Acyclic Chalcogen Attached Directly To The Five-membered Nitrogen Containing Spiro Hetero Ring By Nonionic Bonding Patents (Class 548/410)
  • Patent number: 10138251
    Abstract: The present invention encompasses compounds of formula (I) wherein the groups R1 to R7, V, W, X, Y, n and q are defined herein, their use as inhibitors of MDM2-p53 interaction, pharmaceutical compositions which contain compounds of this kind, their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases and synthetic intermediates.
    Type: Grant
    Filed: April 10, 2015
    Date of Patent: November 27, 2018
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Andreas Gollner, Christiane Kofink, Juergen Ramharter, Harald Weinstabl, Tobias Wunberg
  • Patent number: 10100060
    Abstract: This invention is directed to asymmetric synthesis of funapide, which is useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.
    Type: Grant
    Filed: June 16, 2017
    Date of Patent: October 16, 2018
    Assignee: Xenon Pharmaceuticals Inc.
    Inventors: Ronen Ben-David, Jian Chen, Michael A. Christie, Mina Gadelrab Dimitri, Graciela Noemi Gershon, Linli He, Nelson G. Landmesser, Daniel V. Levy, Orel Yosef Mizrahi, Partha S. Mudipalli, Harlan F. Reese, Joseph A. Sclafani, Yi Wang
  • Patent number: 10072020
    Abstract: An isatin spiro compound having the following formula (I): R1 is halogen or C1-3 alkyl; R2 is C1-3 alkyl or benzyl; and R3 and R3? are independently H, C1-3 alkyl or phenyl.
    Type: Grant
    Filed: April 19, 2018
    Date of Patent: September 11, 2018
    Assignee: SHAANXI UNIVERSITY OF SCIENCE AND TECHNOLOGY
    Inventors: Chengyuan Liang, Danni Tian, Shunjun Ding
  • Patent number: 9260446
    Abstract: 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: Grant
    Filed: May 7, 2014
    Date of Patent: February 16, 2016
    Assignee: Xenon Pharmaceuticals Inc.
    Inventors: Jean-Jacques Alexandre Cadieux, Mikhail Chafeev, Sultan Chowdhury, Jianmin Fu, Qi Ji, Stefanie Abel, Emad El-Sayed, Elke Huthmann, Thomas Isarno
  • Patent number: 9000189
    Abstract: 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: Grant
    Filed: November 22, 2007
    Date of Patent: April 7, 2015
    Assignee: Bayer CropScience AG
    Inventors: 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
  • Patent number: 8962339
    Abstract: The present invention discloses a fluorescent probe compound which solved the problem of fluorescence quenching by Pd2+, and its preparation method and use as well. Excitation and emission wavelengths of the probe compound are in visible light region. The probe compound is highly sensitive and displays good selectivity for Pd2+ in near-neutral pH range. In detection of Pd2+ in 0-10 ppb level, fluorescence is evidently enhanced, and Pd2+ in the level as low as 5 nM can be detected. Fluorescence intensity is well linearly correlated to Pd2+ concentration. The probe compound can be used for detection of contaminating palladium and residual palladium in drug, soil, water sample and reactor.
    Type: Grant
    Filed: December 6, 2010
    Date of Patent: February 24, 2015
    Assignees: Dalian University of Technology, Dalian Chromas Bioscience Co., Ltd.
    Inventors: Xiaojun Peng, Jiangli Fan, Honglin Li, Jingyun Wang, Shiguo Sun
  • Publication number: 20150025121
    Abstract: 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: Application
    Filed: October 9, 2014
    Publication date: January 22, 2015
    Inventors: Mikhail Chafeev, Jianmin Fu, Jean-Jacques Alexandre Cadieux
  • Publication number: 20140378680
    Abstract: 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: Application
    Filed: September 12, 2014
    Publication date: December 25, 2014
    Inventors: Shaomeng Wang, Shanghai Yu, Wei Sun, SanJeev Kumar, Duxin Sun, Peng Zou, Donna McEachern, Yujun Zhao
  • Publication number: 20140371468
    Abstract: 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: Application
    Filed: August 29, 2014
    Publication date: December 18, 2014
    Inventors: Reiner FISCHER, Thomas HIMMLER
  • Publication number: 20140357655
    Abstract: Spiroindoline derivatives, process for their preparation and pharmaceutical compositions thereof, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially sex-hormone-related diseases in both men and women, in particularly those selected from the group of endometriosis, uterine fibroids, polycystic ovarian disease, hirsutism, precocious puberty, gonadal steroid-dependent neoplasia such as cancers of the prostate, breast and ovary, gonadotrope pituitary adenomas, sleep apnea, irritable bowel syndrome, premenstrual syndrome, benign prostatic hypertrophy, contraception and infertility (e.g., assisted reproductive therapy such as in vitro fertilization). The present application relates in particular to spiroindoline derivatives as gonadotropin-releasing hormone (GnRH) receptor antagonists.
