Abstract: A proinsulin-like disulfide insulin precursor is produced from its corresponding linear chain S-sulfonate insulin precursor by reacting the S-sulfonate with a mercaptan in an amount which provides from about 1 to about 5 --SH moieties per --SSO.sub.3.sup.- moiety in an aqueous medium at a pH of from about 7 to about 11.5 and at an S-sulfonate concentration of up to about 10 mg. per ml. of aqueous medium.
Abstract: A method is described for preventing or minimizing the effects of a drug on an embryo or a fetus by placental transport while alleviating pain and anxiety of the pregnant female by administering a pharmaceutically effective amount of a compound of the formulaH-L-Tyr-D-Ala-Gly-L-Phe-L-(N-CH.sub.3)Met-NH.sub.2or a pharmaceutically acceptable salt thereof.
Abstract: Cephalosporin broad spectrum antibiotics possessing a 7.beta.-[2-[(2-aminooxazol)-4-yl]-2-(substituted oximino)acetamido side chain and a variety of substituents at the 3-position of the cephalosporins are claimed. Also claimed are intermediates in the synthesis of the above cephalosporin antibiotics.
Abstract: This invention provides a novel allylic chlorination process for inserting a chlorine atom on the saturated methyl group of a 3-methyl-2-but-3-enoate group on the ring nitrogen atom of a 2-azetidinone or thiazolinoazetidinone. The chloro-substituted compounds prepared thereby are novel intermediates used in preparation of cephalosporins.
Abstract: Compositions having as the essentially active ingredients a mixture of mefluidide and a pyrimidinemethanol growth regulator are disclosed. A method for controlling seedhead formation in turfgrasses employing the compositions is provided.
Abstract: A .beta.-cyanoethyl blocking group is selectively removed from the phosphate moiety of a nucleotide or polynucleotide by treatment with diethyl amine.
Abstract: This invention describes a process for selectively preparing trans-1-isopropylsulfonyl-2-amino-6-(1-phenyl-1-propenyl)benzimidazole by dehydrating the corresponding benzimidazole carbinol with certain specific acids.
Abstract: Zinc salts are used to effect the regio-selective acylation and alkylation of the 1-amino group of 4-O-substituted-2-deoxystreptamine-containing aminoglycosides. The 1-N-substituted derivatives of apramycin, 3'-hydroxyapramycin, certain .alpha. or .beta.-(lower alkyl)aprosaminides and certain .alpha. or .beta.-(substituted lower alkyl)-aprosaminides are new. The 1-N-substituted-4-O-substituted-2-deoxystreptamine aminoglycosides produced by the process of this invention are antibacterial agents.
Abstract: Nickel salts are used to effect the regio-selective acylation and alkylation of the 2'-amino group of 4-O-substituted-2-deoxystreptamine containing aminoglycosides. The 2'-N-substituted derivatives of apramycin, certain .alpha. or .beta.-(lower alkyl)aprosaminides and certain .alpha. or .beta.-(substituted lower alkyl)aprosaminides are new. The 2'-N-substituted-4-O-substituted-2-deoxystreptamine aminoglycosides produced by the process of this invention are antibacterial agents.
Abstract: 20-Dihydro-20-deoxy-23-de(mycinosyloxy)tylosin (20-deoxo-DMOT), specified 2'-acyl ester derivatives, and their acid addition salts are useful intermediates and antibacterial agents. Methods of preparing 20-deoxo-DMOT and 5-O-mycaminosyltylactone by fermentation of Streptomyces fradiae ATCC 31733 are included.
Abstract: Production of insulin or an insulin analog is provided by combination of an A-chain and a B-chain, which comprises bringing the S-sulfonated form of the A-chain, the S-sulfonated form of the B-chain, and a thiol reducing agent together in an aqueous medium under conditions which produce a mixture having (1) a pH of from about 8 to about 12, (2) a total protein concentration of from about 0.1 to about 50 milligrams per milliliter, and (3) an amount of thiol reducing agent which affords a total of from about 0.4 to about 2.5 --SH groups per each --SSO.sub.3.sup.- group present in the total amount of A- and B-chain S-sulfonates, and allowing formation of insulin or an insulin analog to occur by maintaining the mixture at a temperature of from about 0.degree. C. to about 25.degree. C. and in an environment which provides a source of oxygen.
Abstract: This invention is directed to the use of certain benzimidazoles and benzimidazolines as an agent for the control of colonial insects, especially fire ants.
Abstract: 1-Substituted-2-amino-5(or 6) olefinic benzimidazoles and intermediates therefor are disclosed. The compounds are potent antiviral agents. Pharmaceutical formulations containing such compounds and a method of treating viral infections are provided.
Type:
Grant
Filed:
April 8, 1982
Date of Patent:
December 13, 1983
Assignee:
Eli Lilly and Company
Inventors:
Tina M. Morwick, Charles J. Paget, James H. Wikel
Abstract: 23-Demycinosyltylosin (DMT) which has the formula: ##STR1## 20-dihydro-DMT, specified acyl ester derivatives, and their acid addition salts are useful antibacterial agents. Improved methods of making 5-O-mycaminosyltylonolide (OMT) and 20-dihydro-OMT by mild acid hydrolysis of DMT and 20-dihydro-DMT, respectively, are included.
Type:
Grant
Filed:
May 6, 1981
Date of Patent:
December 6, 1983
Assignee:
Eli Lilly and Company
Inventors:
Richard H. Baltz, Gene M. Wild, Eugene T. Seno
Abstract: A .beta.-cyanoethyl blocking group is selectively removed from the phosphate moiety of a nucleotide or polynucleotide by treatment with a primary amine having from 3 to 5 carbon atoms.