Azides Patents (Class 552/1)
  • Patent number: 11161812
    Abstract: Disclosed are novel processes for the production of cyclic imide compounds such as N-hydroxyphthalimide (NHPI). The processes may be particularly well-suited for commercial-scale production of cyclic imides such as NHPI. Such cyclic imide compounds are suitable for use as oxidation catalysts, and specifically may be used to oxidize cyclohexylbenzene to cyclohexyl-1-phenyl-1-hydroperoxide. Such an oxidation may be particularly useful in a process for the production of phenol and/or cyclohexanone from benzene via a process comprising hydroalkylation of benzene to cyclohexylbenzene, oxidation of the cyclohexylbenzene to cyclohexyl-1-phenyl-1-hydroperoxide, and cleavage of the cyclohexyl-1-phenyl-1-hydroperoxide to phenol and cyclohexanone. The cyclic imide production process may advantageously include water washing and reactant recovery steps to maximize purity and yield.
    Type: Grant
    Filed: April 18, 2017
    Date of Patent: November 2, 2021
    Assignee: ExxonMobil Chemical Patents Inc.
    Inventors: Jörg F. W. Weber, Helge Jaensch, Andrew R. Witt, Christopher L. Becker, Kirk C. Nadler, Kendele S. Galvan, Amy B. Batton
  • Patent number: 10414844
    Abstract: The present invention pertains to semi-crystalline fluoropolymer [polymer (F)] comprising: —recurring units derived from vinylidene fluoride (VDF); —from 10% to 50% by moles [with respect to the total moles of recurring units of polymer (F)] of recurring units derived from trifluoroethylene (TrFE); and —from 0.01% to 10% by moles [with respect to the total moles of recurring units of polymer (F)] of recurring units derived from at least one monomer comprising an azide group [monomer (Az)], to a process for its manufacture, to a crosslinkable composition comprising the same, to a process for crosslinking the same and to a method for manufacturing one of electrical and electronic devices using the same.
    Type: Grant
    Filed: December 6, 2012
    Date of Patent: September 17, 2019
    Assignee: SOLVAY SPECIALTY POLYMERS ITALY S.P.A.
    Inventors: Alessio Marrani, Ivan Wlassics, Vito Tortelli, Ivan Falco
  • Patent number: 10392344
    Abstract: The present invention relates to a method for labelling fluorine-18, which is a radioisotope, and more specifically, to a method for labelling a [18F]fluoride in a method for preparing an organic [18F]fluoro compound by reacting an alkyl halide or an alkyl sulfonate with a [18F]fluoride, wherein a [18F]fluoride supported on a quaternary alkyl ammonium polymer support is eluted using a solution containing a metal salt or a quaternary ammonium salt with an adjusted pH, and a base is not additionally used. The present invention enables a labeling reaction without an additional base after precisely reflecting the concentration of a base absolutely necessary for the nucleophilic substitution of a [18F]fluoride or eluting a [18F]fluoride using a [18F]fluoride eluent with an adjusted pH, thereby stably obtaining a [18F]fluoride-labelled compound in a high yield, and is thus useful for production of fluorine-18-labelled radioactive medical supplies.
    Type: Grant
    Filed: December 21, 2012
    Date of Patent: August 27, 2019
    Assignee: THE ASAN FOUNDATION
    Inventors: Sang Ju Lee, Seung Jun Oh, Dae Hyuk Moon, Jin Sook Ryu, Jae Seung Kim, Jong Jin Lee
  • Patent number: 8946391
    Abstract: The present invention provides for a practical, universal and efficient method to ligate two large macromolecules (e.g., proteins) using the alkyne-azide 1,3-dipolar cycloaddition reaction to produce a conjugated macromolecule, such as a multivalent scFv. The present invention also provides for conjugate macromolecules comprising a plurality of macromolecule components cross-linked through at least one linking group comprising at least one 1,2,3-triazole moiety, wherein at least 50 percent of the macromolecule components in the conjugate macromolecule has only one site available for cross-linking.
    Type: Grant
    Filed: March 26, 2007
    Date of Patent: February 3, 2015
    Assignee: The Regents of the University of California
    Inventors: Jacquelyn Gervay-Hague, Wenjun Du, Sally Denardo, Arutselvan Natarajan
  • Patent number: 8921571
    Abstract: Several different pyrrolysine analogs are disclosed in this application. Those analogs have distinct chemical and biophysical properties. Some analogs are useful in chemical ligation applications. Methods of making and using are also disclosed.
