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    ENRICHED PLANT EXTRACT, COMPOUND, AND METHODS FOR THE TREATMENT OF PROLIFERATIVE DISORDERS
    2.
    发明申请
    ENRICHED PLANT EXTRACT, COMPOUND, AND METHODS FOR THE TREATMENT OF PROLIFERATIVE DISORDERS 审中-公开
    增强植物提取物，化合物和治疗增殖性疾病的方法

    公开(公告)号：WO2008090517A3

    公开(公告)日：2009-12-30

    申请号：PCT/IB2008050227

    申请日：2008-01-23

    Applicant: PIRAMAL LIFE SCIENCES LTD ,  PERIYASAMY GIRIDHARAN ,  SUTHAR ASHISH ,  BALAKRISHNAN ARUN ,  VISHWAKARMA RAM ,  MANOHAR VENKAT ,  PARI KOTEPPA ,  CHAUHAN VIJAY SINGH ,  KULANTHAIVELU PATHMANATHAN

    Inventor： PERIYASAMY GIRIDHARAN ,  SUTHAR ASHISH ,  BALAKRISHNAN ARUN ,  VISHWAKARMA RAM ,  MANOHAR VENKAT ,  PARI KOTEPPA ,  CHAUHAN VIJAY SINGH ,  KULANTHAIVELU PATHMANATHAN

    IPC: A61K31/56 ,  C07D215/00

    CPC classification number: C07J1/00

    Abstract: The present invention relates to an enriched plant extract containing a mixture of two compounds, obtained from the leaves of the plant Vitex negundo, used for the treatment of proliferative disorders such as cancer. The invention also relates to a compound of formula (1) : The compound of formula (1) can be isolated from the enriched extract and has antiproliferative activity. The present invention further relates to a herbal composition including enriched extract of leaves of Vitex negundo containing the mixture of two compounds as main ingredient for the treatment of proliferative disorders such as cancer. The invention also relates to a pharmaceutical composition including the compound of formula (1), for the treatment of proliferative disorders such as cancer. The invention further relates to the method of treatment of proliferative disorders such as cancer, by adapting the compositions in mammals, in need thereof.

    Abstract translation: 本发明涉及富含植物提取物，其含有从植物Vitex negundo的叶子获得的两种化合物的混合物，其用于治疗增殖性疾病如癌症。 本发明还涉及式（1）化合物：式（1）化合物可以从富集的提取物中分离并具有抗增殖活性。 本发明还涉及包含Vitex negundo的叶的富集提取物的草药组合物，其含有两种化合物的混合物作为用于治疗增殖性疾病如癌症的主要成分。 本发明还涉及包含用于治疗增殖性疾病如癌症的式（1）化合物的药物组合物。 本发明还涉及通过使需要的哺乳动物中的组合物适应而治疗增殖性疾病例如癌症的方法。

    ESTROGEN RECEPTOR MODULATORS
    4.
    发明申请
    ESTROGEN RECEPTOR MODULATORS 审中-公开
    雌激素受体调节剂

    公开(公告)号：WO2006081152A2

    公开(公告)日：2006-08-03

    申请号：PCT/US2006/002148

    申请日：2006-01-20

    Applicant: MERCK & CO., INC. ,  BLIZZARD, Timothy, A. ,  GUDE, Candido

    Inventor： BLIZZARD, Timothy, A. ,  GUDE, Candido

    IPC: A61K31/56

    CPC classification number: C07J1/00

    Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, metastatic bone disease, Paget’s disease, periodontal disease, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, inflammation, inflammatory bowel disease and cancer, in particular of the breast, uterus and prostate.

    Abstract translation: 本发明涉及其化合物及其衍生物，其合成及其作为雌激素受体调节剂的用途。 本发明的化合物是雌激素受体的配体，因此可用于治疗或预防与雌激素功能相关的各种病症，包括：骨丢失，骨折，骨质疏松症，转移性骨病，佩吉特氏病，牙周病， 软骨变性，子宫内膜异位症，子宫肌瘤疾病，潮热，LDL胆固醇水平升高，心血管疾病，认知功能障碍，脑退行性疾病，再狭窄，男子母性发育，血管平滑肌细胞增殖，肥胖，失禁，炎症，炎性肠病和 癌症，特别是乳腺癌，子宫癌和前列腺癌。

