Bicyclo Ring System Having The Oxazine Ring As One Of The Cyclos (e.g., Benzoxazines, Etc.) Patents (Class 544/105)
  • Patent number: 9388203
    Abstract: The present disclosure provides for processes and intermediates in the large-scale manufacture of the compound of formula (I) or hydrates thereof.
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: July 12, 2016
    Inventors: Benedict McKeever, Louis Joseph Diorazio, Martin Francis Jones, Leigh Ferris, Sophie Laure Marie Janbon, Pawel Stanislaw Siedlecki, Gwydion Huw Churchill, Peter Alan Crafts
  • Patent number: 9359312
    Abstract: The present invention relates to a process for manufacturing a benzoxazinone of formula (I), by reacting a nitro compound of formula (II) with a reducing agent to obtain an amino compound of formula (III), and then reacting the amino compound of formula (III) with an acid; wherein the variables are defined according to the description, and benzoxazinone of formula (I).
    Type: Grant
    Filed: December 20, 2012
    Date of Patent: June 7, 2016
    Assignee: BASF SE
    Inventors: Maximilian Dochnahl, Michael Rack, Michael Keil, Bernd Wolf, Uwe Josef Vogelbacher, Joachim Gebhardt, Timo Frassetto, Volker Maywald
  • Patent number: 9353070
    Abstract: The present invention relates to carbamat-benzoxazinones of formula (I), wherein the variables are defined according to the description, as well as to a process for manufacturing carbamat-benzoxazinones of formula (I), and to the use of carbamat-benzoxazinones of formula (I) in manufacturing benzoxazinones of formula (X).
    Type: Grant
    Filed: August 7, 2013
    Date of Patent: May 31, 2016
    Assignee: BASF SE
    Inventors: Maximilian Dochnahl, Roland Goetz, Joachim Gebhardt, Uwe Josef Vogelbacher, Timo Frassetto, Michael Rack, Volker Maywald, Bernd Wolf
  • Patent number: 9346817
    Abstract: Dioxino- and oxazin-[2,3-d]pyrimidine PI3K inhibitor compounds of Formula I with anti-cancer activity, anti-inflammatory activity, or immunoregulatory properties, and more specifically with PI3 kinase modulating or inhibitory activity are described. Methods are described for using the tricyclic PI3K inhibitor compounds of Formula I for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, organisms, or associated pathological conditions.
    Type: Grant
    Filed: August 29, 2013
    Date of Patent: May 24, 2016
    Assignee: Genentech, Inc.
    Inventors: Robert Andrew Heald, Neville James McLean
  • Patent number: 9307767
    Abstract: Thiazolopyridinones of the general formula (I) are described as herbicides. In this formula (I), R1, R2, R3 and R4 represent radicals such as hydrogen, organic radicals such as alkyl and other radicals such as halogen, nitro and cyano.
    Type: Grant
    Filed: March 25, 2013
    Date of Patent: April 12, 2016
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Christian Waldraff, Stefan Lehr, Alfred Angermann, Hansjoerg Dietrich, Jan Dittgen, Elmar Gatzweiler, Christopher Hugh Rosinger, Angela Becker
  • Patent number: 9297940
    Abstract: The present invention relates to a compound represented by Formula 1, wherein in Formula 1, each of R1 to R7 is the same as defined in the specification, a photosensitive resin composition comprising the same, and a color filter prepared using the same. The color filter can realize high contrast and high brightness.
    Type: Grant
    Filed: June 18, 2014
    Date of Patent: March 29, 2016
    Assignee: Cheil Industries Inc.
    Inventors: Myoung Youp Shin, Won Jung Kim, Hwan Sung Cheon, Eui Soo Jeong
  • Patent number: 9255076
    Abstract: The present invention provides arylpiperazine derivatives having Formula I as shown below, which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder, and depression,
    Type: Grant
    Filed: February 24, 2015
    Date of Patent: February 9, 2016
    Assignee: REVIVA PHARMACEUTICALS, INC.
    Inventors: Laxminarayan Bhat, Prabhu Prasad Mohapatra, Kouacou Adiey
  • Patent number: 9180201
    Abstract: There is provided a practical method for preparing lipopeptide compounds, which method is capable of inexpensive mass production without requiring complicated operations. The lipopeptide compound of formula (3): is produced by reacting an ester compound of formula (1): with an ?-amino acid compound of formula (2): in the presence of a base and within a solvent containing a nonpolar organic solvent.
