Polycyclo Ring System Having The Five-membered Hetero Ring As One Of The Cyclos Patents (Class 548/414)
  • Publication number: 20110318692
    Abstract: The present invention relates to a photoactive compound of a novel structure represented by Chemical Formula 1 below In Chemical Formula 1, R1 and R2, R3, and A are as defined in the specification, and a photosensitive resin composition comprising the same. The photoactive compound of the present invention comprises a nitro group and a phosphonate structure and thus exhibits excellent sensitivity through efficient absorption for UV light, excellent compatibility between the photoactive compound and the alkali-soluble binder resin, and an improved solubility of the photosensitive resin composition. Furthermore, the photosensitive resin composition of the present invention has excellent residual film thickness and mechanical strength characteristics and heat-resistant, chemical-resistant, and development-resistant properties.
    Type: Application
    Filed: February 12, 2010
    Publication date: December 29, 2011
    Applicant: LG CHEM, LTD.
    Inventors: Chang Ho Cho, Sung Hyun Kim, Raisa Kharbash, Keon Woo Lee, Dong Kung Oh, Won Jin Cung, Sang Kyu Kwak, Chang Soon Lee
  • Publication number: 20110294118
    Abstract: The invention provides a novel class of fluorescent compounds. Also provided are conjugates of the fluorescent compounds, methods of using the fluorescent compounds and their conjugates as well as kits including the fluorescent compounds and their conjugates.
    Type: Application
    Filed: November 29, 2010
    Publication date: December 1, 2011
    Applicant: BIOSEARCH TECHNOLOGIES, INC.
    Inventor: MARK REDDINGTON
  • Publication number: 20110269716
    Abstract: The invention relates to antioxidant substituted isoindoline nitroxide compounds and their use in methods of treating or preventing diseases or disorders related to oxidative stress, methods of reducing oxidative stress and methods of protecting a subject from oxidative stress upon exposure to ionising radiation. Pharmaceutical compositions comprising the antioxidant compounds are also described.
    Type: Application
    Filed: September 30, 2009
    Publication date: November 3, 2011
    Applicant: Queensland University of Technology
    Inventors: Steven Bottle, Kathryn Fairfull-Smith, Farina Schill
  • Publication number: 20110256065
    Abstract: The present invention is directed to a non-isotopic methods for the in vitro and in vivo detection of hydroxyapatite-positive cells and structures.
    Type: Application
    Filed: June 27, 2011
    Publication date: October 20, 2011
    Inventor: John V. Frangioni
  • Patent number: 8012978
    Abstract: The present invention provides prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group containing a sulfonic acid containing phenyl carbamate, in which the protecting group confers enhanced water solubility upon the prodrug, and in which the prodrug also has a moiety, such as a sulfide or a disulfide, that can conjugate to a cell binding reagent such as an antibody, and for the therapeutic use of such prodrug and conjugates, and for processes for preparing such prodrugs and conjugates.
    Type: Grant
    Filed: September 4, 2008
    Date of Patent: September 6, 2011
    Assignee: ImmunoGen, Inc.
    Inventors: Robert Zhao, Ravi V. J. Chari
  • Patent number: 7981527
    Abstract: The invention provides a light-emission material comprising a compound having Formula (I): wherein each of A independently is: each of Rm independently is H, alkyl, alkenyl, alkynyl, CN, CF3, alkylamino, amino, alkoxy, halo, aryl, or heteroaryl.
    Type: Grant
    Filed: June 26, 2009
    Date of Patent: July 19, 2011
    Assignee: National Tsing Hua University
    Inventors: Chien-Hong Cheng, Ho-Hsiu Chou
  • Publication number: 20110172423
    Abstract: An organic light-emitting diode comprising at least one cyclic phosphazene compound, a light-emitting layer formed from at least one matrix material and at least one emitter material, wherein the at least one matrix material comprises at least one cyclic phosphazene compound, the use of cyclic phosphazene compounds in organic light-emitting diodes and a device selected from the group consisting of stationary visual display units, mobile visual display units and illumination units comprising at least one inventive organic light-emitting diode, and selected cyclic phosphazene compounds and processes for preparing them.
