Chalcogen Bonded Directly To Diazine Ring Carbon Patents (Class 544/298)
  • Patent number: 11013742
    Abstract: The present invention relates to a cholesteryl ester transfer protein (CETP) inhibitor: (hereinafter referred to as Compound A) for use in the treatment of subjects suffering from or having an increased risk for cardiovascular diseases, in particular hyperlipidemia or mixed dyslipidemia. A further aspect of the present invention relates to a pharmaceutical composition for use in the treatment of subjects suffering from or having an increased risk for cardiovascular diseases, wherein the composition comprises a therapeutically effective amount of said Compound A CETP inhibitor.
    Type: Grant
    Filed: April 9, 2020
    Date of Patent: May 25, 2021
    Assignee: DEZIMA PHARMA B.V.
    Inventors: John Ford, Patrick Round, John Kastelein, Atsuhiro Kawaguchi, Koichi Tomiyasu, Kozo Oka
  • Patent number: 10851068
    Abstract: A method for preparing a pyrimidone compound and an important intermediate in which raw materials of the preparation method are cheap, the reaction condition of preparation method is mild, the preparation method is simple to operate, and is safe and controllable, has high total yield, and thus is suitable for industrial production.
    Type: Grant
    Filed: July 3, 2018
    Date of Patent: December 1, 2020
    Assignee: SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Runfeng Lin, Xiaojun Wang, Jihua Lin, Liang Chen, Yingjun Zhang, Jiancun Zhang
  • Patent number: 10662162
    Abstract: The present disclosure provides pyrimidine compounds of Formula 1 and uses thereof for example, for the potential treatment of diseases associated with P2X purinergic receptors. In certain aspects, the present disclosure provides P2X3 and/or P2X2/3 antagonists which are useful, for example, for the potential treatment of visceral organ, cardiovascular and pain-related diseases, conditions and disorders.
    Type: Grant
    Filed: March 20, 2017
    Date of Patent: May 26, 2020
    Assignee: Afferent Pharmaceuticals, Inc.
    Inventors: Ronald Charles Hawley, Prabha Ibrahim, Anthony P. Ford, Joel R. Gever
  • Patent number: 10653692
    Abstract: The present invention relates to a cholesteryl ester transfer protein (CETP) inhibitor: (hereinafter referred to as Compound A) for use in the treatment of subjects suffering from or having an increased risk for cardiovascular diseases, in particular hyperlipidemia or mixed dyslipidemia. A further aspect of the present invention relates to a pharmaceutical composition for use in the treatment of subjects suffering from or having an increased risk for cardiovascular diseases, wherein the composition comprises a therapeutically effective amount of said Compound A CETP inhibitor.
    Type: Grant
    Filed: February 5, 2014
    Date of Patent: May 19, 2020
    Assignee: DEZIMA PHARMA BV
    Inventors: John Ford, Patrick Round, John Kastelein, Atsuhiro Kawaguchi, Koichi Tomiyasu, Kozo Oka
  • Patent number: 10647684
    Abstract: This invention relates to 2-aminopyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.
    Type: Grant
    Filed: April 12, 2019
    Date of Patent: May 12, 2020
    Assignee: JANSSEN SCIENCES IRELAND UNLIMITED COMPANY
    Inventors: David Craig McGowan, Pierre Jean-Marie Bernard Raboisson, Tim Hugo Maria Jonckers
  • Patent number: 10538533
    Abstract: The present invention provides a compound of formula I: and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, L1, L2, m, and n, are as described in the specification. Such compounds are inhibitors of VPS34 and thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Grant
    Filed: August 1, 2017
    Date of Patent: January 21, 2020
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Indu T. Bharathan, Chris Blackburn, Jeffrey P. Ciavarri, Jouhara Chouitar, Courtney A. Cullis, Natalie D'Amore, Paul E. Fleming, Kenneth M. Gigstad, Krista E. Gipson, Mario Girard, Yongbo Hu, Janice Lee, Gang Li, Mansoureh Rezaei, Michael D. Sintchak, Francois Soucy, Stephen G. Stroud, Tricia J. Vos, Tzu-Tshin Wong, He Xu, Tianlin Xu, Yingchun Ye
  • Patent number: 10494343
    Abstract: The present invention relates to a novel organic compound, a near-infrared fluorescent constant medium containing the same, and a method for nano-granulating the constant medium.
