The Other Cyclo Of The Bicyclo Ring System Is A Six-membered Carbocyclic Ring To Which Chalcogen Is Directly Attached Patents (Class 549/289)
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Patent number: 10703735Abstract: The invention provides novel 4-phenyl-coumarin derivatives, processes for their preparation and uses thereof as specific mitochondrial RNA polymerase inhibitors for the treatment of cancer.Type: GrantFiled: July 23, 2019Date of Patent: July 7, 2020Assignees: Lead Discovery Center GmbH, Max Planck Gesellschaft zur Förderung der Wissenschaften e. V.Inventors: Raffaella Di Lucrezia, Tim Bergbrede, Peter Nussbaumer, Uwe Koch, Bert Klebl, Axel Choidas, Anke Unger, Nils-Göran Larsson, Maria Falkenberg-Gustafsson, Claes M. Gustafsson
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Patent number: 9663614Abstract: A photoactive coumarin monomer includes a substituted coumarin molecule that has at least two functional groups may be used to produce a polymer with a coumarin unit or a coumarin derivative unit as part of the polymer backbone. The polymer with a coumarin unit or a coumarin derivative unit as part of the polymer backbone may be photoresponsive and/or bioabsorbable. Photoresponsive polymers with a coumarin unit or a coumarin derivative unit as part of the polymer backbone may crosslink when irradiated at a wavelength of about 320 nm to about 420 nm. The crosslink may be separated when the polymers are irradiated at a wavelength of about 230 nm to about 300. The polymers may also photocleave when irradiated with light at a wavelength of about 230 nm to about 300.Type: GrantFiled: November 8, 2013Date of Patent: May 30, 2017Assignee: The University of AkronInventors: Abraham Joy, Murthy V. S. N. Maddipatla
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Publication number: 20150141255Abstract: A compound of general formula (I): in which X represents O, S, NH or an N-alkyl radical, R1 and R2, identical or different, each represent H or a C1-C10 hydrocarbon radical, R1 and R2 not both representing H, R3 represents a C1-C10 hydrocarbon radical, and R represents a phenyl radical monosubstituted or disubstituted by a substituent Y and, if applicable, a substituent Z, chosen from Cl, Br, I and CF3, or R represents a C?R4(R5) radical in which R4 represents an hydrocarbon radical and R5 represents a linear or branched, saturated or unsaturated, hydrocarbon radical, optionally substituted, a COR6 group or a CO2R6 group, where R6 represents a hydrogen atom or a linear or branched, saturated or unsaturated, hydrocarbon radical. This compound can be used for the treatment of higher plants for controlling their growth and architecture.Type: ApplicationFiled: May 23, 2013Publication date: May 21, 2015Inventors: Francois-Didier Boyer, Catherine Rameau, Jean-Paul Pillot, Vincent Servajean, Alexandre De Saint Germain, Jean-Marie Beau, Jean-Bernard Pouvreau, Guillaume Clave
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Publication number: 20150111888Abstract: The present invention provides a small compound targeting at TACC3. The present invention further provides a drug, particularly, an anticancer agent, comprising the small compound targeting at TACC3. A compound represented by the general formula (I) or a pharmaceutically acceptable salt, solvate, or ester derivative thereof binds to TACC3 and inhibits cell growth. Thus, these compounds can be used as drugs, particularly, anticancer agents.Type: ApplicationFiled: April 30, 2013Publication date: April 23, 2015Inventors: Ryoji Yao, Hiroyuki Osada, Yasumitsu Kondoh
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Patent number: 8993700Abstract: Polymers and copolymers of polymerizable fluorescent compounds of 7-hydroxycoumarin such as Ethyl-2-methacrylate Umbelliferone-4-acetate are provided. In addition, a sensor comprising this polymer notably for detecting and/or assaying nitrated and organophosphorus compounds, explosives, and toxic compounds is provided.Type: GrantFiled: September 24, 2010Date of Patent: March 31, 2015Assignee: Commissariat a l'Energie Atomique et aux Energies AlternativesInventors: Pierrick Buvat, Lucie Malosse, Alain Siove, Dominique Ades
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Publication number: 20150018566Abstract: The invention provides combretastatin A-4 like compounds that are modified to have enhanced tubulin binding activity and in some embodiments the ability to promote accumulation in the vasculature undergoing angiogenesis (homing activity). The compounds are based on the combretastatin A-4 skeletal structure having a tubulin-binding pharmacophore comprising two fused rings (A and B rings) in which the B ring is substituted with (a) an aromatic ring structure (C ring) and (b) a second substituent/functional group that comes off the B ring. The aromatic ring structure is typically a six membered ring phenolic or aniline structure, or may also be a fused ring structure such as a substituted or unsubstituted naphthalene.Type: ApplicationFiled: August 27, 2012Publication date: January 15, 2015Inventors: John Jarlath Walsh, Richard Shah, Emmet Martin McCormack, Gillian Joy Hudson, Martina White, Gary Daniel Stack, Brian William Moran, Adrian Coogan, Elaine Carmel Breen
