Abstract: Novel compounds useful as chemotherapeutic and chemopreventive agents are provided. The compounds are analogs of indole-3-carbinol metabolites wherein the structures and substituents of the compounds are selected to enhance the compounds' overall efficacy, particularly with respect to therapeutic activity, oral bioavailability, long-term safety, patient tolerability, and therapeutic window. The compounds are useful not only in treatment of cancer but also in prevention of cancer. One preferred class of the novel compounds have the structure of formula (I)
wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12 are defined herein. Pharmaceutical compositions are provided as well, as are methods of synthesis and use.
Abstract: The invention provides a device for iontophoretically transporting a compound through a localized region of an individual's body tissue. The device comprises first and second iontophoretic electrodes, a reference electrode, a current source, and a monitoring means. The first electrode is placed in ion-conducting relation with the localized region to allow iontophoretic transport of a compound therethrough. The second and transport electrodes are each placed in contact with the individual's body tissue, and all electrodes are spaced apart from each other. The current source is electrically connected to the first and second electrodes and applies a current to the localized region of body tissue to effect iontophoretic transport. The monitoring means monitors the electrical resistance of the localized region by measuring any voltage difference between the reference electrode and the first and/or second electrodes.
Type:
Grant
Filed:
May 3, 2002
Date of Patent:
October 5, 2004
Assignee:
Aciont, Inc.
Inventors:
David J. Miller, William I. Higuchi, Kevin Li, Matthew S. Hastings
Abstract: A polymer blend is provided for use in a lithographic photoresist composition, particularly a chemical amplification photoresist. In a preferred embodiment, the polymer blend is substantially transparent to deep ultraviolet radiation, i.e., radiation of a wavelength less than 250 nm, including wavelengths of 157 nm, 193 nm and 248 nm, and has improved sensitivity and resolution. Processes for preparing and using the polymer blend are also provided, as are lithographic photoresist compositions that contain the polymer blend.
Type:
Grant
Filed:
March 4, 2002
Date of Patent:
September 21, 2004
Assignee:
International Business Machines Corporation
Inventors:
Gregory Breyta, Hiroshi Ito, Hoa D. Truong
Abstract: The invention is directed to the cross-metathesis and ring-closing metathesis reactions between geminal disubstituted olefins and terminal olefins, wherein the reaction employs a Ruthenium or Osmium metal carbene complex. Specifically, the invention relates to the synthesis of &agr;-functionalized or unfunctionalized olefins via intermolecular cross-metathesis and intramolecular ring-closing metathesis using a ruthenium alkylidene complex. The catalysts preferably used in the invention are of the general formula
wherein:
M is ruthenium or osmium;
X and X1 are each independently an anionic ligand;
L is a neutral electron donor ligand; and,
R, R1R6, R7, R8, and R9 are each independently hydrogen or a substituent selected from the group consisting of C1-C20 alkyl, C2-C20 alkenyl, C2-C20 alkynyl, aryl, C1-C20 carboxylate, C1-C20 alkoxy, C2-C20 alkenyloxy, C2-C20 alkynyloxy, aryloxy, C2-C20 alkoxycarbonyl, C1-C20 alkylthio, C1-C20 alkylsulfonyl and C1-C20 alkylsulfinyl.
Type:
Grant
Filed:
June 25, 2001
Date of Patent:
September 21, 2004
Assignee:
California Institute of Technology
Inventors:
Robert H. Grubbs, Arnab K. Chatterjee, John P. Morgan, Matthias Scholl, Tae-Lim Choi
Abstract: Syntheses of steroids such as 3-hydroxy-7&agr;-methyl-21-[2′-methoxy-4′-(diethylaminomethyl)-phenoxy]-19-norpregna-1,3,5(10)triene citrate (“SR 16234”) and analogs thereof are provided, wherein 21-hydroxy-19-norpregna-4-en-3-one serves as a starting material or intermediate. The latter compound may be readily prepared from estrone-3-methyl ether. Certain intermediates in these syntheses also have value as therapeutic agents, for example in the treatment of prostate disorders such as prostatic cancer.
Type:
Grant
Filed:
February 9, 2001
Date of Patent:
August 31, 2004
Assignee:
SRI International
Inventors:
Richard H. Peters, Jyanwei Liu, John G. Johansson, Kenneth J. Ryan, Wan-Ru Chao, Masato Tanabe
Abstract: Europium-containing fluorescent nanoparticles and methods of preparing such nanoparticles are provided. The nanoparticles are comprised of an aluminum oxide framework having a europium activator, a magnesium, calcium, strontium, or barium energy reservoir, and at least one co-activator selected from the group consisting of scandium, yttrium, and certain lanthanide elements. The nanoparticles may be optionally coated with a silane coating containing reactive functional groups that allow for attachment of the nanoparticle to a desired biological or chemical target molecule. The coated nanoparticles may be used to detect a variety of protein ligand interactions, and may also be used in assays for nucleic acids.
