Nitrogen, Other Than As Nitro Or Nitroso, Attached Indirectly To The Quinoline Ring System By Nonionic Bonding Patents (Class 546/176)
  • Patent number: 10266697
    Abstract: The present invention relates to novel methine dyes, methods for the preparation thereof and use thereof for dyeing plastics, especially polyamides, so as to obtain yellow colorings with improved light fastness and improved thermostability.
    Type: Grant
    Filed: December 22, 2015
    Date of Patent: April 23, 2019
    Assignee: LANXESS Deutschland GmbH
    Inventors: Hans-Ulrich Borst, Frank Linke, Stephan Michaelis
  • Patent number: 9238665
    Abstract: A method is provided for producing an aromatic compound, including a step of mixing a compound represented by formula (A) and a compound represented by formula (B): in the presence of at least one phosphine compound selected from the group consisting of a phosphine represented by formula (C) and a phosphonium salt represented by formula (F): a base, a palladium compound, and an aprotic organic solvent.
    Type: Grant
    Filed: July 5, 2013
    Date of Patent: January 19, 2016
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Seiji Oda, Takashi Kamikawa
  • Publication number: 20150111870
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Application
    Filed: October 14, 2014
    Publication date: April 23, 2015
    Applicant: JOHNSON & JOHNSON
    Inventors: KRISTI A. LEONARD, KENT BARBAY, JAMES P. EDWARDS, KEVIN D. KREUTTER, DAVID A. KUMMER, UMAR MAHAROOF, RACHEL NISHIMURA, MAUD URBANSKI, HARIHARAN VENKATESAN, AIHUA WANG, RONALD L. WOLIN, CRAIG R. WOODS, ANNE FOURIE, XIAOHUA XUE, MAXWELL D. CUMMINGS, KELLY MCCLURE, VIRGINIA TANIS
  • Publication number: 20150105366
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Application
    Filed: October 15, 2013
    Publication date: April 16, 2015
    Applicant: Janssen Pharmaceutica NV
    Inventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Anne Fourie, Xiaohua Xue, Maxwell D. Cummings, William Moore Jones, Steven Goldberg
  • Publication number: 20150079622
    Abstract: Disclosed herein are compounds, compositions, methods, and kits for detecting reactive oxygen species (ROS) by conventional fluorescence microscopy, fluorescence spectroscopy, flow cytometry, and/or high content imaging. The compounds disclosed herein are novel reduced nucleic acid binding cyanine dyes, which dyes are probes for detecting ROS and measuring oxidative stress in cells either in vitro and/or in vivo. Also described herein are processes for preparing novel reduced dyes, i.e., ROS probes, for use in the disclosed compositions, methods and kits.
    Type: Application
    Filed: February 26, 2013
    Publication date: March 19, 2015
    Inventors: Yi-Zhen Hu, Aimei Chen, Hee Chol Kang, Kyle Gee, Bhaskar Mandavilli
  • Publication number: 20150065538
    Abstract: Compounds of formula (I) wherein R1, R2, R3, and Y are defined in the description are TRPA1 antagonists. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
    Type: Application
    Filed: November 4, 2014
    Publication date: March 5, 2015
    Inventors: Richard J. Perner, Michael E. Kort, Stanley DiDomenico, Jun Chen, Anil Vasudevan
  • Patent number: 8946431
    Abstract: Provided is a 2-(substituted ethynyl)quinoline derivative having an mGluR5 antagonistic activity and pharmaceutically acceptable salts thereof. The compound of the present invention can be useful as a medicament for treating and preventing mGluR5 receptor-mediated diseases such as Alzheimer's disease, senile dementia, Parkinson's disease, L-DOPA-induced dyskinesia, Huntington's chorea, amyotrophic lateral sclerosis, multiple sclerosis, schizophrenia, anxiety disorder, depression, neuropathic pain, drug dependence, fragile X syndrome, autism, migraine and gastroesophageal reflux disease (GERD).
