1,3-diazole Ring (including Hydrogenated) Patents (Class 544/139)
  • Substituted amides, their preparation and use
    Patent number: 6753327
    Abstract: An amide of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: A —(CH2)p—R1, where R1 can be pyrrolidine, morpholine, piperidine, —NR5R6 and  and R5, R6 and R7 can, independently of one another, be hydrogen, C1-C4-alkyl, CH2Ph, Ph, CH2CH2Ph, it also being possible for the phenyl rings to be substituted by R6, and p can be 1 and 2, and B can be phenyl, pyridyl, pyrimidyl and pyridazyl, it also being possible for the rings to be substituted by up to 2 R8 radicals, and D can be a bond, —(CH2)m, —CH═CH—, —C≡C—, and Y is phenyl, pyridine, pyrimidine and pyrazine and n is a number 0, 1 or 2, and m,q are, independently of one another, a number 0, 1, 2, 3 or 4.
    Type: Grant
    Filed: October 11, 2000
    Date of Patent: June 22, 2004
    Assignee: Abbott GmbH & Co. KG
    Inventors: Wilfried Lubisch, Achim Möller, Hans-Jörg Treiber, Monika Knopp
  • 2-thio-substituted imidazole derivatives and the use thereof in the pharmaceutical industry
    Publication number: 20040116416
    Abstract: The invention relates to 2-thio-substituted imidazole derivatives of the formula I 1
    Type: Application
    Filed: January 28, 2004
    Publication date: June 17, 2004
    Inventors: Stefan Laufer, Dunja Kotschenreuther, Philipp Merckle, Karola Tollmann, Hans-Gunter Striegel
  • 2-Mercapto-4,5-diarylimidazole derivatives and the use thereof as cyclooxygenase inhibitors
    Publication number: 20040116695
    Abstract: The invention relates to the 2-mercapto-4,5-diarylimidazole derivatives of formula (I), wherein R1, R2, R3 and R4 are defined as in the description. The inventive compounds have an immunomodulatory and cyclooxygenase-inhibiting activity and are therefore suitable for the treatment of diseases that are associated with a disturbed immune system.
    Type: Application
    Filed: September 26, 2003
    Publication date: June 17, 2004
    Inventors: Gerd Dannhardt, Linda Hahn
  • Thiohydantoins and use thereof for treating diabetes
    Publication number: 20040116417
    Abstract: The invention relates to 2-thiohydantoin derivative compounds selected from compounds of general formula (I): 1
    Type: Application
    Filed: September 26, 2003
    Publication date: June 17, 2004
    Inventors: Benaissa Boubia, Evelyne Chaput, Khan Ou, Philippe Ratel
  • Carbamate and oxamide compounds
    Patent number: 6743788
    Abstract: Disclosed are novel aromatic compounds of the formula(I) described herein, wherein G, E, W, Ar, X, Y and Z are disclosed herein. The compounds are useful for treating cytokine mediated diseases or conditions such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.
    Type: Grant
    Filed: May 17, 2002
    Date of Patent: June 1, 2004
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Pier Francesco Cirillo, Victor Kamhi, John Robinson Regan, Michele Tsang
  • 1-Aryl-or 1-alkylsulfonylbenzazole derivatives as 5-hydroxytryptamine-6 ligands
    Publication number: 20040092564
    Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.
    Type: Application
    Filed: October 28, 2003
    Publication date: May 13, 2004
    Applicant: Wyeth
    Inventors: Ping Zhou, Michael Gerard Kelly
  • Cis-imidazolines
    Patent number: 6734302
    Abstract: The present invention provides compounds according to formula I and formula II and pharmaceutically acceptable salts and esters thereof, having the designations provided herein and which inhibit the interaction of MDM2 protein with a p53-like peptide and have antiproliferative activity.
    Type: Grant
    Filed: December 11, 2002
    Date of Patent: May 11, 2004
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Norman Kong, Emily Aijun Liu, Binh Thanh Vu
  • Compounds useful as reversible inhibitors of cathespin S
    Patent number: 6730671
    Abstract: Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes, for making such novel compounds.
