Ring Nitrogen Is Shared By Two Of The Cyclos Patents (Class 546/94)
  • Patent number: 10954235
    Abstract: The present invention relates to crystalline valbenazine ditosylate, in particular to a crystalline hydrate of valbenazine ditosylate and a crystalline anhydrate of valbenazine ditosylate, and to methods for their preparation. Furthermore, the invention relates to a pharmaceutical composition comprising the crystalline hydrate or the crystalline anhydrate, preferably in an effective and/or predetermined amount and to the use of said pharmaceutical composition as a medicament, in particular for the treatment of hyperkinetic movement disorders such as tardive dyskinesia.
    Type: Grant
    Filed: February 1, 2018
    Date of Patent: March 23, 2021
    Assignee: Sandoz AG
    Inventors: Christoph Langes, Ulrich Griesser, Erwin Schreiner, Marijan Stefinovic
  • Patent number: 10442800
    Abstract: The present disclosure relates to novel crystalline forms of NBI-98854 (as shown in formula I), preparation process and use thereof. The crystalline forms of NBI-98854 provided by the present disclosure, named as Form CS1 and Form CS2, can be used for preparing drug product treating tardive dyskinesia. The crystalline forms of NBI-98854 provided by the present disclosure have pharmaceutically acceptable solubility and hygroscopicity, good stability and are stable during storage, thereby avoiding changes in drug solubility, dissolution rate, bioavailability and efficacy due to polymorph transformation. This provides a new and better choice for the preparation of drug product containing NBI-98854, which has significant value for future drug development.
    Type: Grant
    Filed: June 29, 2017
    Date of Patent: October 15, 2019
    Assignee: Crystal Pharmaceutical (Suzhou) Co., Ltd.
    Inventors: Minhua Chen, Yanfeng Zhang, Po Zou, Kai Liu, Jinqiu Wang, Xiaoyu Zhang
  • Patent number: 10351558
    Abstract: The present invention provides a compound of Formula I and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing unstable angina, refractory angina, myocardial infarction, transient ischemic attacks, atrial fibrillation, thrombotic stroke, embolic stroke, deep vein thrombosis, disseminated intravascular coagulation, ocular build up of fibrin, and reocclusion or restenosis of recanalized vessels. The compounds are selective Factor IXa inhibitors.
    Type: Grant
    Filed: February 12, 2016
    Date of Patent: July 16, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Dongfang Meng, Hong Li, Meng Yang, Manuel de Lera Ruiz, Sunita V. Dewnani, Tianying Jian, Dann L. Parker, Jr., Ting Zhang, Louis-Charles Campeau, Harold B. Wood, Jiayi Xu, Richard Berger, Jane Yang Wu, Robert K. Orr, Shawn P. Walsh, Bart Harper
  • Patent number: 9777003
    Abstract: The present invention relates to tricyclic 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: Grant
    Filed: February 24, 2016
    Date of Patent: October 3, 2017
    Assignee: Incyte Corporation
    Inventors: Stacey Shepard, Lixin Shao, Haisheng Wang
  • Patent number: 9630921
    Abstract: Compounds of the formula (I) useful as 11-Beta Hydroxysteroid Dehydrogenase Inhibitors
    Type: Grant
    Filed: July 13, 2016
    Date of Patent: April 25, 2017
    Assignee: JANSSEN PHARMACEUTICA NV
    Inventors: Libuse Jaroskova, Joannes Theodorus Maria Linders, Louis Jozef Elisabeth Van Der Veken, Gustaaf Henri Maria Willemsens
  • Patent number: 9447088
    Abstract: The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds in combination with chemotherapeutic agents. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention and also administering a effective amount of a chemotherapeutic agent.
    Type: Grant
    Filed: March 17, 2014
    Date of Patent: September 20, 2016
    Assignee: ArQule, Inc.
    Inventors: Chiang J. Li, Mark A. Ashwell, Jason Hill, Magdi Moussa, Neru Munshi
  • Patent number: 9034895
    Abstract: The disclosure provides methods of treating glioblastoma, methods of screening for compounds that treat glioblastoma, and pharmaceutical compositions useful the treatment of glioblastoma.
