Abstract: The present invention relates to a process for preparing 5-nitroquinoline hydrohalide comprising:
(A) heating a slurry comprising a mixture of nitroquinoline position isomer hydrohalide salts in wet dimethylformamide to form a solution;
(B) cooling the solution of Step (A) until a precipitate comprising 5-nitroquinoline hydrohalide is formed; and
(C) collecting the precipitate.
Abstract: Formulations and applications thereof are described which are useful for the inhibition of various medical conditions associated with estrogen deprivation syndrome including osteoporosis and hyperlipidemia utilizing compounds of structure I represented by the following structure
in combination with compounds of formula II represented by the following structure
where X, Y, R, R′, R6, R7 and R8 are as defined herein.
Type:
Grant
Filed:
September 1, 1999
Date of Patent:
July 10, 2001
Assignee:
Eli Lilly and Company
Inventors:
George Joseph Cullinan, Brian Stephen Muehl, Kenneth Jeff Thrasher
Abstract: A method for alleviating the symptoms of post-menopausal syndrome comprising administering to a woman in need thereof an effective amount of a compound of formula I
wherein
R1a is —H or —OR7a in which R7a is —H or a hydroxy protecting group;
R2a is —H, halo, or —OR8a in which R8a is —H or a hydroxy protecting group;
R3 is 1-piperidinyl, 1-pyrrolidino, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino;
n is 2 or 3; and
Z is —O— or —S—;
or a pharmaceutically acceptable salt thereof.
Abstract: This invention discloses an efficient process for selectively sulfonating the primary alcohol of a diol containing both primary and secondary alcohols.
Type:
Grant
Filed:
February 25, 1998
Date of Patent:
February 27, 2001
Assignees:
Eli Lilly and Company, Wayne State University, University of Hawaii
Abstract: This invention provides methods which are useful for the inhibition of the various medical conditions associated with estrogen deprivation syndrome including osteoporosis and hyperlipidemia utilizing compounds of formula I: ##STR1##
Abstract: A method of increasing sphincter competence comprising administering to a human in need of treatment 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 pyrrolidino, hexamethyleneimino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.Also encompassed by the invention is a method of inhibiting urinary or fecal incontinence, or gastroesophageal disease or its symptoms, which includes administering to a human in need thereof an effective amount of a compound of formula 1.
Abstract: The present invention provides a method of minimizing the uterotrophic effect of a compound of formula II ##STR1## or a pharmaceutically acceptable salt or solvate thereof, comprising concurrently or sequentially administering a compound of formula I ##STR2## or pharmaceutically acceptable salt or solvate thereof.
Type:
Grant
Filed:
June 2, 1997
Date of Patent:
August 29, 2000
Assignee:
Eli Lilly and Company
Inventors:
Henry Uhlman Bryant, Jeffrey Alan Dodge
Abstract: A method of safely lowering platelet count in a human which comprises the administration to a human in need thereof of an effective amount of a compound of formula I ##STR1## wherein R.sup.1 and R.sup.3 are, independently, --H, --CH.sub.3, --CO(C.sub.1 -C.sub.6 alkyl), or --COAr, where Ar is optionally substituted phenyl;R.sup.2 is selected from the group consisting of pyrrolidine, piperidine, and hexamethyleneimino; ora pharmaceutically acceptable salt or solvate thereof.
Abstract: This invention provides methods which are useful for the inhibition of the various medical conditions associated with estrogen deprivation syndrome including osteoporosis and hyperlipidemia utilizing compounds of formula I: ##STR1##
Abstract: Formulations and applications thereof are described which are useful for the inhibition of various medical conditions associated with estrogen deprivation syndrome including osteoporosis and hyperlipidemia utilizing compounds represented by the following structure where X is a halogen.
Type:
Grant
Filed:
September 1, 1999
Date of Patent:
July 11, 2000
Assignee:
Eli Lilly and Company
Inventors:
George Joseph Cullinan, Brian Stephen Muehl, Kenneth Jeff Thrasher
Abstract: The present invention provides a method of treating depression, mood swings, or Alzheimer's disease in a patient in need of such treatment by administering a selective estrogen receptor modulating compound of the formula ##STR1## in which R.sup.1 and R.sup.2 are independently hydroxy and alkoxy of one to four carbon atoms; and R.sup.3 and R.sup.4 are independently methyl or ethyl, or R.sup.3 and R.sup.4, taken together with the nitrogen atom to which they are attached, form a pyrrolidino, methyl-pyrrolidino, dimethylpyrrolidino, piperidino, morpholino, or hexamethyleneimino ring.
