The Additional Hetero Ring Is Five-membered Patents (Class 546/283.4)
  • Patent number: 9040566
    Abstract: The present invention relates to the use of selective adenosine A1 agonists, in particular the dicyanopyridines of formula (I), for the treatment and/or prophylaxis of glaucoma and ocular hypertension as well as the their use for the production of a medicament for the treatment and/or prophylaxis of glaucoma and ocular hypertension.
    Type: Grant
    Filed: August 29, 2011
    Date of Patent: May 26, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Jürgen Klar, Georges Von Degenfeld, Hans-Georg Lerchen, Barbara Albrecht-Küpper, Andreas Knorr, Peter Sandner, Daniel Meibom
  • 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
  • Publication number: 20150094341
    Abstract: The invention relates to compounds of macrocyclic picolinamides of Formula I suitable to control or prevent growth of fungi.
    Type: Application
    Filed: September 29, 2014
    Publication date: April 2, 2015
    Inventors: Fangzheng Li, Kevin G. Meyer, James M. Renga, Chenglin Yao, Jeremy Wilmot, Jessica Herrick, Karla Bravo-Altamirano, Timothy Boebel
  • Publication number: 20150057279
    Abstract: This invention relates to certain heteroaryl compounds which may be used as medicaments, more specifically as medicaments for treating animals. The medicament can be used for the treatment of parasitic infections such as helminth infections and the treatment of parasitosis caused by such infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to pharmaceutical compositions and kits comprising the compounds.
    Type: Application
    Filed: March 27, 2013
    Publication date: February 26, 2015
    Inventors: Michael Berger, Marko Eck, Christopher Kern
  • Patent number: 8952151
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted amidopyridine or amidopyridazine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
    Type: Grant
    Filed: December 23, 2013
    Date of Patent: February 10, 2015
    Assignee: Quanticel Pharmaceuticals, Inc.
    Inventors: Young K. Chen, Toufike Kanouni, Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennan Wallace
  • Publication number: 20150034871
    Abstract: An object is to provide a polymerizable compound having high polymerization reactivity, a high conversion ratio and high solubility in a liquid crystal composition, a polymerizable composition containing the compound, a liquid crystal composite prepared from the composition, and a liquid crystal display device having the composite. A solution is a polymerizable compound represented by formula (1). In the formula, for example, P1 and P2 are —OCO—(CH3)C?CH2; S1 and S2 are a single bond; ring A1, ring A2 and ring A3 are 1,4-phenylene; Z1, Z2 and Z3 are a single bond; two of G is —CH? or —N?; and a is 0 or 1.
    Type: Application
    Filed: July 31, 2014
    Publication date: February 5, 2015
    Applicants: JNC PETROCHEMICAL CORPORATION, JNC CORPORATION
    Inventors: Yasuyuki GOTOH, Teizi SATOU
  • Publication number: 20150038440
    Abstract: This invention recites dihydrofuran substituted azetidine derivatives of Formula (1) stereoisomers thereof, veterinarily acceptable salts thereof, compositions thereof, and their use as a parasiticide in mammals and birds. The substituents A, R1a, R1b, R1c, R2, R3, R4, R6, and n are as described herein.
    Type: Application
    Filed: January 29, 2013
    Publication date: February 5, 2015
    Inventors: Nathan Anthony Logan Chubb, Valerie A. Vaillancourt
  • Publication number: 20150011551
    Abstract: Described herein are compounds that modulate the activity of TNAP. In some embodiments, the compounds described herein inhibit TNAP. In certain embodiments, the compounds described herein are useful in the treatment of conditions associated with hyper-mineralization.
    Type: Application
    Filed: February 21, 2013
    Publication date: January 8, 2015
    Applicant: Sanford- Burnham Medical Reseach Institute
    Inventors: Anthony B. Pinkerton, Russell Dahl, Nicholas D.P. Cosford, Jose Luis Millan
  • Patent number: 8927534
    Abstract: The present invention is related to a compound of formula (I), wherein A is a nonaromatic heterocyclic ring, Ar is either absent or phenylene; ? is a radical of formula (II), R2 is a hydrophobic moiety; and G is a radical containing one or more moieties selected from the group consisting of NH, OH and a basic moiety. The compounds are inhibitors of integrins, especially antagonists of the fibronectin receptor alpha5beta1, useful as anti-angiogenic agents.
