Chalcogen Bonded Directly To Ring Carbon Of The Six-membered Hetero Ring Patents (Class 546/24)
  • Patent number: 9809545
    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 thromboses, embolisms, hypercoaguability or fibrotic changes.
    Type: Grant
    Filed: March 21, 2014
    Date of Patent: November 7, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Anthony Ogawa, Scott Edmondson, Mark Erion, Santhosh Neelamkavil, Zhuyan Guo, Rudrajit Mal, Jiafang He, Weiguo Liu, Ellen K. Vande Bunte
  • Patent number: 9546138
    Abstract: A compound of Formula (I) is provided that has been shown to be useful for treating a disease, disorder or syndrome that is mediated by the inhibition of mycolic acid biosynthesis through inhibition of M. tuberculosis Enoyl Acyl Carrier Protein Reductase enzyme (InhA): wherein R1, R2, R3, R4 and R5 are as defined herein.
    Type: Grant
    Filed: December 12, 2013
    Date of Patent: January 17, 2017
    Assignee: Novartis AG
    Inventors: Ravinder Reddy Kondreddi, Ngai Ling Ma, Stefan Peukert, Srinivasa P S Rao, Manjunatha Ujjini
  • Patent number: 9040175
    Abstract: The present invention relates to an electronic device comprising at least one organic semiconducting material according to the following formula (I): wherein R1-4 are independently selected from H, halogen, CN, substituted or unsubstituted C1-C20-alkyl or heteroalkyl, C6-C20-aryl or C5-C20-heteroaryl, C1-C20-alkoxy or C6-C20-aryloxy, Ar is selected from substituted or unsubstituted C6-C20-aryl or C5-C20-heteroaryl, and R5 is selected from substituted or unsubstituted C6-C20-aryl or C5-C20-heteroaryl, H, F or formula (II).
    Type: Grant
    Filed: June 8, 2011
    Date of Patent: May 26, 2015
    Assignee: NOVALED AG
    Inventors: Omrane Fadhel, Ramona Pretsch
  • Publication number: 20150119366
    Abstract: Pharmaceutical compositions of the invention comprise alkylated imino sugars derivatives having a disease-modifying action in the treatment of diseases associated with glucosidase activity that include Viral hemorrhagic fevers, and any other diseases involving glucosidase activity.
    Type: Application
    Filed: March 27, 2013
    Publication date: April 30, 2015
    Inventors: Yanming Du, Xiaodong Xu, Hong Ye, Jinhong Chang, Timothy M. Block
  • Patent number: 9017829
    Abstract: The present invention relates to a material for an organic electroluminescent device, including a phenanthrocarbazole-based compound having a specific structure, and an organic electroluminescent device including the same. More specifically, the phenanthrocarbazole-based compound is applied as a material for a phosphorescent and fluorescent organic electroluminescent device, thereby providing an organic light emitting device with improved light emitting efficiency, luminance, thermal stability, driving voltage, lifetime and the like.
    Type: Grant
    Filed: May 6, 2011
    Date of Patent: April 28, 2015
    Assignee: Doosan Corporation
    Inventors: Jin-Seok Hong, Eun Jung Lee, Shin Han Kim, Kyoung-Soo Kim
  • Patent number: 8999530
    Abstract: The present invention provides a new compound and an organic electronic device using the same. The compound according to the present invention may serve as hole injection, hole transporting, electron injection and transporting, and light emitting materials and the like in an organic electronic device comprising an organic light emitting device, and the organic electronic device according to the present invention shows excellent properties in terms of efficiency, driving voltage and service life.
    Type: Grant
    Filed: June 12, 2012
    Date of Patent: April 7, 2015
    Assignee: LG Chem, Ltd.
    Inventors: Changhwan Shin, Kongkyeom Kim, Dong Hoon Lee, Jungi Jang, Minseung Chun
  • Patent number: 8986852
    Abstract: The present invention relates to the compounds of the formula (1) and to organic electroluminescent devices, in particular blue-emitting devices, in which these compounds are used as host material or dopant in the emitting layer and/or as hole-transport material and/or as electron-transport material.
