Nitrogen In The Acyclic Chain Patents (Class 558/390)
  • Publication number: 20150140605
    Abstract: The invention includes a selective method of modifying the N-terminus of a protein using an aminoacyl tRNA transferase. In certain embodiments, the method comprises contacting a solution of the protein or peptide with a transferase and a derivative of a molecule, whereby the N-terminus of the protein or peptide is derivatized with the molecule.
    Type: Application
    Filed: June 13, 2013
    Publication date: May 21, 2015
    Inventor: E. James Petersson
  • Publication number: 20150031536
    Abstract: The invention relates to sulfmimidoyl- and sulfonimidoylbenzoyl derivatives of the general formula (I). In said formula (I), R, R?, X, W and Z represent radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogens. Q represents a cyclohexandionyl-, pyrazolyl-oder isoxazolyl radical.
    Type: Application
    Filed: February 18, 2013
    Publication date: January 29, 2015
    Inventors: Hartmut Ahrens, Simon Doerner-Rieping, Stefan Lehr, Hansjoerg Dietrich, Elmar Gatzweiler, Christopher Hugh Rosinger, Dirk Schmutzler
  • Publication number: 20140350284
    Abstract: Provided herein are compositions including diastereomers in substantially diastereomerically pure form and enantiomers in substantially enantiomerically pure form, and processes for preparing them and converting them to metyrosine.
    Type: Application
    Filed: August 8, 2014
    Publication date: November 27, 2014
    Inventors: Kevin John HALLORAN, Alex COMELY, Zhengming CHEN, Shyam KRISHNAN
  • Patent number: 8779151
    Abstract: The present invention concerns compounds and their use to treat cell proliferative diseases such as cancer. Compounds of the present invention display significant potency as inhibitors of Jak2/STAT3 pathways and downstream targets and inhibit the growth and survival of cancerous cell lines.
    Type: Grant
    Filed: April 2, 2007
    Date of Patent: July 15, 2014
    Assignee: The Board of Regents of the University of Texas System
    Inventors: Waldemar Priebe, Izabela Fokt, Slawomir Szymanski, Timothy Madden, Jeffrey Myers, Charles Conrad
  • Patent number: 8748648
    Abstract: The invention provides small molecule drugs that are chemically modified by covalent attachment of a water soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the small molecule drug not attached to the water soluble oligomer.
    Type: Grant
    Filed: September 3, 2008
    Date of Patent: June 10, 2014
    Assignee: Nektar Therapeutics
    Inventors: Zhongxu Ren, Bo-Liang Deng, Jennifer Riggs-Sauthier, Micah Harvey
  • Patent number: 8450337
    Abstract: Embodiments of the invention generally relate to pharmaceutical compositions containing at least one caffeic acid compound and methods for the topical treatment of proliferative and inflammatory skin disorders such as plaque psoriasis, atopic dermatitis, and other disorders. In some embodiments, the topical treatment includes applications of the pharmaceutical composition containing at least one caffeic acid compound or a mixture of caffeic acid compounds such as caffeic acid ester compounds, caffeic acid amide compounds, analogues thereof, derivatives thereof, salts thereof, or mixtures thereof. The pharmaceutical composition or topical dosage may contain the caffeic acid compound at a concentration by weight within a range from about 0.01% to about 20%, preferably, from about 0.1% to about 15%, preferably, from about 1% to about 10%, more preferably, from about 3% to about 7%, and more preferably, from about 4% to about 6%.
    Type: Grant
    Filed: September 30, 2009
    Date of Patent: May 28, 2013
    Assignee: Moleculin, LLC
    Inventors: Waldemar Priebe, Charles Conrad, Timothy Madden
  • Publication number: 20120329974
    Abstract: Disclosed is a polymer film excellent in performance of inducing Rth.
