Acyclic Chalcogen Attached Directly To The Five-membered Nitrogen Containing Spiro Hetero Ring By Nonionic Bonding Patents (Class 548/410)
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Patent number: 8236963Abstract: The present invention is related to the use of spiro derivatives of Formula (I) for the treatment and/or prevention of allergic diseases, inflammatory dermatoses and other diseases with an inflammatory component. Specifically, the present invention is related to the use of spiro derivatives for the modulation of CRTH2 activity.Type: GrantFiled: May 23, 2006Date of Patent: August 7, 2012Assignee: Merck Serono SAInventors: Matthias Schwarz, Eric Sebille, Christophe Cleva, Cedric Merlot, Dennis Church, Patrick Page, Jacqueline A. Macritchie, John Frederick Atherall, Stefano Crosignani, Doris Pupowicz
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Publication number: 20120190865Abstract: The present invention relates to a novel process for the preparation of 1-H-pyrrolidine-2,4-dione derivatives and to novel intermediates and to a process for their preparation.Type: ApplicationFiled: January 25, 2012Publication date: July 26, 2012Applicant: Bayer CropScience AGInventors: Reiner FISCHER, Thomas HIMMLER
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Patent number: 8217044Abstract: There are provided compounds of the formula wherein X, Y and R1 to R8 are as described herein and the enantiomers and pharmaceutically acceptable salts and esters thereof which compounds have anticancer activity.Type: GrantFiled: March 28, 2011Date of Patent: July 10, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Xin-Jie Chu, Qingjie Ding, Nan Jiang, Jing Zhang, Zhuming Zhang
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Patent number: 8217052Abstract: The present disclosure relates to a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I): wherein R1, R2, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, methods of preparation of substituted N-phenyl-bipyrrolidine carboxamides and intermediates therefore are disclosed.Type: GrantFiled: June 2, 2011Date of Patent: July 10, 2012Assignee: SanofiInventors: Zhongli Gao, Ryan Hartung, David Stefany
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Publication number: 20120129833Abstract: The invention relates to 5?-biphenyl-substituted cyclic ketoenols for therapeutic purposes, to pharmaceutical compositions and to their use in therapy, in particular for the prophylaxis and therapy of diabetes, obesity, hyperlipidaemia, fatty livers and of disorders of the cardiovascular system.Type: ApplicationFiled: August 19, 2011Publication date: May 24, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Ningshu LIU, Kai Thede, Philip Lienau, Arne Scholz, Maher Najjar, Ulf Bomer, Knut Eis, Reiner Fischer
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Publication number: 20120122909Abstract: This invention is directed to spiro-oxindole compounds of formula (I): wherein k, j, Q, R1, R2a, R2b, R2c, R2d, R3a, R3b, R3c, and R3d are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. Pharmaceutical compositions comprising the compounds and methods of preparing and using the compounds are also disclosed.Type: ApplicationFiled: April 1, 2011Publication date: May 17, 2012Applicant: Xenon Pharmaceuticals Inc.Inventors: Mikhail Chafeev, Nagasree Chakka, Sultan Chowdhury, Robert Fraser, Jianmin Fu, Duanjie Hou, Tom Hsieh, Rajender Kamboj, Shifeng Liu, Vandna Ralna, Mehran Seid Bagherzadeh, Jianyu Sun, Shaoyi Sun, Serguei Sviridov
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Publication number: 20120122947Abstract: Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.Type: ApplicationFiled: November 11, 2011Publication date: May 17, 2012Applicants: THE REGENTS OF THE UNIVERSITY OF MICHIGAN, SANOFI, ASCENTA THERAPEUTICS, INC.Inventors: Shaomeng Wang, Yujun Zhao, Wei Sun, Sanjeev Kumar, Lance Leopold, Laurent Debussche, Cedric Barriere, Jean-Christophe Carry, Kwame Amaning
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Publication number: 20120101092Abstract: The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).Type: ApplicationFiled: December 23, 2011Publication date: April 26, 2012Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Shaomeng Wang, Ke Ding, Yipin Lu, Zaneta Nikolovska-Coleska, Su Qiu, Guoping Wang, Dongguang Qin, Sanjeev Kumar
