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更新于：2025-03-20

KB-2683

更新于：2025-03-20

概要

概要

基本信息

药物类型

小分子化药

别名

靶点-

作用方式

调节剂

作用机制

免疫调节剂

治疗领域

免疫系统疾病皮肤和肌肉骨骼疾病

在研适应症-

非在研适应症

类风湿关节炎

原研机构

Organon KK

在研机构-

非在研机构

Organon KK

最高研发阶段终止临床1期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C16H13NO2S

InChIKeyRBCGOSAFAPGFGD-UHFFFAOYSA-N

CAS号122589-79-1

关联

100 项与 KB-2683 相关的临床结果

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100 项与 KB-2683 相关的转化医学

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100 项与 KB-2683 相关的专利（医药）

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项与 KB-2683 相关的文献（医药）

1996-01-01·Chemical and Pharmaceutical Bulletin

A Facile Synthetic Approach to Labeled 4-Acetoxy-2-(4-methylphenyl)benzothiazole.

作者: Noriyuki Hori ; Norihiko Seko ; Goro Tsukamoto ; Kohichiro Yoshino

To study the pharmacokinetics and metabolism of 4-acetoxy-2-(4-methylphenyl)benzothiazole (KB-2683), which has potential immunomodulating activity, a practical preparation of labeled KB-2683 was needed.An efficient method for the synthesis of ¹⁴C-labeled KB-2683 by means of procedures which include a metal-catalyzed cross-coupling reaction is described.

1994-03-01·Journal of Pharmaceutical and Biomedical Analysis3区 · 医学

Novel immunoaffinity extraction for liquid chromatographic determination of major metabolites of 4-acetoxy-2-(4-methylphenyl)benzothiazole in plasma

3区 · 医学

Article

作者: Toshio Nambara ; Shinichi Miyairi ; Junichi Goto ; Norio Awata ; Hitoshi Shimada

Group extraction of the metabolites of 4-acetoxy-2-(4-methylphenyl)benzothiazole has been achieved through the use of an immunoaffinity adsorbent. The antisera elicited from an immunogen, 4-hydroxy-2-(4-formylphenyl)benzothiazole O-carboxymethyloxime-bovine serum albumin conjugate, were characterized to have a broad affinity spectrum for major metabolites oxidized at the 4-methyl group of the benzene moiety. One millilitre of the immunoaffinity adsorbent prepared by immobilization of antibodies (12.5 mg ml-1) was capable of retaining up to 4 micrograms of benzothiazoles. The adsorbates were recovered quantitatively by elution with 90% (v/v) methanol without any interfering peaks on the high-performance liquid chromatogram. The peak-height ratio of each metabolite to an internal standard was plotted against the concentration of the former substance; good linearity was observed in the range of 10-500 ng ml-1.

1994-01-01·Biological and Pharmaceutical Bulletin4区 · 医学

Immunoaffinity Extraction of 4-Hydroxy-2-(4-methylphenyl)benzothiazole and Its Metabolites for Determination by Gas Chromatography-Mass Spectrometry.

4区 · 医学

Article

作者: Nambara, Toshio ; Toba, Fumio ; Awata, Norio ; Miyairi, Shinichi ; Ando, Masayuki ; Kato, Toyoaki ; Shimada, Hitoshi ; Goto, Junichi

Immunoaffinity extraction of 4-hydroxy-2-(4-methylphenyl)benzothiazole and its metabolites, together with the corresponding meta-isomers has been achieved by the use of an antibody raised against an immunogen, an O-carboxymethyloxime-bovine serum albumin conjugate of 4-hydroxy-2-(4-formylphenyl)benzothiazole. The antibody produced exhibited a broad spectrum of affinity, not only for metabolites oxidized at the 4-methyl group of the benzene moiety but also for the corresponding meta-isomers. Up to 4 micrograms in total of these benzothiazoles could be extracted on the immunoaffinity adsorbent and recovered almost quantitatively by elution with 90% methanol. The resulting chromatogram was free from any interference. The eluted compounds were derivatized by conversion to their methyl esters and/or trimethylsilyl ethers, and subsequently separated into individual benzothiazoles by means of gas chromatography-mass spectrometry. The derivatized compounds were monitored using a characteristic ion, [M-CH3]+., and the limit of detection was 10 fmole. The peak height ratio of each metabolite to its corresponding meta-isomer internal standard was plotted against the concentration of the former and good linearity was observed over the range 0.2-5 ng/ml.

100 项与 KB-2683 相关的药物交易

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