Nitrogen Attached Directly Or Indirectly To The Diazine Ring By Nonionic Bonding Patents (Class 544/311)
  • Patent number: 10494347
    Abstract: The present invention relates to processes and intermediates for preparing Gonadotropin-Releasing Hormone (GnRH) receptor antagonists of structure (VI); and stereoisomers and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: December 6, 2017
    Date of Patent: December 3, 2019
    Assignee: Neurocrine Biosciences, Inc.
    Inventors: Donald J. Gallagher, Laszlo R. Treiber, Robert Michael Hughes, Onorato Campopiano, Peng Wang, Yuxin Zhao, Shine K. Chou, Michael Allen Ouellette, Donald Nicholas Hettinger
  • Patent number: 10245262
    Abstract: The present invention provides ligands which bind to MR1, some of which induce MR1 to bind to MAIT cells thereby activating or inhibiting MAIT cell activation.
    Type: Grant
    Filed: April 1, 2015
    Date of Patent: April 2, 2019
    Assignees: The University of Queensland, Monash University, The University of Melbourne
    Inventors: Alexandra Jane Corbett, James McCluskey, Lars Kjer-Nielsen, Zhenjun Chen, Jamie Rossjohn, Onisha Patel, Richard William Birkinshaw, Sidonia Barbara Guiomar Eckle, David Paul Fairlie, Ligong Liu, Jeffrey Yam Wing Mak
  • Patent number: 9969696
    Abstract: The present disclosure relates to compound of structural “formula I” and a method for preparing a compound of structural formula I. The disclosure further relates to a method of arresting DNA double-strand break (DSB) repair by employing the compound of structural formula I.
    Type: Grant
    Filed: March 7, 2013
    Date of Patent: May 15, 2018
    Assignee: INDIAN INSTITUTE OF SCIENCE
    Inventors: Sathees Chukkurumbal Raghavan, Mrinal Srivastava, Subhas Somalingappa Karki, Bibha Choudhary
  • Patent number: 9376394
    Abstract: The present application relate to processes for the preparation of bendamustine and its pharmaceutically acceptable salts.
    Type: Grant
    Filed: December 22, 2010
    Date of Patent: June 28, 2016
    Assignees: DR. REDDY'S LABORATORIES LTD., DR. REDDY'S LABORATORIES, INC.
    Inventors: Rajasekhar Kadaboina, Veerender Murki, Venkat Rao Badisa, Nageshwar Gunda
  • Publication number: 20150148340
    Abstract: The present application relates to novel bicyclically substituted uracil derivatives, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases.
    Type: Application
    Filed: May 3, 2013
    Publication date: May 28, 2015
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Chantal Fürstner, Jens Ackerstaff, Alexander Straub, Heinrich Meier, Hanna Tinel, Katja Zimmermann, Adrian Tersteegen, Dmitry Zubov, Raimund Kast, Jens Schamberger, Martina Schäfer, Kirsten Börngen
  • Patent number: 9040550
    Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
    Type: Grant
    Filed: July 16, 2014
    Date of Patent: May 26, 2015
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
  • Patent number: 9034850
    Abstract: Disclosed are compounds useful as gonadotrophin-releasing hormone (“GnRH”) receptor antagonist.
    Type: Grant
    Filed: November 19, 2010
    Date of Patent: May 19, 2015
    Assignee: SK Chemicals Co., Ltd.
    Inventors: Seon Mi Kim, Min Hee Lee, Jae Sun Kim, Hoe Chul Jung, So Young Lee, Soo Min Lee, Eun Jeong Kim, Eui Sun Park, Sung Hoon Park, Bong Yong Lee, Key An Um
  • Publication number: 20150110809
    Abstract: Embodiments of the invention are directed to compounds that inhibit an activity of EP AC proteins and methods of using the same. The inventors have developed a sensitive and robust high throughput screening (HTS) assay for the purpose of identifying EPAC specific inhibitors (Tsalkova et al. (2012) PLOS ONE 7 (1):e30441).