    Type: Grant
    Filed: July 16, 2013
    Date of Patent: February 3, 2015
    Assignee: Korea Institute of Science and Technology
    Inventors: Sun Joon Min, Yong Seo Cho, Ae Nim Pae, Eun Jeong Lim, Ji Yeong Kim, Myung Hee Son, Jae Kyun Lee
  • Publication number: 20150031686
    Abstract: Disclosed are phenyl-oxazolyl derivatives having a general formula (I), a preparation method thereof, and an application of the phenyl-oxazolyl derivatives as an inosine monophosphate dehydrogenase (IMPDH) inhibitor.
    Type: Application
    Filed: March 6, 2013
    Publication date: January 29, 2015
    Inventors: Zhaojin Zhong, Zhuorong Li, Dajun Zhang, Yuhuan Li, Zhen Wang, Rongmei Gao, Jiajia Shen
  • Patent number: 8871940
    Abstract: Unsymmetrical bisazides containing chelating and non-chelating azido groups undergo chemoselective three-component copper(I)-catalyzed azide-alkyne conjugation reactions with two different alkyne molecules. In conjunction with the reactivity gap between aromatic and aliphatic alkynes, a bistriazole molecule can be generated with an excellent regioselectivity by mixing two alkynes and a bisazide in a single reaction container. This method is applicable in aqueous solutions at neutral pH, which may lend utilities in bioconjugation applications.
    Type: Grant
    Filed: July 15, 2013
    Date of Patent: October 28, 2014
    Assignee: The Florida State University Research Foundation, Inc.
    Inventors: Lei Zhu, Zhao Yuan, Gui-Chao Kuang
  • Patent number: 8871941
    Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein A1, A2, A3, A4, A5 and A6 are independently selected from the group consisting of CR3 and N; provided that at most 3 of A1, A2, A3, A4, A5 and A6 is N; B1, B2 and B3 are independently selected from the group consisting of CR2 and N; each R3 is independently H, halogen, C1-C6 alkyl, C1-C6 haloalkyl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkyl sulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfonyl, C1-C6 alkylamino, C2-C6 dialkylamino, —CN or —NO2; and R1, R2, R4, R5, W and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: May 12, 2014
    Date of Patent: October 28, 2014
    Assignee: E.I. du Pont de Nemours and Company
    Inventors: George Philip Lahm, Wesley Lawrence Shoop, Ming Xu
  • Publication number: 20140295437
    Abstract: The present invention provides methods and non-fluorescent carbocyanine quencher compounds having the general formula: Wherein the A moiety is a substituted pyridinium, unsubstituted pyridinium, substituted quinolinium, unsubstituted quinolinium, substituted benzazolium, unsubstituted benzazolium, substituted indolinium, or substituted indolinium. The invention further provides luminescent donor molecule-quencher pairs and luminescent donor molecule-quencher-luminescent acceptor molecule conjugates wherein the quencher is a cyanine compound of the present invention. The energy transfer pairs are used to detect an analyte of interest in a sample.
    Type: Application
    Filed: December 17, 2013
    Publication date: October 2, 2014
    Applicant: LIFE TECHNOLOGIES CORPORATION
    Inventors: Rosaria HAUGLAND, Ching-Ying CHEUNG, Stephen YUE
  • Publication number: 20140296246
    Abstract: This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula (I) wherein R1a, R1b, R2a, R2b, R3, and X are described herein.
    Type: Application
    Filed: March 27, 2014
    Publication date: October 2, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Evangelos Aktoudianakis, Gregory Chin, Britton Kenneth Corkey, Jinfa Du, Kristyna Elbel, Robert H. Jiang, Tetsuya Kobayashi, Ruben Martinez, Samuel E. Metobo, Michael R. Mish, Sophie Shevick, David Sperandio, Hai Yang, Jeff Zablocki
  • Publication number: 20140288133
    Abstract: A compound of Formula (I) or a pharmaceutically acceptable salt thereof: Wherein: Het is a 5 to 10-membered heteroaromatic ring; Either X is N and Y is CR5; or X is C and Y is S; Z is selected from N and CH; R1 is selected from H and C1-2alkyl; R2 is selected from H, C1-2alkyl, OH, —CH2OH and C1-2alkoxy; Each R3 is independently selected from OH, C1-3alkyl, F, Cl, Br, NH2, and C1-3alkoxy; R4 is selected from C1-3alkyl and haloC1-3 alkyl; R5 is selected from H, C1-3alkyl and haloC1-3alkyl; R6 and R7 are either i) each independently selected from H, C1-3alkyl and C1-3alkoxy; or ii) R6 and R7 together with the ring to which they are attached form a 9-membered bicylic ring; p is 0-3; and RA is selected from H and C1-3alkyl, compositions containing them, their use in therapy, for example in the treatment of tuberculosis, and methods for the preparation of such compounds, are provided.
