Cyclic aminophenyl sulfamate derivative
    3.
    发明申请
    Cyclic aminophenyl sulfamate derivative 有权
    环氨基苯基氨基磺酸酯衍生物

    公开(公告)号:US20060189625A1

    公开(公告)日:2006-08-24

    申请号:US10558253

    申请日:2004-05-07

    CPC分类号: C07D211/32 C07D211/14

    摘要: This invention provides cyclicamino-phenyl sulfamate derivatives represented by a formula wherein each of R1 and R2 stands for hydrogen or lower alkyl; each of R3 and R4 stands for hydrogen, halogen, cyano or the like; A stands for nitrogen or CH; B stands for CH2, SO2, CO, optionally substituted phenyl or the like; and R5 stands for alkyl, phenyl, amino or the like, or salts thereof which exhibit excellent steroid sulfatase inhibitory activity and are useful for prevention or treatment of diseases associated with steroids such as estrogen, androgen and the like.

    摘要翻译: 本发明提供由下式表示的环氨基 - 苯基氨基磺酸酯衍生物,其中R 1和R 2各自代表氢或低级烷基; R 3和R 4中的每一个代表氢,卤素,氰基等; A代表氮或CH; B代表CH 2,SO 2,CO,任选取代的苯基等; R 5表示烷基,苯基,氨基等,或其盐,其表现出优异的类固醇硫酸酯酶抑制活性,并且可用于预防或治疗与类固醇如雌激素,雄激素相关的疾病, 喜欢。

    3-substituted-D-homo-1,3,5(10)-estratriene derivatives
    5.
    发明授权
    3-substituted-D-homo-1,3,5(10)-estratriene derivatives 失效
    3-取代-D-均一1,3,5(10) - 三亚甲基衍生物

    公开(公告)号:US6087347A

    公开(公告)日:2000-07-11

    申请号:US254734

    申请日:1999-03-12

    CPC分类号: C07J73/005 C07J73/003

    摘要: Estratriene derivatives of the following formula have a powerful inhibitory effect on estrone sulfatase and are hence useful for the prophylaxis or treatment of diseases caused by estrogens, such as breast cancer, uterine cancer, ovarian cancer, endometriosis, adenomyosis uteri and mastopathy. ##STR1## wherein one of A and B represents C.dbd.O or CH.sub.2 and the other represents O or NH; and R represents --SO.sub.2 NR.sup.1 R.sup.2 or --PO(OM).sub.2 in which R.sup.1 and R.sup.2 each independently represent a hydrogen atom or a lower alkyl group and M represents a hydrogen atom or an alkali metal; provided that, when one of A and B represents NH, the other represents C.dbd.O.

    摘要翻译: PCT No.PCT / JP97 / 03188 Sec。 371 1999年3月12日 102(e)1999年3月12日PCT PCT 1997年9月10日PCT公布。 出版物WO98 / 11124 1998年3月19日下列配方的亚氨基衍生物对雌酮硫酸酯酶具有强大的抑制作用,因此可用于预防或治疗由雌激素引起的疾病,如乳腺癌,子宫癌,卵巢癌,子宫内膜异位症,子宫腺肌症和子宫腺肌症; 乳腺病 其中A和B之一表示C = O或CH 2,另一个表示O或NH; R表示-SO 2 NR 1 R 2或-PO(OM)2,其中R 1和R 2各自独立地表示氢原子或低级烷基,M表示氢原子或碱金属; 条件是当A和B之一表示NH时,另一个表示C = O。

    7-substituted oxa- or azasteroid compound
    6.
    发明授权
    7-substituted oxa- or azasteroid compound 失效
    7-取代的氧杂 - 或氮杂甾族化合物

    公开(公告)号:US5539127A

    公开(公告)日:1996-07-23

    申请号:US403867

    申请日:1995-03-24

    CPC分类号: C07J73/005 C07J73/003

    摘要: A steroid compound represented by the formula ##STR1## which has an excellent aromatase-inhibiting effect and is useful for preventing or treating diseases caused by estrogens, such as breast cancer, uterine cancer and prostatomegaly. This compound has an oxygen or nitrogen atom as the heteroatom at the position A of the ring D and the 7-position (substituent R.sup.1) of the skeleton is substituted by --S--R.sup.2 (wherein R.sup.2 represents hydrogen, lower alkyl which may be substituted by hydroxy, amino or lower alkoxycarbonyl, lower alkenyl, aralkyl, aryl which may be substituted by halogen, amino, di(lower alkyl)amino, lower alkoxy or lower alkyl, acyl, or lower alkoxycarbonyl), --S(O)m--R.sub.3 (wherein R.sup.3 represents lower alkyl; and m represents 1 or 2), or aralkyl.

    摘要翻译: PCT No.PCT / JP93 / 01390 Sec。 371日期:1995年3月24日 102(e)1995年3月24日PCT PCT 1993年9月29日PCT公布。 出版物WO94 / 07908 日期1994年04月14日由具有优异芳香酶抑制作用的式“IMAGE”表示的类固醇化合物,可用于预防或治疗由雌激素(例如乳腺癌,子宫癌和前列腺肥大)引起的疾病。 该化合物在环D的位置A具有氧原子或氮原子作为杂原子,并且骨架的7-位(取代基R 1)被-S-R 2取代(其中R 2表示氢,可被取代的低级烷基 可被卤素取代的芳基,氨基,二(低级烷基)氨基,低级烷氧基或低级烷基,酰基或低级烷氧羰基),-S(O)m - R3(其中R3表示低级烷基,m表示1或2)或芳烷基。