    Type: Application
    Filed: June 20, 2012
    Publication date: December 27, 2012
    Inventors: Hiroshi Inada, Ryo Nakamura, Masaki Noro
  • Publication number: 20120022271
    Abstract: [Object] A novel method for producing an optically active pyrrolidine compound, which is useful as a production intermediate of a pharmaceutical, and a production intermediate thereof, is provided. [Means for Solution] According to the production method of the present invention, a chloro compound that is a key intermediate can be produced efficiently industrially by subjecting a mixture of regioisomers obtained by reacting an optically active epoxy compound substituted with aryl, which is easily available, with an amine compound, to chlorination. Furthermore, an optically active pyrrolidine compound can be produced industrially efficiently with the key intermediate.
    Type: Application
    Filed: April 13, 2010
    Publication date: January 26, 2012
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Atsushi Ohigashi, Takashi Kikuchi
  • Publication number: 20110300567
    Abstract: A method for identifying the redox activity of a subject compound is disclosed. The method can be performed aerobically and can include forming a mixture comprising a free-radical precursor and a compound to be tested, and converting the free-radical precursor into a free-radical anion and a free-radical cation. After the free radical cation and the free radical anion have been formed, the relative redox activity of the subject compound may cause a difference in the rate of photo-bleaching of the mixture and/or the rate of superoxide generation. These differences can be quantified and used to identify the redox activity of the subject compound. This sensitive technique for measuring redox activity can be used to screen compounds for various biological applications. Drugs also can be developed based on the relationship between redox activity and biological activity for particular biological applications.
    Type: Application
    Filed: August 9, 2011
    Publication date: December 8, 2011
    Inventors: Jonathan J. Abramson, Benjamin S. Marinov
  • Publication number: 20110098273
    Abstract: The invention provides small molecule drugs that are chemically modified by covalent attachment of a water soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the small molecule drug not attached to the water soluble oligomer.
    Type: Application
    Filed: September 3, 2008
    Publication date: April 28, 2011
    Applicant: Nektar Therapeutics
    Inventors: Zhongxu Ren, Bo-Liang Deng, Jennifer Riggs-Sauthier, Micah Harvey
  • Publication number: 20100203135
    Abstract: Methods of forming soft connective tissue compositions such as skin equivalents, compositions made by the methods and their uses.
    Type: Application
    Filed: March 14, 2006
    Publication date: August 12, 2010
    Inventors: Paul Kemp, David Shering, Andrew Shering, Penny Johnson, Damian Marshall
  • Publication number: 20100190852
    Abstract: The present invention relates to the use of a pharmaceutically effective amount of an short-acting calcium channel blocking compound to treat ischemic heart conditions, cardiac arrhythmias, hypertensive crisis in an emergency room setting, hypertension before, during, or after surgery, no-reflow phenomenon following reperfusion, and diseases associated with decreased skeletal muscle blood flow. The invention also relates to pharmaceutical compositions formulated for use in such methods and to kits for such methods.
    Type: Application
    Filed: June 19, 2008
    Publication date: July 29, 2010
    Applicant: MILESTONE PHARMACEUTICALS INC.
    Inventors: Martin P. Maguire, Elise Rioux, Harry J. Leighton
  • Publication number: 20100185000
    Abstract: The present invention relates to titanium catalysts for asymmetric synthesis reactions produced by bringing a reaction mixture obtained by contacting water and a titanium alkoxide into contact with an optically active ligand represented by the general formula (a), wherein R1, R2, R3, and R4 are independently a hydrogen atom, an alkyl group, or the like, and A* represents a group with two or more carbon atoms having an asymmetric carbon atom or axial asymmetry. The invention further relates to a process for asymmetric cyanation of imines, wherein the process comprises reacting an imine with a cyanating agent in the presence of the titanium catalyst.
    Type: Application
    Filed: September 28, 2007
    Publication date: July 22, 2010
    Applicants: Agency for Science, Technology and Research, Mitsui Chemicals Inc.
