258516-84-6Relevant academic research and scientific papers
Conjugate of cytotoxin molecule and cell binding receptor molecule
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Paragraph 0066, (2019/10/10)
A conjugate of a strong cytotoxin molecule and a cell binding receptor molecule has a structure shown in a molecular formula (I), wherein T, L, m, n, -----, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and R13 are defined in the text. The conjugate is used for treating cancer, immunological diseases and infectious diseases.
CONJUGATE OF CELL-BINDING RECEPTOR WITH CYTOTOXIC AGENT
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Page/Page column 135, (2017/10/31)
PROBLEM TO BE SOLVED: To provide a conjugate of a potent cytotoxic agent with a cell-surface receptor binding molecule for targeted treatment. SOLUTION: According to the present invention, there is provided a conjugate having a structure of formula (I) and a pharmaceutical acceptable salt and a solvate thereof. The conjugate is used for treating cancer, autoimmune disease, and infectious disease. (T is a targeting or binding ligand; L is a releasable linker; a broken line is a linkage bond that L connects to a molecule inside the bracket independently; n is an integer of 1 to 20; m is an integer of 1 to 10; and a structure in parentheses is a potent antimitotic agent/drug.) SELECTED DRAWING: None COPYRIGHT: (C)2017,JPOandINPIT
METHODS OF BLADDER CANCER TREATMENT WITH CICLOPIROX, CICLOPIROX OLAMINE, OR A CICLOPIROX PRODRUG
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Paragraph 0104, (2016/06/06)
A method of treating bladder cancer is provided. The method of treating bladder cancer can include: providing a pharmaceutical composition having ciclopirox or ciclopirox olamine or a ciclopirox-POM prodrug having a structure of one of the formulae provided herein or derivative thereof or stereoisomer thereof or pharmaceutically acceptable salt thereof; and administering the pharmaceutical composition to a subject having the bladder cancer. The ciclopirox or ciclopirox olamine or a ciclopirox-POM prodrug can be administered in a therapeutically effective amount.
PHENOL DERIVATIVE AND PREPARATION METHOD AND USE IN MEDICINE THEREOF
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Paragraph 0362; 0363; 0364; 0365, (2016/05/02)
The present invention relates to a phenol derivative and the preparation method and use in medicine thereof, and particular to a phenol derivative represented by general formula (A) or a stereoisomer, a solvate, a metabolite, a prodrug, a pharmaceutically
PHENOL DERIVATIVE AND PREPARATION METHOD AND USE IN MEDICINE THEREOF
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Paragraph 1019; 1022; 1023-1025, (2016/10/10)
The present invention relates to a phenol derivative and the preparation method and use in medicine thereof, and particular to a phenol derivative represented by general formula (A) or a stereoisomer, a solvate, a metabolite, a prodrug, a pharmaceutically
METHOD OF TREATMENT WITH PRODRUGS OF 6-CYCLOHEXYL-1-HYDROXY-4-METHYLPYRIDIN IN-2-1H-ONE AND DERIVATIVES THEREOF
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Paragraph 0072, (2015/04/28)
A prodrug can have a structure of Formula 10 or derivative thereof or stereoisomer thereof or pharmaceutically acceptable salt thereof. The prodrug can be included in a pharmaceutical composition for use in treatment of fungus, cancer, dermatitis, superficial mycoses; inflammation, tinea pedis, tinea cruris, and tinea corporis, Trichophyton rubrum, Trichophyton mentagrophytes, Epidermophyton floccosum, and Microsporum canis, candidiasis (moniliasis), Candida albicans, tinea (pityriasis) vesicolor, Malassezia furfur, acute myeloid leukemia, acute lymphoid leukemia, chronic myelogenous leukemia, lymphoma or multiple myeloma.
Fluorescence probe for lysophospholipase C/NPP6 activity and a potent NPP6 inhibitor
Kawaguchi, Mitsuyasu,Okabe, Takayoshi,Okudaira, Shinichi,Hanaoka, Kenjiro,Fujikawa, Yuuta,Terai, Takuya,Komatsu, Toru,Kojima, Hirotatsu,Aoki, Junken,Nagano, Tetsuo
supporting information; experimental part, p. 12021 - 12030 (2011/10/02)
Nucleotide pyrophosphatases/phosphodiesterases (NPPs) are ubiquitous membrane-associated or secreted ectoenzymes that have a role in regulating extracellular nucleotide and phospholipid metabolism. Among the members of the NPP family, NPP1 and -3 act on nucleotides such as ATP, while NPP2, -6, and -7 act on phospholipids such as lysophosphatidylcholine and sphingomyelin. NPP6, a recently characterized NPP family member, is a choline-specific glycerophosphodiester phosphodiesterase, but its functions remain to be analyzed, partly due to the lack of highly sensitive activity assay systems and practical inhibitors. Here we report synthesis of novel NPP6 fluorescence probes, TG-mPC and its analogues TG-mPC3C, TG-mPC5C, TG-mPENE, TG-mPEA, TG-mPhos, TG-mPA, TG-mPMe, and TG-mPPr. Among the seven NPPs, only NPP6 hydrolyzed TG-mPC, TG-mPC3C, and TG-mPENE. TG-mPC was hydrolyzed in the cell lysate from NPP6-transfected cells, but not control cells, showing that it is suitable for use in cell-based NPP6 assays. We also examined the usefulness of TG-mPC as a fluorescence imaging probe. We further applied TG-mPC to carry out high-throughput NPP6 inhibitor screening and found several NPP6-selective inhibitors in a library of about 80 000 compounds. Through structure-activity relationship (SAR) analysis, we identified a potent and selective NPP6 inhibitor with an IC50 value of 0.21 μM. Our NPP6-selective fluorescence probe, TG-mPC, and the inhibitor are expected to be useful to elucidate the biological function of NPP6.
QUINOLINE DERIVATIVES
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Page/Page column 56-58, (2008/06/13)
The invention relates to new quinoline derivatives which are active CLK-1 inhibitors. More specifically, the CLK-1 inhibitors of the invention are compounds of formula (A). The invention also relates to pharmaceutical compositions comprising such compounds and to methods for the prophylaxis and/or treatment of disorders or their associated symptoms for which the inhibition of CLK-1 is beneficial.
A novel synthetic route for the preparation of alkyl and benzyl chloromethyl phosphates
M?ntyl?, Antti,Veps?l?inen, Jouko,J?rvinen, Tomi,Nevalainen, Tapio
, p. 3793 - 3794 (2007/10/03)
An efficient and simple synthesis is described for the production of various chloromethyl phosphates as useful reagents for the preparation of phosphonooxymethyl prodrugs.