    Type: Grant
    Filed: January 31, 2007
    Date of Patent: January 6, 2015
    Assignee: Shire Orphan Therapies GmbH
    Inventors: Gunther Zischinsky, Roland Stragies, Frank Osterkamp, Dirk Scharn, Gerd Hummel, Holger Kalkhof, Grit Zahn, Doerte Vossmeyer, Claudia Christner-Albrecht, Ulrich Reineke
  • Publication number: 20140371274
    Abstract: The present invention relates to novel compounds, their use in the prevention or treatment of symptoms and disorders associated with the bradykinin B1 pathway and pharmaceutical compositions containing them.
    Type: Application
    Filed: June 13, 2014
    Publication date: December 18, 2014
    Inventors: Andrea Rosario BECCARI, Gianluca BIANCHINI, Chiara LIBERATI, Michela FANI', Mara ZIPPOLI
  • Publication number: 20140371195
    Abstract: The present application discloses compounds capable of modulating the activity of histone demethylases (HDMEs), which are useful for prevention and/or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, such as e.g. cancer. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds as a medicament.
    Type: Application
    Filed: August 28, 2014
    Publication date: December 18, 2014
    Inventors: Marc Labelle, Thomas Boesen, Mukund Mehrotra, Qasim Khan, Farman Ullah
  • Publication number: 20140350055
    Abstract: The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases.
    Type: Application
    Filed: August 31, 2012
    Publication date: November 27, 2014
    Applicant: Amakem NV
    Inventors: Jo Alen, Sandro Boland, Arnaud Pierre Jean Bourin, Olivier Defert, Dirk Leysen
  • Patent number: 8895587
    Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4, G1, n, A1, A2, A3, A4, Y1, Y2, and Y3 are as defined in the claims. The invention also relates to processes and intermediates for preparing these compounds, to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising these compounds and to methods of using these compounds to control insect, acarine, nematode and mollusc pests.
    Type: Grant
    Filed: May 15, 2012
    Date of Patent: November 25, 2014
    Assignee: Syngenta Participations AG
    Inventors: Jerome Yves Cassayre, Myriem El Qacemi, Torsten Luksch, Peter Renold
  • Publication number: 20140329825
    Abstract: The invention relates to novel trifluoromethyl-oxadiazole derivatives of formula (I), and pharmaceutically acceptable salts thereof, in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, pharmaceutical combinations thereof, and their use as medicaments, particularly for the treatment of neurodegeneration, muscle atrophy or diabetes/metabolic syndrome via inhibition of HDAC4.
    Type: Application
    Filed: November 26, 2012
    Publication date: November 6, 2014
    Applicant: NOVARTIS AG
    Inventors: Christina Hebach, Joerg Kallen, Joachim Nozulak, Marina Tintelnot-Blomley, Leo Widler
  • Publication number: 20140296073
    Abstract: Compounds of the formula (I) or salts thereof, in which (R1)m, (R2)n, R3 and R4 as defined in Claim 1 are suitable as herbicides for the control of harmful plants or as plant growth regulators. The compounds can be prepared by the processes of Claim 7.