    Type: Grant
    Filed: April 29, 2008
    Date of Patent: March 24, 2015
    Assignee: Merck Patent GmbH
    Inventors: Philipp Stoessel, Arne Buesing, Holger Heil
  • Patent number: 8986858
    Abstract: Disclosed is an organic electroluminescent device (organic EL device) that is improved in luminous efficiency, sufficiently secures driving stability, and has a simple configuration. This organic EL device comprises organic layers between an anode and a cathode piled one upon another on a substrate and at least one organic layer selected from a light-emitting layer, a hole-transporting layer, an electron-transporting layer, and a hole-blocking layer contains a carbazole compound represented by the following formula (1). In the case where the light-emitting layer of the organic electroluminescent device contains a phosphorescent dopant and a host material, it is the carbazole compound that is contained as the host material.
    Type: Grant
    Filed: January 27, 2011
    Date of Patent: March 24, 2015
    Assignee: Nippon Steel & Sumikin Chemical Co., Ltd.
    Inventors: Masashi Tada, Junya Ogawa, Takahiro Kai, Megumi Matsumoto, Yasuhisa Tsutsumi
  • Patent number: 8951647
    Abstract: The present invention relates to organic electroluminescent devices which comprise fluorene derivatives and spirobifluorene derivatives as matrix material for phosphorescent emitters.
    Type: Grant
    Filed: July 8, 2009
    Date of Patent: February 10, 2015
    Assignee: Merck Patent GmbH
    Inventors: Amir Hossain Parham, Joachim Kaiser, Anja Gerhard, Jonas Valentin Kroeber
  • Patent number: 8945728
    Abstract: The invention provides an organic compound incorporating a specific structure into a pyridine skeleton or a 1,3,5-triazine skeleton and adapting the molecular weight to a specific range, a composition comprising the organic compound and a solvent, organic electroluminescent element comprising a layer that is formed by using the composition, and the uses thereof.
    Type: Grant
    Filed: October 7, 2013
    Date of Patent: February 3, 2015
    Assignee: Mitsubishi Chemical Corporation
    Inventors: Koichi Ishibashi, Hideki Gorohmaru, Wataru Shimizu, Tomomi Okamoto
  • Publication number: 20150018555
    Abstract: The invention relates to a series of novel chiral nitrogen-phosphorus ligands of formulae (Ia) and (Ib): wherein R1-R3 and X are as defined herein. The invention also relates to chiral metal complexes prepared with these chiral nitrogen-phosphorus ligands. The chiral metal complexes are useful as catalysts for carrying out asymmetric hydrogenation.
    Type: Application
    Filed: July 9, 2014
    Publication date: January 15, 2015
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Nizar HADDAD, Bo QU, Jolaine SAVOIE, Chris Hugh SENANAYAKE, Xudong WEI
  • Patent number: 8911886
    Abstract: A material for electroluminescent devices which comprises a compound in which a heterocyclic group having nitrogen is bonded to carbazolyl group and an organic electroluminescent device having at least one organic thin film layer which is sandwiched between the cathode and the anode and contains the above material in at least one layer, are provided. The material can provide organic electroluminescent devices emitting bluish light with a high purity of color. The organic electroluminescence device uses the material.
    Type: Grant
    Filed: August 30, 2013
    Date of Patent: December 16, 2014
    Assignee: Idemitsu Kosan Co., Ltd.
    Inventors: Toshihiro Iwakuma, Chishio Hosokawa, Hidetsugu Ikeda, Seiji Tomita, Takashi Arakane
  • Patent number: 8846214
    Abstract: An amine derivative represented by the following general formula (1) and exhibiting a temperature difference of 30° C. or more as defined by the difference of [decomposition temperature (° C.) minus sublimation temperature (° C.)]: wherein R1 and R2 independently represent a substituted or unsubstituted C6-40 aryl or C5-40 heteroaryl group; and R3 and R4 independently represent a hydrogen atom, a straight-chain, branched or cyclic C1-18 alkyl or C1-18 alkoxy group, or a substituted or unsubstituted C6-40 aryl or C5-40 heteroaryl group, provided that R3 and R4 may form together a cyclic hydrocarbon group. The amine derivative is useful as an organic electroluminescent material.
    Type: Grant
    Filed: June 2, 2010
    Date of Patent: September 30, 2014
    Assignee: Tosoh Corporation
    Inventors: Shinichi Ishikawa, Naoki Matsumoto, Takanori Miyazaki, Yasushi Hara
  • Patent number: 8791091
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.
