Imidazo[1,2-a]pyridines are disclosed. Compounds of the invention are useful therapeutic agents and their inclusion in pharmaceutical formulations and use in methods of treatment are disclosed.
Aminonapthoquinone compounds and pharmaceutical composition for blocking ubiquitination-proteasome system in diseases
申请人:TAIPEI MEDICAL UNIVERSITY
公开号:US10577328B2
公开(公告)日:2020-03-03
The invention relates to a compound of formula (I)
with low cytotoxicity for blocking the ubiquitination-proteasome system in diseases. Accordingly, these compounds can be used in treatment of disorders including, but not limited to, multiple myeloma, cancers, neurodegenerative diseases, inflammatory disorders, autoimmune disorders and metabolic disorders.
Bridged bicyclic inhibitors of menin-MLL and methods of use
申请人:Kura Oncology, Inc.
公开号:US10752639B2
公开(公告)日:2020-08-25
The present disclosure provides compounds of Formula (I-E) for inhibiting the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins. The compounds are useful for the treatment of leukemia, solid cancers, diabetes and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, and/or menin.
The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof:
X-A-Y—Z-L-R
1
(I)
which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
SUBSTITUTED FUSED BI- OR TRI- HETEROCYCLIC COMPOUNDS AS EHMT2 INHIBITORS
申请人:Epizyme, Inc.
公开号:US20200039961A1
公开(公告)日:2020-02-06
The present disclosure relates to substituted fused bi- or tri-heterocyclic compounds. The present disclosure also relates to pharmaceutical compositions containing these compounds and methods of treating a disorder (e.g., sickle cell anemia) via inhibition of a methyltransferase enzyme selected from EHMT1 and EHMT2, by administering a substituted fused bi- or tri-heterocyclic compound disclosed herein or a pharmaceutical composition thereof to subjects in need thereof. The present disclosure also relates to the use of such compounds for research or other non-therapeutic purposes.