Polycyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 549/348)
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Publication number: 20120189567Abstract: 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: ApplicationFiled: April 5, 2012Publication date: July 26, 2012Applicant: BIODERM RESEARCHInventor: SHYAM K GUPTA
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Publication number: 20120161089Abstract: A chromene compound having a skeleton represented by the following formula (1) and exhibiting double peak characteristic: wherein Z is a group represented by anyone of the following formulas: (R1 is an electron donor group having a Hammett constant ?p of less than ?0.20, with the proviso that when there are a plurality of R1's, R1's may be the same or different, and R2 is a group having a Hammett constant ?p of ?0.Type: ApplicationFiled: August 26, 2010Publication date: June 28, 2012Inventors: Toshiaki Takahashi, Junji Takenaka
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Patent number: 8207357Abstract: An antitumor agent which is not easily excreted from tumor cells and is suitable for a topical treatment. Specifically disclosed is a rotaxane compound with contains a compound represented by chemical formula 1 as the base structure. (In chemical formula 1, m?2, n?3, and X represents an anionic molecule or an anionic atom.Type: GrantFiled: October 21, 2009Date of Patent: June 26, 2012Assignees: Wan Station Co., Ltd., Tokyo Institute of Technology, Fukuoka University, Kinki UniversityInventors: Toshikazu Takata, Yasuhito Koyama, Kazuko Nakazono, Toshihide Hasegawa, Young-Gi Lee, Nobufumi Ono, Kazuto Nishio, Yoshihiko Fujita
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Publication number: 20120157658Abstract: This invention relates to methods, compositions, and apparatuses for producing macrocyclic compounds. First, one or more reactants are provided in a reaction medium, which are capable of forming the macrocyclic compound through a desired reaction pathway that includes at least cyclization, and which are further capable of forming undesired oligomers through a undesired reaction pathway that includes undesirable oligomerization. Oligomerization of such reactions in the reaction medium is modulated to reduce formation of undesired oligomers and/or to reduce separation of the undesired oligomers from the reaction medium, relative to a corresponding unmodulated oligomerization reaction, thereby maximizing yields of the macrocyclic compound. The macrocyclic compound so formed is then recovered from the reaction medium. Preferably, the macrocyclic compound spontaneously separates from the reaction medium via phase separation.Type: ApplicationFiled: November 8, 2011Publication date: June 21, 2012Inventors: Thomas E. Johnson, Billy T. Fowler
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Publication number: 20120157519Abstract: Tellurium-containing compounds identified for use in a method of treating, or prophylaxis against, a viral infection caused by an influenza virus, uses thereof and pharmaceutical kits and pharmaceutical corn positions comprising the same, are disclosed. The tellurium-containing compounds disclosed herein are suitable for co-administration with an antiviral agent.Type: ApplicationFiled: June 16, 2010Publication date: June 21, 2012Applicant: Biomas Ltd.Inventors: Benjamin Sredni, Michael Albeck
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Patent number: 8193376Abstract: 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 isomers and salts thereof (formula I).Type: GrantFiled: December 1, 2010Date of Patent: June 5, 2012Assignee: Bioderm ResearchInventor: Shyam K Gupta
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Publication number: 20120108545Abstract: 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: ApplicationFiled: May 19, 2010Publication date: May 3, 2012Applicant: 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: 20120095242Abstract: Methods of synthesizing intermediates useful for the synthesis of halichondrin B analogs are described.Type: ApplicationFiled: December 22, 2011Publication date: April 19, 2012Applicant: Eisai R&D Management Co., Ltd.Inventors: Charles Chase, Atsushi Endo, Francis G. Fang, Jing Li