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Publication number: 20150011512Abstract: The invention relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. The invention also provides pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. The invention also provides methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1 B1 and allelic variants thereof. The invention also provides a method for determining the efficacy of a compound of the invention in treating cancer.Type: ApplicationFiled: September 12, 2014Publication date: January 8, 2015Inventors: Steven Albert Everett, Saraj Ulhaq
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Publication number: 20140308696Abstract: Reaction-based fluorscent probes are provided which detect, for example, biologically important sulfane sulfur species (persulfide, polysulfide, and elemental sulfur) in, for example, complex and living systems. The probes are high in selectivity and sensitivity to sulfane sulfurs. Moreover, probes are suitable for bioimaging sulfane sulfurs in living cells.Type: ApplicationFiled: April 11, 2014Publication date: October 16, 2014Applicant: Washington State UniversityInventors: Ming Xian, Wei Chen
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Publication number: 20140296270Abstract: Small molecule inhibitors of Stat3 and their derivatives are disclosed. Also described are methods to inhibit cell growth by use of Stat3 inhibitors, and the use of Stat3 inhibitors for the prevention and/or treatment of cancer. Further, inhibitors of Stat3 that also do not inhibit Stat1 are described as well as their derivatives. Methods of screening additional compounds for Stat3 inhibition activity and/or non-inhibition of Stat1 activity are also described herein.Type: ApplicationFiled: April 15, 2014Publication date: October 2, 2014Applicant: Baylor College of MedicineInventors: David J. Tweardy, Xuejun Xu, Moses M. Kasembeli
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Publication number: 20140248218Abstract: Herein are provided, inter alia, compositions including boronic esters, which in the presence of H2O2, provide for the detection of ROS compounds such as endogenous H2O2 and methods of using the compositions to detect ROS compounds.Type: ApplicationFiled: February 7, 2014Publication date: September 4, 2014Applicant: The Regents of the University of CaliforniaInventors: Kevin B. Daniel, Seth M. Cohen, Jody L. Major Jourden
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Publication number: 20140242606Abstract: The present invention relates to a probe for iFRET and use thereof. Specifically, the present invention relates to a novel probe for iFRET, a method for preparing the probe for iFRET, a method for searching a target protein-specific binding site or a molecule having the binding site using the probe for iFRET, and a method for imaging the target protein using the probe for iFRET. The probe for iFRET according to the present invention utilizes an amino acid in a protein as a fluorescent donor, unlike the conventional FRET method. Therefore, only one fluorescent material is used, and its emission wavelength is distinct from the intrinsic fluorescence of the protein. Thus, high specificity and sensitivity are ensured, and the quantity, activity and mechanism of various proteins can be analyzed in an easy and accurate manner.Type: ApplicationFiled: June 25, 2012Publication date: August 28, 2014Applicant: KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGYInventors: Sang Jeon Chung, Ju Hwan Kim, Elena Ruchkina, Hyo Jin Kang
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Publication number: 20140235619Abstract: This invention relates to methods of screening for modulators of mammalian cell injury cause by TRPM7 gene and protein activity, compounds that modulate TRPM7 gene and protein activity and methods of treatment of mammalian cell injury using modulators of TRPM7 gene and protein activity.Type: ApplicationFiled: November 26, 2013Publication date: August 21, 2014Applicant: NONO INC.Inventors: Xiujun Sun, Michael Tymianski, David Garman
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Publication number: 20140221423Abstract: This invention relates to compounds that modulate TRPM7 protein activity and use of the same for treatment or prophylaxis of ischemia, cancer, pain or glaucoma.Type: ApplicationFiled: June 15, 2012Publication date: August 7, 2014Inventors: Xiujun Sun, Michael Tymianski
