Abstract: Progestational agents administered daily to female mammals during the follicular phase only of the cycle prevents uterine development associated with implantation in the luteal phase, thereby preventing conception.
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: Acylamino heteroaryl compounds in which the heteroaryl nucleus is a 1,2,4-oxadiazole or 1,2,4-thiadiazole nucelus, methods of making the compounds and pharmaceutical formulations containing the compounds. The compounds have anti-allergy activity.
Type:
Grant
Filed:
October 11, 1977
Date of Patent:
September 4, 1979
Assignee:
Lilly Industries Limited
Inventors:
William J. Ross, John P. Verge, William R. N. Williamson
Abstract: Acylamino pyrazolyl compounds of the formula: ##STR1## wherein Ar represents an optionally substituted pyrazolyl group, the acylamino group --NR.sup.1 COR.sup.2 being attached to a carbon atom of the pyrazolyl ring, which have anti-allergic activity, methods of making the compounds and pharmaceutical formulations containing the compounds.
Type:
Grant
Filed:
June 1, 1976
Date of Patent:
August 28, 1979
Assignee:
Lilly Industries Limited
Inventors:
Roger G. Harrison, William B. Jamieson, William J. Ross, John C. Saunders
Abstract: A penicillin sulfoxide ester is reacted with an N-chloro halogenating agent at a temperature of from about 75.degree. C. to about 135.degree. C. and in the presence of an alkylene oxide and calcium oxide to produce a 2-chlorosulfinylazetidin-4-one intermediate. The intermediate, upon separation from the alkylene oxide, calcium oxide, and any conversion products of both the alkylene oxide and calcium oxide, can be treated with stannic chloride to produce a 3-exomethylenecepham sulfoxide.
Abstract: A penicillin sulfoxide ester is reacted with an N-chloro halogenating agent at a temperature of from about 75.degree. C. to about 135.degree. C. to produce a novel 2-chlorosulfinylazetidin-4-one intermediate. The intermediate can be treated with stannic chloride to produce a 3-exomethylenecepham sulfoxide.
Abstract: Acylamino heteroaryl compounds in which the heteroaryl nucleus is a 1,2,4-oxadiazole or 1,2,4-thiadiazole nucleus, methods of making the compounds and pharmaceutical formulations containing the compounds. The compounds having anti-allergy activity.
Type:
Grant
Filed:
June 13, 1977
Date of Patent:
July 31, 1979
Assignee:
Lilly Industries Limited
Inventors:
William J. Ross, John P. Verge, William R. N. Williamson
Abstract: Penicillin sulfoxide derived azetidinone sulfinyl chlorides and related sulfinic acid derivatives are cyclized to 3-methylenecephams by reaction with Friedel-Crafts catalysts or metathetic cation forming agents.
Abstract: Acylamino heteroaryl compounds in which the heteroaryl nucleus is a 1,3,4-oxadiazole or 1,3,4-thiadiazole nucleus, methods of making the compounds and pharmaceutical formulations containing the compounds. The compounds have anti-allergy activity.
Type:
Grant
Filed:
October 7, 1977
Date of Patent:
June 19, 1979
Assignee:
Lilly Industries Limited
Inventors:
William J. Ross, John P. Verge, William R. N. Williamson
Abstract: A class of 2,6-dinitroanilines having a broad range of substituent groups on the anilino nitrogen and in the 3- and 4-positions of the phenyl ring are used for the protection of plants against soil-borne phytopathogens of the genus Phytophthora.
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: Acylamino heteroaryl compounds in which the heteroaryl nucleus is a 1,3,4-oxadiazole or 1,3,4-thiadiazole nucleus, methods of making the compounds and pharmaceutical formulations containing the compounds. The compounds have anti-allergy activity.
Type:
Grant
Filed:
June 22, 1977
Date of Patent:
May 1, 1979
Assignee:
Lilly Industries Limited
Inventors:
William J. Ross, John P. Verge, William R. N. Williamson
Abstract: Propanoic acid derivatives of the formula: ##STR1## where R.sup.1 is a C.sub.1-8 alkyl group optionally substituted by hydroxyl or --COOH and R.sup.2 is hydrogen or a protecting group, are useful as anti-thrombotic agents.
Type:
Grant
Filed:
December 4, 1975
Date of Patent:
April 24, 1979
Assignee:
Lilly Industries Limited
Inventors:
William Dawson, Michael J. Foulis, Norman J. A. Gutteridge, Colin W. Smith
Abstract: Oxazoles which are substituted in the 2,4 or 5-position with an N-substituted-acylamino group have anti-allergic activity. Methods of making such compounds, pharmaceutical compositions containing the active compounds of the invention and methods of treating asthma utilizing such compounds are provided.
Abstract: The silylated and enamine protected D-3- or 4-hydroxyphenylglycine as the sodium salt of the formula ##STR1## wherein A is methyl or ethyl, are crystalline intermediates useful in a new process for the acylation of heterocyclic-thiomethyl-substituted cephalosporin nuclei, e.g. 7-amino-3-(5-methyl-1,3,4-thiadiazole-2-ylthiomethyl)-3-cephem-4-carboxyli c acid and 7-amino-3-(1-methyl-1H-tetrazole-5-ylthiomethyl)-3-cephem-4-carboxylic acid.
Abstract: Novel 1,4-disubstituted-3-nitropyrazoles having antimicrobial, parasiticidal, and herbicidal activity are prepared by a reaction sequence of which the individual steps are conventional. The new 3-nitropyrazoles are characterized by a 1-substituent and a usually carbonyl-containing 4-substituent. The novel 3(5)-nitro-4-pyrazolecarbonitrile is obtained as an intermediate in the preparation of the biologically-active compounds. Preferred compounds are 1-alkyl or -alkenyl-4-pyrazolecarboxamides and carbonitriles. The new compounds are particularly useful for the control of bacterial animal diseases.
Abstract: The present invention is directed to 7-amino-3-carbamoyloxymethyl-3-cephem-4-carboxylic acid: ##STR1## and to precursors and derivatives. The compound, its precursors, and its derivatives exhibit antibacterial activity, which, in the instance of certain of the derivatives, is of an enhanced degree.
Abstract: Novel 3-phenoxyphenylalkyl amines and the amides, alcohols, tetrazoles, and carbamates related thereto as well as novel intermediates useful in the preparation of such compounds. The compounds of this invention are useful as anti-inflammatory, analgesic, and antipyretic agents.
Abstract: A small tablet containing over 90% by weight of an orally active cephalosporin such as cephalexin and which utilizes as a binder polyvinyl pyrrolidone having a number average molecular weight of from 500,000 to 1,500,000.
Abstract: Oxazoles having a sulfinyl or sulfonyl substituent at the 2-position are provided. Such compounds readily react with an alkali metal salt of a secondary amide in a method of making 2-acylamino oxazole derivatives having anti-allergic activity.