disclosed compositions for diagnosing (i.e., by imaging) a target cell and/or treating a disorder associated with a cyclooxygenase-2 biological activity.Type: ApplicationFiled: March 27, 2012Publication date: February 28, 2013Applicant: Vanderbilt UniversityInventors: Lawrence J. Marnett, Md. Jashim Uddin, Brenda C. Crews
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Patent number: 8372991Abstract: Described herein are compounds of Formula (I): wherein A, J, Z, X, R1 and R4 are defined herein, and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: GrantFiled: March 17, 2011Date of Patent: February 12, 2013Assignee: Calcimedica, Inc.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Patent number: 8372870Abstract: The present invention is directed to modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.Type: GrantFiled: August 29, 2011Date of Patent: February 12, 2013Assignee: Incyte CorporationInventors: Andrew P. Combs, Eddy W. Yue
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Patent number: 8367840Abstract: The invention relates to a compound of general formula (I) for use in a pharmaceutical composition for treating infectious diseases caused by Helicobacter pylori. R1 and R2 are O, S or N, and can be identical or different; R3 is O or S; R4 is H or a C1-C6 alkyl group; n represents a value between 0 and 3; and R5 is an NO2, COOR? or SO3R? radical, where R? is a H or a C1-C6 alkyl group.Type: GrantFiled: February 22, 2008Date of Patent: February 5, 2013Assignee: Universidad de ZaragozaInventors: Javier Sancho Sanz, Adrián Velazquez Campoy, Nunilo Cremades Casasin
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Publication number: 20130026459Abstract: A photoelectric conversion device that contains a polymer compound having a structural unit represented by formula (1) has high photoelectric conversion efficiency. (wherein, X1 and X2 are the same or different and represent a nitrogen atom or ?CH—. Y1 represents a sulfur atom, an oxygen atom, a selenium atom, —N(R1)— or —CR2?CR3—. R1, R2 and R3 are the same or different and represent a hydrogen atom or a substituent. W1 represents a cyano group, a monovalent organic group having a fluorine atom or a halogen atom. W2 represents a cyano group, a monovalent organic group having a fluorine atom, a halogen atom or a hydrogen atom.Type: ApplicationFiled: April 21, 2011Publication date: January 31, 2013Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Ken Yoshimura, Kenichiro Ohya
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Publication number: 20130019949Abstract: Provided are compounds with a donor moiety, a first acceptor moiety and a second acceptor moiety, as shown by Formula (I): With the unique molecular design, compounds of Formula (I) can provide a desirable power conversion efficiency. Moreover, this invention also provides organic thin-film solar cells comprising the above-mentioned compounds.Type: ApplicationFiled: January 3, 2012Publication date: January 24, 2013Inventors: KEN-TSUNG WONG, HAO-WU LIN, LI-YEN LIN, FRANCIS LIN, YI-HONG CHEN, SHI-WEN CHIU
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Patent number: 8357704Abstract: A compound of formula I wherein m, n, A, B, D, E, G, H, Y, R1, R2, R3, R4, R5, and R8, are described herein.Type: GrantFiled: June 10, 2010Date of Patent: January 22, 2013Assignee: Bristol-Myers Squibb CompanyInventors: James A. Johnson, John Lloyd, Alexander Kover
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Publication number: 20130018039Abstract: Disclosed are compounds having the formula: wherein R1A, R1B, R2 and R3 are defined herein, and methods of making and using the same.Type: ApplicationFiled: March 31, 2011Publication date: January 17, 2013Inventors: Vera Q. Bodmer, Linda N. Casillas, Michael P. DeMartino, Philip A. Harris, Bryan W. King, Ami Lakdawala Shah, Lara Kathryn Leister, Joshi M. Ramanjulu, Joseph J. Romano, Gren Z. Wang, Matthew A. Wilson, David Duff Wisnoski
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Patent number: 8329915Abstract: An organic compound represented by the following general formula (I) and characterized by the conjugation of thieno[3,2-b]thiophene, thiophene and phenylene units in the conjugated compound.Type: GrantFiled: February 19, 2009Date of Patent: December 11, 2012Assignees: Nanyang Technological University, Agency for Science, Technology and ResearchInventors: Omer E. Ahmed Moawia, Ashok Mishra, Andrew Grimsdale, Siu Choon Ng, Subodh G. Mhaisalkar, Beng Ong, Zhikuan Chen