    Type: Grant
    Filed: January 11, 2016
    Date of Patent: December 3, 2019
    Assignees: COLLEGE OF MEDICINE POCHON CHA UNIV. INDUSTRY-ACADEMIC COOPERATION FOUNDATION, CHAMEDITECH CO., LTD.
    Inventors: Tae Jong Yoon, Kwang Hoe Chung, Jeongbeob Seo, Sin Wook Kang, Kwang Hyuong Lee, Yong Su Kwon, Hye Sun Jeon, Chae Woon Lee, Jin Sung Kim
  • Patent number: 10259793
    Abstract: This invention relates to 2-aminopyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.
    Type: Grant
    Filed: March 20, 2017
    Date of Patent: April 16, 2019
    Assignee: Janssen Sciences Ireland UC
    Inventors: David Craig McGowan, Pierre Jean-Marie Bernard Raboisson, Tim Hugo Maria Jonckers
  • Patent number: 10112904
    Abstract: The present invention relates to a process for the preparation of synthetic intermediates which may be used in the preparation of tetrahydroquinoline derivatives, which derivatives have an inhibitory activity against cholesteryl transfer protein (CETP), show effects of increasing HDL cholesterol level and decreasing LDL cholesterol level, and can be used for the treatment and/or prevention of diseases such as arteriosclerotic diseases, hyperlipidemia, dyslipidemia and the like.
    Type: Grant
    Filed: July 29, 2015
    Date of Patent: October 30, 2018
    Assignee: DEZIMA PHARMA B.V.
    Inventors: John Ford, Johannes Paulus Gerardus Seerden, Amandine Ledru
  • Patent number: 9598378
    Abstract: This invention relates to 2-aminopyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.
    Type: Grant
    Filed: February 20, 2014
    Date of Patent: March 21, 2017
    Assignee: Janssen Sciences Ireland UC
    Inventors: David Craig McGowan, Pierre Jean-Marie Bernard Raboisson, Tim Hugo Maria Jonckers
  • Patent number: 9556127
    Abstract: Compounds and methods for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a compound of formula (I): or a pharmaceutically acceptable salt, solvate or prodrug thereof, wherein D, X, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein.
    Type: Grant
    Filed: August 6, 2014
    Date of Patent: January 31, 2017
    Assignee: Roche Palo Alto LLC
    Inventors: Chris Allen Broka, David Scott Carter, Michael Patrick Dillon, Ronald Charles Hawley, Alam Jahangir, Clara Jeou Jen Lin, Daniel Warren Parish
  • Patent number: 9169217
    Abstract: Arylalkyl esters of 4-aminopicolinic acids and 6-amino-4-pyrimidinecarboxylates are herbicides for control of weeds especially those species common to rice and wheat cropping systems and in pasture management programs.
    Type: Grant
    Filed: October 9, 2014
    Date of Patent: October 27, 2015
    Assignee: Dow AgroSciences LLC
    Inventors: Carla N. Yerkes, Christian T. Lowe, Joseph D. Eckelbarger, Jeffrey B. Epp, Katherine A. Guenthenspberger, Thomas L. Siddall, Paul R. Schmitzer
  • Patent number: 9051319
    Abstract: Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I), or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.
    Type: Grant
    Filed: December 6, 2013
    Date of Patent: June 9, 2015
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Paul S. Charifson, Michael P. Clark, Upul K. Bandarage, Randy S. Bethiel, Michael J. Boyd, Ioana Davies, Hongbo Deng, John P. Duffy, Luc J. Farmer, Huai Gao, Wenxin Gu, Joseph M. Kennedy, Brian Ledford, Mark W. Ledeboer, Francois Maltais, Emanuele Perola, Tiansheng Wang
  • Patent number: 9040697
    Abstract: 4,6-dichloro-2-methyl-5-(1-acyl-2-imidazolin-2-yl)-aminopyrimidine is reacted with methanol in the presence of a non-ionic organic base, and moxonidine is obtained directly from the reaction mixture.
    Type: Grant
    Filed: February 5, 2014
    Date of Patent: May 26, 2015
    Assignee: AREVIPHARMA GmbH
    Inventors: Harald Hofmeier, Michael Limmert, Heike Heydemüller, Helge Hartenhauer
  • Publication number: 20150141403
    Abstract: The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.
