Additional Acyclic Chalcogen Bonded Directly To The Lactone Ring Patents (Class 549/285)
  • Patent number: 11845735
    Abstract: A method for synthesizing (RS)-Warfarin comprising preparing a liquid mixture, wherein the liquid mixture comprises trihexyltetradecylphosphonium bromide, methyl salicylate, acetyl chloride, benzaldehyde, and acetone. The method may further comprise incubating the liquid mixture at a temperature between 20° C. and 30° C. for a time duration between 26 and 34 minutes, and forming (RS)-Warfarin by adding water to the incubated liquid mixture with a volume ratio (water:incubated liquid mixture) between 1:1 and 1.5:1.
    Type: Grant
    Filed: October 24, 2022
    Date of Patent: December 19, 2023
    Inventor: Nasim Batooie
  • Patent number: 10131646
    Abstract: Provided are: an aromatic sulfonium salt compound which exhibits low corrosion to a substrate and excellent photolithographic characteristics and is thus useful as a photoacid generator and as a cationic polymerization agent; and a photoacid generator, a resist composition, a cationic polymerization initiator and a cationically polymerizable agent composition, which include the aromatic sulfonium salt compound. The aromatic sulfonium salt compound is represented by the following Formula (I): (wherein, R1 to R10 each independently represent a hydrogen atom, a halogen atom, a hydroxyl group, a nitro group, a cyano group, an alkyl group having 1 to 18 carbon atoms which is optionally substituted, or the like; R11 to R15 each independently represent a hydrogen atom, an alkoxy group having 1 to 18 carbon atoms which is optionally substituted, or the like; at least one of R11 to R15 is not a hydrogen atom; and X1? represents a monovalent organic sulfonate anion).
    Type: Grant
    Filed: March 18, 2015
    Date of Patent: November 20, 2018
    Assignee: ADEKA CORPORATION
    Inventors: Satoshi Yanagisawa, Hitomi Toda, Koichi Shigeno, Masaki Kimura
  • Publication number: 20150025129
    Abstract: Certain embodiments of the invention include compositions comprising a compound of Formula (I), and salts, isomers, and derivatives thereof. Pharmaceutical compositions of some embodiments of the present invention comprise a compound of Formula (I), and salts, isomers, and derivatives thereof. Other embodiments of this invention include methods for treating disease (e.g., cancer) and methods for administering a compound of Formula (I), and salts, isomers, and derivatives thereof.
    Type: Application
    Filed: November 16, 2012
    Publication date: January 22, 2015
    Inventors: Gerald B. Hammond, Zhuang Jin, Paula J. Bates, Elsa Merit Reyes-Reyes, Abraham Vaisberg
  • Publication number: 20140343137
    Abstract: The polymorphic forms of the compound of Formula I, the preparation thereof including the preparation of the intermediates, the pharmaceutical compositions thereof and the uses of a polymorph above in the manufacture of medicaments for treating a disease, a disorder or a condition are disclosed.
    Type: Application
    Filed: July 30, 2012
    Publication date: November 20, 2014
    Applicants: BEIJING BETTA PHARMACEUTICALS CO., LTD.
    Inventors: Xinshan Kang, Wei Long, Fei Wang, Cunbo Ma, Liufeng Zhou, Yunyan Hu, Yanping Wang, Hong Cao, Yinxiang Wang, Fenlai Tan
  • Publication number: 20140213643
    Abstract: The present invention relates to novel nanoencapsulated compositions, methods for making such compositions, and methods of repelling insects and other arthropod pests away from animals, including humans. The present invention has particular, though not sole, application to repelling insects including flies and mosquitoes. The inventive compositions may be used to repel arthropods from animals, humans, plants, soil, or building structures. The formulations also prevent illness and disease caused by insect/pest-borne vectors, and provide safer, more effective alternatives to existing repellents.
    Type: Application
    Filed: January 28, 2013
    Publication date: July 31, 2014
    Applicant: MERIAL LIMITED
    Inventors: Jean Delaveau, Audrey Minost, Hatem FESSI, Marie-Alexandrine BOLZINGER, Abdelhamid Elaissari
  • Publication number: 20140187625
    Abstract: A novel compound obtained from molecules of the coumarin family, which exhibits rodenticidal activity. Also, compositions which incorporate such compounds and the use thereof for combating rodent pests.
