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36 条记录 (耗时 0.041 秒)

    Retinoid antagonists and use thereof
    1.
    发明授权
    Retinoid antagonists and use thereof 有权
    类视黄醇拮抗剂及其用途

    公开(公告)号：US06326397B1

    公开(公告)日：2001-12-04

    申请号：US09307009

    申请日：1999-05-07

    申请人： Werner Bollag ,  Michael Klaus ,  Peter Mohr ,  Paola Panina-Bordignon ,  Michael Rosenberger ,  Francesco Sinigaglia

    发明人： Werner Bollag ,  Michael Klaus ,  Peter Mohr ,  Paola Panina-Bordignon ,  Michael Rosenberger ,  Francesco Sinigaglia

    IPC分类号： A01N5300

    CPC分类号： C07C57/48 ,  C07C57/42

    摘要： The present invention relates to novel retinoid antagonists of the formula I wherein the dotted bond can be either hydrogenated or form a double bond; and, when the dotted bond forms a double bond, R1 is lower alkyl and R2 is hydrogen; and, when the dotted bond is hydrogenated, R1 and R2 taken together are methylene to form a cis-substituted cyclopropyl ring; R3 is hydroxy or lower alkoxy; R4 is alkyl or alkoxy; and R5 and R6 are, independently, a C4-12 alkyl or a 5-12 cycloalkyl substituent containing from 1-3 rings which are either unsubstituted or substituted with from 1-3 lower alkyl groups, with the carbon atom of R5 and R6 being linked to the remainder of the molecule to form a quaternary carbon atom pharmaceutically acceptable salts of carbocylic acids of the formula I; as well as method for the treatment of osteoporosis and preneoplastic and neoplastic diseases, and a method for reducing or abolishing adverse events in subjects receiving retinoid agonist treatment by administering a retinoid antagonist.

    摘要翻译： 本发明涉及式I的新型类视黄醇拮抗剂，其中虚线键可以被氢化或形成双键; 并且当虚线键形成双键时，R 1为低级烷基且R 2为氢; 并且当点键被氢化时，R 1和R 2一起为亚甲基以形成顺式取代的环丙基环; R3是羟基或低级烷氧基; R4是烷基或烷氧基; 并且R 5和R 6独立地是C 1-4烷基或含有1-3个环的5-12个环烷基取代基，它们是未取代的或被1-3个低级烷基取代，R5和R6的碳原子是 与分子的其余部分连接以形成式I的碳酸的药学上可接受的盐的季碳原子; 以及用于治疗骨质疏松症和肿瘤前和肿瘤性疾病的方法，以及通过施用类视黄醇拮抗剂减少或消除接受类视黄醇激动剂治疗的受试者的不良事件的方法。

    Steroid total synthesis process utilizing a cyanoalkyl A-ring precursor
    5.
    发明授权
    Steroid total synthesis process utilizing a cyanoalkyl A-ring precursor 失效
    使用氰基烷基A环前体的类固醇总合成方法

    公开(公告)号：US4071537A

    公开(公告)日：1978-01-31

    申请号：US735570

    申请日：1976-10-26

    申请人： Noal Cohen ,  Michael Rosenberger ,  Gabriel Saucy

    发明人： Noal Cohen ,  Michael Rosenberger ,  Gabriel Saucy

    IPC分类号： C07C255/45 ,  C07D309/04 ,  C07J1/00 ,  C07J75/00 ,  C07D309/22

    CPC分类号： C07D309/04 ,  C07C255/45 ,  C07J1/00 ,  C07J75/00 ,  C07C2103/16 ,  Y02P20/55

    摘要： A multi-step, stereospecific total synthesis of steroids utilizing intermediates having a cyanoalkyl A-ring precursor is disclosed. The initial starting materials for this process are the relatively inexpensive and commercially available reagents .gamma.-butyrolactone and sodium cyanide. The process is suitable for the preparation of racemic or optically active, medicinally valuable steroids, particularly 19-norsteroids. It is a feature of this process that conditions employed during the multiple step synthesis are selected so as to retain the normally labile nitrile group even during hydrogenation and hydrolysis steps. In this manner, it is possible to employ the nitrile group as an A-ring precursor without resorting to protective groups as was heretofore found necessary in previous steroid total synthesis processes.

    摘要翻译： 公开了使用具有氰基烷基A环前体的中间体的多步立体定向全合成类固醇。 该方法的初始起始原料是相对便宜且市售的试剂γ-丁内酯和氰化钠。 该方法适用于制备外消旋或光学活性的药用价值类固醇，特别是19-降胆固醇。 该方法的特征在于，选择在多步合成期间使用的条件，以便即使在氢化和水解步骤期间也保持正常不稳定的腈基。 以这种方式，可以使用腈基作为A环前体而不诉诸于以前在以前的类固醇总合成方法中必需的保护基。