Astrazeneca Ab

Astra Zeneca U.k. Limited

Brian Springthorpe

Hitesh Jayantilal Sanganee

Matthew Wd Perry

Paul Andrew Willis

Simon David Guile

Anthony Howard Ingall

Aaron Rigby

David Hardern

Louise Lawrence

Richard Evans

Stephen Thom

Thomas McInally

Garry Pairaudeau

Christopher Luckhurst

Roger Brown

Roger Victor Bonnert

Mark Furber

Stephen Brough

Lilian Alcaraz

Andrew Baxter

Mark Purdie

Moya Caffrey

Tobias Mochel

David O'Sullivan

Talbir Austin

Nicholas Kindor

David Harden

David Marriott

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 present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) mediated disease state.

Piperidine derivatives

The invention provides compounds of formula (I): wherein: X is CH, O, S(O)or NR; Y is a bond, CH, NR, CHNH, CHNHC(O), CH(OH), CH(NHCOR), CH(NHSOR), CHO or CHS; Z is C(O), or when Y is a bond Z can also be S(O); Ris optionally substituted aryl, optionally substituted heterocyclyl or Ccycloalkyl fused to a benzene ring; and R, R, R, R, R, Rand R, R, R, R, R, Rand Rare as defined herein; are modulators of chemokine (especially CCR3) activity (for use in, for example, treating asthma). The invention also provides a process for making 4-(3,4-dichlorophenoxy)piperidine, which is useful as an intermediate for making certain compounds of the invention.

Chemical compounds

The present invention provides a compound of formula (I), wherein: Z is (A) OR (B) and wherein the remaining variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of achemokine (such as CCR3) or H1 mediated disease state. 

Piperidine derivatives useful as modulators of chemokine receptor activity

The present invention relates to compounds of formula (I): The variables recited in formula (I) are defined in the specification. The present invention also relates to processes of preparing compounds of formula (I) and uses of such compounds for treating a chemokine (e.g., CCR3) or H1 mediated disease state.

The present invention provides a compound of formula (I), wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) or H1 mediated disease state. 

The invention concerns compounds of formula (I), and their use in therapy, particularly in the modulation of CCR3 activity.

The invention provides a compound of formula (I), wherein: T is C(O) or S(O); W is C(O) or S(O); X is CH, O or NH; Y is CRor N; Ris optionally substituted aryl or optionally substituted heterocyclyl; Ris hydrogen or Calkyl; Ris hydrogen or optionally substituted Calkyl; and Ris alkyl, optionally substituted aryl, optionally substituted aralkyl or optionally substituted heterocyclyl; that are modulators of chemokine (especially CCR3) activity and are especially useful for treating asthma and/or rhinitis 

The invention provides compounds of formula (I): as modulators of chemokine and H1 receptor activity. The compounds are especially useful in the treatment of asthma and rhinitis.

The invention provides compounds of formula (I) wherein: T is C(O) or S(O); W is C(O) or S(O); X is CH, O or NH; Y is CRor N; n is 0, 1 or 2; m is 1 or, when Y is CRm is 0; Ris optionally substituted aryl or optionally substituted heterocyclyl; R, R, R,, R, R, Rand Rare, independently, hydrogen or C?1-6#191 alkyl; Ris hydrogen or C-Calkyl; Ris alkyl, optionally substituted aryl, optionally substituted aralkyl or optionally substituted heterocyclyl; and Ris hydrogen or C-Callkyl; that are modulators of chemokine (especially CCR3) activity and are especially useful for treating asthma and/or rhinitis.

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 present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) or H1 mediated disease state.

The invention provides a compound of formula (I): T is C(O) or S(O); W is CH, (CH), CH(CH), CH(CH)O or cyclopropyl; X is O, CH, C(O), S, S(O), S(O)or NR; m is 0 or 1; Ris optionally substituted aryl or optionally substituted heterocyclyl; Ris alkyl (optionally substituted by OH), cycloalkyl, optionally substituted aryl or optionally substituted heterocyclyl; that are modulators of chemokine (especially CCR3) activity and are especially useful for treating asthma and/or rhinitis.

Piperidine derivatives and their use as modulators of chemokine (especially CCR3) activity

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.

Growing community of inventors

Loughborough, United Kingdom

Brian Springthorpe