    Type: Application
    Filed: July 19, 2012
    Publication date: July 3, 2014
    Applicant: LIPHATECH
    Inventors: Herve Caruel, Adrien Montagut Romans, Etienne Benoit, Stephane Besse, Philippe Berney, Virginie Lattard
  • Patent number: 8742138
    Abstract: This invention relates to new compounds that can serve as hypoxia mimetics. This invention also relates to methods of increasing HIF levels or activity in a subject or treating a condition associated with HIF levels or activity in a subject by administering to the subject at least one of these compounds.
    Type: Grant
    Filed: July 14, 2010
    Date of Patent: June 3, 2014
    Assignees: Betta Pharmaceuticals Co., Ltd.
    Inventors: Xinshan Kang, Wei Long, Cunbo Ma, Yanping Wang, Hong Cao, Yinxiang Wang, Fenlai Tan, Yunyan Hu
  • Patent number: 8598387
    Abstract: Disclosed herein is novel process for preparation of atovaquone, which process includes reacting 1H-2-benzopyran-1,4(3H)-dione with 4-(4-chlorophenyl)cyclohexanecarbaldehyde. The invention further discloses novel intermediates useful in the preparation of atovaquone.
    Type: Grant
    Filed: December 13, 2011
    Date of Patent: December 3, 2013
    Assignee: Glaxo Group Limited
    Inventors: Andrew Neil Dwyer, Andrew Gordon, Michael Urquhart
  • Publication number: 20130281652
    Abstract: 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: Application
    Filed: October 17, 2012
    Publication date: October 24, 2013
    Inventor: Rao S. Bezwada
  • Publication number: 20130267717
    Abstract: Disclosed herein is novel process for preparation of atovaquone, which process includes reacting 1H-2-benzopyran-1,4(3H)-dione with 4-(4-chlorophenyl)cyclohexanecarbaldehyde. The invention further discloses novel intermediates useful in the preparation of atovaquone.
    Type: Application
    Filed: December 13, 2011
    Publication date: October 10, 2013
    Applicant: GLAXO GROUP LIMITED
    Inventors: Andrew Neil Dwyer, Andrew Gordon, Michael Urquhart
  • Patent number: 8497361
    Abstract: An aminocoumarin conjugated to a fluorescent label through a secondary amine, is operative as a fluorescent polarization probe of the DNA gyrase B or topoisomerase IV E subunit. The probe is used for detecting topoisomerase inhibitor binding by fluorescence polarization, particularly in a high-through put topoisomerase inhibitor assay.
    Type: Grant
    Filed: August 22, 2011
    Date of Patent: July 30, 2013
    Assignee: SRI International
    Inventors: Peter Madrid, Bryan Glaser, Jeremiah Malerich
  • Patent number: 8450506
    Abstract: The present invention relates to compounds of formula (I), where R1 and R2, which may be identical or different, are selected from the group comprising H, CnH2n-1, a linear or branched alkyl group having 1 to 6 carbons, or together form an aromatic or aliphatic ring with 5 or 6 atoms; R3 is —CO—CH3, —NHOH, —OH, or —OR6 where R6 is a linear or branched alkyl group having 1 to 6 carbon atoms; R4 is H, linear or branched alkyl group having from 1 to 6 atoms, phenyl, benzyl, —CF3 or CF2CF3, vinyl or allyl; R5, R7, R8 are hydrogen atoms; or R3 and R4, R4 and R5, or R7 and R8 together form a ring, fused to the benzene, aromatic or aliphatic ring with 5 or 6 atoms comprising from 1 to 2 heteroatoms selected independently from the group comprising N, O, and use thereof in the medical field.
    Type: Grant
    Filed: February 15, 2012
    Date of Patent: May 28, 2013
    Assignee: Nogra Pharma Limited
    Inventors: Giancarlo Naccari, Sergio Baroni
  • Patent number: 8445531
    Abstract: A rodenticidal compound of formula (I): as well as the isomers thereof, in particular enantiomers, diastereoisomers, tautomers or mixtures of isomers in all proportions, where: R1 is: H or (II) or (III) with X?H, OH, Cl, Br, F or N02; R2 is: (IV) or (V) or (VI) with X?H, OH, Cl, Br, F or NO2; R3 is: O or S or (VII) with X?H, OH, Cl, Br, F or N02. Compositions containing such compounds as well as a method of use thereof in controlling harmful rodents are also described.