    Type: Application
    Filed: June 17, 2009
    Publication date: July 14, 2011
    Applicants: BASF SE, KONINKLIJKE PHILIPS ELECTRONICS N.V., OSRAM OPTO SEMICONDUCTORS GMBH
    Inventors: Evelyn Fuchs, Oliver Molt, Nicolle Langer, Christian Lennartz, Peter Strohriegl, Pamela Schroegel, Herbert Friedrich Boerner, Volker Van Elsbergen, Arvid Hunze, Ralf Krause
  • Publication number: 20110130349
    Abstract: The present invention relates to compounds and methods useful in the prevention or treatment of diseases or conditions associated with Toll-like receptor 2 activation.
    Type: Application
    Filed: November 23, 2010
    Publication date: June 2, 2011
    Inventors: Jesse Chow, Fabian Gusovksy, Lynn Hawkins, Mark Spyvee
  • Publication number: 20110129871
    Abstract: A specific culture medium for growth, detection, identification and/or counting of Staphylococcus aureus bacteria, said medium includes at least one fluorogenic, chromogenic or luminescent substrate of phospholipase C. Said medium permits differentiation between Staphylococcus aureus and coagulase-negative staphylococci.
    Type: Application
    Filed: August 13, 2009
    Publication date: June 2, 2011
    Applicant: BIOMERIEUX
    Inventors: David Mosticone, Sylvain Orenga, Antoine Vimont, Yuping Guo, Martine Dhedin
  • Publication number: 20110118210
    Abstract: Compounds of formula I: wherein R1, R2, n and m are as defined in the specification, processes for their production, their uses and pharmaceutical compositions containing them.
    Type: Application
    Filed: January 28, 2011
    Publication date: May 19, 2011
    Inventors: Rainer ALBERT, Eric Francotte, Frédéric Zecri, Markus Zollinger
  • Publication number: 20110070194
    Abstract: Provided are pyrrolo[1,2-f][1,2,4]triazinyl, imidazo[1,5-f][1,2,4]triazinyl, imidazo[1,2-f][1,2,4]triazinyl, and [1,2,4]triazolo[4,3-f][1,2,4]triazinyl nucleosides, nucleoside phosphates and prodrugs thereof, wherein the 2? position of the nucleoside sugar is substituted with halogen and carbon substitutents. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections caused by both wild type and mutant strains of HCV.
    Type: Application
    Filed: September 20, 2010
    Publication date: March 24, 2011
    Applicant: Gilead Sciences, Inc.
    Inventors: Aesop Cho, Choung U. Kim, Samuel E. Metobo, Adrian S. Ray, Jie Xu
  • Patent number: 7902175
    Abstract: Compounds of formula I: wherein R1, R2, n and m are as defined in the specification, processes for their production, their uses and pharmaceutical compositions containing them.
    Type: Grant
    Filed: February 24, 2009
    Date of Patent: March 8, 2011
    Assignee: Novartis AG
    Inventors: Rainer Albert, Eric Francotte, Frederic Zecri, Markus Zollinger
  • Publication number: 20110054188
    Abstract: A compound represented by general formula (I) below, or a pharmacologically acceptable salt thereof: wherein X represents sulfonic acid group or phosphoric acid group; R1 and R2 represent substituents; R3 to R6 represent optionally substituted alkyl groups; R7 and R8 represent optionally substituted alkyl groups; L1 to L3 represent optionally substituted methine groups; r represents an integer of from 0 to 3, and when r is 2 or more, the plural L2 and the plural L3 may be the same or different, respectively; each of m and n represent integers of 0 to 3; at least one of the substituents is an acid group selected from sulfonic acid group, carboxylic acid group, and phosphonic acid group or a group comprising the acid group; and two or more of the acid groups and X are selected from carboxylic acid group and phosphonic acid group.
