Abstract: Selective .alpha..sub.2 -adrenergic receptor antagonists are effective in modifying gastrointestinal motility in a manner useful in the treatment of colonic spasm, irritable bowel syndrome and constipation.
Abstract: Benzo(f)isoquinoline compounds, particularly, penta- and tetrahydrobenzo(f)isoquinoline dicarboxylic acid compounds, their preparation and their use as calcium entry blockers are disclosed.
Abstract: Novel 2-sulfamoylbenzo[b]thiophenes and derivatives thereof are shown to be useful for the treatment of elevated intraocular pressure in compositions including ophthalmic drops and inserts.
Abstract: There is disclosed a macrolide isolated from the fermentation broth, with 22,23-dihydro avermectin Bla aglycone as a substrate, of a known microorganism identified as MA-5853. The structure of the novel compound isolated from the microorganism is presented based upon analytical studies. The compound is a highly potent antiparasitic, insecticidal, and anthelmintic agent. Compositions for such uses are also disclosed.
Type:
Grant
Filed:
July 29, 1985
Date of Patent:
May 26, 1987
Assignee:
Merck & Co., Inc.
Inventors:
Robert T. Goegelman, Raymond F. White, Edward S. Inamine
Abstract: There are disclosed novel compounds which are derived from 22,23-dihydro avermectin Bla aglycone, 13-deoxy-22,23 dihydro overmectin Bla aglycone and 13-deoxy-22,23-dihydro overmectin Blb aglycone. The six compounds are hydroxy adducts of the substrate avermectin compound at the 12a, 24, 24a, 26, 26a and 27 positions. The hydroxy adducts are prepared by incubating the substrate with the microorganism Cunninghamella blakesleeana and isolating the hydroxy adducts from the fermentation broth. The compounds are highly potent antiparasitic, insecticidal and anthelmintic agents.
Type:
Grant
Filed:
February 20, 1986
Date of Patent:
May 19, 1987
Assignee:
Merck & Co., Inc.
Inventors:
Robert T. Goegelman, Edward S. Inamine, Raymond F. White
Abstract: Substituted lactams and related compounds and methods for their preparation are disclosed. These compounds are useful as angiotensin converting enzyme inhibitors and as antihypertensives.
Abstract: Thiophene-2-sulfonamides with a 5-alkyl-substituent are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.
Abstract: Hydroxyalkyl-phenoxy-propan-2-olamines and novel esters thereof are oculoselective .beta.-blockers useful in the treatment of elevated intraocular pressure with little or no effect on the pulmonary or cardiovascular system.
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 formula (I): ##STR1## are disclosed. Also disclosed are pharmaceutical compositions and methods of use of the compounds of formula (I).
Abstract: 3-Hydroxybenzo[b]thiophene derivatives, such as 2-aralkyl, 2-alkyl and 2-alkenyl-3-hydroxybenzo[b]-thiophenes, were prepared by, among other methods, ring closure of 2-(2-carboxy-phenylthio)-.alpha.-substituted acetic acids. These compounds are found to be useful in the treatment of pain, fever, inflammation, arthritic conditions, asthma, allergic disorders, skin diseases, cardiovascular disorders, psoriasis, inflammatory diseases and other prostaglandin and/or leukotriene mediated diseases.
Type:
Grant
Filed:
March 11, 1985
Date of Patent:
May 5, 1987
Assignee:
Merck & Co., Inc.
Inventors:
Philippe L. Durette, Bruce E. Witzel, Kathleen M. Rupprecht, Allan N. Tischler, Timothy F. Gallagher
Abstract: The invention relates to compositions and methods of enhancing rectal absorption of L-dopa via the formation of an ester prodrug and optionally with a decarboxylase inhibitor.
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) and (II): ##STR1## and pharmaceutically acceptable salts of the compounds (II) in which Z is hydrogen are disclosed.
Type:
Grant
Filed:
May 5, 1986
Date of Patent:
April 28, 1987
Assignee:
Merck & Co., Inc.
Inventors:
William F. Hoffman, Clarence S. Rooney, Ta J. Lee
Abstract: The present invention is directed to a synergistic antimicrobial admixture comprising 2-bromo-2-bromomethylglutaronitrile and a formaldehyde donor.
Abstract: Compounds of the formula Het-O-CH.sub.2 -CHOR-CH.sub.2 -NHaralkyl where Het is a 10 membered N-containing ring are disclosed. The compounds are useful as pharmaceuticals.
Type:
Grant
Filed:
October 13, 1983
Date of Patent:
April 7, 1987
Assignee:
Merck & Co., Inc.
Inventors:
Joseph G. Atkinson, John J. Baldwin, David E. McClure
Abstract: A simple single step process for preparing alkyl and substituted alkyl esters of amino acids is described. The products are bioactive compounds including compounds useful as antihypertensive agents.
Abstract: Certain 6-(substituted-naphthyl)hydrocarbyl-4-hydroxytetrahydropyran-2-ones are unexpectedly potent in the treatment of familial hypercholesterolemia, hyperlipemia and atherosclerosis by virtue of their ability to inhibit the enzyme, 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG-CoA reductase).
Abstract: A stereoselective process for the preparation of antihypercholesterolemic agents of the HMG-CoA reductase inhibitor type comprises treatment of an intermediate .beta.-hydroxyketone with a trialkylborane and sodium borohydride at low temperatures.
Type:
Grant
Filed:
April 25, 1985
Date of Patent:
February 24, 1987
Assignee:
Merck & Co., Inc.
Inventors:
Thomas R. Verhoeven, James M. McNamara, Meyer Sletzinger
Abstract: Substituted imidazoles and methods for their preparation are disclosed. These imidazoles, and their salts, exhibit pharmacological activity which includes antihypertensive activity and .beta.-adrenergic blocking activity.
Abstract: The instant invention is directed to an admixture, and its use in inhibiting scale and corrosion in aqueous systems, comprising:(a) a water-soluble polymer having a weight average molecular weight of less than 25,000, as determined by low angle laser light scattering, comprising an unsaturated carboxylic acid and an unsaturated sulfonic acid, or their salts, having a ratio of 1:20 to 20:1, and(b) at least one compound selected from the group consisting of water-soluble polycarboxylates, phosphonates, phosphates, polyphosphates, metal salts and sulfonates.The instant invention is also directed to a method of inhibiting the formation of insoluble alluvial, metal oxide and metal hydroxide deposits in an aqueous system, comprising adding to the system at least 0.
Type:
Grant
Filed:
May 9, 1985
Date of Patent:
February 3, 1987
Assignee:
Calgon Corporation
Inventors:
Leonard J. Persinski, Jerry L. Walker, Bennett P. Boffardi