Spiro Ring System Patents (Class 514/409)
  • Patent number: 10633347
    Abstract: Disclosed are a method for preparing an imidazole derivative and crystal form A and crystal form B thereof, and also disclosed is a method for preparing a compound of formula (I) and an intermediate thereof.
    Type: Grant
    Filed: January 8, 2019
    Date of Patent: April 28, 2020
    Assignee: SHANDONG DANHONG PHARMACEUTICAL CO., LTD.
    Inventors: Weihua Shi, Feng Xu, Zheng Wang, Weidong Li, Linghui Wu, Hongwei Li, Minggao Zeng, Kunmin Lai, Zhigan Jiang, Haiying He
  • Patent number: 10369150
    Abstract: A compound, or a pharmaceutically acceptable salt or ester thereof, having a structure of: wherein X is a divalent linking moiety; and R1-R10 are each individually H, optionally-substituted alkyl, optionally-substituted alkoxy, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted heterocyclic, halogen, amino, or hydroxy, provided that at least one of R3 or R8 is an optionally-substituted alkyl, a substituted alkoxy, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted heterocyclic, or halogen.
    Type: Grant
    Filed: October 10, 2018
    Date of Patent: August 6, 2019
    Assignees: University of Pittsburgh—Of the Commonwealth System of Higher Education, The United States of America as represented by the Department of Veterans Affairs
    Inventors: Beibei Chen, Rama K. Mallampalli
  • Patent number: 10323012
    Abstract: The present disclosure relates to miliusane and analogs thereof that are useful as anti-virals, such as anti-HIV and anti-influenza virus agents. The present disclosure provides methods for treating viral infections, such as AIDS, HIV, and influenza infections.
    Type: Grant
    Filed: November 3, 2017
    Date of Patent: June 18, 2019
    Assignee: Hong Kong Baptist University
    Inventor: Hongjie Zhang
  • Patent number: 10227309
    Abstract: Disclosed are a method for preparing an imidazole derivative and crystal form A and crystal form B thereof, and also disclosed is a method for preparing a compound of formula (I) and an intermediate thereof.
    Type: Grant
    Filed: June 7, 2016
    Date of Patent: March 12, 2019
    Assignee: SHANDONG DANHONG PHARMACEUTICAL CO., LTD.
    Inventors: Weihua Shi, Feng Xu, Zheng Wang, Weidong Li, Linghui Wu, Hongwei Li, Minggao Zeng, Kunmin Lai, Zhigan Jiang, Haiying He
  • Patent number: 9849127
    Abstract: The present invention relates to a pharmaceutical composition comprising a compound of formula (I) and methods of treating or preventing cell proliferation disorders comprising administering to a subject a therapeutically active amount or a preventive amount of such a compound.
    Type: Grant
    Filed: May 14, 2014
    Date of Patent: December 26, 2017
    Assignee: Medizinisch Hochschule Hannover
    Inventors: Michael Heuser, Anuhar Chaturvedi, Matthias Preller
  • Patent number: 9849109
    Abstract: Described herein are compounds that are inhibitors of autotaxin. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such inhibitors, alone and in combination with other compounds, for treating autotaxin-dependent or autotaxin-mediated conditions or diseases.
    Type: Grant
    Filed: February 23, 2015
    Date of Patent: December 26, 2017
    Assignee: AMIRA PHARMACEUTICALS, INC.
    Inventors: Jeffrey Roger Roppe, Timothy Andrew Parr, Nicholas Simon Stock, Deborah Volkots, John Howard Hutchinson
  • Patent number: 9822071
    Abstract: The present invention is in the field of pharmaceuticals and chemical industries. In particular, the present invention relates to new anticancer miliusane lactam compounds. The present invention also includes its preparation and application method for treating cancer.
    Type: Grant
    Filed: June 1, 2017
    Date of Patent: November 21, 2017
    Assignee: Hong Kong Baptist University
    Inventor: Hongjie Zhang
  • Patent number: 9695141
    Abstract: The present invention is in the field of pharmaceuticals and chemical industries. In particular, the present invention relates to new anticancer agents based on miliusane compounds. The present invention also includes its preparation and application method for treating cancer.
