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：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：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：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：NZ532713A

公开(公告)日：2005-10-28

申请号：NZ53271302

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: Disclosed are compounds of formula (Ia), wherein: A is -C(Rb)= or -C(Rb)(Rc)-, Ra, Rb and Rc are independently H or optionally substituted alkyl, X is O or S, Y is N, CH or substituted C, n is 0 or 1, Alk1 is an optionally substituted aliphatic or heteroaliphatic chain, L1 is a bond, or linker atom or group, Cy1 is H, or optionally substituted cycloaliphatic, polycycloaliphati, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic, Ar is an optionally substituted aromatic or heteroaromatic. The compounds are used in the manufacture of medicaments for the treatment of immune and inflammatory diseases.

公开(公告)号：NO20050306L

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

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：CA2528602A1

公开(公告)日：2004-12-29

申请号：CA2528602

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 ,  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 disorde rs.