Nitrogen Attached Indirectly To The Hetero Ring By Nonionic Bonding Patents (Class 549/426)
  • Patent number: 6902777
    Abstract: A liquid-crystalline mediums which contain one or more compounds of the formula A and at least one compound of the formula B wherein compounds of formula A contain at least one ring selected from and in which Ra, Rb, ring A and ring B, Y, Z1, Z2, a, L1, L2, L3, L4, L5, L6, L7, L8 and L9 are as defined herein, are suitable for use in twisted nematic (TN) and supertwisted nematic (STN) liquid-crystal displays. Such displays have very short response times and good steepnesses and angle dependencies.
    Type: Grant
    Filed: December 22, 2003
    Date of Patent: June 7, 2005
    Assignee: Merck Patent GmbH
    Inventors: Harald Hirschmann, Eike Poetsch, Peer Kirsch, Sabine Schoen
  • Patent number: 6890937
    Abstract: A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9, and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. The administered enzyme inhibitor corresponds in structure to formula (I), below, or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are both hydrido or R1 and R2 together with the atoms to which they are bonded form a 5- to 8-membered ring containing one, two, or three heteroatoms in the ring that are oxygen, sulfur, or nitrogen. R3 in formula (I) is an optionally substituted aryl or optionally substituted heteroaryl radical.
    Type: Grant
    Filed: January 7, 2003
    Date of Patent: May 10, 2005
    Assignee: Pharmacia Corporation
    Inventors: Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, Jeffery N. Carroll, Gary A. DeCrezcenzo, Theresa R. Fletcher, John N. Freskos, Daniel P. Getman, Gunnar J. Hanson, Susan L. Hockerman, Carol P. Howard, Stephen A. Kolodziej, Madeleine H. Li, Joseph J. McDonald, Deborah A. Mischke, Patrick B. Mullins, Joseph G. Rico, Nathan W. Stehle, Clara I. Villamil
  • Patent number: 6869696
    Abstract: The invention concerns an electro-luminescent device in which the luminescent layer contains a compound of general formula I as doping agent or as luminescent compound, whereby the radicals R1 to R12 are identical or are different, and mean hydrogen, straight chain or branched C1-C6 alkyl, aralkyl, aryl or substituted aryl; R1 and R2 and/or R3 and R4 and/or R4 and R5 and/or R5 and R11 and/or R8 and R5 and/or R4 and R12 can form an alicyclic, heterocyclic or aromatic ring; R5 can furthermore be H, OH, OR9, N,N-di-(C1-C6) alkylamino, acetylamino or halogen; R6 and R7 together can form an alicyclic or heterocyclic ring; A1 and A2 are identical or different and are —CN, —NO2 or —COOR8; X is —CH, —CR11 or N; and Y is O, —NH, —NR12, S or Se. The doping agents together luminesce predominately red with very good quantum efficiency together with the luminescent compound as a function of concentration.
    Type: Grant
    Filed: May 10, 2002
    Date of Patent: March 22, 2005
    Assignee: Sensient Imaging Technologies GmbH
    Inventors: Andreas Richter, Dietmar Keil, Gerhard Diener
  • Patent number: 6867309
    Abstract: A red-emitting organic electroluminescent compound, the structure of the compound as follows: wherein n is an integer of 1˜6; Ar represents aryl or heteroaryl; R1 and R2 individually represent alkyl of from 1 to 20 carbon atoms, aryl, carbocyclic and other heterocyclic systems; R3 and R4 individually represent hydrogen, alkyl of from 1 to 10 atoms, branched or unbranched 5 or 6 member substituent ring connecting respectively with R1 and R2, or alkyl methyl silane group; R5 represents alkyl of from 1 to 20 atoms, aryl, or heteroaryl; and R6 represents alkyl of from 1 to 10 atoms, and a 5 or 6-member carbocyclic ring connecting with R5.