    Type: Grant
    Filed: October 6, 2010
    Date of Patent: December 30, 2014
    Assignee: The Ohio State University
    Inventors: Michael K. Chan, Tomasz Fekner, Xin Li, Marianne Lee, Manoj Nair, Jennifer Jo Ottensen
  • Publication number: 20140256970
    Abstract: A stacked reactor vessel provides two separate reaction vessel compartments for performing chemical reactions and is particularly suited to multi-step chemical reactions and for incorporation into a cassette for automated operation.
    Type: Application
    Filed: September 28, 2012
    Publication date: September 11, 2014
    Applicant: GE HEALTHCARE LIMITED
    Inventor: Alexander Jackson
  • Patent number: 8779194
    Abstract: The present invention relates to carbamoylation of amines, mercaptanes, thiophenols and phenols employing organic azides. More specifically, the invention relates to a method for generating urea derivatives, thiocarbamate derivatives and carbamate derivatives, and is based on the intermediate formation of isocyanate, starting from an organic azide. The reaction as described is useful in applications for modified nucleoside synthesis, oligonucleotide synthesis, as well as modification, labeling and conjugation of polymers and biomolecules.
    Type: Grant
    Filed: October 25, 2007
    Date of Patent: July 15, 2014
    Assignee: Metkinen Chemistry Oy
    Inventors: Andrey Yagodkin, Alex Azhayev
  • Publication number: 20140121187
    Abstract: Disclosed are 1,3-Dioxoindene derivatives, pharmaceutically acceptable salts thereof or enantiomers, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of viral diseases, comprising the same as an active ingredient. The 1,3-Dioxoindene derivatives have excellent inhibitory activity against picornaviruses including coxsackie-, entero-, echo-, Polio-, and rhinoviruses, as well as exhibiting low cytotoxicity, so that they can be useful as an active ingredient of a pharmaceutical composition for the prevention or treatment of viral diseases including poliomyelitis, paralysis, acute hemorrhagic conjunctivitis, viral meningitis, hand-foot-and-mouth disease, vesicular disease, hepatitis A, myositis, myocarditis, pancreatitis, diabetes, epidemic myalgia, encephalitis, flu, herpangina, foot-and-mouth disease, asthma, chronic obstructive pulmonary disease, pneumonia, sinusitis or otitis media.
    Type: Application
    Filed: June 18, 2012
    Publication date: May 1, 2014
    Applicants: KATHOLIEKE UNIVERSITEIT LEUVEN K.U. LEUVEN R & D, KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
    Inventors: Young Sik Jung, Chong Kgo Lee, Ihl Young Choi, Hae Soo Kim, Pil Ho Kim, Soo Bong Han, Johan Neyts, Hendrik Jan Thibaut
  • Publication number: 20140106979
    Abstract: Polymers having orthogonal reactive groups and solid supports comprising polymers immobilized thereto are provided. The polymers find utility in any number of applications including immobilizing analyte molecules to solid supports for high throughput assays.
    Type: Application
    Filed: October 11, 2013
    Publication date: April 17, 2014
    Applicant: NVS Technologies, Inc.
    Inventors: Aldrich N. K. Lau, Robert G. Eason
  • Patent number: 8680260
    Abstract: The present invention provides an 18F-labeled azide compound usable in the Huisgen reaction which enables 18F-labeling although only a small quantity of alkyne compound is available as a counterpart substrate, more specifically the 18F-labeled azide compound enabling the PET to be applied to peptides or oligonucleotides and enabling the 18F-labeling of any sites of oligonucleotide other than the 5? end or 3? end thereof, a reagent for 18F-labeling, and a method for 18F-labeling of an alkyne compound using the same.
    Type: Grant
    Filed: May 14, 2010
    Date of Patent: March 25, 2014
    Assignee: Riken
    Inventors: Yasuyoshi Watanabe, Masaaki Suzuki, Hisashi Doi, Takeshi Kuboyama, Satoshi Obika, Takeshi Imanishi
  • Patent number: 8592565
    Abstract: The invention relates to carbon surfaces modified with one or more azide groups. The invention also relates to methods of modifying carbon surfaces with one or more azide groups.
