Polycyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 549/348)
  • Patent number: 12156915
    Abstract: New compositions are provided containing artemisinin dimers with high activity as anti-protozoal agents, including anti-malarial and anti-leishmanial properties, and methods for the treatment of protozoal infections, including malaria or leishmaniasis.
    Type: Grant
    Filed: February 25, 2020
    Date of Patent: December 3, 2024
    Inventors: Mahmoud A. ElSohly, Waseem Gul
  • Patent number: 11559556
    Abstract: Methods disclosed herein provide for an environmentally-friendly approach that employ citric extracts from fruits as unique reducing and stabilizing agents for making a tellurium nanomaterial. A particular method of making a tellurium nanomaterial includes combining citrus fruit extract with a tellurium salt to form a mixture of citrus fruit extract and dissolved tellurium salt; and heating the mixture of citrus fruit extract and dissolved tellurium salt, thereby making the tellurium nanomaterial. The resulting nanoparticles exhibit enhanced and desirable biomedical properties toward treatment of both infectious diseases and cancer.
    Type: Grant
    Filed: March 13, 2020
    Date of Patent: January 24, 2023
    Assignee: Northeastern University
    Inventors: David Medina Cruz, William Tien-Street, Bohan Zhang, Xinjing Huang, Ada Vernet Crua, Thomas J. Webster
  • Patent number: 11365202
    Abstract: The present invention provides a new artemisinin-dipeptidyl vinyl based compound of Formula (I) or a pharmaceutically acceptable salt thereof and a process for the preparation thereof. The present invention further also provides a pharmaceutical composition comprising compounds of Formula (I) or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, diluent or excipient to treat malaria.
    Type: Grant
    Filed: April 16, 2019
    Date of Patent: June 21, 2022
    Assignees: Council of Scientific and Industrial Research, International Centre for Genetic Engineering and Biotechnology (ICGEB)
    Inventors: Asish Kumar Bhattacharya, Eswar Kumar Aratikatla, Pawan Malhotra, Asif Mohmmed
  • Patent number: 11077161
    Abstract: This invention relates to methods for administering an effective amount of a dietary or nutritional supplement composition that effectively changes the levels of biomarkers in the synovium of a joint and resulting in decreased pain and ultimately better outcomes for subjects. The formulation comprises an effective amount of the following: Boswellia; Vitamin C; Ginger; Turmeric; Vitamin D3; and Rutin. In a preferred embodiment of the composition of the invention, the composition is substantially free of omega-3 fatty acids.
    Type: Grant
    Filed: March 16, 2018
    Date of Patent: August 3, 2021
    Assignee: Orthopedic Solutions LLC
    Inventors: Michael B. Gross, Javad Parvizi
  • Patent number: 10676481
    Abstract: The invention relates to methods and intermediates useful in the synthesis of eribulin.
    Type: Grant
    Filed: February 10, 2017
    Date of Patent: June 9, 2020
    Assignee: EISAI R&D MANAGEMENT CO., LTD.
    Inventors: Phil S. Baran, Charles E. Chase, Francis G. Fang
  • Patent number: 10450324
    Abstract: In general, the present invention features improved methods useful for the synthesis of analogs of halichondrin B, such as eribulin and pharmaceutically acceptable salts thereof (e.g., eribulin mesylate).
    Type: Grant
    Filed: July 10, 2018
    Date of Patent: October 22, 2019
    Assignee: EISAI R&D MANAGEMENT CO., LTD.
    Inventors: Yongbo Hu, Huiming Zhang, Hiroyuki Chiba, Yuki Komatsu, Bryan M. Lewis
  • Patent number: 10308661
    Abstract: The invention provides methods for the synthesis of a halichondrin macrolides through a macrocyclization strategy. The macrocyclization strategy of the present invention involves subjecting a non-macrocyclic intermediate to a carbon-carbon bond-forming reaction (e.g., an olefination reaction (e.g., Homer-Wadsworth-Emmons olefination), catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic macrolide. The invention also provides compounds useful as intermediates in the synthesis of a halichondrin macrolides and methods for preparing the same.
