公开(公告)号：NZ537740A

公开(公告)日：2006-03-31

申请号：NZ53774003

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: Disclosed are compounds of the formula (I), wherein The dashed line joining A and C(Ra) is present and represents a bond, and A is a ûC(Rb)= group, or the dashed line is absent and A is a ûC(Rb)(Rc)- group; R is H or a straight or branched C1-6- alkyl group; X is an ûO- or ûS- atom; Y is a N or substituted C atom or a ûCH= group; N is 0 or 1; Alk1 is an optionally substituted aliphatic or heteroaliphatic chain; L1 is a covalent bond or a linker atom or group; Cy1 is a H or an optionally a substituted cycloaliphatic, poly cycloaliphatic, hetereocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; Ar is an optionally substituted aromatic or heteroaromatic group; And the salts, solvates, hydrates and N-oxides thereof. Further disclosed are pharmaceutical compositions comprising a compound of formula (I); and the use of one of the compounds of the invention for the manufacture of a medicament for the treatment of rheumatoid arthritis.

公开(公告)号：NO20041975L

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

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：ECSP055560A

公开(公告)日：2005-05-30

申请号：ECSP055560

申请日：2005-01-20

Applicant: CELLTECH R&D LTD

Inventor： BROOKINGS DANIEL CHRISTOPHER ,  DAVIS JEREMY MARTIN

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 ,  A61P29 ,  A61P37

Abstract: Se describen derivados heteroaromáticos bicíclicos de fórmula (1): donde:la línea discontinua que une a A y C(Ra) está presente y representa un enlace yA es un átomo -N= o un grupo -C(Rb)=, o la línea discontinua está ausente y A es un grupo -N(Rb)-, o -C(Rb)(Rc)-;X es un átomo de -O-, -S- o de nitrógeno sustituido o un grupo -S(O)-, -S(O2)- o -NH-;Y es un átomo de nitrógeno o de carbono sustituido o un grupo -CH=;n es cero o el número entero 1;Alk1 es una cadena alifática o heteroalifática opcionalmente sustituidaL1 es un enlace covalente o un átomo o grupo de unión;Cy1 es un átomo de hidrógeno o un grupo cicloalifático, policicloalifático, heterocicloalifático, poliheterocicloalifático, aromático o heteroaromático opcionalmente sustituido;Ar es un grupo aromático o heteroaromático opcionalmente sustituido; y los sustituyentes restantes fueron definidos en la especificación.Los compuestos son inhibidores selectivos y potentes de la quinasa p38 y son útiles en la profilaxis y el tratamiento de los trastornos inmunitarios o inflamatorios.

公开(公告)号：IS7652A

公开(公告)日：2005-01-18

申请号：IS7652

申请日：2005-01-18

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

公开(公告)号：AU2004249498A1

公开(公告)日：2004-12-29

申请号：AU2004249498

申请日：2004-06-18

Applicant: CELLTECH R&D LTD

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

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

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 accordingly of use in medicine, for example in the treatment and/or prevention of immune or inflammatory disorders.

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.