    Type: Application
    Filed: June 4, 2014
    Publication date: September 25, 2014
    Applicant: GLAXO GROUP LIMITED
    Inventors: JULIA CASTRO PICHEL, RAQUEL FERNANDEZ MENENDEZ, ESTHER PILAR FERNANDEZ VELANDO, SILVIA GONZALEZ DEL VALLE, ARACELI MALLO-RUBIO
  • Publication number: 20140275028
    Abstract: The present invention relates to compounds of Formula (I), and solvates, hydrates, and pharmaceutically acceptable salts thereof, wherein ring A, R1, R5 and R6 are as defined herein, useful as FLAP modulators. The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Inventors: Wenying Chai, Charlotte Deckhut, Curt A. Dvorak, Wendy Eccles, James P. Edwards, Steven D. Goldberg, Paul J. Krawczuk, Alec D. Lebsack, Jing Liu, Virginia M. Tanis, Kyle T. Tarantino
  • Publication number: 20140238900
    Abstract: The present invention is related to formulations consisting by block copolymers ?,?-di-aryl or alkyl sulfonates of poly(ethylene oxide)w-poly(propylene oxide)-poly(ethylene oxide)w of bis-ammonium and block copolymers ?,?-di-amine of poly(ethylene oxide)w-poly(propylene oxide)-poly(ethylene oxide)w, that are effective in the dewatering and desalting crude whose specific gravities are within the range of 14 to 23° API.
    Type: Application
    Filed: February 25, 2014
    Publication date: August 28, 2014
    Inventors: Eugenio Alejandro FLORES OROPEZA, Cesar Andres FLORES SANDOVAL, Reyna REYES MARTINEZ, Jose Gonzalo HERNANDEZ CORTEZ, Alfonso LOPEZ ORTEGA, Laura Veronica CASTRO SOTELO, Fernando ALVAREZ RAMIREZ, Arquimedes ESTRADA MARTINEZ, Flavio Salvador VAZQUEZ MORENO
  • Publication number: 20140221658
    Abstract: The disclosed modulators of Rb:Raf-1 interactions are potent, selective disruptors of Rb:Raf-1 binding, with IC50 values ranging from 80 nM to 500 nM. Further, these compounds are surprisingly effective in inhibiting a wide variety of cancer cells, including osteosarcoma, epithelial lung carcinoma, non-small cell lung carcinoma, three different pancreatic cancer cell lines, two different glioblastoma cell lines, metastatic breast cancer, melanoma, and prostate cancer. Moreover, the disclosed compounds effectively disrupt angiogenesis and significantly inhibited tumors in nude mice derived from human epithelial lung carcinoma tumors. Accordingly, the disclosed compounds, pharmaceutical compositions comprising the compounds, methods of inhibiting cell proliferation, methods of treating subjects with cancer, and methods of preparing the disclosed compounds are provided.
    Type: Application
    Filed: February 3, 2014
    Publication date: August 7, 2014
    Applicant: University of South Florida
    Inventors: Said M. Sebti, Srikumar Chellappan, Nicholas James Lawrence
  • Publication number: 20140206876
    Abstract: Provided is a 2-(substituted ethynyl)quinoline derivative having an mGluR5 antagonistic activity and pharmaceutically acceptable salts thereof. The compound of the present invention can be useful as a medicament for treating and preventing mGluR5 receptor-mediated diseases such as Alzheimer's disease, senile dementia, Parkinson's disease, L-DOPA-induced dyskinesia, Huntington's chorea, amyotrophic lateral sclerosis, multiple sclerosis, schizophrenia, anxiety disorder, depression, neuropathic pain, drug dependence, fragile X syndrome, autism, migraine and gastroesophageal reflux disease (GERD).