    Type: Application
    Filed: January 15, 2013
    Publication date: December 4, 2014
    Inventors: Olaf Panknin, Stefan Bäurle, Sven Ring, Wolfgang Schwede, Wilhelm Bone, Katrin Nowak-Reppel, Eckhard Bender, Reinhard Nubbemeyer, Mark Jean Gnoth
  • Publication number: 20140336390
    Abstract: 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: Application
    Filed: May 7, 2014
    Publication date: November 13, 2014
    Applicant: Xenon Pharmaceuticals Inc.
    Inventors: Jean-Jacques Alexandre Cadieux, Mikhail Chafeev, Sultan Chowdhury, Jianmin Fu, Qi Ji, Stefanie Abel, Emad El-Sayed, Elke Huthmann, Thomas Isarno
  • Publication number: 20140275005
    Abstract: The present disclosure relates to a series of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and formula (Ib). wherein R1, R2, R3, R4, X, m, l, n, p and s 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, this disclosure relates to methods of preparation of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and (Ib), and intermediates therefor.
    Type: Application
    Filed: May 5, 2014
    Publication date: September 18, 2014
    Applicant: Sanofi
    Inventor: Zhongli GAO
  • Patent number: 8742121
    Abstract: 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: Grant
    Filed: September 13, 2012
    Date of Patent: June 3, 2014
    Assignee: The Regents of the University of Michigan
    Inventors: Shaomeng Wang, Ke Ding, Guoping Wang
  • Publication number: 20140148494
    Abstract: 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: Application
    Filed: January 31, 2014
    Publication date: May 29, 2014
    Applicants: The Regents of the University of Michigan, Sanofi, Ascenta Licensing Corporation
    Inventors: Shaomeng Wang, Yujun Zhao, Wei Sun, Sanjeev Kumar, Lance Leopold, Laurent Debussche, Cedric Barriere, Jean-Christophe Carry, Kwame Amaning
  • Patent number: 8722578
    Abstract: Herbicidal compositions containing as active ingredients spiroheterocyclic pyrrolidine dione compounds.
    Type: Grant
    Filed: October 28, 2009
    Date of Patent: May 13, 2014
    Assignee: Syngenta Participations AG
    Inventors: Werner Zambach, Ottmar Franz Hueter, Jean Wenger, Marcela Goeghova, Thomas Pitterna, Peter Maienfisch, Stephane André´Marie Jeanmart, Michel Muehlebach
  • Publication number: 20140121196
    Abstract: A compound that inhibits interaction between, murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity is provided. The present invention provides a dispiropyrrolidine derivative represented by the following formula (1), which has various substituents, inhibits interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity, wherein R1, R2, R3, ring A, and ring B in formula (1) respectively have the same meanings as defined in the specification.
    Type: Application
    Filed: November 14, 2013
    Publication date: May 1, 2014
    Applicant: Daiichi Sankyo Company, Limited
    Inventors: Yuuichi Sugimoto, Kouichi Uoto, Takanori Wakabayashi, Masaki Miyazaki, Masaki Setoguchi, Toru Taniguchi, Keisuke Yoshida, Akitake Yamaguchi, Shoko Yoshida
  • Patent number: 8703165
    Abstract: Compounds of the formula (I) wherein the substituents are as defined in claim 1, are useful as pesticides.
    Type: Grant
    Filed: November 30, 2010
    Date of Patent: April 22, 2014
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Thomas Pitterna, Michel Muehlebach, Jurgen Harry Schaetzer
  • Patent number: 8633238
    Abstract: The present invention provides novel lactams extracted from an alcohol extract of dehulled adlay seeds. The present invention also provides a process for the preparation of the lactams and a method for treating breast cancer in a subject, which method comprises administering to said subject an effective amount of the lactam and a pharmaceutically acceptable carrier or excipient.
    Type: Grant
    Filed: February 1, 2012
    Date of Patent: January 21, 2014
    Assignee: Joben Bio-Medical Co., Ltd.
