公开(公告)号：JP2009057371A

公开(公告)日：2009-03-19

申请号：JP2008188089

申请日：2008-07-22

Applicant: Celltech R & D Ltd ,  セルテック アール アンド ディ リミテッド

Inventor： BAILEY STUART ,  BROWN JULIEN ALISTAIR ,  BRAND STEPHEN ,  JOHNSON JAMES ANDREW ,  PORTER JOHN ROBERT ,  HEAD JOHN CLIFFORD

IPC: C07C229/36 ,  A61K31/198 ,  A61K31/223 ,  A61K31/352 ,  A61K31/4375 ,  A61K31/44 ,  A61K31/4406 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/497 ,  A61P1/04 ,  A61P3/10 ,  A61P9/00 ,  A61P11/06 ,  A61P17/00 ,  A61P17/02 ,  A61P17/06 ,  A61P19/02 ,  A61P25/00 ,  A61P29/00 ,  A61P37/00 ,  A61P37/06 ,  A61P43/00 ,  C07C229/34 ,  C07C229/46 ,  C07C233/81 ,  C07C233/82 ,  C07C321/22 ,  C07C323/30 ,  C07D213/81 ,  C07D213/89 ,  C07D311/96 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D471/04

CPC classification number: C07D213/81 ,  C04B35/632 ,  C07C229/10 ,  C07C229/46 ,  C07C233/81 ,  C07C233/82 ,  C07C323/30 ,  C07C2601/04 ,  C07C2603/94 ,  C07C2603/96 ,  C07D213/79 ,  C07D213/89 ,  C07D311/96 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D471/04

Abstract: PROBLEM TO BE SOLVED: To provide a compound inhibiting the binding of integrin with a ligand and useful in the prevention and treatment of immune or inflammatory diseases associated with inappropriate cell proliferation or migration. SOLUTION: The compound is represented by formula (1) and is exemplified by 3-oxocyclobut-1-enylamino-group-containing methyl(2S)-2-ä(3-oxospiro[3,5]-non-1-en-1-yl)amino}-3-(2,6-dimethoxy[1,1'-biphenyl]-4-yl)propanoate. COPYRIGHT: (C)2009,JPO&INPIT

Abstract translation: 要解决的问题：提供抑制整联蛋白与配体结合并可用于预防和治疗与不适当细胞增殖或迁移相关的免疫或炎性疾病的化合物的问题。 解决方案：化合物由式（1）表示，并且例示为含有3-氧代环丁-1-烯基氨基的（2S）-2-（3-氧代螺[3,5] - 壬-1 丁-1-基）氨基} -3-（2,6-二甲氧基[1,1'-联苯] -4-基）丙酸乙酯。 版权所有（C）2009，JPO＆INPIT

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：WO2005117984A2

公开(公告)日：2005-12-15

申请号：PCT/GB2005002084

申请日：2005-05-25

Applicant: CELLTECH R&D LTD ,  EATON MICHAEL ANTHONY WILLIAM ,  NORMAN TIMOTHY JOHN ,  PORTER JOHN ROBERT

Inventor： EATON MICHAEL ANTHONY WILLIAM ,  NORMAN TIMOTHY JOHN ,  PORTER JOHN ROBERT

IPC: A61K47/48

CPC classification number: A61K47/542 ,  A61K47/60

Abstract: The present invention provides an albumin-binding compound essentially of the following elements: a spacer group, a water-soluble bridging group, a fatty acid chain and an acidic group characterised in that the acidic group is attached to the distal end of the fatty acid chain. The invention also provides an albumin-binding compound to which one or more biologically active moieties are attached.

Abstract translation: 本发明提供了基本上具有以下元素的白蛋白结合化合物：间隔基，水溶性桥连基团，脂肪酸链和酸性基团，其特征在于酸性基团连接到脂肪酸的末端 链。 本发明还提供了与一个或多个生物活性部分连接的白蛋白结合化合物。

公开(公告)号：DE60218436D1

公开(公告)日：2007-04-12

申请号：DE60218436

申请日：2002-01-18

Applicant: CELLTECH R&D LTD

Inventor： BAILEY SLOUGH ,  BROWN JULIEN ALISTAIR ,  BRAND SLOUGH ,  JOHNSON JAMES ANDREW ,  PORTER JOHN ROBERT ,  HEAD JOHN CLIFFORD

IPC: C07D213/81 ,  A61K31/198 ,  A61K31/4375 ,  A61K31/44 ,  A61K31/4406 ,  A61K31/497 ,  A61P3/10 ,  A61P9/00 ,  A61P17/00 ,  A61P17/06 ,  A61P19/02 ,  A61P25/00 ,  A61P29/00 ,  A61P37/00 ,  A61P37/06 ,  A61P43/00 ,  C07C229/34 ,  C07C229/36 ,  C07C229/46 ,  C07C233/82 ,  C07C321/22 ,  C07C323/30 ,  C07D213/89 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D471/04