    Type: Grant
    Filed: February 13, 2003
    Date of Patent: May 4, 2004
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Charles L. Cywin, Michel J. Emmanuel, Tina Morwick, Denice M. Spero, David S. Thomson, Yancey D. Ward
  • Amino methyl imidazoles as C5a receptor modulators
    Publication number: 20040082577
    Abstract: Amino methyl imidazoles of Formula I are provided: 1
    Type: Application
    Filed: August 21, 2003
    Publication date: April 29, 2004
    Applicant: Neurogen Corporation
    Inventors: Andrew Thurkauf, He Zhao, Suoming Zhang, Yang Gao
  • Aryl-benzimidazole compounds having antiinfective activity
    Patent number: 6716866
    Abstract: Aryl-benzimidazole compounds according to the formula where Ar1, R1, R2, Y, W, and N are as defined herein, bind to DNA and have antibacterial activity.
    Type: Grant
    Filed: June 6, 2002
    Date of Patent: April 6, 2004
    Assignee: GeneSoft Pharmaceuticals, Inc.
    Inventors: Dustin L. McMinn, Roland W. Bürli, Jacob Kaizerman, Eldon E. Baird, Matthew J. Taylor
  • Preparation and use of imidazole derivatives for treatment of obesity
    Publication number: 20040063691
    Abstract: This invention relates to substituted imidazole derivatives which have been found to suppress appetite and induce weight loss. The invention also provides methods for synthesis of the compounds, pharmaceutical compositions comprising the compounds, and methods of using such compositions for inducing weight loss and treating obesity and obesity-related disorders.
    Type: Application
    Filed: September 24, 2002
    Publication date: April 1, 2004
    Inventors: Roger A. Smith, Stephen J. O'Connor, Stephan-Nicholas Wirtz, Wai C. Wong, Soongyu Choi, Harold C.E. Kluender, Ning Su, Gan Wang, Furahi Achebe, Shihong Ying
  • Technical field
    Patent number: 6710044
    Abstract: Chemical compounds of the formula as well as pharmaceutical compositions containing them and methods for their use in the treatment of disorders and diseases responsive to modulation of the GABAA receptor complex of the central nervous system, such disorders and diseases including anxiety, sleep disorders, anesthesia, memory disorders, and epilepsy and other convulsive disorders.
    Type: Grant
    Filed: November 20, 2002
    Date of Patent: March 23, 2004
    Assignee: NeuroSearch A/S
    Inventors: Lene Teuber, Frank Wätjen
  • Novel isoindole derivatives
    Publication number: 20040053923
    Abstract: This invention relates to compounds represented by the general formula [I] 1
    Type: Application
    Filed: April 8, 2003
    Publication date: March 18, 2004
    Applicant: Banyu Pharmaceutical Co., Ltd.
    Inventors: Toshio Nagase, Tomoharu Iino, Yoshiyuki Sato, Teruyuki Nishimura, Jun-Ichi Eiki
  • Heterocyclically substituted benzimidazoles, the production and application thereof
    Patent number: 6696437
    Abstract: The present invention relates to novel benzimidazoles, their preparation and their use as inhibitors of the enzyme poly(ADP-ribose) polymerase or PARP (EC 2.4.2.30) for producing drugs.
    Type: Grant
    Filed: March 25, 2002
    Date of Patent: February 24, 2004
    Assignee: Abbott GmbH & Co. KG
    Inventors: Wilfried Lubisch, Michael Kock, Thomas Hoeger, Roland Grandel, Uta Holzenkamp, Sabine Schult, Reinhold Mueller
  • 2-(substituted-phenyl)amino-imidazoline derivatives
    Patent number: 6693200
    Abstract: This invention relates to IP receptor antagonists selected from the group of compounds represented by Formula I: where: R1 is a group represented by formula (A), (B) or (C); and other substituents as defined in the specification, and their pharmaceutically acceptable salts or crystal forms thereof; and pharmaceutical compositions containing them; and methods for their use as therapeutic agents.
    Type: Grant
    Filed: April 29, 2003
    Date of Patent: February 17, 2004
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Keith Roger Bley, Robin Douglas Clark, Alam Jahangir, Bruce Andrew Kowalczyk, Francisco Javier Lopez-Tapia, Alexander Victor Muehldorf, Counde O'Yang, Thomas Weitao Sun
  • New biphenyl and biphenyl-analogous compounds as integrin antagonists
    Publication number: 20040030132
    Abstract: The present invention relates to biphenyl and biphenyl-analogous compounds, their preparation and use as pharmaceutical compositions, as integrin antagonists and in particular for the production of pharmaceutical compositions for the treatment and prophylaxis of cancer, arteriosclerosis, restenosis, osteolytic disorders such as osteoporosis and ophthalmic diseases.
