Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Five- Membered Hetero Ring Patents (Class 546/278.1)
  • Patent number: 9777020
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts, esters, amides, or radiolabelled forms thereof, wherein R1, Z1, Z2, and n are as defined in the specification, are useful in treating conditions or disorders prevented by or ameliorated by Tropomysin receptor kinases (Trk). Methods for making the compounds are disclosed. Also disclosed are pharmaceutical compositions of compounds of formula (I), and methods for using such compounds and compositions.
    Type: Grant
    Filed: January 22, 2015
    Date of Patent: October 3, 2017
    Assignee: AbbVie Inc.
    Inventors: Robert J. Altenbach, Huaqing Liu, Bruce Clapham, Ana L. Aguirre, Marlon Cowart, John R. Koenig, Kathy Sarris, Marc J. Scanio, Kerren K. Swinger, Anil Vasudevan, Clara I. Villamil, Kevin R. Woller
  • Patent number: 9663492
    Abstract: Processes for the preparation of charged crosslinkers bearing a sulfonic acid moiety are disclosed. These procedures also optionally include methods to convert the resulting products to substantially a single salt form.
    Type: Grant
    Filed: December 15, 2015
    Date of Patent: May 30, 2017
    Assignee: ImmunoGen, Inc.
    Inventors: Wei Li, Robert Yongxin Zhao
  • Patent number: 9242936
    Abstract: Processes for the preparation of charged crosslinkers bearing a sulfonic acid moiety are disclosed. These procedures also optionally include methods to convert the resulting products to substantially a single salt form.
    Type: Grant
    Filed: November 12, 2014
    Date of Patent: January 26, 2016
    Assignee: ImmunoGen, Inc.
    Inventors: Wei Li, Robert Yongxin Zhao
  • Patent number: 9023871
    Abstract: The present invention provides materials and methods to induce cell death by methuosis, a non-apoptotic cell death mechanism, to induce vacuolization without cell death, or to induce cell death without vacuolization. Small molecules herein are useful for treating cell proliferation disorders or anomalies, particularly, but not exclusively, cancer. Methods related to the research and pharmaceutical use of the small molecules are also provided herein.
    Type: Grant
    Filed: April 7, 2014
    Date of Patent: May 5, 2015
    Assignee: The University of Toledo
    Inventors: William A. Maltese, Paul W. Erhardt, Christopher Trabbic, Jean H. Overmeyer
  • Publication number: 20150119402
    Abstract: The present application is related to compounds represented by Formula I, which are novel positive allosteric modulators of al nAChRs. The application also discloses the treatment of disorders that are responsive to enhancement of acetylcholine action on al nAChRs in a mammal by administering an effective amount of a compound of Formula I.
    Type: Application
    Filed: May 8, 2013
    Publication date: April 30, 2015
    Inventor: Derk Hogenkamp
  • Publication number: 20150105393
    Abstract: The present invention relates to amide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.
    Type: Application
    Filed: April 25, 2013
    Publication date: April 16, 2015
    Inventors: Tatsuya Yamagishi, Kiyoshi Kawamura, Mikio Morita
  • Publication number: 20150099758
    Abstract: The present application is related to compounds represented by Formula I, which are novel positive allosteric modulators of al nAChRs. The application also discloses the treatment of disorders that are responsive to enhancement of acetylcholine action on al nAChRs in a mammal by administering an effective amount of a compound of Formula I.
    Type: Application
    Filed: May 8, 2013
    Publication date: April 9, 2015
    Applicant: Anvyl LLC
    Inventors: David Putnam, Olivier Dasse
  • Patent number: 8969383
    Abstract: The present invention relates to picolinamide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.
    Type: Grant
    Filed: June 12, 2014
    Date of Patent: March 3, 2015
    Assignee: RaQualia Pharma Inc.