Abstract: Phenylalanine enamide derivatives of formula (1) are described: wherein R 1 , R x , R y , R z , X and V are as defined in claim 1. The compounds are able to inhibit the 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：HK1059087A1

公开(公告)日：2004-06-18

申请号：HK04102092

申请日：2004-03-22

Applicant: CELLTECH R&D LTD

Inventor： BAILEY STUART ,  BROWN JULIEN ALISTAIR ,  BRAND STEPHEN ,  JOHNSON JAMES ANDREW ,  PORTER JOHN ROBERT ,  HEAD JOHN CLIFFORD

IPC: C07D20060101 ,  A61K31/198 ,  A61K31/4375 ,  A61K31/44 ,  A61K31/4406 ,  A61K31/497 ,  A61P20060101 ,  A61P3/10 ,  A61P9/00 ,  A61P17/00 ,  A61P17/06 ,  A61P19/02 ,  A61P25/00 ,  A61P29/00 ,  A61P37/00 ,  A61P37/06 ,  A61P43/00 ,  C07C20060101 ,  C07C229/34 ,  C07C229/46 ,  C07C233/82 ,  C07C321/22 ,  C07C323/30 ,  C07D213/81 ,  C07D213/89 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D471/04

Abstract: Phenylalanine enamide derivatives of formula (1) are described: wherein R 1 , R x , R y , R z , X and V are as defined in claim 1. The compounds are able to inhibit the 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：BR0207166A

公开(公告)日：2004-02-10

申请号：BR0207166

申请日：2002-01-18

Applicant: CELLTECH R&D LTD

Inventor： BAILEY STUART ,  BROWN JULIEN ALISTAIR ,  BRAND STEPHEN ,  JOHNSON JAMES ANDREW ,  PORTER JOHN ROBERT ,  HEAD JOHN CLIFFORD

IPC: A61K31/198 ,  A61K31/4375 ,  A61K31/44 ,  A61K31/4406 ,  A61K31/497 ,  A61P3/10 ,  A61P9/00 ,  A61P17/00 ,  A61P17/06 ,  A61P19/02 ,  A61P25/00 ,  A61P29/00 ,  A61P37/00 ,  A61P37/06 ,  A61P43/00 ,  C07C229/34 ,  C07C229/46 ,  C07C233/82 ,  C07C321/22 ,  C07C323/30 ,  C07D213/81 ,  C07D213/89 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D471/04 ,  C07C229/36

Abstract: Phenylalanine enamide derivatives of formula (1) are described: wherein R 1 , R x , R y , R z , X and V are as defined in claim 1. The compounds are able to inhibit the 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：NO20033710A

公开(公告)日：2003-10-22

申请号：NO20033710

申请日：2003-08-20

Applicant: CELLTECH R&D LTD

Inventor： BAILEY STUART ,  BROWN JULIEN ALISTAIR ,  BRAND STEPHEN ,  JOHNSON JAMES ANDREW ,  PORTER JOHN ROBERT ,  HEAD JOHN CLIFFORD

IPC: A61K31/198 ,  A61K31/4375 ,  A61K31/44 ,  A61K31/4406 ,  A61K31/497 ,  A61P3/10 ,  A61P9/00 ,  A61P17/00 ,  A61P17/06 ,  A61P19/02 ,  A61P25/00 ,  A61P29/00 ,  A61P37/00 ,  A61P37/06 ,  A61P43/00 ,  C07C229/34 ,  C07C229/46 ,  C07C233/82 ,  C07C321/22 ,  C07C323/30 ,  C07D213/81 ,  C07D213/89 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D471/04

CPC classification number: C07D213/81 ,  C04B35/632 ,  C07C229/10 ,  C07C229/46 ,  C07C233/81 ,  C07C233/82 ,  C07C323/30 ,  C07C2601/04 ,  C07C2603/94 ,  C07C2603/96 ,  C07D213/79 ,  C07D213/89 ,  C07D311/96 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D471/04

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：DE60218436T2

公开(公告)日：2007-10-31

申请号：DE60218436

申请日：2002-01-18

Applicant: CELLTECH R&D LTD

Inventor： BAILEY SLOUGH ,  BROWN JULIEN ALISTAIR ,  BRAND SLOUGH ,  JOHNSON JAMES ANDREW ,  PORTER JOHN ROBERT ,  HEAD JOHN CLIFFORD

IPC: C07D213/81 ,  A61K31/198 ,  A61K31/4375 ,  A61K31/44 ,  A61K31/4406 ,  A61K31/497 ,  A61P3/10 ,  A61P9/00 ,  A61P17/00 ,  A61P17/06 ,  A61P19/02 ,  A61P25/00 ,  A61P29/00 ,  A61P37/00 ,  A61P37/06 ,  A61P43/00 ,  C07C229/34 ,  C07C229/36 ,  C07C229/46 ,  C07C233/82 ,  C07C321/22 ,  C07C323/30 ,  C07D213/89 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D471/04

Abstract: Phenylalanine enamide derivatives of formula (1) are described: wherein R 1 , R x , R y , R z , X and V are as defined in claim 1. The compounds are able to inhibit the 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.