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Patent number: 8148554Abstract: The invention provides methods and compositions for use in treating diseases associated with excessive cellular proliferation, such as cancer, and intermediates for the synthesis of such compositions.Type: GrantFiled: August 12, 2010Date of Patent: April 3, 2012Assignee: Eisai R&D Management Co., Ltd.Inventors: Boris M. Seletsky, Melvin J. Yu, Wanjun Zheng
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Publication number: 20120041153Abstract: The present invention is generally directed toward a regiofunctional carbon nanotube beam structures and a method the same. The regiofunctional carbon nanotube beam structures contain chemical moieties attached selectively to the ends and/or the sidewalls of the nanotube which differentiate the physico-chemical properties of the nanotube ends from the physico-chemical of the sidewalls to enable directed self-assembly. The method comprises the steps including opening carbon nanotube ends, protecting those ends from sidewall functionalization chemistry by chemically differentiating the open carbon nanotube ends from the nanotube sidewall, functionalizing the sidewalls, functionalizing the ends of the carbon nanotube and attaching crown to ends.Type: ApplicationFiled: August 11, 2010Publication date: February 16, 2012Inventor: Nolan Walker Nicholas
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Publication number: 20120029213Abstract: Intermediates and methods of their use in the synthesis of analogs of halichondrin B are provided.Type: ApplicationFiled: June 29, 2011Publication date: February 2, 2012Applicant: Eisai R&D Management Co., Ltd.Inventors: Brian Austad, Farid Benayoud, Trevor Calkins, Silvio Campagna, Charles E. Chase, William Christ, Francis G. Fang, Yongbo Hu, Bryan M. Lewis, Marc Pesant, Matthew Schnaderbeck, Gordon Wilkie, Xiaojie Zhu
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Publication number: 20120022150Abstract: A method of treating a benign pigmented mole or a dermatomycosis. The method comprises locally applying to a subject in need thereof artemisinine and/or one or more structurally related compounds. Also disclosed is a plaster which comprises a topical formulation comprising artemisinine and/or one or more structurally related compounds.Type: ApplicationFiled: September 1, 2011Publication date: January 26, 2012Applicant: EPIPHARM GMBHInventor: Rosemarie SIFT CARTER
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Publication number: 20120015922Abstract: Artesunate is a derivative of artemisinin isolated from a Chinese herb Artemisia annua L. It is used clinically for the treatment of malaria. We investigated potential anti-inflammatory actions of artemisinin derivatives. artemisinin derivatives significantly inhibited OVA-induced signs, symptoms and parameter of airway disorders Taken together, our results clearly demonstrate anti-inflammatory effects of artemisinin derivatives. Artemisinin derivatives can be used to complement or to replace oral steroids during asthma exacerbation treatment. Further artemisinin derivatives can be used as an anti-inflammatory agent for controlling airway disorders.Type: ApplicationFiled: March 24, 2010Publication date: January 19, 2012Applicant: NATIONAL UNIVERSITY OF SINGAPOREInventor: Wai Shiu Fred Wong
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Publication number: 20110237807Abstract: An antitumor agent which is not easily excreted from tumor cells and is suitable for a topical treatment. Specifically disclosed is a rotaxane compound with contains a compound represented by chemical formula 1 as the base structure.Type: ApplicationFiled: October 21, 2009Publication date: September 29, 2011Applicants: WAN STATION CO., LTD., TOKYO INSTITUTE OF TECHNOLOGY, FUKUOKA UNIVERSITY, KINKI UNIVERSITYInventors: Toshikazu Takata, Yasuhito Koyama, Kazuko Nakazono, Toshihide Hasegawa, Young-Gi Lee, Nobufumi Ono, Kazuto Nishio, Yoshihiko Fujita
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Patent number: 8013011Abstract: A method of treating a benign pigmented mole or a dermatomycosis. The method comprises locally applying to a subject in need thereof artemisinine and/or one or more structurally related compounds. Also disclosed is a plaster which comprises a topical formulation comprising artemisinine and/or one or more structurally related compounds.Type: GrantFiled: October 19, 2006Date of Patent: September 6, 2011Assignee: EPIPHARM GmbHInventor: Rosemarie Sift Carter