Abstract: Nonmetallic organic catalysts are provided that facilitate the enantioselective reaction of &agr;,&bgr;-unsaturated aldehydes. The catalysts are chiral imidazolidinone compounds having the structure of formula (IIA) or (IIB)
or are acid addition salts thereof, wherein, in one preferred embodiment, R1 is C1-C6 alkyl, R2 is tri(C1-C6 alkyl)-substituted methyl, R3 and R4 are hydrogen, and R5 is phenyl optionally substituted with 1 or 2 substituents selected from the group consisting of halo, hydroxyl, and C1-C6 alkyl. The chiral imidazolidinones are useful in catalyzing a wide variety of reactions, including cycloaddition reactions, Friedel-Crafts alkylation reactions, and Michael additions.
Abstract: A method is disclosed for providing a patterned surface wherein predetermined regions of the surface are masked with a self-assembled monolayer (“SAM”) covalently bound to a brush polymer overlayer. The remainder of the substrate surface will generally be functionalized with a second self-assembled monolayer. Preferably, the method involves a microcontact printing technique, wherein a molecular moiety capable of spontaneously forming an SAM upon transfer to a surface is “stamped” onto a substrate surface, followed by growth (or covalent attachment) of a polymer on exposed functional groups within the SAM molecules. Coverage of surface regions with both an SAM and a polymer overlayer provides a number of advantages, particularly with regard to surface masking during etching and the like. The method is useful in the manufacture of microelectronic circuitry, biosensors, high-density assay plates, and the like.
Type:
Grant
Filed:
February 11, 2002
Date of Patent:
August 24, 2004
Assignees:
International Business Machines Corporation, The Regents of the University of California
Inventors:
Craig Jon Hawker, James Lupton Hedrick, Nicholas Abbott
Abstract: The present invention features novel methods and compositions for coating textile substrates, wherein the coating compositions are composed of a coating agent selected from one of (a) an azetidinium polymer, (b) a guanidine polymer, (c) a mixture of an azetidinium polymer and a guanidine polymer, and (d) a copolymer of an azetidinium monomer and a guanidine monomer. Textile substrates coated with the compositions provide high quality printed images when printed with an ink containing a reactive dye having ionizable and/or nucleophilic groups capable of reacting with the coating agent in the textile coating composition. Images printed on a textile substrate coated with a coating composition of the invention are bleed-resistant, water-resistant (e.g., water-fast), detergent-resistant (e.g., detergent-fast), and/or are characterized by an enhanced chroma and hue.
Abstract: Compositions and methods are provided for improving the quality of images printed on a substrate. The novel image-enhancing compositions contain as an image-enhancing agent (a) an azetidinium polymer, (b) a guanidine polymer, (c) a mixture of an azetidinium polymer and a guanidine polymer, or (d) a copolymer of an azetidinium monomer and a guanidine monomer. When applied to a substrate, the compositions provide for high quality printed images when the treated substrate is printed on with an ink containing a reactive dye capable of reacting with the image-enhancing agent. Images printed on a substrate treated with the image-enhancing compositions of the invention are water-resistant (e.g., water-fast), bleed-resistant, rub-resistant, and/or are characterized by an enhanced chroma and hue.
Abstract: Novel anti-estrogenic compounds are provided which are useful to treat a variety of disorders, particularly estrogen-dependent disorders. Preferred compounds have a 1,3,5-estratriene nucleus, and are substituted at the C-17 or C-11 position with a molecular moiety which renders the compounds effective to competitively block the binding of estrogen to its receptor. Particularly preferred compounds are 17-desoxy-1,3,5-estratrienes. Therapeutic methods and pharmaceutical compositions are provided as well.
Type:
Grant
Filed:
December 19, 2002
Date of Patent:
June 8, 2004
Assignee:
SRI International
Inventors:
Masato Tanabe, Richard H. Peters, Wan-Ru Chao, Ling Jong
Abstract: The present invention provides a unique and highly accurate method for generating molecular arrays of very high density on porous surfaces. The method involves the application of focused acoustic energy to each of a plurality of fluid-containing reservoirs to eject a small fluid droplet—on the order of 1 picoliter or less—from each reservoir to a site on a porous substrate surface. High density molecular arrays are provided as well, in which greater than about 62,500 molecular moieties, serving as array elements, are present on a porous surface. Biomolecular arrays that can be generated using focused acoustic ejection include oligonucleotide arrays and peptidic arrays.
Type:
Grant
Filed:
September 25, 2001
Date of Patent:
June 8, 2004
Assignee:
Picoliter Inc.