    Type: Application
    Filed: October 29, 2012
    Publication date: October 2, 2014
    Inventors: Harald Jakobi, Marc Mosrin, Hansjörg Dietrich, Elmar Gatzweiler, Isolde Häuser-Hahn, Ines Heinemann, Christopher Hugh Rosinger
  • Publication number: 20140296066
    Abstract: A compound of formula (I) (I), wherein R1 to R4 are, for example, each hydrogen, R5 is pyridyl, which has one or more substituents at least one of which is, for example, a 5 membered heterocycle; 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
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Thomas Pitterna, Olivier Loiseleur, Anthony Cornelius O'Sullivan, Torsten Luksch
  • Publication number: 20140275112
    Abstract: Disclosed herein are methods and compositions comprising compounds capable of normalizing neuronal calcium dyshomeostasis. Also disclosed are methods comprising these compounds for treating neuronal or neurological disorders, including Alzheimer's disease, Parkinson's disease, Huntington's disease, fronto-temporal dementia, Pick's disease, chronic traumatic encepholopathy, traumatic brain injury, stroke, cerebellar ataxia, multiple sclerosis, Down syndrome, and aging-related CNS disorders.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: Rosalind Franklin University of Medicine and Science
    Inventors: Grace E. Stutzmann, Russell Dahl
  • Publication number: 20140228408
    Abstract: The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and respiratory diseases.
    Type: Application
    Filed: August 31, 2012
    Publication date: August 14, 2014
    Applicant: AMAKEM NV
    Inventors: Jo Alen, Sandro Boland, Arnaud Pierre, Jean Bourin, Olivier Defert, Dirk Leysen
  • Publication number: 20140213591
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted amidopyridine or amidopyridazine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
    Type: Application
    Filed: December 23, 2013
    Publication date: July 31, 2014
    Applicant: Quanticel Pharmaceuticals, Inc.
    Inventors: Young K. Chen, Toufike Kanouni, Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennan Wallace
  • Publication number: 20140213616
    Abstract: The invention relates to pyridone amide compounds of formula I and I? or pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels: The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including pain.
    Type: Application
    Filed: January 29, 2014
    Publication date: July 31, 2014
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Sara Sabina Hadida-Ruah, Corey Anderson, Vijayalaksmi Arumugam, Iuliana Luci Asgian, Brian Richard Bear, Andreas P. Termin, James Philip Johnson
  • Publication number: 20140194349
    Abstract: A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.
    Type: Application
    Filed: March 11, 2014
    Publication date: July 10, 2014
    Applicant: AbbVie Inc.
    Inventors: David A. DeGoey, Charles A. Flentge, William J. Flosi, David J. Grampovnik, Dale J. Kempf, Larry L. Klein, Ming C. Yeung, John T. Randolph, Xiu C. Wang, Su Yu
  • Publication number: 20140187555
    Abstract: The present invention relates to new phosphodiesterase inhibitors, more specifically soft PDE4 inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new soft PDE4 inhibitors compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including inflammatory diseases.
    Type: Application
    Filed: August 9, 2012
    Publication date: July 3, 2014
    Applicant: AMAKEM NV
    Inventors: Dirk Leysen, Olivier Defert, Sandro Boland
  • Patent number: 8729105
    Abstract: The present invention relates to compounds of the formula wherein A1, A2, A3 and R1 to R8 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 7, 2011
    Date of Patent: May 20, 2014
    Assignee: Hoffmann La-Roche Inc.
    Inventors: Paul Hebeisen, Hugues Matile, Stephan Roever, Matthew Wright, Sannah Zoffmann Jensen
  • Publication number: 20140135329
    Abstract: The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.
    Type: Application
    Filed: June 20, 2013
    Publication date: May 15, 2014
    Inventors: Urs BAETTIG, Kamlesh BALA, Emma BUDD, Lee EDWARDS, Catherine HOWSHAM, Glyn Alan HUGHES, Darren Mark LEGRAND, Katrin SPIEGEL
  • Publication number: 20140107161
    Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R2, R3, R4, G1, n, A1, A2, A3, A4, Y1, Y2, and Y3 are as defined in the claims. The invention also relates to processes and intermediates for preparing these compounds, to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising these compounds and to methods of using these compounds to control insect, acarine, nematode and mollusc pests.
    Type: Application
    Filed: May 12, 2012
    Publication date: April 17, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Jerome Yves Cassayre, Myriem El Qacemi, Torsten Luksch, Peter Renold
  • Publication number: 20140094455
    Abstract: Compounds, including 3-carboxy aryl sulfonamide compounds, which agonize or antagonize aquaporin channels and methods of using them to treat disorders or diseases mediated by aquaporins.
