Substituted 1,4-benzodiazepines and uses thereof

Details Substituted 1,4-benzodiazepines and uses thereof Substituted 1,4-benzodiazepines and uses thereof

2006-06-27

2006-06-27

Kifle, Bruck (Department: 1624)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

C540S504000, C540S505000, C540S506000, C540S512000

Reexamination Certificate

active

07067512

ABSTRACT:
The present invention is directed to novel 1,4-benzodiazepines, pharmaceutical compositions thereof, and the use thereof as inhibitors of HDM2-p53 interactions. Compounds have Formula I:or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein:X and Y are independently —C(O)—, —CH2— or —C(S)—;R1, R2, R3, R4, R7, R8, Rb, Rc, Rdand M are defined herein;R5is hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aralkyl, optionally substituted heteroaralkyl, carboxyalkyl, alkoxycarbonyl, alkoxycarbonylalkyl, aminocarbonyl, aminocarbonylalkyl, alkylaminocarbonyl or alkylaminocarbonylalkyl;R6is cycloalkyl, aryl, heteroaryl, cycloalkylalkyl, aralkyl, heteroarylalkyl, or a saturated or partially unsaturated heterocycle, each of which is optionally substituted;R9is cycloalkyl, aryl, heteroaryl, a saturated or partially unsaturated heterocycle, cycloalkyl(alkyl), aralkyl or heteroarylalkyl, each of which is optionally substituted; andR10is —(CH2)n—CO2Rb, —(CH2)m—CO2M, —(CH2)i—OH or —(CH2)j—CONRcRdn is 0–8, m is 0–8, i is 1–8 and j is 0–8.

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