Baylor University

Oxigene, Inc.

Merck Patent Gmbh

Sepracor, Inc.

James Michael Dorsey

Kevin G Pinney

Zhi Chen

Vani P Mocharla

David J Chaplin

Robert J Foglesong

Klaus Edvardsen

Joseph Anthony Prezioso

Charles M Garner

Mallinath Hadimani

Brian Lewis Hodous

Qun Kevin Fang

Nadia Brugger

Kerry Leigh Spear

Theresa L Johnson

Michele L R Heffernan

Seth C Hopkins

Thomas E Richardson

Cyprian Okwara Ogbu

Justin Potnick

Amanda E Sutton

Mustapha Soukri

Maria Graciela Miranda

Raymond Kessler

Usha Ghatak, Legal Representative

Usha R Ghatak, Legal Representative

Thomas Francis Nelson Haxell

Jimmy Kessler

Anjan Ghatak

Robert James Foglesong

The present invention relates to novel spiro-quinazolinone derivatives as positive allosteric modulators for modulating metabotropic glutamate receptor subtype 4 (mGluR4) and/or altering glutamate level or glutamatergic signalling.

Spiro-quinazolinone derivatives and their use as positive allosteric modulators of mGluR4

A serotonin reuptake inhibitor which can be used in the treatment of depression and which has a decreased occurrence of unwanted side effects. The serotonin reuptake inhibitors are bi-functional organic molecules which combine serotonin transporter reuptake inhibition with serotonin (5-HT, such as 5-HT2A) receptor antagonism in one molecular entity. The serotonin-selective reuptake inhibitor (SSRI) homologue portion of the molecule shows an affinity to the serotonin reuptake transporter (SERT) and has antidepressant properties. The piperazine or piperidine portion of the molecule demonstrates an affinity to 5-HT receptors and restores the undesired side effects of SSRIs.

Serotonin reuptake inhibitors

This invention provides fused heterocycles having the formula: in which Ris a member selected from the group consisting of H, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. Ris a member selected from the group consisting of H substituted or unsubstituted alkenyl, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. Ris a member selected from the group consisting of H, C-Csubstituted or unsubstituted alkyl, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. Ris a member selected from OH and OX, in which Xis positive ion which is a member selected from organic positive ions and inorganic positive ions. Substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl moieties have the formula: in which Ar is a member selected from the group consisting of substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl. The index n is an integer from 1 to 4.

Fused heterocycles

A diverse set of tubulin binding agents have been discovered which are structurally characterized, in a general sense, by a semi-rigid molecular framework capable of maintaining aryl-aryl, pseudo pi stacking distances appropriate for molecular recognition of tubulin. In phenolic or amino form, these ligands may be further functionalized to prepare phosphate esters, phosphate salts, phosphoramidates, and other prodrugs capable of demonstrating selective targeting and destruction of tumor cell vasculature.

Tubulin binding ligands and corresponding prodrug constructs

Tubulin binding agents and corresponding prodrug constructs

A diverse set of tubulin binding ligands have been discovered which are structurally characterized, in a general sense, by a semi-rigid molecular framework capable of maintaining aryl&mdash;aryl, pseudo pi stacking distances appropriate for molecular recognition of tubulin. In phenolic or amino form, these ligands may be further functionalized to prepare phosphate esters, phosphate salts, and phosphoramidates capable of demonstrating selective targeting and destruction of tumor cell vasculature.

Growing community of inventors

Durham, NC, United States of America

James Michael Dorsey