Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To Pyridine Or Partially Hydrogenated Pyridine Ring Patents (Class 546/262)
  • Patent number: 10053426
    Abstract: Process for preparing metyrapone type compounds are generally described herein. In particular, one step process for preparing metyrapone type compounds are described herein. Such processes generally include an alpha-carbon arylation coupling reaction between 3-isobutyrylpyridine and 3-halopyridine compounds in the presence of a palladium catalyst and a phosphine ligand to form the metyrapone-type compounds.
    Type: Grant
    Filed: October 5, 2015
    Date of Patent: August 21, 2018
    Assignee: Albemarle Corporation
    Inventors: Eric L. Williams, James D. Sunderhaus, James J. Springer
  • Publication number: 20150141433
    Abstract: Compounds that selectively negatively modulate NMDA receptors containing an NR2A subunit, pharmaceutical compositions comprising the compounds, and methods of treating a disease using the compounds are disclosed.
    Type: Application
    Filed: September 26, 2014
    Publication date: May 21, 2015
    Inventors: David R. Anderson, Robert A. Volkmann
  • Patent number: 9035063
    Abstract: This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung c
    Type: Grant
    Filed: December 9, 2014
    Date of Patent: May 19, 2015
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Hilary Schenck Eidam, Huiping Amy Guan, Chengde Wu, Mui Cheung
  • Publication number: 20150133473
    Abstract: The present invention provides a compound of formula (A): as described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula I, and pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: May 20, 2013
    Publication date: May 14, 2015
    Applicant: NOVARTIS AG
    Inventors: Matthew Burger, Joseph E. Drumm III, Gisele Nishiguchi, Alice Rico, Robert Lowell Simmons, Benjamin Taft, Huw Tanner
  • Publication number: 20150111879
    Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.
    Type: Application
    Filed: December 24, 2014
    Publication date: April 23, 2015
    Applicants: CURIS, INC., GENENTECH, INC.
    Inventors: Janet L. GUNZNER, Daniel P. SUTHERLIN, Mark S. STANLEY, Liang BAO, Georgette M. CASTANEDO, Rebecca L. LALONDE, Shumei WANG, Mark E. REYNOLDS, Scott J. SAVAGE, Kimberly MALESKY, Michael S. DINA, Michael F.T. KOEHLER
  • Publication number: 20150105550
    Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Applicants: CURIS, INC., GENENTECH, INC.
    Inventors: Janet L. GUNZNER, Daniel SUTHERLIN, Mark S. STANLEY, Liang BAO, Georgette M. CASTANEDO, Rebecca L. LALONDE, Shumei WANG, Mark E. REYNOLDS, Scott J. SAVAGE, Kimberly MALESKY, Michael S. DINA, Michael F.T. KOEHLER
  • Publication number: 20150099888
    Abstract: The present invention provides a compound of general formulae A useful as potential antitumor agents against human cancer cell lines and a process for the preparation thereof.
    Type: Application
    Filed: February 25, 2014
    Publication date: April 9, 2015
    Inventors: Ahmed Kamal, Mohammed Ashraf, Shaikh Faazil Bagwan, Yellamelli Valli Venkata Srikanth, Syed Mohammed Ali Hussaini, Adla Malla Reddy
  • Publication number: 20150094338
    Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
    Type: Application
    Filed: December 5, 2014
    Publication date: April 2, 2015
    Applicant: PFIZER INC.
    Inventors: Gary Erik Aspnes, Mary Theresa Didiuk, Kevin James Filipski, Angel Guzman-Perez, Jeffrey Allen Pfefferkorn, Benjamin Dawson Stevens, Meihua Mike Tu
  • Patent number: 8987457
    Abstract: The present invention provides a compound of formula (A): as described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula I, and pharmaceutical compositions comprising such compounds.
    Type: Grant
    Filed: May 20, 2013
    Date of Patent: March 24, 2015
    Assignee: Novartis AG
    Inventors: Matthew Burger, Joseph E. Drumm, III, Gisele Nishiguchi, Alice Rico, Robert Lowell Simmons, Benjamin Taft, Huw Tanner
  • Patent number: 8937071
    Abstract: This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung c
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: January 20, 2015
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Hilary Schenck Eidam, Kaushik Raha, Zhen Gong, Huiping Amy Guan, Chengde Wu, Haiying Yang, Haiyu Yu, Zhiliu Zhang, Mui Cheung
  • Patent number: 8933104
    Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
    Type: Grant
    Filed: July 18, 2014
    Date of Patent: January 13, 2015
    Assignee: Pfizer Inc.