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Publication number: 20140212328Abstract: Embodiments herein generally relate to the use, devices, and compounds for generating singlet oxygen. In some embodiments, the singlet oxygen can be used for fluid purification and/or sterilization.Type: ApplicationFiled: July 24, 2012Publication date: July 31, 2014Applicant: EMPIRE TECHNOLOGY DEVELOPMENT LLCInventors: William Brenden Carlson, Gregory David Phelan
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Publication number: 20140148400Abstract: Derivatized coumarin-based pharmaceutical compositions and methods to use them are provided. The compositions are characterized in that they inhibit the activity of tumor-related CAIX and CAXII to a greater degree than they inhibit the activity of CAI and CAII. The compositions can be used to suppress tumor growth and/or suppress tumor metastases in a mammal.Type: ApplicationFiled: November 12, 2013Publication date: May 29, 2014Applicants: METASIGNAL THERAPEUTICS INC., CNRS-DIRE, UNIVERSITE MONTPELLIER 2 SCIENCES ET TECHNIQUESInventors: Claudiu Supuran, Shoukat Dedhar, Fabrizio Carta, Jean-Yves Winum, Paul C. McDonald
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Patent number: 8729279Abstract: Agents or pharmaceutical compositions for promoting osteoblast differentiation include purified auraptene or coumarin analogs thereof represented by the following formula 1: wherein R1 represents a hydrogen, a hydroxy, a methoxy, a methyl, an ethyl, a propyl, a carboxyl, a carboxymethyl, or a carboxyethyl; R2 represents a hydrogen, a hydroxy, a methoxy, a methyl, an ethyl, a propyl, a carboxyl, a carboxymethyl, a carboxyethyl or a coumarinyl; R3 represents a hydrogen, a hydroxy, a methoxy, a methyl, an ethyl, a propyl, a carboxyl, a carboxymethyl or a carboxyethyl; and R4 represents a hydrogen, a C1-C15 liner or branched alkyl, an alkenyl, an alkadienyl or an alkatrienyl.Type: GrantFiled: February 28, 2011Date of Patent: May 20, 2014Assignee: Erina Co., Inc.Inventors: Je-Tae Woo, Ayaka Hibino, Takayuki Yonezawa, Midori Asai, Toshiaki Teruya, Byung-Yoon Cha, Kazuo Nagai
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Patent number: 8729280Abstract: This invention discloses that the five crystal forms of XLF-III-43 can be used as crude drugs. The invention also relates to the preparation methods of the five crystal forms of XLF-III-43 as crude drugs, to the applications of the sterling of the five crystal forms of XLF-III-43 and mixed crystals in different proportions as medicinally active components to develop various kinds of medicines and compound medicines. In addition, this invention also relates to applying the crystal samples of XLF-III-43 as crude drugs to treat kidney dysfunction, cardiocerebral vessel diseases, hypertension, type II diabetic mellitus, complications of hypertension and diabetic mellitus, tumor, precancerosis, edema, and achieves therapeutic effects by enhancing blood drug levels resulted from effects of crystal forms in the processes of treating all kinds of diseases.Type: GrantFiled: November 28, 2009Date of Patent: May 20, 2014Assignee: Institute of Mataria Medica, Chinese Academy of Medical SciencesInventors: Yang Lv, Xiaoguang Chen, Ping Xie, Li Zhang, Cheng Wang
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Patent number: 8716496Abstract: Substituted sulfonated coumarins are expressed in the general formula (I), where: R1 is H, OH, or a substituted or unsubstituted, straight or branched C1-C6 alkyl radical, or —COR4, or —COOR4, or —CONHR4, R2 is H or a halogen, in particular fluorine, or a substituted or unsubstituted, straight or branched C1-C6 alkyl radical, or —COR4, or —COOR4, or —CONHR4, R1 and R2 being capable of together forming a ring, such as a substituted or unsubstituted aryl or furane, R3 is H or a halogen, in particular fluorine, or a substituted or unsubstituted, straight or branched C1-C6 alkyl radical, or —COR4, or —COOR4, or —CONHR4, where R4 is H, or a substituted or unsubstituted, straight or branched C1-C6 alkyl radical, or a substituted or unsubstituted aryl, and M is Na or K.Type: GrantFiled: September 16, 2011Date of Patent: May 6, 2014Assignees: Universite de StrasbourgInventors: Antoine Drevelle, Sylvain Ladame, Majdi Najah, Estelle Mayot
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Publication number: 20140099695Abstract: An object of the present invention is to enable simpler operation in real time and culture while removing unnecessary cells from cultured cells for purification in analyzing, fractionating, and culturing the cells alive and to analyze and fractionate desired cells from the cultured cells to increase the purity, recovery rate, and viability of the cells. The present invention employs a cell-adhesive photocontrollable base material, wherein light irradiation causes the bond dissociation of a photolabile group comprising a coumarinylmethyl skeleton to produce the separation of a cell-adhesive material to leave a non-cell-adhesive material. As a result, cell images can be detected and analyzed to obtain the positional information of desired cells. Based on the positional information thus obtained, the cells can be analyzed and fractionated alive.Type: ApplicationFiled: April 11, 2012Publication date: April 10, 2014Applicants: HITACHI HIGH-TECHNOLOGIES CORPORATION, TOHO UNIVERSITYInventors: Toshiaki Furuta, Akinobu Suzuki, Hisashi Sugiyama, Satoshi Ozawa, Hiroko Tada
