Abstract: The present invention relates to benzimidazolinylpiperidine derivatives useful as ligands for CGRP (Calcitonin Gene-Related Peptide) receptors, their use in therapy, pharmaceutical compositions comprising them and methods of treatment using them.
Type:
Grant
Filed:
May 30, 2001
Date of Patent:
April 22, 2003
Assignees:
Merck Sharpe & Dohme Ltd., Merck & Co, Inc.
Inventors:
Arthur A. Patchett, Raymond George Hill, Lihu Yang
Abstract: The invention encompasses the novel class of compounds represented by formula I, which are caspase-3 inhibitors.
The invention also encompasses certain pharmaceutical compositions for treatment of caspase-3 mediated diseases comprising compounds of formula I.
Type:
Grant
Filed:
December 2, 1999
Date of Patent:
April 22, 2003
Assignee:
Merck Frosst Canada & Co.
Inventors:
Erich L. Grimm, Johanne Renaud, Renee Aspiotis, Christopher I. Bayly, Robert Zamboni, Shawn Black
Abstract: The present invention is directed to compounds of the formula I:
(wherein R1, R2, R3, R4, R5, R6 and X 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.
Type:
Grant
Filed:
August 16, 2001
Date of Patent:
April 8, 2003
Assignee:
Merck & Co., Inc.
Inventors:
Lihu Yang, Gabor Butora, William H. Parsons, Alexander Pasternak
Abstract: The present invention provides a method of treating a neurodegenerative disease, and in particular Alzheimer's disease, Mild Cognitive Impairment or other objective memory impairment which comprises the co-administration of ARICEPT or other cholinesterase inhibitor or cholenergic angonist and an effective amount of a selective COX-2 inhibitor. Although a wide range of COX-2 inhibitors may be employed in combination with ARICEPT, there are preferred choices which are specifically set forth herein.
Abstract: Bronchial and respiratory disorders are treated by the separate, sequential, or simultaneous administration of i) an amount of N-(3,5-dichloropyrid-4-yl)-cyclopropylmethoxy-4-difluoromethoxybenzamide, the pyridyl N-oxide thereof, or a pharmaceutically acceptable salt of either compound; and ii) an amount of a leukotriene antagonist, wherein the sum of the first and second amounts is a therapeutically effective amount.
Abstract: Trisubstituted pyrroles are antiprotozoal agents useful in the treatment and prevention of protozoal diseases in human and animals, including the control of coccidiosis in poultry.
Type:
Grant
Filed:
November 10, 2000
Date of Patent:
March 4, 2003
Assignee:
Merck & Co., Inc.
Inventors:
Tesfaye Bitfu, Danqing D. Feng, Gui-Bai Liang, Mitree M. Ponpipom, Xiaoxia Qian, Michael H. Fisher, Matthew J. Wyvratt, Robert L. Bugianesi
Abstract: This invention encompasses the novel compounds of Formula I, which are useful in the treatment of caspase-3 mediated diseases.
The invention also encompasses certain pharmaceutical compositions comprising compounds of Formula I as well as methods for treatment of caspase-3 mediated diseases.
Type:
Grant
Filed:
September 7, 2001
Date of Patent:
February 25, 2003
Assignee:
Merck Frosst Canada & Co.
Inventors:
Yongxin Han, Andre Giroux, Erich L. Grimm, Renee Aspiotis, Cameron Black
Abstract: This invention encompasses the Form V polymorph of Compound A of structural formula:
which is useful in the treatment of cyclooxygenase-2 mediated diseases. The invention encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising the Form V polymorph of Compound A. The invention also encompasses a process for synthesizing the Form V polymorph of Compound A.
Type:
Grant
Filed:
May 25, 2001
Date of Patent:
February 18, 2003
Assignee:
Merck & Co., Inc.
Inventors:
Louis S. Crocker, Ian W. Davies, Richard G. Osifchin, Andrew Kotliar
Abstract: This invention encompasses a process for making a compound of Formula A
These compounds are intermediates useful in the preparation of certain non-steroidal anti-inflammnatory agents.
Type:
Grant
Filed:
January 17, 2002
Date of Patent:
December 17, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Cheng Yi Chen, Weirong Chen, Paul O'Shea, Lushi Tan, Richard Tillyer, Feng Xu, Philippe Dagneau
Abstract: 4-substituted cyclohexanes substituted in the 1-position with imidazopyridine either directly or through a C1-C4alkyl, C1-C4alkenyl, C1-C4alkynyl, C1-C4alkoxy, amino, aminoC1-C4alkyl, hydroxyC1-C4alkyl, carbonyl, cycloC3-C6alkyl or aminocarbonyl chain are effective as NMDA NR2B antagonists useful for relieving pain.
Type:
Grant
Filed:
May 21, 2001
Date of Patent:
December 17, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Wayne J. Thompson, David A. Claremon, Peter M. Munson, John A. McCauley
Abstract: There are disclosed compounds of formula (I)
and pharmaceutically acceptable salts thereof which exhibit utility for the treatment of cytokine mediated diseases such as arthritis.
Type:
Grant
Filed:
May 4, 2000
Date of Patent:
December 10, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Nigel J. Liverton, David A. Claremon, Cory R. Theberge
Abstract: The present invention is directed to pyrrolidine compounds of the formula I:
(wherein R1, R2, R3, R4c, R4d, and R4f are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-3 and/or CCR-5.
Type:
Grant
Filed:
March 1, 2000
Date of Patent:
December 3, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Jianming Bao, Robert K. Baker, William H. Parsons, Kathleen Rupprecht
Abstract: A COX-2 selective inhibiting drug is disclosed as useful in treating or preventing prostate cancer. The compound is used alone or in combination with other drugs.
Type:
Grant
Filed:
January 26, 2001
Date of Patent:
November 26, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Joanne Waldstreicher, Briggs W. Morrison
Abstract: The present invention provides a method of treating a neurodegenerative disease and in particular Alzheimers disease which comprises administering to a human in need thereof a therapeutically effective amount of a non-steroid COX-II inhibitor.
Type:
Grant
Filed:
February 28, 2001
Date of Patent:
November 26, 2002
Assignee:
Merck Frosst Canada, Inc.
Inventors:
Yves Ducharme, Jacques Yves Gauthier, Petpiboon Prasit, Yves Leblanc, Zhaoyin Wang, Serge Leger, Michel Therien
Abstract: The most thermodynamically stable crystalline form of the benzoic acid salt of 4″-deoxy-4″-epi-methylamino avermectin B1a/B1b as the hemihydrate is obtained by crystallization from organic solvents containing a controlled amount of water.
Type:
Grant
Filed:
January 20, 1995
Date of Patent:
November 26, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Raymond Cvetovich, James A. McCauley, Richard Demchak, Richard J. Varsolona
Abstract: Compounds of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.
Type:
Grant
Filed:
May 21, 2001
Date of Patent:
November 19, 2002
Assignee:
Merck & Co., Inc.
Inventors:
William K. Hagmann, George A. Doherty, Shrenik Shah
Abstract: Michael addition conducted in the presence of a zinc-amine complex and additional amounts of the amine component results in product with high diastereomeric excess.
Type:
Grant
Filed:
April 7, 2000
Date of Patent:
November 12, 2002
Assignees:
Merck & Co., Inc., Banyu Pharmaceutical Co., Ltd,
Inventors:
Ioannis Houpis, Ralph P. Volante, Fengrui Lang, Ilias Dorziotis, David Tschaen, Shinji Kato, Toshiaki Mase