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Publication number: 20120298976Abstract: There is presently provided organic compounds of formula I, n-type acceptor materials derived from such compounds and devices comprising such n-type acceptor materials.Type: ApplicationFiled: October 22, 2009Publication date: November 29, 2012Applicant: AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCHInventors: Prashant Sonar, Richard Yee Cheong Shin Koy Sien, Zhikuan Chen, Kok Haw Ong, Ging Meng Ng, Achmad Zen
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Publication number: 20120295897Abstract: This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.Type: ApplicationFiled: July 25, 2012Publication date: November 22, 2012Applicant: Xenon Pharmaceuticals Inc.Inventors: Mikhail Chafeev, Sultan Chowdhury, Lauren Fraser, Jianmin Fu, Jonathan Langille, Shifeng Liu, Jianyu Sun, Shaoyi Sun, Serguei Sviridov, Mark Wood, Alla Yurevna Zenova, Qi Jia, Jean-Jacques Cadieux, Simon J. Gauthier, Amy Frances Douglas, Tom Hsieh, Nagasree Chakka, Zoran Cikojevic
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Publication number: 20120269864Abstract: The present invention is a compound of formula (I) or formula (II) which are suitable as NP-1 antagonists.Type: ApplicationFiled: June 11, 2012Publication date: October 25, 2012Inventors: Haiyan Jia, Ian ZACHARY, Michelle TICKNER, Lili CHENG, Chris CHAPMAN, Katie ELLARD, Basil HARTZOULAKIS, Ashley JARVIS, Rosemary LYNCH, Jamie NALLY, David SELWOOD, Mark STEWART
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Publication number: 20120252784Abstract: Novel 2,3,4-benzothiadiazepines-2,2-dioxides and processes for the preparation thereof are disclosed. The compounds influence the central nervous system and may be used to treat or prevent Alzheimer's disease, Parkinson's disease or Huntington's disease, senile dementia not of the Alzheimer's type, vascular dementia, post-stroke dementia, Korsakoff's syndrome, Down's syndrome, schizophrenia, panic disorder, post-traumatic stress disorder, anxiety or depression.Type: ApplicationFiled: March 13, 2012Publication date: October 4, 2012Inventors: Jozsef FETTER, Ferenc BERTHA, Balazs MOLNAR, Gyula SIMIG, Jozsef BARKOCZY, Balazs VOLK, Gyoergy LEVAY, Istvan GACSALYI, Gabor GIGLER, Hajnalka KOMPAGNE, Bernadett MARKO, Katalin NAGY, Peter KIRICSI, Laszlo Gabor HARSING, Gabor SZENASI
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Publication number: 20120245208Abstract: The present invention relates to 2-oxo-1-pyrrolidine imidazothiadiazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: October 21, 2010Publication date: September 27, 2012Applicant: UCB PHARMA, S.A.Inventors: Yannick Quesnel, Laurent Turet, Joël Mercier
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Publication number: 20120232071Abstract: The present invention relates to compounds of formula I wherein R1a to R1e, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.Type: ApplicationFiled: May 22, 2012Publication date: September 13, 2012Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
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Publication number: 20120207729Abstract: The invention relates to substituted benzothiazoles, benzoxazoles—and their counterparts having pyridine and pyrimidine rings replacing the benzene ring—that are PDE4 inhibitors useful for treating stroke, myocardial infarct, and cardiovascular inflammatory conditions, to pharmaceutical compositions comprising these compounds, and to methods for the treatment of stroke, myocardial infarct, and cardiovascular inflammatory conditions in a mammal. The compounds have general formula I: in which A and B are carbocycles or heterocycles.Type: ApplicationFiled: April 24, 2012Publication date: August 16, 2012Applicant: DECODE GENETICS EHFInventors: Jasbir SINGH, Mark E. GURNEY, Alex BURGIN, Alexander KISELYOV, Munagala RAO
