Claims for Patent: 5,496,931

Summary for Patent: 5,496,931

Title:	Insecticide and miticide A83543 compounds and their method of production by fermentation
Abstract:	Fermentation product A83543, comprising major components A83543A and A83543D and minor components A83543B, A83543C, A83543E, A983543F, A83543G, A83543H and A83543J, is produced by a newly described species, Saccharopolyspora spinosa. The A83543 components and their acid-addition salts (A83543 compounds) are useful as insecticides, particularly against Lepidoptera and Diptera species. Insecticidal, miticidal or ecto-parasiticidal combinations, compositions and methods are provided.
Inventor(s):	LaVerne D. Boeck, Hang Chio, Tom E. Eaton, Otis W. Godfrey, Jr., Karl H. Michel, Walter M. Nakatsukasa, Raymond C. Yao
Assignee:	Corteva Agriscience LLC
Application Number:	US08/406,760
Patent Claims:	1. A compound of the formula ##STR4## wherein R is H or a group selected from ##STR5## R2 is ##STR6## R1, R3, R5 and R6 are hydrogen or methyl; R4 is methyl or ethyl; andprovided that R, R1, R3, R4 R5 and R6 must be present in one of the following combinations: ______________________________________ R R.sup.1 R.sup.3 R.sup.4 R.sup.5 R.sup.6 ______________________________________ (a) Me H Et Me Me (b) Me H Et Me Me (c) Me H Et Me Me (a) Me Me Et Me Me (a) Me H Me Me Me (a) H H Et Me Me (d) Me H Et Me Me (a) Me H Et H Me (a) Me H Et Me H H Me H Et Me Me H Me Me Et Me Me H Me H Me Me Me H H H Et Me Me H Me H Et H Me H Me H Et Me H ______________________________________ an acid addition salt of a compound wherein R is other than hydrogen. 2. A compound of claim 1 wherein R is other than H, or an acid addition salt thereof. 3. A compound of claim 2 wherein R is an (a) group. 4. A compound of claim 2 wherein R is a (b) group. 5. A compound of claim 2 wherein R is a (c) group. 6. The compound of claim 2 wherein R is (d), R1 is methyl; R3 is hydrogen; R4 is ethyl; R5 is methyl; and R6 is methyl. 7. The compound of claim 3 wherein: R1, R5, and R6 ═CH3 ; R3 ═H; and R4 =ethyl; or an acid addition salt thereof. 8. The compound of claim 4 wherein: R1, R5 and R6 =CH3 ; R3 ═H; and R4 =ethyl; or an acid addition salt thereof. 9. The compound of claim 5 wherein: R1, R5 and R6 ═CH3 ; R3 ═H; and R4 =ethyl; or an acid addition salt thereof. 10. The compound of claim 3 wherein: R1, R3, R5 and R6 ═CH3 ; and R4 =ethyl; or an acid addition salt thereof. 11. The compound of claim 3 wherein: R1, R4, R5 and R6 ═CH3 ; and R3 ═H; or an acid addition salt thereof. 12. The compound of claim 3 wherein: R1 and R3 ═H; R4 =ethyl; and R5 and R6 ═CH3 ; or an acid addition salt thereof. 13. The compound of claim 3 wherein: R1 and R6 ═CH3 ; R4 =ethyl; and R3 and R5 ═H; or an acid addition salt thereof. 14. The compound of claim 3 wherein: R1 and R5 =CH3 ; R4 =ethyl; and R3 and R6 ═H; or an acid addition salt thereof. 15. A compound of claim 1 wherein R═H. 16. A compound of claim 15 wherein R4 =ethyl. 17. The compound of claim 15 wherein R4 ═CH3. 18. The compound of claim 16 wherein R1, R5 and R6 ═CH3 and R3 ═H. 19. The compound of claim 16 wherein R3 ═CH3. 20. The compound of claim 16 wherein R1 ═H. 21. The compound of claim 16 wherein R5 ═H. 22. The compound of claim 16 wherein R6 ═H. 23. Fermentation product A83543, comprising A83543A, A83543B, A83543C, A83543D, A83543E, A83543F, A83543G, A83543H and A83543J, which is produced by culturing a Saccharopolyspora spinosa strain selected from NRRL 18395, NRRL 18537, NRRL 18538 or NRRL 18539, or an A83543-producing mutant thereof, under submerged aerobic conditions in a suitable culture medium until a recoverable amount of A83543 is produced. 