    Inventors: Gary Erik Aspnes, Mary Theresa Didiuk, Kevin James Filipski, Angel Guzman-Perez, Jeffrey Allen Pfefferkorn, Benjamin Dawson Stevens, Meihua Mike Tu
  • Patent number: 8921370
    Abstract: The present invention provides bicyclo[3.2.1]octyl amide derivatives of formula (I): wherein L, R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.
    Type: Grant
    Filed: December 22, 2011
    Date of Patent: December 30, 2014
    Assignee: H. Lundbeck A/S
    Inventors: Guiying Li, Hao Zhou, Jesse Weiss, Dario Doller, James Ford Burns
  • Publication number: 20140350030
    Abstract: The present invention provides compounds of formula (I): where R1, R2, X, Y and n are as described herein, and pharmaceutical compositions, uses and methods comprising same.
    Type: Application
    Filed: September 17, 2012
    Publication date: November 27, 2014
    Inventors: Dario Doller, Guiying Li
  • Publication number: 20140329862
    Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
    Type: Application
    Filed: July 18, 2014
    Publication date: November 6, 2014
    Applicant: Pfizer Inc.
    Inventors: Gary Erik Aspnes, Mary Theresa Didiuk, Kevin James Filipski, Angel Guzman-Perez, Jeffrey Allen Pfefferkorn, Benjamin Dawson Stevens, Meihua Mike Tu
  • Publication number: 20140323486
    Abstract: The present invention provides a compound of the following formula, racemates, enantiomers and salts thereof. Also provided is the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.
    Type: Application
    Filed: December 21, 2012
    Publication date: October 30, 2014
    Inventors: Edward Malcolm Tyndall, Lloyd George Czaplewski, Colin William Gordon Fishwick, Andrew Ian Yule, Jeffrey Peter Mitchell, Kelly Helen Anderson, Gary Robert William Pitt
  • Publication number: 20140303206
    Abstract: The invention provides certain 3-pyridyl carboxamide-containing compounds of the Formula (I) (I) or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
    Type: Application
    Filed: October 1, 2012
    Publication date: October 9, 2014
    Inventors: Michael D. Altman, Kaleen Konrad Childers, Anthony Donofrio, John Michael Ellis, Sandra Lee Knowles, Alan B. Northrup
  • Publication number: 20140296067
    Abstract: A compound of formula (I) wherein R1 to R4 are, for example, each hydrogen, R5 is pyridyl, which has two or more substituents selected, for example, from halogen, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, and cyano; R6 is, for example, hydrogen; R7 is, for example, hydrogen, cyano, hydroxyl, formyl, C1-C4-alkyl, C1-C4-alkoxy, C2-C4-alkenyl, or C2-C4-alkynyl; and A1 to A5 are, independently selected, from, for example, N, and C—H; and its use as a pesticidal agent.
    Type: Application
    Filed: October 31, 2012
    Publication date: October 2, 2014
    Applicants: SYNGENTA PARTICIPATIONS AG, University of Exeter
    Inventors: Thomas Pitterna, Olivier Loiseleur, Paul Anthony Worthington, Anthony Cornelius O'Sullivan, Torsten Luksch, Vladimir Bobosik
  • Publication number: 20140256728
    Abstract: The present invention relates to the use of predominantly known pyridyl carboxamide derivatives as nematicides, compositions containing such compounds and methods for the control of nematodes.
    Type: Application
    Filed: October 29, 2012
    Publication date: September 11, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Jörg Nico Greul, Heiko Rieck, Christian Paulitz, Matthias Riedrich, Ralf Dunkel, Arianna Martelletti, Alexander Sudau, Peter Lösel, Olga Malsam, Arnd Voerste, Hans-Georg Schwarz, Ulrich Görgens, Kerstin Ilg, Michael Maue, Pierre-Yves Coqueron, Philippe Desbordes, Philippe Meresse, Stephanie Gary, Pierre Cristau, David Bernier
  • Publication number: 20140249135
    Abstract: New compounds, compositions and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.