    Inventors: Abdul Majeed Seayad, Christina Chai, Balamurugan Ramalingam, Takushi Nagata, Kazuhiko Yoshinaga
  • Publication number: 20100184989
    Abstract: The invention provides methods for the preparation of small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer obtained from a water-soluble oligomer composition. Such drugs are produced through modification of a synthetic pathway to attach the oligomer to an intermediate compound followed by completion of the synthetic path.
    Type: Application
    Filed: March 12, 2008
    Publication date: July 22, 2010
    Applicant: Nektar Therapeutics
    Inventors: Jennifer Riggs-Sauthier, Bo-Liang Deng, Zhongxu Ren, Wen Zhang, Xuyuan Gu, Franco J. Duarte
  • Publication number: 20100160446
    Abstract: The present invention relates to new 3,4-dimethoxyphenethylamine modulators of L-type calcium channel activity, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: December 18, 2009
    Publication date: June 24, 2010
    Applicant: AUSPEX PHARMACEUTICALS, INC.
    Inventors: Thomas G. Gant, Sepehr Sarshar
  • Patent number: 7705047
    Abstract: The invention relates to compounds of the general formula wherein either R signifies C1-C6-alkyl, halo-C1-C6-alkyl, C1-C6-alkoxy-C2-C6-alkyl or halo-C1-C6-alkoxy-halo-C2-C6-alkyl; and X1 signifies a single bond, O, S, S(O) or S(O)2; or R signifies halogen and X1 signifies a single bond; X2 signifies CN, halogen, C1-C6-alkyl, halo-C1-C6-alkyl, C1-C6-alkoxy, halo-C1-C6-alkoxy, C1-C6-alkoxycarbonyl, C1-C6-alkylthio, C1-C6-alkylsulfinyl, C1-C6-alkylsulfonyl, C1-C6-alkylsulfonylamino, halo-C1-C6-alkylsulfonylamino, OH, NH2, COOH, CONH2, C1-C6-alkylaminocarbonyl or C1-C6-alkylcarboxamido, whereby if n is greater than 1, X2 may differ from each other; m signifies 1, 2, 3 or 4; and n is 1, 2, 3, 4 or 5, and optionally the enantiomers thereof. The active ingredients have advantageous pesticidal properties. They are especially suitable for controlling parasites on warm-blooded animals.
    Type: Grant
    Filed: December 9, 2004
    Date of Patent: April 27, 2010
    Assignee: Novartis AG
    Inventors: Thomas Goebel, Noëlle Gauvry, Pierre Ducray
  • Publication number: 20100063287
    Abstract: Disclosed is a method for preparing a compound of Formula 1 comprising (1) contacting a compound of Formula 2, with (2) at least one alkali metal cyanide and (3) at least one compound of Formula 4 wherein R1 is NHR3 or OR4; R2 is CH3 or Cl; R3 is H, C1-C4 alkyl, cyclopropyl, cyclopropylcyclopropyl, cyclopropylmethyl or methylcyclopropyl; R4 is H or C1-C4 alkyl; and X is Br, Cl or I.
    Type: Application
    Filed: June 23, 2008
    Publication date: March 11, 2010
    Applicant: E.I. Du Pont De Nemours and Company
    Inventor: Gary David Annis
  • Patent number: 7494956
    Abstract: The invention relates to compounds of the general formula (I) wherein X, Y and W have the significances given in claim 1 and optionally the enantiomers thereof. The active ingredients have advantageous pesticidal properties. They are especially suitable for controlling parasites in and on warm-blooded animals.
