Abstract: A method of inhibiting one or more CNS disorders in a post-menopausal woman comprising administering to a female human in need of treatment an effective amount of a compound having the formula
wherein R1 and R3 are independently hydrogen,
wherein Ar is optionally substituted phenyl;
R2 is selected from the group consisting of pyrrolidine, hexamethyleneamino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.
Type:
Grant
Filed:
December 21, 1993
Date of Patent:
July 9, 2002
Assignee:
Eli Lilly and Company
Inventors:
Henry U. Bryant, Andrew L. Glasebrook, Timothy A. Grese, David L. Phillips
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:
Abstract: The present invention provides method of treating endometriosis using novel benzothiophene compounds of formula I
wherein
R is —H, —OH, —O(C1-C4 alkyl), —O—CO—(C1-C6 alkyl), —O—CO—Ar in which Ar is optionally substituted phenyl, or —O—SO2—(C4-C6 alkyl);
R1 is —H, —OH, —O(C1-C4 alkyl),, —O—CO—(C1-C6 alkyl), —O—CO—Ar in which Ar is optionally substituted phenyl, —O—SO2—(C4-C6 alkyl) chloro or bromo;
R2 is —H or —OH;
n is 2 or 3; and
R3 and R4 each are independently C1-C4 alkyl, or combine to form 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, or 1-hexamethyleneimino;
or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
April 19, 1995
Date of Patent:
June 4, 2002
Assignee:
Eli Lilly and Company
Inventors:
Henry U. Bryant, George J. Cullinan, Jeffrey A. Dodge, Kennan J. Fahey, Charles D. Jones
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:
Abstract: The present invention provides a compound of formula I
wherein
R1 is H, OH, halo, OCO(C1-C6 alkyl), OCO(aryl), OSO2(C4-C6 alkyl), OCOO(C1-C6 alkyl), OCOO(aryl), OCONH(C1-C6 alkyl), or OCON(C1-C6 alkyl)2;
R2 is aryl, C1-C6 alkyl, C3-C6 cycloalkyl, or 4-cyclohexanol;
R3 is O(CH2)2 or O(CH2)3;
R4 and R5 are optionally CO(CH2)3, CO(CH2)4, C1-C6 alkyl, or R4 and R5 combine to form, with the nitrogen to which they are attached, piperidine, morpholine, pyrrolidine, 3-methylpyrrolidine, 3,3-dimethylpyrrolidine, 3,4-dimethylpyrrolidine, azepine, or pipecoline;
R6 is
and pharmaceutically acceptable salts thereof; useful in treating estrogen deficient pathology.
Abstract: The present invention provides a compound of formula I
wherein
R1 is H, OH, halo, OCO(C1-C6 alkyl), OCO(aryl), OSO2(C4-C6 alkyl), OCOO(C1-C6 alkyl), OCOO(aryl), OCONH(C1-C6 alkyl), or OCON(C1-C6 alkyl)2;
R2 is aryl, C1-C6 alkyl, C3-C6 cycloalkyl, or 4-cyclohexanol;
R3 is O(CH2)2 or O(CH2)3;
R4 and R5 are optionally CO(CH2)2CH3, CO(CH2)3CH3, C1-C6 alkyl, or R4 and R5 combine to form, with the nitrogen to which they are attached, piperidine, morpholine, pyrrolidine, 3-methylpyrrolidine, 3,3-dimethylpyrrolidine, 3,4-dimethylpyrrolidine, azepine, or pipecoline;
and pharmaceutically acceptable salts thereof.
The invention further provides pharmaceutical compositions containing compounds of formula I and methods of use for the compounds of formula I.
Abstract: This invention relates to the fields of pharmaceutical and organic chemistry and provides novel 1-benzyl-naphthyls which are &agr;-substituted with ether, thioether amino, cyano or halo that are useful for the treatment of the various medical indications associated with post-menopausal syndrome, as well as estrogen dependent diseases including cancer of the breast, uterus and cervix. The present invention further relates to intermediate compounds and processes useful for preparing the pharmaceutically active compounds of the present invention, and pharmaceutical compositions.
Abstract: The current invention relates to a method for decreasing levels of homocysteine and/or C-reactive protein in humans comprising administering to a mammal in need thereof an effective amount of a compound of formula I:
or a pharmaceutical salt or solvate thereof.
Abstract: A method of preventing breast cancer comprising administering for a sufficient term to a human in need thereof an effective amount of a compound having the formula
and pharmaceutically acceptable salts and solvates thereof.
Type:
Grant
Filed:
August 5, 1999
Date of Patent:
October 16, 2001
Assignee:
Eli Lilly and Company
Inventors:
Fredric J Cohen, Robert S Eckert, Joan E Glusman, Ronald K Knickerbocker, Nikolaus T Nickelsen, Teri J Scott
Abstract: A method of inhibiting ulcerative mucositis comprising administering to a human in need thereof an effective amount of a compound having the formula
wherein R1 and R3 are independently hydrogen,
wherein Ar is optionally substituted phenyl;
R2 is selected from the group consisting of pyrrolidine, hexamethyleneamino, and piperidino; or a pharmaceutically acceptable salt of 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: 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: A method of inhibiting detrimental side-effects of GnRH or GnRH agonist administration in a mammal which comprises the administration to a mannal 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.3 is selected from the group consisting of pyrrolidine, piperidine, and hexamethyleneimino; ora pharmaceutically acceptable salt or solvate thereof.
Type:
Grant
Filed:
August 14, 1998
Date of Patent:
August 1, 2000
Assignee:
Eli Lilly and Company
Inventors:
Henry Uhlman Bryant, George Joseph Cullinan, Jeffrey Alan Dodge
Abstract: This invention provides novel benzothiophene compounds of the formula I: ##STR1## which are useful for the treatment of the various medical conditions associated with postmenopausal syndrome, as well as estrogen dependent diseases including cancer of the breast, uterus, and cervix. The present invention further relates to pharmaceutical formulations of compounds of formula I.
Type:
Grant
Filed:
August 4, 1998
Date of Patent:
July 18, 2000
Assignee:
Eli Lilly and Company
Inventors:
Henry Uhlman Bryant, Jeffrey Alan Dodge
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: This invention provides novel bis-indolemaleimide macrocycle derivatives of the formula: ##STR1## wherein R.sub.1, R.sub.2, X, W, and Y are as defined in the specification. The invention further provides the preparation, pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals.
Type:
Grant
Filed:
November 14, 1997
Date of Patent:
May 2, 2000
Assignee:
Eli Lilly and Company
Inventors:
William F. Heath, Jr., Michael R. Jirousek, John H. McDonald, III, Christopher J. Rito