公开(公告)号：DE60011940D1

公开(公告)日：2004-08-05

申请号：DE60011940

申请日：2000-12-22

Applicant: CELLTECH R&D LTD

Inventor： LANGHAM JOHN ,  ALEXANDER PETER ,  HEAD CLIFFORD ,  LINSLEY MARSHA ,  PORTER ROBERT ,  ARCHIBALD CATHERINE ,  WARRELLOW JOHN

IPC: C07C229/34 ,  C07C229/36 ,  C07D471/04 ,  C07C225/20 ,  C07C229/46 ,  C07D295/12 ,  A61K31/13 ,  A61K31/435 ,  A61P29/00

Abstract: Squaric acid derivatives of formula (1) are described:whereinR1 is a group Ar1Ar2Alk- in whichAr1 is an optionally substituted aromatic or heteroaromatic group;Ar2 is an optionally substituted phenylene or nitrogen-containing six-membered heteroarylene group; and Alk is a chain-CH2-CH(R)-, -CH=C(R)-,in which R is a carboxylic acid (-CO2H) or a derivative or biostere thereof;R2 is a hydrogen atom or a C1-6 alkyl group;L1 is a covalent bond or a linker atom or group;n is zero or the integer 1;Alk1 is an optionally substituted aliphatic chain;R3 is a hydrogen atom or an optionally substituted heteroaliphatic, cycloaliphatic, heterocycloaliphatic, polycycloaliphatic, heteropolycycloaliphatic, aromatic or heteroaromatic group: and the salts, solvates, hydrates and N-oxides thereof.The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders, or disorders involving the inappropriate growth or migration of cells.

公开(公告)号：DE60011940T2

公开(公告)日：2005-07-21

申请号：DE60011940

申请日：2000-12-22

Applicant: CELLTECH R&D LTD

Inventor： LANGHAM JOHN ,  ALEXANDER PETER ,  HEAD CLIFFORD ,  LINSLEY MARSHA ,  PORTER ROBERT ,  ARCHIBALD CATHERINE ,  WARRELLOW JOHN

IPC: C07C229/34 ,  C07C229/36 ,  C07D471/04 ,  C07C225/20 ,  C07C229/46 ,  C07D295/12 ,  A61K31/13 ,  A61K31/435 ,  A61P29/00

Abstract: Squaric acid derivatives of formula (1) are described:whereinR1 is a group Ar1Ar2Alk- in whichAr1 is an optionally substituted aromatic or heteroaromatic group;Ar2 is an optionally substituted phenylene or nitrogen-containing six-membered heteroarylene group; and Alk is a chain-CH2-CH(R)-, -CH=C(R)-,in which R is a carboxylic acid (-CO2H) or a derivative or biostere thereof;R2 is a hydrogen atom or a C1-6 alkyl group;L1 is a covalent bond or a linker atom or group;n is zero or the integer 1;Alk1 is an optionally substituted aliphatic chain;R3 is a hydrogen atom or an optionally substituted heteroaliphatic, cycloaliphatic, heterocycloaliphatic, polycycloaliphatic, heteropolycycloaliphatic, aromatic or heteroaromatic group: and the salts, solvates, hydrates and N-oxides thereof.The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders, or disorders involving the inappropriate growth or migration of cells.