Abstract: The present invention is directed to compounds of the formula I: I(wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, n and the dashed line are defined herein) which are useful as modulators of chemokine receptor activity.
Inventors:
Richard Jiao, Stephen D. Goble, Sander G. Mills, Gregori Morriello, Alexander Pasternak, Lihu Yang, Changyou Zhou, Gabor Butora, Shankaran Kothandaraman, Deodialsingh Guiadeen, Christopher Moyes
Abstract: Triazole compounds substituted directly, or by a bridge, with a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl which are metabotropic glutamate receptor—subtype 5 (“mGluR5”) modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, bipolar disorder and panic, as well as in the treatment of pain, Parkinson's disease, cognitive dysfunction, epilepsy, circadian rhythm disorders, drug addiction, drug abuse, drug withdrawal and other diseases.
Type:
Grant
Filed:
December 13, 2002
Date of Patent:
September 12, 2006
Assignee:
Merck & Co., Inc.
Inventors:
Nicholas D. P. Cosford, Petpiboon Prasit, Jeffrey R. Roppe, Nicholas D. Smith, Lida R. Tehrani
Abstract: In accordance with the present invention, there are provided methods of modulating the activity of excitatory amino acid receptors using a specifically defined class of heterocyclic compounds. In one embodiment, there are provided methods of modulating metabotropic glutamate receptors. The present invention also discloses methods of treating disease using heterocyclic compounds.
Type:
Grant
Filed:
August 31, 1999
Date of Patent:
October 18, 2005
Assignee:
Merck & Co., Inc.
Inventors:
Nicholas D. P. Cosford, Ian A. McDonald, Stephen D. Hess, Mark A. Varney
Abstract: The present invention is directed to compounds of the formula I:
(wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, n and the dashed line are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
Inventors:
Richard Jiao, Gregori Morriello, Lihu Yang, Stephen D. Goble, Sander G. Mills, Alexander Pasternak, Changyou Zhou, Gabor Butora, Shankaran Kothandaraman, Deodialsingh Guiadeen, Christopher Moyes, Cheng Tang
Abstract: In accordance with the present invention, there is provided a novel class of heterocyclic compounds. Compounds of the invention contain a substituted, unsaturated five, six or seven membered heterocyclic ring that includes at least one nitrogen atom and at least one carbon atom. The ring additionally includes three, four or five atoms independently selected from carbon, nitrogen, sulfur and oxygen atoms. The heterocyclic ring has at least one substituent located at a ring position adjacent to a ring nitrogen atom. This mandatory substituent of the ring includes a moiety (B), linked to the heterocyclic ring via a carbon-carbon double bond, a carbon-carbon triple bond or an azo group. The mandatory substituent is positioned adjacent to the ring nitrogen atom. Invention compounds are capable of a wide variety of uses. For example heterocyclic compounds can act to modulate physiological processes by functioning as agonists and antagonists of receptors in the nervous system.
Type:
Grant
Filed:
August 13, 2002
Date of Patent:
August 10, 2004
Assignee:
Merck & Co., Inc.
Inventors:
Nicholas David Peter Cosford, Leo Solomon Bleicher, Jean-Michel Andre Vernier, Rowena V. Cube, Edwin Schweiger, Ian McDonald
Abstract: There are disclosed compounds of formula (I)
and pharmaceutically acceptable salts thereof which may be useful for the treatment of cytokine mediated diseases such as arthritis.
Type:
Grant
Filed:
December 20, 2000
Date of Patent:
July 27, 2004
Assignee:
Merck & Co., Inc
Inventors:
Christopher F. Claiborne, Nigel J. Liverton, David A. Claremon
Abstract: In accordance with the present invention, a novel class of substituted pyridine compounds (optionally containing ether, ester, amide, ketone or thioether substitutions) that promote the release of ligands involved in neurotransmission have been discovered. In a particular aspect compounds of the present invention are capable of modulating acetylcholine receptors. The compounds of the present invention are capable of modulating acetylcholine receptors. Invention compounds may act as agonists, partial agonists, antagonists or allosteric modulators of acetylcholine receptors.
Type:
Grant
Filed:
December 22, 1997
Date of Patent:
October 14, 2003
Assignee:
Merck & Co., Inc.
Inventors:
Jean-Michel Vernier, Nicholas D. P. Cosford, Ian A. McDonald
Abstract: A self-emulsifying system comprises i) microcrystalline cellulose and ii) an oily substance, surfactant, and water is useful for providing solid dosage forms of hydrophobic or water sensitive agents when dried or extruded and spheronized.
Type:
Grant
Filed:
October 15, 2001
Date of Patent:
October 7, 2003
Assignee:
Merck Sharp & Dohme Limited
Inventors:
Steven William Booth, Ashley Clarke, John Michael Newton
Abstract: Amino acid di- and tri-peptide analogs having C-terminal vinylic groups, pharmaceutical compositions containing the analogs and methods of treating diseases using cysteinyl protease inhibitors; particularly neurodegenerative, autoimmune, cognitive disorders, stroke and traumatic injury.
Type:
Grant
Filed:
June 22, 1999
Date of Patent:
September 9, 2003
Inventors:
Benito Munoz, Kuman Srinivasan, Bowei Wang