Abstract: The present invention provides a compound of the formula (I) wherein R1 is —H, —OH, —O(C1–C4 alkyl), —OCOC6H5, —OCO(C1–C6 alkyl), or —OSO2(C2–C6 alkyl); R0, R2 and R3 are each independently —H, —OH, —O(C1–C4 alkyl), —OCOC6H5, —OCO(C1–C6 alkyl), —OSO2(C2–C6 alkyl) or halo; R4 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3; X is —S— or —HC?CH—; G is —O—, —S—, —SO—, SO2, or —N(R5)—, wherein R5 is —H or C1–C4 alkyl; and Y is —O—, —S—, —NH—, —NMe-, or —CH2—; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions thereof, optionally in combination with estrogen and progestin; methods of inhibiting a disease associated with estrogen deprivation; and methods for inhibiting a disease associated with an aberrant physiological response to endogenous estrogen.
Abstract: The current invention provides novel 2-substituted 1,2,3,4-tetrahydroquinolin-6-ols and derivatives thereof of the formula (I) (A); pharmaceutical compositions thereof, optionally in combination with estrogen or progestin; methods for inhibiting a disease associated with estrogen deprivation; and methods for inhibiting a disease associated with an aberrant physiological response to endogenous estrogen.
Abstract: The present invention relates to a ?3 adrenergic receptor agonist of formula I: or a pharmaceutical salt thereof; which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful for treating Type 2 diabetes and/or obesity.
Type:
Grant
Filed:
December 24, 2002
Date of Patent:
March 7, 2006
Assignee:
Eli Lilly and Company
Inventors:
Cynthia Darshini Jesudason, Don Richard Finley
Abstract: The invention is particularly, although not exclusively, concerned with a protective container (1; 1?) for fragile articles (100), such as bottles, vials or ampoules of fluid medicament. In one aspect, the protective container is provided with impact energy-absorbing structural features for protecting the fragile article in the event of it being dropped, for instance impact energy-absorbing collars (45, 47; 45?, 47?) at, or adjacent to, the forward and rear end surfaces, respectively. In other aspects of the invention, the protective container (1; 1?) has a hanging member (17; 17?) and/or a corrugated wall structure (37, 39, 41, 43; 37?, 39?41?43?) and/or a latchable flap (55; 55?) for a dispensing aperture (57; 57?) in the container. In yet further aspects, there is provided a protective container having a re-formable label (101; 101?) and/or an internal skirt (73; 73?) for locating and retaining a feature on an article to be housed therein.
Type:
Grant
Filed:
November 21, 2001
Date of Patent:
January 10, 2006
Assignee:
Eli Lilly and Company
Inventors:
Peter Van Geert, Mischa Marteleur, Johan Berte
Abstract: A non-irritant topically acceptable carrier selected from the group consisting of: a) i) at least one of tripropylene glycol methyl ether and dipropylene glycol methyl ether, and ii) at least one of alcohol, wool grease and propylene glycol, wherein (i) is present in an amount of at least about 60% wt of the carrier; b) i) at least one of octyl palmitate, octyl stearate and glyceryl tri caprylate/caprate, and ii) at least one of dioctyl succinate, isopropyl myristate, cetearyl octanoate, propylene glycol 2 myristyl ether propionate, isopropyl palmitate, isopropyl laurate, isocetyl stearate, oleic acid and methyl oleate, and optionally including iii) at least one of alcohol, wool grease and propylene glycol, wherein (ii) is present in an amount of up to about 40% wt of the carrier; and c) i) at least one of octyl palmitate, octyl stearate and glyceryl tri caprylate/caprate, and ii) at least one of alcohol, wool grease and propylene glycol, wherein (i) is present in an amount of at least about 60% wt of the car
Type:
Grant
Filed:
November 17, 2000
Date of Patent:
October 18, 2005
Assignee:
Eli Lilly and Company
Inventors:
Kristina Clare Hacket, Lionel Barry Low, James Terence Rothwell
Abstract: This invention provides topical ectoparasiticidal fomulations comprising an ectoparasiticide, preferably a pyrethroid or a spinosyn, a spreading agent at is a (C3-C6) branched alkyl (C10-C20) alkanoate, preferably isopropyl myristate, and optionally a miscibilizing agent compatible with organic solvent systems, and methods of controlling an ectoparasite infestation on certain animals comprising topically applying such formulations to the animal.
Type:
Grant
Filed:
July 26, 2000
Date of Patent:
August 23, 2005
Assignee:
Eli Lilly and Company
Inventors:
James Web Kassebaum, Paul Thomas Pugh, William Webster Thompson
Abstract: The invention provides a stable ectoparasiticidal aqueous suspension formulation of a spinosyn, comprising the spinosyn, or a physiologically acceptable derivative or salt thereof, milled to an average particle size of 1 to 15 microns, a surfactant in an amount effective to facilitate wetting the milled particles; a dispersant in an amount that forms a spinosyn;dispersant weight ration of from 3:1 to 1:5; and water. It also provides a method of controlling an ectoparasite infestation on a small ruminant or companion animal comprising administering an effective amount of such an aqueous suspension formulation.
