Plural Chalcogens Bonded Directly To The Tricyclo Ring System Patents (Class 549/391)
  • Patent number: 10508124
    Abstract: To develop a protecting group that facilitates separation and purification, after reaction, of a compound including a protected functional group, without solidifying or insolubilizing the compound.
    Type: Grant
    Filed: July 24, 2017
    Date of Patent: December 17, 2019
    Assignee: SEKISUI MEDICAL CO., LTD.
    Inventors: Shinya Yano, Toshihiro Mori, Hideki Kubota
  • Patent number: 9987567
    Abstract: Raw plant material is mixed with ethanol under pressure to extract essential elements. The resulting crude oil and ethanol with the dissolved essential elements is separated from the raw plant material and filtered to remove particulates, waxes, lipids, fats and dissolved impurities. The ethanol is then evaporated from the resulting mixture of crude oil and ethanol, and the remaining crude oil then undergoes decarboxylation and distillation to obtain the essential elements. The ethanol may be chilled before adding it to the raw plant material.
    Type: Grant
    Filed: September 29, 2017
    Date of Patent: June 5, 2018
    Assignee: NextLeaf Solutions Ltd.
    Inventor: Ryan Delmoral Ko
  • Patent number: 9808494
    Abstract: Processes are described herein for the extraction of cannabinoids from cannabis using lipids as an extraction solvent.
    Type: Grant
    Filed: January 22, 2016
    Date of Patent: November 7, 2017
    Assignee: RM3 Labs, LLC
    Inventor: Ian Barringer
  • Publication number: 20150126754
    Abstract: The present invention relates to a method for preparing a Cannabis plant ?9-tetrahydrocannabinol isolate from a crude solvent extract of Cannabis plant material. The invention relates further to a Cannabis plant THC isolate comprising ?9-tetrahydrocannabinol, Cannabinol (CBN) and/or Cannabidiol (CBD) and to a pharmaceutical composition comprising the Cannabis plant THC isolate.
    Type: Application
    Filed: May 3, 2013
    Publication date: May 7, 2015
    Applicant: Echo Pharmaceuticals B.V.
    Inventors: Maria Vanesa Fernandez Cid, Dennis Van Houten
  • Publication number: 20150125892
    Abstract: The invention relates to fused cyclooctyne compounds, and to a method for their preparation. The invention also relates to a conjugate wherein a fused cyclooctyne compound according to the invention is conjugated to a label, and to the use of these conjugates in bioorthogonal labeling, imaging and/or modification, such as for example surface modification, of a target molecule. The invention further relates to a method for the modification of a target molecule, wherein a conjugate according to the invention is reacted with a compound comprising a 1,3-dipole or a 1,3-(hetero)diene.
    Type: Application
    Filed: October 10, 2014
    Publication date: May 7, 2015
    Applicant: SynAffix B.V.
    Inventors: Floris Louis VAN DELFT, Floris Petrus Johannes Theodorus Rutjes, Frederik Jan Dommerholt
  • Publication number: 20140329895
    Abstract: The invention relates to (among other things) oligomer-cannabinoid conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered un-conjugated cannabinoid compounds.
    Type: Application
    Filed: July 22, 2014
    Publication date: November 6, 2014
    Inventors: Jennifer Riggs-Sauthier, C. Simone Jude-Fishburn, Guy Lalonde
  • Patent number: 8865914
    Abstract: The invention provides fluorescent sensors for the selective detection of a metal such as copper. The sensors may be considered to be derivatives of cyanine, fluorescein, rhodamine, rhodol, Tokyo green, or BODIPY. The sensors find particular use in detecting copper in cells and living animals.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: October 21, 2014
    Assignee: The Regents of the University of California
    Inventors: Christopher J. Chang, Genevieve C. Van De Bittner, Tasuku Hirayama, Jefferson Chan
  • Publication number: 20140305336
    Abstract: There is provided a compound represented by the following Formula (3): wherein in Formula (3), R201, R202 and R203 each independently represent a monovalent substituent, n201 and n202 each independently represent a number of 0 to 4, and n203 represents a number of 0 to 4, when n201, n202 and n203 each represent a number of 2 or more, a plurality of R201's, R202's and R203's may be the same or different, M represents a hydrogen atom or a counter cation, and M's may be the same or different, and a coloring composition containing the compound.