    Inventors: Hirohide Noguchi, Tadashi Inoue, Mikio Morita, Yoshimasa Arano
  • Patent number: 8933099
    Abstract: The present invention provides a novel compound having FGFR inhibitory activity or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same. Specifically, the present invention provides a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof: wherein n represents 0 to 2; A represents an arylene group or a heteroarylene group; G represents a single bond, an oxygen atom or —CH2—; E represents a nitrogen-containing non-aromatic heterocycle; R1 represents an alkoxy group or the like; R2 represents a hydrogen atom or the like; and R3 represents a hydrogen atom, an alkyl group, an alkoxy group or the like, with the proviso that when E represents an azetidine ring and R2 or R3 is present on a nitrogen atom on the azetidine ring, the R2 or R3 does not represent a hydrogen atom.
    Type: Grant
    Filed: February 19, 2014
    Date of Patent: January 13, 2015
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Setsuo Funasaka, Toshimi Okada, Keigo Tanaka, Satoshi Nagao, Isao Ohashi, Yoshinobu Yamane, Yusuke Nakatani, Yuki Karoji
  • Publication number: 20150011546
    Abstract: Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
    Type: Application
    Filed: February 11, 2013
    Publication date: January 8, 2015
    Inventors: Brian K. Albrecht, James Edmund Audia, Andrew S. Cook, Les A. Dakin, Martin Duplessis, Victor S. Gehling, Jean-Christophe Harmange, Christopher G. Nasveschuk, Rishi G. Vaswani
  • Patent number: 8921566
    Abstract: Processes for the preparation of charged crosslinkers bearing a sulfonic acid moiety are disclosed. These procedures also optionally include methods to convert the resulting products to substantially a single salt form.
    Type: Grant
    Filed: October 3, 2013
    Date of Patent: December 30, 2014
    Assignee: ImmunoGen, Inc.
    Inventors: Wei Li, Robert Yongxin Zhao
  • Publication number: 20140350034
    Abstract: The invention relates to compound of the formula (I) in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.
    Type: Application
    Filed: January 25, 2013
    Publication date: November 27, 2014
    Applicant: NOVARTIS AG
    Inventors: Trixi Brandl, Stefanie Flohr, Christian Markert, Kenji Namoto, Bernard Pirard, Martin Renatus
  • Publication number: 20140349989
    Abstract: The invention relates to compounds, pharmaceutical compositions and methods useful for treating cancer, systemic or chronic inflammation, rheumatoid arthritis, diabetes, obesity, T-cell mediated autoimmune disease, ischemia, and complications associated with these diseases and disorders.
    Type: Application
    Filed: December 20, 2013
    Publication date: November 27, 2014
    Applicant: ALZHEIMER'S INSTITUTE OF AMERICA
    Inventors: Dange Vijay Kumar, Paul M. Slattum, Kraig M. Yager, Mark D. Shenderovich, Rajendra Tangallapally, Se-Ho Kim
  • Patent number: 8884020
    Abstract: Indole derivatives that are useful for treating pain, inflammation and other conditions are described. Certain of the compounds are benzyl derivatives and others are benzoyl derivatives. The compounds are substituted at least at the 3 position of the indole.
    Type: Grant
    Filed: August 7, 2007
    Date of Patent: November 11, 2014
    Assignee: Ironwood Pharmaceuticals, Inc.
    Inventors: John Jeffrey Talley, Kevin Sprott, James Philip Pearson, G. Todd Milne, Wayne Schairer, Jane Yang, Charles Kim, Timothy Barden, Regina Lundrigan, Ara Mermerian, Mark G. Currie
  • Publication number: 20140296237
    Abstract: The present invention relates to picolinamide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.
    Type: Application
    Filed: June 12, 2014
    Publication date: October 2, 2014
    Inventors: Hirohide NOGUCHI, Tadashi INOUE, Mikio MORITA, Yoshimasa ARANO
  • Publication number: 20140288126
    Abstract: The present invention provides novel organic compounds of Formula (I): methods of use, and pharmaceutical compositions thereof.