    Type: Application
    Filed: July 16, 2013
    Publication date: July 24, 2014
    Inventors: Sun Joon MIN, Yong Seo CHO, Ae Nim PAE, Eun Jeong LIM, Ji Yeong KIM, Myung Hee SON, Jae Kyun LEE
  • Patent number: 8771665
    Abstract: The present invention provides, among other things, compounds represented by the general Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, R1A, R1B, R2, and R3 are as defined in classes and subclasses herein and compositions (e.g., pharmaceutical compositions) comprising such compounds, which compounds are useful as inhibitors of hepatitis C virus polymerase, and thus are useful, for example, as medicaments for the treatment of HCV infection.
    Type: Grant
    Filed: December 16, 2011
    Date of Patent: July 8, 2014
    Assignee: Cocrystal Discovery, Inc.
    Inventors: Sam S K Lee, Wang Shen, Xiaoling Zheng, Irina C. Jacobson
  • Publication number: 20140142307
    Abstract: Singly and multiply charged imidazolium cations (ICs) have been identified as a class of chemical compositions that possess potent antineoplastic, antibacterial and antimicrobial properties. The imidazolium cations disclosed demonstrate greater or equivalent potency towards cancerous cells as the current clinical standard, cisplatin. These imidazolium cations, however, achieve this efficacy without any of the known toxic side effects caused by heavy metal-based antineoplastic drugs such as cisplati.
    Type: Application
    Filed: April 30, 2012
    Publication date: May 22, 2014
    Inventors: Wiley Youngs, Matthew Panzner, Claire Tessier, Michael Deblock, Brian Wright, Patrick Wagers, Nikki Robishaw
  • Patent number: 8716265
    Abstract: The present invention relates to substituted 4-qinolinemethanols and pharmaceutical compositions thereof and methods of using the same for treating of malaria, tuberculosis, and other infectious diseases.
    Type: Grant
    Filed: November 18, 2011
    Date of Patent: May 6, 2014
    Assignee: Jenrin Discovery, Inc.
    Inventors: John F. McElroy, Robert J. Chorvat, David Nugiel
  • Patent number: 8716472
    Abstract: A tri-podal compound according to formula (I) wherein, each Z is the same and is a substituted or unsubstituted N-heteroaromatic single-, multiple-, or fused-ring; and each A is the same, and can represent a direct bond between the cyclohexane ring and Z, or a carboxamide group (—C(O)—N(H)—). Use of the compounds in combinatorial libraries, methods of making the tripodal compounds, sensor devices for detecting carbohydrate targets, and methods of using the tripodal compounds to detect carbohydrate targets in a sample are also disclosed.
    Type: Grant
    Filed: October 16, 2007
    Date of Patent: May 6, 2014
    Assignee: University of Rochester
    Inventors: Benjamin L. Miller, Prakash B. Palde, Peter C. Gareiss
  • Publication number: 20140107094
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Application
    Filed: October 15, 2013
    Publication date: April 17, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Joan Pierce, Steven Goldberg, Anne Fourie, Xiaohua Xue
  • Patent number: 8680115
    Abstract: The present invention relates to tetrahydroquinoline compounds as muscarinic receptor agonists; compositions comprising the same; methods of inhibiting an activity of a muscarinic receptor with said compounds; methods of treating a disease condition associated with a muscarinic receptor using said compounds; and methods for identifying a subject suitable for treatment using said compounds.
    Type: Grant
    Filed: May 27, 2009
    Date of Patent: March 25, 2014
    Assignee: Acadia Pharmaceuticals, Inc.
    Inventors: Niels Skjaerback, Kristian Norup Koch, Bo Lennart Mikael Friberg, Bo-Ragnar Tolf
  • Publication number: 20140066424
    Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of HIF pathway activity for the treatment or prevention of cancer and other hypoxia-mediated diseases.
