预约演示

更新于：2025-05-07

CJ-13981

更新于：2025-05-07

概要

概要

基本信息

药物类型

小分子化药

别名

靶点

SQS

作用方式

抑制剂

作用机制

SQS抑制剂(角鲨烯合成酶抑制剂)

治疗领域-

在研适应症-

非在研适应症-

原研机构

Pfizer Pharmaceuticals, Inc.

在研机构

Pfizer Pharmaceuticals, Inc.

非在研机构-

权益机构-

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 CJ-13981 相关的临床结果

登录后查看更多信息

100 项与 CJ-13981 相关的转化医学

登录后查看更多信息

100 项与 CJ-13981 相关的专利（医药）

登录后查看更多信息

项与 CJ-13981 相关的文献（医药）

2021-10-15·The Journal of Organic Chemistry2区 · 化学

Flow-Assisted Synthesis of Alkyl Citrate Natural Products

2区 · 化学

Article

作者: Rizzacasa, Mark A. ; Polyzos, Anastasios ; Rossouw, Nikolai Piers

The development of a flow-assisted synthesis of alkyl citrate natural products is described. The flow route harnesses a number of steps including the generation of ketene silyl acetal, a formal [2 + 2] cycloaddition, and a methanolysis cascade to efficiently generate a highly substituted, and stereodefined tetrahydrofuran intermediate. A heterogeneous pseudo-Finkelstein reaction and zinc-mediated elimination furnish a key alkene alkyl citrate fragment in high yield over a multistep sequence that provides direct entry to compounds such as (-)-CJ-13982 (1), (-)-CJ-13,981 (2), L-731,120 (3), and related natural products. The flow methodology developed in this study enables a new machine-assisted approach toward the efficient and scalable synthesis of the alkyl citrate family of natural products.

2018-07-20·Organic Letters1区 · 化学

Synthesis of Alkyl Citrates (−)-CJ-13,981, (−)-CJ-13,982, and (−)-L-731,120 via a Cyclobutene Diester

1区 · 化学

Article

作者: Robertson, Angus ; Rizzacasa, Mark A. ; Sturgess, Dayna ; Chen, Zongjia ; White, Jonathan M. ; Atkin, Liselle

An efficient and step-economic new approach to alkyl citrate natural products from a cyclobutene diester is presented. The key sequence involves a formal [2 + 2]-cycloaddition of a silylketene acetal with dimethylacetylene dicarboxylate to provide the cyclobutene diester 14 with 4.5:1 stereoselectivity. Exposure of diester 14 in acidic methanol effected a hydrolysis, intramolecular oxy-Michael reaction, and cyclobutanone methanolysis cascade to give the triester 15. Iodination and elimination then afforded a key alkyl citrate alkene intermediate, which was converted into the natural products (-)-CJ-13,982 (1), (-)-CJ-13,981 (2), and (-)-L-731,120 (3) via a cross-metathesis and subsequent reduction.

2001-01-01·The Journal of Antibiotics4区 · 医学

CJ-13,981 and CJ-13,982, New Squalene Synthase Inhibitors.

4区 · 医学

Article

作者: H. James Harwood ; Takahito Kambara ; Shuzo Watanabe ; Nakao Kojima ; Yuji Yamauchi ; Hiroyuki Nlshida ; Yasuhiro Kojima ; Nobuji Yoshikawa ; Ayumu Sugiura ; Hideo Hirai ; Liang Hsiung Huang

Two new squalene synthase (SSase) inhibitors, CJ-13,981 (I) and CJ-13,982 (II), were isolated from the fermentation broth of an unidentified fungus CL 15036. They inhibited human liver microsomal SSase with IC50s of 2.8 and 1.1 microM, respectively, but showed no inhibitory activity against human brain protein farnesyltransferase (PFTase) at 100 microM. Based on FAB-MS and NMR analyses, the structures of I and II were determined to be 3-hydroxy-3,4-dicarboxy-15-hexadecenoic acid and 3-hydroxy-3,4-dicarboxyhexadecanoic acid, respectively.

100 项与 CJ-13981 相关的药物交易

登录后查看更多信息