    Type: Application
    Filed: October 31, 2002
    Publication date: February 12, 2004
    Inventors: Markus Albers, Klaus Urbahns, Andrea Vaupel, Michael Harter, Delf Schmidt, Beatrix Stelte-Ludwig, Christoph Gerdes, Elke Stahl, Jorg Keldenich, Ulf Brueggemeier, Klemens Lustig
  • Lactam glycogen phosphorylase inhibitors and method of use
    Publication number: 20040002495
    Abstract: A compound of formula I 1
    Type: Application
    Filed: May 19, 2003
    Publication date: January 1, 2004
    Inventors: Philip Sher, Gang Wu, Terry Stouch, Bruce Ellsworth
  • Small molecules useful for the treatment of inflammatory disease
    Publication number: 20030232817
    Abstract: Compounds of the formula I 1
    Type: Application
    Filed: February 24, 2003
    Publication date: December 18, 2003
    Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventor: Roman Wolfgang Fleck
  • Viral polymerase inhibitors
    Publication number: 20030232816
    Abstract: A compound of the formula I: 1
    Type: Application
    Filed: September 10, 2002
    Publication date: December 18, 2003
    Applicant: Boehringer Ingelheim (Canada) Ltd.
    Inventors: Pierre Louis Beaulieu, Gulrez Fazal, James Gillard, George Kukolj, Volkhard Austel
  • 1-Phenyl-2-heteroaryl-substituted benzimdazole derivatives, their use for the production of pharmaceutical agents as well as pharmaceutical preparations that contain these derivatives
    Publication number: 20030229085
    Abstract: New benzimidazole derivatives are described, their production and their use for the production of pharmaceutical agents for treatment and prevention of diseases that are associated with a microglia activation and T-cell-mediated immunological diseases, as well as pharmaceutical preparations that contain the new benzimidazole derivatives.
    Type: Application
    Filed: February 14, 2003
    Publication date: December 11, 2003
    Applicant: Schering Aktiengesellschaft
    Inventors: Thorsten Blume, Wolfgang Halfbrodt, Joachim Kuhnke, Ursula Moenning, Bernd Elger, Herbert Schneider
  • Compounds useful in treating cytokine mediated diseases
    Publication number: 20030225053
    Abstract: Disclosed are amide compounds of formula(I): 1
    Type: Application
    Filed: April 10, 2003
    Publication date: December 4, 2003
    Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Donghong Amy Gao, Daniel R. Goldberg, Abdelhakim Hammach, Ming-Hong Hao, Victor Marc Kamhi, Neil Moss, Kevin Chungeng Qian, Gregory Paul Roth, Christopher Ronald Sarko, Alan David Swinamer, Zhaoming Xiong
  • Substituted indoles as alpha-1 agonists
    Publication number: 20030220319
    Abstract: This invention relates to compounds which are alpha-1 receptor agonists, preferably alpha-1A/L receptor agonists, and which are represented by Formula I: 1
    Type: Application
    Filed: January 31, 2003
    Publication date: November 27, 2003
    Inventors: Robert Greenhouse, Saul Jaime-Figueroa, Lubica Raptova
  • Melanin concentrating hormone receptor ligands: substituted benzoimidazole analogues
    Publication number: 20030216390
    Abstract: Melanin concentrating hormone receptor ligands (especially substituted benzoimidazole analogues), capable of modulating MCH receptor activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).
    Type: Application
    Filed: January 9, 2003
    Publication date: November 20, 2003
    Inventors: Robert W. DeSimone, John Peterson, Cheryl Steenstra, Yiping Shen, Linda Gustavson, Rajagopal Bakthavatchalam, Alan Hutchison
  • Benzimidazole derivatives and pharmaceutical compositions comprising these compounds
    Patent number: 6649609
    Abstract: The present invention relates to novel 1-phenylbenzimidazole derivatives having particular alkoxycarbonyl substituents in the 5-position of the benz ring and having particular cyclic substituents in the meta-position of the phenyl ring, as well as to pharmaceutical compositions containing these compounds and to methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of GABAA receptor complex, and in particular for inducing and maintaining anaesthesia, sedation, and muscle relaxation, as well as for combating febrile convulsions in children. The compounds of the invention may also be used by veterinarians.