    Type: Grant
    Filed: May 9, 2016
    Date of Patent: June 4, 2019
    Assignee: EISAI R&D MANAGEMENT CO., LTD.
    Inventors: Francis G. Fang, Dae-Shik Kim, Hyeong-Wook Choi, Charles E. Chase
  • Patent number: 9783549
    Abstract: The invention provides methods for the synthesis of eribulin or a pharmaceutically acceptable salt thereof (e.g., eribulin mesylate) through a macrocyclization strategy. The macrocyclization strategy of the present invention involves subjecting a non-macrocyclic intermediate to a carbon-carbon bond-forming reaction (e.g., an olefination reaction (e.g., Homer-Wadsworth-Emmons olefination), Dieckmann reaction, catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic intermediate. The invention also provides compounds useful as intermediates in the synthesis of eribulin or a pharmaceutically acceptable salt thereof and methods for preparing the same.
    Type: Grant
    Filed: November 4, 2014
    Date of Patent: October 10, 2017
    Assignee: EISAI R&D MANAGEMENT CO., LTD.
    Inventors: Francis G. Fang, Dae-Shik Kim, Hyeong-Wook Choi, Charles E. Chase, Jaemoon Lee
  • Patent number: 9695188
    Abstract: In general, the present invention features improved methods useful for the synthesis of analogs of halichondrin B, such as eribulin and pharmaceutically acceptable salts thereof (e.g., eribulin mesylate).
    Type: Grant
    Filed: March 3, 2016
    Date of Patent: July 4, 2017
    Assignee: EISAI R&D MANAGEMENT CO., LTD.
    Inventors: Yongbo Hu, Huiming Zhang, Hiroyuki Chiba, Yuki Komatsu, Bryan M. Lewis
  • Patent number: 9611273
    Abstract: Monomeric and dimeric trioxane thioacetals and methods of their use for treating subjects infected with malaria or other parasitic infectious diseases including, but not limited to, toxoplasmic infection; subjects afflicted with psychiatric conditions associated with toxoplasmic infection; and subjects afflicted with cancer.
    Type: Grant
    Filed: February 28, 2013
    Date of Patent: April 4, 2017
    Assignee: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Gary H. Posner, Alexander M. Jacobine, Rachel D. Slack, Jennifer R. Mazzone
  • Patent number: 9493480
    Abstract: Anilide derivatives of the natural trioxane artemisinin were prepared and evaluated for antimalarial efficacy in Plasmodium berghei-infected mice. Selected anilides derivatives administered orally as one single-digit dose combined with mefloquine hydrochloride were completely curative, i.e., all 5 of the mice in the particular treatment group had no detectable parasitemia on day 30 post infection, gained as much weight by day 30 post infection as the control mice (no infection), and behaved normally.
    Type: Grant
    Filed: April 16, 2012
    Date of Patent: November 15, 2016
    Assignee: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Gary H. Posner, Rachel D. Slack
  • Patent number: 9487538
    Abstract: Two-carbon linked artemisinin-derived trioxane dimers and methods of their use for treating subjects infected with malaria or other parasitic infectious diseases including, but not limited to, toxoplasmic infection; subjects afflicted with psychiatric conditions associated with toxoplasmic infection; and subjects afflicted with cancer.
    Type: Grant
    Filed: January 22, 2014
    Date of Patent: November 8, 2016
    Assignee: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Gary H. Posner, Bryan T. Mott
  • Patent number: 9409142
    Abstract: The present invention is directed to a method for producing artemisinin having the formula from dihydroartemisinic acid in a continuous flow reactor using singlet oxygen as well as to the continuous flow reactor for producing artemisinin.
    Type: Grant
    Filed: July 28, 2015
    Date of Patent: August 9, 2016
    Assignee: Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V.
    Inventors: Peter H. Seeberger, Daniel Kopetzki, Francois Lévesque
  • Patent number: 9303039
    Abstract: In general, the present invention features improved methods useful for the synthesis of analogs of halichondrin B, such as eribulin and pharmaceutically acceptable salts thereof (e.g., eribulin mesylate).
