公开(公告)号：UA78578C2

公开(公告)日：2007-04-10

申请号：UA2005000509

申请日：2003-06-20

Applicant: CELLTECH R&D LTD

Inventor： BROOKINGS DANIEL CHRISTOPHER ,  DAVIS JEREMY MARTIN ,  LANGHEM BARRY JOHN

IPC: A61K31/4743 ,  A61P1/04 ,  A61P1/16 ,  A61P3/10 ,  A61P7/00 ,  A61P7/02 ,  A61P7/04 ,  A61P7/06 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P13/12 ,  A61P17/00 ,  A61P17/02 ,  A61P17/06 ,  A61P19/02 ,  A61P19/08 ,  A61P19/10 ,  A61P21/04 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P31/00 ,  A61P31/12 ,  A61P31/16 ,  A61P31/22 ,  A61P35/00 ,  A61P35/02 ,  A61P37/00 ,  A61P37/02 ,  A61P37/08 ,  A61P43/00 ,  C07D495/04

Abstract: Bicyclic heteroaromalic derivatives of formula(l)are described: F(l)where: the dashed line joining A and C(Ra) is present and represents a bond and A is a -N= atom or a -C(Rb)= group, or the dashed line is absent and A is a -N(Rb)-, or -C(Rb)(Rc)-1 group; X is an -O-, -S- or substituted nitrogen atom or a -S(O)-, -S(O2)- or -NH- group; Y is a nitrogen or substituted carbon atom or 1 a -CH= group; n is zero or the integer 1; Alk1 is an optionally substituted aliphatic or heteroaliphatic chain L1 is a covalent bond or a linker atom or group; Cy1 is a hydrogen atom or an optionally substituted cycloaliphatic, polycycloaliphatic, heterocycloaliphalic, polyheterocycloaliphalic, aromatic or heleroaromatic group; Ar is an optionally substituted aromatic or heteroaromalic group; and the remaining substituenis are defined in the specification. The compounds are potent and selective inhibitors of p38 kinase and are of use in the prophylaxis and treatment of immune or inflammatory disorders. (1)

公开(公告)号：AT348817T

公开(公告)日：2007-01-15

申请号：AT00940569

申请日：2000-06-19

Applicant: CELLTECH R&D LTD

Inventor： BATCHELOR MARK JAMES ,  MOFFAT DAVID FESTUS CHARLES ,  DAVIS JEREMY MARTIN ,  HUTCHINGS MARTIN CLIVE

IPC: A61K31/505 ,  A61K31/506 ,  A61P9/10 ,  A61P9/14 ,  A61P17/06 ,  A61P19/02 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D239/42 ,  C07D401/04 ,  C07D401/14 ,  C07D403/12 ,  C07D409/04

Abstract: Pyrimidines of formula (1) are described wherein Ar is an optionally substituted aromatic or heteroaromatic group; R is a hydrogen atom or a straight or branched chain alkyl group; R is a -X -R group where X is a direct bond or a linker atom or group, and R is an optionally substituted aliphatic, cycloaliphatic, heteroaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are selective KDR Kinase and/or FGFr Kinase inhibitors and are of use in the prophylaxis and treatment of disease states assoicated with angiogenesis.

公开(公告)号：ES2253265T3

公开(公告)日：2006-06-01

申请号：ES00969695

申请日：2000-10-19

Applicant: CELLTECH R&D LTD

Inventor： DAVIS JEREMY MARTIN ,  MOFFAT DAVID FESTUS CHARLES

IPC: A61K31/505 ,  A61P9/00 ,  A61P9/10 ,  A61P9/14 ,  A61P17/06 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D239/42 ,  C07D401/12 ,  C07D403/12 ,  C07D521/00

Abstract: Un compuesto de fórmula (1): en la que R1 es un grupo -XR6 [donde X es un enlace covalente, -O-, -S-, -C(O)-, -C(S)-, -C(O)O-, -S(O)-, - S(O2)-, -CH2- o N(R7)- [donde R7 es un átomo de hidrógeno o un grupo alquilo lineal o ramificado] y R6 es un átomo de hidrógeno o halógeno o un grupo alifático, cicloalifático, heteroalifático, heterocicloalifático, aromático o heteroaromático opcionalmente sustituido, o un grupo -NO2, -CN, -SO2N(R8)(R9) [donde R8 y R9, que pueden ser iguales o diferentes, son un átomo de hidrógeno o un grupo alifático, cicloalifático, heteroalifático, heterociciloalifático, aromático o heteroaromático opcionalmente sustituido], - CON(R8)(R9), -CSN(R8)(R9), -NH2 o un grupo amino sustituido; R4 es un grupo X1R11 donde X1 es un enlace covalente o un grupo -C(R12)(R13)- [donde cada uno de R12 y R13 es un átomo de hidrógeno o halógeno o un grupo hidroxilo, alquilo o haloalquilo] o un grupo -C(O)- y R11 es un grupo fenilo, tienilo, tiazolilo o indolilo opcionalmente sustituido; R5 es un átomo de halógeno o un grupo alquinilo; y las sales, solvatos, hidratos y N-óxidos del mismo.