    Type: Application
    Filed: May 28, 2014
    Publication date: September 25, 2014
    Applicant: NOVARTIS AG
    Inventors: Christopher Michael ADAMS, Qi-Ying HU, Leslie Wighton MCQUIRE, Julien Papillon
  • Patent number: 8815908
    Abstract: Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein X, Y, R1 and R2 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Grant
    Filed: January 4, 2013
    Date of Patent: August 26, 2014
    Assignee: Ardelyx, Inc.
    Inventors: Jason G. Lewis, Jeffrey W. Jacobs, Nicholas Reich, Michael R. Leadbetter, Noah Bell, Han-Ting Chang, Tao Chen, Marc Navre, Dominique Charmot, Christopher Carreras, Eric Labonte
  • Publication number: 20140235614
    Abstract: The present invention provides a novel compound having FGFR inhibitory activity or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same. Specifically, the present invention provides a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof: wherein n represents 0 to 2; A represents an arylene group or a heteroarylene group; G represents a single bond, an oxygen atom or —CH2—; E represents a nitrogen-containing non-aromatic heterocycle; R1 represents an alkoxy group or the like; R2 represents a hydrogen atom or the like; and R3 represents a hydrogen atom, an alkyl group, an alkoxy group or the like, with the proviso that when E represents an azetidine ring and R2 or R3 is present on a nitrogen atom on the azetidine ring, the R2 or R3 does not represent a hydrogen atom.
    Type: Application
    Filed: February 19, 2014
    Publication date: August 21, 2014
    Applicant: Eisai R&D Management Co., Ltd.
    Inventors: Setsuo Funasaka, Toshimi Okada, Keigo Tanaka, Satoshi Nagao, Isao Ohashi, Yoshinobu Yamane, Yusuke Nakatani, Yuki Karoji
  • Publication number: 20140221431
    Abstract: Disclosed in the present invention is a novel histone deacetylase inhibitor of benzamides and use thereof. The inhibitor has good efficacy in treating diseases caused by abnormal gene expression, such as tumours, endocrine disorders, immune system diseases, genetic diseases and nerve system diseases. The histone deacetylase inhibitor of benzamides is a compound of the following general chemical structural formula (I) or a salt thereof.
    Type: Application
    Filed: June 26, 2012
    Publication date: August 7, 2014
    Applicants: Shanghai Institute of Pharmaceutical Industry, Sinopharm A-think Pharmaceutical Co., Ltd
    Inventors: Jianqi Li, Qingwei Zhang, Zhidan Jia, Jiajing Wang
  • Publication number: 20140213615
    Abstract: The present invention provides materials and methods to induce cell death by methuosis, a non-apoptotic cell death mechanism, to induce vacuolization without cell death, or to induce cell death without vacuolization. Small molecules herein are useful for treating cell proliferation disorders or anomalies, particularly, but not exclusively, cancer. Methods related to the research and pharmaceutical use of the small molecules are also provided herein.
    Type: Application
    Filed: April 7, 2014
    Publication date: July 31, 2014
    Applicant: THE UNIVERSITY OF TOLEDO
    Inventors: William A. Maltese, Paul W. Erhardt, Christopher Trabbic, Jean H. Overmeyer
  • Publication number: 20140212495
    Abstract: The present invention is directed to novel pharmaceutical compositions comprising nano- and micro-particulate formulations of poorly water soluble tubulin inhibitors of the indole chemical class, preferably N-substituted indol-3-glyoxyamides, and more preferably N-(Pyridin-4-yl)-[1-(4-chlorobenzyl)-indol-3-yl]glyoxylic acid amide (D-24851), also known as “Indibulin,” and methods of making and using such compositions for the treatment of anti-tumor agent resistant cancers and other diseases.
    Type: Application
    Filed: August 15, 2013
    Publication date: July 31, 2014
    Applicant: ZIOPHARM ONCOLOGY, INC.
    Inventors: Pavlos Papadopoulos, Gerhard Raab, Mark J. Doty, James E. Kipp, Berthold Roessler
  • Patent number: 8785489
    Abstract: Disclosed are compounds and compositions of the formula I as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula I.