Type:
Grant
Filed:
April 9, 1998
Date of Patent:
June 20, 2000
Assignee:
Eli Lilly and Company
Inventors:
Kelly Renee Bales, Henry Uhlman Bryant, Steven Marc Paul, Mary Patricia Knadler
Abstract: A method for alleviating the symptoms of post-menopausal syndrome comprising administering to a woman in need thereof an effective amount of a compound of formula I ##STR1## wherein R.sup.1a is --H or --OR.sup.7a in which R.sup.7a is --H or a hydroxy protecting group;R.sup.2a is --H, halo, or --OR.sup.8a in which R.sup.8a is --H or a hydroxy protecting group;R.sup.3 is 1-piperidinyl, 1-pyrrolidino, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino;n is 2 or 3; andZ is --O-- or --S--;or a pharmaceutically acceptable salt thereof.
Abstract: A method of preventing headache in a human is disclosed which comprises the administration to a human in need thereof of an effective amount of a compound of formula I ##STR1## wherein R.sup.1 and R.sup.3 are, independently, --H, --CH.sub.3, --CO(C.sub.1 -C.sub.6 alkyl), or --COAr, where Ar is optionally substituted phenyl;R.sup.2 is selected from the group consisting of pyrrolidine, piperidine, and hexamethyleneimino; ora pharmaceutically acceptable salt or solvate thereof.
Abstract: A method for alleviating the symptoms of post-menopausal syndrome comprising administering to a woman in need thereof an effective amount of a compound of formula I ##STR1## wherein R.sup.1a is --H or --OR.sup.7a in which R.sup.7a is --H or a hydroxy protecting group;R.sup.2a is --H, halo, or --OR.sup.8a in which R.sup.8a is --H or a hydroxy protecting group;R.sup.3 is 1-piperidinyl, 1-pyrrolidino, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino;n is 2 or 3; andZ is --O--or --S--;or a pharmaceutically acceptable salt thereof, and further comprising administering to said woman an effective amount of estrogen.
Abstract: The current invention provides methods for the up-regulation of trkA in a mammal, including humans, comprising the administration of an effective amount of a compound of formula I ##STR1## wherein R.sup.1 and R.sup.3 are, independently, --H, --CH.sub.3, --CO(C.sub.1 -C.sub.6 alkyl), or --COAr, where Ar is optionally substituted phenyl;R.sup.2 is selected from the group consisting of pyrrolidine, piperidine, and hexamethyleneimino; ora pharmaceutically acceptable salt or solvate thereof.In addition, the current invention provides method to increase the effect of NGF (Nerve Growth Factor), NGF-like activities or NGF agonists, whether such is from endogenous or exogenous sources.Further, the current invention provides methods for maintaining the homeostasis and health of the hippocampus, hypothalamus, and cortex, thus maintaining their biological functions.
Type:
Grant
Filed:
September 9, 1998
Date of Patent:
November 23, 1999
Assignee:
Eli Lilly and Company
Inventors:
Henry Uhlman Bryant, Robert Frank Santerre
Abstract: A method of increasing gastroesophageal sphincter competence comprising administering to a human in need of treatment 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 pyrrolidino, hexamethyleneimino, and piperidino; or a pharmaceutically acceptable salt or solvate thereof.
Abstract: A compound of fomula XIV: ##STR1## wherein: R.sup.1a is --H or --OR.sup.7a in which R.sup.7a is a hydoxy protecting group;R.sup.2a is --H, halo, or OR.sup.8a in which R.sup.8a is a hydroxy protecting group; andR.sup.
Type:
Grant
Filed:
June 18, 1998
Date of Patent:
November 16, 1999
Assignee:
Eli Lilly and Company
Inventors:
Alan David Palkowitz, Kenneth Jeff Thrasher
Abstract: A method for alleviating the symptoms of post-menopausal syndrome comprising administering to a woman in need thereof an effective amount of a compound of formula I ##STR1## wherein R.sup.1a is --H or --OR.sup.7a in which R.sup.7a is --H or a hydroxy protecting group;R.sup.2a is --H, halo, or --OR.sup.8a in which R.sup.8a is --H or a hydroxy protecting group;R.sup.3 is 1-piperidinyl, 1-pyrrolidino, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino;n is 2 or 3; andZ is --O-- or --S--;or a pharmaceutically acceptable salt thereof.
Abstract: The present invention provides a compound of formula ##STR1## wherein R.sup.1a is --H or --OR.sup.7a in which R.sup.7a is a hydroxy protecting group;R.sup.2a is --H, halo, or --OR.sup.8a in which R.sup.8a is a hydroxy protecting group;R.sup.6 is --H or a hydroxy protecting group which can be selectively removed;R.sup.11 is non-existent or .dbd.O; andZ is --O-- or --S--;or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
June 18, 1998
Date of Patent:
November 9, 1999
Assignee:
Eli Lilly and Company
Inventors:
Alan David Palkowitz, Kenneth Jeff Thrasher