    Type: Application
    Filed: February 8, 2013
    Publication date: April 23, 2015
    Applicant: The Board of Regents of the University of Texas System
    Inventors: Xiaodong Cheng, Jia Zhou, Tamara Tsalkova, Fang Mei, Haijun Chen
  • Publication number: 20150099756
    Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema.
    Type: Application
    Filed: December 15, 2014
    Publication date: April 9, 2015
    Inventors: Yun JIN, Zehong WAN, Qing ZHANG
  • Patent number: 8987277
    Abstract: The invention relates to fungicides and can be used for treating diseases caused by fungi, and also for preventing damage to various materials and agricultural products by fungi. The fungicide is a 2,4-dioxo-5-(2-hydroxy-3,5-dichlorobenzylidiene)amino-1,3-pyrimidine salt of general formula: (A) or a dimer thereof: (B), where X is selected from the series consisting of: Na+, K+, Li+ and NH4+. An effective preparation having anti-fungal activity with a broad spectrum of action is created.
    Type: Grant
    Filed: March 3, 2011
    Date of Patent: March 24, 2015
    Assignees: Viktor Veniaminovich Tets, Georgy Viktorovich Tets
    Inventors: Viktor Veniaminovich Tets, Georgy Viktorovich Tets, Viktor Iosifovich Krutikov
  • Publication number: 20150080570
    Abstract: Described herein are monomers capable of forming a biologically useful multimer when in contact with one, two, three or more other monomers in an aqueous media. In one aspect, such monomers may be capable of binding to another monomer in an aqueous media (e.g. in vivo) to form a multimer, (e.g. a dimer). Contemplated monomers may include a ligand moiety, a linker element, and a connector element that joins the ligand moiety and the linker element. In an aqueous media, such contemplated monomers may join together via each linker element and may thus be capable of modulating one or more biomolecules substantially simultaneously, e.g., modulate two or more binding domains on a protein or on different proteins.
    Type: Application
    Filed: April 11, 2014
    Publication date: March 19, 2015
    Applicants: Coferon, Inc., Cornell University
    Inventors: Lee Daniel Arnold, Maneesh Pingle
  • Publication number: 20150065505
    Abstract: The present invention provides compounds of Formula (I), as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Application
    Filed: March 29, 2013
    Publication date: March 5, 2015
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang, Ji Jiang
  • Publication number: 20150056164
    Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Application
    Filed: April 24, 2014
    Publication date: February 26, 2015
    Applicant: AbbVie Inc.
    Inventors: David A. Betebenner, John K. Pratt, David A. DeGoey, Pamela L. Donner, Charles A. Flentge, Douglas K. Hutchinson, Warren M. Kati, Allan C. Krueger, Kenton L. Longenecker, Clarence J. Maring, John T. Randolph, Todd W. Rockway, Michael D. Tufano, Rolf Wagner, Dachun Liu
  • Publication number: 20150031715
    Abstract: The invention relates to compounds of formula I: wherein R1, R2, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula I for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to VLA-4 integrin antagonists to target cells expressing VLA-4.
    Type: Application
    Filed: January 24, 2013
    Publication date: January 29, 2015
    Inventors: Robert Alan Goodnow, JR., Matthew Michael Hamilton, Achyutharao Sidduri
  • Publication number: 20150018553
    Abstract: The present invention relates to processes and intermediates for preparing Gonadotropin-Releasing Hormone (GnRH) receptor antagonists of structure (VI); and stereoisomers and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: June 19, 2014
    Publication date: January 15, 2015
    Inventors: Donald J. Gallagher, Laszlo R. Treiber, Robert Michael Hughes, Onorato Campopiano, Peng Wang, Yuxin Zhao, Shine K. Chou, Michael Allen Ouellette, Donald Nicholas Hettinger
  • Publication number: 20140378490
    Abstract: A pharmaceutical product comprising at least one phenyl uracil-based pharmaceutically active agent or an agent of related structural type and processes for obtaining such product.