    Type: Grant
    Filed: January 10, 2008
    Date of Patent: November 26, 2013
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Christopher E. D. Chidsey, Anando Devadoss, Neal K. Devaraj
  • Publication number: 20120203102
    Abstract: This invention is directed to non-benzenoid aromatic compounds. Other aspects include methods of using non-benzenoid aromatic compounds for imaging and phototherapeutic uses thereof. Non-benzenoid compounds provided herein generally have one or more substituent groups which allow tailoring of the spectral properties or provide photoreactivity or targeting ability.
    Type: Application
    Filed: September 10, 2010
    Publication date: August 9, 2012
    Applicant: MALLINCKRODT LLC
    Inventor: Raghavan Rajagopalan
  • Publication number: 20120035369
    Abstract: The problem to be solved is to provide an important intermediate for production of an FXa inhibitor. The solution thereto is a method for industrially producing a compound (1) or a compound (4), comprising: [Step 1]: adding a quaternary ammonium salt and a metal azide salt to water to prepare an aqueous solution of an azidification reagent complex comprising quaternary ammonium salt-metal azide salt, and subsequently dehydrating the aqueous solution using an aromatic hydrocarbon solvent to form a mixed solution of the azidification reagent complex comprising quaternary ammonium salt-metal azide salt and the aromatic hydrocarbon solvent with a water content of 0.2% or less; and [Step 2]: adding, to the mixed solution prepared in [Step 1], a compound (2) wherein L represents a leaving group.
    Type: Application
    Filed: September 13, 2011
    Publication date: February 9, 2012
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventor: Koutarou Kawanami
  • Publication number: 20110306088
    Abstract: A honeycomb body is disclosed having cells extending along a common direction, a first plurality of the cells being open at both ends of the body and a second plurality of the cells being closed at one or both ends of the body, the second plurality of cells arranged in one or more groups of cells cooperating to define one or more fluid passages extending through the body at least in part perpendicularly to the common direction, wherein, in a plane perpendicular to the common direction, the ratio of the area of cells of the first plurality to the area of cells of the second plurality varies along the length of at least one of the one or more fluid passages.
    Type: Application
    Filed: February 26, 2010
    Publication date: December 15, 2011
    Inventors: Peng Chen, Yi Jiang, James Scott Sutherland, Andrew David Woodfin
  • Publication number: 20110201577
    Abstract: The present application relates to processes for the preparation of oseltamivir and the H3PO4 salt of oseltamivir, Tamiflu®. The application further relates to novel intermediate compounds and to pharmaceutical compositions containing said compounds. The application further relates to a method of using the novel intermediates to treat or prevent influenza.
    Type: Application
    Filed: May 12, 2009
    Publication date: August 18, 2011
    Applicant: BROCK UNIVERSITY
    Inventors: Tomas Hudlicky, Bradford Sullivan
  • Publication number: 20110184196
    Abstract: The invention relates to carbon surfaces modified with one or more azide groups. The invention also relates to methods of modifying carbon surfaces with one or more azide groups.
    Type: Application
    Filed: January 10, 2008
    Publication date: July 28, 2011
    Applicant: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Christopher E.D. Chidsey, Anando Devadoss, Neal K. Devaraj
  • Publication number: 20110112293
    Abstract: The present invention provides novel and advantageous processes for preparing and purifying chemical compounds such as pharmaceuticals. The processes comprise a nucleophilic substitution reaction with a moiety X wherein the leaving group L of a substrate S in the reaction is covalently attached to a purification moiety M. This concept offers a convenient and lime-saving way to purity the desired product S-X from non-reacted precursors S-L-M and by-products L-M.
    Type: Application
    Filed: April 9, 2009
    Publication date: May 12, 2011
    Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
    Inventors: John Cyr, Ananth Srinivasan, Mathias Berndt, Keith Graham, Dae Yoon Chi, Byoung Se Lee, So Young Chu, Song-Yi Lim, Sang Ju Lee, Jin-Sook Ryu, Seung Jun Oh
  • Patent number: 7605191
    Abstract: The invention provides a photosensitive resin which can readily form, through photo-crosslinking, a surface coating which has hydrophilicity and high bioadaptability; a photosensitive composition containing the photosensitive resin; and a photo-crosslinked structure obtained from the photosensitive composition.
    Type: Grant
    Filed: March 31, 2006
    Date of Patent: October 20, 2009
    Assignee: Toyo Gosei Co., Ltd.