    Type: Grant
    Filed: September 7, 2010
    Date of Patent: November 10, 2015
    Assignee: NISSAN CHEMICAL INDUSTRIES, LTD.
    Inventors: Nobuyuki Kakiuchi, Takeaki Shoji, Kazuki Hirasada, Keigo Matsumoto, Hiroki Yamaguchi
  • Patent number: 9169221
    Abstract: Exemplary embodiments of the present invention relate to benzoxazines having various N-protecting groups. An R1 functional group is at least one selected from the group consisting of H and a halogen, an R2 functional group is at least one selected from the group consisting of H, an amide, or a carbamate, and a Z functional group is at least one selected from the group consisting of a phenyl, substituted phenyl group, methyl, and t-butyl group. The exemplary embodiments provide compounds with benzoxazines having various cleavable protecting groups such as amides and carbamates.
    Type: Grant
    Filed: September 30, 2013
    Date of Patent: October 27, 2015
    Assignee: COMSATS Institute of Information Technology
    Inventor: Muhammad Yar
  • Patent number: 9073834
    Abstract: The present invention provides a compound of formula (I) or its salts or pharmaceutically acceptable derivatives thereof wherein X1, R1, R2, R3, R4, and R5 are defined as set forth in the specification. The compounds are useful as potassium ion channel inhibitors.
    Type: Grant
    Filed: February 6, 2014
    Date of Patent: July 7, 2015
    Assignee: Xention Limited
    Inventors: Mushtaq Mulla, Derek Edward John, Richard John Hamlyn, Sasha Louise Garrett, Basil Hartzoulakis, David Madge, John Ford
  • Patent number: 9066519
    Abstract: The present invention relates to benzoxazinones of the general formula (I) wherein the variables are defined according to the description, processes and intermediates for preparing the benzoxazinones of the formula (I), compositions comprising them and their use as herbicides, i.e. for controlling harmful plants, and also a method for controlling unwanted vegetation which comprises allowing a herbicidal effective amount of at least one benzoxazinones of the formula (I) to act on plants, their seed and/or their habitat.
    Type: Grant
    Filed: May 2, 2014
    Date of Patent: June 30, 2015
    Assignee: BASF SE
    Inventors: Matthias Witschel, Trevor William Newton, Thomas Seitz, Helmut Walter, Bernd Sievernich, Anja Simon, Ricarda Niggeweg, Klaus Groβmann, Liliana Parra Rapado, Richard Roger Evans
  • Patent number: 9062012
    Abstract: The present invention relates to a process for manufacturing 4-substituted amino-benzoxazinones of formula (I), by reacting a NH-benzoxazinone of formula (II) with a compound of formula (III); wherein the variables are defined according to the description.
    Type: Grant
    Filed: December 20, 2012
    Date of Patent: June 23, 2015
    Assignee: BASF SE
    Inventors: Bernd Wolf, Joachim Gebhardt, Uwe Josef Vogelbacher, Maximilian Dochnahl, Michael Rack, Michael Keil, Timo Frassetto, Volker Maywald
  • Publication number: 20150148328
    Abstract: The invention relates to the novel products of formula (I) with p, q=0, 1 or 2; R1=phenyl, pyridyl; —(CH2)m—Ra; alkylene; cycloalkyl; heterocycloalkyl; alkyl; —SO2 —Rb; —CO—Re; m=1 or 2; Ra=aryl, heteroaryl, —CO-cycloalkyl, —CO-heterocycloalkyl, —CO—Rb, —C(Rb)?N—ORc, —CO 2 Rd, —CONRxRy; Rb=alkyl, aryl, heteroaryl; Rc=H, alkyl; Rd=alkyl, cycloalkyl; Re=alkyl, cycloalkyl, aryl, heteroaryl; NRxRy with Rx,Ry=H, alkyl, cycloalkyl, alkoxy, phenyl, or form with N a ring with optionally O, N; R2, R3=H, alkyl, CF 3, or form with C a ring with optionally O, S and N; R4=H, F, Cl, CH3 or CN; the morpholine is substituted with Me, and optionally substituted with F, OH; or is (Formula 1a) and the isomer of configuration R,R (Formula 1b) these products being in all the isomer forms and the salts, as medicaments, in particular as anticancer medicaments.