    Type: Application
    Filed: June 25, 2014
    Publication date: October 16, 2014
    Applicant: FUJIFILM Corporation
    Inventors: Yoshihiko FUJIE, Clive Edwin FOSTER, Keiichi TATEISHI
  • Patent number: 8846749
    Abstract: The present invention provides a novel xanthone derivative compound or a pharmaceutically acceptable salt thereof. The compound is useful as a chemosensitizer that reduces anticancer drug resistance.
    Type: Grant
    Filed: August 19, 2010
    Date of Patent: September 30, 2014
    Assignee: Ewha University-Industry Collaboration Foundation
    Inventors: Young Hwa Na, Young Joo Kwon, Hwa Jeong Lee, Song Wha Chae, Sang Wook Woo, Hee Ju Cho
  • Publication number: 20140256803
    Abstract: The present invention is directed to compounds that are allosteric inhibitors of tumor necrosis factor receptor I, compositions comprising such compounds, and methods of using such compounds and compositions thereof in the treatment of TNF-? mediated conditions.
    Type: Application
    Filed: May 16, 2014
    Publication date: September 11, 2014
    Applicant: THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA
    Inventors: MARK I. GREENE, RAMACHANDRAN MURALI, XIN CHENG, RAPHAEL OTTENBRITE, YINGXIN XIAO
  • Patent number: 8829043
    Abstract: The invention relates to (among other things) oligomer-cannabinoid conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered un-conjugated cannabinoid compounds.
    Type: Grant
    Filed: February 6, 2009
    Date of Patent: September 9, 2014
    Assignee: Nektar Therapeutics
    Inventors: Jennifer Riggs-Sauthier, C. Simone Jude-Fishburn, Guy Lalonde
  • Publication number: 20140105920
    Abstract: Described herein are compositions and methods for preventing and/or treating diseases involving aberrant angiogenesis employing one or more benzo[c]chromen-6-one derivatives.
    Type: Application
    Filed: May 23, 2013
    Publication date: April 17, 2014
    Inventor: David Sherris
  • Publication number: 20140093907
    Abstract: Compounds and methods for determining transmembrane potential, monitoring changes in transmembrane potential, and/or drug screening are provided. In one aspect, compounds of the invention have a structure according to the formula: E-M-A, wherein A is a fluorophore, selected from xanthenes, eoumarins, cyanines, bimanes, and difluoroboradizaindacenes, charged at physiological pH; M is a molecular wire; and E is a hydrophobic moiety, wherein A and E are capable of being involved in a photo-induced, intramolecular electron transfer that quenches the fluorescence of A in response to a voltage condition. When in use, compounds of the invention are membrane-impermeant and oriented within the cell membrane such that the charged moiety localizes at the outer leaflet of the lipid bilayer and the hydrophobic moiety and molecular wire associate with the hydrophobic portion of the lipid bilayer.
    Type: Application
    Filed: May 21, 2012
    Publication date: April 3, 2014
    Applicant: The Regents of the University of California
    Inventors: Evan Walker Miller, Roger Y. Tsien
  • Patent number: 8664411
    Abstract: Disclosed are novel gamma secretase inhibitors of the formula. Also disclosed are methods of inhibiting gamma-secretase, methods of treating neurodegenerative diseases, and methods of treating Alzheimer's Disease. Also disclosed are processes for preparing alkenes in one reaction step using a mixture of an aldehyde (or ketone) and an alkyl substituted with two electron withdrawing groups, and reacting the mixture with: (a) a sulfonyl halide (e.g., a sulfonyl chloride) and a basic tertiary amine, or, (b) a sulfonyl anhydride and a basic amine, or (c) an aryl-C(O)-halide and a basic tertiary amine, or (d) an aryl-C(O)—O—C(O)-aryl and a basic tertiary amine, or (e) an heteroaryl-C(O)-halide and a basic tertiary amine, or (f) a heteroaryl-C(O)—O—C(O)-heteroaryl and a basic tertiary amine.