公开(公告)号：NO20060279A

公开(公告)日：2006-03-20

申请号：NO20060279

申请日：2006-01-19

Applicant: CELLTECH R&D LTD

Inventor： DAVIS JEREMY MARTIN ,  BROOKINGS DANIEL CHRISTOPHER ,  LANGHAM BARRY JOHN

IPC: C07D495/04 ,  A61P29/00

CPC classification number: C07D495/04

公开(公告)号：NO20041975A

公开(公告)日：2005-07-16

申请号：NO20041975

申请日：2004-05-13

Applicant: CELLTECH R&D LTD

Inventor： DAVIS JEREMY MARTIN ,  BROOKINGS DANIEL CHRISTOPHER ,  LANGHAM BARRY JOHN

IPC: A61K31/4365 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61P1/04 ,  A61P1/16 ,  A61P3/10 ,  A61P5/14 ,  A61P7/02 ,  A61P7/06 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P13/12 ,  A61P17/00 ,  A61P17/06 ,  A61P19/02 ,  A61P19/08 ,  A61P19/10 ,  A61P21/04 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P31/04 ,  A61P31/12 ,  A61P31/14 ,  A61P31/18 ,  A61P31/20 ,  A61P35/00 ,  A61P35/02 ,  A61P35/04 ,  A61P37/00 ,  A61P37/02 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  C07D471/04 ,  C07D495/04

CPC classification number: C07D471/04 ,  C07D495/04

公开(公告)号：ES2188429B2

公开(公告)日：2005-06-16

申请号：ES200150085

申请日：2000-06-19

Applicant: CELLTECH R&D LTD

Inventor： BATCHELOR MARK JAMES ,  MOFFAT DAVID FESTUS CHARLES ,  DAVIS JEREMY MARTIN ,  HUTCHINGS MARTIN CLIVE

IPC: A61K31/505 ,  A61K31/506 ,  A61P9/10 ,  A61P9/14 ,  A61P17/06 ,  A61P19/02 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D239/42 ,  C07D401/04 ,  C07D401/14 ,  C07D403/12 ,  C07D409/04

Abstract: Se describen pirimidinas de fórmula (I) en la que Ar es un grupo aromático o heteroaromático opcionalmente sustiuido; R1 es un átomo de hidrógeno o un grupo alquilo de cadena lineal o ramificada; R2 es un grupo -X1-R3 en el que X1 es un enlace directo o un átomo o grupo de enlace, y R3 es un grupo alifático, cicloalifático, heteroalifático, heterocicloalifático, aromático o heteroaromático opcionalmente sustituido; y las sales, solvatos, hidratos y N-óxidos del mismo. Los compuestos son inhibidores selectivos de la quinasa KDR y/o la quinasa FGFr y son de utilidad en la profilaxis y tratamiento de estados de enfermedad asociados con la angiogénesis.

公开(公告)号：BR0311842A

公开(公告)日：2005-03-15

申请号：BR0311842

申请日：2003-06-20

Applicant: CELLTECH R&D LTD

Inventor： BROOKINGS DANIEL CHRISTOPHER ,  DAVIS JEREMY MARTIN ,  LANGHAM BARRY JOHN

IPC: A61K31/4743 ,  A61P1/04 ,  A61P1/16 ,  A61P3/10 ,  A61P7/00 ,  A61P7/02 ,  A61P7/04 ,  A61P7/06 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P13/12 ,  A61P17/00 ,  A61P17/02 ,  A61P17/06 ,  A61P19/02 ,  A61P19/08 ,  A61P19/10 ,  A61P21/04 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P31/00 ,  A61P31/12 ,  A61P31/16 ,  A61P31/22 ,  A61P35/00 ,  A61P35/02 ,  A61P37/00 ,  A61P37/02 ,  A61P37/08 ,  A61P43/00 ,  C07D495/04 ,  A61K31/44

Abstract: Bicyclic heteroaromatic derivatives of formula (1) are described: F(1) where: the dashed line joining A and C(Ra) is present and represents a bond and A is a —N═ atom or a —C(Rb)═ group, or the dashed line is absent and A is a —N(Rb)—, or —C(Rb)(Rc)— group; X is an —O—, —S— or substituted nitrogen atom or a —S(O)—, —S(O2)— or —NH-group; Y is a nitrogen or substituted carbon atom or a —CH═ group; n is zero or the integer 1; Alk1 is an optionally substituted aliphatic or heteroaliphatic chain L1 is a covalent bond or a linker atom or group; Cy1 is a hydrogen atom or an optionally substituted cycloaliphatic, polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; Ar is an optionally substituted aromatic or heteroaromatic group; and the remaining substituents are defined in the specification. The compounds are potent and selective inhibitors of p38 kinase and are of use in the prophylaxis and treatment of immune or inflammatory disorders.