    Type: Grant
    Filed: November 29, 2012
    Date of Patent: July 29, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Huji Turdi, Jon J. Hangeland, R. Michael Lawrence, Saleem Ahmad, Wei Meng, Robert Paul Brigance, Pratik Devasthale, Guohua Zhao
  • Publication number: 20140199243
    Abstract: Compounds of the following Formula (I): in which A represents either a nitrogen atom, or a ring having 3 to 6 carbon atoms, or an aromatic ring having 5 to 10 members, the ring and the aromatic ring optionally include one or more heteroatoms selected from N, O and S, and W represents a grafting function and X and Y represent chelating functions.
    Type: Application
    Filed: June 18, 2012
    Publication date: July 17, 2014
    Applicant: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Loic Charbonniere, Câline Christine, Alexandre Lecointre, Katia Nchmimi Nono
  • Publication number: 20140193801
    Abstract: A composition, method and kit for performing a two-reagent enzymatic homocysteine assay, wherein a single homocysteinase enzyme and a Schiff-based conjugate of N,N-dibutyl-p-phenyldiamine (DBPDA) with pyridoxal 5?-phosphate (PLP) are used to measure total homocysteine in plasma or serum. The assay measures a chromophore reaction product of H2S and the DBPDA released from the Schiff-base conjugate in the presence of a Fe+3 containing compound. The resulting chromophore may be measured absorbance or fluorescence spectrophotometry.
    Type: Application
    Filed: January 10, 2014
    Publication date: July 10, 2014
    Applicant: ANTICANCER, INC.
    Inventors: Yuying Tan, Shukuan Li
  • Publication number: 20140171393
    Abstract: The present invention relates to novel aromatic thio derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: December 9, 2013
    Publication date: June 19, 2014
    Applicant: Allergan, Inc.
    Inventors: Phong X. Nguyen, John R. Cappiello, Todd M. Heidelbaugh
  • Patent number: 8748012
    Abstract: Novel aryl silicon and aryl germanium host materials are described. These compounds improve OLED device performance when used as hosts in the emissive layer of the OLED.
    Type: Grant
    Filed: May 25, 2011
    Date of Patent: June 10, 2014
    Assignee: Universal Display Corporation
    Inventors: Lichang Zeng, Alexey B. Dyatkin, Gregg Kottas
  • Patent number: 8703300
    Abstract: Disclosed is a long-life organic electroluminescent element which can be driven at low voltage. Also disclosed are a display and illuminator using the same. Specifically disclosed is an organic electroluminescent element comprising on a substrate, an anode, a cathode and an organic compound layer arranged between the anode and the cathode and including at least one light emission layer. This organic electroluminescent element is characterized in that the organic compound layer includes an electron transport material-containing layer which contains an electron transport material represented by Formula (a) and at least one substance selected from the group consisting of metals, salts of the metals and electron-donating compounds. Formula (a) Ar1-(Ar2)n [In the formula, Ar1 represents a group derived from an aromatic hydrocarbon ring or a group derived from an aromatic heterocycle; Ar2 represents a group derived from an aromatic heterocycle; and n represents an integer of 2 or more.
    Type: Grant
    Filed: March 14, 2006
    Date of Patent: April 22, 2014
    Assignee: Konica Minolta Holdings, Inc.
    Inventors: Yoshiyuki Suzuri, Akira Kawakami, Hiroshi Kita
  • Publication number: 20140107075
    Abstract: The present invention relates to novel amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: February 21, 2013
    Publication date: April 17, 2014
    Applicant: ALLERGAN, INC.
    Inventors: TODD M. HEIDELBAUGH, PHONG X. NGUYEN
  • Patent number: 8679645
    Abstract: The present invention relates to novel materials which can be used in organic electronic devices, in particular electroluminescent devices, and are certain derivatives of fused aromatic systems.
    Type: Grant
    Filed: May 16, 2006
    Date of Patent: March 25, 2014
    Assignee: Merck Patent GmbH
    Inventors: Holger Heil, Arne Buesing, Philipp Stoessel, Horst Vestweber
  • Patent number: 8653270
    Abstract: The present invention relates to novel derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: November 18, 2011
    Date of Patent: February 18, 2014
    Assignee: Allergan, Inc.