    Type: Grant
    Filed: July 1, 2008
    Date of Patent: March 4, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Wen-Lian Wu, Thomas A. Bara, Duane A. Burnett, John W. Clader, Martin S. Domalski, Yan Jin, Hubert B. Josien, Hongmei Li, Xian Liang, Dmitri A. Pissarnitski, Thavalakulamgara K. Sasikumar, Jesse K. Wong, Ruo Xu, Zhiqiang Zhao, Paul McNamara
  • Patent number: 8569360
    Abstract: Derivatives and analogs of inhibitors of receptor tyrosine kinase c-Met obtained by virtual screening, pharmaceutical compositions containing derivatives and analogs of c-Met inhibitors are provided. Methods of making derivatives and analogs of c-Met inhibitors and methods of use thereof are provided.
    Type: Grant
    Filed: March 31, 2009
    Date of Patent: October 29, 2013
    Inventors: Donald P. Bottaro, Megan Peach, Marc Nicklaus, Nelly Tan
  • Patent number: 8497299
    Abstract: The present invention relates to cannabinoic quinone compounds, and especially to their medical use. In particular five cannabinoic quinones, designated HU-331, HU-336, HU-345, HU-395 and HU-396, are described as active agents in pharmaceutical compositions. These compounds and compositions thereof are intended for the treatment of inflammatory, infectious, auto-immune and particularly hyperproliferative disorders. Thus, the compounds of the invention may be used as anti-tumor agents, or for the treatment of cancer. Furthermore, three of these compounds, HU-345, HU-395 and HU-396, are novel cannabinoic quinones.
    Type: Grant
    Filed: January 14, 2005
    Date of Patent: July 30, 2013
    Assignee: Yissum Research Development Company of The Hebrew University of Jerusalem
    Inventors: Raphael Mechoulam, Natalya M. Kogan, Ruth Rabinowitz, Michael Schlesinger
  • Publication number: 20130123487
    Abstract: The invention relates to solid supports useful in medical applications that provide controlled release of drugs, such as peptides, nucleic acids and small molecules. The drugs are covalently coupled to the solid support through a linkage that releases the drug or a prodrug through controlled beta elimination.
    Type: Application
    Filed: May 5, 2011
    Publication date: May 16, 2013
    Applicant: PROLYNX LLC
    Inventors: Gary Ashley, Daniel V. Santi
  • Patent number: 8394850
    Abstract: A compound represented by the following general formula (IA) or (IB) (R1 represents an electron withdrawing substituent, R2 and R3 represent a hydrogen atom or a halogen atom; R4 and R3 represent a hydrogen atom, an alkylcarbonyl group, or an alkylcarbonyloxymethyl group, and R6 represents a hydrogen atom or an alkyl group) or a salt thereof, and a reagent for measuring hydrogen peroxide comprising the compound or a salt thereof.
    Type: Grant
    Filed: March 4, 2009
    Date of Patent: March 12, 2013
    Assignee: The University of Tokyo
    Inventors: Tetsuo Nagano, Yasuteru Urano, Masahiro Abo
  • Publication number: 20120264736
    Abstract: This invention discloses novel gamma secretase inhibitors of the formula: R2 and R3, or R2 and R4, or R3 and R4, together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substituents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.
    Type: Application
    Filed: October 6, 2011
    Publication date: October 18, 2012
    Applicant: Schering Corporation
    Inventors: Theodros Asberom, Thomas A. Bara, Chad E. Bennett, Duane A. Burnett, Mary Ann Caplen, John W. Clader, David J. Cole, Martin S. Domalski, Hubert B. Josien, Chad E. Knutson, Hongmei Li, Mark D. McBriar, Dmitri A. Pissarnitski, Li Qiang, Murali Rajagopalan, Thavalakulamgara K. Sasikumar, Jing Su, Haiqun Tang, Wen-Lian Wu, Ruo Xu, Zhiqiang Zhao
  • Patent number: 8258322
    Abstract: An improved process is provided for the synthesis of hexahydrodibenzo[b,d]pyran-9-ones, such as nabilone.
