Abstract: The present invention relates to sulfonate and carbamate derivatives of 3-aroylbenzo[b]thiophenes, pharmaceutical formulations containing these compounds and methods of using such compounds for inhibiting the loss of bone, lowering serum cholesterol levels and therapeutically treating hormone dependent mammalian breast and uterine carcinoma.
Type:
Grant
Filed:
February 22, 1995
Date of Patent:
November 30, 1999
Assignee:
Eli Lilly and Company
Inventors:
Larry J. Black, Henry U. Bryant, George J. Cullinan
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. The reaction is a very efficient and robust macrocyclization methodology.
Type:
Grant
Filed:
August 22, 1997
Date of Patent:
November 23, 1999
Assignee:
Eli Lilly and Company
Inventors:
Margaret Mary Faul, Leonard Larry Winneroski, Jr.
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 therefore.
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: The invention relates to benzopyranol derivatives which are intermediates in a process for stereoselectively forming N-substituted dihydro-2,3 benzodiazopines which are useful as AMPA receptor antagonists. The process includes an opening reduction step which sets the stereochemistry of the intermediates and the final compounds to the desired enantiomer. The reduction step may be carried out by an enzymatic reduction.
Abstract: A process for preparing 1H-indole-3-glyoxamides useful for inhibiting SPLA.sub.2 and novel intermediates useful in the preparation of such compounds.
Type:
Grant
Filed:
June 26, 1998
Date of Patent:
November 16, 1999
Assignee:
Eli Lilly and Company
Inventors:
Vien Van Khau, Michael John Martinelli, Joseph Matthew Pawlak
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: This invention provides thiomorpholinone compounds useful for treating multiple sclerosis of formula I wherein:R.sup.1 and R.sup.2 are each independently selected from C.sub.1 -C.sub.8 alkyl; C.sub.2 -C.sub.8 alkenyl; C.sub.2 -C.sub.8 alkynyl; C.sub.1 -C.sub.8 alkyloxy; C.sub.1 -C.sub.8 alkylthio; trifluoromethyl; C.sub.1 -C.sub.4 alkyl substituted with phenyl; phenyl; F; Cl; NO.sub.2 ; phenoxy; C.sub.1 -C.sub.4 alkyl substituted with phenoxy; thiophenyl; C.sub.1 -C.sub.4 alkylthiophenyl; --COOR.sup.7 ; --N(R.sup.7).sub.2 or --N(R.sup.7)SO.sub.2 R.sup.7 where each R.sup.7 is independently hydrogen or C.sub.1 -C.sub.6 alkyl;R.sup.3 is H or C.sub.1 -C.sub.4 alkyl;R.sup.4 and R.sup.5 are each individually H, or when taken together form a bond;R.sup.6 is H; C.sub.1 -C.sub.8 alkyl; C.sub.2 -C.sub.8 alkenyl; C.sub.2 -C.sub.8 alkynyl; --SO.sub.2 CH.sub.3 ; --(CH.sub.2).sub.n NR.sup.8 R.sup.9 ; --(CH.sub.2).sub.n CO.sub.2 R.sup.8 ; --(CH.sub.2).sub.n OR.sup.8 where n is an integer from 1 to 6, both inclusive, and R.
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
Abstract: The invention provides benzothiophene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, cardiovascular-related pathological conditions, including hyperlipidemia.
Type:
Grant
Filed:
September 22, 1997
Date of Patent:
November 9, 1999
Assignee:
Eli Lilly and Company
Inventors:
Henry Uhlman Bryant, George Joseph Cullinan, Jeffrey Alan Dodge
Abstract: The invention provides a compound of formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical formulations containing a compound of formula I, and methods of using a compound of formula I for the inhibition of bone loss or bone resorption and for treatment of cardiovascular-related pathological conditions.
Abstract: There is disclosed a method of treating atherosclerosis, of preventing atherosclerotic lesions and plaque formation, of inhibiting atherogenesis, and of decreasing intracellular cholesterol accumulation through the administration of an effective amount of moxonodine, or a pharmaceutically acceptable salt thereof.
Abstract: This invention provides novel fungal strains altered in IPC synthase production, and a method for screening for inhibitors of fungal IPC synthase using whole cells.
Type:
Grant
Filed:
April 9, 1997
Date of Patent:
November 2, 1999
Assignee:
Eli Lilly and Company
Inventors:
Steven Alan Heidler, Jeffrey Alan Radding, Debra Ann Young
Abstract: The present invention provides novel complexes consisting of certain GLP-1 molecules associated with a divalent metal cation that is capable of co-precipitating with a GLP-1 molecule. Pharmaceutical compositions and methods of using such complexes for enhancing the expression of insulin in B-type islet cells is claimed, as is a method for treating maturity onset diabetes mellitus in mammals, particularly humans.