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    • 21. 发明申请
    • NOVEL NUCLEAR HORMONE RECEPTOR LIGANDS AND METHODS
    • 新的核激素受体配体和方法
    • WO2004037792A2
    • 2004-05-06
    • PCT/EP2003/010108
    • 2003-09-10
    • KARO BIO ABRUDA, MarcusWENSBO, David
    • RUDA, MarcusWENSBO, David
    • C07D215/00
    • C07D221/10
    • The present invention relates to compounds and derivatives thereof, their synthesis, and their use as nuclear hormone receptor modulators. The compounds of the instant invention are ligands for nuclear hormone receptors and as such may be useful for treatment or prevention of a variety of conditions related to nuclear hormone functioning including proliferative diseases, cancers, benign prostate hyperplasia, adenomas and neoplasisms of the prostate, benign or malignant tumor cells containing the androgen receptor, cardiovascular diseases, angiogenic conditions or disorders, hirsutism, acne, hyperpilosity, inflammation, immune modulation, seborrhea, endometriosis, polycycstic ovary syndrome, androgen alopecia, hypogonadism, osteoporosis, suppressing spermatogenesis, libido, cachexia, anorexia, cancers expressing the estrogen receptor, prostate cancer, breast cancer, endometrial cancer, incontinence, hot flashes, vaginal dryness, menopause, contraception, pregnancy termination, cancers containing the progesterone receptor, endometriosis, cachexia, menopause fibrosis, labor induction, autoimmune diseases, impairment of cognitive functioning, cerebral degenerative disorders, Alzheimer's disease, psychotic disorders, type-II diabetes, congestive heart failure, disregulation of cholesterol or lipid homeostasis, and/or obesity.
    • 本发明涉及其化合物及其衍生物,其合成及其作为核激素受体调节剂的用途。 本发明的化合物是核激素受体的配体,因此可用于治疗或预防与核激素功能相关的各种病症,包括增殖性疾病,癌症,良性前列腺增生,前列腺腺瘤和肿瘤,良性 或含有雄激素受体的恶性肿瘤细胞,心血管疾病,血管生成病症或病症,多毛症,痤疮,高通气,炎症,免疫调节,脂溢性皮脂血症,子宫内膜异位症,多环性卵巢综合征,雄激素性脱发,性腺机能减退,骨质疏松症,抑制精子发生,性欲,恶病质, 厌食症,表达雌激素受体的癌症,前列腺癌,乳腺癌,子宫内膜癌,失禁,潮热,阴道干燥,更年期,避孕,妊娠终止,含有孕酮受体的癌症,子宫内膜异位症,恶病质,绝经纤维化,劳动诱导,自身免疫性疾病 ,认知障碍 老年痴呆症,精神障碍,II型糖尿病,充血性心力衰竭,胆固醇或脂质体内平衡失调和/或肥胖。