发明名称 Spirocyclic compounds as HDAC inhibitors
摘要 The present invention relates to a novel class of substituted spirocyclic compounds, represented by the following structural Formula: I Wherein A, B and D are independently selected from CR , NR, C(O) and O; E is selected from a bond, CR . NR, C(O) and O; wherein at least one of A, B, D or E is CR ; and provided that when A is O, then E is not O; G is CR ; R is selected from NH and OH; These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing termin differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the compounds of the instant invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of these compounds in vivo.
申请公布号 AU2006318773(B2) 申请公布日期 2012.03.22
申请号 AU20060318773 申请日期 2006.11.17
申请人 MERCK SHARP & DOHME CORP. 发明人 HEIDEBRECHT, RICHARD W.;CLOSE, JOSHUA;KATTAR, SOLOMON D.;TEMPEST, PAUL;MAMPREIAN, DAWN M.;KLIMAN, LAURA T.;MILLER, THOMAS;SLOMAN, DAVID L.;ZABIEREK, ANNA A.;BERK, SCOTT C.;STANTON, MATTHEW G.;HAMBLETT, CHRISTOPHER;METHOT, JOEY L.
分类号 C07D471/10;A61K31/407;A61K31/424;A61K31/438;A61P25/00;A61P29/00;A61P35/00;C07D487/10;C07D491/10;C07D498/10 主分类号 C07D471/10
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