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Patent number: 8153623Abstract: Compounds of formula (I), pharmaceutical compositions thereof, and methods for treatment using the same.Type: GrantFiled: August 4, 2010Date of Patent: April 10, 2012Assignee: Convergence Pharmaceuticals LimitedInventors: Giuseppe Alvaro, David Amantini, Markus Bergauer, Francesca Bonetti, Roberto Profeta
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Patent number: 8134017Abstract: A compound represented by the following formula (1) or (2):Type: GrantFiled: December 2, 2010Date of Patent: March 13, 2012Assignee: RikenInventors: Shinichiro Kamino, Shuichi Enomoto
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Publication number: 20120046306Abstract: There are provided compounds of the general formula wherein A, B, V, W, R1, R2, R3, R3, and R4, are as described herein and enantiomers and pharmaceutically acceptable salts thereof. The compounds are useful as anticancer agents.Type: ApplicationFiled: July 12, 2011Publication date: February 23, 2012Inventors: David Joseph Bartkovitz, Xin-Jie Chu, Qingjie Ding, Prabha Saba Karnachi, Jin-Jun Liu, Sung-Sau So, Jing Zhang, Zhuming Zhang
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Publication number: 20120035199Abstract: This invention is directed to spiroheterocyclic compounds of formula (I): wherein k, j, p, Q, R1, R3a, R3b, R3e, and R3d are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, that are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. Pharmaceutical compositions comprising the compounds and methods of using the compounds are also disclosed.Type: ApplicationFiled: August 12, 2010Publication date: February 9, 2012Applicant: Xenon Pharmaceuticals Inc.Inventors: Mikhail Chafeev, Sultan Chowdhury, Robert Fraser, Jianmin Fu, Rajender Kamboj, Shifeng Liu, Mehran Seid Bagherzadeh, Jianyu Sun, Serguei Sviridov
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Publication number: 20120029044Abstract: Muscarinic acetylcholine receptor antagonists and methods of using them for the treatment of muscarinic acetylcholine receptor-mediated diseases, such as pulmonary diseases, are provided.Type: ApplicationFiled: January 27, 2011Publication date: February 2, 2012Inventors: Jürg R. Pfister, Gwenaella Rescourio, Meenakshi S. Venkatraman, Xiaoming Zhang
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3-BIPHENYL-SUBSTITUTED-3-SUBSTITUTED-4-KETOLACTAM AND KETOLACTONE AND THEIR UTILIZATION AS PESTICIDE
Publication number: 20120028804Abstract: The present invention relates to novel 3-biphenyl-substituted, 3-substituted 4-ketolactams and -lactones of the formula (I) in which A, B, Q, G, W, X, Y and Z are as defined in the disclosure, to processes for their preparation, and to their use as pesticides and/or microbicides and/or herbicides.Type: ApplicationFiled: October 23, 2007Publication date: February 2, 2012Inventors: Reiner Fischer, Astrid Ullmann, Thomas Bretschneider, Mark Wilhelm Drewes, Christoph Erdelen, Angelika Lubos-Erdelen, Dieter Feucht, Udo Reckmann, Karl-Heinz Kuck, Ulrike Wachendorff-Neumann -
Patent number: 8101647Abstract: 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: GrantFiled: October 13, 2009Date of Patent: January 24, 2012Assignee: 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 Zenova
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Publication number: 20120015807Abstract: The present invention relates to novel trifluoromethoxyphenyl-substituted tetramic acid derivatives of the formula (I), in which J, X, Y, A, B, D and G have the meanings given above, to a number of processes for their preparation, and to their use as pesticides and/or herbicides. The invention further provides selective herbicidal compositions which comprise, firstly, trifluoromethoxyphenyl-substituted tetramic acid derivatives and, secondly, a crop plant compatibility-improving compound. The invention further relates to the boosting of the action of crop protection compositions comprising compounds of the formula (I) through the additions of ammonium salts or phosphonium salts and optionally penetrants.Type: ApplicationFiled: October 13, 2007Publication date: January 19, 2012Applicant: Bayer CropScience AGInventors: Reiner Fischer, Stefan Lehr, Christian Arnold, Thomas Auler, Jan Dittgen, Dieter Feucht, Eva-Maria Franken, Waltraud Hempel, Martin Jeffrey Hills, Heinz Kehne, Peter Losel, Olga Malsam, Christopher Hugh Rosinger, Erich Sanwald, Ulrich Gorgens, Stefan Antons, Wolfgang Ebenbeck, Axel Pleschke, Marielouise Schneider, Ralf Wischnat
