Astrazeneca Ab

Astra Zeneca U.k. Limited

Simon David Guile

Anthony Howard Ingall

Brian Springthorpe

Paul Andrew Willis

David Hardern

Martin E Cooper

Rukhsana Rasul

Barrie Martin

Garry Pairaudeau

Mark Richard Ebden

Toby Thompson

Rachel Heulwen Reynolds

Roger Brown

David Hardem

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 provides a compound of formula (I) as defined in the specification, a process for its preparation, pharmaceutical compositions containing it, a process for preparing the pharmaceutical composition, and its use in therapy.

Quinoline derivatives 057

The invention provides compounds of formula (I), processes for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy, wherein R, R, Rand n are as defined in the specification 

Compounds 679

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 thienopyrimidinediones of formula (1) wherein Rand Reach independently represent a Calkyl, Calkyl, Calkenyl, CcycloalkylCalkyl or Ccycloalkyl; each of which may be optionally substituted by 1 to 3 halogen atoms Ris a group CO-G or SO-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; the ring being substituted by at least one group as defined in the specification, Q is CRRwhere Ris hydrogen, fluorine or Calkyl and Ris hydrogen, fluorine or hydroxy; and Ar is a 5-10-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 groups defined in the specification; as well as pharmaccutically acceptable salts and solvates thereof. Processes for their preparation of the compounds, pharmaceutical compositions containing them and their use in therapy, in particular in immunosuppressive therapy are also described 

Thienopyrimidinediones and their use in the 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 

The invention provides novel substituted cyclopentane compounds (in particular, substituted [1,2,3]triazolo[4,5-d]pyrimidines), their use as medicaments (in particular, their use as anti-thrombotic agents), compositions containing them and processes for their preparation.

Substituted [1,2,3]triazolo[4,5-d]pyrimidines

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

The invention provides novel 1,2,3-triazolo[4,5-d]pyrimidine compounds, such as those represented by formula (I):their use as medicaments, particularly in platelet aggregation disorders, compositions containing them and processes for their preparation.

Cyclopentan-2-ol-1-yl-[1,2,3]triazolo[4,5-D]pyrimidine compounds

The invention provides a compound of formula (I):wherein Ris alkyl Cor alkenyl C, both independently optionally substituted by one or more groups selected from alkyl Cor halogen; Ris cycloalkyl C, optionally substituted by R; Ris phenyl, optionally substituted by one or more groups selected from alkyl Cor halogen; Rand Rare alkyl Cor together cycloalkyl C. These compounds are useful for the treatment of stable and unstable angina.

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Loughborough, United Kingdom

Simon David Guile