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:
March 31, 1997
Date of Patent:
April 28, 1998
Assignee:
Merck & Co., Inc.
Inventors:
Philip E. Sanderson, Adel M. Naylor-Olsen, Dona L. Dyer, Joseph P. Vacca, Richard C. A. Isaacs, Bruce D. Dorsey, Mark E. Fraley
Abstract: Compounds of the following general structure X-Y-Z-Aryl-A-B, for example, ##STR1## which inhibit osteoclast mediated bone resorption. Specifically, the compounds are useful for treating mammals suffering from a bone condition caused or mediated by increased bone resorption, who are in need of such therapy. The compounds may be administered in oral dosage forms such as tablets, capsules, e.g. sustained release capsules, powders, granules, and suspensions.
Type:
Grant
Filed:
September 26, 1996
Date of Patent:
April 21, 1998
Assignee:
Merck & Co., Inc.
Inventors:
George D. Hartman, Mark E. Duggan, William F. Hoffman, Nathan C. Ihle
Abstract: The invention is a pharmaceutical composition for intravenous administration to a patient comprisinga) a pharmaceutically effective amount of a compound having the formula ##STR1## as 2-S-(n-Butylsulfonylamino)-3-?4-(4-(piperidin-4-yl)butyloxy)phenyl!propion ic acid;b) a pharmaceutically acceptable amount of a citrate buffer effective to provide a pH of between about 5 and 7; andc) a pharmaceutically acceptable amount of a tonicity adjusting agent effective to make the formulation substantially isotonic with the osmotic pressure of the biological system of the patient.
Abstract: Fibrinogen receptor antagonists of the formula: ##STR1## are disclosed for use in inhibiting the binding of fibrinogen to blood platelets and for inhibiting the aggregation of blood platelets.
Type:
Grant
Filed:
September 23, 1996
Date of Patent:
February 24, 1998
Assignee:
Merck & Co., Inc.
Inventors:
George D. Hartman, Melissa S. Egbertson, Wasyl Halczenko, Ben Askew
Abstract: Fibrinogen receptor antagonists having the formula ##STR1## where L is L is (CH.sub.2).sub.p, where p is 1 or 2; and Z is --CR.sup.1 .dbd.CR.sup.
Type:
Grant
Filed:
February 22, 1995
Date of Patent:
February 17, 1998
Assignee:
Merck & Co., Inc.
Inventors:
George D. Hartman, John H. Hutchinson, Wasyl Halczenko
Abstract: Compounds of the invention have the following structure: ##STR1##
Type:
Grant
Filed:
January 16, 1997
Date of Patent:
February 3, 1998
Assignee:
Merck & Co., Inc.
Inventors:
William C. Lumma, Roger M. Freidinger, Stephen F. Brady, Philip E. Sanderson, Dong-Mei Feng, Terry A. Lyle, Kenneth J. Stauffer, Thomas J. Tucker, Joseph P. Vacca
Abstract: The invention is a highly efficient synthesis for making compounds of formula (iv) wherein R is C.sub.1-4 alkyl or benzyl; and R.sup.1, when present, is C.sub.1-4 alkyl, OH, O--C.sub.1-4 alkyl, or S--C.sub.1-4 alkyl; which are useful intermediates for making compounds such as those represented in formula (I).
Type:
Grant
Filed:
August 29, 1996
Date of Patent:
November 11, 1997
Assignee:
Merck & Co., Inc.
Inventors:
John Y. L. Chung, Dalian Zhao, David J. Mathre
Abstract: Peptides having the general sequence A-B-C-D-E-F-Z wherein A is Ala, B is pFPhe, C is, for example, Arg, D is Cha, E is, for example, hArg, F is, for example, Tyr, and Z is, for example NH.sub.2. The peptides are useful for promoting wound healing and arresting bleeding in a patient.
Type:
Grant
Filed:
December 15, 1995
Date of Patent:
October 28, 1997
Assignee:
Merck & Co., Inc.
Inventors:
Daniel F. Veber, Ruth F. Nutt, Dong-Mei Feng, Robert J. Gould, Thomas M. Connolly
Abstract: 4-substituted cyclohexylamine derivatives which are thrombin catalytic site inhibitors and which are useful as anticoagulants. These compounds show selectivity for thrombin over other trypsin-like enzymes and have oral bioavailability.
Type:
Grant
Filed:
October 12, 1994
Date of Patent:
September 30, 1997
Assignee:
Merck & Co., Inc.
Inventors:
Daniel F. Veber, S. Dale Lewis, Jules A. Shafer, Dong-Mei Feng, Ruth F. Nutt, Stephen F. Brady
Abstract: A method for treating a patient suffering from heartburn and having no substantial esophageal erosion, comprising administering to the patient a composition comprising an amount of famotidine between about 5 mg and 10 mg. In one embodiment, the amount of famotidine is about 5 mg. In another embodiment, the amount of famotidine is about 10 mg.A method for treating a patient suffering from heartburn and having no substantial esophageal erosion, comprising administering to the patient a composition comprising an amount of famotidine between about 5 mg and 10 mg, and an antacid. In one embodiment, the amount of famotidine is about 5 mg. In another embodiment, the amount of famotidine is about 10 mg.