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Patent number: 8088815Abstract: There are provided compounds of the formula wherein X, Y and R1 to R8 are described herein along with the enantiomers, pharmaceutically acceptable salts and esters thereof. The compounds are useful as anticancer agents.Type: GrantFiled: November 4, 2010Date of Patent: January 3, 2012Assignee: Hoffman-La Roche Inc.Inventors: David Joseph Bartkovitz, Xin-Jie Chu, Qingjie Ding, Bradford James Graves, Nan Jiang, Jing Zhang, Zhuming Zhang
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Publication number: 20110306499Abstract: The invention relates to novel compounds of the formula (I) in which W, X, Y, Z and CKE have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides, and also to selective herbicidal compositions comprising, firstly, the compounds of the formula (I) and, secondly, at least one crop plant compatibility-improving compound. The invention further relates to the boosting of the action of crop protection compositions comprising compounds of the formula (I) through the additions of ammonium salts or phosphonium salts and optionally penetrants.Type: ApplicationFiled: November 22, 2007Publication date: December 15, 2011Applicant: Bayer CropScience AGInventors: Thomas Bretschneider, Reiner Fischer, Rolf Pontzen, Christian Arnold, Ulrich Görgens, Olga Malsam, Udo Reckmann, Erich Sanwald, Stefan Lehr, Jan Dittgen, Dieter Feucht, Martin Hills, Christopher Rosinger
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Publication number: 20110295009Abstract: The invention relates to streptospirole derivatives of the general formula (I), wherein R1, R2, R3, X1, X2, Y1 and Y2 are as defined herein, a process for the preparation of said compounds by fermenting the microorganism Streptomyces sp. ST 108140 (DSM 19369) and optionally derivatizing the compounds produced by said microorganism, a pharmaceutical composition comprising at least one compound of the formula (I), and the use of a compound of the formula (I) for the preparation of a medicament for the treatment and/or prophylaxis of bacterial infections.Type: ApplicationFiled: July 16, 2009Publication date: December 1, 2011Applicant: SANOFI-AVENTISInventors: Cosima Dufour-Schroif, Joachim Wink, Martin Gerlitz, Helene Olivan, Michael Kurz
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Publication number: 20110294783Abstract: The present invention concerns boosting the activity of crop protection materials comprising inhibitors of fatty acid biosynthesis (for example phenyl-substituted cyclic ketoenols) through the addition of ammonium salts and/or phosphonium salts or through the addition of ammonium salts and/or phosphonium salts and penetrants, the corresponding materials, processes for preparing them, and their use in crop protection.Type: ApplicationFiled: August 10, 2011Publication date: December 1, 2011Applicant: BAYER CROPSCIENCE AGInventors: Reiner FISCHER, Stefan LEHR, Peter MARCZOK, Udo Reckmann, Christian Arnold, Waltraud Hempel, Erich SANWALD, Rolf Pontzen
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Patent number: 8058288Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.Type: GrantFiled: June 17, 2010Date of Patent: November 15, 2011Assignee: Incyte CorporationInventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Colin Zhang, Brian W. Metcalf, Chunhong He, Ding-Quan Qian