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Publication number: 20120205596Abstract: The present invention provides a macromolecular compound by which the short-circuit current density and the photoelectric conversion efficiency are enhanced when the macromolecular compound is used in an organic layer contained in a photovoltaic cell.Type: ApplicationFiled: October 29, 2010Publication date: August 16, 2012Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Ken Yoshimura, Kenichiro Ohya
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Publication number: 20120202781Abstract: The present invention relates to anindane derivative according to formula I wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising one or more of said indane derivatives and to their use in therapy, for instance in the treatment or prevention of psychiatric diseases where an enhancement of synaptic responses mediated by AMPA receptors is required, including schizophrenia, depression and Alzheimer's disease.Type: ApplicationFiled: April 8, 2010Publication date: August 9, 2012Inventors: Kevin James Gillen, Jonathan Gillespie, Craig Jamieson, John Kinnaird Ferguson MacLean, Elizabeth Margaret Moir, Zoran Rankovic
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Patent number: 8236964Abstract: The invention relates to novel thiazolidine derivatives of the formula (I) wherein A and R1 are as described in the description and their use as medicaments, especially as orexin receptor antagonists.Type: GrantFiled: March 25, 2008Date of Patent: August 7, 2012Assignee: Actelion Pharmaceuticals Ltd.Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen
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Publication number: 20120190098Abstract: Fluorophores derived from photoactivatable azide-pi-acceptor fluorogens or from a thermal reaction of an azide-pi-acceptor fluorogen with an alkene or alkyne are disclosed. Fluorophores derived from a thermal reaction of an alkyne-pi-acceptor fluorogen with an azide are also disclosed. The fluorophores can readily be activated by light and can be used to label a biomolecule and imaged on a single-molecule level in living cells.Type: ApplicationFiled: March 1, 2012Publication date: July 26, 2012Applicants: LELAND STANFORD JUNIOR UNIVERSITY, KENT STATE UNIVERSITYInventors: ROBERT J. TWIEG, WILLIAM E. MOERNER, SAMUEL J. LORD, NA LIU, REICHEL SAMUEL
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Patent number: 8217064Abstract: Tetrasubstituted benzenes that act as modulators of gamma secretase and their use in the treatment of one or more symptoms of treating neurodegenerative disorders, e.g., Alzheimer's disease, are described.Type: GrantFiled: December 22, 2008Date of Patent: July 10, 2012Assignee: EnVivo Pharmaceuticals, Inc.Inventors: Gideon Shapiro, Richard Chesworth
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Publication number: 20120152357Abstract: High performance organic photovoltaic cells based on donor acceptor polymers in the active layer. A composition comprising: at least one copolymer comprising at least one first donor moiety and at least one first acceptor moiety in the copolymer backbone, wherein the first acceptor moiety comprises at least one first ring which is bivalently linked to the copolymer backbone and at least one second ring fused to the first ring and not bivalently linked to the copolymer backbone, wherein the first ring or the second ring comprises two adjacent fluoro ring substituents, and optionally, wherein the donor comprises at least one fused ring system. High efficiency, high Voc, and a combination of both can be achieved.Type: ApplicationFiled: December 14, 2011Publication date: June 21, 2012Inventors: Christopher T. BROWN, Elena E. Sheina, Ting Xu
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Publication number: 20120142689Abstract: In one aspect, the invention relates to compounds of formula I: where Y, R1, R2, n, and Q are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: ApplicationFiled: December 1, 2011Publication date: June 7, 2012Applicant: THERAVANCE, INC.Inventors: Eric L. STANGELAND, Lori Jean VAN ORDEN, Daisuke Roland SAITO
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Patent number: 8193228Abstract: Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.Type: GrantFiled: October 16, 2007Date of Patent: June 5, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: David Chen, Christopher L. Franklin, Peter R. Guzzo, Linus S. Lin, Michael M. C. Lo, Ravi P. Nargund, Iyassu K. Sebhat
