Nitrogen Or C(=x), Wherein X Is Chalcogen, Attached Indirectly To The Seven-membered Hetero Ring By Acyclic Nonionic Bonding Patents (Class 514/217.12)
  • Aminopyridinyl-, aminoguanidinyl- and Alkoxyguanidinyl-substituted phenyl acetamides as protease inhibitors
    Publication number: 20020061872
    Abstract: Phenyl acetamide compounds are described, including compounds of Formula I: 1
    Type: Application
    Filed: October 5, 2001
    Publication date: May 23, 2002
    Applicant: 3-Dimensional Pharmaceuticals
    Inventors: Wenxi Pan, Tianbao Lu, Thomas P. Markotan, Bruce E. Tomczuk
  • NEW USE
    Publication number: 20020058655
    Abstract: The invention provides a method of treatment or prophylaxis of obesity, comprising administering to a patient in need of such treatment a therapeutically effective amount of an aryl sulfonamide compound of formula (I) or formula (II) 1
    Type: Application
    Filed: July 20, 2001
    Publication date: May 16, 2002
    Inventors: Patrizia Caldirola, Sukhwinder Jossan, Kjell S. Sakariassen, Jan Svartengren
  • Protein:prenyl transferase inhibitors
    Patent number: 6376468
    Abstract: The invention pertains to novel peptide analogs suitable for inhibiting protein:prenyl transferases. As such they are therapeutically useful in e.g. inhibiting oncogenesis and other unwanted cell proliferation, and in supressing aberrant high signal transduction. The analogs comply with the following formula: in which: R1 is hydrogen or a thiol-protecting group; R2 and R3 are independently hydrogen or C1-C4 alkyl; R4 is hydrogen, C1-C4 alkyl, C1-C4 acyl or peptidyl; R5 is hydrogen or C1-C4 alkyl; R6 is hydrogen or optionally substituted C1-C6 alkyl; A is a direct bond or an optionally substituted C1-C4 alkylene chain; Y represents an oxo group or two hydrogen atoms; Z is oxygen, sulphur, imino or C1-C5 alkyl-, aryl- or acylimino; M is 0, 1 or 2; N is 0 or 1.
    Type: Grant
    Filed: February 3, 2000
    Date of Patent: April 23, 2002
    Assignees: Nederlandse Organisatie Voor Toegepast-Natuurwetenschappelijk Onderzoek TNO, Rijksuniversiteit Leiden
    Inventors: Herman Steven Overkleeft, Steven Hendrik Leonard Verhelst, Nicolaas Johannes Meeuwenoord, Elsbet Jantine Pieterman, Louis Hartog Cohen, Mark Overhand, Gijsbert Arie Van der Marel, Jacobus Hubertus Van Boom
  • Phenyl-and phenylalkyl-substituted ethanolamines and ethylenediamines
    Publication number: 20020042410
    Abstract: Compounds of formula 1, 1
    Type: Application
    Filed: July 24, 2001
    Publication date: April 11, 2002
    Inventors: Klaus Fuchs, Werner Stransky, Matthias Grauert, Adrian Carter, Wolfram Gaida, Thomas Weiser, Helmut Ensinger
  • N-hydroxy-2-(alkyl, aryl, or heteroaryl sulfanyl, sulfinyl or sulfonyl)-3-substituted alkyl, aryl or heteroarylamides as matrix metalloproteinase inhibitors
    Publication number: 20020032186
    Abstract: Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF-&agr; converting enzyme (TACE), a pro-inflmatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states.
    Type: Application
    Filed: July 3, 2001
    Publication date: March 14, 2002
    Applicant: American Cyanamid Company
    Inventors: Aranapakam Mudumbai Venkatesan, Jannie Lea Baker, Jeremy Ian Levin
  • Substituted AZA- and diazacycloheptane and -cyclooctane
    Patent number: 6352981
    Abstract: Aza- and diazacyclohexane and -cyclooctane compounds of the following formula: Ar1—A—B—Ar2  (I) where Ar1, A, B and Ar2 have the meanings stated in the description have a high affinity for the dopamine D3 receptor and can therefore be used to treat disorders which respond to dopamine D3 ligands.
