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US 2003/0144260 A1Published application
Heterocyclic compounds, method of developing new drug leads and combinatorial libraries used in such method
AssigneeYissum Research Development Company of the Hebrew University of Jerusalem
InventorChaim Gilon
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Abstract
The present invention provides according to a first of its aspects, new compounds that have a flexible scaffold with various degrees of conformational restriction and accordingly are useful as drug candidates. These compounds may be used to produce new combinatorial libraries that will permit to screen for and select drug candidates for a variety of uses in human medicine, veterinary medicine and in agriculture.
Claims34
Scaffold-based compound having the following general formula (B):
- 12
- including pharmaceutically acceptable salts, esters or solvates thereof, wherein
- Z is selected from C═O and —CH2—,
- W is selected from C═O and a bond, provided that at least one of Z and W is C═O,
- X and Y are independently selected from CH2, O, S, NH, N—R5, NH—CO, CO, CH2CO, S═O and SO2, or X and Y may form together a group selected from CH═CH, CO—NR5, NH—CO—N, O—CH(R5)—O, NH—CH(R5)—O and NH—CH(R5)—NH, where the hydrogen in the above groups may optionally be substituted by an alkyl group,
- (a) and (b) are parts of the scaffold and are nitrogen containing bivalent organic radicals, each independently providing between 1 to 4 atoms to said scaffold,
- R1, R2, R3 and R4 are each independently selected from H and substituted or unsubstituted allyl, and
- n and m are integers from 1 to 6, with the exclusion of the following compound:
- glycinamide, L-tyrosyl-N-[2-[(2S)-4-[(1S)-1-carboxy-3-methylbutyl]-3,4,5,8-tetrahydro-3-oxo-2-(phenymethyl)-1,4-diazocin-1(2H)-yl]2-oxoethyl.
6 more elements
Compound of the formula I, II, III or IV:
- 13
- including pharmaceutically acceptable salts, esters or solvates thereof, wherein
- X and Y are independently selected from CH2, O, S, NH, N—R5, NH—CO, CO, CH2CO, S═O and SO2, or X and Y may form together a group selected from CH═CH, CO—NR5, NH—CO—NH, O—CH(R5)—O, NH—CH(R5)—O and NH—CH(R5)—NH, where the hydrogen in the above groups may optionally be substituted by an alkyl group;
- R1, R2, R3 and R4 are each independently selected from H and substituted or unsubstituted alkyl;
- R5, R6, R7 and R8 are each independently selected from H, substituted or unsubstituted alkyl, cycloalkyl, aryl, aralkyl, hetroaryl, heterocyclyl, hetroaralkyl, acyl, carboxyaryl, carboxyalkyl, side chains of naturally and artificially occurring amino acids as well as derivatives and mimics of such side chains, and linear or cyclic peptide;
- L is selected from H, OH, NH2, NHR5, a peptide and a solid support, where R5 is as defined above, and
- n and m are integers from 1 to 6, with the exclusion of the following compound:
- glycinamide, L-tyrosyl-N-[2-[(2S)-4-[(1S)-1-carboxy-3-methylbutyl]-3,4,5,8-tetrahydro-3-oxo-2-(phenymethyl)-1,4-diazocin-1(2H)-yl]2-oxoethyl.
5 more elements
Dependencies are inferred from the claim text.