Abstract: Improved processes for producing a polyether antibiotic compound represented by A82810 comprising: (1) cultivating Actinomadura fibrosa sp. nov. NRRL 18348 or Actinomadura sp. NRRL 18880, (2) feeding acid hydrolyzed casein at a rate from about 2.50-7.50 gm/L/day, (3) feeding glucose at a rate from about 2.50-7.50 gm/L/day, and (4) feeding propionate at a rate from about 0.50-1.5 gm/L/day to the appropriate culture medium during fermentation, are provided.
Abstract: Fermentation product A87689 is produced by a strain of Amycolatopsis mediterranei selected from NRRL 18815 and NRRL 18851, or an A87689-producing mutant thereof. A87689, its C.sub.1-6 -alkyl ether and C.sub.1-6 -alkanoyl ester derivatives and pharmaceutically acceptable salts thereof are phospholipase A.sub.2 inhibitors that are useful as antiinflammatory agents. Fermentation products known as BU-3889V, its components and pharmaceutically acceptable salts thereof, are phospholipase A.sub.2 inhibitors that are also useful as antiinflammatory agents.
Type:
Grant
Filed:
May 4, 1992
Date of Patent:
January 11, 1994
Assignee:
Eli Lilly and Company
Inventors:
Dennis R. Berry, Anne H. Dantzig, Manuel Debono, Robert Hamill, R. Michael Molloy, Raymond C. Yao
Abstract: The present invention provides a process for preparing a 4-hydroxypyrrolo[2,3-d]pyrimidine derivative of the formula ##STR1## wherein R is NHC*H(COOR.sup.1)CH.sub.2 CH.sub.2 COOR.sup.1 or OR.sup.1 ;R.sup.1 is H or a carboxyl protecting group;the configuration about the carbon atom designated * is L;n is 0 or 1; andA is an aryl group optionally having, in addition to the COR substituent, one or two substituents selected from the group consisting of halo, hydroxy, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 alkoxy; or a salt thereof, which comprises(a) halogenating a compound of the formula ##STR2## wherein R, R.sup.1, A and * are as defined above;j is 0 or 1; and(b) reacting 2,4-diamino-6-hydroxypyrimidine, or a salt thereof, with the reaction product from step (a), in the presence of a polar solvent.
Abstract: This invention relates to intermediates and processes thereto, for the preparation of 5,6-dihydropyrro[2,3-d]pyrimidines which are useful for the treatment of susceptible neoplasms
Abstract: 4-Hydroxypyrrolo[2,3-d]pyrimidines are regiospecifically halogenated at the C-5 position by silylation in the presence of an inert organic solvent and iodination, bromination or chlorination.
Type:
Grant
Filed:
June 22, 1992
Date of Patent:
August 10, 1993
Assignee:
Eli Lilly and Company
Inventors:
Charles J. Barnett, Michael E. Kobierski
Abstract: Newly-discovered antibiotic A10255 factors B, C, E, F, G, H, and J are produced by submerged aerobic fermentation of Streptomyces gardneri NRRL 15537 and NRRL 18260 or an A10255-producing variant or mutant thereof. The antibiotics are active against a wide variety of pathogenic bacteria, and also enhance feed-utilization efficiency in chickens, weanling pigs, cattle and sheep. The antibiotics can also be used to detect the thiostrepton-resistance gene in Streptomyces species.
Abstract: Administration of a folate binding protein binding agent in conjunction with use of an antitumor agent which is an inhibitor of glycinamide ribonucleotide transformylase or other antifolate reduces the toxic effects of such agent and provides an enhanced therapeutic index.
Abstract: Derivatives of melatonin and the pharmaceutically acceptable salts thereof are useful for therapeutically treating hormonally dependent mammalian breast carcinoma. Combination treatments of melatonin derivatives and an antiestrogen compound are especially useful.
Abstract: This invention relates to N-[2-amino-4-substituted-[[(pyrrolo or pyrido) [2,3-d]pyrimidinyl]-alkyl]benzoyl]-L-glutamic acid compounds, intermediates for their synthesis, pharmaceutical formulations containing those compounds, and their use as antineoplastic agents.
Abstract: New glycopeptide antibiotic A83850, comprising A83850A, and A83850B, is produced by Amycolatopsis albus strain NRRL 18532. A83850A and A83850B can be reduced to give new biologically active derivatives. The A83850 antibiotics have activity against Gram-positive bacteria comparable to that of vancomycin.
Abstract: 4-Deaza-10-oxo- and 5-deaza-10-thio-5,6,7,8-tetrahydrofolic acid derivatives are provided as agents useful for treatment susceptible neoplasms in mammals. Pharmaceutical formulations and intermediates are also provided.
Abstract: New Polyether antibiotic A82810, its acyl and alkyl ester, acyl ester and urethane derivatives, and salts thereof, are useful antibacterial and anticoccidial agents and increase feed-utilization efficiency in animals. Methods of making A82810 by culture of Actinomodura fibrosa sp. nov. NRRL 18348 and synergistic compositions of the A82810 compounds with nicarbazin, 4,4'-dinitrocarbanilide, certain napthalenamine and benzenamine compounds and metichlorpindol are also provided.