    Type: Grant
    Filed: December 5, 2014
    Date of Patent: April 5, 2016
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Huiming Zhang, Bryan M. Lewis
  • Patent number: 9278979
    Abstract: Disclosed is a compound of formula 1, or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, R6, R7, R7?, R8, R9, R10, R11, R12 and R13 are as disclosed herein. Also, disclosed is a process for the preparation of the compound of formula 1, or a pharmaceutically acceptable salt thereof, and intermediates used therein. The compound of formula 1 can be used in the preparation of halichondrin analogs, such as Eribulin; and a process for its preparation from the compound of formula 1 is also disclosed.
    Type: Grant
    Filed: March 28, 2013
    Date of Patent: March 8, 2016
    Assignee: ALPHORA RESEARCH INC.
    Inventors: Fabio E. S. Souza, Alena Rudolph, Ming Pan, Boris Gorin, Teng Ko Ngooi, Jason A. Bexrud, Ricardo Orprecio, Huzaifa Rangwala
  • Patent number: 9206194
    Abstract: The invention includes halichondrin B analogs having pharmaceutical activity; in some cases, crystalline forms thereof, and in some cases, halichondrin B analogs having a further utility as synthetic intermediate.
    Type: Grant
    Filed: October 21, 2013
    Date of Patent: December 8, 2015
    Assignee: Eisai R&D Management Co., Ltd.
    Inventor: Yongbo Hu
  • Patent number: 9035077
    Abstract: The present invention provides a method for manufacturing artemisinin and its congeners from cyclohexenone as a starting material.
    Type: Grant
    Filed: May 10, 2012
    Date of Patent: May 19, 2015
    Assignee: Indiana University Research & Technology Corporation
    Inventors: Silas Cook, Chun-Yin Zhu
  • Patent number: 9029573
    Abstract: The invention includes halichondrin B analogs having pharmaceutical activity; in some cases, crystalline forms thereof, and in some cases, halichondrin B analogs having a further utility as synthetic intermediate.
    Type: Grant
    Filed: October 21, 2013
    Date of Patent: May 12, 2015
    Assignee: Eisai R&D Management Co., Ltd.
    Inventor: Yongbo Hu
  • Publication number: 20150090935
    Abstract: The invention relates to bimesogenic compounds of formula I wherein R11, R12, MG11, MG12, X11, X12 and Sp1 have the meaning given in claim 1, to the use of bimesogenic compounds of formula I in liquid crystal media and particular to flexoelectric liquid crystal devices comprising a liquid crystal medium according to the present invention. Furthermore the invention relates to bimesogenic compounds of formula I inducing a second nematic phase in nematic mixtures that do not show this additional phase without compounds of formula I.
    Type: Application
    Filed: May 7, 2013
    Publication date: April 2, 2015
    Applicant: Merck Patent GmbH
    Inventors: Kevin Adlem, Owain Llyr Parri, Rachel Tuffin, Benjamin Snow, Mariam Namutebi
  • Publication number: 20150065733
    Abstract: Disclosed is a compound of formula 1, or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, R6, R7, R7?, R8, R9, R10, R11, R12 and R13 are as disclosed herein. Also, disclosed is a process for the preparation of the compound of formula 1, or a pharmaceutically acceptable salt thereof, and intermediates used therein. The compound of formula 1 can be used in the preparation of halichondrin analogs, such as Eribulin; and a process for its preparation from the compound of formula 1 is also disclosed.
    Type: Application
    Filed: March 28, 2013
    Publication date: March 5, 2015
    Inventors: Fabio E.S. Souza, Alena Rudolph, Ming Pan, Boris Gorin, Teng Ko Ngooi, Jason A. Bexrud, Ricardo Orprecio, Huzaifa Rangwala
  • Patent number: 8969594
    Abstract: Fullerene?CTV complexes, comprising fullerene?CTV hemicarceplexes, formed by various cyclotriveratrylene (CTV)-based molecular cages and various fullerene guests are disclosed. A method of direct isolating at least a fullerene from fullerene mixtures by using the above fullerene CTV hemicarceplexes but without using crystallization or HPLC is also disclosed.