    Type: Grant
    Filed: February 16, 2011
    Date of Patent: May 21, 2013
    Assignee: Liphatech
    Inventors: Romain Lasseur, Etienne Benoit, Philippe Berny, Stephane Besse
  • Publication number: 20130079394
    Abstract: 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: Application
    Filed: September 21, 2012
    Publication date: March 28, 2013
    Applicants: CNRS (CENTRE NATIONAL RECHERCHE SCIENTIFIQUE), MERIAL LIMITED
    Inventors: Jean Delaveau, Pierre Nicolas Stebe, Nathalie Marchand-Geneste
  • Publication number: 20130039854
    Abstract: A mechanism of monoamine oxidases (MAOs) driven epithelium-to-mesenchymal transition (EMT) is disclosed. Also disclosed are methods for treating cancer by inhibiting or suppressing MAOs in cancer cells. Novel MAOs inhibitors, such as small molecules, siRNA, shRNA, antisense oligonucleotides, aptamers, decoys, and pharmaceutical compositions useful for treating cancer by disrupting the workings of MAOs are provided. In particular, a class of conjugates formed by covalently conjugating near infrared dye 783, IR-780, and MHI-148 to a MAO inhibitor, such as clorgyline, with and without encapsulation it in a nanoparticle is provided. Other aspects of the invention include methods for forming the nano-conjugates, method for monitoring treatment progress in a cancer patient by monitoring the changes in MAO activity, methods for screening patients who are at risk of cancer or differentiating different forms of cancer by assaying the level and location of MAO activity.
    Type: Application
    Filed: July 26, 2012
    Publication date: February 14, 2013
    Applicant: UNIVERSITY OF SOUTHERN CALIFORNIA
    Inventors: Jean C. SHIH, Leland CHUNG, Haiyen E. ZHAU, Boyang Jason WU, Bogdan Z. OLENYUK
  • Publication number: 20120329832
    Abstract: 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: Application
    Filed: June 21, 2012
    Publication date: December 27, 2012
    Inventors: Jean Delaveau, Emile Vialle, Marc Lemaire, Stephane Pellet-Rostaing, Bruno Andrioletti
  • Publication number: 20120316231
    Abstract: A rodenticidal compound of formula (I): as well as the isomers thereof, in particular enantiomers, diastereoisomers, tautomers or mixtures of isomers in all proportions, where: R1 is: H or (II) or (III) with X?H, OH, Cl, Br, F or N02; R2 is: (IV) or (V) or (VI) with X?H, OH, Cl, Br, F or NO2; R3 is: O or S or (VII) with X?H, OH, Cl, Br, F or N02. Compositions containing such compounds as well as a method of use thereof in controlling harmful rodents are also described.
    Type: Application
    Filed: February 16, 2011
    Publication date: December 13, 2012
    Applicant: LIPHATECH
    Inventors: Romain Lasseur, Etienne Benoit, Philippe Berny, Stephane Besse
  • Patent number: 8324405
    Abstract: The present invention relates to novel compounds of formula (I), methods, and compositions capable of decreasing HIF hydroxylase activity, thereby increasing the stability and/or activity of hypoxia inducible factor (HIF).
    Type: Grant
    Filed: February 5, 2009
    Date of Patent: December 4, 2012
    Assignee: FibroGen, Inc.
    Inventors: Wen-bin Ho, Lee Wright, Shaojiang Deng, Eric Turtle, Lee A. Flippin
  • Publication number: 20120172399
    Abstract: This invention relates to new compounds that can serve as hypoxia mimetics. This invention also relates to methods of increasing HIF levels or activity in a subject or treating a condition associated with HIF levels or activity in a subject by administering to the subject at least one of these compounds.