    Type: Grant
    Filed: November 5, 2004
    Date of Patent: February 24, 2009
    Assignee: Novartis AG
    Inventors: Noëlle Gauvry, Thomas Goebel, Pierre Ducray, François Pautrat, Ronald Kaminsky, Martin Jung
  • Publication number: 20090042973
    Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
    Type: Application
    Filed: July 2, 2008
    Publication date: February 12, 2009
    Inventors: Michael R. Hale, Christopher T. Baker, Timothy A. Stammers, Ronald George Sherrill, Andrew Spaltenstein, Eric Steven Furfine, Francois Maltais, Clarence Webster Andrews, III, John Franklin Miller, Vicente Samano
  • Patent number: 7442718
    Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
    Type: Grant
    Filed: July 2, 2003
    Date of Patent: October 28, 2008
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Michael R Hale, Christopher T Baker, Timothy A Stammers, Ronald G Sherrill, Andrew Spaltenstein, Eric S Furfine, Francois Maltais, Clarence W Andrews, III, John F Miller, Vicente Samano
  • Patent number: 7304018
    Abstract: The invention relates to compounds of the general formula: (I) and optionally the enantiomers thereof. The active ingredients have advantages pesticidal properties. They are especially suitable for controlling parasites on warm-blooded animals.
    Type: Grant
    Filed: June 15, 2003
    Date of Patent: December 4, 2007
    Assignee: Novartis Animal Health US, Inc.
    Inventors: Pierre Ducray, Thomas Goebel, Jacques Bouvier
  • Patent number: 7241776
    Abstract: Novel cyanoamidines compounds of formula (I) and (II) and their derivatives wherein R1-R12 are as defined in the specification act as antagonists of the P2X7 receptor. These compounds are particularly useful in the treatment of pain, inflammation and neurodegeneration states.
    Type: Grant
    Filed: August 2, 2004
    Date of Patent: July 10, 2007
    Assignee: Abbott Laboratories
    Inventors: William A. Carroll, Arturo Perez-Medrano, Sridhar Peddi, Alan S. Florjancic
  • Patent number: 7135585
    Abstract: Compounds of Formula I are disclosed which are useful as fungicides wherein Q is Z is X is —O—, —CH(R11)— or ?C(R11)—; R1 is H or C1–C2 alkyl; R2 is H; C1–C6 alkyl; C3–C6 cycloalkyl; or phenyl optionally substituted with halogen, cyano, C1–C2 alkyl or C1–C2 alkoxy; and R3–R11 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula I and a method for controlling plant diseases caused by fungal plant pathogens which involves applying an effective amount of a compound of Formula I.
    Type: Grant
    Filed: March 2, 2001
    Date of Patent: November 14, 2006
    Inventors: Gregory Steven Basarab, Douglas Brian Jordan, Thomas Arend Lessen, Stephen L. Hansen
  • Patent number: 7064231
    Abstract: The invention relates to stereoisomerically enriched diamines, to metal complexes comprising these diamines and also to their use in a process for asymmetrically reducing ketones using silanes, in particular polymethylhydrosiloxane, as reducing agents.
    Type: Grant
    Filed: August 19, 2003
    Date of Patent: June 20, 2006
    Assignee: Bayer Aktiengesellschaft
    Inventor: Jürgen Köcher
  • Patent number: 6995180
    Abstract: A compound of the formula I: wherein R1, R2, R3 and R4 are as defined herein. Further provided are methods of using such compounds for the treatment of diabetes and related diseases, and to pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: October 21, 2003
    Date of Patent: February 7, 2006
    Assignee: Bristol Myers Squibb Company
    Inventors: David R. Magnin, Lawrence G. Hamann
  • Publication number: 20040266867
    Abstract: The invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1 is H, chlorine, or bromine; R2 is electron attractive groups selected from the group consisting of CF3, CN, fluorine, CH3SO3, CF3SO3, and NO2; R3 is linear or branched alkyl having 1 to 10 carbon atoms, linear or branched alkoxyalkyl having 2 to 10 carbon atoms, aliphatic alcohol having 1 to 10 carbon atoms, or cycloalkyl having 3 to 6 carbon atoms. The invention also relates to methods for preparing the said compounds and the composition comprising the same. The compounds of the present invention have the effect of &bgr;2-receptor agonist and can be used for the treatment of asthma and bronchitis.