    Type: Application
    Filed: August 26, 2010
    Publication date: March 3, 2011
    Applicant: FUJIFILM Corporation
    Inventors: Hiroshi KOORI, Masahiko TANIGUCHI
  • Publication number: 20110046239
    Abstract: The present invention relates to a method for forming a calcium-based carrier particle consisting of the calcium-based material, an active, with or without a surface modification, a stabilizing agent, and the related composition. The calcium-based particle is illustrated by the general formula Cax(PO4)y(OH)zR and may also include a silica or silica oxide substituent. R is an active or actives such as an organic or inorganic molecule that includes markers, amines, thiols, epoxies, organosilicones, organosilanes, sulfates, and water soluble agents and, as needed, a surface modification, S, which may be either organic or inorganic. A stabilizing agent may be necessary to maintain dispersion of the particles in aqueous media. Examples of a surface modifying material and stabilizing agents are inorganic salts of aluminum and boron or organic materials such as organosilanes or low molecular weight polymers.
    Type: Application
    Filed: August 24, 2009
    Publication date: February 24, 2011
    Inventors: Bruce A. Keiser, Timothy S. Keizer, Brett M. Showalter, Tiffany Bohnsack, James H. Adair, Mylisa Parette, Amy Knupp, Andrei S. Zelenev, Jason R. Burney
  • Publication number: 20110046238
    Abstract: The present invention relates to a method for forming a calcium-based carrier particle consisting of the calcium-based material, an active, with or without a surface modification, a stabilizing agent, and the related composition. The calcium-based particle is illustrated by the general formula Cax(PO4)y(OH)zR and may also include a silica or silica oxide substituent. R is an active or actives such as an organic or inorganic molecule that includes markers, amines, thiols, epoxies, organosilicones, organosilanes, sulfates, and water soluble agents and, as needed, a surface modification, S, which may be either organic or inorganic. A stabilizing agent may be necessary to maintain dispersion of the particles in aqueous media. Examples of a surface modifying material and stabilizing agents are inorganic salts of aluminum and boron or organic materials such as organosilanes or low molecular weight polymers.
    Type: Application
    Filed: August 24, 2009
    Publication date: February 24, 2011
    Inventors: Bruce A. Keiser, Timothy S. Keizer, Brett M. Showalter, Tiffany Bohnsack, James H. Adair, Mylisa Parette, Amy Knupp, Andrei S. Zelenev, Jason R. Burney
  • Patent number: 7888336
    Abstract: The invention provides well-defined aryl and/or heteroaryl substituted indoles that are useful as spingosine-1-phosphate agonists or antagonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: September 18, 2008
    Date of Patent: February 15, 2011
    Assignee: Allergan, Inc.
    Inventors: Richard L. Beard, Haiqing Yuan, John E. Donello
  • Publication number: 20110008373
    Abstract: Prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group such as a piperazino carbamate, a 4-piperidino-piperidino carbamate or a phosphate, in which the protecting group confers enhanced water solubility and stability upon the prodrug, and in which the prodrug also has a moiety, such as a disulfide, that can conjugate to a cell binding reagent such as an antibody. The therapeutic use of such prodrug conjugates is also described; such prodrugs of cytotoxic agents have therapeutic use because they can deliver cytotoxic prodrugs to a specific cell population for enzymatic conversion to cytoxic drugs in a targeted fashion.
    Type: Application
    Filed: September 20, 2010
    Publication date: January 13, 2011
    Applicant: IMMUNOGEN, INC.
    Inventors: Robert Yongxin ZHAO, Ravi V.J. CHARI
  • Publication number: 20100331543
    Abstract: The quenching compounds of the invention are weakly luminescent cyanines that are substituted by one or more heteroaromatic quenching moieties. The quenching compounds of the invention exhibit little or no observable luminescence and efficiently quench a broad spectrum of luminescent compounds. The chemically reactive quenching compounds possess utility for labeling a wide variety of substances, including biomolecules. These labeled substances are highly useful for a variety of energy-transfer assays and applications.