    Type: Application
    Filed: July 14, 2010
    Publication date: July 5, 2012
    Inventors: Xinshan Kang, Wei Long, Cunbo Ma, Yanping Wang, Hong Cao, Yinxiang Wang, Fenlai Tan, Yunyan Hu
  • Patent number: 8138357
    Abstract: Therefore the present invention relates specifically to the compounds of general formula (I), in which R1 and R2, which may be identical or different, are selected from the group comprising H, —CnH2n-1, a linear or branched alkyl group having from 1 to 6 carbon atoms, or together form an aromatic or aliphatic ring with 5 or 6 atoms; R3 is selected from —CO—CH3, —NHOH, —OH, —OR6 in which R6 is a linear or branched alkyl group having from 1 to 6 carbon atoms; R4 is selected from H, a linear or branched alkyl group having from 1 to 6 carbon atoms, phenyl, benzyl, —CF3 or —CF2CF3, vinyl or allyl; R5, R7, R8 are hydrogen atoms; or R3 and R4, R4 and R5, or R7 and R8 together form a ring, fused to the benzene, aromatic or aliphatic ring with 5 or 6 atoms comprising from 1 to 2 heteroatoms selected independently from the group comprising N, O. and use thereof in the medical field.
    Type: Grant
    Filed: July 24, 2006
    Date of Patent: March 20, 2012
    Assignee: Giuliani International Limited
    Inventors: Giancarlo Naccari, Sergio Baroni
  • Publication number: 20110294783
    Abstract: The present invention concerns boosting the activity of crop protection materials comprising inhibitors of fatty acid biosynthesis (for example phenyl-substituted cyclic ketoenols) through the addition of ammonium salts and/or phosphonium salts or through the addition of ammonium salts and/or phosphonium salts and penetrants, the corresponding materials, processes for preparing them, and their use in crop protection.
    Type: Application
    Filed: August 10, 2011
    Publication date: December 1, 2011
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Reiner FISCHER, Stefan LEHR, Peter MARCZOK, Udo Reckmann, Christian Arnold, Waltraud Hempel, Erich SANWALD, Rolf Pontzen
  • Publication number: 20110071142
    Abstract: The present invention relates to methods of identifying small molecule candidate agents capable of modulating transcription factor function such that the function/expression of a target transcription factor and/or proteins downstream of this target protein comprises the screening of small molecule libraries using in silico high throughput docking for candidate small molecules/agents that are selectively identified for their ability to target and disrupt the transcription factor-DNA interface through unique transcription factor and/or DNA descriptors that are defined within a pharmacophore, and then testing/evaluating the candidate agents identified above through one or more in vitro assays for their ability to modulate transcription factor function including expression of this target protein and/or proteins that are downstream of the target transcription factor. The present invention also relates to various compounds described herein (e.g.
    Type: Application
    Filed: March 19, 2010
    Publication date: March 24, 2011
    Applicant: BETH ISRAEL DEACONESS MEDICAL CENTER
    Inventors: Peter Oettgen, Alan C. Rigby, Towia Libermann
  • Publication number: 20110021621
    Abstract: The present invention relate to a drug for treating circulatory insufficiency containing a benzopyran derivative represented by the following general formula (I): and/or a physiologically acceptable salt thereof as an active ingredient, wherein R1 is an alkyl group having 1 to 10 carbon atoms, or an alkenyl group having 2 to 10 carbon atoms; and any one of R2, R3, R4 and R5 is a hydroxyl group, an alkoxy group, an alkenyloxy group, an alkoxy group substituted with a hydroxyl group, or an alkoxy group substituted with a carboxy group, and the others are hydrogen atoms.
    Type: Application
    Filed: September 29, 2010
    Publication date: January 27, 2011
    Applicant: ACTIVUS PHARMA CO., LTD.
    Inventors: Hidetsugu Takagaki, Yasuo Aoki, Mitsuteru Ishiwara
  • Publication number: 20100331400
    Abstract: The present invention relates to novel compounds of formula (I), methods, and compositions capable of decreasing HIF hydroxylase activity, thereby increasing the stability and/or activity of hypoxia inducible factor (HIF).
    Type: Application
    Filed: February 5, 2009
    Publication date: December 30, 2010
    Inventors: Wen-bin Ho, Lee Wright, Shaojiang Deng, Eric Turtle, Lee A. Flippin
  • Publication number: 20100324266
    Abstract: Novel compounds are provided, which are useful as linking groups in chemical synthesis, preferably in the solid phase synthesis of oligonucleotides and polypeptides. These compounds are generally photolabile and comprise protecting groups which can be removed by photolysis to unmask a reactive group. The protecting group has the general formula Y, wherein Y is a chemical structure as shown in FIG. 1. Also provided is a method of forming, from component molecules, a plurality of compounds on a support, each compound occupying a separate predefined region of the support, using the protected compounds described above.
