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)
  • Patent number: 6716990
    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
  • Patent number: 6703368
    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
  • Patent number: 6689804
    Abstract: A method for treating inflammatory and immune cell-mediated diseases by the administration of compounds of the formula I Exemplary are:
    Type: Grant
    Filed: July 16, 2002
    Date of Patent: February 10, 2004
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Jiang-Ping Wu, Terence Alfred Kelly, Rene Lemieux, Daniel R. Goldberg, Jonathan Emilian Emeigh, Ronald John Sorcek
  • Publication number: 20040010025
    Abstract: The present invention relates to new substituted benzimidazoles, their preparation and their use as agents against parasitic protozoa.
    Type: Application
    Filed: July 3, 2003
    Publication date: January 15, 2004
    Inventors: Gisela Greif, Axel Haberkorn, Bernd Baasner, Folker Lieb, Albrecht Marhold
  • Patent number: 6664283
    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.
    Type: Grant
    Filed: May 15, 2002
    Date of Patent: December 16, 2003
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Masamichi Okada, Yukinori Nagakura, Tetsuo Kiso, Takashi Toya, Satoshi Hayashibe
  • Patent number: 6664282
    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
  • Publication number: 20030203909
    Abstract: The present invention provides a compound represented by the formula (I) 1
    Type: Application
    Filed: April 29, 2003
    Publication date: October 30, 2003
    Inventors: Hiroyuki Ushio, Youichiro Naito, Naoki Sugiyama, Takafumi Kawaguchi, Makio Ohtsuki, Kenji Chiba
  • Publication number: 20030195361
    Abstract: This invention relates to compounds of Formula I 1
    Type: Application
    Filed: February 14, 2003
    Publication date: October 16, 2003
    Applicant: Pfizer Inc.
    Inventor: Daisy Joe Du Bois
  • Patent number: 6620529
    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.
    Type: Grant
    Filed: October 27, 2000
    Date of Patent: September 16, 2003
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Toshihiro Ise, Hisashi Okada
  • Publication number: 20030135056
    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
  • Publication number: 20030091861
    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):
    Type: Application
    Filed: August 21, 2002
    Publication date: May 15, 2003
    Applicant: FUJI PHOTO FILM CO., LTD.
    Inventors: Hisashi Okada, Toshihiro Ise
  • Patent number: 6545032
    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
  • Publication number: 20030055094
    Abstract: The invention provides compounds of the formula I 1
    Type: Application
    Filed: July 31, 2002
    Publication date: March 20, 2003
    Inventors: Chongqing Sun, Jeffrey A. Robl, Mark E. Salvati, Tammy Wang, Lawrence Hamann, David Augeri
  • Publication number: 20020193608
    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
  • Patent number: 6492408
    Abstract: Compounds of the formula I which are useful for treating or preventing inflammatory and immune cell-mediated diseases.
    Type: Grant
    Filed: June 27, 2000
    Date of Patent: December 10, 2002
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Jiang-Ping Wu, Terence Alfred Kelly, Rene Lemieux, Daniel R. Goldberg, Jonathan Emilian Emeigh, Ronald John Sorcek
  • Publication number: 20020183320
    Abstract: A novel bicyclic imidazo-5-yl-amine derivative of Formula I, 1
    Type: Application
    Filed: April 8, 2002
    Publication date: December 5, 2002
    Inventors: Matthias Gerlach, Corinna Maul
  • Publication number: 20020183369
    Abstract: This invention relates to compounds of Formula I 1
    Type: Application
    Filed: April 5, 2002
    Publication date: December 5, 2002
    Inventor: Daisy Joe Du Bois
  • Publication number: 20020183375
    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
  • Patent number: 6479527
    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
  • Patent number: 6461747
    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.
    Type: Grant
    Filed: July 21, 2000
    Date of Patent: October 8, 2002
    Assignee: Fuji Photo Co., Ltd.
    Inventors: Hisashi Okada, Toshihiro Ise
  • Patent number: 6462041
    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
  • Patent number: 6433183
    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
  • Patent number: 6414161
    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
  • Publication number: 20020072615
    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
  • Publication number: 20020045759
    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.
    Type: Application
    Filed: April 6, 2001
    Publication date: April 18, 2002
    Inventors: Craig A. Stump, Theresa M. Williams
  • Patent number: 6359144
    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
  • Publication number: 20020028949
    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
  • Publication number: 20010049385
    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
  • Patent number: 6316380
    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
  • Publication number: 20010003744
    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
  • Patent number: 6200987
    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.
    Type: Grant
    Filed: April 11, 2000
    Date of Patent: March 13, 2001
    Assignee: Celgene Corporation
    Inventor: George W. Muller