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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..
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2.
公开(公告)号:SI1370531T1
公开(公告)日:2007-08-31
申请号:SI200230546
申请日:2002-01-18
Applicant: UCB PHARMA SA
Inventor: BAILEY STUART , BROWN JULIEN , BRAND STEPHEN , JOHNSON JAMES ANDREW , PORTER JOHN ROBERT , HEAD JOHN CLIFFORD
IPC: C07D213/00 , A61K31/198 , A61K31/4375 , A61K31/44 , A61K31/4406 , A61K31/497 , A61P3/10 , A61P9/00 , A61P17/00 , A61P17/06 , A61P19/02 , A61P25/00 , A61P29/00 , A61P37/00 , A61P37/06 , A61P43/00 , C07C229/00 , C07C229/34 , C07C229/46 , C07C233/82 , C07C321/22 , C07C323/30 , C07D213/81 , C07D213/89 , C07D401/00 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/00 , C07D471/04
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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.
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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.
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公开(公告)号:ES2282403T3
公开(公告)日:2007-10-16
申请号:ES02715515
申请日:2002-01-18
Applicant: UCB PHARMA SA
Inventor: BAILEY STUART , BROWN JULIEN ALISTAIR , BRAND STEPHEN , JOHNSON JAMES ANDREW , PORTER JOHN ROBERT , HEAD JOHN CLIFFORD
IPC: C07D213/81 , A61K31/198 , A61K31/4375 , A61K31/44 , A61K31/4406 , A61K31/497 , A61P3/10 , A61P9/00 , A61P17/00 , A61P17/06 , A61P19/02 , A61P25/00 , A61P29/00 , A61P37/00 , A61P37/06 , A61P43/00 , C07C229/34 , C07C229/36 , C07C229/46 , C07C233/82 , C07C321/22 , C07C323/30 , C07D213/89 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/04
Abstract: Un compuesto de **fórmula**, en la que Ar1 es un grupo aromático o heteroaromático opcionalmente sustituido; en el que los sustituyentes opcionales se seleccionan de uno, dos o tres átomos de halógeno, y/o grupos alquiloC1-6, cicloalquiloC3-8, hidroxialquilo1-6, carboxialquiloC1-6, alquilC1-6tio, carboxialquilC1-6tio, alcoxiC1-6, hidroxialcoxiC1-6, haloalquiloC1-6, haloalcoxiC1-6, alquilC1-6amino, -NH2, aminoalquiloC1-6, dialquilC1-6amino, alquilC1-6amino-alquiloC1-6, dialquilC1-6amino-alquiloC1-6, aminoalcoxiC1-6, alquilC1-6amino-alcoxiC1-6, dialquilC1-6amino-alcoxiC1-6, nitro, ciano, amidino, -OH, HC(O)-, -CO2H, -CO2R5, alcanoíloC1-6, -SH, tioalquiloC1-6, -SO3H, -SO2R5, alquilC1-6sulfinilo, alquilC1-6sulfonilo, -SO2NH2, alquilC1-6aminosulfonilo, dialquilC1-6aminosulfonilo, fenilaminosulfonilo, -CONH2, alquilC1-6aminocarbonilo, dialquilC1-6aminocarbonilo, aminoalquilC1-6aminocarbonilo, alquilC1-6aminoalquilC1-6aminocarbonilo, dialquilC1-6aminoalquilC1-6aminocarbonilo, aminocarbonilamino, alquilC1-6aminocarbonilamino, dialquilC1-6aminocarbonilamino, alquilC1-6amino-carbonilalquilC1-6amino, aminotiocarbonilamino, alquilC1-6aminotiocarbonilamino, dialquilC1-6aminotiocarbonilamino, alquilC1-6aminotiocarbonilalquilC1-6amino, alquilC1-6sulfonilamino, dialquilC1-6sulfonilamino, -NHSO2NH2, alquilC1-6aminosulfonilamino, dialquilC1-6aminosulfonilamino, alcanoC1-6ilamino, aminoalcanoC1-6ilamino, dialquilC1-6aminoalcanoC1-6ilamino, alcanoC1-6ilaminoC1-6alquilo, alcanoC1-6ilaminoalquilC1-6amino o