    Type: Grant
    Filed: August 28, 2009
    Date of Patent: September 4, 2012
    Assignee: Watson Laboratories, Inc.
    Inventors: Valeriy Mikaylo, Subakar Paramanantham, Ilya Avrutov, Martyn A. Brown, Zemin Li, Natalie Lazarowych
  • Publication number: 20120122917
    Abstract: This invention discloses cannabinoid derivatives and pharmaceutical uses thereof.
    Type: Application
    Filed: January 23, 2012
    Publication date: May 17, 2012
    Inventor: Craig Rick Travis
  • Patent number: 8173698
    Abstract: The present invention provides fluorogenic probes and corresponding fluorescent compounds, methods of using the probes, compounds and kits that include the probes.
    Type: Grant
    Filed: February 29, 2008
    Date of Patent: May 8, 2012
    Assignee: Life Technologies Corporation
    Inventors: Iain Johnson, Jixiang Liu, Brian Patch, Wai-Yee Leung
  • Publication number: 20120069289
    Abstract: The present invention relates to polymerisable compounds, to processes and intermediates for the preparation thereof, and to the use thereof for optical, electro-optical and electronic purposes, in particular in liquid-crystal (LC) media and LC displays, especially in LC displays of the PS (polymer stabilised) and PSA (polymer sustained alignment) type.
    Type: Application
    Filed: April 19, 2010
    Publication date: March 22, 2012
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Andreas Taugerbeck, Alexander Hahn, Achim Goetz
  • Publication number: 20120042398
    Abstract: The invention provides methods and compositions for detecting and measuring the amount of autophagosomes in cells or tissues, including biopsy samples, in vitro, in situ and/or in vivo. By detecting and measuring the amount of autophagosomes in cells or tissues, the methods and compositions of the invention also measure the amount of autophagic activity in a cell or a tissue. In one aspect, the invention can be adapted to a plate-reader format for high-throughput screening of drugs that modulate autophagy, i.e., high-throughput detection of autophagic (autophagosome) activity in cells or tissues. In alternative embodiments, the compositions of the invention can localize into autophagosomes (AV), and these compositions can comprise any detectable moiety or group, e.g., a cadaverine, a radioactive, fluorescent-, bioluminescent and/or paramagnetic-conjugated reagent.
    Type: Application
    Filed: October 13, 2009
    Publication date: February 16, 2012
    Applicant: SAN DIEGO STATE UNIVERSITY (SDSU) FOUNDATION
    Inventors: Roberta A. Gottlieb, Thomas E. Cole, Cynthia N. Perry-Garza, Raquel Sousa Carreira, Bryan J. Bartlett, Kim Finley
  • Publication number: 20120022063
    Abstract: The invention relates to (among other things) oligomer-cannabinoid conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered un-conjugated cannabinoid compounds.
    Type: Application
    Filed: February 6, 2009
    Publication date: January 26, 2012
    Applicant: Nektar Therapeutics
    Inventors: Jennifer Riggs-Sauthier, C. Simone Jude-Fishburn, Guy Lalonde
  • Publication number: 20110281907
    Abstract: Derivatives and analogs of inhibitors of receptor tyrosine kinase c-Met obtained by virtual screening, pharmaceutical compositions containing derivatives and analogs of c-Met inhibitors are provided. Methods of making derivatives and analogs of c-Met inhibitors and methods of use thereof are provided.
    Type: Application
    Filed: March 31, 2009
    Publication date: November 17, 2011
    Applicant: The Government of the United States of America, as represented by the Secretary, Dept.of Health and.
    Inventors: Donald P. Bottaro, Megan Peach, Marc Nicklaus, Nelly Tan
  • Patent number: 7998541
    Abstract: The present invention relates to benzochromene derivatives of the formula I where the various parameters have the meaning indicated in the text, and to liquid-crystal media which comprise these compounds, and to the use of the media in electro-optical displays, in particular in TN, OCB, LCOS and/or IPS-LCDs, and to the use of the compounds and physiologically acceptable derivatives thereof as therapeutic active ingredients.