    Type: Grant
    Filed: March 5, 2014
    Date of Patent: March 3, 2015
    Assignee: National Taiwan University
    Inventors: Sheng-Hsien Chiu, Ming-Jhe Li
  • Publication number: 20150044117
    Abstract: Cavitand compositions that comprise void spaces are disclosed. The void spaces may be empty, which means that voids are free of guest molecules or atoms, or the void spaces may comprise guest molecules or atoms that are normally in their gas phase at standard temperature and pressure. These cavitands may be useful for industrial applications, such as the separation or storage of gasses. Novel cavitand compounds are also disclosed.
    Type: Application
    Filed: March 22, 2013
    Publication date: February 12, 2015
    Applicant: GEORGETOWN UNIVERSITY
    Inventors: Kevin Travis Holman, Christopher Kane
  • Publication number: 20150034869
    Abstract: A novel material of a binaphthyl compound represented by General Formula (G1) is provided. Ar11 and Ar12 independently represent a substituted or unsubstituted arylene group having 6 to 12 carbon atoms, a substituted or unsubstituted cycloalkylene group having 3 to 12 carbon atoms, or a substituted or unsubstituted cycloalkenylene group having 3 to 12 carbon atoms, m represents 1 or 2, and n represents any one of 0 to 2. R12 represents a substituted or unsubstituted alkylene group having 1 to 12 carbon atoms, or a single bond. R13 represents hydrogen, a substituted or unsubstituted alkyl group having 1 to 12 carbon atoms, or a substituted or unsubstituted alkoxy group having 1 to 12 carbon atoms. One of R10 and R11 represents a substituent represented by General Formula (G2), and the other represents hydrogen.
    Type: Application
    Filed: July 23, 2014
    Publication date: February 5, 2015
    Inventors: Momoko KATO, Yasuhiro NIIKURA, Tetsuji ISHITANI
  • Patent number: 8921412
    Abstract: Disclosed is a novel C-aryl ansa compound having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney, and a pharmaceutical composition comprising the same as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes. Also provided are a method for preparing the compound, and a method for preventing or treating metabolic disorders, particularly diabetes, by using the compound.
    Type: Grant
    Filed: June 14, 2012
    Date of Patent: December 30, 2014
    Assignee: Green Cross Corporation
    Inventors: Min Ju Kim, Suk Ho Lee, Soongyu Choi
  • Publication number: 20140364630
    Abstract: The present invention is directed to a method for producing artemisinin having the formula from dihydroartemisinic acid in a continuous flow reactor using singlet oxygen as well as to the continuous flow reactor for producing artemisinin.
    Type: Application
    Filed: August 29, 2012
    Publication date: December 11, 2014
    Applicant: MAX-PLANCK-GESELLSCHAFT ZUR FÖRDERUNG DER WISSENSC
    Inventors: Peter H. Seeberger, Daniel Kopetzki, Francois Levesque
  • Patent number: 8884032
    Abstract: Monomeric and dimeric trioxane fluoroaryl amides, 5-carbon-linked, C-10 non-acetal trioxane dimer esters; trioxane silylamides; and trioxane dimer orthoesters and methods of their use for treating subjects infected with malaria or other parasitic infectious diseases including, but not limited to, toxoplasmic infection; subjects afflicted with psychiatric conditions associated with toxoplasmic infection; and subjects afflicted with cancer.
    Type: Grant
    Filed: May 19, 2010
    Date of Patent: November 11, 2014
    Assignee: The Johns Hopkins University
    Inventors: Gary H. Posner, Lauren E. Woodard, David R. Levine, Deuk Kyu Moon, Bryan T. Mott
  • Publication number: 20140323744
    Abstract: The specification relates to compounds and process for the preparation of a compound of formula 7, where LG is a leaving group and hal is a halide and is Cl, Br or I. The compound of formula 7 can be useful in the preparation of natural products, such as halichondrin and its derivatives.
    Type: Application
    Filed: November 29, 2012
    Publication date: October 30, 2014
    Inventors: Fabio E.S. Souza, Huzaifa Rangwala, Boris Gorin, Ming Pan
  • Patent number: 8841466
    Abstract: This invention relates to the synthesis of certain novel Baylis-Hillman adducts of artremisinin derived aldehyde 2-[10??-deoxoartemisininyl]-ethanal. The capabilities of introduction of three functional groups into a molecule in one step using Baylis-Hillman reaction encouraged us to synthesize some highly functionalized derivatives of artemisinin. These highly functionalized artemisinin derivatives embodied in this document are found to be active against various cancer cell-lines.
