公开(公告)号：WO0179173A2

公开(公告)日：2001-10-25

申请号：PCT/GB0101682

申请日：2001-04-12

Applicant: CELLTECH R&D LTD ,  NORMAN TIMOTHY JOHN ,  PORTER JOHN ROBERT ,  HUTCHINSON BRIAN WOODSIDE ,  RATCLIFFE ANDREW JAMES ,  HEAD JOHN CLIFFORD ,  ALEXANDER RIKKI PETER ,  LANGHAM BARRY JOHN ,  WARRELLOW GRAHAM JOHN ,  ARCHIBALD SARAH CATHERINE ,  LINSLEY JANEEN MARSHA

Inventor： NORMAN TIMOTHY JOHN ,  PORTER JOHN ROBERT ,  HUTCHINSON BRIAN WOODSIDE ,  RATCLIFFE ANDREW JAMES ,  HEAD JOHN CLIFFORD ,  ALEXANDER RIKKI PETER ,  LANGHAM BARRY JOHN ,  WARRELLOW GRAHAM JOHN ,  ARCHIBALD SARAH CATHERINE ,  LINSLEY JANEEN MARSHA

IPC: A61K31/198 ,  A61K31/223 ,  A61K31/4375 ,  A61K31/4409 ,  A61K31/4436 ,  A61K31/4545 ,  A61K31/472 ,  A61P1/04 ,  A61P3/10 ,  A61P11/06 ,  A61P17/00 ,  A61P17/02 ,  A61P17/06 ,  A61P19/02 ,  A61P19/08 ,  A61P19/10 ,  A61P21/00 ,  A61P25/28 ,  A61P29/00 ,  A61P37/06 ,  A61P43/00 ,  C07C229/36 ,  C07D213/81 ,  C07D217/22 ,  C07D409/12 ,  C07D471/04 ,  A61K31/44 ,  C07C225/20

CPC classification number: C07D213/81 ,  C07C229/36 ,  C07C2601/10 ,  C07D217/22 ,  C07D471/04

Abstract: Enamine derivatives of formula (1) are described. In said formula , R a group Ar L Ar Alk- in which Ar is an aromatic or heteroaromatic group, L is a covalent bond or a linker atom or group, Ar is an arylene or heteroarylene group and Alk is a chain -CH2-CH(R)-, -CH=C(R)- or (a) in which R is a carboxylic acid or a derivative or biostere thereof; R is a hydrogen atom or a C1-6alkyl group; Cy is a cycloaliphatic or heterocycloaliphatic ring in which X is a N atom or a C(R ) group; R is a oxo, thioxo, or imino group; R and R are each a hydrogen atom or optional substituent; provided that Cy is not a cyclobutenedione group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders, or disorders involving the inappropriate growth or migration of cells.

Abstract translation: 描述式（1）的烯胺衍生物。 在所述式中，R 1，Ar 1，Ar 2，Ar 2 Al，其中Ar 1是芳族或杂芳族基团，L 2是共价键或连接原子或 基团，Ar 2是亚芳基或亚杂芳基，Alk是链-CH 2 -CH（R） - ， - CH = C（R） - 或（a）其中R是羧酸或衍生物或生物固体 物; R 2是氢原子或C 1-6烷基; Cy是其中X是N原子或C（R））基团的脂环族或杂脂环族环; R x是氧代，硫代或亚氨基; R w和R z各自为氢原子或任选的取代基; 只要Cy不是环丁烯二酮基团; 及其盐，溶剂合物，水合物和N-氧化物。 这些化合物能够抑制整联蛋白与其配体的结合，并且可用于预防和治疗免疫或炎性疾病或涉及细胞不适当生长或迁移的病症。

公开(公告)号：WO0144194A3

公开(公告)日：2001-12-13

申请号：PCT/GB0004831

申请日：2000-12-15

Applicant: CELLTECH R&D LTD ,  ALEXANDER RIKKI PETER ,  LANGHAM BARRY JOHN ,  REUBERSON JAMES THOMAS ,  TROWN EMMA LOUISE ,  WARRELLOW GRAHAM JOHN

