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    • 5. 发明申请
    • N-BRIDGED SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF
    • N-桥选择性受体调节剂及其使用方法
    • WO2003106401A1
    • 2003-12-24
    • PCT/US2003/016219
    • 2003-06-17
    • UNIVERSITY OF TENNESSEE RESEARCH FOUNDATIONDALTON, JamesMILLER, Duane, D.MARHEFKA, Craig, A.GAO, Wenqing
    • DALTON, JamesMILLER, Duane, D.MARHEFKA, Craig, A.GAO, Wenqing
    • C07C233/05
    • C07D211/72A61K31/415A61K31/44A61K31/505A61K31/65C07C237/10C07C255/60C07D233/44C07D239/02
    • This invention provides a class of androgen receptor targeting agents (ARTA) The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor. The SARM compounds, either alone or as a composition, 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 acute and/or chronic muscular wasting conditions; e) preventing and/or treating dry eye conditions; f) oral androgen replacement therapy, and/or g) decreasing the incidence of, halting or causing a regression of prostate cancer.
    • 本发明提供了一类雄激素受体靶向剂(ARTA)。该药物定义了一种新的化合物亚类,它们是选择性雄激素受体调节剂(SARM)。 已经发现几种SARM化合物对雄激素受体具有非甾类化合物的意想不到的雄激素和合成代谢活性。 已经发现其他SARM化合物对雄激素受体具有非甾类配体的意想不到的抗雄激素活性。 SARM化合物,单独或作为组合物,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)治疗与雄激素降解有关的疾病(ADIF),如性功能障碍,性欲降低,性腺机能减退,肌肉减少症,骨质减少症,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 ,子宫癌和卵巢癌; d)治疗和/或预防急性和/或慢性肌肉消瘦病症; e)预防和/或治疗干眼症状; f)口服雄激素替代疗法,和/或g)降低前列腺癌的发作,停止或导致消退。
    • 9. 发明申请
    • NON-METAL TANNING PROCESS
    • 非金属鞣制工艺
    • WO2012055483A1
    • 2012-05-03
    • PCT/EP2011/004975
    • 2011-10-05
    • CLARIANT INTERNATIONAL LTDREINEKING, ClausGAMARINO, RobertaTRIMARCO, LiciaQUAGLIERINI, MaurizioGISLER, MarkusNUSSER, Rainer
    • REINEKING, ClausGAMARINO, RobertaTRIMARCO, LiciaQUAGLIERINI, MaurizioGISLER, MarkusNUSSER, Rainer
    • C14C3/26
    • C14C3/00C07D237/00C07D237/06C07D239/02C07D247/02C14C3/02C14C3/04C14C3/26
    • Tanned leather, skin or pelt is produced by non-metal tanning, comprising the step of tanning a bated hide, skin or pelt with a tanning agent (A), the tanning agent (A) being at least a mixture of compounds of formula (I) and formula (II), wherein Hal signifies fluorine or chlorine, R1 signifies hydrogen, C 1-8 -alkyl or an alkyleneoxy radical of formula (III), - (- C 2-3 alkylene - O -) q - H (III) R2 signifies a) phenyl, mono- or di-substituted with SO 3 M or COOM and optionally substituted also with hydroxyl or C 1-4 -alkyl or C 1-4 alkoxy, or b) naphthyl, mono- or di- or tri-substituted with SO 3 M and optionally substituted also with hydroxyl, or c) C 1-8 -alkylene, substituted with (S0 3 M) or (COOM), or d) a radical of formula (IV), - (- C 2-3 alkylene - O -) p - Y (IV) e) or a radical of formula (IVa), -(C 2-3 alkylene - O) p -C 2-3 alkylene - SO 2 CH 2 CH2O -Y (IVa) m signifies 1 or 2, P signifies 0 or 1, Y signifies hydrogen or -SO 3 M, q is of from 1 to 10, M signifies hydrogen or an alkali metal cation or an ammonium cation, the ammonium cation being a protonated tertiary amine or a quaternary ammonium cation, R3 signifies hydrogen or chlorine, in a tanning bath, the tanning bath having a pH of from 6 to 10 at the beginning of tanning step.
    • 鞣制的皮革,皮肤或毛皮是通过非金属鞣制制成的,包括用鞣剂(A)鞣制皮肤,皮肤或皮肤的步骤,鞣制剂(A)至少是式 I)和式(II),其中Hal表示氟或氯,R1表示氢,C1-8 - 烷基或式(III)的亚烷基氧基, - ( - C2-3亚烷基-O - )q-H(III )R2表示a)苯基,被SO 3 M或COOM单取代或二取代,并任选也被羟基或C 1-4 - 烷基或C 1-4烷氧基取代,或b)萘基,被SO 3 M单取代或二取代或三取代 或任选地被羟基取代,或c)被(S03M)或(COOM)取代的C 1-8 - 亚烷基,或d)式(Ⅳ)基团, - ( - C 2-3亚烷基-O - ) - Y(IV)e)或式(Ⅳa)基团, - (C2-3亚烷基-O)p -C2-3亚烷基-SO2CH2CH2O -Y(Ⅳa)m表示1或2,P表示0或1,Y 表示氢或-SO 3 M,q为1至10,M表示氢或碱金属 铵阳离子是质子化叔胺或季铵阳离子,R3表示氢或氯,在鞣制浴中,鞣制浴在鞣制步骤开始时pH为6至10。