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Publication number: 20110172446Abstract: The invention provides methods and compositions for use in treating diseases associated with excessive cellular proliferation, such as cancer, and intermediates for the synthesis of such compositions.Type: ApplicationFiled: August 12, 2010Publication date: July 14, 2011Inventors: Bruce A. Littlefield, Boris M. Seletsky, Murray J. Towle, Melvin J. Yu, Wanjun Zheng
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Publication number: 20110082194Abstract: A composition is provided that, when utilized in combination with warfarin, greatly improves the anticoagulant effects of warfarin in mammalian subjects. The composition is a compound having a naphthohydroquinone ring system substantially similar to the ring system of the reduced form of vitamin K1 and has the general formula: where R1 and R4 are hydrogen or acyl, R2 is a saturated or unsaturated alkyl group with up to 6 carbons, and R3 is a saturated or unsaturated alkyl group with up to 20 carbons, or R2 and R3 are part of a cyclic or polycyclic ring system.Type: ApplicationFiled: September 30, 2010Publication date: April 7, 2011Inventors: David E. Lewis, Michael D. Caldwell
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Publication number: 20110077193Abstract: 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 isomers and salts thereof (formula I).Type: ApplicationFiled: December 1, 2010Publication date: March 31, 2011Applicant: BIODERM RESEARCHInventor: Shyam K. Gupta
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Patent number: 7910750Abstract: The invention provides a type of artemisinin derivatives having following structure I, its preparation method and use, as well as a pharmaceutical composition containing such artemisinin derivatives and its use. The arteminsinin derivatives of the present invention and their pharmaceutical composition containing the artemisinin derivatives. have immunosuppressive activities and can be used more safely. The composition which comprises the artemisinin derivatives can be formulated into long-term dosage forms such as tablet, pellet and the like, and have wider productive and use value.Type: GrantFiled: January 27, 2006Date of Patent: March 22, 2011Assignee: Shanghai Institute of Materia Medica, Chinese Academy of SciencesInventors: Ying Li, Jianping Zuo, Zhongshun Yang, Wenliang Zhou, Yi Sui, Junxia Wang, Yu Zhang, Yu Zhou, Jinming Wu
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Publication number: 20110054194Abstract: 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: ApplicationFiled: April 3, 2009Publication date: March 3, 2011Applicant: Eisai R&D Management Co., Ltd.Inventor: Yongbo Hu
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Publication number: 20110028382Abstract: The invention provides compounds for use in a method of treating oral pharyngeal dysphagia in an individual and related products. One embodiment of the invention comprises administering to an individual an effective amount of a vanilloid receptor 1 (VR-1) agonist or high-affinity partial agonist to promote a swallow reflex.Type: ApplicationFiled: October 7, 2008Publication date: February 3, 2011Inventor: Kevin Burke Miller
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Patent number: 7842720Abstract: This invention comprises compositions containing dihydroartemisinin- and dihydroartemisitene-dimers with activity as anticancer or anticancer metastasis agents and anti-protozal, including anti-malarial and anti-leishmanial properties. This invention also describes methods of preparation of these compositions and methods of use of such compositions for the treatment of cancer or prevention of cancer metastasis, and protozoal infections, including malaria, or leishmaniasis. The compounds of this invention represent a potential new class of anti-tumor or anti-metastasis agents, one that has shown promising activity against solid tumors.Type: GrantFiled: June 21, 2005Date of Patent: November 30, 2010Assignee: Elsohly Laboratories, IncorporatedInventors: Mahmoud A. Elsohly, Waseem Gul