    Type: Grant
    Filed: December 5, 2006
    Date of Patent: August 16, 2011
    Assignee: Merck Patent GmbH
    Inventors: Andreas Taugerbeck, Elvira Montenegro, Atsutaka Manabe, Herbert Plach
  • Patent number: 7932014
    Abstract: A photosensitive compound has two or more structural units, in a molecule, represented by the following general formula (1): wherein R1 to R8 are selected from the group consisting of a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, an acetoxy group, a phenyl group, a naphthyl group, and an alkyl group in which some or all of the hydrogen atoms are optionally replaced by fluorine atoms; R9 is a hydrogen atom or a hydroxyl group; X is a substituted or unsubstituted phenylene group or a substituted or unsubstituted naphthalene group; and Y is an oxygen atom or a single bond.
    Type: Grant
    Filed: February 14, 2008
    Date of Patent: April 26, 2011
    Assignee: Canon Kabushiki Kaisha
    Inventor: Toshiki Ito
  • Publication number: 20110092584
    Abstract: The present invention relates to cannabinoic quinone compounds, and especially to their medical use. In particular five cannabinoic quinones, designated HU-331, HU-336, HU-345, HU-395 and HU-396 are herein described as active agents in pharmaceutical compositions. Said compounds and compositions thereof are intended for the treatment of inflammatory, infectious, auto-immune and particularly hyperproliferative disorders. Thus, the compounds of the invention may be used as anti-tumor agents, or for the treatment of cancer. Furthermore, three of these compounds, HU-345, HU-395 and HU-396, are novel cannabinoic quinones and thus are also claimed herein.
    Type: Application
    Filed: January 14, 2005
    Publication date: April 21, 2011
    Applicant: YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM
    Inventors: Raphael Mechoulam, Natalya M. Kogan, Ruth Rabinowitz, Michael Schlesinger
  • Publication number: 20100311826
    Abstract: The present invention relates to xanthone compounds isolated from the plant Psorospermum molluscum Hochr. (Clusiaceae), a Madagascar plant, which are potent cytotoxic agents.
    Type: Application
    Filed: September 11, 2008
    Publication date: December 9, 2010
    Inventors: John E. Leet, Craig R. Fairchild, Stephen W. Mamber, Xiaohong Liu
  • Publication number: 20100168086
    Abstract: The present invention relates to new 7,8,10,10a-tetrahydro-6H-benzo[c]chromen-9(6aH)-one modulators of cannabinoid receptors, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: September 23, 2009
    Publication date: July 1, 2010
    Applicant: AUSPEX PHARMACEUTICALS, INC.
    Inventors: Thomas G. Gant, Manoucherhr M. Shahbaz
  • Patent number: 7696245
    Abstract: A compound represented by the following general formula (IA) or (IB) or a salt thereof which specifically traps a zinc ion and emits fluorescence, and is useful as a fluorescent probe for zinc: wherein R1 and R2 represent a hydrogen atom or a group represented by the following formula (A): wherein X1 to X4 represent a hydrogen atom, a 2-pyridylmethyl group, a 2-pyridylethyl group, a 2-methyl-6-pyridylmethyl group, or a 2-methyl-6-pyridylethyl group, provided that at least one is the group except a 2-pyridylmethyl group, and m and n represent 0 or 1, provided that they are not simultaneously 0; provided that R1 and R2 are not simultaneously hydrogen atoms; R3 and R4 represent a hydrogen atom or a halogen atom; R5 and R6 represent a hydrogen atom, an alkylcarbonyl group, or an alkylcarbonyloxymethyl group; and R7 represents a hydrogen atom or an alkyl group.
    Type: Grant
    Filed: January 30, 2004
    Date of Patent: April 13, 2010
    Assignees: Sekisui Medical Co., Ltd.
    Inventors: Kensuke Komatsu, Tomoya Hirano, Kazuya Kikuchi, Tetsuo Nagano
  • Patent number: 7674922
    Abstract: The present invention relates to a process for preparation of a delta-9-tetrahydrocannabinol compound or derivative thereof involving treating a first intermediate compound with an organoaluminum-based Lewis acid catalyst, under conditions effective to produce the delta-9-tetrahydrocannabinol compound or derivative thereof. Another aspect of the present invention relates to a process for preparation of a cannabidiol or cannabidiolate compound involving reacting a first starting compound with a second starting compound in the presence of a metal triflate catalyst, under conditions effective to form the cannabidiol or cannabidiolate compound. The present invention also relates to a compound of the formula: where R8, R9, and R10 are the same or different and independently selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or halo, with R1, R2, and R3 defined herein.
