Abstract: Phenylpiperazine derivatives of formula (I): ##STR1## where R.sup.1 is benzyl, C.sub.1-6 alkyl or optionally substituted phenyl; R.sup.2 is optionally substituted phenyl; R.sup.3 is hydrogen or C.sub.1-4 alkyl; Q is furan, thiophene, oxazole or thiazole; m is 1 to 3 and n is 0 or 1; and pharmaceutically-acceptable salts thereof are active in the chemotherapy of immediate hypersensitivity conditions such as asthma.
Abstract: 2,6-Di(fluoroalkyl)-4-nitrobenzimidazoles and certain N-acyl derivatives thereof, including sulfonates, thiocarboxamides, and carboxylates, are used to control a broad spectrum of mites and insects with particularly good effect against members of the orders Hemiptera, Coleoptera, Orthoptera, and Lepidoptera.
Abstract: 3'-hydroxy and 3'-keto derivatives of 4'-deoxy VLB (deoxy VLB "A"), 4'-deoxyleurosidine (deoxy VLB "B"), 4'-deoxyvincristine and 4'-deoxy-1-desmethyl-1-formylleurosidine and related 4-desacetyl and C-3 carboxamide derivatives, useful as anti-tumor agents in mammals.
Abstract: 5'-Acetonylvincristine and related compounds including the corresponding 1-desmethyl derivative, useful in inhibiting the growth of experimental tumors.
Type:
Grant
Filed:
May 27, 1977
Date of Patent:
August 29, 1978
Assignee:
Eli Lilly and Company
Inventors:
Charles J. Barnett, Richard A. Bimm, George C. Cullinan
Abstract: 1-Hydroxy-9-keto-3-alkyl-dibenzo[b,d]pyrans or 1,9-dihydroxy-3-alkyl-dibenzo[b,d]pyrans are oxygenated on the penultimate carbon of the alkyl side chain by fermentation with a strain of the micro-organism Bacillus cereus.
Type:
Grant
Filed:
August 8, 1977
Date of Patent:
August 1, 1978
Assignee:
Eli Lilly and Company
Inventors:
David S. Fukuda, Bernard J. Abbott, Robert A. Archer
Abstract: Benzoxazoles substituted in the 2-position with sulfhydryl or halogen and substituted in the 5- or 6-position with an acetic or propionic acid group or a salt or ester thereof or a nitrile convertible thereto useful as intermediates in the preparation of 5- or 6-Substituted benzoxazole propionic or acetic acid derivatives, substituted in the 2-position of the oxazole nucleus by a group of the formula AR.sup.4 wherein A is --CH.sub.2 --, --CO--, --CHOR--, or --NR--, wherein R is hydrogen, C.sub.1-6 alkyl or C.sub.2-7 acyl, and R.sup.4 is optionally substituted phenyl, useful as non-steroidal, non-narcotic, analgesic, antipyretic and anti-inflammatory agents.
Type:
Grant
Filed:
February 7, 1977
Date of Patent:
July 11, 1978
Assignee:
Lilly Industries Ltd.
Inventors:
David William Dunwell, Delme Evans, Terence Alan Hicks
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: Vincaleukoblastine (VLB, vinblastine) is reacted with thionyl chloride to form a bis-sulfite ester which is converted to various 5'-oxygenated derivatives.
Type:
Grant
Filed:
October 20, 1976
Date of Patent:
May 2, 1978
Assignee:
Eli Lilly and Company
Inventors:
Allen S. Katner, Gerald E. Gutowski, Jean C. Miller
Abstract: Crude preparations of 2-phenyl-5-benzoxazolylalkanoic acids are purified by forming the ammonium salt thereof in an organic solvent and thermally reconverting the separated ammonium salt to the acid. Gaseous ammonia is a by-product.