    Type: Grant
    Filed: October 30, 2015
    Date of Patent: July 4, 2017
    Assignee: HONG KONG BAPTIST UNIVERSITY
    Inventors: Hongjie Zhang, Yifu Guan
  • Patent number: 9567299
    Abstract: Inhibitors of HBV replication of formula (I) including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein X, R1 to R7 have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HBV inhibitors, in HBV therapy.
    Type: Grant
    Filed: October 22, 2014
    Date of Patent: February 14, 2017
    Assignee: JANSSEN SCIENCES IRELAND UC
    Inventors: Koen Vandyck, Geerwin Yvonne Paul Haché, Bart Rudolf Romanie Kesteleyn, Pierre Jean-Marie Bernard Raboisson
  • Patent number: 9480677
    Abstract: This invention is directed to the (S)-enantiomer of the compound of formula (I): or a pharmaceutically acceptable solvate or prodrug thereof. This (S)-enantiomer is useful for the treatment of diseases or conditions, such as pain, which are ameliorated or alleviated by the modulation of voltage-gated sodium channels.
    Type: Grant
    Filed: October 9, 2014
    Date of Patent: November 1, 2016
    Assignee: Xenon Pharmaceuticals Inc.
    Inventors: Mikhail Chafeev, Jianmin Fu, Jean-Jacques Alexandre Cadieux
  • Patent number: 9428504
    Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are antagonists of P2Y1 receptor and may be used as medicaments in the treatment and/or prophylaxis of thromboembolic disorders.
    Type: Grant
    Filed: July 30, 2013
    Date of Patent: August 30, 2016
    Assignee: Bristol-Myers Squibb Company
    Inventors: Carl Thibeault, Charles G. Clark, Indawati DeLucca, Carol Hui Hu, Yoon Jeon, Patrick Y. S. Lam, Jennifer X. Qiao, Wu Yang, Yufeng Wang, Tammy C. Wang
  • Patent number: 9320731
    Abstract: Muscarinic acetylcholine receptor antagonists and methods of using them for the treatment of muscarinic acetylcholine receptor-mediated diseases, such as pulmonary diseases, are provided.
    Type: Grant
    Filed: April 14, 2014
    Date of Patent: April 26, 2016
    Assignee: THERON PHARMACEUTICALS, INC.
    Inventors: Jürg R. Pfister, Gwenaella Rescourio, Meenakshi S. Venkatraman, Xiaoming Zhang
  • Patent number: 9221836
    Abstract: Compounds represented by the formulas wherein each symbol is as defined in the specification, and a prodrug thereof have a superior renin inhibitory activity, and are useful as agents for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension and the like.
    Type: Grant
    Filed: March 23, 2015
    Date of Patent: December 29, 2015
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Takanobu Kuroita, Yasuhiro Imaeda, Kouichi Iwanaga, Naohiro Taya, Hidekazu Tokuhara
  • Patent number: 9211333
    Abstract: The present invention is in the field of pharmaceuticals and chemical industries. In particular, the present invention relates to new anticancer agents based on miliusane compounds. The present invention also includes its preparation and application method for treating cancer.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: December 15, 2015
    Assignee: HONG KONG BAPTIST UNIVERSITY
    Inventor: Hongjie Zhang
  • Patent number: 9120797
    Abstract: Spirocyclic cyclohexane compounds corresponding to formula I a method for producing them, pharmaceutical compositions containing them, and methods of using them.
    Type: Grant
    Filed: September 2, 2011
    Date of Patent: September 1, 2015
    Assignee: Gruenenthal GmbH
    Inventors: Claudia Hinze, Otto Aulenbacher, Bernd Sundermann, Stefan Oberboersch, Elmar Friderichs, Werner Englberger, Babette-Yvonne Koegel, Klaus Linz, Hans Schick, Helmut Sonnenschein, Birgitta Henkel, Valerie Sarah Rose, Michael Jonathan Lipkin
  • Patent number: 9079913
    Abstract: Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.
    Type: Grant
    Filed: September 12, 2014
    Date of Patent: July 14, 2015
    Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Shaomeng Wang, Shanghai Yu, Wei Sun, Sanjeev Kumar, Duxin Sun, Peng Zou, Donna McEachern, Yujun Zhao
  • Publication number: 20150126489
    Abstract: The disclosure provides fumagillol type compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of using, e.g. in the treatment of obesity are provided.
