N⁴-ethyl-6-methoxy-pyrimidine-2,4-diyldiamine | 856974-74-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: N⁴-ethyl-6-methoxy-pyrimidine-2,4-diyldiamine
• 英文别名: N⁴-Aethyl-6-methoxy-pyrimidin-2,4-diyldiamin；4-N-ethyl-6-methoxypyrimidine-2,4-diamine
• CAS: 856974-74-8
• 化学式: C₇H₁₂N₄O
• 分子量: 168.198
• InChiKey: RYNXYGUULQVSGK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  12
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  73.1
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  N⁴-ethyl-6-methoxy-pyrimidine-2,4-diyldiamine 在 盐酸 、 乙醇 作用下， 生成 2-氨基-6-(乙基氨基)-4(1H)-嘧啶酮
  参考文献：
  名称：

  Effects of Transdermal Testosterone on Cognitive Function and Health Perception in Older Men With Low Bioavailable Testosterone Levels

  摘要：

  Background. Many men older than 50 years have bioavailable testosterone levels below the reference range for young adult men. The impact of the decreased androgen levels oil cognition and health perception has received little attention.Methods. Sixty-seven men (mean age 76 +/- 4 years, range 65-87) with bioavailable testosterone levels below 128 ng/dl (lower limit for adult normal range) were randomized to receive transdermal testosterone (2-2.5 mg patches/d) or placebo patches for I year. All men received 500 mg Supplemental calcium and 400 IU vitamin D. Outcome measures included sex hormones [testosterone, bioavailable testosterone, sex hormone binding globulin (SHBG), estradiol, and estrone], cognitive tests, (Digit Symbol, Digit Span, Trailmaking A and B), health perception (Medical Outcome Survey Short-form 36 or SF-36), lower extremity muscle strength and power. and calcium intake.Results. Twenty-three men (34%) withdrew from the Study; 44 men completed the trial. Bioavailable testosterone levels increased from 93 +/- 34 (SD) to 162 +/- 100 ng/dl (p < .002) at 12 months in the testosterone group (n = 24) while no change occurred in the control group (n 20). While there was no change in estradiol levels in either group, estrone levels increased in the testosterone group (28 +/- 7 to 32 +/- 9 pg/dl, p = .017). Scores oil the Digit Symbol test improved in both the testosterone and placebo groups. Scores on Trailmaking B improved in men treated with testosterone (p < .005), although the changes were not statistically different from the changes seen in the placebo group. Twelve-month scores on Trailmaking B for the entire group were correlated with 12-month testosterone levels (p = .016). Scores for health perception measured by SF-36 did not change significantly, though scores of mental and general health declined in both groups during the 12-month intervention. Twelve-month bioavailable testosterone scores were directly correlated with scores for physical role (p = .022), vitality (p = .036), and the physical composite score (p = .010).Conclusions. Transdermal testosterone treatment in men with low bioavailable testosterone levels does not impair and may improve cognitive function. Treatment did not improve health perception but this may have been due to the side effects of skin irritation suggested by similar reactions in both the testosterone and placebo groups.

  DOI：

  10.1093/gerona/57.5.m321
• 作为产物：
  描述：

  sodium methylate 、 6-chloro-4-N-ethylpyrimidine-2,4-diamine 在 甲醇 作用下， 生成 N⁴-ethyl-6-methoxy-pyrimidine-2,4-diyldiamine
  参考文献：
  名称：

  Effects of Transdermal Testosterone on Cognitive Function and Health Perception in Older Men With Low Bioavailable Testosterone Levels