    Type: Grant
    Filed: August 22, 2011
    Date of Patent: May 19, 2015
    Assignee: University of Washington Through its Center for Commercialization
    Inventors: Nephi Stella, Toni Kline
  • Patent number: 9023864
    Abstract: Compound of formula I are antagonists of the PGD2 receptor, CRTH2, and as such are useful in the treatment and/or prevention of CRTH2-mediated diseases such as asthma.
    Type: Grant
    Filed: February 7, 2013
    Date of Patent: May 5, 2015
    Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: Carl Berthelette, Michael Boyd, John Colucci, Karine Villeneuve, Joey L. Methot
  • Patent number: 9000005
    Abstract: The present invention relates to highly-pure pyrroloquinolinyl-pyrrole-2,5-dione and pyrroloquinolinyl-pyrrolidine-2,5-dione, for example, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione, and pharmaceutically acceptable salts, solvates, and diastereomers thereof. The present invention also relates to methods for preparing highly-pure pyrroloquinolinyl-pyrrole-2,5-dione and pyrroloquinolinyl-pyrrolidine-2,5-dione, for example, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione, and pharmaceutically acceptable salts, solvates, and diastereomers thereof.
    Type: Grant
    Filed: March 7, 2013
    Date of Patent: April 7, 2015
    Assignee: ArQule, Inc.
    Inventors: Yoshitaka Nakamura, Jo Ooyama
  • Patent number: 8993766
    Abstract: The present invention relates to a method for preparing tetrabenazine (TBZ) and dihydrotetrabenazine (DTBZ), and more specifically to a method for preparing tetrabenazine (TBZ) and dihydrotetrabenazine (DTBZ) by using simple and short reaction processes of using 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline and 4-methyl-2-(3-(trimethylsilyl)prop-1-ene-2-yl)pentane as starting materials to sequentially perform an alkylation reaction, an Aza-Prins cyclization reaction in the presence of an oxidant and an oxidation reaction.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: March 31, 2015
    Assignee: Korea Institute of Science and Technology
    Inventors: Sun Joon Min, Yong Seo Cho, Jae Kyun Lee, Ae Nim Pae, Young Wook Son
  • Publication number: 20150048284
    Abstract: Problem to Be Solved: to provide a chromophore having a far superior nonlinear optical activity to conventional chromophores and to provide a nonlinear optical element comprising said chromophore. Solution: a chromophore comprising a donor structure D, a ?-conjugated bridge structure B, and an acceptor structure A, the donor structure D comprising an aryl group substituted with a substituted oxy group; and a nonlinear optical element comprising said chromophore.
    Type: Application
    Filed: June 27, 2014
    Publication date: February 19, 2015
    Inventors: Akira OTOMO, Isao AOKI, Hideki MIKI, Hidehisa TAZAWA, Shiyoshi YOKOYAMA
  • Publication number: 20140378444
    Abstract: Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.
    Type: Application
    Filed: November 22, 2013
    Publication date: December 25, 2014
    Applicant: University of Pittsburgh - Of the Commonwealth System of Higher Education
    Inventors: Peter Wipf, Marie-Celine Frantz
  • Publication number: 20140350043
    Abstract: The invention relates to FSH receptor antagonist according to general formula (I) or a pharmaceutically acceptable salt thereof and to a pharmaceutical composition containing the same. The compounds can be used for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, and for the treatment of uterine fibroids and other menstrual-related disorders.
    Type: Application
    Filed: September 14, 2012
    Publication date: November 27, 2014
    Inventors: Wesley Peter Blackaby, Martin De Kort, Mark Enthoven, Paul Stuart Hinchliffe, Christian Bernard Matthijs Poulie, Cornelis Marius Timmers, Saskia Verkaik
  • Patent number: 8871933
    Abstract: The present invention relates to a form 1 and form 2 polymorph of (?)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione. The present invention also relates to (?)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione compounds having a chiral purity greater than 99%, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising these (?)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione compounds.
    Type: Grant
    Filed: September 25, 2013
    Date of Patent: October 28, 2014
    Assignee: ArQule, Inc.
    Inventors: David P. Reed, Neil R. Barnes, John C. Kane, Christopher A. Lee, Jian-Xie Chen, Martin P. Redmon
  • Publication number: 20140296280
    Abstract: Pure S-(?)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,-5H-benzo[i,j]quinolizine-2-carboxylic acid L-arginine salt tetrahydrate and a process for its preparation is disclosed.