    Type: Application
    Filed: December 1, 2014
    Publication date: May 21, 2015
    Inventors: Jose Maria CID-NUNEZ, Daniel OEHLRICH, Andres Avelino TRABANCO-SUAREZ, Gary John TRESADERN, Juan Antonio VEGA RAMIRO, Gregor James MACDONALD
  • Publication number: 20150126372
    Abstract: 4-Amino-6-(heterocyclic)picolinic acids and their derivatives; 6-amino-2-(heterocyclic)pyrimidine-4-carboxylates and their derivatives; and methods of using the same as herbicides.
    Type: Application
    Filed: November 13, 2014
    Publication date: May 7, 2015
    Inventors: Joseph D. Eckelbarger, Jeffrey B. Epp, Stephen Craig Fields, Lindsey G. Fischer, Natalie C. Giampietro, Katherine A. Guenthenspberger, Christian T. Lowe, Jeff Petkus, Joshua Roth, Norbet M. Satchivi, Paul R. Schmitzer, Thomas L. Siddall, Nick X. Wang
  • Publication number: 20150112063
    Abstract: The present disclosure provides process for preparation of azimsulfuron or its salts, isomers, and other derivatives thereof. The process involves treating a compound of formula I, with aqueous acetic acid or formic acid and chlorine gas or sodium hypochlorite in presence of hydrochloric acid in chlorinated solvents such as dichloromethane, 1,2-dichloroethane or with aqueous acetic acid and N-chlorosuccinimide or hydrogen peroxide in presence of hydrochloric acid in aqueous cyclic ether such as tetrahydrofuran, 1,4-dioxane to obtain 1-methyl-4-(2-methyl-2H-tetrazol-5-yl)-1H-pyrazole-5-sulfonyl chloride; converting the sulfonyl chloride to a sulfonamide and treating the sulfonamide with a phenyl(4,6-dimethoxypyrimidin-2-yl) carbamate to obtain azimsulfuron or its salts, isomers, and other derivatives thereof.
    Type: Application
    Filed: April 12, 2013
    Publication date: April 23, 2015
    Applicant: RALLIS INDIA LIMITED
    Inventors: Jivan Dhanraj Pawar, Sanjay Sambhajirao Palimkar, B. Sankar, Subhash Rajaram Kadam, Rama Mohan Hindupur, Venkatesh M. Prabhu, Hari Narayan Pati, Vadiraj Gopinath Suphala, Avinash Sheshrao Mane
  • Patent number: 9012451
    Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of formula I, wherein X is CH2 or a single bond; Y is a group of formula and wherein R has the meanings as defined in the specification, which compounds are alpha 7 nicotinic acetylcholine receptor (nAChR) agonists; to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.
    Type: Grant
    Filed: May 2, 2012
    Date of Patent: April 21, 2015
    Assignee: Novartis AG
    Inventors: Dominik Feuerbach, Konstanze Hurth, Timothy John Ritchie
  • Patent number: 9000163
    Abstract: Provided is a method for selectively demethylating a 2-methoxy group. Specifically provided is a production method of a compound represented by formula (7) below through the following reactions.
    Type: Grant
    Filed: October 29, 2013
    Date of Patent: April 7, 2015
    Assignee: Zeria Pharmaceutical Co., Ltd.
    Inventors: Masaaki Nagasawa, Kazuyasu Asami, Ryu Nakao, Nobuyuki Tanaka, Yoshiyuki Aida
  • Publication number: 20150086491
    Abstract: The invention relates to a TRPM8 modulator for achieving a cooling effect on the skin or a mucous membrane.
    Type: Application
    Filed: November 5, 2014
    Publication date: March 26, 2015
    Inventors: Thomas Subkowski, Michael Backes, Heiko Oertling, Arnold Machinek, Hubert Loges, Ulrike Simchen, Horst Surburg, Claus Bollschweiler, Jens Wittenberg, Wolfgang Siegel
  • Publication number: 20150065504
    Abstract: Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).
