Polycyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 549/348)
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Patent number: 11559556Abstract: 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: GrantFiled: March 13, 2020Date of Patent: January 24, 2023Assignee: Northeastern UniversityInventors: David Medina Cruz, William Tien-Street, Bohan Zhang, Xinjing Huang, Ada Vernet Crua, Thomas J. Webster
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Patent number: 11365202Abstract: 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: GrantFiled: April 16, 2019Date of Patent: June 21, 2022Assignees: 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
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Patent number: 11077161Abstract: 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: GrantFiled: March 16, 2018Date of Patent: August 3, 2021Assignee: Orthopedic Solutions LLCInventors: Michael B. Gross, Javad Parvizi
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Patent number: 10676481Abstract: The invention relates to methods and intermediates useful in the synthesis of eribulin.Type: GrantFiled: February 10, 2017Date of Patent: June 9, 2020Assignee: EISAI R&D MANAGEMENT CO., LTD.Inventors: Phil S. Baran, Charles E. Chase, Francis G. Fang
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Patent number: 10450324Abstract: 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: GrantFiled: July 10, 2018Date of Patent: October 22, 2019Assignee: EISAI R&D MANAGEMENT CO., LTD.Inventors: Yongbo Hu, Huiming Zhang, Hiroyuki Chiba, Yuki Komatsu, Bryan M. Lewis
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Patent number: 10308661Abstract: 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: GrantFiled: May 9, 2016Date of Patent: June 4, 2019Assignee: EISAI R&D MANAGEMENT CO., LTD.Inventors: Francis G. Fang, Dae-Shik Kim, Hyeong-Wook Choi, Charles E. Chase
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Patent number: 9783549Abstract: 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: GrantFiled: November 4, 2014Date of Patent: October 10, 2017Assignee: EISAI R&D MANAGEMENT CO., LTD.Inventors: Francis G. Fang, Dae-Shik Kim, Hyeong-Wook Choi, Charles E. Chase, Jaemoon Lee
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Patent number: 9695188Abstract: 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: GrantFiled: March 3, 2016Date of Patent: July 4, 2017Assignee: EISAI R&D MANAGEMENT CO., LTD.Inventors: Yongbo Hu, Huiming Zhang, Hiroyuki Chiba, Yuki Komatsu, Bryan M. Lewis
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Patent number: 9611273Abstract: 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: GrantFiled: February 28, 2013Date of Patent: April 4, 2017Assignee: THE JOHNS HOPKINS UNIVERSITYInventors: Gary H. Posner, Alexander M. Jacobine, Rachel D. Slack, Jennifer R. Mazzone
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Patent number: 9493480Abstract: 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: GrantFiled: April 16, 2012Date of Patent: November 15, 2016Assignee: THE JOHNS HOPKINS UNIVERSITYInventors: Gary H. Posner, Rachel D. Slack
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Patent number: 9487538Abstract: 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: GrantFiled: January 22, 2014Date of Patent: November 8, 2016Assignee: THE JOHNS HOPKINS UNIVERSITYInventors: Gary H. Posner, Bryan T. Mott
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Patent number: 9409142Abstract: 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: GrantFiled: July 28, 2015Date of Patent: August 9, 2016Assignee: Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V.Inventors: Peter H. Seeberger, Daniel Kopetzki, Francois Lévesque
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Patent number: 9303039Abstract: 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: GrantFiled: December 5, 2014Date of Patent: April 5, 2016Assignee: Eisai R&D Management Co., Ltd.Inventors: Huiming Zhang, Bryan M. Lewis
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Patent number: 9278979Abstract: 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: GrantFiled: March 28, 2013Date of Patent: March 8, 2016Assignee: ALPHORA RESEARCH INC.Inventors: Fabio E. S. Souza, Alena Rudolph, Ming Pan, Boris Gorin, Teng Ko Ngooi, Jason A. Bexrud, Ricardo Orprecio, Huzaifa Rangwala
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Patent number: 9206194Abstract: 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: GrantFiled: October 21, 2013Date of Patent: December 8, 2015Assignee: Eisai R&D Management Co., Ltd.Inventor: Yongbo Hu
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Patent number: 9035077Abstract: The present invention provides a method for manufacturing artemisinin and its congeners from cyclohexenone as a starting material.Type: GrantFiled: May 10, 2012Date of Patent: May 19, 2015Assignee: Indiana University Research & Technology CorporationInventors: Silas Cook, Chun-Yin Zhu
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Patent number: 9029573Abstract: 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: GrantFiled: October 21, 2013Date of Patent: May 12, 2015Assignee: Eisai R&D Management Co., Ltd.Inventor: Yongbo Hu
