At Least Three Ring Hetero Atoms In The Bicyclo Ring System (e.g., Furo- Imidazole, (1,2-a) Imidazole, Pyrazo (1,2-a) Imidazolidine, Etc.) Patents (Class 548/303.1)
Abstract: The invention relates to compounds of formula (2) in which R1, R2, R3 and R4 have the meanings indicated in the description, their preparation and their further reaction to give compounds of formula (1), in which A1, A2 and R4 have the meanings indicated in the description. The compounds of the formula (1) are valuable intermediates for the preparation of medicaments.
Type:
Grant
Filed:
June 11, 2002
Date of Patent:
April 6, 2004
Assignee:
Altana Pharma AG
Inventors:
Wolf-Rüdiger Ulrich, Christian Scheufler, Thomas Fuchss, Jörg Senn-Bilfinger
Abstract: This invention relates to peptide-containing &agr;-ketoamide inhibitors of cysteine and serine proteases, methods for making these compounds, and methods for using the same.
Type:
Grant
Filed:
June 12, 2001
Date of Patent:
March 9, 2004
Assignee:
Cephalon, Inc.
Inventors:
Sankar Chatterjee, John P. Mallamo, Ron Bihovsky, Gregory J. Wells
Abstract: This invention relates to pharmaceuticals for neuropathic pains comprising an mGluR1 receptor antagonist for systemic administration. Drugs efficacious in treating various neuropathic pain can be provided by the invention.
Abstract: Individual substituted [3,5,7]-1H-imidazo[1,5-a]imidazol-2(3H)-one compounds and their pharmaceutically-acceptable salts are disclosed, as are libraries of such compounds. Methods of preparing and using the libraries of compounds as well as individual compounds of the libraries are also disclosed.
Type:
Grant
Filed:
May 8, 2002
Date of Patent:
December 16, 2003
Assignee:
Torrey Pines Institute for Molecular Studies
Inventors:
Hassan M. ElAbdellaoui, John M. Ostresh, Richard A. Houghten
Abstract: A compound represented by general formula (113):
wherein R1 and R2 each represents a hydrogen atom, an aliphatic hydrocarbon group, an aryl group or a heterocylic group; Z1 represents an atomic group necessary to form a heterocycle; L represents a connecting group; and X represents O, S, Se, Te or N—R, wherein R represents a hydrogen atom, an aliphatic hydrocarbon group; an aryl group or a heterocyclic group.
Abstract: A novel class of imidazo heterocyclic compounds, pharmaceutical compositions comprising them and use thereof in the treatment and/or prevention of diseases and disorders related to the histamine H3 receptor. More particularly, the compounds are useful for the treatment and/or prevention of diseases and disorders in which an interaction with the histamine H3 receptor is beneficial.
Type:
Application
Filed:
July 23, 2002
Publication date:
July 17, 2003
Inventors:
Knud Erik Andersen, Florencio Zaragoza Dorwald, Bernd Peschke, Ulla Grove Sidelmann, Klaus Rudolf, Dirk Stenkamp, Rudolf Hurnaus, Stephan Georg Muller, Bernd Krist, Birgitte Eriksen
Abstract: Disclosed is a material for a light emitting device excellent in color purity, good in light emitting characteristics and excellent in stability, which consists of a compound represented by the following general formula (I):
Abstract: Individual substituted [3,5,7]-1H-imidazo[1,5-a]imidazol-2(3H)-one compounds and their pharmaceutically-acceptable salts are disclosed, as are libraries of such compounds. Methods of preparing and using the libraries of compounds as well as individual compounds of the libraries are also disclosed.
Type:
Grant
Filed:
September 12, 2000
Date of Patent:
April 8, 2003
Assignee:
Torrey Pines Institute for Molecular Studies
Inventors:
Hassan M. ElAbdellaoui, John M. Ostresh, Richard A. Houghten
Abstract: Individual substituted [3,5,7]-1H-imidazo[1,5-a]imidazol-2(3H)-one compounds and their pharmaceutically-acceptable salts are disclosed, as are libraries of such compounds. Methods of preparing and using the libraries of compounds as well as individual compounds of the libraries are also disclosed.
Type:
Application
Filed:
May 8, 2002
Publication date:
December 19, 2002
Inventors:
Hassan M. Elabdellaoui, John M. Ostresh, Richard A. Houghten
Abstract: The present invention relates to novel heterocyclic antagonists of Formula (I) and pharmaceutical compositions comprising said antagonists of the corticotropin releasing factor receptor (“CRF receptor”) 1
Type:
Application
Filed:
January 11, 2002
Publication date:
December 5, 2002
Inventors:
Gene M. Dubowchik, Xiaojun Han, Vivekananda M. Vrudhula, Dmitry Zuev, Bireshwar Dasgupta, Jodi A. Michne
Abstract: A pharmaceutical composition comprising a compound of formula (I):
or a pharmaceutically acceptable salt, ester or amide thereof, which is an inhibitor of monocyte chemoattractant protein-1 and wherein A and B together form an optionally substituted 5-member aromatic ring which includes at least one heteroatom; R1 is an optionally substituted aryl or heteroaryl ring; R2 is selected from a range of organic groups including carboxy, and R3 is hydrogen, or a range of organic groups; in combination with a pharmaceutically acceptable carrier. Certain compounds of formula (I) are novel and these form a further aspect of the invention.