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Publication number: 20100286393Abstract: 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: ApplicationFiled: September 10, 2008Publication date: November 11, 2010Applicant: DAFRA PHARMA N.V.Inventors: Frans Herwing Jansen, Shahid Ahmed Soomro
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Publication number: 20100216970Abstract: This invention relates to methods, compositions, and apparatuses for producing macrocyclic compounds. First, one or more reactants are provided in a reaction medium, which are capable of forming the macrocyclic compound through a desired reaction pathway that includes at least cyclization, and which are further capable of forming undesired oligomers through a undesired reaction pathway that includes undesirable oligomerization. Oligomerization of such reactions in the reaction medium is modulated to reduce formation of undesired oligomers and/or to reduce separation of the undesired oligomers from the reaction medium, relative to a corresponding unmodulated oligomerization reaction, thereby maximizing yields of the macrocyclic compound. The macrocyclic compound so formed is then recovered from the reaction medium. Preferably, the macrocyclic compound spontaneously separates from the reaction medium via phase separation.Type: ApplicationFiled: May 3, 2010Publication date: August 26, 2010Inventors: Thomas E. Johnson, Billy T. Fowler
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Publication number: 20100216869Abstract: The invention relates to Artemisinin derivatives of general formula (I) wherein A and B are as defined in the specification. Compounds (I) have proved able to inhibit cell proliferation, in particular of uveal melanoma cells, and can therefore be used, either alone or in association with other antitumoral drugs, for the preparation of medicaments intended for the treatment of malignant melanoma.Type: ApplicationFiled: September 25, 2008Publication date: August 26, 2010Inventors: Luigi Villanova, Felicia Cisale, Felicia Cisale, Azzurra Villanova, Luciano Villanova
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Patent number: 7771800Abstract: The invention relates to chiral compounds, methods of their preparation, and to their use in optical, electrooptical, electronic, semiconducting or luminescent components or devices, and in decorative, security, cosmetic or diagnostic applications.Type: GrantFiled: September 20, 2006Date of Patent: August 10, 2010Assignee: Merck Patent GmbHInventor: Louise Diane Farrand
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Patent number: 7771801Abstract: The invention relates to chiral compounds, methods of their preparation, and to their use in optical, electrooptical, electronic, semiconducting or luminescent components or devices, and in decorative, security, cosmetic or diagnostic applications.Type: GrantFiled: September 20, 2006Date of Patent: August 10, 2010Assignee: Merck Patent GmbHInventor: Louise Diane Farrand
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Publication number: 20100184846Abstract: A method for the manufacture of a sterile intravenous or intramuscular formulation of artesunic acid and the formulation are the subject of this invention. First the artesunic acid powder is sterilized with ethylene oxide and placed into a sterile container. The contained sterilized powder is then dissolved in sterile sodium phosphate buffered solution to produce an injectable intravenous or intramuscular formulation. The sodium phosphate dissolves and dilutes the artesunic acid powder without caking or frothing resulting in an improved drug product. The invention also relates to the formulation and a method of treating a patient with either uncomplicated or severe and complicated malaria.Type: ApplicationFiled: February 4, 2010Publication date: July 22, 2010Inventors: William Y. Ellis, Peter Lim, Manaj Maniar
