Abstract: The invention provides benzo?b!indenothiophene compounds of formula I ##STR1## wherein, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.6, are as defined in the specification, intermediates, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, cardiovascular-related pathological conditions including hyperlipidemia and related cardiovascular pathologies, and estrogen-dependent cancer.
Type:
Grant
Filed:
September 19, 1997
Date of Patent:
January 5, 1999
Assignee:
Eli Lilly and Company
Inventors:
Michael Gregory Bell, Brian Stephen Muehl, Mark Alan Winter
Abstract: The present invention provides anti-obesity proteins, which when administered to a patient regulate fat tissue. Accordingly, such agents allow patients to overcome their obesity handicap and live normal lives with much reduced risk for type II diabetes, cardiovascular disease and cancer.
Type:
Grant
Filed:
August 4, 1997
Date of Patent:
December 22, 1998
Assignee:
Eli Lilly and Company
Inventors:
Margret B. Basinski, Richard D. DiMarchi, David B. Flora, William F. Heath, Jr., James A. Hoffmann, Brigitte E. Schoner, James E. Shields, David L. Smiley
Abstract: This invention relates to carbamoyl substituted heterocycles which are .omega.-phenyl-.omega.-(3-pyridyl)-.omega.-alkenoic acid derivatives bearing a carbamoyl substituted oxazolyl or oxazolinyl group on the phenyl ring and which demonstrate utility for thromboxane receptor antagonism and/or thromboxane synthase inhibition, as well as pharmaceutical formulations containing them, methods for their use, and processes and intermediates for their preparation.
Type:
Grant
Filed:
May 23, 1997
Date of Patent:
December 15, 1998
Assignee:
Eli Lilly and Company
Inventors:
Joseph Anothony Jakubowski, Dale Eugene Mais, Kumiko Takeuchi
Abstract: This invention relates to a highly selective process for preparation of E-.omega.-phenyl-.omega.-(3-pyridyl)-.omega.-alkenoic acid derivatives bearing a carbamoyl substituted oxazolyl or oxazolinyl group on the phenyl ring which demonstrate utility for thromboxane receptor antagonism and/or thromboxane synthase inhibition, as well as to intermediates therefor.
Abstract: This invention provides methods of inhibiting pulmonary hypertensive disease which comprise administering to a mammal in need thereof a compound having activity as a tachykinin receptor antagonist.
Type:
Grant
Filed:
May 23, 1997
Date of Patent:
December 8, 1998
Assignee:
Eli Lilly and Company
Inventors:
Donald Richard Gehlert, Mitchell Irvin Steinberg
Abstract: This invention provides a method for treating a condition resulting from the cessation or withdrawal of tobacco or nicotine, opioids, ethanol or combinations thereof comprising administering an effective amount of 4-chloro-5-(imidazoline-2-y(amino)-6-methoxy-2-methylpyrimidine.
Abstract: The invention provides substituted-2-amino-1,2,3,4-tetrahydrodibenzofurans and 2-aminocyclohepta?b!benzo-furans useful as 5-HT.sub.1F agonists.
Type:
Grant
Filed:
August 25, 1997
Date of Patent:
December 8, 1998
Assignee:
Eli Lilly and Company
Inventors:
Michael E. Flaugh, Anton D. Kiefer, Jr.
Abstract: A method of inhibiting melanoma comprising administering to a human in need thereof an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine, hexamethyleneamino, and piperidino, or a pharmaceutically acceptable salt of solvate thereof; alone or in combination with one or more melanoma-inhibiting agents.
Abstract: New glycopeptide antibiotic A82846, comprising A82846A, A82846B and A82846C, is produced by Nocardia orientalis strains NRRL 18098, NRRL 18099 and NRRL 18100. The A82846 antibiotics have activity against Gram-positive bacteria comparable to that of vancomycin.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
December 1, 1998
Assignee:
Eli Lilly and Company
Inventors:
Robert L. Hamill, James A. Mabe, David F. Mahoney, Walter M. Nakatsukasa, Raymond C. Yao
Abstract: Sulfated benzothiophenes of the formula I ##STR1## wherein R.sup.1 is hydrogen, hydroxy, C.sub.1 -C.sub.4 alkoxy, --OCOO(C.sub.1 -C.sub.6 alkyl), --OCO(C.sub.1 -C.sub.6 alkyl), --OCOAr wherein Ar is phenyl or optionally substituted phenyl, --OSO.sub.2 (C.sub.4 -C.sub.6 straight chain alkyl), or --OSO.sub.3 H;R.sup.2 is R.sup.1, Cl or F; with the proviso that at least one of R.sup.1 or R.sup.2 is --OSO.sub.3 H;R.sup.3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; andn is 2 or 3;or a pharmaceutically acceptable salt or solvate thereof.
Type:
Grant
Filed:
April 14, 1997
Date of Patent:
December 1, 1998
Assignee:
Eli Lilly and Company
Inventors:
Michael Paul Clay, Charles Alan Frolik, Charles David Jones, Terry Donald Lindstrom
Abstract: This invention provides novel bis-indolemaleimide macrocycle derivatives of the formula: ##STR1## The invention further provides the preparation, pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals.
Type:
Grant
Filed:
July 12, 1997
Date of Patent:
December 1, 1998
Assignee:
Eli Lilly and Company
Inventors:
William F. Heath, Jr., Michael R. Jirousek, John H. McDonald, III, Christopher J. Rito
Abstract: The present invention provides glycopeptide antibiotic derivative compounds. These derivative compounds possess antibacterial activity aginst a wide variety of bacteria, including activity against vancomycin-resistant isolates. Methods of making and using these glycopeptide antibiotic derivative compounds are also provided.
Type:
Grant
Filed:
March 12, 1997
Date of Patent:
December 1, 1998
Assignee:
Eli Lilly and Company
Inventors:
Robin D. G. Cooper, Bret E. Huff, Thalia I. Nicas, John T. Quatroche, Michael J. Rodriguez, Nancy J. Snyder, Michael A. Staszak, Richard C. Thompson, Stephen C. Wilkie, Mark J. Zweifel
Abstract: The invention provides benzothiophene compounds, of formula I, ##STR1## wherein R1, R2, R3, R4 and n are as defined in the specification, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions, including hyperlipidemia, and other cardiovascular pathologies.
Type:
Grant
Filed:
September 19, 1997
Date of Patent:
December 1, 1998
Assignee:
Eli Lilly and Company
Inventors:
Kenneth Lee Hauser, Alan David Palkowitz, Kenneth Jeff Thrasher
Abstract: The invention provides benzothiophene compounds, formulations, and methods of 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:
December 1, 1998
Assignee:
Eli Lilly and Company
Inventors:
George Joseph Cullinan, Brian Stephen Muehl
Abstract: The use of a compound of the formula: ##STR1## in which X is --O-- or --NH--, or a pharmaceutically-acceptable acid addition salt thereof, in the treatment of atherosclerosis.
Abstract: A method of inhibiting endometrial mitoses comprising administering to a human in need thereof an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, --CH.sub.3, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine, hexamethyleneamino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.