    Type: Grant
    Filed: December 12, 2001
    Date of Patent: November 18, 2003
    Assignee: Neurosearch A/S
    Inventors: Lene Teuber, Frank Watjen
  • Phenylsulphonyl derivatives as 5-HT receptor ligands
    Publication number: 20030203889
    Abstract: A class of phenylsulphonyl derivatives wherein the sulphonyl moiety is also attached to an N-arylalkyl-substituted azetidine, pyrrolidine or piperidine ring are selective antagonists of the human 5-HT2A receptor and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of adverse conditions of the central nervous system, including schizophrenia and depression.
    Type: Application
    Filed: April 1, 2003
    Publication date: October 30, 2003
    Applicant: Merck & Co., Inc.
    Inventors: Peter Blurton, Frank Burkamp, Susan Koon-Fung Cheng, Stephen Robert Fletcher, Angus Murray MacLeod, Daniel Spinks, Monique Bodil Van Niel
  • Morpholine and thiomorpholine tachykinin receptor antagonists
    Patent number: 6638930
    Abstract: Substituted heterocycles of the general structural formula: are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.
    Type: Grant
    Filed: April 17, 2001
    Date of Patent: October 28, 2003
    Assignee: Merck & Co. Inc.
    Inventors: Conrad P. Dorn, Paul E. Finke, Jeffrey J. Hale, Malcolm Maccoss, Sander G. Mills, Shrenik K. Shah, Mark Stuart Chambers, Timothy Harrison, Tamara Ladduwahetty, Brian John Williams
  • Aryl fused aminoalkyl-imidazole derivatives: selective modulators of GABAa receptors
    Patent number: 6627624
    Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein the A, B, C, D, X, R1, R2, R3, R4, R5, and R6, are variables defined herein, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors, and are therefore useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, depression, overdose with benzodiazepine drugs, and enhancement of memory and alertness.
    Type: Grant
    Filed: March 31, 2000
    Date of Patent: September 30, 2003
    Assignee: Neurogen Corporation
    Inventors: Robert W. DeSimone, Alan Hutchison, Kenneth Shaw, Daniel L. Rosewater
  • Endothelin receptor antagonists
    Patent number: 6620826
    Abstract: Novel N-phenyl imidazole derivatives, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists are described.
    Type: Grant
    Filed: January 29, 2003
    Date of Patent: September 16, 2003
    Assignee: SmithKline Beecham Corporation
    Inventors: John Duncan Elliott, Joseph Weinstock, Jia-Ning Xiang
  • Substituted 3-heteroaryl(amino- or oxy)pyrrolidin-2-ones, their preparation and use as herbicides or plant growth regulators
    Publication number: 20030171218
    Abstract: A description is given of substituted 3-heteroaryl(amino- or oxy)pyrrolidin-2-ones of the formula (I), processes for preparing them, and their use as herbicides or as plant growth regulators.
    Type: Application
    Filed: July 9, 2002
    Publication date: September 11, 2003
    Inventors: Guido Bojack, Lothar Willms, Alfred Angermann, Hermann Bieringer, Hubert Menne, Thomas Auler
  • Technical field
    Publication number: 20030166638
    Abstract: Chemical compounds of the formula 1
    Type: Application
    Filed: November 20, 2002
    Publication date: September 4, 2003
    Applicant: NeuroSearch A/S
    Inventors: Lene Teuber, Frank Watjen
  • Heterocyclo-substituted imidazoles for the treatment of inflammation
    Patent number: 6613789
    Abstract: A class of imidazolyl compounds is described for use in treating inflammation. Compounds of particular interest are defined by Formula V: and pharmaceutically-acceptable salts thereof.
    Type: Grant
    Filed: December 5, 2001
    Date of Patent: September 2, 2003
    Assignee: G. D. Searle & Co.
    Inventors: Ish K. Khanna, Richard M. Weier, Paul W. Collins, Yi Yu, Xiangdong Xu, Richard A. Partis, Francis J. Koszyk, Renee M. Huff
  • Compounds useful as reversible inhibitors of cathepsin S
    Publication number: 20030158406
    Abstract: Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I), (Ia) and (II), (IIa) as defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes for making such novel compounds.