    Type: Grant
    Filed: December 5, 2002
    Date of Patent: March 15, 2005
    Assignees: Chi Mei Optoelectronics Corporation, Kyocera Corporation
    Inventors: Ruey-Min Chen, Jun-Wen Chung, Chun-Che Hsu
  • Patent number: 6849660
    Abstract: Provided are antibacterial compounds having Formula I: In such compositions, X is O or S; Y is CH2; n is 0 or 1. One of R1 and R1? is —C(O)NR5R5?, —C(O)—Q—NR5R5?, —CH2NR5R5? or —S(O)2NR5R5? and the other is H or R3. One of R2 and R2? is —NHC(O)R6 or —NHS(O)2R6 and the other is H or R4. Q is an amino acid or peptide. R3 is H, halogen, —NR5R5? or —NHC(O)R6; and R4 is selected from the group consisting of H, halogen, hydroxyl, amino, carboxyl, alkyl, alkenyl and alkynyl. R5 is selected from the group consisting of H, alkyl, alkenyl or alkynyl optionally substituted with halogen, OH, amino, amidinyl, guanidinyl, urea, alkyl, carboxyl, oxo, carboxamide; R5? is H or R5 and R5? together form a 5-16 member heterocycle optionally substituted with halogen, OH, amino, alkyl, carboxyl, carbonyl or carboxamide.
    Type: Grant
    Filed: August 1, 2000
    Date of Patent: February 1, 2005
    Assignee: ISIS Pharmaceuticals, Inc.
    Inventors: Elizabeth Jefferson, Eric Swayze
  • Patent number: 6835845
    Abstract: A is a novel methine compound, for example, which is represented by the following formula (I): wherein R1, R2, R3, R4 and R5 each represents a hydrogen atom or a substituent; X represents an oxygen atom, a sulfur atom, or N—R6; Z represents —NR7R8, or —OG; R6, R7 and R8 each represents a hydrogen atom or a substituent; G represents a hydrogen atom, a cation or a substituent; L1, L2 and L3 each represents a substituted or unsubstituted methine group; n represents 1 or 2; and W represents an electron attractive group. Also, a material for organic luminescence element and organic luminescence element using the same are disclosed.
    Type: Grant
    Filed: July 26, 2002
    Date of Patent: December 28, 2004
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Hisashi Okada, Terukazu Yanagi
  • Patent number: 6833453
    Abstract: Methods of synthesizing pharmacologically useful oxazolidinones are disclosed, and, in particular, a method of manufacturing a 5-(tert-butylcarbamoyl)-aminomethyl-oxazolidinone by condensing a carbamate with a tert-butylcarbamoyl protected derivative of glycidylamine or 3-amino-1-halopropanol.
    Type: Grant
    Filed: October 17, 2001
    Date of Patent: December 21, 2004
    Assignee: Pharmacia & Upjohn Company
    Inventors: William R. Perrault, Robert C. Gadwood
  • Patent number: 6818638
    Abstract: Mevinolin derivatives wherein the lactone ring is modified have interesting pharmaceutical properties, particularly in preventing or treating disorders or diseases mediated by LFA-1/ICAM-1 interactions.
    Type: Grant
    Filed: July 11, 2002
    Date of Patent: November 16, 2004
    Assignee: Novartis AG
    Inventors: Rolf Baenteli, Wilfried Bauer, Sylvain Cottens, Claus Ehrhardt, Ulrich Hommel, Jörg Kallen, Josef Gottfried Meingassner, François Nuninger, Gabriele Weitz Schmidt
  • Patent number: 6812352
    Abstract: Multidentate phosphite ligands are disclosed for use in reactions such as hydrocyanation and isomerization. The catalyst compositions made therefrom and the various catalytic processes which employ such multidentate phosphite ligands are also disclosed. In particular, the ligands have heteroatom-containing substituents on the carbon attached to the ortho position of the terminal phenol group.