    Type: Application
    Filed: August 23, 2013
    Publication date: March 6, 2014
    Applicant: Institute For Applied Cancer Science/The University of Texas MD Anderson Cancer Center
    Inventors: Philip Jones, Maria Emilia DiFrancesco, Alessia Petrocchi, Christopher L. Carroll, Joe Marszalek, Barbara Czako, Ryan Johnson, Jay Theroff
  • Publication number: 20140033450
    Abstract: The invention relates to a dyeing composition comprising a fluorescent disulphide dye and to a method of dyeing keratin materials, with a lightening effect, that employs said composition. It likewise relates to new fluorescent disulphide dyes and to their uses in the lightening of keratin materials. This composition allows a particularly persistent lightening effect to be obtained.
    Type: Application
    Filed: October 10, 2013
    Publication date: February 6, 2014
    Applicant: L'OREAL
    Inventors: Nicolas DAUBRESSE, Andrew GREAVES, Henri SAMAIN
  • Publication number: 20140018541
    Abstract: Unsymmetrical bisazides containing chelating and non-chelating azido groups undergo chemoselective three-component copper(I)-catalyzed azide-alkyne conjugation reactions with two different alkyne molecules. In conjunction with the reactivity gap between aromatic and aliphatic alkynes, a bistriazole molecule can be generated with an excellent regioselectivity by mixing two alkynes and a bisazide in a single reaction container. This method is applicable in aqueous solutions at neutral pH, which may lend utilities in bioconjugation applications.
    Type: Application
    Filed: July 15, 2013
    Publication date: January 16, 2014
    Applicant: The Florida State University Research Foundation, Inc.
    Inventors: Lei Zhu, Zhao Yuan, Gui-Chao Kuang
  • Publication number: 20140014925
    Abstract: A compound represented by Formula 1 below and an organic light-emitting device including the compound are provided: Substituents in Formula 1 are the same as defined in the specification.
    Type: Application
    Filed: June 21, 2013
    Publication date: January 16, 2014
    Inventors: Hye-Jin Jung, Seok-Hwan Hwang, Young-Kook Kim, Jin-O Lim, Sang-Hyun Han, Eun-Jae Jeong, Soo-Yon Kim, Jun-Ha Park, Eun-Young Lee, Chang-Ho Lee, Jong-Hyuk Lee
  • Publication number: 20140010763
    Abstract: Novel fluorogenic compounds designed such that upon a chemical event, compounds capable of emitting NIR light are generated, are disclosed. The compounds comprise two or more acceptor-containing moieties and a cleavable donor-containing moiety, being in complete pi-electrons conjugation and being such that no delocalization of pi-electrons is enabled. Also disclosed are fluorescent compounds generated upon subjecting the fluorogenic compounds to a chemical event (e.g., deprotonation). Also disclosed are uses of the fluorogenic compounds as NIR probed with a Turn-ON mechanism in monitoring presence and/or level of various analytes.
    Type: Application
    Filed: September 15, 2013
    Publication date: January 9, 2014
    Applicant: Ramot at Tel-Aviv University Ltd.
    Inventors: Doron SHABAT, Ronit Satchi-Fainaro
  • Publication number: 20140005221
    Abstract: The present invention relates to a compound that has URAT1 inhibitory action, and a URAT1 inhibitor, a blood uric acid level-reducing agent and a pharmaceutical composition comprising the compound. More specifically, the present invention relates to a compound represented by Formula (I) below.
    Type: Application
    Filed: January 30, 2012
    Publication date: January 2, 2014
    Applicant: SATO PHARMACEUTICAL CO., LTD.
    Inventors: Keita Nagai, Koh Nagasawa, Hirobumi Takahashi, Motoaki Baba, Shinichi Fujioka, Eri Kondoh, Kenichi Tanaka, Yoshiki Itoh
  • Publication number: 20130331414
    Abstract: Methods for preventing or treating retroviral infection, such as human immunodeficiency virus, in vivo utilize transcriptional inhibitory compounds. These include cortistatin A and analogs of the cortistatin family.