    Type: Grant
    Filed: January 20, 2011
    Date of Patent: September 23, 2014
    Assignee: Council of Scientific & Industrial Research
    Inventors: Gakul Baishya, Nabin Chandra Barua, Abhishek Goswami, Partha Pratim Saikia, Paruchuri Gangadhar Rao, Ajit Kumar Saxena, Nitasha Suri, Madhunika Sharma
  • Publication number: 20140232977
    Abstract: The invention relates to bimesogenic compounds of formula I R1-MG1-Sp-MG2-R2??I wherein R1, R2, MG1, MG2 and Sp have the meaning given in claim 1, to the use of bimesogenic compounds of formula I in liquid crystal media and particular to flexoelectric liquid crystal devices comprising a liquid crystal medium according to the present invention. Furthermore the invention relates to bimesogenic compounds of formula I inducing a second nematic phase in nematic mixtures that do not show this additional phase without compounds of formula I.
    Type: Application
    Filed: June 12, 2012
    Publication date: August 21, 2014
    Applicant: MERCK PATENT GMBH
    Inventors: Kevin Adlem, David Wilkes, Patricia Eileen Saxton, Benjamin Snow, Rachel Tuffin, Owain Llyr Parri, Geoffrey Luckhurst
  • Patent number: 8801811
    Abstract: A stabilized nano-Fe6-iron-crown ether complex is formed by preparing a solution of an iron salt and an oligomer crown compound in dialkylamine or diethylamine. Sodium tetrahydroboron (NaBH4) and dialkylamine or ethylendiamine are added at a temperature of 0-10° C. The mixture is heated to room temperature and boiled, thereby converting the formed iron (II)-borhydride complex (Fe(BH4)2) to a crown ether-iron-hydride complex [CWFe06].(2H)6. At higher temperature this last complex is converted to the Fe06-crown nanocomposite complex. The prepared nanoparticle Fe6° complex may be stabilized by inclusion into a cavity of a macrocyclic compound, and may be (1) added to diesel fuel to reduce NOx emissions upon combustion of that fuel; (2) added to lubricating oils as an anti-corrosion additive; and (3) used as an additive to secondary recovery processes within liquid hydrocarbon formations to increase the sweep efficiency and recovery factor of water-flooding operations.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: August 12, 2014
    Assignee: Asiacom Group Investments, Inc.
    Inventors: Alimamed L. Shabanov, Elmira M. Ramazanova, Uliviyya A. Gasanova
  • Publication number: 20140213642
    Abstract: Disclosed is a novel C-aryl ansa compound having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney, and a pharmaceutical composition comprising the same as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes. Also provided are a method for preparing the compound, and a method for preventing or treating metabolic disorders, particularly diabetes, by using the compound.
    Type: Application
    Filed: June 14, 2012
    Publication date: July 31, 2014
    Applicant: GREEN CROSS CORPORATION
    Inventors: Min Ju Kim, Suk Ho Lee, Soongyu Choi
  • Publication number: 20140187800
    Abstract: Fullerene?CTV complexes, comprising fullerene?CTV hemicarceplexes, formed by various cyclotriveratrylene (CTV)-based molecular cages and various fullerene guests are disclosed. A method of direct isolating at least a fullerene from fullerene mixtures by using the above fullerene CTV hemicarceplexes but without using crystallization or HPLC is also disclosed.
    Type: Application
    Filed: March 5, 2014
    Publication date: July 3, 2014
    Applicant: NATIONAL TAIWAN UNIVERSITY
    Inventors: Sheng-Hsien Chiu, Ming-Jhe Li
  • Publication number: 20140163244
    Abstract: The invention includes halichondrin B analogs having pharmaceutical activity; in some cases, crystalline forms thereof, and in some cases, halichondrin B analogs having a further utility as synthetic intermediate.