    Inventors: Todd M. Heidelbaugh, Phong X. Nguyen
  • Patent number: 8617722
    Abstract: The present invention provides a polymer material capable of preparing organic EL elements having low driving voltage and high durability. The polymer compound of the present invention includes a constituting unit derived from a monomer represented by the formula (1); (in the formula (1), each of A1's is independently a condensed polycyclic aromatic group optionally having a heteroatom as a ring-constituting atom; the condensed polycyclic aromatic group links to A2 at the meta position to the bonding position of the ring represented by the following formula; each of A2's is independently a six-membered ring aromatic group optionally having a heteroatom as a ring-constituting atom; at least one of A1 and A2 has a substituent having a polymerizable functional group; at least one of X's is a nitrogen atom, and n's are independently 1 or 2).
    Type: Grant
    Filed: February 20, 2009
    Date of Patent: December 31, 2013
    Assignee: Showa Denko K.K.
    Inventors: Masahiko Toba, Tsuyoshi Kato
  • Publication number: 20130338110
    Abstract: The inventions disclosed include methods of treating cancers and related neoplasias, especially prostate cancer, with pharmaceutically acceptable salts comprising lipophilic cation moieties linked to nitroxide or linked to hydroxylamine anti-oxidant groups.
    Type: Application
    Filed: May 20, 2013
    Publication date: December 19, 2013
    Inventors: David A. ZARLING, Hirak S. BASU, Balaraman KALYANARAMAN, Joy JOSEPH
  • Patent number: 8609637
    Abstract: A prodrug can have a structure of Formula 10 or derivative thereof or stereoisomer thereof or pharmaceutically acceptable salt thereof. The prodrug can be included in a pharmaceutical composition for use in treatment of fungus, cancer, dermatitis, superficial mycoses; inflammation, tinea pedis, tinea cruris, and tinea corporis, Trichophyton rubrum, Trichophyton mentagrophytes, Epidermophyton floccosum, and Microsporum canis, candidiasis (moniliasis), Candida albicans, tinea (pityriasis) vesicolor, Malassezia furfur, acute myeloid leukemia, acute lymphoid leukemia, chronic myelogenous leukemia, lymphoma or multiple myeloma.
    Type: Grant
    Filed: December 2, 2011
    Date of Patent: December 17, 2013
    Assignee: The University of Kansas
    Inventors: Mehmet Tanol, Scott J. Weir
  • Patent number: 8530183
    Abstract: The present invention provides compounds for use as zinc ligand sensors in cellular imaging. These compounds are sensitive imaging agents that can be used with techniques such a laser scanning microscopy in intact cells in culture or in tissue preparations.
    Type: Grant
    Filed: June 10, 2011
    Date of Patent: September 10, 2013
    Assignee: The Board of Regents of the University of Texas System
    Inventors: Wen-Hong Li, Daliang Li
  • Patent number: 8512877
    Abstract: Naphthylcarbazole derivatives are provided. The naphthylcarbazole derivatives are represented by Formula 1. Further provided are KL host materials, organic electroluminescent devices employing the host materials, and displays and lighting systems comprising the devices.
    Type: Grant
    Filed: March 27, 2008
    Date of Patent: August 20, 2013
    Assignee: Dongwoo Fine-Chem
    Inventors: Kyong Min Kang, Deug Sang Lee, Chang Jun Lee, Kyoung Moon Go, Jong Soon Lee, Se Hoon Kim
  • Publication number: 20130203704
    Abstract: Disclosed are novel compounds having the structure of Formula (I): which are useful for treating mammals for dependence upon substances of addiction, for example addiction to a dopamine-producing agent such as cocaine, morphine, amphetamines, nicotine, and/or alcohol. Also disclosed are pharmaceutical compositions comprising a therapeutically effective amount of a compound of Formula (I) and methods of using the compounds of Formula (I) in the treatment of addiction to a dopamine-producing agent.
    Type: Application
    Filed: March 8, 2013
    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
  • Publication number: 20130178444
    Abstract: The present application describes prodrugs of the compound of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis using the prodrug compounds of the invention are disclosed.
