Novel bicyclic compounds
    111.
    发明申请
    Novel bicyclic compounds 失效
    新型双环化合物

    公开(公告)号:US20030191174A1

    公开(公告)日:2003-10-09

    申请号:US10258817

    申请日:2002-10-28

    摘要: Compounds of the general formula (I): 1 or a salt thereof, wherein R1 is hydrogen, hydroxyl or halogen; R2 is NHSO2CH3, SO2NHCH3 or the like; R5 and R6 each independently is hydrogen, C1-6 alkyl, optionally substituted phenyl or optionally substituted benzyl; X is NH, sulfur, oxygen or methylene; Y is oxygen, NR7, sulfur, methylene or a bond; and * represents an asymmetric carbon atom. The compounds are useful as a medicine for treating or preventing diabetes, obesity, hyperlipidemia, digestive diseases, depression or urinary disturbances.

    摘要翻译: 通式(I)的化合物或其盐,其中R 1是氢,羟基或卤素; R 2是NHSO 2 CH 3,SO 2 NHCH 3等; R 5和R 6各自独立地是氢,C 1-6烷基,任选取代的苯基或任选取代的苄基; X是NH,硫,氧或亚甲基; Y是氧,NR 7,硫,亚甲基或键; 和*表示不对称碳原子。 该化合物可用作治疗或预防糖尿病,肥胖症,高脂血症,消化系统疾病,抑郁症或尿失调的药物。

    Formulations comprising selective androgen receptor modulators
    112.
    发明申请
    Formulations comprising selective androgen receptor modulators 有权
    包含选择性雄激素受体调节剂的制剂

    公开(公告)号:US20030162761A1

    公开(公告)日:2003-08-28

    申请号:US10270232

    申请日:2002-10-15

    摘要: The present invention relates to pharmaceutical compositions and formulations comprising a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. The agents define a new subclass of compounds which are selective androgen receptor modulators (SARM) which are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia,osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of chronic muscular wasting; and/or e) decreasing the incidence of, halting or causing a regression of prostate cancer. The present invention provides pharmaceutical compositions comprising the selective androgen receptor modulator compounds, together with pharmaceutically acceptable excipients.

    摘要翻译: 本发明涉及包含新型雄激素受体靶向剂(ARTA)的药物组合物和制剂,其表现出雄激素受体的非甾体配体的雄激素和合成代谢活性。 这些药剂定义了一种新的选择性雄激素受体调节剂(SARM)的化合物亚类,它们可用于a)男性避孕; b)治疗各种激素相关病症,例如与老年雄性雄激素降低有关的病症(ADAM),如疲劳,抑郁,性欲降低,性功能障碍,勃起功能障碍,性腺机能减退,骨质疏松症,脱发,贫血, 肥胖,肌营养不良,骨质减少,骨质疏松症,良性前列腺增生,情绪和认知和前列腺癌的改变; c)治疗与男性雄激素降低相关的病症(ADIF),如性功能障碍,性欲降低,性腺机能减退,肌营养不良,骨质减少,骨质疏松症,认知和情绪改变,抑郁症,贫血,脱发,肥胖,子宫内膜异位症,乳腺癌 癌症,子宫癌和卵巢癌; d)治疗和/或预防慢性肌肉消瘦; 和/或e)降低前列腺癌的发生率,停止或导致消退。 本发明提供了包含选择性雄激素受体调节剂化合物以及药学上可接受的赋形剂的药物组合物。

    Method for cancer therapy
    114.
    发明申请
    Method for cancer therapy 审中-公开
    癌症治疗方法

    公开(公告)号:US20030139373A1

    公开(公告)日:2003-07-24

    申请号:US10290652

    申请日:2002-11-08

    IPC分类号: A61K031/7072 A61K031/404

    摘要: Disclosed are compositions and a method of treating a patient suffering from cancer. The method comprises administering to a patient over a period of up to about 15 days a first component and a second component. The first component consists of a pharmaceutical composition containing as an active ingredient a compound of formula I or a pharmaceutically acceptable salt or ester of said compound. The second component consists of an injection solution containing as an active ingredient gemcitabine. The amount of each component in the combination is such that the combination is therapeutically effective. The components are administered concomitantly or sequentially in a three week to four week treatment cycle for as long as the tumor remains under control and the patient tolerates the regimen. The compositions comprise an antineoplastic combination of a compound for formula I and gemcitabine.