    Type: Application
    Filed: January 10, 2012
    Publication date: December 12, 2013
    Inventors: Susana Valente, Phil S. Baran
  • Publication number: 20130331413
    Abstract: Disclosed are compositions and methods for treating and/or preventing infections in mammals, by administering to a mammal a therapeutically effective amount of at least one defensin-like molecule, e.g., in a composition that includes such molecule. Also disclosed are kits that include such molecules, or compositions that include such molecules, as well as instructions for using such molecules to treat a mammal.
    Type: Application
    Filed: June 6, 2013
    Publication date: December 12, 2013
    Inventors: Erik DE LEEUW, Alexander D. MACKERELL, JR.
  • Patent number: 8569505
    Abstract: This invention is directed to vanilloid receptor VR1 ligands. More particularly, this invention relates to ?-aminotetralin-derived ureas that are potent antagonists or agonists of VR1 which are useful for the treatment and prevention of inflammatory and other pain conditions in mammals.
    Type: Grant
    Filed: January 22, 2010
    Date of Patent: October 29, 2013
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Ellen Codd, Scott L. Dax, Michele Jetter, Mark McDonnell, James J. McNally, Mark Youngman
  • Patent number: 8569508
    Abstract: A synthesis method for preparing Montelukast sodium intermediate 2-(2-(3-(2-(7-chloro-2-quinolyl)vinyl)phenyl-3-oxopropyl)phenyl) propanol is provided. In this method, the target compound is prepared by condensing the starting materials 7-chloroquinaldine and 3-cyanobenzaldehyde, and then reacting the resultant product with 2-(2-ortho-(2-haloethyl)-phenylpropyl)tetrahydropyrane ether. The present invention can easily obtain start materials and is applicable for mass production.
    Type: Grant
    Filed: August 24, 2010
    Date of Patent: October 29, 2013
    Assignee: Shandong New Time Pharmaceutical Co., Ltd.
    Inventors: Zhiquan Zhao, Haixin Wang, Zengxue Wang
  • Patent number: 8541596
    Abstract: Novel heterocyclic derivatives as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.
    Type: Grant
    Filed: April 21, 2011
    Date of Patent: September 24, 2013
    Assignee: Probiodrug AG
    Inventors: Ulrich Heiser, Daniel Ramsbeck, Torsten Hoffmann, Livia Boehme
  • Patent number: 8541582
    Abstract: The present invention relates to novel phenyl bicyclic methyl amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: April 13, 2012
    Date of Patent: September 24, 2013
    Assignee: Allergan, Inc.
    Inventors: Janet A. Takeuchi, Ling Li, Wha Bin Im
  • Publication number: 20130245062
    Abstract: Disclosed are nitrile derivatives and pharmaceutical compositions comprising nitrile derivatives. The pharmaceutical compositions comprise compounds of the formula I and the pharmaceutically acceptable salts of such compounds. Also disclosed are processes for the preparation of such compounds, intermediates used in the preparation of such compounds, and the uses of such compounds in treating hyperproliferative diseases, inflammatory diseases and viral and bacterial infections and inducing apoptosis in cancer cells.
    Type: Application
    Filed: November 27, 2012
    Publication date: September 19, 2013
    Applicant: CELLCEUTIX CORPORATION
    Inventor: KRISHNA MENON
  • Patent number: 8513418
    Abstract: The present invention relates to novel substituted bicyclic methyl amine derivatives which are useful as sphingosine-1-phosphate receptors modulators and useful for treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: April 13, 2012
    Date of Patent: August 20, 2013
    Assignee: Allergan, Inc.
