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US 8,618,283 B2Granted
Ligand libraries for screening GPCRs
AssigneeCambridge Enterprise Limited
InventorsDavid J Grainger, David John Fox
Life of this patent
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Abstract
The invention provides compounds of general formulae (I)-(IV) or pharmaceutically acceptable salts thereof: The invention also provides methods of preparing the compounds, pharmaceutical compositions comprising the compounds and use of the compounds for the preparation of medicaments intended to modulate the activity of one or more members of the G-protein coupled receptor (GPCR) class. Compounds of the invention may be used to create a compound library for use in screening for agents which modulate signalling through GPCRs.
Claims12
A compound of general formula (III)
- wherein:
- X is —CO—(Y)k—(Z)n or SO2—(Y)k—(Z)n;
- k is 0 or 1;
- Y is a cycloalkyl or polycyloalkyl group;
- or Y is a cycloalkenyl or polycycloalkenyl group;
- each Z is independently selected from hydrogen, or an alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, alkynyl, alkylamino, alkylaminoalkyl, alkylaminodialkyl, charged alkylaminotrialkyl or charged alkylcarboxylate radical of 1 to 20 carbon atoms;
- or each Z is independently selected from fluoro, chloro, bromo, iodo, hydroxy, oxyalkyl, amino, aminoalkyl, aminodialkyl, charged aminotrialkyl, or carboxylate radical;
- and
- n is any integer from 1 to m, where m is the maximum number of substitutions permissible on the cyclo-group Y;
- or
- each Z may be independently a peptido radical;
- and
- wherein R2 is an alkyl, aryl or an acyl group;
- and wherein R3 is a side-chain of an α-amino acid used in formation of (III);
- and wherein R4 is a 2-substituent of a β-amino alcohol used in formation of (III).
12 more elements
Dependencies are inferred from the claim text.