    Type: Application
    Filed: May 9, 2014
    Publication date: September 4, 2014
    Applicant: NOVARTIS AG
    Inventors: Matthew Burger, Mika Lindvall, Wooseok Han, Jiong Lan, Gisele Nishiguchi, Cynthia Shafer, Cornelia Bellamacina, Kay Huh, Gordana Atallah, Christopher McBride, William Antonios-McCrea, JR., Tatiana Zavorotinskaya, Annette Walter, Pablo Dominguez Garcia
  • Publication number: 20140248299
    Abstract: The invention relates to compounds of structural formula (Ia): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein X1, X2, X3, X4, X6, X10, R1, Y, Z, L, and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Application
    Filed: May 9, 2014
    Publication date: September 4, 2014
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Gary Bohnert, Shoujun Chen, Yu Xie
  • Publication number: 20140243336
    Abstract: The invention provides certain 2-pyridyl carboxamide-containing compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
    Type: Application
    Filed: October 1, 2012
    Publication date: August 28, 2014
    Inventors: Michael D. Altman, Corey E. Bienstock, John W. Butcher, Kaleen Konrad Childers, Maria Emilia Di Francesco, Anthony Donofrio, John Michael Ellis, Christian Fischer, Andrew M. Haidle, James P. Jewell, Sandra Lee Knowles, Alan B. Northrup, Ryan D. Otte, Scott L. Peterson, Graham Frank Smith
  • Publication number: 20140241989
    Abstract: Compounds of formula (I) in which: >R is a linear or branched (C1-C6) alkyl, >L is a spacer group, >A is a diagnostic agent, and >m is equal to 1 or 2.
    Type: Application
    Filed: July 12, 2012
    Publication date: August 28, 2014
    Applicants: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS), LES LABORATOIRES SERVIER
    Inventors: Alain Lepape, Stéphanie Lerondel, Guillaume Reveillon, Jean-Marie Delbos, Luc Demuynck, Hubert Grandon, François Lefoulon, Gordon Tucker
  • Patent number: 8815905
    Abstract: The invention relates to propionic acids, propionic acid esters, and related compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds for the treatment of various diseases or conditions, including but not limited to diseases and/or conditions of Central Nervous System (CNS).
    Type: Grant
    Filed: March 8, 2011
    Date of Patent: August 26, 2014
    Assignee: Promentis Pharmaceuticals, Inc.
    Inventors: Mark A. Wolf, Keith D. Barnes
  • Patent number: 8809342
    Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
    Type: Grant
    Filed: December 22, 2011
    Date of Patent: August 19, 2014
    Assignee: Pfizer Inc.
    Inventors: Gary Erik Aspnes, Mary Theresa Didiuk, Kevin James Filipski, Angel Guzman-Perez, Jeffrey Allen Pfefferkorn, Benjamin Dawson Stevens, Meihua Mike Tu
  • Publication number: 20140228363
    Abstract: The present invention provides a compound of formula (I): as further described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula I, and pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: April 22, 2014
    Publication date: August 14, 2014
    Applicant: NOVARTIS AG
    Inventors: Matthew Burger, Yu Ding, Wooseok Han, Gisele Nishiguchi, Alice Rico, Robert Lowell Simons, Aaron R. Smith, Victoriano Tamez, JR., Huw Tanner, Lifeng Wan
  • Publication number: 20140221334
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
    Type: Application
    Filed: April 10, 2014
    Publication date: August 7, 2014
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Juan-Miguel Jimenez, Guy William Bemis, Francois Maltais, Tiansheng Wang, Ronald Marcellus Alphonsus Knegtel, Christopher John Davis, Damien Fraysse, Dean Boyall, Luca Settimo, Stephen Young, Michael Paul Mortimore
  • Publication number: 20140206877
    Abstract: The present invention relates to novel compounds, (2-chlorophenyl)-[2-(2-hydroxy-2-pyridin-4-yl-vinyl)pyridin-3-yl]methanone benzoate, and (2-chlorophenyl)-[2-(2-hydroxy-2-pyridin-4-yl-vinyl)pyridin-3-yl]methanone toluate, which are useful intermediates for the preparation of the compound of Formula I: The present invention further relates to novel processes for preparing a crystalline compound, which is {2-[1-(3,5-bis-trifluoromethyl-benzyl)-5-pyridin-4-yl-1H-[1,2,3]triazol-4-yl]-pyridin-3-yl}-(2-chlorophenyl)-methanone, Form IV.