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Publication number: 20110275161Abstract: The teachings provided herein are directed to compounds and methods for detecting nerve agents using rhodamine-derived detection compounds. A rhodamine-derived detection compound for nerve agents can include any rhodamine derivative that can bind to a nerve agent and produce a detectable signal for detection of the nerve agent. In some embodiments, the rhodamine-derived detection compound comprises rhodamine B-hydroxamate and the nerve agent can be detected in amounts as low as about 10 ppm.Type: ApplicationFiled: May 5, 2010Publication date: November 10, 2011Applicant: MCLABInventors: SHOUFA HAN, Changping Shi
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Publication number: 20110269809Abstract: There are provided compounds of the formula wherein X, Y and R1 to R8 are as described herein and the enantiomers and pharmaceutically acceptable salts and esters thereof which compounds have anticancer activity.Type: ApplicationFiled: March 28, 2011Publication date: November 3, 2011Inventors: Xin-Jie Chu, Qingjie Ding, Nan Jiang, Jing Zhang, Zhuming Zhang
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Publication number: 20110251225Abstract: The present disclosure relates to a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I): wherein R1, R2, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, methods of preparation of substituted N-phenyl-bipyrrolidine carboxamides and intermediates therefore are disclosed.Type: ApplicationFiled: June 2, 2011Publication date: October 13, 2011Applicant: SANOFIInventors: Zhongli GAO, Ryan HARTUNG, David STEFANY
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Publication number: 20110251224Abstract: This invention is directed to spiro-oxindole compounds of formula (I): wherein k, j, Q, R1, R2a, R2b, R2c, R2d, R3a, R3b, R3c, and R3d are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. Pharmaceutical compositions comprising the compounds and methods of preparing and using the compounds are also disclosed.Type: ApplicationFiled: April 1, 2011Publication date: October 13, 2011Inventors: Mikhail Chafeev, Nagasree Chakka, Sultan Chowdhury, Robert Fraser, Jianmin Fu, Duanjie Hou, Tom Hsieh, Rajender Kamboj, Shifeng Liu, Vandna Ralna, Mehran Seid Bagherzadeh, Jianyu Sun, Shaoyi Sun, Serguei Sviridov
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Publication number: 20110230346Abstract: The invention relates to novel compounds of the formula (I) in which W, X, Y, Z, and CKE have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides and/or fungicides. Moreover, the invention relates to selectively herbicidal compositions comprising, firstly, the biphenyl-substituted cyclic ketoenols and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to the boosting of the action of crop protection compositions comprising in particular biphenyl-substituted cyclic ketoenols through the addition of ammonium or phosphium salts and optionally penetrants, to the corresponding compositions, to processes for their preparation and to their use in crop protection as insecticides and/or nematicides and/or acaricides and/or fungicides and/or for preventing unwanted plant growth.Type: ApplicationFiled: February 10, 2011Publication date: September 22, 2011Applicant: Bayer CropScience AGInventors: Reiner FISCHER, Stefan Lehr, Isolde Häuser-Hahn, Christopher Hugh Rosinger, Chieko Ueno, Arnd Voerste, Elmar Gatzweiler, Ines Heinemann, Ulrich Görgens
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Publication number: 20110213160Abstract: The invention relates to novel 2,4,6-phenyl-substituted cyclic ketoenols of the formula (I), in which CKE, W, X and Y are as defined above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides, and also to selective herbicidal compositions comprising firstly the 2,4,6-phenyl-substituted cyclic ketoenols and secondly at least one compound which improves crop plant tolerance.Type: ApplicationFiled: April 15, 2011Publication date: September 1, 2011Applicant: BAYER CROPSCIENCE AGInventors: Thomas BRETSCHNEIDER, Reiner Fischer, Oliver Gaertzen, Klaus Kunz, Stefan Lehr, Dieter Feucht, Peter Lösel, Olga Malsam, Guido Bojack, Christian Arnold, Thomas Auler, Jeffrey Martin Hills, Heinz Kehne, Chris Rosinger
