31127-85-2Relevant articles and documents
BIFUNCTIONAL COMPOUNDS FOR DEGRADING BTK VIA UBIQUITIN PROTEOSOME PATHWAY
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Paragraph 0972; 0975; 0976, (2020/05/21)
The present invention relates to compounds useful for degrading BTK via a ubiquitin proteolytic pathway. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
PEPTIDIC LINKERS AND CRYPTOPHYCIN CONJUGATES, USEFUL IN THERAPY, AND THEIR PREPARATION
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Page/Page column 239, (2018/12/02)
The present disclosure relates to compounds of formula (I): RCG1-L-P (I) wherein RCG1 represents a reactive chemical group being reactive towards a chemical group present on a polypeptide such as an antibody; P represents H, OH or an activated O; and L represents a specific linker. The disclosure also relates to cryptophycin payloads, as well as to cryptophycin conjugates, to compositions containing them and to their therapeutic use, especially as anticancer agents. The disclosure also relates to the process for preparing these conjugates.
Intramolecular End-to-End Reactions of Photoactive Terminal Groups Linked by Poly(oxyethylene) Chains
Ashikaga, Kazuo,Ito, Shinzaburo,Yamamoto, Masahide,Nishijima, Yasunori
, p. 2443 - 2450 (2007/10/02)
The triplet-sensitized photochemical reaction using a series of poly(oxyethylene) chains with a pair of photoactive terminal groups, dibenzazepine (DBA) chromophores (DBA-COCH2CH2(OCH2CH2)nOCH2CH2CO-DBA, n=0-10) was examined.The photoirradiation of bichromophoric compounds caused either intra- or intermolecular reactions.These reactions were kinetically analyzed by two different methods: the measurement of deactivation processes of the reaction intermediates (excited triplet state of DBA) by nanosecond laser photolysis and the quantitative analysis of the reaction products by GPC.The intramolecular deactivation rate constant, kintra, showed a remarkable chain-length dependence; the maximum kintra value appeared at n=5 and it was found to be 5.9X104 s-1.On the other hand, the intramolecular cyclization rate also depends on the chain length; the maximum quantum yield, φintrad, was given at n=7 (φintrad=0.51).The chain length for the maximum cyclization yield shifted slightly to the longer region than that for the maximum kintra value due to the restriction of the terminal structure (anti-configuration).The results obtained for this reaction system are compared with those obtained for the previously reported polymethylene system and the effect of chain flexibility on the intramolecular ring-closure reaction is discussed.
Radiopaque contrast media. XXIV. Synthesis and structure activity relationships of new hexaiodinated radiopaque compounds
Felder,Pitre,Fumagalli,Lorenzotti
, p. 912 - 924 (2007/10/06)
The synthesis of a series of new hexaiodinated radiopaque compounds is described. The relationship of structure to tolerability and biliary and urinary excretion was studied. Optimum tolerability was achieved with a compound which has been selected for further investigation as an angiographic contrast agent of the 'dimer' type. Iodoxamic acid showed a high biliary excretion combined with good tolerability, and is being developed as an injectable cholecystographic agent.