SYNTHESIS OF (-)-BETA-ELEMENE, (-)-BETA-ELEMENAL, (-)-BETA-ELEMENOL, (-)-BETA-ELEMENE FLUORIDE AND THEIR ANALOGUES, INTERMEDIATES AND COMPOSITION AND USES THEREOF
    3.
    发明申请
    SYNTHESIS OF (-)-BETA-ELEMENE, (-)-BETA-ELEMENAL, (-)-BETA-ELEMENOL, (-)-BETA-ELEMENE FLUORIDE AND THEIR ANALOGUES, INTERMEDIATES AND COMPOSITION AND USES THEREOF 审中-公开
    ( - ) - BETA-ELEMENE,( - ) - BETA-ELEMENOL,( - ) - BETA-ELEMENE氟化物及其类似物,中间体和组合物的合成及其用途

    公开(公告)号:WO2006016912A2

    公开(公告)日:2006-02-16

    申请号:PCT/US2005/014699

    申请日:2005-05-02

    Inventor: HUANG, Lan

    Abstract: The present invention provides convergent processes for preparing (-)-beta-elemene, (-)-beta-elemenal, (-)-beta-elemenol, and (-)-beta-elemene fluoride and analogues thereof. Also provided are intermediates useful for preparing (-)-beta-elemene. The present invention further provides novel compositions based on analogues of (-)-beta-elemene, (-)-beta-elemenal, (-)-beta-elemenol, (-)-beta-elemene fluoride and methods for the treatment of cancer, such as brain tumor, lung cancer, breast cancer, prostate cancer, ovarian cancer, colorectal cancer, gastric intestional cancer, and stomach cancer. The inventors propose a combination therapy using 1) one or more of the following anti-cancer agents: including, but not limited to, Cisplatin, 5-FU, Taxol, Taxol derivatives, and any anti-cancer agent, and 2) one or more of the following (-)-beta-elemene and its analogs, including (-)-beta-elemene, (-)-beta-elemenol, (-)-beta-elemenol, (-)-beta-elemene fluoride, and their analogs, and (-)-beta-elemene's intermediate in its chemical synthesis, for the treatment of cancer, especially for the treatment of brain tumor, lung cancer, ovarian cancer, bladder cancer, cervical cancer,. colon cancer, breast cancer, and prostate cancer.

    Abstract translation: 本发明提供( - ) - β-榄香烯,( - ) - β-元素,( - ) - β-榄香烯和( - ) - β-榄香烯氟化物及其类似物的收敛方法。 还提供了可用于制备( - ) - β-榄香烯的中间体。 本发明还提供了基于( - ) - β-榄香烯,( - ) - β-元素,( - ) - β-榄香烯,( - ) - β-榄香烯氟化物类似物和治疗癌症的新方法 ,例如脑肿瘤,肺癌,乳腺癌,前列腺癌,卵巢癌,结肠直肠癌,胃肠癌和胃癌。 本发明人提出了使用以下1种或多种抗癌药物的组合疗法:包括但不限于顺铂,5-FU,紫杉醇,紫杉醇衍生物和任何抗癌剂,以及2)一种或多种 ( - ) - β-榄香烯,( - ) - β-榄香烯,( - ) - β-榄香烯,( - ) - β-榄香烯氟化物和 他们的类似物和( - ) - β-榄香烯在其化学合成中的中间体,用于治疗癌症,特别是用于治疗脑肿瘤,肺癌,卵巢癌,膀胱癌,子宫颈癌。 结肠癌,乳腺癌和前列腺癌。

    DERIVATIVES OF PHENANTRENE FOR MEDICINAL USE AND A PROCESS FOR THEIR PREPARATION
    5.
    发明申请
    DERIVATIVES OF PHENANTRENE FOR MEDICINAL USE AND A PROCESS FOR THEIR PREPARATION 审中-公开
    苯丙胺用于药物使用的衍生物及其制备方法

    公开(公告)号:WO00017143A1

    公开(公告)日:2000-03-30

    申请号:PCT/IT1999/000299

    申请日:1999-09-23

    Abstract: New active compounds are provided for the preparation of pharmaceutical compositions for medicinal use in general, and for use in dermatology, oncology, and the treatment of kidney, liver and nervous system disorders, and in which is present the group of formula (I) having three six-carbon condensed homocyclic rings including an aromatic central ring and two saturated or unsaturated aliphatic side rings in the meta position with respect to the aromatic central ring, and wherein the lateral substitutes R1 and R2 are alkyl groups with a carbon number of 1 to 4; both the aliphatic side rings also possibly having one or more further lateral substitutes.

    Abstract translation: 提供新的活性化合物用于制备用于药物用途的药物组合物,并用于皮肤病学,肿瘤学和肾脏,肝脏和神经系统疾病的治疗,其中存在式(I)的基团,其具有 三个六碳稠合的环状环,包括相对于芳族中心环的间位的芳族中心环和两个饱和或不饱和脂族侧环,并且其中侧面取代基R1和R2是碳数为1至 4; 脂肪族侧环也可能具有一个或多个另外的侧面替代物。

    A NOVEL METHOD FOR SYNTHESIZING TBE-31
    7.
    发明申请
    A NOVEL METHOD FOR SYNTHESIZING TBE-31 审中-公开
    一种合成TBE-31的新方法

