17-amino substituted 4-azasteroid 5.alpha.-reductase inhibitors
    13.
    发明授权
    17-amino substituted 4-azasteroid 5.alpha.-reductase inhibitors 失效
    17-氨基取代的4-azasteroid5α-还原酶抑制剂

    公开(公告)号:US5639741A

    公开(公告)日:1997-06-17

    申请号:US338472

    申请日:1995-03-20

    CPC分类号: C07J73/005

    摘要: Novel amino substituted 4-azasteroid 5.alpha.-reductase inhibitors of formula (I). ##STR1## wherein A is (a), (b) or (c), are claimed as well as pharmaceutically acceptable salts and formulations thereof. These compounds are effective in inhibiting testosterone 5.alpha.-reductase(s) and are thus useful in the treatment of a number of hyperandrogenic conditions including benign prostatic hypertrophy, acne, seborrhea, female hirsutism, and male and female pattern baldness (alopecia).

    摘要翻译: PCT No.PCT / US93 / 04633 Sec。 371日期1995年3月20日 102(e)1995年3月20日PCT PCT 1993年5月17日PCT公布。 公开号WO93 / 23038 PCT 日期:1993年11月25日新颖的式(I)的氨基取代的4-azasteroid5α-还原酶抑制剂。 (a)(a)(b)(c)其中A为(a),(b)或(c))及其药学上可接受的盐和制剂 。 这些化合物有效抑制睾丸激素5α-还原酶,因此可用于治疗许多雄激素过多症状,包括良性前列腺肥大,痤疮,皮脂溢,女性多毛症以及男性和女性型秃发(脱发)。

    Arylsulfonyloxy purine intermediates
    17.
    发明授权
    Arylsulfonyloxy purine intermediates 失效
    芳基磺酰氧基嘌呤中间体

    公开(公告)号:US4897479A

    公开(公告)日:1990-01-30

    申请号:US165360

    申请日:1988-02-29

    IPC分类号: C07D473/00 C07F9/6561

    CPC分类号: C07D473/00 C07F9/65616

    摘要: Compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof are disclosed. In these compounds, R.sup.1 is halogen, --SR.sup.4 wherein R.sup.4 is H or alkyl of 1 to 4 carbon atoms, --OCH.sub.3, --OSO.sub.2 Ar wherein Ar is phenyl or alkyl substituted phenyl wherein the alkyl group has 1 to 6 carbon atoms, --NR.sup.4 R.sup.5 wherein R.sup.4 is as defined above and R.sup.5 is H, alkyl of 1 to 4 carbon atoms, amino, alkanoyl of 1 to 8 carbon atoms, benzoyl, methoxy or hydroxy or R.sup.1 is --N(CH.sub.3).sub.3.sup.+ X.sup.-whereinX is halogen or --OSO.sub.2 Ar wherein Ar is phenyl or alkyl substituted phenyl wherein the alkyl group has 1 to 6 carbon atoms;R.sup.2 is H, alkanoyl of 1 to 8 carbon atoms or benzoyl;R.sup.3 is A or B whereinA is ##STR2## and B is ##STR3## wherein R.sup.6 and R.sup.7 are independently selected from H and ##STR4## wherein R.sup.8 and R.sup.9 are independently selected from pharmaceutically acceptable cations and H, or R.sup.6 and R.sup.7 taken together are ##STR5## wherein R.sup.10 is selected from pharmaceutically acceptable cations and H; with the proviso that R.sup.4 is not H when: R.sup.5 is H, R.sup.3 is A, and R.sup.6 and R.sup.7 are H. The compounds have anti-viral activity.

    摘要翻译: 公开了式“IMAGE”的化合物及其药学上可接受的盐。 在这些化合物中,R 1是卤素,-SR 4,其中R 4是H或1-4个碳原子的烷基,-OCH 3,-OSO 2 Ar,其中Ar是苯基或烷基取代的苯基,其中烷基具有1-6个碳原子,-NR4R5其中 R 4如上所定义,R 5为H,具有1至4个碳原子的烷基,氨基,1至8个碳原子的烷酰基,苯甲酰基,甲氧基或羟基或R 1为-N(CH 3)3 + X-,其中X为卤素或 -OSO 2 Ar,其中Ar是苯基或烷基取代的苯基,其中烷基具有1至6个碳原子; R2是H,1-8个碳原子的烷酰基或苯甲酰基; R3是A或B,其中A是,B是,其中R6和R7独立地选自H和IMA,其中R8和R9独立地选自药学上可接受的阳离子,H或R6和R7一起 其中R 10选自药学上可接受的阳离子和H; 条件是当R 5为H,R 3为A且R 6和R 7为H时,R 4不为H。化合物具有抗病毒活性。