Polycyclo Ring System Having The Five-membered Hetero Ring As One Of The Cyclos Patents (Class 548/126)
  • Publication number: 20130109019
    Abstract: 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: Application
    Filed: July 1, 2011
    Publication date: May 2, 2013
    Inventors: Adrian E. Murillo, Jerome W. Kosmeder, Eric May, William Day, Mark Lefever, Anne M. Pedata, Christopher Bieniarz, Phillip Miller
  • Publication number: 20130102609
    Abstract: 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: Application
    Filed: December 14, 2012
    Publication date: April 25, 2013
    Applicant: LIGAND PHARMACEUTICALS INC.
    Inventor: Ligand Pharmaceuticals Inc.
  • Publication number: 20130085256
    Abstract: 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: Application
    Filed: October 31, 2012
    Publication date: April 4, 2013
    Inventors: Mingqian He, Jianfeng Li, James Robert Matthews, Weijun Niu, Arthur L. Wallace
  • Publication number: 20130074927
    Abstract: 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: Application
    Filed: September 25, 2012
    Publication date: March 28, 2013
    Applicant: NITTO DENKO CORPORATION
    Inventor: NITTO DENKO CORPORATION
  • Publication number: 20130052138
    Abstract: 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: Application
    Filed: March 27, 2012
    Publication date: February 28, 2013
    Applicant: Vanderbilt University
    Inventors: Lawrence J. Marnett, Md. Jashim Uddin, Brenda C. Crews
  • Patent number: 8372991
    Abstract: 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: Grant
    Filed: March 17, 2011
    Date of Patent: February 12, 2013
    Assignee: Calcimedica, Inc.
    Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • Patent number: 8372870
    Abstract: The present invention is directed to modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.
    Type: Grant
    Filed: August 29, 2011
    Date of Patent: February 12, 2013
    Assignee: Incyte Corporation
    Inventors: Andrew P. Combs, Eddy W. Yue
  • Patent number: 8367840
    Abstract: 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: Grant
    Filed: February 22, 2008
    Date of Patent: February 5, 2013
    Assignee: Universidad de Zaragoza
    Inventors: Javier Sancho Sanz, Adrián Velazquez Campoy, Nunilo Cremades Casasin
  • Publication number: 20130026459
    Abstract: 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: Application
    Filed: April 21, 2011
    Publication date: January 31, 2013
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Ken Yoshimura, Kenichiro Ohya
  • Publication number: 20130019949
    Abstract: 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: Application
    Filed: January 3, 2012
    Publication date: January 24, 2013
    Inventors: KEN-TSUNG WONG, HAO-WU LIN, LI-YEN LIN, FRANCIS LIN, YI-HONG CHEN, SHI-WEN CHIU
  • Patent number: 8357704
    Abstract: 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: Grant
    Filed: June 10, 2010
    Date of Patent: January 22, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: James A. Johnson, John Lloyd, Alexander Kover
  • Publication number: 20130018039
    Abstract: Disclosed are compounds having the formula: wherein R1A, R1B, R2 and R3 are defined herein, and methods of making and using the same.
    Type: Application
    Filed: March 31, 2011
    Publication date: January 17, 2013
    Inventors: 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
  • Patent number: 8329915
    Abstract: 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: Grant
    Filed: February 19, 2009
    Date of Patent: December 11, 2012
    Assignees: Nanyang Technological University, Agency for Science, Technology and Research
    Inventors: Omer E. Ahmed Moawia, Ashok Mishra, Andrew Grimsdale, Siu Choon Ng, Subodh G. Mhaisalkar, Beng Ong, Zhikuan Chen
  • Publication number: 20120298976
    Abstract: 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: Application
    Filed: October 22, 2009
    Publication date: November 29, 2012
    Applicant: AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH
    Inventors: Prashant Sonar, Richard Yee Cheong Shin Koy Sien, Zhikuan Chen, Kok Haw Ong, Ging Meng Ng, Achmad Zen
  • Publication number: 20120295897
    Abstract: 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: Application
    Filed: July 25, 2012
    Publication date: November 22, 2012
    Applicant: 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
  • Publication number: 20120269864
    Abstract: The present invention is a compound of formula (I) or formula (II) which are suitable as NP-1 antagonists.