    Type: Application
    Filed: August 19, 2014
    Publication date: March 5, 2015
    Inventors: Guangyi Wang, Leonid Beigelman, Anh Truong, Carmela Napolitano, Daniele Andreotti, Haiying He, Karin Ann Stein
  • Publication number: 20150057298
    Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1, X, m, R2, Y, R3, Z, n, R4, A and B are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: August 20, 2014
    Publication date: February 26, 2015
    Inventors: William BUFFHAM, Hannah CANNING, Richard DAVENPORT, William FARNABY, Stephen MACK, Alka PARMAR, Susanne WRIGHT
  • Patent number: 8952026
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting PRMT1 activity. Methods of using the compounds for treating PRMT1-mediated disorders are also described.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: February 10, 2015
    Assignee: Epizyme, Inc.
    Inventors: Lorna Helen Mitchell, Gideon Shapiro, Richard Chesworth, Paula Ann Boriack-Sjodin, Oscar Miguel Moradei
  • Publication number: 20150031883
    Abstract: 2,6-Dihalo-5-alkoxy-4-substituted-pyrimidines, 2,6-dihalo-5-alkoxy-4-pyrimdine carbaldehydes, and derivatives of each are useful intermediates in forming potent herbicides that demonstrate a broad spectrum of weed control. These compounds are disclosed, as are methods of forming and using these compounds.
    Type: Application
    Filed: October 2, 2014
    Publication date: January 29, 2015
    Inventors: Thomas Lyman Siddall, Joshua John Roth
  • Publication number: 20150031709
    Abstract: Provided herein are thiophene compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.
    Type: Application
    Filed: February 8, 2013
    Publication date: January 29, 2015
    Applicant: SUNOVION PHARMACEUTICALS, INC.
    Inventors: John Emmerson Campbell, Una Campbell, Taleen G. Hanania, Liming Shao
  • Patent number: 8940375
    Abstract: The present invention relates to a liquid-crystal (LC) display of the PS (polymer stabilized) or PSA (polymer sustained alignment) type, and to polymerizable compounds and LC media for use in PS (polymer stabilized) and PSA displays.
    Type: Grant
    Filed: July 3, 2008
    Date of Patent: January 27, 2015
    Assignee: Merck Patent GmbH
    Inventors: Matthias Bremer, Georg Bernatz
  • Publication number: 20150025237
    Abstract: The present disclosure provides compounds and methods that are useful for the preparation of compounds useful as orexin-2 receptor antagonists.
    Type: Application
    Filed: February 14, 2013
    Publication date: January 22, 2015
    Inventors: George Anthony Moniz, Annie Zhu Wilcoxen, Farid Benayoud, Jaemoon Lee, Huiming Zhang, Taro Terauchi, Ayumi Takemura, Yu Yoshida, Toshiaki Tanaka, Keiichi Sorimachi, Yoshimitsu Naoe, Yuji Kazuta
  • Publication number: 20150025065
    Abstract: The present invention relates to compounds of general formula I, wherein the group R1, R2, X and Y are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the AMP-activated protein kinase (AMPK) and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
    Type: Application
    Filed: July 15, 2014
    Publication date: January 22, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Frank HIMMELSBACH, Elke LANGKOPF, Holger WAGNER
  • Publication number: 20150024936
    Abstract: The present invention relates to fungicidal pyrimidine compounds I, to their use and to methods for combating phytopathogenic fungi. The present invention also relates to seeds treated with at least one such compound. Furthermore the invention relates to processes for preparing compounds of formula I.
    Type: Application
    Filed: February 1, 2013
    Publication date: January 22, 2015
    Inventors: Wassilios Grammenos, Ian Robert Craig, Nadege Boudet, Bernd Mueller, Jochen Dietz, Erica May Wilson Lauterwasser, Jan Klaas Lohmann, Jurith Montag
  • Publication number: 20140378488
    Abstract: Provided are derivatives substituted by urea associated with 4-substituted-(3-substituted-1H-pyrazole-5-amino)-pyrimidine-2-amino of formula (I), wherein these compounds may selectively regulate or inhibit an information transmission process controlled by natural or variant tyrosine kinase. Also provided are preparation methods and uses of the compounds.
    Type: Application
    Filed: September 5, 2011
    Publication date: December 25, 2014
    Applicant: ZHEJIANG HISUN PHARMACEUTICAL CO., LTD.
