Bicyclo Ring System Having The Oxazine Ring As One Of The Cyclos (e.g., Benzoxazines, Etc.) Patents (Class 544/105)
  • Patent number: 10370330
    Abstract: A method for producing (2S,5S)/(2R,5R)-5-hydroxypiperidine-2-carboxylic acid represented by the formula (10) below: the method comprising the step of removing the protecting group from the hydroxyl group in a compound represented by the formula (7) below: (wherein P represents a protecting group, R3 represents an alkyl group containing 1 to 4 carbon atoms, and A represents an alkyl group containing 1 to 10 carbon atoms, an aryl group containing 6 to 12 carbon atoms, an alkyloxy group containing 1 to 4 carbon atoms, or an aralkyloxy group containing 7 to 20 carbon atoms) to synthesize a compound represented by the formula (8) below: (wherein R3 represents an alkyl group containing 1 to 4 carbon atoms, and A represents an alkyl group containing 1 to 10 carbon atoms, an aryl group containing 6 to 12 carbon atoms, an alkyloxy group containing 1 to 4 carbon atoms, or an aralkyloxy group containing 7 to 20 carbon atoms).
    Type: Grant
    Filed: April 27, 2018
    Date of Patent: August 6, 2019
    Assignee: API CORPORATION
    Inventors: Jun Takehara, Masato Murai, Takashi Ohtani, Tomoko Maeda, Tsugihiko Hidaka
  • Patent number: 10364237
    Abstract: The invention provides tetrahydroquinoline sulfonamide compounds, tetrahydronaphthalene sulfonyl compounds, and related compounds, pharmaceutical compositions, methods of promoting RORy activity, methods of increasing the amount of IL-17 in a subject, and methods of treating cancer and other medical disorders using such compounds.
    Type: Grant
    Filed: December 20, 2017
    Date of Patent: July 30, 2019
    Assignee: Lycera Corporation
    Inventors: Thomas D. Aicher, Clarke B. Taylor, Chad A. VanHuis
  • Patent number: 10329257
    Abstract: The present invention provides compounds for the treatment of a bacterial infection. Additionally, the present invention provides compositions and methods for using these compounds and compositions in the treatment of a bacterial infection in a subject.
    Type: Grant
    Filed: August 12, 2016
    Date of Patent: June 25, 2019
    Assignee: The Broad Institute, Inc.
    Inventors: Michael H. Serrano-Wu, Chao Fang
  • Patent number: 10308620
    Abstract: The present invention relates to compound of formula (I), or stereoisomers and pharmaceutically acceptable salts as muscarinic M1 receptor positive allosteric modulators. This invention also relates to methods of preparing such compounds and pharmaceutical compositions comprising such compounds. The compounds of this invention are useful in the treatment of various disorders that are related to muscarinic M1 receptor.
    Type: Grant
    Filed: June 8, 2016
    Date of Patent: June 4, 2019
    Assignee: SUVEN LIFE SCIENCES LIMITED
    Inventors: Ramakrishna Nirogi, Abdul Rasheed Mohammed, Anil Karbhari Shinde, Shankar Reddy Gagginapally, Venkateswarlu Jasti
  • Patent number: 10294222
    Abstract: Compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.
    Type: Grant
    Filed: September 1, 2017
    Date of Patent: May 21, 2019
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Andrew Felts
  • Patent number: 10266528
    Abstract: The present invention relates to imidazo pyridine compounds, and pharmaceutically acceptable compositions thereof, useful as BTK inhibitors.
    Type: Grant
    Filed: August 15, 2017
    Date of Patent: April 23, 2019
    Assignee: Merck Patent GmbH
    Inventor: Richard D. Caldwell
  • Patent number: 10150742
    Abstract: Disclosed herein are pyrimidine compounds of formula I and formula II and methods for treating or preventing a viral infection, such as infections caused by dengue virus in a subject, comprising administering to said subject an effective amount of a pyrimidine compound of formula I or formula II.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: December 11, 2018
    Assignees: President and Fellows of Harvard College, Dana-Farber Cancer Institute, Inc.
    Inventors: Priscilla Yang, Nathanael S. Gray, Chandrasekhar Miduturu, Margaret J. Clark
  • Patent number: 10125231
    Abstract: A method of forming carbon-carbon composites includes molding carbon fibers with a compound comprising a blend of benzoxazine resin and cyanate ester resin; and pyrolyzing the compound to form the carbon-carbon composite. A carbon-carbon composite includes carbon fibers impregnated with a compound comprising a blend of benzoxazine resin and cyanate ester.