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Publication number: 20140038856Abstract: The present invention provides methods and fluorescent compounds that facilitate detecting and labeling of a fusion protein by being capable of selectively binding to an affinity tag. The fluorescent compounds have the general formula A(B)n, wherein A is a fluorophore, B is a binding domain that is a charged chemical moiety, a protein or fragment thereof and n is an integer from 1-6 with the proviso that the protein or fragment thereof not be an antibody or generated from an antibody. The present invention provides specific fluorescent compounds and methods used to detect and label fusion proteins that contain a poly-histidine affinity tag. These compounds have the general formula A(L)m(B)n wherein A is a fluorophore, L is a linker, B is an acetic acid binding domain, m is an integer from 1 to 4 and n is an integer from 1 to 6.Type: ApplicationFiled: May 8, 2013Publication date: February 6, 2014Applicant: LIFE TECHNOLOGIES CORPORATIONInventors: Kyle GEE, Aleksey RUKAVISHNIKOV, Courtenay HART, Richard HAUGLAND, Wai-Yee LEUNG, Wayne PATTON, Zhenjun DIWU
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Patent number: 8592007Abstract: The present invention relates to polymerizable 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 stabilized) or PSA (polymer sustained alignment) type.Type: GrantFiled: September 29, 2009Date of Patent: November 26, 2013Assignee: Merck Patent GmbHInventors: Achim Goetz, Erdal Durmaz, Malgorzata Rillich, Andreas Taugerbeck
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Publication number: 20130308081Abstract: 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 sustained”) or PSA (“polymer sustained alignment”) type.Type: ApplicationFiled: December 27, 2011Publication date: November 21, 2013Applicant: Merck Patent GmbHInventors: Andreas Taugerbeck, Achim Goetz, Alexander Hahn, Martin Engel
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Publication number: 20130281507Abstract: The invention relates to compounds of formula (I): The invention likewise relates to a cosmetic method for depigmenting, lightening and/or whitening keratin materials, more particularly the skin, that utilizes these compoundsType: ApplicationFiled: November 23, 2011Publication date: October 24, 2013Applicant: L'OREALInventor: Xavier Marat
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Publication number: 20130281652Abstract: The present invention relates to compounds of formula I, which are functionalized phenolic compounds, and polymers formed from the same. Ar—[O—(X)p—R?]q??I Polymers formed from the functionalized phenolics are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.Type: ApplicationFiled: October 17, 2012Publication date: October 24, 2013Inventor: Rao S. Bezwada
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Publication number: 20130252268Abstract: The present invention relates to the visualization of acidic organelles based upon organelle enzyme activity. The organelle substrates of the invention are specific for enzyme activity of the organelle and label these organelles, such as lysosomes, rendering them visible and easily observed. Substrates of the present invention include substrates that produce a fluorescent signal. The fluorogenic acidic organelle enzyme substrates of this invention are designed to provide high fluorescence at low pH values and are derivatized to permit membrane permeation through both outer and organelle membranes of intact cells and can be used for staining cells at very low concentrations. They can be used for monitoring enzyme activity in cells at very low concentrations and are not toxic to living cells or tissues.Type: ApplicationFiled: May 14, 2013Publication date: September 26, 2013Applicant: Marker Gene Technologies, Inc.Inventors: John J. Naleway, Daniel J. Coleman
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Publication number: 20130203688Abstract: The present document describes a nutraceutical or cosmeceutical composition for the prophylaxis of an ailment comprising a therapeutically effective amount of a sugar plant syrup filtration residue in association with a pharmaceutically acceptable carrier. The present document also describes a nutraceutical or cosmeceutical composition for improving health condition of skin. The present document describes a method of producing a sugar plant syrup-derived product; wherein the improvement is characterized in the step of: collecting a sugar plant syrup residue during the production of sugar or syrup to produce a syrup-derived by-product.Type: ApplicationFiled: August 19, 2011Publication date: August 8, 2013Applicant: FÉDÉRATION DES PRODUCTEURS ACÉRI-COLES DU QUÉBECInventors: Julie Barbeau, Geneviève Béland
