Abstract: The compounds of this invention are substituted benzofurans and benzothiophenes having pharmacological activity. In particular, these compounds have coronary vasodilator activity and are useful in the treatment of angina pectoris.
Type:
Grant
Filed:
November 17, 1975
Date of Patent:
May 17, 1977
Assignee:
SmithKline Corporation
Inventors:
L. Martin Brenner, John M. Petta, Stephen T. Ross
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 of this invention are cephalosporins having a 7.beta.-acyloxy group and 7.beta.-hydroxy intermediates for the preparation thereof. The compounds have antibacterial activity.
Abstract: Thallous salts of .beta.-dicarbonyl compounds, prepared by reaction of the .beta.-dicarbonyl compounds with a thallous alkoxide, are treated with alkyl halides to give C-alkyl products in high yield, with acyl halides at room temperature to give C-acyl products, and with acyl halides at low temperatures to give O-acyl products. Thallous phenolates are esterified with acyl or aroyl halides. Anhydrides are also prepared, as are biaryls and bi-sec-alkyls. N-heterocyclics, including purines and pyrimidines, are N-alkylated. Lactams are O-acylated or N-alkylated.
Abstract: Cephalosporins containing a heterocyclicthiomethyl group at position 3 are prepared. The heterocyclic group is 5-oxo-.DELTA..sup.2 -1,2,4-triazolinyl, 5-thiono-.DELTA..sup.2 -1,2,4-triazolinyl, 5-oxo-.DELTA..sup.2 -1,2,4-thiadiazolinyl or 5-thiono-.DELTA..sup.2 -1,3,4-thiadiazolinyl. The compounds have antibacterial activity.
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 pyridyl substituted aminoalkylthioureas and ureas which are inhibitors of H-2 histamine receptors. A compound of this invention is N-methyl-N'-[2-(2-pyridylmethylamino)ethyl]thiourea.
Type:
Grant
Filed:
October 29, 1975
Date of Patent:
April 19, 1977
Assignee:
Smith Kline & French Laboratories Limited
Inventors:
Graham John Durant, John Colin Emmett, Charon Robin Ganellin
Abstract: Stable oxidase reagent solutions containing N,N,N',N'-tetramethyl-p-phenylenediamine or N,N-dimethyl-p-phenylenediamine for determining the presence of oxidase in microbial colonies.
Abstract: Substituted 3-(1-aminoethylidene)-5-cinnamoyl-2H-pyran-2,6(3H)-diones useful as inhibitors of certain antigen-antibody reactions, particularly in alleviating allergic manifestations such as asthma, are prepared by reaction of a 3-(1-aminoethylidene)-5-acetyl-2H-pyran-2,6(3H)-dione with an appropriately substituted benzaldehyde.
Abstract: Pharmaceutical compositions comprising a substituted 3-cinnamoyl-2H-pyran-2,6(3H)-dione and methods of inhibiting the antigen-antibody reaction by administering said compositions. Certain of the 3-cinnamoyl-2H-pyran-2,6(3H)-diones are novel compounds per se.
Type:
Grant
Filed:
February 19, 1976
Date of Patent:
March 29, 1977
Assignee:
SmithKline Corporation
Inventors:
Lawrence William Chakrin, Kenneth Means Snader, Chester Rhodes Willis
Abstract: Bis-phenoxypropanolamine derivatives are prepared. These compounds have .beta.-adrenergic stimulant activity particularly as selective bronchodilators.
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-aminocephalosporinic acid. The compounds have antibacterial activity.
Abstract: Novel cephalosporins with the trifluoroethyl-mercaptoacetamido, trifluoroethylsulfinylacetamido, and trifluoroethylsulfonylacetamido groups at position 7 are prepared. These compounds have antibacterial activity.
Abstract: The compounds are ethylene derivatives which are inhibitors of histamine activity, in particular, inhibitors of H-2 histamine receptors. A compound of this invention is 1-nitro-2-[2-((4-methyl-5-imidazolyl)methylthio)ethylamino]-2-[2-((3-chlor o-2-pyridyl)methylthio)ethylamino]ethylene.
Type:
Grant
Filed:
November 5, 1975
Date of Patent:
March 22, 1977
Assignee:
Smith Kline & French Laboratories Limited
Inventors:
Graham John Durant, John Colin Emmett, Charon Robin Ganellin, Hunter Douglas Prain
Abstract: Process for preparing heterocyclicalkylthioalkyl-N-cyanoguanidines and thioureas by treating a heterocyclicalkyl derivative with a mercaptoalkyl-N-cyanoguanidine or thiourea. Two specific products are N-cyano-N'-methyl-N"-[2-((5-methyl-4-imidazolyl)methylthio)ethyl]guanidine and N-methyl-N'-[2-((5-methyl-4-imidazolyl)methylthio)ethyl]thiourea, both useful as histamine H.sub.2 -antagonists.
Type:
Grant
Filed:
August 20, 1975
Date of Patent:
March 22, 1977
Assignee:
Smith Kline & French Laboratories Limited
Inventors:
Thomas Henry Brown, Graham John Durant, John Colin Emmett, Charon Robin Ganellin
Abstract: .alpha.-Aminoalkyl-3-(1,2-dihydroxyethyl)-4-hydroxy-benzyl alcohols having .beta.-adrenergic stimulant activity, particularly as selective bronchodilators, are disclosed.
Type:
Grant
Filed:
June 13, 1975
Date of Patent:
March 15, 1977
Assignee:
SmithKline Corporation
Inventors:
Timothy Yu-Wen Jen, Carl Kaiser, Joe R. Wardell