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Publication number: 20100116749Abstract: A mixed extractant solvent that includes at least one dialkyloxycalix[4]arenebenzocrown-6 compound, 4?,4?,(5?)-di-(t-butyldicyclohexano)-18-crown-6, at least one modifier, and, optionally, a diluent. The dialkyloxycalix[4]arenebenzocrown-6 compound is 1,3-alternate-25,27-di(octyloxy)calix[4] arenebenzocrown-6, 1,3-alternate-25,27-di(decyloxy)calix[4]arene-benzocrown-6, 1,3-alternate-25,27-di(dodecyloxy)calix[4]arenebenzocrown-6, 1,3-alternate-25,27-di(2-ethylhexyl-1-oxy)calix[4]arenebenzocrown-6, 1,3-alternate-25,27-di(3,7-dimethyloctyl-1-oxy)calix[4] arenebenzocrown-6, 1,3-alternate-25,27-di(4-butyloctyl-1-oxy)calix[4]arenebenzocrown-6, or combinations thereof. The modifier is a primary alcohol. A method of separating cesium and strontium from an aqueous feed is also disclosed, as are dialkyloxycalix[4]arenebenzocrown-6 compounds and an alcohol modifier.Type: ApplicationFiled: November 10, 2008Publication date: May 13, 2010Inventors: DEAN R. PETERMAN, DAVID H. MEIKRANTZ, JACK D. LAW, CATHERINE L. RIDDLE, TERRY A. TODD, MITCHELL R. GREENHALGH, RICHARD D. TILLOTSON, RICHARD A. BARTSCH, BRUCE A. MOYER, LAETITIA H. DELMAU, PETER V. BONNESEN
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Patent number: 7696362Abstract: A new artemisinin derivatives, of following general formula (I): In which: a and b are a single or a double bond, n1 and n2 are 0 or 1, R1 is a fluoroalkyl group or a fluoroaryl group, R2 is a hydrogen atom, or a halogen atom, or a group, if appropriate ionisable, making it possible to render said compounds of formula (I) water-soluble, R3 is a group, if appropriate ionisable, making it possible to render said compounds of formula (I) water-soluble, R4 is H or OH. The invention also relates to the process by which they are obtained, and their uses in pharmaceutical compositions intended for the treatment of malaria.Type: GrantFiled: July 9, 2008Date of Patent: April 13, 2010Assignee: Centre National de la Recherche ScientifiqueInventors: Jean-Pierre Begue, Danièle Bonnet-Delpon, Benoît Crousse, Michèle Ourevitch, Fatima Chorki, Fabienne Grellepois, Guillaume Magueur
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Patent number: 7642362Abstract: Compounds represented by the general formula (1) wherein R1 and R3 are each independently hydrogen or a carboxyl group and R2 and R4 are each independently hydrogen or a hydroxyl group, or pharmaceutically acceptable salts thereof, which exhibit semaphorin-inhibitory activity and are useful as preventives or remedies for neuropathic and neurodegenerative diseases are provided.Type: GrantFiled: January 22, 2003Date of Patent: January 5, 2010Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Kazuo Kumagai, Nobuo Hosotani
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Publication number: 20090298881Abstract: Water-soluble artemisinin derivatives, their preparation methods, the pharmaceutical compositions containing the same derivatives and the use thereof are disclosed. The artemisinin derivatives have following formula I. It has been proved by pharmacological tests that these compounds and compositions have evident immuno-suppressive activities, and may be used in the preparation of novel immuno-suppressants for treating the diseases caused by hyperfunction of human immunity (e.g. the auto-immune diseases such as lupus erythematosus, rheumatoid arthritis, multiple sclerosis and the like), and for inhibiting the graft rejection after cell or organ transplantation.Type: ApplicationFiled: July 20, 2006Publication date: December 3, 2009Inventors: Ying Li, Jianping Zuo, Zhongshun Yang, Junxia Wang, Yu Zhang, Wei Tang, Jianxin Zhang
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Publication number: 20090291923Abstract: The invention provides novel trioxane dimers having formulae III, IV or V: methods for their preparation, pharmaceutical compositions containing these compounds, and methods for treating cancer and/or malaria using these compounds and compositions.Type: ApplicationFiled: November 17, 2006Publication date: November 26, 2009Applicants: Johns Hopkins Universoty, The Government of the United States of America as Represented by the Secretary of the DHHS NIH, OffiInventors: Gary H. Posner, Ikhyeon Paik, Kristina Borstnik, Wonsuk Chang, Sandra Sinishtaj, William Malo, John Gaetano D'Angelo, Lauren Elaine Woodard, Alvin Solomon Kalinda, Aimee R. Usera, Lindsey Catherine Hess, Andrew Scott Rosenthal, Seongho Oh, Astrid C. Baege
