Plural Ring Hetero Atoms In The Additional Hetero Ring Patents (Class 514/217.09)
  • Publication number: 20030114436
    Abstract: One aspect of the present invention relates to novel heterocyclic compounds comprising urea functionality. A second aspect of the present invention relates to the use of the novel heterocyclic compounds comprising urea functionality as ligands for various cellular receptors, including opioid receptors, other G-protein-coupled receptors and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds comprising urea functionality as analgesics.
    Type: Application
    Filed: November 5, 2002
    Publication date: June 19, 2003
    Inventors: Brian M. Aquila, Gregory D. Cuny, James R. Hauske, Liming Shao, Xinhe Wu
  • Publication number: 20030100548
    Abstract: 1 Compounds of formula (I) wherein Z is —CH2SR and R represents hydrogen or —COCH3, are useful as metalloproteinase inhibitors, especially as inhibitors of MMP 13.
    Type: Application
    Filed: September 20, 2002
    Publication date: May 29, 2003
    Inventors: Bernard Christophe Barlaam, Nicholas John Newcombe, Howard Tucker, David Waterson
  • Publication number: 20030100545
    Abstract: Benzimidazolidinone derivative compounds, which increase acetylcholine signaling or effect in the brain, and highly selective muscarinic agonists, particularly for the M1 and/or M4 receptor subtypes, pharmaceutical compositions comprising the same, as well as methods of treating psychosis using these compounds are disclosed.
    Type: Application
    Filed: September 30, 2002
    Publication date: May 29, 2003
    Inventors: Nicholas Michael Kelly, Kristian Norup Koch, Bo-Ragnar Tolf
  • Publication number: 20030055037
    Abstract: Benzimidazole and indole derivatives that act as selective modulators of CRF 1 receptors are provided. These compounds are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided.
    Type: Application
    Filed: October 5, 2001
    Publication date: March 20, 2003
    Inventors: Stephane DeLombaert, Ping Ge, Raymond F. Horvath, Taeyoung Yoon
  • Publication number: 20030055045
    Abstract: Compounds of general formula (I) 1
    Type: Application
    Filed: April 15, 2002
    Publication date: March 20, 2003
    Applicant: Astra Pharma Inc.
    Inventors: Benjamin Pelcman, Edward Roberts
  • Publication number: 20030018025
    Abstract: Disclosed are compounds of the formula: 1
    Type: Application
    Filed: May 28, 2002
    Publication date: January 23, 2003
    Applicant: Neurogen Corporation, Corporation of the State of Delaware
    Inventors: Andrew Thurkauf, Raymond F. Horvath, Jun Yuan, John M. Peterson
  • Publication number: 20030018022
    Abstract: Compounds, compositions and methods are provided that are useful in the treatment of chemokine receptor-mediated conditions and diseases. In particular, the invention provides compounds which modulate CCR4 function or a CCR4-mediated response. The subject compounds and compositions are useful for the treatment or prevention of inflammatory conditions and diseases.
    Type: Application
    Filed: May 22, 2002
    Publication date: January 23, 2003
    Applicant: Tularik Inc.
    Inventors: Tassie Collins, Hossen Mahmud, Jonathan Houze, Alan Xi Huang, Julio C. Medina, Xuemei Wang, Feng Xu, Qingge Xu, Liusheng Zhu
  • Publication number: 20020119963
    Abstract: The invention provides compounds of formula 1 1
    Type: Application
    Filed: July 31, 2001
    Publication date: August 29, 2002
    Inventors: Mark A. Sanner, Chris J. Helal, Christoper B. Cooper, Frank S. Menniti, Michael K. Ahlijanian, Anabella Villalobos, Lit-Fui Lau, Patricia A. Seymour
  • Publication number: 20020115656
    Abstract: A method for treating an allergic condition, including an atopic allergic condition, using substituted pyrazoles.