    Type: Application
    Filed: June 11, 2012
    Publication date: October 25, 2012
    Inventors: Haiyan Jia, Ian ZACHARY, Michelle TICKNER, Lili CHENG, Chris CHAPMAN, Katie ELLARD, Basil HARTZOULAKIS, Ashley JARVIS, Rosemary LYNCH, Jamie NALLY, David SELWOOD, Mark STEWART
  • Publication number: 20120252784
    Abstract: 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: Application
    Filed: March 13, 2012
    Publication date: October 4, 2012
    Inventors: 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
  • Publication number: 20120245208
    Abstract: 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: Application
    Filed: October 21, 2010
    Publication date: September 27, 2012
    Applicant: UCB PHARMA, S.A.
    Inventors: Yannick Quesnel, Laurent Turet, Joël Mercier
  • Publication number: 20120232071
    Abstract: 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: Application
    Filed: May 22, 2012
    Publication date: September 13, 2012
    Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
  • Publication number: 20120207729
    Abstract: 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: Application
    Filed: April 24, 2012
    Publication date: August 16, 2012
    Applicant: DECODE GENETICS EHF
    Inventors: Jasbir SINGH, Mark E. GURNEY, Alex BURGIN, Alexander KISELYOV, Munagala RAO
  • Publication number: 20120205596
    Abstract: 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: Application
    Filed: October 29, 2010
    Publication date: August 16, 2012
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Ken Yoshimura, Kenichiro Ohya
  • Publication number: 20120202781
    Abstract: 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: Application
    Filed: April 8, 2010
    Publication date: August 9, 2012
    Inventors: Kevin James Gillen, Jonathan Gillespie, Craig Jamieson, John Kinnaird Ferguson MacLean, Elizabeth Margaret Moir, Zoran Rankovic
  • Patent number: 8236964
    Abstract: 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: Grant
    Filed: March 25, 2008
    Date of Patent: August 7, 2012
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen
  • Publication number: 20120190098
    Abstract: 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: Application
    Filed: March 1, 2012
    Publication date: July 26, 2012
    Applicants: LELAND STANFORD JUNIOR UNIVERSITY, KENT STATE UNIVERSITY
    Inventors: ROBERT J. TWIEG, WILLIAM E. MOERNER, SAMUEL J. LORD, NA LIU, REICHEL SAMUEL
  • Patent number: 8217064
    Abstract: 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: Grant
    Filed: December 22, 2008
    Date of Patent: July 10, 2012
    Assignee: EnVivo Pharmaceuticals, Inc.
    Inventors: Gideon Shapiro, Richard Chesworth
  • Publication number: 20120152357
    Abstract: 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: Application
    Filed: December 14, 2011
    Publication date: June 21, 2012
    Inventors: Christopher T. BROWN, Elena E. Sheina, Ting Xu
  • Publication number: 20120142689
    Abstract: 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: Application
    Filed: December 1, 2011
    Publication date: June 7, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Eric L. STANGELAND, Lori Jean VAN ORDEN, Daisuke Roland SAITO
  • Patent number: 8193228
    Abstract: 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: Grant
    Filed: October 16, 2007
    Date of Patent: June 5, 2012
    Assignee: 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
  • Patent number: 8183275
    Abstract: 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: Grant
    Filed: October 16, 2007
    Date of Patent: May 22, 2012
    Assignees: 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
  • Publication number: 20120122862
    Abstract: The present invention is a compound of formula (I) or formula (II) which are suitable as NP-1 antagonists.
    Type: Application
    Filed: January 30, 2012
    Publication date: May 17, 2012
    Inventors: Haiyan Jia, Ian Zachary, Michelle Tickner, Lili Cheng, Chris Chapman, Katie Ellard, Basil Hartzoulakis, Ashley Jarvis, Rosemary Lynch, Jamie Nally, David Selwood, Mark Stewart
  • Publication number: 20120122937
    Abstract: Methods and pharmaceutical compositions for treating cancer utilizing compounds characterized by the following structure: and their pharmaceutically acceptable salts.
    Type: Application
    Filed: December 14, 2011
    Publication date: May 17, 2012
    Inventors: HSU-SHAN HUANG, TSUNG-CHIH CHEN, TAI-LUNG CHA
  • Publication number: 20120115841
    Abstract: 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: Application
    Filed: May 17, 2010
    Publication date: May 10, 2012
    Applicant: ACTELION PHARMACEUTICALS LTD.
    Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
  • Patent number: 8153446
    Abstract: 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: Grant
    Filed: May 13, 2009
    Date of Patent: April 10, 2012
    Assignees: Kent State University, Leland Stanford Junior University
    Inventors: Robert J. Twieg, William E. Moerner, Samuel J. Lord, Na Liu, Reichel Samuel
  • Patent number: 8133515
    Abstract: 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: Grant
    Filed: November 21, 2008
    Date of Patent: March 13, 2012
    Assignee: University of Georgia Research Foundation, Inc.
