公开(公告)号：ES2295150T3

公开(公告)日：2008-04-16

申请号：ES01921580

申请日：2001-04-12

Applicant: UCB PHARMA SA

Inventor： NORMAN TIMOTHY JOHN ,  PORTER JOHN ROBERT ,  HUTCHINSON BRIAN ,  RATCLIFFE ANDREW JAMES ,  HEAD JOHN CLIFFORD ,  ALEXANDER RIKKI PETER

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: Un compuesto según la fórmula (1) en el que R1 es un grupo Ar1L2Ar2Alq- en la que Ar1 es un grupo aromático o heteroaromático, opcionalmente sustituido, L2 es un enlace covalente o un átomo o grupo enlazador L2a o un enlazador -(Alqa)L2a-, donde Alqa es una cadena alifática o heteroalifática, y L2a es un átomo o grupo enlazador seleccionado de átomos -O- o -S- o grupos -C(O)-, -C(O)O-, -OC(O)-, -C(S)-, -S(O)-, -S(O)2-, -N(R8)- [donde R8 es un átomo de hidrógeno o un grupo alquilo (C1-6), lineal o ramificado], -CON(R8)-, -OC(O)N(R8)-, -CSN(R8)-, -N(R8)CO-, -N(R8)C(O)O-, -N(R8)CS-, -S(O)2N(R8)-, -N(R8)S(O)2-, -N(R8)O-, -ON(R8)-, -N(R8)N(R8)-, N(R8)CON(R8)-, N(R8)CSN(R8)-, o -N(R8SO2N(R8)-, Ar2 es un grupo arileno o heteroarileno, opcionalmente sustituido, y Alq es una cadena -CH2-CH(R)-, en la que R es un ácido carboxílico (-CO2H) o un grupo -CO2Alq7; Alq7 es un grupo alquilo(C1-8), lineal o ramificado, o un alquenilo C2-8, alquinilo C2-8, cicloalquilo(C3-8), cicloalquil(C3-8)-alquilo(C1-8), heterocicloalquil(C3-8)-alquilo(C1-6), alquil(C1-6)oxialquilo(C1-6), alquil(C1-6)tioalquilo(C1-6), alquil(C1-6)sulfinilalquilo(C1-6), alquil(C1-6)sulfonilalquilo(C1-6), cicloalquil(C3-8)oxialquilo(C1-6), cicloalquil(C3-8)-tioalquilo(C1-6), cicloalquinil(C3-8)sulfinilalquilo(C1-6), cicloalquinil(C3-8)sulfonilalquilo(C1-6), alquil(C1-6)oxicarbonilalquilo(C1-6), alquil(C1-6)oxicarbonilalquenilo(C1-6), alquil(C1-6)-oxicarboniloxialquilo(C1-6), alquil(C1-6)oxicarboniloxialquenilo(C1-6), cicloalquil(C3-8)-oxicarboniloxialquilo(C1-6), N-di-[alquil(C1-8)aminoalquilo(C1-8)], N-aril(C6-12)-N-[alquil(C1-6)aminoalquilo(C1-6)], N-di-[alquil(C1-8)carbamoilalquilo(C1-8)], aril(C6-10)alquilo(C1-6), arilo(C6-10), aril(C6-10)oxialquilo(C1-8), aril(C6-12)tioalquilo(C1-8), aril(C6-12)sulfinilalquilo(C1-8), aril(C6-12)sulfonilalquilo(C1-8), alcanoil(C1-8)oxialquilo(C1-8), imido(C4-8)alquilo(C1-8), aroil(C6-12)oxialquilo(C1-8) o un grupo triglicérido; y las sales, sus solvatos, hidratos y N-óxidos..

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.