    Type: Grant
    Filed: April 9, 2002
    Date of Patent: November 2, 2004
    Assignee: Invista North America S.a.r.l.
    Inventors: Kristina Ann Kreutzer, Wilson Tam, J. Michael Garner, John Ronald Boyles
  • Patent number: 6809207
    Abstract: The present invention provides certain alpha-amino acids and derivatives thereof, such as, but not limited to, esters, amides and salts. These derivatives may comprise such representative side groups as a phenyl, pyridyl, piperidinyl, tetrahydropyranyl, tetrahydrothiopyranyl, or thienyl group. The present invention further provides a method for synthesizing alpha-amino acids and derivatives thereof via a modified Ugi type reaction using an aldehyde, ammonium formate and a C1-C5 alkyl isocyanide. The compounds provided by this method are useful in the development of new pharmaceuticals for the treatment of human diseases.
    Type: Grant
    Filed: July 24, 2002
    Date of Patent: October 26, 2004
    Assignee: PharmaCore, Inc.
    Inventors: Sekar Alla, Seung-Yong Choi, Dale Dhanoa, Elso DiFranco, Galina Krokhina, Keqiang Li, Balasubramanian Thiagarajan, Wen-Chun Zhang
  • Patent number: 6762198
    Abstract: Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compounds have a structure according to the following Formula (I): where J, M, Q, T, W, X, Z, R1, R2, R3, R4, R4′, R5, R6, R6′, R7, m, and n have the meanings described in the specification. This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. Also disclosed are pharmaceutical compositions comprising these compounds, and methods of treating or preventing metalloprotease-related maladies using the compounds or the pharmaceutical compositions.
    Type: Grant
    Filed: March 25, 2003
    Date of Patent: July 13, 2004
    Assignee: The Procter & Gamble Company
    Inventors: Menyan Cheng, Neil Gregory Almstead, Michael George Natchus, Stanislaw Pikul, Biswanath De
  • Patent number: 6737420
    Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formula (XII): useful in treating Alzheimer's disease and other similar diseases.
    Type: Grant
    Filed: March 23, 2001
    Date of Patent: May 18, 2004
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: Roy Hom, Shumeye S. Mamo, Jay Tung, Andrea Gailunas, Varghese John, Lawrence Y. Fang
  • Patent number: 6730783
    Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.
    Type: Grant
    Filed: April 22, 2003
    Date of Patent: May 4, 2004
    Assignee: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Carl R. Illig, Thomas P. Markotan
  • Patent number: 6703425
    Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof which is useful for the treatment of conditions associated with glutamate hypofunction, such as psychiatric and neurological disorders
    Type: Grant
    Filed: November 15, 2002
    Date of Patent: March 9, 2004
    Assignee: Eli Lilly and Company
    Inventors: James Allen Knobelsdorf, Timothy Alan Shepherd, Eric George Tromiczak, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
  • Publication number: 20040033988
    Abstract: Compounds of the formula: 1
    Type: Application
    Filed: February 27, 2003
    Publication date: February 19, 2004
    Applicant: Wyeth
    Inventors: Jeremy I. Levin, James M. Chen, Derek C. Cole, Mila T. Du, Leif M. Laakso
  • Patent number: 6686348
    Abstract: A compound of formula (I): wherein: R1 represents hydrogen, halogen, alkyl or alkoxy, X represents oxygen, sulphur or NR wherein R represents hydrogen or alkyl, A represents any one of the groups described in the description, their isomers and addition salts thereof with a pharmaceutically acceptable acid or base and medicinal products containing the same are useful as metalloprotease inhibitor.