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Publication number: 20150090935Abstract: 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: ApplicationFiled: May 7, 2013Publication date: April 2, 2015Applicant: Merck Patent GmbHInventors: Kevin Adlem, Owain Llyr Parri, Rachel Tuffin, Benjamin Snow, Mariam Namutebi
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Publication number: 20150065733Abstract: 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: ApplicationFiled: March 28, 2013Publication date: March 5, 2015Inventors: Fabio E.S. Souza, Alena Rudolph, Ming Pan, Boris Gorin, Teng Ko Ngooi, Jason A. Bexrud, Ricardo Orprecio, Huzaifa Rangwala
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Patent number: 8969594Abstract: 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: GrantFiled: March 5, 2014Date of Patent: March 3, 2015Assignee: National Taiwan UniversityInventors: Sheng-Hsien Chiu, Ming-Jhe Li
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Publication number: 20150044117Abstract: 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: ApplicationFiled: March 22, 2013Publication date: February 12, 2015Applicant: GEORGETOWN UNIVERSITYInventors: Kevin Travis Holman, Christopher Kane
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Publication number: 20150034869Abstract: 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: ApplicationFiled: July 23, 2014Publication date: February 5, 2015Inventors: Momoko KATO, Yasuhiro NIIKURA, Tetsuji ISHITANI
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Patent number: 8921412Abstract: 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: GrantFiled: June 14, 2012Date of Patent: December 30, 2014Assignee: Green Cross CorporationInventors: Min Ju Kim, Suk Ho Lee, Soongyu Choi
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Publication number: 20140364630Abstract: 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: ApplicationFiled: August 29, 2012Publication date: December 11, 2014Applicant: MAX-PLANCK-GESELLSCHAFT ZUR FÖRDERUNG DER WISSENSCInventors: Peter H. Seeberger, Daniel Kopetzki, Francois Levesque
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Patent number: 8884032Abstract: 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: GrantFiled: May 19, 2010Date of Patent: November 11, 2014Assignee: The Johns Hopkins UniversityInventors: Gary H. Posner, Lauren E. Woodard, David R. Levine, Deuk Kyu Moon, Bryan T. Mott
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Publication number: 20140323744Abstract: 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: ApplicationFiled: November 29, 2012Publication date: October 30, 2014Inventors: Fabio E.S. Souza, Huzaifa Rangwala, Boris Gorin, Ming Pan
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Patent number: 8841466Abstract: 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: GrantFiled: January 20, 2011Date of Patent: September 23, 2014Assignee: Council of Scientific & Industrial ResearchInventors: Gakul Baishya, Nabin Chandra Barua, Abhishek Goswami, Partha Pratim Saikia, Paruchuri Gangadhar Rao, Ajit Kumar Saxena, Nitasha Suri, Madhunika Sharma
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Publication number: 20140232977Abstract: 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: ApplicationFiled: June 12, 2012Publication date: August 21, 2014Applicant: MERCK PATENT GMBHInventors: Kevin Adlem, David Wilkes, Patricia Eileen Saxton, Benjamin Snow, Rachel Tuffin, Owain Llyr Parri, Geoffrey Luckhurst
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Patent number: 8801811Abstract: 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: GrantFiled: March 13, 2013Date of Patent: August 12, 2014Assignee: Asiacom Group Investments, Inc.Inventors: Alimamed L. Shabanov, Elmira M. Ramazanova, Uliviyya A. Gasanova
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Publication number: 20140213642Abstract: 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: ApplicationFiled: June 14, 2012Publication date: July 31, 2014Applicant: GREEN CROSS CORPORATIONInventors: Min Ju Kim, Suk Ho Lee, Soongyu Choi
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Publication number: 20140187800Abstract: 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: ApplicationFiled: March 5, 2014Publication date: July 3, 2014Applicant: NATIONAL TAIWAN UNIVERSITYInventors: Sheng-Hsien Chiu, Ming-Jhe Li
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Publication number: 20140163244Abstract: 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: ApplicationFiled: October 21, 2013Publication date: June 12, 2014Applicant: Eisai R&D Management Co., Ltd.Inventor: Yongbo HU
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Publication number: 20140135507Abstract: The present invention provides a method for manufacturing artemisinin and its congeners from cyclohexenone as a starting material.Type: ApplicationFiled: May 10, 2012Publication date: May 15, 2014Applicant: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATIONInventors: Silas Cook, Chun-Yin Zhu
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Patent number: 8692003Abstract: 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: GrantFiled: September 10, 2008Date of Patent: April 8, 2014Assignee: Dafra Pharma N.V.Inventors: Frans Herwig Jansen, Shahid Ahmed Soomro
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Patent number: 8691111Abstract: 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: GrantFiled: April 26, 2012Date of Patent: April 8, 2014Assignee: Kent Displays Inc.Inventors: Donald R. Diehl, Thomas Welter, Erica N. Montbach, J. William Doane, Nithya Venkataraman