    Type: Grant
    Filed: October 13, 2009
    Date of Patent: July 22, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Asitha Abeywardane, Bennett Farmer, Neil Alexander Farrow, Donghong Amy Gao, Alexander Heim-Riether, Lana Louise Smith Keenan, Ingo Andreas Mugge, Steven John Taylor, Zhaoming Xiong, Yang Yu, Qiang Zhang
  • Patent number: 8772500
    Abstract: Disclosed herein are modulators of TRPV3 of formula (II): wherein G1, X1, X2, X3, X4, X5, G2, Ra, Rb, and u are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also presented.
    Type: Grant
    Filed: October 23, 2012
    Date of Patent: July 8, 2014
    Assignee: AbbVie Inc.
    Inventors: Erol K. Bayburt, Bruce Clapham, Phil B. Cox, Jerome F. Daanen, Michael J. Dart, Gregory A. Gfesser, Arthur Gomtsyan, Michael E. Kort, Philip R. Kym, Robert G. Schmidt
  • Patent number: 8772499
    Abstract: Disclosed herein are modulators of TRPV3 of Formula (I) wherein p is 1, 2, 3, or 4, and G1, X1, X2, X3, X4, X5, G2, Z1, Ra, Rb, and u are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also presented.
    Type: Grant
    Filed: October 23, 2012
    Date of Patent: July 8, 2014
    Assignee: AbbVie Inc.
    Inventors: Erol K. Bayburt, Bruce Clapham, Phil B. Cox, Jerome F. Daanen, Michael J. Dart, Gregory A. Gfesser, Arthur Gomtsyan, Michael E. Kort, Philip R. Kym, Robert G. Schmidt, Eric A. Voight
  • Patent number: 8765757
    Abstract: The present invention relates to 3-Heterocyclic Substituted Indole Derivatives, compositions comprising at least one 3-Heterocyclic Substituted Indole Derivative, and methods of using the 3-Heterocyclic Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Grant
    Filed: November 13, 2008
    Date of Patent: July 1, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tin-Yau Chan, Jose S. Duca, Liwu Hong, Charles A. Lesburg, Brian A. McKittrick, Haiyan Pu, Li Wang, Henry M. Vaccaro
  • Publication number: 20140155413
    Abstract: The present invention is directed to compounds of formula I and 1a: which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
    Type: Application
    Filed: July 6, 2012
    Publication date: June 5, 2014
    Inventors: Barbara Hanney, Peter Manley, Michael T. Rudd, John M. Sanders, Shawn J. Stachel, Darrell Henze
  • Publication number: 20140051683
    Abstract: Compounds which inhibit the activity of anti-apoptotic Mcl-1 protein, compositions containing the compounds, and methods of treating diseases involving overexpressed or unregulated Mcl-1 protein are disclosed.
    Type: Application
    Filed: April 23, 2013
    Publication date: February 20, 2014
    Applicant: AbbVie Inc.
    Inventors: Xilu WANG, Xiaohong Song, Steven W. Elmore, Milan Bruncko, David J. Madar, Andrew J. Souers, Lisa A. Hasvold, Le Wang, Zhi-Fu Tao, Aaron R. Kunzer
  • Publication number: 20140004174
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.
    Type: Application
    Filed: May 20, 2013
    Publication date: January 2, 2014
    Applicant: Pharmacyclics, Inc.
    Inventors: Erik VERNER, Sriram BALASUBRAMANIAN, Joseph J. BUGGY
  • Publication number: 20140005386
    Abstract: Novel p53-Mdm2 antogonists that conform to Formula I or to Formula II: where the prescribed substituent groups are defined, are useful in treating or preventing cancer. In particular, the compounds and their pharmaceutical compositions are useful for treating relapsed/refractory acute myeloid and lymphoid leukemia and refractory chronic lymphocytic leukemia/small cell lymphocytic lymphomas.