    Type: Application
    Filed: January 6, 2012
    Publication date: October 2, 2014
    Inventors: Kiran Kumar Gangakhedkar, Aniruddha Varangaonkar, Furqan Mohammed Diwan, Ravindra Dattatraya Yeole, Keshav Deo
  • Patent number: 8846955
    Abstract: Problem to Be Solved: to provide a chromophore having a far superior nonlinear optical activity to conventional chromophores and to provide a nonlinear optical element comprising said chromophore. Solution: a chromophore comprising a donor structure D, a ?-conjugated bridge structure B, and an acceptor structure A, the donor structure D comprising an aryl group substituted with a substituted oxy group; and a nonlinear optical element comprising said chromophore.
    Type: Grant
    Filed: August 24, 2010
    Date of Patent: September 30, 2014
    Assignees: National Institute of Information and Communications Technology, Sumitomo Electric Industries, Ltd., Kyushu University, National University Corporation
    Inventors: Akira Otomo, Isao Aoki, Hideki Miki, Hidehisa Tazawa, Shiyoshi Yokoyama
  • Patent number: 8796303
    Abstract: The present invention relates to compounds of formula (I), racemates, isomers and/or salts thereof useful in the treatment of viral infections, in particular respiratory syncytial virus (RSV) infections. The present invention also relates to processes for preparing the compounds.
    Type: Grant
    Filed: November 22, 2011
    Date of Patent: August 5, 2014
    Assignee: Biota Scientific Management Pty Ltd.
    Inventors: Penelope Anne Mayes, Jeffrey Peter Mitchell, Alistair George Draffan, Gary Robert William Pitt, Kelly Helen Anderson, Chin Yu Lim
  • Publication number: 20140200199
    Abstract: The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds in combination with chemotherapeutic agents. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention and also administering a effective amount of a chemotherapeutic agent.
    Type: Application
    Filed: March 17, 2014
    Publication date: July 17, 2014
    Inventors: Chiang J. Li, Mark A. Ashwell, Jason Hill, Magdi Moussa, Neru Munshi
  • Publication number: 20140187784
    Abstract: It is intended to provide a radioactive compound that has higher selectivity for CYP11B2 than that for CYP11B1, exhibits highly selective accumulation in the adrenal gland compared with blood and organs adjacent to the adrenal gland, and permits commercial supply. The present invention provides a radioactive quinolinone derivative represented by the predetermined general formula or a salt thereof.
    Type: Application
    Filed: December 19, 2013
    Publication date: July 3, 2014
    Applicants: Nihon Medi-Physics Co., Ltd., Kyoto University
    Inventors: Hideo Saji, Hiroyuki Kimura, Masahiro Ono, Hiroki Matsumoto
  • Publication number: 20140179682
    Abstract: Compounds that modulate GluR5 activity and methods of using the same are disclosed.
    Type: Application
    Filed: June 8, 2012
    Publication date: June 26, 2014
    Applicant: SUNOVION PHARMACEUTICALS INC.
    Inventors: Michele L. R. Heffernan, Larry Wendell Hardy, Frank Xinhe Wu, Lakshmi D. Saraswat, Kerry L. Spear
  • Publication number: 20140179014
    Abstract: Nitric oxide probes including a compound represented by Formula, I, II, III, IV, V, VI or a combination thereof are provided. Methods of using these nitric oxide probes to detect nitric oxide are also provided.
    Type: Application
    Filed: December 20, 2013
    Publication date: June 26, 2014
    Inventors: Eric V. Anslyn, Youjun Yang, Michelle M. Adams
  • Patent number: 8754078
    Abstract: The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds in combination with chemotherapeutic agents. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention and also administering a effective amount of a chemotherapeutic agent.
    Type: Grant
    Filed: February 7, 2013
    Date of Patent: June 17, 2014
    Assignee: ArQule, Inc.
    Inventors: Chiang J. Li, Mark A. Ashwell, Jason Hill, Magdi M. Moussa, Neru Munshi
  • Patent number: 8748452
    Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level and the like. That is, the present invention relates to indolizine derivatives represented by the following formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, salts thereof or the like. In the formula, ring U represents aryl or heteroaryl; R1 represents halogen, a hydroxy group or the like; R2 represents halogen, a hydroxy group, alkyl, alkoxy, alkyl substituted by fluorine, alkoxy substituted by fluorine or the like; m represents a number from 0 to 2; n represents a number from 0 to 3; and R3 represents hydrogen, fluorine or the like.