    Type: Application
    Filed: March 5, 2013
    Publication date: July 11, 2013
    Inventor: Bristol-Myers Squibb Company
  • Publication number: 20130157982
    Abstract: The present invention relates to novel amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: February 11, 2013
    Publication date: June 20, 2013
    Applicant: ALLERGAN, INC.
    Inventor: ALLERGAN, INC.
  • Publication number: 20130143843
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.
    Type: Application
    Filed: November 29, 2012
    Publication date: June 6, 2013
    Inventor: Bristol-Myers Squibb Company
  • Patent number: 8420230
    Abstract: Provided is an organic light emitting diode employing a luminescent efficiency improvement layer containing a compound represented by Formula 1 below: The OLED including the luminescent efficiency improvement layer containing the compound represented by Formula 1 can have excellent luminescent efficiency.
    Type: Grant
    Filed: August 14, 2009
    Date of Patent: April 16, 2013
    Assignee: Samsung Display Co., Ltd.
    Inventors: Seung-Gak Yang, Hee-Yeon Kim, Jae-Yong Lee, Jong-Hyuk Lee
  • Patent number: 8378100
    Abstract: The present invention provides ?-hydroxy phosphonate compounds that are autotaxin inhibitors.
    Type: Grant
    Filed: January 9, 2009
    Date of Patent: February 19, 2013
    Assignee: University of Virginia Patent Foundation
    Inventors: Kevin R. Lynch, Timothy L. Macdonald
  • Publication number: 20130005689
    Abstract: Disclosed are novel compounds having the structure of Formula (I): which are useful for treating mammals for dependence upon substances of addiction, for example addiction to a dopamine-producing agent such as cocaine, morphine, amphetamines, nicotine, and/or alcohol. Also disclosed are pharmaceutical compositions comprising a therapeutically effective amount of a compound of Formula (I) and methods of using the compounds of Formula (I) in the treatment of addiction to a dopamine-producing agent.
    Type: Application
    Filed: June 29, 2012
    Publication date: January 3, 2013
    Applicant: Gilead Sciences, Inc.
    Inventors: Carina E. Cannizzaro, Michael Graupe, Juan A. Guerrero, Yafan Lu, Robert G. Strickley, Chandrasekar Venkataramani, Jeff Zablocki
  • Publication number: 20120220551
    Abstract: The present invention relates to compounds represented by formula (I), which can modulate the activity of protein kinases. The invention also relates to a composition containing a compound of formula (I), and a method for synthesizing and using such compound for preventing or treating ALK or cMet mediated disorders or conditions.
    Type: Application
    Filed: February 22, 2012
    Publication date: August 30, 2012
    Applicant: Eternity Bioscience Inc.
    Inventors: Baihua Hu, Kan He, Minsheng Zhang
  • Publication number: 20120194894
    Abstract: Disclosed are electrochromic compounds represented by the formulas defined in the specification.
    Type: Application
    Filed: October 8, 2010
    Publication date: August 2, 2012
    Applicant: RICOH COMPANY, LTD.
    Inventors: Tohru Yashiro, Shigenobu Hirano, Yousuke Manabe, Satoshi Hayashi
  • Publication number: 20120142637
    Abstract: A prodrug can have a structure of Formula 10 or derivative thereof or stereoisomer thereof or pharmaceutically acceptable salt thereof. The prodrug can be included in a pharmaceutical composition for use in treatment of fungus, cancer, dermatitis, superficial mycoses; inflammation, tinea pedis, tinea cruris, and tinea corporis, Trichophyton rubrum, Trichophyton mentagrophytes, Epidermophyton floccosum, and Microsporum canis, candidiasis (moniliasis), Candida albicans, tinea (pityriasis) vesicolor, Malassezia furfur, acute myeloid leukemia, acute lymphoid leukemia, chronic myelogenous leukemia, lymphoma or multiple myeloma.
    Type: Application
    Filed: December 2, 2011
    Publication date: June 7, 2012
    Applicant: THE UNIVERSITY OF KANSAS
    Inventors: Mehmet Tanol, Scott J. Weir
  • Publication number: 20120129813
    Abstract: The present invention relates to novel derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: November 18, 2011
    Publication date: May 24, 2012
    Inventors: Todd M. Heidelbaugh, Phong X. Nguyen
  • Publication number: 20120129812
    Abstract: Provided is a heterocyclic derivative showing a thyroid hormone ? receptor agonist action, which is effective for the prophylaxis or treatment of the diseases relating to the action. A compound represented by the formula [I]: wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, and a medicament containing the compound as an active ingredient.