    Type: Application
    Filed: March 16, 2012
    Publication date: December 25, 2014
    Applicant: AbbVie Inc.
    Inventors: Huailiang Wu, Hao Hou, Adivaraha Jayasankar, Ameesha Patel, David Beno, Eric A. Schmitt, Geoff G. Zhang
  • Patent number: 8895573
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, Y, R2, R3, and Ra are defined herein.
    Type: Grant
    Filed: February 13, 2013
    Date of Patent: November 25, 2014
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Steven J Coats, Yue-Mei Zhang, Shu-Chen Lin, Li Liu, Tamara A Miskowski, Scott L. Dax, Henry J Breslin, Bart L. De Corte, Wei He
  • Patent number: 8853397
    Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
    Type: Grant
    Filed: February 5, 2013
    Date of Patent: October 7, 2014
    Assignee: Rigel Pharmacuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
  • Patent number: 8841314
    Abstract: Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.
    Type: Grant
    Filed: May 2, 2013
    Date of Patent: September 23, 2014
    Assignee: Pfizer Inc.
    Inventors: David Hepworth, Roger B. Ruggeri
  • Publication number: 20140275508
    Abstract: Artificial nucleosides including 2-methyl-nucleobase-substituted butane-1,3-diol nucleosides are disclosed. Four different stereoisomers of such nucleosides are possible. Oligonucleotides made up of the artificial nucleosides form homoduplexes of greater stability than DNA duplexes and have a reduced ability to hybridize to DNA or RNA.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Applicant: Elitech Holding B.V.
    Inventors: Noah Scarr, Eugeny A. Lukhtanov
  • Patent number: 8835449
    Abstract: Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.
    Type: Grant
    Filed: November 7, 2012
    Date of Patent: September 16, 2014
    Assignee: Pfizer Inc.
    Inventors: Edward L. Conn, David Hepworth, Roger B. Ruggeri
  • Publication number: 20140256747
    Abstract: The present invention relates to the field of organic synthesis and describes the synthesis of specific triazolopyrimidine compounds and intermediates thereof as well as related derivatives.
    Type: Application
    Filed: October 26, 2012
    Publication date: September 11, 2014
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Borut Zupancic, Nenad Maras, Damjan Sterk
  • Patent number: 8822685
    Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
    Type: Grant
    Filed: August 7, 2013
    Date of Patent: September 2, 2014
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
  • Patent number: 8765948
    Abstract: The present invention relates to processes and intermediates for preparing Gonadotropin-Releasing Hormone (GnRH) receptor antagonists of structure (VI); and stereoisomers and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: November 7, 2008
    Date of Patent: July 1, 2014
    Assignee: Neurocrine Biosciences, Inc.
    Inventors: Donald J. Gallagher, Laszlo R. Treiber, Robert Michael Hughes, Onorato Campopiano, Peng Wang, Yuxin Zhao, Michael Allen Ouellette, Donald Nicholas Hettinger, Helen Chou
  • Patent number: 8754190
    Abstract: The invention relates to conjugates of macromolecular carriers and drugs comprising linkers that release the drug or a prodrug through rate-controlled beta-elimination, and methods of making and using the conjugates.
    Type: Grant
    Filed: May 5, 2011
    Date of Patent: June 17, 2014
    Assignee: Prolynx LLC
    Inventors: Gary Ashley, Daniel V. Santi
  • Patent number: 8748603
    Abstract: There is provided crystalline forms of N-[2-[[(2,3-difluorophenyl)methyl]thio]-6-{[(1R,2S)-2,3-dihydroxy-1-methylpropyl]oxy}-4-pyrimidinyl]1-azetidinesulfon-amide anhydrate. Such compounds/forms may be useful in the treatment of a disease/condition in which modulation of chemokine receptor activity is beneficial.