    Inventors: Yili Ding, Xuan Yang, Qingyan Yan, Hua Bai, Lifeng Cai, Kenneth Smith, Jian Chai
  • Patent number: 8906895
    Abstract: Substantially optically pure (S)-trans-{4-[({2-[({1-[3,5-bis(trifluoromethyl)phenyl]ethyl}{5-[2-(methylsulfonyl)ethoxy]pyrimidin-2-yl}amino)methyl]-4-(trifluoromethyl)phenyl}(ethyl)amino)methyl]cyclohexyl}acetic acid, or a salt thereof, or a solvate thereof, which has actions of reducing amount of PCSK9 protein and increasing amount of LDL receptor.
    Type: Grant
    Filed: June 3, 2011
    Date of Patent: December 9, 2014
    Assignee: Kowa Company, Ltd.
    Inventors: Tadaaki Ohgiya, Takeshi Murakami, Katsutoshi Miyosawa, Kimiyuki Shibuya, Koichi Yamazaki, Taichi Kusakabe
  • Publication number: 20140357629
    Abstract: Compounds and methods for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a compound of formula (I): or a pharmaceutically acceptable salt, solvate or prodrug thereof, wherein D, X, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein.
    Type: Application
    Filed: August 6, 2014
    Publication date: December 4, 2014
    Applicant: ROCHE PALO ALTO LLC
    Inventors: Chris Allen Broka, David Scott Carter, Michael Patrick Dillon, Ronald Charles Hawley, Alam Jahangir, Clara Jeou Jen Lin, Daniel Warren Parish
  • Publication number: 20140343029
    Abstract: The invention provides novel imidazole amine compounds according to Formula (I) and Formula (II) their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
    Type: Application
    Filed: September 12, 2012
    Publication date: November 20, 2014
    Applicant: MERCK PATENT GMBH
    Inventors: Ruoxi Lan, Bayard R. Huck, Xiaoling Chen, Yufang Xiao, Lizbeth Celeste Deselm, Hui Qiu, Constantin Neagu, Donald Bankston, Christopher Charles Victor Jones
  • Publication number: 20140343070
    Abstract: A proton pump inhibitor containing a compound represented by the formula (I) wherein X and Y are the same or different and each is a bond or a spacer having 1 to 20 carbon atoms in the main chain, R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R2, R3 and R4 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted thienyl group, an optionally substituted benzo[b]thienyl group, an optionally substituted furyl group, an optionally substituted pyridyl group, an optionally substituted pyrazolyl group, an optionally substituted pyrimidinyl group, an acyl group, a halogen atom, a cyano group or a nitro group, R5 and R6 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, which has a superior proton pump action and shows an antiulcer activity and the like after conversion to a proton pump inhibitor in the body, or a salt thereof, or a prodrug the
    Type: Application
    Filed: August 1, 2014
    Publication date: November 20, 2014
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Masahiro Kajino, Atsushi Hasuoka, Naoki Tarui, Terufumi Takagi
  • Patent number: 8877925
    Abstract: 2,6-Dihalo-5-alkoxy-4-substituted-pyrimidines, 2,6-dihalo-5-alkoxy-4-pyrimdine carbaldehydes, and derivatives of each are useful intermediates in forming potent herbicides that demonstrate a broad spectrum of weed control. These compounds are disclosed, as are methods of forming and using these compounds.
    Type: Grant
    Filed: December 28, 2012
    Date of Patent: November 4, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Thomas Lyman Siddall, Joshua John Roth
  • Patent number: 8877751
    Abstract: Compounds of the formula I, in which R1, R2, R3, R3?, R4, R4?, E, E?, E? and E?? have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumors.
    Type: Grant
    Filed: December 8, 2009
    Date of Patent: November 4, 2014
    Assignee: Merck Patent GmbH
    Inventors: Frank Stieber, Oliver Schadt, Dieter Dorsch, Andree Blaukat
  • Patent number: 8877734
    Abstract: Provided are novel selenyl-methyluracil compounds and a pharmaceutical composition for enhancing the effect of radiation treatment. The composition contains at least one compound selected from the group consisting of the selenyl-methyluracil compounds or pharmaceutically acceptable salts thereof, as an active ingredient.
