Polycyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 549/220)
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Patent number: 11542288Abstract: The present application provides compounds and methods of treating viral infections, including viral infections caused by HIV or HTLV.Type: GrantFiled: May 28, 2021Date of Patent: January 3, 2023Assignee: University of MassachusettsInventors: Celia A. Schiffer, Akbar Ali, Nese Kurt-Yilmaz, Linah N. Rusere, Gordon J. Lockbaum, Mina Henes
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Patent number: 10981951Abstract: The present invention provides benzothiadiazine and chroman derivatives and particularly diazoxide and cromakalim derivatives for use in treating glaucoma, retinopathy, treating age related macular degeneration, treating, stabilizing and/or inhibiting blood and lymph vascularization, and reducing intraocular pressure by administering a pharmaceutically effective amount of a prodrug disposed in an ophthalmically acceptable carrier to the eye, wherein the prodrug specifically modulates a KATP channel to reduce an intraocular pressure.Type: GrantFiled: January 30, 2015Date of Patent: April 20, 2021Assignees: Mayo Foundation for Medical Education and Research, Regents of the University of MinnesotaInventors: Michael P. Fautsch, Peter Dosa, Michael A. Walters, Gunda I. Georg
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Patent number: 10787467Abstract: A polycyclic compound and an organic electroluminescence device, the polycyclic compound being represented by Formula 1:Type: GrantFiled: November 15, 2017Date of Patent: September 29, 2020Assignee: Samsung Display Co., Ltd.Inventor: Junta Fuchiwaki
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Patent number: 9816048Abstract: The present invention relates to a novel compound and its use as a fragrance material.Type: GrantFiled: July 27, 2016Date of Patent: November 14, 2017Assignee: INTERNATIONAL FLAVORS & FRAGRANCES INC.Inventors: Paul D Jones, Edward Mark Arruda, Anthony T Levorse, Jr.
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Patent number: 9029571Abstract: Provided are a novel 1,2-bis(dialkylphosphino)-4,5-(methylenedioxy)benzene derivative that forms a metal complex having particularly high asymmetry induction capacity and catalytic activity on ?-dehydroamino acids, a method for manufacturing the same, a metal complex having this 1,2-bis(dialkylphosphino)-4,5-(methylenedioxy)benzene derivative as a ligand, and an asymmetric hydrogenation method using this metal complex. A 1,2-bis(dialkylphosphino)-4,5-(methylenedioxy)benzene derivative represented by general formula (1). (In the formula, R1 and R2 represent an alkyl group having 1-10 carbon atoms, and R1 and R2 have different numbers of carbon atoms.Type: GrantFiled: June 21, 2012Date of Patent: May 12, 2015Assignee: Nippon Chemical Industrial Co., Ltd.Inventors: Zhenfeng Zhang, Tsuneo Imamoto, Ken Tamura
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Publication number: 20150093339Abstract: The present invention relates to the discovery that certain non-naturally occurring, non-peptide amide compounds and amide derivatives, such as oxalamides, ureas, and acrylamides, are useful flavor or taste modifiers, such as a flavoring or flavoring agents and flavor or taste enhancer, more particularly, savory (the “umami” taste of monosodium glutamate) or sweet taste modifiers,—savory or sweet flavoring agents and savory or sweet flavor enhancers, for food, beverages, and other comestible or orally administered medicinal products or compositions.Type: ApplicationFiled: October 8, 2014Publication date: April 2, 2015Inventors: Catherine TACHDJIAN, Andrew P. PATRON, Sara L. ADAMSKI-WERNER, Farid BAKIR, Qing CHEN, Vincent DARMOHUSODO, Stephen Terrence HOBSON, Xiaodong LI, Ming QI, Daniel H. ROGERS, Marketa RINNOVA, Guy SERVANT, Xiao-Qing TANG, Mark ZOLLER, David WALLACE, Amy XING, Klaus GUBERNATOR