    Type: Grant
    Filed: July 12, 2011
    Date of Patent: June 10, 2014
    Assignee: AstraZeneca AB
    Inventors: Britt Anne Ingela Gullberg, Thomas Peter Larsson, Jeffrey Paul Stonehouse
  • Publication number: 20140148410
    Abstract: Disclosed are nucleopeptide compounds that include a nucleobase, and an amino acid. Certain compounds further comprise a glycoside. The compounds may self-assemble to form supramolecular hydrogels. Also, the compounds may be used as a platform to examine specific biological functions (e.g., binding to DNA and RNA) of a dynamic supramolecular system that is able to interact with both proteins and nucleic acids. Other uses include: methods of growing cells and methods of delivering a substance to a cell.
    Type: Application
    Filed: December 2, 2013
    Publication date: May 29, 2014
    Applicant: Brandeis University
    Inventor: Bing Xu
  • Publication number: 20140142094
    Abstract: This disclosure relates to compounds, methods for their preparation, pharmaceutical compositions including these compounds and methods for the treatment of cellular proliferative disorders, including, but not limited to cancer. The method includes administering to the patient a therapeutically effective amount of a compound of formula (I), or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: April 30, 2012
    Publication date: May 22, 2014
    Applicant: ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI
    Inventors: M.V. Ramana Reddy, E. Premkumar Reddy
  • Patent number: 8722883
    Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: May 13, 2014
    Assignee: AstraZeneca AB
    Inventors: David Ranulf Cheshire, Rhona Jane Cox, Premji Meghani, Cherylin Francis Preston, Jeffrey Paul Stonehouse, Neal Michael Smith
  • Patent number: 8685991
    Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Grant
    Filed: April 3, 2012
    Date of Patent: April 1, 2014
    Assignee: AbbVie Inc.
    Inventors: Rolf Wagner, Warren M. Kati, Dachun Liu, Yaya Liu, Kenton L. Longenecker, Clarence J. Maring, John K. Pratt, Todd W. Rockway, Kent D. Stewart, Michael D. Tufano
  • Publication number: 20140031545
    Abstract: Processes for making an organozinc reagents are disclosed comprising reacting (A) organomagnesium or organozinc complexes with (B) at least one coordination compound comprising one or more carboxylate groups and/or alcoholate groups and/or tertiary amine groups, optionally in combination with zinc ions and/or lithium ions and/or halide ions, wherein the halide ions are selected from chloride, bromide and iodide, the organozinc complex comprises an aryl group, a heteroaryl group or a benzyl group when the coordinating compound is a chelating polyamine, and the reaction is conducted in the presence of zinc complexed with at least one coordinating compound when reactant (A) comprises at least one organomagnesium complex. The resulting organozinc reagents may optionally be isolated from solvents to obtain a solid reagent. The reagents may be used for making organic compounds via Negishi cross-coupling reactions or via aldehyde and/or ketone oxidative addition reactions.
    Type: Application
    Filed: December 21, 2011
    Publication date: January 30, 2014
    Applicant: LUDWIG-MAXIMILIAN-UNIVERSITAT MUNCHEN
    Inventors: Paul Knochel, Sebastian Bernhardt, Georg Manolikakes
  • Publication number: 20140011997
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: September 12, 2013
    Publication date: January 9, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Cameron Smith, Melissa Fleury, Roland Gendron, Ryan Hudson, Adam D. Hughes
  • Patent number: 8609864
    Abstract: The disclosure includes hydroxamic compounds of Formula I: (I) wherein P, Z, and m are defined herein. Also disclosed is a method for treating a neoplastic disease or an immune disease with these compounds.
    Type: Grant
    Filed: January 7, 2010
    Date of Patent: December 17, 2013
    Assignee: Purdue Pharmaceutical Products, L.P.