    Type: Application
    Filed: October 21, 2013
    Publication date: June 12, 2014
    Applicant: Eisai R&D Management Co., Ltd.
    Inventor: Yongbo HU
  • Publication number: 20140135507
    Abstract: The present invention provides a method for manufacturing artemisinin and its congeners from cyclohexenone as a starting material.
    Type: Application
    Filed: May 10, 2012
    Publication date: May 15, 2014
    Applicant: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION
    Inventors: Silas Cook, Chun-Yin Zhu
  • Patent number: 8692003
    Abstract: The present invention relates to compounds with an increased in vivo biological activity, and especially an increased pharmaceutical activity, such as an anti-nematodal or antifungal activity, an immunosuppresive activity, a metabolism influencing activity and/or an anti-cancer activity. Specifically, the present invention relates to compound comprising an artemisinin derivative according to the general formula (I) covalently linked at the 1 or the 2 position to a compound with a biological activity thereby increasing the biological activity of said compound or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: September 10, 2008
    Date of Patent: April 8, 2014
    Assignee: Dafra Pharma N.V.
    Inventors: Frans Herwig Jansen, Shahid Ahmed Soomro
  • Patent number: 8691111
    Abstract: A liquid crystal composition comprising a chiral dopant compound represented by the following formula: wherein: R1, R2 are independently aryl, alkyl, alkenyl, cycloalkyl, alkoxyaryl, alkaryl or heterocyclic all either substituted or unsubstituted, or combine to form a carbocyclic or heterocyclic ring; R3 and R4 are independently hydrogen, halogen, cyano, alkoxy, NHCOR7, NHSO2R7, COOR7, OCOR7, aryl, alkyl, alkenyl, cycloalkyl, alkoxyaryl, alkaryl or heterocyclic all either substituted or unsubstituted, or combine with either R1 or R2 to form a carbocylic or heterocyclic ring; R5 and R6 are independently hydrogen, CH2, CH, alkyl or aryl either substituted or unsubstituted, COOR7, or combine with L to form a carbocyclic or heterocyclic ring; R7 is aryl, alkyl, alkenyl, cycloalkyl, alkoxyaryl or heterocyclic all either substituted or unsubstituted; L is the non-metallic elements required to form a carbocyclic or heterocyclic ring, or a single bond or a double bond; m is 1-3; n is 0-12.
    Type: Grant
    Filed: April 26, 2012
    Date of Patent: April 8, 2014
    Assignee: Kent Displays Inc.
    Inventors: Donald R. Diehl, Thomas Welter, Erica N. Montbach, J. William Doane, Nithya Venkataraman
  • Patent number: 8673890
    Abstract: The present invention is directed to novel 2,3-dihydro-1H-isoindol-1-imine derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the thrombin PAR-1 receptor antagonists.
    Type: Grant
    Filed: October 28, 2010
    Date of Patent: March 18, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Han-Cheng Zhang, Bruce Maryanoff, Kimberly White, Stephen C. Yabut, Hong Ye, Cailin Chen
  • Patent number: 8614339
    Abstract: The present invention relates to dimeric derivatives of 10-trifluoromethylated artemisinin of formula (I) below: Formula (I) and the pharmaceutically acceptable salts thereof, and also to the preparation method thereof and to the uses thereof, especially in the treatment of cancer.
    Type: Grant
    Filed: July 29, 2009
    Date of Patent: December 24, 2013
    Assignees: Pierre Fabre Medicament, Centre National de la Recherche Scientifique (CNRS), Universite Paris-Sud 11
    Inventors: Jean-Pierre Begue, Danièle Bonnet-Delpon, Benoît Crousse, Anaïs Fournial, Céline Mordant, Jacques Fahy
  • Patent number: 8598373
    Abstract: The invention includes halichondrin B analogs having pharmaceutical activity; in some cases, crystalline forms thereof, and in some cases, halichondrin B analogs having a further utility as synthetic intermediates.
    Type: Grant
    Filed: April 3, 2009
    Date of Patent: December 3, 2013
    Assignee: Eisai R&D Management Co., Ltd.