    Type: Application
    Filed: September 8, 2011
    Publication date: January 2, 2014
    Inventor: Alexander Doemling
  • Patent number: 8614229
    Abstract: The present invention relates to Substituted Indole Derivatives, compositions comprising at least one Substituted Indole Derivative, and methods of using these Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Grant
    Filed: August 27, 2008
    Date of Patent: December 24, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Gopinadhan N. Anilkumar, Frank Bennett, Tin-Yau Chan, Kevin X. Chen, Mousumi Sannigrahi, Francisco Velazquez, Srikanth Venkatraman, Qingbei Zeng, Jose S. Duca, Charles A. Lesburg, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Neng-Yang Shih
  • Publication number: 20130331568
    Abstract: The invention provides compounds of formula I wherein n, A, R, R?, R?, R0, X and Y are as defined in the description, and their preparation. The compounds of formula I are useful as pharmaceuticals.
    Type: Application
    Filed: August 15, 2013
    Publication date: December 12, 2013
    Applicant: Novartis AG
    Inventors: Fabrizio Gasparini, Yves Auberson, Silvio Ofner, Terance W. Hart, Kaspar Zimmermann
  • Patent number: 8598362
    Abstract: Processes for the preparation of charged crosslinkers bearing a sulfonic acid moiety are disclosed. These procedures also optionally include methods to convert the resulting products to substantially a single salt form.
    Type: Grant
    Filed: December 8, 2011
    Date of Patent: December 3, 2013
    Assignee: ImmunoGen, Inc.
    Inventors: Wei Li, Robert Yongxin Zhao
  • Patent number: 8586573
    Abstract: The invention concerns compounds of general formula (I): Wherein n, X1, X2, X3, X4, Y, Z, Z1, Z2, Z3 and Z4 are as defined herein. The invention also concerns a process for the preparation of compounds of formula (I) and their therapeutic use.
    Type: Grant
    Filed: July 19, 2010
    Date of Patent: November 19, 2013
    Assignee: Sanofi
    Inventors: Laurent Dubois, Yannick Evanno, Andre Malanda, David Machnik, Catherine Gille
  • Publication number: 20130303538
    Abstract: The invention relates to compounds of the formula (I) in which the substituents are as defined in the specification; in free form or in salt form; to their preparation, to their use as medicament and to medicaments comprising them.
    Type: Application
    Filed: January 20, 2012
    Publication date: November 14, 2013
    Inventors: Joachim Nozulak, Dieter Oser
  • Publication number: 20130303526
    Abstract: The invention relates to substituted pyridine compounds of Formula (I) and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein R1a, A1, A2, E, G, Z1, and Z2 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: September 16, 2011
    Publication date: November 14, 2013
    Applicant: Purdue Pharma L.P.
    Inventors: Chiyou NI, Bin Shao, Laykea Tafesse, Jiangchao Yao, Jianming Yu, Xiaoming Zhou
  • Publication number: 20130274294
    Abstract: The invention relates to compound of the formula (I) or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it.
    Type: Application
    Filed: December 19, 2011
    Publication date: October 17, 2013
    Inventors: David Carcache, Manuel Koller, Silvio Ofner, David Orain, Johanne Renaud
  • Publication number: 20130267493
    Abstract: The present invention relates to indole and indazole compounds of Formula (I) that activate 5? adenosine monophosphate-activated protein kinase (AMPK). The invention also encompasses pharmaceutical compositions containing these compounds and methods for treating or preventing diseases, conditions, or disorders ameliorated by activation of AMPK.
    Type: Application
    Filed: March 15, 2013
    Publication date: October 10, 2013
    Applicant: PFIZER INC.
    Inventors: Samit Bhattacharya, Kimberly Cameron, Matthew Dowling, Dilinie Fernando, David Ebner, Kevin Filipski, Daniel Kung, Esther Lee, Aaron Smith, Meihua Tu
  • Patent number: 8524917
    Abstract: The invention provides compounds represented by the formula I, each of which compounds may have sphingosine-1-phosphate receptor agonist and or antagonist biological activity: and wherein the variables Y, R4, n, o, A, A1, A2, X, Z, R1, R3, R2, p, q and r are as defined in the specification. These compounds are useful for treating a disease or condition selected from the group consisting of glaucoma, dry eye, angiogenesis, cardiovascular conditions and diseases, and wound healing.
