申请人:Teikoku Hormone Mfg. Co., Ltd.
公开号:US06762205B1
公开(公告)日:2004-07-13
Phenyl sulfamate derivatives represented by the following formula or salts thereof have a powerful inhibitory effect on steroid sulfatase and are hence useful for the prophylaxis or treatment of diseases associated with steroids such as estrogens, such as breast cancer, corpus uteri cancer, endometrial hyperplasia, infertility, endometriosis, adenomyosis uteri, autoimmune disease, dementia or Alzheimer's disease.
wherein R1 and R2 each independently represent a hydrogen atom or a lower alkyl group; R3 represents a hydrogen atom, a halogen atom, a lower alkyl group, —OSO2NR1R2, a lower alkanoylamino group, a nitro group or a cyano group; and A represents a substituted or unsubstituted phenyl group, a group of the formula —X—NR4R5, or the like.
以下公式所代表的苯磺酰胺衍生物或其盐对类固醇磺酸酶具有强大的抑制作用,因此对于预防或治疗与类固醇有关的疾病,如雌激素,如乳腺癌,子宫体癌,子宫内膜增生,不孕症,子宫内膜异位症,子宫内膜腺肌症,自身免疫疾病,痴呆或阿尔茨海默病等有用。其中,R1和R2各自独立地表示氢原子或低碳基;R3表示氢原子,卤素原子,低碳基,-OSO2NR1R2,低脂肪酰氨基基团,硝基或氰基;A表示取代或未取代的苯基,-X-NR4R5基团等。