Abstract: 8,8-Disubstituted-6-methylergolines and 9-ergolenes, are prepared by alkylation of lysergic, or isolysergic acid or their 9,10-dihydro analogues.
Abstract: Vincaleukoblastine (VLB, vinblastine) is converted to leurosidine, its 4' epimer, by reaction with thionyl chloride to form a bis-sulfite ester followed by treatment of the bis-sulfite ester with silver perchlorate. The bis-sulfite ester is covertible to novel 4' ethers by treatment with a lower alkanol or 4' esters of leurosidine perchlorate with acetic anhydride.
Type:
Grant
Filed:
May 17, 1976
Date of Patent:
February 21, 1978
Assignee:
Eli Lilly and Company
Inventors:
Allen S. Katner, Gerald E. Gutowski, Jean C. Miller
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:
June 9, 1976
Date of Patent:
December 20, 1977
Assignee:
Eli Lilly and Company
Inventors:
David S. Fukuda, Bernard J. Abbott, Robert A. Archer
Abstract: Descarboxylysergic acid prepared from 2,3-dihydro-8.beta.-hydroxy-6-methyl-9-ergolene or from penniclavine has oxytocic, serotonin antagonist, prolactin inhibition and muscle contracting activities.
Type:
Grant
Filed:
November 3, 1975
Date of Patent:
June 21, 1977
Assignee:
Eli Lilly and Company
Inventors:
Nicholas J. Bach, David A. Hall, Edmund C. Kornfeld
Abstract: Dimeric Vinca alkaloids are converted to three separable anhydro derivatives, useful as mitotic inhibitors or as intermediates for the preparation of other oncogenetically active alkaloids.
Abstract: The invention provides 3-(2-formyl-3-hydroxy-5-oxocyclopent-1-enyl)-propanoic acid and derivatives thereof having anti-thrombotic activity coupled with low toxicity. Also provided is a method for preparing such compounds by subjecting a 3-[3-hydroxy-5-oxo-2-(.beta.-styryl)cyclopent-1-enyl]-propanoic acid or derivative thereof to oxidative cleavage.
Type:
Grant
Filed:
April 10, 1974
Date of Patent:
May 31, 1977
Assignee:
Lilly Industries, Ltd.
Inventors:
William Dawson, Michael John Foulis, Norman James Albert Gutteridge, Colin William Smith
Abstract: The invention provides novel 5- and 6-benzoxazolyl alkanoic acids, optionally substituted in the 2-position, and derivatives thereof which possess anti-inflammatory, anti-pyretic and analgesic activity. Also provided is a process for preparing such compounds by cyclizing an appropriately substituted o-aminophenol and, if necessary, converting the resultant benzoxazole to the desired compound.
Type:
Grant
Filed:
February 1, 1977
Date of Patent:
April 11, 1978
Assignee:
Lilly Industries Limited
Inventors:
Delme Evans, David William Dunwell, Terence Alan Hicks