公开(公告)号：DE60024854D1

公开(公告)日：2006-01-19

申请号：DE60024854

申请日：2000-10-19

Applicant: CELLTECH R&D LTD

Inventor： DAVIS MARTIN ,  MOFFAT FESTUS

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

公开(公告)号：DE60024854T2

公开(公告)日：2006-08-24

申请号：DE60024854

申请日：2000-10-19

Applicant: CELLTECH R&D LTD

Inventor： DAVIS MARTIN ,  MOFFAT FESTUS

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

公开(公告)号：DE60032482T2

公开(公告)日：2007-09-27

申请号：DE60032482

申请日：2000-06-19

Applicant: CELLTECH R&D LTD

Inventor： BATCHELOR JAMES ,  MOFFAT FESTUS ,  DAVIS MARTIN ,  HUTCHINGS CLIVE

IPC: C07D239/42 ,  A61K31/505 ,  A61K31/506 ,  A61P9/10 ,  A61P9/14 ,  A61P17/06 ,  A61P19/02 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  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：DE60032482D1

公开(公告)日：2007-02-01

申请号：DE60032482

申请日：2000-06-19

Applicant: CELLTECH R&D LTD

Inventor： BATCHELOR JAMES ,  MOFFAT FESTUS ,  DAVIS MARTIN ,  HUTCHINGS CLIVE

IPC: C07D239/42 ,  A61K31/505 ,  A61K31/506 ,  A61P9/10 ,  A61P9/14 ,  A61P17/06 ,  A61P19/02 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  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.