    Inventors: Wenchang Chiang, Yueh-Hsiung Kuo, Yun-Lian Lin, Cheng-Pei Chung
  • Patent number: 8629084
    Abstract: The invention relates to novel iodophenyl-substituted cyclic ketenols of the formula (I) in which CKE, J, 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 iodophenyl-substituted cyclic ketonols of the formula (I) and secondly at least one crop plant compatibility-improving compound.
    Type: Grant
    Filed: September 13, 2005
    Date of Patent: January 14, 2014
    Assignee: Bayer CropScience AG
    Inventors: Reiner Fischer, Thomas Bretschneider, Kerstin Ilg, Stefan Lehr, Dieter Feucht, Olga Malsam, Udo Reckmann, Guido Bojack, Christian Arnold, Thomas Auler, Martin Jeffrey Hills, Heinz Kehne, Waltraud Hempel, Erich Sanwald
  • Patent number: 8629133
    Abstract: A compound that inhibits interaction between murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity is provided. The present invention provides a dispiropyrrolidine derivative represented by the following formula (1), which has various substituents, inhibits interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity, wherein R1, R2, R3, ring A, and ring B in formula (1) respectively have the same meanings as defined in the specification.
    Type: Grant
    Filed: March 9, 2012
    Date of Patent: January 14, 2014
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Yuuichi Sugimoto, Kouichi Uoto, Takanori Wakabayashi, Masaki Miyazaki, Masaki Setoguchi, Toru Taniguchi, Keisuke Yoshida, Akitake Yamaguchi, Shoko Yoshida
  • Publication number: 20130331369
    Abstract: The invention relates to derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of a disorder or a disease mediated by the ghrelin receptor.
    Type: Application
    Filed: August 8, 2013
    Publication date: December 12, 2013
    Applicant: Novartis AG
    Inventors: Ameet Vijay Ambarkhane, Gurdip Bhalay, Martin Beckett, James Dale, Ahmed Hamadi, Alessandro Mazzacani, Jeffrey McKenna, Christopher Thomson
  • Publication number: 20130296303
    Abstract: 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: Application
    Filed: July 17, 2013
    Publication date: November 7, 2013
    Inventors: Shaomeng Wang, Shanghai Yu, Wei Sun, Sanjeev Kumar, Duxin Sun, Peng Zou, Donna McEachern, Yujun Zhao
  • Patent number: 8575208
    Abstract: 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: Grant
    Filed: February 20, 2008
    Date of Patent: November 5, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Luc Farmer, Randy Scott Bethiel, Dylan Jacobs, Robert B. Perni, John Maxwell, Kevin Cottrell, Summer Halas
  • Publication number: 20130274483
    Abstract: This invention is directed to asymmetric syntheses of certain spiro-oxindole derivatives, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.
    Type: Application
    Filed: March 11, 2013
    Publication date: October 17, 2013
    Inventors: Shaoyi Sun, Jianmin Fu, Sultan Chowdhury, Ivan William Hemeon, Michael Edward Grimwood, Tarek Suhayl Mansour
  • Patent number: 8551982
    Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.
    Type: Grant
    Filed: March 13, 2012
    Date of Patent: October 8, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Asitha Abeywardane, Michael J. Burke, Thomas Martin Kirrane, Matthew Russell Netherton, Anil Kumar Padyana, Lana Louise Smith Keenan, Hidenori Takahashi, Michael Robert Turner, Qiang Zhang, Qing Zhang
  • Publication number: 20130252962
    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: March 6, 2013
    Publication date: September 26, 2013
    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 Alexandre CADIEUX, Simon J. GAUTHIER, Amy Frances DOUGLAS, Tom HSIEH, Nagasree CHAKKA, Zoran CIKOJEVIC
  • Patent number: 8541343
    Abstract: Compounds of the formula (I), wherein the substituents are as defined in claim 1, are useful as a pesticides.
    Type: Grant
    Filed: November 29, 2010
    Date of Patent: September 24, 2013
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Thomas Pitterna, Michel Muehlebach, Jurgen Harry Schaetzer
  • Publication number: 20130197050
    Abstract: The present invention provides novel lactams extracted from an alcohol extract of dehulled adlay seeds. The present invention also provides a process for the preparation of the lactams and a method for treating breast cancer in a subject, which method comprises administering to said subject an effective amount of the lactam and a pharmaceutically acceptable carrier or excipient.
    Type: Application
    Filed: February 1, 2012
    Publication date: August 1, 2013
    Inventors: WENCHANG CHIANG, YUEH-HSIUNG KUO, YUN-LIAN LIN, CHENG-PEI CHUNG
  • Publication number: 20130196973
    Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.
