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    Preparation of Ambrox from Labdanes of Dysoxylum hongkongense, and the Preparation of New Diterpenoids from Dysoxylum hongkongense
    6.
    发明申请
    Preparation of Ambrox from Labdanes of Dysoxylum hongkongense, and the Preparation of New Diterpenoids from Dysoxylum hongkongense 有权
    香from from from ense ense ense ense ense ense ense ense ense ense ense ense ense ense ense ense ense ense ense ense ense ense ense ense ense ense ense ense ense ense

    公开(公告)号：US20160046593A1

    公开(公告)日：2016-02-18

    申请号：US14548374

    申请日：2014-11-20

    Applicant: National Taiwan University

    Inventor： YA-CHING SHEN

    IPC: C07D307/92 ,  C07C49/743 ,  C07C45/78

    CPC classification number: C07D307/92 ,  C07C45/78 ,  C07C45/79 ,  C07C49/743 ,  C07C2602/28

    Abstract: The present invention discloses eight new diterpenoids, i.e. Dysongensins A to H, extracted from the leaves and twigs of Dysoxylum hongkongense, wherein AMBROX® which is applicable in the perfume industry is prepared from Dysongensin A via a series of chemical reactions, and the cytotoxicity of Dysongensins A to H against human cancer cell lines and their antiviral and anti-inflammatory activities are determined. Therefore, in the present invention, AMBROX® prepared from Dysongensin A is a new idea for application as an odorous compound in the perfume industry, and the novel diterpenoids can be prepared as a pharmaceutical compositions and/or a drug having antiviral, anti-inflammatory and/or anti-cancer activities.

    Abstract translation: 本发明公开了从香叶苦参的叶子和枝条提取的八种新的二萜类化合物，即丹参素A至H，其中可应用于香精工业的AMBROX®通过一系列化学反应由丹参素A制备，细胞毒性 测定对人类癌细胞系的依赖菌素A至H及其抗病毒和抗炎活性。 因此，在本发明中，由Densongensin A制备的AMBROX®是在香水工业中作为恶臭化合物应用的新思路，新颖的二萜类化合物可以制备成具有抗病毒，抗炎作用的药物组合物和/或药物 和/或抗癌活动。

    D-homo vitamin D.sub.3 derivatives
    8.
    发明授权
    D-homo vitamin D.sub.3 derivatives 失效
    D-homo维生素D3衍生物

    公开(公告)号：US5919986A

    公开(公告)日：1999-07-06

    申请号：US170453

    申请日：1998-10-13

    Applicant: Pierre Barbier ,  Franz Bauer ,  Peter Mohr ,  Marc Muller ,  Wolfgang Pirson

    Inventor： Pierre Barbier ,  Franz Bauer ,  Peter Mohr ,  Marc Muller ,  Wolfgang Pirson

    IPC: C07C35/36 ,  C07C45/29 ,  C07C49/743 ,  C07F7/18 ,  C07C49/115 ,  C07C35/08

    CPC classification number: C07F7/1856 ,  C07C35/36 ,  C07C45/292 ,  C07C49/743

    Abstract: Compounds of formula I: ##STR1## wherein the dotted carbon-carbon bond in the D-ring is C--C or C.dbd.C; C(R,R) is CH.sub.2 or C.dbd.CH.sub.2,R.sup.1 is H, F or OH,R.sup.2 and R.sup.3 are each independently C.sub.1-4 -alkyl or CF.sub.3, or together with the carbon to which they are bound form C.sub.3-6 -cycloalkyl.are useful in the treatment of vitamin D dependent disorders, such as psoriasis, leukemia; acne and seborrhoic dermatitis; osteoporosis hyperparathyroidism accompanying renal failure; and multiple sclerosis.

    Abstract translation: 式I化合物：其中D环中的点状碳 - 碳键为C-C或C = C; C（R，R）是CH 2或C = CH 2，R 1是H，F或OH，R 2和R 3各自独立地是C 1-4 - 烷基或CF 3，或与它们结合的碳一起形成C 3-6 - 环烷基。 可用于治疗维生素D依赖性疾病，如牛皮癣，白血病; 痤疮和脂溢性皮炎; 伴有肾衰竭的骨质疏松性甲状旁腺功能亢进; 和多发性硬化症。

    2-alkylidene-19-nor-vitamin D compounds
    9.
    发明授权
    2-alkylidene-19-nor-vitamin D compounds 失效
    2-亚烷基-19-去甲维生素D化合物

    公开(公告)号：US5843928A

    公开(公告)日：1998-12-01

    申请号：US819693

    申请日：1997-03-17

    Applicant: Hector F. Deluca ,  Sicinski R. Rafal

    Inventor： Hector F. Deluca ,  Sicinski R. Rafal

    IPC: A61K31/593 ,  A61P19/08 ,  A61P19/10 ,  C07C35/17 ,  C07C49/743 ,  C07C69/732 ,  C07C69/757 ,  C07C401/00 ,  C07F7/18 ,  C07F9/53 ,  C07F19/00 ,  A61K31/59

    CPC classification number: C07F7/1856 ,  C07C401/00 ,  C07F7/1852 ,  Y02P20/55

    Abstract: This invention provides a novel class of vitamin D related compounds, namely, the 2-alkylidene-19-nor-vitamin D derivatives, as well as a general method for their chemical synthesis. The compounds have the formula: ##STR1## where Y.sub.1 and Y.sub.2, which may be the same or different, are each selected from the group consisting of hydrogen and a hydroxy-protecting group, R.sub.6 and R.sub.8, which may be the same or different, are each selected from hydrogen, alkyl, hydroxyalkyl and fluoroalkyl, or when taken together represent the group --(CH.sub.2).sub.x -- where x is an integer from 2 to 5, and where the group R represents any of the typical side chains known for vitamin D type compounds. These 2-substituted compounds are characterized by low intestinal calcium transport activity and high bone calcium mobilization activity resulting in novel therapeutic agents for the treatment of diseases where bone formation is desired, particularly low bone turnover osteoporosis. These compounds also exhibit pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as anti-cancer agents and for the treatment of diseases such as psoriasis.

    Abstract translation: 本发明提供了一类维生素D相关化合物，即2-亚烷基-19-去甲维生素D衍生物，以及它们的化学合成的一般方法。 化合物具有下式：其中Y 1和Y 2可以相同或不同，各自选自氢和羟基保护基，R6和R8可以相同或不同， 各自选自氢，烷基，羟基烷基和氟烷基，或者一起表示基团 - （CH 2）x - ，其中x是2至5的整数，并且其中基团R表示维生素已知的任何典型侧链 D型化合物。 这些2-取代的化合物的特征在于低钙运输活性和高的钙钙动员活性，导致用于治疗需要骨形成，特别是低骨转换性骨质疏松症的疾病的新型治疗剂。 这些化合物在阻止未分化细胞的增殖并诱导其分化为单核细胞方面也表现出显着的活性，因此证明其用作抗癌剂并用于治疗诸如牛皮癣的疾病。

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