    Type: Grant
    Filed: December 23, 2010
    Date of Patent: November 4, 2014
    Assignee: Kongju National University Industry-University Cooperation Foundation
    Inventors: In Seok Hong, Sung Hee Hong, Marc M. Greenberg
  • Patent number: 8877741
    Abstract: The invention relates to new pyrrolidine derivatives of the formula to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: January 22, 2014
    Date of Patent: November 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Martin Fleck, Niklas Heine, Bernd Nosse, Gerald Juergen Roth
  • Patent number: 8877766
    Abstract: The neuroprotective multifunctional antioxidants are compounds that contain a 2-diacetylamino-5-hydroxypyrimidine moiety, having the structural formula: wherein R1 is CH2 or C2H4; R2 is H or —OR4 where R4 is H or aryl; and R3a and R3b are independently selected from the group consisting of H and —O-alkyl. The antioxidants are orally bioavailable metal-attenuating multifunctional antioxidants that can independently attenuate transition metals, as well as scavenger free radicals. The multifunctional antioxidant compounds, by their ability to independently chelate metals, such as Fe, Cu or Zn, and scavenge free radicals generated from different sources, are neuroprotective and are beneficial for the treatment of various neurological disorders, such as Alzheimer's disease, Parkinson's disease, ALS, traumatic brain injury, ocular disorders, such as cataract, glaucoma, age-related macular degeneration and other retinal degeneration, as well as for reducing the progression of diabetic complications.
    Type: Grant
    Filed: February 15, 2013
    Date of Patent: November 4, 2014
    Inventor: Peter F. Kador
  • Publication number: 20140315869
    Abstract: The invention relates to a composition containing ectoine, hydroxyectoine and/or a salt, ester or amide of these compounds for the suppression of anti-apoptotic signals to neutrophil granulocytes and other cells taking part in inflammations. The delayed apoptosis of the neutrophils is a main component for various types of inflammation. Through the administration of ectoine restoring the normal rate of apoptosis is accomplished at least partially which is associated with a corresponding improvement of the inflammatory phenomena.
    Type: Application
    Filed: September 7, 2012
    Publication date: October 23, 2014
    Inventors: Klaus Unfried, Ulrich Sydlik, Jean Krutmann, Andreas Bilstein
  • Publication number: 20140315934
    Abstract: Compounds of formula (I) and their use as pharmaceutical.
    Type: Application
    Filed: December 17, 2012
    Publication date: October 23, 2014
    Inventors: Marion Hitchcock, Anne Mengel, Anja Richter, Hans Briem, Knut Eis, Vera Pütter, Gerhard Siemeister, Stefan Prechtl, Amaury Ernesto Fernandez-Montalvan, Christian Stegmann, Simon Holton, Mark Jean Gnoth, Cornelia Preuße
  • Publication number: 20140315917
    Abstract: Described are compounds of Formula I which find utility in the treatment of cancer, autoimmune diseases and metabolic bone disorders through inhibition of c-FMS (CSF-1R), c-KIT, and/or PDGFR kinases. These compounds also find utility in the treatment of other mammalian diseases mediated by c-FMS, c-KIT, or PDGFR kinases.
    Type: Application
    Filed: March 14, 2014
    Publication date: October 23, 2014
    Applicant: Deciphera Pharmaceuticals, LLC
    Inventors: Daniel L. Flynn, Michael D. Kaufman, Thiwanka Samarakoon, Timothy Malcolm Caldwell, Lakshminarayana Vogeti, YuMi Ahn, William C. Patt, Karen M. Yates
  • Publication number: 20140309212
    Abstract: The present invention provides compounds useful as inhibitors of Btk, compositions thereof, and methods of using the same.
