NOVEL N-SUBSTITUTED-PYRROLIDINES AS INHIBITORS OF MDM2-P-53 INTERACTIONS
申请人:Bartkovitz David Joseph
公开号:US20110086854A1
公开(公告)日:2011-04-14
There are provided compounds of the formula
wherein X, Y, R
1
, R
2
, R
3
, R
3
, R
4
, and R
5
are as described herein
and enantiomers and pharmaceutically acceptable salts and esters thereof which are useful as anticancer agents.
There are provided compounds of the formula
wherein X, Y, R
1
, R
2
, R
3
, R
3
, R
4
, R
5
, R
6
and R
7
are as described herein and enantiomers and pharmaceutically acceptable salts and esters thereof. The compounds are useful as anticancer agents.
This application discloses 6-(2-Hydroxymethyl-phenyl)-2-methyl-2H-pyridazin-3-one derivatives according to generic Formula I:
wherein, variables X, R, and Y
4
, are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation, such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.
Provided herein are compounds of the formula (I):
as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.
There are provided compounds of the formula
wherein X, Y and R
1
to R
8
are described herein along with the enantiomers, pharmaceutically acceptable salts and esters thereof. The compounds are useful as anticancer agents.