    Inventors: Geert-Jan Boons, Jun Guo, Xinghai Ning, Margaretha Wolfert
  • Publication number: 20120046255
    Abstract: The present invention relates to non-steroidal compounds useful in the treatment of inflammatory conditions and pharmaceutical compositions comprising them.
    Type: Application
    Filed: April 14, 2008
    Publication date: February 23, 2012
    Applicant: THE UNIVERSITY OF MELBOURNE of ROYAL PARADE PARKVILLE
    Inventors: Alastair Stewart, Martin Banwell, Brenda Leung, Anu Augustine, Jacki Kitching, Tomasz Bilski
  • Publication number: 20120040011
    Abstract: 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: Application
    Filed: November 21, 2008
    Publication date: February 16, 2012
    Applicant: University of Georgia Research Foundation, Inc.
    Inventors: Geert-Jan Boons, Jun Guo, Xinghai Ning, Margaretha Wolfert
  • Publication number: 20120035173
    Abstract: 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: Application
    Filed: September 6, 2011
    Publication date: February 9, 2012
    Inventors: Leslie Street, Rudolf Mueller, Steven Lee
  • Publication number: 20120021007
    Abstract: 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: Application
    Filed: January 15, 2010
    Publication date: January 26, 2012
    Inventors: Antonella Viola, Enzo Bronte, Marco Crosetti, Loretta Lazzarato, Roberta Fruttero, Alberto Gasco
  • Publication number: 20120015990
    Abstract: 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: Application
    Filed: June 17, 2011
    Publication date: January 19, 2012
    Applicant: THE WASHINGTON UNIVERSITY
    Inventors: James Hsieh, Emily Cheng
  • Publication number: 20120015989
    Abstract: 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: Application
    Filed: January 15, 2010
    Publication date: January 19, 2012
    Inventors: Steven J. Metallo, Edward V. Prochownik, Ariele Viacava Follis
  • Patent number: 8097730
    Abstract: 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: Grant
    Filed: October 15, 2009
    Date of Patent: January 17, 2012
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Xuqing Zhang, Zhihua Sui
  • Patent number: 8080569
    Abstract: 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: Grant
    Filed: May 15, 2009
    Date of Patent: December 20, 2011
    Assignee: Sanofi-Aventis
    Inventors: Gerhard Zoller, Hartmut Strobel, David William Will, Paulus Wohlfart
  • Publication number: 20110306542
    Abstract: 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: Application
    Filed: June 9, 2011
    Publication date: December 15, 2011
    Applicant: 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
  • Publication number: 20110306082
    Abstract: 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: Application
    Filed: December 29, 2009
    Publication date: December 15, 2011
    Applicant: LIFE TECHNOLOGIES CORPORATION
    Inventors: Kyle Gee, Vladimir Martin
  • Publication number: 20110288089
    Abstract: 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: Application
    Filed: January 13, 2010
    Publication date: November 24, 2011
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Peter Renold, Jerome Yves Cassayre, Jagadish Pabba, Myriem El Qacemi, Thomas Pitterna
  • Publication number: 20110281879
    Abstract: 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: Application
    Filed: January 12, 2011
    Publication date: November 17, 2011
    Applicant: ViroBay, Inc.
    Inventor: Craig Mossman
  • Publication number: 20110275680
    Abstract: 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: Application
    Filed: December 17, 2009
    Publication date: November 10, 2011
    Applicant: TROPHOS
    Inventors: Cyrille Drouot, Abdesslame Nazih, Corinne Chaimbault
  • Publication number: 20110274655
    Abstract: 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: Application
    Filed: May 5, 2011
    Publication date: November 10, 2011
    Applicant: Infinity Pharmaceuticals
    Inventors: Adilah BAHADOOR, Alfredo C. Castro, Lawrence K. Chan, Gregg F. Keaney, Marta Nevalainen, Vesa Nevalainen, Stephane Peluso, Daniel A. Snyder, Thomas T. Tibbitts
  • Publication number: 20110269960
    Abstract: 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: Application
    Filed: July 11, 2011
    Publication date: November 3, 2011
    Applicant: TAISHO PHARMACEUTICAL CO., LTD.
    Inventors: Naoya ONO, Tetsuo Takayama, Fumiyasu Shiozawa, Hironori Katakai, Tetsuya Yabuuchi, Tomomi Ota, Makoto Yagi, Masakazu Sato
  • Publication number: 20110269804
    Abstract: 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: Application
    Filed: July 24, 2009
    Publication date: November 3, 2011
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: 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