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Publication number: 20110207941Abstract: The invention relates in a first embodiment to a method for the manufacture of esters of the formula I, or especially of amides of the formula II, wherein the symbols have the meanings given in the specification, as well as other intermediates and compounds useful in the synthesis of tryptamines and other substances mentioned in the title. The synthesis methods and intermediates are useful in the synthesis of pharmaceuticals.Type: ApplicationFiled: May 2, 2011Publication date: August 25, 2011Inventors: ULRICH BERENS, OLIVER DOSENBACH, DANIEL SPRENGER
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Publication number: 20110201635Abstract: There is provided a compound of the formula wherein X, Y, W, R1, R2 and R3 are as described herein. The compounds have activity as anticancer agents.Type: ApplicationFiled: January 19, 2011Publication date: August 18, 2011Inventors: Jin-Jun Liu, Jing Zhang, Zhuming Zhang
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Patent number: 7998959Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1 and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 such as obesity and diabetes.Type: GrantFiled: January 11, 2007Date of Patent: August 16, 2011Assignee: Incyte CorporationInventors: Wenqing Yao, David M. Burns, Lihua Chen, Jincong Zhuo, Chunhong He
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Publication number: 20110195024Abstract: Isatin 5-sulfonamide derivatives, pharmaceutical compositions comprising the derivatives, their use as molecular imaging agents, their use for the diagnosis or treatment of diseases or disorders associated with dysregulation of apoptosis, methods for synthesizing the derivatives, methods for the molecular imaging of caspase activity and apoptosis, and methods of assessing the therapeutic effect of a test substance on caspase activity are disclosed.Type: ApplicationFiled: September 4, 2009Publication date: August 11, 2011Applicants: Imperial Innovations Limited, Hammersmith Imanet LimitedInventors: Eric Ofori Aboabye, Graham Smith, Quang-De Nguyen, Erik Arstad, Matthias Eberhard Glaser
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Publication number: 20110190493Abstract: The invention relates to novel spiroketal-substituted cyclic ketoenols of the formula (I) in which A, B, Q1, Q2, D, G, W, X, Y, and Z are as defined above, to processes and intermediates for their preparation and to their use as pesticides and/or microbicides and/or herbicides. Moreover, the invention relates to selective herbicidal compositions comprising, firstly, spiroketal-substituted cyclic ketoenols and, secondly, a crop plant compatibility-improving compound.Type: ApplicationFiled: February 25, 2011Publication date: August 4, 2011Applicant: Bayer CropScience AGInventors: Thomas Bretschneider, Reiner Fischer, Oliver Gaertzen, Stefan Lehr, Mark Wilhelm Drewes, Dieter Feucht, Olga Malsam, Udo Reckmann, Christian Arnold, Thomas Auler, Waltraud Hempel, Martin Jeffrey Hills, Heinz Kehne, Christopher Hugh Rosinger, Erich Sanwald
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Publication number: 20110166297Abstract: Molecularly imprinted smart polymers (MISPs) are provided herein, as well as novel monomers for preparing MISPs, and processes for preparing MISPs. The MISPs can be used applications such as, for example, detecting/absorbing or isolating biological and non-biological agents. The MISPs described herein comprise responsive monomeric units which undergo a physico-chemical change (e.g., a bond formation or cleavage) in response to an external change, such that the MISP selectively binds to a target molecule and releases a bound target molecule in response to the external change.Type: ApplicationFiled: September 9, 2009Publication date: July 7, 2011Applicant: Sailo Nanotechnologies Ltd.Inventors: Flavio Grynszpan, Eran Partouche, Vladimir Shkoulev, Alex Aizikovich, Sharon Gazal, Rachel Nakash-Ozeri, Isaac Zigelboim