    Type: Application
    Filed: March 27, 2014
    Publication date: July 24, 2014
    Applicant: Eli Lilly and Company
    Inventors: Michael Edward Kobierski, Michael E. Kopach, Pingyun Chen
  • Publication number: 20140187586
    Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein Y, L, X1, X2, Z, R3, R4, and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Application
    Filed: March 12, 2014
    Publication date: July 3, 2014
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Jun Jiang, Zhiqiang Xia, Junyi Zhang, Gary Bohnert, Shoujun Chen, Yu Xie
  • Publication number: 20140171446
    Abstract: The invention relates to certain compounds or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Application
    Filed: May 3, 2012
    Publication date: June 19, 2014
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Shoujun Chen, Gary Bohnert, Jun Jiang, Zhiqiang Xia
  • Patent number: 8741931
    Abstract: The present invention relates to compounds having formula: which are useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
    Type: Grant
    Filed: April 9, 2012
    Date of Patent: June 3, 2014
    Inventors: Juan-Miguel Jimenez, Guy William Bemis, Francois Maltais, Tiansheng Wang, Ronald Marcellus Alphonsus Knegtel, Christopher John Davis, Damien Fraysse, Dean Boyall, Luca Settimo, Stephen Young, Michael Paul Mortimore
  • Publication number: 20140142097
    Abstract: Compounds of the formula (I) in which R, R1 and X have the meanings indicated in claim 1, are inhibitors of TBK1 and IKK? and can be employed, inter alia, for the treatment of cancer and inflammatory diseases
    Type: Application
    Filed: April 11, 2012
    Publication date: May 22, 2014
    Applicant: Merck Patent GmbH
    Inventors: Guenter Hoelzemann, Hans-Michael Eggenweiler, Srinivasa R. Karra
  • Publication number: 20140135496
    Abstract: An isoxazoline-substituted benzamide compound of formula (1) or a salt thereof: wherein A1, A2 and A3 independently of one another are carbon atom or nitrogen atom, G is benzene ring, etc., W is oxygen atom or sulfur atom, etc., X is halogen atom, C1-C6haloalkyl, etc., Y ia halogen atm, C1-C6alkyl, etc., R1 is —CH?NOR1a, —C(O)OR1c, —C(O)NHR1d, phenyl substituted with (Z)p1, D-14, D-52, D-53, D-55 to D-59, etc., R1a is C1-C6alkyl, etc., R1c is C1-C6alkyl, etc., R1d is hydrogen atom, —C(O)R15, —C(O)OR15, etc., R2 is C1-C6alkyl, —CH2R14a, C1-C6alkynyl, —C(O)R15, —C(O)OR15, etc., further when R1 is —CH?NOR1a, —C(O)OR1c or —C(O)N(R1e)R1d, R2 may be hydrogen atom, R3 is C1-C6haloalkyl, etc., R14a is cyano, —OR25, etc., R15 is C1-C6alkyl, C1-C6haloalkyl, C1-C4alkoxy C1-C4alkyl, C1-C4alkylthio C1-C4alkyl, C3-C6cycloalkyl, C2-C6alkenyl, etc., R25 is C1-C4alkyl, C1-C4haloalkyl, —C(O)R32 or —C(O)OR32, etc., R32 is C1-C6alkyl or C3-C6cycloalkyl, etc., Z is halogen atom, cyano, nitro, C1-C6alkyl, C1-C6alkoxy, etc.
    Type: Application
    Filed: January 16, 2014
    Publication date: May 15, 2014
    Applicant: Nissan Chemical Industries, Ltd.
    Inventors: Takeshi MITA, Yuki FURUKAWA, Ken-ichi TOYAMA, Manabu YAOSAKA, Eitatsu IKEDA, Yoshihide MASUZAWA, Mitsuaki KOMODA
  • Patent number: 8710234
    Abstract: A compound represented by Formula (1): The compound can be used as insecticides.
    Type: Grant
    Filed: September 20, 2013
    Date of Patent: April 29, 2014
    Assignee: Mitsui Chemicals, Inc.
