Abstract: Dialkyl 1-(2-pyridinylthio)-1,2-hydrazinedicarboxylate, N-oxides are prepared by reacting a 2-mercaptopyridine-N-oxide and a dialkyl azodicarboxylate. The end products are useful as antimicrobial agents and, especially, growth promotants in monogastric meat producing animals. A species of the group is diethyl 1-(2-pyridinylthio)-1,2-hydrazinecarboxylate, N-oxide.
Abstract: Certain N-carboxyalkyl prolyl-containing tripeptides have been prepared and found to improve kidney function. A species of the group of new compounds is N-(2-carboxyethyl)-L-prolyl-L-alanyl-L-proline which has diuretic activity and increases renal blood flow. The compounds are prepared by chemical reactions which couple an amino acid with a dipeptide.
Abstract: Prodrugs are described whose structures have a oligopeptide chain which is substituted by a nucleophilic chemotherapeutic residue at the .alpha.-position. The products have increased cell membrane permeability and beneficial physico-chemical properties.
Abstract: A new chemical sequence for preparing certain indoles is disclosed which employes certain 2-substituted-6-nitrophenylacetaldehyde semicarbazones claimed here. Said semicarbazones are cyclized to the indoles by low pressure hydrogenation.
Abstract: Copper salts of 2-hydroxypyridine-N-oxides have been demonstrated to possess an ability to alter the metabolic pattern in the digestive tract of food producing animals to make energy producing metabolic units which are more available for absorption by the animals. The copper salts, such as cupric 2-hydroxypyridine-N-oxide, are active ingredients in feed compositions and methods for increasing growth and feed efficiency of these animals.
Abstract: A series of new chemical compounds which are 4-aminoalkyl-2(3H)-indolones has been demonstrated to be D.sub.2 -agonists useful for treating hypertension. A representative compound of the series is 4-di-n-propylaminoethyl-2(3H)-indolone.
Abstract: A group of adamantyl containing intermediates is useful to prepare certain oligopeptides which improve kidney function. A representative species of this group is N-(1-adamantyl)-ethanoylproline.
Abstract: 2-(4-tert.-Butyl-2,6-dichlorophenylimino)imidazolidine is a anti-hypertensive chemical compound which has unexpected biological properties compared to those of clonidine.
Abstract: 1-(3,4-bis-(3-lower alkoxycarbonyl)-2-thioureido)-phenyl)-1-phenylethylenes, which have anthelmintic activity, are prepared by reacting various 1-(3,4-diaminophenyl)-1-phenylethylenes with an alkoxycarbonylisothiocyanate which is prepared, in turn, from an alkali metal thiocyanate and a lower alkyl haloformate.
Abstract: New 2-acylamino-5-phenylethenylbenzimidazoles have been prepared and found to have anthelmintic activity. A species of the invention is methyl [5-(1-phenylethenyl)-1H-benzimidazol-2-yl]carbamate.
Abstract: A series of prodrugs is described which have improved antimicrobial activity and physico-chemical properties. The structures of the biologically active ingredients are characterized by having a selected oligopeptide backbone attached, via the .alpha.-carbon of an L-alanyl unit thereof, by means of a disulfide link to the residue of an antimicrobial mercaptan.
Abstract: Methods and compositions using as active ingredients 2-(3H)-indolones whose structures having an aminoalkyl substituent at position 4 and a hydroxy group at position 7 of the indolone nucleus are used to produce selective dopaminergic activity resulting in improved kidney function, relief of the symptoms of congestive heart failure, long lasting anti-hypertensive activity and anti-anginal activity. A species of the active ingredients is 4-di-n-propylaminoethyl-7-hydroxy-2(3H)-indolone or its salts.
Abstract: 3-Carboxy-2-(.omega.-carboxyalkanoyl)-2-azabicyclo-[2.2.1]heptenes have been demonstrated to improve kidney function. 3-Carboxy-2-azabicyclo[2.2.1]heptane and its esters are important new chemical intermediates.
Type:
Grant
Filed:
April 5, 1982
Date of Patent:
September 20, 1983
Assignee:
SmithKline Beckman Corporation
Inventors:
Dimitri Gaitanopoulos, Joseph Weinstock
Abstract: A group of prolyl-.alpha.-lower alkylphenylalanine dipeptides have been found to improve kidney function especially on cumulative administration. A species is N-4-(4'-hydroxyphenyl)-butyryl-L-propyl-D,L-.alpha.-methyl-3,4-dimethoxyph enylalanyl-L-arginine.
Abstract: A new chemical sequence for preparing indoles is disclosed whose key reactions are reaction of a o-nitrotoluene with tris(dimethylamino)methane to give a .beta.-dimethylamino-o-nitrostyrene which is converted into a semicarbazone and cyclized.
Abstract: New 6-chloro-7,8-dihydroxy-1-(p-hydroxyphenyl)-2,3,4,5-tetrahydro-1H-3-benzaze pine hydrogen sulfate monoesters have been prepared and found to have potent renal dopaminergic activity. The most potent compound of the series is 6-chloro-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepin-4'-yl-h ydrogen sulfate.
Type:
Grant
Filed:
January 6, 1982
Date of Patent:
June 14, 1983
Assignee:
SmithKline Beckman Corporation
Inventors:
Richard H. Dewey, Bruce Y. Hwang, George Y. Kuo
Abstract: A group of adamantyl containing di- and tripeptides have been found to improve kidney function. A representative species of this group is N-(1-adamantyl)ethanoyl-L-proline-D,L-.alpha.-methylphenylalanyl-L-arginin e together with its salts.
Abstract: N-Acyltetrapeptides are described which are active in improving renal function. An exemplary species is N-4-(4-hydroxyphenyl)-butyryl-L-prolyl-D,L-.alpha.-methylphenylalanyl-glyc yl-L-proline.
Abstract: A chemical process is described for preparing 7,8-acetamido, hydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines which involves reacting a 7,8-quinone derivative of a 1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine with a benzyl or benzhydrylamine followed by hydrolysis of the resulting imine and reaction with acetic anhydride or acetyl chloride.
Type:
Grant
Filed:
August 14, 1981
Date of Patent:
May 3, 1983
Assignee:
SmithKline Beckman Corporation
Inventors:
Kenneth G. Holden, Carl Kaiser, Joseph Weinstock
Abstract: 3-Furylmethyl-6-halo-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzaze pines have potent dopaminergic activity. As such they have utility as antihypertensive and especially anti-Parkinsonism agents.