    Type: Grant
    Filed: September 27, 2016
    Date of Patent: November 13, 2018
    Assignee: RAYTHEON COMPANY
    Inventor: Gray E. Fowler
  • Patent number: 10087150
    Abstract: The present invention provides a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity, which may be useful as a prophylactic or therapeutic drug for Alzheimer's disease, schizophrenia, pain, sleep disorder, Parkinson's disease dementia, dementia with Lewy bodies and the like. The present invention relates to a compound represented by the formula (I) or a salt thereof: wherein each symbol is as defined in the attached DESCRIPTION.
    Type: Grant
    Filed: October 31, 2017
    Date of Patent: October 2, 2018
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Takahiro Sugimoto, Shinkichi Suzuki, Hiroki Sakamoto, Masami Yamada, Minoru Nakamura, Makoto Kamata, Kenichiro Shimokawa, Takuto Kojima
  • Patent number: 10087169
    Abstract: Compounds and compositions comprising compounds that activate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that activate PKM2 in the treatment of cancer.
    Type: Grant
    Filed: July 10, 2017
    Date of Patent: October 2, 2018
    Assignee: Agios Pharmaceuticals, Inc.
    Inventors: Francesco G. Salituro, Jeffrey O. Saunders
  • Patent number: 10065928
    Abstract: Provided herein are a quinolinone compound, pharmaceutical composition thereof, and use of the compound or the pharmaceutical composition in drug preparation, the drug being used to prevent, manage, treat or relieve diseases related to HIF and/or EPO of a patient, including anemia, vascular disease, myocardial ischemia, dysmetabolism, or for wound healing.
    Type: Grant
    Filed: September 1, 2015
    Date of Patent: September 4, 2018
    Assignee: SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Yinglin Zuo, Xiaojun Wang, Yingjun Zhang, Liang Wen, Shoutao Wu, Xiaofeng Yuan
  • Patent number: 10045985
    Abstract: The present invention relates to pyrimidine compounds, and pharmaceutically acceptable compositions thereof, useful as BTK inhibitors.
    Type: Grant
    Filed: July 8, 2016
    Date of Patent: August 14, 2018
    Assignee: Merck Patent GmbH
    Inventors: Hui Qiu, Richard D. Caldwell, Lesley Liu-Bujalski
  • Patent number: 9988351
    Abstract: A method for producing (2S,5S)/(2R,5R)-5-hydroxypiperidine-2-carboxylic acid represented by the formula (10) below: the method including removing the protecting group from the hydroxyl group in a compound represented by formula (7) below: (wherein P represents a protecting group, R3 represents an alkyl group containing 1 to 4 carbon atoms, and A represents an alkyl group containing 1 to 10 carbon atoms, an aryl group containing 6 to 12 carbon atoms, an alkyloxy group containing 1 to 4 carbon atoms, or an aralkyloxy group containing 7 to 20 carbon atoms) to synthesize a compound represented by formula (8) below: (wherein R3 represents an alkyl group containing 1 to 4 carbon atoms, and A represents an alkyl group containing 1 to 10 carbon atoms, an aryl group containing 6 to 12 carbon atoms, an alkyloxy group containing 1 to 4 carbon atoms, or an aralkyloxy group containing 7 to 20 carbon atoms).
    Type: Grant
    Filed: September 15, 2017
    Date of Patent: June 5, 2018
    Assignee: API CORPORATION
    Inventors: Jun Takehara, Masato Murai, Takashi Ohtani, Tomoko Maeda, Tsugihiko Hidaka
  • Patent number: 9957268
    Abstract: The present invention relates to substituted pyrrolopyridinones and substituted pyrazolopyridinones 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: Grant
    Filed: November 17, 2016
    Date of Patent: May 1, 2018
    Assignee: Incyte Corporation
    Inventors: Andrew P. Combs, Thomas P. Maduskuie, Jr., Nikoo Falahatpisheh
  • Patent number: 9949976
    Abstract: The invention relates to a CDK4/6 kinase inhibitor, or a pharmaceutically acceptable salt, ester, or solvate thereof, or their isomers; a pharmaceutical formulation, pharmaceutical composition and kit comprising said CDK4/6 kinase inhibitor, or a pharmaceutically acceptable salt, ester, or solvate thereof, or their isomers, and use of said CDK4/6 kinase inhibitor, or a pharmaceutically acceptable salt, ester, or solvate thereof, or their isomers. For example, the compounds of the invention are useful for reducing or inhibiting the activity of CDK4/6 kinase in a cell, and/or treating and/or preventing a cancer-related disease mediated by CDK4/6 kinase.