    Inventors: Yu Chen, Yi Chen
  • Publication number: 20130324724
    Abstract: Methods for the synthesis of disubstituted aminouracils and xanthine and/or xanthine-related compounds are provided.
    Type: Application
    Filed: May 31, 2013
    Publication date: December 5, 2013
    Inventors: Nhut Diep, Yuriy B. Kalyan
  • Patent number: 8569298
    Abstract: The present invention relates to compounds that inhibit of focal adhesion kinase function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm-blooded animals such as humans of diseases such as cancer.
    Type: Grant
    Filed: June 15, 2009
    Date of Patent: October 29, 2013
    Assignee: Astrazeneca AB
    Inventors: Bernard Christophe Barlaam, Patrick Ple, Kevin Michael Foote, Clifford David Jones
  • Publication number: 20130261301
    Abstract: The invention relates to fungicides and can be used for treating diseases caused by fungi, and also for preventing damage to various materials and agricultural products by fungi. The fungicide is a 2,4-dioxo-5-(2-hydroxy-3,5-dichlorobenzylidiene)amino-1,3-pyrimidine salt of general formula: (A) or a dimer thereof: (B), where X is selected from the series consisting of: Na+, K+, Li+ and NH4+. An effective preparation having anti-fungal activity with a broad spectrum of action is created.
    Type: Application
    Filed: March 3, 2011
    Publication date: October 3, 2013
    Inventors: Viktor Veniaminovich Tets, Georgy Viktorovich Tets, Viktor Iosifovich Krutikov
  • Publication number: 20130261302
    Abstract: The invention relates to medicine and can be used for treating a range of diseases in the treatment of which interferon is used. The agent for inducing endogenous interferon is comprised of the compound 6-(3-methoxycarbonyl phenyl) amino-2,4 (1H, 3H)-pyrimidinedione C12H11N3O4 of general formula: (I). The preparation exhibits greater activity both when injected and when administered orally.
    Type: Application
    Filed: October 10, 2011
    Publication date: October 3, 2013
    Inventors: Viktor Veniaminovich Tets, Georgy Viktorovich Tets, Viktor Iosifovich Krutikov
  • Publication number: 20130252963
    Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, or example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema.
    Type: Application
    Filed: December 5, 2011
    Publication date: September 26, 2013
    Inventors: Yun Jin, Zehong Wan, Qing Zhang
  • Patent number: 8513413
    Abstract: Subject of the present invention is a new improved process for the preparation of nitroorotic acid via nitration of orotic acid.
    Type: Grant
    Filed: February 22, 2010
    Date of Patent: August 20, 2013
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Rolf Dach, Xiangrui Jiang, Jingshan Shen, Jin Suo, Yi Zhu
  • Patent number: 8501941
    Abstract: The present invention provides compounds and pharmaceutical compositions that are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents. Also provided are processes for the preparation of the compounds and their intermediates.
    Type: Grant
    Filed: May 17, 2012
    Date of Patent: August 6, 2013
    Assignee: Dogwood Pharmaceuticals, Inc.
    Inventors: Guoquan Wang, Jayson M. Rieger, Robert D. Thompson
  • Patent number: 8501749
    Abstract: Disclosed are small molecule inhibitors of the formula (I), which are useful in treating various diseases and conditions involving chymase.
    Type: Grant
    Filed: January 26, 2010
    Date of Patent: August 6, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Xin Guo, Chuk Chui Man, Hidenori Takahashi
  • Patent number: 8492390
    Abstract: The invention relates to a novel strategy for the synthesis of Locked Nucleic Acid derivatives, such as ?-L-oxy-LNA, amino-LNA, ?-L-amino-LNA, thio-LNA, ?-L-thio-LNA, seleno-LNA and methylene LNA, which provides scalable high yielding reactions utilising intermediates that also can produce other LNA analogues such as oxy-LNA. Also, the compounds of the formula X are important intermediates that may be reacted with varieties of nucleophiles leading to a wide variety of LNA analogues.