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Publication number: 20150087620Abstract: The present invention provides a compound represented by the following formula (I): wherein each symbol is as described in the DESCRIPTION, which has a superior peripheral blood lymphocyte decreasing action, and is useful for the treatment or prophylaxis of autoimmune diseases; prophylaxis or suppression of resistance or acute rejection or chronic rejection of transplantation of organ or tissue; treatment or prophylaxis of graft-versus-host (GvH) disease due to bone marrow transplantation; or treatment or prophylaxis of allergic diseases.Type: ApplicationFiled: April 23, 2013Publication date: March 26, 2015Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Maiko Hamada, Kaoru Tashiro, Hiroshi Sakashita, Masatoshi Kiuchi, Shuzo Takeda, Kunitomo Adachi
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Patent number: 8981123Abstract: A compound represented by the following General Formula (1): where R1 represents a protective group for a hydroxyl group or a hydrogen atom, and R2 represents a methyl group or an ethyl group.Type: GrantFiled: June 11, 2014Date of Patent: March 17, 2015Assignee: Microbial Chemistry Research FoundationInventors: Masakatsu Shibasaki, Naoya Kumagai
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Publication number: 20150045529Abstract: The present invention relates to compounds suitable for use in electronic devices, and to electronic devices, especially organic electroluminescent devices, comprising these compounds.Type: ApplicationFiled: February 28, 2013Publication date: February 12, 2015Applicant: Merck Patent GmbHInventors: Philipp Stoessel, Elvira Montenegro, Arne Buesing, Teresa Mujica-Fernaud, Joachim Kaiser
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Publication number: 20150034927Abstract: A compound represented by the following formula (1-1):Type: ApplicationFiled: February 7, 2013Publication date: February 5, 2015Applicant: Idemitsu Kosan Co., Ltd.Inventors: Yuki Nakano, Hiroshi Yamamoto, Ryohei Hashimoto, Hideaki Nagashima
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Publication number: 20150025280Abstract: A catalytic system for reductive carbonylation of an alcohol that includes a rhodium complex, an iodide-containing catalyst promoter, and a supporting phosphorus-containing bidentate ligand for the rhodium complex containing at least one aromatic substituent covalently attached to at least one phosphorus of the supporting phosphorus-containing bidentate ligand in an ortho position with an alkoxy substituent or an aryloxy substituent.Type: ApplicationFiled: December 20, 2012Publication date: January 22, 2015Applicant: Dow Global Technologies LLCInventors: Thomas P. Clark, Heather A. Spinney, Jason MacDonald, Clark H. Cummins, Jerzy Klosin, John R. Briggs
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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: 20140378344Abstract: Fluorescent dyes useful for preparing fluorescent metal ion indicators, the fluorescent indicators themselves, and the use of the fluorescent indicators for the detection, discrimination and quantification of metal cations are provided.Type: ApplicationFiled: August 4, 2014Publication date: December 25, 2014Inventors: Zhenjun Diwu, Haitao Guo, Ruogu Peng, Qin Zhao, Jixiang Liu, Jinfang Liao
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Publication number: 20140371446Abstract: The disclosure is directed to: (a) phosphacycle ligands; (b) methods of using such phosphacycle ligands in bond forming reactions; and (c) methods of preparing phosphacycle ligands.Type: ApplicationFiled: August 25, 2014Publication date: December 18, 2014Applicant: AbbVie Inc.Inventors: Shashank Shekhar, Thaddeus S. Franczyk, David M. Barnes, Travis B. Dunn, Anthony R. Haight, Vincent S. Chan
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Patent number: 8912346Abstract: A phosphine ligand suitable for use in telomerizing butadiene comprises two phenyl groups and a xanthene moiety.Type: GrantFiled: May 14, 2009Date of Patent: December 16, 2014Assignee: Dow Global Technologies LLCInventors: Petrus Van Leeuwen, Mathieu Tschan, Eduardo Jose Garcia-Suarez, Zoraida Freixa, Henk Hagen
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Publication number: 20140296539Abstract: A compound represented by the following General Formula (1): where R1 represents a protective group for a hydroxyl group or a hydrogen atom, and R2 represents a methyl group or an ethyl group.Type: ApplicationFiled: June 11, 2014Publication date: October 2, 2014Inventors: Masakatsu SHIBASAKI, Naoya KUMAGAI