    Inventors: Kei Yoshida, Takeo Wakita, Hiroyuki Katsuta, Akiyoshi Kai, Yutaka Chiba, Kiyoshi Takahashi, Hiroko Kato, Nobuyuki Kawahara, Michikazu Nomura, Hidenori Daido, Junji Maki, Shinichi Banba
  • Publication number: 20140107160
    Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.
    Type: Application
    Filed: October 9, 2013
    Publication date: April 17, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Paul E. Fleming, Geraldine C.B. Harriman, Zhan Shi, B. Shaowu Chen
  • Publication number: 20140072981
    Abstract: A cysteine hydrazide nicotinamide (Cyhn) reagent designed for the enrichment of bacterial glycoproteins is provided. Methods for purification of free oligosaccharides and their analysis are also provided.
    Type: Application
    Filed: September 4, 2013
    Publication date: March 13, 2014
    Applicant: California Institute of Technology
    Inventors: William M. Clemons, Kyoung-Soon Jang, Roger Nani, Sergiy Levin, Sarah Reisman
  • Publication number: 20140038960
    Abstract: Novel hetaryl-[1,8]naphthyridine derivatives of formula (I) wherein R1, R2, W1, W3, W5 and W6 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.
    Type: Application
    Filed: October 4, 2013
    Publication date: February 6, 2014
    Applicant: MERCK PATENT GMBH
    Inventors: Alfred Jonczyk, Dieter Dorsch, Guenter Hoelzemann, Christiane Amendt, Frank Zenke
  • Patent number: 8633323
    Abstract: Disclosed herein are methods of preparing a bis(thio-hydrazide amides) compounds of the following structural formula: wherein R1, R2, R3, R4, R5, R6 and R13 are defined herein.
    Type: Grant
    Filed: March 31, 2009
    Date of Patent: January 21, 2014
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Shoujun Chen, Jun Jiang, Lijun Sun, Keizo Koya
  • Publication number: 20140018368
    Abstract: The present invention provides compounds which antagonize hedgehog signaling and inhibit HDAC activity. The compounds can be used in methods of treating proliferative diseases and disorders such as cancer.
    Type: Application
    Filed: July 1, 2013
    Publication date: January 16, 2014
    Applicants: Genetech, Inc., Curis, Inc.
    Inventors: Xiong Cai, Changgeng Qian, Haixiao Zhai
  • Publication number: 20140005212
    Abstract: The invention relates to substituted pyridine compounds of Formula I: (I) and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein R1a, R1b, R2a, R2b, R2c, A1, A2, and X are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Application
    Filed: December 21, 2011
    Publication date: January 2, 2014
    Applicant: Purdue Pharma L.P.
    Inventors: Chiyou Ni, Minnie Park, Bin Shao, Laykea Tafesse, Jiangchao Yao, Mark Youngman, Xiaoming Zhou
  • Publication number: 20130336965
    Abstract: The present invention provides a compound of formula (A): as described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula I, and pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: May 20, 2013
    Publication date: December 19, 2013
    Applicant: Novartis AG
    Inventors: Matthew Burger, Joseph E. Drumm, III, Gisele Nishiguchi, Alice Rico, Robert Lowell Simmons, Benjamin Taft, Huw Tanner
  • Patent number: 8609701
    Abstract: Methods are provided for administering pirfenidone to a patient that has exhibited abnormal biomarkers of liver function in response to pirfenidone administration. The methods include administering to a patient pirfenidone at doses lower than the full target dosage for a time period, followed by administering to the patient pirfenidone at the full target dosage. The methods also include administering pirfenidone at the full target dose with no reduction and administering permanently reduced doses of pirfenidone.
    Type: Grant
    Filed: November 9, 2009
    Date of Patent: December 17, 2013
    Assignee: Intermune, Inc.
    Inventors: Williamson Ziegler Bradford, Javier Szwarcberg
  • Patent number: 8603945
    Abstract: This disclosure relates to methods and compositions for modulating disease resistance in plants and transgenic plants.
    Type: Grant
    Filed: July 23, 2009
    Date of Patent: December 10, 2013
    Assignee: The Regents of the University of California
    Inventors: Colleen Marie Knoth, Thomas Eulgem, Thomas Girke
  • Patent number: 8592462
    Abstract: Methods are provided for administering pirfenidone to a patient that has exhibited abnormal biomarkers of liver function in response to pirfenidone administration. The methods include administering to a patient pirfenidone at doses lower than the full target dosage for a time period, followed by administering to the patient pirfenidone at the full target dosage. The methods also include administering pirfenidone at the full target dose with no reduction and administering permanently reduced doses of pirfenidone.