Inventors:
Richard N. Ellson, Mitchell W. Mutz, James K. Foote
Abstract: A method for preparing a wide range of substituted poly(aniline)s from a single precursor is described. The method uses a variety of reactions, including a boron activation/electrophilic displacement reaction resulting in ipso-substitution. The ability to tune the properties of poly(aniline) through the generation of new structures is useful in numerous fields ranging from polymer-based electronics to sensors.
Abstract: The invention relates to microfluidic devices and methods that employ electromagnetic radiation to move a droplet of fluid on a fluid-transporting surface of a substrate. Typically, radiation of a particular wavelength is directed through a substantially transparent material, and the radiation imparts an optical trapping force to move the droplet. In addition, a means for reducing evaporative loss from the droplet may be provided.
Type:
Grant
Filed:
August 7, 2002
Date of Patent:
May 11, 2004
Assignee:
SRI International
Inventors:
Gregory W. Faris, John S. Bashkin, William H. Wright, Richard P. Heydt, David MacQueen
Abstract: A lithographic photoresist composition is provided that can be used as a chemical amplification photoresist. In a preferred embodiment, the composition is substantially transparent to deep ultraviolet radiation, i.e., radiation of a wavelength less than 250 nm, including 157 nm, 193 nm and 248 nm radiation, and has improved sensitivity and resolution. The composition comprises a fluorinated vinylic polymer, particularly a fluorinated methacrylate, a fluorinated methacrylonitrile, or a fluorinated methacrylic acid, and a photoacid generator. The polymer may be a homopolymer or a copolymer. A process for using the composition to generate resist images on a substrate is also provided, i.e., in the manufacture of integrated circuits or the like.
Type:
Grant
Filed:
January 26, 2001
Date of Patent:
May 4, 2004
Assignee:
International Business Machines Corporation
Inventors:
Phillip Joe Brock, Daniel Joseph Dawson, Hiroshi Ito, Gregory Michael Wallraff
Abstract: The invention provides conjugated polymers that have good solubility and semiconductivity, and that display high photoluminescent and electroluminescent efficiency.
Abstract: The present invention features processes and compositions for producing a metallic-looking image on a substrate having a reflective or luminescent surface. The process utilizes an opaque coating composition containing an opaque coating agent comprising a mixture of a polyacid and a polybase. When applied to a light-emitting, reflective or luminescent substrate, the opaque coating composition at least partially masks the light-emitting reflective or luminescent surface of the substrate, but becomes increasingly translucent or transparent when contacted with a recording liquid such as an ink, revealing the light-emitting, reflective or luminescent surface.
Abstract: This invention relates to processes for making phosphorus compounds R2P—X—PR2, R2P-M, R2P-L and R3P, and the novel cation R2P+(L)-X—P+(L)R2, where R represents an optionally substituted hydrocarbyl group, X represents a bridging group, L represents a leaving group and M represents an alkali metal atom. The invention relates further to a process for making a compound R2P-L from a compound R—H via a new process for making the compound R—Li followed by its reaction with a compound Hal2P-L. The compound R2P—X—PR2 is a ligand suitable for making catalysts for copolymerizing carbon monoxide and a olefinically unsaturated compound.
Type:
Grant
Filed:
January 15, 2003
Date of Patent:
April 13, 2004
Assignee:
SRI International
Inventors:
Roelof Van Ginkel, Alexander Van Der Made, Jan De With, Wolf Eilenberg
Abstract: Methods, compositions and drug delivery systems are provided for the transdermal administration of a pharmacologically active amine. The active agent is administered with a hydroxide-releasing agent that serves as a permeation enhancer. Exemplary hydroxide-releasing agents are inorganic hydroxides, inorganic oxides, and alkali metal or alkaline earth metal salts of weak acids. Inorganic hydroxides include, for example, ammonium hydroxide, alkali metal hydroxides and alkaline earth metal hydroxides, such as sodium hydroxide, calcium hydroxide, potassium hydroxide, magnesium hydroxide, and the like.
Type:
Grant
Filed:
December 14, 2000
Date of Patent:
April 13, 2004
Assignee:
Dermatrends, Inc.
Inventors:
Tsung-Min Hsu, Russell Macy, Eric C. Luo
Abstract: The invention relates to a method for shaping small three-dimensional articles such as nanotube exhibiting a layered structure through material removal such that the article is controllably shaped to exhibit a desired contour. Typically, material removal does not require use of a chemical etchant and is carried out while the article and a shaping electrode are positioned in contact material removal relationship with under a potential difference. The invention also relates to nanotubes and small three-dimensional articles exhibiting a layered structure having a controllably shaped contour.
Type:
Grant
Filed:
July 24, 2001
Date of Patent:
March 23, 2004
Assignee:
The Regents of the University of California