    摘要翻译: 公开了治疗患有癌症的患者的组合物和方法。 该方法包括向患者施用最多约15天的第一组分和第二组分。 第一组分由含有作为活性成分的式I化合物或所述化合物的药学上可接受的盐或酯的药物组合物组成。 第二组分由含有吉西他滨活性成分的注射液组成。 组合中每种组分的量使得组合是治疗有效的。 只要肿瘤保持控制并且患者耐受该方案,组分在三周至四周的治疗周期中同时或依次施用。 组合物包含式I化合物和吉西他滨的抗肿瘤组合。

    Antidiabetic 4-hydroxy-2-furoic acids

    公开(公告)号:US20030134890A1

    公开(公告)日:2003-07-17

    申请号:US10274461

    申请日:2002-10-18

    IPC分类号: A61K031/404 C07D45/14

    CPC分类号: C07D405/14 C12P17/16

    摘要: Substituted 4-hydroxy-2-furoic acids are obtained by the fermentation of an asterriquinone, which is a natural product having a 2,5-dioxy-3,6-bis(indolyl)quinone structure. The compounds modulate insulin receptor tyrosine kinase activity and may be useful in the treatment of diabetes and other diseases or conditions characterized by impaired endogenous insulin production or an impaired response to endogenous insulin.

    Natural food supplement
    116.
    发明申请
    Natural food supplement 审中-公开
    天然食品补充

    公开(公告)号:US20030133945A1

    公开(公告)日:2003-07-17

    申请号:US10045824

    申请日:2002-01-11

    摘要: The present invention is a food supplement for a human body's natural immune function, formed from natural occurring substances in the form of a broth. The food supplement consists of the following: (a) 1 to 35 mg. per mnilliliternullApigenin (b) 200 to 600 mg.nullChrysin (c) 200 to 600 mg.nullColorius Versicolor (d) 50 to 150 mg.null3,3null Diindolymethane (DIM) (e) 50 to 150 mg.nullResveratrol 25% (f) 50 to 150 mg.nullTurmeric Extract 95% (g) 40 to 140 mg.nullGreen Tea Extract 95% (h) 20 to 80 mg.nullQuercitin Dihydrate 99% (i) 15 to 75 mg.nullPhosphtidyl Choline 50% (j) Trace mineral selenium-Lnull10 to 60 mgs. L-Selenium Methionine (5000 mcg/gr) It may be advantageous to also include 25 mg to about 150 mg. of Myricetin.

    摘要翻译: 本发明是由肉汤形式的天然发生物质形成的人体天然免疫功能的食品补充剂。 食物补充剂包括以下物质:(a)1至35mg。 (b)200至600mg.- Chrysin(c)200至600mg- Colorius Versicolor(d)50至150mg.-3,3'二聚甲烷(DIM)(e)50至150mg。 - 白藜芦醇25%(f)50至150mg-姜黄提取物95%(g)40至140mg-绿茶提取物95%(h)20至80mg-槲皮素二水合物99%(i)15至75 mg.-磷脂酰胆碱50%(j)痕量矿物硒-L-10至60mg。 L-硒甲硫氨酸(5000mcg / gr)也可以包括25mg至约150mg。 的杨梅素。

    Diindolylmethane for the treatment of HPV infection
    119.
    发明申请
    Diindolylmethane for the treatment of HPV infection 有权
    二吲哚甲烷用于治疗HPV感染

    公开(公告)号:US20030096855A1

    公开(公告)日:2003-05-22

    申请号:US10117288

    申请日:2002-04-05

    发明人: Michael A. Zeligs

    IPC分类号: A61K031/56 A61K031/404

    摘要: New methods and compositions are disclosed that comprise the phytochemical Diindolylmethane, alone or in combination with immune potentiating steroids. These methods and compositions are utilized to treat subjects suffering from common cutaneous warts (verrucae) and Human Papilloma Virus (HPV) related conditions of the oropharynx, larynx, genitalia, and uterine cervix.

    摘要翻译: 公开了新的方法和组合物,其包含单独的或与免疫增强类固醇组合的植物化学二吲哚基甲烷。 这些方法和组合物用于治疗患有口咽,喉,生殖器和子宫颈的普通皮肤疣(疣)和人乳头状瘤病毒(HPV)相关病症的受试者。