Abstract: The invention provides tetrahydroquinolinylalkylamino pyrimidones, and ring homologues thereof, of the general formula (1): ##STR1## wherein R.sup.1 is hydrogen or an alkyl, alkoxy, halogen or amino-substituent, m and n are each 2, 3 or 4 and R.sup.2 is hydrogen, alkyl or variously substituted benzyl.The compounds are useful as histamine-H.sub.1 -receptor antagonists.
Abstract: A tamper evident seal for containers having a plastic shrink sleeve placed around the cap and neck and extending over the shoulder. A paper label is placed over a portion of the sleeve to prevent the sleeve from being removed intact. The sleeve has zigzag, saw-tooth perforations above and below a median line. The perforations are between the shoulder and cap of the container. When the cap is twisted and removed the plastic sleeve is randomly fragmented making it difficult, if not impossible to match in any attempt to reseal the container.
Abstract: Vasopressin antagonists which have a tripeptide side chain comprised of three basic amino acids, such as arginine, lysine or ornithine, demonstrate potent V.sub.1 and V.sub.2 -antagonist activity. A species of the invention, which is prepared by conventional peptide sequencing, is [1-(.beta.-mercapto-.beta.,.beta.-cyclopentamethylenepropionic acid)-2-(O-ethyl)-D-tyrosine-4-valine-7-arginine-8-arginine-9-arginine]-va sopression.
Abstract: Potent dopamine-.beta.-hydroxylase inhibitors having the Formula: ##STR1## which are useful to inhibit dopamine-.beta.-hydroxylase activity, pharmaceutical compositions including these inhibitors, and methods of using these inhibitors to inhibit dopamine-.beta.-hydroxylase activity in mammals. Also disclosed are novel intermediates useful in preparing the presently invented inhibitors.
Type:
Grant
Filed:
October 31, 1985
Date of Patent:
January 12, 1988
Assignee:
SmithKline Beckman Corporation
Inventors:
Carl Kaiser, Lawrence I. Kruse, Stephen T. Ross
Abstract: The invention relates to 5-oxo-1-imidazolidineacetamide derivatives which help restore learning and memory difficulties associated with ageing. A compound of the invention is 2,2-dimethyl-5-oxo-1-imidazolidineacetamide.
Type:
Grant
Filed:
June 20, 1986
Date of Patent:
January 12, 1988
Assignee:
Societe I.S.F. S.p.A.
Inventors:
Mario Pinza, Carlo Farina, Silvano Banfi, Ugo Pfeiffer
Abstract: 2- or 3-.beta.-Indolylalanyl and .beta.-indolylglycyl vasopressins are prepared by standard peptide synthetic methods. These 2- or 3-TRP vasopressins have vasopressin antagonist activity.
Abstract: A DNA fragment from Streptomyces sp. which contains a gene which can code for an excretable protein is isolated, inserted into a plamid vector and used to transform other Streptomycetes.
Type:
Grant
Filed:
December 14, 1984
Date of Patent:
January 5, 1988
Assignee:
SmithKline Beckman Corporation
Inventors:
Mary E. Brawner, Thomas G. Eckhardt, Louis R. Fare
Abstract: Vasopressin antagonists which have a dipeptide side chain comprised of two basic amino acids demonstrate potent V.sub.1 and V.sub.2 -antagonist activity. A species of the invention, which is prepared by conventional peptide sequencing, is [1-(.beta.-mercapto-.beta.,.beta.-cyclopentamethylene propionic acid)-2-(O-ethyl)-D-tyrosine-4-valine-7-arginine-8-arginine-9-desglycine]- vasopressin.
Abstract: Heterocyclic phosphine compounds, pharmaceutical compositions containing an effective, tumor cell growth-inhibiting amount of such a compound, and a method for treating tumor cells sensitive to such a compound which comprises administering a tumor cell growth-inhibiting amount of such a compound to an animal afflicted by said tumor cells.
Abstract: Disclosed is a temperature - sensitive (ts) mutant of bovine viral diarrhoea (BVD) virus which shows a considerably limited replication ability at the animal body temperature. The mutant is prepared by reacting wild-type BVD with a chemical mutagen such as nitrous acid. The mutant virous is advantageously used in vaccine compositions because it is capable of inducing immunity in bovines without causing serious side effects.
Abstract: Cysteamine is used as an active ingredient in animal feed compositions and in methods for increasing the feed efficiency of immature, monogastric, meat-producing animals. A particularly useful active ingredient of this invention is cysteamine hydrochloride in a quantity selected from the range of 15-1200 ppm.
Abstract: Vasopressin derivatives having unexpected VSP site binding activity whose structures are characterized by a Mpr unit at position 1 and a Pen unit at position 6 are prepared by standard peptide synthetic methods also using an oxidative cyclization of a linear peptide dimercaptan. A representative species is [1-.beta.-mercaptopropionic acid-2-(O-ethyl)-D-tyrosine-4-valine-6-penicillamine-8-arginine]vasopressi n.
Abstract: 1-Phenyl-3-benzazepine compounds are useful in treating gastrointestinal motility disorders. A particular compound of this invention is 8-hydroxy-3-methyl-1-phenyl-7-phenylthio-2,3,4,5-tetrahydro-1H-3-benzazepi ne.
Type:
Grant
Filed:
December 20, 1985
Date of Patent:
November 17, 1987
Assignee:
Smithkline Beckman Corporation
Inventors:
William E. Bondinell, Thomas Wen-Fu Ku, Herbert S. Ormsbee, III
Abstract: Compounds having the formula ##STR1## are .beta.-adrenergic receptor antagonists. Also disclosed are pharmaceutical compositions and methods for producing .beta.-adrenergic receptor antagonistic activity in animals including man.
Abstract: New intermediates, namely 2-(2-halo-3,4-dimethoxybenzyl)-5-(4-methoxyphenyl)-oxazolidines, are prepared by a synthetic sequence which uses a Darzen's reaction in a homogeneous solvent system.