    Type: Grant
    Filed: September 14, 2017
    Date of Patent: April 24, 2018
    Assignees: XUANZHU PHARMA CO., LTD., SIHUAN PHARMACEUTICAL HOLDINGS GROUP LTD.
    Inventors: Frank Wu, Bo Chen
  • Patent number: 9896441
    Abstract: The invention provides tetrahydroquinoline sulfonamide compounds, tetrahydronaphthalene sulfonyl compounds, and related compounds, pharmaceutical compositions, methods of promoting ROR? activity, methods of increasing the amount of IL-17 in a subject, and methods of treating cancer and other medical disorders using such compounds.
    Type: Grant
    Filed: May 5, 2015
    Date of Patent: February 20, 2018
    Assignee: LYCERA CORPORATION
    Inventors: Thomas D. Aicher, Clarke B. Taylor, Chad A. VanHuis
  • Patent number: 9890154
    Abstract: A series of substituted 3H-imidazo[4,5-c]pyridine derivatives of formula (I), being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
    Type: Grant
    Filed: December 8, 2014
    Date of Patent: February 13, 2018
    Assignee: UCB Biopharma SPRL
    Inventors: Victoria Elizabeth Jackson, Boris Kroeplien, John Robert Porter
  • Patent number: 9878989
    Abstract: The present invention provides a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity, which may be useful as a prophylactic or therapeutic drug for Alzheimer's disease, schizophrenia, pain, sleep disorder, Parkinson's disease dementia, dementia with Lewy bodies and the like. The present invention relates to a compound represented by the formula (I) or a salt thereof: wherein each symbol is as defined in the attached DESCRIPTION.
    Type: Grant
    Filed: June 23, 2016
    Date of Patent: January 30, 2018
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Takahiro Sugimoto, Shinkichi Suzuki, Hiroki Sakamoto, Masami Yamada, Minoru Nakamura, Makoto Kamata, Kenichiro Shimokawa, Masataka Murakami, Jinichi Yonemori, Takuto Kojima
  • Patent number: 9822085
    Abstract: A tetrazolinone compound represented by formula (1): [in the formula, R1 represents an alkyl group having 1-6 carbon atoms or the like] can be produced by reacting a compound represented by formula (2): [in the formula, X1 represents a bromine atom or the like, and R1 represents an alkyl group having 1-6 carbon atoms or the like] with a compound represented by formula (A): R—Mg—X??(A) [in the formula, R represents an alkyl group having 1-6 carbon atoms or the like, and X1 represents a bromine atom or the like] to provide a compound represented by formula (3): [in the formula, X2 represents a chlorine atom or the like] and reacting the compound represented by formula (3) with formaldehyde or a compound represented by formula (4): [in the formula, R6 represents an alkyl group having 1-6 carbon atoms or the like, and X3 represents a chlorine atom, bromine atom or iodine atom].
    Type: Grant
    Filed: March 3, 2015
    Date of Patent: November 21, 2017
    Assignee: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Satoru Ujita, Takayuki Shioda
  • Patent number: 9809561
    Abstract: The invention provides certain bicylic heterocyclic compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein X1, X2, R1, R2, R3, R4, and Cy are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds of the Formula (I) or pharmaceutically acceptable salts thereof, and methods of using the compounds of the Formula (I) or pharmaceutically acceptable salts thereof or pharmaceutical compositions comprising the same for treating diseases or conditions mediated by RORgammaT.
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: November 7, 2017
    Assignees: MERCK SHARP & DOHME CORP., LYCERA CORPORATION
    Inventors: Thomas D. Aicher, Chad A. VanHuis, William D. Thomas, John K. MacLean, Brian M. Andresen, Kenneth J. Barr, Corey E. Bienstock, Neville J. Anthony, Matthew Daniels, Kun Liu, Yuan Liu, Catherine M. White, Blair T. Lapointe, Nunzio Sciammetta, Vladimir Simov
  • Patent number: 9783511
    Abstract: The invention provides certain benzoxazine compounds of the Formula (I) or pharmaceutically acceptable salts thereof wherein R1, R2, Ra1, Ra2, Rb1, Rb2, Rc, Rd, and Cy are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds of the Formula (I) or pharmaceutically acceptable salts thereof, and methods of using the compounds of the Formula (I) or pharmaceutically acceptable salts thereof or pharmaceutical compositions comprising the same for treating diseases or conditions mediated by RORgammaT.
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: October 10, 2017
    Assignees: Lycera Corporation, Merck Sharp & Dohme Corp.
