摘要:
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.
摘要翻译:式(I)的N- phenylarylsulfonylamide化合物(R 1是COOH等; R 2为氢,甲基,等; R 3和R 4是甲基和甲基的组合,等等; R 5为异丙基等。 Ar是噻唑基,吡啶基,5-甲基-2-呋喃基各自与甲基OPTIONALLY substituiertem; n是零或1),的合成中间体的化合物及其制备方法。 式(I)的化合物结合到前列腺素E 2受体,尤其是爱到EP 1亚型受体,并拮抗它。 它较少受蛋白结合的影响,因此它在体内具有活性的令人满意的。 因此,它被认为是作为解热剂的镇痛剂,用于或抗肿瘤剂的尿频(尿频)和/或下泌尿道疾病综合征的治疗的药剂。
摘要:
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.