公开(公告)号：WO02087587A3

公开(公告)日：2003-01-09

申请号：PCT/GB0202011

申请日：2002-05-02

Applicant: CELLTECH R&D LTD ,  MOFFAT DAVID FESTUS CHARLES ,  BATCHELLOR MARK JAMES ,  BROOKINGS DANIEL CHRISTOPHER ,  DAVIS PETER DAVID

Inventor： MOFFAT DAVID FESTUS CHARLES ,  BATCHELLOR MARK JAMES ,  BROOKINGS DANIEL CHRISTOPHER ,  DAVIS PETER DAVID

IPC: A61P35/00 ,  C07D239/93 ,  C07D239/94 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  A61K31/517

CPC classification number: C07D401/12 ,  C07D239/93 ,  C07D239/94 ,  C07D403/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12

Abstract: Compounds of formula (1) are described wherein Ar is an optionally substituted aryl, heteroaryl, aralkyl, heteroaralkyl or alkyl group, X is a nitrogen atom or a C(R ) group, n is zero or the integer 1 or 2 and R, R , R , R and R are substituents defined in the specification. The compounds are able to inhibit the activity of Class 1 receptor tyrosine kinases and are of use in the treatment of hyperproliferative disorders such as psoriasis.

Abstract translation: 描述式（1）化合物，其中Ar是任选取代的芳基，杂芳基，芳烷基，杂芳烷基或烷基，X是氮原子或C（R 1a）基团，n是0或整数1或2 R 1，R 2，R 2，R 3和R 4是说明书中定义的取代基。 该化合物能够抑制1类受体酪氨酸激酶的活性，并且可用于治疗过度增殖性疾病如牛皮癣。

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：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：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.

公开(公告)号：AU5548800A

公开(公告)日：2001-01-09

申请号：AU5548800

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：PL352163A1

公开(公告)日：2003-07-28

申请号：PL35216300

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：CZ20014583A3

公开(公告)日：2002-05-15

申请号：CZ20014583

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：IS6166A

公开(公告)日：2001-11-19

申请号：IS6166

申请日：2001-11-19

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

公开(公告)号：AU7935100A

公开(公告)日：2001-04-30

申请号：AU7935100

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: Pyrimidines of formla (1) are described: wherein R 1 is a -XR 6 group; R 2 and R 3 which may be the same or different is each a hydrogen or halogen atom or a group selected from an optionally substituted aliphatic, cycloaliphatic, heteroaliphatic, heterocycloaliphatic, -OH, -OR 10 [where R 10 is an optionally substituted aliphatic, cycloaliphatic, heteroaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group) -SH, -NO 2 , -CN, -SR 10 , -COR 10 , S(O)R 10 , -SO 2 R 8 , -SO 2 N(R 8 )(R 9 ), -CO 2 R 8 , -CON(R 8 )(R 9 ), -CSN(R 8 )(R 9 ), -NH 2 or substituted amino group; R 4 is a X 1 R 11 group where X 1 is a covalent bond or a -C(R 12 )(R 13 )- [where each of R 12 and R 13 is a hydrogen or halogen atom or a hydroxyl, alkyl or haloalkyl group] or -C(O)- group and R 11 is an optionally substituted phenyl, thienyl, thiazolyl or indolyl group; R 5 is a halogen atom or an alkynyl 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 associated with angiogenesis