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Publication number: 20110143943Abstract: The present invention relates to novel C2-phenyl-substituted cyclic ketoenols of the formula (I) in which W, X, Y, Z and CKE are as defined in the description, to processes for their preparation and to their use as pesticides and herbicides.Type: ApplicationFiled: February 17, 2011Publication date: June 16, 2011Applicant: Bayer AktiengesellschaftInventors: Michael RUTHER, Hermann Hagemann, Udo Schneider, Markus Dollinger, Peter Dahmen, Ulrike Wachendorff-Neumann, Reiner Fischer, Alan Graff, Thomas Bretschneider, Christoph Erdelen, Mark Wilhelm Drewes, Dieter Feucht, Folker Lieb
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Publication number: 20110130398Abstract: There are provided compounds of the formula wherein X, Y and R1 to R8 are described herein along with the enantiomers, pharmaceutically acceptable salts and esters thereof. The compounds are useful as anticancer agents.Type: ApplicationFiled: November 4, 2010Publication date: June 2, 2011Inventors: David Joseph Bartkovitz, Xin-Jie Chu, Qingjie Ding, Bradford James Graves, Nan Jiang, Jing Zhang, Zhuming Zhang
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Publication number: 20110112052Abstract: Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.Type: ApplicationFiled: November 12, 2010Publication date: May 12, 2011Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Shaomeng Wang, Shanghai Yu, Wei Sun, Sanjeev Kumar Shangary, Duxin Sun, Peng Zou, Donna McEachern, Yujun Zhao
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Publication number: 20110112162Abstract: 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: October 13, 2009Publication date: May 12, 2011Applicant: 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 Zenova
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Publication number: 20110087027Abstract: This invention is directed to methods of preparing certain spiro-oxindole derivatives, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.Type: ApplicationFiled: October 14, 2010Publication date: April 14, 2011Applicant: XENON PHARMACEUTICALS INC.Inventors: Jean-Jacques Cadieux, Mikhail Chafeev, Sultan Chowdhury, Jianmin Fu, Qi Jia, Stefanie Abel, Emad El-Sayed, Elke Huthmann, Thomas Isarno
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Patent number: 7897787Abstract: A compound represented by the following general formula (I): [wherein R1 and R2 independently represent hydrogen atom, or a group represented by the following formula (A): (wherein X1 and X2 represent hydrogen atom, an alkyl group, an alkoxy group, or a halogen atom), provided that R1 and R2 do not simultaneously represent hydrogen atom; R3 and R6 represent an alkyl group; R4 and R7 represent hydrogen atom, an alkyl group, carboxy group, an alkoxycarbonyl group, or sulfo group; and R5 and R8 represents an alkyl group, an aryl group, an alkoxycarbonyl group, a vinyl group, a thienyl group, or a pyrrolyl group], or a salt thereof, which is usable for efficient screening for a chemical substance having applicability as a catalyst of the reaction of Michael addition.Type: GrantFiled: September 13, 2006Date of Patent: March 1, 2011Assignee: The University of TokyoInventors: Takuya Matsumoto, Takuji Shoda, Yasuteru Urano, Tetsuo Nagano
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Publication number: 20110034500Abstract: This invention is directed to spiroheterocyclic compounds of formula (I): wherein k, j, p, Q, R1, R3a, R3b, R3e, and R3d are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, that are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. Pharmaceutical compositions comprising the compounds and methods of using the compounds are also disclosed.Type: ApplicationFiled: August 12, 2010Publication date: February 10, 2011Applicant: Xenon Pharmaceuticals Inc.Inventors: Mikhail Chafeev, Sultan Chowdhury, Robert Fraser, Jianmin Fu, Rajender Kamboj, Shifeng Liu, Mehran Seid Bagherzadeh, Jianyu Sun, Serguei Sviridov
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Publication number: 20100331386Abstract: This invention is directed to the (S)-enantiomer of the compound of formula (I): or a pharmaceutically acceptable solvate or prodrug thereof. This (S)-enantiomer is useful for the treatment of diseases or conditions, such as pain, which are ameliorated or alleviated by the modulation of voltage-gated sodium channels.Type: ApplicationFiled: June 28, 2010Publication date: December 30, 2010Applicant: XENON PHARMACEUTICALS INC.Inventors: Mikhail Chafeev, Jianmin Fu, Jean-Jacques Cadieux
