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    21-SUBSTITUTED PROGESTERONE DERIVATIVES AS NEW ANTIPROGESTATIONAL AGENTS
    6.
    发明申请
    21-SUBSTITUTED PROGESTERONE DERIVATIVES AS NEW ANTIPROGESTATIONAL AGENTS 有权
    21替代的孕酮衍生物作为新的抗菌药物

    公开(公告)号：US20100113408A1

    公开(公告)日：2010-05-06

    申请号：US12641172

    申请日：2009-12-17

    申请人： Hyun K. Kim ,  Richard P. Blye ,  Pemmaraju N. Rao ,  James W. Cessac ,  Carmie K. Acosta

    发明人： Hyun K. Kim ,  Richard P. Blye ,  Pemmaraju N. Rao ,  James W. Cessac ,  Carmie K. Acosta

    IPC分类号： A61K31/56 ,  A61P15/00

    CPC分类号： C07J5/00 ,  C07J5/0053 ,  C07J7/00 ,  C07J7/0085 ,  C07J9/00 ,  C07J21/006 ,  C07J41/00 ,  C07J41/0016 ,  C07J41/0083 ,  C07J41/0094 ,  C07J51/00 ,  C07J71/001 ,  Y10S514/841

    摘要： A compound having the general formula: in which: R1 is a member selected from the group consisting of —OCH3, —SCH3, —N(CH3)2, —NHCH3, —CHO, —COCH3 and —CHOHCH3; R2 is a member selected from the group consisting of halogen, alkyl, acyl, hydroxy, alkoxy, acyloxy, alkyl carbonate, cypionyloxy, S-alkyl and S-acyl; R3 is a member selected from the group consisting of alkyl, hydroxy, alkoxy and acyloxy; R4 is a member selected from the group consisting of hydrogen and alkyl; and X is a member selected from the group consisting of ═O and ═N—OR5, wherein R5 is a member selected from the group consisting of hydrogen and alkyl.In addition to providing the compounds of Formula I, the present invention provides methods wherein the compounds of Formula I are advantageously used, inter alia, to antagonize endogenous progesterone; to induce menses; to treat endometriosis; to treat dysmenorrhea; to treat endocrine hormone-dependent tumors; to treat uterine fibroids; to inhibit uterine endometrial proliferation; to induce labor; and for contraception.

    摘要翻译： 具有以下通式的化合物：其中：R 1是选自-OCH 3，-SCH 3，-N（CH 3）2，-NHCH 3，-CHO，-COCH 3和-CHOHCH 3的成员; R2是选自卤素，烷基，酰基，羟基，烷氧基，酰氧基，碳酸烷基酯，环戊氧基，S-烷基和S-酰基的成员; R3是选自烷基，羟基，烷氧基和酰氧基的成员; R4是选自氢和烷基的成员; 并且X是选自由以下组成的组的成员：= O和= NO-OR 5，其中R 5是选自氢和烷基的成员。 除了提供式I化合物之外，本发明提供了其中式I化合物有利地用于拮抗内源性孕酮的方法; 诱发月经; 治疗子宫内膜异位症; 治疗痛经; 治疗内分泌激素依赖性肿瘤; 治疗子宫肌瘤; 抑制子宫内膜增生; 诱导劳动; 和避孕。

    One-pot processes for preparing prednisolone derivatives
    9.
    发明申请
    One-pot processes for preparing prednisolone derivatives 审中-公开
    制备泼尼松龙衍生物的一锅法

    公开(公告)号：US20070117974A1

    公开(公告)日：2007-05-24

    申请号：US11602479

    申请日：2006-11-20

    申请人： Minghua Ying ,  Dingwei Wu ,  Hongpeng Chen

    发明人： Minghua Ying ,  Dingwei Wu ,  Hongpeng Chen

    IPC分类号： C07J71/00

    CPC分类号： C07J71/00 ,  C07J7/00

    摘要： Disclosed is a one-pot process for the preparation of a prednisolone derivative of formula I, comprising reacting the compound of formula II with the compound of formula III and the compound of formula IV The process does not need to separate and purify the intermediate formed, and therefore the process reduces the reaction time and increases the yield of the product compared to the prior art.

    摘要翻译： 公开了用于制备式I泼尼松龙衍生物的一锅法，其包括使式II化合物与式III化合物和式IV化合物反应。该方法不需要分离和纯化形成的中间体， 因此与现有技术相比，该方法减少了反应时间并提高了产品的产率。

    Novel steroidal antiestrogens and antiandrogens and uses thereof
    10.
    发明申请
    Novel steroidal antiestrogens and antiandrogens and uses thereof 审中-公开
    新型甾体抗雌激素和抗雄激素及其用途

    公开(公告)号：US20060148773A1

    公开(公告)日：2006-07-06

    申请号：US11369582

    申请日：2006-03-07

    申请人： Robert Hanson ,  Carolyn Friel ,  Choon Lee

    发明人： Robert Hanson ,  Carolyn Friel ,  Choon Lee

    IPC分类号： C07J43/00 ,  A61K31/58 ,  A61K31/56 ,  C07J9/00

    CPC分类号： C07J9/00 ,  C07J5/00 ,  C07J7/00 ,  C07J17/00 ,  C07J71/00

    摘要： The present invention comprises the design, synthesis and development of a new class of chemotherapeutic agents for prophylactic and therapeutic treatments in a mammal, particularly a human, believed to be at risk of suffering from a hormone-responsive disorder. In an embodiment of the invention, such treatments include therapeutic compositions comprising novel steroidal antiestrogen and antiandrogen compounds. In a preferred embodiment, such a novel compound of the present invention has an address and a message component, which are made into a single composite entity for more aggressive intervention and effective treatment of hormone-responsive disorders, thereby prolonging the disease-free interval for the patient and reducing a number of side effects.

    摘要翻译： 本发明包括设计，合成和开发用于预防和治疗治疗的新一类化学治疗剂，其被认为具有患有激素反应性病症危险的哺乳动物，特别是人类。 在本发明的一个实施方案中，这种治疗包括包含新型甾族抗雌激素和抗雄激素化合物的治疗组合物。 在优选的实施方案中，本发明的这种新型化合物具有地址和消息组分，其被制成单个复合实体以用于更积极干预和有效治疗激素反应性病症，从而延长无疾病间隔 患者减少了一些副作用。