    Type: Application
    Filed: February 13, 2003
    Publication date: August 21, 2003
    Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Charles L. Cywin, Michel J. Emmanuel, Tina Morwick, Denice M. Spero, David S. Thomson, Yancey D. Ward
  • Isoindole derivatives
    Patent number: 6608098
    Abstract: This invention relates to compounds represented by the general formula [I]   wherein, R represents an azido group, etc., R1 and R2 are the same or different and represent hydrogen atoms, etc., R3 and R4 are the same or different and represent hydrogen atoms, etc., X1 represents an oxygen atom, etc., X2 represents an oxygen atom, etc., Y represents an oxygen atom, etc., and Z represents a condensed aryl group, etc., or a pharmaceutically acceptable salt thereof, preparation processes thereof, and an agent for treating diabetes, a prophylactic agent for chronic complications of diabetes or a drug against obesity, containing, as an effective ingredient, the compound or the pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: February 25, 2002
    Date of Patent: August 19, 2003
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Toshio Nagase, Tomoharu Iino, Yoshiyuki Sato, Teruyuki Nishimura, Jun-ichi Eiki
  • Compounds useful as reversible inhibitors of cathepsin S
    Patent number: 6608057
    Abstract: Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases.
    Type: Grant
    Filed: October 24, 2001
    Date of Patent: August 19, 2003
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Charles L. Cywin, Michel J. Emmanuel, Tina Morwick, Denice M. Spero, David S. Thomson, Yancey D. Ward
  • Endothelin receptor antagonists
    Publication number: 20030153567
    Abstract: Novel N-phenyl imidazole derivatives, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists are described.
    Type: Application
    Filed: January 29, 2003
    Publication date: August 14, 2003
    Applicant: SmithKline Beecham Corporation
    Inventors: John Duncan Elliott, Joseph Weinstock, Jia-Ning Xiang
  • 1-aryl- or 1-alkylsulfonylbenzazole derivatives as 5-hydroxytryptamine-6 ligands
    Publication number: 20030149018
    Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.
    Type: Application
    Filed: December 9, 2002
    Publication date: August 7, 2003
    Applicant: Wyeth
    Inventors: Ping Zhou, Michael Gerard Kelly
  • Substituted benzimidazole compounds
    Publication number: 20030144281
    Abstract: Disclosed are substituted benzimidazole compounds of formula(I): 1
    Type: Application
    Filed: November 5, 2002
    Publication date: July 31, 2003
    Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Charles Cywin, Jinbo Lee, Steven S. Pullen, Gregory Paul Roth, Christopher Ronald Sarko, Roger John Snow, Noel Stewart Wilson
  • Benzimidazole derivatives
    Publication number: 20030144286
    Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of inflammatory and immune-related conditions or disorders. In particular, the invention provides compounds which modulate the expression and/or function of proteins involved in inflammation, immune response regulation and cell proliferation. The subject compounds are 2-amino-imidazole derivatives.
    Type: Application
    Filed: October 9, 2002
    Publication date: July 31, 2003
    Applicant: Tularik, Inc
    Inventors: Alexander David Frenkel, Sarah Elizabeth Lively, Jay P. Powers, Andrew Smith, Daqing Sun, Craig Tomooka, Zhulun Wang
  • Substituted 2-cyclohexyl-4-phenyl-1H-imidazole derivatives
    Publication number: 20030144290
    Abstract: Substituted 2-cyclohexyl-4-phenyl-1H-imidazole derivatives capable of modulating NPY5 receptor activity, are provided. Such compounds may be used to modulate NPY binding to NPY5 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of disorders (e.g., eating disorders such as obesity or bulimia, psychiatric disorders, diabetes and cardiovascular disorders such as hypertension) in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such compounds for detecting NPY5 receptors.
    Type: Application
    Filed: October 21, 2002
    Publication date: July 31, 2003
    Applicant: NEUROGEN CORPORATION
    Inventors: Charles A. Blum, Harry L. Brielmann, Stephane De Lombaert, Xiaozhang Zheng
  • Method and structure for inhibiting activity of serine elastases
    Publication number: 20030134856
    Abstract: Therefore, it is critical that the roles these enzymes play in biological processes outside of extracellular matrix degradation or remodeling be understood in order to assess their potential as targets for therapeutic intervention, and to design safe, conveniently produced, orally active inhibitors.
    Type: Application
    Filed: December 23, 2002
    Publication date: July 17, 2003
    Inventor: John C. Cheronis
  • Compounds useful for treating hepatitis C virus
    Publication number: 20030134853
    Abstract: A series of compounds of Formula I are disclosed which are useful in treating viral hepatitus C.