    Type: Grant
    Filed: March 30, 2010
    Date of Patent: June 10, 2014
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Kazuo Shimizu, Masato Iizuka, Yasushi Takigawa
  • Publication number: 20140138669
    Abstract: A delayed fluorescence material comprising a compound represented by the general formula below. At least one of R1 to R8 represent an electron-donating group and the others represent a hydrogen atom; at least one of R9 to R16 represent an electron-withdrawing group and the others represent a hydrogen atom.
    Type: Application
    Filed: July 13, 2012
    Publication date: May 22, 2014
    Applicant: KYUSHU UNIVERSITY NATIONAL UNIVERSITY CORPORATION
    Inventors: Tetsuya Nakagawa, Chihaya Adachi
  • Patent number: 8723017
    Abstract: The present invention pertains to an electrode layer comprising a porous film made of oxide semiconductor fine particles sensitized with certain methin dyes. Moreover the present invention pertains to a photoelectric conversion device comprising said electrode layer, a dye sensitized solar cell comprising said photoelectric conversion device and to novel methin dyes.
    Type: Grant
    Filed: February 26, 2009
    Date of Patent: May 13, 2014
    Assignee: BASF SE
    Inventors: Kazuhiko Kunimoto, Hiroshi Yamamoto, Shinji Nakamichi, Ryuichi Takahashi, Junichi Tanabe
  • Patent number: 8685960
    Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and the use of these compounds and other heteroaryl substituted quinolinone derivatives for the treatment of hyperaldosteronism and/or disorders or diseases that are mediated by 11 ?-hydroxylase (CYP11 B1).
    Type: Grant
    Filed: May 5, 2009
    Date of Patent: April 1, 2014
    Assignee: Elexopharm GmbH
    Inventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
  • Publication number: 20140073623
    Abstract: The invention provides tricyclic sulfonamide compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tricyclic compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.
    Type: Application
    Filed: May 7, 2012
    Publication date: March 13, 2014
    Applicant: Zafgen, Inc.
    Inventors: Susan Mary Cramp, Hazel Joan Dyke, Thomas David Pallin, Robert Zahler
  • Patent number: 8669367
    Abstract: To provide a method whereby a 2-azaadamantane can easily be obtained in good yield. A method for producing a 2-azaadamantane represented by the formula (1), which comprises cyclizing a compound represented by the following formula (2) in the presence of an acid.
    Type: Grant
    Filed: August 14, 2012
    Date of Patent: March 11, 2014
    Assignees: Nissan Chemical Industries, Ltd., Tohoku Techno Arch Co., Ltd.
    Inventors: Toshimasa Hamada, Noriaki Nagahama, Masami Kozawa, Yoshiharu Iwabuchi, Masatoshi Shibuya, Masaki Tomizawa, Yusuke Sasano
  • Patent number: 8658796
    Abstract: The present invention provides ruthenium complexes of the formula wherein: X and X? denote an anionic ligand selected independently from the group consisting of anions of halogens, the phenolate anion (C6H5O?) the perfluorophenolate anion (C6F5O?), and residues of arylcarboxylic, alkylcarboxylic, perfluoroalkylcarboxylic, alkylsulphonic, arylsulphonic, or perfluoroalkylsulphonic acids; A denotes either nitrogen or carbon with an R5 group; R1 denotes hydrogen, C1-C5 alkyl, C2-C5 alkene or C3-C7 cycloalkyl; and R2, R3, R4, R5, R6, R7 denote independently hydrogen, C1-C25 alkyl, C1-C25 perfluoroalkyl, C5-C24 aryl, C2-C25 alkene, C3-C7 cycloalkyl, nitro (—NO2), cyano (—CN), formyl (—CHO), carboxyl (—COOH), or an ester (—COOR?), sulphone (—SO2R?), sulphonamide (—SO2NR?2), or ketone (—COR?) group, in which R? is a C1-C5 alkyl, C1-C5 perfluoroalkyl, or C5-C24 aryl group.