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Publication number: 20100324022Abstract: Compounds of formula (I), pharmaceutical compositions thereof, and methods for treatment using the same.Type: ApplicationFiled: August 4, 2010Publication date: December 23, 2010Applicant: GLAXO GROUP LIMITEDInventors: Giuseppe Alvaro, David Amantini, Markus Bergauer, Francesca Bonetti, Roberto Profeta
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Publication number: 20100317661Abstract: The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).Type: ApplicationFiled: June 14, 2010Publication date: December 16, 2010Applicant: The Regents of the University of MichiganInventors: Shaomeng Wang, Dongguang Qin, Jianyong Chen, Shanghai Yu
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Publication number: 20100272681Abstract: The present invention relates to compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention.Type: ApplicationFiled: February 20, 2008Publication date: October 28, 2010Applicant: Vertex Pharmaceuticals IncorporatedInventors: Luc Farmer, Randy Scott Bethiel, Dylan Jacobs, Robert B. Perni, John Maxwell, Kevin Cottrell, Summer Halas
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Publication number: 20100273799Abstract: The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).Type: ApplicationFiled: June 24, 2010Publication date: October 28, 2010Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Shaomeng Wang, Ke Ding, Yipin Lu, Zaneta Nikolovska-Coleska, Su Qiu, Guoping Wang, Dongguang Qin, Sanjeev Kumar
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Patent number: 7759383Abstract: The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).Type: GrantFiled: February 22, 2006Date of Patent: July 20, 2010Assignee: The Regents of the University of MichiganInventors: Shaomeng Wang, Ke Ding, Yipin Lu, Zaneta Nikolovska-Coleska, Su Qiu, Guoping Wang, Dongguang Qin, Sanjeev Kumar
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Publication number: 20100137299Abstract: 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: October 13, 2009Publication date: June 3, 2010Applicant: 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 Zenova, Qi Jia, Jean-Jacques Cadieux, Simon J. Gauthier, Amy Frances Douglas, Tom Hsieh, Nagasree Chakka, Zoran Cikojevic
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Publication number: 20100130487Abstract: This invention is directed to spiro-oxindole compounds of formula (I): wherein k, j, Q, R1, R2a, R2b, R2c, R2d, R3a, R3b, R3c, and R3d are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. Pharmaceutical compositions comprising the compounds and methods of preparing and using the compounds are also disclosed.Type: ApplicationFiled: December 30, 2009Publication date: May 27, 2010Applicant: XENON PHARMACEUTICALS INC.Inventors: Mikhail Chafeev, Nagasree Chakka, Sultan Chowdhury, Robert Fraser, Jianmin Fu, Duanjie Hou, Tom Hsieh, Rajender Kamboj, Shifeng Liu, Vandna Raina, Mehran Seid Bagherzadeh, Jianyu Sun, Shaoyi Sun, Serguei Sviridov
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Publication number: 20100125072Abstract: This invention is directed to spiro-oxindole compounds of formula (I): wherein k, j, Q, R1, R2a, R2b, R2c, R2d, R3a, R3b, R3c, and R3d are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. Pharmaceutical compositions comprising the compounds and methods of preparing and using the compounds are also disclosed.Type: ApplicationFiled: December 30, 2009Publication date: May 20, 2010Applicant: XENON PHARMACEUTICALS INC.Inventors: Mikhail Chafeev, Nagasree Chakka, Sultan Chowdhury, Robert Fraser, Jianmin Fu, Duanjie Hou, Tom Hsieh, Rajender Kamboj, Shifeng Liu, Vandna Raina, Mehran Seid Bagherzadeh, Jianyu Sun, Shaoyi Sun, Serguei Sviridov
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Publication number: 20100099728Abstract: 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: October 13, 2009Publication date: April 22, 2010Applicant: 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 Zenova