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Publication number: 20140288027Abstract: (?)-(S)-3-(3?-hydroxy)-butylphthalide (a compound shown by Formula I) and an ester formed of the same and an acid are proved by experiments to be applicable to treatment and prevention of cerebral ischemic diseases and have a sleep-improving function. The acid refers to a pharmaceutically acceptable inorganic or organic acid. The inorganic acid refers to nitric acid, sulfuric acid, or phosphoric acid. In addition to an acid radical, the organic acid at least comprises at least one of an amino group, a hydroxyl group, and a carboxyl group. None of the compound shown by Formula I and the ester thereof is water-soluble. An ester generated from the compound and the acid further react with an acid or a base to generate a salt which is water-soluble and is used to prepare injection preparation. The experiment proves that the salt does not stimulate vessels.Type: ApplicationFiled: September 26, 2012Publication date: September 25, 2014Inventors: Wei Wang, Yayao Zhou, Ya'nan Liu
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Patent number: 8841008Abstract: Compositions for use in lubricating thin film storage media are provided, as well as storage media formed using the compositions, the compositions including one or more central cores having a cyclic group, and a plurality of arms extending from the central cores, wherein each arm comprises phenol or piperonyl. Methods of preparing the compositions are also provided. Methods of preparing storage media that incorporate the compositions therein are further provided.Type: GrantFiled: February 28, 2011Date of Patent: September 23, 2014Assignee: Seagate Technology LLCInventors: Lei Li, Michael Joseph Stirniman, Jiping Yang
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Publication number: 20140213800Abstract: Provided are a novel 1,2-bis(dialkylphosphino)-4,5-(methylenedioxy)benzene derivative that forms a metal complex having particularly high asymmetry induction capacity and catalytic activity on ?-dehydroamino acids, a method for manufacturing the same, a metal complex having this 1,2-bis(dialkylphosphino)-4,5-(methylenedioxy)benzene derivative as a ligand, and an asymmetric hydrogenation method using this metal complex. A 1,2-bis(dialkylphosphino)-4,5-(methylenedioxy)benzene derivative represented by general formula (1). (In the formula, R1 and R2 represent an alkyl group having 1-10 carbon atoms, and R1 and R2 have different numbers of carbon atoms.Type: ApplicationFiled: June 21, 2012Publication date: July 31, 2014Applicant: NIPPON CHEMICAL INDUSTRIAL CO., LTD.Inventors: Zhenfeng Zhang, Tsuneo Imamoto, Ken Tamura
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Patent number: 8772487Abstract: The present disclosure is directed to fluorogenic schiff base-forming dyes capable of detecting analytes containing aldehyde and ketone groups. The dyes contain nucleophilic hydrazinyl appendages and are capable of binding and detecting analytes in situ.Type: GrantFiled: January 23, 2009Date of Patent: July 8, 2014Assignee: Life Technologies CorporationInventors: Aimei Chen, Kyle Gee, Hee Chol Kang
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Patent number: 8765977Abstract: A method of diagnostic imaging is disclosed comprising administering a medical formulation to a subject, the formulation comprising a contrast enhancement agent having structure I and salts thereof wherein R1 is independently at each occurrence a hydroxy group, a C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, and b is 0-4; R2-R7 are independently at each occurrence hydrogen, a C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, with the proviso that at least one of R1-R7 is a hydroxy group or a C1-C3 hydroxyalkyl group; and wherein Q is one or more charge balancing counterions; and one or more pharmaceutically acceptable carriers and excipients. The subject is subjected to a diagnostic imaging technique such as magnetic resonance imaging. The technique may be used in a variety of diagnostic imaging regimes, such as imaging of circulatory systems, genitourinary systems, hepatobiliary systems, central nervous systems, tumors, and abscesses among others.Type: GrantFiled: March 31, 2011Date of Patent: July 1, 2014Assignee: General Electric CompanyInventors: Brian James Grimmond, Michael James Rishel, Rong Zhang, Jeannette Christine Roberts