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Publication number: 20130183700Abstract: Substituted sulfonated coumarins are expressed in the general formula (I), where: R1 is H, OH, or a substituted or unsubstituted, straight or branched C1-C6 alkyl radical, or —COR4, or —COOR4, or —CONHR4, R2 is H or a halogen, in particular fluorine, or a substituted or unsubstituted, straight or branched C1-C6 alkyl radical, or —COR4, or —COOR4, or —CONHR4, R1 and R2 being capable of together forming a ring, such as a substituted or unsubstituted aryl or furane, R3 is H or a halogen, in particular fluorine, or a substituted or unsubstituted, straight or branched C1-C6 alkyl radical, or —COR4, or —COOR4, or —CONHR4, where R4 is H, or a substituted or unsubstituted, straight or branched C1-C6 alkyl radical, or a substituted or unsubstituted aryl, and M is Na or K.Type: ApplicationFiled: September 16, 2011Publication date: July 18, 2013Applicants: UNIVERSITE DE STRASBOURG, ETS J. SOUFFLETInventors: Antoine Drevelle, Sylvain Ladame, Majdi Najah, Estelle Mayot
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Publication number: 20130171664Abstract: This invention relates to compounds having the following structure: wherein Y is O, X is O, bond ? is absent and bond ? is present, or Y is H, X is CH, bond ? is present, and bond ? is absent; atom Z is a carbon and bonds ?, ? and ? are present, or atom Z is a nitrogen and bonds ?, ? and ? are absent, or atom Z is a nitrogen and bonds ? and ? are present and ? is absent. R1, R2, R3, R4, R5, and R6 are various substituents as described in the specification.Type: ApplicationFiled: January 28, 2011Publication date: July 4, 2013Inventors: Dalibor Sames, David Sulzer, Minhee Lee, Niko Gubernator
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Publication number: 20130102796Abstract: Agents or pharmaceutical compositions for promoting osteoblast differentiation include purified auraptene or coumarin analogs thereof represented by the following formula 1: wherein R1 represents a hydrogen, a hydroxy, a methoxy, a methyl, an ethyl, a propyl, a carboxyl, a carboxymethyl, or a carboxyethyl; R2 represents a hydrogen, a hydroxy, a methoxy, a methyl, an ethyl, a propyl, a carboxyl, a carboxymethyl, a carboxyethyl or a coumarinyl; R3 represents a hydrogen, a hydroxy, a methoxy, a methyl, an ethyl, a propyl, a carboxyl, a carboxymethyl or a carboxyethyl; and R4 represents a hydrogen, a C1-C15 liner or branched alkyl, an alkenyl, an alkadienyl or an alkatrienyl.Type: ApplicationFiled: February 28, 2011Publication date: April 25, 2013Applicant: ERINA CO., INC.Inventors: Je-Tae Woo, Ayaka Hibino, Takayuki Yonezawa, Midori Asai, Toshiaki Teruya, Byung-Yoon Cha, Kazuo Nagai
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Publication number: 20130079394Abstract: This invention relates to novel coumarin derivatives, formulations comprising same, and to methods of making and using these compounds and formulations, which are useful as repellents against insects and/or pests. The compounds also prevent illness and disease caused by insect/pest-borne vectors, and provide safer, more effective alternatives to existing repellents. This invention also relates to novel methods for modeling and/or predicting the repellency of unknown compounds.Type: ApplicationFiled: September 21, 2012Publication date: March 28, 2013Applicants: CNRS (CENTRE NATIONAL RECHERCHE SCIENTIFIQUE), MERIAL LIMITEDInventors: Jean Delaveau, Pierre Nicolas Stebe, Nathalie Marchand-Geneste
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Patent number: 8366963Abstract: A liquid crystal compound is to be obtained that has stability to heat, light and so forth, a high clearing point, a suitable optical anisotropy, a large negative dielectric anisotropy, and excellent compatibility with other liquid crystal compounds. A liquid crystal composition containing the compound is also to be obtained that has a low viscosity, a suitable optical anisotropy, a suitable negative dielectric anisotropy, a low threshold voltage, a high maximum temperature of a nematic phase (phase transition temperature from a nematic phase to an isotropic phase), and a low minimum temperature of a nematic phase. A compound having a hydrocoumarin skeleton is synthesized, and a liquid crystal composition containing the compound is produced.Type: GrantFiled: April 11, 2011Date of Patent: February 5, 2013Assignees: JNC Corporation, JNC Petrochemical CorporationInventors: Mayumi Goto, Teruyo Sugiura, Norikatsu Hattori, Kouki Sagou
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Publication number: 20120329832Abstract: This invention relates to novel coumarin derivative, formulations comprising same, and to methods of making and using these compounds and formulations, which are useful as repellents against insects and/or pests. The compounds also prevent illness and disease caused by insect/pest-borne vectors, and provide safer, more effective alternatives to existing repellents.Type: ApplicationFiled: June 21, 2012Publication date: December 27, 2012Inventors: Jean Delaveau, Emile Vialle, Marc Lemaire, Stephane Pellet-Rostaing, Bruno Andrioletti
