Synthesis of selective androgen receptor modulators
    3.
    发明申请
    Synthesis of selective androgen receptor modulators 有权
    选择性雄激素受体调节剂的合成

    公开(公告)号:US20040014975A1

    公开(公告)日:2004-01-22

    申请号:US10277108

    申请日:2002-10-22

    摘要: The present invention relates to a synthetic process for the preparation of 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; e) decreasing the incidence of, halting or causing a regression of prostate cancer; f) oral androgen relacement and/or other clinical therpauetic and/or diagnostic areas. The process of the present invention is suitable for large-scale preparation, since all of the steps give rise to highly pure compounds, thus avoiding complicated purification procedures which ultimately lower the yield. Thus the present invention provides methods for the synthesis of non-steroidal agonist compounds, that can be used for industrial large-scale synthesis, and that provide highly pure products in high yield.

    摘要翻译: 本发明涉及一种用于制备新型雄激素受体靶向剂(ARTA)的合成方法,其表现出雄激素受体的非甾族化合物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; e)降低前列腺癌的发生率,停止或导致消退; f)口服雄激素替代和/或其他临床治疗和/或诊断领域。 本发明的方法适用于大规模制备,因为所有步骤都产生高纯度的化合物,因此避免了复杂的纯化方法,从而降低产率。 因此,本发明提供了可用于工业大规模合成的非甾体激动剂化合物的合成方法,并以高产率提供高纯度产品。

    Method for producing polyisocyanates
    4.
    发明申请
    Method for producing polyisocyanates 有权
    聚异氰酸酯的制造方法

    公开(公告)号:US20030078450A1

    公开(公告)日:2003-04-24

    申请号:US10144612

    申请日:2002-05-13

    IPC分类号: C07C271/26 C07C265/00

    摘要: The invention relates to a method for making oligomeric isocyanates by reacting diisocyanates in the presence of a catalyst, wherein the catalyst comprises a saline compound prepared from a five-membered N-heterocycles and the N-heterocycle comprises at least one N-H function in the five-membered ring, to the products produced in this way and to polymers prepared from these products.

    摘要翻译: 本发明涉及一种通过在催化剂存在下使二异氰酸酯反应制备低聚异氰酸酯的方法,其中催化剂包含由五元N-杂环制备的盐水化合物,N-杂环包括五元醇中的至少一个NH官能团 以这种方式生产的产品和由这些产品制备的聚合物。

    Viscosity conditioner
    5.
    发明授权
    Viscosity conditioner 失效
    粘度调节剂

    公开(公告)号:US5977398A

    公开(公告)日:1999-11-02

    申请号:US701768

    申请日:1996-08-26

    申请人: Kaoru Komiya

    发明人: Kaoru Komiya

    摘要: A viscosity conditioner is disclosed which is comprised of a compound represented by the following formula ##STR1## where R.sup.1 to R.sup.3 each are hydrocarbyl groups which may be identical or different, m ranges from 2 to 4, and n ranges from 1 to 1,000. The specified viscosity conditioner is by nature non-ionic and excellent in leveling.

    摘要翻译: 公开了一种粘度调节剂,其由下式表示的化合物组成,其中R 1至R 3各自为可相同或不同的烃基,m为2至4,n为1至1,000。 特定的粘度调节剂本质上是非离子的,并且在流平方面是优异的。

    Isocyanate prepolymers produced from toluene diisocyanate residue
dissolved in toluene diisocyanate
    9.
    发明授权
    Isocyanate prepolymers produced from toluene diisocyanate residue dissolved in toluene diisocyanate 失效
    由甲苯二异氰酸酯残基溶解在甲苯二异氰酸酯中产生的异氰酸酯预聚物

    公开(公告)号:US5756636A

    公开(公告)日:1998-05-26

    申请号:US774278

    申请日:1996-12-27

    摘要: A substantially solid free isocyanate prepolymer is made by reacting an isocyanate mixture which is made up of a toluene diisocyanate residue containing monomeric toluene diisocyanate and optionally, additional monomeric toluene diisocyanate in an amount such that the total NCO content is at least 37% with a polyether polyol having an ethylene oxide content of at least 30%. The polyether polyol has a molecular weight of from about 200 to about 6,000 and a functionality of from 2 to 6. The product prepolymers are particularly useful in the production of polyurethanes.

    摘要翻译: 通过使由含有单体甲苯二异氰酸酯的甲苯二异氰酸酯残基和任选的另外的单体甲苯二异氰酸酯组成的异氰酸酯混合物与总聚NCO含量至少为37%的量与聚醚反应制备基本上无固体的异氰酸酯预聚物 环氧乙烷含量至少为30%的多元醇。 聚醚多元醇具有约200至约6,000的分子量和2至6的官能度。该产品预聚物特别可用于生产聚氨酯。