SUBSTITUTED 1,4-BENZODIAZEPINES AND USES THEREOF FOR THE TREATMENT OF CANCER

Application 563/KOLNP/2004 published 2006-04-28, filed 2004-04-28
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, Rd and M are defined herein, R5 is hydrogen, alkyl cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aralkyl, optionally substituted heteroaryl, carboxyalkyl, alkoxycarbonyl, alkoxycarbonylalkyl, aminocarbonyl, aminocarbonylalkyl, alkylaminocarbonyl or alkylaminocarbonylalkyl; R6 is cycloalkyl, aryl, heteroaryl, cycloalkylalkyl, aralkyl, heteroarylalkyl, or a saturated or partially unsaturated heterocycle, each of which is optionally substituted; R9 is cycloalkyl, aryl, heteroaryl, a saturated or partially unsaturated heterocycle, cycloalkyl(alkyl), aralkyl or heteroarylalkyl, each of which is optionally substituted; and R10 is -(CH2)n-CO2Rb, -(CH2)m-CO2M, -(CH2)i-OH or -(CH2)j-CONRcRd n is 0-8, m is 0-8, i is 1-8 and j is 0-8 (FIG. - NIL)

Applicant

3 DIMENSIONAL PHARMACEUTICALS INC
THREE LOWER MAKEFIELD CORPORATE CENTER 1020 STONY HILL ROAD, SUITE 300, YARDLEY PENNSYLVANIA 19067 USA

Inventor

1. LU TIANBO 2. LAFRANCE LOUIS V III 3. PARKS DANIEL J 4. MILKIEWICZ KAREN L 5. CALVO RAUL R 6. CUMMINGS MAZWELL DAVID 7. KIM ALEXANDER J 8. GRASBERGER BRUCE L 9. CARVER THEODORE E JR.

International Info

Classification: A61K 31/5513,C07D 243/14,401/04,401/06,403/04 405/04,407/04,409/04,A61P 35/00,37/02
Publication Number: WO 03/041715 A1
Application Date: 2002-11-13

Priority Information

60/331,235 US 2001-11-13