    Inventors: Takeshi Ikeya, Toru Shibuya, Kana Miyazaki
  • Publication number: 20090105491
    Abstract: The invention is directed to a process for producing intermediates of a compound which exhibits an activated blood coagulation factor Xa inhibitory action and which is a useful preventive and a therapeutic agent for thrombotic diseases. The intermediate production process is represented by the following reaction scheme.
    Type: Application
    Filed: September 15, 2006
    Publication date: April 23, 2009
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Koji Sato, Kotaro Kawanami, Tsutomu Yagi
  • Patent number: 7385068
    Abstract: An improved alkaline earth metal stearate composition is disclosed and is prepared by reacting a fatty acid component including stearic acid and palmitic acid with an alkali hydroxide to form an alkaline soap. An aqueous metal salt solution is then added to the soap, and pH adjusted to less than about pH 8 to form the improved alkaline earth metal stearate. The improved alkaline earth metal stearate provides a substantially pure amount of the dihydrate form of the stearate.
    Type: Grant
    Filed: June 16, 2005
    Date of Patent: June 10, 2008
    Assignee: Mallinckrodt Inc.
    Inventors: Todd P. Heider, Steven M. Wolfgang, Scot R. Randle
  • Publication number: 20070238710
    Abstract: This invention concerns N-(ortho phenylaminoaryl), N?-alkyl sulfamides which are inhibitors of MEK and are useful in the treatment of cancer and other hyperproliferative diseases.
    Type: Application
    Filed: April 11, 2007
    Publication date: October 11, 2007
    Applicant: ARDEA BIOSCIENCES
    Inventors: Shunqi Yan, Jean-Michel Vernier, Zhi Hong
  • Patent number: 7070941
    Abstract: The invention provides methods and compositions for azide tagging of biomolecules. In one embodiment of the invention, proteins are tagged by metabolic incorporation of prenylated azido-analog substrates. Examples of such analogs are azido farnesyl diphosphate and azido farnesyl alcohol. The azido moiety in the resulting modified proteins provides an affinity tag, which can be chemoselectively captured by an azide-specific conjugation reaction, such as the Staudinger reaction, using a phosphine capture reagent. When the capture agent is biotinylated, the resulting conjugates can be detected and affinity-purified by streptavidin-linked- HRP and streptavidin-conjugated agarose beads, respectively. The invention allows detection and isolation of proteins with high yield, high specificity, and low contamination without harsh treatment of proteins.
    Type: Grant
    Filed: November 17, 2003
    Date of Patent: July 4, 2006
    Assignee: Board of Regents, The University of Texas System
    Inventors: Yingming Zhao, John R. Falck
  • Patent number: 6962633
    Abstract: A novel family of amine azides having a cyclic structure therein is disclosed. These compounds have attractive properties as rocket propellants.
    Type: Grant
    Filed: March 18, 2003
    Date of Patent: November 8, 2005
    Assignee: The United States of America as represented by the Secretary of the Army
    Inventor: Michael J. McQuaid
  • Patent number: 6861456
    Abstract: The present invention provides a novel photosensitive compound having an azido group suitable for exposure to light of a short wavelength; a photosensitive resin containing the photosensitive compound; and a photosensitive composition containing the photosensitive compound or photosensitive resin. The photosensitive compound containing a photosensitive unit represented by formula (1): wherein R is selected from among the following groups, R: X is selected from among the following groups, X: and each of Y and Z represents a hydrogen atom, an alkyl group, an acetal-group-containing alkyl group, an aryl group, an aralkyl group, or a substituent containing a base-forming nitrogen atom, wherein at least one of R and X contains an azido group.
    Type: Grant
    Filed: March 27, 2003
    Date of Patent: March 1, 2005
    Assignee: Toyo Gosei Kogyo Co., Ltd.
    Inventors: Toru Shibuya, Masanori Kurihara, Mineko Takeda, Kazuo Yamada
  • Publication number: 20040236131
    Abstract: A method for preparing organic products from aqueous solutions, such as waste or byproduct liquid streams and waste or byproduct gas or vapor streams, uses phase transfer catalysis to transfer a chemical species in low concentration from the aqueous solution to the organic phase or the aqueous-organic interface. The system has little or no organic solvent, and the organic phase contains an electrophile which participates in the reaction. In one embodiment, the aqueous solution is contacted with the electrophile and a phase transfer catalyst and, optionally, a pH adjusting agent in the event that the chemical species in the aqueous solution is not sufficiently ionized to react with the electrophile, and optionally an organic solvent. A method for continuously converting a chemical species involves this contacting step, separating the phases, then dividing the organic phase into the product, the phase transfer catalyst, and the optional organic solvent.