公开(公告)号：CA2495518A1

公开(公告)日：2004-02-19

申请号：CA2495518

申请日：2003-08-11

Applicant: CELLTECH R&D LTD

Inventor： DAVIS JEREMY MARTIN ,  LANGHAM BARRY JOHN ,  BROOKINGS DANIEL CHRISTOPHER

IPC: A61K31/4365 ,  A61P1/02 ,  A61P1/04 ,  A61P1/16 ,  A61P1/18 ,  A61P3/10 ,  A61P7/02 ,  A61P7/04 ,  A61P7/06 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P13/12 ,  A61P17/02 ,  A61P17/04 ,  A61P17/06 ,  A61P19/02 ,  A61P19/06 ,  A61P19/08 ,  A61P19/10 ,  A61P21/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/16 ,  A61P25/28 ,  A61P27/02 ,  A61P29/00 ,  A61P31/00 ,  A61P31/04 ,  A61P31/12 ,  A61P31/14 ,  A61P31/16 ,  A61P31/18 ,  A61P31/20 ,  A61P31/22 ,  A61P33/06 ,  A61P35/00 ,  A61P35/02 ,  A61P37/02 ,  A61P37/06 ,  A61P37/08 ,  A61P39/02 ,  A61P43/00 ,  C07D495/04

Abstract: A series of 5-6 fused ring bicyclic heteroaromatic derivatives, based in particular on the 6-oxo-6,7-dihydrothieno[2,3-b]pyridine ring system, being inhibitors of p38 kinase, are accordingly of use in medicine, for example in the treatment and/or prevention of immune or inflammatory disorders.

公开(公告)号：CA2462147A1

公开(公告)日：2003-04-24

申请号：CA2462147

申请日：2002-10-16

Applicant: CELLTECH R&D LTD

Inventor： DAVIS JEREMY MARTIN ,  LANGHAM BARRY JOHN ,  BROOKINGS DANIEL CHRISTOPHER

IPC: A61K31/4365 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61P1/04 ,  A61P1/16 ,  A61P3/10 ,  A61P5/14 ,  A61P7/02 ,  A61P7/06 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P13/12 ,  A61P17/00 ,  A61P17/06 ,  A61P19/02 ,  A61P19/08 ,  A61P19/10 ,  A61P21/04 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P31/04 ,  A61P31/12 ,  A61P31/14 ,  A61P31/18 ,  A61P31/20 ,  A61P35/00 ,  A61P35/02 ,  A61P35/04 ,  A61P37/00 ,  A61P37/02 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  C07D471/04 ,  C07D495/04 ,  C07D209/00 ,  C07D221/00 ,  C07D333/00

Abstract: Compounds of formulae (1 a) and (1 b) are described: in which the dashed lin e represents an optional bond; A is a -N= atom or a -N(Rb)-, -C(Rb)= or - C(Rb)(RC)- group; Ra, Rb and Rc is each independently a hydrogen atom or an optionally substituted C1-6alkyl group; X is an -O- or -S- atom or -NH- grou p or substituted N atom; each Y is independently a N atom or CH group or substituted C atom; n is zero or the integer 1; Alk1 is an optionally substituted aliphatic or heteroaliphatic chain L1 is a covalent bond or a linker atom or group; Cy1 is a hydrogen atom or an optionally substituted cycloaliphatic, polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; Ar is an optionally substituted aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof; The compounds are potent inhibitors of p38 kinase and are use in the prophylaxis or treatment of p38 kinase mediated diseases or disorders, such as rheumatoid arthritis.

公开(公告)号：HK1048815A1

公开(公告)日：2003-04-17

申请号：HK03101022

申请日：2003-02-12

Applicant: CELLTECH R&D LTD

Inventor： BATCHELOR MARK JAMES ,  MOFFAT DAVID FESTUS CHARLES ,  DAVIS JEREMY MARTIN

IPC: A61K31/505 ,  A61K31/506 ,  A61P9/10 ,  A61P9/14 ,  A61P17/06 ,  A61P19/02 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D239/42 ,  C07D401/04 ,  C07D401/14 ,  C07D403/12 ,  C07D409/04 ,  C07D ,  A61K ,  A61P

Abstract: Pyrimidines of formula (1) are described wherein Ar is an optionally substituted aromatic or heteroaromatic group; R is a hydrogen atom or a straight or branched chain alkyl group; R is a -X -R group where X is a direct bond or a linker atom or group, and R is an optionally substituted aliphatic, cycloaliphatic, heteroaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are selective KDR Kinase and/or FGFr Kinase inhibitors and are of use in the prophylaxis and treatment of disease states assoicated with angiogenesis.