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:
June 24, 1996
Date of Patent:
September 16, 1997
Assignee:
Merck & Co., Inc.
Inventors:
Philip E. Sanderson, Adel M. Naylor-Olsen, Dona L. Dyer, Joseph P. Vacca, Richard C. A. Isaacs, Bruce D. Dorsey, Mark E. Fraley
Abstract: The invention is a highly efficient synthesis for making compounds of formula: ##STR1## wherein n=0, 1, R is C.sub.1-4 alkyl or benzyl; andR.sup.1, when present, is C.sub.1-4 alkyl, OH, O--C.sub.1-4 alkyl or S--C.sub.1-4 alkyl. The process involves silane-mediated conjugation of 4-vinylpyridine to a substituted lactam.
Type:
Grant
Filed:
August 29, 1996
Date of Patent:
September 9, 1997
Assignee:
Merck & Co., Inc.
Inventors:
John Y. L. Chung, Dalian Zhao, James M. McNamara, David L. Hughes
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:
July 21, 1995
Date of Patent:
August 19, 1997
Assignee:
Merck & Co., Inc.
Inventors:
Mark E. Duggan, Melissa S. Egbertson, Wasyl Halczenko, George D. Hartman, William L. Laswell
Abstract: Novel fibrinogen receptor antagonists of the formula:X--Y--Z--Aryl--A--Bare provided in which the claimed compounds exhibit fibrinogen receptor antagonist activity, inhibit platelet aggregation and are therefore useful in modulating thrombus formation.
Type:
Grant
Filed:
June 1, 1995
Date of Patent:
July 15, 1997
Assignee:
Merck & Co., Inc.
Inventors:
Melissa S. Egbertson, Laura M. Vassallo, George D. Hartman, Wasyl Halczenko, David B. Whitman, James J. Perkins, Amy E. Krause, Nathan Ihle, David Alan Claremon, William Hoffman, Mark E. Duggan
Abstract: The invention concerns the identification on eosinophils of the A3 adenosine receptor subtype and the blockade of said receptor in order to achieve inhibition of eosinophil activation and degranulation.
Type:
Grant
Filed:
April 25, 1994
Date of Patent:
July 8, 1997
Assignee:
Merck & Co., Inc.
Inventors:
Marlene A. Jacobson, Robert G. Johnson, Christopher A. Salvatore
Abstract: The invention is directed to a series of novel compounds, and their pharmaceutically acceptable salts, of the formula ##STR1## wherein R is C.sub.0-6 alkyl substituted with R.sup.5 or a mono or polycyclic aromatic or heteroaromatic system comprised of 5 or 6-membered aromatic or heteroaromatic rings that are either unsubstituted or substituted with one or more of R.sup.1 and R.sup.2 ; R.sup.1 and R.sup.2 are independently C.sub.1-6 alkyl, carboxyl, hydroxyl, azido, nitro, amino, C.sub.1-6 alkylamino, C.sub.1-6 dialkylamino, arylamino, aryl C.sub.1-6 alkylamino, hydroxysulfonyl or arylazo; aryl is a phenyl or naphthyl ring which is unsubstituted or substituted with one or more of R.sup.3 and R.sup.4 ; R.sup.3 and R.sup.4 are independently C.sub.1-6 alkyl, azido, nitro, amino, C.sub.1-6 dialkylamino or hydroxysulfonyl; R.sup.5 is ##STR2## provided that when R is an unsubstituted monocyclic ring, the monocyclic ring is not phenyl or pyridyl.
Type:
Grant
Filed:
September 29, 1994
Date of Patent:
July 8, 1997
Assignee:
Merck & Co., Inc.
Inventors:
Bohumil Bednar, Melissa Egbertson, Robert J. Gould, George D. Hartman, Jules A. Shafer
Abstract: Compounds of the invention have the following structure: ##STR1## for example ##STR2## These compounds inhibit thrombin and associated thrombosis.
Type:
Grant
Filed:
April 10, 1995
Date of Patent:
May 13, 1997
Assignee:
Merck & Co., Inc.
Inventors:
Joseph P. Vacca, William C. Lumma, Stephen F. Brady, Thomas J. Tucker
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 utilized in an assay to identify and evaluate entities that bind to or enhance binding to adenosine receptors.
Type:
Grant
Filed:
December 5, 1994
Date of Patent:
February 4, 1997
Assignee:
Merck & Co., Inc.
Inventors:
Marlene A. Jacobson, Christopher J. Luneau, Robert G. Johnson, Christopher A. Salvatore