    Type: Application
    Filed: February 13, 2002
    Publication date: August 22, 2002
    Inventors: Christopher R. Butler, Hui Cai, James P. Edwards, Cheryl A. Grice, Yin Gu, Darin J. Gustin, Lars Karlsson, Haripada Khatuya, Steven P. Meduna, Barbara A. Pio, Clark A. Sehon, Siquan Sun, Kevin L. Tays, Robin L. Thurmond, Jianmei Wei
  • Publication number: 20020103185
    Abstract: The invention provides compounds of formula 1 1
    Type: Application
    Filed: August 28, 2001
    Publication date: August 1, 2002
    Inventors: Mark A. Sanner, Chris J. Helal, Christopher B. Cooper, Travis T. Wager
  • Patent number: 6420395
    Abstract: The present invention discloses compounds of formula (1) or (2), any of its enantiomers or any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein n is 0, or 1; R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalky-alkyl, aryl or aralkyl; and R1 is aryl which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cyloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl and a monocyclic 5 to 6-membered heteroaryl group a monocyclic 5 to 6-membered heteroaryl group which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3.
    Type: Grant
    Filed: November 29, 1999
    Date of Patent: July 16, 2002
    Assignee: Neurosearch A/S
    Inventors: Dan Peters, Gunnar M. Olsen, Simon F. Nielsen, Elsebet O. Nielsen
  • Publication number: 20020055497
    Abstract: A method for treating an allergic condition, including an atopic allergic condition, using substituted pyrazoles.
    Type: Application
    Filed: September 5, 2001
    Publication date: May 9, 2002
    Inventors: Christopher R. Butler, Hui Cai, James P. Edwards, Cheryl A. Grice, Yin Gu, Darin J. Gustin, Lars Karlsson, Haripada Khatuya, Steven P. Meduna, Barbara A. Pio, Clark A. Sehon, Siquan Sun, Kevin L. Tays, Robin L. Thurmond, Jianmei Wei
  • Patent number: 6372736
    Abstract: Compounds of the formula (I): wherein A, Y, R, X, R1, R2, R3 and R4 are as defined above are inhibitors of rotamase enzymes in particular FKBP-12 and FKBP-52. The compounds therefore moderate neuronal regeneration and outgrowth and can be used for treating neurological disorders arising from neurodegenerative diseases or other disorders involving nerve damage.
    Type: Grant
    Filed: July 21, 1999
    Date of Patent: April 16, 2002
    Assignee: Pfizer INC
    Inventors: Mark Ian Kemp, Michael John Palmer, Mark Allen Sanner, Martin James Wythes
  • Patent number: 6365584
    Abstract: Arylsulphonamide-substituted benzimidazole derivatives of formula (I) having tryptase-inhibiting activity. Exemplary are: 1-Methyl-2-[2-(4-amidinophenyl)-ethyl]-5-[N-(2-diethylaminoethyl)-benzenesulphonylamino]-benzimidazole; 1-Methyl-2-[2-(4-amidinophenyl)-ethyl]-5-[N-(2-diethlylaminoethyl)-benzylsulfonylamino]-benzimidazole; and, 1-Methyl-2-[2-(4-amidinophenyl)-ethyl]-5-[N-(3-diethylaminopropyl)-benzenesulphonylamino]-benzimidazole.
    Type: Grant
    Filed: September 21, 2000
    Date of Patent: April 2, 2002
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Ralf Anderskewitz, Christine Braun, Hans Briem, Bernd Disse, Christoph Hoenke, Hans Michael Jennewein, Georg Speck
  • 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
  • Patent number: 6335329
    Abstract: Selected novel carboxylic acid substituted heterocycle compounds are effective for prophylaxis and treatment of inflammation, tissue degradation, cancer, fibrosis and related diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of inflamation, tissue degradation and related diseases. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Grant
    Filed: December 16, 1998
    Date of Patent: January 1, 2002
    Assignee: Amgen Inc.
    Inventors: Kevin Koch, Andreas Termin, John A. Josey
  • Patent number: 6291450
    Abstract: Selected novel carboxylic acid substituted heterocycle compounds are effective for prophylaxis and treatment of inflammation, tissue degradation, cancer, fibrosis and related diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of inflamation, tissue degradation and related diseases. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Grant
    Filed: June 7, 2000
    Date of Patent: September 18, 2001
    Assignee: Amgen Inc.
    Inventors: Kevin Koch, Andreas Termin, John A. Josey