We report the synthesis of two novel cisplatin-N-mustardconjugates. In these compounds two potentially DNA-damaging molecules are combined and are separated by a spacer containing either one or four ethylene glycol units. We have shown that these conjugates are capable of forming novel clustered DNA adducts, thereby strongly increasing the lesion density in double-stranded DNA, which is thought to
我们报告了两种新型顺铂-N-芥末偶联物的合成。在这些化合物中,两个潜在的 DNA 损伤分子结合在一起,并被一个含有一个或四个乙二醇单元的间隔物隔开。我们已经证明这些缀合物能够形成新的成簇 DNA 加合物,从而大大增加双链 DNA 的损伤密度,这被认为会阻止 DNA 修复和跨损伤合成。它们抑制细胞分裂的能力在大肠杆菌试验中得到证实。
NOVEL BINDER-DRUG CONJUGATES (ADCs) AND USE OF SAME
申请人:SEATTLE GENETICS, INC.
公开号:US20150246136A1
公开(公告)日:2015-09-03
The present patent application relates to novel binder-drug conjugates (ADCs) of N,N-dialkylauristatins directed against the target epidermal growth factor receptor (EGFR, gene ID 1956), effective metabolites of these ADCs, methods for producing these ADCs, use of these ADCs for treatment and or prevention of diseases as well as the use of these ADCs to produce pharmaceutical drugs for treatment and/or prevention of diseases, in particular hyperproliferative and/or angiogenic diseases such as cancer, for example. Such treatments may be administered as monotherapy or in combination with other pharmaceutical drugs or other therapeutic measures.
6-APA derivatives were considered as selective labels for the construction of bifunctional linkers dedicated to the oriented immobilization of proteins on materials. Sulbactam-like compounds (i.e., 6-β-sulfonamido-penam sulfones) and penicillin G—like compounds (i.e., para-substituted 6-β-phenylacetamido-penams) were prepared and tested as irreversible inhibitors of representative β-lactamases and
The invention provides conjugates that comprise a bivalent targeting moiety, a nucleic acid, and optional linking groups as well as synthetic intermediates and synthetic methods useful for preparing the conjugates, compositions comprising the bidentate targeting ligands and the conjugates, as well as methods for targeting therapeutic nucleic acids with the bidentate conjugates. The conjugates are useful to target therapeutic nucleic acids.
Simultaneous dual isotope imaging of cardiac perfusion and cardiac inflammation
申请人:——
公开号:US20030003049A1
公开(公告)日:2003-01-02
The present invention provides novel diagnostic compositions comprising a radiolabeled LTB4 binding agent and a radiolabeled perfusion imaging agent, diagnostic kits comprising such compositions, and methods of concurrent imaging in a mammal comprising administering a radiolabeled LTB4 binding agent and a radiolabeled perfusion imaging agent, and concurrently detecting the radiolabeled LTB4 binding agent bound at the LTB4 receptor and the radiolabeled perfusion imaging agent.