公开(公告)号：DE60130910T2

公开(公告)日：2008-07-10

申请号：DE60130910

申请日：2001-04-12

Applicant: UCB PHARMA SA

Inventor： NORMAN TIMOTHY JOHN ,  PORTER JOHN ROBERT ,  HUTCHINSON BRIAN ,  RATCLIFFE ANDREW ,  HEAD JOHN CLIFFORD ,  ALEXANDER RIKKI ,  LANGHAM BARRY JOHN ,  WARRELLOW GRAHAM JOHN ,  ARCHIBALD SARAH ,  LINSLEY JANEEN MARSHA

IPC: C07D213/81 ,  A61K31/198 ,  A61K31/223 ,  A61K31/4375 ,  A61K31/44 ,  A61K31/4409 ,  A61K31/4436 ,  A61K31/4545 ,  A61K31/472 ,  A61P1/04 ,  A61P3/10 ,  A61P11/06 ,  A61P17/00 ,  A61P17/02 ,  A61P17/06 ,  A61P19/02 ,  A61P19/08 ,  A61P19/10 ,  A61P21/00 ,  A61P25/28 ,  A61P29/00 ,  A61P37/06 ,  A61P43/00 ,  C07C225/20 ,  C07C229/36 ,  C07D217/22 ,  C07D409/12 ,  C07D471/04

Abstract: Enamine derivatives of formula (1) are described:whereinR is a group Ar L Ar Alk- in, which Ar is an aromatic or heteroaromatic group, L is a covalent bond or a linker atom or group, Ar is an arylene or heteroarylene group and Alk is a chain -CH2-CH(R)-, -CH=C(R)- orin which R is a carboxylic acid or a derivative or biostere thereof;R is a hydrogen atom or a C1-6alkyl group;Cy is a cycloaliphatic or heterocycloaliphatic ring in which X is a N atom or a C(R ) group;R is a oxo, thioxo, or imino group;R and R is each a hydrogen atom or optional substituent; provided that Cy is not a cyclobutenedione 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：DE60130910D1

公开(公告)日：2007-11-22

申请号：DE60130910

申请日：2001-04-12

Applicant: UCB PHARMA SA

Inventor： NORMAN TIMOTHY JOHN ,  PORTER JOHN ROBERT ,  HUTCHINSON BRIAN ,  RATCLIFFE ANDREW ,  HEAD JOHN CLIFFORD ,  ALEXANDER RIKKI ,  LANGHAM BARRY JOHN ,  WARRELLOW GRAHAM JOHN ,  ARCHIBALD SARAH ,  LINSLEY JANEEN MARSHA

IPC: C07D213/81 ,  A61K31/198 ,  A61K31/223 ,  A61K31/4375 ,  A61K31/44 ,  A61K31/4409 ,  A61K31/4436 ,  A61K31/4545 ,  A61K31/472 ,  A61P1/04 ,  A61P3/10 ,  A61P11/06 ,  A61P17/00 ,  A61P17/02 ,  A61P17/06 ,  A61P19/02 ,  A61P19/08 ,  A61P19/10 ,  A61P21/00 ,  A61P25/28 ,  A61P29/00 ,  A61P37/06 ,  A61P43/00 ,  C07C225/20 ,  C07C229/36 ,  C07D217/22 ,  C07D409/12 ,  C07D471/04

Abstract: Enamine derivatives of formula (1) are described:whereinR is a group Ar L Ar Alk- in, which Ar is an aromatic or heteroaromatic group, L is a covalent bond or a linker atom or group, Ar is an arylene or heteroarylene group and Alk is a chain -CH2-CH(R)-, -CH=C(R)- orin which R is a carboxylic acid or a derivative or biostere thereof;R is a hydrogen atom or a C1-6alkyl group;Cy is a cycloaliphatic or heterocycloaliphatic ring in which X is a N atom or a C(R ) group;R is a oxo, thioxo, or imino group;R and R is each a hydrogen atom or optional substituent; provided that Cy is not a cyclobutenedione 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：CA2620362A1

公开(公告)日：2007-03-22

申请号：CA2620362

申请日：2006-09-12

Applicant: UCB PHARMA SA

Inventor： ALI MEZHER HUSSEIN ,  NORMAN TIMOTHY JOHN ,  DE CANDOLE BENJAMIN CHARLES

IPC: C08F2/38 ,  A61K47/48 ,  C08F8/04 ,  C08F8/32 ,  C08F120/36

Abstract: The present invention provides a process for producing a comb polymer comprising the steps of : a) providing: (i) (w+z) molar equivalents of a monomer; (ii) one molar equivalent of an initiator compound of formula (IX), wherein B3 represents a halogen, B2 represents H or a halogen, Y1 represents a group capable of attaching the residue of an antibody or fragment thereof or capable of being converted into such a group, L represents a linker group, y is 1, 2 or 3, w is at least 1 and z is 0 or greater; (iii) a catalyst capabl e of catalysing the polymerisation of a plurality of the monomers to produce t he comb polymer; and b) causing the catalyst to catalyse, in combination with t he initiator, the polymerisation of a plurality of the monomers (i) to produce the comb polymer.