    Type: Application
    Filed: June 9, 2010
    Publication date: December 23, 2010
    Applicant: Affymetrix, INC.
    Inventors: Anthony D. Barone, Glenn H. McGall
  • Patent number: 7776912
    Abstract: Disclosed are acetals of nepetalic acid. They may be prepared by reaction of an alcohol with nepetalic acid, and are useful as repellents for insects and arthropods, in addition to other uses.
    Type: Grant
    Filed: June 27, 2007
    Date of Patent: August 17, 2010
    Assignee: E.I. du Pont de Nemours and Company
    Inventors: Mark A. Scialdone, Ann Y. Liauw
  • Publication number: 20100168225
    Abstract: Compounds of Formula 5 and prodrug compounds of Formula 5 wherein G1 is H or OH; G2 is H, R?, or CO2R?; G3, G4 and G5, are each independently selected from the group consisting of: H, R?, OH, OR?, F, Cl, Br, I, NH2, NHR?,NR?2, CN, SH, SR?, SO3H, SO3R?, SO2R?, OSO3R?, and NO2; and R? is a one to four carbon alkyl group are provided. Uses of these compounds and methods of medical treatment involving these compounds for the treatment of hepatitis C are also provided.
    Type: Application
    Filed: April 18, 2008
    Publication date: July 1, 2010
    Inventors: Francois Jean, Raymond Andersen
  • Patent number: 7674398
    Abstract: Present invention refers to substituted cumarines that are capable to emit fluorescent light when illuminated by wave lengths within ultraviolet range. Present invention also refers to process of production of said substituted cumarines, well as provides compositions containing said substituted cumarines, especially compositions containing said cumarines and volatile solvents and/or adjuvants. Said compositions can be used in objects of great value for its owner, in view of facilitating the identification of such objects.
    Type: Grant
    Filed: September 20, 2005
    Date of Patent: March 9, 2010
    Assignee: Universidade Federal do Rio de Janerio UFRJ
    Inventors: Claudio Cerqueira Lopes, Rosangela Sabattini Capella Lopes, Jari Cardoso Norbega, Glaucia Slans Alves Barbosa, Maicon Guerra, Jose Roque Mota Carvalho
  • Publication number: 20100048882
    Abstract: Novel analogues and derivatives of novobiocin are provided, including compounds having modifications to the amide side chain, coumarin ring, and sugar moieties. The compounds of the present invention are useful as heat shock protein 90 inhibitors, and may be used as anticancer and neuroprotective agents.
    Type: Application
    Filed: October 1, 2009
    Publication date: February 25, 2010
    Applicant: UNIVERSITY OF KANSAS
    Inventors: Brian S. Blagg, Len Neckers, Xiao Ming Yu
  • Patent number: 7642364
    Abstract: The invention relates to pesticide and bactericide, specifically to the benzopyrone compounds and its preparation method and use thereof. The benzopyrone compounds of the invention having general formula (I): The present invention, having good pesticide activity and broad bactericide activity, applied for controlling various pests in plants such as army worm, diamond backmoth and aphid, carmine spider mite, two-spotted spider mite, ladybeetle, mites and mosquito larvae. Various disease in plants can be controlled by the invention and that of grape downy mildew, rice sheath and culm blight, rice blast, tomato early blight, tomato late blight, wheat leaf rust, wheat leaf blotch, wheat powdery mildew, cucumber powdery mildew, cucumber downy mildew, cucumber grey mold and so on.
    Type: Grant
    Filed: November 4, 2004
    Date of Patent: January 5, 2010
    Assignee: Shenyang Research Institute of Chemical Industry
    Inventors: Changling Liu, Aiying Guan, Hong Zhang, Mingxing Zhang, Zhengming Li, Miao Li, Lin Li, Zhinian Li, Chunqing Hou
  • Patent number: 7553869
    Abstract: Coumarine/chinolone and Martina-type compounds, compositions, and method of using the compounds and compositions for protein detection, assay, quantitation, etc. are disclosed. The composition, also referred to as a dye, has enhanced sensitivity over commercially available protein stains, and may be used to stain proteins in solution, proteins separated on gels, proteins transferred to solid supports, etc.
