# US 7,078,195 B2 · Antibiotics AA-896 > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 7,078,195 B2 - Document ID: US7078195B2 - Status: Granted - Kind: B2 - Application number: 10/713,881 - Filed: 2003-11-14 - Published: 2004-06-17 - Granted: 2006-07-18 - Earliest claimed: 2001-04-25 - Assignees: Wyeth Holdings Corporation - Inventors: Guy Thomas Carter; Jason Arnold Lotvin; Leonard Alexander McDonald - Web page: https://patentgrep.com/patent/US7078195B2 ## CPC - C12N 1/205: Bacterial isolates - C07H 19/06: Pyrimidine radicals - C07K 9/001: {the peptide sequence having less than 12 amino acids and not being part of a ring structure} - C12P 17/16: containing two or more hetero rings {(thiamine open chain analogs C12P17/167, i.e. not condensed among themselves or through a common carbocyclic ring system)} - A61K 38/00: Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00) - C12R 2001/465: Streptomyces - Y10S 435/886: Streptomyces - C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00) - C07H: SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS (derivatives of aldonic or saccharic acids C07C, C07D; aldonic acids, saccharic acids C07C59/105, C07C59/285; cyanohydrins C07C255/16; glycals C07D; compounds of unknown constitution C07G; polysaccharides, derivatives thereof C08B; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification C12N15/00; sugar industry C13) - C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00) - C12P: FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE {(brewing of beer C12C; producing vinegar C12J; producing specific peptides or proteins C07K; producing enzymes C12N9/00; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification C12N15/00; measuring or testing processes involving enzymes or microorganisms C12Q; measuring or testing processes involving nucleic acid amplification reactions C12Q1/6844; fermentation processes to form a food composition, A21 or A23; compounds in general, see the relevant compound class, e.g. C01, C07)} - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - C12R: INDEXING SCHEME ASSOCIATED WITH SUBCLASSES C12C - C12Q, RELATING TO MICROORGANISMS - Y10S: TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS ## Abstract This invention relates to new antibiotics designated AA-896-A1, AA-896-A2, AA-896-A3, AA-896-A4, AA-896-A5, AA-896-A6, AA-896-Bl, AA-896-B2, AA-896-B3, AA-896-B4, AA-896-B5, AA-896-B6, AA-896-B7, AA-896-C1, AA-896-C2, AA-896-C3, AA-896-C4, AA-896-C5, AA-896-D1, AA-896-D2, AA-896-D3 and AA-896-D4 derived from the microorganism Streptomyces spp. LL-AA896 which are useful an anti-bacterial agents. ## Claims ### Claim 1 A process for producing a antibiotic AA-896 compound of the formula wherein: or pharmaceutically acceptable salts thereof said process comprising: cultivating a producing strain of Streptomyces spp. selected from the group LL4774, LL4794, LL4802, LL4808 and LL4892 or an antibiotic AA-896 producing mutant thereof, under aerobic conditions, in a suitable culture medium until a recoverable amount of said antibiotic AA-896 compound is formed in said medium and recovering said antibiotic AA-896 compound therefrom. ### Claim 2 A process for producing a antibiotic AA-896 compound of the formula wherein: or pharmaceutically acceptable salts thereof said process comprising: cultivating a producing strain of Streptomyces spp. selected from the group LL4774, LL4794, LL4802, LL4808, LL4879 and LL4892 or an antibiotic AA-896 producing mutant thereof, under aerobic conditions, in a suitable culture medium until a recoverable amount of said antibiotic AA-896 compound is formed in said medium and recovering said antibiotic AA-896 compound therefrom. ### Claim 3 A process for producing a antibiotic AA-896 compound of the formula wherein: or pharmaceutically acceptable salts thereof said process comprising: cultivating a producing strain of Streptomyces spp. selected from the group LL4774, LL4794, LL4802, LL4808, LL4879, LL4889 and LL4892 or an antibiotic AA-896 producing mutant thereof under aerobic conditions, in a suitable culture medium until a recoverable amount of said antibiotic AA-896 compound is formed in said medium and recovering said antibiotic AA-896 compound therefrom. ### Claim 4 A process for producing a antibiotic AA-896 compound of the formula or pharmaceutically acceptable salts thereof said process comprising: cultivating a producing strain of Streptomyces spp. selected from the group LL4774, LL4794, LL4802, LL4808, LL4879 and LL4892 or an