    Type: Application
    Filed: June 29, 2004
    Publication date: November 25, 2004
    Inventors: Peter J. Joyce, Roman Bielski, Marc Halpern
  • Publication number: 20040214999
    Abstract: The present invention relates to a chemical compound comprising a light emitting moiety precursor and a precursor of a leaving group, bound to each other by an amide or by an ester bond and characterized in that the leaving group precursor upon oxidation is converted into the leaving group. The invention also relates to compounds additionally comprising a coupling group to the use of such compounds for labeling of biomolecules and more generally to the use of such compounds in chemiluminescence detection procedures.
    Type: Application
    Filed: June 14, 2004
    Publication date: October 28, 2004
    Inventors: Dieter Heindl, Rupert Herrmann, Hans-Peter Josel, Erasmus Huber, Ursula Klause
  • Publication number: 20040180864
    Abstract: The present invention discloses novel aromatic azide derivatives and their bioconjugates for phototherapy of tumors and other lesions. The organic azides of the present invention are designed to absorb low-energy ultraviolet, visible, or near-infrared (NIR) region of the electromagnetic spectrum. The phototherapeutic effect is caused by direct interaction of nitrene, the reactive intermediate produced upon photoexcitation of the aromatic azide, with the tissue of interest. The compounds of the present invention are administered to a patient, allowed to accumulate at the site of the tumor or other lesion, and are exposed to light in order to perform a phototherapeutic procedure.
    Type: Application
    Filed: March 24, 2004
    Publication date: September 16, 2004
    Applicant: MALLINCKRODT INC.
    Inventors: Raghavan Rajagopalan, Gary Cantrell, Samuel I. Achilefu, Joseph E. Bugai, Richard B. Dorshow
  • Publication number: 20040176331
    Abstract: The invention encompasses novel compounds of Formula I, which are nitric oxide-releasing prodrugs of diaryl-2-(5H) furanones useful in the treatment of cyclooxygenase-2 mediated diseases.
    Type: Application
    Filed: March 1, 2004
    Publication date: September 9, 2004
    Inventors: Carl Berthelette, Lianhai Li, Claudio Sturino, Zhaoyin Wang
  • Publication number: 20040142983
    Abstract: Disclosed are nitrone compounds and pharmaceutical compositions containing such compounds. The nitrone compounds have one to six additional carbons bridging between the nitrone functionality and the nitrone aryl ring. The disclosed compositions are useful as therapeutics for inflammation-related conditions and analgesia in mammals, such as arthritis, and for neuropathic pain and traumatic injuries such as traumatic brain injury and acute spinal cord injury.
    Type: Application
    Filed: October 14, 2003
    Publication date: July 22, 2004
    Inventors: M. Amin Khan, Ravindra B. Upasani, Paul L. Wood
  • Publication number: 20040116408
    Abstract: The present invention is generally drawn to novel isolated therapeutic agents, termed resolving, generated from the interaction between a dietary omega-3 polyunsaturated fatty acid (PUFA) such as eicosapentaenoic acid (EPA) or docosahexaenoic acid (DHA), cyclooxygenase-II (COX-2) and an analgesic, such as aspirin (ASA). Surprisingly, careful isolation of compounds generated from the combination of components in an appropriate environment provide di- and tri-hydroxy EPA or DHA compounds having unique structural and physiological properties. The present invention therefore provides for many new useful therapeutic di- or tri-hydroxy derivatives of EPA or DHA (resolvins) that diminish, prevent, or eliminate inflammation or PMN migration, for example. The present invention also provides methods of use, methods of preparation, and packaged pharmaceuticals for use as medicaments for the compounds disclosed throughout the specification.
    Type: Application
    Filed: August 12, 2003
    Publication date: June 17, 2004
    Inventor: Charles N. Serhan
  • Publication number: 20040110730
    Abstract: Reagents and methods are provided for crosslinking and immobilizing biomolecules, drugs and synthetic polymers. The reagents possess (i) a thiol or amino reactive group; and (ii) a hydrazino or oxyamino moiety. Conjugates and immobilized biomolecules are also provided.
