Abstract: 2-(3-Substituted amino-2-hydroxypropoxy)-3-substituted pyrazine compounds optionally having substituents in the 5 and/or 6 positions, possessing .beta.-adrenergic blocking properties are described. The products are prepared by reaction of a 2-chloro (or hydroxy) pyrazine with a 5-hydroxymethyl (or sulfonyloxymethyl) oxazolidine followed by acid hydrolysis.
Abstract: Organic chemical compounds based upon the urea molecule are disclosed which have potent gastric secretion inhibitory properties. The urea is substituted with a 6 membered heterocyclic substituent containing 2 or 3 heteroatoms, and also with a substituted amino alkyl group. Further substitution is also possible. The compounds have profound effects on the inhibition of gastric secretions in the gastro-intestinal tract, and compositions for such uses are also disclosed.
Abstract: Certain novel substituted imidazo [1,2-a] pyridines with a substituted amino group at the 2- or 3- position and a heterocyclic moiety on the pyrido portion of the molecule are active anthelmintic agents. The heterocyclic moiety is connected to the imidazo [1,2-a] pyridine molecule through an oxygen, sulfur, sulfinyl or sulfone. The novel compounds are prepared from the appropriately substituted 2-amino pyridine precursor. Compositions which utilize said novel imidazo [1,2-a] pyridines as the active ingredient thereof for the treatment of helminthiasis are also disclosed.
Abstract: Organic chemical compounds based upon the urea molecule are disclosed which have potent gastric secretion inhibitory properties. The urea is substituted with a 6 membered heterocyclic substituent containing 2 or 3 heteroatoms, and also with a substituted amino alkyl group. Further substitution is also possible. The compounds have profound effects on the inhibition of gastric secretions in the gastro-intestinal tract, and compositions for such uses are also disclosed.
Abstract: Carbohydrate derivatives of the antibiotic substance milbemycin, also identified as B-41, and of 13-hydroxy milbemycin are prepared. The carbohydrate groups are attached to the available hydroxy groups of milbemycin and to the hydroxy group synthesized at the 13-position. The reactions may be made selectively such that more than one carbohydrate group may be attached to a single position, or that multiple carbohydrate groups may be attached at different positions on the molecule. The described carbohydrate derivatives have antiparasitic activity.
Abstract: Certain novel substituted imidazo [1,2-a] pyridines with a substituted amino group at the 2- or 3-position are active anthelmintic agents. The novel compounds are prepared from the appropriate substituted 2-aminopyridine precursor. Compositions which utilize said novel imidazo [1,2-a] pyridines as the active ingredient thereof for the treatment of helminthiasis are also disclosed.
Abstract: The invention disclosed herein relates to a novel process for preparing the monomer, 3-[N-(3-chloropropyl)methylamino]-N,N,N-trimethyl-propan-1-aminium chlorid e, which comprises reacting N,N-bis(3-chloropropyl)methylamine with trimethylamine. The 3,3-ionene monomer thus obtained is a key intermediate for making the linear, unbranched, non-cross-linked polymer, poly-[{methyl-(3-trimethylammoniopropyl)imino}trimethylene dichloride], which is valuable as an oral bile acid sequestrant.
Abstract: The invention disclosed herein relates to antiandrogenic compositions active, in vivo, as inhibitors of the aggregation of mammalian blood platelets, and to the method of preventing, arresting or reversing blood platelet aggregation by the administration to mammals of such antiandrogenic compositions.
Type:
Grant
Filed:
June 23, 1977
Date of Patent:
May 30, 1978
Assignee:
Merck & Co., Inc.
Inventors:
Glen E. Arth, Sumner Wood, Jr., deceased
Abstract: Novel cyano substituted (3-loweralkylamino-2-R.sub.1 O-propoxy)pyridines, their pharmaceutically acceptable salts and their preparation are disclosed. The pyridines are vasodilators having antihypertensive activity of rapid onset and extended duration and reduced tendency to cause undesirable tachychardia; they are also .beta.-adrenergic blocking agents.