    Type: Application
    Filed: June 21, 2013
    Publication date: May 28, 2015
    Inventors: Youssef El-Ahmad, Bruno Filoche-Romme, Jean-Philippe Letallec, Gilbert Marciniak, Baptiste Ronan, Bertrand Vivet, Maurice Brollo
  • 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
  • Publication number: 20150148341
    Abstract: The present invention provides octahydro fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.
    Type: Application
    Filed: November 21, 2014
    Publication date: May 28, 2015
    Inventors: Hazel Hunt, Iain Walters, Benoit Gourdet
  • Publication number: 20150148327
    Abstract: The invention provides certain substituted pyridines of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, Cy, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
    Type: Application
    Filed: June 17, 2013
    Publication date: May 28, 2015
    Applicant: Merck Canada Inc.
    Inventors: Andrew M. Haidle, Sandra Lee Knowles, Solomon D. Kattar, Denis Deschenes, Jason Burch, Joel Robichaud, Matthew Christopher, Michael D. Altman, James P. Jewell, Alan B. Northrup, Marc Blouin, John Michael Ellis, Hua Zhou, Christian Fischer, Adam J. Schell, Michael H. Reutershan, Brandon M. Taoka, Anthony Donofrio, Joel Robichaud
  • Publication number: 20150148534
    Abstract: Disclosed is a novel enantiomeric synthesis ceramide-like inhibitors of UDP-glucose: N-acylsphingosine glucosyltransferase. Also disclosed are novel intermediates formed during the synthesis.
    Type: Application
    Filed: June 26, 2014
    Publication date: May 28, 2015
    Inventors: Bradford H. Hirth, Craig Siegel
  • Publication number: 20150148342
    Abstract: The present invention relates to bicyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.
    Type: Application
    Filed: November 26, 2014
    Publication date: May 28, 2015
    Applicant: INCYTE CORPORATION
    Inventors: Eddy W. Yue, Andrew P. Combs, Brent Douty
  • Patent number: 9040527
    Abstract: Disclosed embodiments provide pyrimidinediamine compounds useful for inhibiting kinase activity, including the activity of polo-like kinase 1 (PLK1). Also disclosed are pharmaceutical compositions comprising these compounds and methods of treating diseases associated with kinase activity, in particular enhanced PLK1 catalytic activity, such as diseases associated with abnormal cell proliferation, including neoplastic disorders.
    Type: Grant
    Filed: July 23, 2013
    Date of Patent: May 26, 2015
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Andy Atuegbu, John Ramphal, Hui Li, Marina Gelman, Jeffrey Clough, Carlos Valdez, Somasekhar Bhamidipati, Sambaiah Thota, Darren McMurtrie
  • Publication number: 20150141253
    Abstract: The present invention relates to a novel crystalline form B of 1,5-dimethyl-6-thioxo-3-(2,2,7-trifluoro-3-oxo-4-(prop-2-ynyl)-3,4-dihydro-2H-benzo[b][1,4]oxazin-6-yl)-1,3,5-triazinane-2,4-dione The invention also relates to a process for the production of this crystalline form and formulations for plant protection which contains the novel crystalline form of 1,5-dimethyl-6-thioxo-3-(2,2,7-trifluoro-3-oxo-4-(prop-2-ynyl)-3,4-dihydro-2H-benzo[b][1,4]oxazin-6-yl)-1,3,5-triazinane-2,4-dione.
    Type: Application
    Filed: May 15, 2013
    Publication date: May 21, 2015
    Inventors: Robert Reinhard, Tiziana Chiodo, Bernd Wolf, Stefan Scherer, Matthias Bratz, Matthias Witschel, Trevor William Newton, Thomas Seitz
  • Publication number: 20150141643
    Abstract: The invention relates to Substituted-Quinoxaline-Type Piperidine Compounds, compositions comprising an effective amount of a Substituted-Quinoxaline-Type Piperidine Compound and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Substituted-Quinoxaline-Type Piperidine Compound.
    Type: Application
    Filed: July 14, 2014
    Publication date: May 21, 2015
    Inventors: Kouki FUCHINO, R. Richard GOEHRING, Akira MATSUMURA, Bin SHAO, Yoshiyuki TAODA, Naoki TSUNO, John William Frank WHITEHEAD, Jiangchao YAO
  • Publication number: 20150141396
    Abstract: The present invention provides compounds of Formula (I) for the treatment of cancer, rheumatoid arthritis and other diseases.
