Substituted 1,4-diazepines and uses thereof

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

2006-10-03

2006-10-03

Kifle, Bruck (Department: 1624)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

C540S506000, C540S509000

Reexamination Certificate

active

07115598

ABSTRACT:
The present invention is directed to novel 1,4-diazepines, 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:R1, R2, R9, R10, Ra, Rdand M are defined herein;X is a bivalent radical of: an alkane, a cycloalkane, an optionally-substituted arene, an optionally-substituted heteroarene, an optionally-substituted arylalkane or an optionally-substituted heteroarylalkane; andR3is —CO2Rd, —CO2M, —OH, —NHRd, —SO2Rd, —NHCONHRd, optionally-substituted amidino or optionally-substituted guanidino;or R3—X— is hydrogen or an electron pair;R4is oxygen or —NR9R10;R5is cycloalkyl, aryl, heteroaryl, cycloalkylalkyl, aralkyl, heteroarylalkyl, or a saturated or partially unsaturated heterocycle, each of which is optionally substituted; andR6, R7and R8are independently hydrogen, alkyl, cycloalkyl, aryl, heteroaryl, a saturated or partially unsaturated heterocycle, cycloalkylalkyl, aralkyl or heteroarylalkyl, each of which is optionally substituted; or R6and R7, together with the carbon atom to which they are attached form a 3- to 7-membered carbocyclic ring optionally substituted 1 to 3 times with Ra.

REFERENCES:
Chen et al.,Proc. Natl. Acad. Sci. USA, 95:195-200 (1998).
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Kussie et al.,Science, 274:948-953 (1996).
Bottger et al.,J. Mol Biol., 269:744-756 (1997).
International Search Report dated Oct. 20, 2005 for International Appln. No. PCT/US04/12240.
Hulme et al. Improved Procedure for the Solution Phase Preparation of 1,4-Benzodiazepine-2,5-dione Libraries via Armstrong's Convertible Isonitrile and the Ugi Reaction, J. Org. Chem, 1998, vol. 63, pp. 8021-8023.

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