24. An insecticidal or miticidal combination which comprises at least 1% by weight of a compound of claim 2 in combination with a second insecticide or miticide. 25. An insecticide or miticide composition comprising an insect- or mite-inactivating amount of a compound of claim 2 in combination with a phytologically-acceptable carrier. 26. An insecticide or miticide composition of claim 25 wherein the compound is selected from, Formula 1 where R is (a), R1 is methyl, R3 is hydrogen, R4 is ethyl, R5 is methyl and R6 is methyl; R is (b), R1 is methyl, R3 is hydrogen, R4 is ethyl, R5 is methyl and R6 is methyl; R is (c), R1 is methyl, R3 is hydrogen, R4 is ethyl, R5 is methyl and R6 is methyl; R is (a), R1 is methyl, R3 is methyl, R4 is ethyl, R5 is methyl and R6 is methyl; R is (a), R1 is methyl, R3 is hydrogen, R4 is methyl, R5 is methyl and R6 is methyl; R is (a) , R1 is hydrogen, R3 is hydrogen, R4 is ethyl, R5 is methyl and R6 is methyl; R is (d) , R1 is methyl, R3 is hydrogen, R4 is ethyl, R5 is methyl and R6 is methyl R is (a) , R1 is methyl, R3 is H, R4 is ethyl, R5 is hydrogen and R6 is methyl; or R is (a) , R1 is methyl, R3 is hydrogen, R4 is ethyl, R5 is methyl and R6 is hydrogen or a phytologically acceptable salt thereof. 27. An insecticide or miticide composition of claim 26 wherein the compound is present together with the dried fermentation broth in which it is produced. 28. An insecticide or miticide method which comprises applying to the locus of an insect or mite an insect- or mite-inactivating amount of a compound of claim 2. 29. An insecticide or miticide method of claim 28 wherein the compound is selected from, Formula 1 where R is (a), R1 is methyl, R3 is hydrogen, R4 is ethyl, R5 is methyl and R6 is methyl; R is (b), R1 is methyl, R3 is hydrogen, R4 is ethyl, R5 is methyl and R6 is methyl; R is (c) , R1 is methyl, R3 is hydrogen, R4 is ethyl, R5 is methyl and R6 is methyl; R is (a) , R1 is methyl, R3 is methyl, R4 is ethyl, R5 is methyl and R6 is methyl; R is (a) , R1 is methyl, R3 is hydrogen, R4 is methyl, R5 is methyl and R6 is methyl; R is (a) , R1 is hydrogen, R3 is hydrogen, R4 is ethyl, R5 is methyl and R6 is methyl; R is (d) , R.1 is methyl, R3 is hydrogen, R4 is ethyl, R5 is methyl and R6 is methyl; R is (a) , R1 is methyl, R3 is H, R4 is ethyl, R5 is hydrogen and R6 is methyl; or R is (a) , R1 is methyl, R3 is hydrogen, R4 is ethyl, R5 is methyl and R6 is hydrogen or a phytologically acceptable salt thereof. 30. A method of controlling a population of insect ectoparasites which consume blood of a host animal which comprises administering to the host animal an effective amount of a compound of claim 2. 31. A method of claim wherein the compound is selected from, Formula 1 where R is (a), R1 is methyl, R3 is hydrogen, R4 is ethyl, R5 is methyl and R6 is methyl; R is (b) , R1 is methyl, R3 is hydrogen, R4 is ethyl, R5 is methyl and R6 is methyl; R is (c) , R1 is methyl, R3 is hydrogen, R4 is ethyl, R5 is methyl and R6 is methyl; R is (a), R1 is methyl, R3 is methyl, R4 is ethyl, R5 is methyl and R6 is methyl; R is (a) , R1 is methyl, R3 is hydrogen, R4 is methyl, R5 is methyl and R6 is methyl; R is (a) , R1 is hydrogen, R3 is hydrogen, R4 is ethyl, R5 is methyl and R6 is methyl; R is (d), R.sup. 1 is methyl, R3 is hydrogen, R4 is ethyl, R5 is methyl and R6 is methyl; R is (a) , R1 is methyl, R3 is H, R4 is ethyl, R5 is hydrogen and R6 is methyl; or R is (a), R1 is methyl, R3 is hydrogen, R4 is ethyl, R5 is methyl and R6 is hydrogen or a phytologically acceptable salt thereof.