    Type: Application
    Filed: July 3, 2013
    Publication date: May 21, 2015
    Applicant: Ares Trading S.A.
    Inventors: Stefano Crosignani, Catherine Jorand-Lebrun, Patrick Gerber, Mathilde Muzerelle
  • Publication number: 20150141644
    Abstract: The present invention relates to a pyrrolo[2,1-f][1,2,4]triazine compound, an isomer thereof or a pharmaceutically acceptable salt, ester or hydrate thereof, and a preparation method and application thereof. The pyrrolo[2,1-f][1,2,4]triazine compound has a structure expressed in general formula (I). The pyrrolo[2,1-f][1,2,4]triazine compound expressed in general formula (I) can inhibit a phosphatidylinositol-3 kinase (PI3K) signal pathway, thereby being used to prepare medicine for treating phosphatidylinositol-3 kinase related diseases such as cancer.
    Type: Application
    Filed: April 23, 2013
    Publication date: May 21, 2015
    Applicants: Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai Haihe Pharmaceutical Co., Ltd.
    Inventors: Chunhao Yang, Linghua Meng, Yanhong Chen, Xiang Wang, Cun Tan, Jiapeng Li, Jian Ding, Yi Chen
  • Publication number: 20150141407
    Abstract: The present invention relates to a compound of Formula I or a pharmaceutically acceptable salt thereof, its preparation method, a pharmaceutical composition comprising the compound, and its use in manufacture of a medicament for treatment of a disease or disorder, wherein R1, R2, R5, R6, X, Y, Q, W, n1 and n2 are defined as those stated in the description.
    Type: Application
    Filed: May 30, 2013
    Publication date: May 21, 2015
    Applicant: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
    Inventors: Lan Xie, Xiaofeng Wang, Kuo-Hsiung Lee
  • Publication number: 20150133437
    Abstract: The invention provides tetrahydro[1,8]naphthyridine and related compounds, methods of promoting RORy activity and/or increasing the amount of iL-17 in a subject, and therapeutic uses of the tetrahydro[1,8]naphthyridine and related compounds. In particular, the invention provides sulfonamide-tetrahydro[1,8]naphthyridine and related compounds, methods of using such compounds to promote RORy activity and/or increase the amount of iL-17 in a subject, and treat medical conditions in which activation of immune response would be beneficial such as in cancer and infections.
    Type: Application
    Filed: May 8, 2013
    Publication date: May 14, 2015
    Inventors: Thomas D. Aicher, Peter L. Toogood, Xiao Hu
  • Publication number: 20150133429
    Abstract: Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.
    Type: Application
    Filed: January 14, 2015
    Publication date: May 14, 2015
    Inventors: Julia Haas, Steven W. Andrews, Yutong Jiang, Gan Zhang
  • Publication number: 20150133426
    Abstract: The present invention relates to substituted pyrrolopyrimidine compounds general formula I: in which A, X, R1, R2, m and n are as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: May 17, 2013
    Publication date: May 14, 2015
    Inventors: Ulrich Klar, Georg Kettschau, Detlev Sülzle, Florian Puehler, Dirk Kosemund, Philip Lienau, Ulf Bömer, Lars Wortmann
  • Publication number: 20150126491
    Abstract: Compounds of the formula I: or a pharmaceutical salt thereof, wherein X, Ar1, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Application
    Filed: November 5, 2014
    Publication date: May 7, 2015
    Applicant: Genentech, Inc.