    Type: Application
    Filed: August 16, 2004
    Publication date: December 30, 2004
    Inventors: Maosheng Cheng, Li Pan, Lie Ji, Li Zhang, Jianmin Shen, Guilan Song, Zhiging Li
  • Publication number: 20040259919
    Abstract: A compound of the formula I: 1
    Type: Application
    Filed: October 21, 2003
    Publication date: December 23, 2004
    Inventors: David R. Magnin, Lawrence G. Hamann
  • Publication number: 20040236116
    Abstract: Novel bicyclic-cannabinoids and hexahydrocannabinol analogs are presented. These compounds, when administered in a therapeutically effective amount to an individual or animal, results in a sufficiently high level of that compound in the individual or animal to cause a physiological response. The physiological response useful to treat a number of physiological conditions.
    Type: Application
    Filed: July 12, 2004
    Publication date: November 25, 2004
    Inventors: Alexandros Makriyannis, Spyridon P Nikas, Atmaram D Khanolkar
  • Publication number: 20040229923
    Abstract: A method for resolving enantiomers of a compound containing the structure of the formula: 1
    Type: Application
    Filed: June 16, 2004
    Publication date: November 18, 2004
    Inventors: Glenn E. Wilcox, Mark E. Flanagan, Michael J. Munchhof, Ton Vries, Christian Koecher
  • Patent number: 6800659
    Abstract: Novel styrylacrylonitrile compounds which are useful in treating a variety of cell proliferative disorders such as cancer are disclosed.
    Type: Grant
    Filed: April 12, 2001
    Date of Patent: October 5, 2004
    Assignee: HSC Research and Development Limited Partnership
    Inventors: Chaim M. Roifman, Thomas Grunberger, Olga Rounova, Demin Peter, Nigel Sharfe
  • Publication number: 20040192741
    Abstract: Novel calcilytic compounds and methods of using them are provided.
    Type: Application
    Filed: January 21, 2004
    Publication date: September 30, 2004
    Applicant: SmithKline Beecham Corporation & NPS Pharmaceuticals
    Inventors: Maria Amparo Lago, James Francis Callahan, Pradip Kumar Bhatnagar, Eric G. Del Mar, William M. Bryan, Joelle L. Burgess
  • Patent number: 6743929
    Abstract: Sulfonamide-containing hydroxyethylamine compounds are effecive as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: September 6, 2000
    Date of Patent: June 1, 2004
    Assignee: G. D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
  • Patent number: 6703420
    Abstract: This invention relates generally to amino-thio-acrylonitriles of formula Ia or Ib: as MEK inhibitors, pharmaceutical compositions containing the same, and methods of using the same as for treatment and prevention of inflammatory disorders or as an anticancer radiosensitizing agent.
    Type: Grant
    Filed: March 17, 2000
    Date of Patent: March 9, 2004
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventor: Frank Worden Hobbs, Jr.
  • Publication number: 20040039220
    Abstract: The invention relates to a process for the preparation of compounds of the formula 1
    Type: Application
    Filed: August 19, 2003
    Publication date: February 26, 2004
    Inventors: Saleem Farooq, Stephan Trah, Hugo Ziegler, Rene Zurfluh
  • Publication number: 20030191310
    Abstract: The present invention relates to a method for producing 3,5-diamino-6-(2,3-dichlorophenyl)-1,2,4-triazine (lamotrigine) by cyclization reaction from &agr;-oxo-2,3-dichlorophenylacetamidino-aminoguanidino-hydrazone.