    Type: Application
    Filed: June 26, 2014
    Publication date: October 16, 2014
    Inventors: Minna Bui, Patrick Conlon, Julio H. Cuervo, Daniel A. Erlanson, Junfa Fan, Bing Guan, Brian T. Hopkins, Tracy J. Jenkins, Gnanasambandam Kumaravel, Alexey A. Lugovskoy, Doug Marcotte, Noel Powell, Daniel Scott, Laura Silvian, Art Taveras, Deping Wang, Min Zhong
  • Patent number: 8859768
    Abstract: This invention provides compounds of formula IA or IB: wherein HY, R1, R2, and G1, are as described in the specification. The compounds are inhibitors of VPS34 and/or PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Grant
    Filed: August 10, 2011
    Date of Patent: October 14, 2014
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Courtney A. Cullis, Krista E. Granger, Jianping Guo, Masaaki Hirose, Gang Li, Miho Mizutani, Tricia J. Vos
  • Publication number: 20140274702
    Abstract: Novel 4-amino-6-(heterocyclic)picolinic acids and their derivatives and 6-amino-2-(heterocyclic)pyrimidine-4-carboxylates and their derivatives are useful to control undesirable vegetation.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Applicant: Dow AgroSciences, LLC
    Inventors: Joseph D. Eckelbarger, Thomas L. Siddall, Norbert M. Satchivi, Paul R. Schmitzer
  • Publication number: 20140274696
    Abstract: Provided herein are 4-amino-6-(4-substituted-phenyl)-picolinic acids and their derivatives, and 6-amino-2-(4-substituted-phenyl)-pyrimidine-4-carboxylic acids and their derivatives, compositions comprising the acids and their derivatives, and methods of use thereof as herbicides.
    Type: Application
    Filed: March 15, 2013
    Publication date: September 18, 2014
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Joseph D. ECKELBARGER, Jeffrey B. Epp, Lindsey G. Fischer, Natalie C. Giampietro, Nicholas M. Irvine, Jeremy Kister, William C. Lo, Christian T. Lowe, Jeffrey Petkus, Joshua Roth, Norbert M. Satchivi, Paul R. Schmitzer, Thomas L. Siddall, Carla N. Yerkes
  • Publication number: 20140271543
    Abstract: New pyridin-2(1H)-one derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).
    Type: Application
    Filed: July 23, 2012
    Publication date: September 18, 2014
    Applicant: ALMIRALL, S.A.
    Inventors: Paul Robert Eastwood, Jordi Bach Taña, Lluis Miquel Pages Santacana
  • Publication number: 20140274703
    Abstract: 4-amino-6-(pyridyl and 2-substitutedphenyl)-picolinic acids and their derivatives; 6-amino-2-(pyridyl and 2-substitutedphenyl)-pyrimidine-4-carboxylates and their derivatives; and methods of using the same as herbicides.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Applicant: Dow AgroSciences LLC
    Inventors: Joseph D. ECKELBARGER, Jeffrey B. EPP, Lindsey G. FISCHER, Natalie C. GIAMPIETRO, Jeremy KISTER, Jeffrey PETKUS, Joshua ROTH, Norbert M. SATCHIVI, Paul R. SCHMITZER, Thomas L. SIDDALL, Carla N. YERKES
  • Publication number: 20140249133
    Abstract: Compounds of formula (I) which are inhibitors of Bub1 kinase, processes for their production and their use as pharmaceuticals.
    Type: Application
    Filed: October 4, 2012
    Publication date: September 4, 2014
    Inventors: Marion Hitchcock, Anne Mengel, Vera Pütter, Gerhard Siemeister, Antje Margret Wengner, Hans Briem, Knut Eis, Volker Schulze, Amaury Ernesto Fernandez-Montalvan, Stefan Prechtl, Simon Holton, Jörg Fanghänel, Philip Lienau, Cornelia Preusse, Mark Jean Gnoth
  • Publication number: 20140235858
    Abstract: The neuroprotective multifunctional antioxidants are compounds that contain a 2-diacetylamino-5-hydroxypyrimidine moiety, having the structural formula: wherein R1 is CH2 or C2H4; R2 is H or —OR4 where R4 is H or aryl; and R3a and R3b are independently selected from the group consisting of H and —O-alkyl. The antioxidants are orally bioavailable metal-attenuating multifunctional antioxidants that can independently attenuate transition metals, as well as scavenger free radicals. The multifunctional antioxidant compounds, by their ability to independently chelate metals, such as Fe, Cu or Zn, and scavenge free radicals generated from different sources, are neuroprotective and are beneficial for the treatment of various neurological disorders, such as Alzheimer's disease, Parkinson's disease, ALS, traumatic brain injury, ocular disorders, such as cataract, glaucoma, age-related macular degeneration and other retinal degeneration, as well as for reducing the progression of diabetic complications.
    Type: Application
    Filed: February 15, 2013
    Publication date: August 21, 2014
    Inventor: PETER F. KADOR