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US 6,713,580 B2Granted
Quaternary amino acids on solid supports
AssigneePharmacore, Inc.
InventorsMichael Johnson, Keqiang Li, Elso DiFranco, Daljit S. Dhanoa
Life of this patent
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Abstract
The present invention relates to novel templates useful for generating novel compounds and to compounds produced utilizing the templates. The templates comprise quaternary amino acids that may be linked to solid supports. These templates make possible the production of novel classes of chemical compounds through a plurality of chemical reactions. The templates are advantageous for use in drug discovery regimes.
Claims67
A compound of the following formula
- wherein
- Z comprises the residue of a solid polymer support having hydroxyl or amino functionality;
- L1 comprises a divalent group of the formula —O—, —NH—, —O—CH2—C6H4—CH2O—;
- L2 and L3 comprise, independently, alkylene, alkenylene, alkynylene, or a direct single bond;
- L4 comprises alkylene, —O—, —S—, —C(O)—, —S(O)—, —S(O)2—,
- or a direct single or double bond;
- L5 comprises —CH2CH2— or —CH2CH2CH2—;
- E and K comprise, independently, —N—, —CH—, or —C═;
- PG comprises hydrogen or an amino protecting group;
- R1 and R2 comprise, independently, alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, hydrogen, halo, —O—G3, —O—G4, —G3, —G4, or —N(G3)G4;
- R1 and R2 may be taken together to constitute a cycloalkyl or heterocyclyl ring, or, where L4 is a direct bond, R1 and R2 may be taken together to constitute a fused aryl or heteroaryl ring;
- G3 and G4 comprise, independently,
- where
- L7, L8, L9, L10, L11, L12 comprise, independently, alkylene, alkenylene, alkynylene, cycloalkylene, cycloalkenylene, arylene, heterocyclylene, heteroarylene, fused cycloalkylarylene, fused cycloakylheteroarylene, fused heterocyclylarylene, fused heterocyclylheteroarylene, or a direct bond;
- and
- R10, R11, R12, R13, R14, R15 comprise, independently, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocyclyl, heteroaryl, aryl, fused cycloalkylaryl, fused cycloakylheteroaryl, fused heterocyclylaryl, fused heterocyclylheteroaryl, —NR18R19, —OR18, —SR18, or hydrogen, where R18 and R19 are as defined below;
- R18 and R19 comprise, independently, hydrogen, alkyl, alkynyl, alkenyl, cycloalkyl, cycloalkenyl, aryl, heterocyclyl, or heteroaryl.
14 more elements
Dependencies are inferred from the claim text.