    Type: Application
    Filed: May 15, 2003
    Publication date: October 9, 2003
    Inventors: Geza Schneider, Csaba Lehel Geg, Levente Ondi, Attila Gergely Mate, Ferenc Lukacs, Miklos Nyerges, Sandor Garaczi
  • Publication number: 20030109705
    Abstract: Accordingly, the present invention provides a compound of Formula I, or tautomers or isomers thereof, 1
    Type: Application
    Filed: February 27, 2002
    Publication date: June 12, 2003
    Inventor: Jonas Grina
  • Publication number: 20030083518
    Abstract: The invention relates to substituted alcohol compounds of the formula (I): 1
    Type: Application
    Filed: June 27, 2002
    Publication date: May 1, 2003
    Inventors: Varghese John, Roy Hom, John Tucker
  • Patent number: 6515162
    Abstract: Chiral hydroxyethylamine, hydroxyethylurea or hydroxyethylsulfonamide isostere containing retroviral protease and renin inhibitors can be prepared by multi-step syntheses that utilize key chiral amine intermediates. This invention is a cost effective method of obtaining such key chiral amine intermediates enantiomerically, diastereomerically and chemically pure. The method is suitable for large scale (multikilogram) productions. This invention also encompasses organic acid and inorganic acid salts of the amine intermediates.
    Type: Grant
    Filed: December 21, 2000
    Date of Patent: February 4, 2003
    Assignee: G.D. Searle & Co.
    Inventors: John S Ng, Claire S. Przybyla, Shu-Hong Zhang
  • Publication number: 20020177716
    Abstract: This invention relates to intermediates useful in the preparation of CETP inhibitors and methods of preparation thereof.
    Type: Application
    Filed: April 30, 2002
    Publication date: November 28, 2002
    Inventors: David B. Damon, Robert W. Dugger, Robert W. Scott
  • Publication number: 20020151566
    Abstract: PDE4 inhibition is achieved by novel compounds, e.g., N-substituted aniline and diphenylamine analogs.
    Type: Application
    Filed: January 22, 2002
    Publication date: October 17, 2002
    Applicant: MEMORY PHARMACEUTICALS CORP.
    Inventors: Richard A. Schumacher, William F. Brubaker, Michael De Vivo, Hans-Jurgen Ernst Hess, Allen Hopper, Ashok Tehim, Ruiping Liu, Axel Unterbeck
  • Patent number: 6451854
    Abstract: The present invention relates to &agr;-amino acid phenyl ester derivatives having general formula (I) wherein R1 is (C1-3)alkyloxy; R2 is (C1-3)alkyl, (C1-3)alkyloxy or (C2-3)alkenyl; R3 is hydrogen, (C1-3)alkyl, (C1-3)alkyloxy or (C2-3)alkenyl; R4 is (C1-6)alkyl; R5 and R6 are independently (C1-6)alkyl, (C2-6)alkenyl, (C2-6)alkynyl or aralkyl, each of which may be optionally substituted with (C1-3)alkyloxy, (C1-3)alkyloxycarbonyl, cyano or NR7R8; R7 and R8 are independently (C1-6)alkyl; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these &agr;-amino acid phenyl ester derivatives as hypnotics for the induction and maintenance of general anaesthesia.
    Type: Grant
    Filed: January 18, 2001
    Date of Patent: September 17, 2002
    Assignee: Akzo Nobel N.V.
    Inventor: Niall Morton Hamilton
  • Publication number: 20020107406
    Abstract: A novel calcium receptor active compound having the formula is provided:
    Type: Application
    Filed: January 17, 2002
    Publication date: August 8, 2002
    Applicant: NPS Pharmaceuticals, Inc.
    Inventors: Teruyuki Sakai, Atsuya Takami, Rika Nagao
  • Patent number: 6413947
    Abstract: This invention is to provide a compound of the formula: wherein R1 is an optionally substituted 5- to 6-membered ring; W is a divalent group of the formula: wherein the ring A is an optionally substituted 5- to 6-membered aromatic ring, X is an optionally substituted C, N or O atom, and the ring B is an optionally substituted 5- to 7-membered ring; Z is a chemical bond or a divalent group; R2 is (1) an, optionally substituted amino group in which a nitrogen atom may form a quaternary ammonium, etc., or a salt thereof, which is useful for antagonizing MCP-1 receptor.
