Glaxo Wellcome Inc.

Novatarg, Inc.

Brad Richard Henke

Francis Xavier Tavares

Timothy Mark Willson

Jeffery Edmond Cobb

Kristjan S Gudmundsson

Marcus Brackeen

Kenneth Batchelor

Robert Anthony Mook

Istvan Kaldor

David Norman Deaton

Jon Loren Collins

Milana Dezube

Elizabeth Ellen Sugg

Grady Evan Boswell

Matthew J Sharp

Christopher Joseph Aquino

Peter W Jeffs

Gavin Charles Hirst

John Mark O'Callaghan

Greg Alan Erickson

Tanya Momtahen

Edward Martin Suh

Jeffrey Edmond Cobb

The present invention provides novel fused bicyclic alkylene linked imidodicarbonimidic diamides. In particular, described herein are N-[2-(indol-3-yl)alkylene]-linked imidodicarbonimidic diamides and N-[2-(pyrrolopyridin-3-yl)alkylene]-linked imidodicarbonimidic diamides (compound of formula (I) or formula (II)), and uses therefor. The compounds of the present invention are believed to be organic cation transporter selective compounds, useful for the treatment of diseases and conditions caused by reduced activity of 5' adenosine monophosphate-activated protein kinase (AMPK).

Fused bicyclic alkylene linked imidodicarbonimidic diamides, methods for synthesis, and uses in therapy

A compound having formula (I), wherein A is selected from the group consisting of: (i) phenyl, wherein said phenyl is optionally substituted by one or more halogen atoms, C,alkyl, C,alkoxy, C,fluoroalkoxy, nitrile, or &mdash;NR,R,where R,and R,are independently hydrogen or C,alkyl; (ii) a 5- or 6-membered hetrocyclic group containing at least one heteroatom selected from oxygen, nitrogen and sulfur; and (iii) a fused bicyclic ring (a), wherein ring C represents a heterocyclic group as defined in point (ii) above, which bicyclic ring is attached to group B via a ring atom of ring C; B is selected from the group consisting of: (iv) C,alkylene; (v) &mdash;MC,alkylene or C,alkyleneMC,alkylene, wherein M is O, S, or &mdash;NR,wherein R,represents hydrogen or C,alkyl; (vi) a 5- or 6-membered heterocyclic group containing at least one nitrogen heteroatom and optionally at least one further heteroatom selected from oxygen, nitrogen and sulfur and optionally substituted by C,alkyl; and (vii) Het-C,alkylene, wherein Het represents a heterocyclic group as defined in point (vi) above; Alk represents C,alkylene; R,represents hydrogen or C,alkyl; Z is selected from the group consisting of: (viii) &mdash;(C,alkylene) phenyl, which phenyl is optionally substituted by one or more halogen atoms; and (ix) &mdash;NR,R,, wherein R,represents hydrogen or C,alkyl, and R,represents &mdash;Y&mdash;(C&boxH;O)&mdash;T&mdash;R,, or &mdash;Y&mdash;(CH(OH))&mdash;T&mdash;R,.

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Cary, NC, United States of America

Brad Richard Henke