Vernalis &r&d) Ltd.

Vernalis Limited

Ian Yule

Allan Michael Jordan

Simon Bedford

Klenke Burkhard

Karine Poullennec

Allan Jordan

Karinne Poullennec

Compounds of formula (I) are Areceptor antagonists: Wherein Ris optionally substituted aryl or an optionally substituted 5- or 6-membered heteroaryl ring; Rand Rare independently selected from hydrogen, C-Calkyl, C-Ccycloalkyl, C-Ccycloalkyl-(C-C)-alkyl, aryl-(C-C)-alkyl optionally substituted in the ring part thereof, a 5- or 6-membered monocyclic heterocyclic group optionally linked via a C-Calkylene chain and optionally substituted in the ring part thereof, benzimidazol-2-yl-methyl, pyrid-3-yl-carbonyl, or (1-methyl-piperidin-4-yl)-carbonyl-methyl; or Rand Rtaken together with the nitrogen atom to which they are attached form an optionally substituted 5- or 6-membered ring; Ris C-Calkyl, C-Calkenyl, &#x2014;N(&#x2014;R)&#x2014;R, or optionally substituted heteroarylmethylamino; and Rand Rare independently selected from hydrogen or C-Calkyl; or Rand Rtaken together with the nitrogen atom to which they are attached form an optionally substituted 4- to 6-membered saturated ring.

Thienopyrimidine compounds

Compounds of formula (I) are Areceptor antagonists:  Wherein Ris optionally substituted aryl or an optionally substituted 5- or 6-membered heteroaryl ring; Rand Rare independently selected from hydrogen, C-Calkyl, C-Ccycloalkyl, C-Ccycloalkyl-(C-C)-alkyl, aryl-(C-C)-alkyl optionally substituted in the ring part thereof, a 5- or 6-membered monocyclic heterocyclic group optionally linked via a C-Calkylene chain and optionally substituted in the ring part thereof, benzimidazol-2-yl-methyl, pyrid-3-yl-carbonyl, or (1-methyl-piperidin-4-yl)-carbonyl-methyl; or Rand Rtaken together with the nitrogen atom to which they are attached form an optionally substituted 5- or 6-membered ring; Ris C-Calkyl, C-Calkenyl, &#x2014;(&#x2014;R)&#x2014;R, or optionally substituted heteroarylmethylamino; and Rand Rare independently selected from hydrogen or C-Calkyl; or Rand Rtaken together with the nitrogen atom to which they are attached form an optionally substituted 4- to 6-membered saturated ring.

Compounds of formula (I) are Areceptor antagonists, wherein Ris optionally substituted aryl or an optionally substituted 5- or 6-membered heteroaryl ring; Rand Rare independently selected from hydrogen, C-Calkyl, C-Ccycloalkyl, C-Ccycloalkyl-(C-C)-alkyl, aryl-(C-C)-alkyl optionally substituted in the ring part thereof, a 5- or 6-membered monocyclic heterocyclic group optionally linked via a C-Calkylene chain and optionally substituted in the ring part thereof, benzimidazol-2-yl-methyl, pyrid-3-yl-carbonyl, or (1-methyl-piperidin-4-yl)-carbonyl-methyl; or Rand Rtaken together with the nitrogen atom to which they are attached form an optionally substituted 5- or 6-membered ring; Ris C-Calkyl, C-Calkenyl, &#x2014;N(&#x2014;R)&#x2014;R, or optionally substituted heteroarylmethylamino; and Rand Rare independently selected from hydrogen or C-Calkyl; or Rand Rtaken together with the nitrogen atom to which they are attached form an optionally substituted 4- to 6-membered saturated ring. 

Compounds of formula (I) are Awherein R1 and R2 are independently selected from hydrogen, or optionally substituted CrC6 alkyl, C-Calkoxy-(C-C)-alkyl, C-Ccycloalkyl, aryl, heteroaryl, aryl-(C-C)-alkyl, or heteroaryl-(C-C)-alkyl; or Rand Rtaken together with the nitrogen atom to which they are attached form an optionally substituted 5- or 6-membered ring; Rand Rare independently selected from hydrogen, or optionally substituted C-Calkyl, C-Calkoxy-(C-C)-alkyl, C-Ccycloalkyl, aryl, heteroaryl, aryl-(C-C)-alkyl, or heteroaryl-C-C)-alkyl; or Rand Rtaken together with the nitrogen atom to which they are attached form an optionally substituted 5- or 6-membered ring; Rand Rare independently selected from hydrogen, C-Calkyl, aryl, aryl-(C-C)-alkyl, &#x2014;NHR&#x2014;N(&#x2014;R)&#x2014;R, &#x2014;NH&#x2014;(C&#x2550;O)&#x2014;R, &#x2014;(C&#x2550;O)&#x2014;NH&#x2014;R, &#x2014;(C&#x2550;O)&#x2014;O&#x2014;R, or halo; and R, R, R, R, R, and Rare independently selected from C-Calkyl, aryl, aryl-(C-C)-alkyl and heteroaryl. 

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Winnersh, United Kingdom

Ian Yule