    Type: Application
    Filed: August 30, 2010
    Publication date: December 30, 2010
    Inventors: Zhenjun Diwu, Jianheng Zhang, Yi Tang
  • Patent number: 7858784
    Abstract: Ligands for transition metals are disclosed herein, which may be used in various transition-metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The disclosed methods provide improvements in many features of the transition-metal-catalyzed reactions, including the range of suitable substrates, number of catalyst turnovers, reaction conditions, and efficiency. For example, improvements have been realized in transition-metal-catalyzed cross-coupling reactions.
    Type: Grant
    Filed: December 12, 2008
    Date of Patent: December 28, 2010
    Assignee: Massachusetts Institute of Technology
    Inventors: Stephen L. Buchwald, Brett P. Fors, David S. Surry
  • Publication number: 20100292187
    Abstract: The present invention provides compounds, pharmaceutical compositions, and methods of using such compounds or compositions for treating infection by a virus, or for affecting viral IRES activity.
    Type: Application
    Filed: June 14, 2010
    Publication date: November 18, 2010
    Applicant: PTC THERAPEUTICS, INC.
    Inventors: Gary M. Karp, Peter Seongwoo Hwang, James J. Takasugi, Hongyu Ren, Richard Gerald Wilde, Anthony A. Turpoff, Alexander Arefolov, Guangming Chen, Jeffrey A. Campbell, Chunshi Li, Steven Paget, Nanjing Zhang, Xiaoyan Zhang, Jin Zhu
  • Publication number: 20100292448
    Abstract: An extractor and a method using the extractor for extracting active principle from solid materials using an extracting fluid, said extractor comprising among others an extractor column (1), having a first side (22), a second side (23), a top side (24), and a bottom side (25); a top plate (10) for sealing the said extractor column (1), said top plate (10) positioned at said top side (24), at least one perforated plate (4) having projections (5); wherein said perforated plate (4) is positioned inside said extractor column (1) by means of a screw shaft (3), wherein said screw shaft (3) passes through said top plate (10) by means of a leak proof joint (12); wherein said joint (12) allows rotation of said screw shaft (3).
    Type: Application
    Filed: April 3, 2008
    Publication date: November 18, 2010
    Inventor: Bjorn Hagerup Nilssen
  • Publication number: 20100284931
    Abstract: The invention generally relates to novel fluorescent phospholipid compounds, compositions comprising these compounds, and their use in a variety of diagnostic applications, including fluorescence imaging of tumors.
    Type: Application
    Filed: May 11, 2009
    Publication date: November 11, 2010
    Inventors: Anatoly Pinchuk, Jamey P. Weichert, Marc Longino, Irawati Kandela, William R. Clarke
  • Publication number: 20100261903
    Abstract: Reagents are provided for the introduction of phosphonate groups into fluorescent dyes. Methods are also provided for preparing dye conjugates.
    Type: Application
    Filed: January 6, 2010
    Publication date: October 14, 2010
    Inventors: Eugeny Lukhtanov, Alexei Vorobiev
  • Publication number: 20100253212
    Abstract: The invention provides a light-emission material comprising a compound having Formula (I): , wherein each of A independently is: each of Rm independently is H, alkyl, alkenyl, alkynyl, CN, CF3, alkylamino, amino, alkoxy, halo, aryl, or heteroaryl.
    Type: Application
    Filed: June 26, 2009
    Publication date: October 7, 2010
    Inventors: Chien-Hong Cheng, Ho-Hsiu Chou
  • Publication number: 20100240612
    Abstract: The invention provides methods to treat a mycobacterium infection and methods to inhibit mycobacterial polyprenyl pyrophosphate synthesis with a compound of formula I. The invention also provides novel compounds of formula I as well as salts and prodrugs thereof.
    Type: Application
    Filed: March 22, 2010
    Publication date: September 23, 2010
    Applicant: University of Iowa Research Foundation
    Inventors: David F. Wiemer, Rocky J. Barney, Raymond J. Hohl
  • Publication number: 20100240614
    Abstract: The invention provides well-defined aryl and/or heteroaryl substituted indoles that are useful as spingosine-1-phosphate agonists or antagonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: September 18, 2008
    Publication date: September 23, 2010
    Inventors: Richard L. Beard, Haiqing Yuan, John E. Donello
  • Publication number: 20100210595
    Abstract: The present invention relates to substituted arylsulphonylaminomethyl-phosphonic acid derivatives of general formula wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.