    Inventor: Yongbo Hu
  • Publication number: 20130317095
    Abstract: The invention demonstrates the application of an artemisinin derivative and its pharmaceutical salt. The artemisinin derivatives diarteether amine and its pharmaceutical salt inhibit the proliferation of leukemic cells, block the cell cycle of leukemic cells and induce the apoptosis of leukemic cells. Artemisinin derivatives of the present invention and its pharmaceutical salt can be used for the preparation of anti-leukemia medicines, especially for treatment of acute leukemia and, what's more, for the treatment of acute myeloid leukemia.
    Type: Application
    Filed: January 16, 2012
    Publication date: November 28, 2013
    Applicant: Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Jianqing Mi, Ying Li, Yu Peng, Yu Zhang, Ruimin Nie, Jingjing Liu, Jin Wang, Yueying Wang, Xun Cai, Yang Li, Saijuan Chen, Zhenyi Wang
  • Patent number: 8592611
    Abstract: The disclosure provides novel trioxane sulfur dimers having Formula I: methods for their preparation, pharmaceutical compositions containing these compounds, and methods for treating cancer, proliferative disorders, and/or malaria using these compounds and/or compositions.
    Type: Grant
    Filed: July 17, 2009
    Date of Patent: November 26, 2013
    Assignee: The Johns Hopkins University
    Inventors: Gary H. Posner, Andrew S. Rosenthal
  • Publication number: 20130296412
    Abstract: The present invention relates to novel artemisinin-like derivates, and especially dihydroartemisinin derivates and pharmaceutical compositions comprising the present compounds. The present invention further relates to the use of the present compounds for the treatment of cancer, especially by oral administration. Especially, the present invention relates to dihydroartemisinin compounds (DHA) substituted by, through an ester linkage by a linear or branched C1 to C6 alkyl optionally substituted by one or more halogens. Especially preferred substituents are acetate, propionate, isopropionate, butyrate and isobutyrate.
    Type: Application
    Filed: August 3, 2011
    Publication date: November 7, 2013
    Applicant: DAFRA PHARMA N.V.
    Inventor: Frans Herwig Jansen
  • Patent number: 8420837
    Abstract: A stabilized nano-Fe6-iron-crown ether complex is formed by preparing a solution of an iron salt and an olygomer crown compound in dialkylamine or diethylamine. Sodium tetrahydroboron (NaBH4) and dialkylamine or ethylendiamine are added at a temperature of 0-10° C. The mixture is heated to room temperature and boiled, thereby converting the formed iron (II)-borhydride complex (Fe(BH4)2) to a crown ether—iron-hydride complex [CWFe06]·(2H)6. At higher temperature this last complex is converted to the Fe06-crown nanocomposite complex.
    Type: Grant
    Filed: August 5, 2009
    Date of Patent: April 16, 2013
    Assignee: Asiacom Group Investments, Inc.
    Inventors: Alimamed L. Shabanov, Elmira M. Ramazanova, Ulviyya A. Gasanova
  • Patent number: 8399689
    Abstract: Embodiments of antimicrobial chrysophaentin compounds, pharmaceutical compositions including the chrysophaentin compounds, and methods for using the chrysophaentin compounds are disclosed. Some embodiments of the disclosed compounds are isolated from Chrysophaeum taylori. Certain embodiments of the chrysophaentin compounds inhibit FtsZ protein, thereby inhibiting the growth of clinically relevant bacteria, including drug-resistant strains.
    Type: Grant
    Filed: February 25, 2011
    Date of Patent: March 19, 2013
    Assignee: The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: Carole A. Bewley, Alberto Plaza, Jessica Keffer
  • Publication number: 20130030044
    Abstract: This invention relates to the synthesis of certain novel Baylis-Hillman adducts of artremisinin derived aldehyde 2[10??-deoxoartemisininyl]-ethanal. The capabilities of introduction of three functional groups into a molecule in one step using Baylis-Hillman reaction encouraged us to synthesize some highly functionalized derivatives of artemisinin.