    公开(公告)号:WO2014151181A1

    公开(公告)日:2014-09-25

    申请号:PCT/US2014/025172

    申请日:2014-03-13

    Abstract: A process for the synthesis of (±)-(4bS,8aR,10aS)-10a-ethynyl-4b,8,8-trimethyl-3,7-dioxo-3,4b,7,8,8a,9,10,10a-octahydrophenanthrene-2,6-dicarbonitrile ("TBE-31"), which is useful for the treatment of various diseases and disorder in mammals. (±)-8a-(Hydroxymethyl)-1,4a-dimethyl-2,3,4,4a,6,7,8,8a,9,10-decahydrophenanthren-2-ol; (±)-8a-(Hydroxymethyl)-1,4a-dimethyl-4,4a,6,7,8,8a,9,10-octahydrophenanthren-2(3H)-one; (±)-(2R,4aS,8aS)-8a-(Hydroxymethyl)-1,4a-dimethyl-2,3,4,4a,6,7,8,8a,9,10-decahydrophenanthren-2-ol; (±)-(2S,4aS,8aS)-8a-(Hydroxymethyl)-1,4a-dimethyl-2,3,4,4a,6,7,8,8a,9,10-decahydrophenanthren-2-ol; and (±)-(4aS,8aS)-8a-(Hydroxymethyl)-1,4a-dimethyl-4,4a,6,7,8,8a,9,10-octahydrophenanthren-2(3H)-one (4).

    Abstract translation: 合成(±) - (4bS,8aR,10aS)-10a-乙炔基-4,4,8,8-三甲基-3,7-二氧代-3,4b,7,8,8a,9,10, 10a-八氢菲-2,6-二腈(“TBE-31”),其可用于治疗哺乳动物的各种疾病和病症。 (±)-8a-(羟基甲基)-1,4a二甲基甲基-2,3,4,4a,6,7,8,8a,9,10- decahydrophenanthren -2-醇; (±)-8a-(羟基甲基)-1,4a二甲基甲基-4,4a,6,7,8,8a,9,10- octahydrophenanthren -2(3H) - 酮; (±) - (2R,4AS,8AS)-8a-(羟基甲基)-1,4a二甲基甲基-2,3,4,4a,6,7,8,8a,9,10- decahydrophenanthren -2-醇; (±) - (2S,4AS,8AS)-8a-(羟基甲基)-1,4a二甲基甲基-2,3,4,4a,6,7,8,8a,9,10- decahydrophenanthren -2-醇; 和(±) - (4aS,8aS)-8a-(羟甲基)-1,4a-二甲基-4,4a,6,7,8,8a,9,10-八氢菲-2(3H) - 酮(4) 。

    PI MARANE DITERPENES FROM ANISOCHILUS VERTICILLATUS
    8.
    发明申请
    PI MARANE DITERPENES FROM ANISOCHILUS VERTICILLATUS 审中-公开
    来自ANISOCHILUS VERTICILLATUS的PI MARANE DITERPENES

    公开(公告)号:WO2013021399A1

    公开(公告)日:2013-02-14

    申请号:PCT/IN2012/000544

    申请日:2012-08-06

    Abstract: This invention discloses diterpenes class of novel compounds of general formula I from a novel source. More particularly the invention relates to extracts /fractions containing pimarane diterpenes from Anisochillus (Lamiaceae), useful for prevention, treatment, inhibition or controlling growth and proliferation of mycobacterial activity in mammals. The invention further relates to extracts, fractions standardized to diterpenes class of novel compounds useful for the treatment of cancers.

    Abstract translation: 本发明公开了一种新型来源的通式I的新型化合物二萜类。 更具体地,本发明涉及含有来自Anisochillus(Lamiaceae)的异丙苯二萜的提取物/级分,其可用于预防,治疗,抑制或控制哺乳动物中分枝杆菌活性的生长和增殖。 本发明还涉及标准化为二萜类的提取物,用于治疗癌症的新化合物的级分。

    BINUCLEAR NON-HEME IRON CATALYSTS
    9.
    发明申请
    BINUCLEAR NON-HEME IRON CATALYSTS 审中-公开
    不锈钢非铁镍催化剂

    公开(公告)号:WO99010357A1

    公开(公告)日:1999-03-04

    申请号:PCT/US1998/017610

    申请日:1998-08-21

    Abstract: The subject invention provides a binuclear metal complex having structure (I) wherein M1, and M2 are independently selected from the group consisting of Fe, Co, Mn and Ru; wherein m and n are independently +2 or +3; wherein R1, R2, R3, R4, R5 and R6 are independently a linear C1-C6 alkyl, C5-C6 cycloalkyl, phenyl, etc.; wherein (i) R1 and R2, (ii) R3 and R4, or (iii) R5 and R6 independently and optionally are linked covalently and together with the respective adjoining C atom comprise a spirocyclic ring; wherein i, j and k are integers such that 2

    Abstract translation: 本发明提供具有结构(I)的双核金属络​​合物,其中M1和M2独立地选自Fe,Co,Mn和Ru; 其中m和n独立地是+2或+3; 其中R1,R2,R3,R4,R5和R6独立地为直链C1-C6烷基,C5-C6环烷基,苯基等; 其中(i)R 1和R 2,(ⅱ)R 3和R 4,或(ⅲ)R 5和R 6独立地且任选被共价连接并与相邻的C原子一起包含一个螺环; 其中i,j和k是整数,使得2 i + j + k 4; 其中p为1或2,q为0,1或2,使得m + n-4 = p×q; 其中(i)R 1或R 2和R 3或R 4,(ⅱ)R 3或R 4和R 4或R 5,或(ⅲ)R 1或R 2和R 5或R 6独立且任选地与相邻的C原子共价连接并连接 稠环; 其中Ar为1,2-亚苯基,1,2-或2,3-亚萘基等,其中所述Ar任选被C 1 -C 6烷基或烷氧基取代; 其中L是N-甲基咪唑,N-乙基咪唑等; 并且其中X是氟,氯,溴等。还提供了使用双核金属络​​合物作为催化剂的烷烃,芳烃和硫化物的氧化方法和制备所述络合物的方法。

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