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Publication number: 20090270492Abstract: Biologically active compounds related to the bryostatin family of compounds, including methods of utilizing the same.Type: ApplicationFiled: August 28, 2008Publication date: October 29, 2009Inventor: PAUL A. WENDER
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Patent number: 7531359Abstract: The chemical compound: Each R1 is H or CH3. A device for detecting an analyte having: a substrate; a film on the substrate, a flow cell for delivering air containing the analyte to the film, and an apparatus for measuring the refractive index of the film. Each R2 is an alkyl group. Each X is O or S.Type: GrantFiled: March 1, 2006Date of Patent: May 12, 2009Assignee: The United States of America as Represented by the Secretary of the NavyInventors: Devanand Shenoy, Elias Feresenbet, Enrico Dalcanale, Susan Daly
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Publication number: 20090082426Abstract: The present invention relates to dimers of artemisinin derivatives, to processes for the preparation of such dimers, to methods of treatment comprising administration of such dimers, and to intermediates to such dimers.Type: ApplicationFiled: October 2, 2008Publication date: March 26, 2009Applicant: SANOFI-AVENTISInventors: Alain COMMERCON, Jidong ZHANG, Augustin HITTINGER
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Publication number: 20090069412Abstract: The present application describes deuterium-enriched sugammadex, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: August 21, 2008Publication date: March 12, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Patent number: 7452915Abstract: This invention relates to the use of certain C-10 substituted derivatives of artemisinin of general formula (I) in the treatment and/or prophylaxis of diseases caused by infection with a parasite, certain novel C-10 substituted derivatives of artemisinin, processes for their preparation and pharmaceutical compositions containing such C-10 substituted derivatives. The compounds are particularly effective in the treatment of malaria, neosporosis and coccidiosis.Type: GrantFiled: January 9, 2006Date of Patent: November 18, 2008Assignee: The Hong Kong University of Science and TechnologyInventors: Richard K. Haynes, William Wai-Lun Lam, Ho-Wai Chan, Hing-Wo Tsang, Man-Ki Cheung, Gisela Greif, Gabriele Schmuck, Arnd Voerste
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Publication number: 20080281108Abstract: The invention relates to chiral compounds, methods of their preparation, and to their use in optical, electrooptical, electronic, semiconducting or luminescent components or devices, and in decorative, security, cosmetic or diagnostic applications.Type: ApplicationFiled: September 20, 2006Publication date: November 13, 2008Inventor: Louise Diane Farrand
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Publication number: 20080272337Abstract: The invention relates to chiral compounds, methods of their preparation, and to their use in optical, electrooptical, electronic, semiconducting or luminescent components or devices, and in decorative, security, cosmetic or diagnostic applications.Type: ApplicationFiled: September 20, 2006Publication date: November 6, 2008Inventor: Louise Diane Farrand
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Publication number: 20080275106Abstract: This invention comprises compositions containing dihydroartemisinin- and dihydroartemisitene-dimers with activity as anticancer or anticancer metastasis agents and anti-protozal, including anti-malarial and anti-leishmanial properties. This invention also describes methods of preparation of these compositions and methods of use of such compositions for the treatment of cancer or prevention of cancer metastasis, and protozoal infections, including malaria, or leishmaniasis. The compounds of this invention represent a potential new class of anti-tumor or anti-metastasis agents, one that has shown promising activity against solid tumors.Type: ApplicationFiled: June 21, 2005Publication date: November 6, 2008Applicant: THE UNIVERSITY OF MISSISSIPPIInventors: Mahmoud A. Elsohly, Waseem Gul