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Publication number: 20120302748Abstract: The disclosure relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. Also provided are pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. Provided are methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1B1 and allelic variants thereof. Finally, provided is a method for determining the efficacy of a compound as described herein in treating cancer.Type: ApplicationFiled: February 28, 2012Publication date: November 29, 2012Applicant: THE UNIVERSITY COURT OF THE UNIVERSITY OF DUNDEEInventors: Steven Albert Everett, Saraj Ulhaq
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Publication number: 20120277297Abstract: The present invention relates to pharmaceutical composition comprising the naturally occurring compounds selected from (±) Marrnesin, Columbianetin, Dihydroxanthyletin and substituted coumarin derivatives of 7-allyloxy coumarin, 7-benzyloxy coumarin, 7 -methoxycoumarin, 7-acetyloxy coumarin, 4-methyl-7-hydroxy coumarin and 4-methyl-7-acetyloxy coumarin. The said compositions possess a high degree of acetylcholinesterase inhibitory (AChE) property.Type: ApplicationFiled: April 30, 2012Publication date: November 1, 2012Applicant: Council of Scientific and Industrial ResearchInventors: Janaswamy Madhusudana Rao, Bhimapaka China Raju, Pullela Venkata Srinivas, Katragadda Suresh Babu, Jhillu Singh Yadav, Kondapuram Vijaya Raghvan, Hemant Kumar Singh, Chandiswar Nath
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Patent number: 8278465Abstract: The present invention provides a compound represented by general formula (1) below or a pharmaceutically acceptable salt thereof: wherein: X is selected from heteroaryl etc., Y1 and Y2 are selected from —N? etc., Y3 and Y4 are selected from —CH? etc., A is selected from sulfamide etc., R1 is selected from hydrogen etc., and R2 is selected from C1-6 alkyl etc. The compound or salt has sufficiently high antitumor activity, and is useful in the treatment of cell proliferative disorders, particularly cancers. The present invention also provides a pharmaceutical composition containing the compound or salt as an active ingredient.Type: GrantFiled: December 3, 2010Date of Patent: October 2, 2012Assignees: Chugai Seiyaku Kabushiki Kaisha, Sakai ToshiyukiInventors: Hitoshi Iikura, Ikumi Hyoudoh, Toshihiro Aoki, Noriyuki Furuichi, Masayuki Matsushita, Fumio Watanabe, Sawako Ozawa, Masahiro Sakaitani, Pil-Su Ho, Yasushi Tomii, Kenji Takanashi, Naoki Harada
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Publication number: 20120214897Abstract: The present invention relates generally to molecularly imprinted polymers (MIPs). In particular, the present invention relates to reusable, ecologically friendly MIPs that can be produced in relatively large quantities, methods of producing the same, and methods of utilizing the same (e.g., to sequester and/or adsorb target compounds (e.g., mycotoxins)). Compositions and methods of the invention find use in a variety of applications including dietary therapeutic, prophylactic, food and beverage processing and manufacture, as well as research, quality control and traceability applications.Type: ApplicationFiled: April 9, 2012Publication date: August 23, 2012Applicant: ALLTECH, INC.Inventors: Alexandros Yiannikouris, Stefan Kwiatkowski, Manoj Bojappa Kudupoje, Clayton Matney
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Publication number: 20120196295Abstract: 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: ApplicationFiled: January 30, 2012Publication date: August 2, 2012Applicant: LIFE TECHNOLOGIES CORPORATIONInventor: Linda G. Lee
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Publication number: 20120190639Abstract: The invention relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. The invention also provides pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. The invention also provides methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1 B1 and allelic variants thereof. The invention also provides a method for determining the efficacy of a compound of the invention in treating cancer.Type: ApplicationFiled: April 30, 2010Publication date: July 26, 2012Applicant: UNIVERSITY COURT OF THE UNIVERSITY OF DUNDEEInventors: Steven Albert Everett, Saraj Ulhaq
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Publication number: 20120178172Abstract: Polymers and copolymers of polymerizable fluorescent compounds of 7-hydroxycoumarin such as Ethyl-2-methacrylate Umbelliferone-4-acetate are provided. In addition, a sensor comprising this polymer notably for detecting and/or assaying nitrated and organophosphorus compounds, explosives, and toxic compounds is provided.Type: ApplicationFiled: September 24, 2010Publication date: July 12, 2012Applicant: Commissariat a l'energie Atomique et aux energies alternativesInventors: Pierrick Buvat, Lucie Malosse, Alain Siove, Dominique Ades