    Type: Grant
    Filed: January 11, 2008
    Date of Patent: September 3, 2013
    Assignee: Allergan, Inc.
    Inventors: Richard L. Beard, Haiqing Yuan, John E. Donello, Xiaoxia Liu, Tien Duong
  • Publication number: 20130172390
    Abstract: The present invention relates to halogen-substituted amide derivatives of the general formula (I) in which R1 to R6, Q1 to Q8, A, V, W, X, Y, n and m are each defined as described in the description—and to a process for preparation thereof and to the use thereof as insecticides and acaricides.
    Type: Application
    Filed: September 14, 2012
    Publication date: July 4, 2013
    Applicant: Bayer Intellectual Property GmbH
    Inventors: Markus Heil, Eike Kevin Heilmann, Alexander Sudau, Tobias Kapferer, Friedrich August Mühlthau, Peter Jeschke, Arnd Voerste, Ulrich Görgens, Klaus Raming, Ulrich Ebbinghaus-Kintscher, Mark Drewes, Martin Adamczewski, Angela Becker
  • Patent number: 8450310
    Abstract: Isoxazoles of formula (A) or (B) wherein R1 is a group of formula (IB) The isoxazoles are inhibitors of HSP90 activity, and useful for the treatment of, for example, cancers.
    Type: Grant
    Filed: June 18, 2012
    Date of Patent: May 28, 2013
    Assignees: Vernalis (R&D) Limited, Cancer Research Technology Ltd., The Institute of Cancer Research
    Inventors: Martin James Drysdale, Brian William Dymock, Harry Finch, Paul Webb, Edward McDonald, Karen Elizabeth James, Kwai Ming Cheung, Thomas Peter Matthews
  • Publication number: 20130116430
    Abstract: An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. The present invention provides a nicotinamide derivative represented by the following formula (I) (wherein R1 represents a halogen atom; R2 represents a C1-12 alkyl group, a C2-12 alkenyl group, a C2-12 alkynyl group, a C3-8 cycloalkyl group, an aryl group, an ar-C1-6 alkyl group or a heterocyclic group, each optionally having at least one substituent; R3 represents an aryl group or a heterocyclic group each optionally having at least one substituent; and R4 and R5 each independently represent a hydrogen atom; and R2 and R4 may form a cyclic amino group optionally having at least one substituent together with the nitrogen atom to which they bind) or a salt thereof, and a pharmaceutical composition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.
    Type: Application
    Filed: December 28, 2012
    Publication date: May 9, 2013
    Applicant: FUJIFILM CORPORATION
    Inventors: Hideyasu FUJIWARA, Kimihiko SATO, Shinsuke MIZUMOTO, Yuichiro SATO, Hideki KURIHARA, Yohei KUBO, Hiyoku NAKATA, Yasutaka BABA, Takashi TAMURA, Hidenobu KUNIYOSHI, Shinji HAGIWARA, Mari YAMAMOTO
  • Publication number: 20130109721
    Abstract: The present disclosure relates to N-benzyl pyrrole compounds of formula (I) useful as inhibitors of the enzyme Fatty Acid Amide Hydrolase (FAAH). The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the compositions in the treatment or prevention of various disorders.
    Type: Application
    Filed: December 8, 2010
    Publication date: May 2, 2013
    Applicant: Ironwood Pharmaceuticals, Inc.
    Inventors: Kevin Sprott, John Jeffrey Talley, Jane Yang, Bo Peng
  • Patent number: 8426448
    Abstract: CB-1 receptor inverse agonist compounds of Formula and pharmaceutical compositions for the treatment of obesity or cognitive impairment associated with schizophrenia.
    Type: Grant
    Filed: April 2, 2009
    Date of Patent: April 23, 2013
    Assignee: Eli Lilly and Company
    Inventor: Jingdan Hu
  • Publication number: 20130079313
    Abstract: The invention relates to inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are derivatives of 1-phenyl-2-pyridinyl alkyl alcohols, methods of preparing such compounds, compositions containing them and therapeutic use thereof.