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Publication number: 20080255223Abstract: A method of treating a benign pigmented mole or a dermatomycosis. The method comprises locally applying to a subject in need thereof artemisinine and/or one or more structurally related compounds. Also disclosed is a plaster which comprises a topical formulation comprising artemisinine and/or one or more structurally related compounds.Type: ApplicationFiled: October 19, 2006Publication date: October 16, 2008Inventor: Rosemarie Sift Carter
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Patent number: 7425356Abstract: The invention relates to chiral compounds of formula I wherein X1, X2, X1, X2, x1, x2, y1, y2, B, C, U1, U2, V1, V2, W1 and W2 have the meaning given in claim 1, to liquid crystal mixtures comprising at least one chiral compound of formula I, to chiral linear or crosslinked liquid crystal polymers obtainable by polymerizing a polymerizable mixture comprising at least one chiral compound of formula I, to the use of chiral compound of formula I and mixtures and polymers obtained thereof in liquid crystal displays, active and passive optical elements, adhesives, synthetic resins with anisotropic mechanical properties, cosmetic and pharmaceutical compositions, diagnostics, liquid crystal pigments, for decorative and security applications, nonlinear optics, optical information storage or as chiral dopants, and to a liquid crystal display comprising a mixture comprising at least one chiral compound of formula I.Type: GrantFiled: May 24, 2007Date of Patent: September 16, 2008Assignee: Merck Patent GmbHInventors: Andreas Taugerbeck, Peer Kirsch, Detlef Pauluth, Joachim Krause, Juliane Suermann, Michael Heckmeier
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Publication number: 20080206103Abstract: Methods for the preparation of a stable, self-assembled monolayer on the silicon surface or metallic coating of a microcantilever are disclosed. The methods produce a microcantilever suitable as a chemical sensor. In a microcantilever produced using one version of the method, a metallic coating is disposed on a side of the microcantilever, a bridging atom is bonded to the metallic coating, a first spacer group is bonded to the bridging atom, a second spacer group is bonded to the bridging atom, and a chemical recognition agent is bonded to the first spacer group. In another version of the method, a silicon surface of a microcantilever is hydrogen terminated, and a calixarene chemical recognition agent is carbon linked to the silicon surface using photochemical hydrosilylation. Among other things, the calixarene may be bonded to a crown ether for ion detection or bonded to a area for the recognition of explosives by hydrogen bonding to nitro groups.Type: ApplicationFiled: September 14, 2005Publication date: August 28, 2008Applicants: UT-BATTELLE, LLC, UNIVERSITY OF TENNESSEE RESEARCH FOUNDATIONInventors: Lal A. Pinnaduwage, Thomas G. Thundat, Gilbert M. Brown, Peter V. Bonnesen, Vassil Boiadjiev, Gudron Goretzki
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Patent number: 7417155Abstract: A new artemisinin derivatives, of following general formula (I): In which: a and b represent a single or a double bond, n1 and n2 represent 0 or 1, R1 represents a fluoroalkyl group or a fluoroaryl group, R2 represents a hydrogen atom, or a halogen atom, or a group, if appropriate ionisable, making it possible to render said compounds of formula (I) water-soluble, R3 represents a group, if appropriate ionisable, making it possible to render said compounds of formula (I) water-soluble, R4 represents H or OH. The invention also relates to the process by which they are obtained, and their uses in pharmaceutical compositions intended for the treatment of malaria.Type: GrantFiled: October 25, 2002Date of Patent: August 26, 2008Assignee: Centre National de la Recherche ScientifiqueInventors: Jean-Pierre Begue, Danièle Bonnet-Delpon, Benoît Crousse, Michèle Ourevitch, Fatima Chorki, Fabienne Grellepois, Guillaume Magueur