    Type: Application
    Filed: May 8, 2013
    Publication date: May 7, 2015
    Applicant: ZAFGEN, INC.
    Inventors: Robert Zahler, James E. Vath
  • Publication number: 20150118258
    Abstract: The present invention relates to fluorinated bridged spiro[2.4]heptane derivatives of formula (I), wherein n and R1 are as defined in the description, their preparation and their use as pharmaceutically active compounds.
    Type: Application
    Filed: May 15, 2013
    Publication date: April 30, 2015
    Inventors: Olivier Corminboeuf, Davide Pozzi
  • Publication number: 20150111939
    Abstract: A pharmaceutical dosage form for administration twice daily, once daily or less frequently, which contains 6?-fluoro-(N-methyl- or N,N-dimethyl)-4-phenyl-4?,9?-dihydro-3?H-spiro[cyclohexane-1,1?-pyrano[3,4,b]indol]-4-amine or a physiologically acceptable salt thereof.
    Type: Application
    Filed: December 22, 2014
    Publication date: April 23, 2015
    Inventors: Nadja GRUENING, Marc SCHILLER, Ashish HEMANI, Chris KIRBY, Ingo FRIEDRICH
  • Patent number: 9000026
    Abstract: The invention relates to substituted 3-(biphenyl-3-yl)-8,8-difluoro-4-hydroxy-1-azaspiro[4.5]dec-3-en-2-ones of the formula (Ia) for therapeutic purposes, to pharmaceutical compositions and to their use in therapy, in particular for the prophylaxis and therapy of tumor disorders. The invention also relates to novel compounds of the formula (I) in which W, X, Y, Z, A, B, D and G have the meanings given above, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides and/or fungicides. The invention also relates to selectively herbicidal compositions comprising, firstly, the halogen-substituted spirocyclic ketoenols and, secondly, a crop plant compatibility-improving compound.
    Type: Grant
    Filed: February 14, 2012
    Date of Patent: April 7, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Ningshu Liu, Kai Thede, Ursula Mönning, Arne Scholz, Christoph-Stephan Hilger, Ulf Bömer, Reiner Fischer
  • Patent number: 9000025
    Abstract: Described herein are compounds that are inhibitors of autotaxin. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such inhibitors, alone and in combination with other compounds, for treating autotaxin-dependent or autotaxin-mediated conditions or diseases.
    Type: Grant
    Filed: August 19, 2011
    Date of Patent: April 7, 2015
    Assignee: Amira Pharmaceuticals, Inc.
    Inventors: Jeffrey Roger Roppe, Timothy Andrew Parr, Nicholas Simon Stock, Deborah Volkots, John Howard Hutchinson
  • Patent number: 9000189
    Abstract: The invention relates to novel compounds of the formula (I) in which W, X, Y, Z and CKE have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides, and also to selective herbicidal compositions comprising, firstly, the compounds of the formula (I) and, secondly, at least one crop plant compatibility-improving compound. The invention further relates to the boosting of the action of crop protection compositions comprising compounds of the formula (I) through the additions of ammonium salts or phosphonium salts and optionally penetrants.
    Type: Grant
    Filed: November 22, 2007
    Date of Patent: April 7, 2015
    Assignee: Bayer CropScience AG
    Inventors: Thomas Bretschneider, Reiner Fischer, Rolf Pontzen, Christian Arnold, Ulrich Görgens, Olga Malsam, Udo Reckmann, Erich Sanwald, Stefan Lehr, Jan Dittgen, Dieter Feucht, Martin Hills, Christopher Rosinger
  • Publication number: 20150094304
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Application
    Filed: December 11, 2014
    Publication date: April 2, 2015
    Inventors: SARA SABINA HADIDA RUAH, PETER DIEDERIK JAN GROOTENHUIS, FREDRICK F. VAN GOOR, JINGLAN ZHOU, BRIAN RICHARD BEAR, MARK THOMAS MILLER, JASON MC CARTNEY, MEHDI MICHEL DJAMEL NUMA
  • Patent number: 8993782
    Abstract: The invention relates to novel compounds of the formula (I) in which W, X, Y, Z, A and G have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides, and also to selective herbicidal compositions comprising, firstly, the cis-alkoxyspirocyclic biphenyl-substituted tetramic acid derivatives of the formula (I) and, secondly, at least one crop plant compatibility-improving compound. The invention relates furthermore to increasing the activity of crop protection compositions comprising compounds of the formula (I) by adding ammonium or phosphonium salts and, if appropriate, penetrants.
