Intrinsically labelled solid support
AssigneeZeneca Limited, a London corporation
InventorsBrian Geoffrey Main, Richard Eden Shute
Life of this patent
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Abstract
A compound library comprises a plurality of different units each comprising a solid support with which is associated a single member of the compound library, each solid support has a defined chemical composition which acts as an intrinsic label capable of identifying the first choice in the synthesis of the associated member of the compound library.
Claims18
A compound library comprising a plurality of different units each comprising a solid support with which is associated a single member of the compound library, characterised in that each solid support has a defined chemical composition which acts as an intrinsic label capable of identifying the first reaction choice in the synthesis of the associated member of the compound library.
A compound library according to any one of the preceding claims, wherein the intrinsic label comprises at least one substituted styrene incorporated into the chemical composition of the solid support.
A compound library according to any one of the preceding claims, wherein the solid support contains up to 20% w/w of the intrinsic label.
A compound library according to any one of the preceding claims, wherein the solid supports have one or more inert secondary labels which are introduced during library synthesis by controlled chemical modification of the solid support.
A method for the synthesis of a compound library comprising a plurality of different units each comprising a solid support with which is associated a single member of the compound library, which method comprises:
- a) apportioning solid supports among a plurality of reaction vessels such that each reaction vessel contains a portion of solid support having a unique defined chemical composition which acts as an intrinsic label capable of identifying the first reaction choice in the synthesis of the associated member of the compound library;
- b) exposing the supports in each reaction vessel to a first reaction choice;
- c) pooling the supports;
- d) apportioning the supports among a plurality of reaction vessels;
- e) exposing the supports in each reaction vessel to a further reaction choice;
- and
- f) repeating steps c), d) and e) as required.
A method for the characterisation of members of a compound library comprising a plurality of different units each comprising a solid support with which is associated a single member of the compound library, which method comprises:
- i) synthesising the library by a method comprising:
- a) apportioning solid supports among a plurality of reaction vessels such that each reaction vessel contains a portion of solid support having a unique defined chemical composition which acts as an intrinsic label capable of identifying the first reaction choice in the synthesis of the associated member of the compound library;
- b) exposing the supports in each reaction vessel to a first reaction choice;
- c) pooling the supports;
- d) apportioning the supports among a plurality of reaction vessels;
- e) exposing the supports in each reaction vessel to a further reaction choice;
- and
- f) repeating steps c), d) and e) as required;
- ii) testing members of the compound library for a characteristic of interest;
- iii) selecting library compounds of interest;
- and
- iv) identifying the intrinsic labels of the associated solid supports and identifying the first reaction choice in the synthesis of such compounds by reference to said intrinsic labels.
A kit of solid supports for compound library synthesis comprising a plurality of portions of a solid support upon which associated members of a compound library can be synthesised, characterised in that each portion of the solid support has a unique defined chemical composition which acts as an intrinsic label capable of identifying the first reaction choice in the synthesis of the associated member of the compound library.
Dependencies are inferred from the claim text.