公开(公告)号：CA2487718A1

公开(公告)日：2003-12-31

申请号：CA2487718

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) wher e: the dashed line joining A and C(Ra) is present and represents a bond and A i s 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 kina se and are of use in the prophylaxis and treatment of immune or inflammatory disorders.

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

公开(公告)号：CA2387034A1

公开(公告)日：2001-04-26

申请号：CA2387034

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 formula (1) are described, wherein R1 is a -XR6 group; R2 and R3 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, -OR10 [where R10 is an optionall y substituted aliphatic, cycloaliphatic, heteroaliphatic, heterocycloaliphatic , aromatic or heteroaromatic group] -SH, -NO2, -CN, -SR10, -COR10, S(O)R10, - SO2R8, -SO2N(R8)(R9), -CO2R8, -CON(R8)(R9), -CSN(R8)(R9), -NH2 or substitute d amino group; R4 is a X1R11 group where X1 is a covalent bond or a -C(R12)(R1 3)- [where each of R12 and R13 is a hydrogen or halogen atom or a hydroxyl, alky l or haloalkyl group] or -C(O)- group and R11 is an optionally substituted phenyl, thienyl, thiazolyl or indolyl group; R5 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：CA2375182A1

公开(公告)日：2000-12-28

申请号：CA2375182

申请日：2000-06-19

Applicant: CELLTECH R&D LTD

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

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; R1 is a hydrogen atom or a straight or branched chain alkyl group; R2 is a -X1-R3 group where X1 is a direct bond or a linker atom or group, and R3 is an optionally substituted aliphatic, cycloaliphatic, heteroaliphatic, heterocycloaliphatic, aromatic o r 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 associated with angiogenesis.