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Patent number: 7417156Abstract: In only two steps and in 65% overall yield, natural trioxane artemisinin (I) was converted on gram scale into C-10-carba trioxane dimer (3). This new, very stable dimer was then transformed easily in one additional step into four different dimers (4-7). Alcohol and diol dimers (4 and 5) and ketone dimer (7) are 10 times more antimalarially potent in vitro than artemisinin (I), and alcohol and diol dimers (4 and 5) are strongly inhibitory but not cytotoxic toward several human cancer cell lines. Water-soluble carboxylic acid derivatives (8a-10c and 12) were easily prepared from dimers (4-6); they are thermally stable even at 60° C. for 24 hours, are more orally efficacious as antimalarials than either artelinic acid or sodium artesunate, and have potent and selective anticancer activities.Type: GrantFiled: September 26, 2003Date of Patent: August 26, 2008Assignee: Johns Hopkins UniversityInventors: Gary H. Posner, Theresa A. Shapiro, Surojit Sur, Tanzina Labonte, Kristina Borstnik, Ik-Hyeon Paik, Andrew J. McRiner
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Patent number: 7223450Abstract: The invention relates to chiral compounds of formula I wherein X1,X2,X1,X2,x1,x2,y1,y2,B,C,U1,U2,V1,V2,W1 and W2 have the meaning given in claim 1, to liquid crystal mixtures comprising at least one chiral compound of formula I, to chiral linear or crosslinked liquid crystal polymers obtainable by polymerizing a polymerizade mixture comprising at least one chiral compound of formula I, to the use of chiral compound of formula I and mixtures and polymers obtained thereof in liquid crystal display, active and passive optical elements, adhesives, synthetic resins with anisotropic mechanical properties, cosmetic and pharmaceutical compositions, diagnostics, liquid crystal pigments, for decorative and security applications, nonlinear optics, optical information storage or as chiral dopants, and to a liquid crystal display comprising a mixture comprising at least one chiral compound of formula I.Type: GrantFiled: April 25, 2002Date of Patent: May 29, 2007Assignee: Merck GmbHInventors: Andreas Taugerbeck, Peer Kirsch, Detlef Pauluth, Joachim Krause, Juliane Suermann, Michael Heckmeier
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Patent number: 7214538Abstract: The present invention relates to a novel device and method for the detection of lithium ions in a biological fluid. In a preferred embodiment, the present invention provides a novel compound and a optical sensor which incorporates said compound for the detection of lithium ions. Additionally, the present invention provides a method of detecting lithium ions which comprises placing the novel optical sensor into communication with a biological fluid. Once the novel compound of the present invention encounters a lithium ion(s), a fluorescence is generated, the intensity of which is measured and allows for the determination of lithium ion concentration. The present invention provides a medical professional with the ability to selectively determine lithium ion concentration in a biological fluid thereby facilitating the treatment of various diseases, such as manic-depressive illness.Type: GrantFiled: February 11, 2004Date of Patent: May 8, 2007Assignees: Worcester Polytechnic Institute, Bayer Health Care, LLC.Inventors: John S. Benco, Hubert A. Nienaber, W. Grant McGimpsey
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Patent number: 7205401Abstract: Diketo- and pyridine-containing chiral crown ligands having at least two chiral bulky groups attached to two different chiral carbon atoms of the crown that are covalently bonded to or coated on suitable solid supports, and further coated by hydrophobic organic solvents are disclosed. These compositions and associated methods are characterized by selectivity of several target amine or amino acid enantiomers over their counter-enantiomers and derivatives. The composition preferably has an ?-value greater than or equal to 4. This allows for the separation of such enantiomers with non-chromatographic resin bed separations of three separation stages or less.Type: GrantFiled: September 16, 2003Date of Patent: April 17, 2007Assignee: IBC Advanced Technologies, Inc.Inventors: Ronald L. Bruening, Krzysztof E. Krakowiak
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Patent number: RE39593Abstract: 1-phenyl-3-dimethylaminopropane compounds corresponding to the formula I a method of preparing them, and the use of these substances as analgesic active ingredients in pharmaceutical compositions.Type: GrantFiled: June 17, 2003Date of Patent: April 24, 2007Assignee: Gruenenthal GmbHInventors: Helmut Buschmann, Wolfgang Strassburger, Elmar Friderichs