公开(公告)号：NO20016162A

公开(公告)日：2002-02-18

申请号：NO20016162

申请日：2001-12-17

Applicant: CELLTECH R&D LTD

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

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

CPC classification number: C07D239/42 ,  C07D401/04 ,  C07D403/12 ,  C07D409/04

公开(公告)号：NO20016162D0

公开(公告)日：2001-12-17

申请号：NO20016162

申请日：2001-12-17

Applicant: CELLTECH R&D LTD

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

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

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：ES2277841T3

公开(公告)日：2007-08-01

申请号：ES00940569

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: 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: 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：ZA200402803B

公开(公告)日：2006-06-28

申请号：ZA200402803

申请日：2004-04-13

Applicant: CELLTECH R&D LTD

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

IPC: A61K20060101 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61P20060101 ,  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 ,  C07D20060101 ,  C07D471/04 ,  C07D495/04

Abstract: Compounds of formulae (1a) and (1b) are described: in which the dashed line represents an optional bond; A is a -N- atom or a -N(R b )-, -C(R b )- or -C(R b )(R C )- group; R a , R b and R c is each independently a hydrogen atom or an optionally substituted C 1-6 alkyl group; X is an -O- or -S- atom or -NH- group 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; Alk 1 is an optionally substituted aliphatic or heteroaliphatic chain L 1 is a covalent bond or a linker atom or group; Cy 1 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：NO20060279L

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

Abstract: A series of thieno[2,3-b]pyridin-6(7H)-one derivatives, substituted in the 2-position by a carbonyl- or sulfonyl-linked pyrrolidin-1-yl or related moiety, being inhibitors of p38 MAP 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：AT312826T

公开(公告)日：2005-12-15

申请号：AT00969695

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：PL375083A1

公开(公告)日：2005-11-14

申请号：PL37508303

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：PL369867A1

公开(公告)日：2005-05-02

申请号：PL36986702

申请日：2002-10-16

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

Abstract: Compounds of formulae (1a) and (1b) are described: in which the dashed line represents an optional bond; A is a -N- atom or a -N(R b )-, -C(R b )- or -C(R b )(R C )- group; R a , R b and R c is each independently a hydrogen atom or an optionally substituted C 1-6 alkyl group; X is an -O- or -S- atom or -NH- group 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; Alk 1 is an optionally substituted aliphatic or heteroaliphatic chain L 1 is a covalent bond or a linker atom or group; Cy 1 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：NO20050306A

公开(公告)日：2005-03-16

申请号：NO20050306

申请日：2005-01-19

Applicant: CELLTECH R&D LTD

Inventor： DAVIS JEREMY MARTIN ,  BROOKINGS DANIEL CHRISTOPHER ,  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

CPC classification number: C07D495/04

公开(公告)号：CA2528603A1

公开(公告)日：2004-12-29

申请号：CA2528603

申请日：2004-06-18

Applicant: CELLTECH R&D LTD

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

IPC: C07D495/04 ,  A61K31/4365 ,  A61P19/02 ,  A61P29/00 ,  A61P37/02 ,  C07D221/00 ,  C07D333/00

Abstract: A series of thieno[2,3-b]pyridin-6(7H)-one derivatives, substituted in the 2 - position by a carbonyl- or sulfonyl-linked pyrrolidin-3-yl, pyrrolidin-3- ylamino or related moiety, being inhibitors of p38 MAP kinase, are according ly of use in medicine, for example in the treatment and/or prevention of immune or inflammatory disorders.