Merck Sharp + Dohme Corp.

Oxford University Innovation Ltd

Other

Merck + Co., Inc.

Merck Sharpe & Dohme Corp.

David James Hallett

Leslie Joseph Street

Simon Charles Goodacre

Michael Geoffrey Neil Russell

Mark Stewart Chambers

Richard Thomas Lewis

Philip Jones

Wesley Peter Blackaby

Andrew S Jennings

Craig William Lindsley

William Robert Carling

Kevin William Moore

Jose Luis Castro Pineiro

Scott E Wolkenberg

Robert James Maxey

Edward Cochrane

Brett Stevenson

Tim Sparey

Andrew Ratcliffe

Alexandre Froidbise

Michael Rowley

Kevin John Merchant

Zhijian Zhao

Helen Jane Szekeres

Alexander Charles Humphries

Michela Bettati

Michael Reader

Gilbert Lassalle

George D Hartman

Mark E Duggan

Timothy Harrison

Angus Murray MacLeod

Ian James Collins

Kevin J Wilson

Andrew Pate Owens

Martin Richard Teall

Cory R Theberge

William D Shipe

Peter Blurton

Linda Elizabeth Keown

Elizabeth Mary Naylor

M Brad Nolt

David Wisnoski

Franz Lagasse

James Michael Crawforth

Sarah Margaret Kelly

Yi Wang

Monique Bodil Van Neil

William H Leister

Leslie Jospeh Street

Elizabeth M Naylor

This invention relates to compounds that are useful as cancer therapies. The compounds comprise azithromycin derivatives having a phosphonium cation tethered to the azithromycin macrocycle. The invention also relates to methods of using said compounds and to pharmaceutical formulations comprising said compounds.

Azithromycin derivatives containing a phosphonium ion as anticancer agents

This invention relates to compounds that are useful as cancer therapies. The compounds comprise derivatives of tetracycline antibiotics, e.g. doxycycline, having a phosphonium cation tethered to the tetracycline tetracycle. The invention also relates to methods of using said compounds and to pharmaceutical formulations comprising said compounds.

Phosphonium-ion tethered tetracycline drugs for treatment of cancer

Triphenylphosphonium-tethered tetracyclines for use in treating cancer

The present invention is directed to quinolone compounds of general formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, pain or sleep disorders, and to novel M1 receptor positive allosteric modulator compounds of formulae (II) to (VIII). The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases in which the M1 receptor is involved.

Quinolone M1 receptor positive allosteric modulators

The present invention is directed to piperidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neurotransmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.

Piperidine glycine transporter inhibitors

The present invention is directed to pyridyl, pyridazinyl, pyrimidinyl and pyrazinyl piperidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neurotransmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.

Heteroaryl piperidine glycine transporter inhibitors

The present invention is directed to azetidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neurotransmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.

Azetidine glycine transporter inhibitors

The present invention discloses a compound of formula I, or a pharmaceutically acceptable salt thereof: (I) wherein &#x2014;U&#x2014;V&#x2014; represents &#x2014;CH&#x2550;CH&#x2014;, or &#x2014;CH&#x2014;CH&#x2014;, &#x2014;N&#x2550;CH&#x2014; or &#x2014;CH&#x2550;N&#x2014;; Xrepresents hydrogen, halogen, Calkyl, trifluoromethyl or Calkoxy; Xrepresents hydrogen or halogen; Y represents a chemical bond, an oxygen atom, or a &#x2014;NH&#x2014; or &#x2014;OCH&#x2014; linkage; Z represents an optionally substituted aryl or heteroaryl group; Rrepresents hydrocarbon, a heterocyclic group, trifluoromethyl, &#x2014;SOR, &#x2014;SONRR, &#x2014;COR, &#x2014;CORor &#x2014;CONRR; and Rand Rindependently represent hydrogen, hydrocarbon or a heterocyclic group; pharmaceutical compositions comprising it; its use in methods of treatment; use of it in the manufacture of a medicament for treating and/or preventing anxiety; convulsions or a cognitive disorder; and methods of treatment using it. 

Imidazopyrazinones as GABA-A receptor anxiolytics

A class of 8-fluoro-3-phenylimidazo[1,2-&#x3b1;]pyridine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group, or by a pyrrolidinonyl group, which is directly attached or bridged by an oxygen atom or by a &#x2014;NH&#x2014; or &#x2014;OCH&#x2014; linkage, being selective ligands for GABAreceptors, in particular having high affinity for the &#x3b1;2 and/or &#x3b1;3 and/or &#x3b1;5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.

Imidazo-pyridine derivatives as ligands for GABA receptors

A class of 8-fluoroimidazo[1,2-&#x3b1;]pyridine derivatives, substituted at the 3-position by an optionally substituted five-membered or six-membered heteroaromatic ring, being selective ligands for GABAreceptors, in particular having high affinity for the &#x3b1;2 and/or &#x3b1;3 and/or &#x3b1;5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.

8-fluoroimidazo 1,2-a pyridine derivatives as ligands for GABA receptors

The present invention provides a compound of formula I: wherein

Imidazo[1,2-b]pyridazine analogues as anxiolytics and cognition enhancers

A class of imidazo[1,2][1,2,4]triazine derivatives, substituted at the 7-position by an optionally substituted five-membered or six-membered heteroaromatic ring, being selective ligands for GABAreceptors, in particular having good affinity for the &#x3b1;2 and/or &#x3b1;3 and/or &#x3b1;5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.

Imidazo-triazine derivatives as ligands for gaba receptors

The present invention discloses a compound of formula 1, or a pharmaceutically acceptable salt thereof: wherein Xrepresents hydrogen, halogen, Calkyl, trifluoromethyl or Calkoxy; Xrepresents hydrogen or halogen; Y represents a chemical bond, an oxygen atom, or a &#x2014;NH&#x2014; linkage; Z represents an optionally substituted aryl or heteroaryl group; Rrepresents hydrogen, hydrocarbon, a heterocyclic group, halogen, cyano, trifluoromethyl, nitro, &#x2014;OR, &#x2014;SR, &#x2014;SOR, &#x2014;SOR, &#x2014;SONRR, NRR, &#x2014;NRCOR, &#x2014;NRCOR, &#x2014;COR, &#x2014;COR, &#x2014;CONRRor &#x2014;CR&&#x2550;NOR; and Ra and Rb independently represent hydrogen, hydrocarbon or a heterocyclic group; a pharmaceutical composition comprising it; its use in a method of treatment; use of it to manufacture a medicament; and a method of using it to prevent or treat anxiety, convulsions or cognitive disorders. 

[object Object]

A class of imidazo[1,2-&#x3b1;]pyrimidine derivatives, substituted at the 3-position by an optionally substituted five-membered or six-membered heteroaromatic ring, are selective ligands for GABAreceptors, in particular having good affinity for the &#x3b1;2 and/or &#x3b1;3 and/or &#x3b1;5 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.

Imidazo-pyrimidine derivatives as ligands for GABA receptors

A class of 7-phenylimidazo[1,2-b][1,2,4]triazine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a &#x2014;NH&#x2014; linkage, and substituted on the phenyl ring by one or two further substituents as defined herein, being selective ligands for GABAreceptors, in particular having good affinity for the &#x3b1;2 and/or &#x3b1;3 and/or &#x3b1;5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.

Growing community of inventors

Watford, United Kingdom

David James Hallett