Inventor： ALEXANDER RIKKI PETER ,  LANGHAM BARRY JOHN ,  REUBERSON JAMES THOMAS ,  TROWN EMMA LOUISE ,  WARRELLOW GRAHAM JOHN

IPC: C07D213/74 ,  C07D213/89 ,  C07D401/12 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/444 ,  A61P29/00 ,  A61P35/00

CPC classification number: C07D213/74 ,  C07D213/89 ,  C07D401/12

Abstract: Propanoic acid derivatives of formula (1) are described: Ar-X -Ar -Z-R; in which Ar is a nitrogen base containing group; X is a linker atom or group; Ar is an optionally substituted pyridine or pyridine-N-oxide; Z is a group -CH(R )CH2- [in which R is R or Alk R , R is a hydrogen atom or an optionally substituted aliphatic, cycloaliphatic heteroaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group and Alk is an optionally substituted C1-3alkylene chain], -C(R )(R )-CH(R )- [in which R and R together with the carbon atoms to which they are attached form a C3-7cycloalkyl group] or -C(R )=CH-; R is a carboxylic acid (-CO2H) or a derivative or biostere thereof; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.

Abstract translation: 式（1）的丙酸衍生物描述为：Ar-X 1 -Ar 1 -Z-R; 其中Ar是含氮碱基团; X 1是接头原子或基团; Ar 1是任选取代的吡啶或吡啶-N-氧化物; Z为基团-CH（R 13）CH 2 - [其中R 13为R 13a或Alk 1a R 13a，R 13a为氢原子或任选取代的脂族基团， 脂环族杂脂族基，杂环脂族基，芳族或杂芳族基团且Alk 1a为任选取代的C 1-3亚烷基链]，-C（R 12a）（R 13）-CH（R 12b） - [ R 12a和R 12b与它们所连接的碳原子一起形成C 3-7环烷基]或-C（R 13）= CH-; R是羧酸（-CO 2 H）或其衍生物或生物等排物; 及其盐，溶剂化物，水合物和N-氧化物。 该化合物能够抑制整联蛋白与其配体的结合，并且可用于预防和治疗免疫或炎性疾病。

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：CA2409617A1

公开(公告)日：2001-12-06

申请号：CA2409617

申请日：2001-05-30

Applicant: CELLTECH R&D LTD

Inventor： LANGHAM BARRY JOHN ,  HEAD JOHN CLIFFORD ,  WARRELLOW GRAHAM JOHN ,  LINSLEY JANEEN MARSHA ,  PORTER JOHN ROBERT ,  ARCHIBALD SARAH CATHERINE ,  ALEXANDER RIKKI PETER

IPC: C07D487/08 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  A61K31/551 ,  A61P1/04 ,  A61P3/10 ,  A61P11/06 ,  A61P17/06 ,  A61P19/02 ,  A61P25/28 ,  A61P29/00 ,  A61P37/00 ,  A61P37/06 ,  A61P43/00 ,  C07D471/04 ,  C07D519/00 ,  C07D221/00 ,  A61K31/435

Abstract: 2,7-Naphthyridine containing squaric acids of formula (1) are described, wherein Ar1 is an optionally substituted 2,7-naphthridin-1-yl group; L2 is a covalent bond or a linker atom or group; Ar2 is an optionally substituted aromatic or heteroaromatic chain; Alk is a chain (2) in which R is a carboxylic acid (-CO2H) or a derivative or biostere thereof; R1 is a hydroge n atom or a C1-6alkyl group; L1 is a covalent bond or a linker atom or group; Alk1 is an optionally substituted aliphatic chain; n is zero or the integer 1; R2 is a hydrogen atom or an optionally substituted heteroaliphatic, cycloaliphatic, heterocycloaliphatic, polycycloaliphatic, heteropolycycloaliphatic, aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit t he binding of integrins to their ligands and are of use in the prophylaxis and treatment of immuno or inflammatory disorders or disorders involving the inappropriate growth or migration of cells.