    Type: Application
    Filed: July 25, 2008
    Publication date: August 19, 2010
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Holger Wagner, Elke Langkopf, Matthias Eckhardt, Ruediger Streicher, Corinna Schoelch, Annette Schuler-Metz, Alexander Pautsch
  • Publication number: 20100210594
    Abstract: The present invention relates to substituted arylsulphonylaminomethyl-phosphonic acid derivatives of general formula wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.
    Type: Application
    Filed: July 25, 2008
    Publication date: August 19, 2010
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Holger Wagner, Elke Langkopf, Matthias Eckhardt, Ruediger Streicher, Corinna Schoelch, Annette Schuler-Metz, Alexander Pautsch
  • Patent number: 7772216
    Abstract: The present invention provides a method for identifying inhibitors of protein kinases and/or protein phosphatases. Methods are also provided for inhibiting protein kinase and/or protein phosphatase activity. Specific non-peptide protein tyrosine kinase and/or protein phosphatase inhibitors are provided. The protein kinase or protein phosphatase inhibitors of the present invention may be used to treat a number of conditions in patients, including cancer, psoriasis, arthrosclerosis, immune system activity, Type II diabetes, and obesity.
    Type: Grant
    Filed: August 16, 2005
    Date of Patent: August 10, 2010
    Assignee: The Research Foundation of State University of New York
    Inventors: David G. Hangauer, Jr., Moustafa E. El-Araby, Karen L. Milkiewicz
  • Patent number: 7750037
    Abstract: A PKB (Akt) activating agent comprising a compound represented by the formula (I): wherein R1 and R2: H, a hydrocarbon group or a heterocyclic group or R1 and R2 form a ring in cooperation with the adjacent carbon atom; R3: H, a hydrocarbon group or a heterocyclic group; W: represents a group represented by the formulas: wherein ring A: an optionally substituted benzene ring; ring B: an optionally substituted 5- to 7-membered nitrogen-containing heterocycle; R4: an aliphatic hydrocarbon group substituted with an aromatic group and further optionally substituted, or an acyl group containing an aromatic group; R5: H, C1-6 alkyl or acyl; R4c: an aromatic group, an aliphatic hydrocarbon group or acyl; and X: O or S; Y: O, S or NH; and ring C: an optionally substituted benzene ring, or a salt or a prodrug thereof, and use of the activating agent in prevention or treatment of depression, anxiety, manic-depressive psychosis or PTSD are provided.
    Type: Grant
    Filed: June 27, 2006
    Date of Patent: July 6, 2010
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Shigenori Ohkawa, Masaomi Miyamoto
  • Publication number: 20100143960
    Abstract: A subject matter of the invention is cyanine derivatives of formula: in which the dotted lines represent the atoms necessary for the formation of one or two fused aromatic rings, each ring comprising 5 or 6 carbon atoms; R1, R2, R3 and R4 represent, independently of one another: H; substituted or unsubstituted C1-C15 alkyl; C1-C6 alkoxy; (C2-C12)dialkylamino; C1-C6 alkoxycarbonyl; di(C2-C12)alkylamido; a substituted or unsubstituted aryl, arylalkyl or aryloxy group; a halogen atom; a nitro; an L1-W, L2-M, L2-A or L2-G group; R5 and R6 represent, independently of one another: substituted or unsubstituted C1-C15 alkyl; a substituted or unsubstituted aryl or arylalkyl group; an L1-W, L2-M, L2-A or L2-G group; X is chosen from: O, S or CR7R8; Y is chosen from: O, S or CR9R10; R7, R8, R9 and R10 independently represent: substituted or unsubstituted C1-C15 alkyl; substituted or unsubstituted aryl, arylalkyl or aryloxy; an L1-W, L2-M, L2-A or L2-G group; R7 and R8 and/or R9 and R10 can also together form a ring
    Type: Application
    Filed: March 7, 2008
    Publication date: June 10, 2010
    Applicant: CIS BIO INTERNATIONAL
    Inventor: Herve Bazin
  • Publication number: 20100136567
    Abstract: The invention provides a novel class of cyanine dyes that are functionalized with a linker moiety that facilitates their conjugation to other species. Also provided are conjugates of the dyes, methods of using the dyes and their conjugates and kits including the dyes and their conjugates.