    Type: Grant
    Filed: December 21, 2001
    Date of Patent: February 3, 2004
    Assignee: Les Laboratoires Servier
    Inventors: Guillaume De Nanteuil, Alain Benoist, Philippe Pastoureau, Massimo Sabatini, John Hickman, Alain Pierre, Gordon Tucker
  • Publication number: 20040019083
    Abstract: The present invention provides methods for the asymmetric synthesis of (S,S,R)-(−)-actinonin and its analogs and the compounds thereby synthesized having a structural formula: 1
    Type: Application
    Filed: June 25, 2003
    Publication date: January 29, 2004
    Applicant: Sloan-Kettering Institute for Cancer Research
    Inventors: William G. Bornmann, Francis Sirotnak, Howard Scher, Ephraim Vidal, Christopher Borelle, David Scheinberg
  • Publication number: 20030236168
    Abstract: Processes for preparing &agr;-substituted benzylnitroguanidines include the steps of providing a reaction mixture comprising water, alcohol, an S-alkyl nitroisothiourea, and an &agr;-substituted benzylamine; heating the reaction mixture; steam distilling the alcohol from the reaction mixture; and isolating an &agr;-substituted benzylnitroguanidine from the remaining water layer.
    Type: Application
    Filed: June 20, 2002
    Publication date: December 25, 2003
    Inventors: David M. Mayes, Vijay C. Desai, Eric Rivadeneira
  • Publication number: 20030228486
    Abstract: The invention concerns an electro-luminescent device in which the luminescent layer contains a compound of general formula I as doping agent or as luminescent compound, whereby the radicals R1 to R12 are identical or are different, and mean hydrogen, straight chain or branched C1-C6 alkyl, aralkyl, aryl or substituted aryl; R1 and R2 and/or R3 and R4 and/or R4 and R5 and/or R5 and R11 and/or R8 and R5 and/or R4 and R12 can form an alicyclic, heterocyclic or aromatic ring; R5 can furthermore be H, OH, OR9, N,N-di-(C1-C6) alkylamino, acetylamino or halogen; R6 and R7 together can form an alicyclic or heterocyclic ring; A1 and A2 are identical or different and are -CN, -NO2 or -COOR8; X is -CH, -CR11 or N; and Y is O, -NH, -NR12, S or Se. The doping agents together luminesce predominately red with very good quantum efficiency together with the luminescent compound as a function of concentration.
    Type: Application
    Filed: May 10, 2002
    Publication date: December 11, 2003
    Applicant: SynTec Gesellschaft fuer Chemie und Technologie der Informationsaufzeichnung mbH
    Inventors: Andreas Richter , Dietmar Keil , Gerhard Diener
  • Publication number: 20030225133
    Abstract: N- and O-substituted 4[2-diaromaticmethoxy and methylamino)alkyl]piperidines exhibit high CNS activity with respect to the dopamine transporter (DAT) and serotonin transporter (SERT). Preferred compounds exhibit highly differential behavior as between the DAT and SERT and between the DAT and the norepinephrine transporter (NET). The compounds have utility in treating CNS disorders, including but not limited to cocaine addiction, depression, and Parkinson's disease.
    Type: Application
    Filed: March 28, 2003
    Publication date: December 4, 2003
    Inventor: Aloke A Dutta
  • Publication number: 20030216434
    Abstract: The present application describes modulators of MCP-1 of formula (I): 1
    Type: Application
    Filed: March 7, 2003
    Publication date: November 20, 2003
    Inventor: Robert J. Cherney
  • Patent number: 6638931
    Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.
    Type: Grant
    Filed: November 28, 2000
    Date of Patent: October 28, 2003
    Assignee: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Carl R. Illig, Thomas P. Markotan, Thomas P. Stagnaro
  • Publication number: 20030165714
    Abstract: Red organic electroluminescent compounds containing bis-condensed DCM derivatives, a method for synthesizing the same and an organic electroluminescent device using the same.
    Type: Application
    Filed: November 21, 2002
    Publication date: September 4, 2003
    Inventors: Jeong-ik Lee, Byung-Jun Jung, Hong-ku Shim, Hye-Yong Chu, Lee-mi Do, Tae-hyoung Zyung
  • Publication number: 20030162054
    Abstract: The present invention discloses a red organic EL device containing compound which allows EL emission to be shifted to the red spectral region, and a higher purity in color for red EL devices is obtained. The, synthesis of the compound is easy and the product yield is improved compared to the prior art. Moreover, the red organic EL devices fabricated conform with existing NTSC standards.
