Abstract: Cephalosporin compounds having a substituted phenylglycyl substituent at the 7-position and any of a variety of groups at the 3-position are prepared by acylation of a 7-aminocephalosporanic acid. The compounds have antibacterial activity.
Abstract: The compounds are N-(heterocyclomethylthioalkyl)derivatives of alkylguanidines, C-alkyl and C-aryl amidines and S-alkylisothioureas. The compounds may also have N'-lower alkyl or N'-(heterocyclomethylthioalkyl)substituents. Three compounds of the invention are S-methyl-N-[2-(5-methyl-4-imidazolylmethylthio)ethyl]isothiourea, N,N'-bis-[2-(5-methyl-4-imidazolylmethylthio)ethyl]acetamidine, N,N'-bis-[2-(5-methyl-4-imidazolylmethylthio)ethyl]N"-methylguanidine. The compounds of this invention are histamine H.sub.2 -antagonists.
Type:
Grant
Filed:
May 5, 1977
Date of Patent:
August 15, 1978
Assignee:
Smith Kline & French Laboratories Limited
Inventors:
Graham John Durant, Charon Robin Ganellin, Rodney Christopher Young
Abstract: A new method for preparing ticrynafen comprises reacting 2,3-dichloro-4-hydroxyphenyl-2-thienylmethanone with an alkali metal salt of chloro or bromo acetic acid in aqueous solvent. An advantageous aspect of the reaction is that yields are increased with the addition of an alkali metal iodide to the reaction mixture.
Abstract: New semisynthetic cephalosporins characterized by having structures with a 3-sulfomethyl-1,2,4-triazol-5-ylthiomethyl group at position 3. Exemplary is the antibacterially effective 7-D-mandelamido-3-(3-sulfomethyl-1,2,4-triazol-5-ylthiomethyl)-3-cephem-4- carboxylic acid disodium salt.
Abstract: The compounds are heterocyclomethylsulphinylethyl derivatives of N-cyanoguanidines, thioureas and 2-amino-1-nitroethylene which are histamine H.sub.2 -antagonists or are converted into histamine H.sub.2 -antagonists in the animal body. Two specific compounds of the present invention are 1-nitro-2-[2-((2-thiazolyl)methylsulphinyl)ethylamino]-2-[2-((2-thiazolyl) methylthio)ethylamino]ethylene and 1-nitro-2,2-bis-[2-((2-thiazolyl)methylsulphinyl)ethylamino]ethylene.
Type:
Grant
Filed:
April 13, 1977
Date of Patent:
August 8, 1978
Assignee:
Smith Kline & French Laboratories Limited
Inventors:
Graham J. Durant, Charon R. Ganellin, Torben Hesselbo, George R. White
Abstract: Heterocyclic compounds which are inhibitors of histamine activity, in particular, inhibitors of H-2 histamine receptors. A specific compound of this invention is 2-[2-(4-methyl-5-imidazolylmethylthio)ethylamino]-4-pyrimidone.
Type:
Grant
Filed:
October 29, 1976
Date of Patent:
August 1, 1978
Assignee:
Smith Kline & French Laboratories Limited
Inventors:
Graham John Durant, John Colin Emmett, Charon Robin Ganellin
Abstract: A group of 1-phenyl-1H-3-benzazepines whose structures are characterized by having a functional thio containing group on the 1-phenyl moiety and which have pronounced peripheral and diminished central dopaminergic activity. This activity is manifested in an anti-hypertensive effect in humans. Particular species of this group include 6-chloro-7,8-dihydroxy-1-p-methylthiophenyl-2,3,4,5-tetrahydro-1H-3-benzaz epine and its derivatives which have dopaminergic activity.
Type:
Grant
Filed:
January 19, 1977
Date of Patent:
August 1, 1978
Assignee:
SmithKline Corporation
Inventors:
Gregory Gallagher, Jr., Francis R. Pfeiffer, Joseph Weinstock
Abstract: New imidazolemethylphosphonium salts having a degradable group at the 2-position which are useful intermediates for preparing histamine H.sub.2 antagonists.