    Inventors: Monique Bodil van Niel, Andrew Cridland, Benjamin Fauber, Alberto Gobbi, Christopher Hurley, David Hurst, Jonathan Killen, Robert Maxey, Stuart Ward
  • Publication number: 20150126503
    Abstract: The invention relates to new substituted naphthyridines of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein R1 is selected from among —O—R3 or —NR3R4, R3 is C1-6-alkyl which is substituted by R5 and R6, R5 is selected from hydrogen, branched or linear C1-6-alkyl, C2-6-alkenyl, —C1-6-alkylen-O—C1-3-alkyl, C1-3-haloalkyl, R6 is ring X wherein n is either 0 or 1, and is a either a single or a double bond and wherein A, B, D and E are each independently from one another selected from CH2, CH, C, N, NH, O or S and wherein ring X is attached to the molecule either via position A, B, D or E, wherein said ring X may optionally be further substituted by one, two or three residues each selected individually from the group consisting of -oxo, hydroxy, —C1-3-alkyl, —C1-3-haloalkyl, —O—C1-3-alkyl, —C1-3-alkanol and halogen, and wherein R4, R2, R7, R8, R9, R10, R11 and Q may have the meanings as given in claim 1, as well as pha
    Type: Application
    Filed: January 8, 2015
    Publication date: May 7, 2015
    Inventors: Matthias HOFFMANN, Georg DAHMANN, Dennis FIEGEN, Sandra HANDSCHUH, Jasna KLICIC, Guenter LINZ, Gerhard SCHAENZLE, Andreas SCHNAPP, Stephen Peter EAST, Michael Philip MAZANETZ, Robert John SCOTT, Edward Walker
  • Publication number: 20150126504
    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: Application
    Filed: January 12, 2015
    Publication date: May 7, 2015
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Donald Payan, Susan Molineaux, Sacha Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander Rossi
  • Publication number: 20150126490
    Abstract: The present invention provides a compound of Formula (I) or a salt thereof; and therapeutic uses of these compounds. The present invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds with a therapeutic co-agent.
    Type: Application
    Filed: October 29, 2014
    Publication date: May 7, 2015
    Applicant: Novartis AG
    Inventors: Jeffrey T. BAGDANOFF, Yu DING, Wooseok HAN, Zilin HUANG, Qun JIANG, Jeff Xianming JIN, Xiang KOU, Patrick LEE, Mika LINDVALL, Zhongcheng MIN, Yue PAN, Sabina PECCHI, Keith Bruce PFISTER, Daniel POON, Vivek RAUNIYAR, Xiaojing Michael WANG, Qiong ZHANG, Jianguang ZHOU, Shejin ZHU
  • Publication number: 20150119385
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing said compound, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.
    Type: Application
    Filed: October 24, 2014
    Publication date: April 30, 2015
    Applicant: Novartis AG
    Inventors: Nicole Buschmann, Robin Alec Fairhurst, Pascal Furet, Thomas Knöpfel, Catherine Leblanc, Lv Liao, Robert Mah, Pierre Nimsgern, Sebastien Ripoche, Jing Xiong, Bo Han, Can Wang, Xianglin Zhao
  • Publication number: 20150111871
    Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Application
    Filed: October 16, 2014
    Publication date: April 23, 2015
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Paul S. Charifson, Kevin Michael Cottrell, Hongbo Deng, John P. Duffy, Huai Gao, Simon Giroux, Jeremy Green, Katrina Lee Jackson, Joseph M. Kennedy, David J. Lauffer, Mark Willem Ledeboer, Pan Li, John Patrick Maxwell, Mark A. Morris, Albert Charles Pierce, Nathan D. Waal, Jinwang Xu
  • Publication number: 20150111877
    Abstract: The invention provides tetrahydronaphthyridine and related compounds, pharmaceutical compositions, methods of inhibiting ROR? activity, reducing the amount of IL-17 in a subject, and treating immune disorders and inflammatory disorders using such tetrahydronaphthyridine and related compounds.
    Type: Application
    Filed: May 7, 2013
    Publication date: April 23, 2015
    Inventors: Thomas D. Aicher, Kenneth J. Barr, Blair T. Lapointe, Valdimir Simov, Karin A. Stein, William D. Thomas, Peter L. Toogood, Chad A. Van Huis, Catherine M. White
  • Publication number: 20150111886
    Abstract: The invention relates to a compound of formula (I) wherein A1, R1 and R2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Application
    Filed: December 22, 2014
    Publication date: April 23, 2015
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Atsushi Kimbara, Uwe Grether, Matthias Nettekoven, Bernd Puellmann, Mark Rogers-Evans, Tanja Schulz-Gasch
  • Publication number: 20150111885
    Abstract: The present invention relates to substituted heterocyclic derivative compounds, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibition of bromodomain-mediated recognition of acetyl lysine regions of proteins, such as histones. Said compositions and methods are useful for the treatment of cancer and neoplastic disease.