    Type: Application
    Filed: March 24, 2003
    Publication date: August 28, 2003
    Applicant: Industrial Technology Research Institute
    Inventors: Liang-Jyi Chen, Wen-Kou Weng, Chun-Neng Ku, Po-Yen Lu
  • Publication number: 20030144322
    Abstract: The invention provides a compound of formula (I): 1
    Type: Application
    Filed: October 23, 2002
    Publication date: July 31, 2003
    Inventors: Alan P. Kozikowski, Gian Luca Araldi
  • Publication number: 20030127975
    Abstract: A red-emitting organic electroluminescent compound, the structure of the compound as follows: 1
    Type: Application
    Filed: December 5, 2002
    Publication date: July 10, 2003
    Applicant: CHI MEI OPTOELECTRONICS CORPORATION
    Inventors: Ruey-Min Chen, Jun-Wen Chung, Chun-Che Hsu
  • Patent number: 6566381
    Abstract: Heterocyclic substituted compounds having the general structure: which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes.
    Type: Grant
    Filed: March 1, 2000
    Date of Patent: May 20, 2003
    Assignee: The Procter & Gamble Company
    Inventors: Menyan Cheng, Neil Gregory Almstead, Michael George Natchus, Stanislaw Pikul, Biswanath De
  • Publication number: 20030080323
    Abstract: Disclosed is a novel methine compound, for examples, which is represented by the following formula (I): 1
    Type: Application
    Filed: July 26, 2002
    Publication date: May 1, 2003
    Applicant: FUJI PHOTO FILM CO., LTD.
    Inventors: Hisashi Okada, Terukazu Yanagi
  • Patent number: 6545022
    Abstract: Novel amines of formulas 1D and 1E are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammatory diseases, and gastrointestinal disorders, especially IBS. Processes for the preparation and intermediates useful in the preparation are also disclosed.
    Type: Grant
    Filed: April 7, 2000
    Date of Patent: April 8, 2003
    Assignee: Pfizer Inc.
    Inventors: Justin Stephen Bryans, David Christopher Horwell, Clare Octavia Kneen, David Juergen Wustrow
  • Publication number: 20030065185
    Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds aslo inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
    Type: Application
    Filed: April 8, 2002
    Publication date: April 3, 2003
    Inventors: Eugene D. Thorsett, Christopher M. Semko, Michael A. Pleiss, Louis John Lombardo, Francine S. Grant, Darren B. Dressen, Michael S. Dappen
  • Patent number: 6541632
    Abstract: A carbocyclic or heterocyclic compound, ammonia and an oxygen-containing gas are subjected to fluid catalytic reaction in vapor phase in the presence of a catalyst containing alkali metal to produce an aromatic or heterocyclic nitrile. The use of the catalyst containing a specific amount of alkali metal enables the stable production of the aromatic or heterocyclic nitrile in high yields with little change with time even when water is present in the reaction system. The use of the catalyst containing the alkali metal also enables the recycle and reuse of unreacted ammonia which is usually accompanied by water, thereby reducing production costs.
    Type: Grant
    Filed: June 19, 2002
    Date of Patent: April 1, 2003
    Assignee: Mitsubishi Gas Chemical Company, Inc.
    Inventors: Hideaki Ogino, Takashi Okawa, Shuji Ebata, Yoshinori Kanamori
  • Patent number: 6518310
    Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.