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Publication number: 20140171642Abstract: The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerisation inhibitors.Type: ApplicationFiled: February 19, 2014Publication date: June 19, 2014Applicant: BIONOMICS LIMITEDInventors: JASON HUGH CHAPLIN, GURMIT SINGH GILL, DAMIAN WOJCIECH GROBELNY, BERNARD LUKE FLYNN, GABRIEL KREMMIDIOTIS
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Patent number: 8716267Abstract: The present invention relates to novel bicyclic methyl amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: GrantFiled: April 13, 2012Date of Patent: May 6, 2014Assignee: Allergan, Inc.Inventors: Janet A. Takeuchi, Ling Li, Wha Bin Im
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Publication number: 20140100194Abstract: The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated disorders. Pharmaceutical and veterinary compositions and methods of treating pain and various other disease states or conditions using compounds of the invention are also described.Type: ApplicationFiled: December 5, 2013Publication date: April 10, 2014Applicant: Janssen Pharmaceutica, NVInventors: Raymond W Colburn, Scott L. Dax, Christopher M. Flores, Jay M. Matthews
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Publication number: 20140086843Abstract: The present invention relates to a bifunctional hydroxy-bisphosphonic acid derivative of formula (I) below: or a pharmaceutically-acceptable salt thereof, a method for producing the same, pharmaceutical compositions containing the same, and the use thereof as a medicament, as well as a compound of formula (II) below: or a pharmaceutically-acceptable salt thereof, and the use thereof for producing a vectorized molecule of therapeutic or diagnostic purpose.Type: ApplicationFiled: March 28, 2012Publication date: March 27, 2014Applicant: ATLANTHERAInventors: Maxim Egorov, Jean-Yves Goujon, Ronan Le Bot
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Patent number: 8674119Abstract: The present invention relates to the scaled-up synthesis of biologically active compounds which display useful therapeutic activity in treating proliferative disorders. In particular the invention relates to process methods for the kilogram scale synthesis of a particular class of substituted benzofuran tubulin polymerisation inhibitors.Type: GrantFiled: July 15, 2011Date of Patent: March 18, 2014Assignee: Bionomics LimitedInventor: Bernard Luke Flynn
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Patent number: 8637685Abstract: The invention provides fluorescent schweinfurthin analogs of formula (I) which are useful as probes and for the treatment of cancer and other diseases.Type: GrantFiled: June 25, 2009Date of Patent: January 28, 2014Assignee: University of Iowa Research FoundationInventors: David F. Wiemer, Jeffrey D. Neighbors, Raymond J. Hohl, Craig Kuder
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Publication number: 20140011773Abstract: A compound of formula (I), or a pharmaceutically acceptable salt thereof: The compound is used in pharmaceutical compositions and in a method of treatment of a disease or medical condition which benefits from inhibition of gap junction activity by administering to a subject suffering from such disease or condition.Type: ApplicationFiled: July 3, 2013Publication date: January 9, 2014Inventors: Edward Savory, Martyn Pritchard, Mike Ashwood
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Publication number: 20130345176Abstract: The present invention discloses esters of 4,9-dihydroxy-naphtho[2,3-b]furans and methods of making and using the same. The present invention also discloses conversion of the esters into therapeutically active 4,9-dihydroxy-naphtho[2,3-b]furans in vivo. The present invention furthermore discloses pharmaceutical compositions comprising the esters of 4,9-dihydroxy-naphtho[2,3-b]furans for the treatment of various indications including proliferative diseases.Type: ApplicationFiled: March 4, 2011Publication date: December 26, 2013Applicant: Zhoushan Haizhongzhou Xinsheng Pharmaceuticals Co., Ltd.Inventors: Zhiwei Jiang, Aijin Wang, Hongwei Hu, Jiali Xu, Yuesong Hu, Xian Li, Yan Ye, Jie Wang, Qinglong Li
