Abstract: This invention is directed to the use of certain arylacetylene compounds, principally as anti-inflammatory agents but also as anti-pyretic agents and as analgesic agents.
Abstract: 7-Acylamido- and 7-amino-3-halo-3-cephem-4-carboxylic acids, esters and pharmaceutically-acceptable salts and esters thereof are new cephalosporin compounds provided by the reaction of a 7-acylamido-3-hydroxy-3-cephem-4-carboxylic acid ester or a 7-amino-3-hydroxy-3-cephem-4-carboxylic acid ester with an iodinating, fluorinating, chlorinating, or brominating reagent. For example, 7-amino-3-chloro-3-cephem-4-carboxylic acid and 7-phenoxyacetamido-3-chloro-3-cephem-4-carboxylic acid are provided. The 7-acylamido-3-halo cephalosporin acids and pharmaceutically acceptable salts and esters provided are valuable antibiotic compounds having desirable therapeutic properties.
Abstract: Benzimidazolyl, benzothiazolyl and benzoxazolyl ureas and thioureas are employed as immune regulatory agents, as agents capable of altering the immune response in mammals.
Abstract: There is disclosed a class of fluoroalkoxyphenyl-substituted nitrogen-containing heterocycles which are useful as herbicides, plant fungicides, and plant growth regulators. Internodal elongation of plants is inhibited by treatment with compounds of this invention.
Abstract: Novel oxiodinium and thiaiodinium compounds having a superior inhibitory effect against micro-organisms coupled with outstanding stability and low toxicity are described.
Abstract: Novel compounds identified as acetal derivatives of 4-(substituted amino)-3,5-dinitrobenzaldehydes, effective as herbicides, and intermediates for their preparation.
Abstract: Antibiotic A16886I and antibiotic A16886II and their salts, having antibacterial and anthelmintic activity, prepared by fermentation of Streptomyces clavuligerus NRRL 3585.
Type:
Grant
Filed:
May 20, 1976
Date of Patent:
March 4, 1980
Assignee:
Eli Lilly and Company
Inventors:
Marvin Gorman, Calvin E. Higgens, Ramakrishnan Nagarajan
Abstract: 5,6-Diaryl-1,2,4-triazines, topically-active anti-inflammatory agents, having the formula, ##STR1## wherein R is hydrogen or -(X).sub.n R.sub.1, in which X is either O or S, n is an integer which is either 0 or 1, and R.sub.1 is C.sub.1 -C.sub.8 alkyl, C.sub.7 -C.sub.8 aralkyl, C.sub.3 -C.sub.8 cycloalkyl, or C.sub.4 -C.sub.8 (cycloalkyl)alkyl; and R.sub.2 and R.sub.3 independently are C.sub.1 -C.sub.3 alkoxy or di(C.sub.1 -C.sub.3 alkyl)amino; with the proviso that when R.sub.2 and R.sub.3 both are methoxy, R cannot be H or methylthio; and the pharmaceutically-acceptable acid addition salts of basic members thereof.
Abstract: Acylamino heteroaryl compounds in which the heteroaryl nucleus is a 5-membered ring containing a single heteroatom, which may be oxygen, or sulphur, methods of making the compounds and pharmaceutical formulations containing the compounds. The compounds have anti-allergy activity.
Type:
Grant
Filed:
January 19, 1978
Date of Patent:
February 5, 1980
Assignee:
Lilly Industries Limited
Inventors:
Delme Evans, Michael R. J. Jolley, William J. Ross, Brian P. Swann
Abstract: Acylamino tetrazolyl compounds having anti-allergic activity, methods of making the compounds and pharmaceutical formulations containing the compounds.
Type:
Grant
Filed:
February 1, 1979
Date of Patent:
January 29, 1980
Assignees:
Eli Lilly and Company, Lilly Industries Limited
Inventors:
Roger G. Harrison, William B. Jamieson, William J. Ross, John C. Saunders
Abstract: It has been discovered that fungal foliar phytopathogens may be controlled by the use of a broad class of 2,6-dinitroanilines. The fungicidally-effective compounds may bear a broad range of substituent groups on the anilino nitrogen and in the 3- and 4-positions of the benzene ring.
Abstract: Certain halogenated phenylthioacetamido cephalosporanic acids and derivatives thereof, e.g., 7-[2'-(2",5"-dichlorophenylthio)acetamido]cephalosporanic acid, are effective antibiotics against Staphylococcus aureus cultures which show heterogeneous resistance to methicillin.
Abstract: A class of novel 2-oxazolyl ureas and carbamates having anti-allergic activity are described together with methods of making such compounds and pharmaceutical compositions containing the active compounds of the invention.
Type:
Grant
Filed:
December 27, 1977
Date of Patent:
November 20, 1979
Assignee:
Lilly Industries Limited
Inventors:
William J. Ross, Alex Todd, John P. Verge
Abstract: Novel 1,3,4-trisubstituted-4-arylpiperidines are prepared by alkylating a 2,3-disubstituted-3-arylpyrroline to afford a 1,2,3-trisubstituted-3-aryl-1-pyrrolinium salt, reacting the salt with diazomethane to provide a 1,2,3-trisubstituted-3-aryl-1,2-methylene-pyrrolidinium salt, heating the pyrrolidinium salt to effect a ring expansion to the corresponding 1,3,4-trisubstituted-4-aryl-1,4,5,6-tetrahydropyridinium salt, neutralizing the salt and reducing the tetrahydropyridine to provide a 1,3,4-trisubstituted-4-arylpiperidine. The piperidines so formed are useful as pharmacological agents and as intermediates in the preparation of other piperidines of the invention. The compounds provided herein are especially useful as narcotic agonists analgesics and as narcotic antagonists.
Abstract: Antibiotic A16886I and antibiotic A16886II and their salts, having antibacterial and anthelmintic activity, prepared by fermentation of Streptomyces clavuligerus NRRL 3585.
Type:
Grant
Filed:
August 10, 1970
Date of Patent:
November 6, 1979
Assignee:
Eli Lilly and Company
Inventors:
Marvin Gorman, Calvin E. Higgens, Ramakrishnan Nagarajan
Abstract: Thieno[1,5]benzodiazepines having useful CNS activity containing the novel tricyclic ring system: ##STR1## the 10-position being substituted by an amino, preferably a piperazino, group.