    Type: Grant
    Filed: November 22, 2007
    Date of Patent: March 31, 2015
    Assignee: Bayer CropScience AG
    Inventors: Reiner Fischer, Christian Arnold, Olga Malsam, Jan Dittgen, Dieter Feucht, Ulrich Görgens, Martin Jeffrey Hills, Christopher Hugh Rosinger
  • Publication number: 20150057326
    Abstract: A method of synthesizing cycloalkanyl[b]indoles, as well as related cycloalkanyl[b]benzofurans and cycloalkanyl[b]benzothiophenes is provided. The method is a single, multicomponent reaction that combines (1) an indole, benzofuran, or benzothiopene, (2) an aldehyde, ketone, or ketal, and (3) a diene in the presence of an acid, in particular a Ga(III) or In(III) salt. Compositions and methods of using these compounds to stimulate secretion and/or production of glucagon-like peptide-1 or inhibit the activity of Calcitonin Gene-Related Peptide receptor are also provided.
    Type: Application
    Filed: November 10, 2014
    Publication date: February 26, 2015
    Applicant: Trustees of Dartmouth College
    Inventor: Jimmy Wu
  • Patent number: 8962672
    Abstract: The invention relates to novel active compound combinations having very good insecticidal and acaricidal properties and containing (a) cyclic ketoenols having the formula in which the groups W, X, Y, Z, A, B, D, AND G have the meanings given in the disclosure, and (b) the active compounds (1) to (29) listed in the disclosure.
    Type: Grant
    Filed: September 19, 2011
    Date of Patent: February 24, 2015
    Assignee: Bayer Cropscience AG
    Inventors: Reiner Fischer, Christoph Erdelen
  • Publication number: 20150031691
    Abstract: The present invention relates to compounds represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. Definitions for the variables are provided herein.
    Type: Application
    Filed: October 8, 2014
    Publication date: January 29, 2015
    Inventors: Lawrence Wayne Dillard, Jing Yuan, Katerina Leftheris, Shankar Venkatraman, Guosheng Wu, Lanqi Jia, Zhenrong Xu, Salvacion Cacatian, Angel Morales-Ramos, Suresh B. Singh, Yajun Zheng
  • Publication number: 20150025121
    Abstract: This invention is directed to the (S)-enantiomer of the compound of formula (I): or a pharmaceutically acceptable solvate or prodrug thereof. This (S)-enantiomer is useful for the treatment of diseases or conditions, such as pain, which are ameliorated or alleviated by the modulation of voltage-gated sodium channels.
    Type: Application
    Filed: October 9, 2014
    Publication date: January 22, 2015
    Inventors: Mikhail Chafeev, Jianmin Fu, Jean-Jacques Alexandre Cadieux
  • Publication number: 20150005260
    Abstract: The present invention relates to methods and kits for detecting diastolic dysfunction in subjects without clinical signs of heart failure.
    Type: Application
    Filed: January 2, 2013
    Publication date: January 1, 2015
    Inventors: Faiez Zannad, Patrick Rossignol
  • Publication number: 20150005358
    Abstract: The present invention relates to the control of fish parasites, especially Copepodae, by means of phenyl-substituted ketoenols.
    Type: Application
    Filed: January 22, 2013
    Publication date: January 1, 2015
    Inventors: Jan Koesling, Reiner Fischer
  • Patent number: 8921576
    Abstract: The present invention provides a novel compound represented by a general formula (1) as shown below, which has a glucokinase-activating action in the liver and pancreatic ?-cells and which is useful as an agent for preventing and/or treating diseases caused by hyperglycemia, such as diabetes. A spiroindoline compound represented by the general formula (1), or a salt thereof, or a solvate of the compound or the salt: [wherein ring A represents a nitrogen-containing 5-10 membered heteroaryl group; R1 and R2, which are the same or different, each represent a hydrogen atom, a halogen atom, a halo C1-6 alkyl group, a C6-10 aryl group, a cyano group, a C1-6 alkyl group optionally having a substituent, a C2-6 alkenyl group optionally having a substituent, etc.; R3 represents a hydrogen atom, a C1-6 alkyl group optionally having a substituent, etc.; and R4 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group optionally having a substituent, etc.