    Type: Application
    Filed: October 17, 2014
    Publication date: April 23, 2015
    Inventors: Michael John Bennett, Juan Manuel Betancort, Amogh Boloor, Stephen W. Kaldor, Jeffrey Alan Stafford, James Marvin Veal
  • Patent number: 9012447
    Abstract: The present invention provides 5-HT3 receptor antagonists of Formula (I): which are useful for the treatment of diseases treatable by inhibition of 5-HT3 receptor such as emesis, pain, drug addiction, neurodegenerative and psychiatric disorders, and GI disorders. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
    Type: Grant
    Filed: July 16, 2013
    Date of Patent: April 21, 2015
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Stephen Hitchcock, Holger Monenschein, Holly Reichard, Huikai Sun, Shota Kikuchi, Todd Macklin, Maria Hopkins
  • Publication number: 20150104384
    Abstract: The present invention relates to certain amido-benzyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
    Type: Application
    Filed: March 1, 2013
    Publication date: April 16, 2015
    Inventors: Kenneth W. Bair, Timm R. Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Peter Dragovich, Francis Gosselin, Janet Gunzner-Toste, Bingsong Han, Jian Lin, Xiongcai Liu, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Mark Zak, Yamin Zhang, Guiling Zao, Xiaozhang Zheng, Po-Wai Yuen
  • Publication number: 20150105374
    Abstract: The present application relates to novel substituted annellated pyrimidines, methods for production thereof, use thereof alone or in combinations for treating and/or preventing diseases and use thereof for the production of medicinal products for treating and/or preventing diseases, in particular for treating and/or preventing cardiovascular diseases.
    Type: Application
    Filed: September 19, 2014
    Publication date: April 16, 2015
    Inventors: Markus FOLLMANN, Johannes-Peter STASCH, Gorden REDLICH, Nils GRIEBENOW, Dieter LANG, Frank WUNDER, Walter HÜBSCH, Niels LINDNER, Alexandros VAKALOPOULOS, Adrian TERSTEEGEN
  • Publication number: 20150105549
    Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, X is CH or N; Y is C(O) or S(O)2; provided that when Y is S(O)2, then X is CH; A is a radical selected from the group consisting of and B1, B2, B3, T, R1, R2R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and R13 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: December 17, 2014
    Publication date: April 16, 2015
    Inventors: KANU MAGANBHAI PATEL, Thomas Paul Selby, Brenton Todd Smith, Andrew Edmund Taggi, Patrick Ryan Kovacs
  • Patent number: 9006235
    Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.
    Type: Grant
    Filed: March 1, 2013
    Date of Patent: April 14, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Zhizhen Barbara Zheng, Stanley D'Andrea, David R. Langley, B. Narasimhulu Naidu
  • Publication number: 20150099737
    Abstract: The invention is directed to novel pyrrolopyrimidine compounds of formula (1) wherein R1, R2y, R4, R8-R11, A and L are defined herein and to salts, including pharmaceutically acceptable salts thereof. The compounds of the present invention are CDK4/6 inhibitors and could be useful in the treatment of diseases and disorders mediated by CDK4/6, such as cancer, including mantle cell lymphoma, liposarcoma, non small cell lung cancer, melanoma, squamous cell esophageal cancer and breast cancer. The invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CDK4/6 activity and to the treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
    Type: Application
    Filed: December 12, 2014
    Publication date: April 9, 2015
    Applicant: NOVARTIS AG
    Inventors: Christopher Thomas BRAIN, Young Shin CHO, John William GIRALDES, Bharat LAGU, Julian Roy LEVELL, Michael Joseph LUZZIO, Lawrence Blas PEREZ, Yaping WANG, Fan YANG
  • Publication number: 20150099631
    Abstract: The present invention relates to a novel crystalline form A of 1,5-dimethyl-6-thioxo-3-(2,2,7-trifluoro-3-oxo-4-(prop-2-ynyl)-3,4-dihydro-2H-benzo[b][1,4]oxazin-6-yl)-1,3,5-triazinane-2,4-dione. The invention also relates to a process for the production of this crystalline form and formulations for plant protection which contains the novel crystalline form of 1,5-dimethyl-6-thioxo-3-(2,2,7-trifluoro-3-oxo-4-(prop-2-ynyl)-3,4-dihydro-2H-benzo[b][1,4]oxazin-6-yl)-1,3,5-triazinane-2,4-dione.