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Patent number: 8183275Abstract: Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.Type: GrantFiled: October 16, 2007Date of Patent: May 22, 2012Assignees: Merck Sharp & Dohme Corp., Albany Molecular Research, Inc.Inventors: Peter H. Dobbelaar, Christopher L. Franklin, Allan Goodman, Cheng Guo, Peter R. Guzzo, Mark Hadden, Shuwen He, Alan J. Henderson, Tianying Jian, Linus S. Lin, Jian Liu, Ravi P. Nargund, Megan Ruenz, Bruce J. Sargent, Iyassu K. Sebhat, Larry Yet
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Publication number: 20120122862Abstract: The present invention is a compound of formula (I) or formula (II) which are suitable as NP-1 antagonists.Type: ApplicationFiled: January 30, 2012Publication date: May 17, 2012Inventors: Haiyan Jia, Ian Zachary, Michelle Tickner, Lili Cheng, Chris Chapman, Katie Ellard, Basil Hartzoulakis, Ashley Jarvis, Rosemary Lynch, Jamie Nally, David Selwood, Mark Stewart
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Publication number: 20120122937Abstract: Methods and pharmaceutical compositions for treating cancer utilizing compounds characterized by the following structure: and their pharmaceutically acceptable salts.Type: ApplicationFiled: December 14, 2011Publication date: May 17, 2012Inventors: HSU-SHAN HUANG, TSUNG-CHIH CHEN, TAI-LUNG CHA
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Publication number: 20120115841Abstract: The present invention relates to bridged spiro[2.4]heptane derivatives of formula (I), wherein W, Y, Z, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds as ALX receptor and/or FPRL2 agonists for the treatment of inflammatory and obstructive airways diseases.Type: ApplicationFiled: May 17, 2010Publication date: May 10, 2012Applicant: ACTELION PHARMACEUTICALS LTD.Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
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Patent number: 8153446Abstract: Fluorophores derived from photoactivatable azide-pi-acceptor fluorogens or from a thermal reaction of an azide-pi-acceptor fluorogen with an alkene or alkyne are disclosed. Fluorophores derived from a thermal reaction of an alkyne-pi-acceptor fluorogen with an azide are also disclosed. The fluorophores can readily be activated by light and can be used to label a biomolecule and imaged on a single-molecule level in living cells.Type: GrantFiled: May 13, 2009Date of Patent: April 10, 2012Assignees: Kent State University, Leland Stanford Junior UniversityInventors: Robert J. Twieg, William E. Moerner, Samuel J. Lord, Na Liu, Reichel Samuel
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Patent number: 8133515Abstract: 1,3-Dipole-functional compounds (e.g., azide functional compounds) can be reacted with certain alkynes in a cyclization reaction to form heterocyclic compounds. Useful alkynes (e.g., strained, cyclic alkynes) and methods of making such alkynes are also disclosed. The reaction of 1,3-dipole-functional compounds with alkynes can be used for a wide variety of applications including the immobilization of biomolecules on a substrate.Type: GrantFiled: November 21, 2008Date of Patent: March 13, 2012Assignee: University of Georgia Research Foundation, Inc.Inventors: Geert-Jan Boons, Jun Guo, Xinghai Ning, Margaretha Wolfert
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Publication number: 20120046255Abstract: The present invention relates to non-steroidal compounds useful in the treatment of inflammatory conditions and pharmaceutical compositions comprising them.Type: ApplicationFiled: April 14, 2008Publication date: February 23, 2012Applicant: THE UNIVERSITY OF MELBOURNE of ROYAL PARADE PARKVILLEInventors: Alastair Stewart, Martin Banwell, Brenda Leung, Anu Augustine, Jacki Kitching, Tomasz Bilski
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Publication number: 20120040011Abstract: 1,3-Dipole-functional compounds (e.g., azide functional compounds) can be reacted with certain alkynes in a cyclization reaction to form heterocyclic compounds. Useful alkynes (e.g., strained, cyclic alkynes) and methods of making such alkynes are also disclosed. The reaction of 1,3-dipole-functional compounds with alkynes can be used for a wide variety of applications including the immobilization of biomolecules on a substrate.Type: ApplicationFiled: November 21, 2008Publication date: February 16, 2012Applicant: University of Georgia Research Foundation, Inc.Inventors: Geert-Jan Boons, Jun Guo, Xinghai Ning, Margaretha Wolfert
