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    • 6. 发明申请
    • TETRAHYDROPYRIDAZINE DERIVATIVES
    • 四氢哒衍生品
    • WO2000059890A1
    • 2000-10-12
    • PCT/EP2000002275
    • 2000-03-15
    • MERCK PATENT GMBHROCHUS, JonasWOLF, MichaelBEIER, NorbertKLUXEN, Franz-WernerFITTSCHEN, Claus
    • MERCK PATENT GMBH
    • C07D237/04
    • A61K31/501A61K31/50C07D237/04C07D401/12
    • The invention relates to tetrahydropyridazine derivatives selected from the following group: 1-(4-ureido-benzoyl) -3-(3-ethoxy- 4-methoxy-phenyl) -1,4,5,6-tetrahydro- pyridazine, 1-(4-nicotinoylamino- benzoyl)-3- (3-propoxy-4- methoxyphenyl) -1,4,5,6-tetrahydro- pyridazine, 1-(4-trifluoracetamido- benzoyl)-3- (3-ethoxy-4- methoxyphenyl) -1,4,5,6-tetrahydro- pyridazine, 1-(4-ethoxycarbonylamino- benzoyl)-3- (3-propoxy-4- methoxyphenyl) -1,4,5,6-tetrahydro- pyridazine, 1-(4-isopropoxycarbonylamino- benzoyl)-3- (3-ethoxy-4- methoxyphenyl) -1,4,5,6-tetrahydro- pyridazine, 1-(4-propoxycarbonylamino- benzoyl)-3- (3-ethoxy-4- methoxyphenyl) -1,4,5,6-tetrahydro- pyridazine, 1-(4-nicotinoylamino- benzoyl)-3- (3,4-dimethoxyphenyl) -4-ethyl-1,4,5,6- tetrahydro- pyridazin, 1-(4-ethoxycarbonylamino- benzoyl)-3- (3,4-dimethoxyphenyl)- 4-ethyl-1,4,5,6- tetrahydro- pyridazine and 1-(4-acetamido- benzoyl)-3- (3,4-dimethoxyphenyl)- 4-ethyl-1,4,5,6- tetrahydro- pyridazine and their salts and solvates. Said tetrahydropyridazine derivatives present an inhibiting effect on phosphodiesterase IV and can be used for treating osteoporosis, tumours, arteriosclerosis, rheumatoid arthritis, multiple sclerosis, diabetes mellitus, inflammatory processes, allergies, asthma, autoimmune diseases and AIDS, atopic dermatitis, psoriasis and transplant rejection reactions.
    • Tetrahydropyridazinderivate选自1-(4-脲基苯甲酰基)-3-(3-乙氧基-4-甲氧基 - 苯基)-1,4,5,6-四氢哒嗪,1-(4-烟酰氨 - 苯甲酰基) -3-(3-丙氧基-4-甲氧基苯基)-1,4,5,6-四氢哒嗪,1-(4-三氟乙酰氨基苯甲酰基)-3-(3-乙氧基-4-甲氧基苯基)-1,4- ,5,6-四氢哒嗪,1-(4-乙氧羰基氨基苯甲酰基)-3-(3-丙氧基-4-甲氧基苯基)-1,4,5,6-四氢哒嗪,1-(4-异丙氧羰基 苯甲酰基)-3-(3-乙氧基-4-甲氧基苯基)-1,4,5,6-四氢哒嗪,1-(4-丙氧羰基苯甲酰基)-3-(3-乙氧基-4-甲氧基苯基)-1- -1,4,5,6-四氢 - 哒嗪,1-(4-烟酰氨 - 苯甲酰基)-3-(3,4-二甲氧基苯基)-4-乙基-1,4,5,6-四氢哒嗪,1-( 4-乙氧羰基氨基苯甲酰基)-3-(3,4-二甲氧基苯基)-4-乙基-1,4,5,6-四氢哒嗪和1-(4-乙酰氨基苯甲酰基)-3-(3,4- 二甲氧基苯基)-4-乙基-1,4,5,6-四氢哒嗪,以及它们的盐和溶剂化物,显示出磷酸二酯酶IV抑制和可以用于治疗骨质疏松症,肿瘤 S,动脉粥样硬化,类风湿性关节炎,多发性硬化,糖尿病,炎性过程,过敏,哮喘,自身免疫性疾病和AIDS,特应性皮炎,银屑病和移植排斥被使用。