Abstract: This specification describes modified growth hormone having substantially diminished insulin-like and diabetogenic potencies relative to the native hormone with retention of substantially all of the anabolic potency of the native hormone. The modified growth hormone has the following structure: (a) elimination of from 1-5 to 1-19 amino acid residues from the amino terminus of the hormone; (b) cleavage of a peptide bond at any point from the carboxy moiety of residue 127 to residue 153; and (c) optionally, elimination of one or more of amino acid residues 128-152 of the hormone.
Abstract: Novel substituted quinazolinones have been found to exhibit specific binding to cholecystokinin (CCK) receptors in the brain and/or peripheral site such as the pancreas and ileum. The quinazolinones are CCK receptor antagonists and find therapeutic application in the treatment of gastrointestinal disorders and central nervous system disorders, and are useful for appetite regulation in mammals. Pharmaceutical formulations for such indications are described.
Type:
Grant
Filed:
September 13, 1990
Date of Patent:
December 24, 1991
Assignee:
Eli Lilly and Company
Inventors:
Melvin J. Yu, Jefferson R. McCowan, K. Jeff Thrasher
Abstract: A sulfoxide of human growth hormone has been produced and characterized. The sulfoxide derivative arises from a selective oxidation of Met.sup.14. The sulfoxide exhibits full biological activity.
Abstract: An enantiomerically selective process for acylating racemic 3-amino azetidinone intermediates is provided using penicillin G amidase(acylase) as biocatalyst.
Type:
Grant
Filed:
October 2, 1990
Date of Patent:
October 15, 1991
Assignee:
Eli Lilly and Company
Inventors:
Milton J. Zmijewski, Jr., Jeffrey N. Levy
Abstract: Cis .alpha.,.alpha./.beta., .beta.-3-amino-4-[2-(2-furyl)eth-1-yl]-1-methoxycarbonylmethyl-azetidin-2- one is resolved via (-)-2,3:4,6-di-O-isopropylidene-2-keto-L-gulonic acid hydrate (DAG).
Abstract: 3-Exomethylenecepham sulfoxide esters are obtained in improved yields via cyclization of 3-methyl-2-(4-chlorosulfinyl-2-oxo-3-acylamino-1-azetidinyl)-3-butenoic acid esters under anhydrous conditions with stannic chloride in the presence of both an oxo compound, e.g., an ether such as diethyl ether, a ketone such as acetone or methylethyl ketone, and an unsaturated compound, e.g., an alkene such as 1- or 2-hexene, a non-conjugated alkadiene such as 1,4-hexadiene, a cycloalkene such as cyclohexene, an allene, or a non-conjugated cycloalkadiene such as 1,4-cyclohexadiene.
Abstract: There is herein described an invention for promoting the rate and improving the quality of wound healing by topically applying insulin-like growth factor-II to the wound.
Abstract: This invention provides an insulin formulation stabilized against aggregation containing a hydroxybenzene and a polyethylene glycol-polypropylene glycol polymer of the formula ##STR1## having an average molecular weight of about 8350 and in which the average number of ethyleneoxy units per molecule, designated by the sum of a and c, is about 150, and the average number of propyleneoxy units per molecule, designated as b, is about 30.
Abstract: This application discloses a process for reducing methionine sulfoxide residues in peptides and proteins to methionine residues. The process comprises subjecting said peptide or protein to a substantially anhydrous trifluoroacetic acid reaction medium containing from about 0.01M to about 3M of an organic sulfide and from about 0.01M to about 3M of a haloacid selected from the group consisting of hydrochloric acid, hydrobromic acid, and hydroiodic acid.
Abstract: Method of blocking 5HT without effect on alpha receptors with 1-loweralkyl-6-straight chain alkyl-8.beta.-hydroxycycloalkyloxycarbonylergolines.
Type:
Grant
Filed:
July 25, 1988
Date of Patent:
March 7, 1989
Assignee:
Eli Lilly and Company
Inventors:
Marlene L. Cohen, Ray W. Fuller, William L. Garbrecht, Kathleen R. Whitten
Abstract: The invention relates to a process and compounds useful therein for producing a compound having an amino acid sequence defining a biologically active peptide or protein from a compound of the formulaH--X--Pro--Peptidein which X is the residue of a naturally occurring amino acid and Peptide is a sequence of amino acids defining a biologically active peptide or protein, which comprises subjecting H--X--Pro--Peptide to conditions under which a diketopiperazine of the H--X--Pro-- moiety is formed with accompanying cleavage and release of Peptide.
Abstract: This disclosure provides a crystalline human proinsulin, the preparation of which comprises(a) preparing an aqueous mixture containing from about 5 to about 50 mg/ml human proinsulin, from about 0.1 to about 5 mg/ml of a phenolic substance, from about 0.03 to about 0.6 milliequivalents/ml of a salt of a cation selected from the group consisting of lithium, calcium, sodium, potassium, ammonium, magnesium, and barium, and from about 0.2 to about 5 milliequivalents of Zn.sup.+2 cation;(b) adjusting the aqueous mixture to a pH in the range of from about 5.4 to about 6.5;(c) allowing crystal formation to occur; and(d) recovering crystalline human proinsulin from the aqueous mixture.