摘要 考虑到人碳酸酐酶 III (hCA III) 尚未被认识的生理病理作用,我们建立了基于结构的药物设计,以确定这种被忽视的亚型的一流的有效和选择性抑制剂。hCA III 靶向的计划考虑到其活性位点在其他 hCA 同工型中的独特特征,即干扰芳香族/杂环磺酰胺和其他抑制剂结合的 Leu198/Phe198 取代。因此,具有长而灵活的(CH 2 ) n SO 2 NH 2部分的新型脂肪族伯磺酰胺被设计来配位锌(II)离子,绕过庞大的Phe198残基。它们结合了 1,2,3-三唑连接体,将尾部部分连接到磺酰胺头部,从而增强了活性位点入口处的接触。其中一些化合物比其他亚型更能作为 hCA III 的纳摩尔选择性抑制剂。对接/分子动力学模拟用于研究这些磺胺类药物的配体/靶标相互作用,这可能会提高我们对 hCA III 生理病理作用的理解。
PRECURSOR COMPOUND CONNECTED TO SOLID SUPPORT FOR MANUFACTURING 18F RADIOPHARMACEUTICAL, METHOD FOR MANUFACTURING SAME, AND APPLICATION THEREOF
申请人:Chi Dae-Yoon
公开号:US20140011961A1
公开(公告)日:2014-01-09
The present invention relates to a solid precursor in the form of an organic salt, the solid precursor having a solid support, a method for manufacturing same, and an application thereof. The solid precursor of the present invention enables omission of the [
18
F]fluoride refining process using additional cartridge, and the use of excessive phase-transfer catalyst, and can easily remove remaining substance after reaction through the solid support inside the precursor. The solid precursor of the present invention is very appropriate for an automated synthesis device as an all-in-one system that can carry out overall process of [
18
F]fluorosis reaction, when used by charging in a cartridge.
[EN] AURISTATIN DERIVATIVES AND CONJUGATES THEREOF<br/>[FR] DÉRIVÉS D'AURISTATINE ET CONJUGUÉS DE CEUX-CI
申请人:NOVARTIS AG
公开号:WO2015189791A1
公开(公告)日:2015-12-17
Disclosed herein are novel compounds of formula (I) as described herein, and the use of such peptides in making immunoconjugates (i.e Antibody Drug Conjugates) Also described herein are immunoconjugates (i.e Antibody Drug Conjugates) comprising such novel compound linked to an antigen binding moiety, such as an antibody; where such immunoconjugates are useful for treating cell proliferative disorders. The invention further provides pharmaceutical compositions comprising these immunoconjugates, compositions comprising the immunoconjugates with a therapeutic co-agent, and methods to use these immunoconjugates and compositions for treating cell proliferation disorders.
[EN] ANTIBODY DRUG CONJUGATES<br/>[FR] CONJUGUÉS ANTICORPS-MÉDICAMENT
申请人:NOVARTIS AG
公开号:WO2016203432A1
公开(公告)日:2016-12-22
This application discloses anti-P-cadherin antibodies, antigen binding fragments thereof, and antibody drug conjugates of said antibodies or antigen binding fragments, particularly antibody drug conjugates comprising anti-P-cadherin antibodies conjugated to auristatin analogs. The invention also relates to methods of treating cancer using the antibody drug conjugates. Also disclosed herein are methods of making the antibodies, antigen binding fragments, and antibody drug conjugates, and methods of using the antibodies and antigen binding fragments as diagnostic reagents.
METHODS, COMPOUNDS, COMPOSITIONS AND VEHICLES FOR DELIVERING 3-AMINO-1-PROPANESULFONIC ACID
申请人:Kong Xianqi
公开号:US20080146642A1
公开(公告)日:2008-06-19
The invention relates to methods, compounds, compositions and vehicles for delivering 3-amino-1-propanesulfonic acid (3APS) in a subject, preferably a human subject. The invention encompasses compounds that will yield or generate 3APS, either in vitro or in vivo. Preferred compounds include amino acid prodrugs of 3APS for use, including but not limited to, the prevention and treatment of Alzheimer's disease.