Abstract: The compositions and methods of the invention provide a convenient means for systemically administering an integrin receptor antagonist or a pharmaceutically effective amount thereof to a patient by introducing the antagonist, in an ophthalmic formulation, to the patient's eye.
Type:
Grant
Filed:
August 26, 1997
Date of Patent:
May 4, 1999
Assignee:
Merck & Co., Inc.
Inventors:
Michael F. Sugrue, George D. Hartman, Robert J. Gould
Abstract: A series of non-peptide derivatives that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet anti-aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.
Type:
Grant
Filed:
August 6, 1998
Date of Patent:
March 9, 1999
Assignee:
Merck & Co., Inc.
Inventors:
Mark E. Duggan, Melissa S. Egbertson, Wasyl Halczenko, George D. Hartman, William L. Laswell
Abstract: A compound which inhibits human thrombin and which has the general structure ##STR1##
Type:
Grant
Filed:
September 10, 1997
Date of Patent:
February 16, 1999
Assignee:
Merck & Co., Inc.
Inventors:
Adel M. Naylor-Olsen, Gerald S. Ponticello, Joseph P. Vacca, Randall W. Hungate, Craig Coburn, Brian T. Phillips, S. D. Lewis, Mark E. Fraley
Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: ##STR1## for example: ##STR2##
Type:
Grant
Filed:
April 21, 1997
Date of Patent:
February 2, 1999
Assignee:
Merck & Co., Inc.
Inventors:
Philip E.. Sanderson, Terry A.. Lyle, Bruce D. Dorsey, Richard J. Varsolona
Abstract: Fibrinogen receptor antagonists having the structureX--Y--Z--A--Band pharmaceutically acceptable salts, wherein X is a 5, 6 or 7 membered aromatic or nonaromatic ring, and Y is a 5 or 6 membered aromatic ring, e.g.
Type:
Grant
Filed:
June 26, 1997
Date of Patent:
December 29, 1998
Assignee:
Merck & Co., Inc.
Inventors:
Mark E. Duggan, Melissa S. Egbertson, George D. Hartman, Steven D. Young, Nathan C. Ihle
Abstract: A method for preventing heartburn episodes in a patient susceptible to suffering heartburn episodes following ingestion of heartburn-inducing food or beverage, comprising administering to the patient, 30 minutes prior to consumption by the patient of the food or beverage, a composition comprising an amount of famotidine of 10 mg.
Type:
Grant
Filed:
June 2, 1995
Date of Patent:
December 29, 1998
Assignees:
Merck & Co., Inc., Mc Neil-PPC, Inc.
Inventors:
Roger Berlin, Thomas N. Gates, Thomas Simon
Abstract: Fibrinogen receptor antagonists having the structure, for example, of ##STR1## for example ##STR2##
Type:
Grant
Filed:
October 15, 1996
Date of Patent:
December 22, 1998
Assignee:
Merck & Co., Inc.
Inventors:
Ben C. Askew, George D. Hartman, Mark E. Duggan, Steven D. Young, John H. Hutchinson, John S. Wai, Melissa S. Egbertson, Laura M. Vassallo, Laura A. Libby, Amy E. Krause, Wasyl Halczenko, Nathan C. Ihle
Abstract: The invention concerns recombinant human adenosine receptors A1, A2a, A2b and A3 which have been prepared by cDNA cloning and polymerase chain reaction techniques. The invention also concerns expression systems for these receptors and an assay using the expression systems. The recombinant adenosine receptors comprising the invention can be utililized in an assay to identify and evaluate entities that bind to or enhance binding to adenosine receptors.
Type:
Grant
Filed:
March 27, 1996
Date of Patent:
October 6, 1998
Assignee:
Merck & Co., Inc.
Inventors:
Marlene A. Jacobson, Christopher J. Luneau, Robert G. Johnson, Christopher A. Salvatore
Abstract: A series of non-peptide derivatives that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet anti-aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.
Type:
Grant
Filed:
May 22, 1997
Date of Patent:
September 29, 1998
Assignee:
Merck & Co., Inc.
Inventors:
Mark E. Duggan, Melissa S. Egbertson, Wasyl Halczenko, George D. Hartman, William L. Laswell
Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions and have the following structure: ##STR1## for example: ##STR2##
Type:
Grant
Filed:
February 19, 1997
Date of Patent:
August 11, 1998
Assignee:
Merck & Co., Inc.
Inventors:
Philip E. Sanderson, Terry A. Lyle, Joseph P. Vacca, William C. Lumma, Stephen F. Brady, Thomas J. Tucker
Abstract: Novel fibrinogen receptor antagonists of the formula: X--Y--Z-Aryl-A--B and the pharmaceutically acceptable salts thereof, wherein Aryl is a 5-membered aromatic ring system containing 1 or 2 heteroatoms chosen from N, O or S wherein ring atoms may be unsubstituted or substituted with R.sup.5 and wherein S may be substituted with 0, 1 or 2 oxygen atoms; and X comprises various Nitrogen substituents including aromatic or nonaromatic systems; Y comprises, for example, alkyl or alkylaminocarbonylalkyl groups and Z and A are substituents which when present are independently chosen from alkyl or alkyloxyalkyl or other groups as defined herein; B is (a) or (b). The claimed compounds exhibit fibrinogen receptor antagonist activity, inhibit platelet aggregation and are therefore useful in modulating or preventing thrombus formation.
Type:
Grant
Filed:
May 31, 1995
Date of Patent:
July 28, 1998
Assignee:
Merck & Co., Inc.
Inventors:
George D. Hartman, John D. Prugh, Melissa S. Egbertson, Mark E. Duggan, William Hoffman
Abstract: Fibrinogen receptor antagonists of the general formula:X-A-Y-Z-B Iand which includes, for example, the compounds of formula ##STR1## are useful for inhibiting the binding of fibrinogen to blood platelets, inhibiting the aggregation of blood platelets, treating thrombus formation or embolus formation, and preventing thrombus or embolus formation.
Type:
Grant
Filed:
February 26, 1997
Date of Patent:
July 14, 1998
Assignee:
Merck & Co., Inc.
Inventors:
John Wai, Thorsten E. Fisher, Mark E. Duggan, George D. Hartman, James J. Perkins
Abstract: The invention is a method for inhibiting activation of the human A3 adenosine receptor with adenosine, by treating the receptor a compound of the formula ##STR1## to treat asthma.
Type:
Grant
Filed:
August 8, 1996
Date of Patent:
July 14, 1998
Assignee:
Merck & Co., Inc.
Inventors:
Marlene A. Jacobson, Richard Norton, Prasun K. Chakravarty
Abstract: The invention provides a process for regioselective substitution of trifluorobenzoate/trifluorobenzonitrile to afford the difluorobenzoate/difluorobenzonitrile in good yields. The resulting difluorobenzoate/difluorobenzonitrile can again be regioselectively substituted with a second nucleophile to give monofluorobenzoate/monofluorobenzonitrile also in good yields. This process is particularly useful for forming key intermediates in the synthesis of oxytocin antagonist compounds.
Type:
Grant
Filed:
February 27, 1997
Date of Patent:
July 7, 1998
Assignee:
Merck & Co., Inc.
Inventors:
Joseph E. Lynch, Yao-Jun Shi, Kenneth M. Wells