Abstract: The compounds of the following general structural formula (I) ##STR1## wherein R is hydrogen or C.sub.1-3 alkyl and the tetrahydro analogs thereof, are 3-hydroxy-3-methylglutarylcoenzyme A (HMG-CoA) synthase inhibitors and useful as antihypercholesterolemic agents for the treatment of disease in which the inhibition of cholesterol biosynthesis would by useful, such as arteriosclerosis, hyperlipidemia and familial hypercholesterolemia.
Type:
Grant
Filed:
April 28, 1986
Date of Patent:
June 14, 1988
Assignee:
Merck & Co., Inc.
Inventors:
John C. Chabala, Arthur A. Patchett, Michael D. Greenspan
Abstract: Novel lysine esters used as absorption enhancing agents for gastrointestinally and rectally administered drugs. Also provided are processes for preparation of said lysine ester compounds as well as pharmaceutical formulations and methods for their use as absorption enhancing agents.
Abstract: A dosage device for the delivery of a measured quantity of a liquid or flowable paste, such as a medicament, comprises a cup component and a compartmented component which is secured within the cup component and rotatable with respect thereto about an axis, the cup component having a radial base wall with an opening radially offset from the axis, the compartmented component having axially extending walls bounding a plurality of compartments each of which has an open end and each of which can be brought, by relative rotation of the two components, into alignment with the base wall opening, each compartment having in its outer wall an outlet which is at a respective different axial spacing from its open end, the cup component and that outer wall bounding a dispensing space to receive liquid or flowable paste from the compartment.
Abstract: Compounds having somatostatin-like activity have been found to be useful as local anti-inflammatory agents in the treatment of such conditions as, for example, psoriasis, eczema, seborrhea, and other localized inflammatory and allergic conditions. Particularly useful are cyclic and bridged somatostatin analogs.
Type:
Grant
Filed:
September 2, 1987
Date of Patent:
May 31, 1988
Assignee:
Merck & Co., Inc.
Inventors:
Evan R. Morgan, Daniel F. Veber, Sanford L. Steelman
Abstract: The addition of organolithium to dimethylhydrazones of certain ethers of a-hydroxyaldehydes results in the synthesis of threo- or erythro- intermediates readily convertible to threo- or erythro-2-amino alcohols.
Abstract: Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) or (II): ##STR1## and pharmaceutically acceptable salts thereof the compounds of the formula (II) in which R is hydrogen are disclosed.
Type:
Grant
Filed:
April 28, 1986
Date of Patent:
April 19, 1988
Assignee:
Merck & Co., Inc.
Inventors:
Byron H. Arison, Michael D. Greenspan, Joel B. Yudkovitz
Abstract: Novel substituted aminohydroxypropoxyphenyl oxazole and thiazole compounds and methods for their preparation are disclosed. These compounds, and their salts exhibit cardioselective .beta.-adrenergic blocking activity, and are useful as antihypertensive, cardioprotective, antiarrhythmic and antianginal agents.
Abstract: Novel substituted 4-heteroaryl-1,4-dihydropyridine compounds useful as calcium channel blockers, pharmaceutical compositions therof, and methods of treatment are disclosed.
Type:
Grant
Filed:
September 13, 1985
Date of Patent:
April 5, 1988
Assignee:
Merck & Co., Inc.
Inventors:
John J. Baldwin, Wasyl Halczenko, George D. Hartman, Brian T. Phillips
Abstract: Prodrugs of 3-hydroxy-3-methylglutarylcoenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formula (I): ##STR1## and pharmaceutically acceptable salts thereof are disclosed.
Type:
Grant
Filed:
September 29, 1986
Date of Patent:
April 5, 1988
Assignee:
Merck & Co., Inc.
Inventors:
John J. Baldwin, Wasyl Halczenko, George Hartman
Abstract: Drug delivery device retained in the stomach comprising at least one drug and a continuous solid-stick figure made from polymer(s) that releases said drug slowly over a controlled, predictable and extended period of time.
Type:
Grant
Filed:
May 7, 1987
Date of Patent:
April 5, 1988
Assignee:
Merck & Co., Inc.
Inventors:
Larry J. Caldwell, Colin R. Gardner, Robyn C. Cargill
Abstract: There is disclosed an overcap for a container with a primary cap for the removal of the contents thereof, whereby the overcap is easily assembled onto the container and completely surrounds the primary cap. When assembled, the overcap prevents access to the primary cap, and when removed, the overcap becomes irreversibly deformed such that visual evidence is clearly apparent that access to the primary cap has been gained. The irreversible deformity consists of tabs connecting the pull-tab to the overcap, and weakened areas in the side of the overcap which must be torn to allow removal of the primary cap.
Type:
Grant
Filed:
June 2, 1986
Date of Patent:
March 29, 1988
Assignee:
Merck & Co., Inc.
Inventors:
Norman D. Knopf, Heinz P. Meyer, Abraham Leibson
Abstract: Substituted 2-benzyl-mercapto-imidazoles and analogs were prepared from the nucleophlic substitution of an appropriately substituted benzoxyacetate with a 2-imidazole mercapto anion or an analog thereof. These compounds were found to be anti-inflammatory agents.
Abstract: The present invention is directed to compounds of the general formula I and pharmaceutically acceptable salts thereof: ##STR1## wherein: R=ethyl, propyl or isopropyl; andA=(CH.sub.2).sub.n wherein n is 2, 4 or 5, and C(CH.sub.2).sub.3.
Type:
Grant
Filed:
April 4, 1986
Date of Patent:
March 15, 1988
Assignee:
Merck & Co., Inc.
Inventors:
Donald J. Abraham, Otto W. Woltersdorf, Jr., Edward J. Cragoe, Jr.
Abstract: Thienopyridine sulfonamides are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure and disorders associated therewith such as glaucoma.
Type:
Grant
Filed:
December 8, 1986
Date of Patent:
March 15, 1988
Assignee:
Merck & Co., Inc.
Inventors:
Jacob M. Hoffman, Jr., Kenneth L. Shepard
Abstract: The present invention is directed to a method of treating a person for sickle cell anemia comprising administering to the person a therapeutically effective dosage of a compound of the general formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: R=ethyl, propyl or isopropyl; and ##STR2##
Type:
Grant
Filed:
April 4, 1986
Date of Patent:
March 15, 1988
Assignee:
Merck & Co., Inc.
Inventors:
Donald J. Abraham, Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr.
Abstract: Ocular inserts with or without pharmacologically active agents comprising low molecular weight polymers have a lower propensity to cause blurred vision compared with inserts prepared from high molecular weight hydroxypropyl cellulose. When an enteric coating material is included as a constituent of the matrix there is provided a means for controlling and predicting dissolution rates of the insert to yield a prolonged residence time.