Methods for inhibiting angiogenesis and tumor growth

Details Methods for inhibiting angiogenesis and tumor growth Methods for inhibiting angiogenesis and tumor growth

2006-10-03

2006-10-03

Pryor, Alton (Department: 1616)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

N-c doai

C514S483000, C514S506000, C514S532000, C514S613000, C514S617000

Reexamination Certificate

active

07115660

ABSTRACT:
Angiogenesis, tumor growth, and metalloproteinase 2 (MMP2) interaction with integrin-αvβ3are inhibited by an inhibitor compound of formula (I): wherein G1and G2are each independently NH—C(O)—O—R1, —NH—C(O)—O—(CH2)v—(C6H4)—X3, —NH—C(O)—NH—(CH2)v—(C6H4)—X3, —O—C(O)—NH—(CH2)v—(C6H4)—X3, —O—C(O)—O—(CH2)v—(C6H4)—X3, or NH—C(O)—CH2—(C6H4)—X3; Y1and Y2are each independently OH, C1–C4alkyl, C1–C4hydroxyalkyl, C1–C4alkoxy, phenyl, benzyl, or NH2; R1is C1–C4alkyl; X1and X2are each independently halo or C1–C4alkoxy; X3is halo, nitro, C1–C4alkyl, C1–C4alkoxy, or C1–C4perfluoroalkyl; Z is —C≡C—, —C6H4—, cis-CH═CH—, trans CH═CH—, cis-CH2—CH═CH—CH2—, trans —CH2—CH═CH—CH2—, 1,4-naphthyl, cis-1,3-cyclohexyl, trans-1, 3-cyclohexyl, cis-1,4-cyclohexyl, or trans-1,4-cyclohexyl; A is H or a covalent bond; m and n are each independently an integer having a value of 0 or 1; t is an integer having a value of 0 or 1; and p, r, and v are each independently an integer having a value of 1 or 2; with provisos that when A is H, t is O; when A is a covalent bond, t is 1; when m is 0, Y1is C1–C4hydroxyalkyl; and when n is 0, Y2is C1C4hydroxyalkyl.

REFERENCES:
Kitoh et al, MMP2 and its activator membrane type 1-matrix metalloproteinase, J. Cell Sci., 109, 953-8, 1986.

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