公开(公告)号：CA2375218A1

公开(公告)日：2000-12-07

申请号：CA2375218

申请日：2000-05-26

Applicant: CELLTECH R&D LTD

Inventor： LANGHAM BARRY JOHN ,  PORTER JOHN ROBERT ,  LINSLEY JANEEN MARSHA ,  HEAD JOHN CLIFFORD ,  ALEXANDER RIKKI PETER ,  ARCHIBALD SARAH CATHERINE ,  WARRELLOW GRAHAM JOHN

IPC: A61K31/198 ,  A61K31/223 ,  A61K31/381 ,  A61K31/4375 ,  A61K31/4409 ,  A61K31/472 ,  A61K31/505 ,  A61P7/00 ,  A61P29/00 ,  A61P37/00 ,  A61P43/00 ,  C07B61/00 ,  C07C229/34 ,  C07C229/36 ,  C07C233/55 ,  C07C233/81 ,  C07C235/16 ,  C07C235/24 ,  C07C235/56 ,  C07C235/64 ,  C07C235/84 ,  C07C237/40 ,  C07C255/57 ,  C07C271/22 ,  C07C271/28 ,  C07C271/58 ,  C07D213/79 ,  C07D213/81 ,  C07D215/42 ,  C07D217/22 ,  C07D239/34 ,  C07D239/42 ,  C07D239/88 ,  C07D239/94 ,  C07D241/42 ,  C07D241/44 ,  C07D295/135 ,  C07D333/40 ,  C07D333/70 ,  C07D471/04 ,  C07D295/12 ,  A61K31/122 ,  A61K31/44

Abstract: Squaric acid Derivatives of formula (1) are described: wherein R1 is an integrin binding group; R2 is a hydrogen atom or a C1-6 alkyl group; L1 is a covalent bond or a linker atom or group; n is zero or the integer 1; Alk1 is an optionally substituted aliphatic chain; R3 is a hydrogen atom or an optionally substituted heteroaliphatic, cycloaliphatic, heterocycloaliphatic , polycycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group: and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders, or disorders involving the inappropriate growth or migration of cells.

公开(公告)号：MXPA05013227A

公开(公告)日：2006-03-09

申请号：MXPA05013227

申请日：2004-06-18

Applicant: CELLTECH R&D LTD

Inventor： LANGHAM BARRY JOHN

IPC: A61K31/4365 ,  A61P29/00 ,  C07D495/04

Abstract: Se describe una serie de derivaos de tieno[2,3-b]piridin-6(7H)-ona, sustituidos en la posicion 2 por una porcion pirrolidin-1-ilo enlazada a carbonilo o sulfonilo o porcion relacionada, los cuales son inhibidores de p38 MAP cinasa, y son en consecuencia de utilizad en medicina, por ejemplo en el tratamiento y/o prevencion de trastornos inmunes o inflamatorios.

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：ES2223639T3

公开(公告)日：2005-03-01

申请号：ES00987574

申请日：2000-12-22

Applicant: CELLTECH R&D LTD

Inventor： LANGHAM BARRY JOHN ,  ALEXANDER RIKKI PETER ,  HEAD JOHN CLIFFORD ,  LINSLEY JANEEN MARSHA ,  PORTER JOHN ROBERT ,  ARCHIBALD SARAH CATHERINE

IPC: C07C229/34 ,  C07C229/36 ,  C07D471/04 ,  C07C225/20 ,  C07C229/46 ,  C07D295/12 ,  A61K31/13 ,  A61K31/435 ,  A61P29/00

Abstract: Un compuesto de fórmula (1): en la que R1 es un grupo Ar1Ar2Alk- en el que: Ar1 es un grupo aromático o heteroaromático opcionalmente sustituido; Ar2 es un grupo fenileno opcionalmente sustituido o un grupo heteroarileno de seis miembros que contiene nitrógeno; y Alk es una cadena en la que R es un ácido carboxílico (-CO2H) o un derivado o bióstero del mismo; R2 es un átomo de hidrógeno o un grupo alquilo C1-6; L1 es un enlace covalente o un átomo o grupo de engarce; n es cero o el número entero 1; Alk1 es una cadena alifática opcionalmente sustituida; R3 es un átomo de hidrógeno o un grupo heteroalifático, cicloalifático, heterocicloalifático, policicloalifático, heteropolicicloalifático, aromático o heteroaromático opcionalmente sustituido; y las sales, solvatos, hidratos y N-óxidos del mismo.

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.