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31 条记录 (耗时 0.021 秒)

    Process for preparing 24-fluoro-25-hydroxycholecalciferol
    1.
    发明授权
    Process for preparing 24-fluoro-25-hydroxycholecalciferol 失效
    制备24-氟-25-羟基胆钙化甾醇的方法

    公开(公告)号：US4305880A

    公开(公告)日：1981-12-15

    申请号：US189513

    申请日：1980-09-22

    申请人： Hector F. DeLuca ,  Yoko Tanaka ,  Nobuo Ikekawa ,  Yoshiro Kobayashi

    发明人： Hector F. DeLuca ,  Yoko Tanaka ,  Nobuo Ikekawa ,  Yoshiro Kobayashi

    IPC分类号： C07J9/00

    CPC分类号： C07J9/00 ,  C07J9/005

    摘要： The invention provides a new derivative of vitamin D.sub.3, 24-fluoro-25-hydroxycholecalciferol.The compound is characterized by vitamin D-like activity in its ability to increase intestinal calcium transport, increase serum calcium and inorganic phosphorous concentration and to prevent the development of rickets. It would find ready application as a substitute for vitamin D.sub.3 and in the treatment of disease states evincing calcium-phosphorous imbalance and which are nonresponsive to vitamin D.sub.3 therapy.

    摘要翻译： 本发明提供维生素D3，24-氟-25-羟基胆钙化甾醇的新衍生物。 该化合物的特征在于维生素D样活性增加肠钙运输能力，增加血清钙和无机磷浓度，并防止r the病的发展。 它可以作为维生素D3的替代品和治疗表现出钙磷不平衡的疾病状态，并且对维生素D3治疗无反应。

    24,24-Difluoro-1.alpha.,25-dihydroxycholecalciferol
    2.
    发明授权
    24,24-Difluoro-1.alpha.,25-dihydroxycholecalciferol 失效
    24,24-二氟-1α，25-二羟基胆钙化甾醇

    公开(公告)号：US4201881A

    公开(公告)日：1980-05-06

    申请号：US24848

    申请日：1979-03-28

    申请人： Hector F. DeLuca ,  Heinrich K. Schnoes ,  Nobuo Ikekawa ,  Yoko Tanaka ,  Yoshiro Kobayashi

    发明人： Hector F. DeLuca ,  Heinrich K. Schnoes ,  Nobuo Ikekawa ,  Yoko Tanaka ,  Yoshiro Kobayashi

    IPC分类号： A61K31/59 ,  A61P3/02 ,  A61P3/14 ,  C07C35/32 ,  C07C67/00 ,  C07C401/00

    CPC分类号： C07C401/00 ,  C07C35/52 ,  C07C2101/14 ,  C07C2102/24

    摘要： The invention provides new derivatives of vitamin D, 24,24-difluoro-1.alpha.,25-dihydroxycholecalciferol and 24,24-difluoro-1.alpha.,25-dihydroxy-5,6-trans-cholecalciferol and processes for preparing the same.The compounds are characterized by vitamin D-like activity essentially equivalent to the vitamin D-like activity of 1.alpha.,25-dihydrocholecalciferol which is considered to be the hormonal form and most active derivative of vitamin D. The compounds of this invention are characterized by their ability to increase intestinal calcium transport, increase serum calcium and to prevent the development of rickets. These compounds would find ready application as a substitute for vitamin D and in the treatment of disease states evincing metabolic calcium and phosphorus deficiencies.