    Inventors: Thomas D. Aicher, Chad A. VanHuis, John MacLean, Brian M. Andresen, Kenneth J. Barr, Corey Bienstock, Matthew Daniels, Kun Liu, Yuan Liu, Catherine White, Nunzio Sciammetta, Vladimir Simov
  • Patent number: 9763952
    Abstract: The invention relates to dihydro-benzo-oxazine and dihydro-pyrido-oxazine compounds of the formula (I) and/or pharmaceutically acceptable salts and/or solvates thereof, wherein Y, V, W, U, Q, R1, R5, R7 and R30 are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.
    Type: Grant
    Filed: December 21, 2015
    Date of Patent: September 19, 2017
    Assignee: NOVARTIS AG
    Inventors: Giorgio Caravatti, Sylvie Chamoin, Pascal Furet, Klemens Hogenauer, Konstanze Hurth, Karen Kammertoens, Ian Lewis, Henrik Moebitz, Alexander Baxter Smith, Nicolas Soldermann, Romain Wolf, Frederic Zecri
  • Patent number: 9751846
    Abstract: The present invention provides an industrially advantageous method for producing a 1,4-benzoxazine compound useful as a medicine while avoiding safety and health risks. Specifically, the present invention provides a method for producing a 1,4-benzoxazine compound [A], which comprises the three steps in the following scheme, namely, a step of converting the amino group at 7-position in a compound [a] into a dimesylamino group, a step of coupling a compound [b] with a boronic acid compound, and a step of converting the 7-position in a compound [c] into a monomesylamino group. In the above scheme, Ms is a methanesulfonyl group, and each of R? and R? is a hydrogen atom etc.
    Type: Grant
    Filed: July 8, 2016
    Date of Patent: September 5, 2017
    Assignee: MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Tomoyuki Okabe, Takeshi Hamada, Kaori Tomikawa, Yukie Okamoto, Toru Iijima, Hidenori Akatsuka, Kenichi Toyama, Atsushi Moroda, Yoshihiro Sugiura
  • Patent number: 9738612
    Abstract: Disclosed are a use of a methylacryloyl benzimidazolone derivative, an optical isomer or a pharmaceutically acceptable salt or prodrug thereof in the preparation of: (a) a pharmaceutical composition or reagent for down-regulating the activity of PI3K/Akt pathways; (b) a pharmaceutical composition or reagent for treating or inhibiting a tumour; and/or inhibiting tumour cell growth; and/or (c) a pharmaceutical composition or reagent for blocking the cell cycle. The compounds involved in the present invention can down-regulate the level of Akt phosphorylation in P13K/Akt signaling pathways, and the functional effects of the compounds are equivalent to those of a novel small-molecular targeting drug MK2206; while the research at the cellular level has found that the methylacryloyl benzimidazolone derivatives represented by FD1 have a good proliferation inhibiting effect on tumour cells. What is different from MK2206 is that FD1 has better effects on a PTEN deleted cell.
    Type: Grant
    Filed: March 23, 2015
    Date of Patent: August 22, 2017
    Assignees: Shanghai Nature Standard R&D and Biotech Co., Ltd, Shanghai Standard Technology Co., Ltd., Shanghai Founder Biomed R&D Co., Ltd.
    Inventors: Jiapeng Li, Zhiqin Ji, Xiaoya Zhou, Shaopeng Wei, Yong Qian, Tianpei Xie
  • Patent number: 9695204
    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: June 10, 2016
    Date of Patent: July 4, 2017
    Assignee: Rigel Pharmaceuticals, Inc.
    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: 9598382
    Abstract: A method for producing a purified compound represented by the formula (II), comprising; obtaining a reaction mixture containing a compound represented by the formula (I) from a crude compound represented by the formula (II) such as reacting the crude compound with a ketone compound, and reacting the obtained reaction mixture or a solution by filtering thus obtained reaction mixture containing the compound represented by the formula (I) with water.
    Type: Grant
    Filed: December 25, 2014
    Date of Patent: March 21, 2017
    Assignee: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Tadafumi Matsunaga, Hiromi Kaise
  • Patent number: 9567305
    Abstract: The present invention provides oxazine compounds, method of using and method of making oxazine compounds and its pharmaceutical use.
    Type: Grant
    Filed: January 20, 2014
    Date of Patent: February 14, 2017
    Assignee: Southern Methodist University
    Inventors: Edward R. Biehl, Haribabu Ankati, Sukanta Kamila
  • Patent number: 9539260
    Abstract: The invention relates to dihydro-benzo-oxazine and dihydro-pyrido-oxazine compounds of the formula (I) and/or pharmaceutically acceptable salts and/or solvates thereof, wherein Y, V, W, U, Q, R1, R5, R7 and R30 are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.