    Type: Grant
    Filed: March 16, 2001
    Date of Patent: February 11, 2003
    Assignee: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L Fedde, Carl R Illig, Thomas P. Markotan, Thomas P Stagnaro
  • Patent number: 6514633
    Abstract: A light emitting device material comprising a compound represented by the following formula (I): wherein R1, R2 and R3, which may be the same or different, each represents an aryl group, a heterocyclic group or an aliphatic hydrocarbon group, provided that at least one of R1, R2 and R3 represents an aryl group or a heterocyclic group, containing a group represented by the following formula (II): wherein R4, R5 and R6, which may be the same or different, each represents a hydrogen atom or a substituent; X1 represents an oxygen atom, a sulfur atom, N—RX1 or CRX2RX3; RX1, RX2, RX3, which may be the same or different, each represents a hydrogen atom or a substituent; R4, R5, R6 and X1 may be linked to each other to form a ring; Y represents an oxygen atom, a sulfur atom, or N—RY1; and RY1 represents a hydrogen atom or a substituent.
    Type: Grant
    Filed: September 18, 2000
    Date of Patent: February 4, 2003
    Assignee: Fuji Photo Film Co., Ltd.
    Inventor: Kazumi Nii
  • Patent number: 6495546
    Abstract: Propanolamine derivatives represented by the following formula (I): These derivatives may be &bgr;3 agonists and exert sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic and anti-urinary incontinence and anti-pollakiuria activities. Pharmaceutical compositions containing such propanolamine derivatives, methods for the prevention and/or treatment diseases using these propanolamine derivatives, and processes for their preparation are also described.
    Type: Grant
    Filed: November 22, 2000
    Date of Patent: December 17, 2002
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
  • Patent number: 6482986
    Abstract: The invention concerns compounds of formula (I) wherein A, X, Y, n, R1, R2 and R3 are as defined in claim 1. Said compounds are specifically binding to sigma receptors particularly those of the peripheral nervous system.
    Type: Grant
    Filed: February 27, 2002
    Date of Patent: November 19, 2002
    Assignee: Sanofi-Synthelabo
    Inventors: Robert Boigegrain, Bernard Bourrie, Martine Bourrie, Pierre Casellas, Jean Marc Herbert, Pierre Lair, Dino Nisato, Raymond Paul, Jean Claude Vernieres
  • Patent number: 6479674
    Abstract: The present invention relates to compounds which are useful for efficient synthesis of 2-amino-4-oxobicyclo[3.1.0]hexane-2,6-dicarboxylic acids. The compounds according to the present invention comprise 2-oxobicyclo[3.1.
    Type: Grant
    Filed: September 24, 2001
    Date of Patent: November 12, 2002
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Atsuro Nakazato, Toshihito Kumagai, Kazunari Sakagami, Kazuyuki Tomisawa
  • Patent number: 6472422
    Abstract: The invention provides a compound of formula (I): wherein R1, R2, R3, and Y have any of the meanings defined in the specification; as well a pharmaceutical composition comprising a compound of formula I; intermediates and methods useful for preparing a compound of formula I; and therapeutic methods for treating drug addiction, Parkinson's disease or depression comprising administering a compound of formula I, to a mammal in need of such treatment.
    Type: Grant
    Filed: January 25, 2001
    Date of Patent: October 29, 2002
    Assignee: Georgetown University
    Inventors: Alan P. Kozikowski, Gian Luca Araldi
  • Patent number: 6458474
    Abstract: Disclosed is a novel methine compound, for example, which is represented by the following formula (I): wherein R1, R2, R3, R4 and R5 each represents a hydrogen atom or a substituent; X represents an oxygen atom, a sulfur atom, or N—R6; Z represents —NR7R8, or —OG; R6, R7 and R8 each represents a hydrogen atom or a substituent; G represents a hydrogen atom, a cation or a substituent; L1, L2 and L3 each represents a substituted or unsubstituted methine group; n represents 1 or 2; and W represents an electron attractive group.
    Type: Grant
    Filed: March 18, 1999
    Date of Patent: October 1, 2002
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Hisashi Okada, Terukazu Yanagi
  • Patent number: 6451791
    Abstract: An amidoaromatic ring sulfonamide hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed, as are a treatment process that comprises administering a contemplated amidoaromatic ring sulfonamide hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.
