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US 7,030,123 B2Granted
Indole derivatives with vascular damaging activity
AssigneeAstraZeneca AB
InventorsJean-Claude Arnould, Thomas Geoffrey Bird, Francis Thomas Boyle, David Charles Blakey
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Abstract
The invention provides a compound of Formula (I). Wherein R1, R2, R3, R10 and R11 have the meanings given in the description. Such compounds are predicted to cause the selective destruction of tumour vasculature. They may therefore be used to inhibit and/or reverse, and/or alleviate symptoms of angiogenesis and/or any disease state associated with angiogenesis.
Claims10
A compound of Formula (I):
- wherein R1 is a group of Formula (II):
- wherein W is an aryl or a heterocyclic group;
- R4 is independently selected from —OH, amino, —OPO3H2, and a lower alkanoylamino group, wherein the amino group is optionally substituted by an amino acid residue and the hydroxy group is optionally esterified;
- X is selected from —S—, —O—, —S(O)—, —S(O2)—, and —NH—;
- p is an integer from 0 to 4;
- and
- q is an integer from 1 to 4;
- R2 is selected from hydrogen, halogen, and a lower alkyl group;
- R3 and R10 are independently selected from hydrogen, lower alkyl, and a group of Formula (IV):
- wherein Y is selected from —NH—, —O—, and a bond;
- Z is selected from —NH—, —O—, —C(O)—, and a bond;
- r is an integer from 0 to 4;
- t is an integer from 0 to 1;
- R6 is hydrogen, lower alkyl, a lower alkoxy group, an aryl group, a heterocyclic group or a group of Formula (V), wherein the aryl group and heterocyclic group are optionally substituted by lower alkyl or a lower alkanoyl group:
- wherein n is an integer of from 1 to 6;
- R7 and R8 are independently selected from hydrogen and an alkaryl group;
- and
- R11 is hydrogen or lower alkyl;
- or a pharmaceutically acceptable salt, or solvate thereof.
16 more elements
A compound of Formula (I):
- wherein:
- R1 is a group of Formula (II):
- wherein W is aryl or a heterocyclic group,
- R4 is independently selected from hydrogen, fluoro, —OH, amino, —OPO3H2, a lower alkanoylamino group, and a lower alkoxy group, wherein the amino group is optionally substituted by an amino acid residue and the hydroxy group is optionally esterified;
- X is selected from —S(O)—, —S(O2)— and —Nh—;
- p is an integer from 0 to 4;
- and
- q is an integer from 1 to 4;
- R2 is selected from:
- hydrogen, halogen and a lower alkyl group;
- R3 and R10 are independently selected from hydrogen, lower alkyl and a group of Formula (IV):
- wherein Y is selected from —NH—, —O— and a bond;
- Z is selected from —NH—, —O—, —C(O)— and a bond;
- r is an integer from 0 to 4;
- t is an integer from 0 to 1;
- R6 is hydrogen, lower alkyl, a lower alkoxy group, an aryl group, a heterocyclic group or a group of Formula (V), wherein the aryl group and heterocyclic group are optionally substituted by lower alkyl or a lower alkanoyl group:
- wherein n is an integer of from 1 to 6, and;
- R7 and R8 are independently selected from hydrogen and an alkaryl group;
- and
- R11 is hydrogen or lower alkyl;
- or a salt or solvate thereof.
18 more elements
A compound of Formula (I):
- wherein:
- R1 is a group of Formula (II):
- wherein W is aryl or a heterocyclic group,
- R4 is independently selected from hydrogen, fluoro, —OH, amino, —OPO3H2, a lower alkanoylamino group, and a lower alkoxy group, wherein the amino group is optionally substituted by an amino acid residue and the hydroxy group is optionally esterified;
- X is selected from —S(O)—, —S(O2)— and —NH—;
- p is an integer from 0 to 4;
- and
- q is an integer from 1 to 4;
- R2 is selected from:
- hydrogen, halogen and a lower alkyl group;
- R3 is a lower alkyl or a group of Formula (IV);
- wherein Y is selected from —NH—, —O— or a bond;
- Z is selected from —NH—, —O—, —C(O)— or a bond;
- r is an integer from 0 to 4;
- t is an integer from 0 to 1;
- R6 is hydrogen, an aryl group, a heterocyclic group or a group of Formula (V), wherein the aryl group and heterocyclic group are optionally substituted by lower alkyl or a lower alkanoyl group:
- wherein n is an integer of from 1 to 6, and;
- R7 and R8 are independently selected from hydrogen and an alkaryl group;
- and
- R10 is hydrogen, lower alkyl or lower carbarnoylalkyl group;
- R11 is hydrogen or lower alkyl;
- or a salt or solvate thereof.
19 more elements
Dependencies are inferred from the claim text.