    Type: Grant
    Filed: December 23, 2011
    Date of Patent: July 23, 2013
    Assignee: Santaris Pharma A/S
    Inventors: Mads Detlef Sorensen, Jesper Wengel, Troels Koch, Signe M. Christensen, Christoph Rosenbohm, Daniel Sejer Pedersen
  • Publication number: 20130137661
    Abstract: Disclosed are compounds useful as gonadotrophin-releasing hormone (“GnRH”) receptor antagonist.
    Type: Application
    Filed: November 19, 2010
    Publication date: May 30, 2013
    Applicant: SK CHEMICALS CO. LTD.
    Inventors: Seon Mi Kim, Min Hee Lee, Jae Sun Kim, Hoe Chul Jung, So Young Lee, Soo Min Lee, Eun Jeong Kim, Eui Sun Park, Sung Hoon Park, Bong Yong Lee, Key An Um
  • Patent number: 8450304
    Abstract: The present invention comprises compounds of Formula (I). wherein: R1, R2, R3, and R4 are as defined in the specification. The invention also comprises pharmaceutical compositions comprising the compounds of formula (I) and methods of preventing, treating or ameliorating a CCR2 mediated syndrome, disorder or disease, for example, type II diabetes, obesity or asthma, by administering the compounds of formula (I).
    Type: Grant
    Filed: December 9, 2009
    Date of Patent: May 28, 2013
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Xuqing Zhang, Heather Rae Hufnagel, Cuifen Hou, Dana L. Johnson, Zhihua Sui, Barry Fegely, David Breslin
  • Publication number: 20130131075
    Abstract: The present invention relates to the compounds of general formula I wherein n, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and X are defined as described hereinafter, the enantiomers, the diastereomers, the mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable properties, the preparation thereof, the medicaments containing the pharmacologically effective compounds, the preparation thereof and the use thereof.
    Type: Application
    Filed: January 15, 2013
    Publication date: May 23, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Norbert HAUEL, Angelo CECI, Henri DOODS, Ingo KONETZKI, Juergen MACK, Henning PRIEPKE, Annette SCHULER-METZ, Rainer WALTER, Dieter WIEDENMAYER
  • Publication number: 20130116407
    Abstract: The invention relates to conjugates of macromolecular carriers and drugs comprising linkers that release the drug or a prodrug through rate-controlled beta-elimination, and methods of making and using the conjugates.
    Type: Application
    Filed: May 5, 2011
    Publication date: May 9, 2013
    Inventors: Gary Ashley, Daniel V. Santi
  • Patent number: 8415351
    Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Grant
    Filed: March 17, 2010
    Date of Patent: April 9, 2013
    Assignee: Abbott Laboratories
    Inventors: Rolf Wagner, Warren M. Kati, Dachun Liu, Yaya Liu, Kenton L. Longenecker, Clarence J. Maring, John K. Pratt, Todd W. Rockway, Kent D. Stewart, Michael D. Tufano
  • Patent number: 8410123
    Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.
    Type: Grant
    Filed: December 23, 2011
    Date of Patent: April 2, 2013
    Assignee: AstraZeneca AB
    Inventors: David Ranulf Cheshire, Rhona Jane Cox, Premji Meghani, Neal Michael Smith, Jeffrey Paul Stonehouse, Cherylin Francis Preston
  • Patent number: 8410266
    Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
    Type: Grant
    Filed: November 3, 2011
    Date of Patent: April 2, 2013
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li
  • Publication number: 20130079518
    Abstract: The present invention relates to a method of making pyrimidines of formula (III) wherein X1, X2, R1 and R2 have the meanings as defined herein.
    Type: Application
    Filed: November 16, 2012
    Publication date: March 28, 2013
    Inventors: Guenter LINZ, Gerd KRAEMER, Adil DURAN