    Type: Grant
    Filed: June 4, 1999
    Date of Patent: September 17, 2002
    Assignee: Monsanto Company
    Inventors: Robert M. Heintz, Daniel P. Getman, Joseph J. McDonald, Gary A. DeCrescenzo, Susan C. Howard, S. Zaheer Abbas
  • Publication number: 20020127428
    Abstract: An organic light emitting display is provided which comprises as an emitting layer a fluorescent dye having at least one amine moiety substituted with two aryl groups. Also provided are new fluorescent compounds having N-aryl substituents which exhibit reduced pH sensitivity and enhanced stability to protonation.
    Type: Application
    Filed: March 6, 2001
    Publication date: September 12, 2002
    Applicant: International Business Machines Corporation
    Inventors: Sally Ann Swanson, Gregory Michael Wallraff
  • Patent number: 6440996
    Abstract: The invention provides compounds of formula (I): X—L—X1  (I) wherein X and X1 are substituted piperidine, cyclohexane, or tetrahydropyran rings, and L is a linking group between X and X1; as well a pharmaceutical composition comprising a compound of formula I; intermediates and methods useful for preparing a compound of formula I; and therapeutic methods for treating drug addiction, Parkinson's disease, depression, or a disease wherein the administration of cocaine is indicated, comprising administering a compound of formula I or a pharmaceutically acceptable salt thereof to a mammal in need of such treatment.
    Type: Grant
    Filed: October 7, 1999
    Date of Patent: August 27, 2002
    Assignee: Georgetown University
    Inventors: Alan P. Kozikowski, Gian Luca Araldi, Amir P. Tamiz
  • Patent number: 6420573
    Abstract: This invention provides processes for the preparation of a compound of Formula I: Y—C(═O)—C(R1)(R2)—CH2—S(O)nR3 wherein: Y is hydroxy or XONX, where each X is independently hydrogen, lower alkyl or lower acyl; R1 is hydrogen or lower alkyl; R2 is hydrogen, lower alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, or R1 and R2 together with the carbon atom to which they are attached form a cycloalkyl or heterocyclo group; R3 is aryl; and n is 0, 1 or 2. The invention also provides novel aryl haloalkyl sulfide intermediates useful for the preparation of compounds of Formula I and novel methods of preparing aryl alkyl sulfides.
    Type: Grant
    Filed: November 9, 2001
    Date of Patent: July 16, 2002
    Assignee: Syntex (U.S.A.) LLP
    Inventors: Jeffrey Allen Campbell, Lawrence Emerson Fisher, Charles Alois Dvorak, Paul Leo McGrane
  • Patent number: 6384237
    Abstract: A novel pyrylium compound is represented by the general formula (I): wherein X is oxygen or sulfur, Y− is a monovalent anion, n is an integer of 2 or 3, and M is hydrogen or an alkali metal. This pyrylium compound functions as a labeling agent by intermolecular bonding to nucleic acids, and as a fluorescence label having a chemical bond with the nucleic acids and an excitation wavelength in a visible light region.
    Type: Grant
    Filed: July 24, 2000
    Date of Patent: May 7, 2002
    Assignee: Canon Kabushiki Kaisha
    Inventors: Tomohiro Suzuki, Tadashi Okamoto, Nobuko Yamamoto
  • Patent number: 6380258
    Abstract: A sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.
    Type: Grant
    Filed: June 24, 1999
    Date of Patent: April 30, 2002
    Assignee: G. D. Searle, L.L.C.
    Inventors: Louis J. Bedell, Joseph J. McDonald, Thomas E. Barta, Daniel P. Becker, Shashidhar N. Rao, John N. Freskos, Brent V. Mischke, Daniel P. Getman, Gary A. DeCrescenzo
  • Patent number: 6358980
    Abstract: Compounds of the formula: useful in the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.
