Abstract: Acylamino pyrrole compounds having anti-allergic activity, methods of making the compounds and pharmaceutical formulations containing the compounds.
Type:
Grant
Filed:
June 1, 1976
Date of Patent:
May 9, 1978
Assignee:
Lilly Industries Limited
Inventors:
Delme Evans, Michael R. J. Jolley, William J. Ross, Brian P. Swann
Abstract: Vincaleukoblastine (VLB, vinblastine) is reacted with thionyl chloride to form a bis-sulfite ester which is converted to various 5'-oxygenated derivatives.
Type:
Grant
Filed:
October 20, 1976
Date of Patent:
May 2, 1978
Assignee:
Eli Lilly and Company
Inventors:
Allen S. Katner, Gerald E. Gutowski, Jean C. Miller
Abstract: Substituted 1-hydroxy-2-(1,1-difluoroalkyl)-1H-imidazo-(4,5-b)pyridine compounds useful as herbicides; and intermediates useful in the synthesis of these compounds. In addition to exhibiting herbicidal activity, the substituted 1-hydroxy-2-(1,1-difluoroalkyl)-1H-imidazo(4,5-b)pyridine compounds are of low mammalian toxicity.
Type:
Grant
Filed:
September 8, 1975
Date of Patent:
May 2, 1978
Assignee:
Eli Lilly and Company
Inventors:
George O. P. O'Doherty, Kenneth H. Fuhr
Abstract: 2,6-Dimethoxyphenol reacts with a tertiary carbinol in the presence of an acid to provide exclusively a 1-hydroxy-2,6-dimethoxy-4-tertiary alkyl)benzene, which when reacted with a halogenated disubstituted phosphite affords a 2,6-dimethoxy-4-tertiary alkyl)phenyl disubstituted phosphate. Reduction of the phenyl phosphate derivative by reaction with an alkali metal affords a 1-(tertiary alkyl)-3,5-dimethoxybenzene, which upon reaction with a demethylating agent provides a 5-(tertiary alkyl)resorcinol.
Abstract: The tetradecapeptides ##STR1## in which Y is L-Asn or L-Ala are described along with corresponding non-toxic pharmaceutically-acceptable acid addition salts as well as intermediates useful in the synthesis of the tetradecapeptides. These tetradecapeptides as well as their pharmaceutically-acceptable acid addition salts exhibit various activities including inhibition of the release of gastric acid.
Abstract: 5'-Deoxy-5'-(3'-aminopiperidin-2-one-6-yl)adenosine and 5'-deoxy-5'-(1-amino-4-ureido-4-carboxyamidobutyl)-adenosine and the pharmaceutically acceptable acid addition salts thereof are antifungal antibiotics active vs. systemic infections produced by culturing Streptomyces griseolus NRRL 3739 and are isolated from the broth and obtained pure via chromatography over cationic resin.
Type:
Grant
Filed:
September 27, 1976
Date of Patent:
May 2, 1978
Assignee:
Eli Lilly and Company
Inventors:
Robert L. Hamill, Ramakrishnan Nagarajan
Abstract: Crude preparations of 2-phenyl-5-benzoxazolylalkanoic acids are purified by forming the ammonium salt thereof in an organic solvent and thermally reconverting the separated ammonium salt to the acid. Gaseous ammonia is a by-product.
Abstract: A ventilated animal cage system is provided in which a plurality of animal cages are removably suspended on shelves of a portable rack. Each shelf is hollow to form an air duct that is in communication with the cages suspended therefrom, thus minimizing the possibility of cross-contamination between animals in the cages and personnel in the laboratory room.
Type:
Grant
Filed:
September 17, 1976
Date of Patent:
April 25, 1978
Assignee:
Eli Lilly and Company
Inventors:
Thomas M. Gland, Robert C. A. Frederickson
Abstract: Antibiotic A-28086 complex, comprising microbiologically active, structurally related factors A, B, and D, produced by submerged aerobic fermentation of Streptomyces aureofaciens NRRL 5758. Individual factors A, B, and D are separated and isolated by chromatography. The A-28086 antibiotics are antibacterial, antifungal, antiviral, anti-PPLO, anticoccidial, insecticidal and acaricidal agents and also increase feed-utilization efficiency in ruminants.
Type:
Grant
Filed:
September 2, 1976
Date of Patent:
April 18, 1978
Assignee:
Eli Lilly and Company
Inventors:
David H. Berg, Robert L. Hamill, Marvin M. Hoehn
Abstract: Antibiotic A-35512 complex, comprising microbiologically active, related factors A, B, C, E and H, is produced by submerged aerobic fermentation of Streptomyces candidus NRRL 8156. The individual A-35512 factors are separated and isolated by chromatography. The A-35512 antibiotics are antibacterial and growth-promoting agents and increase feed-utilization efficiency in animals. In addition, A-35512 factor B is useful in the treatment of dental caries and acne.
Abstract: Synergistic coccidiocidal combinations comprise two ionophorous fermentation-derived coccidiocides, each of which is administered to poultry in a concentration too low to produce satisfactory coccidiocidal effect alone. Preferred combinations include monensin and A204, monensin and lasalocid, and monensin and A28086.
Abstract: Acylamino heteroaryl compounds in which the heteroaryl nucleus is a 5-membered ring containing a single heteroatom, which may be oxygen, or sulphur, methods of making the compounds and pharmaceutical formulations containing the compounds. The compounds have anti-allergy activity.
Type:
Grant
Filed:
June 1, 1976
Date of Patent:
April 4, 1978
Assignee:
Lilly Industries Limited
Inventors:
Delme Evans, Michael Ralph John Jolley, William James Ross, Brian Picton Swann
Abstract: N-Chlorophthalimide is prepared by contacting an alkali metal salt of phthalimide with chlorine under substantially non-aqueous conditions in the presence of a halogenated aliphatic hydrocarbon and at a temperature of from about -10.degree. C. to about +40.degree. C.
Abstract: Methylenation of catechol by reaction with a methylene dihalide under alkaline conditions is improved by adding the pre-formed catechol dianion in a heated protic alkaline medium to a solution of methylene dihalide in dimethyl sulfoxide.