    Type: Application
    Filed: September 26, 2002
    Publication date: July 17, 2003
    Inventors: Eldon Scott Priestley, Carl P. Decicco, Thomas W. Hudyma, Xiaofan Zheng
  • Benzimidazole compounds and drugs containing the same
    Patent number: 6593323
    Abstract: A benzimidazole compound or a salt thereof which has an inhibitory action of forming of macrophages and is useful as an active ingredient of a medicament for preventive and/or therapeutic treatment of arteriosclerosis, which is represented by the formula (I): wherein, R1 represents a functional group on the benzene ring selected from the group consisting of hydrogen atom, a halogen atom, a lower alkyl group and a lower alkoxy group; R2 represents hydrogen atom, an alkyl group or an acyl group; R3 represents a functional group on the ring containing the nitrogen atom and Z; Z represents a divalent group which forms a 5- or 6-membered ring; L represents a C4-C8 alkylene group or an ethyleneoxy linking group represented by (CH2CH2O)nCH2CH2 wherein n represents 1 or 2; and X represents O or S.
    Type: Grant
    Filed: June 3, 2002
    Date of Patent: July 15, 2003
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Kozo Aoki, Kazuhiro Aikawa, Masayuki Kawakami
  • Hydantoins and related heterocycles as inhibitors of matrix metalloproteinases and/or TNF-alpha converting enzyme (TACE)
    Publication number: 20030130273
    Abstract: The present application describes novel hydantoin derivatives of formula (I): 1
    Type: Application
    Filed: May 23, 2002
    Publication date: July 10, 2003
    Inventors: James E. Sheppeck, Jingwu Duan, Chu-Biao Xue, Zelda Wasserman
  • Benzimidazole derivatives, a process for their manufacture and use as a medicine
    Publication number: 20030130265
    Abstract: The invention concerns benzimidazole derivatives of the general formula (I) 1
    Type: Application
    Filed: September 9, 2002
    Publication date: July 10, 2003
    Applicant: Boehringer Ingelheim Pharma KG
    Inventors: Pascale Pouzet, Christoph Hoenke, Claudia Heine, Ralf Anderskewitz, Horst Dollinger, Herbert Nar, Hans Michael Jennewein, Bernd Disse
  • 1-Aryl-2-N-, S- or O-substituted benzimidazole derivatives, their use for the production of pharmaceutical agents as well as pharmaceutical preparations that contain these derivatives
    Publication number: 20030125550
    Abstract: The invention relates to novel benzimidazole derivatives with general formula I, whereby radicals R1, R2, R3, A, B, Y and Z have the meanings that are indicated in the description and the claims, the use of these compounds for the production of a pharmaceutical agent for treatment and prevention of diseases associated with microglia activation as well as pharmaceutical preparations that contain these compounds.
    Type: Application
    Filed: July 9, 2002
    Publication date: July 3, 2003
    Inventors: Thorsten Blume, Wolfgang Halfbrodt, Joachim Kuhnke, Ursula Monning, Herbert Schneider
  • Substituted guanidine derivatives
    Publication number: 20030119828
    Abstract: The present application relates to novel guanidine derivatives of the formula (I) 1
    Type: Application
    Filed: October 1, 2002
    Publication date: June 26, 2003
    Inventors: Klaus Wagner, Christoph Erdelen, Wolfram Andersch, Ulrike Wachendorff-Neumann, Andreas Turberg, Norbert Mencke
  • Method for producing heterocyclic compounds
    Publication number: 20030114667
    Abstract: The present invention relates to a process for the preparation of compounds of the formula (I) 1
    Type: Application
    Filed: March 26, 2002
    Publication date: June 19, 2003
    Inventors: Hermann Seifert, Uwe Stelzer
  • 3-substituted piperidines comprising urea functionality, and methods of use thereof
    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
  • Novel substituted imidazole compounds
    Publication number: 20030114452
    Abstract: Novel 1,4,5-substituted imidazole compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.
    Type: Application
    Filed: May 17, 2002
    Publication date: June 19, 2003
    Applicant: SmithKline Beecham Corporation
    Inventors: Jerry L. Adams, Ralph F. Hall
  • Transition metal mediated process
    Publication number: 20030109714
    Abstract: This invention relates to a transition metal mediated process for the preparation of optionally substituted 2-amino-benzoxazoles and or 2-amino-benzimidazoles, which are useful as therapeutic agents or as intermediates in the synthesis of therapeutic agents.
    Type: Application
    Filed: September 20, 2002
    Publication date: June 12, 2003
    Inventors: Neil Wishart, Alena Rudolph, Kurt Ritter