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Publication number: 20120035173Abstract: This invention relates to compounds, pharmaceutical compositions and methods for use in the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for basic and higher order behaviors. These brain networks, which are involved in regulation of breathing, and cognitive abilities related to memory impairment, such as is observed in a variety of dementias, in imbalances in neuronal activity between different brain regions, as is suggested in disorders such as Parkinson's disease, schizophrenia, respiratory depression, sleep apneas, attention deficit hyperactivity disorder and affective or mood disorders, among numerous others. In a particular aspect, the invention relates to compounds useful for treatment of such conditions, and methods of using these compounds for such treatment.Type: ApplicationFiled: September 6, 2011Publication date: February 9, 2012Inventors: Leslie Street, Rudolf Mueller, Steven Lee
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Publication number: 20120021007Abstract: The present invention relates to nitric oxide furoxan derivative compounds which showed to be active in the treatment of tumors. In addition, they may be used as adjuvants in cancer immunotherapy.Type: ApplicationFiled: January 15, 2010Publication date: January 26, 2012Inventors: Antonella Viola, Enzo Bronte, Marco Crosetti, Loretta Lazzarato, Roberta Fruttero, Alberto Gasco
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Publication number: 20120015990Abstract: Provided herein are small molecule inhibitors of Taspase1 and methods of using the small molecule inhibitors of Taspase1 to treat neoplasm in subjects in need thereof.Type: ApplicationFiled: June 17, 2011Publication date: January 19, 2012Applicant: THE WASHINGTON UNIVERSITYInventors: James Hsieh, Emily Cheng
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Publication number: 20120015989Abstract: Provided herein are compounds and compositions for interfering with the association of Myc and Max. These compounds and compositions are useful in methods for inhibiting growth or proliferation of a cell. Methods of inhibiting growth or proliferation of a cell comprise contacting the cell with an amount of a compound that interferes with Myc and Max association effective to inhibit growth or proliferation of the cell.Type: ApplicationFiled: January 15, 2010Publication date: January 19, 2012Inventors: Steven J. Metallo, Edward V. Prochownik, Ariele Viacava Follis
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Patent number: 8097730Abstract: The present invention is directed to novel bicyclic heterocycles, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.Type: GrantFiled: October 15, 2009Date of Patent: January 17, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Xuqing Zhang, Zhihua Sui
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Patent number: 8080569Abstract: The present invention relates to derivatives of imidazo[2,1-b]thiazoles of formula I, in which R, R1 to R3 and n have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired.Type: GrantFiled: May 15, 2009Date of Patent: December 20, 2011Assignee: Sanofi-AventisInventors: Gerhard Zoller, Hartmut Strobel, David William Will, Paulus Wohlfart
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Publication number: 20110306542Abstract: Compounds that bind the glucagon-like peptide 1 receptor (GLP-1) receptor are provided including compounds which are modulators of the GLP-1 receptors and compounds which are capable of inducing a stabilizing effect on the receptor for use in structural analyses of the GLP-1 receptor. Methods of synthesis, methods of therapeutic and/or prophylactic use, and methods of use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor of such compounds are provided.Type: ApplicationFiled: June 9, 2011Publication date: December 15, 2011Applicant: Receptos, Inc.Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Liming Huang, Junko Tamiya, Mark T. Griffith, Thomas Fowler, Andrew Novak, Michael Knaggs, Premji Meghani