    Type: Grant
    Filed: September 13, 2000
    Date of Patent: July 2, 2002
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Mitsuru Shiraishi, Takahito Kitayoshi, Yoshio Aramaki, Susumu Honda, Tsuneo Oda
  • Patent number: 6365754
    Abstract: The present invention relates to a process for reacting &agr;-aminoaldehyde derivatives having a sterically bulky amino group which are commercially available with a metal cyanide in the presence of an acid chloride, an acid anhydride or the like to synthesize 3-amino-2-hydroxybutyronitrile derivatives in high yields and high erythro selectivity. When optically active &agr;-aminoaldehyde derivatives are used, racemization hardly occurs during the reaction, and the desired products are obtained in high optical purity.
    Type: Grant
    Filed: June 22, 2000
    Date of Patent: April 2, 2002
    Assignee: Daiso Co., Ltd.
    Inventors: Yoshiro Furukawa, Keisuke Yaegashi, Kazumasa Hinoue
  • Patent number: 6359061
    Abstract: Amide compounds of formula (I), combinatorial libraries of amide compounds and methods of preparing the same are provided. Libraries of the invention are useful for screening in biological assays in order to identify pharmaceutically useful compounds.
    Type: Grant
    Filed: March 19, 1999
    Date of Patent: March 19, 2002
    Assignee: ISIS Pharmaceuticals, Inc.
    Inventors: Eric Edward Swayze, Peter William Davis
  • Patent number: 6306840
    Abstract: The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.
    Type: Grant
    Filed: January 23, 1995
    Date of Patent: October 23, 2001
    Assignee: Biogen, Inc.
    Inventors: Steven P. Adams, Ko-Chung Lin, Wen-Cherng Lee, Alfredo C. Castro, Craig N. Zimmerman, Charles E. Hammond, Yu-Sheng Liao
  • Patent number: 6294531
    Abstract: Novel arylalkylamino compounds exhibiting calcilytic properties are provided.
    Type: Grant
    Filed: October 1, 1999
    Date of Patent: September 25, 2001
    Assignee: SmithKline Beecham Corporation
    Inventors: Robert M. Barmore, Pradip Kumar Bhatnagar, William M. Bryan, Joelle Lorraine Burgess, James Francis Callahan, Raul Rolando Calvo, Eric G. Del Mar, Maria Amparo Lago, Thomas The Nguyen, Derek Sheehan, Robert Lawrence Smith, Linda Sue Southall, Bradford C. Van Wagenen
  • Publication number: 20010016602
    Abstract: A class of substituted phenylacetonitrile-alkylaminoalkyl-ortho-substituted aryl compounds having immunosuppressive properties is described. Compounds of this class would be useful in reducing recipient rejection of transplanted organs and for treatment of autoimmune or inflammatory diseases.
    Type: Application
    Filed: January 22, 2001
    Publication date: August 23, 2001
    Applicant: G.D. Searle & Co.,
    Inventors: Chi-Dean Liang, John P. McKearn, John M. Farah, Richard A. Mueller
  • Patent number: 6277885
    Abstract: Hydroxamic acids having the formula are useful in treating disease conditions mediated by TNF-&agr;, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.
    Type: Grant
    Filed: January 27, 2000
    Date of Patent: August 21, 2001
    Assignee: American Cyanamid Company
    Inventors: Jeremy I. Levin, James M. Chen
  • Patent number: 6258973
    Abstract: The invention relates to a process for the preparation of compounds having the formula (I) wherein W, R2, R3, R5 and R6 are as defined in the description, which are useful as intermediates in the synthesis of pesticidally active compounds.
    Type: Grant
    Filed: May 17, 2000
    Date of Patent: July 10, 2001
    Assignee: Rhone-Poulenc Agro
    Inventors: Themistocles D. J. D'Silva, Jean-Erick Ancel