Abstract: The invention disclosed herein relates to novel partially cross-linked, fully quaternized poly-[(methylimino)trimethylene] polymers wherein a minor proportion (1% to 20%) of the nitrogen atoms in adjacent poly-[(methylimino)trimethylene] linear chains are, by quaternization, joined through trimethylene or 2-hydroxy-trimethylene bridges, the non-cross-linked nitrogens in the said linear chains being fully quaternized with lower alkyl or trialkylammoniopropyl groupings; and to the novel process for preparing these partially cross-linked, fully quaternized polymers which comprises reacting poly-[(methylimino)trimethylene] with 0.01 to 0.2 equivalents of 1,3-dihalo-propane or 1,3-dihalo-2-hydroxypropane per equivalent of tertiary amine in said poly-[(methylimino)trimethylene], and subsequently reacting the resulting product with excess alkyl halide or 3-halopropyltrialkylammonium halide.
Abstract: Anthelmintically active 3-loweralkyl-1,2,4-oxadiazoles are stabilized by the formation of homogeneous mixtures thereof with water and with certain alcohols, the molar ratio of stabilizer to oxadiazole being adjusted to within 0.1:1 to 2:1 to achieve required stability.
Type:
Grant
Filed:
January 9, 1976
Date of Patent:
January 10, 1978
Assignee:
Merck & Co., Inc.
Inventors:
Michael H. Fisher, George B. Smith, Dale R. Hoff
Abstract: Substituted trichloroacetamidine derivatives are prepared by treating an appropriately substituted imidate with ammonia. The imidate intermediates are prepared by treating an appropriately substituted amine with an imidating reagent.
Abstract: Substituted trichloroacetamidine derivatives are prepared by reacting trichloroacetamidine with an appropriately substituted compound also substituted with a suitable leaving group. The leaving groups are halogen, quaternary or tertiary amines, methanesulfonate, toluenesulfonate, and the like.
Abstract: Substituted trichloroacetamidine derivatives are prepared by reacting an appropriately substituted amine with trichloroacetamidine or a trichloroacetimidate. The substituted amines are 3-aminomethyl indole and 2-acetoxy-3-phenoxy propylamine.
Abstract: Novel substituted benzenedisulfonamides are disclosed which compounds are active anthelmintic agents being particularly useful against fascioliasis in sheep and cattle. Specifically the active compounds are 4-amino-1,3-benzenedisulfonamide with an unsaturated substituted alkyl group. Compositions and methods containing the novel substituted benzenedisulfonamides for use in anthelmintic therapy particularly against liver fluke are also disclosed.
Abstract: Substituted benzenedisulfonamides are disclosed, which are active anthelmintic agents being particularly useful against fascioliasis in sheep and cattle. Specifically the active compounds are 4-amino-1,3-benzenedisulfonamide compounds substituted at the 6-position with certain alkyl groups. Compositions and methods containing the novel substituted benzenedisulfonamides for use in anthelmintic therapy, particularly against liver fluke are also disclosed.
Abstract: The nutritional disease, lactic acidosis, is successfully prevented by orally administering to the animal an effective amount of a sulfur-containing peptide antibiotic. In particular thiopeptin and thiostrepton are particularly effective sulfur-containing peptide antibiotics useful against lactic acidosis.
Abstract: Novel pharmaceutical compositions are disclosed which comprise a hypotensive agent and a phenyl hydrazino substituted propionic acid decarboxylase inhibitor. The compositions have enhanced anti-hypertensive activity.
Abstract: 5-Deazariboflavin, its phosphate ester and non-toxic salts thereof and its novel bis(loweralkoxymethylene) derivatives have antiprotozoal and antiparasitic activity. They are particularly useful for controlling cecal and/or intestinal coccidiosis when administered in minor quantities to animals, in particular to poultry, usually in admixture with animal sustenance. The compounds are included in compositions useful for the prevention and treatment of coccidiosis in poultry.
Type:
Grant
Filed:
November 2, 1976
Date of Patent:
October 11, 1977
Assignee:
Merck & Co., Inc.
Inventors:
Donald W. Graham, Edward F. Rogers, Wallace T. Ashton
Abstract: Compounds useful in the treatment of asthma, the symptoms of allergy and in some instances in gout and hyperuricemia are described. The novel compounds are 1-substituted-1,2,4-triazoles being additionally substituted at the 3- and 5-positions with a pyridyl radical. Methods of preparing these tri-substituted triazoles are described.