    ANTIANDROGENS WITH MARGINAL AGONIST ACTIVITY AND METHODS OF USE
    5.
    发明申请
    ANTIANDROGENS WITH MARGINAL AGONIST ACTIVITY AND METHODS OF USE 审中-公开
    具有肌肉激素活性的抗体和使用方法

    公开(公告)号：WO2004089304A3

    公开(公告)日：2005-05-06

    申请号：PCT/US2004009739

    申请日：2004-03-30

    Applicant: HOLLIS EDEN PHARMACEUTICALS ,  LARDY HENRY A ,  MARWAH ASHOK K ,  MARWAH PADMA

    Inventor： LARDY HENRY A ,  MARWAH ASHOK K ,  MARWAH PADMA

    IPC: A61K20060101 ,  A61K31/4745 ,  A61K31/58 ,  C07D471/02 ,  C07J1/00 ,  C07J21/00

    CPC classification number: C07J1/00 ,  C07J1/0011 ,  C07J21/00 ,  C07J21/008

    Abstract: The instant invention provides potent antiandrogen compounds, such as 3beta -acetoxyandrost-1,5-diene-17-ethylene ketal and 3beta-hydroxyandrost-1, 5-diene-17ethylene ketal, and methods for their use in the prevention and treatment of biological conditions mediated by androgen receptors. Thus, for example, compounds of the invention are useful in the prevention and treatment of prostrate cancer. Furthermore, it has been discovered that compounds of the invention are useful in the prevention and treatment of androgen-independent cancers such as androgen-independent prostrate cancer. Finally, inventive compounds may be used to treat antiandrogen induced withdrawal syndrome.

    Abstract translation: 本发明提供了有效的抗雄激素化合物，例如3β-乙酰氧基雄甾-1,5-二烯-17-亚乙基缩酮和3,3-羟基雄甾-1,5-二烯-17-乙二醇缩酮，以及用于预防和治疗生物 由雄激素受体介导的情况。 因此，例如，本发明的化合物可用于预防和治疗前列腺癌。 此外，已经发现本发明的化合物可用于预防和治疗雄激素依赖性癌症如雄激素依赖性前列腺癌。 最后，本发明化合物可用于治疗抗雄激素诱导的戒断综合征。

    15alpha-SUBSTITUTED ESTRADIOL CARBOXYLIC ACID ESTERS AS LOCALLY ACTIVE ESTROGENS
    9.
    发明申请
    15alpha-SUBSTITUTED ESTRADIOL CARBOXYLIC ACID ESTERS AS LOCALLY ACTIVE ESTROGENS 审中-公开
    15α-取代的ESTRADIOL羧酸酯作为局部活性雌激素

    公开(公告)号：WO2004085345A2

    公开(公告)日：2004-10-07

    申请号：PCT/US2004007092

    申请日：2004-03-09

    Applicant: UNIV YALE ,  HOCHBERG RICHARD

    Inventor： HOCHBERG RICHARD

    IPC: A61K31/56 ,  C07C20060101 ,  C07J1/00 ,  C07C

    CPC classification number: C07J1/00

    Abstract: The present invention relates to analogs of estradiol, which, in their most preferred embodiment, act as locally active estrogens without significant systemic action. A series of 15alpha-estradiol ester compounds is presented which exhibit excellent biological activity for use in pharmaceutical compositions for the treatment of symptomology associated with menopause. The present invention is therefore directed to compounds according to the structure: where X is , R is H, a C1 to C5 alkyl group, optionally substituted with at least one halogen group, such as CH2CH2F, or other group (e.g., CH2CHF2, CH2CF3 or CF3 group); and m is from 0-5, preferably from 0-2.

    Abstract translation: 本发明涉及雌二醇的类似物，其在其最优选的实施方案中用作局部活性雌激素而没有显着的全身作用。 提出了一系列15α-雌二醇酯化合物，其表现出优异的生物活性用于药物组合物用于治疗与更年期相关的症状。 因此，本发明涉及以下结构的化合物：其中X为<（CH 2）m>，R为H，任选被至少一个卤素基团取代的C 1至C 5烷基，例如CH 2 CH 2 F或其它基团 （例如，CH 2 CHF 2，CH 2 CF 3或CF 3基团）; m为0-5，优选为0-2。

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