    Type: Application
    Filed: January 5, 2010
    Publication date: June 3, 2010
    Applicant: Biosearch Technologies, Inc.
    Inventors: Tim Carter, Mark Reddington
  • Patent number: 7705150
    Abstract: The invention provides a novel class of cyanine dyes that are functionalized with a linker moiety that facilitates their conjugation to other species. Also provided are conjugates of the dyes, methods of using the dyes and their conjugates and kits including the dyes and their conjugates.
    Type: Grant
    Filed: February 4, 2005
    Date of Patent: April 27, 2010
    Assignee: Biosearch Technologies, Inc.
    Inventors: Tim Carter, Mark Reddington
  • Patent number: 7700765
    Abstract: There is provided an oligopeptide compound comprising: (a) at least one nitrogen-containing basic group attached to at least one end of the oligopeptide; and (b) two or more heterocyclic monomers, at least one of which is substituted in the heterocyclic part by a branched, cyclic or part cyclic C3-5 alkyl group, or a pharmaceutically acceptable salt or solvate thereof; which compound, salt or solvate binds to the minor groove of DNA.
    Type: Grant
    Filed: December 24, 2002
    Date of Patent: April 20, 2010
    Assignee: University of Strathclyde
    Inventors: Abedawn Khalaf, Roger Waigh, Colin Suckling
  • Patent number: 7683186
    Abstract: A phosphorus compound of formula (1): wherein R1 denotes a hydrogen atom or a hydroxy protective group; R2 denotes a group defined by the following formula (R2-1) or (R2-2); R3, R4, R5, and R6 may be the same or different and independently denote a hydrogen atom, an alkyl group, an alkoxy group, an acyloxy group, a halogen atom, a haloalkyl group, or a dialkylamino group; two among R3, R4, R5, and R6 may form an aromatic ring optionally having a substituent group, and two among R3, R4, R5, and R6 may form a methylene chain optionally having a substituent group or a (poly)methylenedioxy group optionally having a substituent group: wherein (R2-1) and (R2-2), R7 denotes an alkyl group, a cycloalkyl group, an aryl group, an alkoxy group, or an aryloxy group; R8 and R9 independently denote a hydrogen atom, an alkyl group, or an aryl group; z denotes a divalent group; and a denotes an integer of 0 or 1.
    Type: Grant
    Filed: December 7, 2007
    Date of Patent: March 23, 2010
    Assignees: National University Corporation Tokyo University of Agriculture and technology, Takasago International Corporation
    Inventors: Ken Tanaka, Wataru Kuriyama
  • Patent number: 7655691
    Abstract: Novel indole compounds are disclosed. Also disclosed are methods for using the compounds to treat human and animal disease, pharmaceutical compositions of the compounds, and kits including the compounds.
    Type: Grant
    Filed: September 27, 2005
    Date of Patent: February 2, 2010
    Inventors: Howard P. Sard, Louis Shuster, Bryan Roth, Cynthia Morency, Govindaraj Kumaran, Liang Xu
  • Patent number: 7655660
    Abstract: Prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group such as a piperazino carbamate, a 4-piperidino-piperidino carbamate or a phosphate, in which the protecting group confers enhanced water solubility and stability upon the prodrug, and in which the prodrug also has a moiety, such as a disulfide, that can conjugate to a cell binding reagent such as an antibody. The therapeutic use of such prodrug conjugates is also described; such prodrugs of cytotoxic agents have therapeutic use because they can deliver cytotoxic prodrugs to a specific cell population for enzymatic conversion to cytoxic drugs in a targeted fashion.
