Studies on Disease-Modifying Antirheumatic Drugs. II. Synthesis and Activity of the Metabolites of Ethyl 4-(3,4-Dimethoxyphenyl)-6,7-dimethoxy-2-(1,2,4-triazol-1-ylmethyl)quinoline-3-carboxylate (TAK-603)
スポンサーリンク
概要
- 論文の詳細を見る
The metabolites of ethyl 4-(3,4-dimethoxyphenyl)-6,7-dimethoxy-2-(1,2,4-triazol-1-ylmethyl)quinoline-3-carboxylate (1,TAK-603), which is under clinical evaluation as a new type of disease-modifying antirheumatic drug (DMARD), were prepared to confirm their structures and to study their pharmacological properties. Of the metabolites identified, the 4-(4-hydroxy-3-methoxyphenyl) derivative (2c, M-I) was found to have an anti-inflammatory effect in an adjuvant arthritic rat model, although its potency in this model was slightly lower than that of the parent compound.
- 公益社団法人日本薬学会の論文
- 1998-07-15
著者
-
左右田 隆
武田薬品工業株式会社医薬研究本部
-
Sohda T
Takeda Chemical Industries Ltd. Pharmaceutical Research Division
-
Makino H
Pharmaceutical Research Division Takeda Chemical Industries Ltd.
-
Ohta Y
Fujita Health Univ. School Of Medicine Aichi Jpn
-
Ohta Yoshikazu
Pharmacology Research Laboratories Ii Takeda Pharmaceutical Company
-
BABA Atsuo
Pharmaceutical Research Division Takeda Chemical Industries, Ltd.,
-
MAKINO Haruhiko
Pharmaceutical Research Division Takeda Chemical Industries, Ltd.,
-
SOHDA Takashi
Pharmaceutical Research Division Takeda Chemical Industries, Ltd.,
-
Baba A
Pharmaceutical Research Division Takeda Chemical Industries Ltd.
-
Ohta Yoshikazu
Pharmaceutical Research Division, Takeda Chemical Industries, Ltd.,
関連論文
- インスリン抵抗性改善薬ピオグリタゾンの創製
- Studies on Antidiabetic Agents. II. Synthesis of 5-[4-(1-Methylcyclohexylmethoxy)-benzyl] thiazolidine-2,4-dione (ADD-3878) and Its Derivatives
- Studies on Antidiabetic Agents. I. Synthesis of 5-[4-(2-Methyl-2-phenylpropoxy)-benzyl] thiazolidine-2,4-dione (AL-321) and Related Compounds
- 新規抗リウマチ薬TAK-603の骨吸収抑制作用
- Studies on Antidiabetic Agents. XII. Synthesis and Activity of the Metabolites of (±)-5-[p-[2-(5-Ethyl-2-pyridyl)ethoxy]benzyl]-2,4-thiazolidinedione (Pioglitazone)
- Studies on Antidiabetic Agents. X. Synthesis and Biological Activities of Pioglitazone and Related Compounds
- 骨芽細胞分化促進作用を有する新規3-ベンゾチエピン誘導体TAK-778による in vitro および in vivo の骨形成促進作用
- New 1,4-Dihydropyridine Derivatives with Potent and Long-Lasting Hypotensive Effect
- Studies on Antidiabetic Agents. VI. Asymmetric Transformation of (±)-5-[4-(1-Methylcyclohexylmethoxy) benzyl]-2,4-thiazolidinedione (Ciglitazone) with Optically Active 1-Phenylethylamines
- Studies on Antidiabetic Agents. IV. Synthesis and Activity of the Metabolites of 5-[4-(1-Methylcyclohexylmethoxy) benzyl]-2,4-thiazolidinedione (Ciglitazone)
- Antiulcer Activity of 5-Benzylthiazolidine-2,4-dione Derivatives
- Studies on Antidiabetic Agents. III. 5-Arylthiazolidine-2,4-diones as Potent Aldose Reductase Inhibitors
- Increased phosphorylation of Akt in triple-negative breast cancers
- Studies on Non-Thiazolidinedione Antidiabetic Agents. 1. Discovery of Novel Oxyiminoacetic Acid Derivatives
- Studies on Disease-Modifying Antirheumatic Drugs. III. Bone Resorption Inhibitory Effects of Ethyl 4-(3,4-Dimethoxyphenyl)-6,7-dimethoxy-2-(1,2,4-triazol-1-ylmethyl)quinoline-3-carboxylate (TAK-603) and Related Compounds
- Studies on Disease-Modifying Antirheumatic Drugs. IV. Synthesis of Novel Thieno[2,3-b : 5,4-c']dipyridine Derivatives and Their Anti-inflammatory Effect
- Studies on Disease-Modifying Antirheumatic Drugs. II. Synthesis and Activity of the Metabolites of Ethyl 4-(3,4-Dimethoxyphenyl)-6,7-dimethoxy-2-(1,2,4-triazol-1-ylmethyl)quinoline-3-carboxylate (TAK-603)