Patents Represented by Attorney William C. Martens
  • Patent number: 5079345
    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.
    Type: Grant
    Filed: August 19, 1988
    Date of Patent: January 7, 1992
    Assignee: Eli Lilly and Company
    Inventors: Gerald W. Becker, Carl J. Shaar
  • Patent number: 5075313
    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
  • Patent number: 5068317
    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.
    Type: Grant
    Filed: March 15, 1988
    Date of Patent: November 26, 1991
    Assignee: Eli Lilly and Company
    Inventors: Gerald W. Becker, Ralph M. Riggin
  • Patent number: 5057607
    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
  • Patent number: 5030725
    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).
    Type: Grant
    Filed: February 6, 1990
    Date of Patent: July 9, 1991
    Assignee: Eli Lilly and Company
    Inventors: John A. Rieck, III, Ian G. Wright
  • Patent number: 5026707
    Abstract: This invention provides ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes which are selective inhibitors of serotonin reuptake.
    Type: Grant
    Filed: January 16, 1990
    Date of Patent: June 25, 1991
    Assignee: Eli Lilly and Company
    Inventors: James A. Nixon, Richard P. Pioch, John M. Schaus, Robert D. Titus
  • Patent number: 4968802
    Abstract: Alkoxycycloalkyl esters of 1-substituted-6-C.sub.1-4 straight chain alkyl (or allyl)ergoline-8.beta.-carboxylic acids, useful as 5HT receptor antagonists.
    Type: Grant
    Filed: January 10, 1990
    Date of Patent: November 6, 1990
    Assignee: Eli Lilly and Company
    Inventors: William L. Garbrecht, Gifford P. Marzoni, Kathleen R. Whitten
  • Patent number: 4950753
    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.
    Type: Grant
    Filed: May 17, 1989
    Date of Patent: August 21, 1990
    Assignee: Eli Lilly and Company
    Inventors: James D. Copp, Gregg A. Tharp
  • Patent number: 4939258
    Abstract: Cycloalkyl or ketocycloalkyl esters of 1-substituted-6-C.sub.1-4 straight chain alkyl (or allyl)-ergoline-8.beta.-carboxylic acids, useful as 5HT receptor antagonists.
    Type: Grant
    Filed: January 10, 1990
    Date of Patent: July 3, 1990
    Assignee: Eli Lilly and Company
    Inventors: Kathleen R. Whitten, William L. Garbrecht, Gifford P. Marzoni, C. John Parli
  • Patent number: 4914107
    Abstract: This invention relates to the use in vivo of 1-isopropyldihydrolysergic acid as a 5-HT.sub.2 antagonist.
    Type: Grant
    Filed: January 17, 1989
    Date of Patent: April 3, 1990
    Assignee: Eli Lilly and Company
    Inventors: Marlene L. Cohen, Mark J. Goldberg, Louis Lemberger
  • Patent number: 4914100
    Abstract: Alkoxycycloalkyl esters of 1-substituted-6-C.sub.1-4 straight chain alkyl (or allyl)ergoline-8.beta.-carboxylic acids, useful as 5HT receptor antagonists.
    Type: Grant
    Filed: April 24, 1989
    Date of Patent: April 3, 1990
    Assignee: Eli Lilly and Company
    Inventors: William L. Garbrecht, Gifford P. Marzoni, Kathleen R. Whitten
  • Patent number: 4906639
    Abstract: Cycloalkyl or ketocycloalkyl esters of 1-substituted-6-C.sub.1-4 straight chain alkyl (or allyl)-ergoline-8.beta.-carboxylic acids, useful as 5HT receptor antagonists.
    Type: Grant
    Filed: April 11, 1989
    Date of Patent: March 6, 1990
    Assignee: Eli Lilly and Company
    Inventors: Kathleen R. Whitten, William L. Garbrecht, Gifford P. Marzoni, C. John Parli
  • Patent number: 4885163
    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.
    Type: Grant
    Filed: February 24, 1987
    Date of Patent: December 5, 1989
    Assignee: Eli Lilly and Company
    Inventors: Carl J. Shaar, Michele C. Smith
  • Patent number: 4847261
    Abstract: Alkoxycycloalkyl esters of 1-substituted-6-C.sub.1-4 straight chain alkyl (or allyl)ergoline-8.beta.-carboxylic acids, useful as 5HT receptor antagonists.
    Type: Grant
    Filed: September 29, 1988
    Date of Patent: July 11, 1989
    Assignee: Eli Lilly and Company
    Inventors: William L. Garbrecht, Gifford P. Marzoni, Kathleen R. Whitten
  • Patent number: 4845224
    Abstract: Cycloalkyl or ketocycloalkyl esters of 1-substituted-6-C.sub.1-4 straight chain alkyl (or allyl)-ergoline-8.beta.-carboxylic acids, useful as 5HT receptor antagonists.
    Type: Grant
    Filed: April 29, 1987
    Date of Patent: July 4, 1989
    Assignee: Eli Lilly and Company
    Inventors: Kathleen R. Whitten, William L. Garbrecht, Gifford P. Marzoni, C. John Parli
  • Patent number: 4839341
    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.
    Type: Grant
    Filed: November 13, 1987
    Date of Patent: June 13, 1989
    Assignee: Eli Lilly and Company
    Inventors: Eddie H. Massey, Theodore A. Sheliga
  • Patent number: 4835254
    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.
    Type: Grant
    Filed: August 24, 1987
    Date of Patent: May 30, 1989
    Assignee: Eli Lilly and Company
    Inventors: Richard D. DiMarchi, Harlan B. Long
  • Patent number: 4810710
    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
  • Patent number: 4782139
    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.
    Type: Grant
    Filed: October 23, 1986
    Date of Patent: November 1, 1988
    Assignee: Eli Lilly and Company
    Inventors: Richard D. DiMarchi, Gerald S. Brooke
  • Patent number: 4764592
    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.
    Type: Grant
    Filed: April 23, 1987
    Date of Patent: August 16, 1988
    Assignee: Eli Lilly and Company
    Inventors: Eddie H. Massey, Richard L. Jackson