    Type: Application
    Filed: September 26, 2012
    Publication date: March 28, 2013
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventor: Chiesi Farmaceutici S.p.A.
  • Patent number: 8399491
    Abstract: This disclosure relates to compounds of formula (I): wherein G1, G2, G3, G4, n, Y, Z, Z1, Z2, Z3, and Z4 are as defined in the disclosure, or a salt thereof, or a hydrate or solvate thereof, and to processes for the preparation of these compounds and the therapeutic use thereof.
    Type: Grant
    Filed: July 21, 2010
    Date of Patent: March 19, 2013
    Assignee: Sanofi
    Inventors: Laurent Dubois, Yannick Evanno, André Malanda
  • Publication number: 20130046095
    Abstract: The invention concerns compounds of general formula (I), wherein n, X1, X2, X3, X4, Y and W are as defined herein. The invention also concerns a method for preparing said compounds and their therapeutic use.
    Type: Application
    Filed: October 23, 2012
    Publication date: February 21, 2013
    Inventors: Laurent DUBOIS, Yannick EVANNO, Andre MALANDA
  • Publication number: 20130028843
    Abstract: The present invention relates to the crystal structure of the serine protease kallikrein 7 and to the use of this crystal structure in drug discovery. The present invention also relates to compounds binding specifically to this active site of kallikrein 7.
    Type: Application
    Filed: October 10, 2012
    Publication date: January 31, 2013
    Applicant: NOVARTIS AG
    Inventor: NOVARTIS AG
  • Patent number: 8309596
    Abstract: The present invention relates to the crystal structure of the serine protease kallikrein 7 and to the use of this crystal structure in drug discovery. The present invention also relates to compounds binding specifically to this active site of kallikrein 7.
    Type: Grant
    Filed: June 26, 2008
    Date of Patent: November 13, 2012
    Assignee: Novartis AG
    Inventors: Stefanie Flohr, Stefan Andreas Randl, Nils Ostermann, Ulrich Hassiepen, Frederic Berst, Ursula Bodendorf, Bernd Gerhartz, Andreas Marzinzik, Claus Ehrhardt, Josef Gottfried Meingassner
  • Patent number: 8242125
    Abstract: The invention relates to novel organic compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula I and to the use of a compound of formula I for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in the treatment of tumor diseases and ocular neovascular diseases.
    Type: Grant
    Filed: December 7, 2009
    Date of Patent: August 14, 2012
    Assignee: Novartis AG
    Inventors: Gerald David Artman, III, Jason Matthew Elliott, Nan Ji, Donglei Liu, Fupeng Ma, Nello Mainolfi, Erik Meredith, Karl Miranda, James J. Powers, Chang Rao
  • Publication number: 20120202817
    Abstract: A compound having the following formula [I] or a pharmaceutically acceptable salt thereof: wherein A is an aromatic five-membered heterocycle which optionally is fused with a cycloalkane ring; B is an alkylene; R1 and R2 are hydrogen, hydroxyl, alkoxy, aryloxy, alkyl, cycloalkyl, aryl, heterocycle, amino, alkylamino, arylamino or acyl, or R1 and R2 join together to form a heterocycle; X and Y are hydrogen, halogen, hydroxyl, alkoxy, aryloxy, alkyl, cycloalkyl, aryl, mercapto, alkylthio, arylthio, carboxyl, an ester of carboxyl, an amide of carboxyl, cyano or nitro; p is 0, 1 or 2; and q is 0 or 1. The compound is useful for treating diseases in which angiogenesis or augmentation of vascular permeability is involved.
    Type: Application
    Filed: April 18, 2012
    Publication date: August 9, 2012
    Applicant: SANTEN PHARMACEUTICAL CO., LTD.
    Inventors: Takahiro Honda, Hisashi Tajima, Yoshimasa Sasabuchi, Kenji Kawashima, Kazuyoshi Okamoto, Minoru Yamamoto, Masakazu Ban