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Patent number: 8673890Abstract: 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: GrantFiled: October 28, 2010Date of Patent: March 18, 2014Assignee: Janssen Pharmaceutica NVInventors: Han-Cheng Zhang, Bruce Maryanoff, Kimberly White, Stephen C. Yabut, Hong Ye, Cailin Chen
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Patent number: 8614339Abstract: 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: GrantFiled: July 29, 2009Date of Patent: December 24, 2013Assignees: Pierre Fabre Medicament, Centre National de la Recherche Scientifique (CNRS), Universite Paris-Sud 11Inventors: Jean-Pierre Begue, Danièle Bonnet-Delpon, Benoît Crousse, Anaïs Fournial, Céline Mordant, Jacques Fahy
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Patent number: 8598373Abstract: 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: GrantFiled: April 3, 2009Date of Patent: December 3, 2013Assignee: Eisai R&D Management Co., Ltd.Inventor: Yongbo Hu
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Publication number: 20130317095Abstract: 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: ApplicationFiled: January 16, 2012Publication date: November 28, 2013Applicant: Shanghai Institute of Materia Medica, Chinese Academy of SciencesInventors: Jianqing Mi, Ying Li, Yu Peng, Yu Zhang, Ruimin Nie, Jingjing Liu, Jin Wang, Yueying Wang, Xun Cai, Yang Li, Saijuan Chen, Zhenyi Wang
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Patent number: 8592611Abstract: 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: GrantFiled: July 17, 2009Date of Patent: November 26, 2013Assignee: The Johns Hopkins UniversityInventors: Gary H. Posner, Andrew S. Rosenthal
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Publication number: 20130296412Abstract: 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: ApplicationFiled: August 3, 2011Publication date: November 7, 2013Applicant: DAFRA PHARMA N.V.Inventor: Frans Herwig Jansen
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Patent number: 8420837Abstract: 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: GrantFiled: August 5, 2009Date of Patent: April 16, 2013Assignee: Asiacom Group Investments, Inc.Inventors: Alimamed L. Shabanov, Elmira M. Ramazanova, Ulviyya A. Gasanova
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Patent number: 8399689Abstract: 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: GrantFiled: February 25, 2011Date of Patent: March 19, 2013Assignee: The United States of America, as represented by the Secretary, Department of Health and Human ServicesInventors: Carole A. Bewley, Alberto Plaza, Jessica Keffer
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Publication number: 20130030044Abstract: 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: ApplicationFiled: January 20, 2011Publication date: January 31, 2013Applicant: Council of Scientific & Industrial ResearchInventors: Gakul Baishya, Nabin Chandra Barua, Abhishek Goswami, Partha Pratim Saikia, Paruchuri Gangadhar Rao, Ajit Kumar Saxena, Nitasha Suri, Madhunika Sharma
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Publication number: 20130030027Abstract: 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: ApplicationFiled: July 23, 2010Publication date: January 31, 2013Applicants: The Regents of the University of California, The Trustes of The University of PennsylvaniaInventors: Amos B. Smith, III, Zhuqing Liu, Anne-Marie L. Hogan, Doralyn S. Dalisay, Tadeusz F. Molinski
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Publication number: 20120316227Abstract: 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: ApplicationFiled: February 25, 2011Publication date: December 13, 2012Inventors: Carole A. Bewley, Alberto Plaza, Jessica Keffer
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Publication number: 20120273725Abstract: 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: ApplicationFiled: April 26, 2012Publication date: November 1, 2012Applicants: Kent State University, Kent Displays IncorporatedInventors: Donald R. Diehl, Thomas Welter, Erica N. Montbach, J. William Doane, Nithya Venkataraman
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Patent number: 8236850Abstract: 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: GrantFiled: December 22, 2008Date of Patent: August 7, 2012Assignees: Pierre Fabre Medicament, Centre National de la Recherche Scientifique, Universite Paris-Sud 11Inventors: Jean-Pierre Begue, Danielle Bonnet-Delpon, Benoît Crousse, Fabienne Grellepois, Constance Chollet, Jacques Fahy, Céline Mordant
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Patent number: 8232417Abstract: The present invention discloses certain derivatives of artemisinin and the active principles contained in Artemisia annua extracts with amino acids, peptides, and amino sugars and salts thereof (formula I).Type: GrantFiled: April 5, 2012Date of Patent: July 31, 2012Assignee: Bioderm ResearchInventor: Shyam K Gupta
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Patent number: RE46965Abstract: 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: GrantFiled: June 24, 2013Date of Patent: July 24, 2018Assignee: Eisai R&D Management Co., Ltd.Inventors: Brian Austad, Charles E. Chase, Francis G. Fang, Trevor Calkins, Bryan M. Lewis