    Type: Application
    Filed: August 19, 2013
    Publication date: April 3, 2014
    Applicant: ARIZONA BOARD OF REAGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA
    Inventors: Gary A. Flynn, Andrea J. Yool, Elton Rodrigues Migliati, Leslie S. Ritter
  • Publication number: 20140057920
    Abstract: This invention relates to substituted 4-pyridones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other auto-immune and allergic disorders, allograft rejection, and oncological diseases.
    Type: Application
    Filed: August 20, 2013
    Publication date: February 27, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Thorsten OOST, Dennis FIEGEN, Christian GNAMM, Sandra HANDSCHUH, Stefan PETERS, Gerald Juergen ROTH
  • Publication number: 20140057926
    Abstract: This invention relates to substituted 4-pyridones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other auto-immune and allergic disorders, allograft rejection, and oncological diseases.
    Type: Application
    Filed: August 20, 2013
    Publication date: February 27, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Thorsten OOST, Dennis FIEGEN, Christian GNAMM
  • Patent number: 8653270
    Abstract: The present invention relates to novel derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: November 18, 2011
    Date of Patent: February 18, 2014
    Assignee: Allergan, Inc.
    Inventors: Todd M. Heidelbaugh, Phong X. Nguyen
  • Publication number: 20130324550
    Abstract: The invention relates to compounds of formula I: where X, HAr, a, and R1 through R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: August 9, 2013
    Publication date: December 5, 2013
    Applicant: THERAVANCE, INC.
    Inventors: Eric L. Stangeland, Lori Jean Patterson, Sheila Zipfel
  • Publication number: 20130310378
    Abstract: The present invention relates to novel 4-(4-pyridyl)-benzamides of the formula (I). The compounds I possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of Rho kinases (ROCKs).
    Type: Application
    Filed: April 23, 2013
    Publication date: November 21, 2013
    Applicants: AbbVie Inc., AbbVie Deutschland GmbH & Co KG
    Inventors: AbbVie Deutschland GmbH & Co KG, AbbVie Inc.
  • Publication number: 20130296369
    Abstract: The present invention relates to cyanoenamine derivatives, their process of preparation, intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants and in material protection, using these compounds or compositions.
    Type: Application
    Filed: November 11, 2011
    Publication date: November 7, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Jürgen Benting, Ulrike Wachendorff-Neumann, Philippe Desbordes, Christophe Dubost, Pierre Genix, Shinichi Narabu, Jean-Pierre Vors
  • Patent number: 8487112
    Abstract: The present invention relates to a process for preparing 4-aminobut-2-enolides and also corresponding intermediates and starting compounds which are passed through or used in the process according to the invention.
    Type: Grant
    Filed: September 5, 2008
    Date of Patent: July 16, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Norbert Lui, Jens-Dietmar Heinrich
  • Patent number: 8476269
    Abstract: The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.
    Type: Grant
    Filed: July 9, 2012
    Date of Patent: July 2, 2013
    Assignee: Novartis AG
    Inventors: Urs Baettig, Kamlesh Jagdis Bala, Emma Budd, Lee Edwards, Catherine Howsham, Glyn Alan Hughes, Darren Mark Legrand, Katrin Spiegel
  • Publication number: 20130136794
    Abstract: Heteroaryl(alkyl)dithiocarbamate compounds represented by general formula (I) or their pharmaceutically acceptable salts, their preparing methods, and their uses for preparing antitumor medicines are disclosed, wherein each said substituent is defined as in the description. The compounds are new tyrosine kinase inhibitors useful as an anti-tumor agents, preferably useful in the preparation of medicines for treating breast cancer, liver cancer, non-small cell lung cancer, gastric cancer, colon cancer, leukaemia or nasal cancer.