    Type: Grant
    Filed: October 18, 2012
    Date of Patent: December 30, 2014
    Assignee: Kowa Company, Ltd.
    Inventors: Takahisa Ogamino, Yukiyoshi Yamazaki, Shin Tanikawa, Ayumu Okuda, Tomoaki Fukuda, Okihisa Tokuda, Yoshiharu Miyake, Shinsuke Itoh, Hiroyuki Ishiwata
  • Patent number: 8912226
    Abstract: The invention relates to a pharmaceutical composition comprising a first pharmacologically active ingredient selected from (1r,4r)-6?-fluoro-N,N-dimethyl-4-phenyl-4?,9?-dihydro-3?H-spiro[cyclohexane-1,1?-pyrano[3,4,b]indol]-4-amine and the physiologically acceptable salts thereof, and a second pharmacologically active ingredient which is a non-steroidal anti-rheumatic drug selected from the group consisting of indometacin, diclofenac, sulindac, tolmetin, zomepirac, aclofenac, bumadizone, etodolac, lonazolac, fentiazac, acemetacin, difenpiramide, oxametacin, proglumetacin, ketorolac, aceclofenac, bufexamac, mefenamic acid, tolfenamic acid, flufenamic acid, meclofenamic acid, and the physiologically acceptable salts thereof.
    Type: Grant
    Filed: May 13, 2013
    Date of Patent: December 16, 2014
    Assignee: Gruenenthal GmbH
    Inventors: Stefanie Frosch, Klaus Linz, Klaus Schiene
  • Publication number: 20140357655
    Abstract: Spiroindoline derivatives, process for their preparation and pharmaceutical compositions thereof, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially sex-hormone-related diseases in both men and women, in particularly those selected from the group of endometriosis, uterine fibroids, polycystic ovarian disease, hirsutism, precocious puberty, gonadal steroid-dependent neoplasia such as cancers of the prostate, breast and ovary, gonadotrope pituitary adenomas, sleep apnea, irritable bowel syndrome, premenstrual syndrome, benign prostatic hypertrophy, contraception and infertility (e.g., assisted reproductive therapy such as in vitro fertilization). The present application relates in particular to spiroindoline derivatives as gonadotropin-releasing hormone (GnRH) receptor antagonists.
    Type: Application
    Filed: January 15, 2013
    Publication date: December 4, 2014
    Inventors: Olaf Panknin, Stefan Bäurle, Sven Ring, Wolfgang Schwede, Wilhelm Bone, Katrin Nowak-Reppel, Eckhard Bender, Reinhard Nubbemeyer, Mark Jean Gnoth
  • Patent number: 8901038
    Abstract: The invention relates to novel compounds of the formula (I) in which W, X, Y, Z, and CKE have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides and/or fungicides. Moreover, the invention relates to selectively herbicidal compositions comprising, firstly, the biphenyl-substituted cyclic ketoenols and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to the boosting of the action of crop protection compositions comprising in particular biphenyl-substituted cyclic ketoenols through the addition of ammonium or phosphium salts and optionally penetrants, to the corresponding compositions, to processes for their preparation and to their use in crop protection as insecticides and/or nematicides and/or acaricides and/or fungicides and/or for preventing unwanted plant growth.
    Type: Grant
    Filed: February 10, 2011
    Date of Patent: December 2, 2014
    Assignee: Bayer CropScience AG
    Inventors: Reiner Fischer, Stefan Lehr, Isolde Häuser-Hahn, Christopher Hugh Rosinger, Chieko Ueno, Arnd Voerste, Elmar Gatzweiler, Ines Heinemann, Ulrich Görgens
  • Patent number: 8901117
    Abstract: The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).