    Type: Grant
    Filed: August 10, 2012
    Date of Patent: February 25, 2014
    Assignee: Umicore AG & Co. KG
    Inventors: Karol Grela, Michal Barbasiewicz, Anna Szadkowska
  • Publication number: 20140045870
    Abstract: The present invention relates to 7-(heteroaryl-amino)-6,7,8,9-tetrahydropyrido[1,2-a]indol acetic acid derivatives of the formula (I), wherein R1, R2, R3 and R4 are as described in the description and their use as prostaglandin receptor modulators, most particularly as prostaglandin D2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.
    Type: Application
    Filed: April 13, 2012
    Publication date: February 13, 2014
    Applicant: Actelion Pharmaceuticals Ltd.
    Inventors: Hamed Aissaoui, Christoph Boss, Jerome Gabillet, Sylvia Richard-Bildstein, Romain Siegrist
  • Patent number: 8642764
    Abstract: Compounds that selectively bind to copper ions in a sample and methods of preparing and using the compounds are described. Disclosed herein are planar julolidine based compounds that display characteristic absorbance in the visible and near-infrared (NIR, 700-1000 nm) region in the presence of copper ions. Methods to detect Cu2+ ions by fluorometry and colorimetry are disclosed.
    Type: Grant
    Filed: August 29, 2012
    Date of Patent: February 4, 2014
    Assignee: Jawaharlal Nehru Centre for Advanced Scientific Research
    Inventors: Govindaraju Thimmaiah, Debabrata Maity, Swapan Kumar Pati, Tapas Kumar Kundu, Arun Kumar Manna, Karthigeyan Dhanasekaran
  • Publication number: 20140031551
    Abstract: The present invention relates to a form 1 and form 2 polymorph of (?)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione. The present invention also relates to (?)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione compounds having a chiral purity greater than 99%, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising these (?)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione compounds.
    Type: Application
    Filed: September 25, 2013
    Publication date: January 30, 2014
    Applicant: ArQule, Inc.
    Inventors: David P. Reed, Neil R. Barnes, John C. Kane, Christopher A. Lee, Jian-Xie Chen, Martin P. Redmon
  • Patent number: 8637541
    Abstract: The compound (+) {7R-[[(4-fluorophenyl)sulfonyl] (methyl)ammo]-6,7,8,9-tetrahydropyrido[1,2-a]mdol-10-yl}acetic acid and pharmaceutically acceptable salts thereof are antagonists of the PGD2 receptor, CRTH2, and as such are useful in the treatment and/or prevention of CRTH2-meidated diseases such as asthma.
    Type: Grant
    Filed: September 17, 2009
    Date of Patent: January 28, 2014
    Assignee: Merck Canada Inc.
    Inventor: Zhaoyin Wang
  • Patent number: 8637671
    Abstract: Compound of formula I are antagonists of the PGD2 receptor, CRTH2, and as such are useful in the treatment and/or prevention of CRTH2-mediated diseases such as asthma.
    Type: Grant
    Filed: September 17, 2009
    Date of Patent: January 28, 2014
    Assignee: Merck Canada Inc.
    Inventors: John Colucci, Michael Boyd, Mohamed Helmi Zaghdane, Michel Gallant
  • Publication number: 20140005292
    Abstract: A compound represented by the following general formula (1). In the formula, A represents a benzene ring, a naphthalene ring and the like, wherein these rings may be substituted with a halogen atom and the like, R1 represents a hydrogen atom and the like, R2 represents a C1-35 hydrocarbon group having or not having at least one group selected from an epoxy group, 4-vinylphenyl group and a (meth)acryloyloxy group, or a hydrogen atom, wherein at least one of R2 with n occurrences is a C3-35 hydrocarbon group having at least one group selected from an epoxy group, a 4-vinylphenyl group and a (meth)acryloyloxy group, n represents an integer of 1 to 6, and X represents a nitrogen atom, an oxygen atom, a sulfur atom, a phosphorus atom, or an n-valent organic group having 35 or less carbon atoms.