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Publication number: 20130323770Abstract: The invention relates to novel substrates and methods for staining live stem cells. The stain may be used to identify induced pluripotent stem cell colonies during the process of somatic cell reprogramming.Type: ApplicationFiled: February 14, 2012Publication date: December 5, 2013Applicant: LIFE TECHNOLOGIES CORPORATIONInventors: Uma Lakshmipathy, Upinder Singh, Scott Grecian, Rene Quintanilla, Kyle Gee, Mahendra Rao
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Patent number: 8598371Abstract: Compounds of the formula (I) in the form of a mixture of predominantly one diastereomer or in the form of pure diastereomers, Z1-Q-P*R0R1??(I), wherein: Z1 is a C-bonded, secondary phosphine group of the formula —P(R)2, wherein R is a hydrocarbon radical or O-atom(s)-containing heterohydrocarbon radical having 1 to 18 carbon atoms and optionally substituted by C1-C6-alkyl, trifluoromethyl, C1-C6-alkoxy, trifluoromethoxy, (C1-C4-alkyl)2amino, (C6H5)3Si, (C1-C12-alkyl)3Si or halogen; Q is selected from the group consisting of: (i) an optionally substituted achiral aromatic group, wherein the achiral aromatic group is bonded directly to Z1 through a carbon atom of the achiral aromatic group and bonded directly to P*R0R1 through a carbon atom of the achiral aromatic group, and (ii) an optionally substituted C1-C4-alkylene group; P* is a chiral phosphorus atom; R0 is methyl; and R1 is a C-bonded optically enriched or optically pure chiral, mono- or polycyclic, nonaromatic hydrocarbon ring; and preparatType: GrantFiled: April 26, 2013Date of Patent: December 3, 2013Assignee: Solvias AGInventors: Benoit Pugin, Matthias Lotz, Heidi Landert, Adrian Wyss, Raphael Aardoom, Bjorn Gschwend, Andreas Pfaltz, Felix Spindler
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Patent number: 8598145Abstract: This invention relates to anti-cancer compounds and to methods for treating or preventing cancer. In one aspect the invention concerns mitochondrially delivered pro-oxidant anti-cancer compounds that generate reactive oxygen species and induce apoptosis of cancerous cells. The delivery moiety can be a lipophilic cation and the pro-oxidant vitamin E analogue, such as ?-tocopheryl succinate, ?-tocopheryl maleate, ?-tocopheryl maleyl amide, or 2,5,7,8-tetramethyl-2R-(4R,8R,12-trimethyltridecyl)-chroman-6-yloxyacetic acid (?-tocopheryloxyacetic acid).Type: GrantFiled: March 16, 2009Date of Patent: December 3, 2013Inventors: Stephen John Ralph, Jiri Neuzil
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Patent number: 8592611Abstract: The disclosure provides novel trioxane sulfur dimers having Formula I: methods for their preparation, pharmaceutical compositions containing these compounds, and methods for treating cancer, proliferative disorders, and/or malaria using these compounds and/or compositions.Type: GrantFiled: July 17, 2009Date of Patent: November 26, 2013Assignee: The Johns Hopkins UniversityInventors: Gary H. Posner, Andrew S. Rosenthal
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Publication number: 20130288911Abstract: The present disclosure is directed to fluorogenic schiff base-forming dyes capable of detecting analytes containing aldehyde and ketone groups. The dyes contain nucleophilic hydrazinyl appendages and are capable of binding and detecting analytes in situ.Type: ApplicationFiled: March 11, 2013Publication date: October 31, 2013Inventor: LIFE TECHNOLOGIES CORPORATION
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Patent number: 8569515Abstract: The trivalent phosphorous atom of a compound is reacted with a reagent in such a manner that a stable phosphate mimetic or a specifier is formed. Phosphoramidites with a phosphorous atom containing at least one hydroxyl residue which is provided with a protective group are reacted for this purpose with a free hydroxyl group: In the first synthesis cycle the hydroxyl group is linked to a solid support via a cleavable or non-cleavable linker. In further synthesis cycles the hydroxyl group is created by cleavage of the protective group from the growing oligomer. This results in formation of a phosphorous acid triester which is reacted with azides. By selecting suitable monomers for the synthesis which have a defined stereoconformation compounds of Formula 1 are produced in a stereocontrolled manner.Type: GrantFiled: May 3, 2011Date of Patent: October 29, 2013Assignee: Roche Diagnostics Operations, Inc.Inventors: Dieter Heindl, Dirk Kessler, Angelika Roesler, Christoph Seidel, Wilma Thuer