    Type: Grant
    Filed: July 28, 2006
    Date of Patent: June 30, 2009
    Assignee: Pierce Biotechnology, Inc.
    Inventors: Peter T. Czerney, Surbhi Desai, Frank G. Lehmann, Zakir S. Murtaza, Bernd G. Schweder, Matthias S. Wenzel, Brian David Wolf
  • Patent number: 7541478
    Abstract: The present invention relates to an alkaline earth metal salt or an organic amine salt of a compound represented by the formula [I]: wherein R1 and R2 are each a hydrogen atom, a halogen atom, or an optionally substituted linear hydrocarbon group; ring A is an optionally further substituted benzene ring; B is an optionally substituted benzene ring; R is a carboxyl group or a linear hydrocarbon group substituted with a carboxyl group and the like.
    Type: Grant
    Filed: March 1, 2005
    Date of Patent: June 2, 2009
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Shogo Marui, Masaki Ogino, Hiroyuki Tawada, Osamu Yabe
  • Patent number: 7538233
    Abstract: The present invention relates to coumarins of the formula (I): that are useful as inhibitors of nitric oxide synthase. Pharmaceutical compositions and methods of using these compounds as inhibitors of nitric oxide synthase are described herein.
    Type: Grant
    Filed: August 24, 2004
    Date of Patent: May 26, 2009
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Sharon Jackson, Thaddeus Nieduzak, Sam Rebello, Guyan Liang, Yulin Chiang, Jean Merrill
  • Patent number: 7531646
    Abstract: This invention provides a method of detecting enzyme activity on a solid medium. The enzyme substrate has a chromogenic portion comprising a catechol residue, in which a derivitising moiety is linked to the aromatic ring of the catechol via a bond, and an enzyme cleavable group which is attached via an ester or ether linkage to the oxygen atom derived from a hydroxyl group of the catechol residue. If the enzyme substrate contacts an enzyme capable of cleaving the enzyme cleavable groups and the cleaved compound contacts a chelatable metal ion, a substantially non-diffusable coloured precipitate is formed.
    Type: Grant
    Filed: October 24, 2002
    Date of Patent: May 12, 2009
    Inventor: Michael Burton
  • Publication number: 20090104711
    Abstract: Disclosed herein are fluorescent markers having a double bond ester group and a method for marking and detecting the same. More particularly, disclosed are a method for identifying oil products, which comprises marking the oil products with fluorescent markers having an unsaturated double bond ester group, adding a developing agent having a function of inducing specific fluorescence to the marked oil products, and detecting the fluorescent marker with a fluorescence spectrophotometer in the UV/VIS region, as well as said markers.
    Type: Application
    Filed: July 28, 2006
    Publication date: April 23, 2009
    Inventor: Hyun-Ho Sim
  • Publication number: 20090087387
    Abstract: Disclosed are acetals of nepetalic acid. They may be prepared by reaction of an alcohol with nepetalic acid, and are useful as repellents for insects and arthropods, in addition to other uses.
    Type: Application
    Filed: June 27, 2007
    Publication date: April 2, 2009
    Inventors: MARK A. SCIALDONE, ANN Y. LIAUW
  • Patent number: 7439077
    Abstract: The present invention relates to the albumin-guided development of coumarin analogs and the analogs developed thereby. The coumarin analogs of the present invention are identified and isolated by the fact that they have binding sites to albumin which are different than the binding sites of conventional coumarin analogs such as sodium warfarin, and as a result will be less prone to be displaced since the binding site of sodium warfarin is shared by numerous drugs such as aspirin. The coumarin analogs of the invention are advantageous because they can achieve the effects of the prior coumarin analogs with a minimum of metabolic complications and undesirable side effects.
    Type: Grant
    Filed: February 20, 2007
    Date of Patent: October 21, 2008
    Assignee: New Century Pharmaceuticals, Inc.
    Inventor: Daniel C. Carter
  • Patent number: 7411076
    Abstract: A medicament for enhancing an effect of a cancer therapy based on a mode of action of DNA injury, which comprises as an active ingredient a compound represented by the following general formula (I): wherein X represents a single bond or a C1 to C6 alkylene group which may be substituted; A represents a C1 to C6 alkyl group which may be substituted, a C6 to C10 aryl group which may be substituted, or a 4 to 10-membered monocyclic or bicyclic and unsaturated, partly saturated, or completely saturated heterocyclic group which may be substituted, wherein said heterocyclic group comprises as ring-constituting atoms 1 to 4 hetero atoms selected from the group consisting of nitrogen atom, oxygen atom, and sulfur atom.