    Type: Grant
    Filed: September 28, 2006
    Date of Patent: March 9, 2010
    Assignee: Albany Molecular Research, Inc.
    Inventors: David C. Burdick, Steven J. Collier, Frédéric Jos, Betina Biolatto, Bernhard J. Paul, Harold Meckler, Mark A. Helle, Alicia J. Habershaw
  • Publication number: 20100056811
    Abstract: An improved process is provided for the synthesis of hexahydrodibenzo[b,d]pyran-9-ones, such as nabilone.
    Type: Application
    Filed: August 28, 2009
    Publication date: March 4, 2010
    Inventors: Valeriy Mikaylo, Subakar Paramanantham, Ilya Avrutov, Martyn A. Brown, Zemin Li, Natalie Lazarowych
  • Publication number: 20090238765
    Abstract: The invention relates to contrast agents for imaging of diseases associated with inflammations. More specifically the invention provides optical imaging contrast agents for imaging of activated leukocytes and methods for imaging of such. The contrast agent changes its fluorescent properties upon reaction with oxidants produced by the activated leukocytes.
    Type: Application
    Filed: December 13, 2005
    Publication date: September 24, 2009
    Inventor: Helge Tolleshaug
  • Publication number: 20090062543
    Abstract: Novel energy transfer dyes which can be used with shorter wavelength light sources are provided. These dyes include a donor dye with an absorption maxima at a wavelength between about 250 to 450 nm and an acceptor dye which is capable of absorbing energy emitted from the donor dye. One of the energy transfer dyes has a donor dye which is a member of a class of dyes having a coumarin or pyrene ring structure and an acceptor dye which is capable of absorbing energy emitted from the donor dye, wherein the donor dye has an absorption maxima between about 250 and 450 nm and the acceptor dye has an emission maxima at a wavelength greater than about 500 nm.
    Type: Application
    Filed: July 18, 2008
    Publication date: March 5, 2009
    Applicant: Applied Biosystems Inc.
    Inventor: Linda G. Lee
  • Publication number: 20090029389
    Abstract: The present invention provides fluorogenic compounds for the detection of target metal ions wherein the compounds exhibit a Stokes shift greater than 50 nm and the detectable signal is modulated by photoinduced electron transfer (PET). The present compounds consist of three functional elements, the ion sensing moiety (chelating moiety), the reporter moiety (fluorophore or fluorescent protein) and spacer or linker between the sensing and reporter moieties of the present compound that allows for PET upon binding of a metal ion and excitation by an appropriate wavelength.
    Type: Application
    Filed: July 25, 2008
    Publication date: January 29, 2009
    Applicant: INVITROGEN CORPORATION
    Inventors: Kyle Richard Gee, Vladimir Martin
  • Publication number: 20080318255
    Abstract: The present invention relates to a method (assay) for determining the activity of an enzyme selected from the group consisting of a sphingosine kinase and a phosphatase involved in the sphingolipid pathway by use of a labeled sphingosine.
    Type: Application
    Filed: September 28, 2004
    Publication date: December 25, 2008
    Inventors: Andreas Billich, Peter Ettmayer, Diana Mechtcheriakova, Peter Nussbaumer, Alexander Wlachos
  • Publication number: 20080275215
    Abstract: The present invention is related to new fluorescein derivatives, the method for producing such derivatives and their use for the synthesis of fluorogenic peptides and in particular protease substrates and peptide ligands.
    Type: Application
    Filed: July 25, 2006
    Publication date: November 6, 2008
    Applicant: COMMISSARIAT A L'ENERGIE ATOMIQUE
    Inventors: Maxim Balakirev, Olga Burchak
  • Publication number: 20080275257
    Abstract: Hydroxymethyl fluorescein derivatives are provided. The derivatives can be easily conjugated to other molecules, and are more permeable than other fluorescein derivatives. Methods of making the derivatives are also provided.