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Publication number: 20130274212Abstract: The present invention relates to sesterterpene compounds, to the precursors thereof that are hydrolysable in a living body, or to the pharmaceutically acceptable salts thereof, and also relates to the prevention and treatment efficacy of the sesterterpene compounds with respect to non-insulin dependent diabetes mellitus, diabetic complications (renal failure and foot ulcers caused by diabetes), alcoholic, non-alcoholic, and viral fatty liver diseases, obesity, hyperlipidemia, atherosclerosis, cardiovascular diseases such as atherosclerotic stroke, and cerebropathies (Parkinsonism, schizophrenia and Alzheimer's disease). In addition, the present invention relates to compositions for functional foods, functional beverages, functional cosmetics, and functional feed.Type: ApplicationFiled: September 7, 2011Publication date: October 17, 2013Applicant: SNU R&DB FOUNDATIONInventors: Heon Joong Kang, Dong Hwan Won, In Ho Yang, Eun Oh Kim, Jung Ah Kim, Awadut Gajendra Giri, Venkat Reddy Mallepally
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Publication number: 20130267714Abstract: Compounds of the formula (I) in the form of a mixture of predominantly one diastereomer or in the form of pure diastereomers, Z1-Q-P*R0R1??(I), wherein: Z1 is a C-bonded, secondary phosphine group of the formula —P(R)2, wherein R is a hydrocarbon radical or O-atom(s)-containing heterohydrocarbon radical having 1 to 18 carbon atoms and optionally substituted by C1-C6-alkyl, trifluoromethyl, C1-C6-alkoxy, trifluoromethoxy, (C1-C4-alkyl)2-amino, (C6H5)3Si, (C1-C12-alkyl)3Si or halogen; Q is selected from the group consisting of: (i) an optionally substituted achiral aromatic group, wherein the achiral aromatic group is bonded directly to Z1 through a carbon atom of the achiral aromatic group and bonded directly to P*R0R1 through a carbon atom of the achiral aromatic group, and (ii) an optionally substituted C1-C4-alkylene group; P* is a chiral phosphorus atom; R0 is methyl; and R1 is a C-bonded optically enriched or optically pure chiral, mono- or polycyclic, nonaromatic hydrocarbon ring; and preparType: ApplicationFiled: April 26, 2013Publication date: October 10, 2013Inventors: Benoit PUGIN, Matthias LOTZ, Heidi LANDERT, Adrian WYSS, Raphael AARDOOM, Bjorn GSCHWEND, Andreas PFALTZ, Felix SPINDLER
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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: 20130211102Abstract: The present invention relates to the scaled-up synthesis of biologically active compounds which display useful therapeutic activity in treating proliferative disorders. In particular the invention relates to process methods for the kilogram scale synthesis of a particular class of substituted benzofuran tubulin polymerisation inhibitors.Type: ApplicationFiled: July 15, 2011Publication date: August 15, 2013Applicant: BIONOMICS LIMITEDInventor: Bernard Luke Flynn
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Patent number: 8507552Abstract: The invention provides compounds of formula (I): or a salt thereof. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods using the compounds of formula I.Type: GrantFiled: May 7, 2010Date of Patent: August 13, 2013Assignee: Regents of the University of MinnesotaInventors: Ingrid Gunda Georg, Satish Prakash Patil, Ashok K. Saluja, Rohit Chugh, Selwyn M. Vickers
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Publication number: 20130172295Abstract: A process for the synthesis of bisfuran intermediates useful for preparing antiviral HIV protease inhibitor compounds is hereby disclosedType: ApplicationFiled: February 27, 2013Publication date: July 4, 2013Applicant: Gilead Sciences, Inc.Inventor: Gilead Sciences, Inc.