    Type: Application
    Filed: November 24, 2003
    Publication date: June 10, 2004
    Inventor: David A. Schwartz
  • Publication number: 20040092489
    Abstract: Polysubstituted indan-1-ol compounds, methods for their preparation; and methods for their use are disclosed herein.
    Type: Application
    Filed: October 27, 2003
    Publication date: May 13, 2004
    Applicant: Aventis Pharma Deutschland GmBH
    Inventors: Gerhard Jaehne, Volker Krone, Martin Bickel, Matthias Gossel
  • Publication number: 20040010154
    Abstract: The invention relates to a novel process of diastereoselective hydrogenation of 1,3-hydroxyketones of formula (I) 1
    Type: Application
    Filed: July 2, 2003
    Publication date: January 15, 2004
    Inventors: Martin Studer, Stephan Burkhardt, Ulrike Nettekoven
  • Patent number: 6664272
    Abstract: The present invention is directed to curcumin analogs exhibiting anti-tumor and anti-angiogenic properties, pharmaceutical formulations including such compounds and methods of using such compounds.
    Type: Grant
    Filed: December 4, 2000
    Date of Patent: December 16, 2003
    Assignee: Emory University
    Inventors: James P. Snyder, Matthew C. Davis, Brian Adams, Mamoru Shoji, Dennis C. Liotta, Eva M. Ferstl, Ustun B. Sunay
  • Publication number: 20030215876
    Abstract: The present invention provides compositions and methods to facilitate the identification of compounds that are capable of interacting with a biological macromolecule of interest. In one aspect, a composition is provided that comprises an array of one or more types of chemical compounds attached to a solid support, wherein the density of the array of compounds is at least 1000 spots per cm2. In particularly preferred embodiments, these compounds are attached to the solid support through a covalent interaction.
    Type: Application
    Filed: February 20, 2003
    Publication date: November 20, 2003
    Inventors: Seung Bum Park, David Barnes-Seeman, Angela N. Koehler, Stuart L. Schreiber
  • Publication number: 20030216586
    Abstract: The invention concerns bi-aromatic compounds of formula (I) in which Ar represents (a), Z being O or S, R1 is CH3, —CH2—O—R6, —OR6 or —COR7; R2 is —OR8, —SR8 or a polyether radical if in the latter case R4 is C1-C20alkyl and is in ortho or meta position relative to X—Ar: R3 is alkyl or R2 and R3 together form a cycle optionally interrupted by O or S, R4 is aryl radical; R5 is H, halogen, C1-C20 alkly or —OR8; R6 is H, alkyl or —COR9; R7 is H, alkyl, —N(r′)(r″) or —OR10; R8 is H, alkyl or —COR9; R9 is alkyl; R10 is H, C1-C20 alkyl, alkenyl, monohydroxyalkyl or polyhydroxyalyl, aryl or aralkyl or a sugar residue, r′ and r″ are H, alkyl mono- or polyhydroxyalkyl, aryl, an amino acid or sugar residue or together form a heterocycle, X represents a radical of formula (d) or (e) in which R11 is H or —OR6; R12 is H or alkyl; or R11 and R12 form an oxo radical, and the salts, optical and geometrical isomers of t
    Type: Application
    Filed: October 31, 2001
    Publication date: November 20, 2003
    Applicant: Galderma Research & Development
    Inventors: Jean-Michel Bernardon, Simon Trouille
  • Publication number: 20030158421
    Abstract: The invention relates to a method for the 1,3 dipolar cycloaddition of organic compounds, characterised in that the reaction is carried out in a microreactor.
    Type: Application
    Filed: April 18, 2003
    Publication date: August 21, 2003
    Inventors: Hanns Wurziger, Joeran Stoldt, Guido Pieper, Norbert Schwesinger
  • Patent number: 6590071
    Abstract: The present invention provides lipidized conjugates comprising an amino group-containing biologically active substance and a lipophilic group capable of penetrating a biological membrane. Under neutral or mildly acidic conditions, including those found in vivo, the free amino group-containing biologically active substance is released from the conjugate by hydrolysis of an amide bond. The present invention is also directed to methods of preparing lipidizing agents and lipidized conjugates, pharmaceutical compositions comprising lipidized conjugates and methods of increasing the delivery of amino group-containing substances into a cell. Preferred amino group-containing substances include peptides, proteins and derivatives thereof.