    Type: Application
    Filed: April 21, 2011
    Publication date: May 30, 2013
    Applicant: PEKING UNIVERSITY
    Inventors: Runtao Li, Zemei Ge, Jingrong Cui, Xingyl Sun, Zhongqing Wang, Xu Yan
  • Publication number: 20130131321
    Abstract: The present invention relates to the use for affinity purification of an antibody or an fragment of an antibody, of a ligand-substituted matrix comprising a support material and at least one ligand covalently bonded to the support material, the ligand being represented by formula (I) wherein Sp is a spacer group; v is 0 or 1; Am is an amide group —NR1—C(O)—, and wherein either NR1 is attached to Ar1 and —C(O)— is attached to Ar2, or —C(O)— is attached to Ar1 and NR1 is attached to Ar2; and R1 is hydrogen or C1 to C4 alkyl, preferably hydrogen or methyl; and more preferably hydrogen; Ar1 is a divalent 5- or 6-membered substituted or unsubstituted aromatic ring; Ar2 is 5- or 6-membered heterocyclic aromatic ring which is (a) attached to a further 5- or 6-membered aromatic ring via a single bond; or (b) fused to a further 5- or 6-membered aromatic ring as part of a multicyclic ring system; or (c) attached to at least one substituent selected from C1 to C4 alkyl; C2 to C4 alkenyl; C2 to C4 alkynyl; a
    Type: Application
    Filed: August 3, 2011
    Publication date: May 23, 2013
    Applicant: GRAFFINITY PHARMACEUTICALS GMBH
    Inventors: Holger Bittermann, Klaus Burkert, Marc Arnold, Oliver Keil, Thomas Neumann, Inge Ott, Kristina Schmidt, Daniel Schwizer, Renate Sekul
  • Publication number: 20130131036
    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: Application
    Filed: October 23, 2012
    Publication date: May 23, 2013
    Applicant: AbbVie Inc.
    Inventor: AbbVie Inc.
  • Publication number: 20130109713
    Abstract: The invention provides a compound of formula I:or a salt thereof, wherein R3-R8 and X and Y have any of the values described in the specification, as well as compositions comprising a compound of formula I. The compounds are useful as antibacterial agents.
    Type: Application
    Filed: June 24, 2011
    Publication date: May 2, 2013
    Inventors: Edmond J. Lavoie, Ajit Parhi, Daniel S. Pilch
  • Publication number: 20130053364
    Abstract: The invention provides sulphone compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various sulphone compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.
    Type: Application
    Filed: April 23, 2012
    Publication date: February 28, 2013
    Inventors: Hazel J. Dyke, Susan M. Cramp, Thomas D. Pallin, Janusz J. Kulagowski, John G. Montana, Robert Zahler
  • Patent number: 8383658
    Abstract: The invention relates to isoxazole derivatives, compositions comprising such compounds, and methods of preventing or treating conditions and disorders using such compounds and compositions.
    Type: Grant
    Filed: June 3, 2009
    Date of Patent: February 26, 2013
    Assignee: Abbott Laboratories
    Inventors: Murali Gopalakrishnan, Jianguo Ji, Chih-Hung Lee, Tao Li, Kevin B. Sippy
  • Publication number: 20130040975
    Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates, and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
    Type: Application
    Filed: August 10, 2012
    Publication date: February 14, 2013
    Applicant: NEUROCRINE BIOSCIENCES, INC.
    Inventors: Graham Beaton, Mi Chen, Timothy Richard Coon, Todd Ewing, Wanlong Jiang, Jinghua Yu, Willy Moree, Warren Wade, Liren Zhao, Yun-fei Zhu, Martin Rowbottom, Neil Ashweek
  • Publication number: 20130040992
    Abstract: The present invention relates to substituted 2,6-diamino-3,5-dicyano-4-arylpyridines of the formula (I) wherein the definitions of substituent groups R1-R7 are as provided in the specification and claims, to a pharmaceutical composition containing such a compound, to a process for preparation of such materials, and to their use as medicaments for the treatment of cardiovascular disorders and diabetes.