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Patent number: 8071794Abstract: Reactive fluorescent dyes compositions and methods of using same are disclosed. Squaraine nucleus, Nile Red nucleus, benzodioxazole nucleus, coumarin nucleus or aza coumarin nucleus dyes are disclosed having thiol-reactive groups. Squaraine nucleus, Nile Red nucleus, benzodioxazole nucleus, coumarin nucleus or aza coumarin nucleus dyes are disclosed that exhibit a fluorescence emission of at least about 575 nm. Biosensors are disclosed having a binding protein and a squaraine nucleus, Nile Red nucleus, benzodioxazole nucleus, coumarin nucleus or aza coumarin nucleus.Type: GrantFiled: June 22, 2009Date of Patent: December 6, 2011Assignee: Becton, Dickinson and CompanyInventors: J. Bruce Pitner, Douglas B. Sherman, Joseph Thomas
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Publication number: 20110226610Abstract: Inventors have developed a chromophore (nitrodibenzylfuranyl, or NBDF) for ultra efficient uncaging of a caged substrate (e.g., an organic molecule such as, for example, an amino acid, a biological molecules, such as, for example, second messengers inside cells). Photolysis of a NBDF derivative of EGTA (i.e. caged calcium) is about 50 times more efficient than others calcium cages (the quantum yield of photolysis is 0.6 and the extinction coefficient is 18,400. NDBF-EGTA has a 2-photon cross section of about 0.3-0.6 GM).Type: ApplicationFiled: February 18, 2011Publication date: September 22, 2011Applicant: Philadelphia Health & Education Corporation d/b/a Drexel University College of MedicineInventors: Graham Ellis-Davies, Atsuya Momotake
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Publication number: 20110205482Abstract: 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) or PSA (polymer sustained alignment) type.Type: ApplicationFiled: September 29, 2009Publication date: August 25, 2011Applicant: MERCH PATENT GESELLSCHAFT MIT BESCHRANKTE HAFTUNGInventors: Achim Goetz, Erdal Durmaz, Malgorzata Rillich, Andreas Taugerbeck
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Publication number: 20110193021Abstract: A liquid crystal compound is to be obtained that has stability to heat, light and so forth, a high clearing point, a suitable optical anisotropy, a large negative dielectric anisotropy, and excellent compatibility with other liquid crystal compounds. A liquid crystal composition containing the compound is also to be obtained that has a low viscosity, a suitable optical anisotropy, a suitable negative dielectric anisotropy, a low threshold voltage, a high maximum temperature of a nematic phase (phase transition temperature from a nematic phase to an isotropic phase), and a low minimum temperature of a nematic phase. A compound having a hydrocoumarin skeleton is synthesized, and a liquid crystal composition containing the compound is produced.Type: ApplicationFiled: April 11, 2011Publication date: August 11, 2011Applicants: CHISSO CORPORATION, CHISSO PETROCHEMICAL CORPORATIONInventors: Mayumi GOTO, Teruyo SUGIURA, Norikatsu HATTORI, Kouki SAGOU
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Publication number: 20110196029Abstract: New pharmaceutical compositions extracted from Ferula assa-foetida are confirmed to effectively treat influenza A (H1N1) virus. The extraction method of the new pharmaceutical compositions mainly includes steps of (a) extracting F. assa-foetida with methanol to obtain a crude extract; (b) fractioning the crude extract with n-hexane-methanol to obtain a methanol extract; (c) fractioning the methanol extract with chloroform-water to obtain a chloroform extract; and (d) chromatographing the chloroform extract to obtain the pharmaceutical compositions, which can be further fractioned and chromatographed to obtain various sesquiterpene coumarins.Type: ApplicationFiled: August 18, 2010Publication date: August 11, 2011Applicant: KAOHSIUNG MEDICAL UNIVERSITYInventors: Yang-Chang Wu, Fang-Rong Chang, Lien-Chai Chiang
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COUMARIN COMPOUNDS FOR THE TREATMENT OF CARDIOVASCULAR DISEASES AND A PROCESS FOR PREPARING THE SAME
Publication number: 20110178168Abstract: The present invention relates to compounds of Formula (I): wherein—X and Y represent O, S, NR?; Rn represents alkyl, aryl, OR1, NH2, SR1, NR1R2. wherein R1, R2=H, alkyl, phenyl, aryl, OCOR3, SCOR3, NHCOR3, NR1COR3, etc. (wherein R3 represents alkyl, phenyl, aryl, heteroaryl); R? and R? represent H, alkyl, phenyl, substituted phenyl, phenyloxy, substituted phenyloxy, amino, mono substituted amino, disubstituted amino, aryl, heteroaryl, aryloxy, heteroaryloxy, alkoxy, thioalkyl, thioalkyloxy, halo and a process for preparing the same.Type: ApplicationFiled: June 23, 2009Publication date: July 21, 2011Inventors: Virender Singh Parmar, Hanumanthrao Guru Raj, Ashok Kumar Prasad, Subhash Chand Jain -