    Type: Grant
    Filed: December 9, 1999
    Date of Patent: July 8, 2003
    Assignee: University of Southern California
    Inventors: Wei-Chiang Shen, Hashem Heiati
  • Publication number: 20030083269
    Abstract: Disclosed are compounds that inhibit the microbial NAD synthetase enzyme. For example, disclosed are compounds of the formula Ar1—X—Ar2—Y—L—Z—Q, wherein Q is Q1Ar3 or Ar3Q1; Ar1, Ar2, and Ar3 are independently aryl or heteroaryl, optionally substituted with one or more substituents; X, Y, and Z are independently selected from the group consisting of a covalent bond or groups containing one or more of C, H, N, O, S atoms; L is a linker and Q1 is an alkylenyl, alkylenyl carbonyloxy alkyl, or alkylenyl carbonylamino alkyl group, optionally having a substituent; a covalent bond; a group containing amidine or guanidine function wherein the amidine or guanidine may be optionally N-substituted with an alkyl; or a zwitterion; or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: February 22, 2002
    Publication date: May 1, 2003
    Applicant: Virtual Drug Development, Inc.
    Inventors: Wayne J. Brouillette, Lawrence DeLucas, Christie Brouillette, Sadanandan E. Velu, Yong-Chul Kim, Liyuan Mou, R. Stephen Porter
  • Publication number: 20020169331
    Abstract: A reaction product and an imide compound can be separated from a reaction mixture obtained by reacting a substrate in the presence of the imide compound having an imide unit represented by the following formula (1): 1
    Type: Application
    Filed: December 4, 2001
    Publication date: November 14, 2002
    Inventors: Hiroyuki Miura, Hitoshi Watanabe, Akihiro Kuwana, Mami Shimamura, Naruhisa Hirai
  • Publication number: 20020169107
    Abstract: The present invention discloses novel aromatic azide derivatives and their bioconjugates for phototherapy of tumors and other lesions. The organic azides of the present invention are designed to absorb low-energy ultraviolet, visible, or near-infrared (NIR) region of the electromagnetic spectrum. The phototherapeutic effect is caused by direct interaction of nitrene, the reactive intermediate produced upon photoexcitation of the aromatic azide, with the tissue of interest. The compounds of the present invention are administered to a patient, allowed to accumulate at the site of the tumor or other lesion, and are exposed to light in order to perform a phototherapeutic procedure.
    Type: Application
    Filed: January 19, 2001
    Publication date: November 14, 2002
    Applicant: Mallinckrodt Inc.
    Inventors: Raghavan Rajagopalan, Gary Cantrell, Samuel I. Achilefu, Joseph E. Bugaj, Richard B. Dorshow
  • Publication number: 20020049343
    Abstract: Fluorinated olefins and fluorinated vinyl ethers, each having sulfonyl azide groups, are useful monomers in preparing fluoropolymers having functional side groups. Such functional side groups are useful in curing the fluoropolymers and also for enhancing the adhesion of the fluoropolymers to other substrates.
    Type: Application
    Filed: December 13, 2001
    Publication date: April 25, 2002
    Inventor: Ming-Hong Hung
  • Publication number: 20020019382
    Abstract: The present invention is directed to curcumin analogs exhibiting anti-tumor and anti-angiogenic properties, pharmaceutical formulations including such compounds and methods of using such compounds.
    Type: Application
    Filed: December 4, 2000
    Publication date: February 14, 2002
    Inventors: James P. Snyder, Matthew C. Davis, Brian Adams, Mamoru Shoji, Dennis C. Liotta, Eva M. Ferstl, Ustun B. Sunay
  • Patent number: 6340764
    Abstract: A pyridazinyl derivative (I) and its use as a reference compound in the determination of potentially genotoxic impurities in levosimendan samples. An analytic method for the determination of potentially genotoxic impurities in levosimendan samples wherein (I) is used as a reference compound. Levosimendan is a medicament useful in the treatment of heart failure.
    Type: Grant
    Filed: February 20, 2001
    Date of Patent: January 22, 2002
    Assignee: Orion Corporation
    Inventors: Reijo Bäckström, Tuula Heinonen, Tuula Hauta-Aho
  • Patent number: 6232451
    Abstract: A process for the addition of an azide function to an organic compound in which process a mixture is prepared by adding an epoxide-derivative of the organic compound and an alkali metal azide salt to a solvent is described. The mixture is heated to a reaction temperature at which the epoxide-derivative and the azide can react to form an azide derivative of the organic compound. An amount, near equimolar to the epoxide derivative, of a (1-6C)alkyl-(2-4C)carboxylic acid ester having a boiling point above the reaction temperature is added to the mixture before and/or during the reaction.