    Type: Application
    Filed: January 28, 2008
    Publication date: November 6, 2008
    Inventors: Kazunori Koide, Amanda L. Garner, Fengling Song
  • Publication number: 20080269510
    Abstract: Three new acylphloroglucinols, myrtucommulone-D (Compound 1), myrtucommulone-E (Compound 2), myrtucommulone-C (Compound 3), and a known acyphloroglucinol myrtucommulone B (Compound 4) were isolated from a methanolic extract of Myrtus communis L. The structures of compounds 1, 2 and 4 were also unambiguously determined by single X-ray diffraction analysis. The compounds 1-4 were found to be more potent ?-glucosidase inhibitors than the clinically used standards, acarbose and deoxynojirimycin. The compound 3 exhibited the highest activity among all the acylphloroglucinols, with an IC50=35.4±1.15 ?M. The compounds 1 and 2 also exhibited strong antibacterial activities.
    Type: Application
    Filed: December 23, 2005
    Publication date: October 30, 2008
    Applicant: INTERNATIONAL INSTITUTE OF CHEMICAL SCIENCES
    Inventors: Attaur Rahman, Mohammad Iqbal Choudhary, Farzana Shaheen, Manzoor Ahmad, Shamsun Nahar Khan, Shazia Anjum
  • Patent number: 7317038
    Abstract: To provide a semaphorin inhibitor; a peripheral or central nerve regeneration promoter which contains said semaphorin inhibitor as an active ingredient; and a preventive or remedy for a neuropathic disease and a neurodegenerative disease containing said nerve regeneration promoter, or the like. A low-molecular weight compound, which acts at a concentration of 10 ?g/ml or below to inhibit the growth cone collapse activity of semaphorin such as semaphorin 3A, semaphorin 6C or the like and/or the nerve outgrowth inhibitory activity of semaphorin in a collagen gel and which does not substantially affect cell proliferation, is obtained from the culture of strain SPF-3059 belonging to the genus Penicillium. The low-molecular weight compound with the semaphorin inhibitory activity thus obtained exhibits the in vivo nerve-regeneration promoting action.
    Type: Grant
    Filed: August 24, 2006
    Date of Patent: January 8, 2008
    Assignee: Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Toru Kimura, Kaoru Kikuchi, Kazuo Kumagai, Nobuo Hosotani, Akiyoshi Kishino
  • Patent number: 7244760
    Abstract: Psorospermin is a cytotoxic dihydroflranoxanthone that has found to exhibit significant activity against various tumor cell lines. Unfortunately, psorospermin is no longer readily available from its natural plant source. The present invention is directed to a method for preparing psorospermin and psorospermin analogs. Methods are also disclosed for utilizing psorospermin analogs to inhibit cellular proliferation.
    Type: Grant
    Filed: May 20, 2002
    Date of Patent: July 17, 2007
    Assignees: Board of Regents, The University of Texas System, Cylene Pharmaceuticals, Inc.
    Inventors: Laurence Hurley, Ingrid Fellows, Michael Kenric Schwaebe, Jeffrey Paul Whitten
  • Patent number: 7244761
    Abstract: To provide a semaphorin inhibitor; a peripheral or central nerve regeneration promoter which contains said semaphorin inhibitor as an active ingredient; and a preventive or remedy for a neuropathic disease and a neurodegenerative disease containing said nerve regeneration promoter, or the like. A low-molecular weight compound, which acts at a concentration of 10 ?g/ml or below to inhibit the growth cone collapse activity of semaphorin such as semaphorin 3A, semaphorin 6C or the like and/or the nerve outgrowth inhibitory activity of semaphorin in a collagen gel and which does not substantially affect cell proliferation, is obtained from the culture of strain SPF-3059 belonging to the genus Penicillium. The low-molecular weight compound with the semaphorin inhibitory activity thus obtained exhibits the in vivo nerve-regeneration promoting action.