  摘要：

  Background. Many men older than 50 years have bioavailable testosterone levels below the reference range for young adult men. The impact of the decreased androgen levels oil cognition and health perception has received little attention.Methods. Sixty-seven men (mean age 76 +/- 4 years, range 65-87) with bioavailable testosterone levels below 128 ng/dl (lower limit for adult normal range) were randomized to receive transdermal testosterone (2-2.5 mg patches/d) or placebo patches for I year. All men received 500 mg Supplemental calcium and 400 IU vitamin D. Outcome measures included sex hormones [testosterone, bioavailable testosterone, sex hormone binding globulin (SHBG), estradiol, and estrone], cognitive tests, (Digit Symbol, Digit Span, Trailmaking A and B), health perception (Medical Outcome Survey Short-form 36 or SF-36), lower extremity muscle strength and power. and calcium intake.Results. Twenty-three men (34%) withdrew from the Study; 44 men completed the trial. Bioavailable testosterone levels increased from 93 +/- 34 (SD) to 162 +/- 100 ng/dl (p < .002) at 12 months in the testosterone group (n = 24) while no change occurred in the control group (n 20). While there was no change in estradiol levels in either group, estrone levels increased in the testosterone group (28 +/- 7 to 32 +/- 9 pg/dl, p = .017). Scores oil the Digit Symbol test improved in both the testosterone and placebo groups. Scores on Trailmaking B improved in men treated with testosterone (p < .005), although the changes were not statistically different from the changes seen in the placebo group. Twelve-month scores on Trailmaking B for the entire group were correlated with 12-month testosterone levels (p = .016). Scores for health perception measured by SF-36 did not change significantly, though scores of mental and general health declined in both groups during the 12-month intervention. Twelve-month bioavailable testosterone scores were directly correlated with scores for physical role (p = .022), vitality (p = .036), and the physical composite score (p = .010).Conclusions. Transdermal testosterone treatment in men with low bioavailable testosterone levels does not impair and may improve cognitive function. Treatment did not improve health perception but this may have been due to the side effects of skin irritation suggested by similar reactions in both the testosterone and placebo groups.

  DOI：

  10.1093/gerona/57.5.m321

文献信息

• [EN] RESOLUTION OF OPTICALLY ACTIVE DIAZASPIRO[4.5]DECANE DERIVATIVES<br/>[FR] RÉSOLUTION DE DÉRIVÉS DE DIAZASPIRO [4,5] DÉCANE OPTIQUEMENT ACTIFS
  申请人：ROIVANT SCIENCES GMBH

  公开号：WO2018087602A1

  公开（公告）日：2018-05-17

  The present invention is directed to diazaspiro[4.5]decane intermediates and salts thereof useful for the preparation of spirocyclic compounds which are inhibitors of tryptophan hydroxylase (TPH), particularly isoform 1 (TPH1). Processes of preparing the intermediates and their salts are also provided.

  本发明涉及一种用于制备螺环化合物的二氮杂螺[4.5]癸烷中间体及其盐，该化合物是色氨酸羟化酶（TPH）的抑制剂，特别是TPH1。本发明还提供了制备中间体及其盐的方法。
• Effects of Transdermal Testosterone on Cognitive Function and Health Perception in Older Men With Low Bioavailable Testosterone Levels
  作者：A. M. Kenny、S. Bellantonio、C. A. Gruman、R. D. Acosta、K. M. Prestwood

  DOI：10.1093/gerona/57.5.m321

  日期：2002.5.1

  Background. Many men older than 50 years have bioavailable testosterone levels below the reference range for young adult men. The impact of the decreased androgen levels oil cognition and health perception has received little attention.Methods. Sixty-seven men (mean age 76 +/- 4 years, range 65-87) with bioavailable testosterone levels below 128 ng/dl (lower limit for adult normal range) were randomized to receive transdermal testosterone (2-2.5 mg patches/d) or placebo patches for I year. All men received 500 mg Supplemental calcium and 400 IU vitamin D. Outcome measures included sex hormones [testosterone, bioavailable testosterone, sex hormone binding globulin (SHBG), estradiol, and estrone], cognitive tests, (Digit Symbol, Digit Span, Trailmaking A and B), health perception (Medical Outcome Survey Short-form 36 or SF-36), lower extremity muscle strength and power. and calcium intake.Results. Twenty-three men (34%) withdrew from the Study; 44 men completed the trial. Bioavailable testosterone levels increased from 93 +/- 34 (SD) to 162 +/- 100 ng/dl (p < .002) at 12 months in the testosterone group (n = 24) while no change occurred in the control group (n 20). While there was no change in estradiol levels in either group, estrone levels increased in the testosterone group (28 +/- 7 to 32 +/- 9 pg/dl, p = .017). Scores oil the Digit Symbol test improved in both the testosterone and placebo groups. Scores on Trailmaking B improved in men treated with testosterone (p < .005), although the changes were not statistically different from the changes seen in the placebo group. Twelve-month scores on Trailmaking B for the entire group were correlated with 12-month testosterone levels (p = .016). Scores for health perception measured by SF-36 did not change significantly, though scores of mental and general health declined in both groups during the 12-month intervention. Twelve-month bioavailable testosterone scores were directly correlated with scores for physical role (p = .022), vitality (p = .036), and the physical composite score (p = .010).Conclusions. Transdermal testosterone treatment in men with low bioavailable testosterone levels does not impair and may improve cognitive function. Treatment did not improve health perception but this may have been due to the side effects of skin irritation suggested by similar reactions in both the testosterone and placebo groups.