    Type: Grant
    Filed: February 8, 2000
    Date of Patent: May 15, 2001
    Assignee: Akzo Nobel N.V.
    Inventor: Henricus Cornelis Jozephus Claassen
  • Patent number: 6057446
    Abstract: A compound having the formula: ##STR1## wherein X' is nitrogen or carbon bonded to a substituent species characterized as having a sigma m value greater than 0, less than 0 or 0; X is nitrogen or carbon bonded to a substituent species characterized as having a sigma m value greater than 0, less than 0, but not equal to 0; A, A' and A" are individually substituent species characterized as having a sigma m value greater than 0, less than 0 or 0; Z' is a substituent other than hydrogen; j is an integer from 0 to 5; and the wavy line in the structure indicates that the compound can exist in the form of an enantiomer or a diasteromer; Z" is hydrogen or a substituent other than hydrogen; Y is C.dbd.O, C(OH)R' or C--A, where R' is hydrogen or lower alkyl.
    Type: Grant
    Filed: April 2, 1998
    Date of Patent: May 2, 2000
    Inventors: Peter Anthony Crooks, Haeil Park, Balwinder Singh Bhatti, William Scott Caldwell, Gary Maurice Dull
  • Patent number: 6020093
    Abstract: The photosensitive compound of the present invention contains the following unit: ##STR1## and is particularly expressed by the following formula: ##STR2## Different photosensitive resin compositions can be prepared from this novel photosensitive resin compound, and the resulting photosensitive resin compositions do not raise the problem of environmental pollution, exhibit high resolution, possess a high level of sensitivity, and exhibit excellent adhesion with substrates, coating characteristics and storage stability.
    Type: Grant
    Filed: May 13, 1998
    Date of Patent: February 1, 2000
    Assignee: Toyo Gosei Kogyo, Ltd.
    Inventors: Toru Shibuya, Jian Rong Xie, Noriaki Tochizawa
  • Patent number: 5998595
    Abstract: Azidohalogenobenzyl derivatives of the formula (I) ##STR1## wherein A is a halogen atom, B is a halogen atom or a hydrogen atom, and X is a group reactive with a hydroxy group, methods of protecting hydroxy group(s) using said derivatives, and sugar compounds wherein a hydrogen atom of at least one hydroxy group is substituted by an azidohalogenobenzyl group. According to the present invention, there are provided novel derivatives capable of introducing a group into a compound having hydroxy group(s), which group is useful as a stable hydroxy-protecting group even in solid phase synthesis for the purpose of the extension of sugar chain under continuous acidic conditions and of being removed under mild conditions; sugar compounds protected by using said derivatives; and methods of protecting hydroxy group(s) using said derivatives.
    Type: Grant
    Filed: October 30, 1997
    Date of Patent: December 7, 1999
    Assignee: Wako Pure Chemical Industries, Ltd.
    Inventors: Shoichi Kusumoto, Koichi Fukase
  • Patent number: 5955501
    Abstract: Compounds having anti-inflammatory and other activities are disclosed. The compounds are derived from phorboids of the diterpene- and benzolactam-classes.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: September 21, 1999
    Assignee: Procyon Pharmaceuticals, Inc.
    Inventors: Paul E. Driedger, James Quick
  • Patent number: RE38947
    Abstract: A chiral catalyst is disclosed together with methods of using it for enantioselective syntheses. The chiral catalyst includes a nucleus with two metal atoms that has four bridging ligands oriented radially to the axis of the nucleus. Each of these ligands includes a two complexing atoms each complexed to one of the metal atoms. At least one of the bridging ligands includes a chiral center which is bonded to one of the complexing atoms. Preferably, all four of the bridging ligands include a chiral center bonded to one of the complexing atoms. The catalyst of the invention has been found to be useful in catalyzing carbenoid transformation reactions such as cyclopropanation.
    Type: Grant
    Filed: February 14, 1996
    Date of Patent: January 24, 2006
    Assignee: Research Corporation Technologies, Inc.
    Inventor: Michael P. Doyle