Type:
Grant
Filed:
July 26, 2000
Date of Patent:
November 12, 2002
Assignee:
AstraZeneca UK Limited
Inventors:
Andrew J. Barker, Alan W Faull, Jason G. Kettle
Abstract: Disclosed is a material for a light emitting device excellent in color purity, good in light emitting characteristics and excellent in stability, which consists of a compound represented by the following general formula (I):
L&Parenopenst;A)m (I)
wherein A represents a heterocyclic group in which two or more aromatic heterocycles are condensed; m represents an integer of 2 or more, and the heterocyclic groups represented by A may be the same or different; and L represents a connecting group.
Abstract: The present invention is directed to gambogic acid, analogs and derivatives thereof, represented by the general Formulae I-III:
wherein R1-R5 are defined herein. The present invention also relates to the discovery that compounds having Formula I-III are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled cell growth and spread of abnormal cells occurs.
Type:
Grant
Filed:
February 1, 2000
Date of Patent:
October 8, 2002
Assignee:
Cytovia, Inc.
Inventors:
Sui Xiong Cai, Han-Zhong Zhang, Yan Wang, Ben Tseng, Shailaja Kasibhatla, John A. Drewe
Abstract: A novel process for the preparation of (R)-3-(4-Bromobenzyl)-1-(3,5-dichlorophenyl)-5-iodo-3-methyl-1-H-imidazo[1,2-&agr;]imidazol-2-one (1):
This compound is useful as an intermediate in the preparation of certain small molecules that are useful in the treatment or prevention of inflammatory and immune cell-mediated diseases. The present invention also relates to certain intermediates used in this novel process.
Type:
Grant
Filed:
February 15, 2002
Date of Patent:
August 13, 2002
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Rogelio P. Frutos, Michael Dale Johnson
Abstract: A novel process for the preparation of (R)-3-(4-Bromobenzyl)-1-(3,5-dichlorophenyl)-5-iodo-3-methyl- 1-H-imidazo[ 1 ,2-a]imidazol-2-one (1):
This compound is useful as an intermediate in the preparation of certain small molecules that are useful in the treatment of prevention of inflammatory and immune cell-mediated diseases. The present invention also relates to certain intermediates used in this novel process.
Type:
Grant
Filed:
July 31, 2001
Date of Patent:
July 2, 2002
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Rogelio P. Frutos, Michael Dale Johnson
Abstract: A novel process for the preparation of (R)-3-(4-Bromobenzyl)-1-(3,5-dichlorophenyl)-5-iodo-3-methyl-1-H-imidazo[1,2-a]imidazol-2-one (1): 1
Type:
Application
Filed:
February 15, 2002
Publication date:
June 13, 2002
Inventors:
Rogelio P. Frutos, Michael Dale Johnson
Abstract: The present invention is directed to peptidomimetic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
Abstract: The invention provides a rapid approach for combinatorial synthesis and screening of combinatorial libraries of bicyclic guanidine compounds. The present invention further provides the compounds made by the combinatorial synthesis and individually as well as methods of using the same.
Type:
Grant
Filed:
February 3, 1998
Date of Patent:
March 19, 2002
Assignee:
Lion Bioscience AG
Inventors:
John M. Ostresh, Jean-Philippe Meyer, Colette T. Dooley, Sylvie E. Blondelle, Christa C. Schoner, Richard A. Houghten
Abstract: A novel process for the preparation of (R)-3-(4-Bromobenzyl)-1-(3,5-dichlorophenyl)-5-iodo-3-methyl-1-H-imidazo[1,2-&agr;]imidazol-2-one (1): 1
Type:
Application
Filed:
July 31, 2001
Publication date:
March 7, 2002
Inventors:
Rogelio P. Frutos, Michael Dale Johnson
Abstract: A novel class of imidazo heterocyclic compounds, pharmaceutical compositions comprising them and use thereof in the treatment and/or prevention of diseases and disorders related to the histamine H3 receptor. More particularly, the compounds are useful for the treatment and/or prevention of diseases and disorders in which an interaction with the histamine H3 receptor is beneficial.
Type:
Application
Filed:
March 16, 2001
Publication date:
December 6, 2001
Inventors:
Knud Erik Andersen, Florencio Zaragoza Dorwald, Bernd Peschke
Abstract: This invention provides a catalyst system useful in many coupling reactions, such as Suzuki, Kumada, Heck, and amination reactions. The catalyst system of the present invention makes use of N-heterocyclic carbenes or their protonated salts. The composition of the catalyst system comprises at least one transition metal compound and at least one N-heterocyclic carbene or its protonated salt. This invention further provides novel N-heterocyclic carbenes and their protonated salts. One type of N-heterocyclic carbene used in this invention is an imidazolinc-2-ylidene wherein the 1 and 3 positions are each, independently, substituted by an aromatic group in which each ortho position is, independently, substituted by a secondary or tertiary group which has at least three atoms.
Type:
Grant
Filed:
February 22, 2000
Date of Patent:
November 13, 2001
Assignee:
University of New Orleans Research & Technology
Foundation
Inventors:
Steven P. Nolan, Jinkun Huang, Mark L. Trudell, Chunming Zhang
Abstract: The present invention relates to benzimidazole derivatives and their use in medical therapy particularly for the treatment or prophylaxis of virus infections such as those caused by herpes viruses. The invention also relates to the preparation of the benzimidazole derivatives and pharmaceutical formulations containing them.
Type:
Application
Filed:
December 14, 2000
Publication date:
June 14, 2001
Inventors:
Stanley Dawes Chamberlain, Susan Mary Daluge, George Walter Koszalka
Abstract: Cyclic amides are inhibitors of tumor necrosis factor and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is 3-phenyl-3-(1-oxoisoindolin-2-yl)propionamide.