06-04-2017 дата публикации
Номер: US20170095576A1
Автор:
Chae Jeiwook,
Cho Jong Un,
Chung Chul-Woong,
Jung Doo Hwan,
Kim Sun Young,
Kim Yong Zu,
Lee Hyang Sook,
MIN Ji Young,
Oh Kyu Man,
Oh Yeong Soo,
Park Tae Kyo,
Park Yun Hee,
Ryu Jeong Hee,
SONG Ho Young,
Woo Sung Ho,
Yang Jeon
Provided are methods of use of compounds comprising a self-immolative group, which compounds may include a protein (for example, an oligopeptide, a polypeptide, an antibody, or the like) having substrate-specificity for a target and an active agent (for example, a drug, a toxin, a ligand, a detection probe, or the like) having a specific function or activity. 3. The method of claim 1 , wherein W is —C(O)— claim 1 , —C(O)NR′— claim 1 , —C(O)O— claim 1 , —SONR′— claim 1 , —P(O)R″NR′— claim 1 , —SONR′— claim 1 , or —PONR′— claim 1 , and R′ and R″ are each independently hydrogen claim 1 , (C-C)alkyl claim 1 , (C-C)cycloalkyl claim 1 , (C-C)alkoxy claim 1 , (C-C)alkylthio claim 1 , mono-or di-(C-C)alkylamino claim 1 , (C-C)heteroaryl or (C-C)aryl.4. The method of claim 1 , wherein the linker L is alkylene having 1 to 50 carbon atoms and satisfies at least one of the following (i) to (iv):(i) the alkylene includes at least one unsaturated bond,(ii) the alkylene includes at least one heteroarylene,(iii) the carbon atom of the alkylene is substituted with one or more hetero atoms selected from nitrogen (N), oxygen (O), and sulfur (S), and(iv) the alkylene is further substituted with one or more alkyls having 1 to 20 carbon atoms.6. The method of claim 5 , wherein the linker L further includes a binding unit formed by 1 claim 5 ,3-dipolar cycloaddition reactions claim 5 , hetero-Diels Alder reactions claim 5 , nucleophilic substitution reactions claim 5 , non-aldol type carbonyl reactions claim 5 , additions to carbon-carbon multiple bonds claim 5 , oxidation reactions claim 5 , or click reactions.7. The method of claim 6 , wherein the binding unit is formed by a reaction between acetylene and azide claim 6 , or a reaction between an aldehyde or ketone group and hydrazine or hydroxylamine.9. The compound method of claim 6 , wherein the linker L further includes a connection unit represented by the following Chemical Formula F or G:{'br': None, 'sub': 2', 'r', '2', 'p', 'q, ...
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