路漫漫其修远兮分享 http://blog.sciencenet.cn/u/zhpd55 追求科学,勇于探索,苦海无涯,愿作小舟。

博文

首次透露5种药物候选者结构式,并附相关专利文献

已有 6264 次阅读 2013-4-13 20:51 |个人分类:新科技|系统分类:博客资讯| 专利, 美国化学会, 新药结构式, 药物候选者

       2013年4月10日,来自美国化学会新奥尔良(New Orleans)会议的信息,首次透露了5种药物候选者的结构式,它们分别转载如下(见下图),因为每一种药物候选者均已经申请了专利,有些还不止一项专利,而是多项专利,而且已经列出了专利号,通过GOOGLE 搜索均可以得到相关专利文献,如利用世界知识产权组织网也可以得到。下面的5种化合物,每一种均已经有一项专利文件(红色字体)可以直接点击即可下载。尽管并非每一种药物候选者最终都有可能成为可以用于临床,而且真正成为药物的概率很低,但是了解其相关信息或许对于新药研发有所帮助和启发。

IMG_3813
BMS-906024
Company: Bristol-Myers Squibb
Meant to treat: cancers including breast, lung, colon, and leukemia
Mode of action: pan-Notch inhibitor
Medicinal chemistry tidbit: The BMS team used an oxidative enolate heterocoupling en route to the candidate– a procedure from Phil Baran’s lab at Scripps Research Institute. JACS 130, 11546
Status in the pipeline: Phase I
Relevant documents: WO 2012/129353
IMG_3810
LGX818
Company: Novartis Institutes for Biomedical Research and Genomics Institute of the Novartis Research Foundation
Meant to treat: melanoma with a specific mutation in B-RAF kinase: V600E
Mode of action: selective mutant B-RAF kinase inhibitor
Status in the pipeline: Phase Ib/II
Relevant documents: WO 2011/023773 ; WO 2011/025927
IMG_3812
AZD5423
Company: AstraZeneca
Meant to treat: respiratory diseases, in particular chronic obstructive pulmonary disease
Mode of action: non-steroidal glucocorticoid receptor modulators
Medicinal chemistry tidbit: This compound originated in part from a collaboration with Bayer Pharma.
Status in the pipeline: Phase II
Relevant documents: WO 2011/061527 ; WO 2010/008341 ; WO 2009/142568
IMG_3811
Birinapant (formerly known as TL32711)
Company: TetraLogic Pharmaceuticals
Meant to treat: cancer
Mode of action: blocks the inhibitor of apoptosis proteins to reinstate cancer cell death
Status in the pipeline: Phase II
Relevant documents: US 8,283,372
IMG_3814
MGL-3196 (previously VIA-3196)
Company: Madrigal Pharmaceuticals, acquired from VIA Pharmaceuticals, licensed from Roche
Meant to treat: high cholesterol/high triglycerides
Mode of action: mimics thyroid hormone, targeted to thyroid hormone receptor beta in the liver
Medicinal chemistry tidbit: this molecule was discovered at Roche’s now-shuttered Nutley site.
Status in the pipeline: completed Phase I trials
Relevant documents: WO 2007/009913 ; WO 2009/03717



https://blog.sciencenet.cn/blog-212210-679888.html

上一篇:合成生物学:抗疟药青蒿素半合成的里程碑(修改稿)
下一篇:绿藻动力生物智商(BIQ)屋在汉堡(Hamburg)建成
收藏 IP: 61.134.23.*| 热度|

3 梁建华 叶威源 崔庆彬

该博文允许注册用户评论 请点击登录 评论 (3 个评论)

数据加载中...
扫一扫,分享此博文

Archiver|手机版|科学网 ( 京ICP备07017567号-12 )

GMT+8, 2024-12-24 20:16

Powered by ScienceNet.cn

Copyright © 2007- 中国科学报社

返回顶部