    Type: Application
    Filed: March 13, 2012
    Publication date: August 1, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Asitha Abeywardane, Michael J. Burke, Thomas Martin Kirrane, Matthew Russell Netherton, Anil Kumar Padyana, Lana Louise Smith Keenan, Hidenori Takahashi, Michael Robert Turner, Qiang Zhang, Qing Zhang
  • Publication number: 20130165424
    Abstract: A compound that inhibits interaction between murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity is provided. The present invention provides a dispiropyrrolidine derivative represented by the following formula (1), which has various substituents, inhibits interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity, wherein R1, R2, R3, ring A, and ring B in formula (1) respectively have the same meanings as defined in the specification.
    Type: Application
    Filed: March 9, 2012
    Publication date: June 27, 2013
    Inventors: Yuuichi Sugimoto, Kouichi Uoto, Takanori Wakabayashi, Masaki Miyazaki, Masaki Setoguchi, Toru Taniguchi, Keisuke Yoshida, Akitake Yamaguchi, Shoko Yoshida
  • Publication number: 20130137879
    Abstract: A fluorescence probe compound, its preparation method and use are provided.
    Type: Application
    Filed: December 3, 2010
    Publication date: May 30, 2013
    Applicants: DALIAN CHRPMAS BIOSCIENCE CO., LTD., DALIAN UNIVERSITY OF TECHNOLOGY
    Inventors: Xiaojun Peng, Jiangli Fan, Jianjun Du, Jingyun Wang, Jianzhou Zhang, Shiguo Sun
  • Patent number: 8450358
    Abstract: 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: Grant
    Filed: June 28, 2010
    Date of Patent: May 28, 2013
    Assignee: Xenon Pharmaceuticals Inc.
    Inventors: Mikhail Chafeev, Jianmin Fu, Jean-Jacques Cadieux
  • Patent number: 8445696
    Abstract: 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: Grant
    Filed: October 14, 2010
    Date of Patent: May 21, 2013
    Assignee: Xenon Pharmaceuticals Inc.
    Inventors: Jean-Jacques Cadieux, Mikhail Chafeev, Sultan Chowdhury, Jianmin Fu, Qi Jia, Stefanie Abel, Emad El-Sayed, Elke Huthmann, Thomas Isarno
  • Patent number: 8431407
    Abstract: Temperature and/or irradiation and/or polymerization indicators comprise at least one 1,3-dipole and at least one dipolarophile, the dipole preferably being an ylide from the group of azomethines (sydnones), azomethinylides (munchnones), carbonylylides (isomunchnones), thiocarbonylylides (thioisomunchnones), or 1,3-dithiolylium-4-olates.
    Type: Grant
    Filed: May 26, 2006
    Date of Patent: April 30, 2013
    Assignee: Heraeus Kulzer GmbH
    Inventor: Andreas Grundler
  • Publication number: 20130072537
    Abstract: 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: Application
    Filed: September 14, 2012
    Publication date: March 21, 2013
    Applicant: XENON PHARMACEUTICALS INC.
    Inventors: Mikhail Chafeev, Jianmin Fu, Jean-Jacques Cadieux
  • Patent number: 8383814
    Abstract: 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: Grant
    Filed: May 30, 2012
    Date of Patent: February 26, 2013
    Assignee: Sanofi
    Inventors: Zhongli Gao, Ryan Hartung, David Stefany
  • Publication number: 20130040935
    Abstract: 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 tumour disorders.
    Type: Application
    Filed: February 8, 2011
    Publication date: February 14, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Ningshu Liu, Kai Thede, Philip Lienau, Arne Scholz, Christoph-Stephan Hilger, Ulf Bömer, Maher Najjar, Knut Eis, Reiner Fischer, Wahed Ahmed Moradi
  • Publication number: 20130030173
    Abstract: 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: Application
    Filed: September 13, 2012
    Publication date: January 31, 2013
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Shaomeng Wang, Ke Ding, Guoping Wang
  • Patent number: 8361500
    Abstract: Pharmaceutical formulations containing a salt of (5S,8S)-8-[{(1R)-1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one, represented by Formula I, which are suitable for forming into a tablet dosage form, as well as tablet dosage forms are disclosed. Disclosed also are methods of treatment utilizing such dosage forms.
    Type: Grant
    Filed: March 20, 2008
    Date of Patent: January 29, 2013
    Assignee: Opko Health, Inc.