    Type: Grant
    Filed: September 12, 2002
    Date of Patent: August 12, 2008
    Assignee: Institute of Medicinal Molecular Design, Inc.
    Inventors: Susumu Muto, Masayuki Komukai, Akiko Itai
  • Publication number: 20080026478
    Abstract: Coumarine/chinolone and Martina-type compounds, compositions, and method of using the compounds and compositions for protein detection, assay, quantitation, etc. are disclosed. The composition, also referred to as a dye, has enhanced sensitivity over commercially available protein stains, and may be used to stain proteins in solution, proteins separated on gels, proteins transferred to solid supports, etc.
    Type: Application
    Filed: July 28, 2006
    Publication date: January 31, 2008
    Applicant: PIERCE BIOTECHNOLOGY, INC.
    Inventors: Peter T. Czerney, Surbhi Desai, Frank G. Lehmann, Zakir S. Murtaza, Bernd G. Schweder, Matthias S. Wenzel, Brian David Wolf
  • Patent number: 7256158
    Abstract: The invention relates to new phenyl-substituted cyclic ketoenols of the formula (I) in which Het represents one of the groups ?wherein A, B, D, G, X, Y and Z have the meaning given in the description, several processes and intermediate products for their preparation and their use as pest control agents and herbicides.
    Type: Grant
    Filed: August 20, 2004
    Date of Patent: August 14, 2007
    Assignee: Bayer AG
    Inventors: Folker Lieb, Hermann Hagemann, Arno Widdig, Michael Ruther, Reiner Fischer, Thomas Bretschneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Peter Dahmen, Markus Dollinger, Hans Joachim Santel, Alan Graff, Norbert Mencke, Andreas Turberg
  • Patent number: 7235674
    Abstract: The present invention is directed to substituted coumarins and quinolines and analogs thereof, represented by the general Formula I: wherein A, B, X, Y, and Z are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
    Type: Grant
    Filed: November 16, 2004
    Date of Patent: June 26, 2007
    Assignee: Cytovia, Inc.
    Inventors: Sui Xiong Cai, Hong Zhang, William E. Kemnitzer, Songchun Jiang, John Drewe, Richard Storer
  • Patent number: 7148253
    Abstract: 4-Thio substituted coumarin derivatives, 4,5-dithio substituted coumarin derivatives, and coumarin dimers are provided, as well as processes for their preparation. The invention also provides a method and composition for the treatment of hepatitis C virus (HCV) by adiministering 4-thio substituted coumarin derivatives, 4,5-dithio substituted coumarin derivatives, and coumarin dimers.
    Type: Grant
    Filed: January 6, 2004
    Date of Patent: December 12, 2006
    Assignee: XTL Biopharmaceuticals Ltd.
    Inventors: Jie Wu, Zhen Yang, Reza Fathi, Qiang Zhu
  • Patent number: 7145020
    Abstract: This invention is drawn to compounds which are more easily metabolized by the metabolic drug detoxification systems. Particularly, warfarin analogs which have been designed to include esters within the structure of the compounds are taught. The invention teaches methods of reducing the toxicity of drugs comprising the introduction of ester groups into drugs during the synthesis of the drug. This invention is also drawn to methods of treating coagulation disorders comprising the administration of compounds which have been designed to be metabolized by serum or intracellular hydrolases and esterases. Pharmaceutical compositions of the ester containing warfarin, analogs are also taught.
    Type: Grant
    Filed: April 8, 2004
    Date of Patent: December 5, 2006
    Assignee: Aryx Therapeutics
    Inventors: Pascal Druzgala, Xiaoming Zhang, Jurg R. Pfiste
  • Patent number: 7109043
    Abstract: A fluorescent probe for measuring magnesium ion, which can selectively form a complex with magnesium ion in aqueous system is disclosed. The fluorescent probe for measuring magnesium ion according to the present invention has the structure represented by the following Formula [I]: (wherein R1 represents a hydrogen atom, metal atom or an ester-forming group; A represents a group which forms a ring structure together with carbon atom 1 and carbon atom 2; and X is a fluorescent group which may form a condensed ring together with the ring containing the group A).
