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.

公开(公告)号：DE69533589T2

公开(公告)日：2005-02-10

申请号：DE69533589

申请日：1995-06-22

Applicant: CELLTECH R&D LTD

Inventor： ALEXANDER PETER ,  WARRELLOW JOHN

IPC: C07D213/30 ,  A61K31/44

公开(公告)号：DE69433594T2

公开(公告)日：2004-08-05

申请号：DE69433594

申请日：1994-12-21

Applicant: CELLTECH R&D LTD

Inventor： WARRELLOW JOHN ,  BOYD CAMPBELL ,  ALEXANDER PETER

IPC: A61K31/41 ,  A61K31/44 ,  A61P1/04 ,  A61P11/00 ,  A61P29/00 ,  C07D413/10

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：DE69532808D1

公开(公告)日：2004-05-06

申请号：DE69532808

申请日：1995-06-21

Applicant: CELLTECH R&D LTD

Inventor： WARRELLOW JOHN ,  ALEXANDER PETER

IPC: A61K31/44 ,  A61P11/06 ,  A61P43/00 ,  C07C1/26 ,  C07C1/32 ,  C07C15/02 ,  C07C15/12 ,  C07C17/263 ,  C07C25/02 ,  C07C25/18 ,  C07C43/20 ,  C07C57/30 ,  C07C59/64 ,  C07C237/04 ,  C07C307/04 ,  C07C311/00 ,  C07C323/00 ,  C07C327/00 ,  C07C327/48 ,  C07C335/04 ,  C07D213/30 ,  C07D521/00

Abstract: Tri-substituted phenyl derivatives and processes for their preparation. In a preferred embodiment, the compounds have the general formula (1) wherein L may be -OR; Z may be -C(R3)(R4)-C(R5)(R6)(R7); R may be an optionally substituted cycloalkyl group; R3, R6 and R7 may be hydrogen; R4 may be -(CH2)t-Ar-(L1)n-Ar'; R5 may be -(CH2)tAr; Ar may be a monocyclic or bicyclic aryl or heteroaryl group; L1 may be a divalent linking group; and Ar' is Ar or an Ar containing group. Compounds of the invention may be potent and selective phosphodiesterase type IV inhibitors and are useful in the prophylaxis and treatment of various diseases, such as asthma, which are associated with an unwanted inflammatory response or muscular spasm.