Publication number: 20110092700Abstract: The present invention provides a compound represented by general formula (1) below or a pharmaceutically acceptable salt thereof: wherein: X is selected from heteroaryl etc., Y1 and Y2 are selected from —N? etc., Y3 and Y4 are selected from —CH? etc., A is selected from sulfamide etc., R1 is selected from hydrogen etc., and R2 is selected from C1-6 alkyl etc. The compound or salt has sufficiently high antitumor activity, and is useful in the treatment of cell proliferative disorders, particularly cancers. The present invention also provides a pharmaceutical composition containing the compound or salt as an active ingredient.Type: ApplicationFiled: December 3, 2010Publication date: April 21, 2011Inventors: Hitoshi Iikura, Ikumi Hyoudoh, Toshihiro Aoki, Noriyuki Furuichi, Masayuki Matsushita, Fumio Watanabe, Sawako Ozawa, Masahiro Sakaitani, Pil-Su Ho, Yasushi Tomii, Kenji Takanashi, Naoki Harada
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Patent number: 7923562Abstract: Bifunctional linkers are provided that comprise a photocleavable moiety flanked by two different amine reactive moieties. In some embodiments the photocleavable moiety is a dimethoxynitrobenzyl moiety. In other embodiments the photocleavable moiety is 8-bromo-7-hydroxyquinoline. In other embodiments the photocleavable moiety is nitrodibenzofuran. In other embodiments the photocleavable moiety is 6-bromo-7-hydroxycoumarin-4-ylmethyl. The linkers find use in synthetic methods, including the generation of photocleavable oligonucleotides, e.g. caged morpholinos.Type: GrantFiled: June 16, 2009Date of Patent: April 12, 2011Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: James K. Chen, Surajit Sinha, Ilya Shestopalov, Xiaohu Ouyang
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Patent number: 7897792Abstract: The present invention provides a compound represented by general formula (1) below or a pharmaceutically acceptable salt thereof: wherein: X is selected from heteroaryl etc., Y1 and Y2 are selected from —N? etc., Y3 and Y4 are selected from —CH? etc., A is selected from sulfamide etc., R1 is selected from hydrogen etc., and R2 is selected from C1-6 alkyl etc. The compound or salt has sufficiently high antitumor activity, and is useful in the treatment of cell proliferative disorders, particularly cancers. The present invention also provides a pharmaceutical composition containing the compound or salt as an active ingredient.Type: GrantFiled: February 9, 2007Date of Patent: March 1, 2011Assignees: Chugai Seiyaku Kabushiki KaishaInventors: Hitoshi Iikura, Ikumi Hyoudoh, Toshihiro Aoki, Noriyuki Furuichi, Masayuki Matsushita, Fumio Watanabe, Sawako Ozawa, Masahiro Sakaitani, Pil-Su Ho, Yasushi Tomii, Kenji Takanashi, Naoki Harada
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Publication number: 20110046378Abstract: Disclosed here in are compounds and methods of diagnosing Alzheimer's Disease or a predisposition thereto in a mammal, the method comprising administering to the mammal a diagnostically effective amount of a radiolabeled compound, wherein the compound is selected from the group consisting of radiolabeled flavones, coumarins, carbazoles, quinolinones, chromenones, imidazoles and triazoles derivatives, allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing Alzheimer's DiseaseType: ApplicationFiled: February 17, 2009Publication date: February 24, 2011Applicant: SIEMENS MEDICAL SOLUTIONS USA, INC.Inventors: Hartmuth C. Kolb, Joseph C. Walsh, Qianwa Liang, Brian A. Duclos, Wei Zhang, Peter J.H. Scott, Kai Chen, Zhiyong Gao, Tieming Zhao, Vani P. Mocharla, Dhanalakshmi Kasi, Gang Chen, Eric Wang, Anjana Sinha, Chunfang Xia, Henry Clifton Padgett, Farhad Karimi
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Publication number: 20110015410Abstract: Disclosed herein are a pharmaceutical composition for inhibiting the proliferation of vascular smooth muscle cells, which contains scoparone as an active ingredient, the use of scoparone for inhibiting the proliferation of vascular smooth muscle cells and a method for inhibiting the proliferation of vascular smooth muscle cells using scoparone. According to the disclosed invention, it has been found that scoparone can inhibit the proliferation of vascular smooth muscle cells by increasing the activity of AMPK. Accordingly, scoparone can be advantageously used as an active ingredient' in drugs for inhibiting the proliferation of vascular smooth muscle cells, particularly preventing or treating blood vessel restenosis.Type: ApplicationFiled: September 10, 2008Publication date: January 20, 2011Applicant: Kyungpook National University Industry Academic Cooperation FoundationInventor: In Kyu Lee