    Type: Grant
    Filed: January 5, 2007
    Date of Patent: February 2, 2010
    Assignee: Immunogen Inc.
    Inventors: Robert Yongxin Zhao, Ravi V. J. Chari
  • Publication number: 20090234136
    Abstract: A method of making a phosphono-substituted dipyrromethane comprises reacting an aldehyde or acetal having at least one phosphono group substituted thereon with pyrrole to produce a phosphono-substituted dipyrromethane; and wherein the phosphono is selected from the group consisting of dialkyl phosphono, diaryl phosphono, and dialkylaryl phosphono. Additional methods, intermediates and products are also described.
    Type: Application
    Filed: May 28, 2009
    Publication date: September 17, 2009
    Inventors: Jonathan S. Lindsey, Robert S. Loewe, Kannan Muthukumaran, Arounaguiry Ambroise
  • Publication number: 20090221820
    Abstract: Ligands for transition metals are disclosed herein, which may be used in various transition-metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The disclosed methods provide improvements in many features of the transition-metal-catalyzed reactions, including the range of suitable substrates, number of catalyst turnovers, reaction conditions, and efficiency. For example, improvements have been realized in transition-metal-catalyzed cross-coupling reactions.
    Type: Application
    Filed: December 12, 2008
    Publication date: September 3, 2009
    Applicant: Massachusetts Institute of Technology
    Inventors: Stephen L. Buchwald, Brett P. Fors, David S. Surry
  • Publication number: 20090208499
    Abstract: The present invention relates to an N-(phosphonoalkyl)-amino acid, a related compound or a derivative thereof, the N-(phosphonoalkyl)-amino acid, related compound or derivative thereof being in a form as a free acid, salt, partial salt, lactone, amide or ester, or in stereoisomeric or non-stereoisomeric form, other than N-(phosphonomethyl)-glycine or N,N-bis(phosphonomethyl)-glycine. Also included is a composition including an N-(phosphonoalkyl)-amino acid, a related compound or a derivative thereof in a form as a free acid, salt, partial salt, lactone, amide or ester, or in stereoisomeric or non-stereoisomeric form, and a cosmetically or pharmaceutically acceptable vehicle for topical or systemic administration to a mammalian subject, as well as a method of administering an effective amount of such a composition for alleviating or improving a condition, disorder, symptom or syndrome associated with at least one of a nervous, vascular, musculoskeletal or cutaneous system.
    Type: Application
    Filed: April 23, 2009
    Publication date: August 20, 2009
    Inventors: Ruey J. Yu, Eugene J. Van Scott
  • Publication number: 20090186855
    Abstract: The present invention relates to compounds and methods useful in the prevention or treatment of diseases or conditions associated with Toll-like receptor 2 activation.
    Type: Application
    Filed: April 1, 2009
    Publication date: July 23, 2009
    Applicant: Eisai R&D Management Co., Ltd.
    Inventors: Jesse Chow, Fabian Gusovksy, Lynn Hawkins, Mark Spyvee
  • Publication number: 20090167166
    Abstract: The present invention relates to compounds according to formula (1) and/or according to formulae (4) to (10) and their use in organic electroluminescent devices, in particular as a matrix material in phosphorescent devices.
    Type: Application
    Filed: May 21, 2007
    Publication date: July 2, 2009
    Applicant: MERCK PATENT GMBH
    Inventors: Ingrid Bach, Arne Buesing, Susanne Heun, Philipp Stoessel, Michael Holbach, Jonas Kroeber, Amir Hossain Parham
  • Publication number: 20090156556
    Abstract: Compounds of formula I: wherein R1, R2, n and m are as defined in the specification, processes for their production, their uses and pharmaceutical compositions containing them.
    Type: Application
    Filed: February 24, 2009
    Publication date: June 18, 2009
    Inventors: Rainer Albert, Eric Francotte, Frederic Zecri, Markus Zollinger
  • Patent number: 7528120
    Abstract: Compounds of formula I: wherein R1, R2, n and m are as defined in the specification, processes for their production, their uses and pharmaceutical compositions containing them.