    Type: Grant
    Filed: December 20, 2012
    Date of Patent: January 10, 2017
    Assignee: NOVARTIS AG
    Inventors: Giorgio Caravatti, Sylvie Chamoin, Pascal Furet, Klemens Hogenauer, Konstanze Hurth, Karen Kammertoens, Ian Lewis, Henrik Moebitz, Alexander Baxter Smith, Nicolas Soldermann, Romain Wolf, Frederic Zecri
  • Patent number: 9518045
    Abstract: The present invention relates to a process for manufacturing benzoxazinones of formula (I), wherein the variables are defined according to the description, by reacting carbamates of formula (II) are reacted with carbamat-benzoxazinones of formula (III) in the presence of a base.
    Type: Grant
    Filed: August 9, 2013
    Date of Patent: December 13, 2016
    Assignee: BASF SE
    Inventors: Maximilian Dochnahl, Roland Goetz, Joachim Gebhardt, Uwe Josef Vogelbacher, Timo Frassetto, Michael Rack, Volker Maywald, Bernd Wolf
  • Patent number: 9456606
    Abstract: The present invention relates to pesticidal mixtures comprising a component A and a component B, wherein component A is a compound of formula (I) wherein B1, B2, B3, X1, X2, X3, X4, Y1, Y2, Y3 and R9 are as defined in claim 1 and component B is an insecticide. The present invention also relates to methods of using said mixtures for the control of plant pests.
    Type: Grant
    Filed: December 12, 2012
    Date of Patent: October 4, 2016
    Assignee: Syngenta Participations AG
    Inventors: Myriem El Qacemi, Jerome Yves Cassayre
  • Patent number: 9446012
    Abstract: This invention relates to novel substituted nitrocatechol derivatives, their use in the treatment of some central and peripheral nervous system disorders and pharmaceutical compositions containing them.
    Type: Grant
    Filed: August 30, 2013
    Date of Patent: September 20, 2016
    Assignee: BIAL—PORTELA & CA, S.A.
    Inventors: David Alexander Learmonth, Laszlo Erno Kiss, Pedro Nuno Leal Palma, Humberto dos Santos Ferreira, Patricio Manuel V. A. Soares da Silva
  • Patent number: 9409874
    Abstract: The present invention provides an industrially advantageous method for producing a 1,4-benzoxazine compound useful as a medicine while avoiding safety and health risks. Specifically, the present invention provides a method for producing a 1,4-benzoxazine compound [A], which comprises the three steps in the following scheme, namely, a step of converting the amino group at 7-position in a compound [a] into a dimesylamino group, a step of coupling a compound [b] with a boronic acid compound, and a step of converting the 7-position in a compound [c] into a monomesylamino group. In the above scheme, Ms is a methanesulfonyl group, and each of R? and R? is a hydrogen atom etc.
    Type: Grant
    Filed: August 8, 2013
    Date of Patent: August 9, 2016
    Assignee: MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Tomoyuki Okabe, Takeshi Hamada, Kaori Tomikawa, Yukie Okamoto, Toru Iijima, Hidenori Akatsuka, Kenichi Toyama, Atsushi Moroda, Yoshihiro Sugiura
  • Patent number: 9409894
    Abstract: The present invention relates to carbamates of formula (I), wherein the variables are defined according to the description, as well as to a process for manufacturing carbamates of formula (I), and to the use of carbamates of formula (I) in manufacturing benzoxazinones of formula (VII).
    Type: Grant
    Filed: July 29, 2013
    Date of Patent: August 9, 2016
    Assignee: BASF SE
    Inventors: Maximilian Dochnahl, Roland Götz, Joachim Gebhardt, Uwe Josef Vogelbacher, Timo Frassetto, Michael Rack, Volker Maywald, Bernd Wolf
  • Patent number: 9394315
    Abstract: The invention provides tetrahydro[1,8]naphthyridine and related compounds, pharmaceutical compositions, methods of promoting ROR? activity, increasing the amount of IL-17 in a subject, and treating cancer, bacterial infections, and fungal infections using such tetrahydro[1,8]naphthyridine and related compounds.
    Type: Grant
    Filed: May 8, 2013
    Date of Patent: July 19, 2016
    Assignee: Lycera Corporation
    Inventors: Thomas D. Aicher, Peter L. Toogood, Xiao Hu
  • 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: 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: 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
  • 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