    Type: Application
    Filed: April 19, 2010
    Publication date: May 24, 2012
    Applicant: MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Shinji Kawata, Koji Matsumoto, Maki Nijima, Taichi Takahashi
  • Publication number: 20120122820
    Abstract: The present application relates to prodrug derivatives of 2-amino-6-({[2-(4-chlorophenyl)-1,3-thiazol-4-yl]methyl}thio)-4-[4-(2-hydroxyethoxy)phenyl]pyridine-3,5-dicarbonitrile, processes for their preparation, 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 of cardiovascular disorders.
    Type: Application
    Filed: July 23, 2008
    Publication date: May 17, 2012
    Inventors: Nicole Diedrichs, Thomas Krahn, Ursula Krenz, Jörg Keldenich, Hanna Tinel, Claudia Hirth-Dietrich, Hans-Georg Lerchen
  • Patent number: 8133882
    Abstract: Provided are quinolone derivatives having a lower alkyl or cycloalkyl at the 1-position; —N(R0)C(O)-lower alkylene-CO2R0, lower alkylene-CO2R0, lower alkenylene-CO2R0, —O-lower alkylene-CO2R0, —O-(lower alkylene which may be substituted with —CO2R0)-aryl or —O-lower alkenylene-CO2R0 (wherein R0 is H or lower alkyl) at the 3-position; halogen at the 6-position; and amino group substituted with a substituent group having a ring structure at the 7-position, respectively, or pharmaceutically acceptable salts thereof. Pharmaceutical composition containing the quinolone derivatives and methods of using the compositions are provided.
    Type: Grant
    Filed: March 14, 2007
    Date of Patent: March 13, 2012
    Assignee: Astellas Pharma Inc
    Inventors: Yuji Koga, Takao Okuda, Susumu Watanuki, Takashi Kamikubo, Fukushi Hirayama, Hiroyuki Moritomo, Jiro Fujiyasu, Michihito Kageyama, Toshio Uemura, Jun Takasaki
  • Patent number: 8124768
    Abstract: Disclosed are compounds of Formula (I): and salts thereof. Also, disclosed are methods of using the compounds in the treatment of proliferative diseases, such as cancer, and to pharmaceutical compositions comprising at least one compound of Formula (I) or a pharmaceutically acceptable salt.
    Type: Grant
    Filed: January 22, 2009
    Date of Patent: February 28, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: Robert M. Borzilleri, Zhen-Wei Cai
  • Publication number: 20120029021
    Abstract: Nitroxide free radicals attached to antineoplastic agents can synergize their potencies to cancer cells. This invention relates to any antineoplastic agents and their derivatives chemically attached with nitroxide free radicals, such as TEMPO and its radical derivatives. This invention also relates to precursors of such compounds, as well as the products formed from the adducts after administration.