    Type: Grant
    Filed: December 6, 2011
    Date of Patent: November 26, 2013
    Assignee: Intermune, Inc.
    Inventors: Williamson Ziegler Bradford, Javier Szwarcberg
  • Publication number: 20130310347
    Abstract: High throughput methods for identifying novel inhibitors of Hsp90 chaperone protein folding are disclosed. The inhibitors so identified disrupt the binding of p23 to either Hsp90? or Hsp90? and have selective activity against the proliferation of cancer cells. In particular are provided embodiments of therapeutic compositions that comprise at least one inhibitor of an Hsp90 chaperone activity, the inhibitor being any of the compounds designated as CP1-CP19 as shown in FIGS. 1A-1D or a 2-(trifluoromethyl)pyrimidin-2-yl)thio)acetamide derivatives.
    Type: Application
    Filed: May 21, 2013
    Publication date: November 21, 2013
    Applicant: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Carmel Chan, Sanjiv S. Gambhir, David E. Solow-Cordero, Aileen Hoehne, Ramasamy Paulmurugan
  • Publication number: 20130210793
    Abstract: The present invention provides compounds of Formula I: along with compositions comprising the same and methods of using the same, such as for photodynamic therapy in the treatment of cancer.
    Type: Application
    Filed: March 21, 2013
    Publication date: August 15, 2013
    Applicant: Duke University
    Inventor: Duke University
  • Patent number: 8476257
    Abstract: Compounds of formula I: wherein X, R2, R3, R3a, R3b, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.
    Type: Grant
    Filed: December 3, 2008
    Date of Patent: July 2, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Pierre L. Beaulieu, Pasquale Forgione, Alexandre Gagnon, Cedrickx Godbout, Marc-Andre Joly, Montse Llinas-Brunet, Julie Naud, Martin Poirier, Jean Rancourt
  • Publication number: 20130150358
    Abstract: This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.
    Type: Application
    Filed: February 4, 2013
    Publication date: June 13, 2013
    Applicant: HMI MEDICAL INNOVATIONS, LLC.
    Inventor: HMI MEDICAL INNOVATIONS, LLC.
  • Patent number: 8455501
    Abstract: The present invention relates to compounds of the formula wherein R1 to R3 are defined in the description, and to pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as particularly dyslipidemia, atherosclerosis and cardiovascular diseases.
    Type: Grant
    Filed: September 10, 2012
    Date of Patent: June 4, 2013
    Assignee: Hoffmann-La Roche Inc
    Inventors: Uwe Grether, Stephan Roever
  • Patent number: 8455654
    Abstract: A nanoscale pigment particle composition includes an organic benzimidazolone pigment, and a sterically bulky stabilizer compound, wherein the benzimidazolone pigment associates non-covalently with the sterically bulky stabilizer compound that is a substituted pyridine derivative; and the presence of the associated stabilizer limits the extent of particle growth and aggregation, to afford nanoscale pigment particles.
    Type: Grant
    Filed: July 18, 2011
    Date of Patent: June 4, 2013
    Assignees: Xerox Corporation, National Research Council of Canada
    Inventors: Rina Carlini, Darren Andrew Makeiff
  • Publication number: 20130137660
    Abstract: The present invention relates to pyridines or pyrazines that inhibit kinases. In particular the compounds of the invention inhibit members of the class III PTK receptor family such as FMS (CSF-IR), c-KIT, PDGFR?, PDGFR? or FLT3 and KDR, SRC, EphA2, EphA3, EphA8, FLT1, FLT4, HCK, LCK, PTK5 (FRK), SYK, DDR1 and DDR2 and RET. The compounds of the invention are useful in the treatment of kinase associated diseases such as immunological and inflammatory diseases; hyperproliferative diseases including cancer and diseases involving neo-angiogenesis; renal and kidney diseases; bone remodeling diseases; metabolic diseases; and vascular diseases.
    Type: Application
    Filed: January 22, 2013
    Publication date: May 30, 2013
    Applicant: YM Biosciences Australia Pty Ltd
    Inventor: YM Biosciences Australia Pty Ltd