Astrazeneca Ab

Astra Pharmaceuticals Limited

Fisons Ltd.

Astra Zeneca U.k. Limited

Anthony Howard Ingall

Simon David Guile

Paul Andrew Willis

Brian Springthorpe

David Hardern

David Cox

Peter A Cage

Martin E Cooper

Nicholas David Kindon

John L Suschitzky

Rukhsana Rasul

David E Hall

Rachel Heulwen Reynolds

Roger Victor Bonnert

Hugh Cairns

John R Bantick

Matthew William Dampier Perry

Hossein A Dowlatshahi

David Hardem

Simon Guile

Triazolo[4,5-d]pyrimidine compounds, their use as medicaments, compositions containing them and processes for their preparation. The compounds of the invention have the formula (I) as follows: wherein R, X and Rthrough Rare as defined in the specification.

Triazolo(4,5-D)pyrimidine compounds

The invention relates to thienopyrimidinediones of formula (I): wherein: Processes for the preparation of compounds of formula (I), pharmaceutical compositions containing them and their use in therapy are also described and claimed.

Thienopyrimidinedinones and their use in modulation of autoimmune disease

The invention relates to a compound of formula (1); wherein: Rand Reach independently represent a Calkyl, Calkenyl, Ccycloalkyl Calkyl or Ccycloalkyl; each of which may be optionally substituted by 1 to 3 halogen atoms; Ris isoxyzolidin-2-ylcarbonyl or tetrahydroisoxazin-2-ylcarbonyl wherein each ring is optionally substituted by one hydroxy group; Q is CO&#x2014; or C(R)(R)-(wherein Ris a hydrogen atom or Calkyl and Ris a hydrogen atom or hydroxy group); Ar is a 5- to 10-membered aromatic ring system wherein up to 4 ring atoms may be heteroatoms independently selected from nitrogen, oxygen and sulphur, the ring system being optionally substituted by one or more substituents as defined in the specification. It also relates to methods of preparing, pharmaceutical compositions containing and methods of using the compound of the formula (1), particularly in the modulation of autoimmune disease 

Thienopyrimidinediones and their use in the modulation of autoimmune disease

The invention relates to a compound of formula (1)(A chemical formula should be inserted here&#x2014;please see paper copy enclosed) wherein Q is &#x2014;CO&#x2014; or &#x2014;C(R)(R)&#x2014; (wherein Ris a hydrogen atom or Calkyl and Ris a hydrogen atom or hydroxy group) and Ar is a 5- to 10-membered aromatic ring system wherein up to 4 ring atoms may be heteroatoms independently selected from nitrogen, oxygen and sulphur, the ring system being optionally substituted by one or more substituents as defined in the specification. It also relates to methods of preparing, pharmaceutical compositions containing and methods of using the compound of the formula (1), particularly in the modulation of autoimmune disease. 

Chemical compounds

The invention provides new triazolo[4,5-d]pyrimidine compounds, their use as medicaments, compositions containing them and processes for their preparation.

Trisubstituted triazolopyrimidines for use in platelet aggregation inhibition

The invention relates to thienopyridazinones of formula (I): wherein: Ris Calkyl, Calkenyl or Ccycloalkyl which is optionally substituted by Calkyl, each of the above being optionally substituted by one or more halogen atoms; Ris Calkyl; Ris a group CO&#x2014;G or SO&#x2014;G where G is a 5- or 6-membered ring containing a nitrogen atom and a second heteroatom selected from oxygen and sulphur adjacent to the nitrogen, and optionally substituted by up to 3 groups selected from hydroxyl and Calkyl; Q is CRRwhere Rand Rare as defined in the specification; and Ris a 5- to 10-membered mono- or bi-cyclic aromatic ring system, containing 0 to 4 heteroatoms independently selected from nitrogen, oxygen and sulphur, the ring system being optionally substituted as described in the specification, and pharmaceutically acceptable salts and solvates thereof. Processes for their preparation, pharmaceutical compositions containing them and their use in therapy, in particular in the modulation of autoimmune disease are also described. 

Compounds

A compound of formulaor a pharmaceutically acceptable salt thereof, wherein R is &#x2014;C(O)Ar, &#x2014;C(R)(R)Aror Ar; Rrepresents a group X&#x2014;Ror Ar; X represents a bond or a group NR; and Rrepresents Calkyl, Calkenyl or Calkynyl, each of which may be optionally substituted by one or more substituents independently selected from carboxyl, hydroxyl, &#x2014;C(O)&#x2014;R, Ccycloalkyl, morpholinyl, &#x2014;NRR, &#x2014;SR, &#x2014;OR, phenyl and halophenyl, or Rrepresents a Ccycloalkylcarbonyl, &#x2014;C(O)CHCN, halophenylcarbonyl or trifluoromethylcarbonyl group. The compounds or compositions thereof are useful in the treatment or prophylaxis of autoimmune, inflammatory, proliferative and hyperproliferative diseases.

Triazolo(4,5-d)pyrimidine compounds

The invention relates to triazolo&lsqb;4,5-d&rsqb;pyrimidin-3-yl derivatives which are useful in the treatment of platelet aggregation disorders.

Triazolo&lsqb;4,5-D&rsqb;pyrimidinyl derivatives and their use as medicaments

Compounds of formula having the following stereochemistry

1,2,3-triazolo&lsqb;4,5-d&rsqb;pyrimidines as P2T receptor antagonists

There are disclosed compounds of formula I, ##STR1## wherein R.sup.1 and R.sup.2 independently represent hydrogen or halogen, R.sup.3 and R.sup.4 independently represent phenyl, or alkyl C.sub.1-6 optionally substituted by one or more substituents selected from OR.sup.5, alkylthio C.sub.1-6, NR.sup.6 R.sup.7, phenyl, COOR.sup.8 and halogen,

N-alkyl-2-substituted ATP analogues for treatment of embolic disease

Inhibitors of platelet aggregation

There are disclosed compounds of formula I, ##STR1## wherein R.sup.1 and R.sup.2 independently represent hydrogen or halogen, R.sup.3 and R.sup.4 independently represent phenyl, or alkyl C.sub.1-6, optionally substituted by one or more substituents selected from OR.sup.5, alkylthio C.sub.1-6, NR.sup.6 R.sup.7, phenyl, COOR.sup.8 and halogen,

N-alkyl-2-substituted ATP analogues and administration to inhibit

There are disclosed compounds of formula I, ##STR1## wherein Q represents CR.sup.1 R.sup.2, R represents O or CR.sup.3 R.sup.4, W represents O or CH.sub.2, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen or halogen, X represents S(O).sub.n R.sup.5, alkyl C.sub.1-6 alkoxy C.sub.1-6, acylamino C.sub.1-6, CONR.sup.6 R.sup.7, NR.sup.8 R.sup.9, halogen, a 5- or 6-membered S containing heterocycle, or phenyl optionally substituted by alkyl C.sub.1-6, n represents 0, 1 or 2, R.sup.5 represents aryl or alkyl C.sub.1-6 optionally substituted by one or more substituents selected from hydroxy, alkoxy C.sub.1-6, halogen and aryl; R.sup.6, R.sup.7, R.sup.8 and R.sup.9 independently represent hydrogen or alkyl C.sub.1-6, Y represents NH.sub.2 or alkoxy C.sub.1-6, and Z represents an acidic moiety, in addition, when R represents CR.sup.3 R.sup.4, then --Q--Z may also represent hydroxy or --OP(O)(OH).sub.2, and pharmaceutically acceptable salts thereof, with certain provisos, for use as pharmaceuticals.

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Loughborough, United Kingdom

Anthony Howard Ingall