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    2.
    发明专利
    未知

    公开(公告)号：DE60011940D1

    公开(公告)日：2004-08-05

    申请号：DE60011940

    申请日：2000-12-22

    Applicant: CELLTECH R&D LTD

    Inventor： LANGHAM JOHN ,  ALEXANDER PETER ,  HEAD CLIFFORD ,  LINSLEY MARSHA ,  PORTER ROBERT ,  ARCHIBALD CATHERINE ,  WARRELLOW JOHN

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

    Abstract: Squaric acid derivatives of formula (1) are described:whereinR1 is a group Ar1Ar2Alk- in whichAr1 is an optionally substituted aromatic or heteroaromatic group;Ar2 is an optionally substituted phenylene or nitrogen-containing six-membered heteroarylene group; and Alk is a chain-CH2-CH(R)-, -CH=C(R)-,in which R is a carboxylic acid (-CO2H) or a derivative or biostere thereof;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, heteropolycycloaliphatic, 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.

    3.
    发明专利
    未知

    公开(公告)号：DE60011940T2

    公开(公告)日：2005-07-21

    申请号：DE60011940

    申请日：2000-12-22

    Applicant: CELLTECH R&D LTD

    Inventor： LANGHAM JOHN ,  ALEXANDER PETER ,  HEAD CLIFFORD ,  LINSLEY MARSHA ,  PORTER ROBERT ,  ARCHIBALD CATHERINE ,  WARRELLOW JOHN

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

    Abstract: Squaric acid derivatives of formula (1) are described:whereinR1 is a group Ar1Ar2Alk- in whichAr1 is an optionally substituted aromatic or heteroaromatic group;Ar2 is an optionally substituted phenylene or nitrogen-containing six-membered heteroarylene group; and Alk is a chain-CH2-CH(R)-, -CH=C(R)-,in which R is a carboxylic acid (-CO2H) or a derivative or biostere thereof;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, heteropolycycloaliphatic, 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.

    4.
    发明专利
    未知

    公开(公告)号：DE69628853D1

    公开(公告)日：2003-07-31

    申请号：DE69628853

    申请日：1996-12-20

    Applicant: CELLTECH R&D LTD

    Inventor： HEAD CLIFFORD ,  REUBERSON THOMAS

    IPC: A61K31/00 ,  A61K31/44 ,  A61K31/4409 ,  A61P1/00 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P13/00 ,  A61P13/12 ,  A61P17/00 ,  A61P19/00 ,  A61P19/02 ,  A61P29/00 ,  A61P43/00 ,  C07D213/40 ,  C07D213/64 ,  C07D213/74 ,  C07D213/62 ,  C07D311/60

    Abstract: Tri-substituted phenyl derivatives and pharmaceutical compositions containing them. In a preferred embodiment, the compounds have the general formula (2): (2) wherein L is preferably -OR; Ra is preferably an optionally substituted alkyl group; R is preferably an optionally substituted cycloalkyl group; R3 is preferably hydrogen; hydrogen, R4 is preferably -(CH2)tAr, -(CH2)t-Ar-(L1)n-Ar' or -(CH2)tArN(Rb)CX1N(Rb)L2(Alk)mAr; R5 is preferably -(CH2)tAr, -(CH2)t-Ar-(L1)n-Ar' or -(CH2)tArN(Rb)CX1N(Rb)L2(Alk)mAr; R6 and R7 are preferably hydrogen, L1 and L2 are preferably divalent linking groups; Ar is preferably a monocyclic or bicyclic aryl or heteroaryl group; and Ar' is preferably Ar or an Ar containing group. Compounds of the invention are potent and selective phosphodiesterase type IV inhibitors and are useful in the prophylaxis and treatment of various diseases, such as asthma, which are associated with an unwanted inflammatory response or muscular spasm.

    5.
    发明专利
    未知

    公开(公告)号：DE69628853T2

    公开(公告)日：2004-05-06

    申请号：DE69628853

    申请日：1996-12-20

    Applicant: CELLTECH R&D LTD

    Inventor： HEAD CLIFFORD ,  REUBERSON THOMAS

    IPC: A61K31/00 ,  A61K31/44 ,  A61K31/4409 ,  A61P1/00 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P13/00 ,  A61P13/12 ,  A61P17/00 ,  A61P19/00 ,  A61P19/02 ,  A61P29/00 ,  A61P43/00 ,  C07D213/40 ,  C07D213/64 ,  C07D213/74 ,  C07D213/62 ,  C07D311/60

    Abstract: Tri-substituted phenyl derivatives and pharmaceutical compositions containing them. In a preferred embodiment, the compounds have the general formula (2): (2) wherein L is preferably -OR; Ra is preferably an optionally substituted alkyl group; R is preferably an optionally substituted cycloalkyl group; R3 is preferably hydrogen; hydrogen, R4 is preferably -(CH2)tAr, -(CH2)t-Ar-(L1)n-Ar' or -(CH2)tArN(Rb)CX1N(Rb)L2(Alk)mAr; R5 is preferably -(CH2)tAr, -(CH2)t-Ar-(L1)n-Ar' or -(CH2)tArN(Rb)CX1N(Rb)L2(Alk)mAr; R6 and R7 are preferably hydrogen, L1 and L2 are preferably divalent linking groups; Ar is preferably a monocyclic or bicyclic aryl or heteroaryl group; and Ar' is preferably Ar or an Ar containing group. Compounds of the invention are potent and selective phosphodiesterase type IV inhibitors and are useful in the prophylaxis and treatment of various diseases, such as asthma, which are associated with an unwanted inflammatory response or muscular spasm.

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