    Type: Grant
    Filed: October 27, 2000
    Date of Patent: March 5, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Hans-Jörg Treiber, Stefan Blank, Dorothea Starck, Liliane Unger, Hans-Jürgen Teschendorf, Karsten Wicke
  • Aniline disulfide derivatives for treating allergic diseases
    Publication number: 20020013311
    Abstract: Methods and compositions for preventing or treating allergic diseases of the eye, nose, skin, ear, gastrointestinal tract, airways or lung and preventing or treating manifestations of systemic mastocytosis are disclosed. The compositions contain a mast cell stabilizing disulfide derivative as an active ingredient.
    Type: Application
    Filed: April 25, 2001
    Publication date: January 31, 2002
    Applicant: Alcon Universal Ltd.
    Inventors: Mark R. Hellberg, Zixia Feng, Steven T. Miller
  • Sulphonamide derivatives
    Publication number: 20020002158
    Abstract: Glutamate receptor function in a mammal may be potentiated using an effective amount of a compound of formula
    Type: Application
    Filed: July 25, 2001
    Publication date: January 3, 2002
    Inventors: MacKlin B. Arnold, Stephen R. Baker, Thomas J. Bleisch, Buddy E. Cantrell, Ana M. Escribano, Ken Matsumoto, Tracey E. McKennon, Paul L. Ornstein, Richard L. Simon, Edward C.R. Smith, Hamideh Zarrinmayeh, Dennis M. Zimmerman
  • Cyclic amine derivatives- CCR-3 receptor antagonists
    Patent number: 6323223
    Abstract: This invention relates to certain cyclic amine derivatives of Formula (I) that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.
    Type: Grant
    Filed: August 14, 1998
    Date of Patent: November 27, 2001
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Leyi Gong, Denis John Kertesz, David Bernard Smith, Francisco Xavier Talamas, Robert Stephen Wilhelm
  • Beta-phenylalanine derivatives as integrin antagonists
    Publication number: 20010031788
    Abstract: The present invention relates to compounds of the general formula (1) 1
    Type: Application
    Filed: May 30, 2001
    Publication date: October 18, 2001
    Inventors: Andreas Schoop, Gerhard Mueller, Ulf Brueggemeier, Delf Schmidt, Beatrix Stelte-Ludwig, Joerg Keldenich
  • Calcium channel blockers
    Publication number: 20010023249
    Abstract: The present invention provides compounds that block calcium channels having the Formula I shown below.
    Type: Application
    Filed: January 25, 2001
    Publication date: September 20, 2001
    Inventors: Lain-Yen Hu, Michael Francis Rafferty, Todd Robert Ryder
  • Amidino protease inhibitors
    Patent number: 6281206
    Abstract: Amidino and benzamidino compounds, including compounds of the formula: wherein R1-R4, R6-R9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit a number of proteolytic enzymes are described. Also described are methods for preparing the compounds of Formula I.
    Type: Grant
    Filed: February 11, 2000
    Date of Patent: August 28, 2001
    Assignee: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Tianbao Lu, Bruce E. Tomczuk, Carl R. Illig, Richard M. Soll
  • Amidino protease inhibitors
    Patent number: 6225302
    Abstract: Amidino and benzamidino compounds, including compounds of the formula: wherein R1-R4, R6-R9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit a number of proteolytic enzymes are described. Also described are methods for preparing the compounds of Formula I.
    Type: Grant
    Filed: August 1, 2000
    Date of Patent: May 1, 2001
    Assignee: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Tianbao Lu, Bruce E. Tomczuk, Carl R. Illig, Richard M. Soll
  • N-acyl and N-aroyl aralkyl amides as serotonergic agents
    Patent number: 6197773
    Abstract: A compound of the formula wherein m, R1, R2, R3, R4, R5 and X are as defined above, useful in treating or preventing migraine, depression and other disorders for which a 5-HT1 agonist or antagonist is indicated.
    Type: Grant
    Filed: May 31, 2000
    Date of Patent: March 6, 2001
    Assignee: Pfizer Inc
    Inventor: Harry R. Howard
  • Aminocyclohexylesters and uses thereof
    Patent number: 6174879
    Abstract: Aminocyclohexylester compounds, including thioesters, are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the blockade of ion channels and the treatment of arrhythmias.
    Type: Grant
    Filed: March 17, 1999
    Date of Patent: January 16, 2001
    Assignee: University of British Columbia
    Inventors: Bernard A. MacLeod, Michael J. A. Walker, Richard A. Wall