Abstract: Substituted cyclopentanoindole derivatives are antagonists of prostaglandins, and as such are useful for the treatment of prostaglandin mediated diseases.
Type:
Grant
Filed:
July 20, 2001
Date of Patent:
June 25, 2002
Assignee:
Merck Frosst Canada & Co.
Inventors:
Marc Labelle, Claudio Sturino, Bruno Roy, Carl Berthelette, Michael Boyd, Nicolas Lachance, John Scheigetz
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:
June 15, 2001
Date of Patent:
June 11, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Stephen E. de Laszlo, Clare E. Gutteridge, William K. Hagmann, Theodore M. Kamenecka
Abstract: The present invention relates to novel nodulosporic acid derivatives, which are acaricidal, antiparasitic, insecticidal and anthelmintic agents.
Type:
Grant
Filed:
July 9, 2001
Date of Patent:
June 4, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Steven L. Colletti, Michael H. Fisher, Peter T. Meinke, Matthew J. Wyvratt
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:
August 17, 2000
Date of Patent:
March 5, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Stephen E. DeLaszlo, William K. Hagmann, Theodore M. Kamenecka
Abstract: The present invention relates to a process for the preparation of a compound of formula (I) or a sodium salt thereof
wherein HET is 7-chloroquinolin-2-yl or 6,7-difluoroquinolin-2-yl, which comprises: reacting the dilithium dianion of 1-(mercapto-methyl)cyclopropaneacetic acid with a compound of formula (II)
wherein HET is as defined above and L is arylsulfonyl or alkylsulfonyl. The invention further provides the dicyclohexylamine salt of a compound of formula (I).
Type:
Grant
Filed:
March 22, 1999
Date of Patent:
November 20, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Mahadevan Bhupathy, Daniel R. Sidler, James M. McNamara, Ralph P. Volante, James Bergan
Abstract: Certain novel spiropiperidine compounds are agonists of melanocortin receptor(s) and are useful for the treatment, control or prevention of diseases and disorders responsive to the activation of melanocortin receptors. The compounds of the present invention are therefore useful for treatment of diseases and disorders such as obesity, diabetes, sexual dysfunction including erectile dysfunction and female sexual dysfunction.
Type:
Grant
Filed:
June 10, 1999
Date of Patent:
September 25, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Ravi P. Nargund, Brenda L. Palucki, Zhixiong Ye, Raman K. Bakshi, Arthur A. Patchett, Leonardus H. T. Van Der Ploeg
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:
September 18, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Tesfaye Biftu, Danqing Dennis Feng, Gui-Bai Liang, Mitree M. Ponpipom, Xiaoxia Qian, Michael H. Fisher, Matthew J. Wyvratt
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 asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.
Type:
Grant
Filed:
July 22, 1999
Date of Patent:
September 18, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Philippe L. Durette, William K. Hagmann, Malcolm MacCoss, Sander G. Mills, Richard A. Mumford
Abstract: Amide derivatives are selective &bgr;3 adrenergic receptor agonists with very little &bgr;1 and &bgr;2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.
Type:
Grant
Filed:
October 12, 2000
Date of Patent:
September 18, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Ann E. Weber, Emma R. Parmee, Robert Mathvink, Wallace T. Ashton, Elizabeth M. Naylor
Abstract: Cyclic amino acid derivatives 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 asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.
Type:
Grant
Filed:
May 23, 2000
Date of Patent:
August 7, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Linda Chang, William K. Hagmann, Malcolm MacCoss
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 asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.
Type:
Grant
Filed:
November 29, 1999
Date of Patent:
April 24, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Philippe L. Durette, William K. Hagmann, Malcolm Maccoss, Sander G. Mills, Richard A. Mumford
Abstract: Leukotriene C4 synthase polypeptide identified by photoaffinity labelling, and purification of leukotriene C4 synthase to homogeneity is described.
Abstract: Substituted 5-aryl-2,4-thiazolidinediones are potent agonists of PPAR, and are therefore useful in the treatment, control or prevention of diabetes, hyperglycemia, hyperlipidemia (including hypercholesterolemia and hypertriglyceridemia), atherosclerosis, obesity, vascular restenosis, and other PPAR &agr;, &dgr; and/or &ggr; mediated diseases, disorders and conditions.
Type:
Grant
Filed:
November 23, 1999
Date of Patent:
March 13, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Soumya P. Sahoo, Wei Han, Richard L. Tolman, Jeffrey Bergman, Conrad Santini, Ranjit Desai, Victoria K. Lombardo, Julia K. Boueres, Dominick F. Gratale
Abstract: para-Aminomethylaryl carboxamides 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 asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.
Type:
Grant
Filed:
November 13, 1998
Date of Patent:
February 20, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Stephen E. DeLaszlo, William K. Hagmann
Abstract: Long-acting injectable formulations are formed from a) a therapeutic agent selected from insecticides, acaricides, parasiticides, growth enhancers or oil-soluble NSAIDs, b) hydrogenated castor oil, and c) a hydrophobic carrier comprising i) triacetin, benzyl benzoate, ethyl oleate, or a combination thereof, and ii) acylated monoglycerides, propyl dicaprylates/dicaprates, caprylic/capric acid triglycerides or a combination thereof.
Abstract: Substituted pyrrole derivatives of Formula I are antagonists of VLA-4 and/or .alpha..sub.4 .beta..sub.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 asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.
Type:
Grant
Filed:
November 9, 1998
Date of Patent:
July 18, 2000
Assignee:
Merck & Co., Inc.
Inventors:
Linda Chang, Malcolm MacCoss, William K. Hagmann
Abstract: Azapeptide acids of Formula I are antagonists of VLA-4 and/or .alpha..sub.4 .beta..sub.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 asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.
Abstract: Indolylquinones are useful for the treatment and prevention of diabetes mellitus, and in particular, for the treatment or prevention of hyperglycemia in diabetic patients. Some of the indolylquinones are produced by fermentation of the novel fungus Pseudomassaria sp. ATCC 74411.
Type:
Grant
Filed:
June 10, 1998
Date of Patent:
April 18, 2000
Assignee:
Merck & Co., Inc.
Inventors:
Bei Zhang, Royo Inmaculada, Fernando Pelaez, Gino M. Salituro, Gerald F. Bills
Abstract: Fused piperidine substituted arylsulfonamides are .beta..sub.3 adrenergic receptor agonists with very little .beta..sub.1 and .beta..sub.2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for decreasing gut motility are also disclosed.
Type:
Grant
Filed:
February 25, 1999
Date of Patent:
March 28, 2000
Assignee:
Merck & Co., Inc.
Inventors:
Linda Brockunier, Ann E. Weber, Emma R. Parmee