Type:
Grant
Filed:
August 2, 2000
Date of Patent:
August 9, 2005
Assignee:
Eli Lilly and Company
Inventors:
William Webster Thompson, Joseph Raymond Winkle
Abstract: Disclosed is a compound represented by structural formula (I): R1 is a substituted or unsubstituted aryl group. R2 and R3 are independently —H, a C1-C4 straight chained or branched alkyl group. R4 and R5 are independently —H, a C1-C4 straight chained or branched alkyl group or, taken together with the nitrogen atom to which each is bonded, a non-aromatic heterocyclic ring. Ring A and Ring B are independently further substituted with zero, one or two substituents. Physiologically acceptable salts of structural formula shown above are also included. Also disclosed is a method promoting growth, efficiency of feed utilization and/or production of lean body mass in a livestock animal. The method comprises administering to the animal an effective amount of one or more compounds represented by the structural formula as shown or a physiologically acceptable salt thereof.
Type:
Grant
Filed:
November 13, 2000
Date of Patent:
January 11, 2005
Assignee:
Eli Lilly and Company
Inventors:
Randall Bruce Hopkins, Deana Lori Hancock, Michael Eugene Quimby
Abstract: The invention provides single-dose oral formulations for controlling an ectoparasite infestation on a companion animal for a prolonged time, said formulations comprising a spinosyn component, or a physiologically acceptable derivative or salt thereof, and a carrier in oral dosage form. It also provides methods for controlling such infestations comprising orally administering a single dose of these formulations to the animal.
Abstract: Novel compounds and methods for preparing same, immunopotentiating compositions, and a method for potentiating the immune system of a host animal. The method comprises administering to the animal an effective amount of an immunopotentiating compound of Formula I or Formula II, or a physiologically acceptable salt.
Type:
Grant
Filed:
November 15, 2001
Date of Patent:
December 16, 2003
Assignee:
Eli Lilly and Company
Inventors:
Lawrence Camillo Creemer, Janice Rhea Herring, Edward Deorsey McGruder
Abstract: Disclosed is compound represented by Structural Formula (I), wherein Ring A, Ring B and Ring C are independently substituted or unsubstituted. R1 and R2 are independently a C1-C4 straight chained or branched alkyl group. Also disclosed is a method of increasing the quantity and improving quality of meat obtained from a livestock animal. The method comprises administering to the animal an effective amount of one or more compounds represented by Structural Formula (I).
Type:
Grant
Filed:
April 16, 2002
Date of Patent:
March 18, 2003
Assignee:
Eli Lilly and Company
Inventors:
Deana Lori Hancock, Randall Bruce Hopkins, Michael Eugene Quimby, Andrew Jason Wuethrich
Abstract: A dry composition of an ionophore antibiotic such as monensin comprising
from 10 to 95% (when expressed as the sodium salt) of at least one crystalline ionophore antibiotic,
from 0 to 10% antifoam agent(s),
from 0.1 to 20% wetting and/or surfactant agent(s),
from 0.1 to 10% dispersal agent(s), and
from 0.1 to 20% suspension agent(s).
The use of the composition is as a suspension in water alone or in conjunction with a milk replacer composition and/or a milk extender composition in water as a calf feed composition.
Abstract: The invention provides new fluorinated cephalosporin antibiotics of Formula I
wherein
Ra, Rb, Rc, Rd and Re, independently, are H, F or a C1-C6 alkyl-(Z)n— group having at least one fluorine substituent;
X is O or S;
Y is S, O, or —CH2—;
Z is O, S, —SO—, or —SO2—;
m and n independently are 0 or 1; and
R1 is H, C1-C6-alkyl, phenyl or benzyl, each of which may optionally have up to three substituents selected from halo, C1-C4-alkoxy, phenyl, NO2, C1-C6-alkanoyl, benzoyl, or C1-C6-alkanoyloxy; or a physiologically acceptable salt thereof;
and methods of preventing or treating or treating infection, particularly mastitis in ruminants, using these antibiotics.
Abstract: A wettable powder composition of crystalline monensin comprising from 90 to 95% (when expressed as the sodium salt) of crystalline monensin
from 0.1 to 2% antifoam agent,
from 0.1 to 5% wetting agent,
from 0.1 to 5% dispersal agent, and
from 0.1 to 5% suspension agent.
The use of the composition is as a suspension in water alone or in conjunction with a milk replacer composition or a milk extender composition in water as a calf feed composition.
Abstract: Safer pediculicidal formulations comprising a spinosyn, or a physiologically acceptable derivative or salt thereof, and a physiologically acceptable carrier, and methods of controlling lice infestations in a human with these formulations are provided.
Abstract: The invention provides new fluorinated cephalosporin antibiotics and methods of preventing or treating infection, particularly mastitis in ruminants, using these antibiotics, and veterinary and pharmaceutical formulations comprising these antibiotics.
Abstract: The present application relates to a series of novel sulfonic acid metal cation salts of the formula ##STR1## which are useful intermediates to prepare antifolate 5-substituted pyrrolo[2,3-d]pyrimidines. The present invention also relates to a novel process for preparing the sulfonic acid metal cation salts and to a novel process for preparing aldehydes of the formula ##STR2## from the corresponding sulfonic acid metal cation salts.
Type:
Grant
Filed:
September 24, 1998
Date of Patent:
January 11, 2000
Assignee:
Eli Lilly and Company
Inventors:
Douglas Patton Kjell, Brian James Slattery, Charles Jackson Barnett
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: 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: 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.
Type:
Grant
Filed:
August 12, 1996
Date of Patent:
March 31, 1998
Assignee:
Eli Lilly and Company
Inventors:
August M. Watanabe, Thomas F. Bumol, Mitchell I. Steinberg, Mary J. Kallman, Kurt Rasmussen