    Inventors: Zhihui Qiu, Wing-Kee Philip Cho, Na Zhao, Victor Ming-she Wong
  • Patent number: 8334317
    Abstract: The present invention relates generally to novel calcimimetic compounds and pharmaceutical compositions comprising them. The invention also relates to methods of treating of diseases or disorders related to the function of the calcium sensing receptor using the compounds represented in Formula I.
    Type: Grant
    Filed: October 15, 2008
    Date of Patent: December 18, 2012
    Assignee: Amgen Inc.
    Inventors: Thomas S. Coulter, Christopher H. Fotsch, Chiara Ghiron, Paul E. Harrington, Michael G. Kelly, Philip Miller, Gilbert M. Rishton, David J. St. Jean, Jr., David J. Semin
  • Publication number: 20120302540
    Abstract: The invention relates to derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of a disorder or a disease mediated by the ghrelin receptor.
    Type: Application
    Filed: May 24, 2012
    Publication date: November 29, 2012
    Inventors: Ameet Vijay Ambarkhane, Gurdip Bhalay, Martin Beckett, James Dale, Ahmed Hamadi, Alessandro Mazzacani, Jeffrey McKenna, Christopher Thomson
  • 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: 20120288947
    Abstract: The present invention discloses a fluorescent probe compound which solved the problem of fluorescence quenching by Pd2+, and its preparation method and use as well. Excitation and emission wavelengths of the probe compound are in visible light region. The probe compound is highly sensitive and displays good selectivity for Pd2 in near-neutral pH range. In detection of Pd2 in 0-10 ppb level, fluorescence is evidently enhanced, and Pd2 in the level as low as 5 nM can be detected. Fluorescence intensity is well linearly correlated to Pd2 concentration. The probe compound can be used for detection of contaminating palladium and residual palladium in drug, soil, water sample and reactor.
    Type: Application
    Filed: December 6, 2010
    Publication date: November 15, 2012
    Applicants: DALIAN CHROMAS BIOSCIENCE CO., LTD, DALIAN UNIVERSITY OF TECHNOLOGY
    Inventors: Xiaojun Peng, Jiangli Fan, Honglin Li, Jingyun Wang, Shiguo Sun
  • Publication number: 20120289494
    Abstract: 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: Application
    Filed: May 11, 2012
    Publication date: November 15, 2012
    Applicants: Sanofi, The Regents of the University of Michigan
    Inventors: Shaomeng Wang, Wei Sun, Angelo Aguilar, Carlos Garcia-Echeverria
  • Publication number: 20120264738
    Abstract: A compound that inhibits interaction between murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity is provided. The present invention provides a dispiropyrrolidine derivative represented by the following formula (1), which has various substituents, inhibits interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity, wherein R1, R2, R3, ring A, and ring B in formula (1) respectively have the same meanings as defined in the specification.
    Type: Application
    Filed: March 9, 2012
    Publication date: October 18, 2012
    Inventors: Yuuichi Sugimoto, Kouichi Uoto, Takanori Wakabayashi, Masaki Miyazaki, Masaki Setoguchi, Toru Taniguchi, Keisuke Yoshida, Akitake Yamaguchi, Shoko Yoshida
  • Patent number: 8288431
    Abstract: 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: Grant
    Filed: January 19, 2011
    Date of Patent: October 16, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jin-Jun Liu, Jing Zhang, Zhuming Zhang
  • Publication number: 20120238757
    Abstract: 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: Application
    Filed: May 30, 2012
    Publication date: September 20, 2012
    Applicant: SANOFI
    Inventors: Zhongli GAO, Ryan HARTUNG, David STEFANY
  • Publication number: 20120220782
    Abstract: 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: Application
    Filed: April 30, 2012
    Publication date: August 30, 2012
    Inventors: Ulrich BERENS, Oliver DOSENBACH, Daniel SPRENGER
  • Patent number: 8236963
    Abstract: 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: Grant
    Filed: May 23, 2006
    Date of Patent: August 7, 2012
    Assignee: Merck Serono SA
    Inventors: Matthias Schwarz, Eric Sebille, Christophe Cleva, Cedric Merlot, Dennis Church, Patrick Page, Jacqueline A. Macritchie, John Frederick Atherall, Stefano Crosignani, Doris Pupowicz
  • Publication number: 20120190865
    Abstract: 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: Application
    Filed: January 25, 2012
    Publication date: July 26, 2012
    Applicant: Bayer CropScience AG
    Inventors: Reiner FISCHER, Thomas HIMMLER