antibiotic AA-896 producing mutant thereof, under aerobic conditions, in a suitable culture medium until a recoverable amount of said antibiotic AA-896 compound is formed in said medium and recovering said antibiotic AA-896 compound therefrom. ### Claim 5 A process for producing a antibiotic AA-896 compound of the formula or pharmaceutically acceptable salts thereof said process comprising: cultivating a producing strain of Streptomyces spp. selected from the group LL4774, LL4794, LL4802, LL4808, LL4879, LL4889 and LL4892 or an antibiotic AA-896 producing mutant thereof, under aerobic conditions, in a suitable culture medium until a recoverable amount of said antibiotic AA-896 compound is formed in said medium and recovering said antibiotic AA-896 compound therefrom. ### Claim 6 An isolated microorganism Streptomyces spp. LL-AA896, strain LL4774 or an AA-896 antibiotic producing mutant thereof. ### Claim 7 (depends on 6) The isolated microorganism of claim 6 wherein the AA-896 antibiotic producing mutant is strain LL4794, prepared by mutagenesis of strain LL4774. ### Claim 8 (depends on 6) The isolated microorganism of claim 6 wherein the AA-896 antibiotic producing mutant is strain LL4802, prepared by mutagenesis of strain LL4774. ### Claim 9 (depends on 6) The isolated microorganism of claim 6 wherein the AA-896 antibiotic producing mutant is strain LL4808, prepared by mutagenesis of strain LL4774. ### Claim 10 (depends on 6) The isolated microorganism of claim 6 wherein the AA-896 antibiotic producing mutant is strain LL469, prepared by mutagenesis of strain LL4774. ### Claim 11 (depends on 6) The isolated microorganism of claim 6 wherein the AA-896 antibiotic producing mutant is strain LL479, prepared by mutagenesis of strain LL4774. ### Claim 12 (depends on 6) The isolated microorganism of claim 6 wherein the AA-896 antibiotic producing mutant is strain LL482, prepared by mutagenesis of strain LL4774. ### Claim 13 A process for producing a antibiotic AA-896 compound of the formula or pharmaceutically acceptable salts thereof wherein: said process comprising: cultivating a producing strain of Streptomyces spp. selected from the group LL4774, LL4794, LL4802, LL4808, LL479 and LL482 or an antibiotic AA-896 producing mutant thereof under aerobic conditions, in a suitable culture medium until a recoverable amount of said antibiotic AA-896 compound is formed in said medium and recovering said antibiotic AA-896 compound therefrom. ### Claim 14 A process for producing a antibiotic AA-896 compound of the formula wherein: R1 is H or R2 is H, OH or OCH3; R3 is H or CH3; R4is represented by the formula n is an integer from 4 to 12; R5 is straight and branched alkyl of 1 to 4 carbon atoms, carbamimidoylamino or carbamimidoylhydroxyamino; or a pharmaceutically acceptable salt thereof said process comprising: cultivating a producing strain of Streptomyces spp. selected from the group LL4774, LL4794, LL4802, LL4808, LL479, LL469 and LL482 or an antibiotic AA-896 producing mutant thereof, under aerobic conditions, in a suitable culture medium until a recoverable amount of said antibiotic AA-896 compound is formed in said medium and recovering said antibiotic AA-896 compound therefrom. ### Claim 15 (depends on 14) The process according to claim 14, wherein the producing strain is selected from the group LL4774, LL4794, LL4802, LL4808, LL479, and LL482. ### Claim 16 (depends on 1) The process according to claim 1 wherein the producing strain of Streptomyces spp. is selected from the group LL4774, LL4794, LL4802, LL4808 and LL482. ### Claim 17 (depends on 2) The process according to claim 2 wherein the producing strain of Streptomyces spp. is selected from the group LL4774, LL4794, LL4802, LL4808, LL469 and LL482. ### Claim 18 (depends on 3) The process according to claim 3 wherein the producing strain of Streptomyces spp. is selected from the group LL4774, LL4794, LL4802, LL4808, LL469, LL479 and LL482. ### Claim 19 (depends on 4) The process according to claim 4 wherein the producing strain of Streptomyces spp. is selected from the group LL4774, LL4794, LL4802, LL4808, LL469, and LL482. ### Claim 20 (depends on 5) The process according to claim 5 wherein the producing strain of Streptomyces spp. is selected from the group LL4774, LL4794, LL4802, LL4808, LL469, LL479 and LL482. ### Claim 21 (depends on 13) The process according to claim 13 wherein the producing strain of Streptomyces spp. is selected from the group LL4774, LL4794, LL4802, LL4808, LL479 and LL482.