    Inventors: Janet A. Takeuchi, Ling Li, Wha Bin Im
  • Publication number: 20130203802
    Abstract: A compound of Formula (I) or a pharmaceutically acceptable salt thereof: Wherein: Het is a 5 to 10-membered heteroaromatic ring; Either X is N and Y is CR5; or X is C and Y is S; Z is selected from N and CH; R1 is selected from H and C1-2alkyl; R2 is selected from H, C1-2alkyl, OH, —CH2OH and C1-2alkoxy; Each R3 is independently selected from OH, C1-3alkyl, F, Cl, Br, NH2, and C1-3alkoxy; R4 is selected from C1-3alkyl and haloC1-3alkyl; R5 is selected from H, C1-3alkyl and haloC1-3alkyl; R6 and R7 are either i) each independently selected from H, C1-3alkyl and C1-3alkoxy; or ii) R6 and R7 together with the ring to which they are attached form a 9-membered bicyclic ring; p is 0-3; and RA is selected from H and C1-3alkyl, compositions containing them, their use in therapy, for example in the treatment of tuberculosis, and methods for the preparation of such compounds, are provided.
    Type: Application
    Filed: October 11, 2011
    Publication date: August 8, 2013
    Applicant: GLAXO GROUP LIMITED
    Inventors: Julia Castro Pichel, Raquel Fernandez Menendez, Esther Pilar Fernandez Velando, Silvia Gonzalez Del Valle, Araceli Mallo-Rubio
  • Publication number: 20130203747
    Abstract: Compounds of formula I: wherein a, R1, R2, R3, R4, R5 and R6 are defined herein, are useful as inhibitors of HIV replication.
    Type: Application
    Filed: November 21, 2012
    Publication date: August 8, 2013
    Applicant: Gilead Sciences, Inc.
    Inventor: Gilead Sciences, Inc.
  • Publication number: 20130196952
    Abstract: The invention relates to compounds of Formula (1) and to processes for the preparation of intermediates used in the preparation of compositions containing and the uses of such derivatives. The compounds according to the present invention are useful in numerous diseases in which ALK protein is involved or in which inhibition of ALK activity may induce benefit, especially for the treatment of cancer mediated by a mutated EML4-ALK fusion protein.
    Type: Application
    Filed: May 4, 2011
    Publication date: August 1, 2013
    Applicant: PFIZER INC.
    Inventors: Mark Edward Bunnage, Andrew Simon Cook, Jingrong Jean Cui, Kevin Nell Dack, Judith Gail Deal, Danlin Gu, Mingying He, Patrick Stephen Johnson, Ted William Johnson, Phuong Thi Quy Le, Cynthia Louise Palmer, Hong Shen
  • Patent number: 8481543
    Abstract: A compound, particularly an antimalarial compound, according to formula I: or a pharmaceutically acceptable salt thereof, wherein: X is an electron-withdrawing group; A is an optionally substituted alkanediyl or an optionally substituted cycloalkanediyl that includes 2 to 5 carbon atoms; and R1 and R2 are each individually H, tert-butyl, isopropyl, or optionally substituted cycloalkyl.
    Type: Grant
    Filed: November 17, 2009
    Date of Patent: July 9, 2013
    Assignees: Oregon Health & Science University, The United States of America as represented by the Department of Veterans Affairs
    Inventors: Michael K. Riscoe, Rolf W. Winter, David J. Hinrichs
  • Publication number: 20130158034
    Abstract: Compounds of Formula I are useful as antagonists of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.
    Type: Application
    Filed: June 21, 2012
    Publication date: June 20, 2013
    Applicant: Amgen Inc.
    Inventors: James BROWN, Jian J. CHEN, Vijay Keshav GORE, Scott HARRIED, Daniel B. Horne, Matthew R. KALLER, Qingyian LIU, Holger MONENSCHEIN, Thomas T. NGUYEN, Nobuko NISHIMURA, Wenge ZHONG
  • Publication number: 20130158031
    Abstract: This invention relates to novel alkyne-bridged hetero-aromatics as described in the specification which are PDE10A inhibitors and useful for the treatment of neurological, psychiatric disorder, metabolic disorders, such as Schizophrenia, Parkinson's disease, Huntington's disease, Alzheimer's disease, learning memory disorder, drug addiction (abuse), sleeping disorder, depression, obesity, non-insulin dependent diabetes, bipolar disorder, obsessive compulsive disorder, or pain; to process for their preparation; to pharmaceutical compositions comprising them; and to methods of using them.
