Eli Lilly and Company

Dowelanco

Dow Agrosciences LLC

Herbert A Kirst

Lawrence C Creemer

John E Toth

Jan R Turner

Mary L Huber

Mary C Broughton

Manuel Debono

Jon S Mynderse

James W Martin

Brenda A Truedell

Walter M Nakatsukasa

James A Mabe

Earl E Ose

Richard H Baltz

Eugene T Seno

Gene M Wild

James P Leeds

Julie A Wind

Gary D Crouse

Thomas Clarence Sparks

Carl Vincent DeAmicis

David W Robertson

Karl H Michel

James Michael Gifford

Vidyadhar Babu Hegde

Rosanne Bonjouklian

Jaswant S Gidda

Peter Biagio Anzeveno

Michael John Ricks

Joe Raymond Schoonover

Thomas V Worden

Frederick Richard Green, Iii

Brian R Thoreen

Christopher J Hatton

Kevin L McLaren

Jacek G Martynow

The compounds of the present invention are prepared directly or indirectly by modifying the compounds that are naturally produced from Saccharopolyspora spinosa. The compounds of the invention have been shown to have activity against insects and mites. The compounds are prepared by modifying the rhamnose sugar, modification of the forosamine sugar, or starting with pseuodoaglycone and then replacement with a nonsugar derivative or different sugar, modification of the 5,6,5-tricyclic and 12-membered macrocyclic lactone part of the compounds naturally produced or of the pseudoaglycone of the natural compounds.

Synthetic modification of Spinosyn compounds

New A83543 components, including fermentation products A83543K, A835430, A83543P, A83543U, A83543V, A83543W and A83543Y and N-demethyl derivatives, and salts thereof, are useful for the control of insects and mites. The pseudoaglycones of the new A83543 components are useful for the preparation of A83543 components. Methods are provided for making the new A83543 components by culturing of Saccharopolyspora spinosa NRRL 18395, NRRL 18537, NRRL 18538, or NRRL 18539, or NRRL 18743 or NRRL 18719 or NRRL 18823 in suitable culture medium. Insecticidal and ectoparasiticidal compositions containing new A83543 components are also provided.

A83543 compounds and process for production thereof

New A83543 components, including fermentation products A83543K, A83543O, A83543P, A83543U, A83543V, A83543W and A83543Y and N-demethyl derivatives, and salts thereof, are useful for the control of insects and mites. The pseudoaglycones of the new A83543 components are useful for the preparation of A83543 components. Methods are provided for making the new A83543 components by culturing of Saccharopolyspora spinosa NRRL 18395, NRRL 18537, NRRL 18538, or NRRL 18539, or NRRL 18743 or NRRL 18719 or NRRL 18823 in suitable culture medium. Insecticidal and ectoparasiticidal compositions containing new A83543 components are also provided.

A83543 Aglycones A83543AgA, A83543AgD, A83543AgE, and A83543AgF, and A83543 pseudoaglycones A83543PsaA2, A83543PsaB2, A83543PsaD2, and A83543PsaN2 are intermediates useful in preparation of known insecticides.

A83543 aglycones and pseudoglycones

This invention relates to derivatives of Wortmannin and particularly to 11,17 substituted derivatives of Wortmannin. The invention also relates to a method of using these compounds as PI-3-kinase inhibitors and as anti-tumor agents.

Stereochemical Wortmannin derivatives

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.

Antibiotic A10255 complex and factors, and process and production

New fermentation products A83543L, A83543M, and A83543N, N-demethyl derivatives thereof, and salts thereof, are useful for the control of insects. A83543PsaL1 is useful for the preparation of A83543 components. Methods for making A83543J, A83543L, A83543M, and A83543N by culture of Saccharopolyspora spinosa NRRL 18719 or NRRL 18720 are provided. Insecticidal and ectoparasiticidal compositions containing A83543L, A83543M, A83543N, and N-demethyl derivatives thereof are also provided.

A83543 compounds and processes for production thereof

Three new groups of 9-N-substituted derivatives of erythromycylamine with superior oral activity against Gram-positive pathogens, new processes for preparing derivatives of erythromycylamine and aliphatic aldehydes by controlling the pH of the reaction and by catalytic hydrogenation, and pharmaceutical compositions and methods using the new compounds are provided.

Derivatives of erythromycylamine

Novel 12-membered lactone and 11-membered lactone derivatives of erythromycin, having antimicrobial activity against certain Gram-positive pathogens such as Steptococcus pyogenes and Gram-negative cocci such as Haemophilus influenzae, and useful as intermediates to other macrolide derivatives, are disclosed.

Erythromycin ring-contracted derivatives

Novel ring-contracted macrolides which enhance gastrointestinal motility and novel methods and compositions for treating gtastrointestinal disorders in animals with these macrolides and with certain other previously known ring-contracted macrolides are provided.

Method for treating gastrointestinal disorders

New 4''-O-modified-20-modified tylosin and 4'-O-modified-20-modified-desmycosin and 4'-deoxydesmycosin derivatives of formula 1 have significant oral antibacterial activity. Compositions containing and methods of using these compounds are also provided.

Modifications of mycinose and 3-O-demethylmycinose in tylosin-type

C-20-Dihydro-deoxy-(cyclic amino)-derivatives of the macrolide antibiotics tylosin, desmycosin, macrocin, lactenocin, 2''-O-demethylmacrocin and 2'-O-demethyllactenocin, which inhibit pathogenic bacteria, especially gram-positive bacteria, Pasteurella species, and Mycoplasma species, and pharmaceutical compositions thereof, are provided.

C-20-dihydro-deoxy-(cyclic amino)-derivatives of macrolide antibiotics

New 3'' and/or 4''-modified macrocin and 3' and/or 4'-modified-lactenocin derivatives of formula 1 have significant antibacterial activity. Compositions positions containing and methods of using these derivatives are also provided.

Modifications of 3-O-demethylmycinose in macrocin and lactenocin

C-20-Modified derivatives of macrolide antibiotics which include demycinosyltylosin (DMT), 20-dihydro-23-demycinosyltylosin (dihydro-DMT), 23-de(mycinosyloxy)tylosin (DMOT), 20-dihydro-23-de(mycinosyloxy)tylosin (dihydro-DMOT), 5-O-mycaminosyltylonolide (OMT), 20-dihydro-5-O-mycaminosyltylonolide (dihydro-OMT), 23-deoxy-5-O-mycaminosyltylonolide (DOMT), and 20-dihydro-23-deoxy-5-O-mycaminosyltylonolide (dihydro-DOMT) inhibit pathogenic bacteria, especially gram-positive bacteria, and Mycoplasma species; and pharmaceutical compositions thereof.

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Indianapolis, IN, United States of America

Herbert A Kirst