Vernalis &r&d) Ltd.

Vernalis Limited

Stephen Stokes

Martin James Drysdale

Paul Webb

Simon Bedford

Andrea Fiumana

Nicolas Foloppe

Christopher John Graham

Stuart Christopher Ray

Emma Jayne Stefaniak

Christoper John Graham

The inventions relates to compounds of (I) and therapeutic uses thereof: (I) The terms Z, Y, and Rare as defined in the claims. 

1H-pyrrolo [2,3-b] pyridine derivatives and their use as kinase inhibitors

A method of treating a mammal suffering from a cancer responsive to inhibition of protein kinase activity, by administering to the mammal an amount of a compound of formula (I), or a pharmaceutically acceptable salt thereof, effective to inhibit protein kinase activity, wherein the compound of formula (I) is: 

Indolyl-pyridone derivatives having checkpoint kinase 1 inhibitory activity

1H-pyrrolo[2,3-B] pyridine derivatives and their use as kinase inhibitors

Compounds of formula (I) have checkpoint kinase 1 (CHK1) inhibitory activity: wherein R, R, Rand Rare independently selected from hydrogen, hydroxy, methyl, trifluoromethyl, hydroxymethyl, methoxy, trifluoromethoxy, methylamino and dimethylamino; R, and Rare independently selected from hydrogen, hydroxy, C-Calkyl, fluoro-(C-C)-alkyl, hydroxy-(C-C)-alkyl, C-Calkoxy, fluoro-(C-C)-alkoxy, hydroxy-(C-C)-alkoxy, &#x2014;N(R)&#x2014;R, -Alk-N(R)&#x2014;R, &#x2014;O-Alk-N(R)&#x2014;R, &#x2014;C(&#x2550;O)OH, carboxy-(C-C)-alkyl, or &#x2014;C(&#x2550;O)&#x2014;NH&#x2014;R; Alk is a straight or branched chain divalent C-Calkylene radical; Rand Rare independently selected from hydrogen, hydroxy, or C-Calkoxy; X is a straight chain divalent C-Calkylene radical, optionally substituted on one or more carbons by Rand/or R; W is selected from &#x2014;C(&#x2550;O)&#x2014;N(&#x2014;R)&#x2014; or &#x2014;N(&#x2014;R)&#x2014;C(&#x2550;O)&#x2014;; Y is hydrogen, C-Calkyl, C-Calkoxy, or halo; and Q is selected from optionally substituted phenyl, optionally substituted cyclohexyl, or an optionally substituted 6-membered monocyclic heteroaryl ring.

Compounds of formula (I) have checkpoint kinase 1 (CHK1) inhibitory activity: wherein R, R, Rand Rare independently selected from hydrogen, hydroxy, methyl, trifluoromethyl, hydroxymethyl, methoxy, trifluoromethoxy, methylamino and dimethylamino; R, and Rare independently selected from hydrogen, hydroxy, C-Calkyl, fluoro-(C-C)-alkyl, hydroxy-(CC)-alkyl, C-Calkoxy, fluoro-(C-C)-alkoxy, hydroxy-(C-C)-alkoxy, -AIk-N(R)&#x2014;R, -0-AIk-N(R)&#x2014;R, &#x2014;C(&#x2550;O)OH, carboxy-(C-C)-alkyl, or &#x2014;C(&#x2550;O)&#x2014;NH&#x2014;R; AIk is a straight or branched chain divalent C-Calkylene radical; Rand Rare independently selected from hydrogen, hydroxy, or C-Calkoxy; X is a straight chain divalent C-Calkylene radical, optionally substituted on one or more carbons by Rand/or R; W is selected from &#x2014;C(&#x2550;O)&#x2014;N(&#x2014;R)&#x2014; or &#x2014;N(&#x2014;R)&#x2014;C(&#x2550;O)&#x2014;; Y is hydrogen, C-Calkyl, C-Calkoxy, or halo; and Q is selected from optionally substituted phenyl, optionally substituted cyclohexyl, or an optionally substituted 6-membered monocyclic heteroaryl ring. 

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Winnersh, United Kingdom

Stephen Stokes