    Type: Application
    Filed: December 18, 2012
    Publication date: June 20, 2013
    Applicant: SU ZHOU JING HONG BIOTECH CO., LTD.
    Inventors: Zhen-Wei CAI, Ding ZHOU, Yougang LIN, Ping CHEN
  • Publication number: 20130116275
    Abstract: Inhibitors of the Hypoxia Inducible Factor (HIF) and angiogenesis and their methods of use including the treatment of cancer, hypoxia related pathologies, disorders leading to ischemia, for example stroke and ischemic heart disease, and non-cancerous angiogenic diseases are provided.
    Type: Application
    Filed: April 20, 2011
    Publication date: May 9, 2013
    Applicants: GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, EMORY UNIVERSITY
    Inventors: Erwin G. Van Meir, Binghe Wang
  • Publication number: 20130102756
    Abstract: A curable resin comprising a compound having the structure (I): wherein each carbon 2, together with either its carbon 1 or carbon 3, arc members of a fused cycloaliphatic ring, and when carbon 1 is a member of the ring so is N, and wherein each of the aliphatic or aromatic ring-member carbons may either be members of further fused cycloaliphatic rings or be bonded to a group selected from H or linear or branched C1 to C5 alkyl.
    Type: Application
    Filed: March 21, 2011
    Publication date: April 25, 2013
    Applicant: HEXCEL COMPOSITES LIMITED
    Inventor: John Cawse
  • Patent number: 8420812
    Abstract: A process for the palladium-catalyzed coupling of terminal alkynes with heteroaryl tosylates and heteroaryl benzenesulfonates The present invention relates to a process for the regioselective synthesis of compounds of the formula (I), wherein D, J and W have the meanings indicated in the claims. The present invention provides an efficient and general palladium-catalyzed coupling process of heteroaryl tosylates with terminal alkynes to a wide variety of substituted, multifunctional heteroaryl-1-alkynes of the formula I.
    Type: Grant
    Filed: December 23, 2009
    Date of Patent: April 16, 2013
    Assignee: Sanofi
    Inventors: Omar Rkyek, Marc Nazare, Andreas Lindenschmidt, Jorge Alonso, Matthias Urmann, Nis Halland
  • Publication number: 20130065893
    Abstract: The present invention provides a compound of formula (I) or pharmaceutically acceptable salt thereof, wherein the variables R1, R2, R3, R4, R5, R7 and p are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: November 29, 2010
    Publication date: March 14, 2013
    Applicant: NOVARTIS AG
    Inventors: Robert Sun, Lauren G. Monovich, Sylvie Chamoin, John Westbrook
  • Patent number: 8349830
    Abstract: The present invention is directed to aryl aminopyridine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Grant
    Filed: October 26, 2010
    Date of Patent: January 8, 2013
    Assignee: Merck Sharp & Dohme
    Inventors: Michael J. Breslin, Christopher D. Cox, Izzat T. Raheem
  • Publication number: 20130005705
    Abstract: The present invention relates to novel carboxamide compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating or controlling medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.
    Type: Application
    Filed: June 27, 2012
    Publication date: January 3, 2013
    Applicants: Abbott Laboratories, Abbott GmbH & Co. KG
    Inventors: Hervé Geneste, Michael Ochse, Karla Drescher, Berthold Behl, Loic Laplanche, Jürgen Dinges, Clarissa Jakob
  • Publication number: 20120329772
    Abstract: A compound having Formula (I) or Formula (II) is disclosed as an P2X7 antagonist, wherein A, B, C, Y, Y, Z, m, v, R1, R2, R3, R4, and R5, are as defined in the description. Methods and compositions for treating disease or condition modulated by P2X7 are also disclosed.
    Type: Application
    Filed: July 9, 2012
    Publication date: December 27, 2012
    Applicant: ABBOTT LABORATORIES
    Inventors: William A. Carroll, Arturo Perez-Medrano, Alan S. Florjancic, Derek W. Nelson, Sridhar Peddi, Tongmei Li, Eric M. Bunnelle, Gavin Hirst, Biqin C. Li