    Type: Grant
    Filed: July 25, 2001
    Date of Patent: September 19, 2006
    Assignees: Japan Science and Technology Corporation, The Kanagawa Academy of Science and Technology Foundation, Keio University
    Inventors: Koji Suzuki, Yoshio Suzuki, Kotaro Oka
  • Patent number: 7094378
    Abstract: Methods and apparatuses for treating fluids to inactivate microorganisms which may be present therein, said fluid containing one or more components selected from the group consisting of protein, blood and blood constituents are provided. The methods comprise adjusting the percentage of plasma in said fluid to a desired value; mixing an inactivation-effective, substantially non-toxic amount of an endogenous photosensitizer or endogenously-based derivative photosensitizer to said fluid; exposing said fluid to photoradiation of sufficient wavelength and energy to activate the photosensitizer, whereby said microorganisms are inactivated.
    Type: Grant
    Filed: June 15, 2000
    Date of Patent: August 22, 2006
    Assignee: Gambro, Inc.
    Inventors: Raymond Paul Goodrich, Jr., Dennis Hlavinka
  • Patent number: 6921776
    Abstract: A compound is described. In particular, a non-steroidal sulphamate compound is described. The compound is suitable for use as an inhibitor of oestrone sulphatase. The compound is of general Formula (A), wherein R1-R6 are independently selected from H, halo, hydroxy, sulphamate, alkyl and substituted variants or salts thereof, but wherein at least one of R1-R6 is a sulphamate group; and wherein X is any one of S, NH, a substituted N, CH2, or a substituted C.
    Type: Grant
    Filed: August 14, 2000
    Date of Patent: July 26, 2005
    Assignee: Sterix Limited
    Inventors: Michael John Reed, Barry Victor Lloyd Potter
  • Patent number: 6864279
    Abstract: This invention is drawn to compounds which are more easily metabolized by the metabolic drug detoxification systems. Particularly, warfarin analogs which have been designed to include esters within the structure of the compounds are taught. The invention teaches methods of reducing the toxicity of drugs comprising the introduction of ester groups into drugs during the synthesis of the drug. This invention is also drawn to methods of treating coagulation disorders comprising the administration of compounds which have been designed to be metabolized by serum or intracellular hydrolases and esterases. Pharmaceutical compositions of the ester containing warfarin, analogs are also taught.
    Type: Grant
    Filed: April 24, 2002
    Date of Patent: March 8, 2005
    Assignee: Aryx Therapeutics
    Inventors: Pascal Druzgala, Xiaoming Zhang, Jürg Pfister
  • Publication number: 20040180950
    Abstract: 4-Thio substituted coumarin derivatives, 4,5-dithio substituted coumarin derivatives, and coumarin dimers are provided, as well as processes for their preparation. The invention also provides a method and composition for the treatment of hepatitis C virus (HCV) by adiministering 4-thio substituted coumarin derivatives, 4,5-dithio substituted coumarin derivatives, and coumarin dimers.
    Type: Application
    Filed: January 6, 2004
    Publication date: September 16, 2004
    Inventors: Jie Wu, Zhen Yang, Reza Fathi, Qiang Zhu
  • Patent number: 6780887
    Abstract: The present invention is related to a compound of formula (I), salts and pro-drugs of the compound (I) and methods for treating and/or preventing partial or total ischemia, methods for treating and/or preventing pathologies associated with ischemia or with mitochondrial deficiencies.
    Type: Grant
    Filed: July 30, 2002
    Date of Patent: August 24, 2004
    Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
    Inventors: Carine Michiels, Martine Redon, Jose Remacle
  • Patent number: 6703514
    Abstract: 4-thio substituted coumarin derivatives and coumarin dimers are provided, as well as processes for their preparation. A synthetic process for the preparation of 4-thio substituted coumarin derivatives is provided using mild reaction conditions, which maintains a high substituent tolerance and is appropriate for use in solid phase syntheses for producing a library of 4-thio substituted coumarin derivatives for biological screening.
    Type: Grant
    Filed: May 13, 2003
    Date of Patent: March 9, 2004
    Assignee: Vivo Quest, Inc.
    Inventors: Jie Wu, Zhen Yang, Reza Fathi, Qiang Zhu, Lisha Wang