    摘要翻译： 本发明提供维生素D，24,24-二氟-1α，25-二羟基胆钙化甾醇和24,24-二氟-1α，25-二羟基-5,6-反式胆钙化甾醇的新衍生物及其制备方法。 该化合物的特征在于维生素D样活性，其基本上等同于被认为是维生素D的激素形式和最活泼的衍生物的1α，25-二氢胆钙化醇的维生素D样活性。本发明的化合物的特征在于 增加肠钙运输能力，增加血清钙，防止r the病的发展。 这些化合物可以作为维生素D的替代物和治疗代谢钙和磷缺乏症的疾病状态得到准备。

    26,26,26,27,27-pentafluoro-1.alpha.-hydroxy-27-methoxyvitamin D.sub.3
    3.
    发明授权
    26,26,26,27,27-pentafluoro-1.alpha.-hydroxy-27-methoxyvitamin D.sub.3 失效
    26,26,26,27,27-五氟-1α-羟基-27-甲氧基维生素D3

    公开(公告)号：US4619920A

    公开(公告)日：1986-10-28

    申请号：US776342

    申请日：1985-09-16

    申请人： Hector F. DeLuca ,  Nobuo Ikekawa ,  Yoshiro Kobayashi ,  Yoko Tanaka

    发明人： Hector F. DeLuca ,  Nobuo Ikekawa ,  Yoshiro Kobayashi ,  Yoko Tanaka

    IPC分类号： C07J1/00 ,  C07C67/00 ,  C07C401/00 ,  C07J9/00

    CPC分类号： C07C401/00 ,  C07J9/00

    摘要： The invention provides a new derivative of vitamin D.sub.3, 26,26,26,27,27-pentafluoro-1.alpha.-hydroxy-27-methoxy-cholecalciferol and a process for preparing the same.The compound is characterized by some vitamin D-like activity except that it exhibits negligible activity in mobilizing bone. This characteristic indicates that the compound would find ready application in the treatment of disease or physiological states which evince loss of bone mass and application in other situations where metabolic calcium imbalances are found.

    摘要翻译： 本发明提供维生素D3,26,26,26,27,27-五氟-1α-羟基-27-甲氧基胆钙化甾醇的新衍生物及其制备方法。 该化合物的特征在于一些维生素D样活性，除了它在动员骨中显示出可忽略的活性。 该特征表明该化合物可用于治疗疾病或生理状态，这些疾病或生理状态证明骨质量的损失和在发现代谢钙不平衡的其他情况下的应用。

    23,23-Difluoro-25-hydroxy-vitamin D.sub.3 and process for preparing same
    7.
    发明授权
    23,23-Difluoro-25-hydroxy-vitamin D.sub.3 and process for preparing same 失效
    23,23-二氟-25-羟基维生素D3及其制备方法

    公开(公告)号：US4564474A

    公开(公告)日：1986-01-14

    申请号：US639776

    申请日：1984-08-13

    申请人： Hector F. DeLuca ,  Yoko Tanaka ,  Nobuo Ikekawa ,  Yoshiro Kobayashi

    发明人： Hector F. DeLuca ,  Yoko Tanaka ,  Nobuo Ikekawa ,  Yoshiro Kobayashi

    IPC分类号： C07C401/00 ,  C07J9/00 ,  C07J17/00 ,  C07J31/00 ,  C07J51/00 ,  C07J53/00

    CPC分类号： C07J17/00 ,  C07C401/00 ,  C07J31/006 ,  C07J51/00 ,  C07J53/00 ,  C07J9/00 ,  C07J9/005

    摘要： The invention provides new derivatives of vitamin D, 23,23-difluoro-25-hydroxycholecalciferol and the acylates thereof, a method for preparing said compounds and various new intermediates utilized in such process.The derivative compounds are characterized by vitamin D-like activity as evidenced by their ability to increase intestinal calcium transport and serum calcium. The compounds are further characterized by resistance to hydroxylation at C-23, which is recognized as an essential metabolic step to the inactivation of vitamin D. The compounds should, therefore, provide vitamin D-like activity of greater time duration.

    摘要翻译： 本发明提供了维生素D，23,23-二氟-25-羟基胆钙化甾醇及其酰化物的新衍生物，该方法用于制备所述化合物和各种新的中间体。 衍生化合物的特征在于维生素D样活性，其证据是其增加肠钙运输和血清钙的能力。 该化合物的进一步特征在于C-23的抗羟化反应，其被认为是维生素D失活的基本代谢步骤。因此，化合物应当提供更长时间的维生素D样活性。