Type:
Grant
Filed:
May 24, 1977
Date of Patent:
August 1, 1978
Assignee:
SmithKline Corporation
Inventors:
Clifford Steven Labaw, Robert Lee Webb, George Robert Wellman
Abstract: A method of treating magnesium/potassium depletion which comprises administering pharmaceutical compositions comprising magnesium and potassium compounds, the equivalent weight of the magnesium being between 1 and 3 times the equivalent weight of the potassium, together with a pharmaceutical carrier such that the rate of release of the magnesium and potassium into the digestive system is controlled.
Type:
Grant
Filed:
November 19, 1975
Date of Patent:
August 1, 1978
Assignee:
Smith Kline & French Laboratories Limited
Abstract: Pharmaceutical compositions and methods of inhibiting H-1 and H-2 histamine receptors by administering an antihistamine and an H-2 histamine receptor inhibitor. Exemplary of the antihistamine in the compositions and methods of this invention is mepyramine and exemplary of the H-2 histamine receptor inhibitor is N-cyano-N'-methyl-N"-[2-((4-methyl-5-imidazolyl)-methylthio)ethyl]guanidin e.
Type:
Grant
Filed:
September 27, 1976
Date of Patent:
August 1, 1978
Assignee:
Smith Kline & French Laboratories Limited
Inventors:
James Whyte Black, Michael Edward Parsons
Abstract: Novel bicyclic .beta.-lactams and intermediates useful in their preparation are disclosed. In particular, 7.beta.-acyl-amino- and 7.beta.-amino-8-oxo-4-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acids are prepared. The acylated compounds are antibacterial agents.
Type:
Grant
Filed:
June 8, 1976
Date of Patent:
July 25, 1978
Assignee:
SmithKline Corporation
Inventors:
John G. Gleason, Kenneth G. Holden, William F. Huffman
Abstract: The compounds of this invention are cephalosporins having various acyl substituents at the 7-position and an alkanesulfonamidoalkyl substituted tetrazolylthiomethyl group at the 3-position of the cephem nucleus and intermediates for the preparation thereof. The 7-acylated compounds have antibacterial activity.
Abstract: 7.beta.-Substituted mercaptoacetamido-7.alpha.-methoxycephalosporanic acid and derivatives thereof are prepared. These compounds are antibacterial agents with improved properties.
Abstract: The compounds are novel N-substituted-N'-heterocyclic alkylthioureas, guanidines and 1-nitro-2,2-diaminoethylene compounds which are histamine H.sub.2 -antagonists.
Type:
Grant
Filed:
May 13, 1976
Date of Patent:
July 4, 1978
Assignee:
Smith Kline & French Laboratories Limited
Inventors:
Graham John Durant, Charon Robin Ganellin, Geoffrey Robert Owen, Rodney Christopher Young
Abstract: The compounds of this invention are cephalosporins having various acyl substituents at the 7-position and an ureidoalkyl substituted tetrazolylthiomethyl group at the 3-position of the cephem nucleus and intermediates for the preparation thereof. The 7-acylated compounds have antibacterial activity.
Abstract: The compounds are trialkylphosphinegold(I)2,3,4,6-tetra-O-(N-loweralkylcarbamoyl)-1-thio-.be ta.-D-glucopyranosides which have antiarthritic activity and, in particular, are of use in the treatment of rheumatoid arthritis.
Abstract: A new series of lower alkyl sulfonyl esters of S-tri-lower-alkylphosphinegold 1-thio-.beta.-D-glucopyranosides has been prepared and found to have anti-arthritic activity and, in particular, are of use in treating rheumatoid arthritis.
Abstract: The compounds are tri-substituted phosphinegold(I) 1-thio-.beta.-D-glucopyranosides which have antiarthritic activity and, in particular, are of use in the treatment of rheumatoid arthritis. Of the three substituents on the phosphine one is optionally substituted phenyl and the others are lower alkyl or lower alkoxy.
Abstract: A new series of lower alkyl ethers of S-tri-lower-alkylphosphinegold 1-thio-.beta.-D-glucopyranoside has been prepared and found to have anti-arthritic activity and, in particular, are of use in the treatment of rheumatoid arthritis.