Abstract: There are disclosed perhydro-1,4-thiazepin-5-one and perhydro-1,4-thiazocin-5-one derivatives and related compounds which are useful as angiotensin converting enzyme inhibitors and as antihypertensives.
Type:
Grant
Filed:
April 29, 1985
Date of Patent:
June 10, 1986
Assignee:
Merck & Co., Inc.
Inventors:
Yak-Fa Cheung, Eugene D. Thorsett, Arthur A. Patchett
Abstract: 1-Aryloxy-3-(substituted aminoalkylamino)-2-propanols and pharmaceutically acceptable salts thereof have .beta.-adrenergic blocking activity with some cardioselectivity and hence are useful as antihypertensive, antianginal, antiarrhythmic and cardioprotective agents and in the treatment of elevated intraocular pressure such as glaucoma.
Type:
Grant
Filed:
April 2, 1984
Date of Patent:
June 3, 1986
Assignee:
Merck & Co., Inc.
Inventors:
John J. Baldwin, Sandor L. Varga, Gerald S. Ponticello
Abstract: Novel substituted indeno[2,1-c] pyridine compounds useful as calcium channel blockers, pharmaceutical compositions thereof, and methods of treatment are disclosed.
Type:
Grant
Filed:
April 24, 1985
Date of Patent:
June 3, 1986
Assignee:
Merck & Co., Inc.
Inventors:
George D. Hartman, Wasyl Halczenko, Steven D. Young
Abstract: Novel cyclopropyl pyridine compounds useful as calcium channel blockers, pharmaceutical compositions thereof, and methods of treatment are disclosed.
Abstract: The instant invention is directed to a method of inhibiting the precipitation and deposition of alkaline earth metal scales in an aqueous system, comprising adding to said system an effective amount of (a) an anionic polyelectrolyte; and (b) an anionic surfactant, wherein said polyelectrolyte/surfactant ratio ranges from 1000:1 to 1:10, by weight.
Abstract: Novel 5-amino or substituted amino 1,2,3-triazoles are disclosed as having anticoccidial activity. The compounds are useful for controlling coccidiosis when administered in minor quantities to animals, in particular to poultry, usually in admixture with animal sustenance.
Type:
Grant
Filed:
February 2, 1984
Date of Patent:
May 20, 1986
Assignee:
Merck & Co., Inc.
Inventors:
Richard J. Bochis, John C. Chabala, Michael H. Fisher
Abstract: N-(2-Imidazolidinylidene)-5H-dibenzo[a,d]cyclohepten-5-amine compounds are disclosed. The compounds have the property of inhibiting calcium induced contraction of smooth muscle. Certain of the compounds have properties of .alpha..sub.2 -adrenergic antagonists and others of .alpha..sub.2 -adrenergic agonists.
Abstract: An external bond at the 6-position of a 3,4,5,6-tetrahydro-2H-pyran-2-one, as found in the 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors, is readily epimerized by treating an amide of the corresponding hydroxy acid with a sulfonyl chloride reagent.
Abstract: Novel substituted and unsubstituted 13-(alkoxy)methoxy derivatives of the avermectin aglycones are useful as anthelmintic and antiparasitic agents. The compounds are also useful as pesticides and insecticides against agricultural pests. Included herein are novel intermediates useful in the process for preparing said avermectin aglycone derivatives. Compositions of said derivatives and methods of administering said compositions are also disclosed.
Abstract: Novel substituted and bridged pyridine compounds useful as calcium channel blockers and analgesics, pharmaceutical compositions thereof, and methods of treatment are disclosed.
Abstract: The invention in its broad aspects relates to caprylolactam derivatives which are useful as angiotensin converting enzyme inhibitors and as antihypertensives.
Type:
Grant
Filed:
July 9, 1982
Date of Patent:
May 6, 1986
Assignee:
Merck & Co., Inc.
Inventors:
Elbert E. Harris, Arthur A. Patchett, Eugene D. Thorsett
Abstract: The invention in its broad aspects relates to enantholactam derivatives which are useful as angiotensin converting enzyme inhibitors and antihypertensives.
Type:
Grant
Filed:
February 11, 1985
Date of Patent:
May 6, 1986
Assignee:
Merck & Co., Inc.
Inventors:
Elbert E. Harris, Eugene D. Thorsett, Arthur A. Patchett
Abstract: 5-[2(or 3)-Hydroxyphenylsulfonyl]thiophene-2-sulfonamides are useful for the topical treatment of elevated intraocular pressure. Ophthalmic compositions including drops and inserts are disclosed.
Abstract: Cyclic and bridged cyclic somatostatin analogs 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.
Abstract: The invention relates to fused tricyclic lactams and related compounds which are useful as angiotensin converting enzyme inhibitors and as antihypertensives.
Abstract: There are disclosed novel avermectin 8,9-cyclopropyl compounds (also referred to as 8,9-dihydro-8,9-methano avermectin compounds). The 8,9-cyclopropyl compounds are prepared by treating an avermectin compound with an iodohalomethane compound in the presence of an activated form of zinc. The avermectin 8,9-cyclopropyl compounds have utility as anti-parasitic agents and compositions for that use are also disclosed. The compounds are also highly potent insecticides against agricultural pests.
Abstract: There are disclosed novel avermectin and milbemycin compounds wherein the 13-position is oxidized to a keto function. The 13-keto derivatives are prepared from the 13-hydroxy compounds by oxidizing the 13-position with a suitable oxidizing agent. The avermectin and milbemycin 13-keto derivatives are active in their own right and also serve as intermediates in the preparation of 13-imino and 13-amino derivatives. The 13-keto, imino and amino compounds have utility as anti-parasitic agents and compositions for that use are also disclosed. The compounds are also highly potent insecticides against agricultural pests.
Abstract: A process is disclosed for obtaining manipulated proportions of the (+) and (-) enantiomers of [(6,7-dichloro-2,3-dihydro-2-methyl-1-oxo-2-phenyl-1H-inden-5-yl)oxy]aceti c acid by asymmetric chiral phase transfer catalysis.
Type:
Grant
Filed:
February 17, 1984
Date of Patent:
March 25, 1986
Assignee:
Merck & Co., Inc.
Inventors:
Ulf H. Dolling, Seemon H. Pines, Edward J. J. Grabowski