    Type: Grant
    Filed: January 27, 2000
    Date of Patent: March 19, 2002
    Assignee: American Cyanamid Company
    Inventors: Jeremy I. Levin, Aranapakam M. Venkatesan, James M. Chen, Arie Zask, Vincent P. Sandanayaka, Mila T. Du, Jannie L. Baker
  • Patent number: 6355674
    Abstract: A class of novel aminotetralins is disclosed useful as 5-HT1D&agr; agonists.
    Type: Grant
    Filed: May 2, 2000
    Date of Patent: March 12, 2002
    Assignee: Eli Lilly and Company
    Inventors: John M Schaus, Clint D Walker, Yao-Chang Xu
  • Patent number: 6329523
    Abstract: Novel compounds having the formula: wherein the constituent variables are defined herein. The compounds are constructed to include a central aromatic, aliphatic, or heterocyclic ring system. Attached to the central ring system are two linear groups having nitrogenous moieties that are derivatized with chemical functional groups. The ring system can include further nitrogenous moieties, either as ring atoms or on pendant groups attached to the ring, that may also be derivatized with chemical functional groups. The totality of the chemical functional groups imparts certain conformational and other properties to the these compounds. In accordance with certain embodiments of the invention, libraries of such compounds are prepared utilizing permutations and combinations of the chemical functional groups and the nitrogenous moieties to build complexity into the libraries.
    Type: Grant
    Filed: March 10, 1999
    Date of Patent: December 11, 2001
    Assignee: ISIS Pharmaceuticals, Inc.
    Inventors: Phillip Dan Cook, Haoyun An
  • Patent number: 6303782
    Abstract: A process is described for preparing an aromatic compound substituted by a tertiary nitrile of Formula (1.0.0): comprising treating a substituted aromatic compound of Formula (2.0.0): with a secondary nitrile of Formula (3.0.0): in the presence of a base having a pKa numerical value in the range of from about 17 to about 30, provided that the difference in pKa numerical values between said base and the corresponding tertiary nitrile of Formula (3.0.0) is no more than about 6; in an aprotic solvent having a dielectric constant (∈) of less than about 20; and at a reaction temperature in the range of from about 0° C. to about 120° C.; whereby there is formed said tertiary-nitrile-substituted aromatic compound final product of Formula (1.0.0); wherein the constituent parts W1, W2, W3, W4, and W5; and the substituent moieties R1, R2, R3, R4, R5, R6, and R7 in the compounds of Formulas (1.0.0), (2.0.0) and (3.0.
    Type: Grant
    Filed: March 1, 2000
    Date of Patent: October 16, 2001
    Assignee: Pfizer Inc
    Inventor: Stéphane Caron
  • Patent number: 6281211
    Abstract: This invention is related to substituted semicarbazides represented by Formula (I) or a pharmaceutically acceptable salt or prodrug thereof, wherein: R1 and R2 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; R3, R4, R5 and R6 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl, or R3 and R4 is defined as above, and R5 and R6 together with the nitrogen atom to which they are attached form a heterocycle, including piperidine, piperazine, morpholine; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one of O, S, NR7, CH2, C(O), NR7C(O), C(O)NR7, SO, SO2 or a covalent bond; where R7 is hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; n is
    Type: Grant
    Filed: September 21, 2000
    Date of Patent: August 28, 2001
    Assignee: Euro-Celtique S.A.
    Inventors: Sui Xiong Cai, Nancy C. Lan, Soo Hong-Bae
  • Patent number: 6281365
    Abstract: Organic platinum complexes active as anti-tumor agents in warm-blooded animals, and methods for synthesis of same, are described.
    Type: Grant
    Filed: May 26, 1989
    Date of Patent: August 28, 2001
    Assignee: American Cyanamid Company
    Inventors: Ralph Grassing Child, Panayota Bitha, Joseph John Hlavka, Yang-I Lin