    Type: Application
    Filed: January 20, 2011
    Publication date: January 31, 2013
    Applicant: Council of Scientific & Industrial Research
    Inventors: Gakul Baishya, Nabin Chandra Barua, Abhishek Goswami, Partha Pratim Saikia, Paruchuri Gangadhar Rao, Ajit Kumar Saxena, Nitasha Suri, Madhunika Sharma
  • Publication number: 20130030027
    Abstract: The present invention is directed to hemi phorboxazole A: and its stereoisomers, as well as derivatives of hemi phorboxazole A of formula I: wherein ring A is aryl or a 5- or 6-membered heteroaryl optionally substituted with one or more of halogen, —OH, or —C1-6alkyl; and R is —CN, a 5- or 6-membered heteroaryl, or halogen; and the pharmaceutically acceptable salt forms thereof, in addition to methods of using these compounds.
    Type: Application
    Filed: July 23, 2010
    Publication date: January 31, 2013
    Applicants: The Regents of the University of California, The Trustes of The University of Pennsylvania
    Inventors: Amos B. Smith, III, Zhuqing Liu, Anne-Marie L. Hogan, Doralyn S. Dalisay, Tadeusz F. Molinski
  • Publication number: 20120316227
    Abstract: Embodiments of antimicrobial chrysophaentin compounds, pharmaceutical compositions including the chrysophaentin compounds, and methods for using the chrysophaentin compounds are disclosed. Some embodiments of the disclosed compounds are isolated from Chrysophaeum taylori. Certain embodiments of the chrysophaentin compounds inhibit FtsZ protein, thereby inhibiting the growth of clinically relevant bacteria, including drug-resistant strains.
    Type: Application
    Filed: February 25, 2011
    Publication date: December 13, 2012
    Inventors: Carole A. Bewley, Alberto Plaza, Jessica Keffer
  • Publication number: 20120273725
    Abstract: A liquid crystal composition comprising a chiral dopant compound represented by the following formula: wherein: R1, R2 are independently aryl, alkyl, alkenyl, cycloalkyl, alkoxyaryl, alkaryl or heterocyclic all either substituted or unsubstituted, or combine to form a carbocyclic or heterocyclic ring; R3 and R4 are independently hydrogen, halogen, cyano, alkoxy, NHCOR7, NHSO2R7, COOR7, OCOR7, aryl, alkyl, alkenyl, cycloalkyl, alkoxyaryl, alkaryl or heterocyclic all either substituted or unsubstituted, or combine with either R1 or R2 to form a carbocylic or heterocyclic ring; R5 and R6 are independently hydrogen, CH2, CH, alkyl or aryl either substituted or unsubstituted, COOR7, or combine with L to form a carbocyclic or heterocyclic ring; R7 is aryl, alkyl, alkenyl, cycloalkyl, alkoxyaryl or heterocyclic all either substituted or unsubstituted; L is the non-metallic elements required to form a carbocyclic or heterocyclic ring, or a single bond or a double bond; m is 1-3; n is 0-12.
    Type: Application
    Filed: April 26, 2012
    Publication date: November 1, 2012
    Applicants: Kent State University, Kent Displays Incorporated
    Inventors: Donald R. Diehl, Thomas Welter, Erica N. Montbach, J. William Doane, Nithya Venkataraman
  • Patent number: 8236850
    Abstract: The present invention relates to dimeric derivatives of 10-trifluoromethylated artemisinin of formula (I): or a pharmaceutically acceptable salt thereof with B1 and B2 selected from C?O, CHOH and CH2, as well as to their use in treating cancer and to their preparation method.
    Type: Grant
    Filed: December 22, 2008
    Date of Patent: August 7, 2012
    Assignees: Pierre Fabre Medicament, Centre National de la Recherche Scientifique, Universite Paris-Sud 11
    Inventors: Jean-Pierre Begue, Danielle Bonnet-Delpon, Benoît Crousse, Fabienne Grellepois, Constance Chollet, Jacques Fahy, Céline Mordant
  • Patent number: RE46965
    Abstract: The present invention provides macrocyclic compounds, synthesis of the same and intermediates thereto. Such compounds, and compositions thereof, are useful for treating or preventing proliferative disorders Formula (F-4).
    Type: Grant
    Filed: June 24, 2013
    Date of Patent: July 24, 2018
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Brian Austad, Charles E. Chase, Francis G. Fang, Trevor Calkins, Bryan M. Lewis