Eli Lilly and Company

Oregon State University

Eli Lilly Company

David T Wong

David W Robertson

Joseph H Krushinski, Jr

Juan I Oguiza

Dennis C Thompson

John M Schaus

James E Audia

Vincent Patrick Rocco

Kurt Rasmussen

Jeffrey S Nissen

Thomas Edward Mabry

Edward E Beedle

David J Hibschman

Yao-Chang Xu

William B Lacefield

David Edward Tupper

Terrence M Hotten

Larry W Hertel

Daniel Timothy Kohlman

Sidney Xi Liang

William J Wheeler

Gregory Alan Stephenson

Donald R Gehlert

John Fairhurst

Mark M Foreman

James David White

David Mitchell

Ray W Fuller

Clint Duane Walker

Jongtae Yang

Edward Louis Mattiuz

Arthur Cherkin

James F Flood

David B Chan

Juan Ignacio Oguiza

Rajan Juniku

John-Michael Sauer

Lei Zhang

Hui Zhou

Hua Xiao

The present disclosure concerns a compound, or a pharmaceutically acceptable salt thereof, having a formula: where at least one of R-Ris a heterocycle, at least one of R-Ris an aryl group coupled to the ring by a linker atom, functional group, or other moiety, or where none of R-Ris an amide, and any and all combinations thereof. Remaining R-Rsubstituents independently are aliphatic, substituted aliphatic, amine, substituted amine, aryl, substituted aryl, cyclic, substituted cyclic, halide, heteroaryl, substituted heteroaryl, heterocyclic, substituted heterocyclic, hydrogen or hydroxyl. A method for treating a subject also is provided comprising administering a disclosed compound or compounds, or a prodrug that is converted into the disclosed compound or compounds, or a composition comprising the compound, compounds, or prodrugs thereof, to a subject. A method for making disclosed compounds also is provided.

Inhibitor(s) of transporters or uptake of monoaminergic neurotransmitters

The present invention provides compounds and methods for the inhibition of monoamine uptake in mammals.

Inhibitor of monoamine uptake

Piperidine derivatives having effects on serotonin related systems

Arylpiperazines as serotonin reuptake inhibitors and 5-HT1D&agr; antagonists

A series of hetero-oxy alkanamines are effective pharmaceuticals for the treatment of conditions related to or affected by the reuptake of serotonin and by the serotonin 1,receptor. The compounds are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal, and for the treatment of depression and other conditions for which serotonin reuptake inhibitors are used.

Compounds having effects on serotonin-related systems

The power of citalopram, fluvoxamine and paroxetine to increase the availability of sarotonin, norepinephrine and dopamine, particularly serotonin, is augmented by administration in combination with a drug which is a serotonin 1A receptor antagonist.

Potentiation of drug response

Pharmaceutical compounds of the formula ##STR1## in which R.sup.1 is hydrogen or halo, and R.sup.2 is C.sub.1-10 alkyl, C.sub.2-10 alkenyl, C.sub.2-10 alkynyl, C.sub.3-6 cycloalkyl optionally substituted by 1 to 3 C.sub.1-4 alkyl groups, C.sub.3-6 cycloalkyl-C.sub.1-4 alkyl in which the cycloalkyl group is optionally substituted by 1 to 3 C.sub.1-4 alkyl groups, or optionally substituted phenyl-C.sub.1-4 alkyl; or a salt thereof. Such compounds are useful for treating a disorder of the central nervous system which is associated with the modulation of a 5-HT.sub.3 receptor.

Thienobenzodiazepine compounds

Potentiation of serotonin response

A series of hetero-oxy alkanamines are effective pharmaceuticals for the treatment of conditions related to or affected by the reuptake of serotonin and by the serotonin 1.sub.A receptor. The compounds are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal, and for the treatment of depression and other conditions for which serotonin reuptake inhibitors are used.

This invention provides a method of selectively antagonizing-the 5-HT.sub.1A receptor in mammals by administering aryloxypropanolamines. Aryloxypropanolamines are also claimed.

Use of propanolamine derivatives as selective 5-HT.sub.1 antagonists

The power of fluoxetine, venlafaxine, milnacipran and duloxetine to increase the availability of serotonin, norepinephrine and dopamine, particularly serotonin, is augmented by administration in combination with a drug which is a serotonin 1A receptor antagonist.

Growing community of inventors

Indianapolis, IN, United States of America

David T Wong