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Publication number: 20130137755Abstract: The present invention relates to a novel delivery system for delivering therapeutic agents into living cells, and more particularly, to novel chemical moieties that are designed capable of targeting and/or penetrating cells or other targets of interest and further capable of binding therapeutic agents to be delivered to these cells, and to delivery systems containing same.Type: ApplicationFiled: October 22, 2012Publication date: May 30, 2013Applicant: Segev Laboratories LimitedInventor: Segev Laboratories Limited
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Publication number: 20130130289Abstract: The present invention provides compounds and methods for assaying redox state of metabolically active cells and methods for assaying enzyme activity and/or metabolite level by coupling to redox defining co-factor NAD(P)/NAD(P)H measurement.Type: ApplicationFiled: August 31, 2012Publication date: May 23, 2013Applicant: PROMEGA CORPORATIONInventors: Helene A. BENINK, James J. CALI, Sarah DUELLMAN, Dieter KLAUBERT, Donna LEIPPE, Martha O'BRIEN, John SHULTZ, Jolanta VIDUGIRIENE, Wenhui ZHOU, Mary SOBOL
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Patent number: 8383609Abstract: A new anticancer compounds of formula (1) Drugs and pharmaceutical compositions to be used in human or veterinary medicine, which include at least one compound of formula (1).Type: GrantFiled: July 7, 2008Date of Patent: February 26, 2013Assignee: Centre National de la Recherche ScientifiqueInventors: Jean-Luc Pirat, David Virieux, Ludovic Clarion, Jean-Noël Volle, Norbert Bakalara, Marcel Mersel, Jerôme Montbrun, Henri-Jean Cristau
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Publication number: 20130018195Abstract: The preparation and use of fluorescent cell markers of the structure F—S1—S2-L is described where F is a fluorophore, S1—S2 is a spacer linking F to L, and L is a diacyl lipid.Type: ApplicationFiled: January 20, 2012Publication date: January 17, 2013Applicant: Kode Biotech LimitedInventors: Elena Korchagina, Nicolai Bovin, Stephen Henry
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Publication number: 20130012725Abstract: A process for the conversion of a tertiary phosphine oxide to the corresponding tertiary phosphine includes reacting the tertiary phosphine oxide with a reducing tertiary phosphine, in the presence of a catalyst that catalyzes the conversion.Type: ApplicationFiled: March 30, 2011Publication date: January 10, 2013Applicant: CHROMAFORA ABInventors: Gaston Laven, Martin Kullberg
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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: 20120301880Abstract: Alkyl amine dyes, oligonucleotide probes prepared from the alkyl amine dyes, phosphoramidites and solid supports prepared from the alkyl amine dyes, and methods of labeling biological agents using the alkyl amine dyes.Type: ApplicationFiled: May 29, 2012Publication date: November 29, 2012Applicant: BLOOD CELL STORAGE, INC.Inventors: Michael W. Reed, Robert O. Dempcy
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Publication number: 20120289484Abstract: Described herein are ?9-THC prodrugs, methods of making ?9-THC prodrugs, formulations comprising ?9-THC prodrugs and methods of using ?9-THC. One embodiment described herein relates to the transdermal administration of a ?9-THC prodrug for treating and preventing diseases and/or disorders.Type: ApplicationFiled: July 23, 2012Publication date: November 15, 2012Inventors: Audra Lynn STINCHCOMB, Miroslaw Jerzy GOLINSKI, Dana Carmel HAMMELL, Jeffrey Lynn HOWARD