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: 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:
June 12, 2000
Date of Patent:
June 11, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Nigel J. Liverton, David A. Claremon, John W. Butcher, Cory R. Theberge
Abstract: Substituted 5-aryl-2,4-thiazolidinediones or 5-aryl-2,4-oxazolidinediones that also carry a second substituent in the 5-position of the heterocyclic ring 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:
June 16, 2000
Date of Patent:
June 4, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Soumya P. Sahoo, Conrad Santini, Julia K. Boueres, James V. Heck, Edward Metzger, Victoria K. Lombardo
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: Novel ethanes substituted with i) a phenyl, ii) a thiazole, and iii) a pyridyl moiety are PDE4 inhibitors.
Type:
Grant
Filed:
March 16, 2001
Date of Patent:
June 4, 2002
Assignee:
Merck Frosst Canada & Co.
Inventors:
Richard Freisen, Yves Ducharme, Bernard Cote, Marc Blouin, Evelyn Martins, Daniel Guay, Pierre Hamel, Mario Girard, Richard Frenette, Sebastien Laliberte
Abstract: Compounds according to Formula (I) or a pharmaceutically acceptable salt thereof are GABA-A Alpha 5 ligands useful for enhancing cognition:
where A is C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-6cycloalkyl, arylC1-6alkyl, or aryl wherein the aryl group is optionally substituted by halogen, C1-6alkyl, CF3, CN, NO2 or NH2, NR1R10, S(O)pR1, heteroarylC1-6alkyl or heteroaryl where heteroaryl is a 5- or 6-membered heteroaromatic ring as defined for B; and B is phenyl or a 5-membered ring having one or two unsaturations containing 1, 2, 3, or 4 heteroatoms chosen from O, N and S provided that not more than one heteroatom is other than N, a 6-membered heteroaromatic ring containing 1, 2, 3 or 4 nitrogen atoms, each of which rings is optionally substituted by one or more substituents.
Type:
Grant
Filed:
November 6, 2000
Date of Patent:
May 28, 2002
Assignee:
Merck Sharp & Dohme Limited
Inventors:
Howard Barff Broughton, Helen Jane Bryant, Mark Stuart Chambers, Neil Roy Curtis
Abstract: This invention relates to non-peptide somatostatin agonist compounds which are potent with high selectivity toward the receptor subtype 2. The compounds provide an improved therapeutic index in the treatment of diabetes, cancer, acromegaly and retenosis. Many of the compounds are orally active.
Type:
Grant
Filed:
June 16, 2000
Date of Patent:
May 14, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Changyou Zhou, Alexander Pasternak, Gregori Morriello, Liangqin Guo, Yanping Pan, Lihu Yang, Arthur Patchett
Abstract: The present invention is directed to a pesticidal composition of a water-soluble pesticide and processes for its manufacture. More specifically, the invention relates to a soluble granule (SG) pesticidal formulation comprising a water-soluble pesticide and a water-soluble filler. The present invention provides a pesticidal formulation with efficacy equal to the corresponding liquid formulation, yet with improved handler safety, such as lower eye irritation.
Type:
Grant
Filed:
May 25, 1999
Date of Patent:
May 14, 2002
Assignee:
Merck & Co., Inc.
Inventors:
John Misselbrook, Robert F. Peterson, Jr.
Abstract: Substituted 5-aryl-2,4-thiazolidinediones and oxazolidinediones 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; and/or &ggr; mediated diseases, disorders and conditions.
Type:
Grant
Filed:
June 16, 2000
Date of Patent:
April 30, 2002
Assignee:
Merck & Co. Inc.
Inventors:
Ranjit C. Desai, Soumya P. Sahoo, Jeffrey P. Bergman, Victoria K. Lombardo, Edward J. Metzger, Hiroo Koyama
Abstract: 4-substituted cyclohexanes substituted in the 1-position with quinazoline 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:
April 30, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Wayne Thompson, David A. Claremon, Peter M. Munson, John A. McCauley
Abstract: The invention encompasses novel compounds of Formula I as well as a method of treating NMDA mediated diseases comprising administration to a patient in need of such treatment a non-toxic amount of a compound of Formula I effective to block the NMDA NR2B receptor sub-unit.
The invention also encompasses certain pharmaceutical compositions for the treatment of NMDA mediated diseases comprising compounds of Formula I and a pharmaceutically acceptable carrier.
Type:
Grant
Filed:
April 17, 2000
Date of Patent:
April 23, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Christopher F. Claiborne, Nigel J. Liverton, David A. Claremon
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:
April 16, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Jianming Bao, Robert K. Baker, William H. Parsons, Kathleen Rupprecht
Abstract: Disclosed herein are compounds of Formula I
and pharmaceutically acceptable salts thereof which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders, including neurodegenerative disorders, disorders of gastrointestinal motility and inflammation.
Type:
Grant
Filed:
January 4, 2000
Date of Patent:
April 16, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Charles G. Caldwell, Malcolm Maccoss, William K. Hagmann, Shrenik K. Shah, Kothandaraman Shankaran, Karla L. Furman
Abstract: The present invention relates compounds of the formula (I):
wherein
R1, R2, R3, R4 and R5 represent a variety of substituents;
R6 represents hydrogen, CORa, CO2Ra, COCONRaRb, COCO2Ra, C1-6alkyl optionally substituted by a group selected from (CO2Ra, CONRaRb, hydroxy, CN, CORa, NRaRb, C(NOH)NRaRb, CONHphenyl(C1-4alkyl), COCO2Ra, CONHNRaRb, C(S)NRaRb, CONRaC1-6alkylR12, CONR13C2-6alkenyl, CONR13C2-6alkynyl, COCONRaRb, CONRaC(NRb)NRaRb, CONRaheteroaryl, and phenyl optionally substituted by one, two or three substituents selected from C1-6alky, C1-6alkoxy, halogen and trifluoromethyl); or R6 represents a group of formula —CH2C≡CCH2NR7R8 where R7 and R8 are as defined below; or R6 represents C1-6alkyl, optionally substituted by oxo, substituted by a 5-membered or 6-membered heterocyclic ring containing 1, 2 or 3 nitrogen atoms optionally substituted by ═O or ═S and optionally substituted by a group of the formula ZNR7R8;
or a pharmaceutical acceptable salt thereof.
Abstract: This invention encompasses the novel compounds of formula A, which are useful in the treatment of prostaglandin mediated diseases,
or a pharmaceutically acceptable salt, hydrate or ester thereof. The invention also encompasses certain pharmaceutical compositions and methods for treatment of prostaglandin mediated diseases comprising the use of compounds of formula A.
Type:
Grant
Filed:
September 14, 2000
Date of Patent:
April 9, 2002
Assignee:
Merck Frosst Canada & Co.
Inventors:
Patrick Lacombe, Marc Labelle, Rejean Ruel
Abstract: Novel 5-benzyl-octahydroindoles and 6-benzyl-decahydroquinolines substituted in the 1-position are effective as NMDA NR2B antagonists useful for relieving pain.
Type:
Grant
Filed:
October 25, 2000
Date of Patent:
April 9, 2002
Assignee:
Merck & Co. Inc.
Inventors:
Wayne Thompson, David A. Claremon, Peter M. Munson