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Thrombopoietic compounds

  • US 20080070840A1
  • Filed: 06/18/2007
  • Published: 03/20/2008
  • Est. Priority Date: 06/19/2006
  • Status: Active Grant
First Claim
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1. A compound that binds to an mp1 receptor comprising a structure set out in Formula I,
[(X1)a

  • (F1)z

    (X2)b]-(L1)c-WSPd



    Formula I and multimers thereof, wherein;

    F1 is a vehicle;

    X1 is independently selected from;

    P1-(L2)e- P2-(L3)f-P1-(L2)e- P3-(L4)g-P2-(L3)f-P1-(L2)e- and P4-(L5)h-P3-(L4)g-P2-(L3)f-P1-(L2)e- X2 is independently selected from;

    -(L2)e-P1, -(L2)e-P1-(L3)f-P2, -(L2)e-P1-(L3)f-P2-(L4)g-P3, and -(L2)e-P1-(L3)f-P2-(L4)g-P3-(L5)h-P4 wherein P1, P2, P3, and P4 are each independently sequences of pharmacologically active peptides;

    L1, L2, L3, L4, and L5 are each independently linkers;

    a, b, c, d, e, f, g, and h are each independently 0 or 1;

    z is 0, 1, 2, or more; and

    WSP is a water soluble polymer, the attachment of which is effected at any reactive moiety in F1;

    wherein P is a molecule comprising the structure U1-Y1-Y2-Y3-Y4-Y5-Y6-Y7-U2 wherein U1-Y1(Cys, Leu, Met, Pro, Gln, Val, or X1)-Y2 (Phe, Lys, Leu, Asn, Gln, Arg, Ser, Thr, Val, or X2)-Y3(Cys, Phe, Ile, Leu, Met, Arg, Ser, Val, Trp, or X3)-Y4-Y5(Ala, Asp, Glu, Gly, Lys, Met, Gln, Arg, Ser, Thr, Val, Tyr, or XS)-Y6(Cys, Phe, Gly, Leu, Met, Ser, Val, Trp, Tyr, or X6)-Y7(Cys, Gly, Ile, Lys, Leu, Met, Asn, Arg, Val, or X7)-U2, wherein at least one of Y1-Y3 and Y5-Y7 corresponds to a respective X1-X3 and X5-X7;

    wherein U1 or U2 is any amino acid or peptide;

    wherein when Y1 is not an amino acid selected from the group consisting of Cys, Leu, Met, Pro, Gln, and Val, then X1 is selected from the group consisting of Ala, Asp, Glu, Phe, Gly, His, Ile, Lys, Asn, Arg, Ser, Thr, Trp, and Tyr;

    wherein when Y2 is not an amino acid selected from the group consisting of Phe, Lys, Leu, Asn, Gln, Arg, Ser, Thr, and Val, then X2 is selected from the group consisting of Ala, Cys, Asp, Glu, Gly, His, Ile, Met, Pro, Trp, and Tyr;

    wherein when Y3 is not an amino acid selected from the group consisting of Cys, Phe, Ile, Leu, Met, Arg, Ser, Val, and Trp, then X3 is selected from the group consisting of Ala, Asp, Glu, Gly, His, Lys, Asn, Pro, Gln, Thr, and Tyr;

    wherein when Y4 is any amino acid;

    wherein when Y5 is not an amino acid selected from the group consisting of Ala, Asp, Glu, Gly, Lys, Met, Gln, Arg, Ser, Thr, Val, and Tyr, then X5 is selected from the group consisting of Cys, Phe, His, Ile, Leu, Asn, Pro, and Trp;

    wherein when Y6 is not an amino acid selected from the group consisting of Cys, Phe, Gly, Leu, Met, Ser, Val, Trp, and Tyr, then X6 is selected from the group consisting of Ala, Asp, Glu, His, Ile, Lys, Asn, Pro, Gln, Arg, and Thr; and

    wherein when Y7 is not an amino acid selected from the group consisting of Cys, Gly, Ile, Lys, Leu, Met, Asn, Arg, and Val, then X7 is selected from the group consisting of Ala, Asp, Glu, Phe, His, Pro, Gln, Ser, Thr, Trp, and Tyr;

    and physiologically acceptable salts thereof.

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