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US 6,150,527 AGranted
Synthetic multimerizing agents
AssigneeARIAD Pharmaceuticals, Inc.
InventorsDennis A. Holt, Terence P. Keenan, Tao Guo, Edgardo Laborde, Wu Yang
Life of this patent
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Abstract
New compounds are disclosed for multimerizing immunophilins and proteins containing immunophilin or immunophilin-related domains. The compounds are of the formula M-L-Q where M is a synthetic ligand for an FKBP protein
Claims51
A compound of a formula selected from the group consisting of ##STR186## wherein G and G' are independently selected from the group comprising of:
- ##STR187## Q comprises a naturally occuring macrocyclic immunophilin ligand or derivative thereof, or a moiety of the following formula:
- ##STR188## n and n' are each independently 1 or 2;
- B.sup.1, B.sup.2, B.sup.1' and B.sup.2' are each independently hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynl, heteroalkyl, heteroalkenyl, heteroalkynyl, heterocycloalkyl, heterocycloalkenyl, heterocycloalkynyl, aryl, or heteroaryl moieties;
- Y and Y' are each independently O, S, NH, --NH(C.dbd.O)--, NH(C.dbd.O)--O--, NH(SO.sub.2)--, NR.sub.3, or a covalent bond;
- X and X' can be O, NH, or CH.sub.2 ;
- R.sup.1, R.sup.2, R.sup.1', R.sup.2' and R.sup.3 are the same or different and are each independently hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, heteroalkyl, heteroalkenyl, heteroalkynyl, heterocycloalkyl, heterocycloalkenyl, heterocycloalkayl, aryl, or heteroaryl moieties;
- and
- L is a covalently linker moeity.
5 more elements
A compound represented by the formula:
- M-L-Q
- wherein
- M comprises a moiety of the formula below ##STR191## Q is another moiety of formula M above, a naturally occuring macrocyclic immunophilin ligand or derivative thereof, or a moiety of the formula below:
- ##STR192## G is a moiety selected from the formulae below:
- ##STR193## n is 1 or 2;
- B.sup.1 and B.sup.2 are each independently hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, heteroalkyl, heteroalkenyl, heteroalkynyl, heterocycloalkyl, heterocycloalkenyl, heterocycloalkynyl, aryl, or heteroaryl moieties;
- Y is O, S, NH, --NH(C.dbd.O)--, NH(C.dbd.O)--O--, NH(SO.sub.2)--NR.sup.3, or a covalent bond;
- X is O, S, or CH.sub.2 ;
- R.sup.1, R.sup.2 and R.sup.3 are the same or different and are each independently hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, heteroalkyl, heteroalkenyl, heteroalkynyl, heterocycloalkyl, heterocycloalkenyl, heterocycloalkynyl, aryl, or heteroaryl moieties;
- and
- L is a covalent linker moiety.
8 more elements
Dependencies are inferred from the claim text.