我们发现了双环氮杂芳烃的开环氟化。在用亲电氟化剂处理双环氮杂芳烃例如吡唑并[1,5- a ]吡啶时,芳环的氟化之后是开环反应。尽管这种整体转变可以归类为芳环的亲电氟化,但它是一种新型氟化,会导致叔碳氟键的构建。本方案可应用于一系列双环氮杂芳烃、耐受吖嗪和各种官能团。此外,还对机理研究和对映选择性氟化进行了检查。
[EN] METHODS OF TREATING NEURODEGENERATIVE DISEASES<br/>[FR] MÉTHODES DE TRAITEMENT DE MALADIES NEURODÉGÉNÉRATIVES
申请人:SEAL ROCK THERAPEUTICS INC
公开号:WO2020046975A1
公开(公告)日:2020-03-05
Described herein are methods of treating or preventing an ASK1 or DYRK1A associated disease, disorder, or condition comprising administering to a subject in need thereof a dual inhibitor of ASK1 and DYRK1A; including administering pharmaceutically acceptable salts and solvates thereof.
HETEROARYL COMPOUNDS USEFUL AS RAF KINASE INHIBITORS
申请人:Chuaqui Claudio
公开号:US20120040951A1
公开(公告)日:2012-02-16
The present invention provides compounds of formula (I) useful as inhibitors of Raf protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.
This invention provides compounds of formula IA-i-a or IB-i-a and subsets thereof:
wherein Z, HY, R
1
, R
2
, R
3
, G
1
, W, n, and A and subsets thereof are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
Disclosed are compounds of Formula 1, N-oxides, and salts thereof,
wherein
Z is O or S; and
R
1
, R
2
, R
3
, Q and n are as defined in the disclosure.
Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling a parasitic nematode comprising contacting the parasitic nematode or its environment with a biologically effective amount of a compound or a composition of the invention.