    Type: Grant
    Filed: August 27, 2004
    Date of Patent: May 5, 2009
    Assignee: Novartis AG
    Inventors: Rainer Albert, Eric Francotte, Frédéric Zecri, Markus Zollinger
  • Publication number: 20090111998
    Abstract: There is provided processes for preparing carvedilol dihydrogen phosphate hemihydrate, which processes include at least one of the steps of: (a) providing a solution of carvedilol in a mixture of organic solvent (s) and/or water; (b) adding a phosphonating agent to the reaction mixture of step (a); and (c) further processing to obtain carvedilol dihydrogen phosphate hemihydrate. There is also provided pharmaceutical compositions comprising carvedilol dihydrogen phosphate hemihydrate and processes for their preparation.
    Type: Application
    Filed: October 24, 2008
    Publication date: April 30, 2009
    Inventors: Srinivas Reddy Gade, Srinivas Reddy Mallepalli
  • Publication number: 20090081158
    Abstract: Provided herein are phosphadiazine polymerase inhibitor, for example, of any of Formulas IV, IV?, I?, II?, or IVa, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
    Type: Application
    Filed: August 27, 2008
    Publication date: March 26, 2009
    Applicant: Idenix Pharmaceuticals, Inc.
    Inventors: Cyril Dousson, Dominique Surleraux, Jean-Laurent Paparin, Claire Pierra, Arlene Roland
  • Publication number: 20090047246
    Abstract: The embodiments provide compounds of the general Formula I, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.
    Type: Application
    Filed: February 11, 2008
    Publication date: February 19, 2009
    Applicant: InterMune, Inc.
    Inventors: Leonid Beigelman, Brad Buckman, Vladimir Serebryany, Guangyi Wang, Jasenka Matulic-Adamic, Antitsa Dimitrova Stoycheva, Steven W. Andrews, Shawn Maurice Misialek, P.T. Ravi Rajagopalan, Andrew M. Fryer, Indrani Gunawardana, Julia Haas, Lily Huang, Machender R. Madduru, Gan Zhang, Karl Kossen, Scott D. Seiwert, Lawrence M. Blatt
  • Publication number: 20090036409
    Abstract: The present invention is directed to a compound of formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof, and methods for treating inflammatory and serine protease mediated disorders.
    Type: Application
    Filed: August 20, 2008
    Publication date: February 5, 2009
    Inventors: Michael J. Hawkins, Michael N. Greco, Eugene Powell, Lawrence De Garavilla, Bruce E. Maryanoff
  • Publication number: 20090028925
    Abstract: The present invention relates to compounds of phosphonic acid-containing T3 mimetics and monoesters thereof, stereoisomers, pharmaceutically acceptable salts, co-crystals, and prodrugs thereof and pharmaceutically acceptable salts and co-crystals of the prodrugs, as well as their preparation and uses for preventing and/or treating metabolic diseases such as obesity, NASH, hypercholesterolemia and hyperlipidemia, as well as associated conditions such as atherosclerosis, coronary heart disease, impaired glucose tolerance, metabolic syndrome x and diabetes.
    Type: Application
    Filed: May 26, 2006
    Publication date: January 29, 2009
    Inventors: Mark D. Erion, Hongjian Jiang, Serge H. Boyer
  • Publication number: 20080318902
    Abstract: The present invention relates to novel Triheterocyclic Compounds, compositions comprising a Triheterocyclic Compound, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering a Triheterocyclic Compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or neoplastic cell, treating or preventing a viral infection, or inhibiting the replication and/or infectivity of a virus.
    Type: Application
    Filed: July 18, 2008
    Publication date: December 25, 2008
    Applicant: Gemin X Pharmaceuticals Canada Inc.
    Inventors: Giorgio Attardo, Jean-Francois Lavallee, Elise Rioux, Sasmita Tripathy, Terrence W. Doyle