    Type: Application
    Filed: May 15, 2013
    Publication date: April 9, 2015
    Inventors: Robert Reinhard, Tiziana Chiodo, Bernd Wolf, Stefan Scherer, Matthias Bratz, Matthias Witschel, Trevor William Newton, Thomas Seitz
  • Patent number: 9000152
    Abstract: The present invention relates to a process for manufacturing triazinon-benzoxazinones of formula (I), by reacting amino-benzoxazinones of formula (II) with 1,1?-carbonyldiimidazole (CDI) and a (thio)urea compound of formula (III); wherein the variables are defined according to the description.
    Type: Grant
    Filed: December 20, 2012
    Date of Patent: April 7, 2015
    Assignee: BASF SE
    Inventors: Bernd Wolf, Volker Maywald, Uwe Josef Vogelbacher, Michael Rack, Maximilian Dochnahl, Michael Keil, Timo Frassetto, Joachim Gebhardt
  • Publication number: 20150094302
    Abstract: Alkylated piperazine compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating cancer mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of cancer in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: December 11, 2014
    Publication date: April 2, 2015
    Applicant: Genentech, Inc.
    Inventors: James John Crawford, Wendy B. Young
  • Patent number: 8993072
    Abstract: Described herein are precursors and methods of forming films. In one aspect, there is provided a precursor having Formula I: XmR1nHpSi(NR2R3)4-m-n-p??I wherein X is selected from Cl, Br, I; R1 is selected from linear or branched C1-C10 alkyl group, a C2-C12 alkenyl group, a C2-C12 alkynyl group, a C4-C10 cyclic alkyl, and a C6-C10 aryl group; R2 is selected from a linear or branched C1-C10 alkyl, a C3-C12 alkenyl group, a C3-C12 alkynyl group, a C4-C10 cyclic alkyl group, and a C6-C10 aryl group; R3 is selected from a branched C3-C10 alkyl group, a C3-C12 alkenyl group, a C3-C12 alkynyl group, a C4-C10 cyclic alkyl group, and a C6-C10 aryl group; m is 1 or 2; n is 0, 1, or 2; p is 0, 1 or 2; and m+n+p is less than 4, wherein R2 and R3 are linked or not linked to form a ring.
    Type: Grant
    Filed: September 18, 2012
    Date of Patent: March 31, 2015
    Assignee: Air Products and Chemicals, Inc.
    Inventors: Manchao Xiao, Xinjian Lei, Mark Leonard O'Neill, Bing Han, Ronald Martin Pearlstein, Haripin Chandra, Heather Regina Bowen, Agnes Derecskei-Kovacs
  • Publication number: 20150087585
    Abstract: Derivatives of purine, 3H-imidazo[4,5-b]pyrimidine and 1H-imidazo[4,5-d]pyrazine of Formula I that inhibit the activity of the diacylglycerol acyltransferase 2 (DGAT2) and their uses in the treatment of diseases linked thereto in animals are described herein.
    Type: Application
    Filed: March 26, 2013
    Publication date: March 26, 2015
    Applicant: PFIZER INC.
    Inventors: Kay Ahn, Markus Boehm, Shawn Cabral, Philip A. Carpino, Kentaro Futatsugi, David Hepworth, Daniel W. Kung, Suvi Orr, Jian Wang
  • Patent number: 8987170
    Abstract: A compound represented by formula (1): is effective for controlling Pythium spp., and it is useful for controlling Pythium spp. and protecting crops from pythium diseases.
    Type: Grant
    Filed: August 19, 2014
    Date of Patent: March 24, 2015
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Shigeyuki Itoh, Ryo Ishikawa
  • Patent number: 8987250
    Abstract: Compounds disclosed herein including compounds of formula I?: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.
    Type: Grant
    Filed: April 19, 2013
    Date of Patent: March 24, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Kerim Babaoglu, Gediminas Brizgys, Jake Cha, Xiaowu Chen, Hongyan Guo, Randall L. Halcomb, Xiaochun Han, Richard Huang, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu, Hong Yang
  • Publication number: 20150080374
    Abstract: This invention relates to novel 2,3-dihydroimidazo[1,2-c]quinazoline compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for phosphotidylinositol-3-kinase (PI3K) inhibition and treating diseases associated with phosphotidylinositol-3-kinase (PI3K) activity, in particular treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: November 25, 2014
    Publication date: March 19, 2015
    Inventors: William Scott, Ningshu LIU, Manfred MÖWES, Andrea HÄGEBARTH, Ursula MÖNNING, Ulf BÖMER