Abstract: The invention provides naphthofluorene compounds, intermediates, formulations, processes, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, cardiovascular-related pathological conditions, including hyperlipidemia, and estrogen-dependent cancer.
Type:
Grant
Filed:
September 30, 1998
Date of Patent:
September 28, 1999
Assignee:
Eli Lilly and Company
Inventors:
Henry Uhlman Bryant, Jeffrey Alan Dodge, Charles Willis Lugar, III
Abstract: The invention provides a compound of formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical compositions containing a compound of formula I, and methods of using a compound of formula I for inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions including hyperlipidemia, and estrogen dependent cancer.
Type:
Grant
Filed:
October 23, 1997
Date of Patent:
September 14, 1999
Assignee:
Eli Lilly and Company
Inventors:
George Joseph Cullinan, Brian Stephen Muehl
Abstract: This invention is concerned with improved processes for reductive alkylation of glycopeptide antibiotics. The improvement residing in providing a source of copper which results in the initial production of a copper complex of the glycopeptide antibiotic. Reductive alkylation of this complex favors regioselective alkylation and increased yields. Copper complexes of the glycopeptide antibiotic starting materials and of the alkylated products are also part of the invention.
Type:
Grant
Filed:
November 12, 1997
Date of Patent:
September 14, 1999
Assignee:
Eli Lilly and Company
Inventors:
Richard Alan Berglund, Nancy Anne Lockwood, Howard Eugene Magadanz, Hua Zheng
Abstract: The present invention is directed to glycopeptides and more particularly to derivatives of the glycopeptide A82846B. In these derivatives, the leucyl has been removed to create "hexapeptides" of A82846B and its N.sup.DISACC variations. These hexapeptides are useful as antibacterials and also as starting materials from which further antibacterial compounds are prepared.
Type:
Grant
Filed:
April 30, 1998
Date of Patent:
September 14, 1999
Assignee:
Eli Lilly and Company
Inventors:
Richard Craig Thompson, Stephen Charles Wilkie
Abstract: The present invention provides novel methods of lowering serum cholesterol and inhibiting smoother muscle cell proliferation, particularly restenosis, in humans, and inhibiting uterine fibroid disease and endometriosis in women comprising administering to a human/woman in need of treatment an effective amount of a compound of formula I ##STR1## wherein R is C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, halo, or trifluoromethyl;R.sup.1 and R.sup.2 each are the same or different C.sub.1 -C.sub.6 alkyl group;n is an integer from 2 to 6; andR.sup.3 and R.sup.4 each are independently C.sub.1 -C.sub.4 alkyl, or combine to form a substituent selected from the group consisting of pyrrolidino, morpholino, piperidino, piperazino, 4-(C.sub.1 -C.sub.6 alkyl)piperazino, and 4-phenyl-piperazino;or a pharmaceutically acceptable salt thereof.
Abstract: The present invention provides a method for treating neuropathic pain comprising administering an analgesic dosage of a compound of formula I to an animal in need of such treatment certain phenyl oxazoles or phenyl thiazoles.
Abstract: The present invention discloses various parenteral pharmaceutical formulations having a protracted effect, which comprise: a sterile aqueous suspension of about 20 U/mL to about 500 U/mL insulin analog, about 5 mg/mL to about 10 mg/mL sodium chloride, about 0.2 to about 2.0 mg/mL physiologically acceptable buffer, a zinc ion content of about 0.07 mg/mL to about 0.1 mg/mL, and a physiologically acceptable preservative at a pH of about 6.5 to about 7.8; such that less than 5% of the analog present in the suspension is in the dissolved state.
Abstract: The invention provides isolated nucleic acid compounds encoding the stem peptide biosynthetic gene murI of Streptococcus pneumoniae. Also provided are vectors and transformed heterologous host cells for expressing the MurI enzyme product and a method for identifying compounds that inhibit stem peptide biosynthesis.
Type:
Grant
Filed:
December 4, 1996
Date of Patent:
September 7, 1999
Assignee:
Eli Lilly and Company
Inventors:
Jo Ann Hoskins, Franklin Harpold Norris, Pamela Kay Rockey, Paul Robert Rosteck, Jr., Paul Luther Skatrud, Patti Jean Treadway, Michele Louise Young Bellido, Chyun-Yeh Earnest Wu
Abstract: Novel benzothiophenes, ##STR1## wherein R.sub.1, R.sub.2, and R.sub.3 are independently --OH, --OCO(C.sub.1 -C.sub.6 alkyl), --O(CO)O(C.sub.1 -C.sub.6 alkyl), --OCO--Ar, where Ar is phenyl or substituted phenyl, or --O(CO)O--phenyl; and R.sub.4 is N-pyrrolidinyl, N-piperidinyl, or N-hexamethyleneimino, and intermediates thereof, and the uses and formulations thereof, are provided by the present invention.
Type:
Grant
Filed:
June 25, 1997
Date of Patent:
September 7, 1999
Assignee:
Eli Lilly and Company
Inventors:
David Thompson Berg, George Joseph Cullinan, Brian William Grinnell, Mark Alan Richardson
Abstract: The present invention provides for the reaction of optionally substituted indole-3-acetamides with optionally substituted methyl indole-3-glyoxyl reagent to prepare potent PKC inhibitors.
Type:
Grant
Filed:
May 19, 1998
Date of Patent:
September 7, 1999
Assignee:
Eli Lilly and Company
Inventors:
Margaret Mary Faul, Leonard Larry Winneroski, Jr.
Abstract: This invention relates to the field of pharmaceutical and organic chemistry and provides benzothiophene compounds, intermediates, formulations, and methods.
Type:
Grant
Filed:
September 3, 1997
Date of Patent:
September 7, 1999
Assignee:
Eli Lilly and Company
Inventors:
Henry Uhlman Bryant, Michael John Martin, Ken Matsumoto
Abstract: A DNA molecule isolated from Streptomyces ambofaciens encodes the multi-functional proteins which direct the synthesis of the polyketide platenolide.
Type:
Grant
Filed:
February 21, 1997
Date of Patent:
August 31, 1999
Assignee:
Eli Lilly and Company
Inventors:
Stanley G. Burgett, Stuart A. Kuhstoss, Ramachandra N. Rao, Mark A. Richardson, Paul R. Rosteck, Jr.
Abstract: The invention provides isolated nucleic acid compounds encoding a multiple drug resistance protein of Aspergillus nidulans. Vectors and transformed host cells comprising the multiple drug resistance-encoding DNA of Aspergillus nidulans atrC are also provided. The invention further provides assays which utilize these transformed host cells.
Type:
Grant
Filed:
December 23, 1997
Date of Patent:
August 31, 1999
Assignee:
Eli Lilly and Company
Inventors:
Paul Luther Skatrud, Maarten A. de Waard, Alan C. Andrade, Robert Brown Peery
Abstract: The present invention provides a method for treating pain using a composition comprising olanzapine and Drug Useful in the Treatment of Pain.
Abstract: The present invention provides a method for treating pain using a composition comprising certain phenyl oxazoles or phenyl thiazoles in combination with a Drug Useful in the Treatment of Pain.
Abstract: The invention provides novel 5-HT.sub.1f agonists of formula (I) where X, R.sup.1, R.sup.2, and R.sup.3 are defined in the specification, which are useful for the treatment of migraine and associate disorders.
Type:
Grant
Filed:
March 13, 1998
Date of Patent:
August 24, 1999
Assignee:
Eli Lilly and Company
Inventors:
James E Fritz, Patric J Hahn, Stephen W Kaldor, Miles G Siegel, Yao-Chang Xu