21-substituted progesterone derivatives as new antiprogestational agents
    1.
    发明授权
    21-substituted progesterone derivatives as new antiprogestational agents 有权
    21位替代孕酮衍生物作为新的抗孕剂

    公开(公告)号:US08003629B2

    公开(公告)日:2011-08-23

    申请号:US12641172

    申请日:2009-12-17

    Abstract: 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.

    Abstract translation: 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。

    Nandrolone 17 Beta-Carbonates
    2.
    发明申请
    Nandrolone 17 Beta-Carbonates 有权
    Nandrolone 17β-碳酸盐

    公开(公告)号:US20080167283A1

    公开(公告)日:2008-07-10

    申请号:US11815532

    申请日:2006-01-24

    CPC classification number: C07J1/0074

    Abstract: Disclosed are compounds of the formula (I) wherein R is C1-C30 alkyl, which may be optionally further substituted with one or more C5-C8 cycloalkyl groups, or a C5-C12 cycloalkyl, which may be optionally substituted with one or more C1-C30 alkyl groups, R′ is hydrogen or lower alkyl, R″ is a C1-C30 alkyl or halo, and the bond between C14 and C15 can be a single bond or double bond. Also disclosed are pharmaceutical compositions comprising such compounds and methods of use thereof. These compounds can find use in treating a number of diseases or conditions such as hypogonadism, hypergonadism, osteoporosis, and anemia, in providing hormonal therapy and contraception, as an anabolic agent, and in suppressing the release of hormones such as the luteinizing hormone.

    Abstract translation: 公开了式(I)的化合物,其中R是C 1 -C 30烷基,其可任选进一步被一个或多个C 5 - C 1 -C 8环烷基或C 5 -C 12环烷基,其可以任选地被一个或多个C 烷基或卤素,C14和C15之间的键可以是单键或双键。 还公开了包含这些化合物的药物组合物及其使用方法。 这些化合物可用于治疗许多疾病或病症如性腺机能不良,超神经痛,骨质疏松症和贫血,提供激素治疗和避孕作为合成代谢药物,以及抑制激素如黄体生成激素的释放。

    21-substituted progesterone derivatives as new antiprogestational agents
    3.
    发明授权
    21-substituted progesterone derivatives as new antiprogestational agents 有权
    21位替代孕酮衍生物作为新的抗孕剂

    公开(公告)号:US06861415B2

    公开(公告)日:2005-03-01

    申请号:US09180132

    申请日:1997-04-30

    Abstract: 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.

    Abstract translation: 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; R 2是选自卤素,烷基,酰基,羟基,烷氧基,酰氧基,碳酸烷基酯,Cypion氧基,S-烷基和S-酰基的成员。 R 3是选自烷基,羟基,烷氧基和酰氧基的成员; R 4是选自氢和烷基的成员; 并且X是选自= O和= N-OR 5的成员,其中R 5是选自氢和烷基的成员。除了提供式I化合物外, 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。

    21-substituted progesterone derivatives as new antiprogestational agents
    6.
    发明授权
    21-substituted progesterone derivatives as new antiprogestational agents 有权
    21位替代孕酮衍生物作为新的抗孕剂

    公开(公告)号:US07759330B2

    公开(公告)日:2010-07-20

    申请号:US11500627

    申请日:2006-08-07

    Abstract: 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.

    Abstract translation: 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。

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