N-phenyl-arylsulfonamide compound, drug comprising the compound as active ingredient, intermediate for the compound

通式(I)代表的N-苯基芳基磺酰胺化合物,用于该化合物的中间体;以及制备这些化合物的方法。通式(I)的化合物与前列腺素E#-[2]受体,特别是EP#-[1]亚型受体,结合,并且拮抗它,并且通式(I)化合物因为较少受蛋白质结合的影响,所以具有令人满意的体内活性。因此,它可以用作止痛剂、解热剂、用于治疗尿频或下泌尿道疾病综合征的药剂或抗肿瘤剂。在式I中,R#+[1]代表COOH等;R#+[2]代表氢、甲基等;R#+[3]和R#+[4]代表甲基和甲基的组合等;R#+[5]代表异丙基等;Ar代表任选被甲基取代的噻唑基、吡啶基或5-甲基-2-呋喃基;n为零或1。 An N-phenylarylsulfo...

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Hauptverfasser: NEGANAWA ATSUSHI, SAITOH TETSUJI, KOBAYASHI KAORU
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Sprache:chi ; eng
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Zusammenfassung:通式(I)代表的N-苯基芳基磺酰胺化合物,用于该化合物的中间体;以及制备这些化合物的方法。通式(I)的化合物与前列腺素E#-[2]受体,特别是EP#-[1]亚型受体,结合,并且拮抗它,并且通式(I)化合物因为较少受蛋白质结合的影响,所以具有令人满意的体内活性。因此,它可以用作止痛剂、解热剂、用于治疗尿频或下泌尿道疾病综合征的药剂或抗肿瘤剂。在式I中,R#+[1]代表COOH等;R#+[2]代表氢、甲基等;R#+[3]和R#+[4]代表甲基和甲基的组合等;R#+[5]代表异丙基等;Ar代表任选被甲基取代的噻唑基、吡啶基或5-甲基-2-呋喃基;n为零或1。 An N-phenylarylsulfonylamide compound of formula (I) (R 1 is COOH etc .; R 2 is hydrogen, methyl, etc .; R 3 and R 4 are a combination of methyl and methyl, etc .; R 5 is isopropyl etc .; Ar is thiazolyl, pyridyl, 5-methyl-2-furyl each optionally substituted with methyl; n is zero or 1), a synthetic intermediate for the compound and a process for its preparation. The compound of formula (I) binds to a prostaglandin E 2 receptor, especially an EP 1 subtype receptor, and antagonizes it. It is less affected by protein binding, so it has a satisfactory in vivo activity. Therefore, it is considered to be useful as an analgesic, an antipyretic agent, an agent for the treatment of pollakiuria (frequent urination) and/or lower urinary tract disease syndrome or an antineoplastic agent.