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Publication number: 20110306082Abstract: Disclosed are benzoxazole-based compounds, kits, and methods of producing and using the described compounds in fluorescence-based detection of analytes (e.g., metal ions). Also disclosed are uses of benzoxazole-based compounds as ratiometric metal ion indicators.Type: ApplicationFiled: December 29, 2009Publication date: December 15, 2011Applicant: LIFE TECHNOLOGIES CORPORATIONInventors: Kyle Gee, Vladimir Martin
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Publication number: 20110288089Abstract: A compound of Formula (I): wherein A1, A2, A3, A4, A5, G1, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode and mollusc pests.Type: ApplicationFiled: January 13, 2010Publication date: November 24, 2011Applicant: SYNGENTA CROP PROTECTION LLCInventors: Peter Renold, Jerome Yves Cassayre, Jagadish Pabba, Myriem El Qacemi, Thomas Pitterna
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Publication number: 20110281879Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.Type: ApplicationFiled: January 12, 2011Publication date: November 17, 2011Applicant: ViroBay, Inc.Inventor: Craig Mossman
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Publication number: 20110275680Abstract: The invention relates to novel chemical compounds, in particular oxime derivatives of 3,5-seco-4-nor-cholestane, to the application thereof as drugs, in particular cytoprotective drugs, and more particularly as neuroprotective, cardioprotective and/or hepatoprotective drugs.Type: ApplicationFiled: December 17, 2009Publication date: November 10, 2011Applicant: TROPHOSInventors: Cyrille Drouot, Abdesslame Nazih, Corinne Chaimbault
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Publication number: 20110274655Abstract: Provided herein are tetrazolone FASN inhibitors of the formula (I): or a pharmaceutically acceptable form thereof; wherein the variables RA, RB and RC are defined herein. Also provided herein are pharmaceutical compositions of the compounds provided herein as well as methods of their use for the treatment of various disorders such as hyperproliferative disorders, inflammatory disorders, obesity-related disorders and microbial infections.Type: ApplicationFiled: May 5, 2011Publication date: November 10, 2011Applicant: Infinity PharmaceuticalsInventors: Adilah BAHADOOR, Alfredo C. Castro, Lawrence K. Chan, Gregg F. Keaney, Marta Nevalainen, Vesa Nevalainen, Stephane Peluso, Daniel A. Snyder, Thomas T. Tibbitts
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Publication number: 20110269960Abstract: An object of the present invention is to provide a compound having an action of inhibiting binding between S1P and its receptor, Edg-1 (S1P1), and is useful as a pharmaceutical compound. A compound or a pharmaceutically acceptable salt thereof, which compound is represented by the formula below (where A represents an oxygen atom, a sulfur atom, a group represented by Formula —SO—, a group represented by Formula —SO2—, or the like, R1 represents a hydrogen atom, an alkyl group having 1-6 carbon atoms, or the like, R1A represents a hydrogen atom or the like, R2 represents an alkyl group having 1-6 carbon atoms, a cycloalkyl group having 3-6 carbon atoms, or the like, R3 represents an aryl group, R4 represents a hydrogen atom or an alkyl group having 1-6 carbon atoms and optionally substituted with a carboxyl group, and R5 represents an alkyl group having 1-10 carbon atoms, a cycloalkyl group having 3-8 carbon atoms, an aryl group which is optionally substituted, or the like).Type: ApplicationFiled: July 11, 2011Publication date: November 3, 2011Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Naoya ONO, Tetsuo Takayama, Fumiyasu Shiozawa, Hironori Katakai, Tetsuya Yabuuchi, Tomomi Ota, Makoto Yagi, Masakazu Sato
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Publication number: 20110269804Abstract: A compound of formula (I): where A, B, C, G, m, n, o, p, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.Type: ApplicationFiled: July 24, 2009Publication date: November 3, 2011Applicant: SYNGENTA CROP PROTECTION LLCInventors: Jérôme Yves Cassayre, Peter Renold, Thomas Pitterna, Vladimir Bobosik, Myriem El Qacemi, Anne Jacqueline Dalencon, Werner Zambach, Christopher Richard Ayles Godfrey, Pierre Joseph Marcel Jung, Jagadish Pabba