    Type: Application
    Filed: January 17, 2011
    Publication date: February 2, 2012
    Applicant: THE TRUSTEES OF CALIFORNIA STATE UNIVERSITY
    Inventors: Yong Ba, Errol V. Mathias
  • Publication number: 20120015908
    Abstract: A compound of Formula I is disclosed as follows: or a pharmaceutically acceptable salt, prodrug, solvate, or metabolite thereof, wherein R is hydrogen, P(?O)(OH)2, P(?O)(O(C1-C18)alkylene(C6-C20)aryl)2, P(?O)(OH)(OM), P(?O)(OM)2, P?O(O2M), S(?O)(OH)2, S(?O)(O(C1-C18)alkylene(C6-C20)aryl)2, S(?O)(OH)(OM), S(?O)(OM)2; M is a monovalent or divalent metal ion, or alkylammonium ion; W is (C6-C20)aryl, (C6-C20)heteroaryl, (C1-C18)alkyl(C6-C20)aryl, (C1-C18)alkyl(C6-C20)heteroaryl, hydroxy(C6-C20)aryl, hydroxy(C6-C20)heteroaryl, (C1-C18)alkoxy(C6-C20)aryl, (C1-C18)alkoxy(C6-C20)heteroaryl, (C1-C18)alkylenedioxy(C6-C20)aryl, (C1-C18)alkylenedioxy(C6-C20)heteroaryl, halo(C6-C20)aryl, halo(C6-C20)heteroaryl, (C1-C18)alkylamino(C6-C20)aryl, (C1-C18)alkylamino(C6-C20)heteroaryl, (C1-C18)cycloalkylamino(C6-C20)aryl, or (C1-C18)cycloalkylamino(C6-C20)heteroaryl, and their OR8 substutes; R5 is (C1-C18alkoxy, hydrogen, hydroxyl, O—(C1-C18)alkyl(C6-C20)aryl, halo or OR8, or R5 and R6 are (C1-C18)dioxy provided that R7 i
    Type: Application
    Filed: July 13, 2011
    Publication date: January 19, 2012
    Applicant: Efficient Pharma Management Corporate
    Inventors: Sheng-Chu Kuo, Kuo-Hsiung Lee, Li-Jiau Huang, Li-Chen Chou, Tian-Shung Wu, Tzong-Der Way, Jing-Gung Chung, Jai-Sing Yang, Chi-Hung Huang, Meng-Tung Tsai
  • Publication number: 20110274679
    Abstract: Compositions and methods of SIRT activation are presented in which one or more vitamin compounds, and especially vitamin B compounds are used to significantly increase SIRT activity in vitro and in vivo. In especially preferred compositions, vitamin B6, vitamin B12, and vitamin B2 are present in synergistic quantities.
    Type: Application
    Filed: November 5, 2009
    Publication date: November 10, 2011
    Applicant: VDF FutureCeuticals, Inc.
    Inventor: Zbigniew Pietrzkowski
  • Publication number: 20110218174
    Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
    Type: Application
    Filed: October 22, 2009
    Publication date: September 8, 2011
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Jianming Bao, Ping Lan, Huagang Lu, Gergely M. Makara, F. Anthony Romero, Iyassu Sebhat, Dariusz Wodka, Qun Dang, De Michael Chung, Tony S. Gibson, Hongjian Jiang, Daniel K. Cashion
  • Patent number: 8012949
    Abstract: The disclosure provides, inter alia, novel bisphosphonate compounds and methods of making and using such compounds. In certain embodiments, compounds of the invention include bisphosphonates that are capable of selectively inhibiting one or more of farnesyl diphosphate synthase (FPPS), geranylgeranyl diphosphate synthase (GGPPS), and decaprenyl pyrophosphate synthase (DPPS). In preferred embodiments, compounds of the invention are capable of selectively inhibiting two or more of FPPS, GGPPS, and DPPS. In embodiments, compounds and methods of the invention demonstrate superior activity levels, such as in the anti-cancer context, immunostimulation context, and other contexts, which in several cases exceed the activity levels of previous generation bisphosphonate drugs by orders of magnitude. In embodiments, the invention provides compounds and methods in connection with research and therapeutic applications, e.g.
    Type: Grant
    Filed: April 11, 2008
    Date of Patent: September 6, 2011
    Assignee: The Board of Trustees of the University of Illinois
    Inventors: Eric Oldfield, Yonghui Zhang, Fenglin Yin
  • Publication number: 20110104110
    Abstract: The present invention relates to Substituted Indole Derivatives, compositions comprising at least one Substituted Indole Derivative, and methods of using these Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Application
    Filed: August 27, 2008
    Publication date: May 5, 2011
    Inventors: Gopinadhan N. Anikumar, Frank Bennett, Tin-Yau Chan, Kevin X. Chen, Mousumi Sannigrahi, Francisco Velazquez, Srikanth Venkatraman, Qingbei Zeng, Jose S. Duca, Charles A. Lesburg, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Neng-Yang Shih
  • Publication number: 20110082113
    Abstract: The present application describes prodrugs of the compound of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis using the prodrug compounds of the invention are disclosed.
    Type: Application
    Filed: October 4, 2010
    Publication date: April 7, 2011
    Inventors: John Hynes, Percy H. Carter, Lyndon A.M. Cornelius, T.G. Murali Dhar, John V. Duncia, Joseph B. Santella, Hong Wu, Satheesh Nair, Jayakumar S. Warrier