    Type: Application
    Filed: August 13, 2012
    Publication date: February 14, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Ulrich Rosentreter, Thomas Krämer, Andrea Vaupel, Walter Hübsch, Nicole Diedrichs, Thomas Krahn, Klaus Dembowsky, Johannes-Peter Stasch
  • Patent number: 8367838
    Abstract: The invention relates to the use of compounds of formula I wherein the substituents are described in the description and claims for the treatment of psychoses, dysfunction in memory and learning, schizophrenia, dementia, attention deficit disorders or Alzheimer's disease. The invention also relates to some compounds of formula I and pharmaceutical compositions containing them.
    Type: Grant
    Filed: May 25, 2012
    Date of Patent: February 5, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Sabine Kolczewski, Hans-Peter Marty, Robert Narquizian, Emmanuel Pinard, Henri Stalder
  • Patent number: 8350026
    Abstract: The invention relates to compounds of general formula (I) wherein W, D, E, G, J, L, R1, R2, R3, R4, R5 and Y are as defined herein, and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for treating diseases associated with deregulated angiogenesis, such as cancer and skin and eye diseases.
    Type: Grant
    Filed: August 27, 2009
    Date of Patent: January 8, 2013
    Assignee: Leo Pharma A/S
    Inventors: Jakob Felding, Xifu Liang, Anne Marie Horneman, Tina Dahlerup Poulsen, Jens Christian Højland Larsen
  • Publication number: 20120329769
    Abstract: The present invention relates to compounds of formula (I) wherein Q is Q1 or Q2 P is P1, heterocyclylor heterocyclyl substituted by one to five Z; and wherein A1, A2, A3, A4, G1, Y1, Z, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.
    Type: Application
    Filed: January 31, 2011
    Publication date: December 27, 2012
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Myriem El Qacemi, Jerome Yves Cassayre, Julie Clementine Toueg, Peter Renold, Thomas Pitterna
  • Publication number: 20120322801
    Abstract: The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases.
    Type: Application
    Filed: March 4, 2011
    Publication date: December 20, 2012
    Applicant: Amakem NV
    Inventors: Dirk Leysen, Olivier Defert, Nadzeya Kaval, Petra Blom, Sandro Boland
  • Publication number: 20120316147
    Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Application
    Filed: June 1, 2012
    Publication date: December 13, 2012
    Inventors: Caterina Bissantz, Uwe Grether, Paul Hebeisen, Atsushi Kimbara, Qingping Liu, Matthias Nettekoven, Marco Prunotto, Stephan Roever, Mark Rogers-Evans, Tanja Schulz-Gasch, Christoph Ullmer, Zhiwei Wang, Wulun Yang
  • Patent number: 8324133
    Abstract: The present invention relates to 2-pyridyl-methylene-carboxamide derivatives of formula (I) in which the substituents are as in the description, their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions:
    Type: Grant
    Filed: May 11, 2006
    Date of Patent: December 4, 2012
    Assignee: Bayer Cropscience AG
    Inventors: Stéphanie Gary, Brian Hill, Joseph Perez, Rachel Rama, Gilbert Spica, Jean-Pierre Vors
  • Publication number: 20120277232
    Abstract: The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.
    Type: Application
    Filed: July 9, 2012
    Publication date: November 1, 2012
    Inventors: Urs BAETTIG, Kamlesh Jagdis BALA, Emma BUDD, Lee EDWARDS, Catherine Howsham, Glyn HUGHES, Darren Mark LEGRAND, Katrin SPIEGEL
  • Publication number: 20120252670
    Abstract: Compounds of the formula (I), or salts thereof, in which R1 to R4 are as defined in formula (I) of claim 1 are suitable as useful-plant-protecting agents for reducing or preventing harmful effects of agrochemicals on the useful plants and their method of preparation are described.
    Type: Application
    Filed: June 14, 2012
    Publication date: October 4, 2012
    Inventors: Frank ZIEMER, Lothar Willms, Christopher Rosinger, Thomas Auler, Erwin Hacker, Udo Bickers