    Type: Grant
    Filed: December 23, 2011
    Date of Patent: December 2, 2014
    Assignee: The Regents of The University of Michigan
    Inventors: Shaomeng Wang, Ke Ding, Yipin Lu, Zaneta Nikolovska-Coleska, Su Qiu, Guoping Wang, Dongguang Qin, Sanjeev Kumar
  • Publication number: 20140349987
    Abstract: The invention provides modulators for the orphan nuclear receptor ROR? and methods for treating ROR? mediated diseases by administrating these novel ROR? modulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolo carboxamide compounds of Formula (1) and the enantiomers, diastereomers, N-oxides, tautomers, solvates and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: December 3, 2012
    Publication date: November 27, 2014
    Inventors: Christoph Steeneck, Olaf Kinzel, Christian Gege, Gerald Kleymann, Thomas Hoffmann
  • Publication number: 20140343077
    Abstract: A compound of formula (I) useful for the treatment or prevention of hepatitis C viral infection, (Formula (I)) wherein: X1 and X2 are each independently CRB or N; RB is H, (C1-6)alkyl, (C1-6)haloalkyl, halo.
    Type: Application
    Filed: August 22, 2012
    Publication date: November 20, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Christian Brochu, Chantal Grand-Maitre, Lee Fader, Cyrille Kuhn, Megan Bertrand-Laperle, Marc Pesant
  • Patent number: 8889703
    Abstract: The present invention relates to compounds represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. Definitions for the variables are provided herein.
    Type: Grant
    Filed: February 23, 2011
    Date of Patent: November 18, 2014
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: Lawrence W. Dillard, Jing Yuan, Katerina Leftheris, Shankar Venkatraman, Guosheng Wu, Lanqi Jia, Zhenrong Xu, Salvacion Cacatian, Angel Morales-Ramos, Suresh Singh, Yajun Zheng
  • Publication number: 20140336233
    Abstract: Compounds of the formulae (I) and (II) for controlling pathogens by foliar application.
    Type: Application
    Filed: August 2, 2012
    Publication date: November 13, 2014
    Applicant: Bayer Intellectual Property GmbH
    Inventors: Marie-Pascale Latorse, Marie-Claire Grosjean-Cournoyer
  • Publication number: 20140336202
    Abstract: Methods of treating subjects with cancer and screening for MDM2 inhibitors that may be effective cancer therapeutics are provided herein. The cancers that may be treated using MDM2 inhibitors using the methods described herein include those that are or may become resistant to treatment with tyrosine kinase inhibitors. Methods of treating subjects with cancers that have, or develop in response to treatment with tyrosine kinase inhibitors, elevated levels of MDM2, Mcl-1 or PP5 or decreased levels of Huwe1 or CAS using MDM2 inhibitors are provided herein. The MDM2 inhibitors may be effective at treating these cancers alone or in combination with a tyrosine kinase inhibitor regardless of p53 status (mutant or wild-type) of the cancer.
    Type: Application
    Filed: December 7, 2012
    Publication date: November 13, 2014
    Applicant: DUKE UNIVERSITY
    Inventors: Sally Kornbluth, Manabu Kurokawa, Neil Spector, Mark Dewhirst
  • Patent number: 8883840
    Abstract: This invention is directed to the (S)-enantiomer of the compound of formula (I): or a pharmaceutically acceptable solvate or prodrug thereof. This (S)-enantiomer is useful for the treatment of diseases or conditions, such as pain, which are ameliorated or alleviated by the modulation of voltage-gated sodium channels.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: November 11, 2014
    Assignee: Xenon Pharmaceuticals Inc.
    Inventors: Mikhail Chafeev, Jianmin Fu, Jean-Jacques Cadieux
  • Publication number: 20140329865
    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, R5, R7, and R8 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: Application
    Filed: December 12, 2012
    Publication date: November 6, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Myriem El Qacemi, Jerome Yves Cassayre
  • Patent number: 8877796
    Abstract: Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.
    Type: Grant
    Filed: July 17, 2013
    Date of Patent: November 4, 2014
    Assignee: The Regents of the University of Michigan
    Inventors: Shaomeng Wang, Shanghai Yu, Wei Sun, Sanjeev Kumar, Duxin Sun, Peng Zou, Donna McEachern, Yujun Zhao
  • Patent number: 8859782
    Abstract: The present invention relates to a novel process for the preparation of 1-H-pyrrolidine-2,4-dione derivatives and to novel intermediates and to a process for their preparation.