    Type: Application
    Filed: April 12, 2012
    Publication date: January 2, 2014
    Applicant: Adeka Corporation
    Inventors: Yosuke Maeda, Masaaki Shimizu, Koich Shigeno
  • Patent number: 8609685
    Abstract: The present invention relates to compounds conformationally constrained mimetics of Smac with function as inhibitors of Inhibitor of Apoptosis Proteins (IAPs), the invention also relates to the use of these compounds in therapy, wherein the induction of apoptotic cell death is beneficial, especially in the treatment of cancer, alone or in combination with other active ingredients.
    Type: Grant
    Filed: November 5, 2008
    Date of Patent: December 17, 2013
    Assignee: CISI SCRL
    Inventors: Carlo Scolastico, Leonardo Pierpaolo Manzoni, Pierfausto Seneci, Laura Belvisi, Domenico Delia, Martino Bolognesi, Eloise Mastrangelo, Mario De Mayo De Mari Milani, Ilaria Motto, Carmelo Drago
  • Patent number: 8604029
    Abstract: The invention provides compounds of formula (I), and pharmaceutically acceptable salts thereof wherein: R1, R2, R3, R4, R5, R6, R7, X and X1 are as defined herein. These compounds are useful in the manufacture of medicaments for use in the prevention or treatment of a fungal disease. Compounds of formula (I), and agriculturally acceptable salts thereof, may also be used as agricultural fungicides.
    Type: Grant
    Filed: November 21, 2007
    Date of Patent: December 10, 2013
    Assignee: F2G Ltd British Body Corporate
    Inventors: Robert Downham, Graham Edward Morris Sibley, Lloyd James Payne, Philip Edwards, Gareth Morse Davies
  • Patent number: 8598198
    Abstract: The invention provides novel compounds and compositions of Formulas I and II, as well as methods of using them. The compounds can be used, for example, to quantify an amount of double stranded DNA in a sample subjected to nucleic acid amplification, or for real time monitoring of a nucleic acid amplification reaction. The compounds can be provided in a kit, for example, with other reagents and instructions for using the compounds and reagents.
    Type: Grant
    Filed: March 16, 2010
    Date of Patent: December 3, 2013
    Assignee: Promega Corporation
    Inventors: Mark McDougall, Stephen Dwight
  • Publication number: 20130317055
    Abstract: An embodiment relates to a selective agonist of neuronal nicotinic acetylcholine receptor ?7 subtype, a pharmaceutically suitable salt, prodrug, or a metabolite thereof, for the prevention and treatment of diseases and conditions that are mediated by nicotinic acetylcholine receptors, and methods of use thereof. Another embodiment is a method of administering a pharmaceutically effective amount of a selective agonist of neuronal nicotinic acetylcholine receptor ?7 subtype, a pharmaceutically suitable salt, prodrug, or a metabolite thereof, to a mammal in need thereof.
    Type: Application
    Filed: March 13, 2013
    Publication date: November 28, 2013
    Applicant: ABBVIE INC.
    Inventors: George M. HAIG, Jeffrey D. BAKER
  • Publication number: 20130317054
    Abstract: An embodiment relates to a selective agonist of neuronal nicotinic acetylcholine receptor ?7 subtype, a pharmaceutically suitable salt, prodrug, or a metabolite thereof, for the prevention and treatment of diseases and conditions that are mediated by nicotinic acetylcholine receptors, and methods of use thereof. Another embodiment is a method of administering a pharmaceutically effective amount of a selective agonist of neuronal nicotinic acetylcholine receptor ?7 subtype, or a pharmaceutically suitable salt, prodrug, or a metabolite thereof, to a mammal in need thereof.
    Type: Application
    Filed: March 13, 2013
    Publication date: November 28, 2013
    Applicant: ABBVIE INC.
    Inventors: George M. HAIG, Jeffrey D. BAKER, Weining Z. Robieson
  • Publication number: 20130302903
    Abstract: Nitric oxide probes comprising a compound represented by Formula, I, II, III, IV, V, VI or a combination thereof are provided. Methods of using these nitric oxide probes to detect nitric oxide are also provided.
    Type: Application
    Filed: October 4, 2012
    Publication date: November 14, 2013
    Applicant: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
    Inventors: Eric V. Anslyn, Youjun Yang, Michelle M. Adams
  • Publication number: 20130281699
    Abstract: The present invention relates to highly-pure pyrroloquinolinyl-pyrrole-2,5-dione and pyrroloquinolinyl-pyrrolidine-2,5-dione, for example, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione, and pharmaceutically acceptable salts, solvates, and diastereomers thereof. The present invention also relates to methods for preparing highly-pure pyrroloquinolinyl-pyrrole-2,5-dione and pyrroloquinolinyl-pyrrolidine-2,5-dione, for example, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione, and pharmaceutically acceptable salts, solvates, and diastereomers thereof.