alcoxiC1-6carbonilamino; R5 es un átomo de hidrógeno, o un grupo alquiloC1-6 o cicloalquiloC3-8; L2 es un enlace covalente o un grupo L2a o -(Alc3)L2a, en el que Alc3 es una cadena alifática o heteroalifática opcionalmente sustituida y L2a es un átomo de -O- o -S- o un grupo -C(O)-, -C(O)O-, -C(S)-, -S(O)-, -S(O)2-, -N(R8)- [en el que R8 es un átomo de hidrógeno o un grupo alquiloC1-6 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(R8)SO2N(R8)-; los sustituyentes opcionales que pueden estar presentes en Alc3 se seleccionan de uno, dos o tres sustituyentes donde cada sustituyente puede ser el mismo o diferente y se selecciona de átomos de halógeno, o grupos -OH, -CO2H, -CO2R9, donde R9 es un grupo alquiloC1-6 lineal o ramificado, -CONHR9, -CON(R9)2, -COR9, alcoxiC1-6, tiol, -S(O)R9, -S(O)2R9, alquiltioC1-6, amino, -NHR9 o -N(R9)2; Ar2 es un grupo arileno o heteroarileno opcionalmente sustituido; en el que los sustituyentes opcionales que pueden estar presentes en Ar2 se seleccionan de átomos de halógeno, o grupos alquiloC1-6, halo alquiloC1-6, alcoxiC1-6, haloalcoxiC1-6, -CN, -CO2CH3, -NO2, -NH2, -NR5R6 y -N(R5)COCH3; R6 es como se definió para R5; y Alc es una cadena -CH2-CH(R)-, -CH=C(R)- y las sales, solvatos, hidratos y N-óxidos del mismo.
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6.
公开(公告)号:AU2002225163B2
公开(公告)日:2007-08-02
申请号:AU2002225163
申请日:2002-01-18
Applicant: UCB PHARMA SA
Inventor: PORTER JOHN ROBERT , BRAND STEPHEN , BAILEY STUART , JOHNSON JAMES ANDREW , HEAD JOHN CLIFFORD , BROWN JULIEN ALISTAIR
IPC: C07D213/81 , A61K31/198 , A61K31/4375 , A61K31/44 , A61K31/4406 , A61K31/497 , A61P3/10 , A61P9/00 , A61P17/00 , A61P17/06 , A61P19/02 , A61P25/00 , A61P29/00 , A61P37/00 , A61P37/06 , A61P43/00 , C07C229/34 , C07C229/46 , C07C233/82 , C07C321/22 , C07C323/30 , C07D213/89 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/04
Abstract: Phenylalanine enamide derivatives of formula (1) are described: wherein R 1 , R x , R y , R z , X and V are as defined in claim 1. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immuno or inflammatory disorders or disorders involving the inappropriate growth or migration of cells.
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公开(公告)号:NO326554B1
公开(公告)日:2009-01-12
申请号:NO20033710
申请日:2003-08-20
Applicant: UCB PHARMA SA
Inventor: PORTER JOHN ROBERT , BAILEY STUART , BROWN JULIEN ALISTAIR , BRAND STEPHEN , JOHNSON JAMES ANDREW , HEAD JOHN CLIFFORD
IPC: C07D213/81 , A61K31/198 , A61K31/4375 , A61K31/44 , A61K31/4406 , A61K31/497 , A61P3/10 , A61P9/00 , A61P17/00 , A61P17/06 , A61P19/02 , A61P25/00 , A61P29/00 , A61P37/00 , A61P37/06 , A61P43/00 , C07C229/34 , C07C229/46 , C07C233/82 , C07C321/22 , C07C323/30 , C07D213/89 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/04
Abstract: Phenylalanine enamide derivatives of formula (1) are described: wherein R 1 , R x , R y , R z , X and V are as defined in claim 1. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immuno or inflammatory disorders or disorders involving the inappropriate growth or migration of cells.
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