Patent ID: 6217848
Filing Date: 2001-04-17
Classification: A61K

Abstract:
A composition comprising a cyanine dye bioconjugate of formula, ##STR3##wherein a and b are independently any value from 0 to 5; W.sup.1 and X.sup.1 are the same or different and are selected from the group consisting of --CR.sup.10 R.sup.11 ; Q.sup.1 is a single bond or is selected from the group consisting of --O--, --S--, --Se--, and --NR.sup.13 ; R.sup.1, R.sup.10, R.sup.11, R.sup.13, R.sup.31 -R.sup.34, R.sup.36 -R.sup.38 and R.sup.40 are the same or different from the group consisting of hydrogen, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxyl, C.sub.1 -C.sub.10 polyalkoxyalkyl, --CH.sub.2 (CH.sub.2 OCH.sub.2).sub.c --CH.sub.2 --OH, C.sub.1 -C.sub.20 polyhydroxyalkyl, C.sub.1 -C.sub.10 aminoalkyl, --(CH.sub.2).sub.d --CO.sub.2 H, --(CH.sub.2).sub.e --CONH-Bm, --CH.sub.2 --(CH.sub.2 OCH.sub.2).sub.f --CH.sub.2 --CONH-Bm, --(CH.sub.2).sub.g --NHCO-Bm, --CH.sub.2 --(CH.sub.2 OCH.sub.2).sub.h --CH.sub.2 --NHCO-Bm, --(CH.sub.2).sub.yy --OH or --CH.sub.2 --(CH.sub.2 OCH.sub.2).sub.zz --CH.sub.2 --OH; Y.sup.1 is selected from the group consisting of --CH.sub.2 --(CH.sub.2 OCH.sub.2).sub.j --CH.sub.2 --CONH-Bm, --CH.sub.2 --(CH.sub.2 OCH.sub.2).sub.l --CH.sub.2 --NHCO-Bm, --CH.sub.2 --(CH.sub.2 OCH.sub.2).sub.ee --CH.sub.2 --N(R.sup.31)--(CH.sub.2).sub.ff --CONH-Bm, --CH.sub.2 --(CH.sub.2 OCH.sub.2).sub.gg --CH.sub.2 --N(R.sup.32)--(CH.sub.2).sub.hh --NHCO-Bm, --CH.sub.2 --(CH.sub.2 OCH.sub.2).sub.ii --CH.sub.2 --N(R.sup.33)--CH.sub.2 --(CH.sub.2 OCH.sub.2).sub.jj --CH.sub.2 --CONH-Bm or --CH.sub.2 --(CH.sub.2 OCH.sub.2).sub.kk --CH.sub.2 --N(R.sup.34)--CH.sub.2 --(CH.sub.2 OCH.sub.2).sub.ll --CH.sub.2 --NHCO-Bm; d, e, g, i, k, m, n, p, aa, bb, cc, ff, hh and yy are independently any value from 1 to 10; c, f, h, j, l, q, dd, ee, gg, ii, jj, kk, ll and zz are independently any value from 1 to 100; Bm is octreotate; Z.sup.1 is selected from the group consisting of --CH.sub.2 --(CH.sub.2 OCH.sub.2).sub.s --CH.sub.2 --CO.sub.2 H, --CH.sub.2 --(CH.sub.2 OCH.sub.2).sub.s --CH.sub.2 --OH, --CH.sub.2 --(CH.sub.2 OCH.sub.2).sub.s --CH.sub.2 --NH.sub.2, --CH.sub.2 --(CH.sub.2 OCH.sub.2).sub.u --CH.sub.2 --CONH-Dm, --CH.sub.2 --(CH.sub.2 OCH.sub.2).sub.o --CH.sub.2 --NHCO-Dm, --CH.sub.2 --(CH.sub.2 OCH.sub.2).sub.ww --CH.sub.2 --N(R.sup.40)--(CH.sub.2).sub.xx --CONH-Dm, --CH.sub.2 --(CH.sub.2 OCH.sub.2).sub.oo --CH.sub.2 --N(R.sup.36)--(CH.sub.2).sub.pp --NHCO-Dm, --CH.sub.2 --(CH.sub.2 OCH.sub.2).sub.qq --CH.sub.2 --N(R.sup.37)--CH.sub.2 --(CH.sub.2 OCH.sub.2).sub.rr --CH.sub.2 --CONH-Dm or --CH.sub.2 --(CH.sub.2 OCH.sub.2).sub.ss --CH.sub.2 --N(R.sup.38)--CH.sub.2 --(CH.sub.2 OCH.sub.2).sub.tt --CH.sub.2 --NHCO-Dm; r, t, v, w, x, y, mm, nn, pp, uu and xx are independently any value from 1 to 10, and o, s, u, z, oo, qq, rr, ss, tt, vv and ww are independently any value from 1 to 100; and Dm is octreotate; R.sup.2 to R.sup.9 are the same or different and are selected from the group consisting of hydrogen, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 aryl, hydroxyl, C.sub.1 -C.sub.10 polyhydroxyalkyl, C.sub.1 -C.sub.10 alkoxyl, amino, C.sub.1 -C.sub.10 aminoalkyl, cyano, nitro, or halogen; wherein said composition further comprises a pharmaceutically acceptable carrier or excipient.