    Type: Application
    Filed: March 7, 2013
    Publication date: October 24, 2013
    Applicant: ARQULE, INC.
    Inventors: Yoshitaka Nakamura, Jo Ooyama
  • Patent number: 8563567
    Abstract: The present invention relates to substituted heterocyclic compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted heterocyclic compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Grant
    Filed: December 29, 2010
    Date of Patent: October 22, 2013
    Assignee: ArQule, Inc.
    Inventors: Syed M. Ali, Mark A. Ashwell, Yanbin Liu, Magdi Moussa, Jianqiang Wang, Hui Wu
  • Patent number: 8552192
    Abstract: The present invention relates to a form 1 and form 2 polymorph of (?)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione. The present invention also relates to (?)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl) pyrrolidine-2,5-dione compounds having a chiral purity greater than 99%, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising these (?)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione compounds.
    Type: Grant
    Filed: December 22, 2010
    Date of Patent: October 8, 2013
    Assignee: ArQule, Inc.
    Inventors: David P. Reed, Neil R. Barnes, John C. Kane, Christopher A. Lee, Jian-Xie Chen, Martin P. Redmon
  • Publication number: 20130251647
    Abstract: The invention relates to new types of modulators of the cold menthol receptor TRPM8, to methods of modulating the TRPM8 receptor using these modulators; and in particular the use of the modulators for inducing a sensation of coldness; and also the articles and compositions produced using these modulators.
    Type: Application
    Filed: September 20, 2012
    Publication date: September 26, 2013
    Applicant: BASF SE
    Inventors: Thomas Subkowski, Claus Bollschweiler, Jens Wittenberg, Wolfgang Siegel, Ralf Pelzer
  • Patent number: 8540521
    Abstract: Disclosed are benzoxazole-based compounds, kits, and methods of producing and using the described compounds in fluorescence-based detection of analytes (e.g., metal ions). Also disclosed are uses of benzoxazole-based compounds as ratiometric metal ion indicators.
    Type: Grant
    Filed: December 29, 2009
    Date of Patent: September 24, 2013
    Assignee: Life Technologies Corporation
    Inventors: Kyle Gee, Vladimir Martin
  • Patent number: 8541404
    Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and a method of treating of hyperaldosteronism and/or disorders or diseases that are mediated by 11?-hydroxylase (CYP11B1) with these compounds.
    Type: Grant
    Filed: November 3, 2010
    Date of Patent: September 24, 2013
    Assignee: ElexoPharm GmbH
    Inventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
  • Patent number: 8513292
    Abstract: The present invention relates to pyrrolidine-2,5-dione compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising pyrrolidine-2,5-dione compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a compound or pyrrolidine-2,5-dione compound of the present invention.
    Type: Grant
    Filed: June 19, 2008
    Date of Patent: August 20, 2013
    Assignee: ArQule, Inc.
    Inventors: Neil Westlund, Jason Hill, Mark A. Ashwell, Nivedita Namdev, Jianqiang Wang, Syed Ali
  • Patent number: 8507519
    Abstract: The present invention relates to optically pure S-(?)-benzoquinolizine carboxylic acid, lysine salt and to pharmaceutical compositions comprising the S(?)-benzoquinolizine carboxylic acid, lysine salt.
    Type: Grant
    Filed: May 21, 2007
    Date of Patent: August 13, 2013
    Assignee: Wockhardt Limited
    Inventors: Mahesh Vithalbhai Patel, Shivkumar Agarwal, Sreenivas Kandepu
  • Publication number: 20130197026
    Abstract: The disclosure provides methods of treating glioblastoma, methods of screening for compounds that treat glioblastoma, and pharmaceutical compositions useful the treatment of glioblastoma.
    Type: Application
    Filed: August 22, 2011
    Publication date: August 1, 2013
    Applicant: Unversity of Washington Through its Center for Commercialization
    Inventors: Nephi Stella, Toni Kline