    Type: Grant
    Filed: January 25, 2012
    Date of Patent: October 14, 2014
    Assignee: Bayer CropScience AG
    Inventors: Reiner Fischer, Thomas Himmler
  • Patent number: 8859608
    Abstract: A spiro-amino compound of Formula (VI) wherein m is 1 or 2 or 3, n is 1 or 2, R is selected from a 5- or 6-membered aromatic ring and a 5- or 6-membered heteroaromatic ring comprising 1 to 3 heteroatoms selected from S, O and N, such ring being substituted with one or two substituents selected from the group consisting of (C1-C3)alkyl, halogen, (C3-C5)cycloalkyloxy, (C1-C3)alkylcarbonyl, phenyl optionally substituted with one or more halogen atoms, a 5- or 6-membered heterocycle comprising at least one nitrogen atom; P is a substituent Q or COQ, wherein Q is selected from the group consisting of phenyl, pyridyl, pyrimidyl, quinolyl, isoquinolyl, quinoxalyl, benzofuranyl, imidazotriazolyl, being such Q optionally substituted with one or more substituents selected from the group consisting of (C1-C3)alkyl, halogen, trifluoromethyl, carbammido, methylcarbammido, carboxy, methylcarboxy or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: July 15, 2010
    Date of Patent: October 14, 2014
    Assignee: Rottapharm Biotech S.R.L.
    Inventors: Luigi Piero Stasi, Lucio Rovati
  • Patent number: 8859466
    Abstract: The present invention relates to novel oxaspirocyclic spirophenyl-substituted tetramic acid and tetronic acid derivatives of the formula (I) in which W, X, Y, Z, A, B, D, Q1, Q2, and G have the meanings given above, to a plurality of processes for their preparation and to their use as pesticides and/or herbicides. The invention also provides selective herbicidal compositions comprising, firstly, oxaspirocyclic spirophenyl-substituted tetramic acid and tetronic acid derivatives and, secondly, a crop plant compatibility-improving compound. The invention furthermore relates to increasing the activity of crop protection compositions comprising compounds of the formula (I) by addition of ammonium salts or phosphonium salts and, if appropriate, penetrants.
    Type: Grant
    Filed: July 22, 2008
    Date of Patent: October 14, 2014
    Assignee: Bayer CropScience AG
    Inventors: Thomas Bretschneider, Reiner Fischer, Gudrun Lange, Stefan Lehr, Christian Arnold, Dieter Feucht, Eva-Maria Franken, Martin Jeffrey Hills, Heinz Kehne, Olga Malsam, Christopher Hugh Rosinger, Jan Dittgen, Ulrich Görgens, Isolde Häuser-Hahn
  • Publication number: 20140303125
    Abstract: Spirocyclic cyclohexane compounds useful in pharmaceutical compositions for use in the treatment of substance dependency.
    Type: Application
    Filed: June 20, 2014
    Publication date: October 9, 2014
    Inventors: Elmar FRIDERICHS, Babette-Yvonne KOEGEL, Klaus LINZ
  • Patent number: 8846568
    Abstract: The present invention relates to novel active compound combinations comprising, firstly, at least one known compound of the formula (I) in which R1 and A have the meanings given in the description and, secondly, at least one further known active compound from the class of the tetronic or tetramic acids, which combinations are highly suitable for controlling animal pests such as insects and unwanted acarids.
    Type: Grant
    Filed: March 25, 2009
    Date of Patent: September 30, 2014
    Assignee: Bayer CropScience AG
    Inventors: Peter Jeschke, Robert Velten, Heike Hungenberg, Reiner Fischer, Wolfgang Thielert
  • Publication number: 20140288091
    Abstract: Beta-secretase inhibitors, of formula (I) as described in the specification, pharmaceutical compositions comprising them and therapeutic methods using them for the treatment and/or prevention of A?-related pathologies such as Down's syndrome, ?-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's Disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.
    Type: Application
    Filed: October 10, 2012
    Publication date: September 25, 2014
    Applicants: ASTRAZENECA AB, ASTRAZENECA AB
    Inventors: Anna Minidis, Fredrik Rahm, Jenny Viklund
  • Publication number: 20140288042
    Abstract: This invention relates to compounds of Formula I having the following general structure: Z1—Y1—(CH2)n1—R—(CH2)n2—Y2—Z2 wherein R represents a fused bicyclic or spirocyclic aliphatic diamine and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.
    Type: Application
    Filed: October 25, 2012
    Publication date: September 25, 2014
    Inventors: Shawn P. Walsh, Alexander Pasternak, Zhi-Cai Shi, Brian Cato, Esther Y. Kim