    Type: Grant
    Filed: July 27, 2001
    Date of Patent: July 17, 2007
    Assignee: Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Toru Kimura, Kaoru Kikuchi, Kazuo Kumagai, Nobuo Hosotani, Akiyoshi Kishino
  • Patent number: 7105685
    Abstract: The invention provides cannabinol derivatives and pharmaceutical preparations thereof.
    Type: Grant
    Filed: December 22, 2002
    Date of Patent: September 12, 2006
    Inventor: Craig R. Travis
  • Patent number: 7041821
    Abstract: The invention provides Zn-chelating compounds that are molecularly engineered to bind to a specific target sequence in a protein of interest. The Zn2+ ion is far less toxic and promiscuous than nickel and therefore provides an attractive alternative to Ni-based labeling systems. Invention Zn-chelating compounds also do not require oxidizable thiols and therefore can be used in non-reducing environments such as the surface of living cells. In addition, the target sequence is genetically encodable and requires incorporation of only a few amino acids, unlike fusions to fluorescent proteins such as GFP.
    Type: Grant
    Filed: January 16, 2004
    Date of Patent: May 9, 2006
    Assignee: The Regents of the University of California
    Inventors: Roger Y. Tsien, Christina Hauser
  • Patent number: 7019024
    Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: January 9, 2001
    Date of Patent: March 28, 2006
    Assignee: Allelix Neuroscience Inc.
    Inventors: Vassil Iliya Ognyanov, Laurence A. Borden, Stanley Charles Bell, Jing Zhang
  • Patent number: 6939977
    Abstract: Disclosed are novel compounds represented by the following structural formula: R-X-Y; and physiologically acceptable salts thereof. R is a tricyclic core of a cannabinoid or substituted cannabinoid. X is a covalent bond, —CH2— or —CHR1—, wherein R1 a C1 to C3 substituted or unsubstituted alkyl group. Y is a heterocyclic ring, a substituted heterocyclic ring, a carbocyclic ring, a substituted carbocyclic ring, a fused bicyclic ring system, a substituted fused bicyclic ring system, a bridged bicyclic ring system, a substituted bridged bicyclic ring system, a bridged tricyclic ring system or a substituted bridged tricyclic ring system. Also disclosed is a method of stimulating a CB1 and/or CB2 receptor in a subject. The method comprises administering to the subject a therapeutically effective amount of R-X-Y.
    Type: Grant
    Filed: December 4, 2002
    Date of Patent: September 6, 2005
    Assignee: The University of Connecticut
    Inventors: Alexandros Makriyannis, Dai Lu, Atmaram Khanolkar
  • Patent number: 6933384
    Abstract: The invention provides Zn-chelating compounds that are molecularly engineered to bind to a specific target sequence in a protein of interest. The Zn2+ ion is far less toxic and promiscuous than nickel and therefore provides an attractive alternative to Ni-based labeling systems. Invention Zn-chelating compounds also do not require oxidizable thiols and therefore can be used in non-reducing environments such as the surface of living cells. In addition, the target sequence is genetically encodable and requires incorporation of only a few amino acids, unlike fusions to fluorescent proteins such as GFP.
    Type: Grant
    Filed: January 16, 2003
    Date of Patent: August 23, 2005
    Assignee: The Regents of the University of California
    Inventors: Roger Y. Tsien, Christina Hauser
  • Patent number: RE40572
    Abstract: A compound represented by general formula (IA) or a salt thereof useful as a fluorescent probe for zinc: wherein R1 and R2 represent a hydrogen atom or a group represented by formula (A), wherein X1, X2, X3, and X4 represent a hydrogen atom, an alkyl group, a 2-pyridylmethyl group, or a protective group for an amino group, and m and n represent 0 or 1 provided that R1 and R2 do not simultaneously represent hydrogen atoms; R3 and R4 represent a hydrogen atom or a halogen atom; and R5 and R6 represent a hydrogen atom, an alkylcarbonyl group, or an alkylcarbonyloxymethyl group, and R7 represents a hydrogen atom or an alkyl group.
    Type: Grant
    Filed: February 28, 2001
    Date of Patent: November 11, 2008
    Assignees: Sekisui Medical Co., Ltd.
    Inventors: Tetsuo Nagano, Kazuya Kikuchi, Tomoya Hirano