[EN] SMALL MOLECULE INHIBITORS OF NF-kB INDUCING KINASE<br/>[FR] INHIBITEURS À PETITE MOLÉCULE DE KINASE INDUISANT NF-KB
申请人:JANSSEN PHARMACEUTICA NV
公开号:WO2020239999A1
公开(公告)日:2020-12-03
The present invention relates to compounds that inhibit NIK and pharmaceutical compositions comprising such compounds and methods of using the same. These compounds and pharmaceutical compositions are envisaged to be useful for preventing or treating diseases such as cancer (such as B-cell malignancies including leukemias, lymphomas and myeloma), inflammatory disorders, autoimmune disorders, immunodermatologic disorders such as palmoplantar pustulosis and hidradenitis suppurativa, and metabolic disorders such as obesity and diabetes.
Highly Regio- and Stereoselective Halohydroxylation Reaction of 1,2-Allenyl Phenyl Sulfoxides. Reaction Scope, Mechanism, and the Corresponding Pd- or Ni-Catalyzed Selective Coupling Reactions
作者:Shengming Ma、Hongjun Ren、Qi Wei
DOI:10.1021/ja034039q
日期:2003.4.1
A highlyregio- and stereoselective halohydroxylation of 1,2-allenyl sulfoxides with X(+) and water was developed. The reaction shows E-stereoselectivity. In the iodohydroxylation reaction, I(2) was used to introduce the iodine atom. For bromohalohydroxylation, CuBr(2), NBS, or Br(2) can be used. When using I(2), NBS, or Br(2), the addition of LiOAc.2H(2)O is necessary for high yields of the halohydroxylation
Overriding Felkin Control: A General Method for Highly Diastereoselective Chelation-Controlled Additions to α-Silyloxy Aldehydes
作者:Gretchen R. Stanton、Corinne N. Johnson、Patrick J. Walsh
DOI:10.1021/ja910717p
日期:2010.3.31
Cram-chelation models, nucleophilic additions to alpha-silyloxy aldehydes proceed through a nonchelation pathway due to the steric and electronic properties of the silyl group, giving rise to Felkin addition products. Herein we describe a general method to promote chelation-control in additions to alpha-silyloxy aldehydes. Dialkylzincs, functionalized dialkylzincs, and (E)-disubstituted, (E)-trisubstituted
Chelation-Controlled Addition of Organozincs to α-Chloro Aldimines
作者:Gretchen R. Stanton、Per-Ola Norrby、Patrick J. Carroll、Patrick J. Walsh
DOI:10.1021/ja306781z
日期:2012.10.24
report is C-X bonds reversing the diastereoselectivity throughcoordination to metals during C-C bond-forming reactions (chelationcontrol). Herein we describe chelationcontrol involving C-X bonds in highly diastereoselective additions of organozinc reagents to a variety of α-chloro aldimines. The unique ability of alkylzinc halide Lewisacids to coordinate to the Cl, N, and O of α-chloro sulfonyl
众所周知,α-手性 α-卤代羰基衍生物的亲核加成可通过非螯合途径生成 Cornforth-Evans 产物。在本报告之前前所未有的是 CX 键通过在 CC 键形成反应(螯合控制)期间与金属配位来逆转非对映选择性。在此,我们描述了在将有机锌试剂高度非对映选择性添加到各种 α-氯醛亚胺中时涉及 CX 键的螯合控制。计算研究支持烷基锌卤化物路易斯酸与 α-氯磺酰基亚胺底物的 Cl、N 和 O 配位的独特能力。
SUBSTITUTED 3-((3-AMINOPHENYL)AMINO)PIPERIDINE-2,6-DIONE COMPOUNDS, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH
申请人:Celgene Corporation
公开号:US20200199074A1
公开(公告)日:2020-06-25
Provided herein are piperidine dione compounds having the following structure:
wherein R
N
, R
1
, R
2
, R
3
, R
4
, X, L, V, m, and n are as defined herein, compositions comprising an effective amount of a piperidine dione compound, and methods for treating or preventing an androgen receptor mediated disease.